2. Academic Validation
  3. Anti-inflammatory activities of isopimara-8(14),-15-diene diterpenoids and mode of action of kaempulchraols P and Q from Kaempferia pulchra rhizomes

Anti-inflammatory activities of isopimara-8(14),-15-diene diterpenoids and mode of action of kaempulchraols P and Q from Kaempferia pulchra rhizomes

  • Bioorg Med Chem Lett. 2020 Jan 15;30(2):126841. doi: 10.1016/j.bmcl.2019.126841.
Nwet Nwet Win 1,  Besse Hardianti 2,  Shiori Kasahara 1,  Hla Ngwe 3,  Yoshihiro Hayakawa 4,  Hiroyuki Morita 5
Affiliations

Affiliations

  • 1 Institute of Natural Medicine, University of Toyama, 2630-Sugitani, Toyama 930-0194, Japan.
  • 2 Institute of Natural Medicine, University of Toyama, 2630-Sugitani, Toyama 930-0194, Japan; Sekolah Tinggi Ilmu Farmasi Makassar, Perintis Kemerdekaan Street KM13.7, Makassar 90242, Indonesia.
  • 3 Department of Chemistry, University of Yangon, Yangon 11041, Myanmar.
  • 4 Institute of Natural Medicine, University of Toyama, 2630-Sugitani, Toyama 930-0194, Japan. Electronic address: [email protected].
  • 5 Institute of Natural Medicine, University of Toyama, 2630-Sugitani, Toyama 930-0194, Japan. Electronic address: [email protected].
PMID: 31836445 DOI: 10.1016/j.bmcl.2019.126841
Abstract

Inflammation is an extensively recognized link to many pathological diseases. It is a host response for protection from infections and tissue damage. Infections trigger acute inflammation; however, persistent Infection will contribute to chronic inflammation and higher disease susceptibility. Deregulated inflammatory responses can cause excessive or long-lasting tissue damage, manifested as Cancer, immune disorders, diabetes, etc. NF-κB is a central mediator of pro-inflammatory gene induction and functions in both innate and adaptive immune cells; therefore, the anti-inflammatory regulation of NF-κB is needed. Natural products reportedly play an important role in controlling the inflammatory response pathways. However, the anti-inflammatory activities of isopimara-8-(14),15-diene Diterpenoids have not yet been fully elucidated. To elucidate the anti-inflammatory activities of the isopimara-8(14),15-diene Diterpenoids, we investigated 21 isopimara-8(14),15-diene Diterpenoids previously isolated from Kaempferia pulchra rhizomes. Eleven compounds exhibited NO inhibitory activity against lipopolysaccharide (LPS)-induced RAW264.7 cells, with IC50 values ranging from 30 to 100 μM. Furthermore, the most potent kaempulchraols P and Q, with IC50 values of 39.88 and 36.05 μM, respectively, inhibited the NF-κB-mediated transactivation of a luciferase reporter gene, IL-6 production, and COX-2 expression, with an effective dose of 25 μM. These findings provide new insights into the anti-inflammatory activities of the isopimara-8(14),15-diene Diterpenoids.

Keywords

Inflammation; Isopimarane diterpenoids; Kaempferia pulchra; Kaempulchraols P and Q.

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