Rehabilitative residential treatment in patients with severe mental disorders: personality features associated with short-term outcome.

The aims of this study were to evaluate the outcome of inpatients with severe psychiatric disorders after 6 months of multimodal residential treatment. Ninety-one subjects admitted to residential prolonged treatment at an Italian rehabilitative complex were included in the study. Within 6 months, the program of treatment was effective in reducing symptoms and improving the patients' psychosocial functioning. The study of personality can be useful to "dose" symptomatic (pharmacological and psychotherapeutic) and rehabilitative treatments in the therapy program.

ent-Kaur-16-en-19-oic acid, a KB cells cytotoxic diterpenoid from Elaeoselinum foetidum.

Toxic and cytotoxic activities of the toxic plant Elaeoselinum foetidum (Apiaceae) were evaluated using the brine shrimp toxicity (BST) and KB cell cytotoxicity assays. The active chloroform extract was subjected to a bioactivity-directed fractionation, monitored by the BST assay, that led to the isolation of the diterpenoid ent-kaur-16-en-19-oic acid. This compound was potent against the brine shrimp (LC(50) = 4.8 microg/mL) and KB cells (IC(50) = 1.6 microg/mL).

Investigation of the larvicidal activity of Pothomorphe peltata and isolation of the active constituent.

The insecticidal activity of the leaves of Pothomorphe peltata (Piperaceae) was evaluated on Aedes aegypti larvae. The active methanol extract was subjected to a bioactivity-directed fractionation, monitored by the larvicidal assay, and led to the isolation of a catechol derivative, 4-nerolidylcatechol. This compound was quite potent against Aedes aegypti larvae (LC(50) = 9.1 microg/mL).

Human DNA topoisomerase I poisoning activity of bis-1-aminomethylnaphtalenes. A correlation with their cytotoxic activity.

Symmetrical bis-1-aminmoethylnaphtalenes, a group of compounds that demonstrated cytotoxicity towards human tumor cell lines, showed human topoisomerase I poisoning activity. The compounds tested were: N,N'-bis-1-naphthylmethyl-1,6-hexanediamine (1a), N,N'-bis-1-naphthylmethyl-1,8-octanediamine (1b), N,N'-bis-1-naphthylmethyl-1,12-dodecanediamine (1c), N,N'-bis-1-naphthylmethyl-4,4-bipiperidine (2) and N-(1-naphthylmethyl)-N'-dimethyl-1,3-diaminepropane dichlorhydrate (3). All showed human topoisomerase I inhibition by producing protein-linked DNA breaks. The most active were 1a, 1b, 1c with a percentage stimulation of DNA cleavage of 75, 84 and 70% at 100 micrograms/ml, respectively. Compounds 2 and 3 were moderately active as poisons of topoisomerase I activity, the former showing 58% stimulation of DNA cleavage at 100 micrograms/ml and the latter a 24% stimulation. The correlation observed between topoisomerase I poisoning and in vitro cytotoxic activity suggests that this could be a possible mechanism for the cytotoxicity observed in tumor cell lines.

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.

Bioactive constituents of Conyza albida.

The bioactivity-guided fractionation of an active chloroform extract of Conyza albida led to the isolation of three alkenynes, deca-4,6-diyn-2-(Z)-enoic methyl ester (1), deca-4,6-diyn-2-(Z)-enoic ethyl ester (2) and deca-2,4-diene-4-hydroxy-6-yn-1,4-olide (3), and the terpenoid spathulenol (4), as the active toxic metabolites in the Artemia sp. lethality test. When tested in the KB cell cytotoxicity assay, compounds 1-4 demonstrated IC50 values of 52.2, 38.4, 117.9, and 83.8 microM, respectively. All compounds studied were inactive in the DNA methyl green and DNA strand scission assays, while compounds 3 and 4 showed moderate activity as inhibitors of human topoisomerase I. Compound 2 is reported here for the first time.

Cytotoxic 4-nerolidylcatechol from Pothomorphe peltata inhibits topoisomerase I activity.

Bioactivity-guided fractionation of the leaf methanolic extract of P. peltata (Piperaceae), using the brine shrimp lethality test, led to the isolation of catechol derivative 4-nerolidylcatechol (4-NC). The methanolic extract was active against crown gall tumour in potato discs, showing a 22% crown gall tumour inhibition (SD = 4%), while 4-NC was cytotoxic against KB tumour cells growth (EC50 = 1.3 micrograms/ml). No interaction with DNA could be observed when tested using the methyl green-DNA (MG-DNA) bioassay. An inhibition in the activity of topoisomerase I using agarose gel electrophoresis was detected in the presence of the purified compound (IC50 = 20 micrograms/ml), suggesting that this could be a possible mechanism for the cytotoxicity observed in KB cells.

