Phyto-cytogenotoxic potential assessment of two medicinal plants: Davilla nitida (Vahl) Kubitzki and Davilla elliptica (A. St.-Hill) (Dilleniaceae).

Humans have been using plants in the treatment of various diseases for millennia. Currently, even with allopathic medicines available, numerous populations globally still use plants for therapeutic purposes. Although plants constitute a safer alternative compared to synthetic agents, it is well established that medicinal plants might also exert adverse effects. Thus, the present investigation aimed to assess the phytotoxic, cytotoxic, and genotoxic potential of two plants from the Brazilian Cerrado used in popular medicine, Davilla nitida (Vahl) Kubitzki, and Davilla elliptica (A. St.-Hil.). To this end, germination, growth, and cell cycle analyses were conducted using the plant model Lactuca sativa. Seeds and roots were treated with 0.0625 to 1 g/L for 48 hr under controlled conditions. The germination test demonstrated significant phytotoxic effects for both species at the highest concentrations tested, while none of the extracts produced significant effects in the lettuce growth test. In the microscopic analyses, the aneugenic and cytotoxic action of D. elliptica was evident. In the case of D. nitida greater clastogenic action and induction of micronuclei, (MN) were noted suggesting that the damage initiated by exposure to these extracts was not repaired or led to apoptosis. These findings indicated that the observed plant damage was transmitted to the next generation of cells by way of MN. These differences in the action of the two species may not be attributed to qualitative variations in the composition of the extracts as both are similar, but to quantitative differences associated with synergistic and antagonistic interactions between the compounds present in these extracts.

Antinociceptive Effect of Dillenia indica (Linn.) Mediated by Opioid and Cannabinoid Systems: Pharmacological and Chemical Studies.

Dillenia indica (Linn.) has been reported by several biological activities, including anti-inflammatory, antioxidant, antidiabetic, anti-hyperglycemic, antiproliferative, antimutagenic, anticholinesterase, and antimicrobial. In Brazilian traditional medicine, the fruits of D. indica have been used to treat general topical pain and inflammation, but with no scientific validation. Thus, aiming to study its chemical constitution and antinociceptive properties, the crude extract (CE) and fractions obtained from the fruits of D. indica were submitted to an in vivo pharmacological evaluation and a dereplication study by LC-MS/MS analysis, assisted by the Global Natural Product Social Molecular Networking (GNPS). The oral antinociceptive activity of the fruits of D. indica and the possible participation of the opioid and cannabinoid systems were demonstrated in the formalin-induced nociception model. The chemical dereplication study led us to identify several known chemical constituents, including flavonoids, such as caffeoylmalic acid, naringenin, quercetin, and kaempferol. According to literature data, our results are compatible with significant antinociceptive and anti-inflammatory activities. Therefore, the flavonoid constituents of the fruits of D. indica are probably responsible for its antioxidant, anti-inflammatory, and antinociceptive effects mediated by both opioid and cannabinoid systems, confirming its folk use in the treatment and relief of pain.

Anti-Zika Virus Activity and Isolation of Flavonoids from Ethanol Extracts of Curatella americana L. Leaves.

The ethnomedicinal plant Curatella americana L. (Dilleniaceae) is a common shrub in the Brazilian Cerrado, whose ethanolic extract showed significant in vitro anti-Zika virus activity by the MTT colorimetric method. Currently, there is no drug in clinical use specifically for the treatment of this virus; therefore, in this work, the antiviral and cytotoxic properties of the ethanolic extract, fractions, and compounds were evaluated. The ethanolic extract of the leaves showed no cytotoxicity for the human MRC-5 cell and was moderately cytotoxic for the Vero cell (CC50 161.5 ± 2.01 µg/mL). This extract inhibited the Zika virus multiplication cycle with an EC50 of 85.2 ± 1.65 µg/mL. This extract was fractionated using the liquid-liquid partition technique, and the ethyl acetate fraction showed significant activity against the Zika virus with an EC50 of 40.7 ± 2.33 µg/mL. From the ethyl acetate fraction, the flavonoids quercetin-3-O-hexosylgallate (1), quercetin-3-O-glucoside (2), and quercetin (5) were isolated, and in addition to these compounds, a mixture of quercetin-3-O-rhamnoside (3) and quercetin-3-O-arabinoside (4) was also obtained. The isolated compounds quercetin and quercetin-3-O-hexosylgallate inhibited the viral cytopathic effect at an EC50 of 18.6 ± 2.8 and 152.8 ± 2.0, respectively. Additionally, analyses by liquid chromatography coupled to a mass spectrometer allowed the identification of another 24 minor phenolic constituents present in the ethanolic extract and in the ethyl acetate fraction of this species.

