CN100345538C - Use of ampelopsin for preparing blood sugar reducing medicine - Google Patents
Use of ampelopsin for preparing blood sugar reducing medicine Download PDFInfo
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Abstract
The present invention discloses a medicine composition for reducing blood sugar. The present invention is characterized in that the medicine composition contains ampelopsin with the effective dosage for reducing blood sugar and medicinal acceptable excipient, and the composition preferably contains 2 to 98 wt% of ampelopsin. The present invention also discloses a preparation method of the composition and an application of the ampelopsin in the process of preparing a medicine for reducing blood sugar.
Description
The invention belongs to field of medicaments.
Document Walter Karrerr, Birkhauser Verlag, Bassel undstuttgart (1958), P.652, NO:1640 discloses the structural formula of ampelopsin,
But the activity of ampelopsin is not studied fully.
The inventor is surprisingly found out that ampelopsin has purposes widely at field of medicaments.
The inventor is surprisingly found out that ampelopsin has blood sugar lowering and effect for reducing blood fat, can be prepared into blood sugar lowering and hypolipidemic.Ampelopsin can directly be used as medicine, can also make pharmaceutical composition with pharmaceutical acceptable carrier or mixed with excipients.The ampelopsin that wherein preferably contains 2% to 98% weight ratio adds pharmaceutical acceptable carrier or excipient to 100% weight ratio.Can also be in prior art be mixed with pharmaceutical composition with the compatible active constituents of medicine of ampelopsin, wherein said compatible active constituents of medicine is the flavonoid medicine preferably, and described flavonoid medicine is ampelopsin preferably.Flavonoid medicament contg and ampelopsin content weight ratio can be 2-80: 20-98 in the compositions.The present composition can be prepared into tablet, granule, capsule, medicine for external use.The dosage that preferred active component is used the people is 0.01-5 gram/kg body weight/sky, but also can decide as the case may be, is not limited to this scope.
The regular convention formula of tablet can be: ampelopsin 10%-90% weight ratio, and lactose 90%-10% weight ratio randomly adds an amount of sodium carboxymethyl cellulose, magnesium stearate, 50% ethanol is an amount of.The regular convention formula of electuary can be: ampelopsin 5-100% weight ratio, and (sucrose+dextrin) 95-0% weight ratio, sucrose: dextrin=2: 1, randomly add an amount of other auxiliary agent, total amount is 100%.Capsular regular convention formula can be: ampelopsin 10-100% weight ratio, and starch 90-0% weight ratio randomly adds an amount of other auxiliary agent, and total amount is 100%.But those skilled in the art also can be mixed with other dosage form with technology well known in the art and carrier as required.
Ampelopsin can extract from ampelopsis, also can prepare with above-mentioned document disclosed method.Described ampelopsis comprises ampelopsis cantoniensis, a leaf beautiful Fructus Vitis viniferae, Ampelopsis grossedentata, Cayratia japonica (Thunb.) Gagnep., Radix Ampelopsis, Northeastern Caulis seu folium ampelopsis brevipedunculatae and Vitis Amurensis.Described extracting method can be: decoct vitaceae by all kinds of solvents (water and/or organic solvent), decoct one or many, decoction liquor is through concentrating cooling, standing over night, detect the active ingredient of precipitation and supernatant, get and have active precipitation, after chromatographic isolation, obtain ampelopsin thing of the present invention.Decoct used solvent preferred water, alcohols, esters, ketone, ethers and strong polar organic solvent, more preferably low-level chain triacontanol, low-grade fatty acid ester has ketone and ether and/or water, the most preferably methanol of 3-12 carbon atom, ethanol, propanol, isopropyl alcohol, n-butyl alcohol, isobutanol, sec-butyl alcohol, the tert-butyl alcohol, ethyl acetate, methyl acetate, Ethyl formate, acetone, methyl ethyl ketone, ether, methyl ethyl ether, methyl tertiary butyl ether(MTBE), dichloromethane, chloroform, carbon tetrachloride, dimethyl sulfoxine, N, dinethylformamide and/or water or the like.The chromatographic isolation filler can be a polyamide, polyacrylamide, macroporous adsorbent resin, cation exchange resin, anion exchange resin, preferred polyamide, polyacrylamide, macroporous adsorbent resin, more preferably polyamide.
