Immunomodulatory and antitumour bioactive labdane diterpenoids from Leonurus japonicus. (5th August 2020)

• Record Type: Journal Article
• Authors: Yue, Grace Gar‐Lee; Liang, Xin‐Xin; Li, Xiao‐Li; Lee, Julia Kin‐Ming; Gao, Si; Kwok, Hin‐Fai; Lau, Clara Bik‐San; Xiao, Wei‐Lie
• Is Part Of: Journal of pharmacy and pharmacology. Volume 72:Number 11(2020)
• Page Start: 1657
• Page End: 1665
• Publication Date: 2020-08-05
• Subjects: cytotoxicity -- heteronone -- labdane diterpenoids -- leojapone -- Leonurus japonicus -- lewis lung cancer; Pharmacy -- Periodicals; Pharmacology -- Periodicals; 615.1
• DOI: 10.1111/jphp.13348
• Languages: English
• ISSNs: 0022-3573

Abstract

Abstract: Objectives: Two labdane diterpenoids, leojapone B and heteronone B, were isolated from Leonurus japonicus Houtt., and their biological activity were evaluated in this study. Methods: Human and mouse cancer cells, human peripheral blood mononuclear cells (PBMCs) and mouse macrophages (RAW264.7 cells) were used to evaluate the activity of leojapone B and heteronone B, while the in vivo effects of leojapone B were further examined in Lewis Lung Cancer tumour‐bearing mice. Key findings: In vitro studies showed that leojapone B selectively inhibited the proliferation of lung cancer cells, and both leojapone B and heteronone B inhibited the production of pro‐inflammatory cytokines in activated PBMCs. In tumour‐bearing mice model, lung tumours were reduced in size in mice treated with intraperitoneal injections of leojapone B at 20 and 30 mg/kg for 14 days. The population ratio of CD4 + /CD8 + T cells in mouse spleens was found to be increased, while regulatory T cells were decreased after leojapone B treatment. Conclusions: The inhibitory effects of leojapone B in mouse lung tumours were demonstrated for the first time in this study. The immunomodulatory activity of heteronone B were also demonstrated. Our findings indicated that both leojapone B and heteronone B may act as active components in L. japonicus .