CN108354940A - Application of the forsythiaside A in preparing slimming medicine - Google Patents
Application of the forsythiaside A in preparing slimming medicine Download PDFInfo
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- CN108354940A CN108354940A CN201810450564.3A CN201810450564A CN108354940A CN 108354940 A CN108354940 A CN 108354940A CN 201810450564 A CN201810450564 A CN 201810450564A CN 108354940 A CN108354940 A CN 108354940A
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- forsythiaside
- folium forsythia
- pancreatic lipase
- extract
- isomer
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Abstract
The application that the invention discloses the mixtures or single component of forsythiaside A and its isomer in preparing slimming medicine.Folium Forsythia water extract or the alcohol extract of different ethanol concentration are identified through separation and pancreatic lipase activity are inhibited to detect, the results showed that:Ursolic acid, oleanolic acid, rutin, aurantiamarin, forsythiaside A and its isomer, chlorogenic acid, caffeic acid, arctigenin, 3 O rutinosides of Kaempferol are its main component, they all have external inhibition pancreatic lipase effect.Wherein forsythiaside A inhibits pancreatic lipase activity IC50 to reach 1346 μ g/mL.So the mixture or single component of forsythiaside A and its isomer can be used for preparing slimming medicine, slimming health product and diet food.
Description
Technical field
The present invention relates to plant or the new application of its extract, more particularly to Folium Forsythia or its component is preparing weight reduction product
In application, i.e. the application in preparing slimming medicine, slimming health product and diet food.
Background technology
The World Health Organization is it is expressly intended that obesity is global maximum chronic disease, for global prevalence disease [Report of
a WHO consultation.2000,894:i-xii,1-253].1,000,000,000 adults are had more than in the world and 10% children belong to super
Weight and fat [Haslam DW, et al.Lancet.2005,366 (9492):1197-209].Be grown up overweight rate of China is
22.8%, obesity rates 7.1%, estimated number is respectively more than 2.0 hundred million and 6 000 ten thousand [Wang Longde chief editor's people's health publication
Society, 2005].
Obesity can lead to 57% non-insulin-dependent (II types) diabetes;30% gallbladder disease;17%
Coronary heart disease;17% hypertension;14% osteoarthritis;11% breast cancer/uterus/colorectal cancer [Mary Beth
Chalk et al.The Case Manager.2004,15(6):47-49].Annual at least 3,400,000 adult die of it is overweight or
Fat [M.Ezzati, et al.Lancet.2002,360 (9343):1347-1360].
Fat-reducing effect is best at present and can take the drug of (1-2) only one kind the long period, i.e. Roche Holding Ag produces
Xenical (xenical) also known as orlistat (Orlistat) [Chaput JP, et al.Mini Rev Med
Chem.2007,7(1):3-10.].The medicine is pancreatic lipase inhibitor, but has larger side effect, can especially liver be caused to damage
Wound.
Pancreatic lipase is by pancreatic secretion to duodenum, and the food fat of hydrolyzable 50%-70% is at monoglyceride and fat
Fat acid, inhibits pancreatic lipase activity that can prevent lipolysis, and then it is made directly to be excreted by alimentary canal, subtracts to reach
Fertile purpose.
Fructus Forsythiae (Forsythia suspensa (Thunb.) Vahl) is Oleaceae forsythia, widely distributed Yushan Hill
The ground such as west, Shaanxi, Hebei, Henan.Fructus Forsythiae fruit is one of clinical common traditional Chinese medicine, has multiple pharmacological effect, as antibacterial,
It is antiviral, it is anti-inflammatory, it is anti-oxidant and other effects.Fructus Forsythiae leaf-making quantity is huge, if being developed into diet products, economic benefit will very may be used
It sees.
Invention content
The purpose of the present invention is to provide the new application of Folium Forsythia, i.e. Folium Forsythia or its component is preparing slimming medicine, is subtracting
Application in fertile health products and diet food.
The application of Folium Forsythia provided by the invention or its component in preparing slimming medicine;It is prepared by Folium Forsythia or its component
Application in slimming health product;The application of Folium Forsythia or its component in preparing diet food.
