Plantas do cerrado brasileiro com atividade contra Mycobacterium fortuitum

Mycobacterium fortuitum is a rapidly-growing species of bacteria, ubiquitous in the environment and related to important human mycobacterioses. It has been isolated from blood, abscesses, the endocardium and surgical and traumatic wounds. This mycobacterium is hard to treat, being recognized in the literature as resistant even to the drugs used in the treatment of tuberculosis. The objective of this study was to screen extracts prepared from plants of the Brazilian cerrado (extended savanna-like belt) with known activity against M. fortuitum, employing the Microplate Alamar Blue Assay (MABA) as the analytical method. Out of 26 extracts tested against M. fortuitum, the nonpolar extract of Quassia amara (in methylene dichloride) gave the best result (MIC 62.5μg/ mL), followed by the nonpolar extracts of Syngonanthus macrolepsis, Davilla elliptica and Turnera ulmifolia, with equal MICs of 125μg/ml. The polar extracts (in ethanol and methanol) obtained from the same plants were considered inactive, since the MIC values determined were above 500μg/mL and not significantly different from those of extracts from other plants, without known activity.

Gastroprotective effect of the ethanolic extract and fractions obtained from syngonanthus bisulcatus Rul

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Evaluation of Syngonanthus nitens (Bong.) Ruhl. extract as antifungal and in treatment of vulvovaginal candidiasis

The purpose of this study was to evaluate the in vitro anticandidal activity of a methanolic extract of Syngonanthus nitens scapes against different Candida species and clinical isolates from patients with vulvovaginal candidiasis (VVC), and its effect in vivo in the treatment of vaginal infection. Chemical characterization of the extract was performed by HPLC-UV analyses and showed the presence of flavones derivatives. The extract was effective against several Candida strains from our collection and species recovered from VVC patients, and was able to inhibit the yeast-hyphal transition. No cytotoxic activity against human female reproductive tract epithelial cells and no hemolytic activity against human red blood cells were observed. In the in vivo model of VVC, we evaluated the efficacy of the intravaginal treatment with a cream containing the extract at doses of 0.5, 1.0 and 2.0%. The treatment eradicated the vaginal fungal burden in infected rats after 8 days of treatment. S. nitens extract could be considered as an effective and non-toxic natural antifungal agent in the treatment of vulvovaginal candidiasis. © 2013 ISHAM.

Phytochemical study and antiulcerogenic activity of Syngonanthus bisulcatus (Eriocaulaceae)

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Gastric antiulcer activity of Syngonanthus arthrotrichus SILVEIRA

