期刊
EXPERIMENTAL PARASITOLOGY
卷 236, 期 -, 页码 -出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.exppara.2022.108258
关键词
Pentacyclic triterpenoids; Glycyrrhiza glabra; Theileriosis; Semi-synthesis
类别
This study evaluated the in vitro growth inhibitory effect of 18 beta-Glycyrrhetinic acid and its esters against Theileria annulata, the causative agent of Tropical Bovine Theileriosis. The isopropyl ester of 18 beta-GA showed improved anti-theileriosis efficacy, while propyl, ethyl, and benzyl esters also exhibited considerable inhibitory effect.
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 18 beta-GA (18 beta-Glycyrrhetinic acid) and C-30 esters against Theileria annulata, the causative agent of Tropical Bovine Theileriosis. C-30 esters of 18 beta-GA were synthesized and their structures were elucidated using spectroscopy. The pharmacodynamic properties of 18 beta-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 18 beta-GA (GI(50)- 1.638 mu M; R-2-0.818) showed improved anti-theileriosis efficacy than other 18 beta-GA derivatives. The propyl (GI(50) - 5.549 mu M), ethyl (GI(50) - 5.638 mu M), and benzyl (GI(50) - 7.431 mu M) esters also showed considerable inhibitory effect. The GI(50) value for 18 beta-GA was recorded as 6.829 mu M. This study throws light on the usefulness of 18 beta-GA and its esters for the treatment of Tropical Bovine Theileriosis.
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