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Table of Content
15 March 2004, Volume 13 Issue 1
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Contents
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Journal of Chinese Pharmaceutical Sciences
2004, 13(1): 1-01.
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Chemical Constituents of Angelica sinensis
LU Xin-hua, ZHANG Jin-juan, LIANG Hong
*
, ZHAO Yu-ying
2004, 13(1): 1-3.
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Aim
To investigate the active constituents re sp onsible for the pharmacological activities of Angelica sinensis (Oliv) Diels.
Methods
Chromatography was used to isolate chemical c omp onents, and spectroscopy was used to identify their structures.
Results
Seven compounds were isolated and their structures were identifi ed as ferulic acid (1), coniferylferulate (2), bis-(2-ethylhexyl)-phthalate (3), dibutyl phthalate (4), lignoceric acid (5), palmitic acid (6), and Z-6, 7-cis-dihydroxyligustilide (7).
Conclusion
Bis (2-ethylh exyl) phthalate and dibutyl phthalate were obtained from Angelica sinensis for the first time.
Synthesis of Isonucleoside-Incorporated Oligonucleotides and Their Binding Abilities with Complementary Sequences
SHI Ji-feng, WANG Zhan-li, ZHANG Liang-ren
*
, ZHANG Li-he
2004, 13(1): 4-9.
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Aim
To synthesize isonucleoside-incorporated ol igonucleotides and investigate their binding abilities with complementary sequen ces.
Methods
The synthesis was performed on DNA synthesizer, and the binding behavior was investigated by thermal denaturation studies.
Results
Four kinds of single isonucleoside containing oligonucleoti des were synthesized. The results of thermal denaturation showed that the existe nce of isonucleoside decreased the stability of duplex, and the effect was more obvious when the isonucleoside was in the middle of the sequence. No obvious dif ference was observed when 6'-OH of isonucleoside was free or was protected by allyl group.
Conclusions
The existence of isonucleoside in oli gonucleotide makes chain twist and decreased the stability of duplex.
Synthesis of Resveratrol and Resveratrol Trinicotinate
ZHANG Xue-jing, ZHU Jie, XIONG Xiao-yun, ZOU Yong
*
, LIN Hu i-zhen
2004, 13(1): 10-13.
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Aim
To synthesize a new prodrug, resveratrol trinicotinate.
Methods
In presence of lithium and a catalytic amount of naphthalene, the reaction of p-methoxybenzyl trimethylsilyl ether and 3,5-dimethoxylbenzaldehyde gave resveratrol after a series of translation.Resveratrol trinicotinate was obtained by the reaction of resveratrol and nicotinoyl chloride hydrochloride.
Results
A mutual prodrug resveratrol trinicotinate was designed and synthesized.
Conclusion
A novel method for synthesis of resveratrol and resveratrol trinicotinate has been afforded.The E-isomer is selectivily obtained by dehydration of the compound 2 with KHSO
4
.
Synthesis of Phenylpropanoid Glycoside Analogs
LI Shu-chun, ZHOU Jing, LI Zhong-jun
*
2004, 13(1): 14-18.
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The regioselective acylation of unprotected phenylethyl glucoside with cinnamoyl chloride leads to 6-OH cinnamoylated glucoside.In this manner, thirteen phenylpropanoid glycoside analogs were designed and prepared.Their structure was confirmed by
1
H NMR and
13
C NMR spectra.
Structure Determination of By-product in Grignard Reaction for Preparing Mifepristone Derivatives
CHEN An-ping, LEI Xiao-ping
*
2004, 13(1): 19-23.
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Aim
To determine the structure of the by-product produced in Grignard reaction for preparing mifepristone derivatives, and elucidate the reaction mechanism.
Methods
The structure of the by-product was determined with elemental analysis, one- and two-dimension spectra NMR (DEPT, 1H-1Hcosy, HMQC, HMBC) and compared with those of mifepristone.
Results
The main by-product was 11,17-di-addition product of Grignard reagent of N, N-dimethylamino phenyl bromide.
Conclusion
This is the first complete assignment of
1
H NMR and
13
C NMR of compound (3).
Fragmentation Patterns of Diquaternary Dipiperaziniums Containing Dithiocarboxy lGroups by Electrospray Ionization Tandem Mass Spectrometry
WANG Xin, GE Ze-mei, CHENG Tie-ming, LI Run-tao
*
2004, 13(1): 24-27.
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Aim
To analyze the fragmentation patterns of diquaternary dipiperaziniums containing dithiocarboxyl groups.
Methods
Positive ion electrospray ionization mass spectrometry in conjunction with tandem mass spectrometry (ESI-MSn) was used.
