Synergism between pyronaridine and retinol in Plasmodium falciparum in vitro

Summary Pyronaridine, a naphthyridine derivative and Mannich base, is a highly active blood schizontocide and currently being explored as partner in artemisinin-based combination therapy (ACT). In this study, carried out 2008 in Mae Sot, Thailand, the activity of pyronaridine was found to be comprom...

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Published in:Wiener Klinische Wochenschrift 2009-10, Vol.121 (Suppl 3), p.32, Article 32
Main Authors: Proell, Pippa, Congpuong, Kanungnit, Reinthaler, Franz F., Wernsdorfer, Gunther, Wiedermann, Ursula, Wernsdorfer, Walther H.
Format: Article
Language:English
Subjects:
Antimalarials - administration & dosage
Cell Survival - drug effects
Cells, Cultured
Dose-Response Relationship, Drug
Drug Synergism
Endocrinology
Gastroenterology
Humans
Internal Medicine
Lethal Dose 50
Medicine
Medicine & Public Health
Naphthyridines - administration & dosage
Original Article
Plasmodium falciparum - drug effects
Plasmodium falciparum - physiology
Pneumology/Respiratory System
Vitamin A - administration & dosage
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Summary:Summary Pyronaridine, a naphthyridine derivative and Mannich base, is a highly active blood schizontocide and currently being explored as partner in artemisinin-based combination therapy (ACT). In this study, carried out 2008 in Mae Sot, Thailand, the activity of pyronaridine was found to be compromised, obviously as the result of mono-therapy in an adjacent area. The pyronaridine sensitivity and the interaction between pyronaridine and retinol at concentrations corresponding to the 50 th , 65 th and 80 th percentile of the physiological retinol levels in healthy adults were assessed in 38 fresh isolates of P. falciparum . The mean IC50, IC90 and IC99 values for pyronaridine were 12.7, 201.4 and 3084.2 nM, those for pyronaridine + retinol "low" 1.2, 14.0 and 102.6 nM, those for pyronaridine + retinol "medium" 0.6, 7.4 and 54.8 nM, and those for pyronaridine + retinol "high" 0.9, 8.2 and 47.8 nM. There was significant evidence of strong synergism between pyronaridine and retinol against P. falciparum .
ISSN:0043-5325
1613-7671
DOI:10.1007/s00508-009-1232-5