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https://www.readbyqxmd.com/read/28545259/identification-of-diacetonamine-from-soybean-curd-residue-as-a-sporulation-inducing-factor-toward-bacillus-spp
#1
Aki Ikeda, Dongyeop Kim, Yasuyuki Hashidoko
Under bioassay-guided investigation, a sporulation-inducing factor (SIF) toward Bacillus spp. was searched for in methanol (MeOH) extracts of soybean curd residues, and diacetonamine (1) was identified as the active compound. SIF was first isolated as a monoacetylated derivative (2, 4.1 mg from 655 g soybean curd residues), and its chemical structure was elucidated by field desorption mass spectrometry, electron ionization mass spectrometry, and nuclear magnetic resonance (NMR) analyses. After 48-h incubation, 40 µM diacetonamine hydrochloride (1b) exhibited sporulation-inducing activity with 35% sporulation frequency toward a Bacillus amyloliquefaciens wild-type strain (AHU 2170), whereas 40 µM diacetone acrylamide (3) showed 99% sporulation induction, which was much higher than that of 1b...
December 2017: AMB Express
https://www.readbyqxmd.com/read/28545257/the-reactive-sulfur-species-concept-15-years-on
#2
REVIEW
Gregory I Giles, Muhammad Jawad Nasim, Wesam Ali, Claus Jacob
Fifteen years ago, in 2001, the concept of "Reactive Sulfur Species" or RSS was advocated as a working hypothesis. Since then various organic as well as inorganic RSS have attracted considerable interest and stimulated many new and often unexpected avenues in research and product development. During this time, it has become apparent that molecules with sulfur-containing functional groups are not just the passive "victims" of oxidative stress or simple conveyors of signals in cells, but can also be stressors in their own right, with pivotal roles in cellular function and homeostasis...
May 23, 2017: Antioxidants (Basel, Switzerland)
https://www.readbyqxmd.com/read/28545253/encapsulation-of-the-antioxidant-r-%C3%AE-lipoic-acid-in-permethylated-%C3%AE-and-%C3%AE-cyclodextrins-thermal-and-x-ray-structural-characterization-of-the-1-1-inclusion-complexes
#3
Mino R Caira, Susan A Bourne, Buntubonke Mzondo
The naturally occurring compound α-lipoic acid (ALA) is implicated in manifold critical biological roles and its potent antioxidant properties and potential for treatment of various diseases have led to its widespread use as a dietary supplement. However, shortcomings of poor aqueous solubility and low thermal stability have hampered its development as a medicinal agent, prompting the use of cyclodextrins (CDs) to address these problems. The paucity of published structural data on the nature of the interactions between ALA and CDs motivated the present study, which describes the synthesis and X-ray structural elucidation of crystalline inclusion complexes between the biologically relevant R-(+)-α-lipoic acid (RALA) and the host molecules permethylated α-CD (TMA) and permethylated β-CD (TMB)...
May 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28545227/potential-use-of-chemoprotectants-against-the-toxic-effects-of-cyanotoxins-a-review
#4
REVIEW
Remedios Guzmán-Guillén, María Puerto, Daniel Gutiérrez-Praena, Ana I Prieto, Silvia Pichardo, Ángeles Jos, Alexandre Campos, Vitor Vasconcelos, Ana M Cameán
Cyanobacterial toxins, particularly microcystins (MCs) and cylindrospermopsin (CYN), are responsible for toxic effects in humans and wildlife. In order to counteract or prevent their toxicity, various strategies have been followed, such as the potential application of chemoprotectants. A review of the main substances evaluated for this aim, as well as the doses and their influence on cyanotoxin-induced toxicity, has been performed. A search of the literature shows that research on MCs is much more abundant than research on CYN...
May 23, 2017: Toxins
https://www.readbyqxmd.com/read/28545212/determination-of-phenolic-organohalogens-in-human-serum-from-a-belgian-population-and-assessment-of-parameters-affecting-the-human-contamination
#5
Patrice Dufour, Catherine Pirard, Corinne Charlier
Many in vitro or in vivo studies highlighted the potential deleterious effects of phenolic organohalogenated compounds (POHs) on the health, particularly on the thyroid system homeostasis, however few large scale human epidemiological studies have been carried out, especially in Europe. Further studies monitoring the human contamination by POHs, the sources of exposure and the influence of these compounds on thyroid health are still needed. Therefore we determined the concentrations of 16 POHs (pentachlorophenol (PCP), tetrabromobisphenol A (TBBPA), 4 bromophenols (BPs), 3 hydroxy-polybromodiphenylethers (OH-PBDEs) and 7 hydroxy-polychlorobiphenyls (OH-PCBs)) in serum from 274 people aged from 18 to 76years old living in Liege (Belgium) and the surrounding area...
