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1.
Vitae (Medellín) ; 31(1): 1-7, 2024-05-03. Ilustraciones
Article in English | LILACS, COLNAL | ID: biblio-1538070

ABSTRACT

Background: Moringa peregrina is widely used in the traditional medicine of the Arabian Peninsula to treat various ailments, because it has many pharmacologically active components with several therapeutic effects. Objective: This study aimed to investigate the inhibitory effect of Moringaperegrina seed ethanolic extract (MPSE) against key enzymes involved in human pathologies, such as angiogenesis (thymidine phosphorylase), diabetes (α-glucosidase), and idiopathic intracranial hypertension (carbonic anhydrase). In addition, the anticancer properties were tested against the SH-SY5Y (human neuroblastoma). Results: MPSE extract significantly inhibited α-glucosidase, thymidine phosphorylase, and carbonic anhydrase with half-maximal inhibitory concentrations (IC50) values of 303.1 ± 1.3, 471.30 ± 0.3, and 271.30 ± 5.1 µg/mL, respectively. Furthermore, the antiproliferative effect of the MPSE was observed on the SH-SY5Y cancer cell line with IC50 values of 55.1 µg/mL. Conclusions: MPSE has interesting inhibitory capacities against key enzymes and human neuroblastoma cancer cell line.


Antecedentes: La Moringa peregrina se utiliza ampliamente en la medicina tradicional de la Península Arábiga para tratar diversas dolencias, ya que posee numerosos componentes farmacológicamente activos con varios efectos terapéuticos. Objetivo: Este estudio tenía como objetivo investigar el efecto inhibidor del extracto etanólico de semillas de Moringaperegrina (MPSE) frente a enzimas clave implicadas en patologías humanas, como la angiogénesis (timidina fosforilasa), la diabetes (α-glucosidasa) y la hipertensión intracraneal idiopática (anhidrasa carbónica). Además, se comprobaron las propiedades anticancerígenas frente al SH-SY5Y (neuroblastoma humano). Resultados: El extracto de MPSE inhibió significativamente la α-glucosidasa, la timidina fosforilasa y la anhidrasa carbónica con concentraciones inhibitorias semimáximas (IC50) de 303,1 ± 1,3, 471,30 ± 0,3 y 271,30 ± 5,1 µg/mL, respectivamente. Además, se observó el efecto antiproliferativo del MPSE en la línea celular del cáncer SH-SY5Y con valores de IC50 de 55,1 µg/mL. Conclusiones: MPSE posee interesantes capacidades inhibitorias frente a enzimas clave y línea celular de neuroblastoma canceroso humano.


Subject(s)
Humans , Anticarcinogenic Agents , Moringa , Enzyme Inhibitors , alpha-Glucosidases
2.
Bol. latinoam. Caribe plantas med. aromát ; 23(2): 214-228, mar. 2024. tab, graf
Article in Spanish | LILACS | ID: biblio-1552134

ABSTRACT

Cancer cells modify lipid metabolism to proliferate, Passiflora edulis ( P. edulis ) fruit juice (ZuFru) has antitumor activity, but whether a mechanism is through modulation of cell lipids is unknown. T o establish if ZuFru modifies cholesterol and triglycerides in SW480 and SW620. ZuFru composition was studied by phytochemical march; antiproliferative activity by sulforhodamine B, cholesterol , and triglycerides by Folch method. Z ufru contains anthocyanins, flavonoids, alkaloids , and tannins. Cell lines showed differences in their growth rate ( p =0.049). At 39.6 µg/m L of ZuFru, cell viability was decreased: SW480 (45.6%) and SW620 (45.1%). In SW480, cholesterol (44.6%) and triglycerides (46.5%) decreased; In SW620, cholesterol decreased 14.8% and triglycerides increased 7%, with significant differences for both lines. A ntiproliferative activity of ZuFru could be associated with the inhibition of intracellular biosynthesis of cholesterol and triglycerides in SW480. Action mechanisms need to be further investigated.


Las células cancerosas modifican el metabolismo lipídico para proliferar; el zumo de fruta (ZuFru) de Passiflora edulis ( P. edulis ) tiene activida d antitumoral, sin embargo, se desconoce si se involucran los lípidos celulares. E stablecer si ZuFru modifica colesterol y triglicéridos en células SW480 y SW620. C omposición del ZuFru, actividad antiproliferativa, colesterol y triglicéridos. Se encontraro n antocianinas, flavonoides, alcaloides y taninos. Las líneas celulares mostraron diferencias en su tasa de crecimiento ( p =0 . 049); ZuFru 39,6 µg/ml se disminuyó la viabilidad celular; SW480 (45,6%) y SW620 (45,1%); en SW480 colesterol (44,6%) y triglicérid os (46,5%) en SW620, colesterol (14,8%) y los triglicéridos aumentaron 7%, con diferencias significativas para ambas líneas. La actividad antiproliferativa del ZuFru podría estar asociada a la inhibición de la biosíntesis intracelular de colesterol y de tr iglicéridos en SW480, pero no en SW620. Estos mecanismos de acción deben ser fuertemente investigados.


Subject(s)
Anticarcinogenic Agents , Passiflora , Passifloraceae/metabolism , Triglycerides/physiology , Plant Extracts/pharmacology , Cholesterol/physiology , Fruit
3.
Braz. j. biol ; 83: 1-10, 2023. ilus, graf, tab
Article in English | LILACS, VETINDEX | ID: biblio-1468841

ABSTRACT

The objective of the present study was to analyse the bioactive compounds of the leaves of Conocarpus lancifolius (C. lancifolius). The GC-MS analysis of the hot methanolic extract of the leaves (HMEL) of C. lancifolius exhibited the bioactive compounds such as 1-(3-Methoxy-2-nitrobenzyl) iso quinoline, morphin-4-ol-6,7-dione, 1-bromo N-methyl-, phytol, hexadecanoic acid, 2,3-dihydroxypropyl ester, 2,2’:4’,2”-terthiophene, ethyl iso-allocholate, caryophyllene oxide, campesterol, epiglobulol, cholestan-3-ol, 2-methylene-, (3á,5à)-, dasycarpidan-1-methanol, acetate (ester) and oleic acid, eicosyl ester. The FT-IR analysis of HMEL of C. lancifolius showed a unique peak at 3184, 2413, 1657 cm-¹ representing coumaric acid, chlorogenic acid and ferulic acid. The HMEL of C. lancifolius was actively inhibiting the proliferation of breast cancer cells MCF-7 ATCC at the concentration of 72.66 ± 8.21 µg/ml as IC50 value. The HMEL of C. lancifolius also revealed a good spectrum of activity against Gram-positive and Gram negative bacterial cultures screened in this work. The activity observed has shown more or less similar effects against screened bacteria. However, the magnitude of potentiality was significantly lesser compared to standard ciprofloxacin disc at p< 0.001 level (99% confidence intervals). Furthermore, the study demonstrating the bioactive compounds can be isolated from the leaves of C. lancifolius.


