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Source: Biochemical Pharmacology

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Total 204 results found since Jan 2013.

GR-C/EBP α-IGF1 axis mediated azithromycin-induced liver developmental toxicity in fetal mice.
In this study, we observed the developmental toxicity of fetal liver induced by prenatal azithromycin exposure (PAE) in mice and explored the potential mechanism. Pregnant Kunming mice were intraperitoneally injected with azithromycin (37.5 and 150 mg/kg·d) from gestational day (GD) 9 to 18. After PAE, the bodyweight gain rates of pregnant mice and the birthweights of the offspring were decreased, and the liver morphology, development indexes and metabolic function were all altered in different degree in the PAE fetuses. Meanwhile, PAE decreased the fetal serum insulin-like growth factor 1 (IGF1) levels and liver IGF1 sig...
Source: Biochemical Pharmacology - June 28, 2020 Category: Drugs & Pharmacology Authors: Liu K, Wang G, Li L, Chen G, Gong X, Zhang Q, Wang H Tags: Biochem Pharmacol Source Type: research

RGFP966, a Histone deacetylase 3 inhibitor, promotes glioma stem cell differentiation by blocking TGF- β signaling via SMAD7.
RGFP966, a Histone deacetylase 3 inhibitor, promotes glioma stem cell differentiation by blocking TGF-β signaling via SMAD7. Biochem Pharmacol. 2020 Jun 22;:114118 Authors: Liang H, Wang Q, Wang D, Zheng H, Kalvakolanu DV, Lu H, Wen N, Chen X, Xu L, Ren J, Guo B, Zhang L Abstract Glioma stem cells (GSC) play a major role in drug resistance and tumor recurrence. Using a genetic screen with a set of shRNAs that can target chromatin regulators in a GSC model, we have HDAC3 as a major negative regulator of GSC differentiation. Inhibition of HDAC3 using a pharmacological inhibitor or a siRNA led to the in...
Source: Biochemical Pharmacology - June 21, 2020 Category: Drugs & Pharmacology Authors: Liang H, Wang Q, Wang D, Zheng H, Kalvakolanu DV, Lu H, Wen N, Chen X, Xu L, Ren J, Guo B, Zhang L Tags: Biochem Pharmacol Source Type: research

TIMP1 down-regulation enhances gemcitabine sensitivity and reverses chemoresistance in pancreatic cancer.
Abstract The therapeutic effect of gemcitabine (GEM) in pancreatic ductal adenocarcinoma (PDAC) is limited due to low drug sensitivity and high drug resistance. Tissue inhibitor of matrix metalloprotease 1 (TIMP1) is reportedly associated with GEM resistance in PDAC. However, the effect of TIMP1 down-regulation in combination with GEM treatment is unknown. We analyzed the expression of TIMP1 in human PDAC tissue using western blot, quantitative real-time polymerase chain reaction (qRT-PCR), and immunohistochemistry. TIMP1 was highly expressed in PDAC specimens. Kaplan-Meier survival analysis suggested that a highe...
Source: Biochemical Pharmacology - June 5, 2020 Category: Drugs & Pharmacology Authors: Tan Y, Li X, Tian Z, Chen S, Zou J, Lian G, Chen S, Huang K, Chen Y 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

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

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

NEK7 mediated assembly and activation of NLRP3 inflammasome downstream of potassium efflux in ventilator-induced lung injury.
In this study, we constructed an in vitro cyclic stretch (CS)-stimulated mouse lung epithelial (MLE-12) cell model that was transfected with NIMA-related kinase 7 (NEK7) small interfering RNA (siRNA) or scramble siRNA (sc siRNA) and pretreated with or without glibenclamide (glb). We also established a VILI mouse model, which was pretreated with glibenclamide or oridonin (Ori). Our goal was to investigate the regulatory effects of NEK7 on NLRP3 inflammasome activation and the anti-inflammatory effects of glibenclamide and oridonin on VILI. Mechanical stretch exaggerated the interaction between NEK7 and NLRP3, leading to ass...
Source: Biochemical Pharmacology - April 26, 2020 Category: Drugs & Pharmacology Authors: Liu H, Gu C, Liu M, Liu G, Wang Y 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

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

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

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

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

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

Cytoplasmic expression of EGFR shRNA using a modified T7 autogene-based hybrid mRNA/DNA system induces long-term EGFR silencing and prolongs antitumor effects.
Abstract Unusual activation or overexpression of epidermal growth factor receptor (EGFR) has been found in various cancers, and therefore down-regulation of EGFR expression is recognized as a promising strategy for cancer treatment. For decades, RNAi has emerged as an effective solution to regulate gene overexpression, but transient effects of exogenous siRNA have limited the development of EGFR-targeting siRNA therapeutics. Recently, we developed T7 autogene-based hybrid mRNA/DNA system as a non-viral vector for shRNA production and reported the feasibility of long-term silencing for RFP expression as a concept o...
Source: Biochemical Pharmacology - November 27, 2019 Category: Drugs & Pharmacology Authors: Seraj S, Jae Cho Y, Lee JW, Jun Ahn H Tags: Biochem Pharmacol Source Type: research