Analgesic effect of levo-corydalmine on neuropathic pain in rats and its mechanism / 中国药科大学学报

@#The aim of the present study was to investigate the effects of levo-corydalmine(l-CDL)on chronic constrictive injury(CCI)-induced neuropathic pain and central sensitization in spinal cord. The mechanical withdrawal threshold in rats was assessed by Von-Frey fibers and the thermal withdrawal latency was assessed by thermal stimulus apparatus. The level of phosphorylated N-methyl-D-aspartic acid receptor 1(NR1)in L4-L6 spinal cord was analyzed by immunoblotting and the expression of calcitonin gene related peptide(CGRP)and c-fos in spinal cord dorsal horn were analyzed by immunofluorescence. Results showed that l-CDL(7. 5, 15, 30 mg/kg, ig)inhibited CCI-induced mechanical allodynia and thermal hyperalgesia in a dose-dependent manner. l-CDL significantly inhibited the up-regulation of p-NR1, c-fos and CGRP in CCI rats without tolerance. In conclusion, l-CDL has a good relieving effect on central sensitization in spinal cord, thus generating outstanding analgesic activity on CCI-induced neuropathic pain.

Determination of L-corydalmine in rat plasma by LC-MS/MS and the pharmacokinetic studies / 国际药学研究杂志

Objective To develop a simple, rapid and accurate analysis method for determination of L-corydalmine (L-CDL) in rat plasma. Methods The plasma sample was determined with propranolol as the internal standard (IS), the separation was accomplished in a Capcell PAK C18(2.1 mm×750 mm, 3 μm) column, and the mobile phase consisted of water (including 0.1% formic acid and 5 mmol/L ammonium formate) and acetonitrile (including 0.1% formic acid) at a flow rate of 0.25 ml/min. The mass spectrometer consisted of an ESI interface operating at positive ionization mode and the detection was performed using multiple reaction monitoring(MRM) at the transitions of m/z 342→192.1 for L-CDL and m/z 260→116.2 for propranolol. Method validation included the evaluation of the linearity range, lower LOQ, within-run and between-run precision, accuracy and stability, matrix effect and extraction recovery. Results The calibration curve was linear across the concentration range of 1-5000 ng/ml for L-CDL with a lower LOQ of 1 ng/ml. The within-run and between-run precision (RSD%) was in the range 0.1%-10%. The extraction recovery was in 93.5%-102.8% and the matrix effect for three QC was 108.3%-112.5%. L-CDL reached the peak concentration at 0.5 h after dosing. The main pharmacokinetic parameters of rats after igl administration were as follows: T1/2: (7.04±3.93)h, Cmax: (557.8±330.1)ng/ml, AUC0~24: (2408±630)h•ng/ml. Conclusion A simple, rapid, accurate, high sensitivity and repeatability method has been successfully developed, which can analyze the concentration of L-CDL in rat plasma. The method can be used for the investigation of pharmacokinetics of L-CDL in rats.

Determination of L-corydalmine in rat plasma by LC-MS/MS and the pharmacokinetic studies / 国际药学研究杂志

Objective To develop a simple,rapid and accurate analysis method for determination of L-corydalmine(L-CDL) in rat plasma. Methods The plasma sample was determined with propranolol as the internal standard(IS),the separation was ac?complished in a Capcell PAK C18(2.1 mm×750 mm,3μm)column,and the mobile phase consisted of water( including 0.1%formic acid and 5 mmol/L ammonium formate)and acetonitrile(including 0.1%formic acid)at a flow rate of 0.25 ml/min. The mass spec?trometer consisted of an ESI interface operating at positive ionization mode and the detection was performed using multiple reaction monitoring(MRM)at the transitions of m/z 342?192.1 for L-CDL and m/z 260?116.2 for propranolol. Method validation included the evaluation of the linearity range,lower LOQ,within-run and between-run precision,accuracy and stability,matrix effect and extrac?tion recovery. Results The calibration curve was linear across the concentration range of 1-5000 ng/ml for L-CDL with a lower LOQ of 1 ng/ml. The within-run and between-run precision(RSD%)was in the range 0.1%-10%. The extraction recovery was in 93.5%-102.8%and the matrix effect for three QC was 108.3%-112.5%. L-CDL reached the peak concentration at 0.5 h after dosing. The main pharmacokinetic parameters of rats after igl administration were as follows:T1/2:(7.04 ± 3.93)h,Cmax:(557.8 ± 330.1)ng/ml,AUC0~24:(2408±630)h·ng/ml. Conclusion A simple,rapid,accurate,high sensitivity and repeatability method has been successfully devel?oped,which can analyze the concentration of L-CDL in rat plasma. The method can be used for the investigation of pharmacokinetics of L-CDL in rats.

Effect of 1-corydalmine,an Alkaloid Isolated from Corydalis chaerophylla Roots on Spore Germination of Some Fungi

1-Corydalmine,an alkaloid isolated from roots of Corydalis chaerophylla inhibited spore germination of some plant pathogenic as well as saprophytic fungi e.g. Alternaria brassicae, A. brassicicola, A. solani, Curvularia lunata, C. maculans, C. sp., C. pallscens, Erysiphe pisi, Fusarium udum, Helminthosporium species,H. penniseti and a Heterosporium species. 1-Corydalmine significantly inhibited spore germination of all the fungi at 100 to 1500 ppm. It was effective against all the fungi at 1500 ppm. C. lunata was highly sensitive to this chemical even at 250 ppm.

Inhibitory Effect of Two Alkaloids, (-)-Corydalmine and (-)-Isocorypalmine Isolated from Corydalis chaerophylla on Several Phytopathogenic Fungi

Medicinal plants play important roles in controlling plant diseases as one of the safest and ecofriendly methods. These plants have been used in the form of crude extracts as well as active principles in vitro and under field conditions to control plant diseases. Among the active principles, alkaloids have shown significant antifungal activity. We have investigated the effect of two alkaloids viz., (-)-corydahnine and (-)-isocorypahnine isolated from Corydalis chaerophylla, against spore germination of some plant pathogenic and saprophytic fungal spores. Significant inhibition of spore germination at 100 microg/ml was seen against Curvularia penniseti, Curvularia sp. and Colletotrichum gloeosporioides by (-)-corydahnine but (-)-isocorypalmine was also effective against fungi included in the experiment.