KR20110000323A - Pharmaceutical and health food composition for preventing and treating diabetes mellitus comprising fruit extracts of chaenomeles sinensis as effective component - Google Patents
Pharmaceutical and health food composition for preventing and treating diabetes mellitus comprising fruit extracts of chaenomeles sinensis as effective component Download PDFInfo
- Publication number
- KR20110000323A KR20110000323A KR1020090057764A KR20090057764A KR20110000323A KR 20110000323 A KR20110000323 A KR 20110000323A KR 1020090057764 A KR1020090057764 A KR 1020090057764A KR 20090057764 A KR20090057764 A KR 20090057764A KR 20110000323 A KR20110000323 A KR 20110000323A
- Authority
- KR
- South Korea
- Prior art keywords
- extract
- fruit
- diabetes
- pharmaceutical composition
- extraction
- Prior art date
Links
- 235000017831 Pseudocydonia sinensis Nutrition 0.000 title claims abstract description 35
- 206010012601 diabetes mellitus Diseases 0.000 title claims abstract description 35
- 241001507760 Chaenomeles sinensis Species 0.000 title claims abstract 7
- 239000000203 mixture Substances 0.000 title abstract description 18
- 235000013402 health food Nutrition 0.000 title abstract 3
- 229940068517 fruit extracts Drugs 0.000 title 1
- 239000000284 extract Substances 0.000 claims abstract description 47
- 235000013399 edible fruits Nutrition 0.000 claims abstract description 39
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 23
- 239000002904 solvent Substances 0.000 claims abstract description 20
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 19
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 16
- 102000006995 beta-Glucosidase Human genes 0.000 claims abstract description 14
- 108010047754 beta-Glucosidase Proteins 0.000 claims abstract description 14
- 102100024295 Maltase-glucoamylase Human genes 0.000 claims abstract description 13
- 108010028144 alpha-Glucosidases Proteins 0.000 claims abstract description 13
- 239000004480 active ingredient Substances 0.000 claims abstract description 9
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 33
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims description 30
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims description 28
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 claims description 28
- 235000017788 Cydonia oblonga Nutrition 0.000 claims description 22
- 239000000843 powder Substances 0.000 claims description 13
- 238000000605 extraction Methods 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 10
- 230000002265 prevention Effects 0.000 claims description 9
- 230000036541 health Effects 0.000 claims description 8
- 235000013376 functional food Nutrition 0.000 claims description 4
- 239000012046 mixed solvent Substances 0.000 claims description 4
- 239000007864 aqueous solution Substances 0.000 claims description 3
- 238000001816 cooling Methods 0.000 claims description 3
- 238000004587 chromatography analysis Methods 0.000 claims description 2
- 238000000227 grinding Methods 0.000 claims description 2
- 230000006872 improvement Effects 0.000 claims description 2
- 238000010992 reflux Methods 0.000 claims description 2
- 238000000194 supercritical-fluid extraction Methods 0.000 claims description 2
- 238000002137 ultrasound extraction Methods 0.000 claims description 2
- 238000003809 water extraction Methods 0.000 claims 1
- 102000005840 alpha-Galactosidase Human genes 0.000 abstract description 11
- 108010030291 alpha-Galactosidase Proteins 0.000 abstract description 11
- 102000005936 beta-Galactosidase Human genes 0.000 abstract description 10
- 108010005774 beta-Galactosidase Proteins 0.000 abstract description 10
- 102000004190 Enzymes Human genes 0.000 abstract description 9
- 108090000790 Enzymes Proteins 0.000 abstract description 9
- 239000003814 drug Substances 0.000 abstract description 8
- 229940124597 therapeutic agent Drugs 0.000 abstract description 3
- 244000251905 Pseudocydonia sinensis Species 0.000 description 28
- 235000005078 Chaenomeles speciosa Nutrition 0.000 description 24
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 24
- 239000000287 crude extract Substances 0.000 description 15
- 238000002360 preparation method Methods 0.000 description 13
- 239000008363 phosphate buffer Substances 0.000 description 12
- 239000011541 reaction mixture Substances 0.000 description 12
- 239000000243 solution Substances 0.000 description 11
- 235000013361 beverage Nutrition 0.000 description 9
- 235000013305 food Nutrition 0.000 description 9
- 230000005764 inhibitory process Effects 0.000 description 9
- 229940069774 quince extract Drugs 0.000 description 9
- 241000196324 Embryophyta Species 0.000 description 8
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 8
- 239000000796 flavoring agent Substances 0.000 description 8
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- 239000012454 non-polar solvent Substances 0.000 description 8
- 238000009472 formulation Methods 0.000 description 7
- 239000004615 ingredient Substances 0.000 description 7
- 238000003556 assay Methods 0.000 description 6
- 230000002401 inhibitory effect Effects 0.000 description 6
- 239000000546 pharmaceutical excipient Substances 0.000 description 6
- 230000003178 anti-diabetic effect Effects 0.000 description 5
- 239000002775 capsule Substances 0.000 description 5
- 238000006243 chemical reaction Methods 0.000 description 5
- 235000019634 flavors Nutrition 0.000 description 5
- 239000003960 organic solvent Substances 0.000 description 5
- 239000002798 polar solvent Substances 0.000 description 5
- 239000003826 tablet Substances 0.000 description 5
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 4
- 238000002835 absorbance Methods 0.000 description 4
- 238000004458 analytical method Methods 0.000 description 4
- 239000000872 buffer Substances 0.000 description 4
- 150000001720 carbohydrates Chemical class 0.000 description 4
- 235000014633 carbohydrates Nutrition 0.000 description 4
- 238000007796 conventional method Methods 0.000 description 4
- 239000003085 diluting agent Substances 0.000 description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 230000007071 enzymatic hydrolysis Effects 0.000 description 4
- 238000006047 enzymatic hydrolysis reaction Methods 0.000 description 4
- 238000002474 experimental method Methods 0.000 description 4
- 238000002347 injection Methods 0.000 description 4
- 239000007924 injection Substances 0.000 description 4
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 4
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 239000008213 purified water Substances 0.000 description 4
- 229910000029 sodium carbonate Inorganic materials 0.000 description 4
- 239000011550 stock solution Substances 0.000 description 4
- 239000000758 substrate Substances 0.000 description 4
- 239000000725 suspension Substances 0.000 description 4
- BTJIUGUIPKRLHP-UHFFFAOYSA-N 4-nitrophenol Chemical compound OC1=CC=C([N+]([O-])=O)C=C1 BTJIUGUIPKRLHP-UHFFFAOYSA-N 0.000 description 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 3
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 3
- 229930195725 Mannitol Natural products 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 3
- 229930006000 Sucrose Natural products 0.000 description 3
- 150000001298 alcohols Chemical class 0.000 description 3
- -1 and the like Substances 0.000 description 3
- 239000003472 antidiabetic agent Substances 0.000 description 3
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 235000015872 dietary supplement Nutrition 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 239000012153 distilled water Substances 0.000 description 3
- 239000000839 emulsion Substances 0.000 description 3
- 235000013355 food flavoring agent Nutrition 0.000 description 3
- 241000411851 herbal medicine Species 0.000 description 3
- 239000003112 inhibitor Substances 0.000 description 3
- 239000008101 lactose Substances 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 239000000594 mannitol Substances 0.000 description 3
- 235000010355 mannitol Nutrition 0.000 description 3
- 150000003839 salts Chemical class 0.000 description 3
- 239000005720 sucrose Substances 0.000 description 3
- 239000000829 suppository Substances 0.000 description 3
- 239000000454 talc Substances 0.000 description 3
- 229910052623 talc Inorganic materials 0.000 description 3
- 235000012222 talc Nutrition 0.000 description 3
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 2
- KUWPCJHYPSUOFW-YBXAARCKSA-N 2-nitrophenyl beta-D-galactoside Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1OC1=CC=CC=C1[N+]([O-])=O KUWPCJHYPSUOFW-YBXAARCKSA-N 0.000 description 2
- IFBHRQDFSNCLOZ-ZIQFBCGOSA-N 4-nitrophenyl alpha-D-glucoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC1=CC=C([N+]([O-])=O)C=C1 IFBHRQDFSNCLOZ-ZIQFBCGOSA-N 0.000 description 2
- IFBHRQDFSNCLOZ-RMPHRYRLSA-N 4-nitrophenyl beta-D-glucoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=CC=C([N+]([O-])=O)C=C1 IFBHRQDFSNCLOZ-RMPHRYRLSA-N 0.000 description 2
- IFBHRQDFSNCLOZ-IIRVCBMXSA-N 4-nitrophenyl-α-d-galactoside Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1OC1=CC=C([N+]([O-])=O)C=C1 IFBHRQDFSNCLOZ-IIRVCBMXSA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 2
- 239000004386 Erythritol Substances 0.000 description 2
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 description 2
- 108010010803 Gelatin Proteins 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- 102000004877 Insulin Human genes 0.000 description 2
- 108090001061 Insulin Proteins 0.000 description 2
- DFPAKSUCGFBDDF-UHFFFAOYSA-N Nicotinamide Chemical compound NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- 244000299461 Theobroma cacao Species 0.000 description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 2
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 2
- 235000010443 alginic acid Nutrition 0.000 description 2
- 229920000615 alginic acid Polymers 0.000 description 2
- 239000003125 aqueous solvent Substances 0.000 description 2
- 235000014121 butter Nutrition 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- 239000001913 cellulose Substances 0.000 description 2
- 235000010980 cellulose Nutrition 0.000 description 2
- 229920002678 cellulose Polymers 0.000 description 2
- 239000003153 chemical reaction reagent Substances 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 description 2
- 235000019414 erythritol Nutrition 0.000 description 2
- 229940009714 erythritol Drugs 0.000 description 2
- 239000000706 filtrate Substances 0.000 description 2
