Franco Delle Monache

Sapienza University of Rome, Roma, Latium, Italy

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Publications (311)514.42 Total impact

  • [Show abstract] [Hide abstract] ABSTRACT: Drimys brasiliensis Miers (Winteraceae) is used in folk medicine for the treatment of cancer. Its anti-tumor activity has been demonstrated in vitro models using extracts and isolated compounds. This study investigates the cytotoxic effects of stem bark extracts of D. brasiliensis as well as isolated compounds that may be responsible for the activitys and evaluates them in leukemia cells. The stem bark extract were subjected to column chromatography, and the structures of compounds were elucidated based on spectroscopic methods by using NMR and infrared spectroscopy and GC/MS. The cytotoxicity of the isolated compounds was evaluated in chronic myeloid (K562) and acute B lymphoblastic (Nalm6) leukemia cells using tetrazolium assay (MTT). Two new compounds were isolated 1β-O-p-methoxy-E-cinnamoyl-5α-keto-11α-enol-albicanol (1a) and the isomer 1β-O-p-methoxy-E-cinnamoyl-5α-keto-11β-enol-albicanol (1b) and 1β-O-p-methoxy-E-cinnamoyl-isodrimeninol (2). The known compounds polygonal acid (3a) and the isomer isopolygonal acid (3b), fuegin (4a) and the isomer epifuegin (4b), the mixture drimanial (5) and 1β-O-(p-methoxy-E-cinnamoyl)-6α-hydroxypolygodial (6) were also isolated. The drimanes (1-4) and drimanial (5), 1β-(p-coumaroyloxy)-polygodial (7), 1β-(p-methoxycinnamoyl)-polygodial (8), and polygodial (9) isolated previously were assessed in tumor cells. The IC50 values were between 3.56 and 128.91 μM. 1-β-(p-cumaroiloxi)-polygodial showed the best result with IC50 8.18 and 3.56 μM by K562 and Nalm6, respectively. The chloroform extract of the stem bark of D. brasiliensis is a great source of drimane sesquiterpenes. Our experimental data suggest that drimanes are responsible for cytotoxicity activity demonstrated by this species, especially those with the aldehyde group linked to carbons C-11 and C-12.
    No preview · Article · Apr 2016 · Archiv für Experimentelle Pathologie und Pharmakologie
  • [Show abstract] [Hide abstract] ABSTRACT: Chrysophyllum cainito L. (Sapotaceae), commonly known as caimito or star apple, is a neotropical tree valued for its ornamental quality and edible fruits. Besides its culinary use, the leaves are also popularly used to treat diabetes mellitus and several inflammatory diseases.
    No preview · Article · Mar 2016 · Journal of ethnopharmacology
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    [Show abstract] [Hide abstract] ABSTRACT: Solidago chilensis Meyenmost (Asteraceae), popularly known as "Brazilian arnica" or "arnica-do-campo," is widely used in the folk medicine to treat gastric disorders. Based on this, the gastroprotective activity of S. chilensis methanolic extract was investigated. Besides, a phytochemical study allowed isolation of two flavonoids (quercitrin and afzelin). The gastroprotective effects were investigated in acute gastric ulcer models, and the antisecretory activity was assessed in vivo and in vitro. The adhered mucus levels, reduced glutathione (GSH) content and myeloperoxidase (MPO) activity were quantified in ulcerated tissues. The contribution of isolated compounds in extract effects was evaluated, and its doses were calculated according to its yield. To evaluate the in vivo healing properties of S. chilensis methanolic extract, a chronic gastric ulcer was induced in mice by 10 % acetic acid. Evaluation of tumor necrosis factor (TNF) levels was also performed at the site of the acetic acid-induced gastric ulcer. In parallel, effects on cell viability and cell proliferation of fibroblasts (L929 cells) were determined by in vitro trials. Firstly, the S. chilensis methanolic extract (100 or 300 mg/kg) reduced