Gentianopsis barbata(G.barbata)represents a significant plant species with considerable ornamental and medicinal value in China.This investigation sought to elucidate the primary constituents within the plant and inve...Gentianopsis barbata(G.barbata)represents a significant plant species with considerable ornamental and medicinal value in China.This investigation sought to elucidate the primary constituents within the plant and investigate their pharmacological properties.Fifty triterpenoids(1-50),including nine previously undescribed compounds(1,2,7,10,20,28,29,37,and 41)were isolated and characterized from the whole plants of G.barbata.Notably,compounds 1 and 2 exhibited the novel 3,4;9,10-diseco-24-homo-cycloartane triterpenoid skeleton.The isolated triterpenoids demonstrated substantial anti-inflammatory activity through inhibition of tumor necrosis factorα(TNF-α)and interleukin-6(IL-6)cytokine secretion in LPS-induced RAW264.7 macrophages,and hepatoprotective effects by preventing tertbutyl hydroperoxide(t-BHP)-induced oxidative injury in HepG2 cells.These results demonstrate both the presence of diverse triterpenoids in G.barbata and their therapeutic potential for inflammatory and hepatic conditions,providing scientific evidence supporting the clinical application of this traditional Mongolian medicinal plant.展开更多
Lung cancer remains a leading cause of cancer-related mortality globally,with conventional therapies(chemotherapy,targeted agents)limited by severe toxicities and poor durability.Traditional Chinese medicine(TCMs)herb...Lung cancer remains a leading cause of cancer-related mortality globally,with conventional therapies(chemotherapy,targeted agents)limited by severe toxicities and poor durability.Traditional Chinese medicine(TCMs)herb pairs,particularly Scutellaria barbata–Lobelia chinensis(SL),have emerged as promising alternatives for their multitarget anti-lung cancer activity,but their material basis and mechanisms need systematic clarification.In TCM practice,SL herb pair exerts“heat-clearing and toxin-resolving”effects,aligning with the therapeutic principle of“resolving toxin to suppress tumor”for lung cancer.Phytochemical and pharmacological studies confirm its key active components,including flavonoids(baicalein,luteolin,quercetin),alkaloids,and polysaccharides.These components synergistically act through core signaling pathways:inhibiting angiogenesis via HIF-1α/VEGF axis;inducing apoptosis/autophagy through PI3K/AKT/mTOR and SIRT1/AMPK pathways;suppressing epithelial-mesenchymal transition(EMT)by targeting TGF-β/Smad and Wnt/β-catenin pathways;and regulating immune microenvironment via NLRP3 inflammasome and Th1/Th2 balance.This review systematically summarizes the multi-component(flavonoids,alkaloids)and multi-pathway mechanisms of SL herb pair,validating the scientific connotation of TCM’s“multi-target therapy”paradigm.It provides a theoretical basis for clinical application of SL herb pair and inspires the development of innovative lung cancer therapies(e.g.,component-based nano-drugs),bridging TCM practice with modern pharmacology.展开更多
The emergence of SARS-CoV-2 variants and drug-resistant mutants emphasizes the urgent need to develop novel antiviral agents.In the present study,we examined the therapeutic effect of the Chinese medicinal herb,Scutel...The emergence of SARS-CoV-2 variants and drug-resistant mutants emphasizes the urgent need to develop novel antiviral agents.In the present study,we examined the therapeutic effect of the Chinese medicinal herb,Scutellaria barbata D.Don(SBD),against SARS-CoV-2 infection both in vitro and in vivo.Using a viral replicon particle(VRP)-based mouse model of SARS-CoV-2 infection,our study revealed that SBD extracts can reduce viral load in mouse lungs and alleviate the viral induced pneumonia.In vitro antiviral determination further validated the direct acting antiviral efficacy of SBD extracts against SARS-CoV-2 replication.Mechanistic studies demonstrated that SBD can act against SARS-CoV2 replication by targeting both 3-chymotrypsin-like and papain-like cysteine proteases,via a combination of multiple active constituents.Moreover,SBD can modulate the host inflammation response in a bi-directional manner,which also contribute to the mitigation of viral induced acute lung injury.In summary,our study provides SBD as a promising therapeutic agent to combat SARS-CoV-2 infections that merit further development.展开更多
Objective:Despite the combination of Scutellaria barbata D.Don and Scleromitrion diffusum(Willd.)R.J.Wang(SB-SD)being a recognized Chinese medicinal herbal pair that is commonly used in the treatment of ovarian cancer...Objective:Despite the combination of Scutellaria barbata D.Don and Scleromitrion diffusum(Willd.)R.J.Wang(SB-SD)being a recognized Chinese medicinal herbal pair that is commonly used in the treatment of ovarian cancer,there is a poor understanding of their pharmacological mechanisms.This study examines the antitumor properties and potential mechanisms of SB-SD on human ovarian cancer A2780 cells through a multi-omics approach,establishing a pharmacological basis for clinical utilization.Methods:A range of mass ratios and reagents were used in the hot reflux extraction of SB-SD.The inhibitory effect of the SB-SD extracts on A2780 cell proliferation was assessed using