Background:L-dopa(Levodopa)is well known for managing PD(Parkinson’s disease);however,its prolonged use caused dyskinesia(LID).Due to the varied presentation of LID,effective treatment options are scarce.Flavonoids r...Background:L-dopa(Levodopa)is well known for managing PD(Parkinson’s disease);however,its prolonged use caused dyskinesia(LID).Due to the varied presentation of LID,effective treatment options are scarce.Flavonoids reported their neuroprotective activity by ameliorating acetylcholinesterase,monoamine oxidase,and neuroinflammation.Kaempferol is anotherflavonoid bearing these potentials.Aim:To evaluate neuroprotective activity of kaempferol in dyskinetic rats.Methods:PD was developed in Sprague-Dawley rats by injecting combination of L-ascorbic acid(10µL)+6-OHDA(12µg)in medial forebrain bundle to induce neuronal damage in substantial nigra(SNr).LID was induced by administrating combination of L-dopa(20 mg/kg)+benserazide HCl(5 mg/kg)for 42 days.Rats were concomitantly treated with amantadine(40 mg/kg)or kaempferol(25,50,and 100 mg/kg,p.o.).Results:Kaempferol(50 and 100 mg/kg)markedly(p<0.05)inhibited LID-induced abnormal involuntary movements(AIMs)and alternation in motor function.Kaempferol administration considerably(p<0.05)inhibited reduced mitochondrial complex activities,serotonin and dopamine levels,Bcl-2,and Tyrosine hydroxylase protein expressions in SNr.Additionally,kaempferol considerably(p<0.05)attenuated increased cFOS,FosB,Parkin,and Pdyn mRNAs expressions,Bax,cleaved caspase-3,caspase-3,and pJNK proteins levels;DOPAC and 5-HIAA levels in SNr.A positive correlation was reported between cFOS,FosB,Parkin,Pdyn,apoptosis,and TH with AIMs.Conclusion:Kaempferol effectively attenuated L-dopa-induced AIMs and dyskinesia via amelioration of alterations in cFOS,FosB,Parkin,Pdyn,Tyrosine hydroxylase,and apoptosis in the brain SNr.展开更多
Background:Ginkgo flavone aglycones(GA),a Ginkgo(Ginkgo biloba)extract,has been proven to have good biological activity in atherosclerosis(AS)treatment.Moreover,its active compounds and the corresponding mechanism for...Background:Ginkgo flavone aglycones(GA),a Ginkgo(Ginkgo biloba)extract,has been proven to have good biological activity in atherosclerosis(AS)treatment.Moreover,its active compounds and the corresponding mechanism for the treatment of AS remain unclear.Methods:To evaluate and identify the potential pharmacological mechanisms of GA in AS treatment,the program Cytoscape was used to generate network mappings of the GA-AS-potential target gene.GO and KEGG enrichment analyses were performed to further investigate the potential mechanism of AS and the pharmacological properties of GA.A molecular docking approach was utilized to determine the GA components that interact with Akt.In vitro experiments were carried out to identify the anti-atherosclerotic effects of GA by targeting Akt.Results:Network pharmacological research determined that the active components of GA(quercetin,kaempferol,and isorhamnetin)correlated with AS target genes such as AKT1,EGFR,SRC,ESR1,PTGS2,MMP9,KDR,GSK3B,APP,and MMP2,respectively.GO enrichment and KEGG analysis showed that PI3K-Akt signaling may play an important role in GA treatment.Molecular docking experiments indicated that quercetin,kaempferol,and isorhamnetin integrate into the binding pockets of the most potentially beneficial GA-AS target protein(Akt).Consequently,cell experiments were conducted to support the anti-atherosclerotic activity of GA on AS by inhibiting the phosphorylation of AKT1 and its downstream signaling molecules,which regulated the proliferation of HASMCs.Conclusion:Our results detailed GA's active ingredients,potential targets,and molecular basis against AS.GA may exert anti-atherosclerotic effects by suppressing Akt phosphorylation and inhibiting the proliferation of HASMCs.It also proposed a viable approach to determining the scientific foundation and therapeutic mechanism of Chinese herbal medicine extracts in disease therapy.展开更多
Kaempferol(KA),as one of the flavonoids,has extensive pharmacological properties.However,the poor solubility of KA severely limits its clinical application.In our study,the kaempferol phospholipid complex(KA-PC)has be...Kaempferol(KA),as one of the flavonoids,has extensive pharmacological properties.However,the poor solubility of KA severely limits its clinical application.In our study,the kaempferol phospholipid complex(KA-PC)has been prepared by solvent evaporation for the enhancement of the bioavailability of KA.KA-PC was verified by scanning electron microscope characterization methods.Drug loading,solubility and long-term stability were measured.The characterization results showed that KA-PC was formed through the intermolecular interaction between KA and phospholipids.The solubility of KA-PC in water was 189 times higher than that of KA,and the solubility in n-octanol was also significantly improved.Besides,pharmacodynamic studies showed that KA-PC can significantly reduce the level of serum uric acid in mice without causing renal injury.This study expanded the clinical application of KA by preparing KA-PC.展开更多
Host-directed therapy(HDT)is an emerging novel approach for treating multidrug-resistant Staphylococcus aureus(S.aureus)infection.Functioning as the indispensable specific cellular receptor for a-toxin(Hla),a-disinteg...Host-directed therapy(HDT)is an emerging novel approach for treating multidrug-resistant Staphylococcus aureus(S.aureus)infection.Functioning as the indispensable specific cellular receptor for a-toxin(Hla),a-disintegrin and metalloproteinase 10(ADAM10)is exploited to accelerate S.aureus infection through diverse mechanisms.The extraordinary contribution of ADAM10 to S.aureus pathogenesis renders it an attractive HDT target for combating S.aureus infection.Our study is the first to demonstrate the indispensable role of ADAM10 in S.aureus-induced necroptosis,and it enhances our knowledge of the role of ADAM10 in S.aureus infection.Using a fluorogenic substrate assay,we further identified kaempferol as a potent ADAM10 inhibitor that effectively protected mice from S.aureus infection by suppressing Hla-mediated barrier disruption and necroptosis.Collectively,our work presents a novel hostdirected therapeutic strategy for using the promising candidate kaempferol to treat S.aureus infection and other diseases relevant to the disordered upregulation of ADAM10.展开更多
