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https://www.readbyqxmd.com/read/28425681/schedules-of-controlled-substances-temporary-placement-of-six-synthetic-cannabinoids-5f-adb-5f-amb-5f-apinaca-adb-fubinaca-mdmb-chmica-and-mdmb-fubinaca-into-schedule-i-temporary-scheduling-order
#1
(no author information available yet)
The Administrator of the Drug Enforcement Administration is issuing this temporary scheduling order to schedule six synthetic cannabinoids: methyl 2-(1-(5-fluoropentyl)-1H-indazole-3-carboxamido)-3,3-dimethylbutanoate [5F-ADB; 5F-MDMB-PINACA]; methyl 2-(1-(5-fluoropentyl)-1H-indazole-3-carboxamido)-3-methylbutanoate [5F-AMB]; N-(adamantan-1-yl)-1-(5-fluoropentyl)-1H-indazole-3-carboxamide [5F-APINACA, 5F-AKB48]; N-(1-amino-3,3-dimethyl-1-oxobutan-2-yl)-1-(4-fluorobenzyl)-1H-indazole-3-carboxamide [ADB-FUBINACA]; methyl 2-(1-(cyclohexylmethyl)-1H-indole-3-carboxamido)-3,3-dimethylbutanoate [MDMB-CHMICA, MMB-CHMINACA] and methyl 2-(1-(4-fluorobenzyl)-1H-indazole-3-carboxamido)-3,3-dimethylbutanoate [MDMB-FUBINACA], and their optical, positional, and geometric isomers, salts, and salts of isomers into schedule I pursuant to the temporary scheduling provisions of the Controlled Substances Act...
April 10, 2017: Federal Register
https://www.readbyqxmd.com/read/28425177/design-and-synthesis-of-c3-substituted-%C3%AE-carboline-based-histone-deacetylase-inhibitors-with-potent-antitumor-activities
#2
Yong Ling, Jiao Feng, Lin Luo, Jing Guo, Yanfu Peng, Tingting Wang, Xiang Ge, Qibing Xu, Xinyang Wang, Hong Dai, Yanan Zhang
A series of hydroxamic acid histone deacetylase (HDAC) inhibitors in which the β-carboline motif has been incorporated were designed and synthesized. The effect of substitution at the C3 amide on HDAC inhibition and antiproliferative activities was investigated. Most of these compounds were found to display significant HDAC inhibitory effects and good antiproliferative activity, with IC50 values in the low-micromolar range. In particular, the HDAC inhibition IC50 value of N-(2-(dimethylamino)ethyl)-N-(4-(hydroxylcarbamoyl)benzyl)-1-(4-methoxyphenyl)-9H-pyrido[3,4-b]indole-3-carboxamide (9 h) is five-fold lower than that of suberoylanilide hydroxamic acid (SAHA, vorinostat)...
April 20, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28424944/indirect-interactions-between-arbuscular-mycorrhizal-fungi-and-spodoptera-exigua-alter-photosynthesis-and-plant-endogenous-hormones
#3
Lei He, Changyou Li, Runjin Liu
Peanut (Arachis hypogaea Linn. cv: Luhua 11) and tomato (Lycopersicon esculentum Mill. cv: Zhongshu 4) were inoculated with arbuscular mycorrhizal fungi (AMF) Funneliformis mosseae BEG167 (Fm), Rhizophagus intraradices BEG141 (Ri), and Glomus versiforme Berch (Gv), and/or Spodoptera exigua (S. exigua) under greenhouse conditions. Results indicated that feeding by S. exigua had little influence on colonization of peanut plants by AMF, but improved colonization of tomato by Fm and Gv. Feeding by S. exigua had little influence on leaf net photosynthetic rate, transpiration rate, and stomatal conductance of nonmycorrhizal peanut plants but significantly improved net photosynthetic rate and transpiration rate of mycorrhizal plants of both hosts...
