Simone de Araújo - Academia.edu (original) (raw)
Papers by Simone de Araújo
Cadernos de Prospecção, Dec 30, 2015
Nesta prospecção, objetivou-se realizar um estudo sobre atividades biológicas já descritas para o... more Nesta prospecção, objetivou-se realizar um estudo sobre atividades biológicas já descritas para o mastruz, com especial destaque para as eventuais aplicações farmacológicas desta planta. Para isso, foram obtidas informações sobre artigos científicos nas bases Web of Science TM , ScienceDirect, PubMed e Scielo, bem como sobre documentos de patentes nas bases USPTO, EPO, WIPO e INPI, com o uso da palavra-chave: Chenopodium ambrosioides, sempre utilizada nos campos de busca relativos ao título e ao resumo dos trabalhos. Desse modo, verificou-se que em bases de dados internacionais de artigos científicos, muitos são os trabalhos publicados envolvendo o mastruz, mas há número relativamente baixo de documentos de patentes, principalmente, no que se refere à descrição de eventual ação farmacológica da planta. Isso demonstra que há grandes oportunidades de pesquisa envolvendo a descrição da atividade biológica de extratos ou óleos essesnciais de plantas, como o mastruz. Palavras chave: Prospecção Científica. Atividades Farmacológicas. Mastruz.
International Journal of Biological Macromolecules, 2016
Seaweeds are sources of diverse bioactive compounds, such as sulphated polysaccharides. This stud... more Seaweeds are sources of diverse bioactive compounds, such as sulphated polysaccharides. This study was designed to evaluate the chemical composition and anti-diarrheal activity of a fraction of sulphated polysaccharide (PLS) obtained from the red seaweed Hypnea musciformis in different animal models, and to elucidate the underlying mechanisms. PLS was obtained by aqueous extraction, with a yield of 31.8% of the seaweed dry weight. The total carbohydrate content accounted for 99% of the sample. The sulfate content of the polysaccharide was 5.08% and the percentage of carbon was 25.98%. Pretreatment with all doses of PLS inhibited castor oil-induced diarrhea, with reduction of the total amount of stool, diarrheal stools, and the severity of diarrhea. PLS (90mg/Kg) decreased castor oil- and PGE2-induced enteropooling. In addition, PLS (90mg/Kg) increased the Na(+)/K(+)-ATPase activity in the small intestine and reduced gastrointestinal transit, possibly via activation of cholinergic receptors. Interestingly, the cholera toxin-induced fluid secretion and Cl(-) ion levels decreased in the intestinal contents of the animals pretreated with PLS (90mg/kg), probably via reduction of toxin-GM1 receptor binding. In conclusion, PLS exerts anti-diarrheal activity by increasing Na(+)/K(+)-ATPase activity, inhibiting gastrointestinal motility, and blocking the toxin-GM1 receptor binding.
Mayaro virus (MAYV) is an emerging arbovirus member of theTogaviridaefamily andAlphavirusgenus. M... more Mayaro virus (MAYV) is an emerging arbovirus member of theTogaviridaefamily andAlphavirusgenus. MAYV infection causes an acute febrile illness accompanied by persistent polyarthralgia and myalgia. Understanding the mechanisms involved in arthritis caused by alphaviruses is necessary to develop specific therapies. In this work, we investigated the role of the CCL2/CCR2 axis in the pathogenesis of MAYV-induced disease. For this, WT C57BL/6J and CCR2-/-mice were infected with MAYV subcutaneously and evaluated for disease development. MAYV infection induced an acute inflammatory disease in WT mice. The immune response profile was characterized by an increase in the production of inflammatory mediators, such as IL-6, TNF and CCL2. Higher levels of CCL2 at the local and systemic levels, was followed by significant recruitment of CCR2+macrophages and a cellular response orchestrated by these cells. CCR2-/-mice showed an increase in CXCL-1 levels, followed by a replacement of the macrophage...
