• Journal of Ginseng Research
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• v.46 no.6
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• pp.738-749
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• 2022

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 ¹H-NMR, ¹³C-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 (IC₅₀ < 0.3 µM) was more than 100 times higher than that of 20(R)- panaxotriol (IC₅₀ > 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.

• Journal of Life Science
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• v.26 no.8
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• pp.936-942
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• 2016

As the incidence of environmental diseases is increasing due to harmful environmental factors, there is a rising interest in developing eco-friendly materials for housing. In this study, we sought to develop antimicrobial interior fabric blind materials by employing ethanol extract of a medicinal plant Zanthoxylum piperitum DC. As determined by the disc diffusion method, the zones of inhibition of the pericarp ethanol extract at a concentration of 5 mg/disc against Klebsiella pneumoniae, Staphylococcus aureus, and Streptococcus mutans were 13.5±1.5 mm, 14.0±0.5 mm and 15.0±0.1 mm, respectively, whereas the leaf ethanol extract (5 mg/disc) against K. pneumoniae, S. aureus, and S. mutans were 12.8± 0.3 mm, 13.5±1.0 mm, and 12.0±0.1 mm, respectively. The IC₅₀ of the leaf ethanol extract against K. pneumoniae, S. aureus and S. mutans were about 0.5 mg/ml, 0.1 mg/ml and 1.0 mg/ml respectively. To examine whether the leaf ethanol extract possessing antibacterial activity of Z. piperitum DC can be applicable to production of antimicrobial fabric blind materials, the fabrics treated with either 1.0% or 2.0% of the leaf ethanol extract were tested for antibacterial activity against K. pneumoniae and S. aureus using International Standard Fabrics Test Method. The results indicate that the fabric treated with the ethanol extract of Z. piperitum DC possesses an excellent antimicrobial activity against both pathogenic bacteria. These results suggest that Z. piperitum DC may be applicable to producing functional fabrics which are effective in reducing the harmful bacterial factors in indoor environments.