Papers by Jose Carlos Tavares Carvalho
African Journal of Pharmacy and Pharmacology, 2017
Endopleura uchi (Huber) Cuatrec. (Humiriaceae), the Brazilian Amazon plant, is used in folk medic... more Endopleura uchi (Huber) Cuatrec. (Humiriaceae), the Brazilian Amazon plant, is used in folk medicine to treat arthritis and gastric ulcer. Bergenin, one of the chemical constituents of E. uchi, has antiinflammatory properties. Its acetylation results in acetylbergenin, which is extracted to investigate its potential anti-inflammatory and antiulcer properties using an assay for croton oil-induced ear edema, rat paw edema induced by carrageenan and dextran, carragenin-induced peritonitis, and stress-induced gastric ulcer. In ear erythema induced by croton oil, acetylbergenin presented a significant 75.60% inhibition (p<0.001). The oral administration of 6.8 mg/kg of acetylbergenin significantly inhibited the carrageenan-induced edema formation by 35.09% (p<0.05) and the dextran-induced edema by 33% (p<0.05). The migration of neutrophils toward the peritoneal cavity was inhibited in acetylbergenin (6.8 mg/kg) treated animals by 70% (p<0.01). In the stress-induced gastric ulcer, acetylbergenin inhibited 78.55% of gastric lesions. The results suggest that, the anti-inflammatory action of acetylbergenin appears to be dependent on cyclooxygenase (COX-2) inhibition. Furthermore, although the antiinflammatory activity of acetylbergenin is a characteristic of nonsteroidal compounds, it causes little deleterious interference in the gastric mucosa.
African Journal of Pharmacy and Pharmacology, 2019
Endopleura uchi (Huber) Cuatrec. is a tree found in the Brazilian Amazon, whose barks are used in... more Endopleura uchi (Huber) Cuatrec. is a tree found in the Brazilian Amazon, whose barks are used in folk medicine as an alternative treatment for inflammatory-related diseases. This review, performed using current available international scientific literature, aimed to survey biological activities reported from E. uchi, and describes its phytochemistry. In folk medicine, the barks are used to treat a range of conditions such as intestinal infections, inflammations, diabetes, arthritis, among others; the fruits have some unique nutritional benefits. Phytochemical studies with this plant species indicate the presence of tannins, saponins, and mainly bergenin (a coumarin) in the barks. Among biological activities reported using extracts from the barks are: Inhibition of acetylcholinesterase and butylcholinesterase, bacteriostatic and bactericidal activity, antidiabetic activity through inhibition of αglucosidase, anti-inflammatory and antioxidant activity. Bergenin, the most abundant molecule, has antimicrobial activity mainly against yeasts and anti-inflammatory activity apparently through mitogenactivated protein kinases (MAPK) and muclear factor kappa B (NF-κB) inhibition; its acetylated derivative acetylbergenin has analgesic and more prominent anti-inflammatory activity.
European review for medical and pharmacological sciences
Antimicrobial resistance is a subject of great concern in public health and also in the designing... more Antimicrobial resistance is a subject of great concern in public health and also in the designing of strategies for current therapeutic protocols all over the world. New drugs, including those necessary for a reserve armamentarium and exhibiting less side effects deserve special attention. In rural areas, particularly in Brazil, a huge number of natural products, in different artisanal preparations, mainly from plants, have been used by traditional populations to cure diseases. Despite some of these plants have been studied, many of them are awaiting to have their compounds chemically characterized and investigated their pharmacodynamics properties. Further, as well known, the environment plays a crucial role in the metabolism of these plants, yielding different and varied molecular complexes depending on the period of collection, climate conditions, kind of soil and also the plant speciation. In this report, ethanol crude extract of 10 different botanical specimens from the Amazon ...
Applied Biochemistry and Biotechnology, 2008
Antioxidative and hepatoprotective activity of a cultured lichen Usnea ghattensis has been studie... more Antioxidative and hepatoprotective activity of a cultured lichen Usnea ghattensis has been studied. The methanolic extract of cultured lichen U. ghattensis showed good antioxidant activity by preventing lipid peroxidation by 67% and 86% in Trolox-equivalent antioxidant capacity at 20 microg/ml. It also showed superoxide, 1,1-diphenyl-2-picrylhydrazyl, nitric oxide, and hydroxyl radical-scavenging activity, 89%, 89.6%, 94.8%, and 89.6%, respectively, and found levels higher then that known for the synthetic antioxidants butylated hydroxytoluene, butylated hydroxyanisol, and quercetin at 20 microg/ml concentration. The cultured lichen extract also showed hepatoprotection against ethanol-induced toxicity in the mice liver slice culture model by a significant decrease in the antioxidant enzymes, glutathione peroxidase, catalase, and superoxide dismutase, along with a decrease in lipid peroxidation and lactate dehydrogenase release.
