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1.
J Toxicol Environ Health A ; 87(16): 662-673, 2024 Aug 17.
Artículo en Inglés | MEDLINE | ID: mdl-38808737

RESUMEN

Pseudobombax marginatum, popularly known as "embiratanha," is widely used by traditional communities as anti-inflammatory and analgesic agent. This study aimed to determine the phytochemical profile as well as cytotoxicity, acute oral toxicity, genotoxicity, and mutagenicity attributed to exposure to aqueous (AqEx) and ethanolic (EtEx) extracts of embiratanha bark. Phytochemical screening was conducted using thin-layer chromatography (TLC). Cell viability was analyzed using MTT assay with human mammary gland adenocarcinoma (MDA-MB-231) and macrophage (J774A.1) cell lines, exposed to concentrations of 12.5, 25, 50, or 100 µg/ml of either extract. For acute oral toxicity, comet assay and micronucleus (MN) tests, a single dose of 2,000 mg/kg of either extract was administered orally to Wistar rats. TLC analysis identified classes of metabolites in the extracts, including cinnamic acid derivatives, flavonoids, hydrolyzable tannins, condensed tannins, coumarins, and terpenes/steroids. In the cytotoxicity assay, the varying concentrations of extracts derived from embiratanha induced no significant alterations in the viability of MDA-MB-231 cells. The lowest concentration of EtEx significantly increased macrophage J774A.1 viability. However, the higher concentrations of AqEx markedly lowered macrophage J774A.1 viability. Animals exhibited no toxicity in the parameters analyzed in acute oral toxicity, comet assay, and MN tests. Further, EtEx promoted a significant reduction in DNA damage index and DNA damage frequency utilizing the comet assay, while the group treated with AqEx exhibited no marked differences. Thus, data demonstrated that AqEx or EtEx of embiratanha may be considered safe at a dose of 2,000 mg/kg orgally under our experimental conditions tested.


Asunto(s)
Extractos Vegetales , Ratas Wistar , Extractos Vegetales/toxicidad , Extractos Vegetales/química , Animales , Humanos , Ratas , Línea Celular Tumoral , Masculino , Ensayo Cometa , Pruebas de Micronúcleos , Femenino , Supervivencia Celular/efectos de los fármacos , Fitoquímicos/toxicidad , Fitoquímicos/análisis , Ratones , Corteza de la Planta/química , Mutágenos/toxicidad , Pruebas de Mutagenicidad , Etanol/química
2.
J Toxicol Environ Health A ; 87(12): 497-515, 2024 Jun 17.
Artículo en Inglés | MEDLINE | ID: mdl-38619158

RESUMEN

One prominent aspect of Parkinson's disease (PD) is the presence of elevated levels of free radicals, including reactive oxygen species (ROS). Syagrus coronata (S. coronata), a palm tree, exhibits antioxidant activity attributed to its phytochemical composition, containing fatty acids, polyphenols, and flavonoids. The aim of this investigation was to examine the potential neuroprotective effects of S. coronata fixed oil against rotenone-induced toxicity using Drosophila melanogaster. Young Drosophila specimens (3-4 d old) were exposed to a diet supplemented with rotenone (50 µM) for 7 d with and without the inclusion of S. coronata fixed oil (0.2 mg/g diet). Data demonstrated that rotenone exposure resulted in significant locomotor impairment and increased mortality rates in flies. Further, rotenone administration reduced total thiol levels but elevated lipid peroxidation, iron (Fe) levels, and nitric oxide (NO) levels while decreasing the reduced capacity of mitochondria. Concomitant administration of S. coronata exhibited a protective effect against rotenone, as evidenced by a return to control levels of Fe, NO, and total thiols, lowered lipid peroxidation levels, reversed locomotor impairment, and enhanced % cell viability. Molecular docking of the oil lipidic components with antioxidant enzymes showed strong binding affinity to superoxide dismutase (SOD) and glutathione peroxidase (GPX1) enzymes. Overall, treatment with S. coronata fixed oil was found to prevent rotenone-induced movement disorders and oxidative stress in Drosophila melanogaster.


