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Source: Biochemical Pharmacology

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Total 204 results found since Jan 2013.

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

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

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

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

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

Ginsenoside Rg5 induces G2/M phase arrest, apoptosis and autophagy via regulating ROS-mediated MAPK pathways against human gastric cancer.
In this study, Rg5 could suppress cell proliferation by causing G2/M phase arrest. Treatment with Rg5 could induce apoptosis through the extrinsic death receptor and intrinsic mitochondrial pathways. Autophagy induction was demonstrated by the formation of autophagosomes and autophagy-related proteins. Rg5-induced cell death was drastically restored by the autophagy inhibitor 3-MA and apoptosis inhibitor Z-VAD-FMK. Moreover, the suppression of apoptosis weakened Rg5-induced autophagy, while the inhibition of autophagy attenuated Rg5-induced apoptosis. Further studies revealed that Rg5 induced ROS production and activated M...
Source: Biochemical Pharmacology - July 9, 2019 Category: Drugs & Pharmacology Authors: Liu Y, Fan D Tags: Biochem Pharmacol Source Type: research

Systemic delivery of Eg5 shRNA-expressing plasmids using PEGylated DC-Chol/DOPE cationic liposome: long-term silencing and anticancer effects in vivo.
Abstract Duration of gene silencing due to the short-term silencing effects induced by exogenous siRNA have limited the therapeutic applications of RNAi and the development of RNAi-based therapeutics. We here generated Eg5 shRNA-expressing plasmids using the inverted terminal repeats (ITRs) sequences to produce Eg5 hairpin RNA under the control of U6 promoter. Using PEGylated DC-Chol/DOPE cationic liposomes, we demonstrated that a single systemic administration of Eg5 shRNA-expressing plasmid/liposome lipoplexes induced the long-term Eg5 silencing in the tumor sites of tumor-bearing mice, and ultimately lead to mo...
Source: Biochemical Pharmacology - May 22, 2019 Category: Drugs & Pharmacology Authors: Seraj S, Lee J, Ahn HJ Tags: Biochem Pharmacol Source Type: research

Magnesium isoglycyrrhizinate ameliorates fructose-induced podocyte apoptosis through downregulation of miR-193a to increase WT1.
In this study, we found that MgIG significantly alleviated kidney dysfunction, proteinuria and podocyte injury in fructose-fed rats. It also restored fructose-induced podocyte apoptosis in rat glomeruli and cultured differentiated podocytes. Of note, high-expression of miR-193a, downregulation of Wilms' tumor protein (WT1) and RelA, as well as upregulation of C-Maf inducing protein (C-mip) were observed in these animal and cell models. The data from the transfection of miR-193a mimic, miR-193a inhibitor, WT1 siRNA or LV5-WT1 in cultured differentiated podocytes showed that fructose increased miR-193a to down-regulate WT1, ...
Source: Biochemical Pharmacology - May 10, 2019 Category: Drugs & Pharmacology Authors: Li TS, Chen L, Wang SC, Yang YZ, Xu HJ, Gu HM, Zhao XJ, Dong P, Pan Y, Shang ZQ, Zhang XQ, Kong LD Tags: Biochem Pharmacol Source Type: research

The in vitro and in vivo depigmenting activity of Coenzyme Q10 through the down-regulation of α-MSH signaling pathways and induction of Nrf2/ARE-mediated antioxidant genes in UVA-irradiated skin keratinocytes.
Abstract Coenzyme CoQ10 (CoQ10), a ubiquinone compound, has been reported to inhibit tyrosinase activity and melanin production in melanoma B16F10 cells. However, the molecular mechanism underlying this inhibitory effect is poorly understood. In this paper we aimed to investigate the molecular mechanisms involved in the anti-melanogenic activity of CoQ10 (1-2 μM) in UVA (5 J/cm2)-irradiated keratinocyte HaCaT cells and α-MSH stimulated B16-F10 cells. It was observed that CoQ10 suppressed p53/POMC, α-MSH production as well as inhibited ROS generation in UVA-irradiated keratinocyte HaCaT cells. CoQ10 down-regulat...
Source: Biochemical Pharmacology - April 12, 2019 Category: Drugs & Pharmacology Authors: Hseu YC, Ho YG, Mathew DC, Yen HR, Chen XZ, Yang HL Tags: Biochem Pharmacol Source Type: research

FCPR03, a novel phosphodiesterase 4 inhibitor, alleviates cerebral ischemia/reperfusion injury through activation of the AKT/GSK3 β/ β-catenin signaling pathway.
This study aimed to investigate the effects of FCPR03 on neuronal injury after cerebral ischemia/reperfusion and the underlying signaling pathway. The effects of FCPR03 on cellular apoptosis, intracellular accumulation of reactive oxygen species (ROS), and mitochondrial membrane potential (MMP) were evaluated in HT-22 neuronal cells and cortical neurons exposed to oxygen-glucose deprivation (OGD). The impact of FCPR03 on brain injury, neurological scores and behavioral performance was investigated in rats subjected to middle cerebral artery occlusion (MCAO). The protein kinase B (AKT) inhibitor MK-2206 and β-catenin siRNA...
Source: Biochemical Pharmacology - February 21, 2019 Category: Drugs & Pharmacology Authors: Xu B, Wang T, Xiao J, Dong W, Wen HZ, Wang X, Qin Y, Cai N, Zhou Z, Xu J, Wang H Tags: Biochem Pharmacol Source Type: research

