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https://www.readbyqxmd.com/read/28638869/reducing-toxicity-and-increasing-efficiency-aconitine-with-liquiritin-and-glycyrrhetinic-acid-regulate-calcium-regulatory-proteins-in-rat-myocardial-cell
#1
Yuyan Zhang, Li Yu, Weifeng Jin, Hongjing Fan, Min Li, Tianmei Zhou, Haitong Wan, Jiehong Yang
BACKGROUND: Compatibility of Radix Aconiti Carmichaeli and Liquorice is known to treat heart diseases such as heart failure and cardiac arrhythmias. This work answers the question that whether the active components (Aconitine, Liquiritin and Glycyrrhetinic Acid) of Radix Aconiti Carmichaeli and Liquorice could result in regulating intracellular calcium homeostasis and calcium cycling, and thereby verifies the therapeutic material basis. MATERIALS AND METHODS: The myocardial cells were divided into twelve groups randomly as control group, Aconitine group, nine different dose groups that orthogonal combined with Aconitine, Liquiritin and Glycyrrhetinic Acid, and Verapamil group...
2017: African Journal of Traditional, Complementary, and Alternative Medicines: AJTCAM
https://www.readbyqxmd.com/read/28638577/a-rare-case-of-apical-hypertrophic-cardiomyopathy-ahcm
#2
Seyed Abbas Mirabbasi, Koroush Khalighi, Suresh Mukkamala, Archana Kodali
Apical hypertrophic cardiomyopathy is a rare form of hypertrophic cardiomyopathy that involves thickening of the distal portion of the left ventricular wall. Most commonly seen in the Japan, with a prevalence rate of about 15% of all HCM patient, its incidence in the USA is approximately 3% of HCM cases. We report a case of a 46-year-old woman with history of hypertension who presented to emergency department with worsening dyspnea and orthopnea with features of left ventricular hypertrophy (LVH) and diffuse large T-wave inversions in the lateral leads on a 12-lead ECG...
March 2017: Journal of Community Hospital Internal Medicine Perspectives
https://www.readbyqxmd.com/read/28636609/genomic-and-phenotypic-characterisation-of-fluoroquinolone-resistance-mechanisms-in-enterobacteriaceae-in-durban-south-africa
#3
John Osei Sekyere, Daniel Gyamfi Amoako
Resistance to fluoroquinolones (FQ) is being increasingly reported and found to be mediated by efflux pumps, plasmid-mediated quinolone resistance genes (PMQR) and mutations in gyrA, gyrB, parC and parE. However, studies reporting on FQ resistance mechanisms (FQRM), particularly in Africa, are focused mostly on Salmonella. This study used a whole-genome-based approach to describe FQRM in forty-eight clinical Enterobacteriaceae isolates comprising of Klebsiella pneumoniae (n = 21), Serratia marcescens (n = 12), Enterobacter spp...
2017: PloS One
https://www.readbyqxmd.com/read/28633109/endothelial-nlrp3-inflammasome-activation-and-arterial-neointima-formation-associated-with-acid-sphingomyelinase-during-hypercholesterolemia
#4
Saisudha Koka, Min Xia, Yang Chen, Owais M Bhat, Xinxu Yuan, Krishna M Boini, Pin-Lan Li
The NLRP3 inflammasome has been reported to be activated by atherogenic factors, whereby endothelial injury and consequent atherosclerotic lesions are triggered in the arterial wall. However, the mechanisms activating and regulating NLRP3 inflammasomes remain poorly understood. The present study tested whether acid sphingomyelinase (ASM) and ceramide associated membrane raft (MR) signaling platforms contribute to the activation of NLRP3 inflammasomes and atherosclerotic lesions during hypercholesterolemia. We found that 7-ketocholesterol (7-Keto) or cholesterol crystal (ChC) markedly increased the formation and activation of NLRP3 inflammasomes in mouse carotid arterial endothelial cells (CAECs), as shown by increased colocalization of NLRP3 with ASC or caspase-1, enhanced caspase-1 activity and elevated IL-1β levels, which were markedly attenuated by mouse Asm siRNA, ASM inhibitor- amitriptyline, and deletion of mouse Asm gene...
June 15, 2017: Redox Biology
https://www.readbyqxmd.com/read/28631422/dispersive-micro-solid-phase-extraction-using-carbon-based-adsorbents-for-sensitive-determination-of-verapamil-in-plasma-samples-coupled-with-ce
#5
Abolghasem Jouyban, Samin Hamidi
A dispersive micro solid phase extraction procedure coupled with CE-UV detection was developed for determination of verapamil in plasma samples. Graphene oxide/polydopamin was synthesized by a one-step polymerization method, and graphene oxide/Fe3 O4 nanocomposite was prepared by co-precipitation method. Moreover, they were fully characterized. The use of hazardous and water-immiscible solvents was scaled down, and only 500 μL of acetone was required as the desorption solvent. The detector response-concentration plots were linear in the range of 5-500 ng/mL, and the proposed method was validated according to guidelines...
