Showing papers on "Acacetin published in 2013"
TL;DR: Overall, acacetin inhibits Stat signaling and suppresses angiogenesis in vitro, ex vivo, and in vivo and therefore, it could be a potential agent to inhibit tumorAngiogenesis and growth.
Abstract: Angiogenesis is an effective target in cancer control. The antiangiogenic efficacy and associated mechanisms of acacetin, a plant flavone, are poorly known. In the present study, acacetin inhibited growth and survival (up to 92%; P < 0.001), and capillary-like tube formation on Matrigel (up to 98%; P < 0.001) by human umbilical vein endothelial cells (HUVEC) in regular condition, as well as VEGF-induced and tumor cells conditioned medium–stimulated growth conditions. It caused retraction and disintegration of preformed capillary networks (up to 91%; P < 0.001). HUVEC migration and invasion were suppressed by 68% to 100% ( P < 0.001). Acacetin inhibited Stat-1 (Tyr701) and Stat-3 (Tyr705) phosphorylation, and downregulated proangiogenic factors including VEGF, endothelial nitric oxide synthase (eNOS), inducible nitric oxide synthase (iNOS), matrix metalloproteinase-2 (MMP-2), and basic fibroblast growth factor (bFGF) in HUVEC. It also suppressed nuclear localization of pStat-3 (Tyr705). Acacetin strongly inhibited capillary sprouting and networking from rat aortic rings and fertilized chicken egg chorioallantoic membrane (CAM; ∼71%; P < 0.001). Furthermore, it suppressed angiogenesis in Matrigel plugs implanted in Swiss albino mice. Acacetin also inhibited tyrosine phosphorylation of Stat-1 and -3, and expression of VEGF in cancer cells. Overall, acacetin inhibits Stat signaling and suppresses angiogenesis in vitro , ex vivo , and in vivo , and therefore, it could be a potential agent to inhibit tumor angiogenesis and growth. Cancer Prev Res; 6(10); 1128–39. ©2013 AACR .
58 citations
TL;DR: Quercetin was found to induce apoptosis in KB and KBv200 cells via the mitochondrial pathway, including a decrease of the reactive oxygen species level, loss of mitochondrial membrane potential, release of cytochrome c, activation of caspase-9 and caspases-3, and cleavage of poly (ADP-ribose) polymerase.
Abstract: In this study, anticancer activities of six compounds of flavonoids were investigated in human epidermoid carcinoma KB and KBv200 cells. Among these compounds, quercetin and acacetin showed strong inhibition of cell growth in KB and KBv200 cells. IC50 values of quercetin against KB and KBv200 cells were 17.84 ± 4.14 and 18.94 ± 4.75 μM, respectively. The IC50 values of acacetin against KB and KBv200 cells were 41.33 ± 6.05 and 49.04 ± 3.64 μM. The IC50 values of apigenin, kaempferol, kaempferol 3-O-rhamnoside, and quercetin 3-O-rhamnoside were more than 100 μM. Furthermore, quercetin was found to induce apoptosis in KB and KBv200 cells via the mitochondrial pathway, including a decrease of the reactive oxygen species level, loss of mitochondrial membrane potential, release of cytochrome c, activation of caspase-9 and caspase-3, and cleavage of poly (ADP-ribose) polymerase. The apoptosis induced by quercetin was not related to the regulation of Bcl-2 or Bax in KB and KBv200 cells.
51 citations
TL;DR: The results demonstrate that MCI could induce apoptosis through inhibition of the JAK1/2 and STAT3 signaling pathways.
Abstract: Chrysanthemum indicum L. has been shown to possess antiinflammatory and anticancer activities, but its molecular targets/pathways are not yet fully understood in tumor cells. In the present study, the potential effects of C. indicum on signal transducer and activator of transcription 3 (STAT3) signaling pathway in different tumor cells were examined. The solvent fractions (hexane, CH₂Cl₂, EtOAc, and BuOH,) were obtained from a crude extract (80% EOH extract) of C. indicum. The methylene chloride fraction of C. indicum (MCI) exhibited strong cytotoxic activity as compared with the other fractions and clearly suppressed constitutive STAT3 activation against both DU145 and U266 cells, but not MDA-MB-231 cells. The suppression of constitutive STAT3 activation by MCI is associated with blocking upstream JAK1 and JAK2, but not Src. MCI downregulated the expression of STAT3-regulated gene products; this is correlated with the accumulation of the cell cycle at sub-G1 phase, the induction of caspase-3 activation, and apoptosis. Moreover, the major components of the MCI were bioactive compounds such as sudachitin, hesperetin, chrysoeriol, and acacetin. Sudachitin, chrysoeriol, and acacetin also exerted significantly cytotoxicity, clearly suppressed constitutive STAT3 activation, and induced apoptosis, although hesperetin did not show any significant effect in DU145 cells. Overall, our results demonstrate that MCI could induce apoptosis through inhibition of the JAK1/2 and STAT3 signaling pathways.
