传染病药物:针对Theileria annulata的替代化疗,用于治疗精神分裂期寄生虫
Sonam Kamble1,2, Sakshi Singh1,2, Akash Suresh1
1National Institute of Animal Biotechnology, Hyderabad, India.
Microbiology spectrum
|February 29, 2024
概括
药物耐药性需要热带病的新疗法. 这项研究选了针对Theileria annulata的表观遗传抑制剂,确定了SAHA,Trichostatin A和BVT-948作为新型抗theilerial药物开发的有希望的候选者.
科学领域:
- 兽医寄生虫学 兽医寄生虫学
- 药物发现 药物发现 药物发现
- 表观遗传学 在表观遗传学中,表观遗传学是指表观遗传学.
背景情况:
- 热带病是由Theileria annulata引起的,严重影响牛的健康和生产力.
- 由于新兴的药物耐药性,现有的抗theilerial治疗面临挑战.
- 表观遗传抑制剂为寄生虫感染提供了一种新的治疗策略.
研究的目的:
- 评估表观遗传抑制剂对Theileria annulata的抗寄生虫疗效.
- 识别具有潜在的新型化合物,作为治疗热带病的化疗剂.
- 探索已识别的活性化合物的作用机制和药物相似性.
主要方法:
- 对148种表观遗传抑制剂对T. annulata感染细胞的查.
- 确定50%的抑制度 (IC50) 和细胞毒性测定.
- 分子对接研究和in silico ADME/T预测.
主要成果:
- 27种化合物显示出初始的抗theilerial活性,其中7种具有高疗效 (SAHA,BVT-948,Trichostatin A,Methylstat,Plumbagin,Ryuvidine,TCE-5003).
- 活性化合物向人类酶,如HDAC,SET域和PRMT.
- 与Plumbagin,Methylstat和TCE-5003不同的是,SAHA,Trichostatin A和BVT-948在体中显示出有利的ADME/T概况.
结论:
- SAHA,Trichostatin A和BVT-948是开发新的抗theilerial药物的潜在化合物.
- 表观遗传抑制剂代表了对抗耐药Theileria寄生虫的有希望的途径.
- 需要进一步的研究来优化这些化合物在兽医中用于治疗.
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