CN102058678B - Medicine or health-care food composition for treating fatty liver - Google Patents

Medicine or health-care food composition for treating fatty liver Download PDF

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CN102058678B
CN102058678B CN2010105818831A CN201010581883A CN102058678B CN 102058678 B CN102058678 B CN 102058678B CN 2010105818831 A CN2010105818831 A CN 2010105818831A CN 201010581883 A CN201010581883 A CN 201010581883A CN 102058678 B CN102058678 B CN 102058678B
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fatty liver
extract
radix rhei
rhei emodi
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CN102058678A (en
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王曙
耿向东
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Tibet Jinhada Pharmaceutical Co., Ltd.
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Abstract

The invention provides new application of rheum australe or extract thereof, in particular to application of the rheum australe or extract thereof in the preparation of medicine or health-care food for preventing or/and treating the fatty liver. The invention also provides new application of 3,5,3'4'-tetrahydroxy toluylene-4'-O-beta-D-glucoside which is a component of the rheum australe. The invention further provides a medicament or health-care food composition for treating fatty liver. By improving the resistance of insulin, enhancing the sensitiveness to insulin in a rat body, reducing lipid mobilization, reducing or eliminating the oxidation overload of liver cell, the medicine or health-care food composition for treating fatty liver reduces blood fat, improves the liver function, protects the liver cell and finally achieves the function for treating the fatty liver.

Description

A kind of medicine or health-care food composition for the treatment of fatty liver
Technical field
The present invention relates to the new purposes of Radix Rhei emodi or its extract, particularly, be in the preparation prevention or/and the medicine for the treatment of fatty liver or the purposes in the health food.
Background technology
Radix Rhei emodi Rheum emodi Wall. is root and the rhizome of Polygonaceae Rheum ripple leaf group plant, and sour in the mouth, hardship are cold in nature, mainly are distributed in the ground such as Tibet, Qinghai, Sichuan and Yunnan, all are wild.The Tibetan medicine claims bent prick (Quza), in be used for the treatment of gastroenteritis, be used for hemostasis outward, control skin ulcer, antiinflammatory, wound healing mouth (Liu Bing, etc., the chemical constitution study of Radix Rhei emodi, West China Journal of Pharmaceutical Sciences, 1 phase of 22 volumes in 2007).Find again in recent years its have good blood fat reducing and hypoglycemic effect (Li Junlin, Wang Zhibin, Li Jiashi, the research of Radix Rhei emodi hypoglycemic activity. " Chinese crude drug ", 1997,20 (5): 249-250.).
The Radix Et Rhizoma Rhei kind is a lot, just has more than 40 to plant in China.The Radix Et Rhizoma Rhei that China's nineteen ninety version pharmacopeia is recorded has 3 kinds: sorrel Rheum palmatum L. Rheum tanguticum R.tanguticumMaxim.Ex Balf. or Rheum officinale R.officinale Baill. are called genuine rhubarb; The kind of other Rheum comprises that Radix Rhei emodi all classifies non-genuine rhubarb as, it is generally acknowledged that non-genuine rhubarb should not be medicinal as genuine rhubarb.Radix Et Rhizoma Rhei and Radix Rhei emodi all derive from the root and rhizome of Polygonaceae Rheum plant, and to contain a large amount of anthraquinone components as feature, only Radix Rhei emodi does not contain chrysophanic acid and glycosides (Li Junlin thereof, Deng, Radix Et Rhizoma Rhei and Radix Rhei emodi microscopic quantity are differentiated, " Chinese crude drug ", 5 phases of 19 volumes in 1996).Li Jiudan research thinks that Radix Rhei emodi is different from certified products with Rheum hotaoense C. Y. Cheng et C. T. Kao, does not have Tongli and captures effect; It is medicinal that " the Radix Et Rhizoma Rhei pharmacognostical study " of Guo Jixian thinks that also non-genuine rhubarb should not be made certified products, this be since the composition of non-genuine rhubarb on quality and quantity with genuine rhubarb different or lay particular stress on to some extent due to.
