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https://www.readbyqxmd.com/read/27913846/potent-mutagenicity-of-some-non-planar-tri-and-tetrachlorinated-biphenyls-in-mammalian-cells-human-cyp2e1-being-a-major-activating-enzyme
#1
Yungang Liu, Keqi Hu, Hansi Jia, Guifang Jin, Hansruedi Glatt, Hao Jiang
Polychlorinated biphenyls (PCBs) have been classified as human carcinogens. Mutagenicity of lower chlorinated biphenyls as well as activation of transcription factors by some other congeners may contribute to the carcinogenicity of PCBs. Recently, we reported that human CYP2E1 activates mono- and dichlorobiphenyls to mutagens. However, mutagenicity of other PCBs and the involvement of other CYPs remained unknown. In this study, Chinese hamster V79-derived cell lines genetically engineered for expression of individual human CYP enzymes and a human hepatocyte (L-02) line endogenously expressing various CYPs were used to determine the activities of several tri- and tetrachlorobiphenyls to induce micronuclei and gene mutations...
December 2, 2016: Archives of Toxicology
https://www.readbyqxmd.com/read/27910729/identification-of-cytochrome-p450s-involved-in-the-metabolism-of-6-benzyl-1-benzyloxymethyl-5-iodouracil-w-1-using-human-recombinant-enzymes-and-rat-liver-microsomes-in-vitro
#2
Ying-Yuan Lu, Hai-Xu Cheng, Xin Wang, Xiao-Wei Wang, Jun-Yi Liu, Pu Li, Ya-Qing Lou, Jun Li, Chuang Lu, Guo-Liang Zhang
1. The aim of this study was to identify the hepatic metabolic enzymes, which involved in the biotransformation of 6-benzyl-1-benzyloxymethyl-5-iodouracil (W-1), a novel non-nucleoside reverse transcriptase inhibitor (NNRTIs) in rat and human in vitro. 2. The parent drug of W-1 was incubated with RLMs or recombinant CYPs (CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4 and CYP3A5, respectively) in the presence or absence of NADPH regenerating system. The metabolites of W-1 were analyzed with liquid chromatography-ion trap-time of flight-mass spectrometry (LC-IT-TOF-MS)...
December 2, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/27910036/evaluation-of-the-pharmacokinetic-interaction-between-venetoclax-a-selective-bcl-2-inhibitor-and-warfarin-in-healthy-volunteers
#3
Ahmed Hamed Salem, Beibei Hu, Kevin J Freise, Suresh K Agarwal, Dilraj S Sidhu, Shekman L Wong
BACKGROUND AND OBJECTIVE: Venetoclax is a selective, B-cell lymphoma-2 inhibitor that has demonstrated clinical efficacy in a variety of hematological malignancies. In vitro data indicated weak cytochrome P450 (CYP) 2C9 inhibition by venetoclax; however, it is not predicted to cause clinically relevant inhibition due to high plasma protein binding. A Phase 1 study was conducted in healthy volunteers to evaluate the effect of venetoclax on warfarin pharmacokinetics. METHODS: Subjects received a single oral dose of 5 mg warfarin on day 1 of both periods 1 and 2, separated by a 14 days washout...
December 2, 2016: Clinical Drug Investigation
https://www.readbyqxmd.com/read/27909995/solithromycin-a-novel-fluoroketolide-for-the-treatment-of-community-acquired-bacterial-pneumonia
#4
REVIEW
George G Zhanel, Erika Hartel, Heather Adam, Sheryl Zelenitsky, Michael A Zhanel, Alyssa Golden, Frank Schweizer, Bala Gorityala, Philippe R S Lagacé-Wiens, Andrew J Walkty, Alfred S Gin, Daryl J Hoban, Joseph P Lynch, James A Karlowsky
Solithromycin is a novel fluoroketolide developed in both oral and intravenous formulations to address increasing macrolide resistance in pathogens causing community-acquired bacterial pneumonia (CABP). When compared with its macrolide and ketolide predecessors, solithromycin has several structural modifications which increase its ribosomal binding and reduce its propensity to known macrolide resistance mechanisms. Solithromycin, like telithromycin, affects 50S ribosomal subunit formation and function, as well as causing frame-shift errors during translation...
