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https://www.readbyqxmd.com/read/28346994/gc-ms-analysis-and-potential-cytotoxic-activity-of-calyptranthes-grandifolia-o-berg-calyptranthes-tricona-d-legrand-and-myrciaria-plinioides-d-legrand-essential-oil-in-raw264-7-and-cho-k1-cells
#1
D Faleiro, S M Immich, F Majolo, L Mayer, E M Ethur, M I Goettert
The search for new bioactive substances derived from natural products is daily growing. Among biologically active products used in therapeutic approaches, essential oils are described with wide range of therapeutic and pharmacological potential. Plants from Myrtaceae family have the presence of essential oils in its composition. Calyptranthes grandifolia, Calyptranthes tricona and Myrciaria plinioides species belong to this family and are used by the local population. However, there are no reports in the literature describing relevant characteristics about the potential and possible activities of these species...
March 22, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28346790/synthesis-of-chiral-%C3%AE-lactams-via-in-situ-elimination-iridium-catalyzed-asymmetric-hydrogenation-of-racemic-%C3%AE-hydroxy-%C3%AE-lactams
#2
Qianjia Yuan, Delong Liu, Wanbin Zhang
Chiral γ-lactams have been synthesized in excellent yields and enantioselectivities (up to 99% yield and 96% ee) from easily accessible racemic γ-hydroxy γ-lactams via an iridium-phosphoramidite catalyzed asymmetric hydrogenation. The reaction was designed based on insight into the reaction mechanism demonstrated in previous work and can be carried out at a reduced catalyst loading of 0.1 mol % on a gram scale. Several potential bioactive compounds can be synthesized from the reduced products. Mechanistic studies indicated that the reduced products were obtained via the hydrogenation of the N-acyliminium cations, generated from γ-hydroxy γ-lactams...
March 27, 2017: Organic Letters
https://www.readbyqxmd.com/read/28346393/choerosponins-a-and-b-two-new-cytotoxic-bridged-ring-ketones-and-the-determination-of-their-absolute-configurations
#3
Chang-Wei Li, Bing Han, Bing Cai, Cheng-Bin Cui
Bioactivity-directed fractionation of antitumor compounds from the stem barks of Choerospondias axillaries (Roxb.) Burtt et Hill (Anacardiaceae) afforded two new cytotoxic bridged-ring ketones, choerosponins A (1) and B (2), and their structures were elucidated by spectroscopic methods; their stereochemistry was determined by NOE difference experiments, CD spectra and the modified Mosher's method. Compound 1 has a rare dioxatricyclo skeleton. Flow cytometry and SRB methods were employed to evaluate the antitumor activity of the two compounds against tsFT210, HCT-15, HeLa, A2780 and MCF-7 cell lines, and both of them showed strong cytotoxicity...
March 27, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28346380/constituents-of-the-roots-of-dichapetalum-pallidum-and-their-anti-proliferative-activity
#4
Dorcas Osei-Safo, Godwin Akpeko Dziwornu, Regina Appiah-Opong, Mary Anti Chama, Isaac Tuffour, Reiner Waibel, Richard Amewu, Ivan Addae-Mensah
As part of our search for bioactive compounds from the Dichapetalaceae, repeated chromatographic purification of the roots of a hitherto unexamined species, Dichapetalum pallidum, led to the isolation of the newly occurring 7-hydroxydichapetalin P (1) and the known dichapetalins A (2) and X (3). Also isolated were the known compounds friedelin-2,3-lactone (4), friedelan-3-one (6), friedelan-3β-ol (7) and pomolic (8), as well as the dipeptide aurantiamide acetate (5). The compounds were characterized by direct interpretation of their IR, 1D NMR and 2D NMR spectral data and by comparison of their physico-chemical data, including their chromatographic profiles, with the literature and authentic samples in our compound library for the genus Dichapetalum...
March 27, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28346340/a-place-to-call-home-an-analysis-of-the-bacterial-communities-in-two-tethya-rubra-samaai-and-gibbons-2005-populations-in-algoa-bay-south-africa
#5
Samantha C Waterworth, Meesbah Jiwaji, Jarmo-Charles J Kalinski, Shirley Parker-Nance, Rosemary A Dorrington
Sponges are important sources of bioactive secondary metabolites. These compounds are frequently synthesized by bacterial symbionts, which may be recruited from the surrounding seawater or transferred to the sponge progeny by the parent. In this study, we investigated the bacterial communities associated with the sponge Tethya rubra Samaai and Gibbons 2005. Sponge specimens were collected from Evans Peak and RIY Banks reefs in Algoa Bay, South Africa and taxonomically identified by spicule analysis and molecular barcoding...
