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首页> 外文期刊>BioFactors >Garlic-derived anticancer agents: Structure and biological activity of ajoene
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Garlic-derived anticancer agents: Structure and biological activity of ajoene

机译：大蒜来源的抗癌药：阿霍烯的结构和生物学活性

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摘要

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-trithiadodeca1,641-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.
机译：整个世纪以来，大蒜一直用于治疗感染，心脏病和癌症。 Ajoene是通过加热压碎的大蒜作为E-和Z-异构体（E-和Z-4,5,9-trithiadodeca1,641-triene 9-oxide）的混合物而形成的主要化合物之一。阿霍烯具有广泛的生物活性，包括抗癌活性。据推测，它对癌细胞的细胞毒性是通过凋亡机制发生的，该机制涉及线粒体依赖性胱天蛋白酶级联反应的激活。对阿霍烯和阿霍烯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-异构体活性中等，这表明特定的蛋白质相互作用可能很重要。用亚芳烃中的末端烯丙基取代烷基，芳族或杂芳族基团可产生一些具有比亚芳烯更好的体外抗癌活性的类似物，从而为开发基于亚烯基的抗癌剂开辟了道路。

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