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https://www.readbyqxmd.com/read/28813533/18%C3%A3-glycyrrhetinic-acid-derivative-promotes-proliferation-migration-and-aquaporin-3-expression-in-human-dermal-fibroblasts
#1
Chi-Feng Hung, Chien-Yu Hsiao, Wen-Hao Hsieh, Hsin-Ju Li, Yi-Ju Tsai, Chun-Nan Lin, Hsun-Hsien Chang, Nan-Lin Wu
Licorice (Glycyrrhiza) species have been widely used as a traditional medicine and a natural sweetener in foods. The 18β-glycyrrhetinic acid (18β-GA) is a bioactive compound in licorice that exhibits potential anti-cancer, anti-inflammatory, and anti-microbial activities. Many synthesized derivatives of 18β-GA have been reported to be cytotoxic and suggested for the treatment of malignant diseases. In this study, we explored the possible pharmacological roles of an 18β-GA derivative in skin biology using primary human dermal fibroblasts and HaCaT keratinocytes as cell models...
2017: PloS One
https://www.readbyqxmd.com/read/28812892/designer-extracts-as-tools-to-balance-estrogenic-and-chemopreventive-activities-of-botanicals-for-women-s-health
#2
Birgit M Dietz, Shao-Nong Chen, René F Ramos Alvarenga, Huali Dong, Dejan Nikolić, Martin Biendl, Richard B van Breemen, Judy L Bolton, Guido F Pauli
Botanical dietary supplements contain multiple bioactive compounds that target numerous biological pathways. The lack of uniform standardization requirements is one reason that inconsistent clinical effects are reported frequently. The multifaceted biological interactions of active principles can be disentangled by a coupled pharmacological/phytochemical approach using specialized ("knock-out") extracts. This is demonstrated for hops, a botanical for menopausal symptom management. Employing targeted, adsorbent-free countercurrent separation, Humulus lupulus extracts were designed for pre- and postmenopausal women by containing various amounts of the phytoestrogen 8-prenylnaringenin (8-PN) and the chemopreventive constituent xanthohumol (XH)...
August 16, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28812768/chemical-nutritive-composition-and-a-wide-range-of-bioactive-properties-of-honey-mushroom-armillaria-mellea-vahl-fr-kummer
#3
Marina Kostić, Marija Smiljković, Jovana Petrović, Jasmina Glamočlija, Lillian Barros, Isabel C F R Ferreira, Ana Ćirić, Marina Soković
A. mellea fruiting bodies collected from nature were chemically characterized and shown to be rich in carbohydrates (81.25 g per 100 g dw), ash, fat and proteins (8.84 g per 100 g dw, 1.97 g per 100 g dw and 1.81 g per 100 g dw, respectively). Mannitol was the main free sugar while malic acid was the most abundant organic acid. δ-Tocopherol was the dominant form of tocopherols with 42.41 μg per 100 g dw. Polyunsaturated fatty acids were predominant, followed by saturated and monounsaturated fatty acids. A methanolic extract prepared from these samples was tested for antioxidant, quorum sensing and antimicrobial assays, as well as for its cytotoxicity effects...
August 16, 2017: Food & Function
https://www.readbyqxmd.com/read/28811751/bioactive-potential-of-3d-printed-oleo-gum-resin-disks-b-papyrifera-c-myrrha-and-s-benzoin-loading-nanooxides-tio2-p25-cu2o-and-moo3
#4
Diogo José Horst, Sergio Mazurek Tebcherani, Evaldo Toniolo Kubaski, Rogério de Almeida Vieira
This experimental study investigates the bioactive potential of filaments produced via hot melt extrusion (HME) and intended for fused deposition modeling (FDM) 3D printing purposes. The oleo-gum-resins from benzoin, myrrha, and olibanum in pure state and also charged with 10% of metal oxide nanoparticles, TiO2, P25, Cu2O, and MoO3, were characterized by ultraviolet-visible (UV-Vis) and Fourier transform infrared (FTIR) spectroscopy, energy-dispersive X-ray microanalysis (EDXMA), scanning electron microscopy (SEM), and differential scanning calorimetry (DSC)...
2017: Bioinorganic Chemistry and Applications
https://www.readbyqxmd.com/read/28811187/chiral-resolution-absolute-configuration-and-bioactivity-of-a-new-racemic-asarone-derivative-from-the-rhizome-of-acorus-tatarinowii
#5
En Gao, Fei-Fei Ren, Jian Zou, Yang Yu, Hong-Xia Fan, Zheng-Qun Zhou, Guo-Dong Chen, Rong-Rong He, Xin-Sheng Yao, Hao Gao
A new asarone-derived racemate (1) was isolated from the rhizome of Acorus tatarinowii. The structure of 1 was established by comprehensive spectroscopic analyses, and it was successfully resolved by chiral HPLC, demonstrating that it is racemic. The absolute configurations of 1a [(-)-acortatarone A] and 1b [(+)-acortatarone A] were determined using quantum chemical calculations. Compounds 1a and 1b were the first cases of asarone derivatives with the 5,7-dialkyl-6-aryl-8-oxabicyclo[3.2.1]oct-3-en-2-one core...
