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1.
Fitoterapia ; 139: 104360, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31629869

RESUMO

Five new lignans mubiesins A - E (1-5), together with twenty-seven known compounds (6-32), were isolated from the cytotoxicity and anti-inflammation portions of Momordica cochinchinensis seeds which were widely used for various tumors and inflammations. Their structures were elucidated by extensive spectroscopic analyses (HR-MS, UV, CD, IR, 1D-NMR, and 2D-NMR). Their cytotoxic and anti-inflammatory activities were evaluated in vitro. Various lignans and saponins showed the significant activities, they could obviously inhibit the growth of tumor cells and the release of NO and TNF-α in RAW 264.7 cells induced by LPS.


Assuntos
Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Lignanas/farmacologia , Momordica/química , Saponinas/farmacologia , Sementes/química , Animais , Anti-Inflamatórios/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , China , Humanos , Lignanas/isolamento & purificação , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Células RAW 264.7 , Saponinas/isolamento & purificação
2.
Curr Med Chem ; 26(24): 4585-4605, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31284852

RESUMO

Gac, Momordica cochinchinensis (Lour.) Spreng. belongs to the Cucurbitaceae family. It is more considered as a super fruit. The demand for this plant is growing in countries where its reputation is high, including traditional countries of gac culture and countries fond of super fruits and food supplements. In these latter countries, the industrial strategy aims at producing high added value in food supplements or nutritional rich preparations. However, when marketing is not the driving force and claims have to be related to scientific data, the situation of gac is less "heavenly", mainly because its most remarkable properties are in the field of micronutrients. These latter components are indeed very important for health but their supplementation on healthy populations brings no significant advantage. This paper proposes to review aspects important for the nutritional reputation of this plant: where it comes from, how it is cultured to have an optimal nutritional composition, what is its composition and how it can impact health of consumers, in which products it is used and what are the regulations to use it in different markets. One important goal of this review is to give a critical and scientific approach to confirm data on this fruit, which has been promoted by marketing departments injecting so many wrong and unverified information. Missing data will be highlighted and potential positive applications are proposed all along the text.


Assuntos
Momordica/química , Anti-Inflamatórios/química , Antioxidantes/química , Antioxidantes/uso terapêutico , Carotenoides/química , Carotenoides/uso terapêutico , Suplementos Nutricionais/análise , Frutas/química , Frutas/metabolismo , Humanos , Momordica/metabolismo , Neoplasias/tratamento farmacológico , Polifenóis/química , Polifenóis/uso terapêutico , Vitaminas/química
3.
Biomed Pharmacother ; 116: 108925, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31112874

RESUMO

BACKGROUND: Chronic hyperglycaemia-induced haematological changes increase the risk of cardiovascular complications in diabetic patients. The administration of insulin injection as a bolus is accompanied with increased blood viscosity, which is not recommended for patients with congestive heart failure. Momordica balsamina methanolic extract (MB) has previously been shown to possess anti-hyperglycaemic and renal dysfunction ameliorative effects; however, the haematological effects of MB have not been shown. The current study therefore, investigated the short-term effects MB on selected haematological parameters in streptozotocin (STZ)-induced diabetic rats. METHODS: Briefly, the air-dried Momordica balsamina leaves were sequentially extracted with methanol to yield a methanolic extract. STZ-induced diabetic rats were divided into untreated and treated groups with insulin (170 µg kg-1 s.c.) and metformin (500 mg kg-1 p.o.) MB (250 mg kg-1 p.o.). MB was administered twice daily for the 5-week experimental period. Blood glucose concentration was monitored weekly. Animals were sacrificed terminally. Blood and kidneys were collected for haematological and biochemical analysis respectively. RESULTS: Treatment with MB significantly decreased blood glucose concentration and improved erythropoietin secretion, thus significantly increasing red blood cell production in treated diabetic animals by comparison to untreated animals. MB also significantly improved haemoglobin concentrations and moderately increased erythrocyte indices specifically, mean corpuscular volume (MCV), mean corpuscular haemoglobin concentration (MCHC) and mean corpuscular haemoglobin (MCH) to no significance by comparison to untreated diabetic animals. MB treatment decreased the oxidative stress evoked by the induction of diabetes while improving the antioxidant status of treated animals by comparison to untreated animals respectively. CONCLUSIONS: Administration of Momordica balsamina methanolic extract protects against some injurious haematological changes induced by hyperglycaemia, which may reduce the risks of cardiovascular complications.


Assuntos
Biomarcadores/metabolismo , Diabetes Mellitus Experimental/tratamento farmacológico , Metanol/química , Momordica/química , Extratos Vegetais/uso terapêutico , Animais , Glicemia/metabolismo , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/patologia , Membrana Eritrocítica/metabolismo , Eritropoetina/sangue , Glutationa Peroxidase/metabolismo , Masculino , Malondialdeído/metabolismo , Extratos Vegetais/farmacologia , Ratos Sprague-Dawley , Estreptozocina , Superóxido Dismutase/metabolismo
4.
Curr Pharm Des ; 25(6): 715-728, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30931848

RESUMO

Momordica cochinchinensis (Lour.) Spreng (M. cochinchinensis) is a deciduous vine that grows in Southeast Asia. It is known as gac in Vietnam and as Red Melon in English. Gac is reputed to be extremely benificial for health and has been widely used as food and folk medicine in Southeast Asia. In China, the seed of M. cochinchinensis (Chinese name: Mu biezi) is used as traditional Chinese medicine (TCM) for the treatment of various diseases. More than 60 chemical constituents have been isolated from M. cochinchinensis. Modern pharmacological studies and clinical practice demonstrate that some chemical constituents of M. cochinchinensis possess wide pharmacological activities, such as anti-tumor, anti-oxidation, anti-inflammatory, etc. This paper reviews the phytochemistry, pharmacological activities, toxicity, and clinical application of M. cochinchinensis, aiming to bring new insights into further research and application of this ancient herb.


