Research Progress in Pharmacology of Aesculin and Aesculetin / 中药新药与临床药理

Cortex Fraxini,a kind of traditional Chinese medicinal,has low toxicity and wide clinical application.It is widely used to treat diseases such as swelling and pain of eye,damp-heat diarrhea,leucorrhea with reddish discharge,metrorrhagia,etc..Modern pharmacological studies have found that coumarin compounds are the main active components of Fraxini Cortex,among which aesculin and aesculetin are the most representative components.Numerous studies have reported that aesculin and aesculetin exhibit abundant pharmacological activities including antibacterial,anti-inflammatory,anti-tumor,antioxidant,and the potential development and utilization of these compounds has attracted increasing attention.This paper summarized the research progress of the main pharmacological effects of aesculin and aesculetin by reviewing the relevant literature at home and abroad.Our aim is to provide a reference for the drug development and clinical application of Fraxini Cortex.

Analysis on Quality Standard of Fraxini Cortex（Fraxinus chinensis） Dispensing Granules Based on Standard Decoction / 中国实验方剂学杂志

ObjectiveTo establish the quality standard for Fraxini Cortex（Fraxinus chinensis） dispensing granules based on standard decoction， and to provide a basis for the quality control of this dispensing granules. MethodHigh performance liquid chromatography（HPLC） specific chromatograms of 15 batches of Fraxini Cortex（F. chinensis） standard decoctions and 3 batches of Fraxini Cortex（F. chinensis） dispensing granules were established with the mobile phase of 0.1% phosphoric acid aqueous solution（A）-acetonitrile（B） for gradient elution（0-10 min， 12%-15%B； 10-30 min， 15%-32%B） and the detection wavelength of 220 nm. And similarity evaluation， cluster analysis and principal component analysis（PCA） were also carried out. HPLC quantitative analysis of multi-components by single marker（QAMS） was established to determine the contents of the main components in the standard decoctions and dispensing granules. The contents of the corresponding components in Fraxini Cortex（F. chinensis） decoction pieces were also detected， and the transfer rates from decoction pieces to standard decoctions and dispensing granules were calculated. ResultThe similarities between specific chromatograms of 15 batches of Fraxini Cortex（F. chinensis） standard decoctions and 3 batches of Fraxini Cortex（F. chinensis） dispensing granules were all>0.9， and 7 common peaks were identified. The results of cluster analysis and PCA showed that there was some differences in the composition of different batches of standard decoctions， but did not show aggregation of origin. As the standard decoctions， the extract rate was 6.18%-11.62%， the contents of esculin， syringin， fraxin， esculetin， fraxetin， calceolarioside B were 44.92-103.51， 1.36-11.87， 33.26-90.73， 4.63-29.75， 2.40-16.86， 2.49-17.35 mg·g-1， and the transfer rates from decoction pieces to standard decoction were 25.21%-42.54%， 52.57%-88.84%， 43.43%-79.45%， 49.15%-88.27%， 49.22%-72.69%， 27.66%-47.67%， respectively. The extract rates of Fraxini Cortex（F. chinensis） dispensing granules were 10.4%-10.7%， the transfer rates of the above six components from decoction pieces to dispensing granules were 42.76%-43.17%， 80.01%-80.90%， 59.59%-59.88%， 51.35%-52.67%， 60.50%-60.93%， 37.98%-38.37%， respectively， which were generally consistent with the transfer rates from decoction pieces to standard decoctions. ConclusionThe established quality control standard of Fraxini Cortex（F. chinensis） dispensing granules based on standard decoctions is reasonable and reliable， which can provide reference for the quality control and process research of this dispensing granules.

Effect of Integration of Habitat Processing and Pieces Processing on Anti-inflammatory of Cortex Fraxini / 世界科学技术-中医药现代化

Objective: To compare the anti-inflammatory effect of Fraxini Cortex pieces between integrated production process and traditional processing method. Methods: The model of rat paw swelling induced by carrageenan was used to study the anti-inflammatory and swelling reliving effects of water extracts of Cortex Fraxini with different methods. The main chemical components of the 2 kinds of Cortex Fraxini herbal pieces were determined by high performance liquid phase. Results: Compared with the blank group, the water extracts of the 2 kinds of Cortex Fraxini could reduce the swelling of the rats and improve the various indicators of inflammation. However, the anti-inflammatory and swelling reliving effects of the integrated processing of Cortex Fraxini were more significant. The contents of 4 main active ingredients of esculine, fraxin, aesculetin and fraxetin in the integrated processing of Cortex Fraxini were higher than that of the traditionally processed Cortex Fraxini. The total amount of 4 kinds of coumarins in the integrated Cortex Fraxini was about 1.5 times that of the traditionally processed water extract of Cortex Fraxini. Conclusion: The integrated processing and traditional processing of Cortex Fraxini have similar effects on anti-inflammatory effects, and have the superiority of reducing the loss of active ingredients, which is worthy of popularization and application.