Análise físico-química e atividades antifúngica e antioxidante do óleo essencial da flor de Curatella americana L / Physichochemical analysis, and antifungal and antioxidant activities of the essential oil of Curatella americana L. flower

Introdução: a espécie vegetal Curatella americana produz anualmente inflorescências com aroma adocicado rica em óleo essencial. Objetivo: avaliar as características físico-químicas, e atividades antifúngica e antioxidante do óleo essencial da flor de Curatella americana. Metodologia: as flores foram coletadas em quatro áreas de Cerrado no estado de Goiás; o rendimento de óleo essencial foi obtido através de hidrodestilação; as características físicas foram determinadas para densidade e solubilidade, a atividade antioxidante foi determinada pela redução do radical livre DPPH; a atividade antifúngica foi determinada por inibição das cepas de Candida, Sclerotinia sclerotiorum, Colletotrichum gloeosporioides e Aspergillus flavus. Resultados: o rendimento de óleo foi de 0,18%, densidade de 0,907 g mL-1, solubilidade positiva para EtOH 70%, atividade antioxidante de CI50 µL mL-1 1,95. Atividade de inibição fúngica apenas para Candida tropicalis na concentração de 8% com halo de antibiose de 10 mm. Sensibilidade discreta nas maiores concentrações de 25, 50 e 100 µL-1 para Aspergillus flavus e Sclerotinia sclerotiorum e baixa atividade de inibição para Colletotrichum gloeosporioides. Conclusão: o óleo essencial da flor de Curatella americana apresentou baixo rendimento, entretanto, alta eficiência na redução do radical livre DPPH. As atividades antifúngicas apresentaram bons resultados de inibição, entretanto, torna-se necessário a adição de outros óleos essenciais para aumento das taxas de inibição micelial.

Introduction: the plant species Curatella americana produces annual inflorescences with a sweet flavour rich in essential oil. Objective: to evaluate the physicochemical characteristics, antifungal and antioxidant activities of the essential oil of the Curatella americana flower. Methodology: the flowers were collected in four areas of Cerrado in the state of Goiás; the essential oil yield was obtained through hydrodistillation; the physical characteristics were determined for density and solubility, the antioxidant activity was determined by the reduction of the free radical DPPH; antifungal activity was determined by inhibiting the strains of Candida, Sclerotinia sclerotiorum, Colletotrichum gloeosporioides and Aspergillus flavus. Results: the oil yield was 0.18%, density 0.907 g mL-1, positive solubility for EtOH 70%, antioxidant activity of IC50 µL mL-1 1.95. Fungal inhibition activity only for Candida tropicalis at a concentration of 8% with a 10 mm antibiosis halo. Discrete sensitivity in the highest concentrations of 25, 50 and 100 µL-1 for Aspergillus flavus and Sclerotinia sclerotiorum and low inhibition activity for Colletotrichum gloeosporioides. Conclusion: The essential oil of the Curatella americana flower showed low yield, however, high efficiency in reducing DPPH free radical. Antifungal activities showed good inhibition results, however, it is necessary to add other essential oils to increase mycelial inhibition rates.

Toxicological evaluation of ethanolic extract of leaves from Doliocarpus dentatus in Swiss mice.

Doliocarpus dentatus (Dilleniaceae) has been used in folk medicine to treat inflammation and pain; however, studies evaluating its toxicity potential, as well as its effects on anxiety and depression, are scarce. This study investigated the toxicological profile of an ethanolic extract from leaves of D. dentatus (EEDd), and its effects on anxiety and depression models in mice. Male and female mice received either a single dose (500, 1000 or 2000 mg/kg) or repeated doses (75, 150 or 300 mg/kg) of EEDd by oral gavage. During the subacute toxicity assay, behavioral tests were performed on days 4, 14, 21 and 28. No evidence of toxicity was observed in the animals in both acute and subacute tests. However, males treated with the highest dose presented a reduction in the absolute weight of the kidney, an elevation in the AST levels, in addition to an alteration in the urea levels. The treatment did not affect other biochemical parameters, and did not induce any depressive-like behavior. EEDd exhibited low toxicity after single and repeated exposures. Since some analyzed parameters were compromised, further toxicity studies should be carried out.

