Black ginger extract and its active compound, 5,7-dimethoxyflavone, increase intestinal drug absorption via efflux drug transporter inhibitions.

Black ginger is used as an herbal medicine for self-care and health promotion. Black ginger extract has been shown to alter the function of transporters in several cell types. This study demonstrates the interaction between the extract and 5,7-dimethoxyflavone (DMF) on drug efflux mediated by breast cancer resistance proteins (BCRP) and P-glycoprotein (P-gp) in Caco-2 cells and heterologous cell systems [Madin-Darby canine kidney type II (MDCKII) stably transfected with human BCRP (MDCKII/BCRP) or human P-gp (MDCKII/P-gp)].

Germacrone Reduces Cisplatin-Induced Toxicity of Renal Proximal Tubular Cells via Inhibition of Organic Cation Transporter.

Cisplatin is a widely used chemotherapy for solid tumors; however, its benefits are limited by serious nephrotoxicity, particularly in proximal tubular cells. The present study investigated the renoprotective effect and mechanisms of germacrone, a bioactive terpenoid compound found in Curcuma species on cisplatin-induced toxicity of renal cells. Germacrone (50 and 100 µM) attenuated apoptosis of human renal proximal tubular cells, RPTEC/TERT1 following treatment with 50 µM cisplatin and for 48 h.

Formulation and evaluation of gels containing coconut kernel extract for topical application.

The biological activity of coconut ( L.) extracts from its kernels and various parts was reported by many previous studies, it is therefore believable that the extracts of its kernels might show some activities in topical formulations. Among several kernel extracts, the TC06 extract prepared by soaking the steamed coconut kernels in hot water showed the highest total phenolic content (6.

Fenofibrate down-regulates renal OCT2-mediated organic cation transport via PPARα-independent pathways.

Fibrate drugs, the peroxisome proliferator-activated receptor alpha (PPARα) agonists, are widely prescribed for the treatment of hyperlipidemia. The present study examined the effect of fibrate drugs on renal OCT2 activity in a heterologous cell system [Chinese hamster ovary (CHO-K1) cells stably transfected with rabbit (rb) OCT2], LLC-PK1, and intact mouse renal cortical slices. We found that both in the CHO-K1 cells expressing rbOCT2 and in LLC-PK1 cells, fenofibrate significantly inhibited [³H]-MPP⁺ uptake whereas clofibrate and WY14643 had no effect.

Role of estrogen in renal handling of organic cation, tetraethylammonium: in vivo and in vitro studies.

This study examined the effect of estrogen (17beta-estradiol) on renal handling of organic cation, tetraethylammonium (TEA), both in vivo and in vitro. Clearance of TEA in ovariectomized (OVX) mice was increased by 38% above intact animals, which was able to be returned to control level by estrogen supplementation. The mechanism of this effect was examined in isolated mouse renal proximal tubules (mRPT), showing that [(3)H]-TEA uptake was higher in OVX mice than control, and estrogen supplementation returned uptake to normal level.

Regulatory role of testosterone in organic cation transport: in vivo and in vitro studies.

The renal proximal tubule (RPT) plays a crucial role in organic cation (OC) secretion and has a major impact on pharmacokinetics of OC drugs. Secretory transport is vectorial. Thus, it involves transporters located at both basolateral and apical membranes.