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https://www.readbyqxmd.com/read/29350472/the-chemistry-and-pharmacology-of-synthetic-cannabinoid-sdb-006-and-its-regioisomeric-fluorinated-and-methoxylated-analogues
#1
Samuel D Banister, Alexander Olson, Matthew Winchester, Jordyn Stuart, Amelia R Edington, Richard C Kevin, Mitchell Longworth, Marco Herrera, Mark Connor, Iain S McGregor, Roy R Gerona, Michael Kassiou
Synthetic cannabinoids are the largest and most structurally diverse class of new psychoactive substances, with manufacturers often using isomerism to evade detection and circumvent legal restriction. The regioisomeric methoxy- and fluorine-substituted analogues of SDB-006 (N-benzyl-1-pentyl-1H-indole-3-carboxamide) were synthesized and could not be differentiated by gas chromatography-mass spectrometry (GC-MS), but were distinguishable by liquid chromatography-quadrupole time-of-flight-MS (LC-QTOF-MS). In a fluorescence-based plate reader membrane potential assay, SDB-006 acted as a potent agonist at human cannabinoid receptors (CB1 EC50 = 19 nM)...
January 19, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29345908/a-small-molecule-inhibitor-of-human-dna-polymerase-eta-potentiates-the-effects-of-cisplatin-in-tumor-cells
#2
Maroof K Zafar, Leena Maddukuri, Amit Ketkar, Narsimha Penthala, Megan R Reed, Sarah D Eddy, Peter A Crooks, Robert L Eoff
Translesion DNA synthesis (TLS) performed by human DNA polymerase eta (hpol η) allows tolerance of damage from cis-diamminedichloroplatinum(II) (CDDP or cisplatin). We have developed hpol η inhibitors derived from N-aryl-substituted indole barbituric acid (IBA), indole thiobarbituric acid (ITBA), and indole quinuclidine scaffolds and identified 5-((5-chloro-1-(naphthalen-2-ylmethyl)-1H-indol-3-yl)methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione (PNR-7-02), an ITBA derivative that inhibited hpol η activity with an IC50 value of 8 μM and exhibited five- to ten-fold specificity for hpol η over replicative pols...
January 18, 2018: Biochemistry
https://www.readbyqxmd.com/read/29341448/beneficial-actions-of-microbiota-derived-tryptophan-metabolites
#3
REVIEW
J J Galligan
Tryptophan is an important dietary amino acid and it is the precursor for 5-hydroxytryptamine synthesis in the nervous system and by enterochromaffin cells in the gut mucosa. Tryptophan is also metabolized by enzymes in the gut mucosa and also by enzymes produced by the gut microbiome. Diet and the microbiome can contribute to metabolic disease in part by causing intestinal inflammation and increased permeability. In this issue of Neurogastroenterology and Motility, Jennis et al. test the hypothesis that indole tryptophan metabolites produced by gut bacteria might be responsible for the anti-inflammatory and beneficial metabolic effects of the gut microbiome and Roux-en-Y gastric bypass surgery for weight loss by obese patients...
February 2018: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/29337875/aux-iaa-gene-family-in-plants-molecular-structure-regulation-and-function
#4
REVIEW
Jie Luo, Jing-Jing Zhou, Jin-Zhi Zhang
Auxin plays a crucial role in the diverse cellular and developmental responses of plants across their lifespan. Plants can quickly sense and respond to changes in auxin levels, and these responses involve several major classes of auxin-responsive genes, including the Auxin/Indole-3-Acetic Acid (Aux/IAA) family, the auxin response factor (ARF) family, small auxin upregulated RNA (SAUR), and the auxin-responsive Gretchen Hagen3 (GH3) family. Aux/IAA proteins are short-lived nuclear proteins comprising several highly conserved domains that are encoded by the auxin early response gene family...
January 16, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29333043/picroside-i-and-picroside-ii-from-tissue-cultures-of-picrorhiza-kurroa
#5
Yamjala Ganeshkumar, Ajmera Ramarao, Ciddi Veeresham
Background: Picrorhiza kurroa (PK) belongs to Scrophulariaceae family and is a representative endemic, medicinal herb, widely distributed throughout the higher altitudes of alpine Himalayas from west to east, between 3000 and 4500 m above mean sea level. Objective: The objective of the present study is to assess the production of picroside I and picroside II from tissue cultures of PK. Materials and Methods: Auxiliary shoot tips of PK were incubated in Murashige and Skoog medium supplemented with indole-3-butyric acid and kinetin phytohormones...