48 citations
TL;DR: It is suggested that flavonoids are able to displace warfarin from the surface of HSA and when comparing flavone or flavonol groups to flavanones the latter group seems to be much weaker competitor.
40 citations
TL;DR: In this article, five new secondary metabolites have been isolated from Chrozophora plicata including an acacetin derivative (1), three pyrrole alkaloids plicatanins A-C ( 2 − 4, resp.) and the bilactone plicacanone ( 5 ).
35 citations
TL;DR: Results indicate that the 4′-O-methyl group of flavonoids plays an important role in the induction of melanogenesis by activating its major signal transduction pathway through the upregulation of phospho-CREB in murine B16F10 melanoma cells.
Abstract: Agents to control melanogenesis are in demand for the development of cosmetics to improve pigmentation disorders of skin and hair. In this study, we examined and evaluated the effects of flavonoids on melanogenesis in the melanogenic cells model, murine B16F10 melanoma cells. In the course of this study, we found that incubation of the cells in a medium containing 10 μM of the 4′-O-methylated flavonoids, diosmetin (4′-O-methylluteolin), acacetin (4′-O-methylapigenin) or kaempferide (4′-O-methylkaempferol), increased the melanin contents of the cells 3- to 7-fold higher than the control cells. The concentration-dependence test revealed that 20 μM acacetin showed the highest effect, up to 33-fold higher than the vehicle. On the other hand, the corresponding 4′-OH-type flavonoids, luteolin, apigenin and kaempferol, had a significantly smaller effect. Furthermore, by evaluating the melanogenic proteins, we found that the cells treated with 4′-O-methylated flavonoids showed higher tyrosinase activity, as well as upregulation of tyrosinase expression, preceded by activation of cAMP response element binding protein (CREB) and extracellular signal-regulated kinases types 1 and 2 (ERK1/2). These results indicate that the 4′-O-methyl group of flavonoids plays an important role in the induction of melanogenesis by activating its major signal transduction pathway through the upregulation of phospho-CREB in murine B16F10 melanoma cells.
28 citations
TL;DR: Linarin and its aglycone, acacetin, exhibited sedative and anticonvulsant activities in the present in vivo assays, and it can be considered that linarin is one of the active compounds effective against anxiety, insomnia, and stress, with ac acetin as its active moiety.
Abstract: The flowers or leaves of Chrysanthemum boreale (Compositae) have been traditionally used as herb tea to reduce anxiety, insomnia, and stress. Sedative and anticonvulsant activities were evaluated in mice using pentobarbital-induced sleeping assay and pentylenetetrazole (PTZ)-induced convulsion assay. The flower extract exhibited more potent activities than the extracts of the leaves and stems, and chromatographic isolation yielded the five compounds acacetin, linarin, acacetin 7-O-β-d-glucopyranosyl-(1 → 2)[α-l-rhamnopyranosyl-(1 → 6)]-β-d-glucopyranoside, chlorogenic acid, and 3,5-di-O-caffeoylquinic acid. These compounds were simultaneously analyzed by HPLC, and the method was validated. The contents of linarin, which were shown to be most abundant in C. boreale, were observed in the order of leaf (11.93 mg/g) > flower (8.50 mg/g) > stem (5.60 mg/g). Linarin and its aglycone, acacetin, exhibited sedative and anticonvulsant activities in the present in vivo assays. It can be considered that linarin is one of the active compounds effective against anxiety, insomnia, and stress, with acacetin as its active moiety.
26 citations
TL;DR: Results suggest that acacetin inhibits the expression of E-selectin by regulation of the p38 MAPK signaling pathway and activation of NF-κB.