The Folium Forsythia is fresh Folium Forsythia or dry Folium Forsythia, or through bubble, water steaming, boiling, drying or other is killed
Folium Forsythia processed product obtained by green mode.
The Folium Forsythia component is the water extract of Folium Forsythia, the alcohol extract of the different ethanol concentration of Folium Forsythia, Folium Forsythia
Water extract precipitation, the heavy shallow lake of water of the different ethanol concentration alcohol extract of Folium Forsythia, the water extract of Folium Forsythia through macroreticular resin not
It is eluted through macroreticular resin different ethanol concentration with the component of concentration of alcohol elution or the different ethanol concentration alcohol extract of Folium Forsythia
Component.
The Folium Forsythia or its component contain kaempferol-3-O-rutinoside, arctigenin, forsythiaside A and
The ingredients such as its isomer.Kaempferol-3-O-rutinoside, arctigenin, forsythiaside A and forsythiaside A are different with dividing
The mixture or single component of structure body can be applied in preparing slimming medicine, slimming health product and diet food.Kaempferol -3-O-
Rutinoside inhibits pancreatic lipase activity highest, is preferred for slimming medicine, slimming health product and diet food.
The preparation condition of Folium Forsythia or its component:
The 1 ︰ 2-200 of solid-liquid ratio that Folium Forsythia and processed product water carry, 0 DEG C -100 DEG C of Extracting temperature, extraction time 5min-
120h。
Folium Forsythia and the concentration of alcohol of processed product alcohol extracting are 5%-100%, 1 ︰ 2-200 of solid-liquid ratio, 0 DEG C -100 of Extracting temperature
DEG C, extraction time 5min-120h.
Water extract precipitates or 0-100 DEG C of the water temperature of alcohol extracting-water precipitating, and the volume ratio of precipitation and water is 1 ︰ 1-1000.
In water extract or alcohol extract macroreticular resin ethanol elution component, macroreticular resin includes nonpolarity, middle polarity and polarity
Three classes, ethanol eluate concentration 5%-100%.
The present invention is it has been investigated that the antiobesity action mechanism of Folium Forsythia or its component, is by Kaempferol -3-O- rutinoses
The ingredients such as glycosides, arctigenin, forsythiaside A and its isomer inhibit pancreatic lipase activity, to prevent fat from
Alimentary canal is digested and absorbs, and fat directly plays antiobesity action by the way that alimentary canal excretes, and reaches weight-reducing purpose.Fructus Forsythiae
Glycosides cannot inhibit pancreatic lipase activity, can promote pancreatic lipase activity instead.Folium Forsythia or its component act on class to pancreatic lipase
Type divides Reverse transcriptase, Noncompetition inhibition and uncompetitive inhibitor.
Folium Forsythia or its component have apparent antiobesity action, and 1500 μ g/mL of boiling Folium Forsythia processed product alcohol extract are to pancreas
For lipase active inhibiting rate up to 39.5%, boiling Folium Forsythia processed product alcohol extract macroreticular resin ethanol elution component IC50 is reachable
Kaempferol-3-O-rutinoside IC50 in 230 μ g/mL, Folium Forsythia or its component is up to 1.7 ± 0.3 μ g/mL.
Description of the drawings
Fig. 1 do not process Folium Forsythia water extract, do not process Folium Forsythia absolute ethyl alcohol extract, boiling Folium Forsythia processed product water carries
Object (Aqe) and boiling Folium Forsythia processed product absolute ethyl alcohol extract inhibit pancreatic lipase activity to detect block diagram
Fig. 2 boiling Folium Forsythia processed product different ethanol concentration extract Inhibiting enzyme activities detect block diagram
40% alcohol extract D101 macroreticular resin ethanol waters of Fig. 3 boiling Folium Forsythias processed product elute liquid and inhibit pancreatic lipase
Activity
Forsythiaside A inhibits pancreatic lipase activity in Fig. 4 Folium Forsythias
It finds that arctigenin has in Fig. 5 Folium Forsythias for the first time and inhibits pancreatic lipase activity
The kaempferol-3-O-rutinoside mass spectrogram found for the first time in Fig. 6 Folium Forsythias.A), first mass spectrometric;B), two level matter
Spectrogram
Fig. 7 forsythins cannot inhibit pancreatic lipase activity, instead favorable curve graph.
