Essential oil of Gallesia integrifolia is active against mycobacteria.

Background: There is critical need for new therapeutic options for treatment of diseases caused by mycobacteria. Materials & methods: Gallesia integrifolia essential oils (EOs) and crude extracts (CEs) were tested for their anti-Mycobacterium tuberculosis and anti-nontuberculous mycobacteria activity. Results: Minimum inhibitory concentration (MIC) of EOs ranged from 15.63 to 62.5 µg/ml against M. tuberculosis and 62.5 to >250 µg/ml against nontuberculous mycobacteria. CEs showed low activity. All EO tested demonstrated synergism with antituberculosis drugs. The cytotoxicity of EOs and CEs, in different cell lines, showed selectivity index from 2.2 to 9.8 and >0.056 to 2.0, respectively. Conclusion: G. integrifolia EOs are a candidate for the development of new therapeutic options in the treatment of tuberculosis and other mycobacterial diseases.

Bioactive compounds with antifungal activity against pathogens isolated from pregnant woman: Gallesia integrifolia (garlic wood) is a promising treatment for vulvovaginal candidiasis.

ETHNOPHARMACOLOGICAL RELEVANCE: The leaves, bark, and roots of Gallesia integrifolia are consumed in folk medicine through infusion, decoction, and topical preparation by crushing because of its pharmacological properties in several peripheral system disorders, including microbial infections. The presence of various molecules in different parts of the plant likely confers this species' fungicidal action, but scientific evidence is lacking. Vulvovaginal candidiasis mainly affects women of reproductive age. When left untreated, it can cause pregnancy complications. Currently available antifungals often cause undesirable side effects. New alternative therapeutic strategies based on medicinal plants have been proposed. AIM: To investigate the antifungal activity of G. integrifolia against vulvovaginal candidiasis secretion in pregnant women. MATERIALS AND METHODS: Antifungal activity was determined by the minimum inhibitory concentration (MIC), determined by broth microdilution method using Candida spp (NEWP1210), C. albicans (CCCD-CC001), C. tropicalis (CCCD-CC002) standard and clinical isolates from pregnant women with vulvovaginal candidiasis. Nystatin and fluconazole were used as positive controls. The chemical composition of essential oils that were extracted from leaves, flowers, and fruits of G. integrifolia was determined by gas chromatography coupled to mass spectrometry. Reverse docking was used to suggest a possible target in Candida. Conventional docking was used to identify the most probable compound that inhibits fungal growth. RESULTS: A total of 24 compounds were identified, accounting for ∼99% of volatile constituents in the essential oils. Leaves of G. integrifolia contained 3,5-dithiahexanol-5,5-dioxide (40.93%), flowers contained methionine ethyl ester (46.78%), and fruits contained 2,8-dithianonane (54.01%) as the most abundant compounds. The MICs of essential oils of leaves, flowers, and fruits of G. integrifolia against standard strains of Candida spp, C. albicans, and C. tropicalis ranged from 13.01 to 625.00 µg/mL. The essential oil of flowers more effectively inhibited Candida spp. Essential oils of leaves and flowers were similar to fluconazole against C. albicans. Essential oils of flowers and fruits were similar to fluconazole against C. tropocalis. In Candida yeast species that were isolated from vaginal secretion samples from pregnant patients, the MICs of leaves and flowers ranged from 52.08 to 5000.00 µg/mL. The essential oil of leaves (277.77 µg/mL) was the most active against C. albicans. No significant differences were found between the essential oils of leaves and flowers against C. glabrata. Docking simulations suggested that phytol in leaves and flowers was responsible for the antimicrobial effect. CONCLUSION: The present results suggest the potential therapeutic use of G. integrifolia, especially its leaves and flowers, against Candida and vulvovaginal candidiasis.

