Pharmacokinetic study about compatibility of Eucommia ulmoides and Psoralea corylifolia / 中草药·英文版

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.

Extraction of effective components of Psoralea corylifolia and efficacy evaluation in the treatment of vitiligo / 中国药房

OBJECTIVE To extract the effective components of Psoralea corylifolia and evaluate its efficacy in the treatment of vitiligo. METHODS The concentrations of psoralen， isopsoralen， neobavaisoflavone， corylin， psoralidin， corylifolinin， and bakuchiol in P. corylifolia extract were determined by ultra-performance liquid chromatography. Based on the analytic hierarchy process （AHP） and Plackett-Burman design， with the concentrations of the 7 components as evaluation indexes and the crushing degree， ethanol concentration， and soaking time as factors， the extraction process of P. corylifolia was optimized by Box-Behnken response surface methodology and the validation test was conducted. Zebrafish were divided into blank control group， positive control group （8-methoxypsoralen， 10.8 μg/mL）， and low-， medium-， and high-concentration groups of P. corylifolia extract （500， 1 000， 2 000 μg/mL）， with 6 fish in each group. The effects of P. corylifolia extract on the melanin production of zebrafish were studied by density analysis. RESULTS The best extraction process was P. corylifolia powder over 60 meshes and soaked in 80% ethanol for 72 hours. The average comprehensive score of three validation experiments was 98.27， with an RSD of 1.36%， and the relative error was 1.02% compared with the predicted value of the fitting equation （97.28）. Compared with the blank control group， the melanin pigmentation of zebrafish in the low-， medium-， and high-concentration groups of P. corylifolia extract was significantly increased （P＜0.01）. CONCLUSIONS The optimized extraction process of P. corylifolia is reasonable and feasible， and the obtained P. corylifolia extract can significantly promote the production of melanin in zebrafish.

Study on the objectivity and biological mechanism of Psoralea corylifolia Linn.'s 'Great dryness damages the liver' / 药学学报

According to the theory of 'Xingben Dazao' of Psoralea corylifolia Linn. (BL), the susceptible syndromes and biomarkers of liver injury caused by BL were searched. Rat models of kidney-yin deficiency syndrome (M_yin) and kidney-yang deficiency syndrome (M_yang) were established, and all animal experimental operations and welfare following the provisions of the First Affiliated Experimental Animal Ethics and Animal Welfare Committee of Henan University of Traditional Chinese Medicine (No. YFYDW2020017). The results showed that BL significantly decreased the body weight, water intake, and urine weight of M_yin rats and increase the organ indexes of the liver, testis, adrenal gland, and spleen and the expression of alanine aminotransferase (ALT). Meantime, BL significantly increased the urine weight of M_yang rats and decreased the expression of ALT and aspartate aminotransferase (AST). Hematoxylin and eosin (HE) staining showed that BL could aggravate inflammatory infiltration of hepatocytes in rats with M_yin and alleviate liver injury in rats with M_yang. Metabolomics identified 17 BL co-regulated significant differential metabolic markers in M_yin and M_yang rats. Among them, 8 metabolites such as glutamine, quinolinate, biliverdin, and lactosylceramide showed opposite trends, mainly involving cysteine and methionine metabolism, tyrosine metabolism, tryptophan metabolism, purine metabolism, sphingolipid metabolism, glycerol phospholipid metabolism, glutamine metabolism, and other pathways. M_yin/M_yang may be the susceptible constitution of BL for liver damage or protection, which may be related to the regulation of amino acid metabolism and sphingolipid metabolism. The study can provide some experimental data support for the safe and accurate use of BL in the clinical practice of traditional Chinese medicine.

