Objective:To investigate the effects of Alpiniae oxyphyllae Fructus(AOF)on renal lipid deposition in diabetic kidney disease(DKD)and elucidate its molecular mechanisms.Methods:The mechanism of AOF in treating DKD was ...Objective:To investigate the effects of Alpiniae oxyphyllae Fructus(AOF)on renal lipid deposition in diabetic kidney disease(DKD)and elucidate its molecular mechanisms.Methods:The mechanism of AOF in treating DKD was explored by network pharmacological enrichment analysis,molecular docking,and molecular dynamics simulation.The effects of AOF on renal function and lipid deposition were assessed in a mouse model of DKD and high glucose-stressed HK-2 cells.Cell viability and lipid accumulation were detected by CCK8 and oil red O staining.The expressions of PPARαand fatty acid oxidation-related genes(ACOX1 and CPT1A)were detected by quantitative RT-PCR,Western blot,and immunofluorescence.Furthermore,PPARαknockdown was performed to examine the molecular mechanism of AOF in treating DKD.Results:Network pharmacological enrichment analysis,molecular docking,and molecular dynamics simulation showed that the active compounds in AOF targeted PPARαand thus transcriptionally regulated ACOX1 and CPT1A.AOF lowered blood glucose,improved dyslipidemia,and attenuated renal injury in DKD mice.AOF-containing serum accentuated high glucose-induced decrease in cell viability and ameliorated lipid accumulation.Additionally,it significantly upregulated the expression of PPARα,ACOX1,and CPT1A in both in vivo and in vitro experiments,which was reversed by PPARαknockdown.Conclusions:AOF may promote fatty acid oxidation via PPARαto ameliorate renal lipid deposition in DKD.展开更多
Background:In this study,we analyzed the potential active components,related crucial targets and possible signaling pathway mechanisms of Alpiniae Oxyphyllae Fructus and Saposhnikoviae Radix(AOF-SR)herb pairs in the t...Background:In this study,we analyzed the potential active components,related crucial targets and possible signaling pathway mechanisms of Alpiniae Oxyphyllae Fructus and Saposhnikoviae Radix(AOF-SR)herb pairs in the treatment of diabetic kidney disease(DKD)using network pharmacology and verification experiments.Methods:The active compounds and potential targets of AOF-SR were derived from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,The Encyclopedia of Traditional Chinese Medicine,and PubChem databases,and the potential therapeutic targets of DKD were derived from the OMIM,Drugbank,and DisGeNET databases.The“compounds-diseases-targets”network was constructed using Cytoscape 3.6.0.ClusterMaker functionality in Cytoscape is being used to screen important targets for AOF-SR treatment of DKD.Gene Ontology and Kyoto Encyclopedia of Genes and Genomes enrichment analysis of important targets were performed using DAVID database.In addition,according to the predicted results of network pharmacology,HK-2 cells were used to construct DKD model for verification experiment.HK-2 cells were divided into control group,high glucose(HG)group and AOF-SR(HG+AOF-SR)group to detect survival rate and expression of key proteins in NF-κB and PI3K/Akt signaling pathways.Results:A total of 38 compounds were selected from AOF-SR,of which 23 were Alpiniae Oxyphyllae Fructus and 15 were Saposhnikoviae Radix.Through enrichment analysis of 82 important targets,88 signaling pathways were identified;some of these pathways,such as the NF-κB,PI3K-Akt,IL-17,and JAK/STAT signaling pathways,regulate the pathological process of DKD.In verification experiment,the HK-2 cells survival rate was higher in the HG+AOF-SR group than in the HG group(P<0.05).Moreover,western blotting results showed that the expression levels of NF-κB,p-PI3K,and p-Akt in HG+AOF-SR group were significantly lower than those in HG group(P<0.05).Conclusion:Overall,this study revealed the active compounds,important targets and possible mechanisms of AOF-SR treatment for DKD,and conducted preliminary verification experiments on its correctness,provided novel insights into the treatment of DKD by AOF-SR.展开更多
