选择性环氧合酶—2抑制剂塞来昔布抗肿瘤作用机制的研究进展
2017-06-01郝兴刘建生陈博艺张宝明
郝兴 刘建生 陈博艺 张宝明
[摘要] 近年来,国内外大量研究表明环氧合酶-2(COX-2)在许多肿瘤如肺癌、乳腺癌、消化道恶性肿瘤、前列腺癌等中高表达,其与肿瘤发生、发展和转移有密切联系。抑制肿瘤COX-2的表达具有抗肿瘤作用。塞来昔布(Celecoxib)是一种选择性COX-2的抑制剂,目前发现其对多种肿瘤具有抗肿瘤作用,但其抗肿瘤机制尚不完全明确。本文对近年来塞来昔布抗肿瘤机制的研究进行综述。
[关键词] COX-2;塞来昔布;凋亡;转移
[中图分类号] R730.5 [文献标识码] A [文章编号] 1673-9701(2016)34-0157-04
Reviews the recent progress in anti-tumor mechanism of selective COX-2 inhibitors celecoxib
HAO Xing1 LIU Jiansheng2 CHEN Boyi1 ZHANG Baoming1
1.Shanxi Medical University, Taiyuan 030000, China;2.Department of Genenal Surgery, the First Hospital of Shanxi Medical University,Taiyuan 030000, China
[Abstract] In recent years, many domestic and international research shows that COX-2 is over-expressed in various tumor cells, such as lung cancer, breast cancer, malignant tumor of digestive tract, prostatic cancer, etc. It is closely related to the occurrence, development and metastasis of tumors. By inhibiting the expression of COX-2 in the tumor cells have anti-tumor effect. Celecoxib is one of the selectively COX-2 inhibitors, some studies showed that celecoxib can resist many kinds of tumor cells, but the action mechanism of anti-tumor remains unclear. In this paper, recent reports about anti-tumor mechanism of celecoxib are reviewed.
[Key words] COX-2; Celecoxib; Apoptosis; Metastasis
目前為止,国内外大量流行病学、临床试验及研究发现环氧合酶(cyclooxygenase,COX)与多种肿瘤的发生发展有着密切联系。塞来昔布(Celecoxib)作为一种新型的非甾体类抗炎药,是一种高选择性COX-2抑制剂,已经在多种肿瘤的防治中发挥作用,其抗肿瘤作用机制成为近年来研究热点[1,2]。本文将塞来昔布的抗肿瘤作用进行综述。
1 COX-2的生物学性质
环氧合酶(cyclooxygenase,COX)是催化花生四烯酸转变为前列腺素(prostaglandins,PGs)过程中的关键酶,是膜结合蛋白酶,存在于核膜和微粒体膜中[3]。目前发现有COX-1和COX-2两种同工酶。COX-1是结构型酶,主要存在于正常的组织细胞中,参与血管舒缩、血小板聚集、胃黏膜血流、胃黏液分泌及肾功能等的调节,维持机体正常的生理功能,如保护胃肠黏膜,抑制血小板聚集和调节肾血流分布。COX-2是诱导型酶,主要存在于细胞浆内及细胞核周。正常生理情况下,绝大多数组织细胞不表达COX-2,只有当细胞受到刺激后才能迅速诱导表达,参与多种疾病发生发展的病理过程[4]。……