May 20, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28545188/clinacanthus-nutans-hexane-extracts-induce-apoptosis-through-a-caspase-dependent-pathway-in-human-cancer-cell-lines
#6
Pei Ying Ng, Soi Moi Chye, Chew Hee Ng, Rhun Yian Koh, Yee Lian Tiong, Liew Phing Pui, Yong Hui Tan, Crystale Siew Ying Lim, Khuen Yen Ng
Background: Clinacanthus nutans (C.nutans) is a plant consumed as a cancer treatment in tropical Asia. Despite the availability of numerous anecdotal reports, evaluation of active anticancer effects has remained elusive. Therefore we here examined antiproliferative, reactive oxygen species (ROS)-inducing and apoptosis mechanisms of whole plant extracts in different cancer cell lines. Methods: Antiproliferative actions of five solvent extracts (hexane, chloroform, ethyl acetate, methanol and water) of C.nutans were tested on non-small cell lung cancer (A549), nasopharygeal cancer (CNE1) and liver cancer (HepG2) cells using MTT assay...
April 1, 2017: Asian Pacific Journal of Cancer Prevention: APJCP
https://www.readbyqxmd.com/read/28545183/therapeutic-potential-of-novel-nano-based-curcumin-compounds-in-vitro-and-in-vivo
#7
Homa Mollaei, Esmaeil Babaei
Despite recent advances in cancer medication, malignant tumors continue to be the second leading cause of death worldwide. Furthermore, introducing a therapeutic compound with low-side effects as well as low-price for consumers is controversial. Recent efforts have been focusing on traditional medicines as a rich source of herbal agents. Curcumin, the major turmeric phytochemical, has been widely assessed as an anti-cancer compound in vitro and in vivo. However, the use of curcumin in cancer treatment has limitations because of its low solubility, poor tissue absorption, rapid metabolism and rapid systemic elimination...
April 1, 2017: Asian Pacific Journal of Cancer Prevention: APJCP
https://www.readbyqxmd.com/read/28545167/synthesis-of-s-2-s-3-4-chlorophenyl-n-4-chlorophenyl-sulfonyl-4-phenyl-4-5-dihydro-1h-pyrazole-1-carboximidamido-3-methyl-d3-butanamide-d5-octa-deuterated-jd5037
#8
Malliga R Iyer, Resat Cinar, Nathan J Coffey, Robert J Chorvat, George Kunos
JD5037 (1) is a potent and selective, peripherally acting inverse agonist of the cannabinoid (CB1 R) receptor. Peripheral CB1 receptor antagonists/inverse agonists have great potential in the treatment of metabolic disorders like type 2 diabetes, obesity and NASH. We report the synthesis of octa-deuterated [(2) H8 ]-JD5037 (S, S) (8) along with its (S, R) diastereomer (13) from commercially available L-valine-d8 starting material. The [(2) H8 ]-JD5037 compound will be used to quantitate unlabeled JD5037 during clinical ADME studies and will be used as an LC-MS/MS bioanalytical standard...
May 25, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28545035/novel-ppar%C3%AE-agonist-mhy553-alleviates-hepatic-steatosis-by-increasing-fatty-acid-oxidation-and-decreasing-inflammation-during-aging
#9
Seong Min Kim, Bonggi Lee, Hye Jin An, Dae Hyun Kim, Kyung Chul Park, Sang-Gyun Noh, Ki Wung Chung, Eun Kyeong Lee, Kyung Mok Kim, Do Hyun Kim, Su Jeong Kim, Pusoon Chun, Ho Jeong Lee, Hyung Ryong Moon, Hae Young Chung
Hepatic steatosis is frequently observed in obese and aged individuals. Because hepatic steatosis is closely associated with metabolic syndromes, including insulin resistance, dyslipidemia, and inflammation, numerous efforts have been made to develop compounds that ameliorate it. Here, a novel peroxisome proliferator-activated receptor (PPAR) α agonist, 4-(benzo[d]thiazol-2-yl)benzene-1,3-diol (MHY553) was developed, and investigated its beneficial effects on hepatic steatosis using young and old Sprague-Dawley rats and HepG2 cells...
May 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/28545034/characterization-of-sudan-ebolavirus-infection-in-ferrets
#10
Andrea Kroeker, Shihua He, Marc-Antoine de La Vega, Gary Wong, Carissa Embury-Hyatt, Xiangguo Qiu
Sudan virus (SUDV) outbreaks in Africa are highly lethal; however, the development and testing of novel antivirals and vaccines for this virus has been limited by a lack of suitable animal models. Non-human primates (NHP) remain the gold standard for modeling filovirus disease, but they are not conducive to screening large numbers of experimental compounds and should only be used to test the most promising candidates. Therefore, other smaller animal models are a valuable asset. We have recently developed a guinea-pig adapted SUDV virus that is lethal in guinea pigs...
