Flavone improves liver damage in nicotine-exposed rats via the Nrf2/HO-1 pathway

Objective:To assess the hepatoprotective effects of flavone on nicotine-induced liver damage.Methods:Thirty-six rats were allocated into six groups:the control group,the nicotine group,the flavone alone groups(10 and 25 mg/kg/body weight),and the nicotine groups treated with flavone(10 and 25 mg/kg/body weight).Liver function,oxidative stress,Nrf2 pathway(HO-1,Nrf2,and Keap-1),and inflammatory markers(IL-17,TNF-α,and NF-κB)were evaluated.Additionally,a histopathological examination of liver tissues was performed.Results:Nicotine increased liver damage,inflammation,and oxidative stress.However,flavone suppressed nicotine-induced liver enzymes,oxidative stress,and inflammation,as manifested by increased antioxidants and decreased malondialdehyde level,liver enzymatic activities,and inflammatory markers.Flavone(10 and 25 mg/kg/body weight)also reduced the level of Keap-1 and increased HO-1 and Nrf2 levels in the liver of nicotine-exposed rats.Conclusions:Flavone has hepatoprotective properties and may slow the progression of liver injury by reducing oxidative stress,liver enzymes,and inflammation possibly via the Nrf2 pathway.

Effects of ginkgo flavone aglycone on atherosclerosis based on network pharmacology,molecular docking,and in vitro experiments

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.

A New Diels-Alder Type Adduct and a New Flavone from the Stem and Root Bark of Morus mongolica

A new Diels-Alder type adduct mongolicin G （1） and a new flavone 5＇-（1＂, 1＂-dimethylallyl）-5,7,2＇,4＇-tetrahydroxyflavone （2） were isolated from the stem and root bark of Morus mongolica. Their structures were determined by spectroscopic analysis and chiroptical methods.

Ultrasonic Sound Hot Extract—Ultraviolet Spectrophotometric Determination of Total Flavone in Comb Honey

[Objective] The aim was to establish a rapid method for the determination of the content of total flavonoids in the honey comb. [Method] The content of total flavonoids weas determined based on samples including comb honey, propolis, royal jelly, linden tree honey, with a polyamide column chromatography by spectrophotometry at 360 nm wavelength. [Result] The recovery rate of the method was above 90%, and the variation coefficient was lower than 2%. Compared with the traditional method, this method has less reagent consumption, simple operation and so on.[Conclusion] The content of total flavonoids in comb honey was 14.97 mg/100 g, although is only 0.87% of the total flavone content in propolis. The contained total flavonoids at least doubled than that of others and comb honey is more valuable in the content of flavonoids.

Natural variation of GmFNSII-2 contributes to drought resistance by modulating enzyme activity in soybean

As an essential crop that provides vegetable oil and protein,soybean(Glycine max(L.)Merr.)is widely planted all over the world.However,the scarcity of water resources worldwide has seriously impacted on the quality and yield of soybean.To address this,exploring excellent genes for improving drought resistance in soybean is crucial.In this study,we identified natural variations of GmFNSII-2(flavone synthase II)significantly affect the drought resistance of soybeans.Through sequence analysis of GmFNSII-2 in 632 cultivated and 44 wild soybeans nine haplotypes were identified.The full-length allele GmFNSII-2^(C),but not the truncated allele GmFNSII-2^(A) possessing a nonsense nucleotide variation,increased enzyme activity.Further research found that GmDREB3,known to increase soybean drought resistance,bound to the promoter region of GmFNSII-2^(C).GmDREB3 positively regulated the expression of GmFNSII-2^(C),increased flavone synthase abundance and improved the drought resistance.Furthermore,a singlebase mutation in the GmFNSII-2^(C) promoter generated an additional drought response element(CCCCT),which had stronger interaction strength with GmDREB3 and increased its transcriptional activity under drought conditions.The frequency of drought-resistant soybean varieties with Hap 1(Pro:GmFNSII-2^(C))has increased,suggesting that this haplotype may be selected during soybean breeding.In summary,GmFNSII-2^(C) could be used for molecular breeding of drought-tolerant soybean.