April 20, 2017: Mycorrhiza
https://www.readbyqxmd.com/read/28424722/the-role-of-auxin-ethylene-crosstalk-in-orchestrating-primary-root-elongation-in-sugar-beet
#4
Willem Abts, Bert Vandenbussche, Maurice P De Proft, Bram Van de Poel
It is well-established in Arabidopsis and other species that ethylene inhibits root elongation through the action of auxin. In sugar beet (Beta vulgaris L.) ethylene promotes root elongation in a concentration dependent manner. However, the crosstalk between ethylene and auxin remains unknown during sugar beet seedling development. Our experiments have shown that exogenously applied auxin (indole-3-acetic acid; IAA) also stimulates root elongation. We also show that auxin promotes ethylene biosynthesis leading to longer roots...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/28418923/osu-a9-inhibits-pancreatic-cancer-cell-lines-by-modulating-p38-jak-stat3-signaling
#5
Wan-Chi Tsai, Li-Yuan Bai, Yi-Jin Chen, Po-Chen Chu, Ya-Wen Hsu, Aaron M Sargeant, Jing-Ru Weng
Pancreatic cancer is an aggressive malignancy that is the fourth leading cause of death worldwide. Since there is a dire need for novel and effective therapies to improve the poor survival rates of advanced pancreatic cancer patients, we analyzed the antitumor effects of OSU-A9, an indole-3-carbinol derivative, on pancreatic cancer cell lines in vitro and in vivo. OSU-A9 exhibited a stronger antitumor effect than gemcitabine on two pancreatic cancer cell lines, including gemcitabine-resistant PANC-1 cells. OSU-A9 treatment induced apoptosis, the down-regulation of Akt phosphorylation, up-regulation of p38 phosphorylation and decreased phosphorylation of JAK and STAT3...
March 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/28417922/indole-derivatives-isolated-from-brown-alga-sargassum-thunbergii-inhibit-adipogenesis-through-ampk-activation-in-3t3-l1-preadipocytes
#6
Min-Cheol Kang, Yuling Ding, Eun-A Kim, Youn Kyung Choi, Thiago de Araujo, Soo-Jin Heo, Seung-Hong Lee
Seaweed, a popular and abundant food ingredient mainly consumed in Asian countries, is a good source of bioactive compounds with anti-obesity effects. However, the anti-obesity effects of Sargassum thunbergii have not yet been established. In this study, we isolated six indole derivatives (STCs)-indole-2-carboxaldehyde (STC-1), indole-3-carboxaldehyde (STC-2), indole-4-carboxaldehyde (STC-3), indole-5-carboxaldehyde (STC-4), indole-6-carboxaldehyde (STC-5), and indole-7-carboxaldehyde (STC-6)-from S. thunbergii and evaluated their inhibitory effects on adipocyte differentiation in 3T3-L1 cells...
April 12, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28414098/cytosolic-calcium-mediates-rip1-rip3-complex-dependent-necroptosis-through-jnk-activation-and-mitochondrial-ros-production-in-human-colon-cancer-cells
#7
Wen Sun, Xiaxia Wu, Hongwei Gao, Jie Yu, Wenwen Zhao, Jin-Jian Lu, Jinhua Wang, Guanhua Du, Xiuping Chen
Necroptosis is a form of programmed necrosis mediated by signaling complexes with receptor-interacting protein 1 (RIP1) and RIP3 kinases as the main mediators. However, the underlying execution pathways of this phenomenon have yet to be elucidated in detail. In this study, a RIP1/RIP3 complex was formed in 2-methoxy-6-acetyl-7-methyljuglone (MAM)-treated HCT116 and HT29 colon cancer cells. With this formation, mitochondrial reactive oxygen species (ROS) levels increased, mitochondrial depolarization occurred, and ATP concentrations decreased...
