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Source: Biochemical Pharmacology

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Total 204 results found since Jan 2013.

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

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

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

Rutaecarpine Derivative Cpd-6c Alleviates Acute Kidney Injury by Targeting PDE4B, a Key Enzyme Mediating inflammation in Cisplatin Nephropathy.
Abstract Acute kidney injury (AKI), characterized by a rapid decline in renal function, is triggered by an acute inflammatory response that leads to kidney damage. An effective treatment for AKI is lacking. Using in vitro and in vivo AKI models, our laboratory has identified a series of anti-inflammatory molecules and their derivatives. In the current study, we identified the protective role of rutaecarpine (Ru) on renal tubules. We obtained a series of 3-aromatic sulphonamide-substituted Ru derivatives exhibiting enhanced renoprotective and anti-inflammatory function. We identified Compound-6c(Cpd-6c) as having t...
Source: Biochemical Pharmacology - July 1, 2020 Category: Drugs & Pharmacology Authors: Liu XQ, Jin J, Li Z, Jiang L, Dong YH, Cai YT, Wu MF, Wang JN, Ma TT, Wen JG, Liu MM, Li J, Wu YG, Meng XM Tags: Biochem Pharmacol Source Type: research

TGF- β1-induced miR-424 promotes pulmonary myofibroblast differentiation by targeting Slit2 protein expression.
The objective of this study was to define the pro-fibrotic roles and mechanisms of miRs in TGF-β1-induced pulmonary myofibroblast differentiation. Using RNA sequencing, we identified miR-424 as an important TGF-β1-induced miR in human lung fibroblasts (HLFs). Quantitative RT-PCR confirmed that miR-424 expression was increased by 2.6-fold in HLFs in response to TGF-β1 and was 1.7-fold higher in human fibrotic lung tissues as compared to non-fibrotic lung tissues. TGF-β1-induced upregulation of miR-424 was blocked by the Smad3 inhibitor SIS3, suggesting the involvement of this canonical TGF-β1 signaling pathway. Transfe...
Source: Biochemical Pharmacology - July 22, 2020 Category: Drugs & Pharmacology Authors: Huang Y, Xie Y, Abel PW, Wei P, Plowman J, Toews ML, Strah H, Siddique A, Bailey KL, Tu Y Tags: Biochem Pharmacol Source Type: research

Angiotensin-(1-9) prevents vascular remodeling by decreasing vascular smooth muscle cell dedifferentiation through a FoxO1-dependent mechanism.
Abstract The renin-angiotensin system, one of the main regulators of vascular function, controls vasoconstriction, inflammation and vascular remodeling. Antagonistic actions of the counter-regulatory renin-angiotensin system, which include vasodilation, anti-proliferative, anti-inflammatory and anti-remodeling effects, have also been described. However, little is known about the direct effects of angiotensin-(1-9), a peptide of the counter-regulatory renin-angiotensin system, on vascular smooth muscle cells. Here, we studied the anti-vascular remodeling effects of angiotensin-(1-9), with special focus on the contr...
Source: Biochemical Pharmacology - August 4, 2020 Category: Drugs & Pharmacology Authors: Norambuena-Soto I, Paz Ocaranza M, Cancino-Arenas N, Sanhueza-Olivares F, Villar-Fincheira P, Leiva-Navarrete S, Mancilla C, Moya J, Novoa U, Jalil JE, Castro PF, Lavandero S, Chiong M Tags: Biochem Pharmacol Source Type: research

MicroRNA-101 inhibits cadmium-induced angiogenesis by targeting cyclooxygenase-2 in primary human umbilical vein endothelial cells.
Abstract Exposure to toxic metal contaminants, such as cadmium complexes (Cd2+), has been shown to induce adverse effects on various organs and tissues. In particular, blood vessels are severely impacted by Cd2+ exposure, which may lead to cardiovascular diseases (CVDs). According to previous studies, CVDs are associated with increased cyclooxygenase 2 (COX-2) levels. However, the mechanisms by which CdCl2-induced COX-2 overexpression leads to cardiovascular dysfunction remain unclear. Herein, we show that the relative gene expressions of VEGF and PTGS2 (COX-2 encoding gene) are positively correlated in CVDs patie...
Source: Biochemical Pharmacology - August 8, 2020 Category: Drugs & Pharmacology Authors: Che L, Wu ZL, Huang LY, Wu JS, Du ZB, Lin JX, Su YH, Chen XX, Lin ZN, Lin YC Tags: Biochem Pharmacol Source Type: research