the cell-counting kit 8assay.A zebrafish tumor implantation model was used to evaluate the effects of SB-SD extracts on tumor growth and metastasis in vivo.Transcriptomics and proteomics were used to investigate alterations in biological pathways in A2780 cells after treatment with different concentrations of SB-SD extract.Cell cycle,cell apoptosis,intracellular free iron concentration,intracellular reactive oxygen species(ROS)concentration,malondialdehyde(MDA),and mitochondrial membrane potential were measured.Real-time quantitative reverse transcription polymerase chain reaction and Western blotting were utilized to investigate the effects of heme catabolism and ferritinophagy on ferroptosis induced by SB-SD extract in A2780 cells.Results:The 70%ethanol extract of SB-SD(a mass ratio of 4:1)inhibited A2780 cell proliferation significantly with a half maximal inhibitory concentration of 660μg/m L in a concentration-and timedependent manner.Moreover,it effectively suppressed tumor growth and metastasis in a zebrafish tumor implantation model.SB-SD extract induced the accumulation of free iron,ROS,MDA,and mitochondrial damage in A2780 cells.The mechanisms might involve the upregulated expression of ferritinophagyrelated genes microtubule-associated protein 1 light chain 3,autophagy-related gene 5,and nuclear receptor coactivator 4.Conclusion:SB-SD extract effectively inhibited the development of ovarian cancer both in vitro and in vivo.Its mechanism of action involved inducing ferroptosis by facilitating heme catabolism and ferritinophagy.This herbal pair holds promise as a potential therapeutic option for ovarian cancer treatment and may be utilized in combination with routine treatment to improve the treatment outcomes of ovarian cancer patients.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
An ultra high performance liquid chromatography coupled with hybrid quadrupole-orbitrap mass spectrometry （UHPLC-quadrupole-orbitrap MS） method was developed to systematically analyze chemical constituents of Scutel...An ultra high performance liquid chromatography coupled with hybrid quadrupole-orbitrap mass spectrometry （UHPLC-quadrupole-orbitrap MS） method was developed to systematically analyze chemical constituents of Scutellaria barbata D. Don. The 70% methanol extract was separated on an Agilent Eclipse Plus Cl8 column （1.8μm, 150 mm×2.1 mm）, and eluted with a gradient of methanol-acetonitrile-water containing 0.1% formic acid at a flow rate of 0.25 mL/min. Constituents were identified by HRMS in the negative ion mode using both full scan and two-stage threshold-triggered mass modes. A total of 56 compounds, including 20 free flavonoids, 20 flavonoid O-glycosides, 2 flavonoid C-glycosides, 4 phenylethanoid glycosides, and 10 phenolic compounds were identified by analyzing their high resolution mass spectral data. Among them, 8 flavonoids and 2 phenylethanoid glycosides were unambiguously identified by comparing with reference standards. This study demonstrates that hybrid quadrupole-orbitrap mass spectrometry is a powerful tool in structural identification of unknown compounds in comolicated herbal extracts.展开更多
AIM： To observe the attenuation of ethanol extract of Herba Scutellaria barbata （SE） against diabetic retinopathy （DR） and its engaged mechanism. METHODS： C57BL/6J mice were intraperitoneally injected with stre...AIM： To observe the attenuation of ethanol extract of Herba Scutellaria barbata （SE） against diabetic retinopathy （DR） and its engaged mechanism. METHODS： C57BL/6J mice were intraperitoneally injected with streptozotocin （STZ, 55 mg/kg） for 5 consecutive days to induce diabetes, The diabetic mice were orally given with SE （100, 200 mg/kg） for lmo at lmo after STZ injection. Blood-retinal barrier （BRB） breakdown was detected by using Evans blue permeation assay. Real-time polymerase chain reaction （RT-PCR）, Western blot and immunofiuorescence staining were used to detect mRNA and protein expression. Enzyme-linked immunosorbent assay （ELISA） was used to detect serum contents of tumor necrosis factor-e （TNF-a） and interleukin （IL）-II. RESULTS： SE （100, 200 mg/kg） reversed the breakdown of BRB in STZ-induced diabetic mice. The decreased expression of retinal claudin-1 and claudin-19, which are both tight junction （T J） proteins, was reversed by SE. SE decreased the increased serum contents and retinal mRNA expression of TNF-a and IL-113. SE also decreased the increased retinal expression of intercellular cell adhesion molecule-1 （ICAM-1）. SE reduced the increased phosphorylation of nuclear factor kappa B （NFKB） p65 and its subsequent nuclear translocation in retinas from STZ- induced diabetic mice. Results of Western blot and retinal immunofluorescence staining of ionized calcium-binding adapter molecule 1 （Ibal） demonstrated that SE abrogated the activation of microglia cells in STZ-induced diabetic mice. CONCLUSION： SE attenuates the development of DR by inhibiting retinal inflammation and restoring the decreased expression of TJ proteins including claudin-1 and claudin-19.展开更多
