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Indolocarbazole compounds as well as preparation method and application of indolocarbazole

A technology of indolecarbazoles and compounds, which is applied in the field of marine actinomycete culture and preparation of compounds, can solve the problems of non-natural sources, etc., and achieve the effects of simple experimental operation, good application prospects, and easy expansion of production

Active Publication Date: 2017-12-01
浙江美新控股有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, this type of compound also has good activity on cell cycle-related kinases and nuclear topoisomerases, but it is worth noting that no matter whether it is artificially synthesized or structurally modified, it is not a natural source except UCN-01 metabolite

Method used

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  • Indolocarbazole compounds as well as preparation method and application of indolocarbazole
  • Indolocarbazole compounds as well as preparation method and application of indolocarbazole
  • Indolocarbazole compounds as well as preparation method and application of indolocarbazole

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Experimental program
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Embodiment 1

[0035] 1. Fermentation of compounds

[0036] The marine actinomycete adopts the streptomyces Streptomycessp.CICC 11027 sold by China Common Microorganism Culture Collection and Management Center;

[0037] 1) Inoculate marine actinomycetes into 500mL Erlenmeyer flasks, each bottle contains 250mL Gaoshi No. 1 liquid medium, and cultivate them in a shaker at 28°C and 180rpm for 3 days to obtain seed liquid that can be used for fermentation culture ;

[0038] 2) Inoculate the seed liquid obtained in step 1) into rice medium (rice medium, made of the following components: 40 g of rice mass; 60 mL of seawater, obtained by high-pressure damp heat sterilization after being placed in a 500 ml Erlenmeyer flask), and inoculated The volume is 12 mL, and it is cultured statically at 28° C. for 120 days to obtain a solid fermentation product containing the compound with antitumor activity of the present invention.

[0039] 2. Preparation of compounds

[0040] The solid fermentation produ...

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Abstract

The invention discloses an indolocarbazole compounds as well as a preparation method and application of indolocarbazole. The compound is of a structure shown in a formula I, a formula II and formula III as shown in the description. The compound provided by the invention can be used for treating acute leukemia, chronic leukemia, lymphoma, breast cancer, lung cancer, stomach cancer and other cancers related to inhibition of protein kinase, and can be applied to a drug for treating diseases such as Aids, coronary heart disease, diabetes mellitus and senile dementia. The invention also discloses a preparation method of a compound for resisting tumors, the compound for resisting tumors is prepared by fermenting with a marine-derived actinomycetes rice solid culture medium, and separating and purifying a yeast obtained after extraction of ethyl acetate by adopting gel column chromatography and high performance liquid chromatography, and the operation is easy to operate and implement.

Description

technical field [0001] The invention relates to the technical field of marine actinomycete culture and preparation of compounds, in particular to three indolecarbazole compounds, their preparation methods and their application in the preparation of drugs with antitumor activity. Background technique [0002] Indolecarbazoles are a class of alkaloids derived from microbial fermentation broths. The first isolated natural indolecarbazoles were alkaloids isolated from the culture broth of Streptomyces AM-2282 in 1986. Staurosporine (STA), the study found that the compound has antibacterial, antihypertensive, antitumor and strong protein kinase (PKC) inhibitory activity (IC 50 = 2.7 nM). Protein kinase C is a group of phospholipid-dependent Ca 2+ Activated protein serine M / threonine kinase is an important component of cell growth factor signaling and plays an important role in tumor growth. Therefore, targeting protein kinase-associated cancers may serve as an effective target...

Claims

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Application Information

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IPC IPC(8): C07H19/23C07H9/06C07D487/14C07H1/06C12P17/18C12P19/26A61P35/00A61P35/02C12R1/465
CPCC07D487/14C07H1/06C07H9/06C07H19/23C12P17/182C12P19/26
Inventor 马忠俊秦乐乐丁婉婧王佳楠陈喆刘美星
Owner 浙江美新控股有限公司
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