December 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/29331880/preventive-effects-of-indole-3-carbinol-against-alcohol-induced-liver-injury-in-mice-via-antioxidant-anti-inflammatory-and-anti-apoptotic-mechanisms-role-of-gut-liver-adipose-tissue-axis
#6
Youngshim Choi, Mohamed A Abdelmegeed, Byoung-Joon Song
Indole-3-carbinol (I3C), found in Brassica family vegetables, exhibits antioxidant, anti-inflammatory, and anti-cancerous properties. Here, we aimed to evaluate the preventive effects of I3C against ethanol (EtOH)-induced liver injury and study the protective mechanism(s) by using the well-established chronic-plus-binge alcohol exposure model. The preventive effects of I3C were evaluated by conducting various histological, biochemical, and real-time PCR analyses in mouse liver, adipose tissue, and colon, since functional alterations of adipose tissue and intestine can also participate in promoting EtOH-induced liver damage...
December 10, 2017: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/29330819/preparation-of-a-synthetic-seed-for-the-common-reed-harboring-an-endophytic-bacterium-promoting-seedling-growth-under-cadmium-stress
#7
Ting Gao, Xianyang Shi
Bacterial seed endophytes can facilitate germination and early plant development. Therefore, the introduction of seed-borne endophytes may improve selected plant characteristics across generations. In this study, regenerated plantlets of common reed (Phragmites australis) were inoculated with activated sludge to obtain a specific functional endophytic bacterium. Denaturing gradient gel electrophoresis demonstrated that abundant endophytic bacteria could be enriched in the roots. A siderophore-producing endophytic bacterium was isolated from the roots and identified as Herbaspirillum frisingense RE3-3 based on 16S rRNA sequences...
January 12, 2018: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/29327073/azospirillum-brasilense-increases-co2-fixation-on-microalgae-scenedesmus-obliquus-chlorella-vulgaris-and-chlamydomonas-reinhardtii-cultured-on-high-co2-concentrations
#8
Francisco J Choix, Cecilia Guadalupe López-Cisneros, Hugo Oscar Méndez-Acosta
Mutualism interactions of microalgae with other microorganisms are widely used in several biotechnological processes since symbiotic interaction improves biotechnological capabilities of the microorganisms involved. The interaction of the bacterium Azospirillum brasilense was assessed with three microalgae genus, Scenedesmus, Chlorella, and Chlamydomonas, during CO2 fixation under high CO2 concentrations. The results in this study have demonstrated that A. brasilense maintained a mutualistic interaction with the three microalgae assessed, supported by the metabolic exchange of indole-3-acetic acid (IAA) and tryptophan (Trp), respectively...
January 11, 2018: Microbial Ecology
https://www.readbyqxmd.com/read/29324661/protein-activity-of-the-fusarium-fujikuroi-rhodopsins-caro-and-opsa-and-their-relation-to-fungus-plant-interaction
#9
Alexander Adam, Stephan Deimel, Javier Pardo-Medina, Jorge García-Martínez, Tilen Konte, M Carmen Limón, Javier Avalos, Ulrich Terpitz
Fungi possess diverse photosensory proteins that allow them to perceive different light wavelengths and to adapt to changing light conditions in their environment. The biological and physiological roles of the green light-sensing rhodopsins in fungi are not yet resolved. The rice plant pathogen Fusarium fujikuroi exhibits two different rhodopsins, CarO and OpsA. CarO was previously characterized as a light-driven proton pump. We further analyzed the pumping behavior of CarO by patch-clamp experiments. Our data show that CarO pumping activity is strongly augmented in the presence of the plant hormone indole-3-acetic acid and in sodium acetate, in a dose-dependent manner under slightly acidic conditions...
January 11, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29316692/3-3-diindolylmethane-suppressed-cyprodinil-induced-epithelial-mesenchymal-transition-and-metastatic-related-behaviors-of-human-endometrial-ishikawa-cells-via-an-estrogen-receptor-dependent-pathway
#10
Bo-Gyoung Kim, Jin-Wook Kim, Soo-Min Kim, Ryeo-Eun Go, Kyung-A Hwang, Kyung-Chul Choi
Cyprodinil (CYP) is a pyrimidine amine fungicide that has been extensively used in agricultural areas. 3,3'-Diindolylmethane (DIM) is a derivative of the dietary phytoestrogen, indole-3-carbinol (I3C), which is derived from cruciferous vegetables and considered to be a cancer-preventive phytonutrient agent. In this study, the effects of CYP and DIM were examined on the cell viability, invasion, and metastasis of human endometrial cancer cells, Ishikawa, via epithelial mesenchymal transition (EMT). CYP increased the level of cell viability of Ishikawa cells compared to DMSO as a control, as did E2...