The gelling properties of Dillenia indica mucilage in benzyl benzoate emulgel formulations

Abstract The objective of the study was to evaluate the gelling properties of Dillenia indica mucilage in benzyl benzoate emulgel formulation. Mucilage was extracted from the fruits of Dillenia indica using established methods and characterized by rheology and swelling. Emulsion (F1) was prepared using the continental emulsification method. Gelling agents (2 %w /v) were prepared by dispersing in distilled water with constant stirring at a moderate speed using a magnetic stirrer. F1 was added to the gel (0-75 %w /w) to obtain emulgel formulations and evaluated using viscosity, globule size, pH, release profiles and kinetic modeling. Data were expressed as mean ± SD, and similarity factor (f2) was used to compare all formulations. Formulation viscosity was significantly higher with carbopol than with Dillenia; globule sizes increased with concentration of gelling agents, and pH reduced as the concentration of Dillenia increased. All formulations showed controlled release properties with t80 ranging between 114 and 660 min. The release was governed by Korsmeyer-Peppas model. Formulation F5 prepared with 50 % Dillenia showed highest similarity to F4 prepared with 75 %w /w carbopol. Dillenia indica demonstrated acceptable gelling properties comparable with that of carbopol and could be improved for use in emulgel formulations.

Chemical profiling of Curatella americana Linn leaves by UPLC-HRMS and its wound healing activity in mice.

Based on ethnopharmacological studies, a lot of plants, as well as its compounds, have been investigated for the potential use as wound healing agents. In Brazil, Curatella americana is traditionally used by local people to treat wounds, ulcers and inflammations. However, to the best of our knowledge, its traditional use in the treatment of wounds has not been validated by a scientific study. Here, some compounds, many of them flavonoids, were identified in the hydroethanolic extract from the leaves of C. americana (HECA) by LC-HRMS and LC-MS/MS. Besides that, solutions containing different concentrations of HECA and a gel produced with this extract were evaluated for its antimicrobial, coagulant and wound healing activities on an excision mouse wound model as well as its acute dermal safety. A total of thirteen compounds were identified in HECA, mainly quercetin, kaempferol and glucoside derivatives of both, besides catechin and epicatechin known as wound healing agents. The group treated with 1% of HECA exhibited highest wound healing activity and best rate of wound contraction confirmed by histopathology results. The present study provides scientific evidence of, this extract (HECA) possess remarkable wound healing activity, thereby, supporting the traditional use.

Identificação das classes metabólicas secundárias em extratos etanólicos foliares de Byrsonima verbascifolia, Cardiopetalum calophyllum, Curatella americana e Qualea grandiflora / Identification of secondary metabolites classes in leaf ethanolic extracts of Byrsonima verbascifolia, Cardiopetalum calophyllum, Curatella americana and Qualea grandiflora

O Cerrado representa um banco fitoquímico de grande importância para a humanidade. O objetivo deste estudo foi identificar através da prospecção fitoquímica, os principais compostos químicos presentes nos extratos foliares de Byrsonima verbascifolia, Cardiopetalum calophyllum, Curatella americana e Qualea grandiflora. Neste estudo, foram coletadas folhas das espécies em área de preservação permanente (APP) no município de Rio Verde, GO. Os extratos foliares etanólicos foram avaliados quanto à presença ou não dos principais fitocompostos: ácidos orgânicos, açúcares redutores, alcalóides, antraquinonas, catequinas, cumarinas, depsídeos, depsidonas, ligações olefínicas, fenóis, flavonóides, glicosídeos cardiotônicos, polissacarídeos, purinas, saponinas e taninos. Exceto para grupos olefínicos, polissacarídicos e purínicos, foram observados resultados positivos para a maioria das classes metabólicas secundárias. A pesquisa preliminar dos extratos foliares etanólicos destas quatro espécies, possibilita uma prévia avaliação sobre suas características fitoquímicas devendo ainda ser avaliadas quanto aos seus teores e compostos majoritários para que se possam ser utilizadas como medicamentos fitoterápicos ou sintetização industrial.

