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https://www.readbyqxmd.com/read/28340413/design-synthesis-and-biological-evaluation-of-novel-coumarin-based-benzamides-as-potent-histone-deacetylase-inhibitors-and-anticancer-agents
#1
Tooba Abdizadeh, Mohammad Reza Kalani, Khalil Abnous, Zahra Tayarani-Najaran, Bibi Zahra Khashyarmanesh, Rahman Abdizadeh, Razieh Ghodsi, Farzin Hadizadeh
Histone deacetylases (HDACs) are attractive therapeutic targets for the treatment of cancer and other diseases. It has four classes (I-IV), among them especially class I isozyme are involved in promoting tumor cells proliferation, angiogenesis, differentiation, invasion and metastasis and also viable targets for cancer therapeutics. A novel series of coumarin-based benzamides was designed and synthesized as HDAC inhibitors. The cytotoxic activity of the synthesized compounds (8a-u) was evaluated against six human cancer cell lines including HCT116, A2780, MCF7, PC3, HL60 and A549 and a single normal cell line (Huvec)...
March 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28340411/synthesis-and-biological-evaluation-of-novel-chalcone-derivatives-as-a-new-class-of-microtubule-destabilizing-agents
#2
Xiaochao Huang, Rizhen Huang, Lingxue Li, Shaohua Gou, Hengshan Wang
A series of novel chalcone derivatives were designed and synthesized as potential antitumor agents. Structures of target molecules were confirmed by (1)H NMR, (13)C NMR and HR-MS, and evaluated for their in vitro anti-proliferative activities using MTT assay. Among them, compound 12k displayed potent activity against the test tumor cell lines including multidrug resistant human cancer lines, with the IC50 values ranged from 3.75 to 8.42 μM. In addition, compound 12k was found to induce apoptosis in NCI-H460 cells via the mitochondrial pathway, including an increase of the ROS level, loss of mitochondrial membrane potential, release of cytochrome c, down-regulation of Bcl-2, up-regulation of Bax, activation of caspase-9 and caspase-3, respectively...
March 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28340377/possible-protective-effect-of-royal-jelly-against-cyclophosphamide-induced-prostatic-damage-in-male-albino-rats-a-biochemical-histological-and-immuno-histo-chemical-study
#3
Sara Mohammed Naguib Abdel-Hafez, Rehab Ahmed Rifaai, Walaa Yehia Abdelzaher
Almost all the chemotherapy treat many cancer types effectively, but it leads to severe side effects. Chemotherapy like cyclophosphamide (CP) not works only on the active cells, such as cancer cells, but also acts on the healthy cells. Royal jelly (RJ) was reported to have a lot of therapeutic effects besides being an anti-oxidant and anti-cancer agent. The purpose of this study was to assess the possible protective role of RJ in ameliorating the toxic effects of CP overdose in the rat prostatic tissue. The rats were separated into 4 groups; control group, RJ group, CP group and RJ with CP group...
March 21, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28339315/identification-of-asymptomatic-prosthetic-joint-infection-microbiologic-and-operative-treatment-outcomes
#4
Przemysław L Bereza, Alicja Ekiel, Aleksandra Auguściak-Duma, Małgorzata Aptekorz, Iwona Wilk, Piotr Wojciechowski, Damian J Kusz, Gayane Martirosian
BACKGROUND: This prospective study investigated the role of mechanical and biological factors in aseptic implant loosening or presumed silent prosthetic joint infection (PJI). METHODS: Thirty-seven patients were investigated. Microbiologic and molecular methods were used to detect bacteria on the surface of the failed implants removed during revision arthroplasty. Histopathologic analysis was performed. The influence of body mass index (BMI) and various co-morbidities on implant failure also was determined...
March 24, 2017: Surgical Infections
https://www.readbyqxmd.com/read/28334654/synthesis-and-biological-evaluation-of-a-new-series-of-benzimidazole-derivatives-as-antimicrobial-antiquorum-sensing-and-antitumor-agents
#5
N S El-Gohary, M I Shaaban
New benzimidazole derivatives were synthesized and assessed for antimicrobial efficacy toward Escherichia coli, Bacillus cereus, Staphylococcus aureus, Candida albicans and Aspergillus fumigatus 293. Results indicated that compounds 3c and 3n have promising activity toward S. aureus, whereas 3i exhibited remarkable efficacy toward B. cereus. Moreover, compound 3c was proved to be the most active antifungal analog toward C. albicans. On the other hand, 3n displayed the highest activity against A. fumigatus 293...
