Biomol Ther.  2020 Sep;28(5):397-404. 10.4062/biomolther.2019.180.

Diallyl Biphenyl-Type Neolignans Have a Pharmacophore of PPARα/γ Dual Modulators

Affiliations
  • 1College of Pharmacy and Natural Products Research Institute, Seoul National University, Seoul 08826, Republic of Korea
  • 2SK Bioland, Cheongju 28162, Republic of Korea
  • 3College of Pharmacy, Dongguk University, Goyang 10326, Republic of Korea

Abstract

Adiponectin secretion-promoting compounds have therapeutic potentials in human metabolic diseases. Diallyl biphenyl-type neolignan compounds, magnolol, honokiol, and 4-O-methylhonokiol, from a Magnolia officinalis extract were screened as adiponectin-secretion promoting compounds in the adipogenic differentiation model of human bone marrow mesenchymal stem cells (hBM-MSCs). In a target identification study, magnolol, honokiol, and 4-O-methylhonokiol were elucidated as PPARα and PPARγ dual modulators. Diallyl biphenyl-type neolignans affected the transcription of lipid metabolism-associated genes in a different way compared to those of specific PPAR ligands. The diallyl biphenyl-type neolignan structure provides a novel pharmacophore of PPARα/γ dual modulators, which may have unique therapeutic potentials in diverse metabolic diseases.

Keyword

Diallyl biphenyl-type neolignans; Adiponectin; Human bone marrow mesenchymal stem cells; Peroxisome proliferatoractivated receptor α/γ
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