African Journal of Traditional, Complementary and Alternative Medicines, 2010
Acta Pharmaceutica, 2008
Anti-inflammatory and analgesic activities of some newly synthesized pyridinedicarbonitrile and b... more Anti-inflammatory and analgesic activities of some newly synthesized pyridinedicarbonitrile and benzopyranopyridine derivativesIn continuation of our search for new substituted pyridine based anti-inflammatories, reaction of 1-(2-thienyl or furanyl)-3-(2-hydroxyphenyl)-2-propen-1-ones (1) with malononitrile in alcoholic KOH solution afforded a mixture of 4-alkoxy-2-(2-thienyl or furanyl)-5H-[1]benzopyrano[3,4-c]pyridine-5-ones (2) and 2-alkoxy-4-amino-6- (2-thienyl or furanyl)-3,5-pyridinedicarbonitriles (3). Some of the synthesized compounds were evaluated for their anti-inflammatory and analgesic activities compared to diclofenac potassium as positive control. Detailed synthesis, spectroscopic and toxicity data are reported.
Acta Pharmaceutica, 2007
Fumaria indica (Hausskn.) Pugsley, syn: F. parviflora Lam. (Fumariaceae) is a small, scandent, br... more Fumaria indica (Hausskn.) Pugsley, syn: F. parviflora Lam. (Fumariaceae) is a small, scandent, branched annual herb growing wild in plains and lower hills. The plant is considered to be diuretic, diaphoretic, anthelmintic, laxative and is used to purify blood and in liver obstruction in ethnopharmacology (1, 2). Pharmacological studies show that F. indica possesses antipyretic, antidiarrhoeal and hypoglycemic properties (3-5). It is a smooth muscles relaxant and has hydrocholeretic, by stimulating bile excretion, and hepatoprotective effects (6-10). Phytochemical investigation revealed the presence of alkaloids, viz. protopine (6), parfumine, cryptopine, copticine, fumariline (11), fumaramine, fumaritine, paprafumicin, paprarine, papracinine, papraline, reddeanine (12), fumarophycine (13), narlumicine, narceimine, narlumidine (14); steroids, viz. b-sitosterol, stigmasterol, campesterol; organic acids viz. caffeic acid and fumaric acid (9, 13). As there is no reference in literature to the anti-inflammatory aspects, it was considered worthwhile to study the anti-inflammatory and anti-nociceptive activity of the Fumaria indica whole plant.
Journal of Nanomedicine Research, 2016
Introduction: Perillyl alcohol (POH) is a hydroxylated monocyclic monoterpene found in lemon and ... more Introduction: Perillyl alcohol (POH) is a hydroxylated monocyclic monoterpene found in lemon and lavender essential oils, among others. It's widely recognized by antitumoral activity. Despite the great potential of nanoformulations for pharmaceutics, to the date the obtainment a perillyl alcohol-nanoemulsion (NPOH) and its toxicity investigation were not previously reported. On this context, the present study aim to evaluate the toxicity of NPOH on zebrafish (Danio rerio). Lethal concentration (LC50), effects on behaviour and acute administrations effects (48h) on histopathological parameters of the gills, liver and kidneys were performed. Results: Exposure to different concentrations of NPOH (25, 35, 50 e 125 µg/Lexpressed as POH content) allowed determination of LC50= 33.4 µg/L. Moreover, NPOH at 50 and 125 µg/L induced 100% of mortality, in addition the alterations of behavior. NPOH at 25 and 35 µg/L induced higher damage to gills tissue when compared to remaining concentrations and control group (surfactant at 125 µg/L) (p < 0.001, p < 0.01 and p < 0.05, Anova, Tukey-Kramer test). NPOH at 25, 35 e 50 µg/L induced significative damage to liver tissue, when compared to control (p < 0.01 and p < 0.05). No significant histopathological alterations were observed in kidneys. Thus, our results suggest that NPOH present toxicity pattern in accordance to nanoformulations and xenobiotics.
