Study on effective sites of anti-gonococcus in Polygonum capitatum extract / 中草药

Objective To analyze the components of active anti-gonococcal fractions in the extracts of Polygonum capitatum. Methods Drug sensitive paper method and Neisseria gonorrhoeae culture method were used to detect the antibacterial activity of different parts of the flower bud extract against Neisseria gonorrhoeae. UPLC-TOF-MS was used to identify the effective parts of the flower bud extract with anti-gonococcal effect. Results As a result, in the eluate obtained by extracting with a specific macroporous resin, the hydrolysable tannin was contained in the methanol (35%) eluate (fraction F3), such as trigallocyl glucose. This fraction had a good anti-gonococcal effect. The fractions of F2 and F4-6 had a weak antibacterial effect, while other fractions have no antibacterial effect. Conclusion This study provides a basis for the use of trigalactosyl glucose in the preparation of anti-gonococcal drugs, and lays a foundation for the development of a clinical drug of P. capitatum extracts against Neisseria gonorrhoeae.

UPLC-Q-TOF-MS/MS analysis on prototypes components and metabolites of effective fractions of Polygonum orientale flower in rat serum and urine / 中国中药杂志

Ultra performance liquid chromatography coupled with time-of-flight mass spectrometry( UPLC-Q-TOF-MS/MS) method was applied to analyze the prototypes and metabolites of the effective components of Polygonum orientale in SD rat serum and urine. The separation was performed on Agilent Eclipse Plus C_(18) column( 2. 1 mm×100 mm,1. 8 μm),with 0. 1% formic acid solution( A)-acetonitrile( B) as the mobile phase for gradient elution. Mass spectrometry data of biological samples were obtained under positive and negative electrospray ion mode. By comparing chromatogram differences between blank samples and drug treatment samples,prototype components and metabolites of the effective components of P. orientale extract were identified. The results showed that 12 metabolites were detected in serum and 26 metabolites in urine( including cross-components) of rats. The main metabolic pathways included hydrogenation,hydroxylation,glucuronidation,sulfation reaction,and methylation-glucuronidation,etc. The method established in this study was reliable and effective for studying the metabolic characteristics of the effective components of P. orientale in rats,and it can provide a reference for further studies on therapeutic material basis of this herb.

Metabolism of effective fractions of Polygonum capitatum in rat feces and bile / 中草药

Objective: To investigate the metabolite profile of effective fractions of Polygonum capitatum in rat feces and bile. Methods: In this study, ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC- ESI-Q/TOF-MS) was applied to the identification of metabolites of P. capitatum extracts in rat bile and feces after ig administration. Mass defect filter and Metabolite Tools software were also used. Results: The four parent components and 26 metabolites were identified in rats metabolic experiments in vivo, including 12 metabolites in feces and 19 metabolites in bile. The major metabolites were glucuronide conjugation, methyl-glucuronide conjugation, and sulfate conjugation of quercetin; Conclusion: The studies have established a high-resolution mass spectrometry method to analyze the metabolites of effective fractions of P. capitatum in vivo. The in vivo metabolic characteristics of the components presented in the fraction have been clarified. The work lays a foundation for the clinical application and development of P. capitatum.

Compatibility Studies of Effective Fractions in Shengmaisan on Cerebral Ischemia and Anoxia in Mice / 中药新药与临床药理

Objective To explore the proper proportion of effective fractions in Shengmaisan(saponins of Radix ginseng,saponins of Radix ophiopogonis,Lignans of Fructus schisandrae)in different anoxia models.Methods Acute cerebral hypoxia was induced by sodium nitrite and decapitation in mice,and the orthogonal design was used in these two models to find the proper proportion of three effective fractions.The gasping time of the mice,which were decapitated was observed to compare the anti-anoxia effects of XZF with other clinical drugs,and cerebral ischemic reperfusion injury model of mice was also used to study the effect of XZF on related biochemical index.Results XZF(the proportion of saponins of Radix ginseng,saponins of Radix ophiopogonis,Lignans of Fructus schisandrae as 7 ∶ 2 ∶ 6)significantly prolonged the gasping time,and decreased brain nitrogen monoxidum(NO)content after reperfusion of the mice at dosages of 50 mg/kg and 150mg/kg.Meanwhile,XZF also reduced malondialdehyde(MDA)content and increased superoxide dismutase(SOD)activity at the higher dosage.Conclusion XZF obtained by experimental screening exerts a significant protective effect on cerebral ischemia injury in mice,which provide some pharmacological evidence for further development of new modern Chinese drug composed with effective fractions for cerebral vascular diseases.

Recent development on effective fractions of compounded prescription of Chinese crude drug / 中国药理学通报

The compounded prescription of Chinese crude drug is a key problem in the study of traditional Chinese medicine.A new research field that focuses on the group of effective fractions of Chinese crude drugs becomes more important as the result of combination of the theorem of traditional Chinese medicine and techniques of modern medicine.Up to date,the researches on this field are preliminary,remaining a lot of subjects to be explored.