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 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.

• Authors: Grace Gar-Lee Yue, Xin-Xin Liang, Xiao-Li Li, Julia Kin-Ming Lee, Si Gao, Hin-Fai Kwok, Clara Bik-San Lau, Wei-Lie Xiao
• Journal: The Journal of pharmacy and pharmacology (J Pharm Pharmacol) Vol. 72 Issue 11 Pg. 1657-1665 (Nov 2020) ISSN: 2042-7158 [Electronic] England
• PMID: 32757490 (Publication Type: Journal Article)
• Copyright: © 2020 Royal Pharmaceutical Society.

Chemical References

• Antineoplastic Agents, Phytogenic
• Cytokines
• Diterpenes
• Immunologic Factors
• Inflammation Mediators
• Plant Extracts
• heteronone B
• labdane

Topics

• Animals
• Antineoplastic Agents, Phytogenic (isolation & purification, pharmacology)
• Carcinoma, Lewis Lung (drug therapy, immunology, metabolism, pathology)
• Cell Proliferation (drug effects)
• Cytokines (metabolism)
• Diterpenes (isolation & purification, pharmacology)
• HT29 Cells
• Hep G2 Cells
• Humans
• Immunologic Factors (isolation & purification, pharmacology)
• Inflammation Mediators (metabolism)
• Leonurus (chemistry)
• Leukocytes, Mononuclear (drug effects, immunology, metabolism)
• MCF-7 Cells
• Macrophages (drug effects, immunology, metabolism)
• Male
• Mice
• Mice, Inbred C57BL
• Plant Extracts (isolation & purification, pharmacology)
• RAW 264.7 Cells
• T-Lymphocyte Subsets (drug effects, immunology, metabolism)
• Tumor Burden (drug effects)