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Pancreatic lipase (PL), a crucial enzyme in the digestive system of mammals, has been proven as a therapeutic target to prevent and treat obesity. The purpose of this study is to evaluate and characterize the PL inhibition activities of the major constituents from Fructus Psoraleae (FP), one of the most frequently used Chinese herbs with lipid-lowering activity. To this end, a total of eleven major constituents isolated from Fructus Psoraleae have been obtained and their inhibition potentials against PL have been assayed by a fluorescence-based assay. Among all tested compounds, isobavachalcone, bavachalcone and corylifol A displayed strong inhibition on PL (IC < 10 μmol·L). Inhibition kinetic analyses demonstrated that isobavachalcone, bavachalcone and corylifol A acted as mixed inhibitors against PL-mediated 4-methylumbelliferyl oleate (4-MUO) hydrolysis, with the K values of 1.61, 3.77 and 10.16 μmol·L, respectively. Furthermore, docking simulations indicated that two chalcones (isobavachalcone and bavachalcone) could interact with the key residues located in the catalytic cavity of PL via hydrogen binding and hydrophobic interactions. Collectively, these finding provided solid evidence to support that Fructus Psoraleae contained bioactive compounds with lipid-lowering effects via targeting PL, and also suggested that the chalcones in Fructus Psoraleae could be used as ideal leading compounds to develop novel PL inhibitors.
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Objective: To analyze and identify the chemical constituents from Fructus Psraleae(FP)in the rat liver after intragastric FP administration, and explore the potential mechanism of FP- induced hepatotoxicity via the network toxicology study. Methods: UPLC-QTOF-MS and UNIFI data screening platform were used to quickly identify the chemical constituents from FP in the rat liver afte intragastric FP administration, and multiple databases were used to search for information about chemical component targets, hepatotoxic targets, component hepatotoxic common targets and indirect targets. The construction of protein protein interaction (PPI)network and the enrichment analysis of gene ontology(GO)biological function and Kyoto Encycolpenia of Genes and Genomes (KEGG)pathway were carried out on the searched targets by using the String database and Cytoscape 3.6.1 software to explore the key targets and potential mechanism of hepatotoxicity induced by constituents from FP. Results: Eleven prototypic components of FP were identified in the rat liver. The network toxicology studies showed that there were a total of 52 potential targets and 23 pathways for the FP hepatotoxicity, among which ALB, HOMX1, GSR, GSTM3 and CYP2C9 targets, as well as the thyroid synthesis pathway and the glutathione metabolism pathway had a strong correlation with the FP hepatotoxicity. Conclusion: By UPLC-QTOF-MS combined with the UNIFI platform, the 11 chemical constituents from FP could be quickly identified in the liver of rats that were intragastrically administered FP, and the network toxicology study has predicted potential molecular mechanism of the hepatotoxicity induced by FP. The present results provide a reference for further study the hepatotoxicity of FP.
