Central Institute of Medicinal and Aromatic Plants, P.O. CIMAP, Kukrail Picnic Spot Road, Lucknow-226 015, India.
Med Res Rev. 2010 Jul;30(4):603-45. doi: 10.1002/med.20170.
Mycobacterium tuberculosis is the most lethal pathogen causing tuberculosis in human. After the discovery of antitubercular drugs pyrazinamide, rifampicin, isoniazid, streptomycin, and ethambutol (PRISE), the disease was controlled for a limited period. However, over the course of their usage, the pathogen acquired resistance and evolved into multi-drug resistant, single-drug resistant, and extensive drug resistant forms. A good number of plant secondary metabolites are reported to have antitubercular activity comparable to the existing antitubercular drugs or sometimes even better in potency. A well-defined strategy is required to exploit these phytomolecules as antitubercular drugs. This review gives concise up-to-date information regarding the chemistry and pharmacology of plant-based leads and some insight into their structure-activity relationship.
结核分枝杆菌是导致人类结核病的最致命病原体。在发现抗结核药物吡嗪酰胺、利福平、异烟肼、链霉素和乙胺丁醇（PRISE）后，这种疾病在有限的时间内得到了控制。然而，在它们的使用过程中，病原体产生了耐药性，演变成了耐多药、单药耐药和广泛耐药的形式。有大量的植物次生代谢产物被报道具有与现有抗结核药物相当的抗结核活性，有时甚至在效力上更好。需要制定明确的策略来利用这些植物分子作为抗结核药物。本综述提供了关于基于植物的先导化合物的化学和药理学的简明最新信息，并对它们的结构-活性关系进行了一些探讨。
