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https://www.readbyqxmd.com/read/27907843/triphenyltin-degradation-and-proteomic-response-by-an-engineered-escherichia-coli-expressing-cytochrome-p450-enzyme
#1
Wenying Yi, Kunliang Yang, Jinshao Ye, Yan Long, Jing Ke, Huase Ou
Although triphenyltin (TPT) degradation pathway has been determined, information about the enzyme and protein networks involved was severely limited. To this end, a cytochrome P450 hydroxylase (CYP450) gene from Bacillus thuringiensis was cloned and expressed in Escherichia coli BL21 (DE3), namely E. coli pET32a-CYP450, whose dosage at 1gL(-1) could degrade 54.6% TPT at 1mgL(-1) within 6 d through attacking the carbon-tin bonds of TPT by CYP450. Sequence analysis verified that the CYP450 gene had a 1214bp open reading frame, encoding a protein with 404 amino acids...
November 28, 2016: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/27904813/glycyrrhetinic-acid-might-increase-the-nephrotoxicity-of-bakuchiol-by-inhibiting-cytochrome-p450-isoenzymes
#2
Aifang Li, Nana Ma, Zijing Zhao, Mei Yuan, Hua Li, Qi Wang
BACKGROUND: Licorice, a popular traditional Chinese medicine (TCM), is widely used to moderate the effects (detoxification) of other herbs in TCM and often combined with Fructus Psoraleae. However, the classical TCM book states that Fructus Psoraleae is incompatible with licorice; the mechanism underlying this incompatibility has not been identified. Glycyrrhetinic acid (GA), the active metabolite of licorice, may increase the toxicity of bakuchiol (BAK), the main chemical ingredient in Psoralea corylifolia, by inhibiting its detoxification enzymes CYP450s...
2016: PeerJ
https://www.readbyqxmd.com/read/27899252/the-effects-of-metronidazole-on-cytochrome-p450-activity-and-expression-in-rats-after-acute-exposure-to-high-altitude-of-4300m
#3
Rong Wang, Yuhuan Sun, Qiang Yin, Hua Xie, Wenbin Li, Chang Wang, Jiankui Guo, Ying Hao, Rui Tao, Zhengping Jia
BACKGROUND: The purpose is to observe the changes of CYP450 enzyme activity expression as well as the physiological and pathological states of Wistar rats given metronidazole drug intervention after acute exposure to high altitude of 4300m. METHODS AND RESULTS: Thirty healthy adult male Wistar rats of average weight 200 ± 20 g were randomly assigned into three groups of 10 rats per group as follows: Group A (55m), Group B (4300m) and Group C (metronidazole intervention, 4300m)...
November 26, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27889497/in-vivo-effect-of-borneol-on-rat-hepatic-cyp2b-expression-and-activity
#4
Jing-Ya Chen, Xiang-Tao Huang, Jun-Jun Wang, Yong Chen
CYP2B subfamily accounts for 2-10% of total hepatic CYP450 enzymes and participate in the metabolism of around 8% of clinical drugs. Borneol has been widely used in traditional Chinese medicine for thousands of years. There are many studies about borneol-induced promoting penetration role for a number of drugs through various physiologic barriers, whereas there is no report involved the effect of borneol on hepatic CYP2B. The present work studied the in vivo effect of borneol on the expression and activity of rat hepatic CYP2B...
November 23, 2016: Chemico-biological Interactions
https://www.readbyqxmd.com/read/27884721/comparison-of-xenobiotic-metabolising-human-porcine-rodent-and-piscine-cytochrome-p450
#5
REVIEW
Viktoriia Burkina, Martin Krøyer Rasmussen, Nadezhda Pilipenko, Galia Zamaratskaia
Cytochrome P450 proteins (CYP450s) are present in most domains of life and play a critical role in the metabolism of endogenous compounds and xenobiotics. The effects of exposure to xenobiotics depend heavily on the expression and activity of drug-metabolizing CYP450s, which is determined by species, genetic background, age, gender, diet, and exposure to environmental pollutants. Numerous reports have investigated the role of different vertebrate CYP450s in xenobiotic metabolism. Model organisms provide powerful experimental tools to investigate Phase I metabolism...