- 235000015203 fruit juice Nutrition 0.000 description 2
- 229920000159 gelatin Polymers 0.000 description 2
- 239000008273 gelatin Substances 0.000 description 2
- 235000019322 gelatine Nutrition 0.000 description 2
- 235000011852 gelatine desserts Nutrition 0.000 description 2
- 239000008103 glucose Substances 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- 239000012676 herbal extract Substances 0.000 description 2
- 229940125396 insulin Drugs 0.000 description 2
- 229940041476 lactose 100 mg Drugs 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 2
- 208000030159 metabolic disease Diseases 0.000 description 2
- 239000000401 methanolic extract Substances 0.000 description 2
- 235000013824 polyphenols Nutrition 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- HELXLJCILKEWJH-NCGAPWICSA-N rebaudioside A Chemical compound O([C@H]1[C@H](O)[C@@H](CO)O[C@H]([C@@H]1O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O HELXLJCILKEWJH-NCGAPWICSA-N 0.000 description 2
- 230000002829 reductive effect Effects 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000000600 sorbitol Substances 0.000 description 2
- 235000010356 sorbitol Nutrition 0.000 description 2
- 239000008107 starch Substances 0.000 description 2
- 235000019698 starch Nutrition 0.000 description 2
- 230000001954 sterilising effect Effects 0.000 description 2
- 238000004659 sterilization and disinfection Methods 0.000 description 2
- 239000006188 syrup Substances 0.000 description 2
- 235000020357 syrup Nutrition 0.000 description 2
- 235000013343 vitamin Nutrition 0.000 description 2
- 229930003231 vitamin Natural products 0.000 description 2
- 239000011782 vitamin Substances 0.000 description 2
- 229940088594 vitamin Drugs 0.000 description 2
- 239000000080 wetting agent Substances 0.000 description 2
- 239000000811 xylitol Substances 0.000 description 2
- 235000010447 xylitol Nutrition 0.000 description 2
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 2
- 229960002675 xylitol Drugs 0.000 description 2
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 description 1
- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 description 1
- IQUPABOKLQSFBK-UHFFFAOYSA-N 2-nitrophenol Chemical compound OC1=CC=CC=C1[N+]([O-])=O IQUPABOKLQSFBK-UHFFFAOYSA-N 0.000 description 1
- FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 description 1
- 244000144725 Amygdalus communis Species 0.000 description 1
- 108010011485 Aspartame Proteins 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 101100283604 Caenorhabditis elegans pigk-1 gene Proteins 0.000 description 1
- PTHCMJGKKRQCBF-UHFFFAOYSA-N Cellulose, microcrystalline Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC)C(CO)O1 PTHCMJGKKRQCBF-UHFFFAOYSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
- 208000017667 Chronic Disease Diseases 0.000 description 1
- 235000005979 Citrus limon Nutrition 0.000 description 1
- 244000131522 Citrus pyriformis Species 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- 229920000858 Cyclodextrin Polymers 0.000 description 1
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 208000002249 Diabetes Complications Diseases 0.000 description 1
- LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 description 1
- 241000588724 Escherichia coli Species 0.000 description 1
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 1
- 239000001512 FEMA 4601 Substances 0.000 description 1
- DKKCQDROTDCQOR-UHFFFAOYSA-L Ferrous lactate Chemical compound [Fe+2].CC(O)C([O-])=O.CC(O)C([O-])=O DKKCQDROTDCQOR-UHFFFAOYSA-L 0.000 description 1
- 239000004606 Fillers/Extenders Substances 0.000 description 1
- 229930091371 Fructose Natural products 0.000 description 1
- 239000005715 Fructose Substances 0.000 description 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 1
- 102000005744 Glycoside Hydrolases Human genes 0.000 description 1
- 108010031186 Glycoside Hydrolases Proteins 0.000 description 1
- 239000004378 Glycyrrhizin Substances 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 240000007472 Leucaena leucocephala Species 0.000 description 1
- 235000010643 Leucaena leucocephala Nutrition 0.000 description 1
- 208000015439 Lysosomal storage disease Diseases 0.000 description 1
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 208000008589 Obesity Diseases 0.000 description 1
- 229920002230 Pectic acid Polymers 0.000 description 1
- 201000007100 Pharyngitis Diseases 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 208000003251 Pruritus Diseases 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- HELXLJCILKEWJH-SEAGSNCFSA-N Rebaudioside A Natural products O=C(O[C@H]1[C@@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1)[C@@]1(C)[C@@H]2[C@](C)([C@H]3[C@@]4(CC(=C)[C@@](O[C@H]5[C@H](O[C@H]6[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O6)[C@@H](O[C@H]6[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O6)[C@H](O)[C@@H](CO)O5)(C4)CC3)CC2)CCC1 HELXLJCILKEWJH-SEAGSNCFSA-N 0.000 description 1
- AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 description 1
- 235000004789 Rosa xanthina Nutrition 0.000 description 1
- 241000220222 Rosaceae Species 0.000 description 1
- 240000004808 Saccharomyces cerevisiae Species 0.000 description 1
- 235000014680 Saccharomyces cerevisiae Nutrition 0.000 description 1
- 241000533293 Sesbania emerus Species 0.000 description 1
- 244000228451 Stevia rebaudiana Species 0.000 description 1
- 241000193996 Streptococcus pyogenes Species 0.000 description 1
- 235000005764 Theobroma cacao ssp. cacao Nutrition 0.000 description 1
- 235000005767 Theobroma cacao ssp. sphaerocarpum Nutrition 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- FPIPGXGPPPQFEQ-BOOMUCAASA-N Vitamin A Natural products OC/C=C(/C)\C=C\C=C(\C)/C=C/C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-BOOMUCAASA-N 0.000 description 1
- 229930003268 Vitamin C Natural products 0.000 description 1
- 229930003427 Vitamin E Natural products 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000002730 additional effect Effects 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- 229940072056 alginate Drugs 0.000 description 1
- 239000000783 alginic acid Substances 0.000 description 1
- 229960001126 alginic acid Drugs 0.000 description 1
- 150000004781 alginic acids Chemical class 0.000 description 1
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 description 1
- 235000020224 almond Nutrition 0.000 description 1
- 239000003708 ampul Substances 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 230000002587 anti-hemolytic effect Effects 0.000 description 1
- 230000000767 anti-ulcer Effects 0.000 description 1
- 230000000840 anti-viral effect Effects 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- 239000000605 aspartame Substances 0.000 description 1
- 235000010357 aspartame Nutrition 0.000 description 1
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 1
- 229960003438 aspartame Drugs 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 230000003851 biochemical process Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 244000309464 bull Species 0.000 description 1
- 239000002034 butanolic fraction Substances 0.000 description 1
- 235000001046 cacaotero Nutrition 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 239000001506 calcium phosphate Substances 0.000 description 1
- 229910000389 calcium phosphate Inorganic materials 0.000 description 1
- 235000011010 calcium phosphates Nutrition 0.000 description 1
- 239000000378 calcium silicate Substances 0.000 description 1
- 229910052918 calcium silicate Inorganic materials 0.000 description 1
- 235000012241 calcium silicate Nutrition 0.000 description 1
- OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 230000023852 carbohydrate metabolic process Effects 0.000 description 1
- 239000001569 carbon dioxide Substances 0.000 description 1
- 229910002092 carbon dioxide Inorganic materials 0.000 description 1
- 235000014171 carbonated beverage Nutrition 0.000 description 1
- 235000013351 cheese Nutrition 0.000 description 1
- 235000019219 chocolate Nutrition 0.000 description 1
- 238000004040 coloring Methods 0.000 description 1
- 238000013329 compounding Methods 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 238000005520 cutting process Methods 0.000 description 1
- 230000034994 death Effects 0.000 description 1
- 231100000517 death Toxicity 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 150000002016 disaccharides Chemical class 0.000 description 1
- 231100000676 disease causative agent Toxicity 0.000 description 1
- 208000016097 disease of metabolism Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 229920001971 elastomer Polymers 0.000 description 1
- 239000003792 electrolyte Substances 0.000 description 1
- HELXLJCILKEWJH-UHFFFAOYSA-N entered according to Sigma 01432 Natural products C1CC2C3(C)CCCC(C)(C(=O)OC4C(C(O)C(O)C(CO)O4)O)C3CCC2(C2)CC(=C)C21OC(C1OC2C(C(O)C(O)C(CO)O2)O)OC(CO)C(O)C1OC1OC(CO)C(O)C(O)C1O HELXLJCILKEWJH-UHFFFAOYSA-N 0.000 description 1
- 238000009585 enzyme analysis Methods 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 239000000469 ethanolic extract Substances 0.000 description 1
- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 description 1
- 229940093471 ethyl oleate Drugs 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 239000004744 fabric Substances 0.000 description 1
- 239000004225 ferrous lactate Substances 0.000 description 1
- 235000013925 ferrous lactate Nutrition 0.000 description 1
- 229940037907 ferrous lactate Drugs 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 238000005194 fractionation Methods 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 235000020510 functional beverage Nutrition 0.000 description 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 239000003316 glycosidase inhibitor Substances 0.000 description 1
- LPLVUJXQOOQHMX-UHFFFAOYSA-N glycyrrhetinic acid glycoside Natural products C1CC(C2C(C3(CCC4(C)CCC(C)(CC4C3=CC2=O)C(O)=O)C)(C)CC2)(C)C2C(C)(C)C1OC1OC(C(O)=O)C(O)C(O)C1OC1OC(C(O)=O)C(O)C(O)C1O LPLVUJXQOOQHMX-UHFFFAOYSA-N 0.000 description 1
- 229960004949 glycyrrhizic acid Drugs 0.000 description 1
- UYRUBYNTXSDKQT-UHFFFAOYSA-N glycyrrhizic acid Natural products CC1(C)C(CCC2(C)C1CCC3(C)C2C(=O)C=C4C5CC(C)(CCC5(C)CCC34C)C(=O)O)OC6OC(C(O)C(O)C6OC7OC(O)C(O)C(O)C7C(=O)O)C(=O)O UYRUBYNTXSDKQT-UHFFFAOYSA-N 0.000 description 1
- 235000019410 glycyrrhizin Nutrition 0.000 description 1
- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 0.000 description 1
- 230000013632 homeostatic process Effects 0.000 description 1
- 201000001421 hyperglycemia Diseases 0.000 description 1
