CN105055471A - Application of radix bupleuri total saponin and monomer saponin thereof in pharmacy - Google Patents
Application of radix bupleuri total saponin and monomer saponin thereof in pharmacy Download PDFInfo
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- CN105055471A CN105055471A CN201510562478.8A CN201510562478A CN105055471A CN 105055471 A CN105055471 A CN 105055471A CN 201510562478 A CN201510562478 A CN 201510562478A CN 105055471 A CN105055471 A CN 105055471A
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- RHQDCVBEHBPMRM-YDQBRKALSA-N C=[O][C@H](C(CO)O[C@H]1O)C(O)=C1O Chemical compound C=[O][C@H](C(CO)O[C@H]1O)C(O)=C1O RHQDCVBEHBPMRM-YDQBRKALSA-N 0.000 description 1
- BIWWGSPZDGZEAG-DHJFATIGSA-N CC([C@@H](CC1O)O)O[C@H]1[IH]C Chemical compound CC([C@@H](CC1O)O)O[C@H]1[IH]C BIWWGSPZDGZEAG-DHJFATIGSA-N 0.000 description 1
- XGODCVPMUHDWDG-SXONVWONSA-N C[C@@H](CC1)[C@@](C)(CO)C2[C@@]1(C)C1=CC=C(C(CC(C)(C)CC3)[C@@]3(CO)C(C3)O)[C@]3(C)[C@]1(C)CC2 Chemical compound C[C@@H](CC1)[C@@](C)(CO)C2[C@@]1(C)C1=CC=C(C(CC(C)(C)CC3)[C@@]3(CO)C(C3)O)[C@]3(C)[C@]1(C)CC2 XGODCVPMUHDWDG-SXONVWONSA-N 0.000 description 1
- DUORPEPKKFOECU-DIWMSMEYSA-N C[C@@H]1CC(CC(C)(C)CCCCO)=C2C=CC([C@@](C)(CC3)C(CC4)[C@](C)(CO)[C@H]3O)[C@]4(C)[C@]2(C)C1 Chemical compound C[C@@H]1CC(CC(C)(C)CCCCO)=C2C=CC([C@@](C)(CC3)C(CC4)[C@](C)(CO)[C@H]3O)[C@]4(C)[C@]2(C)C1 DUORPEPKKFOECU-DIWMSMEYSA-N 0.000 description 1
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Abstract
The invention provides an application of radix bupleuri total saponin and monomer saponin thereof in preparation of medicines for preventing and treating obesity, and a pharmaceutical composition taking the radix bupleuri total saponin and the monomer saponin as active components. A pharmacological experiment proves that the radix bupleuri total saponin and a monomer compound thereof have obvious agonist activity on a 5-HT2C receptor, has obvious effects of inhibiting appetite and inhibiting weight gain on SD rats in an animal experiment, and can be applied to prevention and treatment of obesity.
Description
Technical field:
The invention belongs to technical field of pharmaceuticals.Specifically, the present invention relates to extraction and isolation from bupleurum Chinese and obtain Radix Bupleuri total saponin and monomer saponin thereof, their application in the medicine preparing prevention and therapy obesity.
Background technology:
Obesity (obesity) refers to that generally fat content is more than 30% in woman's health, and man, more than 20% ~ 25%, can confirm as obesity containing excess fat tissue in health.The various diseases such as obesity and hypertension, hyperlipidemia, diabetes there is close relationship, it makes a lot of country be classified as the disease of preventability death on the impact of health.The slimming medicine now commercially sold mainly through appetite inhibiting, increase energy expenditure and suppress intestinal the aspect such as to digest and assimilate and play a role, such as sibutramine (sibutramine), Orlistat (orlistat) etc.But the toxic and side effects of these medicines limits their application.Natural product due to complex structure various, therefrom find high-efficiency low-toxicity, the lead compound of action target spot novelty become novel slimming medicine research and development important component part and achieved certain achievement (RayalamS. etc., J.Nutr.Biochem., 2008,19:717-726; YunJ.W.Phytochemistry, 2010,71:1625-1641.).