Principle of the present invention is to follow the trail of the drug activity of ampelopsin by setting up the pharmacological screening model, finds its pharmaceutical usage.The evidence ampelopsin has blood sugar lowering and effect for reducing blood fat.
Ampelopsin can be mixed with pharmaceutical composition by conventional preparation technique of drug world and carrier.The present composition can be prepared into tablet, granule, capsule, medicine for external use.But those skilled in the art also can be mixed with other dosage form with technology well known in the art and carrier as required.
Describe the present invention in detail by the following examples.But should be appreciated that these embodiment just illustrate the present invention, rather than in office where face limits the scope of the invention.
Embodiment 1: tablet:
Ampelopsin 25g,
Lactose 53g,
Sodium carboxymethyl cellulose 1.5g,
Magnesium stearate 0.5g,
50% ethanol 5ml
Said components is mixed the back compacting in flakes in mixer.
Embodiment 2: syrup
Ampelopsin 100g,
Sucrose 20g,
Dextrin 10g,
Ethanol 50ml
Mix mentioned component and obtain syrup.
Embodiment 3: electuary
Ampelopsin 55g,
Icing Sugar 345g,
Dextrin 145g,
Ethanol 5ml
Said components is mixed after drying, obtains electuary.
Embodiment 4: capsule
Ampelopsin 200g,
Starch 20g,
Behind the said components mix homogeneously, incapsulate.
Embodiment 5: tablet:
Ampelopsin 5g,
Ampelopsin 30g
Lactose 53g,
Sodium carboxymethyl cellulose 1.5g,
Magnesium stearate 0.5g,
50% ethanol 5ml
Said components is mixed the back compacting in flakes in mixer.
Embodiment 6: electuary
Ampelopsin 520g,
Icing Sugar 350g,
Dextrin 150g,
Ethanol 10ml
Said components is mixed after drying, obtains electuary.
The hypoglycemic test of example 7 ampelopsins
1. materials and methods
1.1. tried thing: the crude drug (wherein the content of ampelopsin is 73%) that contains ampelopsin
1.2. experimental animal and testing conditions
Select the female Kunming mouse of healthy cleaning level for use, body weight 24 ± 2g, animal feed operative norm GB14924-94.Sense environmental conditions, temperature range 20-25 ℃, relative humidity scope 40-70%.
1.3. dosage is selected
Test divides intact animal and two batches of hyperglycemia model animals to carry out, and respectively establishes 1 matched group (distilled water) and is tried thing 0.25,0.50,1.50g/kg dosage group, is equivalent to 5,10 and 30 times of people's recommended intake respectively, irritates the stomach amount and is 0.1ml/10g.
1.4. key instrument and reagent
Alloxan (Alloxan): Sigma company; 50% glucose injection: new Cao in Yancheng pharmaceutical factory.
The super blood sugar detection instrument of SUPER GLUCOCARD II GT-1640 type: Japanese capital person first science Co., Ltd. produces: the GLUCOCARD blood sugar test paper: Japanese capital person first science Co., Ltd. produces.
1.5. experimental technique
1.5.1. intact animal: fasting was got mice and is surveyed blood glucose after 5 hours.40 of the mice of screening fasting glucose in normal range are divided into four groups at random by blood sugar level, 10 every group, are respectively each dosage group of normal control group and sample (difference is not more than 1.1mmol/L between group) "
1.5.2. hyperglycemia model animal: strict fasting is after 24 hours, mouse tail vein injection alloxan 50mg/kgBW, and fasting is 5 hours after 6 days, surveys blood glucose.The mice 40 of screening fasting blood sugar＞10mmol/L is done, and is divided into four groups at random by blood sugar level, 10 every group, is respectively each dosage group of model control group and sample (difference is not more than 1.1mmol/L between group).