O objetivo do presente estudo foi analisar os compostos bioativos das folhas de Conocarpus lancifolius (C. lancifolius). A análise por GC-MS do extrato metanólico quente das folhas (HMEL) de C. lancifolius exibiu os compostos bioativos como 1- (3-Metoxi-2-nitrobenzil) isoquinolina, morfina-4-ol-6,7- diona, 1-bromo-N-metil-, fitol, ácido hexadecanoico, 2,3-di-hidroxipropil éster, 2,2 ‘: 4’, 2 ” - tertiofeno, isoalocolato de etil, óxido de cariofileno, campesterol, epiglobulol, colestano -3-ol, 2-metileno-, (3á, 5à) -, dasycarpidan-1-metanol, acetato (éster) e ácido oleico, éster eicosílico. A análise FT-IR de HMEL de C. lancifolius mostrou um pico único em 3184, 2413, 1657 cm-¹ representando ácido cumarico, ácido clorogênico e ácido ferúlico. O HMEL de C. lancifolius inibiu ativamente a proliferação de células de câncer de mama MCF-7 ATCC na concentração de 72,66 ± 8,21 µg/ml como valor de IC50. O HMEL de C. lancifolius também revelou bom espectro de atividade contra culturas de bactérias Gram-positivas e Gram-negativas rastreadas neste trabalho. A atividade observada mostrou efeitos mais ou menos semelhantes contra bactérias rastreadas. No entanto, a magnitude da potencialidade foi significativamente menor em comparação com o disco de ciprofloxacina padrão em nível de p < 0,001 (intervalos de confiança de 99%). Além disso, o estudo demonstrando os compostos bioativos pode ser isolado das folhas de C. lancifolius.


Subject(s)
Anti-Bacterial Agents/analysis , Anticarcinogenic Agents/analysis , Combretaceae/cytology , Combretaceae/chemistry , Combretaceae/toxicity , Drug Resistance, Multiple
4.
Semina cienc. biol. saude ; 43(2): 295-304, jul./dez. 2022. ilus
Article in Portuguese | LILACS | ID: biblio-1426506

ABSTRACT

O papel dos produtos naturais, em especial os nutracêuticos, vem ganhando destaque nos últimos anos devido aos efeitos positivos em parâmetros relacionados à saúde. O açafrão é uma espécie originária do sudeste da Ásia e considerado uma preciosa especiaria. Além da principal utilização como condimento, possui substâncias com atividades antioxidante, antimicrobiana e corante, que lhe conferem possibilidade de emprego nas áreas de cosméticos, têxtil e alimentícia, sendo também muito utilizado nas medicinas tradicionais chinesa e indiana. Seu principal composto fenólico, a curcumina, tem sido amplamente estudado, por apresentar uma variedade de propriedades para a saúde, como efeitos antioxidantes, anti-inflamatórios, antivirais, antibacterianos, antidepressivos e anticancerígenos e, assim, potencial de ação contra várias doenças crônicas. Portanto, o objetivo do presente estudo foi revisar os efeitos do açafrão nos parâmetros biológicos e comportamentais, bem como sua utilização na manutenção da saúde e qualidade de vida dos indivíduos.


The role of natural products, especially nutraceuticals, has been gaining prominence in recent years due to their positive effects on health-related parameters. Turmeric is a species native to Southeast Asia and considered a precious spice. In addition to its main use as a condiment, it has substances with antioxidant, antimicrobial, and coloring activity, which give it the possibility of being used in the areas of cosmetics, textiles, and food; It is also widely used in traditional Chinese and Indian medicine. Its main phenolic compound, curcumin, has been widely studied, as it has a variety of health properties, such as antioxidant, anti-inflammatory, antiviral, antibacterial, antidepressant and anticancer effects and, thus, potential for action against various chronic diseases. Therefore, the objective of the present study was to review the effects of saffron on biological and behavioral parameters, as well as its use in maintaining the health and quality of life of individuals.


Subject(s)
Humans , Antiviral Agents , Health , Anticarcinogenic Agents , Anti-Inflammatory Agents , Anti-Bacterial Agents , Antidepressive Agents , Antioxidants
5.
J. oral res. (Impresa) ; 11(4): 1-13, jul. 21, 2022. tab
Article in English | LILACS | ID: biblio-1427176

ABSTRACT

Introduction: DMBA is a chemical carcinogen that induces carcinomas within a few weeks of its application. We developed an experimental model of carcinogenesis induced by DMBA dissolved in 0,5% paraffin oil (DMBA-PO), verifying the inhibitory effect of the carcinogenicity of phenyl isothiocyanate (PhITC), phenethyl (PhnITC) and benzyl isothiocyanate (BITC). Material and Methods: For this, 88 hamsters were distributed into three groups: one exposed to DMBA-PO (Group 1, n=12), three subgroups (n=12) exposed to PhITC, PhnITC, BITC and DMBA-PO (Group 2, n=36) and four control subgroups (n=10) that were not exposed to the carcinogen in which PO (paraffin oil) and isothiocyanates were applied (Group 3, n=40). Results: The experiment had a duration of 20 weeks, at the end of which the inhibitory effect was established by comparing the lesions developed in the groups that received isothiocyanates with the group that was only treated with DMBA-PO. The carcinogenic effect of DMBA-PO is 100% (35 carcinomas) and the inhibitory effect was 0, whereas in the presence of isothiocyanates the carcinogenic effect decreases, with an inhibitory effect of 86% for BITC (5 carcinomas) and 74% for PhITC (9 carcinomas). Conclusion: The inhibitory effect for PhnITC is 80% in relation to invasive OSCC (1 carcinoma).


Introducción: El DMBA es un carcinógeno químico que induce carcinomas a las pocas semanas de su aplicación. Desarrollamos un modelo experimental de carcinogénesis inducida por DMBA disuelto en aceite de parafina al 0,5% (DMBA-Ap) comprobando el efecto inhibidor de la carcinogénesis de los isotiocianatos fenil (PhITC), fenetil (PhnITC) y bencil isotiocianato (BITC). Material y Métodos: Para ello, se distribuyeron 88 hámsteres en 3 grupos: uno expuesto al DMBA-Ap (Grupo 1, n=12), tres subgrupos (n=12) expuestos a PhITC, PhnITC, BITC y DMBA-Ap (Grupo 2, n=36) y cuatro subgrupos controles (n=10), no expuestos al carcinógeno en el que se aplicaron Ap e isotiocianatos (Grupo 3, n=40). Resultados:El experimento tuvo una duración de 20 semanas, al final de la cual se establece de forma comparativa el efecto inhibidor comparando las lesiones desarrolladas en los grupos que recibieron isotiocianatos con respecto al grupo tratado sólo con DMBA-Ap. El efecto carcinógeno del DMBA-Ap es del 100% (35 carcinomas) y el efecto inhibidor 0, mientras que en presencia de isotiocianatos el efecto carcinógeno disminuye, con un efecto inhibidor del 86% para BITC (5 carcinomas) y del 74% para el PhITC (9 carcinomas). Conclusión:El efecto inhibidor del PhnITC es del 80% en relación con el COCE invasivo (1 carcinoma).


