This review examines the biological properties of coumarins, widely distributed at the highest levels in the fruit, followed by the roots, stems and leaves, by considering their beneficial effects in the prevention of...This review examines the biological properties of coumarins, widely distributed at the highest levels in the fruit, followed by the roots, stems and leaves, by considering their beneficial effects in the prevention of some diseases and as anti-cancer agents. These compounds are well known photosensitizing drugs which have been used as pharmaceuticals for a broad number of therapeutic applications requiring cell division inhibitors. Despite this, even in the absence of ultraviolet rays they are active. The current paper mainly focuses on the effects of psoralens on human breast cancer as they are able to influence many aspects of cell behavior, such as cell growth, survival and apoptosis. In addition, analytical and pharmacological data have demonstrated that psoralens antagonize some metabolizing enzymes, affect estrogen receptor stability and counteract cell invasiveness as well as cancer drug resistance. The scientific findings summarized highlight the pleiotropic functions of phytochemical drugs, given that recently their target signals and how these are modified in thecells have been identified. The encouraging results in this field suggest that multiple modulating strategies based on coumarin drugs in combination with canonical chemotherapeutic agents or radiotherapy could be a useful approach to address the treatment of many types of cancer.展开更多
The hepatitis B virus(HBV) is a global public health challenge due to its highly contagious nature. It is estimated that almost 300 million people live with chronic HBV infection annually. Although nucleoside analogs ...The hepatitis B virus(HBV) is a global public health challenge due to its highly contagious nature. It is estimated that almost 300 million people live with chronic HBV infection annually. Although nucleoside analogs markedly reduce the risk of liver disease progression, the analogs do not fully eradicate the virus. As such, new treatment options and drugs are urgently needed. Psoralen is a nourishing monomer of Chinese herb and is known to inhibit virus replication and inactivate viruses. In this study, we evaluated the potential of psoralen as an anti-HBV agent.Quantitative PCR and Southern blot analysis revealed that psoralen inhibited HBV replication in Hep G2.2.15 cells in a concentration-dependent manner. Moreover, psoralen was also active against the 3TC/ETV-dual-resistant HBV mutant. Further investigations revealed that psoralen suppressed both HBV RNA transcription and core protein expression. The transcription factor FOXO1, a known target for PGC1α co-activation, binds to HBV precore/core promoter enhancer II region and activates HBV RNA transcription. Co-immunoprecipitation showed that psoralen suppressed the expression of FOXO1, thereby decreasing the binding of FOXO1 co-activator PGC1αto the HBV promoter. Overall, our results demonstrate that psoralen suppresses HBV RNA transcription by downregulating the expression of FOXO1 resulting in a reduction of HBV replication.展开更多
[Objectives]This study aimed to establish a qualitative identification and content determination method for psoralen in Ficus pandurata Hance and compare the psoralen contents in roots,stems and leaves of F.pandurate ...[Objectives]This study aimed to establish a qualitative identification and content determination method for psoralen in Ficus pandurata Hance and compare the psoralen contents in roots,stems and leaves of F.pandurate Hance and Ficus pandurata Hance var.holophylla Migo.[Methods]Thin-layer chromatography(TLC)was used for qualitative identification,and the content of psoralen was determined by high-performance liquid chromatography.The chromatographic conditions were as follows:column,Agilent ZORBAX Eclipse Plus C18(250 mm×4.6 mm,5μm);mobile phase,methanol-water(55∶45);flow rate,1 mL/min;detection wavelength,246 nm;column temperature,30℃;and injection volume,10μL.[Results]The TLC chromatogram of F.pandurate Hance showed clear spots and good separation.The concentration of psoralen detected in the range of 2.06-41.20μg/mL had a good linear relationship with the peak area(r=0.9999).The RSD values of the precision,stability and reproducibility tests were all less than 2%.The average recovery rate was 100.2%(RSD=1.13%,n=6).[Conclusions]The established method is simple,easy,accurate and reproducible.It can be used for quality control of F.pandurate Hance.展开更多
