1401414-17-2Relevant academic research and scientific papers
Synthesis and bioactivities evaluation of oleanolic acid oxime ester derivatives as α-glucosidase and α-amylase inhibitors
Deng, Xu-Yang,Ke, Jun-Jie,Li, Dong-Li,Wu, Jing-Ying,Wu, Pan-Pan,Xiong, Zhuang,Xu, Xue-Tao,Zhang, Kun,Zheng, Xi,Zheng, Ying-Ying
, p. 451 - 461 (2022/01/20)
Different oleanolic acid (OA) oxime ester derivatives (3a-3t) were designed and synthesised to develop inhibitors against α-glucosidase and α-amylase. All the synthesised OA derivatives were evaluated against α-glucosidase and α-amylase in?vitro. Among them, compound 3a showed the highest α-glucosidase inhibition with an IC50 of 0.35 μM, which was ～1900 times stronger than that of acarbose, meanwhile compound 3f exhibited the highest α-amylase inhibitory with an IC50 of 3.80 μM that was ～26 times higher than that of acarbose. The inhibition kinetic studies showed that the inhibitory mechanism of compounds 3a and 3f were reversible and mixed types towards α-glucosidase and α-amylase, respectively. Molecular docking studies analysed the interaction between compound and two enzymes, respectively. Furthermore, cytotoxicity evaluation assay demonstrated a high level of safety profile of compounds 3a and 3f against 3T3-L1 and HepG2 cells.Highlights Oleanolic acid oxime ester derivatives (3a–3t) were synthesised and screened against α-glucosidase and α-amylase. Compound 3a showed the highest α-glucosidase inhibitory with IC50 of 0.35 μM. Compound 3f presented the highest α-amylase inhibitory with IC50 of 3.80 μM. Kinetic studies and in silico studies analysed the binding between compounds and α-glucosidase or α-amylase.
Efficient synthesis and anti-fungal activity of oleanolic acid oxime esters
Zhao, Hanqing,Zhou, Minjie,Duan, Lifeng,Wang, Wei,Zhang, Jianjun,Wang, Daoquan,Liang, Xiaomei
, p. 3615 - 3629 (2013/05/22)
In order to develop potential glucosamine-6-phosphate synthase inhibitors and anti-fungal agents, twenty five oleanolic acid oxime esters were synthesized in an efficient way. The structures of the new compounds were confirmed by MS, HRMS, 1H-N
