1. Screening 5‐lipoxygenase inhibitors from selected traditional Chinese medicines and isolation of the active compounds from Polygoni Cuspidati Rhizoma by an on‐line bioactivity evaluation system.
- Author
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Xu, Hong‐Bo, Yang, Yuan‐Gui, Xu, Huai‐Li, Yuan, Meng‐Meng, Chen, Shi‐Zhong, Song, Zhong‐Xing, and Tang, Zhi‐Shu
- Abstract
To identify natural products as new prototypes for 5‐lipoxygenase (5‐LOX), 12 traditional Chinese medicines (TCMs) were selected for screening their 5‐LOX inhibition activities. The results showed that the methanol extracts of all selected TCMs (n = 12) possessed inhibitory activities against 5‐LOX at 200 μg/mL, of which six extracts of the TCMs showed significant inhibitory effects with IC50 values in the range from 33.2 ± 1.4 μg/mL to 153.5 ± 1.7 μg/mL, and the extract of Polygoni Cuspidati Rhizoma (RPC) was the most active sample. An on‐line ultra‐performance liquid chromatography–photodiode array–MSn–5‐LOX–fluorescence detector (UPLC–PDA–MSn–5‐LOX–FLD) method was applied to further identify the potential 5‐LOX inhibitory constituents in RPC extracts, which resulted in the identification of seven components with 5‐LOX‐binding activities. Finally, four compounds (polydatin, resveratrol, emodin‐8‐O‐glucoside, and emodin) were successfully purified from RPC extracts. The 5‐LOX inhibition action was assayed in vitro, and the results showed that these compounds possessed potent inhibitory effects against 5‐LOX with IC50 values of 15.3 ± 2.1, 4.5 ± 1.2, 23.8 ± 0.4, and 11.8 ± 1.5 μg/mL, respectively. This was the first study to reveal the 5‐LOX inhibitory constituents of RPC, and the present investigation might provide a valuable approach for the rapid discovery of natural inhibitors from TCMs. [ABSTRACT FROM AUTHOR]
- Published
- 2022
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