Assuntos
Momordica/química , Extratos Vegetais/farmacologia , Sementes/química , Medicina Tradicional Chinesa , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química
5.
Acta Biochim Biophys Sin (Shanghai) ; 51(4): 365-374, 2019 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-30877761

RESUMO

Momordica grosvenori is a valuable edible plant with medicinal purposes, and it is widely used in medicated diets and traditional Chinese medicine in Asia. Mogroside V (MV), the main bioactive component from M. grosvenori, is commonly used as a natural sweetener. M. grosvenori extracts have been reported to exert potent anti-inflammatory property, however the underlying molecular mechanism still remains unknown. In the present study, the biological effect of MV in inflammation was investigated in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. The ELISA and western blot analysis results showed that MV significantly inhibited LPS-induced prostaglandin E2 (PGE2) production and cyclooxygenase-2 (COX-2) expression. MV markedly decreased the phosphorylation of IκB-α, increased IκB-α, and reduced nuclear p-65 and C/EBPδ. Furthermore, MV attenuated LPS-induced phosphorylation of MAPKs and AKT1, and only the phosphorylation status of AKT1 was found to be consistent with the expression trend of COX-2. Moreover, MV reduced ROS level and restored overexpressed HO-1 and AP-1 to basal level, which can be markedly reversed by AKT1 inhibitor LY294002. These results revealed that AKT1 plays a key role in LPS-induced COX-2 expression, and acts as a mediator to keep the redox balance in LPS-stimulated RAW264.7 cells. MV exerts anti-inflammatory property by blocking AKT1-mediated NF-κB and C/EBPδ activation, ROS generation and AP-1/ HO-1 expression. Therefore, the present study indicated that MV has a significant chemopreventive effect on the inflammatory lesions and suggested that AKT1 is a potential specific target of MV for relieving inflammation.


Assuntos
Ciclo-Oxigenase 2/genética , Heme Oxigenase-1/genética , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-akt/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Triterpenos/farmacologia , Animais , Ciclo-Oxigenase 2/metabolismo , Dinoprostona/metabolismo , Regulação da Expressão Gênica/efeitos dos fármacos , Heme Oxigenase-1/metabolismo , Macrófagos/citologia , Macrófagos/metabolismo , Camundongos , Estrutura Molecular , Momordica/química , Fosforilação/efeitos dos fármacos , Células RAW 264.7 , Triterpenos/química
6.
J Sci Food Agric ; 99(1): 379-390, 2019 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-29888551

RESUMO

BACKGROUND: In the USA, Momordica charantia is relatively unknown and is usually found in specialty markets. In the present study, cultivation of five bitter melon cultivars grown under field conditions in College Station (TX, USA), was evaluated. Additionally, ascorbic acid, amino acids and phenolic compounds were quantified from various cultivars grown in different years. RESULTS: The yield of the first year of evaluation was comparable to other bitter melon growing regions, ranging from 9371.5 kg ha-1 for the Japanese Spindle cultivar to 20 839.1 kg ha-1 for the Hong Kong Green cultivar. Multivariate analysis suggests a strong correlation between yield and growth degree days, water use efficiency and organic matter, as well as an inverse correlation with the amount or precipitation during the growing season. The highest levels of total ascorbic acid were shown in the Japanese Spindle cultivar (162.97 mg 100 g-1 fresh fruit), whereas the lowest levels were expressed in the Hong Kong Green cultivar (42.69 mg 100 g-1 fresh fruit). The highest levels of total phenolics were consistently found the Indian White cultivar, in the range 10.6-12.5 mg g-1 catechin equivalents. Seven phenolics and organic acids were identified and quantified by liquid chromatography-mass spectrometry and high-performance liquid chromatography, respectively. Additionally, the highest levels of total amino acids were found in the Large Top cultivar. CONCLUSION: The current 3-year field study demonstrates that it is feasible to grow bitter melon commercially in Texas with proper climatic and agronomic conditions. Bitter melon is a rich source for ascorbic acid, amino acids and phenolic compounds, which makes it a valuable food source with respect to improving human health. © 2018 Society of Chemical Industry.


