二甲基塞来昔布抗肿瘤作用的研究进展

Advances in anti-tumor effects of 2,5-dimethyl-celecoxib(DMC)

近年来,国内外大量文献报道,传统的非甾体抗炎药物塞来昔布可以通过COX-2依赖或非依赖机制在多种恶性肿瘤中发挥抗肿瘤作用。但是,塞来昔布通过抑制COX-2可以减少血管中前列环素的产生,从而导致血栓形成事件。而2,5-二甲基塞来昔布(DMC)作为塞来昔布的紧密衍生物,尽管缺乏COX-2抑制功能,显示出比塞来昔布高20%~50%的肿瘤抑制活性,并且可能避免心血管毒性,因此,可能更适合用于恶性肿瘤的治疗。其可以通过诱导内质网应激、抑制增殖、诱导细胞凋亡、影响细胞周期、抗血管生成以及增加药物敏感性等机制发挥肿瘤抑制活性。本文对二甲基塞来昔布抗肿瘤作用的研究进展进行了详尽综述,为相关研究提供参考。

In recent years,a large number of literatures at home and abroad have reported that the traditional non-steroidal anti-inflammatory drug celecoxib can exert anti-tumor effects in various malignant tumors through COX-2 dependent or non-dependent mechanisms.However,celecoxib can reduce the production of prostacyclin in blood vessels by inhibiting COX-2,leading to thrombotic events.2,5-Dimethyl celecoxib(DMC),as a compact derivative of celecoxib,showed 20%~50%higher tumor suppressive activity than celecoxib despite the lack of COX-2 inhibitory function,and may avoid cardiovascular toxicity.Therefore,it may be more suitable for the treatment of malignant tumors.It can exert tumor suppressive activity by inducing endoplasmic reticulum stress,inhibiting proliferation,inducing apoptosis,affecting cell cycle,anti-angiogenesis,and increasing drug sensitivity.In this paper,the research progress of anti-tumor effect of dimethyl celecoxib is reviewed in detail,which provides reference for related research.