Asunto(s)
Trastornos del Movimiento , Rotenona , Animales , Drosophila melanogaster , Simulación del Acoplamiento Molecular , Estrés Oxidativo , Antioxidantes/farmacología , Óxido Nítrico/metabolismo
3.
Inflammopharmacology ; 32(1): 595-602, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-37823930

RESUMEN

Wounds encompass physical, chemical, biological, induced damages to the skin or mucous membranes. In wound treatment, combating infections is a critical challenge due to their potential to impede recovery and inflict systemic harm on patients. Previously, the essential oil extracted from Psidium glaziovianum (PgEO) demonstrated antinociceptive and anti-inflammatory attributes, along with negligible oral toxicity. Hence, our study aimed to assess the effects of topically applying a gel formulation containing PgEO to excisional wounds in mice. Additionally, an in vitro antimicrobial assessment was conducted. The formulated gel underwent characterization and toxicological evaluation on erythrocytes, as well as a dermal irritation test. Its antimicrobial activity was tested against both gram-positive and gram-negative bacteria, as well as fungi. Subsequently, an assessment of its efficacy in excisional wound healing was conducted in mice. The findings of this investigation highlight the gel's efficacy against both gram-positive and gram-negative bacteria, as well as fungi. Moreover, this study underscores that the PgEO-gel treatment enhances skin wound healing, potentially due to its capacity to trigger antioxidant enzymes and suppress pro-inflammatory cytokines. Furthermore, the gel exhibited minimal toxicity to erythrocytes and skin irritation. These findings hold promise for prospective preclinical and clinical trials across diverse wound types. In conclusion, this study sheds light on the potential therapeutic applications of the gel formulation containing essential oil from P. glaziovianum in the context of wound healing.


Asunto(s)
Aceites Volátiles , Psidium , Humanos , Animales , Ratones , Antibacterianos , Estudios Prospectivos , Bacterias Gramnegativas , Bacterias Grampositivas , Cicatrización de Heridas , Aceites Volátiles/farmacología
4.
Parasitol Int ; 98: 102820, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-37884077

RESUMEN

Aedes aegypti, a mosquito, is responsible for the spread of many diseases, including dengue, zika, and chikungunya. However, due to this mosquito's developed resistance to conventional pesticides, effectively controlling it has proven to be challenging. This study aimed to evaluate the insecticidal potential of the essential oil from the leaves of Eugenia stipitata against Ae. aegypti, offering a natural and sustainable alternative for mosquito control. Tests were conducted using third-stage larvae to evaluate larvicidal activity and pupae collected up to 14 h after transformation to investigate pupicidal activity. Throughout the bioassays, the organisms were exposed to various essential oil concentrations. The findings demonstrated that the essential oil of E. stipitata exhibited larvicidal action, resulting in 100% larval mortality after 24 h and an LC50 value of 0.34 mg/mL. The effectiveness of essential oil as a pupicidal agent was also demonstrated by its LC50 value of 2.33 mg/mL and 100% larval mortality in 24 h. It can be concluded that the essential oil of E. stipitata holds promise as a natural pest control agent. Its use may reduce the reliance on conventional chemical pesticides, providing a more sustainable and effective strategy to combat diseases spread by mosquitoes.


Asunto(s)
Aedes , Insecticidas , Aceites Volátiles , Infección por el Virus Zika , Virus Zika , Animales , Insecticidas/farmacología , Aceites Volátiles/farmacología , Aceites Volátiles/química , Hojas de la Planta/química , Larva , Extractos Vegetales/química
5.
Inflammopharmacology ; 31(6): 3143-3151, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37498376

RESUMEN

Myrciaria floribunda is a plant that is distributed across different Brazilian biomes such as the Amazon, Caatinga, Cerrado, and Atlantic Forest, and it possesses antioxidant, antimicrobial, and anticancer properties. The antinociceptive and anti-inflammatory properties of the essential oil from M. floribunda leaves (MfEO) were examined in this study using mouse models. Gas chromatography-mass spectrometry was employed to describe the oil, and the results revealed that δ-cadinene, bicyclogermacrene, α-cadinol, and epi-α-muurolol predominated in the chemical profile. The oil stimulated a decrease in nociception in the chemical and thermal models used to evaluate acute antinociceptive activity. Findings from the use of pain pathway blockers to study the presumed underlying mechanism indicated opioid pathway activity. The anti-edematogenic effect, decreased cell migration, and generation of pro-inflammatory cytokines provided evidence of the anti-inflammatory potential of the essential oil from M. floribunda. According to this research, the essential oil from M. floribunda can effectively alleviate acute pain and inflammation.