the ulcer area induced by ethanol/HCl in mice when compared to the vehicle group. Moreover, the S. chilensis extract (300 mg/kg) prevented the mucus depletion, the increase in MPO activity and the decrease in the GSH levels in the ulcerated gastric tissue. The S. chilensis extract also was able to decrease the indomethacin-induced gastric ulcer in rats at a dose of 100 mg/kg. The antisecretory effect of the extract (100 mg/kg, intraduodenal (i.d.)) was confirmed by the reduction in the volume and acidity in parallel to an increase in the pH of gastric content. In addition, quercitrin (1.38 mg/kg, but not 0.46 mg/kg) and afzelin (0.026 and 0.078 mg/kg) decreased the ethanol/HCl-induced gastric ulcer. In this model, quercitrin (1.38 mg/kg) prevented the depletion of gastric GSH content and both quercitrin (1.38 mg/kg) and afzelin (0.078 mg/kg) reduced the MPO activity. These compounds also inhibited the H(+),K(+)-ATPase activity at a concentration of 1-100 μg/ml. In addition, the participation of quercitrin and afzelin in these effects also was confirmed. Furthermore, after 4 days of the treatment, an oral administration of S. chilensis methanolic extract (100 mg/kg) reduced the area of the gastric ulcer induced by acetic acid and the regeneration of the gastric mucosa was accompanied by a reduction in gastric TNF levels. The healing properties of the extract also were confirmed by enhancement of proliferation and coverage of scratched wounds in a fibroblast monolayer. Together, our results confirmed the gastroprotective effect of S. chilensis methanolic extract as well as its gastric healing potential and provided some support to the traditional use of S. chilensis for prevention and treatment of gastric lesions in complementation to its known anti-inflammatory properties.
    Full-text · Article · Jan 2016 · Archiv für Experimentelle Pathologie und Pharmakologie
  • [Show abstract] [Hide abstract] ABSTRACT: Context Garcinia achachairu Rusby (Clusiaceae) popularly known as 'achachairu' is used in folk medicine to treat rheumatism, inflammation, pain and gastric disorder. Objective The present study investigated the chemical profile and antiproliferative effects of the methanolic extract, fractions and two xanthones, against some carcinoma cell lines in vitro. Materials and methods The compounds were isolated and identified by chromatographic and spectroscopic methods. The extract, fractions and compounds were tested human tumour cell lines of U-251 (glioma), MCF-7 (breast), NCI/ADR-RES (ovary expressing multi-drug resistance phenotype), 786-0 (kidney), NCI-H460 (lung, non-small cells), PC-3 (prostate) and HT-29 (colon), non-tumour cell line HaCat (human keratinocytes) in doses of 0.25-250 μg mL (-) (1) for 48 h. The antiproliferative activity was determined by spectrophotometric quantification (at 540 nm) of the cellular protein content using sulphorhodamine B assay. The prediction of parameters involved in the molecular bioavailability was executed directly by ChemDoodle (version 5.0.1) software (iChemLabs, LLC, Somerset, NJ). Results 3-Demethyl-2-geranyl-4-prenylbellidypholine (1) and 1,5,8-trihydroxy-4',5'-dimethyl-2H-pyrane (2,3:3,2)-4-(3-methylbut-2-enyl) xanthone (2), gartanin (3) and stigmasterol (4) were identified on the basis of spectroscopic techniques. Compounds 1 and 2 exhibited cytocidal activity, especially against breast, prostate and kidney cell lines, with TGI values of 15.8, 4.9, 9.1 and 39.4, 44.7, 40.9 μg/mL, respectively. Discussion and conclusion The presence of two sets of hydrophobic and hydrophilic groups in separate domains in each molecule might play a role in the mediation of tumour-specific action. Our data show that G. achachairu have potent antiproliferative action and should be considered an important source of potent anticancer compounds.
