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https://www.readbyqxmd.com/read/28945041/-dynamic-serum-metabolomics-study-of-liver-injury-in-rats-caused-by-polygonum-multifulorum
#1
Zhi-Jie Ma, Qi Li, Kui-Jun Zhao, Jia-Bo Wang, Xiao-He Xiao
Liquid chromatography-mass spectrometry method was used for determination of metabolic fingerprint spectrum in rat serum, and the method of multivariate statistical analysis was used to compare the metabolism spectrum difference and screen significantly related biomarkers. The dynamic change trend was investigated at the same time. The dynamic metabonomics changes of liver injury in rats caused by Polygonum multifulorum(PM) were investigated; significantly related biomarkers were found and their dynamic change trend was investigated to provide basis for internal mechanism and early clinical diagnosis...
January 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28945011/prediction-of-drug-drug-interaction-between-tacrolimus-and-principal-ingredients-of-wuzhi-capsule-in-chinese-healthy-volunteers-using-physiologically-based-pharmacokinetic-modelling
#2
Hongyan Zhang, Fengjiao Bu, Lei Li, Zheng Jiao, Guo Ma, Weimin Cai, Xiaomei Zhuang, Hai-Shu Lin, Jae-Gook Shin, Xiaoqiang Xiang
Schisantherin A and schisandrin A, the most abundant active ingredients of Wuzhi capsule, are known to inhibit tacrolimus metabolism by inhibiting CYP3A4/5. We aimed to predict the contribution of schisantherin A and schisandrin A to drug-drug interaction (DDI) between Wuzhi capsule and tacrolimus using physiologically-based pharmacokinetic (PBPK) modelling. Firstly, the inhibition mechanism of schisantherin A and schisandrin A on CYP3A4/5 were investigated. Thereafter, PBPK models of schisantherin A, schisandrin A and tacrolimus were established...
September 25, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28944989/the-combination-of-valsartan-and-sacubitril-in-the-treatment-of-hypertension-and-heart-failure-an-update
#3
Peter Munch Nielsen, Daniela Grimm, Markus Wehland, Ulf Simonsen, Marcus Krüger
A novel antihypertensive drug, LCZ696 (Entresto(®) ), has recently been introduced, which combines the action of an antagonist of the renin-angiotensin-aldosterone-system (RAAS), effectively decreasing the blood pressure, with an inhibition of neprilysin, which is responsible for metabolizing natriuretic peptides exerting anti-hypertensive and anti-fibrotic effects. In this MiniReview, we describe the pharmacokinetics and -dynamics, efficacy and side effects of the combined angiotensin receptor antagonist and neprilysin inhibitor LCZ696...
September 25, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28944880/edoxaban-improves-venous-thrombosis-via-increasing-hydrogen-sulfide-and-homocysteine-in-rat-model
#4
Wei Song, Hongbo Ci, Guanglei Tian, Yanjun Zhang, Xiaohu Ge
Anticoagulant therapy is prescribed to millions of patients worldwide for the prevention and treatment of venous thrombosis. Evidence has indicated that edoxaban is a potential drug of oral anticoagulant in the acute treatment of venous thromboembolism. Hydrogen sulfide and homocysteine plasma concentration are indicators of cardiovascular and neurovascular disease risk factors that have attracted considerable attention for regulation of vascular health and homeostasis. However, the molecular mechanism of edoxaban‑mediated differences of hydrogen sulfide and homocysteine has not been investigated in the progression of venous thrombosis...
September 21, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28944856/systemic-overexpression-of-the-11%C3%AE-%C3%A2-hsd1-promotes-endoplasmic-reticulum-stress-in-multiple-tissues-and-the-development-of-metabolic-syndrome-in-mice
#5
Chenxiao Li, Jihan Xia, Wenjuan Zhu, Leilei Xin, Cuiping An, Shulin Yang, Kui Li
Glucocorticoids are associated with lipid metabolism and their abnormal expression has an important function in the development of metabolic syndrome. The 11β‑hydroxysteroid dehydrogenase type 1 (11β‑HSD1) is a metabolic enzyme of glucocorticoids and may be a potential drug target for the treatment of metabolic syndrome. However, the association between the systemic expression of 11β‑HSD1 and metabolic syndrome remains to be elucidated. The present study used a cytomegalovirus promoter to obtain mice that systemically overexpressed the 11β‑HSD1 gene...