May 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/28545002/pd169316-a-specific-p38-inhibitor-shows-antiviral-activity-against-enterovirus71
#11
Zhe Zhang, Busen Wang, Shipo Wu, Yanbo Wen, Xinyi Wang, Xiaohong Song, Jinlong Zhang, Lihua Hou, Wei Chen
Enterovirus71 (EV71) is the major causative agent of hand, foot and mouth disease, which threatens the health of infants and young children. The expression of inflammatory cytokines induced by this viral infection aggravate the illness. Here, we describe the anti-EV71 activity of a specific p38 inhibitor that regulates the p38-MAPK signaling pathway. PD169316 was specifically selected from a MAPK compound library due to its significant inhibitory effect on EV71 replication. PD169316 also reduced EV71-induced apoptosis...
May 22, 2017: Virology
https://www.readbyqxmd.com/read/28545000/occurrence-and-effects-of-plastic-additives-on-marine-environments-and-organisms-a-review
#12
REVIEW
Ludovic Hermabessiere, Alexandre Dehaut, Ika Paul-Pont, Camille Lacroix, Ronan Jezequel, Philippe Soudant, Guillaume Duflos
Plastics debris, especially microplastics, have been found worldwide in all marine compartments. Much research has been carried out on adsorbed pollutants on plastic pieces and hydrophobic organic compounds (HOC) associated with microplastics. However, only a few studies have focused on plastic additives. These chemicals are incorporated into plastics from which they can leach out as most of them are not chemically bound. As a consequence of plastic accumulation and fragmentation in oceans, plastic additives could represent an increasing ecotoxicological risk for marine organisms...
May 16, 2017: Chemosphere
https://www.readbyqxmd.com/read/28544982/an-evaluation-of-minor-groove-binders-as-anti-fungal-and-anti-mycobacterial-therapeutics
#13
Fraser J Scott, Ryan J O Nichol, Abedawn I Khalaf, Federica Giordani, Kirsten Gillingwater, Soumya Ramu, Alysha Elliott, Johannes Zuegg, Paula Duffy, Michael-Jon Rosslee, Lerato Hlaka, Santosh Kumar, Mumin Ozturk, Frank Brombacher, Michael Barrett, Reto Guler, Colin J Suckling
This study details the synthesis and biological evaluation of a collection of 19 structurally related Minor Groove Binders (MGBs), derived from the natural product distamycin, which were designed to probe antifungal and antimycobacterial activity. From this initial set, we report several MGBs that are worth more detailed investigation and optimisation. MGB-4, MGB-317 and MGB-325 have promising MIC80s of 2, 4 and 0.25 μg/mL, respectively, against the fungus C. neoformans.MGB-353 and MGB-354 have MIC99s of 3...
May 17, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28544981/synthesis-and-in%C3%A2-vitro-evaluation-of-new-fluorinated-quinoline-derivatives-with-high-affinity-for-pde5-towards-the-development-of-new-pet-neuroimaging-probes
#14
Jianrong Liu, Aurélie Maisonial-Besset, Barbara Wenzel, Damien Canitrot, Ariane Baufond, Jean-Michel Chezal, Peter Brust, Emmanuel Moreau
The increasing incidence of Alzheimer's disease (AD) worldwide is a major public health problem. Current treatments provide only palliative solutions with significant side effects. Therefore, new efficient treatment options and novel early diagnosis tools are urgently needed. Recently, strong pre-clinical evidences suggested that phosphodiesterase 5 (PDE5) may be clinically relevant both as biomarker and drug-target in AD. In this study, we intended to develop a new radiofluorinated tracer for the visualisation of PDE5 in brain using PET imaging...
April 19, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28544967/novel-glycosylated-mycosporine-like-amino-acid-13-o-%C3%AE-galactosyl-porphyra-334-from-the-edible-cyanobacterium-nostoc-sphaericum-protective-activity-on-human-keratinocytes-from-uv-light
#15
Kenji Ishihara, Ryuichi Watanabe, Hajime Uchida, Toshiyuki Suzuki, Michiaki Yamashita, Hiroyuki Takenaka, Ehsan Nazifi, Seiichi Matsugo, Minami Yamaba, Toshio Sakamoto
A UV-absorbing compound was purified and identified as a novel glycosylated mycosporine-like amino acid (MAA), 13-O-β-galactosyl-porphyra-334 (β-Gal-P334) from the edible cyanobacterium Nostoc sphaericum, known as "ge xian mi" in China and "cushuro" in Peru. Occurrence of the hexosylated derivative of shinorine (hexosyl-shinorine) was also supported by LC-MS/MS analysis. β-Gal-P334 accounted for about 86.5% of total MAA in N. sphaericum, followed by hexosyl-shinorine (13.2%) and porphyra-334 (0.2%). β-Gal-P334 had an absorption maximum at 334nm and molecular absorption coefficient was 46,700 at 334nm...
