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Nucleotides, nucleosides and nucleobases have been proven as important bioactive compounds related to many physiological processes. Abelmoschus manihot (L.) Medicus from the family of Malvaceae is an annual herbal plant of folk medicine widely distributed in Oceania and Asia. However, up to now, no detailed information could be available for the types and contents of nucleotides, nucleosides and nucleobases contained in A. manihot roots, stems, leaves as well as the flowers. In the present study, an UPLC-TQ-MS/MS method was established for detection of the twelve nucleotides, nucleosides and nucleobases. The validated method was successfully applied to identify the 12 analytes in different parts of A. manihot harvested at ten growth periods. 2′-deoxyinosine was not detected in all of the A. manihot samples. The data demonstrated that the distribution and concentration of the 12 compounds in A. manihot four parts were arranged in a decreasing order as leaf > flower > stem > root. Based on the results, the leaves and flowers of A. manihot could be developed as health products possessed nutraceutical and bioactive properties in the future. This method might also be utilized for the quality control of the A. manihot leaves and other herbal medicines being rich in nucleotides, nucleosides and nulecobases. [ABSTRACT FROM AUTHOR]

A rapid, sensitive, and selective UPLC-TQ-MS/MS method was established and validated for the determination and pharmacokinetic investigation of rhein, coptisine, berberine, palmatine, baicalin and wogonoside from Sanhuang Xiexin Decoction (SXD) extracts. A Waters BEH C 18 UPLC column was used with the mobile phases of Acetonitrile-0.1% formic acid-water. The lower limits of quantification (LLOQ) for rhein, coptisine, berberine, palmatine, baicalin and wogonoside were 24.16, 0.72, 0.68, 0.53, 18.07 and 28.56 ng/mL, respectively. All calibration curves displayed good linearity (r 2 > 0.995). The precision was evaluated by intra-day and inter-day assays and the RSD% were all within 9.12%, and the bias of the accuracies ranged from −7.50% to 8.03%. The recovery ranged from 74.83% to 94.32% and the matrix effects of six analytes were found to be between 90.17% and 103.10%. The stability study showed that compounds were stable during the experiment. Finally, the data showed that the pharmacokinetic (PK) profiles (especially AUC , T max and C max) of six analytes in diabetic rats were significantly diverse from that in normal group rats. The PK study under the pathological condition could provide more helpful information to guide the clinical usage of SXD to treat T2DM. [ABSTRACT FROM AUTHOR]

Kansui, the root of Euphorbia kansui T.N. Liou ex T.P. Wang (Euphorbiaceae), is a well-known poisonous traditional Chinese medicine (TCM). However, many monographs of TCM indicated that it cannot be co-used with licorice, as kansui-licorice is a typical “eighteen incompatible” medicaments. Our previous studies have indicated that kansui was effective in treating malignant pleural effusion (MPE), and the efficacy could be weakened by the co-use of licorice, even causing serious toxicity at the given ratio. Nevertheless, the actual mechanisms of their dosage-toxicity-efficacy relationship need to be well clarified. The present study aimed to investigate the effect of individual and combined use of kansui and licorice on MPE rats, and explain the underlying mechanisms from a metabolomic perspective. Urine samples were analyzed by ultra-high-performance liquid chromatography coupled to quadrupole time-of-flight mass spectrometry (UHPLC-QTOF/MS). Partial least-squares discriminate analysis (PLS-DA) models were built to evaluate the interaction between kansui and licorice. Seven potential biomarkers contribute to the separation of model group and control group were tentatively identified. And selenoamino acid metabolism and nicotinate and nicotinamide metabolism with the impact-value 0.31 and 0.24, respectively, were filtered out as the most important metabolic pathways. Kansui and kansui-licorice at a ratio of 4:1 can treat MPE rats by adjusting abnormal metabolic pathways to the normal state, while it may have opposite result with kansui-licorice 1:4. The different influences to the two metabolic pathways may partially explain the dosage-toxicity-efficacy relationship of kansui-licorice with different ratios. The results could offer valuable insights into the compatibility property changes for the two herbs. [ABSTRACT FROM AUTHOR]

• XXT was eluted into 5 fractions by the macroporous absorption resin separation method. The fingerprints of different fractions were built and main chemical components were identified by UPLC-Q-TOF/MS technology. • The rat model of T2DM was successfully established and applied to assess the efficacy of different fractions from XXT. Results showed that XXT-1 and XXT-2 were the most active fractions. • The bioactive constituents of XXT were screened out by spectrum-effect relationship with grey relational analysis and pearson bivariate correlation analysis. Xiexin Tang (XXT) is a classic prescription for treating diabetes in clinical practices for thousands of years in China, which has been also proved by a large number of modern pharmacological studies. However, due to its complex composition, the bioactive ingredients of XXT is still unclear. In present researches, spectrum-effect relationship analysis is widely used to explore the material basis of traditional medical herbs, so this method was adopted in this study. Firstly, the extract of XXT was separated and enriched into 5 fractions by macroporous adsorption resin. Then, UPLC-Q-TOF/MS method was used for qualitative identification of components in each eluting part, and efficacy of each fraction was assessed by the T2DM rat model. Based on grey relational analysis and pearson bivariate correlation analysis, it was found that the components such as berberine, gallic acid, catechin, epicatechin, acteoside, berberastine and 1-O-galloyl-β-D-glucose might be the main effective basis of XXT to improve T2DM. [ABSTRACT FROM AUTHOR]