Piperlongumine-induced nuclear translocation of the FOXO3A transcription factor triggers BIM-mediated apoptosis in cancer cells.
We report here that an association of FOXO3A with the pro-apoptotic protein BIM (also known as BCL2-like 11, BCL2L11) has a direct and specific function in PL-induced cancer cell death. Using HeLa cells stably expressing a FOXO3A-GFP fusion protein and several other cancer cell lines, we found that PL treatment induces FOXO3A dephosphorylation and nuclear translocation and promotes its binding to the BIM gene promoter, resulting in the up-regulation of BIM in the cancer cell lines. Accordingly, PL inhibited cell viability and caused intrinsic apoptosis in a FOXO3A-dependent manner. Of note, siRNA-mediated FOXO3A knockdown ...
Source: Biochemical Pharmacology - February 9, 2019 Category: Drugs & Pharmacology Authors: Liu Z, Shi Z, Lin J, Zhao S, Hao M, Xu J, Li Y, Zhao Q, Tao L, Diao A Tags: Biochem Pharmacol Source Type: research

Gelsemine and koumine, principal active ingredients of Gelsemium, exhibit mechanical antiallodynia via spinal glycine receptor activation-induced allopregnanolone biosynthesis.
Abstract Gelsemine, the principal active alkaloid from Gelsemium sempervirens Ait., and koumine, the most dominant alkaloids from Gelsemium elegans Benth., produced antinociception in a variety of rodent models of painful hypersensitivity. The present study explored the molecular mechanisms underlying gelsemine- and koumine-induced mechanical antiallodynia in neuropathic pain. The radioligand binding and displacement assays indicated that gelsemine and koumine, like glycine, were reversible and orthosteric agonists of glycine receptors with full efficacy and probably acted on same binding site as the glycine recep...
Source: Biochemical Pharmacology - January 19, 2019 Category: Drugs & Pharmacology Authors: Shoaib RM, Zhang JY, Mao XF, Wang YX Tags: Biochem Pharmacol Source Type: research

An N6-methyladenosine at the transited codon 273 of p53 pre-mRNA promotes the expression of R273H mutant protein and drug resistance of cancer cells.
This study uncovers a novel function of pre-mRNA m6A as a determinant of mutant protein expression in cancer cells heterozygously carrying the TP53 R273H mutation. Suppressing both RNA methylation and ceramide glycosylation might constitute an efficacious and specific approach for targeting TP53 missense mutations coding for a G>A transition, thereby improving cancer treatments. PMID: 30578766 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - December 19, 2018 Category: Drugs & Pharmacology Authors: Uddin MB, Roy KR, Hosain SB, Khiste SK, Hill RA, Jois SD, Zhao Y, Tackett AJ, Liu YY Tags: Biochem Pharmacol Source Type: research

RNA interference screen identifies NAA10 as a regulator of PXR transcription.
Abstract The pregnane X receptor (PXR) is a principal xenobiotic receptor crucial in the detection, detoxification, and clearance of toxic substances from the body. PXR plays a vital role in the metabolism and disposition of drugs, and elevated PXR levels contribute to cancer drug resistance. Therefore, to modulate PXR activity and mitigate drug resistance, it is imperative to fully understand its regulation. To this end, we screened a transcription factor siRNA library in pancreatic cancer cells that express high levels of PXR. Through a comprehensive deconvolution process, we identified N-alpha-acetyltransferase...
Source: Biochemical Pharmacology - December 16, 2018 Category: Drugs & Pharmacology Authors: Oladimeji PO, Wright WC, Wu J, Chen T Tags: Biochem Pharmacol Source Type: research

3-dehydroandrographolide protects against lipopolysaccharide-induced inflammation through the cholinergic anti-inflammatory pathway.
In this study, murine macrophage RAW 264.7 cells and BALB/c mice were treated with LPS (lipopolysaccharide, 100 ng/ml in vitro; 3 mg/kg, intratracheal) to establish inflammation models. 3-DA attenuated the release of pro-inflammatory cytokines IL-6 and TNF-α, inhibited the degradation and phosphorylation of IκBα, and suppressed the nuclear translocation of NF-κB p65 as well as the phosphorylation of Akt at Ser473 in LPS-stimulated RAW 264.7 macrophage cells. Furthermore, 3-DA increased α7nAchR expression level and bound with α7nAchR. More importantly, the anti-inflammatory effects of 3-DA were counteracted in the pre...
Source: Biochemical Pharmacology - November 1, 2018 Category: Drugs & Pharmacology Authors: Lu Z, Xie P, Zhang D, Sun P, Yang H, Ye J, Cao H, Huo C, Zhou H, Chen Y, Ye W, Yu L, Liu J Tags: Biochem Pharmacol Source Type: research