7,885 results match your criteria Chemico-biological interactions[Journal]


Suppression of BACE1 and amyloidogenic/RAGE axis by sitagliptin ameliorates PTZ kindling-induced cognitive deficits in rats.

Chem Biol Interact 2020 Jul 9:109144. Epub 2020 Jul 9.

Pharmacology and Toxicology Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

The debilitating nature of cognitive impairment in epilepsy and the potential of some traditional antiepileptics to further deteriorate cognitive function are areas of growing concern. Glucagon-like peptide-1 (GLP-1) deficiency has been linked to reduced seizure threshold as well as cognitive dysfunction. Here, we tested whether sitagliptin (SITA), by virtue of its neuroprotective properties, could alleviate both epilepsy and associated cognitive dysfunction in a rat model of kindling epilepsy. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109144DOI Listing

BAY60-2770 attenuates doxorubicin-induced cardiotoxicity by decreased oxidative stress and enhanced autophagy.

Chem Biol Interact 2020 Jul 8:109190. Epub 2020 Jul 8.

Division of Cardiology, Department of Internal Medicine, Kyung Hee University Hospital, Kyung Hee University, Seoul, South Korea. Electronic address:

Background: Doxorubicin (DOX) administration decreases cardiac soluble guanylate cyclase (sGC) activity. We hypothesized that bypassing impaired NO-sGC-cGMP pathway resulting from the activation of oxidized and heme-free soluble guanylate cyclase (sGC) could be a therapeutic target for DOX-mediated cardiomyopathy (DOX-CM). The present study investigated the therapeutic roles and mechanism of BAY60-2770, an activator of oxidized sGC, in alleviating DOX-CM. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109190DOI Listing

Prioritizing aromatic amines for biomonitoring studies.

Chem Biol Interact 2020 Jul 8:109191. Epub 2020 Jul 8.

Medantox LLC, Pittsburgh, PA, 15241, USA; ReNeuroGen LLC, Elm Grove, WI, 53122, USA.

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http://dx.doi.org/10.1016/j.cbi.2020.109191DOI Listing
July 2020
2.577 Impact Factor

Di-n-butyl phthalate exposure induced abnormal autophagy in renal tubular cells via hedgehog signaling in newborn rats.

Chem Biol Interact 2020 Jul 2:109189. Epub 2020 Jul 2.

Department of Urology, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, 200080, China. Electronic address:

Di-n-butyl phthalate (DBP) is a pollutant that is widely present in the environment. We have previously demonstrated that maternal exposure to DBP resulted in renal fibrosis in offspring, but the underlying mechanism was not well elucidated. Therefore, the current study aims to understand the underlying molecular mechanisms in these sex-specific developmental alterations. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109189DOI Listing

Cytotoxicity of juglone and thymoquinone against pancreatic cancer cells.

Chem Biol Interact 2020 Jun 28:109142. Epub 2020 Jun 28.

School of Nutrition and Food Sciences, Louisiana State University, Baton Rouge, LA, 70803, USA. Electronic address:

Juglone and thymoquinone are cytotoxic to pancreatic cancer cells. The aim of this study was to investigate, using an analysis of isobolograms, the type and degree of interactions between juglone and thymoquinone on MIA PaCa-2 pancreatic cancer cells. Cell viability was evaluated using the MTT assay. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109142DOI Listing

Folic acid and RAAS blockers in ischemia/reperfusion-induced hepatic injury: A current mechanistic concept for understanding the incidence, significance & outcome.

Chem Biol Interact 2020 Jun 28:109187. Epub 2020 Jun 28.

Department of Anesthesiology, The First Hospital of Jilin University, Xinmin Street, Changchun, China. Electronic address:

Hepatic ischemia-reperfusion injury (IRI) is not only one of the pathophysiological process involving the liver, but also a complex systemic process affecting multiple tissues and organs. IRI after liver transplant occurs due to in major resections and occlusion of vessels, or during the perioperative period, leads to acute liver failure which shows the dynamic process that involves two interrelated phases of local ischemic insult and inflammation-mediated reperfusion injury and has an impact on morbidity and mortality. The renin-angiotensin-aldosterone system (RAAS) is activated locally in the injured cells by the occurrence of I/R, which plays an essential role in the fate of the damaged tissue. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109187DOI Listing

Anti-diabetic and lipid-lowering effects of drimane sesquiterpenoids isolated from Zygogynum pancheri.

Chem Biol Interact 2020 Jun 27:109167. Epub 2020 Jun 27.

Laboratory of Organic Chemistry (LR17-ES08), Natural Substances Team, University of Sfax, Faculty of Sciences of Sfax, PB « 1171 », PC « 3000 », Sfax, Tunisia.

