Adriana Rolim Campos

Investigations on the antinociceptive activity of crude extracts from Croton cajucara leaves in mice

The crude leaf extracts of Croton cajucara Benth. were studied for their antinociceptive property in chemical and thermal models of nociception in mice. All the tested extracts (hexanic, chloroformic and methanolic), at oral doses of 100 and 200 mg/kg demonstrated significant inhibition of acetic acid-induced writhing and the second phase response of formalin, but did not manifest a significant effect in hot-plate test.

Antioestrogenic effect of trans‐dehydrocrotonin, a nor‐clerodane diterpene from Croton cajucara Benth. in rats

This study examined trans‐dehydrocrotonin (t‐DCTN), a nor‐clerodane diterpene isolated from the Brazilian medicinal plant Croton cajucara Benth., for a possible antioestrogenic activity using immature rats as a model system for bioassay of oestrogen, and for an antiimplantation effect in regularly cycling rats of proven fertility. In the antioestrogen test, t‐DCTN (25 and 50 mg/kg) effectively prevented oestrogen‐induced increases of uterine wet weights. In addition, the vaginal openings provoked by oestrogen were completely prevented by t‐DCTN. However, blastocyst‐implantation was only insignificantly affected in t‐DCTN pretreated animals. These results suggest that t‐DCTN may be an antioestrogen and warrants further studies with regard to its mechanism of action. Copyright

Chemical composition, antibacterial and antifungal activities of essential oil from Cordia verbenacea DC leaves.

Background: Cordia verbenacea is a Brazilian coastal shrub popularly known as “erva baleeira”. The essential oil from fresh leaves was obtained by hydrodistillation and analyzed by CG/MS. The main components were identified as β-caryophyllene (25.4%), bicyclogermacrene (11.3%), δ-cadinene (9.%) and α-pinene (9.5%). In this study, the antimicrobial activity of Cordia verbenacea was evaluated. Materials and Methods: The minimal inhibitory concentration (MIC) of the essential oil was obtained using the broth microdilution assay (from 512 to 8 μg/ml). Results: The results showed that the essential oil presented fungistatic activity against Candida albicans and Candida krusei and antibacterial activity against Gram-positive strains (Staphylococcus aureus and Bacillus cereus) and against multiresistant Gram-negative (Escherichia coli 27), in all tests the MIC was 64 μg/ml. When the essential oil was associated to aminoglycosides (subinhibitory concentrations, MIC/8), a synergic and antagonic activity was verified. The synergic effect was observed to the amikacin association (MIC reduction from 256 mlto 64 μg/ml) in all strains tested. Conclusion: The essential oil of Cordia verbenacea influences the activity of antibiotics and may be used as an adjuvant in antibiotic therapy against respiratory tract bacterial pathogens.

Study of the Interference between Plectranthus Species Essential Oils from Brazil and Aminoglycosides

Plectranthus is one of the most representative genera of Lamiaceae family. In this study, the essential oils from Plectranthus amboinicus, Plectranthus ornatus, and Plectranthus barbatus were investigated for their chemical composition and antimicrobial and modulatory activities. The major components found were carvacrol (54.4%—P. amboinicus) and eugenol (22.9%—P. ornatus e 25.1%—P. barbatus). In vitro antimicrobial activity was conducted against Escherichia coli, Proteus vulgaris, Bacillus cereus, Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus aureus (multiresistant) using microdilution method. The results of bioassay showed that all strains were sensitive to the oils, except P. aeruginosa that was resistant to P. amboinicus and P. ornatus. A synergistic effect of all essential oils combined with the aminoglycosides was demonstrated. These results show that P. amboinicus, P. ornatus, and P. barbatus inhibit the growth of pathogenic microorganism, and besides this they present antibiotic modifying activity, providing a new perspective against the problem of bacterial resistance to antibiotics.

Attenuation of visceral nociception by α-bisabolol in mice: investigation of mechanisms.