- 229940126904 hypoglycaemic agent Drugs 0.000 description 1
- 230000002218 hypoglycaemic effect Effects 0.000 description 1
- 206010022000 influenza Diseases 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 238000000185 intracerebroventricular administration Methods 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- VMPHSYLJUKZBJJ-UHFFFAOYSA-N lauric acid triglyceride Natural products CCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCC)COC(=O)CCCCCCCCCCC VMPHSYLJUKZBJJ-UHFFFAOYSA-N 0.000 description 1
- 230000037356 lipid metabolism Effects 0.000 description 1
- 229940057995 liquid paraffin Drugs 0.000 description 1
- 244000144972 livestock Species 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 229960003511 macrogol Drugs 0.000 description 1
- 239000000845 maltitol Substances 0.000 description 1
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 description 1
- 235000010449 maltitol Nutrition 0.000 description 1
- 229940035436 maltitol Drugs 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 description 1
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 235000010755 mineral Nutrition 0.000 description 1
- 239000002480 mineral oil Substances 0.000 description 1
- 235000010446 mineral oil Nutrition 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 150000002772 monosaccharides Chemical class 0.000 description 1
- 230000003472 neutralizing effect Effects 0.000 description 1
- 235000005152 nicotinamide Nutrition 0.000 description 1
- 239000011570 nicotinamide Substances 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 235000015097 nutrients Nutrition 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- LCLHHZYHLXDRQG-ZNKJPWOQSA-N pectic acid Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)O[C@H](C(O)=O)[C@@H]1OC1[C@H](O)[C@@H](O)[C@@H](OC2[C@@H]([C@@H](O)[C@@H](O)[C@H](O2)C(O)=O)O)[C@@H](C(O)=O)O1 LCLHHZYHLXDRQG-ZNKJPWOQSA-N 0.000 description 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol group Chemical group C1(=CC=CC=C1)O ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 1
- 235000017807 phytochemicals Nutrition 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000004069 plant analysis Substances 0.000 description 1
- 239000000419 plant extract Substances 0.000 description 1
- 229930000223 plant secondary metabolite Natural products 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 239000010318 polygalacturonic acid Substances 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 150000004804 polysaccharides Chemical class 0.000 description 1
- 229920000136 polysorbate Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 1
- 229960003415 propylparaben Drugs 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
- 235000019203 rebaudioside A Nutrition 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 235000019204 saccharin Nutrition 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 229940081974 saccharin Drugs 0.000 description 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229960002920 sorbitol Drugs 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 238000007619 statistical method Methods 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000005846 sugar alcohols Chemical class 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 235000013616 tea Nutrition 0.000 description 1
- JZRWCGZRTZMZEH-UHFFFAOYSA-N thiamine Chemical compound CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N JZRWCGZRTZMZEH-UHFFFAOYSA-N 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 206010044008 tonsillitis Diseases 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
- 238000003828 vacuum filtration Methods 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
- 235000019155 vitamin A Nutrition 0.000 description 1
- 239000011719 vitamin A Substances 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 229940045997 vitamin a Drugs 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 239000011787 zinc oxide Substances 0.000 description 1
Images
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/73—Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
- A61K36/732—Chaenomeles, e.g. flowering quince
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2200/00—Function of food ingredients
- A23V2200/30—Foods, ingredients or supplements having a functional effect on health
- A23V2200/328—Foods, ingredients or supplements having a functional effect on health having effect on glycaemic control and diabetes
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2250/00—Food ingredients
- A23V2250/20—Natural extracts
- A23V2250/21—Plant extracts
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/10—Preparation or pretreatment of starting material
- A61K2236/15—Preparation or pretreatment of starting material involving mechanical treatment, e.g. chopping up, cutting or grinding
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/37—Extraction at elevated pressure or temperature, e.g. pressurized solvent extraction [PSE], supercritical carbon dioxide extraction or subcritical water extraction
Abstract
Description
본 발명은 모과 열매 추출물을 유효성분으로 함유하는 당뇨병의 예방 및 치료용 약학 조성물 및 건강기능식품에 관한 것이다.The present invention relates to a pharmaceutical composition for preventing and treating diabetes and a health functional food containing the Chinese quince fruit extract as an active ingredient.
당뇨병 (DM)은 탄수화물 및 지질 대사의 항상성이 부적절하게 조절되어 혈중 글루코스가 증가하여 생기는 생명을 위협하는 주요한 만성 질환이다. DM은 환자의 건강과 삶의 질과 수명 및 헬스 케어 시스템에 현저한 영향을 주는 심각한 대사 질환이다. WHO에 따르면, 현재 전 세계적으로 적어도 1억 7천만명이 당뇨병을 앓고 있으며, 2030년에는 이 숫자가 두배 이상으로 증가할 예측되며, 매년 대략 320만명이 당뇨 합병증으로 사망한다; 분당 6명의 사망자 (WHO, 2007. www.who.int/dietphysicalactivity/publications/facts/diabetes/en/).Diabetes mellitus (DM) is a life-threatening major chronic disease caused by improperly regulated homeostasis of carbohydrate and lipid metabolism resulting in increased blood glucose. DM is a serious metabolic disease that has a significant impact on the patient's health, quality of life and longevity, and the healthcare system. According to the WHO, at least 170 million people worldwide now have diabetes, and this number is expected to more than double in 2030, with approximately 3.2 million people dying from diabetes complications each year; 6 deaths per minute (WHO, 2007. www.who.int/dietphysicalactivity/publications/facts/diabetes/en/).
당뇨병에는 인슐린 의존성 (I형) 및 인슐린 비의존성 (II형)이 있으며 그 중에서, II형이 더욱 빈번한 형태이며, 비만의 증가 및 노령화 따라 당뇨병의 발병 빈도도 증가되고 있다 (Kim et al. 2004. Carbohydr. Res., 339: 715-717). 최근에, 생약을 이용한 DM 치료에 관심이 고조되었는데, 이는 생약은 일반적으로 비독성이며, 또한 저개발국에서 안전한 현대 약물이 부족한 상황에서 WHO가 전통식물을 이용한 치료 방법을 추천했기 때문이다. 저혈당 특성을 갖는 식물 유도체가 매우 오랜 옛날부터 토속 약물로서 이용되어 왔다 (Yeh et al. 2003. Diabetes Care, 26: 1277-1294). 천연 및 합성 혈당강하제의 도입에도 불구하고, 당뇨병 및 이의 이차 합병증은 사람들에게 주요한 의학적인 문제가 되어 왔다 (Ravi et al. 2005. Food Chem. Toxicol., 43: 1433-1439). 이제까지 전통적으로 고혈당의 치료에 사용되던 약용 식물은 그 식물의 여러 다른 부위가 당뇨병 치료 활성이 함유된 것으로 인지되어 있어서 이로부터 당뇨병 치료제를 개발하려는 연구가 아주 활발하게 진행되어서 몇 가지 당뇨병 치료제가 이로부터 개발되었고 또 지금도 계속적으로 새로운 식물을 대상으로 당뇨병 치료약 및 예방약 탐색되어 개발되는 중이다. Diabetes mellitus has insulin dependency (type I) and insulin independent (type II), of which type II is the more frequent form, and the incidence of diabetes increases with the increase in obesity and aging (Kim et al. 2004. Carbohydr.Res., 339: 715-717). In recent years, there has been a growing interest in the treatment of DM with herbal medicines, because herbal medicines are generally non-toxic, and WHO has recommended treatment with traditional plants in the absence of safe modern drugs in underdeveloped countries. Plant derivatives with hypoglycemic properties have long been used as indigenous drugs (Yeh et al. 2003. Diabetes Care, 26: 1277-1294). Despite the introduction of natural and synthetic hypoglycemic agents, diabetes mellitus and its secondary complications have been a major medical problem for people (Ravi et al. 2005. Food Chem. Toxicol., 43: 1433-1439). Medicinal plants, which have traditionally been used for the treatment of hyperglycemia, have been recognized that different parts of the plant contain anti-diabetic activity, and research on the development of anti-diabetics is very active. It has been developed and is still being searched and developed for anti-diabetic and preventive drugs targeting new plants.
본 발명에서, 한국 약용식물 추출물이 다양한 효소 (예를 들면, α-글루코시다아제, β-글루코시다아제, α-갈락토시다아제 및 β-갈락토시다아제)에 미치는 영향을 조사하였는데, 이는 상기 효소들이 대사 질환 및 당뇨병 같은 질환, 바이러스성 또는 세균성 감염, 리소솜 축적 질환(lysosomal storage disorder) 및 암에 관련된 다양한 생화학적 과정에 관련되기 때문이다. 그럼으로, 더욱 우수한 글리코시다아제 저해제를 탐색하기 위한 연구과 오랜 동안 진행되어 그 결과 모과가 우수한 저해제를 함유한 식물로 선별되어 모과의 추가적인 특성을 조사하였다. (Naumov, D., 2004. Mol. Biol. (Mosk), 38: 388-399). In the present invention, the effects of Korean medicinal plant extracts on various enzymes (eg, α-glucosidase, β-glucosidase, α-galactosidase and β-galactosidase) were investigated. The enzymes are involved in various biochemical processes related to metabolic diseases and diseases such as diabetes, viral or bacterial infections, lysosomal storage disorders and cancer. Thus, research has been underway for a long time to search for better glycosidase inhibitors, and as a result, the Chinese quince was selected as a plant containing an excellent inhibitor to investigate the additional properties of the quince. (Naumov, D., 2004. Mol. Biol. (Mosk), 38: 388-399).
장미과 (Rosaceae family)에 속하는 식물인 모과 (Chaenomeles sinensis (Thouin) Koehne)(또한, Pseudocydonia sinensis (Thouin) CK Schneid로도 불리며, 일반명은 Chinese-quince, ma gua 임)는 주로 한국, 중국 및 일본에 분포한다. 그 열매는 많은 양의 페놀화합물(phenolics)을 가진 것으로 나타났다. 이러한 높은 페놀화합물 함량은 건강 개선 인자로서 작용할 것으로 예상될 수 있다 (Hamauzu et al. 2006. J. Agric. Food Chem., 54: 765-772). 이의 열매는 목(throat) 질환을 치료하기 위한 전통적인 한약으로서 이용된다. 또한 이 열매에서 항인플루엔자, 항산화, 항궤양, 항바이러스, 항용혈, 항가려움 및 항세균 (편도염 및 인두염의 원인 물질인 스트렙토코커스 파이로젠(Streptococcus pyogenes)에 대한) 활성이 보고되었다 (Hamauzu et al. 2006. J. Agric. Food Chem., 54: 765-772). Chaenomeles sinensis (Thouin) Koehne (also called Pseudocydonia sinensis (Thouin) CK Schneid), a plant belonging to the Rosaceae family, is commonly distributed in Korea, China, and Japan. do. The fruit appeared to have a large amount of phenolics. This high phenolic content can be expected to act as a health improving factor (Hamauzu et al. 2006. J. Agric. Food Chem., 54: 765-772). Its fruit is used as a traditional Chinese medicine to treat throat disorders. In addition, anti-influenza, antioxidant, anti-ulcer, antiviral, antihemolytic, anti-itch and antibacterial (to Streptococcus pyogenes , the causative agents of tonsillitis and pharyngitis) have been reported in this fruit (Hamauzu et al. 2006. J. Agric.Food Chem., 54: 765-772).
