Five new isoprenylated flavones, artochamins A-E (1-5), together with eight known flavones (6-13), were isolated from the roots of Artocarpus chama. All structures were elucidated by spectroscopic methods. Artonin E (12) showed strong cytotoxicity against 1A9 (ovarian), significant activity against MCF-7 (breast adenocarcinoma), and moderate activity against HCT-8 (ileocecal) and MDA-MB-231 (breast adenocarcinoma) tumor cell lines. Artochamin C (3) was more potent against MCF-7, 1A9, HCT-8, and SK-MEL-2 (melanoma) than A549 (lung carcinoma), KB (epidermoid carcinoma of the nasopharynx), and its drug-resistant (KB-VIN) variant. Artocarpin (6) displayed weak but relatively broad inhibitory effects compared with 3 and 12.
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.
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