A comparative study and management has been conducted in (KTHDV). For some patients who attend the out patients clinic concern on treatment of the vitiligo with a new formula (Oxabet) alone VS Oxabet (oxpsolaren plus ...A comparative study and management has been conducted in (KTHDV). For some patients who attend the out patients clinic concern on treatment of the vitiligo with a new formula (Oxabet) alone VS Oxabet (oxpsolaren plus betamethasone) formula plus NB. UVB311 is during a period from (Jan 2011-Jan 2013). The study sample includes different age groups of both sexes. The study revealed that the formula alone gives good results. The localized vitiligo has a good response to the formula than generalized one. The early lesions have good responses than the old ones. The continuations of applying the treatment and the follow up of the patients enhance the efficacy of the treatment.展开更多
[Objectives]To explore the effect of psoralen combined with paclitaxel on the apoptosis of MCF-7 cells.[Methods]The effects of different concentrations of psoralen,paclitaxel,or the combination of psoralen and paclita...[Objectives]To explore the effect of psoralen combined with paclitaxel on the apoptosis of MCF-7 cells.[Methods]The effects of different concentrations of psoralen,paclitaxel,or the combination of psoralen and paclitaxel on cell viability were detected using CCK-8 assay kit.Cell cycle distribution and apoptosis after 24 h of psoralen(0.16,0.32,0.64 mmol/L),paclitaxel(0.1μmol/L),combined action of psoralen(0.32 mmol/L)and paclitaxel(0.1μmol/L)were detected using flow cytometry.[Results]Lower concentration of psoralen(0.04-0.32 mmol/L)showed no significant inhibitory effect on cells.After combined with paclitaxel,the inhibitory effect on MCF-7 cell proliferation was significantly higher than that of the group treated alone.Compared with the paclitaxel group,the cell apoptosis rate in the drug combination group was significantly increased.Different low concentrations of psoralen can block the cell cycle of MCF-7 at G 0/G 1 phase,while paclitaxel can block the cell cycle at G 2/M phase.After combined action,the number of cells blocked at G 2/M phase decreased.[Conclusions]Overall,the combined effect of psoralen and paclitaxel can enhance anti-tumor ability by inhibiting cell proliferation,inducing apoptosis,and blocking cell cycle.展开更多
Buguzhi(Psoraleae fructus),the seed of Psoralea corylifolia Linn,is used to treat osteoporosis,nephritis,vitiligo and other diseases.However,long-term routine or overdose of Psoraleae fructus may lead to hepatotoxicit...Buguzhi(Psoraleae fructus),the seed of Psoralea corylifolia Linn,is used to treat osteoporosis,nephritis,vitiligo and other diseases.However,long-term routine or overdose of Psoraleae fructus may lead to hepatotoxicity and become a major obstacle of its clinical usage.Psoralen was a key active component of Psoraleae fructus,and a main cause of Psoraleae fructus toxicity.This research was to investigate the hepatotoxicity of psoralen and whether it’s related with bile acid imbalance.Methods:C57BL/6 mice were randomly divided into 4 groups(n=10).Psoralen(20 mg/kg,40 mg/kg and 80 mg/kg)was administrated intragastrically once every day and control group with equivalent water until 4 weeks.Results:The results showed that psoralen caused an increase in liver coefficient and the injury of hepatocytes microstructure of mice.It also inhibited cell viability of HepG2 cells.Mice treated with psoralen exerted liver total bile acid increased while serum total bile acid decreased,which indicated that psoralen-induced liver injury may partly associate with cholestasis.For further study of liver transporters,high dose of psoralen inhibited the expression of some important hepatic efflux transporters(including BSEP,p-gp and ABCG5)in vivo and in vitro.Conclusion:We provide evidence for the first time that psoralen may induce cholestatic hepatotoxicity for the bile acid retention by inhibition on bile acid export pumps.展开更多
