scholarly journals Optical assessment of the cardiac rhythm of contracting cardiomyocytes in vitro and a pulsating heart in vivo for pharmacological screening

2014 ◽  
Vol 5 (5) ◽  
pp. 1616 ◽  
Author(s):  
Yu-Cheng Lai ◽  
Wei-Tien Chang ◽  
Kuen-You Lin ◽  
Ian Liau
Keyword(s):  
Cardiac Rhythm ◽  
Pharmacological Screening

scholarly journals Evaluation of Plant Phenolic Metabolites as a Source of Alzheimer's Drug Leads

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Yara Hassaan ◽  
Heba Handoussa ◽  
Ahmed H. El-Khatib ◽  
Michael W. Linscheid ◽  
Nesrine El Sayed ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Amyloid Beta ◽  
Epidemiological Studies ◽  
Aqueous Alcohol ◽  
Alcohol Extract ◽  
Y Maze ◽  
Pharmacological Screening

Epidemiological studies have proven an association between consumption of polyphenols and prevention of Alzheimer’s disease, the most common form of dementia characterized by extracellular deposition of amyloid beta plaques. The aim of this study is pharmacological screening of the aqueous alcohol extract ofMarkhamia platycalyxleaves,Schotia brachypetalaleaves and stalks, and piceatannol compared to aqueous alcohol extract ofCamellia sinensisleaves as potential Alzheimer’s disease drugs. LC-HRESI(-ve)-MSnwas performed to identify phenolics’ profile ofSchotia brachypetalastalks aqueous alcohol extract and revealed ten phenolic compounds as first report: daidzein, naringin, procyanidin isomers, procyanidin dimer gallate, quercetin 3-O-rhamnoside, quercetin 3-O-glucuronide, quercetin hexose gallic acid, quercetin hexose protocatechuic acid, and ellagic acid. Alzheimer’s disease was induced by a single intraperitoneal injection of LPS. Adult male Swiss albino mice were divided into groups of 8–10 mice each receiving treatment for six days.In vivobehavioral tests (Y maze and object recognition) andin vitroestimation of amyloid beta 42 by ELISA showed significant differences between results of treated and nontreated animals.

scholarly journals Design, Synthesis and Characterization of Some Novel benzamide derivatives and it's Pharmacological Screening

2020 ◽  
pp. 68-74 ◽  
Author(s):  
Akshay R. Yadav ◽  
Shrinivas K. Mohite
Keyword(s):  
Chemical Structure ◽  
Design Synthesis ◽  
Different Types ◽  
Anti Inflammatory ◽  
Benzoyl Isothiocyanate ◽  
Pharmacological Screening ◽  
Benzamide Derivatives

The new series of substituted N-(phenylcarbamothioyl)benzamide derivatives (2a-2f) was designed, development and synthesized by using conventional and microwave method. In present work 6 different N-(phenylcarbamothioyl)benzamide were synthesized. Substituted benzoyl chloride is converted into benzoyl isothiocyanate by esterification. Benzoyl isothiocyanate is converted into Substituted (phenylcarbamothioyl)benzamide by treating with different types of substituted aniline. Confirmation of the chemical structure of the synthesized was substantiated by TLC, IR, 1H NMR, MS spectroscopy.Novel synthesized compounds screened for their in vivo and in-vitro anti-inflammatory studies and compound 2f shows promising anti-inflammatory activity.

Fibroblast growth factor-23 promotes rhythm alterations and contractile dysfunction in adult ventricular cardiomyocytes

2019 ◽  
Vol 34 (11) ◽  
pp. 1864-1875 ◽  
Author(s):  
José Alberto Navarro-García ◽  
Carmen Delgado ◽  
María Fernández-Velasco ◽  
Almudena Val-Blasco ◽  
Elena Rodríguez-Sánchez ◽  
...  
Keyword(s):  
Growth Factor ◽  
Fibroblast Growth Factor ◽  
Cardiac Rhythm ◽  
Fibroblast Growth ◽  
Premature Ventricular Contractions ◽  
Ec Coupling ◽  
Ventricular Cardiomyocytes ◽  
Fgf 23

