Supervisor(s):Chinese Pharmaceutical Association Sponsor(s):Tianjin Institute of Pharmaceutical Research；Chinese Pharmaceutical Association ISSN:0253-2670 CN:12-1108/R
Chinese Traditional and Herbal Drugs is supervised by Chinese Pharmaceutical Association and sponsored by Tianjin Institute of Pharmaceutical Research and Chinese Pharmaceutical Association. Launched in 1970, the journal is an academic journal with a broad scope in publishing research papers, brief reports, reviews, dissertations, and special treatises on the recent achievements of basic study, production, quality control, and clinic application on traditional Chinese medicine and Chinese materia medica.
The journal is included in CA, JST and CSCD.
Objective To develop a method for simultaneous determination of several triterpenic acids in Jujubae Fructus and provide the technical support for the quality control of Jujubae Fructus. Methods Betulinic acid was used as the internal reference substance, and the relative correlation factors (RCF) of oleanolic acid, ursolic acid, betulonic acid, oleanonic acid, and ursonic acid were determined by HPLC-ELSD. The contents of the five components were calculated according to the RCF, respectively. The contents of these six triterpene acids in 15 batches of Jujubae Fructus were determined by the external standard method. The rationality, feasibility, and repeatability for the method of quantitative analysis of multi-components by single-marker (QAMS) were verified by comparing with the results obtained from the external standard method. Results The reproducibility of the RCF was acceptable. For the six triterpene acids, there was no significant difference between the quantitative results with the two different methods in the 15 batches of Jujubae Fructus. Conclusion The method established in this research is accurate and feasible that it just needs to assay single-marker (betulinic acid) for determination of six triterpenic acids in Jujubae Fructus simultaneously. Therefore, this method is helpful for quality control of Jujubae Fructus and can provide a new reference for quality assess of multi components in Chinese materia medica.
Objective Taking luteolin-7-O-β-D-glucuronide, rosmarinic acid, and tilianin as indicators, the concentrations of extract from Dracocephalum moldavica (EDM) and the indicator components in various solvents and surfactant solutions, and apparent oil/water partition coefficient (P) at different pH values were detected. Then, the stability of EDM in artificial gastrointestinal fluid was investigated. This research would give the reference for selection and preparation of further novel formulation. Methods Apparent solubilities of EDM in various solvents and surfactant solutions were determined by precipitation method, the shake-flask method was used to determine the P value of EDM in octanol–water/phosphate buffer, and the stability of EDM in artificial gastrointestinal fluid was investigated. HPLC was adopted to determine the concentration of the indicator components, with Shim-pack ODS column (250 mm × 4.6 mm, 5 μm), mobile phase of acetonitrile (A)–0.5% formic acid aqueous solution (B) for gradient elution (0–30 min, 15% A; 30–55 min, 15%→25% A; 55–80 min, 25%→35% A) as mobile phase at flow rate of 1.0 mL/min. The detection wavelength was set at 324 nm and the column temperature was maintained at 35 °C. Results At 37 °C, the equilibrium solubilities of the three indicator components decreased obviously in acid buffer, but gradually increased in alkaline buffer. In 32 g/L sodium dodecyl sulfate solution, the equilibrium solubilities of luteolin-7-O-β-D-glucuronide, rosmarinic acid, and tilianin increased to 1 679.61, 1 249.20, and 2 765.27 μg/mL. The P values of luteolin-7-O-β-D-glucuronide, rosmarinic acid, and tilianin were 0.173 1 (lgP = −0.761 8), 0.068 4 (lgP = −1.165 0), and 1.082 9 (lgP = 0.034 6), and increased with the increase of pH value. The three components were stable in artificial intestinal fluid, and rosmarinic acid, and tilianin were stable in artificial gastric fluid. Conclusions The method can be used to determine the apparent solubilities and P values of the extract and the indicator components. The EDM in artificial gastrointestinal fluid is stable. The research will give reference for selection and preparation of the further novel formulation.
Objective To optimize the extracting and processing conditions of Compound Jianshen Granules (CJG). Methods Ultraviolet analytical methods of total saponin and total polysaccharides were established. The optimal ethanol extraction process and water extraction process were confirmed according to single factor and orthogonal design tests. The influences of different excipients and wetting agents were investigated, taking forming rate, solubility, and hygroscopic rate as indexes, the materials added prescription varieties, ratio, and optimum molding process were screened. Results The optimal ethanol extraction technology of CJG was: using 10-fold amount of 85% ethanol, extracting for three times, 2 h each time. The optimal water extraction technology was using 14-fold amount of water, decocting 3 times, 30 min each time. The optimized conditions of CJG were obtained with accessories ratio for dextrin: lactose (4:1), and the ratio of extract powder to accessories (1:1), with 85% ethanol as wetting agent which accounted for 15% of the main drug. Conclusion The established extraction process and forming process are feasible and stable, and the quality is controllable.
