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https://www.readbyqxmd.com/read/28821467/in-vitro-characterization-of-cyp102g4-from-streptomyces-cattleya-a-self-sufficient-p450-naturally-producing-indigo
#1
Joonwon Kim, Pyung-Gang Lee, Eun-Ok Jung, Byung-Gee Kim
Self-sufficient CYP102As possess outstanding hydroxylating activity to fatty acids such as myristic acid. Other CYP102 subfamily members share substrate specificity of CYP102As, but, occasionally, unusual characteristics of its own subfamily have been found. In this study, only one self-sufficient cytochrome P450 from Streptomyces cattleya was renamed from CYP102A_scat to CYP102G4, purified and characterized. UV-Vis spectrometry pattern, FAD/FMN analysis, and protein sequence comparison among CYP102s have shown that CYP102 from Streptomyces cattleya belongs to CYP102G subfamily...
August 15, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28820269/reaction-phenotyping-to-assess-victim-drug-drug-interaction-risks
#2
Li Di
Reaction phenotyping provides critical information regarding the fraction metabolized (fm) of drug candidates. It has become increasingly important in drug discovery and development as it can be used to assess victim drug-drug interaction potential, guide structural modification to reduce fm, inform clinical study design, predict individual variability in pharmacokinetics, and evaluate the impact of genetic polymorphisms. Areas covered: The currently available in vitro and in vivo methods for reaction phenotyping are summarized along with their advantages, limitations and timings for application during the different stages of drug discovery and development...
August 18, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28818751/nutritional-modulation-of-intestinal-drug-metabolizing-cytochrome-p450-by-butyrate-of-different-origin-in-chicken
#3
Anna Kulcsár, Gábor Mátis, Andor Molnár, Janka Petrilla, László Wágner, Hedvig Fébel, Ferenc Husvéth, Károly Dublecz, Zsuzsanna Neogrády
Intestinal cytochrome P450 (CYP) enzymes play key role in the first pass metabolism of orally ingested xenobiotics, providing a primary metabolic barrier, being of special importance in maintaining animal health and production. This study was aimed to investigate how intestinal drug-metabolizing CYPs can be modulated by nutritional factors in broiler chicken. We investigated the effects of the natural growth promoter (n-)butyrate of different origin (feed supplementation of protected or non-protected forms and/or inducing caecal microbial production by supporting higher level of dietary non-starch polysaccharides [NSP]) on the activity of duodenal CYPs...
August 1, 2017: Research in Veterinary Science
https://www.readbyqxmd.com/read/28812125/recombinant-expression-and-biochemical-characterization-of-mycobacterium-tuberculosis-3fe-4s-ferredoxin-rv1786
#4
Yun Lu, Feng Qiao, Yue Li, Xiao-Hong Sang, Cong-Ran Li, Jian-Dong Jiang, Xin-Yi Yang, Xue-Fu You
Ferredoxins are iron-sulfur protein that mediate electron transfer in cytochrome P450 mono-oxygenase (CYP)-related catalytic reactions in a wide variety of organisms. Rv1786 is a putative ferredoxin, encoded by a gene located downstream of the gene encoding CYP143A1 in the Mycobacterium tuberculosis genome. However, the structure and function of Rv1786 have remained unclear. Here, the recombinant Mtb Rv1786 was expressed, purified as a His-tagged form and characterized with [3Fe-4S] clusters as its cofactors using a series of measurements including SDS-PAGE, western blot, UV/Visible, MALDI-TOF/TOF-MS, and electron paramagnetic resonance spectroscopic analysis...
August 15, 2017: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28806569/metabolic-profiling-of-dehydrodiisoeugenol-using-xenobiotic-metabolomics
#5
Qian-Qian Lv, Xiao-Nan Yang, Dong-Mei Yan, Wei-Qing Liang, Hong-Ning Liu, Xiu-Wei Yang, Fei Li
Dehydrodiisoeugenol (DDIE), a representative and major benzofuran-type neolignan in Myristica fragrans Houtt., shows anti-inflammatory and anti-bacterial actions. In order to better understand its pharmacological properties, xenobiotic metabolomics was used to determine the metabolic map of DDIE and its influence on endogenous metabolites. Total thirteen metabolites of DDIE were identified through in vivo and in vitro metabolism, and seven of them were reported for the first time in the present study. The identity of DDIE metabolites was achieved by comparison of the MS/MS fragmentation pattern with DDIE using ultra-performance chromatography electrospray ionization quadrupole time-of-flight mass spectrometry (UPLC-ESI- QTOFMS)...
