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https://www.readbyqxmd.com/read/28432945/exploring-isoxsuprine-hydrochloride-binding-with-human-serum-albumin-in-the-presence-of-folic-acid-and-ascorbic-acid-using-multispectroscopic-and-molecular-modeling-methods
#1
Fereshteh Shiri, Somaye Shahraki, Amin Shahriyar, Mostafa Heidari Majd
Isoxsuprine hydrochloride (vasodilator drug), folic acid and ascorbic acid are medicines which can be utilized alone or simultaneously by pregnant women. In the present work the competitive binding of isoxsuprine hydrochloride (ISO) with human serum albumin (HSA) in the absence and presence of folic acid (FOL) and ascorbic acid (AS) was investigated using different spectroscopic probes and molecular docking studies. The results of fluorescence suggested that isoxsuprine alone or in the presence of ascorbic acid can bind to HSA and quench the fluorescence of HSA with static mechanism but For HSA-folic acid-isoxsuprine system, dynamic type of quenching mechanisms is involved...
April 11, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28432819/identification-of-bioactive-compounds-in-shaoyao-gancao-decoction-using-%C3%AE-2-adrenoceptor-affinity-chromatography
#2
Zehua Li, Haiyang Gao, Jiangying Li, Yajun Zhang
Shaoyao-Gancao decoction, a Chinese herbal formula, is composed of Paeoniae Radix alba and Glycyrrhiza Radix et rhizoma. It has been widely used to treat muscle spasms and asthma. However, little is known about the bioactive components of Shaoyao-Gancao decoction. In the present study, the bioactive compounds in water-extract of Shaoyao-Gancao decoction were separated by the immobilized β2 -adrenoceptor affinity column and identified using quadrupole time-of-flight mass spectrometry. The affinity constants of the separated compounds that bound to β2 -adrenoceptor were determined by frontal analysis...
April 22, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28432729/novel-amino-acid-ester-chlorantraniliprole-conjugates-design-synthesis-phloem-accumulation-and-bioactivity
#3
Guangkai Yao, Yingjie Wen, Chen Zhao, Hanhong Xu
BACKGROUND: Conjugating amino acid and glucose fragments with existed pesticide structures has been proven to be an effective way to introduce phloem mobility to non-phloem mobile species. However, the resulting derivatives always suffered from lower bioactivity compared to their parent compound. To solve this problem, herein, we designed and synthesized a series of ester-capped amino acid conjugated chlorantraniliprole. RESULTS: The systemic test showed that all conjugates exhibited excellent phloem mobility and xylem mobility in a Ricinus communis model...
April 22, 2017: Pest Management Science
https://www.readbyqxmd.com/read/28432381/modulation-of-the-multidrug-efflux-pump-emrd-3-from-vibrio-cholerae-by-allium-sativum-extract-and-the-bioactive-agent-allyl-sulfide-plus-synergistic-enhancement-of-antimicrobial-susceptibility-by-a-sativum-extract
#4
Merissa M Bruns, Prathusha Kakarla, Jared T Floyd, Mun Mun Mukherjee, Robert C Ponce, John A Garcia, Indrika Ranaweera, Leslie M Sanford, Alberto J Hernandez, T Mark Willmon, Grace L Tolson, Manuel F Varela
The causative agent of cholera, Vibrio cholerae, is a public health concern. Multidrug-resistant V. cholerae variants may reduce chemotherapeutic efficacies of severe cholera. We previously reported that the multidrug efflux pump EmrD-3 from V. cholerae confers resistance to multiple structurally distinct antimicrobials. Medicinal plant compounds are potential candidates for EmrD-3 efflux pump modulation. The antibacterial activities of garlic Allium sativum, although poorly understood, predicts that a main bioactive component, allyl sulfide, modulates EmrD-3 efflux...
April 21, 2017: Archives of Microbiology
https://www.readbyqxmd.com/read/28432280/small-molecules-targeting-histone-demethylase-genes-kdms-inhibit-growth-of-temozolomide-resistant-glioblastoma-cells
#5
Barbara Banelli, Antonio Daga, Alessandra Forlani, Giorgio Allemanni, Daniela Marubbi, Maria Pia Pistillo, Aldo Profumo, Massimo Romani
In glioblastoma several histone demethylase genes (KDM) are overexpressed compared to normal brain tissue and the development of Temozolomide (TMZ) resistance is accompanied by the transient further increased expression of KDM5A and other KDMs following a mechanism that we defined as "epigenetic resilience". We hypothesized that targeting KDMs may kill the cells that survive the cytotoxic therapy.We determined the effect of JIB 04 and CPI-455, two KDM inhibitors, on glioblastoma cells and found that both molecules are more effective against TMZ-resistant rather than native cells...
