Immunomodulatory and antitumour bioactive labdane diterpenoids from Leonurus japonicus

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...

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Veröffentlicht in:Journal of pharmacy and pharmacology 2020-11, Vol.72 (11), p.1657-1665
Hauptverfasser: 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
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Sprache:eng
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Zusammenfassung: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.
ISSN:0022-3573
2042-7158
DOI:10.1111/jphp.13348