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Sophoridine is a quinolizidine alkaloid extracted from Sophora in legumes, which is one of the main active ingredients of Sophora alopecuroides L, Sophora flavescentis Ait and Sophora davidii (Franch.) skeels. Its molecular formula is C
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Objective: To establish the chemical fingerprint of Sophora alopecuroides extracts based on high performance liquid chromatography (HPLC), and determine the LD50 of different extracts of S. alopecuroides to analyze its “spectrum toxicity” relationship. Methods: A series of extracts were prepared by 75% ethanol reflux (ER), water decoction (WD), 75% ethanol ultrasound (EU) and water ultrasound (WU), and their fingerprints were established to determine the acute toxicity LD50 of different extracts. The relationship between chemical composition and acute toxicity LD50 of S. alopecuroides extracts were studied by means of fingerprint similarity evaluation system. Results: The LD50 of ER, WD, EU, and WU extracts were 38.397, 24.994, 18.536, and 19.957 g/kg, respectively. The ocular lesions of mice viscera were mainly manifested in liver and kidney, and the toxicity of ER extracts was the greatest. The 10 common peaks of S. alopecuroides extracts can be divided into two categories; Peaks 4 and 10, oxymatrine and sophocarpidine were negatively correlated with acute toxicity LD50. Conclusion: The spectral toxicity relationship analysis method of S. alopecuroides was constructed. The unidentified peaks 4, 10 and oxymatrine and sophocarpidine were the main chemical components of the toxicity reaction, which laid a good foundation for clinical application and scientific and rational development of S. alopecuroides.
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AIM To establish a gas chromatography-flame ionization detector (GC-FID) method for the simultaneous content determination of four constituents in Kaihoujian Spray (a spray for management of oral and laryngopharyngeal inflammatory condition,containing Sophorae tonkinensis Radix et Rhizoma,Cicadae Periostracum,menthol,etc.).METHODS The analysis of mixure of Kaihoujian Spray and internal standard (dibutyl phthalate) solution was conducted on an HP-INNOWax column (30 m ×0.25 mm ×0.25 μm),both of the injector temperature and detector temperature were set at 260 ℃,the split ratio was 5 ∶ 1,and the flowing rate was 1.5 mL/min.RESULTS Menthol,matrine,sophocarpine and sophoridine showed good linear relationships within the ranges of 0.228 7-2.287 0 mg/mL (r =0.999 7),0.011 1-0.111 0 mg/mL (r =0.999 6),0.016 8-0.168 0 mg/mL (r =0.999 8) and 0.003 4-0.034 0 mg/mL (r =0.999 4),whose average recoveries (n =9) were 98.4％ (RSD=1.2％),95.9％ (RSD=1.8％),96.2％ (RSD=2.1％) and 97.1％ (RSD=1.7％),respectively.CONCLUSION This accurate,sensitive and simple method can be used for the quality control of Kaihoujian Spray.
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OBJECTIVE: To investigate the molecular mechanisms of proliferation inhibition and apoptosis induction by sophoridine on cell lines from adenocarcinoma in esophagogastric junction. METHODS: After treatment of OE-19 and SK-GT2 cells with 0-3.0 mg·mL-1 of sophoridine for 24, 48 and 72 h, CCK8 was used to examine the proliferation, flow cytometry was used to examine apoptosis, biochemical assay for intracellular ROS and GSH, real-time PCR and Western blot were used to examine FoxM1 mRNA and protein expression, and dual-luciferase reporter gene assay was used for measurement of the transcriptional activity of FoxM1. RESULTS: Sophoridine could significantly inhibit the proliferation of OE-19 and SK-GT2 cell lines, induces apoptosis and G0/G1 arrest of OE-19 cell lines at the concentration of 0.5-1.0 mg·mL-1. Intracellular ROS increase and GSH decrease were observed as well. Moreover, sophoridine attenuated the expression of FoxM1 through suppression of its transcriptional activity. CONCLUSION: It suggests that sophoridine may inhibit proliferation and induce apoptosis of adenocarcinoma from esophagogastric junction in vitro through down-regulating the expression of FoxM1.
