CN1363367A - Active components of Chinese-medicinal medicine with weight-losing and hypolipemic actions and its relative medicine - Google Patents

Abstract

The active hypolipemic components in 40 Chinese-medicinal materials and their relative medicines are disclosed. Said active components can suppress the activity of fatty acid synthetase and the differentiation from profat cells to fat cells and activate the activity of acyl-CoA synthetase. Said medicines feature high effect and low toxic by-effect.

Description

The active component and the relative medicine that have fat-reducing and antihyperglycemic in the part Chinese herbal medicine

Technical field:

The invention belongs to natural medicine technical field, relate in particular to the active skull cap components and the relative medicine that are used for Weight-reducing and lipid-lowering.

Background technology:

Obesity is a global medical problem.Existing a large amount of evidences show fat closely related with multiple disease, as hypertension, and hyperlipidemia, diabetes, cardiovascular and cerebrovascular disease, breast carcinoma, infertility, children's intelligence is low inferior.With BMI (Body Mass Index) male greater than 27.8, the women is greater than 27.3 as obesity standard, the population of being obese sum is about 7,000 ten thousand in the present 18-74 of China year population, accounts for 5.8% of population; Population of being obese sum is about 6,800 ten thousand in U.S.'s population of the same age, accounts for 20% of population.About 10,000,000,000 yuans of the consumption total value that China is used to lose weight every year and obesity-related disease is treated, the U.S. then is 1,000 hundred million dollars.China's population of being obese ratio increases rapidly at present, and it is more and more outstanding that the puppy fat problem has seemed.

The exploitation of slimming medicine is main according to two principles in the world at present: the first, and appetite-suppressing is such as sibutramine (sibutramine); The second, reduce absorption, such as Orlistat (orlistat).The two also is only two appetrol on the present Chinese market, and the former commodity Qu Mei by name can be elegant and difficult to understand bent light, latter's commodity celestial Buddhist nun's gram by name.The side effect of the two is fairly obvious, and sibutramine causes xerostomia, cardiopalmus, weak, and Orlistat causes oiliness just and fat-soluble avitaminosis.Western countries are also developing slimming medicine according to new principle always, such as, find that xanthine derivative class material can add the macro-energy expenditure by accelerating the vivo oxidation metabolism, a large amount of clinical trial proof caffeine (caffeine), ephedrine (ephedrine) uses separately or unites to use has certain fat-reducing effect, but because it can cause the side effect of tachycardias and cardiopalmus not obtain clinical permission always; Mice ob expression of gene product leptin (leptin) is found and cloned to middle nineteen nineties in last century, and prove that its rat for the genotype obesity has certain antiobesity action, but the individuality of genotype obesity only accounts for the 5-10% of obese individuals sum, and cause serious local congestion and swelling pain during this material drug administration by injection, therefore also so far for obtaining clinical permission.In sum, the main weak point of existing slimming medicine is that side effect is big and clinical effective rate is low, and to design not enough science relevant and these 2 deficiencies are all with drug target.

Chinese herbal medicine is the drug resource of Chinese unique advantage, records the example of a large amount of Chinese herbal medicine Weight-reducing and lipid-lowerings at all times in the classic of TCM.But because the Chinese herbal medicine active component is indeterminate, pharmacological mechanism is unclear to wait restriction, and traditional Chinese herbal medicine can not be gone to the world, therefore China's slimming medicine of also not having independent intellectual property right so far.Beijing in 2000 world obesity and fat-reducing conference propose to develop as early as possible the target that China has the Weight-reducing and lipid-lowering new drug of independent intellectual property right.

Summary of the invention:

The objective of the invention is to solve the existing shortcoming that the slimming medicine clinical effective rate is low, side effect is big, a kind of target spot design science is provided, thus the slimming medicine that side effect is little, clinical effective rate is high.

