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https://www.readbyqxmd.com/read/29055030/identification-of-absorbed-constituents-and-in-vivo-metabolites-in-rats-after-oral-administration-of-physalisalkekengi-var-franchetii-by-ultrahigh-pressure-liquid-chromatography-quadrupole-time-of-flight-mass-spectrometry
#1
Xinchi Feng, Xiaoguang Huo, Hongxia Liu, Liwei Chai, Liqin Ding, Feng Qiu
The calyces of Physalisalkekengi var. franchetii (Chinese Lantern, JDL) are well-known traditional Chinese medicine owing to its various therapeutic effects. However, the bioactive constituents responsible for the pharmacological effects of JDL and their metabolites in vivo are still unclear to date. In this paper, an ultrahigh-pressure liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC/Q-TOF-MS/MS) method was established to identify absorbed constituents and in vivo metabolites in rat biological fluids after oral administration of JDL...
October 20, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29055017/new-generation-nanomedicines-constructed-from-self-assembling-small-molecule-prodrugs-alleviate-cancer-drug-toxicity
#2
Hangxiang Wang, Zhongjie Lu, Lijiang Wang, Tingting Guo, Jiaping Wu, Jianqin Wan, Liqian Zhou, Hui Li, Zhen Li, Donghai Jiang, Penghong Song, Haiyang Xie, Lin Zhou, Xiao Xu, Shusen Zheng
The therapeutic index for chemotherapeutic drugs is determined in part by systemic toxicity, so strategies for dose intensification to improve efficacy must also address tolerability. In addressing this issue, we have investigated a novel combinatorial strategy of reconstructing a drug molecule and using sequential drug-induced nanoassembly to fabricate supramolecular nanomedicines (SNM). Using cabazitaxel (CTX) as a target agent, we established that individual synthetic prodrugs tethered with polyunsaturated fatty acids were capable of recapitulating self-assembly behavior independent of exogenous excipients...
October 20, 2017: Cancer Research
https://www.readbyqxmd.com/read/29054733/disrupted-ionic-homeostasis-in-ischemic-stroke-and-new-therapeutic-targets
#3
REVIEW
Hui-Jie Hu, Mingke Song
BACKGROUND: Stroke is a leading cause of long-term disability. All neuroprotectants targeting excitotoxicity have failed to become stroke medications. In order to explore and identify new therapeutic targets for stroke, we here reviewed present studies of ionic transporters and channels that are involved in ischemic brain damage. METHOD: We surveyed recent literature from animal experiments and clinical reports in the databases of PubMed and Elsevier ScienceDirect to analyze ionic mechanisms underlying ischemic cell damage and suggest promising ideas for stroke therapy...
October 17, 2017: Journal of Stroke and Cerebrovascular Diseases: the Official Journal of National Stroke Association
https://www.readbyqxmd.com/read/29054705/cistanches-herba-an-overview-of-its-chemistry-pharmacology-and-pharmacokinetics-property
#4
REVIEW
Zhifei Fu, Xiang Fan, Xiaoying Wang, Xiumei Gao
ETHNOPHARMACOLOGICAL RELEVANCE: Cistanches Herba is an Orobanchaceae parasitic plant. As a commonly used Traditional Chinese Medicine (TCM), its traditional functions include treating kidney deficiency, impotence, female infertility and senile constipation. Chemical analysis of Cistanches Herba revealed that phenylethanoid glycosides, iridoids, lignans, oligosaccharides, and polysaccharides were the main constituents. Pharmacological studies demonstrated that Cistanches Herba exhibited neuroprotective, immunomodulatory, hormonal balancing, anti-fatigue, anti-inflammatory, hepatoprotection, anti-oxidative, anti-bacterial, anti-viral, and anti-tumor effects, etc...
October 17, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29054588/titanium-dioxide-nanoparticles-induce-human-eosinophil-adhesion-onto-endothelial-ea-hy926-cells-via-activation-of-phosphoinositide-3-kinase-akt-cell-signalling-pathway
#5
Maxime Murphy-Marion, Denis Girard
The use of nanoparticles (NPs) for developing new therapeutic strategies in a variety of diseases is gaining increasing attention. However, NPs could possess undesired effects, including pro-inflammatory activities. Despite the fact that several studies reported that NPs may induce or exacerbate eosinophilic inflammation in vivo in rodents, the information regarding the direct interaction between NPs and human eosinophils is lacking. In the present study, we test the possibility that NPs could alter the capacity of human eosinophils to adhere onto a cellular substratum...
