title: Antifungal and cytotoxic activity of withanolides from Acnistus arborescens.
abstract: Three compounds were isolated from Acnistus arborescens, a tree commonly used in South and Central America in traditional medicine against several infectious diseases, some of which are caused by fungi. Bioassay-guided fractionation of a MeOH extract of leaves, based on its anti-Pneumocystis carinii activity, led to the isolation of compounds 1-3. Mono- and bidimensional NMR analyses enabled identification of two new withanolides, (20R,22R)-5beta,6beta-epoxy-4beta,12beta,20-trihydroxy-1-oxowith-2-en-24-enolide (1) and (20R,22R)-16beta-acetoxy-3beta,4beta;5beta,6beta-diepoxy-12beta,20-dihydroxy-1-oxowith-24-enolide (2), and withanolide D (3). Antifungal activity on 13 fungi responsible for human infections (five dermatophytes, one nondermatophyte mold, six yeasts, and Pneumocystis carinii) was examined. Cytotoxicity of these compounds was also evaluated in vitro.
authors.affiliation: Laboratoire de Pharmacognosie, EA4481 (GRIIOT), Faculte des Sciences Pharmaceutiques et Biologiques, Universite Lille Nord de France (Lille 2), Lille Cedex, France. vincent.roumy@univ-lille2.fr
authors.forename: Vincent
authors.initials: V
authors.lastname: Roumy
authors.forename: Murielle
authors.initials: M
authors.lastname: Biabiany
authors.forename: Thierry
authors.initials: T
authors.lastname: Hennebelle
authors.forename: El Moukhtar
authors.initials: el M
authors.lastname: Aliouat
authors.forename: Muriel
authors.initials: M
authors.lastname: Pottier
authors.forename: Henry
authors.initials: H
authors.lastname: Joseph
authors.forename: Sami
authors.initials: S
authors.lastname: Joha
authors.forename: Bruno
authors.initials: B
authors.lastname: Quesnel
authors.forename: Racha
authors.initials: R
authors.lastname: Alkhatib
authors.forename: Sevser
authors.initials: S
authors.lastname: Sahpaz
authors.forename: François
authors.initials: F
authors.lastname: Bailleul
mesh_terms: D000935:Antifungal Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D001549:Benzamides; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D019430:Guadeloupe; D006801:Humans; D000068877:Imatinib Mesylate; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010879:Piperazines / Q000494:pharmacology; D018515:Plant Leaves / Q000737:chemistry; D010946:Plants, Medicinal / Q000737:chemistry*; D045363:Pneumocystis carinii / Q000187:drug effects; D011743:Pyrimidines / Q000494:pharmacology; D019657:Solanaceae / Q000737:chemistry; D013237:Stereoisomerism; D054358:Withanolides / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*
chemical_list: C551610:(20R,22R)-16beta-acetoxy-3beta,4beta;5beta,6beta-diepoxy-12beta,20-dihydroxy-1-oxowith-24-enolide; C551611:(20R,22R)-5beta,6beta-epoxy-4beta,12beta,20-trihydroxy-1-oxowith-2-en-24-enolide; D000935:Antifungal Agents; D001549:Benzamides; D010879:Piperazines; D011743:Pyrimidines; D054358:Withanolides; C010376:withanolide D; D000068877:Imatinib Mesylate