Journal of Nanobiotechnology, Jan 3, 2017
Background: Preparation of nanoformulations using natural products as bioactive substances is con... more Background: Preparation of nanoformulations using natural products as bioactive substances is considered very promising for innovative larvicidal agents. On this context, oil in water nanoemulsions develop a main role, since they satisfactorily disperse poor-water soluble substances, such as herbal oils, in aqueous media. Pterodon emarginatus, popularly known as sucupira, has a promising bioactive oleoresin. However, to our knowledge, no previous studies were carried out to evaluate its potential against Culex quinquefasciatus, the main vector of the tropical neglected disease called lymphatic filariasis or elephantiasis. Thus, we aimed to investigate influence of different pairs of surfactants in nanoemulsion formation and investigate if a sucupira oleoresin-based nanoemulsion has promising larvicidal activity against this C. quinquefasciatus. We also evaluated morphological alteration, possible mechanism of insecticidal action and ecotoxicity of the nanoemulsion against a non-target organism. Results: Among the different pairs of surfactants that were tested, nanoemulsions obtained with polysorbate 80/ sorbitan monooleate and polysorbate 80/sorbitan trioleate presented smallest mean droplet size just afterwards preparation, respectively 151.0 ± 2.252 and 160.7 ± 1.493 nm. They presented high negative zeta potential values, low polydispersity index (<0.300) and did not present great alteration in mean droplet size and polydispersity index after 1 day of preparation. Overall, nanoemulsion prepared with polysorbate 80/sorbitan monooleate was considered more stable and was chosen for biological assays. It presented low LC 50 value against larvae (34.75; 7.31-51.86 mg/L) after 48 h of treatment and some morphological alteration was observed. The nanoemulsion did not inhibit acetylcholinesterase of C. quinquefasciatus larvae. It was not toxic to green algae Chlorella vulgaris at low concentration (25 mg/L). Conclusions: Our results suggest that optimal nanoemulsions may be prepared with different surfactants using a low cost and low energy simple method. Moreover, this prototype proved to be effective against C. quinquefasciatus, being considered an ecofriendly novel nanoproduct that can be useful in integrated control programs of vector control.
Molecules
The species Trattinnickia rhoifolia Willd, (T. rhoifolia), which belongs to the Burseraceae famil... more The species Trattinnickia rhoifolia Willd, (T. rhoifolia), which belongs to the Burseraceae family, is widely used in ethnopharmacological cultural practices by traditional Amazonian people for anti-inflammatory purposes, sometimes as their only therapeutic resource. Although it is used in teas, infusions, macerations and in food, the species is still unexplored in regard to its pharmacophoric potential and chemical profile. Therefore, the aim of this study was to conduct a phytochemical characterization of the hydroethanolic extract of T. rhoifolia leaves (HELTr) and to evaluate the acute toxicity and anti-inflammatory activity of this species using zebrafish (Danio rerio). The extract was analyzed by gas chromatography–mass spectrometry (GC-MS). The evaluation of the acute toxicity of the HELTr in adult zebrafish was determined using the limit test (2000 mg/kg), with behavioral and histopathological evaluations, in addition to the analysis of the anti-inflammatory potential of HEL...
Nutraceuticals
Dyslipidemia is a metabolic condition linked to increased morbidity. This study aimed to evaluate... more Dyslipidemia is a metabolic condition linked to increased morbidity. This study aimed to evaluate the effect of two new nutraceuticals derived from annatto (Bixa orellana), açaí (Euterpe oleracea), and soybean germ or red clover isoflavones (Trifolium pratense) against high-fat-induced dyslipidemia in female Wistar rats. The formulations were assessed through GC-MS and HPLC-UV/Vis. Next, female Wistar rats received daily administrations of coconut oil and were treated with Ormona® SI (OSI), Ormona® RC (ORC), soybean germ (SG), simvastatin (simv.), simvastatin + Ormona® SI (simv. + OSI), or only distilled water (control). Biochemical tests were performed using the animals’ blood, and their arteries were screened for atheroma formation. The results show abnormal TC, TG, LDL, and HDL levels caused by the high-fat diet, increased glucose levels, hepatotoxicity, nephrotoxicity, and atherogenesis. The nutraceuticals significantly ameliorated all conditions, with results that are similar t...