The study was designed to examine the apoptosis inducing activity of the AO-95 from the aerial part ofAlpiniae officinarum. The AO-95 treatment to three human lung cancer cell lines （A549, NCI-H460 and NCI-H23） resu...The study was designed to examine the apoptosis inducing activity of the AO-95 from the aerial part ofAlpiniae officinarum. The AO-95 treatment to three human lung cancer cell lines （A549, NCI-H460 and NCI-H23） resulted in a dose-dependent inhibition of cell growth. The authors selected A549 cell line as a test model system. The AO-95 induced apoptosis ofA549 obviously, as shown by the results of cell cycle distribution analysis and cell apoptosis assay. Treatment of A549 with AO-95 markedly decreased the mitochondrial transmembrane potential （△ψm） suggesting AO-95-induced apoptosis may involve a mitochondrial-related pathway. Two compounds were isolated from AO-95 and their structures were identified as 3-phenylpropanal and 4-phenylbutan-2-one. Meanwhile, ten different components accounting for 98.38% of the total A0-95 composition were identified by gas chromatography-mass spectrometry. The major components were 3-phenylpropanal （33.09%） and 4-phenylbutan-2-one （51.16%）. And these two compounds showed notable cytotoxic activity with IC50 values of 14.90-78.46 μg/mL. In summary, the AO-95, dominated by phenylpropanoid constituents, shows effective apoptosis inducing activity by mitochondrial-related pathway and may be developed as an agent against human lung cancer.展开更多
Objective:To investigate the therapeutic potential of octaarginine(R8)-modified essential oil from Fructus Alpiniae zerumbet(EOFAZ)lipid microspheres(EOFAZ@^(R8)LM)for cardiovascular therapy.Methods:EOFAZ@^(R8)LM was ...Objective:To investigate the therapeutic potential of octaarginine(R8)-modified essential oil from Fructus Alpiniae zerumbet(EOFAZ)lipid microspheres(EOFAZ@^(R8)LM)for cardiovascular therapy.Methods:EOFAZ@^(R8)LM was developed by leveraging the volatilization of EOFAZ and integrating it with the oil phase of LM,followed by surface modification with cell-penetrating peptide R8 to target the site of vascular endothelial injury.The therapeutic effects of this formulation in alleviating lipopolysaccharide-induced vascular endothelial inflammation were evaluated by assessing mitochondrial membrane potential(MMP),intracellular reactive oxygen species(ROS)levels,as well as inflammatory factors interleukin-6(IL-6)and interleukin-1β(IL-1β)levels.Results:EOFAZ@^(R8)LM effectively delivered EOFAZ to the site of injury and specifically targeted the mitochondria in vascular endothelial cells,thereby ameliorating mitochondrial dysfunction through regulation of MMP and reduction of intracellular ROS levels.Moreover,it attenuated the expression levels of IL-6 and IL-1β,exerting protective effects on the vascular endothelium.Conclusion:Our findings highlight the significant therapeutic potential of EOFAZ@^(R8)LM in cardiovascular therapy,providing valuable insights for developing novel dosage forms utilizing EOFAZ for effective treatment against cardiovascular diseases.展开更多
Objective:To investigate the separation and extraction process of the primary chemical constituents of Alpinia oxyphylla Miq.against Salmonella typhi,and its antibacterial effi cacy,providing theoretical basis for nov...Objective:To investigate the separation and extraction process of the primary chemical constituents of Alpinia oxyphylla Miq.against Salmonella typhi,and its antibacterial effi cacy,providing theoretical basis for novel gastrointestinal epidemic drugs and interventions against pathogen transmission.Methods:Alpinia oxyphylla Miq.:purified water-to-material ratio 1:5,refl uxed at 100°C for 6 hours,repeated three times.Alpinia oxyphylla Miq.extract was concentrated by freeze-drying at a 30:1 solid-to-liquid ratio to obtain the fi nal extract.The effi cacy of the extraction method and antibacterial activity were assessed using the disk diffusion method.The minimum inhibitory concentration(MIC)and minimum bactericidal concentration(MBC)were determined to establish the minimum therapeutic thresholds.Gas chromatography-mass