Lall N, Meyer J J Marion, Wang Y, Bapela N B, van Rensburg C E J, Fourie B, Franzblau S G
a Department of Botany, University of Pretoria, Pretoria, South Africa.
b Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, Chicago, Illinois, USA.
Pharm Biol. 2005;43(4):353-357. doi: 10.1080/13880200590951829.
Naphthoquinones and triterpenes isolated from the roots of Euclea natalensis. A.DC (Ebenaceae) were evaluated for their inhibitory activity against Mycobacterium tuberculosis.. Crude extract, diospyrin and 7-methyljuglone isolated from the plant, exhibited minimum inhibitory concentrations of 8.0, 8.0, and 0.5 µg ml, respectively, against M. tuberculosis. H37 Rv (ATCC 27294), a drug-sensitive strain. Minimum inhibitory concentrations (MICs) of 7- methyljuglone against a panel of clinical pan-sensitive and drug-resistant strains of M. tuberculosis. ranged from 0.32 to 1.25 µg/ml. The concentration of 7-methyljuglone that effected a 90% reduction of growth of M. tuberculosis. Erdman within J774.1 macrophages was 0.57 µg/ml. The superior intracellular and extracellular inhibition of M. tuberculosis. by 7-methyljuglone relative to that of the antituberculosis drugs streptomycin and ethambutol suggests that this compound be considered as a lead for further investigations.
从纳塔尔核果木(Euclea natalensis. A.DC,柿科)根部分离得到的萘醌和三萜类化合物,针对其对结核分枝杆菌的抑制活性进行了评估。从该植物中分离得到的粗提物、柿菌素和7-甲基胡桃醌,对结核分枝杆菌H37 Rv(ATCC 27294)这一药物敏感菌株的最低抑菌浓度分别为8.0、8.0和0.5 µg/ml。7-甲基胡桃醌对一组临床全敏感和耐药结核分枝杆菌菌株的最低抑菌浓度(MICs)范围为0.32至1.25 µg/ml。在J774.1巨噬细胞内,使结核分枝杆菌埃尔德曼菌株生长减少90%的7-甲基胡桃醌浓度为0.57 µg/ml。相对于抗结核药物链霉素和乙胺丁醇,7-甲基胡桃醌对结核分枝杆菌具有更强的细胞内和细胞外抑制作用,这表明该化合物可被视为进一步研究的先导物。