한국특허등록 제10-0540033호에는 모과 및 기타 성분을 유효성분으로 함유하는 관절염 치료용 생약 조성물 및 그 제조방법이 개시되어 있으며, 한국특허공개 제2006-0085731호에는 모과 추출물 및 기타 추출물을 포함하는 알코올 흡수 저해용 조성물이 개시되어 있다.Korean Patent Registration No. 10-0540033 discloses a herbal composition for treating arthritis containing a Chinese quince and other ingredients as an active ingredient, and a method of manufacturing the same. Korean Patent Publication No. 2006-0085731 includes Chinese quince extract and other extracts. Disclosed is a composition for inhibiting alcohol absorption.
본 발명은 상기와 같은 요구에 의해 안출된 것으로서, 지금까지 모과의 항당뇨 활성에 관해 논의된 이전의 특허가 없으므로, 본 발명에서는 글리코시다아제를 포함한 여러 효소의 저해 연구를 통해 모과의 조추출물 및 이의 다양한 분획의 항당뇨 가능성을 조사하여, 모과 열매 추출물을 상기 효소와 관련된 질병의 예방 및 치료제로 이용하고자 한다.The present invention has been made in accordance with the above requirements, and thus there is no previous patent discussed about antidiabetic activity of quince, so in the present invention, crude extracts of quince through study of inhibition of various enzymes including glycosidase and By investigating the antidiabetic potential of various fractions thereof, the Chinese quince fruit extract is intended to be used as a prophylactic and therapeutic agent for diseases related to the enzyme.
상기 과제를 해결하기 위해, 본 발명은 모과 열매 추출물을 유효성분으로 함유하는 당뇨병의 예방 및 치료용 약학 조성물을 제공한다.In order to solve the above problems, the present invention provides a pharmaceutical composition for the prevention and treatment of diabetes mellitus containing quince fruit extract as an active ingredient.
또한, 본 발명은 상기 추출물을 유효성분으로 함유하는 당뇨병 예방 및 개선용 건강기능식품을 제공한다.The present invention also provides a dietary supplement for preventing and improving diabetes containing the extract as an active ingredient.
본 발명에 따르면, 본 발명의 모과 열매 추출물은 α-글루코시다아제, β-글루코시다아제, α-갈락토시다아제 및 β-갈락토시다아제를 저해하였다. 따라서, 모과 열매 추출물은 상기 효소와 관련된 당뇨병의 증상 완화제나 치료제로 사용될 수 있다.According to the present invention, the Chinese quince fruit extract of the present invention inhibited α-glucosidase, β-glucosidase, α-galactosidase and β-galactosidase. Thus, the Chinese quince fruit extract can be used as a symptomatic or therapeutic agent for diabetes related to the enzyme.
본 발명의 목적을 달성하기 위하여, 본 발명은 모과 (Chaenomeles sinensis) 열매의 용매 추출물을 유효성분으로 함유하는 당뇨병의 예방 및 치료용 약학 조성 물을 제공한다.In order to achieve the object of the present invention, the present invention provides a pharmaceutical composition for the prevention and treatment of diabetes mellitus containing a solvent extract of the fruit of Chaenomeles sinensis .
본 발명의 약학 조성물에서, 상기 용매는 물과 메탄올, 에탄올, 부탄올 등과 같은 C1 내지 C4의 저급 알콜과 이들의 혼합용매 등을 포함한 다양한 유기용매일 수 있다.In the pharmaceutical composition of the present invention, the solvent may be various organic solvents including water, C1 to C4 lower alcohols such as methanol, ethanol, butanol, and the like, mixed solvents thereof, and the like.
본 발명의 약학 조성물에서, 상기 용매 추출물을 물과 부탄올, 에틸 아세테이트, 헥산, 또는 메틸렌 클로라이드 등을 포함하는 다양한 비극성 용매를 이용하여 얻은 가용 분획이나 그 후 여러 가지 크로마토그래피 기술을 사용하여 얻은 더 높은 순도의 분획이 α-글루코시다아제를 저해할 수 있으며, 상기 용매 추출물의 물 가용 분획이 β-글루코시다아제를 저해할 수 있다.In the pharmaceutical composition of the present invention, the solvent extract is obtained by soluble fraction obtained using various nonpolar solvents including water and butanol, ethyl acetate, hexane, methylene chloride and the like, or higher obtained using various chromatographic techniques. Fractions of purity can inhibit α-glucosidase and water soluble fractions of the solvent extracts can inhibit β-glucosidase.
본 발명은 또한, 모과 (Chaenomeles sinensis) 열매의 용매 추출물을 유효성분으로 함유하는 당뇨병 예방 및 개선용 건강기능식품을 제공한다.The present invention also provides a dietary supplement for preventing and improving diabetes containing a solvent extract of Chaenomeles sinensis fruit as an active ingredient.
이하, 본 발명을 더욱 상세히 설명한다.Hereinafter, the present invention will be described in more detail.
상기 모과 열매 조추출물은 물과 메탄올, 에탄올, 부탄올 등과 같은 C1 내지 C4의 저급 알콜과 이들의 혼합용매 및 이외에도 다양한 유기용매에, 바람직하게는 메탄올에 가용한 추출물을 포함한다.The crude extract of Chinese quince comprises water and C1 to C4 lower alcohols such as methanol, ethanol, butanol and the like, mixed solvents thereof, and various organic solvents, preferably extracts available in methanol.
또한, 상기 모과 열매 비극성 용매 가용 분획은 헥산, 클로로포름, 메틸렌클로라이드 또는 에틸아세테이트를 포함한 다양한 비극성 용매에 가용한 분획을 포함한다.In addition, the quince fruit nonpolar solvent soluble fraction includes fractions soluble in various nonpolar solvents including hexane, chloroform, methylene chloride or ethyl acetate.
또한, 상기 모과 열매 극성 용매 가용 분획은 아세톤, 부탄올, 에탄올, 메탄 올 또는 물을 포함한 다양한 극성용매, 바람직하게는 부탄올로 추출한 것을 포함한다.In addition, the quince fruit polar solvent soluble fraction includes those extracted with various polar solvents, preferably butanol, including acetone, butanol, ethanol, methanol or water.
본 발명의 모과 열매 조추출물, 비극성 용매 가용 분획 및 극성 용매 가용 분획은 예를 들면 모과의 어린 열매(건조된 것 혹은 생 것)와 성숙한 열매(건조된 것 혹은 생 것) 등을 포함한 전단계의 열매를 이용하여 하기와 같이 수득될 수 있다.The quince fruit crude extract, nonpolar solvent soluble fraction and polar solvent soluble fraction of the present invention are fruits of the previous stage including, for example, young fruits (dried or raw) and mature fruits (dried or raw) of quince. Can be obtained as follows.
본 발명의 모과 열매를 통째로 혹은 작은 조각으로 썰거나 혹은 마쇄기로 갈아 미세분말화한 후, 모과 열매 중량의 0.1배에서 50 배 사이의 부피의 물 및 메탄올, 에탄올, 부탄올 등과 같은 C1 내지 C4의 저급알콜 또는 이들의 약 1:0.1 내지 1:10의 혼합비를 갖는 혼합용매 및 이외에도 다양한 유기용매로, 바람직하게는 메탄올로 약 5 내지 80 ℃, 바람직하게는 약 24 ℃에서 약 2개월간 열수 추출, 냉침 추출, 환류 냉각 추출, 초음파 추출, 초임계 추출 등을 포함한 다양한 추출방법들을 사용하여 추출한 후, 진공여과에 의해 여과액을 회수한 다음, 상기의 과정을 1 내지 5회, 바람직하게는 2회 반복 수행하여 여과액을 모으고 감압농축하여 모과 열매 조추출물을 수득할 수 있다.After cutting the quince fruit of the present invention as a whole or in small pieces or grinding into a crusher, and finely powdered, the volume of water between 0.1 and 50 times the weight of the quince fruit and lower levels of C1 to C4 such as methanol, ethanol, butanol, etc. Hydrothermal extraction, cooling with alcohol or a mixed solvent having a mixing ratio of about 1: 0.1 to 1:10 and other organic solvents, preferably about 5 to 80 ° C., preferably about 24 ° C., for about 2 months with various organic solvents. After extraction using various extraction methods including extraction, reflux cooling extraction, ultrasonic extraction, supercritical extraction, etc., the filtrate is recovered by vacuum filtration, and the above procedure is repeated 1 to 5 times, preferably 2 times. The filtrate was collected and concentrated under reduced pressure to obtain a crude extract of Chinese quince.
또한, 본 발명의 모과 열매 비극성 용매 가용 분획은 상기의 모과 열매 조추출물을 증류수에 현탁한 후, 이들 현탁액의 약 1 내지 100배, 바람직하게는 약 1 내지 55배 부피의 헥산, 에틸아세테이트, 메틸렌 클로라이드, 클로로포름, 부탄올 등을 포함한 다양한 비극성 용매를 가하여 1회 내지 10회, 바람직하게는 2회 내지 5회 비극성용매 가용층을 추출, 분리하여 수득할 수 있다. 또한 추가로 통상의 분 획 공정을 수행할 수도 있다(Harborne J.B. Phytochemical methods: A guide to modern techniques of plant analysis, 3rd Ed., pp6-7, 1998).In addition, the quince fruit nonpolar solvent soluble fraction of the present invention is prepared by suspending the crude fruit extract of the quince in distilled water, and then, about 1 to 100 times the volume of these suspensions, preferably about 1 to 55 times the volume of hexane, ethyl acetate, and methylene. Various nonpolar solvents including chloride, chloroform, butanol and the like can be added to extract and separate the soluble layers of the nonpolar solvent from 1 to 10 times, preferably from 2 to 5 times. In addition, conventional fractionation processes can also be performed (Harborne J. B. Phytochemical methods: A guide to modern techniques of plant analysis, 3rd Ed., Pp 6-7, 1998).
