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1.
J Ovarian Res ; 14(1): 126, 2021 Sep 27.
Artigo em Inglês | MEDLINE | ID: mdl-34579761

RESUMO

BACKGROUND: Infections by the SARS-CoV-2 virus causing COVID-19 are presently a global emergency. The current vaccination effort may reduce the infection rate, but strain variants are emerging under selection pressure. Thus, there is an urgent need to find drugs that treat COVID-19 and save human lives. Hence, in this study, we identified phytoconstituents of an edible vegetable, Bitter melon (Momordica charantia), that affect the SARS-CoV-2 spike protein. METHODS: Components of Momordica charantia were tested to identify the compounds that bind to the SARS-CoV-2 spike protein. An MTiOpenScreen web-server was used to perform docking studies. The Lipinski rule was utilized to evaluate potential interactions between the drug and other target molecules. PyMol and Schrodinger software were used to identify the hydrophilic and hydrophobic interactions. Surface plasmon resonance (SPR) was employed to assess the interaction between an extract component (erythrodiol) and the spike protein. RESULTS: Our in-silico evaluations showed that phytoconstituents of Momordica charantia have a low binding energy range, -5.82 to -5.97 kcal/mol. A docking study revealed two sets of phytoconstituents that bind at the S1 and S2 domains of SARS-CoV-2. SPR showed that erythrodiol has a strong binding affinity (KD = 1.15 µM) with the S2 spike protein of SARS-CoV-2. Overall, docking, ADME properties, and SPR displayed strong interactions between phytoconstituents and the active site of the SARS-CoV-2 spike protein. CONCLUSION: This study reveals that phytoconstituents from bitter melon are potential agents to treat SARS-CoV-2 viral infections due to their binding to spike proteins S1 and S2.


Assuntos
COVID-19/tratamento farmacológico , Momordica charantia/química , Extratos Vegetais/farmacologia , Glicoproteína da Espícula de Coronavírus/genética , Sítios de Ligação/efeitos dos fármacos , COVID-19/genética , COVID-19/virologia , Humanos , Interações Hidrofóbicas e Hidrofílicas/efeitos dos fármacos , Simulação de Acoplamento Molecular , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/química , Ácido Oleanólico/farmacologia , Extratos Vegetais/química , Ligação Proteica/efeitos dos fármacos , SARS-CoV-2/efeitos dos fármacos , SARS-CoV-2/patogenicidade , Glicoproteína da Espícula de Coronavírus/antagonistas & inibidores , Ressonância de Plasmônio de Superfície
2.
Nutrients ; 13(7)2021 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-34371875

RESUMO

Polycyclic aromatic hydrocarbons (PAHs) have been recognized to cause neurobehavioral dysfunctions and disorder of cognition and behavioral patterns in childhood. Momordica charantia L. (MC) has been widely known for its nutraceutical and health-promoting properties. To date, the effect of MC for the prevention and handling of PAHs-induced neurotoxicity has not been reported. In the current study, the neuroprotective effects of MC and its underlying mechanisms were investigated in mouse hippocampal neuronal cell line (HT22); moreover, in silico analysis was performed with the phytochemicals MC to decipher their potential function as neuroprotectants. MC was demonstrated to possess neuroprotective effect by reducing reactive oxygen species' (ROS') production and down-regulating cyclin D1, p53, and p38 mitogen-activated protein kinase (MAPK) protein expressions, resulting in the inhibition of cell apoptosis and the normalization of cell cycle progression. Additionally, 28 phytochemicals of MC and their competence on inhibiting cytochrome P450 (CYP: CYP1A1, CYP1A2, and CYP1B1) functions were resolved. In silico analysis of vitamin E and stigmasterol revealed that their binding to either CYP1A1 or CYP1A2 was more efficient than the binding of each positive control (alizarin or purpurin). Together, MC is potentially an interesting neuroprotectant including vitamin E and stigmasterol as probable active components for the prevention for PAHs-induced neurotoxicity.


