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Molecules 2018, 23(6), 1445;

Alkaloids from Tetrastigma hemsleyanum and Their Anti-Inflammatory Effects on LPS-Induced RAW264.7 Cells

College of Pharmacy, Chungnam National University, Daejeon 34134, Korea
Immunoregulatory Material Research Center, Korea Research Institute of Bioscience and Biotechnology, 181 Ipsin-gil, Jeongeup-si, Jeonbuk 56212, Korea
State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin 541004, China
Authors to whom correspondence should be addressed.
Academic Editor: Helen D. Skaltsa
Received: 7 April 2018 / Revised: 7 June 2018 / Accepted: 9 June 2018 / Published: 14 June 2018
(This article belongs to the Special Issue Biological Activity of Secondary Metabolites)
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Alkaloids 110 were isolated from the aerial parts of Tetrastigma hemsleyanum (APTH) and obtained from species of the genus Tetrastigma for the first time. The chemical structures of the isolated compounds were identified by NMR, UV, and MS analyses. Their anti-inflammatory activities were investigated by measuring nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW264.7 macrophages. Among all the isolates, compounds 6, 7 and 10 showed potent inhibitory activity against LPS-stimulated NO production in RAW264.7 cells (IC50: 31.9, 25.2 and 6.3 μM, respectively). Furthermore, APTH and S-(−)-trolline (10) inhibited induction of inflammatory cytokines or mediators such as interleukin-1β (IL-1β) and inducible nitric oxide synthase (iNOS) via suppression of nuclear factor κB (NF-κB) translocation into the nucleus. In addition, 10 suppressed extracellular signal-regulated protein kinase 1/2 (ERK1/2) mitogen-activated protein kinase (MAPK) phosphorylation in a dose-dependent manner. These results conclusively demonstrated that compound 10 displays anti-inflammatory activity via suppression of NF-κB activation and the ERK-MAPK signaling pathway in LPS-stimulated RAW264.7 cells. View Full-Text
Keywords: Tetrastigma hemsleyanum; alkaloid; NO production; anti-inflammatory activity Tetrastigma hemsleyanum; alkaloid; NO production; anti-inflammatory activity

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Wang, C.Y.; Jang, H.-J.; Han, Y.K.; Su, X.D.; Lee, S.W.; Rho, M.-C.; Wang, H.-S.; Yang, S.Y.; Kim, Y.H. Alkaloids from Tetrastigma hemsleyanum and Their Anti-Inflammatory Effects on LPS-Induced RAW264.7 Cells. Molecules 2018, 23, 1445.

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