The Cerrado represents a phytochemical bank of great importance for humanity. The objective of this study was to identify through phytochemical prospecting, the main chemical compounds present in the leaf extracts of Byrsonima verbascifolia, Cardiopetalum calophyllum ,Curatella americana and Qualea grandiflora. In this study, leaves of the species were collected in a permanent preservation area (APP) in the city of Rio Verde, State of Goiás. Ethanolic foliar extracts for the presence or absence of the main phytocomponents: organic acids, reducing sugars, alkaloids, anthraquinones, catechins, coumarins, depsidones, olefinic bonds, phenols, flavonoids, cardiotonic glycosides, polysaccharides, purines, saponins and tannins were evaluated. Except for olefin, polysaccharide and purine groups, positive results were observed for most of the secondary metabolic classes. Preliminary research on the ethanolic foliar extracts of these four species makes possible a preliminary evaluation about their phytochemical characteristics and should be evaluated for their contents and major compounds so that they can be used as herbal medicines or industrial synthesis.

Identificação das classes metabólicas secundárias em extratos etanólicos foliares de Byrsonima verbascifolia, Cardiopetalum calophyllum, Curatella americana e Qualea grandiflora / Identification of secondary metabolites classes in leaf ethanolic extracts of Byrsonima verbascifolia, Cardiopetalum calophyllum, Curatella americana and Qualea grandiflora

O Cerrado representa um banco fitoquímico de grande importância para a humanidade. O objetivo deste estudo foi identificar através da prospecção fitoquímica, os principais compostos químicos presentes nos extratos foliares de Byrsonima verbascifolia, Cardiopetalum calophyllum, Curatella americana e Qualea grandiflora. Neste estudo, foram coletadas folhas das espécies em área de preservação permanente (APP) no município de Rio Verde, GO. Os extratos foliares etanólicos foram avaliados quanto à presença ou não dos principais fitocompostos: ácidos orgânicos, açúcares redutores, alcalóides, antraquinonas, catequinas, cumarinas, depsídeos, depsidonas, ligações olefínicas, fenóis, flavonóides, glicosídeos cardiotônicos, polissacarídeos, purinas, saponinas e taninos. Exceto para grupos olefínicos, polissacarídicos e purínicos, foram observados resultados positivos para a maioria das classes metabólicas secundárias. A pesquisa preliminar dos extratos foliares etanólicos destas quatro espécies, possibilita uma prévia avaliação sobre suas características fitoquímicas devendo ainda ser avaliadas quanto aos seus teores e compostos majoritários para que se possam ser utilizadas como medicamentos fitoterápicos ou sintetização industrial.(AU)

The Cerrado represents a phytochemical bank of great importance for humanity. The objective of this study was to identify through phytochemical prospecting, the main chemical compounds present in the leaf extracts of Byrsonima verbascifolia, Cardiopetalum calophyllum ,Curatella americana and Qualea grandiflora. In this study, leaves of the species were collected in a permanent preservation area (APP) in the city of Rio Verde, State of Goiás. Ethanolic foliar extracts for the presence or absence of the main phytocomponents: organic acids, reducing sugars, alkaloids, anthraquinones, catechins, coumarins, depsidones, olefinic bonds, phenols, flavonoids, cardiotonic glycosides, polysaccharides, purines, saponins and tannins were evaluated. Except for olefin, polysaccharide and purine groups, positive results were observed for most of the secondary metabolic classes. Preliminary research on the ethanolic foliar extracts of these four species makes possible a preliminary evaluation about their phytochemical characteristics and should be evaluated for their contents and major compounds so that they can be used as herbal medicines or industrial synthesis.(AU)

Study of the potential adverse effects caused by the dermal application of Dillenia indica L. fruit extract standardized to betulinic acid in rodents.

