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https://www.readbyqxmd.com/read/28544428/design-synthesis-and-evaluation-of-the-anti-cancer-activity-of-2-amino-aryl-7-aryl-benzoxazole-compounds
#1
Patcharaporn Khajondetchairit, Oraphan Phuangsawai, Praphasri Suphakun, Siriruk Rattanabunyong, Kiattawee Choowongkomon, M Paul Gleeson
A series of 2-aminoaryl-7-arylbenzoxazole derivatives have been designed, synthesized and evaluated as anti-cancer agents. Fourteen of the compounds exhibited cytotoxic effects towards Human A549 lung cancer cells. We found 12l was the most potent with an EC50 of 0.4 μM, equivalent to the anti-cancer drug doxorubicin, but had low selectivity following cross screening in monkey kidney Vero cells. Eight of the most potent or most selective compounds were further profiled in additional cell lines (MCF7, NCI-H187 and KB) to better understand their cytotoxic activity...
May 23, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28533468/vacuolation-activity-and-intracellular-trafficking-of-artb-the-binding-subunit-of-an-ab5-toxin-produced-by-salmonella-enterica-serovar-typhi
#2
Brock P Herdman, James C Paton, Hui Wang, Travis Beddoe, Adrienne W Paton
Various Salmonella enterica serovars, including S Typhi, encode an AB5 toxin (ArtAB), the A subunit of which is an ADP-ribosyltransferase related to the S1 subunit of pertussis toxin. However, although the A subunit is able to catalyse ADP-ribosylation of host G proteins, a cytotoxic phenotype has yet to be identified for the holotoxin. Here we show that its B subunit pentamer (ArtB) binds to receptors on the surface of Vero (African green monkey kidney), CHO (Chinese hamster ovary), U937 (human monocyte) and HBMEC (human brain microvascular endothelial) cell lines...
May 22, 2017: Infection and Immunity
https://www.readbyqxmd.com/read/28494087/investigation-of-twenty-selected-medicinal-plants-from-malaysia-for-anti-chikungunya-virus-activity
#3
Yik Sin Chan, Kong Soo Khoo, Nam Weng Weng Sit
Chikungunya virus is a reemerging arbovirus transmitted mainly by Aedes mosquitoes. As there are no specific treatments available, Chikungunya virus infection is a significant public health problem. This study investigated 120 extracts from selected medicinal plants for anti-Chikungunya virus activity. The plant materials were subjected to sequential solvent extraction to obtain six different extracts for each plant. The cytotoxicity and antiviral activity of each extract were examined using African monkey kidney epithelial (Vero) cells...
September 2016: International Microbiology: the Official Journal of the Spanish Society for Microbiology
https://www.readbyqxmd.com/read/28470417/characterization-of-porcine-epidemic-diarrhea-virus-infectivity-in-human-embryonic-kidney-cells
#4
Jian Zhang, Longjun Guo, Yunfei Xu, Lijun Yang, Hongyan Shi, Li Feng, Yue Wang
Porcine epidemic diarrhea virus (PEDV), a causative agent of porcine epidemic diarrhea, causes economic loss in the global swine industry. Vero cell, an African green monkey kidney cell line, has been commonly used to isolate and propagate PEDV. However, since the production of interferon in these cells is defective, Vero cells are not the ideal cell type to study the molecular mechanisms of PEDV infection and the host antiviral innate immune response. In this study, we observed that human embryonic kidney 293 (HEK293) cells were susceptible to infection with PEDV vaccine strain CV777 (G1 subtype) and field isolate LNCT2 (G2 subtype)...
May 3, 2017: Archives of Virology
https://www.readbyqxmd.com/read/28460582/comprehensive-analysis-of-circulating-microrna-specific-to-the-liver-heart-and-skeletal-muscle-of-cynomolgus-monkeys
#5
Takuma Iguchi, Noriyo Niino, Satoshi Tamai, Ken Sakurai, Kazuhiko Mori
Circulating microRNAs (miRNAs) could represent sensitive and specific biomarkers for tissue injury. However, their utility as biomarkers in nonclinical toxicological studies using nonhuman primates is limited by a lack of information on their organ specificity and circulating levels under resting condition of the animals. Herein, liver, heart, and skeletal muscle-specific expression patterns of miRNAs were determined in 27 tissues/organs from male and female monkeys (n =2/sex) by next-generation sequencing (NGS) analysis...
