Wan-Chao Zhong, En-Can Li, Rui-Rui Hao
Jun 1, 2021
Citations
0
Influential Citations
7
Citations
Quality indicators
Journal
Chinese journal of natural medicines
Abstract
Guided by cell-based anti-anaphylactic assay, eighteen cage-like monoterpenoid glycosides ( 1 - 18 ) were obtained from the bioactive fraction of P. lactiflora extract. Among these, compounds 1 , 5 , 6 , 11 , 12 , 15 , and 17 can significantly reduce the release rate of β-HEX and HIS without or with less cytotoxicity. Additionally, the most potent inhibitor benzoylpaeoniflorin ( 5 ) was selected as the prioritized compound for the study of action of mechanism, indicating that its anti-anaphylactic activity was medicated by dual-inhibiting HDC and MAPK signal pathway. Moreover, the molecular docking simulation explained that benzoylpaeoniflorin ( 5 ) could block the conversion of L-histidine to HIS by occupying the HDC active site. Finally, in vivo on PCA using BALB/c mice, benzoylpaeoniflorin ( 5 ) can suppress the IgE-mediated PCA reaction in antigen-challenged mice. These findings indicate that cage-like monoterpenoid glycosides, especially benzoylpaeoniflorin ( 5 ), mainly contributed to the anti-anaphylactic activity of P. lactiflora by dual-inhibiting HDC and MAPK signal pathway. Therefore, benzoylpaeoniflorin ( 5 ) may be considered as a novel drug candidate for the treatment of anaphylactic diseases.