    No preview · Article · Dec 2015 · Pharmaceutical Biology
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    [Show abstract] [Hide abstract] ABSTRACT: This study shows the evaluation the antiproliferative effect of the extract, fractions, and uncommon compounds isolated from R. rosaefolius leaves. The compounds were identified by conventional spectroscopic methods such as NMR-H 1 and C 13 and identified as 5,7-dihydroxy-6,8,4′-trimethoxyflavonol ( 1 ), 5-hydroxy-3,6,7,8,4′-pentamethoxyflavone ( 2 ), and tormentic acid ( 3 ). Both hexane and dichloromethane fractions showed selectivity for multidrug-resistant ovary cancer cell line (NCI-ADR/RES) with total growth inhibition values of 11.1 and 12.6 μ g/ml, respectively. Compound 1 also showed selective activity against the same cell line (18.8 μ g/ml); however, it was especially effective against glioma cells (2.8 μ g/ml), suggesting that this compound may be involved with the in vitro antiproliferative action.
    Full-text · Article · Dec 2015 · Evidence-based Complementary and Alternative Medicine
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    [Show abstract] [Hide abstract] ABSTRACT: The genus Eugenia are used as feed. One of its species is Eugenia umbelliflora, which is used for its fruits. The aim of the study was to isolate the constituents of the CH2Cl2 fraction obtained from Eugenia umbelliflora O. Berg (Myrtaceae), and also to evaluate its antimicrobial properties. Two novel meroterpenoids, eugenial C (3) and eugenial D (4), were isolated from the unripe fruits of Eugenia umbelliflora, and their structures established mainly by extensive NMR spectroscopy. In previous studies, the CH2Cl2 extract showed significant antibacterial activity, this activity can be attributed to meroterpenoids isolated in this study. The compounds eugenial C and D exhibited potent activity against B. subtilis and S. aureus and different strains of MRSA, and similar activity to the antibiotics used in antimicrobial therapies. The results demonstrate the antimicrobial potential of compounds eugenial C and D isolated from the unripe fruits of Eugenia umbelliflora, these compounds showed equivalent activity to antibiotics commonly used in anti-infection therapy.
    Full-text · Article · Aug 2015 · Journal of Agricultural and Food Chemistry
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    [Show abstract] [Hide abstract] ABSTRACT: A new indole alkaloid strychnosinol (1) and a new phenolic-glycoside (2) were isolated from the bark and leaves of Strychnos fendleri Sprague & Sandwith, together with six known compounds reported for the first time in this species. The structures of these compounds were determined on the basis of spectroscopic data; mainly those obtained by using (1)H and (13)C NMR (1D and 2D) and mass spectrometry. Strychnosinol (1) and the phenolic glycoside (2) together with compounds 3-8 were evaluated for cytotoxicity against a panel of five tumour cell lines; IC50 values between 0.090 and 0.227 μM for the human tumour cell lines were observed for compound 2.
    Full-text · Article · Mar 2015 · Natural Product Research
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    [Show abstract] [Hide abstract] ABSTRACT: Abstract This paper describes the seasonal phytochemical variation and the antimicrobial potential of V. zizanioides roots collected in Brazil. Considering the high levels of chemical constituents and their biological activity in dichloromethane fraction, the plants were grown in different seasons and the respective dichloromethane fractions were analyzed by gas chromatography-mass spectrometry. The antimicrobial activity was evaluated against several pathogenic microorganisms by determining the minimum inhibitory concentration (MIC) using the agar dilution method. Yields of dichloromethane fractions from plants collected in the autumn and spring occurred in a higher proportion than in other seasons. Khusimol (2) was isolated by column chromatography and identified by NMR and CG-MS, along with other sesquiterpenes, including β-vetivenene (1), vetiselinenol (3), isovalencenol (4), vetivenic acid (5), α-vetivone (6) and β-vetivone (7). Some extracts showed promising antimicrobial effects, with MICs ranging from 31.25 to 500 μg mL-1. Kushimol was slightly active against the tested microorganisms.
