Epimedii Folium(EF)combined with Psoraleae Fructus(PF)is a common modern preparation,but liver injury caused by Chinese patent medicine preparations containing EF and PF has been frequently reported in recent years.Zh...Epimedii Folium(EF)combined with Psoraleae Fructus(PF)is a common modern preparation,but liver injury caused by Chinese patent medicine preparations containing EF and PF has been frequently reported in recent years.Zhuangguguanjiewan pills(ZGW),which contain EF and PF,could induce immune idiosyncratic liver injury according to clinical case reports and a nonhepatotoxic dose of lipopolysaccharide(LPS)model.This present study evaluated the liver injury induced by EF or PF alone or in combination and investigated the related mechanism by using the LPS model.Liver function indexes and pathological results showed that either EF or PF alone or in combination led to liver injury in normal rats;however,EF or PF alone could lead to liver injury in LPS-treated rats.Moreover,EF combined with PF could induce a greater degree of injury than that caused by EF or PF alone in LPS-treated rats.Furthermore,EF or PF alone or in combination enhanced the LPS-stimulated inflammatory cytokine production,implying that IL-1β,which is processed and released by activating the NLRP3 inflammasome,is a specific indicator of EF-induced immune idiosyncratic hepatotoxicity.Thus,EF may induce liver injury through enhancing the LPS-mediated proinflammatory cytokine production and activating the NLRP3 inflammasome.In addition,the metabolomics analysis results showed that PF affected more metabolites in glycerophospholipid and sphingolipid metabolic pathways compared with EF in LPS model,suggesting that PF increased the responsiveness of the liver to LPS or other inflammatory mediators via modulation of multiple metabolic pathways.Therefore,EF and PF combination indicates traditional Chinese medicine incompatibility,considering that it induces idiosyncratic hepatotoxicity under immunological stress conditions.展开更多
Lycii Fructus（Lycium barbarum, Gouqizi in Chinese name） is one of the most popular Chinese material medica and a common ingredient in tonic food. This fruit has been paid rapidly growing attention for its nutrient v...Lycii Fructus（Lycium barbarum, Gouqizi in Chinese name） is one of the most popular Chinese material medica and a common ingredient in tonic food. This fruit has been paid rapidly growing attention for its nutrient value and noticeable pharmacological properties. The present paper focuses on the legal resource of Gouqizi and reviews the main research in medicinal field including botanical identification,ethnopharmacological functions, phytochemistry, pharmacological effects, clinic usages, and safety issues.In addition, some issues needed address will be also discussed. We strongly believe that further investigation will deepen our knowledge of Gouqizi and promote the industrial development in the world.展开更多
Objective It is imperative to provide some consistent experimental results for the extraction of flavonid from Fructus Gardeniae. Methods The key extraction parameters that influenced the yield of flavonid from Fructu...Objective It is imperative to provide some consistent experimental results for the extraction of flavonid from Fructus Gardeniae. Methods The key extraction parameters that influenced the yield of flavonid from Fructus Gardeniae were optimized by employing an orthogonal experiment [L9（3）4], including the ratio of buffer solution （Na2B4O7· 10H2O） to raw material, concentration of Fructus Gardeniae in extracting solution, extraction time and pH of buffer solution. An UV/Vis detector was used to perform the qualitative and quantitative analyses of the extracted flavonid with the using of the standard sample. Results The maximum extraction yield of the crude extract was 5.0533 （mg/g） after 20 min when the mass ratio of Na2B4O7 · 10H2O to raw material was 0.4%, the concentration of Fructus Gardeniae in the extraction solution was 1/12 （g/mL）, and pH of buffer solution was 4.5. The positive reactions to the Molish and HCI-Mg tests suggested that the extracted compound was flavonoid, and FTIR measurements also identified the presence of flavonoid in the extracts. Conclusion This work is expected to provide a basis for further research, development, and utilization of Fructus gardenia in flavonid extraction.展开更多
