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The α2,3-selective potentiator of GABAA receptors, KRM-II-81, reduces nociceptive-associated behaviors induced by formalin and spinal nerve ligation in rats

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PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR 2019年 180卷 22-31页

作者： Witkin, J. M. Cerne, R. Davis, P. G. freeman, K. B. do Carmo, J. M. Rowlett, J. K. Methuku, K. R. Okun, A. Gleason, S. D. Li, X. Krambis, M. J. Poe, M. Li, G. Schkeryantz, J. M. Jahan, R. Yang, L. Guo, W. Golani, L. K. Anderson, W. H. Catlow, J. T. Jones, T. M. Porreca, f. Smith, J. L. Knopp, K. L. Cook, J. M. Eli Lilly & Co Lilly Res Labs Indianapolis IN 46285 USA Univ Wisconsin Dept Chem & Biochem Milwaukee WI 53201 USA Millsaps Coll Jackson MS 39210 USA Univ Mississippi Med Ctr Dept Psychiat & Human Behav Jackson MS 39216 USA Univ Mississippi Med Ctr Dept Physiol & Biophys Jackson MS 39216 USA Univ Arizona Dept Pharmacol Tucson AZ USA Indiana Univ Sch Med Lab Antiepilept Drug Discovery Dept Neurol Surg Indianapolis IN 46202 USA

Clinical evidence indicates that positive allosteric modulators (PAMs) of GABA(A) receptors have analgesic benefit in addition to efficacy in anxiety disorders. However, the utility of GABA(A) receptor PAMs as analgesics is compromised by the central nervous system side effects of non-selective potentiators. A selective potentiator of GABA(A) receptors associated with alpha 2/3 subunits, KRM-II-81(5-(8-ethynyl-6-(pyridin-2-yl)-4H-benzo [f] imidazo[1,5-a] [1,4]diazepin-3-yl)oxazole), has demonstrated anxiolytic, anticonvulsant, and antinociceptive effects in rodents with reduced motoric side effects. The present study evaluated the potential of KRMII-81 as a novel analgesic. Oral administration of KRM-II-81 attenuated formalin-induced flinching;in contrast, diazepam was not active. KRM-II-81 attenuated nociceptive-associated behaviors engendered by chronic spinal nerve ligation (L5/L6). Diazepam decreased locomotion of rats at the dose tested in the formalin assay (10 mg/kg) whereas KRM-II-81 produced small decreases that were not dose-dependent (10-100 mg/kg). Plasma and brain levels of KRM-II-81 were used to demonstrate selectivity for alpha 2/3- over al-associated GABA(A) receptors and to define the degree of engagement of these receptors. Plasma and brain concentrations of ICRM-H-81 were positively-associated with analgesic efficacy. GABA currents from isolated rat dorsal-root ganglion cultures were potentiated by KRM-II-81 with an ED50 of 32 nM. Measures of respiratory depression were reduced by alprazolam whereas KRM-II-81 was either inactive or produced effects with lower potency and efficacy. These findings add to the growing body of data supporting the idea that alpha 2/3-selective GABA(A) receptor PAMs will have efficacy and tolerability as pain medications including those for neuropathic pain. Given their predicted anxiolytic effects, alpha 2/3-selective GABA(A) receptor PAMs offer an additional inroad into the management of pain.

关键词： HZ-166 HZ-166 ethyl 8-ethynyl-6-(pyridin-2-yl)-4 H -benzo[ f ]imidazo[1,5- a ][1,4]diazepine-3-carboxylate KRM-II-81 5-(8-ethynyl-6-(pyridin-2-yl)-4 H -benzo[ f ]imidazo[1,5- a ][1,4]diazepin-3-yl)oxazole

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Prenatal BPA and its analogs BPB, BPf, and BPS exposure and reproductive axis function in the male offspring of Sprague Dawley rats

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HUMAN & EXPERIMENTAL TOXICOLOGY 2019年第12期38卷 1344-1365页

作者： Ullah, A. Pirzada, M. Jahan, S. Ullah, H. Razak, S. Rauf, N. Khan, M. J. Mahboob, S. Z. Quaid I Azam Univ Dept Anim Sci Reprod Physiol Lab Islamabad Pakistan

