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Ding Tang, Keli Chen, Luqi Huang, Juan Li
Apigenin, a natural flavone, is widely distributed in plants such as celery, parsley and chamomile. It is present principally as glycosylated in nature. Higher intake of apigenin could reduce the risk of chronic diseases. It has gained particular interest in recent years as a beneficial, health-promoting agent with low intrinsic toxicity. Areas covered: This review summarizes and the absorption, distribution, metabolism and excretion (ADME) properties of apigenin, and drug-drug interaction of apigenin. Expert opinion: Since apigenin is a bioactive plant flavone and is widely distributed in common food, its consumption through the diet is recommended...
October 21, 2016: Expert Opinion on Drug Metabolism & Toxicology
Qiang Zhang, Yaqing Zhang, Joshua D Parsels, Ines Lohse, Theodore S Lawrence, Marina Pasca di Magliano, Yi Sun, Meredith A Morgan
Pancreatic cancers driven by KRAS mutations require additional mutations for tumor progression. The tumor suppressor FBXW7 is altered in pancreatic cancers, but its contribution to pancreatic tumorigenesis is unknown. To determine potential cooperation between Kras mutation and Fbxw7 inactivation in pancreatic tumorigenesis, we generated P48-Cre;LSL-Kras(G12D);Fbxw7(fl/fl) (KFC(fl/fl)) compound mice. We found that KFC(fl/fl) mice displayed accelerated tumorigenesis: all mice succumbed to pancreatic ductal adenocarcinoma (PDA) by 40 days of age, with PDA onset occurring by 2 weeks of age...
October 17, 2016: Neoplasia: An International Journal for Oncology Research
Man Koon Suh, Kyo Ho Lee, Aram Harijan, Hyung-Gu Kim, Euicheol C Jeong
BACKGROUND: Alloplastic materials are a mainstay in Asian rhinoplasty. However, the outline of alloplastic implants can become conspicuous over time in rhinoplasty patients, which is a significant cause for revision. In revision rhinoplasty, alloplastic materials can remain a viable and affordable option in Asian patients. The acellular dermal matrices (ADM) are often used to interface between the silicone material and the skin envelope. This study assesses histologic changes following implantation of ADM-covered silicone material in rats...
October 14, 2016: Journal of Craniofacial Surgery
Man Zhao, Shuliang Yu, Man Zhang
Multidrug resistance (MDR) is the major obstacle to bladder cancer chemotherapy. Several mechanisms have been implicated in the development of MDR, including extrusion of the drug by cell membrane pumps, associated with P‑glycoprotein (P‑gp) and multidrug resistance‑associated protein (MRP); increased DNA damage repair, associated with topoisomerase II (Topo II); suppression of drug‑induced apoptosis, associated with p53; and regulation of cancer cell growth, associated with vascular endothelial growth factor (VEGF)...
October 5, 2016: Molecular Medicine Reports
Philippa Douglas, Sean F Tyrrel, Robert P Kinnersley, Michael Whelan, Philip J Longhurst, Anna L Hansell, Kerry Walsh, Simon J T Pollard, Gillian H Drew
Bioaerosols are released in elevated quantities from composting facilities and are associated with negative health effects, although dose-response relationships are unclear. Exposure levels are difficult to quantify as established sampling methods are costly, time-consuming and current data provide limited temporal and spatial information. Confidence in dispersion model outputs in this context would be advantageous to provide a more detailed exposure assessment. We present the calibration and validation of a recognised atmospheric dispersion model (ADMS) for bioaerosol exposure assessments...
September 26, 2016: International Journal of Hygiene and Environmental Health
Raquib Alam, Divya Wahi, Raja Singh, Devapriya Sinha, Vibha Tandon, Abhinav Grover, Rahisuddin
In an attempt to find potential anticancer agents, a series of novel ethyl 4-(3-(aryl)-1-phenyl-1H-pyrazol-4-yl)-2-oxo-6-(pyridin-3-yl)cyclohex-3-enecarboxylates 5a-i and 5-(3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)-3-(pyridin-3-yl)-4,5-dihydropyrazole-1-carbothioamides 6a-i were designed, synthesized and evaluated for their topoisomerase IIα inhibitory activity and in vitro cytotoxicity against a panel of cancerous cell lines (MCF-7, NCI-H460, HeLa) and a normal cell line (HEK-293T). Molecular docking studies of all the synthesized compounds into the binding site of topoisomerase IIα protein (PDB ID: 1ZXM) were performed to gain a comprehensive understanding into plausible binding modes...
October 5, 2016: Bioorganic Chemistry
P Douglas, S F Tyrrel, R P Kinnersley, M Whelan, P J Longhurst, K Walsh, S J T Pollard, G H Drew
Bioaerosols are released in elevated quantities from composting facilities and are associated with negative health effects, although dose-response relationships are not well understood, and require improved exposure classification. Dispersion modelling has great potential to improve exposure classification, but has not yet been extensively used or validated in this context. We present a sensitivity analysis of the ADMS dispersion model specific to input parameter ranges relevant to bioaerosol emissions from open windrow composting...