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OBJECTIVE To study the effect of the ethanol extract of Fructus Psoraleae(EEFP)on endogenous metabolites in rat urine based on metabolomics. METHODS Male SD rats were orally administered with EEFP at the doses of 0.54,1.08 and 1.62 g · kg-1,respectively,once a day for two consecutive weeks. Urine samples were collected for 12 h after the last administration. Data were acquired with the MassLynx software based on ultra-performance liquid chromatography quadrupole-time-of-flight mass spectrometry(UPLC-Q-TOF-MS). The principal component analysis(PCA)and partial least squares-discriminant analysis(PLS-DA)were used to analyze the difference of endogenous metabolites in different groups,then putative biomarkers were found through the orthogonal partial least-squares-discriminant analysis(OPLS-DA),variable importance in the projection(VIP)and t test and their relative intensity were determined. RESULTS The results of PCA showed that samples of each group were clustered,all the groups were separated,and that the distance between the EEFP groups and the blank control group was increased in a dose-dependent manner. The relative contents of p-cresol glucuronide and galactose-beta-1,4-xylose were 40.0 ± 11.2,2.7 ± 2.6,16.8 ± 6.3 and 45.9 ± 16.4,32.6±22.1,8.0±8.3 in the EEFP 0.54,1.08 and 1.62 g·kg-1 groups,respectively,significantly lower than those of the control group,which were 107.0 ± 26.9 and 82.3 ± 13.6(P<0.01),respectively. The relative contents of 5-L-glutamyl-taurine,and gluconolactone were 22.4 ± 10.0,47.6 ± 19.1 and 138.2 ± 18.8,337.3±64.0 in EEFP 1.08 and 1.62 g·kg-1groups,respectively,significantly higher than those of the blank control group,which were 2.6±1.6 and 20.5±6.8,respectively(P<0.01). The relative content of D-pantothenoyl-L-cysteine was 74.2 ± 31.5 in the EEFP 1.62 g · kg-1 group,significantly higher than that in the blank control group(0.6±0.5)(P<0.01). As the dose of EEFP increased,D-pantothenoyl-L-cysteine,5-L-glutamyl-taurine,and gluconolactone had an upward trend(P<0.01),while galactose-beta-1,4-xylose and p-cresol glucuronide had a downward trend(P<0.01). CONCLUSION The two-week administration of EEFP has effect on the endogenous metabolites in urine. The substances identified are mainly related to energy metabolism,taurine,tyrosine and glucose metabolism.
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Objective:To develop a method for determining deoxynivalenol in four kinds of traditional Chinese herbal medicines. Methods:After being extracted by water, purified by an immunoaffinity column, deoxynivalenol was analyzed by LC-MS-MS. Results:The calibration curve was linear within the range of 2-50 ng·ml-1 for deoxynivalenol. The recovery was 68. 7%-88. 3%. Conclusion:The method is simple, sensitive and accurate in the determination of deoxynivalenol in Semen Ziziphi Spinosae, Semen Sojae Praepara-tum, Semen Coicis and Fructus Psoraleae.
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Objective To provide scientific evidence for the identification and development of fructus psoraleae through its pharmacognostical study.Methods To identify fructus psoraleae by paraffin section and powder method,meanwhile,morphological identification and physical and chemical identification were also adopted.Results The morphological and microscopic characteristics of transverse section and powder of fructus psoraleae were described; fluorescent speckles of the same color were found in the same place of test samples and psoralen and isopsoralen reference by thin layer chromatography; results of water and ash determination all complied with Chinese pharmacopoeia specification,water and 70％ ethanol extractives were 21.93～39.68％,22.03～31.77％,respectively.Conclusion The established method was simple and practical with reliable results,and suitable for the identification of fructus psoraleae.
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A simple, sensitive and selective method of high-performance liquid chromatography (HPLC) has been successfully developed for separation of bavachinin enantiomers in Fructus Psoraleae and rat plasma. The separation and detection conditions of HPLC were optimized. Chiral bavachinin were separated with the mobile phase of methanol and water (70:30, v/v) at a flow rate of 1.0 mL/min. The linear ranges were in the range of 20-1000 mg/mL. The detection limits were tested as 4 ng/mL and 6 ng/mL for (t)-bavachinin and (à)-bavachinin, respectively. The method has been applied to analyze chiral bavachinin in rat plasma. HPLC-MS method was used to test the accuracy.
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The qualitative and quantitative analysis of active constituents in Fructus Psoraleae is presented by high-performance liquid chromatography (HPLC) coupled with different detections.Extracts of Fructus Psoraleae were examined by HPLC with ion trap mass spectrometry (IT-MS) and 18 major compounds of coumarins,benzofuran glycosides,flavonoids,and meroterpene were identified.The determination of four major constituents including bavachin,isobavachalcone,bavachinin,and bakuchiol was accomplished by HPLC with UV,MS,and electrochemical detection (ECD).These methods were evaluated for a number of validation characteristics (repeatability,LOD,calibration range,and recovery).ECD obtained a high sensitivity for analysis of the four components; MS provided a high selectivity and sensitivity for determination of bavachin,isobavachalcone,and bavachinin in negative-ion mode.After optimization of the methods,separation,identification.and quantification of the four components in Fructus Psoraleae were comprehensively tested by HPLC with UV,MS,and ECD.
