2. Academic Validation
  3. Lactones from the pericarps of Litsea japonica and their anti-inflammatory activities

Lactones from the pericarps of Litsea japonica and their anti-inflammatory activities

  • Bioorg Med Chem Lett. 2018 Jun 15;28(11):2109-2115. doi: 10.1016/j.bmcl.2018.04.023.
Quynh-Mai Thi Ngo 1,  Thao Quyen Cao 2,  Phi-Long Tran 3,  Jeong Ah Kim 4,  Sang-Tae Seo 5,  Jin-Cheol Kim 6,  Mi Hee Woo 2,  Jeong Hyung Lee 7,  Byung Sun Min 8
Affiliations

Affiliations

  • 1 College of Pharmacy, Drug Research and Development Center, Daegu Catholic University, Gyeongbuk 38430, Republic of Korea; College of Pharmacy, Hai Phong University of Medicine and Pharmacy, 72A Nguyen Binh Khiem, Hai Phong 180000, Viet Nam.
  • 2 College of Pharmacy, Drug Research and Development Center, Daegu Catholic University, Gyeongbuk 38430, Republic of Korea.
  • 3 Department of Biochemistry, College of Natural Sciences, Kangwon National University, Chuncheon, Gangwon 24414, Republic of Korea.
  • 4 College of Pharmacy, Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 41566, Republic of Korea.
  • 5 Division of Forest Disease and Insect Pest, National Institute of Forest Science, Seoul 02455, Republic of Korea.
  • 6 College of Agriculture and Life Sciences, Chonnam National University, Gwangju 61186, Republic of Korea.
  • 7 Department of Biochemistry, College of Natural Sciences, Kangwon National University, Chuncheon, Gangwon 24414, Republic of Korea. Electronic address: jhlee36@kangwon.ac.kr.
  • 8 College of Pharmacy, Drug Research and Development Center, Daegu Catholic University, Gyeongbuk 38430, Republic of Korea. Electronic address: bsmin@cu.ac.kr.
PMID: 29730029 DOI: 10.1016/j.bmcl.2018.04.023
Abstract

Five new lactones, litsenolide F1 (1), lisealactone H1 (10), lisealactone H2 (11), akolactone D (13), and akolactone E (14), along with thirteen known compounds were isolated from the pericarps of Litsea japonica (Thunb.) Jussieu. Their chemical structures were elucidated by extensive spectroscopic analyses, including 1D and 2D NMR, HRMS, and chemical methods. The isolated compounds were evaluated for their inhibitory effects on NO production in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Among them, 2-alkylidene-3-hydroxy-4-methylbutanolide derivatives (compounds 1-9) exhibited the most potent activity, with IC50 values in the range of 2.9-12.8 μM. In additon, compounds 1, 3, 4, and 6 showed inhibition of iNOS and COX-2 expression in concentration-dependent manner. Compound 3 suppresses mRNA expression of iNOS, COX-2, IL-6, and TNF-α in LPS-stimulated RAW264.7 cells. Based on these evidence, the isolated lactones from L. japonica could be promissing candidates for the development of new anti-inflammatory agents.

Keywords

Anti-inflammation; Lactone; Lauraceae; Litsea japonica; NO production.

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