Read by QxMD icon Read

Curcumin resveratrol HepG2

Abdulmajeed A Bahman, Mohamed Salah I Abaza, Sarah I Khoushiash, Rajaa J Al-Attiyah
Sorafenib (Nexavar, BAY43‑9006 or Sora) is the first molecular targeted agent that has exhibited significant therapeutic benefits in advanced hepatocellular carcinoma (HCC). However, not all HCC patients respond well to Sora and novel therapeutic strategies to optimize the efficacy of Sora are urgently required. Plant‑based drugs have received increasing attention owing to their excellent chemotherapeutic and chemopreventive activities; they are also well tolerated, non‑toxic, easily available and inexpensive...
June 8, 2018: International Journal of Molecular Medicine
Matheus de Freitas Silva, Letícia Ferreira Coelho, Isadora Mitestainer Guirelli, Rodrigo Machado Pereira, Guilherme Álvaro Ferreira-Silva, Graciana Y Graravelli, Renato de Oliveira Horvath, Ester Siqueira Caixeta, Marisa Ionta, Claudio Viegas
Curcumin (1) and resveratrol (2) are bioactive natural compounds that display wide pharmacological properties, including antitumor activity. However, their clinical application has been limited due to their low solubility and bioavailability. Nevertheless, independent studies have considered these compounds as interesting prototypes for developing new chemical structures useful for anticancer therapy. Here in, we report the synthesis of novel curcumin-like hydrazide analogues (3a and 3b), and a series of curcumin-resveratrol hybrid compounds (4a-f), and the evaluation of their cytotoxic potential on three tumor cell lines MCF-7 (breast), A549 (lung), and HepG2 (liver)...
March 2, 2018: Toxicology in Vitro: An International Journal Published in Association with BIBRA
Tiong Chai Seah, Yea Lu Tay, Heng Kean Tan, Tengku Sifzizul Tengku Muhammad, Habibah Abdul Wahab, Mei Lan Tan
A cell-based assay to measure cytochrome P450 3A4 (CYP3A4) induction was developed to screen for potential CYP3A4 inducers. This 96-well format assay utilizes HepG2 cells transfected with a gene construct of CYP3A4 proximal promoter linked to green fluorescence protein (GFP) gene, and the expression of the GFP is then measured quantitatively. Bergamottin at 5 to 25 µmol/L produced low induction relative to the positive control. Both curcumin and lycopene were not found to affect the expression of GFP, suggesting no induction properties toward CYP3A4...
September 2015: International Journal of Toxicology
Afshin Mohammadi-Bardbori, Johanna Bengtsson, Ulf Rannug, Agneta Rannug, Emma Wincent
Several polyphenols have been shown to activate the aryl hydrocarbon receptor (AHR) in spite of the fact that they bind to the receptor with low affinity. The aim of this study was to investigate whether quercetin (QUE), resveratrol (RES), and curcumin (CUR) interfere with the metabolic degradation of the suggested endogenous AHR ligand 6-formylindolo[3,2-b]carbazole (FICZ) and thereby indirectly activate the AHR. Using recombinant human enzyme, we confirmed earlier reported inhibitory effects of the polyphenols on cytochrome P4501A1 (CYP1A1) activity, and inhibition of metabolic clearance of FICZ was documented in FICZ-treated immortalized human keratinocytes (HaCaT)...
September 17, 2012: Chemical Research in Toxicology
Ban-Feng Ruan, Xiang Lu, Ting-Ting Li, Jian-Feng Tang, Yao Wei, Xiao-Liang Wang, Shi-Li Zheng, Ri-Sheng Yao, Hai-Liang Zhu
A series of resveratrol derivatives possessing curcumin moiety were synthesized and evaluated for their antiproliferative activity against three cancer cell lines including murine melanoma B16-F10, human hepatoma HepG2 and human lung carcinoma A549. Among them, compound C5 displayed the most potent in vitro antiproliferative activity against B16-F10 with IC(50) value of 0.71 μg/mL. Compound C5 also exhibited good tubulin polymerization inhibitory activity with IC(50) value of 1.45 μg/mL. Furthermore, docking simulation was carried out to position C5 into the tubulin-colchicine binding site to determine the probable binding mode...
January 15, 2012: Bioorganic & Medicinal Chemistry
Nathalie Arnal, María J Tacconi de Alaniz, Carlos Alberto Marra
The effect of the simultaneous exposure to transition metals and natural antioxidants frequently present in food is a question that needs further investigation. We aimed to explore the possible use of the natural polyphenols caffeic acid (CA), resveratrol (RES) and curcumin (CUR) to prevent damages induced by copper-overload on cellular molecules in HepG2 and A-549 human cells in culture. Exposure to 100μM/24h copper (Cu) caused extensive pro-oxidative damage evidenced by increased TBARS, protein carbonyls and nitrite productions in both cell types...
February 2012: Food and Chemical Toxicology
Judy L Raucy
Human CYP3A4 metabolizes a majority of clinically important substrates at variable rates. Accounting for these unpredictable rates is the wide variation noted in expression of this enzyme that is due, in part, to xenobiotic exposure. We used primary cultures of human hepatocytes from 17 individuals to assess the inducibility of CYP3A4 mRNA by prototypical inducers, dietary flavonoids, and botanicals. Those agents producing the greatest mRNA accumulation were 10 microM RIF (699 +/- 307% of control levels) 100 microM phenytoin (707 +/- 188% of control), 1 mM phenobarbital (536 +/- 207% of control), and 100 microM omeprazole (404 +/- 8% of control)...
May 2003: Drug Metabolism and Disposition: the Biological Fate of Chemicals
S W Allen, L Mueller, S N Williams, L C Quattrochi, J Raucy
We examined the effects of several agents, including dietary flavonoids, on CYP1A1 expression utilizing a recently developed high-throughput screening system for assessing human cytochrome P450 (CYP) induction. HepG2 cells, stably integrated with regulatory regions of human CYP1A1, were treated with resveratrol, apigenin, curcumin, kaempferol, green tea extract (GTE), (-)-epigallocatechin gallate (EGCG), quercetin, and naringenin. Of these flavonoids, resveratrol produced the greatest increase in CYP1A1-mediated luciferase activity (10-fold), whereas GTE, apigenin, curcumin, and kaempferol produced 2- to 3-fold increases in activity...
August 2001: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"