Assuntos
Hipocampo/efeitos dos fármacos , Momordica charantia , Neurônios/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Extratos Vegetais/farmacologia , Hidrocarbonetos Policíclicos Aromáticos/toxicidade , Estigmasterol/farmacologia , Vitamina E/farmacologia , Animais , Apoptose/efeitos dos fármacos , Proteínas Reguladoras de Apoptose/metabolismo , Ciclo Celular/efeitos dos fármacos , Proteínas de Ciclo Celular/metabolismo , Linhagem Celular , Citocromo P-450 CYP1A1/metabolismo , Citocromo P-450 CYP1A2/metabolismo , Hipocampo/metabolismo , Hipocampo/patologia , Camundongos , Momordica charantia/química , Neurônios/metabolismo , Neurônios/patologia , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/isolamento & purificação , Ligação Proteica , Espécies Reativas de Oxigênio/metabolismo , Estigmasterol/isolamento & purificação , Vitamina E/isolamento & purificação
3.
Molecules ; 26(15)2021 Jul 23.
Artigo em Inglês | MEDLINE | ID: mdl-34361596

RESUMO

The bitter melon, Momordica charantia L., was once an important food and medicinal herb. Various studies have focused on the potential treatment of stomach disease with M. charantia and on its anti-diabetic properties. However, very little is known about the specific compounds responsible for its anti-inflammatory activities. In addition, the in vitro inhibitory effect of M. charantia on pro-inflammatory cytokine production by lipopolysaccharide (LPS)-stimulated bone marrow-derived dendritic cells (BMDCs) has not been reported. Phytochemical investigation of M. charantia fruit led to the isolation of 15 compounds (1-15). Their chemical structures were elucidated spectroscopically (one- and two-dimensional nuclear magnetic resonance) and with electrospray ionization mass spectrometry. The anti-inflammatory effects of the isolated compounds were evaluated by measuring the production of the pro-inflammatory cytokines interleukin IL-6, IL-12 p40, and tumor necrosis factor α (TNF-α) in LPS-stimulated BMDCs. The cucurbitanes were potent inhibitors of the cytokines TNF-α, IL-6, and IL-12 p40, indicating promising anti-inflammatory effects. Based on these studies and in silico simulations, we determined that the ligand likely docked in the receptors. These results suggest that cucurbitanes from M. charantia are potential candidates for treating inflammatory diseases.


Assuntos
Células da Medula Óssea/efeitos dos fármacos , Células Dendríticas/efeitos dos fármacos , Frutas/química , Momordica charantia/química , Triterpenos/farmacologia , Animais , Células Cultivadas , Citocinas/metabolismo , Camundongos , Camundongos Endogâmicos C57BL
4.
J Genet ; 1002021.
Artigo em Inglês | MEDLINE | ID: mdl-34282734

RESUMO

Mutants with unique characters have played a key role in discovery of gene, mapping, functional genomics and breeding in many vegetable crops, but information on bitter gourd is lacking. Induction of mutation by gamma rays (Co60 source) at five different doses (50 Gy, 100 Gy, 150 Gy, 200 Gy and 250 Gy) was studied in four widely divergent bitter gourd genotypes BG-1346501, Meghna-2, Special Boulder and Selection-1 in M1 generation. Reduction in seed germination percentage, vine length and pollen fertility occurred in M1 generation with the increasing doses of mutagens. LD50 dose for BG-1346501, Meghna-2, Special Boulder and Selection-1 corresponded to 290.76 Gy, 206.12 Gy, 212.81 Gy and 213.49 Gy ᵞ radiation, respectively suggested low to medium doses (200-250 Gy) of gamma rays would be helpful in producing useful and exploitable mutants for further breeding. No remarkable effect of ᵞ radiation on fruit physicochemical characters in M1 generation were observed. M2 generation, raised from two widely divergent genotypes, BG-1346501 and Meghna-2, were screened critically and observed no significant reduction in seed germination and pollen viability, however little damage occurred particularly in vine length. There is possibility of isolating segregates in M2 generation with enhanced nutrient contents at low radiation dose. Highest mutation frequency resulted by treating Meghna-2 at 200 Gy and BG-1346501 at 100 Gy. Both genotype and mutagenic doses influenced mutagenic effectiveness. Spectrum of mutation was very low; number of putative mutants isolated from M2 generation was five in Meghna-2 and three in BG-1346501. Among six putative macro mutants isolated from M3 generation, we could identify two putative mutants, namely Meghna-2 with gynoecious sex form and BG-1346501 with high charantin, appreciable ß-carotene and high ascorbic acid contents having ample promise for further utilization in bitter gourd breeding after critical testing in subsequent generations for estimation of genetic gain and trait heritability to confirm the mutant stability.


