Division of Microbiology and NCDs, ICMR-Regional Medical Research Centre, Bhubaneswar, India.
Central Research Laboratory, Institute of Medical Sciences and SUM Hospital, Siksha 'O' Anusandhan Deemed to be University, Bhubaneswar, India.
Chem Biol Drug Des. 2020 Aug;96(2):714-730. doi: 10.1111/cbdd.13685. Epub 2020 May 14.
Mycobacterium tuberculosis (Mtb) causes one of the most grievous pandemic infectious diseases, tuberculosis (TB), with long-term morbidity and high mortality. The emergence of drug-resistant Mtb strains, and the co-infection with human immunodeficiency virus, challenges the current WHO-TB stewardship programs. The first-line anti-TB drugs, isoniazid (INH) and rifampicin (RIF), have become extensively obsolete in TB control from chromosomal mutations during the last decades. However, based on clinical trial statistics, the production of well-tolerated anti-TB drug(s) is miserably low. Alternately, semi-synthesis or structural modifications of first-line obsolete antitubercular drugs remain as the versatile approach for getting some potential medicines. The use of any suitable phytochemicals with INH in a hybrid formulation could be an ideal approach for the development of potent anti-TB drug(s). The primary objective of this review was to highlight and analyze available INH-phytochemical hybrid research works. The utilization of phytochemicals through chemical conjugation is a new trend toward the development of safer/non-toxic anti-TB drugs.
结核分枝杆菌（Mtb）引起了最严重的流行传染病之一，结核病（TB），其长期发病率和高死亡率。耐药结核分枝杆菌菌株的出现，以及与人类免疫缺陷病毒的合并感染，对当前世卫组织的结核病管理方案提出了挑战。一线抗结核药物异烟肼（INH）和利福平（RIF）在过去几十年中由于染色体突变而在结核病控制中广泛失效。然而，根据临床试验统计数据，生产耐受性良好的抗结核药物的数量少得可怜。另外，对一线过时抗结核药物进行半合成或结构修饰仍然是获得一些潜在药物的通用方法。在混合制剂中使用任何合适的 INH 与植物化学物质的组合可能是开发有效抗结核药物的理想方法。本综述的主要目的是强调和分析现有的 INH-植物化学物质混合研究工作。通过化学偶联利用植物化学物质是开发更安全/无毒抗结核药物的新趋势。
