In vitro tests to evaluate potential biological activity in natural substances.

The biological activity of polysaccharides from the mycelia of 40 Basidiomycetes was studied using an uncommon toxicity test technique, the planaria bioassay, and the better known potato disk bioassay. The results showed the utility of this duo of 'in vitro' tests as a preliminary screening of the toxicity of substances that are present in aqueous fungal extracts.

Experimental studies on the toxicity of some compounds isolated from Ferula communis in the rat.

The antithrombinic activity of some naturally occurring omega-oxygenated derivatives of ferulenol and ferprenin has been tested. On the basis of these results, both the type of the oxygenated function and the stereochemistry of the terminal double bond seem important for the biological activity.

Experimental studies on the toxicity of Ferula communis in the rat.

The study of two chemically characterized varieties of Ferula communis showed that only plants containing prenylated coumarins are toxic. The contrasting data on the toxicity of Ferula communis most probably raised from the use of chemically uncharacterized specimens. Among the constituents of the toxic variety, both ferulenol, a 4-hydroxycoumarin derivative, and ferprenin, a pyrane (3,2-c) coumarin derivative, affected blood clotting. No hepatotoxicity was elicited by these two compounds.

GLC-ECD determination of 1-(2-hydroxyethyl)-3-hydroxy-7-chloro-1,3-dihydro-5-(O-fluorophenyl)-2H-1,4-benzodiazepin-2-one (SAS 643) in plasma and urine and identification of its main biotransformation products.

A method using gas-liquid chromatography-electron-capture detection method is described for rapid, accurate determination of SAS 643 in plasma and urine. The drug is extracted from biological fluid with benzene and converted to the O, O'-bistrimethylsilyl derivative with bis(trimethylsilyl) trifluoroacetamide. The glucuronide form of the drug is extracted after hydrolysis with beta-glucuronidase. Nimetazepam is used as internal standard. Moreover, some metabolites such as glucuronide and the N-1-dealkylated and N-1-yl-acetic products are identified. All compounds were confirmed by thin-layer chromatography, mass spectroscopy, and gas-liquid chromatography-mass spectroscopy by comparison with reference products.

[Synthesis of analogues of acetohydroxam lacetic acid with phytotoxic activity]. / Sintesi di analoghi dell'acido acetidrossamoilacetico e loro attivitá fitotossica

Syntheses, spectroscopic data and phytotoxic activities of some N-acyl-O-alkylhydroxylamines, similar in structure to the natural compoud, methyl acetohydroxamyl acetate, are reported. Many of synthesized compounds show strong growth-inhibiting activity on both roots and coleoptiles of Triticum vulgare seedlings.