Department of Pharmacology, Faculty of Medicine, University of Malaya, Kuala Lumpur 50603, Malaysia.
Molecules. 2019 Jul 10;24(14):2522. doi: 10.3390/molecules24142522.
Colon cancer is the third most common type of cancer in the world. Diosmetin (Dis), a natural -methylated flavone, has been reported to have anti-cancer effects against different types of cancer. Although the mechanisms of action of Dis against several cancer cell lines are well reported, in vivo anti-tumorigenesis properties of this compound are still obscure. Therefore, this study aimed to investigate the anti-tumorigenesis properties of Dis against HCT-116 colon cancer xenografts in nude mice. HCT-116 colon cancer cells were injected in NCr nu/nu nude mice and treatment with Dis was initiated after the tumor volumes reached 100 mm and continued for four weeks. On the sacrificing date nude mice treated with 100 mg/kg of Dis showed significant lower tumor volume (264 ± 238.3 mm) as compared to the untreated group (1428.8 ± 459.6 mm). Anti-apoptotic Bcl-2 protein was significantly downregulated, while apoptotic protein (Bax) was significantly overexpressed in nude mice treated with 100 mg/kg Dis as compared to untreated mice. In conclusion, our in vivo results indicate that Dis significantly reduces tumor growth rate of HCT-116 colon cancer cells in nude mice at a dose of 100 mg/kg, and has no toxic effects in ICR mice up to 2000 mg/kg.
结直肠癌是世界上第三常见的癌症类型。山奈素（Dis），一种天然的 -甲基化黄酮类化合物，已被报道具有抗多种癌症的作用。尽管 Dis 对几种癌细胞系的作用机制已有详细报道，但该化合物在体内的抗肿瘤特性仍不清楚。因此，本研究旨在探讨 Dis 对裸鼠 HCT-116 结肠癌异种移植瘤的抗肿瘤作用。将 HCT-116 结肠癌细胞注入 NCr nu/nu 裸鼠中，在肿瘤体积达到 100mm 后开始用 Dis 治疗，并持续四周。在处死日期，用 100mg/kg Dis 治疗的裸鼠的肿瘤体积明显低于未治疗组（264±238.3mm）（1428.8±459.6mm）。用 100mg/kg Dis 治疗的裸鼠中抗凋亡蛋白 Bcl-2 显著下调，而凋亡蛋白（Bax）显著过表达。结论：本研究结果表明，Dis 在 100mg/kg 剂量下可显著降低裸鼠 HCT-116 结肠癌细胞的肿瘤生长速度，在 2000mg/kg 剂量下对 ICR 小鼠无毒性作用。