April 14, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28412508/methyl-5-1h-indol-3-yl-selanyl-1h-benzoimidazol-2-ylcarbamate-m-24-a-novel-tubulin-inhibitor-causes-g2-m-arrest-and-cell-apoptosis-by-disrupting-tubulin-polymerization-in-human-cervical-and-breast-cancer-cells
#8
Daiying Zuo, Xuewei Jiang, Mengting Han, Jiwei Shen, Binyue Lang, Qi Guan, Zhaoshi Bai, Chunming Han, Zengqiang Li, Weige Zhang, Yingliang Wu
Methyl 5-[(1H-indol-3-yl)selanyl]-1H-benzoimidazol-2-ylcarbamate (M-24) is a newly synthesized analogue of nocodazole by our group and has been found to be active for some cancer cells. However, its sensitivity to different cell lines and the underlying anticancer mechanism are still unclear. In this study, we proved that M-24 had strong time- and dose-dependent anti-proliferative effects on human cervical cancer HeLa cells and human breast carcinoma MCF-7 cells. We demonstrated that the growth inhibitory effects of M-24 in both cell lines were associated with microtubule depolymerization...
April 13, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28411052/selective-enrichment-of-eicosapentaenoic-acid-20-5n-3-in-n-oceanica-casa-cc201-by-natural-auxin-supplementation
#9
Aswathy Udayan, Muthu Arumugam
The present study aims to evaluate the effect of different concentration of natural auxin, Indole-3 acetic acid (IAA) on growth, lipid yield, PUFA and EPA accumulation in Nannochloropsis oceanica CASA CC201. It was observed that the, treatment with 10ppm concentration of IAA resulted in high cell number 579.5×10(6)cells/ml than the control (215.5×10(6)cells/ml). Treatment with IAA at a concentration of 40ppm gives the highest cellular lipid accumulation of 60.9% DCW than the control 31.05% DCW). Lipid yield is also found to be increased by the addition of 40ppm IAA (319...
March 27, 2017: Bioresource Technology
https://www.readbyqxmd.com/read/28406627/diindolylmethane-derivatives-potent-agonists-of-the-immunostimulatory-orphan-g-protein-coupled-receptor-gpr84
#10
Thanigaimalai Pillaiyar, Meryem Köse, Katharina Sylvester, Heike Weighardt, Dominik Thimm, Gleice Borges, Irmgard Förster, Ivar von Kügelgen, Christa E Müller
The Gi protein-coupled receptor GPR84, which is activated by (hydroxy)fatty acids, is highly expressed on immune cells. Recently 3,3'-diindolylmethane was identified as a heterocyclic, non-lipid-like GPR84 agonist. We synthesized a broad range of diindolylmethane derivatives by condensation of indoles with formaldehyde in water under microwave irradiation. The products were evaluated at the human GPR84 in cAMP and β-arrestin assays. Structure-activity relationships (SARs) were steep. 3,3'-Diindolylmethanes bearing small lipophilic residues at the 5- and/or 7-position of the indole rings displayed the highest activity in cAMP assays, the most potent agonists being di-(5-fluoro-1H-indole-3-yl)methane (38, PSB-15160, EC50 80...
April 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28406060/auxin-signaling-through-scf-tir1-afbs-mediates-feedback-regulation-of-iaa-biosynthesis
#11
Shin Takato, Yusuke Kakei, Marie Mitsui, Yosuke Ishida, Masashi Suzuki, Chiaki Yamazaki, Ken-Ichiro Hayashi, Takahiro Ishii, Ayako Nakamura, Kazuo Soeno, Yukihisa Shimada
We previously reported that exogenous application of auxin to Arabidopsis seedlings resulted in downregulation of indole-3-acetic acid (IAA) biosynthesis genes in a feedback manner. In this study, we investigated the involvement of the SCF(TIR1/AFB)-mediated signaling pathway in feedback regulation of the indole-3-pyruvic acid-mediated auxin biosynthesis pathway in Arabidopsis. Application of PEO-IAA, an inhibitor of the IAA signal transduction pathway, to wild-type seedlings resulted in increased endogenous IAA levels in roots...
