In vitro conservation and low cost micropropagation of Cochlospermum regium (Mart. Ex. Scharank)

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

Avaliacao da atividade da nova cefalosporina de quarta geracao cefpiroma contra amostras clinicas isoladas em unidades de terapia intensiva e unidades de oncoematologia de varios hospitais brasileiros

Objective: To evaluate the in vitro activity of the fourth-generation cephalosporin cefpirome in comparison to that of ceftazidime, ceftriaxone, cefotaxime and imipenem in a multicenter study involving nine hospitals from six cities (four states). Material and methods: A total of 804 isolates from patients hospitalized in either intensive care units or Oncology/Hematology units was evaluated. The isolates were collected between June and November of 1995, i.e. before cefpirome became commercially available in Brazil, and susceptibility tested by broth microdilution following the NCCLS procedures. All isolates resistant to cefpirome were retested by B-test. Results: Against Enterobacteriaceae (n = 344), cefpirome demonstrated an activity 2 to 32-fold higher than that of the third-generation cephalosporins (TGCs) and similar to that of imipenem. The percentages of Enterobacteriaceae susceptible were: 88%, 69% and 96% for cefpirome, TGCs and imipenem, respectively, The cefpirome spectrum were greater or equal to that of imipenem against Citrobacter freundii, Enterobacter aerogenes, Morganellao morganii and Serratia marcescens. Against Acinetobacter sp. (n = 77), cefpirome was slightly more active than ceftazidime; however, the percentages of isolates resistant to these compounds were high (84% and 88%, respectively). The activities of cefpirome, ceftazidime and imipenem were very similar against P. aeruginosa isolates (n = 128), with MIC50 (μg/ml) percent susceptible of 8/59%, 8/62% and 4/62% respectively, Against aerobic gram-positive bacteria, the cefpirome activity was 4 to 16-fold higher than that of TGCs but 2 to 8-fold lower than that of imipenem. Conclusion: The results of our study suggest that, in Brazil, cefpirome has a spectrum of activity which is higher than that of the TGCs against aerobic gram-negative (Enterobacteriaceae and non-Enterobacteriaceae) and gram-positive bacteria and similar to that of imipenem against some Enterobacteriaceae species and P. aeruginosa.

Antibiotic 26-deoxylaidlomycin isolated from Streptomyces sp. Ar386 from Brazilian soil

An actinomycete strain (Ar386) was isolated from the soil of the Araraquara regio, SP, Brazil. The strain, named Streptomyces jacareensis, formed irregular rayed, rugose, grayish-white mycelium with sinuous, branched hyphae carrying rare isolated spores; assimilated glucose, galactose, inositol, ribose, maltose, sucrose, melibiose and starch but not mannitol, rhamnose, arabinose, xylose, lactose and raffinose; and contained LL- diaminopimelic acid in its cell wall. An antibiotic active against Gram- positive bacteria, which was characterized as being 26-deoxylaidlomycin and which may have application against poultry coccidiosis, was isolated from cultures of the strain. This was the first isolation of this antibiotic from a microorganism of the genus Streptomyces and also the first isolation of this antibiotic in Brazil.

Atividade comparada da cefepima, cefpiroma e amicacina em amostras bacterianas hospitalares

The objective of this study was to evaluate the in vitro activity of cefepime, cefpirome and amikacin against the most prevalent nosocomial bacteria. Initially a prospective study was designed to compare the bacterial susceptibility to the three drugs using 1,022 pathogenic strains. The strains were isolated from hospitalized patients of the Hospital das Clinicas - Faculdade de Medicina de Botucatu, SP, from March to December of 1996, by using the Bauer-Kirby susceptibility diffusion controlled method. The activity of cefepime by the Kirby-Bauer method was significantly higher (χ2, p ≤ 0.05) than cefpirome and amikacin for the following bacteria: P. aeruginosa (72% x 56% x 64%, respectively), Enterobacter cloacae (98% x 88% x 80%) and total strains (79.5% x 74.3% x 76.8%). Cefpirome exhibited higher activity than cefepime only to Enterococcus faecalis (42% x 23%). In the 12 other bacterial groups studied the sensibility of the three drugs was similar (χ2, p ≥ 0.05). The minimal inhibitory concentration (MIC) for 127 bacterial strains - Enterobacter cloacae (12), Citrobacter sp (15), Pseudomonas aeruginosa (50), Acinetobacter baumannii (12), BGNF others (22) and Enterococcus faecalis (16)-from the same origin previously described and isolated during 1997, was determined by E-test. Ranges of MIC intervals, MIC(50%), MIC(90%) and the proportion of the sensitive bacterial strains were determined and permitted the following analysis: the activity of cefepime against Gram-negative bacteria was 2 or more times higher than that of cefpirome and amikacin, specially when CIM(90%) was considered; the activity of cefpirome was higher only against E. faecalis. This information must be considered in the rational use of antibiotic, specially in patients with nosocomial infections.

