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1.
Cell Mol Biol (Noisy-le-grand) ; 69(15): 167-173, 2023 Dec 31.
Artigo em Inglês | MEDLINE | ID: mdl-38279455

RESUMO

Inflammatory responses are involved in various diseases, such as insulin resistance, atherosclerosis, and hypogonadism. This study investigates the effects of SCE on anti-inflammation and molecular mechanisms in LPS-induced macrophages. RAW 264.7 macrophage cells were treated with LPS for 24 hr, followed by SCE, schisandrin C (Sch C) (1, 10, and 100 µM), and gomisin N (GN) (1, 10, and 100 µM) for 24 hr. Gene expression levels of pro-inflammatory cytokines were measured by qPCR. Protein expression of NLPR3 inflammasome was examined by western blot analysis. The expression levels of pro-inflammatory cytokines, including IL-1ß, IL-6, and TNFα, were significantly reduced after SCE treatment. Sch C significantly inhibits these pro-inflammatory cytokines, while GN suppresses only IL6. Furthermore, Sch C significantly prevented the activation of NLRP3 inflammasome complexes such as NLRP3 and caspase-1. Sch C is the major active compound of SCE on anti-inflammation through attenuation of NLRP3 inflammasome.


Assuntos
Lignanas , Proteína 3 que Contém Domínio de Pirina da Família NLR , Compostos Policíclicos , Schisandra , Proteína 3 que Contém Domínio de Pirina da Família NLR/genética , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Inflamassomos/metabolismo , Frutas , Lipopolissacarídeos/farmacologia , Anti-Inflamatórios/farmacologia , Fator de Necrose Tumoral alfa/farmacologia , Ciclo-Octanos
2.
Chem Commun (Camb) ; 58(96): 13365-13368, 2022 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-36377645

RESUMO

In this study, we examine the site-selctive iridium(III)-catalyzed C-H amidation between 2-aryl azlactones and acyl azides. This transformation produces a range of ortho-amidated azlactones, which act as precursors for the synthesis of chiral amino acids via organocatalyzed ring-opening reactions. To test its effectiveness, the method developed is applied to the late-stage C-H amidation of complex drug molecules. The isolation of an iridacycle species supports a proposed reaction pathway.


Assuntos
Aminoácidos , Irídio , Irídio/química , Estrutura Molecular , Catálise , Azidas/química
4.
Arch Pharm Res ; 44(11): 1012-1023, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34664211

RESUMO

The site-selective and metal-free C-H nitration reaction of quinoxalinones and pyrazinones as biologically important N-heterocycles with t-butyl nitrite is described. A wide range of quinoxalinones were efficiently applied in this transformation, providing C7-nitrated quinoxalinones without undergoing C3-nitration. From the view of mechanistic point, the radical addition reaction exclusively occurred at the electron-rich aromatic region beyond electron-deficient N-heterocycle ring. This is a first report on the C7-H functionalization of quinoxalinones under metal-free conditions. In contrast, the nitration reaction readily takes place at the C3-position of pyrazinones. This transformation is characterized by the scale-up compatibility, mild reaction conditions, and excellent functional group tolerance. The applicability of the developed method is showcased by the selective reduction of NO2 functionality on the C7-nitrated quinoxalinone product, providing aniline derivatives. Combined mechanistic investigations aided the elucidation of a plausible reaction mechanism.


Assuntos
Técnicas de Química Sintética/métodos , Nitritos/química , Pirazinas/química , Quinoxalinas/química , Compostos de Anilina/síntese química
5.
Org Lett ; 23(14): 5518-5522, 2021 Jul 16.
Artigo em Inglês | MEDLINE | ID: mdl-34228466

RESUMO

The Rh(III)-catalyzed C-H functionalization and subsequent intramolecular cyclization between azobenzenes and vinylene carbonate is described herein. Depending on the electronic property of azobenzenes, this transformation results in the formation of (2H)-indazoles or dihydrocinnolin-4-ones through the generation of ortho-alkylated azo-intermediates followed by decarboxylation. Surprisingly, vinylene carbonate acts as an acetaldehyde or acetyl surrogate to enable the [4 + 1] or [4 + 2] annulation reaction. This transformation is characterized by its mild reaction conditions, simplicity, and excellent functional group compatibility.

6.
Twin Res Hum Genet ; 20(3): 226-235, 2017 06.
Artigo em Inglês | MEDLINE | ID: mdl-28347396

RESUMO

Research shows that perceived family cohesion is positively related to prosocial behavior in adolescents. In this study, we investigated heritability of prosocial behavior (PB) and perceived family cohesion (FC) among Nigerian twins attending public schools in Lagos State, Nigeria (mean age = 14.7 years, SD = 1.7 years), and explored the issue of whether children's perception of cohesive family environment moderated genetic and environmental influences on (PB). The PB scale of the Strengths and Difficulties Questionnaire and the FC scale of the Family Adaptability and Cohesion Evaluation Scale III were completed by 2,376 twins (241 monozygotic (MZ) male, 354 MZ female, 440 dizygotic (DZ) male, 553 DZ female, and 788 opposite-sex DZ twins). A general sex-limitation and the bivariate genotype by environment interaction (G×E) models were applied to the data. The general sex-limitation model showed no significant sex differences, indicating that additive genetic and non-shared environmental influences were, 38% (95% CI = 31, 46) and 62% (95% CI = 54, 69) for PB and 33% (95% CI = 24, 40) and 67% (95% CI = 60, 76) for FC in both sexes. These estimates were similar to those found in Western and Asian twin studies to date. The correlation between PB and FC was 0.36. The best-fitting bivariate G×E model indicated that FC significantly moderated non-shared environmental influence unique to PB (E×E interaction). Specifically, non-shared environmental contributions to PB were highest when FC was lowest, and decreased as the levels of FC increased. However, genetic variances in PB were stable across all levels of FC. These findings suggest that FC reduces individual differences in PB by changing non-shared environmental experiences rather than genetic factors in PB.


Assuntos
Família/psicologia , Interação Gene-Ambiente , Gêmeos Dizigóticos/genética , Gêmeos Monozigóticos/genética , Adolescente , Criança , Feminino , Genótipo , Humanos , Masculino , Caracteres Sexuais , Comportamento Social , Gêmeos Dizigóticos/psicologia , Gêmeos Monozigóticos/psicologia
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