Psoraleae Fructus(PF)is a well-known traditional herbal medicine in China,and it is widely used for osteoporosis,vitiligo,and other diseases in clinical settings.However,liver injury caused by PF and its preparations ...Psoraleae Fructus(PF)is a well-known traditional herbal medicine in China,and it is widely used for osteoporosis,vitiligo,and other diseases in clinical settings.However,liver injury caused by PF and its preparations has been frequently reported in recent years.Our previous studies have demonstrated that PF could cause idiosyncratic drug-induced liver injury(IDILI),but the mechanism underlying its hepatotoxicity remains unclear.This paper reports that bavachin isolated from PF enhances the specific stimuli-induced activation of the NLRP3 inflammasome and leads to hepatotoxicity.Bavachin boosts the secretion of IL-ip and caspase-1 caused by ATP or nigericin but not those induced by poly(I:C),monosodium urate crystal,or intracellular lipopolysaccharide.Bavachin does not affect AIM2 or NLRC4 inflammasome activation.Mechanistically,bavachin specifically increases the production of nigericin-induced mitochondrial reactive oxygen species among the most important upstream events in the activation of the NLRP3 inflammasome.Bavachin increases the levels of aspartate transaminase and alanine aminotransferase in serum and hepatocyte injury accompanied by the secretion of IL-ip via a mouse model of lipopolysaccharide-mediated susceptibility to IDILI.These results suggest that bavachin specifically enhances the ATP-or nigericin-induced activation of the NLRP3 inflammasome.Bavachin also potentially contributes to PF-induced idiosyncratic hepatotoxicity.Moreover,bavachin and PF should be evaded among patients with diseases linked to the ATP-or nigericin-mediated activation of the NLRP3 inflammasome,which may be a dangerous factor for liver injury.展开更多
The present study was designed to optimize the processing of Fructus Arctii by response surface methodology （RSM）. Based on single factor studies, a three-variable, three-level Box-Behnken design （BBD） was used to...The present study was designed to optimize the processing of Fructus Arctii by response surface methodology （RSM）. Based on single factor studies, a three-variable, three-level Box-Behnken design （BBD） was used to monitor the effects of independent variables, including processing temperature and time, on the dependent variables. Response surfaces and contour plots of the contents of total lignans, chlorogenic acid, arctiin, and aretigenin were obtained through ultraviolet and visible （UV-Vis） monitoring and high performance liquid chromatography （HPLC）. Fructus Arctii should be processed under heating in a pot at 311℃, medicine at 119℃ for 123s with flipping frequently. The experimental values under the optimized processing technology were consistent with the predicted values. In conclusion, RSM is an effective method to optimize the processing of traditional Chinese medicine （TCM）.展开更多
AIM: To examine the effect of aqueous fructus aurantii immaturus(FAI) extracts on the intestinal plexus of cathartic colons.METHODS: Cathartic colons were induced in rats with dahuang,a laxative used in traditional Ch...AIM: To examine the effect of aqueous fructus aurantii immaturus(FAI) extracts on the intestinal plexus of cathartic colons.METHODS: Cathartic colons were induced in rats with dahuang,a laxative used in traditional Chinese medicine. Once the model was established(after approximately 12 wk),rats were administered mosapride(1.54 mg/kg) or various doses of aqueous FAI extracts(1-4 g/kg) for 14 d. Transit function was assessed using an ink propulsion test. Rats were then sacrificed,and the ultramicrostructure of colonic tissue was examined using transmission electron microscopy. The expression of the 5-hydroxytryptamine receptor 4(5-HTR4) and neurofilament-H was assessed in colon tissues using real-time PCR,Western blot,and immunohistochemistry.RESULTS: Mosapride and high dose(4 g/kg) of aqueous FAI extracts significantly improved the bowel movement in cathartic colons compared to untreated model colons as measured by the intestinal transit rate(70.06 ± 7.25 and 72.02 ± 8.74,respectively,vs 64.12 ± 5.19; P < 0.05 for both). Compared to controls,the ultramicrostructure of cathartic colons showed signsof neural degeneration. Treatment with mosapride and aqueous FAI extracts resulted in recovery of ultrastructural pathology. Treatment with mosapride alone upregulated the gene and protein expression of 5-HTR4 compared to untreated controls(P < 0.05 for both). Treatment with aqueous FAI extracts(≥ 2 g/kg) increased 5-HTR4 m RNA levels(P < 0.05),but no change in protein level was observed by Western blot or immunohistochemistry. The m RNA and protein levels of neurofilament-H were significantly increased with mosapride and ≥ 2 g/kg aqueous FAI extracts compared to controls(P < 0.05 for all).CONCLUSION: Aqueous FAI extracts and mosapride strengthen bowel movement in cathartic colons via increasing the expression of 5-HTR4 and neurofilament-H.展开更多
Alternariol caused DNA single-strand breakage. Conversion of the closed circular double-stranded supercoiled DNA (pBR 322) to the nicked circular form and linear form was used to investigate the effect of extracts of ...Alternariol caused DNA single-strand breakage. Conversion of the closed circular double-stranded supercoiled DNA (pBR 322) to the nicked circular form and linear form was used to investigate the effect of extracts of some Chinese medical herbs on DNA nicking induced by alternariol. Some substances in the extracts of Rhizoma polygonati (RP) and Fructus lycii (FL) were shown to protect DNA from the attack by alternariol.Some substance in the RP may bind to plasmid DNA, and this binding reduces the electrophoretic mobility of DNA. These results indicate that substances from FL and RP may be used as DNA protectors. It is possible that they play an important role in preventing cancer.展开更多
