OBJECTIVE:To investigate the effect of ethanol extracts of Muxiang(Radix Aucklandiae)(RA)on gastric ulcers in rats and explore the potential mechanisms.METHODS:A model was established by ethanol(0.75 m L/kg).According...OBJECTIVE:To investigate the effect of ethanol extracts of Muxiang(Radix Aucklandiae)(RA)on gastric ulcers in rats and explore the potential mechanisms.METHODS:A model was established by ethanol(0.75 m L/kg).According to body weight,rats were pretreated with RA extracts(2.5 or 5 g/kg).The rats were administered 95%ethanol orally after 1 h.The effects of ethanol were evaluated by measuring the gastric secretion volume,p H,pepsin activity,and ulcer area.Histological analysis and immunohistochemistry were also conducted.Furthermore,the effect of the ethanol extract of RA on transiting activity of the gastrointestinal tract was observed in mice.RESULTS:Intragastric administration of RA extracts protected the gastric mucosa from ethanol-induced gastric ulcers,while reducing submucosal edema and preventing hemorrhagic damage.Moreover,the extracts increased the production of gastric mucus,upregulated Bcl-2,and downregulated Bax expression.Importantly,pretreated rats exhibited no significant change in the gastric secretion volume,gastric juice acidity,or pepsin.Furthermore,pretreatment prominently(P<0.05)enhanced propulsive movement of the gastrointestinal tract in normal mice and mice with gastrointestinal motility disorders.CONCLUSION:Ethanol extracts of RA ameliorated gastric lesions in the gastric ulcer rat model.The mechanisms of action were related to improvement of gastrointestinal dynamics,maintenance of mucus integrity,and inhibition of apoptosis by downregulating proapoptotic Bax protein and upregulating anti-apoptotic Bcl-2 protein.展开更多
Radix aucklandiae from Yunnan Province in China is a significant medicinal plant. In the present study, the essential oil composition from?Radix aucklandiae roots was investigated by gas chromatography-mass spectromet...Radix aucklandiae from Yunnan Province in China is a significant medicinal plant. In the present study, the essential oil composition from?Radix aucklandiae roots was investigated by gas chromatography-mass spectrometry (GC-MS). A total of 23 compounds representing 57.95% of the essential oil were tentatively identified. The main constituents were eremanthin (12.74%), d-Guaiene (6.26%), ζ-Himachalene (6.16%) and l-Caryophyllene (4.84%). The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the essential oil from R. aucklandiae were evaluated against three Gram-positive bacteria (Staphylococcus aureus, Staphylococcus albus and Bacillus subtilis) three Gram-negative bacteria (Salmonella typhimurium, Escherichia coli and Shigella dysenteriae). Results revealed that the essential oil exhibited significant in vitro antimicrobial property. Among all the tested microorganisms, the essential oil showed the strongest inhibitory effect against S. typhimurium. The data of this study suggests that the essential oil from Radix aucklandiae has great potential for application as a natural antimicrobial agent to preserve food.展开更多
[Objectives] To explore the potential targets and action mechanism of radix aucklandiae (RA) in the treatment of gastric ulcer (GU) by network pharmacology. [Methods] Gene targets were obtained through TCMSP, DisGeNet...[Objectives] To explore the potential targets and action mechanism of radix aucklandiae (RA) in the treatment of gastric ulcer (GU) by network pharmacology. [Methods] Gene targets were obtained through TCMSP, DisGeNet, OMIM, GeneCards databases, which related to GU and the active components of RA. The mutual potential functional targets were selected through Venny to constitute the PPI protein interaction network. The DAVID database was applied for GO and KEGG enrichment analysis of the common targets to construct the "Active component-Target-Pathway" network and analyze the relationship between them. [Results] There are 31 active components, 82 related targets and 16 common targets in the treatment of GU. The active components in Ra may exert anti-ulcer effects through six signaling pathways, including NF-κB, Toll-like receptors, VEGF and HIF-1. In addition, PTGS2, TNF, TLR4, JUN, IL2, SRC, RELA, KDR, NOS2 and PLAU may be the 10 key targets of Ra in the treatment of GU. [Conclusions] Ra controls GU through the synergies of multiple components, targets and pathways. It can provide a theoretical basis for further study on the mechanism of RA in treating GU.展开更多