Abstract: Since E-selectin-mediated adhesion of leukocytes or tumor cells to the vascular endothelium is a key early event in the initiation of inflammatory response and cancer metastasis, E-selectin inhibition is thought to be a good target for therapeutic intervention. Several flavones have been shown to have anti-inflammatory and anticancer properties. In the present study, we investigated the effects of plant flavones on expression of E-selectin in human umbilical vein endothelial cells. Among 11 flavones, acacetin strongly inhibited TNF-α-induced E-selectin expression in HUVECs. Acacetin suppressed the TNF-α-induced phosphorylation of p38 but did not inhibit TNF-α-induced phosphorylations of JNK and ERK. Acacetin also inhibited the activation of NF-κB by stimulation with TNF-α. Furthermore, adhesion of monocytes to TNF-α-treated endothelial cells was inhibited by cotreatment with acacetin. These results suggest that acacetin inhibits the expression of E-selectin by regulation of the p38 MAPK signaling pathway and activation of NF-κB.
26 citations
TL;DR: The results demonstrate the novel information that acacetin may inhibit the closed channels and block the open state of the channels by binding to their P-loop filter helix and S6 domain.
Abstract: The natural flavone acacetin has been demonstrated to inhibit transient outward potassium current (Ito) in human atrial myocytes. However, the molecular determinants of acacetin for blocking Ito are unknown. The present study was designed to investigate the properties and molecular determinants of this compound for blocking hKv4.3 channels (coding Ito) stably expressed in HEK 293 cells using the approaches of whole-cell patch voltage-clamp technique and mutagenesis. It was found that acacetin inhibited hKv4.3 current by binding to both the closed and open channels, and decreased the recovery from inactivation. The blockade of hKv4.3 channels by acacetin was use- and frequency-dependent, and IC50s of acacetin for inhibiting hKv4.3 were 7.9, 6.1, 3.9, and 3.2 µM, respectively, at 0.2, 0.5, 1, and 3.3 Hz. The mutagenesis study revealed that the hKv4.3 mutants T366A and T367A in the P-loop helix, and V392A, I395A and V399A in the S6-segment had a reduced channel blocking efficacy of acacetin (IC50, 44.5 µM for T366A, 25.8 µM for T367A, 17.6 µM for V392A, 16.2 µM for I395A, and 19.1 µM for V399A). These results demonstrate the novel information that acacetin may inhibit the closed channels and block the open state of the channels by binding to their P-loop filter helix and S6 domain. The use- and rate-dependent blocking of hKv4.3 by acacetin is likely beneficial for managing atrial fibrillation.
25 citations
TL;DR: In this chemical study, morolic acid was isolated as the major component (47.54% of the total composition of acetone extract) of Voradendron brachystachyum and 19 known compounds were identified.
19 citations
TL;DR: It was concluded that the therapeutic potential of this plant is due to its antioxidant potential and the antioxidant effect of P. evestita is dueto the presence of these three isolated antioxidant compounds.
Abstract: In the present research work acacetin (1), chrysin (2) and umbelliferone (3) were isolated for the first time from the chloroform fraction of Potentilla evestita. The isolated compounds as well as various solvent fractions of the crude ethanolic extract were assessed for their antioxidant potentials. A significant DPPH free radical scavenging effect was observed in the methanolic and chloroform fractions. The acacetic and chrysin demonstrated significant free radical scavenging activity. Likewise compound 3 showed moderate activity as comparative. It was concluded that the therapeutic potential of this plant is due to its antioxidant potential and the antioxidant effect of P. evestita is due to the presence of these three isolated antioxidant compounds.
Key words: Potentilla evestita, acacetin, chrysin, and umbelliferone, antioxidant activity.
TL;DR: The results show that TPE-based screening assays represent valuable methods to discover new compounds targeting telomeres and that acacetin and chrysin are able to specifically alleviate TPE in human cells.
Abstract: We took advantage of the ability of human telomeres to silence neighboring genes (telomere position effect or TPE) to design a high-throughput screening assay for drugs altering telomeres. We identified, for the first time, that two dietary flavones, acacetin and chrysin, are able to specifically alleviate TPE in human cells. We further investigated their influence on telomere integrity and showed that both drugs drastically deprotect telomeres against DNA damage response. However, telomere deprotection triggered by shelterin dysfunction does not affect TPE, indicating that acacetin and chrysin target several functions of telomeres. These results show that TPE-based screening assays represent valuable methods to discover new compounds targeting telomeres.
