CN101023952A - Use of aesin in releasing abdominal distention and astriction - Google Patents
Use of aesin in releasing abdominal distention and astriction Download PDFInfo
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- CN101023952A CN101023952A CN 200610009183 CN200610009183A CN101023952A CN 101023952 A CN101023952 A CN 101023952A CN 200610009183 CN200610009183 CN 200610009183 CN 200610009183 A CN200610009183 A CN 200610009183A CN 101023952 A CN101023952 A CN 101023952A
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Abstract
The present invention provides a new application of aescine. The invented tests show that the invented aescine can be mainly used for curing the diseases of abdominal distension and constipation, etc, due to gastrointestinal peristalsis reduction and gastrointestinal dysfunction resulated from diabetes, angiocardiopathy, senile diseases and other diseases. It can obtain obvious therapeutic effect for curing abdominal distension and constipation, etc.
Description
Invention field
The present invention relates to aescine and its esters in the purposes of alleviating abdominal distention and constipation.
Background technology
Aescine (Aescin) is the saponin that extracts from Europe Aesculus hippocastanum (Aesculus hippocastanum) seed, uses for 30 years in Germany, and more than 20 countries and regions get the nod in the world at present, is recorded by the big pharmacopeia of Martin in 1993.China begins to produce the aescine injection from the eighties, used aescine for " extract of a Semen Aesculi that records of Chinese pharmacopoeia, through identify with external aescine be same substance.The extract of the fruits and seeds of Aesculus turbinata B1 (Aesculus turbinataBlume) and Chinese Heavenly Teacher chestnut (Aesculus wilsonii Rehd) also contains this chemical compound.Show to have antiinflammatory, exudation clinically, recover capillary permeability, improve intravenous tension, improve blood circulation, promote effects such as brain function recovery.We discover that it has the effect of tangible promotion gastrointestinal peristalsis, can be used for treating abdominal distention and the constipation that a variety of causes causes.
Abdominal distention and constipation are the pathological states that a kind of common digestive tract power weakens.Common have gastroparesis that old people's habitual constipation, diabetic constipation, irritability constipation, wound and postoperative intestine functional disorder, reflux esophagitis, a variety of causes cause and congenital megacolon syndrome etc.Medicine mainly contains bulking agent (as Testa Tritici, Psyllium etc.), permeability laxative (as Macrogol 4000, lactulose etc.) and motor activation regulator (as cisapride and mosapride etc.) at present, bulking agent and permeability laxative only have certain curative effect at light-duty constipation patient, the patient of back or long-term bed can not be used to perform the operation, especially the patient with operation at gastrointestinal tract position, cisapride and mosapride etc. are used the toxic and side effects that is considered to potential cardiovascular system clinically.We discover, aescine has the effect of facilitating digestion road power significantly, and it is at the obvious facilitating digestion road power of approach such as oral, percutaneous dosing and drug administration by injection.The discovery of the mechanism of action that this is new can be used for the treatment of because diabetes, cardiovascular diseases, Senile disease, long-term bed patient, development in children defective and congenital diseases constipation induced.Be used for the treatment of diabetic gastroparesis, congenital megacolon, reflux esophagitis.Promote wound and postoperative intestinal function recovery etc.
Technology contents
The invention provides with aescine and its esters and treating abdominal distention and constipation purposes.
Aescine provided by the invention and its esters etc.The chemical compound that its architectural feature is made up of pentacyclic triterpene structure (nonpolar) and glycosidic linkage structure (polarity).Mainly contain 4 kinds of effective ingredient, be respectively aescine A, B, C and D.Wherein the content of aescine A is between 10-98%.(document sees reference: Wang Xuying, Zhao Yongfang.The research of the chemical constituent of Chinese medicine Semen Aesculi and aescine medical value.The Tangshan Teachers College journal.The 23rd the 5th phase of volume of calendar year 2001: 7-11).
Aescine that the present invention relates to and its esters can extract from plant and obtain, also can chemosynthesis, or make salt through the biological or chemical method.Salt comprising aescine sodium salt, potassium salt, aescine and basic amino acid composition, for example arginine aescine and with lysine, histidine, ornithine, the salt that 2,4 one DABs or sarcosine are made etc. (are seen Chinese patent: application number: 200510020572.7).