Research in the past has indicated associated long-term and low levels of exposure of bisphenol A (BPA) in early life and neuroendocrine disorders, such as obesity, precocious puberty, diabetes, and hypertension. BPA and its analogs bisphenol B (BPB), bisphenol f (BPf), and bisphenol S (BPS) have been reported to have similar or even more toxic effect as compared to BPA. Exposure of rats to BPA and its analogs BPB, BPf, and BPS resulted in decreased sperm production, testosterone secretion, and histological changes in the reproductive tissues of male rats. In the present study, BPA, BPB, BPf, and BPS were administered in drinking water at concentrations of (5, 25, and 50 mu g/L) from pregnancy day (PD) 1 to PD 21. Body weight (BW), hormonal concentrations, antioxidant enzymes, and histological changes were determined in the reproductive tissues. BPA and its analogs prenatal exposure to female rats induced significant statistical difference in the antioxidant enzymes, plasma testosterone, and estrogen concentrations in the male offspring when compared with the control. Histological parameters of both testis and epididymis revealed prominent changes in the reproductive tissues. The present study suggests that BPA and its analogs BPB, BPf, and BPS different concentrations led to marked alterations in the development of the male reproductive system.

关键词： Bisphenols (A B f and S) oxidative stress antioxidant enzymes hormones histology

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Effect of Grain Sizes on Thermoelectric Properties of Extruded Samples of Bi0.5Sb1.5Te3 Solution

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RUSSIAN PHYSICS JOURNAL 2019年第4期62卷 664-672页

作者： Barkhalov, B. Sh Tagiyev, M. M. Bagiyeva, G. Z. Abdinova, G. D. Aliyev, R. Yu Magerramova, K., I Natl Acad Sci Azerbaijan Inst Phys Baku Azerbaijan Azerbaijan State Econ Univ Baku Azerbaijan

Electrical and thermal properties of single crystalline and extruded samples of a p-type Bi0.5Sb1.5Te3 solid solution with various grain sizes are studied in a wide temperature range of 80-300 K. It is revealed that the grain sizes significantly affect the values of the thermal-e. m. f. (alpha), electrical conductivity (sigma), and thermal conductivity (chi) coefficients of the samples under study.

关键词： single crystal extrusion grain electrical conductivity thermal-e m f thermal conductivity electrons phonons grain boundaries

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Regulation of terpenoid biosynthesis by miRNA in Persicaria minor induced by fusarium oxysporum

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BMC GENOMICS 2019年第1期20卷 1-22页

作者： Samad, Abdul fatah A. Rahnamaie-Tajadod, Reyhaneh Sajad, Muhammad Jani, Jaeyres Murad, Abdul Munir Abdul Noor, Normah Mohd Ismail, Ismanizan UKM Fac Sci & Technol Sch Biosci & Biotechnol Bangi 43600 Selangor Malaysia UKM Inst Syst Biol Bangi 43600 Selangor Malaysia Univ Malaysia Sabah Fac Med & Hlth Sci Borneo Med & Hlth Res Ctr Kota Kinabalu Malaysia Islamia Univ Bahawalpur Univ Coll Agr & Environm Sci Dept Plant Breeding & Genet Punjab Pakistan Univ Teknol Malaysia Fac Sci Dept Biosci Skudai 81310 Johor Malaysia

BackgroundPersicaria minor (kesum) is an herbaceous plant with a high level of secondary metabolite compounds, particularly terpenoids. These terpenoid compounds have well-established roles in the pharmaceutical and food industries. Although the terpenoids of P. minor have been studied thoroughly, the involvement of microRNA (miRNA) in terpenoid regulation remains poorly understood and needs to be explored. In this study, P. minor plants were inoculated with the pathogenic fungus fusarium oxysporum for terpenoid *** GC-MS analysis showed the highest terpenoid accumulation on the 6th day post-inoculation (dpi) compared to the other treatment time points (0 dpi, 3 dpi, and 9 dpi). Among the increased terpenoid compounds, alpha-cedrene, valencene and beta-bisabolene were prominent. P. minor inoculated for 6days was selected for miRNA library construction using next generation sequencing. Differential gene expression analysis showed that 58 miRNAs belonging to 30 families had significantly altered regulation. Among these 58 differentially expressed genes (DEGs), 33 miRNAs were upregulated, whereas 25 miRNAs were downregulated. Two putative novel pre-miRNAs were identified and validated through reverse transcriptase PCR. Prediction of target transcripts potentially involved in the mevalonate pathway (MVA) was carried out by psRobot software, resulting in four miRNAs: pmi-miR530, pmi-miR6173, pmi-miR6300 and a novel miRNA, pmi-Nov_13. In addition, two miRNAs, miR396a and miR398f/g, were predicted to have their target transcripts in the non-mevalonate pathway (MEP). In addition, a novel miRNA, pmi-Nov_12, was identified to have a target gene involved in green leaf volatile (GLV) biosynthesis. RT-qPCR analysis showed that pmi-miR6173, pmi-miR6300 and pmi-nov_13 were downregulated, while miR396a and miR398f/g were upregulated. Pmi-miR530 showed upregulation at 9 dpi, and dynamic expression was observed for pmi-nov_12. Pmi-6300 and pmi-miR396a cleavage sites