Radix Et Rhizoma Rhei (refers to that the plant origin that pharmacopeia is recorded is dry rhizome and the root of sorrel, Rheum officinale and Rheum tanguticum, be so-called genuine rhubarb, give birth to product Radix Et Rhizoma Rhei or slap leaf group Radix Et Rhizoma Rhei) main effective ingredient be anthraquinone analog compound, include the dianthracene quinone that strongly causes the effect of letting out, if any Sennoside A, B, C, D, E, F etc.; Stilbene methods of glycosides content is few, and do not contain 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides (seeing: the modern study of Radix Et Rhizoma Rhei: medical publishing society of Peking University, Zheng Junhua, fruit Dean in October, 2007 P361).And strongly do not cause the dianthracene quinones of the effect of letting out in the contained anthraquinone of Radix Rhei emodi (for ripple leaf group Radix Et Rhizoma Rhei), and its main component should be the stilbene methods of glycosides, comprise 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides.The dianthracene quinones is fully different from stilbene glycoside pharmacologically active, and further specifying present Radix Rhei emodi can not be as the reason of genuine rhubarb use.
Fatty liver is that a kind of multi-pathogenesis causes, the pathological changes main body lobules of liver, in the hepatocyte neutral fat abnormal deposition as main clinical syndrome.Along with socio-economic development, the fatty liver prevalence rate increases rapidly, has now become one of three large hepatopathys of harm humans health, there is no so far specific medicament.At present, the scholar generally acknowledges in the industry, and the structure type of natural drug and activity are extremely abundant, and having demonstrated is having very large potentiality aspect the treatment fatty liver, and especially there be Chinese medicine and the ethnic drug of long applicating history in China, is worth actively conscientious research and development.At present, still not be not used for the treatment of the relevant report of fatty liver about Radix Rhei emodi, also not about 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides is used for the treatment of the relevant report of fatty liver.
Summary of the invention
Technical scheme of the present invention has provided the new purposes of Radix Rhei emodi.Another technical scheme of the present invention has provided a kind of new purposes of chemical compound.
The invention provides Radix Rhei emodi or its extract prevents or/and the medicine for the treatment of fatty liver or the purposes in the health food in preparation.
Further preferably, described medicine is that prevention is or/and the medicine for the treatment of non-alcoholic fatty liver disease.
Wherein, described Radix Rhei emodi is root or the rhizome of Polygonaceae Rheum ripple leaf group plant Rheum emodi Wall..
Wherein, described Radix Rhei emodi extract be Radix Rhei emodi water or extractive with organic solvent.
Wherein, described Radix Rhei emodi extract is the Radix Rhei emodi ethanol extraction.
Wherein, contain chemical compound in the described Radix Rhei emodi extract: 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-weight percentage of O-β-D-Glucose glycosides is 30%~99.8%.
The present invention also provides chemical compound as shown in Equation 1 to prevent or/and the medicine for the treatment of fatty liver or the purposes in the health food in preparation
Figure BSA00000380847100021
Formula 1,
Wherein, R 1For
Figure BSA00000380847100022
Or H.
Further preferably, described chemical compound is 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides, its structural formula is as follows:
Figure BSA00000380847100031
The present invention also provides a kind of medicine or health-care food composition for the treatment of fatty liver, it is to be active component by the chemical compound shown in the Radix Rhei emodi of effective dose or its extract or the formula 1, adds that pharmaceutically acceptable adjuvant or complementary composition are prepared into preparation pharmaceutically commonly used.
Wherein, described preparation is solid or liquid dosage form.
The present invention with the Radix Rhei emodi extract (contain 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides is more than 30%) and 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides is primary raw material, the medicine of preparation treatment fatty liver.Modern pharmacological research proves, the mixture of isolating stilbene glycosides compound or multiple compounds from Polygonaceae Rheum plant Radix Rhei emodi has good therapeutical effect and health care for the patient's of fatty liver and hyperlipemia crowd, and takes safety.Medicine of the present invention is by improving insulin resistant, increases in the rat body the sensitivity of insulin, reduces lipid mobilization, and alleviate or relieving liver cellular oxidation overload, thereby blood fat reducing, improve liver function, the protection hepatocyte, thus reach the effect for the treatment of fatty liver.