Ultraviolet(UV)phototherapy stands as a pivotal clinical approach for managing diverse skin diseases.However,its application is constrained by concerns over UV-induced toxicity and imprecise photosensitizer delivery.T...Ultraviolet(UV)phototherapy stands as a pivotal clinical approach for managing diverse skin diseases.However,its application is constrained by concerns over UV-induced toxicity and imprecise photosensitizer delivery.This work introduces a light-converting microneedle patch(EU-MN),exemplified by its remarkable efficacy in psoriasis treatment.The EU-MN patch could release upconversion nanoparticles(UCNPs)and the photosensitizer methoxypsoralen(MOP)in controlled amounts in response to elevated matrix metalloproteinase(MMP)levels within the skin.Under near-infrared(NIR)excitation,UCNPs emit UV light(345/361 nm),which is combined with MOP to achieve more precise intradermal UV photoche-motherapy,effectively inhibiting abnormal proliferation of human immortalized epidermal cells(HaCaT)and bacterial growth(Staphylococcus aureus and Escherichia coli).Comet assay highlights DNA damage correlation.In addition,the microneedles,designed with a reactive oxygen species(ROS)-responsive shell,release epigallocatechin gallate(EGCG)to counteract excessive inflammation and mitigate UV-induced damage.In psoriasis mice,the EU-MN patch demonstrates significant therapeutic efficacy and recurrence prevention.As further evidenced by the suppression of epidermal hyperplasia and inflammation(through RNA sequencing identifying cell cycle arrest),this EU-MN patch offers a safer,more precise,and more effective alternative strategy for conventional direct UV phototherapy.展开更多
Objective:Salt-processed Psoraleae Fructus(SPF)is widely used as a phytoestrogen-like agent in the treatment of osteoporosis.However,due to improper clinical use or misuse,resulting in liver damage.In this study,netwo...Objective:Salt-processed Psoraleae Fructus(SPF)is widely used as a phytoestrogen-like agent in the treatment of osteoporosis.However,due to improper clinical use or misuse,resulting in liver damage.In this study,network pharmacology was employed to analyze the mechanism of cholestatic liver damage.An adeno-associated virus overexpressing SULT1E1(rAAV8-SULT1E1)was constructed and the hepatotoxicity of SPF,psoralen,and isopsoralen was determined.Methods:By utilizing three databases inclding TCMSP,TCMID,and BATMAN-TCM,the targets of the three databases were summarized,and a total of 45 psoralen compounds were included.Network pharmacology analysis was then performed.The adenoviral vectors were injected into the tail vein of C57BL6 mice to elucidate the role of SULT1E1 in SPF-induced cholestasis-mediated hepatotoxicity in vivo.SPF(10 g/kg),psoralen,and isopsoralen(50 mg/kg each)were intragastrically administered to mice for30 d.B-ultrasound and samples were collected and examined for follow-up experiments.Results:A total of 854 targets were predicted for 45 active components,with 151 cholestasis-mediated hepatotoxicity-related disease targets obtained for SPF.A total of 126 pathways were enriched based on KEGG pathway analysis,with the"estrogen signaling pathway"identified as one of the top 20 pathways.In terms of pathological hepatic changes,treated mice had visually swollen hepatocytes,dilated bile ducts,and elevated serum biochemical markers,which were more prominent in mice treated with isopsoralen than in those treated with other compounds.Notably,the overexpression of SULT1E1 could reverse liver damage in each treatment group.B-ultrasound was used to observe the size of the gallbladder in vivo.The size of the gallbladder was found to significantly increase on day 30 after treatment in the SPF-,psoralen-,and isopsoralen-treated groups,especially the SPF group.Compared with the expression levels in the negative control group(rAAV8-empty+con),the expression levels of FXR,Mrp2,Bsep,SULT1E1,SULT2A1,Ntcp,and Nrf2 decreased,whereas those of CYP7a1 and IL-6 increased in the SPF-,psoralen-,and isopsoralen-treated groups.Conclusion:The overexpression of SULT1E1 could alleviate the decreased or increased expression of indicators,indicating that SULT1E1 is an important target gene for SPF-induced liver damage.The severity of liver damage was significantly lower in the rAAV8-SULT1E1 groups than in the rAAV8-empty groups.展开更多
