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[PMID]: 29428540
[Au] Autor:Bicker J; Alves G; Fortuna A; Soares-da-Silva P; Falcão A
[Ad] Address:Laboratory of Pharmacology, Faculty of Pharmacy, University of Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal; CNC - Center for Neuroscience and Cell Biology, University of Coimbra, 3004-517 Coimbra, Portugal.
[Ti] Title:In vitro assessment of the interactions of dopamine ß-hydroxylase inhibitors with human P-glycoprotein and Breast Cancer Resistance Protein.
[So] Source:Eur J Pharm Sci;117:35-40, 2018 Feb 08.
[Is] ISSN:1879-0720
[Cp] Country of publication:Netherlands
[La] Language:eng
[Ab] Abstract:Inhibition of the biosynthesis of noradrenaline is a currently explored strategy for the treatment of hypertension, congestive heart failure and pulmonary arterial hypertension. While some dopamine ß-hydroxylase (DBH) inhibitors cross the blood-brain barrier (BBB) and cause central as well as peripheral effects (nepicastat), others have limited access to the brain (etamicastat, zamicastat). In this context, peripheral selectivity is clinically advantageous, in order to prevent alterations of noradrenaline levels in the CNS and the occurrence of adverse central effects. A limited brain exposure results from the combination of several factors, such as a reduced passive permeability or affinity for efflux transporters, but efflux liabilities may also lead to unwanted drug-drug interactions (DDIs) in the presence of co-administered substrates or inhibitors. Thus, the purpose of the study herein presented was to explore the interaction of P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP), the two major efflux transporters of the BBB that hamper the entry of several drugs to the brain, with the DBH inhibitors, etamicastat, nepicastat and zamicastat. Madin-Darby canine kidney cells (MDCK II) and transfected lines with human MDR1 (MDCK-MDR1) and ABCG2 (MDCK-BCRP) genes were used as a BBB surrogate model. P-gp and BCRP substrates and/or inhibitors were identified through intracellular accumulation and bidirectional permeability assays. The obtained data revealed that zamicastat is a concentration-dependent dual P-gp and BCRP inhibitor with IC values of 73.8 ±â€¯7.2 µM and 17.0 ±â€¯2.7 µM, while etamicastat and nepicastat inhibited BCRP to greater extent than P-gp, with IC values of 47.7 ±â€¯1.8 µM and 59.2 ±â€¯9.4 µM, respectively. Additionally, etamicastat was identified as P-gp and BCRP dual substrate, as demonstrated by net flux ratios of 5.84 and 3.87 and decreased >50% by verapamil and Ko143. Conversely, nepicastat revealed to be a P-gp-only substrate, with a net flux ratio of 2.01, reduced to 0.92 in the presence of verapamil. Furthermore, nepicastat displayed a consistently higher apparent permeability (>8.49 × 10 cm s ) than etamicastat (<0.58 × 10 cm s ). The identification of etamicastat as a dual efflux substrate suggests that P-gp and BCRP may be partially responsible for the limited central exposure of this compound, in association with its low passive permeability. Moreover, the weak efflux inhibitory potencies of etamicastat and nepicastat revealed a low DDI risk, while the dual P-gp/BCRP inhibition of zamicastat could be studied in the future with synergically effluxed compounds, for which BBB penetration is severely impaired.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1802
[Cu] Class update date: 180310
[Lr] Last revision date:180310
[St] Status:Publisher

  2 / 25069 MEDLINE  
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[PMID]: 29269687
[Au] Autor:Hirano T; Kaneda T; Ozaki H; Hori M
[Ad] Address:Department of Veterinary Pharmacology, Graduate School of Agriculture and Life Sciences, The University of Tokyo, Bunkyo-ku, Tokyo 113-8657, Japan.
[Ti] Title:Angiotensin II, a unique vasoactive agent dissociates myosin light chain phosphorylation from contraction.
[So] Source:J Vet Med Sci;80(2):219-224, 2018 Feb 09.
