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Source: Biochemical Pharmacology

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Total 204 results found since Jan 2013.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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