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https://www.readbyqxmd.com/read/29793211/synthesis-and-evaluation-of-novel-triazolyl-quinoline-derivatives-as-potential-antileishmanial-agents
#1
Akanksha Upadhyay, Pragati Kushwaha, Sampa Gupta, Ranga Prasad Dodda, Karthik Ramalingam, Ruchir Kant, Neena Goyal, Koneni V Sashidhara
The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover novel series of 25 compounds for the development of new antileishmanial agents. A series of triazolyl 2-methyl-4-phenylquinoline-3-carboxylate derivatives has been synthesized via click chemistry inspired molecular hybridization approach and evaluated against Leishmania donovani. Most of the screened derivatives exhibited significant in vitro anti-leishmanial activity against promastigote (IC50 ranging from 2...
May 12, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29792906/four-novel-antibacterial-sesquiterpene-%C3%AE-amino-acid-quaternary-ammonium-hybrids-from-the-mycelium-of-mushroom-stereum-hirsutum
#2
Yuan-Chang Duan, Jun Feng, Na Bai, Guo-Hong Li, Ke-Qin Zhang, Pei-Ji Zhao
The mushroom Stereum hirsutum is parasitized by Tremella aurantia to form a heterogeneous basidiocarp Jin'er, which has been used as food and folk medicine in Chinese society. In present work, the S. hirsutum was fermented in YMG broth, and four novel mixed terpenes, stereumamides A-D (1-4), which are sesquiterpenes combined with α-amino acids to form quaternary ammonium hybrids, were isolated from the Stereum hirsutum FP-91666 and their structures were elucidated by spectroscopic data analysis. Stereumamides A and D showed antibacterial activity against Escherichia coli, Staphylococcus aureus, and Salmonella typhimurium, with the minimum inhibitory concentration (MIC) values of 12...
May 21, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29792895/pharmacogenomics-of-drug-induced-liver-injury-dili-molecular-biology-to-clinical-applications
#3
REVIEW
Kalaiyarasi Kaliyaperumal, Jane I Grove, Robin M Delahay, William J H Griffiths, Adam Duckworth, Guruprasad P Aithal
A number of drug-specific and host-related factors contribute to the development of drug-induced liver injury (DILI). Investigations focused on genetic susceptibility to DILI have advanced our understanding of the pathogenesis of this rare, yet potentially life-threatening adverse reaction. Candidate gene studies involving well-characterized patients with DILI and drug-exposed controls have identified single nucleotide polymorphisms (SNPs) affecting the metabolism and clearance of specific drugs and hence, influencing individual's susceptibility to DILI...
May 21, 2018: Journal of Hepatology
https://www.readbyqxmd.com/read/29792672/biosynthesis-of-lincosamide-antibiotics-reactions-associated-with-degradation-and-detoxification-pathways-play-a-constructive-role
#4
Daozhong Zhang, Zhijun Tang, Wen Liu
Natural products typically are small molecules produced by living organisms. These products possess a wide variety of biological activities and thus have historically played a critical role in medicinal chemistry and chemical biology either as chemotherapeutic agents or as useful tools. Natural products are not synthesized for use by human beings; rather, living organisms produce them in response to various biochemical processes and environmental concerns, both internal and external. These processes/concerns are often dynamic and thus motivate the diversification, optimization, and selection of small molecules in line with changes in biological function...
May 24, 2018: Accounts of Chemical Research
https://www.readbyqxmd.com/read/29792365/protective-effects-of-piceatannol-on-methylglyoxal-induced-cytotoxicity-in-mc3t3-e1-osteoblastic-cells
#5
Kwang Sik Suh, Suk Chon, Eun Mi Choi
Methylglyoxal (MG) is a reactive α-oxoaldehyde that increases under diabetic conditions and subsequently contributes to the complications associated with this disease. Piceatannol is a naturally occurring analogue of resveratrol that possesses multiple biological functions. The present study investigated the effects of piceatannol on MG-induced cytotoxicity in MC3T3-E1 osteoblastic cells. Piceatannol significantly restored MG-induced reductions in cell viability and reduced lactate dehydrogenase release in MG-treated MC3T3-E1 osteoblastic cells, which suggests that it suppressed MG-induced cytotoxicity...
