Search

Volatile components of Porana volubilis Burm. f. flowers from Bangkok were extracted by using steam distillation and solvent extraction prior to analysis by gas chromatography-mass spectrometry (GC-MS) and their antiinflammatory activity was assessed in vitro and in silico. Forty-two compounds were identified with essential oil. The key volatile components were detected in the hexane-scented extract. Twenty-one compounds were detected with major volatile components of octacosanaol, dodecanoic acid, nonacosane, n-hexadecanoic acid, and tetratriacontane for ethanolic scented extract. The essential oil and extract were evaluated for their in vitro anti-inflammatory effect by protein denaturation assay. The essential oil showed the most potent anti-denaturation activity with IC50 values of 537.6 g/mL. The primary components of essential oil were submitted ta molecular docking research based on their anti-inflammatory effect. The obtained results revealed that the main components were found as the crucial interactions for binding in the bovine serum albumin (BSA) binding site. The results obtained demonstrated the essential oil of P. volubilis is the potential source for the anti-inflammatory agent. [ABSTRACT FROM AUTHOR]

A simple and low cost method for rapid detection of Pb 2+ was developed in this study using a simple fluorescent probe, biotin-4-fluorescein. The presence of Pb 2+ induced the color change of fluorescein from yellow to pink which can be detected visually by naked eyes. The color change of biotin-4-fluorescein was not observed while testing with other metal ions, such as Fe 3+ , Cu 2+ , Ca 2+ , Co 2+ and Cd 2+ , indicating the selectivity of fluorescein derivative with Pb 2+ . Moreover, the color change was observed at pH above 7.0, and the pink color got more intense when increasing pH. Adding EDTA, a chelating reagent, into the solution of biotin-4-fluorescein/Pb 2+ resulted to the rebound of the color to the original color of free biotin-4-fluorescein. The fluorescence spectra of fluorescein decreased with increasing Pb 2+ concentration, and the quenching was enhanced at higher pH. The association constant (K a ) of 2.00 × 10 4  M -1 was calculated from the fluorescence spectra with the limit of detection (LOD) and the limit of quantitation (LOQ) of 1.38 × 10 -5  M (2.86 ppm) and 4.61 × 10 -5  M (9.55 ppm), respectively. Job's plot analysis indicated 2:1 ratio of binding interaction. Pb 2+ in untreated wastewater was quantified for 24.99 ppm using this method. This quick analysis can be beneficial for the application of lead detection in real sample solutions, such as wastewater from industrial factories., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier B.V. All rights reserved.)

In vitro screening for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of the Artocarpus lakoocha root-bark extracts revealed interesting results. Bioassay-guided fractionation resulted in the isolation of two new (1 and 2) and six known 2-arylbenzofurans 3-8, along with one stilbenoid 9 and one flavonoid 10. The structures of the isolated compounds were elucidated by UV, IR, 1D- and 2D-NMR and MS spectroscopic data analysis. Compounds 4, 6 and 7 exhibited more potent AChE inhibitory activity (IC 50  = 0.87-1.10 μM) than the reference drug, galantamine. Compounds 4, 8 and 9 displayed greater BChE inhibition than the standard drug. The preferential inhibition of BChE over AChE indicated that 4 also showed a promising dual AChE and BChE inhibitor. The synthetic mono-methylated analogs 4a-c and 6a-b were found to be good BChE inhibitors with IC 50 values ranging between 0.31 and 1.11 μM. Based on the docking studies, compounds 4 and 6 are well-fitted in the catalytic triad of AChE. Compounds 4 and 6 showed different binding orientations on BChE, and the most potent BChE inhibitor 4 occupied dual binding to both CAS and PAS more efficiently., (Copyright © 2017 Elsevier Masson SAS. All rights reserved.)

Aims: Previous investigation showed that polyphenols abundantly found in many plants could inhibit Cl(-) secretion. The present study was aimed to investigate the effect of phenol containing xanthone derivatives on cAMP-activated intestinal Cl(-) secretion and evaluate potential benefits of these compounds in the treatment of cholera., Main Methods: Four hydroxy xanthones were synthesized via oxidative coupling reaction of the corresponding ortho-hydroxybenzoic acids and hydroxyphenols. Short-circuit current and apical Cl(-) current measurements across monolayers of human intestinal epithelial (T84) cell and Fisher rat thyroid cells transfected with human CFTR (FRT-hCFTR cell) were performed to determine the effect of hydroxyxanthones on cAMP-activated Cl(-) secretion. Intracellular cAMP was measured by immunoassay methods. Anti-diarrheal efficacy was evaluated using closed loop model of cholera., Key Findings: Among the tested xanthones, 1,3,6-trihydroxyxanthone (THX-001) was found to be the most potent derivative in the inhibition of cAMP-activated Cl(-) secretion across T84 cell monolayers (IC(50)~100μM). Electrophysiological analysis of T84 cells and FRT-hCFTR cells revealed that THX-001 targeted two distinct cAMP-activated Cl(-) channels in the apical membrane of T84 cells, namely, CFTR and inward rectifying Cl(-) channel (IRC). In contrast, THX-001 had no effect on intracellular cAMP levels in these cells. Importantly, THX-001 completely abolished cholera toxin-induced Cl(-) secretion across T84 cell monolayers and significantly inhibited cholera toxin-induced intestinal fluid secretion in mouse closed loop models., Significance: This study revealed that hydroxyxanthone represents another chemical class of polyphenolic compounds that may hold promise as anti-secretory therapy for cholera., (Copyright © 2012 Elsevier Inc. All rights reserved.)