January 8, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29315590/brassinosteroids-regulate-glucosinolate-biosynthesis-in-arabidopsis-thaliana
#11
Ji Hyea Lee, Jeongyeo Lee, HyeRan Kim, Won Byoung Chae, Sun-Ju Kim, Yong Pyo Lim, Man-Ho Oh
Plants must constantly adjust their growth and defense responses to deal with the wide variety of stresses they encounter in their environment. Among phytohormones, brassinosteroids (BRs) are an important group of plant steroid hormones involved in numerous aspects of the plant lifecycle including growth, development, and responses to various stresses including insects. Here, we show that BRs regulate glucosinolate (GS) biosynthesis and function in insect herbivory. Preference tests and larval feeding experiments using the generalist herbivore, diamondback moth (Plutella xylostella), revealed that the larvae of this moth prefer to feed on Arabidopsis thaliana brassinosteroid insensitive 1 (bri1-5) plants than on wild-type Ws-2 or BRI1-Flag (bri1-5 background) transgenic plants, which leads an increase in larval weight...
January 5, 2018: Physiologia Plantarum
https://www.readbyqxmd.com/read/29291069/an-efficient-synthesis-of-4h-pyrano-quinolinone-derivatives-catalysed-by-a-versatile-organocatalyst-tetra-n-butylammonium-fluoride-and-their-pharmacological-screening
#12
Pratibha Prasad, Pratik G Shobhashana, Manish P Patel
A new series of indole-based pyranoquinoline derivatives P1-24 has been synthesized by a one-pot cyclocondensation reaction of 2-(4-substituted)phenyl-N-allyl-indole-3-carbaldehydes 1a-d; active methylenes 2a-c; and 4-hydroxy-1-substituted quinolin-2(1H)-one 3a-b catalysed by an organocatalyst tetra-n-butylammonium fluoride (TBAF) in aqueous ethanol. The easy experimental procedure of the reaction leads to excellent yields of pyranoquinoline derivatives. All the compounds were screened against a representative panel of bacteria and fungi...
November 2017: Royal Society Open Science
https://www.readbyqxmd.com/read/29288947/synthesis-and-biological-evaluation-of-novel-2-arylvinyl-substituted-naphtho-2-3-d-imidazolium-halide-derivatives-as-potent-antitumor-agents
#13
Qingyun Wei, Ju Li, Feng Tang, Yin Yin, Yong Zhao, Qizheng Yao
Two series of novel 2-arylvinyl-naphtho[2,3-d]imidazol-3-ium iodide derivatives and 2-arylvinyl-naphtho[2,3-d]imidazol-3-ium bromide derivatives were designed and synthesized by the structural combination of YM155 with stilbenoids. All compounds were tested for anti-proliferative activity against PC-3, A375 and HeLa human cancer cell lines. Two of the compounds were selected for further investigation: 12b, which showed potent cytotoxicity against the three tested cell lines with IC50 values in the range of 0...
December 6, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29288464/methods-for-the-characterization-of-plant-growth-promoting-rhizobacteria
#14
Md Motaher Hossain, Farjana Sultana
A detailed description of methods most frequently used for the identification and characterization of beneficial microbial strains is presented in this chapter. The methods include microbiological, biochemical, and molecular approaches. Microbiological and biochemical methods comprise a broad range of techniques that are based on the analysis of phosphate solubilization, nitrogenase activity, indole-3-acetic acid production, bacterial motility, presence of catalase and nitrate reductase enzyme, Gram's staining of the cell wall, siderophore production, and microbial chemotaxis...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/29288361/genome-sequence-and-comparative-analysis-of-jiangella-alba-yim-61503t-isolated-from-a-medicinal-plant-maytenus-austroyunnanensis
#15
Jian-Yu Jiao, Nimaichand Salam, Lan Liu, Manik Prabhu Narsing Rao, Xiao-Tong Zhang, Bao-Zhu Fang, Ming-Xian Han, Zi-Tong Zhang, Jing Chen, Jiao Zhao, Yu Zhou, Dalal Hussien M Alkhalifah, Qing Liu, Min Xiao, Hans-Peter Klenk, Wen-Jun Li
A draft genome sequence of Jiangella alba YIM 61503T revealed a genome size of 7,664,864 bp arranged in 33 scaffolds. The genome was predicted to contain 7196 predicted genes, including 51 coding for RNA. Phylogenetic and comparative analyses of the draft genome of J. alba YIM 61503T with the available genomes of other Jiangella species suggested a proximal similarity between strains J. alba YIM 61503T and J. muralis DSM 45357T, while indicating a high divergence between J. gansuensis YIM 002T and other Jiangella species...