Syntheses of 2,3-dimethyl-4H-furo[3,2-c]coumarin and 3-phenyl-4H-furo[3,2-c]coumarin as angular furocou- marins were carried out through Williamson reaction of 4-hydroxycoumarin with a-haloketones followed by cycli- z...Syntheses of 2,3-dimethyl-4H-furo[3,2-c]coumarin and 3-phenyl-4H-furo[3,2-c]coumarin as angular furocou- marins were carried out through Williamson reaction of 4-hydroxycoumarin with a-haloketones followed by cycli- zation. Photooxygenation of the synthesized furocoumarin derivatives was performed and the photoproducts were isolated and characterized. The affinity of 2,3-dimethyl-4H-furo[3,2-c]coumarin towards DNA and the antibacterial activity were evaluated and compared with 8-methoxypsoralen （8-MOP）.展开更多
Objective To identify and analyze the volatile constituents in the leaves and fruits of Ficus carica. Methods Gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) were used. Results The major compo...Objective To identify and analyze the volatile constituents in the leaves and fruits of Ficus carica. Methods Gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) were used. Results The major components detected in volatile oil of the leaves were psoralen (10.12%), β-damascenone (10.17%), benzyl alcohol (4.56%), behenic acid (4.79%), and bergapten (1.99%), etc. The major components detected in volatile oil of the fruits were furfural (10.55%), 5-methyl-2-furaldehyde (10.1%), and benzeneacetaldehyde (6.59%), etc. Conclusion A total of 121 volatile constituents are identified in the leaves and 108 in the fruits of F. carica, among which 103 constituents are identified for the first time in the leaves and 100 in the fruits. Eighteen volatile constituents are identified in both leaves and fruits.展开更多
A high performance liquid chromatography-tandem mass spectrometry(HPLC-MS/MS)method was built to determine icarside,hyperoside and psoralen in food.The samples were extracted with 70%methanol,the solid and semi-solid ...A high performance liquid chromatography-tandem mass spectrometry(HPLC-MS/MS)method was built to determine icarside,hyperoside and psoralen in food.The samples were extracted with 70%methanol,the solid and semi-solid hotpot seasoning samples were purified by solid phase extraction column,and then determined by HPLC-MS/MS.Acetonitrile and 0.1%formic acid solution were used as the mobile phase,and the gradient elution was adopted for analysis.As shown in the results,the analytes had good linearity in the range of 0.05−100 ng/mL,and the correlation coeffificients(R^(2))were greater than 0.999.In this method,the limits of quantitation(LOQ)of psoralen,icariside and hyperoside in liquid samples were 1.25,25.0 and 12.5μg/L respectively;while the LOQs of psoralen,icariside and hyperoside in solid samples and hotpot seasoning samples were 1.25,25.0 and 12.5μg/kg,respectively.The liquid beverage,solid beverage,health food(in the form of oral liquid,capsule,tablet),integrated alcoholic beverage and solid hotpot seasoning were selected as representative samples and used for method validation.The average spiked recoveries at 3 levels(LOQ,2 LOQ,10 LOQ)were in the range of 83.7%−115.0%,and the relative standard deviations were in range of 0.5%−9.4%(n=6).The method is rapid,accurate and sensitive,which is suitable for the simultaneous determination of icariside,hyperoside and psoralen in different food matrices.展开更多
Objective: To optimize a self-emulsifying drug delivery system(SEDDS) formulation for psoralen and isopsoralen(PSO and IPSO) isolated from Psoraleae Fructus.Methods: A D-optimal design was used to investigate the infl...Objective: To optimize a self-emulsifying drug delivery system(SEDDS) formulation for psoralen and isopsoralen(PSO and IPSO) isolated from Psoraleae Fructus.Methods: A D-optimal design was used to investigate the influence of oil percentage, surfactant percentage and cosurfactant percentage on several properties of SEDDS including particle size, polydispersity,equilibrium solubility, in situ intestine absorption rate and intestinal permeability. Furthermore, the desirability function approach was applied to obtain the optimal formulation for the system.Results: The oil percentage, surfactant percentage and cosurfactant percentage were optimized to be53.6%, 35.7% and 10.7%, respectively, which means the model is available.Conclusions: The D-optimal design is valuable to optimize the SEDDS formulation and understand formulation compositions’ functions on SEDDS properties.展开更多
