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BMC Pharmacology & Toxicology

Ying Li, Xiu-Liang Cui, Qing-Shan Chen, Jing Yu, Hai Zhang, Jie Gao, Du-Xin Sun, Guo-Qing Zhang
BACKGROUD: Cationic liposomes (CLs) can be used as non-viral vectors in gene transfer and drug delivery. However, the underlying molecular mechanism of its cytotoxicity has not been well elucidated yet. METHODS: We herein report a systems biology approach based on whole-transcriptome sequencing coupled with computational method to identify the predominant genes and pathways involved in the cytotoxicity of CLs in HepG2 cell line. RESULTS: Firstly, we validated the concentration-dependent cytotoxicity of CLs with an IC50 of 120 μg/ml in HepG2 exposed for 24 h...
July 11, 2018: BMC Pharmacology & Toxicology
Arthur Cássio de Lima Luna, Greice Kelle Viegas Saraiva, Gilberto Orivaldo Chierice, Henrique Hesse, Durvanei Augusto Maria
BACKGROUND: Current studies have demonstrated that DODAC/PHO-S (Dioctadecyldimethylammonium Chloride/Synthetic phosphoethanolamine) liposomes induces cytotoxicity in Hepa1c1c7 and B16F10 murine tumor cells, with a higher proportion than PHO-S. Therefore, our aim was to evaluate the potential of DODAC/PHO-S to elucidate the mechanism of cell death whereby the liposomes induces cytotoxicity in hepatocellular carcinoma Hepa1c1c7, compared to the PHO-S alone. METHODS: Liposomes (DODAC/PHO-S) were prepared by ultrasonication...
July 11, 2018: BMC Pharmacology & Toxicology
Guanhao Zheng, Li Cao, Zaiqian Che, Enqiang Mao, Erzhen Chen, Juan He
BACKGROUND: Polymyxin B (PMB), which is regarded as the ultimate antibacterial treatment against some intractable gram-negative bacteria with its outstanding anti-bacterial activities, inflicts several adverse effects on patients. However, skin hyperpigmentaion (SH) induced by PMB is very rare. Here, we report a case of polymyxin B-induced skin hyperpigmentation (PMB-iSH) in a 21-year-old female. To the best of our knowledge, this is the first case of PMB-iSH in China. CASE PRESENTATION: A 21-year-old female patient with sepsis received the administration of PMB by intravenous injection for the treatment of multi-drug resistant Klebsiella pneumoniae (MDR-KP) infection...
July 4, 2018: BMC Pharmacology & Toxicology
Peter Kardos, Kai-Michael Beeh, Ulrike Sent, Tobias Mueck, Heidemarie Gräter, Martin C Michel
BACKGROUND: Ambroxol relieves cough symptoms based on its secretagogue, anti-inflammatory, anti-oxidant, anti-bacterial, anti-viral, immunomodulatory and local anesthetic effects. The present study was designed to explore differential patient profiles and efficacy against acute respiratory symptoms of four formulations registered as over-the-counter medicines. METHODS: Nine hundred sixty-five pharmacy customers purchasing one of four branded ambroxol formulations (extended release capsules, adult syrup, pediatric syrup and soft pastilles) filled a questionnaire including a patient-adapted version of the Bronchitis Severity Scale, several questions on degree of impairment by acute cough, time to onset of symptom relief and duration of treatment...
July 4, 2018: BMC Pharmacology & Toxicology
Yichen Jia, Rulin Wang, Long Li, Ying Zhang, Jiawei Li, Jina Wang, Xuanchuan Wang, Guisheng Qi, Ruiming Rong, Ming Xu, Tongyu Zhu
BACKGROUND: Immunosuppressant drugs for renal transplant mycophenolate mofetil (MMF) and enteric-coated mycophenolate sodium (EC-MPS) cause gastrointestinal (GI) disorders. The specific site of GI tract targeted by MMF and EC-MPS remains unclear. METHODS: In this study, we investigated the effects of MMF and EC-MPS on stomach, duodenum, jejunum, ileum, colon and rectum using a rat model. Rats were randomized into five groups: control, MMF (100 mg/kg·d), mofetil (30 mg/kg·d), EC-MPS (72 mg/Kg·d), mofetil + EC-MPS...
July 4, 2018: BMC Pharmacology & Toxicology
Moses N Ngemenya, Grace Ntube Abwenzoh, Hermia Nalova Ikome, Denis Zofou, Fidele Ntie-Kang, Simon M N Efange
BACKGROUND: Emergence of resistance to artemisinins and some of their combinations in chemotherapy of clinical malaria has intensified the search for novel safe efficacious antimalarial molecules. Fourteen synthetic 1, 4-disubstituted piperidines with simple molecular structures were evaluated in this study. METHODS: Antiplasmodial activity were determined against cultured chloroquine-sensitive 3D7 and resistant Dd2 strains of P. falciparum by in vitro parasite growth inhibition...