December 1, 2016: Drugs
https://www.readbyqxmd.com/read/27904813/glycyrrhetinic-acid-might-increase-the-nephrotoxicity-of-bakuchiol-by-inhibiting-cytochrome-p450-isoenzymes
#5
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/27904043/role-of-the-drug-metabolizing-enzyme-cyp-during-mouse-liver-development
#6
Wataru Ochiai, Akiyo Hirose, Taisuke Kawamura, Kyoko Komachi, Yuka Yamamoto, Satoshi Kitaoka, Jo Hatogai, Yoshiki Kusunoki, Risako Kon, Nobutomo Ikarashi, Kiyoshi Sugiyama
The drug-metabolizing enzyme CYP is mainly involved in the metabolism of various substances in the liver, such as drugs, endogenous substances, and carcinogens. Recent reports have also revealed that CYP1B1 plays a major role in the developmental process. Because the level of CYP expression is markedly high in the liver, we hypothesize that CYP plays a role in the developmental process of the liver. To verify this hypothesis, we analyzed the expression patterns of various CYP molecular species and their functions during the differentiation of embryonic stem cells (ES cells) into hepatocytes and the developmental process in mice...
2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27904037/analysis-of-cyp2r1-and-cyp26a1-expression-patterns-in-regeneration-in-mice-with-liver-injury
#7
Akiyo Hirose, Wataru Ochiai, Yuka Yamamoto, Masashi Fukaya, Hiroshi Iwasaki, Nozomi Wakui, Ayumi Takahashi, Yusuke Takahashi, Satoshi Kitaoka, Jo Hatogai, Nobutomo Ikarashi, Kiyoshi Sugiyama
Cytochrome P450 enzymes (CYPs) are involved in the metabolism of various substances in the liver and small intestine and show markedly higher expression levels in the liver compared to other organs. The liver exhibits a remarkable capacity to regenerate. After excision of 70% of the liver, the organ can regenerate to its original size in approximately 1 week. Unlike the normal liver, in the injured liver, hepatic stem cells known as oval cells are considered to play an important role in regeneration. However, the role of CYPs in liver regeneration remains unclear...
2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27902373/feline-coronavirus-replication-is-affected-by-both-cyclophilin-a-and-cyclophilin-b
#8
Yoshikazu Tanaka, Yuka Sato, Takashi Sasaki
Feline coronavirus (FCoV) causes the fatal disease feline infectious peritonitis (FIP), which is currently incurable by drug treatment, and no effective vaccines are available. Cyclosporin A (CsA), a cyclophilin (Cyp) inhibitor, inhibits the replication of FCoV in vitro and in vivo as well as the replication of human and animal coronaviruses (CoVs). However, the mechanism underlying the regulation of CoV replication by CsA is unknown. In this study, we analyzed the role of Cyps in FCoV replication using knockdown (KD) and knockout (KO) cells specific to Cyps...
November 21, 2016: Journal of General Virology
https://www.readbyqxmd.com/read/27899995/systematic-tracking-of-disrupted-modules-identifies-significant-genes-and-pathways-in-hepatocellular-carcinoma
#9
Meng-Hui Zhang, Qin-Hai Shen, Zhao-Min Qin, Qiao-Ling Wang, Xi Chen
The objective of the present study is to identify significant genes and pathways associated with hepatocellular carcinoma (HCC) by systematically tracking the dysregulated modules of re-weighted protein-protein interaction (PPI) networks. Firstly, normal and HCC PPI networks were inferred and re-weighted based on Pearson correlation coefficient. Next, modules in the PPI networks were explored by a clique-merging algorithm, and disrupted modules were identified utilizing a maximum weight bipartite matching in non-increasing order...
November 2016: Oncology Letters
https://www.readbyqxmd.com/read/27896399/cytochrome-p450-mediated-metabolism-of-triclosan-attenuates-its-cytotoxicity-in-hepatic-cells
#10
Yuanfeng Wu, Priyanka Chitranshi, Lucie Loukotková, Gonçalo Gamboa da Costa, Frederick A Beland, Jie Zhang, Jia-Long Fang
Triclosan is a widely used broad-spectrum anti-bacterial agent. The objectives of this study were to identify which cytochrome P450 (CYP) isoforms metabolize triclosan and to examine the effects of CYP-mediated metabolism on triclosan-induced cytotoxicity. A panel of HepG2-derived cell lines was established, each of which overexpressed a single CYP isoform, including CYP1A1, CYP1A2, CYP1B1, CYP2A6, CYP2A7, CYP2A13, CYP2B6, CYP2C8, CYP2C9, CYP2C18, CYP2C19, CYP2D6, CYP2E1, CYP3A4, CYP3A5, CYP3A7, CYP4A11, and CYP4B1...
