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Deep learning-based discovery of compounds for blood pressure lowering effects.
Sci Rep
January 2025
School of Pharmacy, Guilin Medical University, Guilin, 541199, China.
The hypotensive side effects caused by drugs during their use have been a vexing issue. Recent studies have found that deep learning can effectively predict the biological activity of compounds by mining patterns and rules in the data, providing a potential solution for identifying drug side effects. In this study, we established a deep learning-based predictive model, utilizing a data set comprised of compounds known to either elevate or lower blood pressure.
View Article and Find Full Text PDFGuanethidine Enhances the Antibacterial Activity of Rifampicin Against Multidrug-Resistant Bacteria.
Microorganisms
October 2024
Institute of Animal Husbandry and Veterinary Medicine, Jilin Academy of Agricultural Science, Kemao Street No.186, Gongzhuling 136100, China.
The escalating global threat of antibiotic resistance necessitates innovative strategies, such as the combination of antibiotics with adjuvants. Monotherapy with rifampicin is more likely to induce resistance in pathogens compared to other antibiotics. Herein, we found that the antihypertensive drug guanethidine enhanced the activity of rifampicin against certain clinically resistant Gram-negative bacteria, resulting in a reduction of up to 128-fold in the minimum inhibitory concentration.
View Article and Find Full Text PDFGuanethidine Restores Tetracycline Sensitivity in Multidrug-Resistant Carrying Gene.
Antibiotics (Basel)
October 2024
College of Animal Science and Technology, Jilin Agricultural University, Xincheng Street No. 2888, Changchun 130118, China.
The worrying issue of antibiotic resistance in pathogenic bacteria is aggravated by the scarcity of novel therapeutic agents. Antibiotic adjuvants offer a promising solution due to their cost-effectiveness and high efficacy in addressing this issue, such as the β-lactamase inhibitor sulbactam (a β-lactam adjuvant) and the dihydrofolate reductase inhibitor trimethoprim (a sulfonamide adjuvant). This study aimed to discover potential adjuvants for tetracyclines from a list of previously approved drugs to restore susceptibility to carrying the gene.
View Article and Find Full Text PDFStress-induced impairment of parasympathetic NO-mediated inhibition of sympathetic vasoconstriction in submucosal arteriole of rat rectum.
Pflugers Arch
October 2024
Department of Cell Physiology, Nagoya City University Graduate School of Medical Sciences, 1, Kawasumi, Mizuho-Cho, Mizuho-Ku, Nagoya, 467-8601, Japan.
In the gastrointestinal tract, nitrergic inhibition of the arteriolar contractility has not been demonstrated. Here, we explored whether neurally-released nitric oxide (NO) inhibits sympathetic vasoconstrictions in the rat rectal arterioles. Changes in sympathetic vasoconstrictions and their nitrergic modulation in rats exposed to water avoidance stress (WAS, 10 days, 1 h per day) were also examined.
View Article and Find Full Text PDFRole of Phenylethanolamine-N-methyltransferase on Nicotine-Induced Vasodilation in Rat Cerebral Arteries.
Microcirculation
July 2024
Division of Urology, Department of Surgery, Taipei Tzu Chi Hospital, New Taipei, Taiwan.
Objective: The sympathetic-parasympathetic (or axo-axonal) interaction mechanism mediated that neurogenic relaxation, which was dependent on norepinephrine (NE) releases from sympathetic nerve terminal and acts on β-adrenoceptor of parasympathetic nerve terminal, has been reported. As NE is a weak β-adrenoceptor agonist, there is a possibility that synaptic NE is converted to epinephrine by phenylethanolamine-N-methyltransferase (PNMT) and then acts on the β-adrenoceptors to induce neurogenic vasodilation.
Methods: Blood vessel myography technique was used to measure relaxation and contraction responses of isolated basilar arterial rings of rats.
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