کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
3394056 1221442 2009 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
In vitro antimalarial interactions between mefloquine and cytochrome P450 inhibitors
موضوعات مرتبط
علوم زیستی و بیوفناوری ایمنی شناسی و میکروب شناسی انگل شناسی
پیش نمایش صفحه اول مقاله
In vitro antimalarial interactions between mefloquine and cytochrome P450 inhibitors
چکیده انگلیسی

The treatment and control of malaria is becoming increasingly difficult due to resistance of Plasmodium falciparum strains resistance to commonly used antimalarials. Combination therapy is currently the strategy for combating multi-drug resistant falciparum malaria, through exploiting phamacodynamic synergistic effect and delaying the emergence of drug resistance. The objective of the present study was to investigate antimalarial activity of inhibitors of cytochrome P450 (CYP) enzyme including their interactions with the antimalarial mefloquine against chloroquine-resistant (K1) and chloroquine-sensitive (3D7) P. falciparum clones in vitro. Results showed IC50 (drug concentration which produces 50% schizont maturation inhibition) values [mean (range)] of mefloquine against K1 and 3D7 clones to be 8.6 (8.0–9.3) and 12.1 (10.5–13.8) nM, respectively. The corresponding values for the IC50 of quinidine were 32.2 (31.9–32.5) and 28.7 (28.4–29.0) nM, and for ketoconazole were 3.9 (3.7–4.1) and 4.8 (4.6–5.1) μM, respectively. Analysis of isobologram revealed a trend of decreasing of fraction IC50 (FIC), which indicates synergistics of the either quinidine or ketoconazole with mefloquine for both chloroquine-resistant and chloroquine-sensitive clones.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Acta Tropica - Volume 112, Issue 1, October 2009, Pages 12–15
نویسندگان
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