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OBJECTIVE To provide a reference for comprehensive quality evaluation and control of the effective parts of Dracocephalum moldavica （EPDM）. METHODS A total of 10 batches of EPDM were prepared， and chemical information of EPDM was collected by HPLC-Q-Exactive-MS. EPDM components were identified by literature search， database comparison and manual analysis. HPLC fingerprints of 10 batches of EPDM were established by using the Similarity Evaluation System for Traditional Chinese Medicine Chromatographic Fingerprint （2004 A edition）； the similarity evaluation and common peak identification were carried out， and the contents of 5 index components were determined by HPLC. RESULTS A total of 11 compounds in EPDM were identified. The fingerprint similarities of EPDM samples from 10 batches were all above 0.96. Among 11 chromatographic peaks， 5 peaks were identified， such as luteolin-7-O-β-D-glucuronide（LG）， apigenin-7-O-glucuronide（APG）， rosmarinic acid（RA）， diosmetin-7-O-β-D-glucuronide（DG）， tilianin（TL） . The results of the quantitative analysis showed that all above 5 components had good linearity （R2≥0.999）， and the average recoveries were in the range of 95.12%-98.37%. The contents of LG， APG， RA， DG， TL were 21.268 3-29.243 9， 6.365 4-7.771 7， 37.327 4-45.671 2， 17.169 9-21.985 9， 66.940 4-91.206 3 mg/g， respectively. CONCLUSIONS The established method of component identification， fingerprint and content determination is stable， feasible and reliable， which is suitable for the comprehensive quality evaluation and control of EPDM.
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OBJECTIVE To establish the method for t he content determination of 5 active components in Yixin badiran jibuya granules and their fingerprints. METHODS High performance liquid chromatography method was adopted to determine the contents of luteolin- 7-O-β-D-glucuronide（LG），apigenin-7-O-glucuronide（APG），rosmarinic acid （RA），diosmetin-7-O-β-D-glucuronide （DG）and tilianin （TL）in 10 batches（No. S 1-S10）of Yixin badiran jibuya granules. The fingerprints of 10 batches of Yixin badiran jibuya granules were drawn by Similarity Evaluation System of Chromatographic Fingerprint of Traditional Chinese Medicine（2004 A edition ），and similarity evaluation and cluster analysis were also performed. RESULTS The contents of LG ， APG，RA，DG and TL in 10 batches of Yixin badiran jibuya granules were 0.279 5-0.449 9，0.082 4-0.135 3，0.184 8-0.472 1， 0.149 0-0.332 6，0.311 2-0.623 3 mg/g，respectively. A total of 13 common peaks were demarcated in the fingerprints and were identified as LG （peak 2）APG（peak 6），RA（peak 7），DG（peak 8），TL（peak 11）. The similarity ranged from 0.598 to 0.990. The results of cluster analysis showed that S 6-S10 were clustered into one category and S 1-S5 were clustered into one category. CONCLUSIONS Established method for content determination and fingerprints can be used for the quality control for Yixin badiran jibuya granules.