Recently, it has been shown that drimane-type sesquiterpenoids isolated from Zygogynum pancheri, a species native to New Caledonia, possessed significant α-amylase inhibitory activities. To further explore their antidiabetic potential, we investigated the effect of 1β-O-(E-cinnamoyl)-6α-hydroxy-9epi-polygodial (D) and 1β-E-O-p-methoxycinnamoyl-bemadienolide (L), two of the most active compounds of the series, on diabetic model rats. Compounds D and L (2 mg kg/day) were daily and orally administrated for 30 days to streptozotocin (STZ) (150 mg/kg) induced male diabetic Wistar rats. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109167DOI Listing

Sappanchalcone, a flavonoid isolated from Caesalpinia sappan L., induces caspase-dependent and AIF-dependent apoptosis in human colon cancer cells.

Chem Biol Interact 2020 Jun 23:109185. Epub 2020 Jun 23.

Department of Biomedical Science, Daegu Catholic University, Gyeongsan-Si, Republic of Korea. Electronic address:

The present study examined the apoptotic effects and the underlying mechanism of sappanchalcone, a major bioactive compound isolated from Caesalpinia sappan L., on human colon cancer cells. To achieve this, we used two different colon cancer cell lines, namely HCT116 (as wild-type p53 cells) and SW480 (as p53-mutant cells) cells. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109185DOI Listing

FB-15 inhibits MGC-803 cells growth by regulating energy metabolism.

Chem Biol Interact 2020 Jun 23:109186. Epub 2020 Jun 23.

Institute of Pharmacy and Pharmacology, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China, Hengyang City, Hunan Province, PR China; Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Hengyang City, Hunan Province, PR China. Electronic address:

In this study, we scrutinized the anticancer effects of FB-15 on human gastric carcinoma MGC-803 cells in vitro and vivo, and its preliminary effect on tubulin and HIF-1α. We confirmed that FB-15 not only inhibited the proliferation of a large number of cells in a concentration and time-dependent manner but also inhibited proliferation of a single cell to form clones. FB-15 manifested little cytotoxicity for normal stomach cells GES-1. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109186DOI Listing

Scoulerine promotes cell viability reduction and apoptosis by activating ROS-dependent endoplasmic reticulum stress in colorectal cancer cells.

Chem Biol Interact 2020 Jun 23:109184. Epub 2020 Jun 23.

Department of Colorectal Surgery, Cancer Hospital of China Medical University, Liaoning Cancer Hospital and Institute, Shenyang, 110042, China. Electronic address:

Scoulerine, an isoquinoline alkaloid isolated from Corydalis plants, has been reported to possess potent anti-proliferative and pro-apoptotic function in cancer cells. However, the effects and underlying mechanisms of scoulerine on colorectal cancer (CRC) progression remain elusive. CCK-8 and LDH assays were used to evaluate cell viability. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109184DOI Listing

Carvedilol attenuates l-arginine induced acute pancreatitis in rats through modulation of oxidative stress and inflammatory mediators.

Chem Biol Interact 2020 Jun 20;327:109181. Epub 2020 Jun 20.

Department of Pharmacology and Toxicology, Faculty of Pharmacy, Misr University for Science and Technology (MUST), 6th of October City, Giza, Egypt.

Acute pancreatitis (AP) is a sudden pancreatic inflammation accompanied by an excessive reactive oxygen species production that provokes inflammation. The present study investigated whether carvedilol can protect against l-arginine induced AP in a rat model and studied the mechanisms associated with its protection. Rats were divided into four groups: a control group, an AP group (injected with 2 doses of l-arginine 250 mg/100 g body weight at 1 h interval, intraperitoneally) on the 22nd day of the experiment, a carvedilol group (10 mg/kg, orally) for 21 successive days, and finally a carvedilol + AP group. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109181DOI Listing

Cyclosporine a induces testicular injury via mitochondrial apoptotic pathway by regulation of mir-34a and sirt-1 in male rats: The rescue effect of curcumin.

Chem Biol Interact 2020 Jun 20;327:109180. Epub 2020 Jun 20.

Nephrology and Kidney Transplant Research Center, Urmia University of Medical Sciences, Urmia, Iran; Department of Physiology, Faculty of Medicine, Urmia University of Medical Sciences, Urmia, Iran. Electronic address:

Testicular damage contributes to cyclosporine A (CsA) induced male infertility. However, the exact underlying molecular mediators involved in CsA-induced testis disorder remains unclear. The present study aimed to characterize the role of mir-34a/sirt-1 in CsA induced testicular injury alone or in combination with curcumin. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109180DOI Listing

Effect of CYP3A inducer/inhibitor on pharmacokinetics of five alkaloids in Evodiae Fructus.

Chem Biol Interact 2020 Jun 17;327:109146. Epub 2020 Jun 17.

School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning, 110016, China. Electronic address:

Evodiae Fructus (EF), the dried nearly mature scented fruit of Tetradium ruticarpum (A.Juss.) T. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109146DOI Listing

Melatonin regulates the expression of inflammatory cytokines, VEGF and apoptosis in diabetic retinopathy in rats.

Chem Biol Interact 2020 Jun 15;327:109183. Epub 2020 Jun 15.

