Tabrez Shams, Rahman Fazlur, Ali Rahat, Alouffi Abdulaziz S, Alshehri Bader Mohammed, Alshammari Fahdah Ayed, Alaidarous Mohammed A, Banawas Saeed, Bin Dukhyil Abdul Aziz, Rub Abdur
Infection and Immunity Lab (414), Department of Biotechnology, Jamia Millia Islamia (A Central University), New Delhi 110025, India.
King Abdulaziz City for Science and Technology, P.O. Box 6086, Riyadh 11442, Saudi Arabia.
ACS Omega. 2021 Jan 11;6(3):2318-2327. doi: 10.1021/acsomega.0c05629. eCollection 2021 Jan 26.
has a wide array of biologically active and therapeutically important class of compounds. important drug targets, sterol 24-c methyltransferase (SMT), trypanothione reductase (TR), pteridine reductase (PTR1), and nucleoside hydrolase (NH), were modelled, and molecular docking was performed against the abundant phytochemicals of its leaf extract. Molecular docking results provided the significant prima facie evidence of the leaf extract to have antileishmanial potential. To confirm this, we performed antileishmanial and cytotoxicity assays. Methanolic extract of leaves showed growth inhibition and proliferation of promastigote with an IC value of 43.31 ± 4.202 μg/mL. It also inhibited the growth of intra-macrophagic amastigotes with an IC value of 80.76 ± 3.626 μg/mL. extract was found cytotoxic at a very high concentration on human macrophages (CC = 626 ± 39 μg/mL). Annexin V/propidium iodide (PI) staining assay suggested partial apoptosis induction in parasites by to exert its antileishmanial activity. Here, for the first time, we have shown the antileishmanial potential of leaves. Overall, our results could open new insight for an affordable and natural antileishmanial with high efficacy and less toxicity.
具有一系列生物活性且在治疗上很重要的化合物类别。对重要的药物靶点,即甾醇24 - c甲基转移酶(SMT)、锥虫硫醇还原酶(TR)、蝶啶还原酶(PTR1)和核苷水解酶(NH)进行了建模,并针对其叶提取物中丰富的植物化学物质进行了分子对接。分子对接结果提供了叶提取物具有抗利什曼原虫潜力的重要初步证据。为了证实这一点,我们进行了抗利什曼原虫和细胞毒性测定。叶的甲醇提取物对前鞭毛体的生长具有抑制作用,其IC值为43.31±4.202μg/mL。它还抑制巨噬细胞内无鞭毛体的生长,IC值为80.76±3.626μg/mL。该提取物在非常高的浓度下对人巨噬细胞具有细胞毒性(CC = 626±39μg/mL)。膜联蛋白V/碘化丙啶(PI)染色试验表明,该提取物可诱导寄生虫部分凋亡以发挥其抗利什曼原虫活性。在此,我们首次展示了该叶的抗利什曼原虫潜力。总体而言,我们的结果可为一种价格合理、天然、高效且低毒的抗利什曼原虫药物开辟新的思路。