Obviously, according to foregoing of the present invention, according to ordinary skill knowledge and the customary means of this area, not breaking away under the above-mentioned basic fundamental thought of the present invention prerequisite, can also make modification, replacement or the change of other various ways.
The specific embodiment
Below test and data thereof only are exemplary, the scope of this patent do not consisted of any restriction, what those skilled in the art and scientific research personnel understood should be: under condition without departing from the spirit and scope of the present invention, can make amendment or replace the details of technical solution of the present invention, as change chemical compound 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-extracting method of O-β-D-Glucose glycosides and change the molecular structure etc. of chemical compound.But these modifications and replacement all fall in protection scope of the present invention.
The extracting method of embodiment 1 Radix Rhei emodi extract
Preparation technology's flow process of Radix Rhei emodi extract is: it is an amount of to get the Radix Rhei emodi medical material, and medicinal material coarse powder is crossed 20 mesh sieves after pulverizing, and adds 80% soak with ethanol 30h, with 7mlmin again -1The flow velocity percolation extract, with 4 times of column volumes, 80% ethanol elution eluting, the collection eluent is evaporated to dried, namely obtains the Radix Rhei emodi extract.
Embodiment 2 monomeric compounds 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-the O-β-extraction of D-Glucose glycosides, separation
In the Radix Rhei emodi 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-preparation technology's flow process of O-β-D-Glucose glycosides (PDG) is: the coarse powder of getting after the Radix Rhei emodi pulverizing medicinal materials is crossed 20 mesh sieves, adds 80% soak with ethanol 30h, with 10mlmin -1The flow velocity percolation extract, with 4 times of column volume 80% ethanol elutions, the collection eluent is evaporated in right amount.Get concentrated solution with 4 times of volume petroleum ether (60~90 ℃ of boiling ranges) extraction repeatedly, collect the water layer residue.Water intaking layer residue, with ethyl acetate extraction (ratio is 1: 1), extraction repeatedly obtains acetic acid ethyl ester extract and water layer residue.Getting acetic acid ethyl ester extract is partially soluble in a small amount of distilled water, take by weighing 40 times of the about example weight of 100-200 order polyamide, adopt wet method dress post, adopt water, 10% ethanol, 20% ethanol, 30% ethanol, 40% ethanol as gradient eluent, each gradient is collected merging 30% ethanol and 40% ethanol elution part with 4 times of column volume eluent eluting, be evaporated to a certain amount of, with 1.5 times of ethyl acetate extractions repeatedly, collect acetic acid ethyl acetate extract, be concentrated into the dried solids that obtains.200-300 order silicagel column on the solids dry method, adopt chloroform-methanol system eluting, adopt chloroform, chloroform methanol (12: 1), chloroform methanol (5: 1), chloroform methanol (3: 1), methanol to carry out gradient elution, 4 times of column volume eluting of each gradient, collect the eluent part of chloroform methanol (5: 1), the recovery solvent is evaporated to dried, namely obtains the PDG sterling.
3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides (PDG) structure elucidation
Figure BSA00000380847100041
Formula 2:3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides
White amorphous powder (ethanol).Point places aobvious bluish violet fluorescence under the uviol lamp (365nm) on silica gel thin-layer plate. 13The CNMR spectrum provides 14 unsaturated carbon signals and hexose signal. 1HNMR δ 4.77 (1H, d, J=7.2Hz, anomeric-H) and 13CNMR δ 104.1,78.2,77.6,74.8, and 71.3,62.4 infer and are β-D-Glucose. 1Two phenyl ring that the HNMR spectrum provides trans olefinic proton (δ 6.83,6.92, each 1H, J=16Hz, olefinic H) and 3 fragrant protons are respectively arranged, a ring is ABX type signal, and (δ 7.02,1H, d, J=2Hz, H-2 '; δ 6.93,1H, dd, J=8.4,2Hz, H-6 '; δ 7.15,1H, d, J=8.4Hz, H-5 '), another ring is AX 2(δ 6.44,2H, d, J=2Hz, H-2,6 for the type signal; δ 6.16,1H, t, J=2Hz, H-4).Acid hydrolysis detects glucose and piceatannol, 1HNMR and 13CNMR data and bibliographical information piceatannol-4 '-O-β-D-glucopyranoside is consistent, so be accredited as 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides.
