Shikonin tetramer compound and purpose thereof in pharmacy

A technology of shikonin and tetramer, which is applied in the fields of organic chemistry, anti-tumor drugs, drug combination, etc., can solve the problems of anti-complement and anti-tumor effects of shikonin tetramer compounds that have not been reported.
CN103086864BInactive Publication Date: 2015-01-07FUDAN UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
FUDAN UNIV
Publication Date
2015-01-07
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention belongs to the field of pharmacy, and relates to a purpose of a shikonin tetramer compound in preparing medicines. According to the invention, the shikonin tetramer compound is extracted from an ethyl acetate extract of a boraginaceae plant arnebia euchroma (Royle) Johnst. With an in-vitro complement activity evaluation test, it is verified that the compound has high inhibition effect and cytotoxic effect upon classical pathway and alternative pathway of a complement system. The compound provided by the invention has both inhibition effects upon classical pathway and alternative pathway of a complement system. The CH50 of the compound is 0.14 (plus or minus 0.01)-0.57 (plus or minus 0.11)mM, and AP50 is 0.06 (plus or minus 0.01)-0.16 (plus or minus 0.02)mM. The novel shikonin E in the compound has substantial inhibition effects against lung cancer cells (A549), prostate cancer cells (DU145), nasopharynx cancer cells (KB), and KB resistant strains (KBvin), wherein ED50 are respectively 5.00mM, 5.42mM, 3.71mM and 4.57mM. The compound can be used for preparing anti-complement or antitumor medicines.
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Description

technical field

[0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to shikonin tetramer compounds and their use in pharmacy, especially the use in preparing anti-complement or anti-tumor drugs. Background technique

[0002] It has been reported that overactivation of the complement system can lead to various diseases such as systemic lupus erythematosus, rheumatoid arthritis, and acute respiratory distress syndrome. At present, there is no ideal drug for the treatment of these diseases clinically. Studies have shown that the cost of researching and developing complement inhibitors directly from natural products is low, and most active ingredients can be directly digested and absorbed by the body as part of natural products. Drugs are getting more and more attention. Scholars at home and abroad have isolated a large number of monomeric compounds with inhibitory effects on the complement system from natural products including mari...

Claims

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