title: Simple and rapid physico-chemical methods to examine action of antimalarial drugs with hemin: its application to Artemisia annua constituents.
abstract: Malaria is a major health problem in many countries and according to an estimate of the WHO, more than 500 million infections occur per year. Artemisinin, a sesquiterpene from Artemisia annua L., has received considerable attention as a promising and potent antimalarial drug for its stage speciticity, its rather low toxicity, effectiveness against drug-resistant Plasmodium species and activity against cerebral malaria. From recent studies it seems that hemin is primarily involved in the antimalarial activity of the constituents of Artemisia annua L. Thus, the interaction of a compound with hemin may represent a crucial screening test to define its efficacy. In this study the interaction between artemisinin and hemin was investigated by UltraViolet/Visible (UV/Vis) spectrophotometry and High Performance Liquid Chromatography/Diode Array Detector/Mass Spectrometry (HPLC/DAD/MS). In addition, some flavonols isolated from Artemisia annua L. were also tested to investigate their possible role in the interaction between artemisinin and hemin. These two simple physico-chemical methods can be useful as rapid and widespread screening methods for the search of other alkylating antimalarial constituents from natural sources or for the evaluation of the activity of semisynthetic analogues of artemisinin.
authors.affiliation: Department of Pharmaceutical Sciences, University of Florence, Firenze, Italy. ar.bilia@unifi.it
authors.forename: Anna Rita
authors.initials: AR
authors.lastname: Bilia
authors.forename: Diamanto
authors.initials: D
authors.lastname: Lazari
authors.forename: Luigi
authors.initials: L
authors.lastname: Messori
authors.forename: Vania
authors.initials: V
authors.lastname: Taglioli
authors.forename: Claudia
authors.initials: C
authors.lastname: Temperini
authors.forename: Franco Francesco
authors.initials: FF
authors.lastname: Vincieri
mesh_terms: D000962:Antimalarials / Q000737:chemistry*; D019306:Artemisia / Q000737:chemistry*; D037621:Artemisinins; D002627:Chemistry, Physical / Q000379:methods; D002851:Chromatography, High Pressure Liquid; D004347:Drug Interactions; D004365:Drugs, Chinese Herbal; D005419:Flavonoids / Q000302:isolation & purification; D006427:Hemin / Q000737:chemistry*; D010946:Plants, Medicinal / Q000737:chemistry*; D012717:Sesquiterpenes / Q000737:chemistry*; D013056:Spectrophotometry, Ultraviolet
chemical_list: D000962:Antimalarials; D037621:Artemisinins; D004365:Drugs, Chinese Herbal; D005419:Flavonoids; D012717:Sesquiterpenes; D006427:Hemin; C031327:artemisinin