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Application of a kind of acetylgastrodin and acetylgastrodin derivatives

A technology of acetylgastrodin and its derivatives, applied in the field of medicine, to achieve the effect of reducing stress and increasing the number of bacteria

Active Publication Date: 2020-02-14
KPC PHARM INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] With the continuous development of society, the prevalence of fatty liver disease is higher, and the number of people with fatty liver is increasing. The drugs for treating fatty liver on the market are far from meeting the market demand. Therefore, it is necessary to develop a fatty liver drug that meets the market demand. very necessary

Method used

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  • Application of a kind of acetylgastrodin and acetylgastrodin derivatives
  • Application of a kind of acetylgastrodin and acetylgastrodin derivatives
  • Application of a kind of acetylgastrodin and acetylgastrodin derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Effects of acetylgastrodin and acetylgastrodin derivatives on blood lipid CHO and TG values ​​in rat model of non-alcoholic fatty liver

[0031] Compounds involved in Table 1 Examples

[0032]

[0033] Experimental materials and methods:

[0034] 1. Animals and materials

[0035] 165 SD rats were provided by the Animal Center of Kunming Medical University, weighing 180±20g, free to eat and drink, and kept at 22±2°C. Acetylgastrodin and acetylgastrodin derivatives are self-made by Kunpharm Group.

[0036] Silibinin Capsules were purchased from Tianjin Tasly Pharmaceutical Co., Ltd.; CHO, TG, and were tested in the Department of Biology of Kunming Pharmaceutical Group.

[0037] 2. Establishment and grouping of non-alcoholic fatty liver rat model

[0038] 2.1 Grouping:

[0039] 165 rats were randomly divided into 11 groups, namely blank group, positive group, model group, KPC-3000157 group, KPC-3000159 group, KPC-3000161 group, KPC-3000162 group, KPC-3000165 group,...

Embodiment 2

[0051] Acetylgastrodin and acetylgastrodin derivatives upregulate Bacteroides bacteria in the gut of rats with nonalcoholic fatty liver disease

[0052] As Gram-negative cells, Bacteroides are the most dominant commensal bacteria in the gut. Bacteroides is generally considered to be an obligate anaerobic bacterium of chemoorganic nutrition in the gut, and we found that the progression of non-alcoholic fatty liver disease was associated with a decline in intestinal Bacteroides. A large number of articles have demonstrated that Firmicutes significantly increased in the intestinal tract of obese patients, while Bacteroidetes decreased. figure 1 Shown is the relative quantification of rat fecal bacteria (Bacteroidetes). Compared with normal healthy rats, the relative content of Bacteroides (Firmicutes) in the feces of nonalcoholic fatty liver rats was significantly reduced, and the bacteria of Bacteroides in rats treated with acetylgastrodin and acetylgastrodin derivatives return...

Embodiment 3

[0054] Acetylgastrodin and acetylgastrodin derivatives inhibit alpha-proteobacteria in the gut of rats with nonalcoholic fatty liver disease

[0055] Proteus species are parasites and pathogens of humans and animals. Proteus is widely distributed in nature and in the intestinal tract of humans or animals. The majority of Proteus bacteria are Gram-negative bacteria. Proteus food poisoning is one of the common food poisoning in our country. Proteus bacteria that cause food poisoning are mainly P. vulgaris and P. mirabikis. Proteus food poisoning also includes Providencia (Providencid) in Rettgeri Providencia (P. rettgeri) and Morganella (Morganella) in Morganella (M. morganii).

[0056] In this invention, we found that the progression of nonalcoholic fatty liver disease was associated with an increase in intestinal α-proteobacteria. Importantly, we found that oral administration of acetylgastrodin and acetylgastrodin derivatives inhibited the rise of intestinal α-proteobacte...

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Abstract

The invention discloses application of acegastrodine and an acegastrodine derivative. The application of the acegastrodine and the acegastrodine derivative refers to application of the acegastrodine and the acegastrodine derivative in preparing fatty liver treatment medicines, the acegastrodine and the acegastrodine derivative are of structures as shown in the specification, and in the formula, R is H or a compound residue with bioactivity. The invention provides the application of the acegastrodine and the acegastrodine derivative in preparing medicines for treating non-alcoholic fatty liver diseases, and novel options are provided for clinical treatment on non-alcoholic fatty liver diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of acetylgastrodin and acetylgastrodin derivatives. Background technique [0002] Nonalcoholic fatty liver disease (NAFLD) has become an important cause of chronic liver disease in many areas, among which nonalcoholic steatohepatitis (NASH) has the highest incidence. Non-alcoholic steatohepatitis is characterized by patients without a history of alcoholism, but histological changes are similar to alcoholic hepatitis with hepatomegaly and elevated serum transaminases. Severe cases can develop into liver fibrosis, cirrhosis, and even liver cancer. [0003] Studies have shown that the imbalance of intestinal flora structure can lead to the increase of endotoxin in the blood plasma of the host circulatory system, induce continuous low-grade inflammation, block the intracellular signal transmission system of insulin, and lead to insulin resistance. Insul...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7034A61K31/706A61P1/16
CPCA61K31/7034A61K31/706
Inventor 宋立明杨兆祥刘一丹普俊学董知旭
Owner KPC PHARM INC