January 1, 2017: International Journal of Toxicology
https://www.readbyqxmd.com/read/28456731/different-involvement-of-oat-in-renal-disposition-of-oral-anticoagulants-rivaroxaban-dabigatran-and-apixaban
#6
Yuri Tsuruya, Takeo Nakanishi, Hisakazu Komori, Xinying Wang, Naoki Ishiguro, Tomoko Kito, Kouji Ikukawa, Wataru Kishimoto, Sumito Ito, Olaf Schaefer, Thomas Ebner, Norio Yamamura, Hiroyuki Kusuhara, Ikumi Tamai
This study aimed to investigate the interactions of three anti-coagulants, rivaroxaban, apixaban, and dabigatran, with five human SLC transporters, hOAT1, hOAT3, hOCT2, hOATP1B1, and hOATP1B3. Apixaban inhibited hOAT3, hOATP1B1, and hOATP1B3, and rivaroxaban inhibited hOAT3 and hOATP1B3, with IC50 values of > 20 and >5 μM, respectively. The effect of dabigatran was negligible or very weak, so significant drug interactions at therapeutic doses are unlikely. Specific uptake of rivaroxaban was observed only in human and mouse OAT3-expressing cells...
April 26, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28444791/trialling-nutrient-recommendations-for-slow-lorises-nycticebus-spp-based-on-wild-feeding-ecology
#7
F Cabana, E Dierenfeld, W Wirdateti, G Donati, K A I Nekaris
Slow loris (Nycticebus spp.) captive diets have been based on routine and anecdotes rather than scientific fact. The growing body of evidence contradicts the high fruit diet supported by such anecdotes. Non-human primate nutrient requirements are grouped into new (based on the common marmoset Callithrix jacchus) or old world (based on rhesus macaques Macaca mulatta) primates. Slow lorises are known to suffer from many health ailments in captivity such as dental disease, obesity, wasting and kidney issues all of which have been linked to diet...
April 26, 2017: Journal of Animal Physiology and Animal Nutrition
https://www.readbyqxmd.com/read/28434690/assessment-of-potential-mirna-biomarkers-of-vero-cell-tumorigenicity-in-a-new-line-agmk1-9t7-of-african-green-monkey-kidney-cells
#8
Belete Teferedegne, Daniel M Rotroff, Juliete Macauley, Gideon Foseh, Gladys Lewis, Alison Motsinger-Rief, Andrew M Lewis
Patterns of microRNA expression appear to delineate the process of spontaneous neoplastic development-transformation (SPNDT) occurring in the African green monkey kidney (AGMK) VERO cell line (Teferedegne et al., 2010). Analysis of microarray data identified 6 microRNAs whose high-level of expression peaked when the World Health Organization 10-87 VERO cells became tumorigenic at passage (p) 190. Six miRNAs were identified as potential biomarkers for the expression of the VERO-cell tumorigenic phenotype (Teferedegne et al...
April 20, 2017: Vaccine
https://www.readbyqxmd.com/read/28389265/preclinical-pharmacokinetics-pharmacodynamics-tissue-distribution-and-interspecies-scaling-of-recombinant-human-coagulation-factor-xa-i16l
#9
Chuenlei Parng, Victoria Markiewicz, Jianqing Chen, Beth Leary, Nicole Duriga, Lisa Dyleski, Teresa Caiazzo, Michael Bolt, Alison Joyce, Boris Gorovits, Debra D Pittman, Robert Webster
FXa(I16L) is a recombinant human FXa variant which is currently being evaluated in the clinic for treating intracerebral hemorrhage. The aim of our studies was to investigate overall pharmacokinetics, pharmacodynamics and distribution of FXa(I16L) in preclinical species, and to understand its potential implication in human. Pharmacokinetics of FXa(I16L) was examined using active site probes and the results showed that FXa(I16L) displayed fast clearance, low volume of distribution and a very short plasma resident time in mice, rats and monkeys...
April 4, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28373047/sodium-alginate-and-gum-acacia-hydrogels-of-zinc-oxide-nanoparticles-reduce-hemolytic-and-oxidative-stress-inflicted-by-zinc-oxide-nanoparticles-on-mammalian-cells
#10
R Raguvaran, Anju Manuja, Balvinder K Manuja, T Riyesh, Sandeep Singh, M Kesavan, U Dimri
Zinc oxide nanoparticles are important nanomaterials currently under research due to their applicability in nanomedicine. Toxicity of ZnO NPs has been extensively studied and has been shown to affect various cell types and animal systems. In this study, we investigated hemolytic potential and oxidative stress inflicted by ZnO NPs and ZnO NPs-loaded-sodium alginate-gum acacia hydrogels on horse erythrocytes and African green monkey kidney (Vero) cells. Our study provides a better understanding of the hemolytic and oxidative effects of interaction of ZnO NPs and ZnO NPs released from polymeric hydrogels with the biological system...