Insulin resistance is a hallmark of type-2 diabetes(T2D)pathogenesis.Because skeletal muscle(SkM)is the major tissue for insulin-mediated glucose disposal,insulin resistance in SkM is considered a major risk factor fo...Insulin resistance is a hallmark of type-2 diabetes(T2D)pathogenesis.Because skeletal muscle(SkM)is the major tissue for insulin-mediated glucose disposal,insulin resistance in SkM is considered a major risk factor for developing T2D.Thus,the identifi cation of compounds that enhance the ability of SkM to take up glucose is a promising strategy for preventing T2D.Our previous work showed that kaempferol,a fl avonol present in many foods,improves insulin sensitivity in obese mice,however,the mechanism underlying this beneficial action remains unclear.Here,we show that kaempferol directly stimulates glucose uptake and prevents lipotoxicity-impaired glucose uptake in primary human SkM.Kaempferol stimulates Akt phosphorylation in a time-dependent manner in human SkM cells.The effect of kaempferol on glucose uptake was blunted by inhibition of glucose transporter 4,phosphoinositide 3-kinase(PI3K),or AMPK.In addition,kaempferol induced AMPK phosphorylation,and inhibition of AMPK prevented kaempferol-stimulated Akt phosphorylation.In vivo,kaempferol administration induced rapid glucose disposal accompanied with increased Akt and AMPK phosphorylation in SkM tissue of the mice.Taken together,these fi ndings suggest that kaempferol stimulates glucose uptake in SkM via an AMPK/Akt dependent mechanism,and it may be a viable therapeutic agent for insulin resistance.展开更多
Kaempferol,a natural plant-origin flavonoid,exhibits therapeutic anti-inflammatory,antioxidant,anticancer,antidiabetic,and neuroprotective properties.Kaempferol acts within several distinct mechanisms like apoptotic i...Kaempferol,a natural plant-origin flavonoid,exhibits therapeutic anti-inflammatory,antioxidant,anticancer,antidiabetic,and neuroprotective properties.Kaempferol acts within several distinct mechanisms like apoptotic induction in cancer cells,enzymatic inhibition,signalling pathway inhibition,and downregulation in cell viability during the G2/M phase of cell division.This review summarizes the therapeutic effects of kaempferol against several health ailments.The recent progress on kaempferol obtained from fruits and vegetables as an antioxidant,anti-inflammatory,anticancer,antidiabetic,and neuroprotective agent and its mechanisms of action are also discussed.In addition,kaempferol has been reported to be present in wastes and byproducts from post-fruit and vegetable processing.Thus,a paradigm shift towards valorizing fruits and vegetable industrial wastes/byproducts to obtain bioactive kaempferol can support the circular economy pillar for generating wealth from waste and for finding a sustainable alternative source.展开更多
Dysosma versipellis is the rhizome of Bajiaolian in Berberaceae.It is a unique medicinal plant in China and it was the first to be recorded in Shennong’s Classic of Materia Medica(unknown author,25–220 C.E.).It has ...Dysosma versipellis is the rhizome of Bajiaolian in Berberaceae.It is a unique medicinal plant in China and it was the first to be recorded in Shennong’s Classic of Materia Medica(unknown author,25–220 C.E.).It has complex chemical components as well as complex,pharmacological and toxicological effects are extensive.Based on the recent research progress,the chemical constituents,pharmacological activities and toxicological effects of Dysosma versipellis were summarized.Combined with the core concept of quality markers of traditional Chinese medicine,the prediction and analysis were carried out from the aspects of phytogenetics and the source pathway of specific chemical constituents,traditional medicinal properties,traditional efficacy,chemical composition measurability,blood components,and pharmacokinetics,in order to provide reference for further study of Dysosma versipellis.展开更多
Alzheimer's disease(AD) is associated with oxidative stress, and ultimately results in cognitive deficit. Despite existing literature on the pathophysiology of AD, there is currently no cure for AD. The present stu...Alzheimer's disease(AD) is associated with oxidative stress, and ultimately results in cognitive deficit. Despite existing literature on the pathophysiology of AD, there is currently no cure for AD. The present study investigated the effects of kaempferol(Kmp) isolated from the extract of Mespilus germanica L.(medlar) leaves on cognitive impairment, hippocampal antioxidants, apoptosis, lipid peroxidation and neuro-inflammation markers in ovariectomized(OVX) rat models of sporadic AD. Kaempferol, as the main flavonoid of medlar extract has been previously known for anti-oxidative, anti-inflammatory and anti-neurotoxic effects. Thirty-two female Wistar rats were ovariectomized, and randomly divided into four groups: sham, OVX + saline, OVX + streptozotocin(STZ) + saline, OVX + STZ + Kmp. Animals received intracerebroventricular injection of STZ(3 mg/kg, twice with one day interval) to establish models of sporadic AD. Intraperitoneal injection of Kmp(10 mg/kg) for 21 days was performed in the OVX + STZ + Kmp group. Spatial learning and memory of rats were evaluated using a Morris water maze. Finally, brain homogenates were used for biochemical analysis by enzyme-linked immunosorbent assay. The results showed a significant improvement in spatial learning and memory as evidenced by shortened escape latency and searching distance in Morris water maze in the OVX + STZ + Kmp group compared with the OVX + STZ group. Kmp also exhibited significant elevations in brain levels of antioxidant enzymes of superoxide dismutase and glutathione, while reduction in tumor necrosis factor-α and malondialdehyde. Our results demonstrate that Kmp is capable of alleviating STZ-induced memory impairment in OVX rats, probably by elevating endogenous hippocampal antioxidants of superoxide dismutase and glutathione, and reducing neuroinflammation. This study suggests that Kmp may be a potential neuroprotective agent against cognitive deficit in AD.展开更多
Severe acute respiratory syndrome coronavirus type 2(SARS-CoV-2)is a novel coronavirus identified at the end of 2019.It is recognized as the causative agent of coronavirus disease 2019(COVID-19).Flavonoids have been s...Severe acute respiratory syndrome coronavirus type 2(SARS-CoV-2)is a novel coronavirus identified at the end of 2019.It is recognized as the causative agent of coronavirus disease 2019(COVID-19).Flavonoids have been shown to exhibit therapeutical effect on complications related to COVID-19.The present study reviews possible therapeutic benefits of flavonoids on SARS-CoV-2.The Web of Science,PubMed,Scopus,and Google Scholar were searched using keywords:“COVID-19”,“SARS-CoV-2”,“Kaempferol”and“Quercetin”in the Title/Abstract.Relevant published articles in the English language until August 2020 were considered.Kaempferol and quercetin showed antiviral properties such as inhibition of protein kinase B and phosphorylation of protein kinase and blocking effects on a selective channel(3a channel)expressed in SARS-CoV infected cells.They also reduced the level of reactive oxygen species,expression of inducible nitric oxide synthase,pro-inflammatory mediators including TNF-α,IL-1α,IL-1β,IL-6,IL-10,and IL-12 p70,and chemokines.Kaempferol and quercetin might exert beneficial effects in the control or treatment of COVID-19 because of their antiviral,antioxidant,anti-inflammatory,and immunomodulatory effects.展开更多