    Full-text · Article · Dec 2014 · Acta Pharmaceutica
  • [Show abstract] [Hide abstract] ABSTRACT: Objectives Litchi chinensis has been traditionally used in folk medicine to treat several ailments. In this study, we investigated the chemical composition, antioxidant and antinociceptive activity of L. chinensis leaves.Methods The antioxidant capacity of the extract, fraction and compounds was evaluated using the 1,1-diphenyl-picrylhydrazyl (DPPH) and 2,2′-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays, and the liposome model with peroxyl radicals generated by 2,2′-azobis (2-amidinopropane) dihydrochloride radical. The pharmacological models of acute nociception used in mice were: writhing test with acetic acid (AA), hotplate (HP), glutamate (GLU), capsaicin (CP) and formalin (FM) tests.Key findingsThe main compounds isolated were procyanidin A2 (PA2), procyanidin B2 (PB2) and (–)-epicatechin. The biochemical features of the crude extracts and their ethyl acetate fraction (EtOAcFR) presented high antioxidant activity, and the antioxidant activity of PA2 and PB2 was remarkably high, with DPPH and ABTS. The crude methanol extract (MeOHEXTR), EtOAcFR and PB2 were effective in reducing nociception in FM and HP models. MeOHEXTR and EtOAcFR treatments also reduced pain induced by GLU and AA. In the CP model, only EtOAcFR and PB2 were effective.Conclusions The results demonstrate the antinociceptive and antioxidant of MeOHEXTR, EtOAcFR and PB2.
    No preview · Article · Oct 2014
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    [Show abstract] [Hide abstract] ABSTRACT: Previous phytochemical studies carried out with Rubus imperialis Chum. Schl. (Rosaceae) have demonstrated the presence of triterpenes (niga-ichigoside F1 and 2β,3β,19α-trihydroxyursolic acid) in this species. The literature indicates that triterpenes are closely related to some pharmacological activities, including antiulcer activity. Therefore, in view of the previous promising results with this species, this work extends the phytochemical studies, as well as investigates its gastroprotective action in different models using rodents. The hydroalcoholic extract was tested using the following protocols in mice: ethanol/HCl and nonsteroidal anti-inflammatory drug (NSAID)-induced ulcer, acetic acid-induced chronic ulcer, ligature pylorus model, and free mucus quantification in mucosa. Isolated triterpenes were investigated in the ethanol/HCl-induced ulcer model. The results of this study show that R. imperialis extract (100, 250, or 500 mg) displays gastroprotective activity in the ethanol-induced ulcer model with a percentage of inhibition of gastric lesions of 70, 71, and 86 %, respectively. The extract also significantly reduced the ulcerative lesions in the indomethacin-induced ulcer. In this model, the percentage of inhibition of ulcer was 41, 44, and 70 %, respectively. Regarding the model of gastric secretion, a reduction of gastric juice volume and total acidity was observed, as well as an increase in gastric pH; however, gastric mucus production was not altered by treatment with the extract. It was also observed that the ethyl acetate fraction presented higher activity, leading to the isolation of niga-ichigoside F1 and 2β,3β-19-α-trihydroxyursolic acid, which presented antiulcer activity comparable to that of omeprazole, with an inhibition percentage of 98 and 99 %, respectively. These results demonstrate that R. imperialis extract and isolated compounds (niga-ichigoside F1 and 2β,3β-19-α-trihydroxyursolic acid) produce gastroprotective effects, and this activity seems, at least in part, to be related to antisecretory effects.
    Full-text · Article · Jan 2014 · Archiv für Experimentelle Pathologie und Pharmakologie
  • [Show abstract] [Hide abstract] ABSTRACT: Chrysophyllum cainito, popularly known as "star apple", caimito, "abiu-roxo" or "abiu-do-Pará", is a tree of about 25m in height. Besides its culinary use, it is also used in fork medicine for the treatment of diabetes mellitus and several inflammatory diseases. The crude methanolic extract (CME) was submitted to phytochemical studies for obtaining fractions and isolated compounds. They were monitored by thin-layer-chromatography (TLC). The biological activity was evaluated in mice using the carrageenan-induced mechanical hypersensitivity and paw oedema. Biochemical assays, such as myeloperoxidase (MPO) and activity and cytokines levels quantification, were carried out to analyse the involvement of neutrophil migration and IL-1β and TNFα production. Some adverse effects were investigated using the open-field and rota-rod tests, and it was also measured the rectal temperature. This study demonstrates, for the first time, the anti-hypersensitivity and anti-inflammatory effects of CME, fractions and two isolated triterpenes obtained from the leaves of C. cainito on carrageenan-induced hypersensitivity and paw-oedema. The mice treated with CME or chloroform fraction (CHCl3) presented reduction in mechanical hypersensitivity. The effect of the CME seemed to be partially related to the anti-inflammatory activity, as the paw-oedema and MPO activity were also significantly inhibited. The isolated compound Lup-20(29)-en-3β-O-hexanoate demonstrated more reduction of the hypersensitivity than 3β-Lup-20(29)-en-3-yl acetate, suggesting that this molecule might be partially responsible for the biological effects obtained with CME and CHCl3 fractions. Finally, animals treated with CME and CHCl3 did not present changes in locomotor activity, motor performance or body temperature. Our data demonstrates, for the first time, that the crude extract, fractions and pure compounds obtained from the C. cainito leaves possess important anti-hypersensitive properties against inflammatory pain in mice. The mechanisms through which C. cainito exerts its anti-hypersensitive actions are still unclear, and require further investigation; however, this could well constitute a new and attractive alternative for the management of persistent inflammatory and neuropathic pain in humans.