Brazil's biodiversity is extremely vast, but only a small fraction is used for research and d... more Brazil's biodiversity is extremely vast, but only a small fraction is used for research and development of medicines. Medicinal plants and secondary metabolites may represent the opportunity to develop effective and low-cost treatments. This literature review article seeks to promote the importance of Brazilian vegetable biodiversity in the development of health resources. For this, we searched in national and international databases (Scielo, Lilacs, Medline / Pubmed and Google Scholar). Despite having a wealth still unexplored, large areas of Cerrado, Amazon and Caatinga have already suffered deforestation. It is considered necessary and urgent that more governmental policies to protect these areas be developed in order to encourage the conservation of flora biodiversity, especially of medicinal plants, and to ensure the genetic variability and the phytochemical characteristics that are important sources for obtaining molecular identities for the pharmaceutical industry.
Revista Gestão Inovação e Tecnologias, 2018
O objetivo deste estudo foi realizar uma revisão literária a partir de artigos, dissertações e te... more O objetivo deste estudo foi realizar uma revisão literária a partir de artigos, dissertações e teses, e uma prospecção baseada na busca por patentes para apresentar uma visão geral das aplicações farmacológicas e tecnológicas relacionadas à utilização da goma do cajueiro (GC). As bases Periódicos Capes, ScienceDirect e Web of ScienceTM, foram acessadas para a busca por publicações e os bancos de patentes: USPTO, EPO, WIPO e INPI para a busca por patentes referentes a aplicação da GC na indústria farmacêutica, alimentícia e na área de nanotecnologia. Observou-se apenas 4 atividades farmacológicas para a GC: cicatrizante, antibacteriana, gastroprotetora e antidiarreica. Quanto às patentes, foram encontrados apenas dois registros na EPO relacionados à aplicação tecnológica de GC. Contudo, não havia nenhuma patente da GC relacionada a nanotecnologia, mostrando que o campo de pesquisa é bastante amplo nessa área. Observa-se, portanto, que é necessário maior investimento quanto à aplicação tecnológica da GC nas áreas farmacêutica e alimentícia.
Nutrients, 2019
This study aimed to evaluate the effect of Lactobacillus reuteri DSM 17938 (DSM) on ethanol-induc... more This study aimed to evaluate the effect of Lactobacillus reuteri DSM 17938 (DSM) on ethanol-induced gastric injury, and if its possible mechanism of action is related to inhibiting the transient receptor potential vanilloid type 1 (TRPV1). We evaluated the effect of supplementing 108 CFU•g body wt−1•day−1 of DSM on ethanol-induced gastric injury. DSM significantly reduced the ulcer area (1.940 ± 1.121 mm2) with 3 days of pretreatment. The effects of DSM supplementation were reversed by Resiniferatoxin (RTX), TRPV1 agonist (3 nmol/kg p.o.). Substance P (SP) (1 μmol/L per 20 g) plus 50% ethanol resulted in hemorrhagic lesions, and DSM supplementation did not reverse the lesion area induced by administering SP. TRPV1 staining intensity was lower, SP, malondialdehyde (MDA) and nitrite levels were reduced, and restored normal levels of antioxidant parameters (glutathione and superoxide dismutase) in the gastric mucosa in mice treated with DSM. In conclusion, DSM exhibited gastroprotectiv...
Nitric oxide : biology and chemistry, Jan 30, 2018
Activation of 5' adenosine monophosphate-activated protein kinase (AMPK) stimulates productio... more Activation of 5' adenosine monophosphate-activated protein kinase (AMPK) stimulates production of the gaseous mediators nitric oxide (NO) and carbon monoxide (CO), which are involved in mucosal defense and gastroprotection. As AMPK itself has gastroprotective effects against several gastric ulcer etiologies, in the present study, we aimed to elucidate whether AMPK may also prevent ethanol-induced injury and play a key role in the associated gastroprotection mediated by hydrogen sulfide (HS), NO, and CO. Mice were pretreated with AICAR (20 mg/kg, an AMPK activator) alone or with 50% ethanol. Other groups were pretreated with respective gaseous mediator inhibitors PAG, l-NAME, or ZnPP IX 30 min prior to AICAR, or with gaseous mediator donors NaHS, Lawesson's reagent and l-cysteine (HS), SNP, l-Arginine (NO), Hemin, or CORM-2 (CO) 30 min prior to ethanol with or without compound C (10 mg/kg, a non-selective AMPK inhibitor). HS, nitrate/nitrite (NO/NO), bilirubin levels, GSH and...
