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Indolocarbazole alkaloids as well as preparation method and application thereof

A technology of indolecarbazole and alkaloids, which is applied in the field of preparation of active compounds from secondary metabolites of actinomycetes, can solve problems such as poor selectivity, and achieve the effects of simple operation, easy cultivation, and easy expansion of production

Active Publication Date: 2018-05-29
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these compounds have poor selectivity and have inhibitory effects on cancer cells and normal somatic cells

Method used

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  • Indolocarbazole alkaloids as well as preparation method and application thereof
  • Indolocarbazole alkaloids as well as preparation method and application thereof
  • Indolocarbazole alkaloids as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1. the fermentation of actinomycetes

[0035] The actinomycete adopts the streptomyces Streptomycessp.CICC 11031 sold by China Common Microorganism Culture Collection and Management Center;

[0036] 1) Inoculate the actinomycetes in Gao's No. 1 medium, culture at 28°C, and culture on a shaker at 180rpm for 4-6 days to obtain seed liquid;

[0037] 2) Inoculate the seed solution obtained in step 1) into rice culture medium (rice culture medium, made of the following components: 40 g of rice mass; 60 mL of seawater salt water, obtained by high-pressure damp heat sterilization after being placed in a 500 mL Erlenmeyer flask), The inoculum size of each bottle is 10 mL, and the culture is statically cultured at 28° C. for 70 days. The culture is soaked in ethyl acetate, extracted and concentrated to obtain a fermented crude extract containing the compound of the present invention.

Embodiment 2

[0038] Embodiment 2. The preparation of compound

[0039] The obtained fermented crude extract is subjected to gel column chromatography (the filler is hydroxypropyl sephadex LH-20), and the eluent is methanol- In the water system, each 1 / 4 column volume is a fraction, and the fractions containing the target compound are combined for TLC analysis. Medium-pressure preparative chromatographic separation (Sepax Amethyst C-18 (10μm, 30×400mm) chromatographic column, detection wavelength 291nm, filler is octadecylsilane bonded silica gel), mobile phase is 40%-100% by volume methanol+ Gradient elution with 0.05% TFA-water solution, TLC analysis The part containing staurosporine and the part not containing staurosporine were combined respectively, and the new compound was located in the part not containing staurosporine. The staurosporine-free fraction was subjected to silica gel column chromatography (300-400 mesh), and the eluent was a methanol-dichloromethane system (methanol:dic...

Embodiment 3

[0041] Example 3. Identification of Compounds

[0042] The compound of the present invention is light yellow powder, high-resolution mass spectrometry HR-ESI-MS gives quasi-molecular ion peak m / z497.1819[M+H] + (calculated 497.1825), suggesting that the molecular formula is C 28 h 24 N 4 o 5 , named actinocarbazole B, the specific structural analysis results are shown in Table 1 below:

[0043] Table 1

[0044]

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Abstract

The invention discloses indolocarbazole alkaloids as well as a preparation method and an application thereof. The structural formula of the indolocarbazole alkaloids is shown in the following formula(I) in the description. The indolocarbazole alkaloids are produced from actinomycetes through fermentation in a rice solid culture medium, a fermentation product obtained after extraction with ethyl acetate is separated and purified with gel column chromatography, medium pressure liquid chromatography, silica gel column chromatography and high performance liquid chromatography. The indolocarbazolealkaloids can be used for preparing medicines for treating cancers such as acute and chronic leukemia, lymphoma, breast cancer, lung cancer and the like as well as diseases such as Aids, coronary heart disease, diabetes, senile dementia and the like associated with inhibition of protein kinases, tyrosine kinases and the like.

Description

technical field [0001] The invention relates to the field of preparing active compounds from secondary metabolites of actinomycetes, in particular to an indolecarbazole alkaloid and its preparation method and application. Background technique [0002] Indolecarbazoles, a class of bisindole alkaloid natural products derived from L-tryptophan, have attracted extensive attention due to their unique structural features and potential clinical applications. Indolecarbazole alkaloids (such as staurosporine, rebeccamycin, K252a, etc.) have a wide range of biological activities, such as anti-tumor, anti-hypertensive, anti-bacterial, anti-fungal, anti-malarial, anti-tuberculosis, neuroprotective, anti-platelet aggregation, etc. Its mechanism of action mainly includes inhibition of protein kinases, tyrosine kinases, DNA topoisomerases, immunosuppression, and DNA intercalation. [0003] Many indolecarbazole alkaloids have shown good biological activity and have entered clinical researc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D498/22A61K31/553A61P35/00A61P35/02A61P31/18A61P9/10A61P3/10A61P25/28C12P17/18C12R1/465
Inventor 马忠俊王金慧丁婉婧
Owner ZHEJIANG UNIV
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