A mathematical model for quality evaluation of total saponins of Panax japonicas based on hypolipidemic activity / 中草药·英文版

Objective: The chemical finger printing-based methods for evaluating TCMs quality can report partial of TCMs quality without linking to effective constituents. In this study, a mathematical model was established for the quality evaluation of total saponins of Panax japonicus (TSPJ), a folk medicine in China and Japan for treating diseases, through coupling the dynamic changes of chemical constitutions with corresponding activities. Methods: High-performance liquid chromatography (HPLC) fingerprints were applied to establish the chromatographic database of TSPJ. The associated hypolipidemic activity database was determined by TG assay using HepG2 cell model. Correlation analyses of two databases were performed by partial least squares (PLS) for calculating regression coefficients, and the interval value of YZL value (the ratio of positive and negative peak-to-peak area coefficient) closely related to hypolipidemic activity was refined by the formula of Norminv function to value the quality of TSPJ. Results: In this study, the chromatographic data of 16 common peaks were obtained from 20 batches of TSPJ. After the estimate by this mathematical evaluation model, seven peaks were positively correlated with hypolipidemic activity, and nine peaks were negatively correlated with hypolipidemic activity. When the YZL value was less than 0.7861, the quality of sample was inferior, while YZL value was more than 6.6992, and the quality of samples was superior. The quality of another ten batches of TSPJ was further assessed to verify this method. Conclusion: These results indicated that the established model could be usefully applied to evaluate the quality of TSPJ in the hypolipidemic activity.

Advance in glycosyltransferases, the important bioparts for production of diversified ginsenosides / 中国天然药物

Ginsenosides are a series of glycosylated triterpenoids predominantly originated from Panax species with multiple pharmacological activities such as anti-aging, mediatory effect on the immune system and the nervous system. During the biosynthesis of ginsenosides, glycosyltransferases play essential roles by transferring various sugar moieties to the sapogenins in contributing to form structure and bioactivity diversified ginsenosides, which makes them important bioparts for synthetic biology-based production of these valuable ginsenosides. In this review, we summarized the functional elucidated glycosyltransferases responsible for ginsenoside biosynthesis, the advance in the protein engineering of UDP-glycosyltransferases (UGTs) and their application with the aim to provide in-depth understanding on ginsenoside-related UGTs for the production of rare ginsenosides applying synthetic biology-based microbial cell factories in the future.

Anti-inflammatory effect of the compounds from the flowers of Trollius chinensis

In order to investigate the anti-inflammatory activity of flavonoids, phenolic acids, and alkaloids from the flowers of Trollius chinensis, some representative compounds, namely, orientin, 2"-O-Beta-L-galactopyranosylorientin, vitexin, quercetin, isoquercetin, luteolin, veratric acid, proglobeflowery acid, trollioside, and trolline were selected to study their inhibitory effects against LPS-induced NO, IL-6, and TNF-Alpha release in RAW264.7 cells. At the higher concentration, both phenolic acids and flavonoids inhibited the production of NO, whereas only phenolic acids showed this effect at the lower concentration. Although trolline had stronger cytotoxicity, it exhibited a potential effect of decreasing NO production induced by LPS in the non-toxic concentration range. In addition, all tested compounds ecreased the production of IL-6 and TNF-Alpha by almost 50% at both the higher and lower concentrations. It is concluded that the anti-inflammatory activity of the phenolic acids is stronger than that of the flavonoids

Prediction of Antiviral and Anti-inflammatory Mechanisms of Major Compounds from Flowers of Trollius Chinensis Based on Molecular Docking Technology / 中国中医药信息杂志

Objective To predict the antiviral and anti-inflammatory mechanisms of major compounds from the flowers of Trollius chinensis, namely, vitexin, orientin, 2"-O-β-L-galactopyranosylvitexin, 2"-O-β-L-galactopyranosylorientin, veratric acid, and trolline, by using the molecular docking technique. Methods Discovery Studio 2.5 software and Chinese Medicine Chemistry Database were employed for docking between the ligands including 6 compounds and the proteins including Toll-like receptors (TLRs) and neuraminidase (NA). The docking results and interactions of their functional domains were obtained by simulation analysis. Results Vitexin, orientin, 2"-O-β-L-galactopyranosylvitexin, veratric acid, and trolline were applied to one or more TLR, whereas 2"-O-β-L-galactopyranosylorientin could interact with neither of the proteins investigated. Flavonoids, namely vitexin, orientin, 2"-O-β-L-galactopyranosylvitexin and 2"-O-β-L-galactopyranosylorientin were applied to NA, whereas veratric acid and trolline could not interact with NA. Conclusion Five out of the 6 compounds have influence on the signaling pathways mediated by TLRs, and TLR3, 4, and 7 are their potential targets for antivirus and anti-inflammation. Four flavonoids can affect the activity of influenza virus by interacting with NA. This study can provide a basis for the investigation of the antiviral and anti-inflammatory effective compounds of the flowers of Trollius chinensis and the further development.

