Gao Shanghui, Yang Kai, Nohara Toshihiro, Ikeda Tsuyoshi, Zhou Jian-Rong, Yokomizo Kazumi, Fang Jun
Faculty of Pharmaceutical Sciences, Sojo University, Kumamoto 860-0082, Japan.
Department of Medical Technology, Anhui Medical College, No. 632, Furong Road, Hefei 230601, China.
Antioxidants (Basel). 2023 Apr 3;12(4):869. doi: 10.3390/antiox12040869.
This study aimed to investigate the pharmacological activities of garlicnin B1, a cyclic sulfide compound found abundantly in garlic and structurally similar to onionin A1, which has been shown to possess strong anti-tumor effects. In vitro studies demonstrated that garlicnin B1 significantly reduced intracellular reactive oxygen species triggered by hydrogen peroxide in colon cancer cells. In a mouse colitis model induced by dextran sulfate sodium, garlicnin B1 at a low dose (5 mg/kg) remarkably ameliorated the symptoms and pathological progression. Additionally, garlicnin B1 exhibited considerable tumoricidal activity with an IC50 value of ~20 μM, as observed in cytotoxicity assays. In vivo experiments using the mouse sarcoma S180 transplanted model and the azoxymethane (AOM) or DSS-induced colon cancer model showed that garlicnin B1 effectively suppressed tumor growth in a dose-dependent manner, with marked inhibition at 80 mg/kg. These results suggest that garlicnin B1 has diverse functions that could be achieved by carefully manipulating the dosing regimen. We anticipate that garlicnin B1 has the potential to be used beneficially in the future for the treatment of cancer and inflammatory diseases, although further studies are warranted to elucidate its mechanisms of action.
本研究旨在探究大蒜素B1的药理活性，大蒜素B1是一种在大蒜中大量存在的环状硫化物化合物，其结构与已被证明具有强大抗肿瘤作用的洋葱素A1相似。体外研究表明，大蒜素B1能显著降低结肠癌细胞中由过氧化氢引发的细胞内活性氧水平。在葡聚糖硫酸钠诱导的小鼠结肠炎模型中，低剂量（5毫克/千克）的大蒜素B1能显著改善症状和病理进展。此外，如细胞毒性试验所示，大蒜素B1表现出相当可观的杀肿瘤活性，其IC50值约为20微摩尔。使用小鼠肉瘤S180移植模型以及氧化偶氮甲烷（AOM）或葡聚糖硫酸钠（DSS）诱导的结肠癌模型进行的体内实验表明，大蒜素B1能以剂量依赖性方式有效抑制肿瘤生长，在80毫克/千克时具有显著抑制作用。这些结果表明，通过仔细调整给药方案，大蒜素B1可发挥多种功能。我们预计，大蒜素B1未来有可能用于癌症和炎症性疾病的有益治疗，不过仍需进一步研究以阐明其作用机制。
