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Source: Biochemical Pharmacology

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Total 204 results found since Jan 2013.

Salinomycin enhances cisplatin-induced cytotoxicity in human lung cancer cells via down-regulation of AKT-dependent thymidylate synthase expression.
In this study, we showed that salinomycin (0.5 - 2 μg/mL) treatment down-regulating of TS expression in an AKT inactivation manner in two NSCLC cell lines, human lung adenocarcinoma A549 and squamous cell carcinoma H1703 cells. Knockdown of TS using small interfering RNA (siRNA) or inhibiting AKT activity with PI3K inhibitor LY294002 enhanced the cytotoxicity and cell growth inhibition of salinomycin. A combination of cisplatin and salinomycin resulted in synergistic enhancement of cytotoxicity and cell growth inhibition in NSCLC cells, accompanied with reduced activation of phospho-AKT, and TS expression. Overexpression ...
Source: Biochemical Pharmacology - September 21, 2016 Category: Drugs & Pharmacology Authors: Ko JC, Zheng HY, Chen WC, Peng YS, Wu CH, Wei CL, Chen JC, Lin YW Tags: Biochem Pharmacol Source Type: research

Role for Human arylamine N-acetyltransferase 1 in the methionine salvage pathway.
Abstract The Phase II drug metabolizing enzyme arylamine N-acetyltransferase 1 (NAT1) has been implicated in the growth and survival of cancer cells, although the mechanisms that underlies these effects are unknown. Here, a focused metabolomics approach was used to identify changes in folate catabolism as well as the S-adenosylmethionine (SAM) cycle following NAT1 knockdown with shRNA. Although acetylation of the folate catabolite p-aminobenzoylglutamate (pABG) was significantly decreased, there were no changes in intracellular pABG or the various components of the SAM cycle. By contrast, the flux of homocysteine ...
Source: Biochemical Pharmacology - November 15, 2016 Category: Drugs & Pharmacology Authors: Witham KL, Minchin RF, Butcher NJ Tags: Biochem Pharmacol Source Type: research

Protein kinase CK2 α catalytic subunit ameliorates diabetic renal inflammatory fibrosis via NF-κB signaling pathway.
This study indicates the essential role of CK2α in regulating the diabetic renal pathological process of inflammatory fibrosis via NF-κB pathway, and inhibition of CK2α may serve as a promising therapeutic strategy for diabetic nephropathy. PMID: 28237649 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - February 21, 2017 Category: Drugs & Pharmacology Authors: Huang J, Chen Z, Li J, Chen Q, Li J, Gong W, Huang J, Liu P, Huang H Tags: Biochem Pharmacol Source Type: research

Resveratrol inhibits BK-induced COX-2 transcription by suppressing acetylation of AP-1 and NF- κB in human rheumatoid arthritis synovial fibroblasts.
Resveratrol inhibits BK-induced COX-2 transcription by suppressing acetylation of AP-1 and NF-κB in human rheumatoid arthritis synovial fibroblasts. Biochem Pharmacol. 2017 Mar 10;: Authors: Yang CM, Chen YW, Chi PL, Lin CC, Hsiao LD Abstract Bradykinin (BK) induces inflammation in rheumatoid arthritis (RA). Resveratrol is a potent activator of Sirt1 which could modulate inflammation through deacetylating histones of transcription factors. Here, we investigated the mechanisms underlying BK-induced COX-2 expression which is modulated by resveratrol/Sirt1 in human rheumatoid arthritis synovial fibrobla...
Source: Biochemical Pharmacology - March 9, 2017 Category: Drugs & Pharmacology Authors: Yang CM, Chen YW, Chi PL, Lin CC, Hsiao LD Tags: Biochem Pharmacol Source Type: research

Axl molecular targeting counteracts aggressiveness but not platinum-resistance of ovarian carcinoma cells.
Abstract Ovarian carcinoma, the most common gynecological cancer, is characterized by high lethality mainly due to late diagnosis and treatment failure. The efficacy of platinum drug-based therapy in the disease is limited by the occurrence of drug resistance, a phenomenon often associated with increased metastatic potential. Because the Tyr-kinase receptor Axl can be deregulated in ovarian carcinoma and plays a pro-metastatic/anti-apoptotic role, the aim of this study was to examine if Axl inhibition modulates drug resistance and aggressive features of ovarian carcinoma cells, using various pairs of cisplatin-sen...
Source: Biochemical Pharmacology - April 9, 2017 Category: Drugs & Pharmacology Authors: Corno C, Gatti L, Arrighetti N, Carenini N, Zaffaroni N, Lanzi C, Perego P Tags: Biochem Pharmacol Source Type: research