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In order to research and enhance bioavailability of chlorogenic acid and rutin[CA-R] via the oral route, chitosan coated composite phospholipid liposomes [C-CPLs] were applied to study on preparation, permeability and pharmacokinetic of C-CA-R-CPLs. TheC-CA-R-CPLs were prepared by the method of ethanol injection. The entrapment efficiency [EE], average particle sizes, polymer disperse index [PDI], zeta potential, shape and in vitro drug release were investigated to characterize physicochemical parameters of C-CA-R-CPLs. The penetration properties from C-CA-R-CPLs were studied through Caco-2 cells model and the pharmacokinetics in Sprague-Dawley [SD] rats were evaluated by rat jugular vein intubation tube. The EE of C-CA-R-CPLs of CA and R was 91.3+/-2.13% and 92.6+/-2.44%, particle size of C-CA-R-CPLs was 176.7+/-2.3 nm, PDI was 0.207+/-0.014 and zeta potential of 12.61+/-1.33 mV. CA-RCPLs and C-CA-R-CPLs were spherical or elliptical sphere and the bilayer of the CPL was observed obviously under transmission electron. The C [max], t1/2 and AUC[0-12] h values of CA and R for groups of C-CA-R-CPLs were significantly increased.In conclusion, TheC-CA-R-CPLs as a novel nano-formulation have potential to be used to enhance the oral bioavailability of poorlywater-soluble drugs after oral administration
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OBJECTIVE:To study the effects of tilianin(TIL)on brain tissue in rats with cerebral ischemia-reperfusion injury. METHODS:Totally 120 male SD rats were randomly divided into sham operation group(0.9% sodium chloride solution),model group(0.9% sodium chloride solution),nimodipine group(32 mg/kg)and TIL low-dose and medium-dose,high-dose groups(4, 8,16 mg/kg),with 20 rats in each group. The rats were given relevant medicine intragastrically,once a day,for consecutive 7 d. 15 min after last medication,cerebral ischemia-reperfusion injury model was established by reforming suture-occluded method. The neurological deficit score in rats were evaluated, and percentage of cerebral infarction volume of rats was determined. Histopathological changes of brain tissue were observed by HE staining. The activities of SOD,CAT and LDH,MDA content in cerebral tissue of rats were determined. The expression of calcitonin gene-related peptide(CGRP)and peripheral vascular endothelial growth factor receptor 2 (VEGFR2) protein were determined by Western blot assay. RESULTS:Compared with sham operation group,neurological deficit score and percentage of cerebral infarction volume of model group were increased significantly(P＜0.01);the nerve cells in brain tissue were significantly reduced and the interstitial edema was obvious. SOD and CAT activities were decreased significantly,LDH activity was increased significantly,MDA content was decreased significantly,protein expression of CGRP and VEGFR2were increased significantly(P＜0.05 or P＜0.01). Compared with model group,neurological deficit score of nimodipine group,TIL medium-dose and high-dose groups were decreased significantly;percentage of cerebral infarction volume was decreased significantly (P＜0.05 or P＜0.01);above pathological conditions of cerebral tissue in rats were relieved significantly;SOD and CAT activities were strengthened significantly,MDA content and LDH activities were decreased significantly,protein expression of CGRP and VEGFR2were increased significantly (P＜0.05 or P＜0.01). CONCLUSIONS: TIL has certain protective effects on cerebral ischemia-reperfusion injury model rats,and its mechanism may be related to the up-regulation of CGRP and VEGFR2expression.
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Objective To evaluate the effects of capparis spinosa total alkaloid on transforming growth factor-β( TGF-β)/Smad4 signalling pathways in systemic sclerosis (SSc). Methods A total of 90 BALB/c mice were randomly divided into normal control group, model control group, penicillamine ( 125 mg·kg-1) group and Capparis spinosa total alkaloid low (225 mg·kg-1),medium (450 mg·kg-1) and high ( 900 mg·kg-1) dose group. Except for the normal control group,SSc mouse model was established by daily subcutaneous injection of bleomycin in the back of the mice.After the establishment of the model,Capparis spinosa total alkaloid emulsifiable paste was externally applied to Capparis spinosa total alkaloid group,ground substance was externally applied to the mice in normal control group and model control groups, and penicillamine was intragastrically administrated in the penicillamine group for 60 days,once daily.After the treatment,The expression of TGF-β1in skin tissue was detected by Western-blotting and the levels of actin / in receptor-like kinase / Smad4, nuclear factor-κB in skin tissue were measured by ELISA. Results The expression of TGF-β1was significantly decreased after administration of 225,450 and 900 mg·kg-1capparis spinosa total alkaloid, and the levels of ALK1 and Smad4 were significantly decreased after administration of 900 mg·kg-1capparis spinosa total alkaloid as compared with model control group (P<0.05 or P<0.01),but the content of NF-κB was not influenced (P>0.05). Conclusion Capparis spinosa total alkaloid can accommodate abnormal expression of TGF-β1/Smad4 signalling pathways in SSc.