Subject(s)
Animals , Male , Anticarcinogenic Agents/therapeutic use , 9,10-Dimethyl-1,2-benzanthracene/toxicity , Carcinogens , Isothiocyanates , Models, Animal , Carcinogenesis , Squamous Cell Carcinoma of Head and Neck
6.
Biosci. j. (Online) ; 38: e38097, Jan.-Dec. 2022. ilus, graf
Article in English | LILACS | ID: biblio-1415851

ABSTRACT

Garcinia humilis, known commonly as achachairú or bacupari, has great medicinal value. Their fruits have pharmacological, antibacterial, antioxidant, and anticancer properties. Therefore, the objective of the present study was to evaluate the cytotoxicity and genotoxicity of G. humilis crude extract in breast tumor cells. Cytotoxicity was determined using the Resazurin reduction assay and genotoxicity by the single cell gel electrophoresis assay (Comet assay) on human MCF-7 cells. Crude extract of G. humilis was cytotoxic only when used at high concentrations (IC50 = 5.084 mg mL-1). The Comet assay showed that the crude extract did not induce genotoxicity at 1 and 5 mg mL-1 but did show signs of DNA fragmentation and DNA fragmentation at 10 mg mL-1. The cytotoxic activity against breast adenocarcinoma cells at high concentrations suggests that this medicinal plant could be used with caution and must be further studied to understand better its therapeutic and toxicological potential in the human body.


Subject(s)
Anticarcinogenic Agents , Garcinia , Antioxidants
7.
Bol. latinoam. Caribe plantas med. aromát ; 21(1): 1-40, ene. 2022. ilus, tab
Article in English | LILACS | ID: biblio-1370311

ABSTRACT

Cancer is an abnormal and uncontrolled growth of cells that spreads through cell division. There are different types of medicines available to treat cancers, but no drug is found to be fully effective and safe for humans. The major problem involved in the cancer treatments is the toxicity of the established drug and their side effects. Medicinal plants are used as folk medicines in Asian and African populations for thousands of years. 60% of the drugs for treating cancer are derived from plants. More than 3000 plants have anticancer activity. The present review aims at the study of a broad spectrum survey of plants having anticancer components for different type of cancers. This article consists of 364 medicinal plants and their different parts as potential Source of Anticancer Agents.


El cáncer es un crecimiento anormal y descontrolado de células que se disemina a través de la división celular. Hay diferentes tipos de medicamentos disponibles para tratar el cáncer, pero no se ha encontrado ningún medicamento que sea completamente efectivo y seguro para los seres humanos. El principal problema involucrado en los tratamientos del cáncer es la toxicidad del fármaco establecido y sus efectos secundarios. Las plantas medicinales se utilizan como medicinas populares en poblaciones asiáticas y africanas durante miles de años. El 60% de los medicamentos para el tratamiento del cáncer se derivan de plantas. Más de 3000 plantas tienen actividad anticancerígena. La presente revisión tiene como objetivo el estudio de un estudio de amplio espectro de plantas que tienen componentes anticancerígenos para diferentes tipos de cánceres. Este artículo consta de 364 plantas medicinales y sus diferentes partes como fuente potencial de agentes anticancerígenos.


Subject(s)
Plants, Medicinal/chemistry , Anticarcinogenic Agents/pharmacology , Phytochemicals/analysis , Cell Line, Tumor/drug effects , Phytochemicals/pharmacology
8.
Bol. latinoam. Caribe plantas med. aromát ; 21(1): 66-80, ene. 2022. ilus, tab
Article in English | LILACS | ID: biblio-1372378

ABSTRACT

Melastoma malabathricum (M. malabathricum) extracts have been reported to exert various pharmacological activities including antioxidants, anti-inflammatory and antiproliferative activities. The objective of the present study was to determine the anticarcinogenic activity of its methanol extract (MEMM) against the azoxymethane (AOM)-induced early colon carcinogenesis in rats. Rats were randomly assigned to five groups (n=6) namely normal control, negative control, and treatment (50, 250 or 500 mg/kg of MEMM) groups. Colon tissues were harvested for histopathological analysis and endogenous antioxidant system determination. MEMM was also subjected to HPLC analysis. Findings showed that MEMM significantly (p<0.05) reversed the AOM-induced carcinogenicity by: i) reducing the formation of aberrant crypt foci (ACF) in colon tissues, and; ii) enhancing the endogenous antioxidant activity (catalase, superoxide dismutase and glutathione peroxidase). Moreover, various phenolics has been identified in MEMM. In conclusion, MEMM exerts the in vivo anticarcinogenic activity via the activation of endogenous antioxidant system and synergistic action of phenolics.


Se ha informado que los extractos de Melastoma malabathricum (M. malabathricum) ejercen diversas actividades farmacológicas, incluidas actividades antioxidantes, antiinflamatorias y antiproliferativas. El objetivo del presente estudio fue determinar la actividad anticancerígena de su extracto de metanol (MEMM) contra la carcinogénesis de colon temprana inducida por azoximetano (AOM) en ratas. Las ratas se asignaron al azar a cinco grupos (n=6), a saber, los grupos de control normal, control negativo y tratamiento (50, 250 o 500 mg/kg de MEMM). Tejidos de colon fueron recolectados para análisis histopatológico y determinación del sistema antioxidante endógeno. MEMM también se sometió a análisis de HPLC. Los hallazgos mostraron que MEMM invirtió significativamente (p<0.05) la carcinogenicidad inducida por AOM al: i) reducir la formación de focos de criptas aberrantes (ACF) en los tejidos del colon, y; ii) potenciar la actividad antioxidante endógena (catalasa, superóxido dismutasa y glutatión peroxidasa). Además, se han identificado varios fenólicos en MEMM. En conclusión, MEMM ejerce la actividad anticancerígena in vivo mediante la activación del sistema antioxidante endógeno y la acción sinérgica de los fenólicos.


