Wang Ya-Lan, Jin Li-Li, Cheng Xu, Yan Wei-Feng, Deng Hao, Shen Qing-Kun, Quan Zhe-Shan, Jin Chun-Mei, Zhang Chang-Hao
Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affifiliated Ministry of Education, College of Pharmacy, Yanbian University, Yanji, Jilin, China.
Nat Prod Res. 2023 Oct-Nov;37(21):3654-3662. doi: 10.1080/14786419.2022.2098497. Epub 2022 Jul 14.
A series of derivatives of ursolic acid (UA) were synthesised, the anti- activity was tested, and the selectivity index (SI) of these compounds was calculated to determine the derivative with the best anti- activity. Compound A7 showed the best activity against the (IC in infected GES-1 cells: 9.1 ± 7.2 μM), better than the lead compound UA and the positive control drug Spiramycin. Compound A7 was selected for further in vivo research: A7 was tested for its effect on the inhibition rate of tachyzoites in mice and its biochemical parameters, such as alanine aminotransferase, aspartate aminotransferase, glutathione, and malondialdehyde were determined. Compound A7 was evaluated for its anti-Toxoplasma activity and partial damage to the liver. Therefore, the results show that compound A7 could be a potential lead compound for developing a novel anti-Toxoplasma gondii molecule.
合成了一系列熊果酸（UA）衍生物，测试了其抗活性，并计算了这些化合物的选择性指数（SI）以确定具有最佳抗活性的衍生物。化合物A7对（感染GES-1细胞中的IC：9.1±7.2μM）显示出最佳活性，优于先导化合物UA和阳性对照药物螺旋霉素。选择化合物A7进行进一步的体内研究：测试A7对小鼠速殖子抑制率的影响，并测定其生化参数，如丙氨酸转氨酶、天冬氨酸转氨酶、谷胱甘肽和丙二醛。评估了化合物A7的抗弓形虫活性和对肝脏的部分损伤。因此，结果表明化合物A7可能是开发新型抗弓形虫分子的潜在先导化合物。