Technical scheme of the present invention is as follows:

In the following Chinese herbal medicine to fatty acid synthetase (fatty acid synthase, FAS) activity has the combination of inhibiting all the components and composition; To fatty acyl-CoA synthetase (acyl-CoA synthase, ACS) activity has all the components of activation and composition combination; Preceding adipose cell (preadipocyte) to mice, rat or people has inhibiting all the components and composition combination to adipose cell (adipocyte) differentiation:

Fructus Jujubae, Radix Et Rhizoma Rhei, Fructus Crataegi, oolong tea, Radix Oenotherae erythrosepalae, Stigma Maydis, Radix Glycyrrhizae, CitrusaurantiumL.Var.amara Engl., the Rhizoma Pinelliae, Radix Rehmanniae, Semen Cassiae, Radix Angelicae Sinensis, Flos Carthami, Fructus Hordei Germinatus, Pericarpium Zanthoxyli, Aloe, Radix Polygoni Multiflori, Ganoderma, Pericarpium Citri Reticulatae, Folium Ilicis, Flos Jasmini Sambac, Folium Acanthopanacis Senticosi, Rhizoma Polygoni Cuspidati, Herba Apocyni veneti, Rhizoma Alismatis, Herba Artemisiae Scopariae, Radix Rubiae, Poria, gynostemma pentaphyllum, Fructus Lycii, Fructus Gardeniae, Folium Nelumbinis, Radix Bupleuri, Radix Scutellariae, the Radix Astragali, Rhizoma Coptidis, Flos Chrysanthemi, Folium Ginkgo, Folium Sennae, Radix Puerariae

These active component or its combination have significant fat-reducing and antihyperglycemic, and part combination or whole combination in the said herbal medicine can be mixed with Weight-lossing hypolipemic medicine.

The authentication method of related activity composition is in the said herbal medicine:

One, identify whether to contain in the Chinese herbal medicine have the method for inhibiting active component to be to fatty acid synthetase:

1. separation and purification rat body fat acid enzyme:

Reach testis fat on every side around winning subcutaneous rat, kidney, merge, shred.The 0.25M sucrose solution that adds about 3 times of volumes, homogenate.Homogenate centrifugal 60 minutes in 100000 * g is got supernatant, is the FAS crude extract.In this crude extract, add solid ammonium sulfate to 25% saturation while stirring, continue to stir 10 minutes, centrifugal 10 minutes of 12000 * g discards precipitation, adds solid ammonium sulfate to 40% saturation in supernatant again, stirred 15 minutes, centrifugal collecting precipitation is dissolved in and contains 1mM DTT in right amount, 1mM EDTA, in the 4mM kaliumphosphate buffer of pH7.0, be the FAS of purification.More than operation is all carried out under 0-4 ℃.

2. the water extract or the ethanol extraction that prepare Chinese herbal medicine:

A, water extract preparation:

Each single Chinese herbal medicine is drunk sheet, prefabricated, pulverizing.Add 5 times of volume distilled water, boiled 30 minutes, 8 layers of white filtered through gauze are got clear liquid; Sediment adds 5 times of volume distilled water again, boils 30 minutes, and 8 layers of white filtered through gauze are got clear liquid.Twice clear liquid merges lyophilization.Gained dry powder is dissolved in an amount of distilled water, obtains pale brown color or brownish red transparency liquid extract, measure soluble solid content, make in each time extraction of each single Chinese herbal medicine and be stabilized in 30-100mg/ml with the evaporated under reduced pressure method.This extract is preserved down for 2-8 ℃ muddy the appearance more than 72 hours.

B, ethanol extraction preparation:

Each single Chinese herbal medicine is drunk sheet, prefabricated, pulverizing.Dehydrated alcohol refluxes 3 times, and backflow merges, and obtains pale brown color or brownish red transparency liquid extract, measures soluble solid content with the evaporated under reduced pressure method, makes in each time extraction of each single Chinese herbal medicine and is stabilized in 20-40mg/ml.

3. set up fatty acid synthetase and survey live body system, in surveying live body system, add Chinese herbal medicine extract, carry out the fatty acid synthetase activity and suppress experiment, calculate the inhibition degree, confirm whether contain the active composition of inhibition fatty acid synthetase in the Chinese herbal medicine.

Set up fatty acid synthetase and survey live body system: use spectrophotography.Surveying live body is cumulative volume 1.0ml, comprises that reaction starts thing malonyl coenzyme A 0.05ml.The enzyme amount that depends on the NADPH oxidation of malonyl coenzyme A with 37 ℃ of following per minute catalysis 1.0 μ mol is the unit of activity of FAS, and the unit of activity number that every milligram of pheron contains is the ratio vigor (u/mg) of FAS.