April 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28431483/bioassay-guided-isolation-identification-of-compounds-from-origanum-rotundifolium-and-investigation-of-their-antiproliferative-and-antioxidant-activities
#6
Ramazan Erenler, Bilal Meral, Ozkan Sen, Mahfuz Elmastas, Ali Aydin, Ozgur Eminagaoglu, Gulacti Topcu
CONTEXT: Origanum (Lamiaceae) has been used in food and pharmaceutical industries. OBJECTIVE: Isolation and identification of bioactive compounds from Origanum rotundifolium Boiss. and investigation of their antiproliferative and antioxidant activities. MATERIALS AND METHODS: The aerial part of O. rotundifolium was dried and powdered (1.0 kg ±2.0 g) then extracted with hexane, ethyl acetate, methanol and water. Solvent (3 × 1 L) was used for each extraction for a week at room temperature...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28431473/structures-and-bioactivities-of-seven-flavonoids-from-osmanthus-fragrans-jinqiu-essential-oil-extraction-residues
#7
Jiang-Lian Zhou, Xian-Ying Fang, Jing-Qiu Wang, Lin-Guo Zhao, Yi Li, Feng Tang, Yong-De Yue
Osmanthus fragrans are well-known for their fragrance, but it is wasteful if to discard O. fragrans flower after extracting their essential oils. In this paper, we found that O. fragrans flower residues were rich in flavonoids. Six flavonoids and one phenylethanoid glycoside were isolated from the ethanol extract of O. fragrans flower residues, identified as quercetin (1), rutin (2), verbascoside (3), genistin (4), kaempferol (5), isorhamnetin (6) and naringin (7). In bioactivity study, kaempferol (IC50 = 1...
April 21, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28431297/nano-zirconia-evaluation-of-its-antioxidant-and-anticancer-activity
#8
Siripireddy Balaji, Badal Kumar Mandal, Shivendu Ranjan, Nandita Dasgupta, Ramalingam Chidambaram
Bioactivity of nanomaterials largely depends on its size, shape and crystalline nature. In this work, the smaller sized spherical shaped nano-zirconia (ZrO2 NPs) (of ~9 to 11nm) was fabricated and studied its biological activity especially antioxidant and cytotoxicity against human colon carcinoma (HCT-116) and human lung carcinoma (A-549) cell lines. To have its real applications in biological aspects readily available Eucalyptus globulus (E. globulus) leaf extract was used as an effective capping and reducing agent for its synthesis...
April 8, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28431028/hybrid-de-novo-genome-assembly-of-the-chinese-herbal-fleabane-erigeron-breviscapus
#9
Jing Yang, Guanghui Zhang, Jing Zhang, Hui Liu, Wei Chen, Xiao Wang, Yahe Li, Yang Dong, Shengchao Yang
Background: The plants in the Erigeron genus of the Compositae (Asteraceae) family are commonly called fleabanes, possibly due to the belief that certain chemicals in these plants repel fleas. In the traditional Chinese medicine, Erigeron breviscapus , which is native to China, was widely used in the treatment of cerebrovascular disease. A handful of bioactive compounds, including scutellarin, 3,5-dicaffeoylquinic acid, and 3,4-dicaffeoylquinic acid, have been isolated from the plant...
April 18, 2017: GigaScience
https://www.readbyqxmd.com/read/28430345/healing-response-of-rat-pulp-treated-with-an-injectable-keratin-hydrogel
#10
Lavanya Ajay Sharma, Robert M Love, Mohammad A Ali, Ajay Sharma, Soraia Macari, Avadhoot Avadhani, George J Dias
BACKGROUND: Keratin has shown promising outcomes as a biomaterial due to its inherent bioactivity, biocompatibility and regenerative effects. The effect of keratin on repair and regeneration of dental tissues has never been studied before. Current therapies to treat pulp tissues involve its replacement with inert, synthetic materials that do not have a proper biological function, leading to failure and tooth loss. This study aimed to develop a biocompatible keratin hydrogel (KH) suitable for pulp therapies...
