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https://www.readbyqxmd.com/read/28822169/-effect-factors-and-mechanisms-of-borneol-s-bidirectional-regulation-on-blood-brain-barrier-permeability
#1
Hong-Jin Wang, Jun-Jie Wu, Qiang Xue, Ji-Fen Zhang, Xiao-Yu Xu
In recent twenty years, there are a lot of studies about the effect of borneol on permeability of blood-brain barrier(BBB); however, it isDODOrt of regular conclusions of effect factors and in-depth analysis of functional mechanisms. The current researching data were collected and analyzed in this paper for illuminating the effect factors and mechanisms of borneol on permeability of BBB.The following conclusions were obtained: five factors about borneol influencing the permeability of BBB. First, opticity activity of borneol had no significant effect on action effects...
June 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28822161/-synergistic-mechanism-of-traditional-chinese-medicine-based-on-target-combination-of-pept1-and-ppar%C3%AE
#2
Lian-Sheng Qiao, Yan-Kun Chen, Gang-Gang Luo, Fang Lu, Si-Jia Liu, Gong-Yu Li, Yan-Ling Zhang
Synergistic effect is main pharmacological mechanism of traditional Chinese medicine(TCM). The research method based on the key targets combination is an important method to explore the synergistic effect of TCM. Peptide transporter 1 (PepT1) is an essential target for drug uptake into the bloodstream, accounting for about 50% of the total transporter protein content from the small intestine. Peroxisome proliferator-activated receptor α(PPARα) is the lipid-lowering target of fibrates, which have a good hypolipidemic effect by activating PPARα...
June 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28821463/lymphatic-transport-and-lymph-node-targeting-of-methotrexate-conjugated-pegylated-dendrimers-is-enhanced-by-reducing-the-length-of-the-drug-linker-or-masking-interactions-with-the-injection-site
#3
Gemma M Ryan, Victoria M McLeod, Dharmini Mehta, Brian D Kelly, Pauline C Stanislawski, David J Owen, Lisa M Kaminskas, Christopher J H Porter
Drug conjugation to dendrimer-based delivery systems has been shown to enhance delivery to the lymphatic system after subcutaneous administration. Dendrimer interaction with components of the interstitium at the injection site, however, may prevent drainage from the injection site. The current study sought to vary the length of a linker employed to conjugate methotrexate (MTX) to a PEGylated dendrimer, in an attempt to reduce MTX interaction with interstitial binding sites and enhance lymphatic drainage. Dendrimers with shorter linkers resulted in higher lymphatic drainage, presumably via shielding of interaction sites by the PEG mantle, but were not retained in lymph nodes...
August 15, 2017: Nanomedicine: Nanotechnology, Biology, and Medicine
https://www.readbyqxmd.com/read/28821406/structural-insight-into-lipopolysaccharide-transport-from-the-gram-negative-bacterial-inner-membrane-to-the-outer-membrane
#4
REVIEW
Haohao Dong, Xiaodi Tang, Zhengyu Zhang, Changjiang Dong
Lipopolysaccharide (LPS) is an important component of the outer membrane (OM) of Gram-negative bacteria, playing essential roles in protecting bacteria from harsh environments, in drug resistance and in pathogenesis. LPS is synthesized in the cytoplasm and translocated to the periplasmic side of the inner membrane (IM), where it matures. Seven lipopolysaccharide transport proteins, LptA-G, form a trans‑envelope complex that is responsible for LPS extraction from the IM and transporting it across the periplasm to the OM...
August 15, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28821154/design-and-characterization-of-a-biocompatible-physical-hydrogel-based-on-scleroglucan-for-topical-drug-delivery
#5
Patrizia Paolicelli, Gabriele Varani, Settimio Pacelli, Elisa Ogliani, Martina Nardoni, Stefania Petralito, Alessandra Adrover, Maria Antonietta Casadei
Physical hydrogels of a high-carboxymethylated derivative of scleroglucan (Scl-CM300) were investigated as potential systems for topical drug delivery using three different therapeutic molecules (fluconazole, diclofenac and betamethasone). Rheological tests were carried out on drug-loaded hydrogels along with in-vitro release studies in a vertical Franz cell, in order to investigate if and how different drugs may influence the rheological and release properties of Scl-CM300 hydrogels. Experimental results and theoretical modeling highlighted that, in the absence of drug/polymer interactions (as for fluconazole and betamethasone) Scl-CM300 matrices offer negligible resistance to drug diffusion and a Fickian transport model can be adopted to estimate the effective diffusion coefficient in the swollen hydrogel...