November 21, 2016: Toxicology
https://www.readbyqxmd.com/read/27876840/transcriptome-profiling-shows-gene-regulation-patterns-in-ginsenoside-pathway-in-response-to-methyl-jasmonate-in-panax-quinquefolium-adventitious-root
#6
Juan Wang, Jinxin Li, Jianli Li, Shujie Liu, Xiaolei Wu, Jing Li, Wenyuan Gao
Here, we combine elicitors and transcriptomics to investigate the inducible biosynthesis of the ginsenoside from the Panax quinquefolium. Treatment of P. quinquefolium adventitious root with methyl jasmonate (MJ) results in an increase in ginsenoside content (43.66 mg/g compared to 8.32 mg/g in control group). Therefore, we sequenced the transcriptome of native and MJ treated adventitious root in order to elucidate the key differentially expressed genes (DEGs) in the ginsenoside biosynthetic pathway. Through DEG analysis, we found that 5,759 unigenes were up-regulated and 6,389 unigenes down-regulated in response to MJ treatment...
November 23, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27875319/enhanced-oral-bioavailability-of-metoprolol-with-gallic-acid-and-ellagic-acid-in-male-wistar-rats-involvement-of-cyp2d6-inhibition
#7
Bhargavi Latha Athukuri, Prasad Neerati
BACKGROUND: Cytochrome P450-2D6 (CYP2D6), a member of the CYP450 mixed function oxidase system, is an important CYP isoform with regard to herbal-drug interactions and is responsible for the metabolism of nearly 25% of drugs. Until now, studies on the effects of various phytochemicals on CYP2D6 activity in vivo have been very rare. Gallic acid and ellagic acid are natural polyphenols which are widely distributed in fruits and medicinal plants. In the present study, the effects of gallic acid and ellagic acid pretreatment on intestinal transport and oral bioavailability of metoprolol were investigated...
December 1, 2016: Drug Metabolism and Personalized Therapy
https://www.readbyqxmd.com/read/27872784/ciprofloxacin-and-clozapine-a-potentially-fatal-but-underappreciated-interaction
#8
Jonathan M Meyer, George Proctor, Michael A Cummings, Laura J Dardashti, Stephen M Stahl
Objective. Clozapine provides a 50%-60% response rate in refractory schizophrenia but has a narrow therapeutic index and is susceptible to pharmacokinetic interactions, particularly with strong inhibitors or inducers of cytochrome P450 (CYP) 1A2. Case Report. We report the case of a 28-year-old nonsmoking female with intellectual disability who was maintained for 3 years on clozapine 100 mg orally twice daily. The patient was treated for presumptive urinary tract infection with ciprofloxacin 500 mg orally twice daily and two days later collapsed and died despite resuscitation efforts...
2016: Case Reports in Psychiatry
https://www.readbyqxmd.com/read/27867264/traditional-herbal-formulas-to-as-treatments-for-musculoskeletal-disorders-their-inhibitory-effects-on-the-activities-of-human-microsomal-cytochrome-p450s-and-udp-glucuronosyltransferases
#9
Seong Eun Jin, Chang-Seob Seo, Hyeun-Kyoo Shin, Hyekyung Ha
OBJECTIVE: The aim of this study was to assess the influence of traditional herbal formulas, including Bangpungtongseong-san (BPTSS; Fangfengtongsheng-san, Bofu-tsusho-san), Ojeok-san (OJS; Wuji-san, Goshaku-san), and Oyaksungi-san (OYSGS; Wuyaoshungi-san, Uyakujyunki-san), on the activities of the human cytochrome P450s (CYP450s) and UDP-glucuronosyltransferases (UGTs), which are drug-metabolizing enzymes. MATERIALS AND METHODS: The activities of the major human CYP450 isozymes (CYP1A2, CYP3A4, CYP2B6, CYP2C9, CYP2C19, CYP2D6, and CYP2E1) and UGTs (UGT1A1, UGT1A4, and UGT2B7) were investigated using in vitro fluorescence-based and luminescence-based enzyme assays, respectively...
October 2016: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/27849442/to-genotype-or-phenotype-for-personalized-medicine-cyp450-drug-metabolizing-enzyme-genotype-phenotype-concordance-and-discordance-in-the-ecuadorian-population
#10
Fernando De Andrés, Santiago Terán, Francisco Hernández, Enrique Terán, Adrián LLerena
Genetic variations within the cytochrome P450 (CYP450) superfamily of drug metabolizing enzymes confer substantial person-to-person and between-population differences in pharmacokinetics, and by extension, highly variable clinical effects of medicines. In this context, "personalized medicine," "precision medicine," and "stratified medicine" are related concepts attributed to what is essentially targeted therapeutics and companion diagnostics, aimed at improving safety and effectiveness of health interventions...
