Steroid compound as well as preparation method and application thereof

A technology of compounds and steroids, applied in the application of antineoplastic drugs, in the field of preparation of steroids, can solve problems such as adverse reactions, inability to completely kill tumor cells, and influence on pharmacokinetic properties

Pending Publication Date: 2021-08-31
HAINAN NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinical practice also shows that single-target tyrosine kinase inhibitor antineoplastic drugs, such as erlotinib and gefitinib, although they have strong selectivity and low toxicity and side effects, are prone to drug resistance during use. Tumor cells cannot be completely killed, and the combined drug will bring serious adverse reactions and affect their respective pharmacokinetic properties

Method used

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  • Steroid compound as well as preparation method and application thereof
  • Steroid compound as well as preparation method and application thereof
  • Steroid compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment one: the preparation method of compound artoheterophoid

[0022] A. The sun-dried jackfruit fruit powder (22.9kg, Hainan) is extracted by cold soaking with 85% ethanol solution for 5 times, each extraction for three days, filtering, collecting the filtrate, concentrating under reduced pressure to no alcohol, and obtaining the alcohol extract;

[0023] B. The alcohol extract was added with distilled water to make a suspension, extracted successively with petroleum ether and ethyl acetate, and the petroleum ether extract was concentrated under reduced pressure to obtain 827.8 g of petroleum ether extract and 983.3 g of ethyl acetate extract; ;

[0024] C. Purify the petroleum ether extract by column chromatography:

[0025] (1) Cut off the petroleum ether extract extract by silica gel column chromatography, and use petroleum ether-ethyl acetate (volume ratios of 95:5, 85:15, 75:25, 55:45) as the eluent for gradient Elution, collecting petroleum ether-ethyl ac...

Embodiment 2

[0031] Embodiment two: the preparation method of compound artoheterophoid

[0032] A. The dry powder (108.5kg, Hainan) of dried Jackfruit pulp is extracted by cold immersion in methanol 5 times, each time for 5 days, filtered, the filtrate is collected, and concentrated under reduced pressure until it has no alcohol smell to obtain a methanol extract;

[0033] B. The methanol extract was added with distilled water to make a suspension, extracted successively with petroleum ether and ethyl acetate, and the petroleum ether extract was concentrated under reduced pressure to obtain 4258.7 g of petroleum ether extract and 5023.5 g of ethyl acetate extract;

[0034] C. Purify the petroleum ether extract by column chromatography:

[0035] (1) Use silica gel column chromatography to separate the extract from petroleum ether, and use petroleum ether-ethyl acetate (volume ratio 95:5, 85:15, 75:25 and 55:45) as the eluent for gradient elution , collecting sherwood oil-ethyl acetate (vol...

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Abstract

The invention relates to the field of natural medicines, and discloses a steroidal compound which is derived from artocarpus heterophyllus pulp and has a novel chemical structure, a preparation method of the steroidal compound and application of the steroidal compound in antitumor medicines. Various in-vitro antitumor activity evaluation results of the compound artoheterophoid show that the compound has remarkable antitumor activity, presents protein tyrosine kinase inhibition activity equivalent to the tyrosine kinase inhibition activity of a positive control drug, can be further developed into an anti-tumor drug taking protein tyrosine kinase as a target, can be applied to the anti-tumor drug, is simple in separation and purification process and mild in reaction conditions, and has practical significance.

Description

technical field [0001] The invention belongs to the field of natural medicines, and in particular relates to a preparation method of a steroid compound with a novel chemical structure derived from jackfruit pulp and its application in antitumor drugs. Background technique [0002] Malignant tumors have become the largest cause of death in humans, and the morbidity and mortality of malignant tumors continue to rise worldwide. With the continuous elucidation of the mechanism of tumorigenesis and the discovery of anti-tumor targets, targeted inhibition of tumor signal transduction has become an important direction for the development of new anti-tumor drugs. Among various molecular targets, protein tyrosine kinase (PTK) is currently one of the most studied and most effective anti-tumor drug targets, and has become the research focus and hotspot of anti-tumor targeted therapy drugs ,with broadly application foreground. The small molecule targeted antineoplastic drugs currently...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J1/00A61P35/00
CPCA61P35/00C07J1/00C07J1/0007
Inventor 刘艳萍付艳辉蒋波谢澜吴英菊
Owner HAINAN NORMAL UNIV
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