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Objective: To detect the influence of peiminine on the invasion and migration of human lung cancer A549 cells. Methods A549 cells were treated with peiminine at the final concentrations of 0, 50, 100, and 200 μmol/L, respectively. The influence of peiminine on the invasion and migration of A549 cells and its underlying mechanisms were investigated by cell invasion experiment, cell scratch experiment, real-time quantitative PCR, ELISA, and Western blotting. Results Compared with 0 μmol/L peiminine group, the cell transmembrane number and scratch wound healing rate and expressions of MMP-9 and MMP-2 in the group treated with different concentrations of peiminine significantly decreased (P < 0.01). Compared with 0 μmol/L peiminine group, the mRNA expression of E-cadherin increased significantly (P < 0.01), while the mRNA expressions of N-cadherin and vimentin decreased significantly (P < 0.01). Compared with 0 μmol/L peiminine group, FN protein expression was significantly decreased in all the groups with different concentrations of peiminine group except treatment with 50 μmol/L peiminine after 24 h (P < 0.05, 0.01). Compared with 0 μmol/L peiminine group, the ratio of p-PI3K/PI3K and p-mTOR/mTOR in all concentrations of peiminine groups and p-Akt/Akt in 100 and 200 peiminine groups were significantly decreased (P < 0.05, 0.01). Conclusion Peiminine can inhibit the invasion and migration of A549 cells, which may be related to the activation of PI3K/Akt/mTOR pathway and decreasing the epithelial- mesenchymal transition process.
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Objective: To develop an HPLC-ELSD method for the determination of amygdalin, aucubin, harpagide, peimisine, peimine and peiminine in Keling capsules simultaneously.Methods: An Ultimate XB C 18 (250 mm× 4.6 mm , 5 μm) chromatographic column was adopted with an ELSD (the drift tube temperature was 105℃, the flow rate of nitrogen was 2.0 L·min-1).The mobile phase was acetonitrile-methanol (1∶1) and 0.4% acetic acid solution with gradient elution at a flow rate of 0.7 ml·min-1 , and the column temperature was set at 35 ℃.Results: Amygdalin, aucubin, harpagide, peimisine, peimine and peiminine was linear within the range of 13.56-271.20 μg·ml-1 (r=0.999 2), 8.48-169.60 μg·ml-1 (r=0.999 9), 4.89-97.80 μg·ml-1 (r=0.999 7), 2.66-53.20 μg·ml-1 (r=0.999 4), 1.82-36.40 μg·ml-1 (r=0.999 8) and 2.04-40.80 μg·ml-1 (r=0.999 6), respectively.The average recovery and the corresponding RSD were 97.90% (1.20%), 99.21% (1.62%), 97.68% (0.75%), 98.36% (1.38%), 99.70% (0.79%) and 97.95% (1.56%)(n =6), respectively.Conclusion: The method is simple and specific, and the results are accurate and repeatable.The method is helpful to the quality control of Keling capsules.
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Objective: To study the influence of sulfur-fumigation on pharmacokinetic of peimine and peiminine of Fritillaria thunbergii in rat plasma by LC-MS/MS. Methods: After random grouping, 18 SD rats were given the solution of fresh-cut and sulfur-fumigated F. thunbergii by ig administration. The blood drug concentration of peimine and peiminine in rat plasma was determined by HPLC-MS/MS, and the pharmacokinetic parameters were calculated with 3P97 software. Results: The pharmacokinetic parameters of peimine and peiminine of sulfur-fumigated F. thunbergii in rat plasma were (66.40 ± 4.65), (146.72 ± 10.88) ng/mL for Cmax, and (181.79 ± 7.85), (457.38 ± 58.81) ng∙h/mL for AUC, respectively. Those of fresh-cut sample in rat plasma were (186.37 ± 18.8), (227.65 ± 7.01) ng/mL for Cmax, and (197.70 ± 18.69), (566.16 ± 41.55) ng∙h/mL for AUC, respectively. The pharmacokinetic parameters of perimine and peiminine of sulfur-fumigated sample in rat plasma were less than those of fresh-cut sample. Conclusion: The results showed that sulfur-fumigation decreased the bioavailability of peimine and peiminine. This study could provide a basis for further clarifying the influence of sulfur-fumigation on efficacy material base of F.thunbergii.