Nitric Oxide, 2017
Hydrogen sulphide (H 2 S) is a gasotransmitter that participates in various physiological and pat... more Hydrogen sulphide (H 2 S) is a gasotransmitter that participates in various physiological and pathophysiological processes within the gastrointestinal tract. We studied the effects and possible mechanism of action of H 2 S in secretory diarrhoea caused by cholera toxin (CT). The possible mechanisms of action of H 2 S were investigated using an intestinal fluid secretion model in isolated intestinal loops on anaesthetized mice treated with CT. NaHS and Lawesson's reagent and L-cysteine showed antisecretory activity through reduction of intestinal fluid secretion and loss of Cl À induced by CT. Pretreatment with an inhibitor of cystathionine-g-lyase (CSE), DL-propargylglycine (PAG), reversed the effect of L-cysteine and caused severe intestinal secretion. Co-treatment with PAG and a submaximal dose of CT increased intestinal fluid secretion, thus supporting the role of H 2 S in the pathophysiology of cholera. CT increased the expression of CSE and the production of H 2 S. Pretreatment with PAG did not reverse the effect of SQ 22536 (an AC inhibitor), bupivacaine (inhibitor of cAMP production), KT-5720 (a PKA inhibitor), and AICAR (an AMPK activator). The treatment with Forskolin does not reverse the effects of the H 2 S donors. Co-treatment with either NaHS or Lawesson's reagent and dorsomorphin (an AMPK inhibitor) did not reverse the effect of the H 2 S donors. H 2 S has antisecretory activity and is an essential molecule for protection against the intestinal secretion induced by CT. Thus, H 2 S donor drugs are promising candidates for cholera therapy. However, more studies are needed to elucidate the possible mechanism of action.
Journal of Pharmacy and Pharmacology, 2017
Objectives We aimed to determine whether carvacryl acetate acts as a TRPA1 receptor agonist and i... more Objectives We aimed to determine whether carvacryl acetate acts as a TRPA1 receptor agonist and its effects against irinotecan (CPT-11) induced intestinal mucositis in mice. Methods TRPA1 structure was obtained from a protein databank, and the 3D structure of carvacryl acetate was determined. Appropriate binding conformations were discovered via automatic docking simulations. To determine the effect of carvacryl acetate in vivo, mice were treated with either DMSO 2%, CPT-11, carvacryl acetate followed by CPT-11, or HC-030031, a TRPA1 antagonist, followed by carvacryl acetate. Jejunum samples were taken and structural, inflammatory and antioxidant parameters were studied. Key findings Eight amino acids residues in TRPA1 established stable interactions with carvacryl acetate, which led to pharmacological efficacy against CPT-11-induced intestinal mucositis via reduction of both neutropenia and bacteremia, increase in villi height and crypt depth, decrease in pro-inflammatory cytokines...
International journal of biological macromolecules, Jan 24, 2017
Inflammation is a protective reaction of the microcirculation. However, sustained inflammation ca... more Inflammation is a protective reaction of the microcirculation. However, sustained inflammation can lead to undesired effects. Thuja occidentalis Linn has many pharmacological properties but has no anti-inflammatory activity described. Thus, this study aims evaluating the anti-inflammatory activity of the aqueous extract (AE) and the polysaccharide fraction (PLS) of T. occidentalis L. in mice. The results of our evaluations in various experimental models indicated that AE and PLS (3, 10, and 30mg/kg, i.p.) reduced (p˂0.05) paw edema induced by carrageenan, dextran sulfate (DEX), compound 48/80, serotonin (5-HT), bradykinin (BK), histamine (HIST), and prostaglandin E2 (PGE2). Furthermore, it inhibited neutrophils recruitment; decreased MPO activity, tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) levels, vascular permeability, nitrite concentration, and MDA concentration; and maintained the GSH levels in the peritoneal exudate. The AE and PLS reduced neutrophil infiltration a...