March 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28334528/why-prodrugs-and-propesticides-succeed
#6
John E Casida
What are the advantages of bioactivation in optimizing drugs and pesticides? Why are there so many prodrugs and propesticides? These questions are examined here by considering compounds selected on the basis of economic value or market success. The 100 major drugs and 90 major pesticides are divided into ones acting directly and those definitely or possibly requiring bioactivation. Established or candidate prodrugs accounted for 19% of the total drug sales with corresponding values of 20, 37 and 17% for proinsecticides, proherbicides and profungicides...
March 23, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28334233/does-long-term-feeding-on-alternative-prey-affect-the-biological-performance-of-neoseiulus-barkeri-acari-phytoseiidae-on-the-target-spider-mites
#7
Ya-Ying Li, Guo-Hao Zhang, Chuan-Bei Tian, Ming-Xiu Liu, Yi-Qing Liu, Huai Liu, Jin-Jun Wang
The predatory mite Neoseiulus barkeri (Hughes) is a good biological control agent for many small sucking pests. We aimed to determine whether rearing long term on alternative prey versus target prey species affected the performance of N. barkeri. Therefore, we investigated the prey preference, life tables, and population parameters of N. barkeri between alternative prey Tyrophagus putrescentiae (Schrank) and three species of spider mites, Tetranychus urticae Koch, Panonychus citri (McGregor), and Eotetranychus kankitus Ehara...
March 3, 2017: Journal of Economic Entomology
https://www.readbyqxmd.com/read/28334172/evaluation-of-neoseiulus-barkeri-acari-phytoseiidae-for-control-of-eotetranychus-kankitus-acari-tetranychidae
#8
Ya-Ying Li, Ming-Xiu Liu, Hai-Wei Zhou, Chuan-Bei Tian, Guo-Hao Zhang, Yi-Qing Liu, Huai Liu, Jin-Jun Wang
Eotetranychus kankitus Ehara (Acari: Tetranychidae) is an important pest in Chinese citrus orchards. In the present study, we aimed to evaluate the potential of Neoseiulus barkeri (Hughes) (Acari: Phytoseiidae) for the biological control of E. kankitus. A two-sex life table of E. kankitus and N. barkeri was constructed to estimate development and fecundity. The functional response and stage-specific predation rate were analyzed to evaluate predation capacity. In addition, a timing model was used to project populations of E...
March 3, 2017: Journal of Economic Entomology
https://www.readbyqxmd.com/read/28334137/geographic-variation-of-diapause-induction-rates-in-trichogramma-drendrolimi-hymenoptera-trichogrammatidae-in-china
#9
Jun-Jie Zhang, Nicolas Desneux, Giovanni Benelli, Lian-Sheng Zang, Wen-Mei Du, Chang-Chun Ruan
Diapause variation is a key factor affecting the development and success of parasitoids employed as biological control agents. Trichogramma dendrolimi Matsumura is mass-reared for biocontrol purposes in several countries around the world. Here we investigated the rate of diapause induction in three populations of T. dendrolimi from different regions in China: Heilongjiang (44° 55' N, 128° 26' E; HLJ), Liaoning (40° 18' N, 123° 22' E; LN), and Jiangsu province (32° 30' N, 120° 09' E; JS). We measured the rates of diapause induction for populations from each region when exposed to temperatures of 8, 10, 12, and 14 °C, for periods ranging from 5 to 35 d...
February 19, 2017: Journal of Economic Entomology
https://www.readbyqxmd.com/read/28334130/effective-biological-control-depends-on-life-history-strategies-of-both-parasitoid-and-its-host-evidence-from-aphidius-colemani-myzus-persicae-system
#10
Diwas Khatri, Xiong Z He, Qiao Wang
Mechanisms behind the success and failure of aphid biological control using parasitoids are largely unknown, probably because of the lack of knowledge of life history strategies of the insects involved. Here, we measured and compared life history strategies of Myzus persicae (Sulzer) (Hemiptera: Aphididae) and its parasitoid Aphidius colemani (Viereck) (Hymenoptera: Aphidiidae), providing essential information for evaluation of the potential of A. colemani to control M. persicae. Our results show that one A...