Results
The fragment ion [M
2+
Cl
-
]
+
showed characteristic double peaks with high intensity instead of the parent molecular ion being detected.And [M
2+
-CH
3
+
]
+
ion had relatively low intensity. Meanwhile, [M
2+
Cl
-
-Cl
-
-PhCH
2
+
]
+
species had the highest intensity as the base peak, which was originated from [M
2+
Cl
-
]
+
. The detailed fragmentation mechanisms are supported with the tandem mass spectrometry.
Hypoglycemic Effect of Intravenous Polyethylene Glycol-Coated Liposomal Insulin on Normal Rats
ZHANG Xuan, ZHANG Hua, WANG Gui-ling, ZHANG Da-wei, WANG Jing, LIN Wei, ZHANG Qiang
*
2004, 13(1): 28-31.
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Aim
To evaluate liposome as an injectable delivery system of proteins, insulin was chosen as model drug and the hypoglycemic effect of PEG-coated liposomal insulin was tested.
Methods
The PEG-coated liposomal insulin was prepared by reversal-phase emulsion evaporation.For pharmacodynamic study, insulin (2.5 IU·kg
-1
) was intravenously administered in phosphated-buffered saline (PBS) solution, conventional liposomes, and PEG-coated liposomes, separately, to normal Wistar rats.Blood glucose levels were determined by the glucose oxidase method.
Results
The mean diameter of the PEG-coated liposomal insulin was 58.4 nm, while the encapsulation ratio reached 18.33%.After intravenous administration of insulin solution, insulin liposome, and PEG-coated liposomal insulin, the minimum blood glucose concentrations (C
min
%) reached 25.26±5.75%, 33.92±12.42%, and 42.39±10.5% of the initial level, respectively, and the time periods to reach the minimum blood glucose level (T
min
) were 0.7±0.3 h, 1.2±0.4 h, and 2.3±0.7 h, respectively.The relative pharmacological bioavailabilities of insulin liposome and PEG-coated liposomal insulin were 98.03% and 99.70%, respectively, compared with the control of insulin solution.
Conclusion
PEG-coated liposome can be developed as a relatively sustained injectable delivery system for insulin. Moreover, the liposome coated with PEG may have advantages over normal liposome.
Influence of pH Environment on Nasal Absorption of Meptazinol Hydrochloride
SHI Zhen-qi, JIANG Xin-guo
*
2004, 13(1): 32-36.
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Aim
To investigate the relationship between pH environment of meptazinol hydrochloride (MEP) and its nasal absorption.
Methods
In situ nasal perfusion was performed to study the effect of pH environment on the nasal absorption. Its effect on the transport from nose to brain was further researched by in vivo experiment.
Results
In in situ perfusion experiment, the nasal absorption of MEP in basic environment was significantly higher than that in acid condition, but the difference was not observed in
in vivo
experiment.
Conclusion
The pH environment of meptazinol hydrocloride in formulation cannot be regarded as an important factor influencing nasal absorption and transport from nose to brain.
Pharmacokinetics and Bioavailability of 2-Amino-6-Cyclopropylamino-9-(2,3-Dideoxy-β-D-glyceropent-2-enofuranosyl) Purine (Cyclo-D4G) in Rats
LIU Yi, YANG Zhen-jun
*
, BOUDINOT F.Douglas, CHU Chung Kuang, ZHANG Li-he
2004, 13(1): 37-41.
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Aim
To characterize the pharmacokinetics of 2-amino-6-cyclopropylamino-9-(2,3-dideoxy-β-D-glyceropent-2-enofuranosyl) purine (Cyclo-D4G) following intravenous administration and oral administration to rats.
Methods
The concentrations of Cyclo-D4G in rat (Sprague-Dawley male rats) plasma and urine were analyzed by high performance liquid chromatography (HPLC).
Results
Following intravenous administration to rats, concentrations of Cyclo-D4G in plasma declined with a terminal phase half-life of 0.78±0.14 h (x±s).Total clearance was 0.90±0.21 L·h
-1
·kg
-1
. Renal excretion of unchanged Cyclo-D4G accounted for approximately 20% of total clearance.Steady state volume of distribution was 0.91±0.07 L·kg
-1
. After oral administration to rats, concentrations of Cyclo-D4G in plasma declined with a terminal phase half-life of 0.83±0.13 h (x±s).Total clearance was 3.81±2.03 L·h
-1
·kg
-1
. Renal excretion of unchanged Cyclo-D4G accounted for approximately 9% of total clearance.Oral bioavailability of Cyclo-D4G in rat was 26.9%.
