Irwin Alencar Menezes - Academia.edu (original) (raw)
Papers by Irwin Alencar Menezes
African journal of pharmacy and pharmacology
Caryocar coriaceum Wittm. (pequi) has been popularly used in Northeastern Brazil in the treatment... more Caryocar coriaceum Wittm. (pequi) has been popularly used in Northeastern Brazil in the treatment of inflammation, pain and respiratory affections. This study evaluated the topical anti-inflammatory activity of C. coriaceum hydroethanolic extract (CCHE) and methanolic fraction (CCMF) from pequi tree leaves against different skin sensitizer agents (arachidonic acid, croton oil, phenol and histamine), as well their antioxidant activity and phenolic compound profile. High performance liquid chromatography with diode array detection (HPLC-DAD) analysis pointed the presence of chlorogenic acid, rutin, quercetin and lower concentrations of caffeic and gallic acids. Both CCHE and CCMF 1 mg/ear demonstrated significant topical anti-inflammatory effect against arachidonic acid, phenol and histamine single application (antiedematous effect ranging from 48 to 69% for CCHE and 36 to 64% for CCMF; P < 0.05 vs. negative control). In contrast, both extracts did not antagonize the croton oil sin...
Raphiodon echinus (R. echinus) is used in Brazilian folk medicine for the treatment of inflammat... more Raphiodon echinus (R. echinus) is used in Brazilian folk medicine for the treatment of inflammation, coughs, and infectious diseases. However, no information is available on the
potential antioxidant, cytotoxicity and genotoxicity of this plant. In this study, the polyphenolic constituents, antioxidant capacity and potential toxic effects of aqueous and ethanolic extracts of
R. echinus on human erythrocytes and leukocytes were investigated for the first time. R. echinus extracts showed the presence of Gallic, chlorogenic, caffeic and ellagic acids, rutin, quercitrin and quercetin. Aqueous and ethanolic extracts of R. echinus exhibited antioxidant activity in DPPH
radical scavenging with IC50 = 111.9 μg/mL (EtOH extract) and IC50 = 227.9 μg/mL (aqueous extract). The extracts inhibited Fe2+ (10 μM) induced thiobarbituric acid reactive substances (TBARS) formation in rat brain and liver homogenates. The extracts (30–480 μg/mL) did not induce genotoxicity, cytotoxicity or osmotic fragility in human blood cells. The findings of this present study therefore suggest that the therapeutic effect of R. echinus may be, in part, related to its antioxidant potential. Nevertheless, further in vitro and in vivo studies are required to ascertain the safety margin of its use
in folk medicine.
American Fern Journal, 2012
Chagas disease is caused by Trypanosoma cruzi, and is considered a public health problem. The cur... more Chagas disease is caused by Trypanosoma cruzi, and is considered a public health problem. The current treatments for this disease are the synthetic drugs nifurtimox and benzonidazol, which are highly toxic. Pityrogramma calomelanos, a plant used in traditional medicine as an astringent, analgesic, anti-hemorrhagic, pectoral depurative, emmenagogue, anti-hypertensive, anti-pyretic and an anti-tussive was tested for antiepimastigote activity in vitro. An ethanol extract and hexane fraction of P. calomelanos was prepared and tested against T. cruzi (CL-B5 clone). The effective concentration capable of killing 50% of parasites (EC 50 ) was 55.26 mg/mL and 73.57 mg/mL for the ethanol extract and hexane fraction, respectively. This is the first record of tripanocidal activity for P. calomelanos. Our results indicate that P. calomelanos could be a source of antiepimastigote natural products with only moderate toxicity toward healthy human cells.
Acta Biológica Colombiana, 2015
Tropidurus hispidus has been used in traditional medicine in several regions of Northeastern Regi... more Tropidurus hispidus has been used in traditional medicine in several regions of Northeastern Region of Brazil. Its medicinal use
involves the treatment of diseases such as warts, sore throat, tonsillitis, chicken pox, varicella, measles, asthma, alcoholism, and
dermatomycosis.The present study evaluated the topical anti-inflammatory activity of Tropidurus hispidus fat in treating ear edema
in an animal model. Oil from T. hispidus (OTH) was evaluated on its effect against experimental inflammation in mice. OTH was
extracted frombody fat located in the ventral region of Tropidurus hispidus using hexane as a solvent.We used themodel of mouse
ear edema induced by phlogistic agents, croton oil (single and multiple applications), arachidonic acid, phenol, capsaicin, and
histamine, applied into the right ears of animals pretreated with acetone (control), dexamethasone, or OTH. OTH inhibited the
dermatitis induced by all noxious agents, except capsaicin. This effect may be related to the fatty acids present in OTH.