June 2018: Free Radical Research
https://www.readbyqxmd.com/read/29792199/nanoparticle-delivery-of-grape-seed-derived-proanthocyanidins-to-airway-epithelial-cells-dampens-oxidative-stress-and-inflammation
#6
S Castellani, A Trapani, A Spagnoletta, L di Toma, T Magrone, S Di Gioia, D Mandracchia, G Trapani, E Jirillo, M Conese
BACKGROUND: Chronic respiratory diseases, whose one of the hallmarks is oxidative stress, are still incurable and need novel therapeutic tools and pharmaceutical agents. The phenolic compounds contained in grape are endowed with well-recognized anti-oxidant, anti-inflammatory, anti-cancer, and anti-aging activities. Considering that natural anti-oxidants, such as proanthocyanidins, have poor water solubility and oral bioavailability, we have developed a drug delivery system based on solid lipid nanoparticles (SLN), apt to encapsulate grape seed extract (GSE), containing proanthocyanidins...
May 23, 2018: Journal of Translational Medicine
https://www.readbyqxmd.com/read/29791877/enzyme-assisted-extraction-chemical-characteristics-and-immunostimulatory-activity-of-polysaccharides-from-korean-ginseng-panax-ginseng-meyer
#7
Young-Ran Song, Su-Kyung Sung, Mi Jang, Tae-Gyu Lim, Chang-Won Cho, Chun-Ji Han, Hee-Do Hong
In this study, enzyme-assisted extraction was used to isolate functional polysaccharides from Korean ginseng (Panax ginseng Meyer) and the physicochemical and biological properties of the extracted polysaccharides were investigated, comparing with those from traditional hot-water extraction (FGWP). In macrophages, their effects on cytokines production could be ordered as FGEP-CA ≥ FGEP-A > FGEP-C > FGWP, suggesting that FGEP-CA (combined cellulase- and α-amylase-extracted polysaccharide) is a potent immunostimulator...
May 20, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29791876/extraction-and-characterization-of-cashew-tree-anacardium-occidentale-gum-use-in-aceclofenac-dental-pastes
#8
M Saquib Hasnain, Poonam Rishishwar, Sanjay Rishishwar, Sadath Ali, Amit Kumar Nayak
In the current work, the usefulness of extracted cashew tree gum (CG) as pharmaceutical excipient in dental pastes containing AC (for the pain management in the periodontitis) was investigated. CG was extracted from crude exudate of cashew tree (Anacardium occidentale, family: Anacardiaceae) (yield 19.22%). Physicochemical characteristics like colour, odour, taste, solubility, pH and viscosity of extracted CG were estimated; the phytochemical identification tests indicated the presence of carbohydrates and mucilage within it...
May 20, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29791145/slow-starter-enzymes-role-of-active-site-architecture-in-the-catalytic-control-in-the-biosynthesis-of-taxadiene-by-taxadiene-synthase
#9
Tamar Ansbacher, Yehoshua Freud, Dan Thomas Major
Taxadiene synthase (TXS) catalyzes the formation of the natural product Taxa-4(5),11(12)-diene (henceforth Taxadiene). Taxadiene is the precursor in the formation of Taxol, which is an important natural anti-cancer agent. In the current study, we present a detailed mechanistic view of the biosynthesis of Taxadiene by TXS, using a hybrid quantum mechanics-molecular mechanics potential in conjunction with free energy simulation methods. The obtained free energy landscape displays initial endergonic steps followed by a step-wise downhill profile, which is an emerging free energy fingerprint for type I terpene synthases...
May 23, 2018: Biochemistry
https://www.readbyqxmd.com/read/29791083/structure-and-biocatalytic-scope-of-coclaurine-n-methyltransferase
#10
Matthew Bennett, Mark Thompson, Sarah Shepherd, Mark Dunstan, Abigail Herbert, Duncan Smith, Victoria Cronin, Binuraj Menon, Colin Levy, Jason Micklefield
Benzylisoquinoline alkaloids (BIAs) are a structurally diverse family of plant secondary metabolites which have been exploited to develop analgesics, antibiotics, antitumor agents and other therapeutic agents. Biosynthesis of BIAs proceeds via a common pathway from tyrosine to (S)-reticulene at which point the pathway diverges. Coclaurine N-methyltransferase (CNMT) is a key enzyme in the pathway to (S)-reticulene, installing the N-methyl substituent that is essential for the bioactivity of many BIAs. In this paper, we describe the first crystal structure of CNMT which, along with mutagenesis studies, defines the enzymes active site architecture...