Department of Morphology and Animal Physiology, Federal Rural University of Pernambuco, Recife, Brazil. Electronic address:

The present study analyzed whether melatonin could mediate the expression of VEGF, IL-6 and TNF-α, as well as the apoptotic index in rats with diabetic retinopathy. Fifty Wistar albino rats were divided into the following groups: GC: rats without induction of diabetes by streptozotocin; GD: rats induced to diabetes by streptozotocin and treated with placebo; GDM: rats induced to diabetes by streptozotocin and after confirmation treated with melatonin at a dose of 10 mg/kg for 20 days; GDMS: rats induced to diabetes by streptozotocin and treated simultaneously with melatonin at a dosage of 10 mg/kg for 20 days; GDI: rats induced to diabetes by streptozotocin and after confirmation treated with insulin for 20 days. Diabetes was induced by intraperitoneal injections of streptozotocin (60 mg/kg), and insulin (5 U/day) was administered subcutaneously. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109183DOI Listing

Nitric oxide and Ca-activated high-conductance K channels mediate nothofagin-induced endothelium-dependent vasodilation in the perfused rat kidney.

Chem Biol Interact 2020 Jun 15;327:109182. Epub 2020 Jun 15.

Laboratory of Electrophysiology and Cardiovascular Pharmacology, Faculty of Health Sciences, Universidade Federal da Grande Dourados, Dourados, MS, Brazil. Electronic address:

Nothofagin is a natural 3'-C-β-D-glucoside of the polyphenol phloretin that is mainly found in Aspalathus linearis, Nothofagus fusca, and Leandra dasytricha. In recent years, nothofagin has been described as a potential therapeutic agent for renal disorders, but the mechanisms that are involved in its renoprotective effects remain unclear. In the present study, perfused rat kidneys were used to test the hypothesis that nothofagin causes the direct relaxation of renal arteries. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109182DOI Listing

Tablysin-15 inhibits osteoclastogenesis and LPS-induced bone loss via attenuating the integrin αβ pathway.

Chem Biol Interact 2020 Jun 11;327:109179. Epub 2020 Jun 11.

Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China. Electronic address:

Excessive osteoclast leads to the imbalance in bone reconstruction and results in osteolytic diseases, such as osteoporosis and rheumatic arthritis. Integrin αβ abundantly expresses on osteoclast and plays a critical role in the formation and function of osteoclast, therefore, blockage of αβ has become an attractive therapeutic option for osteolytic diseases. In this study, we find that Tablysin-15, a RGD motif containing disintegrin, concentration-dependently suppresses RANKL-induced osteoclastogenesis, F-actin ring formation and bone resorption without affecting the cell viabilities. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109179DOI Listing

Roles of peroxisome proliferator-activated receptor α in the pathogenesis of ethanol-induced liver disease.

Chem Biol Interact 2020 Jun 11;327:109176. Epub 2020 Jun 11.

Institute of Toxicology, School of Public Health, Cheeloo College of Medicine, Shandong University, Jinan, Shandong, 250012, China. Electronic address:

Alcoholic liver disease (ALD) is a progressively aggravated liver disease with high incidence in alcoholics. Ethanol-induced fat accumulation and the subsequent lipopolysaccharide (LPS)-driven inflammation bring liver from reversible steatosis, to irreversible hepatitis, fibrosis, cirrhosis, and even hepatocellular carcinoma. Peroxisome proliferator-activated receptor α (PPARα) is a member of the nuclear receptor superfamily of ligand-activated transcription factors and plays pivotal roles in the regulation of fatty acid homeostasis as well as the inflammation control in the liver. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109176DOI Listing

Novel benzimidazole derivatives: Synthesis, in vitro cytotoxicity, apoptosis and cell cycle studies.

Chem Biol Interact 2020 Jun 12;327:109163. Epub 2020 Jun 12.

Giresun University, Faculty of Science and Art, Department of Chemistry, Giresun, Turkey.

The aim of the study was to synthesize a new series of benzimidazole derivatives and to investigate the underlying molecular mechanisms of the potential cell cycle inhibition and apoptotic effects against a panel of selected human cancer cell lines along with HEK-293 human embryonic kidney cells. MTT assay was used to evaluate cytotoxic effects. Muse™ Cell Analyzer was used to assess cell cycle progression. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109163DOI Listing

Research trends in chemico-biological interactions: The golden jubilee (1969-2019).

Chem Biol Interact 2020 Jun 10;327:109177. Epub 2020 Jun 10.

Departamento de Bioquímica e Biologia Molecular, Programa de Pós-Graduação Em Bioquímica Toxicológica, Universidade Federal de Santa Maria, Santa Maria, RS, 97105-900, Brazil.