    No preview · Article · Dec 2013 · Journal of ethnopharmacology
  • [Show abstract] [Hide abstract] ABSTRACT: As part of the program of our research group to search for new and effective substances from the Brazilian biodiversity, the present work evaluates the antibacterial activity of four species from the Brazilian flora (Garcinia achachairu, Macrosiphonia velame, Rubus niveus and Pilea microphylla) against Bacillus subtilis, Staphylococcus aureus and S. saprophyticus (Gram-positive bacteria), Escherichia coli (Gram-negative bacterium) and Candida albicans (yeast). The extracts of R. niveus and M. velame showed promising antibacterial activity with MICs, ranging from 1000 to 125 microg/mL. Bio-guided fractionation of M. velame yielded four compounds, with the highest inhibition being observed for compound 3, with a MIC of 125 microg/mL against S. aureus. The combinations of fractions 2 and 4 showed beneficial effect against Gram-positive bacteria (additive effect), suggesting a possible synergistic effect.
    No preview · Article · Nov 2013 · Natural product communications
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    [Show abstract] [Hide abstract] ABSTRACT: Protein tyrosine phosphatase B (PtpB) is one of the virulence factors secreted into the host cell by Mycobacterium tuberculosis. PtpB attenuates host immune defenses by interfering with signal transduction pathways in macrophages and, therefore, it is considered a promising target for the development of novel anti-tuberculosis drugs. Here we report the discovery of natural compound inhibitors of PtpB among an in house library of more than 800 natural substances by means of a multidisciplinary approach, mixing in silico screening with enzymatic and kinetics studies and MS assays. Six natural compounds proved to inhibit PtpB at low micromolar concentrations (< 30 µM) with Kuwanol E being the most potent with K i = 1.6 ± 0.1 µM. To the best of our knowledge, Kuwanol E is the most potent natural compound PtpB inhibitor reported so far, as well as it is the first non-peptidic PtpB inhibitor discovered from natural sources. Compounds herein identified may inspire the design of novel specific PtpB inhibitors.
    Preview · Article · Oct 2013 · PLoS ONE
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    [Show abstract] [Hide abstract] ABSTRACT: This paper evaluates CHCl3 and CH3OH extracts of the stem bark, branches and leaves of Drimys brasiliensis and drimane sesquiterpenes isolated from the stem bark against strains of Leishmania amazonensis and Leishmania braziliensis promastigotes and Plasmodium falciparum trophozoites. All of the extracts and compounds were tested in cell lines in comparison with reference standards and cell viability was determined by the XTT method. The CHCl3 and CH3OH extracts from the stem bark and branches yielded promising results against two strains of Leishmania, with 50% inhibitory concentrations (IC50 ) values ranging from 39-100 µg/mL. The CHCl3 extract of the stem bark returned IC50 values of 39 and 40.6 µg/mL for L. amazonensis and L. braziliensis, respectively. The drimanes were relatively effective: 1-β-(p-coumaroyloxy)-polygodial produced IC50 values of 5.55 and 2.52 µM for L. amazonensis and L. braziliensis, respectively, compared with 1-β-(p-methoxycinnamoyl)-polygodial, which produced respective IC50 values of 15.85 and 17.80 µM. The CHCl3 extract demonstrated activity (IC50 of 3.0 µg/mL) against P. falciparum. The IC50 values of 1-β-(p-cumaroyloxyl)-polygodial and 1-β-(p-methoxycinnamoyl)-polygodial were 1.01 and 4.87 µM, respectively, for the trophozoite strain. Therefore, the results suggest that D. brasiliensis is a promising plant from which to obtain new and effective antiparasitic agents.