Short-chain fatty acids (SCFAs) produced by the intestinal bacteria are very critical for the intestinal barrier, mucosal cytoprotection and normal intestinal biology. However, accumulation of SCFAs promoted by the polysaccharides from Chrysanthemum morifolium Ramat remains unknown. Thus, it is necessary to investigate SCFAs in the colonic contents of dextran sulfate sodium (DSS) induced colitis mice after oral administration of the polysaccharides from C. morifolium Ramat which is very helpful to unravel how it works. In this study, a rapid and reliable gas chromatographic method with flame ionization detector (GC-FID) for simultaneous determination of six SCFAs such as acetic acid (AA), propionic acid (PA), butyric acid (BA), isobutyric acid (IBA), valeric acid (VA) and isovaleric acid (IVA) has been developed and validated. Under the optimized chromatographic conditions and sample extraction procedure, good separation for 6 target compounds was obtained on a HP-INNOWAX column within 12 min. Results revealed that polysaccharides from C. morifolium Ramat positively affected the SCFAs intestinal production. The polysaccharides group had greater SCFAs concentration in colonic content than the DSS-treated group (P < 0.05), which was decreased remarkably compared to the normal group (P < 0.01). With the decrease of the polysaccharides dosage, the contents of AA, PA and VA increased gradually, while the change of BA concentration was the opposite. There was no significant difference in the content of IBA at the different administration concentrations. And the content of IVA reached the highest concentration 0.953 mg/g at lower dose of the polysaccharides. Additionally, oral administration of the polysaccharides prominently attenuated the body weight loss, reduced the disease activity index, rectal bleeding and stool consistency, improved colon shortening and macroscopic score of colitis. Our results indicated that the polysaccharides of C. morifolium Ramat might be used as prebiotic agents to prevent gut dysbiosis and inflammatory bowel disease. [ABSTRACT FROM AUTHOR]

Buddleoside (also known as linarin) as the major flavonoid in Chrysanthemum morifolium Ramat., has been reported to possess a wide range of pharmacological activities. The human intestinal microbiota might have an important impact on drug metabolism and ultimately on the drug oral bioavailability. However, the interaction of the buddleoside with human intestinal bacteria remains unknown. In this study, the conversion of buddleoside by different bacteria from human feces was firstly investigated. A reliable, sensitive and rapid analytical method, ultra performance liquid chromatography was established and successfully applied to investigate the metabolites and metabolic profile of buddleoside by human intestinal bacteria. Among the isolated bacteria, four strains including Escherichia sp. 4, Escherichia sp. 34, Enterococcus sp. 45 and Bacillus sp. 46 showed more powerful conversion capability. Based on the accurate mass data and the characteristic MS n product ions, the parent and six metabolites were detected and tentatively identified compared with blank samples. The metabolites were produced by four main metabolic pathways including deglycosylation, acetylation, methylation and hydroxylation. Buddleoside could be firstly converted to its aglycon acacetin (M2) by the majority of the isolated intestinal bacteria. Subsequently, M2 was further metabolize to its methylated (M3), acetylated (M4), hydroxylated (M5) and hydrogenated product (M6). However, acacetin-7-glucosid (M1) was obtained only from the minor bacterial samples like Bacillus sp. 46. To further explain the metabolism of buddleoside, the β- d -glucosidase and α- l -rhamnosidase activities of four strains were analyzed. Bacillus sp. 46 could only produce α- l -rhamnosidase, while the other three strains showed two kinds of enzyme activities. Furthermore, the activities of α- l -rhamnosidase and β- d -glucosidase reached the highest level at 12–18 h and 10–12 h, respectively. The metabolic routes and metabolites of buddleoside produced by human intestinal microflora were firstly reported in this paper. The results will be very helpful for the further investigation of the pharmacokinetic research of buddleoside and to unravel how it works in vivo . [ABSTRACT FROM AUTHOR]

• Based on the fecal metabolomics, the underlying mechanism of Xiexin Decoction on the amelioration of T2DM by the metabolic activity of gut microbiota was firstly investigated. • The altered endogenous metabolites were closely related to SCFAs-producing and anti-inflammatory gut microflora. • Xiexin Decoction modulated the function of the host gut microbiota in dose-dependent manner. Xiexin Decoction (XXD), a traditional Chinese medicine prescription composed of Rhei rhizome (RR), Scutellaria radix (SR) and Coptidis rhizome (CR), has been used to cure diabetes in clinical practices for thousands of years, but its mechanism is not clear. Our previous study indicated that XXD could significantly ameliorate the symptom of type 2 diabetes mellitus (T2DM) rats by shifting the composition of gut microbiota. However, the effect of XXD on the metabolic activity of gut microbiota is not clarified. In this study, the underlying mechanism of XXD on the amelioration of T2DM was explored by fecal metabolic profiling analysis based on ultra performance liquid chromatography coupled with quadrupole time-of-fight mass spectrometry (UPLC-Q-TOF/MS). The disordered metabolic profiles in T2DM rats were notably improved by XXD. Ten potential biomarkers, which were mainly involved in arachidonic acid metabolism, amino acid metabolism, bile acid metabolism, glycolysis and gluconeogenesis, were identified. Furthermore, these metabolites were closely related to SCFAs-producing and anti-inflammatory gut microflora. After XXD intervention, these biomarkers restored to the normal level at some extent. This study not only revealed potential biomarkers and related pathways in T2DM rats affected by XXD, but also provided a novel insight to uncover how traditional herb medicines worked from fecal metabolomics. [ABSTRACT FROM AUTHOR]