Anti-neuroinflammatory effects of sesquiterpenoids isolated from Nardostachys jatamansi

[Display omitted] Two new nardosinone-type sesquiterpenoids, namely kanshone J (1) and kanshone K (2) along with seven known terpenoids (3–9) were isolated from the rhizomes and roots of Nardostachys jatamansi DC (Valerianaceae). The structures of these compounds were determined mainly by analysis o...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2018-01, Vol.28 (2), p.140-144
Hauptverfasser: Yoon, Chi-Su, Kim, Kwan-Woo, Lee, Sang-Chan, Kim, Youn-Chul, Oh, Hyuncheol
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container_end_page 144
container_issue 2
container_start_page 140
container_title Bioorganic & medicinal chemistry letters
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creator Yoon, Chi-Su
Kim, Kwan-Woo
Lee, Sang-Chan
Kim, Youn-Chul
Oh, Hyuncheol
description [Display omitted] Two new nardosinone-type sesquiterpenoids, namely kanshone J (1) and kanshone K (2) along with seven known terpenoids (3–9) were isolated from the rhizomes and roots of Nardostachys jatamansi DC (Valerianaceae). The structures of these compounds were determined mainly by analysis of 1D-, 2D-NMR and MS data. In addition, the absolute configuration of compound 1 was assigned by application of the modified Mosher’s method. In an initial assay to evaluate their anti-neuroinflammatory effects, compounds 1–5 and 9 exhibited dose-dependent inhibitory effects on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in BV2 cells, with IC50 values ranging from 2.43 to 46.54 μM. Particularly, desoxo-narchinol A (3) and narchinol B (4) significantly inhibited LPS-induced NO overproduction in BV2 cells with IC50 values of 3.48 ± 0.47 and 2.43 ± 0.23 μM, respectively. Furthermore, compounds 3 and 4 exhibited anti-neuroinflammatory effects by inhibiting the production of pro-inflammatory mediators, including prostaglandin E2 (PGE2), inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) proteins, and pro-inflammatory cytokines, such as interleukin (IL)-1β, IL-6, and tumor necrosis factor-α (TNF)-α, in LPS-stimulated BV2 and primary microglial cells.
doi_str_mv 10.1016/j.bmcl.2017.11.041
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The structures of these compounds were determined mainly by analysis of 1D-, 2D-NMR and MS data. In addition, the absolute configuration of compound 1 was assigned by application of the modified Mosher’s method. In an initial assay to evaluate their anti-neuroinflammatory effects, compounds 1–5 and 9 exhibited dose-dependent inhibitory effects on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in BV2 cells, with IC50 values ranging from 2.43 to 46.54 μM. Particularly, desoxo-narchinol A (3) and narchinol B (4) significantly inhibited LPS-induced NO overproduction in BV2 cells with IC50 values of 3.48 ± 0.47 and 2.43 ± 0.23 μM, respectively. Furthermore, compounds 3 and 4 exhibited anti-neuroinflammatory effects by inhibiting the production of pro-inflammatory mediators, including prostaglandin E2 (PGE2), inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) proteins, and pro-inflammatory cytokines, such as interleukin (IL)-1β, IL-6, and tumor necrosis factor-α (TNF)-α, in LPS-stimulated BV2 and primary microglial cells.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2017.11.041</identifier><identifier>PMID: 29221883</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Anti-neuroinflammation ; BV2 microglial cells ; Nardostachys jatamansi ; Primary microglial cells ; Sesquiterpenoids</subject><ispartof>Bioorganic &amp; medicinal chemistry letters, 2018-01, Vol.28 (2), p.140-144</ispartof><rights>2017 Elsevier Ltd</rights><rights>Copyright © 2017 Elsevier Ltd. 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subjects Anti-neuroinflammation
BV2 microglial cells
Nardostachys jatamansi
Primary microglial cells
Sesquiterpenoids
title Anti-neuroinflammatory effects of sesquiterpenoids isolated from Nardostachys jatamansi
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