1.The basic and applied basic researches are the foundation of research and development of new drugs
Journal of Peking University(Health Sciences) 2001;33(3):193-198
From the soon-to-be-completed Human Genome Project to Combinatorial Chemistry and High-Throughput Screening combined with bioinformatic tools, scie n tific advances are poised to revolutionize drug discovery and even health care. The research directions in the State Key Laboratory of Natural and Biomimetic Dr ugs of Peking University mainly focus on the study of interaction between biolog ical targets and active compounds with structural diversity including endogeno us and exogenous substances, especially the natural products that come from anim als, plants and inorganic medicines. The new lead compounds have been designed and s ynthesized based on the structure-activity relationship and computer modeling. T he research activities are involved in 76 national research projects. From 1996 -20 00, 310 papers have been published, 8 patents obtained an d 14 prizes of scientific achievements awarded by the Chinese government and min istries.
2.Pharmacokinetics of nodakenin in rats
Chinese Pharmacological Bulletin 2003;0(09):-
Aim To investigate the pharmacokinetics of nodakenin(ND),one of main chemical constituents in the rhizome and root of Notopterygium incisum Ting ex H.T.Chang and N.forbesii Boiss.,in rats.Methods SD rats were used throughout the experiment and their body weights ranged from 200 to 220 g.All of them were distributed randomly to different test groups(5 rats per group).Nodakenin was administered at a single dose of 80 mg?kg-1 via tail vein.The blood was collected from the orbital venous plexus at different time points.A reversed-phase high performance liquid chromatography(RP-HPLC) method,in which the analyte was isocratically eluted and the external standard method was used,was developed to determine concentrations of ND in rats.The main parameters of pharmacokinetics were calculated by 3P87 software.Results Under the established conditions of HPLC,the retention time of ND was 6.7 min.The calibration curve was Y=2.0?10-4 X+0.4(r=0.9999) with a validated quantitation range from 0.2 mg?L-1 to 80 mg?L-1.The lower limits of detection(LLOD) and quantification(LLOQ) in rats plasma were 0.01 mg?L-1(S/N=3) and 0.1 mg?L-1(S/N=10),respectively.At the concentrations of 1.0,10.0 and 40.0 mg?L-1,extraction recoveries were ranged from 76.23% to 83.72%.The RSD of the precision intra-and inter-day were less than 5.60%(n=3).ND was stable at room temperature and freeze-thaw cycles.The concentration-time course of ND was best fitted to a two-compartment open model after a single intravenous injection dose of 80 mg?kg-1,which the main pharmacokinetic parameters t1/2?,t1/2?,AUC,Vc,Vp,Vss,CL were 7.02 min,219.27 min,1384.34 mg?min?L-1,0.92 L?kg-1,6.04 L?kg-1,6.96 L?kg-1,0.06 L?kg-1?min-1,respectively.Conclusion The developed method is shown to be rapid,accurate and simple,and can satisfy the requirement of pharmacokinetic study of ND in rat.ND was distributed widely and eliminated moderately after a single intravenous injection dose of 80 mg?kg-1 in rats.
3.Grosmomoside I , a new cucurbitane triterpenoid glycoside from fruits of Momordica grosvenori
Xiuwei YANG ; Jianye ZHANG ; Zhongming QIAN
Chinese Traditional and Herbal Drugs 2005;36(9):1285-1290
Objective To carry out a systematic study on the chemical constituents in the fruits of Momordica grosvenori. Methods To isolate pure compounds by using repeated column chromatography,while the structure of a new compound was determined by detailed spectral analysis. Results Four cucurbitane triterpenoid glycosides, mogroside Ⅱ E (Ⅰ), mogroside Ⅲ (Ⅱ), grosmomoside Ⅰ (Ⅲ), and mogroside Ⅴ (Ⅳ) were isolated from the 50% ethanolic extract of the fruits of M. grosvenori. Conclusion Grosmomoside Ⅰ is a new compound identified as mogrol-3-O-β-D-glucopyranoside-24-O-{[β-D-glucopyranosyl (2-1 ) ]- [β-D-glucopyranosyl (6-1 ) ]-β-D-galactopyranoside } and the other three compounds are known compounds.