TL;DR: It is shown that linarin-mediated inhibition of cell proliferation is associated with suppression of Akt activation and induction of cyclin-dependent kinase inhibitor p27(Kip1) as evidenced by cell cycle analysis and treatment with LY294002, an inhibitor of phosphatidylinositol 3-kinase/Akt pathway.
Abstract: In this study, we report the anti-proliferative effect and molecular mechanism of Chrysanthemum indicum (C. indicum) on A549 human alveolar basal epithelial cells. We also analyzed the changes in C. indicum component profiles due to modifications of predrying process, flower size, and extraction method. Among the varieties of modifications tested, high-temperature heat dry (HTD) of small flower biotype followed by the methanolic extraction resulted in the strongest anti-proliferative activity of C. indicum extract in A549 cells. High-performance liquid chromatography of C. indicum revealed that the levels of acacetin 7-O-rutinoside (linarin) are markedly increased by heat treatment, especially HTD. Finally, we showed that linarin-mediated inhibition of cell proliferation is associated with suppression of Akt activation and induction of cyclin-dependent kinase inhibitor p27(Kip1) as evidenced by cell cycle analysis and treatment with LY294002, an inhibitor of phosphatidylinositol 3-kinase/Akt pathway. Taken together, these findings suggest the need for further development and evaluation of linarin from C. indicum for the treatment and prevention of lung cancer.
TL;DR: The results demonstrate that the multi‐target efficacy of the herbal sample may indicate the potential for the development of more effective and safer drugs that will act as substitutes for existing antibiotics.
Abstract: The Chrysanthemum lavandulifolium extract, which includes chrysoeriol, sudachitin, and acacetin, has excellent antibiotic effects on Escherichia coli O157:H7 (E. coli O157). A notable point is that the antibiotic targets of the herb extract are similar to the targets of commonly used antibiotic drugs, including bacterial cell wall biosynthesis, bacterial protein synthesis, and bacterial DNA replication and repair. In addition, the herbal antibiotic inhibits the etiological factors that contribute to the pathogenic property. The herbal sample was extracted and fractionated and then inoculated through a disk diffusion method to confirm its antibiotic effect against E. coli O157. Total RNA was isolated from the affected bacterial cells, and its expression level was analyzed through a microarray analysis. To confirm the accuracy of the microarray data, a real-time PCR was performed. Three active compounds, chrysoeriol, sudachitin, and acacetin, were identified with a high-performance liquid chromatography-electrospray ionization/mass spectrometry chromatogram, and the disk diffusion study confirmed that chrysoeriol and sudachitin contribute to the antibiotic properties of the herb extract. The results demonstrate that the multi-target efficacy of the herbal sample may indicate the potential for the development of more effective and safer drugs that will act as substitutes for existing antibiotics. Copyright © 2012 John Wiley & Sons, Ltd.
TL;DR: The 70% ethanol crud extract and its successive chloroform, ethyl acetate, and 100% ethanol extracts showed significant anti-inflammatory activity, analgesic effect, antipyretic activity, antioxidant activity, and anti-hyperglycemic activity.
Abstract: Background: Nothing is reported on Amphilophium paniculatum (L.) Kunth. This study aimed at investigation of chemical constituents of the leaves of Amphilophium paniculatum, grown in Egypt, in addition to pharmacological evaluation. Materials and Methods: Isolation of a new compound, along with 5 known flavonoids. Pharmacological activities were carried out on different extracts of A. paniculatum leaves. Results: Identification of a new flavone glycoside, acacetin 8- C -β-D- glucopyranosy l-(1→2)-α-L-rhamnopyranoside (1) in addition to 5 known flavonoids. The 70% ethanol crud extract and its successive chloroform, ethyl acetate, and 100% ethanol extracts showed significant anti-inflammatoryactivity,analgesic effect, antipyretic activity, antioxidant activity, and anti-hyperglycemic activity. Determination of the median lethal dose (LD 50 ) revealed that the different extracts were safe.
Journal Article•
TL;DR: Seventeen compounds were isolated from the 95% ethanolic extract of the root of Ficus hirta and their structures were identified on the basis of physicochemical properties and spectral data analysis.
