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1.
Acta Pharmaceutica Sinica ; (12): 3268-3276, 2021.
Article in Chinese | WPRIM | ID: wpr-906841

ABSTRACT

Cryptotanshinone (CPT), an active ingredient with the inhibitory effect on brain glioma cells, is trapped with poor solubility and low tumor permeability. Therefore, it is urgent to design nano drug delivery systems characterized with deep penetration and accurate targeting. In the present study, tLyp-1 modified liposomes loaded with CPT (tLipo/CPT) was prepared by emulsion solvent evaporation method. Peptide tLyp-1 which targeting tumor angiogenesis and neuropilin receptors (NRP) was modified on surface of CPT liposomes, with the aim of active targeting brain glioma cells and further release CPT precisely. The size and polymer dispersity index (PDI) of tLipo/CPT were (162.2 ± 14.6) nm and 0.24 ± 0.03. The optimal molar ratio of tLyp-1 modified on CPT liposomes was 0.5% determined by intracellular fluorescence parameters. The morphology displayed a smooth sphericity structure as determined by transmission electron microscope. Efficiency of CPT encapsulated in tLipo/CPT was detected by high performance liquid chromatography. The encapsulation efficiency of CPT was (70.06 ± 7.22) %. Liposomes modified with tLyp-1 peptide (tLipo) were internalized more than liposomes not modified with tLyp-1 (Lipo) by GL261 cells. Fluorescence intensity of tLipo in GL261 cells increased 40% than that of Lipo. Furthermore, we proved that the intake of tLipo/CPT in GL261 cells was mediated by NRP-1 receptor. MTT analysis indicated that tLipo/CPT significantly inhibit the proliferation of GL261 cells. The half maximal inhibitory concentration (IC50) was 5.70 μmol·L-1. In vitro blood-brain barrier (BBB) model experiment indicated that tLipo/CPT could penetration across BBB. Moreover, in vivo fluorescence biodistribution study indicated tail vein injection of DiR labeled tLipo after 0.5 h, DiR fluorescence could be observed in the brain of mice. Even after 24 h, DiR fluorescence still was observed in the brain. Our research certified that tLipo/CPT can penetrate the BBB and show effect of anti-glioma by inhibiting the proliferation of GL261 cells. The animal experiment was carried out in accordance with protocol evaluated and approved by the Ethics Committee of Nanjing University of Chinese Medicine.

2.
Acta Pharmaceutica Sinica ; (12): 2112-2118, 2021.
Article in Chinese | WPRIM | ID: wpr-887061

ABSTRACT

Ma-Xing-Shi-Gan Decoction is a classic prescription. However, the interaction among multiple components of the decoction and the change of phase state are not clear. Moreover, the relationship between the physical phase state aggregated by multiple components and the efficacy still needs to be studied. In this study, we monitored the particle size changes of Ma-Xing-Shi-Gan Decoction in real time. Then we isolated different phase states by centrifugation, analyzed their composition distribution and tested their antibacterial activity. We added chemical interference agents to investigate the interaction of multi-component physical phase states accompanied by the observation of particle size change and morphology. We also studied the correlation between antibacterial activity and physical structure of phase states. The results showed during boiling process the degree of hybridization of particles was decreased and the particle size distribution was narrowed and stabilized at 170 nm. The distribution of organic and inorganic components was heterogeneous among different phase states. S-13500, supernatant isolated by 13 500 ×g centrifugation, constituted by ephedrine, amygdalin, glycyrrhizic acid and inorganic components Ca, K, Mg, etc., had the strongest antibacterial activity. The molecular interaction force in the active physical phase state was mainly hydrophobic and hydrogen bond. The destruction of the interaction force will lead to the change of phase structure and the decrease of antibacterial activity in vitro and in vivo. This study confirms that, in the boiling process of the Ma-Xing-Shi-Gan Decoction, the chemical components interweave and interact to form new physical phase states, leading to heterogeneous distribution of components. The antimicrobial activity of the active phase depends on both chemical composition and physical structure, which provides a direct evidence for the physical basis of the efficacy of traditional Chinese medicine.