Transformation of trollioside and isoquercetin by human intestinal flora in vitro / 中国天然药物

The present study was designed to determine the intestinal bacterial metabolites of trollioside and isoquercetin and their antibacterial activities. A systematic in vitro biotransformation investigation on trollioside and isoquercetin, including metabolite identification, metabolic pathway deduction, and time course, was accomplished using a human intestinal bacterial model. The metabolites were analyzed and identified by HPLC and HPLC-MS. The antibacterial activities of trollioside, isoquercetin, and their metabolites were evaluated using the broth microdilution method with berberine as a positive control, and their potency was measured as minimal inhibitory concentration (MIC). Our results indicated that trollioside and isoquercetin were metabolized by human intestinal flora through O-deglycosylation, yielding aglycones proglobeflowery acid and quercetin, respectively The antibacterial activities of both metabolites were more potent than that of their parent compounds. In conclusion, trollioside and isoquercetin are totally and rapidly transformed by human intestinal bacteria in vitro and the transformation favors the improvement of the antibacterial activities of the parent compounds.

Pharmacokinetics and tissue distributions of veratric acid after intravenous administration in rats / 中国天然药物

The present study was designed to investigate the pharmacokinetics and tissue distributions of veratric acid following intravenous administration in rats. The concentrations of veratric acid in rat plasma at various times after administrated at doses of 2.5, 5, and 10 mg·kg(-1) were quantified by HPLC. The tissue distributions of veratric acid at various times after a single intravenous dose of 2.5 mg·kg(-1) were also analyzed. The plasma pharmacokinetic parameters at the three doses were as follows: t(1/2), (86.23 ± 6.83), (72.66 ± 4.10) and (71.20 ± 2.90) min; C0, (11.10 ± 1.47), (23.67 ± 1.24) and (39.17 ± 3.90) μg·mL(-1); and AUC(0→∞), (1 240.90 ± 129.14), (2 273.84 ± 132.47) and (3 516.4 ± 403.37) min·μg·mL(-1), respectively. The compound was distributed into tissues rapidly and extensively after intravenous administration and was mainly distributed into the liver, heart and kidneys.

Structure and biological action on cardiovascular systems of saponins from Panax notoginseng / 中国中药杂志

Notoginseng Radix et Rhizoma (Sanqi), the underground part of Panax notoginseng (Burk.) F. H. Chen (Araliaceae) is commonly used in Chinese medicine for treatment of haemorrhage, haemostasis, swelling, etc. The aerial part including leaves, flowers and fruits are also applied for similar functions. Triterpenoid saponins are considered to be responsible for the biological activities of Sanqi. Up to date, more than 100 saponins have been isolated from theroots, rhizomes, leaves, flowers and fruits of P. notoginseng. The reported saponins can be classified into protopanaxadiol (PPD), protopanaxatriol (PPT), C17 side-chain varied and other types, according to the skeletons of the aglycons. The present review summarizes the saponins isolated from P. notoginseng and their distribution in different medicinal organs, as well as the pharmacological actions on cardiovascular system.

Absorption properties and mechanism of trolline and veratric acid and their implication to an evaluation of the effective components of the flowers of Trollius chinensis / 中国天然药物

AIM@#To study the absorption properties and mechanism of two important components, trolline and veratric acid, from the flowers of Trollius chinensis, in order to better understand the contribution of these two compounds to the effectiveness of these flowers.@*METHOD@#The human Caco-2 cell monolayer model was employed to study the transport of trolline and veratric acid from apical side (AP) to basal side (BL), and from BL to AP by determining the transport rates as the function of time and concentration and calculating apparent permeability coefficients (Papp).@*RESULTS@#Trolline and veratric acid were transported across Caco-2 cell monolayer through different mechanisms in a concentration dependent manner. Trolline was transported at a Papp level of 10(-6) cm·s(-1) with a Papp AP→BL/Papp BL→AP ratio of more than 1.8 or less than 0.8, while veratric acid was transported at a Papp level of 10(-5)cm·s(-1) with a Papp AP→BL/Papp BL→AP ratio of close to 1.0.@*CONCLUSION@#Trolline is moderately absorbed through an associative mechanism involving active and passive transport, and veratric acid is well-absorbed mainly through passive diffusion. These factors should be taken into account when chemically assessing the pharmacodynamic material basis of the flowers of T. chinensis.

