CN101011454A - Application of pongamia pinnata extract in preparation of anti-gastric-ulcer medicament and anti-inflammation and analgesic medicament - Google Patents
Application of pongamia pinnata extract in preparation of anti-gastric-ulcer medicament and anti-inflammation and analgesic medicament Download PDFInfo
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- CN101011454A CN101011454A CN 200610094866 CN200610094866A CN101011454A CN 101011454 A CN101011454 A CN 101011454A CN 200610094866 CN200610094866 CN 200610094866 CN 200610094866 A CN200610094866 A CN 200610094866A CN 101011454 A CN101011454 A CN 101011454A
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Abstract
The invention relates to a method for using karanjin to prepare the drug used to treat gastric ulcer and antiphlogistic function. The invention uses the mouse alcohol gastric ulcer model and the mouse alserin gastric ulcer model, to watch the karanjin alcohol extractive on the hurt of gastric mucosa, which proves that the karanjin alcohol extractive and relative acetic acid ethyl ester extractive can significant restrain the gastric mucosa hurt. The invention uses the mouse dimethylbenzene ear expanding model and the mouse acetate ease pain test to watch the antiphlogistic function of karanjin extractive. The invention also processes the mouse acute toxicity test on the karanjin alcohol extractive, to prove the little toxicity of it.
Description
Technical field
The present invention relates to medical technical field, be specifically related to that the Indian beech extract is used for preparing the application of gastritis gastric ulcer medicine and in the application of preparation anti-inflammation analgesis medicament.
Background technology
Gastric ulcer belongs to commonly encountered diseases, frequently-occurring disease, and domestic and international at present research report is more, but many employing chemotherapys, and untoward reaction is more.Chinese medicine has in treatment that its source is abundant aspect the disease, economy, advantage that toxicity is little.And be applied in the medicine of clinical treatment gastric ulcer at present, the Chinese medicine with definite curative effect is also few.The medicine of anti-inflammatory and antalgic mostly is chemicals at present, because its side effect is many, uses and is limited to, and the Chinese medicine of therefore developing anti-inflammatory and analgesic effect has significant values.
Indian beech Pongamia pinnata (L.) Merr. (different name Pongamia glabra) is pulse family (Leguminos-ae) Pongamia (Pongamia Vent.) plant, the another name Semen Pongamiae Pinnatae.Indian beech has multiple biological activity, and China mainly is distributed in Hainan, Guangdong and ALONG GUANGXI COAST.The expressed oil treatment scabies of China's its seed of usefulness among the people, abscess and rheumatism (Jiangsu medical college, " Chinese medicine voluminous dictionary " [M]. Science and Technology of Shanghai publishing house, 1997).So far do not see that relevant Indian beech root extract is used for the report of the effective site of anti-inflammatory and antalgic and anti-gastric-ulcer.
Summary of the invention:
The purpose of this invention is to provide a kind of Indian beech extract, this extract has the effect and the anti-inflammatory and analgesic effect of good anti-gastric-ulcer, can be used for preparing the medicine of anti-gastric-ulcer.
The medicinal part of Indian beech is a root, stem and leaf among the present invention, when the medicine of preparation such use, Indian beech rhizome leaf can be extracted, and extract is made medicine.Indian beech extract of the present invention is to be raw material with (Pongamia pinnat.Merr) rhizome leaf, adopts conventional chemical extracting method known in the art to prepare total extract or fat-soluble position.According to the present invention, Indian beech rhizome leaf is pulverized, or/and water extraction prepares total extract, used organic solvent can adopt alcohols with organic solvent, as ethanol, methanol etc., wherein preferred 50%-80% (volume ratio) ethanol.
With total extract water-soluble after, use petroleum ether, esters (or halogenated hydrocarbon) solvent extraction respectively in succession, get esters (or halogenated hydrocarbon) solvent extraction phase, reclaim the solvent after drying and promptly obtain fat-soluble position, used esters or halogenated hydrocarbon solvent can adopt ethyl acetate, chloroform or dichloromethane etc., wherein ethyl acetate.Carbon dioxide (CO also can directly be passed through in fat-soluble position
2) the supercritical extraction acquisition.
Carry out zoopery with the animal model (rat ethanol-type gastric ulcer model and mice reserpine type gastric ulcer model) that is widely used at present the screening medicament for anti-gastric ulcer both at home and abroad, confirmed that Indian beech extract of the present invention is to gastric ulcer model, can significantly reduce gastric mucosal damage, suppress the formation of ulcer.Illustrate that thus the Indian beech extract has definite anti-gastric-ulcer effect, therefore can be used to prepare the medicine of anti-gastric-ulcer.Adopt dimethylbenzene induced mice ear swelling model, acetic acid induced mice to turn round the body analgesic experiment, confirmed that Indian beech extract of the present invention has clear and definite anti-inflammatory and analgesic effect, therefore also can be used to prepare the medicine of anti-inflammatory and antalgic.