3.
Article in English | WPRIM | ID: wpr-922768

ABSTRACT

Chansu has demonstrated adverse reactions in clinical settings, which is associated with its toxicity and limits its clinical applications. But there are methodological limitations for drug safety evaluation. In the current study, ultra-high performance liquid chromatography, lipidomic profiling, and molecular docking were used to systemically assess Chansu-induced acute inflammatory irritation and further identify the underlying drug targets. Compared with the EtOAc extract, Chansu water fraction containing indolealkylamines caused acute inflammatory irritation in rats, including acute pain (spontaneous raising foot reaction), and inflammation (paw edema). At the molecular level, lipids analysis revealed significantly higher levels of pro-inflammatory mediators of the COX and LOX pathways. However, anti-inflammatory mediators from the CYP 450, ALA, and DHA pathways markedly decreased after exposure to Chansu water fraction. Moreover, four indolealkylamines from Chansu showed a high theoretical affinity to a known irritation target, 5-HT


Subject(s)
Animals , Bufanolides , Edema/drug therapy , Inflammation , Lipidomics , Molecular Docking Simulation , Rats , Water
4.
Article in Chinese | WPRIM | ID: wpr-879145

ABSTRACT

The research on the pharmacodynamic substance basis of traditional Chinese medicine(TCM) is a key scientific issue for the inheritance and development of TCM. At present, a large number of remarkable achievements have been made in the field of chemical components in Chinese medicine, however, another important aspect, namely the physical structure and mode of action of the multi-component assembly of TCM, has not been clearly understood and deeply studied. From the bottleneck of restricting material ba-sic research, we objectively analyzed the common cause of the existing problems. Based on the new discoveries and advances of active substances from TCM emerging in recent years, we extracted and summarized the concept of structural Chinese medicine, elaborated the basic ideas, main features and research modes, hoping to provide theoretical and practical references for the study on the pharmacodynamic substance basis and other research fields of TCM.


Subject(s)
Drugs, Chinese Herbal/pharmacology , Medicine, Chinese Traditional
5.
Article in Chinese | WPRIM | ID: wpr-878919

ABSTRACT

To establish the HPLC fingerprint and multi-component determination method of fried Glycyrrhizae Radix et Rhizoma pieces. HPLC analysis was performed on Thermo Acclaim ~(TM)120 C_(18) column(4.6 mm×250 mm, 5 μm). Acetonitrile-0.1% phosphoric acid aqueous solution was taken as the mobile phase for gradient elution. The flow rate was 1 mL·min~(-1),the column temperature was maintained at 30 ℃, and the detection wavelength was 237 nm and 360 nm. The similarity of 15 batches of fried Glycyrrhizae Radix et Rhizoma pieces was higher than 0.849, and 17 common peaks were identified. Liquiritin, isoliquiritin apioside, isoliquiritin, liquiritigenin, isoliquiritigenin and glycyrrhizic acid were identified; among them, the mass fractions of Liquiritin, isoliquiritin apioside, isoliquiritin, liquiritigenin, glycyrrhizic acid were were 0.519%-3.058%, 0.227%-0.389%, 0.070%-0.439%, 0.038%-0.173%, 1.381%-4.252%, respectively. According to the cluster analysis, the 15 batches of decoction pieces were classified into three categories; principal component analysis screened out four principal components, with the cumulative variance contribution rate of 86.630%, indicating that the principal components contained most information of original data. Partial least squares discriminant ana-lysis marked 6 differential components in the decoction pieces. The established fingerprint and multicomponent determination are stable and reliable, and can provide a reference for the quality control of Radix Glycyrrhizae Radix et Rhizomae and fried Glycyrrhizae Radix et Rhizoma pieces.