July 31, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28806472/effects-of-clarithromycin-on-the-pharmacokinetics-of-evogliptin-in-healthy-volunteers
#6
E S Oh, C Choi, C O Kim, K H Kim, Y N Kim, S J Kim, M S Park
WHAT IS KNOWN AND OBJECTIVE: Evogliptin (DA-1229), a novel dipeptidyl peptidase (DPP)-4 inhibitor with high potency and selectivity, was approved in Korea for the treatment of type 2 diabetes. Preclinical studies suggest that it is metabolized by cytochrome (CYP) P450 isozymes. Based on these findings, a clinical study was designed to investigate the pharmacokinetic (PK) interaction of evogliptin with a CYP inhibitor, clarithromycin. METHODS: An open-label, two-phase, crossover study was conducted with 12 healthy subjects...
August 14, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28806298/effect-of-cyproheptadine-on-weight-and-growth-velocity-in-children-with-silver-russell-syndrome
#7
Anaïs Lemoine, Madeleine D Harbison, Jennifer Salem, Patrick Tounian, Irène Netchine, Béatrice Dubern
OBJECTIVES: Nutritional management of children with Silver-Russell syndrome (SRS) is crucial, especially before initiating growth hormone therapy (GHT). Since cyproheptadine (CYP) has been reported to be orexigenic, we retrospectively investigated the effects of CYP on changes in weight and height in SRS patients. METHODS: Anthropometric parameters (weight [W], length or height [H], relative body weight for height [W/H] and body mass index [BMI]) were recorded for 34 children with SRS receiving CYP...
August 11, 2017: Journal of Pediatric Gastroenterology and Nutrition
https://www.readbyqxmd.com/read/28805685/re-adaption-on-earth-after-spaceflights-affects-the-mouse-liver-proteome
#8
Viktoria Anselm, Svetlana Novikova, Victor Zgoda
Harsh environmental conditions including microgravity and radiation during prolonged spaceflights are known to alter hepatic metabolism. Our studies have focused on the analysis of possible changes in metabolic pathways in the livers of mice from spaceflight project "Bion-M 1". Mice experienced 30 days of spaceflight with and without an additional re-adaption period of seven days compared to control mice on Earth. To investigate mice livers we have performed proteomic profiling utilizing shotgun mass spectrometry followed by label-free quantification...
August 12, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28800957/insight-into-the-mode-of-action-and-selectivity-of-pbrm-a-covalent-steroidal-inhibitor-of-17%C3%AE-hydroxysteroid-dehydrogenase-type-1
#9
Alexandre Trottier, René Maltais, Diana Ayan, Xavier Barbeau, Jenny Roy, Martin Perreault, Richard Poulin, Patrick Lagüe, Donald Poirier
17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is involved in the biosynthesis of estradiol, the major bioactive endogenous estrogen in mammals, and constitutes an interesting therapeutic target for estrogen-dependent diseases. A steroidal derivative, 3-{[(16β,17β)-3-(2-bromoethyl)-17-hydroxyestra-1,3,5(10)-trien-16-yl]methyl} benzamide (PBRM), has recently been described as a non-estrogenic, irreversible inhibitor of 17β-HSD1. However, the mode of action of this inhibitor and its selectivity profile have not yet been elucidated...
August 8, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28800917/thyrotoxic-rubber-antioxidants-2-mercaptobenzimidazole-and-its-methyl-derivatives-cause-both-inhibition-and-induction-of-drug-metabolizing-activity-in-rat-liver-microsomes-after-repeated-oral-administration
#10
Atsuko Miyajima, Kazue Sakemi-Hoshikawa, Makoto Usami, Katsuyoshi Mitsunaga, Tomohiko Irie, Yasuo Ohno, Momoko Sunouchi
We examined the effects of thyrotoxic rubber antioxidants, 2-mercaptobenzimidazole (MBI, 0.3 mmol/kg/day) and its methyl derivatives, methyl-MBIs [4-methyl-MBI (4-MeMBI, 0.6 mmol/kg/day), 5-methyl-MBI (5-MeMBI, 0.6 mmol/kg/day), and 4(or 5)-methyl-MBI (4(5)-MeMBI, 0.6 or 1.2 mmol/kg/day)], on the drug-metabolizing activity in male rat liver microsomes by 8-day repeated oral administration. The weight of liver and thyroid were increased by all the test chemicals; MBI was most potent, and there was no additive or synergistic effect between 4-MeMBI and 5-MeMBI...