March 25, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28346089/a-chemogenomic-screening-platform-used-to-identify-chemotypes-perturbing-hsp90-pathways
#6
Fiona M Thomas, Kourtney M Goode, Bartek Rajwa, Andrew B Bieberich, Larisa V Avramova, Tony R Hazbun, V Jo Davisson
Compounds that modulate the heat shock protein (HSP) network have potential in a broad range of research applications and diseases. A yeast-based liquid culture assay that measured time-dependent turbidity enabled the high-throughput screening of different Saccharomyces cerevisae strains to identify HSP modulators with unique molecular mechanisms. A focused set of four strains, with differing sensitivities to Hsp90 inhibitors, was used to screen a compound library of 3680 compounds. Computed turbidity curve functions were used to classify strain responses and sensitivity to chemical effects across the compound library...
January 1, 2017: SLAS Discov
https://www.readbyqxmd.com/read/28346030/antimicrobial-activity-of-eugenol-and-essential-oils-containing-eugenol-a-mechanistic-viewpoint
#7
Anna Marchese, Ramona Barbieri, Erika Coppo, Ilkay Erdogan Orhan, Maria Daglia, Seyed Fazel Nabavi, Morteza Izadi, Mohammad Abdollahi, Seyed Mohammad Nabavi, Marjan Ajami
Eugenol is a hydroxyphenyl propene, naturally occurring in the essential oils of several plants belonging to the Lamiaceae, Lauraceae, Myrtaceae, and Myristicaceae families. It is one of the major constituents of clove (Syzygium aromaticum (L.) Merr. & L.M. Perry, Myrtaceae) oil and is largely used in both foods and cosmetics as a flavoring agent. A large body of recent scientific evidence supports claims from traditional medicine that eugenol exerts beneficial effects on human health. These effects are mainly associated with antioxidant and anti-inflammatory activities...
March 27, 2017: Critical Reviews in Microbiology
https://www.readbyqxmd.com/read/28345579/inhibition-of-delta-secretase-improves-cognitive-functions-in-mouse-models-of-alzheimer-s-disease
#8
Zhentao Zhang, Obiamaka Obianyo, Elfriede Dall, Yuhong Du, Haian Fu, Xia Liu, Seong Su Kang, Mingke Song, Shan-Ping Yu, Chiara Cabrele, Mario Schubert, Xiaoguang Li, Jian-Zhi Wang, Hans Brandstetter, Keqiang Ye
δ-secretase, also known as asparagine endopeptidase (AEP) or legumain, is a lysosomal cysteine protease that cleaves both amyloid precursor protein (APP) and tau, mediating the amyloid-β and tau pathology in Alzheimer's disease (AD). Here we report the therapeutic effect of an orally bioactive and brain permeable δ-secretase inhibitor in mouse models of AD. We performed a high-throughput screen and identified a non-toxic and selective δ-secretase inhibitor, termed compound 11, that specifically blocks δ-secretase but not other related cysteine proteases...
March 27, 2017: Nature Communications
https://www.readbyqxmd.com/read/28345490/challenges-and-complexity-of-functionality-evaluation-of-flavan-3-ol-derivatives
#9
Akiko Saito
Flavan-3-ol derivatives are common plant-derived bioactive compounds. In particular, (-)-epigallocatechin-3-O-gallate shows various moderate biological activities without severe toxicity, and its health-promoting effects have been widely studied because it is a main ingredient in green tea and is commercially available at low cost. Although various biologically active flavan-3-ol derivatives are present as minor constituents in plants as well as in green tea, their biological activities have yet to be revealed, mainly due to their relative unavailability...
March 27, 2017: Bioscience, Biotechnology, and Biochemistry
https://www.readbyqxmd.com/read/28345372/screening-of-intestinal-crypt-organoids
#10
Svenja Ley, Olaf Galuba, Adrian Salathe, Nicolas Melin, Alexandra Aebi, Monika Pikiolek, Judith Knehr, Walter Carbone, Martin Beibel, Florian Nigsch, Guglielmo Roma, Giovanni d'Ario, Susan Kirkland, Laure C Bouchez, Caroline Gubser Keller, Tewis Bouwmeester, Christian N Parker, Heinz Ruffner
Oral and intestinal mucositis is a debilitating side effect of radiation treatment. A mouse model of radiation-induced mucositis leads to weight loss and tissue damage, reflecting the human ailment as it responds to keratinocyte growth factor (KGF), the standard-of-care treatment. Cultured intestinal crypt organoids allowed the development of an assay monitoring the effect of treatments of intestinal epithelium to radiation-induced damage. This in vitro assay resembles the mouse model as KGF and roof plate-specific spondin-1 (RSPO1) enhanced crypt organoid recovery following radiation...