October 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28819699/cudc-907-a-dual-hdac-and-pi3k-inhibitor-reverses-platinum-drug-resistance
#6
Kenneth K W To, Li-Wu Fu
Platinum (Pt)-based anticancer drugs are the mainstay of treatment for solid cancers. However, resistance to Pt drugs develops rapidly, which can be caused by overexpression of multidrug resistance transporters and activation of DNA repair. CUDC-907 is a potent molecular targeted anticancer agent, rationally designed to simultaneously inhibit histone deacetylase (HDAC) and phosphatidylinositol 3-kinase (PI3K). We investigated the potentiation effect of CUDC-907 on Pt drugs in resistant cancer cells. ABCC2 stably-transfected HEK293 cells and two pairs of parental and Pt-resistant cancer cell lines were used to test for the circumvention of resistance by CUDC-907...
August 17, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/28819448/preparation-and-application-of-cell-membrane-camouflaged-nanoparticles-for-cancer-therapy
#7
REVIEW
Yihui Zhai, Jinghan Su, Wei Ran, Pengcheng Zhang, Qi Yin, Zhiwen Zhang, Haijun Yu, Yaping Li
Cancer is one of the leading causes of death worldwide. Many treatments have been developed so far, although effective, suffer from severe side effects due to low selectivity. Nanoparticles can improve the therapeutic index of their delivered drugs by specifically transporting them to tumors. However, their exogenous nature usually leads to fast clearance by mononuclear phagocytic system. Recently, cell membrane-camouflaged nanoparticles have been investigated for cancer therapy, taking advantages of excellent biocompatibility and versatile functionality of cell membranes...
2017: Theranostics
https://www.readbyqxmd.com/read/28819436/epithelial-mesenchymal-transition-potential-regulator-of-abc-transporters-in-tumor-progression
#8
REVIEW
Zong-Sheng Jiang, Yan-Zi Sun, Shao-Ming Wang, Jun-Shan Ruan
Epithelial-mesenchymal transition (EMT) can directly contribute to some malignant phenotypes of tumor cells including invasion, metastasis and resistance to chemotherapy. Although EMT is widely demonstrated to play a critical role in chemoresistance and metastasis, the potential signaling network between EMT and drug resistance is still unclear. The distribution of drugs in the internal and external environment of the tumor cells is tightly linked with ATP-binding cassette (ABC) transporters. Recent studies have shown that ABC transporters expression changed continuously during EMT...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/28819225/cytochrome-p450-abc-transporter-inhibition-simultaneously-enhances-ivermectin-pharmacokinetics-in-the-mammal-host-and-pharmacodynamics-in-anopheles-gambiae
#9
Carlos J Chaccour, Felix Hammann, Marta Alustiza, Sandra Castejon, Brian B Tarimo, Gloria Abizanda, Ángel Irigoyen Barrio, Helena Martí Soler, Rafael Moncada, José Ignacio Bilbao, Azucena Aldaz, Marta Maia, José Luis Del Pozo
Mass administration of endectocides, drugs that kill blood-feeding arthropods, has been proposed as a complementary strategy to reduce malaria transmission. Ivermectin is one of the leading candidates given its excellent safety profile. Here we provide proof that the effect of ivermectin can be boosted at two different levels by drugs inhibiting the cytochrome or ABC transporter in the mammal host and the target mosquitoes. Using a mini-pig model, we show that drug-mediated cytochrome P450/ABC transporter inhibition results in a 3-fold increase in the time ivermectin remains above mosquito-killing concentrations...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28819176/use-of-biocompatible-sorafenib-gold-nanoconjugates-for-reversal-of-drug-resistance-in-human-hepatoblatoma-cells
#10
Sandeep Kumar Vishwakarma, Priyanka Sharmila, Avinash Bardia, Lakkireddy Chandrakala, N Raju, G Sravani, B V S Sastry, Md Aejaz Habeeb, Aleem Ahmed Khan, Marshal Dhayal
The present study identifies the potential of highly biocompatible SF-GNP nano-conjugate to enhance the chemotherapeutic response to combat drug resistance in cancer cells. We developed a stable colloidal suspension of sorafenib-gold nanoconjugate (SF-GNP) of <10 nm size in aqueous medium for reverting the cancer drug resistance in SF-resistant HepG2 cells in a 3D ex-vivo model system. In-vivo biocompatibility assay of SF-GNPs showed absence of systemic toxicological effects including hematological, biochemical and histological parameters...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28818691/multi-center-evaluation-of-the-cobas-%C3%A2-liat-%C3%A2-influenza-a-b-rsv-assay-for-rapid-point-of-care-diagnosis
#11
Jane Gibson, Elissa M Schechter-Perkins, Patricia Mitchell, Sharon Mace, Yu Tian, Kemi Williams, Robert Luo, Belinda Yen-Lieberman
Point of Care Testing (POCT) provides the capability for rapid laboratory test results in patient care environments where a traditional clinical laboratory is not available. POCTs have shorter turn-around times (TATs), they may be performed by non-laboratory personnel, and the need for transport time is eliminated. The Food and Drug Administration (FDA) recently granted Clinical Laboratory Improvements Amendment (CLIA) waiver status to the cobas(®) Influenza A/B & RSV assay, a rapid, accurate point-of-care test for Influenza and respiratory syncytial virus (RSV) performed on the Liat(®) System...