5-hydroxy tryptamine (5-Hydroxytryptamine5-HT) is a kind of central nervous system's mediator multiple physiological activity to important regulative, and its receptor is divided into 14 kinds of hypotypes according to structure difference, is wherein distributed in the 5-HT in cerebral hippocampus district
2Creceptor has obvious regulating action to appetite.Zoopery widely and gene analysis show 5-HT
2Creceptor can be used as the target spot of weight reduction with drugs effect.Existing bibliographical information is a series of has 5-HT
2Cthe synthesis compound of receptor agonism and antiobesity action, wherein locarserin entered clinical research (Smith, B.M. etc., J.Med.Chem., 2008,51,305-313 in 2012; WackerD.A. etc., J.Med.Chem., 2007,50:365-1379; FevigJ.M. etc., Bioorg.Med.Chem.Lett., 2013,330-335).Now not yet have with 5-HT
2Creceptor is the report of the natural slimming medicine of action target spot.
Radix Bupleuri (Bupleurumchinense) is Umbelliferae Bupleunim. L, and root is used as medicine as Radix Bupleuri, and its nature and flavor hardship is cool, enters liver and gall warp, have and to show in solution, the effect of soothing the liver, yang invigorating.Research shows that triterpene saponin, flavone, lignanoid, polyacetylene etc. are main chemical compositions.Present pharmacological research shows that Radix Bupleuri has antiinflammatory, immunomodulating, antiviral, the multiple pharmacologically active (.J.Pharm.Pharmacol. such as Ashour, M.L., 2011,63:305-321) such as to protect the liver.But for Radix Bupleuri total saponin or saikoside monomer compounds to 5-HT
2Cnot yet there is bibliographical information receptor agonism and appetite inhibiting effect aspect, also do not have their reports of application in the medicine of preparation prevention or treatment of obesity.
Summary of the invention:
The object of the present invention is to provide Radix Bupleuri total saponin and the application of all kinds of saikoside monomeric compound in the medicine preparing prevention or treatment of obesity, the pharmaceutical composition of the prevention and therapy obesity being active component with them.
In order to realize above-mentioned purpose of the present invention, the invention provides following technical scheme:
The application of Radix Bupleuri total saponin in the medicine preparing prevention or treatment of obesity.
As described in Radix Bupleuri total saponin preparation prevention or treatment of obesity medicine in application, wherein said Radix Bupleuri total saponin is prepared by following method and obtains: get Radix Bupleuri BupleurumchinenseDC, pulverize, 70%EtOH reflux, extract, three times, merge extractive liquid, be concentrated into small size, D101 macroporous resin column chromatography, use water, 70%EtOH, EtOH eluting successively; 70%EtOH elution fraction Rp-18 reversed phase column chromatography, the MeOH-H of 1:9 → 10:0
2o eluting obtains Radix Bupleuri total saponin.
As described in Radix Bupleuri total saponin preparation prevention or treatment of obesity medicine in application, wherein said application is that Radix Bupleuri total saponin passes through 5-HT
2Creceptor agonism and appetite inhibiting effect reach prevention or treatment of obesity.
As described in Radix Bupleuri total saponin preparation prevention or treatment of obesity medicine in application, in wherein said Radix Bupleuri extracting solution, Radix Bupleuri total saponin content is 20-70% weight, and described application is that Radix Bupleuri total saponin passes through 5-HT
2Creceptor agonism and appetite inhibiting effect reach prevention or treatment of obesity.
