The present study investigated the effects of equol on cardiovascular K+ channel currents. The cardiovascular K+ channel currents were determined in HEK 293 cells stably expressing cloned differential cardiovascular K+ channels with conventional whole-cell patch voltage-clamp technique. We found that equol inhibited hKv1.5 (IC50: 15.3 μM), hKv4.3 (IC50: 29.2 μM and 11.9 μM for hKv4.3 peak curre...

The present study aimed to investigate the antioxidant and antiradical activities of Wu Ling Shen, a popular medicinal fungus (Xylaria nigripes) used in traditional Chinese medicine preparations. Two different X. nigripes materials, the cultivated X. nigripes mycelia (XN) and a commercial X. nigripes product (XNP), were used to prepare the aqueous (XN-H vs. XNP-H) and ethanol (XN-E vs. XNP-E) e...

Drug repositioning or repurposing, i.e. identifying new indications for existing drugs, has gained increasing attention in the recent years. This approach enables the scientists to discover "new targets" for known drugs in a cost and time efficient manner. Glycation, the non-enzymatic reaction of sugars with proteins or nucleic acids to form early glycation (Amadori or fructosamine) products, i...

In order to determine the biochemical basis for the cytotoxicity of homofolates, poly-gamma-glutamyl derivatives of homofolate (HPteGlu) and tetrahydrohomofolate (H4HPteGlu) were synthesized and tested as inhibitors of glycinamide ribonucleotide formyltransferase (GARFT), aminoimidazolecarboxamide ribonucleotide formyltransferase (AICARFT), thymidylate synthase, and serine hydroxymethyltransfer...

The twigs of Morus alba L. were found to show strong tyrosinase inhibition activity, and the responsible active components in the extract were further investigated in this study. A flavone, named morusone (1), and sixteen known compounds 2-17 were isolated from M. alba twigs and their structures were identified by interpretation of the corresponding ESI-MS and NMR spectral data. In the tyrosina...

Four sesquiterpenes isolated from Jasonia glutinosa D.C. (Asteraceae), namely lucinone, glutinone, 5-epi-kutdtriol and kutdtriol, have been evaluated for their in vitro anti-inflammatory activity in cellular systems generating cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) metabolites. None of the compounds assayed had a significant effect on leukotriene C4 (LTC4)-release from calcium ionophor...

The present study evaluated the free radical scavenging capacity and antioxidant potential of different solvent fractions (Petroleum ether, Ethyl acetate, Butanol and Water) of methanolic extract of Cissus quadrangularis stem. Ethyl acetate fraction of Cissus quadrangularis stem possessed a high amount of total phenolic and flavonoid contents as compared to other solvent fractions. Also Ethyl a...

Two cyclic nucleotide phosphodiesterase (PDE) activities were identified in pig aortic endothelial cells, a cyclic GMP-stimulated PDE and a cyclic AMP PDE. Cyclic GMP-stimulated PDE had Km values of 367 microM for cyclic AMP and 24 microM for cyclic GMP, and low concentrations (1 microM) of cyclic GMP increased the affinity of the enzyme for cyclic AMP (Km = 13 microM) without changing the Vmax...

Ipomoea imperati (Convolvulaceae) lives on the sandy shores of the Brazilian coast and in other areas of the world. The anti-inflammatory activity of a methanol-water extract of the leaves of I. imperati was investigated in experimental models of acute and subchronic inflammation. Topical application of the extract (10 mg/ear) inhibited mouse ear edema induced by croton oil (89.0 +/- 1.3% by th...

The natural polyoxygenated steroids (20S)-20-hydroxycholestane-3,16-dione (1), (16S, 20S)16,20-dihydroxycholestan-3-one (2), (20S)-20-hydroxycholest-1-ene-3,16-dione (3) and (20S)-20hydroxycholest-4-ene-3,16-dione (4), isolated from the gorgonian, Leptogorgia sarmentosa and unnatural analogs (5) (6), (12) and (13) were synthesized from tigogenin. Antitumor activity against three tumor cell line...