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OBJECTIVE To investigate the anti-pulmonary fibrosis effect of linarin in vivo and in vitro， and investigate its mechanism preliminarily. METHODS C57BL/6J mice were randomly divided into normal group （carboxymethylcellulose sodium）， model group （carboxymethylcellulose sodium）， positive control group （pirfenidone， 200 mg/kg）， linarin low-dose and high-dose groups （12.5， 25 mg/kg）， with 8 mice in each group. Except for normal group， pulmonary fibrosis model was induced in other groups. After modeling， they were given relevant medicine intragastrically， once a day， for consecutive 14 d. The general situation of mice was observed， and their lung indexes were measured； the levels of tumor necrosis factor-α （TNF-α） and transforming growth factor-β1（ TGF-β1） in serum and interleukin-6 （IL-6） in lung tissue were determined. Hematoxylin-eosin （HE） staining and Masson staining were used to observe the histopathological morphology of lung. The pulmonary fibrosis was scored according to Ashcroft score standard. The expressions of α-smooth muscle actin （α-SMA） and （type Ⅰ collagen， Collagen Ⅰ）， phosphorylated extracellular signal-regulated kinase （p-ERK1/2） and TGF-β1 in lung tissues were detected. HFL1 cells were stimulated by TGF- β1 to form pulmonary fibrosis model in vitro， which were divided into normal group， model group and linarin low-， medium- and high-concentration groups （3.7， 7.4， 14.8 mg/L）. After being cultured for 48 h， the protein expressions of α-SMA， Collagen Ⅰ and p-ERK1/2 in HFL1 cells were detected. RESULTS In vivo， compared with normal group， the lung index of model group and the levels of TNF- α， TGF- β1 and IL-6 were significantly increased （P＜0.01）. There were a large number of inflammatory infiltration and cellular fibrosis lesions in the alveoli， and a large number of collagen depositions. The scores of HE staining and Masson staining were significantly increased （P＜0.01）. The protein expressions of α-SMA， Collagen Ⅰ， p-ERK1/2 and TGF-β1 in lung tissue were up-regulated significantly （P＜0.01）. Compared with model group， above indexes of mice were improved significantly in linarin high-dose group （P＜0.05 or P＜0.01）， and most of indexes （except for lung index） were improved significantly in linarin low-dose group （P＜0.05 or P＜0.01）. In vitro， compared with blank group， the density of cells in the model group increased， and obvious proliferation and other changes occurred； protein expressions of α-SMA， Collagen Ⅰ and p-ERK1/2 were significantly up-regulated （P＜0.05 or P＜0.01）. Compared with model group， the cell density of each concentration group was decreased and the morphology gradually returned to normal； the expressions of above proteins in linarin high-concentration group and the protein expression of p-ERK1/2 in linarin medium-concentration group were down-regulated significantly（P＜0.05 or P＜0.01）. CONCLUSIONS Linarin may regulate ERK and inflammatory pathways to reduce the inflammatory response， thereby exerting anti-pulmonary fibrosis effect.
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Pulmonary fibrosis is the end-stage manifestation of a large class of lung diseases characterized by fibroblast proliferation and accumulation of a large amount of extracellular matrix accompanied by inflammatory injury and tissue structure destruction. Studies have shown that flavonoids have anti-pulmonary fibrosis effects through multiple paths， including dihydromyricetin， morin and fisetin can inhibit fibroblast differentiation； Trollius altaicus flavonoids， hesperidin and linarin can play an anti-inflammatory role； total flavonoids from Scutellaria baicalensis， scutellarin and chrysin can inhibit epithelial- mesenchymal transition； total flavonoids of Litchi chinensis， diosmin and silybin can play an anti-oxidative stress role； quercetin， baicalin and apigenin can regulate autophagy； total flavonoids of Oxytropis falcata， calycosin and dihydroquercetin can regulate apoptosis； naringin， scutellarin and total flavonoids of Dracocephalum moldavica can inhibit pyroptosis， thus exerting anti- pulmonary fibrosis effects.
