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2.
J Nat Prod ; 83(6): 1998-2003, 2020 06 26.
Artigo em Inglês | MEDLINE | ID: mdl-32489099

RESUMO

A new dihydrobenzofuran-phenyl acrylate hybrid, aspeterreurone A (1), was obtained from the culture of the deep-sea-derived fungus Aspergillus terreus CC-S06-18. The relative configuration of 1 was elucidated by HSQMBC NMR, calculated NMR chemical shifts coupled with a statistical procedure (DP4+), and the absolute configuration was established by ECD calculations. 1 exhibited cytotoxicities against the gastric cancer cell lines HGC27, MGC803, BGC823, and AGS, with minimal effects on normal gastric epithelial cell line GES-1. Further studies showed that 1 inhibited cell cycle progression and induced apoptosis of gastric cancer MGC803 cells in a concentration-dependent manner. Western blot analysis indicated that 1 inhibited the phosphorylation of STAT3, which might contribute to its cytotoxic activity.


Assuntos
Antibióticos Antineoplásicos/química , Antibióticos Antineoplásicos/farmacologia , Aspergillus/química , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Linhagem Celular , Linhagem Celular Tumoral , Relação Dose-Resposta a Droga , Células Epiteliais/efeitos dos fármacos , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Fosforilação , Fator de Transcrição STAT3/metabolismo , Água do Mar , Neoplasias Gástricas/tratamento farmacológico
3.
J Nat Prod ; 83(4): 1157-1166, 2020 04 24.
Artigo em Inglês | MEDLINE | ID: mdl-32193933

RESUMO

Eight new nitrogenated azaphilones (1-8) and two known compounds (chaetoviridin A and chaetoviridin E, 9, 10) were isolated from the culture of the deep-sea-derived fungus Chaetomium globosum MP4-S01-7. The absolute configurations of new compounds were elucidated by HSQC-HECADE NMR data, J-based configuration analysis, and modified Mosher's method and finally verified by comparison of recorded and computed NMR chemical shifts from quantum chemical calculations coupled with a statistical procedure (DP4+). All of the compounds were evaluated for their in vitro cytotoxicities against the gastric cancer cell lines MGC803 and AGS, and most of them showed significant inhibition on cancer cell viability at 10 µM. Among them, compounds 1, 2, and 5 exerted the most potent cytotoxic activities, with IC50 values less than 1 µM. Further studies showed that compound 2 inhibited cell cycle progression, and both compounds 1 and 2 induced apoptosis of gastric cancer cells in a concentration-dependent manner.


Assuntos
Antineoplásicos/farmacologia , Benzopiranos/toxicidade , Chaetomium/química , Pigmentos Biológicos/toxicidade , Antineoplásicos/química , Benzopiranos/química , Benzopiranos/farmacologia , Linhagem Celular Tumoral , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Pigmentos Biológicos/química , Pigmentos Biológicos/farmacologia
4.
Sheng Li Xue Bao ; 71(3): 388-394, 2019 Jun 25.
Artigo em Chinês | MEDLINE | ID: mdl-31218329

RESUMO

The aim of this study was to determine the effects of extremely low frequency electromagnetic field (ELF-EMF) on energy metabolism and oxidative stress in Caenorhabditis elegans (C. elegans). Worms in three adult stages (young adult stage, egg-laying stage and peak egg-laying stage) were investigated under 50 Hz, 3 mT ELF-EMF exposure. ATP levels, ATP synthase activity in vivo, reactive oxygen species (ROS) content, and changes of total antioxidant capacity (TAC) were detected, and worms' oxidative stress responses were also evaluated under ELF-EMF exposure. The results showed that ATP levels were significantly increased under this ELF-EMF exposure, and mitochondrial ATP synthase activity was upregulated simultaneously. In young adult stage, worms' ROS level was significantly elevated, together with upregulated TAC but with a decreased ROS-TAC score indicated by principal component analysis. ROS level and TAC of worms had no significant changes in egg-laying and peak egg-laying stages. Based on these results, we concluded that ELF-EMF can enhance worm energy metabolism and elicit oxidative stress, mainly manifesting as ATP and ROS level elevation together with ATP synthase upregulation and ROS-TAC score decrease in young adult C. elegans.


Assuntos
Caenorhabditis elegans/efeitos da radiação , Radiação Eletromagnética , Metabolismo Energético , Estresse Oxidativo , Trifosfato de Adenosina/metabolismo , Animais , ATPases Mitocondriais Próton-Translocadoras/metabolismo , Espécies Reativas de Oxigênio/análise
5.
3 Biotech ; 9(7): 286, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31245250

RESUMO

A high-salt-tolerant strain, Meyerozyma guilliermondii, has been isolated from activated sludge which has a great effect in the treatment of high-salt wastewater. To identify the salt tolerance mechanism of the strain, transcriptome sequencing and fluorescence quantitative PCR were used to analyse and compare the thallus, which were growing in the salt-free, low-salt (4%), and high-salt (16%) YPD media for 48 h, respectively, and then the change of intracellular and extracellular glycerol was determined. The results showed that 8220 unigenes were obtained from the sequencing data after de novo splicing, among which 6334 genes had annotation information in the SwissProt library. With salt-free as reference, there were 1135 unigenes that differentially expressed under low-salt stress and 1948 unigenes were differentially expressed under high-salt stress. With low salt as reference, 3056 unigenes were differentially expressed under high-salt stress. The fluorescence quantification results of the six candidate genes selected in this study were consistent with the transcriptome data. Under high-salt stress, the intracellular glycerol of M. guilliermondii reached a maximum value at about 10 min, then decreased quickly and tended to be stable. This study provided valuable data for the next study of salt tolerance of M. guilliermondii, and also contributed to the functional study of yeast salt tolerance genes.

6.
Chem Commun (Camb) ; 53(55): 7784-7787, 2017 Jul 06.
Artigo em Inglês | MEDLINE | ID: mdl-28650506

RESUMO

Dual C-H thiolation reactions using elemental sulphur remain a challenge. This communication discloses an oxidative radical dual sp2/sp3 C-H thiolation strategy for the coupling of imidazopyridines with ethers or alkanes using elemental sulphur.

7.
Chem Commun (Camb) ; 53(45): 6073-6076, 2017 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-28480912

RESUMO

The Langlois reagent was found to be effective for the isothiocyanation of primary amines in the presence of copper iodide and diethyl phosphonate.

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