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

Alkaloids 1–10 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...

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Main Authors: Cai Yi Wang, Hyun-Jae Jang, Yoo Kyong Han, Xiang Dong Su, Seung Woong Lee, Mun-Chual Rho, Heng-Shan Wang, Seo Young Yang, Young Ho Kim
Format: Article
Language:English
Published: MDPI AG 2018-06-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/23/6/1445
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author Cai Yi Wang
Hyun-Jae Jang
Yoo Kyong Han
Xiang Dong Su
Seung Woong Lee
Mun-Chual Rho
Heng-Shan Wang
Seo Young Yang
Young Ho Kim
author_facet Cai Yi Wang
Hyun-Jae Jang
Yoo Kyong Han
Xiang Dong Su
Seung Woong Lee
Mun-Chual Rho
Heng-Shan Wang
Seo Young Yang
Young Ho Kim
author_sort Cai Yi Wang
collection DOAJ
description Alkaloids 1–10 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.
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spelling doaj.art-b230eb043ec84663b46065715d03d0b12022-12-21T18:23:39ZengMDPI AGMolecules1420-30492018-06-01236144510.3390/molecules23061445molecules23061445Alkaloids from Tetrastigma hemsleyanum and Their Anti-Inflammatory Effects on LPS-Induced RAW264.7 CellsCai Yi Wang0Hyun-Jae Jang1Yoo Kyong Han2Xiang Dong Su3Seung Woong Lee4Mun-Chual Rho5Heng-Shan Wang6Seo Young Yang7Young Ho Kim8College of Pharmacy, Chungnam National University, Daejeon 34134, KoreaImmunoregulatory Material Research Center, Korea Research Institute of Bioscience and Biotechnology, 181 Ipsin-gil, Jeongeup-si, Jeonbuk 56212, KoreaCollege of Pharmacy, Chungnam National University, Daejeon 34134, KoreaCollege of Pharmacy, Chungnam National University, Daejeon 34134, KoreaImmunoregulatory Material Research Center, Korea Research Institute of Bioscience and Biotechnology, 181 Ipsin-gil, Jeongeup-si, Jeonbuk 56212, KoreaImmunoregulatory Material Research Center, Korea Research Institute of Bioscience and Biotechnology, 181 Ipsin-gil, Jeongeup-si, Jeonbuk 56212, KoreaState Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University, Guilin 541004, ChinaCollege of Pharmacy, Chungnam National University, Daejeon 34134, KoreaCollege of Pharmacy, Chungnam National University, Daejeon 34134, KoreaAlkaloids 1–10 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.http://www.mdpi.com/1420-3049/23/6/1445Tetrastigma hemsleyanumalkaloidNO productionanti-inflammatory activity
spellingShingle Cai Yi Wang
Hyun-Jae Jang
Yoo Kyong Han
Xiang Dong Su
Seung Woong Lee
Mun-Chual Rho
Heng-Shan Wang
Seo Young Yang
Young Ho Kim
Alkaloids from Tetrastigma hemsleyanum and Their Anti-Inflammatory Effects on LPS-Induced RAW264.7 Cells
Molecules
Tetrastigma hemsleyanum
alkaloid
NO production
anti-inflammatory activity
title Alkaloids from Tetrastigma hemsleyanum and Their Anti-Inflammatory Effects on LPS-Induced RAW264.7 Cells
title_full Alkaloids from Tetrastigma hemsleyanum and Their Anti-Inflammatory Effects on LPS-Induced RAW264.7 Cells
title_fullStr Alkaloids from Tetrastigma hemsleyanum and Their Anti-Inflammatory Effects on LPS-Induced RAW264.7 Cells
title_full_unstemmed Alkaloids from Tetrastigma hemsleyanum and Their Anti-Inflammatory Effects on LPS-Induced RAW264.7 Cells
title_short Alkaloids from Tetrastigma hemsleyanum and Their Anti-Inflammatory Effects on LPS-Induced RAW264.7 Cells
title_sort alkaloids from tetrastigma hemsleyanum and their anti inflammatory effects on lps induced raw264 7 cells
topic Tetrastigma hemsleyanum
alkaloid
NO production
anti-inflammatory activity
url http://www.mdpi.com/1420-3049/23/6/1445
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