Chemical Constituents of <i>Hedyotis diffusa</i> and Their Anti-Inflammatory Bioactivities

• Main Authors: Hsin-Yi Hung (Author), Kun-Ching Cheng (Author), Ping-Chung Kuo (Author), I-Tsen Chen (Author), Yue-Chiun Li (Author), Tsong-Long Hwang (Author), Sio-Hong Lam (Author), Tian-Shung Wu (Author)
• Format: Book
• Published: MDPI AG, 2022-02-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

Seven new anthraquinones with rare 2-isopropyldihydrofuran (<b>1</b>-<b>3</b>) and 2,2-dimethylpyrano (<b>4</b>-<b>7</b>) moieties together with thirty-four known compounds were isolated from the extracts of whole <i>Hedyotis diffusa</i> plants. Their structures were elucidated and established by various spectroscopic and spectrometric analytical methods. Among these isolates, selected compounds were examined for their anti-inflammatory activity. The results showed that rare substituted anthraquinones displayed potent inhibitory activity with IC₅₀ values ranging from 0.15 ± 0.01 to 5.52 ± 1.59 µM on the <i>N</i>-formyl-methionyl-leucyl-phenylalanine/cytochalasin B (fMLP/CB)-induced superoxide anion generation and elastase release cellular models. Meanwhile, the proposed drug target of the active anthraquinone was studied by computer modeling. The binding affinity between the anti-inflammatory anthraquinone and elastase was evaluated by molecular docking. These results provided the scientific insight into the medicinal values of <i>Hedyotis diffusa</i> and vision of development as lead compounds.

Item Description

10.3390/antiox11020335
2076-3921