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1,2-二(喹唑啉-4-基)二硒醚对SiHa宫颈癌细胞的体外疗效的初步评估

Preliminary evaluation of the in vitro efficacy of 1, 2-di (quinazolin-4-yl) diselane against SiHa cervical cancer cells.

作者信息

Huang Yin-Jiu, Zhang Yu-Yuan, Liu Gang, Tang Jie, Hu Jian-Guo, Feng Zhen-Zhong, Liu Fang, Wang Qi-Yi, Li Dan

机构信息

Department of Bioscience, Bengbu Medical College, Bengbu, China E-mail :

出版信息

Asian Pac J Cancer Prev. 2014;15(15):6301-6. doi: 10.7314/apjcp.2014.15.15.6301.

Abstract

Cervical cancer is one the most common malignancies among females. In recent years, its incidence rate has shown a rising trend in some countries so that development of anticancer drugs for cervical cancer is an urgent priority. In our recent anticancer drug discovery screen, 1, 2-di (quinazolin-4-yl)diselane (LG003) was found to possess wide spectrum anticancer efficacy. In the present work, the in vitro anticancer activity of LG003 was evaluated in the SiHa cervical cancer cell line. Compared with commercial anticancer drugs 10-hydroxycamptothecin, epirubicin hydrochloride, taxol and oxaliplatin, LG003 showed better anticancer activity. Furthermore, inhibition effects were time- and dose-dependent. Morphological observation exhibited LG003 treatment results in apoptosis like shrinking and blebbing, and cell membrane damage. Lactate dehydrogenase release assay revealed that LG003 exerts such effects in SiHa cells through a physiology pathway rather than cytotoxicity, which suggests that title compound LG003 can be a potential candidate agent for cervical cancer.

摘要

宫颈癌是女性中最常见的恶性肿瘤之一。近年来,在一些国家其发病率呈上升趋势,因此开发治疗宫颈癌的抗癌药物成为当务之急。在我们最近的抗癌药物发现筛选中,1,2-二(喹唑啉-4-基)二硒烷(LG003)被发现具有广谱抗癌功效。在本研究中,在SiHa宫颈癌细胞系中评估了LG003的体外抗癌活性。与市售抗癌药物10-羟基喜树碱、表柔比星盐酸盐、紫杉醇和奥沙利铂相比,LG003表现出更好的抗癌活性。此外,抑制作用具有时间和剂量依赖性。形态学观察显示,LG003处理导致细胞凋亡,如细胞收缩、出泡和细胞膜损伤。乳酸脱氢酶释放试验表明,LG003通过生理途径而非细胞毒性在SiHa细胞中发挥这些作用,这表明标题化合物LG003可能是宫颈癌的潜在候选药物。

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