November 28, 2016: Archives of Toxicology
https://www.readbyqxmd.com/read/27895582/introduction-of-an-n-glycosylation-site-into-udp-glucuronosyltransferase-2b3-alters-its-sensitivity-to-cytochrome-p450-3a1-dependent-modulation
#11
Tatsuro Nakamura, Naho Yamaguchi, Yuu Miyauchi, Tomoki Takeda, Yasushi Yamazoe, Kiyoshi Nagata, Peter I Mackenzie, Hideyuki Yamada, Yuji Ishii
Our previous studies have demonstrated functional protein-protein interactions between cytochrome P450 (CYP) 3A and UDP-glucuronosyltransferase (UGT). However, the role of carbohydrate chains of UGTs in the interaction with CYP is not well understood. To address this issue, we examined whether CYP3A1 modulates the function of UGT2B3 which lacks potential glycosylation sites. We also examined whether the introduction of N-glycosylation to UGT2B3 affects CYP3A-dependent modulation of UGT function. To introduce a potential glycosylation site into UGT2B3, Ser 316 of UGT2B3 was substituted with Asn by site-directed mutagenesis...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27895462/effects-of-resveratrol-on-p-glycoprotein-and-cytochrome-p450-3a-in-vitro-and-on-pharmacokinetics-of-oral-saquinavir-in-rats
#12
Jiapeng Li, Yang Liu, Jingru Zhang, Xiaotong Yu, Xiaoling Wang, Libo Zhao
BACKGROUND: The intestinal cytochrome P450 3A (CYP 3A) and P-glycoprotein (P-gp) present a barrier to the oral absorption of saquinavir (SQV). Resveratrol (RESV) has been indicated to have modulatory effects on P-gp and CYP 3A. Therefore, this study was to investigate the effects of RESV on P-gp and CYP 3A activities in vitro and in vivo on oral SQV pharmacokinetics in rats. METHODS: In vitro, intestinal microsomes were used to evaluate RESV effect on CYP 3A-mediated metabolism of SQV; MDR1-expressing Madin-Darby canine kidney (MDCKII-MDR1) cells were employed to assess the impact of RESV on P-gp-mediated efflux of SQV...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27892922/convergence-and-divergence-of-bitterness-biosynthesis-and-regulation-in-cucurbitaceae
#13
Yuan Zhou, Yongshuo Ma, Jianguo Zeng, Lixin Duan, Xiaofeng Xue, Huaisong Wang, Tao Lin, Zhiqiang Liu, Kewu Zeng, Yang Zhong, Shu Zhang, Qun Hu, Min Liu, Huimin Zhang, James Reed, Tessa Moses, Xinyan Liu, Peng Huang, Zhixing Qing, Xiubin Liu, Pengfei Tu, Hanhui Kuang, Zhonghua Zhang, Anne Osbourn, Dae-Kyun Ro, Yi Shang, Sanwen Huang
Differentiation of secondary metabolite profiles in closely related plant species provides clues for unravelling biosynthetic pathways and regulatory circuits, an area that is still underinvestigated. Cucurbitacins, a group of bitter and highly oxygenated tetracyclic triterpenes, are mainly produced by the plant family Cucurbitaceae. These compounds have similar structures, but differ in their antitumour activities and ecophysiological roles. By comparative analyses of the genomes of cucumber, melon and watermelon, we uncovered conserved syntenic loci encoding metabolic genes for distinct cucurbitacins...
November 28, 2016: Nature Plants
https://www.readbyqxmd.com/read/27892656/cytochrome-p450-bioconjugate-as-a-nanovehicle-for-improved-chemotherapy-treatment
#14
Katrin Quester, Karla Juarez-Moreno, Isamel Secundino, Yvonne Roseinstein, Karla P Alejo, Alejandro Huerta-Saquero, Rafael Vazquez-Duhalt
Cancer is still a growing public health problem, especially breast cancer that is one of the most important cancers in women. Chemotherapy, even though a successful treatment, is accompanied by severe side effects. Moreover, most of the drugs used for chemotherapy are administered as prodrugs and need to be transformed to the active form by cytochromes P450 (CYPs). In addition, increasing numbers of cancer tissues show lower CYP activity than the surrounding healthy tissues in which prodrugs are preferentially activated causing cytotoxicity...
November 28, 2016: Macromolecular Bioscience
https://www.readbyqxmd.com/read/27891824/lipidomic-profiling-of-high-fat-diet-induced-obesity-in-mice-importance-of-cytochrome-p450-derived-fatty-acid-epoxides
#15
Weicang Wang, Jun Yang, Weipeng Qi, Haixia Yang, Chang Wang, Bowen Tan, Bruce D Hammock, Yeonhwa Park, Daeyoung Kim, Guodong Zhang
OBJECTIVE: Enzymatic metabolism of polyunsaturated fatty acids leads to formation of bioactive lipid metabolites (LMs). Previous studies have shown that obesity leads to deregulation of LMs in adipose tissues. However, most previous studies have focused on a single or limited number of LMs, and few systematical analyses have been carried out. METHODS: A LC-MS/MS-based lipidomics approach was used, which can analyze >100 LMs produced by cyclooxygenase, lipoxygenase, and cytochrome P450 (CYP) enzymes, to analyze the profile of LMs in high-fat diet-induced obesity in mice...