Abstract: Seventeen compounds were isolated from the 95% ethanolic extract of the root of Ficus hirta Their structures were identified on the basis of physicochemical properties and spectral data analysis The structures were elucidated as cyclomorusin (1), 3-O-[(6-O-E-sinapoyl)-beta-D-glucopyranosyl]-(1 --> 2)-beta-D-glucopyranoside (2), 3,5,4'-trihydroxy-6,7,3'-trimethoxyflavone (3), quercetin (4), tricin (5), acacetin (6), luteolin (7), apigenin (8), (E) -suberenol (9), meranzin hydrate (10), methyl eugenol (11), 3-methoxy-4-hydroxybenzoic acid (12), p-hydroxybenzoic acid (13), methyl chlorogenate (14), emodin (15), alpha-amyrin acetate (16), and beta-sitosterol emodin (17), respectively Compounds 1-6, 9-15 were isolated from this plant for the first time
TL;DR: The results of this study into the phosphorylation of ERK 1/2 and p38 MAPK by flavonoids suggest that the inhibition of p38MAPK phosphorylated may effectively enhance neurite outgrowth.
Abstract: Components from Dendranthema × grandiflorum cv. “Mottenohoka” that promote neurite outgrowth of PC12 cells were identified and the mechanism of neurite outgrowth stimulated by isolated components was studied. Components that promoted the phosphorylation of extracellular signal-regulated kinase 1/2 (ERK 1/2) of PC12 cells were isolated. From various structural analyses, the active components were identified as acacetin and luteolin. The effects of acacetin or luteolin on PC12 cells were evaluated by electro-blotting and immunostaining. Slight neurite outgrowth in PC12 cells was observed within 2 days of culture after stimulation by luteolin or acacetin. However, NGF-stimulation induced remarkable neurite outgrowth in comparison. Neurite outgrowth by luteolin or acacetin was significantly enhanced by pretreatment with SB203580 (a p38MAPK inhibitor). The results of this study into the phosphorylation of ERK 1/2 and p38MAPK by flavonoids suggest that the inhibition of p38MAPK phosphorylation may effectively enhance neurite outgrowth.
Journal Article•
TL;DR: Compounds 1, 4 and 6 are isolated from this plant for the first time, and compounds 2, 3 and 5 are firstly obtained from Hyssopus genus.
Abstract: OBJECTIVE To study the chemical constituents of Hyssopus cuspidatus METHODS Compounds were isolated and purified by extraction and different kinds of column chromatography Their structures were determined on the basis of the physicochemical properties and spectral analysis RESULTS Six compounds were identified as caffeic acid methyl ester (1), luteolin 7-O-alpha-L-rhamnopyranosyl (1 --> 6)-beta-D-glucopyranoside (2), luteolin 7-O-beta-D-glucuronide (3), diosmin (4), acacetin 7-O-alpha-L-rhamnopyranosyl(1 --> 6)-beta-D-glucopyranoside (5) and rosmarinic acid (6) CONCLUSION Compounds 1, 4 and 6 are isolated from this plant for the first time, and compounds 2, 3 and 5 are firstly obtained from Hyssopus genus
TL;DR: In this article, the electrochemical behavior of apigenin and acacetin was studied over a wide pH range using a glassy carbon electrode and the formation of two redox products that are reversibly oxidised was observed.
Patent•
24 Apr 2013
TL;DR: In this article, an application of 5,7-dihydroxy-4'-methoxy flavone preparation extracted from snow lotus in preparation of a medicament for treating ischemic stroke was revealed.
Abstract: The invention discloses an application of 5,7-dihydroxy-4'-methoxy flavone preparation extracted from snow lotus in preparation of a medicament for treating ischemic stroke. By effectively extracting the 5,7-dihydroxy-4'-methoxy flavone preparation from the snow lotus and establishing an ischemia reperfusion model of a mouse, the influence of acacetin on the infarct volume and the neurologic impairment caused by ischemia reperfusion injury of the mouse is observed. The study carried out by establishing an SH-SY5Y cell OGD model, testing the cell viability and the cell apoptosis, and demonstrating the integral level of the acacetin shows that the acacetin has the effect of significantly reducing the infarct volume, improving the neurologic function score, promoting the cell survival and reducing the cell apoptosis, clarifies that the acacetin has a neurologic protection effect on the cerebral ischemia reperfusion injury and proves that the 5,7-dihydroxy-4'-methoxy flavone preparation can be well applied to preparing the medicament for treating ischemic stroke and has wide application value.