January 1, 2017: SLAS Discov
https://www.readbyqxmd.com/read/28344322/astragaloside-iv-attenuates-free-fatty-acid-induced-er-stress-and-lipid-accumulation-in-hepatocytes-via-ampk-activation
#11
Bing Zhou, Dan-Li Zhou, Xiao-Hong Wei, Rong-Yu Zhong, Jie Xu, Liao Sun
Although the pathogenesis of non-alcoholic fatty liver disease (NAFLD) is not completely understood, the increased influx of free fatty acids (FFAs) into the liver and the FFA-induced hepatic endoplasmic reticulum (ER) stress are two crucial pathogenic processes in the initiation and development of NAFLD. In this study we investigated the effects of astragaloside IV (AS-IV), a bioactive compound purified from Astragali Radix, on FFA-induced lipid accumulation in hepatocytes and elucidated the underlying mechanisms...
March 27, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28343627/invited-review-milk-phospholipid-vesicles-their-colloidal-properties-and-potential-as-delivery-vehicles-for-bioactive-molecules
#12
E Arranz, M Corredig
The milk fat globule membrane (MFGM) is a unique colloidal assembly of phospholipids and proteins, with numerous potential applications as functional ingredient. The phospholipid components of the MFGM are gaining interest as they are a useful matrix for use as a constituent of delivery systems such as liposomes. Liposomes formulated with milk phospholipids are becoming an alternative to other sources of phospholipids such as soybean or egg yolk. However, incorporation of phospholipids fractionated from the milk fat globule membrane in dairy products requires an in-depth understanding of the functional properties of phospholipids...
March 23, 2017: Journal of Dairy Science
https://www.readbyqxmd.com/read/28343034/bioactivities-of-achillea-phrygia-and-bupleurum-croceum-based-on-the-composition-of-phenolic-compounds-in-vitro-and-in-silico-approaches
#13
Gokhan Zengin, Gizem Bulut, Adriano Mollica, Mehmet Zeki Haznedaroglu, Ahmet Dogan, Abdurrahman Aktumsek
This study presents the effects of the Achillea phrygia Boiss. et Bal. and Bupleurum croceum Fenzl. extracts obtained by different solvents (ethyl acetate, methanol and water) on selected enzyme inhibitory effects and antioxidant ability with screening bioactive compounds. Total and individual bioactive compounds were detected by spectrophotometric and HPLC-DAD techniques. Antioxidant abilities were evaluated by different methods including free radical scavenging (ABTS and DPPH), reducing power (CUPRAC and FRAP), phosphomolybdenum and metal chelating...
March 22, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28342817/complete-genome-sequence-of-streptomyces-griseochromogenes-atcc-14511-t-a-producer-of-nucleoside-compounds-and-diverse-secondary-metabolites
#14
Wu Lijuan, Guoqing Chen, Guozhong Feng
ATCC 14511(T) (=DSM 40499, =NBRC 13413) is a type strain of Streptomyces griseochromogenes. It is known as a producer of nucleoside antibiotic, blasticidin S. In this report we present the complete genome sequence of S. griseochromogenes ATCC 14511(T), which consists of 10,764,674bp with a linear chromosome, 9,822 protein-coding genes, 6 rRNA operons, 74 tRNA and 3 sRNA. The genomic analysis revealed that 52 putative gene clusters are involved in the biosynthesis of secondary metabolites, including four gene clusters of nucleoside antibiotics...
March 22, 2017: Journal of Biotechnology
https://www.readbyqxmd.com/read/28342710/emerging-role-of-chemoprotective-agents-in-the-dynamic-shaping-of-plasma-membrane-organization
#15
REVIEW
Natividad R Fuentes, Michael L Salinas, Eunjoo Kim, Robert S Chapkin
In the context of an organism, epithelial cells by nature are designed to be the defining barrier between self and the outside world. This is especially true for the epithelial cells that form the lining of the digestive tract, which absorb nutrients and serve as a barrier against harmful substances. These cells are constantly bathed by a complex mixture of endogenous (bile acids, mucus, microbial metabolites) and exogenous (food, nutrients, drugs) bioactive compounds. From a cell biology perspective, this type of exposure would directly impact the plasma membrane, which consists of a myriad of complex lipids and proteins...