August 12, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28810534/thymoquinone-prevents-endoplasmic-reticulum-stress-and-mitochondria-induced-apoptosis-in-a-rat-model-of-partial-hepatic-warm-ischemia-reperfusion
#6
Ahlem Bouhlel, Ben Mosbah, Hadj Abdallah, Catherine Ribault, Roselyne Viel, Saber Mannaï, Anne Corlu, Ben Abdennebi
This study was undertaken to evaluate the protective effect of thymoquinone (TQ), the bioactive compound of Nigella sativa seeds, against warm ischemia-reperfusion (I/R) injury in liver. Rats were given an oral administration of a vehicle solution (sham group) or TQ at the appropriate dose (10, 20, 30 and 40mg/kg) for ten days consecutively. Following, they were subjected to 60min of partial hepatic ischemia followed by 24h of reperfusion. .Transaminase activities, histopathological changes, TNFα and antioxidant parameters were evaluated...
August 11, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28810523/reactive-oxygen-species-mediated-nf-%C3%AE%C2%BAb-p38-feedback-loop-implicated-in-proliferation-inhibition-of-hfls-ra-cells-induced-by-1-7-dihydroxy-3-4-dimethoxyxanthone
#7
Jian Zuo, De-Yu Dou, Hui-Fang Wang, Yan-Hong Zhu, Yan Li, Jia-Jie Luan
1,7-Dihydroxy-3,4-dimethoxyxanthone (XAN) is a bioactive compound isolated from Securidaca inappendiculata Hassk. and exerts the inhibitory effects on fibroblast-like synoviocytes by targeting NF-κB and p38. This study was designed to elucidate mechanisms underlying the divergent regulation on the two pathways in HFLS-RA cells by XAN. Expressions of hallmark proteins and transcription of GADD45α mRNA were determined by Western-blot and RT-qPCR methods, respectively. Fluorescence staining was employed to evaluate intracellular oxidative stress...
August 11, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28809458/redox-neutral-manganese-i-catalyzed-c-h-activation-traceless-directing-group-enabled-regioselective-annulation
#8
Qingquan Lu, Steffen Greßies, Sara Cembellín, Felix Klauck, Constantin Daniliuc, Frank Glorius
An unprecedented strategy using traceless directing groups (TDG) to promote the redox-neutral Mn(I)-catalyzed regioselective synthesis of N-heterocycles is reported. Alkyne coupling partners bearing traceless directing group, which serve as both chelator and internal oxidant, were used to control the regioselectivity of the annulation reactions. This operationally simple approach is highly effective with previously challenging unsymmetrical alkyne systems, including unbiased dialkyl alkynes, featuring switchable regioselectivity, simple conditions, and gram-scale synthesis...
August 15, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28808992/a-photoaffinity-labeling-based-chemoproteomics-strategy-for-unbiased-target-deconvolution-of-small-molecule-drug-candidates
#9
Jason R Thomas, Scott M Brittain, Jennifer Lipps, Luis Llamas, Rishi K Jain, Markus Schirle
The combination of photoaffinity labeling (PAL) and quantitative chemoproteomics enables the comprehensive, unbiased determination of protein interaction profiles to support target identification of bioactive small molecules. This approach is amenable to cells in culture and compatible with pharmacologically relevant transmembrane target classes like G-protein coupled receptors and ions channels which have been notoriously hard to access by conventional chemoproteomics approaches. Here, we describe a strategy that combines PAL probe titration and competition with excess parental compounds with the goal of enabling the identification of specific interactors as well as assessing the functional relevance of a binding event for the phenotype under investigation...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28808385/anti-inflammatory-effect-of-etlingera-pavieana-pierre-ex-gagnep-r-m-sm-rhizomal-extract-and-its-phenolic-compounds-in-lipopolysaccharide-stimulated-macrophages
#10
Ekaruth Srisook, Mullika Palachot, Sakulrat Mankhong, Klaokwan Srisook
BACKGROUND: In our continuing search for anti-inflammatory agents from Thai herbs, Etlingera pavieana (Pierre ex Gagnep.) R.M.Sm. showed potent inhibition on nitric oxide (NO) production in lipopolysaccharide (LPS)-induced macrophages. However, the mechanism behind its inhibitory effect has not been yet explored, and little is known regarding its bioactive compounds responsible for the anti-inflammatory effect. OBJECTIVE: In the present study, anti-inflammatory effect of hexane, ethyl acetate, and water fractions of rhizomal ethanol extracts of E...