01 Jan 2013
TL;DR: In this article, the authors used click chemistry to synthesize ten novel galactoconjugates using copper-mediated 1,3-dipolar cycloaddition reactions of acetylgalactose azides and alkynyl-substituted flavonoids 6~10.
Abstract: Five flavonoids 5,7,3',4'-tetramethoxyflavonol (1), 5,7,3'-tribenzyloxy-4'-methoxy flavonol (2), 5,7,4'-trimethoxyflavonol (3), acacetin (4) and 5,7-dihydroxy-4'-benzyloxyflavone (5) were synthesized from diosmetin or rhoifolin by O-methylation, dehydrogenation, glycoside hydrolysis, O-benzylation and dimethyldioxirane (DMDO) oxidation. Based on “Click chemistry”, ten novel flavonoids galactoconjugates 11~20 were synthesized in good yield using copper-mediated 1,3-dipolar cycloaddition reactions of acetylgalactose azides and alkynyl-substituted flavonoids 6~10. Their biological activities against five human cancer cell lines were evaluated by the standard MTT method. The results showed that 11, 13 and 20 exhibited moderate cytotoxicity against HL-60, SMMC-7721, MCF-7, SW480 and A-549 cancer cell lines.
Journal Article•
TL;DR: Nine compounds were isolated and purified by column chromatographic techniques including macroporous resin, silica gel, ODS, Sephadex LH-20, and preparative reversed-phase HPLC on the basis of MS and NMR spectroscopic data analysis.
Abstract: Nine compounds were isolated and purified by column chromatographic techniques including macroporous resin, silica gel, ODS, Sephadex LH-20, and preparative reversed-phase HPLC. Their structures were elucidated as taxifolin (1), naringenin (2), chalconaringenin (3), acacetin (4), quercetin 3-O-beta-D-galactopyranoside (5), 6-prenylnaringenin (6) xanthohumol (7), desmethylxanthohumol (8), xanthohumol B (9) on the basis of MS and NMR spectroscopic data analysis. Compounds 1-5 were isolated from Humulus lupulus for the first time.
TL;DR: A new compound (A) 3,5,7,3-tetrahydroxy-4-methoxyflavone-3-O-?-L-rhamnopyranosyl-7-O,?-D-xylopyranoyl (12)O-?"-Dglucopyraniumide alongwith with two known compounds Luteolin (B) and Acacetin (C) were isolated from methanolic extracts of the defatted seeds of Albizzia Odoratissima Benth as mentioned in this paper
Abstract: A new compound (A) 3,5,7,3-tetrahydroxy-4-methoxyflavone-3-O-?-L-rhamnopyranosyl-7-O-?-D-xylopyranosyl (12)O-?-D-glucopyranoside alongwith with two known compounds Luteolin (B) and Acacetin (C) were isolated from methanolic extracts of the defatted seeds of Albizzia Odoratissima Benth. The structure of a new compound was elucidated on the basis of extensive spectroscopic analysis, colour reactions and chemical degradations. Compound A exhibited higher radical scavenging activity in the 1,1-diphenyl-2-pycrylhydrazyl (DPPH) assay system.
Journal Article•
TL;DR: The ant i- protozoal activity against a chloroquine -resistant Plasmodium falciparum W2 clone was studied by the pLDH method and Acacetin was isolated from the dichloromethane fraction, this being the first report of the occurrence of this flavone in the Microlicia genus.
Abstract: Microlicia crenulata(DC.) Mart (Melastomataceae) has a very restricted occurrence, being considered endem- ic to the state of Minas Gerais, Brazil. To date, the species has been chemically only for taxonomic purposes. The ant i- protozoal activity against a chloroquine -resistant Plasmodium falciparum W2 clone was studied by the pLDH method. Cytotoxic activity was investigated in vitro against the HepG2 A16.cell line. Antiplasmodial activity was exhibited by the dichloromethane fraction, and no cytotoxicity to the HepG2 A16 cell line was observed. Acacetin was isolated from the dichloromethane fraction, this being the first report of the occurrence of this flavone in the Microlicia genus.
Journal Article•
TL;DR: Acacetin can inhibit the differentiaton of splenic CD4+CD62L+T cells into Th17cells in the protocol of Th17-polarization and inhibit the expressions of IL-17Aprotein,IL- 17A mRNA and ROR-γt mRNA in vitro.