Asunto(s)
Antiinfecciosos , Aceites Volátiles , Ratones , Animales , Aceites Volátiles/farmacología , Antiinflamatorios/farmacología , Antiinflamatorios/química , Antioxidantes/farmacología , Antiinfecciosos/farmacología , Extractos Vegetales/química , Analgésicos/farmacología , Analgésicos/química , Hojas de la Planta/química
6.
J Toxicol Environ Health A ; 86(16): 557-574, 2023 08 18.
Artículo en Inglés | MEDLINE | ID: mdl-37350297

RESUMEN

This study aimed to characterize the phytochemical profile of bark and leaves aqueous extract Commiphora leptophloeos, and conduct in vivo and in vitro assays to determine the presence of any toxicological consequences due to exposure. The phytochemical analysis was carried out using high-performance liquid chromatography (HPLC). The antioxidant activity was estimated utilizing DPPH free radical scavenging and phosphomolybdenum assays. Cell viability was measured by the MTT method on J774 and human adenocarcinoma cells, which were treated with concentrations of 12,5, 25, 50, 100 or 200 µg/ml of both extracts. Acute oral toxicity, genotoxicity, and mutagenicity assays were determined using a single oral dose of 2000 g/kg in male Swiss albino mice (Mus musculus). Biochemical analysis of the blood and histological analyses of the kidneys, liver, spleen, pylorus, duodenum and jejunum were undertaken. Genotoxicity and mutagenicity were determined utilizing blood samples. Gallic acid, catechin, and epicatechin were identified in the bark and chlorogenic acid in leaves. Data demonstrated a high content of phenolic compounds and flavonoids associated with significant antioxidant potential. No significant signs in damage or symptoms of toxicity were detected. No marked reduction in cell viability was found at lower concentrations tested. On histomorphometry, only the gastrointestinal organs exhibited significant difference. Renal hepatic and blood parameters were within the normal range. No apparent signs of toxicity, genotoxicity, mutagenicity or cytotoxicity were found in vivo and in vitro experiments.


Asunto(s)
Antioxidantes , Catequina , Ratones , Animales , Masculino , Humanos , Antioxidantes/química , Extractos Vegetales/toxicidad , Extractos Vegetales/química , Commiphora , Corteza de la Planta/química , Fitoquímicos/toxicidad , Hojas de la Planta/química
7.
J Ethnopharmacol ; 303: 115955, 2023 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-36436714

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Members of the Psidium genus have been suggested in ethnobotanical research for the treatment of various human diseases, and some studies have already proven their popular uses through research, such as Psidium glaziovianum, which is found in Brazil's northeast and southeast regions and has antinociceptive and anti-inflammatory properties; however, the safety of use has not yet been evaluated. AIM OF THE STUDY: This study investigated the safety of using essential oil obtained from P. glaziovianum leaves (PgEO) in vitro and in vivo models. MATERIALS AND METHODS: Cytotoxicity was evaluated in murine erythrocytes, while acute toxicity, genotoxicity (comet assay) and mutagenicity (micronucleus test) studies were performed using Swiss albino mice. RESULTS: In the cytotoxicity assay, the hemolysis rate indicated a low capacity of PgEO to cause cell lysis (0.33-1.78%). In the acute oral toxicity study, animals treated with up to up to 5000 mg/kg body weight did not observe mortality or physiological changes. Neither dosage caused behavioral problems or death in mice over 14 days. The control and 2,000 mg/kg groups had higher feed intake and body weight than the 5,000 mg/kg PgEO group. Erythrocyte count, hemoglobin level, mean corpuscular volume, and MCV decreased, but serum alanine and aspartate aminotransferases increased. In the genotoxic evaluation, 5000 mg/kg PgEO enhanced nucleated blood cell DI and DF. CONCLUSIONS: The present study describes that PgEO can be considered well tolerated in acute exposure at doses up to 2000 mg/kg, however the dose of 5000 mg/kg of PgEO should be used with caution.


