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Cytochrome P

Olivier J David, Rhett Behrje, Parasar Pal, Hisanori Hara, Christian D Lates, Robert Schmouder
This open-label, single-sequence study in healthy subjects investigated the effects of steady-state carbamazepine on the pharmacokinetic (PK) profile of a single 2-mg dose of fingolimod. In period 1, a single oral dose of fingolimod 2 mg (day 1) was followed by PK and safety assessments up to 36 days. In period 2, carbamazepine was administered in flexible, up-titrated doses (600 mg twice daily maximum) for 49 days. Fingolimod was administered on day 35, followed by a study completion evaluation (day 71)...
April 25, 2018: Clinical Pharmacology in Drug Development
Ling Liu, Zile Huang, Jingjing Chen, Jiangang Wang, Shuying Wang
Protein phosphatase 2A (PP2A) is an important enzyme within various signal transduction pathways. The present study was investigated PP2A mediates JS-K-induced apoptosis by affecting Bcl-2 family protein. JS-K showed diverse inhibitory effects in five HCC cell lines, especially HepG2 cells. JS-K caused a dose- and time-dependent reduction in cell viability and increased in levels of LDH release. Meanwhile, JS-K- induced apoptosis was characterized by mitochondrial membrane potential reduction, Hoechst 33342+ /PI+ dual staining, release of cytochrome c (Cyt c), and activation of cleaved caspase-9/3...
April 25, 2018: Journal of Cellular Biochemistry
Shan Feng, Xin He, Peiru Zhong, Jinyi Zhao, Cong Huang, Zhuohan Hu
Radix Angelicae dahuricae , containing coumarins, which might affect cytochrome P450 enzyme (CYP450) activity, has been co-administered with ligustrazine, a substrate of CYP450s, for the clinical treatment of migraine. However, whether a pharmacokinetic-based synergy exists between Radix Angelicae dahuricae and ligustrazine is still unknown. In this study, the total coumarin extract (TCE) of Radix Angelicae dahuricae (50 mg/kg, orally) reinforced the anti-migraine activity of ligustrazine by declining head scratching, plasma calcitonin gene-related peptide, and serum nitric oxide, as well as increasing plasma endothelin levels in rats ( p < 0...
April 25, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Enayatollah Seydi, Ahmad Salimi, Hamid Reza Rasekh, Zhaleh Mohsenifar, Jalal Pourahmad
To evaluate the cytotoxicity effects of luteolin (LUT) and kaempferol (KAE) via reactive oxygen species (ROS) mediated mitochondrial targeting on hepatocytes obtained from the liver of hepatocellular carcinoma (HCC) rats. In this study, HCC induced by diethylnitrosamine (DEN) and 2-acetylaminofluorene (2-AAF). In the following, rat liver hepatocytes and mitochondria were isolated and tested for every eventual apoptotic and anti-HCC effects of LUT and KAE. The results of MTT assay showed that LUT and KAE were able to induce selective cytotoxicity in hepatocytes of HCC group in a dose- and time-dependent manner...
April 25, 2018: Nutrition and Cancer
Wenting Shang, Xu Si, Zhongkai Zhou, Padraig Strappe, Chris Blanchard
In this study, the level of gamma-aminobutyric acid (GABA) in wheat bran was increased to be six times higher through the action of endogenous glutamate decarboxylase compared with untreated bran. The process of GABA formation in wheat bran also led to an increased level of phenolic compounds with enhanced antioxidant capacity 2 times higher than the untreated status. The interventional effect of a diet containing GABA-enriched bran on hyperinsulinemia induced by a high-fat diet (HFD) was investigated in a rat model...
April 25, 2018: Food & Function
Guo Wei Zhang, Chang Qin Yang, Rui Xian Liu, Wan Chao Ni
With early-maturing cotton cultivar CCRI-50 widely grown in China as experimental material, water culture experiment was conducted to study the effects of p-hydroxybenzoic acid and phloroglucinol with different concentrations (0.8, 4.0, and 20.0 mmol·L-1 ) on generation rate of reactive oxygen, changes of antioxidant enzyme activities and mitochondria function of cotton roots. Results showed that p-hydroxybenzoic acid and phloroglucinol treatments inhibited the cotton root growth, reduced SOD, POD, CAT and H+ -ATPase activities in root mitochondria, increased the generation rate of O2- · and H2 O2 content...
January 2018: Ying Yong Sheng Tai Xue Bao, the Journal of Applied Ecology
Takaya Uno, Kyoichi Wada, Sachi Matsuda, Yuka Terada, Akira Oita, Atsushi Kawase, Mitsutaka Takada
BACKGROUND AND OBJECTIVE: Tacrolimus, a major immunosuppressant used after transplantation, is associated with large interindividual variation involving genetic polymorphisms in metabolic processes. A common variant of the cytochrome P450 (CYP) 3A5 gene, CYP3A5*3, affects blood concentrations of tacrolimus. However, tacrolimus pharmacokinetics at the early stage of transplantation have not been adequately studied in heart transplantation. We retrospectively examined the impact of the CYP3A5 genotype on tacrolimus pharmacokinetics at the early stage of heart transplantation...