Assuntos
Momordica charantia/genética , Mutagênese/genética , Melhoramento Vegetal/economia , Locos de Características Quantitativas/genética , Frutas/economia , Frutas/genética , Frutas/crescimento & desenvolvimento , Raios gama , Genótipo , Germinação/efeitos da radiação , Humanos , Momordica charantia/crescimento & desenvolvimento , Momordica charantia/efeitos da radiação , Mutagênese/efeitos da radiação , Mutação/efeitos da radiação , Locos de Características Quantitativas/efeitos da radiação
5.
Medicine (Baltimore) ; 100(27): e26606, 2021 Jul 09.
Artigo em Inglês | MEDLINE | ID: mdl-34232214

RESUMO

RATIONALE: Momordica charantia is often used to treat type 2 diabetes mellitus in Korea. Drug-induced acute interstitial nephritis (AIN) accounts for 60% to 70% of AIN cases. However, only 1 case of AIN associated with ingesting M charantia has been reported in the English literature. We report an extremely rare case of AIN that occurred after a patient ingested a pure M charantia extract over 7 months. PATIENT CONCERNS: A 60-year-old Korean woman was admitted to our hospital for a renal biopsy. Her renal function had decreased gradually over the last 9 months without symptoms or signs. DIAGNOSIS: Her blood urea nitrogen and serum creatinine levels were 29.7 mg/dL (range: 8.0-20.0 mg/dL) and 1.45 mg/dL (range: 0.51-0.95 mg/dL) on admission. Renal histology indicated AIN; there was immune cell infiltration into the interstitium, tubulitis, and epithelial casts, although the glomeruli were largely intact. INTERVENTIONS: M charantia was discontinued and prednisolone was prescribed. OUTCOMES: The value of serum creatinine has almost been restored to the baseline level after 3 months. CONCLUSION: s: This is the first case report of AIN associated with the ingestion of a pure M charantia extract. Recognition of the possible adverse effects of these agents by physicians is very important for early diagnosis and appropriate management.


Assuntos
Momordica charantia/efeitos adversos , Nefrite Intersticial/induzido quimicamente , Biópsia , Ingestão de Alimentos , Feminino , Humanos , Rim/diagnóstico por imagem , Rim/efeitos dos fármacos , Pessoa de Meia-Idade , Nefrite Intersticial/diagnóstico , Extratos Vegetais/efeitos adversos , Ultrassonografia
6.
Artigo em Inglês | MEDLINE | ID: mdl-34073706

RESUMO

This study investigated the effects of Momordica charantia (M. charantia) extract in obesity and abnormal lipid metabolism in mice fed high fat diet (HFD). Fruit, root, stem, and leaf extracts of M. charantia were obtained using distilled water, 70% ethanol and 95% hexane. M. charantia leaf distilled water extract (MCLW) showed the highest antioxidant activity in both 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity tests and reducing power. Metabolite profiles of M. charantia leaf extracts were analyzed for identification of bioactive compounds. HFD-fed mice were treated with MCLW (oral dose of 200 mg/kg/d) for 4 weeks. MCLW reduced lipid accumulation, body weight, organ weight, and adipose tissue volume and significantly improved glucose tolerance and insulin resistance in HFD mice. Furthermore, MCLW administration reduced serum total cholesterol and low-density lipoprotein cholesterol, and increased serum high-density lipoprotein cholesterol compared with HFD mice. Moreover, MCLW significantly reduced the levels of serum urea nitrogen, alanine aminotransferase, alkaline phosphatase, and aspartate aminotransferase; alleviated liver and kidney injury. MCLW decreases expression of genes that fatty acid synthesis; increase the expression of catabolic-related genes. These results indicate that MCLW has an inhibitory effect on obese induced by high fat diet intake, and the mechanism may be related to the regulation of abnormal lipid metabolism in liver and adipose tissue, suggesting that MCLW may be a suitable candidate for the treatment of obesity.