关键词： Terpenoid biosynthesis miRNA P minor f Oxysporum Deep sequencing Post-transcriptional regulation

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Performance evaluation of surface texturing on carbide tool under minimum quantity lubrication turning of aluminium alloy Al6061 using canola oil

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Materials Today: Proceedings 2023年

作者： Narinder Singh Gyanendra Goindi Mechanical Engineering Department Chandigarh University Mohali Punjab India

Turning operation is considered an important material removal process and its performance depends largely on the machining parameters. This study presents the analysis of the effect of surface texturing on tool during MQL turning of Aluminium alloy Al6061 using canola oil. Minimum quantity lubrication possesses the benefits of flood lubrication as well as dry machining. Canola oil used in this study possesses good lubrication properties and its kinematic viscosity is 41 mm 2 /s at 40 °C. Tool texturing is in growing trend in the manufacturing industry and it has gained the attention of many researchers in the past few years. In this study parallel textured pattern is used in which the grooves are perpendicular to chip flow direction. Average surface roughness (R a) and tangential cutting forces (f t ) are the responses measured. Chip patterns are also examined under different conditions. It is concluded that high spindle speed of 160 m/min along with low feeding rate of 0.2 mm/rev with MQL system using textured tool generates better results for tangential cutting force as well as average surface roughness in contrast with other machining conditions.

关键词： MQL Textured tool Canola oil Average surface roughness Tangential cutting force MQL Minimum quantity lubrication R a Average surface roughness f.R feed rate f t Tangential cutting force

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Experimental characterization of unidirectional carbon – Carbon composite laminate

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Materials Today: Proceedings 2023年

作者： Mohd Mohinoddin S. Irfan Sadaq Syeda Romana V. Suvarna Kumar Mechanical Engineering Department Muffakham Jah College of Engineering & Technology Hyderabad Telangana 500034 India

Advanced polymeric Composites have wide applications in various industrial sectors of Missile System, Automobile, and Space Structures have been sound prominent and endlessly receiving the wide awareness for many industries. The structural engineer desires to be eminent with the belongings of the composite material structures. The performance of fiber reinforced polymeric composite material beneath dynamic load plays a crucial task in designing such structures. In the recent work, an attempt is made to determine optimum fiber angle and the behavior of the advanced polymeric composite material, i.e., Carbon – Carbon Composites under Tensile and Compressive loads. Mechanical properties, viz., Compressive and Tensile strength are determined by using experimentation method. Hand layup technique is used for fabricating the laminates. fE Analysis (Ansys) is carried out on various fiber angles likely be [0°-90°], [30°], [45°], [60°] to validate the results which is obtained from experimentation.

关键词： Compressive Strength Tensile Strength Carbon - Carbon Composite Volume fraction (V f ) fE Analysis

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Precision frequency Measurement of ^(87)Rb 5S_(1/2)(f=2)→5D_(5/2)(f″=4)Two-Photon Transition through a fiber-Based Optical frequency Comb

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Chinese Physics Letters 2016年第5期33卷 30-34页

作者：夏巍戴少阳张胤李坤乾于齐陈徐宗 Institute of Quantum Electronics School of Electronics Engineering and Computer SciencesPeking University Jiangsu Key Laboratory on Opto-electronic Technology School of Physics and TechnologyNanjing Normal University

The absolute frequency of 87Rb 5S1/2 （f=2）→5D5/2 （f＂ = 4） two-photon transition at 778nm is measured in an accuracy of 44kHz. A home-made erbium-doped fiber laser frequency comb with frequency stability of 5.0 × 10-13@1 s is employed for the light source. By using a periodically poled lithium niobate, the femtosecond pulse operating in 1556 nm is frequency-doubled to 778 nm to obtain the direct two-photon transition spectroscopy of thermal rubidium vapor. Through sweeping the carrier envelope offset frequency （fceo）, the 5S1/2 （f=2）→5D5/2 （f＂ = 4） two-photon transition line is clearly resolved and its absolute frequency is determined via the peak-finding of the fitting curve. After the frequency correction, the measured result agrees well with the previous experiment on this transition. The entire potential candidate of optical frequency standard for system configuration is compact and robust, providing a telecommunication applications.