1.5.3. the mensuration of fasting glucose and carbohydrate tolerance: by design dosage mice continuous irrigation stomach was tried thing 30 days, fasting is 5 hours then, gives glucose 1.5g/kgBW and irritates stomach, measures blood glucose value respectively in 0,0.5,2.0 hour 3 phase.
1.6. statistical method
All experimental data adopts SPSS/PC software kit (one factor analysis of variance) to handle on microcomputer.
2. result
2.1. ampelopsin is to the influence of normal mouse body weight
Table 1 respectively organize normal mouse initial body weight, mid-term body weight, finish body weight
| Group | Initial body weight | Mid-term body weight | Finish body weight | ||||
| Number of animals | Body weight (g) | Number of animals | Body weight (g) | Number of animals | Body weight (g) | ||
| Normal control | 10 | 23.4±1.0 | 10 | 30.5±1.5 | 10 | 32.4±1.6 | |
| Tried thing | 0.25g/kg 0.50g/kg 1.50g/kg | 10 10 10 | 23.6±1.1 23.7±1.2 23.5±1.2 | 10 10 10 | 31.2±1.2 30.9±1.6 31.1±1.2 | 10 10 10 | 33.1±1.6 32.3±1.9 33.5±1.5 |
| F value P value | 0.113 0.952 | 0.478 0.698 | 0.369 0.790 | ||||
Annotate: tried each dosage group mice body weight of thing and compare the equal nonsignificance of difference (variance analysis, P＞0.05) in each experimental period and normal control group
2.2. ampelopsin is to the influence of normal mouse fasting glucose
Table 2 ampelopsin is to the influence of normal mouse fasting glucose
| Group | Number of animals (only) | Fasting blood sugar (mmol/L) | Difference | ||
| Before the test | After the test | ||||
| Normal control | 10 | 4.7±0.5 | 4.6±0.7 | 0.1±06 | |
| Tried thing | 0.25g/kg 0.50g/kg 1.50g/kg | 10 10 10 | 4.5±0.6 4.6±0.8 4.4±0.7 | 4.4±0.7 4.4±0.8 4.4±0.7 | 0.1±1.1 0.2±1.0 0.0±0.5 |
| F value P value | 0.385 0.758 | 0.303 0.819 | 0.098 0.958 | ||
Annotate: tried each dosage group fasting blood sugar of thing and normal control group relatively, difference there are no significant meaning (variance analysis, P＞0.05).
2.3. ampelopsin is to the influence of normal mouse post-prandial glycemia
Table 3 ampelopsin is to the influence of normal mouse post-prandial glycemia
| Group | Number of animals (only) | Glucose (g/kgBW) | Blood glucose value (mmol/L) | |||
| 0h | 0.5h | 2h | ||||
| Normal control | 10 | 1.5 | 4.6±0.7 | 10.4±1.2 | 5.5±0.7 | |
| Tried thing | 0.25g/kg 0.50g/kg 1.50g/kg | 10 10 10 | 1.5 1.5 1.5 | 4.4±0.9 4.5±0.8 4.5±0.9 | 10.7±1.1 10.6±1.7 10.4±1.4 | 5.1±1.1 5.1±1.0 5.2±1.7 |
| F value P value | 0.311 0.823 | 0.221 0.865 | 0.518 0.664 | |||
Annotate: tried each dosage group postprandial plasma glucose level of thing and normal control group relatively, difference there are no significant meaning (variance analysis, P＞0.05).
2.4. ampelopsin is to the influence of normal mouse carbohydrate tolerance
Table 4 ampelopsin is to the influence of normal mouse carbohydrate tolerance
| Group | Number of animals (only) | Blood sugar increasing and reduction amplitude (mmol/L) | ||
| 0.5h-0h | 0.5h-2h | |||
| Normal control | 10 | 5.8±0.9 | 4.8±0.9 | |
| Tried thing | 0.25g/kg 0.50g/kg 1.50g/kg | 10 10 10 | 6.4±0.5 6.0±1.1 6.0±1.3 | 5.6±1.1 5.6±1.1 5.4±1.2 |
| F value P value | 0.995 0.406 | 1.015 0.393 | ||
Annotate: tried each dosage group carbohydrate tolerance value of thing and normal control group relatively, difference there are no significant meaning (variance analysis, P＞0.05).