This study aimed to evaluate the potential adverse effects of the dermal administration of Dillenia indica Linnaeus (D. indica) fruit extract in healthy rodents; the extract was standardized to betulinic acid. In the initial phase, the acute effects were evaluated on the skin application site of a single extract dose. A skin irritation test was performed in male Wistar rats (n = 8/group) receiving the extract (50-150 mg/mL) with betulinic acid (0.5-1.5%, respectively). A photosensitivity test was performed in male BALB/c mice (n = 6/group) receiving the extract (150 mg/mL). Afterwards, other BALB/c mice (n = 20, male:female, 1:1) were used to assess the systemic alterations caused by 14 daily repeated doses (150 mg/mL) by monitoring the effects on mortality, body morphology, behavior, nutrition status, neuromotor reactions, organ morphology and weight, and blood tests. At this time, 0.5 mg/mL clobetasol was used as the positive control. The skin irritation index suggested that negligible skin irritation had occurred, even when the extract was applied to the rat skin at 150 mg/mL. However, the extract acted as a photosensitizer on mouse skin, showing a photosensitizing activity close to that of 10 mg/mL 5-methoxypsoralen. Repeated doses caused no mouse mortality, aggressiveness, piloerection, diarrhea, convulsions, neuromotor alterations or nutrition status changes. The mouse organ weights did not change, and the mice did not have alterations in their blood compositions. Clobetasol caused a reduction in the mononuclear leukocyte numbers. In general, the data suggest that the extract was safe in healthy rodents but indicate that caution should be taken with the photosensitizing activity; in addition, this activity should be further explored as it may be useful for phototherapeutic drug development.

An overview of inventories of gall-inducing insects in Brazil: looking for patterns and identifying knowledge gaps.

We compiled published Brazilian gall-inducing insect inventories aiming to understand trends and biases in this field research and to investigate the factors that potentially explain the diversity of gall-inducing insects among different sampling sites. A total of 51 studies with gall-inducing insect inventories were compiled for Brazil, which sampled 151 sites in 88 municipalities, 13 states and five regions. The number of papers published on gall-inducing insects per year has increased over the last 30 years, being Cecidomyiidae (Diptera) the main galling taxon, Fabaceae the main host-plant family and Protium heptaphyllum (Burseraceae) the most important super-host species in these inventories. We found a great bias in the geographical distribution of Brazilian inventories, with the majority of studies in the Southeast region, and Atlantic Forest and Cerrado biomes. The total richness of gall-inducing insects differed significantly among regions and biomes, with higher gall richnesses being recorded in the North region and Amazon biome. However, Brazilian regions and biomes did not vary in richness of gall-inducing insect morphotypes per plant species. According our results, sampling by cecidologists in less studied regions of Brazil is needed, particularly in the North and South regions and subsampled biomes such as the Amazon, Pampas and Pantanal.

Lopesia davillae (Diptera, Cecidomyiidae), a new species of gall midge from Brazil associated with Davilla rugosa (Dilleniaceae) / Lopesia davillae (Diptera, Cecidomyiidae), uma nova espécie de cecidomiídeo do Brazil associada à Davilla rugosa (Dilleniaceae)

Abstract Lopesia davillae, a new species of gall midge associated with the reproductive structures of Davilla rugosa (Dilleniaceae), is described and illustrated (larva, pupa, male, female, and damage) based on material collected in Rio de Janeiro, Brazil. This new species is compared with its congeneric species. This is the first record of Lopesia on Dilleniaceae.

Resumo Lopesia davillae, uma nova espécie de Cecidomyiidae associada a estruturas reprodutivas de Davilla rugosa (Dilleniaceae), é descrita e ilustrada (larva, pupa, macho, fêmea e dano) com base em material coletado no estado do Rio de Janeiro, Brasil. A nova espécie é comparada com as outras espécies conhecidas do mesmo gênero. Este é o primeiro registro de Lopesia em Dilleniaceae.

Lopesia davillae (Diptera, Cecidomyiidae), a new species of gall midge from Brazil associated with Davilla rugosa (Dilleniaceae).

Lopesia davillae, a new species of gall midge associated with the reproductive structures of Davilla rugosa (Dilleniaceae), is described and illustrated (larva, pupa, male, female, and damage) based on material collected in Rio de Janeiro, Brazil. This new species is compared with its congeneric species. This is the first record of Lopesia on Dilleniaceae.

Healing effect of Dillenia indica fruit extracts standardized to betulinic acid on ultraviolet radiation-induced psoriasis-like wounds in rats.

