Unraveling the distribution of metabolites in traditional Chinese medicine(TCM)provides direct indications for understanding their regulatory and functional basis,which is of paramount significance for better utilizat...Unraveling the distribution of metabolites in traditional Chinese medicine(TCM)provides direct indications for understanding their regulatory and functional basis,which is of paramount significance for better utilization and quality control of medicinal plants[1].Recently,imaging techniques such as near-infrared spectroscopy,Raman spectroscopy,and mass spectrometry(MS)were explored to reveal the spatial context of component accumulation and localization[2,3].展开更多
The seasonal and source variations of flavonoid contents in Scutellariae Radix were investigated by using the materials collected at the same place in Liaoning Province, China, during three years, 1990～1992, and in s...The seasonal and source variations of flavonoid contents in Scutellariae Radix were investigated by using the materials collected at the same place in Liaoning Province, China, during three years, 1990～1992, and in seven other provinces in China. Four principal flavonoids in the plant roots, i.e., baicalin, baicalein, wogonin 7 O glucuronide and wogonin were analyzed by using a reversed phase chromatographic system with a chemically bonded ODS silica gel column and phosphate buffer methanol (68:32 and 1:1) as mobile phase. The contents of the four compounds combined in the herb collected at Chengde, Hebei Province are the highest. The results show that the best time for harvesting the roots in Liaoning Province is the end of August.展开更多
AIM： To investigate the effect of Scutellariae Radix extract （SRE） on ulcerative colitis （UC） in rats induced by dextran-sulfate sodium （DSS）. METHODS： Colitis was induced in male Sprague-Dawley （SD） rats （...AIM： To investigate the effect of Scutellariae Radix extract （SRE） on ulcerative colitis （UC） in rats induced by dextran-sulfate sodium （DSS）. METHODS： Colitis was induced in male Sprague-Dawley （SD） rats （170-180 g） by 4% dextran sulfate sodium （DSS, wt/v, MW 54000） in drinking water for 8 d. The treated rats received 4% DSS and SRE orally （100 mg/kg per day）. Control rats received either tap water or SRE only. Macroscopic assessment which included body weight changes, fecal occult blood and stool consistency were determined daily. At the appointed time, the rats were sacrificed and the entire colons were removed. The colon length and the myeloperoxidase （MPO） activity were measured. The severity of colitis was graded by morphological and histological assessments. The ion transport activity of the colonic mucosa was assessed by electrophysiological technique. RESULTS： Rats treated with oral administration of 4% DSS regularly developed clinical and macroscopic signs of colitis. Treatment with SRE relieved the symptoms, including the reduction in body weight, shortening 2nd ulceration of the colon. Administration of SRE also significantly reduced the histological damage induced by DSS. Moreover, the Isc responses of the colonic mucosa to forskolin, were suppressed after the induction of colitis. The stimulated ion transport activity of DSS-rats treated with SRE displayed significant improvement in the secretory responsiveness. CONCLUSION： SRE was effective in treating acute DSS- induced ulcerative colitis, as gauged by reduced clinical disease, improved macroscopic and histological damage scores, and enhanced recovery of normal colonic secretory function.展开更多
Breast cancer(BCa)is one of the most common malignant tumors that seriously affect women’s physical and mental health and even endanger their lives.Establishing a primary prevention program for BCa remains a challeng...Breast cancer(BCa)is one of the most common malignant tumors that seriously affect women’s physical and mental health and even endanger their lives.Establishing a primary prevention program for BCa remains a challenge.Traditional Chinese medicine,Scutellariae Radix(SR),has been used to treat BCa while its pharmacological mechanism is still unclear.This study aims to reveal the pharmacological mechanism of SR in the treatment of BCa.Chemical constituents of SR were obtained and the targets of the compound were identified via Traditional Chinese Medicine Systems Pharmacology Database(TCMSP).GeneCards and DrugBank databases were used to collect BCa’s related target genes.Disease-compound common target protein interaction network was established by using the STRING database.The network diagrams of the active component-action target and protein-protein interaction(PPI)networks were constructed by Cytoscape software.Gene Ontology(GO)and Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway enrichment analyses were carried out to further explore the BCa mechanism and therapeutic effect of SR.As a result,121 active compounds were obtained.The Venn diagram results showed that SR and BCa had 57 intersection targets,the more frequently targeted ones are TP53,JUN,CCND1,AKT1,which could affect biological processes such as response to steroid hormone and positive regulation of cell death.KEGG analysis revealed that these targets were related to IL-17 signaling pathway,p53 signaling pathway and PI3K-Akt signaling pathway.In conclusion,this study preliminarily verified the target and mode of action of SR in the treatment of BCa,laying a foundation for further research on its mechanism.展开更多
A novel extraction method of baicalin from radix scutellariae was explored in this study. Liquid-liquid continuous biphasic extraction was a new method, and showed the advantage of high extracting contents of total fl...A novel extraction method of baicalin from radix scutellariae was explored in this study. Liquid-liquid continuous biphasic extraction was a new method, and showed the advantage of high extracting contents of total flavone compared with one of the traditional methods. The novel extraction method which is easy to operate and has good reproducibility was much more effective than the traditional one.展开更多
Flavonoids are the main bioactive components of Radix Scutellariae, a well-known traditional Chinese medicine. After oral administration of Radix Scutellariae extract （RSE）, the bile, plasma and urine of rats were a...Flavonoids are the main bioactive components of Radix Scutellariae, a well-known traditional Chinese medicine. After oral administration of Radix Scutellariae extract （RSE）, the bile, plasma and urine of rats were analyzed to identify the absorbed parent components and metabolites by ultra-fast liquid chromatography coupled with ion trap time-of-flight mass spectrometry （UFLC-IT-TOF/MS）. A total of 36 different flavonoids, including 13 new metabolites, were identified or tentatively characterized in bile, plasma and urine of rats based on their fragmentation patterns. Among them, 16 flavonoids were identified in RSE in vitro, 25 flavonoids in rat bile, 15 flavonoids in rat plasma, and 14 flavonoids in rat urine. The results indicated that glucuronidation, sulfation and methylation were the major metabolic pathways of flavonoids. It is the first time that the metabolism of RSE was studied comprehensively.展开更多
