Search

CN-122011075-A - Wilfoside C1N and Cynanchum otophyllum glycoside A, and separation method and application thereof in preparation of medicine for treating constipation

CN122011075ACN 122011075 ACN122011075 ACN 122011075ACN-122011075-A

Abstract

The invention provides wilfoside C N and cynomorium songaricum glycoside A, a separation method thereof and application thereof in preparing medicines for treating constipation, and belongs to the technical field of medicines. Crushing the root tuber of Cynanchum auriculatum, percolating with ethanol, concentrating under reduced pressure to obtain extract, dissolving, separating and purifying by multiple column chromatography to obtain wilfoside C N and Cynanchum otophyllum glycoside A, wherein wilfoside C N and Cynanchum otophyllum glycoside A have application value in preparing medicine for treating constipation, are beneficial to saving raw material resources, reducing production cost and improving medication safety.

Inventors

  • SHEN YONG
  • ZHANG LUYUAN
  • XU XIAOYU
  • CHEN CHAO
  • LOU HONGBO

Assignees

  • 云南农业大学

Dates

Publication Date
20260512
Application Date
20260123

Claims (7)

  1. 1. A method for separating wilfoside C N and cynomorium songaricum methylglucoside, which is characterized by comprising the following steps: S1, crushing the root tuber part of the Cynanchum parthenocarpum, percolating with ethanol, concentrating under reduced pressure to obtain extract, dissolving, separating by silica gel column chromatography, and gradient eluting with chloroform-methanol solution to obtain 7 fractions, wherein the fractions are Fr. -Fr.; s2, separating the selected fraction Fr. 2 by silica gel column chromatography, carrying out gradient elution on petroleum ether-acetone solution to obtain 3 fractions, recording the 3 fractions as Fr. 2.1.1-Fr. 2.3.3, separating the selected fraction Fr. 2.2.2 by an ODS column, carrying out gradient elution on methanol-water solution to obtain 8 fractions as Fr..2.1-Fr. 2.2.8, and purifying the fraction Fr..2.4 to obtain the cynaroside A; S3, separating the selected fraction Fr. by silica gel column chromatography, eluting with chloroform-methanol solution to obtain 4 fractions, namely Fr., 3.1-Fr., 3.4, separating the selected fraction Fr., 3.3 by ODS column, and performing gradient elution with methanol-water solution to obtain 2 fractions, namely Fr., 3.1-Fr., 3.3.2, wherein the fraction Fr., 3.3.2 is purified to obtain wilfoside C N.
  2. 2. The separation method according to claim 1, wherein the chloroform-methanol solution gradient elution in step S1 has a volume ratio of 20:1 to 1:1.
  3. 3. The separation method according to claim 1, wherein the petroleum ether-acetone solution gradient elution in step S2 has a volume ratio of 3:1 to 3:3, and the methanol-water solution gradient elution has a volume ratio of 40:60 to 100:0.
  4. 4. The separation method according to claim 1, wherein the chloroform-methanol solution volume ratio in step S3 is 20-30:1, and the methanol-water solution gradient elution volume ratio is 50:50 to 100:0.
  5. 5. Wilfoside C1N and Cynanchum otophyllum glycoside prepared by the separation process according to any one of claims 1 to 4.
  6. 6. Use of wilfoside C N and cynaropicrin a according to claim 5 in the preparation of a medicament for the treatment of constipation.
  7. 7. The use according to claim 6, wherein said wilfoside C N and qingyang ginseng glucoside a are formulated as tablets, capsules, granules, oral liquid preparations, subcutaneous administration preparations or suppositories.

Description

Wilfoside C1N and Cynanchum otophyllum glycoside A, and separation method and application thereof in preparation of medicine for treating constipation Technical Field The invention relates to the technical field of medicines, in particular to wilfoside C N and Cynanchum otophyllum glycoside A, a separation method thereof and application thereof in preparing a medicine for treating constipation. Background Constipation, particularly chronic functional constipation, is one of the most common dysfunctions of the digestive system, and its pathophysiological mechanism is complex, mainly involving slow colonic transport, discoordination of pelvic floor muscles during defecation, and abnormal intestinal sensory function. These changes result in excessive residence time of the stool in the colon, excessive absorption of moisture, and formation of dry and hard stool, accompanied by a series of clinical symptoms such as laborious defecation, incomplete feeling of defecation, and reduced frequency of defecation. The special features are that the spontaneous defecation is less than 3 times per week, excessive force is needed when defecation is performed, anorectal obstruction or blockage is caused, and the defecation is needed to be assisted by a manual method, so that the life quality and physical and mental health of patients are seriously affected. Along with the change of modern dietary structure (such as insufficient dietary fiber intake), the increase of life rhythm, the aging of social population and the aggravation of the influence of mental and psychological factors, the prevalence of constipation has a remarkable rising trend in the global scope. Epidemiological investigation shows that the prevalence of chronic constipation in adults in our country is about 4% -10%, and increases with age, with prevalence of up to 15% -20% in people over 60 years old. Chronic constipation not only causes discomfort such as abdominal distension, abdominal pain and anorexia, but also can induce cardiovascular and cerebrovascular accidents after long-term defecation, and is closely related to colorectal diseases and anxiety depression, so that the chronic constipation becomes an important public health problem and brings continuous burden to individuals, families and social medical resources. The key pathophysiological basis of constipation is intestinal nerve-muscle dysfunction and intestinal content water metabolism imbalance. Normal intestinal function depends on the dynamic balance of excitatory (e.g. acetylcholine, 5-hydroxytryptamine) and inhibitory (e.g. nitric oxide) neurotransmitters of the enteric nervous system. Experimental administration of opioid receptor agonists (such as loperamide) can significantly inhibit intestinal peristalsis and intestinal fluid secretion, resulting in reduced intestinal propulsion and dry stool, and successful establishment of a functional constipation model, confirming that intestinal motility is highly dependent on excitatory neuromodulation. The concentration of key neurotransmitters (e.g., 5-HT) in colonic tissue and their receptor expression levels, as well as the activity of inhibitory mediators (e.g., nitric oxide), are closely related to intestinal transport function and fecal characteristics. When excitatory transmitters are relatively deficient or inhibitory signals are too strong, they can lead to weakness of the colonic smooth muscle contraction, delay of transmission, and concomitant damage to the intestinal mucosal barrier and local inflammatory response, thus forming a vicious circle of constipation. Therefore, the evaluation of the intestinal canal propulsion rate and the fecal water content state has important significance for judging the severity of constipation and selecting a treatment target. Disclosure of Invention The invention aims to provide wilfoside C N and Cynanchum otophyllum glycoside A, a separation method thereof and application thereof in preparing a medicine for treating constipation, which are beneficial to saving raw material resources, reducing production cost and improving medication safety. The technical scheme of the invention is realized as follows: the invention provides a wilfoside C N separation method of cynomorium songaricum and a cynomorium songaricum, which comprises the following steps: S1, crushing the root tuber part of the Cynanchum parthenocarpum, percolating with ethanol, concentrating under reduced pressure to obtain extract, dissolving, separating by silica gel column chromatography, and gradient eluting with chloroform-methanol solution to obtain 7 fractions, wherein the fractions are Fr. -Fr.; s2, separating the selected fraction Fr. 2 by silica gel column chromatography, carrying out gradient elution on petroleum ether-acetone solution to obtain 3 fractions, recording the 3 fractions as Fr. 2.1.1-Fr. 2.3.3, separating the selected fraction Fr. 2.2.2 by an ODS column, carrying out gradient elution on methanol-water solution to obta