Scielo RSS <![CDATA[Revista Brasileira de Farmacognosia]]> vol. 25 num. 1 lang. en <![CDATA[SciELO Logo]]> <![CDATA[The influence of leaf age on methylxanthines, total phenolic content, and free radical scavenging capacity of <em>Ilex paraguariensis</em> aqueous extracts]]> Yerba-mate (Ilex paraguariensis A. St. Hil., Aquifoliaceae) is a South American native species that is widely used for its industrial potential in the preparation of drinks, teas and cosmetics. Its properties are directly related to the presence of its chemical constituents, such as saponins, methylxanthines and phenolic compounds. This study aimed to investigate the influence of leaf age on methylxanthine and total phenolic contents by High Performance Liquid Chromatography and Ultraviolet Spectroscopy, as well as on free radical scavenging capacity, of aqueous extracts of I. paraguariensis leaves. The results showed great variability in all the metabolites measured. Leaf ageing significantly increased the methylxanthine content and total phenolic content of the extracts. Free radical scavenging capacity was also significantly affected (p &lt; 0.05) by leaf age. A positive correlation was observed, between the antioxidant activity and total phenolic content. <![CDATA[Chromenes from leaves of <em>Calea pinnatifida</em> and evaluation of their leishmanicidal activity]]> Calea pinnatifida (R. Br.) Less., Asteraceae, is popularly known as “quebra-tudo”, “cipó-cruz” or “aruca”. This species is used in the folk medicine for the treatment of stomach pain, giardiasis and amoebiasis. The aim of this study was to isolate and identify chromenes from leaves of C. pinnatifida and evaluate their leishmanicidal activity. A fraction from leaves of C. pinnatifida was analyzed for their chemical constituents, resulting in the isolation and characterization of four known chromenes: 6-acetyl-7-hydroxy-2,2-dimethylchromene (1), 6-acetyl-7-methoxy-2,2-dimethylchromene (2), 6-(1-hydroxyethyl)-7-methoxy-2,2-dimethylchromene (3) and 6-(1-ethoxyethyl)-7-methoxy-2,2-dimethylchromene (4). Structure identification of isolated compounds involved analysis of spectral data of 1D and 2D-NMR. The isolated compounds are here reported for the first time in C. pinnatifida, and the chromenes 1 and 3 show a moderate leishmanicidal activity. <![CDATA[Polycarpol in <em>Unonopsis</em>, <em>Bocageopsis</em> and <em>Onychopetalum</em> Amazonian species: chemosystematical implications and antimicrobial evaluation]]> Polycarpol, a recurrent lanostane-type triterpene in Annonaceae family, was confirmed by thin layer chromatography and mass spectrometry analysis in the aerial parts (twigs and trunk barks) of Unonopsis duckei R.E. Fr., U. floribunda Diels, U. rufescens (Baill.) R.E. Fr., U. stipitata Diels, Onychopetalum amazonicum R.E. Fr. and Bocageopsis pleiosperma Maas. Its chemotaxonomic significance was discussed for these three genera, as well for the Annonaceae family. In addition, the antimicrobial activity against several strains of microorganisms was evaluated for the first time for this compound, being observed significant antibacterial activity against Staphylococcus aureus (ATCC 6538), Staphylococcus epidermidis (ATCC 1228) and Escherichia coli (ATCC 10538 and ATCC 10799) with minimal inhibitory concentration values between 25 and 50 μg ml−1. <![CDATA[Evaluation of mutagenicity and metabolism-mediated cytotoxicity of the naphthoquinone 5-methoxy-3,4-dehydroxanthomegnin from <em>Paepalanthus latipes</em>]]> A large number of quinones have been associated with antitumor, antibacterial, antimalarial, and antifungal activities. Results of previous studies of 5-methoxy-3,4-dehydroxanthomegnin, a naphthoquinone isolated from Paepalanthus latipes Silveira, Eriocaulaceae, revealed antitumor, antibacterial, immunomodulatory, and antioxidant activities. In this study, we assessed the mutagenicity and metabolism-mediated cytotoxicity of 5-methoxy-3,4-dehydroxanthomegnin by using the Ames test and a microculture neutral red assay incorporating an S9 fraction (hepatic microsomal fraction and cofactors), respectively. We also evaluated the mutagenic activity in Salmonella typhimurium strains TA100, TA98, TA102, and TA97a, as well as the cytotoxic effect on McCoy cells with and without metabolic activation in both tests. Results indicated that naphthoquinone does not cause mutations by substitution or by addition and deletion of bases in the deoxyribonucleic acid sequence with and without metabolic activation. As previously demonstrated, the in vitro cytotoxicity of 5-methoxy-3,4-dehydroxanthomegnin to McCoy cells showed a significant cytotoxic index (CI50) of 11.9 μg/ml. This index was not altered by addition of the S9 fraction, indicating that the S9 mixture failed to metabolically modify the compound. Our results, allied with more specific biological assays in the future, would contribute to the safe use of 5-methoxy-3,4-dehydroxanthomegnin, compound that has showed in previous studies beneficial properties as a potential anticancer drug. <![CDATA[<em>In