[Is] ISSN:1347-7439
[Cp] Country of publication:Japan
[La] Language:eng
[Ab] Abstract:Angiotensin II (100 nM) induced bi-phasic increases in cytosolic Ca level ([Ca ] ) through the activation of angiotensin II type 1 receptor. Pharmacological examinations using 10 µM verapamil, 30 µM La , and 1 µM thapsigargin indicated that the first phase of the [Ca ] -increase was mediated by Ca release from sarcoplasmic reticulum (SR) and Ca influx independently of voltage dependent Ca channel (VDC). In contrast, the second phase of [Ca ] -increase was mediated by Ca influx through VDC. Although both [Ca ] and myosin light chain (MLC)-phosphorylation at the first phase was apparently exceeded the threshold for contraction as estimated by high K -induced responses, there was no appreciable contraction, indicating the dissociation between MLC phosphorylation and force during this phase. In contrast, the second phase of [Ca ] was associated with the increases in both MLC phosphorylation and force. These results suggest that angiotensin II is a unique agonist which dissociates MLC-phosphorylation from muscle force during the Ca releases from SR.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1712
[Cu] Class update date: 180311
[Lr] Last revision date:180311
[St] Status:In-Process
[do] DOI:10.1292/jvms.17-0415

  3 / 25069 MEDLINE  
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[PMID]: 29523051
[Au] Autor:Gowarty JL; Herrington JD
[Ad] Address:Scott and White Medical Center-Temple, Temple, TX, USA.
[Ti] Title:Verapamil as a culprit of palbociclib toxicity.
[So] Source:J Oncol Pharm Pract;:1078155218761798, 2018 Jan 01.
[Is] ISSN:1477-092X
[Cp] Country of publication:England
[La] Language:eng
[Ab] Abstract:A promising drug, palbociclib, received accelerated approval as a first line treatment when used with the aromatase inhibitor, letrozole, for postmenopausal women with hormone receptor positive advanced or metastatic breast cancer. We report a case of a patient who presented with febrile neutropenia, grade 3 stomatitis with lip swelling, periorbital edema, and transaminitis while on palbociclib and verapamil. Labs normalized upon discontinuation of verapamil and our patient was able to continue treatment with palbociclib and letrozole. Verapamil's inhibition of both permeability-glycoprotein (P-gp) and CYP3A4 is suspected to have led to the adverse side effects seen in our patient.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1803
[Cu] Class update date: 180310
[Lr] Last revision date:180310
[St] Status:Publisher
[do] DOI:10.1177/1078155218761798

  4 / 25069 MEDLINE  
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[PMID]: 29521222
[Au] Autor:Mukkavilli R; Jadhav G; Vangala S
[Ad] Address:Georgia State University, Atlanta, GA 30303. United States.
[Ti] Title:Evaluation of Drug Transport in MDCKII-Wild Type, MDCKII-MDR1, MDCKII-BCRP and Caco-2 Cell Lines.
[So] Source:Curr Pharm Biotechnol;, 2018 Mar 07.
[Is] ISSN:1873-4316
[Cp] Country of publication:Netherlands
[La] Language:eng
[Ab] Abstract:BACKGROUND: Drug transporters function as gatekeepers and modulate drug access into the body and various tissues. Thus a thorough and precise understanding of transporter liability for compound uptake and efflux is critical during drug development. METHODS: In the present study, we assessed the apparent permeability (Papp) and compared the efflux ratio of various compounds in stably transfected Madin-Darby Canine Kidney (MDCKII) cells overexpressing human P-gp (MDCKII-P-gp), human BCRP (MDCKII-BCRP), wild type (MDCKII-WT), and Caco-2 cell monolayers. RESULTS: We observed that quinidine, a substrate for P-gp transporter, showed efflux ratio (Papp B-A/Papp A-B) of 838 in MDCKII-P-gp cells which plummeted to 14 in presence of verapamil, a known inhibitor of P-gp. With MDCKII-WT cells, Papp of quinidine dropped from 2 to 1, in the presence of verapamil. Caco-2 cells showed a diminutive decrease in efflux ratio of quinidine from 2.5 to 1.6 by verapamil. Prazosin and dantrolene were evaluated in MDCKII-BCRP cells and were found to have 80-fold higher efflux ratio compared to MDCKII-WT cells. In Caco-2 cells, prazosin and dantrolene showed efflux ratio of 4 and 2, respectively. Rhodamine-123, a fluorogenic probe substrate of P-gp showed efflux ratio of 4 in Caco-2 cells and BCRP substrate estrone-3-sulphate showed an efflux ratio of 7. In presence of BCRP inhibitor fumitremorgin-c, the efflux ratio of estrone-3-sulfate dropped to 1 in Caco-2 cells. CONCLUSION: The very high efflux ratios of P-gp and BCRP substrates in transfected MDCKII cells clearly demonstrate the potential usefulness of these models to provide more definitive data to evaluate the transporter involvement compared to Caco-2 or MDCKII-WT cells.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1803
[Cu] Class update date: 180309
[Lr] Last revision date:180309
[St] Status:Publisher
[do] DOI:10.2174/1389201019666180308091855

  5 / 25069 MEDLINE  
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[PMID]: 29215340
[Au] Autor:Yakut K; Erdogan I; Varan B; Atar I
[Ad] Address:Department of Pediatric Cardiology, Baskent University Ankara Hospital, Ankara, Turkey.
