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Objective: To study the chemical constituents from the fruits of Solanum virginianum. Methods: By means of preparative HPTLC and column chromatography over silica gel and Sephadex LH-20, compounds were isolated and purified. Their structures were elucidated by physico-chemical properties and spectral analyses. Results: Twelve compounds were obtained and identified as: 5-hydroxy-8-methoxy-6,7-methylenedioxyflavone (1), 7-hydroxy-6-methoxy coumarin (2), fraxetin (3), 5-hydroxy- 6,7,3',4'-tetramethoxyflavone (4), 5-hydroxy-4',6,7-trimethoxyflavone (5), dihydro-N-feruloyltyramine (6), N-trans-coumaroyltyramine (7), 5,3'-dihydroxy-6,7,4'-tritermethoxyflavone (8), N-[2-(3,4-dihydroxyphenyl)-2-hydroxyethyl]-3-(4-methoxyphenyl)-prop-2-enamide (9), N-trans-coumaroyloctopamine (10), 5,7,4'-trihydroxy-6-methoxyflavone (11), and 5,7,4'-trihydroxy-8-methoxyflavone (12). Conclusion: Compound 1 is a new flavonoid, named as solacarpumon, and compounds 2-12 are isolated from Solanum virginianum for the first time.
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Objective: To study the coumarin from the seeds oil leavings of Xanthoceras sorbifolia. Methods: The chemical constituents were isolated and purified by combination of silica gel, macroporous resin, Sephadex LH-20, and ODS column chromatography. Their structures were elucidated by spectral and chemical methods. The cytotoxicity of the new compound against 10 selected human cancer cell lines was assayed. Results: Five comarins were isolated and identified as fraxetin-7-O-β-D-[6’-(3’'‑hydroxyl‑3’’- methylglutaryl)] glucopyranoside (1), fraxoside (2), fraxetin (3), scopoline (4), and esculetin (5), respectively. Conclusion: Compound 1 is a new compound. Unfortunately, this compound exhibited no cytotoxicity with tested cell lines.
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BACKGROUND: Fraxetin (7,8-dihydroxy-6-methoxy coumarin), a coumarin derivative, has been reported to possess antioxidative, anti-inflammatory and neuroprotective effects. A number of recent observations suggest that the induction of heme oxygenase-1 (HO-1) inhibits inflammation and tumorigenesis. In the present study, we determined the effect of fraxetin on HO-1 expression in HaCaT human keratinocytes and investigated its underlying molecular mechanisms. METHODS: Reverse transcriptase-PCR and Western blot analysis were performed to detect HO-1 mRNA and protein expression, respectively. Cell viability was measured by the MTS test. The induction of intracellular reactive oxygen species (ROS) by fraxetin was evaluated by 2′,7′-dichlorofluorescin diacetate staining. RESULTS: Fraxetin upregulated mRNA and protein expression of HO-1. Incubation with fraxetin induced the localization of nuclear factor-erythroid-2-related factor-2 (Nrf2) in the nucleus and increased the antioxidant response element-reporter gene activity. Fraxetin also induced the phosphorylation of Akt and AMP-activated protein kinase (AMPK)α and diminished the expression of phosphatase and tensin homolog, a negative regulator of Akt. Pharmacological inhibition of Akt and AMPKα abrogated fraxetin-induced expression of HO-1 and nuclear localization of Nrf2. Furthermore, fraxetin generated ROS in a concentration-dependent manner. CONCLUSIONS: Fraxetin induces HO-1 expression through activation of Akt/Nrf2 or AMPKα/Nrf2 pathway in HaCaT cells.
Subject(s)
Humans , AMP-Activated Protein Kinases , Blotting, Western , Carcinogenesis , Cell Survival , Heme Oxygenase-1 , Heme , Inflammation , Keratinocytes , Neuroprotective Agents , Phosphorylation , Reactive Oxygen Species , RNA, MessengerABSTRACT
Objective To investigate the effect of fraxetin on primary cardiomyocyte hypertrophy induced by phenylephrine . Methods Primary SD cardiomyocyte hypertrophy was induced by phenylephrine ,and we observed the effects of fraxetin on cardio‐myocyte hypertrophy induced by phenylephrine .Image‐ProPlus 5 measured the area of cardiomyocyte;[3 H ]‐leucine incorporation assay detected the protein synthesis rate of cardiomyocyte;Real‐time PCR measured the Nrf2 and molecular markers (ANP ,BNP) mRNA expression levels of cardiomyyocyte hypertrophy .Results (1)Primary neonate SD Cardiomyocyte hypertrophy model was successfully established by 80 μmol/L phenylephrine for 48 h ,and Nrf2 expression levels significantly increased in cardiomyocyte hypertrophy model;(2)The increase of cardiomyocyte area ,protein synthesis rate and molecular markers expression of cardiomyyo‐cyte hypertrophy were significantly inhibited by fraxetin in a dose‐dependent manner .Conclusion Fraxetin could significantly inhib‐it the cardiomyyocyte hypertrophy induced by PE .