Psoraleae Fructus(the dried fruits of Psoralea corylifolia), one of the most frequently used Chinese herbs in Asian countries, has a variety of biological activities. In clinical settings, Psoraleae Fructus or Psorale...Psoraleae Fructus(the dried fruits of Psoralea corylifolia), one of the most frequently used Chinese herbs in Asian countries, has a variety of biological activities. In clinical settings, Psoraleae Fructus or Psoraleae Fructus-related herbal medicines frequently have been used in combination with a number of therapeutic drugs for the treatment of various human diseases, such as leukoderma, rheumatism and dysentery. The use of Psoraleae Fructus in combination with drugs has aroused concern of the potential risks of herb-drug interactions(HDI) or herb-endobiotic interactions(HEI). This article reviews the interactions between human drug-metabolizing enzymes and the constituents of Psoraleae Fructus;the major constituents in Psoraleae Fructus, along with their chemical structures and metabolic pathways are summarized, and the inhibitory and inductive effects of the constituents in Psoraleae Fructus on human drug-metabolizing enzymes(DMEs), including target enzyme(s), its modulatory potency, and mechanisms of action are presented. Collectively, this review summarizes current knowledge of the interactions between the Chinese herb Psoraleae Fructus and therapeutic drugs in an effort to facilitate its rational use in clinical settings, and especially to avoid the potential risks of HDI or HEI through human DMEs.展开更多
A simple,rapid and sensitive liquid chromatography-mass spectrometry（LC-MS）method was developed for the determination of salidroside in rat plasma and study of its pharmacokinetics after oral administration of suspe...A simple,rapid and sensitive liquid chromatography-mass spectrometry（LC-MS）method was developed for the determination of salidroside in rat plasma and study of its pharmacokinetics after oral administration of suspension of Erzhi Wan and Fructus Ligustri lucidi into Wistar rats.Plasma sample of 200 μL was extracted with acetic ether-isopropanol（2∶1）and the extraction was performed on a Kromasil C18 column（150 mm×4.6 mm,5 μm）with the mobile phase of methanol-water（41∶59,v/v）within a run time of 6.0 min.The analyte was monitored with positive electrospray ionization（ESI）by selected ion monitoring（SIM）mode.The target ions were m/z 323.05 for salidroside and m/z 411.05 for internal standard（IS）geniposide.A good linear relationship was obtained over the range of 5.0-500.0 ng/mL and the lower limit of quantification was 5.0 ng/mL.The validated method was successfully applied to the pharmacokinetic study of salidroside in rat plasma after oral administration of suspension of Erzhi Wan and Fructus Ligustri lucidi.展开更多
Flos Sophorae and Fructus Sophorae are two kinds of traditional Chinese medicines. In this work, the two kinds of traditional Chinese medicines collected from eleven areas of Dezhou, were analyzed by inductively coupl...Flos Sophorae and Fructus Sophorae are two kinds of traditional Chinese medicines. In this work, the two kinds of traditional Chinese medicines collected from eleven areas of Dezhou, were analyzed by inductively couple plasma-mass spectrometry （ICP-MS） to compare the content and distribution of 14 kinds of rare earth elements （REEs）. The method was verified by analyzing GBW07605 certified reference material. The results showed that ICP-MS is an accurate, sensitive and reliable technique for determining REEs in traditional Chinese medicine. There were big differences in contents for REEs in Flos Sophorae and Fmctus Sophorae from different areas. The contents of total REEs in Flos Sophorae samples from different areas ranged from 1.0785 to 2.2659 μg/g, while those in Fmctus Sophorae from 0.6826 to 1.0527 ktg/g. The contents of total REEs in Flos Sophorae samples from different areas were obviously higher than those in Fmctus Sophorae of the same area and there was big difference between various Flos Sophorae samples. Interestingly, the higher the content of total REEs in Flos Sophorae samples, the lower the content of total REEs in Fmctus Sophorae samples of the same area. The plots of normalized element concentration versus atomic number showed some characteristic distribution trends. The distribution trend of light REEs （La-Gd） was relatively fiat except a positive Eu anomaly, however, that was steep and discrepant for heavy REEs （Tb-Lu）. The results could provide a valuable reference for understanding the relationship between the curative mechanism, pharmacology characteristics and their geological condition for the two traditional Chinese medicines investigated.展开更多