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OBJECTIVE:To study the safety of percutaneous administration of Hongzhi gutong cataplasm. METHODS:Rab-bits were taken for single dose in complete skin irritation test(n=4),single dose in damaged skin irritation test(n=4)and multi-ple doses in complete skin irritation test(n=4). The left and right sides of the skin respectively paste 3 cm×3 cm blank matrix and Hongzhi gutong cataplasm for 24 h(calculated by crude drug of 0.14 g). After removing tape 1,24,48,72 h,the erythema and edema in hair removal site of rabbits in the former 2 tests were observed;after 24 h of administration,the rabbits in the last group were administrated again after exposing the administration area for 1 h,repeated 3 times,the erythema and edema in hair removal site after removing tape the first,second time and 1,24,48,72 h in the third time were respectively observed. RESULTS:In the 3 experiments,the scores of erythema and edema of all rabbits were 0,and skin irritation was evaluated as no irritation. CONCLU-SIONS:Hongzhi gutong cataplasm has no skin irritation in rabbits.
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OBJECTIVE:To study the chemical constituents of 70％ ethanol extract of Breynia fruticosa.METHODS:The 70％ ethanol extract of B.fruticosa were isolated and purified by D101 macroporous resin,silica gel column chromatography,RP-silica gel column chromatography,Sephadex LH-20 gel column chromatography,preparative HPLC.The structure of compound was analyzed and identified according to physicochemical characters and spectral data.RESULTS:10 compounds were separated from 70％ ethanol extract of B.fruticosa,such as Luteolin (1),Quercetin (2),Kaempferol (3),Tiliroside (4),(+)-Lyoniresinol (5),(+)-Isolariciresinol (6),(+)-Nortrachelogenin (7),(+)-Syringaresinol (8),Icariol A2 (9),5,5'-Dimethoxy-7-oxolariciresinol (10),respectively.CONCLUSIONS:Ten compounds are isolated from this plant for the first time.The study play the found for quality evaluation of 70 ％ ethanol extract of B.fruticosa.
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This study was aimed to investigate the research on pharmacological effects, relevant ideas and methods of Guangdong native heat-clearing and toxin-removing herbs. Literatures on pharmacological effects of Guangdong native heat-clearing and toxin-removing herbs were collected, summarized and analyzed. The results showed that most Guangdong native heat-clearing and toxin-removing herbs had obvious effects of anti-microbial, anti-bacterial endotoxin, anti-inflammatory, and antipyretic effect. It also had obvious antivenomous and analgesia effect. Based on research ideas and methods of Guangdong native heat-clearing and toxin-removing herbs, we clarified the confusion species as soon as possible, and adhered to the whole animal experiments in combination with in vitro experiments and computer molecular docking simulations for the complementation of each other. It was concluded that the study on pharmacological effects of Guangdongnative heat-clearing and toxin-removing herbs provided strong support in its clinical application. Ideas and methods provided in this article was the main way to explain pharmacological effects of Guangdong native heat-clearing and toxin-removing herbs.
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OBJECTIVE:To establish a RP-HPLC method for the determination of hydroxy safflor yellow A in Orthopae_dics lotion 1.METHODS:The separation was performed on Phenomenex Luna C18 with mobile phase composed of methanol-acetonitrile-water(26∶ 2∶ 72).The flow rate was 1.0ml/min;the detective wavelength was 403nm and the column temperature was 30℃.RESULTS:At a sample size of 0.1 044? g～ 1.2 528? g(r=0.9 998),hydroxy safflor yellow A was noted to be of good linear relation with peak area score.The average recovery was 98.08%(RSD=0.52%).CONCLUSION:The method is simple,accurate,specific,sensitive,reproducible,and suitable for the quality control of Orthopaedics lotion 1.
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Objective To establish the methods for TLC identification and contents determination of Compound Yantongxiao Spray.Methods Flos Lonicera,Borneolum Syntheticum and Menthol in the spray were identified by TLC,and the content of chlorogenic acid was determined by HPLC.Results The TLC characteristic spots of Flos Lonicera,Borneolum Syntheticum and Menthol can be identified.For content determination,the linear range of chlorogenic acid was in 0.08～0.28 ?g(r=0.999 0),the average recovery of chlorogenic acid was 102.34 %(n=6)and RSD was 2.03 %.Conclusions The methods are simple,accurate,specific and reproducible,can be used for the quality control of Compound Yantongxiao Spray.