C. U Shah College of Pharmacy, S.N.D.T. Women's University, Santacruz West, Mumbai, 400049, India.
National AIDS Research Institute, 73, 'G'-Block, MIDC, Bhosari, Pune, 411 026, India.
BMC Complement Med Ther. 2020 Mar 6;20(1):69. doi: 10.1186/s12906-020-2816-x.
Human Immunodeficiency Virus (HIV) persists to be a significant public health issue worldwide. The current strategy for the treatment of HIV infection, Highly Active Antiretroviral Therapy (HAART), has reduced deaths from AIDS related disease, but it can be an expensive regime for the underdeveloped and developing countries where the supply of drugs is scarce and often not well tolerated, especially in persons undergoing long term treatment. The present therapy also has limitations of development of multidrug resistance, thus there is a need for the discovery of novel anti-HIV compounds from plants as a potential alternative in combating HIV disease.
Ten Indian medicinal plants were tested for entry and replication inhibition against laboratory adapted strains HIV-1, HIV-1 and primary isolates HIV-1, HIV-1 in TZM-bl cell lines and primary isolates HIV-1, HIV-1 in PM1 cell lines. The plant extracts were further evaluated for toxicity in HEC-1A epithelial cell lines by transwell epithelial model.
The methanolic extracts of Achyranthes aspera, Rosa centifolia and aqueous extract of Ficus benghalensis inhibited laboratory adapted HIV-1 strains (IC 3.6-118 μg/ml) and primary isolates (IC 4.8-156 μg/ml) in TZM-bl cells. Methanolic extract of Strychnos potatorum, aqueous extract of Ficus infectoria and hydroalcoholic extract of Annona squamosa inhibited laboratory adapted HIV-1 strains (IC 4.24-125 μg/ml) and primary isolates (IC 18-156 μg/ml) in TZM-bl cells. Methanolic extracts of Achyranthes aspera and Rosa centifolia, (IC1-9 μg/ml) further significantly inhibited HIV-1 primary isolates in PM1cells. Methanolic extracts of Tridax procumbens, Mallotus philippinensis, Annona reticulate, aqueous extract of Ficus benghalensis and hydroalcoholic extract of Albizzia lebbeck did not exhibit anti-HIV activity in all the tested strains. Methanolic extract of Rosa centifolia also demonstrated to be non-toxic to HEC-1A epithelial cells and maintained epithelial integrity (at 500 μg/ml) when tested in transwell dual-chamber.
These active methanolic extracts of Achyranthes aspera and Rosa centifolia, could be further subjected to chemical analysis to investigate the active moiety responsible for the anti-HIV activity. Methanolic extract of Rosa centifolia was found to be well tolerated maintaining the epithelial integrity of HEC-1A cells in vitro and thus has potential for investigating it further as candidate microbicide.
人类免疫缺陷病毒（HIV）仍然是全球一个重大的公共卫生问题。目前治疗 HIV 感染的策略，即高效抗逆转录病毒疗法（HAART），已经降低了与艾滋病相关疾病的死亡率，但对于药物供应稀缺且往往难以耐受的不发达国家和发展中国家来说，这是一种昂贵的治疗方法，尤其是在长期接受治疗的人群中。目前的治疗方法也存在多药耐药性发展的限制，因此需要从植物中发现新的抗 HIV 化合物，作为对抗 HIV 疾病的潜在替代方法。
对十种印度药用植物进行了实验室适应株 HIV-1、HIV-1 和原发性分离株 HIV-1、HIV-1 在 TZM-bl 细胞系和原发性分离株 HIV-1、HIV-1 在 PM1 细胞系中的进入和复制抑制作用的检测。将植物提取物进一步通过 Transwell 上皮模型在 HEC-1A 上皮细胞系中进行毒性评估。
牛膝、玫瑰和榕树叶的甲醇提取物抑制了实验室适应株 HIV-1 株（IC3.6-118μg/ml）和原发性分离株（IC4.8-156μg/ml）在 TZM-bl 细胞中的复制。Strychnos potatorum 的甲醇提取物、榕树叶的水提取物和 Annona squamosa 的水醇提取物抑制了实验室适应株 HIV-1 株（IC4.24-125μg/ml）和原发性分离株（IC18-156μg/ml）在 TZM-bl 细胞中的复制。牛膝和玫瑰的甲醇提取物（IC1-9μg/ml）进一步显著抑制了 PM1 细胞中的 HIV-1 原发性分离株。三达蒲公英、马鲁古桐、印度榕、榕树叶的水提取物和 Albizzia lebbeck 的水醇提取物在所有测试株中均未表现出抗 HIV 活性。玫瑰的甲醇提取物对 HEC-1A 上皮细胞也表现出非毒性，并在 Transwell 双层中以 500μg/ml 的浓度维持上皮完整性。
这些活性的牛膝和玫瑰甲醇提取物可以进一步进行化学分析，以研究负责抗 HIV 活性的活性部分。玫瑰的甲醇提取物在体外被发现具有良好的耐受性，能够维持 HEC-1A 细胞的上皮完整性，因此具有进一步作为候选杀微生物剂进行研究的潜力。