Subject(s)
Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Plant Extracts , Quality Control
6.
Article in Chinese | WPRIM | ID: wpr-802185

ABSTRACT

Wendantang (WDT) is a classical traditional Chinese medicine prescription composed of Pinelliae Rhizoma, Bambuseae Caulis in Taenias, Aurantii Fructus Immaturus, Citri Reticulatae Pericarpium, Zingiberis Rhizoma Recens, Glycyrrhizae Radix et Rhizoma, with the effect in regulating Qi-movement and phlegm and relieving stomach and gallbladder. The clinical studies have proved that WDT has significant therapeutic effects on depression, insomnia, schizophrenia, Alzheimer's disease and other nervous system diseases, but wihtout systematic understanding of material basis and compatibility principle because of the complex chemical composition and the scattered research results. Focusing on the neurological diseases and based on the origin of ancient recipes and modern research examples, the author sorted out and summarized the active ingredients constituting the recipe, paid attention to the effect of the compatibility on the composition and efficacy transmission, and judged the rationality of composition intention and selection. On this basis, it comprehensively identifies the potential components and effective paths that can well treat the nervous system diseases, and had the overall understanding about mutual relationship between composition and efficiency. In this article, we expect to find its scientific basis of effective materials and the key technology of quality standards, and define the direction of future research, so as to provide valuable reference for secondary development and new preparations designed of classic prescriptions.

7.
Article in Chinese | WPRIM | ID: wpr-279263

ABSTRACT

To establish HPLC specific chromatogram and its correlation with the protection effect of Shuanghuanglian on MDCK (Madin-Darby canine kidney) cell injury induced by influenza A virus( H1N1). Nine recipes of Shuanghuanglian based on the official prescription were prepared according to orthogonal test for HPLC analysis and MDCK cells protection experiment separately (cytopathic effect (CPE) method was used for observing the virus infectivity and MTT staining results were used as the determining indexes for drug concentration selection and analyzing cell viability). The results suggested that all the other Shuang-Huang-Lian recipes except recipe1 demonstrate protecting effect on MDCK cell injury induced by influenza A virus (P < 0.01, P < 0.001). Stepwise regression analysis was used for analyzing the relationships between HPLC fingerprint and the protecting effect of Shuanghuanglian on influenza A virus induced MDCK cell injury. Peak 2, 3, 6, 8 and 12 were found to be strongly related with anti-influenza A virus efficacy. Stepwise regression analysis of recipes data and efficacy data showed that Lonicerae Japonicae Flos and Forsythiae Fructus were positively associated with the protecting effect of cells injury. From HPLC fingerprints, we found that peak 2, 3, 12 were from Lonicerae Japonicae Flos and peak 6, 8 were from Forsythiae Fructus. Four peaks were identified through comparing the retention time between the standard and Shuanghuanglian recipes, and they were chlorogenicacid, cryptochlorogenic acid, forsythoside B and 3,4-dicaffeoylquinic acid respectively. Caffeic acid derivatives in Lonicerae Japonicae Flos and Forsythiae Fructus were found to be greatly correlated with anti-influenza A virus efficacy and maybe the substance basis of Shuanghuanglian.


Subject(s)
Animals , Antiviral Agents , Pharmacology , Chromatography, High Pressure Liquid , Methods , Dogs , Drugs, Chinese Herbal , Pharmacology , Forsythia , Chemistry , Influenza A Virus, H1N1 Subtype , Physiology , Lonicera , Chemistry , Madin Darby Canine Kidney Cells , Scutellaria baicalensis , Chemistry
8.
Article in Chinese | WPRIM | ID: wpr-279226

ABSTRACT

To compare the difference of total phenol of magnolia solid dispersion prepared by different methods. Hot melt extrusion, solvent evaporation method, and fusion-cooling method were used to prepare total phenol of Magnolia accessory solid dispersion, Plastone S-630 and HPC. The drug dispersion state in the prepared solid dispersion was evaluated with DSC and X-ray diffraction; FT-IR method was used to analyze the possible connections between drug and accessories. Finally, accelerated stability-in vivo dissolution test was use to compare the stability differences between these three processes. The results of DSC and X-ray diffraction showed that all of the drug in solid dispersion processed by three processes can exist in amorphous form; FT-IR results also could not distinguish the difference between the three processes; accelerated stability-in vivo dissolution test showed the stability of solid dispersion prepared by HPC was better than Plastone S-630, and the same kinds of materials solid dispersion prepared by hot melt extrusion showed a better stability than the other two processes.