Carrying out active inhibition of fatty acid synthetase tests: add Chinese herbal medicine water extract or ethanol extraction in surveying live body system, make itself and enzyme effect add start material after 5 minutes.The extracts of Chinese herbal medicine addition is that every milliliter of survey live body is 5 μ l extracts of Chinese herbal medicine, is contrast with 5 μ l distilled waters or dehydrated alcohol.Calculate the inhibition degree, confirm to have inhibiting active component.

Two, identify whether to contain in the Chinese herbal medicine have the method for the active component of activation to be to fatty acyl-CoA synthetase:

1. separation and purification liver tissues of rats fatty acyl-CoA synthetase:

Win the about 200g of rat liver, chopping.The 0.25M sucrose solution that adds about 3 times of volumes, homogenate.Homogenate centrifugal 10 minutes in 600 * g, deposit seed places the 0.25M sucrose solution recentrifuge of about 3 times of volumes again, and the two times centrifugal supernatant merges.With 230000 * g centrifugal 60 minutes, get precipitation; Precipitation is suspended in (this mixed liquor contains 5mM Triton X-100,50mM pH7.4 kaliumphosphate buffer, 5mM beta-mercaptoethanol and 1mM EDTA in an amount of mixed liquor, the about 4.5mg/ml of protein concentration), left standstill 1 hour centrifugal 60 minutes of 230000 * g, get supernatant, be the ACS crude extract.The solution dilution ACS crude extract that contains 2mMTriton X-100 and 5mM beta-mercaptoethanol with about 5 times of volumes, with Blue-Sepherose chromatographic column (CL-6B on the diluent, 2.6 * 18cm) with Buffer A (the 100mM sodium phosphate that contains 10mM ATP and 0.8M NaCl of 5 times of volumes, the 25mM potassium citrate, pH7.0) wash post, with the Buffer A eluting that contains 10mM ATP and 0.8M NaCl, flow velocity 15ml/ hour, every 15ml collected at last.The part that will contain maximum enzyme activity merges, and is the ACS of purification.More than operation is all carried out under 0-4 ℃.

2. preparation Chinese herbal medicine water extract or ethanol extraction: method is with fatty acid synthetase is carried out step in the molecular level screening technique as target spot.

3. set up fatty acyl-CoA synthetase and survey live body system, in surveying live body system, add Chinese herbal medicine water extract or ethanol extraction, carry out the active activation experiment of fatty acyl-CoA synthetase, the computing activation degree confirms whether contain the active component that fatty acyl-CoA synthetase is had activation in the Chinese herbal medicine.

Set up fatty acyl-CoA synthetase and survey live body system: use isotope method.Surveying live body is cumulative volume 1.0ml, comprises that reaction starts thing coenzyme A 0.05ml.Generate 1.0 μ mol C with 35 ℃ of following per minutes ¹⁴The enzyme amount of-labelling Palmic acid coenzyme A is represented the unit of activity of ACS, and the unit of activity number that contains with every milligram of pheron is represented the ratio vigor (u/mg) of ACS.

Carry out the active activation experiment of fatty acyl-CoA synthetase: in surveying live body system, add Chinese herbal medicine water extract or ethanol extraction, make itself and enzyme effect add start material after 5 minutes.The extracts of Chinese herbal medicine addition is that every milliliter of survey live body is 5 μ l extracts of Chinese herbal medicine, is contrast with 5 μ l distilled waters or dehydrated alcohol.The computing activation degree confirms whether contain the active component that fatty acyl-CoA synthetase is had activation in the Chinese herbal medicine.

Three, identify whether to contain in the Chinese herbal medicine have the method for inhibiting active component to be to the mature fat cell differentiation to adipose cell before mice, rat or the people:

1. preparation Chinese herbal medicine water extract or ethanol extraction: method is with fatty acid synthetase is carried out step in the molecular level screening technique as target spot.

2. carry out mice, rat or the differentiation of people's adipose cell and suppress experiment, detect the repressed degree of cell differentiation, inhibiting active component is arranged thereby confirm whether to contain in the Chinese herbal medicine pair cell differentiation.Method can for:

Adipose cell before mice, rat or the people is inoculated in 96 orifice plates with certain density, cultivates with growth medium is conventional.Changing division culture medium after cell converges into, and add the extracts of Chinese herbal medicine of variable concentrations, is contrast with the distilled water or the dehydrated alcohol of equal volume, cultivated 6 days, during change liquid as required.Measure fat content in the cell with the oil red O stain method, determine differentiation degree, detect the repressed degree of cell differentiation, inhibiting active component is arranged thereby confirm whether to contain in the Chinese herbal medicine pair cell differentiation in conjunction with cellular morphology.

