| Objective: In order to ascertain the difference in efficacy by comparing the pharmacodynamics of the water decoction of Green Forsythiae Fructus and Ripe Forsythiae Fructus. And using the analysis of serum pharmacochemistry to see whether their components into the blood are differences.Methods: Selection Green Forsythiae Fructus and Ripe Forsythiae Fructus grown in Shanxi with traditional water extraction as experiments subjects unfold related experiments.1、Using the classical animal models to compare the difference of the effect in the anti-inflammatory, anti-endotoxin, sweating, hepatoprotective of the Green Forsythiae Fructus and Ripe Forsythiae Fructus.And the experiments of the classic recipe Lianqiaosan in treating sores and Yinqiaosan in treating acute lung injury furtherly verify the difference in efficacy of the Green Forsythiae Fructus and Ripe Forsythiae Fructus.2、Using the technology of serum pharmacochemistry to establish the inside and outside HPLC fingerprints of the water decoction of Green Forsythiae Fructus and Ripe Forsythiae Fructus and the serum fingerprints of inflammation of rats. we can analyze the blood transitional components and compare the component difference between Green Forsythiae Fructus and Ripe Forsythiae Fructus.Then we can initially confirm the antiinflammatory effects material basis of the Forsythiae Fructus.3、The water decoction of Green Forsythiae Fructus can divide into petroleum ether layer, the ethyl acetate layer, n-butanol layer and water layer using the method of solvent system.Then we can select the anti-inflammatory effective part of the Green Forsythiae Fructus using the H1-NMR metabolomicsResults: 1、The pharmacodynamics systematic comparison(1) In terms of anti-inflammatory effects: The water decoction of Green Forsythiae Fructus and Ripe Forsythiae Fructus can inhibit ear swelling in mice by xylene induced. but the Green Forsythiae Fructus treatment acute inflammation(P<0.01) better than the Ripe Forsythiae Fructus(P<0.05);In the chronic inflammation model, The water decoction of Green Forsythiae Fructus and Ripe Forsythiae Fructus can significantly inhibit agar granuloma in rat(P<0.05), there was no significant difference(P>0.05).(2) In terms of anti-endotoxin effects: when the concentration of the Green Forsythiae Fructus is 1.0g / ml,the result of the vitro anti-endotoxin is negative, while the Ripe Forsythiae Fructus is 1.5g / ml. The result indicates that the effects of Green Forsythiae Fructus against endotoxin(P<0.01) better than the Ripe Forsythiae Fructus(P<0.05) in vitro. And Green Forsythiae Fructus have significant differences compared with the model group after 5.5 hours,while Ripe Forsythiae Fructus is 6.5 hours in the experiment of vivo anti-endotoxin. There is not significant differences between Green Forsythiae Fructus and Ripe Forsythiae Fructus.(3) In the aspects of promoting sudation:Compared with the control group, the water decoction of Green Forsythiae Fructus has obvious sweating(P<0.05); Compared with the Ripe Forsythiae Fructus, the water decoction of Green Forsythiae Fructus has obvious sweating(P<0.05), which explains the sweating of Green Forsythiae Fructus is superior to the Ripe Forsythiae Fructus. And the volatile oil of Green Forsythiae Fructus also has obvious sweating,so the volatile oil may be Green Forsythiae Fructus to play one of the material basis of sweating.(4) In terms of protecting liver function: Compared with model group, the water and alcohol extract of Ripe Forsythiae Fructus can obviously reduce the activity of Alanine Transaminase(P<0.05); While the water and alcohol extract of Green Forsythiae Fructus have no significant difference(P>0.05).But with the increase of the dose,the function of the Green Forsythiae Fructus and Ripe Forsythiae Fructus reduce the activity of Alanine Transaminase have no obvious difference, compared with model group(P<0.05).(5) In terms of compound authentication:(1) In the experiment of Lianqiaosan treat sores, it found that three days after the treatment,the water decoction of the Green Forsythiae Fructus and Lianqiaosan which was added in Green Forsythiae Fructus can inhibit red and secretion of acute sore wound in Guinea pigs.When it is seven days after the treatment, the result is the opposite. And the sore skin pathology tissue of Green Forsythiae Fructus improved better than Ripe Forsythiae Fructus,while the sore skin pathology tissue of Lianqiaosan which was added in Ripe Forsythiae Fructus improved better than Lianqiaosan which was added in Green Forsythiae Fructus.