Objective:To identify alpha-glucosidase inhibitors from Ficus benghalensis and analyze gene set enrichment of regulated protein molecules.Methods:The phytoconstituents of Ficu.s benghalen.sis were queried for inhibito...Objective:To identify alpha-glucosidase inhibitors from Ficus benghalensis and analyze gene set enrichment of regulated protein molecules.Methods:The phytoconstituents of Ficu.s benghalen.sis were queried for inhibitors of alphaglucosidase,also identified as aldose reductase inhibitors.Druglikeness score,absorption,distribution,metabolism,excretion and toxicity profile,biological spectrum,and gene expression were predicated for each compound.Docking study was performed to predict the binding affinity with alpha-glucosidase and aldose reductase and compared with clinically proven molecules.Kyoto Encyclopedia of Genes and Genomes pathway analysis was performed for the regulated genes to identify the modulated pathways.Results:Apigenin,3,4’,5,7-tetrahydroxy-3’-methoxyflavone,and kaempferol were identified as inhibitors of alpha-glucosidase and aldose reductase.Kaempferol was predicted to possess the highest binding affinity with both targets.The p53 signaling pathway was predicted to modulate the majority of protein molecules in diabetes mellitus.All the alpha-glucosidase inhibitors were also predicted as membrane integrity agonist and anti-mutagenic compounds.Conclusions:The current study indicates alpha-glucosidase inhibitors from Ficus benghale,nsis can act as aldose reductase inhibitors after absorption from the intestinal tract.Furthermore,these phytoconstituents are involved in the regulation of numerous protein molecules and pathways.Hence,the anti-diabetic efficacies of these compounds are due to their action on multiple protein molecules and synergistic effects which should be confirmed by future investigations.展开更多
OBJECTIVE To investigate the effects of kaempferol(KAE)on chronic cerebral ischemia in rats.METHODS Chronic cerebral ischemia was induced in rats by permanent occlusion of bilateral common carotid arteries(2VO).Then,t...OBJECTIVE To investigate the effects of kaempferol(KAE)on chronic cerebral ischemia in rats.METHODS Chronic cerebral ischemia was induced in rats by permanent occlusion of bilateral common carotid arteries(2VO).Then,the rats with chronic cerebral ischemia were randomly divied into three groups:model group,KAE 10 and 30 mg·kg-1group.Another group rats without occlusion of common carotid arteries were used as the sham-operation group.Memory behavior was investigated by Morris water maze test.Prehensile ability was investigated by prehensile traction test.The structure of hippocampus and cortex neurons was observed with Nissel staining.In addition,the SOD activity and MDA content in brain tissue were determined.The DJ-1protein level was determined by Western blotting.RESULTS KAE 10 and 30 mg·kg-1could significantly improve cognitive impairment and prehensile traction ability(P<0.01)induced by chronic cerebral ischemia in rats.The results of the pathological analysis also suggested that KAE could ameliorate the pathological damage induced by chronic cerebral ischemia.In addition,KAE 30 mg·kg-1significantly increased the activity of SOD(P<0.05),but had no effect on the content of MDA in rat brain tissue.Western-blotting confirmed that KAE 10 and30 mg·kg-1could increase the expression of anti-oxidation proteins DJ-1 in hippocampus(P<0.01).CONCLUSION KAE may attenuate the chronic cerebral ischemic injury in rats.展开更多
[Objectives] To investigate the anti-tumor activity of Sedum bulbiferum Makino in vitro,and establish a HPLC method for determination of quercetin and kaempferol in S. bulbiferum. [Methods] The inhibitory activities o...[Objectives] To investigate the anti-tumor activity of Sedum bulbiferum Makino in vitro,and establish a HPLC method for determination of quercetin and kaempferol in S. bulbiferum. [Methods] The inhibitory activities of different extracts and total flavonoids of S. bulbiferum on proliferation of three kinds of cancer cells( Hep G2,EC109,SW480) were tested by MTT assay. HPLC method for determination of quercetin and kaempferol in S. bulbiferum was established. [Results]The growth and proliferation of the three kinds of cancer cells were all significantly inhibited by ethyl acetate fraction and total flavonoids isolated from S. bulbiferum. With each extraction concentration increasing,stronger anti-tumor activity was found. The linear ranges of quercetin and kaempferol were 0. 03-0. 36 μg( R = 0. 999 9) and0. 08-0. 96 μg( R = 0. 999 9),and the average recoveries were 98. 90%( RSD = 1. 15%) and 98. 27%( RSD = 1. 70%),respectively.[Conclusions]S. bulbiferum has significant anti-tumor activity in vitro. The HPLC method established was accurate,reproducible,and could be used for quality control of this crude drug.展开更多
Tyrosinase inhibitory activity of the extractives from A. cathartica was examined and their new bioactivity and potent active compounds were identified. Five compounds, glabridin, new lignan, kaempferol, naringenin, a...Tyrosinase inhibitory activity of the extractives from A. cathartica was examined and their new bioactivity and potent active compounds were identified. Five compounds, glabridin, new lignan, kaempferol, naringenin, and allamandicin, were isolated by a series of chromatography, and identified by NMR and LC-MS. Among them, glabridin had the high-est tyrosinase inhibitory activity (IC50:2.93 μM) which is 15 times stronger than that of kojic acid used as positive con-trol (IC50:43.7 μM). Moreover the lignan was indentified as 1-[3-(4-allyl-2,6-dimethoxyphenoxy)-4-methoxyphenyl] propane-1,2,diol which was a novel lignan.展开更多
Objective: To characterize the types, contents, and peroxynitrite-scavenging activities of flavonoids in the leaf of Carica papaya(C. papaya).Methods: Chromatographic and spectroscopic techniques along with high perfo...Objective: To characterize the types, contents, and peroxynitrite-scavenging activities of flavonoids in the leaf of Carica papaya(C. papaya).Methods: Chromatographic and spectroscopic techniques along with high performance liquid chromatography quantitative analysis and peroxynitrite-scavenging assay were performed to isolate and quantify flavonoid compounds in the flavonoid-rich fraction(Bu OH fraction) derived from Me OH extract of C. papaya leaves and evaluate their peroxynitrite-scavenging activities.Results: Seven flavonoids were isolated from the leaves of C. papaya, including quercetin 3-(2~G-rhamnosylrutinoside), kaempferol 3-(2~G-rhamnosylrutinoside), quercetin 3-rutinoside, myricetin 3-rhamnoside, kaempferol 3-rutinoside, quercetin, and kaempferol. All of the substances exhibited potent activities on peroxynitrite scavenging(IC50 4.15 mmol/L), which were stronger than the positive control, L-penicillamine(6.90 mmol/L). The content of kaempferol 3-(2~G-rhamnosylrutinoside) was significantly higher than other identified compounds(123.18 mg/g Bu OH fraction and 7.23 mg/g Me OH extract).Conclusions: The results of the present study demonstrate the potent antioxidant flavonoids of C. papaya leaf, with kaempferol 3-(2~G-rhamnosylrutinoside) as the major one.展开更多