Subject(s)
Chemistry, Pharmaceutical , Methods , Drugs, Chinese Herbal , Chemistry , Magnolia , Chemistry , Phenol , Chemistry , Spectroscopy, Fourier Transform Infrared , X-Ray Diffraction
9.
Article in Chinese | WPRIM | ID: wpr-237733

ABSTRACT

HPLC analysis was performed to study the changes in chemical composition of ginseng extracts prepared from high quality ginseng with 0, 2, 4, 8 h of steamed times. An UFLC-MS/MS multiple-reaction monitoring (MRM) quantitative analysis was made to investigate the pharmacokinetic behavior differences of ginsenosides in mice ig administered of ginseng extracts with different steamed times in the negative ion mode, with Digoxin as the internal standard substance. The mice were injected with LPS to establish inflammation model after ig administration of ginseng for a week and the contents of tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) in mice plasma were detected by ELISA, in order to study on anti-inflammatory effects of ginseng with different steamed times. It was determined that levels of TNF-α and IL-1β were significantly decreased in inflammation model group ig administered of ginseng extracts with 8h of steamed time. The results showed that the chemical components in ginseng changed after steaming and the components into the blood changed, correspondingly. Ginseng with steamed 8 h contributes to anti-inflammatory effects. These results provided an experimental basis for revealing the active substance basis and dose-effect relationship of ginseng on anti-inflammatory effect.


Subject(s)
Animals , Anti-Inflammatory Agents , Chemistry , Pharmacokinetics , Chemistry, Pharmaceutical , Methods , Drugs, Chinese Herbal , Chemistry , Pharmacokinetics , Ginsenosides , Chemistry , Pharmacokinetics , Hot Temperature , Humans , Inflammation , Drug Therapy , Male , Mice , Mice, Inbred ICR , Panax , Chemistry , Time Factors
10.
Article in Chinese | WPRIM | ID: wpr-305363

ABSTRACT

Study on the effects of Astragali Radix main active flavone calycosin-7-O-β-D-glucoside on Saposhnikoviae Radix main active ingredients prim-O-glucosylcimifugin and cimifugin, a UPLC-MS/MS method for simultaneous determination of prim-O-glucosylcimifugin and cimifugin in rat plasma was established, and the comparative pharmacokinetics of prim-O-glucosylcimifugin and cimifugin after oral administration of prim-O-glucosylcimifugin and calycosin-7-O-β-D-glucoside-prim-O-glucosylcimifugin to rats were carried out, which might be conductive in exploring the rationality of Astragali Radix - Saposhnikoviae Radix herb couple. Twelve male SD rats were divided into two groups. Prim-O-glucosylcimifugin and cimifugin in rat plasma of different time points after oral administration of prim-O-glucosylcimifugin and calycosin-7-O-β-D-glucoside - prim-O-glucosylcimifugin to rats were determinated. And the main pharmacokinetic parameters were investigated using DAS 3. 2. 4. The established method was rapid, accurate and sensitive for simultaneous determination of prim-O-glucosylcimifugin and cimifugin in rat plasma. The analysis was performed on a Waters Acquity BEH C18 column (2.1 mm x 100 mm, 1.7 μm) with the mixture of acetonitrile and 0.1% formic acid/water as mobile phase, and the gradient elution at a flow rate of 0.3 mL x min(-1). The analytes were detected by tandem mass spectrometry with the electrospray ionization (ESI) source and in the multiple reaction monitoring (MRM) mode. Compared with prim-O-glucosylcimifugin group, the AUC(0-t)., and AUC(0-∞) of p-O-glucosylcimifugin as well as the C(max) of cimifugin significantly increased (P < 0.05) in calycosin-7-O-β-D-glucoside-prim-O-glucosylcimifugin group. Calycosin-7-O-β-D-glucoside could enhance the absorption of prim-O-glucosylcimifugin and cimifugin and improve the bioavailability, explaining preliminarily the rationality of Astragali Radix-Saposhnikoviae Radix herb couple.


