Metabolic disorders are closely associated with the dysregulation of circadian rhythms. Many bioactive components with lipid metabolism-regulating effects have been reported to function through circadian clock-related mechanisms. As the main pungent principle of black pepper, piperine (PIP) has been demonstrated to possess anti-obesity bioactivity by affecting hepatic lipid metabolism-related factors. However, whether the circadian clock genes and are involved in the protective effect of PIP against lipid metabolism disorders remains unknown. In this work, oleic acid (OA) induced lipid accumulation in HepG2 cells. The effect of PIP on redox status, mitochondrial functions, and circadian rhythms of core clock genes were evaluated. Results revealed that PIP alleviated circadian desynchrony, ROS overproduction, and mitochondrial dysfunction. A mechanism study showed that PIP could activate the SREBP-1c/PPARγ and AMPK/AKT-mTOR signaling pathways in a /-dependent manner in HepG2 cells. These results indicated that and played important roles in the regulating effect of PIP on hepatic lipid homeostasis.
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http://dx.doi.org/10.3390/ijms23105611 | DOI Listing |
Drug Dev Res
February 2025
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt.
Five series of new 1,3,4-thiadiazole hybrids were designed and synthesized as promising EGFR inhibitors. Three human cancer cell lines were employed for testing each hybrid's in vitro antiproliferative efficacy; colon HCT-116, liver HepG-2 and breast MCF-7 using MTT assay. Comparing compound 9a to the reference doxorubicin, 9a shown superior activity to that of Dox with respect to MCF-7 (IC 3.
View Article and Find Full Text PDFDrug Dev Res
February 2025
Pharmaceutical Medicinal Chemistry and Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Nasr City, Cairo, Egypt.
New phthalazine-derived inhibitors for VEGFR-2 were synthesized for anticancer evaluations. Also, docking studies were performed to explore the suggested binding orientations of the novel derivatives inside the binding site of VEGFR-2. The achieved biological data were extremely interrelated to that of docking study.
View Article and Find Full Text PDFHeliyon
December 2024
Department of Oriental Medicine Biotechnology, College of Life Sciences, Kyung Hee University, Yongin, 17104, Republic of Korea.
Bakuchiol (), a component of , has been reported to have estrogenic, antimicrobial, and anti-inflammatory activities. Nonetheless, its anticancer mechanisms and effectiveness against hepatocellular carcinoma remain unexplored. This study sought to elucidate the mechanism of apoptosis, autophagy, and cell cycle arrest caused by bakuchiol () and three flavonoids (-) with similar structures to compound in hepatocellular carcinoma.
View Article and Find Full Text PDFAdv Biomed Res
November 2024
Molecular and Cell Biology Research Center, Faculty of Medicine, Mazandaran University of Medical Sciences, Sari, Iran.
Background: Non-alcoholic fatty liver disease is related to lipid accumulation and inflammation. Considering the role of lipin-1 and lipin-2 in fat homeostasis and inflammation, this study aimed to explore the effect of galbanic acid (Gal) and resveratrol (RSV) on alterations in the gene expression levels and protein abundance of lipin-1 and lipin-2 in HepG2 liver cells lipid-enriched with palmitate (Pal).
Materials And Methods: HepG2 cells were subjected to different amounts of Gal and RSV for 24 hours in the presence of Pal to induce lipid accumulation.
Int J Biol Macromol
December 2024
Institute of Lipid Metabolism and Atherosclerosis, School of Pharmacy, Shandong Second Medical University, Weifang 261053, China. Electronic address:
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is known to promote hyperlipidemia primarily by inducing the degradation of the low-density lipoprotein receptor. Notably, recent studies have demonstrated that PCSK9 promotes inflammation in the vascular system, however, the roles of PCSK9 in hepatic inflammation remain unclear. As PCSK9 is primarily expressed in the liver, this study aimed to elucidate the roles of PCSK9 and the underlying mechanisms in lipopolysaccharide (LPS)-challenged hepatocytes.
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