Qualidade de mudas de Pau-d'alho sob diferentes doses e frequências de aplicação de nutrientes / Quality of Pau dalho seedlings under different doses and frequencies of nutrient application

O trabalho teve como objetivo estudar como a dose e a frequência da fertirrigação influenciam o desenvolvimento de mudas de Gallesia integrifolia, por meio de variáveis morfofisiológicas. A pesquisa foi realizada no Viveiro de Produção de Mudas Florestais da FCA/UNESP. Foram desenvolvidos dois experimentos com a espécie, no primeiro ensaio testou-se o parcelamento da fertirrigação em três frequências de aplicação da solução nutritiva (F1 - uma vez na semana, F2 - duas vezes na semana e F15 a cada 15 dias), e no segundo ensaio foram estudadas três doses de solução nutritiva (DP dose padrão, DP + 50% dose 50% superior a padrão e DP+ 100% - 100% superior a padrão). Ao final do experimento foram avaliados: altura da parte aérea, diâmetro do colo, massas secas da parte aérea, radicular e total, índice de Qualidade de Dickson (IQD), conformação do sistema radicular, área foliar, transpiração e o índice de cor verde. Todas as variáveis morfológicas analisadas foram influenciadas pela frequência de aplicação da solução nutritiva, exceto o diâmetro do colo e o IQD. Não houve diferença estatística para as variáveis diâmetro do colo, massa seca total e IQD no experimento com doses. Mudas de maior qualidade de Gallesia integrifolia foram obtidas em uma dose padrão fornecida de forma mais fracionada.(AU)

The current study has as a goal how the dose and the frequency of fertirrigation influence the development of Gallesia integrifolia seedlings by means of morphophysiological variables. The research was carried out at the FCA/UNESP Forest Seedling Production Nursery. Two experiments were carried out with the species, in the first trial three application frequencies of the nutrient solution were tested (F1 - once a week, F2 - twice a week and F15 - every 15 days), and in the second trial three doses of nutrient solution (DP - standard dose, D50 - dose 50% higher than standard and D100 - 100% higher than standard). At the end of the experiment, shoot height, shoot diameter, shoot dry mass, root and total mass, index of Dicksons Quality (IQD), root system conformation, leaf area, transpiration, and green color index were evaluated. All analyzed morphological variables were influenced by the frequency of application of the nutrient solution, except for the collar diameter and the IQD. There was no statistical difference for the variables collar diameter, total dry mass and IQD in the dose experiment. Improved quality of seedlings of Gallesia integrifolia were obtained in a standard dose applied in a more fractional way.(AU)

Qualidade de mudas de Pau-d'alho sob diferentes doses e frequências de aplicação de nutrientes / Quality of Pau d’alho seedlings under different doses and frequencies of nutrient application

O trabalho teve como objetivo estudar como a dose e a frequência da fertirrigação influenciam o desenvolvimento de mudas de Gallesia integrifolia, por meio de variáveis morfofisiológicas. A pesquisa foi realizada no Viveiro de Produção de Mudas Florestais da FCA/UNESP. Foram desenvolvidos dois experimentos com a espécie, no primeiro ensaio testou-se o parcelamento da fertirrigação em três frequências de aplicação da solução nutritiva (F1 - uma vez na semana, F2 - duas vezes na semana e F15 – a cada 15 dias), e no segundo ensaio foram estudadas três doses de solução nutritiva (DP – dose padrão, DP + 50% – dose 50% superior a padrão e DP+ 100% - 100% superior a padrão). Ao final do experimento foram avaliados: altura da parte aérea, diâmetro do colo, massas secas da parte aérea, radicular e total, índice de Qualidade de Dickson (IQD), conformação do sistema radicular, área foliar, transpiração e o índice de cor verde. Todas as variáveis morfológicas analisadas foram influenciadas pela frequência de aplicação da solução nutritiva, exceto o diâmetro do colo e o IQD. Não houve diferença estatística para as variáveis diâmetro do colo, massa seca total e IQD no experimento com doses. Mudas de maior qualidade de Gallesia integrifolia foram obtidas em uma dose padrão fornecida de forma mais fracionada.