December 29, 2017: Antonie Van Leeuwenhoek
https://www.readbyqxmd.com/read/29288233/the-shsp22-heat-shock-protein-requires-the-abi1-protein-phosphatase-to-modulate-polar-auxin-transport-and-downstream-responses
#16
Yan Li Li, Yaqiong Li, Yao Rong Wu, Yongchang Liu, Qi Xie
The phytohormones abscisic acid (ABA) and indole-3-acetic acid (IAA) response pathways interact synergistically or antagonistically to regulate plant development and environmental adaptation. Here, we show that ABI1, a key negative regulator of ABA signaling, is essential for auxin-modulated root development. We performed a microarray analysis using the loss-of-function mutant abi1-3 and Col-0 seedlings treated with IAA. For sHSP22, an endoplasmic reticulum (ER) small heat shock protein-encoding gene, the induction by IAA was dependent on ABI1...
December 29, 2017: Plant Physiology
https://www.readbyqxmd.com/read/29281919/terretonin-m-a-new-meroterpenoid-from-the-thermophilic-aspergillus-terreus-tm8-and-revision-of-the-absolute-configuration-of-penisimplicins
#17
Mohamed Shaaban, Mohammad Magdy El-Metwally, Ahmed Adel Abdel-Razek, Hartmut Laatsch
Terretonin M (1), a new highly oxygenated tetracyclic meroterpenoid, was isolated from the thermophilic fungus Aspergillus terreus TM8 together with 10 known metabolites: terrelumamide A, asterrelenin, 7-prenyl-indolyl-3-carbaldehyde, (3β,5α,6β)-3,5,6-trihydroxy-ergosta-7,22-diene, sitostenone, linoleic acid, ergosterol, uracil, p-hydroxy-benzoic acid, and indole-3-carboxylic acid. The chemical structure of the new compound was elucidated by extensive 1D, 2D NMR, and ESI HR mass measurements, and by comparison with literature data...
December 27, 2017: Natural Product Research
https://www.readbyqxmd.com/read/29275991/phytochrome-a-negatively-regulates-the-shade-avoidance-response-by-increasing-auxin-indole-acidic-acid-protein-stability
#18
Chuanwei Yang, Famin Xie, Yupei Jiang, Zhen Li, Xu Huang, Lin Li
The reduction in the red to far-red light ratio (R/FR) and photosynthetically active radiation caused by dense planting initiates shade avoidance responses (SARs) to help plants compete against their neighbors. However, deep shade attenuates shade-induced stem elongation to suppress excessive reversion toward skotomorphogenic development, in which photoreceptor phytochrome A (PHYA) has been known to play the major role. However, the molecular mechanism underlying PHYA function in deep shade is poorly understood...
December 18, 2017: Developmental Cell
https://www.readbyqxmd.com/read/29274504/a-preliminary-analysis-of-the-effects-of-bisphenol-a-on-the-plant-root-growth-via-changes-in-endogenous-plant-hormones
#19
Xingyi Li, Lihong Wang, Shengman Wang, Qing Yang, Qing Zhou, Xiaohua Huang
Bisphenol A (BPA) is ubiquitous in the environment worldwide, affecting plant growth and development. Endogenous plant hormones serve as switches that regulate plant growth and development. However, plants have different physiological requirements and environmental adaptive capacities during the different growth stages. Here, we investigated the effects of BPA on soybean (Glycine max L.) root growth at the three growth stages and analyzed the mechanisms underlying the effects of BPA on the root growth by assessing changes in endogenous hormone...
December 20, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29259664/a-concise-flow-synthesis-of-indole-3-carboxylic-ester-and-its-derivatisation-to-an-auxin-mimic
#20
Marcus Baumann, Ian R Baxendale, Fabien Deplante
An assembled suite of flow-based transformations have been used to rapidly scale-up the production of a novel auxin mimic-based herbicide which was required for preliminary field trials. The overall synthetic approach and optimisation studies are described along with a full description of the final reactor configurations employed for the synthesis as well as the downstream processing of the reaction streams.
2017: Beilstein Journal of Organic Chemistry
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