October 13, 2016: Journal of Environmental Management
J E Edwards, C LaCerte, T Peyret, N H Gosselin, J F Marier, A F Hofmann, D Shapiro
Obeticholic acid (OCA), a semisynthetic bile acid, is a selective and potent farnesoid X receptor (FXR) agonist in development for the treatment of chronic nonviral liver diseases. Physiologic pharmacokinetic models have been previously used to describe the absorption, distribution, metabolism, and excretion (ADME) of bile acids. OCA plasma levels were measured in healthy volunteers and cirrhotic subjects. A physiologic pharmacokinetic model was developed to quantitatively describe the ADME of OCA in patients with and without hepatic impairment...
October 15, 2016: Clinical and Translational Science
Xiaoting Gu, Chunxiao Lu, Dongxu He, Yangfan Lu, Jian Jin, Dequan Liu, Xin Ma
To define the role of the NOTCH signaling pathway in the development of chemoresistance and the associated epithelial-mesenchymal transition (EMT), we investigated the effect of Notch3 on adriamycin (ADM)-resistant human breast cancer cells (MCF-7/ADM cells). We found that Notch3 was downregulated and involved in the chemoresistance of MCF-7/ADM cells, while forced expression of Notch3 reversed the chemoresistance. Furthermore, fos-related antigen 1 (Fra1) was negatively regulated by Notch3 and was highly expressed in MCF-7/ADM cells...
October 14, 2016: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
Jing Chen, Jie Cheng, Juan Yi, Bei Xie, Li Lin, Zhuan Liu, Huaishun Zhao, Bei Wang, Ziying Ai, Yue Yang, Hulai Wei
There is no cross-resistance between arsenic trioxide and conventional chemotherapeutics. Classical multi-drug resistant (MDR) cells remain sensitive to arsenic trioxide, which may even reverse the drug resistance. Arsenic trioxide is also effective in leukemias/tumors that persist despite conventional cytotoxic or targeted drugs. We obtained a highly arsenic-resistant MDR leukemic cell line, HL-60/RS, by exposing leukemic HL-60 cells to adriamycin selection. We compared the arsenic sensitivity, and the expression and responses to arsenic of the arsenic-related transporters, MRP1, MRP2, and ASNA1, in paired parent/arsenic-resistant HL-60/RS/HL-60 and arsenic-sensitive/parental K562/ADM/K562 cells...
October 3, 2016: Leukemia Research
Huijuan Liu, Jie Wang, Guiyun Ren, Yanning Zhang, Fusheng Dong
OBJECTIVE: To study the relationship between proteoglycan inhibition and the implantation of salivary pleomorphic adenoma (SPA). METHODS: SPA fresh tissue was primitively cultured and identified. The Ad-shRNA-XT-II adenovirus vector was constructed and transfected into SPA cells to silence the XT-II gene. The expression of the XT-II gene and protein was detected using real-time PCR and western blotting, respectively. The proteoglycan content of the cells was determined 48 hours after transfectction...
October 12, 2016: Journal of Oral Pathology & Medicine
A Goto, Y Moriya, T Mandai, T Wakabayashi, T Tsukamoto, Y Tagawa, T Kondo, S Asahi
The non-clinical pharmacokinetics (PK) of TAK-357, a highly lipophilic (clogP>6) potential agent for the amelioration of Alzheimer's disease, was investigated in rats and dogs. A long half-life (t1/2) in plasma was observed in animals and a low total body clearance with high distribution volume was consistent with the long t1/2. The absorption, distribution, metabolism and excretion (ADME) studies using radiolabeled TAK-357 revealed that the total radioactivity was highly distributed to the adipose tissues and sustained with high concentration for over 4 weeks after oral administration...
October 11, 2016: Drug Research
Richard W Siy, Rachel E Pferdehirt, Shayan A Izaddoost
INTRODUCTION: The use of biologic mesh where native tissue deficiencies limit reconstructive options has been well documented in the adult population, with increasing use to address the special requirements of complex abdominal wall reconstruction. There is, however, little documented evidence as to the safety and efficacy of these products in the pediatric population. METHODS: This retrospective case series details 5 pediatric cases of complicated abdominal hernia repair with Strattice®, a non-crosslinked porcine acellular dermal matrix...
September 23, 2016: Journal of Pediatric Surgery
Ranjeet Prasad Dash, R Jayachandra Babu, Nuggehally R Srinivas
1. Several SGLT-2 inhibitors are in clinical use for the management of type 2 diabetes. The objectives of the current review were: a) to provide a comparative pharmacokinetics including absorption, distribution, metabolism and excretory (ADME) profiles of three SGLT2 inhibitors namely: sergliflozin, remogliflozin and ertugliflozin; b) to provide some perspectives on possible developmental issues. 2. Based on the t1/2 values observed in humans, the rank order of the three SGLT-2 inhibitors were ertugliflozin (16 h) > remogliflozin (2-4 h) >sergliflozin (1-1...
