Kundu Juthika, Chun Kyung-Soo, Aruoma Okezie I, Kundu Joydeb Kumar
College of Pharmacy, Keimyung University, Daegu 704 701, Republic of Korea.
School of Pharmacy, American University of Health Sciences, Signal Hill, CA 90755, USA.
Mutat Res. 2014 Oct;768:22-34. doi: 10.1016/j.mrfmmm.2014.05.003. Epub 2014 May 27.
The bioactive natural products (plant secondary metabolites) are widely known to possess therapeutic value for the prevention and treatment of various chronic diseases including cancer. Thymoquinone (2-methyl-5-isopropyl-1,4-benzoquinone; TQ), a monoterpene present in black cumin seeds, exhibits pleiotropic pharmacological activities including antioxidant, anti-inflammatory, antidiabetic and antitumor effects. TQ inhibits experimental carcinogenesis in a wide range of animal models and has been shown to arrest the growth of various cancer cells in culture as well as xenograft tumors in vivo. The mechanistic basis of anticancer effects of TQ includes the inhibition of carcinogen metabolizing enzyme activity and oxidative damage of cellular macromolecules, attenuation of inflammation, induction of cell cycle arrest and apoptosis in tumor cells, blockade of tumor angiogenesis, and suppression of migration, invasion and metastasis of cancer cells. TQ shows synergistic and/or potentiating anticancer effects when combined with clinically used chemotherapeutic agents. At the molecular level, TQ targets various components of intracellular signaling pathways, particularly a variety of upstream kinases and transcription factors, which are aberrantly activated during the course of tumorigenesis.
生物活性天然产物（植物次生代谢产物）因对包括癌症在内的各种慢性疾病具有预防和治疗的治疗价值而广为人知。百里醌（2-甲基-5-异丙基-1,4-苯醌；TQ）是黑种草籽中的一种单萜，具有多种药理活性，包括抗氧化、抗炎、抗糖尿病和抗肿瘤作用。TQ在多种动物模型中抑制实验性致癌作用，并且已显示可在体外阻止各种癌细胞的生长以及体内异种移植肿瘤的生长。TQ抗癌作用的机制基础包括抑制致癌物代谢酶活性和细胞大分子的氧化损伤、减轻炎症、诱导肿瘤细胞的细胞周期停滞和凋亡、阻断肿瘤血管生成以及抑制癌细胞的迁移、侵袭和转移。当与临床使用的化疗药物联合使用时，TQ显示出协同和/或增强的抗癌作用。在分子水平上，TQ靶向细胞内信号通路的各种成分，特别是在肿瘤发生过程中异常激活的多种上游激酶和转录因子。
