title: Labdane diterpenoids from Leonotis leonurus.
abstract: Three known (leoleorins A-C) and eight hitherto unknown (leoleorins D-J and 16-epi-leoleorin F) labdane diterpenoids, were isolated from leaves of Leonotis leonurus. The absolute configurations of leoleorins A and D were established by X-ray crystallographic analyses. In a competitive binding assay, all isolated compounds showed inhibition in excess of 50% at various CNS receptors. Leoleorin C showed moderate binding affinity (Ki=2.9 μM) for the Sigma 1 receptor.
authors.affiliation: Department of Pharmacognosy, School of Pharmacy, University of Mississippi, University, MS 38677-1848, USA.
authors.forename: Hankui
authors.initials: H
authors.lastname: Wu
authors.forename: Jun
authors.initials: J
authors.lastname: Li
authors.forename: Frank R
authors.initials: FR
authors.lastname: Fronczek
authors.forename: Daneel
authors.initials: D
authors.lastname: Ferreira
authors.forename: Charles L
authors.initials: CL
authors.lastname: Burandt
authors.forename: Vincent
authors.initials: V
authors.lastname: Setola
authors.forename: Bryan L
authors.initials: BL
authors.lastname: Roth
authors.forename: Jordan K
authors.initials: JK
authors.lastname: Zjawiony
mesh_terms: D018360:Crystallography, X-Ray; D004224:Diterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D019686:Lamiaceae / Q000737:chemistry*; D008958:Models, Molecular; D008968:Molecular Conformation; D018515:Plant Leaves / Q000737:chemistry; D011950:Receptors, Cholinergic / Q000378:metabolism; D017447:Receptors, Dopamine D1 / Q000037:antagonists & inhibitors; D011969:Receptors, Histamine H1 / Q000378:metabolism; D011985:Receptors, Serotonin / Q000378:metabolism; D017480:Receptors, sigma / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
chemical_list: D004224:Diterpenes; D011950:Receptors, Cholinergic; D017447:Receptors, Dopamine D1; D011969:Receptors, Histamine H1; D011985:Receptors, Serotonin; D017480:Receptors, sigma; C433017:labdane