Subject(s)
Animals , Chromatography, High Pressure Liquid , Chromones , Blood , Pharmacokinetics , Drug Interactions , Drugs, Chinese Herbal , Pharmacokinetics , Glucosides , Blood , Pharmacology , Isoflavones , Blood , Pharmacology , Male , Monosaccharides , Blood , Pharmacokinetics , Rats , Rats, Sprague-Dawley , Xanthenes , Blood , Pharmacokinetics
11.
Article in Chinese | WPRIM | ID: wpr-300239

ABSTRACT

To study on the effects of Achyranthes bidentata on Tongsaimai pellets main active ingredients chlorogenic acid, isoliquiritin, harpagoside and glycyrrhizin in rats in vivo pharmacokinetic behaviors, a method for the simultaneous determination of chlorogenic acid, isoliquiritin, harpagoside and liquiritigenin in rat plasma was established by UPLC-MS/MS. The analysis was performed on a waters Acquity BEH C18 column (2.1 mm x 100 mm, 1.7 microm) with the mixture of acetonitrile and 0.1% formic acid/water as mobile phase, and the gradient elution at a flow rate of 0.3 mL x min(-1). The analytes were detected by tandem mass spectrometry with the electrospray ionization (ESI) source and in the multiple reaction monitoring (MRM) mode. It turned out that the analytes of Tongsaimai pellets groups C(max) and AUC(Q-infinity) values were higher than that with A. bidentata group, and the C(max) values of chlorogenic acid had significantly difference (P < 0.05), the AUC(0-infinity) values of chlorogenic acid and glycyrrhizin had significantly difference (P < 0.05); The T(max) and CL values of two groups had no significantly difference. Results showed that the established method was specific, rapid, accurate and sensitive for the studies of Tongsaimai pellets four main active ingredients in rat in vivo pharmacokinetic, and A. bidentata have varying degrees of effects on Tongsaimai pellets four main active ingredients in rat in vivo pharmacokinetic behaviors.


Subject(s)
Achyranthes , Chemistry , Animals , Chalcone , Blood , Pharmacokinetics , Chlorogenic Acid , Blood , Pharmacokinetics , Drugs, Chinese Herbal , Pharmacokinetics , Glucosides , Blood , Pharmacokinetics , Glycosides , Blood , Pharmacokinetics , Glycyrrhizic Acid , Pharmacokinetics , Herb-Drug Interactions , Male , Pyrans , Blood , Pharmacokinetics , Rats , Rats, Sprague-Dawley , Tandem Mass Spectrometry
12.
Article in Chinese | WPRIM | ID: wpr-300201

ABSTRACT

Flavonoids are a class of important active ingredients in traditional Chinese medicine, pharmacological activity and in vivo process is the focus of research in recent years. Calycosin is the main active ingredients of flavonoids in Astragali Radix, recent studies indicate that it has many kinds of pharmacological activity, but the absorption and transport characteristics in vivo is unclear. The experiment using Caco-2 cell model, with apigenin as internal standard substance, using the method for the determination of drug concentration by HPLC, were studied at different concentrations and absorption transport characteristics of respectively adding different types of protein inhibitors. Data were analyzed by Q test, the results show that low, middle, high concentration of P(app)(BL-AP)/ P(app)(AP-BL) = 1.38 < 1.5, respectively adding different types of protein inhibitors, compared with the control group of P(app)(BL-AP)/ P(app)(AP-BL), there were no significant differences. Calycosin absorption may mainly passive transport, also involved in active transport mechanism, the transport may not be affected by the P-protein, MRP2 protein, SGLT protein.


