Filtered By:
Source: Biochemical Pharmacology

This page shows you your search results in order of date. This is page number 9.

Order by Relevance | Date

Total 204 results found since Jan 2013.

A novel selenonucleoside suppresses tumor growth by targeting Skp2 degradation in paclitaxel-resistant prostate cancer.
In this study, the antitumor activity of a novel selenonucleoside (4'-selenofuranosyl-2,6-dichloropurine, LJ-2618), a third-generation nucleoside, and its plausible mechanisms of action in paclitaxel-resistant prostate cancer (PC-3-Pa) cells were investigated. The established PC-3-Pa cells exhibited over 100-fold resistance against paclitaxel compared to the paclitaxel-sensitive PC-3 cells. LJ-2618, however, effectively inhibited the proliferation of both cell lines with similar IC50 values in vitro. In PC-3-Pa cells, the activated PI3K/Akt signaling pathway was suppressed by LJ-2618 treatment. In addition, Skp2 was found ...
Source: Biochemical Pharmacology - October 4, 2018 Category: Drugs & Pharmacology Authors: Byun WS, Jin M, Yu J, Kim WK, Song J, Chung HJ, Jeong LS, Lee SK Tags: Biochem Pharmacol Source Type: research

Smiglaside A ameliorates LPS-induced acute lung injury by modulating macrophage polarization via AMPK-PPAR γ pathway.
In this study, we evaluated the effects of the natural product smiglaside A, a phenylpropanoid glycoside isolated from the traditional Chinese medicinal herb Smilax riparia, on macrophage polarization and investigated the underlying mechanisms. We found that smiglaside A promoted M2 polarization and reduced M1 polarization in LPS-stimulated RAW264.7 cells and primary mouse peritoneal macrophages. Further mechanistic studies showed that the promoting effect of smiglaside A on M2 polarization was attenuated by pharmacological inhibition or gene silencing of AMP-activated protein kinase (AMPK) or peroxisome proliferator-activ...
Source: Biochemical Pharmacology - September 6, 2018 Category: Drugs & Pharmacology Authors: Wang Y, Xu Y, Zhang P, Ruan W, Zhang L, Yuan S, Pang T, Jia AQ Tags: Biochem Pharmacol Source Type: research

Immunization with Na+/K+ ATPase DR peptide prevents bone loss in an ovariectomized rat osteoporosis model.
Abstract Osteoporosis is characterized by decreased bone strength and microarchitectural deterioration of bone tissue leading to an increase in bone fracture. Here we report a new agent named DR peptide, a conserved sequence of Na+/K+ ATPase (NKA), can be used to prevent osteoporosis. Our results showed that immunization with DR peptide conjunct with Keyhole limpet hemocyanin (DR-KLH) significantly strengthened trabecular bone and improved bone mineral density of femur and the 5th lumbar in the ovariectomized (OVX) rats when compared with those in OVX rats immunized with KLH alone. To study the underlying mechanis...
Source: Biochemical Pharmacology - August 19, 2018 Category: Drugs & Pharmacology Authors: Xiong S, Yang X, Yan X, Hua F, Zhu M, Guo L, Wu Z, Bian JS Tags: Biochem Pharmacol Source Type: research

Salidroside alleviates Ischemic Brain Injury in Mice with Ischemic Stroke through regulating BDNK mediated PI3K/Akt Pathway.
In this study, We preformed MCAO model in C57BL/6J wild-type (BDNK+/+) and BDNK knockout (BDNF-/-) mice respectively, and investigated the neuroprotective effect of Salidroside (Sal) and its underlying mechanisms. The results showed that Sal reversed brain infarct size, reduced cerebral edema, decreased the neurological deficit score and diminished TUNEL positive cells significantly. However, BDNK deficiency inhibited the neuroprotective effect of Sal. In addition, Sal increased cell viability, ameliorated neuron cell injury by decreasing LDH activity, and inhibited cell apoptotic rate. Sal suppressed apoptotic signaling v...
Source: Biochemical Pharmacology - August 13, 2018 Category: Drugs & Pharmacology Authors: Zhang X, Du Q, Yang Y, Wang J, Liu Y, Zhao Z, Zhu Y, Liu C Tags: Biochem Pharmacol Source Type: research

