Hepatoprotective activity assessment of amino acids derivatives of picroside I and II
| Autor: | Hua Han, ZhengQing Li, PeiLiang Dong, Xin Yin, ZhenLei Gao |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Picrorhiza kurroa
Iridoid Glucosides Protective Agents 01 natural sciences Biochemistry Picroside I chemistry.chemical_compound Pharmacokinetics Bromide Drug Discovery Humans Amino Acids Derivatization Cell Proliferation Picrorhiza Pharmacology chemistry.chemical_classification Plants Medicinal Traditional medicine 010405 organic chemistry Organic Chemistry Hep G2 Cells Hydrogen Peroxide In vitro 0104 chemical sciences Amino acid Rhizome 010404 medicinal & biomolecular chemistry Liver chemistry Cinnamates Molecular Medicine |
| Zdroj: | Chemical Biology & Drug Design. 97:341-348 |
| ISSN: | 1747-0285 1747-0277 |
| Popis: | Picrorhiza kurroa has a long medicinal history as a traditional medicinal plant in China and India that is widely used in clinical treatments. It is a common treatment for liver diseases, fever, diarrhoea, indigestion, and some other diseases. Modern pharmacological studies proved that P. kurroa rhizomes have high levels of picroside I and II, which were identified as main constituents with anti-inflammatory and hepatoprotective activities. In our study, we used picroside I and II as the lead compounds to generate derivatives by reactions with Boc-valine or Boc-proline, which underwent dehydration and condensation with the hydroxyl groups in the lead compounds in the presence of coupling reagent N,N'-dicyclohexylcarbodiimide. We synthesized 11 derivatives and examined their hepatoprotective effects in vitro by assessing the proliferation rates of H2 O2 -exposed HepG2 cells using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. We found that some derivatives promoted higher proliferation rates in HepG2 cells than the natural compounds before derivatization, suggesting that those derivatives possessed an improved hepatoprotective capacity. The novel derivatization strategy for picrosides had the additional benefit that the esterification of their hydroxyl groups created derivatives not only with increased stability but also with improved pharmacokinetic properties and potentially prolonged half-life. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text