May 23, 2018: Angewandte Chemie
https://www.readbyqxmd.com/read/29788962/phenolics-from-barleria-cristata-var-alba-as-carcinogenesis-blockers-against-menadione-cytotoxicity-through-induction-and-protection-of-quinone-reductase
#11
Ali M El-Halawany, Hossam M Abdallah, Ahmed R Hamed, Hany Ezzat Khalil, Ameen M Almohammadi
BACKGROUND: There are increasing interests in natural compounds for cancer chemoprevention. Blocking agents represent an important class of chemopreventive compounds. They prevent carcinogens from undergoing metabolic activation and thereby suppressing their interaction with cellular macromolecular targets. METHODS: The effect of phenolic compounds isolated from Barleria cristata var. alba as chemopreventive agent was evaluated. The ethyl acetate fraction of B. cristata was subjected to different chromatographic techniques for isolation of its major phenolic compounds...
May 22, 2018: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/29788916/in-silico-exploration-of-red-sea-bacillus-genomes-for-natural-product-biosynthetic-gene-clusters
#12
Ghofran Othoum, Salim Bougouffa, Rozaimi Razali, Ameerah Bokhari, Soha Alamoudi, André Antunes, Xin Gao, Robert Hoehndorf, Stefan T Arold, Takashi Gojobori, Heribert Hirt, Ivan Mijakovic, Vladimir B Bajic, Feras F Lafi, Magbubah Essack
BACKGROUND: The increasing spectrum of multidrug-resistant bacteria is a major global public health concern, necessitating discovery of novel antimicrobial agents. Here, members of the genus Bacillus are investigated as a potentially attractive source of novel antibiotics due to their broad spectrum of antimicrobial activities. We specifically focus on a computational analysis of the distinctive biosynthetic potential of Bacillus paralicheniformis strains isolated from the Red Sea, an ecosystem exposed to adverse, highly saline and hot conditions...
May 22, 2018: BMC Genomics
https://www.readbyqxmd.com/read/29788877/contribution-of-nrf2-in-gastrointestinal-protection-from-oxidative-injury
#13
Akinori Yanaka
The human gastrointestinal tract is exposed to a variety of toxic agents, such as Helicobacter pylori (H.pylori), nonsteroidal anti-inflammatory drugs (NSAIDs), gastric acid, enteric pathogenic bacteria, excessive auto immune reactions, and chronic mental stresses. These stressors generate free radicals within the gastrointestinal tissues, causing chronic inflammatory diseases, ulcers, cancers, and functional disturbances. Recent studies have demonstrated that some natural food compounds upregulate the nuclear factor erythroid 2-related factor 2-mediated antioxidant system, ameliorating or preventing these disorders...
May 21, 2018: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/29788873/one-molecule-many-targets-and-numerous-effects-the-pleiotropy-of-curcumin-lies-in-its-chemical-structure
#14
Mahdi Hatamipour, Thomas P Johnston, Amirhossein Sahebkar
Curcumin quite possibly represents one of the most diverse therapeutic agents yet isolated from natural sources. Therapeutic benefits of this extraordinary natural compound have been demonstrated during treatment of a variety of diseases, including cancer, inflammatory processes, immunological disorders, diabetes, and oxidative stress often associated with hyperlipidemia. Due to its unique molecular chemical structure and functional groups, curcumin may bind with and subsequently either inhibit or activate a variety of endogenous biomolecules, including enzymes, receptors, signaling molecules, metals, transcription factors, and even certain proteins located in cell membranes...
May 21, 2018: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/29788869/advances-in-the-tyrosinase-inhibitors-from-plant-source
#15
Marco Bonesi, Jianbo Xiao, Rosa Tundis, Francesca Aiello, Vincenzo Sicari, Monica R Loizzo
Tyrosinase is a multifunctional copper-containing oxidase which catalyses the oxidation of tyrosine to produce melanin. The alteration in melanin biosynthesis occurs in many diseases. The pigment has a protecting role against skin photo-carcinogenesis, but anomalous melanin pigmentation is an aesthetic problem in human beings. Moreover, the formation of neuromelanin in human brain could contribute to the neurodegeneration associated with Parkinson's disease. Finally, tyrosinase is also responsible of undesired browning in fruits and vegetables...