September 20, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28944677/a-multiplex-and-label-free-relative-quantification-approach-for-studying-protein-abundance-of-drug-metabolizing-enzymes-in-human-liver-microsomes-using-swath-ms
#6
Rohitash Jamwal, Benjamin J Barlock, Sravani Adusumalli, Ken Ogasawara, Brigitte L Simons, Fatemeh Akhlaghi
We describe a sequential windowed acquisition of all theoretical fragment ion mass spectra (SWATH-MS) based method for label-free, simultaneous, relative quantification of drug metabolism enzymes in human liver microsomes (HLM; n=78). In-solution tryptic digestion was aided by a pressure cycling method which allowed a 90-min incubation time, a significant reduction over classical protocols (12-18 h). Digested peptides were separated on an Acquity UHPLC Peptide BEH C18 column using a 60-min gradient method at a flow rate of 0...
September 25, 2017: Journal of Proteome Research
https://www.readbyqxmd.com/read/28944587/finding-the-genetic-mechanisms-of-folate-deficiency-and-neural-tube-defects-leaving-no-stone-unturned
#7
REVIEW
Kit Sing Au, Tina O Findley, Hope Northrup
Neural tube defects (NTDs) occur secondary to failed closure of the neural tube between the third and fourth weeks of gestation. The worldwide incidence ranges from 0.3 to 200 per 10,000 births with the United States of American NTD incidence at around 3-6.3 per 10,000 dependent on race and socioeconomic background. Human NTD incidence has fallen by 35-50% in North America due to mandatory folic acid fortification of enriched cereal grain products since 1998. The US Food and Drug Administration has approved the folic acid fortification of corn masa flour with the goal to further reduce the incidence of NTDs, especially among individuals who are Hispanic...
September 25, 2017: American Journal of Medical Genetics. Part A
https://www.readbyqxmd.com/read/28944407/oral-thymoquinone-administration-ameliorates-the-effect-of-cisplatin-on-brush-border-membrane-enzymes-energy-metabolism-and-redox-status-in-rat-kidney
#8
Zeba Farooqui, Faaiza Shahid, Subuhi Abidi, Iqbal Parwez, Farah Khan
Therapeutic use of cisplatin (CP), an effective anticancer drug, is limited by dose dependent nephrotoxicity. Thymoquinone (TQ), the major Nigella sativa seed oil constituent has been shown to prevent progression of various renal disorders. The present study investigates the protective effect of TQ on CP-induced nephrotoxicity. Rats were divided into six groups viz. control, CP, CPTQ1, CPTQ2, CPTQ3, and TQ alone group. Animals in CP and TQ combination groups were administered TQ (0.5, 1.5, and 3 mg/kg bwt, orally) with single intraperitoneal dose of CP (6 mg/kg bwt)...
September 24, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28944315/is-chronic-ahr-activation-by-rapidly-metabolized-ligands-safe-for-the-treatment-of-immune-mediated-diseases
#9
Allison K Ehrlich, Nancy I Kerkvliet
There is a long standing perception that AhR ligands are automatically disqualified from pharmaceutical development due to their induction of Cyp1a1 as well as their potential for causing "dioxin-like" toxicities. However, recent discoveries of new AhR ligands with potential therapeutic applications have been reported, inviting reconsideration of this policy. One area of exploration is focused on the activation of AhR to promote the generation of regulatory T cells, which control the intensity and duration of immune responses...
February 2017: Current Opinion in Toxicology
https://www.readbyqxmd.com/read/28943391/cytogenetic-effects-of-jacareubin-from-calophyllum-brasiliense-on-human-peripheral-blood-mononucleated-cells-in-vitro-and-on-mouse-polychromatic-erythrocytes-in-vivo
#10
W R García-Niño, E Estrada-Muñiz, M Valverde, R Reyes-Chilpa, L Vega
Jacareubin is a xanthone isolated from the heartwood of Calophyllum brasiliense with antibacterial and gastroprotective properties and the intention for clinical use as an anti-cancer treatment (due to the similar chemical structure to other anti-neoplastic drugs) requires an investigation of whether this compound can generate adverse effects on non-transformed cells. Jacareubin (0.5-1000μM in DMSO) was more cytotoxic on phytohemagglutinin (PHA)-stimulated normal human peripheral blood mononuclear cells (PBMCs; IC50 at 72h by MTT: 85...