Four prenylated flavonoids compounds 1-4,named sinopodophyllines A-D,and a flavonoid glycoside(compound 13),sinopodophylliside A,together with 19 known compounds(compounds 5-12 and 14-24) were isolated from the fruits...Four prenylated flavonoids compounds 1-4,named sinopodophyllines A-D,and a flavonoid glycoside(compound 13),sinopodophylliside A,together with 19 known compounds(compounds 5-12 and 14-24) were isolated from the fruits of Sinopodophyllum hexandrum.The structures of new compounds were elucidated by extensive spectroscopic analysis,including HRESIMS,1D and 2D NMR.Compounds 1-6,9-11,and 14-17 were tested for their cytotoxicity against human breast-cancer T47 D,MCF-7 and MDA-MB-231 cells in vitro,and compounds 2,5,6,10 and 11 showed significant cytotoxicity(IC50 values < 10 μmol·L^(-1))against T47 D cells.展开更多
Objective To analyze clinical feature and information of medication to explore the risk signals of preparations containing Psoraleae Fructus(BGZP)related with hepatobiliary adverse drug reactions(ADR),in order to rein...Objective To analyze clinical feature and information of medication to explore the risk signals of preparations containing Psoraleae Fructus(BGZP)related with hepatobiliary adverse drug reactions(ADR),in order to reinforce pharmacovigilance.Methods A retrospective study was conducted based on hepatobiliary ADR related with BGZP from the China Adverse Drug Reaction Monitoring System in years from January 2012 to December 2016.Serious and general ADRs were analyzed and assessed.Results There were 355 cases of hepatobiliary ADR related to BGZP.Both the amount of cases and the proportion of serious ADR showed an increasing growth by years(P<0.05).It was found that 10.43%of 355 cases may be involved with irrational drug use,including overdose,repeated medication,and combination of multiple drugs.There were 190 cases which used BGZP(non-combination),and they were mainly for common in diseases caused by abnormal immune activation(accounting for 40.53%of the total cases).Especially at the age group with the most cases with age of 41–50 years,the cases associated with immunological diseases of female were obviously more than that of male(P<0.05).The latency of hepatobiliary ADR related to BGZP ranged from 1 to 386 days,and the median latency was 27.5 days,along with the range of cumulative dose(0.45–520.02 g)as well as the daily dose(0.09–2.64 g/d)after the conversion.Conclusions Cases of hepatobiliary ADR related to BGZP showed significant individual differences,and there was no correlation between drug usage duration and dosage and the occurrence of hepatobiliary ADR.It may be similar with idiosyncratic drug-induced liver injury,and recommended that BGZP should be used with more caution under monitoring liver function,especially in female patients with immunological diseases.展开更多
Fructus Psoraleae,which is commonly consumed for the treatment of osteoporosis,bone fracture,and leucoderma,induces liver injury.This study investigated the pathogenesis of the ethanol extract of Fructus Psoraleae(EEF...Fructus Psoraleae,which is commonly consumed for the treatment of osteoporosis,bone fracture,and leucoderma,induces liver injury.This study investigated the pathogenesis of the ethanol extract of Fructus Psoraleae(EEFP)-induced liver injury in rats.EEFP(1.35,1.80,and 2.25 g·kg^–1)was administrated to Sprague Dawley(SD)rats for 30 d.We measured liver chemistries,histopathology,and quantitative isobaric tags for relative and absolute quantitation(iTRAQ)-based protein profiling.EEFP demonstrated parameters suggestive of liver injury with changes in bile secretion,bile flow rate,and liver histopathology.iTRAQ analysis showed that a total of 4042 proteins were expressed in liver tissues of EEFP-treated and untreated rats.Among these proteins,81 were upregulated and 32 were downregulated in the treatment group.KEGG pathway analysis showed that the drug metabolic pathways of cytochrome P450,glutathione metabolism,glycerolipid metabolism,and bile secretion were enriched with differentially expressed proteins.The expression of key proteins related to the farnesoid X receptor(FXR),i.e.,the peroxisome proliferators-activated receptor alpha(PPAR-α),were downregulated,and multidrug resistance-associated protein 3(MRP3)was upregulated in the EEFP-treated rats.Our results provide evidence that EEFP may induce hepatotoxicity through various pathways.Furthermore,our study demonstrates changes in protein regulation using iTRAQ quantitative proteomics analysis.展开更多
基金supported by the National Natural Science Foundation of China(Nos.81874368 and 81630100)the Beijing Nova Program(No.Z181100006218001)+2 种基金the National Key Technology R&D Program(No.2015ZX 09501-004-001-008)the National Key R&D Program of China(No.2018YFC1707000)the National TCM Industry Science and Technology Program(No.201507004-4-2).