(2) The experiment of Yinqiaosan in treating acute lung injury,the level of TNF-α in the lung washes of Yinqiaosan which was added in Green Forsythiae Fructus significantly decreases.And the level of IL-6, IL-1β obviously reduce compared with the model group.The level of IL-6,IL-1β in the lung washes of Yinqiaosan which was added in Ripe Forsythiae Fructus obviously reduce.While the level of IL-1β has no significant difference compared with the model group(P>0.05).The levels of these three inflammatory factors in the Yinqiaosan which was added in Green Forsythiae Fructus were much lower than Yinqiaosan which was added in Ripe Forsythiae Fructus.2、To screen the effective part of anti-inflammatory effect of Green Forsythiae Fructus(1) The levels of TNF-α, IL-1β in the water decoction group significantly decrease compared with the model group.And the levels of IL-6,TNF-α, IL-1β in the ethyl acetate group obviously reduce. In the n-butyl alcohol group only the level of TNF-α was obviously lower. The inflammatory factors of water layer group did not change significantly.(2) The serum fingerprints of each dosage group rats are analyzed by PCA of unsupervised discriminant model.It found that the water decoction of the Green Forsythiae Fructus and ethyl acetate part have adjust the trend of blank group in inhaled endotoxin inflammation model rats, and have play a certain anti- inflammatory effect. While n-butyl alcohol part has no obvious effect.3、The research of serum pharmacochemistry in the Green Forsythiae Fructus and Ripe Forsythiae Fructus.This study showed that the components go into the blood from model group of Green Forsythiae Fructus regardless of number or the content of some components were significantly higher than the model group of Ripe Forsythiae Fructus.There are 28 transitional components in the model group serum more than 17 transitional elements in the normal group serum of Green Forsythiae Fructus.And the content of some components are much higher than normal group serum.The model group and normal group of Ripe Forsythiae Fructus both have 15 transitional components in serum. And the ingredients are basically identical. Study also found that the absorption rate of Forsythoside A,Forsythoside B,phillyrin,rutin are lower after oral medication, and very few quantity can be into the blood.While the relative content of Forsythiaside and Quercetin in blood improve obviously.It maybe related to phillyrin and rutin is metabolized into Forsythiaside and Quercetin.Conclusions: The comparison by pharmacodynamics system shows that the functions of Green Forsythiae Fructus resist acute inflammation, endotoxin in vitro and sweat are better than the Ripe Forsythiae Fructus.The function of resisted chronic inflammation is slightly better than the Ripe Forsythiae Fructus.The Green Forsythiae Fructus exert antipyretic effect faster than the Ripe Forsythiae Fructus,but it have no obvious difference between the degree of antipyretic. The Ripe Forsythiae Fructus reduce the activity of Alanine Transaminase is better than the Green Forsythiae Fructus. With increasing doses, the function of the Green Forsythiae Fructus and Ripe Forsythiae Fructus reduce the activity of Alanine Transaminase have no obvious difference.Compound authentication further clear that the anti-inflammatory effect of Green Forsythiae Fructus is superior to the Ripe Forsythiae Fructus, and the removing swelling and lump effect of Ripe Forsythiae Fructus is better than Green Forsythiae Fructus.The experiment of serum pharmaco-chemistry found that the components go into the blood from inflammatory model group of Green Forsythiae Fructus regardless of number or the content of some components were significantly higher than the model group of Ripe Forsythiae Fructus.While they are hardly no difference in normal rat serum. While the relative content of Forsythiaside and Quercetin in blood are high,they may be the material basis of the anti-inflammatory effect. It found that the ethyl acetate part is the active ingredient of anti-inflamatory effect in the experiment of filtrate the effective parts of anti-inflammatory effect of Green Forsythiae Fructus. And the Forsythiaside and Quercetin are concentraded in the ethyl acetate part.The Green Forsythiae Fructus mainly through regulate creatine, glycerophosphoryl choline,Succinic acid and Trimethyl-amine oxide to exert anti-inflammatory effects. |
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