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1.
Molecules ; 26(9)2021 Apr 26.
Artigo em Inglês | MEDLINE | ID: mdl-33926133

RESUMO

Combretum quadrangulare Kurz is widely used in folk medicine in Eastern Asia and is associated with various ethnopharmacological properties including hepatoprotective, antipyretic, analgesic, antidysenteric, and anthelmintic activities. Previous phytochemical investigations reported the presence of numerous triterpenes (mostly cycloartanes, ursanes, lupanes, and oleananes) along with dozens of flavonoids. However, the extracts of C. quadrangulare and isolated flavonoids have not been evaluated for their alpha-glucosidase inhibition. In the frame of our efforts dedicated to the chemical investigation of Vietnamese medicinal plants and their biological activities, a phytochemical study of the MeOH extract of the leaves of C. quadrangulare using bioactive guided isolation was undertaken. In this paper, the isolation and structure elucidation of twelve known compounds, 5-hydroxy-3,7,4'-trimethoxyflavone (1), ayanin (2), kumatakenin (3), rhamnocitrin (4), ombuin (5), myricetin-3,7,3',5'-tetramethyl ether (6), gardenin D (7), luteolin (12), apigenin (13), mearnsetin (14), isoorientin (15), and vitexin (16) were reported. Bromination was applied to compounds 2 and 3 to provide four new synthetic analogues 8-11. All isolated and synthesized compounds were evaluated for alpha-glucosidase inhibition and antibacterial activity. Compounds 4 and 5 showed moderate antibacterial activity against methicillin-resistant Staphylococcus aureus while others were inactive. All compounds failed to reveal any activity toward extended spectrum beta-lactamase-producing Escherichia coli. Compounds 2, 4, 6-9, and 11-14 showed good alpha-glucosidase inhibition with IC50 values in the range of 30.5-282.0 µM. The kinetic of enzyme inhibition showed that 8 and 11 were noncompetitive type inhibition against alpha-glucosidase. In silico molecular docking model indicated that compounds 8 and 11 were potential inhibitors against enzyme α-glucosidase.


Assuntos
Combretum/química , Flavonas/química , Flavonas/farmacologia , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Relação Dose-Resposta a Droga , Flavonas/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Ligação de Hidrogênio , Ligantes , Modelos Moleculares , Conformação Molecular , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Estrutura Molecular , Compostos Fitoquímicos/química , Extratos Vegetais/isolamento & purificação , Relação Estrutura-Atividade
2.
Chemosphere ; 307(Pt 1): 135707, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-35842046

RESUMO

Particulate-bound mercury (PBM) is a global environmental concern owing to its large dry deposition velocities and scavenging coefficients, both of which drive Hg into terrestrial and marine ecosystems. PBM observation studies have been widely conducted over East Asia, but comparable studies in Peninsular Southeast Asia (PSEA) remain scarce. This is the first study reporting PBM concentrations for Ho Chi Minh City (HCMC), the biggest metropolitan area in Vietnam. A total of 222 samples were collected in 2018 and contained an average PBM10 (particulate matter - PM with diameter ≤10 µm) concentration and Hg mass fraction (i.e. PBM/PM) of 67.3 ± 45.9 pg m-3 and 1.18 ± 1.12 µg g-1, respectively. Although PBM concentration was lower than those reported in Chinese megacities, the Hg mass fraction was similar to those in China, suggesting strong enrichment from anthropogenic Hg emissions in HCMC. Traffic-induced particulate emission and deposition processes were major factors governing PBM temporal variation at our site. In addition, the prevailing southwest monsoon winds brought air masses that passed through industrial areas and were associated with a higher Hg mass fraction. Statistically significant positive correlations (R2 = 0.11-0.52, p < 0.01) were observed for PBM with PM and the Hg mass fraction, indicating similar PM and Hg sources or oxidized Hg adsorption onto PM via gas-particle partitioning. Moreover, PCA results revealed a higher contribution of primary sources than secondary sources to PBM concentration variability in HCMC. A health risk assessment indicated that the PBM concentrations at HCMC posed minimal non-carcinogenic risks (HI < 1) for children and adults, but dermal contact may act as an important exposure route since lightweight clothing is common among residents. This PBM dataset over PSEA, a region with high atmospheric Hg emissions, provides a valuable resource for the Hg scientific community to improve our understanding of Hg biogeochemical cycle.


Assuntos
Poluentes Atmosféricos , Mercúrio , Poluentes Atmosféricos/análise , Sudeste Asiático , Criança , Poeira/análise , Ecossistema , Monitoramento Ambiental/métodos , Humanos , Mercúrio/análise , Material Particulado/análise , Medição de Risco , Estreptotricinas
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