Assuntos
Momordica charantia , Animais , Dieta Hiperlipídica/efeitos adversos , Metabolismo dos Lipídeos , Fígado/metabolismo , Camundongos , Camundongos Endogâmicos C57BL , Obesidade/tratamento farmacológico , Obesidade/metabolismo , Extratos Vegetais/metabolismo , Extratos Vegetais/farmacologia
7.
J Food Sci ; 86(7): 3109-3121, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34146408

RESUMO

Inhibition of α-glucosidase can slow carbohydrate metabolism, which is known as an effective strategy for diabetes treatment. The aim of this study is to evaluate the effect of thermal treatment (50, 60, and 70℃) for 15 days on the α-glucosidase inhibitory activity of bitter melon. The results show that the bitter melon heated at 70℃ for 12 days had the best α-glucosidase inhibitory effect. However, the amount of free polyphenols, 5-hydroxymethyl-2-furfural (5-HMF), and the browning degree of bitter melon generally increased with the time (15 days) and temperature of the thermal treatment, which is positively related to their antioxidant and α-glucosidase inhibitory activities. In conclusion, aged bitter melon shows great α-glucosidase inhibitory activity, which may be related to the increased free form of the involved phenolic compounds and Maillard reaction products. This suggests that thermal processing may be a good way to enhance the application of bitter melon for diabetes treatment. PRACTICAL APPLICATION: The thermal processing of bitter melon provides an application for diabetes treatment. This study demonstrated that heat-treated bitter melon can lower the blood glucose level; therefore, it can be used as a potential anti-hyperglycemic and functional food.


Assuntos
Antioxidantes/farmacologia , Produtos Finais de Glicação Avançada/metabolismo , Temperatura Alta , Momordica charantia/química , Fenóis/metabolismo , Extratos Vegetais/farmacologia , alfa-Glucosidases/farmacologia , Antioxidantes/química , Produtos Finais de Glicação Avançada/análise , Fenóis/análise , Extratos Vegetais/química , alfa-Glucosidases/química
8.
Environ Res ; 198: 111279, 2021 07.
Artigo em Inglês | MEDLINE | ID: mdl-33961826

RESUMO

p-Aminoazobenzene (pAAB) is a hazardous azo dye that causes considerable harm to human health and the environment. The development of novel and sensitive sensors for the rapid detection of pAAB is in high demand. In this study, a simple fluorescent sensor for pAAB detection is designed based on carbon dots (CDs) which are prepared using green carbon source of Momordica charantia L. via a facile hydrothermal approach. The fluorescence spectra of CDs exhibit considerable overlap with the absorption band of pAAB, and the fluorescence is specifically suppressed in the presence of pAAB ascribed to the inner filter effect. Good and wide linearity is observed in the pAAB concentration range of 0.01-12.5 µg mL-1 with a lower detection limit of 3.9 ng mL-1. The established method achieves good results with a rapid analysis of pAAB in different practical water and soil samples. The as-constructed fluorescent sensor provides a simple, rapid, economical and eco-friendly platform and possesses prospective applications for the effective, selective and sensitive detection of pAAB in the environmental field.


Assuntos
Momordica charantia , Pontos Quânticos , Carbono , Corantes Fluorescentes , Humanos , Estudos Prospectivos , p-Aminoazobenzeno
9.
J Food Biochem ; 45(5): e13683, 2021 05.
Artigo em Inglês | MEDLINE | ID: mdl-33844303

