†Instituto Universitario de Bio-Orgánica "Antonio González", Universidad de La Laguna, Avenida Astrofísico Francisco Sánchez 2, 38206 La Laguna, Tenerife, Spain.
‡Unidad de Inmunopatología, Centro Nacional de Microbiología, Instituto de Salud Carlos III, Carretera Pozuelo Km.2, 28220-Majadahonda, Madrid, Spain.
J Nat Prod. 2015 May 22;78(5):1045-55. doi: 10.1021/np501025r. Epub 2015 Apr 30.
As a part of our investigation into new anti-HIV agents, we report herein the isolation, structure elucidation, and biological activity of six new (1-6) and 20 known (7-26) pentacyclic lupane-type triterpenoids from the stem of Cassine xylocarpa and root bark of Maytenus cuzcoina. Their stereostructures were elucidated on the basis of spectroscopic and spectrometric methods, including 1D and 2D NMR techniques. To gain a more complete understanding of the structural requirements for anti-HIV activity, derivatives 27-48 were prepared by chemical modification of the main secondary metabolites. Sixteen compounds from this series displayed inhibitory effects of human immunodeficiency virus type 1 replication with IC50 values in the micromolar range, highlighting compounds 12, 38, and 42 (IC50 4.08, 4.18, and 1.70 μM, respectively) as the most promising anti-HIV agents.
作为我们对新型抗 HIV 药物研究的一部分，我们在此报告了从木莲叶的茎和南美榆绿木的根皮中分离得到的六个新的（1-6）和 20 个已知的（7-26）五环齐墩果烷型三萜化合物的分离、结构阐明和生物活性。根据光谱和光谱方法，包括 1D 和 2D NMR 技术，阐明了它们的立体结构。为了更全面地了解抗 HIV 活性的结构要求，通过主要次生代谢物的化学修饰制备了衍生物 27-48。该系列中的 16 种化合物对人类免疫缺陷病毒 1 型复制具有抑制作用，IC50 值在微摩尔范围内，其中化合物 12、38 和 42（IC50 分别为 4.08、4.18 和 1.70 μM）表现出最有希望的抗 HIV 作用。