Subject(s)
Absorption , Biological Transport , Caco-2 Cells , Chromatography, High Pressure Liquid , Culture Media, Conditioned , Chemistry , Drug Stability , Drugs, Chinese Herbal , Pharmacokinetics , Humans , Hydrogen-Ion Concentration , Isoflavones , Pharmacokinetics , Models, Biological
13.
Article in Chinese | WPRIM | ID: wpr-346878

ABSTRACT

Fingerprint technology is the key technology in modern Chinese medicine research, while spectrum-effect relationship research is the advanced stage of fingerprint research. Spectrum-effect relationship research can reveal the relationship between fingerprint and pharmacological effect through multiple statistical analyses, which can be used in Chinese medicine research. Spectrum-effect relationship has been used in many areas of Chinese medicine research, such as effective basis of single and compound Chinese medicine research, component compatibility research, processing mechanism research, pharmacological effect forecast research, technology optimization research, and so on. This paper systematically reviewed the application of spectrum-effect relationship in Chinese medicine research, and indicated some problems in spectrum-effect relationship research. At last, the authors give an outlook of the future of spectrum-effect relationship research.


Subject(s)
Animals , Biomedical Research , China , Drugs, Chinese Herbal , Chemistry , Pharmacology , Humans , Spectrum Analysis
14.
Article in Chinese | WPRIM | ID: wpr-291311

ABSTRACT

Drug-loading micro-particles are a targeted, positioned and controlled-release drug delivery carrier with a wide application prospect. Various micro-carrier drug delivery systems have their own advantages in promoting absorption, improving stability, targeting and controlled release. Accordingly, it is of far-reaching significance for the studies on micro carrier drug delivery systems to build oral traditional Chinese medicine (TCM) compound micro-carrier drug delivery systems with effective TCM components and effective fractions. This article introduces several features and advantages of oral micro-carrier drug delivery systems, and summarizes their application in the field of TCMs.


Subject(s)
Administration, Oral , Animals , Drug Carriers , Chemistry , Drug Delivery Systems , Methods , Drugs, Chinese Herbal , Chemistry , Humans
15.
Article in Chinese | WPRIM | ID: wpr-294089

ABSTRACT

Glycosides are important active components in traditional Chinese medicine (TCM). Their pharmacological activity, pharmacokinetic characteristics and in vivo existence become hotspots of current studies. The metabolic pathways of these glycosides are de-glycosylation mainly mediated by gut microbiota. After glycosides were metabolized into aglycones, they could be absorbed more easily and show better pharmacological effects. In this article, we reviewed the main glycosidase in gut microbiota which helps metabolize TCM glycosides, relevant bacterial strains which generate glycosidase, as well as the de-glycosylated metabolic pathways of the representative glycosides, on the basis of gut microbiota's important roles in in vivo metabolism and efficacy of TCM glycosides. We also preliminarily solved problems in studies on de-glycosylation of TCM glycosides.


Subject(s)
Animals , Bacteria , Metabolism , Drugs, Chinese Herbal , Chemistry , Metabolism , Gastrointestinal Tract , Metabolism , Microbiology , Glycosides , Chemistry , Metabolism , Glycosylation , Humans , Metagenome
16.
Acta Pharmaceutica Sinica ; (12): 1366-1369, 2011.
Article in Chinese | WPRIM | ID: wpr-232982

ABSTRACT

In this study, daphnetin and its major metabolites in the intestinal wall of rats were identified by liquid chromatography and quatrupole-time of flight mass spectrometry. Perfusion fluid of duodenum, jejunum, ileum and colon were collected separately for 2 hours from the rat intestine following perfusion with daphnetin. The metabolites of daphnetin in the perfusion fluid of different intestine segments were analyzed by the liquid chromatography and quatrupole-time of flight mass spectrometry. It is shown that the parent drug daphnetin and four metabolites were found in the perfusion fluid of duodenum, jejunum and ileum. However, no metabolites were found in the colon. Among the four metabolites, two daphnetin sulfates (m/z 257) were first discovered as the phase II metabolites of daphnetin in rats, which revealed a new way of daphnetin metabolism in rats.