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OBJECTIVE:To study the effect of peiminine on increasing the chemosensitivity of 5 kinds of cancer cells. METH-ODS:Using human esophageal cancer Eca-109 cell,human breast cancer MCF-7 cell,human small cell lung cancer A549 cell,hu-man hepatoma HepG2 cell and human cervical cancer HeLa cell as objects,MTT colorimetric method was used to detect the growth inhibition rate of above-mentioned 5 kinds of cancer cells after treated by peiminine with maximal non-toxic mass concentra-tion(20 μg/mL)and adriamycin with different gradient mass concentrations(0.026-2.1,0.026-2.1,0.125-2.0,0.125-2.0,0.0625-0.10μg/mL)for 72 h. The half inhibitory concentration(IC50)was calculated. Crystal violet staining method was adopted to observe the proliferation of above-mentioned cancer cells after treated by peiminine with maximal non-toxic mass concentration and adriamycin with low mass concentrations(0.02,0.005,0.04,0.02,0.01 μg/mL)for 7 d. Solvent control,single use of peiminine and adriam-ycin control were conducted. RESULTS:Compared with single use of adriamycin,the combination use of peiminine and adriamy-cin can improve the growth inhibition rate of 5 kinds of cancer cells to certain degree,most of the differences were statistically sig-nificant (P<0.05 or P<0.01);and IC50 was obviously decreased,with statistical significances (P<0.05 or P<0.01). Compared with solvent control,single use of peiminine or adriamycin had no obvious effects on the proliferation of above-mentioned cancer cells in 7 d,and the combination use of peiminine and adriamycin can obviously inhibit the proliferation of above-mentioned cancer cells in 7 d. CONCLUSIONS:Peiminine can enhance the sensitivity of above-mentioned-mentioned 5 kinds of cancer cells to cer-tain degree,showing certain chemosensitivity increasing effect.
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As the essential characteristics of malignant cancer,invasion and metastasis are the main reason for failure treatment and high death rate of cancer patients.It is necessary to find out safe and effective anti-invasion and anti-metastasis drugs for the improvement of clinical efficacy.With the definite therapeutic effect and mild side-effects,Chinese materia medica(CMM) including curcumin,peiminine,β-elemi and so on,have become hotspots in anti-invasion and anti-metastasis drugs research.The mechanisms for the effective ingredients of CMM anti-tumor invasion and metastasis were reviewed in this paper.
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As the essential characteristics of malignant cancer,invasion and metastasis are the main reason for failure treatment and high death rate of cancer patients.It is necessary to find out safe and effective anti-invasion and anti-metastasis drugs for the improvement of clinical efficacy.With the definite therapeutic effect and mild side-effects,Chinese materia medica(CMM) including curcumin,peiminine,β-elemi and so on,have become hotspots in anti-invasion and anti-metastasis drugs research.The mechanisms for the effective ingredients of CMM anti-tumor invasion and metastasis were reviewed in this paper.
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Objective: To develop an ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for simultaneous determination of six components (indirubin, peimine, peiminine, ginkalide A, ginkalide B, and ginkalide C) in Baikening Granules. Methods: Preparing the samples solution by Soxhlet's extraction using methanol-chloroform as solvent, and multiple reaction monitoring (MRM) with a polarity-switching electrospray ionization (ESI) source between positive and negative modes was used for the quantification of indirubin, two peimisines, and three bilobalides. The detection was performed on an Inertsutain C18 column (75 mm × 3.0 mm, 2 μm) using a mobile phase consisted of methanol-acetonitrile and 2 mmol/L ammonium acetate water solution with gradient elution lasting 6 min. Results: All of the analytes showed good linearity (r ≥ 0.995 8) in the tested ranges. The precision, repeatability, and stability of the method were good for the six components. The average recoveries were in the range of 96.5%-105.1% with relative standard deviations (RSD) ≤ 4.2%. Conclusion: The new established polarity-switching LC-MS-MS method has been proven to be highly sensitive and effective in evaluating the quality of Baikening Granules, and peimine, peiminine, ginkalide A, ginkalide B, and ginkalide C are quantified in this drug for the first time.
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Objective To develop a new high performance liquid chromatography (HPLC ) coupled with Evaporative Light Scattering Detector (ELSD) method for simultaneous determination of two indicative components (peimine and peimi-nine) in Xiaoer Baotaikang granules .Methods The analysis was performed on a Thermo C18 column (250 mm × 4 .6 mm , 5 μm) by using a mobile phase consisted of acetonitrile-water and diethylamine (65 ∶ 35 ∶ 0 .03) ,and the flow rate was 1 .0 ml/min;ELSD parameters :the temperature of drift tube was 85 ℃ and the carrier gas flow rate was 2 .2 L/min .Results The linear ranges of peimine and peiminine were 0 .586~5 .860 μg (r=0 .999 6) and 0 .564~5 .640 μg (r=0 .999 9) ,respec-tively .The average recovery rate for peimine and peiminine was 99 .44% (RSD was 0 .7% ) and 98 .56% (RSD was 1 .0% ) , respectively .Conclusions The method is sample ,accurate and reproducible ,which could be used for the quality control of Xiao-er Bao taikang g ranules .
