A new phloroglucinol compound from Dryopteris fragrans / 中国中药杂志

Two phloroglucinol compounds(1-2) were isolated and purified from 95% ethanol extract of Dryopteris fragrans through various column chromatographies on silica gel, Sephadex LH-20, medium pressure column chromatography, and preparative HPLC. Their structures were elucidated as 2',4',6'-trihydroxy-5'-methyl acetate-3'-methyl-1'-butyrophenone(1) and aspidinol B(2) based on their chemical and physicochemical methods and spectroscopic data. Compound 1 is a new phloroglucinol compound named "dryofraginol".

Analysis of Effective Substance of Qingre Chushi Decoction by UPLC-Q-TOF-MS / 中国实验方剂学杂志

Objective:To characterize and compare the chemical information of four extracts of Qingre Chushi (QRCS) decoction by liquid chromatography-mass spectrometry (LC-MS), and combine the chemical information of the four extracts with their results of anti-inflammatory effect for a multivariate statistical analysis, in order to identify the compounds directly relating to the anti-inflammatory effects of QRCS decoction. Method:Four extracts of QRCS decoction were characterized by UPLC-Q-TOF-MS:①ethanol extract+water extract,② ethanol extract+supernatant after water extraction and alcohol precipitation, ③ ethanol extract+precipitation after water extraction and alcohol precipitation,and ④ standard decoction. On the basis of the results of inhibition of the four above extracts on xylene-induced ear swelling in mice,multivariate statistical analysis[principal component analysis (PCA) and orthogonal partial least squares-discriminant analysis (OPLS-DA)] were carried out to lock the chromatographic peaks with significant differences between group ① (the best pharmacological action group) and group ④ (standard decoction group). According to the accuracy of quasi-molecular ion and fragment ion data,and the reference materials and literature data,those chromatographic peaks were identified. Result:PCA could cluster the four extracts of QRCS decoction,and the differences between groups was reflected in the distance between groups. Group ④ (standard decoction) had the most significant differences with the other three groups, especially in the first principal component; group ① (ethanol extract+water extract),group ② (ethanol extract+supernatant after water extraction and ethanol precipitation) and group ③ (ethanol extract+precipitation after water extraction and ethanol precipitation) had certain differences in the second principal component. OPLS-DA was used to compare group ① (the best pharmacological action group) and group ④ (standard decoction group). Eleven chromatographic peaks with great contribution and high reliability to group differences,were identified as gentiopicrin,skimmin,baicalin,baicalin isomer,wogonoside,5,6,7-trihydroxy-8-methoxyflavone-7-O-glucurodonaldehyde,5,6-dihydroxy-6,8,2',3'-tetramethoxyflavone,salicin-6-C-arabinose-8-C-glucoside,plantamajoside and glycyrrhizic acid. Conclusion:In the mode of pectrum-effect combination, this study explores and identifies compounds relating to the anti-inflammatory effect of QRCS decoction,so as to provide the basis for screening the extraction and purification process and optimizing the formulation of preparation of Qingre Chushi decoction.

Quality Control of Realgar in Compound Huanglian Ointment / 中国中医药信息杂志

Objective To control the quality of realgar in compound Huanglian Ointment.Methods As2O3which is the toxic component of realgar was carried limit test by Gutzeit's test; Potassium sulfate, ammonium sulfate and sulfuric acid were used to digest, and then titration method was used to determine the content of As2S2in compound Huanglian Ointment. Results The content of the soluble As in compound Huanglian Ointment was no higher than 15.6 μg/g. The content of As2S2in compound Huanglian Ointment was no less than 2.21 mg/g. Conclusion The method is simple and easy,which can be applied as the quantity control method of compound Huanglian Ointment.

