| Scutellaria baicalensis Georgi,an indigenous medicinal plant in China,was first recorded in Shennong Bencao Jing(the Classic of Herbal Medicine,written between about 200 and 250 AD).Its dried root(Scutellariae Radix)is a typical traditional Chinese medicine and the aerial parts of S.baicalensis have been used as Huangqin teas for thousands of years.At present,it has been sold as a product of "Huangqin Tea" in some areas.Moreover,the flavonoids in the aerial parts of S.baicalensis have also been developed as one kind of detoxification capsules.The biomass of the aerial parts(stem,leaf,and flower)of S.baicalensis is more than roots,it is usually discarded during the root’s harvesting or only a part of them was used as the material of Huangqin Tea.However,there is no quality evaluation method for the Huangqin teas and related products,which significantly hampered the development of the Huangqin Tea industry and the utilization of the aerial parts of S.baicalens.Thus,this study provides essential information to better understand the aerial parts of S.baicalensis with regard to its components,contents determination and bioactivities.Meanwhile,based on the aim to make ultimate use of resources,we also made a primarily pharmacophylogenetic investigation of the Genus Scutellaria.The detailed content and results in this study are as below:1.In this study,11 compounds were isolated by the combination of column chromatography of silica gel,MCI,ODS and Sephadex LH-20 or preparative liquid chromatography from the aerial parts of S.baicalensis,and then identified by spectral techniques such as 1H,13C-NMR,etc.These compounds namely,isocarthamidin-7-O-β-D-glucuronide(1),carthamidin-7-O-β-D-glucuronide(2),apigenin-7-(glucuronide 6-methyl ester)(3),wogonin(4),cosmosiin(5),chrysin(6),isochromatin(7),syringaldehyde(8),trans-hydroxyphenylpropenoic acid(9),isoscutellaeein-8-O-glucuronide(10),4-hydroxybenzyl aldehyde(11).Compounds of 3,8and 11 were isolated from the aerial parts of S.baicalensis for the first time.Compounds of 1 and 2 are two scarcity flavanones in nature,which has high contents in the aerial parts of S.bacalensis and can be used as an index compound for evaluating the quality of the aerial parts of S.baicalensis.2.A HPLC-DAD method for simultaneous determination of 15 flavonoids and systematically compared their contents and distribution in the roots,stems,leaves,and flowers of S.baicalensis was established.The results from 77 samples showed significant differences of the contents and distribution of 15 flavonoids among the different parts of S.baicalensis and the chromatographic fingerprints of different parts of S.baicalensis were established.Chemical analysis of different parts(stem,leaves,flowers,roots)of S.baicalensis was determined by UPLC-QTOF-MS,and the chemometrics analysis method was used for further analyzing and processing.A total of 31 different compounds were identified in the aerial parts and the roots of S.baicalensis,of which 17 were identified according to the literature.3.The method of luciferase reporter gene was used screened the anti-influenza virus activities of the water and alcohol extraction and main compounds of the different parts of S.baicalensis.Also,combined with HPLC-DAD technique,the content and distribution of 15 main flavonoids in different parts of S.baicalensis was determined and the dose-effect relationship was evaluated.The results showed that the main components in the aerial parts of S.baicalensis had certain antiviral activities.Also,the anti-influenza activity of "Kuqin" is stronger than the "Ziqin",and this is consistent with the fact that clinically traditional of "Kuqin" is used mostly for upper respiratory tract infections(clear lung heat).In addition,it was found that there was a dose-effect relationship between the anti-influenza virus activity of the high content of isocarthamidin-7-O-β-D-glucuronide and scutellarin and different extracts of aerial parts of S.baicalensis Georgi.Furthermore,different group of HPG2 cells was treated with isocarthamidin-7-O-β-D-glucuronide,scutellarin and the aerial parts of S.baicalensis extracts.Through the functional enrichment analysis,GO and KEGQ we identified some differentially expressed genes and their related pathways and diseases phenotype.4.The chemical composition of 14 species in Scutellaria was analyzed by UPLC-QTOF-MS.We found that the chemical compositions were similar in the roots of Subsect.Angustifoliae Benth,which all have more developed roots.However,the phytochemical compositions of other lines in the same group could be separated by chemical methods.There are certain differences in the chemical composition of all the tested roots and aboveground parts of different species,indicating that the synthesis pathway of the internal secondary metabolites is different.In addition,the phytochemical compositions of S.tsinyunensis,S.yumanensis.var.salicifolia,S.pekinensis,S.pekinensis var.ussuriensis,S.macrodonta and S.dependens were identified,which have few studies of their chemical background.At the same time,HPLC was adapted for the identification of 15 major flavonoids in 14 plant species in genus Scutellaria.These plants mostly contain the compounds of isocarthamidin-7-O-β-D-glucuronide,carthamidin-7-O-β-D-glucuronide,scutellarin,baicalin,apigenin-7-O-glucoside,isoscutellaeein-8-O-glucuronide,Chrysin 7-O-β-D-glucopyranuronoside and wogonoside.It also suggests that the aerial parts of S.macrodonta and S.rehderiana may be the resources of Huangqin tea.In conclusion,based on the study about chemical constituents of Huangqin Tea,this paper firstly has applied a multi-index method to establish the quantitive method by HPLC to determine the primary components’ contents in the aerial parts of S.baicalensis,and it would promote the establishment of quality standard of the aerial parts of S.baicalensis and its products.Furthermore,this study provided a rational explanation for the use of its roots as a traditional Chinese medicine,while the aerial parts as teas.The studies on the anti-tiviral activity and high-throughput screening of active ingredients,providing a preliminary scientific basis for the application of"Huangqin Tea" and its resources.The analysis and comparison study about the chemical constituents of 14 kinds of Scutellaria,not only filled the chemical background gaps of six kinds of them,but also provided solid basis for further research on pharmacophylogenetic properties of S.baicalensis. |
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