As as described in Radix Bupleuri total saponin preparation prevention or treatment of obesity medicine in application, wherein said Radix Bupleuri total saponin comprises the saponins compound 3-O-β-D-fucopyranosylsaikogeninf (1) being not less than 0.1% weight, saikoside a (saikosaponina, 2), 6 "-O-acetylation saikoside a (6 "-O-acetylsaikosaponina, 3), 3 ", 6 "-two-O-saikoside as (3 ", 6 "-di-O-acetylsaikosaponina, 4), saikoside d (saikosaponind, 5), saikoside e (saikosaponine, 6), saikoside b
1(saikosaponinb
1, 7), bavin saikoside g (saikosaponing, 8),
As described in Radix Bupleuri total saponin preparation prevention or treatment of obesity medicine in application, wherein said Radix Bupleuri total saponin comprises the saikoside a being not less than 0.1% weight.
The application of saikoside a in the medicine preparing prevention or treatment of obesity.
As described in saikoside a preparation prevention or treatment of obesity medicine in application, wherein said saikoside a is prepared by following method and obtains: get Radix Bupleuri BupleurumchinenseDC, pulverize, 70%EtOH reflux, extract, three times, merge extractive liquid, be concentrated into small size, D101 macroporous resin column chromatography, use water, 70%EtOH, EtOH eluting successively; 70%EtOH elution fraction Rp-18 reversed phase column chromatography, the MeOH-H of 1:9 → 10:0
2o eluting obtains Radix Bupleuri total saponin; Radix Bupleuri total saponin is through silica gel column chromatography, and the CHCl3-MeOH eluting of 9:1, obtains saikoside a.
As described in saikoside a preparation prevention or treatment of obesity medicine in application, wherein said application is that saikoside a passes through 5-HT
2Creceptor agonism and appetite inhibiting effect reach prevention or treatment of obesity.
As described in saikoside a preparation prevention or treatment of obesity medicine in application, wherein said saikoside a is as sole active agent in medicine.
The pharmaceutical composition of prevention or treatment of obesity, it comprises is prepared by following method and the Radix Bupleuri total saponin obtained, get Radix Bupleuri BupleurumchinenseDC, pulverize, 70%EtOH reflux, extract, three times, merge extractive liquid, is concentrated into small size, D101 macroporous resin column chromatography, uses water, 70%EtOH, EtOH eluting successively; 70%EtOH elution fraction Rp-18 reversed phase column chromatography, the MeOH-H of 1:9 → 10:0
2o eluting obtains Radix Bupleuri total saponin, and pharmaceutically acceptable carrier,
Described Radix Bupleuri total saponin comprises the saponins compound 3-O-β-D-fucopyranosylsaikogeninf (1), the saikoside a (saikosaponina that are not less than 0.1% weight; 2), 6 "-O-acetylation saikoside a (6 "-O-acetylsaikosaponina; 3), 3 "; 6 "-two-O-saikoside as (3 "; 6 "-di-O-acetylsaikosaponina; 4), saikoside d (saikosaponind; 5), saikoside e (saikosaponine, 6), saikoside b
1(saikosaponinb
1, 7), bavin saikoside g (saikosaponing, 8),
Or described Radix Bupleuri total saponin comprises the saikoside a (saikosaponina, 2) being not less than 0.1% weight.
Or, comprise using saikoside a as sole active agent, and the prevention of pharmaceutically acceptable carrier or the pharmaceutical composition for the treatment of of obesity.
When Radix Bupleuri total saponin of the present invention and all kinds of saikoside monomeric compound are used as medicine, directly can use, or use with the form of pharmaceutical composition.This pharmaceutical composition contains 0.1-99%, and be preferably the compounds of this invention of 0.5-90%, all the other are acceptable on materia medica, pharmaceutically suitable carrier of and inertia nontoxic to humans and animals and/or excipient.
Described pharmaceutical carrier or excipient are one or more solids, semisolid and liquid diluent, filler and pharmaceutical preparation adjuvant.Pharmaceutical composition of the present invention is used with the form of per weight dose.Medicine of the present invention can through injection (quiet note, intramuscular injection) and oral two kinds of form administrations.