With the Indian beech extract is active site, is equipped with suitable carrier or excipient and can makes tablet, granule, capsule, soft capsule, the pharmaceutical dosage form that drop pill or oral liquid etc. are commonly used.
Description of drawings:
The photo of Fig. 1 rat ethanol-type gastric ulcer model matched group gastric mucosa injury
Fig. 2 is the photo of Indian beech total ethanol extract of the present invention to the protective effect of rat ethanol-type gastric mucosa injury
Fig. 3 is the photo of Indian beech acetic acid ethyl ester extract of the present invention to the protective effect of rat ethanol-type gastric mucosa injury
The specific embodiment:
Now, the present invention is described in detail, does not limit the present invention in conjunction with example.
Embodiment 1 Rheum alexandrae Batal. dermatome total ethanol extract preparation: water intaking Radix clausenae lansii dry product, after pulverizing with cracker for medicine, use 70% soak with ethanol, 60 ℃ of water-bath reflux, extract, 3 times, merge and be collected in distilling under reduced pressure in the rotary evaporation bottle after backflow filters, being recycled to does not have the alcohol flavor, the dry sepia dry extract that gets.
Embodiment 2 Rheum alexandrae Batal. dermatome acetic acid ethyl ester extracts preparation: with the ethanol extraction dissolved in distilled water, use the equal-volume petroleum ether in succession, ethyl acetate, n-butanol extraction 3 times, reclaim solvent respectively, obtain residue after petroleum ether extract and acetic acid ethyl ester extract, n-butyl alcohol extract, the extraction behind the vacuum drying (80 ℃).
Embodiment 3 Indian beech root extracts are to the effect of rat ethanol-type gastric ulcer
1. animal: SPF level Kunming mouse, body weight 20 ± 2g, male and female half and half quality certification number: SCXK (Guangdong) 2003-0001; SPF level SD rat, body weight 180 ± 20g, male and female half and half, the quality certification number: SCXK (Guangdong) 2003-0002, provide by Guangdong Province's Experimental Animal Center.The animal subject male and female are separated the full diet nursing and are begun experiment after 5 days, and the control room temperature is 22 ± 2 ℃, and humidity is 55 ± 15%.
2. medicine: cimetidine, Hainan Pharmaceutical Factory Co., Ltd. produces, lot number: 050701; Rheum alexandrae Batal. dermatome acetic acid ethyl ester extract, prepared by example 2.
3. experimental technique: 48 of cleaning level SD rats, male and female half and half are divided into 7 groups at random: get 8 of above-mentioned SD rats as model control group for the 1st group; 2nd, 3,4,5,6 groups is Rheum alexandrae Batal. dermatome total ethanol extract, petroleum ether extract, acetic acid ethyl ester extract, n-butyl alcohol extract, residue group, and 8 every group, irritate stomach according to 4.2g crude drug/kg body weight every day; Get 8 positive matched groups for the 7th group, irritate stomach cimetidine suspension according to the 140mg/kg body weight every day.Each administration group is gastric infusion (1.5ml/100g body weight) according to dosage, the isopyknic 0.5%CMC-Na solution of model group ig, every day 1 time, continuous 5 days.After the last administration 2 hours, 48 hours rats of fasting only all gavaged dehydrated alcohol 0.8ml/.Put to death rat after 1 hour, ligation cardia and pylorus also take out stomach, inject 1% formalin 8ml in gastral cavity.Fixedly 30min tailing edge greater gastric curvature is cut open, perusal glandular stomach portion gastric mucosal damage degree, and scoring is also calculated damage index.
Concrete code of points is as follows: complete gastric mucosa is 0 minute; Petechial hemorrhage (diameter≤1mm) counted 1 fen: the rotten to the corn meter of point-like 1 minute; Streak damaged length＞1mm person measures its length, and every 1mm meter 1 minute is if its width doubles score greater than 1mm person.Score adds up to the mucosa injury index of this rat, and presses the damage suppression ratio of each administration group of column count.Damage suppression ratio=(model group damage index-administration group damage index)/model group damage index * 100%.
4. experimental result: experimental result is seen Fig. 1, Fig. 2, Fig. 3 and table 1.