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.

Inhibition of lipid peroxidation and iron (II)-dependent DNA damage by extracts of Pothomorphe peltata (L). Miq.

Leaves of Pothomorphe peltata (L.) Miq. (Piperaceae) are used locally as anti-inflammatory, antipyretic, hepatoprotective and diuretic infusions and to treat external ulcers and local infections in several parts of the Peruvian, Bolivian and Brazilian Amazon region. The antioxidant activity of different extracts of P. peltata was studied using the hydroperoxide-initiated chemiluminescence assay in liver homogenates, and the methanolic extract was found to have the highest antioxidant activity, with an IC50 = 4 micrograms/ml. Aqueous and dichloromethane extracts did not show antioxidant activity. The extracts were further evaluated using the thiobarbituric acid-reactive substances (TBARS) assay. Finally, an assay of DNA sugar damage induced by Fe (II) salt was used to determine the capacity of the extracts to suppress the oxidative degradation of DNA. All the extracts showed antioxidant activity in the latter two bioassays. The methanolic extract showed the highest activity in reducing oxidative damage to DNA, with an IC50 = 5 micrograms/ml. Since this extract was highly effective in reducing chemiluminescence and DNA damage, and because the latter activity could be due to the presence of compounds that bind to DNA, DNA-binding activity was studied using the DNA-methyl green (DNA-MG) bioassay. A 30% decrease in the initial absorbance of DNA-MG complex was observed in the methanolic extract at 1000 micrograms/ml, suggesting the presence of compounds that bind to genetic material. No DNA-binding activity was observed in the aqueous or dichloromethane extracts.

Inhibition of lipid peroxidation and iron (II)-dependent DNA damage by extracts of Pothomorphe peltata (L.) Miq

Leaves of Pothomorphe peltata (L.) Miq. (Piperaceae) are used locally as anti-inflammatory, antipyretic, hepatoprotective and diuret infusions and to treat external ulcers and local infections in several parts of the Peruvian, Bolivian and Brazilian Amazon region. The antioxidant activity of different extracts of P. peltata was studied using the hydroperoxide-initiated chemiluminescence assay in liver homogenates, and the methanolic extract was found to have the highest antioxidant activity, with an IC50 = 4 mug/ml. Aqueous and dichloromethane extracts did not show antioxidant activity. The extracts were further evaluated using the thiobarbituric acid-reactive substances (TBARS) assay. Finally, an assay of DNA sugar damarge induced by Fe (II) salt was used to determine the capacity of the extracts to suppress the oxidative degradation of DNA. All the extracts showed antioxidant activity in the latter two bioassays. The methanolic extract showed the highest activity in reducing oxidative damage to DNA, with an IC5O = 5 mug/ml. Since this extract was highly effective in reducing chemiluminescence and DNA damage, and because the latter activity could be due to the presence of compounds that bind to DNA, DNA-binding activity was studied using the DNA-methyl green (DNA-MG) bioassay. A 30 per cent decrease in the initial absorbance of DNA-MG complex was observed in the methanolic extract at 1000 mug/ml, suggesting the presence of compounds that bind to genetic material. No DNA-binding activity was observed in the aqueous or dichloromethane extracts.

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.

Studies on the cytotoxicity, antimicrobial and DNA-binding activities of plants used by the Ese'ejas.

Thirty-nine extracts of 13 plants used traditionally as medicinal by the Ese'ejas were studied in order to determine their cytotoxic effect in the brine shrimp. Infusions showed no toxicity. Those plants that tested positive for methanolic and dichloromethane extracts were assayed for DNA-binding activity. Cytotoxicity was not due to the presence of compounds that interact with DNA. Antimicrobial activity of plants used to treat infectious diseases was also performed for the decoctions. These proved to be active against some of the test microrganisms used in the assay.

[Antimicrobial activity and interaction with DNA of medicinal plants from the Peruvian Amazon region]. / Actividad antimicrobiana e interacción con el ADN de plantas medicinales de la Amazonia peruana.