Asunto(s)
Aceites Volátiles , Psidium , Ratones , Humanos , Animales , Aceites Volátiles/farmacología , Mutágenos , Daño del ADN , Ensayo Cometa , Extractos Vegetales/farmacología , Pruebas de Mutagenicidad
8.
Chem Biodivers ; 19(9): e202200034, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-35864035

RESUMEN

The purpose of this study was to analyses the influence of seasonal variation on the chemical composition and antimicrobial, antioxidant and cytotoxicity activities of the essential oil (EO) extracted from the leaves of Eugenia pohliana. Chemical characterization of the samples - by gas chromatography-mass spectrometry - found 35 and 38 components for summer and winter, respectively, of the EO from E. pohliana leaves, totaling 47 different compounds. Analysis of antioxidant capacity (DPPH, ABTS and TAC) revealed that the summer EO showed greater free radical scavenging capacity than the winter. Similarly, the summer EO exhibited superior antimicrobial potential (MIC=128-512 µg/mL and MMC=128-1024 µg/mL, compared to the winter EO (128-2048 µg/mL and 256-2048 µg/mL, respectively). Results showed that both oils had a low potential to cause hemolysis. This study provides new scientific evidence on the influence of seasonality on the pharmacological properties of E. pohliana leaves and its potential for the development of herbal medicines.


Asunto(s)
Antiinfecciosos , Eugenia , Aceites Volátiles , Antibacterianos/farmacología , Antiinfecciosos/farmacología , Antioxidantes/química , Radicales Libres , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/química , Hojas de la Planta/química , Estaciones del Año
9.
Inflammopharmacology ; 30(2): 599-607, 2022 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-35257283

RESUMEN

Plants of the genus Psidium have been employed in "in natura" consumption and agroindustry, and owing to the diversity of phytochemicals, the development of new pharmaceutical forms has received remarkable research interest. In this study, the essential oil obtained from Psidium glaziovianum (PgEO) leaves were evaluated antinociceptive and anti-inflammatory activities were evaluated in mouse models. Initially, PgEO was characterized by gas chromatography-mass spectrometry and gas chromatography with flame ionization detection, and the profile was dominated by sesquiterpene compounds. In the evaluation of acute antinociceptive activity (abdominal contortions induced by acetic acid, formalin, tail immersion, and hot plate tests), PgEO promoted a reduction in nociception in the chemical and thermal models. Additionally, the potential underlying mechanism was investigated using pain pathway blockers, and the results revealed a combined action of opioidergic and muscarinic pathways. The anti-inflammatory potential was confirmed by anti-edematogenic action, reduced cell migration, pro-inflammatory cytokine production, and granuloma formation in chronic processes. This study provides evidence that PgEO can be effective for the treatment of pain and acute and chronic inflammation.


Asunto(s)
Aceites Volátiles , Psidium , Administración Oral , Analgésicos , Animales , Edema/inducido químicamente , Edema/tratamiento farmacológico , Inflamación/tratamiento farmacológico , Ratones , Aceites Volátiles/farmacología , Dolor/tratamiento farmacológico , Extractos Vegetales , Hojas de la Planta/química , Psidium/química
10.
Carbohydr Polym ; 277: 118824, 2022 Feb 01.
Artículo en Inglés | MEDLINE | ID: mdl-34893241

RESUMEN

Polysaccharides are macromolecules with important inherent properties and potential biotechnological applications. These complex carbohydrates exist throughout nature, especially in plants, from which they can be obtained with high yields. Different extraction and purification methods may affect the structure of polysaccharides and, due to the close relationship between structure and function, modify their biological activities. One of the possible applications of these polysaccharides is acting on the skin, which is the largest organ in the human body and can be aged by intrinsic and extrinsic processes. Skincare has been gaining worldwide attention not only to prevent diseases but also to promote rejuvenation in aesthetic treatments. In this review, we discussed the polysaccharides obtained from plants and their innovative potential for skin applications, for example as wound-healing, antimicrobial, antioxidant and anti-inflammatory, antitumoral, and anti-aging compounds.