Subject(s)
Animals , Rats , Plant Extracts/administration & dosage , Anticarcinogenic Agents/administration & dosage , Colonic Neoplasms/drug therapy , Melastomataceae/chemistry , Organ Size/drug effects , Body Weight/drug effects , Chromatography, High Pressure Liquid , Rats, Sprague-Dawley , Colon/pathology , Plant Leaves , Methanol , Phenolic Compounds , Aberrant Crypt Foci , Carcinogenesis/drug effects , Antioxidants
9.
Braz. j. biol ; 82: 1-9, 2022. ilus, graf, tab
Article in English | LILACS, VETINDEX | ID: biblio-1468507

ABSTRACT

L-Asparaginase catalysing the breakdown of L-Asparagine to L-Aspartate and ammonia is an enzyme of therapeutic importance in the treatment of cancer, especially the lymphomas and leukaemia. The present study describes the recombinant production, properties and anticancer potential of enzyme from a hyperthermophilic archaeon Pyrococcus abyssi. There are two genes coding for asparaginase in the genome of this organism. A 918 bp gene encoding 305 amino acids was PCR amplified and cloned in BL21 (DE3) strain of E. coli using pET28a (+) plasmid. The production of recombinant enzyme was induced under 0.5mM IPTG, purified by selective heat denaturation and ion exchange chromatography. Purified enzyme was analyzed for kinetics, in silico structure and anticancer properties. The recombinant enzyme has shown a molecular weight of 33 kDa, specific activity of 1175 U/mg, KM value 2.05mM, optimum temperature and pH 80°C and 8 respectively. No detectable enzyme activity found when L-Glutamine was used as the substrate. In silico studies have shown that the enzyme exists as a homodimer having Arg11, Ala87, Thr110, His112, Gln142, Leu172, and Lys232 being the putative active site residues. The free energy change calculated by molecular docking studies of enzyme and substrate was found as ∆G – 4.5 kJ/mole indicating the affinity of enzyme with the substrate. IC50 values of 5U/mL to 7.5U/mL were determined for FB, caco2 cells and HepG2 cells. A calculated amount of enzyme (5U/mL) exhibited 78% to 55% growth inhibition of caco2 and HepG2 cells. In conclusion, the recombinant enzyme produced and characterized in the present study offers a good candidate for the treatment of cancer. The procedures adopted in the present study can be prolonged for in vivo studies.


A L-asparaginase, que catalisa a degradação da L-asparagina em L-aspartato e amônia, é uma enzima de importância terapêutica no tratamento do câncer, especialmente dos linfomas e da leucemia. O presente estudo descreve a produção recombinante, propriedades e potencial anticancerígeno da enzima de Pyrococcus abyssi, um archaeon hipertermofílico. Existem dois genes que codificam para a asparaginase no genoma desse organismo. Um gene de 918 bp, que codifica 305 aminoácidos, foi amplificado por PCR e clonado na cepa BL21 (DE3) de E. coli usando o plasmídeo pET28a (+). A produção da enzima recombinante foi induzida sob 0,5mM de IPTG, purificada por desnaturação seletiva por calor e cromatografia de troca iônica. A enzima purificada foi analisada quanto à cinética, estrutura in silico e propriedades anticancerígenas. A enzima recombinante apresentou peso molecular de 33 kDa, atividade específica de 1.175 U / mg, valor de KM 2,05 mM, temperatura ótima de 80º C e pH 8. Nenhuma atividade enzimática detectável foi encontrada quando a L-glutamina foi usada como substrato. Estudos in silico mostraram que a enzima existe como um homodímero, com Arg11, Ala87, Thr110, His112, Gln142, Leu172 e Lys232 sendo os resíduos do local ativo putativo. A mudança de energia livre calculada por estudos de docking molecular da enzima e do substrato foi encontrada como ∆G – 4,5 kJ / mol, indicando a afinidade da enzima com o substrato. Valores de IC50 de 5U / mL a 7,5U / mL foram determinados para células FB, células caco2 e células HepG2. Uma quantidade de enzima (5U / mL) apresentou inibição de crescimento de 78% a 55% das células caco2 e HepG2, respectivamente. Em conclusão, a enzima recombinante produzida e caracterizada no presente estudo é uma boa possibilidade para o tratamento do câncer. Os procedimentos adotados na presente pesquisa podem ser aplicados para estudos in vivo.


Subject(s)
Anticarcinogenic Agents/analysis , Asparaginase/genetics , Leukemia/drug therapy , Lymphoma/drug therapy , Pyrococcus abyssi/enzymology
10.
Braz. J. Pharm. Sci. (Online) ; 58: e20954, 2022. tab, graf
Article in English | LILACS | ID: biblio-1420502

ABSTRACT

Abstract Cisplatin is the primary anti-cancer agent for the treatment of most solid tumors. However, platinum-based anti-cancer chemotherapy produces severe side effects due to its poor specificity. There are a broad interest and literature base for a novel mechanism of action on platinum derivatives. Additionally, combining cisplatin with histone deacetylase inhibitors (HDACi) such as 4-hydroxybenzoic acid derivatives showed promising results in treating solid tumors. Here we aimed to conjugate 4-hydroxybenzoic acid with platinum to obtain a novel platinum derivative that can overcome cisplatin resistance. Cis-4-hydroxyphenylplatinum(II)diamine compound was synthesized under mild conditions and characterized. Cytotoxicity assay was performed on SKOV3-Luc and A549-Luc cells. Hemocompatibility and serum protein binding analysis were performed. Treatment potential was evaluated in xenograft tumor models. Biodistribution was tested on tumor-bearing mice via Pt analysis in organs with ICP-MS, ex vivo. In this study, cis-4-hydroxyphenylplatinum (II) diamine was synthesized with a yield of 62%. The MTT assay on A549-Luc and SKOV3-Luc cell lines resulted in IC50 values of 17.82 and 7.81 µM, respectively. While tumor growth was continued in the control group, the tumor volume decreased in the treatment group. All results point to the conclusion that the new compound has the potential to treat solid tumors


Subject(s)
Platinum/pharmacology , Anticarcinogenic Agents/classification , Histone Deacetylase Inhibitors/adverse effects , Lung Neoplasms/pathology
11.
Braz. J. Pharm. Sci. (Online) ; 57: e18954, 2021. tab, graf
Article in English | LILACS | ID: biblio-1345456