Journal of Ethnopharmacology, 2015
Ethnopharmacological relevance: Anacardium occidentale L. (Anacardiaceae) is commonly known as th... more Ethnopharmacological relevance: Anacardium occidentale L. (Anacardiaceae) is commonly known as the cashew tree. It is native to tropical America and extracts of the leaves, bark, roots, chestnut net and exudate have been traditionally used in northeast Brazil for the treatment of various diseases. The exudate of the cashew tree (cashew gum) has been exploited by locals since ancient times for multiple applications, including the treatment of diarrheal diseases. Aim of the study: The primary aim of the present study is to evaluate the antidiarrheal activity of cashew gum (CG), a complex heteropolysaccharide from the exudate of the cashew tree, using various models. Materials and methods: The antidiarrheal activity of cashew gum (CG) against acute diarrhea was investigated using the castor oil-induced diarrhea model. The effects of CG on gastrointestinal transit and castor oil-and PGE 2-induced enteropooling were also examined in rodents. In addition, the effect of CG against secretory diarrhea was investigated using a model of fluid secretion in cholera toxin-treated intestinal closed loops in live mice. Results: Cashew gum (30, 60, and 90 mg/kg, p.o.) showed a significant (P < 0.05-0.01) antidiarrheal effect in rats with castor oil-induced diarrhea, inhibiting the total amount of stool and diarrheal stools. The 60 mg/kg dose of CG exhibited excellent antidiarrheal activity and significantly reduced the severity of diarrhea (diarrhea scores) in rats. CG (60 mg/kg) significantly (P < 0.05) decreased the volume of castor oil-and PGE 2-induced intestinal fluid secretion (enteropooling). In addition, similar to loperamide (standard drug, 5 mg/kg, p.o.), CG treatment reduced the distance travelled by a charcoal meal in the 30-min gastrointestinal transit model by interacting with opioid receptors. In cholera toxin-induced secretory diarrhea, CG (60 mg/kg) significantly inhibited the intestinal fluid secretion and decreased Clion loss in the cholera toxintreated isolated loops model of live mice by competitively binding to cholera toxin-GM1 receptors. Conclusions: In conclusion, our results indicate that a complex heteropolysaccharide extracted from the exudate of A. occidentale L. has antidiarrheal activity in acute, inflammatory, and secretory diarrhea models, which could justify its traditional use in the treatment of diarrhea in northeast Brazil. The antidiarrheal activity might be explained by the capacity of CG to inhibit gastrointestinal motility and thereby reduce the accumulation of intestinal fluid and the secretion of water and chloride ions in the lumen of the intestine.
Research, Society and Development
Type 2 diabetes mellitus (T2DM) is a chronic metabolic disorder that originates from numerous pat... more Type 2 diabetes mellitus (T2DM) is a chronic metabolic disorder that originates from numerous pathogenic mechanisms, all of which result in hyperglycemia. This disease is a major cause of morbidity and mortality worldwide. Effective prevention and treatment strategies for T2DM are therefore necessary. The purpose of this review was to summarize the pharmacotherapy for patients with T2DM by discussing its pathophysiology, the therapeutic classes used in treatment strategies, as well as the mechanisms of action for each one. A literature review was conducted by searching Google Scholar, PubMed, and Science Direct databases using the search terms: type 2 diabetes mellitus, insulin, AMPK, antidiabetic drugs, incretin, SGLT2, and biguanides covering studies up to 2022. The review identified and included studies including qualitative, original research articles, and randomized controlled trial designs. The results of this study are divided into drugs that increase insulin sensitivity (e.g...
