Version 1
: Received: 1 July 2024 / Approved: 1 July 2024 / Online: 1 July 2024 (15:02:24 CEST)
How to cite:
Im, J. W.; Lim, J. H.; Stonik, V. A.; Kwak, J.-Y.; Jin, S.; Son, M.; Bae, H.-R. Stichoposide C and Rhizochalin as Potential Aquaglyceroporin Modulators. Preprints2024, 2024070071. https://doi.org/10.20944/preprints202407.0071.v1
Im, J. W.; Lim, J. H.; Stonik, V. A.; Kwak, J.-Y.; Jin, S.; Son, M.; Bae, H.-R. Stichoposide C and Rhizochalin as Potential Aquaglyceroporin Modulators. Preprints 2024, 2024070071. https://doi.org/10.20944/preprints202407.0071.v1
Im, J. W.; Lim, J. H.; Stonik, V. A.; Kwak, J.-Y.; Jin, S.; Son, M.; Bae, H.-R. Stichoposide C and Rhizochalin as Potential Aquaglyceroporin Modulators. Preprints2024, 2024070071. https://doi.org/10.20944/preprints202407.0071.v1
APA Style
Im, J. W., Lim, J. H., Stonik, V. A., Kwak, J. Y., Jin, S., Son, M., & Bae, H. R. (2024). Stichoposide C and Rhizochalin as Potential Aquaglyceroporin Modulators. Preprints. https://doi.org/10.20944/preprints202407.0071.v1
Chicago/Turabian Style
Im, J. W., Minkook Son and Hae-Rahn Bae. 2024 "Stichoposide C and Rhizochalin as Potential Aquaglyceroporin Modulators" Preprints. https://doi.org/10.20944/preprints202407.0071.v1
Abstract
Aquaporins (AQPs) are a family of integral membrane proteins that selectively transport water and glycerol across the cell membrane. Because AQPs are involved in a wide range of physiological functions and pathophysiological conditions, AQP-based therapeutics may have broad potential for clinical utility, including disorders of water and energy balance. However, AQP modulators have not yet been developed as suitable candidates for clinical applications. In this study, to identify potential modulators of AQPs, we screened 32 natural products by measuring the water and glycerol permeability of mouse erythrocyte membranes using a stopped-flow light scattering method. None of the tested natural compounds substantially affected osmotic water permeability. However, several compounds considerably affected glycerol permeability. Stichoposide C increased the glycerol permeability of mouse erythrocyte membranes, whereas rhizochalin decreased it at nanomolar concentrations. Immunohistochemistry revealed that AQP7 was the main aquaglyceroporin in mouse erythrocyte membranes. We further verified the effects of stichoposide C and rhizochalin on aquaglyceroporins using human AQP3 expressing keratinocyte cells. Stichoposide C, but not stichoposide D, increased AQP3-mediated transepithelial glycerol transport, whereas the peracetyl aglycon of rhizochalin was the most potent inhibitor of glycerol transport among the tested rhizochalin derivatives. Collectively, stichoposide C and the peracetyl aglycon of rhizochalin might function as modulators of AQP3 and AQP7, and suggest the possibility of these natural products as potential drug candidates for aquaglyceroporin modulators
Copyright:
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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