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Source: Biochemical Pharmacology

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Total 204 results found since Jan 2013.

Aromatic Hydrocarbon Receptor Regulates Chicken Cytochrome P450 1A5 Transcription: A Novel Insight into T-2 Toxin-induced Gene Expression and Cytotoxicity in LMH Cells.
Abstract T-2 toxin is a secondary metabolite produced by the Fusarium genus and is highly toxic to both farmed animals and humans. In our previous study, we found that chicken cytochrome P450 1A5 (CYP1A5) can be significantly induced by T-2 toxin in chicken primary hepatocytes and catalyze T-2 toxin into a more toxic product, 3'-OH-T-2. Here, we showed that T-2 toxin also induced the expression of CYP1A5 in LMH cells at both the mRNA and protein levels, and this can be strongly inhibited by both resveratrol and siRNA targeting the aryl hydrocarbon receptor (AhR), indicating the involvement of AhR in T-2 toxin-indu...
Source: Biochemical Pharmacology - July 24, 2019 Category: Drugs & Pharmacology Authors: Liu Q, Wen J, Zhu J, Zhang T, Deng Y, Jiang J Tags: Biochem Pharmacol Source Type: research

Modulation of Sirt1/NF- κB interaction of evogliptin attributed to inhibition of vascular inflammatory response leading to attenuation of atherosclerotic plaque formation.
This study demonstrates that the protective effect of evogliptin on atherosclerotic progression via inhibition of vascular inflammation. The findings imply that evogliptin has potential for anti-atherosclerosis therapy that targets arterial inflammation. PMID: 31421133 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - August 13, 2019 Category: Drugs & Pharmacology Authors: Anh Nguyen P, Soon Won J, Khalilur Rahman M, Ju Bae E, Kyung Cho M Tags: Biochem Pharmacol Source Type: research

M3 Muscarinic receptor activation reduces hepatocyte lipid accumulation via CaMKK β/AMPK pathway.
In conclusion, this proof-of-concept study demonstrates that M3R has protective effects against hepatocyte lipid accumulation by activating AMPK pathway and is a potential therapeutic target for non-alcoholic fatty liver disease. PMID: 31445019 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - August 20, 2019 Category: Drugs & Pharmacology Authors: Jadeja RN, Chu X, Wood C, Bartoli M, Khurana S Tags: Biochem Pharmacol Source Type: research

Nardosinanone N suppresses LPS-induced macrophage activation by modulating the Nrf2 pathway and mPGES-1.
In conclusion, NAN may be a new anti-inflammatory drug that has fewer side effects than NSAIDs and can be a new potential Nrf2 activator and mPGES-1 inhibitor. PMID: 31536727 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - September 15, 2019 Category: Drugs & Pharmacology Authors: Lio CK, Luo JF, Shen XY, Dai Y, Machado J, Xie Y, Yao YD, Yu Y, Liu JX, Yao XS, Luo P, Zhou H Tags: Biochem Pharmacol Source Type: research

DEL-1 ameliorates high-fat diet-induced insulin resistance in mouse skeletal muscle through SIRT1/SERCA2-mediated ER stress suppression.
Abstract Inflammation and endoplasmic reticulum (ER) stress are associated with the development of insulin resistance and diabetes. Developmental endothelial locus-1 (DEL-1) enhances efferocytosis by macrophage and suppresses inflammatory response. However, effects of DEL-1 on ER stress-mediated insulin resistance in skeletal muscle remain unclear. Here, DEL-1 treatment augmented SIRT1 expression in C2C12 myocytes, thereby increasing SERCA2 expression in a dose-dependent fashion, and attenuated ER stress and insulin resistance under palmitate treatment condition. SIRT1/SERCA2 knockdown abrogated effects of DEL-1 o...
Source: Biochemical Pharmacology - November 24, 2019 Category: Drugs & Pharmacology Authors: Long Sun J, Park J, Lee T, Hoon Jeong J, Woo Jung T Tags: Biochem Pharmacol Source Type: research

Hydrogen sulfide modulates epithelial-mesenchymal transition and angiogenesis in non-small cell lung cancer via HIF-1 α activation.
Hydrogen sulfide modulates epithelial-mesenchymal transition and angiogenesis in non-small cell lung cancer via HIF-1α activation. Biochem Pharmacol. 2019 Dec 20;:113775 Authors: Wang M, Yan J, Cao X, Hua P, Li Z Abstract Hydrogen sulfide (H2S) has been frequently implicated in tumor progression. However, the exact regulation mechanism of H2S in human non-small cell lung cancer (NSCLC) has not been fully elucidated. Here, analysis of NSCLC biopsies and adjacent non-tumor tissues revealed selectively high levels of endogenous H2S-producing enzymes, cystathionine-beta-synthase (CBS), cystathionine-gamm...
Source: Biochemical Pharmacology - December 19, 2019 Category: Drugs & Pharmacology Authors: Wang M, Yan J, Cao X, Hua P, Li Z Tags: Biochem Pharmacol Source Type: research

Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
Abstract The present study was aimed to investigate the effects of curcumin, a representative chemopreventive phytochemical with pronounced antioxidant and anti-inflammatory properties, on activation of Nrf2 and its target protein heme oxygenase-1 (HO-1) in mouse skin in vivo and in cultured murine epidermal cells. Treatment of mouse epidermal JB-6 cells with curcumin resulted in the induction of HO-1 expression, and this was abrogated in cells transiently transfected with Nrf2 siRNA. While curcumin treatment increased protein expression of Nrf2, it failed to did not alter the steady-state level of the Nrf2 mRNA t...
Source: Biochemical Pharmacology - January 19, 2020 Category: Drugs & Pharmacology Authors: Shin JW, Chun KS, Kim DH, Kim SJ, Hoon Kim S, Cho NC, Na HK, Surh YJ Tags: Biochem Pharmacol Source Type: research

Activation of notch 3/c-MYC/CHOP axis regulates apoptosis and promotes sensitivity of lung cancer cells to mTOR inhibitor everolimus.
Abstract The mammalian target of rapamycin (mTOR) pathway converges diverse environmental cues to support the lung cancer growth and survival. However, the mTOR-targeted mono-therapy does not achieve expected therapeutic effect. Here, we revealed that fangchinoline (FCL), an active alkaloid that purified from the traditional Chinese medicine Stephania tetrandra S. Moore, enhanced the anti-lung cancer effect of mTOR inhibitor everolimus (EVE). The combination of EVE and FCL was effective to activate Notch 3, and subsequently evoked its downstream target c-MYC. The blockage of Notch 3 signal by the molecular inhibit...
Source: Biochemical Pharmacology - March 18, 2020 Category: Drugs & Pharmacology Authors: Li T, Xu XH, Guo X, Yuan T, Tang ZH, Jiang XM, Xu YL, Zhang LL, Chen X, Zhu H, Shi JJ, Lu JJ Tags: Biochem Pharmacol Source Type: research

Ethacrynic acid inhibits STAT3 activity through the modulation of SHP2 and PTP1B tyrosine phosphatases in DU145 prostate carcinoma cells.
Abstract To identify signal transducer and activator of transcription factor 3 (STAT3) inhibitors, we generated STAT3-dependent gene expression signature by analyzing gene expression profiles of DU145 cancer cells treated with STAT3 inhibitor, piperlongumine and 2-hydroxycinnamaldehyde. Then we explored gene expression signature-based strategies using a connectivity map database and identified several STAT3 inhibitors, including ethacrynic acid (EA). EA is currently used as a diuretic drug. EA inhibited STAT3 activation in DU145 prostate cancer cells and consequently decreased the levels of STAT3 target genes such...
Source: Biochemical Pharmacology - March 18, 2020 Category: Drugs & Pharmacology Authors: Lee YJ, Song H, Yoon YJ, Park SJ, Kim SY, Cho Han D, Kwon BM Tags: Biochem Pharmacol Source Type: research

Modulation of SIRT1-mediated signaling cascades in the liver contributes to the amelioration of nonalcoholic steatohepatitis in high fat fed middle-aged LDL receptor knockout mice by dihydromyricetin.
Abstract Dihydromyricetin (DMY) is the most abundant flavonoid in Ampelopsis grossedentata possessing many pharmacological activities. But less is known about its protective effect against nonalcoholic steatohepatitis (NASH) in the context of metabolic syndrome. The present study is aimed to evaluate the pharmacological effects of DMY on NASH induced by feeding a high fat diet to 12-mo-old male LDLr-/- mice for 12 weeks and its molecular mode of action. At the end of the experiment, the blood samples and liver tissues of mice were collected for analysis. The results showed that DMY treatment improved the steatosis...
Source: Biochemical Pharmacology - March 22, 2020 Category: Drugs & Pharmacology Authors: Zeng Y, Hua YQ, Wang W, Zhang H, Xu XL Tags: Biochem Pharmacol Source Type: research