Pseudorabies virus(PRV),in the family Herpesviridae,is a pathogen of Aujeszky’s disease,which causes great economic losses to the pig industry.Recent outbreaks of Pseudorabies imply that new control measures are urge...Pseudorabies virus(PRV),in the family Herpesviridae,is a pathogen of Aujeszky’s disease,which causes great economic losses to the pig industry.Recent outbreaks of Pseudorabies imply that new control measures are urgently needed.The present study shows that kaempferol is a candidate drug for controlling PRV infection,as it possesses the ability to inhibit PRV replication in a dose-dependent manner in vitro.Kaempferol at a concentration of 52.40μmol L^(-1) could decrease PRV-induced cell death by 90%.With an 50%inhibitory concentration(IC50)value of 25.57μmol L^(-1),kaempferol was more effective than acyclovir(positive control)which has an IC50 value of 54.97μmol L^(-1).A mode of action study indicated that kaempferol inhibited viral penetration and replication stages,decreasing viral loads by 4-and 30-fold,respectively.Addition of kaempferol within 16 h post infection(hpi)could significantly inhibit virus replication,and viral genome copies were decreased by almost 15-fold when kaempferol was added at 2 hpi.Kaempferol regulated the NF-κB and MAPKs signaling pathways involved in PRV infection and changed the levels of the target genes of the MAPKs(ATF-2 and c-Jun)and NF-κB(IL-1α,IL-1βand IL-2)signaling pathways.The findings of the current study suggest that kaempferol could be an alternative measure to control PRV infection.展开更多
Novel uniform-sized magnetic molecularly imprinted polymers (MMIPs) were synthe- sized for selective recognition of active antitumor ingredients of kaempferol (KMF) and protoapi- genone (PA) in Macrothelypteris ...Novel uniform-sized magnetic molecularly imprinted polymers (MMIPs) were synthe- sized for selective recognition of active antitumor ingredients of kaempferol (KMF) and protoapi- genone (PA) in Macrothelypteris torresiana (M. torresiana) by surface molecular imprinting tech- nique in this study. Super paramagnetic core-sheU nanoparticles (γ-MPS-SiO2@Fe3O4) were used as seeds, KMF as template molecule, acrylamide (AM) as functional monomer, and N, N'-methylene bisacrylamide (BisAM) as cross-linker. The prepared MMIPs were characterized by X-ray diffraction (XRD), Fourier transform infrared spectrum fiT/R), transmission electron microscopy (TEM) and thermo-gravimetric analysis (TGA), respectively. The recognition capacity of MMIPs was 2.436 times of non-imprinted polymers. The adsorption results based on kinetics and isotherm analysis were in accordance with the pseudo-second-order model (R2=0.9980) and the Langmuir adsorption model (R2=0.9944). The value of E (6.742 kJ/mol) calculated from the Dubinin-Radushkevich isotherm model suggested that the physical adsorption via hydrogen-bonding might be predominant. The Scatchard plot showed a single line (R2=0.9172) and demonstrated the homogeneous recognition sites on MMIPs for KMF. The magnetic solid phase extraction (MSPE) based on MMIPs as sorbent was established for fast and selective enrichment of KMF and its structural analogue PA from the crude extract of M. torresiana and then KMF and PA were detected by HPLC-UV. The established method showed good performance and satisfactory results for real sample analysis. It also showed the feasi- bility of MMIPs for selective recognition of active structural analogues from complex herbal extracts.展开更多
The contents of rutin,quercetin and kaempferol in powders of tartary buckwheat of different parts were determined by high-performance liquid chromatography( HPLC). The results showed that the contents of the three kin...The contents of rutin,quercetin and kaempferol in powders of tartary buckwheat of different parts were determined by high-performance liquid chromatography( HPLC). The results showed that the contents of the three kinds of flavonoids differed greatly in the powders of tartary buckwheat of different parts. The contents of rutin and quercetin in the powder of tartary buckwheat sprouts were significantly higher than those in the powders of tartary buckwheat leaves and seeds. The content of kaempferol was highest in the powder of tartary buckwheat seeds. It indicates that high-performance liquid chromatography can be used for quality control of tartary buckwheat powder for its time saving,cost saving and accurate and reliable results. The content of rutin in the powder of tartary buckwheat sprouts was highest,suggesting that it is more suitable for the development of various foods based on tartary buckwheat powder.展开更多
Aim To study the chemical composition of Opuntia dillenii Haw. Methods Manykinds of chromatogra-phy methods were used in the isolation procedure, while the structures ofisolated compounds were determined on the aids o...Aim To study the chemical composition of Opuntia dillenii Haw. Methods Manykinds of chromatogra-phy methods were used in the isolation procedure, while the structures ofisolated compounds were determined on the aids of NMR and MS spectral analysis. Result Three newcompounds, together with 14 known compounds, were isolated form the 80% ethanolic extract of itsstems. Conclusion The three new compounds, opuntioside Ⅰ (2), 4-ethoxyl-6-hydroxymethyl-α-pyrone(3) and kaempferol 7-O-β-D-glucopyranosyl (1→4)-β-D-glucopyranoside (4), were characterized.展开更多
A new kaempferol glycoside,named kaempferol 3-O-[6″-O-β-D-glucopyranosyl-6′′′-O-α-L-rhamnopy ranosyl-2′′′′-O-α-L-rhamnopyranosyl]-β-D-glucopyranoside,was isolated from Hydrangea macrophylla(Thunb.) Seringe...A new kaempferol glycoside,named kaempferol 3-O-[6″-O-β-D-glucopyranosyl-6′′′-O-α-L-rhamnopy ranosyl-2′′′′-O-α-L-rhamnopyranosyl]-β-D-glucopyranoside,was isolated from Hydrangea macrophylla(Thunb.) Seringe.Its structure was establishedby spectroscopic techniques including MS,IR,UV,and 2D NMR.展开更多
