Exp Ther Med. 2014 Nov;8(5):1611-1615. |
Germacrone reverses Adriamycin resistance through cell apoptosis in multidrug-resistant breast cancer cells.[Pubmed: 25289068] |
Multidrug resistance (MDR) is a major obstacle to the chemotherapeutic treatment of breast cancer. Germacrone, the main component of Rhizoma Curcuma, has been shown to possess antitumor, anti-inflammatory and immunomodulatory properties. METHODS AND RESULTS: The aim of the present study was to investigate the effect of germacrone on MCF-7/Adriamycin (ADR) multidrug-resistant human breast cancer cells. The treatment of MCF-7/ADR cells with a combination of germacrone and ADR resulted in an increase in cytotoxicity compared with that of ADR alone, as determined using an MTT assay. Flow cytometric analysis revealed that germacrone promoted cell apoptosis in a dose-dependent manner, whilst treatment with germacrone plus ADR enhanced the apoptotic effect synergistically. Furthermore, the results from the western blot analysis demonstrated that augmenting ADR treatment with germacrone resulted in a reduction of anti-apoptotic protein expression levels (bcl-2) and enhancement of pro-apoptotic protein expression levels (p53 and bax) in MCF-7/ADR cells compared with the levels achieved by treatment with ADR alone. In addition, germacrone significantly reduced the expression of P-glycoprotein via the inhibition of the multidrug resistance 1 (MDR1) gene promoter. CONCLUSIONS: These findings demonstrate that germacrone has a critical role against MDR and may be a novel MDR reversal agent for breast cancer chemotherapy. |
Cell Mol Biol (Noisy-le-grand). 2014 Nov 16;60(4):8-12. |
The effects of germacrone on lipopolysaccharide-induced acute lung injury in neonatal rats.[Pubmed: 25399081] |
Germacrone is one of the main bioactive components in the traditional Chinese medicine Rhizoma curcuma and has been shown to possess an anti-inflammatory activity. METHODS AND RESULTS: Our present study aimed to investigate the protective effects of germacrone on lipopolysaccharide (LPS)-induced acute lung injury in neonatal rats. Results showed that germacrone treatment significantly decreased the expression of pro-inflammatory cytokines IL-6 and TNF-α. Meanwhile, the expression of anti-inflammatory mediators TGF-β1 and IL-10 was obviously increased following germacrone administration. The LPS-induced pathological changes in neonatal rats were also attenuated by germacrone treatment. In vitro, MTT and EdU incorporation assay indicated that germacrone administration significantly increased the A549 cell viabilities in a dose-dependent manner. Besides, flow cytometry and TUNEL analysis showed that the cell apoptosis rate was significantly reduced in a concentration-dependent manner after germacrone injection. At the molecular level, we found that germacrone treatment promoted the expression of claudin-4 both in vivo and in vitro as shown by real time PCR and western blot. CONCLUSIONS: Collectively, our study demonstrated that germacrone protected neonatal rats against LPS-induced ALI partially by modulation of claudin-4. |
Antiviral Res. 2013 Dec;100(3):578-88. |
Germacrone inhibits early stages of influenza virus infection.[Pubmed: 24095670] |
Highly pathogenic influenza viruses pose a serious public health threat to humans. Although vaccines are available, antivirals are needed to efficiently control disease progression and virus transmission due to the emergence of drug-resistant viral strains. METHODS AND RESULTS: In this study, germacrone, which is a major component of the essential oils extracted from Rhizoma Curcuma, was found to inhibit influenza virus replication. Germacrone showed antiviral activity against the H1N1 and H3N2 influenza A viruses and the influenza B virus in a dose-dependent manner. The viral protein expression, RNA synthesis and the production of infectious progeny viruses were decreased both in MDCK and A549 cells treated with germacrone. In a time-of-addition study, germacrone was found to exhibit an inhibitory effect on both the attachment/entry step and the early stages of the viral replication cycle. Germacrone also exhibited an effective protection of mice from lethal infection and reduced the virus titres in the lung. Furthermore, the combination of germacrone and oseltamivir exhibited an additive effect on the inhibition of influenza virus infection, both in vitro and in vivo. CONCLUSIONS: Our results suggest that germacrone may have the potential to be developed as a therapeutic agent alone or in combination with other agents for the treatment of influenza virus infection. |