| ObjectiveCarbon medicine is widely used,and its intrinsic quality is the basis of clinical efficacy.Scutellaria baicalensis carbon,as a commonly used charcoal drug,exists in many local processing specifications.It is found that there are no clear and specific provisions on its processing technology,and the judgment of the processing endpoint is subjective,mostly in appearance,the color of section,texture,odor,and other characters,and the expression is not the same in different places.Therefore,the unified quantitative standard of the processing endpoint of Scutellaria carbon needs to be improved.This study took Scutellaria baicalensis carbon as an example,and guided by "anti-inflammatory" activity,then searched for the change rule and internal correlation of three indexes of "morphological,chemical and biological",found out the processing endpoint and the evaluation index of Scutellaria baicalensis carbon.The processing mechanism of scutellaria baicalensis carbon was initially explained from the perspective of pharmacokinetics of flavonoids,so as to verify the rationality and accuracy of the quality evaluation method of Scutellaria baicalensis three-sex system and provide new ideas and methods for the quality evaluation and quality control of other carbon drugs.Methods1.Study on anti-inflammatory mechanism of Scutellaria carbon and screening of active ingredientsThe anti-inflammatory mechanism of Scutellaria baicalensis carbon was explored by network pharmacology and molecular docking techniques,and the main components and target proteins representing its activity were selected.2.Study on the influence of processing degree on morphological,chemical,and biological indexes of Scutellaria baicalensis carbonDetermination of the carbon shape index of Scutellaria baicalensis:the chromaticity values L*,a*,b*were measured by the color difference instrument,and the yield was calculated by weighing,and the curve was drawn for analysis.3.According to the correlation mechanism of three indicators,the processing endpoint of Scutellaria carbon was establishedSpearman correlation analysis was conducted according to SPSS software,and the correlation coefficients between L*,a*,b*,and Eab*values and 5-HMF,baicalin,baicalin,baicalin,baicalin,and polysaccharide were calculated,respectively.Correlation analysis of chemical and biological indicators was conducted according to JMP pro 16 and SPSS software.Principal component analysis was obtained among morphological,chemical,and biological indexes by SIMCA software to find the best processing endpoint and representative indexes.4.Study on the effect of processing degree on the transfer rate of flavonoids in Scutellaria baicalensis carbonThe processing mechanism of Scutellaria baicalensis carbon was preliminarily explored from the perspective of the solubility of the BCS system.5.To explain the processing mechanism of Scutellaria baicalensis carbon from the perspective of the pharmacokinetics of flavonoidsTo investigate the effects of Baicalin and Wogonoside in blood at different time points of SD rats,DAS 2.0 software was used for analysis,and PK parameters such as AUC,Tmax,and Cmax were obtained.The processing mechanism of Scutellaria baicalensis carbon was explored from the perspective of permeability of the BCS system,and the evaluation system of three characteristics of Scutellaria baicalensis carbon was verified.Results1.Through the network model of pharmacology and molecular docking technology,the key active ingredient in Scutellaria baicalensis carbon with TNF-α,VEGFR-1,and HIF-1 docking situation of the target protein was simulated.Cell experiment also found that Baicalein and Wogonin element,compared with Baicalin and Wogonoside,had a shorter window.Finally,Baicalin,Wogonoside,Baicalein,and Wogonin were as representative of the chemical index of flavonoid ingredients,and NO,IL-6,and TNF-α inhibition rates were as anti-inflammatory activity of biological indicators for subsequent research.2.It was found that a*value of chemical indexes of Baicalin,Baicalein,5-HMF,polysaccharide components and morphological indexes all showed a changing pattern of increasing and then decreasing,with an inflection point phenomenon.Combined with the results of antiinflammatory activity,it could be inferred that Scutellaria baicalensis carbon at 150℃-50min,180℃-30min and 210℃-20min was processed moderately.Meanwhile,the correlation analysis results of the three indexes showed that a*value could be used as the shape index of the processing endpoint of Scutellaria baicalensis’s anti-inflammatory effect.The contents of Baicalin and Wogonoside could be used as chemical indexes of the processing endpoint of the anti-inflammatory effect of Scutellaria baicalensis carbon and the inhibition rate of NO and IL6 inflammatory mediators could be used as biological indexes of the processing endpoint of the anti-inflammatory effect of Scutellaria baicalensis carbon.3.Focus on the content transformation and transfer rate changes of four flavonoids in Scutellaria baicalensis carbon extract.Based on the BCS theory,the pharmacokinetics in rats as its permeability experiment to analyze the processing mechanism and processing endpoint,and it was found that the inflection point of flavonoids in its extract may be different from that of decoction pieces.The results showed that the transfer rates of the four components decreased with the deepening of the processing degree.However,the transfer rate increased when the ratio of material to liquid decreased.Pharmacokinetic results in vivo showed that the conditions corresponding to the inflection point of a*value of Scutellaria baicalensis after processing were moderate processing and its bioavailability was the best.However,it still needed to be verified by in vivo pharmacodynamic experiments.ConclusionStarting from the theory of "color discrimination and quality",this study explored the internal correlation between shape,chemistry and anti-inflammatory activity and established a comprehensive quality analysis method of shape,chemical,and biological indicators of Scutellaria baicalensis carbon.Based on the transfer rate of flavonoids and PK parameters in vivo,the processing mechanism of "sauteed charcoal survival" of Scutellaria baicalensis carbon was explained to a certain extent.Find the judgment index of its processing endpoint.It was concluded that Scutellaria baicalensis carbon processed at 150℃-50min,150℃-60min,180℃30min,and 210℃-20min was moderately processed,and the a*value of the shape index could be used as the shape index of the processing endpoint of Scutellaria baicalensis.The contents of baicalin,baicalin,polysaccharide,and 5-HMF can be used as chemical indicators of the processing endpoint of Scutellaria baicalensis carbon.The inhibition rate of NO and IL-6 inflammatory mediators can be used as biological indicators of the processing endpoint of Scutellaria baicalensis carbon,suggesting that the processing endpoint should be evaluated by paying attention to the component transfer rate and in vivo absorption,which provides a theoretical basis for future quality evaluation of Scutellaria baicalensis carbon. |
PDF Full Text Request