April 20, 2017: Journal of Applied Biomaterials & Functional Materials
https://www.readbyqxmd.com/read/28430344/surfactant-assisted-synthesis-of-polyvinylpyrrolidone-hydroxyapatite-composites-as-a-bone-filler
#11
Masoumeh Meskinfam Langroudi, Masoud Giahi Saravani, Azita Nouri
BACKGROUND: Different methods have been used to prepare bone-like composites from inorganic nanoparticles embedded in polymeric matrixes to obtain the properties and structures required for bone fillers. METHODS: Bone-like nano-hydroxyapatite (nHA) was synthesized using a biomimetic method, with polyvinylpyrrolidone (PVP) as template and sodium dodecyl sulfate (SDS) as surfactant. RESULTS: The results demonstrated the formation of HA composites and showed that polymer and surfactant as the polymer capsule can be properly used to control the size, shape, morphology and dispersion of HA crystals...
April 11, 2017: Journal of Applied Biomaterials & Functional Materials
https://www.readbyqxmd.com/read/28430196/organocatalytic-stereoselective-8-2-and-6-4-cycloadditions
#12
Rasmus Mose, Gert Preegel, Jesper Larsen, Sofie Jakobsen, Eva Høgh Iversen, Karl Anker Jørgensen
Cycloadditions that involve more than six π electrons are termed higher-order cycloadditions and are an excellent tool for solving complex synthetic challenges, as they provide direct access to polycyclic scaffolds that contain medium-sized rings. They have interesting synthetic potential for the discovery of new bioactive molecules and in natural product synthesis. It is peculiar that stereocontrolled [8+2] and [6+4] cycloadditions have been largely neglected for the past 50 years. Here we demonstrate a cross-dienamine activation of 2-cyclopentenone and the unprecedented endocyclic linear-dienamine activation of 2-cyclohexenones and 2-cycloheptenones...
May 2017: Nature Chemistry
https://www.readbyqxmd.com/read/28429944/biotechnological-production-of-dimethoxyflavonoids-using-a-fusion-flavonoid-o-methyltransferase-possessing-both-3-and-7-o-methyltransferase-activities
#13
Danbi Lee, Hye Lin Park, Sang-Won Lee, Seong Hee Bhoo, Man-Ho Cho
Although they are less abundant in nature, methoxyflavonoids have distinct physicochemical and pharmacological properties compared to common nonmethylated flavonoids. Thus, enzymatic conversion and biotransformation using genetically engineered microorganisms of flavonoids have been attempted for the efficient production of methoxyflavonoids. Because of their regiospecificity, more than two flavonoid O-methyltransferases (FOMTs) and enzyme reactions are required to biosynthesize di(or poly)-methoxyflavonoids...
April 21, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28429938/high-resolution-accurate-mass-mass-spectrometry-enables-in-depth-characterization-of-in-vivo-biotransformations-for-intact-antibody-drug-conjugates
#14
Jintang He, Dian Su, Carl K Ng, Luna Liu, Shang-Fan Yu, Thomas H Pillow, Geoffrey Del Rosario, Martine Darwish, Byoung-Chul Lee, Rachana Ohri, Hongxiang Zhou, Xueji Wang, Jiawei Lu, Surinder Kaur, Keyang Xu
Antibody-drug conjugates (ADCs) represent a promising class of therapeutics for the targeted delivery of highly potent cytotoxic drugs to tumor cells to improve bioactivity while minimizing side effects. ADCs are composed of both small and large molecules, and therefore have complex molecular structures. In vivo biotransformations may further increase the complexity of ADCs, representing a unique challenge for bioanalytical assays. Quadrupole time-of-flight mass spectrometry (Q-TOF MS) with electrospray ionization has been widely used for characterization of intact ADCs...
April 21, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28429928/a-dual-enzyme-hydrogen-peroxide-generation-machinery-in-hydrogels-supports-antimicrobial-wound-treatment
#15
Daniela Huber, Gregor Tegl, Anna Mensah, Bianca Beer, Martina Baumann, Nicole Borth, Christoph Sygmund, Roland Ludwig, Georg M Guebitz
The aging population and accompanying diseases like diabetes resulted in an increased occurrence of chronic wounds. Topical wound treatment with antimicrobial agents to inhibit bacterial invasion and promote wound healing is often associated with difficulties. Here, we investigated the potential of succinyl chitosan (SC) - carboxymethyl cellulose (CMC) hydrogels which constantly release clinically relevant levels of hydrogen peroxide (H2O2). CMC hydrogel matrix was in-situ converted by limited hydrolysis by a cellulase into substrates accepted by cellobiose dehydrogenase (CDH) for continuous production of H2O2 (30 µM over 24 h)...
