Feriotto Giordana, Marchetti Nicola, Costa Valentina, Beninati Simone, Tagliati Federico, Mischiati Carlo
Department of Chemistry and Pharmaceutical Sciences, University of Ferrara, via Luigi Borsari 46, 44121, Ferrara, Italy.
Department of Biology, University "Tor Vergata", Via della Ricerca Scientifica I-228, Rome, Italy.
Chem Biodivers. 2018 Feb;15(2). doi: 10.1002/cbdv.201700436. Epub 2018 Jan 31.
New drugs would be beneficial to fight resistant HIV strains, in particular those capable of interfering with essential viral functions other than those targeted by highly active antiretroviral therapy drugs. Despite the central role played by Tat protein in HIV transcription, a search for vegetable extracts able to hamper this important viral function was never carried out. In this work, we evaluated the chemical composition and possible interference of essential oil from Thymus vulgaris, Cananga odorata, Cymbopogon citratus, and Rosmarinus officinalis with the Tat/TAR-RNA interaction and with Tat-induced HIV-1 LTR transcription. GC/MS Analysis demonstrated the biodiversity of herbal species translated into essential oils composed of different blends of terpenes. In all of them, 4 - 6 constituents represent from 81.63% to 95.19% of the total terpenes. Essential oils of Thymus vulgaris, Cymbopogon citratus, and Rosmarinus officinalis were active in interfering with Tat functions, encouraging further studies to identify single terpenes responsible for the antiviral activity. In view of the quite different composition of these essential oils, we concluded that their interference on Tat function depends on specific terpene or a characteristic blend.
新型药物将有助于对抗耐药性HIV毒株，特别是那些能够干扰除高效抗逆转录病毒治疗药物所靶向功能之外的基本病毒功能的毒株。尽管Tat蛋白在HIV转录中发挥着核心作用，但从未有人寻找过能够阻碍这一重要病毒功能的植物提取物。在这项研究中，我们评估了百里香、依兰、柠檬香茅和迷迭香精油的化学成分，以及它们对Tat/TAR-RNA相互作用和Tat诱导的HIV-1长末端重复序列（LTR）转录的可能干扰。气相色谱/质谱分析表明，这些草本植物的生物多样性转化为了由不同萜类混合物组成的精油。在所有精油中，4至6种成分占总萜类的81.63%至95.19%。百里香、柠檬香茅和迷迭香的精油在干扰Tat功能方面具有活性，这鼓励进一步研究以确定具有抗病毒活性的单一萜类。鉴于这些精油的成分差异很大，我们得出结论，它们对Tat功能的干扰取决于特定的萜类或特征性混合物。