ABSTRACT

The ethanolic extract of resinous sediment (EERS) of Etlingera elatior young inflorescence was examined for its anticancer effect and potential antioxidant activity. The anticancer effect of the EERS was evaluated on four human cancer cell lines, HCT 116, HT-29, Hela, and MCF-7, using the MTT assay. GC-MS analysis showed that the main components found in the EERS were nonyl cyclopropane (4.44%), 1-tetradecane (3.66%), cyclotetradecane (2.41%), cyclododecane (1.92%), and 1-decene (1.72%). The antioxidant activity was determined through different methods. High amounts of TPC and TFC in the EERS were found. Moderate antioxidant capacity of the EERS was detected by DPPH and ABTS assays, with EC50 values of 44.19 and 56.61 µg/mL and a high FRAP value of 281.79 nmol Fe+2 equivalent/mg extract. In the MTT assay, the EERS showed potent anticancer activity, with IC50 values of 19.82, 37.001, 50.49, and 53.29 µg/mL against HT-29, HCT 116, Hela, and MCF-7 tumour cell lines, respectively. Moreover, the results were comparable to or less potent than the standard reference drug, 5-fluorouracil. The results showed that the EERS of Etlingera elatior inflorescence contained a high amount of polyphenols and flavonoids, which may to the selective antiproliferative effects towards colon cancer in vitro


Subject(s)
Zingiberaceae/classification , Inflorescence/anatomy & histology , Fluorouracil/pharmacology , Neoplasms , Antioxidants/analysis , In Vitro Techniques/methods , Pharmaceutical Preparations , Anticarcinogenic Agents/adverse effects , Colonic Neoplasms/pathology
12.
Braz. arch. biol. technol ; 63: e20180735, 2020. tab, graf
Article in English | LILACS | ID: biblio-1132190

ABSTRACT

Abstract Thevetia peruviana is an ornamental shrub grown-up in many tropical region of the world. This plant produces secondary metabolites with biological properties of interest for the pharmaceutical industry. The objective was to determine the secondary metabolites profile of callus and cell suspension cultures of T. peruviana and compare them with those from explant (fruit pulp). Extracts in 50% aqueous ethanol and ethyl acetate were prepared. The phytochemical analysis was performed using standard chemical tests and thin layer chromatography. In addition, total phenolic and flavonoids compounds (TPC and TFC), total cardiac glycosides (TCG) and total antioxidant activity (TAA) was determined during the cell suspension growth. Phenolic chemical profile was also analyzed by high performance liquid chromatography (HPLC). Common metabolites (alkaloids, amino acids, antioxidants, cardiac glycosides, leucoanthocyanidins, flavonoids, phenols, sugars and triterpenes) were detected in all samples. The maximum production of extracellular TCG, TPC, TFC and TAA in cells suspensions were at 6-12 days; in contrast, intracellular content was relatively constant during the exponential grown phase (0 to 12-days). HPLC analysis detected one compound with retention time at 11.6 min; this compound was tentatively identified as dihydroquercetin, a flavonoid with anti-cancer properties. These results provide evidence on the utility of the in vitro cell cultures of T. peruviana for valuable pharmaceutical compounds production.


Subject(s)
Cells, Cultured , Thevetia/cytology , Phytochemicals/biosynthesis , Triterpenes , Flavonoids , Chromatography, High Pressure Liquid , Anticarcinogenic Agents , Thevetia/chemistry , Culture Techniques , Phytochemicals/analysis , Antioxidants
13.
Hig. aliment ; 33(288/289): 460-464, abr.-maio 2019. ilus
Article in Portuguese | LILACS, VETINDEX | ID: biblio-1481976

ABSTRACT

Na última década, a ciência contribuiu significativamente para inúmeros avanços em relação ao tratamento e prevenção do câncer colorretal (CCR), porém, a prevalência global e a taxa de mortalidade permanecem elevadas. Há relatos sobre efeitos benéficos de espécies de Bifidobacterium e Lactobacillus com potencial probiótico na prevenção de CCR. No entanto, a bactéria probiótica Lactococcus lactis subps. lactis é comumente utilizada para fins industriais, não havendo comprovações in vivo sobre seu potencial anticarcinogênico. Visto o interesse emergente dos efeitos benéficos dos probióticos a fim de prevenir ou tratar o CCR, o presente estudo objetivou explorar os efeitos de L. lactis subsp. lactis sobre o CCR. Ratos Wistar receberam doses subcutâneas de 1,2 dimetilhidrazina (DMH) e suspensão de L. lactis subsp. lactis por via oral. Após 20 semanas, os tecidos intestinais foram analisados e de acordo com o resultado, o isolado demonstrou potencial anticarcinogênico contra CCR.


Subject(s)
Animals , Rats , Lactococcus lactis/isolation & purification , Colorectal Neoplasms/therapy , Probiotics/therapeutic use , Anticarcinogenic Agents , Rats, Wistar
14.
Bol. latinoam. Caribe plantas med. aromát ; 18(1): 81-94, ene. 2019. tab, ilus, graf, mapas
Article in Spanish | LILACS | ID: biblio-1007491

ABSTRACT

Between 2016 and 2017, we conducted structured interviews with herbalists in market stands in the providence of Trujillo, La Libertad, Peru in order to create a catalog of plants with anticarcinogenic properties. Herbalists shared information about species they use in cancer treatment, including common names, part of the plant used, methods of preparation, plant state, and frequency and method of administration as medicine. We combined this information with the Shannon-Wiener diversity and evenness index to complete a quantitative analysis of the anticarcinogenic species. Our results demonstrate that 46 different species representing 24 genera and 19 families are locally used in cancer treatment, with a Shannon-Wiener index of 3.6 and 0.9 respectively. Our catalog thus represents a great variety of species and source of potentially useful knowledge for fighting cancer.


Con el objetivo de registrar las plantas con propiedades anticancerígenas distribuidas en la provincia de Trujillo, La Libertad, durante el 2016 y 2017, realizamos entrevistas estructuradas a hierbateros con puesto de venta en los mercados de abastos, quienes brindaron información sobre las especies usadas para el tratamiento del cáncer, detallando nombres vulgares, parte del vegetal utilizado, formas de preparación, estado de la plantas, frecuencia y forma de administración; así mismo aplicando los índices de diversidad Shannon- Wiener y Equidad se hizo el análisis cuantitativo de los datos encontrados. Se evidenció que para el tratamiento del cáncer se usan 46 especies, representadas 24 géneros y 19 familias; valor que refleja un Índice de Diversidad y de Equidad de 3.6 y 0.9 respectivamente, indicando que existe una gran variedad de especies y un conocimiento potencialmente valioso para combatir esta enfermedad.


