Inhibitory effects of different antioxidants on hyaluronan depolymerization.

Hyaluronan (HA) was depolymerized by hydroxyl radicals generated from hydrogen peroxide and cupric ions. Inhibition of HA degradation by four well-known antioxidants was investigated, as HA can scavenge reactive oxygen species (ROS). Change in hyaluronan molecular weight was observed by size-exclusion chromatography.

Effects of ischemia-reperfusion on the absorption and esterase metabolism of diltiazem in rat intestine.

Intestinal ischemia-reperfusion (I/R) is a serious clinical condition that triggers a complex inflammatory response. Inflammatory processes affect some enzymatic systems related to intestinal drug metabolism and bioavailability. Diltiazem (DTZ) is a calcium channel blocker, which is extensively metabolised in the intestine by esterases and different CYP450 isoforms.

Interaction of enrofloxacin with breast cancer resistance protein (BCRP/ABCG2): influence of flavonoids and role in milk secretion in sheep.

The ATP-binding cassette (ABC) transporter breast cancer resistance protein (BCRP)/ABCG2 is a high-capacity efflux transporter with wide substrate specificity located in apical membranes of epithelia, which is involved in drug availability. BCRP is responsible for the active secretion of clinically and toxicologically important substrates to milk. The present study shows BCRP expression in sheep and cow by immunoblotting with MAb (BXP-53).

Role of ABC transporters in veterinary drug research and parasite resistance.

A considerable body of research has been carried out in order to throw light on the pharmacological and toxicological impact of ATP-binding cassette (ABC) drug efflux transporters such as P-glycoprotein and Breast Cancer Resistance Protein (BCRP/ABCG2/MXR). Most studies focus on their role in rendering cancer cells resistant to anticancer drugs. Drug transporters are expressed in many tissues and they are strongly involved in the oral bioavailability, and the hepatobiliary, direct intestinal and renal excretion of many drugs.

Breast cancer resistance protein (BCRP/ABCG2) transports fluoroquinolone antibiotics and affects their oral availability, pharmacokinetics, and milk secretion.

The breast cancer resistance protein (BCRP/ABCG2) is an ATP-binding cassette drug efflux transporter that extrudes xenotoxins from cells in intestine, liver, mammary gland, and other organs, affecting the pharmacological and toxicological behavior of many compounds, including their secretion into the milk. The purpose of this study was to determine whether three widely used fluoroquinolone antibiotics (ciprofloxacin, ofloxacin, and norfloxacin) are substrates of Bcrp1/BCRP and to investigate the possible role of this transporter in the in vivo pharmacokinetic profile of these compounds and their secretion into the milk. Using polarized cell lines, we found that ciprofloxacin, ofloxacin, and norfloxacin are transported by mouse Bcrp1 and human BCRP.

Transport of anthelmintic benzimidazole drugs by breast cancer resistance protein (BCRP/ABCG2).

Methylcarbamate benzimidazoles [albendazole (ABZ), fenbendazole (FBZ), and their respective sulfoxide derivatives, albendazole sulfoxide (ABZSO) and oxfendazole (OXF)] are therapeutically important anthelmintic agents with low bioavailability. We studied their in vitro interaction with the apical ATP-binding cassette (ABC) drug efflux transporters, breast cancer resistance protein (BCRP/ABCG2), P-glycoprotein (ABCB1), and MRP2 (ABCC2) using MDCKII cells transduced with human MDR1, MRP2, and BCRP, and murine Bcrp1 cDNAs. These ABC drug efflux transporters extrude a wide range of xenotoxins from cells in intestine, liver, and other organs, thus affecting the bioavailability of many compounds.

Ginseng increases intestinal elimination of albendazole sulfoxide in the rat.

Herbal products show potential drug interactions, some of them with adverse effects. The main aim of this work was to study the effect of Panax ginseng on the intestinal elimination of the benzimidazole derivative albendazole sulfoxide (ABZSO). An upper small intestine segment was isolated and perfused in situ with saline, while ABZSO solution (10 mg/kg i.

Intestinal elimination of albendazole sulfoxide: pharmacokinetic effects of inhibitors.

Albendazole (ABZ) is an anthelmintic drug widely used in human and veterinary medicine. Intestinal and hepatic ABZ metabolism leads to albendazole sulfoxide (ABZSO), the active metabolite. This work examines the mechanism involved in intestinal elimination of ABZSO and their pharmacokinetic consequences in rat and sheep.