Previously obtained Pic-BZA is a potent anticonvulsant with low neurotoxicity, but its half-time of action is only about 15 min. In search for equally effective anticonvulsants but with a longer time of action fourteen Pic-BZA analogs were obtained. The compounds were evaluated in the Anticonvulsant Screening Project (ASP) of Antiepileptic Drug Development Program (ADDP) of NIH. Picolinic acid 2-fluorobenzylamide (Pic-2-F-BZA, 7) appeared to be the most effective compound of the series.
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http://dx.doi.org/10.2174/0929866054696046 | DOI Listing |
Front Immunol
December 2024
Department of Thoracic Surgery, Affiliated Hospital of Southwest Medical University, Luzhou, China.
Background: Lichen planus (LP), an autoimmune disorder, remains incompletely understood in terms of its etiological mechanisms. This study aims to elucidate causal relationships among immune cell populations, plasma metabolites, and lichen planus using Mendelian randomization (MR) techniques.
Methods: Employing a two-sample, two-step MR approach, with single nucleotide polymorphisms (SNP) serving as genetic instruments for both exposures and mediators, this study minimizes biases from confounding and reverse causality.
J Appl Microbiol
December 2024
Instituto de Química, Departamento de Productos Naturales. Universidad Nacional Autónoma de México (UNAM). Ciudad Universitaria, Delegación Coyoacán, Ciudad de México, 04510.
Aims: This study aimed to assess the mode of action of fusaric and 9,10-dehydrofusaric acids on cell respiration by measuring the hyphal oxygen consumption rate, and the effects on cell membrane integrity by determining the electrical conductivity of the mycelium.
Methods And Results: Bioactivity-directed fractionation of the active culture medium and mycelium organic extracts from the Fusarium lactis strain SME13-2 isolated from Sapium macrocarpum, led to the isolation of two known alkylpicolinic acid derivatives: fusaric acid and 9,10-dehydrofusaric acid, along with the known polyketide bikaverin. Fusaric acid and 9,10-dehydrofusaric acid exhibited antioomycete and antifungal activities, significantly inhibiting the radial growth of Phytophthora capsici, Pythium aphanidermatum, Alternaria alternata and Fusarium oxysporum.
Nutrients
November 2024
Department of Experimental Medicine, University "Sapienza", 00161 Rome, Italy.
Background: The aim of the present study was to evaluate the effectiveness and safety of a nutraceutical combination given to insulin-resistant overweight patients with altered lipid profiles. To this end, an observational study was designed in which 74 individuals (50 females and 24 males) underwent an observational period of 3 months.
Methods: During this time, a specific nutraceutical combination containing myo-inositol, glycine, , α-lipoic acid, phlorizin, zinc, vitamin B, and chromium picolinate was administered.
Dalton Trans
December 2024
Institute of Nuclear and New Energy Technology, Tsinghua University, 100084, Beijing, China.
The extraction and complexation of trivalent americium (Am) and lanthanides (Ln) using an asymmetric picolinic acid-derived tridentate N,O-hybrid ligand, 6-(dioctylcarbamoyl)picolinic acid (DOAPA), have been studied through both experimental and theoretical methods. DOAPA exhibits effective and fast extraction of Am(III) and Ln(III). The extraction is driven by favorable enthalpy change.
View Article and Find Full Text PDFJ Pharm Biomed Anal
December 2024
School of Medicine and Pharmacy, Ocean University of China, Qingdao, Shandong 266003, PR China; Laboratory for Marine Drugs and Bioproducts, Qingdao Marine Science and Technology Center, Qingdao, Shandong 266237, PR China.
A small molecule, (S)-ethyl 1-(3-(4-chlorophenoxy)-2-hydroxypropyl)-3-(4-methoxyphenyl)-1H-pyrazole-5-carboxylate (SEC), has been reported to be capable of suppressing metastasis of prostate cancer (PCa) cells. In this study, SEC was used to study the metabolic responses of PCa cell lines (LNCaP, PC3, and DU145) with different metastatic potential and the alterations of mTOR, p-mTOR, AMPK, and p-AMPK levels, when the PCa cells were inhibited. The ultra-high performance liquid chromatography-high resolution mass spectrometry (UHPLC-HRMS)-based analysis showed that SEC induced the decreases of intracellular metabolites including glutamic acid, glutamine, and histidine (LNCaP); creatinine, citric acid/isocitric acid, and aspartic acid (PC3); and spermidine, S-hydroxymethylglutathione, LPE (20:3), and palmitic amide (DU145), and the increases of intracellular LPC (18:0) (LNCaP); tyrosine, pyroglutamic acid/pyrroline hydroxycarboxylic acid (PC3); and tyrosine, phenylalanine, phenylacetylglycine, spermine, histidine, and choline (DU145).
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