NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
·
2018
·Vol. 392
·期 2
·177-187
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IF 2.238
Qiao Zhe,Cheng Yao,Liu Shiyuan,Ma Zhenchuan,Li Shaomin,Zhang Wei
Casticin, a flavonoid isolated from Vitex species, has been found to have anti-tumor property in multiple human cancers. The present study aimed to investigate the effect of casticin on the proliferation and apoptosis of esophageal cancer (EC) cells, and further illustrate the underlying mechanisms. In in vitro studies, human EC cell lines TE-1 and ECA-109 were treated with various concentrations of casticin (low-, middle-, and high-dose groups). The results showed that casticin dose-dependently inhibited the proliferation and clonogenicity of EC cells and induced cell cycle arrest in sub-G1 and G2 phases. Furthermore, casticin markedly enhanced EC cell apoptosis as detected by flow cytometry and Hoechst 33342 staining. The level of anti-apoptotic Bcl-2 protein was decreased, while the levels of pro-apoptotic Bax, cleaved-caspase-3, cleaved-caspase-9, and cleaved-PARP were conversely increased in casticin-treated TE-1 and ECA-109 cells. Moreover, casticin decreased the mitochondrial membrane potential and increased the release of mitochondrial cytochrome C into cytoplasm. In addition, the JNK signaling pathway was involved in casticin-medicated anti-proliferation and pro-apoptosis. Cells pretreated with SP600125, a JNK pathway inhibitor, partially abolished the effect of casticin. Finally, the anti-tumor property of casticin was confirmed in in vivo xenograft models. Overall, we provided both in vitro and in vivo evidences that casticin inhibited the proliferation and induced apoptosis of EC cells, and the anti-tumor action of casticin was mediated, in part, by the mitochondrial-dependent apoptosis and the activation of JNK signaling pathway.
研究领域:
肿瘤学
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药理学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2024
·
IF 8.5
Zhi-Xin Peng,Hui-Wen Gu,Yuan Pan,Yan Wang,Jun Yan,Wanjun Long,Haiyan Fu,Yuanbin She
In recent years, red wine drinking has become more popular in China owing to its antioxidant effects. However, the key antioxidant compounds and their action mechanisms of Chinese red wines are still unclear. Herein, the antioxidant activities and chemical compositions of 45 Chinese Cabernet Sauvignon red wine samples were determined using chemical antioxidant assays and an UHPLC-QTOF-MS-based untargeted metabolomics method. The key antioxidant compounds in red wines and potential action mechanisms were revealed by integrating network pharmacology and molecular docking approaches. Results showed that there are 8 key antioxidant compounds in the red wine samples. These compounds are involved in several metabolic pathways in the body, particularly PI3K/AKT. What's more, they bind to the core antioxidant targets through hydrogen bonding and hydrophobic interaction. Among them, myricetin, laricitrin, 2,3,8-tri- O -methylellagic acid and AKT1 have the highest binding energies. This study could provide the theoretical basis for further investigation of physiological activities and functions of Chinese red wines.
研究领域:
食品科学
·
药理学
·
生物化学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Saudi Chemical Society
·
2021
·
IF 3.932
Yujie Hua,Xican Li,Wenhui Zhang,Ban Chen,Yamei Liu,Xiaojun Zhao,Hong Xie,Dongfeng Chen
Folium Hibisci Mutabilis, a new member of Chinese Pharmacopoeia, can treat some diseases induced by reactive oxygen species. The study prepared a lyophilized aqueous extract of Folium Hibisci Mutabilis (LAFHM). LAFHM was found to enrich eight flavonoids (i.e., quercetin, luteolin, hyperoside, isoquercitrin, rutin, kaempferol, tiliroside, and vitexin) by HPLC analysis. These flavonoids were further compared using antioxidant assays, where triliroside and vitexin always exhibited higher IC 50 values than the others. In ultra-performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight tandem mass spectrometry analysis, these flavonoids could basically give two characteristic m / z values (226 and 196) and their corresponding double m / z values (i.e., 602, 570, 926, 926, 570, 1186, and 862), when treated by 1,1-diphenyl-2-picryl-hydrazl radical (DPPH • ). Finally, the coupling products of DPPH • -treated triliroside were investigated using computational chemistry. It was found that the –OH in para- coumaroyl moiety to have the lowest bond disassociation energy among all phenolic -OHs in the triliroside. In conclusion, Folium Hibisci Mutabilis contains the above eight antioxidant flavonoids. Despite of the different antioxidant levels, they can generally produce flavonoid-radical coupling product and flavonoid-flavonoid homodimer during antioxidant process. Especially, tiliroside uses para -coumaroyl as linker to construct a tiliroside-radical coupling product at the meta -carbon atom.
研究领域:
药理学
·
分析化学
·
计算化学
·
植物科学
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）