Hepatoprotective activity assessment of amino acids derivatives of picroside I and II.

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.

Synthesis and biological evaluation of picroside derivatives as hepatoprotective agents.

Picrorhizae Rhizoma as a hepatoprotective herb, has been applied for thousands of years, and picroside was proved to be its active constituent. In this study, twelve derivatives of picroside were synthesized and the hepatoprotective activity of the derivatives was evaluated on SMMC-7721 cells. Six out of the derivatives had shown a better protective effect on H2O2-induced SMMC-7221 cells than picroside, and the activity of two derivatives (2 and 4) was stronger than that of the reference compound, silybin. Compound 2 shown the strongest protective effect (EC50 = 6.064 ± 1.295 µM).

Investigating vulnerability of ecological industrial symbiosis network based on automatic control theory.

System fluctuations of eco-industrial symbiosis network (EISN) organization due to disturbance are very similar to the controller adjustment in the automatic control theory. Thus, a methodology is proposed in this study to assess the vulnerability of EISN based on the automatic control theory. The results show that the regulator plays a key role to enhance the resilience of the network system to vulnerability. Therefore, it is imperative to strengthen the real-time regulation and control of EISN so that the system stability is improved. In order to further explore the impact of various regulations on the system vulnerability, the influence of system stability is simulated by means of proportional, differential, and integral control. A case study with Guigang eco-industrial park (EIP) was undertaken to test this model. The results showed that when the system was disturbed at different positions, the key nodes which had great influence on system vulnerability could be selected according to the magnitude of simulation curve. By changing the ratio coefficient of proportional, differential, and integral units to adjust the ecological chain network, the system's resilience to vulnerability can be enhanced. Firstly, if basic conditions of EISN organization remain unchanged, the integral control of the policy support and infrastructure sharing should be strengthened. Secondly, the differential regulation should be improved continuously for the technological innovation capability of key node enterprises. Finally, the key chain filling projects should be introduced for proportional control so that the chain network design can be optimized from the source.