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Bisindole alkaloid compound or pharmaceutically acceptable salt thereof, and preparation method and application thereof

A technology of bis-indole alkaloids and indole alkaloids, which can be used in organic chemistry, drug combinations, and pharmaceutical formulations, and can solve problems such as large side effects

Active Publication Date: 2019-09-20
SHANDONG ANALYSIS & TEST CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The inventors found that the current clinical treatment of diabetic nephropathy mainly uses glucocorticoids and immunosuppressants. Although the curative effect is remarkable, the long-term use has relatively large side effects

Method used

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  • Bisindole alkaloid compound or pharmaceutically acceptable salt thereof, and preparation method and application thereof
  • Bisindole alkaloid compound or pharmaceutically acceptable salt thereof, and preparation method and application thereof
  • Bisindole alkaloid compound or pharmaceutically acceptable salt thereof, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0094]Take 18kg of air-dried rhizomes of the milk vine plant, heat and reflux with 95% ethanol to extract 4 times, recover the solvent until there is no alcohol smell, add water to suspend, adjust the pH to 2 with 2% HCl, extract 4 times with dichloromethane, The aqueous layer was adjusted to pH 10 with 10% NaOH, extracted 4 times with dichloromethane, recovered dichloromethane to obtain total alkaloids, mixed with silica gel, 200-300 mesh silica gel column chromatography, divided into 8 sections (C1-C8 Section), C1 section uses petroleum ether / acetone 20:1, 15:1, 10:1, 5:1, 2:1, 1:1 as eluent, 150g silica gel column chromatography, through thin layer chromatography (TLC ) after pointing the board, it is determined to be divided into 16 sections (C1-1~C1-16), and the C1-13 section is divided into dichloromethane / methanol 100:1, 80:1, 50:1, 40:1, 20:1, 15:1, 10:1, 8:1, 4:1, 2:1 gradient elution, analyzed by TLC spot plate, combined into 3 segments (C1-13A, C1-13B and C1-13C), C...

Embodiment 2

[0106] According to the method of Example 1, firstly obtain bismuthine A, add 4% hydrochloric acid solution to pH = 4, filter and dry to prepare bismuthine A hydrochloride.

Embodiment 3

[0108] According to the method of Example 1, firstly obtain biscarina, add 4% sulfuric acid ethanol solution to pH = 4, filter, dry, and prepare biscarina sulfate.

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Abstract

The present invention provides a bisindole alkaloid compound or a pharmaceutically acceptable salt thereof, and a preparation method and an application thereof. The compound has a structure represented by formula (I) shown in the description; and in the formula, R1 is selected from hydrogen, a hydroxyl group, COOR', a C1-10 alkoxy group, a C2-10 alkenyloxy, a C2-10 alkynyloxy group and a halogen atom, the hydroxyl group can be substituted with a C1-10 alkoxy group, a C2-10 alkenyloxy group, C2-10 alkynyloxy or a halogen atom when the R1 is the hydroxyl group, R3 is selected from hydrogen or COOR', R2, R4 and R5 are respectively independently selected from hydrogen, a hydroxyl group, a carbonyl group, a C1-10 alkoxy group, a C2-10 alkenyloxy group and a halogen atom, R' is selected a C1-10 alkyl group, a C2-10 alkenyl group and a C2-10 alkynyl group, and the halogen atom is preferably fluorine, chlorine, bromine or iodine. The bisindole alkaloid compound of the formula or the pharmaceutically acceptable salt thereof has an amyloid protein-beta inhibition activity, and also has an activity of inhibiting podocyte injuries caused by high sugar.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a bisindole alkaloid compound or a pharmaceutically acceptable salt thereof and a preparation method and application thereof. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Apocynaceae (Apocynaceae) is a family with high medicinal value in dicotyledonous plants, with about 250 genera and more than 2,000 species. There are 47 genera and about 180 species in China, mainly distributed in the south of the Yangtze River and Taiwan Province. More genera in this family are rich in alkaloids with better pharmacological activity, such as the genus Rauwolfia for lowering blood pressu...

Claims

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Application Information

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IPC IPC(8): C07D519/00A61K31/4375A61P25/28A61P3/10A61P13/12A61K36/24
CPCA61K36/24A61P3/10A61P13/12A61P25/28C07D519/00
Inventor 王志伟闫慧娇穆岩林云良耿岩玲刘伟王晓
Owner SHANDONG ANALYSIS & TEST CENT
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