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A kind of steroid compound and its use

A technology of compounds and steroids, applied in the field of steroids, can solve the problems of strong cardiotoxicity and cytotoxicity, affecting clinical application, etc., and achieve the effect of cardiotonic effect, significant effect, and weak cytotoxicity

Active Publication Date: 2019-07-12
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these compounds have good cardiotonic activity, most of them also have strong cardiotoxicity and cytotoxicity, which seriously affects their clinical application.

Method used

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  • A kind of steroid compound and its use
  • A kind of steroid compound and its use
  • A kind of steroid compound and its use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1: the preparation of formula II compound

[0043] a) Using 2 kg of dried toad venom pulp as raw material, add 8 times the amount of 95wt% methanol aqueous solution, and carry out reflux extraction for 3 times, each time for 2 hours; combine the filtrates, concentrate under reduced pressure until there is no alcohol smell, and obtain a liquid extract; The paste was suspended in water, and extracted with dichloromethane until the extract was colorless; the extracts were combined, concentrated under reduced pressure to extract, and a crude extract was obtained;

[0044] b) The crude extract is separated by silica gel column chromatography, and the volume ratio is 10:10:1, 8:8:1, 6:6:1, 4:4:1, 2:2:1, 1: A 1:1 mixed solvent of petroleum ether-dichloromethane-methanol was used for gradient elution, each eluent was evaporated under reduced pressure and then analyzed by TLC to obtain eight components according to the order of elution, denoted as Fr.E1~ E8;

[0045...

Embodiment 2

[0052] Embodiment 2: the preparation of formula III compound

[0053] a) Using 2 kg of dried toad venom pulp as raw material, add 8 times the amount of 60wt% methanol aqueous solution, and carry out reflux extraction for 3 times, each time for 2 hours; combine the filtrates, concentrate under reduced pressure until there is no alcohol smell, and obtain a liquid extract; The paste was suspended in water, and extracted with dichloromethane until the extract was colorless; the extracts were combined, concentrated under reduced pressure to extract, and a crude extract was obtained;

[0054] b) The crude extract is separated by silica gel column chromatography, and the volume ratio is 10:10:1, 8:8:1, 6:6:1, 4:4:1, 2:2:1, 1: A 1:1 mixed solvent of petroleum ether-dichloromethane-methanol was used for gradient elution, each eluent was evaporated under reduced pressure and then analyzed by TLC to obtain eight components according to the order of elution, denoted as Fr.E1~ E8;

[005...

Embodiment 3

[0062] Embodiment 3: the preparation of formula IV compound

[0063] a) Using 2 kg of dried toad venom pulp as raw material, add 8 times the amount of 60wt% methanol aqueous solution, and carry out reflux extraction for 3 times, each time for 2 hours; combine the filtrates, concentrate under reduced pressure until there is no alcohol smell, and obtain a liquid extract; The paste was suspended in water, and extracted with dichloromethane until the extract was colorless; the extracts were combined, concentrated under reduced pressure to extract, and a crude extract was obtained;

[0064] b) The crude extract is separated by silica gel column chromatography, and the volume ratio is 10:10:1, 8:8:1, 6:6:1, 4:4:1, 2:2:1, 1: A 1:1 mixed solvent of petroleum ether-dichloromethane-methanol was used for gradient elution, each eluent was evaporated under reduced pressure and then analyzed by TLC to obtain eight components according to the order of elution, denoted as Fr.E1~ E8;

[0065...

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Abstract

The invention discloses a steroid compound and application thereof. The steroid compound is a compound having a structure shown as a formula I or pharmaceutically acceptable salt, tautomer, stereisomer, a precursor compound, hydrate or solvate of the compound (show in the description). An experiment shows that H on the steroid compound C10 having the structure shown as the formula I is substituted by a hydrogen peroxide group, the cardiac muscular tension of the frog heart can be remarkably increased, the steroid compound has a remarkable cardiotonic effect, the cytotoxicity is lower, and the steroid compound is efficient and low in toxicity, can be expected to serve as an active ingredient for preparation of drugs for preventing and / or treating acute heart failure and has a wide application prospect.

Description

technical field [0001] The invention relates to a steroid compound and its application, belonging to the field of medicine. Background technique [0002] Heart failure (HF) refers to a pathophysiological state in which abnormal cardiac function leads to the inability of the heart to pump blood to meet the needs of tissue metabolism ([J]. Circulation, 2008, 117(4): e25-e146). Heart failure is a complex clinical manifestation of the final progression of various heart diseases. Blood flow in the systemic and pulmonary circulation and hypoperfusion of human tissues are its main characteristics. The main pathophysiological mechanism is dysfunction of the left ventricle and / or right ventricle and abnormal regulation of neurohumoral fluid. , resulting in fluid retention, reduced exercise tolerance and significantly shortened survival time ([M]. People's Medical Publishing House, 2009:129.). At present, it is believed that the pathogenesis of heart failure is related to the patholo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J71/00A61K31/58A61P9/04
CPCC07J71/0021
Inventor 李医明吴迎春陈瀛澜郭夫江吕少东张捷伍宇娟
Owner SHANGHAI UNIV OF T C M
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