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The present study was undertaken to optimize the preparation conditions of total flavonoids extract from Dracocephalum Moldavuca composite phospholipid liposome [TFDMCPL]by response surface methodology [RSM] and to investigate the in vitro release [IVR] of TFDMCPL. Method of ethanol injection was adopted to prepare TFDMCPL. The single factor experiments were used for the key experimental factors and their test range. Based on the single factor experiments, with encapsulation efficiency [EE] Size of TFDMCPL and polymey disperse index [PDI] as dependent variable, central composite design was adopted to optimize preparation technology by taking content of phospholipid and content of cholesterol as independent variables, fitting of various mathematical equations were performed using a statisitical software of Design-Expert 8.0.6. Preparation parameters were optimized through response surface plotted by optimum fitting equations, optimized procedure was validated through experimental preparation of TFDMCPL. Optimum preparation technology was as following: phospholipid 505mg and cholesterol 50mg. Under these condition, encapsulation efficiency was 90.2+/-1.2%, size of TFDMCPL was 115.6+/-4.3nm, PDI was 0.169+/-0.015 and Zeta potential was -15.38+/-0.5. These indicated that TFDMCPL with high entrapping efficiency and small particle size could be prepared by the ethanol injection method. And TFDMCPL were found to enhance the release of drugs more effectively than TFDM based on the in vitro model
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In Vitro Techniques , Plant Extracts , Phospholipids , Liposomes , FlavonoidsABSTRACT
Objective To observe the effects of Capparis spinosa total alkaloid on vascular endothelial growth factor (VEGF),endothelin-1(ET-1) and soluble vascular cell adhesion molecule-1 (sVCAM-1) levels in systemic sclerosis (SSc) mouse model and explore the therapeutic mechanism of Capparis spinosa total alkaloid for the treatment of SSc. Methods A total of 90 BALB/c mice were randomly divided into blank control group,model control group,penicillamine (125 mg·kg-1) group and Capparis spinosa total alkaloid low(225 mg·kg-1),medium(450 mg·kg-1) and high(900 mg·kg-1) dose group. Except for the blank control group,SSc mouse model was established by daily subcutaneous injection of bleomycin in the back of the mice.After establishing model successfully,Capparis spinosa total alkaloid emulsifiable paste was externally applied with Capparis spinosa total alkaloid group,ground substance was externally applied to the mice in blank control group and model control groups,penicillamine was intragastrically administrated in the penicillamine group for 60 days,once daily.After the treatment,the content of VEGF in skin tissue and ET-1,sVCAM-1 in serum were measured by ELISA. Results The levels of VEGF and ET-1 were significantly decreased in Capparis spinosa total alkaloid high dose group as compared with model control group(P<0.05, P<0.01),but the content of sVCAM-1 wasn't influenced(P>0.05). Conclusion Capparis spinosa total alkaloid is effective in adjusting abnormal expression of VEGF and ET-1 in SSc mice.
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Objective To investigate the effects of capparis spinosa total alkaloid on type collagen (ColⅣ - ),Ⅳmatrix metalloproteinase-9 (MMP-9), tissue inhibitor of metalloproteinase-1 (TIMP-1) and plasminogen activator inhibitor-1 (PAI-1) in bleomycin-induced systemic sclerosis (SSc) mice; To explore the effective mechanism of capparis spinosa total alkaloid on fibrosis of SSc. Methods Totally 90 BALB/c mice were randomly divided into control group, model group, penicillamine group and capparis spinosa total alkaloid low-, medium- and high-dose group. Mice models with SSc were established by repeated local injections of bleomycin in mice back, except for the control group. Mice in medication groups received external application with capparis spinosa total alkaloid cream;mice in penicillamine group were given penicillamine for gavage; mice in the control and model group received external application without substance, one time a day, for 60 days. The contents of MMP-9, TIMP-1 and PAI-1 in serum and Col- in skin tissue were dⅣ etected respectively by ELISA after the last medication. Results Compared with the model group, the levels of MMP-9 and ratio of MMP-9/TIMP-1 markedly increased and the levels of Col-Ⅳand TIMP-1 markedly decreased in medium and high- dose of capparis spinosa total alkaloid group (P0.05). Conclusion Capparis spinosa total alkaloid is effective in treating fibrosis of SSc by adjusting imbalance of MMP-9/TIMP-1 and decreasing expression of Col-Ⅳ.
