Optimization of processing technology and study on antioxidant activity in vivo of superfine powder of Granati Pericarpium / 中草药

Objective: Processing technology and antioxidant activity in vivo of pomegranate superfine powder were investigated. Methods: Processing technology of superfine powder of Granati Pericarpium was optimized using single-factor tests and response surface methodology (RSM). The antioxidant effect in vivo of superfine powder of Granati Pericarpium with different particle, vitamin E, and normal saline were studied. Results: The optimally grinding conditions for Granati Pericarpium were grinding time of 25 min, grinding temperature of -17℃, and input quantity of 198 g. Under the optimally grinding conditions, the minimum particle size of superfine powder of Granati Pericarpium was 7.68 μm which was close to the predicted value of 7.96 μm. Therefore, the established regression model has good prediction capability. Experimental results show that the superfine powder and vitamin E groups compared with the coarse powder and blank groups could significantly improve the activity of SOD, CAT, and GSH-Px, and reduce the content of MDA in serum of mice. Conclusion: The ability of superfine powder group on the protection of membrane lipid peroxidation and scavenge free radical is quite superior. It indicates that the active ingredients in the superfine powder of Granati Pericarpium could be dissolved better and more quickly in solvent than those in coarse powder. Therefore, the superfine powder of Granati Pericarpium has the better anti-oxidant effect in vivo.

Research progress on plant resources distribution of vitexin and its pharmacological effects / 中国中药杂志

Vitexin, a naturally occurring flavone glycoside in plants, has many pharmacological effects, which is widely distributed in nature. This paper reviewed the research progress of the distribution of vitexin in the plant resources and its pharmacological effects, and summarized its application prospects, aiming to provide a useful reference for the development of vitexin-enriched plant resources.

Simultaneous quantitative determination of five alkaloids in Catharanthus roseus by HPLC-ESI-MS/MS / 中国天然药物

AIM@#To establish a method to simultaneously determine the main five alkaloids of Catharanthus roseus for trace samples, a high-performance liquid chromatography-electrospray ionization-tandem mass spectrometry (HPLC-ESI-MS/MS) analysis method was developed.@*METHOD@#The five Catharanthus alkaloids, vinblastine, vincristine, vinleurosine, vindoline, and catharanthine were chromatographically separated on a C18 HPLC column. The mobile phase was methanol-15 nmol·L(-1) ammonium acetate containing 0.02% formic acid (65 : 35, V/V). The quantification of these alkaloids was based on the Multiple Reaction Monitoring (MRM) mode.@*RESULTS@#This method was validated, and the results achieved the aims of the study. The intra- and inter-day precision and accuracy of the five alkaloids were within 1.2%-11.5% (RSD%) and -10.9%-10.5% (RE%). The recovery rates of the five alkaloids of samples were from 79.9% to 91.5%. The five analytes were stable at room temperature for 2 h, at 4 °C for 12 h, and at -20 °C for two weeks. The developed method was applied successfully to determine the content of the five alkaloids in three plant parts of three batches of C. roseus with a minute amount collected from three regions of China.@*CONCLUSION@#The HPLC-ESI-MS/MS method can be used for the simultaneous determination of five important alkaloids in trace C. roseus samples.

Preparation, activity and targeting ability evaluation in vitro on folate mediated epigallocatechin-3-gallate albumin nanoparticles / 药学学报

