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Euglobal-IIIa, a novel acylphloroglucinol-sesquiterpene derivative from Eucalyptus robusta: absolute structure and cytotoxicity

ABSTRACT: Euglobal-IIIa (1), a novel acylphloroglucinol-sesquiterpene derivative, and a known analogue, have been isolated from leaves of Eucalyptus robusta. The structures was elucidated by extensive spectroscopic data and by comparison with data reported in literature, while the absolute configuration of 1 was determined by the X-ray diffraction analysis. Compound 1 exhibited comparable cytotoxicity with that of cisplatin against five human cancer cell lines HL-60, SMMC-7721, A-549, MCF-7, and SW480 with IC50 values of 15.7, 15.5, 17.6, 14.3, and 21.8 µM, respectively.

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Supplementary material is available for this article at 10.1007/s13659-011-0021-9 and is accessible for authorized users.

SUBMITTER: Peng L

PROVIDER: S-EPMC4131649 | biostudies-literature | 2011 Oct

REPOSITORIES: biostudies-literature

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Project description:Background: Gout is the most common inflammatory arthritis worldwide. It is a painful inflammatory disease induced by the deposition of monosodium urate (MSU) crystals in the joints and peri-articular tissues. Sesquiterpene lactones (SLs) are secondary metabolite biosynthesized mainly by species from the family Asteraceae. It has been demonstrated that SLs present anti-inflammatory, analgesic, antitumoral, antiparasitic, and antimicrobial activities. In this study, we aimed at evaluating the efficacy of the SL budlein A in a model of acute gout arthritis in mice. Methods: Experiments were conducted in male Swiss or male LysM-eGFP mice. Animals were treated with budlein A (1 or 10 mg/kg) or vehicle 30 min before stimulus with MSU (100 ?g/10 ?L, intra-articular). Knee joint withdrawal threshold and edema were evaluated using electronic von Frey and caliper, respectively, 1-15 h after MSU injection. Leukocyte recruitment was determined by counting cells (Neubauer chamber), H&E staining, and using LysM-eGFP mice by confocal microscopy. Inflammasome components, Il-1?, and Tnf-? mRNA expression were determined by RT-qPCR. IL-1? and TNF-? production (in vitro) and NF-?B activation (in vitro and in vivo) were evaluated by ELISA. In vitro analysis using LPS-primed bone marrow-derived macrophages (BMDMs) was performed 5 h after stimulation with MSU crystals. For these experiments, BMDMs were either treated or pre-treated with budlein A at concentrations of 1, 3, or 10 ?g/mL. Results: We demonstrated that budlein A reduced mechanical hypersensitivity and knee joint edema. Moreover, it reduced neutrophil recruitment, phagocytosis of MSU crystals by neutrophils, and Il-1? and Tnf-? mRNA expression in the knee joint. In vitro, budlein A decreased TNF-? production, which might be related to the inhibition of NF-?B activation. Furthermore, budlein A also reduced the IL-1? maturation, possibly by targeting inflammasome assembly in macrophages. Conclusion: Budlein A reduced pain and inflammation in a model of acute gout arthritis in mice. Therefore, it is likely that molecules with the ability of targeting NF-?B activation and inflammasome assembly, such as budlein A, are interesting approaches to treat gout flares.

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Euglobal-IIIa, a novel acylphloroglucinol-sesquiterpene derivative from Eucalyptus robusta: absolute structure and cytotoxicity

Electronic Supplementary Material

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