Jing Gao,Shun Yao,Yu Wang,Zhengbo Hou,Chang Yang,Hang Song
Trichosanthin (TCS) is a kind of basic protein separated from Trichosanthes kirilowii Maxim, which is a good food source for human nutrients and has important uses for health. In this study, a series of imidazole-based ionic liquids (ILs) were chosen as catalysts for TCS hydrolysis in both heating and microwave-assisted modes and the hydrolysis was compared with chlorhydric acid and sulfuric acid together with sodium hydroxide for the degree of hydrolysis (DH) of TCS. It was found that the performance of acidic ILs > neutral ILs > basic ILs; [Hmim][HSO4] among the ILs presented the highest DH which was even better than those of inorganic strong acids. Furthermore, the process of hydrolysis was optimized with 3D-response surface methodology (RSM), and the highest degree of hydrolysis could reach to 48.3% (in heating mode) and 93.9% (in microwave-assisted mode). Finally, D001Na type cation-exchange resins were used in the selective adsorption of amino acid products and ILs in an effluent that could be reused. The hydrolysates from TCS showed an enhanced antioxidant activity which was evaluated in three ways. This study could provide a useful foundation for further research and exploitation of TCS.
Triptolide (TP) is a promising anti-tumor candidate derived from the herb Tripterygium wilfordii , but its poor water solubility and multi-organ toxicity limit its application. Here, we developed novel nanoparticles (TP-SP@NPs) modified with dextran sulfate and RGD peptide for double-targeted delivery of TP to both tumor cells and pro-tumor macrophages in pancreatic cancer treatment. TP-SP@NPs exhibited suitable particle size (about 98 nm), good stability and controlled release performance. TP-SP@NPs showed high cellular uptake in Pan02 cells and M2 macrophages through α v β 3 integrin-RGD interaction and SR-A-DS interaction, effectively inhibiting tumor growth by triggering apoptosis of these cells. In Pan02 tumor-bearing mice, TP-SP@NPs specifically accumulated at the tumor site and efficiently decreased the number of M2 macrophages, thereby exerting better curative effect on pancreatic cancer and lower systemic toxicity as compared with TP. As a result, TP-SP@NPs had achieved selective anti-tumor effect, good biosafety and great promise in clinical application.
Background: Panax ginseng Meyer which has been cultivated and grown naturally in mountainous forests is formally called “Lin-Xia-Shan-Shen” (LXSS), but when cultivated it is called garden ginseng (GG), according to the Chinese Pharmacopoeia (2015 edition). The medicinal value of LXSS is significantly higher than that of GG based on the clinical experience of TCM. This study aimed to evaluate the variety of chemical constituents in LXSS and GG. Methods: 18 LXSS and 6 GG samples were investigated using a UPLC-Q-TOF-MS technique. Results: the contents of 16 metabolites, mainly involved in the biosynthesis of rare ginsenosides (ginsenosides Rg3, -Rh1, -Rh2), galactose metabolism (myo-inositol), the citric cycle (citric acid and succinic acid), GABA shunt (GABA) and amino metabolism (alanine and aspartic acid), were higher in LXSS than in GG; while 14 metabolites, mainly involved in starch and sucrose metabolism (fructose and sucrose), amino metabolism (tryptophan, proline, dencichine and pyroglutamic acid) and campesterol biosynthesis (campesterol), were lower in LXSS than in GG. For LXSS with different growing years, 5 metabolites showed a tendency to increase dependent on the number of years, and these were related mainly to galactose metabolism (melibiose), the citric cycle (malic acid), fatty acid metabolism (2-hydroxy stearic acid); while 5 metabolites showed a tendency to decrease on ascending the grades, and these were related to sucrose metabolism (fructose and sucrose), fatty acid metabolism (2-hydroxy hexadecanoic acid) and campesterol biosynthesis (campesterol). Conclusion: this proposed analytical method coupled with multivariate analysis is fast, accurate, and reliable for discriminating GG and high cultivation ages of LXSS samples.
危险品化学品经营许可证（带存储）