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Objective To determine the content of sophocarpine, matrine, oxysophocarpine, sophoridine, oxymatrine in Sophora Flavescentis Radix from different areas. Methods Agilent ZORBAX NH2 column (4.6 mm×150 mm, 5 μm) was used with mobile phase of acetonitrile-ethanol-3% phosphate (84∶10∶6), at a flow rate of 1 mL/min. The wavelength of detection was 210 nm. Results The linear range of sophocarpine, matrine, oxysophocarpine, sophoridine and oxymatrine were 0.022 88-0.114 4 μg (r=0.999 7), 0.083 2-0.416 0 μg (r=0.999 7), 0.376 2-1.836 0 μg (r=0.999 8), 0.104 4-0.522 μg (r=0.999 2), 0.491 2-2.456 μg (r=0.999 9), respectively. The average recovery were 101.63% (RSD=2.08%), 98.29%(RSD=1.87%), 101.89% (RSD=1.97%), 99.87% (RSD=2.06%), 102.66% (RSD=1.34%), respectively. Conclusion The method is simple, rapid and accurate, and suitable for the quality control of Sophorae Flavescentis Radix.
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Objective: To establish a high performance liquid chromatography approach for determining matrine and sophoridine contents in Ganlibao capsule. Methods: Agilent NH2 (4. 6 mm × 250 mm, 5μm) column was used with 1% phosphoric acid: ethanol: acetonitrile (V/V/V=10:22: 68) as the mobile phase. The flow rate was 0. 8 ml/min, and the temperature was at 25°C. The detection wavelength was set at 210 nm. Results: The calibration curve of matrine showed a good linearity in the range of 5.21-156.3 μg/ml (r=l) and that of sophoridine in the range of 5. 29-158. 7 μg/ml (r=0.9999). The equations of linear regression of matrine and sophoridine were Y = 9. 586 IX + 1. 003 8 and Y = 7. 604 3X - 5.9201,respectively. The recovery was 98. 73% (RSD=3.67%) for matrine and 100. 10% (RSD = 2.24%) for sophoridine. The matrine content of 15 batches of Ganlibao capsule was (30.13 ± 0. 19)-(44.70 ±0.17) mg/g and the sophoridine content was (21.60 ± 0.25)-(52.07 ± 0.11) mg/g. Conclusion: The present method is simple, accurate, and reproducible, and it can be used for the quality control of Ganlibao capsule.
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Objective To explore the effects of sophoridine on cardiac function and myocardial ultrastructure of rats with myocardial infarction. Methods The SD rat model of myocardial infarction (MI) was obtained by permanent ligation of the left anterior descending coronary artery (LAD), and the model ratswere randomly divided into model group (rats with MI), lowdose group (5 mg/kg sophoridine), middle-dose group (10 mg/kg sophoridine), and high-dose group (20 mg/kg sophoridine); a sham operated group was also included. Each group had 10 rats. The elevated left ventricular end-diastolic pressure (LVEDP), ±dp/cdmax and heart mass/body mass (HM/BM) were determined after experiment, and the changes of myocardial ultrastructure were observed by transmission electron microscope. Results Compared with the sham operated group, ±dp/cdmax in MI group was significantly decreased, and LVEDP and HM/BM were remarkably increased (all P<0. 01). Compared with MI group, ±dp/cdm in the 3 sophoridine groupswere significantly increased, and LVEDP and HM/BM were significantly decreased (P<0. 01, P<0. 05), except for-dp/cdmax in the low-dose sophoridine group. Transmission electron microscope foundthat the myofilaments of myocardial cells in the sham operated group were well arranged, with normal mitochondria. The myofilaments were dissolved in MI rats, with swollen mitochondria and blurred cristae, showing distinct pathological changes. Therewas a slight improvement in myofilament dissolution in the low-dose sophoridine group, and the myofilament dissolution disappeared in the middle and high-dose group, with well arranged myofilaments. Conclusion Sophoridine can improve the cardiac function of MI rats, and has protective effects on ultrastructure of myocardial cells.
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Objective: To investigate and optimize the formulation of sophoridine liposomes. Methods: Sophoridine liposomes were prepared by ammonium sulfate transmembrane gradient method. On the basis of single factor experiments, the effects of influence factors, such as entrapment efficiency, drug loading, and comprehensive indexes, were investigated by using central composite design and response surface method. The influence factors included the concentration of drug and ammonium sulfate. The data were imitated using multi-linear equation and second-order polynomial equation. Results: The latter was prior to the former considering from multiple correlation coefficients. Under the optimal conditions, the entrapment efficiency and drug loading of sophoridine liposomes were 51.81% and 5.39%. Conclusion: The optimized preparation technique for sophoridine liposomes is stable and feasible.