Background We previously described the visceral antinociceptive property of α-bisabolol (BISA) in mouse models of visceral nociception induced by cyclophosphamide and mustard oil (MO). This study examined the effect of BISA in mouse models of visceral nociception induced by acetic acid, capsaicin, formalin, and the contribution of the nitric oxide system, α2, KATP, 5-HT3 and TRPV1 receptors to the effect of BISA on MO-evoked nociceptive behaviors. Mice were pretreated orally with BISA (50, 100 and 200 mg/kg) or vehicle, and the pain-related behavioral responses to intraperitoneal administration of acetic acid or intracolonic injection of MO were analyzed. Results BISA significantly suppressed the nociceptive behaviors in a dose-unrelated manner. The antinociceptive effect of BISA (50 mg/kg) was show to be glibenclamide resistant, but it was not blocked by pretreatment with the other antagonists tested. In the open-field test that detects sedative or motor abnormality, mice received 50 mg/kg BISA did not show any per se influence in ambulation frequency. Conclusions However, their precise antinociceptive mechanisms of action have not been determined.

Chemical composition and synergistic interaction between aminoglycosides antibiotics and essential oil of Lantana montevidensis Briq.

The chemical composition of the essential oil from Lantana montevidensis Briq. and its antibiotic resistance modifying activity were investigated by gas chromatography/mass spectrometry (GC/MS) and microdilution assay, respectively. β-Caryophyllene (31.50%), germacrene D (27.50%) and bicyclogermacrene (13.93%) were the main constituents. The essential oil was examined for antibiotic activity alone in association with aminoglycosides against Escherichia coli Ec27 and Staphylococcus aureus Sa358. The results showed antibacterial activities of the oil and synergistic effects combined with aminoglycosides. The most expressive effect was the potentiating of amikacin on E. coli with minimal inhibitory concentration decrease (512–5 µg mL−1). The data obtained are indicative of the antibacterial activity of the essential oil of L. montevidensis and its potential in modifying the resistance of aminoglycosides analysed.

Relaxant effects of an alkaloid-rich fraction from Aspidosperma ulei root bark on isolated rabbit corpus cavernosum

We described earlier that an alkaloid-rich fraction (F3–5) from Aspidosperma ulei (Markgr) induces penile erection-like behavioral responses in mice. This study verified a possible relaxant effect of this fraction on isolated rabbit corpus cavernosum (RbCC) strips precontracted by phenylephrine (1 μM) or K+ 60 mM. F3–5 (1–300 μg ml−1) relaxed the RbCC strips in a concentration-dependent and reversible manner. The relaxant effect of F3–5 (100 μg ml−1) on phenylephrine contraction was unaffected in the presence of atropine, N-ω-nitro-L-arginine methyl ester or 1H-[1,2,4]oxadiazole[4,3-a] quinoxalin-1-one and by preincubation with tetrodotoxin, glibenclamide, apamine and charybdotoxin suggesting that mechanisms other than cholinergic, nitrergic, sGC activation or potassium channel opening are probably involved. However, the phasic component of the contraction induced by K+ 60 mM as well as the maximal contraction elicited by increasing external Ca2+ concentrations in depolarized corpora cavernosa was inhibited by F3–5. We conclude that F3–5 relaxes the RbCC smooth muscle, at least in part, through a blockade of calcium influx or its function.

