Facultad de Ciencias Químicas, Universidad Autónoma de Nuevo León, Monterrey, Nuevo León, Mexico.
Eur J Med Chem. 2012 Mar;49:1-23. doi: 10.1016/j.ejmech.2011.12.029. Epub 2012 Jan 9.
Currently, one third of the world's population is infected with Mycobacterium tuberculosis and 8.9-9.9 million new and relapse cases of tuberculosis are reported every year. The emergence of new cases, the increased incidence of multi-drug resistant strains of M. tuberculosis, and the adverse effects of first- and second-line antituberculosis drugs have led to renewed research interest in natural products in the hope of discovering new antitubercular leads. Interestingly, hundreds of natural products, possessing novel, uncommon, and known structural architectures, have been reported to exhibit activity towards non-resistant and multi-drug resistant strains of M. tuberculosis. The present review covers literature published during the last five years about those naturally occurring compounds with reported growth inhibitory activity in vitro towards sensitive and resistant M. tuberculosis strains. Compounds with antitubercular properties at minimal inhibitory concentrations (MICs) of less than 50 μg/mL or 60 μM were selected and grouped according to their source of origin (plants, bacteria, fungi, marine organisms, etc) and chemical type (terpenes, steroids, alkaloids, flavonoids, poliketides, peptides, etc). In some cases, the selection covers those structurally relevant natural products with low bioactivity (MICs of ≤128 μg/mL), and also those semisynthetic derivatives with remarkable antitubercular activity (MICs of ≤10 μg/mL). Additionally, this review includes a special section for those natural products that specifically target genes or enzymes of M. tuberculosis.
目前,全球有三分之一的人口感染结核分枝杆菌,每年报告的新发病例和复发病例有 890 万至 990 万例。新发病例的出现、结核分枝杆菌耐多药株的发病率上升,以及一线和二线抗结核药物的不良反应,都促使人们重新对天然产物产生研究兴趣,希望能发现新的抗结核先导化合物。有趣的是,已有数百种天然产物被报道具有针对非耐药和耐多药结核分枝杆菌株的活性,这些天然产物具有新颖、不常见和已知的结构架构。本文综述了过去五年间报道的具有体外抑制敏感和耐药结核分枝杆菌生长活性的天然产物的文献。选择最低抑菌浓度(MIC)低于 50μg/ml 或 60μM 的具有抗结核特性的化合物,并根据其来源(植物、细菌、真菌、海洋生物等)和化学类型(萜类、甾体、生物碱、类黄酮、多酮、肽等)进行分组。在某些情况下,选择范围包括那些结构相关但生物活性较低(MIC 为≤128μg/ml)的天然产物,以及那些具有显著抗结核活性的半合成衍生物(MIC 为≤10μg/ml)。此外,本文还包括了针对结核分枝杆菌特定基因或酶的天然产物的专门部分。