Duguetia furfuraceais frequently used as a medicinal plant in Brazil. However, studies have evide... more Duguetia furfuraceais frequently used as a medicinal plant in Brazil. However, studies have evidenced its cytotoxic, bactericide, and antitumor activities. In the present study we aimed to evaluate the potential toxicity of hydroalcoholic leaves extracts ofD. furfuracea (HEDF) in aDrosophila melanogastermodel. Toxicity was assessed as changes in locomotor performance, mitochondrial activity,
oxidative stress, MAPKs phosphorylation, and apoptosis induction after exposure to HEDF concentrations (1–50 mg/mL) for 7 days. The phytoconstituents of the plant were screened for the presence of alkaloids, tannins, xanthones, chalcones, flavonoids, aurones,
and phenolic acids. Exposure of adult flies to HEDF caused mitochondrial dysfunction, overproduction of ROS, and alterations inthe activity of detoxifying enzymes GST, SOD and CAT. Induction of ERK phosphorylation and PARP cleavage was also observed, indicating occurrence of HEDF-induced cell stress and apoptotic cell death. In parallel, alterations in cholinesterase activity and impairments in negative geotaxis behavior were observed. Our study draws attention to the indiscriminate use of this plant by population and suggests oxidative stress asa major mechanism underlying its toxicity.
Background: The challenge of antibiotic resistance and the emergence of new infections have gener... more Background: The challenge of antibiotic resistance and the emergence of new infections have generated considerable interest in the exploration of natural products from plant origins as combination therapy. In this context, crude ethanolic extract (CEE), ethyl acetate fraction (EAF), and methanolic fraction (MF) from Anacardium microcarpum were tested alone or in combination with antibiotics (amikacin, gentamicin, ciprofloxacin, and imipenem) against Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus.
Methods: Antibiotic resistance-modifying activity was performed using the microdilution method by determining the minimal inhibitory concentration (MIC). In addition, phytochemical prospecting analyses of tested samples were carried out. Results: Our results indicated that all the extracts showed low antibacterial activity against multidrug-resistant strains (MIC =512 µg/mL). However, addition of CEE, EAF, and MF to the growth medium at the subinhibitory concentration (MIC/8=64 µg/mL) significantly modulated amikacin- and gentamicin-resistant E. coli 06. CEE and EAF also demonstrated a
significant (P,0.001) synergism with imipenem against S. aureus. In contrast, MF antagonized the antibacterial effect of ciprofloxacin and gentamicin against P. aeruginosa 03 and
S. aureus 10, respectively. Qualitative phytochemical analysis of the extracts revealed the
presence of secondary metabolites including phenols, flavonoids, xanthones, chalcones, and
tannin pyrogallates.
Conclusion: Taken together, our results suggest that A. microcarpum is a natural resource with
resistance-modifying antibacterial activity that needs to be further investigated to overcome the
present resistant-infection problem.
European Journal of Medicinal Chemistry, 1999
Background: The challenge of antibiotic resistance and the emergence of new infections have gener... more Background: The challenge of antibiotic resistance and the emergence of new infections have generated considerable interest in the exploration of natural products from plant origins as combination therapy. In this context, crude ethanolic extract (CEE), ethyl acetate fraction (EAF), and methanolic fraction (MF) from Anacardium microcarpum were tested alone or in combination with antibiotics (amikacin, gentamicin, ciprofloxacin, and imipenem) against Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus.
Methods: Antibiotic resistance-modifying activity was performed using the microdilution method by determining the minimal inhibitory concentration (MIC). In addition, phytochemical prospecting analyses of tested samples were carried out.
Results: Our results indicated that all the extracts showed low antibacterial activity against multidrug-resistant strains (MIC =512 μg/mL). However, addition of CEE, EAF, and MF to the growth medium at the subinhibitory concentration (MIC/8=64 μg/mL) significantly modulated amikacin- and gentamicin-resistant E. coli 06. CEE and EAF also demonstrated a significant (P,0.001) synergism with imipenem against S. aureus. In contrast, MF antagonized the antibacterial effect of ciprofloxacin and gentamicin against P. aeruginosa 03 and S. aureus 10, respectively. Qualitative phytochemical analysis of the extracts revealed the presence of secondary metabolites including phenols, flavonoids, xanthones, chalcones, and tannin pyrogallates.
Conclusion: Taken together, our results suggest that A. microcarpum is a natural resource with resistance-modifying antibacterial activity that needs to be further investigated to overcome the present resistant-infection problem.
This work aims to record the therapeutical practices of the community Catolé utilizing local dive... more This work aims to record the therapeutical practices of the community Catolé utilizing local diversity of medicinal plants
verifying the versatility of the species, consensus usage and knowledge of the informants. Were recorded 46 native species for medicinal
purposes, belonging to 42 genres and 26 families, highlighting Fabaceae. Ten specimens exhibited great versatility of use, however
Ximennia americana L. and Croton heliotropiifolius Kunth showed the highest values of IR (2.0 and 1.65). The Therapeutic uses were
grouped in 15 categories of bodily systems, with higher factor consensus among informants in: Infectious and parasitic diseases (1.0),
disorder of the respiratory system (0.82) and Endocrine, nutrition and of metabolism (0.81). Due to the diversity of native species registered,
it can be concluded that the preservation of these areas is of great importance for biodiversity conservation site and the informants involved have a vast knowledge of the vegetation contributing to the knowledge of potentially useful plants of the cerrado.
The Cluster Analysis is a type of pattern recognition applicable to the drug design. In this pape... more The Cluster Analysis is a type of pattern recognition applicable to the drug design. In this paper, we present an agglomerative classification model in order to group substituents on the basis of similarities of their physical and chemical parameters. Once grouped, we investigate the relationship between the hierarchical model and the biological responses of compounds from the Quantitative Structure-Activity Relationship (QSAR). The method is then implemented by a new algorithm, called Winclus, for which we developed a dedicated software. This work addresses the software development and the application to a series of indole-2-carboxylate with anticonvulsant activity, described in the literature. The study was seeking to establish a relationship between groups of substituents (derived from the proposed model) and the biological activities of compounds already synthesized. To this end, we used the graphical form of dendrogram and offered the developed program as a tool in the design of new biologically active compounds.
