• Journal of the Korean Society of Tobacco Science
• /
• v.2 no.2
• /
• pp.8-13
• /
• 1980

The inhibition effect of flavone and butylatedhydroxyanisole (BHA) on the microsomal activation of Cigarette Smoke Condensate (CSC) or its Neutral Portion (NP) was investigated in Rat. The activities of Latic acid dehydrogenase (LDH) in serum was measured in the time intervals of 3, 6, 12, 18, 24 and 30 hr, respectively, after the injection (ip) of CSC (5mg/kg) or NP (10mg/kg) to Wistar male rat. Flavone (1mg/kg) and BHA (1mg/kg) were injected along with CSC or NP. The significant enhancement of the LDH activity in serum was observed in both cases of rats treated with CSC and NP. A drastic decrease of LDH activity from 1040 unit to 641 unit was observed after 12 hours of injection of CSC along with flavone. In contrast with the case of flavone, BHA reduced the enzyme activity from 825 unit to 652 unit at the same condition of flavone. Therefore, flavone can be considered to be a better inhibitor on action of CSC in vivo.

• YAKHAK HOEJI
• /
• v.47 no.2
• /
• pp.98-103
• /
• 2003

The purpose of this study was to investigate the effect of flavone (20 mg/kg) on the pharmacokinetic parameters and the bioavailability of paclitaxel (40 mg/kg) orally coadministered in rats. The plasma concentration of paclitaxel in combination with flavone was increased significantly (coadministration p＜0.05, pretreatment p＜0.0l) compared to that of control. Area under the plasma concentration-time curve (AVC) of paclitaxel with flavone was significantly (coadministration p＜0.05, pretreatment p＜0.0l) higher than that of control. Peak concentration (Cmax) of paclitaxel with flavone were significantly increased (coadministration p＜0.05, pretreatment p＜0.01) compared to that of control. Time to peak concentration (Tmax) of paclitaxel with flavone decreased significantly (p＜0.05) than that of control. The total body clearance (CLt) and elimination rate constant ($\beta$) of paclitaxel with flavone were significantly reduced (p＜0.05) compared to those of control. Half-life (t$_{1}$2/) of paclitaxel with flavone was significantly prolonged (p＜0.05) compared to that of control. Based on these results, it might be concluded that flavone may enhance bioavailability of paclitaxel through the inhibition of cytochrome P450 and P-glycoprotein, which are engaged in paclitaxel absorption and metabolism in liver and gastrogintestinal mucosa, respectively.

• Molecules and Cells
• /
• v.27 no.3
• /
• pp.345-350
• /
• 2009

We previously reported that flavone induces embryonic lethality in Caenorhabditis elegans, which appeared to be the result of cell cycle arrest during early embryogenesis. To test this possibility, here we examined whether flavone inhibits the activity of a key cell cycle regulator, CDC-25.1 in C. elegans. A gain-of-function cdc-25.1 mutant, rr31, which exhibits extra cell divisions in intestinal cells, was used to test the inhibitory effects of flavone on CDC-25 activity. Flavone inhibited the extra cell divisions of intestinal cells in rr31, and modifications of flavone reduced the inhibitory effects. The inhibitory effects of flavone on CDC-25.1 were partly, if not completely, due to transcriptional repression.

• The Korean Journal of Physiology and Pharmacology
• /
• v.13 no.3
• /
• pp.201-207
• /
• 2009

Our previous study demonstrated that flavone inhibits vascular contractions by decreasing the phosphorylation levelof the myosin phosphatase target subunit (MYPT1). In the present study, we hypothesized that flavone attenuates vascular contractions through the inhibition of the RhoA/Rho kinase pathway. Rat aortic rings were denuded of endothelium, mounted in organ baths, and contracted with either 30 nM U46619 (a thromboxane A2 analogue) or 8.0 mM NaF 30 min after pretreatment with either flavone (100 or 300 $({\mu}M$) or vehicle. We determined the phosphorylation level of the myosin light chain ($MLC_{20}$), the myosin phophatase targeting subunit 1 (MYPT1) and the protein kinase C-potentiated inhibitory protein for heterotrimeric myosin light chain phophatase of 17-kDa (CPI17) by means of Western blot analysis. Flavone inhibited, not only vascular contractions induced by these contractors, but also the levels of $MLC_{20}$ phosphorylation. Furthermore, flavone inhibited the activation of RhoA which had been induced by either U46619 or NaF. Incubation with flavone attenuated U46619 or NaF-induced phosphorylation of $MYPT1^{Thr855}$ and $CPI17^{Thr38}$, the downstream effectors of Rho-kinase. In regards to the $Ca^{2+}$-free solution, flavone inhibited the phosphorylation of $MYPT1^{Thr855}$ and $CPI17^{Thr38}$, as well as vascular contractions induced by U 46619. These results indicate that flavone attenuates vascular contractions, at least in part, through the inhibition of the RhoA/Rho-kinase pathway.

• Natural Product Sciences
• /
• v.8 no.4
• /
• pp.127-128
• /
• 2002

A flavone glycoside was isolated from the roots of Angelica gigas (Umbelliferae) and identified as diosmin $[diosmetin-7-O-{\alpha}-{_L}-rhamnopyranosyl \;(1{\rightarrow}6)-{\beta}-{_D}-glucopyranoside]$ by spectroscopic methods. This is the first report of a flavone gylcoside from Angelica species.