Fig. 8 Folium Forsythia processed product water extract zoopery rat epididymis fat is sliced microexamination, and (A is Normal group;B
For model control group;C is Aqe low dose groups)
Fig. 9 Folium Forsythia processed product water extract zoopery jejunum in rats fuzzy surfaces accumulate microexamination, and (A is normal control
Group;B is model control group;C is Aqe low amounts group)
Specific implementation mode
The present invention is further illustrated with following embodiments, but the present invention is not limited by following embodiments.
Embodiment 1:The detection of Folium Forsythia water extract Inhibiting enzyme activity is not processed
Fresh Folium Forsythia is picked, washing removal leaf surface attachment dry, pulverize, precise powder 100g, solid-liquid ratio
1:10, refluxing extraction 2h, water extract are concentrated and dried, inhibited pancreatic lipase activity detection, and 1500 μ g/mL inhibiting rates are reachable
26.5% (Fig. 1).
Embodiment 2:The detection of Folium Forsythia absolute ethyl alcohol extract Inhibiting enzyme activity is not processed
Fresh Folium Forsythia is picked, washing removal leaf surface attachment dry, pulverize, precise powder 100g, solid-liquid ratio
1:10, refluxing extraction 2h, absolute ethyl alcohol extract are concentrated and dried, and inhibited pancreatic lipase activity detection, 1500 μ g/mL inhibiting rates can
Up to 33.8% (Fig. 1).
Embodiment 3:Boiling Folium Forsythia processed product water extract Inhibiting enzyme activity detects
Fresh Folium Forsythia, washing removal leaf surface attachment are picked, boiling water boiling 5-7min dry, pulverize, precise powder
Last 100g, solid-liquid ratio 1:10, refluxing extraction 2h, water extract are concentrated and dried, and are confirmed through Inhibiting enzyme activity detection and zoopery, the company
The inhibited pancreatic lipase activity detection of leaf processed product water extract is stuck up, 1500 μ g/mL inhibiting rates are up to 33.2% (Fig. 1).
Embodiment 4:Boiling Folium Forsythia processed product alcohol extract Inhibiting enzyme activity detects
Fresh Folium Forsythia, washing removal leaf surface attachment are picked, boiling water boiling 5-7min dry, pulverize, precise powder
Last 100g, solid-liquid ratio 1:10, refluxing extraction 2h, absolute ethyl alcohol extract are concentrated and dried, are detected through Inhibiting enzyme activity, 1500 μ g/mL
Inhibiting rate is up to 39.5% (Fig. 1).
Embodiment 5:Boiling Folium Forsythia processed product water carries or the detection of different ethanol concentration extract Inhibiting enzyme activity
Accurately weigh the Folium Forsythia powder of 100g processings respectively, totally 8 parts, respectively with 10%, 20%, 30%, 40%,
50%, 70%, 80%, 100% ethyl alcohol presses 1:10 solid-liquid ratio refluxing extractions 2 times, each 1h are filtered, and are concentrated, dry.It measures each
To the inhibiting rate of pancreatic lipase when extract 1.5mg/mL.To pancreas fat when Folium Forsythia different concentration ethanol extract 1.5mg/mL
Enzyme inhibition result is shown in Fig. 2.
Embodiment 6:Boiling Folium Forsythia processed product alcohol extract macroreticular resin ethanol elution component Inhibiting enzyme activity detects
Fresh Folium Forsythia, washing removal leaf surface attachment are picked, boiling water boiling 5-7min dry, pulverize, precise powder
Last 100g, solid-liquid ratio 1:10,40% alcohol reflux extracts 2 times, each 1h, and extracting solution is concentrated and dried, and then carries out D101 macropores
Resin detaches.Blade diameter length ratio 1:10, distillation water elution 6BV, 60% ethanol elution 10BV, ethanol eluate are concentrated and dried.Its ethyl alcohol
Eluent is detected through Inhibiting enzyme activity and is confirmed, IC50 is up to 230 μ g/mL (Fig. 3).