Subject(s)
Humans , Male , Female , Adult , Middle Aged , Aged , Plants, Medicinal , Anticarcinogenic Agents/therapeutic use , Neoplasms/prevention & control , Peru , Surveys and Questionnaires , Ethnobotany , Medicine, Traditional
15.
Journal of Southern Medical University ; (12): 561-565, 2019.
Article in Chinese | WPRIM | ID: wpr-772043

ABSTRACT

OBJECTIVE@#To investigate the inhibitory effect of genistein on activation of hepatic stellate cells (HSCs) and the role of the autophagy pathway regulated by PPAR-γ in mediating this effect.@*METHODS@#Cultured HSC-T6 cells were exposed to different concentrations of genistein for 48 h, and HSC activation was verified by detecting the expressions of -SMA and 1(I) collagen; autophagy activation in the cells was determined by detecting the expressions of LC3-II and p62 using Western blotting. The autophagy inhibitor 3-MA was used to confirm the role of autophagy in genistein-induced inhibition of HSC activation. A PPAR-γ inhibitor was used to explore the role of PPAR-γ in activating autophagy in the HSCs.@*RESULTS@#Genistein at concentrations of 5 and 50 μmol/L significantly inhibited the expressions of -SMA and 1(I) collagen ( < 0.05), markedly upregulated the expressions of PPAR-γ and the autophagy-related protein LC3-II ( < 0.05) and significantly down-regulated the expression of the ubiqutin-binding protein p62 ( < 0.05) in HSC-T6 cells. The cells pretreated with 3-MA prior to genistein treatment showed significantly increased protein expressions of -SMA and 1(I) collagen compared with the cells treated with genistein only ( < 0.05). Treatment with the PPAR-γ inhibitor obviously lowered the expression of LC3-II and enhanced the expression p62 in genistein-treated HSC-T6 cells, suggesting the activation of the autophagy pathway.@*CONCLUSIONS@#PPAR-γ- regulated autophagy plays an important role in mediating genistein-induced inhibition of HSC activation .


Subject(s)
Humans , Anticarcinogenic Agents , Pharmacology , Autophagy , Collagen Type I , Genistein , Pharmacology , Hepatic Stellate Cells , PPAR gamma , Physiology
16.
Rev. bras. enferm ; 71(5): 2561-2569, Sep.-Oct. 2018. tab, graf
Article in English | LILACS, BDENF | ID: biblio-958723

ABSTRACT

ABSTRACT Objective: To identify in the literature the cardiovascular adverse events resulting from oral antineoplastic therapy. Method: Integrative review of the literature through the SCOPUS, Scientific Electronic Library Online (SciELO), Cumulative Index to Nursing and Allied Health Literature (CINAHL), Medical Literature Analysis and Retrieval System Online (MEDLINE) databases. The antineoplastic, cardiotoxicity, cardiovascular system and adverse reaction descriptors were used in Portuguese, English and Spanish. We selected 23 articles published between 1985 and 2015. Results: Twenty studies were related to cardiac events and eleven to peripheral vascular events. The most frequent adverse cardiac events were reduced left ventricular ejection fraction, myocardial infarction, changes in the electrocardiogram, heart failure and angina, whereas peripheral vascular events were hypertension and thromboembolism. Conclusion: Oral antineoplastic therapy is associated with different adverse events, including cardiac and peripheral vascular events.


RESUMEN Objetivo: Identificar en la literatura los eventos adversos cardiovasculares derivados de la terapia antineoplásica oral. Método: Revisión integrativa de literatura en las bases de datos SCOPUS, Scientific Electronic Library Online (SciELO), Cumulative Index to Nursing and Allied Health Literature (CINAHL) y Medical Literature Analysis and Retrieval System Online (MEDLINE). Se utilizaron descriptores antineoplásicos, cardiotoxicidad, el sistema cardiovascular y reacción adversa en Portugués, Inglés y Español. Se seleccionaron 23 artículos publicados entre 1985 y 2015. Resultados: Veinte estudios estaban relacionados con los eventos cardiacos y once con los eventos vasculares periféricos. Los eventos adversos cardiacos más frecuentes fueron la disminución de la fracción de eyección del ventrículo izquierdo, infarto de miocardio, cambios en el electrocardiograma, insuficiencia cardíaca y angina, mientras que los vasculares periféricos fueron hipertensión arterial y tromboembolismo. Conclusión: La terapia antineoplásica oral está asociada a diferentes eventos adversos, entre ellos los cardíacos y los vasculares periféricos.


RESUMO Objetivo: Identificar na literatura os eventos adversos cardiovasculares decorrentes da terapia antineoplásica oral. Método: Revisão integrativa de literatura nas bases de dados SCOPUS, Scientific Electronic Library Online (SciELO), Cumulative Index to Nursing and Allied Health Literature (CINAHL) e Medical Literature Analysis and Retrieval System Online (MEDLINE). Utilizaram-se os descritores antineoplásicos, cardiotoxicidade, sistema cardiovascular e reação adversa, em português, inglês e espanhol. Foram selecionados 23 artigos publicados entre 1985 e 2015. Resultados: Vinte estudos estavam relacionados aos eventos cardíacos e onze aos eventos vasculares periféricos. Os eventos adversos cardíacos mais frequentes foram diminuição da fração de ejeção do ventrículo esquerdo, infarto do miocárdio, alterações no eletrocardiograma, insuficiência cardíaca e angina, enquanto que os vasculares periféricos foram hipertensão arterial e tromboembolismo. Conclusão: A terapia antineoplásica oral está associada a diferentes eventos adversos, dentre eles os cardíacos e os vasculares periféricos.


Subject(s)
Humans , Cardiovascular Diseases/etiology , Antineoplastic Agents/adverse effects , Administration, Oral , Anticarcinogenic Agents/adverse effects , Anticarcinogenic Agents/therapeutic use , Drug-Related Side Effects and Adverse Reactions , Drug-Related Side Effects and Adverse Reactions/etiology , Antineoplastic Agents/therapeutic use
17.
The Korean Journal of Physiology and Pharmacology ; : 235-248, 2018.
Article in English | WPRIM | ID: wpr-728618

ABSTRACT

Ursolic acid (UA) is a natural triterpene compound found in various fruits and vegetables. There is a growing interest in UA because of its beneficial effects, which include anti-inflammatory, anti-oxidant, anti-apoptotic, and anti-carcinogenic effects. It exerts these effects in various tissues and organs: by suppressing nuclear factor-kappa B signaling in cancer cells, improving insulin signaling in adipose tissues, reducing the expression of markers of cardiac damage in the heart, decreasing inflammation and increasing the level of anti-oxidants in the brain, reducing apoptotic signaling and the level of oxidants in the liver, and reducing atrophy and increasing the expression levels of adenosine monophosphate-activated protein kinase and irisin in skeletal muscles. Moreover, UA can be used as an alternative medicine for the treatment and prevention of cancer, obesity/diabetes, cardiovascular disease, brain disease, liver disease, and muscle wasting (sarcopenia). In this review, we have summarized recent data on the beneficial effects and possible uses of UA in health and disease managements.