According to the method described above, we have carried out Preliminary Identification to the related activity composition in described 40 kinds of Chinese herbal medicine, these 40 kinds of Chinese herbal medicine extracts are to fatty acid synthetase (fatty acid synthase, FAS) active inhibitory action, to fatty acyl-CoA synthetase (acyl-CoA synthase, ACS) active activation, mice, rat or people's preceding adipose cell (preadipocyte) is seen Table 1 to the inhibitory action of adipose cell (adipocyte) differentiation, the number of "+" in the table is represented its size to the index of correlation influence.

Table 1:

The Chinese herbal medicine title	Inhibitory action to FAS		Activation to ACS		The adipose cell differentiation suppresses
							Water extract	Alcohol extract	Water extract	Alcohol extract	Water extract	Alcohol extract
	Fructus Jujubae				+
Radix Et Rhizoma Rhei							++	++++				+++
	Fructus Crataegi				+
Oolong tea							++	+				++
	Radix Oenotherae erythrosepalae			+
Stigma Maydis									+++
	Radix Glycyrrhizae	++
CitrusaurantiumL.Var.amara Engl.										+
	The Rhizoma Pinelliae				+
Radix Rehmanniae							+
	Semen Cassiae	+++				++
Radix Angelicae Sinensis								+
	Flos Carthami			+	+
Fructus Hordei Germinatus									+
	Pericarpium Zanthoxyli			+	+
Aloe							++	+				+
	Radix Polygoni Multiflori				+
Ganoderma									+
	Pericarpium Citri Reticulatae	++	+										++
Folium Ilicis							+++					++
	Flos Jasmini Sambac	+
Radix Et Caulis Acanthopanacis Senticosi							+
	Rhizoma Polygoni Cuspidati				+
Herba Apocyni veneti							+			+
	Rhizoma Alismatis		+
Herba Artemisiae Scopariae							++	++				+
	Radix Rubiae		+
Poria							+
	Herb Gynostemmae Pentaphylli	++											+
Fructus Lycii									+	+
	Fructus Gardeniae			+
Folium Nelumbinis							++	++
	Radix Bupleuri		++
Radix Scutellariae							+
	The Radix Astragali		+
Rhizoma Coptidis							+
	Flos Chrysanthemi	+++											++
Folium Ginkgo							+
	Folium Sennae	+	+
Radix Puerariae										+

Inhibition fatty acid synthetase, activation fatty acyl-CoA synthetase that contains in the above-mentioned table 1 of reference pair each Chinese herbal medicine and the prompting that suppresses the active component of adipose cell differentiation are depended on pine torch 300g, oolong tea 180g, Flos Chrysanthemi 150g, Pericarpium Citri Reticulatae 150g, Stigma Maydis 120g.Choosing is chosen, is mixed.Added the 2000ml water boil 30 minutes, with 8 layers of white filtered through gauze; Place 1500ml water to boil once more 30 minutes medicinal residues, filter.Twice filtrate merges, and lyophilization obtains about 180g dry powder.The animal effect experiment is divided into 6 groups: negative control, the contrast of high fat, positive control 1, positive control 2, low dose group, high dose group.Negative control is a normal diet, high fat contrast adds yolk powder, cholesterol, Adeps Sus domestica for normal diet, positive control 1 adds Qu Mei for high lipid food, positive control 2 adds Xuezhikang for high lipid food, low dose group is that high lipid food adds 500mg and tried thing/kg body weight/sky, and high dose group is that high lipid food adds 3000mg and tried thing/kg body weight/sky.Every single cage of rat is raised, and experimental period is 35 days.

Test item is that body weight (BWFE) after the preceding body weight (BWSE) of the experiment of every rat, the experiment, weight increase (IBW), experiment back fatty heavy (BFFE), fat body are than (PBFBW), total foodstuff consumption (TAIF), food utilization (GIBWGFI, IPBFGFI), serum levels of triglyceride (TG), T-CHOL (TC), low density lipoprotein, LDL (LDL), fatty tissue fatty acid synthetase (FAS) activity and hepatic tissue fatty acyl-CoA synthetase (ACS) activity.