September 21, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28943209/a-novel-high-drug-loading-mussel-inspired-polydopamine-hybrid-nanoparticle-as-a-ph-sensitive-vehicle-for-drug-delivery
#11
Jie Hou, Chunlei Guo, Yuzhi Shi, Ergang Liu, Weibing Dong, Bo Yu, Shiyuan Liu, Junbo Gong
A novel high drug loading pH-cleavable polymer hybrid nanoparticle was prepared via doxorubicin (DOX) grafted onto PEGylated, mussel-inspired polydopamine (PDA) and then coated onto hollow silica nanoparticles for drug delivery. A series of characterization shed light on the formation mechanisms of PDA coatings on hollow silica. We hypothesized that dopamine was first absorbed onto the surface of hollow silica and then began self-polymerization. A Dox-containing thiol moiety was fabricated with conjugation between doxorubicin hydrochloride and Mercaptopropionyalkali with a pH-cleavable hydrozone bond...
September 21, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28942842/a-green-fluorescent-protein-based-assay-for-high-throughput-ligand-binding-studies-of-a-mycobacterial-biotin-protein-ligase
#12
Thomas E H Bond, Alanna E Sorenson, Patrick M Schaeffer
Biotin protein ligase (BirA) has been identified as an emerging drug target in Mycobacterium tuberculosis due to its essential metabolic role. Indeed, it is the only enzyme capable of covalently attaching biotin onto the biotin carboxyl carrier protein subunit of the acetyl-CoA carboxylase. Despite recent interest in this protein, there is still a gap in cost-effective high-throughput screening assays for rapid identification of mycobacterial BirA-targeting inhibitors. We present for the first time the cloning, expression, purification of mycobacterial GFP-tagged BirA and its application for the development of a high-throughput assay building on the principle of differential scanning fluorimetry of GFP-tagged proteins...
December 2017: Microbiological Research
https://www.readbyqxmd.com/read/28942212/peptide-biosensors-for-anticancer-drugs-design-in-silico-to-work-in-denaturizing-environment
#13
Filomena Guida, Anna Battisti, Ivan Gladich, Mauro Buzzo, Elena Marangon, Luciana Giodini, Giuseppe Toffoli, Alessandro Laio, Federico Berti
One of the main targets in current clinical oncology is the development of a cheap device capable of monitoring in real-time the concentration of a drug in the blood of a patient. This would allow fine-tuning the dosage according to the patient's metabolism, a key condition to reduce side effects. By using surface plasmon resonance and fluorescence spectroscopy we here show that short peptides designed in silico by a recently developed algorithm are capable of binding the anticancer drug irinotecan (CPT-11) with micromolar affinity...
September 14, 2017: Biosensors & Bioelectronics
https://www.readbyqxmd.com/read/28942133/bush-mint-hyptis-suaveolens-and-spreading-hogweed-boerhavia-diffusa-medicinal-plant-extracts-differentially-affect-activities-of-cyp1a2-cyp2d6-and-cyp3a4-enzymes
#14
Nicholas Ekow Thomford, Kevin Dzobo, Faustina Adu, Shadreck Chirikure, Ambroise Wonkam, Collet Dandara
ETHNO-PHARMACOLOGICAL RELEVANCE: Hyptis suaveolens (L) Poit and Boerhavia diffusa Linn are medicinal herbal plants commonly found in the tropics and sub-tropics. They are used to treat various conditions among them boils, dyslipidaemia, eczema, malaria, jaundice and gonorrhoea. Thus, the herbal medicinal extracts are now found as part of some commercial herbal formulations. There has not been adequate characterisation of these medicinal herbs on their effects on drug metabolising enzymes...
September 20, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28942006/effect-of-dronedarone-on-the-pharmacokinetics-of-carvedilol-following-oral-administration-to-rats
#15
Min-Soo Kim, In-Hwan Baek
Dronedarone is a CYP2D6 inhibitor; therefore, it is prudent to exercise caution when concurrently administering CYP2D6-metabolized β-blockers because of a lack of published data on potential drug interactions. The aim of this study was to investigate the effect of dronedarone on the pharmacokinetics of orally administered carvedilol in rats. Twenty male Sprague-Dawley rats were randomly divided into two groups and 10mg/kg carvedilol was administered to the rat with or without dronedarone pretreatment in a parallel design...
September 20, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28941398/the-mechanisms-mediating-the-antiepileptic-effects-of-the-ketogenic-diet-and-potential-opportunities-for-improvement-with-metabolism-altering-drugs
#16
REVIEW
Neil A Youngson, Margaret J Morris, Bill Ballard
The ketogenic diet (KD) is increasingly being used to treat patients with intractable epilepsy. Despite decades of research, the reason for its success, when anticonvulsants have failed, is still not completely understood. There are, however, many candidate mechanisms which can be grouped into those that alter neuronal excitability at the synapse, and those that confer neuroprotection. The molecular underpinning of these mechanisms centres on the shift from glucose- to lipid-based energy generation that accompanies a high fat/low carbohydrate diet...