March 31, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28372287/organ-reconstruction-dream-or-reality-for%C3%A2-the%C3%A2-future
#11
J-F Stoltz, L Zhang, J S Ye, N De Isla
The relevance of research on reconstructed organs is justified by the lack of organs available for transplant and the growing needs for the ageing population. The development of a reconstructed organ involves two parallel complementary steps: de-cellularization of the organ with the need to maintain the structural integrity of the extracellular matrix and vascular network and re-cellularization of the scaffold with stem cells or resident cells.Whole organ engineering for liver, heart, lung or kidneys, is particularly difficult because of the structural complexity of organs and heterogeneity of cells...
2017: Bio-medical Materials and Engineering
https://www.readbyqxmd.com/read/28321043/immunolocalization-of-novel-corticomedullary-tubule-injury-markers-in-cynomolgus-monkeys-treated-with-amphotericin-b
#12
J Eric McDuffie, Jing Ying Ma, Yunhai Zhang, Frederic S Almy, Xiaoyun Wu, Ke Li, Manisha Sonee, Ryan Meng, Michele Rizzolio, Sandra S Snook
Amphotericin B (AmpB) nephrotoxicity was used to assess the utility of drug‑induced kidney injury (DIKI) biomarkers in an exploratory study in male cynomolgus monkeys. All animals had quantifiable levels of AmpB in plasma on days 1 and 4. There were no clinical signs of AmpB‑induced toxicity in this study. The gold standard method used to confirm AmpB‑induced DIKI was anatomic pathology which revealed microscopic lesions with varying grades of severity. Immunolocalization of alpha‑1 microglobulin (α‑1M), kidney injury molecule 1 (KIM‑1), osteopontin (OPN) and neutrophil gelatinase‑associated lipocalin (NGAL) proteins was evaluated in formalin‑fixed, paraffin‑embedded monkey kidney tissue sections...
2017: Journal of Toxicological Sciences
https://www.readbyqxmd.com/read/28277843/nanoethosomal-formulation-of-gammaoryzanol-for-skin-aging-protection-and-wrinkle-improvement-a-histopathological-study
#13
Saman Heydari, Saeed Ghanbarzadeh, Behzad Anoosh, Mohammad Reza Ranjkesh, Yousef Javadzadeh, Maryam Kouhsoltani, Hamed Hamishehkar
BACKGROUND: Free radical scavengers and antioxidants, with the main focus on enhanced targeting to the skin layers, can provide protection against skin ageing. OBJECTIVE: The aim of the present study was to prepare nanoethosomal formulation of Gammaoryzanol (GO), a water insoluble antioxidant, for its dermal delivery to prevent skin aging. METHODS: Nanoethosomal formulation was prepared by a modified ethanol injection method and characterized by using laser light scattering, scanning electronic microscope (SEM) and X-ray diffraction (XRD) techniques...
March 3, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28274810/non-clinical-safety-evaluation-and-risk-assessment-to-human-of-aleglitazar-a-dual-ppar-%C3%AE-%C3%AE-agonist-and-its-major-human-metabolite
#14
Martin Bopst, Elke-Astrid Atzpodien
The non-clinical safety profile of aleglitazar, a peroxisome proliferator activated receptor alpha/gamma agonist, and its major human metabolite M6 was studied in a complete package consisting of drug metabolism and pharmacokinetics characterization, safety pharmacology, genotoxicity, repeat dose toxicity, reproductive toxicity and carcinogenicity studies. These studies identified the following main targets similar to other PPAR agonists: red blood cell parameters, liver, heart, kidney, ovaries, testes, bone marrow, adipose tissue, and fluid accumulation...
March 6, 2017: Regulatory Toxicology and Pharmacology: RTP
https://www.readbyqxmd.com/read/28245462/cashew-nut-positioning-during-stone-tool-use-by-wild-bearded-capuchin-monkeys-sapajus-libidinosus
#15
Tiago Falótico, Lydia V Luncz, Magdalena S Svensson, Michael Haslam
Wild capuchin monkeys (Sapajus libidinosus) at Serra da Capivara National Park, Brazil, regularly use stone tools to break open cashew nuts (Anacardium spp.). Here we examine 2 approaches used by the capuchins to position the kidney-shaped cashew nuts on an anvil before striking with a stone tool. Lateral positioning involves placing the nut on its flatter, more stable side, therefore requiring less attention from the monkey during placement. However, the less stable and never previously described arched position, in which the nut is balanced with its curved side uppermost, requires less force to crack the outer shell...