Since its inception in 1969, Chemico-Biological Interactions (CBI) has persistently published high quality research articles. As part of the journal's golden anniversary (50 years), we performed an electronic search on Scopus to get all publications details. Based on citescore, ranking & percentile, CBI holds 21st position in the top 113 relevant journals (in 2018). Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109177DOI Listing
June 2020
2.577 Impact Factor

Gastroprotective effect of the alkaloid boldine: Involvement of non-protein sulfhydryl groups, prostanoids and reduction on oxidative stress.

Chem Biol Interact 2020 Jun 9:109166. Epub 2020 Jun 9.

Programa de Pós-Graduação Em Ciências Farmacêuticas (PPGCF), Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí (UNIVALI), Itajaí, SC, Brazil.

Boldine is the main alkaloid of Peumus boldus Molina, widely used in the traditional medicine for the treatment of digestive disorders. It is a compound with excellent antioxidant and anti-inflammatory properties already described. Despite the widespread use of P. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109166DOI Listing

An identification and functional evaluation of a novel CYP2C9 variant CYP2C9*62.

Chem Biol Interact 2020 Jun 9;327:109168. Epub 2020 Jun 9.

Cardiovascular Department, Beijing Hospital, National Center of Gerontology, Institute of Geriatric Medicine, Chinese Academy of Medical Sciences, Beijing, 100730, PR China. Electronic address:

Warfarin is the most commonly used anticoagulant in the clinical treatment of thromboembolic diseases. The dose of warfarin varies significantly within populations, and the dose is closely related to the genetic polymorphisms of the CYP2C9 and VKORC1 genes. In this study, a new CYP2C9 nonsynonymous mutation (8576C > T) was detected after the genetic screening of 162 patients took warfarin. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109168DOI Listing
June 2020
2.577 Impact Factor

Studies of selenium and arsenic mutual protection in human HepG2 cells.

Chem Biol Interact 2020 Jun 7;327:109162. Epub 2020 Jun 7.

Division of Analytical and Environmental Toxicology, Department of Laboratory Medicine and Pathology, University of Alberta, Edmonton, Alberta, Canada; Membrane Protein Disease Research Group, University of Alberta, Edmonton, Alberta, Canada; Department of Physiology, University of Alberta, Edmonton, Alberta, Canada. Electronic address:

Hundreds of millions of people worldwide are exposed to unacceptable levels of carcinogenic inorganic arsenic. Animal models have shown that selenium and arsenic are mutually protective through the formation and elimination of the seleno-bis(S-glutathionyl) arsinium ion [(GS)AsSe]. Consistent with this, human selenium deficiency in arsenic-endemic regions is associated with arsenic-induced disease, leading to the initiation of human selenium supplementation trials. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109162DOI Listing

Pharmacodynamic elucidation of glutamate & dopamine in ketamine-induced anaesthesia.

Chem Biol Interact 2020 Jun 7;327:109164. Epub 2020 Jun 7.

Department of Anesthesiology, The Second Hospital of Jilin University, 218 Ziqiang Street, Changchun, 130041, China. Electronic address:

General anaesthetics are some of the most widely used and essential therapeutic agents. However, despite over a century of research, the molecular mechanisms of general anaesthesia in the central nervous system remain elusive. Ketamine (ketamine hydrochloride) has been approved for use in general anaesthesia either alone or in combination with other medications. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109164DOI Listing

Inhibitory effects of organophosphate esters on carboxylesterase activity of rat liver microsomes.

Chem Biol Interact 2020 Jun 5;327:109148. Epub 2020 Jun 5.

Nihon Pharmaceutical University, Komuro 10281, Inamachi, Kitaadachi-gun, Saitama, 362-0806, Japan. Electronic address:

We investigated the inhibitory effects of 13 organophosphate esters (OPEs) and hydrolytic metabolites on the carboxylesterase activity of rat liver microsomes in vitro in order to examine whether there might be a potential impact on human health, and to elucidate the structure activity relationship. Among the test compounds, 2-ethylhexyl diphenyl phosphate (EDPhP) was the most potent inhibitor of carboxylesterase activity, as measured in terms of 4-nitrophenol acetate hydrolase activity, followed by tri-m-cresyl phosphate (TmCP), cresyl diphenyl phosphate (CDPhP) and triphenyl phosphate (TPhP). The IC values were as follows: EDPhP (IC: 0. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109148DOI Listing

Can image analysis provide evidence that lysosomal sequestration mediates daunorubicin resistance?

Chem Biol Interact 2020 May 30;327:109138. Epub 2020 May 30.

Department of Anatomy, Faculty of Medicine and Dentistry, Palacky University Olomouc, Hnevotinska 3, Olomouc, 77515, Czech Republic.

Altered intracellular distribution of weak base anticancer drugs owing to lysosomal sequestration is one purported mechanism contributing to chemotherapy resistance. This has often been demonstrated with the example of daunorubicin (DNR), chemotherapy with its characteristic red fluorescence used to trace it in cellular compartments. Here we addressed the question whether image analysis of DNR fluorescence can reflect its real intracellular distribution. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109138DOI Listing

Aliskiren - A promising antioxidant agent beyond hypertension reduction.