Three novel sesquiterpenoid heterodimers,designated as auckcostusolides A-C(1-3),were isolated from Aucklandia costus leaves.The structures of compounds 1-3 were elucidated through comprehensive spectroscopic analysis...Three novel sesquiterpenoid heterodimers,designated as auckcostusolides A-C(1-3),were isolated from Aucklandia costus leaves.The structures of compounds 1-3 were elucidated through comprehensive spectroscopic analysis,with their absolute configurations established using a combination of X-ray single-crystal diffraction and electronic circular dichroism(ECD)calculations.Notably,compounds 1 and 2,despite sharing identical planar structures derived from two identical sesquiterpenoids,exhibited oppos-ite configurations at C-11 and C-8'.This configurational difference can be attributed to distinct Diels-Alder cycloaddition processes between the sesquiterpenoid monomers.Additionally,the cytotoxic effects of compounds 1-3 were evaluated against colorectal can-cer HCT116 cells,fibrosarcoma HT1080 cells,and hepatocellular carcinoma HepG2 cells.Compounds 1-3 induced cell death was characterized by endoplasmic reticulum(ER)swelling and cytoplasmic vacuolization,typical morphological changes associated with paraptosis.Mechanistic studies revealed that compounds 1 and 3 triggered paraptosis-like cell death through the accumulation of react-ive oxygen species(ROS),activation of ER stress,and stimulation of the MAPK signaling pathway.展开更多
The medicinal part of Aucklandia lappa(Asteraceae) is its dried root,which is one of the commonly used Chinese medicinal materials.Here we reviewed sesquiterpene lactones isolated from A.lappa over the past ten years ...The medicinal part of Aucklandia lappa(Asteraceae) is its dried root,which is one of the commonly used Chinese medicinal materials.Here we reviewed sesquiterpene lactones isolated from A.lappa over the past ten years in the following aspects of pharmacological activities,pharmacokinetics,toxicology,structure-activity relationship.Pharmacological activities consist of anti-cancer,anti-inflammatory activity,anti-immunity activity,anti-oxidant activity,antimicrobial activity,spasmolytic activity and so on.The extractive,showing similar pharmacokinetics parameters,may exert their various biological activities by the interaction of their α-methylene-γ-butyrolactone moiety with the thiol groups of biomacromolecules through Michael-addition.However,the poor aqueous solubility,non-selective binding as a Michael acceptor at undesired targets limited clinical translation of this class.In order to evaluate the potential effect of the extractive applied in clinical trial,the present review outlines information on pharmacological activities,pharmacokinetics,toxicology,and structure-activity relationship,as well as the future research directions of the extractive for further development and utilization of A.lappa.展开更多
This work achieved the encapsulation of valuable bioactive substances from Aucklandia costus(AC)in nanophytosomes as a new phytoconstituent delivery system.Supercritical fluid extraction(SFE)and solvent-maceration met...This work achieved the encapsulation of valuable bioactive substances from Aucklandia costus(AC)in nanophytosomes as a new phytoconstituent delivery system.Supercritical fluid extraction(SFE)and solvent-maceration methods were used to extract oil and phenolics from AC,respectively.The physicochemical characterization of SFE-oil and phenolic extract(PE)-High-performance liquid chromatography(HPLC)and Gas chromatography–mass spectrometry(GC-MS)were used to identify and quantify all compounds extracted from AC using both extraction methods.loaded nanophytosomes was studied using dynamic light scattering(DLS),encapsulation efficiency(EE),and transmission electron microscopy(TEM).The in vitro digestibility of SFE-oil and PE-loaded nanophytosomes after in vitro digestion was determined.Yoghurt was selected as a food model for fortification with AC-loaded nanophytosomes at different concentrations(5%,10%,and 15%).pH,acidity,water holding capacity(WHC),and viscosity were evaluated in all yoghurt samples during storage,while color analysis and sensory evaluation were evaluated at 0 days.Optimized SFE-oil-and PE-loaded nanophytosomes showed promising results,and the bioavailability suggested that nanoencapsulation provided a controlled release of the phenolic and flavonoid compounds.Moreover,the addition of AC-loaded nanophytosomes into yoghurt resulted in increases in the viscosity(16.53 Pa s^(-1))and decreases in WHC(59.50%).Yoghurts with AC-loaded nanophytosomes were more stable than the control(yoghurt without nanophytosomes).Overall,the current findings indicated that AC-loaded nanophytosomes would be a preferable candidate for incorporation into yoghurt to improve its quality.This research might provide scientific evidence supporting AC-loaded nanophytosomes as possible fortifying elements in manufacturing functional yoghurt and a new vision for designing unique dairy products with functional qualities.展开更多
基金Supported by the Science and Technique Plan of the Education Department of Yunnan Province:the Effect of the Ethanol Extract of Muxiang(Radix Aucklandiae)on Gastric Ulcer in Rats(No.2018JS285)Yunnan Innovation Team of Application Research on Tradtional Chinese Medicine Theory of Disease Prevention at Yunnan University of TCM(No.2017HC011)Yunnan Provincial University Key Laboratory of Aromatic Chinese Herb Research.