关键词： Precision frequency Measurement of in is f=2 on as been Rb 5S f Two-Photon Transition through a fiber-Based Optical frequency Comb

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The Mechanism for Mimicry: Instant Biosemiotic Selection or Gradual Darwinian fine-Tuning Selection?

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BIOSEMIOTICS 2019年第1期12卷 39-55页

作者： Alexander, V. N. Dactyl Fdn 64 Grand St New York NY 10013 USA US Dept State Fulbright Specialist Program Bur Educ & Cultural Affairs Washington DC 20520 USA

Biological mimicry is regarded by many as a textbook illustration of Darwin's idea of evolution by random mutation followed by differential selection of reproductively fit specimens, resulting in gradual phenotypic change in a population. In this paper, I argue that some cases of so-called mimicry are probably merely look-a-likes and do not gain an advantage due to their similarity in appearance to something else. In cases where a similar appearance does provide a benefit, I argue that it is possible that these forms of mimicry were created in a single generation. An interpretive response to an appearance as a sign can make a new structure perform drastically differently in an environment. In such cases, Darwin's natural selection mechanism only helps to explain gradual the spread of these new forms, not the creation of them. I argue that biosemiosis should be regarded as a much more powerful mechanism for affecting evolutionary trajectories than the gradualist view allows. I focus on two cases of butterfly mimicry: the Viceroy (Nymphalidae: Limenitis archippus) and Monarch (Nymphalidae: Danaus plexippus) butterflies, supposed Mullerian mimics, and deadleaf mimic butterflies (Kallima).

关键词： Saltationism Turing patterns Mimicry Pattern formation Genus Kallima Mimicry skepticism H f Nijhout

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Identification of the bHLH gene family in Dracaena cambodiana reveals candidate genes involved in flavonoid biosynthesis

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INDUSTRIAL CROPS AND PRODUCTS 2020年 150卷

作者： Zhu, Jia-Hong Xia, Dong-Nan Xu, Jing Guo, Dong Li, Hui-Liang Wang, Ying Mei, Wen-Li Peng, Shi-Qing Chinese Acad Trop Agr Sci Inst Trop Biosci & Biotechnol Key Lab Biol & Genet Resources Trop Crops Minist Agr 4 Xueyuan Rd Haikou 571101 Hainan Peoples R China CATAS Hainan Acad Trop Agr Resource Haikou 571101 Hainan Peoples R China Hainan Acad Agr Sci Inst Cereal Crops Key Lab Crop Genet & Breeding Hainan Prov Haikou Hainan Peoples R China

The basic helix-loop-helix (bHLH) transcription factors (Tfs) regulate multiple biological processes by altering the expression of target genes. However, the bHLH superfamily genes in the dragon tree (Dracaena cambodiana Pierre ex Gagnep) have not been characterized, and their role in flavonoid biosynthesis remain unclear. Here, 62 bHLH genes in D. cambodiana were identified, and these genes were classified into 19 subfamilies based on a phylogenetic comparison with proteins from Arabidopsis. Transcriptomic analysis revealed that 8 DcbHLHs were up-regulated when exposed to the inducer of dragon's blood and ultraviolet radiation b (UVB). Interaction network analysis revealed that 3 bHLHs (DcbHLH2, DcbHLH5 and DcbHLH56) are likely involved in flavonoid biosynthesis. In addition, DcbHLH5 and flavonoids biosynthetic genes were co-expressed in response to the inducer and UVB exposure. furthermore, DcbHLH5 could bind to the promoters of flavonoid biosynthesis genes and activate their expression. This study suggests that DcbHLH proteins maybe involved in flavonoid biosynthesis.

