Ju Mi Hyun1,
Yeon Jeong Jo1,
Jung Eun Kim1,
Hyun Joo An2,
Young Hun Choi2,
Chang-Gu Hyun1,
Nam Ho Lee1 
For correspondence:- Nam Lee Email: namho@jejunu.ac.kr Tel:+82647543548
Accepted: 18 August 2017 Published: 30 September 2017
Citation: Hyun JM, Jo YJ, Kim JE, An HJ, Choi YH, Hyun C, et al. Tetramethyl-O-scutellarin isolated from peels of immature Shiranuhi fruit exhibits anti-inflammatory effects on LPS-induced RAW264.7 cells. Trop J Pharm Res 2017; 16(9):2197-2205 doi: 10.4314/tjpr.v16i9.22
© 2017 The authors.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..
Purpose: To investigate the anti-inflammatory activity of the ethanol extract of the immature fruit of a citrus, Shiranuhi, and to identify the active ingredient.
Methods: The immature Shiranuhi peel was extracted with 80 % ethanol, and the extract was fractionated with solvents (n-hexane, ethyl acetate and n-butanol) to afford the corresponding fractions and water residue. Among them, the EtOAc-soluble portion was subjected to medium pressure liquid chromatography (MPLC) over a reversed-phase SiO2 column to give compound 1. The isolated compound was identified based on the proton and carbon nuclear magnetic resonance (NMR) spectra. The release of nitric oxide, prostaglandin (PG)E2, tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6 secreted by mouse macrophages was measured using RAW264.7 cell culture supernatant.
Results: Shiranuhi (Korean name, Hallabong) is an important citrus species cultivated in Jeju Island, Korea. A polymethoxyflavonoid (PMF), tetramethyl-O-scutellarin (1), was isolated from the peels of immature Shiranuhi fruit. Upon the evaluation of anti-inflammatory effects, the flavonoid 1 decreased the nitric oxide production in macrophage cells with high efficiency, viz, 50 % inhibition concentration, IC50 of 57.4 μM. Subsequent studies demonstrated that PMF 1 effectively inhibited the generation of PGE2, TNF-α, IL-1β, and IL-6 cytokine in a dose-dependent manner.
Conclusion: Tetramethyl-O-scutellarin (1) has been successfully isolated from Shiranuhi species for the first time. Thus, Shiranuhi fruit peel extract containing PMF 1 can potentially be applied as an anti-inflammatory ingredient in food or cosmetic industries.
Archives
News Updates
Fulltext in PDF