더욱 바람직하게는 상기 공정으로 수득된 모과 열매 조추출물, 바람직하게는 모과 열매 메탄올 추출물을 물에 녹인 후 그 수용액과 n-부탄올, 에틸아세테이트, 메틸렌클로라이드, 헥산 등을 포함한 다양한 유기용매를 극성이 낮은 용매부터 극성이 높은 용매순으로 순차적으로 혼합한 후, 바람직하게는 헥산, 메틸렌클로라이드, 에틸아세테이트, n-부탄올, 물의 순으로 순차적으로 용매분획한 후, 감압농축하여 모과 열매 헥산, 에틸아세테이트, 메틸렌 클로라이드, n-부탄올 분획물을 수득할 수 있다.More preferably, the crude Chinese quince extract obtained by the above process, preferably the Chinese quince fruit methanol extract is dissolved in water, and then the aqueous solution and various organic solvents including n-butanol, ethyl acetate, methylene chloride, hexane, etc. have low polarity. After sequentially mixing the solvent in the order of high polar solvent, preferably hexane, methylene chloride, ethyl acetate, n-butanol, water and then sequentially fractionated the solvent, concentrated under reduced pressure and concentrated quince fruit hexane, ethyl acetate, methylene Chloride, n-butanol fractions can be obtained.
본 발명은 상기의 제법으로 얻어진 모과 열매 조추출물, 비극성 용매 가용 분획 및 극성 용매 가용 분획을 유효성분으로 함유하는 당뇨병의 예방 및 치료용 약학 조성물을 제공한다. 상기 당뇨병은 바람직하게는 II형 당뇨병일 수 있다.The present invention provides a pharmaceutical composition for the prevention and treatment of diabetes mellitus containing the crude extract of Chinese quince, the nonpolar solvent soluble fraction and the polar solvent soluble fraction obtained as the active ingredient. The diabetes may preferably be type II diabetes.
또한, 모과 열매는 오랫동안 생약으로 사용되어 오던 약재로서 이로부터 추출된 본 발명의 추출물들 역시 독성 및 부작용 등의 문제가 없다.In addition, the Chinese quince has been used as a herbal medicine for a long time, the extracts of the present invention extracted therefrom also have no problems such as toxicity and side effects.
상기와 같은 방법으로 얻어진 모과 열매 메탄올 추출물 및 각 용매 분획물이 α-글루코시다아제, β-글루코시다아제, α-갈락토시다아제 및 β-갈락토시다아제를 저해함을 확인할 수 있었다.It was confirmed that the quince fruit methanol extract and each solvent fraction obtained by the above method inhibited α-glucosidase, β-glucosidase, α-galactosidase and β-galactosidase.
본 발명의 당뇨병의 예방 및 치료용 약학 조성물은, 조성물 총 중량에 대하여 상기 추출물을 0.02 내지 50 중량%로 포함할 수 있다.The pharmaceutical composition for preventing and treating diabetes of the present invention may include 0.02 to 50% by weight of the extract based on the total weight of the composition.
본 발명의 추출물을 포함하는 약학조성물은 약학적 조성물의 제조에 통상적 으로 사용하는 적절한 담체, 부형제 및 희석제를 더 포함할 수 있다.Pharmaceutical compositions comprising the extract of the present invention may further comprise suitable carriers, excipients and diluents commonly used in the manufacture of pharmaceutical compositions.
본 발명의 추출물의 약학적 투여 형태는 이들의 약학적 허용 가능한 염의 형태로도 사용될 수 있고, 또한 단독으로 또는 타 약학적 활성 화합물과 결합뿐만 아니라 적당한 집합으로 사용될 수 있다.The pharmaceutical dosage forms of the extracts of the present invention may be used in the form of their pharmaceutically acceptable salts, and may be used alone or in combination with other pharmaceutically active compounds as well as in a suitable collection.
본 발명에 따른 추출물을 포함하는 약학조성물은, 각각 통상의 방법에 따라 산제, 과립제, 정제, 캡슐제, 현탁액, 에멀젼, 시럽, 에어로졸 등의 경구형 제형, 외용제, 좌제 및 멸균 주사용액의 형태로 제형화하여 사용될 수 있다. 추출물을 포함하는 조성물에 포함될 수 있는 담체, 부형제 및 희석제로는 락토즈, 덱스트로즈, 수크로스, 솔비톨, 만니톨, 자일리톨, 에리스리톨, 말티톨, 전분, 아카시아 고무, 알지네이트, 젤라틴, 칼슘 포스페이트, 칼슘 실리케이트, 셀룰로즈, 메틸 셀룰로즈, 미정질 셀룰로스, 폴리비닐 피롤리돈, 물, 메틸히드록시벤조에이트, 프로필히드록시벤조에이트, 탈크, 마그네슘 스테아레이트 및 광물유 등을 포함한 다양한 화합물 혹은 혼합물을 들 수 있다. 제제화할 경우에는 보통 사용하는 충진제, 증량제, 결합제, 습윤제, 붕해제, 계면활성제 등의 희석제 또는 부형제를 사용하여 조제된다. 경구투여를 위한 고형제제에는 정제, 환제, 산제, 과립제, 캡슐제 등이 포함되며, 이러한 고형제제는 상기 추출물에 적어도 하나 이상의 부형제 예를 들면, 전분, 칼슘카보네이트 (calcium carbonate), 수크로스(sucrose) 또는 락토오스(lactose), 젤라틴 등을 섞어 조제된다. 또한 단순한 부형제 이외에 마그네슘 스테아레이트, 탈크 같은 윤활제들도 사용된다. 경구를 위한 액상 제제로는 현탁제, 내용액제, 유제, 시럽제 등이 해당되는데 흔히 사용되는 단순 희석제인 물, 리퀴드 파라핀 이외에 여러 가지 부형제, 예를 들면 습윤제, 감미제, 방향제, 보존제 등이 포함될 수 있다. 비경구 투여를 위한 제제에는 멸균된 수용액, 비수성용제, 현탁제, 유제, 동결건조 제제, 좌제가 포함된다. 비수성용제, 현탁제로는 프로필렌글리콜(propylene glycol), 폴리에틸렌 글리콜, 올리브 오일과 같은 식물성 기름, 에틸올레이트와 같은 주사 가능한 에스테르 등이 사용될 수 있다. 좌제의 기제로는 위텝솔(witepsol), 마크로골, 트윈 (tween) 61, 카카오지, 라우린지, 글리세로제라틴 등이 사용될 수 있다.Pharmaceutical compositions comprising extracts according to the invention, in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols and the like, oral preparations, suppositories and sterile injectable solutions, respectively, according to conventional methods. Can be formulated and used. Carriers, excipients and diluents that may be included in the composition comprising the extract include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate And various compounds or mixtures including cellulose, methyl cellulose, microcrystalline cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, mineral oil and the like. When formulated, diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrating agents, and surfactants are usually used. Solid preparations for oral administration include tablets, pills, powders, granules, capsules and the like, and such solid preparations may include at least one excipient such as starch, calcium carbonate and sucrose in the extract. ) Or lactose, gelatin and the like are mixed. In addition to simple excipients, lubricants such as magnesium stearate and talc are also used. Oral liquid preparations include suspensions, solvents, emulsions, and syrups, and may include various excipients, such as wetting agents, sweeteners, fragrances, and preservatives, in addition to commonly used simple diluents such as water and liquid paraffin. . Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized preparations, suppositories. As the non-aqueous solvent and suspending agent, propylene glycol, polyethylene glycol, vegetable oil such as olive oil, injectable ester such as ethyl oleate and the like can be used. As the base of the suppository, witepsol, macrogol, tween 61, cacao butter, laurin butter, glycerogelatin and the like can be used.
본 발명의 추출물의 바람직한 투여량은 환자의 상태 및 체중, 질병의 정도, 약물형태, 투여경로 및 기간에 따라 다르지만, 당업자에 의해 적절하게 선택될 수 있다. 그러나, 바람직한 효과를 위해서, 본 발명의 추출물은 1일 0.0001 내지 100 mg/kg으로, 바람직하게는 0.001 내지 100 mg/kg으로 투여하는 것이 좋다. 투여는 하루에 한번 투여할 수도 있고, 수회 나누어 투여할 수도 있다. 상기 투여량은 어떠한 면으로든 본 발명의 범위을 한정하는 것은 아니다.Preferred dosages of the extracts of the present invention vary depending on the condition and weight of the patient, the extent of the disease, the form of the drug, the route of administration and the duration, and may be appropriately selected by those skilled in the art. However, for the desired effect, the extract of the present invention is preferably administered at 0.0001 to 100 mg / kg, preferably 0.001 to 100 mg / kg per day. Administration may be administered once a day or may be divided several times. The dosage does not limit the scope of the invention in any aspect.
본 발명의 추출물은 쥐, 생쥐, 가축, 인간 등의 포유동물에 다양한 경로로 투여될 수 있다. 투여의 모든 방식은 예상될 수 있는데, 예를 들면, 경구, 직장 또는 정맥, 근육, 피하, 자궁내 경막 또는 뇌혈관내 (intracerebroventricular) 주사에 의해 투여될 수 있다.The extract of the present invention can be administered to mammals such as rats, mice, livestock, humans and the like in various routes. All modes of administration can be expected, for example, by oral, rectal or intravenous, intramuscular, subcutaneous, intrauterine dural or intracerebroventricular injection.
또한, 본 발명은 당뇨병의 예방 및 개선 효과를 나타내는 상기 모과 열매 추출물 및 식품학적으로 허용 가능한 식품보조첨가제를 포함하는 건강기능식품을 제공한다. 상기 모과 열매 추출물은 바람직하게는 에탄올추출물 및 이산화탄소를 이 용한 초임계 추출물이다. 상기 추출물을 첨가할 수 있는 식품으로는, 예를 들어, 각종 식품류, 음료, 껌, 차, 비타민 복합제, 건강 기능성 식품류 등이 있다.In addition, the present invention provides a health functional food comprising the Chinese quince fruit extract and food acceptable food supplements exhibiting a prevention and improvement effect of diabetes. The Chinese quince fruit extract is preferably a supercritical extract using ethanol extract and carbon dioxide. Examples of the food to which the extract can be added include various foods, beverages, gums, teas, vitamin complexes, and health functional foods.
또한, 당뇨병의 예방 및 개선 효과를 목적으로 식품 또는 음료에 첨가될 수 있다. 이 때, 식품 또는 음료 중의 상기 추출물의 양은 전체 식품 중량의 0.01 내지 15 중량%로 가할 수 있으며, 건강 음료 조성물은 100 ㎖를 기준으로 0.02 내지 5 g, 바람직하게는 0.3 내지 1g의 비율로 가할 수 있다.It may also be added to foods or beverages for the purpose of preventing and improving diabetes. At this time, the amount of the extract in the food or beverage may be added in 0.01 to 15% by weight of the total food weight, the health beverage composition may be added in a ratio of 0.02 to 5 g, preferably 0.3 to 1g based on 100 ml. have.
