Identification of New Polyacetylenes from Dendropanax morbifera with PPAR-α Activity Study

  • Molecules. 2024 Dec 16;29(24):5942. doi: 10.3390/molecules29245942.
Donglan Piao  1 ,  Isoo Youn  1 ,  Thanh-Hau Huynh  2 ,  Hyun Woo Kim  3 ,  Sang Gyun Noh  3 ,  Hae Young Chung  3 ,  Dong-Chan Oh  2 ,  Eun Kyoung Seo  1
Affiliations
  • 1. Graduate School of Pharmaceutical Sciences, College of Pharmacy, Ewha Womans University, Seoul 03760, Republic of Korea.
  • 2. Natural Products Research Institute, College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea.
  • 3. Department of Pharmacy and Research Institute for Drug Development, College of Pharmacy, Pusan National University, Busan 46241, Republic of Korea.
PMID: 39770031 DOI: 10.3390/molecules29245942
Abstract

Dendropanax morbifera Leveille is a traditional medicine used to treat migraine headache and dysmenorrhea. In this study, three polyacetylenes, methyl (10E,9R,16R)-16-acetoxy-9-hydroxyoctadeca-10,17-dien-12,14-diynoate (1), methyl (10E,9R,16S)-9,16-dihydroxyoctadeca-10-en-12,14-diynoate (2), and methyl (10Z,9R,16S)-9,16-dihydroxyoctadeca-10,17-dien-12,14-diynoate (3), were isolated from the aerial parts of D. morbifera, together with seven known compounds (4-10). Importantly, the isolates (6 and 8) were found in the family Araliaceae for the first time in this study. Compounds 1-10 were evaluated for their binding affinity to AMPK and CTSS receptors using in silico docking simulations. Only compound 7 increased the protein expression levels of PPAR-α, SIRT1, and AMPK when administered to HepG2 cells as a PPAR-α agonist. On the Other hand, 7 did not produce any significant reduction in CTSS activity. This study could pave the way for the discovery of novel treatments from D. morbifera targeting PPAR-α and AMPK.

Keywords
AMP-activated protein kinase; Dendropanax morbifera Leveille; Peroxisome proliferator-activated receptor; cathepsin S; polyacetylene.
Products