Study on chemical compositions and hepatotoxicity of water extract and ethanol precipitate of processed products of Psoralea corylifolia / 中国药房

OBJECTIVE To study the content changes of 5 chemical compositions in water extract and ethanol precipitate of different processed products of Psoralea corylifolia， and to preliminarily evaluate its hepatotoxicity. METHODS The water extracts from crude product of P. corylifolia and processed products by Leigong method， running water rinsing method， and salt stir-frying method were prepared， as well as the ethanol precipitates of processed products by Leigong method and salt stir-frying method were prepared. The contents of psoralenoside， isopsoralenoside， psoralen， isopsoralen and bakuchiol were determined by high- performance liquid chromatography and compared. The median lethal concentration （LC50） and maximum non-lethal concentration （MNLC） of each sample to wild-type zebrafish juveniles were calculated after 72 h of treatment with different concentrations of water extracts from raw product and processed products by running water rinsing method， Leigong method and salt stir-frying method， different concentrations of ethanol precipitates from processed products by Leigong method and salt stir-frying method， and the acetaminophen was used as the positive control. The basic morphology of wild-type zebrafish juveniles and the liver phenotype of transgenic zebrafish juveniles were observed after 72 h of treatment with the above samples （MNLC）. Pearson correlation analysis was used to evaluate the correlation between component content and hepatotoxicity. RESULTS Compared with the water extract of raw products， the contents of psoralenoside and isopsoralenoside in the water extract of different processed products were generally decreased （P＜0.05）， while the contents of psoralen， isopsoralen and bakuchiol in the ethanol precipitate of Leigong method and salt stir-frying products were significantly increased （P＜0.05）. The LC50 of water extracts of crude product and processed products by running water rinsing method， Leigong method， salt stir-frying method， and ethanol precipitates of processed products by Leigong method and salt stir- frying method were 2.45， 5.00， 5.38， 1.55， 2.36， 0.64 g/L （calculated by crude drug）， and MNLC were 2.21， 4.53， 5.02， 1.37， 2.13， 0.53 g/L （calculated by crude drug）. Compared with the blank control group， the zebrafish juveniles in each sample treatment group showed different degrees of deformity， the liver relative fluorescence intensity was significantly weakened （P＜0.05 or P＜ 0.01）. Fat-soluble components such as bakuchiol， isopsoralen and psoralen were highly correlated with liver fluorescence intensity （R 2＞0.7）. CONCLUSIONS The processed products of P. corylifolia mainly compose of psoralenoside and isopsoralenoside after water extraction， the contents of psoralen， isopsoralen and bakuchiol increase after alcohol precipitation， and the hepatotoxicity is positively correlated with the contents of liposoluble compositions in P. corylifolia.

Evaluation of three different remineralizing agents on artificially demineralized enamel lesions Using scanning electron microscopy-energy dispersive X-ray and magic-angle spinning nuclear magnetic resonance - An in vitro study

Aim: Demineralization can be arrested or reversed when remineralization agents are applied to incipient carious or noncavitated carious lesions. A large number of therapeutic agents, including nonfluoridated products, have been developed to promote enamel remineralization. This study aims to evaluate the efficacy of different remineralizing agents on artificially demineralized enamel lesions. Materials and Methods: The present in vitro study was conducted on 75 sound premolars divided into three groups of normal, demineralized (n = 15 each), and remineralized teeth (n = 45). The remineralized teeth were further subdivided into three groups (n = 15) as remineralized with 2% sodium fluoride (NaF), 2% NaF, and Psoralea corylifolia (bakuchi) and white mineral trioxide aggregate. Specimens of each group were treated with the above-mentioned remineralizing agents and then subjected to Vickers hardness number (VHN), scanning electron microscopy–energy dispersive X-ray (SEM-EDX), and magic-angle spinning nuclear magnetic resonance (MAS-NMR) for further evaluation. Results: The test results showed significantly the highest VHN and the emission peak of elements under the EDX test, such as calcium, phosphorous, oxygen, and fluorine with remineralized with NaF + bakuchi. MAS-NMR spectra showed fluorine and phosphorous peak in a group with NaF + bakuchi indicative of the increase in remineralization. NaF + bakuchi showed effective results in VHN, SEM-EDX, and MAS-NMR with no antagonist interaction. Conclusion: Thus, P. Corylifolia presents an advantage in enhancing remineralization and inhibiting demineralization for early carious lesions and can be used as a herbal extract for effective reduction in pathogenic bacteria.