文摘Epimedii Folium(EF)combined with Psoraleae Fructus(PF)is a common modern preparation,but liver injury caused by Chinese patent medicine preparations containing EF and PF has been frequently reported in recent years.Zhuangguguanjiewan pills(ZGW),which contain EF and PF,could induce immune idiosyncratic liver injury according to clinical case reports and a nonhepatotoxic dose of lipopolysaccharide(LPS)model.This present study evaluated the liver injury induced by EF or PF alone or in combination and investigated the related mechanism by using the LPS model.Liver function indexes and pathological results showed that either EF or PF alone or in combination led to liver injury in normal rats;however,EF or PF alone could lead to liver injury in LPS-treated rats.Moreover,EF combined with PF could induce a greater degree of injury than that caused by EF or PF alone in LPS-treated rats.Furthermore,EF or PF alone or in combination enhanced the LPS-stimulated inflammatory cytokine production,implying that IL-1β,which is processed and released by activating the NLRP3 inflammasome,is a specific indicator of EF-induced immune idiosyncratic hepatotoxicity.Thus,EF may induce liver injury through enhancing the LPS-mediated proinflammatory cytokine production and activating the NLRP3 inflammasome.In addition,the metabolomics analysis results showed that PF affected more metabolites in glycerophospholipid and sphingolipid metabolic pathways compared with EF in LPS model,suggesting that PF increased the responsiveness of the liver to LPS or other inflammatory mediators via modulation of multiple metabolic pathways.Therefore,EF and PF combination indicates traditional Chinese medicine incompatibility,considering that it induces idiosyncratic hepatotoxicity under immunological stress conditions.
基金financial support by Key Scientific Research Projects in 2015 at North Minzu University(2015KJ33)Key Scientific Research Projects in 2017 at North Minzu University(2017KJ29)+1 种基金Natural Science Foundation of Ningxia(NZ 16089)Innovative Research Team of Ningxia Hui Autonomous Region for Functional Materials and Separation Technology
文摘Lycii Fructus（Lycium barbarum, Gouqizi in Chinese name） is one of the most popular Chinese material medica and a common ingredient in tonic food. This fruit has been paid rapidly growing attention for its nutrient value and noticeable pharmacological properties. The present paper focuses on the legal resource of Gouqizi and reviews the main research in medicinal field including botanical identification,ethnopharmacological functions, phytochemistry, pharmacological effects, clinic usages, and safety issues.In addition, some issues needed address will be also discussed. We strongly believe that further investigation will deepen our knowledge of Gouqizi and promote the industrial development in the world.
基金supported by National Natural Science Foundation of China(No.21067004)Research Fund for the Doctoral Program of Jiangxi University of Science and Technology(22020)
文摘Objective It is imperative to provide some consistent experimental results for the extraction of flavonid from Fructus Gardeniae. Methods The key extraction parameters that influenced the yield of flavonid from Fructus Gardeniae were optimized by employing an orthogonal experiment [L9（3）4], including the ratio of buffer solution （Na2B4O7· 10H2O） to raw material, concentration of Fructus Gardeniae in extracting solution, extraction time and pH of buffer solution. An UV/Vis detector was used to perform the qualitative and quantitative analyses of the extracted flavonid with the using of the standard sample. Results The maximum extraction yield of the crude extract was 5.0533 （mg/g） after 20 min when the mass ratio of Na2B4O7 · 10H2O to raw material was 0.4%, the concentration of Fructus Gardeniae in the extraction solution was 1/12 （g/mL）, and pH of buffer solution was 4.5. The positive reactions to the Molish and HCI-Mg tests suggested that the extracted compound was flavonoid, and FTIR measurements also identified the presence of flavonoid in the extracts. Conclusion This work is expected to provide a basis for further research, development, and utilization of Fructus gardenia in flavonid extraction.
基金This work has been supported by the Beijing Nova Program(No.Z181100006218001)the National Natural Science Foundation of China(Nos.81874368,81630100,81903891,and 81573676)+1 种基金the National Science and Technology Major Project “Key New Drug Creation and Manufacturing Program”(Nos.2017ZX09301022 and 2018ZX09101002-001-002)the Innovation Groups of the National Natural Science Foundation of China(No.81721002).