April 21, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28429871/potentiation-of-antibiotic-against-psedomonas-aeruginosa-biofilm-a-study-with-plumbagin-and-gentamicin
#16
Priya Gupta, Arpita Sarkar, Padmani Sandhu, Akshay Daware, Manash C Das, Yusuf Akhter, Surajit Bhattacharjee
AIM: Pseudomonas aeruginosa is one of the fatal biofilm forming pathogens which pose to be a problem in clinical infections, contamination of food and marine ecosystems. In this report a napthoquinone - Plumbagin has been explored for its antimicrobial (antibacterial and antibiofilm) activity against P. aeruginosa biofilm. The ability of Plumbagin to enhance the bioactivity of a known broad spectrum antibiotic was further assayed by combining the sub-MIC doses of Plumbagin with sub-MIC doses of Gentamicin against P...
April 21, 2017: Journal of Applied Microbiology
https://www.readbyqxmd.com/read/28429590/palladium-catalyzed-n-2-aminophenyl-acetamide-assisted-ortho-arylation-of-substituted-benzamides-application-to-the-synthesis-of-urolithins-b-m6-and-m7
#17
M Damoder Reddy, Alexandra N Blanton, E Blake Watkins
Pd-catalyzed, selective, monoarylation of ortho-C-H bonds of various benzamides with aryl/heteroaryl iodides has been realized using N-(2-aminophenyl)acetamide (APA) as a new bidentate directing group for the first time. The reaction was tolerant of a wide range of functional groups, and a variety of biaryl amide derivatives were successfully prepared in good to moderate yield. The utilization of N-(2-aminophenyl)acetamide as a novel directing group, Mn(OAc)2 as a co-oxidant (silver free reaction conditions), and absolute ortho-monoaryl selectivity are notable features of this reaction...
April 21, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28429060/engineered-jadomycin-analogues-with-altered-sugar-moieties-revealing-jads-as-a-substrate-flexible-o-glycosyltransferase
#18
Liyuan Li, Guohui Pan, Xifen Zhu, Keqiang Fan, Wubin Gao, Guomin Ai, Jinwei Ren, Mingxin Shi, Carlos Olano, José A Salas, Keqian Yang
Glycosyltransferases (GTs)-mediated glycodiversification studies have drawn significant attention recently, with the goal of generating bioactive compounds with improved pharmacological properties by diversifying the appended sugars. The key to achieving glycodiversification is to identify natural and/or engineered flexible GTs capable of acting upon a broad range of substrates. Here, we report the use of a combinatorial biosynthetic approach to probe the substrate flexibility of JadS, the GT in jadomycin biosynthesis, towards different non-native NDP-sugar substrates, enabling us to identify six jadomycin B analogues with different sugar moieties...
April 20, 2017: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28428793/transcriptomics-targeted-metabolomics-and-gene-expression-of-blackberry-leaves-and-fruits-indicate-flavonoid-metabolic-flux-from-leaf-to-red-fruit
#19
Enrique Gutierrez, Ana García-Villaraco, José A Lucas, Ana Gradillas, F Javier Gutierrez-Mañero, Beatriz Ramos-Solano
Blackberries (Rubus spp.) are among the high added value food products relevant for human health due to the increasing evidence of the beneficial effects of polyphenols, which are very abundant in these fruits. Interestingly, these compounds also play a role on plant physiology, being especially relevant their role in plant defense against biotic and abiotic stress. Hence, we hypothesize that since blackberry fruits have high amounts of flavonols and anthocyanins, leaves would also have high amounts of these compounds, and can be studied as a source of active molecules; furthermore, leaf synthesis would support their high contents in fruits...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/28428353/development-of-a-bnp1-32-immunoassay-that-does-not-cross-react-with-probnp
#20
Lynley K Lewis, Sara D Raudsepp, Tim G Yandle, Timothy C Prickett, A Mark Richards
BACKGROUND: Plasma B-type natriuretic peptide (BNP) concentration reflects cardiac dysfunction and assists in determining the diagnosis and prognosis of heart failure (HF). Current BNP assays overestimate circulating bioactive BNP1-32 concentrations as they also detect less active BNP metabolites and proBNP. A specific BNP1-32 assay with negligible cross-reactivity to proBNP and/or BNP metabolites may be advantageous. METHODS: We developed a Luminex-based specific BNP1-32 immunoassay and compared results obtained from 3 other BNP assays (a Luminex-based total-BNP assay, our BNP RIA, and the commercially available Abbott Architect BNP assay) in plasma from 42 patients with HF and 22 healthy controls...
April 20, 2017: Clinical Chemistry
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