European Journal of Medical Chemistry, 1999
A new agglomerative (bottom-up) hierarchical cluster technique referred to as the Adaptive Mean-L... more A new agglomerative (bottom-up) hierarchical cluster technique referred to as the Adaptive Mean-Linkage algorithm is derived. Cluster algorithms are also offered as a tool to explore the descriptor space knowing the quantitative structure–activity relationship (QSAR). The substituents are clustered building a dendrogram (cluster tree) per site. Choosing appropriate pathways on such cluster trees according to the QSAR equation, an automated search for potentially active substituted compounds can be performed. Applications to a series of substituted phenylguanidines with anticancer activity are focused illustrating this approach.
The medicinal plants and natural products are products with a great scientific interest due their... more The medicinal plants and natural products are products with a great scientific
interest due their possible use like phytodrugs. In this context, the
phytochemical composition and the antibacterial and antibiotic modulatory
activity of the extract and fractions of Annona squamosa against Staphylococus
aureus and Escherichia coli were performed. All natural products have not
showed clinically relevant antibacterial activity, with MIC ≥ 1024 mg/mL.
However, the extract combined with some aminoglycoside showed a synergistic
effect against multiresistant strains E. coli 27 and S. aureus 358. Due these
results, A. squamosa (Annonaceae) must be more studied to be used as a
source of natural products with adjuvant potential to enhance the antibiotic
activity, combating by this way the microbial antibiotic resistance
Bowdichia virgilioides (Fabaceae - Papilionoidea), popularly known as Sucupira-preta, is a Brazil... more Bowdichia virgilioides (Fabaceae - Papilionoidea), popularly known as Sucupira-preta, is a Brazilian native tree used in the traditional medicine against throat infections. Due this fact and due the interest to validate the traditional use, the objective of this work was evaluates the in vitro antibacterial activity of extracts and fractions of the stem and heartwood of the plant. The phytochemical profile revealed the presence of tannins and flavonoids in the stem and heartwood, and only alkaloids in the stem.The HPLC analysis revealed the presence of flavonoids and phenolic acids, natural products with several biological activities, including the modifying antibiotic activity. All microrganisms were inhibited only with MIC ≥ 1024 μg/mL. However, when associated with aminoglycosides, was demonstrated a potentiation of these antibiotics when associated with almost all products assayed and against one bacterium at least.
A doença de Chagas e a leishmaniose são doenças que prevalecem em países pobres. Os fármacos disp... more A doença de Chagas e a leishmaniose são doenças que prevalecem em países pobres. Os fármacos disponíveis para o tratamento dessas doenças são altamente tóxicos, sendo este um dos motivos que dificulta à adesão terapêutica e, assim, levando à busca por novas drogas eficazes e seguras para seus tratamentos. A pesquisa utilizando produtos naturais tem se mostrado uma alternativa na procura de novos compostos com potencial clínico-terapêutico. O gênero Passiflora possui as seguintes atividades farmacológicas centrais como calmantes, sedativas, ansiolíticas e indutor do sono e atividades antiparasitarias. A Passiflora cincinnata possui ampla distribuição pelo Brasil sendo popularmente utilizada para distúrbios de sono. Neste estudo avaliamos sua atividade antiparasitária contra Leishmania brasiliensis, Leishmania infantum e Trypanosoma cruzi, bem como sua citotoxicidade em fibroblastos. Foram testados extratos hidroalcoólicos obtidos das folhas, casca, sementes e caule em diferentes concentrações. Os extratos das folhas, casca e sementes não foram eficazes contra L. brasiliensis e T. cruzi, porém, o extrato do caule promoveu uma inibição de 29,12 % contra T. cruzi numa concentração de 500 μg/mL, entretanto o extrato da casca de P. cincinnata foi o que apresentou a melhor atividade contra as formas parasitárias de L. infantum, causando um percentual de morte >20 % nas concentrações de 250 a 1000 μg/mL. Referente à toxicidade, o extrato das folhas foi o que apresentou maior citotoxicidade, quando comparado com os demais, causando a mortalidade de 68,63 % dos fibroblastos numa concentração de 1000 μg/mL. A baixa citotoxicidade revelada abre espaço para novos estudos biológicos
The specie Lippia gracilis Schauer is largely utilized for their antimicrobial properties, which ... more The specie Lippia gracilis Schauer is largely utilized for their antimicrobial properties, which
are attributed to the presence of phenolic monoterpenes such as thymol and carvacrol. The aim of this study
was to determine the yields and chemical composition of the essential oils obtained from fresh and dry leaves
of collected at different times in the city of Crato-CE, in January 2009. The essential oils were extracted by
hydrodistillation, and its components were identified by gas chromatography coupled with mass
spectrophotometry. The time of plant collection should coincide with the moment of greatest expression of the
active principle.