Baicalein (BA) is a flavonoid with wide-ranging pharmacological activity. However, its biological... more Baicalein (BA) is a flavonoid with wide-ranging pharmacological activity. However, its biological evaluation is hampered by its low solubility in aqueous medium, making forms of incorporation that improve its solubility necessary. In the present study, BA was combined with a solution of silk fibroin protein (SF), a biomaterial used as a drug carrier, to evaluate the anti-inflammatory potential of this combination, in vivo, in an experimental model, zebrafish (Danio rerio). Baicalein-Silk fibroin (BASF) improved the DPPH (2,2‐diphenyl‐1‐picryl‐hydrazyl‐hydrate) free radical scavenging rate (95%) in comparison with BA in solution. The acute toxicity study and histopathological analysis in zebrafish showed that BASF showed low cytotoxic potential up to a dose of 2.000 mg/kg. The use of BA in combination with SF enhanced the anti-inflammatory effect of flavonoids by inducing inflammatory peritoneal edema through carrageenan and achieved 77,6% inhibition of abdominal edema at a dose of 7...
Molecules, 2021
This study aimed to evaluate and compare the effects of co-treatment with purified annatto oil (P... more This study aimed to evaluate and compare the effects of co-treatment with purified annatto oil (PAO) or its granules (GRA, Chronic®) with that of testosterone on the orchiectomy-induced osteoporosis in Wistar rats. After surgery, rats were treated from day 7 until day 45 with testosterone only (TES, 7 mg/kg, IM) or TES + PAO or GRA (200 mg/kg, p.o.). The following parameters were evaluated: food/water intake, weight, HDL, LDL, glucose, triglycerides (TG), total cholesterol (TC), alkaline phosphatase levels, blood phosphorus and calcium contents, femur weight, structure (through scanning electron microscopy), and calcium content (through atomic absorption spectrophotometry). Our results show that orchiectomy could significantly change the blood lipid profile and decrease bone integrity parameters. Testosterone reposition alone could improve some endpoints, including LDL, TC, bone weight, and bone calcium concentration. However, other parameters were not significantly improved. Co-tre...
The Aedes aegypti mosquito is a vector of several diseases, such as dengue, malaria and the Zika ... more The Aedes aegypti mosquito is a vector of several diseases, such as dengue, malaria and the Zika virus. Synthetic insecticides such as chlorpyrifos and chlorothalonil have been used for plague control, despite causing damage to the environment and to humans. It is therefore important to study natural active compounds with a low environmental impact. The present paper developed an environmentally friendly formulation of silk fibroin (SF) associated with fatty acid esters [ethyl (FAEE-SF), propyl (FAPE-SF) and butyl (FABE-SF)] from Astrocaryum murumuru Mart. fat, which was effective against Aedes aegypti 3th instar larvae. The FABE-SF nanoemulsion induced a higher mortality rate in the larvae of the A. aegypti after 48 h (LC50 = 18.92 µg / mL). The stabilities of the nanoemulsions were monitored for 21 days, and FABE-SF exhibited greater stability throughout the monitored period, with average particle, zeta and PDI values of around 217 ± 0.85 nm, -25.6 ± 3.24 mV and 0.338 ± 0.01, resp...
Inflammopharmacology, 2021
Fatty amides (N-alkylamides) are a group of bioactive lipids widely distributed in microorganisms... more Fatty amides (N-alkylamides) are a group of bioactive lipids widely distributed in microorganisms, animals, and plants. The low yield in the extraction process of spilantol, a grease amide, which has been related mainly to diverse biological effects, compromises its application on a large scale. Thus, this study proposed an alternative to the synthesis of fatty amides from Bertholletia excelsa (AGBe) oil, with a chemical structure similar to that of spilantol. In vivo models induced by carrageenan were used in Zebra sh (Danio rerio). In in vivo studies, oral AGBe produced no signs of toxicity. In the histopathological study, AGBe did not cause signi cant changes in the main metabolizing organs (liver, kidneys, and intestines). In the anti-in ammatory evaluation, all doses (45 mg/kg, 500 mg/kg, and 1000 mg/kg) were effective, signi cantly reducing edema and producing a dose-response effect when compared to spilantol. In the in silico study, with the use of molecular docking, he showed that among the AGBe, the molecules 18:1, ω-7-ethanolamine and 18:1, ω-9-ethanolamine stood out, which had 21 interactions for COX-2 and 20 interactions for PLA 2 , respectively, surpassing the spilantol standard with 15 interactions for COX-2 and PLA 2. The hypothesis of anti-in ammatory action was con rmed in the in silico study, demonstrating the involvement of AGBe in the process of inhibiting the enzymes COX-2 and PLA 2. Therefore, based on all the results obtained and the fact that until the dose of 1000 mg/kg, orally, in zebra sh, it was not possible to determine the LD 50 , it can be said that AGBe is effective and safe for the activity anti-in ammatory.