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Objective To boserve the effects of sophoridine on central nervous system in mice. Methods Behavioral methodology was employed to observe the effect of sophoridine on the normal mouse autonomic activities, and sleeping latency and sleep-lasting time of mice under threshold dosage of pentobarbital sodium. And to observe the synergistic effects of inducing convulsion between sophoridine and pentylenetetrazol, nicotin, strychine, isoniazid, and picrotoxin by subthreshold dosage. Results Sophoridine ip administrated (10 and 20 mg/kg) made the autonomic activities of mice suppressed by the rate of 66.9% and 76.6%, the sleeping latency of mice given pentobarbital sodium (40 mg/kg) prolonged, and sleeping time shortened (P
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AIM: To establish an HPLC method for determining sophocarpine,sophoridine and oxymatrine in Sophora flavescens Ait,so as to investigate their contents in different years and different parts. METHODS: An Elite Hypersil NH2 column(250 mm ? 4. 6 mm,5 ?m) was used with the mobile phase being acetonitrile-absolute alcohol-3% phosphoric acid solution(82 ∶ 10 ∶ 8),flow rate being 1 mL/min,determinating wavelength being 220 nm,the column temperature being 26 ℃,The injection volume was 5 ?L. RESULTS: The calibration curves of sophocarpine,sophoridine and oxymatrine were in good linearity over the ranges of 0. 004 99 - 0. 149 7 ?g(r = 0. 999 9),0. 025 08 - 0. 752 25 ?g(r = 0. 999 9),0. 075 38 - 2. 261 25 ?g(r = 0. 999 9); and the average recovery of sophocarpine,sophoridine and oxymatrine was 99. 91% ,99. 26% ,100. 27% with RSD of 1. 11% , 0. 82% ,2. 18% respectively. CONCLUSION: The HPLC method shows a good separation,reproducibility and accuracy,there are obvious differences in the contents of three alkaloids in different years and different parts of Sophora flavescens Ait. The results provide important data for quality evaluation and utilization of Sophora flavescens materials.
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AIM: To study the effect of the four alkaloids of Sophora Alopecuroides On cycloxygenase(COX) activities in vitro. METHODS: The effect of matrine, oxymatrine sophocarpine and sophoridine on COX2 and COX1 activity were evaluated by the content of Prostaglandin E_2(PGE_2) and 6-Keto-PGF_~1a , respectively. The PGE_2 came from exogenous AA in cultured mouse peritoneal macrophage supernatants induced by lipopolysaccharide(LPS) 1 ug?mL~-1 was measured with radioimmunoassay(RIA) method using ~ 3H-labelled PGE_2. The 6-Keto-PGF_~1a from exogenous AA in cultured mouse peritoneal macrophage supernatants induced by calcium ionophore A23187 1 ?mol?L~-1 was measured with RIA method using~125 I-labelled 6-Keto-PGF_~1a . RESULTS: The COX2 activities were markedly inhibited in a dose dependent manner by oxymatrine, sophocarpine and sophoridine, Respectively. Excluding the sophoridine, all the other three alkaloids of Sophora Alopecuroids obviously suppressed the activities of COX1, respectively. CONCLUSION: The in vitro results show that oxymatrine, sophocarpine and sophoridine may have the significant specific inhibitory action for COX2, in contrase, matrine may be COX1 selective inhibitor.
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The LVdP/dtmax, LVSP, AP and Vmax of the rat hearts in vivo were increased by Sophoridine ( 2 mg/kg, given to rats iv ) by 19.5, 13.1, 14.8 and 28.2% respectively. Such a positive inotropic effect lasted for more than 5 min and was statistically significant. Adrenaline (0.16 ?g/kg, iv ) could also increase the LVdP/dtmax and Vmax of the heart obviously and this action was not stronger than Sri after uses of drugs except at 0.5 min and vanished more quickly. There was an increment of MVO2I because of the increased arterial pressure within 3 min after use of Sri, which was much less than adrenaline. The present results show Sri strengthened the cardial force for longer time and affected the arterial pressure and MVO2I less than adrenaline in the rat hearts in vivo.
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Aim To investigate the growth-inhibition and the mechanism of apoptosis induced by sophoridine(SRI) on SW620 cells.Method MTT assay was used to detect the half-inhibition concentration(IC50),and fluorescence microscopy,electron microscopy,DNA fragmentation analysis,flow cytometry(FCM) were used to demonstrate the presence of apoptosis.Results SRI inhibited the growth of SW620 cells significantly in a dose-and time-dependent manner,and morphological characteristics of apoptosis were observed with condensation of nucleus,bubble of cytoplasm,fragment of nucleus.A DNA ladder pattern of internucleosomalfragmentation was observed.Compared with that of control group,the percentage of the G0/G1 phase and the Sphase cells increased after treated by SRI.SW620 cells were induced to undergo apoptosis and underwent G0/G1 arrest with exposure to SRI shown by FCM.Conclusions Sophoridine could induce the inhibition of cell growth by means of apoptosis in a dose-and time-dependent manner,and the blocking of G0/G1 phase of cells was involved in the mechanism of apoptosis.