Cadernos de Prospecção, Dec 30, 2015
Nesta prospecção, objetivou-se realizar um estudo sobre atividades biológicas já descritas para o... more Nesta prospecção, objetivou-se realizar um estudo sobre atividades biológicas já descritas para o mastruz, com especial destaque para as eventuais aplicações farmacológicas desta planta. Para isso, foram obtidas informações sobre artigos científicos nas bases Web of Science TM , ScienceDirect, PubMed e Scielo, bem como sobre documentos de patentes nas bases USPTO, EPO, WIPO e INPI, com o uso da palavra-chave: Chenopodium ambrosioides, sempre utilizada nos campos de busca relativos ao título e ao resumo dos trabalhos. Desse modo, verificou-se que em bases de dados internacionais de artigos científicos, muitos são os trabalhos publicados envolvendo o mastruz, mas há número relativamente baixo de documentos de patentes, principalmente, no que se refere à descrição de eventual ação farmacológica da planta. Isso demonstra que há grandes oportunidades de pesquisa envolvendo a descrição da atividade biológica de extratos ou óleos essesnciais de plantas, como o mastruz. Palavras chave: Prospecção Científica. Atividades Farmacológicas. Mastruz.
International Journal of Biological Macromolecules, 2016
Seaweeds are sources of diverse bioactive compounds, such as sulphated polysaccharides. This stud... more Seaweeds are sources of diverse bioactive compounds, such as sulphated polysaccharides. This study was designed to evaluate the chemical composition and anti-diarrheal activity of a fraction of sulphated polysaccharide (PLS) obtained from the red seaweed Hypnea musciformis in different animal models, and to elucidate the underlying mechanisms. PLS was obtained by aqueous extraction, with a yield of 31.8% of the seaweed dry weight. The total carbohydrate content accounted for 99% of the sample. The sulfate content of the polysaccharide was 5.08% and the percentage of carbon was 25.98%. Pretreatment with all doses of PLS inhibited castor oil-induced diarrhea, with reduction of the total amount of stool, diarrheal stools, and the severity of diarrhea. PLS (90mg/Kg) decreased castor oil- and PGE2-induced enteropooling. In addition, PLS (90mg/Kg) increased the Na(+)/K(+)-ATPase activity in the small intestine and reduced gastrointestinal transit, possibly via activation of cholinergic receptors. Interestingly, the cholera toxin-induced fluid secretion and Cl(-) ion levels decreased in the intestinal contents of the animals pretreated with PLS (90mg/kg), probably via reduction of toxin-GM1 receptor binding. In conclusion, PLS exerts anti-diarrheal activity by increasing Na(+)/K(+)-ATPase activity, inhibiting gastrointestinal motility, and blocking the toxin-GM1 receptor binding.
Mayaro virus (MAYV) is an emerging arbovirus member of theTogaviridaefamily andAlphavirusgenus. M... more Mayaro virus (MAYV) is an emerging arbovirus member of theTogaviridaefamily andAlphavirusgenus. MAYV infection causes an acute febrile illness accompanied by persistent polyarthralgia and myalgia. Understanding the mechanisms involved in arthritis caused by alphaviruses is necessary to develop specific therapies. In this work, we investigated the role of the CCL2/CCR2 axis in the pathogenesis of MAYV-induced disease. For this, WT C57BL/6J and CCR2-/-mice were infected with MAYV subcutaneously and evaluated for disease development. MAYV infection induced an acute inflammatory disease in WT mice. The immune response profile was characterized by an increase in the production of inflammatory mediators, such as IL-6, TNF and CCL2. Higher levels of CCL2 at the local and systemic levels, was followed by significant recruitment of CCR2+macrophages and a cellular response orchestrated by these cells. CCR2-/-mice showed an increase in CXCL-1 levels, followed by a replacement of the macrophage...