To study the preparation, activity and targeting ability evaluation in vitro on epigallocatechin-3-gallate (EGCG) bovine serum albumin nanoparticles targeting to PC-3 cells, the folate mediated EGCG bovine serum albumin nanoparticles (FA-EGCG-BSANP) were prepared by desolvation process. The morphology and particle size of the nanoparticles were determined by atomic force microscope (AFM). HPLC was used to analyse the entrapment efficiency and drug loading rate of EGCG The amount of folate conjugation on the BSANP was determined by quantitative ultraviolet (UV) spectrophotometer analysis. The targeting ability to PC-3 was observed using laser scanning confocal microscope (LSCM) and fluorophotometer microscope. And the activity of FA-EGCG-BSANP was mensurated by MTT method. The morphology and particle size distribution of FA-EGCG-BSANP were uniform and even with the mean particle size of 200 nm. The entrapment efficiency and loading rate of EGCG were (81.5 +/- 1.8) % and (29.3 +/- 0.6) %, respectively, and the amount of folate conjugation was 18.363 microg x mg(-1) BSA. The FA-EGCG-BSANP uptakes by cultured PC-3 cells were 23.65 times the amount of EGCG-BSANP in a concentration dependant manner. The lethality of PC-3 cells treated with FA-EGCG-BSA was 82.8%, while those treated with EGCG and EGCG-BSANP were 58.6% and 55.1%, respectively. And lethality of PC-3 cells was positively correlated with the nanoparticles uptake amount. FA-EGCG-BSANP can significantly promote EGCG to PC-3 cells sites and improve their efficacy, which is considered to an experimental foundation for further research on its activity, targeting ability and metabolism in vivo.

Isolation and purification of 10-hydroxycamptothecin and vincoside-lactam from Camptotheca acuminata seed by polyamide / 中国中药杂志

To investigate the technological parameters of the isolation and purification of 10-hydroxycamptothecin and vincoside-lactam from Camptotheca acuminata seed by polyamide. The static arid dynamic adsorption characteristics of 10-hydroxycamptothecin and vincoside-lactam on polyamide were studied, and the contents were determined by HPLC. The optimum parameters for adsorption were as follows: the contents of 10-hydroxycamptothecin and vincoside-lactam in the extracts were 0.189 g x L(-1) and 0.334 g x L(-1), respectively, pH 6, flow rate was 1.0 mL x min(-1), processing volume was 3 BV; for desorption: ethanol-water (60:40), flow rate was 1.0 mL x min(-1), 5 BV as an eluent. After treated with polyamide, the contents of 10-hydroxycamptothecin and vincoside-lactam were 17.52% and 32.87%, respectively, the recovery yields were 66.05% and 75.86%, respectively. Results showed that polyamide revealed a good ability to separate 10-hydroxycamptothecin and vincoside-lactam. Therefore, we concluded that results in this study may provide scientific references for the large-scale production of 10-hydroxycamptothecin and vincoside-lactam extracted from C. acuminata seed.

Synthesis of camptothecin glycosides by phase transfer-catalysis and its inhibitory activity against topo I / 药学学报

<p><b>AIM</b>To find new anticancer drug based on the structure of 10-hydroxy camptothecin.</p><p><b>METHODS</b>Six camptothecin glycosides (7-12) were synthesized by phase transfer catalysis. The structures of all compounds synthesized were determined by 1H NMR, IR and MS. Their antitumor activity was evaluated on cancer cells in vitro, and inhibitory activity against Topo I was evaluated by molecular biologic method.</p><p><b>RESULTS AND CONCLUSION</b>The result indicated that the yield of camptothecin glycosides by phase transfer catalysis is much higher than by the method from literature, camptothecin glycosides have much lower cytotoxicities on cancer cell in vitro, but have better inhibitory activity of topo I.</p>

Synthesis and antitumor activities of 10-hydroxy camptothecin derivatives / 药学学报

<p><b>AIM</b>To find new anticancer drug based on the structure of 10-hydroxy camptothecin.</p><p><b>METHODS</b>Seven camptothecin derivatives (3 -9) were synthesized and the antitumor activities of these derivatives were evaluated.</p><p><b>RESULTS</b>Structures of seven new compounds were determined by 1HNMR, IR, MS. Seven compounds showed inhibitory effects on Hela, BEL-7402, 7901 cell lines in vitro. Especially, compound 4 showed high bioactivities to all of the tumor cells in vitro, its anticancer activity against human cervical carcinoma Hela was much higher than that of 10-hydroxy camptothecin.</p><p><b>CONCLUSION</b>Some compounds are worth further studying.</p>