The effect experiment result shows that the above-mentioned thing that tried can obviously reduce rat body weight, body fat amount, serum levels of triglyceride and T-CHOL amount, and can significantly suppress FAS and ACS activity.It loses weight and the effect of body fat weight is better than Qu Mei, and its effect that reduces TG, TC and LDL is better than Xuezhikang.The Weight-reducing and lipid-lowering experimental result of five kinds of Chinese herbal medicine extracts sees Table 2-5.

Table 2: Qu Mei and Xuezhikang be to BWFE, IBW, and BFFE, PBFBW, TG, TC and LDL influences Groups BWSE BWFE IBW BFFE PBFBW TG TC LDL

(g) (g) (g) (g) (%) mmol.L ^-1Mmol.L ^-1Mmol.L ^-1B ₁49.6 340.3 290.7 24.4 7.17 3.26 3.40 0.32 B ₂47.8 328.2 280.4 26.0 7.92 3.34 4.31 0.38 B ₃46.8 310.3 263.5 23.4 7.54 2.93 3.07 0.27 B ₄55.0 344.1 289.1 28.8 8.37 3.60 3.78 0.39 B ₅45.4 301.4 256.0 22.3 7.40 3.08 3.44 0.32 B ₆48.2 325.6 277.4 24.9 7.65 3.55 3.57 0.28 B ₇52.2 335.0 282.7 25.2 7.52 3.19 3.15 0.30 B ₈46.0 315.5 269.5 26.7 8.46 3.81 3.99 0.40average, 48.9 325.1 276.2 25.2 7.75 3.35 3.59 0.33 ± s, 3.281 14.989 12.260 2.008 0.460 0.292 0.420 0.051 C ₁54.4 279.0 224.6 21.8 7.81 2.50 3.34 0.29 C ₂46.8 290.3 243.5 23.0 7.92 2.88 3.77 0.36 C ₃56.0 291.8 235.8 20.8 7.13 3.75 3.52 0.37 C ₄50.7 258.6 207.9 17.7 6.84 3.14 2.80 0.32 C ₅45.3 255.0 209.7 18.4 7.22 3.33 3.03 0.41 C ₆46.7 260.7 214.0 17.8 6.83 3.69 3.49 0.36 C ₇48.1 244.0 195.9 17.9 7.34 2.97 3.28 0.40 C ₈45.8 248.9 203.1 18.5 7.43 2.81 3.94 0.31average 49.2 266.0 ^*216.8 ^*19.5 ^*7.32 ^*3.13 3.40 0.35 ± s, 4.062 18.537 16.461 2.075 0.402 0.435 0.371 0.043 D ₁48.6 318.8 270.2 23.1 7.25 2.66 2.33 0.22 D ₂51.9 340.7 288.6 25.0 7.34 2.43 1.64 0.24 D ₃46.5 334.9 288.4 24.2 7.23 2.28 2.52 0.17 D ₄54.3 335.6 281.3 24.6 7.33 1.98 2.40 0.25 ^#D ₅44.8---------D ₆46.0 306.2 260.2 21.1 6.89 2.74 1.88 0.27 D ₇47.2 320.0 272.8 22.6 7.06 2.14 1.76 0.19 D ₈45.3 308.3 263.0 22.0 7.14 2.19 2.09 0.18average 48.1 323.5 274.9 23.2 ^*7.18 ^*2.35 ^*2.09 ^*0.22 ^*± s 3.373 13.765 11.512 1.438 0.161 0.279 0.340 0.038#: rat D ₅Unexpected dead in experiment.