April 13, 2017: Bioscience, Biotechnology, and Biochemistry
https://www.readbyqxmd.com/read/28405774/bacillus-methylotrophicus-m4-96-isolated-from-maize-zea-mays-rhizoplane-increases-growth-and-auxin-content-in-arabidopsis-thaliana-via-emission-of-volatiles
#12
Paola Pérez-Flores, Eduardo Valencia-Cantero, Josué Altamirano-Hernández, Ramón Pelagio-Flores, José López-Bucio, Perla García-Juárez, Lourdes Macías-Rodríguez
Plant growth-promoting rhizobacteria stimulate plant growth and development via different mechanisms. In this study, we characterized the effect of volatiles from Bacillus methylotrophicus M4-96 isolated from the maize rhizosphere on root and shoot development, and auxin homeostasis in Arabidopsis thaliana. Phytostimulation occurred after 4 days of interaction between M4-96 and Arabidopsis grown on opposite sides of divided Petri plates, as revealed by enhanced primary root growth, root branching, leaf formation, and shoot biomass accumulation...
April 12, 2017: Protoplasma
https://www.readbyqxmd.com/read/28401461/continuous-production-of-indole-3-acetic-acid-by-immobilized-cells-of-arthrobacter-agilis
#13
Murat Ozdal, Ozlem Gur Ozdal, Alev Sezen, Omer Faruk Algur, Esabi Basaran Kurbanoglu
Indole acetic acid (IAA) is a plant growth-promoting hormone used in agriculture; therefore, its continuous production is of paramount importance. IAA-producing eight bacteria were isolated from the rhizosphere of Verbascum vulcanicum. Among them, Arthrobacter agilis A17 gave maximum IAA production (75 mg/L) and this strain was used to immobilization studies. The A. agilis A17 cells were immobilized in calcium alginate for the production of IAA. Optimization of process parameters for IAA production was carried out to enhance IAA production using immobilized cells...
May 2017: 3 Biotech
https://www.readbyqxmd.com/read/28397062/multi-metal-resistance-and-plant-growth-promotion-potential-of-a-wastewater-bacterium-pseudomonas-aeruginosa-and-its-synergistic-benefits
#14
Jayanta Kumar Biswas, Monojit Mondal, Jörg Rinklebe, Santosh Kumar Sarkar, Punarbasu Chaudhuri, Mahendra Rai, Sabry M Shaheen, Hocheol Song, Muhammad Rizwan
Water and soil pollution by toxic heavy metals (HMs) is increasing globally because of increase in population, industrialization and urbanization. It is a burning problem for the public, scientists, academicians and politicians how to tackle the toxic contaminants which jeopardize the environment. One possible solution for pollution abatement is a bioremediation-effective and innovative technology that uses biological systems for treatment of contaminants. Many bacteria synthesize indole-3-acetic acid (IAA) which is a product of L-tryptophan metabolism and belongs to the auxin class of plant growth-promoting hormone...
April 10, 2017: Environmental Geochemistry and Health
https://www.readbyqxmd.com/read/28396636/enhancing-drug-efficacy-and-therapeutic-index-through-cheminformatics-based-selection-of-small-molecule-binary-weapons-that-improve-transporter-mediated-targeting-a-cytotoxicity-system-based-on-gemcitabine
#15
Justine M Grixti, Steve O'Hagan, Philip J Day, Douglas B Kell
The transport of drug molecules is mainly determined by the distribution of influx and efflux transporters for which they are substrates. To enable tissue targeting, we sought to develop the idea that we might affect the transporter-mediated disposition of small-molecule drugs via the addition of a second small molecule that of itself had no inhibitory pharmacological effect but that influenced the expression of transporters for the primary drug. We refer to this as a "binary weapon" strategy. The experimental system tested the ability of a molecule that on its own had no cytotoxic effect to increase the toxicity of the nucleoside analog gemcitabine to Panc1 pancreatic cancer cells...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28395284/indole-3-carbinol-induces-apoptosis-of-hepatic-stellate-cells-through-k63-de-ubiquitination-of-rip1-in-rats
#16
Bin Li, Meng Cong, Yanan Zhu, Ying Xiong, Wenyi Jin, Yang Wan, Yunjiao Zhou, Ying Ao, Hui Wang
BACKGROUND/AIMS: The apoptosis of activated hepatic stellate cells (HSCs) is the central event in the reversal of liver fibrosis. K63 de-ubiquitinated receptor-interacting protein (RIP)1 promotes apoptosis in tumor necrosis factor (TNF)-α signaling pathway. In the previous study, we have proved that indole-3-carbinol (I3C) could reverse different models of liver fibrosis in rats, but the mechanism is still unclear. Thus, the present research aimed to demonstrate the induction of I3C on apoptosis of HSCs and the underlying molecular mechanism...