Ethnopharmacological relevance: Ethnobotanical studieshavecontributedsignificantly inresearchof p... more Ethnopharmacological relevance: Ethnobotanical studieshavecontributedsignificantly inresearchof
plants withtherapeuticpotential.Theaimofthepresentstudywastolearnabouttheuseofnative
medicinal plantscitedbythetraditionalpopulationin “cerradão” (savannawoodland)areasinNortheast
Brazil, providingdataontherapeuticindicationsofthespeciesusedandtheirversatility.
Materials andmethods: Semi-structured interviewswereconductedonthebasisofastandardized
questionnairedesignedforkeyinformantsselectedusingthe “snowball” technique.Theselectionof
plants specieswiththerapeuticpotentialwasperformedonthebasisoftherelativeimportance(RI)and
informant consensusfator(ICF).
Results: A totalof78specieswereindicatedfor87therapeuticpurposes.Ofthese,11speciespresented
great versatilityofuse(RI41), ase.g.including Copaiferalangsdorffii Desf., Hybanthus calceolaria (Mart.)
Plumel., Heliotropium cf. indicum L., Crotonzehntneri, Crotonheliotropiifolius, Myracrodruonurundeuva,
Stryphnodendrorotundifolium. MedicinalusescouldbegeneralizedPax&K.Hoffmand Hymenaea
courbaril L. Thetherapeuticindicationsweregroupedinto14use15categorieswith594species–category
combinations. Thelargestnumberofmedicinalspecieswasindicatedforillnessesorundefined pain,
followedbydiseasesassociatedwithrespiratory,digestiveandgenitourinaryofbodysystems.Thefactor
informant consensushighlightedtheagreementintheuseofplantsandshowedthatthe,ofwhich
Diseases oftheNervousSystemand,DiseasesoftheCirculatorySystemhadthegreatestagreement
1.0and0.87repectively,DisordersoftheVisualSensorySystem – EyesandRespiratorySystemDisorder
showedthehighestagreementofuse.
Conclusions: Most ofthespeciescitedbythekeyinformantsarewellknownscientifically,butitis
interestingthatsomehavebeenstudiedlittleornotallwithregardtoconfirming theirpurported
medicinal propertiesandcancontributesubstantiallytopharmacologicalandphytochemicalinvestiga-
tions inthesearchfornewdrugs.
Lippia alba is empirically used for infusions, teas, macerates, and hydroalcoholic extracts becau... more Lippia alba is empirically used for infusions, teas, macerates, and hydroalcoholic extracts because of its antispasmodic,
analgesic, sedative, and anxiolytic effects. Citral is a mixture of trans-geranial and cis-neral and is the main constituent of L. alba
essential oil and possesses analgesic, anxiolytic, anticonvulsant, and sedative effects. The present study evaluated the effects
of the essential oil of L. alba (EOLa) and citral on compound action potentials (CAPs) in Wistar rat sciatic nerves. Both drugs
inhibited CAP in a concentration-dependent manner. The calculated half-maximal inhibitory concentrations (IC50) of peak-topeak
amplitude were 53.2 mg/mL and 35.00 mg/mL (or 230 mM) for EOLa and citral, respectively. Peak-to-peak amplitude of the
CAP was significantly reduced by 30 mg/mL EOLa and 10 mg/mL citral. EOLa and citral (at 60 and 30 mg/mL, values close to
their respective IC50 for CAP blockade) significantly increased chronaxy and rheobase. The conduction velocity of the first and
second CAP components was statistically reduced to B86% of control with 10 mg/mL EOLa and B90% of control with 3 mg/mL
citral. This study showed that EOLa inhibited nerve excitability and this effect can be explained by the presence of citral in its
composition. Both EOLa and citral showed inhibitory actions at lower concentrations compared with other essential oils and
constituents with local anesthetic activity. In conclusion, these data demonstrate that EOLa and citral are promising agents in
the development of new drugs with local anesthetic activity.
The use of medicinal plants is widespread around the world including Brazil, where there are seve... more The use of medicinal plants is widespread around the world including Brazil, where there are several species and a large tradition in their use. It was
aimed to know the perception of the nurses about the use of phytotherapy in Health Family Strategy (HFS). Exploratory descriptive study, qualitative
approach, developed in Crato-CE with fifteen nurses from HFS. It was employed the Theme-Category Analysis. It were constructed six categories and two
subcategories which were described the knowledge of professionals about phytotherapy, their views about use in primary care, the use of this practice and
the strategies developed for this use. The results revealed that the knowledge of the interviewees mostly is narrow and informal, and they find difficulties
to implement phytotherapic practices such as no valuation by the management and the rest of the health group. It should be emphasized as well the
importance of developing strategies that enable the safe and efficient integration of phytotherapy in care and thus the appreciation of local culture
The rising of the drug resistant microrganisms and the toxicity related with the antimicrobial dr... more The rising of the drug resistant microrganisms and the toxicity related with the antimicrobial drugs enhances the necessity about
the search of new bioactive compounds. Morinda citrifolia L. is a fruit tree traditionally used as antibacterial and with several other
pharmacological properties. This plant presents several phytocompounds as flavonoids, alkaloids and triterpenes. The objective of
this work was assay the antimicrobial and modulatory potential of the fruit extract. The extract was assayed alone and associated
with antibiotics and antifungals against pathogenic microrganisms using the microdilution assay. The results demonstrated that
the association between extract and antimicrobial drugs resulted in a potentiation of the drug activity clinically relevant against
Pseudomonas aeruginosa and Escherichia coli.