文摘Psoraleae Fructus(PF)is a well-known traditional herbal medicine in China,and it is widely used for osteoporosis,vitiligo,and other diseases in clinical settings.However,liver injury caused by PF and its preparations has been frequently reported in recent years.Our previous studies have demonstrated that PF could cause idiosyncratic drug-induced liver injury(IDILI),but the mechanism underlying its hepatotoxicity remains unclear.This paper reports that bavachin isolated from PF enhances the specific stimuli-induced activation of the NLRP3 inflammasome and leads to hepatotoxicity.Bavachin boosts the secretion of IL-ip and caspase-1 caused by ATP or nigericin but not those induced by poly(I:C),monosodium urate crystal,or intracellular lipopolysaccharide.Bavachin does not affect AIM2 or NLRC4 inflammasome activation.Mechanistically,bavachin specifically increases the production of nigericin-induced mitochondrial reactive oxygen species among the most important upstream events in the activation of the NLRP3 inflammasome.Bavachin increases the levels of aspartate transaminase and alanine aminotransferase in serum and hepatocyte injury accompanied by the secretion of IL-ip via a mouse model of lipopolysaccharide-mediated susceptibility to IDILI.These results suggest that bavachin specifically enhances the ATP-or nigericin-induced activation of the NLRP3 inflammasome.Bavachin also potentially contributes to PF-induced idiosyncratic hepatotoxicity.Moreover,bavachin and PF should be evaded among patients with diseases linked to the ATP-or nigericin-mediated activation of the NLRP3 inflammasome,which may be a dangerous factor for liver injury.
基金financially supported by the Natural Science Foundation of Jiangsu Province(BK2011135)Found Project for Transformation of Scientific and Technological Achievements of Jiangsu Province(No.BZ2011053)+1 种基金Open Project of National First Class Key Discipline for Science of Chinese Materia Medica,Nanjing University of Chinese Medicine(No.2011ZYX2-013)Scientific Innovation Research of University Graduate of Jiangsu Province(CXZZ130626)
文摘The present study was designed to optimize the processing of Fructus Arctii by response surface methodology （RSM）. Based on single factor studies, a three-variable, three-level Box-Behnken design （BBD） was used to monitor the effects of independent variables, including processing temperature and time, on the dependent variables. Response surfaces and contour plots of the contents of total lignans, chlorogenic acid, arctiin, and aretigenin were obtained through ultraviolet and visible （UV-Vis） monitoring and high performance liquid chromatography （HPLC）. Fructus Arctii should be processed under heating in a pot at 311℃, medicine at 119℃ for 123s with flipping frequently. The experimental values under the optimized processing technology were consistent with the predicted values. In conclusion, RSM is an effective method to optimize the processing of traditional Chinese medicine （TCM）.
基金Supported by National Natural Science Foundation of China,No.81473506Natural Science Foundation of Zhejiang Province,No.LY13H030011State Administration of Traditional Chinese Medicine of Zhejiang Province,No.2013ZB050
文摘AIM: To examine the effect of aqueous fructus aurantii immaturus(FAI) extracts on the intestinal plexus of cathartic colons.METHODS: Cathartic colons were induced in rats with dahuang,a laxative used in traditional Chinese medicine. Once the model was established(after approximately 12 wk),rats were administered mosapride(1.54 mg/kg) or various doses of aqueous FAI extracts(1-4 g/kg) for 14 d. Transit function was assessed using an ink propulsion test. Rats were then sacrificed,and the ultramicrostructure of colonic tissue was examined using transmission electron microscopy. The expression of the 5-hydroxytryptamine receptor 4(5-HTR4) and neurofilament-H was assessed in colon tissues using real-time PCR,Western blot,and immunohistochemistry.RESULTS: Mosapride and high dose(4 g/kg) of aqueous FAI extracts significantly improved the bowel movement in cathartic colons compared to untreated model colons as measured by the intestinal transit rate(70.06 ± 7.25 and 72.02 ± 8.74,respectively,vs 64.12 ± 5.19; P < 0.05 for both). Compared to controls,the ultramicrostructure of cathartic colons showed signsof neural degeneration. Treatment with mosapride and aqueous FAI extracts resulted in recovery of ultrastructural pathology. Treatment with mosapride alone upregulated the gene and protein expression of 5-HTR4 compared to untreated controls(P < 0.05 for both). Treatment with aqueous FAI extracts(≥ 2 g/kg) increased 5-HTR4 m RNA levels(P < 0.05),but no change in protein level was observed by Western blot or immunohistochemistry. The m RNA and protein levels of neurofilament-H were significantly increased with mosapride and ≥ 2 g/kg aqueous FAI extracts compared to controls(P < 0.05 for all).CONCLUSION: Aqueous FAI extracts and mosapride strengthen bowel movement in cathartic colons via increasing the expression of 5-HTR4 and neurofilament-H.
文摘Alternariol caused DNA single-strand breakage. Conversion of the closed circular double-stranded supercoiled DNA (pBR 322) to the nicked circular form and linear form was used to investigate the effect of extracts of some Chinese medical herbs on DNA nicking induced by alternariol. Some substances in the extracts of Rhizoma polygonati (RP) and Fructus lycii (FL) were shown to protect DNA from the attack by alternariol.Some substance in the RP may bind to plasmid DNA, and this binding reduces the electrophoretic mobility of DNA. These results indicate that substances from FL and RP may be used as DNA protectors. It is possible that they play an important role in preventing cancer.