Chemistry and bioactivity of Raulinoa echinata Cowan, an endemic Brazilian rutaceae species

The hexane extract of the stems of Raulinoa echinata afforded the sesquiterpenes germacrene D (6), 1β,6α-dihydroxy-4-(15)-eudesmene (4) and oplopanone (5); the triterpenes squalene, isomultiflorenol (7), isobauerenol (8) and friedelin (9); the protolimonoids melianone (2) and melianodiol (3); and the pyranocoumarin 3-(1′-1′-dimethylallyl)-lomatin (1), which has not been reported previously as a natural product; together with β-sitosterol. The hexane extract and some of these compounds were assayed in vitro against trypomastigote forms of Trypanosoma cruzi. Brine shrimp lethality and antimicrobial activities of the crude extract and pure compounds were also evaluated.

In vitro cytotoxicity of some natural and semi-synthetic isocoumarins from Paepalanthus bromelioides

Numerous natural compounds have a potential for therapeutic applications, but may have to be chemically modified to alter toxic side effects. We investigated structural parameters that could affect the cytotoxicity of isocoumarins similar to 9,10-dihydroxy-5,7-dimethoxy-1H-naphtho(2,3c)pyran-1-one (paepalantine 1). Paepalantine 1 has antimicrobial activity, as well as significant in vitro cytotoxic effects in the McCoy cell line. Two other natural and two semi-synthetic isocoumarins with similar structures obtained from the capitula of Paepalanthus bromelioides were tested on the same cell line by the neutral red assay. Substitution of the 9 and/or 10-OH group made these compounds less cytotoxic.

Contribuição ao estudo farmacognóstico da mutamba (Guazuma ulmifolia - Sterculiaceae)

Guazuma ulmifolia Lam., Sterculiaceae, popularly known as mutamba, has a wide geographical distribution, ranging from Mexico to Southern Brazil. The interest in its chemical properties is due to its popular use for hair loss treatment. This activity can be attributed to tannins that have many pharmacological activities such anti-inflammatory, anti-ulcerogenic, anti-microbial, anti-viral, capillary protective action and radical scavenging properties. In the microscopic analysis of barks and leaves, large secretor ducts could be detected among the parenchyma cells, as well as star shaped trichoms on the epidermis. One of the aims of the anatomical study was to detect tissues with polyphenolic compounds. The results indicated two tissues rich in these compounds: the phloematic region and the periderm. Chemical analyses were carried out on the bark and showed the presence of the following chemical groups: flavonoids, tannins, saponins and mucilages.

Antibiótico antifungico produzido por um estreptomiceto da região de Araraquara

With the significant increase in the incidence of invasive fungal infections during the last decade, mainly in patients with cancer, AIDS and other hospitalized patients who stay for long periods in intensive care units, there is an urgent need to screen for new antifungal agents possessing some advantages over known ones. This article reports a search in the field for a microorganism producing antibacterial and antifungal substances. Strains from soil samples collected in the region of Araraquara, Brazil, were isolated and analyzed for their antimicrobial potential against standard microorganisms (fungi Candida albicans and Aspergillus oryzae and bacteria Staphylococcus aureus and Escherichia coli). Out of the 64 strains isolated, 34 produced detectable antimicrobial activity. The streptomycete strain Ar4014 was chosen for further study, owing to its good antimicrobial activity against Candida albicans. Two of the fermentation media tested, 608-K and 602-B, were found to be best for the production and extraction of the antibiotic from Ar4014. After chromatographic separation of the crude extract on a silica column, the active fractions obtained showed UV-VIS absorption peaks characteristic of normal pentaenic antibiotics. The antibiotic was provisionally designated Ara 4014-75.