Pharmaceuticals, 2021
Hancornia speciosa Gomes is a tree native to Brazil and has therapeutic potential for several dis... more Hancornia speciosa Gomes is a tree native to Brazil and has therapeutic potential for several diseases. Ethnopharmacological surveys have reported that the plant is used as a hypoglycemic agent and to lose weight. This study aimed to evaluate the effects of the aqueous extract from H. speciosa latex (LxHs) in a zebrafish model of diabetes. The extract was evaluated through high-performance thin-layer chromatography (HTPLC), nuclear magnetic resonance (NMR), and Fourier-transform infrared spectroscopy (FT-IR). We then tested treatments with LxHs (500, 1000, and 1500 mg/kg) by assessing blood glucose levels in alloxan-induced diabetic animals, and metformin was used as a control. The toxicity was evaluated through histopathology of the pancreas and biochemical assessment of serum levels of AST, ALT, creatinine, and urea. The extract was also assessed for acute toxicity through several parameters in embryos and adult animals. Finally, we performed in silico analysis through the SEA ser...
Journal of Fish Diseases, 2017
Outbreaks of diseases pose a major threat to sustainable aquaculture development worldwide. Appli... more Outbreaks of diseases pose a major threat to sustainable aquaculture development worldwide. Application of herbal products to combat parasitic diseases provides an alternative approach for sustainable aquaculture. This study investigated the in vitro antiparasitic effects of an oil‐in‐water nanoemulsion prepared using the essential oil from Pterodon emarginatus, against monogeneans infesting Colossoma macropomum. Gill arches from C. macropomum (47.6 ± 14.5 g and 13.5 ± 1.4 cm) that were naturally parasitized by Anacanthorus spathulatus, Notozothecium janauachensis and Mymarothecium boegeri were immersed in different dispersions of the P. emarginatus nanoemulsions (0, 50, 100, 200, 400 and 600 mg/L). The major compounds presented in the essential oil of P. emarginatus were β‐elemene, β‐caryophyllene and α‐humulene. Characterization of these nanoemulsions showed that they have a small mean droplet size and low polydispersity index, which is concordant with stable systems. In this in v...
Revista Brasileira de Farmacognosia, 2018
Diabetes mellitus is a syndrome that reaches more than 382 million people worldwide. It interfere... more Diabetes mellitus is a syndrome that reaches more than 382 million people worldwide. It interferes with the metabolism of carbohydrates, causing chronic hyperglycemia. The objective of this study was to evaluate the effect of the Copaifera duckei, Dwyer, Fabaceae, oleoresin on streptozotocin-induced (STZ) diabetic rats. This study was based on the induction of diabetes mellitus by streptozotocin (55 mg/kg, i.p.) in Wistar rats and treated with doses of C. duckei oleoresin (250 and 500 mg/kg, p.o.). Subsequently, the clinical, biochemical and histopathological of the pancreas parameters were evaluated. Gas chromatographic analysis indicated that -bisabolene (22.29%), -caryophyllene (21.25%) and ␣-farnesene (15.58%) sesquiterpenes were the major components of the C. duckei oleoresin. In streptozotocin-induced diabetes mellitus, it was possible to observe that the C. duckei oleoresin treatment had a significant effect (p < 0.001) on the clinical parameters, and that there was a positive improvement. This was attenuated by the urea, creatinine, and transaminases alterations (p < 0.001) observed in animals with diabetes mellitus, as well as the significantly reduced (p < 0.001) values of total cholesterol, triacylglycerides, and glucose. In the histopathological analyses of the pancreas, it was observed that the C. duckei oleoresin was able to restore -cells and to significantly increase the quantity and diameter of the Langerhans islets (p < 0.05), when compared to the diabetic group. The treatment with C. duckei oleoresin, employed under the conditions of this study, presented antidiabetic activity and can improve the complications found in this syndrome.