April 24, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Jeffrey W Johnson, Jessica Worthington Wilmer
Three new species of pinguipedid fishes from northern Australia are described based on specimens collected by deep water demersal trawling. Parapercis algrahami sp. nov. is recorded from off Dunk Island, Qld, south to Newcastle, NSW, in 67-333 m. It is distinct in having five narrow transverse dark bars across the upper body and a dark spot dorsally on the caudal-fin base, 6 canine teeth in outer row at front of lower jaw, palatines with 1-2 rows of teeth, and predorsal scales extending far forward on the nape to the posterior portion of the interorbital region...
March 1, 2018: Zootaxa
Yukio Iwatsuki, Stephen J Newman, Fumiya Tanaka, Barry C Russell
Psammoperca datnioides Richardson 1848, long considered a synonym of P. waigiensis (Cuvier in Cuvier Valenciennes 1828), is redescribed as a valid species of Psammoperca Richardson 1848. The species is likely to be endemic to Australia, where it was formerly considered to be P. waigiensis, but differs from P. waigiensis in having the following characters: more slender body (mean depth 28.9% of SL vs. mean depth 36.7% of SL in P.  waigiensis), pored lateral-line scales 49-54 (vs. 46-48 in P. waigiensis), scale rows above and below lateral line 6½ / 10½-11½ (vs 4½ / 9½-10½ in P...
March 29, 2018: Zootaxa
Ke-Long Jiao, Hao Wang, De-Wei Wei, Jian-You Mo, Yuan-Hong Wang, Wen-Jun Bu, Peter Kolesik
Larvae of a previously unknown species of gall midge were found feeding on young fruit of mango, Mangifera indica (Anacardiaceae), in Guangxi Autonomous Region in southern China, causing severe damage to the crop. The new species is named Procontarinia fructiculi Jiao, Wang, Bu Kolesik, its morphology is described, the basic biology is given, and the Cytochrome Oxidase subunit I (COI) mitochondrial gene segment is sequenced and compared to other congeners. Procontarinia contains now 16 described species, each feeding on mango...
April 23, 2018: Zootaxa
Michael P Hammer, Gerald R Allen, Keith C Martin, Mark Adams, Brendan C Ebner, Tarmo A Raadik, Peter J Unmack
The freshwater melanotaeniid genus Cairnsichthys is endemic to a relatively small area of specialised habitat within the Wet Tropics bioregion of north-eastern Queensland, Australia. It was previously considered as monotypic, including only a single species, C. rhombosomoides (Nichols Raven, 1928). The recent discovery of an apparently-isolated population in the Daintree rainforest, approximately 120 km north of the known range extent, prompted a detailed investigation of its taxonomic status using a combined lines of evidence approach...
April 23, 2018: Zootaxa
Naİme Arslan, Tarmo Timm, VerÓnica Rojo, AntÓn VizcaÍno, RÜdiger M Schmelz
Enchytraeus polatdemiri sp. nov. (Enchytaeidae, Oligochaeta) was discovered in the framework of a sampling campaign of the benthic invertebrate fauna of the hyperalkaline Lake Van in Eastern Anatolia, Turkey, the third-largest closed lake and the largest soda lake on Earth. It was the only oligochaete species found in all samples. DNA sequencing included a fragment of the mitochondrial cytochrome c oxidase subunit I (COI) gene, and a fragment of the nuclear histone 3 (H3) gene. For comparison, specimens from laboratory cultures of E...
February 21, 2018: Zootaxa
Hassib Narchi, Pramathan Thachillath, Abdul-Kader Souid
BACKGROUND: Hypoglycemia occurs frequently in the neonate and may result in neurologic dysfunction. Its impact on the kinetics of cellular respiration and bioenergetics in the neonatal brain remains to be explored. AIMS: Develop murine model to investigate the effects of hypoglycemia on neonatal brain bioenergetics. STUDY DESIGN: Forebrain fragments were excised from euthanized BALB/c pups aged <24 hours to 14 days. We measured cellular respiration (μM O2 min-1...
2018: Journal of Neonatal-perinatal Medicine
L Shao, Y-Y Gu, C-H Jiang, C-Y Liu, L-P Lv, J-N Liu, Y Zou
OBJECTIVE: Non-small cell lung cancer (NSCLC) is the most common type of lung cancer, which is the leading cause of cancer-related morbidity and mortality worldwide. The carbon monoxide-releasing molecules (CO-RMs) are transition metal carbonyls with the capacity to release carbon monoxide (CO). The aims of our study were to assess the effects and underlying mechanisms of CO-releasing molecules-2 (CORM-2) on proliferation, migration, invasion and apoptosis in NSCLC cells, and to evaluate its potential application for lung cancer...