• Journal of Applied Biological Chemistry
• /
• v.52 no.1
• /
• pp.15-20
• /
• 2009

Poplar contains various flavonoids including naringenin, kaempferol, myricetin, apigenin, luteolin, rhamnetin, and quercetin. These flavonoids are synthesized from naringenin with various enzymes. However, none of genes from poplar involved in flavonoid biosynthesis have been biochemically characterized. We cloned PFNS I-1 from Populus deltoids by RT-PCR method. The open reading frame of PFNS I-1 consisted of 1,017-bp and it showed high similarity with other FNS genes. The purified recombinant PFNS I-1, expressed in Escherichia coli, catalyzed the reaction from flavanone (naringenin) to flavone (apigenin). The reaction of PFNS I-1 was enhanced by cofactors such as oxoglutarate, $Fe^{2+}$, ascorbate and catalase. Thus, it is concluded that PFNS N-1 encodes a flavone synthase I.

• Archives of Pharmacal Research
• /
• v.27 no.6
• /
• pp.610-614
• /
• 2004

The in vitro antioxidant properties of some flavone-6(4)-carboxaldehyde oxime ether deriva-tives (Ia-f, lIa-f） were determined by their effects on the rat liver microsomal NADPH-dependent lipid peroxidation (LP） levels by measuring the formation of 2-thiobarbituric acid reactive substances. The free radical scavenging properties of the compounds were also examined in vitro by determining their capacity to scavenge superoxide anions and interact with the stable free radical 2, 2-diphenyl-1-picrylhydrazyl (DPPH). The most active compounds, lib (Flavone-4＇-carboxaldehyde-O-ethyl oxime） and Id (Flavone-6-carboxaldehyde-O-［2-(1-pyrolidino） ethyl］ oxime）, caused 98 and 79％ inhibition of superoxide anion production and DPPH stable free radical at $10^{-3}{\;}M$, respectively.

• YAKHAK HOEJI
• /
• v.50 no.6
• /
• pp.398-402
• /
• 2006

Flavone was found to inhibit tyrosinase and reduce synthesis of melanin to show skin-lightening effect. With the hope of identifying skin-lightening flavones, we synthesized flavone analogs. Substituted benzoic acids (1) were treated with oxalyl chloride in DMF to yield benzoyl chlorides (2), which were reacted with 2-hydroxyacetophenones (3) to afford 2-benzoyloxyacetophenones (4). These acetophenones (4) were converted into 1,3-diketones (5) with base and then treated with acid to give flavone derivatives (6).

• Mycobiology
• /
• v.36 no.2
• /
• pp.121-133
• /
• 2008

Aspergillus niger isolated from Allium sativum was used at large scale fermentation (150 mg flavone/200ml medium) to obtain suitable amounts of the products, efficient for identification. Then spectral analysis (UV, IR, $^1H$-NMR, $^{13}C$-NMR) and mass spectrometry were performed for the two products, which contributed to the identification process. The metabolite (1) was identified as 2'-hydroxydihydrochalcone, and the metabolite (2) was identified as 2'-hydroxyphenylmethylketone, which were more active than flavone itself. Antioxidant activities of the two isolated metabolites were tested compared with ascorbic acid. Antioxidant activity of metabolite (1) was recorded 64.58% which represented 79% of the antioxidant activity of ascorbic acid, and metabolite (2) was recorded 54.16% (67% of ascorbic acid activity). However, the antioxidant activity of flavone was recorded 37.50% which represented 46% of ascorbic acid activity. The transformed products of flavone have anti-microbial activity against Pseudomonas aeruginosa, Aspergillus flavus and Candida albicans, with MIC was recorded $250{\mu}g/ml$ for metabolite (2) against all three organism and 500, 300, and $300{\mu}g/ml$ for metabolite (1) against tested microorganisms (P. aeruginosa, Escherichia coli, Bacillus subtilis, and Klebsiella pneumonia, Fusarium moniliforme, A. flavus, Saccharomyces cerviceae, Kluveromyces lactis and C. albicans) at this order.

• KSBB Journal
• /
• v.13 no.3
• /
• pp.259-267
• /
• 1998

Optimal feeding strategies in bioreactor operation of Scutellaria baicalensis G. plant cell culture were investigated to maximize the production of flavone glycosides by using a structured kinetic model which can predict culture growth and flavone glycosides synthesis in a rigorous, quantitative manner. For the production of baicalin and wogonin-7-0-GA, the strategies for glucose feeding into Scutellaria baicalensis G. plant cell culture were proposed based on the model, which are a periodic fed-batch operation with maintenance of cell viability and of specific production rate respectively, and a perfusion operation with maintenance of specific production rate for baicalin and wogonin-7-0-GA. Simulation results showed that the highest volumetric concentration of flavone glycosides was obtained in a periodic fed-batch operation with maintenance of cell viability among all the suggested strategies. In the periodic fed-batch operations, the higher volumetric production of flavone glycosides was achieved compared with that in the perfusion operation. It can be concluded that a periodic fed-batch operation with maintenance of cell viability would be the optimal and practical operating strategy of Scutellaris baicalensis G. plant cell culture for the production of flavone glycosides.