PDF(Pubmed)
Abstract：
BACKGROUND: Plant-derived compounds have chemopreventive properties to be used as alternative medicine. Pericarp of Mangosteen (Garcinia mangostana Linn.), a tropical fruit in Southeast Asia contains a phytochemical α-mangostin (α-MG) that demonstrates potent anticancer effects against various types of cancer. α-MG has been reported to be the most effective agent in human cancer cell lines. The objectives of this study were to develop oral gel formulations containing α-MG and determine their (1) anticancer activity, (2) anti-HPV-16 and antimicrobial activities, (3) nitric oxide (NO) inhibitory activity, and (4) wound healing effect.
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.
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.
摘要：
背景：植物来源的化合物具有化学预防特性，可用作替代药物。山竹果果皮（藤黄。),东南亚的一种热带水果含有植物化学物质α-芒果素（α-MG），对各种类型的癌症具有有效的抗癌作用。已报道α-MG是人癌细胞系中最有效的试剂。这项研究的目的是开发含有α-MG的口服凝胶制剂并确定其（1）抗癌活性，（2）抗HPV-16和抗菌活性，（3）一氧化氮（NO）抑制活性，和(4)伤口愈合效果。
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。
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。