Three new monophenanthrene compounds were isolated from an acetone extract of the tubers of Monomeria barbata Lindl. (Orchidaceae).Using spectroscopic methods,the structures of compounds 1-3 were determined as 1,4,7-t...Three new monophenanthrene compounds were isolated from an acetone extract of the tubers of Monomeria barbata Lindl. (Orchidaceae).Using spectroscopic methods,the structures of compounds 1-3 were determined as 1,4,7-trihydroxy-2-methoxy- 9,10-dihydrophenanthrene(1),1-(p-hydroxybenzoyl)-2-methoxy-4,7-dihydroxy-9,10-dihydrophenanthrene(2),1,3,8-tri(p-hydroxybenzyl) -4-methoxy-phenanthrene-4,7-diol(3).These compounds showed cytotoxicities on four tumor cell lines(HepG2, HL-60,Skov-3,A431).展开更多
OBJECTIVE Hedyotis diffusa Willd and Scutellaria barbata D Don are most commonly used herb pair for cancer treatment in traditional Chinese medicine.This study aimed to evaluated the in vitro and in vivo antitumor eff...OBJECTIVE Hedyotis diffusa Willd and Scutellaria barbata D Don are most commonly used herb pair for cancer treatment in traditional Chinese medicine.This study aimed to evaluated the in vitro and in vivo antitumor effects and the compatibility mechanisms of Hedyotis diffusa-Sculellaria barbata herb pair.METHODS Hedyotic diffusa extract,Scutellariae Barbatae extract,and herb pair extract were prepared and the component were detected by UPLC-Q-TOF-MS.The effects of different concentrations of Hedyotic diffusa extract,Scutellariae Barbatae extract,and herb pair extract were detected using MTS assay.The in vivo antitumor effects were evaluated in Panc28 pancreatic cells bearing nude mice model.The compatibility mechanism of Hedyotis diffusa-Sculellaria barbata herb pair were evaluated based on the network pharmacology,using TCMSP,Cytoscape 3.6.1 software,and DAVID 6.8.The anticancer mechanism were further validated in vitro.RESULTS Both the MTS and in vivo results showed that herb pair extract showed more obvious inhibitory effects on cancer cells compared to each individual.A total of 37 active components were selected from Hedyotis diffusa and Sculellaria barbata,33 kinds of active ingredients are involved in their anti-tumor effects.58 cancer-related targets and 66 KEGG pathways were identified.The potential targets for the herb pair might be prostaglandin G/H synthase 2(PTGS2),HSP90,EGFR,72 ku typeⅣcollagenase,PPAR-γ,et al.In vitro validation result showed that compatibility mech⁃anisms was related with HSP90,EGFR related pathways.CONCLUSION The result of the study preliminarily verified the basic anti-tumor pharmacological effects of Hedyotis diffusa-Sculellaria barbata herb pair,and lays a solid foundation for further studies on the anti-tumor mechanism of the herbal pair.展开更多
OBJECTIVE To investigate the effect of SBF on cortical cytoplasm apoptotic factors disturbances induced by complex Aβ25-35in rats.METHODS The cerebral injuries model was established by rats received intracere-brovent...OBJECTIVE To investigate the effect of SBF on cortical cytoplasm apoptotic factors disturbances induced by complex Aβ25-35in rats.METHODS The cerebral injuries model was established by rats received intracere-broventricular injection of RHTGF-β1,Aβ25-35and Al Cl3and then accepted SBF treatment.All the rats were sacrificed by decapitation for indicators detection at last the drug treatment.Western blotting method was for caspase-3 protein expression and RT-PCR method detected cytochrome c,apoptotic protease activating factor-1(Apaf-1),caspase-9 m RNA expression in cortical cytoplasm.RESULTS The protein expression of caspase-3in cortical cytoplasm of rats was assayed by Western blotting.The results indicated that compared with the sham group,the caspase-3 protein expression of cortical cytoplasm in Aβgroup was significantly increased(P<0.01).However,the increased expression can be obviously reversed by SBF at doses of 35,70 and 140mg·kg-1,as compared with model group(P<0.01).The Cyt-C,Apaf-1 and caspase-9 m RNA expressions in cortical cytoplasm of rats were determined by RT-PCR.The results indicated that compared with the sham group,the Cyt-C Apaf-1 and caspase-9 m RNA relative expressions of cortical cytoplasm in Aβgroup was significantly increased(P<0.01).However,these increased expressions can be differently reversed by SBF at doses of 35,70 and 140 mg·kg-1,as compared with model group(P<0.01).CONCLUSION SBF can definitely improve rats′cortical cytoplasm apoptotic factors disorders induced by complex Aβ25-35,which maybe benefit for treatment of degenerative disease.展开更多
Avena barbata,a wild oat species within the genus Avena,is a widely used model for studying plant ecological adaptation due to its strong environmental adaptability and disease resistance,serving as a valuable genetic...Avena barbata,a wild oat species within the genus Avena,is a widely used model for studying plant ecological adaptation due to its strong environmental adaptability and disease resistance,serving as a valuable genetic resource for oat improvement.Here,we phased the high-quality chromosome-level genome assembly of A.barbata(6.88 Gb,contig N50=53.74 Mb)into A(3.57 Gb with 47,687 genes)and B(3.31 Gb with 46,029 genes)subgenomes.Comparative genomics and phylogenomic analyses clarified the evolutionary relationships and trajectories of A,B,C and D subgenomes in Avena.We inferred that the A subgenome donor of A.barbata was Avena hirtula,while the B subgenome donor was probably an extinct diploid species closely related to Avena wiestii.Genome evolution analysis revealed the dynamic transposable element(TE)content and subgenome divergence,as well as extensive structure variations across A,B,C,and D subgenomes in Avena.Population genetic analysis of 211 A.barbata accessions from distinct ecotypes identified several candidate genes related to environmental adaptability and drought resistance.Our study provides a comprehensive genetic resource for exploring the genetic basis underlying the strong environmental adaptability of A.barbata and the molecular identification of important agronomic traits for oat breeding.展开更多
