In vitro growth inhibitory effect of selected 18β-glycyrrhetinic acid esters on Theileria annulata

K Buvanesvaragurunathan,J Ganesh,S Nagul Kumar, V Porchezhiyan, A Radha,P Azhahianambi,P Pandikumar,S Ignacimuthu

Experimental Parasitology(2022)

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摘要
Glycyrrhetinic acid (GA) is one of the important Pentacyclic Triterpenoids (PT) found in the roots of licorice. This study aimed to evaluate the in vitro growth inhibitory effect of 18β-GA (18β-Glycyrrhetinic acid) and C-30 esters against Theileria annulata, the causative agent of Tropical Bovine Theileriosis. C-30 esters of 18β-GA were synthesized and their structures were elucidated using spectroscopy. The pharmacodynamic properties of 18β-GA and its C-30 esters were predicted using DataWarrior and Swiss ADME tools. Cattle isolates of T. annulata schizont-infected bovine lymphoblastoid cells were cultured using standard conditions and the growth inhibitory effect of GA and its esters were evaluated using MTT assay. The isopropyl ester of 18β-GA (GI50- 1.638 μM; R2- 0.818) showed improved anti-theileriosis efficacy than other 18β-GA derivatives. The propyl (GI50 - 5.549 μM), ethyl (GI50 - 5.638 μM), and benzyl (GI50 - 7.431 μM) esters also showed considerable inhibitory effect. The GI50 value for 18β-GA was recorded as 6.829 μM. This study throws light on the usefulness of 18β-GA and its esters for the treatment of Tropical Bovine Theileriosis.
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关键词
Pentacyclic triterpenoids,Glycyrrhiza glabra,Theileriosis,Semi-synthesis
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