October 16, 2017: Immunobiology
https://www.readbyqxmd.com/read/29054369/exosome-is-a-mechanism-of-intercellular-drug-transfer-application-of-quantitative-pharmacology
#6
Jin Wang, Bertrand Z Yeung, Minjian Cui, Cody J Peer, Ze Lu, William D Figg, M Guillaume Wientjes, Sukyung Woo, Jessie L-S Au
PURPOSE: Exosomes are small membrane vesicles (30-100nm in diameter) secreted by cells into extracellular space. The present study evaluated the effect of chemotherapeutic agents on exosome production and/or release, and quantified the contribution of exosomes to intercellular drug transfer and pharmacodynamics. METHODS: Human cancer cells (breast MCF7, breast-to-lung metastatic LM2, ovarian A2780 and OVCAR4) were treated with paclitaxel (PTX, 2-1000nM) or doxorubicin (DOX, 20-1000nM) for 24-48h...
October 17, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29053727/impaired-glucose-metabolism-in-subjects-with-the-williams-beuren-syndrome-a-five-year-follow-up-cohort-study
#7
Maria Elena Lunati, Maria Francesca Bedeschi, Veronica Resi, Valeria Grancini, Eva Palmieri, Simona Salera, Faustina Lalatta, Giuseppe Pugliese, Emanuela Orsi
OBJECTIVE: The Williams-Beuren syndrome (WS) is associated with impaired glucose metabolism (IGM) early in adulthood. However, the pathophysiology of IGM remains poorly defined, due to the lack of longitudinal studies investigating the contribution of β-cell dysfunction and impaired insulin sensitivity. This study aimed at assessing incidence of IGM and the underlying mechanisms in WS adults. METHODS: This observational, longitudinal (5-year), cohort study enrolled thirty-one consecutive WS subjects attending a tertiary referral center...
2017: PloS One
https://www.readbyqxmd.com/read/29053717/gpr40-partial-agonists-and-agopams-differentiating-effects-on-glucose-and-hormonal-secretions-in-the-rodent
#8
Michele J Pachanski, Melissa E Kirkland, Daniel T Kosinski, Joel Mane, Boonlert Cheewatrakoolpong, Jiyan Xue, Daphne Szeto, Gail Forrest, Corin Miller, Michelle Bunzel, Christopher W Plummer, Harry R Chobanian, Michael W Miller, Sarah Souza, Brande S Thomas-Fowlkes, Aimie M Ogawa, Adam B Weinglass, Jerry Di Salvo, Xiaoyan Li, Yue Feng, Daniel A Tatosian, Andrew D Howard, Steven L Colletti, Maria E Trujillo
GPR40 agonists are effective antidiabetic agents believed to lower glucose through direct effects on the beta cell to increase glucose stimulated insulin secretion. However, not all GPR40 agonists are the same. Partial agonists lower glucose through direct effects on the pancreas, whereas GPR40 AgoPAMs may incorporate additional therapeutic effects through increases in insulinotrophic incretins secreted by the gut. Here we describe how GPR40 AgoPAMs stimulate both insulin and incretin secretion in vivo over time in diabetic GK rats...
2017: PloS One
https://www.readbyqxmd.com/read/29053689/whole-cell-currents-induced-by-puff-application-of-gaba-in-brain-slices
#9
Yangjian Feng, Binliang Tang, Ming Chen, Li Yang
Pharmacological administration is commonly used when conducting whole-cell patch-clamp recording in brain slices. One of the best methods of drug application during electrophysiological recording is the puff technique, which can be used to study the effect of pharmacological reagents on neuronal activities in brain slices. The greatest advantage of puff application is that the drug concentration around the recording site increases rapidly, thus preventing desensitization of membrane receptors. Successful use of puff application involves careful attention to the following elements: the concentration of the drug, the parameters of the puff micropipette, the distance between the tip of a puff micropipette and the neuron recorded, and the duration and pressure driving the puff (pounds per square inch, psi)...
October 12, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/29053638/neuroprotective-surgical-strategies-in-parkinson-s-disease-role-of-preclinical-data
#10
REVIEW
Napoleon Torres, Jenny Molet, Cecile Moro, John Mitrofanis, Alim Louis Benabid
Although there have been many pharmacological agents considered to be neuroprotective therapy in Parkinson's disease (PD) patients, neurosurgical approaches aimed to neuroprotect or restore the degenerative nigrostriatal system have rarely been the focus of in depth reviews. Here, we explore the neuroprotective strategies involving invasive surgical approaches (NSI) using neurotoxic models 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and 6-hydroxydopamine (6-OHDA), which have led to clinical trials. We focus on several NSI approaches, namely deep brain stimulation of the subthalamic nucleus, glial neurotrophic derived factor (GDNF) administration and cell grafting methods...
