title: Low antiplasmodial activity of alkaloids and amides from the stem bark of Zanthoxylum rubescens (Rutaceae).
abstract: The stem bark of Zanthoxylum rubescens (syn. Fagara rubescens) is used for treating fevers associated with malaria in the Ivory Coast. Three alkaloids: N-nornitidine, 7,9-dimethoxy-2,3-methylenedioxybenzophenanthridine, and bis[6-5,6-dihydrochelerythrinyl)] ether; and two amides: zanthomamide and lemairamide, were isolated from the stem bark of this plant. These compounds were screened in vitro against the chloroquine-sensitive 3D7 strain and the chloroquine-resistant FCM29 strain of P. falciparum. N-nornitidine was found to be inactive. 7,9-dimethoxy-2,3-methylenedioxybenzophenanthridine, lemairamide and zanthomamide showed weak activity with average IC50 values ranging from 45.6 microM to 149.9 microM. Bis[6-15,6-dihydrochelerythrinyl)] ether was the most active of the tested compounds with mean IC50s of 14.9 +/- 1.4 microM in FCM29 strain and 15.3 +/- 3.4 microM in 3D7 strain (approximately 58 to approximately 1130 times less active than chloroquine respectively). The anti-Plasmodium activities of the tested alkaloids of Z. rubescens were low; and do not encourage the use of this plant as antimalarial.
authors.affiliation: Malariology Department, Institut Pasteur de Côte d'Ivoire, 01 BP 490 Abidjan 01, Ivory Coast.
authors.forename: L
authors.initials: L
authors.lastname: Penali
authors.forename: D A
authors.initials: DA
authors.lastname: Mulholland
authors.forename: K D
authors.initials: KD
authors.lastname: Tano
authors.forename: P K
authors.initials: PK
authors.lastname: Cheplogoi
authors.forename: M
authors.initials: M
authors.lastname: Randrianarivelojosia
mesh_terms: D000470:Alkaloids / Q000302:isolation & purification / Q000627:therapeutic use; D000577:Amides / Q000302:isolation & purification / Q000627:therapeutic use; D000818:Animals; D000962:Antimalarials / Q000627:therapeutic use*; D002738:Chloroquine / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D006801:Humans; D020128:Inhibitory Concentration 50; D016778:Malaria, Falciparum / Q000188:drug therapy*; D010936:Plant Extracts / Q000627:therapeutic use*; D010963:Plasmodium falciparum / Q000187:drug effects*; D016896:Treatment Outcome; D032106:Zanthoxylum / Q000737:chemistry*
chemical_list: D000470:Alkaloids; D000577:Amides; D000962:Antimalarials; D010936:Plant Extracts; D002738:Chloroquine