Background:The breast cancer has been the most common form of cancer among women.The triple negative subtype represents 20%of all breast cancer cases in the world and is standing out by affecting young women and being...Background:The breast cancer has been the most common form of cancer among women.The triple negative subtype represents 20%of all breast cancer cases in the world and is standing out by affecting young women and being aggressive.The main cause of death of patients with cancer is due to metastasis,which can reach the liver and lungs.Objective:The activities of ID7 fraction of the stems of Bauhinia variegata L.on breast cancer,lung metastasis and liver inflammatory process were evaluated.Method:ID7 was characterized by mass-spectrometry.The viability of murine mammary cells(4T1)treated with ID7 was assessed by MTT,trypan blue and fluorescence assay and viability of BT-20,MDA-MB-231 and MCF-7 human breast cancer tumor lines by MTS.The cell migration,invasion using matrigel and adhesion were performed.The expression of cell death proteins was quanitified by western blot and the gelatinases by zimogram.The ID7 activity of the tumor(4T1)and metastatic progession in vivo was evaluated.Results:ID7 reduced the 4T1 and MDA-MB-231viability and increased the late apoptosis,inhibited the 4T1 migration and invasion,increased the 4T1 adhesion and decreased the secreted active gelatinases.ID7 also increased the expression of PARP,caspase-7 and caspase-8,RIP and TNF-R1.In vivo,the ID7 decreased the volume and weight of the tumors and decreased lung metastasis and inflammation in the liver.The characterization showed mainly the presence of oleic acid,myricetin,quercetin and kaempferol in ID7.Conclusion:Thus,it was found that ID7 fraction exhibits selective antitumor and on the mechanisms of breast cancer metastasis activity,preventing lung metastasis and inflammation in the liver.It is suggested that fatty acids and flavonoids are correlated with such activities.展开更多
文摘Background:L-dopa(Levodopa)is well known for managing PD(Parkinson’s disease);however,its prolonged use caused dyskinesia(LID).Due to the varied presentation of LID,effective treatment options are scarce.Flavonoids reported their neuroprotective activity by ameliorating acetylcholinesterase,monoamine oxidase,and neuroinflammation.Kaempferol is anotherflavonoid bearing these potentials.Aim:To evaluate neuroprotective activity of kaempferol in dyskinetic rats.Methods:PD was developed in Sprague-Dawley rats by injecting combination of L-ascorbic acid(10µL)+6-OHDA(12µg)in medial forebrain bundle to induce neuronal damage in substantial nigra(SNr).LID was induced by administrating combination of L-dopa(20 mg/kg)+benserazide HCl(5 mg/kg)for 42 days.Rats were concomitantly treated with amantadine(40 mg/kg)or kaempferol(25,50,and 100 mg/kg,p.o.).Results:Kaempferol(50 and 100 mg/kg)markedly(p<0.05)inhibited LID-induced abnormal involuntary movements(AIMs)and alternation in motor function.Kaempferol administration considerably(p<0.05)inhibited reduced mitochondrial complex activities,serotonin and dopamine levels,Bcl-2,and Tyrosine hydroxylase protein expressions in SNr.Additionally,kaempferol considerably(p<0.05)attenuated increased cFOS,FosB,Parkin,and Pdyn mRNAs expressions,Bax,cleaved caspase-3,caspase-3,and pJNK proteins levels;DOPAC and 5-HIAA levels in SNr.A positive correlation was reported between cFOS,FosB,Parkin,Pdyn,apoptosis,and TH with AIMs.Conclusion:Kaempferol effectively attenuated L-dopa-induced AIMs and dyskinesia via amelioration of alterations in cFOS,FosB,Parkin,Pdyn,Tyrosine hydroxylase,and apoptosis in the brain SNr.
基金supported by the Science and Technology Foundation of Basic Research Program of Guizhou Province([2023]General 371,[2020]1Y381)the Administration of Traditional Chinese Medicine of Guizhou Province(QZYY-2018-130)+3 种基金the project of Key Laboratory of Basic Pharmacology of Ministry of Education,Zunyi Medicial University(No.qianjiaoheKYzi[2022]395)the Cultivation Plan of the NSFC(National Natural Science Foundation of China)of the affiliated hospital of Guizhou Medical University(GYFYNSFC-2021-55,GYFYNSFC-2021-56)the Cultivation Plan of the NSFC(National Natural Science Foundation of China)of Guizhou Medical University(21NSFCP13)the Science and Technology Foundation of Health Commission of Guizhou Province(gzwkj 2022-221).
文摘Background:Ginkgo flavone aglycones(GA),a Ginkgo(Ginkgo biloba)extract,has been proven to have good biological activity in atherosclerosis(AS)treatment.Moreover,its active compounds and the corresponding mechanism for the treatment of AS remain unclear.Methods:To evaluate and identify the potential pharmacological mechanisms of GA in AS treatment,the program Cytoscape was used to generate network mappings of the GA-AS-potential target gene.GO and KEGG enrichment analyses were performed to further investigate the potential mechanism of AS and the pharmacological properties of GA.A molecular docking approach was utilized to determine the GA components that interact with Akt.In vitro experiments were carried out to identify the anti-atherosclerotic effects of GA by targeting Akt.Results:Network pharmacological research determined that the active components of GA(quercetin,kaempferol,and isorhamnetin)correlated with AS target genes such as AKT1,EGFR,SRC,ESR1,PTGS2,MMP9,KDR,GSK3B,APP,and MMP2,respectively.GO enrichment and KEGG analysis showed that PI3K-Akt signaling may play an important role in GA treatment.Molecular docking experiments indicated that quercetin,kaempferol,and isorhamnetin integrate into the binding pockets of the most potentially beneficial GA-AS target protein(Akt).Consequently,cell experiments were conducted to support the anti-atherosclerotic activity of GA on AS by inhibiting the phosphorylation of AKT1 and its downstream signaling molecules,which regulated the proliferation of HASMCs.Conclusion:Our results detailed GA's active ingredients,potential targets,and molecular basis against AS.GA may exert anti-atherosclerotic effects by suppressing Akt phosphorylation and inhibiting the proliferation of HASMCs.It also proposed a viable approach to determining the scientific foundation and therapeutic mechanism of Chinese herbal medicine extracts in disease therapy.
基金funded by Young and Middle Aged Teachers’Career Development Support Project of Shenyang Pharmaceutical University(ZQN2019005).
文摘Kaempferol(KA),as one of the flavonoids,has extensive pharmacological properties.However,the poor solubility of KA severely limits its clinical application.In our study,the kaempferol phospholipid complex(KA-PC)has been prepared by solvent evaporation for the enhancement of the bioavailability of KA.KA-PC was verified by scanning electron microscope characterization methods.Drug loading,solubility and long-term stability were measured.The characterization results showed that KA-PC was formed through the intermolecular interaction between KA and phospholipids.The solubility of KA-PC in water was 189 times higher than that of KA,and the solubility in n-octanol was also significantly improved.Besides,pharmacodynamic studies showed that KA-PC can significantly reduce the level of serum uric acid in mice without causing renal injury.This study expanded the clinical application of KA by preparing KA-PC.