vitro</em> and <em>in vivo</em> antifungal activity, liver profile test, and mutagenic activity of five plants used in traditional Mexican medicine]]> Berberis hartwegii Benth., Berberidaceae, Hamelia patens Jacq., Rubiaceae, Dendropanax arboreus (L.) Decne &amp; Planch., Araliaceae, Erythrina herbacea L., Fabaceae, and Zanthoxylum caribaeum Lam., Rutaceae, acetone extracts were selected on the basis of their use in traditional Mexican medicine to treat scabies or skin diseases. Anti-dermatophyte activity in vitro was evaluated using the agar dilution assay, and the therapeutic efficacy of B. hartwegii and Z. caribaeum were tested against experimental tinea pedis. The infected animals were treated intragastrically daily for seven days with 2.5 and 5 mg/kg of acetone extracts. The acetone extract of H. patens exhibited 100% growth inhibition against T. mentagrophytes and E. floccosum at 100.0 and 50.0 µg/ml, respectively, and B. hartwegii inhibited growth of M. canis and T. mentagrophytes at 100.0 µg/ml. Effective treatments with 2.5 mg/kg of Z. caribaeum and B. hartwegii extract were comparable with 1 mg/kg of clotrimazole in mice. Liver profile tests and histological analyses did not exhibit any signs of toxicity and the Ames test indicated that both extracts were safe when evaluated in strains TA98, TA100 and TA102. Our results suggest the potential for the future development of new antifungal drugs from B. hartwegii or Z. caribaeum. <![CDATA[Combined administration of silymarin and vitamin C stalls acetaminophen-mediated hepatic oxidative insults in Wistar rats]]> Oxidative insult by free radicals has been implicated in drug-induced hepatic damage and this has resulted in frequent episodes of liver disorders. Therapeutic efficacy of antioxidants may provide a possible solution to this menace. This study was carried out to investigate the effect of combined administration of silymarin and vitamin C in rescuing acetaminophen-induced hepatotoxicity in rats. Hepatotoxic rats were orally administered with silymarin and vitamin C at 100 and 200 mg/kg body weight, respectively. At the end of the experiment, liver function indices, antioxidant parameters and histological analysis were evaluated. We observed that the significantly increased (p &lt; 0.05) activities of alkaline phosphatase, alanine aminotransferase, aspartate aminotransferase, as well as levels of thiobarbituric acid reactive substances and serum total bilirubin, were markedly reduced following co-administration of silymarin and vitamin C. The compounds also effectively reversed the reduced activities of superoxide dismutase, catalase, glutathione peroxidase, glutathione S-transferase and total protein concentration in the hepatotoxic rats. These findings are indicative of hepatoprotective and antioxidant attributes of the two compounds which are also supported by the histological analysis. The available evidences in this study suggest that the complementary effects of silymarin and vitamin C proved to be capable of ameliorating acetaminophen-mediated hepatic oxidative damage and the probable mechanism is via antioxidative action. <![CDATA[<em>Hyptis pectinata</em> gel prevents alveolar bone resorption in experimental periodontitis in rats]]> Hyptis pectinata (L.) Poit., Lamiaceae, is an aromatic, abundant and broadly used plant species in Sergipe to treat oral and gastrointestinal pain and inflammation. The aim of the present study was to analyze the relation between periodontitis and changes in the corporal mass and alveolar bone structure after induction of experimental periodontal disease in rat treated or not treated with H. pectinata gel at 5% (GS5%) and 10% (GS10%), comparing their effects with doxycycline gel at 10% (D10%, positive control), vehicle gel (negative control) and a group with experimental periodontal disease, but non-treated. The gels were locally applied in the gingival region immediately after the experimental periodontal disease induction by ligature (3×/day, 11 days). Bone destruction was determined through clinical exam, histopathological analysis and cone beam computed tomography of the experimental animals (n = 36). After 11 days of periodontitis induction, all groups that received ligature presented a decrease in the corporal mass, except to the naïve group (without experimental periodontal disease) (p &lt; 0.05). Computed tomography results have shown healthy bone structure in the group I and bone resorption for the test groups. Histopathological analysis confirmed the healthy bone structure for naïve group animals, while the test groups exhibited bone loss in several degrees. In particular, the non-treated group animals had an intense inflammatory process. When the periodontium of the animals treated with GS10% was histopathologically analyzed, insertion periodontium was preserved. The results for these groups were significantly different of the vehicle group (p &lt; 0.05). According to the results, the gel based in the aqueous extract of H. pectinata at 10% can prevent bone loss in