| Schaefflera octophylla?Lour.?Harms?abbreviated as SO subsequent to this abstract?of the Araliaceae family are even widely distributed in southern China.Its stems,leaves,root bark and nectar are used as folk medicines to treat colds,pain,inflammation and liver protection since ancient times,furthermore the stems and leaves of which are the basic materials of traditional Chinese medicines named as Qiyelianpian.However,the basic research on the effective components and pharmacological effects of SO is still lacking.On the other hand,with the growing demand in the medicinal herbs market,not only the resources of wild SO are excessively reclaimed,but also other fake SO are mixed in the market,resulting in that the medicinal herbs SO are of different quality.People realize that it is necessary to establish the objective evaluation criteria of medicinal herbs quality which can ensure the quality of herbs can be controlled.Therefore,in order to deeply explore the quality assessment methods and effective ingredient quality standards of traditional Chinese medicine SO,and expect to acquire the scientific and rational use of Chinese herbal medicines,this article focuses on the study as the following aspects based on our previous study on it.1.Optimization of extraction process for total triterpenoids of Schefflera octophylla?SOTT,total triterpenoid compound of Schefflera chinensis?and isolation and identification of monomeric compounds.1)On the basis of four single-factor experiments including Volume concentration of ethanol,extraction time,ratio of liquid to material,the SOTT extraction process was optimized by response surface methodology and a mathematical model was established.The optimum process parameters for SOTT extraction were optimized by the experimental model equations:ethanol concentration is 80%,extraction time is 100 min,liquid material ratio is 10:1,and the extraction times is 3.The actual verified SOTT maximum extraction rate is2.29%.2)nine compounds were isolated from SOTT by column chromatography and HPLC preparation.Nine pentacyclic triterpenoids were identified by physicochemical constants and spectral analysis techniques,one of which is a new compound,and two compounds were isolated for the first time from SO.2.Experimental Study on the content of SOTT in medicinal materials of SO and its quality evaluation.1)triterpenoids.The content of three kinds of triterpenoid compounds which are rich in different medicinal original plants?S.octophylla,S.arboticola,S.venulosa,S.kangsiensis?with anti-inflammatory activity?SOT-3:betulinic acid-3-Sulfate;SOT-4:Pentapenic acid;SOT-8:Pentadecanoic acid-28-O-?-L-rhamnoyl-?1-4?-O-?-D-glucosyl-?1-6?-?-D-glucoside?were measured by HPLC?High performance Liquid Chromatography?.The results showed that the content of triterpene compounds in the herbs from Schefflera ocarina was higher than that in other plants?Scheffenbrutchus sinensis,M.chinense,and Schisandra chinensis?.The content of three compounds in the fruit of Chai is higher than that of the stem and leaf.Therefore,it is suggested that SOTT,especially SOT-4,can be used as a quality index for inspecting the medicinal material of Schisandra chinensis.The fruit of Schisandra chinensis should also be recommended for medicinal use in the article by the experiment conclusion.3.Experimental Study on main pharmacodynamics of SOTT&its monomers.1)Pharmacodynamic test in vitro:The activity of RAW264.7 macrophage inflammatory model induced by LPS in vitro was studied.?a?The study on the activity of LPS-induced RAW264.7 macrophage inflammatory model in vitro showed SOTT and9 monomeric compounds isolated from S.Octophylla,to different extent,had different inhibition to the release of NO of LPS-induced Raw-264.7 cells.The anti-inflammatory mechanism of SOTT is to reduce inflammation by reducing the level of pro-inflammatory cytokines IL-1?,TNF-?,IL-6,NO and promote the level of anti-inflammatory factor IL-10 reaction.2)Pharmacodynamic