April 2018: European Review for Medical and Pharmacological Sciences
Muhammad Qasim, Wang Baohua, Huasong Zou, Yongwen Lin, Chandra Kanta Dash, Bamisope Steve Bamisile, Mubasher Hussain, Zhao Zhiwen, Liande Wang
Asian citrus psyllid (ACP), Diaphorina citri Kuwayama (Hemiptera: Liviidae), is a severely devastating pest of Rutaceae plants, mainly citrus, across the globe, and causal agent of Huanglongbing (HLB) disease. To find out the genetic relationship and diversity among the populations of ACP and associated Candidatus Liberibacter asiaticus (CLas) from two countries (China and Pakistan), sequence data of three different genes, cytochrome oxidase subunit I (COI), Cu-transporting protein (ATOX1) and 16S rRNA, were used to characterize all populations...
April 20, 2018: Molecular Phylogenetics and Evolution
M J Dickson, C L Hager, A Al-Shaibi, P Q Thomas, L H Baumgard, J W Ross, A F Keating
Environmental conditions that impede heat dissipation and increase body temperature cause heat stress (HS). The study objective was to evaluate impacts of HS on the follicular phase of the estrous cycle. Post-pubertal gilts (126.0 ± 21.6 kg) were orally administered altrenogest to synchronize estrus, and subjected to either 5 d of thermal neutral (TN; 20.3 ± 0.5°C; n = 6) or cyclical HS (25.4 - 31.9°C; n = 6) conditions during the follicular phase preceding behavioral estrus. On d 5, blood samples were obtained, gilts were euthanized, and ovaries collected...
April 19, 2018: Journal of Animal Science
Naveen A Mallangada, Joselin M Vargas, Swaroopa Thomas, Matthew G DiGiovanni, Brandon M Vaeth, Matthew D Nemesure, Ruixue Wang, Joseph F LaComb, Jennie L Williams, Lorne M Golub, Francis Johnson, Gerardo G Mackenzie
Pancreatic Cancer (PC) is a deadly disease in need of new therapeutic options. We recently developed a novel tricarbonylmethane agent (CMC2.24) as a therapeutic agent for PC, and evaluated its efficacy in preclinical models of PC. CMC2.24 inhibited the growth of various human PC cell lines in a concentration and time-dependent manner. Normal human pancreatic epithelial cells were resistant to CMC2.24, indicating selectivity. CMC2.24 reduced the growth of subcutaneous and orthotopic PC xenografts in mice by up to 65% (p < 0...
April 23, 2018: Molecular Carcinogenesis
Ranjeet Prasad Dash, R Jayachandra Babu, Nuggehally R Srinivas
The recent approval of edaravone has provided an intravenous option to treat amyotrophic lateral sclerosis (ALS) in addition to the existing oral agent, riluzole. The present work was primarily undertaken to provide a comprehensive clinical pharmacokinetic summary of the two approved ALS therapeutics. The key objectives of the review were to (i) tabulate the clinical pharmacokinetics of riluzole and edaravone with emphasis on absorption, distribution, metabolism and excretion (ADME) properties; (ii) provide a comparative scenario of the pharmacokinetics of the two drugs wherever possible; and (iii) provide perspectives and introspection on the gathered clinical pharmacokinetic data of the two drugs with appropriate conjectures to quench scientific curiosity...
April 23, 2018: Clinical Pharmacokinetics
Xu-Gui Chen, Li-Hua Chen, Ru-Xiang Xu, Hong-Tian Zhang
PURPOSE: To investigate the combination effect of methylprednisolone (MP) and mitochondrial division inhibitor-1 (Mdivi-1) on the neurological function recovery of rat spinal cord injury (SCI) model. METHODS: The weight-drop method was used to establish the rat SCI model; then, rats were randomized into sham group, SCI group, MP group, Mdivi-1 group and MP+Mdivi-1 group. Motor function scores were quantified to evaluate locomotor ability; HE staining was used to assess spinal cord histopathology; tissue water content, oxidative stress, tissue mitochondrial function, neurons apoptosis, and apoptosis-related protein expression were detected...
April 23, 2018: Child's Nervous System: ChNS: Official Journal of the International Society for Pediatric Neurosurgery
Ting Wang, Fangyi Long, Gang Jiang, Hong Cai, Qian Jiang, Kai Cheng, Zhiqiang Hu, Yuxi Wang
Docetaxel, frequently used for the treatment of breast cancer, is mainly metabolized via hepatic cytochrome P450 (CYP) 3A in humans and is also a substrate of P-glycoprotein (P-gp). Wogonin has been shown to be able to modulate the activities of CYPs and P-gp, and it could be served as an adjuvant chemotherapeutic agent. However, the impacts of co-administration of wogonin and docetaxel on their pharmacokinetics have not been studied for lacking analytical method of their simultaneous measurement. In the present study, we established an HPLC-MS/MS method for simultaneous measurement of wogonin and docetaxel in rat plasma, and it was then utilized to explore the pharmacokinetics of wogonin and the herb-drug interactions between wogonin and docetaxel after the combined administration in rats with mammary tumors...
April 21, 2018: Biomedical Chromatography: BMC
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