spectrometry(GCMS)was employed to identify the primary bioactive constituents and their relative concentrations in the Alpinia oxyphylla Miq.aqueous extract.Results:The water extract of Alpinia oxyphylla Miq.Miq.demonstrated potent antibacterial activity against Salmonella typhi(P<0.001),with an inhibition zone diameter of 8.43±0.11 mm,MIC of 0.25 g/ml,and MBC of 0.5 g/ml.The extraction process was established as follows:Alpinia oxyphylla Miq.:purifi ed water ratio 1:5,refl ux heating at 100°C for 6 hours,repeated three times,followed by freeze-drying at 30:1 concentration.This yielded an extract rich in,primarily comprising octadecanoic acid(44.27%),palmitic acid(26.18%),caproic acid(8.15%),10-hydroxydecanoic acid(7.83%)as the main components,supplemented by 3-hydroxy-dodecanoic acid(1.78%),cis-13-eicosenoic acid(1.58%),valeric acid(1.21%),heptanoic acid(1.13%),nonanoic acid(1.06%),oleic acid(0.87%),and butyric acid(0.47%).Conclusion:This extraction process for novel antimicrobial compounds from Alpinia oxyphylla Miq.demonstrates high stability,operational feasibility,and precise composition and effi cacy.It provides a practical theoretical foundation for developing novel natural medicines against infectious diseases caused by Salmonella typhi,while off ering further insights for antimicrobial drug development.展开更多
Two novel 4,5-secoeudesmane sesquiterpenoids, oxyphyllones A （1） and B （2） were isolated from the fruits of Alpinia oxyphylla. Their structures were established by spectroscopic methods including 1D and 21） NMR s...Two novel 4,5-secoeudesmane sesquiterpenoids, oxyphyllones A （1） and B （2） were isolated from the fruits of Alpinia oxyphylla. Their structures were established by spectroscopic methods including 1D and 21） NMR spectra. These two compounds are the first example of naturally occurring sesquiterpenoids with a 4,5-secoeudesmane skeleton in the family of Zingiberaceae and oxyphyllone A （1） is the first 4,5-secoeudesmane type of 13-norsesquiterpenoid. Compounds 1 and 2 exhibited no cytotoxicities against three cancer cell lines at 10 μg/mL. ？ 2009 Ning Hua Tan. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.展开更多
Objective:To study the effect of Alpinia officinarum Hance(A.officinarum) 80% alcohol extract on the primary dysmenorrhea.Methods:A.officinarum 80% alcohol extract were enriched by macroporous adsorption resins.Female...Objective:To study the effect of Alpinia officinarum Hance(A.officinarum) 80% alcohol extract on the primary dysmenorrhea.Methods:A.officinarum 80% alcohol extract were enriched by macroporous adsorption resins.Female mice of primary dysmenorrhea model were established by oxytocin induction; the effects of A.officinarum 80% alcohol extract on primary dysmenorrhea were observed by body twist method; and the homogenate level of prostaglandin F_(2α)(PGF_(2α)),prostaglandin E_2(PGE_2) and Ca^(2+) in the uterus were observed in oxytocin-induced female mice.Results:The writhing frequency of primary dysmenorrhea mice was significantly decreased after treatment of A.officinarum 80% alcohol extract and the level of PGF_(2α),PGE_2 and Ca^(2+) in mice uterus was significantly decreased(P<0.05,P<0.01) in groups of mice treated with middle and high dosage of A.officinarum 80% alcohol extract compared with that of model group.Conclusions:These findings suggest that A.Officinarum 80% alcohol extract can significantly relieve primary dysmenorrhea.展开更多
A novel diarylheptanoid bearing flavonol moiety,named officinin A(1),along with two known compounds galangin and kaempferide were isolated from the rhizomes of Alpina officinarum Hance.The structure elucidation was ac...A novel diarylheptanoid bearing flavonol moiety,named officinin A(1),along with two known compounds galangin and kaempferide were isolated from the rhizomes of Alpina officinarum Hance.The structure elucidation was accomplished by HRESI -MS,1D and 2D NMR methods.展开更多
基金This work was supported by the grants from National Natural Science Foundation of China(No.82174334)2022 Postgraduate Innovation Research Projects in Hainan Province(No.Qhys2022-273).