Analysis of Flavone Content in Honey of Pomegranate Flowers

[Objective] The aim was to analyze content of flavones in honey of pomegranate flowers. [Method] Contents of total flavones in 24 honey samples of pomegranate flowers from Mengzi City in 2011 and 2012 were measured as per- spectrophotometry method with acetone as an extractant and rutin as a control. [Result] The average content of flavones in honey of pomegranate flowers was at （2.36±1.36）mg/100 g in 2011 and significantly higher than that in 2012 at （1.71± 0.53）mg/100 g. Analysis was conducted on flavones content in different batches and the results indicated that content of flavones in honey in different batches changed from increasing to decreasing, namely, the content was maximal in peak flowering stage, followed by late flowering stage and initial flowering stage. [Conclusion] The research provides references for development, use and function exploration of the honey of pomegranate flowers.

The superiority of PMFs on reversing drug resistance of colon cancer and the effect on aerobic glycolysis-ROS-autophagy signaling axis

Background:Polymethoxylatedflavones(PMFs)are compounds present in citrus peels and other Rutaceae plants,which exhibit diverse biological activities,including robust antitumor and antioxidant effects.However,the mechanism of PMFs in reversing drug resistance to colon cancer remains unknown.In the present study,we aimed to investigate the potential connection between the aerobic glycolysis-ROS-autophagy signaling axis and the reversal of PTX resistance in colon cancer by PMFs.Methods:MTT Cell viability assay and colony formation assay were used to investigate the effect of PMFs combined with PTX in reversing HCT8/T cell resistance ex vivo;the mRNA and protein levels of the target were detected by SDS-PAGE(sodium dodecyl sulfate-polyacrylamide gel electrophoresis),quantitative real-timefluorescence polymerase chain reaction(qRT-PCR)and Western blot protein immunoblotting(WB);An HCT8/T cell xenograft model was established to investigate the MDR reversal activity of PMFs in vivo;The extracellular acidification rate(ECAR)and the oxygen consumption rate(OCR)were detected to assess the cellular oxygen consumption rate and glycolytic process.Results:HCT8/T cells demonstrated significant resistance to PTX,up-regulating the expression levels of ABCB1 mRNA,P-gp,LC3-I,and LC3-II protein,and increasing intracellular reactive oxygen species(ROS)content.PMFs mainly contain two active ingredients,nobiletin,and tangeretin,which were able to reverse drug resistance in HCT8/T cells in a concentration-dependent manner.PMFs exhibited high tolerance in the HCT8/T nude mouse model while increasing the sensitivity of PTX-resistant cells and suppressing tumor growth significantly.PMFs combined with PTX reduced extracellular acidification rate(ECAR)and oxygen consumption rate(OCR)in HCT8/T cells.Additionally,PMFs reduced intracellular ROS content,down-regulated the expression levels of autophagy-related proteins LC3-I,LC3-II,Beclin1,and ATG7,and significantly reduced the number of autophagosomes in HCT8/T cells.Conclusions:The present study demonstrated that PMFs could potentially reverse PTX resistance in colon cancer by regulating the aerobic glycolysis-ROS-autophagy signaling axis,which indicated that PMFs would be potential potentiators for future chemotherapeutic agents in colon cancer.

Flavones Isolated from Codonopsis xundianensis

Genus Codonopsis comprises more than 40 species in China. The roots of these plants have been used as traditional Chinese medicines or folk love herbs. Codonopsis xundianensis Wang ZT et Xu GJ grows in Yunnan Province and its roots are often used as a tonic. In this paper, we report the isolation and structural elucidation of chrysoeriol (1), tricin (2), wogonin (3) and luteolin (4) from the roots of Codonopsis xundianensis. Compounds 1-3 were found in Codonopsis for the first time.

A new flavone glycoside from Selaginella moellendorffii Hieron.