Authors:
Saeed Alshahrani

Chem Biol Interact 2020 Aug 30;326:109145. Epub 2020 May 30.

Department of Pharmacology and Toxicology, College of Pharmacy, Jazan University, Jizan, Saudi Arabia. Electronic address:

The renin-angiotensin-aldosterone system (RAAS) is a hormonal system that has a critical role in maintaining the normotensive state and electrolyte balance of the organism. The RAAS also has an important influence in the development of various pathophysiological conditions especially those concerning the renal system, cardiovascular system and hypertension. One of the consequences of the RAAS system is an increase in the generation of the reactive oxygen species (ROS) that causes an increase in oxidative stress, which may play a role in the development or exacerbation of such pathological conditions. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109145DOI Listing
August 2020
2.577 Impact Factor

In vitro cytotoxicity of montelukast in HAPI and SH-SY5Y cells.

Chem Biol Interact 2020 Aug 25;326:109134. Epub 2020 May 25.

School of Pharmacy and Pharmacology, Griffith University, Queensland, 4222, Australia; Quality Use of Medicines Network, Queensland, Australia. Electronic address:

Montelukast is a cysteinyl leukotriene (CysLT) receptor antagonist with efficacy against a variety of diseases, including asthma and inflammation-related conditions. However, various neuropsychiatric events (NEs) suspected to be related to montelukast have been reported recently, with limited understanding on their association and underlying mechanisms. This study aimed to investigate whether montelukast can induce neuroinflammation and neurotoxicity in microglial HAPI cells and neural SH-SY5Y cells. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109134DOI Listing

3,3',5,5'-tetramethoxybiphenyl-4,4'diol induces cell cycle arrest in G2/M phase and apoptosis in human non-small cell lung cancer A549 cells.

Chem Biol Interact 2020 Aug 24;326:109133. Epub 2020 May 24.

Laboratory of Immunoparasitology of Neglected Diseases and Cancer, State University of Londrina, PR, Brazil.

Lung cancer is one of the leading causes of cancer-related death worldwide. It has aggressive manifestation, high ability to promote metastasis and late diagnosis. In the present study, we investigated the cytotoxic effect of 3,3',5,5'-tetramethoxybiphenyl-4,4'diol (TMBP), against the A549 human non-small cell lung carcinoma lineage. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109133DOI Listing

Cytotoxicity of a naturally occuring spirostanol saponin, progenin III, towards a broad range of cancer cell lines by induction of apoptosis, autophagy and necroptosis.

Chem Biol Interact 2020 Aug 23;326:109141. Epub 2020 May 23.

Department of Pharmaceutical Biology, Institute of Pharmacy and Biochemistry, University of Mainz, Staudinger Weg 5, 55128, Mainz, Germany. Electronic address:

This study was aimed to investigate the cytotoxic potential of a natural compound, progenin III on a broad range of cancer cell lines, including various sensitive and drug-resistant phenotypes. The cytotoxicity, progenin III-induced autophagic, ferroptotic and necroptotic cell death were evaluated by the resazurin reduction assay (RRA). Spectrophotometric analysis of caspases activity was performed using caspase-Glo assay. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109141DOI Listing

Synthesis and in vitro evaluation of novel non-oximes for the reactivation of nerve agent inhibited human acetylcholinesterase.

Chem Biol Interact 2020 Aug 23;326:109139. Epub 2020 May 23.

TNO, Lange Kleiweg 137, 2288, GJ Rijswijk, the Netherlands.

Since several decades oximes have been used as part of treatment of nerve agent intoxication with the aim to restore the biological function of the enzyme acetylcholinesterase after its covalent inhibition by organophosphorus compounds such as pesticides and nerve agents. Recent findings have illustrated that, besides oximes, certain Mannich phenols can reactivate the inhibited enzyme very effectively, and may therefore represent an attractive complementary class of reactivators. In this paper we further probe the effect of structural variation on the in vitro efficacy of Mannich phenol based reactivators. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109139DOI Listing

Corrigendum to "Irisin attenuates angiotensin II-induced cardiac fibrosis via Nrf2 mediated inhibition of ROS/ TGFβ1/Smad2/3 signaling axis" [Chem Biol Interact 302 (2019) 11-21].

Chem Biol Interact 2020 07 22;325:109130. Epub 2020 May 22.

Department of Cardiology, The Second Affiliated Hospital of Air Force Medical University, Xi'an, Shaanxi Province, 710068, China; Department of Cardiology, Tangdu Hospital, Fourth Military Medical University, Xi'an, Shaanxi Province, 710068, China. Electronic address:

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http://dx.doi.org/10.1016/j.cbi.2020.109130DOI Listing

Lipid peroxidation inhibition study: A promising case of 1,3-di([1,1'-biphenyl]-3-yl)urea.

Chem Biol Interact 2020 Aug 19;326:109137. Epub 2020 May 19.