关键词： Dracaena cambodiana bHLH transcription factor D ragon's blood f lavonoid biosynthesis

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Data on ADME parameters of bisphenol A and its metabolites for use in physiologically based pharmacokinetic modelling

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DATA IN BRIEf 2023年 48卷 109101页

作者： Wisniowska, Barbara Linke, Susanne Polak, Sebastian Bielecka, Zofia Luch, Andreas Pirow, Ralph Jagiellonian Univ Fac Pharm Med Coll Med 9 St PL-30688 Krakow Poland German Fed Inst Risk Assessment BfR Dept Chem & Prod Safety Max Dohrn Str 8-10 D-10589 Berlin Germany Free Univ Berlin Inst Pharm Dept Biol Chem Pharm Berlin Germany Certara UK Ltd Simcyp Div Level 2 Acero1 Concourse Way Sheffield S1 2BJ England

Abbreviations: ADAM, advanced dissolution, absorption and metabolism;ADME, absorption, distribution, metabolism, excretion;AUC, area under the concentration-time curve;B/P ratio, blood-to-plasma concentration ratio;BPA, bisphenol A;BPAG, glucuronidated BPA;BPAS, sulfated BPA;BW, body weight;CES, carboxylesterase;Cmax, maximum concentra-tion in plasma;CLint, in vitro intrinsic clearance;CLiv , total intravenous clearance;CLperm, permeability clearance;CLrenal, renal clearance;CLint,bile, in vitro intrinsic biliary clearance;CLuint,G, net intrinsic metabolic clearance in the gut based on unbound BPA concentration;CL int,gutlumen, gut lumen intrinsic clearance;EHR, enterohepatic recirculation;fa, fraction absorbed;fugut, fraction of BPA unbound in the enterocyte;fuinc, fraction unbound in in vitro incubation;fumic, frac-tion unbound in microsomal incubation;fup, fraction unbound in plasma;fg, fraction of BPA escaping gut metabolism;HBD, number of hydrogen bond donors;HPGL, hepatocytes per gram of liver;IV, intravenous;IVIVE, in vitro to in vivo extrapolation;ka, absorption rate constant;Ka, acid dissociation constant;Km, Michaelis-Menten constant;Kp, tissue -to-plasma partition coefficient;MechPeff, mechanistic permeability;MPPGL, microsomal protein per gram of liver;MW, molecular weight;Qgut, hybrid parameter of blood flow and compound permeability through enterocytes;QSAR, quanti-tative structure-activity relationship;P , octanol:water partition coefficient;Papp, apparent permeability;Peff,man, effective intestinal permeability in human;PBPK, physiologically based pharmacokinetics;PSA, polar surface area;RAf, relative activity factor;rhUGT, recombinant human UGT;SULT, sulfotransferase;UGT, UDP-glucuronosyltransferase;Vmax, maxi-mum velocity;Vss, volume of distribution at steady-state.

关键词： BPA Bisphenol A PBPK ADME Modelling Oral route ADAM advanced dissolution, absorption and metabolism ADME absorption, distribution, metabolism, excretion AUC area under the concentration-time curve B/P ratio blood-to-plasma concentration ratio BPA bisphenol A BPAG glucuronidated BPA BPAS sulfated BPA BW body weight CES carboxylesterase C max maximum concentration in plasma CL int in vitro intrinsic clearance CL iv total intravenous clearance CL perm permeability clearance CL renal renal clearance CL int,bile in vitro intrinsic biliary clearance CLu int,G net intrinsic metabolic clearance in the gut based on unbound BPA concentration CL int,gutlumen gut lumen intrinsic clearance EHR enterohepatic recirculation f a fraction absorbed fu gut fraction of BPA unbound in the enterocyte fu inc fraction unbound in in vitro incubation fu mic fraction unbound in microsomal incubation fu p fraction unbound in plasma f g fraction of BPA escaping gut metabolism HBD number of hydrogen bond donors HPGL hepatocytes per gram of liver IV intravenous IVIVE in vitro to in vivo extrapolation k a absorption rate constant K a acid dissociation constant K m Michaelis-Menten constant K p tissue-to-plasma partition coefficient MechPeff mechanistic permeability MPPGL microsomal protein per gram of liver MW molecular weight Q gut hybrid parameter of blood flow and compound permeability through enterocytes QSAR quantitative structure-activity relationship P octanol:water partition coefficient P app apparent permeability P eff,man effective intestinal permeability in human PBPK physiologically based pharmacokinetics PSA polar surface area RAf relative activity factor rhUGT recombinant human UGT SULT sulfotransferase UGT UDP-glucuronosyltransferase V max maximum velocity V ss volume of distribution at steady-state

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