H2S-induced S-sulfhydration of lactate dehydrogenase A (LDHA) stimulates cellular bioenergetics in HCT116 colon cancer cells.
Abstract Cystathionine-β-synthase (CBS) is upregulated and hydrogen sulfide (H2S) production is increased in colon cancer cells. The functional consequence of this response is stimulation of cellular bioenergetics and tumor growth and proliferation. Lactate dehydrogenase A (LDHA) is also upregulated in various colon cancer cells and has been previously implicated in tumor cell bioenergetics and proliferation. In the present study, we sought to determine the potential interaction between the H2S pathway and LDH activity in the control of bioenergetics and proliferation of colon cancer, using the colon cancer line ...
Source: Biochemical Pharmacology - April 9, 2017 Category: Drugs & Pharmacology Authors: Untereiner AA, Oláh G, Módis K, Hellmich MR, Szabo C Tags: Biochem Pharmacol Source Type: research

Ligand-dependent and -independent regulation of human hepatic sphingomyelin phosphodiesterase acid-like 3A expression by pregnane X receptor and crosstalk with liver X receptor.
In conclusion, this study describes that decrease of PXR expression levels and ligand-dependent activation of PXR and LXR increase hepatic SMPDL3A levels, which possibly connects these receptors to hepatic purinergic signaling and phospholipid metabolism and may result in drug-drug interactions with phosphoramidate pro-drugs. PMID: 28414139 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - April 13, 2017 Category: Drugs & Pharmacology Authors: Jeske J, Bitter A, Thasler WE, Weiss TS, Schwab M, Burk O Tags: Biochem Pharmacol Source Type: research

Therapeutic effect of Cryptotanshinone on experimental rheumatoid arthritis through downregulating p300 mediated-STAT3 acetylation.
CONCLUSION AND IMPLICATIONS: Our study suggested that the anti-arthritis effects of CTS were attained through suppression of p300-mediated STAT3 acetylation. Our data suggest that CTS might be a potential immune modulator for RA treatment. PMID: 28522406 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - May 15, 2017 Category: Drugs & Pharmacology Authors: Wang Y, Zhou C, Gao H, Li C, Li D, Liu P, Huang M, Shen X, Liu L Tags: Biochem Pharmacol Source Type: research

Anti-inflammatory mechanism of galangin in lipopolysaccharide-stimulated microglia: critical role of PPAR- γ signaling pathway.
Anti-inflammatory mechanism of galangin in lipopolysaccharide-stimulated microglia: critical role of PPAR-γ signaling pathway. Biochem Pharmacol. 2017 Jul 27;: Authors: Choi MJ, Lee EJ, Park JS, Kim SN, Park EM, Kim HS Abstract Since microglia-associated neuroinflammation plays a pivotal role in the progression of neurodegenerative diseases, controlling microglial activation has been suggested as a potential therapeutic strategy. Here, we investigated the anti-inflammatory effects of galangin (3,5,7-trihydroxyflavone) in microglia and analyzed the underlying molecular mechanisms. Galangin inhibited t...
Source: Biochemical Pharmacology - July 27, 2017 Category: Drugs & Pharmacology Authors: Choi MJ, Lee EJ, Park JS, Kim SN, Park EM, Kim HS Tags: Biochem Pharmacol Source Type: research

Computational discovery and experimental verification of farnesoid X receptor agonist auraptene to protect against cholestatic liver injury.
Abstract Recently obeticholic acid (OCA) which is a farnesoid X receptor (FXR) agonist was approved by FDA to treat cholestatic liver diseases, which provided us a novel therapeutic strategy against cholestasis. Herein, we used a novel computational strategy with two-dimensional virtual screening for FXR agonists. For the first time, we found that auraptene (AUR), a natural product, can activate FXR to exert hepatoprotective effect against cholestatic liver injury in vivo and in vitro. Importantly, AUR was found to significantly decrease the mortality of cholestatic mice. Dynamic change analysis of bile acids and ...
Source: Biochemical Pharmacology - October 4, 2017 Category: Drugs & Pharmacology Authors: Gao X, Fu T, Wang C, Ning C, Kong Y, Liu Z, Sun H, Ma X, Liu K, Meng Q Tags: Biochem Pharmacol Source Type: research

