Institute of Biochemistry, Food Science, and Nutrition, The Robert H. Smith Faculty of Agriculture, Food, and Environment, The Hebrew University of Jerusalem, Rehovot, Israel.
Nutr Cancer. 2010;62(7):947-57. doi: 10.1080/01635581.2010.509837.
Allicin (diallyl thiosulfinate) is the best-known biologically active component in freshly crushed garlic extract. We developed a novel, simple method to isolate active allicin, which yielded a stable compound in aqueous solution amenable for use in in vitro and in vivo studies. We focused on the in vitro effects of allicin on cell proliferation of colon cancer cell lines HCT-116, LS174T, HT-29, and Caco-2 and assessed the underlying mechanisms. This allicin preparation exerted a time- and dose-dependent cytostatic effect on these cells at concentrations ranging from 6.2 to 310 μM. Treatment with allicin resulted in HCT-116 apoptotic cell death as demonstrated by enhanced hypodiploid DNA content, decreased levels of B-cell non-Hodgkin lymphoma-2 (Bcl-2), increased levels of bax and increased capability of releasing cytochrome c from mitochondria to the cytosol. Allicin also induced translocation of NF-E2-related factor-2 (Nrf2) to the nuclei of HCT-116 cells. Luciferase reporter gene assay showed that allicin induces Nrf2-mediated luciferase transactivation activity. SiRNA knock down of Nrf2 significantly affected the capacity of allicin to inhibit HCT-116 proliferation. These results suggest that Nrf2 mediates the allicin-induced apoptotic death of colon cancer cells.
大蒜素（二烯丙基硫代亚磺酸酯）是新鲜压碎的大蒜提取物中最知名的生物活性成分。我们开发了一种新颖、简单的方法来分离活性大蒜素，得到一种在水溶液中稳定的化合物，适用于体外和体内研究。我们专注于大蒜素对结肠癌细胞系 HCT-116、LS174T、HT-29 和 Caco-2 细胞增殖的体外影响，并评估了其潜在机制。这种大蒜素制剂在浓度为 6.2 至 310 μM 范围内对这些细胞表现出时间和剂量依赖性的细胞生长抑制作用。大蒜素处理导致 HCT-116 细胞凋亡性细胞死亡，表现为低二倍体 DNA 含量增加、B 细胞非霍奇金淋巴瘤-2（Bcl-2）水平降低、Bax 水平升高以及线粒体细胞色素 c 向细胞质释放的能力增强。大蒜素还诱导 NF-E2 相关因子-2（Nrf2）向 HCT-116 细胞核内易位。荧光素酶报告基因检测表明，大蒜素诱导 Nrf2 介导的荧光素酶转录激活活性。Nrf2 的 siRNA 敲低显著影响大蒜素抑制 HCT-116 增殖的能力。这些结果表明，Nrf2 介导大蒜素诱导的结肠癌细胞凋亡性死亡。