August 8, 2017: Journal of Clinical Virology: the Official Publication of the Pan American Society for Clinical Virology
https://www.readbyqxmd.com/read/28818458/colonic-delivery-of-indometacin-loaded-pga-co-pdl-microparticles-coated-with-eudragit-l100-55-from-fast-disintegrating-tablets
#12
Hesham M Tawfeek, Ahmed A H Abdellatif, Thomas J Dennison, Afzal R Mohmmed, Younis Sadiq, Imran Y Saleem
The aim of this work was to investigate the efficient targeting and delivery of indometacin (IND), as a model anti-inflammatory drug to the colon for treatment of inflammatory bowel disease. We prepared fast disintegrating tablets (FDT) containing IND encapsulated within poly(glycerol-adipate-co-ɷ-pentadecalactone), PGA-co-PDL, microparticles and coated with Eudragit L100-55 at different ratios (1:1.5, 1:1, 1:0.5). Microparticles encapsulated with IND were prepared using an o/w single emulsion solvent evaporation technique and coated with Eudragit L-100-55 via spray drying...
August 14, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28816632/the-liver-circadian-clock-modulates-biochemical-and-physiological-responses-to-metformin
#13
Emma Henriksson, Anne-Laure Huber, Erin K Soto, Anna Kriebs, Megan E Vaughan, Drew Duglan, Alanna B Chan, Stephanie J Papp, Madelena Nguyen, Megan E Afetian, Katja A Lamia
Metformin is widely used in the treatment of type 2 diabetes to lower blood glucose. Although metformin is a relatively safe and effective drug, its clinical efficacy is variable and under certain circumstances it may contribute to life-threatening lactic acidosis. Thus, additional understanding of metformin pharmacokinetics and pharmacodynamics could provide important information regarding therapeutic use of this widely prescribed drug. Here we report a significant effect of time of day on acute blood glucose reduction in response to metformin administration and on blood lactate levels in healthy mice...
August 2017: Journal of Biological Rhythms
https://www.readbyqxmd.com/read/28816386/chemotaxis-guided-hybrid-neutrophil-micromotor-for-actively-targeted-drug-transport
#14
Jingxin Shao, Mingjun Xuan, Hongyue Zhang, Xiankun Lin, Zhiguang Wu, Qiang He
Engineering self-propelled micromotors with good biocompatibility and biodegradability for actively seeking sites of diseases and targeted drug transport remains a huge challenge. Here we demonstrate that neutrophils with intrinsic chemotaxis ability could be transformed into self-guided biohybrid motors through integrating mesoporous silica nanoparticles (MSNs) with high loading capability. To realize the compatibility of neutrophil cells with drug-loaded MSNs, bacteria membranes derived from E. coli were coated onto MSNs in advance by using a camouflaging strategy...
