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https://www.readbyqxmd.com/read/28938642/facile-total-synthesis-of-lysicamine-and-the-anticancer-activities-of-the-ru-ii-rh-iii-mn-ii-and-zn-ii-complexes-of-lysicamine
#1
Jiao-Lan Qin, Ting Meng, Zhen-Feng Chen, Xiao-Li Xie, Qi-Pin Qin, Xiao-Ju He, Ke-Bin Huang, Hong Liang
Lysicamine is a natural oxoaporphine alkaloid, which isolated from traditional Chinese medicine (TCM) herbs and has been shown to possess cytotoxicity to hepatocarcinoma cell lines. Reports on its antitumor activity are scarce because lysicamine occurs in plants at a low content. In this work, we demonstrate a facile concise total synthesis of lysicamine from simple raw materials under mild reaction conditions, and the preparation of the Ru(II), Rh(III), Mn(II) and Zn(II) complexes 1-4 of lysicamine (LY). All the compounds were fully characterized by elemental analysis, IR, ESI-MS, (1)H and (13)C NMR, as well as single-crystal X-ray diffraction analysis...
August 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28938624/addition-of-2-ethylamino-acetonitrile-group-to-nitroxoline-results-in-significantly-improved-anti-tumor-activity-in-vitro-and-in-vivo
#2
Ana Mitrović, Izidor Sosič, Špela Kos, Urša Lampreht Tratar, Barbara Breznik, Simona Kranjc, Bojana Mirković, Stanislav Gobec, Tamara Lah, Gregor Serša, Janko Kos
Lysosomal cysteine peptidase cathepsin B, involved in multiple processes associated with tumor progression, is validated as a target for anti-cancer therapy. Nitroxoline, a known antimicrobial agent, is a potent and selective inhibitor of cathepsin B, hence reducing tumor progression in vitro and in vivo. In order to further improve its anti-cancer properties we developed a number of derivatives using structure-based chemical synthesis. Of these, the 7-aminomethylated derivative (compound 17) exhibited significantly improved kinetic properties over nitroxoline, inhibiting cathepsin B endopeptidase activity selectively...
August 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28938573/iatc-mhyb-a-hybrid-multi-label-classifier-for-predicting-the-classification-of-anatomical-therapeutic-chemicals
#3
Xiang Cheng, Shu-Guang Zhao, Xuan Xiao, Kuo-Chen Chou
Recommended by the World Health Organization (WHO), drug compounds have been classified into 14 main ATC (Anatomical Therapeutic Chemical) classes according to their therapeutic and chemical characteristics. Given an uncharacterized compound, can we develop a computational method to fast identify which ATC class or classes it belongs to? The information thus obtained will timely help adjusting our focus and selection, significantly speeding up the drug development process. But this problem is by no means an easy one since some drug compounds may belong to two or more than two ATC classes...
August 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28938525/toxic-effects-of-tripterygium-wilfordii-hook-f-on-the-reproductive-system-of-adolescent-male-rats
#4
Xiaoping Jing, Weiwei Cheng, Sheng Guo, Ya Zou, Ting Zhang, Li He
Tripterygium wilfordii Hook F. (TWHF) is a compound extracted from Lei Gong Teng (Thunder God Vine) that has been used to treat a variety of immune-related diseases in clinical practice, particularly in pediatrics. Nevertheless, clinical data indicated that glycosides from Tripterygium wilfordii Hook F (GTW) are toxic to the male reproductive system, but the mechanism is unknown. Here, the administration of a high dose of GTW for 4 weeks and a low dose for 12 weeks can reduce the body weights and testes weights in adolescent male rats...
September 18, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28938521/beneficial-health-applications-and-medicinal-values-of-pedicularis-plants-a-review
#5
REVIEW
Mohd Iqbal Yatoo, Umesh Dimri, Arumugam Gopalakrishnan, Kumaragurubaran Karthik, Marappan Gopi, Rekha Khandia, Mani Saminathan, Archana Saxena, Mahmoud Alagawany, Mayada Ragab Farag, Ashok Munjal, Kuldeep Dhama
Pedicularis plants (Orobanchaceae), popularly known as lousewort, are found in Asia, Europe, and North America, and have been used in Sowa-Rigpa, the Himalayan art of healing and a traditional system of medicine for treating various ailments in humans. A comprehensive compilation on this valuable medicinal plant is not available, however. The present extensive review provides insight into the salient medicinal properties of Pedicularis plants with respect to various health issues and diseases. Our previous studies on Pedicularis plants from the Changthang region of Ladakh (India) and research advances leading to new developments in this field have prompted this review...
