Screening of commonly prescribed drugs for effects on the CAT1-mediated transport of L-arginine and arginine derivatives.

The cationic amino acid transporter 1 (CAT1/SLC7A1) plays a key role in the cellular uptake or export of L-arginine and some of its derivatives. This study investigated the effect of 113 chemically diverse and commonly used drugs (at 20 and 200 µM) on the CAT1-mediated cellular uptake of L-arginine, L-homoarginine, and asymmetric dimethylarginine (ADMA). Twenty-three (20%) of the tested substances showed weak inhibitory or stimulatory effects, but only verapamil showed consistent inhibitory effects on CAT1-mediated transport of all tested substrates.

Transport of L-Arginine Related Cardiovascular Risk Markers.

L-arginine and its derivatives, asymmetric and symmetric dimethylarginine (ADMA and SDMA) and L-homoarginine, have emerged as cardiovascular biomarkers linked to cardiovascular outcomes and various metabolic and functional pathways such as NO-mediated endothelial function. Cellular uptake and efflux of L-arginine and its derivatives are facilitated by transport proteins. In this respect the cationic amino acid transporters CAT1 and CAT2 (SLC7A1 and SLC7A2) and the system y+L amino acid transporters (SLC7A6 and SLC7A7) have been most extensively investigated, so far, but the number of transporters shown to mediate the transport of L-arginine and its derivatives is constantly increasing. In the present review we assess the growing body of evidence regarding the function, expression, and clinical relevance of these transporters and their possible relation to cardiovascular diseases.

Inhibitory effect of koji Aspergillus terreus on alpha-glucosidase activity and postprandial hyperglycemia.

The compounds that could inhibit the activity of a-glucosidase are potentially used for antidiabetic by suppressing postprandial hyperglycemia. This research aimed to investigate the hypoglycemic activity in A. terreus koji extracted by ethyl acetate. The extracts was dissolved in methanol: water (1:4), followed by fractionations with n-hexane, methylene chloride and ethyl acetate. Each fraction was assayed for its activity against a-glucosidase. The active fraction was purified by column chromatography using silica gel and resin as adsorbent. The kopi extract showed potential as alpha-glucosidase inhibition with IC50 <10 microg mL(-1) and showed combination of non-competitive and uncompetitive inhibition mode against a-glucosidase. Ethyl acetate fraction showed potential as inhibitor alpha-glucosidase with IC50 = 8.6 microg mL(-1). In animal experiment, active fraction (F10-4) of ethyl acetate fraction suppressed the increase of postprandial blood glucosidase level compare to the control. Thus it showed potential as alpha-glucosidase inhibitor and demonstrated depressed postprandial blood glucose level and may have potential use in the management of type 2 diabetes.