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At least 847 records · Page 47Linked to original sources
PubMed1991

Differential efficacy of flavone acetic against liver versus lung metastases in a human tumour xenograft.

A human ovarian carcinoma, IGROV-1, was xenografted into different sites (i.p., s.c., i.v., and intrasplenically) in nude athymic female mice to investigate the pattern of antitumour efficacy of FAA and compare it to that of doxorubicin and cisplatin, two established cytotoxic drugs. Ascitic and lung-growing tumours totally failed to respond to FAA, whereas s.c. and liver-growing tumours were significantly growth inhibited. This pattern of activity differs from that achieved by the two conventional cytotoxic drugs, which were active against the IGROV-1 tumour growing in all of the tested sites. These studies indicate that cytotoxicity is not the major determinant of FAA antitumour efficacy even against human tumour xenografts. Moreover, the dramatic difference between the sensitivity of lung and liver tumour colonies demonstrates the great importance of the site of tumour growth for FAA efficacy.

Animals↗
PubMed1993

Flavone acetic acid (FAA) with recombinant interleukin-2 (rIL-2) in advanced malignant melanoma: I. Clinical and vascular studies.

A trial of FAA and rIL-2 has been performed both to study the clinical efficacy of this combination and to determine whether they cause haemorrhagic necrosis by acting upon tumour vasculature. FAA and rIL-2 were given to 23 patients with progressing metastatic melanoma. FAA 4.8 gm m-2 was given as a 1 h infusion without urine alkalinisation on days 1, 8 and 15. rIL-2 (6-18 x 10(6) IU/m2/day) was given as a continuous infusion days 8-12 and 15-19 (nine patients) or days 8-12 only (14 patients). Treatment was repeated after 2 weeks unless there was disease progression. Of the 21 assessable patients there have been one complete (skin and liver) and two partial responses (skin and liver, skin and nodes) lasting 20 + 17 + and 15 months, overall response rate 14%. Unexpectedly severe hypotension after the third FAA, when given 2-4 days after RIL-2, was the major toxicity (8/15 grade 3 or 4). No alteration in coagulation parameters were seen during therapy of the first ten patients. No increase in tumour necrosis was seen in any of the 15 biopsies taken from ten patients after therapy. This suggests that FAA does not have similar vascular effects in human as it does in murine tumours.

Adult↗
PubMed2000

Interaction of flavones from the roots of Scutellaria baicalensis with the benzodiazepine site.

A radioreceptor binding assay was used to guide the isolation of four chemical constituents in the organic solvent extracts of Scutellaria baicalensis Georgi capable of binding to the benzodiazepine site (BZD-S) of the GABAA receptor: wogonin (Ki = 2.03 +/- 0.24 microM), baicalin (Ki = 77.10 +/- 4.79 microM), baicalein (Ki = 5.69 +/- 0.95 microM), and scutellarein (Ki = 12.00 +/- 1.27 microM). All four compounds contain the flavonoid phenylbenzopyrone nucleus. Based on BZD-S binding, the order of affinity among these four compounds was wogonin > baicalein > scutellarein > baicalin.

Benzodiazepines↗
PubMed2005

Synthesis and biological activity of some new flavone derivatives.

In this study, a new series of 2-(4-[substituted benzylamino-methyl)-phenyl]-4H-benzopyrane-4-one (IVa-e) and N-substituted benzyl-N-[4-(4-oxo-4H-benzopyrane-2-yl)benzyl]-3-phenyl-acrylamide (Va-e) derivatives was synthesized and the results of their biological activity are reported. The synthesized compounds were tested for their in vitro antifungal and antibacterial activities. Compound IVa showed the best antifungal activity compared with miconazole (CAS 22916-47-8). Compound IVe indicated the same antibacterial activity compared with the control drug ampicillin (CAS 69-53-4).

Anti-Infective Agents↗
PubMed2000

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

A new series of 4'-flavonyl-2,4-thiazolidinedione, 2,4-imidazolidinedione and 2-thiohydantoin derivatives (1-10) were synthesized. Their chemical structures have been elucidated by IR, 1H-NMR, mass spectra and elementary analysis. The synthesized compounds were tested for their insulinotropic effects in INS-1 cells. Inhibitory effects were observed for compounds 1, 2, 6 and 7.

Cells, Cultured↗