본 발명의 건강 기능성 음료 조성물은 지시된 비율로 필수 성분으로서 상기 추출물을 함유하는 외에는 다른 성분에는 특별한 제한이 없으며 통상의 음료와 같이 여러 가지 향미제 또는 천연 탄수화물 등을 추가 성분으로서 함유할 수 있다. 상술한 천연 탄수화물의 예는 모노사카라이드, 예를 들어, 포도당, 과당 등; 디사카라이드, 예를 들어 말토스, 슈크로스 등; 및 폴리사카라이드, 예를 들어 덱스트린, 시클로덱스트린 등과 같은 통상적인 당, 및 자일리톨, 소르비톨, 에리트리톨 등의 당알콜이다. 상술한 것 이외의 향미제로서 천연 향미제(타우마틴, 스테비아 추출물, 예를 들어 레바우디오시드 A, 글리시르히진 등) 및 합성 향미제(사카린, 아스파르탐 등)를 유리하게 사용할 수 있다. 상기 천연 탄수화물의 비율은 본 발명의 조성물 100 ㎖당 일반적으로 약 1 내지 20 g, 바람직하게는 약 5 내지 12 g이다.The health functional beverage composition of the present invention has no particular limitation on the other ingredients other than the above-mentioned extract as an essential ingredient in the indicated ratio, and may contain various flavors or natural carbohydrates as an additional ingredient such as ordinary beverages. Examples of the above-mentioned natural carbohydrates include monosaccharides such as glucose, fructose and the like; Disaccharides such as maltose, sucrose and the like; And conventional sugars such as polysaccharides such as dextrin, cyclodextrin, and sugar alcohols such as xylitol, sorbitol, and erythritol. As flavoring agents other than those mentioned above, natural flavoring agents (tauumatin, stevia extract, for example, rebaudioside A, glycyrrhizin, etc.) and synthetic flavoring agents (saccharin, aspartame, etc.) can be advantageously used. . The proportion of such natural carbohydrates is generally about 1 to 20 g, preferably about 5 to 12 g per 100 ml of the composition of the present invention.
상기 외에 본 발명의 추출물은 여러 가지 영양제, 비타민, 광물(전해질), 합성 풍미제 및 천연 풍미제 등의 풍미제, 착색제 및 중진제(치즈, 초콜릿 등), 펙트산 및 그의 염, 알긴산 및 그의 염, 유기산, 보호성 콜로이드 증점제, pH 조절제, 안정화제, 방부제, 글리세린, 알콜, 탄산 음료에 사용되는 탄산화제 등을 함유할 수 있다. 그 밖에 본 발명의 추출물들은 천연 과일 쥬스 및 과일 쥬스 음료 및 야채 음료의 제조를 위한 과육을 함유할 수 있다. 이러한 성분은 독립적으로 또는 조합하여 사용할 수 있으며, 이러한 첨가제의 비율은 그렇게 중요하진 않지만 본 발명의 추출물 100 중량부 당 0 내지 약 20 중량부의 범위에서 선택되는 것이 일반적이다.In addition to the above, the extract of the present invention includes various nutrients, vitamins, minerals (electrolytes), flavors such as synthetic flavors and natural flavors, coloring and neutralizing agents (such as cheese and chocolate), pectic acid and salts thereof, alginic acid and its Salts, organic acids, protective colloidal thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohols, carbonation agents used in carbonated beverages, and the like. In addition, the extracts of the present invention may contain flesh for the production of natural fruit juices and fruit juice beverages and vegetable beverages. These components may be used independently or in combination, and the proportion of such additives is not so critical but is generally selected in the range of 0 to about 20 parts by weight per 100 parts by weight of the extract of the present invention.
이하, 본 발명을 실시예에 의해 상세히 설명한다. 단, 하기 실시예는 본 발명을 예시하는 것일 뿐, 본 발명의 내용이 하기 실시예에 한정되는 것은 아니다.Hereinafter, the present invention will be described in detail by way of examples. However, the following examples are illustrative of the present invention, and the present invention is not limited to the following examples.
재료 및 방법Materials and methods
식물 재료Plant material
모과의 건조되고 성숙된 열매를 한국의 바이오텍 회사인 "Korean Collection of Herbal Extracts"로부터 얻었다. 위 식물의 보증시료는 주식회사 약용자원콜렉션에 보관되어 있다 (Korea Collection of Herbal Extracts, 2000).The dried and mature fruits of the Chinese quince were obtained from the Korean biotech company "Korean Collection of Herbal Extracts." The guarantee samples of the above plants are stored in the Medicinal Resources Collection, Inc. (Korea Collection of Herbal Extracts, 2000).
추출extraction
건조되고 익은 열매를 작은 조각으로 썰고 미세한 분말로 분쇄하였다. 분말화된 모과 열매 (2 Kg, 건조 중량)를 80% 메탄올을 첨가한 후 실온ㅇ음지에서 2개월간 침지하였다. 이어서 추출물을 회전식 감압 농축기를 이용하여 20-30℃에서 농축하여 건조된 조추출물(210 g)을 얻었다.The dried and ripe fruit was cut into small pieces and ground into fine powder. Powdered Chinese quince fruits (2 Kg, dry weight) were soaked for 2 months at room temperature after adding 80% methanol. Subsequently, the extract was concentrated at 20-30 ° C. using a rotary vacuum concentrator to obtain dried crude extract (210 g).
분획Fraction
메탄올 조추출물(210 g)을 증류수(1L)에 현탁하고, n-헥산, 메틸렌 클로라이드, 에틸 아세테이트 및 n-부탄올을 이용하여 분획하여 각각 n-헥산 (17 g), 메틸렌 클로라이드 (12 g), 에틸 아세테이트 (26 g), n-부탄올 (77 g) 및 수성 (64 g) 분획을 얻었다. 효소 저해 활성 분석을 조추출물 및 다양한 분획에 대해 500 ㎍/mL 농도를 이용하여 수행하였다.Methanol crude extract (210 g) was suspended in distilled water (1 L) and fractionated with n-hexane, methylene chloride, ethyl acetate and n-butanol to give n-hexane (17 g), methylene chloride (12 g), Ethyl acetate (26 g), n-butanol (77 g) and aqueous (64 g) fractions were obtained. Enzyme Inhibitory Activity Assay 500 ㎍ / mL for Crude Extracts and Various Fractions It was performed using the concentration.
시약reagent
α-글루코시다아제 (사카로마이세스 세레비지애(Saccharomyces cerevisiae) type I 유래), β-글루코시다아제 (아몬드 유래), α-갈락토시다아제 (녹색 커피빈 유래), β-갈락토시다아제 (대장균 유래), 4-니트로페닐 α-D-글루코피라노시드, 4-니트로페닐 β-D-글루코피라노시드, 4-니트로페닐 α-D-갈락토피라노시드, 2-니트로페닐 β-D-갈락토피라노시드를 Sigma-Aldrich (St. Louis, MO, USA)로부터 구입하였다. 기타 시판되는 시약 및 용매를 이용하였다.α-glucosidase (from Saccharomyces cerevisiae type I), β-glucosidase (from almonds), α-galactosidase (from green coffee beans), β-galactosida Aze (from E. coli), 4-nitrophenyl α-D-glucopyranoside, 4-nitrophenyl β-D-glucopyranoside, 4-nitrophenyl α-D-galactopyranoside, 2-nitrophenyl β-D-galactopyranoside was purchased from Sigma-Aldrich (St. Louis, Mo., USA). Other commercial reagents and solvents were used.
효소 분석Enzyme analysis
α-글루코시다아제, β-글루코시다아제, α-갈락토시다아제 및 β-갈락토시다아제에 대한 효소 저해 활성을 이전에 보고된 Shibano 등의 방법 (Shibano et al. 1997. Chem. Pharm. Bull., 45: 700-775)을 약간 변형하여 평가하였다.The previously reported methods of enzyme inhibitory activity against α-glucosidase, β-glucosidase, α-galactosidase and β-galactosidase (Shibano et al. 1997. Chem. Pharm. Bull., 45: 700-775) with a slight modification.
α-글루코시다아제 분석α-glucosidase assay
반응 혼합물은 50 ㎕의 0.1 M 인산염 완충액 (pH 7.0), 25 ㎕의 0.5 mM 4-니트로페닐 α-D-글루코피라노시드 (0.1 M 인산염 완충액, pH 7.0에 용해), 10 ㎕의 시료 (농도: 500 ㎍mL-1) 및 25 ㎕의 α-글루코시다아제 용액 (0.01 M 인산염 완충액, pH 7.0 중의 스톡 용액 1 mgmL-1 을 분석 직전에 pH 7.0의 동일한 완충액으로 0.04 Units mL-1 로 희석하였다)으로 이루어졌다. 상기 반응 혼합물을 이어서 37℃에서 30 분간 배양하였다. 이어서, 상기 반응을 100 ㎕의 0.2 M 탄산나트륨 용액을 첨가하여 종료시켰다. 기질의 효소 가수분해를 반응 혼합물 중에 방출된 p-니트로페놀의 양을 마이크로플레이트 해독기를 이용하여 410 nm에서 흡광도를 측정하여 분석하였다. 모든 실험을 3 반복으로 수행하였다.The reaction mixture consists of 50 μl 0.1 M phosphate buffer (pH 7.0), 25 μl 0.5 mM 4-nitrophenyl α-D-glucopyranoside (soluble in 0.1 M phosphate buffer, pH 7.0), 10 μl sample (concentration). : to 500 ㎍mL -1) and of 25 ㎕ α- glucosidase solution (0.01 M phosphate buffer, pH 7.0 in the stock solution 1 mgmL -1 just before analysis with the same buffer of pH 7.0 was diluted with 0.04 mL Units -1 ) The reaction mixture was then incubated at 37 ° C. for 30 minutes. The reaction was then terminated by addition of 100 μl 0.2 M sodium carbonate solution. Enzymatic hydrolysis of the substrate was analyzed by measuring the absorbance at 410 nm using a microplate reader to determine the amount of p-nitrophenol released in the reaction mixture. All experiments were performed in 3 replicates.
