Cock Ian Edwin, Matthews Benjamin, Basson Adriaan Erasmus
Centre for Planetary Health and Food Security, Griffith University, Brisbane 4222, Australia.
Queensland Brain Institute, University of Queensland, Brisbane 4072, Australia.
Molecules. 2025 Apr 10;30(8):1701. doi: 10.3390/molecules30081701.
The emergence of HIV strains resistant to the current anti-retroviral drugs has necessitated the search for new anti-retroviral medications. Methanolic and aqueous fruit extracts have potent inhibitory activity against several phases of the HIV-1 replicative cycle. Cell infectivity studies using a non-resistant HIV-1 pseudovirus demonstrated that the methanolic (IC 16 µg/mL) and aqueous extracts (IC 19 µg/mL) were potent inhibitors of viral infection in a non-replicating HIV-1 assay. Both extracts also inhibited HIV-1 reverse transcriptase (IC values of 35 and 33 µg/mL for methanolic and aqueous extracts, respectively) and HIV-1 protease (IC values of 19 and 27 µg/mL, respectively) in recombinant enzyme assays. Given their inhibitory activities against multiple phases of HIV-1 replication, fruit extracts may be particularly useful as HIV-1 therapeutics. Furthermore, both extracts displayed good safety profiles and therapeutic indices, indicating their suitability for therapeutic usage. LC-MS metabolomic profiling analysis of the methanolic extract identified several interesting constituents, including a relative abundance of tannins, as well as several flavonoids and stilbenes. All of these compounds have previously been reported to have bioactivities consistent with the anti-HIV-1 activities reported herein. Based on these studies, methanolic and aqueous fruit extracts are promising potential therapies for the prevention, treatment and management of HIV-1.
对当前抗逆转录病毒药物产生耐药性的艾滋病毒毒株的出现，使得人们有必要寻找新的抗逆转录病毒药物。甲醇提取物和水提取物对HIV-1复制周期的多个阶段具有强大的抑制活性。使用非耐药HIV-1假病毒进行的细胞感染性研究表明，在非复制性HIV-1检测中，甲醇提取物（IC为16 µg/mL）和水提取物（IC为19 µg/mL）是病毒感染的有效抑制剂。在重组酶检测中，两种提取物还抑制了HIV-1逆转录酶（甲醇提取物和水提取物的IC值分别为35和33 µg/mL）和HIV-1蛋白酶（IC值分别为19和27 µg/mL）。鉴于其对HIV-1复制多个阶段的抑制活性，水果提取物作为HIV-1治疗药物可能特别有用。此外，两种提取物都显示出良好的安全性和治疗指数，表明它们适合用于治疗。甲醇提取物的LC-MS代谢组学分析鉴定出了几种有趣的成分，包括相对丰富的单宁，以及几种黄酮类化合物和芪类化合物。所有这些化合物此前都被报道具有与本文报道的抗HIV-1活性一致的生物活性。基于这些研究，甲醇提取物和水提取物有望成为预防、治疗和管理HIV-1的潜在疗法。
