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Application of transformed type ginsenosides in preparation of hypolipidemic drugs

The technology of a hypolipidemic drug and ginsenoside, which is applied in the field of biomedicine, can solve the problems of single type and high incidence of side effects, and achieve the effects of small molecular weight, strong biological activity and strong fat solubility.

Pending Publication Date: 2020-06-19
SHENZHEN INST FOR DRUG CONTROL SHENZHEN TESTING CENT OF MEDICAL DEVICES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinical lipid-lowering drugs such as statins, Myzhebuyi (cholesterol absorption inhibitors) and bile acid sequestrants occupy a dominant position in the market. Blood lipid-lowering drugs, the incidence of side effects of Chinese patients with dyslipidemia is higher than that of Western countries
[0003] Traditional Chinese medicine is an important resource bank for the development of blood lipid-lowering drugs. However, currently there are few prescription drugs for blood lipid-lowering traditional Chinese medicine, and the types are single

Method used

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  • Application of transformed type ginsenosides in preparation of hypolipidemic drugs
  • Application of transformed type ginsenosides in preparation of hypolipidemic drugs
  • Application of transformed type ginsenosides in preparation of hypolipidemic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] In this example, a transformed ginsenoside is prepared, and its structure identification and content determination are carried out. The specific operations are as follows:

[0066] (1) Transformation of transformed ginsenosides

[0067] Panax ginseng stem and leaf saponins (80% total saponin content, UV detection) were purchased from Jilin Hongjiu Biotechnology Co., Ltd. Weigh 300 g of American ginseng stem and leaf saponins, dissolve it in 1.5 L of distilled water, and place it in a high-pressure steam sterilizer for heating at 130° C. for 3 h. Take out, cool and set aside.

[0068] (2) Enrichment of transformed ginsenosides

[0069] Load the converted saponin onto HP-20 macroporous resin, elute with 2 times the volume of water, 30%, 60%, 80%, and 95% (v / v) ethanol, and collect the 60% ethanol eluate , concentrated with a rotary evaporator at 45° C., and freeze-dried to obtain the transformed ginsenoside.

[0070] (3) Structure identification and content determinat...

Embodiment 2

[0088] In this example, the hamster, which is very similar to the cholesterol metabolism of the human body, was selected as the experimental animal model. In the study of lowering blood lipids, hamsters have more advantages than rats and mice. First of all, hamsters are similar to humans in that they are prone to high TC and high TG hyperemia caused by the increase of dietary cholesterol content, while rats and mice are less sensitive to the increase of dietary cholesterol than hamsters, and their blood TG content will also decrease. Secondly, the symptoms of hypercholesterolemia caused by increased dietary cholesterol in hamsters are similar to those in humans, and they all show elevated TC, LDL-C, and HDL-C. In rats and mice, with the increase of high cholesterol in the diet, the level of LDL-C in the blood increased, but the level of HDL-C decreased significantly. Thirdly, after ingesting a high-cholesterol diet, the proportion of HDL-C in TC in human and hamster blood is ...

Embodiment 3

[0140] The formation of macrophage-derived foam cells is an early change in the development and progression of atherosclerosis. In the pathophysiological process of atherosclerosis, macrophage-derived foam cells play a crucial role from the early fatty streak stage to the further plaque formation stage. Macrophages can phagocytose and absorb a large amount of modified low-density lipoproteins under the endothelium, and absorb cholesterol in cells more than excretion of cholesterol. At this time, macrophages become foam cells overloaded with lipids. In this example, Raw264.7 macrophages were induced into foam cells by ox-LDL, a foam model was established, the intracellular lipids were observed by Oil Red O staining, and the improvement effect of transformed ginsenosides on intracellular lipids was explored. The specific operation is as follows:

[0141] (1) Cell culture and induction of differentiation

[0142] RAW264.7 cells were statically cultured in DMEM medium containing...

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Abstract

The invention relates to an application of transformed type ginsenosides or pharmaceutically acceptable sodium, ester, and solvate in preparation of hypolipidemic drugs. The transformed type ginsenosides are found for the first time to have effect of lowering blood fat, and can reduce contents of TC and non-HDL-C in the blood, and reduce ratio of the contents of the non-HDL-C and the HDL-C; also can suppress formation of foam cells to reduce area of atherosclerotic plaque on the inner walls of aorta, can help to develop a new hypolipidemic drug suitable for patients with abnormal blood lipids,and provides theoretical and technical guidance for prevention and control of the vascular diseases.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to the application of a transformed ginsenoside in the preparation of blood lipid-lowering drugs, in particular to the application of a transformed ginsenoside or a pharmaceutically acceptable salt, ester, and solvate thereof in the preparation of blood lipid-lowering drugs. application in medicine. Background technique [0002] Cardiovascular disease is the number one killer of human health. It has the characteristics of "high morbidity, high disability rate, high mortality rate, high recurrence rate, and many complications", that is, "four highs and one many". So far, more than 300 risk factors for cardiovascular disease have been discovered, among which dyslipidemia, hypertension, diabetes, smoking, and obesity are the main risk factors for cardiovascular disease events. Among these risk factors, dyslipidemia is the most manageable risk factor for cardiovascular disease. Dysl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61P3/06
CPCA61K31/704A61P3/06A61K2300/00
Inventor 王丽君王铁杰鲁艺殷果张启航王珏刘霞妹刘凯双
Owner SHENZHEN INST FOR DRUG CONTROL SHENZHEN TESTING CENT OF MEDICAL DEVICES
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