July 4, 2018: BMC Pharmacology & Toxicology
Tomoki Fukuyama, Sarah Ehling, Jenny Wilzopolski, Wolfgang Bäumer
BACKGROUND: Topical administration of PR022, 0.05% hypochlorous acid (HOCl) in gel has been demonstrated to be beneficial in a chronic murine atopic dermatitis model. In a follow up study we tested a higher concentration (0.1%) of PR022 HOCl gel in comparison to the Janus kinase inhibitor tofacitinib, both of which are currently in clinical phase studies for treatment of human atopic dermatitis. METHODS: The effect of topically administered HOCl (0.1%) in gel was compared to a topical formulation of tofacitinib (0...
July 3, 2018: BMC Pharmacology & Toxicology
Girish Parthan, Shobhit Bhansali, Anura V Kurpad, Rama Walia, Kishor Bhat, Anil Bhansali
BACKGROUND: Dipeptidyl peptidase 4 (DPP4) inhibitors improve glycemic control by promoting GLP1-mediated glucose-dependent insulin secretion and suppression of glucagon. Sitagliptin and vildagliptin have been shown to improve insulin sensitivity in patients with type 2 diabetes mellitus (T2DM). However, these patients had uncontrolled blood glucose at inclusion; therefore, the improvement in insulin sensitivity observed in these studies could be attributed to the drug per se and/or reduction in glucotoxicity...
July 3, 2018: BMC Pharmacology & Toxicology
Alireza Abdi, Azam Faraji, Fateme Dehghan, Alireza Khatony
BACKGROUND: The possibility of self-medication is higher in health sciences students than other students because of easy access to drug information resources and relatively sufficient familiarity with various kinds of drugs. The current study was aimed to determine the prevalence of self-medication and its related factors among the health sciences students. METHODS: A total of 250 health sciences students were included in this cross-sectional study via random sampling...
July 3, 2018: BMC Pharmacology & Toxicology
Filip Caisberger, Jaroslav Pejchal, Jan Misik, Jiri Kassa, Martin Valis, Kamil Kuca
BACKGROUND: The aim of our study was to compare the ability of two combinations of oximes (HI-6 + trimedoxime and HI-6 + K203) with atropine to counteract acute sarin-induced brain damage with the efficacy of antidotal treatment involving single oxime (HI-6) and atropin using in vivo methods. METHODS: Brain damage and neuroprotective effects of antidotal treatment were evaluated in rats poisoned with sarin at a sublethal dose (108 μg/kg i.m.; 90% LD50 ) using histopathological, Fluoro-Jade B and Terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) analysis 24 h after sarin administration...
June 28, 2018: BMC Pharmacology & Toxicology
Anum Saqib, Muhammad Rehan Sarwar, Muhammad Sarfraz, Sadia Iftikhar
BACKGROUND: A large number of hospital admissions are attributed to adverse drug reactions (ADRs) and they are the fifth leading cause of death worldwide. The present study aimed to assess the causality and preventability of adverse drug events (ADEs) of antibiotics among inpatients having different lengths of hospital stay. METHODS: A prospective, observational study was conducted in four tertiary-care public sector hospitals of Lahore, Pakistan. Study population consisted of hospitalized patients who were prescribed one or more antibiotics...
June 25, 2018: BMC Pharmacology & Toxicology
Hadi Molanaei, Abdul Rashid Qureshi, Olof Heimbürger, Bengt Lindholm, Ulf Diczfalusy, Björn Anderstam, Leif Bertilsson, Peter Stenvinkel
BACKGROUND: Recent studies indicate that inflammation may also affect CYP3A4 activity. Associations of CYP3A4-mediated metabolism of quinine, with inflammatory biomarkers were investigated in patients undergoing maintenance hemodialysis (HD). METHODS: A single dose of 100 mg quinine was given to 44 HD patients and the plasma concentration of quinine and its metabolite 3-OH-quinine were measured 12 h after drug intake. The ratios of quinine/3-OH-quinine and 4β-OH-cholesterol/cholesterol were used as markers of CYP3A4 activity...
June 25, 2018: BMC Pharmacology & Toxicology
Pimradasiri Srijiwangsa, Saranyoo Ponnikorn, Kesara Na-Bangchang
BACKGROUND: Cholangiocarcinoma (CCA), an epithelial malignancy of the biliary tree, is one of the aggressive cancers with poor prognosis and unsatisfactory response to chemotherapy with acquired resistance. NAD(P)H-quinone oxidoreductase 1 (NQO1), an antioxidant/detoxifying enzyme, plays important roles in chemo-resistance and proliferation in several cancer cells. The study aimed to investigate the inhibitory effect of β-eudesmol on NQO1 enhanced chemotherapeutic effects of 5-fluorouracil (5-FU) and doxorubicin (DOX) in the high NQO1-expressing human CCA cell line, NQO1-KKU-100...