Mechanism of Psoralea corylifolia Linn on liver injury based on bioinformatics / 药学实践杂志

Objective To explore the mechanism of Psoralea corylifolia Linn (PCL) on liver injury by establishing the biological function and pathway network of PCL components, targets and protein interactions based on bioinformatics. Methods The components of PCL and potential liver-injury related targets were collected from TCMIP database. The targets of PCL were predicted by the reverse pharmacophore matching method. Cytoscape software was applied for the construction of active components-targets network map. Protein-protein interaction network was constructed by STRING database. Gene ontology functional enrichment analysis and KEGG pathway enrichment analysis were conducted to predict the liver injury mechanism of PCL. Results 22 components were identified from PCL with the corresponding 31 potential liver injury targets, mainly on serum albumin (ALB), glutathione S-transferase P (GSTP1), transthyretin (TTR) and peroxisome proliferator activated receptor gamma (PPARG) by PPI network analysis. The chemical carcinogenesis, adenosine 5 '- monophosphate activated protein kinase (AMPK) signal, PPAR signal, liver enzyme P450 and its harmful substance metabolism, glutathione metabolism and other signaling pathways were selected by KEGG analysis. Conclusion The active components of PCL may target on ALB, GSTP1, TTR and PPARG to regulate AMPK and PPAR signaling pathways, leading to liver injury.

Effects of compatibility of Schisandra chinensis on Psoralea corylifolia -induced oxidative damage and endoplasmic reticulum stress in hepatocytes / 中国药房

OBJECTIVE To study the effects of the compatibility of Schisandra chinensis on Psoralea corylifolia -induced oxidative damage and endoplasmic reticulum stress in L 02 hepatocytes，and to provide reference for clinical use of the compatibility attenuation of P. corylifolia -S. chinensis . METHODS L02 cells were divided into blank control group ，P. corylifolia model group （1 200 μg/mL P. corylifolia ，calculated by crude drug ），P. corylifolia -S. chinensis low-dose，medium-dose and high-dose groups （1 200 μg/mL P. corylifolia combined with 600，1 200，2 400 μg/mL S. chinensis ，respectively，calculated by crude drug ）. After the cells in each group were cultured in culture medium or drug solution for 48 hours，the levels of aspartate aminotransferase（AST）and alanine aminotransferase （ALT）were detected ；the levels of glutathione （GSH），superoxide dismutase （SOD）and malondialdehyde （MDA）in cell culture medium were detected ；reactive oxygen species （ROS）level and mitochondrial membrane potential in cells were detected ；mRNA and protein expressions of glucose-regulated protein 78（GRP-78）and protein kinase R-like endoplasmic reticulum kinase （PERK）were detected. RESULTS Compared with blank control group ，the levels of AST，ALT，MDA and ROS ，mRNA and protein expressions of GRP- 78 and PERK were increased significantly in P. corylifolia model group （P＜0.05 or P＜0.01）；while GSH and SOD levels ，mitochondrial membrane potential were decreased significantly （P＜0.05 or P＜0.01）. Compared with P. corylifolia model group ，above indexes of P. corylifolia -S. chinensis low-dose， medium-dose and high-dose groups were all improved significantly （P＜0.05 or P＜0.01）. CONCLUSIONS The compatibility of P. corylifolia -S. chinensis can alleviate P. corylifolia -induced oxidative damage and endoplasmic reticulum stress of L 02 cells.