基金supported by the National Natural Science Foundation of China(U22A20523,32172912,and 32102722)the Interdisciplinary Integration and Innovation Project of Jilin University(JLUXKJC2021QZ04)。
文摘Host-directed therapy(HDT)is an emerging novel approach for treating multidrug-resistant Staphylococcus aureus(S.aureus)infection.Functioning as the indispensable specific cellular receptor for a-toxin(Hla),a-disintegrin and metalloproteinase 10(ADAM10)is exploited to accelerate S.aureus infection through diverse mechanisms.The extraordinary contribution of ADAM10 to S.aureus pathogenesis renders it an attractive HDT target for combating S.aureus infection.Our study is the first to demonstrate the indispensable role of ADAM10 in S.aureus-induced necroptosis,and it enhances our knowledge of the role of ADAM10 in S.aureus infection.Using a fluorogenic substrate assay,we further identified kaempferol as a potent ADAM10 inhibitor that effectively protected mice from S.aureus infection by suppressing Hla-mediated barrier disruption and necroptosis.Collectively,our work presents a novel hostdirected therapeutic strategy for using the promising candidate kaempferol to treat S.aureus infection and other diseases relevant to the disordered upregulation of ADAM10.
基金partially supported by grants from Diabetes Action Research and Education Foundation。
文摘Insulin resistance is a hallmark of type-2 diabetes(T2D)pathogenesis.Because skeletal muscle(SkM)is the major tissue for insulin-mediated glucose disposal,insulin resistance in SkM is considered a major risk factor for developing T2D.Thus,the identifi cation of compounds that enhance the ability of SkM to take up glucose is a promising strategy for preventing T2D.Our previous work showed that kaempferol,a fl avonol present in many foods,improves insulin sensitivity in obese mice,however,the mechanism underlying this beneficial action remains unclear.Here,we show that kaempferol directly stimulates glucose uptake and prevents lipotoxicity-impaired glucose uptake in primary human SkM.Kaempferol stimulates Akt phosphorylation in a time-dependent manner in human SkM cells.The effect of kaempferol on glucose uptake was blunted by inhibition of glucose transporter 4,phosphoinositide 3-kinase(PI3K),or AMPK.In addition,kaempferol induced AMPK phosphorylation,and inhibition of AMPK prevented kaempferol-stimulated Akt phosphorylation.In vivo,kaempferol administration induced rapid glucose disposal accompanied with increased Akt and AMPK phosphorylation in SkM tissue of the mice.Taken together,these fi ndings suggest that kaempferol stimulates glucose uptake in SkM via an AMPK/Akt dependent mechanism,and it may be a viable therapeutic agent for insulin resistance.
文摘Kaempferol,a natural plant-origin flavonoid,exhibits therapeutic anti-inflammatory,antioxidant,anticancer,antidiabetic,and neuroprotective properties.Kaempferol acts within several distinct mechanisms like apoptotic induction in cancer cells,enzymatic inhibition,signalling pathway inhibition,and downregulation in cell viability during the G2/M phase of cell division.This review summarizes the therapeutic effects of kaempferol against several health ailments.The recent progress on kaempferol obtained from fruits and vegetables as an antioxidant,anti-inflammatory,anticancer,antidiabetic,and neuroprotective agent and its mechanisms of action are also discussed.In addition,kaempferol has been reported to be present in wastes and byproducts from post-fruit and vegetable processing.Thus,a paradigm shift towards valorizing fruits and vegetable industrial wastes/byproducts to obtain bioactive kaempferol can support the circular economy pillar for generating wealth from waste and for finding a sustainable alternative source.
基金the National Natural Science foundation of China(No.82204938).
文摘Dysosma versipellis is the rhizome of Bajiaolian in Berberaceae.It is a unique medicinal plant in China and it was the first to be recorded in Shennong’s Classic of Materia Medica(unknown author,25–220 C.E.).It has complex chemical components as well as complex,pharmacological and toxicological effects are extensive.Based on the recent research progress,the chemical constituents,pharmacological activities and toxicological effects of Dysosma versipellis were summarized.Combined with the core concept of quality markers of traditional Chinese medicine,the prediction and analysis were carried out from the aspects of phytogenetics and the source pathway of specific chemical constituents,traditional medicinal properties,traditional efficacy,chemical composition measurability,blood components,and pharmacokinetics,in order to provide reference for further study of Dysosma versipellis.
基金supported by a grant from Research and Technology Chancellor of Guilan University of Medical Sciences,Iran(No.IR.GUMS.REC.1936.51)
文摘Alzheimer's disease(AD) is associated with oxidative stress, and ultimately results in cognitive deficit. Despite existing literature on the pathophysiology of AD, there is currently no cure for AD. The present study investigated the effects of kaempferol(Kmp) isolated from the extract of Mespilus germanica L.(medlar) leaves on cognitive impairment, hippocampal antioxidants, apoptosis, lipid peroxidation and neuro-inflammation markers in ovariectomized(OVX) rat models of sporadic AD. Kaempferol, as the main flavonoid of medlar extract has been previously known for anti-oxidative, anti-inflammatory and anti-neurotoxic effects. Thirty-two female Wistar rats were ovariectomized, and randomly divided into four groups: sham, OVX + saline, OVX + streptozotocin(STZ) + saline, OVX + STZ + Kmp. Animals received intracerebroventricular injection of STZ(3 mg/kg, twice with one day interval) to establish models of sporadic AD. Intraperitoneal injection of Kmp(10 mg/kg) for 21 days was performed in the OVX + STZ + Kmp group. Spatial learning and memory of rats were evaluated using a Morris water maze. Finally, brain homogenates were used for biochemical analysis by enzyme-linked immunosorbent assay. The results showed a significant improvement in spatial learning and memory as evidenced by shortened escape latency and searching distance in Morris water maze in the OVX + STZ + Kmp group compared with the OVX + STZ group. Kmp also exhibited significant elevations in brain levels of antioxidant enzymes of superoxide dismutase and glutathione, while reduction in tumor necrosis factor-α and malondialdehyde. Our results demonstrate that Kmp is capable of alleviating STZ-induced memory impairment in OVX rats, probably by elevating endogenous hippocampal antioxidants of superoxide dismutase and glutathione, and reducing neuroinflammation. This study suggests that Kmp may be a potential neuroprotective agent against cognitive deficit in AD.
文摘Severe acute respiratory syndrome coronavirus type 2(SARS-CoV-2)is a novel coronavirus identified at the end of 2019.It is recognized as the causative agent of coronavirus disease 2019(COVID-19).Flavonoids have been shown to exhibit therapeutical effect on complications related to COVID-19.The present study reviews possible therapeutic benefits of flavonoids on SARS-CoV-2.The Web of Science,PubMed,Scopus,and Google Scholar were searched using keywords:“COVID-19”,“SARS-CoV-2”,“Kaempferol”and“Quercetin”in the Title/Abstract.Relevant published articles in the English language until August 2020 were considered.Kaempferol and quercetin showed antiviral properties such as inhibition of protein kinase B and phosphorylation of protein kinase and blocking effects on a selective channel(3a channel)expressed in SARS-CoV infected cells.They also reduced the level of reactive oxygen species,expression of inducible nitric oxide synthase,pro-inflammatory mediators including TNF-α,IL-1α,IL-1β,IL-6,IL-10,and IL-12 p70,and chemokines.Kaempferol and quercetin might exert beneficial effects in the control or treatment of COVID-19 because of their antiviral,antioxidant,anti-inflammatory,and immunomodulatory effects.
