Sesquiterpenes, limonoid and coumarin from the wood bark of Guarea guidonia.

Investigation of the wood bark of Guarea guidonia (Meliaceae) led to the isolation of a limonoid (mombasol), a coumarin (scopoletin), and six sesquiterpenes [trans-1(10)-epoxy-4(15)-caryophyllene, 1(10)-epoxy-4,7-humuladiene, viridiflorol, 1(10),4-diepoxy-7-humulene, 3-oxo-10-alloaromadendranol, 1beta-6alpha-dihydroxyeudesm-4(15)ene]. The occurrence of these metabolites in the Guarea genus is reported for the first time. Stigmasterol, sitosterol and its oleate and palmitate esters were also obtained. Some corrections to the previously reported chemical shift assignments of 3-oxo-10-alloaromadendranol ( (13)C-NMR) were made.

Antimitotic action of extracts of Petiveria alliacea on sea urchin egg development.

The hydroethanol extract of the roots of Petiveria alliacea L. (Phytolaccaceae) has been investigated previously as an antitumor agent against mouse Ehrlich ascites. The extract and its methanol, butanol and ether fractions exhibited an antimitotic effect on sea urchin egg development. The aqueous fraction did not produce inhibition of cell cleavage. At the first cleavage the inhibition, at the lowest concentration (10 micrograms/ml), produced by the ether fraction was 42%, whereas the inhibition produced by the total extract and by the other fractions was only 5 to 10% showing that the ether fraction was the most active. Even at higher concentrations the butanol and methanol fractions inhibit the cleavage about 30%. At the first cleavage, the ED50 of the hydroethanol extract and of the ether fraction were 45.02 and 12.40 micrograms/ml, respectively. Furthermore, in the second cleavage, the hydroethanol extract was about twice as potent as the methanol or butanol fractions (ED50 of 22.40, 44.80 and 54.10 micrograms/ml, respectively).

Antimitotic action of extracts of Petiveria alliacea on sea urchin egg development

The hydroethanol extract of the roots of Petiveria alliacea L. (Phytolaccaceae) has been investigated previously as an antitumor agent against mouse Ehrlich ascites. The extract and its methanol, butanol and ether fractions exhibited an antimitotic effect on sea urchin egg development. The aqueous fraction did not produce inhibition of cell cleavage. At the first cleavage the inhibition, at the lowest concentration (10 micrograms/ml), produced by the ether fraction was 42 per cent , whereas the inhibition produced by the total extract and by the other fractions was only 5 to 10 per cent showing that the ether fraction was the most active. Even at higher concentrations the butanol and methanol fractions inhibit the cleavage about 30 per cent . At the first cleavage, the ED50 of the hydroethanol extract and of the ether fraction were 45.02 and 12.40 micrograms/ml, respectively. Furthermore, in the second cleavage, the hydroethanol extract was about twice as potent as the methanol or butanol fractions (ED50 of 22.40, 44.80 and 54.10 micrograms/ml, respectively)

Analgesic activity of a triterpene isolated from Scoparia dulcis L. (Vassourinha).

Analgesic and anti-inflammatory activities of water (WE) and ethanolic (EE) extracts of Scoparia dulcis L. were investigated in rats and mice, and compared to the effects induced by Glutinol, a triterpene isolated by purification of EE. Oral administration (p.o.) of either WE or EE (up to 2 g/kg) did not alter the normal spontaneous activity of mice and rats. The sleeping time induced by sodium pentobarbital (50 mg/kg, i.p.) was prolonged by 2 fold in mice pretreated with 0.5 g/kg EE, p.o. Neither extract altered the tail flick response of mice in immersion test, but previous administration of EE (0.5 g/kg, p.o.) reduced writhings induced by 0.8% acetic acid (0.1 ml/10 g, i.p.) in mice by 47%. EE (0.5 and 1 g/kg, p.o.) inhibited the paw edema induced by carrageenan in rats by respectively 46% and 58% after 2 h, being ineffective on the paw edema induced by dextran. No significant analgesic or anti-edema effects were detected in animals pretreated with WE (1 g/kg, p.o.). Administration of Glutinol (30 mg/kg, p.o.) reduced writhing induced by acetic acid in mice by 40% and the carrageenan induced paw edema in rats by 73%. The results indicate that the analgesic activity of S. dulcis L. may be explained by an anti-inflammatory activity probably related to the triterpene Glutinol.

Antimicrobial activity of kaurenoic acid derivatives substituted on carbon-15.

The antibacterial and antifungic activities of two kaurenic acids, ent kaurenoic acid and cinnamoylgrandifloric acid isolated from a hexane extract of aerial parts of Mikania laevigata, were investigated and compared with the activities of other kaurenic acid derivatives substituted on carbon-15. Only acetylgrandifloric acid (ent-kaur-16-en-15 alpha-acetyloxy-19-oic) and its epimer xylopic acid (ent-kaur-16-en-15 beta-acetyloxy-19-oic) displayed significant antibacterial activity at concentrations greater than or equal to 250 micrograms/ml, the 15 alpha epimer being the most active.

Antimicrobial activity pf kaurenoic acid derivatives substituted on carbon-15

The antibacterial and antifungic activities of two kaurenic acids, ent kaurenoic acid and cinnamoylgrandifloric acid isolated from a hexane extract of aerial parts of Mikania laevigata, were investigated and compared with the activities of other kaurenic acid-derivatives substituted on carbon-15. Only acetylgrandifloric acid (en-kaur-16-en-15 alfa-acetyloxy-19-oic) and its epimer xylopic acid (ent-kaur-16-4n-15 beta-acetyloxy-19-oic) displayed significant antibacterial activity at concentrations >=250 microng/ml., the 15 alfa epimer being the most active