Ação farmacológica de Syzygium cumini (L.) skeels

Natural products have received new interest recently, maybe in men's attempt to turn into the nature for the prevention and the relief of diseases, mainly because of those untreated by the traditional medicine. Syzygium cumini (L.) Skeels, popularly known as 'jambolão, is a well-known plant by several pharmacological actions so much in the popular use as in the scientific literature. In this search antidiabetic, anti-diarrhoeal, anti-inflammatory, antioxidant and antimicrobial activities of 'jambolão' were described, among other actions.

Molecular hybridization: A useful tool in the design of new drug prototypes

Molecular hybridization is a new concept in drug design and development based on the combination of pharmacophoric moieties of different bioactive substances to produce a new hyrid compound with improved affinity and efficacy, when compared to the parent drugs. Additionally, this strategy can results in compounds presenting modified selectivity profile, different and/or dual modes of action and reduced undesired side effects. So, in this described several example of different strategies for drug design, discovery and pharmacomodulation focused on new innovative hybrid compounds presenting analgesic, anti-inflammatory, platelet anti-aggregating, anti-infections, anticancer, cardio- and neuroactive properties.

Bioprospecção de atividade antioxidante e antimicrobiana da casca de Stryphnodendron adstringens (Mart.) Coville (Leguminosae-Mimosoidae)

The aim of this work was to evaluate the class of secondary metabolites responsible for the antioxidant and antimicrobial activities of bark extracts of Stryphnodendron adstringens (Mart.) Coville (Leguminosae-Mimosoidae), a plant widely used in folk medicine in Brazil. Extracts of the bark were prepared with 50% ethanol, 70% ethanol, acetone:water (7:3, v/v) and chloroform. Antioxidant activity was prospected by spraying thin-layer chromatographs of the extracts with 2,2-diphenyl-1-picryl-hydrazyl (DPPH) and measuring the DPPH radical scavenging capacity by spectrophotometry. Antibacterial activity was revealed by the agar diffusion method and bioautography. TLC spots assigned to tannins in the polar extracts showed antioxidant activity by DPPH radical scavenging and the chloroform extract showed the least scavenging activity. Antimicrobial activity was indicated by the bacterial growth inhibition haloes around polar extracts and bioautography showed activity in the TLC spots assigned to tannins. It was concluded that polar extracts of the bark of S. adstringens possessed antioxidant and antimicrobial activities which were due to secondary metabolite derived from the tannin class, which are the main constituent of these bark extracts, according to the literature.

Myotoxic phospholipases A2 isolated from Bothrops brazili snake venom and synthetic peptides derived from their C-terminal region: Cytotoxic effect on microorganism and tumor cells

This paper reports the purification and biochemical/pharmacological characterization of two myotoxic phospholipases A2 (PLA2s) from Bothrops brazili venom, a native snake from Brazil. Both myotoxins (MTX-I and II) were purified by a single chromatographic step on a CM-Sepharose ion-exchange column up to a high purity level, showing Mr ∼ 14,000 for the monomer and 28,000 Da for the dimer. The N-terminal and internal peptide amino acid sequences showed similarity with other myotoxic PLA2s from snake venoms, MTX-I belonging to Asp49 PLA2 class, enzymatically active, and MTX-II to Lys49 PLA2s, catalytically inactive. Treatment of MTX-I with BPB and EDTA reduced drastically its PLA2 and anticoagulant activities, corroborating the importance of residue His48 and Ca2+ ions for the enzymatic catalysis. Both PLA2s induced myotoxic activity and dose-time dependent edema similar to other isolated snake venom toxins from Bothrops and Crotalus genus. The results also demonstrated that MTXs and cationic synthetic peptides derived from their 115-129 C-terminal region displayed cytotoxic activity on human T-cell leukemia (JURKAT) lines and microbicidal effects against Escherichia coli, Candida albicans and Leishmania sp. Thus, these PLA2 proteins and C-terminal synthetic peptides present multifunctional properties that might be of interest in the development of therapeutic strategies against parasites, bacteria and cancer. © 2008 Elsevier Inc. All rights reserved.