The present invention adopts various method, is separated and obtains Radix Bupleuri total saponin and all kinds of saikoside monomeric compound from Radix Bupleuri root.Prove that Radix Bupleuri total saponin and all kinds of monomeric compound all have 5-HT through pharmacological evaluation
2Creceptor agonist activity and appetite inhibiting, body weight growth inhibition activity to rat.The present invention is effective component extracting from Chinese medicine, proves generation and the development that significantly can suppress obesity through pharmacological evaluation.
Accompanying drawing illustrates:
Fig. 1. be separated the part of compounds obtained in Radix Bupleuri;
Fig. 2. Radix Bupleuri total saponin increases (B) inhibitory action (n=6) * P<0.05 compared with blank group to the appetite (A) of rat with body weight;
Fig. 3 .saikosaponina (2) increases (B) inhibitory action (n=6) * P<0.05 compared with blank group to the appetite (A) of rat with body weight; * is P<0.01 compared with blank group.
Detailed description of the invention:
Below in conjunction with accompanying drawing, illustrate that Radix Bupleuri total saponin and monomer saponin are to 5-HT by test example of the present invention of the present invention
2Cthe agonist activity of receptor, and Radix Bupleuri total saponin and main component saikosaponina (2) are to appetite inhibiting, the body weight growth inhibition active function result of rat, but do not limit the present invention with this.
Test example 1:
1. materials and methods
1.1 materials: Radix Bupleuri total saponin and saikoside monomeric compound; 5-hydroxy tryptamine (being purchased from AlfaAesar), HEK293 cell (HDBiosciencesCo.Ltd, Shanghai, China), hyclone (GIBCO), 96 orifice plates (GIBCO); Calcium current detection kit (HDBiosciencesCo.Ltd, Shanghai, China); Sprague-Dawley rat (Kunming Medical University's Experimental Animal Center).
1.2 instruments: microplate reader Bio-RAD680 (U.S.); CO
2incubator ThermoForma3310 (U.S.); Inverted biological microscope XD-101 type (Nanjing).
1.3 experiment flow
1.3.15-HT
2Creceptor agonist activity is tested
Cell culture: in the DuEM culture medium that transfection has the HEK293 cell of receptor to be seeded in containing 10% hyclone, this operates on superclean bench and completes; Be positioned over containing 5%CO after inoculation
2, temperature is be cultured to cell in 37 DEG C of incubators to cover with culture bottle inwall.Bed board: suck the culture medium in culture bottle, with trypsin, cell is disintegrated down from culture bottle inwall, after add 10ml culture medium by cell suspension, the 96 hole Hei Bi being seeded in Matrigel bag quilt reveal the exact details on cell plates, every hole 100 μ l, controls its density and is about 4 × 10
4/ hole, this operates on superclean bench and completes; Be positioned over containing 5%CO after inoculation
2, temperature is be cultured to cell in 37 DEG C of incubators to cover with bottom cell plates.
Cell dyeing: discard culture fluid, add the dyeing liquor (the disposable test kit of calcium 8: HBSS buffer 9680 μ l, probenecid 100 μ l, compd A 20 μ l, compd B 200 μ l mix homogeneously under lucifuge condition) configured, every hole 100 μ l, is positioned over 1h in 37 DEG C of incubators.Positive drug and the configuration for reagent: 5-HT is diluted to variable concentrations as positive drug using HBSS buffer solution; HBSS buffer is as blank; The variable concentrations sample that the HBSS buffer of 990 μ l and 10 μ lDMSO dissolve is as supplying reagent.Draw positive drug, blank group and on reagent to 96 orifice plate, every hole 100 μ l, each sample repeats 3 holes.
The test of calcium current agonist activity: the agonist activity of sample has detected (excitation wavelength: 485nm on instrument FlexStation3BenchtopMulti-ModeMicroplateReader, emission wavelength: 525nm, reference wavelength: 515nm, sample pipetting volume amount: 50 μ l/ holes).The calculating of result: by exciting rate and the EC of GraphPadPrism5 computed in software sample
50value.