March 24, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28388893/genome-wide-identification-and-expression-analysis-of-cllax-clpin-and-clabcb-genes-families-in-citrullus-lanatus-under-various-abiotic-stresses-and-grafting
#17
Chenliang Yu, Wenqi Dong, Yihua Zhan, Zong-An Huang, Zhimiao Li, Il Seop Kim, Chenghao Zhang
BACKGROUND: Auxin plays an important role in regulating plant growth and development as well as in the response of plants to abiotic stresses. Auxin is transported by three kinds of major protein families, including the AUXIN RESISTANT 1/LIKE AUX1 (AUX⁄LAX) influx carriers, the PIN-FORMED (PIN) efflux carriers and the ATP binding cassette B/P-glycoprotein/Multidrug-resistance (ABCB/MDR/PGP) efflux/condition carriers. The biological function of several auxin transporter genes has been well characterized in Arabidopsis thaliana...
April 7, 2017: BMC Genetics
https://www.readbyqxmd.com/read/28382865/multitargeted-molecular-docking-study-of-natural-derived-alkaloids-on-breast-cancer-pathway-components
#18
Ramit Singla, Vikas Jaitak
BACKGROUND: Targeting of multiple sites is a pharmacologically, pharmacokinetic and dynamically more acceptable approach for complex diseases such as BC. It is recommended that the women who are at high risk of developing BC might be given foods enhanced by indole alkaloids from vegetables like cabbage and broccoli. Administration of indole-3-carbinol is associated with decreased incidence of hormone-responsive BC (HRBC) which is implicated due to the induction of cytochrome P450 and glutathione-S-transferase which metabolizes chemical mutagens and by altering estrogen metabolism...
April 6, 2017: Current Computer-aided Drug Design
https://www.readbyqxmd.com/read/28371691/changes-in-aba-iaa-and-ja-levels-during-calyx-fruit-and-leaves-development-in-cape-gooseberry-plants-physalis-peruviana-l
#19
F Álvarez-Flórez, C López-Cristoffanini, O Jáuregui, L M Melgarejo, M López-Carbonell
Changes in abscisic acid (ABA), indole-3-acetic acid (IAA) and jasmonic acid (JA) content in developing calyx, fruits and leaves of Physalis peruviana L. plants were analysed. Plant hormones have been widely studied for their roles in the regulation of various aspects related to plant development and, in particular, into their action during development and ripening of fleshly fruits. The obtained evidences suggest that the functions of these hormones are no restricted to a particular development stage, and more than one hormone is involved in controlling various aspects of plant development...
March 30, 2017: Plant Physiology and Biochemistry: PPB
https://www.readbyqxmd.com/read/28371476/detection-of-the-recently-emerged-synthetic-cannabinoid-5%C3%A2-f-mdmb-pica-in-legal-high-products-and-human-urine-samples
#20
Lukas Mogler, Florian Franz, Daniel Rentsch, Verena Angerer, Georg Weinfurtner, Mitchell Longworth, Samuel D Banister, Michael Kassiou, Bjoern Moosmann, Volker Auwärter
Indole or indazole based synthetic cannabinoids (SCs) bearing substituents derived from valine or tert-leucine are frequently abused new psychoactive substances (NPS). The emergence of 5 F-MDMB-PICA (methyl N-{[1-(5-fluoropentyl)-1H-indol-3-yl]carbonyl}-3-methylvalinate) on the German drug market is a further example of a substance synthesized in the context of scientific research being misused by clandestine laboratories by adding it to 'legal high' products. In this work we present the detection of 5 F-MDMB-PICA in several 'legal high' products by GC-MS analysis...
March 31, 2017: Drug Testing and Analysis
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