August 17, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28815721/rgd-peptide-based-target-drug-delivery-of-doxorubicin-nanomedicine
#15
Yuan Sun, Chen Kang, Fei Liu, You Zhou, Lei Luo, Hongzhi Qiao
Preclinical Research Doxorubicin (DOX) is commonly used for the treatment of breast cancer and lymphoma. However, its clinical use has been severely limited due to cardiotoxicity, requiring the development of safer and more efficient pharmaceutical formulations of DOX. Advances in nanotechnology have provided new ways to administer chemotherapeutic drugs like DOX are conveyed into the body and to tumor sites. These Nanotechnology approaches have aided in the selective accumulation of DOX into tumor sites via the enhanced permeability and retention...
August 16, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28815595/sigma-1-receptor-ligands-inhibit-catecholamine-secretion-from-adrenal-chromaffin-cells-due-to-block-of-nicotinic-acetylcholine-receptors
#16
Rebecca L Brindley, Mary Beth Bauer, Nolan D Hartley, Kyle J Horning, Kevin P M Currie
Adrenal chromaffin cells (ACCs) are the neuroendocrine arm of the sympathetic nervous system and key mediators of the physiological stress response. Acetylcholine (ACh) released from preganglionic splanchnic nerves activates nicotinic acetylcholine receptors (nAChRs) on chromaffin cells causing membrane depolarization, opening voltage-gated Ca(2+) channels (VGCC), and exocytosis of catecholamines and neuropeptides. The serotonin transporter (SERT) is expressed in ACCs and interacts with 5-HT1A receptors to control secretion...
August 16, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28815028/the-majority-of-hepatitis-c-patients-treated-with-direct-acting-antivirals-are-at-risk-for-relevant-drug-drug-interactions
#17
Elise J Smolders, Floor Ac Berden, Clara Tmm de Kanter, Wietske Kievit, Joost Ph Drenth, David M Burger
BACKGROUND: Direct-acting antivirals have improved treatment of chronic hepatitis C virus infection significantly. Direct-acting antivirals inhibit/induce and can also be substrates of drug-metabolising enzymes and transporters. This increases the risk for drug-drug interactions. OBJECTIVE: The purpose of this study was to predict drug-drug interactions with co-medication used by hepatitis C virus-infected patients. METHODS: We assembled a nationwide cohort of hepatitis C patients and collected cross-sectional data on co-medication use...
August 2017: United European Gastroenterology Journal
https://www.readbyqxmd.com/read/28815024/stem-cell-derived-organoids-to-model-gastrointestinal-facets-of-cystic-fibrosis
#18
REVIEW
Meike Hohwieler, Lukas Perkhofer, Stefan Liebau, Thomas Seufferlein, Martin Müller, Anett Illing, Alexander Kleger
Cystic fibrosis (CF) is one of the most frequently occurring inherited human diseases caused by mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) which lead to ample defects in anion transport and epithelial fluid secretion. Existing models lack both access to early stages of CF development and a coeval focus on the gastrointestinal CF phenotypes, which become increasingly important due increased life span of the affected individuals. Here, we provide a comprehensive overview of gastrointestinal facets of CF and the opportunity to model these in various systems in an attempt to understand and treat CF...
August 2017: United European Gastroenterology Journal
https://www.readbyqxmd.com/read/28814238/structural-insights-for-drugs-developed-for-phospholipase-d-enzymes
#19
Kimberly Stieglitz
BACKGROUND: In recent years human phospholipase D enzymes (PLD1 and PLD2 isozymes) have emerged as drug targets for various diseases such as cardiovascular disease, cancer, infectious diseases and neurodegenerative conditions such as Alzheimer's and Parkinson's disease. The interest in PLD as a drug target is due to the fact that PLD enzymes belong to a superfamily of phospholipases that are essential to intracellular and extracellular signaling. Many bioactive lipid signaling molecules are generated by these enzymes including phosphatidic and lysophosphatidic acid, arachidonic acid, and diacylglycerol (DAG)...
August 15, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28814193/sirolimus-and-mirabegron-interaction-in-a-hematopoietic-cell-transplant-patient
#20
Jeff A Engle, Christina Fair
Purpose Hematopoietic cell transplant patients are exposed to numerous classes of medications. Transplant practitioners must vigilantly monitor for drug interactions especially involving immunosuppressants. We report a hematopoietic cell transplant patient receiving sirolimus who developed supratherapeutic serum concentrations after initiating mirabegron. Summary A 31-year-old, 98 kg female received a second umbilical cord blood transplant four years after the first transplant for relapsed acute myeloid leukemia...
January 1, 2017: Journal of Oncology Pharmacy Practice
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