Current Issue : January - March Volume : 2021 Issue Number : 1 Articles : 5 Articles
The aim of this study was to investigate the effects of a combination of ranolazine with\ndifferent selective inhibitors of the Na+/Ca2+-exchanger (NCX) in an established experimental model\nof atrial fibrillation (AF). Eighteen hearts of New Zealand white rabbits were retrogradely perfused.\nAtrial catheters were used to record monophasic action potentials (aPRR). Hearts were paced at\nthree different cycle lengths. Thereby, atrial action potential durations (aAPD90), atrial effective\nrefractory periods (aERP) and atrial post-repolarization refractoriness were obtained. Isoproterenol\nand acetylcholine were employed to increase the occurrence of AF. Thereafter, the hearts were\nassigned to two groups (n = 9 each group) and additionally perfused with a combination\n....................................
Luteolin is a common phytochemical from the flavonoid family with a flavone structure. Studies reported several bioactivities for\nluteolin and similar flavones. Attenuating the increased adipogenesis of bone marrow cells (hBM-MSCs) has been regarded as a\ntherapeutic target against osteoporotic bone disorders. In the present study, the potential roles of luteolin and its sulfonic acid\nderivative luteolin-OSO3Na in regulating adipogenic differentiation of hBM-MSCs were investigated. Adipo-induced cells were\ntreated with or without compounds, and their effect on adipogenesis was evaluated by adipogenic marker levels such as lipid\naccumulation and PPARc pathway activation. Luteolin hindered the adipogenic lipid accumulation in adipo-induced hBMMSCs.\nImmunoblotting and reverse transcription-polymerase chain reaction analysis results indicated that luteolin downregulated\n...................................
Cariprazine (Car) is a recently approved second generation antipsychotic (SGA) with\nunique pharmacodynamic profile, being a partial agonist at both dopamine..........................
Human immunodeficiency virus 1 (HIV-1) infection is a global health issue since neither\na cure nor a vaccine is available. However, the highly active antiretroviral therapy (HAART)\nhas improved the life expectancy for patients with acquired immunodeficiency syndrome (AIDS).\nNucleoside reverse transcriptase inhibitors (NRTIs) are in almost all HAART and target reverse\ntranscriptase (RT), an essential enzyme for the virus. Even though NRTIs are highly effective,\nthey have limitations caused by RT resistance. The main mechanisms of RT resistance to NRTIs\nare discrimination and excision. Understanding the molecular mechanisms for discrimination and\nexcision are essential to develop more potent and selective NRTIs. Using protein X-ray crystallography,\nwe determined the first crystal structure of RT in its post-catalytic state in complex with emtricitabine,\n(-)FTC or stavudine (d4T). Our structural studies provide the framework for understanding how RT\ndiscriminates between NRTIs and natural nucleotides, and for understanding the requirement of\n(-)FTC to undergo a conformation change for successful incorporation by RT. The crystal structure of\nRT in post-catalytic complex with d4T provides a â??snapshotâ? for considering the possible mechanism\nof how RT develops resistance for d4T via excision. The findings reported herein will contribute to\nthe development of next generation NRTIs...
Leishmaniases are neglected diseases that are endemic in many tropical and sub-tropical\nCountries. Therapy is based on different classes of drugs which are burdened by severe side\neffects, occurrence of resistance and high costs, thereby creating the need for more efficacious,\nsafer and inexpensive drugs. Herein, sixteen 9-thioxanthenone derivatives (lucanthone analogues)\nand four compounds embodying the diarylethene substructure of amitriptyline (amitriptyline\nanalogues) were tested in vitro for activity against Leishmania tropica and L. infantum promastigotes.\nAll compounds were characterized by the presence of a bulky quinolizidinylalkyl moiety.\nAll compounds displayed activity against both species..........................
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