Asunto(s)
Antibacterianos/farmacología , Antiinflamatorios/farmacología , Antineoplásicos/farmacología , Antioxidantes/farmacología , Neoplasias/tratamiento farmacológico , Polisacáridos/farmacología , Envejecimiento/efectos de los fármacos , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Antineoplásicos/química , Antineoplásicos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Bacterias/efectos de los fármacos , Humanos , Plantas Medicinales/química , Polisacáridos/química , Polisacáridos/aislamiento & purificación , Cuidados de la Piel , Cicatrización de Heridas/efectos de los fármacos
11.
Nat Prod Res ; 36(4): 1038-1042, 2022 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-33207966

RESUMEN

Neglected tropical diseases (NTDs) are a group of pathologies caused by infectious agents or parasites, including the protozoa Leishmania sp. and Trypanosoma cruzi, which cause leishmaniasis and Chagas disease, respectively. The complications of the treatment regimen indicate the urgent need to search for new strategies and therapeutic agents. Among these is the essential oil of Psidium myrsinites DC. The essential oil of the leaves (PMEO) was evaluated in vitro, and cytotoxic activity was analysed against promastigotes of Leishmania braziliensis and Leishmania infantum and epimastigotes of Trypanosoma cruzi, as well as mammalian cells. The results showed that the PMEO had relevant activity against L. braziliensis, low cytotoxicity and a high selectivity index SI = 6.6. These results suggest that PMEO has antiparasitic potential against L. braziliensis, making this species is a possible alternative therapeutic source, given its effectiveness in the in vitro tests performed, opening the possibility of new biological studies in vivo.


Asunto(s)
Antiprotozoarios , Enfermedad de Chagas , Leishmania infantum , Aceites Volátiles , Psidium , Tripanocidas , Trypanosoma cruzi , Animales , Antiprotozoarios/farmacología , Enfermedad de Chagas/tratamiento farmacológico , Aceites Volátiles/farmacología , Aceites Volátiles/uso terapéutico , Tripanocidas/uso terapéutico
12.
J Biomol Struct Dyn ; 40(23): 13001-13016, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-34632943

RESUMEN

Cutaneous Leishmaniasis (CL) is a neglected disease characterized by highest morbidity rates worldwide. The available treatment for CL has several limitations including serious side effects and resistance to the treatment. Herein we aimed to evaluate the activity of essential oil from the peel of Myrciaria floribunda fruits (MfEO) on Leishmania amazonensis. The cytotoxic potential of MfEO on host mammalian cells was evaluated by MTT. The in vitro leishmanicidal effects of MfEO were investigated on the promastigote and intracellular amastigote forms. The ultrastructural changes induced by MfEO were evaluated by Scanning Electron Microscopy (SEM). The molecular docking of the major compounds δ-Cadinene, γ-Cadinene, γ-Muurolene, α-Selinene, α-Muurolene and (E)-Caryophyllene onto the enzymes trypanothione reductase (TreR) and sterol 14-alpha demethylase (C14DM) were performed. Our results showed that MfEO presented moderate cytotoxicity for Vero cells and macrophages. The MfEO inhibited the growth of promastigote and the survival of intracellular amastigotes, in a dose- and time- dependent way. The MfEO presented high selectivity towards amastigote forms, being 44.1 times more toxic for this form than to macrophages. Molecular docking analysis showed that the major compounds of MfEO interact with Leishmania enzymes and that δ-Cadinene (δ-CAD) presented favorable affinity energy values over TreR and C14DM enzymes, when compared with the other major constituents. Molecular dynamics (MD) simulation studies revealed a stable binding of δ-CAD with lowest binding free energy values in MMGBSA assay. Our results suggested that δ-CAD may be a potent inhibitor of TreR and C14DM enzymes. Communicated by Ramaswamy H. Sarma.


Asunto(s)
Antiprotozoarios , Leishmania , Aceites Volátiles , Animales , Chlorocebus aethiops , Simulación del Acoplamiento Molecular , Simulación de Dinámica Molecular , Aceites Volátiles/farmacología , Aceites Volátiles/química , Frutas , Células Vero , Antiprotozoarios/química , Mamíferos
13.
Pestic Biochem Physiol ; 177: 104901, 2021 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-34301362