Revista Brasileira de Farmacognosia, 2018
Aedes aegypti (Diptera: Culicidae) is the main vector of some neglected diseases, including dengu... more Aedes aegypti (Diptera: Culicidae) is the main vector of some neglected diseases, including dengue. It is very important to develop formulations that increase effectiveness of vector control with low toxicity. Quercetin is a plant-derived flavonoid that modulates the development of some insects. The low water solubility of quercetin impairs the development of water-dispersible commercial products. To circumvent this problem, the preparation of nanoformulations is considered promising. Thus, this study aimed to evaluate the effect of bulk and quercetin nanosuspension against A. aegypti larvae and also to investigate their ecotoxicity. Quercetin nanosuspension was produced by a solvent displacement method followed by solvent evaporation and was maintained in two different temperatures (4 and 25 • C). Its size distribution and zeta potential were monitored along 30 days. The influence of quercetin nanosuspension and bulk-quercetin was investigated at various concentrations against A. aegypti and the green algae Chlorella vulgaris. The quercetin nanosuspension presented higher stability at 4 • C and negative zeta potential values. Quercetin nanosuspension and bulk-quercetin adversely affected the larvae development, especially at the highest concentrations. Larvae mortality was between 44% and 100% (48 h) for quercetin nanosuspension at 100 and 500 ppm, respectively. The bulk-quercetin induced around 50% mortality regardless the concentration used at this same time-period. Absence of emerging mosquitoes from water was observed on the survival larvae of all the treated groups. Quercetin nanosuspension was less toxic than bulk-quercetin against C. vulgaris, especially at higher concentrations. These data indicate that quercetin nanosuspension may represent a potential larvicide for A. aegypti control, once they induced larvae death and inhibited the survival ones to emerge from water. In addition, it did not demonstrated ecotoxicity against a non-target organism, highlighting its better properties, when compared to the bulk-quercetin.
Toxicology Reports, 2020
Endopleura uchi, is used for the treatment of inflammatory disease and related to the female repr... more Endopleura uchi, is used for the treatment of inflammatory disease and related to the female reproductive tract. The aim of this study was to evaluate the acute toxicity of the Endopleura uchi stem bark hydroethanolic extract (EEu) in zebrafish, emphasizing the histopathological and biochemical parameters, as well as evaluating the in silico pharmacokinetic and toxicological parameters of the phytochemical/pharmacological marker, bergenin, as their metabolites. The animals were orally treated with EEu at a single dose of 75 mg/kg, 500 mg/kg, 1000 mg/ kg and 3000 mg/kg. the oral LD 50 of the EEu higher to the dose of 3000 mg/kg. Behavioral, biochemical and histopathological changes were dose dependent. In silico pharmacokinetic predictions for bergenin and its metabolites showed moderate absorption in high human intestinal absorption (HIA) and Caco-2 models, reduced plasma protein binding, by low brain tissue binding and no P-glycoprotein (P-Gp) inhibition. Their metabolism is defined by the CYP450 enzyme, in addition to bergenin inhibition of CYP2C9, CYP3A4 and CYP2C19. In the bergenin and its metabolites in silico toxicity test it have been shown to cause carcinogenicity and a greater involvement of the bergenin with the CYP enzymes in the I and II hepatic and renal metabolism's phases was observed. It is possible to suggest that the histopathological damages are involved with the interaction of this major compound and its metabolites at the level of the cellular-biochemical mechanisms which involve the absorption, metabolization and excretion of these possible prodrug and drug. 1. Introduction Yellow uchi, scientifically known as Endopleura uchi, is a medicinal plant belonging to the family Humiriaceae. It is a species of the non-flooded forest, that presents high canopy and fruits very appreciated by the people, throughout the Brazilian Amazon [1]. The stem stumps are used in the form of tea, in traditional medicine for the treatment of arthritis, rheumatism, hypercholesterolemia and diabetes mellitus with
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Papers by Jose Carlos Tavares Carvalho