1.3.2 the appetite inhibiting of rat and the experiment of body weight growth inhibition
1.3.2.1 the appetite inhibiting experiment of rat
SD male rat conforms three days, is divided at random three groups (n=6) afterwards, and wherein one group as blank group, and other three groups is administration group, blank group lumbar injection solvent (3%DMSO+97%H
2o), after the administering medical liquids of administration group lumbar injection variable concentrations respectively, 1h enters 12h night, 12h light cycle; To weigh after administration 0 respectively, 3,6,12, remain Mus grain weight to calculate the food ration of rat in different time sections to obtain the average food ration of rat in different time sections after 24h; The appetite suppressant activity of sample is drawn by following formulae discovery:
Suppression ratio (%)=(W
blank group– W
administration group)/W
blank group× 100%
1.3.2.2 rat body weight growth inhibition is tested
SD male rat, conforms three days, is divided at random three groups (n=6) afterwards, and wherein one group as blank group, and other two groups is administration group, blank group lumbar injection solvent (3%DMSO+97%H
2o), the medicinal liquid of administration group difference lumbar injection variable concentrations, is administered once every 24h, and successive administration 7 days weighs rat body weight and also notes down before each administration.Respectively respectively is organized comparing to obtain and often organize rat average weight rate of increase before the average weight of rat and administration every day:
Body weight rate of increase (%)=(W
after administration– W
before administration)/W
before administration× 100%
Administration group rat body weight rate of increase is organized rat and compared to obtain with blank the suppression situation that medicine increases rat average weight: body weight growth inhibition rate (%)=blank organizes body weight rate of increase (%) – administration group body weight rate of increase (%)
2. experimental result
2.1 saikosides are to 5-HT
2Cthe agonist activity of receptor
Table 1. saikoside is to 5-HT
2Cthe agonist activity of receptor
* the EC of positive drug 5-hydroxy tryptamine
50value is 0.52 ± 0.21nM; The exciting rate of all compounds measures under the concentration conditions of 333 μ g/ml
2.2 Radix Bupleuri total saponin are to the appetite of rat and body weight growth inhibition effect (see Fig. 2), and Fig. 2 shows Radix Bupleuri total saponin and increases (B) inhibitory action (n=6) * P<0.05 compared with blank group to the appetite (A) of rat with body weight.
2.3saikosaponina (2) is to the appetite of rat and body weight growth inhibition effect (see Fig. 3).Fig. 3 shows saikosaponina (2) and increases (B) inhibitory action (n=6) * P<0.05 compared with blank group to the appetite (A) of rat with body weight; * is P<0.01 compared with blank group.
3. conclusion
Experimental result shows that saikoside is to 5-HT
2Creceptor has obvious agonist activity, EC
50value is between 18.38 and 147.41 μMs; In zoopery, Radix Bupleuri total saponin increases inhibited to the appetite of rat and body weight under the dosage of 3.0/kg, 9.0mg/kg (lumbar injection); Therefrom be separated the compound saikosaponina (2) that obtains under the dosage of 3.0/kg, 6.0mg/kg (lumbar injection), after administration 24h, 39.1% and 69.2% are respectively to the suppression ratio of rat food ration, body weight growth inhibition rate after administration 7d is respectively 13.6% and 16.4%, all higher than Radix Bupleuri total saponin.
Carry out to illustrate further medicine of the present invention composition by the following examples, but do not limit essentiality content of the present invention with this.