Syngonanthus arthrotrichus SILVEIRA, popularly known as sempre-vivas mini-saia, is found in mountains of the Espinhaco range in the Brazilian states of Bahia and Minas Gerais. Extracts of this species contain several constituents, including flavonoids which may have antiulcerogenic activity. An ethanolic extract (EEOH), and flavonoid-rich (FRF) and flavonoid-deficient (FDF) fractions obtained from the scapes of S. arthrotrichus were investigated for their ability to prevent ulceration of the gastric mucosa in mice and rats. In the ethanol/HCl-induced ulcer model, lansoprazole (30 mg/kg), EEOH (50, 100, 250 mg/kg) given orally protected the gastric mucosal against injury in mice by 79%, 78%, 73%, and 64% respectively. In the ethanol-induced gastric ulcer model in rats, the lansoprazole (30 mg/kg), FRF and FDF (100 mg/kg) significantly protected the gastric mucosal of rats by 65%, 38% and 25% respectively when compared with the negative control group. In indomethacin/ bethanechol-induced gastric ulcers, cimetidine (100 mg/kg) and the EEOH (100, 250 mg/kg) inhibited gastric ulcer formation by 73%, 55% and 32% respectively. In this exactly model other treatments as cimetidine, FRF and FDF (100 mg/kg) each caused 54%, 36% and 45% inhibition, respectively. In the stress-induced gastric ulcer model, cimetidine (100 mg/kg) and the EEOH (50, 100, 250 mg/kg), inhibited gastric ulcer formation by 63%, 73%, 68% and 69% respectively. In the same model, cimetidine, FRF and FDF (100 mg/kg) significantly protected the gastric mucosal of the mice by 60%, 51% and 47% when compared to the control group. In pylorus-ligated mice, cimetidine (positive control) and FRF significantly decreased gastric acid secretion, increased gastric pH and reduced the acid output when compared to the negative control. FDF had no significant effect on these parameters. The protection provided by FRF probably involved an antisecretory mechanism mediated by flavonoids which were absent in FDF. The amount of adherent mucous in the stomach contents was also evaluated with the treatments carbenoxolone (200 mg/kg), FRF and FDF (100 mg/kg) treatment. Each treatments significantly increased the amount of adherent mucous in the gastric juice (8.67 +/- 1.73, 3.35 +/- 1.59, 2.1 +/- 0.41 mg/g of wet tissue, respectively) compared to the control group, indicating a cytoprotective action on the gastric mucosa. Treatment with FRF plus indomethacin and FDF plus indomethacin reduced the prostaglandin biosyntesis (13.6 +/- 6.5, 27 +/- 5.5 pg/well) by the mucosa, indicating that the cytoprotective action on the gastric mucosa was not related to the level of prostaglandins. Only FDF (38 +/- 17 pg/well) maintained the level of prostaglandins and guaranteed the integrity of the mucosa. The results indicate that the EEOH, FRF and FDF have antisecretory and cytoprotective actions, that may be related to the presence of luteoline in the extract and active fractions.

Estrogenic and chemopreventive activities of xanthones and flavones of Syngonanthus (Eriocaulaceae)

The possible benefits of some bioactive flavones and xanthones present in plants of the genus Syngonanthus prompted us to screen them for estrogenic activity. However, scientific research has shown that such substances may have undesirable properties, such as mutagenicity, carcinogenicity and toxicity, which restrict their use as therapeutic agents. Hence, the aim of this study was to assess the estrogenicity and mutagenic and antimutagenic properties. We used recombinant yeast assay (RYA), with the strain BY4741 of Saccharomyces cerevisiae, and Ames test, with strains TA100, TA98, TA97a and TA102 of Salmonella typhimirium, to evaluate estrogenicity, mutagenicity and antimutagenicity of methanolic extracts of Syngonanthus dealbatus (S.d.), Syngonanthus macrolepsis (S.m.), Syngonanthus nitens (S.n.) and Syngonanthus suberosus (S.s.), and of 9 compounds isolated from them (1 = luteolin, 2 = mix of A-1,3,6-trihydroxy-2-methoxyxanthone and B-1,3,6-trihydroxy-2,5- dimethoxyxanthone, 3 = 1,5,7-trihydroxy-3,6-dimethoxyxanthone, 4 = 1,3,6,8-tetrahydroxy-2,5-dimethoxyxanthone, 5 = 1,3,6,8-tetrahydroxy-5- methoxyxanthone, 6 = 7-methoxyluteolin-8-C-β-glucopyranoside, 7 = 7-methoxyluteolin-6-C-β-glucopyranoside, 8 = 7,3′-dimethoxyluteolin- 6-C-β-glucopyranoside and 9 = 6-hydroxyluteolin). The results indicated the estrogenic potential of the S. nitens methanol extract and four of its isolated xanthones, which exhibited, respectively, 14.74 ± 1.63 nM; 19.54 ± 6.61; 7.20 ± 0.37; 6.71 ± 1.02 e 10.01 ± 4.26 nM of estradiol-equivalents (EEQ). None of the extracts or isolated compounds showed mutagenicity in any of the test strains and all of them showed antimutagenic potential, in particular preventing mutations caused by aflatoxin B1 (AFB1) and benzo[a]pyrene (B[a]P). The results show that the xanthones, only isolated from the methanol extract of S. nitens capitula, probably were the responsible for its estrogenic activity and could be useful as phytoestrogens, providing a new opportunity to develop hormonal agents. In addition, flavones and xanthones could also be used as a new antimutagenic agent. Since, the mutagens are involved in the initiation and promotion of several human diseases, including cancer, the significance of novel bioactive phytocompounds in counteracting these pro-mutagenic and carcinogenic effects is now gaining credence. © 2013 Elsevier Inc. All rights reserved.