RESUMO

Liver cancer is one of the leading causes of cancer-related deaths in the world. Bitter melon seed (BMS) is well known for anti-inflammatory and anticancer properties. MicroRNA-421 (miR-421) is considered as a regulator of cancer initiation, tumor metastasis, and progression, interfering with transcription of the mRNAs responsible for the cancer pathogenesis. HepG2 cells were treated with BMS water extract (BMSW) for 24 hr, and the IC50 was 586.27 ± 0.07 µg/ml. The ROS, mitochondrial membrane potential, the protein expression, and the nuclear fragmentation after the treatment of BMSW were respectively detected. The increase of ROS resulted in the decrease of mitochondrial membrane potential, which induced the apoptosis of cells subsequently. BMSW inhibited the proliferation of HepG2 cells by blocking cell cycle in the S phase and influenced the nuclei and the expression of protein, leading to cellular laxity and apoptosis. The expression level of miR-421 in HepG2 was distinctly down-regulated by 13.74 fold with 600 µg/ml of BMSW. Comprehensive microarray and RT-PCR analysis identified six putative target genes of miR-421 (GADD45B, DUSP6, DUSP3, DUSP10, CASP3, and CAPN2). The relationships of DUSP6, CASP3, and miR-421 were further confirmed by miR-421 mimics/inhibitor transfection by RT-PCR and western blot. The CASP3 was identified as target gene of miR-421. BMSW induced the apoptosis of HepG2 cell by regulating miR-421 and CASP3. PRACTICAL APPLICATIONS: Hepatocellular carcinoma (HCC) is a malignant tumour with the fourth highest mortality rate in the world. Bitter melon seed (BMS) as edible and medical food has significant anticancer activity. Our study indicated the anticancer mechanisms of BMS and provided the scientific basis for the application of BMS in healthy or novel functional foods. BMS can be used as dietary supplements or nutritional fortifiers to improve the survival status of patients with liver cancer due to safety and effectiveness.


Assuntos
Carcinoma Hepatocelular , Neoplasias Hepáticas , MicroRNAs , Momordica charantia , Apoptose , Carcinoma Hepatocelular/tratamento farmacológico , Carcinoma Hepatocelular/genética , Proliferação de Células , Fosfatases de Especificidade Dupla , Regulação Neoplásica da Expressão Gênica , Células Hep G2 , Humanos , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/genética , Fosfatases da Proteína Quinase Ativada por Mitógeno
10.
Biomolecules ; 11(5)2021 04 28.
Artigo em Inglês | MEDLINE | ID: mdl-33924809

RESUMO

Ascorbic acid is an organic compound with antioxidant properties that can protect the human body from the threat of free radicals. Therefore, it is important to detect the existence and measure the concentration of ascorbic acid to regulate its content in the human body. In this work, we prepared bitter gourd polysaccharide (BGP)-stabilized platinum nanoclusters (Pt-BGP NCs) by reacting BGP with K2PtCl4. Pt-BGP NCs and catalyzed the decomposition of H2O2 to generate •OH radicals, which could oxidize TMB to form oxidized TMB (oxTMB), indicating their peroxidase-like properties. The kinetics followed the Michaelis-Menten equation. Furthermore, the colorimetric detection of ascorbic acid using Pt-BGP NCs showed high selectivity and a low detection limit of 0.191 µM. The accuracy of real sample detection using Pt-BGP NCs was as high as 98.9%. More importantly, Pt-BGP NCs had high cell biocompatibility and extremely low hemolysis rate due to the component of BGP. In summary, the prepared Pt-BGP NCs with reductive activity and good biocompatibility have good application prospects in colorimetric detection of ascorbic acid.


Assuntos
Ácido Ascórbico/análise , Momordica charantia/química , Nanoestruturas/química , Ácido Ascórbico/química , Catálise , Colorimetria/métodos , Corantes/química , Radicais Livres/química , Peróxido de Hidrogênio , Indicadores e Reagentes/química , Cinética , Limite de Detecção , Nanopartículas Metálicas/química , Momordica charantia/metabolismo , Oxirredução , Oxirredutases , Tamanho da Partícula , Peroxidases , Platina/química , Polissacarídeos/química
11.
Braz J Biol ; 82: e236498, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33787746

