METHODS: Formulations of oral gel containing α-MG were developed. Anticancer activity on SCC-25 was assessed. Apoptotic induction was determined using flow cytometry technique. Antiviral activity against HPV-16 pseudovirus and antimicrobial activity against S. mutans, P. gingivalis and C. albicans were investigated. NO inhibition was carried out. Fibroblast cell migration was determined by in vitro scratch assay.
RESULTS: The formulation of 1% α-MG in orabase gel demonstrated anticancer activity by promoting apoptosis in SCC-25. The induction of apoptotic activity was dose dependent with pronounced effect in late apoptosis. The formulation appeared to reduce cell viability of oral keratinocytes (OKC). At CC50 it showed an inhibition against HPV-16 pseudovirus infection. The formulation had no antimicrobial activity against S. mutans, P. gingivalis and C. albicans. No significant NO inhibitory activity and wound healing effects were found.
CONCLUSIONS: 1% α-MG in orabase gel exhibited anticancer activity by inducing apoptosis although low level of cytotoxicity observed in OKC was present. The appropriate carrier for novel nano-particles targeting cancer cells should be further investigated.
方法:开发了含有α-MG的口服凝胶制剂。评估对SCC-25的抗癌活性。使用流式细胞术技术确定凋亡诱导。抗HPV-16假病毒的抗病毒活性和抗变形链球菌的抗菌活性,研究了牙龈卟啉单胞菌和白色念珠菌。进行NO抑制。通过体外划痕测定确定成纤维细胞迁移。
结果:1%α-MG在orabase凝胶中的制剂通过促进SCC-25中的细胞凋亡而表现出抗癌活性。凋亡活性的诱导是剂量依赖性的,在晚期凋亡中具有显着的作用。该制剂似乎降低了口腔角质形成细胞(OKC)的细胞活力。在CC50时,它显示出对HPV-16假病毒感染的抑制作用。该制剂对变形链球菌没有抗菌活性,牙龈卟啉单胞菌和白色念珠菌。没有发现明显的NO抑制活性和伤口愈合作用。
结论:1%的α-MG在orabase凝胶中通过诱导细胞凋亡表现出抗癌活性,尽管在OKC中观察到低水平的细胞毒性。应进一步研究靶向癌细胞的新型纳米颗粒的合适载体。