RESUMEN
Background: The rhizomes of Kaempferia parviflora (KP) have been widely used in Thai traditional medicine to treat several diseases such as hypertension. Recent studies have shown that the ethanolic extract of KP (KPE) exerts vasorelaxant effects in the rat aorta. However, the underlying mechanisms of these vascular responses remain unclear. Objectives: Investigate the mechanisms of KPE-induced vasorelaxation in the rat aorta. Methods: Aortic rings from male Wistar rats were precontracted with methoxamine. Changes in tension were measured using an isometric force transducer and recorded on the MacLab recording system. Vasorelaxation to KPE was examined in the presence of 10 μM indomethacin, 300 μM NG-nitro L-arginine methyl ester (L-NAME), 60 mM KCl, 5 mM tetraethylammonium chloride (TEA), 10 μM glibenclamide, 1 mM 4-aminopyridine (4-AP) or 30 μM barium chloride (BaCl2). The effects of KPE on vascular responses to carbachol, sodium nitroprusside, and CaCl2 were evaluated. Results: KPE (0.1-100 μg/mL) caused vasorelaxations, which were reduced with removal of the endothelium. In addition, indomethacin, L-NAME, and indomethacin plus L-NAME reduced KPE-induced vasorelaxation. Raising the extracellular KCl concentration to 60 mM, or pre-treatment with BaCl2, TEA, or glibenclamide reduced relaxant responses to KPE. Contractions to CaCl2 were inhibited after pre-incubation with KPE. Pre-treatment with KPE enhanced endothelium-dependent relaxations to carbachol, but not to sodium nitroprusside. Conclusion: KPE had a vasodilator effect in the rat isolated aortic rings. These effects involved endotheliumderived NO and prostanoids via a COX pathway. In addition, KPE-induced vasorelaxation was due to increasing K+ efflux probably through KCa, KIR and KATP channels. These provide pharmacological evidence for mechanism of KPE-induced vasorelaxation and support the traditional use of KPE as an antihypertensive agent.
RESUMEN
The in vitro antimalarial activities against Plasmodium falciparum K1 of four extracts from the stembark of Picrasma javanica B1; ie water, methanol, chloroform and hexane extracts were studied using a modification of the [3H]hypoxanthine incorporation method. It was found that the hexane extract showed in vitro antimalarial activity with IC50 of 3.3 microg/ml. The extract was further fractionated using quick column chromatography, resulting in ten fractions. Fraction V was the most effective against P. falciparum K1 with IC50 of 4.4 microg/ml. Further isolation of fraction V using a column chromatographic technique provided six fractions. According to 1H- and 13C-NMR spectra, it could be concluded that the major compound in fraction V-3 was beta-sitosterol. Unfortunately, the antimalarial activity of beta-sitosterol could not be determined because of its low solubility in DMSO. However, fractions V-2 and V-4 still showed in vitro antimalarial activities with IC50 of 2.8 and 3.4 microg/ml, respectively. The further fractionation of these two active fractions could lead to promising candidates as antimalarial agents.