RESUMO

Mormodica charantia (Curcubitaceae) is a plant with great medicinal potential, also used as an alternative of mosquitoes control as demonstrated by previous studies. We evaluated the larvicidal activity of crude extracts of ethyl acetate, methanol and hexane from flowers and fruits of M. charantia against Aedes aegypti (Culicidae). Flowers and fruits were macerated in methanol, ethyl acetate and hexane. Bioassays were performed with application of the extracts at final concentrations of 1 - 200 µg/mL in the middle of the third instar larvae of A. aegypti (L3). The results showed high toxicity to ethyl acetate extracts from flowers and fruits at concentrations of 200 µg/mL and 100 µg/mL, with 97% and 87% of larvae mortality (L3), respectively. Hexane extract demonstrated low toxicity, while methanol extract exhibited 78% larval mortality. The data suggested that the ethyl acetate extracts of flowers and fruits of M. charantia can effectively contribute to larvicidal activity. In addition, purification of M. charantia extracts may lead to a promising larvicidal activity to control the A. aegypti population.


Assuntos
Aedes , Inseticidas , Momordica charantia , Animais , Inseticidas/farmacologia , Larva , Extratos Vegetais/farmacologia , Folhas de Planta
12.
BMC Genomics ; 22(1): 190, 2021 Mar 16.
Artigo em Inglês | MEDLINE | ID: mdl-33726664

RESUMO

BACKGROUND: The preferred choice for molecular marker development is identifying existing variation in populations through DNA sequencing. With the genome resources currently available for bitter gourd (Momordica charantia), it is now possible to detect genome-wide insertion-deletion (InDel) polymorphisms among bitter gourd populations, which guides the efficient development of InDel markers. RESULTS: Here, using bioinformatics technology, we detected 389,487 InDels from 61 Chinese bitter gourd accessions with an average density of approximately 1298 InDels/Mb. Then we developed a total of 2502 unique InDel primer pairs with a polymorphism information content (PIC) ≥0.6 distributed across the whole genome. Amplification of InDels in two bitter gourd lines '47-2-1-1-3' and '04-17,' indicated that the InDel markers were reliable and accurate. To highlight their utilization, the InDel markers were employed to construct a genetic map using 113 '47-2-1-1-3' × '04-17' F2 individuals. This InDel genetic map of bitter gourd consisted of 164 new InDel markers distributed on 15 linkage groups with a coverage of approximately half of the genome. CONCLUSIONS: This is the first report on the development of genome-wide InDel markers for bitter gourd. The validation of the amplification and genetic map construction suggests that these unique InDel markers may enhance the efficiency of genetic studies and marker-assisted selection for bitter gourd.


Assuntos
Momordica charantia , Ligação Genética , Genoma , Humanos , Mutação INDEL , Momordica charantia/genética , Análise de Sequência de DNA
13.
Biomed Res Int ; 2021: 5550180, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33763471

RESUMO

Diabetes mellitus is the most common chronic disorder and leading cause of renal, neurological, and gastrointestinal manifestations in developed and developing countries. Despite of many drugs and combinational therapies, the complications of diabetes are still listed due to severe consequences of those drugs. In past few years, plant-derived drugs draw special attention due to their higher efficacy and fewer side-effects. Momordica charantia also known as bitter melon is referred as an antidiabetic and hypoglycemic plant in native populations of Asia and East Africa. In current study, an in silico approach was used to evaluate the interactions and binding patterns of plant-derived peptides devised from a hypoglycemic protein adMc1 of M. charantia as potential inhibitor of DPP-IV, SGLT1, and GLUT2 receptor proteins. The study has described a novel approach to investigate hypoglycemic peptides to cure diabetes. A total of eighty tetra-, penta-, and hexapeptides were devised from conserved regions of adMc1 homologs. The molecular docking approach using MOE software was employed to reveal inhibiting potentials of devised peptides against three selected proteins. Out of 30 shortlisted ligands six peptides (i.e. SMCG, DECC, TTIT, RTTI, ARNL and TVEV) accomplished the criteria of being good drug candidates against selected receptor proteins following the drugability assessment test. The overall results are acceptable on the basis of ADMET profiling for being good drug candidates against selected proteins.