Ribociclib mitigates cisplatin-associated kidney injury through retinoblastoma-1 dependent mechanisms.
Abstract Aberrant cell cycle activation is a hallmark of carcinogenesis. Recently three cell cycle targeting cyclin-dependent kinase 4/6 (CDK4/6) inhibitors have been approved for the treatment of metastatic breast cancer. CDK4/6 inhibitors suppress proliferation through inhibition of CDK4/6-dependent retinoblastoma-1 (Rb1) phosphorylation and inactivation, a key regulatory step in G1-to-S-phase transition. Interestingly, aberrant cell cycle activation is also linked with several non-oncological diseases including acute kidney injury (AKI). AKI is a common disorder caused by toxic, inflammatory, and ischemic damag...
Source: Biochemical Pharmacology - March 26, 2020 Category: Drugs & Pharmacology Authors: Young Kim J, Jayne LA, Bai Y, Feng MJHH, Clark MA, Chung S, W Christman J, Cianciolo RE, Singh Pabla N Tags: Biochem Pharmacol Source Type: research

DC591017, a phosphodiesterase-4 (PDE4) inhibitor with robust anti-inflammation through regulating PKA-CREB signaling.
This study was intended to assess the anti-inflammatory effects of the PDE4 inhibitor, DC591017, both in vitro and in vivo. Murine RAW264.7 cells, BMDMs, BMDCs, and human NHEKs were incubated with DC591017 and then inflammatory mediators, intracellular cAMP and cAMP-mediated signaling pathways were analyzed. Carrageenan-induced acute inflammation in murine air pouches and rat paws, as well as imiquimod (IMQ)-induced psoriasis-like skin lesions were conducted to explore the therapeutic effects and underlying mechanisms of DC591017. We demonstrated herein that DC591017 suppressed the inflammatory responses of macrophages and...
Source: Biochemical Pharmacology - April 2, 2020 Category: Drugs & Pharmacology Authors: Li H, Li J, Zhang X, Feng C, Fan C, Yang X, Zhang R, Zhu F, Zhou Y, Xu Y, Liu H, Tang W Tags: Biochem Pharmacol Source Type: research

Tetrahydroxy stilbene glycoside alleviated inflammatory damage by mitophagy via AMPK related PINK1/Parkin signaling pathway.
In conclusion, these phenomena suggested that TSG prevented LPS/ATP and Aβ-induced inflammation via AMPK/PINK1/Parkin-dependent enhancement of mitophagy. We found the neuroprotective effect of TSG, suggesting it may be beneficial for AD prevention and treatment by suppressing the activation of inflammation. PMID: 32353422 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - April 26, 2020 Category: Drugs & Pharmacology Authors: Gao Y, Li J, Li J, Hu C, Zhang L, Yan J, Li L, Zhang L Tags: Biochem Pharmacol Source Type: research

Ginsenoside Rh4 suppresses aerobic glycolysis and the expression of PD-L1 via targeting AKT in esophageal cancer.
Abstract Ginsenoside Rh4, as a bioactive component obtained from Panax notoginseng, has excellent pharmacological efficacy especially antitumor effects. However, its anticancer effects and target mechanisms in regulating human esophageal cancer are still poorly understood. Here, the results suggested that Rh4 exhibited potent anti-esophageal cancer effects in vivo and in vitro. Flow cytometric analysis and Western Blot showed that Rh4 significantly inhibited the growth by inducing G1 phase arrest. In parallel, Rh4 inhibited aerobic glycolysis in esophageal cancer cells by hindering lactate production, glucose upta...
Source: Biochemical Pharmacology - May 14, 2020 Category: Drugs & Pharmacology Authors: Deng X, Zhao J, Qu L, Duan Z, Fu R, Zhu C, Fan D Tags: Biochem Pharmacol Source Type: research

Chrysophanol ameliorates renal interstitial fibrosis by inhibiting the TGF- β/Smad signaling pathway.
Chrysophanol ameliorates renal interstitial fibrosis by inhibiting the TGF-β/Smad signaling pathway. Biochem Pharmacol. 2020 Jun 05;:114079 Authors: Dou F, Ding Y, Wang C, Duan J, Wang W, Xu H, Zhao X, Wang J, Wen A Abstract Renal interstitial fibrosis (RIF) is a major pathological feature of chronic kidney disease at middle and end stages. Chrysophanol (CP), 1,8-dihydroxy-3-methyl-9,10-anthraquinone, is an anthraquinone isolated from Rheum palmatum L.with a variety of pharmacological activities including the suppression of RIF. However, the effect of CP on renal fibrosis and its potential mechanism ...
Source: Biochemical Pharmacology - June 4, 2020 Category: Drugs & Pharmacology Authors: Dou F, Ding Y, Wang C, Duan J, Wang W, Xu H, Zhao X, Wang J, Wen A Tags: Biochem Pharmacol Source Type: research