CONTEXT: Dillenia indica Linn. (Dilleniaceae) is traditionally used to treat skin inflammation. OBJECTIVE: This study evaluated the healing effect of Dillenia indica fruit extracts on induced psoriasis-like wounds in Wistar rats. MATERIALS AND METHODS: Extracts were standardized to betulinic acid, including an aqueous ethanolic extract (AEE), ethyl acetate extract (EAE) and petroleum ether extract. Effects against lipid peroxidation were assessed in vitro. Wounds were created at rat tails (n = 12). Topical treatments were applied once daily for 7 days (1 mL of AEE or EAE at 5 or 50 mg/mL). Maximal dose was defined by the extract solubility. A 10-fold lower dose was also tested. Positive and negative controls were treated with clobetasol (0.5 mg/mL) or excipient. Half of each group was euthanized for histology. The remaining animals were observed for 20 days for wound measurements. RESULTS: Yields of AEE and EAE were 4.3 and 0.7%, respectively. Betulinic acid concentrations in AEE and EAE were 4.6 and 107.6 mg/g. Extracts neutralized lipid peroxidation in vitro at 0.02 µg/mL, accelerating healing at 50 mg/mL. Complete healing in mice treated with AEE occurred 16 days after wound induction. This time was 14 and 12 days in mice treated with EAE and clobetasol. Compared to orthokeratosis, parakeratosis was reduced by AEE (25%), EAE (45%) and clobetasol (55%). EAE caused superior protection against biomolecules oxidation of skin compared to AEE. DISCUSSION AND CONCLUSION: EAE exhibited activity closer to that of clobetasol. Betulinic acid may be an active constituent, which should be assessed in future studies.

Antioxidant and Hypolipidemic Activity of the Hydroethanolic Extract of Curatella americana L. Leaves.

High levels of reactive oxygen species in the body and hyperlipidemia are key factors for the development of cardiovascular diseases such as atherosclerosis. The present study investigated the antioxidant and hypolipidemic activity of hydroethanolic extract of Curatella americana L. leaves (ExC). The antioxidant activity of ExC was assessed by 2,2-diphenyl-1-picrylhydrazyl free radical (DPPH) scavenging capacity and protection against hemolysis induced by 2,2'-azobis(2-amidinopropane) dihydrochloride (AAPH), followed by quantification of malondialdehyde (MDA). Wistar rats with hyperlipidemia induced by high-fructose diet (60%) were treated for 60 days with water, simvastatin (30 mg·Kg(-1)), ciprofibrate (2 mg·Kg(-1)), and ExC (200 mg·Kg(-1)). ExC revealed IC50 of 6.0 ± 0.5 µg·mL(-1), an intermediary value among positive controls used in the assay of DPPH scavenging capacity. At all concentrations (50 to 125 µg·mL(-1)) and times (60 to 240 min) evaluated, ExC protected erythrocytes against AAPH-induced hemolysis, which was confirmed by lower MDA levels. In vivo tests showed a reduction of 34 and 45%, respectively, in serum concentration of cholesterol and triglycerides in hyperlipidemic rats treated with ExC, a similar effect compared to the reference drugs, simvastatin and ciprofibrate, respectively. Together, the results showed the antioxidant activity of ExC and its ability to improve the serum lipid profile in hyperlipidemic rats.

The Anti-Inflammatory Effects of the Methanolic Extract and Fractions from Davilla elliptica St. Hil. (Dilleniaceae) on Bothrops jararaca Envenomation.

Inflammation and haemorrhage are the main characteristics of tissue injury in botropic envenomation. Although some studies have shown that anti-venom prevents systemic reactions, it is not efficient in preventing tissue injury at the site of the bite. Therefore, this work was undertaken to investigate the anti-inflammatory effects of the methanolic extract and fractions from D. elliptica and to evaluate the role of matrix metalloproteinases (MMPs) in this process. Effects of the extract and fractions from D. elliptica were evaluated using a carrageenan-induced paw oedema model in rats, and leukocyte rolling was visualized by intravital. The quantification of MMPs activities (MMP-2 and MMP-9) extracted from the dermis of mice treated with extract and fractions alone or incubated with venom was determined by zymographic analyses. Our results show that intraperitoneal (i.p.) injection of fractions significantly reduced paw oedema after the carrageenan challenge. Treatment with the tannins fraction also resulted in considerable inhibition of the rolling of leukocytes and this fraction was able to decrease the activation of MMP-9. These results confirmed the anti-inflammatory activity of the methanolic extract and tannins fraction of D. elliptica and showed that the dermonecrosis properties of B. jararaca venom might be mediated through the inhibition of MMP-9 activity.