Two new neo-clerodane diterpenoids, 6,7-dibenzoyloxybarbatin C （1, named barbatin D） and 6-（2-acetoxy-3-methylbutanoloxy）-7-（2-carbonyl-3-methylbutanoyloxy） barbatin C （2, named barbatin E） were isolated from ...Two new neo-clerodane diterpenoids, 6,7-dibenzoyloxybarbatin C （1, named barbatin D） and 6-（2-acetoxy-3-methylbutanoloxy）-7-（2-carbonyl-3-methylbutanoyloxy） barbatin C （2, named barbatin E） were isolated from the whole plant of Scutellaria barbata D. Don. Their structures were elucidated by spectroscopic methods including extensive 1 D and 2D NMR analyses. In vitro, compounds 1-2 showed cytotoxic activities against three human cancer lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, and with IC50 values in the range of 3.5-6.7μM.展开更多
Objective： To investigate the effect of the ethanol extract of Scutellaria barbata D. Don（EESB） on colorectal cancer（CRC） growth and Wnt/β-catenin signaling pathway in vivo and in vitro. Methods： In vivoexperim...Objective： To investigate the effect of the ethanol extract of Scutellaria barbata D. Don（EESB） on colorectal cancer（CRC） growth and Wnt/β-catenin signaling pathway in vivo and in vitro. Methods： In vivoexperiment, CRC xenograft mouse model was constructed with injection of HT-29 cells. Following xenograft implantation, twenty mice were randomly divided into EESB-treated group（n=10） and control group（n=10） by a random number table, and were given with intra-gastric administration of 2 g/kg EESB or saline, 5 days a week for 16 days, respectively. At the end of experiment, tumors were removed and weighed by electronic scales. The proliferation biomarker Ki-67 of tumor was evaluated by immunohistochemistry（IHC） assay. In vitro study, HT-29 cells were treated with 0, 0.5, 1.5, 2.5 mg/m L EESB for 24 h. At the end of the treatment, the viability and survival of HT-29 cells were determined by methylthiazolyldiphenyl-tetrazolium bromide（MTT） assay and colony formation assay, respectively. The m RNA expression of c-Myc, Survivin and adenomatous polyposis coli（APC） was examined by reverse transcription-polymerase chain reaction（RT-PCR） both in tumor tissues of CRC xenograft mice and HT-29 cells. Protein expression of c-Myc, Survivin, APC, and β-catenin as well as β-catenin phosphorylation level were evaluated by IHC assay or Western blotting. Results： EESB significantly reduced tumor weight in CRC xenografts mice, compared with the control group（P〈0.05）. IHC assay showed that EESB significantly inhibited protein expression of Ki-67 in tumor tissues（P〈0.05）. MTT assay showed that EESB significantly reduced HT-29 cell viability in a dose-dependent manner（P〈0.05）. Colony formation assay showed that EESB dose-dependently decreased the survival of HT-29 cells（P〈0.05）. In addition, RT-PCR assay showed that EESB decreased the m RNA expression of c-Myc and Survivin and increased APC expression, both in tumor tissues of CRC xenograft mice and HT-29 cells（P〈0.05）. IHC assay or Western blotting showed that EESB decreased protein expression of β-catenin, c-Myc and Survivin, as well as increased APC expression and β-catenin phosphorylation in tumor tissues or HT-29 cells（P〈0.05）. Conclusions： EESB significantly reduced tumor growth in CRC xenografts mice, and inhibited the viability and survival of HT-29 cells. EESB could suppress the activation of the Wnt/β-catenin pathway, which might be one of the mechanisms whereby Scutellaria barbata D. Don exerts its anticancer activity.展开更多
基金supported by the National Natural Science Foundation of China(Nos.21937006,U23A20510,82204245,82222072,and U24A20806)the Strategic Priority Research Program of the Chinese Academy of Sciences(No.XDB1230000)the Research Project of Yunnan Province(Nos.202401BC070016 and 202402AA310047)。
文摘Gentianopsis barbata(G.barbata)represents a significant plant species with considerable ornamental and medicinal value in China.This investigation sought to elucidate the primary constituents within the plant and investigate their pharmacological properties.Fifty triterpenoids(1-50),including nine previously undescribed compounds(1,2,7,10,20,28,29,37,and 41)were isolated and characterized from the whole plants of G.barbata.Notably,compounds 1 and 2 exhibited the novel 3,4;9,10-diseco-24-homo-cycloartane triterpenoid skeleton.The isolated triterpenoids demonstrated substantial anti-inflammatory activity through inhibition of tumor necrosis factorα(TNF-α)and interleukin-6(IL-6)cytokine secretion in LPS-induced RAW264.7 macrophages,and hepatoprotective effects by preventing tertbutyl hydroperoxide(t-BHP)-induced oxidative injury in HepG2 cells.These results demonstrate both the presence of diverse triterpenoids in G.barbata and their therapeutic potential for inflammatory and hepatic conditions,providing scientific evidence supporting the clinical application of this traditional Mongolian medicinal plant.
