Bioactive flavonoids in medicinal plants:Structure, activity and biological fate

Flavonoids, a class of polyphenol secondary metabolites, are presented broadly in plants and diets. They are believed to have various bioactive effects including anti-viral, antiinflammatory, cardioprotective, anti-diabetic, anti-cancer, anti-aging, etc. Their basic structures consist of C_6—C_3—C_6 rings with different substitution patterns to produce a series of subclass compounds, and correlations between chemical structures and bioactivities have been studied before. Given their poor bioavailability, however, information about associations between structure and biological fate is limited and urgently needed. This review therefore attempts to bring some order into relationships between structure, activity as well as pharmacokinetics of bioactive flavonoids.

Quantitative analysis of a novel antimicrobial peptide in rat plasma by ultra performance liquid chromatography-tandem mass spectrometry

We described the first results of a quantitative ultra performance liquid chromatographytandem mass spectrometry method for a novel antimicrobial peptide （phylloseptin, PSN-1）. Chromatographic separation was accomplished on a Waters bridged ethyl hybrid （BEH） C18 （50mm× 2.1 mm, 1.7 μm） column with acetonitrile-water （25：75, v/v） as isocratic mobile phase. Mass spectrometry detection was performed in the positive electrospray ionization mode and by monitoring of the transitions at m/z 679.6/120, 509.6/120 （PSN-1） and m/z 340.7/165 （Thymopentin, IS）. Protein precipitation was investigated and the recovery was satisfactory （above 82%）. The method was shown to be reproducible and reliable with intra-day precision below 5.3%, inter-day precision below 14.2%, and linear range from 0.02 to 2 lag/mL with r〉0.994. The method was successfully applied to a pharmacokinetic study of PSN-1 in rats after intravenous administration.

Development of the fingerprints for the quality evaluation of Viscum coloratum by high performance liquid chromatography

A high-performance liquid chromatography coupled ultraviolet （HPLC-UV） method was developed for a chemical fingerprint analysis of Viscum coloratura. Eighteen peaks were selected as the common peaks and Homoeriodictyol-7-O-β-D-apiosiyl-（1→2）-β-D-glucoside was used as a reference. The relative areas of common peaks were used for hierarchical clustering analysis and similarity calculation. Thirty-seven samples collected from different sources were classified into five groups. The similarities of 21 batches Viscum coloratura samples were beyond 0.90. The results obtained suggest that the chromatographic fingerprint can efficiently identify Viscum coloratum. Additionally, the fingerprints can then be used to evaluate the correlation between Viscum coloratura and hosts.

Authentication and distinction of Shenmai injection with HPLC fingerprint analysis assisted by pattern recognition techniques

In this paper, the feasibility and advantages of employing high performance liquid chromatographic （HPLC） fingerprints combined with pattern recognition techniques for quality control of Shenmai injection were investigated and demonstrated. The Similarity Evaluation System was employed to evaluate the similarities of samples of Shenmai injection, and the HPLC generated chromatographic data were analyzed using hierarchical clustering analysis （HCA） and soft independent modeling of class analogy （SIMCA）. Consistent results were obtained to show that the authentic samples and the blended samples were successfully classified by SIMCA, which could be applied to accurate discrimination and quality control of Shenmai injection. Furthermore, samples could also be grouped in accordance with manufacturers. Our results revealed that the developed method has potential perspective for the original discrimination and quality control of Shenmai injection.

