Background: Cytochrome b 5 reductase 3 (CYB5R3) regulates nitric oxide (NO) diffusion in the artery wall. Results: Novel CYB5R3 small molecule inhibitors were discovered that increase NO bioavailability. Conclusion: A potent new CYB5R3 inhibitor improves vascular function. Significance: These data provide a platform for further drug development and new tools for understanding CYB5R3 function.

Ten new polyhydroxyolean-12-ene pentacyclic triterpenoidal saponins, named rogchaponins 1-10, were isolated from the methanolic extract of the roots of Camellia sinensis by a series of chromatographic methods (silica gel flash column and C18 MPLC followed by C18 HPLC). Their structures were established by 1D and 2D-NMR techniques along with IR and HR-TOF-MS. Rogchaponins R4 ( 4) and R5 (5) showed inhibitory activities against yeast alcohol dehydrogenase (ADH) with IC (50) values of 16.1 ± 3.2 and 15.4 ± 3.3 µM, respectively. A 4-methylpyrazole positive control exhibited an IC (50) of 2750 ± 50 µM. However, the saponins showed no inhibitory activity against yeast aldehyde dehydrogenase (ALDH).

Other bioactive products U 1300Gamnamoside, a Phenylpropanoid Glycoside from Persimmon Leaves (Diospyros kaki) with an Inhibitory Effect Against an Alcohol Metabolizing Enzyme. -From the aqueous methanol extract of the title leaves, gamnamoside (I) is isolated together with osmanthuside and (-)-catechin. All compounds show good inhibitory activity against alcohol dehydrogenase. -(VARUGHESE, T.; RAHAMAN, M.; KIM, N.