Table 1 Indian beech root extract is to the effect (n=8) of rat ethanol-type gastric ulcer
Annotate: 1: model control group; 2: Rheum alexandrae Batal. dermatome total ethanol extract group; 3: Rheum alexandrae Batal. dermatome petroleum ether extract; 4: Rheum alexandrae Batal. dermatome acetic acid ethyl ester extract low dose group; 5: dosage group in the Rheum alexandrae Batal. dermatome acetic acid ethyl ester extract; 6: Rheum alexandrae Batal. dermatome acetic acid ethyl ester extract high dose group; 7: the cimetidine positive controls
As seen from Figure 1, the model control group gastric mucosa injury shows as myxedema, hyperemia, extensively kitchen range shape and streak damage mainly in glandular stomach portion.By Fig. 2 and Fig. 3 as can be seen Rheum alexandrae Batal. dermatome total ethanol extract with and acetic acid ethyl ester extract the ethanol-type gastric mucosa injury is had obvious inhibitory action.Rheum alexandrae Batal. dermatome total ethanol extract and model group compare as can be seen from Table 1, and ulcer index obviously reduces (P＜0.01), and ulcer inhibition rate is 86.4%.Rheum alexandrae Batal. dermatome acetic acid ethyl ester extract is compared with model group, and ulcer index obviously reduces (P＜0.01), and ulcer inhibition rate is 85.4%.Confirm that thus Rheum alexandrae Batal. dermatome total ethanol extract has significant inhibitory effect to the ethanol-type gastric mucosa injury, and to point out its effective site be fat-soluble position.
Embodiment 4 Indian beech root extracts are to the effect of mice reserpine type gastric ulcer
1. animal: SPF level Kunming mouse, body weight 20 ± 2g, male and female half and half quality certification number: SCXK (Guangdong) 2003-0001, provide by Guangdong Province's Experimental Animal Center.The animal subject male and female are separated the full diet nursing and are begun experiment after 5 days, and the control room temperature is 22 ± 2 ℃, and humidity is 55 ± 15%.
2. medicine: cimetidine, Hainan Pharmaceutical Factory Co., Ltd. produces, lot number: 050701; Rheum alexandrae Batal. dermatome acetic acid ethyl ester extract, prepared by example 1 and 2.
3. experimental technique: 70 of cleaning level kunming mices, be divided into 7 groups (grouping is with examples 3) at random, every group 10, the 7th group of positive controls is according to 0.20g/kg body weight administration every day, all the other respectively are subjected to the reagent group all by 6g crude drug/kg administration, each administration group according to dosage gastric infusion volume is the 0.2ml/10g body weight, the isopyknic 0.5%CMC-Na solution of model group ig, every day 1 time, continuous 5 days, after 1 hour, fasting was respectively organized mice in 24 hours all at once through subcutaneous injection of reserpine 10mg/kg in the last administration, and dislocation of cervical vertebra is put to death after 6 hours.Open the abdominal cavity, ligation stomach cardia and pylorus, and in gastral cavity, inject 1% formaldehyde 2ml through coat of the stomach, stomach is taken out, 30min tailing edge greater gastric curvature is cut open in the immersion formalin, refers to and calculate the ulcer inhibition rate of each administration group by the ulcer of example 3 code of points calculating glandular stomach portion appearance.
4. result's experiment the results are shown in Table 2.
Table 2 Indian beech root extract is to the effect (n=10) of mice reserpine type gastric ulcer
Annotate: each organizes note with table 1
Rheum alexandrae Batal. dermatome total ethanol extract and model group compare as can be seen from Table 2, and ulcer index obviously reduces (P＜0.01), and ulcer inhibition rate is 37.8%.Rheum alexandrae Batal. dermatome acetic acid ethyl ester extract is compared with model group, and ulcer index obviously reduces (P＜0.01), and ulcer inhibition rate is 33.8%.Illustrate that thus Rheum alexandrae Batal. dermatome total ethanol extract has significant inhibitory effect to the ethanol-type gastric mucosa injury, and to point out its effective site be fat-soluble position.
The anti-inflammatory and analgesic effect of embodiment 5 Indian beech root extracts
1. animal: mice, described with example 3.
2. medicine: dexamethasone, dragon source, Queshan pharmaceutcal corporation, Ltd, lot number: 040821; Aspirin, Xi'an Lijun pharmaceutical Co., Ltd, lot number: 0407182.Rheum alexandrae Batal. dermatome total ethanol extract, described with example 1.
3. experimental technique:
(1) 30 mices that influence of Indian beech extract xylol induced mice ear swelling are divided into 3 groups, 10 every group at random.Be dosage group in model group, the Indian beech extract (6g crude drug/kg body weight) and positive controls (dexamethasone, 2mg/kg).Each administration group is gastric infusion respectively, and the administration volume is 20ml/kg, and model group is irritated the isopyknic solvent of stomach, once a day, and totally 5 days.Behind the 5th day gastric infusion 1 hour, each mice is smeared dimethylbenzene 0.05ml in auris dextra, take off neck after 2 hours and put to death animal, sweep away the disk at left ear and the same position of auris dextra with diameter 8mm card punch, on analytical balance, claim quality, with two auricle quality differences is inflammation swelling degree, and calculates inhibitory rate of intumesce.