2.5. ampelopsin is to the influence of the hyperglycemia mice body weight that causes
Table 5 respectively organize the hyperglycemia model mice initial body weight, mid-term body weight, finish body weight
| Group | Initial body weight | Mid-term body weight | Finish body weight | ||||
| Number of animals | Body weight (g) | Number of animals | Body weight (g) | Number of animals | Body weight (g) | ||
| Normal control | 10 | 24.3±1.3 | 10 | 30.7±2.0 | 10 | 31.2±1.9 | |
| Tried thing | 0.25g/kg 0.50g/kg 1.50g/kg | 10 10 10 | 24.4±2.5 24.2±1.3 24.2±1.4 | 10 10 10 | 31.7±2.1 31.6±2.5 31.1±1.8 | 10 10 10 | 32.5±2.3 32.2±2.8 31.5±1.5 |
| F value P value | 0.273 0.845 | 0.569 0.628 | 1.423 0.250 | ||||
Annotate: tried each stage body weight of each dosage group of thing and model control group relatively, difference there are no significant meaning (variance analysis, P＞0.05).
2.6. ampelopsin is to the influence of the hyperglycemia mice fasting glucose that causes
Table 6 ampelopsin is to the influence of hyperglycemia model mice fasting glucose
| Group | Number of animals (only) | Fasting blood sugar (mmol/L) | Difference | ||
| Before the test | After the test | ||||
| Normal control | 10 | 22.9±3.3 | 20.4±5.1 | 2.5±4.2 | |
| Tried thing | 0.25g/kg 0.50g/kg 1.50g/kg | 10 10 10 | 22.6±2.8 22.3±2.5 22.6±3.5 | 13.3±4.1* 15.5±6.1 17.4±6.5 | 9.3±3.6 * 7.8±4.5 5.2±6.3 |
| F value P value | 0.067 9.976 | 3.010 0.039 | 4.230 0.015 | ||
Annotate: compare with model control group,
*P＞0.05 (q check)
Tried thing low dose group test back fasting blood sugar and front and back fasting glucose difference and model control group relatively, difference all has significantly (variance analysis, P＞0.05).
2.7. ampelopsin is to the influence of the hyperglycemia mice post-prandial glycemia that causes
Table 7 ampelopsin is to the influence of hyperglycemia type mice post-prandial glycemia
| Group | Number of animals (only) | Glucose (g/kgBW) | Blood glucose value (mmol/L) | |||
| 0h | 0.5h | 2h | ||||
| Normal control | 10 | 1.5 | 20.4±5.1 | 31.2±2.7 | 24.7±3.7 | |
| Tried thing | 0.25g/kg 0.50g/kg 1.50g/kg | 10 10 10 | 1.5 1.5 1.5 | 13.4±4.1* 15.2±6.0 17.6±6.1 | 26.9±4.6 27.9±5.6 28.6±4.8 | 16.8±6.9* 17.5±7.9 * 20.7±7.8 |
| F value P value | 3.132 0.043 | 2.415 0.079 | 3.689 0.032 | |||
Annotate: tried the low agent group of thing after the meal the 0h blood glucose value and low in the dosage group after the meal the 2h blood glucose value compare with model control group, difference all has significantly (variance analysis, P＞0.05).