Osteoporosis is a bone metabolic disease caused by the imbalance between osteoblasts and osteoclasts due to excess osteoclastogenesis,manifesting in the decrease of bone density and bone strength.Scutellariae Radix sh...Osteoporosis is a bone metabolic disease caused by the imbalance between osteoblasts and osteoclasts due to excess osteoclastogenesis,manifesting in the decrease of bone density and bone strength.Scutellariae Radix shows good anti-osteoporosis activity,but the effective component is still unclear.Cell membrane chromatography(CMC)is a biological affinity chromatography with membrane immobilized on a silica carrier as the stationary phase.It can realize a dynamical simulation of interactions between drugs and receptors on cell membrane,which is suitable for screening active compounds from complex systems.In this study,the components of Scutellariae Radix with potential anti-osteoporosis activity through inhibiting the differentiation from bone marrow mononuclear cells(BMMCs)to osteoclast were screened by a BMMC/CMC analytical system.Firstly,a new3-mercaptopropyltrimethoxysilane(MPTS)-modified BMMC/CMC stationary phase was developed to realize covalent binding with cell membrane fractions.By investigating the retention time(tR)of the positive drug,the life span of the MPTS-modified CMC columns was significantly improved from 3 to 12 days.Secondly,6 components of Scutellariae Radix were screened to show affinity to membrane receptors on BMMCs by a two-dimensional BMMC/CMC-TOFMS analytical system.Among them,tectochrysin demonstrated the best anti-osteoporosis effect in vitro,which has never been reported.We found that tectochrysin could inhibit the differentiation of BMMCs into osteoclasts induced by receptor activator of nuclear factor-κB ligand(RANKL)and macrophage colony-stimulating factor(M-CSF)in a concentration-dependent manner in vitro.In vivo,it significantly reduced the loss of bone trabeculae in ovariectomized mice,and decreased the level of C-terminal cross-linking telopeptides of type 1 collagen(CTX-1),tartrate-resistant acid phosphatase 5 b(TRAP-5 b),interleukin 6(IL-6)in serum.In conclusion,tectochrysin serves as a potential candidate in the treatment of osteoporosis.The proposed twodimensional MPTS-modified BMMC/CMC-TOFMS analytical system shows the advantages of longlife span and fast recognition ability,which is very suitable for infrequent cell lines.展开更多
A series of animal models are used to investigate the anti-depression mechanism of flavonoids in scutellariae radix （SR） in vivo. Depression-like behavior in mice was studied after intraperitoneal administra- tion o...A series of animal models are used to investigate the anti-depression mechanism of flavonoids in scutellariae radix （SR） in vivo. Depression-like behavior in mice was studied after intraperitoneal administra- tion of SR. The results showed that SR administered to mice by the intraperitoneal route obviously short- ened the duration in the tail suspension test and the forced swimming test, aggravated the symptoms of eyelid ptosis, akinesia, and mortality caused by reserpine, prolonged climbing times, affected the condi- tioned place preference, and increased sugar consumption in mice. However the SR did not affect the head twitches induced by 5-HTP, locomotor activity in mice, the toxicity of yohimbine, and the body temperature decrease caused by high dosage of apomorphine. The tests show that SR has some anti-depression effect related to the dopamine system. Furthermore another anti-depression mechanism was possible that could affect the mechanism of brain reward, bring positive reinforcement, and increase the sensitivity to euphoria in mice.展开更多
Background:It is widely accepted that the causes and mechanisms of abortion are very complicated.In China,Scutellariae Radix(SR)(Scutellaria baicalensis Georgi)is widely used as a traditional Chinese herbal medicine w...Background:It is widely accepted that the causes and mechanisms of abortion are very complicated.In China,Scutellariae Radix(SR)(Scutellaria baicalensis Georgi)is widely used as a traditional Chinese herbal medicine with anti-abortion effects.However,the chemical components and pharmacologic profiles of SR have not been elucidated.The network pharmacology approach can provide a system-level perspective to explore the components,targets,and mechanism of herbal medicines.Thus,this approach was employed to identify the absorbable compounds,potential targets,and signaling pathways associated with SR.Materials and Methods:In this study,we used the Lipinski rule and an oral bioavailability of>30%to identify the bioactive compounds in SR.Targets of the anti-abortion activity of SR were obtained from the PharmMapper website server database.The Search Tool for the Retrieval of Interacting Genes and DAVID databases were utilized to perform protein–protein interaction analysis and pathway enrichment analysis,respectively.Finally,Cytoscape software was used to visualize the active compound–target–Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway network of SR.Results:In total,286 chemical compounds were identified in SR;of these,27 compounds could be absorbed into the blood,and 10 compounds that had a high docking score with their corresponding targets were determined.These potentially active compounds of SR regulated 142 targets and clearly affected 29 KEGG pathways.From these targets,a total of 11 targets,which were expressed in the breast and female reproductive system,were associated with the anti-abortion effects of SR:EGFR,HRAS,HSP90 AA1,ESR1,PRKACA,SRC,GSK3 B,JAK2,IGF1 R,CDK2,and AR.In the KEGG pathway analysis,five pathways were related to the anti-abortion effect of SR,including the estrogen signaling pathway,the prolactin signaling pathway,progesterone-mediated oocyte maturation,and oocyte meiosis.Conclusions:The network pharmacology approach used in our study attempted to explain the mechanism of the anti-abortion effects of SR and has provided an alternative approach for the investigation of the effects of this complex compound.展开更多