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OBJECTIVE:To establish a method for the determination of the content of total Flavonoid in Fructus Psoraleae by UV spectrophotometry.METHODS:The determination was performed using Bavachin standard as control substance,and sodium hydroxide as color-developing agent,with the wavelength set at 440nm.RESULTS:The absorbency and concentration of Bavachin have good linearity in the range of 4.10～ 12.30? g? mL-1(r=0.999 8).The average recovery rate was 100.5%(RSD=1.57%,n=9).CONCLUSION:The method is easy to operate,highly accurate,reproducible and can be applied to determine the content of total Flavonoid in Fufang Psoralen corylifolia sustained-release tablets.
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Objective To study the quality control standard of Gushuling capsule. Methods Fructus Psoraleae and Fructus Ligustri Lucidi in Gushuling capsule were identified by TLC; The content of ieariin was determined by HPLC with acetonitrile-water (30: 70) as mobile phase and the wavelength at 270 nm. Results TLC identification was positive; the linear range of icariin was 0.0968～0.4840 ?g(r=0.9999), the average recovery was 97.27%(RSD=1.88%, n=5). Conclusion This method can be used as a standard of the quality control for Gushuling capsule.
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Objective To screen out the effective constituents with estrogenic action in Fructus psoraleae. Methods Fructus psoraleae was separated by using systemic solvent distillation method, and the effective fraction was screened out by the experiment of increasing the uterine weight in mice. Then the petroleum fraction was separated by sil; ca gel chromatrography and the effective constituent was screened by the experiment of increasing the uterine weight in mice. Results High-dose(5g/kg) of the petroleum fraction showed obvious estrogenic action (P
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Objective To establish a HPLC method for the assay of psoralen and isopsoralen in different effective extracts of Fructus Psoraleae. Methods HPLC was carried out on the column of Kromasil RP-C18. The mobile phase was methanol -water(65 ∶35). The flow rate was 1.0 mL/min and the UV detection wavelength was 245 nm. Results Good linearity of psoralen was showed within the range of 10.5 ng～525 ng(r= 0.999 3)and isopsoralen within the range of 9 ng～450 ng (r= 0. 999 9). The content of psoralen and isopsoralen differed in different extractions of Fructus Psoraleae. Among them,the extract C (extracted by ethyl acetate ) contained the highest contents of psoralen and isopsoralen,while the contents of psoralen and isopsoralen were very low in the extract D (extracted by n-butyl alcohol) and E (supernatant of water extract). Conclusion The method is simple,accurate and reproducible. The anti-asthma effect and the dose-effect relationship of the different effective extracts of Fructus Psoralea need further pharmacodynamics study.
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Objective To investigate the effect of Fructus Psoraleae on the proliferation and differentiation of cultured osteoblast isolated from neonatal rat's calvarium.Methods Calvarium osteoblasts of new born SD rat were cultured and exposed to different concentrations of Fructus Psoraleae extract,then the content of alkaline phosphatase(ALP)in the cell was measured and the cell proliferation was detected by tetrazoline colorimetry(MTT).Results Ethyl acetate extract and alcohol extract from Fructus Psoraleae can improve the activity of ALP and the proliferation of rat's cultured osteoblasts,the optimum concentration was 2.0?10-3 mg/mL.Conclusion Ethyl acetate extract and alcohol extract from Fructus Psoraleae can stimulate the differentiation and proliferation of osteoblasts in vitro.