From the ethanol extract of Selaginella moellendorffii Hieron., a new flavone O-glycoside and three known flavone C-glycosides have been isolated and identified as 5-carboxymethyl-4′-hydroxyflavone-7-O-β-D-glucopyranoside 1, 6,8-di-C-β-D-glueopyranosylapigenin 2, 6-C-[3-D-glucopyranosyl-8-C-β-D-xylopyranosyl apigenin 3, 6-C-B-D-xylopyranosyl-8-C-β-glucopyranosylapigenin 4, respectively. Their structures were elucidated by spectroscopic methods.

Antioxidations and Their Correlations with Total Flavones and Anthocyanin Contents in Different Black Rice Varieties

The antioxidations and their correlations with total flavones and anthocyanin contents in different black rice varieties were studied. The results indicated that the great differences in total antioxidant capacity （TAC）, scavenging free radical capacity （SFRC）, total flavones and anthocyanin contents existed among 242 black rice varieties. Comparisons of TAC, SFRC, total flavones and anthocyanin contents of different black rice types showed that the differences between black rice and white rice, indica one and japonica one, and nonglutinous one and glutinous one were significant at 0.01 levels, respectively. This showed that the TAC, SFRC, total flavones and anthocyanin contents of japonica type were higher than those of indica one, and nonglutinous type were higher than glutinous one. According to the fast clustering procedure, 242 black rice varieties could be clustered into 10 clusters, 184 indica rice varieties into 10 clusters, and 58 japonica rice varieties into 6 clusters. Most significant （P〈0.01） correlations existed between TAC and total flavones and anthocyanin contents, and between SFRC and total flavones and anthocyanin contents of black rice, respectively. This showed that the antioxidation of black rice was closely correlated with its active compositions of flavones and anthocyanin.

Total flavone of Abelmoschus manihot suppresses epithelial-mesenchymal transition via interfering transforming growth factor-β1 signaling in Crohn's disease intestinal fibrosis

AIM To explore the role and mechanism of total flavone of Abelmoschus manihot(TFA) on epithelial-mesenchymal transition(EMT) progress of Crohn's disease(CD) intestinal fibrosis.METHODS First,CCK-8 assay was performed to assess TFA on the viability of intestinal epithelial(IEC-6) cells and select the optimal concentrations of TFA for our further studies.Then cell morphology,wound healing and transwell assays were performed to examine the effect of TFA on morphology,migration and invasion of IEC-6 cells treated with TGF-β1.In addition,immunofluorescence,real-time PCR analysis(q RT-PCR) and western blotting assays were carried out to detect the impact of TFA on EMT progress.Moreover,western blotting assay was performed to evaluate the function of TFA on the Smad and MAPK signaling pathways.Further,the role of co-treatment of TFA and si-Smad or MAPK inhibitors has been examined by q RTPCR,western blotting,morphology,wound healing andtranswell assays.RESULTS In this study,TFA promoted transforming growth factor-β1(TGF-β1)-induced(IEC-6) morphological change,migration and invasion,and increased the expression of epithelial markers and reduced the levels of mesenchymal markers,along with the inactivation of Smad and MAPK signaling pathways.Moreover,we revealed that si-Smad and MAPK inhibitors effectively attenuated TGF-β1-induced EMT in IEC-6 cells.Importantly,co-treatment of TFA and si-Smad or MAPK inhibitors had better inhibitory effects on TGF-β1-induced EMT in IEC-6 cells than either one of them.CONCLUSION These findings could provide new insight into the molecular mechanisms of TFA on TGF-β1-induced EMT in IEC-6 cells and TFA is expected to advance as a new therapy to treat CD intestinal fibrosis.

Preparation and Dyeing Performance of a Novel Crosslinking Polymeric Dye Containing Flavone Moiety

A yellow crosslinking polymeric dye was prepared by grafting the flavone moiety containing azo chromophore onto polyvinylamine backbone.The λ max of this polymeric dye in water is 382 nm.The polymeric dye is fixed to silk and cotton with a crosslinking agent,2-chloro-4,6-di(aminobenzene-4'-β-sulphatoethylsulphone)-1,3,5-s-triazine,which acts as a bridge between the fiber and dye molecules.The fixation of this polymeric dye reaches 99% and the dyed samples exhibit excellent rubbing and washing fastness.

