Inhibition of the Dimerization and Active Site of HIV-1 Protease by Secondary Metabolites from the Vietnamese Mushroom Ganoderma colossum

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• 作者：Riham Salah El Dine ; Ali M. El Halawany ; Chao-Mei Ma ; Masao Hattori
• 刊名：Journal of Natural Products
• 出版年：2009
• 出版时间：November 30, 2009
• 年：2009
• 卷：72
• 期：11
• 页码：2019-2023
• 全文大小：207K
• 年卷期：v.72,no.11(November 30, 2009)
• ISSN：1520-6025

文摘

A new farnesyl hydroquinone, ganomycin I (1), was isolated along with ganomycin B (2) from the chloroform extract of the fruiting bodies of the Vietnamese mushroom Ganoderma colossum. These compounds inhibited HIV-1 protease with IC₅₀ values of 7.5 and 1.0 μg/mL, respectively. Kinetic studies using Zhang−Poorman and Lineweaver plots revealed that compound 2 competitively inhibited the active site of the enzyme, whereas the tetracyclic triterpene schisanlactone A, previously isolated from the same fungus, was a dimerization inhibitor, with an IC₅₀ value of 5.0 μg/mL. The previous findings were also confirmed by the virtual docking of both compounds with HIV-1 protease crystal structure.