Assuntos
Frutas/química , Momordica/crescimento & desenvolvimento , Compostos Fitoquímicos/análise , Aminoácidos/análise , Ácido Ascórbico/análise , Cromatografia Líquida de Alta Pressão , Frutas/crescimento & desenvolvimento , Espectrometria de Massas , Momordica/química , Momordica/classificação , Valor Nutritivo , Fenóis/análise , Extratos Vegetais/análise , Estações do Ano , Texas
7.
Molecules ; 23(8)2018 Jul 29.
Artigo em Inglês | MEDLINE | ID: mdl-30060618

RESUMO

Obesity and nonalcoholic fatty liver disease (NAFLD) are highly prevalent and cause numerous metabolic diseases. However, drugs for the prevention and treatment of obesity and NAFLD remain unavailable. In this study, we investigated the effects of mogrosides (luo han guo, LH) in Siraitia grosvenorii saponins on high-fat-diet-induced obesity and NAFLD in mice. We found that compared with the negative control, LH reduced body and liver weight. LH also decreased fat accumulation and increased AMP-activated protein kinase (AMPK) phosphorylation (pAMPK) levels in mouse livers. We also found that high-purity mogroside V upregulated pAMPK expression in HepG2 cells. In addition, high-purity mogroside V inhibited reactive oxygen species production and upregulated sequestosome-1 (SQSTM1, p62) expression in THP-1 cells. These results suggest that LH may affect obesity and NAFLD by enhancing fat metabolism and antioxidative defenses. Mogroside V may be a main component of LH. However, the exact molecular mechanisms and active components responsible for the inhibitory effects of LH on obesity and NAFLD require further investigation.


Assuntos
Fármacos Antiobesidade/farmacologia , Anticolesterolemiantes/farmacologia , Momordica/química , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Obesidade/tratamento farmacológico , Triterpenos/farmacologia , Proteínas Quinases Ativadas por AMP/genética , Proteínas Quinases Ativadas por AMP/metabolismo , Tecido Adiposo/efeitos dos fármacos , Tecido Adiposo/metabolismo , Tecido Adiposo/patologia , Animais , Fármacos Antiobesidade/química , Fármacos Antiobesidade/isolamento & purificação , Anticolesterolemiantes/química , Anticolesterolemiantes/isolamento & purificação , Peso Corporal/efeitos dos fármacos , Dieta Hiperlipídica/efeitos adversos , Regulação da Expressão Gênica , Células Hep G2 , Humanos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Masculino , Camundongos , Hepatopatia Gordurosa não Alcoólica/etiologia , Hepatopatia Gordurosa não Alcoólica/metabolismo , Hepatopatia Gordurosa não Alcoólica/patologia , Obesidade/etiologia , Obesidade/metabolismo , Obesidade/patologia , Tamanho do Órgão/efeitos dos fármacos , Espécies Reativas de Oxigênio/antagonistas & inibidores , Espécies Reativas de Oxigênio/metabolismo , Saponinas/química , Saponinas/isolamento & purificação , Saponinas/farmacologia , Proteína Sequestossoma-1/agonistas , Proteína Sequestossoma-1/genética , Proteína Sequestossoma-1/metabolismo , Células THP-1 , Triterpenos/química , Triterpenos/isolamento & purificação
8.
Planta Med ; 84(18): 1372-1379, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29996165

RESUMO

The collateral sensitivity effect is among the most promising strategies for overcoming multidrug resistance in cancer. In this work, 28 cucurbitane-type triterpenoids (1: -28: ), previously isolated from the African medicinal plant Momordica balsamina and its derivatives, were evaluated for their collateral sensitivity effect on three different human cancer entities, gastric (EPG85-257), pancreatic (EPP85-181), and colon (HT-29), each with two different multidrug-resistant variants. One was selected for its resistance to daunorubicin (EPG85-257RDB, EPP85-181RDB, HT-29RDB) and the other was selected for its resistance to mitoxantrone (EPG85-257RNOV, EPP85-181RNOV, HT-29RNOV). On gastric cell lines, the best results were obtained for compounds 3: and 10: , which exhibited a collateral sensitivity effect together with high antiproliferative activity. In turn, on colon cancer cell lines, the best multidrug resistance-selective antiproliferative effects were observed for derivatives 11, 13: , and 15: , which showed collateral sensitivity effects against both resistant variants. Compounds 11: and 3: were also the most selective against the multidrug resistance pancreatic cells lines. Some compounds, such 6, 10, 11: and 15: , were previously found to be strong P-glycoprotein modulators, thus highlighting their potential as promising leads for overcoming multidrug resistance in cancer cells.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , Momordica/química , Triterpenos/química , Antineoplásicos Fitogênicos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Resistência a Múltiplos Medicamentos/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Concentração Inibidora 50 , Componentes Aéreos da Planta/química , Triterpenos/farmacologia
9.
J Diabetes Res ; 2018: 7341242, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30009183