The invention provides that aescine and its esters are used for the treatment of because abdominal distention, the constipation due to diabetes, cardiovascular diseases, Senile disease, long-term bed patient, development in children defective, wound and operation and the congenital diseases.Mainly with full, glutted, appetite attenuating after meal early, flatulence, too much belch, anorexia, feel sick, vomiting or similar ulcer are chief complaint symptom.For example promote wound and postoperative intestinal function recovery, treatment diabetic gastroparesis, congenital megacolon, reflux esophagitis and constipation (comprising the constipation that constipation that senile constipation, long-term bed cause and other reasons cause) etc.Also comprise the treatment of stomach-esophageal regurgitation, esophagitis and keep the propelling wriggling deficiency that treatment, the intestinal pseudo obstruction relevant with the gastrointestinal motility functional disorder cause and gastrointestinal contents is detained and be the propelling campaign that recovers colon-as chronic constipation patient's long-term treatment.
Aescine provided by the invention and its esters can be used as the independent medication of effective ingredient, also can share with other materials, can make various types of agents according to the method for pharmaceutics with medical dressing in effective dose, comprise injection, oral formulations and through the preparation of skin mucosa delivery.Also can be added in food and the functional food and use.
Specific embodiment
The oral influence of embodiment 1. aescine sheets to the small intestine movement of mice ahead running
Animal and reagent: the aescine sheet is produced by Shandong Green Leaf Pharmaceutical Co., Ltd, specification 30mg/ sheet.Kunming mice is available from University Of Qingdao's animal center.
Method: get 50 of KM mices, body weight 18～20g, male and female half and half.Be divided into 5 groups at random, 10 every group, be respectively medicine high dose group, middle dosage group, low dose group, blank group and cisapride matched group.The dosage of high, medium and low dosage group is respectively 50mg/kg, 25mg/kg and 12.5mg/kg, and the dosage of cisapride is 10mg/kg, and the administration volume is 0.3ml/, and every day, gastric infusion was 1 time, successive administration 3 days.The blank group gavages the isometric(al) normal saline.30min after the last administration, every mice is irritated stomach with 0.1g/ml charcoal end suspension (being suspended in 2% cmc soln) 0.3mL respectively.Behind the 20min, the mice dislocation is caused death, open the abdominal cavity and take out small intestinal, be tiled on the pallet, measurement, is obtained the charcoal end and is advanced percentage rate to distance (small intestinal total length) and charcoal end advance distance between the ileocecus from pylorus.
Charcoal end propelling rate (%)=charcoal end advance distance (cm) ÷ small intestinal total length (cm) * 100% in small intestinal.
All data all represent with X ± sd, relatively t check between the employing group, with p＜0.05 as the significance,statistical index.
The result shows that aescine and its esters can obviously improve the charcoal end propelling rate of small intestinal, show the effect (table 1) that aescine and its esters have increases intestinal propulsion.
Table 1. aescine is to the influence of mouse small intestine charcoal end advance distance
| Group | Dosage (mg/kg) | Small intestinal length overall (cm) | Advance distance (cm) | Charcoal end propelling rate (%) |
| The blank group | Normal saline | 41.21±3.12 | 19.23±2.16 | 46.66±3.29 |
| High dose group | 40 | 42.46±3.64 | 38.26±2.64 | 90.11±3.85 * |
| Middle dosage group | 20 | 40.74±3.53 | 39.66±3.63 | 97.35±4.29 * |
| Low dose group | 10 | 42.25±3.04 | 27.38±4.16 | 64.50±5.22 * |
| The cisapride matched group | 10 | 41.62±3.41 | 36.32±3.12 | 87.27±3.09 * |
Compare with the blank group: p＜0.01
Embodiment 2.The low mice intestinal of the intestine movement function charcoal propulsive influence in end due to aescine is sodium intravenous is it right the coffee
Aescine is produced by Shandong Green Leaf Pharmaceutical Co., Ltd.Animal origin is with embodiment 1.
Get 25 of KM mices, male and female half and half, body weight 18～22g, water 24h is can't help in fasting, be divided into 6 groups at random, be respectively blank group, model group, high dose group, middle dosage group, low dose group and neostigmine matched group, except that the blank group, each organizes mice subcutaneous injection morphine 0.5mg/kg in advance, behind the 20min, the tail vein injection administration, the dosage of high, medium and low dosage group is respectively 5,2.5,1.25mg/kg, the dosage of neostigmine is 4mg/kg, and the administration volume is every 0.3ml.The blank group gives isometric normal saline.10min respectively organizes the charcoal end suspension of mouse gavaging 0.1g/ml after the administration, after 20min, takes off cervical vertebra and puts to death mice, presses the method for embodiment 1 and calculates charcoal end propelling rate.
Display model group intestinal propulsion rate is obviously suppressed as a result, compares P＜0.01 with the blank group.The intestinal propulsion rate (table 2) that aescine can obviously increase Small Intestine when being suppressed.