November 16, 2016: Omics: a Journal of Integrative Biology
https://www.readbyqxmd.com/read/27848009/the-effects-of-p-gp-and-cyp450-modulated-by-rifampicin-on-the-steroid-induced-osteonecrosis-of-the-femoral-head
#11
Teng Fei, Yunchao Shao, Zuoqin Yan, Liang Zhu, Shuo Li, Jianfeng Pan, Changan Guo
This study investigated the effects of rifampicin-modulated P-glycoprotein (P-gp) and cytochrome P450 (CYP450) activity on the development of steroid-induced osteonecrosis of the femoral head. Thirty-two rabbits were equally divided into four groups: control group, oral administration group, intramuscular injection group, and local release group, in which rifampicin-loaded artificial bone graft was implanted in the left femur cavity and blank bone graft was implanted in the right femur cavity. Dexamethasone was given 1 week after rifampicin administration...
November 15, 2016: Journal of Bone and Mineral Metabolism
https://www.readbyqxmd.com/read/27845750/inhibitory-interactions-of-aspalathus-linearis-rooibos-extracts-and-compounds-aspalathin-and-z-2-%C3%AE-d-glucopyranosyloxy-3-phenylpropenoic-acid-on-cytochromes-metabolizing-hypoglycemic-and-hypolipidemic-drugs
#12
Oelfah Patel, Christo Muller, Elizabeth Joubert, Johan Louw, Bernd Rosenkranz, Charles Awortwe
Rooibos extract, due to its glucose and lipid lowering effects, has potential as a nutraceutical for improvement of metabolic dysfunction. Potential herb-drug interactions as a result of the use of natural products are of increasing concern. Cytochrome P450 enzymes, CYP2C8, CYP2C9, and CYP3A4, are important in the metabolism of hypoglycemic drugs, such as thiazolidinediones (TZDs) and sulfonylureas, and hypocholesterolemic drugs, such as atorvastatin. This study investigated the effects of rooibos extracts, prepared from "unfermented" and "fermented" rooibos plant material and two of the major bioactive compounds, Z-2-(β-d-glucopyranosyloxy)-3-phenylpropenoic acid (PPAG) and aspalathin (ASP), on Vivid(®) recombinant CYP450 enzymes...
November 12, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27843822/impact-of-antiepileptic-drugs-on-bone-health-need-for-monitoring-treatment-and-prevention-strategies
#13
REVIEW
Ekta Arora, Harmanjit Singh, Yogendra Kumar Gupta
Epilepsy is the most common neurological disorder affecting approximately 50 million people worldwide. In India, overall prevalence of epilepsy is reported to be 5.59/1000 population. Antiepileptic drugs (AEDs) constitute the main-stay of treatment with a large number of AEDs available in the market. High incidence of adverse effects is a major limitation with AEDs. One of the major concerns is significant metabolic effects on the bone. However, little attention has been paid to this issue because most of the bone effects remain subclinical for a long time and may take years to manifest clinically...
April 2016: Journal of Family Medicine and Primary Care
https://www.readbyqxmd.com/read/27834912/curcumin-prevents-aflatoxin-b%C3%A2-hepatoxicity-by-inhibition-of-cytochrome-p450-isozymes-in-chick-liver
#14
Ni-Ya Zhang, Ming Qi, Ling Zhao, Ming-Kun Zhu, Jiao Guo, Jie Liu, Chang-Qin Gu, Shahid Ali Rajput, Christopher Steven Krumm, De-Sheng Qi, Lv-Hui Sun
This study was designed to establish if Curcumin (CM) alleviates Aflatoxin B₁ (AFB₁)-induced hepatotoxic effects and to determine whether alteration of the expression of cytochrome P450 (CYP450) isozymes is involved in the regulation of these effects in chick liver. One-day-old male broilers (n = 120) were divided into four groups and used in a two by two factorial trial in which the main factors included supplementing AFB₁ (< 5 vs. 100 μg/kg) and CM (0 vs. 150 mg/kg) in a corn/soybean-based diet...
November 10, 2016: Toxins
https://www.readbyqxmd.com/read/27818929/cloning-and-expression-of-sgcyp450-4-from-siraitia-grosvenorii
#15
Dongping Tu, Xiaojun Ma, Huan Zhao, Changming Mo, Qi Tang, Liuping Wang, Jie Huang, Limei Pan
CYP450 plays an essential role in the development and growth of the fruits of Siraitia grosvenorii. However, little is known about the SgCYP450-4 gene in S. grosvenorii. Here, based on transcriptome data, a full-length cDNA sequence of SgCYP450-4 was cloned by reverse transcriptase-polymerase chain reaction (RT-PCR) and rapid-amplification of cDNA ends (RACE) strategies. SgCYP450-4 is 1677 bp in length (GenBank accession No. AEM42985.1) and contains a complete open reading frame (ORF) of 1422 bp. The deduced protein was composed of 473 amino acids, the molecular weight is 54...