October 20, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29053625/traditional-uses-origins-chemistry-and-pharmacology-of-bombyx-batryticatus-a-review
#11
REVIEW
Meibian Hu, Zhijie Yu, Jiaolong Wang, Wenxiang Fan, Yujie Liu, Jianghua Li, He Xiao, Yongchuan Li, Wei Peng, Chunjie Wu
Bombyx batryticatus (B. batryticatus), a well-known traditional animal Chinese medicine, has been commonly used in China for thousands of years. The present paper reviewed advances in traditional uses, origin, chemical constituents, pharmacology and toxicity studies of B. batryticatus. The aim of the paper is to provide more comprehensive references for modern B. batryticatus study and application. In Traditional Chinese Medicine (TCM) culture, drugs containing B. batryticatus have been used to treat convulsions, headaches, skin prurigo, scrofula, tonsillitis and fever...
October 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29053620/self-nanoemulsifying-drug-delivery-systems-containing-plantago-lanceolata-an-assessment-of-their-antioxidant-and-antiinflammatory-effects
#12
Azin Kalantari, Dóra Kósa, Dániel Nemes, Zoltán Ujhelyi, Pálma Fehér, Miklós Vecsernyés, Judit Váradi, Ferenc Fenyvesi, Ákos Kuki, Sándor Gonda, Gábor Vasas, Rudolf Gesztelyi, Anayatollah Salimi, Ildikó Bácskay
The most important components of Plantago lanceolata L. leaves are catalpol, aucubin, and acteoside (=verbascoside). These bioactive compounds possess different pharmacological effects: anti-inflammatory, antioxidant, antineoplastic, and hepatoprotective. The aim of this study was to protect Plantago lanceolata extract from hydrolysis and to improve its antioxidant effect using self-nano-emulsifying drug delivery systems (SNEDDS). Eight SNEDDS compositions were prepared, and their physical properties, in vitro cytotoxicity, and in vivo AST/ALT values were investigated...
October 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29053584/lomefloxacin-induces-oxidative-stress-and-apoptosis-in-colo829-melanoma-cells
#13
Artur Beberok, Dorota Wrześniok, Martyna Szlachta, Jakub Rok, Zuzanna Rzepka, Michalina Respondek, Ewa Buszman
Although some fluoroquinolones have been found to exert anti-tumor activity, studies on the effect of these drugs on melanoma cells are relatively rare. The aim of this study was to examine the effect of lomefloxacin on cell viability, reactive oxygen species production, redox balance, cell cycle distribution, DNA fragmentation, and apoptosis in COLO829 melanoma cells. Lomefloxacin decreases the cell viability in a dose- and time-dependent manner. For COLO829 cells treated with the drug for 24, 48, and 72 h, the values of IC50 were found to be 0...
October 20, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29053268/synthesis-pharmacology-and-molecular-modeling-studies-on-6-desoxo-n-methylmorphinans-as-potent-%C3%A2%C2%B5-opioid-receptor-agonists
#14
Maria Dumitrascuta, Tanila Ben Haddou, Elena Guerrieri, Stefan M Noha, Lea Schläfer, Helmut Schmidhammer, Mariana Spetea
Position 6 of the morphinan skeleton plays a key role on the µ-opioid receptor (MOR) activity in vitro and in vivo. We describe the consequence of the 6-carbonyl group deletion in N-methylmorphinan-6-ones 1-4 on ligand-MOR interaction, signaling and antinociception. While 6-desoxo compounds 1a, 2a and 4a show similar profiles to their 6-keto counterparts, the 6-desoxo-14-benzyloxy substituted 3a displays significantly increased MOR binding and agonist potency, and a distinct binding mode than its analogue 3...
October 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29053217/behavioral-control-by-striatal-a2a-dopamine-d2-receptor-heteromers
#15
Jaume Taura, Marta Valle-León, Kristoffer Sahlholm, Masahiko Watanabe, Katheleen Van Craenenbroeck, Víctor Fernández-Dueñas, Sergi Ferré, Francisco Ciruela
G protein-coupled receptors (GPCR) exhibit the ability to form receptor complexes that include molecularly different GPCR (i.e. GPCR heteromers), which endow them with singular functional and pharmacological characteristics. The relative expression of GPCR heteromers remains a matter of intense debate. Recent studies support that adenosine A2A receptors (A2A R) and dopamine D2 receptors (D2 R) predominantly form A2A R-D2 R heteromers in the striatum. The aim of the present study was evaluating the behavioral effects of pharmacological manipulation and genetic blockade of A2A R and D2 R within the frame of such a predominant striatal heteromeric population...