The current study has as a goal how the dose and the frequency of fertirrigation influence the development of Gallesia integrifolia seedlings by means of morphophysiological variables. The research was carried out at the FCA/UNESP Forest Seedling Production Nursery. Two experiments were carried out with the species, in the first trial three application frequencies of the nutrient solution were tested (F1 - once a week, F2 - twice a week and F15 - every 15 days), and in the second trial three doses of nutrient solution (DP - standard dose, D50 - dose 50% higher than standard and D100 - 100% higher than standard). At the end of the experiment, shoot height, shoot diameter, shoot dry mass, root and total mass, index of Dickson’s Quality (IQD), root system conformation, leaf area, transpiration, and green color index were evaluated. All analyzed morphological variables were influenced by the frequency of application of the nutrient solution, except for the collar diameter and the IQD. There was no statistical difference for the variables collar diameter, total dry mass and IQD in the dose experiment. Improved quality of seedlings of Gallesia integrifolia were obtained in a standard dose applied in a more fractional way.

Chemical characterization, toxicology and mechanism of gastric antiulcer action of essential oil from Gallesia integrifolia (Spreng.) Harms in the in vitro and in vivo experimental models.

Gallesia integrifolia is a Brazilian Amazon tree whose bark decoction is popularly used to treat peptic ulcer. The essential oil from the inner stem bark of G. integrifolia (EOGi) was chemically characterized by GC/MS. The in vitro cytotoxicity and genotoxicity were evaluated in CHO-K1 cells, while the in vivo oral acute toxicity was performed in mice. The gastroprotective effect of EOGi was assessed in acidified ethanol and piroxicam and ulcer healing on acetic acid -induced ulcer models in rodents. Anti-secretory, mucus, K+-ATP channels, prostaglandins (PGs), nitric oxide (NO), TNF-α, IL-1ß, IL-10, catalase (CAT) and myeloperoxidase (MPO) activities and in vitro Helicobacter pylori action by EOGi were evaluated. EOGi exhibited cytotoxic effects only at 72h and no acute toxicity. EOGi showed gastroprotective and ulcer healing effects. EOGi gastroprotection was attenuated by indomethacin pre-treatment. Gastric volume and total acidity were reduced, while gastric pH was elevated. EOGi increased mucus and NO productions and CAT activity, and inhibited MPO activity, TNF-α and IL-1ß concentrations and augmented IL-10. EOGi was not active against H. pylori. These results indicated that EOGi is safe and exerts preventive and curative gastric ulcer effects by multitarget actions. Twenty compounds were identified and (-)-alpha-santalene was the main compound.

Gallesia integrifolia (Spreng.) Harms: In vitro and in vivo antibacterial activities and mode of action.

ETHNOPHARMACOLOGICAL RELEVANCE: Gallesia integrifolia (Phytolaccaceae) is commonly known as "pau-d'alho" in Brazil or "garlic plant" due to the strong scent of garlic peculiar to all parts of the plant. The bark decoction is used for the treatment of microbial infections among other diseases by different ethnic groups in Brazil, Peruvian Amazonians, Bolivia and Mosetene Indians. This study aimed to advance in the antibacterial activity and characterize the mode of action of the hydroethanolic extract of the inner stem bark of G. integrifolia (HEGi) using in vivo and in vitro experimental models. MATERIALS AND METHODS: The qualitative and quantitative phytochemical analyzes of HEGi were carried out using colorimetric and HPLC technique. The cytotoxic potential of HEGi was evaluated against CHO-K1 cells by Alamar blue assay and its acute toxicity was assessed by the Hippocratic screening test using Swiss-Webster mice. The antibacterial activity was evaluated by micro- dilution method against ten strains of Gram-positive and Gram-negative bacteria. The mode of action of HEGi was investigated by outer membrane permeability, nucleotide leakage and potassium efflux assays. In vivo infection model was established by using Staphylococcus aureus infection model Wistar rats. RESULTS: Qualitative phytochemical analysis of HEGi revealed the presence of saponins, alkaloids, phenolic compounds and flavonoids. Phytochemical quantification of HEGi showed that higher total phenolic (80.10±0.62mg GAE/g) and flavonoid (16.10±0.03mg RE/g) contents. HPLC fingerprint analysis revealed the presence of gallic acid, rutin, and morin. In the Alamar blue assay no cytotoxic effect of HEGi in CHO-K1 cells was observed up to 200µg/mL, and no signs or symptoms of acute toxicity were observed in mice of both sexes at higher doses of up to 2000mg/kg, p.o. HEGi demonstrated bacteriostatic effect against selected Gram positive and Gram negative bacterial pathogens. Its mode of action is associated, at least partly, with changes in the permeability of bacterial membranes, evidenced by the increased entry of hydrophobic antibiotic in Pseudomonas aeruginosa, intense K(+) efflux and nucleotides leakage in Shigella flexneri, Streptococcus pyogenes and S. aureus. HEGi attenuated the experimental blood borne S. aureus infection in rats at all the tested doses levels (10, 50 and 250mg/kg). CONCLUSION: HEGi is safe at the dose tested when used acutely, and it presented broad antibacterial effect, which support its traditional use in the treatment of bacterial infections. It contains well known important phytochemicals, recognized to be active against bacterial pathogens in vitro and might be collectively responsible for the antibacterial activity of HEGi. It is bacteriostatic in nature, with membrane perturbation being one of it mode of action. HEGi represent a potential phytotherapic antibacterial agent.