β-글루코시다아제 분석β-glucosidase assay
반응 혼합물은 50 ㎕의 0.1 M 인산염 완충액 (pH 7.0), 25 ㎕의 0.5 mM 4-니트로페닐 β-D-글루코피라노시드 (0.1 M 인산염 완충액, pH 7.0에 용해), 10 ㎕의 시료 (농도: 500 ㎍ mL-1) 및 25 ㎕의 β-글루코시다아제 용액 (0.01 M 인산염 완충액, pH 7.0 중의 스톡 용액 1 mgmL-1 을 분석 직전에 pH 7.0의 동일한 완충액으 로 0.04 Units mL-1 로 희석하였다)로 이루어졌다. 상기 반응 혼합물을 이어서 37℃에서 30 분간 배양하였다. 이어서, 상기 반응을 100 ㎕의 0.2 M 탄산나트륨 용액을 첨가하여 종료시켰다. 기질의 효소 가수분해를 반응 혼합물 중에 방출된 p-니트로페놀의 양을 마이크로플레이트 해독기를 이용하여 410 nm에서 흡광도를 측정하여 분석하였다. 모든 실험을 3 반복으로 수행하였다.The reaction mixture was prepared with 50 μl 0.1 M phosphate buffer (pH 7.0), 25 μl 0.5 mM 4-nitrophenyl β-D-glucopyranoside (dissolved in 0.1 M phosphate buffer, pH 7.0), 10 μl sample (concentration). : 500 μg mL- 1 ) and 25 μl of β-glucosidase solution (0.01 M phosphate buffer, 1 mgmL- 1 of stock solution in pH 7.0, diluted 0.04 Units mL- 1 with the same buffer at pH 7.0 immediately before analysis) It was made). The reaction mixture was then incubated at 37 ° C. for 30 minutes. The reaction was then terminated by addition of 100 μl 0.2 M sodium carbonate solution. Enzymatic hydrolysis of the substrate was analyzed by measuring the absorbance at 410 nm using a microplate reader to determine the amount of p-nitrophenol released in the reaction mixture. All experiments were performed in 3 replicates.
α-갈락토시다아제 분석α-galactosidase assay
반응 혼합물은 50 ㎕의 0.1 M 인산염 완충액 (pH 7.0), 25 ㎕의 0.5 mM 4-니트로페닐 α-D-갈락토피라노시드 (0.1 M 인산염 완충액, pH 7.0에 용해), 10 ㎕의 시료 (농도: 500 ㎍ mL-1) 및 25 ㎕의 α-갈락토시다아제 용액 (0.01 M 인산염 완충액, pH 7.0 중의 스톡 용액 1 mgmL-1 을 분석 직전에 pH 7.0의 동일한 완충액으로 0.04 Units mL-1 로 희석하였다)로 이루어졌다. 상기 반응 혼합물을 이어서 37℃에서 30 분간 배양하였다. 이어서, 상기 반응을 100 ㎕의 0.2 M 탄산나트륨 용액을 첨가하여 종료시켰다. 기질의 효소 가수분해를 반응 혼합물 중에 방출된 p-니트로페놀의 양을 마이크로플레이트 해독기를 이용하여 410 nm에서 흡광도를 측정하여 분석하였다. 모든 실험을 3 반복으로 수행하였다.The reaction mixture was prepared with 50 μl 0.1 M phosphate buffer (pH 7.0), 25 μl 0.5 mM 4-nitrophenyl α-D-galactopyranoside (dissolved in 0.1 M phosphate buffer, pH 7.0), 10 μl sample ( concentration to 500 ㎍ mL -1) and 25 ㎕ α- galactosidase solution (0.01 M phosphate buffer, the same buffer having a pH of 0.04 Units mL -1 stock solution pH 1 to 7.0 in 7.0 mgmL -1 just prior to analysis Diluted). The reaction mixture was then incubated at 37 ° C. for 30 minutes. The reaction was then terminated by addition of 100 μl 0.2 M sodium carbonate solution. Enzymatic hydrolysis of the substrate was analyzed by measuring the absorbance at 410 nm using a microplate reader to determine the amount of p-nitrophenol released in the reaction mixture. All experiments were performed in 3 replicates.
β-갈락토시다아제 분석β-galactosidase assay
반응 혼합물은 50 ㎕의 0.1 M 인산염 완충액 (pH 7.0), 25 ㎕의 0.5 mM 2-니트로페닐 β-D-갈락토피라노시드 (0.1 M 인산염 완충액, pH 7.0에 용해), 10 ㎕의 시료 (농도: 500 ㎍ mL-1) 및 25 ㎕의 β-갈락토시다아제 용액 (0.01 M 인산염 완충액, pH 7.0 중의 스톡 용액 1 mgmL-1 을 분석 직전에 pH 7.0의 동일한 완충액으로 0.04 Units mL-1 로 희석하였다)로 이루어졌다. 상기 반응 혼합물을 이어서 37℃에서 30 분간 배양하였다. 이어서, 상기 반응을 100 ㎕의 0.2 M 탄산나트륨 용액을 첨가하여 종료시켰다. 기질의 효소 가수분해를 반응 혼합물 중에 방출된 o-니트로페놀의 양을 마이크로플레이트 해독기를 이용하여 410 nm에서 흡광도를 측정하여 분석하였다. 모든 실험을 3 반복으로 수행하였다.The reaction mixture was prepared with 50 μl 0.1 M phosphate buffer (pH 7.0), 25 μl 0.5 mM 2-nitrophenyl β-D-galactopyranoside (dissolved in 0.1 M phosphate buffer, pH 7.0), 10 μl sample ( concentration to 500 ㎍ mL -1) and 25 ㎕ β- galactosidase solution (0.01 M phosphate buffer, the same buffer having a pH of 0.04 Units mL -1 stock solution pH 1 to 7.0 in 7.0 mgmL -1 just prior to analysis Diluted). The reaction mixture was then incubated at 37 ° C. for 30 minutes. The reaction was then terminated by addition of 100 μl 0.2 M sodium carbonate solution. Enzymatic hydrolysis of the substrate was analyzed by measuring the absorbance at 410 nm using a microplate reader to determine the amount of o-nitrophenol released in the reaction mixture. All experiments were performed in 3 replicates.
통계학적 분석Statistical analysis
모든 분석을 3반복으로 적어도 3회 수행하였다. 모든 분석에 대한 저해율을 저해제 없는 대조구 (MeOH을 함유하는 완충액)의 백분율로서 계산하였다. 모든 결과를 평균ㅁSD로서 표시하였다.All analyzes were performed at least three times in three replicates. Inhibition rates for all assays were calculated as percentage of control (inhibitor containing MeOH) without inhibitor. All results are expressed as mean W SD.
실시예 1: 본 발명의 모과 추출물의 당뇨병 관련 효소 저해 효과Example 1 Diabetes-Related Enzyme Inhibitory Effect of the Chinese Quince Extract
모과의 조추출물 및 이의 다양한 분획을 α-글루코시다아제, β-글루코시다아제, α-갈락토시다아제 및 β-갈락토시다아제 효소 저해 연구에 대해 5 ㎍/210 ㎕ 농도에서 평가하였다.The crude extracts of the quince and various fractions thereof were evaluated at 5 μg / 210 μl concentrations for the α-glucosidase, β-glucosidase, α-galactosidase and β-galactosidase enzyme inhibition studies.
모든 모과 추출물은 82-99% 범위의 현저한 α-글루코시다아제 저해 활성 (5 ㎍/210 ㎕ 반응의 농도에서)을 보여주었다 (도 1): n-부탄올 (99%) > 물(97%) > 에틸 아세테이트 (92%) > n-헥산 (91%) > 조추출물 (89%) > 메틸렌 클로라이드 (82%).All quince extracts showed significant α-glucosidase inhibitory activity (at concentrations of 5 μg / 210 μl reaction) in the range of 82-99% (FIG. 1): n-butanol (99%)> water (97%) > Ethyl acetate (92%)> n-hexane (91%)> crude extract (89%)> methylene chloride (82%).
또한 β-글루코시다아제 저해 결과는 하기와 같다: 물 (85%) > 조추출물 (58%) > 에틸 아세테이트 (48%) > 메틸렌 클로라이드 (40%) > n-부탄올 (37%) > n-헥산 (5%). 이는 단지 물 추출물에서 현저한 β-글루코시다아제 저해 활성을 보여준다 (도 2).In addition, β-glucosidase inhibition results are as follows: water (85%)> crude extract (58%)> ethyl acetate (48%)> methylene chloride (40%)> n-butanol (37%)> n- Hexane (5%). It only shows significant β-glucosidase inhibitory activity in the water extract (FIG. 2).
덜 현저한 α-갈락토시다아제 (18-35%) 및 β-갈락토시다아제 (10-34%) 저해가 모든 모과 분획에서 조사되었다 (도 3 및 도 4).Less significant α-galactosidase (18-35%) and β-galactosidase (10-34%) inhibition were investigated in all quince fractions (Figures 3 and 4).
하기에 본 발명의 추출물을 포함하는 약학조성물의 제제예를 설명하나, 본 발명은 이를 한정하고자 함이 아닌 단지 구체적으로 설명하고자 함이다.Hereinafter, an example of the preparation of a pharmaceutical composition including the extract of the present invention will be described, but the present invention is not intended to limit the present invention, but is intended to be described in detail.
제제예 1: 산제의 제조Formulation Example 1 Preparation of Powder
모과 열매 추출물 분말 20 mgChinese
유당 100 mg
탈크 10 mgTalc 10 mg
상기의 성분들을 혼합하고 기밀포에 충진하여 산제를 제조한다.The above ingredients are mixed and filled in an airtight cloth to prepare a powder.
제제예 2: 정제의 제조Formulation Example 2: Preparation of Tablet
모과 열매 추출물 분말 10 mgChinese quince extract powder 10 mg
옥수수전분 100 mg
유당 100 mg
스테아린산 마그네슘 2 mg2 mg magnesium stearate
상기의 성분들을 혼합한 후 통상의 정제의 제조방법에 따라서 타정하여 정제를 제조한다.After mixing the above components, tablets are prepared by tableting according to a conventional method for preparing tablets.
제제예 3: 캅셀제의 제조Formulation Example 3: Preparation of Capsule
모과 열매 추출물 분말 10 mgChinese quince extract powder 10 mg
결정성 셀룰로오스 3 mg3 mg of crystalline cellulose
락토오스 14.8 mgLactose 14.8 mg
마그네슘 스테아레이트 0.2 mgMagnesium Stearate 0.2 mg
통상의 캡슐제 제조방법에 따라 상기의 성분을 혼합하고 젤라틴 캡슐에 충전하여 캡슐제를 제조한다.According to a conventional capsule preparation method, the above ingredients are mixed and filled into gelatin capsules to prepare capsules.