Assuntos
Dipeptidil Peptidase 4/química , Inibidores da Dipeptidil Peptidase IV/química , Transportador de Glucose Tipo 2 , Hipoglicemiantes/química , Momordica charantia/química , Peptídeos/química , Proteínas de Plantas/química , Transportador 1 de Glucose-Sódio , Diabetes Mellitus Tipo 2/tratamento farmacológico , Diabetes Mellitus Tipo 2/metabolismo , Inibidores da Dipeptidil Peptidase IV/uso terapêutico , Transportador de Glucose Tipo 2/antagonistas & inibidores , Transportador de Glucose Tipo 2/química , Humanos , Hipoglicemiantes/uso terapêutico , Peptídeos/uso terapêutico , Transportador 1 de Glucose-Sódio/antagonistas & inibidores , Transportador 1 de Glucose-Sódio/química
14.
Molecules ; 26(4)2021 Feb 16.
Artigo em Inglês | MEDLINE | ID: mdl-33669312

RESUMO

Diabetes mellitus is a chronic disease and one of the fastest-growing health challenges of the last decades. Studies have shown that chronic low-grade inflammation and activation of the innate immune system are intimately involved in type 2 diabetes pathogenesis. Momordica charantia L. fruits are used in traditional medicine to manage diabetes. Herein, we report the purification of a new 23-O-ß-d-allopyranosyl-5ß,19-epoxycucurbitane-6,24-diene triterpene (charantoside XV, 6) along with 25ξ-isopropenylchole-5(6)-ene-3-O-ß-d-glucopyranoside (1), karaviloside VI (2), karaviloside VIII (3), momordicoside L (4), momordicoside A (5) and kuguaglycoside C (7) from an Indian cultivar of Momordica charantia. At 50 µM compounds, 2-6 differentially affected the expression of pro-inflammatory markers IL-6, TNF-α, and iNOS, and mitochondrial marker COX-2. Compounds tested for the inhibition of α-amylase and α-glucosidase enzymes at 0.87 mM and 1.33 mM, respectively. Compounds showed similar α-amylase inhibitory activity than acarbose (0.13 mM) of control (68.0-76.6%). Karaviloside VIII (56.5%) was the most active compound in the α-glucosidase assay, followed by karaviloside VI (40.3%), while momordicoside L (23.7%), A (33.5%), and charantoside XV (23.9%) were the least active compounds. To better understand the mode of binding of cucurbitane-triterpenes to these enzymes, in silico docking of the isolated compounds was evaluated with α-amylase and α-glucosidase.


Assuntos
Anti-Inflamatórios/farmacologia , Simulação por Computador , Frutas/química , Glicosídeos/química , Glicosídeos/farmacologia , Hipoglicemiantes/farmacologia , Momordica charantia/química , Triterpenos/química , Triterpenos/farmacologia , Animais , Anti-Inflamatórios/química , Bioensaio , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Glicosídeos/isolamento & purificação , Hipoglicemiantes/química , Ligantes , Camundongos , Conformação Molecular , Simulação de Acoplamento Molecular , Espectroscopia de Prótons por Ressonância Magnética , Células RAW 264.7 , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Triterpenos/isolamento & purificação , alfa-Amilases/química , alfa-Amilases/metabolismo , alfa-Glucosidases/química , alfa-Glucosidases/metabolismo
15.
Food Funct ; 12(6): 2617-2630, 2021 Mar 21.
Artigo em Inglês | MEDLINE | ID: mdl-33634806

RESUMO

Obesity is a chronic disease characterized by overweight resulting from fat accumulation, along with disturbance of metabolism and gut microbiota. Fermentation, as a green processing method, is beneficial for improving the nutrition capacity of food components. Polysaccharides are considered as one of the important components in food and are also potential supplements for anti-obesity treatment. This study aimed to investigate the anti-obesity effects of polysaccharides from fermented and non-fermented Momordica charantia L. with Lactobacillus plantarum NCU116 (FP and NFP) on obese rats by serum metabolomics and gut microbiota analysis. Metabolomics results revealed that abnormal lipid metabolism was formed due to obesity. The supplement of FP and NFP improved the glycerophospholipids, glycosphingolipids, and amino acid metabolism of the obese rats, which alleviated the hypercholesterolemia and overweight in rats. Furthermore, the disorder of gut microbiota was ameliorated by FP and NFP. FP promoted the growth of beneficial bacteria, such as phylum Firmicutes, Actinobacteria, and genera Anaerostipes, Coprococcus, Lactobacillus, and Bifidobacterium. FP also reduced several harmful bacteria belonging to the phylum Proteobacteria and genera Helicobacter. The positive correlation of the weight loss and lowering of serum lipids with the increased beneficial bacteria further elucidated that the anti-obesity effect of FP in obese rats is associated with the regulation of gut microbiota and serum metabolites. The results of this study could provide information for developing probiotic products in the future that may have beneficial effects on the prevention or treatment of obesity.