March 22, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28342583/affinity-chromatographic-methodologies-based-on-immobilized-voltage-dependent-anion-channel-isoform-1-and-application-in-protein-ligand-interaction-analysis-and-bioactive-compounds-screening-from-traditional-medicine
#16
Qian Li, Pan Qiao, Xiu Chen, Jing Wang, Liujiao Bian, Xiaohui Zheng
Voltage dependent anion channel isoform 1 (VDAC-1) serves as an attractive target of anti-cancer drugs by mediating the entry and exit of metabolites between cytoplasm and mitochondria. This work reports on the preparation of a VDAC-1-based bioaffinity chromatographic stationary phase by linking the protein on lecithin modified microspheres. An assay of chromatographic methods including frontal analysis, zonal elution, injection dependent analysis and nonlinear chromatography were utilized to investigate the bindings of ATP, NADH and NADPH to VDAC-1...
March 18, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28342399/design-synthesis-and-biological-evaluation-of-pegylated-xenopus-glucagon-like-peptide-1-derivatives-as-long-acting-hypoglycemic-agents
#17
Jing Han, Yiyun Wang, Qinghua Meng, Guangchao Li, Fangmin Huang, Su Wu, Yingying Fei, Feng Zhou, Junjie Fu
In order to develop novel long-acting GLP-1 derivatives, a peptide hybrid (1a) from human GLP-1 and Xenopus GLP-1 discovered in our previous research was selected as the lead compound. Exendin-4 inspired modification resulted in peptide 1b with enhanced glucose-lowering activity. Cysteine mutated 1b derivatives with reserved bioactivity were further site-specifically connected with mPEG2000-MAL to provide conjugates 3a-h, among which 3d and 3e were found to have significantly improved hypoglycemic activity and insulinotropic ability than GLP-1...
March 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28340896/bioactive-constituents-from-transformed-root-cultures-of-nepeta-teydea
#18
Braulio M Fraga, Azucena González-Coloma, Sergio Alegre-Gómez, Matías López-Rodríguez, Leonardo J Amador, Carmen E Díaz
A phytochemical study of an extract from transformed root cultures of Nepeta teydea, induced by Agrobacterium rhizogenes, led to the isolation of the following new compounds: the sesquiterpene (-)-cinalbicol, the diterpene teydeadione (6,11,14-trihydroxy-12-methoxy-abieta-5,8,11,13,15-penten-7-one), a degraded C23-triterpene (teydealdehyde) and three fatty acid esters of lanosta-7,24-dien-3β-ol. The propyl ester of rosmarinic acid was also isolated for the first time from a natural source. In addition, two dehydroabietane diterpenes, eight triterpenes and eighteen known phenolic compounds were obtained...
January 2017: Phytochemistry
https://www.readbyqxmd.com/read/28340490/a-novel-method-of-neo-osseous-flap-prefabrication-induction-of-free-calvarial-periosteum-with-bioactive-glass
#19
Ali Aliyev, Omer Ekin, Ozan Bitik, Gokhan Tuncbilek
Background Reconstruction of craniofacial bone defects is a primary focus of craniofacial surgery. Although autogenous bone grafts remain as the gold standard, alloplastic materials have also gained widespread popularity due to their off-the-shelf availability, ease of use, and durability. In addition to replacing the missing bone, some of these alloplastic materials have also been found to induce new bone formation. Objectives In this study, the phenomenon of neo-osseous induction with bioactive glass was investigated for different implant-soft tissue configurations...
March 24, 2017: Journal of Reconstructive Microsurgery
https://www.readbyqxmd.com/read/28340400/pharmacoinformatics-exploration-of-polyphenol-oxidases-leading-to-novel-inhibitors-by-virtual-screening-and-molecular-dynamic-simulation-study
#20
Mubashir Hassan, Qamar Abbas, Zaman Ashraf, Ahmed A Moustafa, Sung-Yum Seo
Polyphenol oxidases (PPOs)/tyrosinases are metal-dependent enzymes and known as important targets for melanogenesis. Although considerable attempts have been conducted to control the melanin-associated diseases by using various inhibitors. However, the exploration of the best anti-melanin inhibitor without side effect still remains a challenge in drug discovery. In present study, protein structure prediction, ligand-based pharmacophore modeling, virtual screening, molecular docking and dynamic simulation study were used to screen the strong novel inhibitor to cure melanogenesis...
March 15, 2017: Computational Biology and Chemistry
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