1. Enantioselective actions of 4-amino-3-hydroxybutanoic acid and (3-amino-2-hydroxypropyl)methylphosphinic acid at recombinant GABA(C) receptors
Tina Hinton, Mary Chebib, Graham A R Johnston Bioorg Med Chem Lett. 2008 Jan 1;18(1):402-4. doi: 10.1016/j.bmcl.2007.10.019. Epub 2007 Oct 17.
The R- and S-enantiomers of 4-amino-3-hydroxybutanoic acid (GABOB) were full agonists at human recombinant rho1 GABA(C) receptors. Their enantioselectivity (R>S) matched that reported for their agonist actions at GABA(B) receptors, but was the opposite to that reported at GABA(A) receptors (S>R). The corresponding methylphosphinic acid analogues proved to be rho1 GABA(C) receptor antagonists with R(+)-CGP44533 being more potent than S(-)-CGP44532, thus showing the opposite enantioselectivity to the agonists R(-)- and S(+)-GABOB. These studies highlight the different stereochemical requirements for the hydroxy group in these analogues at GABA(A), GABA(B) and GABA(C) receptors.
2. Bis-Boric Acid-Mediated Regioselective Reductive Aminolysis of 3,4-Epoxy Alcohols
Wei Tang, Chuan Wang J Org Chem. 2022 Nov 18;87(22):15653-15660. doi: 10.1021/acs.joc.2c01878. Epub 2022 Nov 3.
Herein we report a bis-boric acid-mediated regioselective reductive aminolysis of 3,4-epoxy alcohols, providing new access to prepare amino diols in high diastereofidelity directly starting from nitroarenes. Notably, this step-economical process is enabled by the essential dual function of bis-boric acid, which is engaged initially in the 4,4'-bipyridine-catalyzed reduction of nitro compounds as the reductant and subsequently promotes the ring opening reaction of 3,4-epoxy alcohols with the in situ-generated anilines.
3. A Vegan Diet Is Associated with a Significant Reduction in Dietary Acid Load: Post Hoc Analysis of a Randomized Controlled Trial in Healthy Individuals
Alexander Müller, Amy Marisa Zimmermann-Klemd, Ann-Kathrin Lederer, Luciana Hannibal, Stefanie Kowarschik, Roman Huber, Maximilian Andreas Storz Int J Environ Res Public Health. 2021 Sep 23;18(19):9998. doi: 10.3390/ijerph18199998.
The composition of diet strongly affects acid-base homeostasis. Western diets abundant in acidogenic foods (meat and cheese) and deficient in alkalizing foods (fruits and vegetables) increase dietary acid load (DAL). A high DAL has been associated with numerous health repercussions, including cardiovascular disease and type-2-diabetes. Plant-based diets have been associated with a lower DAL; however, the number of trials exploring this association is limited. This randomized-controlled trial sought to examine whether an isocaloric vegan diet lowers DAL as compared to a meat-rich diet. Forty-five omnivorous individuals were randomly assigned to a vegan diet (n = 23) or a meat-rich diet (n = 22) for 4 weeks. DAL was determined using potential renal acid load (PRAL) and net endogenous acid production (NEAP) scores at baseline and after 3 and 4 weeks, respectively. After 3 weeks, median PRAL (-23.57 (23.87)) and mean NEAPR (12.85 ± 19.71) scores were significantly lower in the vegan group than in the meat-rich group (PRAL: 18.78 (21.04) and NEAPR: 60.93 ± 15.51, respectively). Effects were mediated by a lower phosphorus and protein intake in the vegan group. Our study suggests that a vegan diet is a potential means to reduce DAL, whereas a meat-rich diet substantially increases the DAL burden.