2.8. ampelopsin is to the influence of the hyperglycemia mice carbohydrate tolerance that causes
Table 8 ampelopsin is to the influence of hyperglycemia model mice carbohydrate tolerance
| Group | Number of animals (only) | Blood sugar increasing and reduction amplitude (mmol/L) | ||
| 0.5h-0h | 0.5h-2h | |||
| Normal control | 10 | 10.8±3.2 | 6.5±2.9 | |
| Tried thing | 0.25g/kg 0.50g/kg 1.50g/kg | 10 10 10 | 13.9±1.6 12.0±3.3 11.4±2.7 | 10.1±2.9 9.1±3.9 8.7±4.5 |
| F value P value | 1.311 0.265 | 2.278 0.120 | ||
Annotate: tried each dosage group carbohydrate tolerance value of thing and model control group relatively, difference all has significantly (variance analysis, P＞0.05).
Experimental result shows that ampelopsin has the blood sugar regulation effect.
Embodiment 8: the test of ampelopsin blood fat reducing
Animal is divided into 4 groups at random, normal control group, positive controls, model control group, extracting solution group.Every group of 10 mices, once-a-day, successive administration 10 days, the normal control group is not given any medicine.All the other all to high lipoprotein emulsion 0.5ml/ only respectively organize mice, form experimental hyperlipidemia, overnight fasting after medication in 10 days, press enzyme process and detect serum total cholesterol (TC), triglyceride (TG), HDL-C (HDL-C) content from the mouse orbit extracting vein blood next day.The result shows that model control group serum TC, TG value obviously raise, and the HDL-C value descends, compare with model, the ampelopsin group can obviously reduce serum TC, TG value, and HDL-C is slightly raise, illustrate that this extract can suppress the mice blood fat rising that high lipoprotein emulsion causes, has effect for reducing fat.
1. material and method
1.1. tried thing: contain the raw material (wherein the content of ampelopsin is 65%) of ampelopsin, be for experiment with the turbid solution that distilled water is mixed with desired concn with trying thing.
1.2. laboratory animal: SPF level Wistar rat, body weight 170-190g, female, totally 55 (5 are standby).Experimental temperature: 23-25 ℃, relative humidity: 65-70%.
1.3. feedstuff:
1.3.1. the pure Mus material of common normal feedstuff: Wistar.
1.4. the dosage grouping: experiment is divided into five groups, be normal control group, hyperlipidemia model matched group and tried basic, normal, high three the dosage groups of thing, dosage is respectively 0.5,1.0,1.5g/kg.bw, is equivalent to recommend 10,20,30 times of human body daily intaking amount 3g/60kg.bw.
1.5. experimental technique:
The rat adaptability is raised and is begun experiment after 3 days.Get rat tail blood, measure serum total cholesterol (TCO), triglyceride (TGO), HDL-C (HDL-c0) basic value.According to the TCO level, rat is divided into five groups at random, every group of 10 animals, promptly basic, normal, high dosage group, normal control group and hyperlipidemia model matched group.Except that the normal control group gives the normal feedstuff, all the other each groups all give high lipid food.Three are tried agent amount group and irritate stomach by the capacity per os of 1.0ml/100g.bw and give, the feed of freely drinking water of normal control group and hyperlipidemia model matched group.Give 30 days continuously, detected TC, TG, HDL-C value on the 30th day in irritating stomach.
1.6. key instrument and reagent: SABA-18 type automatic clinical chemistry analyzer (Italy produces), standard quality controlled serum and corresponding reagent box are produced by Shanghai Foxing Changzheng medical science Co., Ltd.
1.7. date processing: adopt the STATA statistical software to carry out statistical analysis
2. result
2.1. ampelopsin is to the influence of hyperlipidemia model the weight of animals: as seen from Table 9, compare with model control group, basic, normal, high dosage group around the time rat body weight all be lower than model control group, basic, normal, high dosage group and model control group comparing difference have significance (P＜0.01, P＜0.01, P＜0.01).With the normal control group relatively, body weight all is higher than the normal control group around the basic, normal, high dosage group the, but credit is analysed by statistics, difference does not have significance.
2.2. ampelopsin is to the influence of high blood lipid model rat body weight: as shown in Table 9, compare with matched group, ampelopsin does not have obvious influence to rat body weight.