September 18, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28938517/green-tea-camellia-sinensis-and-l-theanine-medicinal-values-and-beneficial-applications-in-humans-a-comprehensive-review
#6
REVIEW
Muhammad Saeed, Muhammad Naveed, Muhammad Arif, Mohib Ullah Kakar, Robina Manzoor, Mohamed Ezzat Abd El-Hack, Mahmoud Alagawany, Ruchi Tiwari, Rekha Khandia, Ashok Munjal, Kumaragurubaran Karthik, Kuldeep Dhama, Hafiz M N Iqbal, Maryam Dadar, Chao Sun
Green tea (Camellia sinensis) is a famous herb, and its extract has been extensively used in traditional Chinese medicinal system. In this context, several studies have revealed its health benefits and medicinal potentialities for several ailments. With ever increasing scientific knowledge, search for safer, potential and novel type of health-related supplements quest, scientists are re-directing their research interests to explore natural resources i.e. medicinal herbs/plant derived compounds. Green tea consumption has gained a special attention and popularity in the modern era of changing lifestyle...
September 18, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28938514/-2-4-fluorobenzamido-4-methylthiazole-5-carboxylic-acid-a-novel-thiazole-compound-ameliorates-insulin-sensitivity-and-hyperlipidaemia-in-streptozotocin-induced-diabetic-rats-plausible-role-of-inflammatory-and-oxidative-stress-markers
#7
Yam Nath Paudel, Md Rahmat Ali, Mohammad Adil, Sandhya Bawa, Manju Sharma
Emerging evidence suggests that thiazole compounds are of great interest due to their protective effect against DM. Protective effects of thiazole derivatives against hyperglycemia have been demonstrated in earlier in vitro and in vivo studies. Previously, anti-oxidant and free radical scavenging activities of 2-(4-Fluorobenzamido)-4-methylthiazole-5-carboxylicacid, a newly developed thiazole derivative (NDTD), have been well-documented. Current study investigated the pharmacological effect of NDTD on hyperglycaemia, insulin sensitivity, lipid profile, anti-inflammatory and oxidative stress markers in an animal model...
September 18, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28938498/-loudness-optimized-registration-of-compound-action-potential-in-cochlear-implant-recipients
#8
Klaus Berger, Thomas Hocke, Horst Hessel
Background Postoperative measurements of compound action potentials are not always possible due to the insufficient acceptance of the CI-recipients. This study investigated the impact of different parameters on the acceptance of the measurements. Methods Compound action potentials of 16 CI recipients were measured with different pulse-widths. Recipients performed a loudness rating at the potential thresholds with the different sequences. Results Compound action potentials obtained with higher pulse-widths were rated softer than those obtained with smaller pulse-widths...
September 22, 2017: Laryngo- Rhino- Otologie
https://www.readbyqxmd.com/read/28938495/polyphenol-enriched-fractions-of-cyclopia-intermedia-selectively-affect-lipogenesis-and-lipolysis-in-3t3-l1-adipocytes
#9
Babalwa U Jack, Christiaan J Malherbe, Elize L Willenburg, Dalene de Beer, Barbara Huisamen, Elizabeth Joubert, Christo J F Muller, Johan Louw, Carmen Pheiffer
Cyclopia species are increasingly investigated as sources of phenolic compounds with potential as therapeutic agents. Recently, we demonstrated that a crude polyphenol-enriched organic fraction (CPEF) of Cyclopia intermedia, currently forming the bulk of commercial production, decreased lipid content in 3T3-L1 adipocytes and inhibited body weight gain in obese db/db mice. The aim of the present study was to determine whether a more effective product and/or one with higher specificity could be obtained by fractionation of the CPEF by purposely increasing xanthone and benzophenone levels...
September 22, 2017: Planta Medica
https://www.readbyqxmd.com/read/28938494/supercritical-fluid-chromatography-in-natural-product-analysis-an-update
#10
Nora Gibitz Eisath, Sonja Sturm, Hermann Stuppner
The wide chemical diversity of natural products has challenged analysts all over the world and has been a driving force for the development of innovative technologies since decades. In the last years, supercritical fluid chromatography (SFC) has finally emerged from the shadow of liquid chromatography (LC) and gas chromatography (GC) and has become a powerful tool in modern natural product analysis. Whereas in the past the technique had mainly been restricted to a small group of nonpolar compounds, it has largely expanded its suitability in the last years and has demonstrated possibilities without boundaries...