February 19, 2017: Journal of Economic Entomology
https://www.readbyqxmd.com/read/28333443/systematic-investigation-of-ginkgo-biloba-leaves-for-treating-cardio-cerebrovascular-diseases-in-an-animal-model
#11
Yinfeng Yang, Yan Li, Jinghui Wang, Ke Sun, Weiyang Tao, Zhenzhong Wang, Wei Xiao, Yanqiu Pan, Shuwei Zhang, Yonghua Wang
Globally, cardio-cerebrovascular diseases (CCVDs) account for the leading cause of death, and thus the development of novel strategies for preventing and treating such diseases is in urgent need. Traditional Chinese Medicine (TCM), used for thousands of years in Asia and other regions, have been proven effective in certain disorders. As a medicinal herb for a long time in TCM, Ginkgo Biloba Leaves (GBLs), have been widely used to treat various diseases including CCVDs. However, the underlying molecular mechanisms of medicinal herb in treating these diseases are still unclear...
March 23, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28333111/solanesol-biosynthesis-in-plants
#12
REVIEW
Ning Yan, Yanhua Liu, Hongbo Zhang, Yongmei Du, Xinmin Liu, Zhongfeng Zhang
Solanesol is a non-cyclic terpene alcohol composed of nine isoprene units that mainly accumulates in solanaceous plants. Solanesol plays an important role in the interactions between plants and environmental factors such as pathogen infections and moderate-to-high temperatures. Additionally, it is a key intermediate for the pharmaceutical synthesis of ubiquinone-based drugs such as coenzyme Q10 and vitamin K2, and anti-cancer agent synergizers such as N-solanesyl-N,N'-bis(3,4-dimethoxybenzyl) ethylenediamine (SDB)...
March 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28333108/the-biology-of-pichia-membranifaciens-killer-toxins
#13
REVIEW
Ignacio Belda, Javier Ruiz, Alejandro Alonso, Domingo Marquina, Antonio Santos
The killer phenomenon is defined as the ability of some yeast to secrete toxins that are lethal to other sensitive yeasts and filamentous fungi. Since the discovery of strains of Saccharomyces cerevisiae capable of secreting killer toxins, much information has been gained regarding killer toxins and this fact has substantially contributed knowledge on fundamental aspects of cell biology and yeast genetics. The killer phenomenon has been studied in Pichia membranifaciens for several years, during which two toxins have been described...
March 23, 2017: Toxins
https://www.readbyqxmd.com/read/28333031/new-approaches-regarding-the-in-vitro-maturation-of-oocytes-manipulating-cyclic-nucleotides-and-their-partners-in-crime
#14
REVIEW
Ramon Cesar Botigelli, Eduardo Montanari Razza, Elisa Mariano Pioltine, Marcelo Fábio Gouveia Nogueira
Several discoveries have been described recently (5-10 years) about the biology of ovarian follicles (oocyte, cumulus cells and granulosa cells), including new aspects of cellular communication, the control of oocyte maturation and the acquisition of oocyte competence for fertilization and further embryo development. These advances are nourishing assisted reproduction techniques (ART) with new possibilities, in which novel culture systems are being developed and tested to improve embryo yield and quality. This mini-review aims to describe how the recent knowledge on the physiological aspects of mammalian oocyte is reflecting as original or revisited approaches into the context of embryo production...
February 1, 2017: JBRA Assisted Reproduction
https://www.readbyqxmd.com/read/28332573/discovery-of-multi-target-receptor-tyrosine-kinase-inhibitors-as-novel-anti-angiogenesis-agents
#15
Jinfeng Wang, Lin Zhang, Xiaoyan Pan, Bingling Dai, Ying Sun, Chuansheng Li, Jie Zhang
Recently, we have identified a biphenyl-aryl urea incorporated with salicylaldoxime (BPS-7) as an anti-angiogenesis agent. Herein, we disclosed a series of novel anti-angiogenesis agents with BPS-7 as lead compound through combining diarylureas with N-pyridin-2-ylcyclopropane carboxamide. Several title compounds exhibited simultaneous inhibition effects against three pro-angiogenic RTKs (VEGFR-2, TIE-2 and EphB4). Some of them displayed potent anti-proliferative activity against human vascular endothelial cell (EA...