[Ti] Title:A Report of Brugada Syndrome Presenting with Cardiac Arrest Triggered by Verapamil Intoxication.
[So] Source:Balkan Med J;34(6):576-579, 2017 12 01.
[Is] ISSN:2146-3131
[Cp] Country of publication:Turkey
[La] Language:eng
[Ab] Abstract:BACKGROUND: Brugada syndrome is a disease characterized by a specific electrocardiographic pattern and an increased risk of sudden cardiac death. We present this case with the updated literature to emphasise the need to consider the diagnosis of Brugada syndrome in patients admitted to the emergency ward with sudden cardiac arrest. CASE REPORT: A 16-year-old female patient was admitted to the emergency ward with complaints of weakness and abdominal pain, and she had four cardiac arrests during her evaluation period. She was referred to our clinic for permanent pacemaker implantation. She was on a temporary pace maker after having had C-reactive protein. Her physical exam was normal except for bilaterally decreased lung sounds. Lung x-ray and computed tomography, which were performed by another institution, revealed minimal pleural effusion and nothing else of significance. Blood and peritoneal fluid samples were sterile. Echocardiographic exam and cardiac enzymes were also in the normal ranges. Electrocardiographic showed incomplete right branch block in leads V1 and V2. An ajmaline test revealed specific electrocardiographic findings of the type I Brugada pattern. We proposed implanting an implantable cardioverter defibrillator to the patient as there were positive findings on the ajmaline test as well as a history of sudden cardiac arrest. After this treatment proposal, the patient's family admitted that she had taken a high dose of verapamil and thus, the encountered bradycardia was associated with verapamil overuse. The ajmaline test was repeated as it was contemplated that the previous positive ajmaline test had been associated with verapamil overuse. Implantable cardioverter defibrillator implantation was proposed again as there was a history of sudden cardiac arrest; however, the family did not consent to implantable cardioverter defibrillator, and the patient was discharged and followed up. CONCLUSION: Brugada syndrome should be considered for patients who are admitted to the emergency ward with sudden cardiac arrest though surface electrocardiographic is normal. If there is a suspicion of Brugada syndrome, repeated electrocardiographic should be performed on different occasions. Diagnosis can be clarified by upper costal electrocardiographic or by administering Na channel blockers during electrocardiographic performance.
[Mh] MeSH terms primary: Anti-Arrhythmia Agents/poisoning
Brugada Syndrome/chemically induced
Heart Arrest/chemically induced
Verapamil/poisoning
[Mh] MeSH terms secundary: Adolescent
Ajmaline/pharmacology
Brugada Syndrome/diagnosis
Brugada Syndrome/physiopathology
Diagnosis, Differential
Electrocardiography
Female
Genetic Testing
Heart Arrest/physiopathology
Humans
Precipitating Factors
Sodium Channel Blockers/administration & dosage
Suicide, Attempted
Treatment Outcome
[Pt] Publication type:CASE REPORTS; JOURNAL ARTICLE
[Nm] Name of substance:0 (Anti-Arrhythmia Agents); 0 (Sodium Channel Blockers); 1PON08459R (Ajmaline); CJ0O37KU29 (Verapamil)
[Em] Entry month:1801
[Cu] Class update date: 180308
[Lr] Last revision date:180308
[Js] Journal subset:IM
[Da] Date of entry for processing:171208
[St] Status:MEDLINE
[do] DOI:10.4274/balkanmedj.2016.1301

  6 / 25069 MEDLINE  
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[PMID]: 28954371
[Au] Autor:Ajima MNO; Pandey PK; Kumar K; Poojary N
[Ad] Address:Department of Fisheries and Aquaculture Technology, Federal University of Technology, Owerri, Nigeria. Electronic address: malajimo@gmail.com.
