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OBJECTIVE@#The compatibility of Eucommia ulmoides (Eu) and Psoralea corylifolia (Pc) on the pharmacokinetic (PK) properties in the rat was explored in this study.@*METHODS@#Eu extract, Pc extract and the combined extracts (crude drug ratio was 2:1) was administered by gavage, respectively. Two PK experiments were conducted. In first one, the blood samples were collected via the occuli chorioideae vein to get the PK properties of the components. In second one, the blood samples were simultaneously collected via the internal jugular vein or portal vein at different time points and the concentrations of target ingredients were detected by LC/MS/MS to clear the location where the interaction of Eu and Pc took place in vivo.@*RESULTS@#Eight of 11 ingredients in Eu and Pc extract were determined in rat plasma. The exposure levels of geniposidic acid (GPA), aucubin (AU), geniposide (GP), pinoresinol diglucoside (PDG), psoralen glycosides (PLG) and isopsoralen glycosides (IPLG) were decreased 1/5-2/3 after administration of combined extracts. Comparing to the combined administration, the exposure of GPA and AU in plasma of single Eu administration collected via the portal vein were decreased 1/3-2/3, and the values of AUC0-24h and AUC0-∞ of GP collected from the portal vein or internal jugular vein were double increased. The other components' parameters were not significantly changed.@*CONCLUSION@#In summary, the Pc and Eu combined administration could affect the exposure of the main components of Eu extract in rats due to the changed intestinal absorption. The research on the compatibility of Pc and Eu was helpful to guide the clinical administration of Eu and Pc simultaneously.
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Aim: To investigate the regulation effect and molecular mechanism of corylin on NLRP3, NL-RC4, AIM2 inflammasomes with immortalized bone marrow-derived macrophages. Methods: The effect of corylin on the NLRP3, NLRC4, AIM2 inflammasome activation was evaluated with LPS-induced ATP, nigericin, salmonella, poly(dA: dT). Caspase-1 activity was determined by Caspase-Glo® 1 Inflammasome Assay. Western blot was performed to observe the protein expression levels of mature IL-1β, caspase-1 p20 in the culture supernatants, pro-caspase-1, pro-IL-1β, ASC, NLRP3 in the cell lysates. Results: Corylin blocked the self-slicing of pro-caspase-1 induced by ATP, nigericin, salmonella and poly(dA: dT), then suppressed the secretion of mature IL-1β mediated by caspase-1, which showed that corylin inhibited the NL-RP3, NLRC4, AIM2 inflammasomes activation. Moreover, corylin irreversibly attenuated the activation of NLRP3 inflammasome without affecting NF-κB signaling pathway. Conclusions: Corylin inhibits the inflammasome activation of NLRP3, NLRC4, and AIM2, and further reduces its mediated immune inflammatory response. Meanwhile, it provides new ideas and strategies for the treatment of immune inflammatory diseases by using corylin-related preparations.
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Objective To analyze and identify the transitional constituents of combination Psoralea corylifolia-Myristica fragrans in vivo and in vitro, and further study the effect of this combination on transitional components. Methods A rapid ultra-performance liquid chromatography/orthogonal acceleration time-of-flight mass spectrometry (UPLC-Q-TOF/MS) method was established to rapidly analyze constituents of before and after combination P. corylifolia-M. fragrans after oral administration in rats, and combined with Peakview software analysis. Results Compared with in vitro extract of P. corylifolia, there are 15 prototypes absorbed into the blood. Compared with in vitro combination P. corylifolia-M. fragrans extract, 26 prototype components were absorbed into the blood. Compared with M. fragrans extract, six prototype components were absorbed into the blood. Conclusion By using UPLC-Q-TOF/MS method, the main chemical constituents from the combination can be rapidly and accurately identified, and the results would facilitate the quality control of combination P. corylifolia-M. fragrans for safe and efficient use.
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OBJECTIVE: To investigate active constituents of Psoralea corylifolia L. against osteoporosis using chromatography capture combined with zebrafish model. METHODS: High performance liquid chromatography (HPLC) was used for analysis and capture components of Psoralea corylifolia L. including coumarins, flavonoids and bakuchiol, and which anti-osteoporosis activity was evaluated by zebrafish model induced by 25 μmol•L-1 prednisolone, 25 μmol•L-1 prednisolone as model group, and 0.4% DMSO medium as vehicle group. Bone of juvenile zebrafish cultured to 8 dpf (day post fertilization) were stained with alizarin red, and inspected with optical microscope, and bone staining area was quantitative analyzed using image software. RESULTS: The RESULTS showed that coumarins and flavonoids can significantly resist bone loss of zebrafish by prednisolone, while the action of bakuchiol was relative weak with heavy toxicity, high dose of bakuchiol led to zebrafish larval death. CONCLUSION HPLC can system analysis and capture ingredients/components of Psoralea corylifolia L., and zebrafish osteoporosis model can evaluate activity of micro ingredients/components, combination of these two METHODS: can broke through double bottleneck of complex components capture and activity evaluation in vivo. It is expected to realize efficient anti-osteoporosis screening of the whole component of Chinese herbal medicine.