Subject(s)
Animals , Chromatography, High Pressure Liquid , Colon , Metabolism , Duodenum , Metabolism , Ileum , Metabolism , Intestines , Metabolism , Jejunum , Metabolism , Male , Perfusion , Random Allocation , Rats , Rats, Sprague-Dawley , Spectrometry, Mass, Electrospray Ionization , Umbelliferones , Metabolism , Pharmacokinetics
17.
Acta Pharmaceutica Sinica ; (12): 1576-1581, 2010.
Article in Chinese | WPRIM | ID: wpr-250592

ABSTRACT

This study aimed to investigate the effects of concentration, intestinal section and borneol on the intestinal absorption of salvianolic acids. The experiment not only studied the intestinal absorption properties of three concentrations of rosmarinic acid, salvianolic acid B and salvianolic acid A at duodenum, jejunum and ileum, but also of salvianolic acids compatible with borneol at different concentrations using single-pass intestinal perfusion model in rat with phenol red as the marker. The results showed that salvianolic acids was stable under weak-acid condition and affected by metabolism enzyme; The Peff and Ka significantly different among three concentrations of rosmarinic acid and salvianolic acid B, whose intestinal absorption were saturated in high concentration, suggesting that the transport mechanisms of rosmarinic acid and salvianolic acid B were similar to active transport or facilitated diffusion; However, there was inconspicuousness in the Peff and Ka of salvianolic acid A at different concentrations, whose absorption was not saturated in high concentration, indicating that the transport mechanisms of salvianolic acid A was passive diffusion; The Peff and Ka in the ileum obviously higher than those in the duodenum and jejunum, namely the ileum was the best absorption section; When concentration of borneol increased, the enhancing effect of intestinal absorption of salvianolic acids increased, but significantly decreased when borneol increased to some degree. The enhancing effect of medium borneol concentration was the optimum. This implied that borneol can enhance the intestinal absorption of salvianolic acids, and the capacity of enhancing effect was influenced by the concentration of borneol.


Subject(s)
Animals , Benzofurans , Pharmacokinetics , Camphanes , Pharmacokinetics , Pharmacology , Caffeic Acids , Pharmacokinetics , Cinnamates , Pharmacokinetics , Depsides , Pharmacokinetics , Dose-Response Relationship, Drug , Duodenum , Metabolism , Ileum , Metabolism , Intestinal Absorption , Jejunum , Metabolism , Lactates , Pharmacokinetics , Male , Perfusion , Methods , Plants, Medicinal , Chemistry , Rats , Rats, Sprague-Dawley , Salvia miltiorrhiza , Chemistry
18.
Acta Pharmaceutica Sinica ; (12): 652-658, 2010.
Article in Chinese | WPRIM | ID: wpr-354575

ABSTRACT

The aim of the study is to investigate rat intestinal absorption behavior of three main active components, schisandrol A, schisandrin A and schisandrin B in Schisandra chinensis Baill extracts in intestine of rats. With phenol red as the indicator, in situ single pass intestinal perfusion (SPIP) model was used and the concentrations of three main active components in perfusion solution of different intestinal segments (duodenum, jejunum, ileum, and colon) were determined by HPLC in combination with diode array detection. The results showed that the absorption rate constant (Ka) and effective permeability values (Peff) of three main active components in Schisandra chinensis Baill extracts had significant difference (P < 0.05) at different concentrations of perfusion solution, the Ka and Peff first increased and then decreased with the increase of drug concentration, the middle concentration was higher than those of the other two concentrations. The saturate absorption phenomena were observed, and it suggested that the transport mechanisms of three main active components in vivo were similar to active transport or facilitated diffusion. Three active components can be well absorbed in all of the intestinal segments, while duodenum is the best absorption region. The Ka and Peff of three active components in jejunum and ileum had no significant difference (P > 0.05). The absorption of the three active components displayed significant difference (P < 0.05) at different intestinal segments of rats. Schisandrin A had the best absorption in duodenum. The Ka and Peff among three active components were sequenced as follows: schisandrin A > schisandrin B > schisandrol A in other intestinal segments, and there is significant difference (P < 0.05) between them.