Contribution evaluation of the floral parts to orientin and vitexin concentrations in the flowers of Trollius chinensis / 中国天然药物

AIM@#To provide a comprehensive procedure to evaluate the contribution of the floral parts to the yield of the major components from the flowers of Trollius chinensis, to underlay the selective breeding, cultivation, development, and utilization of the flowers.@*METHODS@#Five floral parts from eleven batches of the flowers of T. chinensis were examined by HPLC analysis for the content of orientin and vitexin, and by gravimetric analysis for their respective mass fraction. The contribution of each floral part was calculated using mathematical methods based on the results of the content and mass fraction. Variance analysis was carried out by Kruskal-Wallis H test and PCA method.@*RESULTS@#The calculated mean contributions of calyx, corolla, stamens and pistils, stalk, and ovary to the yield of both orientin and vitexin were 76.99% and 71.93%, 9.60% and 8.33%, 9.21% and 8.10%, 2.17% and 6.62%, and 2.03% and 5.02%, respectively.@*CONCLUSION@#The floral parts contribute unequally to the yield of orientin and vitexin, and the calyx contributes the highest and makes a significant difference compared with any other part.

Investigation on Flos Trollii: constituents and bioactivities / 中国天然药物

Flos Trollii, the flowers of Trollius chinensis Bunge, has been widely used in Chinese and Mongolian medicine for its efficacy of heat-clearing and detoxification. This drug has both medicinal and edible applications, and has led to various pharmacognosy, natural product chemistry, and pharmacology studies. As a result, its chemical constituents and bioactivities have been well-characterized in recent years. Nevertheless, a couple of critical issues, such as the major effective components, are still unresolved. The present review summarizes research progress on this drug regarding the constituents and bioactivities based on investigations in these laboratories and the results reported in recent publications. In addition, the pending issues are discussed and constructive suggestions for further investigation are proposed.

Research progress of alternative production approaches of salidroside / 中国中药杂志

Salidroside, one of the active components of Rhodiola plants, is a phenolic glycoside with significant biological activities. The investigation and development of alternative production approaches of salidroside is of high academic and application values due to the limited resource of Rhodiola plants, and from which the low yield of salidroside. This review summarized the research progress and perspective of the alternative production approaches of salidroside including both chemosynthetic and biosynthetic methods and pathways.

A new comprehensive procedure for the quality control of Semen Cassiae and its application in evaluating commercially available material in China / 中国天然药物

AIM@#To establish a more comprehensive and suitable procedure for the quality control of Semen Cassiae which can be used to supplement the evaluation procedure adopted by the Pharmacopoeia of the Peoples Republic of China.@*METHODS@#A HPLC assay-based comprehensive quality evaluation procedure for Semen Cassiae using three bioactive compounds including anthraquinones and naphthopyrones, i.e., chrysophanol-1-O-β-D-glucopyranosyl-(1→3)-β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside (1), rubrofusarin-6-O-β-D-gentiobioside (2) and toralactone-9-O-β-D-gentiobioside (3) as the index components was established. The resultant data were further analyzed by principal component analysis (PCA) and data distribution methods using software SPSS 16.0.@*RESULTS@#Sixty-six batches of Semen Cassiae obtained from various regions of China were analyzed with the procedure. Based on the test results of these batches, the content limits of the three bioactive compounds in Semen Cassiae were proposed.@*CONCLUSION@#The procedure established herein is more comprehensive and appropriate for the quality evaluation of Semen Cassiae commercially available in China, and can be used as a useful supplement to the current official method in China for the quality evaluation of Semen Cassiae.

Analysis of fatty acids in the seeds of Sterculia lychnophora by GC-MS / 中国中药杂志

<p><b>OBJECTIVE</b>To analyze and identify fatty acids in the seeds of Sterculia lychnophora.</p><p><b>METHOD</b>The compositions was isolated and determined by GC-MS technique, and area normalization method was used to make quantitative analyze of the content of compositions.</p><p><b>RESULTS</b>21 Fatty acids and 5 other compositions were isolated and determined.</p><p><b>CONCLUSION</b>The major fatty acids are 9,12(Z,Z)-octadecadienoic acid(37.96%), hexadecanoic acid(24.77%), 9-(Z)-octadecenoic acid(19.77%) and octadecanoic acid(5.01%).</p>