Brazil's biodiversity is extremely vast, but only a small fraction is used for research and d... more Brazil's biodiversity is extremely vast, but only a small fraction is used for research and development of medicines. Medicinal plants and secondary metabolites may represent the opportunity to develop effective and low-cost treatments. This literature review article seeks to promote the importance of Brazilian vegetable biodiversity in the development of health resources. For this, we searched in national and international databases (Scielo, Lilacs, Medline / Pubmed and Google Scholar). Despite having a wealth still unexplored, large areas of Cerrado, Amazon and Caatinga have already suffered deforestation. It is considered necessary and urgent that more governmental policies to protect these areas be developed in order to encourage the conservation of flora biodiversity, especially of medicinal plants, and to ensure the genetic variability and the phytochemical characteristics that are important sources for obtaining molecular identities for the pharmaceutical industry.
Revista Gestão Inovação e Tecnologias, 2018
O objetivo deste estudo foi realizar uma revisão literária a partir de artigos, dissertações e te... more O objetivo deste estudo foi realizar uma revisão literária a partir de artigos, dissertações e teses, e uma prospecção baseada na busca por patentes para apresentar uma visão geral das aplicações farmacológicas e tecnológicas relacionadas à utilização da goma do cajueiro (GC). As bases Periódicos Capes, ScienceDirect e Web of ScienceTM, foram acessadas para a busca por publicações e os bancos de patentes: USPTO, EPO, WIPO e INPI para a busca por patentes referentes a aplicação da GC na indústria farmacêutica, alimentícia e na área de nanotecnologia. Observou-se apenas 4 atividades farmacológicas para a GC: cicatrizante, antibacteriana, gastroprotetora e antidiarreica. Quanto às patentes, foram encontrados apenas dois registros na EPO relacionados à aplicação tecnológica de GC. Contudo, não havia nenhuma patente da GC relacionada a nanotecnologia, mostrando que o campo de pesquisa é bastante amplo nessa área. Observa-se, portanto, que é necessário maior investimento quanto à aplicação tecnológica da GC nas áreas farmacêutica e alimentícia.
Nutrients, 2019
This study aimed to evaluate the effect of Lactobacillus reuteri DSM 17938 (DSM) on ethanol-induc... more This study aimed to evaluate the effect of Lactobacillus reuteri DSM 17938 (DSM) on ethanol-induced gastric injury, and if its possible mechanism of action is related to inhibiting the transient receptor potential vanilloid type 1 (TRPV1). We evaluated the effect of supplementing 108 CFU•g body wt−1•day−1 of DSM on ethanol-induced gastric injury. DSM significantly reduced the ulcer area (1.940 ± 1.121 mm2) with 3 days of pretreatment. The effects of DSM supplementation were reversed by Resiniferatoxin (RTX), TRPV1 agonist (3 nmol/kg p.o.). Substance P (SP) (1 μmol/L per 20 g) plus 50% ethanol resulted in hemorrhagic lesions, and DSM supplementation did not reverse the lesion area induced by administering SP. TRPV1 staining intensity was lower, SP, malondialdehyde (MDA) and nitrite levels were reduced, and restored normal levels of antioxidant parameters (glutathione and superoxide dismutase) in the gastric mucosa in mice treated with DSM. In conclusion, DSM exhibited gastroprotectiv...
Nitric oxide : biology and chemistry, Jan 30, 2018
Activation of 5' adenosine monophosphate-activated protein kinase (AMPK) stimulates productio... more Activation of 5' adenosine monophosphate-activated protein kinase (AMPK) stimulates production of the gaseous mediators nitric oxide (NO) and carbon monoxide (CO), which are involved in mucosal defense and gastroprotection. As AMPK itself has gastroprotective effects against several gastric ulcer etiologies, in the present study, we aimed to elucidate whether AMPK may also prevent ethanol-induced injury and play a key role in the associated gastroprotection mediated by hydrogen sulfide (HS), NO, and CO. Mice were pretreated with AICAR (20 mg/kg, an AMPK activator) alone or with 50% ethanol. Other groups were pretreated with respective gaseous mediator inhibitors PAG, l-NAME, or ZnPP IX 30 min prior to AICAR, or with gaseous mediator donors NaHS, Lawesson's reagent and l-cysteine (HS), SNP, l-Arginine (NO), Hemin, or CORM-2 (CO) 30 min prior to ethanol with or without compound C (10 mg/kg, a non-selective AMPK inhibitor). HS, nitrate/nitrite (NO/NO), bilirubin levels, GSH and...