Determination of calcium and magnesium in hydroethanolic extracts of propolis by atomic absorption flame spectrophotometry

Propolis is a natural product collected by honeybees and has a large range of pharmacological activity, including antimicrobial, antitumoral, antioxidant and anti-inflammatory. Its use as a popular medicine is increasing all over the world, creating a need for quality control of the commercial products. In this study the levels of calcium and magnesium in commercial hydroalcoholic propolis extracts from varies states of Brazil were determined by atomic absorption flame spectrophotometry and different values were obtained for northern and southern states. This study can be extended to the analysis of metals that are harmful to health. The results showed that the calibration curves were linear over a wide concentration range (0.5-4.0 μg.mL -1 for calcium and 0.05-0.4 μg.mL -1 for magnesium) with good correlation coefficients (0.999 and 0.988, respectively). Good analytical recovery (94%) was obtained. The proposed method showed adequate precision and relative standard deviation lower than 2 %. The method is accurate and precise as well as having advantages such as simplicity and speed.

Atividade antioxidante e antimicrobiana do alecrim (Rosmarinus officinalis L.) em filés de tilápia (Oreochromis ssp) salgados secos durante o armazenamento congelado

Rosemary (Rosmarinus officinalis L.) is a spice from Lamiaceae family known since ancient times because its medicinal effects and, currently, several studies have pointed its antioxidant and antimicrobian effects. Lipid oxidation is a problem in food production because proceed the lost of organoleptical and nutritional qualities so required in Market. Fish salting is an ancient conservation method that expect reduce water activity and, consequently, microorganism growth in food, except halophillic bacteria. In the meantime, the inconvenient of this procedure is that the salt accelerates tissue's lipid oxidation. The aim of this work was evaluate the antioxidative and antimicrobian effects by treatment and pre treatment with rosemary (Rosmarinus officinalis L.) aqueous extract in dry salted tilapia fillets, storaged in freezing temperatures. To follow the oxidative, dry salted tilapia fillets were treated or pre treated with rosemary natural extract and storage at -18°C for 240 days. Analisys of 2-thiobarbituric acid reactive substances (TBARS), soluble nitrogen in trichloroacetic acid (TCA), water activity and microbiology were done. The pre treatment (3.39±0,53) and the treatment with rosemary (3.31±0.79) had oxidative index twice lower than the control treatment (6.14±1.21) in the last time of the research. The microbiological rosemary analisys showed count levels of resistant microorganisms to salt (2.0×103CFU/g of sample), whom causes the initial fillets contamination. The microbiological counts remained invariable in all groups during storage periods.

Verificação da atividade antibacteriana de sabonete líquido contendo extrato glicólico de Dimorphandra mollis Benth.

Dimorphandra mollis Benth., Compositae, false barbatimão, has been used topically as a healing, astringent and antibacterial. In this study, antibacterial activity was verified on liquid soap containing glycolic extract of D. mollis (DGE) at different concentrations (8, 15 and 20%) and at different pH levels (6 and 8). Five soap formulations (F) were prepared: F1 - tryclosan (0.1%), F2 - DGE (8%), F3 - DGE (15%), F4 - DGE (20%) and F5 - without preservatives. Bark of D. mollis were dried in a circulating air oven and ground. The rude extracts were prepared by turbo extraction with ethanol. After screening, the extract were concentrated in rotating evaporator, lyophilized and resuspended in propileneglycol to obtain the glycolic extract. The antimicrobial activity was verified by diffusion in agar method, using cylinder in plate. Plates containing Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli were incubated at 37°C for 24 hours. After incubation, the results were analysed with a pachymeter, observing the bacterial grouth inhibition halo diameter. It was verified that the liquid soap containing tryclosan caused on inhibition of bacterial growth at both pH levels; the soaps without preservatives and containing DGE, independently of the concentration and pH levels used, did not present antibacterial activity.