Abstract Background Cardiac dysfunction and arrhythmia are common and onerous cardiovascular events in end-stage renal disease (ESRD) patients, especially those on dialysis. Fibroblast growth factor (FGF)-23 is a phosphate-regulating hormone whose levels dramatically increase as renal function declines. Beyond its role in phosphorus homeostasis, FGF-23 may elicit a direct effect on the heart. Whether FGF-23 modulates ventricular cardiac rhythm is unknown, prompting us to study its role on excitation–contraction (EC) coupling. Methods We examined FGF-23 in vitro actions on EC coupling in adult rat native ventricular cardiomyocytes using patch clamp and confocal microscopy and in vivo actions on cardiac rhythm using electrocardiogram. Results Compared with vehicle treatment, FGF-23 induced a significant decrease in rat cardiomyocyte contraction, L-type Ca2+ current, systolic Ca2+ transients and sarcoplasmic reticulum (SR) load and SR Ca2+-adenosine triphosphatase 2a pump activity. FGF-23 induced pro-arrhythmogenic activity in vitro and in vivo as automatic cardiomyocyte extracontractions and premature ventricular contractions. Diastolic spontaneous Ca2+ leak (sparks and waves) was significantly increased by FGF-23 via the calmodulin kinase type II (CaMKII)-dependent pathway related to hyperphosphorylation of ryanodine receptors at the CaMKII site Ser2814. Both contraction dysfunction and spontaneous pro-arrhythmic Ca2+ events induced by FGF-23 were blocked by soluble Klotho (sKlotho). Conclusions Our results show that FGF-23 reduces contractility and enhances arrhythmogenicity through intracellular Ca2+ mishandling. Blocking its actions on the heart by improving sKlotho bioavailability may enhance cardiac function and reduce arrhythmic events frequently observed in ESRD.

Interference of GSM mobile phones with communication between Cardiac Rhythm Management devices and programmers: A combined in vivo and in vitro study

2015 ◽  
Vol 36 (5) ◽  
pp. 367-376 ◽  
Author(s):  
Dong Huang ◽  
Zhi-Feng Dong ◽  
Yan Chen ◽  
Fa-Bin Wang ◽  
Zhi Wei ◽  
...  
Keyword(s):  
Mobile Phones ◽  
Cardiac Rhythm ◽  
In Vitro Study ◽  
Vitro Study

scholarly journals The synthesis and the antioxidant activity of 1-phenoxymethyl-4-aryl-5,6,7,8-tetrahydro-2a,4a,8a-triazacyclopenta[cd]azulene-3-carboxylic (or carbothionic) acid derivatives

Pharmacia ◽  
2021 ◽  
Vol 68 (1) ◽  
pp. 251-258
Author(s):  
Sergii Demchenko ◽  
Hanna Yeromina ◽  
Yulia Fedchenkova ◽  
Zinaida Ieromina ◽  
Vitaliy Yaremenko ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
Carboxylic Acid ◽  
In Silico ◽  
Pharmacokinetic Profile ◽  
High Antioxidant Activity ◽  
Pharmacological Screening

New 1-phenoxymethyl-4-aryl-5,6,7,8-tetrahydro-2а,4a,8a-triazacyclopenta[cd]azulene-3-carboxylic (or carbothionic) acid derivatives have been designed, synthesized and evaluated for their in vitro antioxidant activity under conditions of the artificial oxidative stress using ionol, ascorbic acid and α-tocopherol as the reference drugs. It has been found that 1-phenoxymethyl-4-aryl-5,6,7,8-tetrahydro-2а,4a,8a-triazacyclopenta[cd]azulene-3-carbothionic acid derivatives 9b, 9c, 9d, 9e, 9f, 9i and 1-phenoxymethyl-4-(41-chlorophenyl)-5,6,7,8-tetrahydro-2,2a,8-triazacyclopenta[cd]azulene-3-carboxylic acid phenylamide 10 reveal a high antioxidant activity and a good in silico pharmacokinetic profile. The data obtained allowed us to select the most promising objects from the substances synthesized for further pharmacological screening for the presence of the antioxidant activity in vivo.

scholarly journals Modulation of TRPV-1 by prostaglandin-E2 and bradykinin changes cough sensitivity and autonomic regulation of cardiac rhythm in healthy subjects

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Filippo Liviero ◽  
Maria Cristina Scarpa ◽  
Diego De Stefani ◽  
Franco Folino ◽  
Manuela Campisi ◽  
...  
Keyword(s):  
Sympathetic Activity ◽  
Healthy Subjects ◽  
Cardiac Rhythm ◽  
Autonomic Regulation ◽  
Prostaglandin E ◽  
Double Blind ◽  
Diesel Exhaust Particulate ◽  
Cough Response