Monomeric compound 3,5,3 in the embodiment 3 Radix Rhei emodi extracts of the present invention ', 4 '-tetrahydroxystilbene-4 '-assay of O-β-D-Glucose glycosides (PDG)
The preparation precision of reference substance solution takes by weighing 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides sterling is an amount of, and add methanol and be mixed with in contrast product solution of solution that every 1ml contains 0.4mg approximately.
It is an amount of, accurately weighed that dry Radix Rhei emodi extract is got in the preparation of need testing solution, puts in the tool plug conical flask, the accurate methanol 25ml that adds, weighed weight, supersound process (150W, 40kHz) 40min, let cool, weighed weight is supplied the weight that subtracts mistake with methanol again, shakes up, filter, get subsequent filtrate and namely get need testing solution.
Chromatographic condition and system suitability condition are take octadecylsilane chemically bonded silica as filler, and the detection wavelength is 320nm, and mobile phase is acetonitrile-water (12: 88), and flow velocity is 1.0mlmin -1, column temperature is 30 ℃, number of theoretical plate by 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides peak calculates and should be not less than 3000.3,5,3 ', 4 '-tetrahydroxystilbene-4 '-separating degree of O-β-D-Glucose glycosides main peak and other impurity peaks should reach requirement.
Algoscopy is accurate reference substance solution 10 μ l and the sample solution 5 μ l injection liquid chromatographies drawn respectively, measure, and get final product.
Concrete outcome is as follows:
In the table 1 Radix Rhei emodi extract 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides content (%)
Sample number into spectrum Sampling (g) Chromatographic peak area Content (%)
1 0.5971 613599 30.54
2 0.4897 748213 37.24
3 0.2985 1227399 61.09
4 0.2672 1371255 68.25
5 0.1932 1896451 94.39
6 0.1843 1988471 98.97
Below prove beneficial effect of the present invention by concrete pharmacodynamics test.
Test example 1 toxicity trial of the present invention
1 experiment material
Laboratory animal: the ICR mice, male, body weight 18~22g provides the (quality certification number: 1037764) by Sichuan University's West China Experimental Animal Center.
Experimental agents: 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-(PDG presses the method for embodiment 2 and extract acquisition, content: 92.80%) from the Radix Rhei emodi medical material O-β-D-Glucose glycosides.
2 test methods and result
Medicine of the present invention is carried out acute toxicity test as test specimen to mouse gavaging.The result shows: the maximum tolerated dose of mouse gavaging medicine of the present invention is 20g/kg/24h, becomes 1000 times of human oral consumption per day (1.2g/60kg/24h) for the 60kg body weight; The disposable LD that gavages of mice 50Be 15.2g/kg, 95% confidence limit is 22.60~34.23g/kg.Long term toxicity test shows, rat gavages medicine 0.4 of the present invention, 0.8,1.6g/kg (be equivalent to clinical amount 20,40,80 times) every day, hematology, blood biochemical are learned index, organ coefficient and the more equal no significant difference of matched group after 24 weeks, and pathological examination results also has no the pathologic change that health food causes.Stop using the invention medicine after 2 weeks, and the indices of each administration group and blank group compare, and all no significant difference points out this medicine without obvious retardance toxicity.Illustrate that medicine long-term taking of the present invention also is safe.