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To establish an optimized determination method for the alkaloids peimine and peiminine in three varieties of Fritillaria. Methods:The samples were refluxed in a mixed solution, the pH value of the mixed solution was adjusted, and then the solution was extracted by ether to obtain the test solution. A Shim-pack VP-ODS column (4. 6 mm × 250 mm,5 μm) was used, the mobile phase consisted of acetonitrile-0. 02% diethylamine(75∶25), and the flow rate was 1. 0 ml·min-1. An Alltech 2000ES ELSD detector was used, the drift tube temperature and the flow rate of nitrogen carrier gas in the ELSD was set at 93℃ and 2. 4 L·min-1 , respectively. The regression equation was calculated between the logarithm values of the reference solution concentration and the corre-sponding peak area. Results:The method could effectively extract the alkaloids from the samples. Peimine and peiminine were well separated by the method, and showed good linearity within the respectively given ranges. The average recovery of the alkaloids in the three varieties of Fritillaria was within the range of 95. 22%-103. 51%. Conclusion: The method is simple,convenient and universal with easy operation,which provides references for the determination of alkaloids in the other varieties of Fritillaria.
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Objective: To investigate the effect of peiminine (PMI) on reversing the multi-drug resistance (MDR) of gastric cancer cell and enhancing the antitumor activity of adriamycin (ADR) on SGC7901/VCR cell xenograft and to explore its functional mechanisms. Methods: The model of SGC7901/VCR cell line xenograft on athymic mice was established, and the mice were randomized to groups with ip injection of different drugs once every other day, for six times in all. The tumor volume and the body weight of mice were measured during the drug therapy. The mice were sacrificed after the last administration. The tumors were weighed and then the inhibitory rate was calculated. Western blotting was employed to detect the expression of P-glycoprotein (P-gp) and Cleaved Caspase-3. Results: During the treatment, the tumor volume of mice in PMI + ADR group was decreased significantly compared with the control group (P < 0.01). At the end of the treatment the mice were sacrificed and the tumor weight was measured. The tumor weight and inhibitory rate of mice in PMI + ADR group were obviously decreased compared with the control group (P < 0.05). The expression of P-gp in tumor of mice in ADR + PMI group was decreased. On the contrary, the expression of Cleaved Caspase-3 was increased. Conclusion: The PMI is able to enhance the sensitivity of drug resistance on gastric cancer cell to adriamycin and its mechanism may be related to decreasing the expression of P-gp and increasing the expression of Cleaved Caspase-3 in tumor tissues.
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OBJECTIVE: To develop a UPLC-Q-TOF-MS method for determination of six components (guanosine, peiminine, platycodin D, platycodin D3, oleanolic acid and ursolic acid) in Zhikechuanbeipipa dropping pills. METHODS: The analysis was performed on a Waters Acquity BEH C18 column (2.1 mm×100 mm, 1.7 μm) with the mixture of acetonitrile-water-formic acid as mobile phase, and the flow rate was 0.4 mL·min-1; The PDA detection wavelength was 190-400 nm; The column temperature was room temperature (30°C). RESULTS: The linear relationship between the concentration and peak areas of the six compounds were all linear (r>0.9996). The average recoveries (n=6) were between 99%-101%. CONCLUSION: This method was simple, accurate and reliable to determine the six contents of Zhikechuanbeipipa dropping pills for the quality control. Copyright 2012 by the Chinese Pharmaceutical Association.
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OBJECTIVE:To determine the content of Peiminine in Wenglitong tablets by TLC.METHODS:The content of Peiminine was determined by dual wavelength TLC with gel silica G as thin layer plate.The developing solvent was chloroform-ethyl acetate-methanol-ammonia water(2∶6.5∶1∶0.5)and the developer was modified potassium heptaiodobismuthate.RESULTS:The liner range of Peimine was 0.4～2.4 ?g with an average recovery rate of 99.28%(RSD=1.17%,n=6).CONCLUSION:This method is simple,reliable,reproducible and suitable for the quality control of Wenglitong tabl-ets.
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Object To develop a method for the quantitative analysis of peiminine, imperialine and imperialine 3? D glucoside in Fritillaria L by capillary electrophoresis Methods 9 species of bulbus Fritillaria L. were analysed with internal standard by the mode of capillary zone electrophoresis Results The 3 alkaloids were separated completely with the method which showed good recovery and reproducibility Conclusion The method was proved to be quick, simple, and efficient, and provided a reliable basis for the quality control and evaluation of this plant medicine