May 15, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28544898/aerosol-and-snow-transfer-processes-an-investigation-on-the-behavior-of-water-soluble-organic-compounds-and-ionic-species
#16
Elena Barbaro, Roberta Zangrando, Sara Padoan, Ornela Karroca, Giuseppa Toscano, Warren R L Cairns, Carlo Barbante, Andrea Gambaro
The concentrations of water-soluble compounds (ions, carboxylic acids, amino acids, sugars, phenolic compounds) in aerosol and snow have been determined at the coastal Italian base "Mario Zucchelli" (Antarctica) during the 2014-2015 austral summer. The main aim of this research was to investigate the air-snow transfer processes of a number of classes of chemical compounds and investigate their potential as tracers for specific sources. The composition and particle size distribution of Antarctic aerosol was measured, and water-soluble compounds accounted for 66% of the PM10 total mass concentration...
May 17, 2017: Chemosphere
https://www.readbyqxmd.com/read/28544873/3d-qsar-studies-of-some-reversible-acetyl-cholinesterase-inhibitors-based-on-comfa-and-ligand-protein-interaction-fingerprints-using-pc-ls-svm-and-pls-ls-svm
#17
Hamidreza Ghafouri, Mohsen Ranjbar, Amirhossein Sakhteman
A great challenge in medicinal chemistry is to develop different methods for structural design based on the pattern of the previously synthesized compounds. In this study two different QSAR methods were established and compared for a series of piperidine acetylcholinesterase inhibitors. In one novel approach, PC-LS-SVM and PLS-LS-SVM was used for modeling 3D interaction descriptors, and in the other method the same nonlinear techniques were used to build QSAR equations based on field descriptors. Different validation methods were used to evaluate the models and the results revealed the more applicability and predictive ability of the model generated by field descriptors (Q(2)LOO-CV=1, R(2)ext=0...
May 10, 2017: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/28544816/analytical-characterization-of-three-cathinone-derivatives-4-mpd-4%C3%A2-f-php-and-bk-epdp-purchased-as-bulk-powder-from-online-vendors
#18
Orapan Apirakkan, Anca Frinculescu, Trevor Shine, Mark C Parkin, Agostino Cilibrizzi, Nunzianda Frascione, Vincenzo Abbate
Novel emerging drugs of abuse, also referred as new psychoactive substances (NPS), constitute an ever-changing mixture of chemical compounds designed to circumvent legislative controls by means of chemical modifications of previously banned recreational drugs. One of such class, synthetic cathinones, namely β-keto derivatives of amphetamines, has been largely abused over the past decade. A number of new synthetic cathinones are detected each year, either in bulk powders/crystals or in biological matrices. It is therefore important to continuously monitor the supply of new synthetic derivatives and promptly report them...
May 23, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28544784/presynaptic-congenital-myasthenic-syndrome-with-a-homozygous-sequence-variant-in-lama5-combines-myopia-facial-tics-and-failure-of-neuromuscular-transmission
#19
Ricardo A Maselli, Juan Arredondo, Jessica Vázquez, Jessica X Chong, Michael J Bamshad, Deborah A Nickerson, Marian Lara, Fiona Ng, Victoria L Lo, Peter Pytel, Craig M McDonald
Defects in genes encoding the isoforms of the laminin alpha subunit have been linked to various phenotypic manifestations, including brain malformations, muscular dystrophy, ocular defects, cardiomyopathy, and skin abnormalities. We report here a severe defect of neuromuscular transmission in a consanguineous patient with a homozygous variant in the laminin alpha-5 subunit gene (LAMA5). The variant c.8046C>T (p.Arg2659Trp) is rare and has a predicted deleterious effect. The affected individual, who also carries a rare homozygous sequence variant in LAMA1, had muscle weakness, myopia, and facial tics...
May 25, 2017: American Journal of Medical Genetics. Part A
https://www.readbyqxmd.com/read/28544762/the-effect-of-a-tooth-tongue-gel-and-mouthwash-regimen-on-morning-oral-malodour-a-3-week-single-blind-randomized-clinical-trial
#20
E Van der Sluijs, G A Van der Weijden, N L Hennequin-Hoenderdos, D E Slot
AIM: To compare the effects of a regimen consisting of a tooth/tongue gel, tongue cleaner and mouthwash with the effects of using standard fluoride dentifrice on the organoleptic oral malodour score (ORG) and volatile sulphur compounds (VSCs). MATERIALS AND METHODS: A total, 66 non-dental students participated in a 3-week parallel, single-blind, randomized, controlled clinical trial. The test group used a tongue cleaner, a tooth/tongue gel and mouthwash containing amine fluoride/stannous fluoride and zinc lactate as oral malodour counteractive...
May 24, 2017: International Journal of Dental Hygiene
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