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Objective To investigate the effects of capparis spinosa total alkaloid on the pathological changes and the type Ⅲ collagen(COL?Ⅲ)expression in systemic sclerosis(SSc)mice. Methods Mice models with SSc were established by repeated local injection of bleomycin in BALB/c mice back. After administration of capparis spinosa total alkaloid ,the pathological changes of skin and lung tissue were observed ,and the COL?Ⅲ expression was detected by ELISA. Results Compared with the model group,the inflammation and fibrosis of skin and lung tissue were improved,and the level of COL?Ⅲ was markedly reduced by treatment of high dose capparis spinosa total alkaloid(P<0.05). Conclusion Cap?paris spinosa total alkaloid is effective in treating fibrosis of SSc.
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OBJECTIVE:To establish a method for content determination of rosmarinic acid and total polysaccharide in Hysso-pus. offcinalis. METHODS:HPLC was conducted to determine the content of rosmarinic acid in H. offcinalis. The column was Shim-pack VP-ODS with mobile phase of acetonitrile-0.5% formic(17:83,V/V) at flow rate of 1.0 ml/min,detection wavelength was 330 nm,column temperature was 30 ℃,and the injection volume was 10 μl. UV-visible spectrophotometry was conducted to determine the content of total polysaccharide,detection wavelength was 620 nm. RESULTS:The linear range was 10.86-54.30 μg/ml (r=0.999 8)for rosmarinic acid and 1.996-15.97 μg/ml for total polysaccharide(r=0.999 6);RSDs of precision,stability and re-producibility tests were lower than 1.0% and 2.0%,respectively;recoveries were 98.20%-101.79%(RSD=1.68%,n=6) and 96.62%-101.68%(RSD=1.88%,n=6). CONCLUSIONS:The method is simple and reproducible,and can be used for the con-tents determination of rosmarinic acid and total polysaccharide in H. offcinalis.
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Hot-melt extrusion (HME) is the process of pumping raw materials with a rotating screw under the elevated temperature and pressure through a die to from a product with the uniform shape. This technique combines many advantages of solid dispersion technology and mechanical preparation, including dust reduction, short duration of extrusion process, without use of organic solvents and water, without heat drying and hydrolysis, etc. In addition, it has the superiority in solubility, taste masking, drug stability and drug release. Besides, this technique has good reproducibility, high production efficiency, and it can be online monitored in the mass production. Therefore, this technique is widely used in the research and development of drug dosage forms involved in rapid and immediate drug release, sustained drug release, gastrointestinal drug site-specific release, transdermal drug delivery systems and so on. This paper reviews the advantages of HME and its recent application in the pharmaceutical research.
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Objective To investigate the effect of moldavica total flavone on pulmonary function and collagen type Ⅲ in lung tissue of ovalbumin-induced bronchial asthmatic rats. Methods A total of 60 SD rats were randomly divided into control group, model group, dexamethasone group, and moldavica total flavone low, medium and high dose group. Rat asthma model was established by ovalbumin challenge methods except the control group. The control and model group were intragastrically given distilled water, medicine groups were intragastrically given moldavica total flavone and dexamethasone for 30 d, once per day. After the last administration, the pulmonary function and airway responsiveness including breathing frequency (F), minute ventilation (MVb), peak inspiratory flow (PIFb), peak expiratory flow (PEFb) and enhanced pause (Penh) were measured by using non-invasive measurement system (Penh system, Buxco, USA). The collagen type Ⅲ in lung tissue were detected by ELISA. Results The moldavica total flavone at 180 and 360 mg/kg decreased F and Penh (P<0.05, P<0.01), increased MVb, PIFb and PEFb (P<0.05), and decreased collagen type Ⅲ in lung tissue (P<0.05, P<0.01). Conclusion Moldavica total flavone can relieve the airway hyperresponsiveness and remodeling, improve respiratory function of ovalbumin-induced bronchial asthmatic rats.
