Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Yushan Road 5, Qingdao 266003, China.
Laboratory of Marine Drugs and Biological Products, National Laboratory for Marine Science and Technology, Qingdao 266235, China.
Mar Drugs. 2018 Apr 13;16(4):127. doi: 10.3390/md16040127.
Three new sesquiterpenoids (sinuketal (), sinulins A and B ( and )) and two new cembranoids (sinulins C and D ( and )), as well as eight known sesquiterpenoids () and eight known cembranoids (), were isolated from the Xisha soft coral sp. Their structures were elucidated by extensive spectroscopic analysis. Compound possesses an unprecedented isopropyl-branched bicyclo [6.3.0] undecane carbon skeleton with unique endoperoxide moiety, and a plausible biosynthetic pathway of it was postulated. According to the reported biological properties of endoperoxide, the antimalarial, cytotoxic, antiviral, and target inhibitory activities of were tested. Compound showed mild in vitro antimalarial activity against 3D7, weak cytotoxic activities toward Jurkat, MDA-MB-231, and U2OS cell lines, inhibitory effects against influenza A viruses H1N1 and PR8, as well as mild target inhibitory activity against acetylcholinesterase. The other compounds were evaluated for cytotoxicities against HeLa, HCT-116, and A549 tumor cell lines and target inhibitory activities against protein tyrosine phosphatase 1B (PTP1B). Compound exhibited cytotoxicities against HeLa and HCT-116, and compounds , , and showed mild target inhibitory activities against PTP1B.
从西沙软珊瑚 sp. 中分离得到三个新的倍半萜(sinuketal (),sinulins A 和 B ( 和 ))和两个新的柏木烷(sinulins C 和 D ( 和 )),以及八个已知的倍半萜 () 和八个已知的柏木烷 ()。通过广泛的光谱分析阐明了它们的结构。化合物 具有前所未有的异丙基支链双环 [6.3.0] 十一烷碳骨架和独特的内过氧化物部分,提出了其可能的生物合成途径。根据内过氧化物的报道生物活性,测试了 的抗疟、细胞毒性、抗病毒和靶标抑制活性。化合物 对 3D7 具有温和的体外抗疟活性,对 Jurkat、MDA-MB-231 和 U2OS 细胞系表现出较弱的细胞毒性,对流感 A 病毒 H1N1 和 PR8 具有抑制作用,以及对乙酰胆碱酯酶的温和靶标抑制活性。其他化合物被评估对 HeLa、HCT-116 和 A549 肿瘤细胞系的细胞毒性和对蛋白酪氨酸磷酸酶 1B(PTP1B)的靶标抑制活性。化合物 对 HeLa 和 HCT-116 表现出细胞毒性,化合物 、 、 和 对 PTP1B 表现出温和的靶标抑制活性。