September 13, 2017: Seizure: the Journal of the British Epilepsy Association
https://www.readbyqxmd.com/read/28941172/characterization-of-in-vitro-generated-metabolites-of-selected-peptides-2-kda-prohibited-in-sports
#17
Andreas Thomas, Andre Knoop, Wilhelm Schänzer, Mario Thevis
With an increasing number of prohibited substances in doping controls, knowledge about their metabolism is crucial for efficient analysis. While for low molecular mass molecules, standard protocols for in-vitro metabolism experiments are well established, the situation with peptidic drugs has been shown to be substantially more heterogeneous and complex. Two principle strategies aiming at simulating the metabolism of lower molecular mass peptides in-vitro are presented within this study. The prohibited peptides ARA-290, GHRP-3 and Peforelin, with a to date unknown metabolism, were chosen as model compounds for these experiments and metabolism after incubation with different blood specimens (EDTA-, heparin-, citrate-plasma and serum) and exposure to recombinant amidase were investigated...
September 22, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28940752/supplementation-with-docosahexaenoic-acid-and-extra-virgin-olive-oil-prevents-liver-steatosis-induced-by-a-high-fat-diet-in-mice-through-ppar-%C3%AE-and-nrf2-upregulation-with-concomitant-srebp-1c-and-nf-kb-downregulation
#18
María C Hernández-Rodas, Rodrigo Valenzuela, Francisca Echeverría, Miguel Ángel Rincón-Cervera, Alejandra Espinosa, Paola Illesca, Patricio Muñoz, Alicia Corbari, Nalda Romero, Daniel Gonzalez-Mañan, Luis A Videla
SCOPE: Non alcoholic fatty liver disease (NAFLD) is the most common cause of liver disease, for which there is no validated drug therapy at present time. In this respect, the polyunsaturated fatty acid docosahexaenoic acid (C22:6 n-3, DHA) modulate lipid metabolism in the liver, and extra virgin olive oil (EVOO) has hepatoprotective effects. METHODS AND RESULTS: Effect of combined docosahexaenoic acid (DHA; C22:6 n-3) and extra virgin olive oil (EVOO) administration to mice on oxidative stress and metabolic disturbances induced by high-fat diet (HFD) was evaluated...
September 21, 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/28940667/drugs-for-metabolic-conditions-and-prostate-cancer-death-in-men-on-gnrh-agonists
#19
Cecilia Bosco, Chloe Wong, Hans Garmo, Danielle Crawley, Lars Holmberg, Niklas Hammar, Jan Adolfsson, Pär Stattin, Mieke Van Hemelrijck
BACKGROUND: It is unclear whether metabolic syndrome and its related drugs is affecting treatment response in men with prostate cancer (PCa) on Gonadotropin releasing Hormone (GnRH) agonists. We aimed to evaluate whether drugs for metabolic conditions influence PCa-specific mortality in men starting GnRH agonists. METHODS: We selected all men receiving GnRH agonists as primary treatment in PCBaSe Sweden (n=9,267). Use of drugs for metabolic conditions (i.e. anti-diabetes, anti-dyslipidaemia, and anti-hypertension) in relation to all cause, cardiovascular disease (CVD), and PCa-specific death was studied using multivariate Cox proportional hazard and Fine and Gray competing regression models...
September 20, 2017: BJU International
https://www.readbyqxmd.com/read/28940476/impact-of-cyp2d6-functional-allelic-variations-on-phenoconversion-and-drug-drug-interactions
#20
F Storelli, A Matthey, S Lenglet, A Thomas, J Desmeules, Y Daali
We investigated whether CYP2D6 extensive metabolizers (EM) carrying a non-functional allele are at higher risk of phenoconversion to poor metabolizers in presence of CYP2D6 inhibitors. Seventeen homozygous carriers of two fully-functional alleles and seventeen heterozygous carriers of one fully-functional and one non-functional allele participated in this trial. Dextromethorphan 5mg and tramadol 10mg were given at each of the three study sessions. CYP2D6 was inhibited by duloxetine 60mg (session 2) and paroxetine 20mg (session 3)...
September 23, 2017: Clinical Pharmacology and Therapeutics
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