Embodiment 7:Water extraction or alcohol extract constituent analysis and Inhibiting enzyme activity detection
Water extract or alcohol extract are identified through separation and pancreatic lipase activity are inhibited to detect:Ursolic acid, oleanolic acid, rutin,
Aurantiamarin, forsythiaside A (Fig. 4) and its isomer, chlorogenic acid, caffeic acid, arctigenin (Fig. 5), Kaempferol -3-O-
Rutinoside (Fig. 6) is its main component, they all have external inhibition pancreatic lipase effect.Forsythiaside A, arctiin
Member, kaempferol-3-O-rutinoside inhibit pancreatic lipase activity IC50 respectively reach 1346 μ g/mL, 793 μ g/mL and 1.7 ±
0.3μg/mL。
Embodiment 8:Forsythin cannot inhibit pancreatic lipase activity, play a driving role instead to pancreatic lipase activity
Inhibited Enzyme assay, forsythin cannot inhibit pancreatic lipase activity, rise promote to pancreatic lipase activity instead
Effect, is shown in Fig. 7.
Embodiment 9:Folium Forsythia processed product water extract SD rats prevent obese model experiment
SD rats prevent obese model it is experimentally confirmed that Folium Forsythia processed product water extract can reach antiobesity action, as a result can join
It is shown in Table 1, table 2, table 3, Fig. 8 and Fig. 9.
Influences of 1 Aqe of table to obese rat weight
The P compared with Normal group<0.05#, P<0.01##;The P compared with model control group<0.05*, P<0.01**.
Influences of 2 Aqe of table to obese rat blood lipid level
The P compared with Normal group<0.05#, P<0.01##;The P compared with model control group<0.05*, P<0.01**.
Influences of 3 Aqe of table to obese rat fat weight in wet base and adipocyte
The P compared with Normal group<0.05#, P<0.01##;The P compared with model control group<0.05*, P<0.01**.
Claims (3)
1. application of the mixture or single component of forsythiaside A and its isomer in preparing slimming medicine.
2. application of the mixture or single component of forsythiaside A and its isomer in preparing slimming health product.
3. application of the mixture or single component of forsythiaside A and its isomer in preparing diet food.
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CN201510669879.3A CN105168372A (en) | 2015-10-16 | 2015-10-16 | Application of forsythia suspensa leaves or ingredients of forsythia suspensa leaves to preparation of weight reducing products |
CN201810450564.3A CN108354940A (en) | 2015-10-16 | 2015-10-16 | Application of the forsythiaside A in preparing slimming medicine |
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CN201810448735.9A Pending CN108451950A (en) | 2015-10-16 | 2015-10-16 | Application of the arctigenin in preparing slimming medicine |
CN201810450564.3A Pending CN108354940A (en) | 2015-10-16 | 2015-10-16 | Application of the forsythiaside A in preparing slimming medicine |
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CN201810448735.9A Pending CN108451950A (en) | 2015-10-16 | 2015-10-16 | Application of the arctigenin in preparing slimming medicine |
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JP2008297209A (en) * | 2007-05-29 | 2008-12-11 | Yomeishu Seizo Co Ltd | Lipid metabolism-improving composition |
EP2890370B1 (en) * | 2012-08-31 | 2019-10-09 | The Regents of the University of California | Agents useful for treating obesity, diabetes and related disorders |
KR101618116B1 (en) * | 2014-02-18 | 2016-05-04 | 경희대학교 산학협력단 | Composition of extracts of Arctium lappa or compounds isolated therefrom for preventing, improving or treating obesity or obesity-related disease |
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李飞鹤等: "连翘叶的减肥作用研究", 《中国优秀硕士学位论文全文数据库》 * |
栗亚云等: "天然植物中胰脂肪酶抑制剂的筛选", 《中国优秀硕士学位论文全文数据库》 * |
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