文摘OBJECTIVE:To investigate the effect of ethanol extracts of Muxiang(Radix Aucklandiae)(RA)on gastric ulcers in rats and explore the potential mechanisms.METHODS:A model was established by ethanol(0.75 m L/kg).According to body weight,rats were pretreated with RA extracts(2.5 or 5 g/kg).The rats were administered 95%ethanol orally after 1 h.The effects of ethanol were evaluated by measuring the gastric secretion volume,p H,pepsin activity,and ulcer area.Histological analysis and immunohistochemistry were also conducted.Furthermore,the effect of the ethanol extract of RA on transiting activity of the gastrointestinal tract was observed in mice.RESULTS:Intragastric administration of RA extracts protected the gastric mucosa from ethanol-induced gastric ulcers,while reducing submucosal edema and preventing hemorrhagic damage.Moreover,the extracts increased the production of gastric mucus,upregulated Bcl-2,and downregulated Bax expression.Importantly,pretreated rats exhibited no significant change in the gastric secretion volume,gastric juice acidity,or pepsin.Furthermore,pretreatment prominently(P<0.05)enhanced propulsive movement of the gastrointestinal tract in normal mice and mice with gastrointestinal motility disorders.CONCLUSION:Ethanol extracts of RA ameliorated gastric lesions in the gastric ulcer rat model.The mechanisms of action were related to improvement of gastrointestinal dynamics,maintenance of mucus integrity,and inhibition of apoptosis by downregulating proapoptotic Bax protein and upregulating anti-apoptotic Bcl-2 protein.
文摘Radix aucklandiae from Yunnan Province in China is a significant medicinal plant. In the present study, the essential oil composition from?Radix aucklandiae roots was investigated by gas chromatography-mass spectrometry (GC-MS). A total of 23 compounds representing 57.95% of the essential oil were tentatively identified. The main constituents were eremanthin (12.74%), d-Guaiene (6.26%), ζ-Himachalene (6.16%) and l-Caryophyllene (4.84%). The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the essential oil from R. aucklandiae were evaluated against three Gram-positive bacteria (Staphylococcus aureus, Staphylococcus albus and Bacillus subtilis) three Gram-negative bacteria (Salmonella typhimurium, Escherichia coli and Shigella dysenteriae). Results revealed that the essential oil exhibited significant in vitro antimicrobial property. Among all the tested microorganisms, the essential oil showed the strongest inhibitory effect against S. typhimurium. The data of this study suggests that the essential oil from Radix aucklandiae has great potential for application as a natural antimicrobial agent to preserve food.
基金Supported by Natural Science Foundation of Yunnan Province(202101AZ070001-210)Scientific Research Foundation of Education Department of Yunnan Province(2022Y268)Research Project of Pharmacy Innovation Foundation of Anhui Medical University(YXCX202201).
文摘[Objectives] To explore the potential targets and action mechanism of radix aucklandiae (RA) in the treatment of gastric ulcer (GU) by network pharmacology. [Methods] Gene targets were obtained through TCMSP, DisGeNet, OMIM, GeneCards databases, which related to GU and the active components of RA. The mutual potential functional targets were selected through Venny to constitute the PPI protein interaction network. The DAVID database was applied for GO and KEGG enrichment analysis of the common targets to construct the "Active component-Target-Pathway" network and analyze the relationship between them. [Results] There are 31 active components, 82 related targets and 16 common targets in the treatment of GU. The active components in Ra may exert anti-ulcer effects through six signaling pathways, including NF-κB, Toll-like receptors, VEGF and HIF-1. In addition, PTGS2, TNF, TLR4, JUN, IL2, SRC, RELA, KDR, NOS2 and PLAU may be the 10 key targets of Ra in the treatment of GU. [Conclusions] Ra controls GU through the synergies of multiple components, targets and pathways. It can provide a theoretical basis for further study on the mechanism of RA in treating GU.
基金supported by Yunnan RevitalizationTalentSupport Program“Top Team”Project(No.202305AT350001)“Young Talent”Project(No.YNQR-QNRC-2019-091)+5 种基金the National Natural Science Foundation of China(Nos.32170408,32000280,and 32000548)the Ten Thousand Talents Plan of Yunnan Province for Industrial Technology Leading Talents(No.YNWR-CYJS-2019-011)the Project of Yunnan Characteristic Plant Screening and R&D Service CXO Platform(No.2022YKZY001)the CAS Pioneer Hundred Talents Program,the Training of Technological Innovation Talents of Yunnan Province(No.202305AD160009)the Special Research Assistant of Chinese Academy of Sciences(No.E3292211Q1)the Young Academic and Technical Leader Raising Foundation of Yunnan Province(No.202005AC160035).