文摘This review examines the biological properties of coumarins, widely distributed at the highest levels in the fruit, followed by the roots, stems and leaves, by considering their beneficial effects in the prevention of some diseases and as anti-cancer agents. These compounds are well known photosensitizing drugs which have been used as pharmaceuticals for a broad number of therapeutic applications requiring cell division inhibitors. Despite this, even in the absence of ultraviolet rays they are active. The current paper mainly focuses on the effects of psoralens on human breast cancer as they are able to influence many aspects of cell behavior, such as cell growth, survival and apoptosis. In addition, analytical and pharmacological data have demonstrated that psoralens antagonize some metabolizing enzymes, affect estrogen receptor stability and counteract cell invasiveness as well as cancer drug resistance. The scientific findings summarized highlight the pleiotropic functions of phytochemical drugs, given that recently their target signals and how these are modified in thecells have been identified. The encouraging results in this field suggest that multiple modulating strategies based on coumarin drugs in combination with canonical chemotherapeutic agents or radiotherapy could be a useful approach to address the treatment of many types of cancer.
基金supported by the National Science Fund (82104240)Shanghai Science and Technology Innovation Project (20S11906200)self-deployed scientific research projects (State Key Laboratory of Drug Research) (SIMM1903ZZ-03)。
文摘The hepatitis B virus(HBV) is a global public health challenge due to its highly contagious nature. It is estimated that almost 300 million people live with chronic HBV infection annually. Although nucleoside analogs markedly reduce the risk of liver disease progression, the analogs do not fully eradicate the virus. As such, new treatment options and drugs are urgently needed. Psoralen is a nourishing monomer of Chinese herb and is known to inhibit virus replication and inactivate viruses. In this study, we evaluated the potential of psoralen as an anti-HBV agent.Quantitative PCR and Southern blot analysis revealed that psoralen inhibited HBV replication in Hep G2.2.15 cells in a concentration-dependent manner. Moreover, psoralen was also active against the 3TC/ETV-dual-resistant HBV mutant. Further investigations revealed that psoralen suppressed both HBV RNA transcription and core protein expression. The transcription factor FOXO1, a known target for PGC1α co-activation, binds to HBV precore/core promoter enhancer II region and activates HBV RNA transcription. Co-immunoprecipitation showed that psoralen suppressed the expression of FOXO1, thereby decreasing the binding of FOXO1 co-activator PGC1αto the HBV promoter. Overall, our results demonstrate that psoralen suppresses HBV RNA transcription by downregulating the expression of FOXO1 resulting in a reduction of HBV replication.
文摘[Objectives]This study aimed to establish a qualitative identification and content determination method for psoralen in Ficus pandurata Hance and compare the psoralen contents in roots,stems and leaves of F.pandurate Hance and Ficus pandurata Hance var.holophylla Migo.[Methods]Thin-layer chromatography(TLC)was used for qualitative identification,and the content of psoralen was determined by high-performance liquid chromatography.The chromatographic conditions were as follows:column,Agilent ZORBAX Eclipse Plus C18(250 mm×4.6 mm,5μm);mobile phase,methanol-water(55∶45);flow rate,1 mL/min;detection wavelength,246 nm;column temperature,30℃;and injection volume,10μL.[Results]The TLC chromatogram of F.pandurate Hance showed clear spots and good separation.The concentration of psoralen detected in the range of 2.06-41.20μg/mL had a good linear relationship with the peak area(r=0.9999).The RSD values of the precision,stability and reproducibility tests were all less than 2%.The average recovery rate was 100.2%(RSD=1.13%,n=6).[Conclusions]The established method is simple,easy,accurate and reproducible.It can be used for quality control of F.pandurate Hance.