Estudo químico e atividades mutagênica e antiulcerogênica de Syngonanthus nitens (Bong.) Ruhland

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Caracterização do pontencial biológico de Leiothrix spiralis Ruhland E Syngonanthus nitens (Bong.) Ruhland (Eriocaulaceae)

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Syngonanthus nitens (Bong.) Ruhland: caracterização biológica e prospecção terapêutica do extrato metanólico incorporado ou não em sistema nanoestruturado para aplicação no tratamento da candidíase vulvovaginal

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Acute lethal and sublethal effects of neem leaf extract on the neotropical freshwater fish Prochilodus lineatus

The aim of this study was to determine the toxicity of the aqueous extract of neem leaves, a product extensively used in fish-farms as alternative for the control of fish parasites and fish fry predators, for the neotropical fish Prochilodus lineatus. The 24 It LC(50) of neem leaf extract for juveniles P lineatus was estimated as 4.8 g L(-1); the fish were then exposed for 24 h to 2.5, 5.0 and 7.5 g L(-1) or only clean water (control). Plasma glucose levels were higher in fish exposed to 2.5 g L(-1) and 5.0 g L(-1) neem extract, relative to control, indicating a typical stress response. Neem extract did not interfere with the osmoregulating capacity of the fish, as their plasma sodium, chloride, total protein and osmolarity did not change. The presence of the biopesticide interfered with the antioxidant defense system of P. lineatus, as there was a decrease in liver catalase activity at all neem concentrations and the detoxifying enzyme glutathione-S-transferase was activated in fish exposed to 5.0 g L(-1). Fish exposed to all neem extract concentrations exhibited damaged gill and kidney tissue. These results indicate that although neem extract is less toxic to P. lineatus than other synthetic insecticides used in fish-farming it does cause functional and morphological changes in this fish species. (c) 2006 Elsevier B.V. All rights reserved.

Effect of Aloe vera extract on the improvement of the respiratory activity of leukocytes of matrinxã during the transport stress

This study evaluated the effect of extract of Aloe vera in the transport water of matrinxã (Brycon amazonicus) fish on stress response and leukocyte respiratory activity. Fish was transported for 4 h in water containing Aloe at levels 0; 0.02; 0.2 and 2 mg/L, and sampled before transport 2, 4, 24 and 96 h after for determination of plasma glucose and respiratory activity of leukocytes. An additional in vitro assay was conducted with another fish species, pacu (Piaractus mesopotamicus), to test the respiratory burst of leukocytes exposed to Aloe extract (0.0, phosphate-buffered saline (PBS) only) at 0.1, 0.2, 0.5 and 1 mg/L). Plasma glucose increased after 2 and 4 h of transport and returned to control levels within 24 h, but the addition of Aloe in the transport water did not affect the level of blood glucose. However, at 2 h of transport, Aloe enhanced the respiratory activity of leukocytes in a dose-dependent way. The highest value of respiratory burst activity of leukocytes was observed in the fish transported in water containing Aloe at 2 mg/L. The enhancing effect of the plant extract on the production of oxygen radicals was confirmed in vitro in leukocytes of pacu incubated in Aloe at concentrations 0.1 and 0.2 mg/L. The results suggest that Aloe vera is a modulator of the immune system in fish improving the innate immune response tested.