RESUMO

Background: Studies suggest that Momordica balsamina (intshungu) possesses hypoglycaemic effects. The effects of Momordica balsamina on diabetic complications such as DN, however, have not been established. Accordingly, this study seeks to investigate the effects of M. balsamina on kidney function in STZ-induced diabetic rats. Methods: Methanolic extracts (ME) of M. balsamina's leaves were used in this study. Short-term effects of M. balsamina methanolic extract on kidney function and MAP were studied in STZ-induced diabetic rats treated twice daily with M. balsamina methanolic extract (250 mg/kg), insulin (175 µg/kg, s.c.), and metformin (500 mg/kg) for 5 weeks. Results: M. balsamina methanolic extract significantly increased Na+ excretion outputs in STZ-induced diabetic rats by comparison to STZ-diabetic control rats. M. balsamina methanolic extract significantly increased GFR in STZ-diabetic rats with a concomitant decrease in creatinine concentration and also reduced kidney-to-body ratio, albumin excretion rate (AER), and albumin creatinine ratio (ACR). M. balsamina methanolic extract significantly reduced MAP in STZ-diabetic animals by comparison with STZ-diabetic control animals. These results suggest that M. balsamina methanolic extract not only lowers blood glucose but also has beneficial effects on kidney function and blood pressure. Conclusion: These findings suggest that M. balsamina may have beneficial effects on some processes that are associated with renal derangement in STZ-induced diabetic rats.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Rim/efeitos dos fármacos , Momordica/química , Extratos Vegetais/farmacologia , Albuminas/metabolismo , Aldosterona/sangue , Animais , Pressão Sanguínea , Creatinina/metabolismo , Eletrólitos , Taxa de Filtração Glomerular , Hipoglicemiantes/farmacologia , Insulina/química , Rim/fisiologia , Testes de Função Renal , Masculino , Metformina/química , Estresse Oxidativo , Folhas de Planta/metabolismo , Ratos , Ratos Sprague-Dawley , Sódio/química
10.
Mol Carcinog ; 57(10): 1319-1331, 2018 10.
Artigo em Inglês | MEDLINE | ID: mdl-29873419

RESUMO

p-Hydroxylcinnamaldehyde isolated from the Cochinchina momordica seed (CMSP) has been identified to inhibit growth and metastasis in oesophageal squamous cell carcinoma (ESCC) by inducing differentiation. The aim of the present study was to evaluate the effect and underlying mechanism of CMSP on 4-nitroquinoline 1-oxide (4NQO)-induced oesophageal tumourigenesis. In the present study, a mouse model of oesophageal preneoplastic lesions was established by providing 4NQO-containing drinking water to C57BL/6 mice. The effect of CMSP on tumourigenesis induced by the chemical mutagen and the effect of CMSP on immune function were investigated. The results showed that the incidence and pathological stage of atypical hyperplasia in oesophageal tissues were significantly reduced in CMSP-treated mice compared with untreated mice. Immunohistochemistry and pull-down assay results revealed that the expression levels of p-ERK1/2, p-SAPK/JNK, and GTP-RhoA were significantly decreased in the oesophageal tissue of CMSP-treated mice. In addition, the proportions of CD4+ T cells, CD8+ T cells, and NK cells were increased, while the proportion of CD4+ CD25+ regulatory T cells (Tregs) was decreased, in the peripheral blood of CMSP-treated mice. These results indicated that CMSP could hamper 4NQO-induced oesophageal tumourigenesis by regulating the RhoA-ERK/JNK signaling pathway and promoting immune system function, thus providing a new potential strategy for treating preneoplastic lesions of the oesophagus.


Assuntos
Carcinogênese/efeitos dos fármacos , Cinamatos/farmacologia , Neoplasias Esofágicas/prevenção & controle , Carcinoma de Células Escamosas do Esôfago/prevenção & controle , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Proteína rhoA de Ligação ao GTP/metabolismo , 4-Nitroquinolina-1-Óxido , Animais , Carcinogênese/induzido quimicamente , Carcinogênese/metabolismo , Progressão da Doença , Neoplasias Esofágicas/induzido quimicamente , Neoplasias Esofágicas/metabolismo , Carcinoma de Células Escamosas do Esôfago/induzido quimicamente , Carcinoma de Células Escamosas do Esôfago/metabolismo , Esôfago/efeitos dos fármacos , Esôfago/metabolismo , Esôfago/patologia , Camundongos Endogâmicos C57BL , Momordica/química , Extratos Vegetais/farmacologia , Lesões Pré-Cancerosas/induzido quimicamente , Lesões Pré-Cancerosas/metabolismo , Lesões Pré-Cancerosas/prevenção & controle , Sementes/química
11.
Zhongguo Zhong Yao Za Zhi ; 43(6): 1175-1181, 2018 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-29676125

RESUMO

The liposoluble constituents in Momordicae Semen were investigated in the present study. By silica gel, Sephadex LH-20 column chromatography, and semi-preparative HPLC, 22 compounds were isolated and purified from dichloromethane and ethyl acetate fraction. Based on NMR and MS spectra analyses, these compounds were identified as lupeol (1), 5-(1'-hydroxypentyl)-5H-furan-2-one (2), palmitic acid (3), viscumamide (4), clavatustide C (5), laxanol (6), threo-1-(4-hydroxyphenyl)-2-{4-[2-formyl-(E)-vinyl]-2-methoxyphenoxyl}-propane-1, 3-diol (7), α-spinasterol-3-O-ß-D-glucoside (8), chushizisin F (9), ehletianol C (10), tanegool (11), (7R, 8R, 8'R)-4'-guaiacylglyceryl-evofolin B (12), ligballinone (13), (7R, 8S, 8'R)- 4, 4', 9-trihydroxy- 7, 9'-epoxy- 8, 8'-lignan (14), chushizisin I (15), chushizisin A (16), chushizisin G (17), p-coumaraldehyde (18), α-spinasterol (19), p-hydroxybenzoic acid (20), chushizisin E (21), and 3-[2-(4-hydroxyphenyl)-3-hydroxyphenyl-2, 3-dihydro-1-benzofuran-5-yl] propane-1-ol (22), respectively. Compounds 1-17 were isolated from Momordica cochinchinensis for the first time. Compound 2 was a new natural product while compounds 4 and 5 were first found in the terrestrial organism.


