Stichoposide C and Rhizochalin as Potential Aquaglyceroporin Modulators DOI Open Access
Ji Woo Im, Ju Hyun Lim, Valentin A. Stonik

и другие.

Опубликована: Июль 1, 2024

Aquaporins (AQPs) are a family of integral membrane proteins that selectively transport water and glycerol across the cell membrane. Because AQPs involved in wide range physiological functions pathophysiological conditions, AQP-based therapeutics may have broad potential for clinical utility, including disorders energy balance. However, AQP modulators not yet been developed as suitable candidates applications. In this study, to identify AQPs, we screened 32 natural products by measuring permeability mouse erythrocyte membranes using stopped-flow light scattering method. None tested compounds substantially affected osmotic permeability. several considerably Stichoposide C increased membranes, whereas rhizochalin decreased it at nanomolar concentrations. Immunohistochemistry revealed AQP7 was main aquaglyceroporin membranes. We further verified effects stichoposide on aquaglyceroporins human AQP3 expressing keratinocyte cells. C, but D, AQP3-mediated transepithelial transport, peracetyl aglycon most potent inhibitor among derivatives. Collectively, might function AQP7, suggest possibility these drug

Язык: Английский

Stichoposide C and Rhizochalin as Potential Aquaglyceroporin Modulators DOI Open Access
Ji Woo Im, Ju Hyun Lim, Valentin A. Stonik

и другие.

Опубликована: Июль 1, 2024

Aquaporins (AQPs) are a family of integral membrane proteins that selectively transport water and glycerol across the cell membrane. Because AQPs involved in wide range physiological functions pathophysiological conditions, AQP-based therapeutics may have broad potential for clinical utility, including disorders energy balance. However, AQP modulators not yet been developed as suitable candidates applications. In this study, to identify AQPs, we screened 32 natural products by measuring permeability mouse erythrocyte membranes using stopped-flow light scattering method. None tested compounds substantially affected osmotic permeability. several considerably Stichoposide C increased membranes, whereas rhizochalin decreased it at nanomolar concentrations. Immunohistochemistry revealed AQP7 was main aquaglyceroporin membranes. We further verified effects stichoposide on aquaglyceroporins human AQP3 expressing keratinocyte cells. C, but D, AQP3-mediated transepithelial transport, peracetyl aglycon most potent inhibitor among derivatives. Collectively, might function AQP7, suggest possibility these drug

Язык: Английский

Процитировано

1