Conclusion
The favorable pharmacokinetic profiles and lower toxicity provide support for further development of Cyclo-D4G clinical trials.
Effects of PVP K30 on Aqueous Solubility and Dissolution Properties of Daidzein
GUO Sheng-rong
*
, GUO Li
2004, 13(1): 42-48.
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Aim
To study effects of PVP K30 on the aqueous solubility and dissolution properties of daidzein.
Methods
To measure the aqueous solubility and dissolution rates of daidzein in three different states (within solid dispersions, physical mixtures and as a pure drug) and investigate drug-polymer interactions in the solid state using X-ray powder diffraction and fourier-transform infrared spectroscopy.
Results
The negative values of the Gibbs free energy and enthalpy of transfer explained the spontaneous transfer of daidzein from phosphate buffer solution (PBS) to a solution of PVP in PBS.X-ray powder diffraction patterns showed that the drug was in the amorphous state (ratio of the drug:PVP<1:5) when dispersed in PVP K30.The infrared spectra indicated there exist interactions between the OH of daidzein and the C=O of PVP K30.
Conclusion
the dispersion of daidzein in PVP K30 considerably enhances the solubility and dissolution rate.
1
H and
13
C NMR Assignments for Amlodipine and Risperidone
YANG Chun-hui, LI Qin, LIU Xue-hui, ZHAO Xing-kai, CUI Yu-xin
*
2004, 13(1): 49-52.
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Aim
To investigate the NMR spectroscopy of amlodipine and risperidone.
Methods
1D NMR and 2D NMR experimental techniques of gCOSY, gHSQC and gHMBC were wsed.
Results
The assignments of the
1
H and
13
C NMR data for the two drugs were performed and confirmed by the evidence of JHF and JCF.
Conclusion
The structures of amlodipine and risperidone were confirmed by careful analysis of regular 1D and 2D NMR spectroscopy.
Preparation of High-Purity Linolenic Acid from Oil of Lithospermum Erythrorhizon by Urea Inclusion and Column Chromatography
HAN Xi-jiang
*
, XU Ping, MENG Xiang-li, LIANG Zhi-hua, ZHANG Zong-shuang, YANG Zhan-cheng
2004, 13(1): 53-57.
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Aim
To separate high purity linolenic acid from the oil of Lithospermum erythrorhizon growing in the Northeast of China.
Methods
Urea inclusion and column chromatography were used.
Results
Unsaturated fatty acid was separated, with a purity of 99.30 wt% of linolenic acid.
Conclusion
The experiment shows excellent reproducibility and high feasibility for industrial production.
Simultaneous Determination of Tetramethylpyrazine and Aspirin in a New Compound Formulation by Liquid Chromatography
WANG Peng, QI Mei-ling
*
, ZHOU Li, FANG Lin
2004, 13(1): 58-62.
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Aim
To establish a reversed-phase liquid chromatographic (LC) method for simultaneous determination of tetramethylpyrazine (TMP) and aspirin in a new compound formulation.
Methods
Chromatographic separation of the two drugs was achieved on a Diamonsil C
18
column, using a binary mixture of methanol-1.5% acetic acid (35:65, V/V, pH = 3.1) as mobile phase at a flow rate of 1.0 mL·min
-1
.
Results
Separation was completed in less than 12 min.Benzoic acid was used as the internal standard.Recoveries at levels corresponding to 80 % to 120 % of the label claim of the formulation ranged from 99.6 to 100.3 % for aspirin and from 99.9 to 101.3% for TMP.The linear range was 12.6-150.9 μg·mL
-1
(r = 0.9997, n = 5) for aspirin and 25.0-300.0 μg·mL
-1
(r = 0.9999, n = 5) for TMP.
Conclusion
The method developed can be used for the simultaneous determination of TMP and aspirin in pharmaceutical preparations.
Inhibitory Effect of Isorhapontigenin on Copper-Mediated Peroxidation of Human Low-Density Lipoprotein in vitro
FANG Ya-nan, LIN Mao, LIU Geng-tao
*
2004, 13(1): 63-67.
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Aim
To study the effect of Isorhapontigenin (Iso) on copper-mediated peroxidation of human low-density lipoprotein (LDL) and on the toxicity of oxidized LDL (ox-LDL) to mouse macrophages in vitro.
