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Source: Biochemical Pharmacology

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Total 204 results found since Jan 2013.

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

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

Metformin-conjugated micellar system with intratumoral pH responsive de-shielding for co-delivery of doxorubicin and nucleic acid.
Abstract A novel PMet-P(cdmPEG2K) polymeric micellar carrier was developed for tumor-targeted co-delivery of DOX and nucleic acids (NA), based on polymetformin and a structure designed to lose the PEG shell in response to the acidic extracellular tumor environment. NA/DOX co-loaded micelleplexes exhibited enhanced inhibition of cell proliferation compared to DOX-loaded micelles, and displayed a higher level of cytotoxicity at an acidic pH (6.8) which mimicks the tumor microenvironment. The PMet-P(cdmPEG2K) micelles achieved significantly improved transfection with either a reporter plasmid or Cy3-siRNA, and enhanc...
Source: Biochemical Pharmacology - February 2, 2021 Category: Drugs & Pharmacology Authors: Liu Y, Sun J, Huang Y, Chen Y, Li J, Liang L, Xu J, Wan Z, Zhang B, Li Z, Li S 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

The growth of siRNA-based therapeutics: updated clinical studies.
Abstract More than two decades after the natural gene-silencing mechanism of RNA interference was elucidated, small interfering RNA (siRNA)-based therapeutics have finally broken into the pharmaceutical market. With three agents already approved and many others in advanced stages of the drug development pipeline, siRNA drugs are on their way to becoming a standard modality of pharmacotherapy. The majority of late-stage candidates are indicated for rare or orphan diseases, whose patients have an urgent need for novel and effective therapies. Additionally, there are agents that have the potential to meet the need of...
Source: Biochemical Pharmacology - January 26, 2021 Category: Drugs & Pharmacology Authors: Zhang MM, Bahal R, Rasmussen TP, Manautou JE, Zhong XB Tags: Biochem Pharmacol Source Type: research

Prolonged cultured human hepatocytes as an in vitro experimental system for the evaluation of potency and duration of activity of RNA therapeutics: Demonstration of prolonged duration of gene silencing effects of a GalNAc-conjugated human hypoxanthine phosphoribosyl transferase (HPRT1) siRNA.
We report here the evaluation of a novel in vitro experimental model, prolonged cultured human hepatocytes (PCHC), as an experimental system to evaluate the potency and duration of effects of oligonucleotide therapeutics. A novel observation was made on the redifferentiation of PCHC upon prolonged culturing based on mRNA profiling of characteristic hepatic differentiation marker genes albumin, transferrin, and transthyretin. Consistent with the known de-differentiation of cultured human hepatocytes, decreases in marker gene expression were observed upon culturing of the hepatocytes for 2 days. A novel observation of re-dif...
Source: Biochemical Pharmacology - December 21, 2020 Category: Drugs & Pharmacology Authors: Yang Q, Humphreys SC, Lade JM, Li AP Tags: Biochem Pharmacol Source Type: research

AMPK upregulates KCa2.3 channels and ameliorates endothelial dysfunction in diet-induced obese mice.
Abstract The opening of endothelial small-conductance calcium-activated potassium channels (KCa2.3) is essential for endothelium-dependent hyperpolarization (EDH), which predominantly occurs in small resistance arteries. Adenosine monophosphate-activated protein kinase (AMPK), an important metabolic regulator, has been implicated in regulating endothelial nitric oxide synthase activity. However, it was unclear whether AMPK regulated endothelial KCa2.3-mediated EDH-type vasodilation. Using bioinformatics analysis and myograph system, we investigated the regulation by AMPK of KCa2.3 in human umbilical vein endotheli...
Source: Biochemical Pharmacology - November 10, 2020 Category: Drugs & Pharmacology Authors: Pang ZD, Wang Y, Song Z, She G, Ma XZ, Sun X, Wu W, Lai BC, Zhang J, Zhang Y, Du XJ, Shyy JYJ, Deng XL 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

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

Antisense Drug Discovery and Development Technology Considered in a Pharmacological Context.
Abstract When coined, the term "antisense" included oligonucleotides of any structure, with any chemical modification and designed to work through any post-RNA hybridization mechanism. However, in practice the term "antisense" has been used to describe single stranded oligonucleotides (ss ASOs) designed to hybridize to RNAswhile the term "siRNA" has come to mean double stranded oligonucleotides designed to activate Ago2. However, the two approaches share many common features. The medicinal chemistry developed for ASOs greatly facilitated the development of siRNA technology and remains the chemical basis for both a...
Source: Biochemical Pharmacology - August 11, 2020 Category: Drugs & Pharmacology Authors: Crooke ST, Liang XH, Crooke RM, Baker BF, Geary RS 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

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

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

α-Linolenic acid inhibits the migration of human triple-negative breast cancer cells by attenuating twist1 expression and suppressing twist1-mediated epithelial-mesenchymal transition.
Abstract α-Linolenic acid (ALA), an essential fatty acid, has anticancer activity in breast cancer, but the mechanism of its effects in triple-negative breast cancer (TNBC) remains unclear. We investigated the effect of ALA on Twist1, which is required to initiate epithelial-mesenchymal transition (EMT) and promotes tumor metastasis, and Twist1-mediated migration in MDA-MB231, MDA-MB468 and Hs578T cells. Twist1 protein was constitutively expressed in these TNBC cells, particularly MDA-MB-231 cells. Treatment with 100 uM ALA and Twist1 siRNA markedly decreased the Twist1 protein level and cell migration. Moreover,...
Source: Biochemical Pharmacology - July 13, 2020 Category: Drugs & Pharmacology Authors: Wang SC, Sun HL, Hsu YH, Liu SH, Lii CK, Tsai CH, Liu KL, Huang CS, Li CC 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