4.Effects of treatment with milkvetch root and red sage root injections on changes in blood viscosity and renal function in patients with early diabetic nephropathy
Xueling RUAN ; Xiuwei ZHANG ; Dongwen ZHENG
Chinese Journal of Practical Internal Medicine 2001;0(02):-
Objective To investigate the influence of treatment with milkvetch root and red sage root injections on changes in blood viscosity and renal function in patients with early diabetic nephropathy(EDN).Methods 160 patients with EDN were randomly divided into two groups.The control group (n=80) was treated with conventional therapy for diabetes,and the treatment group (n=80) was treated with milkvetch root injection combined with red sage root injection based on conventional therapy for 4 weeks.Results After the above-mentioned therapy the parameters of blood viscosity were significantly decreased(P
5.Expression and Significance of TRIM24 in Uroepithelium Cell Carcinoma of Bladder
Xiuwei ZHANG ; Huihui XU ; Dongwei XUE
Journal of China Medical University 2016;45(4):365-367
Objective To detect the expression of TRIM24 in uroepithelium cell carcinoma of bladder(BUCC)and analyze the relationship be?tween its expression and clinical pathological factors. Methods Immunohistochemical methods were employed to evaluate protein level of TRIM24 in BUCC. Results TRIM24 expression was observed in the nuclear compartments of tumor cells,while normal epithelia of bladder tissues exhibited negative results. For 72 BUCC tissues,TRIM24 overexpression(score≥4)was observed in 41.6%of cases(30/72). TRIM24 expression correlat?ed with invasive depth(P=0.029)and patients with high TRIM24 expression had high grade of BUCC(P=0.043). Conclusion There was sig?nificant over expression of TRIM24 in BUCC,which was correlated with poor differentiation and high grade of BUCC. It may become a candidate tar?get gene for the treatment of human uroepithelium cell carcinoma of bladder.
6.New natural saponins from fruits of Momordica grosvenori
Xiuwei YANG ; Jianye ZHANG ; Zhongming QIAN
Chinese Traditional and Herbal Drugs 1994;0(06):-
Objective To study the chemical constituents in the fruits of Momordica grosvenori. Methods Isolation and purification of the constituents were carried out on column chromatography. Their structures were identified by NMR and MS spectral analyses. Results Ten compounds were isolated and elucidated as kaempferol (Ⅰ), kaempferol 7-O-?-L-rhamnopyranoside (Ⅱ), kaempferitrin (Ⅲ), mogroside ⅡE (Ⅳ), mogroside Ⅲ (Ⅴ), kaempferol 3-O-?-L-rhamnopyranoside-7-O-[?-D-glucopyranosyl (1-2)-?-L-rhamnopyranoside] (Ⅵ), mogroside ⅣA (Ⅶ), grosmomoside Ⅰ (Ⅷ), mogroside Ⅴ (Ⅸ), and mogroside ⅡA1 (Ⅹ). Conclusion Compounds Ⅶ and Ⅹ are new natural products, and Ⅰ is isolated from the fruits of M. grosvenori for the first time.
7.Research progress on system management of cancer-related fatigue in lung cancer
Jianying PENG ; Qiuqiang CHEN ; Xiuxia WEI ; Xiuwei ZHANG
Chinese Journal of Practical Nursing 2016;32(11):876-880
To review the scientific evidence of system management for lung cancer patients with cancer- related fatigue by the method of literature review and evaluate researchers on authenticity, importance and applicability, in order to improve the nursing quality and the quality of life of them. Interventions of lung cancer patients with cancer- related fatigue mainly includes: non- drug intervention, drug intervention and self- management. The use of intervention measures should be combined with the situation of the patients. however, many of the effectiveness of the intervention measures not sure, need large sample randomized controlled trial verifies the results .