基金supported by the Wuxi Municipal Special Project for Scientific and Technological Development of Traditional Chinese Medicine for Young Talents(No.ZYQN202407).
文摘Lung cancer remains a leading cause of cancer-related mortality globally,with conventional therapies(chemotherapy,targeted agents)limited by severe toxicities and poor durability.Traditional Chinese medicine(TCMs)herb pairs,particularly Scutellaria barbata–Lobelia chinensis(SL),have emerged as promising alternatives for their multitarget anti-lung cancer activity,but their material basis and mechanisms need systematic clarification.In TCM practice,SL herb pair exerts“heat-clearing and toxin-resolving”effects,aligning with the therapeutic principle of“resolving toxin to suppress tumor”for lung cancer.Phytochemical and pharmacological studies confirm its key active components,including flavonoids(baicalein,luteolin,quercetin),alkaloids,and polysaccharides.These components synergistically act through core signaling pathways:inhibiting angiogenesis via HIF-1α/VEGF axis;inducing apoptosis/autophagy through PI3K/AKT/mTOR and SIRT1/AMPK pathways;suppressing epithelial-mesenchymal transition(EMT)by targeting TGF-β/Smad and Wnt/β-catenin pathways;and regulating immune microenvironment via NLRP3 inflammasome and Th1/Th2 balance.This review systematically summarizes the multi-component(flavonoids,alkaloids)and multi-pathway mechanisms of SL herb pair,validating the scientific connotation of TCM’s“multi-target therapy”paradigm.It provides a theoretical basis for clinical application of SL herb pair and inspires the development of innovative lung cancer therapies(e.g.,component-based nano-drugs),bridging TCM practice with modern pharmacology.
基金supported by the National Natural Science Foundation of China(82274204 and 82104134)the Natural Science Foundation of Shandong Province,China(ZR2024QH110)+1 种基金the Major Basic Program of Shandong Natural Science Foundation,China(ZR2021ZD17)the Project of Youth Innovation Team of Shandong Province(2022KJ254).
文摘The emergence of SARS-CoV-2 variants and drug-resistant mutants emphasizes the urgent need to develop novel antiviral agents.In the present study,we examined the therapeutic effect of the Chinese medicinal herb,Scutellaria barbata D.Don(SBD),against SARS-CoV-2 infection both in vitro and in vivo.Using a viral replicon particle(VRP)-based mouse model of SARS-CoV-2 infection,our study revealed that SBD extracts can reduce viral load in mouse lungs and alleviate the viral induced pneumonia.In vitro antiviral determination further validated the direct acting antiviral efficacy of SBD extracts against SARS-CoV-2 replication.Mechanistic studies demonstrated that SBD can act against SARS-CoV2 replication by targeting both 3-chymotrypsin-like and papain-like cysteine proteases,via a combination of multiple active constituents.Moreover,SBD can modulate the host inflammation response in a bi-directional manner,which also contribute to the mitigation of viral induced acute lung injury.In summary,our study provides SBD as a promising therapeutic agent to combat SARS-CoV-2 infections that merit further development.
