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24(R)-pseudoginsenoside-GQ as well as semisynthesis method and medicinal application thereof

A technology of pseudoginsenosides and ginsenosides, which is applied in the field of 24-pseudoginsenoside-GQ and its semi-synthesis, can solve the problems that have not been seen, and achieve excellent and significant curative effects

Inactive Publication Date: 2010-11-10
李平亚
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there is no report on the synthesis method and compound of 24(R)-pseudoginsenoside-GQ. This compound is a new compound and is the first synthesis; the new drug use of this compound is the first discovery

Method used

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  • 24(R)-pseudoginsenoside-GQ as well as semisynthesis method and medicinal application thereof
  • 24(R)-pseudoginsenoside-GQ as well as semisynthesis method and medicinal application thereof
  • 24(R)-pseudoginsenoside-GQ as well as semisynthesis method and medicinal application thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1 24

[0029] Experimental example 1. Effect of 24(R)-pseudoginsenoside-GQ on hemorrhagic shock

[0030] 1. Experimental materials and methods

[0031] Materials: 6 beagle dogs; 24(R)-PGQ: 10mg / ml aqueous solution

[0032] Methods: The dog was anesthetized intravenously with pentobarbital sodium (1ml he), was fixed on the operating table in supine position, the trachea was separated, and the trachea was intubated. Separate the common carotid artery and connect it to RM-6000 four-lead physiological recorder to measure: BP (SBP / DBP); separate the right bone artery and measure LVSP, LVEDP, ±dp / dt; separate the right femoral vein for drug use .

[0033]Separate the right-dipping femoral artery, prepare for arterial bloodletting, connect ECG leads, measure ECG to calculate HR, connect force sensor with silk thread at the xiphoid process skin, measure respiratory rate, stabilize for 10 minutes after the operation, record all normal indicators, and then Bleeding through the femoral arter...

experiment example 2 24

[0078] Experimental Example 2. Effect of 24(R)-Pseudoginsenoside-GQ on Hemodynamics of Normal Anesthetized Dogs (n=6)

[0079] 1. Experimental materials and methods

[0080] Materials: 6 Beagle dogs, weighing 13kg to 15kg, 3 males and 3 males, 24(R)-pseudoginsenoside-GQ: 10mg / ml solution;

[0081] Method: The method is the same as Experiment 1, so it is omitted.

[0082] 2. Results

[0083] 1. Effect on lipid peroxide (LPO)

[0084] The content of 120'LPO in the 24(R)-PGQ small and high dose groups after administration was significantly lower than that in the saline control group, and the difference between the two groups was significant (p<0.05).

[0085] The content of 120'LPO in the dopamine group was significantly lower than that in the saline control group after administration, and the difference between the two groups was significant (p<0.05). The results are shown in Table 2-1.

[0086] Table 2-124(R)-PGQ Effect on LPO(A / ml)

[0087]

[0088] p<0.05 vs. 0.9% ...

experiment example 3

[0097] Experimental example three, MTT (tetrazolium salt) method to measure the selection of the killing effect of 24 (R)-pseudoginsenoside-GQ on tumor cells

[0098] (1) Experimental design

[0099] Tumor lines used: MCF-7 human breast cancer cells, PC3M human prostate cancer cells, NCI-H446 human lung cancer cells, Helas human cervical cancer cells, H8 human colon cancer cells, SHG-44 human glioma cells, SK-OV- 3 human ovarian cancer cells, 7 human tumor cell lines.

[0100] (Note: Different cells use different culture medium: RPMI1640, IMDM, DMEM.)

[0101] Test grouping: 24(R)-pseudoginsenoside-GQ dosage group:

[0102] 1.0μg / ml, 2.5μg / ml, 5μg / ml, 7.5μg / ml, 10μg / ml, 12.5μg / ml, 15μg / ml, 17.5μg / ml, 20μg / ml;

[0103]Blank control group: solvent;

[0104] Positive control group: 5-fluorouracil (1.0 μg / ml).

[0105] (2) method:

[0106] ① Preparation of MTT solution: put 250mgMTT into a small beaker, add 50ml of PBS (pH7.4, 0.01M), stir for 30min, prepare a solution with ...

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Abstract

The invention relates to 24(R)-pseudoginsenoside-GQ as well as a semisynthesis method and medicinal application thereof, belonging to a new compound as well as a synthesis method and medicinal application thereof. In the invention, 20(S)-ginsenoside Rg3 or 20(R)-ginsenoside Rg3 is used as a raw material, and under an acid condition, a new compound is synthesized through the steps of oxidization, cyclization, and the like, wherein the chemical name of the new compound is 3-O-[beta-D-glucopyranose-(1-2)-beta-D-glucopyranose group]-damma-20S, 24R-epoxy-3beta, 12beta, 25-triol being short for 24(R)-pseudoginsenoside-GQ, the productivity of which reaches higher than 80 percent. The 24(R)-pseudoginsenoside-GQ has wide medicinal application in preparing medicaments for treating coronary heart diseases, myocardial ischemia, ischemic shocks, arrhythmia and reperfusion damages and resisting cancer.

Description

technical field [0001] The invention relates to 24(R)-pseudoginsenoside-GQ and its semi-synthetic method, and its application in the preparation of drugs for treating myocardial ischemia, ischemic shock, arrhythmia, reperfusion injury and anticancer. Background technique [0002] Since ginsenosides were confirmed as the main effective components in ginseng and American ginseng, chemists have devoted themselves to the synthesis of certain monomeric saponins and the transformation of effective monomers. At present, there are mainly the following methods in research and application, such as acid hydrolysis, alkali hydrolysis, enzymatic hydrolysis, condensation and so on. The first three methods are mainly between total saponins and monomeric saponins, by hydrolyzing a certain part or parts of the molecule to realize the conversion of a certain monomeric saponin or several monomeric saponins; Aglycone is obtained through a glycoside reaction to obtain a certain monomer compound...

Claims

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Application Information

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IPC IPC(8): C07J17/00A61K31/7048A61P9/10A61P9/06A61P35/00
Inventor 李平亚刘金平杜秀娟卢丹
Owner 李平亚
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