Centro Nacional de Microbiología, Instituto de Salud Carlos III, Crt. Majadahonda a Pozuelo, 28220 Majadahonda, Madrid, Spain.
Phytomedicine. 2010 Jan;17(1):69-74. doi: 10.1016/j.phymed.2009.08.008. Epub 2009 Sep 11.
Screening of plants from the Iberian Peninsula for anti-human immunodeficiency virus (-HIV) activity revealed that aqueous extract of Tuberaria lignosa gave positive results. Following an activity-guided procedure, the crude extract was counterextracted, and the subsequent fractions obtained tested for their anti-HIV activity in vitro. The bioassay-guided fractionation of the extract afforded an ellagitannin enriched fraction (EEF) isolated for the first time from this species. This EEF exhibited antiviral activity against HIV in MT-2 infected cells, with an IC(50) value of 2.33mug/ml (selectivity index greater than 21). Inhibition of HIV infection by EEF appears to be mediated by CD4 down-regulation, the main receptor for HIV entry. CXCR4 and CCR5 receptors were not affected by EEF, explaining why EEF is able to inhibit R5 and X4 infections.
从伊比利亚半岛筛选具有抗人类免疫缺陷病毒（-HIV）活性的植物，发现块茎腹皮木的水提物呈现阳性结果。经过活性导向的处理，对粗提取物进行了反萃取，随后对获得的各个部分进行了体外抗 HIV 活性测试。该提取物的生物活性导向分离获得了首次从该物种中分离得到的富含鞣花单宁的部分（EEF）。该 EEF 对感染 MT-2 的细胞中的 HIV 具有抗病毒活性，IC50 值为 2.33mug/ml（选择性指数大于 21）。EEF 对 HIV 感染的抑制作用似乎是通过 CD4 下调介导的，CD4 是 HIV 进入的主要受体。EEF 不影响 CXCR4 和 CCR5 受体，这解释了为什么 EEF 能够抑制 R5 和 X4 感染。