Efeitos do sombreamento na anatomia foliar de Gallesia integrifolia (Spreng) Harms e Schinnus terebinthifolius Raddi / Effects of shading on leaf anatomy of Gallesia integrifolia (Spreng) Harms and Schinnus terebinthifolius Raddi

Realizou-se estudo com o objetivo de analisar as alterações na anatomia foliar de Gallesia integrifolia (Spreng) Harms e Schinnus terebinthifolius Raddi quando cultivadas em ambientes de sombra moderada ou densa, simulando as condições naturais encontradas em sistemas agroflorestais tradicionais do sul da Bahia, Brasil. Plantas das duas espécies, com aproximadamente um ano de idade, foram cultivadas em casa de vegetação sob quatro níveis de sombreamento (25%, 17%, 10% e 5%). Estudos anatômicos do limbo foliar foram realizados a partir de material incluído em parafina e seccionado em micrótomo rotativo. Os diferentes níveis de sombreamento ocasionaram alterações na estrutura do mesofilo de ambas as espécies, com diferenças significativas na espessura do parênquima paliçádico, limbo foliar, e densidade estomática. Nas condições em que o experimento foi realizado os resultados obtidos indicaram que G. integrifolia apresenta maior capacidade de aclimatação a ambientes de sombra moderada e densa do que S. terebinthifolius, sendo mais indicada para o cultivo em sistemas agroflorestais pré-estabelecidos.

This study was conducted with the aim of analyzing the changes in the leaf anatomy of Gallesia integrifolia (Spreng) Harms and Schinnus terebinthifolius Raddi when grown in environments with moderate to dense shade, simulating the natural conditions found in traditional agroforestry systems in southern Bahia, Brazil. Plants of both species, being approximately one year-old, were grown at four irradiance levels (25%, 17%, 10% and 5%) in a greenhouse. Leaf anatomical studies were made from material embedded in paraffin and sectioned on a rotary microtome. The different irradiance levels caused a shift in the mesophyll anatomy of both species, with significant differences in palisade parenchyma thickness and leaf stomatal density. In the conditions of this experiment, the results indicated that G. integrifolia has a higher capacity for acclimatization to moderate to dense shade than S. terebinthifolius, and it is thus more suitable for cultivation in pre-established agroforestry systems.

Caracterização farmacognóstica de pau d'alho Gallesia integrifolia (Spreng. ) Harms / Pharmacognostic characterization of pau d'alho Gallesia integrifolia (Spreng. ) Harms

Caracterizou-se farmacognosticamente a droga pau d'alho pertencente a espécie Gallesia integrifoli. (Spreng.) Saras da família Phytolaecaceae. As descriçoes são acompanhadas dos respectivos desenhos. Reações histoquímicas foram efetuadas em folhas frescas, folhas fermentadas a 40ºC e na droga (folha seca).

The authors present a morphological and histologycal study of the leaf of Gallesia integrifolia (Spreng.) Harms, analysing the most characteristics elements for its identification. A screening the histochemical reactions in leaves are also given. Fresh and crude drug are histochemically analysed.