Assuntos
Medicamentos de Ervas Chinesas/química , Momordica/química , Compostos Fitoquímicos/química , Sementes/química , Cromatografia Líquida de Alta Pressão , Espectroscopia de Ressonância Magnética , Compostos Fitoquímicos/isolamento & purificação
12.
ACS Chem Biol ; 13(6): 1525-1535, 2018 06 15.
Artigo em Inglês | MEDLINE | ID: mdl-29630823

RESUMO

The occurrence of autoantibodies is a hallmark of rheumatoid arthritis, specifically those autoantibodies targeting proteins containing the arginine-derived amino acid citrulline. There is strong evidence showing that the occurrence of anticitrullinated protein/peptide antibodies (ACPA) are involved in disease progression, and ACPA was recently shown to induce pain in animals. Here, we explore a novel concept useful for research, diagnostics, and possibly therapy of autoimmune diseases, namely, to directly target and neutralize autoantibodies using peptide binders. A high-affinity peptide-based scavenger of ACPA was developed by grafting a citrullinated epitope derived from human fibrinogen into a naturally occurring stable peptide scaffold. The best scavenger comprises the truncated epitope α-fibrinogen, [Cit573]fib(566-580), grafted into the scaffold sunflower trypsin inhibitor-1, SFTI-1. The final peptide demonstrates low nanomolar apparent affinity and superior stability.


Assuntos
Anticorpos Anti-Proteína Citrulinada/imunologia , Artrite Reumatoide/diagnóstico , Peptídeos Cíclicos/imunologia , Ciclização , Desenho de Fármacos , Epitopos , Fibrinogênio/síntese química , Fibrinogênio/química , Fibrinogênio/imunologia , Helianthus/química , Humanos , Estrutura Molecular , Momordica/química , Fragmentos de Peptídeos/síntese química , Fragmentos de Peptídeos/química , Fragmentos de Peptídeos/imunologia , Peptídeos Cíclicos/síntese química , Peptídeos Cíclicos/química , Ligação Proteica , Estabilidade Proteica
13.
Int J Biol Macromol ; 114: 226-234, 2018 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-29471092

RESUMO

Balsamin, a type I ribosome-inactivating protein (RIP), has been shown to inhibit HIV-1 replication at the translation step. Our recent studies have shown that balsamin also possess anti-tumor, antibacterial and DNase-like activity, however, the amount of natural balsamin in Momordica balsamina seeds is limited and preclinical studies require large quantities of pure, bioactive balsamin. Therefore, in this study, we cloned the balsamin gene, expressed it in E.coli BL21 (DE3) strain and purified it by nickel affinity chromatography. Functional analysis indicated that balsamin exhibits both RNA N-glycosidase activity, releasing the Endo-fragment from rabbit reticulocyte rRNA, and DNase-like activity, converting the supercoiled form of a plasmid into the linear form in a concentration-dependent manner. Analysis of secondary structure revealed that recombinant balsamin mainly consisted of α-helical and random coiled with minimal turns and ß-sheets. Recombinant balsamin was found to be stable in the temperature range of 20-60 °C and pH range of 6-9. Antimicrobial assays showed that the minimum inhibitory concentrations of recombinant balsamin for various pathogens ranged between 1.56 and 12.5 µg/ml. Heterologous expression and purification of balsamin carries great importance as it provides an alternative approach for large-scale preparation of biologically active recombinant balsamin, which is difficult from its natural source.


Assuntos
Momordica , Proteínas de Plantas , RNA Ribossômico/química , Proteínas Inativadoras de Ribossomos , Animais , Momordica/química , Momordica/genética , Proteínas de Plantas/biossíntese , Proteínas de Plantas/química , Proteínas de Plantas/genética , Estrutura Secundária de Proteína , Coelhos , Proteínas Recombinantes/biossíntese , Proteínas Recombinantes/química , Proteínas Recombinantes/genética , Proteínas Inativadoras de Ribossomos/biossíntese , Proteínas Inativadoras de Ribossomos/química , Proteínas Inativadoras de Ribossomos/genética
14.
PLoS One ; 12(9): e0185130, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28926628