Table 3: tried thing to BWFE, IBW, BFFE, PBFBW, TG, TC and LDL influences Groups BWSE BWFE IBW BFFE PBFBW TG TC LDL

(g) (g) (g) (g) (%) mmol.L ^-1Mmol.L ^-1Mmol.L ^-1B ₁49.6 340.3 290.7 24.4 7.17 3.26 3.40 0.32 B ₂47.8 328.2 280.4 26.0 7.92 3.34 4.31 0.38 B ₃46.8 310.3 263.5 23.4 7.54 2.93 3.07 0.27 B ₄55.0 344.1 289.1 28.8 8.37 3.60 3.78 0.39 B ₅45.4 301.4 256.0 22.3 7.40 3.08 3.44 0.32 B ₆48.2 325.6 277.4 24.9 7.65 3.55 3.57 0.28 B ₇52.2 335.0 282.7 25.2 7.52 3.19 3.15 0.30 B ₈46.0 315.5 269.5 26.7 8.46 3.81 3.99 0.40average, 48.9 325.1 276.2 25.2 7.75 3.35 3.59 0.33 ± s, 3.281 14.989 12.260 2.008 0.460 0.292 0.420 0.051 E ₁52.0 310.8 258.8 21.1 6.79 3.27 2.93 0.18 E ₂45.6 290.5 244.9 20.0 6.88 3.00 2.47 0.37 E ₃47.3 320.3 272.9 21.0 6.56 2.75 3.13 0.26 E ₄46.8 299.0 252.2 22.3 7.46 2.96 2.36 0.28 E ₅54.5 295.4 240.9 20.4 6.91 2.67 3.20 0.41 E ₆49.2 315.4 266.2 21.7 6.88 3.44 3.12 0.35 E ₇45.0 301.5 256.5 19.5 6.47 2.89 3.44 0.33 E ₈56.1 322.1 266.0 22.7 7.05 3.05 3.01 0.29average 49.6 306.9 ^*257.3 ^*21.09 ^*6.88 ^*3.00 ^*2.96 ^*0.31 ± s 4.183 11.897 11.019 1.110 0.303 0.255 0.368 0.072 F ₁45.8 297.0 251.2 17.8 5.99 1.35 2.05 0.24 F ₂53.0 294.5 241.5 16.7 5.67 1.68 1.89 0.26 F ₃55.2 293.0 237.8 17.3 5.90 1.61 2.11 0.19 F ₄45.8 288.4 242.6 16.9 5.85 1.48 1.73 0.28 F ₅49.3 306.8 257.5 17.6 5.74 1.84 2.18 0.39 F ₆48.1 311.2 263.1 19.2 6.17 1.26 1.69 0.22 F ₇56.5 313.9 257.4 21.5 6.85 1.82 2.33 0.34 F ₈51.1 317.9 266.8 18.0 5.66 2.01 2.75 0.38average 50.6 302.8 ^*252.2 ^*18.125 ^*5.98 ^*1.63 ^*2.09 ^*0.29 ± s 4.071 10.979 10.704 1.565 0.391 0.258 0.345 0.075 tables 4: tried thing, Qu Mei and Xuezhikang to TAIF, GIBWGFI and IPBFGFI influences Groups TAIF GIBWGFI IPBFGFI Groups TAIF GIBWGFI IPBFGFI

(g)?????????(g)???(％，×10 ^-3)????????????(g)????????(g)?????(％×10 ^-3)?B ₁??????709.5??????0.4097???10.1057???????D ₁??????591.7?????0.4566????12.2528?B ₂??????677.2??????0.4141???11.6952???????D ₂??????710.4?????0.4063????10.3322?B ₃??????639.0??????0.4124???11.7997???????D ₃??????703.7?????0.4098????10.2743?B ₄??????688.4??????0.4200???12.1586???????D ₄??????706.1?????0.3984????10.3810?B ₅??????650.1??????0.3938???11.3829?????? ^#D ₅????—?????????????????—?????????????????—?B ₆??????633.4??????0.4380???12.0777???????D ₆??????598.5?????0.4348????11.5121?B ₇??????700.3??????0.4037???10.7383???????D ₇??????638.4?????0.4273????11.0589?B ₈??????632.8??????0.4259???13.3692???????D ₈??????628.6?????0.4184????11.3586average???666.3??????0.415????11.666????????average??653.9?????0.422 ^*???11.024 ^**?±s??????31.263?????0.014????0.979?????????±s??????51.986????0.020?????0.743?C ₁??????489.6??????0.4587???15.9518???????E ₁??????660.0?????0.3921????10.2879?C ₂??????584.4??????0.4167???13.5534???????E ₂??????561.0?????0.4365????12.2638?C ₃??????681.5??????0.3460???10.4622???????E ₃??????671.6?????0.4063????9.7677?C ₄??????486.5??????0.4273???14.0596???????E ₄??????587.6?????0.4292????12.6957?C ₅??????555.7??????0.3774???12.9926???????E ₅??????624.0?????0.3861????11.0737?C ₆??????718.2??????0.2980???9.5099????????E ₆??????585.6?????0.4546????11.7486?C ₇??????434.9??????0.4504???16.8774???????E ₇??????608.4?????0.4216????10.6345?C ₈??????428.5??????0.4740???17.3396???????E ₈??????633.1?????0.4202????11.1357average???547.4 ^**???0.406 ^**?13.843 ^**?????average??616.4 ^**??0.418?????11.201 ^**?±s??????108.520????0.061????2.852?????????±s??????38.165????0.023?????0.992