Dipartimento di Scienze Biomediche e Cliniche "Luigi Sacco", Università degli Studi diMilano, Via G.B. Grassi 74, 20157, Milano, Italy. Electronic address:

In the present study eighteen inhibitors of the hydrolytic enzymes of the endocannabinoid system were investigated for antioxidant activity using lipid peroxidation (LP) method. Among the assayed compounds ten belong to carbamates with phenyl [1,1'-biphenyl]-3-ylcarbamate (6), reported for the first time, and eight are retro-amide derivatives of palmitamine. Interestingly, results indicated that most of the tested compounds have good antioxidant properties. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109137DOI Listing

Quantitation by liquid chromatography-nanoelectrospray ionization-high resolution tandem mass spectrometry of DNA adducts derived from methyl glyoxal and carboxyethylating agents in leukocytes of smokers and non-smokers.

Chem Biol Interact 2020 May 20;327:109140. Epub 2020 May 20.

Masonic Cancer Center, University of Minnesota, Minneapolis, MN, 55455, USA. Electronic address:

A liquid chromatograpy-nanoelectrospray ionization-high resolution tandem mass spectrometry (LC-NSI-HRMS/MS) method was developed for quantitation of the DNA adducts 7-(2'-carboxyethyl)guanine (7-2'-CEG) and N-(1'-carboxyethyl)guanine (N-1'-CEG), as their methyl esters, in human leukocyte DNA from smokers and non-smokers. 7-2'-CEG has been previously identified in all human liver samples analyzed and is formed from an unknown carboxyethylating agent while N-1'-CEG is formed from the advanced glycation endproduct methyl glyoxal. The method was applied for the analysis of these two DNA adducts in leukocyte DNA from 20 smokers and 20 non-smokers, in part to test the hypothesis that 7-2'-CEG could be formed by endogenous nitrosation, as previously observed in rats treated with nitrosodihydrouracil and nitrite. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109140DOI Listing

Antiangiogenic and antitumoral activity of LQFM126 prototype against B16F10 melanoma cells.

Chem Biol Interact 2020 Jul 11;325:109127. Epub 2020 May 11.

Laboratory of Education and Research in In Vitro Toxicology (Tox In), Faculty of Pharmacy, Universidade Federal de Goiás, Goiânia, Goiás, Brazil. Electronic address:

Inhibition of mouse double minute 2 homolog (MDM2)-p53 interaction and reactivation of p53 signaling have been explored as effective anticancer therapeutic strategy. The potent and specific antitumor activity shown by Nutlins, first class of MDM2-p53 inhibitors discovered, has made these compounds potential antitumor candidates. To this end, we synthesized Nutlin-1 and Nutlin-2 analogs through molecular simplification and selected the compound with the most efficient antitumoral activity. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109127DOI Listing

Molecular and cellular basis of the anticancer activity of the prenylated flavonoid icaritin in hepatocellular carcinoma.

Authors:
Christian Bailly

Chem Biol Interact 2020 Jul 11;325:109124. Epub 2020 May 11.

OncoWitan, Lille, Wasquehal, 59290, France. Electronic address:

The prenylated flavonoid icaritin (ICT) is currently undergoing phase 3 clinical trial for the treatment of advanced hepatocellular carcinoma (HCC), based on a solid array of preclinical and clinical data. The antitumor activity originates from the capacity of the drug to modulate several signaling effectors in cancer cells, mainly the estrogen receptor splice variant ERα36, the transcription factors STAT3 and NFκB, and the chemokine receptor CXCR4. Recent studies have implicated additional components, including different microRNAs, the generation of reactive oxygen species and the targeting of sphingosine kinase-1. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109124DOI Listing

Interaction of alcohol with time of eating on markers of circadian dyssynchrony and colon tissue injury.

Chem Biol Interact 2020 Jul 11;325:109132. Epub 2020 May 11.

Department of Internal Medicine, Division of Gastroenterology, Rush University Medical Center, Chicago, IL, USA; Department of Physiology, Rush University Medical Center, Chicago, IL, USA; Division of Pharmacology, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, Utrecht, Netherlands; Department of Pharmacology, Rush University Medical Center, Chicago, IL, USA.

Background: Alcohol increases the risk of developing colon cancer (CRC), in part via tissue inflammation and impaired barrier integrity. Circadian dyssynchrony (CD) is an understudied but common lifestyle associated factor that increases the risk of multi-organ tissue injury and number of malignancies including CRC. Our prior studies showed that the shift in light-dark cycle exacerbates barrier dysfunction and colonic inflammation in the setting of alcohol treatment, and increases the risk of CRC. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109132DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7315934PMC

Graphene oxide enhances β-amyloid clearance by inducing autophagy of microglia and neurons.

Chem Biol Interact 2020 Jul 11;325:109126. Epub 2020 May 11.