Subject(s)
Animals , Chromatography, High Pressure Liquid , Colon , Metabolism , Cyclooctanes , Pharmacokinetics , Dose-Response Relationship, Drug , Drugs, Chinese Herbal , Pharmacokinetics , Duodenum , Metabolism , Fruit , Chemistry , Ileum , Metabolism , Intestinal Absorption , Jejunum , Metabolism , Lignans , Pharmacokinetics , Male , Perfusion , Permeability , Plants, Medicinal , Chemistry , Polycyclic Compounds , Pharmacokinetics , Rats , Rats, Sprague-Dawley , Schisandra , Chemistry
19.
Acta Pharmaceutica Sinica ; (12): 1373-1378, 2010.
Article in Chinese | WPRIM | ID: wpr-353351

ABSTRACT

This study is to investigate the effects of concentration, intestinal section, pH, paracellular route, substrate/inhibitor of enzyme (CYP3A) and proteins (P-gp, MRP2, SGL1) on the absorption of forsythoside A. The absorption of three concentrations (2.6, 5.2, and 10.4 microg x mL(-1)) of forsythoside A in different intestinal segments was studied with phenol red as the marker by rat circulation in situ. The results showed that the residue of forsythoside A with different concentrations had little significant difference from that obtained after perfusing via duodenum, jejunum, ileum and colon, which indicated that the absorption of forsythoside A was passive diffusion and had no difference in different segments of rat intestine. The residue of forsythoside A increased to 466.160 and 463.429 microg respectively when cyclosporine (4 microg x mL(-1)) or midazolam (50 micromol x L(-1)) was added to the circulation fluid, which showed significant difference compared to the control group (P < 0.05). Moreover, the residue of forsythoside A showed a tendency of increase with the increase of cyclosporine or midazolam. When digoxin (50 micromol x L(-1)) or EDTA (10 microg x mL(-1)) was added to the circulation fluid, the residue of forsythoside A decreased to 325.110 and 369.888 microg respectively, which showed significant difference as compared to the control group (P < 0.05). Besides, the residue of forsythoside A showed a tendency of reduction with the increase of digoxin or EDTA. However, there is no significant change in the absorption of forsythoside A when the different concentrations of mannitol were added to the circulation fluid. The results above indicated that the absorption of forsythoside A was mainly passive diffusion and involved paracellular route at the same time. In addition, the substrates of P-gp or CYP3A had dose-dependent effect on the absorption of forsythoside A.


Subject(s)
Animals , Colon , Metabolism , Cyclosporine , Pharmacology , Digoxin , Pharmacology , Dose-Response Relationship, Drug , Duodenum , Metabolism , Edetic Acid , Pharmacology , Glycosides , Pharmacokinetics , Hydrogen-Ion Concentration , Ileum , Metabolism , Intestinal Absorption , Jejunum , Metabolism , Male , Mannitol , Pharmacology , Midazolam , Pharmacology , Rats , Rats, Sprague-Dawley
20.
Acta Pharmaceutica Sinica ; (12): 922-926, 2009.
Article in Chinese | WPRIM | ID: wpr-344018

ABSTRACT

This study investigated the effects of concentration, intestinal section, pH and P-gp on the absorption of daphnetin. The absorptions of three concentrations (10, 20, 40 microg x mL(-1)) of daphnetin in different intestinal segments were studied with phenol red as the marker by in situ rats single pass perfusion model. The results showed that daphnetin was stable under pH 6.0 condition and little affected by metabolism enzyme. There was upgrade tendency between the Peff of duodenum, jejunum, ileum and colon in different concentration of daphnetin, and it has obvious difference between the high concentration and low concentration in jejunum and colon, which indicated that the absorption of daphnetin was passive diffusion and no difference in different segments of rat intestine. However, compared with colon, the absorption of small intestine was better significantly (P < 0.05). Daphnetin may be not a substrate of P-gp as verapamil had not significantly affected the absorption of daphnetin in different intestinal segments of rats.


Subject(s)
ATP Binding Cassette Transporter, Subfamily B, Member 1 , Metabolism , Animals , Female , Hydrogen-Ion Concentration , Intestinal Absorption , Male , Perfusion , Permeability , Rats , Rats, Sprague-Dawley , Umbelliferones , Pharmacokinetics
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