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1.
Bioorg Med Chem Lett ; 29(1): 89-96, 2019 01 01.
Artículo en Inglés | MEDLINE | ID: mdl-30446312

RESUMEN

The purpose of this study was to investigate the mechanisms underlying the inhibitory effects of rotenoisin A on adipogenesis in 3T3-L1 preadipocytes. 3T3-L1 cells were treated with rotenoisin A for 8 days after the induction of differentiation. Oil-red O staining showed that rotenoisin A significantly inhibited DMI-induced lipid accumulation and adipocyte differentiation. We found that rotenoisin A treatment of 3T3-L1 preadipocytes significantly reduced the mRNA and protein levels of the key adipocyte-specific transcription factors C/EBPß, C/EBPα, and PPARγ and markedly inhibited the expression of fatty acid-binding protein (aP2), fatty acid synthase (FAS), and lipoprotein lipase (LPL). Furthermore, we observed that rotenoisin A substantially increased the phosphorylation of AMP-activated protein kinase (AMPK) and its downstream target phosphorylated acetyl CoA carboxylase (ACC). However, co-treatment with Compound C, an AMPK inhibitor, reversed the rotenoisin A-induced inhibition of the expression of the adipogenic transcription factors C/EBPα and PPARγ and decreased the levels of phosphorylated AMPK in differentiated 3T3-L1 cells. These results demonstrated that the anti-adipogenesis mechanism involves the down-regulation of critical adipogenic transcription factors, including C/EBPß, C/EBPα, and PPARγ, through activation of the AMPK signaling pathway by rotenoisin A.


Asunto(s)
Adipocitos/efectos de los fármacos , Adipogénesis/efectos de los fármacos , Fármacos Antiobesidad/farmacología , Inhibidores de Proteínas Quinasas/farmacología , Rotenona/análogos & derivados , Rotenona/farmacología , Células 3T3-L1 , Proteínas Quinasas Activadas por AMP/antagonistas & inhibidores , Proteínas Quinasas Activadas por AMP/metabolismo , Acetil-CoA Carboxilasa/antagonistas & inhibidores , Acetil-CoA Carboxilasa/metabolismo , Adipocitos/metabolismo , Animales , Fármacos Antiobesidad/química , Relación Dosis-Respuesta a Droga , Ratones , Estructura Molecular , Inhibidores de Proteínas Quinasas/química , Rotenona/química , Relación Estructura-Actividad
2.
Saudi Pharm J ; 27(1): 145-153, 2019 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-30662318

RESUMEN

Samryeongbaekchul-san (SBS) is a traditional herbal formula, which is used for the treatment of dyspepsia, chronic gastritis, and anorexia in Korea. To evaluate the quality of SBS decoction by quantifying its main constituents simultaneously using high-performance liquid chromatography coupled with photodiode array (HPLC-PDA) detection, and secondly to determine the antiadipogenic effect of SBS decoction. The main constituents in a 10-µL injection volume of the decoction were separated on Gemini C18 and Luna NH2 columns (both 250 mm × 4.6 mm, 5 µm) at 40 °C using a gradient of two mobile phases eluting at 1.0 mL/min. 3T3-L1 preadipocytes were differentiated into adipocytes for 8 days with or without SBS. After differentiation, accumulated triglyceride contents and leptin production were measured. The correlation coefficients of all constituents in a calibration curve were ≥0.9998 and showed good linearity in the tested concentration range after validation of the method established. The recovery of the four major compounds were 99.46-102.61% with intra- and interday precisions of 0.08-1.01% and 0.15-0.99%, respectively. The four compounds in the lyophilized SBS sample were detected up to 6.46 mg/g. SBS treatment of the differentiated adipocytes significantly inhibited lipid accumulation and leptin production without cytotoxicity. Optimized simultaneous determination of constituents by HPLC-PDA detection will help to improve quality assessment of SBS or related formulas. SBS has an antiadipogenic effect and further investigation to establish the mechanisms of action of its antiadipogenic effect is warranted.

3.
J Asian Nat Prod Res ; 18(8): 784-90, 2016 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-26959764

RESUMEN

Based on characteristic UV spectrum of the ene-diyne chromophore, one new polyacetylene glucoside and three known polyacetylene glucosides have been isolated from the EtOH extract of Coreopsis tinctoria. Their chemical structures were determined by detailed spectroscopic analysis and by comparison with literature data. Compounds 1-2 were tested for their antiadipogenic effects on 3T3-L1 adipocytes, and both of them reduced lipid accumulation dose-dependently in 3T3-L1 adipocytes.


Asunto(s)
Adipocitos/efectos de los fármacos , Coreopsis/química , Medicamentos Herbarios Chinos/aislamiento & purificación , Medicamentos Herbarios Chinos/farmacología , Glucósidos/aislamiento & purificación , Glucósidos/farmacología , Poliinos/aislamiento & purificación , Poliinos/farmacología , Células 3T3-L1/efectos de los fármacos , Animales , Medicamentos Herbarios Chinos/química , Flavonoides/farmacología , Glucósidos/química , Ratones , Estructura Molecular , Poliinos/química
4.
Probiotics Antimicrob Proteins ; 15(3): 728-737, 2023 06.
Artículo en Inglés | MEDLINE | ID: mdl-35031967

RESUMEN

Intestinal microflora can influence abnormal adipocyte growth. Therefore, this study was aimed to investigate the probiotic properties and antioxidant and antiobesity effects of isolated strains from homemade kimchi. Among the isolated strains, Lactiplantibacillus plantarum KU15120 showed high tolerance to artificial gastric juice and bile salt conditions, high adhesion to HT-29 cells, nonproduction of ß-glucuronidase, nonhemolysis, and acceptable resistance to antibiotics. It showed high antioxidant activity, including DPPH and ABTS radical scavenging and antioxidant activity, as determined by the ß-carotene bleaching assay. Oil red O staining and intracellular triglyceride levels revealed reduced lipid accumulation, which confirmed the anti-adipogenic activity of L. plantarum KU15120. In addition, the expression levels of fatty acid synthase, CCAAT/enhance-binding protein α, and peroxisome proliferator-activated receptor Î³, were significantly lower in the probiotic-treated group than in the control group. These results suggest that L. plantarum KU15120 has probiotic properties, antioxidant, and antiobesity effects and could be used as a therapeutic probiotics.


Asunto(s)
Alimentos Fermentados , Probióticos , Raphanus , Antioxidantes/farmacología , Antioxidantes/metabolismo , Adipogénesis , Raphanus/metabolismo , Probióticos/farmacología , República de Corea
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