Journal of Chinese Pharmaceutical Sciences

Contents list

2003, 12(3): 1-01.

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The Alkaloids from Leaves of Croton hemiargyerius var. gymnodiscus

LIN Wen-han^*, FU Hong-zheng, LI Jun, CHENG Gang, Roderick A.Barnes

2003, 12(3): 117-122.

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Aim Investigation of alkaloids from the leaves of Brazilian medicinal plant Croton hemiargyerius var. gymnodiscus. Methods Silica gel column chromatography was used repeatedly for the isolation and purification, and their structures were identified by extensive spectroscopy and comparison of the chemical and physical data with those of authentic samples reported in literature. Results Twelve alkaloids were isolated and their structures were identified. Conclusion Four new alkaloids named hemiargines A (1), B (5), C (6) and D (7), together with eight known alkaloids namely isocorydine (2), corydine (3), norcorydine (4), salutaridine (8), glaucine (9), tetrahydropalmatrubine (10), xylopinoine (11), and norlaudanosine (12) were isolated.

Synthesis of Boc-Asp(OBzl)-β-Ala-Asp(OBzl)-N(OMe)Me as a Useful Precursor of Aspartyl Peptide Aldehyde Derivatives

ZOU Xiao-min, ZHAO Hong, FU Yi-qiu, ZHANG Xin, XU Ping^*

2003, 12(3): 123-126.

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Aim To synthesize the tripepide Weinreb amide Boc-Asp(OBzl)-β-Ala- Asp(OBzl)-N(OMe)Me (7) as a useful precursor of aspartyl peptide aldehyde derivatives; Methods DCC, IBCF method was used for preparation of Weinreb amide; N-hydroxysuccinimide activated ester was used in peptide synthesis; and Boc as N-protecting group of amino acid. Results Boc-Asp(OBzl)-N(OMe)Me (3), Boc-β-Ala-Asp(OBzl)-N(OMe)Me (5), and Boc-Asp(OBzl)-β-Ala-Asp (OBzl)-N(OMe)Me (7) were synthesized successfully. Conelusion An useful precursor of tripeptide aspartyl aldehydes was synthesized.

Pharmacokinetics of Scutellarin in Dogs

LI Su-hua, JIANG Xue-hua^*, LAN Ke, YANG Jun-yi, ZHOU Jing

2003, 12(3): 127-130.

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Aim To establish an RP-HPLC method for the determination of scutellarin in plasma and study its pharmacokinetics in dogs. Methods Scutellarin was given to dogs by intravenous injection and determined by RP-HPLC, the mean plasma concentration-time curve was plotted and pharmacokinetic parameters were calculated by program 3p87. Results The concentration-time curve of scutellarin could be fitted to three-compartment model with T1/2pi, T1/2α and T1/2β being 1.05±0.80 min, 6.99±2.76 min and 51.61±28.78 min, respectively, Vc being 880.1±508.3 mL, CL being 189.6±53.8 mL·min^-1, and AUC0-90 and AUC0-∞ being 574.43±133.95 μg·min·mL^-1 and 599.34±132.00μg·min·mL^-1, respectively. Conclusion The fact that the concentrations of scutellarin in plasma declined rapidly after the medication suggested that the T1/2 of scutellarin should be taken into account in drug administration and preparation development.

The Stability of Endomorphin-1 Solution

LIU Hui, YANG Ding-jian, NI Jing-man^*, WANG Rui

2003, 12(3): 131-134.

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Aim To study the most stable pH value of endomorphin-1 solution and to estimate the shelf-life of EM-1 solution. Methods The content of EM-1 in its solution was determined by HPLC, and stability was studied by accelerated tests. Results The most stable pH value of EM-1 solution was observed. By the accelerated tests we obtained the Arrhenius relationship and the pharmacokinetic parameters. Conclusion The most stable pH value of EM-1 solution is 4.5-4.8. The t1/2 (25 °C) is 45 d.

Effect of Milrinone Induced Insulin Resistance on Glucose and Lipid Metabolism in Rats

LI Ling^*, YANG Gang-yi

2003, 12(3): 135-141.

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Aim To investigate the effects of milrinone (a selective phosphodiesterase Ⅲ inhibitor PDE3) on insulin secretion, blood glucose, plasma free fatty acids (FFA) and dose-response relationship, and assess possible effects of milrinone on glucose metabolism and insulin sensitivity in conscious rats. Methods The catheterized nonstressed rats were administered various doses of milrinone (1, 5, 25 μmoL·kg^-1) and were compared with controls. A hyperinsulinaemic-euglycaemic clamp was established in counscious rats, and milrinone(25 μmoL·kg^-1) and 25 % dimethyl sulfoxide (DMSO, as a control) were given at 120 min during hyperinsulinaemic-euglycaemic clamping. Glucose turnover was determind with by gas chromatograph mass spectrometer (GC-MS). Results After dosing, plasma FFA levels in 3 milrinone groups significantly increased, compared with the controls and before dosing. The percentages of elevation of FFA by the different milrinone doses were very similar, 50%, and 52%, 55% for 1, 5, and 25 μmoL·kg^-1, repectively, at 2 min after dosing. Plasma insulin levels were significantly elevated in the 5 and 25 μmoL·kg^-1 groups, and the effect of milrione on glucose concentration was detectable only in 25 μ moL·kg^-1 group. During hyperinsulinaemic clamping, there were significant increase, in plasma FFA (from 173±15 to 634±87 μmoL·L^-1) and hepatic glucose production (HGP), and a significant decrease in glucose infusion rates (GIR) to about 21% and a slight increase in plasma insulin after milrinone treatment. Conclusion Milrinone impaires the ability of insulin to suppress lipolysis and HGP, and insulin-mediated glucose utilization in peripheral tissue. Therefore, milrinone administration may induce an acute insulin resistance in vivo.