November 2016: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/27808485/concomitant-use-of-proton-pump-inhibitors-and-dual-antiplatelet-therapy-for-cardiovascular-outcomes
#16
Alessandro Mandurino-Mirizzi, Sergio Leonardi, Chiara Melloni
INTRODUCTION: The aim of this review is to discuss the consequences of potential pharmacokinetic interactions between proton pump inhibitors (PPIs) and antiplatelet therapy on cardiovascular (CV) outcomes and provide guidance on the management of concomitant use of PPIs in patients on dual antiplatelet therapy (DAPT). EVIDENCE ACQUISITION: DAPT combining aspirin and oral P2Y12 receptor inhibitors increases the risk of gastrointestinal (GI) bleeding, with higher rates of morbidity and mortality in patients undergoing percutaneous coronary intervention (PCI)...
November 3, 2016: Minerva Endocrinologica
https://www.readbyqxmd.com/read/27806669/cell-expansion-during-directed-differentiation-of-stem-cells-toward-the-hepatic-lineage
#17
Ravali Raju, David Chau, Dong Seong Cho, Yonsil Park, Catherine Verfaillie, Wei-Shou Hu
The differentiation of human pluripotent stem cells (hPSCs) towards the hepatocyte lineage can potentially provide an unlimited source of functional hepatocytes for transplantation and extracorporeal bioartificial liver applications. It is anticipated that the quantities of cells needed for these applications will be in the order of 10<sup>9</sup>-10<sup>10</sup>cells, because of the size of the liver. An ideal differentiation protocol would be to enable directed differentiation to the hepatocyte lineage with simultaneous cell expansion...
November 2, 2016: Stem Cells and Development
https://www.readbyqxmd.com/read/27783976/heterocyclic-replacements-for-benzene-maximising-adme-benefits-by-considering-individual-ring-isomers
#18
Timothy J Ritchie, Simon J F Macdonald
The impact of replacing a mono-substituted benzene (phenyl) ring with thirty three aromatic and nine aliphatic heterocycles on nine ADME-related screens (solubility, lipophilicity, permeability, protein binding CYP450 inhibition and metabolic clearance) was assessed using matched molecular pair analysis. The results indicate that the influence on the ADME profile can differ significantly depending on the ring identity and importantly on the individual regioisomers that are possible for some rings. This information enables the medicinal chemist to make an informed choice about which rings and regioisomers to employ as mono-substituted benzene replacements, based upon the knowledge of how such replacements are likely to influence ADME-related parameters, for example to target higher solubility whilst avoiding CYP450 liabilities...
October 15, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27767381/the-effect-of-snps-in-cyp450-in-chloroquine-primaquine-plasmodium-vivax-malaria-treatment
#19
Vinicius A Sortica, Juliana D Lindenau, Maristela G Cunha, Maria DO Ohnishi, Ana Maria R Ventura, Ândrea Kc Ribeiro-Dos-Santos, Sidney Eb Santos, Luciano Sp Guimarães, Mara H Hutz
BACKGROUND: Chloroquine/primaquine is the current therapy to eliminate Plasmodium vivax infection in the Amazon region. AIMS: This study investigates CYP1A2, CYP2C8, CYP2C9, CYP3A4 and CYP3A5 genetic polymorphisms influence on cloroquine/primaquine treatment. PATIENTS & METHODS: Generalized estimating equations analyses were performed to determine the genetic influence in parasitemia and/or gametocytemia clearance over treatment time in 164 patients...
October 21, 2016: Pharmacogenomics
https://www.readbyqxmd.com/read/27766562/a-physiologically-based-pharmacokinetic-model-to-predict-human-fetal-exposure-for-a-drug-metabolized-by-several-cyp450-pathways
#20
Maïlys De Sousa Mendes, Gabrielle Lui, Yi Zheng, Claire Pressiat, Deborah Hirt, Elodie Valade, Naïm Bouazza, Frantz Foissac, Stephane Blanche, Jean-Marc Treluyer, Saik Urien, Sihem Benaboud
BACKGROUND: Pregnant women and their fetuses are exposed to numerous drugs; however, they are orphan populations with respect to the safety and efficacy of drugs. Therefore, the prediction of maternal and fetal drug exposure prior to administration would be highly useful. METHODS: A physiologically-based pharmacokinetic (PBPK) model for nevirapine, which is metabolized by the cytochrome P450 (CYP) 3A4, 2B6 and 2D6 pathways, was developed to predict maternal and fetal pharmacokinetics (PK)...
October 21, 2016: Clinical Pharmacokinetics
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