(2) the Indian beech root extract is divided into 3 groups, 10 every group at random to mice acetic acid twisting analgesic 30 mices of experiment.Be dosage group in model group, the Indian beech extract (6g crude drug/kg body weight) and positive controls (aspirin, 0.2g/kg).Each administration group is gastric infusion respectively, the administration volume is 20ml/kg, and model group is irritated the isopyknic solvent of stomach, once a day, respectively organized 1 hour pneumoretroperitoneum of equal gastric infusion or solvent in totally 5 days and only inject 0.6% acetic acid 0.2mL/, write down in 10 minutes and respectively organize the number of times that writhing response appears in mice.
4. experimental result
(1) influence of Indian beech extract xylol induced mice ear swelling
The results are shown in Table 3.Indian beech extract xylol causes mice ear the obvious suppression effect.
(2) the Indian beech root extract is tested mice acetic acid twisting analgesic
The results are shown in Table 4.The Indian beech extract can obviously reduce the number of times that the acetic acid induced mice is turned round body.The pain suppression ratio of dosage can reach 57.40% in the Indian beech extract.
This example explanation Indian beech extract has obvious anti-inflammatory analgesic, can be used for the preparation of anti-inflammation analgesis medicament.
The influence of table 3 Indian beech extract xylol induced mice ear swelling
*Compare with model control group P＜0.01
Table 4 Indian beech root extract is tested mice acetic acid twisting analgesic
*Compare with model control group P＜0.01
The acute toxicity of embodiment 6 Rheum alexandrae Batal. dermatome total ethanol extracts
1. animal: mice, described with example 3.
2. medicine: Rheum alexandrae Batal. dermatome total ethanol extract, described with example 1.
3. experimental technique:
According to the trial test result, determine that 100% dead dosage is 10g/kg, 100% survival dose is 2.5g/kg, 100% cause death and 100% survival volume between establish 6 dosage, ratio is 1: 0.75 between group, is respectively 10,7.5,5.63,4.22,3.16, the 2.37g/kg body weight.Choose body weight and be 60 of (20 ± 2) g white mice, male and female half and half are divided into 6 groups at random by body weight, and 10 every group, fasting is after 12 hours, and each group is pressed the disposable gastric infusion of 0.4ml/10g body weight, observes 14 days dead mouse situations.
4. experimental result:
The record mice gives each concentration total extract and irritates stomach result of the test and see Table 5, and it is as follows to calculate linear regression equation according to table 3 by the bliss method: Y=0.048044+6.1571Log (D), LD50=6.3718g/kg is equivalent to crude drug 59.3g/kg.
This example laboratory proves that Indian beech root extract toxicity is very little, can be used to prepare medicine of the present invention.
The acute toxicity testing of table 5 Rheum alexandrae Batal. dermatome total ethanol extract
| Dosage (g/kg) | Number of animals (only) | Death toll (only) | Per cent death loss (%) |
| 10 | 10 | 9 | 90.00 |
| 7.5 | 10 | 6 | 60.00 |
| 5.63 | 10 | 4 | 40.00 |
| 4.22 | 10 | 2 | 20.00 |
| 3.16 | 10 | 0 | 0.00 |
| 2.37 | 10 | 0 | 0.00 |
Claims (4)
1. an Indian beech extract is characterized in that described extract is for being extracted Indian beech total extract or the fat-soluble position of Indian beech that obtains by the Indian beech root, stem and leaf.
2. the described Indian beech extract of claim 1 is in the purposes of preparation in the medicament for anti-gastric ulcer.
3. the described Indian beech extract of claim 1 is in the purposes of preparation in the anti-inflammation analgesis medicament.
4. according to claim 2,3 described medicines, it is characterized in that said medicament is a said dosage form on any pharmaceutics.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102133258A (en) * | 2010-01-21 | 2011-07-27 | 朱毅 | Extracting and purifying process of pongamia pinnata flavonoids |
| JP7470699B2 (en) | 2018-10-04 | 2024-04-18 | テルヴィーヴァ，インコーポレイテッド | Methods for Analysing Pongamia Composition |
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2006
- 2006-06-29 CN CN 200610094866 patent/CN101011454A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102133258A (en) * | 2010-01-21 | 2011-07-27 | 朱毅 | Extracting and purifying process of pongamia pinnata flavonoids |
| JP7470699B2 (en) | 2018-10-04 | 2024-04-18 | テルヴィーヴァ，インコーポレイテッド | Methods for Analysing Pongamia Composition |
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Open date: 20070808 |