August 9, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28800141/effects-of-strong-cyp3a-inhibition-and-induction-on-the-pharmacokinetics-of-ixazomib-an-oral-proteasome-inhibitor-results-of-drug-drug-interaction-studies-in-patients-with-advanced-solid-tumors-or-lymphoma-and-a-physiologically-based-pharmacokinetic-analysis
#11
Neeraj Gupta, Michael J Hanley, Karthik Venkatakrishnan, Alberto Bessudo, Drew W Rasco, Sunil Sharma, Bert H O'Neil, Bingxia Wang, Guohui Liu, Alice Ke, Chirag Patel, Karen Rowland Yeo, Cindy Xia, Xiaoquan Zhang, Dixie-Lee Esseltine, John Nemunaitis
At clinically relevant ixazomib concentrations, in vitro studies demonstrated that no specific cytochrome P450 (CYP) enzyme predominantly contributes to ixazomib metabolism. However, at higher than clinical concentrations, ixazomib was metabolized by multiple CYP isoforms, with the estimated relative contribution being highest for CYP3A at 42%. This multiarm phase 1 study (Clinicaltrials.gov identifier: NCT01454076) investigated the effect of the strong CYP3A inhibitors ketoconazole and clarithromycin and the strong CYP3A inducer rifampin on the pharmacokinetics of ixazomib...
August 11, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28797884/drifting-of-heme-coordinating-group-in-imidazolylmethylxanthones-leading-to-improved-selective-inhibition-of-cyp11b1
#12
Silvia Gobbi, Qingzhong Hu, Christina Zimmer, Federica Belluti, Angela Rampa, Rolf W Hartmann, Alessandra Bisi
An abnormal increase in glucocorticoid levels is responsible for pathological disorders affecting different organs and systems, and the selective inhibition of appropriate steroidogenic enzymes represents a validated strategy to restore their physiological levels. In continuing our studies on CYP11B inhibitors, in this paper a small series of 6-substituted 3-imidazolylmethylxanthones was designed and synthesized, according to the data acquired from previously reported series of derivatives and from a purposely-performed docking study...
August 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28795267/cyp79-p450-monooxygenases-in-gymnosperms-cyp79a118-is-associated-with-the-formation-of-taxiphyllin-in-taxus-baccata
#13
Katrin Luck, Qidong Jia, Meret Huber, Vinzenz Handrick, Gane Ka-Shu Wong, David R Nelson, Feng Chen, Jonathan Gershenzon, Tobias G Köllner
Conifers contain P450 enzymes from the CYP79 family that are involved in cyanogenic glycoside biosynthesis. Cyanogenic glycosides are secondary plant compounds that are widespread in the plant kingdom. Their biosynthesis starts with the conversion of aromatic or aliphatic amino acids into their respective aldoximes, catalysed by N-hydroxylating cytochrome P450 monooxygenases (CYP) of the CYP79 family. While CYP79s are well known in angiosperms, their occurrence in gymnosperms and other plant divisions containing cyanogenic glycoside-producing plants has not been reported so far...
August 9, 2017: Plant Molecular Biology
https://www.readbyqxmd.com/read/28791666/clinical-pharmacokinetics-and-pharmacodynamics-of-micafungin
#14
REVIEW
Roeland E Wasmann, Eline W Muilwijk, David M Burger, Paul E Verweij, Catherijne A Knibbe, Roger J Brüggemann
Micafungin is a selective inhibitor of the synthesis of fungal 1,3-β-D-glucan, an essential component of the fungal cell wall. It is available as a powder for infusion only and is registered for the treatment of invasive and esophageal candidiasis in addition to prophylaxis of Candida infections in both adults and children. Average exposure after a single intravenous 100 mg dose in healthy adults is 133 mg h/L. Both exposure and maximum plasma concentration show linear dose proportional pharmacokinetics (PK) over a 0...
August 8, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28783601/effects-of-water-accommodated-fractions-wafs-of-crude-oil-in-two-congeneric-copepods-tigriopus-sp
#15
Jeonghoon Han, Hui-Su Kim, Il-Chan Kim, Sanghee Kim, Un-Ki Hwang, Jae-Seong Lee
Oil pollution has deleterious effects on marine ecosystems. However, the toxicity of crude oil towards Antarctic marine organisms has not been well studied. We compared the deleterious effects of water accommodated fractions (WAFs) of crude oil on reproduction, intracellular reactive oxygen species (ROS) levels, and antioxidant enzymatic activity in Antarctic (Tigriopus kingsejongensis) and temperate (Tigriopus japonicus) copepods. Reproductive rates of T. kingsejongensis and T. japonicus were significantly reduced (P < 0...
