Mabhiza Donald, Chitemerere Tariro, Mukanganyama Stanley
School of Pharmacy, College of Health Sciences, University of Zimbabwe, Mt. Pleasant, Harare, Zimbabwe.
Department of Biochemistry, University of Zimbabwe, Mt. Pleasant, Harare, Zimbabwe.
Int J Med Chem. 2016;2016:6304163. doi: 10.1155/2016/6304163. Epub 2016 Jan 20.
The development of new antibiotics from new chemical entities is becoming more and more expensive, time-consuming, and compounded by emerging strains that are drug resistant. Alkaloids are plant secondary metabolites which have been shown to have potent pharmacological activities. The effect of alkaloids from Callistemon citrinus and Vernonia adoensis leaves on bacterial growth and efflux pump activity was evaluated on Staphylococcus aureus and Pseudomonas aeruginosa. At a concentration of 1.67 mg/mL, the alkaloids inhibited bacterial growth with comparable effects to ampicillin, a standard antibiotic. The alkaloids from C. citrinus were the most potent against S. aureus with an MIC of 0.0025 mg/mL and MBC of 0.835 mg/mL. It was shown that effects on P. aeruginosa by both plant alkaloids were bacteriostatic. P. aeruginosa was most susceptible to drug efflux pump inhibition by C. citrinus alkaloids which caused an accumulation of Rhodamine 6G of 121% compared to the control. Thus, C. citrinus alkaloids showed antibacterial activity as well as inhibiting ATP-dependent transport of compounds across the cell membrane. These alkaloids may serve as potential courses of compounds that can act as lead compounds for the development of plant-based antibacterials and/or their adjunct compounds.
从新化学实体开发新型抗生素正变得越来越昂贵、耗时,而且还受到新出现的耐药菌株的影响。生物碱是植物次生代谢产物,已被证明具有强大的药理活性。本研究评估了柠檬桉叶和非洲斑鸠菊叶中的生物碱对金黄色葡萄球菌和铜绿假单胞菌生长及外排泵活性的影响。在浓度为1.67mg/mL时,这些生物碱对细菌生长的抑制作用与标准抗生素氨苄西林相当。柠檬桉叶中的生物碱对金黄色葡萄球菌的活性最强,其最低抑菌浓度(MIC)为0.0025mg/mL,最低杀菌浓度(MBC)为0.835mg/mL。结果表明,两种植物生物碱对铜绿假单胞菌的作用均为抑菌。铜绿假单胞菌对柠檬桉叶生物碱引起的药物外排泵抑制最为敏感,与对照组相比,罗丹明6G的积累量达到121%。因此,柠檬桉叶生物碱表现出抗菌活性,同时还能抑制化合物通过细胞膜的ATP依赖性转运。这些生物碱可能作为潜在的化合物来源,可作为开发植物源抗菌药物及其辅助化合物的先导化合物。