Biological Evaluation of an Antibiotic DC-81-Indole Conjugate Agent in Human Melanoma Cell Lines

抗生素DC-81和lndole Moiety結合成的混成試劑對黑色素腫瘤細胞活性之研究

胡婉萍(Wan-Ping Hu) ； 余幸司(Hsin-Su Yu) ； 陳彥吉(Yen-Chi Chen) ； 王志鉦(Jeh-Jeng Wang)

《The Kaohsiung Journal of Medical Sciences》 19卷1期 (2003/01) Pp. 6-12

https://doi.org/10.6452/KJMS.200301.0006

摘要

由於比咯苯偶氮駢(PBDs)具有辦識DNA鹼基對序列，可與特定DNA序列形成共價結合，因此PBDs對核酸的合成，是一種有效的抑制劑。DC-81是PBDs的一族，由鏈黴菌所分離出來的抗癌抗生素。我們已設計合成出以DC-81(1)為主體和indole carboxylate(IC)2結合成的混成試劑3，此設計是考慮混成試劑3，可增加DNA序列選擇性。本論文就混成試劑3對黑色素腫瘤細胞的活性作一研究，經由細胞毒殺試劑XTT測試，結果發現混成試劑3對黑色素腫瘤細胞具有較強的細胞毒性。

關鍵字

比咯苯偶氮駢 ； indole carboxylate ； 黑色素腫瘤 ； XTT測試

並列摘要

Pyrrolo[2, 1-c][1, 4]benzodiazepines (PBDs) are potent inhibitors of nucleic acid synthesis because of their ability to recognize and bind to specific sequences of DNA and form a labile covalent adduct. DC-SI, an antitumor antibiotic produced by Streptomyces species, is a PBD. We combined DC-81 and an indole carboxylate moiety to synthesize a hybrid designed to have much higher sequence selectivity in DNA interactivity. In this paper, the cytotoxic potency of the hybrid in human melanoma cell lines was studied. XTI assay demonstrated that the DC-81-indole conjugate possessed cytotoxicity against human melanoma cell lines.

並列關鍵字

pyrrolo[2, 1-c][1, 4]benzodiazepines ； PBDs ； DC-81, indole carboxylate moiety ； melanoma ； XTT assay