Embodiment 1:
The preparation of Radix Bupleuri total saponin and monomer saikoside compounds:
Get Radix Bupleuri BupleurumchinenseDC medical material (6.0kg) to pulverize, 70%EtOH reflux, extract, three times, merge extractive liquid, is concentrated into small size, D101 macroporous resin column chromatography, uses water, 70%EtOH, EtOH eluting successively, 70%EtOH elution fraction Rp-18 reversed phase column chromatography, MeOH-H
2o (1:9 → 10:0) eluting obtains Radix Bupleuri total saponin (150g), the various pillar layer separation of Radix Bupleuri total saponin obtains following monomer saikoside compounds 3-O-β-D-fucopyranosylsaikogeninf (1, 60mg), saikoside a (saikosaponina, 2, 2.1g), 6 "-O-acetylation saikoside a (6 "-O-acetylsaikosaponina, 3, 84mg), 3 ", 6 "-two-O-saikoside as (3 ", 6 "-di-O-acetylsaikosaponina, 4, 0.2g), saikoside d (saikosaponind, 5, 234mg), saikoside e (saikosaponine, 6, 102mg), saikoside b
1(saikosaponinb
1, 7,330nmg), bavin saikoside g (saikosaponing, 8,96mg).
Embodiment 2:
By obtained Radix Bupleuri total saponin or monomer saikoside compounds or saikosaponina (2), after dissolving with a small amount of DMSO, inject routinely with water, fine straining, injection is made in embedding sterilizing.
Embodiment 3:
By obtained Radix Bupleuri total saponin or monomer saikoside compounds or saikosaponina (2), after dissolving with a small amount of DMSO, be dissolved in sterile water for injection, be stirred to dissolve, filter with aseptic suction funnel, aseptic fine straining again, is sub-packed in ampoule, and after frozen drying, aseptic sealing by fusing obtains injectable powder.
Embodiment 4:
By obtained Radix Bupleuri total saponin or monomer saikoside compounds or saikosaponina (2), add excipient in itself and excipient weight than the ratio for 9:1 respectively, make powder.
Embodiment 5:
By obtained Radix Bupleuri total saponin or monomer saikoside compounds or saikosaponina (2), add excipient, pelletizing press sheet in itself and excipient weight than the ratio for 5:1 respectively.
Embodiment 6:
By obtained Radix Bupleuri total saponin or monomer saikoside compounds or saikosaponina (2), oral liquid method for making makes oral liquid routinely respectively.
Embodiment 7:
By obtained Radix Bupleuri total saponin or monomer saikoside compounds or saikosaponina (2), add excipient in itself and excipient weight than the ratio for 5:1, make capsule.
Embodiment 8:
By obtained Radix Bupleuri total saponin or monomer saikoside compounds or saikosaponina (2), add excipient in itself and excipient weight than the ratio for 3:1, make capsule.
Embodiment 9:
By obtained Radix Bupleuri total saponin or monomer saikoside compounds or saikosaponina (2), add excipient in itself and excipient weight than the ratio for 5:1 respectively, make granule.
Claims (11)
1. the application of Radix Bupleuri total saponin in the medicine preparing prevention or treatment of obesity.
2. the application of Radix Bupleuri total saponin as claimed in claim 1 in the medicine preparing prevention or treatment of obesity, it is characterized in that described Radix Bupleuri total saponin is prepared by following method and obtains: get Radix Bupleuri BupleurumchinenseDC, pulverize, 70%EtOH reflux, extract, three times, merge Radix Bupleuri extracting solution, be concentrated into small size, D101 macroporous resin column chromatography, use water, 70%EtOH, EtOH eluting successively; 70%EtOH elution fraction through Rp-18 reversed phase column chromatography, the MeOH-H of 1:9 → 10:0
2o eluting obtains Radix Bupleuri total saponin.
3. the application of Radix Bupleuri total saponin as claimed in claim 1 in the medicine preparing prevention or treatment of obesity, is characterized in that described application is that Radix Bupleuri total saponin passes through 5-HT
2Creceptor agonism and appetite inhibiting effect reach prevention or treatment of obesity, and in Radix Bupleuri extracting solution, Radix Bupleuri total saponin content is 20-70% weight.
