Isosteroidal alkaloid compound and use thereof in pharmaceuticals

A technology of isosteroid biological and alkali compounds, which is applied in the field of medicine and can solve problems such as pharmacological activity studies that have not yet been seen

Active Publication Date: 2020-04-07
FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the research on its chemical constituents at home and abroad is still in the initial stage, and so far, there have been no reports on its related pharmacological activities.

Method used

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  • Isosteroidal alkaloid compound and use thereof in pharmaceuticals
  • Isosteroidal alkaloid compound and use thereof in pharmaceuticals
  • Isosteroidal alkaloid compound and use thereof in pharmaceuticals

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1 Extracting Isosteroidal Alkaloid Compounds from Tuoli Fritillaria

[0016] (1) Extraction: Grinding dried Fritillaria bulbs (5.0 kg) and extracting by percolating with 95% ethanol at room temperature, concentrating under reduced pressure to obtain 127 grams of extract, suspending the extract in water, adding 5 % tartaric acid aqueous solution to adjust the pH to 2 for acidification, filter, and degrease the filtrate with dichloromethane, add ammonia water to the remaining water phase to adjust the pH to 11, extract with chloroform, and concentrate under reduced pressure to obtain 10.6 grams of total alkali;

[0017] (2) Separation: The total base is subjected to silica gel column chromatography (200-300 mesh), and the dichloromethane-methanol system (20:1→15:1→10:1→6:1→3:1→0: 1) Gradient elution, the amount of each gradient is 2 liters, and the fractions are collected, wherein the dichloromethane-methanol (10:1) fraction (1.7 g) is subjected to ODS reverse-pha...

Embodiment 2

[0023] Example 2 Determination of the Action Strength of Compounds of Formula (I) Antagonizing Acetylcholine-induced Tracheal Smooth Muscle Contraction

[0024] (1) The preparation method of the test sample: first make a 0.1M mother solution with an appropriate amount of DMSO, and then further dilute it to 10 -2 M and 10 -3 M, the final concentration of the test substance in the test system is 10 -4 M, 10 -5 M, 10 -6 M. The final concentration of DMSO is 0.1%;

[0025] (2) Preparation of Kreb's-Henseleit solution Weigh appropriate amount of sodium chloride, potassium chloride, anhydrous magnesium sulfate, potassium dihydrogen phosphate, anhydrous calcium chloride, sodium bicarbonate, D(+)- Glucose, dissolve in 2 liters of double distilled water and mix well, so that the concentration of each component is (mM): sodium chloride 120; potassium chloride 4.5; anhydrous magnesium sulfate 1.0; potassium dihydrogen phosphate 1.0; anhydrous calcium chloride 2.5; sodium bicarbonat...

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Abstract

The invention belongs to the technical field of medicines, relates to a novel isosteroidal alkaloid compound, and in particular, relates to the isosteroidal alkaloid compound which is separated from fritillaria tortifolia and has a structure (I), and an application of the isosteroidal alkaloid compound in preparation of asthma-relieving medicines. The compound is 5[beta]-cevine-3[alpha],20[beta]-diol-6-one, and experiments prove that the compound has a quite strong antagonistic effect on acetylcholine induced tracheal smooth muscle contraction, can be used for preparing the asthma-relieving medicines, and is used for preventing or treating bronchial asthma, asthma type bronchitis or obstructive emphysema diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a new isosteroid alkaloid compound, in particular to an isosteroid alkaloid compound isolated from fritillary fritillaria and its application in preparing antiasthma medicine. Background technique [0002] The prior art discloses that the traditional Chinese medicine Fritillaria is the dry bulb of various plants of the genus Fritillaria in the family Liliaceae. It has a long history of medicinal use and has the effects of clearing away heat and moistening the lungs, reducing phlegm and relieving cough. The Chinese Pharmacopoeia (2015 edition) contains varieties such as Chuan Fritillaria, Yi Fritillaria, Zhejiang Fritillaria, Flat Fritillaria, and Hubei Fritillaria. Fritillariatortifolia (Fritillariatortifolia X.Z.Duan&X.J.Zheng) is a unique species in Xinjiang, and it is only distributed in the Balik Mountains of Tacheng Prefecture. Its dried bulbs have been used in Uighur medicine...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61P11/00A61P11/06
CPCC07J71/0042A61P11/00A61P11/06Y02A50/30
Inventor 侯爱君阿布力米提·伊力雷春阿吉艾克拜尔·艾萨胡翥
Owner FUDAN UNIV
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