[Ti] Title:Alteration in DNA structure, molecular responses and Na -K -ATPase activities in the gill of Nile tilapia, Oreochromis niloticus (Linnaeus, 1758) in response to sub-lethal verapamil.
[So] Source:Ecotoxicol Environ Saf;147:809-816, 2018 Jan.
[Is] ISSN:1090-2414
[Cp] Country of publication:Netherlands
[La] Language:eng
[Ab] Abstract:The ecotoxicological consequences of residues from pharmaceutical drugs on aquatic biota have necessitated the development of sensitive and reliable techniques to assess the impact of these xenobiotics on aquatic organisms. This study investigated the alteration in DNA structure, molecular responses and the activities of Na -K -ATPase and antioxidant enzymes in the gill of Nile tilapia, Oreochromis niloticus, exposed to long-term effects at the concentrations (0.14, 0.28 and 0.57mgL ) of verapamil in static renewal system for 15, 30, 45 and 60 days. Evaluation of DNA structure, using single cell gel electrophoresis, revealed certain degree of DNA damages in the gill in a time and concentration-dependent relationship. Transcription of mRNA of superoxide dismutase (sod), catalase (cat) and heat shock protein (hsp70) genes in the gill of the fish showed the genes were up-regulated. Na -K -ATPase activity was inhibited in a concentration and time dependent manner. The indices of oxidative stress biomarkers (lipid peroxidation and carbonyl protein) as well as superoxide dismutase, glutathione peroxidase, glutathione-S-transferase were elevated in the treated fish in comparison to the control. Further, the level of reduced glutathione and catalase activity were inhibited at 0.28mgL after day 30. Long-term exposure to sub-lethal concentration of verapamil can cause DNA damages, molecular effects and oxidative stress in O. niloticus. The biomarkers analysed can be used as early warning signals in environmental biomonitoring and assessment of drug contamination in aquatic ecosystem.
[Mh] MeSH terms primary: Cichlids/metabolism
DNA Damage
Gills/drug effects
Sodium-Potassium-Exchanging ATPase/metabolism
Verapamil/toxicity
Water Pollutants, Chemical/toxicity
[Mh] MeSH terms secundary: Animals
Antioxidants/metabolism
Biomarkers/metabolism
Cichlids/genetics
Dose-Response Relationship, Drug
Environmental Monitoring/methods
Gills/metabolism
Oxidative Stress/drug effects
Verapamil/metabolism
Water Pollutants, Chemical/metabolism
[Pt] Publication type:JOURNAL ARTICLE
[Nm] Name of substance:0 (Antioxidants); 0 (Biomarkers); 0 (Water Pollutants, Chemical); CJ0O37KU29 (Verapamil); EC 3.6.3.9 (Sodium-Potassium-Exchanging ATPase)
[Em] Entry month:1803
[Cu] Class update date: 180308
[Lr] Last revision date:180308
[Js] Journal subset:IM
[Da] Date of entry for processing:170929
[St] Status:MEDLINE

  7 / 25069 MEDLINE  
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[PMID]: 29517223
[Au] Autor:Yang CH; Wang C; Ojima I; Horwitz SB
[Ad] Address:Department of Molecular Pharmacology , Albert Einstein College of Medicine , Bronx , New York 10461 , United States.
[Ti] Title:Taxol Analogues Exhibit Differential Effects on Photoaffinity Labeling of ß-Tubulin and the Multidrug Resistance Associated P-Glycoprotein.
[So] Source:J Nat Prod;, 2018 Mar 08.
