Herbal Textual Research on Rhapontici Radix in Famous Classical Formulas / 中国实验方剂学杂志

This article systematically sorted out and researched the name， origin， harvesting and other aspects of Rhapontici Radix by referring to ancient materia medica， medical books and prescription books， combined with modern literature， in order to provide a reference basis for the development of the famous classical formulas containing this herb. According to the results of the herbal textual research， it can be seen that all the generations of the materia medica have taken Loulu as the proper name， and there are also aliases such as Luligen， Laowenghua and Jiahao. The mainstream base of Rhapontici Radix recorded in the past dynasties was the present Compositae plant Rhaponticum uniflorum， which is mostly used as medicine with roots. Since the Tang dynasty， the stems and leaves of Siphonostegia chinensis have been used as Rhapontici Radix in the northern region. Until modern times， Qizhou Pharmacognosy began to differentiate it into two categories， Qizhou Loulu and Yuzhou Loulu， according to the commodity circulation at that time， producing area and origin， of which Yuzhou Loulu is the roots of Echinops latifolius， a plant of Compositae family. In ancient times， the quality of Loulu was based on "the one that comes out of Shanzhou is the best". However， in modern times， the quality of Qizhou Loulu is better if the surface is black， neat， sturdy， firm， not broken， and without a withered heart， while the quality of Yuzhou Loulu is better if the branches are thick and long with an earthy-brown surface， solid texture and neat in length. In ancient times， most of the harvesting and processing of Loulu was "harvesting the roots in lunar August and drying them in the shade"， while in modern times， the roots are mostly excavated in the spring and autumn， and dried in the sun. Its ancient method of processing is to mix and steam with licorice， nowadays， it is prepared by removing impurities， washing， moistening thoroughly， cutting into thick slices and drying in the sun， and then taking the raw products as medicine. Based on the research conclusion， it is suggested that when developing and utilizing the famous classical formulas containing Loulu， the background of the formula should be verified， and if the original formula indicated the requirement of processing， it should be processed according to the requirement， but if not， it is recommended to use raw products as medicine.

Influence of different culture methods in DNA methylation status of breast cancer MDA-MB-23 1 cells / 吉林大学学报(医学版)

Objective:To explore the influence of different cell culture methods in the genome-wide DNA methylation status of breast cancer MDA-MB-231 cells,and to clarify the relationship between genome-wide DNA methylation status and cell growth environment and the role of genome-wide DNA methylation status in the occurrence and development of tumor.Methods:The MDA-MB-231 cells were cultured with 2D and 3D cell culture models and mouse orthotopic transplantation model (Ti model)and collected, then DNA was extracted by DNA extraction kit and the genome-wide DNA methylation status of MDA-MB-231 cells after cultured with three different culture methods was detected by DNA methylation chip,then the value of beta,DiffScore and Delta_Beta of the CpG loci of each gene were calculated by applying Genomestudio software, and the differential methylation genes were screened by Genomestudio software and GO and Pathway analysis of these genes were performed in DAVID on-line analysis tool.Results:All 480 genes of the MDA-MB-231 cells showed significant differences in the degree of methylation in 3D and 2D models (P<0.05);86 448 genes in 3D and Ti models (P<0.05);90 005 genes in Ti and 2D models (P<0.05).The differential methylation genes in 3D and 2D,3D and Ti,and Ti and 2D models were enriched on the multicellular organismal development term and cell differentiation term (P<0.05);also on MAPK signaling pathway,cell adhesion molecules (CAMs),and regulation of actin cytoskeleton (P<0.05). Conclusion:There are differences in genome-wide DNA methylation status of MDA-MB-231 cells cultured in 2D, 3D cell culture and Ti models.

Design, synthesis and anti-proliferative activity of novel coumarin derivatives linking Schiff base and aryl nitrogen mustard / 药学学报

To explore novel coumarin derivatives with more potent anti-proliferative activity, a series of novel compounds were designed and synthesized by linking Schiff base and N, N-bis (2-chloroethyl) amine pharmacophore of nitrogen mustards to the coumarin's framework. Their structures were confirmed by 1H NMR, MS and element analysis techniques. In vitro anti-proliferative activities were evaluated against HepG2, DU145 and MCF7 cell lines by the standard MTT assay. The results showed that some of the target compounds exhibited strong anti-proliferative activities against selected tumor cells, and compounds 7c, 7f, 7g, 7h and 7q were better than or equal to the activities of positive control, they deserved further development.

Design, synthesis and activities of 4-(2-acetoxybenzoylamino) butyramide derivatives / 药学学报

To explore new agents of gamma-aminobutyric acid (GABA) derivatives with more potent antiepileptic activity, a series of 4-(2-acetoxybenzoylamino) butyramide derivatives were designed and synthesized. All of the novel compounds (5a-51) were synthesized from GABA as starting material, and their structures were confirmed with IR, 1H NMR, EI-MS and elemental analysis. Preliminary pharmacological test in vitro showed that all target compounds displayed strong antiepileptic activities and were worth for further study. The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyramide derivatives was also discussed preliminarily.

Synthesis and activities of 4-(2-acetoxybenzoylamino) butyramide heterocyclic compounds / 药学学报

It has been demonstrated by our previous research that 4-(2-acetoxybenzoylamino) butyramide derivatives exhibited good antiepileptic activities. In this paper, to explore the SAR and improve the antiepileptic activities of these derivatives, a series of novel 4-(2-acetoxybenzoylamino) butyramide heterocyclic compounds (5a-5n) were synthesized and biologically evaluated. Their structures were confirmed by 1H MNR, ESI-MS and elemental analysis. Pharmacological test in vivo showed that target compounds (5f, 5i-5n) displayed strong antiepileptic activities on 4-AP induced epilepsy in mice with ED50 values ranging from 0.3137 to 0.3604 mmol x kg(-1).