May 21, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29787240/sulfonium-ion-condensation-the-burden-borne-by-sam-synthetase
#16
Charles A Lewis, Richard Wolfenden
S-Adenosylmethionine (SAM+) serves as the prin-cipal methylating agent in biological systems, but the thermodynamic basis of its reactivity does not appear to have been established. Here, we show that methionine, methanol and H+ combine to form S-methylmethionine (SMM+) with a temperature-independent equilibrium constant of 9.9 M-2. The corresponding group transfer potential of SMM+, i. e. its free energy of hydrolysis at pH 7, is -8.2 kcal/mol. The "energy-rich" nature of sulfonium ions is related to the extreme acidity (pKa -5...
May 22, 2018: Biochemistry
https://www.readbyqxmd.com/read/29786840/spray-drying-of-milk-blackberry-pulp-mixture-effect-of-carrier-agent-on-the-physical-properties-of-powder-water-sorption-and-glass-transition-temperature
#17
Matheus Boeira Braga, Sandra Cristina Dos Santos Rocha, Miriam Dupas Hubinger
Spray dryer was used to produce particles from a milk-blackberry pulp mixture (25%:75% (w/w)). Maltodextrin 10DE and 20DE and gum Arabic were used as adjuvants in order to improve powder quality. The particles were analyzed with emphasis on physical and physicochemical characteristics: moisture content, bulk density, particle size, morphology, water activity, anthocyanins retention, anthocyanins content, hygroscopicity, solubility, water sorption, and glass transition temperature. The best results were obtained for the paste composition of 25% concentrated milk-70% blackberry pulp-5% gum Arabic, yielding high anthocyanins retention (>87...
May 22, 2018: Journal of Food Science
https://www.readbyqxmd.com/read/29786651/clinical-efficacy-associated-with-enhanced-antioxidant-enzyme-activities-of-silver-nanoparticles-biosynthesized-using-moringa-oleifera-leaf-extract-against-cutaneous-leishmaniasis-in-a-murine-model-of-leishmania-major
#18
Manal El-Khadragy, Ebtesam M Alolayan, Dina M Metwally, Mohamed F Serag El-Din, Sara S Alobud, Nour I Alsultan, Sarah S Alsaif, Manal A Awad, Ahmed E Abdel Moneim
Leishmaniasis is one of the most significant vector-borne syndromes of individuals. This parasitic infection can be affected by many species of Leishmania, most of which are zoonotic. Natural products have made and are continuing to make important contributions to the search for new antileishmanial agents. The use of plants in the production assembly of silver nanoparticles has drawn attention because of its rapid, eco-friendly, non-pathogenic, economical protocol and provides a single step technique for the biosynthetic process...
May 22, 2018: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/29786070/selective-elimination-of-senescent-cells-by-mitochondrial-targeting-is-regulated-by-ant2
#19
Sona Hubackova, Eliska Davidova, Katerina Rohlenova, Jan Stursa, Lukas Werner, Ladislav Andera, LanFeng Dong, Mikkel G Terp, Zdenek Hodny, Henrik J Ditzel, Jakub Rohlena, Jiri Neuzil
Cellular senescence is a form of cell cycle arrest that limits the proliferative potential of cells, including tumour cells. However, inability of immune cells to subsequently eliminate senescent cells from the organism may lead to tissue damage, inflammation, enhanced carcinogenesis and development of age-related diseases. We found that the anticancer agent mitochondria-targeted tamoxifen (MitoTam), unlike conventional anticancer agents, kills cancer cells without inducing senescence in vitro and in vivo. Surprisingly, it also selectively eliminates both malignant and non-cancerous senescent cells...
May 21, 2018: Cell Death and Differentiation
https://www.readbyqxmd.com/read/29785529/isolation-and-characterization-of-bacillus-sp-gfp-2-a-novel-bacillus-strain-with-antimicrobial-activities-from-whitespotted-bamboo-shark-intestine
#20
Jia Wu, Guoqiang Xu, Yangyang Jin, Cong Sun, Li Zhou, Guodong Lin, Rong Xu, Ling Wei, Hui Fei, Dan Wang, Jianqing Chen, Zhengbing Lv, Kuancheng Liu
The abuse of antibiotics and following rapidly increasing of antibiotic-resistant pathogens is the serious threat to our society. Natural products from microorganism are regarded as the important substitution antimicrobial agents of antibiotics. We isolated a new strain, Bacillus sp. GFP-2, from the Chiloscyllium plagiosum (Whitespotted bamboo shark) intestine, which showed great inhibitory effects on the growth of both Gram-positive and Gram-negative bacteria. Additionally, the growth of salmon was effectively promoted when fed with inactivated strain GFP-2 as the inhibition agent of pathogenic bacteria...
May 22, 2018: AMB Express
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