International Centre for Genetic Engineering and Biotechnology, Werner and Beit Building South, UCT Campus, Observatory, South Africa, 7925.
Biofactors. 2010 Jan-Feb;36(1):78-85. doi: 10.1002/biof.76.
Garlic has been used throughout the centuries to treat infections, heart disease, and cancer. Ajoene is one of the main compounds formed from heating crushed garlic as a mixture of E- and Z-isomers (E- and Z-4,5,9-trithiadodeca-1,6,11-triene 9-oxide). Ajoene possesses a broad spectrum of biological activities that include anticancer activity. It's cytotoxicity towards cancer cells is postulated to occur via an apoptotic mechanism involving activation of the mitochondrial-dependent caspase cascade. Structure-activity studies on ajoene and ajoene analogues have revealed that the Z-isomer is moderately more active than the E-isomer at inhibiting in vitro tumor cell growth, suggesting that specific protein interactions may be important. Substitution of the terminal end allyl groups in ajoene for alkyl, aromatic, or heteroaromatic groups produces some analogs with superior in vitro anticancer activity to ajoene, opening up the way to developing ajoene-based anticancer agents.
大蒜在几个世纪以来一直被用于治疗感染、心脏病和癌症。阿霍烯是加热粉碎的大蒜形成的主要化合物之一，它是 E-和 Z-异构体（E-和 Z-4,5,9-三硫杂十二-1,6,11-三烯 9-氧化物）的混合物。阿霍烯具有广泛的生物学活性，包括抗癌活性。它对癌细胞的细胞毒性被假设通过涉及线粒体依赖性半胱天冬酶级联激活的凋亡机制发生。对阿霍烯及其类似物的结构活性研究表明，Z-异构体在抑制体外肿瘤细胞生长方面比 E-异构体具有适度的活性，这表明特定的蛋白质相互作用可能很重要。用烷基、芳基或杂芳基取代阿霍烯末端的烯丙基基团，可产生一些比阿霍烯具有更好体外抗癌活性的类似物，为开发基于阿霍烯的抗癌剂开辟了道路。