Test example 23,5,3 '; 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides and Radix Rhei emodi extract (contain 3; 5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides is more than 30%) the rats with nonalcoholic fatty liver disease protective effect is tested
1 experiment purpose: estimate the Radix Rhei emodi extract and (contain 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides is more than 30%) and monomeric compound 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides is on the impact of rats with nonalcoholic fatty liver disease blood fat, liver function and insulin resistant.
2 laboratory animals: 60 of healthy adult SD rats, body weight 190~220g, the SPF level provides the (quality certification number: 1037951) by Sichuan University's Experimental Animal Center.
3 Experimental agents and reagent:
The Radix Rhei emodi extract (by embodiment 1 preparation, wherein, contain 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides 30%); 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-(extract acquisition from the Radix Rhei emodi medical material, content: 92.80%), fenofibrate is available from U.S. sigma company for O-β-D-Glucose glycosides.Cholesterol is available from Xinjin, Chengdu people's livelihood biochemistry factory, and the ELISA test kit is available from Chengdu one section's instrument equipment company limited, and Adeps Sus domestica, rat normal feedstuff and high lipid food provide by Sichuan University's Experimental Animal Center.
4 experimental techniques
The SD rat is normal to be fed after 7 days, be divided at random normal group (A) and two groups of model group (M), normal group gives standard feed, model group gives high lipid food and feeds, after feeding for 6 weeks, from normal group and SD rat of model group random choose, get liver and do pathological section respectively, confirm that non-alcoholic fatty liver disease forms.Again the model group rat is divided into 8 groups at random: blank model group (B), 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-the high, medium and low dosage group of O-β-D-Glucose glycosides (dosage is respectively: C1:160mg/kgd, C2:80mg/kgd and C3:40mg/kgd), fenofibrate group (D), Radix Rhei emodi extract group (is prepared by embodiment 1 method, dosage is respectively: E1:180mg/kgd, and E2:90mg/kgd and E3:50mg/kgd).Normal group continues to feed with standard feed, and all the other each groups are fed with the preparation high lipid food, continue for 7 weeks.After 7 weeks, A group, B group give the normal saline gavage, and C1, C2, C3, E1, E2, E3 organize respectively with the relative medicine gavage.The D group is with 100mg/kgd fenofibrate suspension oral gavage.Administration time continued for 3 weeks.
5 experimental results
5.1 liver is character observation substantially
Normal group (A) rat liver peplos is smooth complete, and surface color is dark red, smoothness, and medium hardness, clear-cut margin, the sense of tangent plane fine grained is without greasy feeling.The all surface jaundice of blank model group (B) rat liver, liver volume obviously increases, and peplos is nervous.3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides group (C1, C2 and C3 group) liver color is dark red, more moist, and tangent plane is without greasy feeling.Fenofibrate group volume slightly increases, and color is dark red, part tangent plane greasy feeling.E1, E2 and E3 group, the liver color is dark red, more moist, and tangent plane is without greasy feeling.Fenofibrate group volume slightly increases, and color is dark red, part tangent plane greasy feeling.
5.2 hepatic pathology is observed
Normal group (A) hepatocyte lobules of liver clear in structure, hepatocyte radially distributes centered by central vein towards periphery, and endochylema is the red state that dyes of uniformity, and sinus hepaticus is high-visible, liver rope marshalling.Model group (B) swelling of liver cell, part of hepatocytes are the balloon sample and become.As seen differ in size in most hepatocyte, the fat that quantity differs drips cavity, liver rope arrangement disorder.3,5,3 ', 4 '-tetrahydroxystilbene-4 '-its fat drop of O-β-D-Glucose glycosides group (C1, C2 and C3 group) and model group obviously reduce, density is rare, sinus hepaticus is clear, and liver rope marshalling is without inflammatory cell infiltration, Radix Rhei emodi extract group (E1, E2 and E3 organize) compare with model group its fat drop and model group obviously reduce, density is rare, and sinus hepaticus is clear, liver rope marshalling.Fenofibrate group (D) is steatosis obviously, and fat drop glue model group is little, and density is slightly rare, and swelling of liver cell is misaligned.