July 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28808259/combination-of-chemical-fingerprint-and-bioactivity-evaluation-to-explore-the-antibacterial-components-of-salvia-miltiorrhizae
#11
Wei-Jun Kong, Shan-Shan Zhang, Yan-Ling Zhao, Ming-Quan Wu, Ping Chen, Xiao-Ru Wu, Xin-Ping Ma, Wei-Ying Guo, Mei-Hua Yang
The aim of this study was to explore the possible antibacterial components of Salvia miltiorrhizae on Pseudomonas aeruginosa using a combination of chemical fingerprint and bioactivity evaluation. The chemical fingerprints of 32 batches of S. miltiorrhizae samples from different sources were developed using high-performance liquid chromatography with diode array detection, and then were evaluated by similarity analysis and hierarchical clustering analysis. Anti-P. aeruginosa activity was determined by microcalorimetry...
August 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28807875/bioactive-isoflavones-from-pueraria-lobata-root-and-starch-different-extraction-techniques-and-carbonic-anhydrase-inhibition
#12
Andrei Mocan, Simone Carradori, Marcello Locatelli, Daniela Secci, Stefania Cesa, Adriano Mollica, Simona Riga, Andrea Angeli, Claudiu T Supuran, Christian Celia, Luisa Di Marzio
Kudzu, the dried root of an important edible plant (Pueraria lobata), is used in Traditional Chinese Medicine for the important nutritional value strictly related to its isoflavone derivatives. These compounds characterize the quality of kudzu contained in different preparations, as pharmaceutical ingredient as well as dietary/food supplement (e.g. starch). The optimization of the isoflavones recovery, monitored by HPLC-PDA, through different innovative and conventional extraction techniques, e.g. microwave-assisted, ultrasound-assisted and conventional extraction, represented a suitable challenge in food industry and natural products evaluation...
August 11, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28807849/danshen-improves-survival-of-patients-with-colon-cancer-and-dihydroisotanshinone-i-inhibit-the-proliferation-of-colon-cancer-cells-via-apoptosis-and-skp2-signaling-pathway
#13
Yin-Yin Lin, I-Yun Lee, Wen-Shih Huang, Yu-Shin Lin, Feng-Che Kuan, Li-Hsin Shu, Yu-Ching Cheng, Yao-Hsu Yang, Ching-Yuan Wu
ETHNOPHARMACOLOGICAL RELEVANCE: Danshen (Salvia miltiorrhiza Bunge) is widely used in traditional Chinese medicine. However, it's definite clinical effect and mechanism on colon carcinoma is unclear. AIM OF THE STUDY: To test the hypothesis that the protective effect of danshen on colon cancer and discover the bioactive compounds through in vitro study. MATERIALS AND METHODS: We conducted a nationwide cohort study by using population-based data from the Taiwan National Health Insurance Research Database (NHIRD)...
August 11, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28807090/mass-spectral-characterization-and-uplc-quantitation-of-3-deoxyanthocyanidins-in-sorghum-bicolor-varietals
#14
Nathan P Stern, Jatinder Rana, Amitabh Chandra, John Balles
A quantitative ultra-performance LC (UPLC) method was developed and validated to successfully separate, identify, and quantitate the major polyphenolic compounds present in different varieties of sorghum (Sorghum bicolor) feedstock. The method was linear from 3.2 to 320 ppm, with an r² of 0.99999 when using luteolinidin chloride as the external standard. Method accuracy was determined to be 99.5%, and precision of replicate preparations was less than 1% RSD. Characterization by UPLC-MS determined that the predominant polyphenolic components of the sorghum varietals were 3-deoxyanthocyanidins (3-DXAs)...
August 10, 2017: Journal of AOAC International
https://www.readbyqxmd.com/read/28806514/phenolic-compounds-profiling-of-virgin-olive-oils-from-different-varieties-cultivated-in-mendoza-argentina-by-using-liquid-chromatography-mass-spectrometry
#15
R P Monasterio, L Olmo-García, A Bajoub, A Fernandez-Gutierrez, A Carrasco-Pancorbo
The aim of this work was to achieve a preliminary characterization of the profile of the phenolic fraction of virgin olive oils (VOOs) from Maipú (Mendoza, Argentina). Thus, 25 commercial VOO samples from Arauco, Arbequina, Picual, Frantoio, Changlot, Empeltre, Nevadillo, Manzanilla and Coratina (both monovarietals and blends) were analyzed using LC-ESI-QTOF MS and LC-ESI-IT MS for identification and quantification purposes, respectively. A rapid LC method (15 min) accomplished quantitative information about a total of 40 phenolic compounds, including secoiridoid derivatives, which have not been evaluated before in samples coming from the sub-region so-called Maipú (Mendoza province, Argentina)...