Subject(s)
Adenosine , Anticarcinogenic Agents , Atrophy , Brain , Brain Diseases , Cardiovascular Diseases , Complementary Therapies , Disease Management , Fruit , Heart , Inflammation , Insulin , Liver , Liver Diseases , Muscle, Skeletal , Oxidants , Protein Kinases , Vegetables
18.
J. venom. anim. toxins incl. trop. dis ; 24: 12, 2018. graf, ilus
Article in English | LILACS | ID: biblio-894176

ABSTRACT

Cnidarian venoms and extracts have shown a broad variety of biological activities including cytotoxic, antibacterial and antitumoral effects. Most of these studied extracts were obtained from sea anemones or jellyfish. The present study aimed to determine the toxic activity and assess the antitumor and antiparasitic potential of Palythoa caribaeorum venom by evaluating its in vitro toxicity on several models including human tumor cell lines and against the parasite Giardia intestinalis. Methods: The presence of cytolysins and vasoconstrictor activity of P. caribaeorum venom were determined by hemolysis, PLA2 and isolated rat aortic ring assays, respectively. The cytotoxic effect was tested on HCT-15 (human colorectal adenocarcinoma), MCF-7 (human mammary adenocarcinoma), K562 (human chronic myelogenous leukemia), U251 (human glyoblastoma), PC-3 (human prostatic adenocarcinoma) and SKLU-1 (human lung adenocarcinoma). An in vivo toxicity assay was performed with crickets and the antiparasitic assay was performed against G. intestinalis at 24 h of incubation. Results: P. caribaeorum venom produced hemolytic and PLA2 activity and showed specific cytotoxicity against U251 and SKLU-1 cell lines, with approximately 50% growing inhibition. The venom was toxic to insects and showed activity against G. intestinalis in a dose-dependent manner by possibly altering its membrane osmotic equilibrium. Conclusion: These results suggest that P. caribaeorum venom contains compounds with potential therapeutic value against microorganisms and cancer.(AU)


Subject(s)
Animals , Male , Rats , Giardiasis/therapy , Giardia lamblia/parasitology , Cnidarian Venoms/antagonists & inhibitors , Cnidarian Venoms/toxicity , Anticarcinogenic Agents , Rats, Wistar , Cnidarian Venoms/therapeutic use , Hemolytic Agents
19.
Braz. J. Pharm. Sci. (Online) ; 54(2): e17513, 2018. tab, graf, ilus
Article in English | LILACS | ID: biblio-951937

ABSTRACT

ABSTRACT Temozolomide is a poorly soluble anti-cancer drug used in the treatment of some brain cancers. Following literature reports about the enhancement of solubility and stability for these kinds of drugs upon complexation with cyclodextrins, we aimed to form an inclusion complex between temozolomide and the different types of cyclodextrins (CDs) to enhance its solubility. In this study, three different cyclodextrins (ß -CD, hydroxyl-ß-CD and γ-CD) were used, and changes in solubility was measured by UV-Vis Spectroscopy and HPLC. Morphological changes upon complexation were shown by the Scanning Electron Microscope (SEM), and weight loss profiles with respect to temperatures which were unique to the compounds were shown by Thermogravimetric Analysis. Changes in heat release profiles were shown by Differential Scanning Calorimeter (DSC). Drug solubility was measured to be increased to around 25% for 1:1 molar ratio for all used CD complexations. Changes of morphology, heat release and weight loss profiles are consistent with the formation of an inclusion complex between CDs and temozolomide. In this study, success was shown in the enhancement of temozolomide solubility upon complexation with different types of CDs. It has been demonstrated that cyclodextrins can be used as complexing agents for poorly soluble anti-cancer drugs, increasing their solubility and hence drug availability


Subject(s)
Solubility , Anticarcinogenic Agents/analysis , Cyclodextrins/adverse effects , Pharmaceutical Preparations , Microscopy, Electron, Scanning/methods
20.
São Paulo; s.n; s.n; 2018. 79 p. graf, ilus, tab.
Thesis in Portuguese | LILACS | ID: biblio-883230

ABSTRACT

O câncer primário de fígado (CPF) apresenta mau prognóstico, o que torna importante sua quimioprevenção. Nesse sentido, a tributirina (TB), um pró-fármaco do ácido butírico (AB), presente em laticínios e no mel, mostrou-se um agente quimiopreventivo promissor da hepatocarcinogênese experimental. Os efeitos inibitórios da TB têm sido relacionados à inibição do desenvolvimento de lesões pré-neoplásicas, bem como indução de apoptose e hiperacetilação de histonas. A quimioterapia é uma das abordagens mais comuns para o tratamento de diversos tipos de câncer, inclusive o CPF. Neste caso, o tratamento com sorafenibe (SO) é capaz de prolongar a sobrevida média dos pacientes com a doença em fases avançadas em aproximadamente apenas três meses. Em vista disso, são necessários estudos da associação do sorafenibe com outros compostos que possam aumentar a eficácia do tratamento quimioterápico. Desta forma, a associação de fármacos anti-neoplásicos com compostos bioativos dos alimentos pode consistir em uma estratégia potencial para aumentar a eficácia contra o câncer. No presente estudo, foi avaliada a atividade anticarcinogênica da TB e do SO, isoladamente ou em associação, na etapa de progressão da hepatocarcinogênese. Para tanto, foram realizados implantes singênicos no flanco de ratos Fischer-344 a partir de células da linhagem tumoral GP7TB. Quando as neoplasias atingiram 1 cm3, os animais foram aleatorizados em grupos experimentais: Grupo controle (CO), constituído por 10 ratos Fischer 344 que receberam Maltodextrina (300mg/ 100 g. p. c.), controle isocolarico e solução de etanol à 12,5% e Cremofor à 12,5% em agua estéril; Grupo Tributirina (TB), constituído por 9 ratos Fischer 344 que receberam TB (200mg/ 100 g. p. c.) e solução de etanol à 12,5% e Cremofor à 12,5% em água estéril; Grupo sorafenibe (SO) constituído por 9 ratos Fischer 344 que receberam Maltodextrina (300 mg/ 100 g. p. c.), controle isocalorico e tosilato de sorafenibe (3mg / 100 g. p. c. ) em água estéril; Grupo associação da tributirina com o sorafenibe (AS) constituído por 9 ratos Fischer 344 que receberam TB (20 mg/ 100 g. p. c.) e tosiliato de sorafenibe (3mg/ 100 g. p. c.); tratados por administração intragástrica (i.g) diariamente por 5 semanas consecutivas. As concentrações de AB e SO foram analisadas por cromatografia gasosa associada à espectrometria de massa e as neoplasias foram caracterizadas por imunoistoquímica. Em relação à evolução do tamanho das neoplasias o grupo AS apresentou menor (p=0,009) tamanho das mesmas em relação ao grupo CO. No entanto, estas diferenças não atingiram diferenças significativas (p>0,05) entre os grupos TB e CO, bem como entre os grupos SO e CO. Contudo, quando ajustados os valores do tamanho da neoplasia pela latência, observou-se alterações significativas (p<0,05) nos diversos grupos quando comparados ao grupo CO. O grupo SO aumentou a área necrótica das neoplasias, embora esta diferença não tenha atingido diferença significativa (p>0,05), enquanto que o grupo TB reduziu essa área necrótica em relação ao grupo CO (p=0,005). O grupo TB e AS apresentaram significativamente maiores (p<0,05) concentrações hepáticas e neoplásicas de AB em relação ao grupo CO. O grupo SO e AS apresentaram significativamente maiores (p<0,05) concentrações neoplásicas de SO em relação ao grupo CO. Os grupos SO e AS reduziram a expressão de PTEN, quando comparados ao grupo CO, embora esta diferença não tenha atingido diferença significativa (p>0,05). O grupo TB por sua vez expressou maiores niveis de PTEN, embora esta diferença não tenha atigindo significância estatística (p>0,05). Todos os grupos expressaram maiores niveis de caspase 3 clivada quando comparada ao grupo CO (p>0,05). OS grupos TB e SO reduziram a expressão de pERK ½ quando comparados ao grupo CO. embora estas diferenças não tenham atingidos diferença estatística (p>0,05). O grupo AS apresentou maior expressão de pERK ½ quando comparada ao grupo CO, embora esta diferença não tenha atingido diferença significativa (p>0,05). A caracterização das neoplasias do grupo CO foi padronizada por imunoistoquímica, apresentando-se positivas para CK 7, CK8, CK19 e Arginase e negativas para HepPar1 e CK18. Assim, os resultados sugerem que as neoplasias obtidas por implantes com células da linhagem GP7TB apresentam características de CPF oriundo de células tronco neoplásicas. Além disso, os grupos experimentais TB e AS apresentaram atividade anticarcinogênica promissora no modelo de implantes singênicos com células GP7TB, que eventualmente envolvem mecanismos de ação distintos da atividade quimioterápica apresentada pelo SO


