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1.
J Chem Educ ; 98(10): 3371-3378, 2021 Oct 12.
Artigo em Inglês | MEDLINE | ID: mdl-37556285

RESUMO

This communication was to share the efforts made in developing the fully online courses in medicinal chemistry during the educational disruption due to the coronavirus disease 2019 (COVID-19) pandemic. In the academic year 2020, the online course was implemented for the first time at the Faculty of Pharmacy, Silpakorn University, Thailand. Various online teaching strategies were integrated, raising the question of whether the developed online courses would deliver similar learning outcomes to the traditional classroom. At the end of each semester, the teaching assessment report was conducted and evaluated in 4 parts: part 1, evaluation of lecturer; part 2, student's self-evaluation; part 3, learning outcome development after studying the course; part 4, appropriateness of class environment and equipment. Overall, student responses toward parts 1-3 in the online class were as satisfactory as those in the previous on-site class. Lower scores toward part 4 were observed in the online class. In addition, student performance in terms of grade distributions between the on-site and online classes was different. On-site students earned the highest proportion of A grades, whereas online students earned a higher proportion of B+'s to F's. While the pandemic persists and the need for online courses remains, we hope that this communication will provide some educational insight and strategies to help in the ongoing efforts to adapt and establish more successful online courses.

2.
Fitoterapia ; 93: 194-200, 2014 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-24370662

RESUMO

Four new sesquiterpene lactones, 8α-(2'Z-tigloyloxy)-hirsutinolide (1), 8α-(2'Z-tigloyloxy)-hirsutinolide-13-O-acetate (2), 8α-(4-hydroxytigloyloxy)-hirsutinolide (3), and 8α-hydroxy-13-O-tigloyl-hirsutinolide (4), along with seven known derivatives (5-11), three norisoprenoids (12-14), a flavonoid (15), and a linoleic acid derivative (16), were isolated from the chloroform partition of a methanol extract from the combined leaves and stems of Vernonia cinerea. Their structures were established by 1D and 2D NMR, UV, and MS analyses. Compounds 1-16 were evaluated for their inhibitory effects against the viability of U251MG glioblastoma and MDA-MB-231 breast cancer cells that harbour aberrantly-active STAT3, compared to normal NIH3T3 mouse fibroblasts that show no evidence of activated STAT3. Among the isolates, compounds 2 and 7 inhibited the aberrant STAT3 activity in glioblastoma or breast cancer cells. Further, compounds 7 and 8 inhibited viability of all three cell lines, compounds 2, 4, and 9 predominantly inhibited the viability of the U251MG glioblastoma cell line.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Lactonas/isolamento & purificação , Fator de Transcrição STAT3/antagonistas & inibidores , Sesquiterpenos/isolamento & purificação , Vernonia/química , Antineoplásicos Fitogênicos/química , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Lactonas/química , Estrutura Molecular , Sesquiterpenos/química
3.
Bioorg Med Chem Lett ; 22(17): 5559-62, 2012 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-22850207

RESUMO

Bioassay-guided fractionation of the hexane extract from the flowers of Vernonia cinerea (Asteraceae) led to the isolation of a new sesquiterpene lactone, 8α-hydroxyhirsutinolide (2), and a new naturally occurring derivative, 8α-hydroxyl-1-O-methylhirsutinolide (3), along with seven known compounds (1 and 4-9). The structures of the new compounds were determined by 1D and 2D NMR experiments and by comparison with the structure of compound 1, whose relative stereochemistry was determined by X-ray analysis. The isolated compounds were evaluated for their cancer chemopreventive potential based on their ability to inhibit nitric oxide (NO) production and tumor necrosis factor alpha (TNF-α)-induced NF-κB activity. Compounds 1, 2, 4, 5, and 9 inhibited TNF-α-induced NF-κB activity with IC(50) values of 3.1, 1.9, 0.6, 5.2, and 1.6 µM, respectively; compounds 4 and 6-9 exhibited significant NO inhibitory activity with IC(50) values of 2.0, 1.5, 1.2, 2.7, and 2.4 µM, respectively.


Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Lactonas/química , Lactonas/farmacologia , Sesquiterpenos/química , Sesquiterpenos/farmacologia , Vernonia/química , Animais , Anti-Inflamatórios/isolamento & purificação , Linhagem Celular , Cristalografia por Raios X , Flores/química , Humanos , Lactonas/isolamento & purificação , Espectroscopia de Ressonância Magnética , Camundongos , Modelos Moleculares , NF-kappa B/imunologia , Neoplasias/prevenção & controle , Óxido Nítrico/antagonistas & inibidores , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Sesquiterpenos/isolamento & purificação , Fator de Necrose Tumoral alfa/imunologia
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