June 20, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28621579/optimization-of-antimicrobial-photodynamic-therapy-in-biofilms-by-inhibiting-efflux-pump
#6
Tatiana Maria Starck Fogaça de Aguiar Coletti, Laura Marise de Freitas, Ana Marisa Fusco Almeida, Carla Raquel Fontana
BACKGROUND: One of the main mechanisms of microbial resistance is given by efflux pumps, which reduce the effectiveness of antimicrobials by decreasing their intracellular concentration. OBJECTIVE AND METHODS: Considering that efflux pump inhibitors are promising adjuvant molecules for antibiotics in infections, in this study, using XTT test and colony forming unit (CFU) counting, we evaluated the association between the pump inhibitor verapamil (VP) and the antimicrobial photodynamic therapy (aPDT) mediated by methylene blue (MB) in biofilms of Escherichia coli and Staphylococcus aureus to optimize the bacterial reduction...
June 15, 2017: Photomedicine and Laser Surgery
https://www.readbyqxmd.com/read/28603132/airways-and-vascular-smooth-muscles-relaxant-activities-of-gaultheria-trichophylla
#7
Fiaz Alam, Qazi Najumus Saqib, Abdul Jabbar Shah
The aim of this experimental work was to explore the potential pharmacological activities of Gaultheria trichophylla Royle in hyperactive respiratory and vascular conditions. Gaultheria trichophylla was extracted with solvents, phytochemical detection tests were performed, and rabbit trachea and aorta strips were used to evaluate its effects on airways and vascular smooth muscles. Qualitative phytochemical tests showed the presence of flavonoids, alkaloids, anthraquinones, saponins, terpenoids, and condensed tannins...
January 2017: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28602600/influence-of-the-dual-combination-of-silymarin-and-epigallocatechin-gallate-natural-dietary-flavonoids-on-the-pharmacokinetics-of-oxcarbazepine-in-rats
#8
Ana Ferreira, Márcio Rodrigues, Alexandre Marques, Amílcar Falcão, Gilberto Alves
Considering the potential of flavonoids in reversing the P-glycoprotein (P-gp)-mediated multidrug resistance, this work aimed to assess the combined effects of silymarin and (-)-epigallocatechin gallate (EPG) on the pharmacokinetics of the P-gp substrates oxcarbazepine (OXC) and licarbazepine (LIC). Rats were pre-treated intraperitoneally with silymarin (25 mg/kg), EPG (25 mg/kg), silymarin/EPG (12.5/12.5 mg/kg; 6.25/18.75 mg/kg; 18.75/6.25 mg/kg) or verapamil (25 mg/kg, reference P-gp inhibitor) before the intraperitoneal administration of OXC (50 mg/kg)...
June 8, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28591563/evaluation-of-the-cytotoxicity-and-intestinal-absorption-of-a-self-emulsifying-drug-delivery-system-containing-sodium-taurocholate
#9
Hang Gao, Miao Wang, Dandan Sun, Shilin Sun, Cheng Sun, Jianguo Liu, Qingxiang Guan
Currently, many surfactants used in self-emulsifying drug delivery systems (SMEDDS) can cause gastrointestinal mucosal irritation and systemic toxicity. In the present study, SMEDDS were loaded with pueraria flavones, using sodium taurocholate to replace polyoxyl 40 dydrogenated castor oil (Cremophor® RH 40) as the surfactant (PF-SMEDDSNR) to reduce the toxicity of SMEDDS using Cremophor® RH 40 as the surfactant (PF-SMEDDSR). The absorption rate constants (Ka) and intestinal permeability coefficients (Peff) were measured...
June 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28590124/terpenoids-from-euphorbia-soongarica-and-their-multidrug-resistance-reversal-activity
#10
Jie Gao, Haji A Aisa
Ten new terpenoids, including five diterpenoids (1-5), three nortriterpenoids (6-8), and two triterpenoids (9, 10), and 15 known terpenoids (11-25) were isolated from an acetone extract of Euphorbia soongarica. Sooneuphoramine (1) is the first example of a euphoractine B-type diterpenoid alkaloid, while sooneuphanones A-C (6-8) are rare nortriterpenoids from the Euphorbia genus. The isolated terpenoids were tested for their cytotoxicity and multidrug resistance (MDR) reversal activity, 10 of which showed moderate cytotoxicity against the KB and KBv200 cell lines, while 11 compounds exhibited P-gp modulating potential...