African journal of pharmacy and pharmacology
Caryocar coriaceum Wittm. (pequi) has been popularly used in Northeastern Brazil in the treatment... more Caryocar coriaceum Wittm. (pequi) has been popularly used in Northeastern Brazil in the treatment of inflammation, pain and respiratory affections. This study evaluated the topical anti-inflammatory activity of C. coriaceum hydroethanolic extract (CCHE) and methanolic fraction (CCMF) from pequi tree leaves against different skin sensitizer agents (arachidonic acid, croton oil, phenol and histamine), as well their antioxidant activity and phenolic compound profile. High performance liquid chromatography with diode array detection (HPLC-DAD) analysis pointed the presence of chlorogenic acid, rutin, quercetin and lower concentrations of caffeic and gallic acids. Both CCHE and CCMF 1 mg/ear demonstrated significant topical anti-inflammatory effect against arachidonic acid, phenol and histamine single application (antiedematous effect ranging from 48 to 69% for CCHE and 36 to 64% for CCMF; P < 0.05 vs. negative control). In contrast, both extracts did not antagonize the croton oil sin...
Raphiodon echinus (R. echinus) is used in Brazilian folk medicine for the treatment of inflammat... more Raphiodon echinus (R. echinus) is used in Brazilian folk medicine for the treatment of inflammation, coughs, and infectious diseases. However, no information is available on the
potential antioxidant, cytotoxicity and genotoxicity of this plant. In this study, the polyphenolic constituents, antioxidant capacity and potential toxic effects of aqueous and ethanolic extracts of
R. echinus on human erythrocytes and leukocytes were investigated for the first time. R. echinus extracts showed the presence of Gallic, chlorogenic, caffeic and ellagic acids, rutin, quercitrin and quercetin. Aqueous and ethanolic extracts of R. echinus exhibited antioxidant activity in DPPH
radical scavenging with IC50 = 111.9 μg/mL (EtOH extract) and IC50 = 227.9 μg/mL (aqueous extract). The extracts inhibited Fe2+ (10 μM) induced thiobarbituric acid reactive substances (TBARS) formation in rat brain and liver homogenates. The extracts (30–480 μg/mL) did not induce genotoxicity, cytotoxicity or osmotic fragility in human blood cells. The findings of this present study therefore suggest that the therapeutic effect of R. echinus may be, in part, related to its antioxidant potential. Nevertheless, further in vitro and in vivo studies are required to ascertain the safety margin of its use
in folk medicine.
American Fern Journal, 2012
Chagas disease is caused by Trypanosoma cruzi, and is considered a public health problem. The cur... more Chagas disease is caused by Trypanosoma cruzi, and is considered a public health problem. The current treatments for this disease are the synthetic drugs nifurtimox and benzonidazol, which are highly toxic. Pityrogramma calomelanos, a plant used in traditional medicine as an astringent, analgesic, anti-hemorrhagic, pectoral depurative, emmenagogue, anti-hypertensive, anti-pyretic and an anti-tussive was tested for antiepimastigote activity in vitro. An ethanol extract and hexane fraction of P. calomelanos was prepared and tested against T. cruzi (CL-B5 clone). The effective concentration capable of killing 50% of parasites (EC 50 ) was 55.26 mg/mL and 73.57 mg/mL for the ethanol extract and hexane fraction, respectively. This is the first record of tripanocidal activity for P. calomelanos. Our results indicate that P. calomelanos could be a source of antiepimastigote natural products with only moderate toxicity toward healthy human cells.
Acta Biológica Colombiana, 2015
Tropidurus hispidus has been used in traditional medicine in several regions of Northeastern Regi... more Tropidurus hispidus has been used in traditional medicine in several regions of Northeastern Region of Brazil. Its medicinal use
involves the treatment of diseases such as warts, sore throat, tonsillitis, chicken pox, varicella, measles, asthma, alcoholism, and
dermatomycosis.The present study evaluated the topical anti-inflammatory activity of Tropidurus hispidus fat in treating ear edema
in an animal model. Oil from T. hispidus (OTH) was evaluated on its effect against experimental inflammation in mice. OTH was
extracted frombody fat located in the ventral region of Tropidurus hispidus using hexane as a solvent.We used themodel of mouse
ear edema induced by phlogistic agents, croton oil (single and multiple applications), arachidonic acid, phenol, capsaicin, and
histamine, applied into the right ears of animals pretreated with acetone (control), dexamethasone, or OTH. OTH inhibited the
dermatitis induced by all noxious agents, except capsaicin. This effect may be related to the fatty acids present in OTH.
Duguetia furfuraceais frequently used as a medicinal plant in Brazil. However, studies have evide... more Duguetia furfuraceais frequently used as a medicinal plant in Brazil. However, studies have evidenced its cytotoxic, bactericide, and antitumor activities. In the present study we aimed to evaluate the potential toxicity of hydroalcoholic leaves extracts ofD. furfuracea (HEDF) in aDrosophila melanogastermodel. Toxicity was assessed as changes in locomotor performance, mitochondrial activity,
oxidative stress, MAPKs phosphorylation, and apoptosis induction after exposure to HEDF concentrations (1–50 mg/mL) for 7 days. The phytoconstituents of the plant were screened for the presence of alkaloids, tannins, xanthones, chalcones, flavonoids, aurones,
and phenolic acids. Exposure of adult flies to HEDF caused mitochondrial dysfunction, overproduction of ROS, and alterations inthe activity of detoxifying enzymes GST, SOD and CAT. Induction of ERK phosphorylation and PARP cleavage was also observed, indicating occurrence of HEDF-induced cell stress and apoptotic cell death. In parallel, alterations in cholinesterase activity and impairments in negative geotaxis behavior were observed. Our study draws attention to the indiscriminate use of this plant by population and suggests oxidative stress asa major mechanism underlying its toxicity.
