Compounds with antitumor activity and their preparation methods and applications
A technology for anti-tumor activity and compounds, which is applied in the field of compounds with anti-tumor activity and their preparation, and can solve the problems of poor specific selectivity and the like
Active Publication Date: 2019-10-15
浙江美新控股有限公司
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Problems solved by technology
[0002] Since the indolecarbazole alkaloid staurosporine (STA) was isolated from Streptomyces clavicularis (ATCC55006) in 1977, it has attracted attention due to its wide range of pharmacological activities, such as: anti-tumor, anti-bacterial, anti-hypertensive, And it has a strong inhibitory effect on protein kinase C (PKC), tyrosine kinase, topoisomerase, extracellular regulatory protein kinase, etc., especially the inhibitory activity on protein kinase C (PKC) (IC 50 =2.7nM), but later studies found that STA had poor specific selectivity to normal cells and tumor cells, and could not be used as a drug, so the discovery and application of its derivatives continued to deepen
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Embodiment 1
[0035] 1. Fermentation of compounds
[0036] The marine actinomycete adopts Streptomyces sp.CICC 11027 sold by China General Microorganism Culture Collection and Management Center;
[0037] 1) Inoculate marine actinomycetes (CICC 11027) 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 a fermentable culture the seed liquid;
[0038] 2) Inoculate the seed solution obtained in step 1) into rice medium (rice medium, made of the following components: 40g of rice, 60mL of seawater, obtained by high-pressure damp heat sterilization after being placed in a 500ml Erlenmeyer flask), the inoculation volume It is 12 mL, and the culture condition is constant temperature static culture at 28°C for 120 days to obtain a solid fermentation product containing the compound with anti-tumor activity of the present invention.
[0039] 2. Preparation of compounds
[0040]The solid fermentati...
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Abstract
The invention discloses compounds with anti-tumor activity as well as a preparation method and an application of the compounds. The structures of the compounds are shown as formulae (I) and (II) in the description. The compounds can be used for preparing drugs for treating diseases such as acute leukemia and chronic leukemia associated with protein kinase inhibition, lymphoma, breast cancer, lung cancer and other cancer, acquired immune deficiency syndrome, coronary heart disease, diabetes mellitus, senile dementia and the like. The invention further provides the preparation method of the compounds with the anti-tumor activity. According to the preparation method, marine actinomycete is fermented with a rice solid medium, a fermentation product obtained after extraction with ethyl acetate is subjected to separation and purification with gel column chromatography and preparative liquid chromatography, and the method is easy to operate and implement.
Description
technical field [0001] The invention relates to the field of preparing active compounds by cultivating marine actinomycetes, in particular to a compound with antitumor activity and its preparation method and application. Background technique [0002] Since the indolecarbazole alkaloid staurosporine (STA) was isolated from Streptomyces clavicularis (ATCC55006) in 1977, it has attracted attention due to its wide range of pharmacological activities, such as: anti-tumor, anti-bacterial, anti-hypertensive, And it has a strong inhibitory effect on protein kinase C (PKC), tyrosine kinase, topoisomerase, extracellular regulatory protein kinase, etc., especially the inhibitory activity on protein kinase C (PKC) (IC 50 =2.7nM), but later studies found that STA had poor specific selectivity to normal cells and tumor cells, and could not be used as a drug, so the discovery and application of its derivatives continued to deepen. PKC is a group of phospholipid-dependent Ca 2+ Activated ...
Claims
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IPC IPC(8): C07D487/14A61K31/407A61P35/00C12P17/18C12R1/465
Inventor 马忠俊秦乐乐丁婉婧陈喆刘美星
Owner 浙江美新控股有限公司