The purpose of the present study was to investigate the role of P-glycoprotein (P-gp) in drug disposition in skin. The distribution of P-gp substrates (rhodamine 123 and itraconazole) to the skin after administration from the epidermal side was lower in P-gp gene knockout (mdr1a/1b(-/-)) mice than that in wild-type mice. Coadministration of propranolol, a P-gp inhibitor, decreased the distribut...

Although Edgeworthia gardneri (Wall.) Meisn and its main component tiliroside (TIL) show good bioactivity, intestinal absorption data supporting low bioavailability have not been reported.The evaluation results of three models in vitro vivo indicated that the Ussing chamber model were basically consistent with experiments. It was thus applied to investigate characteristics TIL across various re...

Development of effective therapeutic strategies to eliminate cancer stem-like cells (CSCs), which play a major role in drug resistance and disease recurrence, is critical to improve cancer treatment outcomes. The current investigation was undertaken to examine the effectiveness of the combination treatment of Hsp90 inhibitor and SIRT1 inhibitor in inhibiting the growth of chemo-resistant stem-l...

Recently, sandwich-cultured (SC) rat hepatocytes have been used as an in vitro model to assess biliary excretion of drugs and xenobiotics. The purpose of the present study was to validate the use of SC rat hepatocytes for the in vitro assessment of P-glycoprotein (P-gp)-mediated biliary drug excretion. The specific and fluorescent P-gp substrate rhodamine 123 (Rh123) and the P-gp substrate digo...

OBJECTIVES The aim of this study was to compare outcomes in patients receiving consistent unfractionated heparin (UFH)/enoxaparin (ENOX) therapy and in those switched at randomization to bivalirudin monotherapy. BACKGROUND Crossover between UFH and ENOX has been associated with increased adverse outcomes in patients with acute coronary syndromes. The ACUITY (Acute Catheterization and Urgent I...

Background: Multidrug resistance (MDR) is known to defeat most chemotherapies as one of the main anticancer strategies. The role of overexpression/overactivation of ABC transporters, especially P-glycoprotein (P-gp), in the development of chemotherapy has long been demonstrated. Salinispora is a marine actinomycete genus known for the production of novel bioactive metabolites. Methods: In this...

P-glycoprotein (P-gp) is a 170 kDa transmembrane protein involved in the outward transport of many structurally unrelated substrates. P-gp activation/induction may function as an antidotal pathway to prevent the cytotoxicity of these substrates. In the present study we aimed at testing rifampicin (Rif) and three newly synthesized Rif derivatives (a mono-methoxylated derivative, MeORif, a perace...

ATP-binding cassette (ABC) proteins include the best known mediators of resistance to anticancer drugs. In particular, ABCB1 [MDR1/P-glycoprotein (P-gp)] extrudes many types of drugs from cancer cells, thereby conferring resistance to those agents. Attempts to overcome P-gp-mediated drug resistance using specific inhibitors of P-gp has had limited success and has faced many therapeutic challeng...

PurposeWith the expansion of donor pool through Hepatitis C viremic donors (HCV+), use DAA agents for treatment and prophylaxis has expanded in cardiothoracic transplant (CTT). Azole antifungal (AAF) is common CTT to prevent systemic fungal infections, several drug interactions (DDI) such as PGP inhibition. Glecaprevir/pibrentasvir (GP) a agent used HCV+ donors, utilizing pathway. While availab...