文摘Objective:To identify alpha-glucosidase inhibitors from Ficus benghalensis and analyze gene set enrichment of regulated protein molecules.Methods:The phytoconstituents of Ficu.s benghalen.sis were queried for inhibitors of alphaglucosidase,also identified as aldose reductase inhibitors.Druglikeness score,absorption,distribution,metabolism,excretion and toxicity profile,biological spectrum,and gene expression were predicated for each compound.Docking study was performed to predict the binding affinity with alpha-glucosidase and aldose reductase and compared with clinically proven molecules.Kyoto Encyclopedia of Genes and Genomes pathway analysis was performed for the regulated genes to identify the modulated pathways.Results:Apigenin,3,4’,5,7-tetrahydroxy-3’-methoxyflavone,and kaempferol were identified as inhibitors of alpha-glucosidase and aldose reductase.Kaempferol was predicted to possess the highest binding affinity with both targets.The p53 signaling pathway was predicted to modulate the majority of protein molecules in diabetes mellitus.All the alpha-glucosidase inhibitors were also predicted as membrane integrity agonist and anti-mutagenic compounds.Conclusions:The current study indicates alpha-glucosidase inhibitors from Ficus benghale,nsis can act as aldose reductase inhibitors after absorption from the intestinal tract.Furthermore,these phytoconstituents are involved in the regulation of numerous protein molecules and pathways.Hence,the anti-diabetic efficacies of these compounds are due to their action on multiple protein molecules and synergistic effects which should be confirmed by future investigations.
基金The project supported by National Natural Science Foundation of China(81473383,81573645)
文摘OBJECTIVE To investigate the effects of kaempferol(KAE)on chronic cerebral ischemia in rats.METHODS Chronic cerebral ischemia was induced in rats by permanent occlusion of bilateral common carotid arteries(2VO).Then,the rats with chronic cerebral ischemia were randomly divied into three groups:model group,KAE 10 and 30 mg·kg-1group.Another group rats without occlusion of common carotid arteries were used as the sham-operation group.Memory behavior was investigated by Morris water maze test.Prehensile ability was investigated by prehensile traction test.The structure of hippocampus and cortex neurons was observed with Nissel staining.In addition,the SOD activity and MDA content in brain tissue were determined.The DJ-1protein level was determined by Western blotting.RESULTS KAE 10 and 30 mg·kg-1could significantly improve cognitive impairment and prehensile traction ability(P<0.01)induced by chronic cerebral ischemia in rats.The results of the pathological analysis also suggested that KAE could ameliorate the pathological damage induced by chronic cerebral ischemia.In addition,KAE 30 mg·kg-1significantly increased the activity of SOD(P<0.05),but had no effect on the content of MDA in rat brain tissue.Western-blotting confirmed that KAE 10 and30 mg·kg-1could increase the expression of anti-oxidation proteins DJ-1 in hippocampus(P<0.01).CONCLUSION KAE may attenuate the chronic cerebral ischemic injury in rats.
文摘[Objectives] To investigate the anti-tumor activity of Sedum bulbiferum Makino in vitro,and establish a HPLC method for determination of quercetin and kaempferol in S. bulbiferum. [Methods] The inhibitory activities of different extracts and total flavonoids of S. bulbiferum on proliferation of three kinds of cancer cells( Hep G2,EC109,SW480) were tested by MTT assay. HPLC method for determination of quercetin and kaempferol in S. bulbiferum was established. [Results]The growth and proliferation of the three kinds of cancer cells were all significantly inhibited by ethyl acetate fraction and total flavonoids isolated from S. bulbiferum. With each extraction concentration increasing,stronger anti-tumor activity was found. The linear ranges of quercetin and kaempferol were 0. 03-0. 36 μg( R = 0. 999 9) and0. 08-0. 96 μg( R = 0. 999 9),and the average recoveries were 98. 90%( RSD = 1. 15%) and 98. 27%( RSD = 1. 70%),respectively.[Conclusions]S. bulbiferum has significant anti-tumor activity in vitro. The HPLC method established was accurate,reproducible,and could be used for quality control of this crude drug.
文摘Tyrosinase inhibitory activity of the extractives from A. cathartica was examined and their new bioactivity and potent active compounds were identified. Five compounds, glabridin, new lignan, kaempferol, naringenin, and allamandicin, were isolated by a series of chromatography, and identified by NMR and LC-MS. Among them, glabridin had the high-est tyrosinase inhibitory activity (IC50:2.93 μM) which is 15 times stronger than that of kojic acid used as positive con-trol (IC50:43.7 μM). Moreover the lignan was indentified as 1-[3-(4-allyl-2,6-dimethoxyphenoxy)-4-methoxyphenyl] propane-1,2,diol which was a novel lignan.
基金Supported by the National Competitive Research Grant funded by the Ministry of Research,Technology and Higher Education,Republic of Indonesia(Grant No.056/UN8.2/PL/2015)
文摘Objective: To characterize the types, contents, and peroxynitrite-scavenging activities of flavonoids in the leaf of Carica papaya(C. papaya).Methods: Chromatographic and spectroscopic techniques along with high performance liquid chromatography quantitative analysis and peroxynitrite-scavenging assay were performed to isolate and quantify flavonoid compounds in the flavonoid-rich fraction(Bu OH fraction) derived from Me OH extract of C. papaya leaves and evaluate their peroxynitrite-scavenging activities.Results: Seven flavonoids were isolated from the leaves of C. papaya, including quercetin 3-(2~G-rhamnosylrutinoside), kaempferol 3-(2~G-rhamnosylrutinoside), quercetin 3-rutinoside, myricetin 3-rhamnoside, kaempferol 3-rutinoside, quercetin, and kaempferol. All of the substances exhibited potent activities on peroxynitrite scavenging(IC50 4.15 mmol/L), which were stronger than the positive control, L-penicillamine(6.90 mmol/L). The content of kaempferol 3-(2~G-rhamnosylrutinoside) was significantly higher than other identified compounds(123.18 mg/g Bu OH fraction and 7.23 mg/g Me OH extract).Conclusions: The results of the present study demonstrate the potent antioxidant flavonoids of C. papaya leaf, with kaempferol 3-(2~G-rhamnosylrutinoside) as the major one.