α1A-Adrenoceptors activate mTOR signalling and glucose uptake in cardiomyocytes.
Abstract The capacity of G protein-coupled receptors to modulate mammalian target of rapamycin (mTOR) activity is a newly emerging paradigm with the potential to link cell surface receptors with cell survival. Cardiomyocyte viability is linked to signaling pathways involving Akt and mTOR, as well as increased glucose uptake and utilization. Our aim was to determine whether the α1A-adrenoceptor (AR) couples to these protective pathways, and increased glucose uptake. We characterised α1A-AR signalling in CHO-K1 cells co-expressing the human α1A-AR and GLUT4 (CHOα1AGLUT4myc) and in neonatal rat ventricular cardio...
Source: Biochemical Pharmacology - November 23, 2017 Category: Drugs & Pharmacology Authors: Sato M, Evans BA, Sandström AL, Yeong Chia L, Mukaida S, San Thai B, Nguyen A, Lim L, Yr Tan C, Baltos JA, White PJ, May LT, Hutchinson DS, Summers RJ, Bengtsson T Tags: Biochem Pharmacol Source Type: research

Zerumbone Protects Human Skin Keratinocytes against UVA-irradiated Damages through Nrf2 Induction.
Abstract Ultraviolet A (UVA) irradiation is toxic to skin as it penetrates deep into the dermis and damages cellular components through excessive reactive oxygen species (ROS) production, which accelerates photoaging and skin cancer. We evaluated the dermato-protective efficacies of zerumbone (natural sesquiterpene of Zingiber zerumbet) in UVA-irradiated human skin keratinocyte (HaCaT) cells and mouse epidermis. Zerumbone pretreatment (2-10 μM) substantially suppressed UVA (15 J/cm2)-induced HaCaT cell death and lactate dehydrogenase release in a dose-dependent manner. UVA-induced excessive ROS production, DNA si...
Source: Biochemical Pharmacology - December 19, 2017 Category: Drugs & Pharmacology Authors: Yang HL, Lee CL, Korivi M, Liao JW, Rajendran P, Wu JJ, Hseu YC Tags: Biochem Pharmacol Source Type: research

Heme oxygnease-1 induction by methylene blue protects RAW264.7 cells from hydrogen peroxide-induced injury.
Abstract Althoughmethylene blue (MB) has showed strong antioxidant effect, its effect related with heme oxygenase-1(HO-1) is still unclear. Thus, we investigated the effects of MB on HO-1 protein content and enzyme activity, and its protective effect against hydrogen peroxide (H2O2)- induced oxidative damage in RAW264.7 macrophage. The cellviability and the release of lactate dehydrogenase of RAW264.7 were determined. The mitochondrial functions were valuated through these indexes: content of adenosine triphosphate, superoxide dismutase, concentration of reactive oxygen species and mitochondrial membrane potential...
Source: Biochemical Pharmacology - January 5, 2018 Category: Drugs & Pharmacology Authors: Zhang XT, Sun XQ, Wu C, Chen JL, Yuan JJ, Pang QF, Wang ZP Tags: Biochem Pharmacol Source Type: research

Baicalein and baicalin alleviate acetaminophen-induced liver injury by activating Nrf2 antioxidative pathway: the involvement of ERK1/2 and PKC.
This study investigated the protection of baicalin and its aglycone baicalein against APAP-induced hepatotoxicity and its mechanism. Baicalein and baicalin alleviated APAP-induced hepatotoxicity both in vitro and in vivo. Moreover, baicalin-provided this protection was not diminished in hepatocytes or mice treated with β-glucuronidase inhibitor. Results of liver glutathione (GSH) and reactive oxygen species (ROS) formation demonstrated the alleviation of baicalein and baicalin on APAP-induced liver oxidative stress injury. Baicalein and baicalin induced the activation of nuclear factor erythroid 2-related factor 2 (Nrf2) ...
Source: Biochemical Pharmacology - January 12, 2018 Category: Drugs & Pharmacology Authors: Shi L, Hao Z, Zhang S, Wei M, Lu B, Wang Z, Ji L Tags: Biochem Pharmacol Source Type: research

Invited submission to the Diamond Jubilee Special Issue of Biochemical PharmacolLeptin induces SIRT1 expression through activation of NF-E2-related factor 2: implications for obesity-associated colon carcinogenesis.
In conclusion, leptin might play a role in colon carcinogenesis by inducing Nrf2-dependent SIRT1 overexpression. PMID: 29427626 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - February 7, 2018 Category: Drugs & Pharmacology Authors: Song NY, Lee YH, Na HK, Baek JH, Surh YJ Tags: Biochem Pharmacol Source Type: research