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© 2022 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.

Abstract

Seven new anthraquinones with rare 2-isopropyldihydrofuran (13) and 2,2-dimethylpyrano (47) moieties together with thirty-four known compounds were isolated from the extracts of whole Hedyotis diffusa 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 N-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 Hedyotis diffusa and vision of development as lead compounds.

Details

Title
Chemical Constituents of Hedyotis diffusa and Their Anti-Inflammatory Bioactivities
Author
Hsin-Yi, Hung 1   VIAFID ORCID Logo  ; Kun-Ching, Cheng 2 ; Ping-Chung, Kuo 1   VIAFID ORCID Logo  ; I-Tsen, Chen 3 ; Li, Yue-Chiun 1 ; Tsong-Long, Hwang 4   VIAFID ORCID Logo  ; Sio-Hong Lam 1 ; Tian-Shung Wu 1 

 School of Pharmacy, College of Medicine, National Cheng Kung University, Tainan 70101, Taiwan; [email protected] (H.-Y.H.); [email protected] (P.-C.K.); [email protected] (Y.-C.L.) 
 Taiwan Sugar Research Institute, Tainan 70176, Taiwan; [email protected] 
 Department of Chemistry, National Cheng Kung University, Tainan 70101, Taiwan; [email protected] 
 Graduate Institute of Natural Products, College of Medicine, Chang Gung University, Taoyuan 33305, Taiwan; [email protected]; Research Center for Chinese Herbal Medicine, Research Center for Food and Cosmetic Safety, Graduate Institute of Health Industry Technology, College of Human Ecology, Chang Gung University of Science and Technology, Taoyuan 33305, Taiwan; Department of Anesthesiology, Chang Gung Memorial Hospital, Taoyuan 33305, Taiwan 
First page
335
Publication year
2022
Publication date
2022
Publisher
MDPI AG
e-ISSN
20763921
Source type
Scholarly Journal
Language of publication
English
ProQuest document ID
2632196137
Copyright
© 2022 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.