June 19, 2018: BMC Pharmacology & Toxicology
Feng Huang
BACKGROUND: In this analysis, we aimed to systematically compare stent thrombosis (ST) and its different subtypes following treatment with DAPT (aspirin + clopidogrel) versus TAPT (aspirin + clopidogrel + cilostazol). METHODS: Studies were included if: they were randomized controlled trials (RCTs) comparing TAPT (cilostazol + aspirin + clopidogrel) with DAPT (aspirin + clopidogrel); they reported ST or its subtype including definite, probable, acute, sub-acute and late ST as their clinical outcomes...
June 18, 2018: BMC Pharmacology & Toxicology
M Mofizul Islam, Ian S McRae, Soumya Mazumdar, Paul Simpson, Dennis Wollersheim, Kaniz Fatema, Tony Butler
BACKGROUND: Patterns of opioid dispensing often exhibit substantial temporal and geographical variability, which has implications for public health policy decisions and interventions. The study examined recent trends in prescription opioid dispensing and identified high dispensing areas and factors associated with the doses dispensed. METHODS: Three years (1 January 2013-31 December 2015) of dispensing data of prescription opioids in local government areas (LGAs) for New South Wales (NSW), Australia's most populous state, were analyzed...
June 18, 2018: BMC Pharmacology & Toxicology
Karen Roksund Hov, Bjørn Erik Neerland, Anders Mikal Andersen, Øystein Undseth, Vegard Bruun Wyller, Alasdair M J MacLullich, Eva Skovlund, Eirik Qvigstad, Torgeir Bruun Wyller
BACKGROUND: The Oslo Study of Clonidine in Elderly Patients with Delirium (LUCID) is an RCT investigating the effect of clonidine in medical patients > 65 years with delirium. To assess the dosage regimen and safety measures of this study protocol, we measured the plasma concentrations and hemodynamic effects of clonidine in the first 20 patients. METHODS: Patients were randomised to clonidine (n = 10) or placebo (n = 10). The treatment group was given a loading dose (75μg every 3rd hour up to a maximum of 4 doses) to reach steady state, and further 75μg twice daily until delirium free for 2 days, discharge or a maximum of 7 days...
June 8, 2018: BMC Pharmacology & Toxicology
Amsalu Bokore, Belay Korme, Getu Bayisa
BACKGROUND: Human Immunodeficiency Virus (HIV) is one of the main causes of morbidity and mortality; because of this it continues to be a major global public health concern. It has believed to kill more than 34 million lives so far. Sub Saharan Africa constitutes about 70% of people living with HIV among the 37 million on the globe. This region, accounted for more than two third of the global new HIV infections and about 15 million (40%) were receiving antiretroviral therapy (ART) at the end of 2014 throught the world...
June 5, 2018: BMC Pharmacology & Toxicology
Abimbola O Opadeyi, Annie Fourrier-Réglat, Ambrose O Isah
BACKGROUND: WHO pharmacovigilance indicators have been recommended as a useful tool towards improving pharmacovigilance activities. Nigeria with a myriad of medicines related issues is encouraging the growth of pharmacovigilance at peripheral centres. This study evaluated the status of pharmacovigilance in tertiary hospitals in the South-South zone of Nigeria with a view towards improving the pharmacovigilance system in the zone. METHODS: A cross-sectional descriptive survey was conducted in six randomly selected tertiary hospitals in the South-South zone of the country...
May 31, 2018: BMC Pharmacology & Toxicology
Yufeng Zhao, Lei Zhang, Aili Yan, Di Chen, Rong Xie, Yingguang Liu, Xiangyan Liang, Yanyan Zhao, Lanlan Wei, Jun Yu, Xi Xu, Xingli Su
BACKGROUND: Grifolic acid is a derivative of grifolin, an antitumor natural compound, and it was reported as an agonist of free fatty acid receptor GPR120. Little is known about its antitumor effects and the involvement of GPR120. METHODS: GH3 cells, the rat anterior pituitary adenoma cells, were cultured and the cell death was measured by MTT assay and Annexin V/PI staining. The mitochondrial membrane potential (MMP) of GH3 cells was measured by JC-1 staining. Cellular ATP levels and the intracellular NAD/NADH ratio were measured...
May 30, 2018: BMC Pharmacology & Toxicology
Tosapol Anukunwithaya, Pilaslak Poo, Natthaphon Hunsakunachai, Ratchanee Rodsiri, Suchinda Malaivijitnond, Phisit Khemawoot
BACKGROUND: Pueraria candollei var. mirifica is a medicinal plant that is promoted as a "Champion Product" by the Government of Thailand. This plant has been reported to relieve postmenopausal symptoms, prevent and reverse bone loss, inhibit the growth of breast cancer, and alleviate cardiovascular diseases in preclinical and clinical studies. However, there is little information on the oral bioavailability and tissue distribution of puerarin with respect to its pharmacodynamic activities...
May 25, 2018: BMC Pharmacology & Toxicology
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