RESUMEN

Lippia alba is an aromatic shrub known to produce a diversity of essential oils, which can be classified into chemotypes. This study reports on the insecticidal activity of essential oil from L. alba leaves collected at Caatinga and its major compound against termite Nasutitermes corniger and maize weevil Sitophilus zeamais. The chromatographic analysis revealed the presence of 19 compounds, with 1,8-cineole being the most common (70.01%). When ingested, the oil promoted the mortality of N. corniger (LC50: 18.25 and 8.4 nL/g for workers and soldiers, respectively). The compound 1,8-cineole was also termiticidal for workers (LC50: 13.7 nL/g). The oil inhibited the activity of N. corniger exoglucanase, xylanase, and proteases. Toxicity by ingestion to S. zeamais was detected for the oil (LC50: 0.297 µL/g) but not for 1,8-cineole; however, both the oil and 1,8-cineole showed anti-nutritional effects. Fumigant effects of the oil and 1,8-cineole against S. zeamais (LC50 of 78.0 and 13.64 µL/L in air, respectively) were detected. This is the first record of a chemotype VI oil from L. alba collected at Caatinga and the first report of the insecticidal activity of a chemotype VI oil. Our study demonstrates that essential oil from L. alba and 1,8 cineole have the potential for the development of natural insecticides.


Asunto(s)
Insecticidas , Isópteros , Lippia , Aceites Volátiles , Gorgojos , Animales , Eucaliptol , Insecticidas/farmacología , Aceites Volátiles/farmacología , Hojas de la Planta
14.
Nat Prod Res ; 35(22): 4828-4832, 2021 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-32081039

RESUMEN

This work aimed to investigate the chemical composition, antimicrobial activity, synergistic effect, and structure changes of the essential oil of Hymenaea rubriflora (EOHr). Forty-five constituents were identified in the essential oil, corresponding to 94.43% of the compounds present, being the main components E-Caryophyllene (36.72 ± 1.05%), Germacrene D (16.13 ± 0.31%), α-Humulene (6.06 ± 0.16%), ß-elemene (5.61 ± 0.14%) and δ-Cadinene (3.76 ± 0.07%). Antimicrobial activity was evaluated, presenting antibacterial and antifungal activity with MIC ranging from 0.62 to 40 µL/mL. The essential oil had a synergistic effect when combined with gentamicin and fluconazole. Structural changes were also evaluated and it was possible to observe that EOHr action was related to changes in membrane permeability. The findings obtained here suggest that the use of the essential oil of H. rubriflora in the treatment of infectious diseases presents a potential for the future development of pharmaceutical products.


Asunto(s)
Antiinfecciosos , Fabaceae , Hymenaea , Aceites Volátiles , Antibacterianos/farmacología , Antiinfecciosos/farmacología , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/farmacología
15.
Int J Biol Macromol ; 168: 676-685, 2021 Jan 31.
Artículo en Inglés | MEDLINE | ID: mdl-33220373

RESUMEN

Egletes viscosa is a plant with therapeutic value due to its antibacterial, antinociceptive and gastroprotective properties. This study aimed to purify, characterize, and evaluate the cytotoxicity of a lectin (EgviL) from the floral capitula of E. viscosa. The lectin was isolated from saline extract through precipitation with ammonium sulfate followed by Sephadex G-75 chromatography. The molecular mass and isoelectric point (pI) of EgviL were determined as well as its temperature and pH stability. Physical-chemical parameters of interaction between EgviL and carbohydrates were investigated by fluorescence quenching and 1H nuclear magnetic resonance (NMR). Cytotoxicity was investigated against human peripheral blood mononuclear cells (PBMCs) and neoplastic cells. EgviL (28.8 kDa, pI 5.4) showed hemagglutinating activity stable towards heating until 60 °C and at the pH range 5.0-7.0. This lectin is able to interact through hydrophobic and electrostatic bonds with galactose and glucose, respectively. EgviL reduced the viability of PBMCs only at the highest concentration tested (100 µg/mL) while was toxic to Jurkat E6-1 cells with IC50 of 24.1 µg/mL,inducing apoptosis. In summary, EgviL is a galactose/glucose-binding protein with acidic character, stable to heating and with cytotoxic effect on leukemic cells.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Asteraceae/química , Leucocitos Mononucleares/citología , Lectinas de Plantas/farmacología , Antineoplásicos Fitogénicos/química , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Precipitación Química , Estabilidad de Medicamentos , Galactosa/metabolismo , Glucosa/metabolismo , Pruebas de Hemaglutinación , Humanos , Interacciones Hidrofóbicas e Hidrofílicas , Concentración 50 Inhibidora , Punto Isoeléctrico , Células Jurkat , Leucocitos Mononucleares/efectos de los fármacos , Células MCF-7 , Lectinas de Plantas/química
16.
Int J Biol Macromol ; 156: 51-66, 2020 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-32289406