OBJECTIVE:To decipher the antidepressant targets and mechanisms of Huangqin(Radix Scutellariae Baicalensis)(RSB)by a novel computational system based on prediction and experimental verification.METHODS:The putative ta...OBJECTIVE:To decipher the antidepressant targets and mechanisms of Huangqin(Radix Scutellariae Baicalensis)(RSB)by a novel computational system based on prediction and experimental verification.METHODS:The putative targets of RSB against depression were identified from Traditional Chinese Medicine Systems Pharmacology(TCMSP)and Drug Bank.Next,protein-protein interaction network of the anti-depression targets of RSB were identified,and differentially expressed genes(DEGs)of depression were mined from the NCBI database.Then,Kyoto Encyclopedia of Genes and Genomes and Gene Ontology were used to analysis the common targets.Finally,the selected pathways and functions were verified by experimentation.RESULTS:Thirty active compounds in RSB were predicted with high confidence by TCMSP and DrugBank,and seventy-one DEGs were identified in the GEO database.Besides,eight core target proteins were screened out by descending order of degree value,including ACHE,IL6,SLC6A4,FOS,SLC6A3,MAOB,DPP4,and JUN.These target genes were further found to be associated with pathways involved in neuronal apoptosis,such as pathways in cancer,Toll-like receptor signaling pathway,and TNF signaling.The cell proliferation assay and wound-healing assay results showed that RSB does not affect PC12 cell proliferation and chemotaxis.Unexpectedly,RSB protected PC12 cells from oxidative stress induced by H2O2 via inhibiting autophagy and apoptosis.We revealed significant changes in mice treated with 400 mg/kg RSB compared with the lipopolysaccharide mice.The possible mechanism for the antidepressive action of RSB is by reducing the expression of LC3-B in CA1 neurons.CONCLUSIONS:Our research partially expounds the mechanism of the antidepressant effect of RSB by the combination of network pharmacology prediction and experimental verification.Furthermore,it is also conducive to the application of Traditional Chinese Medicine within modern medicine.展开更多
The effect of Radix Scutellariae treated on type 2 diabetic rats has been investigated by a liquid chromatography coupled with tandem mass spectrometry（LC-MS/MS） based urinary quantitative approach.In this research,...The effect of Radix Scutellariae treated on type 2 diabetic rats has been investigated by a liquid chromatography coupled with tandem mass spectrometry（LC-MS/MS） based urinary quantitative approach.In this research,multiple reactions monitoring mode of MS/MS in LC-MS/MS analysis was used to quantitatively analyze the concentrations of 7 endogenous compounds in urine of normal control group,type 2 diabetic model group and Radix Scutellariae-treated group,and multivariate statistical analysis was utilized for MS data processing.The above-mentioned three groups can be distinguished via pattern recognition.The obtained results indicated that Radix Scutellariae affect the urinary metabolic profiling of type 2 diabetic rats on the polyol pathway,protein glycation reaction and amino acids metabolism pathway.According to these results,Radix Scutellariae should have the pharmacological effect on preventing or delaying the onset and progression of diabetes and its complications.展开更多
Background: The absence of a safe and effective therapy for recurrent spontaneous abortion due to a maternofetal failure in immunological tolerance remains an intractable clinical obstacle for surgeons. Recently, trad...Background: The absence of a safe and effective therapy for recurrent spontaneous abortion due to a maternofetal failure in immunological tolerance remains an intractable clinical obstacle for surgeons. Recently, traditional Chinese medicine has become a feasible alternative for certain diseases, including recurrent spontaneous abortion. However, because of the complex composition of the traditional Chinese medicine formula, its action mechanism remains unclear. Methods: We selected two isolated active ingredients (RAMP and baicalin) from the traditional Chinese medicine formula and used an abortion-prone CBA/J × DBA/2 model to simulate human RSA and compared the changes in fetal resorption rate, Treg cell percentage, and relevant cytokines before and after combination therapy. In addition, The mechanisms were preliminarily discussed using in vitro differentiation models. Results: In CBA/J × DBA/2 abortion-prone mice, the combination therapy resulted in a lower embryo resorption rate compared to that obtained with individual delivery of either RAMP or baicalin, thereby playing an embryo-protective role through the increase in Treg cells for the maintenance of maternal-fetal immune tolerance. In in vitro primary cell differentiation experiments, the concentration of Treg cells significantly increased from 11% to 17.9% after the combination therapy compared to that of the single administration group. Conclusion: the synergistic effects of RAMP and baicalin were responsible for Treg differentiation. The present study provides a solid basis for improving the applicability of traditional Chinese herbs in the treatment of recurrent spontaneous abortion.展开更多
Aim: This study aimed to investigate the protective effects of flavonoids from the stem and leaves of Scutellaria baicalensis Georgi (SSFs) against Aβ<sub>1-42</sub>-induced oligodendrocytes (OL) damage. ...Aim: This study aimed to investigate the protective effects of flavonoids from the stem and leaves of Scutellaria baicalensis Georgi (SSFs) against Aβ<sub>1-42</sub>-induced oligodendrocytes (OL) damage. Methods: Immunofluorescence was used for the detection of myelin-associated glycoprotein (MAG), a characteristic protein of rat oligodendrocytes (OLN-93 cells). To evaluate the potential protective effects of SSFs on OLN-93 cells injured by Aβ<sub>1-42</sub>, an injury model was established by subjecting OLN-93 cells to Aβ<sub>1-42</sub> exposed. Cell morphology was examined using an inverted microscope, while cell viability was assessed using the colorimetric method of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT). Additionally, lactate dehydrogenase (LDH) was measured using the pyruvic acid reduction assay. The Ginkgo biloba leaf extract (GBE) injection was used as a positive control. Results: A total of >95% of the MAG immunofluorescence-positive cells were identified as oligodendrocytes. Gradually increasing concentrations of SSFs impaired the cells, and the maximum nondetrimental dose for OLN-93 cells was 75 mg/L. This study assessed the effects of SSFs on OLN-93 cells damaged by Aβ<sub>1-42</sub>. The results indicated that SSFs significantly improved OLN-93 cell morphological abnormal changes, increased the OLN-93 cell survival rate, and reduced LDH release. Conclusion: SSFs can alleviate Aβ<sub>1-42</sub>-induced damage of OL.展开更多