文摘Three novel sesquiterpenoid heterodimers,designated as auckcostusolides A-C(1-3),were isolated from Aucklandia costus leaves.The structures of compounds 1-3 were elucidated through comprehensive spectroscopic analysis,with their absolute configurations established using a combination of X-ray single-crystal diffraction and electronic circular dichroism(ECD)calculations.Notably,compounds 1 and 2,despite sharing identical planar structures derived from two identical sesquiterpenoids,exhibited oppos-ite configurations at C-11 and C-8'.This configurational difference can be attributed to distinct Diels-Alder cycloaddition processes between the sesquiterpenoid monomers.Additionally,the cytotoxic effects of compounds 1-3 were evaluated against colorectal can-cer HCT116 cells,fibrosarcoma HT1080 cells,and hepatocellular carcinoma HepG2 cells.Compounds 1-3 induced cell death was characterized by endoplasmic reticulum(ER)swelling and cytoplasmic vacuolization,typical morphological changes associated with paraptosis.Mechanistic studies revealed that compounds 1 and 3 triggered paraptosis-like cell death through the accumulation of react-ive oxygen species(ROS),activation of ER stress,and stimulation of the MAPK signaling pathway.
基金supported by Special Financial Grant from the China Postdoctoral Science Foundation (No.2015T81140)National Natural Science Foundation of China Youth Fund Project (No.81503467)。
文摘The medicinal part of Aucklandia lappa(Asteraceae) is its dried root,which is one of the commonly used Chinese medicinal materials.Here we reviewed sesquiterpene lactones isolated from A.lappa over the past ten years in the following aspects of pharmacological activities,pharmacokinetics,toxicology,structure-activity relationship.Pharmacological activities consist of anti-cancer,anti-inflammatory activity,anti-immunity activity,anti-oxidant activity,antimicrobial activity,spasmolytic activity and so on.The extractive,showing similar pharmacokinetics parameters,may exert their various biological activities by the interaction of their α-methylene-γ-butyrolactone moiety with the thiol groups of biomacromolecules through Michael-addition.However,the poor aqueous solubility,non-selective binding as a Michael acceptor at undesired targets limited clinical translation of this class.In order to evaluate the potential effect of the extractive applied in clinical trial,the present review outlines information on pharmacological activities,pharmacokinetics,toxicology,and structure-activity relationship,as well as the future research directions of the extractive for further development and utilization of A.lappa.
文摘This work achieved the encapsulation of valuable bioactive substances from Aucklandia costus(AC)in nanophytosomes as a new phytoconstituent delivery system.Supercritical fluid extraction(SFE)and solvent-maceration methods were used to extract oil and phenolics from AC,respectively.The physicochemical characterization of SFE-oil and phenolic extract(PE)-High-performance liquid chromatography(HPLC)and Gas chromatography–mass spectrometry(GC-MS)were used to identify and quantify all compounds extracted from AC using both extraction methods.loaded nanophytosomes was studied using dynamic light scattering(DLS),encapsulation efficiency(EE),and transmission electron microscopy(TEM).The in vitro digestibility of SFE-oil and PE-loaded nanophytosomes after in vitro digestion was determined.Yoghurt was selected as a food model for fortification with AC-loaded nanophytosomes at different concentrations(5%,10%,and 15%).pH,acidity,water holding capacity(WHC),and viscosity were evaluated in all yoghurt samples during storage,while color analysis and sensory evaluation were evaluated at 0 days.Optimized SFE-oil-and PE-loaded nanophytosomes showed promising results,and the bioavailability suggested that nanoencapsulation provided a controlled release of the phenolic and flavonoid compounds.Moreover,the addition of AC-loaded nanophytosomes into yoghurt resulted in increases in the viscosity(16.53 Pa s^(-1))and decreases in WHC(59.50%).Yoghurts with AC-loaded nanophytosomes were more stable than the control(yoghurt without nanophytosomes).Overall,the current findings indicated that AC-loaded nanophytosomes would be a preferable candidate for incorporation into yoghurt to improve its quality.This research might provide scientific evidence supporting AC-loaded nanophytosomes as possible fortifying elements in manufacturing functional yoghurt and a new vision for designing unique dairy products with functional qualities.
