Abdel-Mageed Wael M, Bayoumi Soad A H, Chen Caixia, Vavricka Christopher J, Li Li, Malik Ajamaluddin, Dai Huanqin, Song Fuhang, Wang Luoqiang, Zhang Jingyu, Gao George F, Lv Yali, Liu Lihong, Liu Xueting, Sayed Hanaa M, Zhang Lixin
CAS Key Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100190, PR China; Pharmacognosy Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt.
Pharmacognosy Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt.
Bioorg Med Chem. 2014 Apr 1;22(7):2236-43. doi: 10.1016/j.bmc.2014.02.014. Epub 2014 Feb 20.
The high mutation rate of RNA viruses has resulted in limitation of vaccine effectiveness and increased emergence of drug-resistant viruses. New effective antivirals are therefore needed to control of the highly mutative RNA viruses. The n-butanol fraction of the stem bark of Mangifera indica exhibited inhibitory activity against influenza neuraminidase (NA) and coxsackie virus 3C protease. Bioassay guided phytochemical study of M. indica stem bark afforded two new compounds including one benzophenone C-glycoside (4) and one xanthone dimer (7), together with eleven known compounds. The structures of these isolated compounds were elucidated on the basis of spectroscopic evidences and correlated with known compounds. Anti-influenza and anti-coxsackie virus activities were evaluated by determining the inhibition of anti-influenza neuraminidase (NA) from pandemic A/RI/5+/1957 H2N2 influenza A virus and inhibition of coxsackie B3 virus 3C protease, respectively. The highest anti-influenza activity was observed for compounds 8 and 9 with IC50 values of 11.9 and 9.2μM, respectively. Compounds 8 and 9 were even more potent against coxsackie B3 virus 3C protease, with IC50 values of 1.1 and 2.0μM, respectively. Compounds 8 and 9 showed weak cytotoxic effect against human hepatocellular carcinoma and human epithelial carcinoma cell lines through MTT assay.
RNA病毒的高突变率导致疫苗效力受限，耐药病毒出现的频率增加。因此，需要新的有效抗病毒药物来控制高突变性的RNA病毒。芒果茎皮的正丁醇馏分对流感神经氨酸酶（NA）和柯萨奇病毒3C蛋白酶具有抑制活性。对芒果茎皮进行生物测定指导的植物化学研究，得到了两种新化合物，包括一种二苯甲酮C-糖苷（4）和一种呫吨酮二聚体（7），以及十一种已知化合物。这些分离出的化合物的结构通过光谱证据得以阐明，并与已知化合物进行了关联。分别通过测定对大流行的A/RI/5+/1957 H2N2甲型流感病毒的抗流感神经氨酸酶（NA）的抑制作用以及对柯萨奇B3病毒3C蛋白酶的抑制作用，来评估抗流感和抗柯萨奇病毒的活性。化合物8和9表现出最高的抗流感活性，其IC50值分别为11.9和9.2μM。化合物8和9对柯萨奇B3病毒3C蛋白酶的活性更强，IC50值分别为1.1和2.0μM。通过MTT测定，化合物8和9对人肝癌细胞系和人上皮癌细胞系显示出较弱的细胞毒性作用。