8.The effectiveness of intermittent nasogastric feeding on enteral nutrition of critical patients:a Meta-analysis
Xiuxia WEI ; Yiyu ZHUANG ; Jianying PENG ; Xiuwei ZHANG
Chinese Journal of Practical Nursing 2015;(30):2310-2314
Objective To systematically evaluate the effectiveness of intermittent nasogastric feeding on enteral nutrition of critical patients. Methods The relevant randomized controlled trials were searched in the Cochrane Library, PubMed, EMbase, Web of Science, JBI Library and the databases of China National Knowledge Infrastructure (CNKI), China Scientific Journal Database by VIP (VIP), Wanfang Database. The studies were selected according to the inclusion and exclusion criteria by two reviewers. Meta- analysis was conducted by using RevMan 5.2. Results Nine RCTs were included involving 558 patients. The results of meta- analysis showed that intermittent nasogastric feeding was greater than continuous pump feeding in the incidence of constipation, OR=0.32, 95%CI 0.14~0.71, P<0.05, the difference was significant. However, they were alike in the incidences of diarrhea, aspiration pneumonia, gastric residuals, vomiting, abdominal distension and effects of nutrition, there was no statistical difference (P>0.05). Conclusions Intermittent nasogastric feeding and continuous pump feeding did not affect the incidence of diarrhea, aspiration pneumonia, gastric residuals, vomiting, abdominal distension and the effects of nutrition. However, the incidence of constipation was significantly less in patients receiving intermittent nasogastric feeding.
9.A study on yearly and daily circadian rhythm of cardiovascular events
Xiuwei ZHANG ; Zhijun TAN ; Yanling LI ; Bin WANG ; Ai YU ; Guoqing ZHANG
Chinese Journal of Internal Medicine 2009;48(10):818-820
Objective To investigate the circadian and seasonal distribution of cardiovascular events (CVE) and the relationship between average monthly temperature and the incidence of CVE. Methods A total of 5837 emergency patients with CVE were enrolled from 1997 to 2007. The exact admission time of each patient was registered. The average monthly temperature data from a regional weather station for this time period was supplied by the meteorological office of the city. The relationship between the average monthly temperature and the incidence of CVE was explored and the corresponding curves were plotted. Results The occurrence of CVE has obvious seasonal variation, and its a higher tendency of episodes was found in spring and winter periods. High incidence of acute myocardial infarction, angina pectoris, acute left-sided heart failure, hypertensive crisis, and sudden death occurred in spring and winter as wee as the time for a change of season, that is, January, February, March, April, October, November, and December. There was a significant negative correlation between the incidence and the average monthly temperature (P<0.005-0.001). Circadian rhythm of CVE was present, with a peak in the early morning and forenoon. Conclusion There are circadian and circannian rhythms of the incidence of CVE. Cold weather condition is a risk factor for the occurrence of CVE, which usually peaks in the early morning and forenoon.
10.Effects of Sappan Lignum and Chuanxiong Rhizoma on Expression of ABCG2 Protein of PG-BE1 Stem Like Cells in Vivo
Yaohan WANG ; Peitong ZHANG ; Dong YANG ; Haiying HAN ; Xiuwei GUO ; Xin QI ; Yun ZHANG
Chinese Journal of Information on Traditional Chinese Medicine 2017;24(8):60-65
Objective To observe the effects of different doses of Sappan Lignum and Chuanxiong Rhizoma on tumor stem cells marker ABCG2 in vivo. Methods Sphere cells obtained from serum culture were inoculated in nude mouse armpit, which were randomly divided into 5 groups: control group, Sappan Lignum high- and low-dose groups, and Chuanxiong Rhizoma high- and low-dose groups. Each medication group was given relevant medicine for gavage. 21 days later, inhibition tumor rate and ABCG2 protein and mRNA expression were detected with confocal microscope, Western blot, and RT-PCR. Results The sphere cells obtained from serum free culture had the abilities of cancer stem cells, such as proliferation, anti-aptosis and high expression of cancer stem cells markers. Chuanxiong Rhizoma high- and low-dose groups could inhibit tumor growth (P<0.05), and the inhibitory rate of Chuanxiong Rhizoma low-dose group was higher than the Chuanxiong Rhizoma high-dose group. Sappan Lignum high- and low-dose groups inhibited tumor growth without statistical significiance (P>0.05). Compared with the control group, Chuanxiong Rhizoma low-dose group could significantly inhibit the expression of resistant protein of ABCG2. Sappan Lignum high- and low-dose groups could not inhibit the protein expression of ABCG2. Each medication group up-regulated the mRNA expression of ABCG2 except for Chuanxiong Rhizoma low-dose group. Conclusion Low dose of Chuanxiong Rhizoma can inhibit the expression of ABCG2 protein levels, which can be the targeting killer for cancer stem cells.