F ₁??????577.8?????0.4348????10.3669

F ₂??????601.3?????0.4016????9.4296

F ₃??????537.4?????0.4425????10.9788

F ₄??????609.0?????0.3984????9.6059

F ₅??????638.6?????0.4032????8.9884

F ₆??????571.0?????0.4608????10.8056

F ₇??????594.6?????0.4329????11.5203

F ₈??????619.7?????0.4305????9.1335

average??593.7 ^**??0.426 ^**??10.104 ^**

± s 31.447 0.022 0.943# rat D ₅Unexpected dead in experiment.Table 5: tried thing, Qu Mei and Xuezhikang to FAS and the active Groups of the influence FAS of ACS specific activity (u/mg) FAS relative activity ACS specific activity (u/mg) ACS relative activity B ₂210 413B ₄249 1.000 390 1.000B ₆238 382average, 232.3 395.0C ₂222 443C ₄207 0.907 398 1.061C ₆203 416average, 210.7 419.0D ₂217 500D ₄229 0.938 472 1.224D ₆208 478average, 218.0 483.3E ₂190 645E ₄156 0.758 530 1.422E ₆182 510average, 176.0 561.7F ₂109 1050F ₄118 0.505 973 2.455F ₆125 886average 117.3 969.7

Advantage of the present invention and good effect: the present invention identifies the inhibition fatty acid synthetase that contains in some Chinese herbal medicine, the active component that activates fatty acyl-CoA synthetase and the differentiation of inhibition adipose cell first; The combination of these active component has tangible fat-reducing and antihyperglycemic; Its fat-reducing and antihyperglycemic mainly synthesizes, promotes steatolysis and the preceding adipose cell of inhibition to realize to the mature fat cell differentiation by suppressing body fat.

The present invention can be used to develop the preparation Weight-reducing and lipid-lowering natural drug that functional component is clear and definite, mechanism is reliable, clinical effective rate is high, toxic and side effects is little.

Embodiment:

With reference to the prompting that the table 1 in the summary of the invention part provides, depend on pine torch 300g, oolong tea 180g, Flos Chrysanthemi 150g, Pericarpium Citri Reticulatae 150g, Stigma Maydis 120g.Choosing is chosen, is mixed.Added the 2000ml water boil 30 minutes, with 8 layers of white filtered through gauze; Place 1500ml water to boil once more 30 minutes medicinal residues, filter.Twice filtrate merges, and lyophilization obtains about 180g dry powder.This dry powder contains and suppresses fatty acid synthetase, activates fatty acyl-CoA synthetase and suppresses the active component that adipose cell breaks up, and has fat-reducing and antihyperglycemic.

Claims (4)

1. in following each single Chinese herbal medicine the fatty acid synthetase activity there is the combination of corresponding composition in inhibiting composition or the Chinese medicine medicines:

Fructus Jujubae, Radix Et Rhizoma Rhei, Fructus Crataegi, oolong tea, Radix Oenotherae erythrosepalae, Stigma Maydis, Radix Glycyrrhizae, CitrusaurantiumL.Var.amara Engl., the Rhizoma Pinelliae, Radix Rehmanniae, Semen Cassiae, Radix Angelicae Sinensis, Flos Carthami, Fructus Hordei Germinatus, Pericarpium Zanthoxyli, Aloe, Radix Polygoni Multiflori, Ganoderma, Pericarpium Citri Reticulatae, Folium Ilicis, Flos Jasmini Sambac, Folium Acanthopanacis Senticosi, Rhizoma Polygoni Cuspidati, Herba Apocyni veneti, Rhizoma Alismatis, Herba Artemisiae Scopariae, Radix Rubiae, Poria, gynostemma pentaphyllum, Fructus Lycii, Fructus Gardeniae, Folium Nelumbinis, Radix Bupleuri, Radix Scutellariae, the Radix Astragali, Rhizoma Coptidis, Flos Chrysanthemi, Folium Ginkgo, Folium Sennae, Radix Puerariae.