文摘Objective:To investigate the effects of Alpiniae oxyphyllae Fructus(AOF)on renal lipid deposition in diabetic kidney disease(DKD)and elucidate its molecular mechanisms.Methods:The mechanism of AOF in treating DKD was explored by network pharmacological enrichment analysis,molecular docking,and molecular dynamics simulation.The effects of AOF on renal function and lipid deposition were assessed in a mouse model of DKD and high glucose-stressed HK-2 cells.Cell viability and lipid accumulation were detected by CCK8 and oil red O staining.The expressions of PPARαand fatty acid oxidation-related genes(ACOX1 and CPT1A)were detected by quantitative RT-PCR,Western blot,and immunofluorescence.Furthermore,PPARαknockdown was performed to examine the molecular mechanism of AOF in treating DKD.Results:Network pharmacological enrichment analysis,molecular docking,and molecular dynamics simulation showed that the active compounds in AOF targeted PPARαand thus transcriptionally regulated ACOX1 and CPT1A.AOF lowered blood glucose,improved dyslipidemia,and attenuated renal injury in DKD mice.AOF-containing serum accentuated high glucose-induced decrease in cell viability and ameliorated lipid accumulation.Additionally,it significantly upregulated the expression of PPARα,ACOX1,and CPT1A in both in vivo and in vitro experiments,which was reversed by PPARαknockdown.Conclusions:AOF may promote fatty acid oxidation via PPARαto ameliorate renal lipid deposition in DKD.
基金the National Natural Science Foundation of China(grant No.82160897,82205087)Hainan Provincial Natural Science Foundation of China(grant No.820RC635)+1 种基金Scientific Research Foundation of Hainan Medical University(grant No.HYPY201924,HYPY2020037)Hainan Medical University 2020 National Innovation and Entrepreneurship Program for College Students(grant No.202011810006).
文摘Background:In this study,we analyzed the potential active components,related crucial targets and possible signaling pathway mechanisms of Alpiniae Oxyphyllae Fructus and Saposhnikoviae Radix(AOF-SR)herb pairs in the treatment of diabetic kidney disease(DKD)using network pharmacology and verification experiments.Methods:The active compounds and potential targets of AOF-SR were derived from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,The Encyclopedia of Traditional Chinese Medicine,and PubChem databases,and the potential therapeutic targets of DKD were derived from the OMIM,Drugbank,and DisGeNET databases.The“compounds-diseases-targets”network was constructed using Cytoscape 3.6.0.ClusterMaker functionality in Cytoscape is being used to screen important targets for AOF-SR treatment of DKD.Gene Ontology and Kyoto Encyclopedia of Genes and Genomes enrichment analysis of important targets were performed using DAVID database.In addition,according to the predicted results of network pharmacology,HK-2 cells were used to construct DKD model for verification experiment.HK-2 cells were divided into control group,high glucose(HG)group and AOF-SR(HG+AOF-SR)group to detect survival rate and expression of key proteins in NF-κB and PI3K/Akt signaling pathways.Results:A total of 38 compounds were selected from AOF-SR,of which 23 were Alpiniae Oxyphyllae Fructus and 15 were Saposhnikoviae Radix.Through enrichment analysis of 82 important targets,88 signaling pathways were identified;some of these pathways,such as the NF-κB,PI3K-Akt,IL-17,and JAK/STAT signaling pathways,regulate the pathological process of DKD.In verification experiment,the HK-2 cells survival rate was higher in the HG+AOF-SR group than in the HG group(P<0.05).Moreover,western blotting results showed that the expression levels of NF-κB,p-PI3K,and p-Akt in HG+AOF-SR group were significantly lower than those in HG group(P<0.05).Conclusion:Overall,this study revealed the active compounds,important targets and possible mechanisms of AOF-SR treatment for DKD,and conducted preliminary verification experiments on its correctness,provided novel insights into the treatment of DKD by AOF-SR.
基金Acknowledgements This research was partly supported by the Start Fund of Guangdong Medical College （XB1302）, National Natural Science Foundation of China （31301585）, Science ＆ Technology Innovation Fund of Guangdong Medical College （STIF 201104）, and Shenzhen basic research project （JCYJ20120616142424467）.