November 28, 2016: Obesity
https://www.readbyqxmd.com/read/27891633/direct-inhibition-of-re-du-ning-injection-and-its-active-compounds-on-human-liver-cytochrome-p450-enzymes-by-a-cocktail-method
#16
Danyu Kang, Ting Geng, Yuanpei Lian, Yanjing Li, Gang Ding, Wenzhe Huang, Shiping Ma, Zhenzhong Wang, Zheng Ma, Wei Xiao
The aim of this study was to investigate the direct inhibitory effects of Re Du Ning Injection (RDN) and its active compounds on the major CYP isoforms (CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 and CYP3A4) of human liver microsomes by "a cocktail method". The activity of each CYP isform was represented as the formation rate of the specific metabolite from relevant substrate. Then a sensitive and specific ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed and validated to simultaneously analyze the seven metabolites...
November 28, 2016: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/27890789/cyclosporin-derivatives-inhibit-hepatitis-b-virus-entry-without-interfering-the-ntcp-transporter
#17
Satomi Shimura, Koichi Watashi, Kento Fukano, Michael Peel, Ann Sluder, Fumihiro Kawai, Masashi Iwamoto, Senko Tsukuda, Junko S Takeuchi, Takeshi Miyake, Masaya Sugiyama, Yuki Ogasawara, Sam-Yong Park, Yasuhito Tanaka, Hiroyuki Kusuhara, Masashi Mizokami, Camille Sureau, Takaji Wakita
BACKGROUND&AIMS: Most of the specific inhibitors of hepatitis B virus (HBV) entry, including myrcludex-B and cyclosporin A (CsA), target an HBV entry receptor, sodium taurocholate cotransporting polypeptide (NTCP). As all these agents have capacities to impair the NTCP transporter activity for bile acid uptake and thus may cause significant adverse effects, we aim to identify small molecules that inhibit HBV entry but least affecting the NTCP transporter function. METHODS: We focused on derivatives of CsA, which originally inhibited both HBV entry and NTCP-mediated bile acid uptake, to analyze the possibility to distinguish these two activities...
November 24, 2016: Journal of Hepatology
https://www.readbyqxmd.com/read/27890698/clementine-juice-has-the-potential-for-drug-interactions-in-vitro-comparison-with-grapefruit-and-mandarin-juice
#18
Dirk Theile, Nicolas Hohmann, Dominik Kiemel, Giuseppe Gattuso, Davide Barreca, Gerd Mikus, Walter Emil Haefeli, Vedat Schwenger, Johanna Weiss
Adverse drug interactions due to grapefruit juice are well known prompting warnings even in drug labels. Similar issues have not been reported for clementines and available data is scarce, despite of genetic descent. We observed substantially increased tacrolimus trough concentrations in a renal transplant patient consuming high clementine amounts and, thus, scrutinised the effects of clementine juice on drug metabolism and drug transporters in vitro and compared it to the effects of mandarin and grapefruit juice...
November 24, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27890614/structural-insights-into-the-binding-of-lauric-acid-to-cyp107l2-from-streptomyces-avermitilis
#19
Songhee Han, Tan-Viet Pham, Joo-Hwan Kim, Young-Ran Lim, Hyoung-Goo Park, Dabin Jeong, Chul-Ho Yun, Young-Jin Chun, Lin-Woo Kang, Donghak Kim
Streptomyces avermitilis is an actinobacterium known to produce clinically useful macrolides including avermectins. CYP107L2 from S. avermitilis shares a high sequence similarity with the PikC (CYP107L1) from S. venezuelae. To elucidate the structural features of CYP107L2, we conducted biochemical and structural characterization of CYP107L2 from S. avermitilis. The CYP107L2 gene was cloned, and its recombinant protein was expressed and purified. The CYP107L2 showed a low-spin state of heme, and the reduced form yielded the CO difference spectra with a maximal absorption at 449 nm...
November 25, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27888364/in-vitro-reconstitution-of-the-cyclosporine-specific-p450-hydroxylases-using-heterologous-redox-partner-proteins
#20
Yue Sun, Li Ma, Dongfei Han, Lei Du, Fengxia Qi, Wei Zhang, Jingran Sun, Shan Huang, Eung-Soo Kim, Shengying Li
The cytochrome P450 enzymes (CYPs) CYP-sb21 from Sebekia benihana and CYP-pa1 from Pseudonocardia autotrophica are able to hydroxylate the immunosuppressant cyclosporin A (CsA) in a regioselective manner, giving rise to the production of two hair-stimulating agents (with dramatically attenuated immunosuppressant activity), γ-hydroxy-N-methyl-L-Leu4-CsA (CsA-4-OH) and γ-hydroxy-N-methyl-L-Leu9-CsA (CsA-9-OH). Recently, the in vitro activity of CYP-sb21 was identified using several surrogate redox partner proteins...
November 25, 2016: Journal of Industrial Microbiology & Biotechnology
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