کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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3360307 | 1591842 | 2009 | 6 صفحه PDF | دانلود رایگان |

Previous studies have demonstrated that diospyrin (1), a quinonoid plant product, can inhibit the growth of Leishmania donovani parasites. Here, several derivatives of 1 were evaluated by the MTT assay and it was observed that the ethanolamine analogue (10) exhibited maximum cytotoxicity [50% inhibitory concentration (IC50) = 2.9 μM] against L. donovani promastigotes. Subsequently, the mode of cell death in promastigotes was investigated through externalisation of membrane-associated phosphatidylserine, mitochondrial membrane depolarisation, DNA laddering and in situ labelling of DNA fragmentation by terminal deoxyribonucleotidyl transferase-mediated dUTP nick-end labelling (TUNEL) methods. Whilst both 1 and 10 were found to induce apoptosis-like death in promastigotes, the effect of 10 was evidently stronger even at a lower concentration. Hence, the ethanolamine derivative (10) of diospyrin (1) may be a prospective ‘lead’ for the development of novel cytotoxic agents inducing apoptosis in L. donovani parasites.
Journal: International Journal of Antimicrobial Agents - Volume 34, Issue 6, December 2009, Pages 596–601