Table 2. aescine and sodium intravenous to the low mice intestinal of the intestine movement function charcoal propulsive influence in end due to the morphine
| Group | Dosage (mg/kg) | Number of animals (n) | Charcoal end propelling rate (%) |
| The blank group | 10 | 50.23±3.46 | |
| Model control group | 10 | 29.68±5.24 Δ | |
| High dose group | 5 | 10 | 59.72±6.25 * |
| Middle dosage group | 2.5 | 10 | 53.25±5.88 * |
| Low dose group | 1.25 | 10 | 43.114±4.52 * |
| Neostigmine | 4 | 10 | 52.14±4.10 * |
*Compare with model control group: p＜0.01;
ΔCompare with the blank group: p＜0.01
Embodiment 3. Semen Aesculi power balls are to the influence of senile abdominal distention personnel's gastrointestinal function
Semen Aesculi power ball is provided by Qingdao Qiyuan Drug Research Institute, is made up of Horse chest Nut P.E and Stichopus japonicus etc., and every ball contains aescine 10mg.Select old abdominal distention personnel's 30 examples for use, be divided into two groups of first, second at random, first group oral placebo, the second group is taken Stichopus japonicus power ball, and each 1, every day 3 times, observe the recovery situation of belch gas and abdominal distention, and mark according to feces discharge situation: abdominal distention, defecation do not improve, and count 0 fen; Abdominal distention alleviates, and defecation sensation is stronger than in the past, feces than medication before deliquescing, count 1 fen, abdominal distention disappears substantially, defecation is light, feces than medication before obviously deliquescing, count 2 fens; Abdominal distention disappears, and feces is thinning, counts 3 fens.
The result shows, Semen Aesculi power ball takes that 90% above patient's gastrointestinal function obviously improves (table 4) after 3 days.
Table 3 Stichopus japonicus power ball is to the influence of senile abdominal distention personnel's intestinal function
| Group | Belch gas incidence rate | The abdominal distention incidence rate | The accumulative total scoring |
| Matched group | 66.88％ | 87.67％ | 6 |
| Stichopus japonicus power ball | 11.60％ * | 9.29％ * | 38 * |
*Compare with the blank group: p＜0.01
The influence that embodiment 4. aescine arginine emulsifiable pastes recover the rat abdomen postoperative intestine functional
Animal and reagent, animal origin is with embodiment 1, aescine arginine emulsifiable paste (specification is 100mg/g for self-control, lot number 20050102).
Select 30 of wistar rats for use, be divided into 3 groups at random, be respectively sham operated rats, medicine group and matched group, 10 every group.Rat fasting 16 hours, irritate stomach after the chloral hydrate anesthesia and give the barium agent, sham operated rats is done abdominal incision, not seeking and visiting the abdominal cavity then sews up, open the abdominal cavity for all the other 2 groups, intestinal tube is sought and visited to the colon end from the stomach end, after the continued operation 2 times, in the ranks breaking joint closes after the ileum at 1cm place on the caecum cuts off about 1/2, closes the abdominal cavity.The sham operated rats and the matched group edge of a knife are smeared emulsion bases, and the medicine group is smeared aescine arginine emulsifiable paste, every about 0.5g, for three days on end.The single cage in operation back is raised, and every day is in the defecation situations of at 8 in the morning and 8 observations in evening rat.With the time point of seeing white feces as defecation time first.Taking out stitches in the operation back on the 5th day, observes the wound healing situation, according to the cell infiltration degree, inflammatory reaction is divided into 0,1,2,3 grade.The result shows that aescine arginine emulsifiable paste can obviously shorten the defecation time of rat, alleviates the inflammatory reaction (table 4) of edge of a knife surrounding tissue.
The influence that table 4 aescine arginine emulsifiable paste recovers the rat postoperative intestine functional
| Group | N | The inflammatory reaction total points | Defecation time |
| Matched group | 10 | 19 | 56.7±12.48 |
| Aescine arginine emulsifiable paste | 10 | 12 | 25.2±14.75 * |
| Sham operated rats | 10 | 17 | 36.8±9.76 |
Compare with matched group: p＜0.01
Claims (9)
1. aescine is in the purposes of alleviating abdominal distention and constipation.
2. the organic salt of aescine and inorganic salt are alleviated the purposes of abdominal distention and constipation.
3. be that active component is on the purposes way of alleviating abdominal distention and constipation with aescine and its esters.
4. according to described aescine of claim 1-3 and its esters etc.The chemical compound that its architectural feature is made up of pentacyclic triterpene structure (nonpolar) and glycosidic linkage structure (polarity).Mainly contain 4 kinds of effective ingredient, be respectively aescine A, B, C and D.Wherein the content of aescine A is between 10-98%.