OBJECTIVE： To establish and optimize the propaga- tion of Nianmaohuangqin （Radix Scutellariae Viscid- ulae） and induce and characterize polyploidy of Nianmaohuangqin （Radix Scutellariae Viscidulae）. METHODS： Bud...OBJECTIVE： To establish and optimize the propaga- tion of Nianmaohuangqin （Radix Scutellariae Viscid- ulae） and induce and characterize polyploidy of Nianmaohuangqin （Radix Scutellariae Viscidulae）. METHODS： Buds from germinating seed-derived explants were induced by tissue culture. With an or- thogonal test, different concentrations of 6-benzyl- aminopurine （BAP）, indole-3-acetic acid （IAA） and kinetin （KT） were used to determine the optimal concentrations for the propagation of Nianmaohuangqin （Radix Scutellariae Viscidulae）. The differ- ent concentrations of IAA and rooting powder （ABT） were used to induce rooting. A 0.3% w/v col- chicine solution was used to induce polyploidy and the induced buds was identified by root-tip chromosome determination and stomatal apparatus ob- servation. RESULTS： A large number of buds could be in- duced directly from epicotyl and hypocotyl ex- plants on Murashige and Skoog （MS） （Murashige and Skoog 1962） medium supplemented with 1.1-1.3 mg/L BAP and 0.2 mg/L IAA. Root induction and development could be observed within 20 days of inoculation on 1/2 MS medium supplemented with 0.2 mg/L IAA and 0.1 mg/L ABTo Furthermore, 27 lines of autotetraploid individuals were ob- tained with a plantlet chromosome number of 2n= 4x=36. CONCLUSION： Autotetraploid lines could be ob- tained through induction with colchicine in vitro, proving that this method might be used for plant selection and breeding.展开更多
Objective To analyze patent application status of Scutellaria Barbata industrial chain and provide some suggestions for its patent application and product development.Methods Patent data were collected through IncoPat...Objective To analyze patent application status of Scutellaria Barbata industrial chain and provide some suggestions for its patent application and product development.Methods Patent data were collected through IncoPat patent analysis system.Meanwhile,the patent analysis method combined with text mining method was adopted to analyze the situation and development trend of patent application in China’s Scutellaria Barbata industrial chain by using pie chart,bubble chart,trend chart and other visual charts to display the results.Results and Conclusion The patent application of Scutellaria Barbata in China mainly experienced three stages:Slow development,rapid development,and recession period.The number of patents is large,but the authorization rate is low.Individuals and enterprises are the main applicants for patent applications.Product development is involved in the whole industrial chain,but it basically focuses on its efficacy in downstream drugs,health food and other aspects.Therefore,government should enhance the awareness of patent protection,encourage collaborative innovation in industry-university-research to promote the combination of basic research and market application.Besides,it should provide theoretical support to tackle the problem of short board products,which can promote the transformation of scientific and technological achievements and contribute to the upgrading of Scutellaria Barbata industrial chain.展开更多
Scutellariae Radix(SR), the root of Scutellaria baicalensis Georgi, is used as an antipyretic drug and has been demonstrated to have anti-inflammatory activity. SR is divided into two specifications, "Ku Qin"...Scutellariae Radix(SR), the root of Scutellaria baicalensis Georgi, is used as an antipyretic drug and has been demonstrated to have anti-inflammatory activity. SR is divided into two specifications, "Ku Qin"(KQ) and "Zi Qin"(ZQ), for use against different symptoms(upper energizer heat or lower portion of the triple energizer), according to the theory of traditional Chinese medicine(TCM). However, differences in the efficacies of these two specifications have not been determined. In the present study, we aimed to characterize the differences in the anti-inflammatory activities between KQ and ZQ and to explore how their differences are manifested in lipopolysaccharide(LPS)-induced macrophages. Our results showed that, in RAW264.7 cells(a mouse macrophage cell line derived from ascites), KQ and ZQ displayed anti-inflammatory effects by inhibiting the release of nitric oxide(NO), inducible NOS(iNOS), and nuclear factor-κB(NF-κB) in a dose-dependent manner without distinction. In NR8383 cells(a rat alveolar macrophage cell line), KQ and ZQ displayed similar effects on NO, iNOS, and NF-κB as seen in RAW264.7 cells, but KQ showed a higher inhibition rate for NO and i NOS than that shown by ZQ at the same concentration. These results indicated that there were differences in efficacy between KQ and ZQ in treating lung inflammation. Our findings provided an experimental evidence supporting the different uses of KQ and ZQ in clinic, as noted in ancient herbal records.展开更多
OBJECTIVE: To investigate the potential chronic liver toxicity of oral administration of ethanol extract of Huangqin(Radix Scutellariae Baicalensis)(SBE) in Wistar rats.METHODS: SBE was administered to rats by gavage ...OBJECTIVE: To investigate the potential chronic liver toxicity of oral administration of ethanol extract of Huangqin(Radix Scutellariae Baicalensis)(SBE) in Wistar rats.METHODS: SBE was administered to rats by gavage for 26 weeks, at doses of 300, 1250, or 2500 mg·kg-1·d-1 respectively. The rats were euthanized at the end of 13 and 26 weeks daily oral dosing and following 4 weeks of recovery time. The changes of hematology, urinary, blood biochemistry and histomorphology were examined at each time point and focus on liver function and histological changes.RESULTS: When SBE at a dose of up to 2500 mgkg-1 d-1 was fed to male and female rats for 2··6 weeks, the liver tissue showed some inflammatory change that predominated by leukocyte infiltrationbut returned to normal after withdrawal. In addition, high-dose SBE treatment of 26 weeks in rats,glucose, electrolyte and lipid levels also have some changes. In addition, there are no other functional or organic lesions related to SBE treatment.CONCLUSIONS: Long-term and high-dose SBE may cause liver damage, however, the structural damage of the liver can be restored after the ethanol extract stopping. SBE will be well-tolerated for long-term use as a drug or health food, but in order to ensure drug safety, liver function, and serum glucose, electrolyte and lipid levels should be monitored when using SBE long term.展开更多
基金supported by the National Natural Science Foundation of China(Grant No.:81773874).