RESUMO

Diabetes is an irreversible condition characterized by elevated blood glucose levels. Currently, there are no predictive biomarkers for this disease and the existing ones such as hemoglobin A1c and fasting blood glucose are used only when diabetes symptoms are noticed. The objective of this work was first to explore the potential of leucine and isoleucine amino acids as diabetes type 2 biomarkers using their Raman spectroscopic signatures. Secondly, we wanted to explore whether Raman spectroscopy can be applied in comparative efficacy studies between commercially available anti-diabetic drug pioglitazone and the locally used anti-diabetic herbal extract Momordica spinosa (Gilg.)Chiov. Sprague Dawley (SD) rat's blood was used and were pipetted onto Raman substrates prepared from conductive silver paste smeared glass slides. Prominent Raman bands associated with glucose (926, 1302, 1125 cm-1), leucine (1106, 1248, 1302, 1395 cm-1) and isolecucine (1108, 1248, 1437 and 1585 cm-1) were observed. The Raman bands centered at 1125 cm-1, 1395 cm-1 and 1437 cm-1 associated respectively to glucose, leucine and isoleucine were chosen as biomarker Raman peaks for diabetes type 2. These Raman bands displayed decreased intensities in blood from diabetic SD rats administered antidiabetic drugs pioglitazone and herbal extract Momordica spinosa (Gilg.)Chiov. The intensity decrease indicated reduced concentration levels of the respective biomarker molecules: glucose (1125 cm-1), leucine (1395 cm-1) and isoleucine (1437 cm-1) in blood. The results displayed the power and potential of Raman spectroscopy in rapid (10 seconds) diabetes and pre-diabetes screening in blood (human or rat's) with not only glucose acting as a biomarker but also leucine and isoleucine amino-acids where intensities of respectively assigned bands act as references. It also showed that using Raman spectroscopic signatures of the chosen biomarkers, the method can be an alternative for performing comparative efficacy studies between known and new anti-diabetic drugs. Reports on use of Raman spectroscopy in type 2 diabetes mellitus screening with Raman bands associated with leucine and isoleucine molecules acting as reference is rare in literature. The use of Raman spectroscopy in pre-diabetes screening of blood for changes in levels of leucine and isoleucine amino acids is particularly interesting as once elevated levels are noticed, necessary interventions to prevent diabetes development can be initiated.


Assuntos
Diabetes Mellitus Tipo 2/diagnóstico , Isoleucina/sangue , Leucina/sangue , Análise Espectral Raman , Animais , Biomarcadores/sangue , Glicemia/análise , Diabetes Mellitus Tipo 2/tratamento farmacológico , Diabetes Mellitus Tipo 2/veterinária , Hipoglicemiantes/química , Hipoglicemiantes/uso terapêutico , Isoleucina/química , Leucina/química , Momordica/química , Momordica/metabolismo , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Ratos , Ratos Sprague-Dawley
15.
Int. j. morphol ; 35(3): 992-999, Sept. 2017. ilus
Artigo em Inglês | LILACS | ID: biblio-893084

RESUMO

Valproic acid (VPA), an anti-epileptic drug, has been reported to cause male sub/infertility. Together with searching for alternative treatments, the degrees to which testosterone levels and sperm quality are decreased under VPA treatment also need to be clarified. This study aimed to investigate the protective effects of Momordica cochinchinensis (MC) aril extract containing antioxidant capacity on adverse reproductive parameters induced with VPA. Rats were divided into 6 groups (control, VPA, 200 mg kg-1 of MC only, 50, 100, 200 mg kg-1 MC+VPA, respectively, n=8 in each). Animals were pretreated with MC extract for 23 days before co-administration with VPA (500 mg kg-1, i.p.) for 10 consecutive days. All reproductive parameters including histology, and expression of androgen receptor (AR), Ki-67, tyrosine phosphorylated proteins, and steroidogenic proteins in testis were examined. The results showed that MC could prevent all reproductive parameters in VPA-treated rats. Moreover, MC+VPA groups showed significant declining of testicular histopathologies compared to VPA group. It also decreased the malondialdehyde level and changes of the testicular StAR, AR, and tyrosine phosphorylated protein expressions. In conclusion, M. cochinchinensis aril extract can prevent adverse male reproductive parameters and essential testicular proteins damages induced with VPA.


Se ha informado que el ácido valproico (VPA), un fármaco antiepiléptico, causa infertilidad masculina. Junto con la búsqueda de tratamientos alternativos, los grados a los que los niveles de testosterona y la calidad del esperma son disminuidos bajo el tratamiento de VPA también necesitan ser aclarados. El objetivo de este estudio fue investigar los efectos protectores del extracto aril de Momordica cochinchinensis (MC) que contiene capacidad antioxidante sobre parámetros reproductivos adversos inducidos con VPA. Las ratas se dividieron en 6 grupos (control, VPA, 200 mg kg-1 de MC solamente, 50, 100, 200 mg kg-1 de MC + VPA, respectivamente; n = 8 en cada uno). Los animales fueron pretratados con extracto de MC durante 23 días antes de la coadministración con VPA (500 mg kg-1, i.p.) durante 10 días consecutivos. Se examinaron todos los parámetros reproductivos, incluyendo la histología, y la expresión de receptor de andrógenos (AR), Ki-67, proteínas fosforiladas con tirosina y proteínas esteroidogénicas en los testículos. Los resultados mostraron que MC podría prevenir todos los parámetros reproductivos en las ratas tratadas con VPA. Además, los grupos MC + VPA mostraron una disminución significativa de las histopatologías testiculares en comparación con el grupo VPA. También disminuyó el nivel de malondialdehído y los cambios de las expresiones testiculares de las proteínas StAR, AR y tirosina fosforiladas. En conclusión, el extracto de aril de M. cochinchinensis puede prevenir los parámetros reproductivos masculinos adversos y los daños esenciales de proteínas testiculares inducidos con VPA.