Decoctions of four plants used for the treatment of different infections by indigenous groups of the Peruvian Amazon, i.e. Abuta grandifolia, Cyperus articulatus, Gnaphalium spicatum and Pothomorphe peltata were evaluated for antimicrobial activity by the "stroke method" in agar plates. Tested organisms included Staphylococcus aureus, Escherichia coli, Salmonella gallinarum, Klebsiella pneumoniae, Candida albicans, Pseudomonas aeruginosa and Mycobacterium gordonae. All decoctions showed antimicrobial activity against at least one of the tested organisms. The A. grandifolia and C. articulatis decoctions partially inhibited the growth of P. aeruginosa. S. aureus was completely inhibited by C. articulatus decoction and only partially inhibited by G. spicatum and P. peltata. The A. grandifolia decoction also showed a partial inhibition against M. gordonae, showing a clear correlation between the ethnopharmacological use and the observed activity. Methanolic extracts of plants were analyzed by using the DNA-methyl green bioassay. The methanolic extract of P. peltata (concentration 1000 micrograms/ml) showed a decrease of 30% regarding to the initial absorbance of the DNA-MG complex suggesting the possible interaction with DNA.

Bioactivity of certain medicinal latexes used by the Ese'ejas.

Latexes from Croton erythrochilus, Ficus inspidia and Sapium marmieri used traditionally as medicinal by the Ese'ejas were analyzed for bioactivity. The assays run were: the brine shrimp toxicity microplate bioassay, the wheat rootlet growth inhibition and the DNA-methyl green bioassay. The three latexes showed cytotoxicity to the brine shrimp and concentration-related growth inhibition. No interaction with the DNA-methyl green complex was observed with any of the three latex samples. The field bioassays described has demonstrated to be useful for supporting ethnobotanical information.

Actividad antimicrobiana e interacción con el ADN de plantas medicinales de la Amazonia peruana. / [Antimicrobial activity and interaction with DNA of medicinal plants from the Peruvian Amazon region]

Decoctions of four plants used for the treatment of different infections by indigenous groups of the Peruvian Amazon, i.e. Abuta grandifolia, Cyperus articulatus, Gnaphalium spicatum and Pothomorphe peltata were evaluated for antimicrobial activity by the [quot ]stroke method[quot ] in agar plates. Tested organisms included Staphylococcus aureus, Escherichia coli, Salmonella gallinarum, Klebsiella pneumoniae, Candida albicans, Pseudomonas aeruginosa and Mycobacterium gordonae. All decoctions showed antimicrobial activity against at least one of the tested organisms. The A. grandifolia and C. articulatis decoctions partially inhibited the growth of P. aeruginosa. S. aureus was completely inhibited by C. articulatus decoction and only partially inhibited by G. spicatum and P. peltata. The A. grandifolia decoction also showed a partial inhibition against M. gordonae, showing a clear correlation between the ethnopharmacological use and the observed activity. Methanolic extracts of plants were analyzed by using the DNA-methyl green bioassay. The methanolic extract of P. peltata (concentration 1000 micrograms/ml) showed a decrease of 30

regarding to the initial absorbance of the DNA-MG complex suggesting the possible interaction with DNA.

Actividad antimicrobiana e interacción con el ADN de plantas medicinales de la Amazonia peruana / [Antimicrobial activity and interaction with DNA of medicinal plants from the Peruvian Amazon region]

Decoctions of four plants used for the treatment of different infections by indigenous groups of the Peruvian Amazon, i.e. Abuta grandifolia, Cyperus articulatus, Gnaphalium spicatum and Pothomorphe peltata were evaluated for antimicrobial activity by the [quot ]stroke method[quot ] in agar plates. Tested organisms included Staphylococcus aureus, Escherichia coli, Salmonella gallinarum, Klebsiella pneumoniae, Candida albicans, Pseudomonas aeruginosa and Mycobacterium gordonae. All decoctions showed antimicrobial activity against at least one of the tested organisms. The A. grandifolia and C. articulatis decoctions partially inhibited the growth of P. aeruginosa. S. aureus was completely inhibited by C. articulatus decoction and only partially inhibited by G. spicatum and P. peltata. The A. grandifolia decoction also showed a partial inhibition against M. gordonae, showing a clear correlation between the ethnopharmacological use and the observed activity. Methanolic extracts of plants were analyzed by using the DNA-methyl green bioassay. The methanolic extract of P. peltata (concentration 1000 micrograms/ml) showed a decrease of 30

regarding to the initial absorbance of the DNA-MG complex suggesting the possible interaction with DNA.