Effects of Total Flavone of Abelmoschl Manihot L.Medic on the Function of Platelets and Its Mechanism

Objective: To study the effects of total flavone of Abelmoschl Manihot L.Medic (TFA) on the function of platelets and to explore its mechanism. Methods: Rat models of artery-veins bypassing thrombus formation were used. The platelets of rabbits were collected. Platelet aggregation was induced by collagen and intracellular calcium ion concentration ([Ca 2+ ]i) was assayed by Fura-2 method. Results: TFA (25, 50, 100 mg/kg) significantly and dose-dependently reduced the weight of thrombus. TFA (0.025, 0.05, 0.1 mg/ml) possessed dose-dependant inhibitory effects on rabbits' platelet aggregation induced by collagen. TFA significantly reduced the resting and CaCl 2-induced increase of free intracellular calcium concentration ([Ca 2+ ]i) in rabbit platelet in vitro . Conclusion: TFA has an antiplatelet effect via the inhibition on the influx of Ca 2+ .

New flavone and isoflavone glycoside from Belamcanda chinensis

The new flavone, 5,4′-dihydroxy-6,7-methylenedioxy-3′-methoxyflavone, and one new isoflavone glycoside, 3′,5′-dimethoxy irisolone-4′-O-β-d-glucoside were isolated from the rhizomes of Belamcanda chinensis. Their structures were established based on the spectroscopic methods.

A New Flavone Glycoside from Epimedium koreanum

A novel flavone glycoside named 3＇＇＇-carbonyl-2＇＇-β-L-quinovosyl icariside Ⅱ was isolated from the aerial parts of Epimedium koreanum. Its chemical structure was elucidated on the basis of spectral analysis.

Two New Flavone Glucosides fromSerratula strangulata

Genus Serratula（Compositae）consists of about 70 species distributed throughout theworld[1]．Serratula species have been used as folk medicine to treat chickenpox，toxicosis，high cholesterol in China[2]. The phytochemical study of plant S．strangulata has not beenreported so far．In the course of our searching for biologically active substances from thisplant，two new flavone glucosides（1，2）were isolated．The present paper covers the isolationand structural elucidation of the two new compounds．

A Minor New Flavone from Scutellaria baicalensis Georgi

A new flavone, 6, 2-dihydroxy-5, 7, 8, 6-tetramethoxyflavone, was isolated from the roots of Scutellaria baicalensis. Its structure was established on the basis of spectral evidences.

Mahuangchiside, a New Flavone Glycoside from Chirita fimbrisepala

A new flavone glycoside, named mahuangchiside, was isolated from the root of Chirita fimbrisepala Hand.-Mazz. The structure was elucidated as 5,4'-dihydroxy-6-methoxyflavone-7-O-beta-D-xylopyranosyl(1-->2)-beta-D-xylopyranoside on the basis of spectral analysis (H-1-H-1 COSY. C-13-H-1 HETCOR and HMBC) and chemical evidence.

Influence of flavone extract from cultivated saussurea on learning and memory in a mouse model of Alzheimer's disease A comparison with estradiol benzoate

The present study established a mouse model of Alzheimer＇s disease, and investigated the effects of treatment with flavone extract from artificially cultivated saussurea. A positive control group was treated with estradiol benzoate, and learning and memory ability were examined in the 8-arm radial maze. The learning and recognition ability of mice with Alzheimer＇s disease treated with flavone extract was significantly improved and the number of hippocampal neurons was significantly increased in the flavone-treated and positive control groups compared with the model group. The results indicate that flavone extract from artificially cultivated saussurea can improve learning and memory deficits in mice with Alzheimer＇s disease, exerting effects similar to those of estradiol benzoate.