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At least 865 records · Page 48Linked to original sources
PubMed2000

Synthesis and hypoglycemic activity of some new flavone derivatives. 3rd communication: 3'-flavonyl-2,4-thiazolidinediones.

A new series of 3'-flavonyl-2,4-thiazolidinedione, 2,4-imidazolidinedione and 2-thiohydantoin derivatives (1-10) were synthesized and their chemical structures have been elucidated by various spectral data. The prepared compounds were tested for their insulinotropic effects in INS-1 cells. Inhibitory effects were observed for compounds 1 and 2. In contrast compounds 4, 7 and 8 were able to increase insulin release compared with glibenclamide.

Animals↗
PubMed2001

Artelastocarpin and carpelastofuran, two new flavones, and cytotoxicities of prenyl flavonoids from Artocarpus elasticus against three cancer cell lines.

Further study of one of the fractions from the wood of Artocarpus elasticus furnished two new prenylated flavonoids artelastocarpin and carpelastofuran as well as ethyl 2,4-dihydroxybenzoate. The two flavonoids and the prenylated flavonoids artelastin, artelastochromene, artelasticin, artocarpesin, and cyclocommunin isolated earlier from this species were tested for cytotoxicity in vitro against three human cell lines. All seven flavonoids were active, the cytotoxic effect varying from strong to moderate and with artelastin showing the most potent activity.

Antineoplastic Agents, Phytogenic↗
PubMed2003

Evidence for estrogen receptor beta-selective activity of Vitex agnus-castus and isolated flavones.

Recent cell culture experiments indicated that extracts of Vitex agnus-castus (VAC) may contain yet unidentified phytoestrogens. Estrogenic actions are mediated via estrogen receptors (ER). To investigate whether VAC compounds bind to the currently known isoforms ERalpha or ERss, ligand binding assays (LBA) were performed. Subtype specific ER-LBA revealed a binding of VAC to ERss only. To isolate the ERss-selective compounds, the extract was fractionated by bio-guidance. The flavonoid apigenin was isolated and identified as the most active ERss-selective phytoestrogen in VAC. Other isolated compounds were vitexin and penduletin. These data demonstrate that the phytoestrogens in VAC are ERss-selective.

Apigenin↗
PubMed1996

Analgesic and antipyretic activities of an aqueous extract and of the flavone linarin of Buddleia cordata.

The dried aqueous extract of leaves of Buddleia cordata (loganiaceae) and its main flavonoid glycoside, linarin, have been evaluated for analgesic and antipyretic effects in mice and rats, respectively. Both the extract and linarin exerted significant and dose-dependent analgesic and antipyretic activities, the first being obtained against a chemical stimulus (writhing a test in mice) and the second being obtained by a pyretogenic stimulus (yeast-induced hyperthermia test). Furthermore, the response of the animals in the hot plate test was modified by linarin and an aqueous extract. These activities were similar to that showed by morphine sulfate (MS) and they were inhibited by naxolone pretreatment, a specific morphinic antagonist compound. These findings lead to the conclusion that the aqueous extract and linarin exert central analgesic properties. On the other hand, linarin was shown to be responsible for the antipyretic activity of this species.

Analgesics↗
PubMed1991

Induction of hypoxia in the KHT sarcoma by tumour necrosis factor and flavone acetic acid.

The interaction of FAA or TNF with radiation was studied in the murine KHT sarcoma. When used alone both agents showed a dose- and time-dependent toxicity towards the tumour cells and significantly reduced tumour blood flow within 1 h of treatment. When used in combination with radiation, both TNF and FAA caused an increase in the fraction of hypoxic cells in the KHT tumour. This was assessed by an in vivo/in vitro clonogenic assay and by a comparison with the radioprotection provided by clamping tumours prior to and during irradiation. When TNF was given at a dose of 2.5 X 10(5) U/kg an increase in tumour hypoxia was seen after 30 min. Close to 100% radiobiological hypoxia was reached by 1 h after treatment, lasting for up to 16 h. Doses of TNF below 0.25 X 10(5) U/kg did not induce levels of hypoxia comparable to clamping when administered 3 h prior to irradiation. Similarly, FAA produced a rapid increase in tumour hypoxia: a dose of 200 mg/kg induced close to 100% radiobiological hypoxia when give 1 h prior to irradiation. Complete tumour hypoxia was still apparent 18 h after treatment with FAA. Administered doses of FAA below 100 mg/kg did not produce close to 100% radiobiological hypoxia when administered 3 h prior to irradiation.

Animals↗
PubMedDate not supplied

Interactions of the monomeric and dimeric flavones apigenin and amentoflavone with the plasma membrane of L929 cells; a fluorescence study.

Flavonoids are ubiquitous polyphenolic compounds, found in vascular plants, which are endowed with a large variety of biological effects. Some of these effects have been assumed to result from interactions with the cell plasma membrane. In order to investigate the nature of these interactions a fluorescence study was performed with two flavonoids, currently used in one of the laboratories: apigenin and its homologous dimer amentoflavone. After preliminary assays with DPH in several types of phospholipid liposomes, the effects of these flavonoids on the membrane of mouse L929 fibroblasts were compared, using the non-permeant probe TMA-DPH. Amentoflavone, unlike apigenin, induced a static quenching effect, which denoted an important, but reversible, association of the molecule with the plasma membrane. In addition, amentoflavone treatment induced a dose-dependent increase in TMA-DPH fluorescence anisotropy, which could be interpreted as an increase in membrane lipidic order. For apigenin, the effect was much less important. Moreover, exploiting the capacity of TMA-DPH to label endocytic compartments, it was shown that, after association with the membrane, amentoflavone is not internalized into the cell. Possible correlations of these membrane effects with other biological properties are discussed.

Animals↗
PubMed1991

Structure of the flavone hymenoxin.

2-(3,4-Dimethoxyphenyl)-5,7-dihydroxy-6,8-dimethoxy-4H-chromen-4-o ne, C19H18O8, Mr = 374.38, monoclinic, P2(1)/n, a = 9.026(4), b = 15.054(6), c = 12.829(6) A, beta = 100.98(4) degrees, V = 1711(1) A3, Z = 4, Dx = 1.450 g cm-3, lambda (Mo K alpha) = 0.71073 A, mu = 1.07 cm-1, F(000) = 784, T = 295 K, R = 0.0778 for 2280 independent reflections. The nearly planar AB ring system (0.04 A r.m.s.d.), O(1) to C(10), and the planar C ring (0.001 A r.m.s.d.) are almost coplanar with an interplanar angle of only 4.4(4) degrees. The methyl groups at C(6) and C(8) are rotated out of the molecular plane on opposite sides with torsion angles C(5)C(6)O(6)C(11) = -94.5(4) and C(7)C(8)O(8)C(12) = 109.0(4) degrees. The methyl groups of ring C are coplanar with the ring, C(3')C(4')O(4')"(13) = 0.2(5) and C(6')C(5')O(5')C(14) = 1.3(5) degrees. The carbonyl group forms an intramolecular hydrogen bond with O(5), O(5)...O(4) = 2.612(5), H(5O)...O(4) = 1.85(4) A, O(5)-H(5O)...O(4) = 151.9(8) degrees, and an intermolecular hydrogen bond with O(7) of an adjacent molecule, O(7)...O(4) (-0.5 + x, -0.5 - y, 0.5 + z) = 2.689(5), H(7O)...O(4) = 1.92(4) A, and O(7)-H(7O)...O(4) = 163.2(8) degrees.

Flavonoids↗