Medical School, State Key Laboratory of Medicinal Chemical Biology, Key Laboratory of Bioactive Materials for Ministry of Education, Nankai University, Tianjin, 300071, China. Electronic address:

Alzheimer's disease (AD) is a common neurodegenerative disease, and its pathogenesis is closely related to β-amyloid (Aβ) peptide. The deposition of Aβ in the brain due to impaired Aβ clearance is considered as an important cause of AD. The decrease in Aβ clearance is closely related to the autophagy dysfunction in brains of AD patients. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109126DOI Listing

Improved skin decontamination efficacy for the nerve agent VX.

Chem Biol Interact 2020 Jul 16;325:109135. Epub 2020 May 16.

Swedish Defence Research Agency, Division of CBRN Defence and Security, Umeå, Sweden; Department of Public Health and Clinical Medicine, Unit of Respiratory Medicine, Umeå University, Umeå, Sweden.

Early initiated decontamination is demonstrated to be crucial to avoid systemic effects of highly toxic and low volatile agents exposed on the skin. Skin decontamination can be performed by simple procedures, such as washing with soap and water, or by using advanced decontamination products containing absorption and agent degradation properties. Reactive Skin Decontamination Lotion (RSDL) has demonstrated high efficacy to remove nerve agents from the skin. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109135DOI Listing

Role of betaine in inhibiting the induction of RNA Pol III gene transcription and cell growth caused by alcohol.

Chem Biol Interact 2020 Jul 11;325:109129. Epub 2020 May 11.

Department of Medicine, Keck School of Medicine, University of Southern California, Los Angeles, CA, USA. Electronic address:

Alcohol has been classified as carcinogenic to humans by the International Agency for Research on Cancer (IARC). Studies have demonstrated that alcohol intake increases the risk of breast cancer, and alcohol also stimulates breast cancer cell growth. Deregulation of Pol III genes is tightly associated with tumour development. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109129DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7323736PMC

Potential role of gut microbiota, the proto-oncogene PIKE (Agap2) and cytochrome P450 CYP2W1 in promotion of liver cancer by alcoholic and nonalcoholic fatty liver disease and protection by dietary soy protein.

Chem Biol Interact 2020 Jul 14;325:109131. Epub 2020 May 14.

Louisiana State University Health Sciences Center, New Orleans, USA.

We have previously demonstrated promotion of diethylnitrosamine (DEN) initiated liver tumorigenesis after feeding diets high in fat or ethanol (EtOH) to male mice. This was accompanied by hepatic induction of the proto-oncogene PIKE (Agap2). Switch of dietary protein from casein to soy protein isolate (SPI) significantly reduced tumor formation in these models. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109131DOI Listing

Stachydrine attenuates IL-1β-induced inflammatory response in osteoarthritis chondrocytes through the NF-κB signaling pathway.

Chem Biol Interact 2020 Aug 15;326:109136. Epub 2020 May 15.

Department of Orthopaedics, Huaihe Hospital of Henan University, Kaifeng, 475000, Henan Province, China.

Osteoarthritis (OA) is a common degenerative joint disease that is closely associated with inflammation. Stachydrine (STA) is a bioactive alkaloid with anti-inflammatory activity. However, the role of STA in OA remains unknown. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109136DOI Listing
August 2020
2.577 Impact Factor

Celecoxib reduces Deoxynivalenol induced proliferation, inflammation and protein kinase C translocation via modulating downstream targets in mouse skin.

Chem Biol Interact 2020 Aug 13;326:109128. Epub 2020 May 13.

Genotoxicity Laboratory, Division of Toxicology and Experimental Medicine, CSIR-Central Drug Research Institute, Lucknow, 226031, Uttar Pradesh, India. Electronic address:

Exposure to mycotoxins is mostly by ingestion but also occurs by the dermal and inhalation routes. The present study for the first time demonstrated that mycotoxin Deoxynivalenol (DON), permeates through Swiss albino mice skin, which demands awareness of health risks in people who are dermally exposed to mycotoxins especially agricultural farmers. Despite the widespread contamination of DON in food commodities studies to alleviate DON's toxicity are sparsely reported. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109128DOI Listing
August 2020
2.577 Impact Factor

Sorption of G-agent simulant vapours on human scalp hair.

Chem Biol Interact 2020 Aug 13;326:109111. Epub 2020 May 13.

Aix Marseille Univ, CNRS, LCE, Marseille, France.

Human scalp hair is a biological matrix that can trap chemical vapours from explosives (TNT), drugs (THC) and chemical weapons (yperite). The external contamination of human's hair following exposure to organophosphorus (OP) nerve agent was simulated by model compounds: triethyl phosphate (TEP) and diisopropyl fluorophosphate (DFP). In this work were exposed strands of hair to vapours of TEP and DFP (3 and 7 ppm) to model sorption kinetics. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109111DOI Listing

Daphnia magna responses to fish kairomone and chlorpromazine exposures.

Chem Biol Interact 2020 Jul 7;325:109123. Epub 2020 May 7.

Department of Environmental Chemistry, IDAEA-CSIC, Jordi Girona 18, 08034, Barcelona, Spain.