September 22, 2017: Planta Medica
https://www.readbyqxmd.com/read/28938483/varying-susceptibility-of-the-female-mammary-gland-to-in-utero-windows-of-bpa-exposure
#11
Andrea R Hindman, Xiaokui Molly Mo, Hannah L Helber, Claire E Kovalchin, Nanditha Ravichandran, Alina R Murphy, Abigail M Fagan, Pamela M St John, Craig J Burd
In utero exposure to the endocrine disrupting compound bisphenol A (BPA) is known to disrupt mammary gland development and increase tumor susceptibility in rodents. It is unclear if there are different periods of in utero development that may be more susceptible to BPA exposure. Herein, pregnant CD-1 mice were exposed to BPA at different times during gestation that correspond to specific milestones of in utero mammary gland development. Mammary glands of early-life and adult female mice, exposed in utero to BPA, were morphologically and molecularly (ERα and Ki67) evaluated for developmental abnormalities...
August 9, 2017: Endocrinology
https://www.readbyqxmd.com/read/28938444/lack-of-lrp5-signaling-in-osteoblasts-sensitizes-male-mice-to-diet-induced-disturbances-in-glucose-metabolism
#12
Soohyun P Kim, Julie L Frey, Zhu Li, Brian C Goh, Ryan C Riddle
Wnt signaling through the Lrp5 co-receptor regulates osteoblast maturation, matrix mineralization, and intermediary metabolism. In the mature osteoblast, signals downstream of Lrp5 are required for normal long-chain fatty acid β-oxidation and mice rendered deficient for this co-receptor in osteoblasts and osteocytes accumulate body fat with elevated serum lipid levels, but retain normal insulin sensitivity. In this study, we challenged Lrp5 mutant mice with a high fat diet to determine if they are more susceptible to diet-induced disturbances in glucose homeostasis...
September 11, 2017: Endocrinology
https://www.readbyqxmd.com/read/28938224/novel-diphenylthiazole-derivatives-with-multi-target-mechanism-synthesis-docking-study-anticancer-and-anti-inflammatory-activities
#13
Ahmed H Abdelazeem, Mohammed T El-Saadi, Eman G Said, Bahaa G M Youssif, Hany A Omar, Samir M El-Moghazy
Over the last few decades, a growing body of studies addressed the anticancer activity of NSAIDs, particularly selective COX-2 inhibitors. However, their exact molecular mechanism is still unclear and is not fully investigated. In this regard, a novel series of compounds bearing a COXs privilege scaffold, diphenyl thiazole, was synthesized and evaluated for their anticancer activity against a panel of cancer cell lines. The most active compounds 10b, 14a,b, 16a, 17a,b and 18b were evaluated in vitro for COX-1/COX-2 inhibitory activity...
September 12, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28938217/deriving-nitrogen-critical-levels-and-loads-based-on-the-responses-of-acidophytic-lichen-communities-on-boreal-urban-pinus-sylvestris-trunks
#14
Sirkku Manninen
The deposition of reactive nitrogen (N) compounds currently predominates over sulphur (S) deposition in most of the cities in Europe and North America. Acidophytic lichens growing on tree trunks are known to be sensitive to both N and S deposition. Given that tree species and climatic factors affect the composition of epiphytic lichen communities and modify lichen responses to air pollution, this study focused on the impact of urban air pollution on acidophytes growing on boreal conifer trunks. The study was performed in the Helsinki metropolitan area, southern Finland, where annual mean nitrogen dioxide (NO2) concentrations range from 4-5μgm(-3) to >50μgm(-3)...
September 19, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28938203/green-synthesis-biological-and-spectroscopic-study-on-the-interaction-of-multi-component-mannich-bases-of-imidazo-2-1-b-benzothiazoles-with-human-serum-albumin
#15
Swetha K Maddili, Leela Prasad Yandrati, Shakuntala Siddam, Vijaya Kumar Kannekanti, Himabindu Gandham
A series of Mannich bases of imidazo[2, l-b]benzothiazoles were prepared through one-pot multi-component reaction in the presence of water as an eco-friendly solvent. All the synthesized compounds were confirmed from IR, (1)HNMR, (13)CNMR, and Mass spectroscopy. Evaluation of in vitro anti-inflammatory and anti-microbial activities of all the synthesized derivatives was further accomplished. These results clearly displayed that compound 6d exhibited outstanding anti-inflammatory activity with a percentage inhibition of 70...