文摘A comparative study and management has been conducted in (KTHDV). For some patients who attend the out patients clinic concern on treatment of the vitiligo with a new formula (Oxabet) alone VS Oxabet (oxpsolaren plus betamethasone) formula plus NB. UVB311 is during a period from (Jan 2011-Jan 2013). The study sample includes different age groups of both sexes. The study revealed that the formula alone gives good results. The localized vitiligo has a good response to the formula than generalized one. The early lesions have good responses than the old ones. The continuations of applying the treatment and the follow up of the patients enhance the efficacy of the treatment.
基金Supported by the Natural Science Foundation Project of Guangxi University of Chinese Medicine(2020MS058)Youth Fund Project of Guangxi Natural Science Foundation(2022JJB140402)+4 种基金Basic Research Ability Improvement Project of Young and Middle-aged Teachers in Guangxi Universities(2022KY0278)"Youth Project"Talent Cultivation Project of Guangxi International Zhuang Medicine Hospital(2022001)High-level Key Discipline of Traditional Chinese Medicine(Zhuang Pharmacy)Construction Project of National Administration of Traditional Chinese Medicine(GZYYRJH[2022]226)Multidisciplinary Cross Innovation Team Project of Guangxi Traditional Chinese Medicine(GZKJ2309)"High-level Talent Cultivation and Innovation Team"Project of Guangxi University of Chinese Medicine(2022A008).
文摘[Objectives]To explore the effect of psoralen combined with paclitaxel on the apoptosis of MCF-7 cells.[Methods]The effects of different concentrations of psoralen,paclitaxel,or the combination of psoralen and paclitaxel on cell viability were detected using CCK-8 assay kit.Cell cycle distribution and apoptosis after 24 h of psoralen(0.16,0.32,0.64 mmol/L),paclitaxel(0.1μmol/L),combined action of psoralen(0.32 mmol/L)and paclitaxel(0.1μmol/L)were detected using flow cytometry.[Results]Lower concentration of psoralen(0.04-0.32 mmol/L)showed no significant inhibitory effect on cells.After combined with paclitaxel,the inhibitory effect on MCF-7 cell proliferation was significantly higher than that of the group treated alone.Compared with the paclitaxel group,the cell apoptosis rate in the drug combination group was significantly increased.Different low concentrations of psoralen can block the cell cycle of MCF-7 at G 0/G 1 phase,while paclitaxel can block the cell cycle at G 2/M phase.After combined action,the number of cells blocked at G 2/M phase decreased.[Conclusions]Overall,the combined effect of psoralen and paclitaxel can enhance anti-tumor ability by inhibiting cell proliferation,inducing apoptosis,and blocking cell cycle.
基金This study was supported by National Natural Science Foundation of China(No.81202991).
文摘Buguzhi(Psoraleae fructus),the seed of Psoralea corylifolia Linn,is used to treat osteoporosis,nephritis,vitiligo and other diseases.However,long-term routine or overdose of Psoraleae fructus may lead to hepatotoxicity and become a major obstacle of its clinical usage.Psoralen was a key active component of Psoraleae fructus,and a main cause of Psoraleae fructus toxicity.This research was to investigate the hepatotoxicity of psoralen and whether it’s related with bile acid imbalance.Methods:C57BL/6 mice were randomly divided into 4 groups(n=10).Psoralen(20 mg/kg,40 mg/kg and 80 mg/kg)was administrated intragastrically once every day and control group with equivalent water until 4 weeks.Results:The results showed that psoralen caused an increase in liver coefficient and the injury of hepatocytes microstructure of mice.It also inhibited cell viability of HepG2 cells.Mice treated with psoralen exerted liver total bile acid increased while serum total bile acid decreased,which indicated that psoralen-induced liver injury may partly associate with cholestasis.For further study of liver transporters,high dose of psoralen inhibited the expression of some important hepatic efflux transporters(including BSEP,p-gp and ABCG5)in vivo and in vitro.Conclusion:We provide evidence for the first time that psoralen may induce cholestatic hepatotoxicity for the bile acid retention by inhibition on bile acid export pumps.
