Woodylides A–C, New Cytotoxic Linear Polyketides from the South China Sea Sponge Plakortis simplex

Marine Drugs

Hao-Bing Yu¹  Xiang-Fang Liu²  Ying Xu¹  Jian-Hong Gan¹  Wei-Hua Jiao¹  Yang Shen² 

[1] Laboratory of Marine Drugs, Department of Pharmacy, Changzheng Hospital, Second Military Medical University, Shanghai 200003, China;Department of Pharmacy, Shanghai Children’s Hospital, Shanghai Jiao Tong University, Shanghai 200040, China;

关键词: Plakortis simplex;    woodylides;    cytotoxicity;    PTP1B inhibitory activity;   

DOI  :  10.3390/md10051027

来源: mdpi

【 摘 要 】

Three new polyketides, woodylides A–C (1–3), were isolated from the ethanol extract of the South China Sea sponge Plakortis simplex. The structures were elucidated by spectroscopic data (IR, 1D and 2D NMR, and HRESIMS). The absolute configurations at C-3 of 1 and 3 were determined by the modified Mosher’s method. Antifungal, cytotoxic, and PTP1B inhibitory activities of these polyketides were evaluated. Compounds 1 and 3 showed antifungal activity against fungi Cryptococcus neoformans with IC₅₀ values of 3.67 and 10.85 µg/mL, respectively. In the cytotoxicity test, compound 1 exhibited a moderate effect against the HeLa cell line with an IC₅₀ value of 11.2 µg/mL, and compound 3 showed cytotoxic activity against the HCT-116 human colon tumor cell line and PTP1B inhibitory activity with IC₅₀ values of 9.4 and 4.7 µg/mL, respectively.

【 授权许可】

CC BY   
© 2012 by the authors; licensee MDPI, Basel, Switzerland.