G. Ciccia

Insecticidal activity against Aedes aegypti larvae of some medicinal South American plants.

The insecticidal activity of 11 extracts from nine South American medicinal plants has been studied using the Aedes aegypti larvicidal assay. Eight of the 11 plant extracts studied showed toxicity against the A. aegypti larvae (LC(50)<500 microg/ml). The dichloromethane extracts of Abuta grandifolia and Minthostachys setosa demonstrated high larvicidal activity, the most active being the dichloromethane extract of A. grandifolia, with an LC(50)=2.6 microg/ml (LC(100)= 8.1 microg/ml), indicating an activity 2-fold higher than beta-asarone, a natural botanical insecticide used as a positive control (LC(100)=16 microg/ml). On the other hand, the dichloromethane extract of M. setosa was quite potent against A. aegypti larvae showing an LC(50)=9.2 microg/ml (LC(100)=25.2 microg/ml). The results obtained suggest that the extracts of A. grandifolia and M. setosa are promising as larvicides against A. aegypti larvae and could be useful in the search for new larvicidal natural compounds.

Cytotoxic and DNA interaction activities of extracts from medicinal plants used in Argentina

Eight crude extracts from seven Argentine plants with cancer-related ethnobotanical uses have been subjected to a bioscreening study to detect cytotoxic activity. The plants studied were: Aristolochia triangularis, Baccharis grisebachii, Bolax gummifera, Eupatorium hecatanthum, Erythrina crista-galli, Pterocaulon polystachium and Salpichroa origanifolia. Crown gall tumour inhibition, DNA interaction and cytotoxicity towards KB cells were assayed using the potato disc, the DNA-methyl green (DNA-MG) and the KB cells cytotoxicity bioassays respectively. The results obtained indicate that A. triangularis (ED50=47 microg/ml), B. gummifera (ED50=32 microg/ml) and E. hecatanthum (ED50=35 microg/ml) contained cytotoxic compounds against KB cells. All of the plants studied inhibited the growth of crown gall tumours, showing correlation between the experimental data and the uses reported for these plants. Moreover, the results obtained for the extracts of E. hecatanthum and P. polystachium indicate the presence of compounds that interact with DNA (48 and 22% of absorbance decrease, respectively). The results obtained suggest that cytotoxicity could play an important role in the activities claimed for the plants under study.

Evaluation of the in vitro antioxidant activity in extracts of Uncaria tomentosa (Willd.) DC.

Different extracts of U. tomentosa were tested in vitro for their antioxidant activity utilizing tert ‐butyl‐hydroperoxide‐initiated chemiluminescence in rat liver homogenates. Methanol fractions of both stem‐bark and roots were capable of exerting antioxidant activity by this technique. The presence of different concentrations of bark and root methanol extracts also prevented TBARS production and free radical‐mediated DNA‐sugar damage.

In vitro antioxidant and cytotoxic activity of extracts of Baccharis coridifolia DC

The in vitro antioxidant and cytotoxic activities in different extracts of Baccharis coridifolia DC. (Compositae) were studied using different bioassays. Antioxidant activity was tested using hydroperoxide-initiated chemiluminescence (CL) in rat liver homogenates. The aqueous extract showed antioxidant activity (IC50 = 141 microg/ml), while the dichloromethane and methanol extracts were prooxidant. Activity in the aqueous extract was confirmed by determination of thiobarbituric acid-reactive substances (TBARS), showing an IC50 = 556 microg/ml. On the other hand, studies on the cytotoxic activity demonstrated a 78% crown gall tumour inhibition and an ED50 = 4. 2 microg/ml in KB cells growth for the dichloromethane extract. A 56% decrease in the initial absorbance of DNA-Methyl Green complex could also be observed at 1000 microg/ml, suggesting the presence of compounds that interact with DNA.

Biological studies of Bolax gummifera, a plant of the Falkland Islands used as a treatment of wounds

Aqueous and dichloromethane extracts of Bolax gummifera (Lam.) Sprengel (Apiaceae), a plant of the Falkland Islands used as a treatment of wounds, were studied in order to support the ethnopharmacological information related to the medicinal use of this plant. The antimicrobial, antioxidant and red blood cells membrane stabilizing activities were analyzed. The antimicrobial bioassay was carried out using the test turbidity method (OD 620 nm), the aqueous extract showing an 82% inhibition of Staphylococcus aureus but no activity against Pseudomonas aeruginosa. The dichloromethane extract inhibited both microorganisms: S. aureus in 94% and P. aeruginosa in 32%. No antioxidant activity could be observed using hydroperoxide-initiated chemiluminescence in rat liver homogenates. Investigations into the membrane stabilizing activity of the extracts were carried out using human red blood cells subjected to hypotonic- and heat-induced lyses. The aqueous extract showed an important stabilizing activity of the red blood cell membrane.

Diarylsemicarbazones: synthesis, antineoplastic activity and topoisomerase I inhibition assay

A series of diarylsemicarbazones was synthesized and tested against human neoplastic cell lines. The more active members have a l-naphthyl ring at the carbamidic nitrogen, and chloro, dimethylamino or nitro group substituents at the benzylidene moiety. None of these showed affinity to DNA. One of the more active compounds was tested as a topoisomerase I inhibitor and showed a potent effect. SAR studies demonstrated linear correlation between lypophilicity and activity on the most sensitive lines and a definite conformational shape for antineoplastic action.

Extracts of Bolivian plants, Copaifera reticulata and Heisteria pallida inhibit in vitro free radical-mediated DNA damage

The presence of different extracts of antiinflammatory plants Copaifera reticulata and Heisteria pallida in a reaction medium containing calf thymus DNA in a free radical generating system protected DNA against oxidative damage in terms of deoxyribose oxidation. The highest antioxidant activity was obtained using the methanol extract of C. reticulata (IC50=3 μg/mL), followed by the aqueous extracts of H. pallida (IC50=257 μg/mL) and C. reticulata (IC50=380 μg/mL). Both dichloromethane extracts and the methanol extract of H. pallida showed a decreased antioxidant activity at higher concentrations. These results suggest that these extracts are capable of suppressing the in vitro oxidative degradation of DNA.

Bioactive Constituents of Conyza Albida

Alkynes and spathulenol were isolated from Conyza albida (Asteraceae); some of the compounds were lethal against Artemia sp. and cytotoxic against KB cells.