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Objective: To establish a blood-brain barrier (BBB) model for screening the effective ingredients of total salvianolic acids components probably effecting central nervous system (CNS), so as to provide basis for the rapid high throughput screening of CNS drugs. Methods: The permeability parameters and transendothelial electrical resistance (TEER) values showed that the co-cultured human brain microvascular endothelial cells (HBMEC)/HA (human astrocytes) model was of integrity and vitality. The active components in total salvianolic acids were screened with this in vitro BBB model, and then analyzed by HPLC-MS. Results: HA induced HBMEC to produce higher TEER in the first 10 d up to 300 Ω/cm2, sodium fluorescein was used to detect the formation of tight junctions of endothelial cells, and the permeability coefficient of its cross-vitro BBB model was (2.659 ± 0.730) × 10-3 cm/min. We found that six compounds at least from total salvianolic acids could permeate across BBB model, in which danshensu, protocatechuic acid, caffeic acid, isoferulic acid, lithospermic acid, and rosmarinicacid were identified. Conclusion: The co-cultured HBMEC/HA model combined with HPLC-MS analysis is a potential tool for screening of BBB permeable drug candidates from plant-derived materials.
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Objective To investigate the effects of different processing methods on contents of main chemical components isoferulic acid in Cimicifuga heracleifolia. Methods Cimicifuga heracleifolia from the same batch were prepared by processing method. HPLC were used to determine the contents of isoferulic acid in crudes samples, wine-prepared samples, vinegar-prepared samples, and carbonized samples. Results The contents of isoferulic acid of crudes samples and the three different processed products were in the order as follows:carbonized samples (0.404 7%)>vinegar-prepared samples (0.302 3%)>wine-prepared samples (0.262 4%)>crudes samples (0.231 3%). Conclusion Different processing methods had certain effects on the content of isoferulic acid in Cimicifuga heracleifolia.
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Objective: To search for the bioactive compounds from the vine of Lonicera dasystyla. Methods: The compounds were isolated and purified by column chromatography on silica gel, sephadex LH-20 gel, and ODS, and their structures were elucidated on the basis of spectroscopic analysis, such as MS, NMR, etc. Results: Nine compounds were isolated from the vine of L. dasystyla. Their structures were identified as dihydrosesamin-9-O-β-D-glucopyranoside (1), isoferulic acid (2), p-methoxycoumaric acid (3), kaempferol-7-O-(2″-E-p-coumaroyl)-α-L-arabinofuranoside (4), macranthoidin B (5), loganin (6), kaempferol (7), acacetin (8), and quercetin (9). Conclusion: All of these compounds belong to four types, phenylpropanoids (1-3), flavonoids (4, 7-9), triterpenoid saponin (5), and iridoid (6). Compound 1 is a new one and compounds 5 and 6 as marker compounds exist in most of Lonicera Linn. plants, while known compounds 2-4 and 8 were isolated from Lonicera Linn. plants for the first time. The identification of these chemicals lays the foundation for searching bioactive compounds of this plant, and these compounds have great importance for chemotaxonomy of this plant.
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Objective: To study the chemical constituents from Sibiraea laevigata. Methods: The compounds were isolated by column chromatography and their structures were elucidated through spectroscopic analysis (NMR). Results: Twelve compounds were isolated and identified with spectral analysis and compared with authentic samples as lauric acid 1-monoglyceride (1), n-nonane (2), ethyl caffeate (3), isoferulic acid (4), methyl ferulic acid (5), p-methoxy cinnamic acid (6), ω-hydroxypropiovanillone (7), 3-hydroxy-1-(4-hydroxy-3, 5-dimethoxyphenyl)-1-propanone (8), (+)-pinoresinol (9), bis (2-ethylhexyl) phthalate (10), 9α- hydroxymedioresinol (11), and C-veratroylglycol (12). Conclusion: All compounds are found from the plant for the first time, and compounds 9-12 are found from the plants of Sibiraea Maxim. for the first time. The results provide the new chemical evidences for the bioactive investigation of this plant.
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Objective: To observe the action characteristics of ferulic acid and isoferulic acid on cytochrome P450 isoenzymes1A1 and 3A4 (CYP1A1, CYP3A4) in HepG2 cells. Methods: MTT colorimetry was used to investigate the effects of ferulic acid and isoferulic acid at different concentration on the proliferation of in vitro cultured HepG2 cells. Flow cytometry was used to determine the effects of ferulic acid and isoferulic acid on cell cycle of human liver HepG2 cells; The expression of CYP1A1 and CYP3A4 mRNA was tested by real time quantitative PCR technology after drug treatment and then CYP3A4 protein expression was detected by protein immunoblot method (Western blotting). Results: HepG2 cells were inhibited by ferulic acid and isoferulic acid after 48 h action, with a clear dose-response relationship; Two drugs (50 μg/mL) blocked HepG2 cell cycle in G2-M phase; All of the concentration (100, 50, and 25 μg/mL) of the two drugs were CYP1A1 and CYP3A4 mRNA inhibitors; After cells were disposed by the two kinds of drugs (50 μg/mL) with 48 h, protein expression was significantly lower than that in the control group; And compared with the control group, the expression amounts of ferulic acid and isoferulic acid were 0.57 and 0.39. Conclusion: The proliferation of HepG2 cells is inhibited by the two drugs, and the cell cycle was arrested at G2/M phase, which that may be one of its mechanisms, so as to inhibit the mRNA expression of CYP1A1 and CYP3A4. At the same time, both of them could inhibit the protein expression of CYP3A4, as well as the effect degree of difference is bigger, which may be associated with its hydroxyl and the methoxyl isomerisation.
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Trans-isoferulic acid was isolated from the carbon tetrachloride soluble fraction of a methanol extract of the rhizomes of Curcuma longa (Zingiberaceae). The structure of the isolated compound was elucidated by comprehensive analysis of spectroscopic data. This is the first report of its occurrence from this plant.
El ácido trans-isoferulico fue aislado de la fracción soluble en tetracloruro de carbono del extracto metanólico de los rizomas de Curcuma Longa (Zingeraceae). La estructura del compuesto aislado fue elucidada por análisis de los datos espectroscópicos. Este es el primer reporte de su presencia en esta planta.