RESUMEN

Carbohydrates are complex biopolymers naturally found in almost all living organisms; their structural variability is gaining much attention in the field of glycobiology. Originally, macromolecular carbohydrates have been developed on huge industrial scales for foodstuffs, oil well drilling, textiles, paper, and electrical insulation. Over the last few decades, however, in addition to these applications, dependent on the physicochemical properties, carbohydrate polymers has presented biological activities. Polysaccharides are now extensively exploited for their remarkable applications in the pharmaceutical industries and biomedicine. An increasing number of oligo- and poly-saccharides now have their monosaccharide composition and structure defined. Many of their biological activities have been related to their chemical structures. Carbohydrates have the capability of binding onto the cell surface of microorganisms to induce the disruption of the cell membrane. They can reduce worm and egg burden, and act as carriers for biopesticides. Carbohydrates affect immune responses, suggesting potential immunomodulatory functions, including the use of adjuvants in vaccines. In addition, they also have therapeutic potential, for example acting as wound healing agents and blocking the high rate of proliferation of malignant cells. This review provides a summary of recent developments in biotechnology and biomedical treatments using well-established and newly described carbohydrates.


Asunto(s)
Carbohidratos/química , Carbohidratos/farmacología , Animales , Antiinfecciosos/química , Antiinfecciosos/farmacología , Antineoplásicos/química , Antineoplásicos/farmacología , Portadores de Fármacos/química , Portadores de Fármacos/uso terapéutico , Humanos , Factores Inmunológicos/química , Factores Inmunológicos/farmacología , Insecticidas/química , Insecticidas/farmacología , Cicatrización de Heridas/efectos de los fármacos
17.
Curr Med Chem ; 27(21): 3519-3533, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-30674245

RESUMEN

The discovery of new biomarkers associated with cancer, neurological and cardiovascular diseases is necessary, since these are common, recurrent diseases considered as leading causes of death in the human population. Molecular signatures of these disorders that can be identified at the outset of their pathogenesis leading to prompt and targeted treatment may increase patient survival. Cancer is a heterogeneous disease that can be expressed differently among individuals; in addition, treatments may have a differentiated approach according to the type of malignant neoplasm. Thus, these neoplastic cells can synthesize and release specific molecules depending on the site where carcinogenesis begins. Moreover, life expectancy is increasing especially in developed countries, however, cases of neurodegenerative diseases have grown in the older members of the population. Commonly, some neurological disorders, which can occur physiologically by the process of senescence, are confused with Alzheimer's Disease (AD). In addition, cardiovascular diseases are the main cause of death in the world; studies capable of identifying, through molecular probes, the beginning of development of an atherosclerotic process can lead to early treatment to avoid an acute myocardial infarction. Accuracy in the detection of these biomarkers can be obtained through biosensors whose design has been increasingly studied to elaborate inexpensive sensory platforms capable of precise detection, even at low concentrations, of the molecule to be measured. The aim of this review is to address biomarkers to be used in diagnoses instead of invasive exams; biosensors for the specific and sensitive detection of these biological markers are also investigated.


Asunto(s)
Técnicas Biosensibles , Enfermedad de Alzheimer , Biomarcadores , Enfermedades Cardiovasculares , Humanos
18.
Clin Chim Acta ; 498: 52-61, 2019 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-31400314

RESUMEN

Although prostate cancer is notable for its high incidence and mortality in men worldwide, its identification remains a challenge. Biomarkers have been useful tools for the specific detection of prostate cancer. Unfortunately, benign prostate diseases cause similar alterations in screening assays thus reducing the potential for early and specific diagnosis. Changes in glycan and glycoprotein expression have often been associated with the onset and progression of cancer. Abnormal glycans and glycoproteins have been reported as new biomarkers of prostate metabolism that can distinguish benign prostate disease and cancer in non-aggressive and aggressive stages. Carbohydrate-binding proteins known as lectins have been valuable tools to detect these changes, investigate potential biomarkers and improve our understanding aberrant glycosylation in cancer. Here we review progress in elucidating prostate disease and discuss the roles of glycans in the differential detection of benign and cancerous prostate disease. We also summarize the lectin-based tools for detecting glycosylation changes.