4. the application of Radix Bupleuri total saponin as claimed in claim 1 in the medicine preparing prevention or treatment of obesity, it is characterized in that described Radix Bupleuri total saponin comprises the saponins compound 3-O-β-D-fucopyranosylsaikogeninf (1) being not less than 0.1% weight, saikoside a (saikosaponina, 2), 6 "-O-acetylation saikoside a (6 "-O-acetylsaikosaponina, 3), 3 ", 6 "-two-O-saikoside as (3 ", 6 "-di-O-acetylsaikosaponina, 4), saikoside d (saikosaponind, 5), saikoside e (saikosaponine, 6), saikoside b
1(saikosaponinb
1, 7), bavin saikoside g (saikosaponing, 8),
5. the application of Radix Bupleuri total saponin as claimed in claim 1 in the medicine preparing prevention or treatment of obesity, is characterized in that described Radix Bupleuri total saponin comprises the saikoside a being not less than 0.1% weight.
6. the application of saikoside a in the medicine preparing prevention or treatment of obesity.
7. the application of saikoside a as claimed in claim 6 in the medicine preparing prevention or treatment of obesity, it is characterized in that described saikoside a is prepared by following method and obtains: get Radix Bupleuri BupleurumchinenseDC, pulverize, 70%EtOH reflux, extract, three times, merge extractive liquid, be concentrated into small size, D101 macroporous resin column chromatography, use water, 70%EtOH, EtOH eluting successively; 70%EtOH elution fraction Rp-18 reversed phase column chromatography, the MeOH-H of 1:9 → 10:0
2o eluting obtains Radix Bupleuri total saponin; Radix Bupleuri total saponin is through silica gel column chromatography, and the CHCl3-MeOH eluting of 9:1, obtains saikoside a.
8. the application of saikoside a as claimed in claim 6 in the medicine preparing prevention or treatment of obesity, is characterized in that described application is that saikoside a passes through 5-HT
2Creceptor agonism and appetite inhibiting effect reach prevention or treatment of obesity.
9. the application of saikoside a as claimed in claim 6 in the medicine preparing prevention or treatment of obesity, is characterized in that described saikoside a is as the sole active agent in medicine.
10. the pharmaceutical composition of prevention or treatment of obesity, it comprises is prepared by following method and the Radix Bupleuri total saponin obtained, get Radix Bupleuri BupleurumchinenseDC, pulverize, 70%EtOH reflux, extract, three times, merge extractive liquid, is concentrated into small size, D101 macroporous resin column chromatography, uses water, 70%EtOH, EtOH eluting successively; 70%EtOH elution fraction Rp-18 reversed phase column chromatography, the MeOH-H of 1:9 → 10:0
2o eluting obtains Radix Bupleuri total saponin, and pharmaceutically acceptable carrier,
Described Radix Bupleuri total saponin comprises the saponins compound 3-O-β-D-fucopyranosylsaikogeninf (1), the saikoside a (saikosaponina that are not less than 0.1% weight; 2), 6 "-O-acetylation saikoside a (6 "-O-acetylsaikosaponina; 3), 3 "; 6 "-two-O-saikoside as (3 "; 6 "-di-O-acetylsaikosaponina; 4), saikoside d (saikosaponind; 5), saikoside e (saikosaponine, 6), saikoside b
1(saikosaponinb
1, 7), saikoside g (saikosaponing, 8),
Or described Radix Bupleuri total saponin comprises the saikoside a (saikosaponina, 2) being not less than 0.1% weight.
11. comprise using saikoside a as sole active agent, and the prevention of pharmaceutically acceptable carrier or the pharmaceutical composition for the treatment of of obesity.
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Cited By (1)
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| CN113995765A (en) * | 2021-10-29 | 2022-02-01 | 中国药科大学 | Medical application of saikosaponin D in promoting subcutaneous white fat browning to prevent or treat obesity |
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| KR20150067937A (en) * | 2013-12-11 | 2015-06-19 | 대구한의대학교산학협력단 | Composition comprising a saikosaponin a for prevention and treatment of obesity |
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