Abstract A neurogenic pathway, involving airway TRPV-1, has been implicated in acute cardiovascular events occurring after peaks of air pollution. We tested whether inhaled prostaglandin-E2 (PGE2) and bradykinin (BK) regulate TRPV-1 activity in vivo by changing cough response to capsaicin (CPS) and affecting heart rate variability (HRV), while also taking into account the influence of TRPV-1 polymorphisms (SNPs). Moreover, we assessed the molecular mechanism of TRPV-1 modulation in vitro. Seventeen healthy volunteers inhaled 100 μg PGE2, 200 μg BK or diluent in a randomized double-blind fashion. Subsequently, the response to CPS was assessed by cough challenge and the sympathetic activity by HRV, expressed by low (nLF) and high (nHF) normalized frequency components, as well as nLF/nHF ratio. Intracellular [Ca2+] was measured in HeLa cells, transfected with wild-type TRPV-1, pre-treated with increasing doses of PGE2, BK or diesel exhaust particulate (DEP), after CPS stimulation. Six functional TRPV-1 SNPs were characterized in DNA from each subject. Inhalation of PGE2 and BK was associated with significant increases in cough response induced by 30 μM of CPS (cough number after PGE2 = 4.20 ± 0.42; p < 0.001, and after BK = 3.64 ± 0.37; p < 0.01), compared to diluent (2.77 ± 0.29) and in sympathetic activity (nLF/nHF ratio after PGE2 = 6.1; p < 0.01, and after BK = 4.2; p < 0.05), compared to diluent (2.5–3.3). No influence of SNPs was observed on autonomic regulation and cough sensitivity. Unlike PGE2 and BK, DEP directly activated TRPV-1. Inhalation of PGE2 and BK sensitizes TRPV-1 and is associated with autonomic dysregulation of cardiac rhythm in healthy subjects.

scholarly journals PHYTOCHEMICAL SCREENING AND ANTIDIABETIC, ANTIHYPERLIPIDEMIC PROPERTIES OF LEAVES OF Filicium decipiens IN STREPTOZOTOCIN INDUCED DIABETIC RATS.

2019 ◽  
Vol 9 (5) ◽  
pp. 62-66
Author(s):  
Elias Akila ◽  
C Geetha Priya
Keyword(s):  
Ethanolic Extract ◽  
Soxhlet Extraction ◽  
Ethanol Extract ◽  
Diabetic Rats ◽  
In Vivo Studies ◽  
Phytochemical Screening ◽  
Pharmacological Screening ◽  
Selection Of

The Present study was undertaken with a view to evaluate the Phytochemical & Pharmacological activities of the leaves of Filicium decipiens (Sapindaceae).  The shade dried powdered plant material was subjected to successive soxhlet extraction with Petroleum Ether, Chloroform, Ethyl acetate and Ethanol. The various extracts were then subjected to preliminary phytochemical screening which revealed the presence of flavanoids, saponins, tannins, phenols, sugars, lipids, alkaloids & steroids. Selection of active extract for in vivo studies was based on preliminary phytochemical tests and in vitro glucose diffusion inhibition potential and accordingly ethanolic and chloroform extracts were chosen for further studies. Pharmacological screening included evaluation of antidiabetic and hypolipidemic activity of chloroform and ethanolic extracts (200mg/kg b.w) on Streptozotocin induced diabetic rats. The ethanolic extract was found to be more effective and brought about significant antidiabetic & hypolipidemic potential. This was due to the presence of one or more phytoconstituents present in ethanol extract. Thus, the present study validates the traditional claim of the plant and endorses a scientific proof in future.

Brain-on-a-chip Devices for Drug Screening and Disease Modeling Applications

2019 ◽  
Vol 24 (45) ◽  
pp. 5419-5436 ◽  
Author(s):  
Beatrice Miccoli ◽  
Dries Braeken ◽  
Yi-Chen Ethan Li
Keyword(s):  
Animal Models ◽  
Neurodegenerative Diseases ◽  
Drug Screening ◽  
Disease Modeling ◽  
New Drugs ◽  
Screening Process ◽  
Pharmacological Screening ◽  
The Brain

:Neurodegenerative disorders are related to the progressive functional loss of the brain, often connected to emotional and physical disability and, ultimately, to death. These disorders, strongly connected to the aging process, are becoming increasingly more relevant due to the increase of life expectancy. Current pharmaceutical treatments poorly tackle these diseases, mainly acting only on their symptomology. One of the main reasons of this is the current drug development process, which is not only expensive and time-consuming but, also, still strongly relies on animal models at the preclinical stage.:Organ-on-a-chip platforms have the potential to strongly impact and improve the drug screening process by recreating in vitro the functionality of human organs. Patient-derived neurons from different regions of the brain can be directly grown and differentiated on a brain-on-a-chip device where the disease development, progression and pharmacological treatments can be studied and monitored in real time. The model reliability is strongly improved by using human-derived cells, more relevant than animal models for pharmacological screening and disease monitoring. The selected cells will be then capable of proliferating and organizing themselves in the in vivo environment thanks to the device architecture, materials selection and bio-chemical functionalization.:In this review, we start by presenting the fundamental strategies adopted for brain-on-a-chip devices fabrication including e.g., photolithography, micromachining and 3D printing technology. Then, we discuss the state-of-theart of brain-on-a-chip platforms including their role in the study of the functional architecture of the brain e.g., blood-brain barrier, or of the most diffuse neurodegenerative diseases like Alzheimer’s and Parkinson’s. At last, the current limitations and future perspectives of this approach for the development of new drugs and neurodegenerative diseases modeling will be discussed.

Sign in / Sign up

Export Citation Format

Share Document