文摘Unraveling the distribution of metabolites in traditional Chinese medicine(TCM)provides direct indications for understanding their regulatory and functional basis,which is of paramount significance for better utilization and quality control of medicinal plants[1].Recently,imaging techniques such as near-infrared spectroscopy,Raman spectroscopy,and mass spectrometry(MS)were explored to reveal the spatial context of component accumulation and localization[2,3].
文摘The seasonal and source variations of flavonoid contents in Scutellariae Radix were investigated by using the materials collected at the same place in Liaoning Province, China, during three years, 1990～1992, and in seven other provinces in China. Four principal flavonoids in the plant roots, i.e., baicalin, baicalein, wogonin 7 O glucuronide and wogonin were analyzed by using a reversed phase chromatographic system with a chemically bonded ODS silica gel column and phosphate buffer methanol (68:32 and 1:1) as mobile phase. The contents of the four compounds combined in the herb collected at Chengde, Hebei Province are the highest. The results show that the best time for harvesting the roots in Liaoning Province is the end of August.
基金a direct grant for research from The ChineseUniversity of Hong Kong,No. 2041075 awarded to Wing-HungKo
文摘AIM： To investigate the effect of Scutellariae Radix extract （SRE） on ulcerative colitis （UC） in rats induced by dextran-sulfate sodium （DSS）. METHODS： Colitis was induced in male Sprague-Dawley （SD） rats （170-180 g） by 4% dextran sulfate sodium （DSS, wt/v, MW 54000） in drinking water for 8 d. The treated rats received 4% DSS and SRE orally （100 mg/kg per day）. Control rats received either tap water or SRE only. Macroscopic assessment which included body weight changes, fecal occult blood and stool consistency were determined daily. At the appointed time, the rats were sacrificed and the entire colons were removed. The colon length and the myeloperoxidase （MPO） activity were measured. The severity of colitis was graded by morphological and histological assessments. The ion transport activity of the colonic mucosa was assessed by electrophysiological technique. RESULTS： Rats treated with oral administration of 4% DSS regularly developed clinical and macroscopic signs of colitis. Treatment with SRE relieved the symptoms, including the reduction in body weight, shortening 2nd ulceration of the colon. Administration of SRE also significantly reduced the histological damage induced by DSS. Moreover, the Isc responses of the colonic mucosa to forskolin, were suppressed after the induction of colitis. The stimulated ion transport activity of DSS-rats treated with SRE displayed significant improvement in the secretory responsiveness. CONCLUSION： SRE was effective in treating acute DSS- induced ulcerative colitis, as gauged by reduced clinical disease, improved macroscopic and histological damage scores, and enhanced recovery of normal colonic secretory function.
文摘Breast cancer(BCa)is one of the most common malignant tumors that seriously affect women’s physical and mental health and even endanger their lives.Establishing a primary prevention program for BCa remains a challenge.Traditional Chinese medicine,Scutellariae Radix(SR),has been used to treat BCa while its pharmacological mechanism is still unclear.This study aims to reveal the pharmacological mechanism of SR in the treatment of BCa.Chemical constituents of SR were obtained and the targets of the compound were identified via Traditional Chinese Medicine Systems Pharmacology Database(TCMSP).GeneCards and DrugBank databases were used to collect BCa’s related target genes.Disease-compound common target protein interaction network was established by using the STRING database.The network diagrams of the active component-action target and protein-protein interaction(PPI)networks were constructed by Cytoscape software.Gene Ontology(GO)and Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway enrichment analyses were carried out to further explore the BCa mechanism and therapeutic effect of SR.As a result,121 active compounds were obtained.The Venn diagram results showed that SR and BCa had 57 intersection targets,the more frequently targeted ones are TP53,JUN,CCND1,AKT1,which could affect biological processes such as response to steroid hormone and positive regulation of cell death.KEGG analysis revealed that these targets were related to IL-17 signaling pathway,p53 signaling pathway and PI3K-Akt signaling pathway.In conclusion,this study preliminarily verified the target and mode of action of SR in the treatment of BCa,laying a foundation for further research on its mechanism.
文摘A novel extraction method of baicalin from radix scutellariae was explored in this study. Liquid-liquid continuous biphasic extraction was a new method, and showed the advantage of high extracting contents of total flavone compared with one of the traditional methods. The novel extraction method which is easy to operate and has good reproducibility was much more effective than the traditional one.
基金National Key Special Project of Science and Technology for Innovation Drugs of China (Grant No. 2013ZX09402202)
文摘Flavonoids are the main bioactive components of Radix Scutellariae, a well-known traditional Chinese medicine. After oral administration of Radix Scutellariae extract （RSE）, the bile, plasma and urine of rats were analyzed to identify the absorbed parent components and metabolites by ultra-fast liquid chromatography coupled with ion trap time-of-flight mass spectrometry （UFLC-IT-TOF/MS）. A total of 36 different flavonoids, including 13 new metabolites, were identified or tentatively characterized in bile, plasma and urine of rats based on their fragmentation patterns. Among them, 16 flavonoids were identified in RSE in vitro, 25 flavonoids in rat bile, 15 flavonoids in rat plasma, and 14 flavonoids in rat urine. The results indicated that glucuronidation, sulfation and methylation were the major metabolic pathways of flavonoids. It is the first time that the metabolism of RSE was studied comprehensively.