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Objective: To establish the chromatographic fingerprint of components of drug-couple Psoralea corylifolia-Myristica fragrants (PC-MF) absorbed into blood by UPLC. Methods: Twenty SD rats were administered with 10 different batches of PC-MF respectively. The UPLC profiles of serum samples were collected after treatment of PC-MF, blank serum samples and methanol extract were compared, and the transitional constituents to blood and their metabolites were analyzed. Results: The fingerprint of PC-MF was established. Thirteen common peaks were identified and the similarities were over 0.90. The 10 peaks from the in vitro test were prototype components in the product, and three peaks were metabolites. Conclusion: The serum fingerprint of PC-MF is established for the first time. It reflects the oral administration absorption into the blood and provides some data on pharamacodynamic basis study in vivo for PC-MF.
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Objective To observe the effect of raw and salt-processed of psoralen on the function of liver and kidney and the expression of aquaporins 5 (AQP5), AQP4, and AQP2 in the kidney-yang deficiency model rats. Methods Used hydrocortisone made deficiency of kidney-YANG model rats, total protein (TP), albumin (Alb) and aspartate aminotransferase (AST), alanine aminotransferase (ALT), serum creatinine (Scr), and urea nitrogen (BUN) content in serum of rats were determined by chemical reagent method. The expression of AQP5, AQP4, and AQP2 were detected by qRT-PCR. Results The levels of ALT and AST in the raw and salt-processed of psoralen groups increased significantly, and Alb decreased significantly compared with model group (P andlt; 0.05); The levels of ALT and AST in the salt-processed of psoralen group were lower than that in the raw psoralen group; the levels of BUN and Scr in the treated group were significantly higher than that in the model group (P andlt; 0.05). The expression of mRNA for AQP2 and AQP4 of model group was decreased significantly (P andlt; 0.05) compared with control group, and expression of AQP5 mRNA increased significantly (P andlt; 0.05). The expression of AQP4 mRNA in raw psoralen group was significantly higher than that in model group (P andlt; 0.05), and AQP5 mRNA was significantly lower than that in model group (P andlt; 0.05). Moreover, the expression of AQP2 and AQP5 mRNA of salt-processed of psoralen group was significantly higher than that of the raw psoralen group (P andlt; 0.05), and AQP4 mRNA expression was significantly lower than that of salt-processed of psoralen group (P andlt; 0.05). Conclusion Salt-processed of psoralen can reduce the side effects of drugs on liver and kidney function in kidney-yang deficiency model rats, it can also alleviate the dryness of raw psoralen. The relief of dryness by salt-processed of psoralen may be related to the regulation of the gene expression of aquaporins in vivo.
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OBJECTIVE To investigate the bone development activity and differences in safety of ethanol extract (EE) and water decoction (WD) of Psoralea corylifolia L.efficiently.METHODS Zebrafish larvae were co-exposed to prednisolone 25 μmol· L-1 and different concentrations of EE and WD (0.1,1.0,10 and 100 mg crude drug· L-1),and etidronate disodium (ED) 30 mg·L-1.All these groups were incubated at 28.5℃ until 9 dpf.The medium solution was changed every other day.Zebrafish skeleton at 9 dpf was stained with alizarin red and inspected under an optical microscope,in addition,the death toll and organ toxicity of zebrafish were also observed.The mRNA expression of osteoprotegrin (OPG) and receptor activator of NF-κB ligand (RANKL) in 9 dpf zebrafish were determined with fluorescence quantitative PCR.Zebrafish embryos (1 dpf) were exposed to various concentrations of EE (10,20,30,35,40,50 and 60 mg crude drug· L-1),WD (10,50,100,125,150,175,200 and 500 mg crude drug· L-1),psoralen (12.5,25.0,50.0,100.0,200.0 and 400.0 μmol·L-1) and bakuchiol (1,5,10,25 and 50 μmol· L-1).Embryonic morphology of zebrafish (3 dpf) was inspected with an optical microscope and the death toll of embryos or larvale was counted from 2 dpf to 9 dpf and LC50was calculated.Components of EE and WD ware analyzed by HPLC method.RESULTS Both EE (0.1 mg crude drug· L-1) and WD (1.0 mg crude drug· L-1) groups could increase the staining area and optical density values of zebrafish skeleton compared with prednisolone group (P＜0.01),indicating the increase in bone mineralization;the OPG mRNA expression in both EE and WD (1.0 mg crude drug· L-1) groups increased,while the RANKL mRNA expression decreased (P＜0.01) and the ratio of OPG/RANKL improved obviously (P＜0.01).Embryos exposed to EE,WD,psoralen and bakuchiol showed swelling of the heart and yalk sac,and decrease in GOT.The LC50 of WD and psoralen was 5～8 and 5～21 times that EE and bakuchiol,respectively.The composition and relative content of EE and WD also varied considerably.CONCLUSION Bone development activity and toxicity of EE are both stronger than those of WD.The lipid soluble characteristic components of Psoralea corylifolia L.,may be critical components of toxicity.