文摘The study was designed to examine the apoptosis inducing activity of the AO-95 from the aerial part ofAlpiniae officinarum. The AO-95 treatment to three human lung cancer cell lines （A549, NCI-H460 and NCI-H23） resulted in a dose-dependent inhibition of cell growth. The authors selected A549 cell line as a test model system. The AO-95 induced apoptosis ofA549 obviously, as shown by the results of cell cycle distribution analysis and cell apoptosis assay. Treatment of A549 with AO-95 markedly decreased the mitochondrial transmembrane potential （△ψm） suggesting AO-95-induced apoptosis may involve a mitochondrial-related pathway. Two compounds were isolated from AO-95 and their structures were identified as 3-phenylpropanal and 4-phenylbutan-2-one. Meanwhile, ten different components accounting for 98.38% of the total A0-95 composition were identified by gas chromatography-mass spectrometry. The major components were 3-phenylpropanal （33.09%） and 4-phenylbutan-2-one （51.16%）. And these two compounds showed notable cytotoxic activity with IC50 values of 14.90-78.46 μg/mL. In summary, the AO-95, dominated by phenylpropanoid constituents, shows effective apoptosis inducing activity by mitochondrial-related pathway and may be developed as an agent against human lung cancer.
基金supported by the National Natural Science Foundation of China(Nos.82260827 and U1812403-4-4)the Guizhou Provincial Science Technology Project(No.ZK[2022]380)+3 种基金the Guizhou Provincial Natural Science Foundation(Nos.[2020]1Z069 and[2020]1Y210)the Guizhou Provincial Scientific and Technologic Innovation Base(No.[2023]003)the Cultivation Project of National Natural Science Foundation of Guizhou Medical University(Nos.21NSFCP47 and 20NSP053)the High level Innovation Talents(No.GCC[2023]048)。
文摘Objective:To investigate the therapeutic potential of octaarginine(R8)-modified essential oil from Fructus Alpiniae zerumbet(EOFAZ)lipid microspheres(EOFAZ@^(R8)LM)for cardiovascular therapy.Methods:EOFAZ@^(R8)LM was developed by leveraging the volatilization of EOFAZ and integrating it with the oil phase of LM,followed by surface modification with cell-penetrating peptide R8 to target the site of vascular endothelial injury.The therapeutic effects of this formulation in alleviating lipopolysaccharide-induced vascular endothelial inflammation were evaluated by assessing mitochondrial membrane potential(MMP),intracellular reactive oxygen species(ROS)levels,as well as inflammatory factors interleukin-6(IL-6)and interleukin-1β(IL-1β)levels.Results:EOFAZ@^(R8)LM effectively delivered EOFAZ to the site of injury and specifically targeted the mitochondria in vascular endothelial cells,thereby ameliorating mitochondrial dysfunction through regulation of MMP and reduction of intracellular ROS levels.Moreover,it attenuated the expression levels of IL-6 and IL-1β,exerting protective effects on the vascular endothelium.Conclusion:Our findings highlight the significant therapeutic potential of EOFAZ@^(R8)LM in cardiovascular therapy,providing valuable insights for developing novel dosage forms utilizing EOFAZ for effective treatment against cardiovascular diseases.