5.3 respectively organize rat ALT, AST relatively
Experimental result find 3,5,3 of heavy dose of and middle dosage ', 4 '-tetrahydroxystilbene-4 '-when O-β-D-Glucose glycosides and model group comparison, can reduce significantly ALT and AST; In the Radix Rhei emodi extract group, E1 and E2 group can reduce ALT and AST significantly, and significant difference is arranged during with the model group comparison.The results are shown in Table 2.
Table 2 PDG and Radix Rhei emodi extract are on the impact of each group Liver Function
Figure BSA00000380847100081
Figure BSA00000380847100082
*P<0.01 He *Compare with model group (B) P<0.05, △ △P<0.01 He Compare with normal group (A) P<0.05.
5.4 respectively organize rat TG, TC, LDL-C, HDL-C relatively
Experimental result is found 3 of heavy dose of and middle dosage (C1 and C2 group), 5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides and model group be relatively the time, can reduce significantly TG, TC and LDL-C, and can significantly improve the content of HDL-C, its small dose group can reduce TG content significantly; And Radix Rhei emodi extract group and B model group be relatively the time, and E1 and E2 group can reduce TG, TC and LDL-C significantly, and can significantly improve the content of HDL-C, the results are shown in Table 3.
Table 23,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides and extract be to each group rat TG, TC, LDL-C, HDL-C comparison sheet
Figure BSA00000380847100083
Figure BSA00000380847100084
*P<0.01 He *Compare with model group P<0.05, △ △P<0.01 He Compare with normal group P<0.05.
5.5 respectively organize FBG, FNS, IR, ISI relatively
Model group FBG, FNS, IR, ISI and normal group difference all have statistical significance (P<0.01, P<0.01, P<0.01, P<0.01), 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides high dose group and every significant difference P<0.01 that all exists of model group, P<0.01, P<0.01), middle dosage group FBG, FNS, every significant difference (P<0.01 that also all exists of IR and model group, P<0.01, P<0.01), fenofibrate group and model group are relatively at FBG, FNS, IR also exists significant significant difference (P<0.01, P<0.05, and Radix Rhei emodi extract E1 and E2 group also all has significant difference during with the comparison of B model group P<0.01).See Table 4.
Table 43,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides and extract be on the impact of each group Insulin Resistance of Rats
Figure BSA00000380847100091
Figure BSA00000380847100092
*P<0.01 He *Compare with model group P<0.05, △ △P<0.01 He Compare with normal group P<0.05.
Test example 3 Radix Rhei emodi extracts and 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides reduces the fat content test of Models of Fatty Liver mouse liver
One experiment material
Laboratory animal: the ICR mice, male, body weight 18~22g is provided by Sichuan University zoopery center.
Experiment reagent and medicine: the Radix Rhei emodi extract (by embodiment 1 method preparation, contain 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides 30%); Monomeric compound 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-(PDG extracts from the Radix Rhei emodi medical material and obtains content: 98.80%) O-β-D-Glucose glycosides; Fenofibrate, triglyceride test kit and T-CHOL test kit are available from U.S. sigma company; Cholesterol is available from Xinjin, Chengdu people's livelihood biochemistry factory, and rat normal feedstuff and high lipid food provide by Sichuan University's Experimental Animal Center.
Two experimental techniques
All ICR mices were all fed for 2 weeks (14 days) with high lipid food, then be divided at random Normal group (A), model group (B), PDG high dose group (C1:160mg/kg), dosage group (C2:80mg/kg) among the PDG, PDG low dose group (C3:40mg/kg) and fenofibrate positive controls (D), Radix Rhei emodi extract group (dosage is respectively: E1:200mg/kg, E2:100mg/kg and E3:50mg/kg).Since the 10th day, C1, C2, C3, E1, E2 and E3 be gavage respectively, and A group usefulness waits capacity normal saline gavage, and the D group is processed with the fenofibrate gavage of 100mg/kg.Successive administration 4 days, every day 1 time.Administration is after 24 hours the last time, takes out mouse liver, weigh, and homogenate, high speed centrifugation is got the content that supernatant is measured triglyceride and T-CHOL in the hepatic tissue.