Background: The challenge of antibiotic resistance and the emergence of new infections have gener... more Background: The challenge of antibiotic resistance and the emergence of new infections have generated considerable interest in the exploration of natural products from plant origins as combination therapy. In this context, crude ethanolic extract (CEE), ethyl acetate fraction (EAF), and methanolic fraction (MF) from Anacardium microcarpum were tested alone or in combination with antibiotics (amikacin, gentamicin, ciprofloxacin, and imipenem) against Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus.
Methods: Antibiotic resistance-modifying activity was performed using the microdilution method by determining the minimal inhibitory concentration (MIC). In addition, phytochemical prospecting analyses of tested samples were carried out. Results: Our results indicated that all the extracts showed low antibacterial activity against multidrug-resistant strains (MIC =512 µg/mL). However, addition of CEE, EAF, and MF to the growth medium at the subinhibitory concentration (MIC/8=64 µg/mL) significantly modulated amikacin- and gentamicin-resistant E. coli 06. CEE and EAF also demonstrated a
significant (P,0.001) synergism with imipenem against S. aureus. In contrast, MF antagonized the antibacterial effect of ciprofloxacin and gentamicin against P. aeruginosa 03 and
S. aureus 10, respectively. Qualitative phytochemical analysis of the extracts revealed the
presence of secondary metabolites including phenols, flavonoids, xanthones, chalcones, and
tannin pyrogallates.
Conclusion: Taken together, our results suggest that A. microcarpum is a natural resource with
resistance-modifying antibacterial activity that needs to be further investigated to overcome the
present resistant-infection problem.
European Journal of Medicinal Chemistry, 1999
Background: The challenge of antibiotic resistance and the emergence of new infections have gener... more Background: The challenge of antibiotic resistance and the emergence of new infections have generated considerable interest in the exploration of natural products from plant origins as combination therapy. In this context, crude ethanolic extract (CEE), ethyl acetate fraction (EAF), and methanolic fraction (MF) from Anacardium microcarpum were tested alone or in combination with antibiotics (amikacin, gentamicin, ciprofloxacin, and imipenem) against Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus.
Methods: Antibiotic resistance-modifying activity was performed using the microdilution method by determining the minimal inhibitory concentration (MIC). In addition, phytochemical prospecting analyses of tested samples were carried out.
Results: Our results indicated that all the extracts showed low antibacterial activity against multidrug-resistant strains (MIC =512 μg/mL). However, addition of CEE, EAF, and MF to the growth medium at the subinhibitory concentration (MIC/8=64 μg/mL) significantly modulated amikacin- and gentamicin-resistant E. coli 06. CEE and EAF also demonstrated a significant (P,0.001) synergism with imipenem against S. aureus. In contrast, MF antagonized the antibacterial effect of ciprofloxacin and gentamicin against P. aeruginosa 03 and S. aureus 10, respectively. Qualitative phytochemical analysis of the extracts revealed the presence of secondary metabolites including phenols, flavonoids, xanthones, chalcones, and tannin pyrogallates.
Conclusion: Taken together, our results suggest that A. microcarpum is a natural resource with resistance-modifying antibacterial activity that needs to be further investigated to overcome the present resistant-infection problem.
This work aims to record the therapeutical practices of the community Catolé utilizing local dive... more This work aims to record the therapeutical practices of the community Catolé utilizing local diversity of medicinal plants
verifying the versatility of the species, consensus usage and knowledge of the informants. Were recorded 46 native species for medicinal
purposes, belonging to 42 genres and 26 families, highlighting Fabaceae. Ten specimens exhibited great versatility of use, however
Ximennia americana L. and Croton heliotropiifolius Kunth showed the highest values of IR (2.0 and 1.65). The Therapeutic uses were
grouped in 15 categories of bodily systems, with higher factor consensus among informants in: Infectious and parasitic diseases (1.0),
disorder of the respiratory system (0.82) and Endocrine, nutrition and of metabolism (0.81). Due to the diversity of native species registered,
it can be concluded that the preservation of these areas is of great importance for biodiversity conservation site and the informants involved have a vast knowledge of the vegetation contributing to the knowledge of potentially useful plants of the cerrado.
The Cluster Analysis is a type of pattern recognition applicable to the drug design. In this pape... more The Cluster Analysis is a type of pattern recognition applicable to the drug design. In this paper, we present an agglomerative classification model in order to group substituents on the basis of similarities of their physical and chemical parameters. Once grouped, we investigate the relationship between the hierarchical model and the biological responses of compounds from the Quantitative Structure-Activity Relationship (QSAR). The method is then implemented by a new algorithm, called Winclus, for which we developed a dedicated software. This work addresses the software development and the application to a series of indole-2-carboxylate with anticonvulsant activity, described in the literature. The study was seeking to establish a relationship between groups of substituents (derived from the proposed model) and the biological activities of compounds already synthesized. To this end, we used the graphical form of dendrogram and offered the developed program as a tool in the design of new biologically active compounds.