Assuntos
Animais , Masculino , Ratos , Testículo/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Ácido Valproico/toxicidade , Momordica/química , Antioxidantes/administração & dosagem , Fosfoproteínas , Imuno-Histoquímica , Receptores Androgênicos/efeitos dos fármacos , Western Blotting , Ratos Wistar , Antígeno Ki-67
16.
Int. j. morphol ; 35(2): 667-675, June 2017. ilus
Artigo em Inglês | LILACS | ID: biblio-893038

RESUMO

The aim of present study was to investigate the effect of Momordica cochinchinensis (Gag) aril (GA) aqueous extract on male reproductive system of streptozotocin (STZ)-induced hyperglycemia (HG) mice. GA were extracted with distilled water (DW) and analyzed for in vitro antioxidant capacities. ICR male mice were divided into 7 groups: 1) control, 2) DW, 3) GA 1000 mg/kg BW, 4) HG, 5) HG + glibenclamide, 6 and 7) HG + GA 500 and 1000 mg/kg BW respectively (7 mice/ group). In HG groups, mice were induced by STZ at single dose (150 mg/kg BW). They were treated for consecutive 35 days. All groups were compared for blood glucose levels, weights and histopathologies of reproductive organs, sperm concentration including testicular tyrosine phosphorylation protein patterns by Immuno-Western blotting. The results showed that GA processed antioxidant activities and could significantly decrease blood glucose levels and increase sperm concentration in HG mice. Moreover, GA could change the density of a testicular 70 kDa protein in HG-GA groups. In conclusion, GA extract could improve hyperglycemia and male reproductive damages in STZ-induced HG mice.


El objetivo de este estudio fue investigar el efecto del extracto acuoso de Momordica cochinchinensis (Gag) aril (GA) en el sistema reproductor masculino de ratones hiperglucémicos inducidos por estreptozotocina (STZ). GA fue extraída con agua destilada (DW) y se analizaron las capacidades antioxidantes in vitro. Ratones ICR machos fueron divididos en 7 grupos: 1) control, 2) DW, 3) GA 1000 mg / kg PC, 4) HG, 5) HG + glibenclamida, 6 y 7) HG + GA 500 y 1000 mg / kg PC, respectivamente (7 ratones / grupo). En los grupos HG, los ratones fueron inducidos con STZ en dosis única (150 mg / kg BW). Fueron tratados durante 35 días consecutivos. En todos los grupos se compararon los niveles de glucosa en sangre, los pesos y las histopatologías de los órganos reproductores, la concentración de espermatozoides, incluídos los patrones testiculares de proteínas tirosina fosforilada por Inmuno-Western blot. Los resultados mostraron que GA procesaba actividades antioxidantes y podían disminuir significativamente los niveles de glucosa en sangre y aumentar la concentración de espermatozoides en ratones HG. Además, GA podría cambiar la densidad de una proteína testicular de 70 kDa en grupos HG-GA. En conclusión, el extracto de GA podría mejorar la hiperglucemia y los daños reproductivos masculinos inducidos por STZ en ratones HG.


Assuntos
Animais , Masculino , Camundongos , Doenças Testiculares/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Momordica/química , Hiperglicemia/tratamento farmacológico , Hipoglicemiantes/administração & dosagem , Antioxidantes/administração & dosagem , Fenóis/análise , Fosforilação/efeitos dos fármacos , Contagem de Espermatozoides , Espermatozoides/efeitos dos fármacos , Testículo/efeitos dos fármacos , Tirosina , Flavonoides/análise , Western Blotting , Diabetes Mellitus Experimental , Camundongos Endogâmicos ICR , Antioxidantes/química
17.
Am J Chin Med ; 45(3): 459-473, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28367713

RESUMO

Momordica cochinchinensis Spreng (family Cucurbitaceae), also known as gac, or red melon, is an edible Southeast Asian fruit valued for its nutritional and medicinal properties. Specifically, Momordicae Semen, the seeds of the gac fruit, is used in traditional Chinese medicine to treat boils, rheumatic pain, muscle spasm, hemorrhoids, and hemangiomas. In this study, a chemical investigation into a gac seed ethanol (EtOH) extract resulted in the identification of three triterpenoidal saponins (1-3), which were investigated for their anti-inflammatory effects. Among the saponins, momordica saponin I (compound 3) reduced the production of nitric oxide (NO) in LPS-activated RAW264.7 cells without inducing cytotoxicity. The mRNA levels of inducible NO synthase (iNOS) and cyclooxygenase (COX)-2 were decreased by momordica saponin I. Additionally, the translocation of p65 and p50 (subunits of the transcription factor NF-[Formula: see text]B) into the nucleus was remarkably inhibited. Furthermore, the phosphorylation levels of inflammatory signaling proteins (I[Formula: see text]B[Formula: see text], Src, and Syk) known to be upstream regulatory molecules of p65 were decreased under momordica saponin I-treated conditions. The molecular targets of momordica saponin I were confirmed in overexpression experiments and through immunoblot analyses with Src and Syk. This study provides evidence that momordica saponin I could be beneficial in treating inflammatory diseases, and should be considered a bioactive immunomodulatory agent with anti-inflammatory properties.


