Lu Shengsheng, Xie Xi, Hu Jianan, Lin Haixing, Li Fangfang, Zhou Runhong, Guo Jiayin, Wu Shaohua, He Jian
Group of Peptides and Natural Products Research, School of Pharmaceutical Sciences, Southern Medical University, 1838 Guangzhou Avenue North, Guangzhou 510515, People's Republic of China; Department of Pharmacy, Affiliated Tumor Hospital of Guangxi Medical University, Nanning 530021, Guangxi, People's Republic of China.
Group of Peptides and Natural Products Research, School of Pharmaceutical Sciences, Southern Medical University, 1838 Guangzhou Avenue North, Guangzhou 510515, People's Republic of China.
Fitoterapia. 2022 Mar;157:105107. doi: 10.1016/j.fitote.2021.105107. Epub 2021 Dec 22.
Three novel norsesquiterpenoids, (2R,4S,8aR)-8,8a,1,2,3,4-hexahydro-2-hydroxy-4,8a-dimethyl-2(2H)-naphthalenone (1), (1S,3S,4S,4aS,8aR)-4,8a-dimethyloctahydronaphthalene-1,3,4a(3H)-triol(2), (4S,4aS,8aS)-octahydro-4a-hydroxy-4, 8a-dimethyl-1(2H)-naphthalenone (3), as well as six other known analogues (4-9), were isolated from the culture broth of Streptomyces sp. XM17, an actinobacterial strain inhabiting the fresh feces of the giant panda Ailuropoda melanoleuca. The chemical structures of 1-3 were elucidated comprehensively by NMR spectroscopic and MS analyses, furthermore, the stereochemical configurations were resolved by NOESY experiments, along with ECD spectral and single-crystal X-ray crystallographic analyses. These compounds were then tested for their antiviral activities using the "pretreatment of virus" approach, which showed that most of these compounds were potent in inhibiting the entry of influenza A virus, with IC values ranging from 5 to 49 nM and selectivity indices all above 500.
从栖息于大熊猫新鲜粪便中的放线菌菌株链霉菌属XM17的培养液中分离出三种新型倍半萜类化合物，即(2R,4S,8aR)-8,8a,1,2,3,4-六氢-2-羟基-4,8a-二甲基-2(2H)-萘酮(1)、(1S,3S,4S,4aS,8aR)-4,8a-二甲基八氢萘-1,3,4a(3H)-三醇(2)、(4S,4aS,8aS)-八氢-4a-羟基-4,8a-二甲基-1(2H)-萘酮(3)，以及其他六种已知类似物(4-9)。通过核磁共振光谱和质谱分析全面阐明了1-3的化学结构，此外，通过NOESY实验、ECD光谱和单晶X射线晶体学分析确定了立体化学构型。然后使用“病毒预处理”方法测试了这些化合物的抗病毒活性，结果表明这些化合物中的大多数对甲型流感病毒的进入具有强效抑制作用，IC值范围为5至49 nM，选择性指数均高于500。