Effect of psoralen corylifolia on nonalcoholic steatohepatitis in young mice and its possible mechanism / 中国医师杂志

Objective:To study the protective effect and possible mechanism of psoralen corylifolia on non-alcoholic steatohepatitis (NASH) induced by high-fat diet in mice.Methods:The newly weaned female mice in the offspring of C57BL/6J mice fed with normal diet were selected as the control group (gavage of distilled water); the newly weaned female mice in the offspring of C57BL/6J mice fed with high-fat diet were randomly divided into model group (gavage distilled water), low-dose group[psoralen corylifolia 1.125 mg/(g·d)], high-dose group [psoralen corylifolia 2.25 mg/(g·d)] and vitamin E group [vitamin E 0.01 mg/(g·d)]. Six mice in each group were fed continuously for 8 weeks. Automatic biochemical analyzer was used to detect serum alanine aminotransferase (ALT), aspartate transaminase (AST), triglyceride (TG), total cholesterol (TC) level in mice; The liver tissue pathological changes were observed by hematoxylin-eosin (HE) and Sirius-red (SR) staining; The level of reactive oxygen species (ROS) in liver tissue was detected by dihydroethidium (DHE) fluorescence probe; the activity of NADPH oxidase was detected by kit; The protein expressions of nuclear factor-κB (NF-κB), phosphatidylinositol 3 kinase (PI3K p85), protein kinase B (Akt), P47 phox and protein kinase C-α (PKC-α) were detected by Western blot.Western blot. Results:The levels of serum ALT, AST, TG, TC and homeostasis model assessment of insulin resistance (HOMA-IR) index in the model group were higher than those in the control group (all P<0.01). After treatment, the levels of serum ALT, AST, TG, TC and HOMA-IR in low-dose group, high- dose group and vitamin E group were lower than those in model group (all P<0.05). HE and SR staining showed that hepatocytes in the model group were swollen, and there were lipid droplets of different sizes, vacuoles and obvious fibrosis. After treatment, hepatocyte steatosis and fibrosis decreased and the contents of ROS and NADPH oxidase in liver decreased(all P<0.05); Western blot showed that the p-p65/p65, p-Akt/Akt, p-PKC-α/PKC-α, PI3K, p85 and P47 phox protein expression in the model group were higher than those in the control group (all P<0.01). After treatment, the protein expression levels of p-p65/p65, p-Akt/Akt, p-PKC-α/PKC-α, PI3K, p85 and P47 phox decreased (all P<0.01). Among the above indexes, the protective effect of high-dose group on liver NASH was better than those of vitamin E group and low-dose group (all P<0.05). Conclusions:Psoralen corylifolia can improve the liver function of NASH model mice, which may be related to the inhibition of oxidative stress, inflammatory reaction and liver fibrosis, which provides a new idea for the prevention and treatment of children with NASH.

An Experimental Study Of Vrikshayurveda Seed Treatments On Germination Rate And Active Ingredient Of Bakuchi (psoralea Corylifolia Linn.) By Hplc Method

Bakuchi (Psoralea corylifolia Linn.) is one of the important endangered medicinal plants used in Ayurveda and other Traditional systems. Its cultivation and propagation is difficult due to its low germination rate (5-7%) & prolonged seed dormancy. Bakuchi seeds made into 5 groups, the experiment was conducted in a complete randomized block design with 5 treatments and 5 replications totally 500 seeds in each group) & observed for 50 days. Control Group 1 no- seed treatment, Group 2- Standard treated with 1% conc H2SO4, Group 3 Vrikshayurvedic treatment done by soaking in milk subsequently fumigation of Vidanga & Ghee, Group 4- treated with paste of Brihati, Tila, Kamalanaala, Ghee & Group 5 treated by soaking in milk subsequently Cow dung, Vidanga & Honey applied. Number of seeds germinated, germination percentage, emergence index and relative seed germination parameters were observed. HPLC studies carried out of post harvested Bakuchi seeds of all 5 groups to know the effect of seed treatments on Psoralen content quantitatively. Overall results indicates that Group 4 (8.000 ± 0.8367) seeds soaked in 12 hrs milk followed by application of Brihati, Tila, Kamalanaala & Ghee paste for 12 hrs treatment is statistically significant (P value>0.05) in comparison with group 2 (4.600 ± 0.6782) Sulphuric acid treatment and Group 3 (4.200± 0.9165) fumigation with Honey & Vidanga. Rest of the groups shown insignificant changes on germination parameters. HPLC Results found that generally seed treatments may reduce the content of Psoralen as in control (Group 1) maximum percentage (0.04%w/w) of Psoralen is noticed. Among treatment groups Group 4 contains maximum (0.027%w/w) Psoralen next to control (0.039%w/w). Psoralen content is very less in standard Group 2 (0.022%w/w), Group 3 (0.023%w/w) & Group 4 (0.024%w/w). Maximum germination percentage was observed in Group 4 in comparison with the Group 2conventional method of treating with sulphuric acid. Estimation of Psoralen contents in the seeds from the plants grown by various treated seeds reveled that Group 4 is qualitatively better than standard, but inferior to the control, standard & other Vrikshayurveda seed treatment techniques used in the current experiment.