Primary liver cancer (PLC) presents poor prognosis, which makes its chemoprevention important. In this sense, tributyrin (TB), a prodrug of butyric acid (AB), present in dairy products and honey, has been shown to be a promising chemopreventive agent for experimental hepatocarcinogenesis. The inhibitory effects of TB have been related to inhibition of the development of pre-neoplastic lesions, as well as induction of apoptosis and hyperacetylation of histones. Chemotherapy is one of the most common approaches for treating various types of cancer, including PLC. In this case, treatment with sorafenib (SO) is able to prolong the average survival of patients with the disease in advanced stages in approximately three months. In view of this, studies of the association of sorafenib with other compounds that may increase the efficacy of chemotherapeutic treatment are necessary. Thus, the association of anti-neoplastic drugs with bioactive compounds in food may be a potential strategy to increase efficacy against cancer. In the present study, the anticarcinogenic activity of TB and SO was evaluated, alone or in combination, in the progression stage of hepatocarcinogenesis. For this purpose, syngenic implants were performed on the flank of Fischer-344 mice from GP7TB tumor cells. When the neoplasms reached 1 cm3, the animals were randomized into experimental groups: Control group (CO), consisting of 10 Fischer 344 rats receiving Maltodextrin (300mg / 100 g.p.c), isocaloric control and 12.5% ethanol solution, and Cremofor to 12.5% in sterile water; Tributyrin group (TB), consisting of 9 Fischer 344 rats that received TB (200mg / 100 g.p.c.) and 12.5% ethanol solution and Cremofor 12.5% in sterile water; Sorafenib group (SO) consisting of 9 Fischer 344 rats receiving maltodextrin (300 mg / 100 g, w / w), isocaloric control and sorafenib tosylate (3 mg / 100 g, w / w) in sterile water; The association group of tributyrin and sorafenib (AS) consisted of 9 Fischer 344 rats receiving TB (20 mg / 100 g p.o.) and sorafenib tosylate (3 mg / 100 g p.o.); treated intragastric (i.g) daily for 5 consecutive weeks. The concentrations of AB and SO were analyzed by gas chromatography associated with mass spectrometry and the neoplasms were characterized by immunohistochemistry. In relation to the evolution of the size of the neoplasias, the AS group presented smaller (p = 0.009) size of the same ones in relation to the CO group. However, these differences did not reach significant differences (p> 0.05) between the TB and CO groups, as well as between the SO and CO groups. However, when adjusted for size of the neoplasm by latency, significant changes (p <0.05) were observed in the different groups when compared to the CO group. The SO group increased the necrotic area of the neoplasias, although this difference did not reach a significant difference (p> 0.05), while the TB group reduced this necrotic area in relation to the CO group (p = 0.005). The TB and AS groups presented significantly higher (p <0.05) hepatic and neoplastic AB concentrations than the CO group. The SO and AS groups presented significantly higher (p <0.05) neoplastic concentrations of SO in relation to the CO group. The SO and AS groups reduced the PTEN expression when compared to the CO group, although this difference did not reach a significant difference (p> 0.05). The TB group in turn expressed higher levels of PTEN, although this difference did not increase statistical significance (p> 0.05). All groups expressed higher levels of caspase 3 cleaved when compared to the CO group (p> 0.05). The TB and SO groups reduced the expression of pERK ½ when compared to the CO group. although these differences did not reach statistical difference (p> 0.05). The AS group presented higher pERK ½ expression when compared to the CO group, although this difference did not reach a significant difference (p> 0.05). Characterization of the neoplasias of the CO group was standardized by immunohistochemistry, presenting positive for CK 7, CK8, CK19 and Arginase and negative for HepPar1 and CK18. Thus, the results suggest that the neoplasias obtained by implants with GP7TB cells present CPF characteristics originating from neoplastic stem cells. In addition, the experimental groups TB and AS presented promising anticarcinogenic activity in the model of syngeneic implants with GP7TB cells, which eventually involve mechanisms of action distinct from the chemotherapy activity presented by SO


Subject(s)
Animals , Male , Rats , Pharmaceutical Preparations/analysis , Anticarcinogenic Agents/analysis , Liver Neoplasms/prevention & control , Immunohistochemistry/methods , Tumor Cells, Cultured/classification , Blotting, Western/instrumentation , Data Interpretation, Statistical , Carcinoma, Hepatocellular , Butyric Acid/agonists , Gas Chromatography-Mass Spectrometry/methods
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