June 7, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28588548/thyroxine-t4-transfer-from-blood-to-cerebrospinal-fluid-in-sheep-isolated-perfused-choroid-plexus-role-of-multidrug-resistance-associated-proteins-and-organic-anion-transporting-polypeptides
#11
Kazem Zibara, Nabil El Zein, Mirna Sabra, Mohammad Hneino, Hayat Harati, Wael Mohamed, Firas H Kobeissy, Nouhad Kassem
Thyroxine (T4) enters the brain either directly across the blood-brain barrier (BBB) or indirectly via the choroid plexus (CP), which forms the blood-cerebrospinal fluid barrier (B-CSF-B). In this study, using isolated perfused CP of the sheep by single-circulation paired tracer and steady-state techniques, T4 transport mechanisms from blood into lateral ventricle CP has been characterized as the first step in the transfer across the B-CSF-B. After removal of sheep brain, the CPs were perfused with (125)I-T4 and (14)C-mannitol...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28585859/evaluation-of-the-potential-for-drug-interactions-with-patiromer-in-healthy-volunteers
#12
Lawrence J Lesko, Elliot Offman, Christine Taylor Brew, Dahlia Garza, Wade Benton, Martha R Mayo, Alain Romero, Charles Du Mond, Matthew R Weir
INTRODUCTION: Patiromer is a potassium-binding polymer that is not systemically absorbed; however, it may bind coadministered oral drugs in the gastrointestinal tract, potentially reducing their absorption. METHODS: Twelve randomized, open-label, 3-period, 3-sequence crossover studies were conducted in healthy volunteers to evaluate the effect of patiromer (perpetrator drug) on absorption and single-dose pharmacokinetics (PK) of drugs (victims) that might be commonly used with patiromer...
January 1, 2017: Journal of Cardiovascular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28584158/identification-of-novel-efflux-proteins-rv0191-rv3756c-rv3008-and-rv1667c-involved-in-pyrazinamide-resistance-in-mycobacterium-tuberculosis
#13
Yumeng Zhang, Jia Zhang, Peng Cui, Wenhong Zhang, Ying Zhang
Pyrazinamide (PZA) is a critical drug used for the treatment of tuberculosis (TB). PZA is a prodrug that requires conversion to the active component pyrazinoic acid (POA) by pyrazinamidase (PZase) encoded by the pncA gene. Although resistance to PZA is mostly caused by pncA mutations and less commonly by rpsA, panD, and clpC1, clinical strains without these mutations are known to exist. While efflux of POA was demonstrated in Mycobacterium tuberculosis previously, the efflux proteins involved have not been identified...
June 5, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28583845/cav1-2-channel-current-block-by-the-pka-inhibitor-h-89-in-rat-tail-artery-myocytes-via-a-pka-independent-mechanism-electrophysiological-functional-and-molecular-docking-studies
#14
Fabio Fusi, Alfonso Trezza, Ottavia Spiga, Giampietro Sgaragli, Sergio Bova
To characterize the role of cAMP-dependent protein kinase (PKA) in regulating vascular Ca(2+) current through Cav1.2 channels [ICa1.2], we have documented a marked capacity of the isoquinoline H-89, widely used as a PKA inhibitor, to reduce current amplitude. We hypothesized that the ICa1.2 inhibitory activity of H-89 was mediated by mechanisms unrelated to PKA inhibition. To support this, an in-depth analysis of H-89 vascular effects on both ICa1.2 and contractility was undertaken by performing whole-cell patch-clamp recordings and functional experiments in rat tail main artery single myocytes and rings, respectively...
June 2, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28579031/the-antiparasitic-activity-of-avenacosides-against-intestinal-nematodes
#15
Maria Doligalska, Kinga Jóźwicka, Katarzyna Donskow-Łysoniewska, Małgorzata Kalinowska
Avena sativa L., 1753 (Poaceae) is used as feed for livestock and as a crop rotation agent. The purpose of the study was to examine the molecular mechanisms behind the antihelminth activity of the oat saponins avenacoside B (AveB) and 26-desglucoavenacoside B (26DGAveB) by evaluating their effect on Heligmosomoides bakeri, a parasitic nematode of mice. The avenacosides AveB and 26DGAveB were separated and purified from A. sativa green leaves, and their mycotoxic activity was confirmed against the fungus Trichoderma harzianum...
