Potent inhibition of human organic cation transporter 2 (hOCT2) by β-carboline alkaloids

Regulation of human organic cation transporter hOCT2 by PKA, PI3K, and calmodulin-dependent kinases.

Properties and regulation of the human organic cation (OC) transporter type 2 (hOCT2) expressed in HEK-293 cells were extensively characterized using the fluorescent OC 4-[4-(dimethylamino)styryl]-N-methylpyridinium (ASP(+)). ASP(+) uptake was electrogenic and inhibited by TPA(+) (EC(50) = 2.7 microM), tetraethylammonium (EC(50) = 35 microM), cimetidine (EC(50) = 36 microM), or quinine (EC(50) ...

Atenolol Renal Secretion Is Mediated by Human Organic Cation Transporter 2 (hOCT2) and Multidrug and Toxin Extrusion Proteins (hMATEs)

Interaction of Cisplatin with the human organic cation transporter 2.

PURPOSE Cisplatin is predominantly eliminated in the urine through active secretion. As the solute carrier organic cation transporter 2 (OCT2) is highly expressed in the basolateral membrane of proximal tubules, we determined its contribution to cisplatin transport and assessed the relation of variation in the gene encoding OCT2 (SLC22A2) with the disposition of cisplatin. EXPERIMENTAL DESIGN...

Three novel β-carboline alkaloids from Gelsemium elegans.

Three novel β-carboline alkaloids characterized with a unique degraded monoterpenoid moiety, gelebolines A-C (1-3), together with 11 known alkaloids of different types, were isolated from the roots of Gelsemium elegans. The structures of new alkaloids were established on the basis of analysis of spectroscopic data. It is the first example for report of β-carboline from genus Gelsemium (Loganiac...

Production of β-carboline alkaloids on co-culture of peganum harmala L

Introduction: peganum harmala L. (Zygophyllaceae) and varthemia persica DC (Compositeae) were used for co-culture studies. P.harmala was found to be one of the richest natural sources of β-carboline alkaloids. β-carboline alkaloids posses different neuropharmacologic activities including BDZ antagonism, MAOinhibitor and aminoreuptake inhibitor. The production of β-carboline alkaloids in cell ...