基金supported by the National Natural Science Foundation of China(No.81873195)the Applied Basic Research Program of Liaoning Province(No.2023JH2/101300103)+1 种基金the Liaoning Revitalization Talents Program(No.XLYC1907113)the Dalian Medical University Foundation for Teaching Reform Project of Undergraduate Innovative Talents Training(No.111807010303)。
文摘Objective:Despite the combination of Scutellaria barbata D.Don and Scleromitrion diffusum(Willd.)R.J.Wang(SB-SD)being a recognized Chinese medicinal herbal pair that is commonly used in the treatment of ovarian cancer,there is a poor understanding of their pharmacological mechanisms.This study examines the antitumor properties and potential mechanisms of SB-SD on human ovarian cancer A2780 cells through a multi-omics approach,establishing a pharmacological basis for clinical utilization.Methods:A range of mass ratios and reagents were used in the hot reflux extraction of SB-SD.The inhibitory effect of the SB-SD extracts on A2780 cell proliferation was assessed using the cell-counting kit 8assay.A zebrafish tumor implantation model was used to evaluate the effects of SB-SD extracts on tumor growth and metastasis in vivo.Transcriptomics and proteomics were used to investigate alterations in biological pathways in A2780 cells after treatment with different concentrations of SB-SD extract.Cell cycle,cell apoptosis,intracellular free iron concentration,intracellular reactive oxygen species(ROS)concentration,malondialdehyde(MDA),and mitochondrial membrane potential were measured.Real-time quantitative reverse transcription polymerase chain reaction and Western blotting were utilized to investigate the effects of heme catabolism and ferritinophagy on ferroptosis induced by SB-SD extract in A2780 cells.Results:The 70%ethanol extract of SB-SD(a mass ratio of 4:1)inhibited A2780 cell proliferation significantly with a half maximal inhibitory concentration of 660μg/m L in a concentration-and timedependent manner.Moreover,it effectively suppressed tumor growth and metastasis in a zebrafish tumor implantation model.SB-SD extract induced the accumulation of free iron,ROS,MDA,and mitochondrial damage in A2780 cells.The mechanisms might involve the upregulated expression of ferritinophagyrelated genes microtubule-associated protein 1 light chain 3,autophagy-related gene 5,and nuclear receptor coactivator 4.Conclusion:SB-SD extract effectively inhibited the development of ovarian cancer both in vitro and in vivo.Its mechanism of action involved inducing ferroptosis by facilitating heme catabolism and ferritinophagy.This herbal pair holds promise as a potential therapeutic option for ovarian cancer treatment and may be utilized in combination with routine treatment to improve the treatment outcomes of ovarian cancer patients.
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National Natural Science Foundation of China(Grant No.81222054 and 21305005)the Program for New Century Excellent Talents in University from Chinese Ministry of Education(Grant No.NCET-11--0019)National Science and Technology Mega Project for Primary Drug Innovation of China(Grant No.2014ZX09304--307)
文摘An ultra high performance liquid chromatography coupled with hybrid quadrupole-orbitrap mass spectrometry （UHPLC-quadrupole-orbitrap MS） method was developed to systematically analyze chemical constituents of Scutellaria barbata D. Don. The 70% methanol extract was separated on an Agilent Eclipse Plus Cl8 column （1.8μm, 150 mm×2.1 mm）, and eluted with a gradient of methanol-acetonitrile-water containing 0.1% formic acid at a flow rate of 0.25 mL/min. Constituents were identified by HRMS in the negative ion mode using both full scan and two-stage threshold-triggered mass modes. A total of 56 compounds, including 20 free flavonoids, 20 flavonoid O-glycosides, 2 flavonoid C-glycosides, 4 phenylethanoid glycosides, and 10 phenolic compounds were identified by analyzing their high resolution mass spectral data. Among them, 8 flavonoids and 2 phenylethanoid glycosides were unambiguously identified by comparing with reference standards. This study demonstrates that hybrid quadrupole-orbitrap mass spectrometry is a powerful tool in structural identification of unknown compounds in comolicated herbal extracts.
基金Supported by the National Natural Science Foundation of China(No.81173517No.81322053)
文摘AIM： To observe the attenuation of ethanol extract of Herba Scutellaria barbata （SE） against diabetic retinopathy （DR） and its engaged mechanism. METHODS： C57BL/6J mice were intraperitoneally injected with streptozotocin （STZ, 55 mg/kg） for 5 consecutive days to induce diabetes, The diabetic mice were orally given with SE （100, 200 mg/kg） for lmo at lmo after STZ injection. Blood-retinal barrier （BRB） breakdown was detected by using Evans blue permeation assay. Real-time polymerase chain reaction （RT-PCR）, Western blot and immunofiuorescence staining were used to detect mRNA and protein expression. Enzyme-linked immunosorbent assay （ELISA） was used to detect serum contents of tumor necrosis factor-e （TNF-a） and interleukin （IL）-II. RESULTS： SE （100, 200 mg/kg） reversed the breakdown of BRB in STZ-induced diabetic mice. The decreased expression of retinal claudin-1 and claudin-19, which are both tight junction （T J） proteins, was reversed by SE. SE decreased the increased serum contents and retinal mRNA expression of TNF-a and IL-113. SE also decreased the increased retinal expression of intercellular cell adhesion molecule-1 （ICAM-1）. SE reduced the increased phosphorylation of nuclear factor kappa B （NFKB） p65 and its subsequent nuclear translocation in retinas from STZ- induced diabetic mice. Results of Western blot and retinal immunofluorescence staining of ionized calcium-binding adapter molecule 1 （Ibal） demonstrated that SE abrogated the activation of microglia cells in STZ-induced diabetic mice. CONCLUSION： SE attenuates the development of DR by inhibiting retinal inflammation and restoring the decreased expression of TJ proteins including claudin-1 and claudin-19.
