Medical application of berberine derivative

A berberine and drug technology, which is applied in the field of berberine derivatives, can solve the problems of unseen glioma migration and invasion, and unsatisfactory drug efficacy.

Active Publication Date: 2014-12-17
SUN YAT SEN UNIV
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Problems solved by technology

Studies have shown that berberine can inhibit the migration and invasion of liver cancer, human tongue squamous cell carcinoma, melanoma, breast cancer, bladder cancer, etc., but th

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  • Medical application of berberine derivative
  • Medical application of berberine derivative
  • Medical application of berberine derivative

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Experimental program
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Embodiment Construction

[0030] Synthesis and Identification of Berberine Derivatives

[0031]Berberine hydrochloride was purchased from Xi’an Xiaocao Plant Technology Co., Ltd., with a purity of 97%; bromododecane, bromohexadecane, bromooctadecane, and benzyl bromide were all analytically pure, purchased from Aladdin Reagent Co., Ltd. Company; N, N-dimethylformamide (DMF) is analytically pure, dried with molecular sieves, and purchased from Tianjin Fuyu Fine Chemical Co., Ltd.; neutral alumina for chromatography is a product of Sinopharm Group; DMEM medium (R10 -013-cv), fetal bovine serum (FBS), trypsin, penicillin and streptomycin were all purchased from Cellgro, USA; tetramethylazozolium salt (MTT) and dimethyl sulfoxide (DMSO) were purchased from Sigma Company of the United States; 4% paraformaldehyde was purchased from Guangzhou Jingxin Technology Co., Ltd.; the experimental water was ultrapure water. Rat glioma C6 cells and human glioma U87 cells were from the ATCC cell bank in the United St...

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Abstract

The invention provides application of a compound shown in the formula (I) or a salt thereof in the aspects of preparing of medicines for treating malignant glioma or a mitochondrial targeting drug delivery system, and in the formula (I), R is C10-C18 alkyl, or R is benzyl. The experiments find that compared with a control, a berberine derivative not only can more effectively inhibit glioma cell proliferation, and can also effectively inhibit the migration and invasion ability of cells. In addition, the compounds can be well positioned to mitochondria, so that the compounds can be used as the mitochondrial targeting drug delivery system.

Description

technical field [0001] The present invention relates to the new application of berberine derivatives, especially the new application of C9-O substituted long-chain alkyl or benzyl derivatives in treating malignant glioma. Background technique [0002] Malignant glioma (Malignant Glioma) is the most common primary malignant tumor in the central nervous system, accounting for 46% of intracranial tumors. Surgery is the preferred treatment method, but because of its invasive growth and no obvious boundary with normal brain tissue, surgery is difficult to remove, and the postoperative recurrence rate is as high as 96%. Even with supplementary radiotherapy and chemotherapy, the average postoperative survival period is no more than 14 months, and the prognosis is extremely poor. The incurability of malignant glioma is closely related to its strong ability of migration and invasion. Therefore, inhibiting the migration and invasion of glioma cells is extremely critical for the trea...

Claims

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Application Information

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IPC IPC(8): A61K31/4375A61P35/00
Inventor 胡海燕付胜楠庹珏谢彦奇张国光王亚龙朱文博颜光美
Owner SUN YAT SEN UNIV
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