1. Academic Validation
  2. Bioactive lignan derivatives from the stems of Firmiana simplex

Bioactive lignan derivatives from the stems of Firmiana simplex

  • Bioorg Med Chem Lett. 2016 Feb 1;26(3):730-733. doi: 10.1016/j.bmcl.2016.01.008.
Kyeong Wan Woo 1 Won Se Suh 1 Lalita Subedi 2 Sun Yeou Kim 3 Aejung Kim 4 Kang Ro Lee 5
Affiliations

Affiliations

  • 1 Natural Products Laboratory, School of Pharmacy, Sungkyunkwan University, 2066 Seobu-Ro, Jangan-ku, Suwon, Gyeonggi-do, Republic of Korea.
  • 2 College of Pharmacy, Gachon University, #191 Hambakmoe-ro, Yeonsu-gu, Incheon 406-799, Republic of Korea.
  • 3 College of Pharmacy, Gachon University, #191 Hambakmoe-ro, Yeonsu-gu, Incheon 406-799, Republic of Korea; Gachon Medical Research Institute, Gil Medical Center, Incheon, Republic of Korea.
  • 4 The Graduate School of Alternative Medicine, Kyonggi University, Seoul, Republic of Korea.
  • 5 Natural Products Laboratory, School of Pharmacy, Sungkyunkwan University, 2066 Seobu-Ro, Jangan-ku, Suwon, Gyeonggi-do, Republic of Korea. Electronic address: krlee@skku.edu.
Abstract

The CHCl3 soluble fraction of the 80% MeOH extract of the stems of Firmiana simplex strongly inhibited nitric oxide production in lipopolysaccharide-activated BV-2 cells. A bioactivity-guided column chromatographic separation yielded two new Lignans, firmianols A and B (1-2) together with seventeen known Lignans (3-19). The structural elucidation of the new compounds was determined by spectroscopic methods, including 1D, 2D NMR and HR-FAB-MS. All isolated Lignans were evaluated for their antineuroinflammatory effects on nitric oxide (NO) production in lipopolysaccharides (LPS)-activated murine microglia BV2 cells. Among the isolated, compounds 14 and 15 showed potent inhibitory activity against NO production (IC50 1.05 and 0.929 μM, respectively) without cell toxicity in murine microglia BV-2 cells. Compounds 11-13 and 17 also exhibited strong inhibitory effects on NO production, with IC50 values ranging from 7.07 to 15.28 μM.

Keywords

Anti-neuroinflammatory effect; Firmiana simplex; Lignan; Sterculiaceae.

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