[Is] ISSN:1520-6025
[Cp] Country of publication:United States
[La] Language:eng
[Ab] Abstract:Several next-generation taxanes have been reported to possess high potency against Taxol-resistant cancer cell lines overexpressing ßIII-tubulin and/or P-glycoprotein (P-gp), both of which are involved in drug resistance. Using a photoaffinity Taxol analogue, 2-( m-azidobenzoyl)taxol, two potent next-generation taxanes, SB-T-1214 and SB-CST-10202, exhibited distinct inhibitory effects on photolabeling of ß-tubulin from different eukaryotic sources that differ in ß-tubulin isotype composition. They also specifically inhibited photolabeling of P-gp, and the inhibitory effect correlated well with the steady-state accumulation of [ H]vinblastine in a multidrug resistant (MDR) cell line, SKVLB1. Several microtubule-stabilizing agents (MSAs)-resistant cell lines from the human ovarian cancer cell line Hey were isolated, and their MDR1 and ßIII-tubulin levels determined. Distinct potencies of the two taxanes against different MSA-resistant cells expressing unique levels of MDR1 and ßIII-tubulin were found. Cytotoxicity assays, done in the presence of verapamil, indicated that SB-T-1214 is a substrate, although not as good as Taxol, for P-gp. The mechanisms involved in drug resistance are multifactorial, and the effectiveness of new Taxol analogues depends on the interaction between the drugs and all possible targets; in this case the two major cellular targets are ß-tubulin and P-gp.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1803
[Cu] Class update date: 180308
[Lr] Last revision date:180308
[St] Status:Publisher
[do] DOI:10.1021/acs.jnatprod.7b01047

  8 / 25069 MEDLINE  
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[PMID]: 29442035
[Au] Autor:Incecayir T; Ilbasmis-Tamer S; Tirnaksiz F; Degim T
[Ti] Title:Assessment of the potential drug-drug interaction between carvedilol and clopidogrel mediated through intestinal P-glycoprotein.
[So] Source:Pharmazie;71(8):472-477, 2016 08 01.
[Is] ISSN:0031-7144
[Cp] Country of publication:Germany
[La] Language:eng
[Ab] Abstract:The most widely prescribed oral antiplatelet agent, clopidogrel, shows high interindividual variability resulting in an increased risk of cardiovascular events in the patients with reduced platelet inhibition. The purpose of this study was to investigate the role of the P-glycoprotein (P-gp) efflux pump in limiting the intestinal permeability of clopidogrel and the effect of a ß-blocker, namely, carvedilol, on its intestinal transport. Effective permeabilities (Peff) of clopidogrel and carvedilol were investigated in the proximal jejunum and distal ileum of rats using an in situ intestinal perfusion model. Peff values of clopidogrel and carvedilol were found to be concentration dependent with decreased Peff values at the low perfusate concentrations. Coperfusion with the P-gp inhibitors verapamil (100 µM) and carvedilol (10 µM) significantly increased the Peff of clopidogrel in the jejunum (8.31±0.20 x 10-5 and 6.98±0.75 x 10-5 vs. 3.60±0.51 x 10-5, respectively) and ileum (9.08±2.19 x 10-5 and 8.35±1.58 x 10-5 vs. 3.85±0.15 x 10-5, respectively). However, at the highest concentration tested (30 µM), clopidogrel exhibited 3 and 1.4 times higher Peff than those of metoprolol, an FDA high permeability reference standard, in the jejunum and ileum, respectively. Overall, this study indicates that the efflux function appears not to have a significant impact on the in vivo intestinal absorption of clopidogrel due to the saturation of P-gp, suggesting no clinically relevant interaction between carvedilol and clopidogrel mediated through P-gp at intestinal level.
[Mh] MeSH terms primary: ATP-Binding Cassette, Sub-Family B, Member 1/drug effects
Adrenergic beta-Antagonists/pharmacology
Carbazoles/pharmacology
Intestine, Small/drug effects
Platelet Aggregation Inhibitors/pharmacology
Propanolamines/pharmacology
Ticlopidine/analogs & derivatives
[Mh] MeSH terms secundary: ATP-Binding Cassette, Sub-Family B, Member 1/antagonists & inhibitors
Animals
Drug Interactions
Intestinal Absorption/drug effects
Intestine, Small/metabolism
Male
Metoprolol/pharmacology
Perfusion
Permeability/drug effects
Rats
Rats, Wistar
Ticlopidine/pharmacology
Verapamil/pharmacology
[Pt] Publication type:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Name of substance:0 (ATP-Binding Cassette, Sub-Family B, Member 1); 0 (Adrenergic beta-Antagonists); 0 (Carbazoles); 0 (Platelet Aggregation Inhibitors); 0 (Propanolamines); 0K47UL67F2 (carvedilol); A74586SNO7 (clopidogrel); CJ0O37KU29 (Verapamil); GEB06NHM23 (Metoprolol); OM90ZUW7M1 (Ticlopidine)
[Em] Entry month:1803
[Cu] Class update date: 180307
[Lr] Last revision date:180307
[Js] Journal subset:IM
[Da] Date of entry for processing:180215
[St] Status:MEDLINE
[do] DOI:10.1691/ph.2016.6059

  9 / 25069 MEDLINE  
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[PMID]: 29473523
[Au] Autor:Etchegoyen CV; Keller GA; Mrad S; Cheng S; Di Girolamo G
[Ad] Address:Universidad de Buenos Aires - Pharmacology Ciudad Autonoma de Buenos Aires, Buenos Aires. Argentina.