August 4, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/28783133/effects-of-co-culture-media-on-hepatic-differentiation-of-hipsc-with-or-without-huvec-co-culture
#16
Nora Freyer, Selina Greuel, Fanny Knöspel, Nadja Strahl, Leila Amini, Frank Jacobs, Mario Monshouwer, Katrin Zeilinger
The derivation of hepatocytes from human induced pluripotent stem cells (hiPSC) is of great interest for applications in pharmacological research. However, full maturation of hiPSC-derived hepatocytes has not yet been achieved in vitro. To improve hepatic differentiation, co-cultivation of hiPSC with human umbilical vein endothelial cells (HUVEC) during hepatic differentiation was investigated in this study. In the first step, different culture media variations based on hepatocyte culture medium (HCM) were tested in HUVEC mono-cultures to establish a suitable culture medium for co-culture experiments...
August 7, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28782952/biotransformation-of-chrysin-to-baicalein-selective-c6-hydroxylation-of-5-7-dihydroxyflavone-using-whole-yeast-cells-stably-expressing-human-cyp1a1-enzyme
#17
Ibidapo S Williams, Shifali Chib, Vijay K Nuthakki, Linda Gatchie, Prashant Joshi, Niteen A Narkhede, Ram A Vishwakarma, Sandip B Bharate, Saurabh Saran, Bhabatosh Chaudhuri
Naturally occurring polyphenolic compounds are of medicinal importance because of their unique antioxidant, anticancer, and chemopreventive properties. Baicalein, a naturally occurring polyhydroxy flavonoid possessing a diverse range of pharmacological activities, has been used in traditional medicines for treatment of various ailments. Apart from its isolation from natural sources, its synthesis has been reported via multistep chemical approaches. Here, we report a preparative-scale biotransformation, using whole yeast cells stably expressing human cytochrome P450 1A1 (CYP1A1) enzyme that allows regioselective C6-hydroxylation of 5,7-dihydroxyflavone (chrysin) to form 5,6,7-trihydroxyflavone (baicalein)...
August 15, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28782945/fame-2-simple-and-effective-machine-learning-model-of-cytochrome-p450-regioselectivity
#18
Martin Šícho, Christina de Bruyn Kops, Conrad Stork, Daniel Svozil, Johannes Kirchmair
We report on the further development of FAst MEtabolizer (FAME; J. Chem. Inf. MODEL: 2013, 53, 2896-2907), a collection of random forest models for the prediction of sites of metabolism (SoMs) of xenobiotics. A broad set of descriptors was explored, from simple 2D descriptors such as those used in FAME, to quantum chemical descriptors employed in some of the most accurate models for SoM prediction currently available. In line with the original FAME approach, our objective was to keep things simple and to come up with accurate and robust models that are based on a small number of 2D descriptors...
August 7, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28782406/severe-sunitinib-induced-myelosuppression-in-a-patient-with-a-cyp-3a4-polymorphism
#19
Nirav D Patel, Kanishka Chakrabory, Garrett Messmer, Koyamangalath Krishnan, John B Bossaer
Sunitinib, an oral vascular endothelial growth factor receptor, is a first-line option for metastatic renal cell carcinoma and widely used in clinical practice. Despite the proven benefit of sunitnib in metastatic renal cell carcinoma, patients may suffer from a variety of adverse events including hypertension, fatigue, hypothyroidism, hand-foot skin reactions, rash, depigmentation, and myelosuppression. Myelosuppression is usually mild, transient and resolves during the two weeks at the end of each cycle where no drug is taken...
January 1, 2017: Journal of Oncology Pharmacy Practice
https://www.readbyqxmd.com/read/28776443/exploring-the-immunopotentiation-of-chinese-yam-polysaccharide-poly-lactic-co-glycolic-acid-nanoparticles-in-an-ovalbumin-vaccine-formulation-in-vivo
#20
Li Luo, Tao Qin, Yifan Huang, Sisi Zheng, Ruonan Bo, Zhenguang Liu, Jie Xing, Yuanliang Hu, Jiaguo Liu, Deyun Wang
Biocompatible and biodegradable poly(lactic-co-glycolic acid) (PLGA) has been approved by the US Food and Drug Administration and has frequently been used to develop potential vaccine delivery systems. The immunoregulation and immunopotentiation of Chinese yam polysaccharide (CYP) have been widely demonstrated. In the current study, cell uptake mechanisms in dendritic cells (DCs) were monitored in vitro using confocal laser scanning microscopy, transmission electron microscopy, and flow cytometry. To study a CYP-PLGA nanoparticle-adjuvanted delivery system, CYP and ovalbumin (OVA) were encapsulated in PLGA nanoparticles (CYPPs) to act as a vaccine, and the formulation was tested in immunized mice...
November 2017: Drug Delivery
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