Pharmacokinetic and tissue distributions study of adenosine, 4-hydroxybenzyl alcohol and Parishin C from Gastrodia elata extract in rats.

The plant Gastrodia elata is a type of the orchid plant Gastrodia elata Bl. which contains glycosides, phenols, polysaccharides, sterols, and organic acids and a variety of active ingredients are proved to have certain pharmacological activities. To understand the process in the body of Gastridua elata, we used HPLC to study pharmacokinetics and tissue distributions of adenosine, 4-hydroxybenzyl alcohol and Parishin C in rats. The results showed that the three ingredients could be detected in plasma and different organizations at various time points. There was no significant difference in systemic clearance at three ingredients and it may be show that the three ingredients distributed (0.475±0.025, 0.518±0.033, 0.699±0.051) quickly and eliminated (5.37±0.87, 4.54±0.69, 5.34±0.82) slowly in plasma. There was the highest content of adenosine in spleen, followed by liver and lung. The highest content of 4-hydroxybenzylacohol in liver, and was higher in spleen. Parishin C was highest in heart, followed by liver and spleen. It is obvious that the contents of three ingredients are all higher in liver. The trends of the three ingredients' contents in G. rhizome extract were consistent with the contents in the plasma after intravenous administration.

Plasma pharmacokinetics and tissue distribution of arctiin and its main metabolite in rats by HPLC-UV and LC-MS.

The pharmacokinetic profile of arctiin, the major active lignan in fruits of Arctium lappa L., was investigated. Its main meta"bolite arctigenin was identified by an LC-MS method, and an HPLC-UV technique was developed for the simultaneous quantification of the metabolite and arctiin in plasma and organs. Chromatographic separation was performed on an Agilent™ C18 HPLC column with acetonitrile and water by linear gradient elution. Arctiin and arctigenin were identified on-line by LC-MS. The pharmacokinetics and tissue distribution of arctiin and arctigenin were determined for the first time by using a simple, selective, and accurate HPLC method. The AUC0-t values of arctigenin were larger compared with arctiin after oral administration of arctiin. The concentration of the metabolite was significantly higher than the concentration of arctiin in the stomach and small intestine in rats after oral administration of arctiin, indicating that the stomach and small intestine were the major organs of arctiin metabolism. These findings could provide support for the clinical studies conducted with Fructus Arctii.

A new method for studying the mechanism of "Feature Identification based quality assessment" of Traditional Chinese Medicine, taking Gastrodiae Rhizoma as an example.

Aim of the study: The research group proposed that the mechanism of "Feature Identification based Quality Assessment" (FIQA) of Traditional Chinese Medicine (TCM) can be explained according to the relationship between the "Feature" of TCM and the Pharmacodynamic Components representing the holistic effect of TCM. Gastrodiae Rhizoma (GR) was selected as the research object to reveal the close relationship between "Feature" and the quality of TCM. Materials and methods: In this study, the "Feature" such as "Shape", "Color", "Odour" and "Taste" of GR are quantified by the electronic nose, electronic tongue, and other instruments. Then, the Pharmacodynamic Components Group (PCG) of GR was determined which could reflect the holistic effect of GR by spectrum effect relationship analysis. By analyzing the correlation between the "Feature" and the content of PCG, the mechanism of FIQA of GR was determined. Results: The quantitative results of "Shape", "Color", "Odour" and "Taste" of GR from different sources were significantly different. Six components were selected as the PCG, which can represent the holistic effect of GR in the aspect of the neuroprotective effect. There was a good correlation between the components in the PCG and "Feature". Conclusions: The quality of GR can be determined quantitatively according to its "Shape", "Color", "Odour" and "Taste". The mechanism of FIQA of TCM can be explained according to the relationship between the Shape of TCM and the Pharmacodynamic Components representing the quality of TCM. The revelation of this mechanism reflects the holistic characteristics of the multi-component synergistic effect of TCM. This study provides a reference research method for revealing the mechanism of FIQA of TCM.

Synthesis of (-)-arctigenin derivatives and their anticancer activity.

The natural dibenzylbutyrolactone type lignanolide (-)-arctigenin, which was prepared from fructus arctii, showed obvious anticancer activity. The synthesis of four new (-)-arctigenin derivatives and their anticancer bioactivities were examined. The structures of the four new synthetic derivatives were elucidated.

Prediagnostic methods for the hemolysis of herbal medicine injection.

ETHNOPHARMACOLOGICAL RELEVANCE: The Xue-Sai-Tong injection, a traditional Chinese medicine injection with total saponins extracted from Sanchi Ginseng, has been used for more than half a hundred years to treat coronary artery disease. The study is to establish a prediagnostic method for the hemolytic adverse effect of herbal medicine injection by taking Xue-Sai-Tong injection as an example. MATERIALS AND METHODS: A new method named "fuzzy dissemination" was established to identify the hemolytic ginsenosides in Xue-Sai-Tong injection on the basis of fuzzy changes of individual ginsenosides in the injections altered by re-adding the fractions prepared from the total saponins and statistic analysis between hemolytic degrees and individual ginsenosides. Related substances test, safety tests and fingerprints of the injections in different batches were tested. RESULTS: HD(50), P(50) and interactions on hemolysis of individual ginsenosides were examined. Experiment indicated that the content of Rg(1), Rg(2), M(51) (an unknown ingredient with retention time at 51 min in HPLC) and M(70) in Xue-Sai-Tong injection showed a significant positive correlation with hemolytic degree, and the content of R(1), Re, Rb(1) and Rd showed a significant negative correlation with hemolytic activity. Furthermore HD(50) of injection exhibits superiority to other tests for the hemolysis of injections. Abnormal hemolysis in some batches of injections was observed, but there were no significant differences among injections of different batches in related substances test, safety test and fingerprints. CONCLUSIONS: This is an original method to analyze active ingredients of a complicated integrity instead of studying on individual ingredients, it showed that the interactions of some individual ginsenosides and some unknown micro-ingredients in Xue-Sai-Tong injection were the major factors causing hemolysis, and this method could also be utilized in research of corresponding aspects. HD(50) of injection can reflect the changes of hemolytic property of injections caused by not only the change of active constituents of injection, but also the auxiliary materials. Thus it was recommended as an index for the hemolytic prediagnosis of the injections in practice.

A new hexenol glycoside from leaves of Smallanthus sonchifolius.

A new hexenol glycoside with two known compounds was isolated from the leaves of Smallanthus sonchifolius. The structure of the new compound was elucidated as Z-hex-3-en-1-ol O-alpha-L-arabinopyransyl (1''-2')-beta-D-glucopyranoside (1) on the basis of spectroscopic analysis and chemical evidence. The two known compounds were identified as ent-15ß-hydroxy-kaur-16-en-19-oic acid (2) and ent-18-hydroxy-kaur-16-en-19-oic acid (3) by comparison of their spectral data with the reported data. Compounds 2 and 3 were isolated for the first time from the title plant.

New compounds from leaves of Smallanthus sonchifolius.

A new octadecatrienoic acid and a new benzyl glycoside, along with a known compound, were isolated from the leaves of Smallanthus sonchifolius. The structures of the two new compounds were elucidated as 13(R)-hydroxy-octadeca-(9E,11E,15Z)-trienoic acid (1) and benzyl alcohol 7-O-alpha-L-arabinopyranosyl(1" --> 2')-beta-D-glucopyranoside (2) on the basis of spectroscopic analysis and chemical evidence. The known compound was identified as 13(R)-hydroxy-octadeca-(9Z,11E,15Z)-trienoic acid (3) by comparison of its spectral data with that reported. Compound 3 was isolated for the first time from the title plant.