Biphasic modulation of cAMP levels by the contraceptive nomegestrol acetate. Impact on P-glycoprotein expression and activity in hepatic cells.
Abstract ABC transporters are key players in drug excretion with alterations in their expression and activity by therapeutic agents potentially leading to drug-drug interactions. The interaction potential of nomegestrol acetate (NMGA), a synthetic progestogen increasingly used as oral contraceptive, had never been explored. In this work we evaluated (1) the effect of NMGA on ABC transporters in the human hepatic cell line HepG2 and (2) the underlying molecular mechanism. NMGA (5, 50 and 500 nM) increased P-glycoprotein (P-gp) expression at both protein and mRNA levels and reduced intracellular calcein accumulation...
Source: Biochemical Pharmacology - April 20, 2018 Category: Drugs & Pharmacology Authors: Tocchetti GN, Domínguez CJ, Zecchinati F, Arana MR, Ruiz ML, Villanueva SSM, Weiss J, Mottino AD, Rigalli JP Tags: Biochem Pharmacol Source Type: research

Tanshinone IIA suppresses Fc εRI-mediated mast cell signaling and anaphylaxis by activation of the Sirt1/LKB1/AMPK Pathway.
In conclusion, Tan IIA suppresses FcεRI-mediated mast cell activation and anaphylaxis through activation of the inhibitory Sirt1-LKB1-AMPK pathway. Thus, Tan IIA may be useful as a new therapeutic agent for mast cell-mediated allergic diseases. PMID: 29674003 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - April 16, 2018 Category: Drugs & Pharmacology Authors: Li X, Park SJ, Jin F, Deng Y, Yang JH, Chang JH, Kim DY, Kim JA, Lee YJ, Murakami M, Son KH, Chang HW Tags: Biochem Pharmacol Source Type: research

Anti-tumour effects of beta-sitosterol are mediated by AMPK/PTEN/HSP90 axis in AGS human gastric adenocarcinoma cells and xenograft mouse models.
Abstract We investigated the anti-cancer effects of beta-sitosterol (BS), a plant-derived sterol in AGS human gastric adenocarcinoma cells and xenograft mouse models. BS significantly reduced cell viability by inducing apoptosis in AGS adenocarcinoma cells. This was accompanied by the formation of apoptotic bodies, as detected by Annexin V, caspase 3/7 activity, and MitoPotential assay. BS stimulated phosphatase and tensin homolog (PTEN) and phospho-AMP-activated protein kinase (p-AMPK) expression. Pharmacological inhibitors or siRNA were used to further analyse the relationship between the two proteins. AMPK was ...
Source: Biochemical Pharmacology - March 17, 2018 Category: Drugs & Pharmacology Authors: Shin EJ, Choi HK, Sung MJ, Park JH, Chung MY, Chung S, Hwang JT Tags: Biochem Pharmacol Source Type: research

BMP-2 induces angiogenesis by provoking integrin α6 expression in human endothelial progenitor cells.
In this study, we found that BMP-2 promoted cell migration and tube formation of EPCs in a concentration-dependent manner, indicating BMP-2 induced in vitro angiogenesis in human EPCs. Furthermore, BMP-2 significantly increased microvessel formation in Matrigel plug assay, and BMP-2 antagonist noggin prevented BMP-2-induced in vivo angiogenesis. Mechanistic investigations showed BMP-2 profoundly induced the expression of Id-1 and integrinα6 as well as EPCs angiogenesis by activating PI3K/Akt and MEK/Erk signaling pathways. Moreover, knockdown of Id-1 and integrin α6 by siRNA transfection obviously attenuated BMP-2-induec...
Source: Biochemical Pharmacology - February 16, 2018 Category: Drugs & Pharmacology Authors: Chen WC, Chung CH, Lu YC, Wu MH, Chou PH, Yen JY, Lai YW, Wang GS, Liu SC, Cheng JK, Wu YJ, Yeh HI, Wang LY, Wang SW 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

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

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

Heme oxygenase-1 induction by rosiglitazone via PKC α/AMPKα/p38 MAPKα/SIRT1/PPARγ pathway suppresses lipopolysaccharide-mediated pulmonary inflammation.
In this study, we found that upregulation of HO-1 in vitro or in vivo by rosiglitazone attenuated VCAM-1 gene expression and monocyte adhesion to HPAEpiCs challenged with lipopolysaccharide (LPS). The inhibitory effects of rosiglitazone on LPS-mediated responses were reversed by transfection with HO-1 siRNA. LPS-induced VCAM-1 expression was mediated through NF-κB activation which was attenuated by rosiglitazone via suppressing p65 activation and translocation into the nucleus. Moreover, pretreatment with the inhibitor of PKCs (H7), PKCα (Gö6976), AMPKα (Compound C), p38 MAPKα (p38i VIII), SIRT1 (Sirtinol), or PPARγ ...
Source: Biochemical Pharmacology - January 5, 2018 Category: Drugs & Pharmacology Authors: Cho RL, Lin WN, Wang CY, Yang CC, Hsiao LD, Lin CC, Yang CM 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

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

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