Variação sazonal nos teores de flavonoides, taninos e atividade antioxidante de Davilla rugosa Poir / Seasonal variation in the flavonoid and tannin contents and antioxidant activity of Davilla rugosa Poir

Davilla rugosa Poir. (Dilleniaceae) é uma trepadeira, conhecida como folha de lixa e cipó-cabloco, com distribuição geográfica ampla no Brasil. É utilizada como analgésica, vasoconstritora, antiúlcera, útil no tratamento das hemorroidas e varizes. O objetivo do trabalho foi investigar a influência da variação sazonal sobre alguns parâmetros das folhas de D. rugosa, como os teores de flavonoides e taninos. Os teores de flavonoides e taninos, determinados nas 4 estações do ano, foram avaliados segundo a Farmacopeia Brasileira e foram mais elevados no verão (0,71%; 16,73%) seguido do outono (0,58%; 16,39%). Considerando que substâncias fenólicas são, provavelmente, os responsáveis pela atividade anti-inflamatória e antiulcerogênica, podemos inferir que a melhor época de coleta, que conduza a uma matéria-prima com concentrações desejáveis de princípios ativos, é, preferencialmente, no verão seguida do outono. A atividade antioxidante do extrato de acetato de etila, desengordurado com hexano, submetido ao teste do DPPH, apresentou uma CE50 de 24,73 ±2,95 μg/mL e no ensaio do fosfomobdênio de 1,85 ±0,57 mmol de ácido ascórbico/mg de extrato seco. A atividade antioxidante encontrada nos extratos reforça os efeitos anti-inflamatórios e antiúlcera gástrica atribuídos para a espécie.

Davilla rugosa Poir. (Dilleniaceae) is a woody vine, popularly known as “folha de lixa e cipó-caboclo”, native to forest edges widely distributed across Brazil. It is used as an analgesic, vasoconstrictor and anti-ulcer agent and is useful in the treatment of hemorrhoids and varicose veins. The aim of this study was to investigate the influence of seasonal changes on some parameters of its leaves, such as the contents of flavonoids and tannins and antioxidant activity. The contents of flavonoids and tannins were determined in each of the four seasons, as recommended by the Brazilian Pharmacopeia, and found to be highest in summer (0.71%; 16.73%), followed by autumn (0.58%; 16.39%). Considering that phenolic substances are probably responsible for the anti-inflammatory and anti-ulcerogenic activities, we can infer that the best time for collection, to obtain a raw material with good concentrations of these metabolites, is in summer and autumn. The antioxidant activity of the ethyl acetate extract, subjected to the DPPH test after defatting with hexane, showed an EC50 of 24.73 +2.95 μg/mL and the equivalent of 1.85 +0.57 mmol ascorbic acid/mg dry extract in the phosphomolybdenum assay. The antioxidant activity determined for this extract enhances the anti-inflammatory and anti-ulcer activities attributed to the species.

Bioguided isolation of myricetin-3-O-ß-galactopyranoside with antinociceptive activity from the aerial part of Davilla elliptica St.-Hil.

ETHNOPHARMACOLOGICAL RELEVANCE: Davilla elliptica St.-Hil. (Dilleniaceae) is a medicinal plant traditionally used in Brazil to treat inflammatory processes, to relieve pain, as diuretic, gastro- and hepatoprotective agents. AIM OF THE STUDY: To undertake the fractionation of the ethanolic extract from Davilla elliptica leaves guided by an antinociceptive assay. MATERIALS AND METHODS: The antinociceptive activity was evaluated through the formalin test in mice. Extract fractionation was performed by percolation through silica gel and partition between immiscible solvents, followed by successive column chromatography over Sephadex LH-20 and preparative RP-HPLC. Structure elucidation of the isolated compound was accomplished by spectroscopic data. RESULTS: The EtOAc and MeOH fractions derived from the crude extract reduced significantly the licking time in the late phase of the formalin test. The bioguided fractionation of the MeOH fraction resulted in the isolation of myricetin-3-O-ß-galactopyranoside, which produced significant inhibition on nociception induced by formalin (ID50=0.26 mg/kg; p.o.). CONCLUSIONS: These results point out that myricetin-3-O-ß-galactopyranoside contributes for the antinociceptive effect of Davilla elliptica extract, a constituent considerably more potent than diclofenac, employed as reference drug.