October 20, 2017: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/29052925/structural-insights-into-natural-compounds-as-inhibitors-of-fasciola-gigantica-thioredoxin-glutathione-reductase
#16
Rohit Shukla, Harish Shukla, Parismita Kalita, Timir Tripathi
Fascioliasis is caused by the helminth parasites of genus Fasciola. Thioredoxin glutathione reductase (TGR) is an important enzyme in parasitic helminths and plays an indispensable role in its redox biology. In the present study, we conducted a structure-based virtual screening of natural compounds against the Fasciola gigantica TGR (FgTGR). The compounds were docked against FgTGR in four sequential docking modes. The screened ligands were further assessed for Lipinski and ADMET prediction so as to evaluate drug proficiency and likeness property...
October 20, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29052798/curcumin-pretreatment-prevents-hydrogen-peroxide-induced-oxidative-stress-through-enhanced-mitochondrial-function-and-deactivation-of-akt-erk-signaling-pathways-in-rat-bone-marrow-mesenchymal-stem-cells
#17
Xujie Wang, Jianxin Gao, Yunchuan Wang, Bin Zhao, Yijie Zhang, Fu Han, Zhao Zheng, Dahai Hu
Bone marrow mesenchymal stem cells (BMSCs)-based therapy has emerged as a desirable modality for the treatment of tissue injury with promising therapeutic effects; however, low survival rate of transplanted cells due to harsh microenvironment with hypoxia and oxidative stress results in hampered therapeutic benefits of this therapy. Curcumin, a natural bioactive product, is a dietary component which has gained increasing attention owing to its beneficial health properties. Here, we reported the protective effects of curcumin pretreatment on BMSCs injury induced by hydrogen peroxide (H2O2), which was used as ROS source of oxidative stress in vitro...
October 20, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/29052674/egfr-targeting-plga-peg-nanoparticles-as-a-curcumin-delivery-system-for-breast-cancer-therapy
#18
Hua Jin, Jiang Pi, Yue Zhao, Jinhuan Jiang, Ting Li, Xueyi Zeng, Peihui Yang, Colin E Evans, Jiye Cai
Poor bioavailability and non-specificity of chemotherapeutic agents are major challenges in breast cancer treatment. Antibodies and small molecules that block cell signaling pathways have shown promise in the clinic, but their application is also limited by the high costs and treatment dosages required. Novel therapies that aim to rapidly and specifically target malignant cells with long-lasting impact in the tumor microenvironment may ultimately improve clinical outcome in cancer patients. Here, we demonstrate that epidermal growth factor receptor (EGFR)-targeting GE11 peptides conjugated with PEGylated polylactic-co-glycolic acid (PLGA) nanoparticles can be used to effectively deliver an anti-cancer agent, curcumin, into EGFR-expressing MCF-7 cells in vitro and in vivo...
October 20, 2017: Nanoscale
https://www.readbyqxmd.com/read/29052400/-protective-effect-of-ginsenoside-rb%C3%A2-on-doxorubicin-induced-myocardial-autophagy
#19
Long-Fei Li, Zeng-Chun Ma, Yu-Guang Wang, Xiang-Lin Tang, Hong-Ling Tan, Cheng-Rong Xiao, Yue Gao
Ginsenoside Rb₁ (Rb₁), which is one of the main ingredients derived from Panax ginseng, has been found to have extensive pharmacological activities including antioxidant, anti-inflammatory, anticancer properties. In this study, the effect of Rb₁ on doxorubicin-induced myocardial autophagy was studied with H9c2 as the study object. CCK-8 method, transmission electron microscope observation, fluorescence staining observation and Western blot were used to detect changes in H9c2 cell proliferation and autophagy after treatment...
April 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29052385/-research-advances-on-baicalin-and-baicalein-as-potential-therapeutic-agents-for-fibrotic-disease
#20
REVIEW
Qing-Jun Zhu
Tissue and organ fibrosis is the major cause for disability and death related to a variety of diseases worldwide. As specific therapies to halt, or even to reverse the existing tissue fibrosis are not yet available, it is of great significance to find new anti-fibrosis therapeutic agents. Tissue and organ fibrosis is a nonphysiological scarring process, associated with excessive deposition of extracellular matrix, and leads to impairment of organ function. Fibrotic lesions of all organs show similar histological abnormalities...
April 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
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