Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Yushan Road 5, Qingdao 266003, China.
Mar Drugs. 2013 Dec 2;11(12):4788-98. doi: 10.3390/md11124788.
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.
从南海采集的软珊瑚 Sarcophyton sp. 的化学成分研究得到了三种新的多羟基甾醇化合物(1-3),以及七种已知化合物(4-10)。通过广泛的光谱方法和与相关已知化合物的数据比较,确定了它们的结构。所有分离物都具有 3β,5α,6β-三羟基甾核。评估了分离物对选定的 HL-60、HeLa 和 K562 肿瘤细胞系的细胞毒性和抗 H1N1(甲型流感病毒(IAV))活性。化合物 2、3 和 5-8 对 K562 细胞系具有很强的活性,IC₅₀ 值范围为 6.4 至 10.3 μM。化合物 1、6-8 强烈抑制 HL-60 肿瘤细胞系的生长,6 对 HeLa 细胞系也具有细胞毒性。此外,还讨论了分离物的初步构效关系。在 3β,5α,6β-三醇甾醇中,C-11 位的 OAc 基团被认为是其细胞毒性的重要药效团。化合物 4 和 9 对 H1N1 IAV 表现出显著的活性,IC₅₀ 值分别为 19.6 和 36.7 μg/mL。