Table 9 ampelopsin is to the influence of high blood lipid model rat body weight (g, x ± s)
| Dosage g/kg.bw | Number of animals (only) | Body weight | ||||
| Starting weight | First week | Second week | The 3rd week | Heavy eventually | ||
| The normal control model contrasts 0.5 1.0 1.5 | 10 10 10 10 10 | 181.4±2.8 181.7±3.5 181.5±3.90 181.6±2.5 184.2±2.3 | 202.2±6.2 208.7±2.6 207.9±3.2 208.6±3.1 207.9±3.2 | 219.6±4.7 224.5±4.4 220.79±3.2 222.40±2.3 221.5±3.1 | 226.2±3.7 231.4±3.5 226.9±3.4 228.2±3.0 226.5±3.0 | 230.7±4.0** 237.6±3.7 232.1±2.8** 233.9±2.2** 232.0±3.0** |
*Compare P＜0.01 with model control group
2.3. ampelopsin is to the influence of rat total cholesterol level: as seen from Table 10, compare with model control group, middle and high dosage group total cholesterol level descended obviously at experimental session when experiment finished, and credit is analysed by statistics, and difference has significance (p＜0.05, P＜0.01).
Table 10 ampelopsin is to the influence of rat total cholesterol level (mmol/L, x ± s)
| Dosage g/kg.bw | Number of animals (only) | T-CHOL | |||
| Before the test | The P value | After the test | The P value | ||
| The normal control model contrasts 0.5 1.0 1.5 | 10 10 10 10 10 | 1.80±0.07 1.81±0.11 1.82±0.10 1.82±0.10 1.83±0.11 | 0.786 - 0.812 0.916 0.765 | 1.81±0.16 3.72±0.34 3.38±0.62 3.15±0.56* 2.91±0.57** | 0.000 - 0.272 0.010 0.001 |
*Compare P＜0.05 with model control group,
*Compare P＜0.01 with model control group
2.4. ampelopsin is to the influence of rat content of triglyceride: as seen from Table 11, compare with model control group, basic, normal, high dosage group content of triglyceride descends obviously during off-test, and credit is analysed by statistics, and difference has significance (P＜0.05, P＜0.01, P＜0.01).
Table 11 ampelopsin is to the influence of rat content of triglyceride (mmol/L, x ± s)
| Dosage g/kg.bw | Number of animals (only) | T-CHOL | |||
| Before the test | The P value | After the test | The P value | ||
| The normal control model contrasts 0.5 1.0 1.5 | 10 10 10 10 10 | 1.24±0.25 1.26±0.27 1.22±0.18 1.26±0.17 1.22±0.16 | 0.828 - 0.782 0.791 0.645 | 1.29±0.11 2.30±0.47 1.95±0.21* 1.92±0.22** 1.88±0.12** | 0.000 - 0.012 0.009 0.007 |
*Compare P＜0.05 with model control group,
*Compare P＜0.01 with model control group
2.5. ampelopsin is to the influence of rat HDL-C content: as seen from Table 12, compare with model control group, basic, normal, high dosage group has the rising effect to HDL-C, and credit is analysed by statistics, and difference has significance (P＜0.05).
Table 12 ampelopsin is to the influence of rat HDL-C content (mmol/L, x ± s)
| Dosage g/kg.bw | Number of animals (only) | HDL-C | |||
| Before the test | The P value | After the test | The P value | ||
| Normal control | 10 | 1.13±0.12 | 0.872 | 1.06±0.11 | 0.000 |
| Model contrasts 0.5 1.0 1.5 | 10 10 10 10 | 1.12±0.18 1.10±0.07 1.14±0.08 1.14±0.07 | - 0.656 0.859 0.798 | 0.84±0.11 0.97±0.09* 0.94±0.07* 0.95±0.08* | - 0.026 0.041 0.016 |
*Compare P＜0.05 with model control group
2.6. ampelopsin is to the influence of rat fat level: this experimental technique is a high lipid food and tried thing and give simultaneously, belongs to preventative, so TG, TC decline and HDL-c rising value all with the comparison of hyperlipidemia model matched group.By table 13 as seen, middle and high dosage group total cholesterol level fall is respectively 15.8%, 20.2%, basic, normal, high dosage group content of triglyceride fall is respectively 15.9%, 17.3%, 18.0%, and basic, normal, high dosage group HDL-C content lift-off value is 4.48,4.98,4.35mg/dl.
