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Phenolic constituents from Parakmeria yunnanensis and their anti-HIV-1 activity
Shan-Zhai Shang,Huan Chen,Cheng-Qin Liang,Zhong-Hua Gao,Xue Du,Rui-Rui Wang,Yi-Ming Shi,Yong-Tang Zheng,Wei-Lie Xiao,Han Dong Sun 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.10
Three new phenolic compounds, yunnanensinsA–C (1–3), together with fourteen known ones (4–17),were isolated from the leaves and stems of Parakmeriayunnanensis. The structures of new compounds wereestablished on the basis of extensive spectroscopic analyses. Several compounds showed weak anti-HIV-1 activity.
Tsung-Han Hou,Jen-Ping Chung,Shang-Shan Chen,Tsu-Liang Chang 한국식품과학회 2013 Food Science and Biotechnology Vol.22 No.3
Hyperglycemia results in the formation of advanced glycation end-products (AGE), resulting in an inflammatory response that induces insulin resistance. Evidence indicates that antioxidants can suppress the formation of reactive oxygen species, decrease levels of AGEs by inhibiting glycation. Black nightshade (Solanum nigrum) can be used as a medicinal food for improving blood glucose; however, the identities of the active compounds and how they counteract diabetes remain unknown. This study demonstrate that 95% ethanolic extracts of black nightshade exerted significant antioxidative activity compared with 50% ethanolic extracts and aqueous extracts. Moreover,95% ethanolic extracts of black nightshade produced antiglycative activity, which contributed to the inhibition of fructosamine and generation of α-dicarbonyl compounds. The concentrations of solasonine and solamargine in the 95% ethanolic extracts were 0.484 and 0.183 mg/mg,respectively. These results suggest that black nightshade might serve as a novel source of functional ingredients that exert antiglycation and anti-diabetes activities.
Guo, Hong-Yan,Xing, Yue,Sun, Yu-Qiao,Liu, Can,Xu, Qian,Shang, Fan-Fan,Zhang, Run-Hui,Jin, Xue-Jun,Chen, Fener,Lee, Jung Joon,Kang, Dongzhou,Shen, Qing-Kun,Quan, Zhe-Shan The Korean Society of Ginseng 2022 Journal of Ginseng Research Vol.46 No.6
Background: Ginseng possesses antitumor effects, and ginsenosides are considered to be one of its main active chemical components. Ginsenosides can further be hydrolyzed to generate secondary saponins, and 20(R)-panaxotriol is an important sapogenin of ginsenosides. We aimed to synthesize a new ginsengenin derivative from 20(R)-panaxotriol and investigate its antitumor activity in vivo and in vitro. Methods: Here, 20(R)-panaxotriol was selected as a precursor and was modified into its derivatives. The new products were characterized by <sup>1</sup>H-NMR, <sup>13</sup>C-NMR and HR-MS and evaluated by molecular docking, MTT, luciferase reporter assay, western blotting, immunofluorescent staining, colony formation assay, EdU labeling and immunofluorescence, apoptosis assay, cells migration assay, transwell assay and in vivo antitumor activity assay. Results: The derivative with the best antitumor activity was identified as 6,12-dihydroxy-4,4,8,10,14-pentamethyl-17-(2,6,6-trimethyltetrahydro-2H-pyran-2-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl(tert-butoxycarbonyl)glycinate (A11). The focus of this research was on the antitumor activity of the derivatives. The efficacy of the derivative A11 (IC<sub>50</sub> < 0.3 µM) was more than 100 times higher than that of 20(R)- panaxotriol (IC<sub>50</sub> > 30 µM). In addition, A11 inhibited the protein expression and nuclear accumulation of the hypoxia-inducible factor HIF-1α in HeLa cells under hypoxic conditions in a dose-dependent manner. Moreover, A11 dose-dependently inhibited the proliferation, migration, and invasion of HeLa cells, while promoting their apoptosis. Notably, the inhibition by A11 was more significant than that by 20(R)-panaxotriol (p < 0.01) in vivo. Conclusion: To our knowledge, this is the first study to report the production of derivative A11 from 20(R)-panaxotriol and its superior antitumor activity compared to its precursor. Moreover, derivative A11 can be used to further study and develop novel antitumor drugs.