基金supported by the NSF of China(Nos.81922070,81973286,81773687)the National Key Research and Development Program of China(No.2017YFC1700200,2017YFC1702000)+3 种基金Program of Shanghai Academic/Technology Research Leader(No.18XD1403600)Shuguang Program(No.18SG40)Program for applied basic research of Qinghai Provincial Science and Technology Department(No.2017-ZJ-713)Program for Innovative Leading Talents of Qinghai Province(2018&2019)
文摘Psoraleae Fructus(the dried fruits of Psoralea corylifolia), one of the most frequently used Chinese herbs in Asian countries, has a variety of biological activities. In clinical settings, Psoraleae Fructus or Psoraleae Fructus-related herbal medicines frequently have been used in combination with a number of therapeutic drugs for the treatment of various human diseases, such as leukoderma, rheumatism and dysentery. The use of Psoraleae Fructus in combination with drugs has aroused concern of the potential risks of herb-drug interactions(HDI) or herb-endobiotic interactions(HEI). This article reviews the interactions between human drug-metabolizing enzymes and the constituents of Psoraleae Fructus;the major constituents in Psoraleae Fructus, along with their chemical structures and metabolic pathways are summarized, and the inhibitory and inductive effects of the constituents in Psoraleae Fructus on human drug-metabolizing enzymes(DMEs), including target enzyme(s), its modulatory potency, and mechanisms of action are presented. Collectively, this review summarizes current knowledge of the interactions between the Chinese herb Psoraleae Fructus and therapeutic drugs in an effort to facilitate its rational use in clinical settings, and especially to avoid the potential risks of HDI or HEI through human DMEs.
文摘A simple,rapid and sensitive liquid chromatography-mass spectrometry（LC-MS）method was developed for the determination of salidroside in rat plasma and study of its pharmacokinetics after oral administration of suspension of Erzhi Wan and Fructus Ligustri lucidi into Wistar rats.Plasma sample of 200 μL was extracted with acetic ether-isopropanol（2∶1）and the extraction was performed on a Kromasil C18 column（150 mm×4.6 mm,5 μm）with the mobile phase of methanol-water（41∶59,v/v）within a run time of 6.0 min.The analyte was monitored with positive electrospray ionization（ESI）by selected ion monitoring（SIM）mode.The target ions were m/z 323.05 for salidroside and m/z 411.05 for internal standard（IS）geniposide.A good linear relationship was obtained over the range of 5.0-500.0 ng/mL and the lower limit of quantification was 5.0 ng/mL.The validated method was successfully applied to the pharmacokinetic study of salidroside in rat plasma after oral administration of suspension of Erzhi Wan and Fructus Ligustri lucidi.
基金Project supported by the Scientific Project of the Dezhou Government (2006067)the Science Fundation of Shandong Province (Q2008B08)the Key Technologies R&D Programme of Shandong Province (2010GSF10615)
文摘Flos Sophorae and Fructus Sophorae are two kinds of traditional Chinese medicines. In this work, the two kinds of traditional Chinese medicines collected from eleven areas of Dezhou, were analyzed by inductively couple plasma-mass spectrometry （ICP-MS） to compare the content and distribution of 14 kinds of rare earth elements （REEs）. The method was verified by analyzing GBW07605 certified reference material. The results showed that ICP-MS is an accurate, sensitive and reliable technique for determining REEs in traditional Chinese medicine. There were big differences in contents for REEs in Flos Sophorae and Fmctus Sophorae from different areas. The contents of total REEs in Flos Sophorae samples from different areas ranged from 1.0785 to 2.2659 μg/g, while those in Fmctus Sophorae from 0.6826 to 1.0527 ktg/g. The contents of total REEs in Flos Sophorae samples from different areas were obviously higher than those in Fmctus Sophorae of the same area and there was big difference between various Flos Sophorae samples. Interestingly, the higher the content of total REEs in Flos Sophorae samples, the lower the content of total REEs in Fmctus Sophorae samples of the same area. The plots of normalized element concentration versus atomic number showed some characteristic distribution trends. The distribution trend of light REEs （La-Gd） was relatively fiat except a positive Eu anomaly, however, that was steep and discrepant for heavy REEs （Tb-Lu）. The results could provide a valuable reference for understanding the relationship between the curative mechanism, pharmacology characteristics and their geological condition for the two traditional Chinese medicines investigated.
