TY - JOUR
T1 - Anti-inflammatory activities of Sigesbeckia glabrescens Makino
T2 - Combined in vitro and in silico investigations
AU - Zhong, Zhangfeng
AU - Zhang, Qianru
AU - Tao, Hongxun
AU - Sang, Wei
AU - Cui, Liao
AU - Qiang, Wenan
AU - Cheang, Wai San
AU - Hu, Yuanjia
AU - Yu, Hua
AU - Wang, Yitao
N1 - Funding Information:
This work was financially supported by the National Natural Science Foundation of China (NSFC, No. 81470170), the Research Committee of the University of Macau (SRG2015-00060-ICMS-QRCM, MYRG2017-00178-ICMS, MYRG2018-00043-ICMS, and CPG2019-00006-ICMS), the China Postdoctoral Science Foundation funded project (2017M622811), the Natural Science Foundation of Guangdong Province, China (2018A030310226), the Guangzhou Science and Technology Innovation funding (EF007/ICMS-YH/2018/GSTIC), the Features Innovative Projects of General Colleges and Universities of Guangdong Province, China (2017KQNCX084), and the Macao Science and Technology Development Fund (FDCT 013/2015/A1 and FDCT 071/2017/A2).
Publisher Copyright:
© 2019 The Author(s).
PY - 2019/9/23
Y1 - 2019/9/23
N2 - Background: Sigesbeckia glabrescens Makino (SG) is one of the important plant origins of Sigesbeckiae herba and has been widely used for the treatment of chronic inflammatory diseases in China. However, the underlying anti-inflammatory mechanism of SG is rarely investigated and reported. There are more than 40 kinds of chemical constituents in SG, but the action of the bioactive compounds of SG is still unclear. Therefore, we aimed to systemically investigate the mechanisms behind the anti-inflammatory properties of SG by combining in vitro and in silico investigations. Methods: Cytotoxicity was measured using the 3-[4,5-dimethyl-2-Thiazolyl]-2,5-diphenyltetrazolium bromide (MTT) and lactate dehydrogenase (LDH) assays. Nitric oxide (NO) release was detected using the Griess assay. The secretion of pro-inflammatory cytokines and the expression of relevant proteins were assessed using ELISA kits and Western blots, respectively. Molecular docking was performed and scored using AutoDock via a comparison with the molecular docking of N-Acetyl-d-glucosamine (NAG). Results: In lipopolysaccharides (LPS)-stimulated macrophages, SG significantly inhibited NO, MCP-1, and IL-6 secretion; iNOS expression; and NF-κB activation but did not significantly affect MAPK signalling (p38, ERK, and JNK). Moreover, the results from the molecular docking prediction suggested that over 10 compounds in SG could likely target TLR4, p105, and p65. Conclusions: These findings suggest that the anti-inflammatory effects of SG are highly related to the inactivation of NF-κB. Moreover, this study provides a novel approach to investigate the effects of herbal medicine using combined in vitro and in silico investigations.
AB - Background: Sigesbeckia glabrescens Makino (SG) is one of the important plant origins of Sigesbeckiae herba and has been widely used for the treatment of chronic inflammatory diseases in China. However, the underlying anti-inflammatory mechanism of SG is rarely investigated and reported. There are more than 40 kinds of chemical constituents in SG, but the action of the bioactive compounds of SG is still unclear. Therefore, we aimed to systemically investigate the mechanisms behind the anti-inflammatory properties of SG by combining in vitro and in silico investigations. Methods: Cytotoxicity was measured using the 3-[4,5-dimethyl-2-Thiazolyl]-2,5-diphenyltetrazolium bromide (MTT) and lactate dehydrogenase (LDH) assays. Nitric oxide (NO) release was detected using the Griess assay. The secretion of pro-inflammatory cytokines and the expression of relevant proteins were assessed using ELISA kits and Western blots, respectively. Molecular docking was performed and scored using AutoDock via a comparison with the molecular docking of N-Acetyl-d-glucosamine (NAG). Results: In lipopolysaccharides (LPS)-stimulated macrophages, SG significantly inhibited NO, MCP-1, and IL-6 secretion; iNOS expression; and NF-κB activation but did not significantly affect MAPK signalling (p38, ERK, and JNK). Moreover, the results from the molecular docking prediction suggested that over 10 compounds in SG could likely target TLR4, p105, and p65. Conclusions: These findings suggest that the anti-inflammatory effects of SG are highly related to the inactivation of NF-κB. Moreover, this study provides a novel approach to investigate the effects of herbal medicine using combined in vitro and in silico investigations.
KW - Docking
KW - Inflammation
KW - Lipopolysaccharide
KW - NF-κB
KW - Sigesbeckia glabrescens Makino
KW - TLR4
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U2 - 10.1186/s13020-019-0260-y
DO - 10.1186/s13020-019-0260-y
M3 - Article
C2 - 31572487
AN - SCOPUS:85072608276
SN - 1749-8546
VL - 14
JO - Chinese Medicine (United Kingdom)
JF - Chinese Medicine (United Kingdom)
IS - 1
M1 - 35
ER -