제제예 4: 주사제의 제조Formulation Example 4 Preparation of Injection
모과 열매 추출물 분말 10 mgChinese quince extract powder 10 mg
만니톨 180 mgMannitol 180 mg
주사용 멸균 증류수 2974 mgSterile distilled water for injection 2974 mg
Na2HPO4·12H2O 26 mg Na 2 HPO 4 · 12H 2 O 26 mg
통상의 주사제의 제조방법에 따라 1 앰플당(2 ㎖) 상기의 성분 함량으로 제조한다.According to the conventional method for preparing an injection, the amount of the above ingredient is prepared per ampoule (2 ml).
제제예 5: 액제의 제조Formulation Example 5 Preparation of Liquid
모과 열매 추출물 분말 20 mgChinese
이성화당 10 g10 g per isomer
만니톨 5 g5 g mannitol
정제수 적량Purified water quantity
통상의 액제의 제조방법에 따라 정제수에 각각의 성분을 가하여 용해시키고 레몬향을 적량 가한 다음 상기의 성분을 혼합한 다음 정제수를 가하여 전체를 정제수를 가하여 전체 100 ㎖로 조절한 후 갈색병에 충진하여 멸균시켜 액제를 제조한다.According to the conventional method for preparing a liquid, each component is added and dissolved in purified water, lemon flavor is added, the above components are mixed, purified water is added, the whole is adjusted to 100 ml by adding purified water, and then filled in a brown bottle. The solution is prepared by sterilization.
제제예 6: 건강 음료의 제조Formulation Example 6 Preparation of Healthy Drinks
모과 열매 추출물 분말 100 ㎎Chinese Quince Extract Powder 100mg
비타민 C 15 g15 g of vitamin C
비타민 E(분말) 100 g100 g of vitamin E (powder)
젖산철 19.75 g19.75 g of ferrous lactate
산화아연 3.5 g3.5 g of zinc oxide
니코틴산아미드 3.5 gNicotinic acid amide 3.5 g
비타민 A 0.2 gVitamin A 0.2 g
비타민 B1 0.25 gVitamin B 1 0.25 g
비타민 B2 0.3gVitamin B 2 0.3 g
물 정량Water quantification
통상의 건강음료 제조방법에 따라 상기의 성분을 혼합한 다음, 고압용기를 이용하여 약 1시간동안 100℃와 130℃ 사이에서 가열한 후, 만들어진 용액을 여과하여 멸균된 2 ℓ 용기에 취득하여 밀봉 멸균한 뒤 냉장 보관한 다음 본 발명의 건강음료 조성물 제조에 사용한다.After mixing the above components according to a conventional healthy beverage manufacturing method, using a high pressure vessel for about 1 hour and heated between 100 ℃ and 130 ℃, the resulting solution is filtered and obtained in a sterilized 2 L container and sealed After sterilization and refrigerated, it is used to prepare a healthy beverage composition of the present invention.
상기 조성비는 비교적 기호음료에 적합한 성분을 바람직한 실시예로 혼합 조성하였지만 수요계층이나, 수요국가, 사용용도 등 지역적, 민족적 기호도에 따라서 그 배합비를 임의로 변형 실시하여도 무방하다.Although the compositional ratio is relatively mixed with a component suitable for a favorite drink, it is also possible to arbitrarily modify the compounding ratio according to the regional or national preference such as the demand class, the demanding country, and the use purpose.
도 1은 5 ㎍/210 ㎕의 농도에서 모과의 조추출물 및 이의 분획에 의한 α-글루코시다아제 저해 결과이다.1 is a result of α-glucosidase inhibition by the crude extract of quince and fractions thereof at a concentration of 5 μg / 210 μl.
도 2는 5 ㎍/210 ㎕의 농도에서 모과의 조추출물 및 이의 분획에 의한 β-글루코시다아제 저해 결과이다.FIG. 2 shows the results of β-glucosidase inhibition by crude extracts of quince and fractions thereof at a concentration of 5 μg / 210 μl.
도 3은 5 ㎍/210 ㎕의 농도에서 모과의 조추출물 및 이의 분획에 의한 α-갈락토시다아제 저해 결과이다.Figure 3 is the result of α-galactosidase inhibition by the crude extract of quince and fractions thereof at a concentration of 5 μg / 210 μl.
도 4는 5 ㎍/210 ㎕의 농도에서 모과의 조추출물 및 이의 분획에 의한 β-갈락토시다아제 저해 결과이다.Figure 4 shows the results of β-galactosidase inhibition by the crude extract of quince and fractions thereof at a concentration of 5 μg / 210 μl.
Claims (7)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1020090057764A KR20110000323A (en) | 2009-06-26 | 2009-06-26 | Pharmaceutical and health food composition for preventing and treating diabetes mellitus comprising fruit extracts of chaenomeles sinensis as effective component |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR1020090057764A KR20110000323A (en) | 2009-06-26 | 2009-06-26 | Pharmaceutical and health food composition for preventing and treating diabetes mellitus comprising fruit extracts of chaenomeles sinensis as effective component |
Publications (1)
Publication Number | Publication Date |
---|---|
KR20110000323A true KR20110000323A (en) | 2011-01-03 |
Family
ID=43609192
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1020090057764A KR20110000323A (en) | 2009-06-26 | 2009-06-26 | Pharmaceutical and health food composition for preventing and treating diabetes mellitus comprising fruit extracts of chaenomeles sinensis as effective component |
Country Status (1)
Country | Link |
---|---|
KR (1) | KR20110000323A (en) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103446278A (en) * | 2013-08-29 | 2013-12-18 | 河南大学 | Crabapple extract as well as preparation method and application for same |
KR101522371B1 (en) * | 2013-06-05 | 2015-05-26 | 재단법인 전주생물소재연구소 | Food and pharmaceutical composition comprising hot water extract of Chaenomeles sinensis fruit with improved liver function and antioxidant activity |
JP2017193909A (en) * | 2016-04-22 | 2017-10-26 | 株式会社日本コムダック | anchor |
-
2009
- 2009-06-26 KR KR1020090057764A patent/KR20110000323A/en not_active IP Right Cessation
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR101522371B1 (en) * | 2013-06-05 | 2015-05-26 | 재단법인 전주생물소재연구소 | Food and pharmaceutical composition comprising hot water extract of Chaenomeles sinensis fruit with improved liver function and antioxidant activity |
CN103446278A (en) * | 2013-08-29 | 2013-12-18 | 河南大学 | Crabapple extract as well as preparation method and application for same |
JP2017193909A (en) * | 2016-04-22 | 2017-10-26 | 株式会社日本コムダック | anchor |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
KR101052191B1 (en) | Pharmaceutical composition for the prevention and treatment of diabetes mellitus, cancer or neurodegenerative diseases containing ramie grass extract as an active ingredient | |
KR102132655B1 (en) | Composition containing chrysanthemum zawadskii extract | |
TWI679980B (en) | Obesity suppressing composition | |
KR102064651B1 (en) | Composition for preventing or improving diabetes mellitus comprising momrdica charantia (l.) extract, chrysanthemum zawadskii var. latilobum and paeonia lactiflora extract as an effective ingredient | |
KR101209574B1 (en) | Pharmaceutical compositions and health functional foods compositions for the improvement of liver functions containing compound isolated from Youngia denticulata as an active ingredient | |
KR101651082B1 (en) | A Composition Comprising the Fermentate of Puerariae Radix extract for protecting liver damage | |
KR20110000323A (en) | Pharmaceutical and health food composition for preventing and treating diabetes mellitus comprising fruit extracts of chaenomeles sinensis as effective component | |
KR102087167B1 (en) | Pharmaceutical composition for Anti-oxidative or Anti-inflammatory comprising extract processed by Enzymatic hydrolysis of the Bark of Kalopanax pictus(Thunb.) Nakai | |
KR101446784B1 (en) | Pharmaceutical composition for anticancer comprising extract of sea cucumber or its fraction as effective component | |
KR101321879B1 (en) | Hepatoprotective pharmaceutical composition comprising an extract from caryopteris incana and compounds isolated therefrom | |
KR101623209B1 (en) | Composition comprising isolated from Cassia tora or Cassia obtusifolia or for the prevention and treatment of cognitive dysfunction disorder | |
KR101338172B1 (en) | Pharmaceutical composition comprising the extract paeonia lactiflora, fraction thereof or compound isolated therefrom as an active ingredient | |
KR20100055952A (en) | Extract antibiotic to helicobacter pylori extracted from persimmon leaves | |
KR20050003665A (en) | Composition comprising an extract of Peucedanum japonicum for preventing and treating diabetes | |
KR20200117501A (en) | Composition for improving damages of neuronal cells or inhibiting apoptosis of neuronal cells | |
KR101357674B1 (en) | Pharmaceutical composition comprising the extract paeonia lactiflora, fraction thereof or compound isolated therefrom as an active ingredient | |
KR101494436B1 (en) | Novel compound from the fruits of Acanthopanax sessiliflorus | |
KR102588131B1 (en) | Composition for preventing or treating brain diseases caused by ultrafine dust containing mugwort and lizard’s tail extract as an active ingredient | |
KR102227261B1 (en) | Composition for preventing, ameliorating or treating atopic dermatitis comprising enzyme treated Diospyros lotus as effective component | |
KR101715996B1 (en) | Composition for antidiabetic activity comprising dichloromethane or ethyl acetate fraction of Hizikia fusiformis extract as effective component | |
KR20130082249A (en) | Composition for preventing or improving the metabolic syndrome containing parthenocissus tricuspidata extract | |
KR20110118748A (en) | Compositions for prevention and improvement of cancer containing the extracts of ligularia fischeri var. spiciformis nakai as an active ingredient | |
KR101820083B1 (en) | Pharmaceutical compositions for inhibiting tumor comprising an extract of Allium hookeri | |
KR101695186B1 (en) | Composition for treating, improving or preventing diabetes | |
KR102087165B1 (en) | Pharmaceutical composition for Anti-oxidative or Anti-inflammatory comprising extract processed by Enzymatic hydrolysis of the Bark of Eleutherococcus sessiliflorus |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
A201 | Request for examination | ||
E902 | Notification of reason for refusal | ||
E601 | Decision to refuse application | ||
SUBM | Surrender of laid-open application requested |