Preparation and physicochemical characterization of T-OA PLGA microspheres / 中国天然药物

As the carrier of water-insoluble drugs, microspheres can play a role in increasing solubility and delaying releasing essence. The objective of this study was to improve the solubility and to delay the release of a newly discovered antitumor compound 3β-hydroxyolea-12-en-28-oic acid-3, 5, 6-trimethylpyrazin-2-methyl ester (T-OA). Early-stage preparation discovery concept (EPDC) was employed in the present study. The preparation, physicochemical characterization, and drug release properties of PLGA microspheres were evaluated. T-OA-loaded PLGA microspheres were prepared by an oil-in-water (O/W) emulsification solvent evaporation method. Characterization and release behaviors of the T-OA PLGA microspheres were evaluated by X-ray diffract (XRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), and high performance liquid chromatography (HPLC). The results demonstrated that T-OA-loaded PLGA microspheres could be successfully obtained through solvent evaporation method with appropriate morphologic characteristics and high encapsulation efficiency. The XRD analysis showed that T-OA would be either molecularly dispersed in the polymer or distributed in an amorphous form. The DSC and FTIR analysis proved that there were interactions between T-OA and PLGA polymer. SEM observations displayed the morphology of the microspheres was homogeneous and the majority of the spheres ranged between 50 and 150 μm. The drug release behavior of the microspheres in the phosphate buffered saline medium exhibited a sustained release and the duration of the release lasted for more than 23 days, which was fit with zero-order release pattern with r = 0.9947. In conclusion, TOA-loaded PLGA microspheres might hold great promise for using as a drug-delivery system in biomedical applications.

Analysis of digital gene expression profiles of the cultivated Polygala tenuifolia in different phenological phases / 药学学报

The content changes of chemical components in different phenological phase of the cultivated Polygala tenuifolia is one of the important factors for determination of the best harvest time in the production practice. In this study, the digital gene expression (DGE) profiles of the cultivated P. tenuifolia were analyzed in different phenological phase (flowering fruit bearing stage, wilting stage, dormancy stage). The differentially expressed genes were found in the biosynthesis of chemical composition in P. tenuifolia, and the representational ones were validated by RT-qPCR. Then, the key enzymes (CYP450s and UGTs) involved in the downstream of the triterpenoid saponins biosynthesis pathway in P. tenuifolia were predicted through the correlation analysis of gene expression. The number of down-regulated genes was more than that of up-regulated in P. tenuifolia from flowering fruit bearing stage to dormancy stage. Six differentially expressed genes (HMGS, PMK, FPPS, SQS, SE, β-AS) and five (PAL, C4H, 4CL, CAD, peroxidase) were annotated to the triterpenoid saponins and phenylpropanoid biosynthesis pathway in P. tenuifolia, respectively. Compared to wilting and dormancy stages, the saponins, xanthones, and lignins were largely synthesized at the flowering fruit bearing stage of P. tenuifolia. Furthermore, UGT83A1, CYP716B1, CYP98A3, CYP86B1, and CYP94A1 may be the part of key enzymes in the downstream of the triterpenoid saponins biosynthesis pathway in P. tenuifolia. This study provides evidence to support the correctness of traditional harvest time of P. tenuifolia at the level of transcription, and lays the scientific foundation for gene cloning and functional verification of CYP450s and UGTs in the downstream of the triterpenoid saponins biosynthesis pathway in P. tenuifolia in the future.

UPLC/Q-TOF MS and NMR plant metabolomics approach in studying the effect of growth year on the quality of Polygala tenuifolia / 药学学报

Growth year is one of the important factors for the quality of Polygala tenufolia. In this study, primary metabolites and secondary metabolites were compared in 1, 2 and 3 years old P. tenufolia cultivated in Shaanxi Heyang. The samples were subjected to ultra-high performance liquid chromatography (UPLC)-quadrupole time-of-flight mass spectrometry (Q-TOF MS) and nuclear magnetic resonance (NMR) analysis, and the obtained data were analyzed using principal component analysis (PCA) and other statistical analysis methods. In addition, content and correlation of different metabolites were also calculated. The results showed no significance between main component contents in 2 year-old and 3 year-old P. Tenufolia, but 1 year-old was statistically different. The contents of primary metabolites, such as fructose, sucrose, and choline increased as time goes on, while glycine and raffinose decreased. The contents of secondary metabolites, such as onjisaponin Fg, polygalasaponin XXVIII, polygalasaponin XXXII increased, while polygalaxanthone III and parts of oligosaccharide multi-ester including tenuifoliose A, tenuifoliose C, tenuifoliose C2 and tenuifoliose H decreased with the extension of the growth years. Growth years has important impact on the quality of P. tenuifolia and the existing growing years of commodity P. tenuifolia have its scientific evidence. This study supplied a new method for the quality evaluation of Chinese medicinal materials.