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Objective: To optimize the purification process of total coumarin from Fraxini Cortex using macroporous resin. Methods: The single factor methods have been used to investigate the choice of type, adsorption performance, and desorption performance and the purification of the total coumarin from Fraxini Cortex by macroporous resin. The adsorption rate, resolution, resolution rate, and transfer rate of the total coumarin from Fraxini Cortex, four kinds of coumarin constituents, such as aesculin, aesculetin, fraxin, and fraxetin were used as examining indexes. Results: The ADS-5 was the most suitable type for the purification of total coumarin from Fraxini Cortex among the seven kinds of macroporous resin. Adsorption parameters: Crude drug-the resin was 0.8 g/g which was the sample amount; The concentration of sample solution was 0.75 g crude drug/mL; The pH value of sample liquid was 4.0-4.3 (liquid sample); The speed of the sample through the resin column was 2-4 BV/h. Elution parameters: The volume of the water cleaning fluid impurities was 1 BV; The elution solvent was 25% ethanol; The elution speed was 2 BV/h; The elution volume was 3 BV. After the purification, the transfer rate of total coumarin from Fraxini Cortex was 74.27%, the transfer rate of four kinds of coumarin was 83.06%, the extract rate of total coumarin was 7.35%, the removal of impurities was 14.00%, among which the content of total coumarin was 54.72%, the contents of the four kinds of components were 36.01%, the total coumarin extraction yield was 4.02%. Conclusion: This method to purify the total coumarin from Fraxini Cortex using ADS-5 can get better purification effect, the purification process is also stable.
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OBJECTIVE: To study the chemical constituents of Sapium sebiferum leaves. METHODS: The chemical constituents in the petroleum ether and n-butyl alcohol parts of the 95% ethanol extract of Sapium sebiferum leaves were isolated and purified by chromatographic methods. Their structures were elucidated by spectral data and physicochemical properties. RESULTS: Twelve compounds were purified and identified as squalene(1), 3β-hydroxyglutin-5-ene(2), fraxetin(3), friedelin(4), β-sitosterol(5), gallic acid ethyl ester (6), quercetin (7), 5-hydroxymethylfurfural (8), blumenol C glucoside (9), kaempferol-3-O-β-D-glucopyranoside (10), 1'-O-benzyl-α-L-rhamnopyranosyl-(1″-6') -β-D-glucopyranoside(11), and shikimic acid(12). CONCLUSION: Compounds 1-3, and 8-12 are isolated for the first time from this plant.
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OBJECTIVE: To investigate the chemical constituents from the roots of Actinidia chinensis. METHODS: The compounds were isolated and purified by column chromatography and their structures were elucidated by spectroscopic methods. RESULTS: Eight compounds were obtained from the aqueous extract of the roots of Actinidia chinensis.. The structures were determined as(-)-epi-catechin(1), (+)-catechin(2), fraxetin(3), escaletin(4), protocatechuic aldehyde(5), (-)-epi-catechin-5-O-β-D-glucopyranoside(6), erythro-1, 2-bis-(4-hydroxy-3-methoxyphenyl)-1, 3-propanediol(7), and threo-1, 2-bis-(4-hydroxy-3-methoxyphenyl)-1, 3-propanediol(8). CONCLUSION: Compounds 3 - 8 are isolated from the roots of Actinidia chinensis for the first time.
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Objective: To study the chemical constituents in the seeds of Datura metel. Methods: The constituents were isolated and purified by silica gel, ODS, and Sephadex LH-20 column chromatographies as well as HPLC. Their chemical structures were elucidated on the basis of spectral data. Results: The compounds were isolated from the EtOAc fraction of D. metel extract and identified as cannabisin D (1), cannabisin E (2), cis-cannabisin E (3), cannabisin F (4), cannabisin L (5), cannabisin G (6), grossamide K (7), hyoscyamilactol (8), daturaolone (9), N-trans-feruloyl tryptamine (10), and fraxetin (11), respectively. Conclusion: Compounds 2 and 4 are firstly isolated from the plants in Solanaceae, compounds 1, 3, and 5-7 are firstly isolated from the plants in genus Datura L. and compounds 8-11 are isolated from this plant for the first time.
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The determination of fraxetin A and fraxetin B in Cortex Fraxini have been carried out by HPLC on the stationary phase:octodecyl-silicohydride bonded silica gel column. The mobile phase was methanol-water(24:76). The detection wavelength was at 348nm. There was a good linear relationship in a concentration range of 16?g/ml~176?g/ml. The correlation coefficients were 0. 9995 and 0. 9994,respectively. The recovery of the added sample were 99. 1 ?1. 5% (n=5) for fraxetin A and 99.8?2. 5%(n=5) for fraxetin B. This method showed 0. 8% of within-day accuracy and 6. 2% of between-day accuracy,involving the advantages of simplicity,quickness and accuracy.