[Ti] Title:Drug-induced QT Interval prolongation in the Intensive Care Unit.
[So] Source:Curr Clin Pharmacol;, 2018 02 23.
[Is] ISSN:2212-3938
[Cp] Country of publication:United Arab Emirates
[La] Language:eng
[Ab] Abstract:Drug-induced QT interval prolongation is the most frequent cause of Long QT syndrome (LQTS) in the clinical practice. This electrophysiological entity, produced by an extended duration of the myocardial repolarization and reflected as a prolonged QT interval in the superficial electrocardiogram (EKG), increases the risk of polymorphic ventricular tachycardia (Torsades de Pointes) appearance and sudden death. Certain antiarrhythmic drugs such as amiodarone, sotalol, quinidine, procainamide, verapamil and diltiazem are known as drugs that, due to their mechanism of action, prolong the QT interval, demanding constant monitorization. Nevertheless there are other widely used drugs in the Intensive Care Unit (ICU) that have no cardiovascular indication but still are frequently associated with prolonged QT interval such as ondansetron, like macrolides and fluoroquinolones , typical antipsychotic such as haloperidol and thioridazine or atypical such as sertindole. Taking into consideration this unexpected association with the prolongation of the QT interval, these drugs require a closed monitorization in these critical patients. Since ICU patients are particularly vulnerable to this sort of alteration of ventricular repolarization caused by the effect of these drugs itselves or by pharmacological interaction with other medication, which can generate extension of the QT interval as well as other clinical presentation associated with the risk of developing Torsades de Point, the strict and closed control of physicians in charge must be on a daily basis.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1802
[Cu] Class update date: 180307
[Lr] Last revision date:180307
[St] Status:Publisher
[do] DOI:10.2174/1574884713666180223123947

  10 / 25069 MEDLINE  
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[PMID]: 29193364
[Au] Autor:Zheng Q; Tang Y; Hu PY; Liu D; Zhang D; Yue P; Guo Y; Yang M
[Ad] Address:Key Laboratory of Modern Preparation of Traditional Chinese Medicine, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang, 330004, China.
[Ti] Title:The influence and mechanism of ligustilide, senkyunolide I, and senkyunolide A on echinacoside transport through MDCK-MDR1 cells as blood-brain barrier in vitro model.
[So] Source:Phytother Res;32(3):426-435, 2018 Mar.
[Is] ISSN:1099-1573
[Cp] Country of publication:England
[La] Language:eng
[Ab] Abstract:Efficient transcytosis across the blood-brain-barrier is an important strategy for accessing drug targets within the central nervous system. Ligusticum chuanxiong Hort. was used as a messenger drug to increase the distribution of drugs in brain tissue in Traditional Chinese Medicine. The present study investigates the transport of echinacoside (ECH) through MDCK-MDR1 cell and the effects of ligustilide (LIG), senkyunolide A (SENA) and senkyunolide I (SENI) in chuanxiong on its transport. The results indicated that the absorption of ECH was relatively poor in MDCK-MDR1cells, and was concentration dependent and not saturable. The P-glycoprotein inhibitor verapamil could significantly increase the transport of ECH. It indicated that the transport mechanism might be passive diffusion as the dominating process with the active transportation mediated mechanism involved. The increased apparent permeability of ECH in A â†’ B direction by ethylenediaminetetraacetic acid-Na suggested that ECH was absorbed via the paracellular route. The transport of ECH in A â†’ B direction significantly increased when co-administrated with increasing concentrations of LIG, SENI and SENA. Western blot analysis and a decrease in transepithelial electrical resistance during the permeation experiment indicated that LIG, SENI and SENA had enhanced the transport of ECH in the BBB models attribute to down-regulate the expressions of claudin-5 and zonula occludens-1 expression.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1712
[Cu] Class update date: 180306
[Lr] Last revision date:180306
[St] Status:In-Process
[do] DOI:10.1002/ptr.5985


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