Nitric Oxide, 2017
Hydrogen sulphide (H 2 S) is a gasotransmitter that participates in various physiological and pat... more Hydrogen sulphide (H 2 S) is a gasotransmitter that participates in various physiological and pathophysiological processes within the gastrointestinal tract. We studied the effects and possible mechanism of action of H 2 S in secretory diarrhoea caused by cholera toxin (CT). The possible mechanisms of action of H 2 S were investigated using an intestinal fluid secretion model in isolated intestinal loops on anaesthetized mice treated with CT. NaHS and Lawesson's reagent and L-cysteine showed antisecretory activity through reduction of intestinal fluid secretion and loss of Cl À induced by CT. Pretreatment with an inhibitor of cystathionine-g-lyase (CSE), DL-propargylglycine (PAG), reversed the effect of L-cysteine and caused severe intestinal secretion. Co-treatment with PAG and a submaximal dose of CT increased intestinal fluid secretion, thus supporting the role of H 2 S in the pathophysiology of cholera. CT increased the expression of CSE and the production of H 2 S. Pretreatment with PAG did not reverse the effect of SQ 22536 (an AC inhibitor), bupivacaine (inhibitor of cAMP production), KT-5720 (a PKA inhibitor), and AICAR (an AMPK activator). The treatment with Forskolin does not reverse the effects of the H 2 S donors. Co-treatment with either NaHS or Lawesson's reagent and dorsomorphin (an AMPK inhibitor) did not reverse the effect of the H 2 S donors. H 2 S has antisecretory activity and is an essential molecule for protection against the intestinal secretion induced by CT. Thus, H 2 S donor drugs are promising candidates for cholera therapy. However, more studies are needed to elucidate the possible mechanism of action.
Journal of Pharmacy and Pharmacology, 2017
Objectives We aimed to determine whether carvacryl acetate acts as a TRPA1 receptor agonist and i... more Objectives We aimed to determine whether carvacryl acetate acts as a TRPA1 receptor agonist and its effects against irinotecan (CPT-11) induced intestinal mucositis in mice. Methods TRPA1 structure was obtained from a protein databank, and the 3D structure of carvacryl acetate was determined. Appropriate binding conformations were discovered via automatic docking simulations. To determine the effect of carvacryl acetate in vivo, mice were treated with either DMSO 2%, CPT-11, carvacryl acetate followed by CPT-11, or HC-030031, a TRPA1 antagonist, followed by carvacryl acetate. Jejunum samples were taken and structural, inflammatory and antioxidant parameters were studied. Key findings Eight amino acids residues in TRPA1 established stable interactions with carvacryl acetate, which led to pharmacological efficacy against CPT-11-induced intestinal mucositis via reduction of both neutropenia and bacteremia, increase in villi height and crypt depth, decrease in pro-inflammatory cytokines...
International journal of biological macromolecules, Jan 24, 2017
Inflammation is a protective reaction of the microcirculation. However, sustained inflammation ca... more Inflammation is a protective reaction of the microcirculation. However, sustained inflammation can lead to undesired effects. Thuja occidentalis Linn has many pharmacological properties but has no anti-inflammatory activity described. Thus, this study aims evaluating the anti-inflammatory activity of the aqueous extract (AE) and the polysaccharide fraction (PLS) of T. occidentalis L. in mice. The results of our evaluations in various experimental models indicated that AE and PLS (3, 10, and 30mg/kg, i.p.) reduced (p˂0.05) paw edema induced by carrageenan, dextran sulfate (DEX), compound 48/80, serotonin (5-HT), bradykinin (BK), histamine (HIST), and prostaglandin E2 (PGE2). Furthermore, it inhibited neutrophils recruitment; decreased MPO activity, tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) levels, vascular permeability, nitrite concentration, and MDA concentration; and maintained the GSH levels in the peritoneal exudate. The AE and PLS reduced neutrophil infiltration a...