5. can from plant, extract according to described aescine of claim 1-4 and its esters and obtain, also can chemosynthesis, or make salt through the biological or chemical method.The salt of forming comprising aescine sodium salt, potassium salt, aescine and basic amino acid, for example arginine aescine and with lysine, histidine, ornithine, the salt that 2,4 one DABs or sarcosine are made etc.
6. can be used for the treatment of according to the purposes of described alleviation abdominal distention of claim 1-3 and constipation and comprise because abdominal distention and the constipation due to diabetes, cardiovascular diseases, Senile disease, long-term bed patient, development in children defective, wound and operation and the congenital diseases.For example promote wound and postoperative intestinal function recovery, treatment diabetic gastroparesis, congenital megacolon, reflux esophagitis and constipation (comprising the constipation that constipation that senile constipation, long-term bed cause and other reasons cause) etc.Mainly with full, glutted, appetite attenuating after meal early, flatulence, too much belch, anorexia, feel sick, vomiting or similar ulcer are chief complaint symptom.Also comprise the treatment of stomach-esophageal regurgitation, esophagitis and keep the propelling wriggling deficiency that treatment, the intestinal pseudo obstruction relevant with the gastrointestinal motility functional disorder cause and gastrointestinal contents is detained and be the propelling campaign that recovers colon-as chronic constipation patient's long-term treatment.
7. can make medicine or food as effective ingredient with one or a class chemical constituent according to the described aescine of claim 1～7 and its esters, also can share as effective ingredient and make medicine and food with other chemical substances.
8. can make various types of agents according to the method for pharmaceutics according to described aescine of claim 1-6 and its esters with medical dressing in effective dose, comprise injection, oral formulations and through the preparation of skin mucosa delivery.For example make injection, injection powder injection, tablet, capsule, buccal tablet, sliver, gel, suppository etc., with injecting pathway, oral, containing approach and mucocutaneous route of administration to patient's administration.Also can be added in the food, use as food additive.
According to the clinical using dosage of people every day of described aescine of claim 1～8 and its esters in 5～800mg scope, the injecting pathway preferred dosage is 5mg～30mg scope, other approach preferred dosage are 60～300mg scope.
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| CN 200610009183 CN101023952A (en) | 2006-02-20 | 2006-02-20 | Use of aesin in releasing abdominal distention and astriction |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104902911A (en) * | 2012-11-21 | 2015-09-09 | Kbs研究有限公司 | Herbal supplements and methods of use thereof |
| WO2018113285A1 (en) * | 2016-12-22 | 2018-06-28 | 深圳翰宇药业股份有限公司 | Method for preparing sodium aescinate |
| WO2019136744A1 (en) * | 2018-01-15 | 2019-07-18 | 深圳市星银医药有限公司 | Composition of hippocastanum extract and linaclotide |
| CN111939166A (en) * | 2020-09-03 | 2020-11-17 | 中国药科大学 | Application of aescin in preparing medicine for treating ulcerative colitis |
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2006
- 2006-02-20 CN CN 200610009183 patent/CN101023952A/en active Pending
Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104902911A (en) * | 2012-11-21 | 2015-09-09 | Kbs研究有限公司 | Herbal supplements and methods of use thereof |
| CN107375369A (en) * | 2012-11-21 | 2017-11-24 | Kbs研究有限公司 | Herbal supplements and its application method |
| US10022413B2 (en) | 2012-11-21 | 2018-07-17 | KBS Research, LLC | Herbal supplements and methods of use thereof |
| US10940176B2 (en) | 2012-11-21 | 2021-03-09 | KBS Research, LLC | Herbal supplements and methods of use thereof |
| US11931394B2 (en) | 2012-11-21 | 2024-03-19 | KBS Research, LLC | Herbal supplements and methods of use thereof |
| WO2018113285A1 (en) * | 2016-12-22 | 2018-06-28 | 深圳翰宇药业股份有限公司 | Method for preparing sodium aescinate |
| WO2019136744A1 (en) * | 2018-01-15 | 2019-07-18 | 深圳市星银医药有限公司 | Composition of hippocastanum extract and linaclotide |
| CN110337302A (en) * | 2018-01-15 | 2019-10-15 | 深圳市星银医药有限公司 | A kind of hippocastanum extract and Linaclotide composition |
| CN110337302B (en) * | 2018-01-15 | 2023-07-21 | 深圳市星银医药有限公司 | Horse chestnut extract and linaclotide composition |
| CN111939166A (en) * | 2020-09-03 | 2020-11-17 | 中国药科大学 | Application of aescin in preparing medicine for treating ulcerative colitis |
| CN111939166B (en) * | 2020-09-03 | 2022-04-26 | 中国药科大学 | Application of aescin in preparing medicine for treating ulcerative colitis |
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