October 10, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Francisco Valenzuela-Sánchez, Blanca Valenzuela-Méndez, Juan Francisco Rodríguez-Gutiérrez, Ángel Estella-García, María Ángela González-García
Mid-regional pro-adrenomedullin (MR-proADM) has a good biomarker profile: its half-life is several hours, and its plasma concentrations can be determined in clinical practice, it is essentially irrelevant, but proportionally represents the levels and activity of adrenomedullin (ADM). ADM synthesis is widely distributed in tissues, including bone, adrenal cortex, kidney, lung, blood vessels and heart. Its fundamental biological effects include vasodilator, positive inotropic, diuretic, natriuretic and bronchodilator...
September 2016: Annals of Translational Medicine
Liza Margareth Medeiros de Carvalho Sousa, Gabriela Pacheco Mendes, Danila Barreiro Campos, Pietro Sampaio Baruselli, Paula de Carvalho Papa
We hypothesized that stimulatory and superovulatory treatments, using equine chorionic gonadotropin (eCG), modulate the expression of genes related to insulin, cellular modelling and angiogenesis signaling pathways in the bovine corpus luteum (CL). Therefore, we investigated: 1-the effect of these treatments on circulating insulin and somatomedin C concentrations and on gene and protein expression of INSR, IGF1 and IGFR1, as well as other insulin signaling molecules; 2-the effects of eCG on gene and protein expression of INSR, IGF1, GLUT4 and NFKB1A in bovine luteal cells; and 3-the effect of stimulatory and superovulatory treatments on gene and protein expression of ANG, ANGPT1, NOS2, ADM, PRSS2, MMP9 and PLAU...
2016: PloS One
Lingfeng Wang, Chunguang Hao, Biao Zhou, Xue Fu, Junliang Li, Zhigang Wang, Zhidong Rong
INTRODUCTION: This study investigated the application of selective sheepskin acellular dermal matrix (ADM), combined with the anticoagulant heparin, in the wound-healing treatment of deep second-degree burns (DSDB). METHODS: A DSDB model was established, and the test animals were randomly divided into 4 groups: iodophor gauze (IG), pig ADM (PA), selective sheepskin ADM (SSA), and heparinized selective sheepskin ADM (HSSA).The microcirculation of the wound surface, pathological structures, healing rates, and fibroblast apoptosis rates were observed at different times in each group...
September 29, 2016: Wounds: a Compendium of Clinical Research and Practice
Todd J Nilsen, Anouska Dasgupta, Yen-Chen Huang, Henry Wilson, Evangelia Chnari
BACKGROUND: The use of acellular dermal matrices (ADMs) has become the standard of practice in many reconstructive and aesthetic surgical applications. Different methods used to prepare the allograft tissue for surgical use can alter the ADMs natural properties. Aseptic processing has been shown to retain the natural properties of ADMs more favorably than terminally sterilized ADMs. Terminal sterilization has been historically linked to alteration of biological materials. In vitro work was conducted to compare ADM processing methods...
October 3, 2016: Aesthetic Surgery Journal
Karen L Bunday, Roger N Lemon, James M Kilner, Marco Davare, Guy A Orban
Motor resonance is the modulation of M1 corticospinal excitability induced by observation of others' actions. Recent brain imaging studies have revealed that viewing videos of grasping actions led to a differential activation of the ventral premotor cortex depending on whether the entire person is viewed versus only their disembodied hand. Here we used transcranial magnetic stimulation (TMS) to examine motor evoked potentials (MEPs) in the first dorsal interosseous (FDI) and abductor digiti minimi (ADM) during observation of videos or static images in which a whole person or merely the hand was seen reaching and grasping a peanut (precision grip) or an apple (whole hand grasp)...
September 11, 2016: Cortex; a Journal Devoted to the Study of the Nervous System and Behavior
Hana Čipčić Paljetak, Linda Tomašković, Mario Matijašić, Mirjana Bukvić, Andrea Fajdetić, Donatella Verbanac, Mihaela Perića
5-LOX - 5-lipoxygenase; ACT - artemisinin-based combination therapies; ADME - absorption, distribution, metabolism and excretion; BAL - broncho alveolar lavage; CABP - community acquired bacterial pneumonia; cAMP - cyclic adenosine monophosphate; CAP - community-acquired pneumonia; CF - cystic fibrosis, BOS bronchiolitis obliterans syndrome; cGMP - cyclic guanosine monophosphate; COPD - chronic obstructive pulmonary disease; COX - cyclooxygenase; DPB - diffuse panbronchiolitis; HDACs - histone deacetylases; IBD - inflammatory bowel disease; IL-1p - interleukin 1p; IL-6 - interleukin 6; MIC - minimal inhibitory concentrations; MLSB - macrolide, lincosamide, streptogramin B; NSAIDs - non-steroidal anti-inflammatory drugs; OVA - ovalbumin; PDE4 - phosphodiesterase 4; PMA - phorbol 12-myristate 13-acetate; RA - rheumatoid arthritis; RTI - respiratory tract infections; SAHA - suberoylanilide hydroxamic acid; SAR - structure-activity-relationship; Th1 - type 1 helper T-cell; TNBS - trinitrobenzene sulfonic acid; TNF-α - tumour necrosis factor α; UN - United Nations, WHO - World Health Organisation...
September 27, 2016: Current Topics in Medicinal Chemistry
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