基金supported by the National Natural Science Foundation of China(Grant Nos.81973291 to Xiaofei Chen,81573396 to Yifeng Chai,81973275 to Yongfang Yuan,81703674 to Yue Liu,81703779 to Rong Wang,81803815 to Shaozhan Wang and 81871099 to Xiao Chen)Fund of Shanghai Science and Technology Committee,China(19QA1411500 to Xiaofei Chen,17401900800 to Yongfang Yuan and 17YF1424700 to Yue Liu)
文摘Osteoporosis is a bone metabolic disease caused by the imbalance between osteoblasts and osteoclasts due to excess osteoclastogenesis,manifesting in the decrease of bone density and bone strength.Scutellariae Radix shows good anti-osteoporosis activity,but the effective component is still unclear.Cell membrane chromatography(CMC)is a biological affinity chromatography with membrane immobilized on a silica carrier as the stationary phase.It can realize a dynamical simulation of interactions between drugs and receptors on cell membrane,which is suitable for screening active compounds from complex systems.In this study,the components of Scutellariae Radix with potential anti-osteoporosis activity through inhibiting the differentiation from bone marrow mononuclear cells(BMMCs)to osteoclast were screened by a BMMC/CMC analytical system.Firstly,a new3-mercaptopropyltrimethoxysilane(MPTS)-modified BMMC/CMC stationary phase was developed to realize covalent binding with cell membrane fractions.By investigating the retention time(tR)of the positive drug,the life span of the MPTS-modified CMC columns was significantly improved from 3 to 12 days.Secondly,6 components of Scutellariae Radix were screened to show affinity to membrane receptors on BMMCs by a two-dimensional BMMC/CMC-TOFMS analytical system.Among them,tectochrysin demonstrated the best anti-osteoporosis effect in vitro,which has never been reported.We found that tectochrysin could inhibit the differentiation of BMMCs into osteoclasts induced by receptor activator of nuclear factor-κB ligand(RANKL)and macrophage colony-stimulating factor(M-CSF)in a concentration-dependent manner in vitro.In vivo,it significantly reduced the loss of bone trabeculae in ovariectomized mice,and decreased the level of C-terminal cross-linking telopeptides of type 1 collagen(CTX-1),tartrate-resistant acid phosphatase 5 b(TRAP-5 b),interleukin 6(IL-6)in serum.In conclusion,tectochrysin serves as a potential candidate in the treatment of osteoporosis.The proposed twodimensional MPTS-modified BMMC/CMC-TOFMS analytical system shows the advantages of longlife span and fast recognition ability,which is very suitable for infrequent cell lines.
基金Supported by the National Natural Science Foundation of China(Nos. 90713043, 30801523, and 30973896)the Key Technologies Research and Development Program of the Eleventh Five-Year Plan of China (Nos. 2006BAI08B03-09 and 2006BAI14B05)China’s Post-doctoral Science Fund (No. 20080440418)
文摘A series of animal models are used to investigate the anti-depression mechanism of flavonoids in scutellariae radix （SR） in vivo. Depression-like behavior in mice was studied after intraperitoneal administra- tion of SR. The results showed that SR administered to mice by the intraperitoneal route obviously short- ened the duration in the tail suspension test and the forced swimming test, aggravated the symptoms of eyelid ptosis, akinesia, and mortality caused by reserpine, prolonged climbing times, affected the condi- tioned place preference, and increased sugar consumption in mice. However the SR did not affect the head twitches induced by 5-HTP, locomotor activity in mice, the toxicity of yohimbine, and the body temperature decrease caused by high dosage of apomorphine. The tests show that SR has some anti-depression effect related to the dopamine system. Furthermore another anti-depression mechanism was possible that could affect the mechanism of brain reward, bring positive reinforcement, and increase the sensitivity to euphoria in mice.
基金2018 Sichuan Retirement and Old-age Health Collaborative Innovation Project,project number(No:YLZBZ1810)2017 Sichuan Provincial Health and Family Planning Commission Research Project(No:17PJ568)Innovation and Entrepreneurship Project of Chengdu Medical College in 2019,project number(No:s201913705109)。
文摘Background:It is widely accepted that the causes and mechanisms of abortion are very complicated.In China,Scutellariae Radix(SR)(Scutellaria baicalensis Georgi)is widely used as a traditional Chinese herbal medicine with anti-abortion effects.However,the chemical components and pharmacologic profiles of SR have not been elucidated.The network pharmacology approach can provide a system-level perspective to explore the components,targets,and mechanism of herbal medicines.Thus,this approach was employed to identify the absorbable compounds,potential targets,and signaling pathways associated with SR.Materials and Methods:In this study,we used the Lipinski rule and an oral bioavailability of>30%to identify the bioactive compounds in SR.Targets of the anti-abortion activity of SR were obtained from the PharmMapper website server database.The Search Tool for the Retrieval of Interacting Genes and DAVID databases were utilized to perform protein–protein interaction analysis and pathway enrichment analysis,respectively.Finally,Cytoscape software was used to visualize the active compound–target–Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway network of SR.Results:In total,286 chemical compounds were identified in SR;of these,27 compounds could be absorbed into the blood,and 10 compounds that had a high docking score with their corresponding targets were determined.These potentially active compounds of SR regulated 142 targets and clearly affected 29 KEGG pathways.From these targets,a total of 11 targets,which were expressed in the breast and female reproductive system,were associated with the anti-abortion effects of SR:EGFR,HRAS,HSP90 AA1,ESR1,PRKACA,SRC,GSK3 B,JAK2,IGF1 R,CDK2,and AR.In the KEGG pathway analysis,five pathways were related to the anti-abortion effect of SR,including the estrogen signaling pathway,the prolactin signaling pathway,progesterone-mediated oocyte maturation,and oocyte meiosis.Conclusions:The network pharmacology approach used in our study attempted to explain the mechanism of the anti-abortion effects of SR and has provided an alternative approach for the investigation of the effects of this complex compound.