Regulation and mechanism of corylin on inflammasomes / 中国药理学通报

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.

Effect of isopsoralen on hepatic function and bile acid transporters in SD rats with different administration periods / 中国药理学通报

Aim: To investigate the effect of isopsoralen, the active ingredient of Psoralea corylifolia, on rat liver and bile acid transporters after oral administration for different time. Methods: Rats were randomly divided into four groups; the control group and the groups treated with 60 mg · kg-1 isopsoralen for 1, 3 or 7 days. After the experiment, the body weight and liver weight were measured. The levels of ALT, AST, ALP, TBA, TC, TG and TBIL in rat serum were examined by different kits. The mRNA levels of BSEP, NTCP, MRP2, MRP4, MDR1, ABCG5, ABCG8 and OSTa in rat liver were detected by real-time PCR. Results: Compared with control group, isopsoralen could induce the increase of liver weight and liver/body weight ratio. The levels of ALT, AST, TBA, TG and TBIL significantly increased after administration of isopsoralen. The content of ALP did not change significantly and the content of TC decreased remarkably. Furthermore, the level of AST significantly increased after one day of isopsoralen administration. After treatment with isopsoralen, the mRNA levels of BSEP, NT-CP, MRP2, MDR1, ABCG5, ABCG8 and OSTa were distinctly reduced. The mRNA levels of MRP4 showed no significant difference. Conclusions: The administration of isopsoralen for 1 to 3 days may cause obvious liver injury. The mechanism underlying isopsoralen-induced injury may be associated with the interference of bile acid transporters.

Highly Efficient Screening Anti-osteoporosis Activity Components of Psoralea corylifolia L. Based on Zebrafish Model Combined with HPLC Capture / 中国药学杂志

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.

UPLC-Q-TOF/MS analysis on transitional constituents of before and after combination Psoralea corylifolia-Myristica fragrans absorbed into plasma / 中草药

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.

Simultaneous Determination of Bavachin and Bakuchiol in Psorslea corylifolia by HPLC / 中国药房

OBJECTIVE:To establish a method for content determination of bavachin and bakuchiol in Psoralea corylifolia.METHODS:HPLC method was adopted.The determination was performed on Shim-Pack VP-ODS column with mobile phase consisted of acetonitrile-water (gradient elution) at the flow rate of 1.0 mL/min.The detection wavelength was set at 246 nm,the column temperature was 30 ℃,and the sample size was 10 μL.RESULTS:The linear ranges of bavachin and bakuchiol were 48.9-489 ng(r=0.999 8),784-7 840 ng(r=0.999 9).RSDs of precision,stability and reproducibility tests were all lower than 2.0％.Average recoveries ranged 95.30％-99.63％ (RSD=1.45％,n=9),96.89％-100.82％ (RSD=1.36％,n=9).CONCLUSIONS:The method is simple,accurate,stable and reproducible,and can be used for the simultaneous determination of bavachin and bakuchiol in P corylifolia.

Effect of extract ethanol and water decoction of Psoralea corylifolia L.on bone development and their toxicities in zebrafish / 中国药理学与毒理学杂志

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.

Effects of Different Processing Methods on the Antiosteoporotic Effective Compositions of Psoralea corylifolia L / 世界科学技术-中医药现代化

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.

