1.Inhibitory effects of ligustilide and butylidenephthalide on bFGF-stimulated proliferation of rat smooth muscle cells
Acta Pharmaceutica Sinica 2006;41(2):161-165
Aim To investigate the bio-affinities of ligustilide and butylidenephthalide to rat aortic smooth muscle cells and the inhibitory effects of them on bFGF-stimulated proliferation of rat vascular smooth muscle cell (VSMC). Methods VSMCs were cultured from rat aorta pectoralis and identified by an immunohistochemical method. The bio-affinities between solute (ligustilide or butylidenephthalide) and cell membrane were measured by rat aortic cell membrane chromatography (CMC). The inhibitory effects of ligustilide and butylidenephthalide on bFGF-stimulated VSMC proliferation were evaluated by MTT colorimetric method. Results Both ligustilide and butylidenephthalide had selective affinities to rat aortic smooth muscle cell as the same as verapamil, one of the calcium ion antagonists. They could potently separately (P < 0.05 ), but had no effects on the normal VSMC growth. Conclusion Both ligustilide and butylidenephthalide can inhibit the abnormal proliferation of VSMC induced by bFGF.
2.Qualitative and quantitative analysis of the effective part and effective components of Radix Puerariae
Journal of Xi'an Jiaotong University(Medical Sciences) 1981;0(03):-
Objective To establish a qualitative and quantitative method for controlling the quality of Radix Puerariae and its preparation. Methods The qualitative fingerprint of effective part (extract part of ethyl acetate) was obtained by using RP-HPLC with methanol-water (42∶58) as mobile phase and UV detection at 250 nm . The quantitative measurement of effective components (puerarin and daidzein) was finished under the above chromatographic conditions. And the 11 kinds of different samples of Radix Puerariae were analyzed by the method. Results Under the qualitative conditions, the 5 common peaks in RP-HPLC fingerprint of the effective part could be used as index peaks for qualitative identification. In RP-HPLC quantitative analysis, the recoveries of the method were 98.0% with RSD of 1.30% for puerarin and 95.4% with RSD of 1.61% for daidzein, respectively. The amount of puerarin and daidzein in Radix Puerariae was 0.213%~3.626% and 0.012%~ 0.049% , respectively. Conclusion The analytical method with qualitative fingerprint of effective part and quantitative measurement of effective components of Radix Puerariae can be accurately used for controlling its quality.
3.Preparation and dissolution of solid dispersion of angelica dahurica coumarins
Dan HE ; Lin YANG ; Langchong HE
Chinese Traditional Patent Medicine 1992;0(01):-
AIM: To prepare the solid dispersions of angelica dahurica coumarins and measure their dissolution characteristics. METHODS: The solid dispersions were obtained by using the melted and dissolved methods with PEG6000, PVP and poloxamer188 as carriers respectively.The existing state of the coumarins in the solid dispersions were identificated by the differential scanning calorimetery. The dissolution characteristics of the solid dispersions in vitro were analyzed by HPLC method under the chromatographic conditions with ThermoC_(18)(150 mm?4.6 mm,5 ?m) as analytial column and methanol/water(70∶30)as mobile phase,using imperatorin as testing index. RESULTS: The melted and dissolved methods can be used to prepare the solid dispersions.The coumarins were completely dispersed in carrier and formed an euctics mixture with the carrier.The dissolution rates of all solid dispersion were increased obviously. CONCLUSION: The solid dispersion prepared with PVP can increase the solubility and dissolution of the coumarins.
4.STUDIES ON IN-VIVO PROCESS OF THE ENANTIOMERS OF NICARDIPINE IN RABBIT BY COUPLED CHIRAL AND ACHIRAL HPLC
Sicen WANG ; Langchong HE ; Fei LIU
Acta Pharmaceutica Sinica 2001;36(5):364-367
AIM To study the differences of the pharmacokinetics and tissue distribution of two enantiomers of nicardipine in the rabbit. METHODS Biological samples were diluted by 1 mol*L-1 NaOH solution and extracted with n-hexane - ethyl acetate (1∶1). The concentrations of S-nicardipine and R-nicardipine in samples were determined by coupled achiral C18 column (150 mm×4.6 mm, 5 μm) and chiral OJ column (250 mm×4.6 mm, 10 μm) chromatography. RESULTS The racemic nicardipine and the enantiomers in sample were separated well by the coupled system. The linear range was 55-550 ng*mL-1 for both enantiomers. The within-day and between-days RSD (n=5) were 5.25% and 8.97%, and the relative recoveries were 99.99% and 97.10% for R- and S- enantiomer, respectively. The mean Tmax, Cmax and AUC values were (2.49±0.03) h, (134±2) ng*mL-1 and (1082±32) ng*mL-1*h for S-nicardipine and (1.24±0.05) h, (109±2) ng*mL-1 and (778±22) ng*mL-1*h for R-nicardipine. The concentration of S-nicardipine were generally higher than that of R-nicardipine in main target tissues and cells. CONCLUSION There were significant differences between the two enantiomers of nicardipine in rabbit in pharmacokinetics and tissue distribution.
