2. Academic Validation
  3. Anti-Inflammatory Effect of Charantadiol A, Isolated from Wild Bitter Melon Leaf, on Heat-Inactivated Porphyromonas gingivalis-Stimulated THP-1 Monocytes and a Periodontitis Mouse Model

Anti-Inflammatory Effect of Charantadiol A, Isolated from Wild Bitter Melon Leaf, on Heat-Inactivated Porphyromonas gingivalis-Stimulated THP-1 Monocytes and a Periodontitis Mouse Model

  • Molecules. 2021 Sep 17;26(18):5651. doi: 10.3390/molecules26185651.
Tzung-Hsun Tsai 1,  Chi-I Chang 2,  Ya-Ling Hung 3,  Wen-Cheng Huang 3,  Hsiang Chang 4,  Yueh-Hsiung Kuo 5 6 7,  Jong-Ho Chyuan 8,  Lu-Te Chuang 4,  Po-Jung Tsai 3 9
Affiliations

Affiliations

  • 1 Department of Dentistry, Keelung Chang-Gung Memorial Hospital, Keelung 204, Taiwan.
  • 2 Department of Biological Science and Technology, National Pingtung University of Science and Technology, Pingtung 912, Taiwan.
  • 3 Department of Human Development and Family Studies, National Taiwan Normal University, Taipei 106, Taiwan.
  • 4 Department of Biotechnology and Pharmaceutical Technology, Yuanpei University of Medical Technology, Hsinchu 300, Taiwan.
  • 5 Department of Chinese Pharmaceutical Sciences and Chinese Medicine Resources, China Medical University, Taichung 404, Taiwan.
  • 6 Chinese Medicine Research Center, China Medical University, Taichung 404, Taiwan.
  • 7 Department of Biotechnology, Asia University, Taichung 413, Taiwan.
  • 8 Hualien District Agricultural Research and Extension Station, Hualien 973, Taiwan.
  • 9 Program of Nutrition Science, School of Life Science, National Taiwan Normal University, Taipei 116, Taiwan.
PMID: 34577123 DOI: 10.3390/molecules26185651
Abstract

Porphyromonas gingivalis has been identified as one of the major periodontal pathogens. Activity-directed fractionation and purification processes were employed to identify bioactive compounds from bitter melon leaf. Ethanolic extract of bitter melon leaf was separated into five subfractions by open column chromatography. Subfraction-5-3 significantly inhibited P. gingivalis-induced interleukin (IL)-8 and IL-6 productions in human monocytic THP-1 cells and then was subjected to separation and purification by using different chromatographic methods. Consequently, 5β,19-epoxycucurbita-6,23(E),25(26)-triene-3β,19(R)-diol (charantadiol A) was identified and isolated from the subfraction-5-3. Charantadiol A effectively reduced P. gingivalis-induced IL-6 and IL-8 productions and triggered receptors expressed on myeloid cells (TREM)-1 mRNA level of THP-1 cells. In a separate study, charantadiol A significantly suppressed P. gingivalis-stimulated IL-6 and tumor necrosis factor-α mRNA levels in gingival tissues of mice, confirming the inhibitory effect against P. gingivalis-induced periodontal inflammation. Thus, charantadiol A is a potential anti-inflammatory agent for modulating P. gingivalis-induced inflammation.

Keywords

Porphyromonas gingivalis; anti-inflammation; bitter melon; charantadiol A.

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