August 19, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28938177/the-osmotin-of-calotropis-procera-latex-is-not-expressed-in-laticifer-free-cultivated-callus-and-under-salt-stress
#16
Isabel C C Souza, Márcio V Ramos, José H Costa, Cleverson D T Freitas, Raquel S B Oliveira, Frederico B Moreno, Renato A Moreira, Cristina P S Carvalho
The latex of Calotropis procera has previously been reported to contain osmotin. This protein (CpOsm) inhibited phytopathogens and this was mechanistically characterized. Here, the time-course profile of CpOsm transcripts was examined in the salt-stressed cultivated callus of C. procera in order to better understand its role in the physiology of the plant. Stressed callus (80 mM NaCl) showed an unbalanced content of organic compounds (proline and total soluble sugar) and inorganic ions (Na(+), Cl(-), and K(+))...
September 14, 2017: Plant Physiology and Biochemistry: PPB
https://www.readbyqxmd.com/read/28938171/behavior-of-radioactive-cesium-during-incineration-of-radioactively-contaminated-wastes-from-decontamination-activities-in-fukushima
#17
Hiroshi Fujiwara, Hidetoshi Kuramochi, Kazutaka Nomura, Tomoharu Maeseto, Masahiro Osako
Large volumes of decontamination wastes (DW) generated by off-site decontamination activities in Fukushima Prefecture have been incinerated since 2015. The behavior of radioactive cesium during incineration of DW was investigated at a working incineration plant. The incineration discharged bottom ash (BA) and fly ash (FA) with similar levels of radiocesium, and the leachability of the radiocesium from both types of ash was very low (<1%). These results are significantly different from those obtained for the incineration of contaminated municipal solid waste (CMSW) reported in earlier studies...
September 18, 2017: Journal of Environmental Radioactivity
https://www.readbyqxmd.com/read/28938170/aromatic-hydrazones-derived-from-nicotinic-acid-hydrazide-as-fluorimetric-ph-sensing-molecules-structural-analysis-by-computational-and-spectroscopic-methods-in-solid-phase-and-in-solution
#18
T Benković, A Kenđel, J Parlov-Vuković, D Kontrec, V Chiş, S Miljanić, N Galić
Structural analyses of aroylhydrazones were performed by computational and spectroscopic methods (solid state NMR, 1 and 2D NMR spectroscopy, FT-IR (ATR) spectroscopy, Raman spectroscopy, UV-Vis spectrometry and spectrofluorimetry) in solid state and in solution. The studied compounds were N'-(2,3-dihydroxyphenylmethylidene)-3-pyridinecarbohydrazide (1), N'-(2,5-dihydroxyphenylmethylidene)-3-pyridinecarbohydrazide (2), N'-(3-chloro-2-hydroxy-phenylmethylidene)-3-pyridinecarbohydrazide (3), and N'-(2-hydroxy-4-methoxyphenyl-methylidene)-3-pyridinecarbohydrazide (4)...
September 15, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28938159/lunatic-fringe-and-p53-cooperatively-suppress-mesenchymal-stem-like-breast-cancer
#19
Wen-Cheng Chung, Shubing Zhang, Lavanya Challagundla, Yunyun Zhou, Keli Xu
Claudin-low breast cancer (CLBC) is a poor prognosis molecular subtype showing stemness and mesenchymal features. We previously discovered that deletion of a Notch signaling modulator, Lunatic Fringe (Lfng), in the mouse mammary gland induced a subset of tumors resembling CLBC. Here we report that deletion of one copy of p53 on this background not only accelerated mammary tumor development but also led to a complete penetrance of the mesenchymal stem-like phenotype. All mammary tumors examined in the Lfng/p53 compound mutant mice displayed a mesenchymal/spindloid pathology...
September 19, 2017: Neoplasia: An International Journal for Oncology Research
https://www.readbyqxmd.com/read/28938146/the-uncertainty-of-biodegradation-rate-constants-of-emerging-organic-compounds-in-soil-and-groundwater-a-compilation-of-literature-values-for-82-substances
#20
Janek Greskowiak, Enrico Hamann, Victoria Burke, Gudrun Massmann
The present study reports on biodegradation rate constants of emerging organic compounds (EOCs) in soil and groundwater available in the literature. The major aim of this compilation was to provide an assessment of the uncertainty of hydrological models with respect to the fate of EOCs. The literature search identified a total number of 82 EOCs for which 1st-order rate constants could be derived. It was found that for the majority of compounds degradation rate constants vary over more than three orders of magnitude...
September 8, 2017: Water Research
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