基金funded by the Jiangxi Province Key Laboratory of Precision Cell Therapy(No.2024SSY06241 to J.L.)the National Natural Science Foundation of China(No.82360174 to J.L.)+3 种基金the Science and Technology Department Project of Jiangxi Province(No.20224ABC03A02 to J.L.)the Key Research and Development Program of Jiangxi Province(No.20212BBG73004 to X.L.W.)the Jiangxi Province Key Laboratory of Bioengineering Drugs(No.2024SSY07061 to X.L.W.)the Graduate Innovation Special Fund Project of Jiangxi Province(No.YC2023-B046 to L.B.L.).
文摘Ultraviolet(UV)phototherapy stands as a pivotal clinical approach for managing diverse skin diseases.However,its application is constrained by concerns over UV-induced toxicity and imprecise photosensitizer delivery.This work introduces a light-converting microneedle patch(EU-MN),exemplified by its remarkable efficacy in psoriasis treatment.The EU-MN patch could release upconversion nanoparticles(UCNPs)and the photosensitizer methoxypsoralen(MOP)in controlled amounts in response to elevated matrix metalloproteinase(MMP)levels within the skin.Under near-infrared(NIR)excitation,UCNPs emit UV light(345/361 nm),which is combined with MOP to achieve more precise intradermal UV photoche-motherapy,effectively inhibiting abnormal proliferation of human immortalized epidermal cells(HaCaT)and bacterial growth(Staphylococcus aureus and Escherichia coli).Comet assay highlights DNA damage correlation.In addition,the microneedles,designed with a reactive oxygen species(ROS)-responsive shell,release epigallocatechin gallate(EGCG)to counteract excessive inflammation and mitigate UV-induced damage.In psoriasis mice,the EU-MN patch demonstrates significant therapeutic efficacy and recurrence prevention.As further evidenced by the suppression of epidermal hyperplasia and inflammation(through RNA sequencing identifying cell cycle arrest),this EU-MN patch offers a safer,more precise,and more effective alternative strategy for conventional direct UV phototherapy.
基金supported by the National Natural Science Foundation of China(81973484 and 82304736)the 2022 Natural Science Foundation of Nanjing University of Chinese Medicine(XZR2021085)。
文摘Objective:Salt-processed Psoraleae Fructus(SPF)is widely used as a phytoestrogen-like agent in the treatment of osteoporosis.However,due to improper clinical use or misuse,resulting in liver damage.In this study,network pharmacology was employed to analyze the mechanism of cholestatic liver damage.An adeno-associated virus overexpressing SULT1E1(rAAV8-SULT1E1)was constructed and the hepatotoxicity of SPF,psoralen,and isopsoralen was determined.Methods:By utilizing three databases inclding TCMSP,TCMID,and BATMAN-TCM,the targets of the three databases were summarized,and a total of 45 psoralen compounds were included.Network pharmacology analysis was then performed.The adenoviral vectors were injected into the tail vein of C57BL6 mice to elucidate the role of SULT1E1 in SPF-induced cholestasis-mediated hepatotoxicity in vivo.SPF(10 g/kg),psoralen,and isopsoralen(50 mg/kg each)were intragastrically administered to mice for30 d.B-ultrasound and samples were collected and examined for follow-up experiments.Results:A total of 854 targets were predicted for 45 active components,with 151 cholestasis-mediated hepatotoxicity-related disease targets obtained for SPF.A total of 126 pathways were enriched based on KEGG pathway analysis,with the"estrogen signaling pathway"identified as one of the top 20 pathways.In terms of pathological hepatic changes,treated mice had visually swollen hepatocytes,dilated bile ducts,and elevated serum biochemical markers,which were more prominent in mice treated with isopsoralen than in those treated with other compounds.Notably,the overexpression of SULT1E1 could reverse liver damage in each treatment group.B-ultrasound was used to observe the size of the gallbladder in vivo.The size of the gallbladder was found to significantly increase on day 30 after treatment in the SPF-,psoralen-,and isopsoralen-treated groups,especially the SPF group.Compared with the expression levels in the negative control group(rAAV8-empty+con),the expression levels of FXR,Mrp2,Bsep,SULT1E1,SULT2A1,Ntcp,and Nrf2 decreased,whereas those of CYP7a1 and IL-6 increased in the SPF-,psoralen-,and isopsoralen-treated groups.Conclusion:The overexpression of SULT1E1 could alleviate the decreased or increased expression of indicators,indicating that SULT1E1 is an important target gene for SPF-induced liver damage.The severity of liver damage was significantly lower in the rAAV8-SULT1E1 groups than in the rAAV8-empty groups.