test of SOTT on the hepatocarcinoma cells in vivo:To investigate the anti-hepatocarcinoma activity of SOTT with three hepatoma cell lines HuH7,HepG2 and SMMC-7721,and to explore the anticancer activity cycle and the mechanism of cell apoptosis.SOTT showed different inhibitory activity on different liver cancer cell lines,which was related to time and dose.3)To investigate the hepatotoxicity of SOTT induced by CCl4-induced acute liver injury in mice:the expression of liver injury factor CYP2E1 in mRNA and protein levels were detected.Therefore,SOTT has a better protective effect on CCl4-induced mice with acute liver injury.The mechanism may be related to the regulation of oxidative stress after liver injury,the reduction of the lipid peroxidation after injury,the enhancement of the antioxidant capacity of the liver,and the inhibition to overexpression of liver injury effect factor CYP2E1.4)The acute gastric ulcer effect of HLEDA,the main component of SOTT was studied.In order to investigate the protective mechanism,the levels of antioxidant and oxidative factors?SOD,CAT,GSH-Px and MDA?,inflammatory factors?TNF-?,IL-6 and NO?,and anti-inflammatory factor IL-10 in serum,SH and PGE2 in gastric tissue of experimental rats were detected according to test-kits,mRNA and protein expression of COX-1 and COX-2 by PCR,the expression of Hsp70,Bax and Bcl-2 protein were detected by immunohistochemistry.The mechanism of HLEDA on gastric mucosal protection was as follows:HLEDA was able to improve the levels of GSH,SOD,CAT,GSH-PX,IL-10 NP-SH and PGE2,decrease the levels of MDA,TNF-?,IL-6and NO in the serum or gastric tissue of gastric ulcer rats,increase the expression of COX-1,COX-2,Hsp70 and Bcl-2 in gastric tissue,and reduce the expression of Bax.The main pharmacodynamics study of anti-inflammation,anti-tumor and other effects of SO.1)In-vitro pharmacodynamics test?a?Anti-inflammatory effect experiment Using lipopolysaccharide to stimulate RAW264.7 macrophage to establish inflammatory cell model,study SOTT and each The effect of monomer on the secretion of inflammatory cytokines TNF-?,IL-1?,IL-6,and inflammatory mediators NO and anti-inflammatory cytokines IL-10 by macrophages.The results showed that both SOTT and the nine monomer compounds isolated from it have different effects of inhibition of LPS-induced NO release from Raw-264.7 cells,and decreased levels of IL-1?,TNF-?,IL-6,and NO by inflammatory cytokines in the cells.Promotes the level of anti-inflammatory cytokine IL-10 and reduces inflammation.?b?Anti-tumor effect:After intervention with three hepatoma cells,HuH7,HepG2,and SMMC-7721,SOTT showed cell viability inhibition.The mechanism may be to promote the apoptosis of hepatoma cells by regulating the expression of Bcl-2 family proteins.2)In Vivo Pharmacodynamic Testing?a?The Protective Effect of SOTT on CCl4-induced Acute Liver Injury in Mice:SOTT Regulates Oxidative Stress after Liver Injury,Reduces Lipid Peroxidation After Injury,and Enhances Antioxidant Capacity in Liver,inhibiting the overexpression of liver injury effector factor CYP2E1.?b?Experiment on the maintenance of acute gastric ulcer induced by absolute ethanol in monomeric SOT-4?HLEDA?isolated from the three quails of Schmidt.SOT-4 can reduce the degree of rat gastric mucosal damage caused by ethanol,increase serum or tissue levels of GSH,SOD,CAT,GSH-Px,IL-10,NP-SH,and PGE2,or reduce MDA,NO,The levels of TNF-?and IL-6increased the expression of COX-1 and COX-2 mRNA and the expression of Hsp70and Bcl-2 protein in gastric tissue,decreased the protein expression of Bax,and thus maintained gastric mucosal function.The thesis systematically and experimentally studies and evaluates the medicinal value and quality inspection criteria of the three species of SO.in order to search for a scientific basis for the further rational development and utilization of traditional Chinese medicine SO. |
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