基金supported by a program for New Century Excellent talents in University from MOE(No.NCET-08- 0925)a grant from the Natural Science Foundation of Yunnan Province(No.2007B021M)a grant from Yunnan University(No.2007Q003A)
文摘Three new monophenanthrene compounds were isolated from an acetone extract of the tubers of Monomeria barbata Lindl. (Orchidaceae).Using spectroscopic methods,the structures of compounds 1-3 were determined as 1,4,7-trihydroxy-2-methoxy- 9,10-dihydrophenanthrene(1),1-(p-hydroxybenzoyl)-2-methoxy-4,7-dihydroxy-9,10-dihydrophenanthrene(2),1,3,8-tri(p-hydroxybenzyl) -4-methoxy-phenanthrene-4,7-diol(3).These compounds showed cytotoxicities on four tumor cell lines(HepG2, HL-60,Skov-3,A431).
文摘OBJECTIVE Hedyotis diffusa Willd and Scutellaria barbata D Don are most commonly used herb pair for cancer treatment in traditional Chinese medicine.This study aimed to evaluated the in vitro and in vivo antitumor effects and the compatibility mechanisms of Hedyotis diffusa-Sculellaria barbata herb pair.METHODS Hedyotic diffusa extract,Scutellariae Barbatae extract,and herb pair extract were prepared and the component were detected by UPLC-Q-TOF-MS.The effects of different concentrations of Hedyotic diffusa extract,Scutellariae Barbatae extract,and herb pair extract were detected using MTS assay.The in vivo antitumor effects were evaluated in Panc28 pancreatic cells bearing nude mice model.The compatibility mechanism of Hedyotis diffusa-Sculellaria barbata herb pair were evaluated based on the network pharmacology,using TCMSP,Cytoscape 3.6.1 software,and DAVID 6.8.The anticancer mechanism were further validated in vitro.RESULTS Both the MTS and in vivo results showed that herb pair extract showed more obvious inhibitory effects on cancer cells compared to each individual.A total of 37 active components were selected from Hedyotis diffusa and Sculellaria barbata,33 kinds of active ingredients are involved in their anti-tumor effects.58 cancer-related targets and 66 KEGG pathways were identified.The potential targets for the herb pair might be prostaglandin G/H synthase 2(PTGS2),HSP90,EGFR,72 ku typeⅣcollagenase,PPAR-γ,et al.In vitro validation result showed that compatibility mech⁃anisms was related with HSP90,EGFR related pathways.CONCLUSION The result of the study preliminarily verified the basic anti-tumor pharmacological effects of Hedyotis diffusa-Sculellaria barbata herb pair,and lays a solid foundation for further studies on the anti-tumor mechanism of the herbal pair.
基金The project supported by Hebei Provincial Natural Science Foundation(C2009001007,H2014406048)Hebei Provincial Administration of Traditional Chinese Medicine of China(05027,2014062)the Key Discipline Construction in Institution of High Education in Hebei Province
文摘OBJECTIVE To investigate the effect of SBF on cortical cytoplasm apoptotic factors disturbances induced by complex Aβ25-35in rats.METHODS The cerebral injuries model was established by rats received intracere-broventricular injection of RHTGF-β1,Aβ25-35and Al Cl3and then accepted SBF treatment.All the rats were sacrificed by decapitation for indicators detection at last the drug treatment.Western blotting method was for caspase-3 protein expression and RT-PCR method detected cytochrome c,apoptotic protease activating factor-1(Apaf-1),caspase-9 m RNA expression in cortical cytoplasm.RESULTS The protein expression of caspase-3in cortical cytoplasm of rats was assayed by Western blotting.The results indicated that compared with the sham group,the caspase-3 protein expression of cortical cytoplasm in Aβgroup was significantly increased(P<0.01).However,the increased expression can be obviously reversed by SBF at doses of 35,70 and 140mg·kg-1,as compared with model group(P<0.01).The Cyt-C,Apaf-1 and caspase-9 m RNA expressions in cortical cytoplasm of rats were determined by RT-PCR.The results indicated that compared with the sham group,the Cyt-C Apaf-1 and caspase-9 m RNA relative expressions of cortical cytoplasm in Aβgroup was significantly increased(P<0.01).However,these increased expressions can be differently reversed by SBF at doses of 35,70 and 140 mg·kg-1,as compared with model group(P<0.01).CONCLUSION SBF can definitely improve rats′cortical cytoplasm apoptotic factors disorders induced by complex Aβ25-35,which maybe benefit for treatment of degenerative disease.
