Department of Pathology and Internal Medicine, School of Medicine, Barbara Ann Karmanos Cancer Institute, Wayne State University, Detroit, Michigan 48201, USA.
Nutr Cancer. 2010;62(7):938-46. doi: 10.1080/01635581.2010.509832.
Thymoquinone (TQ) is the predominant bioactive constituent present in black seed oil (Nigella sativa) and has been tested for its efficacy against cancer. Here, we summarize the literature about TQ's molecular mechanism of action and its ability to induce apoptosis and inhibit tumor growth in preclinical models. TQ has anti-inflammatory effects, and it inhibits tumor cell proliferation through modulation of apoptosis signaling, inhibition of angiogenesis, and cell cycle arrest. Chemosensitization by TQ is mostly limited to in vitro studies, and it has potential in therapeutic strategy for cancer. The results favor efficacy and enhancement of therapeutic benefit against tumor cells resistant to therapy based on cellular targets that are molecular determinants for cancer cell survival and progression. There have been attempts to synthesize novel analogs of TQ directed toward superior effects in killing tumor cells with more enhanced chemosensitizing potential than parent TQ compound. Based on published reports, we believe that further in-depth studies are warranted including investigation of its bioavailability and Phase I toxicity profiling in human subjects. The results from such studies will be instrumental in advancing this field in support of initiating clinical trials for testing the effects of this ancient agent in cancer therapy.
百里醌(TQ)是黑种草籽油(Nigella sativa)中主要的生物活性成分,已对其抗癌功效进行了测试。在这里,我们总结了关于 TQ 的作用机制及其在临床前模型中诱导细胞凋亡和抑制肿瘤生长的能力的文献。TQ 具有抗炎作用,通过调节细胞凋亡信号、抑制血管生成和细胞周期停滞来抑制肿瘤细胞增殖。TQ 的化学增敏作用主要限于体外研究,并且在癌症治疗策略中有一定的潜力。结果支持基于对肿瘤细胞存活和进展的分子决定因素的细胞靶点,对治疗抵抗的肿瘤细胞的疗效和治疗益处的增强。已经有尝试合成 TQ 的新型类似物,旨在通过更增强的化学增敏潜力来杀死肿瘤细胞,比母体 TQ 化合物具有更好的效果。基于已发表的报告,我们认为需要进一步进行深入的研究,包括对其生物利用度和人体 I 期毒性特征进行研究。这些研究的结果将有助于推动该领域的发展,支持启动临床试验,以测试这种古老药物在癌症治疗中的作用。