School of Pharmaceutical Sciences, Sun Yat-sen University , Guangzhou, Guangdong 510006, P. R. China.
Org Lett. 2014 Jan 3;16(1):282-5. doi: 10.1021/ol403282f. Epub 2013 Dec 12.
Selaginpulvilins A-D (1-4), four new phenols with an unprecedented 9,9-diphenyl-1-(phenylethynyl)-9H-fluorene skeleton, together with four known selaginellins (5-8) were isolated from Selaginella pulvinata. Their structures were elucidated by spectroscopic analysis and chemical correlation. The structure of 1 was confirmed by single-crystal X-ray diffraction. Compounds 1-8 exhibited remarkable inhibitory activities (IC50 values in the range of 0.11-5.13 μM) against phosphodiesterase-4 (PDE4), a drug target for the treatment of asthma and chronic obstructive pulmonary disease.
从卷柏中分离得到四个新的酚类化合物 Selaginpulvilins A-D（1-4），它们具有前所未有的 9,9-二苯基-1-（苯乙炔基）-9H-芴骨架，以及四个已知的 Selaginellins（5-8）。通过光谱分析和化学相关确定了它们的结构。化合物 1 的结构通过单晶 X 射线衍射确定。化合物 1-8 对磷酸二酯酶-4（PDE4）表现出显著的抑制活性（IC50 值在 0.11-5.13 μM 范围内），PDE4 是治疗哮喘和慢性阻塞性肺疾病的药物靶点。