基金Supported by Scientific research project of TCM administration of Hebei province:Based on AC-c AMP-PKA-CREB-BDNF Pathway to Explore the Anti-Epilepsy and Improving Learning and Memory Mechanism of Turbid and Detoxifying Prescriptions(No.2020176)National key research and development projects:Demonstration Study on Large-Scale Cultivation and Targeted Poverty Alleviation of High-Quality Genuine Medicinal Materials Forsythia Suspensa,Sour Jujube and Scutellaria in Taihang Mountain-Collection,Evaluation and Screening of Germplasm Resources of Forsythia Suspensa,Sour Jujube and Huangqin(Radix Scutellariae Baicalensis)(No.2017YFC1701700)the Postgraduate Innovation Funding Project of Hebei University of Chinese Medicine:Study on the Mechanism of Huazhuo Jiedu Shugan Prescription Regulating the Cerebral Interstitial Fluid Microenvironment on the Occurrence and Behavioral Changes of Epilepsy(No.XCXZZBS2021016)。
文摘OBJECTIVE:To decipher the antidepressant targets and mechanisms of Huangqin(Radix Scutellariae Baicalensis)(RSB)by a novel computational system based on prediction and experimental verification.METHODS:The putative targets of RSB against depression were identified from Traditional Chinese Medicine Systems Pharmacology(TCMSP)and Drug Bank.Next,protein-protein interaction network of the anti-depression targets of RSB were identified,and differentially expressed genes(DEGs)of depression were mined from the NCBI database.Then,Kyoto Encyclopedia of Genes and Genomes and Gene Ontology were used to analysis the common targets.Finally,the selected pathways and functions were verified by experimentation.RESULTS:Thirty active compounds in RSB were predicted with high confidence by TCMSP and DrugBank,and seventy-one DEGs were identified in the GEO database.Besides,eight core target proteins were screened out by descending order of degree value,including ACHE,IL6,SLC6A4,FOS,SLC6A3,MAOB,DPP4,and JUN.These target genes were further found to be associated with pathways involved in neuronal apoptosis,such as pathways in cancer,Toll-like receptor signaling pathway,and TNF signaling.The cell proliferation assay and wound-healing assay results showed that RSB does not affect PC12 cell proliferation and chemotaxis.Unexpectedly,RSB protected PC12 cells from oxidative stress induced by H2O2 via inhibiting autophagy and apoptosis.We revealed significant changes in mice treated with 400 mg/kg RSB compared with the lipopolysaccharide mice.The possible mechanism for the antidepressive action of RSB is by reducing the expression of LC3-B in CA1 neurons.CONCLUSIONS:Our research partially expounds the mechanism of the antidepressant effect of RSB by the combination of network pharmacology prediction and experimental verification.Furthermore,it is also conducive to the application of Traditional Chinese Medicine within modern medicine.
基金supported by the National Natural Science Foundation of China(No.81373952,81473537)the Jilin province science and technology development projects(No.20150311039YY)
文摘The effect of Radix Scutellariae treated on type 2 diabetic rats has been investigated by a liquid chromatography coupled with tandem mass spectrometry（LC-MS/MS） based urinary quantitative approach.In this research,multiple reactions monitoring mode of MS/MS in LC-MS/MS analysis was used to quantitatively analyze the concentrations of 7 endogenous compounds in urine of normal control group,type 2 diabetic model group and Radix Scutellariae-treated group,and multivariate statistical analysis was utilized for MS data processing.The above-mentioned three groups can be distinguished via pattern recognition.The obtained results indicated that Radix Scutellariae affect the urinary metabolic profiling of type 2 diabetic rats on the polyol pathway,protein glycation reaction and amino acids metabolism pathway.According to these results,Radix Scutellariae should have the pharmacological effect on preventing or delaying the onset and progression of diabetes and its complications.
基金the National Natural Science Foundation of China(81973221)National Natural Science Foundation for Young Scientists of China(81603647)+2 种基金the Women and Children Health Talent Project of Jiangsu Province(FRC201785)the Chinese Clinical Medicine Innovation Center of Obstetrics,Gynecology,and Reproduction in Jiangsu Province(ZX202102)the Women and Children Health Science Foundation of Jiangsu Province(F202206).
文摘Background: The absence of a safe and effective therapy for recurrent spontaneous abortion due to a maternofetal failure in immunological tolerance remains an intractable clinical obstacle for surgeons. Recently, traditional Chinese medicine has become a feasible alternative for certain diseases, including recurrent spontaneous abortion. However, because of the complex composition of the traditional Chinese medicine formula, its action mechanism remains unclear. Methods: We selected two isolated active ingredients (RAMP and baicalin) from the traditional Chinese medicine formula and used an abortion-prone CBA/J × DBA/2 model to simulate human RSA and compared the changes in fetal resorption rate, Treg cell percentage, and relevant cytokines before and after combination therapy. In addition, The mechanisms were preliminarily discussed using in vitro differentiation models. Results: In CBA/J × DBA/2 abortion-prone mice, the combination therapy resulted in a lower embryo resorption rate compared to that obtained with individual delivery of either RAMP or baicalin, thereby playing an embryo-protective role through the increase in Treg cells for the maintenance of maternal-fetal immune tolerance. In in vitro primary cell differentiation experiments, the concentration of Treg cells significantly increased from 11% to 17.9% after the combination therapy compared to that of the single administration group. Conclusion: the synergistic effects of RAMP and baicalin were responsible for Treg differentiation. The present study provides a solid basis for improving the applicability of traditional Chinese herbs in the treatment of recurrent spontaneous abortion.
文摘Aim: This study aimed to investigate the protective effects of flavonoids from the stem and leaves of Scutellaria baicalensis Georgi (SSFs) against Aβ<sub>1-42</sub>-induced oligodendrocytes (OL) damage. Methods: Immunofluorescence was used for the detection of myelin-associated glycoprotein (MAG), a characteristic protein of rat oligodendrocytes (OLN-93 cells). To evaluate the potential protective effects of SSFs on OLN-93 cells injured by Aβ<sub>1-42</sub>, an injury model was established by subjecting OLN-93 cells to Aβ<sub>1-42</sub> exposed. Cell morphology was examined using an inverted microscope, while cell viability was assessed using the colorimetric method of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT). Additionally, lactate dehydrogenase (LDH) was measured using the pyruvic acid reduction assay. The Ginkgo biloba leaf extract (GBE) injection was used as a positive control. Results: A total of >95% of the MAG immunofluorescence-positive cells were identified as oligodendrocytes. Gradually increasing concentrations of SSFs impaired the cells, and the maximum nondetrimental dose for OLN-93 cells was 75 mg/L. This study assessed the effects of SSFs on OLN-93 cells damaged by Aβ<sub>1-42</sub>. The results indicated that SSFs significantly improved OLN-93 cell morphological abnormal changes, increased the OLN-93 cell survival rate, and reduced LDH release. Conclusion: SSFs can alleviate Aβ<sub>1-42</sub>-induced damage of OL.
