To identify potential substrates for the debrisoquin and mephenytoin hydroxylation polymorphisms, we performed in vitro inhibition studies with human liver microsomes and the respective prototype substrates in the absence and presence of several anticancer drugs. (+)-Bufuralol 1'-hydroxylation (as the prototype reaction for the debrisoquin polymorphism) was tested at 5 microM substrate concentr...

BACKGROUND Glycosmis is a genus of evergreen glabrous shrub and distributed all over India. It possesses various medicinal properties and is used in indigenous medicine for cough, rheumatism, anemia, and jaundice. Glycosmis arborea is a rich source of alkaloids, terpenoids, coumarins, as well as flavonoids. RESULTS The chemical investigation of methanol fraction of the leaves of G. arborea le...

The chemical components and biological activity of Camellia mistletoe, Korthalsella japonica (Loranthaceae) are relatively unknown compared to other mistletoe species. Therefore, we investigated the phytochemical properties and biological activity of this parasitic plant to provide essential preliminary scientific evidence to support and encourage its further pharmaceutical research and develop...

Two new chalcones, artocarpusins A and B (1 and 2), one new flavone, artocarpusin C (3), one new 2-arylbenzofuran derivative, artocarstilene A (4), and 15 flavonoids were isolated from the twigs of Artocarpus heterophyllus. Their structures were established on the basis of extensive spectroscopic analysis. Compounds 9 and 16 showed moderate inhibitory activity on the proliferation of the PC-3 a...

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 th...

The combined effects of flavone acetic acid (FAA), a synthetic flavonoid, and hyperthermia on B16 melanoma cells were investigated. In vitro, FAA alone at concentrations below 100 micrograms/ml was not cytotoxic with a 60-min exposure at 37 degrees C. Hyperthermia at 43 degrees C for 60 min enhanced the cytotoxicity of FAA only at concentrations over 100 micrograms/ml. Inhibition of the growth ...

We have conducted a Phase I and pharmacological study of flavone acetic acid, one of a series of novel flavonoids. The drug was administered i.v. weekly for 4 weeks, with a 2-week rest and then repeated. Flavone acetic acid was given initially in a 1-h infusion, but at the 3900-mg/m2 dose level, the infusion time was lengthened to 3 h. A total of 31 patients were treated with 9 different dose l...

Morphological, chemical and genetic differences of 12 tree basil (Ocimum gratissimum L.) accessions were studied to determine whether volatile oils and flavonoids can be used as taxonomical markers and to examine the relationship between RAPDs to these chemical markers. Eugenol, thymol, and geraniol were the major volatile oil constituents found in Ocimum gratissimum. Xantomicrol and cirsimarit...