Simultaneous determination of four active components in Alisma orientale (Sam.) Juz. by HPLC–DAD using a single reference standard

A rapid, simple and practical high-performance liquid chromatography method coupled with diode array detector（HPLC–DAD） was developed to evaluate the quality of Alisma orientale（Sam.） Juz.through a simultaneous determination of four major active triterpenes using a single standard to determine the multi-components（SSDMCs）. Alisol B 23-acetate was selected as the reference compound for calculating the relative response factors. All calibration curves showed good linearity（R240.9998） within test ranges. RSDs for intra- and inter-day of four analytes were less than 3.6% and 2.3%; the overall recovery was 92.1–110.2%（SSDMC）. The proposed method was successfully applied to quantify the four components in 20 samples from different localities in China. Moreover, significant variations were demonstrated in the content of these compounds. In addition, hierarchical clustering analysis（HCA） and principal components analysis（PCA） were performed to differentiate and classify the samples based on the contents of Alisol C 23-acetate, Alisol A, Alisol A 24-acetate and Alisol B 23-acetate. This simple,rapid, low-cost and reliable HPLC–DAD method using SSDMC is suitable for routine quantitative analysis and quality control of A. orientale（Sam.） Juz.

Study on changes of polyamine levels in mice with the development of U14 cervical cancer

This study was performed to investigate the possible involvement of polyamincs in the development of cervical cancer. The objective of the present study was therefore to lind the specilic polyamine indicators, which could be used as useful markers for the early determination of cervical cancer. A simple method for the simultaneous determination of plasma concentrations ol live polyamines in normal and UI4 model mice was developed by using HPLC-MS. The samples were derivatized by benzoyl chloride. The derived polyamines were separated on a C18 colunm by a gradient elution with methanol water, and then detected with HPLC-MS. The results showed tha! all polyamine levels in the U 14 model mice were higher than those in normal ones. Thc cadaverine. putrescine and 1,3-diaminopropane levels were significantly higher in U 14 model mice plasma than those in normal mice plasma, especially the putrescine and 1, 3-diaminopropane （P〈0.01）. The cadaverine, putrescine and 1, 3-diaminopropane levels were significantly higher in U 14 mice model urine than those in normal mice urine, especially the cadaverine and 1, 3-diaminopropane （P〈0.01）. Putrescine, cadaverine and I, 3-diaminopropane might be the indicators of the cervical cancer.

Quantitative Evaluation of the Compatibility Effects of Aidi Injection on the Treatment of Hepatocellular Carcinoma Using Targeted Metabolomics:A New Strategy on the Mechanism Study of an Anticancer Compound in Traditional Chinese Medicine

Objective:Compound traditional Chinese medicine(CTCM)with the application of compatibility from multiple active ingredients with multiple-specific targets can achieve a synergistic effect on cancer therapy.This study is aimed to observe the compatibility effects of Aidi injection on the treatment of hepatocellular carcinoma and to explore the mechanism of CTCM.Methods:Aidi injection is a clinical compound prescription containing Mylabris,Ginseng,Astragalus,and Acanthopanax,which can inhibit tumor growth and induce apoptosis.In this study,the anticancer activity of Aidi injection,as well as its disassembled and combined compositions,had been evaluated by varying levels of polyamine biomarkers on human hepatoma Hep-G2 cells detected using ultrahigh-performance liquid chromatography-tandem mass spectrometry.Results:According to the different variations in polyamine levels,it was revealed that Mylabris and Ginseng had an antitumor effect,while Astragalus acted as an assistant and Acanthopanax had weak anticancer activity.The increased level of polyamines in Hep-G2 cells had been found in HL-7702 cells.On combining Mylabris and Ginseng,polyamine levels went close to the normal level,which was even more marked when Astragalus was added.Aidi injection acted like the combination of Mylabris,Ginseng,and Astragalus.Conclusions:This study established a quantitative evaluation of the compatibility effects of Aidi injection based on polyamine biomarkers and evaluated the consistency of its anticancer effect,providing a manner to research the efficacy evaluation of CTCM.Moreover,the correlation between polyamine metabolism and anticancer activity can be used in anticancer drug screening.

A novel norsesquiterpene alkaloid from the mushroom-forming fungus Flammulina velutipes

A new norsesquiterpe alkaloid （1） was isolated from the solid culture of mushroom-forming fungus Flammulina velutipes fermented on rice. The structure of I was elucidated by spectroscopic methods. The absolute configuration of C-1 in 1 was determined using the circular dichroism data of their [Rh2（OCOCF3）4] complex.