Three experimental results
Experimental result shows monomeric compound 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides (PDG) and Radix Rhei emodi extract (contain 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-O-β-D-Glucose glycosides is more than 30%) have an effect that reduces the content of triglyceride and T-CHOL in the Models of Fatty Liver mouse liver.It the results are shown in Table 5.
Table 5PDG and Radix Rhei emodi extract are on triglyceride and total cholesterol level impact in the Models of Fatty Liver mouse liver
Figure BSA00000380847100101
Figure BSA00000380847100102
*P<0.01 He *Compare with model group P<0.05, △ △P<0.01 He Compare with normal group P<0.05.
In sum, Radix Rhei emodi extract of the present invention and formula 1 chemical compound have the fatty liver protective effect, are particularly useful for treatment or/and the prevention non-alcoholic fatty liver disease; can reduce hepatic fat content, clinical use safety, effectively; stability is strong, provides a kind of new medication to select for clinical.

Claims (2)

1. the Radix Rhei emodi extract prevents or/and the medicine for the treatment of fatty liver or the purposes in the health food in preparation; Contain chemical compound in the described Radix Rhei emodi extract: 3,5,3 ', 4 '-tetrahydroxystilbene-4 '-weight percentage of O-β-D-Glucose glycosides is 30%~99.8%.
2. purposes according to claim 1 is characterized in that: described medicine is that prevention is or/and the medicine for the treatment of non-alcoholic fatty liver disease.
3, purposes according to claim 1 and 2 is characterized in that: described Radix Rhei emodi is Polygonaceae Rheum ripple leaf group plant Rheum emodiWall. root or rhizome.
4, purposes according to claim 1 and 2 is characterized in that: water or extractive with organic solvent that described Radix Rhei emodi extract is Radix Rhei emodi.
5, purposes according to claim 4 is characterized in that: described Radix Rhei emodi extract is the Radix Rhei emodi ethanol extraction.
6, as shown in Equation 1 chemical compound in preparation prevention or/and the medicine for the treatment of fatty liver or the purposes in the health food
Figure 2010105818831100001DEST_PATH_IMAGE001
Formula 1,
Wherein, R 1For
Figure 928311DEST_PATH_IMAGE002
Or H.
7, purposes according to claim 6 is characterized in that: described chemical compound is:
8, a kind of medicine or health-care food composition for the treatment of fatty liver, it is characterized in that: it is to be active component by the chemical compound shown in the Radix Rhei emodi of effective dose or its extract or the formula 1, adds that pharmaceutically acceptable adjuvant or complementary composition are prepared into preparation pharmaceutically commonly used.
9, medicine according to claim 8 or health-care food composition is characterized in that: described preparation is solid or liquid dosage form.
CN2010105818831A 2010-12-10 2010-12-10 Medicine or health-care food composition for treating fatty liver Active CN102058678B (en)

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CN102225097B (en) * 2011-06-25 2013-02-20 西藏金哈达药业有限公司 Application of extract of Rheum emodi Wall. in preparing anti-fibrosis drug
CN102491869B (en) * 2011-12-07 2014-07-23 中国科学院西北高原生物研究所 Rheumlikiangense extract with liver injury protection activity and preparation method thereof
CN102526227A (en) * 2012-01-13 2012-07-04 西藏金哈达药业有限公司 Use of Rheum emodi extract for preparing drugs for preventing and treating fatty liver diseases
CN102614204A (en) * 2012-03-12 2012-08-01 中国人民解放军第四军医大学 New application of stilbene glucoside to hangover alleviation
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CN104147026A (en) * 2014-08-20 2014-11-19 安树君 New application of resveratrol derivative
CN104761594B (en) * 2015-04-24 2018-01-02 昆药集团股份有限公司 A kind of amorphous state Quzhazhigan and preparation method thereof
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