Mechanisms of Cyclovirobuxine D on APD Prolongation in Rat Ventricular Myocytes

CHEN Qing-wen, SHAN Hong-li, WANG He, LI Zhe, YANG Bao-feng^*

2003, 12(3): 142-147.

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Aim To study the effects of cyclovirobuxine D on inward rectifier K⁺ current (IK1), transient outward K⁺ current (Ito), L-type Ca²⁺ current (ICa-L), and action potential duration (APD) in isolated rat ventricular myocytes.Methods The whole cell patch-clamp techniques were used to study the changes of IK1, Ito, ICa-L and APD in rat ventricular myocytes. Results Cyclovirobuxine D (1-10 μmol·L^-1) significantly prolonged APD50 and APD90 in isolated rat ventricular myocytes. Resting potential (RP) was decreased by 10 μmol·L^-1 of cyclovirobuxine D. Cyclovirobuxine D significantly decreased both inward and outward components of IK1. At - 100 mV, 1 and 10 μmol·L^-1 of cyclovirobuxine D decreased IK1 density from (-8.0±1.1) pA/pF to (-4.1±0.7) pA/pF and (-3.4±0.8) pA/pF, respectively,whereas at - 30 mV, IK1 density was decreased from (1.10±0.24) pA/pF to (0.61±0.18) pA/pF and (0.36±0.11)pA/pF, respectively. IIto was markedly inhibited by cyclovirobuxine D from the test potential of 0 mV to + 60 mV. At + 40 mV, 1 and 10 μmol·L^-1 of cyclovirobuxine D decreased Ito density from (8.9±2.0) pA/pF to (5.5±1.2) pA/pF and (4.9 + 0.9) pA/pF, respectively. Cyclovirobuxine D inhibited ICa-L in a concentration-dependent manner. At 10 mV, 1 and 10 μmol·L^-1 of cyclovirobuxine D decreased ICa-L density from (-9.9±1.8) pA/pF to (-6.4±1.4) pA/pF and (-4.2±0.6) pA/pF, respectively. Conclusion Cyclovirobuxine D significantly prolonged APD and inhibited IK1, Ito and ICa-L in rat ventricular myocytes. The inhibitory effects of cyclovirobuxine D on IK1 and Ito are major molecular mechanisms of APD prolongation in rat.

Neuroprotective Effects of Modafinil on MPTP Mouse Model of Parkinson's Disease

XIAO Yan-li^*, DONG Zhi, FU Jie-min, ZHOU Qi-xin, LIAO Hong

2003, 12(3): 148-153.

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Aim To observe the neuroprotective effects of modafinil on the Parkinson's disease ( PD ) model induced by 1-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine (MPTP). Methods The model of PD was induced by intraperitoneal injection of MPTP into C57BL/6J mice for4 d. Modafinil (ip, 50 or 100 mg·kg^-1·d^-1) was administered following MPTP for 4 d and for another 10 d consecatirely. The effects of modafinil on the locomotor activity, and the incubation, maintenance period and grade of the tremor, the duration of the climbing rod of mouse, and the distribution of positive cells of tyrosine hydroxylase (TH) and Nissl bodies in the striatum and substantia nigra (SN) were observed. The contents of dopamine (DA) , noradrenaline (NA) and 5-hydroxytryptamine (5-HT) in the striatum were determined. Results Modafinil (50 and 100 mg·kg^-1) significantly prevented the locomotor, the tremor and climbing rod defect behavior in a dose-dependent nanner (P<0.05 and P<0.01, n = 10), prevented the decrease in the number of TH-positive cells and Nissl bodies (P<0.05, n = 10), and reduced the decrease of DA, NA, and 5-HT in the striatum (P<0.05, n = 10) induced by MPTP. Conclusion Modafinil improves the behavioral deficits and prevents the monoaminergic neuron lesion in seriously impaired MPTP mouse model.

Modulatory Effect of Pollen Extract on Apoptosis of Lymphocytes in the Elderly

LI Yu-mei , ZHANG Chun-ling, FAN Yun, LIU Jun-da^*

2003, 12(3): 154-159.

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Aim In this study, we investigated the changes of lymphocyte subpopulation and apoptosis process of lymphocytes in the elderly, and the modulatory effect of pollen extract (PE) on apoptosis. Methods Lymphocyte phenotypes were detected using indirect immunofluorescence technique. The proliferation responses were determined by MTT method. Flow cytometry and automatic image analysis were performed to evaluate the apoptosis of lymphocytes. Results The proliferation responses of lymphocytes in the elderly were lower than that in young adults. Decreased CD45 RA+ cells and increased CD45 RA+ cells were found in lymphocyte population of aged people, compared with that of young adults. The CD45 RA+ cells were prone to apoptosis. There is an inhibitory effect of PE on apoptosis of lymphocytes in the elderly. Conclusion It is implied that the susceptibility of lymphocyte in the elderly to apoptosis depends on activation, so called, activation-induced cell death. Present results suggest that apoptosis of lymphocytes in aged people play an important role in the pathogenesis of immunosenescence. Thus, a possibility is open for development of apoptosis-modulating drugs from pollen.

Survey on Natural Radiosensitizing Agents Since 2000

LU Jia, SHAO Hong^*

2003, 12(3): 160-163.

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Survey of Radiosensitizing Agents (Synthesized Chemicals and Gene Therapeutic Agents) Since 2000

SHAO Hong^*, LU Jia

2003, 12(3): 164-169.

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Alginate-Chitosan Microcapsules for Renal Arterial Embolization

LI Sha, HOU Xin-pu^*

2003, 12(3): 170-171.

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