文摘Syntheses of 2,3-dimethyl-4H-furo[3,2-c]coumarin and 3-phenyl-4H-furo[3,2-c]coumarin as angular furocou- marins were carried out through Williamson reaction of 4-hydroxycoumarin with a-haloketones followed by cycli- zation. Photooxygenation of the synthesized furocoumarin derivatives was performed and the photoproducts were isolated and characterized. The affinity of 2,3-dimethyl-4H-furo[3,2-c]coumarin towards DNA and the antibacterial activity were evaluated and compared with 8-methoxypsoralen （8-MOP）.
基金the Project of Researches in Application and Development of Figs in Atushi aided by Atushi Agricultural Bureau in Xinjiang, China
文摘Objective To identify and analyze the volatile constituents in the leaves and fruits of Ficus carica. Methods Gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) were used. Results The major components detected in volatile oil of the leaves were psoralen (10.12%), β-damascenone (10.17%), benzyl alcohol (4.56%), behenic acid (4.79%), and bergapten (1.99%), etc. The major components detected in volatile oil of the fruits were furfural (10.55%), 5-methyl-2-furaldehyde (10.1%), and benzeneacetaldehyde (6.59%), etc. Conclusion A total of 121 volatile constituents are identified in the leaves and 108 in the fruits of F. carica, among which 103 constituents are identified for the first time in the leaves and 100 in the fruits. Eighteen volatile constituents are identified in both leaves and fruits.
基金This work was supported by National Key Research and Development Program of China(2019YFC1606400).
文摘A high performance liquid chromatography-tandem mass spectrometry(HPLC-MS/MS)method was built to determine icarside,hyperoside and psoralen in food.The samples were extracted with 70%methanol,the solid and semi-solid hotpot seasoning samples were purified by solid phase extraction column,and then determined by HPLC-MS/MS.Acetonitrile and 0.1%formic acid solution were used as the mobile phase,and the gradient elution was adopted for analysis.As shown in the results,the analytes had good linearity in the range of 0.05−100 ng/mL,and the correlation coeffificients(R^(2))were greater than 0.999.In this method,the limits of quantitation(LOQ)of psoralen,icariside and hyperoside in liquid samples were 1.25,25.0 and 12.5μg/L respectively;while the LOQs of psoralen,icariside and hyperoside in solid samples and hotpot seasoning samples were 1.25,25.0 and 12.5μg/kg,respectively.The liquid beverage,solid beverage,health food(in the form of oral liquid,capsule,tablet),integrated alcoholic beverage and solid hotpot seasoning were selected as representative samples and used for method validation.The average spiked recoveries at 3 levels(LOQ,2 LOQ,10 LOQ)were in the range of 83.7%−115.0%,and the relative standard deviations were in range of 0.5%−9.4%(n=6).The method is rapid,accurate and sensitive,which is suitable for the simultaneous determination of icariside,hyperoside and psoralen in different food matrices.
文摘Objective: To optimize a self-emulsifying drug delivery system(SEDDS) formulation for psoralen and isopsoralen(PSO and IPSO) isolated from Psoraleae Fructus.Methods: A D-optimal design was used to investigate the influence of oil percentage, surfactant percentage and cosurfactant percentage on several properties of SEDDS including particle size, polydispersity,equilibrium solubility, in situ intestine absorption rate and intestinal permeability. Furthermore, the desirability function approach was applied to obtain the optimal formulation for the system.Results: The oil percentage, surfactant percentage and cosurfactant percentage were optimized to be53.6%, 35.7% and 10.7%, respectively, which means the model is available.Conclusions: The D-optimal design is valuable to optimize the SEDDS formulation and understand formulation compositions’ functions on SEDDS properties.
