Photoreactivity of biologically active compounds. VII. Interaction of antimalarial drugs with melanin in vitro as part of phototoxicity screening.
The drugs commonly used in the treatment of malaria are photochemically unstable. Several of these compounds accumulate in melanin-rich tissues and cause toxic reactions which may be light induced. As part of the screening of the photochemical properties and phototoxic capabilities of antimalarials, the in vitro interaction of eight antimalarials with melanin was studied. The dissociation constant for the drug-melanin complex and the relative number of binding sites on melanin were estimated for six of the drugs using a curve-fitting program. The reaction rate for the formation of the melanin-drug complex was determined, and the complexes were further characterized by zeta potential measurements.
Kristensen
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S
Department of Pharmaceutics, University of Oslo, Blindern, Norway.
Orsteen
A L
AL
Sande
S A
SA
Tønnesen
H H
HH
D000962:Antimalarials / Q000737:chemistry*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D007700:Kinetics; D008543:Melanins / Q000737:chemistry*; D015394:Molecular Structure; D017319:Photosensitizing Agents / Q000737:chemistry*; D013329:Structure-Activity Relationship
D000962:Antimalarials; D008543:Melanins; D017319:Photosensitizing Agents