Methods
Human LDL from sera of normal lipidemic donors was separated by sequential ultracentrifugation.The separated human LDL 1 mg·mL
-1
in phosphate buffer saline, pH 7.4, was incubated with cupric sulfate (10 μmol·L
-1
) at 37
°
C for 10 h in the presence or absence of various concentrations of Iso.Malondialdehyde (MDA) formation, vitamin E consumption, electrophoretic mobility of LDL, mitochondrial membrane potential of mouse peritoneal macrophages, phagocytosis of neutral red, and release of nitric oxide (NO) from macrophages were determined by various methods.
Results
Iso 1-100 μmol·L
-1
significantly inhibited the increase of MDA formation, vitamin E consumption and electrophoretic mobility of LDL induced by Cu
2+
in a concentration-dependent manner.The injury of the mitochondrial membrane potential of mouse peritoneal macrophages due to incubation with ox-LDL (0.1 mg·mL
-1
) at 37
°
C for 12 h was markedly protected by 10 μmol·L
-1
Iso. After pretreatment of the macrophages with 10 μmol·L
-1
of Iso and then exposure to ox-LDL for 4 h, the reduction of phagocytosis of neutral red and release of NO in response to lipopolysaccharide (LPS) stimulation were significantly prevented.
Conclusion
Iso has protective action against Cu
2+
mediated LDL peroxidation and ox-LDL induced toxicity to macrophages in vitro.
Primary Mechanisms for Novel Compound Pivanampeta Against Atherosclerosis in Rat and Rabbit Model of Atherosclerosis
SHAN Li-mei, ZHANG Jin-chao, ZHAO Yan-ling, WANG Hai
*
2004, 13(1): 68-75.
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Aim
To investigate the anti-atherosclerotic mechanisms of the novel compound pivanampeta in the early and later stages of atherosclerosis evolution.
Methods
Rats or rabbits were randomly assigned to the control, the model and the pivanampeta-treated groups. The rats or rabbits in the model group and the pivanampeta-treated group were fed with hypercholesterol diet. The carotids of rabbits were cut into pieces and stained with HE.The rat or rabbit serum levels of TC, LDL-CHO, HDL-CHO, IL-8, ET-1, PGI2, TXA2, and NO were assayed. The expressions of MCP-1 and IL-8 mRNA on rabbit carotid were determined by semi-quantitative RT-PCR.
Results
Pivanampeta exerted an inhibitory effect on TXA2 formation without PGI2 production in the early and later stages of atherosclerosis. The significantly increased release of NO and the decreased release of IL-8 in the animals in pivanampeta-treated group were both detected in the rat atherosclerosis model. In the rabbit atherosclerosis model the expressions of IL-8 and MCP-1 mRNA in pivanampeta-treated group were decreased significantly.However, the treatment with pivanampeta had no effect on the levels of plasma cholesterol, MDA and SOD.
Conclusion
The increase of serum NO contents and the decrease of plasma TXA2 level, as well as its inhibition of expression of IL-8 and MCP-1 are probably involved in the mechanisms underlying the anti-atherosclerotic effects of pivanampeta.
The Potential Pathway of L-arginine·L-aspartate for Inhibition of Platelet Function
WANG Yin-ye, WANG Chao, HAN Mei, PENG Shi-qi, ZHAO Ming
*
2004, 13(1): 76-79.
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Aim
L-Arginine·L-aspartate, a double salt, has been recently reported to inhibit platelet aggregation and thrombosis, but its action mechanism is not clear yet. This study was conducted to investigate its effect on FITC-PAC-1, an anti-glycoprotein Iib/IIIa monoclonal antibody binding to activated platelets, and on correlative autacoid levels in plasma or in platelets in order to explore its potential pathway of inhibiting platelet aggregation and thrombosis.
Methods
Monoclonal antibody binding to activated platelets was assayed by flow cytometry; NO was assessed by colorimetric method.cAMP, TXB2 or 6-keto-PGF1α levels were assessed by radioimmunoassay.
Results
Gavaged 30 mg·kg-1 of L-arginine·L-aspartate increased both concentration of NO in plasma and 6-keto-PGF1α in incubated supernatant of aortic segment of rats ex vivo (P<
0.05), but it did not influence cAMP content in platelets and the level of TXB2 or 6-keto-PGF1α in plasma of rats, whereas ASA significantly lowered TXB2 or 6-keto-PGF1α in plasma.Both 100 μmol·L
-1
of L-arginine·L-aspartate and ASA inhibited FITC-PAC-1 binding to activated platelets in vitro.
Conclusion
The increase in NO and PGI2 release from endothelial cells and consequent inhibition of platelet activation may contribute to the inhibition of platelet aggregation and thrombosis by L-arginine·L-aspartate; whereas arachidonic acid or cAMP metabolic pathway is not closely correlative with the studied effect.
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