European Journal of Medical Chemistry, 1999
A new agglomerative (bottom-up) hierarchical cluster technique referred to as the Adaptive Mean-L... more A new agglomerative (bottom-up) hierarchical cluster technique referred to as the Adaptive Mean-Linkage algorithm is derived. Cluster algorithms are also offered as a tool to explore the descriptor space knowing the quantitative structure–activity relationship (QSAR). The substituents are clustered building a dendrogram (cluster tree) per site. Choosing appropriate pathways on such cluster trees according to the QSAR equation, an automated search for potentially active substituted compounds can be performed. Applications to a series of substituted phenylguanidines with anticancer activity are focused illustrating this approach.
The medicinal plants and natural products are products with a great scientific interest due their... more The medicinal plants and natural products are products with a great scientific
interest due their possible use like phytodrugs. In this context, the
phytochemical composition and the antibacterial and antibiotic modulatory
activity of the extract and fractions of Annona squamosa against Staphylococus
aureus and Escherichia coli were performed. All natural products have not
showed clinically relevant antibacterial activity, with MIC ≥ 1024 mg/mL.
However, the extract combined with some aminoglycoside showed a synergistic
effect against multiresistant strains E. coli 27 and S. aureus 358. Due these
results, A. squamosa (Annonaceae) must be more studied to be used as a
source of natural products with adjuvant potential to enhance the antibiotic
activity, combating by this way the microbial antibiotic resistance
Bowdichia virgilioides (Fabaceae - Papilionoidea), popularly known as Sucupira-preta, is a Brazil... more Bowdichia virgilioides (Fabaceae - Papilionoidea), popularly known as Sucupira-preta, is a Brazilian native tree used in the traditional medicine against throat infections. Due this fact and due the interest to validate the traditional use, the objective of this work was evaluates the in vitro antibacterial activity of extracts and fractions of the stem and heartwood of the plant. The phytochemical profile revealed the presence of tannins and flavonoids in the stem and heartwood, and only alkaloids in the stem.The HPLC analysis revealed the presence of flavonoids and phenolic acids, natural products with several biological activities, including the modifying antibiotic activity. All microrganisms were inhibited only with MIC ≥ 1024 μg/mL. However, when associated with aminoglycosides, was demonstrated a potentiation of these antibiotics when associated with almost all products assayed and against one bacterium at least.
A doença de Chagas e a leishmaniose são doenças que prevalecem em países pobres. Os fármacos disp... more A doença de Chagas e a leishmaniose são doenças que prevalecem em países pobres. Os fármacos disponíveis para o tratamento dessas doenças são altamente tóxicos, sendo este um dos motivos que dificulta à adesão terapêutica e, assim, levando à busca por novas drogas eficazes e seguras para seus tratamentos. A pesquisa utilizando produtos naturais tem se mostrado uma alternativa na procura de novos compostos com potencial clínico-terapêutico. O gênero Passiflora possui as seguintes atividades farmacológicas centrais como calmantes, sedativas, ansiolíticas e indutor do sono e atividades antiparasitarias. A Passiflora cincinnata possui ampla distribuição pelo Brasil sendo popularmente utilizada para distúrbios de sono. Neste estudo avaliamos sua atividade antiparasitária contra Leishmania brasiliensis, Leishmania infantum e Trypanosoma cruzi, bem como sua citotoxicidade em fibroblastos. Foram testados extratos hidroalcoólicos obtidos das folhas, casca, sementes e caule em diferentes concentrações. Os extratos das folhas, casca e sementes não foram eficazes contra L. brasiliensis e T. cruzi, porém, o extrato do caule promoveu uma inibição de 29,12 % contra T. cruzi numa concentração de 500 μg/mL, entretanto o extrato da casca de P. cincinnata foi o que apresentou a melhor atividade contra as formas parasitárias de L. infantum, causando um percentual de morte >20 % nas concentrações de 250 a 1000 μg/mL. Referente à toxicidade, o extrato das folhas foi o que apresentou maior citotoxicidade, quando comparado com os demais, causando a mortalidade de 68,63 % dos fibroblastos numa concentração de 1000 μg/mL. A baixa citotoxicidade revelada abre espaço para novos estudos biológicos
The specie Lippia gracilis Schauer is largely utilized for their antimicrobial properties, which ... more The specie Lippia gracilis Schauer is largely utilized for their antimicrobial properties, which
are attributed to the presence of phenolic monoterpenes such as thymol and carvacrol. The aim of this study
was to determine the yields and chemical composition of the essential oils obtained from fresh and dry leaves
of collected at different times in the city of Crato-CE, in January 2009. The essential oils were extracted by
hydrodistillation, and its components were identified by gas chromatography coupled with mass
spectrophotometry. The time of plant collection should coincide with the moment of greatest expression of the
active principle.
