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.

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.

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.

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.

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.

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.

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.

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．

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.

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.

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+ .

Development and Validation of a HPLC Method for Determination of Flavone Glycoside-Camellianin B in Cephalotaxus Sinensis

A simple,rapid and sensitive method for the quantification of camellianin B in Cephalotaxus sinensis（C.sinensis）a natural plant with anti-hyperglycemic effect,was developed and validated by reversed phase liquid chromatography.Chromatographic separation was achieved on a C18 column and an isocratic elution was carried out at a flow-rate of 1.0 mL·min-1 with the acetonitrile-water containing0.1%formic acid（19∶81,v/v）.The detection wavelength was set at 330 nm.The calibration curve was linear over the concentration range of 0.25-50μg·mL-1 with correlation coefficients larger than0.999 5.The limit of detection and limit of quantification were 0.09μg·mL-1and 0.25μg·mL-1,respectively.The precisions and accuracy for all samples were acceptable.The validated method has been successfully applied for the quantification of camellianin B in C.sinensis harvested in different months and may also be used as the quality evaluation of this herb medicine.

Facile Syntheses of 3-Isopentenyl Flavone and 3-Geranyl Flavone

Although there was a strong steric effect,isopentenyl and geranyl moieties were successfully introduced into C3 position in flavone skeleton so as to synthesize the 3-isopentenyl flavone and 3-geranyl flavone under two cyclization conditions（AcOH/HCl and concentrated H 2 SO 4 /MeOH） in this report.It was found that the optimum cyclization conditions for 3-isopentenyl flavone and 3-geranyl flavone were,respectively,AcOH/HCl and H 2 SO 4 /MeOH.Furthermore,the donating electron ability is in the sequence 3-geranyl flavone3-isopentenyl flavone according to the density functional theory（DFT） calculations,suggesting the longer alkyl chain at 3-position would be more favorable for enhancing the donating electron ability.The present synthetic routes might reveal potential applicability in our continued studies on the total syntheses of other natural 3-alkyl flavonoids.

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.

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.

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.

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.

In Vitro Anti-viral Activities and Structureactivity Relationship Studies of Flavones and Dihydroflavone Derivatives as Influenza Virus Potential Neuraminidase Inhibitors

From the bioassay tests, 14 neuraminidase inhibitors （NIs） flavones and dihydroflavones derivatives from natural plants displayed different degree of inhibitory activities. Further- more, compounds No. 8 and 14 showed good inhibitory activity against influenza A virus with IC50 = 835.4 and 860.6 μg/mL. Then, to investigate interactions between NIs and neuraminidase （NA）, molecular docking was performed. Docking results indicated that Arg118, Asp151, Arg292 and Arg371 were the key residues in the active pocket of 2ht8. Main influencing factors of interactions between NIs and NA were hydrogen bond and electrostatic, then hydrophobic factor. Moreover, experimental activities of NIs were consistent with total scores of the docking. In order to understand the chemical-biological interactions governing their activities toward NA, QSAR models of 14 NIs were developed. The obtained HQSAR （hologram quantitative structure activity relationship）, PLS （partial least squares） and SRA （stepwise regression analysis） models were robust and had good exterior predictive capabilities. Moreover, squared multiple correlation coefficients （R2） and squared cross-validated correlation coefficients （Q2） of HQSAR and PLS models based on descriptors by Gaussian and Sarchitect were 0.832 and 0.721, 0.925 and 0.688, 0.892 and 0.692, respectively. R2 and SE （standard error） of SRA model based on descriptors by Gaussian were 0.922 and 0.072. Therefore, these models may be further used to design and evaluate the bioactivity of new compounds.