    Full-text · Article · Apr 2013 · Memórias do Instituto Oswaldo Cruz
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    [Show abstract] [Hide abstract] ABSTRACT: This study was undertaken to evaluate the gastroprotective properties of seed, leaf, and branch methanolic extracts and guttiferone A obtained from Garcinia achachairu (Clusiaceae). Mice were used in all the models, and treatments were administered orally only in pylorus-ligated model of the extracts, and drugs were administered intraduodenally. Treatment with different extracts (500 mg/kg) significantly reduced the ulcerative lesions in the ethanol/HCl-induced model; however, the seed extract was most active. When tested in different doses (50, 250, or 500 mg/kg), the seed extract of G. achaicharu showed a dose-dependent effect with a percentage of inhibition of gastric lesions of 41, 49, and 85 %, respectively. The seed extract also significantly reduced the ulcerative lesions in the indomethacin/bethanechol-induced ulcer. In this model, the percentage of inhibition of ulcer was 24, 58, and 90 %, respectively. Regarding the model of gastric secretion, a reduction of gastric juice volume and total acidity was observed, as well as an increase in gastric pH. Considering that the seed extract was the most active, it was subjected to silica gel column chromatography, leading to the isolation of guttiferone A. The isolated compound and omeprazole were evaluated in the HCl/ethanol-induced ulcer model. In this assay, both compounds at a dose of 30 mg/kg reduced the ulcerative lesions by about 75 %. These results demonstrate, for the first time, that extracts obtained from G. achachairu and guttiferone A produce gastroprotective effects, corroborating ethnomedicinal use of this plant.
    Full-text · Article · Aug 2012 · Archiv für Experimentelle Pathologie und Pharmakologie
  • [Show abstract] [Hide abstract] ABSTRACT: In a search for new and effective analgesic substances from the Brazilian biodiversity, the present study evaluates the chemical composition and antinociceptive potential of the methanol extract and a pure compound obtained from the seeds of Garcinia achachairu Rusby (Clusiaceae). The methanolic seed extract was directly subjected to purification by column chromatography and the purification was monitored by thin-layer chromatography. The main isolated compound was identified as Guttiferone A by comparison of conventional spectroscopic data (IR, NMR-(1)H and (13)C) to the literature data which was isolated for the first time from this plant. When evaluated in the acetic acid-induced nociception model in mice, the methanolic seed extract had an ID(50) (Inhibitory dose) of 13.1 (11.23-14.91) mg/kg and a maximal inhibition of 72 ± 4%. In the same model, Guttiferone A had an ID(50) of 4.54 (3.29-6.24) mg/kg and a maximal inhibition of 73 ± 5%. The methanolic seed extract and Guttiferone A were also active in pain models induced by formalin, capsaicin, glutamate and carrageenan. These data suggest that the antinociceptive effect of Guttiferone A partly depends on its interference with the synthesis or activity of the cytokine TNF-α, the keratinocyte-derived chemokine KC, and/or PGE(2). These data support, at least in part, the use of G. achachairu in folk medicine and suggest that this plant is an important source of compounds with a suitable profile for development as new and effective medicinal agents to treat pain processes.
    No preview · Article · Mar 2012 · Archives of Pharmacal Research
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    [Show abstract] [Hide abstract] ABSTRACT: Two regioisomeric meroterpenoids, Eugenial A and B, have been isolated from the fruits of Eugenia multiflora and their structures established on the basis of NMR evidences. They possess a phloroglucinol-monoterpene structure similar to the euglobals occurring in the sister genus Eucaliptus. A simple method to distinguish between regioisomeric pairs was pointed.