Table 13 ampelopsin is to the influence of rat fat level
| Dosage g/kg.bw | Number of animals (only) | TC (％) | TG (％) | HDL-C (mg/dl) |
| 0.5 1.0 1.5 criterions: | 10 10 10 | 10.1 15.8 20.2 descend＞10% | 15.9 17.3 18.0 descend＞15% | 4.48 4.98 4.35 rising 4mg/dl |
Annotate: HDL-c lift-off value (mg/dl) is mmol/L * 38.7=mg/dl conversion result
Embodiment 9: the test of ampelopsin enhancing immunity function
1. ampelopsin is to the influence of Turnover of Mouse Peritoneal Macrophages phagocytic function
1.1 experiment purpose
Observe the influence of ampelopsin to the mice phagocytic function.
1.2 be subjected to the reagent thing
Title: ampelopsin
Solvent: hot distilled water
Consumption: 0.5ml/20g mice
1.3 control sample
Bifendate; Shanghai balance pharmaceutical factory, the accurate word (1995) of medicine is defended No. 3765-011 in Shanghai
1.4 animal
Mice, the Kunming kind, male, 19～21g.
Chicken red blood cell: 5% concentration
1.5 method
Kunming mouse, be divided into 5 groups at random, be matched group, ampelopsin 75,150,300mg/kg, bifendate 150mg/kg, matched group gives normal saline, the equal oral administration of administration group, every day 1 time, totally 6 times, lumbar injection 0.5% lactoalbumin hydrolysate 1.5ml/ simultaneously of last administration, pneumoretroperitoneum was injected 5% chicken red blood cell 0.1ml in 24 hours, the blood-letting of breaking end after 30 minutes, use the normal saline flushing abdominal cavity, collect peritoneal macrophage and hatch half an hour for 37 ℃, centrifugal, the precipitate smear, dyeing, counting cells under the oil mirror calculates with following formula, and compares with matched group.
1.6 result
The results are shown in Table 13, the basic, normal, high dosage of ampelopsin can promote all Turnover of Mouse Peritoneal Macrophages to engulf chicken red blood cell and increase phagocytic index that bifendate 150mg/kg dosage group also can promote the Turnover of Mouse Peritoneal Macrophages phagocytic function.
Table 13. ampelopsin to the influence of Turnover of Mouse Peritoneal Macrophages phagocytic function (± SD)
| Group | Dosage mg/kg | Approach | Number of animals (only) | Phagocytic percentage % | Phagocytic index |
| Ampelopsin | 75 | po×6 | 8 | 31.2±3.4 ** | 0.64±0.07 ** |
| 150 | po×6 | 8 | 43.2±4.2 | 0.85±0.02 ** | |
| 300 | po×6 | 8 | 42.3±4.8 ** | 0.81±0.06 ** | |
| Bifendate | 150 | po×6 | 8 | 40.1±4.5 ** | 0.88±0.03 ** |
| Matched group | Coordinative solvent | 8 | 23.0±5.3 | 0.39±0.12 | |
*Compare with model control group P＜0.01
2. ampelopsin is to the influence of mice spleen lymphocytes proliferation
2.1 experiment purpose
Observe the influence of ampelopsin to mice spleen lymphocytes proliferation.
2.2 be subjected to the reagent thing
Title: ampelopsin
Solvent: hot distilled water
Consumption: 0.5ml/20g mice
2.3 control sample
Bifendate; Shanghai balance pharmaceutical factory, the accurate word (1995) of medicine is defended No. 3765-011 in Shanghai
2.4 animal
Mice, C
57BL/6, ♂, 19～21g.
