Please use this identifier to cite or link to this item: http://krishikosh.egranth.ac.in/handle/1/5810084265
Authors: Yadav, Jyotika
Advisor: Goel, Parveen
Title: Evaluation of in vitro growth inhibitory efficacy of some target specific novel drug molecules against Theileria equi
Publisher: LUVAS
Language: en
Type: Thesis
Agrotags: null
Keywords: Equines, Theileria equi, Protein kinase inhibitor, MASP culture
Abstract: In vitro growth inhibitory efficacy of some novel protein kinase inhibitors drug molecules against microaerophilic stationary-phase culture (MASP) culture of Theileria equi parasites was carried out in present study. Various protein kinases were targeted by apigenin (protein kinase C and cyclin dependent kinase inhibitor), FR180204 (MAPK/ERK1 and 2 inhibitor), PD0332991 also known as palbociclib (cyclin dependent kinase 4/6 inhibitor) and SB239063 (p38 MAP kinase inhibitor) and were compared with reference drug diminazene aceturate and imidocarb dipropionate. The 50% inhibitory concentration also known as IC50 value of SB239063, PD0332991, FR180204, diminazene aceturate and imidocarb dipropionate were calculated as 4.25 μM, 10.41 μM, 21 μM, 1.23 μM and 0.139 μg/ml (equivalent to 0.279 μM) respectively. Among all the drug molecules tested in this study, apigenin was found as not effective as it was failed to inhibit progression of T. equi parasites in in vitro growth inhibition assay and on viability testing at 96 h. Whereas, SB239063 was the most effective drug molecule and results were comparable to the reference drug diminazene aceturate. Furthermore in vitro cytotoxicity on horse PBMC of the best one was compared with diminazene aceturate as reference. SB239063 and diminazene aceturate were found 26.19% and 30.38% cytotoxic respectively at 100 μM drug concentration. Imidocarb dipropionate was 7.09% cytotoxic at 125 μg/ml drug concentration. SB239063 showed 1.32% hemolysis at 100 μM drug concentration. Conclusively, SB239063 was found to be potential drug molecule for in vitro inhibition of T. equi parasite culture and MAP kinase may be a good drug target for antipiroplasmic drug development.
Subject: Veterinary Medicine
Theme: Evaluation of in vitro growth inhibitory efficacy of some target specific novel drug molecules against Theileria equi
These Type: M.V.Sc.
Issue Date: 2018
Appears in Collections:Thesis

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