To avoid being preyed, organisms must be able to identify predatory threats by sensing molecules released by predators (kairomones), and to employ effective strategies to prevent detection by predators. Furthermore, in the wild, organisms are also exposed to chemicals that may alter their behavioral traits, such as neuroactive pharmaceuticals. Considering the co-occurrence of both types of chemicals, their possible interaction needs to be studied. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109123DOI Listing

Dysregulation of UDP-glucuronosyltransferases in CCl induced liver injury rats.

Chem Biol Interact 2020 Jul 4;325:109115. Epub 2020 May 4.

School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China; State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, 210009, Jiangsu, China. Electronic address:

UDP-glucuronosyltransferases (UGTs) are a family of phase II drug metabolizing enzymes that catalyze glucuronidation of numerous endogenous and exogenous substrates. Carbon tetrachloride (CCl) is widely used to develop liver injuries mimicking human liver diseases. However, effects of CCl on the expression and activities of UGTs and the mechanism have not been fully elucidated. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109115DOI Listing

Polymethoxyflavones from Gardenia oudiepe (Rubiaceae) induce cytoskeleton disruption-mediated apoptosis and sensitize BRAF-mutated melanoma cells to chemotherapy.

Chem Biol Interact 2020 Jul 4;325:109109. Epub 2020 May 4.

LIENSs UMRi CNRS 7266, La Rochelle Université, 17042, La Rochelle, France.

A series of 10 natural and semisynthetic flavonoids (1 to 10) were obtained from Gardenia oudiepe (Rubiaceae), an endemic plant from New Caledonia. Most of them were polymethoxylated flavones (PMFs) of rare occurrence. After a cell viability screening test, PMFs 2 and 3 showed significant cytotoxic activity against A2058 human melanoma cells (IC = 3. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109109DOI Listing

Plants derived therapeutic strategies targeting chronic respiratory diseases: Chemical and immunological perspective.

Chem Biol Interact 2020 Jul 4;325:109125. Epub 2020 May 4.

Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Ultimo, NSW, 2007, Australia; Centre for Inflammation, Centenary Institute, Sydney, NSW, 2050, Australia; School of Pharmaceutical Sciences, Shoolini University, Bajhol, Sultanpur, Solan, Himachal Pradesh, 173229, India; Priority Research Centre for Healthy Lungs, Hunter Medical Research Institute (HMRI) & School of Biomedical Sciences and Pharmacy, University of Newcastle, Callaghan, NSW, 2308, Australia; Priority Research Centre for Healthy Lungs, Hunter Medical Research Institute (HMRI) & School of Biomedical Sciences and Pharmacy, University of Newcastle, Callaghan, NSW, 2308, Australia. Electronic address:

The apparent predicament of the representative chemotherapy for managing respiratory distress calls for an obligatory deliberation for identifying the pharmaceuticals that effectively counter the contemporary intricacies associated with target disease. Multiple, complex regulatory pathways manifest chronic pulmonary disorders, which require chemotherapeutics that produce composite inhibitory effect. The cost effective natural product based molecules hold a high fervor to meet the prospects posed by current respiratory-distress therapy by sparing the tedious drug design and development archetypes, present a robust standing for the possible replacement of the fading practice of poly-pharmacology, and ensure the subversion of a potential disease relapse. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109125DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7196551PMC
July 2020
2.577 Impact Factor

Human exposure to synthetic endocrine disrupting chemicals (S-EDCs) is generally negligible as compared to natural compounds with higher or comparable endocrine activity. How to evaluate the risk of the S-EDCs?

Chem Biol Interact 2020 Aug 1;326:109099. Epub 2020 May 1.

Department of Chemistry & Pharmaceutical Sciences, Vrije Universiteit, Amsterdam, the Netherlands.

Theoretically, both synthetic endocrine disrupting chemicals (S-EDCs) and natural (exogenous and endogenous) endocrine disrupting chemicals (N-EDCs) can interact with endocrine receptors and disturb hormonal balance. However, compared to endogenous hormones, S-EDCs are only weak partial agonists with receptor affinities several orders of magnitude lower. Thus, to elicit observable effects, S-EDCs require considerably higher concentrations to attain sufficient receptor occupancy or to displace natural hormones and other endogenous ligands. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109099DOI Listing

The GPR55 antagonist CID16020046 mitigates advanced glycation end products (AGEs)- induced chondrocyte activation.

Chem Biol Interact 2020 Jul 1;325:109088. Epub 2020 May 1.

Department of Neurology, The First People's Hospital of Chongqing Liang Jiang New District, Chongqing, 400010, China.

Osteoarthritis (OA) is one of the most common degenerative joint diseases in aging people. The activation of chondrocytes and their dysregulation are closely related to the pathogenesis of OA. GPR55 is an unique orphan G-receptor which binds to cannabinoids. Read More

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http://dx.doi.org/10.1016/j.cbi.2020.109088DOI Listing