    Full-text · Article · Feb 2012 · Natural product research
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    [Show abstract] [Hide abstract] ABSTRACT: a b s t r a c t Litsea guatemalensis Mez., a native plant of Mexico and Central America, is widely used as a food condi-ment, in the same manner as Laurus nobilis L. In folk medicine, it is used to treat several diseases such as respiratory and gastrointestinal complaints. We report here the anti-inflammatory and anti-hyperalgesic properties of ethanolic extract and the compound 5,7,3 0 ,4 0 -tetrahydroxy-isoflavone (3), which was iso-lated in addition to pinocembrin (1), and scopoletin (2). The results confirm that both the ethanolic extract and Compound 3 showed anti-inflammatory activity, by inhibiting paw oedema induced by car-rageenan, and also reduced the influx of leucocytes, particularly neutrophils, to the pleural cavity and consequently anti-hyperalgesic activity, when assessed in the model of persistent pain induced by partial sciatic nerve ligation.
    Full-text · Dataset · Jan 2012
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    [Show abstract] [Hide abstract] ABSTRACT: From the stems of Croton micans Sw., five new 3,4-seco-ent-kaurene dimers: micansinoic acid (1), isomicansinoic acid (2), and the dimethyl (3), monomethyl (4) and monoethyl ester (5) of micansinoic acid were isolated. The structures of the new compounds were elucidated by spectroscopic data interpretation, mainly 1D and 2D NMR experiments and MS. These compounds are the first 3,4-seco-ent-kaurene dimers from a Croton species.
    Full-text · Article · Jan 2012 · Natural product communications
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    [Show abstract] [Hide abstract] ABSTRACT: The increase in antibiotic resistance due to multiple factors has encouraged the search for new compounds which are active against multidrug-resistant pathogens. In this context, chalcones, dihydrochalcones, hydrazones and oxadiazoles were tested against Staphylococcus aureus ATCC 25923 and methicillin-resistant S. aureus (MRSA) isolates, which were obtained from clinical laboratories and were characterized as MRSA using traditional and molecular methods. Among 65 tested compounds, two chalcones, one dihydrochalcone and two hydrazones were active against MRSA. Based on the minimal inhibitory concentration and cytotoxicity, hydrazones provided a better selectivity index than chalcones. Active hydrazones are promising antibiotic-like substances and they should be the subject of further microbiological studies.
    Full-text · Article · Nov 2011 · Bioorganic & medicinal chemistry letters

Publication Stats

5k Citations
514.42 Total Impact Points

Institutions

  • 2011
    • Sapienza University of Rome
      Roma, Latium, Italy
  • 2010
    • National Institute of Geophysics and Volcanology
      Roma, Latium, Italy
  • 1994-2010
    • University of Santiago, Chile
      • Departamento de Ingeniería Química
      CiudadSantiago, Santiago, Chile
    • Federal University of Rio de Janeiro
      • Núcleo de Pesquisa de Produtos Naturais (NPPN)
      Rio de Janeiro, Rio de Janeiro, Brazil
  • 2008
    • University Center for the Development of High Vale and Itajai
      Itajahy, Santa Catarina, Brazil
  • 2006
    • Federal University of Santa Catarina
      Nossa Senhora do Destêrro, Santa Catarina, Brazil
  • 1976-2002
    • Università Cattolica del Sacro Cuore
      Milano, Lombardy, Italy
  • 1971-2001
    • Catholic University of the Sacred Heart
      • Institute of Biochemistry and Clinical Biochemistry
      Milano, Lombardy, Italy
  • 1995
    • Universidade Federal de Santa Maria
      • Department of Chemical Engineering (DEQ)
      Santa Maria, Estado do Rio Grande do Sul, Brazil
  • 1989
    • Központi Élelmiszer-tudományi Kutatóintézet
      Budapeŝto, Budapest, Hungary
  • 1972
    • University of Buenos Aires
      • Faculty of Pharmacy and Biochemistry
      Buenos Aires, Buenos Aires F.D., Argentina