基金Supported by the Natural Science Fund of Anhui University of Chinese Medicine (No.2010zr011B)the Natural Science Fund of Education Department of Anhui Province,China (No.KJ2011A191)
文摘OBJECTIVE： To establish and optimize the propaga- tion of Nianmaohuangqin （Radix Scutellariae Viscid- ulae） and induce and characterize polyploidy of Nianmaohuangqin （Radix Scutellariae Viscidulae）. METHODS： Buds from germinating seed-derived explants were induced by tissue culture. With an or- thogonal test, different concentrations of 6-benzyl- aminopurine （BAP）, indole-3-acetic acid （IAA） and kinetin （KT） were used to determine the optimal concentrations for the propagation of Nianmaohuangqin （Radix Scutellariae Viscidulae）. The differ- ent concentrations of IAA and rooting powder （ABT） were used to induce rooting. A 0.3% w/v col- chicine solution was used to induce polyploidy and the induced buds was identified by root-tip chromosome determination and stomatal apparatus ob- servation. RESULTS： A large number of buds could be in- duced directly from epicotyl and hypocotyl ex- plants on Murashige and Skoog （MS） （Murashige and Skoog 1962） medium supplemented with 1.1-1.3 mg/L BAP and 0.2 mg/L IAA. Root induction and development could be observed within 20 days of inoculation on 1/2 MS medium supplemented with 0.2 mg/L IAA and 0.1 mg/L ABTo Furthermore, 27 lines of autotetraploid individuals were ob- tained with a plantlet chromosome number of 2n= 4x=36. CONCLUSION： Autotetraploid lines could be ob- tained through induction with colchicine in vitro, proving that this method might be used for plant selection and breeding.
文摘Objective To analyze patent application status of Scutellaria Barbata industrial chain and provide some suggestions for its patent application and product development.Methods Patent data were collected through IncoPat patent analysis system.Meanwhile,the patent analysis method combined with text mining method was adopted to analyze the situation and development trend of patent application in China’s Scutellaria Barbata industrial chain by using pie chart,bubble chart,trend chart and other visual charts to display the results.Results and Conclusion The patent application of Scutellaria Barbata in China mainly experienced three stages:Slow development,rapid development,and recession period.The number of patents is large,but the authorization rate is low.Individuals and enterprises are the main applicants for patent applications.Product development is involved in the whole industrial chain,but it basically focuses on its efficacy in downstream drugs,health food and other aspects.Therefore,government should enhance the awareness of patent protection,encourage collaborative innovation in industry-university-research to promote the combination of basic research and market application.Besides,it should provide theoretical support to tackle the problem of short board products,which can promote the transformation of scientific and technological achievements and contribute to the upgrading of Scutellaria Barbata industrial chain.
基金supported by the National Natural Science Foundation of China(No.81373921)
文摘Scutellariae Radix(SR), the root of Scutellaria baicalensis Georgi, is used as an antipyretic drug and has been demonstrated to have anti-inflammatory activity. SR is divided into two specifications, "Ku Qin"(KQ) and "Zi Qin"(ZQ), for use against different symptoms(upper energizer heat or lower portion of the triple energizer), according to the theory of traditional Chinese medicine(TCM). However, differences in the efficacies of these two specifications have not been determined. In the present study, we aimed to characterize the differences in the anti-inflammatory activities between KQ and ZQ and to explore how their differences are manifested in lipopolysaccharide(LPS)-induced macrophages. Our results showed that, in RAW264.7 cells(a mouse macrophage cell line derived from ascites), KQ and ZQ displayed anti-inflammatory effects by inhibiting the release of nitric oxide(NO), inducible NOS(iNOS), and nuclear factor-κB(NF-κB) in a dose-dependent manner without distinction. In NR8383 cells(a rat alveolar macrophage cell line), KQ and ZQ displayed similar effects on NO, iNOS, and NF-κB as seen in RAW264.7 cells, but KQ showed a higher inhibition rate for NO and i NOS than that shown by ZQ at the same concentration. These results indicated that there were differences in efficacy between KQ and ZQ in treating lung inflammation. Our findings provided an experimental evidence supporting the different uses of KQ and ZQ in clinic, as noted in ancient herbal records.
基金Supported by Major National Science and Technology Projects of China(No.2015ZX09501004No.2014 ZX09304307001+1 种基金No.2014ZX09201022-004)Beijing Science and Technology Projects(No.Z161100004916025,No.Z151100000115012)
文摘OBJECTIVE: To investigate the potential chronic liver toxicity of oral administration of ethanol extract of Huangqin(Radix Scutellariae Baicalensis)(SBE) in Wistar rats.METHODS: SBE was administered to rats by gavage for 26 weeks, at doses of 300, 1250, or 2500 mg·kg-1·d-1 respectively. The rats were euthanized at the end of 13 and 26 weeks daily oral dosing and following 4 weeks of recovery time. The changes of hematology, urinary, blood biochemistry and histomorphology were examined at each time point and focus on liver function and histological changes.RESULTS: When SBE at a dose of up to 2500 mgkg-1 d-1 was fed to male and female rats for 2··6 weeks, the liver tissue showed some inflammatory change that predominated by leukocyte infiltrationbut returned to normal after withdrawal. In addition, high-dose SBE treatment of 26 weeks in rats,glucose, electrolyte and lipid levels also have some changes. In addition, there are no other functional or organic lesions related to SBE treatment.CONCLUSIONS: Long-term and high-dose SBE may cause liver damage, however, the structural damage of the liver can be restored after the ethanol extract stopping. SBE will be well-tolerated for long-term use as a drug or health food, but in order to ensure drug safety, liver function, and serum glucose, electrolyte and lipid levels should be monitored when using SBE long term.
