大蒜辣素是大蒜的主要生物活性成分,由其非活性前体蒜氨酸与蒜酶相互作用而产生.在此项研究中,我们观测大蒜辣素对人鼻咽癌细胞的增殖抑制作用与药理机制.研究结果表明,大蒜辣素可明显抑制KB细胞的增殖,具有浓度依赖性,作用48 h的IC50值为(2.2±0.2)μg/mL.而且,大蒜辣素可诱导KB细胞凋亡,作用48 h时诱导凋亡作用在(16～48)μg/mL范围内具有浓度依赖性.大蒜辣素的凋亡诱导作用通过其诱导KB细胞的细胞核凝集、细胞骨架改变以及线粒体膜电势变化得到了进一步确证.大蒜辣素还可阻滞KB细胞周期于S期,在(16～48)μg/mL范围内具有浓度依赖性.此外,大蒜辣素可浓度依赖的解聚KB细胞的微管,其作用类似于已知的微管解聚剂秋水仙碱.大蒜辣素对人鼻咽癌KB细胞的增殖抑制作用可能是通过诱导凋亡,阻滞细胞周期以及解聚微管实现的.%Allicin, a major biologically active component of garlic, is produced from its inactive precursor alliin by the enzyme alliinase. In this study, we investigated its effects on human nasopharyngeal carcinoma KB cells. After incubation for 48 h, allicin inhibited the growth of KB cells in a concentration-dependent manner with an IC50 value of (2.2±0.2) μg/mL. Incubation with allicin for 48 h caused a concentration-dependent induction of apoptosis in the concentration range of (16-48) μtg/mL, and the induction of apoptosis was confirmed by the changes of mitochondrial membrane potential, F-actin contents and nuclear conden- sation in KB cells. Moreover, allicin concentration-dependently arrested KB cells at the S-phase of the cell cycle in the range of (16-48) μg/mL. In addition, treatment with the compound caused concentration-dependent disassembly of microtubule cytoskeleton in KB cells, which is similar to the effect of colchicine, a well-known microtubule destabilizing agent. We concluded that the abilities of allicin to inhibit the proliferation of KB cells probably relate to its apoptosis induction, cell cycle arrest and microtubule destabilizing properties.
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