基金supported by the Young Elite Scientists Sponsorship Program by CAST Grant No.YESS20210080the National Natural Science Foundation of China(Grant No.32100500)+3 种基金the Natural Science Foundation of Hebei Province(Grant Nos:C2021201048 and C2023201074)the Interdisciplinary Research Program of Natural Science of Hebei University(Grant No:513201422004)The Excellent Youth Research Innovation Team of Hebei University(Grant No.QNTD202401)Funded by the Science and Technology Project of the Hebei Education Department(Grant No.QN2024271).
文摘Avena barbata,a wild oat species within the genus Avena,is a widely used model for studying plant ecological adaptation due to its strong environmental adaptability and disease resistance,serving as a valuable genetic resource for oat improvement.Here,we phased the high-quality chromosome-level genome assembly of A.barbata(6.88 Gb,contig N50=53.74 Mb)into A(3.57 Gb with 47,687 genes)and B(3.31 Gb with 46,029 genes)subgenomes.Comparative genomics and phylogenomic analyses clarified the evolutionary relationships and trajectories of A,B,C and D subgenomes in Avena.We inferred that the A subgenome donor of A.barbata was Avena hirtula,while the B subgenome donor was probably an extinct diploid species closely related to Avena wiestii.Genome evolution analysis revealed the dynamic transposable element(TE)content and subgenome divergence,as well as extensive structure variations across A,B,C,and D subgenomes in Avena.Population genetic analysis of 211 A.barbata accessions from distinct ecotypes identified several candidate genes related to environmental adaptability and drought resistance.Our study provides a comprehensive genetic resource for exploring the genetic basis underlying the strong environmental adaptability of A.barbata and the molecular identification of important agronomic traits for oat breeding.
基金the National Natural Science Foundation of China (20772104).
文摘Two new neo-clerodane diterpenoids, 6,7-dibenzoyloxybarbatin C （1, named barbatin D） and 6-（2-acetoxy-3-methylbutanoloxy）-7-（2-carbonyl-3-methylbutanoyloxy） barbatin C （2, named barbatin E） were isolated from the whole plant of Scutellaria barbata D. Don. Their structures were elucidated by spectroscopic methods including extensive 1 D and 2D NMR analyses. In vitro, compounds 1-2 showed cytotoxic activities against three human cancer lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, and with IC50 values in the range of 3.5-6.7μM.
基金Supported by the Natural Science Foundation of Fujian Province of China(No.2013J01333)the Youth Science Foundation of the Health Department of Fujian Province(2012-2-60)the Developmental Fund of Chen Keji Integrative Medicine(No.CKJ2015008)
文摘Objective： To investigate the effect of the ethanol extract of Scutellaria barbata D. Don（EESB） on colorectal cancer（CRC） growth and Wnt/β-catenin signaling pathway in vivo and in vitro. Methods： In vivoexperiment, CRC xenograft mouse model was constructed with injection of HT-29 cells. Following xenograft implantation, twenty mice were randomly divided into EESB-treated group（n=10） and control group（n=10） by a random number table, and were given with intra-gastric administration of 2 g/kg EESB or saline, 5 days a week for 16 days, respectively. At the end of experiment, tumors were removed and weighed by electronic scales. The proliferation biomarker Ki-67 of tumor was evaluated by immunohistochemistry（IHC） assay. In vitro study, HT-29 cells were treated with 0, 0.5, 1.5, 2.5 mg/m L EESB for 24 h. At the end of the treatment, the viability and survival of HT-29 cells were determined by methylthiazolyldiphenyl-tetrazolium bromide（MTT） assay and colony formation assay, respectively. The m RNA expression of c-Myc, Survivin and adenomatous polyposis coli（APC） was examined by reverse transcription-polymerase chain reaction（RT-PCR） both in tumor tissues of CRC xenograft mice and HT-29 cells. Protein expression of c-Myc, Survivin, APC, and β-catenin as well as β-catenin phosphorylation level were evaluated by IHC assay or Western blotting. Results： EESB significantly reduced tumor weight in CRC xenografts mice, compared with the control group（P〈0.05）. IHC assay showed that EESB significantly inhibited protein expression of Ki-67 in tumor tissues（P〈0.05）. MTT assay showed that EESB significantly reduced HT-29 cell viability in a dose-dependent manner（P〈0.05）. Colony formation assay showed that EESB dose-dependently decreased the survival of HT-29 cells（P〈0.05）. In addition, RT-PCR assay showed that EESB decreased the m RNA expression of c-Myc and Survivin and increased APC expression, both in tumor tissues of CRC xenograft mice and HT-29 cells（P〈0.05）. IHC assay or Western blotting showed that EESB decreased protein expression of β-catenin, c-Myc and Survivin, as well as increased APC expression and β-catenin phosphorylation in tumor tissues or HT-29 cells（P〈0.05）. Conclusions： EESB significantly reduced tumor growth in CRC xenografts mice, and inhibited the viability and survival of HT-29 cells. EESB could suppress the activation of the Wnt/β-catenin pathway, which might be one of the mechanisms whereby Scutellaria barbata D. Don exerts its anticancer activity.