Asunto(s)
Glicosilación , Enfermedades de la Próstata/metabolismo , Animales , Biomarcadores/análisis , Diagnóstico Diferencial , Humanos , Lectinas/análisis , Masculino , Polisacáridos/análisis , Neoplasias de la Próstata/diagnóstico
19.
Int J Biol Macromol ; 140: 234-244, 2019 Nov 01.
Artículo en Inglés | MEDLINE | ID: mdl-31400430

RESUMEN

Carbohydrate-binding proteins, also known as lectins, are valuable tools for biotechnology, including pharmacological uses. Mannose lectins obtained from plant and animal sources are applied to protection and characterization of autoimmune diseases as well as defense proteins against pathogens. The presence of mannose-binding lectins in plants that also recognize glucose could be entitled Man/Glc lectins; such specificity has allowed employing these vegetal lectins for several applications. Animal mannose-binding lectins are synthesized in the liver and secreted into the blood stream where both concentration and activity are greatly affected due to gene polymorphisms; these serum proteins play important roles in the immune system by recognizing mannose-like carbohydrate ligands found exclusively on pathogenic microorganisms. Mannose lectins already showed strong binding to relevant bacteria, viruses, protozoa and helminth species, initiating potent host defense mechanisms by inducing growth inhibition or death of such organisms; the ability to prevent the formation or destruction of microbial biofilms has also been reported. Mannose-binding lectins have attracted considerable attention against carcinogenesis and atherogenesis. The aim of this review article is to approach biotechnology characteristics of these lectins from different sources and microorganism/cell surface interactions with mannose; in addition, aspects of mechanisms associated to lectin antipathogenic activities are described.


Asunto(s)
Antiinfecciosos/farmacología , Antineoplásicos Fitogénicos/farmacología , Lectinas/farmacología , Lectinas de Unión a Manosa/farmacología , Plantas/química , Animales , Antiinfecciosos/química , Antineoplásicos Fitogénicos/química , Sitios de Unión , Biotecnología , Proliferación Celular/efectos de los fármacos , Glicosilación , Lectinas/química , Manosa/química , Manosa/metabolismo , Lectinas de Unión a Manosa/química , Modelos Moleculares , Lectinas de Plantas/farmacología , Unión Proteica
20.
Biochimie ; 166: 173-183, 2019 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-30981871

RESUMEN

Formation of new blood vessels from preexisting ones, a process known as angiogenesis, is one of the limiting steps for success in treatment of ischemic disorders. Therefore, efforts to understanding and characterize new agents capable to stimulate neovascularization are a worldwide need. Crataeva tapia bark lectin (CrataBL) has been shown to have chemoattractant properties for endothelial cells through the stimulation of migration and invasiveness of human umbilical vein endothelial cells (HUVEC) because it is a positively charged protein with high affinity to glycosaminoglycan. In addition, CrataBL increased the production of chondroitin and heparan sulfate in endothelial cells. These findings orchestrated specific adhesion on collagen I and phosphorylation of tyrosine kinase receptors, represented by vascular endothelial growth factor receptor-2 (VEGFR-2) and fibroblast growth factor receptor (FGFR), whose downstream pathways trigger the angiogenic cascade increasing cell viability, cytoskeleton rearrangement, cell motility, and tube formation. Moreover, CrataBL inhibited the activity of matrix metalloproteases type 2 (MMP-2), a protein related to tissue remodeling. Likewise, CrataBL improved wound healing and increased the number of follicular structures in lesioned areas produced in the dorsum-cervical region of C57BL/6 mice. These outcomes altogether indicate that CrataBL is a pro-angiogenic and healing agent.


Asunto(s)
Inductores de la Angiogénesis/farmacología , Condroitín/metabolismo , Heparitina Sulfato/metabolismo , Neovascularización Fisiológica/efectos de los fármacos , Lectinas de Plantas/farmacología , Animales , Capparaceae/metabolismo , Movimiento Celular/efectos de los fármacos , Factores Quimiotácticos/farmacología , Células Endoteliales de la Vena Umbilical Humana , Humanos , Masculino , Ratones , Ratones Endogámicos C57BL , Cicatrización de Heridas/efectos de los fármacos
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