Tan Suiyi, Yang Bin, Liu Juan, Xun Tianrong, Liu Yonghong, Zhou Xuefeng
a Guangzhou Key Laboratory of Drug Research for Emerging Virus Prevention and Treatment, Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Science , South Medical University , Guangzhou , China.
b Chinese Academy of Sciences (CAS) Key Laboratory of Tropical Marine Bio-Resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica , South China Sea Institute of Oceanology, CAS , Guangzhou , China.
Nat Prod Res. 2019 May;33(10):1467-1471. doi: 10.1080/14786419.2017.1416376. Epub 2017 Dec 19.
Marine micro-organisms have been proven to be excellent sources of bioactive compounds against HIV-1. Several natural products obtained from marine-derived fungi were screened for their activities to inhibit HIV-1 infection. Penicillixanthone A (PXA), a natural xanthone dimer from jellyfish-derived fungus , displayed potent anti-HIV-1 activity by inhibiting infection against CCR5-tropic HIV-1 SF162 and CXCR4-tropic HIV-1 NL4-3, with IC of 0.36 and 0.26 μM, respectively. Molecular docking study was conducted to understand the possible binding mode of PXA with the CCR5/CXCR4. The results revealed that, the marine-derived PXA, as a CCR5/CXCR4 dual-coreceptor antagonist, presents a new type of potential lead product for the development of anti-HIV therapeutics.
海洋微生物已被证明是抗HIV-1生物活性化合物的优良来源。对几种从海洋来源真菌中获得的天然产物进行了抑制HIV-1感染活性的筛选。青霉黄原酮A（PXA）是一种从水母来源真菌中提取的天然黄原酮二聚体，通过抑制对CCR5嗜性HIV-1 SF162和CXCR4嗜性HIV-1 NL4-3的感染，显示出强大的抗HIV-1活性，其IC50分别为0.36和0.26μM。进行了分子对接研究以了解PXA与CCR5/CXCR4的可能结合模式。结果表明，海洋来源的PXA作为一种CCR5/CXCR4双共受体拮抗剂，为抗HIV治疗药物的开发提供了一种新型的潜在先导产品。