2. in following each single Chinese herbal medicine the fatty acyl-CoA synthetase activity there is the combination of corresponding composition in the composition of activation or the Chinese medicine medicines:

Fructus Jujubae, Radix Et Rhizoma Rhei, Fructus Crataegi, oolong tea, Radix Oenotherae erythrosepalae, Stigma Maydis, Radix Glycyrrhizae, CitrusaurantiumL.Var.amara Engl., the Rhizoma Pinelliae, Radix Rehmanniae, Semen Cassiae, Radix Angelicae Sinensis, Flos Carthami, Fructus Hordei Germinatus, Pericarpium Zanthoxyli, Aloe, Radix Polygoni Multiflori, Ganoderma, Pericarpium Citri Reticulatae, Folium Ilicis, Flos Jasmini Sambac, Folium Acanthopanacis Senticosi, Rhizoma Polygoni Cuspidati, Herba Apocyni veneti, Rhizoma Alismatis, Herba Artemisiae Scopariae, Radix Rubiae, Poria, gynostemma pentaphyllum, Fructus Lycii, Fructus Gardeniae, Folium Nelumbinis, Radix Bupleuri, Radix Scutellariae, the Radix Astragali, Rhizoma Coptidis, Flos Chrysanthemi, Folium Ginkgo, Folium Sennae, Radix Puerariae.

3. the preceding adipose cell to mice, rat or people in following each single Chinese herbal medicine breaks up the combination that corresponding composition in inhibiting composition or the Chinese medicine medicines is arranged to adipose cell:

Fructus Jujubae, Radix Et Rhizoma Rhei, Fructus Crataegi, oolong tea, Radix Oenotherae erythrosepalae, Stigma Maydis, Radix Glycyrrhizae, CitrusaurantiumL.Var.amara Engl., the Rhizoma Pinelliae, Radix Rehmanniae, Semen Cassiae, Radix Angelicae Sinensis, Flos Carthami, Fructus Hordei Germinatus, Pericarpium Zanthoxyli, Aloe, Radix Polygoni Multiflori, Ganoderma, Pericarpium Citri Reticulatae, Folium Ilicis, Flos Jasmini Sambac, Folium Acanthopanacis Senticosi, Rhizoma Polygoni Cuspidati, Herba Apocyni veneti, Rhizoma Alismatis, Herba Artemisiae Scopariae, Radix Rubiae, Poria, gynostemma pentaphyllum, Fructus Lycii, Fructus Gardeniae, Folium Nelumbinis, Radix Bupleuri, Radix Scutellariae, the Radix Astragali, Rhizoma Coptidis, Flos Chrysanthemi, Folium Ginkgo, Folium Sennae, Radix Puerariae.

4. Weight-lossing hypolipemic medicine is characterized in that it being in the following Chinese herbal medicine being that preparation of raw material forms partly or entirely:

Fructus Jujubae, Radix Et Rhizoma Rhei, Fructus Crataegi, oolong tea, Radix Oenotherae erythrosepalae, Stigma Maydis, Radix Glycyrrhizae, CitrusaurantiumL.Var.amara Engl., the Rhizoma Pinelliae, Radix Rehmanniae, Semen Cassiae, Radix Angelicae Sinensis, Flos Carthami, Fructus Hordei Germinatus, Pericarpium Zanthoxyli, Aloe, Radix Polygoni Multiflori, Ganoderma, Pericarpium Citri Reticulatae, Folium Ilicis, Flos Jasmini Sambac, Folium Acanthopanacis Senticosi, Rhizoma Polygoni Cuspidati, Herba Apocyni veneti, Rhizoma Alismatis, Herba Artemisiae Scopariae, Radix Rubiae, Poria, gynostemma pentaphyllum, Fructus Lycii, Fructus Gardeniae, Folium Nelumbinis, Radix Bupleuri, Radix Scutellariae, the Radix Astragali, Rhizoma Coptidis, Flos Chrysanthemi, Folium Ginkgo, Folium Sennae, Radix Puerariae.