L. 叶、树皮和果皮提取物及其主要化合物的体外抗HIV-1逆转录酶和整合酶特性

In Vitro Anti-HIV-1 Reverse Transcriptase and Integrase Properties of L. Leaves, Bark, and Peel Extracts and Their Main Compounds.

作者信息

Sanna Cinzia, Marengo Arianna, Acquadro Stefano, Caredda Alessia, Lai Roberta, Corona Angela, Tramontano Enzo, Rubiolo Patrizia, Esposito Francesca

机构信息

Laboratory of Pharmaceutical Botany, Department of Life and Environmental Sciences, University of Cagliari, Via S. Ignazio da Laconi 13, 09123 Cagliari, Italy.

Department of Drug Science and Technology, University of Turin, Via Pietro Giuria 9, 10125 Turin, Italy.

出版信息

Plants (Basel). 2021 Oct 7;10(10):2124. doi: 10.3390/plants10102124.

Abstract

In a search for natural compounds with anti-HIV-1 activity, we studied the effect of the ethanolic extract obtained from leaves, bark, and peels of L. for the inhibition of the HIV-1 reverse transcriptase (RT)-associated ribonuclease H (RNase H) and integrase (IN) LEDGF-dependent activities. The chemical analyses led to the detection of compounds belonging mainly to the phenolic and flavonoid chemical classes. Ellagic acid, flavones, and triterpenoid molecules were identified in leaves. The bark and peels were characterized by the presence of hydrolyzable tannins, such as punicalins and punicalagins, together with ellagic acid. Among the isolated compounds, the hydrolyzable tannins and ellagic acid showed a very high inhibition (IC values ranging from 0.12 to 1.4 µM and 0.065 to 0.09 µM of the RNase H and IN activities, respectively). Of the flavonoids, luteolin and apigenin were found to be able to inhibit RNase H and IN functions (IC values in the 3.7-22 μM range), whereas luteolin 7--glucoside showed selective activity for HIV-1 IN. In contrast, betulinic acid, ursolic acid, and oleanolic acid were selective for the HIV-1 RNase H activity. Our results strongly support the potential of non-edible organs as a valuable source of anti-HIV-1 compounds.

摘要

在寻找具有抗HIV-1活性的天然化合物的过程中,我们研究了从[植物名称]的叶子、树皮和果皮中提取的乙醇提取物对HIV-1逆转录酶(RT)相关的核糖核酸酶H(RNase H)和整合酶(IN)LEDGF依赖性活性的抑制作用。化学分析导致检测到主要属于酚类和黄酮类化学类别的化合物。在叶子中鉴定出了鞣花酸、黄酮和三萜类分子。树皮和果皮的特征是存在可水解单宁,如石榴苷和石榴皮素,以及鞣花酸。在分离出的化合物中,可水解单宁和鞣花酸表现出非常高的抑制作用(RNase H和IN活性的IC值分别为0.12至1.4μM和0.065至0.09μM)。在黄酮类化合物中,发现木犀草素和芹菜素能够抑制RNase H和IN的功能(IC值在3.7-22μM范围内),而木犀草素7-O-葡萄糖苷对HIV-1 IN表现出选择性活性。相比之下,桦木酸、熊果酸和齐墩果酸对HIV-1 RNase H活性具有选择性。我们的结果有力地支持了非食用器官作为抗HIV-1化合物宝贵来源的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d86/8539310/feb01eb8a452/plants-10-02124-g001.jpg

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