5.Solvent Extraction Methods of Imperatorin in Radix Angelicae Dahurica
Mingjin LIANG ; Guangde YANG ; Langchong HE ;
Chinese Traditional Patent Medicine 1992;0(12):-
Objective: To build an extraction method of coumarins from Radix Angelicae Dahuricae. Methods: The solvent varieties, polarities, and extraction methods were systematically studied by TLC with imperatorin as marker.Results: The more effective way to extract coumarins from Radix Angelicae Dahurica was refluent extraction with 4 times amount of 95% alcohol twice (one hour each time).Conclusion: The Solvent varieties and extraction method showed greater effects than others on the extraction efficiency of imperatorin.
7.Screening the Effective Component of Rhizoma Tupistrae Chinensis with Inhibiting Angiogenesis
Maixia MENG ; Zhifeng YANG ; Langchong HE
Chinese Journal of Information on Traditional Chinese Medicine 2006;0(01):-
Objective To discover the effective component of Rhizoma Tupistrae chinensis with inhibiting angiogenesis. Methods Several parts of Rhizoma Tupistrae chinensis were obtained by using different extraction solvents. They were screened by the model of ECV304 cell membrane chromatography with anti-VEGF antibody as a control drug. The inhibition of effective component (ZGQ-C) on ECV304 proliferation in vitro was examined by MTT assay. Results The inhibition rate (40.51%,51.11%,63.54%,74.32%,81.26%) was correlated with the ZGQ-C concentration. The ECV304 cell had significantly changed in morphology. Conclusion The ZGQ-C is an effective component for inhibiting angiogenesis. The screening results on the model have a good correlation with that of MTT assay.
8.The separation of ?-adrenoceptor antagonist enantiomers on Chiralcel~ OD column
Fei YANG ; Sicen WANG ; Langchong HE
Journal of Xi'an Jiaotong University(Medical Sciences) 1981;0(02):-
Objective To study the enantioselective characteristics and laws of ?-adrenoceptor antagonist isomers on Chiralcel ○R OD column. Methods The experiments were performed under the following HPLC conditions: a Chiralcel OD column (250 mm?4.6 mm, 10 ?m) as analytical column, a mixture of n-hexane/2-propanol/ triethylamine as the mobile phase, the fluorescence detection wavelengths at 275 nm (? ex) and 310 nm (? em), and the flow rate at 0.5 mL?min -1. The effect of interaction between stationary phase and 2-propanol or triethylamine concentration in mobile phase on the enantiomer resolution were investigated by the stoichiometric displacement model for retention. Results The lgI values of R-enantiomers of 3 out of 5 ?-adrenoceptor antagonist were higher than those of S-enantiomers. The 2-propanol in mobile phase would differently affect the resolution between enantiomers for each ?-adrenoceptor. With the increase of triethylamine concentration in mobile phase, the capacity factor (k′) of the enantiomers decreased but the resolution increased. Conclusion The lgI and Z values of SDM-R could be employed to characterize the resolution efficiency of Chiralcel OD column and the specific effect of enantiomers interacted with the stationary phase. Adding triethylamine in mobile phase will increase the resolution efficacy and changing column temperature can promote enantiomer resolution.
9.Analytical methods with qualitative fingerprint and quantitative measurement of effective components of Cortex Moutan
Liang ZHAO ; Langchong HE ; Shengqing DU
Journal of Xi'an Jiaotong University(Medical Sciences) 2003;0(06):-
Objective To establish a qualitative and quanti ta tive method with RP-HPLC for controlling the quality of Cortex Moutan. Methods The experimental conditions of the RP-HPLC method wer e as follows: planetsil C 18 column (150 mm?4.6 mm, 5 ?m), mobile phase of methanol-water-acetic acid ( 44∶56∶0.1), flow rate at 1.0 mL?min -1, detection wavelength at 240 nm and room temperature. The qualitative fingerprint of Cortex Moutan and the quantitative measurement of paeonol wer e carried out under the chromatographic conditions mentioned above. Res ults Eleven comparatively stable peaks were detected among 13 differ ent samples, from which 10 common peaks used as index peaks for qualitative iden tification were conformed by correlating the peak areas. At the same time, the c ontents of paeonol in samples range from 1.32% to 2.78%. Conclusion The analytical method with qualitative fingerprint of Cortex Moutan and quantitative measurement of paeonol can effectively be used to control the quality of Cortex Moutan.
10.Preparation and Stability of Loperamide Hydrochloride Oral Solution
Qiang FU ; Langchong HE ; Chun CHANG
China Pharmacy 2005;0(20):-
OBJECTIVE:To prepare loperamide hydrochloride oral solution,to establish its quality control method,and to study its stability.METHODS:Loperamide hydrochloride oral solution was prepared by using macrogol-400as the anxiliary solvent,water as the solvent,a reversed phase HPLC method was established to determination the content of principal agent loperamide hydrochloride and the method described in Chinese Pharmacopeia was applied to study its stability.RESULTS:A good linear relationship was obtained in the loperamide hydrochloride at concentration of0.05~0.5mg/ml(r=0.9995);The average recoveries of loperamide hydrochloride at the high,medium and low concentrations were100.6%、101.5%and99.1%respectively,with RSD being1.03%、0.49%and0.56%respectively;The stability showed no evident change as compared with before.CONCLUSION:The loperamide hydrochloride oral solution shows the advantages of simple preparation procedure,satisfactory stability and controllable quality.