基金supported by Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine(No.2010JZ-W-01)Ministry of Education,PRC,and National Key Technology R&D Program“New Drug Innovation”of China(Nos.2009ZX09308-004,2013ZX09103002-006)
文摘Four prenylated flavonoids compounds 1-4,named sinopodophyllines A-D,and a flavonoid glycoside(compound 13),sinopodophylliside A,together with 19 known compounds(compounds 5-12 and 14-24) were isolated from the fruits of Sinopodophyllum hexandrum.The structures of new compounds were elucidated by extensive spectroscopic analysis,including HRESIMS,1D and 2D NMR.Compounds 1-6,9-11,and 14-17 were tested for their cytotoxicity against human breast-cancer T47 D,MCF-7 and MDA-MB-231 cells in vitro,and compounds 2,5,6,10 and 11 showed significant cytotoxicity(IC50 values < 10 μmol·L^(-1))against T47 D cells.
基金Supported by the National Natural Science Foundation of China(No.81630100)Beijing Nova Program(No.Z181100006218001)Project of China PLA General Hospital(No.2019MBD-023)。
文摘Objective To analyze clinical feature and information of medication to explore the risk signals of preparations containing Psoraleae Fructus(BGZP)related with hepatobiliary adverse drug reactions(ADR),in order to reinforce pharmacovigilance.Methods A retrospective study was conducted based on hepatobiliary ADR related with BGZP from the China Adverse Drug Reaction Monitoring System in years from January 2012 to December 2016.Serious and general ADRs were analyzed and assessed.Results There were 355 cases of hepatobiliary ADR related to BGZP.Both the amount of cases and the proportion of serious ADR showed an increasing growth by years(P<0.05).It was found that 10.43%of 355 cases may be involved with irrational drug use,including overdose,repeated medication,and combination of multiple drugs.There were 190 cases which used BGZP(non-combination),and they were mainly for common in diseases caused by abnormal immune activation(accounting for 40.53%of the total cases).Especially at the age group with the most cases with age of 41–50 years,the cases associated with immunological diseases of female were obviously more than that of male(P<0.05).The latency of hepatobiliary ADR related to BGZP ranged from 1 to 386 days,and the median latency was 27.5 days,along with the range of cumulative dose(0.45–520.02 g)as well as the daily dose(0.09–2.64 g/d)after the conversion.Conclusions Cases of hepatobiliary ADR related to BGZP showed significant individual differences,and there was no correlation between drug usage duration and dosage and the occurrence of hepatobiliary ADR.It may be similar with idiosyncratic drug-induced liver injury,and recommended that BGZP should be used with more caution under monitoring liver function,especially in female patients with immunological diseases.
基金supported by the the National Key Research and Development Program, Specialized Research on Modernization of TCM (Nos. 2018YFC1708006 and 2018YFC1708003)National Major New Drug Creation Special Project “National Drug New Varieties Research and Development and Its Key Innovative Technology Topics” (No. 2017ZX09301060-005)+3 种基金the National Natural Science Foundation of China (No. 81320108029)Tianshan Cedar Plan (No. 2018XS21)National “Major Scientific and Technological Special Project for Significant New Drugs Creation” Project (No. 2015ZX09501004-002-004)Specific Fund for Pub-lic Interest Research of Traditional Chinese Medicine, Ministry of Finance of China (No. 201507004-002)。
文摘Fructus Psoraleae,which is commonly consumed for the treatment of osteoporosis,bone fracture,and leucoderma,induces liver injury.This study investigated the pathogenesis of the ethanol extract of Fructus Psoraleae(EEFP)-induced liver injury in rats.EEFP(1.35,1.80,and 2.25 g·kg^–1)was administrated to Sprague Dawley(SD)rats for 30 d.We measured liver chemistries,histopathology,and quantitative isobaric tags for relative and absolute quantitation(iTRAQ)-based protein profiling.EEFP demonstrated parameters suggestive of liver injury with changes in bile secretion,bile flow rate,and liver histopathology.iTRAQ analysis showed that a total of 4042 proteins were expressed in liver tissues of EEFP-treated and untreated rats.Among these proteins,81 were upregulated and 32 were downregulated in the treatment group.KEGG pathway analysis showed that the drug metabolic pathways of cytochrome P450,glutathione metabolism,glycerolipid metabolism,and bile secretion were enriched with differentially expressed proteins.The expression of key proteins related to the farnesoid X receptor(FXR),i.e.,the peroxisome proliferators-activated receptor alpha(PPAR-α),were downregulated,and multidrug resistance-associated protein 3(MRP3)was upregulated in the EEFP-treated rats.Our results provide evidence that EEFP may induce hepatotoxicity through various pathways.Furthermore,our study demonstrates changes in protein regulation using iTRAQ quantitative proteomics analysis.
