Ojha Sashi Bhusan, Sah Raj Kumar, Madan Evanka, Bansal Ruby, Roy Shaktirekha, Singh Shailja, Dhangadamajhi Gunanidhi
Department of Biotechnology, Maharaja Sriram Chandra Bhanja Deo University, Baripada, Odisha, 757003, India.
Special Centre for Molecular Medicine, Jawaharlal Nehru University, New Delhi, 110067, India.
Curr Microbiol. 2023 Apr 19;80(5):189. doi: 10.1007/s00284-023-03289-x.
Drug resistance to practically all antimalarial drugs in use necessitate the development of new chemotherapeutics against malaria. In this aspect, traditionally used plants with folklore reputation are the pillar for drug discovery. Cuscuta reflexa being traditionally used in the treatment of malaria in Odisha, India we aimed to experimentally validate its antimalarial potential. Different solvent extracts of C. reflexa or column fractions from a promising solvent extract were evaluated for in vitro anti-plasmodial activity against Plasmodium falciparum strain Pf3D7. Potent fractions were further evaluated for inhibition of parasite growth against different drug resistant strains. Safety of these fractions was determined by in vitro cyto-toxicity, and therapeutic effectiveness was evaluated by suppression of parasitemia and improvement in survival of experimental mice. Besides, their immunomodulatory effect was investigated in Pf-antigen stimulated RAW cells. GCMS fingerprints of active fractions was determined. Column separation of methanol extract which showed the highest in vitro antiplasmodial activity (IC = 14.48 μg/ml) resulted in eleven fractions, three of which (F2, F3, and F4) had anti-plasmodial IC ranging from ≤ 10 to 2.2 μg/ml against various P. falciparum strains with no demonstration of in vitro cytotoxicity. F4 displayed the highest in vivo parasite suppression, and had a mean survival time similar to artesunate (19.3 vs. 20.6 days). These fractions significantly modulated expression of inflammatory cytokines in Pf-antigen stimulated RAW cells. The findings of the study confirm the antimalarial potential of C. reflexa. Exploration of phyto-molecules in GCMS fingerprints of active fractions is warranted for possible identification of lead anti-malarial phyto-drugs.
对几乎所有正在使用的抗疟药物产生耐药性，使得开发新的抗疟化学治疗药物成为必要。在这方面，具有民间传说声誉的传统药用植物是药物发现的支柱。在印度奥里萨邦，菟葵传统上用于治疗疟疾，我们旨在通过实验验证其抗疟潜力。对菟葵的不同溶剂提取物或来自有前景的溶剂提取物的柱分离组分进行了针对恶性疟原虫Pf3D7菌株的体外抗疟原虫活性评估。对有效组分进一步评估其对不同耐药菌株的寄生虫生长抑制作用。通过体外细胞毒性测定这些组分的安全性，并通过抑制寄生虫血症和提高实验小鼠的存活率来评估治疗效果。此外，在Pf抗原刺激的RAW细胞中研究了它们的免疫调节作用。测定了活性组分的GCMS指纹图谱。对体外抗疟活性最高（IC = 14.48μg/ml）的甲醇提取物进行柱分离，得到11个组分，其中3个（F2、F3和F4）对各种恶性疟原虫菌株的抗疟IC范围为≤10至2.2μg/ml，且未表现出体外细胞毒性。F4在体内显示出最高的寄生虫抑制作用，平均存活时间与青蒿琥酯相似（19.3天对20.6天）。这些组分在Pf抗原刺激的RAW细胞中显著调节炎症细胞因子的表达。该研究结果证实了菟葵的抗疟潜力。有必要对活性组分的GCMS指纹图谱中的植物分子进行探索，以可能鉴定出潜在的抗疟植物药物。