Optimization of integrative technology of primary processing for Fraxini Cortex based on response surface methodology / 中草药

Objective To optimize the processing integration technology of Fraxini Cortex based on response surface methodology. Methods The single factor experiment combined with Box-Behnken design was used to optimize the integrative technology, with five major characteristic components (aesculin, aesculetin, fraxetin, fraxin, and total coumarin) as indexes, in order to detect three factors (cutting thickness, drying temperature, and drying time), and research the effect of analgesic and anti-inflammatory of processing integration Fraxini Cortex. Results Optimum integrative technology of primary processing was as follows: cutting 6 mm Fraxini Cortex, and drying for 3.25 h at 75 ℃. The processing integration Fraxini Cortex significantly decreased the times of wrinkle reaction induced by acetic acid in mice, prolonged the latent period, and obviously or partially inhibited the feet swelling degree induced by carrageenan in rats. The analgesic effect of integrated technology group was more obvious than traditional technology group (P < 0.05). Conclusion This optimized integrative technology of Fraxini Cortex is reasonable and feasible with high accuracy. It could provide the scientific basis and innovative idea to the large-scale production of decoction pieces of Chinese materia medica and have the certain value for its promotion and application.

Advance in studies on chemical constituents of Fraxini Cortex and their pharmacological effects / 中草药

Fraxini Cortex is widely distributed in China and rich in resources, and is a kind of medicinal plants with great utilization value. From the phytochemical view, the secondary metabolites such as coumarins, lignans, secoiridoids, phenylethanoids, flavonoids, phenolic acids, and triterpenoids had been reported from this species. Its pharmacological research mainly focused on the antibacterial, antiphlogistic, anti-oxidative, lowing-uric acid, diuretic, and antineoplastic activities. The present paper reviews the phytochemistry and biological activities of Fraxini Cortex through accessing Web of Science and multiple databases for biomedicinal sciences.

Preparation, in vitro and in vivo studies of Fraxini cortex thermosensitive in-situ-forming eye gel / 中国药学杂志

OBJECTIVE: To study on characterization, irritation, the release mechanism and the elimination kinetics of Fraxini Cortex thermosensitive in-situ-forming eye gel (FC-ISG). METHODS: The non-membrane dissolution model was used to observe the release mechanism of FC-ISG. The stabilities of FC-ISG were investigated under following circumstances bright light, freeze test and accelerating test. Single-dose and multiple-dose irritations of FC-ISG were evaluated by draize test. The elimination kinetics of FC-ISG were analyzed by non-compartment model. RESULTS: FC-ISG showed good stability and non-stimulation to rabbit eyes. Drug release from FC-ISG was completely controlled by gel erosion, the release kinetics was coincided with zero-level release. AUC and MRT in FC-ISG group were significantly higher than those in control group (P<0.05). CONCLUSIONS: FC-ISG can improve the bioavailability of drug by prolonging the residence retention time of drug in cornea. FC-ISG shows a great potential in ocular application.

Study on Content Determination of Coumarin in Fraxini Cortex Extract / 中国中医药信息杂志

Objective To establish a UV spectrophotometry method and an HPLC method respectively for the determination of the total content of coumarin and contents of four main constituents of coumarin in Fraxini Cortex extract.Methods UV spectrophotometry was used for the determination of the content of total coumarin in Fraxini Cortex extract. The reference substance was Aesculin, and the maximum ultraviolet absorption wavelength was 334 nm. The HPLC method was used to determine the contents of Aesculin, Fraxin, Aesculetin and Fraxetin in Fraxini Cortex extract, using gradient elution with acetonitrile-phosphate solution (0.01%) as mobile phase on Agilent ZORBAX SB-C18 chromatographic column (4.6 mm × 250 mm, 5μm) at room temperature.Results For the UV method, the linear range of the mass concentration of Aesculin was 5.76-23.04μg/mL (r=0.999 9), and the average recovery was 100.6% (RSD=1.8%). For the HPLC method, the linear ranges of the mass of Aesculin, Fraxin, Aesculetin and Fraxetin were 0.055 0-3.850 0μg (r=0.9997), 0.053 9-3.773 0μg (r=0.999 8), 0.060 0-0.660 0μg (r=0.999 9), and 0.056 2-0.618 2μg (r=0.999 9), respectively, and the average recoveries were 96.97% (RSD=1.26%), 100.80% (RSD=2.22%), 99.04% (RSD=2.47%), and 98.77% (RSD=1.94%), respectively.Conclusion Both of the two methods are simple, accurate and reliable, and can be used for the quality control of total coumarin and the main constituents of coumarin in Fraxini Cortex extract.

Purification process of total coumarin from Fraxini Cortex by macroporous resin / 中草药

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.

Comparison on HPLC fingerprints between fraxini cortex and its eye drop / 中草药·英文版

Objective: To compare the HPLC fingerprints of Fraxini Cortex and its eye drop. Methods: Using esculin and esculetin as reference substances, HPLC method was established for fingerprint chromatography of Fraxini Cortex and its eye drop. The similarity was analyzed by similarity evaluation and system cluster analysis. Results: For Fraxini Cortex, eight peaks were separated, among which four common peaks were obtained; for eye drop, eleven peaks were separated including six common peaks. Similarities of both fingerprints were good. Cluster analysis further showed that different sources resulted in the variance of ingredients in crude drug. Both materials and eye drop had some common peaks such as esculin and esculetin, on the other hand, they had some different peaks which might be caused by extracting process. Conclusion: HPLC fingerprint chromatogram could be applied for the quality control of Fraxini Cortex and its preparations; the pharmaceutical process may be responsible for the variance of ingredients. © 2013 Tianjin Press of Chinese Herbal Medicines.