基金This work was supported by the Program of Sichuan Veterinary Medicine and Drug Innovation Group of China Agricultural Research System(SCCXTD-2020-18)the Science and Technology Project of Sichuan Province,China(2018NZ0043,2018NZ0064 and 2018HH0076).
文摘Pseudorabies virus(PRV),in the family Herpesviridae,is a pathogen of Aujeszky’s disease,which causes great economic losses to the pig industry.Recent outbreaks of Pseudorabies imply that new control measures are urgently needed.The present study shows that kaempferol is a candidate drug for controlling PRV infection,as it possesses the ability to inhibit PRV replication in a dose-dependent manner in vitro.Kaempferol at a concentration of 52.40μmol L^(-1) could decrease PRV-induced cell death by 90%.With an 50%inhibitory concentration(IC50)value of 25.57μmol L^(-1),kaempferol was more effective than acyclovir(positive control)which has an IC50 value of 54.97μmol L^(-1).A mode of action study indicated that kaempferol inhibited viral penetration and replication stages,decreasing viral loads by 4-and 30-fold,respectively.Addition of kaempferol within 16 h post infection(hpi)could significantly inhibit virus replication,and viral genome copies were decreased by almost 15-fold when kaempferol was added at 2 hpi.Kaempferol regulated the NF-κB and MAPKs signaling pathways involved in PRV infection and changed the levels of the target genes of the MAPKs(ATF-2 and c-Jun)and NF-κB(IL-1α,IL-1βand IL-2)signaling pathways.The findings of the current study suggest that kaempferol could be an alternative measure to control PRV infection.
基金supported by grants from the National Natural Science Foundation of China(No.21105032)Doctoral Program Fund of Ministry of Education of China(No.20110142120031)
文摘Novel uniform-sized magnetic molecularly imprinted polymers (MMIPs) were synthe- sized for selective recognition of active antitumor ingredients of kaempferol (KMF) and protoapi- genone (PA) in Macrothelypteris torresiana (M. torresiana) by surface molecular imprinting tech- nique in this study. Super paramagnetic core-sheU nanoparticles (γ-MPS-SiO2@Fe3O4) were used as seeds, KMF as template molecule, acrylamide (AM) as functional monomer, and N, N'-methylene bisacrylamide (BisAM) as cross-linker. The prepared MMIPs were characterized by X-ray diffraction (XRD), Fourier transform infrared spectrum fiT/R), transmission electron microscopy (TEM) and thermo-gravimetric analysis (TGA), respectively. The recognition capacity of MMIPs was 2.436 times of non-imprinted polymers. The adsorption results based on kinetics and isotherm analysis were in accordance with the pseudo-second-order model (R2=0.9980) and the Langmuir adsorption model (R2=0.9944). The value of E (6.742 kJ/mol) calculated from the Dubinin-Radushkevich isotherm model suggested that the physical adsorption via hydrogen-bonding might be predominant. The Scatchard plot showed a single line (R2=0.9172) and demonstrated the homogeneous recognition sites on MMIPs for KMF. The magnetic solid phase extraction (MSPE) based on MMIPs as sorbent was established for fast and selective enrichment of KMF and its structural analogue PA from the crude extract of M. torresiana and then KMF and PA were detected by HPLC-UV. The established method showed good performance and satisfactory results for real sample analysis. It also showed the feasi- bility of MMIPs for selective recognition of active structural analogues from complex herbal extracts.
基金Supported by Key Science and Technology Project for Agriculture in Guizhou Province(NY[2013]3017)Project of Guizhou Tartary Buckwheat Engineering and Technology Research Center([2015]4003-B1)+2 种基金Doctoral Foundation of Science and Technology Plan of Guizhou Province([2017]1191)Youth Foundation of Guizhou Academy of Agricultural Sciences([2017]26)Key Technology Research and Development Program of Guizhou Province([2017]2543)
文摘The contents of rutin,quercetin and kaempferol in powders of tartary buckwheat of different parts were determined by high-performance liquid chromatography( HPLC). The results showed that the contents of the three kinds of flavonoids differed greatly in the powders of tartary buckwheat of different parts. The contents of rutin and quercetin in the powder of tartary buckwheat sprouts were significantly higher than those in the powders of tartary buckwheat leaves and seeds. The content of kaempferol was highest in the powder of tartary buckwheat seeds. It indicates that high-performance liquid chromatography can be used for quality control of tartary buckwheat powder for its time saving,cost saving and accurate and reliable results. The content of rutin in the powder of tartary buckwheat sprouts was highest,suggesting that it is more suitable for the development of various foods based on tartary buckwheat powder.
文摘Aim To study the chemical composition of Opuntia dillenii Haw. Methods Manykinds of chromatogra-phy methods were used in the isolation procedure, while the structures ofisolated compounds were determined on the aids of NMR and MS spectral analysis. Result Three newcompounds, together with 14 known compounds, were isolated form the 80% ethanolic extract of itsstems. Conclusion The three new compounds, opuntioside Ⅰ (2), 4-ethoxyl-6-hydroxymethyl-α-pyrone(3) and kaempferol 7-O-β-D-glucopyranosyl (1→4)-β-D-glucopyranoside (4), were characterized.
文摘Background:The breast cancer has been the most common form of cancer among women.The triple negative subtype represents 20%of all breast cancer cases in the world and is standing out by affecting young women and being aggressive.The main cause of death of patients with cancer is due to metastasis,which can reach the liver and lungs.Objective:The activities of ID7 fraction of the stems of Bauhinia variegata L.on breast cancer,lung metastasis and liver inflammatory process were evaluated.Method:ID7 was characterized by mass-spectrometry.The viability of murine mammary cells(4T1)treated with ID7 was assessed by MTT,trypan blue and fluorescence assay and viability of BT-20,MDA-MB-231 and MCF-7 human breast cancer tumor lines by MTS.The cell migration,invasion using matrigel and adhesion were performed.The expression of cell death proteins was quanitified by western blot and the gelatinases by zimogram.The ID7 activity of the tumor(4T1)and metastatic progession in vivo was evaluated.Results:ID7 reduced the 4T1 and MDA-MB-231viability and increased the late apoptosis,inhibited the 4T1 migration and invasion,increased the 4T1 adhesion and decreased the secreted active gelatinases.ID7 also increased the expression of PARP,caspase-7 and caspase-8,RIP and TNF-R1.In vivo,the ID7 decreased the volume and weight of the tumors and decreased lung metastasis and inflammation in the liver.The characterization showed mainly the presence of oleic acid,myricetin,quercetin and kaempferol in ID7.Conclusion:Thus,it was found that ID7 fraction exhibits selective antitumor and on the mechanisms of breast cancer metastasis activity,preventing lung metastasis and inflammation in the liver.It is suggested that fatty acids and flavonoids are correlated with such activities.