2.5 other materials
Canavaline (ConA): Sigma product, 50 μ g/ml concentration
3H-TdR: Shanghai nuclear research institute, radioactive concentration 1mci/ml
Culture medium: RPMI-1640 includes 15% calf serum, mercaptoethanol, Hepes etc.
2.6 method
C
57The BL/6 mice is divided into 5 groups at random, i.e. normal control group, ampelopsin 75,150,300mg/kg, bifendate 150mg/kg, every day, oral administration was 1 time, and continuous 7 days, after administration finishes, put to death under the animal aseptic condition and get spleen, the counting splenocyte, and the adjustment cell concentration is 1 * 10
7/ ml, every hole adds cell suspension 100 μ l on 96 porocyte culture plates, ConA 50 μ l, and culture fluid, each group is all established three multiple pipes, 37 ℃, 5%CO
2Cultivated 48 hours under the condition, add
3H-TdR 0.5 μ ci/ hole continues to cultivate 18 hours, with bull cell harvestor collecting cell, surveys the CPM value on liquid scintillation instrument, and compares with matched group, the results are shown in Table 14.
2.7 result
Table 14. ampelopsin is to the influence of mice spleen lymphocytes proliferation
| Group | Dosage mg/kg | Approach | Number of animals (only) | The CPM value (± SD) |
| Ampelopsin | 75 | po×7 | 4 | 11763±1985 * |
| 150 | po×7 | 4 | 7547±1369 * | |
| 300 | po×7 | 4 | 7832±1298 * | |
| Bifendate | 150 | po×7 | 4 | 7188±1010 ** |
| Matched group | N.S. | 4 | 5448±917 | |
*P＜0.05
*Compare with matched group P＜0.01
The result shows that Caulis seu folium ampelopsis brevipedunculatae (Caulis Ampelopsis Brevipedunculae) have the effect of tangible promotion mice spleen lymphocytes proliferation, and strong than other two groups with the low dosage effect.
Claims (2)
1. the purposes of compositions in the preparation hypoglycemic drug of forming with the weight ratio of 2-80: 20-98 by ampelopsin and ampelopsin.
2. the purposes of compositions in preparation blood sugar lowering and blood lipid-lowering medicine of forming with the weight ratio of 2-80: 20-98 by ampelopsin and ampelopsin.
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| GB2382808A (en) * | 2001-12-05 | 2003-06-11 | Advanced Technologies Group Lt | Lighter-than-air aircraft with air cushion landing gear |
| CN100345539C (en) * | 2003-05-30 | 2007-10-31 | 任启生 | Composition containing dihydro myricitrin and myricitrin |
| ES2241491B1 (en) * | 2004-04-07 | 2006-12-01 | Provital, S.A. | COSMETIC AND / OR PHARMACEUTICAL COMPOSITION, REGULATOR OF FAT LEVELS IN ADIPOCYTES AND / OR REGULATOR OF ADIPOCITARY DIFFERENTIATION. |
| CN100345540C (en) * | 2004-04-12 | 2007-10-31 | 北京江中泽生科技有限责任公司 | Use of ampelopsin in preparing medicine for treating diseases related with aldose reductase |
| CN100337661C (en) * | 2004-06-04 | 2007-09-19 | 澳美制药厂有限公司 | Application of ampelopsis plant and its extract in preparing medicine and health article |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1375289A (en) * | 2001-03-15 | 2002-10-23 | 北京美林亚科技发展有限公司 | Ampelosis general flavone composition with liver protecting function |
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| CN1375289A (en) * | 2001-03-15 | 2002-10-23 | 北京美林亚科技发展有限公司 | Ampelosis general flavone composition with liver protecting function |
Non-Patent Citations (2)
| Title |
|---|
| 双氢杨梅树皮素降血糖的实验研究 覃洁萍等，中国现代应用药学杂志，第18卷第5期 2001 * |
| 显齿蛇葡萄基本成分研究 张永胜等，天然产物研究与开发，第13卷第5期 2001 * |
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