Ethnopharmacological relevance: Ethnobotanical studieshavecontributedsignificantly inresearchof p... more Ethnopharmacological relevance: Ethnobotanical studieshavecontributedsignificantly inresearchof
plants withtherapeuticpotential.Theaimofthepresentstudywastolearnabouttheuseofnative
medicinal plantscitedbythetraditionalpopulationin “cerradão” (savannawoodland)areasinNortheast
Brazil, providingdataontherapeuticindicationsofthespeciesusedandtheirversatility.
Materials andmethods: Semi-structured interviewswereconductedonthebasisofastandardized
questionnairedesignedforkeyinformantsselectedusingthe “snowball” technique.Theselectionof
plants specieswiththerapeuticpotentialwasperformedonthebasisoftherelativeimportance(RI)and
informant consensusfator(ICF).
Results: A totalof78specieswereindicatedfor87therapeuticpurposes.Ofthese,11speciespresented
great versatilityofuse(RI41), ase.g.including Copaiferalangsdorffii Desf., Hybanthus calceolaria (Mart.)
Plumel., Heliotropium cf. indicum L., Crotonzehntneri, Crotonheliotropiifolius, Myracrodruonurundeuva,
Stryphnodendrorotundifolium. MedicinalusescouldbegeneralizedPax&K.Hoffmand Hymenaea
courbaril L. Thetherapeuticindicationsweregroupedinto14use15categorieswith594species–category
combinations. Thelargestnumberofmedicinalspecieswasindicatedforillnessesorundefined pain,
followedbydiseasesassociatedwithrespiratory,digestiveandgenitourinaryofbodysystems.Thefactor
informant consensushighlightedtheagreementintheuseofplantsandshowedthatthe,ofwhich
Diseases oftheNervousSystemand,DiseasesoftheCirculatorySystemhadthegreatestagreement
1.0and0.87repectively,DisordersoftheVisualSensorySystem – EyesandRespiratorySystemDisorder
showedthehighestagreementofuse.
Conclusions: Most ofthespeciescitedbythekeyinformantsarewellknownscientifically,butitis
interestingthatsomehavebeenstudiedlittleornotallwithregardtoconfirming theirpurported
medicinal propertiesandcancontributesubstantiallytopharmacologicalandphytochemicalinvestiga-
tions inthesearchfornewdrugs.
Lippia alba is empirically used for infusions, teas, macerates, and hydroalcoholic extracts becau... more Lippia alba is empirically used for infusions, teas, macerates, and hydroalcoholic extracts because of its antispasmodic,
analgesic, sedative, and anxiolytic effects. Citral is a mixture of trans-geranial and cis-neral and is the main constituent of L. alba
essential oil and possesses analgesic, anxiolytic, anticonvulsant, and sedative effects. The present study evaluated the effects
of the essential oil of L. alba (EOLa) and citral on compound action potentials (CAPs) in Wistar rat sciatic nerves. Both drugs
inhibited CAP in a concentration-dependent manner. The calculated half-maximal inhibitory concentrations (IC50) of peak-topeak
amplitude were 53.2 mg/mL and 35.00 mg/mL (or 230 mM) for EOLa and citral, respectively. Peak-to-peak amplitude of the
CAP was significantly reduced by 30 mg/mL EOLa and 10 mg/mL citral. EOLa and citral (at 60 and 30 mg/mL, values close to
their respective IC50 for CAP blockade) significantly increased chronaxy and rheobase. The conduction velocity of the first and
second CAP components was statistically reduced to B86% of control with 10 mg/mL EOLa and B90% of control with 3 mg/mL
citral. This study showed that EOLa inhibited nerve excitability and this effect can be explained by the presence of citral in its
composition. Both EOLa and citral showed inhibitory actions at lower concentrations compared with other essential oils and
constituents with local anesthetic activity. In conclusion, these data demonstrate that EOLa and citral are promising agents in
the development of new drugs with local anesthetic activity.
The use of medicinal plants is widespread around the world including Brazil, where there are seve... more The use of medicinal plants is widespread around the world including Brazil, where there are several species and a large tradition in their use. It was
aimed to know the perception of the nurses about the use of phytotherapy in Health Family Strategy (HFS). Exploratory descriptive study, qualitative
approach, developed in Crato-CE with fifteen nurses from HFS. It was employed the Theme-Category Analysis. It were constructed six categories and two
subcategories which were described the knowledge of professionals about phytotherapy, their views about use in primary care, the use of this practice and
the strategies developed for this use. The results revealed that the knowledge of the interviewees mostly is narrow and informal, and they find difficulties
to implement phytotherapic practices such as no valuation by the management and the rest of the health group. It should be emphasized as well the
importance of developing strategies that enable the safe and efficient integration of phytotherapy in care and thus the appreciation of local culture
The rising of the drug resistant microrganisms and the toxicity related with the antimicrobial dr... more The rising of the drug resistant microrganisms and the toxicity related with the antimicrobial drugs enhances the necessity about
the search of new bioactive compounds. Morinda citrifolia L. is a fruit tree traditionally used as antibacterial and with several other
pharmacological properties. This plant presents several phytocompounds as flavonoids, alkaloids and triterpenes. The objective of
this work was assay the antimicrobial and modulatory potential of the fruit extract. The extract was assayed alone and associated
with antibiotics and antifungals against pathogenic microrganisms using the microdilution assay. The results demonstrated that
the association between extract and antimicrobial drugs resulted in a potentiation of the drug activity clinically relevant against
Pseudomonas aeruginosa and Escherichia coli.