Effects of acute and repeated dose administration of caffeine and pentoxifylline on diazepam-induced mouse behavior in the hole-board test

Rationale: The behavioral effects of methyl xanthines and their interactions with benzodiazepines have not been clearly established in animal models of anxiety. Objective: The present study extended the previous studies to determine the effects of acute and repeated administration of caffeine, a non-specific phosphodiesterase (PDE) inhibitor and pentoxyfylline, a specific type-4 phosphodiesterase (PDE4) inhibitor on (1) baseline anxiety-like behavior and (2) the response to an acute challenge with diazepam on anxiety-like behavior in the hole-board test. Methods: Mice were observed for the number of head-dips they made into the holes of the hole-board apparatus during a 5-min period, starting 30 min after acute (20 mg/kg) and repeated oral dose (20 mg/kg, twice a day for 4 days) administration of caffeine and pentoxifylline. In separate experiments, the response to an acute challenge with graded doses of diazepam (0.375–3 mg/kg, SC) was observed in naive mice or mice on acute and repeated dose regimen with methyl xanthines. Results: Mice on acute but not after repeated dose regimen demonstrated a significantly increased number of hole-dips, indicating an anxiolytic-like effect of methylxanthines. Diazepam at the lower doses (0.375 and 0.75 mg/kg) but not at the highest doses (1.5 and 3 mg/kg) examined produced a significant anxiolytic-like effect. After an acute dose exposure of mice to caffeine and pentoxifylline, a rightward shift in the dose-response curve of diazepam was observed and particularly at 1.5 mg/kg dose, the net effect of diazepam was significantly enhanced which was, however, impaired upon repeated administration, more so with caffeine than with pentoxifylline. Conclusions: It is concluded that the xanthine drugs exert anxiolytic-like activity similar to diazepam in the hole-board test. In addition, they seem to modulate the anxiolytic effects of diazepam after both acute and repeated administration, probably as a result of an endogenous adenosinergic mechanism which may have therapeutic significance.

Topical Antinociceptive Effect of Vanillosmopsis arborea Baker on Acute Corneal Pain in Mice

This study aimed to assess the possible topical antinociceptive activity of Vanillosmopsis arborea Baker essential oil (EOVA) and to clarify the underlying mechanism, using the acute model of chemical (eye wiping) nociception in mice. EOVA (25 to 200 mg/kg; p.o. and topical) evidenced significant antinociception against chemogenic pain in the test model of formalin-induced neuroinflammatory pain. Local application of 5 M NaCl solution on the corneal surface of the eye produced a significant nociceptive behavior, characterized by eye wiping. The number of eye wipes was counted during the first 30 s. EOVA (25, 50, 100, and 200 mg/kg; p.o. and topical) significantly decreased the number of eye wipes. Naloxone, yohimbine, L-NAME, theophylline, glibenclamide, and ruthenium red had no effect on the antinociceptive effect of EOVA. However, ondansetron, p-chlorophenylalanine methyl ester (PCPA), capsazepine, prazosin, and atropine prevented the antinociception induced by EOVA. These results indicate the topical antinociceptive effect of EOVA and showed that 5-HT, α1, TRPV1, and central muscarinic receptors might be involved in the antinociceptive effect of EOVA in the acute corneal model of pain in mice.

Evaluation of the antifungal activity and modulation between Cajanus cajan (L.) Millsp. leaves and roots ethanolic extracts and conventional antifungals.

Background: The use and investigation of natural products with antimicrobial activity from vegeral source have been reported by several researchers. Cajanus cajan (Fabaceae) is a multiple use specie mainly as human food. In popular medicine, diverse parts of the plant are used as sedative and to treat cough, hepatitis, and diabetes. Materials and Methods: This study shows the characterization of secondary metabolites present in ehtanolic extracts from leaves and roots of Cajanus cajan by phytochemical prospection. The evaluation of the antifungal activity was performed by the microdilution method, and from the subinhibitory concentrations (MIC 1/8) the modulatory activity of antifungical (fluconazole and ketoconazole) was analyzed by the direct contact assay against C. albicans ATCC40006, Candida krusei ATCC 6538 and Candida tropicalis ATCC 40042. Results: The results showed the presence of tannins, flavonoids, and alkaloids in both extracts as the clinically relevant antifungal activity. The modulatory potential is presented by the antifungal tested against yeasts. Conclusion: The extracts studied here have demonstrated to be a new therapeutic source to treat these microorganism-associated diseases.