August 14, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28806050/linking-high-throughput-screens-to-identify-moas-and-novel-inhibitors-of-mycobacterium-tuberculosis-dihydrofolate-reductase
#16
John P Santa Maria, Yumi Park, Lihu Yang, Nicholas Murgolo, Michael D Altman, Paul Zuck, Greg Adam, Chad Chamberlin, Peter Saradjian, Peter Dandliker, Helena I M Boshoff, Clifton E Barry, Charles Garlisi, David B Olsen, Katherine Young, Meir Glick, Elliott Nickbarg, Peter S Kutchukian
Though phenotypic and target-based high-throughput screening approaches have been employed to discover new antibiotics, the identification of promising therapeutic candidates remains challenging. Each approach provides different information, and understanding their results can provide hypotheses for mechanism of action (MoA) and reveal actionable chemical matter. Here we describe a framework for identifying efficacy targets of bioactive compounds. High throughput biophysical profiling against a broad range of targets coupled with machine learning is employed to identify chemical features with predicted efficacy targets for a given phenotypic screen...
August 14, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28805711/a-dereplication-and-bioguided-discovery-approach-to-reveal-new-compounds-from-a-marine-derived-fungus-stilbella-fimetaria
#17
Sara Kildgaard, Karolina Subko, Emma Phillips, Violaine Goidts, Mercedes de la Cruz, Caridad Díaz, Charlotte H Gotfredsen, Birgitte Andersen, Jens C Frisvad, Kristian F Nielsen, Thomas O Larsen
A marine-derived Stilbella fimetaria fungal strain was screened for new bioactive compounds based on two different approaches: (i) bio-guided approach using cytotoxicity and antimicrobial bioassays; and (ii) dereplication based approach using liquid chromatography with both diode array detection and high resolution mass spectrometry. This led to the discovery of several bioactive compound families with different biosynthetic origins, including pimarane-type diterpenoids and hybrid polyketide-non ribosomal peptide derived compounds...
August 13, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28805683/analysis-and-comparison-of-the-antioxidant-component-of-portulaca-oleracea-leaves-obtained-by-different-solid-liquid-extraction-techniques
#18
Monica Gallo, Esterina Conte, Daniele Naviglio
Portulaca oleracea is a wild plant pest of orchards and gardens, but is also an edible vegetable rich in beneficial nutrients. It possesses many antioxidant properties due to the high content of vitamins, minerals, omega-3 essential fatty acids and other healthful compounds; therefore, the intake of purslane and/or its bioactive compounds could help to improve the health and function of the whole human organism. Accordingly, in this work it was analyzed and compared to the extractive capacity of the antioxidant component of purslane leaves obtained by solid-liquid extraction techniques such as: hot-maceration, maceration with ultrasound, rapid solid-liquid dynamic extraction using the Naviglio extractor, and a combination of two techniques (mix extraction)...
August 12, 2017: Antioxidants (Basel, Switzerland)
https://www.readbyqxmd.com/read/28805459/opuntia-ficus-indica-l-miller-as-a-source-of-bioactivity-compounds-for-health-and-nutrition
#19
M Aragona, E R Lauriano, S Pergolizzi, C Faggio
Plants with beneficial properties are known in traditional medicine. Nowadays, in spite of widespread availability of synthetic compounds, the search goes towards natural compounds to lower cost and few side effects. The increasing interest in preventive medicine encourages use of nutraceuticals, bioactive compounds of vegetable origin with important nutritional values. Among the medicinal plants, Opuntia ficus-indica (L.) Miller (Family Cactaceae, subfamily Opuntiodeae, Genus Opuntia, subgenus Platyopuntia, species Opuntia ficus-indica (L...
August 14, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28804992/gold-catalyzed-4-2-annulation-cyclization-cascades-of-benzisoxazoles-with-propiolate-derivatives-to-access-highly-oxygenated-tetrahydroquinolines
#20
Rajkumar Lalji Sahani, Rai-Shung Liu
This work describes gold-catalyzed annulations of electron-deficient alkynes with benzisoxazoles to yield quinoline oxides chemoselectively. Chemical functionalizations of these resulting azacyclic compounds afforded various oxygenated tetrahydroquinolines that are present as the cores of many bioactive molecules. With the same reactants, a new relay catalysis using gold and Zn(II) catalysts affords highly oxygenated tetrahydroquinoline derivatives stereoselectively.
August 13, 2017: Angewandte Chemie
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