The effect of A375 cells corylin melanin synthesis / 国际中医中药杂志

Objective To study the effect of Corylin on A375 cells melanin synthesis,and explore its mechanism.Methods The cells were randomly divided into the control group, the estradiol group, and corylin group including 10-3μmol/L, 10-2μmol/L, 10-1μmol/L, 1μmol/L, 10μmol/L, 100μmol/L. Estradiol estradiol intervention group were given 10-3 mol/L. Corylin group (10-3μmol/L, 10-2μmol/L, 10-1μmol/L, 1μmol/L, 10μmol/L,100μmol/L) were given 10-3μmol/L, 10-2μmol/L, 10-1μmol/L, 1μmol/L, 10μmol/L, 100μmol/L corylin intervention. The activity of proliferation were detected by MTT, NaOH method, dopa oxidation , both melanin content and tyrosinase activity (tyrosinase, TYR). TYR, yrosinase related protein (tyrosinase related protein, TRP)-1 and TRP-2 expression levels of mRNA were determined by RT-PCR.Results Compared with the control group, 10, 100μmol/L of Corylin group cell proliferation rate significantly decreased (P<0.01). The 1μmol/L, 10-1μmol/L, 10-2μmol/L of Corylin group cell melanin content, TYR significantly decreased (P<0.01 or P<0.05). The 1μmol/L corylin group TYR (0.303 ± 0.003vs. 0.628 ± 0.012), TRP-1 (0.313 ± 0.008 vs. 0.677 ± 0.022), TRP-2 (0.456 ± 0.028vs. 0.687 ± 0.020) mRNA expression level significantly decrease (P<0.01).Conclusions The results showed that Corylin could inhibit melanin synthesis, which worked probably through inhibiting the activity of TYR and cutting the mRNA expressions of TYR,TRP-1/2.

Comparative Study on the Processing Technology of Psoralea corylifolia by Salt Frying and Salt Steaming / 中国药房

OBJECTIVE:To compare the contents of 2 index components in salt frying and salt steaming samples of Psoralea corylifolia,and select better processing technology. METHODS:Under the conditions that ratio of salt and medicinal materials was 1:50,4-5 times salt of adding water,brine run time was 2 h,the amounts of psoralen and isopsoralen in salt frying samples after 10,12,14 min of frying under 150 ℃,170 ℃,190 ℃ and in salt steaming samples after 1,1.5,2,2.5 h of steaming were re-spectively investigated,and the effects of 2 processing technology were compared. RESULTS:Under fixed condition,the contents of index components was the highest in salt frying samples by fried for 12 min under 150 ℃ and in salt steaming samples by steamed for 1 h;the content in salt steaming samples (1.49%) was higher than that in salt frying samples (1.29%)(P=0.011). CONCLUSIONS:According to the comparison of index components'contents in processing samples,salt steaming is superior to salt frying of P. corylifolia.

Safety evaluation and risk control measures of Psoralea corylifolia / 中国中药杂志

Through a systematic and comprehensive study of domestic and foreign literatures and information, this study aims to trace the herbal origin and the toxicity recorded in ancient and current documents, analyze the safety case reports of Psoralea corylifolia and experimental studies on toxicity in recent years, and make a preliminary summary about the clinical characteristics and potential risk factors of cases related to the safety of P. corylifolia and its preparations. The study involved 84 patients in the safety case reports of P. corylifolia. The adverse events were mainly liver damage (55.95%) and light toxic contact dermatitis (38.10%), sugguesting that P. corylifolia may lead to liver damage and photo toxicity. However, reproductive toxicity and renal damage were only reported in animal studies, but not in clinical reports. Because of its complicated ingredients, the toxic components and mechanisms of P. corylifolia have not been clear at present. Therefore, the authors proposed to strictly apply P. corylifolia in clinic, use it rationally and combine it with other medications. Besides, efforts shall be made to strength the guidance for doctors, the safety monitoring of P. corylifolia and relevant preparations, and actively carry out safety-related basic and clinical studies, so as to give a better guidance to safe medication, full exert the efficacy and avoid the medication risk.

Serum fingerprint of drug-couple Psoralea corylifolia-Myristica fragrants / 中草药

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.