基金Hainan University of Science and Technology Institutional Research Grant(HKKY2024-87)Undergraduate Innovation and Entrepreneurship Training Programme(X202511049398)+1 种基金Undergraduate Innovation and Entrepreneurship Training Programme(X202511049201)Undergraduate Innovation and Entrepreneurship Training Programme(D202504071303298456)。
文摘Objective:To investigate the separation and extraction process of the primary chemical constituents of Alpinia oxyphylla Miq.against Salmonella typhi,and its antibacterial effi cacy,providing theoretical basis for novel gastrointestinal epidemic drugs and interventions against pathogen transmission.Methods:Alpinia oxyphylla Miq.:purified water-to-material ratio 1:5,refl uxed at 100°C for 6 hours,repeated three times.Alpinia oxyphylla Miq.extract was concentrated by freeze-drying at a 30:1 solid-to-liquid ratio to obtain the fi nal extract.The effi cacy of the extraction method and antibacterial activity were assessed using the disk diffusion method.The minimum inhibitory concentration(MIC)and minimum bactericidal concentration(MBC)were determined to establish the minimum therapeutic thresholds.Gas chromatography-mass spectrometry(GCMS)was employed to identify the primary bioactive constituents and their relative concentrations in the Alpinia oxyphylla Miq.aqueous extract.Results:The water extract of Alpinia oxyphylla Miq.Miq.demonstrated potent antibacterial activity against Salmonella typhi(P<0.001),with an inhibition zone diameter of 8.43±0.11 mm,MIC of 0.25 g/ml,and MBC of 0.5 g/ml.The extraction process was established as follows:Alpinia oxyphylla Miq.:purifi ed water ratio 1:5,refl ux heating at 100°C for 6 hours,repeated three times,followed by freeze-drying at 30:1 concentration.This yielded an extract rich in,primarily comprising octadecanoic acid(44.27%),palmitic acid(26.18%),caproic acid(8.15%),10-hydroxydecanoic acid(7.83%)as the main components,supplemented by 3-hydroxy-dodecanoic acid(1.78%),cis-13-eicosenoic acid(1.58%),valeric acid(1.21%),heptanoic acid(1.13%),nonanoic acid(1.06%),oleic acid(0.87%),and butyric acid(0.47%).Conclusion:This extraction process for novel antimicrobial compounds from Alpinia oxyphylla Miq.demonstrates high stability,operational feasibility,and precise composition and effi cacy.It provides a practical theoretical foundation for developing novel natural medicines against infectious diseases caused by Salmonella typhi,while off ering further insights for antimicrobial drug development.
基金supported by the grant from The National Natural Science Foundation of China(No.30725048)National Basic Research Program of China(No.2009CB522303)the Foundation of Chinese Academy of Sciences(West Light Program).
文摘Two novel 4,5-secoeudesmane sesquiterpenoids, oxyphyllones A （1） and B （2） were isolated from the fruits of Alpinia oxyphylla. Their structures were established by spectroscopic methods including 1D and 21） NMR spectra. These two compounds are the first example of naturally occurring sesquiterpenoids with a 4,5-secoeudesmane skeleton in the family of Zingiberaceae and oxyphyllone A （1） is the first 4,5-secoeudesmane type of 13-norsesquiterpenoid. Compounds 1 and 2 exhibited no cytotoxicities against three cancer cell lines at 10 μg/mL. ？ 2009 Ning Hua Tan. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
基金supported by the key project supported of Hainan Province(Grant No.ZDZX2013008)Natural Science Foundation of China(Grant No.2014 81403006)
文摘Objective:To study the effect of Alpinia officinarum Hance(A.officinarum) 80% alcohol extract on the primary dysmenorrhea.Methods:A.officinarum 80% alcohol extract were enriched by macroporous adsorption resins.Female mice of primary dysmenorrhea model were established by oxytocin induction; the effects of A.officinarum 80% alcohol extract on primary dysmenorrhea were observed by body twist method; and the homogenate level of prostaglandin F_(2α)(PGF_(2α)),prostaglandin E_2(PGE_2) and Ca^(2+) in the uterus were observed in oxytocin-induced female mice.Results:The writhing frequency of primary dysmenorrhea mice was significantly decreased after treatment of A.officinarum 80% alcohol extract and the level of PGF_(2α),PGE_2 and Ca^(2+) in mice uterus was significantly decreased(P<0.05,P<0.01) in groups of mice treated with middle and high dosage of A.officinarum 80% alcohol extract compared with that of model group.Conclusions:These findings suggest that A.Officinarum 80% alcohol extract can significantly relieve primary dysmenorrhea.
文摘A novel diarylheptanoid bearing flavonol moiety,named officinin A(1),along with two known compounds galangin and kaempferide were isolated from the rhizomes of Alpina officinarum Hance.The structure elucidation was accomplished by HRESI -MS,1D and 2D NMR methods.