Objective To study the effects and mechanisms of p-glycoprotein (P-gp) inhibitor and MRP1 inhibitor on the transportation of gastrodin (GAS). Methods Cell toxicity of GAS was detected by MTT assay, molecular Docking was employed to predicted binding mode and effect ability of GAS with P-gp and MRP1. MDCK-MDR1 cell model was employed to study the influences of Ver, a P-gp inhibitor, and Probenecid, a MRP1 inhibitor, on the transportation of GAS. Results There was no cell cytotoxicity of GAS between the concentration of 100 to 1 000 μg/mL. There was hydrogen-bond and hydrophobic interaction between P-gp and GAS, and hydrogen-bond, hydrophobic interaction and electrostatic-interaction between MRP1 and GAS. Lib Dock Score indicated that both P-gp-verapamil (Ver) and MRP1-Probenecid were more stable than P-gp-GAS and MRP1-GAS. The Papp of GAS BL→AP was greater than that of AP→BL, Efflux ratio (ER) of GAS was about 1.5, which indicated the efflux pump protein might involve the transportation of GAS. The Papp of GAS was significant increased but the ER of GAS was significant decreased when co-administrated with Ver (P < 0.05). The Papp of GAS was slightly increased and the ER of GAS was slightly decreased when co-administrated with Probenecid, while there was no significance. Conclusion The results indicate that GAS is the substrate of P-gp. However, whether GAS is the substrate of MRP1 needs further research. Both Ver and Probenecid could enhance the transportation of GAS by competitive binding with P-gp and MRP1.
Objective Optimization of ginkgolides components (GC) self-microemulsifying drug delivery system (SMDDS) (GC-SMDDS) and similarity analysis on each drug release. Methods Using equilibrium solubility to screen the oil phase, emulsifier, and co-emulsifier; Taking appearance, the proportion of microemulsion particle size, Zeta potential, surfactants and co-surfactants, and surfactant mixing ratio of the oil phase as study factors, pseudo-ternary phase diagrams were used to screen the GC-SMDDS process. The SMEDDS of drug loading, particle size distribution, Zeta potential, and stability were evaluated. With the aid of the similarity factor and the curve linear regression slope analysis, the similarity between the composition of the component and the rate and extent of drug release was analyzed. Results Optimal prescription of polyoxyethylene and polyethylene glycol 200 mass ratio of 4:1, ethoxylates and polyethylene glycol quality and bitterness total mass of 200 capric triglycerides ratio of 9:1, drug content of 100 mg/g. Particle size under 40 nm, ginkgolides 48 h internal components from microemulsion to room temperature, high temperature, and low temperature stability is good. The release quantity achieves the synchronous drug release with the similarity of 96.9%. Conclusion The SMDDS not only can improve the dissolution of difficult soluble drugs, but also independently regulate the drug release behavior of each component so as to make the drug release maintain good consistency.
Objective To investigate the protective effect and the mechanism of loganin (an active component in Cornus officinalis) on the endoplasmic reticulum (ER) stress of glomerular mesangial cells (GMCs) induced by advanced glycation end products (AGEs). Methods Human GMCs were cultured in vitro and divided into control group, model group (AGEs group), loganin group, and amino guanidine group (set as positive control, 0.1, 1.0, and 10.0 μmol/L). After being incubated with loganin (final concentration of 0.1, 1.0, and 10.0 μmol/L) for 1 h, GMCs were stimulated by AGEs (200 mg/L) for 24 h. Then, the cell proliferation was measured of using MTS method. PGE2 was investigated by ELISA. Receptors of advanced glycation end products (RAGE), and ER stress-related protein like GRP78, IRE1, XBP1, and inflammatory factor NF-κB and COX-2 in GMCs were detected by Western blotting. Results Loganin could suppress the proliferation of GMCs induced by AGEs, alleviate the subcellular injury of GMCs, down-regulate the expression of ER stress-related protein GRP78, IRE1, XBP1, and RAGE, reduce the inflammation-related protein NF-κB, COX-2, and the level of PGE2. Conclusion Loganin could alleviate the ER stress of GMCs induced by AGEs, and lessen the inflammation and subcellular injury of GMCs. Its mechanism might be related to the decreased expression of RAGE and the inhibition of the IRE1 pathway.
Objective To study the chemical constituents of Lonicerae Japonicae Caulis produced in Shandong Province. Methods Compounds were isolated and purified by repeated column chromatographies including silica gel, MCI-gel resin, Sephadex LH-20, and so on. Their structures were elucidated by spectral data, including extensive 1D and 2D NMR techniques. Results Four compounds were obtained and identified as 11,14,15-trihydroxy-12-octadecenoic acid methyl ester (1), ochnaflavone (2), β-daucosterol (3), and loganin (4). Conclusion Compound 1 is a new organic acid named as loniceric acid ester, and compound 2 is isolated from Lonicerae Japonicae Caulis for the first time.
Objective Comparing the quality among five species of Angelicae Radix(Danggui) samples, i.e. Chinese Danggui (CDG, the roots of Angelica sinensis), Japanese Danggui (JDG, the roots of A. acutiloba), Korean Danggui (KDG, the roots of A. gigas), Lovage root (LR, the roots of Levisticum officinale), and Angelica archangelica root (AAR, the roots of A. archangelica) by evaluating the contents of their bioactive components. Methods The 3,5-dinitrosalicylic acid colorimetric method (DNS method) was developed to quantify the amount of polysaccharides in a total of 46 species of Angelicae Radix collected from different countries based on the optimization of sampling, comparing the differences of polysaccharide among various species of Angelicae Radix, etc. Results The contents of polysaccharides were found to be significantly different among the five species of Angelicae Radix. The order from high to low amount was AAR (162.5 mg/g, n = 9), LR (142.3 mg/g, n = 4), JDG (126.8 mg/g, n = 13), KDG (126.8 mg/g, n = 13), and CDG (80.75 mg/g, n = 12). For JDG sample, the contents of polysaccharide were significant variety among samples cultivated in Japan (131.37 mg/g, n = 3), China (184.29 mg/g, n = 4), and Korea (94.98 mg/g, n = 4). Conclusion The developed DNS method is suitable to accurately quantify the amount of polysaccharide in Angelicae Radix. The pharmaceutical efficacy is variety among the five Angelicae Radix resulting from the various contents of polysaccharide. These herbs can not be mixed or substituted in clinical use.