Assuntos
Anti-Inflamatórios/farmacologia , Momordica/química , Saponinas/farmacologia , Sementes/química , Quinase Syk/metabolismo , Triterpenos/farmacologia , Quinases da Família src/metabolismo , Animais , Núcleo Celular/metabolismo , Ciclo-Oxigenase 2/metabolismo , Camundongos , NF-kappa B/metabolismo , Proteínas de Neoplasias/metabolismo , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Proteínas de Transporte Nucleocitoplasmático/metabolismo , Fosforilação/efeitos dos fármacos , Células RAW 264.7 , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação
18.
Acta Biol Hung ; 68(1): 88-100, 2017 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-28322091

RESUMO

In vitro cell suspension culture was established for the production of commercially valuable phytochemicals in Momordica dioica. The influence of elicitors in jasmonic acid (JA) and salicylic acid (SA) increased their effect on phytochemical production and biomass accumulation in M. dioica. The results indicate that compared with non-elicited cultures, JA- and SA-elicited cell suspension cultures had significantly enhanced phenolic, flavonoid, and carotenoid production, as well as antioxidant, antimicrobial, and antiproliferative activities. Furthermore, elicited cultures produced 22 phenolic compounds, such as flavonols, hydroxycinnamic acids, and hydroxybenzoic acids. Greater biomass production, phytochemical accumulation, and biological activity occurred in JA- than in SA-elicited cell cultures. This study is the first to successfully establish M. dioica cell suspension cultures for the production of phenolic compounds and carotenoids, as well as for biomass accumulation.


Assuntos
Ciclopentanos/farmacologia , Momordica/efeitos dos fármacos , Oxilipinas/farmacologia , Compostos Fitoquímicos/metabolismo , Ácido Salicílico/farmacologia , Anti-Infecciosos/metabolismo , Anti-Infecciosos/farmacologia , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Biomassa , Carotenoides/metabolismo , Proliferação de Células/efeitos dos fármacos , Células Cultivadas , Cromatografia Líquida de Alta Pressão/métodos , Relação Dose-Resposta a Droga , Flavonoides/metabolismo , Fungos/efeitos dos fármacos , Fungos/crescimento & desenvolvimento , Células HT29 , Humanos , Células MCF-7 , Momordica/química , Momordica/citologia , Fenóis/metabolismo , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Reguladores de Crescimento de Planta/farmacologia , Fatores de Tempo
19.
J Sci Food Agric ; 97(5): 1656-1662, 2017 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-27435184

RESUMO

BACKGROUND: Gac fruit (Momordica cochinchinensis Spreng.) is a rich source of carotenoids for the manufacture of powder, oil and capsules for food, cosmetic and pharmaceutical uses. Currently, only the aril of the Gac fruit is processed and the peel, similar to the other components, is discarded, although it contains high level of carotenoids, which could be extracted for commercial use. In the present study, four different drying methods (hot-air, vacuum, heat pump and freeze drying), different temperatures and drying times were investigated for producing dried Gac peel suitable for carotenoid extraction. RESULTS: The drying methods and drying temperatures significantly affected the drying time, carotenoid content and antioxidant capacity of the dried Gac peel. Among the investigated drying methods, hot-air drying at 80 o C and vacuum drying at 50 o C produced dried Gac peel that exhibited the highest retention of carotenoids and the strongest antioxidant capacity. CONCLUSION: Hot-air drying at 80 o C and vacuum drying at 50 o C are recommended for the drying of Gac peel. © 2016 Society of Chemical Industry.


Assuntos
Antioxidantes/análise , Carotenoides/análise , Dessecação/métodos , Momordica/química , Frutas/química , Temperatura Alta
20.
Sci Rep ; 6: 35347, 2016 10 13.
Artigo em Inglês | MEDLINE | ID: mdl-27734947

RESUMO

Peptide analogues derived from bioactive hormones such as somatostatin or certain growth factors have great potential as angiogenesis inhibitors for cancer applications. In an attempt to combat emerging drug resistance many FDA-approved anti-angiogenesis therapies are co-administered with cytotoxic drugs as a combination therapy to target multiple signaling pathways of cancers. However, cancer therapies often encounter limiting factors such as high toxicities and side effects. Here, we combined two anti-angiogenic epitopes that act on different pathways of angiogenesis into a single non-toxic cyclic peptide framework, namely MCoTI-II (Momordica cochinchinensis trypsin inhibitor-II), and subsequently assessed the anti-angiogenic activity of the novel compound. We hypothesized that the combination of these two epitopes would elicit a synergistic effect by targeting different angiogenesis pathways and result in improved potency, compared to that of a single epitope. This novel approach has resulted in the development of a potent, non-toxic, stable and cyclic analogue with nanomolar potency inhibition in in vitro endothelial cell migration and in vivo chorioallantoic membrane angiogenesis assays. This is the first report to use the MCoTI-II framework to develop a 2-in-1 anti-angiogenic peptide, which has the potential to be used as a form of combination therapy for targeting a wide range of cancers.


Assuntos
Inibidores da Angiogênese/química , Ciclotídeos/química , Epitopos/química , Momordica/química , Neoplasias/tratamento farmacológico , Peptídeos Cíclicos/farmacologia , Animais , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Membrana Corioalantoide/química , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Eritrócitos/citologia , Hemólise , Células Endoteliais da Veia Umbilical Humana , Humanos , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Meliteno/química , Neovascularização Patológica , Codorniz , Transdução de Sinais/efeitos dos fármacos , Tripsina/química
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