March 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28332352/development-of-inhibitors-targeting-hypoxia-inducible-factor-1-and-2-for-cancer-therapy
#16
REVIEW
Tianchi Yu, Bo Tang, Xueying Sun
Hypoxia is frequently observed in solid tumors and also one of the major obstacles for effective cancer therapies. Cancer cells take advantage of their ability to adapt hypoxia to initiate a special transcriptional program that renders them more aggressive biological behaviors. Hypoxia-inducible factors (HIFs) are the key factors that control hypoxia-inducible pathways by regulating the expression of a vast array of genes involved in cancer progression and treatment resistance. HIFs, mainly HIF-1 and -2, have become potential targets for developing novel cancer therapeutics...
May 2017: Yonsei Medical Journal
https://www.readbyqxmd.com/read/28331913/biological-properties-and-chemical-composition-of-jatropha-neopauciflora-pax
#17
A B Hernández-Hernández, F J Alarcón-Aguilar, M Jiménez-Estrada, L B Hernández-Portilla, C M Flores-Ortiz, M A Rodríguez-Monroy, M Canales-Martínez
BACKGROUND: Ethnopharmacological relevance. Jatropha neopauciflora (Pax) is an endemic species of the Tehuacan- Cuicatlan Valley, Mexico. This species has long been used as a remedy to alleviate illnesses of bacterial, fungal and viral origin. Aim of the study. Experimentally test the traditional use of Jatropha neopauciflora in Mexican traditional medicine. MATERIALS AND METHODS: The methanol extract (MeOH1), of Jatropha neopauciflora (Euphorbiaceae) was obtained by maceration...
2017: African Journal of Traditional, Complementary, and Alternative Medicines: AJTCAM
https://www.readbyqxmd.com/read/28331368/new-developments-in-the-management-of-waldenstr%C3%A3-m-macroglobulinemia
#18
REVIEW
Jithma P Abeykoon, Uday Yanamandra, Prashant Kapoor
Waldenström macroglobulinemia (WM) is a rare, immunoglobulin M -associated lymphoplasmacytic lymphoma. With the recent discoveries of CXCR warts, hypogammaglobulinemia, infections, and myelokathexis (WHIM) and MYD88 mutations, our understanding of the biology of WM has expanded substantially. While WM still remains incurable, the field is rapidly evolving, and a number of promising agents with significant activity in this malignancy are being evaluated currently. In this review, we discuss the new developments that have occurred in WM over the past 15 years, with a focus on the role of ibrutinib, an oral Bruton's tyrosine kinase inhibitor that has recently been approved for WM in the United States, Europe, and Canada...
2017: Cancer Management and Research
https://www.readbyqxmd.com/read/28331294/spotlight-on-blisibimod-and-its-potential-in-the-treatment-of-systemic-lupus-erythematosus-evidence-to-date
#19
REVIEW
Aleksander Lenert, Timothy B Niewold, Petar Lenert
B cells in general and BAFF (B cell activating factor of the tumor necrosis factor [TNF] family) in particular have been primary targets of recent clinical trials in systemic lupus erythematosus (SLE). In 2011, belimumab, a monoclonal antibody against BAFF, became the first biologic agent approved for the treatment of SLE. Follow-up studies have shown excellent long-term safety and tolerability of belimumab. In this review, we critically analyze blisibimod, a novel BAFF-neutralizing agent. In contrast to belimumab that only blocks soluble BAFF trimer but not soluble 60-mer or membrane BAFF, blisibimod blocks with high affinity all three forms of BAFF...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28331122/an-autopsy-case-report-of-adult-t-cell-leukemia-accompanied-by-rheumatoid-arthritis-mimicking-diffuse-panbronchiolitis
#20
Tomoko Shiraishi, Hiroshi Ishimoto, Kentaro Akata, Toshinori Kawanami, Kazuhiro Yatera, Hiroshi Mukae
A 50-year-old female with a history of chronic sinusitis and rheumatoid arthritis visited our department with repetitive lower respiratory tract infections of Pseudomonas aeruginosa. Her chest CT showed diffuse panbronchiolitis-like pulmonary lesions, her blood examination revealed atypical lymphocytes, and she was serologically positive for anti-human T-lymphotrophic virus type 1 (HTLV-1) antibody. Her rheumatoid arthritis had been well-controlled after biological agent treatment followed by anti-inflammatory analgesic treatment...
2017: Journal of UOEH
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