The extract of the jellyfish Phyllorhiza punctata promotes neurotoxic effects

Phyllorhiza punctata (P. punctata) is a jellyfish native to the southwestern Pacific. Herewith we present the biochemical and pharmacological characterization of an extract of the tentacles of P. punctata. The tentacles were subjected to three freezethaw cycles, homogenized, ultrafiltered, precipitated, centrifuged and lyophilized to obtain a crude extract (PHY-N). Paralytic shellfish poisoning compounds such as saxitoxin, gonyautoxin-4, tetrodotoxin and brevetoxin-2, as well as several secretory phospholipase A2 were identified. PHY-N was tested on autonomic and somatic neuromuscular preparations. In mouse vas deferens, PHY-N induced phasic contractions that reached a peak of 234 +/- 34.7% of control twitch height, which were blocked with either 100 mu m of phentolamine or 1m m of lidocaine. In mouse corpora cavernosa, PHY-N evoked a relaxation response, which was blocked with either L-NG-Nitroarginine methyl ester (0.5 m m) or 1m m of lidocaine. PHY-N (1, 3 and 10 mu g ml(-1)) induced an increase in tonus of the biventercervicis neuromuscular preparation that was blocked with pre-treatment of galamine (10 mu m). Administration of 6 mg kg(-1) PHY-N intramuscularly produced death in broilers by spastic paralysis. In conclusion, PHY-N induces nerve depolarization and nonspecifically increases neurotransmitter release. Copyright (C) 2011 John Wiley & Sons, Ltd.

Inhibition of the myotoxic activity of Bothrops jararacussu venom and its two major myotoxins, BthTX-I and BthTX-II, by the aqueous extract of Tabernaemontana catharinensis A. DC. (Apocynaceae)

Partial neutralization of the myotoxic effect of Bothrops jararacussu venom (BV) and two of its myotoxins [bothropstoxin-I (BthTX-I), catalytically inactive, and II (BthTX-II), showing low PLA(2) activity], by the lyophilized aqueous extract of Tabernaemontana catharinensis (AE), was studied in rat isolated soleus muscle preparations (in vitro) and through i.m. injection in the gastrocnemius muscle (in vivo) by determination of creatine kinase (CK) activity and histopathological analysis. Incubation of soleus muscle for 1 h with BV or toxins (20 mug/ml) plus AE (400 mug/ml) added immediately after BV, BthTX-I or BthTX-II reduced CK levels by 53%, 37% and 56%, respectively. The myonecrotic effects of BV (20 mug/ml) upon soleus muscle was reduced 24%, 35% and 36% when AE (400 mug/ml) was added 1 h after BV and CK was evaluated 30 min, 1 and 2 h later, respectively. For BthTX-I these values were 46%, 48% and 47%, while for BthTX-II no inhibitory effect was detected. Histological analysis of soleus muscle after incubation with AE (400 mug/ml, I h) did not reveal any change in muscle fibers, but severe necrosis induced by -BV or toxins (20 mug/ml) was clearly in evidence, and decreased significantly when soleus muscle was protected by AE. This protection was also observed when AE was administered 1 h after BV or BthTX-I, but not after BthTX-II. AE did not inhibit the catalytic PLA(2), activity of BthTX-II or BV and did not change the PAGE pattern of BV, BthTX-I or BthTX-II. In vivo assays were performed in 100-g rats and maximal CK release was attained at a dose of 100 mug of BV, 3 h after injection. AE was not effective when injected 20 s after BV or toxins. However, injecting BV or toxins (100 mug), which were pre-incubated with AE (2 mg) caused an inhibition of 57%, 59% and 51%, respectively, with zero time pre-incubation, but was less effective with I h pre-incubation. This plant represents a potential source of promising myotoxin inhibitors. (C) 2004 Elsevier GmbH. All rights reserved.

Effects of the Ottonia martiana Miq. (Piperaceae) extract on dog's ocular surface

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)