July 15, 2017: Veterinary Parasitology
https://www.readbyqxmd.com/read/28578345/calcium-channel-opening-rather-than-the-release-of-atp-causes-the-apoptosis-of-osteoblasts-induced-by-overloaded-mechanical-stimulation
#16
Lu Liu, Hui Li, Ying Cui, Ruixin Li, Fan Meng, Zi Ye, Xizheng Zhang
BACKGROUND: Stress fracture is one of the most common overuse injuries in athletes. Overloaded mechanical stimulation is an important factor affecting stress fractures, but the mechanism is unclear. METHODS: MC3T3-E1 cells and a polycaprolactone (PCL) scaffold were co-cultured, and finite element analysis (FEA) was used to analyze the load-carrying capability. Cell proliferation was investigated with CCK-8 assays. An alkaline phosphatase (AKP) activity assay was used to evaluate cell differentiation...
June 5, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28578165/antihypertensive-and-vasorelaxant-effects-of-aqueous-extract-of-artemisia-campestris-l-from-eastern-morocco
#17
Ikram Dib, Monique Tits, Luc Angenot, Jean Noel Wauters, Asmae Assaidi, Hassane Mekhfi, Mohammed Aziz, Mohammed Bnouham, Abdelkhaleq Legssyer, Michel Frederich, Abderrahim Ziyyat
ETHNOPHARMACOLOGICAL RELEVANCE: Artemisia campestris L. (Asteraceae) has many traditional uses, among which treatment of diabetes and hypertension. AIM OF THE STUDY: This study was conducted in order to confirm the antihypertensive and hypotensive effects of A. campestris L. aqueous extract (AcAE) and to explore the underlying mechanism of action of its vasorelaxant effect, besides the acute toxicity. Also, the chemical composition of AcAE was investigated. MATERIAL AND METHODS: the chemical content of AcAE was determined by using HPLC and NMR techniques...
May 31, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28577929/mrp-1-and-bcrp-promote-the-externalization-of-phosphatidylserine-in-oxalate-treated-renal-epithelial-cells-implications-for-calcium-oxalate-urolithiasis
#18
YiFu Li, ShiLiang Yu, XiuGuo Gan, Ze Zhang, Yan Wang, YingWei Wang, RuiHua An
OBJECTIVES: To investigate the possible involvement of multidrug resistance-associated protein 1 (MRP-1) and breast cancer resistance protein (BCRP) in the oxalate-induced redistribution of phosphatidylserine (PS) in renal epithelial cell membranes. METHODS: A western blot analysis was used to examine the MRP-1 and BCRP expression levels. Surface-expressed PS was detected by the annexin V-binding assay. The cell-permeable fluorogenic probe 2,7-dichlorofluorescein diacetate (DCFH-DA) was used to measure the intracellular reactive oxygen species (ROS) level...
May 31, 2017: Urology
https://www.readbyqxmd.com/read/28569378/cyclosporine-exacerbates-ketamine-toxicity-in-zebrafish-mechanistic-studies-on-drug-drug-interaction
#19
Bonnie L Robinson, Melanie Dumas, Syed F Ali, Merle G Paule, Qiang Gu, Jyotshna Kanungo
Cyclosporine A (CsA) is an immunosuppressive drug commonly used in organ transplant patients to prevent allograft rejections. Ketamine is a pediatric anesthetic that noncompetitively inhibits the calcium-permeable N-methyl-d-aspartic acid receptors. Adverse drug-drug interaction effects between ketamine and CsA have been reported in mammals and humans. However, the mechanism of such drug-drug interaction is unclear. We have previously reported adverse effects of combination drugs, such as verapamil/ketamine and shown the mechanism through intervention by other drugs in zebrafish embryos...
June 1, 2017: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/28568606/coupling-of-excitation-to-ca-2-release-is-modulated-by-dysferlin
#20
Valeriy Lukyanenko, Joaquin M Muriel, Robert J Bloch
Dysferlin concentrates in the transverse tubules of skeletal muscle and stabilizes Ca(2+) transients when muscle fibres are subjected to osmotic shock injury (OSI). We show here that voltage-induced Ca(2+) transients elicited in dysferlin-null A/J myofibers are smaller than control A/WySnJ fibres. Regional expression of Venus-dysferlin chimeras in A/J fibres restores the full amplitude of the Ca(2+) transients and protects against OSI. We also show that drugs that target ryanodine receptors (RyR1: dantrolene, tetracaine, S107) and L-type Ca(2+) channels (LTCC: nifedipine, verapamil, diltiazem) prevent the decrease in Ca(2+) transients in A/J fibres following OSI...
June 1, 2017: Journal of Physiology
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