Journal of Ethnopharmacology, 2015
Ethnopharmacological relevance: Anacardium occidentale L. (Anacardiaceae) is commonly known as th... more Ethnopharmacological relevance: Anacardium occidentale L. (Anacardiaceae) is commonly known as the cashew tree. It is native to tropical America and extracts of the leaves, bark, roots, chestnut net and exudate have been traditionally used in northeast Brazil for the treatment of various diseases. The exudate of the cashew tree (cashew gum) has been exploited by locals since ancient times for multiple applications, including the treatment of diarrheal diseases. Aim of the study: The primary aim of the present study is to evaluate the antidiarrheal activity of cashew gum (CG), a complex heteropolysaccharide from the exudate of the cashew tree, using various models. Materials and methods: The antidiarrheal activity of cashew gum (CG) against acute diarrhea was investigated using the castor oil-induced diarrhea model. The effects of CG on gastrointestinal transit and castor oil-and PGE 2-induced enteropooling were also examined in rodents. In addition, the effect of CG against secretory diarrhea was investigated using a model of fluid secretion in cholera toxin-treated intestinal closed loops in live mice. Results: Cashew gum (30, 60, and 90 mg/kg, p.o.) showed a significant (P < 0.05-0.01) antidiarrheal effect in rats with castor oil-induced diarrhea, inhibiting the total amount of stool and diarrheal stools. The 60 mg/kg dose of CG exhibited excellent antidiarrheal activity and significantly reduced the severity of diarrhea (diarrhea scores) in rats. CG (60 mg/kg) significantly (P < 0.05) decreased the volume of castor oil-and PGE 2-induced intestinal fluid secretion (enteropooling). In addition, similar to loperamide (standard drug, 5 mg/kg, p.o.), CG treatment reduced the distance travelled by a charcoal meal in the 30-min gastrointestinal transit model by interacting with opioid receptors. In cholera toxin-induced secretory diarrhea, CG (60 mg/kg) significantly inhibited the intestinal fluid secretion and decreased Clion loss in the cholera toxintreated isolated loops model of live mice by competitively binding to cholera toxin-GM1 receptors. Conclusions: In conclusion, our results indicate that a complex heteropolysaccharide extracted from the exudate of A. occidentale L. has antidiarrheal activity in acute, inflammatory, and secretory diarrhea models, which could justify its traditional use in the treatment of diarrhea in northeast Brazil. The antidiarrheal activity might be explained by the capacity of CG to inhibit gastrointestinal motility and thereby reduce the accumulation of intestinal fluid and the secretion of water and chloride ions in the lumen of the intestine.
Research, Society and Development
Type 2 diabetes mellitus (T2DM) is a chronic metabolic disorder that originates from numerous pat... more Type 2 diabetes mellitus (T2DM) is a chronic metabolic disorder that originates from numerous pathogenic mechanisms, all of which result in hyperglycemia. This disease is a major cause of morbidity and mortality worldwide. Effective prevention and treatment strategies for T2DM are therefore necessary. The purpose of this review was to summarize the pharmacotherapy for patients with T2DM by discussing its pathophysiology, the therapeutic classes used in treatment strategies, as well as the mechanisms of action for each one. A literature review was conducted by searching Google Scholar, PubMed, and Science Direct databases using the search terms: type 2 diabetes mellitus, insulin, AMPK, antidiabetic drugs, incretin, SGLT2, and biguanides covering studies up to 2022. The review identified and included studies including qualitative, original research articles, and randomized controlled trial designs. The results of this study are divided into drugs that increase insulin sensitivity (e.g...