In vitro: |
Biomed Pharmacother. 2017 Apr;88:878-884 | Shizukaol B, an active sesquiterpene from Chloranthus henryi, attenuates LPS-induced inflammatory responses in BV2 microglial cells.[Pubmed: 28178617 ] | The objective of the current study was to evaluate the anti-inflammatory effects of Shizukaol B, a lindenane-type dimeric sesquiterpene isolated from the whole plant of Chloranthus henryi, on lipopolysaccharide (LPS)-induced activation of BV2 microglial cells in vitro.
METHODS AND RESULTS:
Our data showed that Shizukaol B concentration-dependently suppressed expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), production of nitric oxide (NO), tumor necrosis factor-α (TNF-α), and interleukin-1β (IL-1β) in LPS-stimulated BV2 microglia. Meanwhile, Shizukaol B concentration- and time-dependently inhibited LPS-mediated c-Jun N-terminal kinase 1/2 (JNK) activation, but had little effect on extracellular signal-regulated kinase 1/2 or p38 phosphorylation. Furthermore, Shizukaol B significantly blocked LPS-induced activator protein-1 (AP-1) activation, evidenced by reduced phosphorylation and nuclear translocation of c-Jun and DNA binding activity of AP-1.
CONCLUSIONS:
Taken together, our findings suggest that Shizukaol B exerts anti-inflammatory effects in LPS-activated microglia partly by modulating JNK-AP-1 signaling pathway. | Chem Biodivers. 2014 Jun;11(6):919-28. | Sesquiterpenoids from Chloranthus henryi and their anti-neuroinflammatory activities.[Pubmed: 24934677 ] | METHODS AND RESULTS:
Five new and seven known mono-sesquiterpenoids (1-5 and 6-12, resp.) together with five known lindenane-type disesquiterpenoids, 13-17, were isolated from the whole plant of Chloranthus henryi. Based on spectroscopic methods, the new structures were established to be (5S,6R,8S,10R)-6-hydroxyeudesma-4(15),7(11)-diene-12,8-olide (1), 6α-hydroxyeudesma-4(15),7(11),8(9)-triene-12,8-olide (2), 8,12-epoxy-1β-hydroxyeudesma-4(15),7,11-trien-6-one (3), 12-oxochloraniolide A (4), and (4α)-8-hydroxy-12-norcardina-6,8,10-trien-11-one (5), respectively.
CONCLUSIONS:
Among the isolates, compound 2, zederone epoxide (8), spicachlorantin G (13), chloramultilide A (14), Shizukaol B (15), and spicachlorantin B (17) showed significant anti-neuroinflammatory effects by inhibiting nitric-oxide (NO) production in lipopolysaccharide (LPS)-stimulated murine BV-2 microglial cells with relatively low cytotoxicity. | J Nat Prod. 2011 Jun 24;74(6):1408-13 | Lindenane disesquiterpenoids with anti-HIV-1 activity from Chloranthus japonicus.[Pubmed: 21650224] | Five new lindenane disesquiterpenoids, chlorajaponilides A-E (1-5), together with 11 known analogues were isolated from whole plants of Chloranthus japonicus.
METHODS AND RESULTS:
The structure and absolute configuration of 1 was confirmed by X-ray crystallography. Compounds 1 and 2 represent the first examples of lindenane disesquiterpenoids with a C-5 hydroxy group and a C-4-C-15 double bond. Compounds 8, 9, 11, and 12 showed anti-HIV-1 replication activities in both wild-type HIV-1 and two NNRTIs-resistant strains. Shizukaol B (8) exhibited the best activity against HIV(wt), HIV(RT-K103N), and HIV(RT-K103N) with EC₅₀ values of 0.22, 0.47, and 0.50 μM, respectively.
Compounds 8, 9, 11, and 12 had significant cytotoxicities against C8166 cells with CC₅₀ values of 0.020, 0.089, 0.047, and 0.022, respectively, and exhibited inhibitory activities against HIV-1 with EC₅₀ values of 0.0014, 0.016, 0.0043, and 0.0033 μM, respectively. |
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