Rosmarinic acid inhibits oxLDL-induced inflammasome activation under high-glucose conditions through downregulating the p38-FOXO1-TXNIP pathway.
In this study, we aimed to investigate the protective effect of rosmarinic acid against diabetic atherosclerosis and the related signaling pathway. oxLDL-mediated oxidative stress upregulated thioredoxin-interacting protein (TXNIP) and subsequently induced binding of TXNIP to NLRP3 to mediate NLRP3 inflammasome assembly and activation under HG conditions in ECs. Reactive oxygen species (ROS) scavengers, p38 and FOXO1 inhibitors and TXNIP siRNA inhibited TXNIP protein upregulation and NLRP3 inflammasome assembly and activation. Rosmarinic acid abrogated TXNIP protein upregulation and the interaction between TXNIP and NLRP3 ...
Source: Biochemical Pharmacology - September 30, 2020 Category: Drugs & Pharmacology Authors: Baptiste Nyandwi J, Shin Ko Y, Jin H, Pil Yun S, Won Park S, Jung Kim H Tags: Biochem Pharmacol Source Type: research

3-Deazaadenosine, an S-adenosylhomocysteine hydrolase inhibitor, attenuates lipopolysaccharide-induced inflammatory responses via inhibition of AP-1 and NF- κB signaling.
In this study, we investigated the inhibitory activity and molecular mechanisms of 3-DA in inflammatory responses. 3-DA suppressed the secretion of inflammatory mediators such as nitric oxide (NO) and prostaglandin E2 (PGE2) in lipopolysaccharide-treated RAW264.7 cells and phorbol 12-myristate 13-acetate (PMA)-differentiated U937 cells. It also reduced mRNA expression of inducible nitric oxide synthase, cyclooxygenase-2, tumor necrosis factor-α, interleukin-1β (IL-1 β), and IL-6, indicating that 3-DA has anti-inflammatory properties in murine and human macrophages. Moreover, 3-DA strongly blocked AP-1 and NF-κB lucifer...
Source: Biochemical Pharmacology - October 6, 2020 Category: Drugs & Pharmacology Authors: Seok Yang W, Hye Kim J, Jeong D, Han Hong Y, Hee Park S, Yang Y, Jang YJ, Kim JH, Youl Cho J Tags: Biochem Pharmacol Source Type: research

The anti-melanogenic effects of ellagic acid through induction of autophagy in melanocytes and suppression of UVA-activated α-MSH pathways via Nrf2 activation in keratinocytes.
In conclusion, ellagic acid is an effective skin-whitening agent and might be used as a topical applicant. PMID: 33545118 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - February 2, 2021 Category: Drugs & Pharmacology Authors: Yang HL, Lin CP, Vudhya Gowrisankar Y, Huang PJ, Chang WL, Shrestha S, Hseu YC Tags: Biochem Pharmacol Source Type: research

Shear stress inhibits cardiac microvascular endothelial cells apoptosis to protect against myocardial ischemia reperfusion injury via YAP/miR-206/PDCD4 signaling pathway
In this study, we investigated the mechanism of shear stress in microvascular I/R injury, and try to elucidate the downstream signaling pathways that inhibit CMECs apoptosis to reduce I/R injury. Our results demonstrated that shear stress inhibited the apoptosis protein, increased PECAM-1 expression and eNOS phosphorylation in hypoxia reoxygenated (H/R) CMECs. The mechanism of shear stress was related to up-regulated expression of YAP, the increased number of YAP entering the nucleus by dephosphorylation, the reduced number of TUNEL positive cells, increased miR-206 and inhibited protein level of PDCD4 in CMECs. However, s...
Source: Biochemical Pharmacology - February 21, 2021 Category: Drugs & Pharmacology Authors: Qianlong Zhang Yonggang Cao Yongsheng Liu Wei Huang Jing Ren Peng Wang Chao Song Kai Fan Lina Ba Lixin Wang Hongli Sun Source Type: research

Resveratrol enhances transintestinal cholesterol excretion through selective activation of intestinal liver X receptor alpha
In conclusion, RSV could decrease circulating cholesterol levels through enhancing TICE and limiting cholesterol absorption via selective activation of intestinal LXRα.PMID:33631191 | DOI:10.1016/j.bcp.2021.114481
Source: Biochemical Pharmacology - February 25, 2021 Category: Drugs & Pharmacology Authors: Juan Pang Huihui Xu Xu Wang Xu Chen Qing Li Qiannan Liu Yiran You Hanyue Zhang Zhongliang Xu Yimin Zhao Yinghui Zhang Yan Yang Wenhua Ling Source Type: research

Tetrahydroxystilbene glycoside improves endothelial dysfunction and hypertension in obese rats: the role of omentin-1
CONCLUSIONS: Down-regulation of omentin-1 induces endothelial dysfunction and hypertension in obesity. TSG treatment (at least partially) increases omentin-1 via promoting binding of PPAR-γ and Itln-1 promoter in adipose tissues, subsequently exerts protective effects on endothelial function via activating Akt/eNOS/NO signaling and attenuating oxidative/nitrative stress. These results suggest that TSG could be developed as a promising anti-hypertension agent that protects against endothelial dysfunction and obesity-associated cardiovascular diseases.PMID:33647262 | DOI:10.1016/j.bcp.2021.114489
Source: Biochemical Pharmacology - March 1, 2021 Category: Drugs & Pharmacology Authors: Qianqian Dong Wenjuan Xing Kaifeng Li Xuanxuan Zhou Siwang Wang Haifeng Zhang Source Type: research