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This study aimed at evaluating the effect of different processing methods on the contents of antiosteoporotic compositions in P.corylifolia.HPLC method adopted to analyze the contents of antiosteoporotic compositions,including coumarin (psoralen and isopsoralen),flavonoids (neobavaisoflavone,corylifolin,corylifolinin and corylifol A) and meroterpenes (bakuchiol) in P.corylifolia.The contents were analyzed before and after the processing methods.Results:The results showed that the content of coumarin,flavonoids and meroterpenes obviously changed in different processed P.Corylifolia in comparison with the crude drugs.In conclusion,it was demonstrated that the therapeutic efficacy of osteoporosis was enhanced by CP method which increased all of the three compositions.The testimony tallied with the Chinese medical theory:stir-frying with salt-water could enhance the effect of the tonification of spleen and kidney.
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Objective: For the purpose of finding new bioactive agents from Chinese herbal medicine, the chemical study on Psoralea corylifolia was carried out. Methods: The chemical constituents in the fruits of P. corylifolia were isolated by silica gel, MCI-GEL resin, Sephadex LH-20 column chromatography, and high performance liquid chromatography (HPLC) methods. The structures of compounds were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Results: A new isoflavanone, 3R-6-hydroxy-8-(hydroxymethyl)-4',7-dimethoxy-dihydrogenisoflavone (1) was isolated from the fruit of P. corylifolia. Conclusion: Compound 1 is a new compound named corylisoflavone A, which displays the cytotoxicity against NB4, SH-SY5Y, PC3, A549, and MCF7 cells with IC50 values of 12.6, 5.3, 15.5, 4.8, and 11.2 μmol/L, respectively.
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This study was aimed to establish the ultra high performance liquid chromatography (UHPLC) fingerprints of Psoralea corylifolia L. The separation was achieved on a Shim-pack XR-ODS Ⅲ column (50 mm í 2.0 mm, 1.6μm) by gradient elution with acetonitrile-0.2% glacial acetic acid solution as the mobile phase. The flow rate was 0.1 mL·min-1 and the measurement wavelength was 246 nm. The temperature of the column was 45oC. The results showed that the UHPLC fingerprint of P. corylifolia L. was established and 10 characteristic common peaks were found, among which 6 peaks were recognized by comparing with reference substances. It was concluded that the method was rapid, reliable and reproducible. The established fingerprint can provide references for the study of sub-stance basis and quality control of P. c orylifolia L.
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Objective To find direct effect of Chinese herbs Bu Gu Zhi (Psoralea corylifolia L) and Bai Zhi (Dahurian angelica root) Extracts on melanocyte adhesion and migration in vitro. Methods Ethanol extracts obtained from two kind of Chinese medicinable herbs were tested. Human melanocytes were obtained from neonatal foreskins and 48-well culture dish covered with fibronectin were used to perform melanocyte adhesion assay; Motility was assessed using the micropore filter method. Results: The extracts of Bu Gu Zhi(Psoralea corylifolia L), Bai Zhi(Dahurian angelica root) obviously showed an effect in increasing of human melanocyte adhesion and migration on fibronectin. Conclusion It is suggested that Buguzhi(Fructus Psoraleae) and Baizhi(Radix Angelicae Dahuricae) might induce melanocyte adhesion and/or migration in the treatment of vitiligo.