Abstract: Objective To establish a induced and culture protocol for Th17cells in vitro,evaluate the effect of Acacetin on the differentiation and functions of Th17cells and explore the mechanisms involed.Methods Splenic CD4+CD62L+T cells of BALB/c mice were isolated and purified with magnetic bead methods,and were co-cultured with transforming growth factor(TGF)-β、interleukin(IL)-6、IL-23for Th17- polarization.There were five groups with the cultured Th17cells:the normal group with nothing induced factors;the induced group,in which T cells were cultured with the above protocol;Acacetin 1μM group;Acacetin 10μM group;Acacetin 30μM group.The proportion of Thl7 cells was detected with flow cytometry ELISA detected the levels of IL-17A;Reverse transcriptase polymerase chain reaction(RT-PCR)detected the expression of IL-17A mRNA and ROR-γt mRNA. Results Compared with the normal group,the proportion of Th17cells cultured with the protocol were significantly higher(P0.05).Compared with group model,the Th17cells proportion in Acacetin 1μM、 Acacetin 10μM、Acacetin 30μM groups were significantly decreased,there is dose dependent(P0.05).The protein expression of IL-17Awas inhibited by Acacetin and the inhibitory effect was dose-dependent.The expression of ROR-γt and IL-17A mRNA were also inhibited manner by Acacetin(P 0.05). Conclusions Acacetin can inhibit the differentiaton of splenic CD4+CD62L+T cells into Th17cells in the protocol of Th17-polarization and inhibit the expressions of IL-17Aprotein,IL-17A mRNA and ROR-γt mRNA in vitro.The results may be associated with the inhibitive effect of Acacetin on ROR-γt expression.
Journal Article•
TL;DR: Compounds 1-7 and 10 are isolated from this plant for the first time and their structures were elucidated by phyisochemical properties and spectral analysis.
Abstract: OBJECTIVE To study the chemical constituents of Ajuga nipponensis. METHODS The chemical constituents were isolated by repeated silica gel column chromatography and their structures were elucidated by phyisochemical properties and spectral analysis. RESULTS Ten compounds were isolated and identified as:hexadecanoic acid(1), ajuforrestin A(2), beta-sitosterol(3), acacetin(4), apigenin(5), ajugamacrin B(6), ursolic acid(7), beta-ecdysone(8), 8-acetylharpagide(9) and daucosterol(10). CONCLUSION Compounds 1-7 and 10 are isolated from this plant for the first time.
Journal Article•
TL;DR: In this article, the chemical constituents of petroleum ether extract from the Artemisia sacrorum Ledeb were identified by physicochemical properties and spectroscopic analysis, and four compounds were isolated and identified as β-sitosterol, acacetin,7-methoxy-6-hydroxycoumarin,5-hydrox-7,4 ′-dimethoxyflavone.
Abstract: OBJECTIVE To study the chemical constituents of petroleum ether extract from the Artemisia sacrorum LedebMETHODS Chemical constituents were isolated and purified by silica gel column chromatography and their structures were identified by physicochemical properties and spectroscopic analysisRESULTS Four compounds were isolated and identified as β-sitosterol,acacetin,7-methoxy-6-hydroxycoumarin,5-hydroxy-7,4 ′-dimethoxyflavoneCONCLUSION β-sitosterol,acacetin,7-methoxy-6-hydroxycoumarin,5-hydroxy-7,4′-dimethoxyflavone are isolated from Artemisia sacrorum Ledeb
Patent•
01 May 2013
TL;DR: In this article, an application of chrysin and acacetin in restraining telomere functions was presented. But the authors focused on the effect of the two compounds on the telomeres.
Abstract: The invention relates to an application of chrysin and acacetin in restraining telomere functions, and specifically provides an specific application of chrysin and acacetin in preparing drugs taking telomeres as the targets for cancer treatment or anti-aging, wherein the fact that the telomeres are taken as the targets for cancer treatment or anti-aging refers to causing of telomere injury, telomere function loss and genomic instability According to the application, a TPE (telomere position effect) cell model is used for confirming that the two compounds can cause telomere injury, telomere function loss and genomic instability, and defining the value and the mechanism of chrysin and acacetin in cancer and anti-aging treatment because chrysin and acacetin affect the telomere functions; since the telomeres are the important targets for anti-aging and anti-cancer treatment, the invention broadens the application range of chrysin and acacetin in clinical treatment