Piccinelli A L, Mahmood N, Mora G, Poveda L, De Simone F, Rastrelli L
Dipartimento di Scienze Farmaceutiche, Università di Salerno, Via Ponte Don Melillo, 84084 Fisciano, Salerno, Italy.
J Pharm Pharmacol. 2005 Sep;57(9):1109-15. doi: 10.1211/jpp.57.9.0006.
Previously, we isolated two new dibenzylbutyrolactone-type lignans, named phenaxolactones and, from the leaves of Phenax angustifolius Wedd. (Urticaceae). In this investigation three new dibenzylbutyrolactone lignans (phenaxolactones), together with phenaxolactone, and flavones vitexin, isovitexin, were isolated from Phenax rugosus Wedd. leaves collected in Santa Ana, Costa Rica. The structures were elucidated using 1D and 2D NMR spectroscopy as well as mass spectrometry. Phenaxolactones and flavones and were evaluated for their inhibitory activity against HIV-1MN in infected C8166 cells. The most promising compound was phenaxolactone with an EC50 value of 3.0 microM, no cytotoxicity at 112 microM and a therapeutic index value of 37.3.
此前，我们从狭叶菲纳草（荨麻科）的叶子中分离出两种新的二苄基丁内酯型木脂素，命名为菲纳内酯。在本研究中，从采集于哥斯达黎加圣安娜的皱叶菲纳草的叶子中，分离出了三种新的二苄基丁内酯木脂素（菲纳内酯），以及菲纳内酯、黄酮类化合物牡荆素和异牡荆素。通过一维和二维核磁共振光谱以及质谱对其结构进行了阐明。对菲纳内酯和黄酮类化合物进行了评估，以检测它们对感染HIV-1MN的C8166细胞的抑制活性。最有前景的化合物是菲纳内酯，其半数有效浓度（EC50）值为3.0微摩尔，在112微摩尔浓度下无细胞毒性，治疗指数值为37.3。