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Objective To investigate the effects of moldavica total flavone on vascular endothelial growth factor (VEGF), intercellular adhesion molecule-1 (ICAM-1), nitric oxide (NO) and endothelin-1 (ET-1) in ovalbumin-induced bronchial asthmatic rats, and explore its mechanism. Methods A total of 60 SD rats was randomly divided into control group, model group, dexamethasone (1 mg/kg) group and moldavica total flavone low (90 mg/kg), medium (180 mg/kg) and high (360 mg/kg) dose group. Rats asthma model was established by ovalbumin challenge methods except the control group. After modeling, rats in control and model groups were intragastrically given distilled water, rats in medicine groups were intragastrically given moldavica total flavone and dexamethasone for 30 d. VEGF in lung tissue and ICAM-1 in bronchoalveolar lavage fluid (BALF) were detected respectively by ELISA. The content of ET-1 and NO in BALF were analyzed with radioimmunity method and nitric acid reductase method. Results The VEGF in lung tissue and ICAM-1, NO and ET-1 in BALF were decreased by moldavica total flavone at 180 and 360 mg/kg (P<0.05, P<0.01) in ovalbumin-induced bronchial asthmatic rats. Conclusion Moldavica total flavone is effective in adjusting abnormal increase of VEGF, ICAM-1, ET-1 and NO of bronchial asthma rats.
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<p><b>OBJECTIVE</b>To study the effects of different penetration enhancers on the transcutaneous permeability of syringin, chologenic acid and rutin in Xuelian cataplasm in vitro and to determine the effective enhancer.</p><p><b>METHOD</b>Using improved Franz-type diffusion cell and excised big mouse skin in vitro as transdermal barrier, the kinetics parameters of syringin, chologenic acid and rutin in Xuelian cataplasm such as cumulative permeation quantity, permeation rate were determined by HPLC. The enhancement ability of azone (A-zone), propylene glycol (PG) was investigated when used either uniquely or combinatively.</p><p><b>RESULT</b>With the 7% azone, the syringin, chologenic acid and rutin in Xuelian cataplasm could penetrate through the skin of rats well.</p><p><b>CONCLUSION</b>The selection of the best penetration enhancers provide reference for Xuelian cataplasm.</p>
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Animals , Mice , Rats , Drug Carriers , Chemistry , Drugs, Chinese Herbal , Chemistry , Pharmacokinetics , Glucosides , Chemistry , Pharmacokinetics , In Vitro Techniques , Permeability , Phenylpropionates , Chemistry , Pharmacokinetics , Propylene Glycol , Rutin , Chemistry , Pharmacokinetics , Skin AbsorptionABSTRACT
Objective To study the technological parameters of the purification process for active cons-tituents from Saussurea involucrata.Methods Using absorption and desorption rates of syringin,chologenic acid,and rutin as the primary screening indexes,four resins were selected,and the conditions of absorption and desorption were optimized for active constituents.Results Resin HPD400 gave good separation performance and was selected to purify the active constituents in S.involucrata.The optimum parameters were established as followings:4 BV(bed volume)sample extract whose pH value was adjusted to pH 2-3 by HCl was passed through the column with a flow rate of 1 BV/h,12 h later,the column was washed with 4 BV water,6 BV 30% ethanol and 4 BV 50% ethanol,respectively.The combined 30% and 50% ethanolic elutes were taken as object products.Conclusion The contents of active constituents were increased to about five times.Macroporous absorption resin HPD400 could be well used in separating and purifying the active constittuents from S.involucrata.