title: Polyhydroxylated steroids from the South China Sea soft coral Sarcophyton sp. and their cytotoxic and antiviral activities.
abstract: Chemical investigation on the soft coral Sarcophyton sp. collected from the South China Sea yielded three new polyhydroxylated steroids, compounds (1-3), together with seven known ones (4-10). Their structures were established by extensive spectroscopic methods and comparison of their data with those of the related known compounds. All the isolates possessed the 3β,5α,6β-trihydroxylated steroidal nucleus. The cytotoxicities against selected HL-60, HeLa and K562 tumor cell lines and anti-H1N1 (Influenza A virus (IAV)) activities for the isolates were evaluated. Compounds 2, 3 and 5-8 exhibited potent activities against K562 cell lines with IC₅₀ values ranging from 6.4 to 10.3 μM. Compounds 1, 6-8 potently inhibited the growth of HL-60 tumor cell lines, and 6 also showed cytotoxicity towards HeLa cell lines. In addition, preliminary structure-activity relationships for the isolates are discussed. The OAc group at C-11 is proposed to be an important pharmacophore for their cytotoxicities in the 3β,5α,6β-triol steroids. Compounds 4 and 9 exhibited significant anti-H1N1 IAV activity with IC₅₀ values of 19.6 and 36.7 μg/mL, respectively.
authors: Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Yushan Road 5, Qingdao 266003, China. liguoqiang@ouc.edu.cn.
authors: Kai-Kai
authors: KK
authors: Gong
authors: Xu-Li
authors: XL
authors: Tang
authors: Gang
authors: G
authors: Zhang
authors: Can-Ling
authors: CL
authors: Cheng
authors: Xing-Wang
authors: XW
authors: Zhang
authors: Ping-Lin
authors: PL
authors: Li
authors: Guo-Qiang
authors: GQ
authors: Li
mesh_terms: D000818:Animals; D037421:Anthozoa / Q000737:chemistry*; D000998:Antiviral Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002681:China; D003603:Cytotoxins / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D018922:HL-60 Cells; D006367:HeLa Cells; D006801:Humans; D053118:Influenza A Virus, H1N1 Subtype / Q000187:drug effects; D020014:K562 Cells; D009792:Oceans and Seas; D013256:Steroids / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D003603:Cytotoxins; D013256:Steroids