Avaliação da atividade microbicida de extratos vegetais sobre Staphylococcus aureus isolados de mastite bovina / Evaluation of antibacterial activity of plant extracts on Staphylococcus aureus isolated from bovine mastitis

A resistência bacteriana é responsável perante o fracasso no tratamento de infecções com agentes quimioterápicos. São necessárias novas alternativas para controlar estes micro-organismos. Entre essas alternativas estão plantas utilizadas tradicionalmente na medicina popular. O presente trabalho avaliou a eficiência dos extratos etanólicos e acetonicos de folhas de Cecropia pachystachya e Curatella americana com atividade antibacteriana in vitro em cepas de Staphylococcus aureus isolado de caso de mastite bovina. Os extratos de C. pachystachya e C. americana apresentam MIC de 2,5 mg.mL-1. O composto isolado de C. pachystachya denominado EEB2 apresentou actividade bactericida para uma concentração de 1,25 mg.mL-1. Estes resultados demonstram que os extratos de C. pachystachya e C. americana contém compostos anti-bacterianos.

Bacterial drug resistance is responsible for the failure of the treatment of infection using chemotherapeutic agents. Thus, new approaches are necessary for the control of these microorganisms. Included among these alternatives are several plants that are traditionally used in folk medicine. Therefore, the aim of this study was to evaluate the antibacterial activity of the ethanolic and acetone extracts of leaves of Cecropia pachystachya and Curatela americana in vitro against S. aureus bacteria isolates from cases of bovine mastitis. The extracts from C. pachystachya and Curatela americana had a MIC of 2.5 mg.mL-1. The compound isolated from C. pachystachya called EEB2 showed bactericidal activity at a concentration of 1.25 mg.mL-1. These results demonstrate that the extracts of C. pachystachya and C. americana contains antibacterial compounds.

Antidiabetic and antihyperlipidemic effects of Dillenia indica (L.) leaves extract / Efeitos antidiabético e anti-hiperlipidêmico de extratos de folhas de Dillenia (L. )

The present study was carried out to evaluate antidiabetic and antihyperlipidemic effects of Dillenia indica methanolic leaves extracts in streptozotocin induced diabetic Wistar rats by administering graded oral doses (250 and 500 mg/kg body weight) for 21 days. The extract showed significant antidiabetic activity (p<0.001). Furthermore, the decreased body weight of rats was significantly improved after extract treatments. Daily oral treatment with the extract for 21 days to diabetic rats, also resulted in significant reduction in serum cholesterol, triglycerides and serum transaminase levels but HDL-cholesterol level was found to be improved (p<0.001) as compared to the diabetic control group. The extract treatment also showed to enhance serum insulin level in diabetic rats as compared to the diabetic control group. In conclusion, D. indica leaf extract might be useful for diabetes mellitus management and other abnormalities associated with this metabolic disorder.

Realizou-se o presente estudo para avaliar os efeitos antidiabético e anti-hiperlipidêmico de extratos metanólicos de folhas de Dillenia indica em ratos wistar com diabetes induzido por estreptozotocina por meio da administração de doses orais (250 e 500 mg/kg de peso corporal) por 21 dias. O extrato mostrou atividade antidiabética significativa (p<0,001). Além disso, a diminuição do peso corporal dos ratos foi significativamente melhorada após o tratamento com os extratos. O tratamento com doses orais do extrato por 21 dias aos ratos diabéticos também resultou em redução significativa do colesterol, triglicerídios e níveis de transaminase séricos, mas o nível de HDL-colesterol foi melhorado (p<0,001), quando comparado ao grupo controle diabético. O tratamento com extrato também mostrou aumento do nível sérico de insulina em ratos diabéticos comparativamente ao grupo controle diabético. Em conclusão, o extrato de folha de D. indica poderia ser útil para o controle do diabetes mellitus e de outras anormalidades associadas a essa disfunção metabólica.