experimental periodontal disease similarly to doxycycline 10%. <![CDATA[<em>Aspidosperma subincanum</em> II. Usefulness of uleine and ribonucleic fragments in the treatment of AIDS patients]]> Aids patients were treated during a year with three different food supplements commercially available: para-pau-aspido (Aspidosperma subincanum Mart. ex A. DC., Apocynaceae); 2Leid (nucleic acids and cytokines); and Para Immuno (propolis, pollen and royal jelly). All foods, given either alone or in combination, proved useful to all AIDS patients who received the supplements, be these under tri-therapy (Triomine: stavudine, lamivudine, névirapine) or left unattended. <![CDATA[Anti-inflammatory and antinociceptive activities of non-alkaloids fractions from <em>Aconitum flavum in vivo</em>]]> Aconitum flavum Hand.-Mazz., Ranunculaceae, has been used for the treatment of rheumatism, traumatic injury in folk and clinical medicine, but the alkaloids has high toxicity. This study was designed to investigate the acute toxicity, anti-inflammatory and antinociceptive activities of non-alkaloids fractions from A. flavum in rodents. The anti-inflammatory activity was evaluated by inflammatory models of dimethylbenzene-induced ear vasodilatation and acetic acid-induced capillary permeability enhancement test in mice and carrageenan-induced paw edema in rats whereas the antinociceptive activity was evaluated using acetic acid-induced writhes, hot plate test and formalin test in mice. The result showed that the LD50 value of BtOH and EtOAc fractions could not be determined as no lethality was observed up to 40 g/kg (p.o.) in mice. BtOH fraction significantly decreased the dimethylbenzene-induced ear vasodilatation, carrageenan-induced paw edema and acetic acid-induced capillary permeability. EtOAc fraction only significantly attenuated paw edema and capillary permeability at the dose of 500 mg/kg. In antinociceptive test, BtOH and EtOAc fractions significantly reduced the writhing number evoked by acetic acid injection and the licking time in both phases of the formalin test. Meanwhile BtOH and EtOAc fractions had significant effect on hot plate test after 90 min. Our data indicate that the BtOH and EtOAc fractions of NAF are no toxicity. BtOH and EtOAc fractions not only inhibit inflammatory and peripheral inflammatory pain but also have central antinociceptive effect. <![CDATA[Nanoparticles containing curcuminoids (<em>Curcuma longa</em>): development of topical delivery formulation]]> Solid lipid nanoparticles incorporating Curcuma longa L., Zingiberaceae, curcuminoids were produced by the hot melt emulsion method. A Box–Behnken factorial design was adopted to study the nanoparticles production at different levels of factors such as the percentage of curcuminoids, time of homogenization and surfactant ratio. The optimized nanoparticles were incorporated into hydrogels for stability, drug release and skin permeation tests. The average nanoparticle sizes were 210.4 nm; the zeta potential of −30.40 ± 4.16; the polydispersivity was 0.222 ± 0.125. The average encapsulation efficiency of curcumin and curcuminoids was 52.92 ± 5.41% and 48.39 ± 6.62%, respectively. Solid lipid nanocapsules were obtained with curcumin load varying from 14.2 to 33.6% and total curcuminoids load as high as 47.7%. The topical formulation containing SLN-Curcuminoids showed good spreadability and stability when subjected to mechanical stress test remained with characteristic color, showed no phase separation and no significant change in pH. As a result of slow release, the nanoparticles were able to avoid permeation or penetration in the pig ear epidermis/dermis during 18 h. The topical formulation is stable and can be used in further in vivo studies for the treatment of inflammatory reactions, in special for radiodermitis. <![CDATA[Phytochemicals and antimicrobial potentials of mahogany family]]> Drug resistance to human infectious diseases caused by pathogens lead to premature deaths through out the world. Plants are sources for wide variety of drugs used for treating various diseases. Systematic screening of medicinal plants for the search of new antimicrobial drug candidates that can inhibit the growth of pathogens or kill with no toxicity to host is being continued by many laboratories. Here we review the phytochemical investigations and biological activities of Meliaceae. The mahogany (Meliaceae) is family of timber trees with rich source for limonoids. So far, amongst the different members of Meliaceae, Azadirachta indica and Melia dubia have been identified as the potential plant systems possessing a vast array of biologically active compounds which are chemically diverse and structurally complex. Despite biological activities on different taxa of Meliaceae have been carried out, the information of antibacterial and antifungal activity is a meager with exception to Azadirachta indica. Together we provide new insights of Meliaceae members demonstrating as a potential source as antimicrobial agents using in vitro studies.