2016: Folia Primatologica; International Journal of Primatology
https://www.readbyqxmd.com/read/28228227/%C3%AE-butenolide-and-furanone-derivatives-from-the-soil-derived-fungus-aspergillus-sclerotiorum-psu-rspg178
#16
Patima Phainuphong, Vatcharin Rukachaisirikul, Kwanruthai Tadpetch, Yaowapa Sukpondma, Saowanit Saithong, Souwalak Phongpaichit, Sita Preedanon, Jariya Sakayaroj
Chromatographic separation of the broth extract of the soil-derived fungus Aspergillus sclerotiorum PSU-RSPG178 resulted in isolation of four γ-butenolide-furanone dimers, aspersclerotiorones A-D, a furanone derivative, aspersclerotiorone E, and two γ-butenolide derivatives, aspersclerotiorones F and G, together with six known compounds, penicillic acid, dihydropenicillic acid, 5,6-dihydro-6-hydroxypenicillic acid, 6-methoxy-5,6-dihydropenicillic acid, coculnol and (4R,5R)-4,5-dihydroxy-3-methoxy-5-methylcyclohex-2-en-1-one...
May 2017: Phytochemistry
https://www.readbyqxmd.com/read/28224391/development-and-evaluation-of-a-nanoemulsion-containing-ursolic-acid-a-promising-trypanocidal-agent-nanoemulsion-with-ursolic-acid-against-t-cruzi
#17
Erika Cristina Vargas de Oliveira, Zumira Aparecida Carneiro, Sérgio de Albuquerque, Juliana Maldonado Marchetti
Over a hundred years after the discovery of Chagas disease, this ailment continues to affect thousands of people. For more than 40 years, only two drugs have been available to treat it. Ursolic acid is a naturally occurring terpene that has shown a good trypanocidal action. However, the hydrophobicity of this compound presents a challenge for the development of proper delivery systems. Nanostructured systems are a prominent in delivering lipophilic drugs. Thus, a nanoemulsion containing ursolic acid was developed and had its trypanocidal activity and cytotoxicity evaluated...
February 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28217929/phytochemical-characterization-antibacterial-acetylcholinesterase-inhibitory-and-cytotoxic-properties-of-cryptostephanus-vansonii-an-endemic-amaryllid
#18
Mack Moyo, Adeyemi O Aremu, Jude C Chukwujekwu, Jiri Gruz, Jiri Skorepa, Karel Doležal, Cuthbert A T Katsvanga, Johannes Van Staden
Cryptostephanus vansonii I. Verd., an endemic Amaryllidaceae species from Zimbabwe, was evaluated for its acetylcholinesterase (AChE) inhibitory and cytotoxicity properties using Ellman's colorimetric method and the tetrazolium-based colorimetric assay against Vero monkey kidney cells, respectively. The plant extracts were also evaluated for their antibacterial activity against five bacteria. Furthermore, phytochemical profiles of the extracts were determined using ultra-high performance liquid chromatography coupled with tandem mass spectrometry analysis...
February 20, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28215474/establishment-of-disseminated-intravascular-coagulation-dic-model-by-a-single-iv-administration-of-escherichia-coli-derived-lipopolysaccharide-lps-to-cynomolgus-monkeys-and-evaluation-of-its-pathophysiological-status
#19
Hirofumi Minomo, Kengo Inoue, Shuko Sakaki, Takanobu Okazaki, Kinji Kobayashi, Kazuhiko Inoue, Atsuro Miyata
We prepared a DIC model by administrating LPS to cynomolgus monkeys, and investigated its potential for evaluations of new medicines for DIC therapy. Peripheral blood mononuclear cells (PBMC) collected from cynomolgus monkeys were incubated with LPS (8 types), and TNF-α levels in the media were measured. LPS from Escherichia coli (K-235) was most appropriate in terms of larger increases and smaller variation in TNF-α levels. PBMC from rats, cynomolgus monkeys or humans were incubated with LPS (K-235), and the TNF-α response to LPS was investigated...
February 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28190821/outbreak-of-pasteurellosis-in-captive-bolivian-squirrel-monkeys-saimiri-boliviensis
#20
Mizuki Yoshino, Jun Sasaki, Konomi Kuramochi, Mitsutaka Ikezawa, Natsuko Mukaizawa, Masanobu Goryo
In September 2012, five Bolivian squirrel monkeys housed in a zoological park died within sequential several days without obvious clinical signs. In a necrospy, one monkey presented swelling of the kidney with multifocal white nodules in the parenchyma, and other two had pulmonary congestion. Histopathologically, multifocal bacterial colonies of gram-negative coccobacillus were found in the sinusoid of the liver in all monkeys examined (Nos.1-4). Additionally, purulent pyelonephritis, pneumonia and disseminated small bacterial colonies in blood vessels were observed...
March 23, 2017: Journal of Veterinary Medical Science
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