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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48h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48h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 is the major bioactive component of garlic produced by the interaction of alliin with alliinase, an inactive precursor. In this study, we observed allicin on human nasopharyngeal carcinoma cell proliferation inhibition and pharmacological mechanisms. The results showed that allicin can significantly inhibit the proliferation of KB cells in a concentration-dependent manner, with an IC50 of (2.2 ± 0.2) μg / mL for 48 hours. Moreover, allicin can induce the apoptosis of KB cells, and the effect of inducing apoptosis at concentration of 48-48h is concentration-dependent (16-48) μg / mL. The apoptosis inducing effect of allicin can be further confirmed through its induction of nuclear agglutination, cytoskeleton changes and mitochondrial membrane potential changes in KB cells. Allicin can also block KB cell cycle in S phase, in a concentration range of (16 ~ 48) μg / mL. In addition, allicin can be a concentration-dependent depolymerization of microtubules of KB cells, which acts similarly to the known microtubule depolymerizer colchicine. The inhibitory effect of allicin on the proliferation of human nasopharyngeal carcinoma KB cells may be through inducing apoptosis, arresting cell cycle and depolymerization microtubules.