Assuntos
Microbioma Gastrointestinal/efeitos dos fármacos , Lactobacillus plantarum , Momordica charantia/química , Polissacarídeos/farmacologia , Probióticos/farmacologia , Animais , Peso Corporal/efeitos dos fármacos , Fermentação , Lipídeos/sangue , Masculino , Doenças Metabólicas/metabolismo , Metaboloma/efeitos dos fármacos , Obesidade , Extratos Vegetais/farmacologia , Ratos , Ratos Sprague-Dawley
16.
Chem Phys Lipids ; 235: 105057, 2021 03.
Artigo em Inglês | MEDLINE | ID: mdl-33515592

RESUMO

A close link between cardiovascular diseases and cancer results from sharing the same modifiable risk factors (e.g. nutritional) and cardiotoxicity of anti-cancerous therapies. It justifies cardio-oncological preliminary studies on dietary factors, especially on those of possible anti-carcinogenic or cardioprotective properties. The main purpose was to evaluate the effect of pomegranate seed oil (PSO) and/or bitter melon extract (BME) supplementation of the diet of female rats suffering from mammary tumors on lipidomic profile (expressed as fatty acids, conjugated fatty acids (CFA), malondialdehyde (MDA), cholesterol and oxysterols content) of cardiac tissue. Total lipidomic profile and intensity of lipid peroxidation in hearts of DMBA-treated Sprague-Dawley rats and their healthy equivalents, both obtaining diet supplementation, were evaluated with different chromatographic techniques coupled with appropriate detection systems (GC-MS, GC-TOFMS, Ag+-HPLC-DAD, UF-HPLC-DAD). Dietary modifications neither diminished breast cancer incidence nor exerted explicit cardio-protective influence, however, they diminished cholesterol content, i.a. because of inhibition of the endogenous conversion of squalene to cholesterol in cardiac tissue. CFA were incorporated into cardiac tissue to a lesser extent in the cancerous process. PSO and BME anti-oxidant properties in pathological condition were only slightly reflected in MDA levels but not in oxysterols formation. Obtained results indicate considerable changes in dietary supplements' biological activity in pathological conditions and the need for clear distinction of drugs and dietary supplements, which is of utmost importance, especially for cancer survivors.


Assuntos
Anticarcinógenos/farmacologia , Neoplasias da Mama/tratamento farmacológico , Cardiotônicos/farmacologia , Doenças Cardiovasculares/tratamento farmacológico , Oxisteróis/metabolismo , Extratos Vegetais/farmacologia , Óleos Vegetais/farmacologia , Animais , Anticarcinógenos/administração & dosagem , Anticarcinógenos/química , Neoplasias da Mama/metabolismo , Cardiotônicos/administração & dosagem , Cardiotônicos/química , Doenças Cardiovasculares/metabolismo , Suplementos Nutricionais , Modelos Animais de Doenças , Feminino , Peroxidação de Lipídeos/efeitos dos fármacos , Lipidômica , Momordica charantia/química , Miocárdio/metabolismo , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Óleos Vegetais/administração & dosagem , Óleos Vegetais/química , Romã (Fruta)/química , Ratos , Ratos Sprague-Dawley
17.
Sci Rep ; 11(1): 2101, 2021 01 22.
Artigo em Inglês | MEDLINE | ID: mdl-33483556

RESUMO

The toxicity of seven biorational insecticides [five insect growth regulators (Buprofezin, Fenoxycarb, Pyriproxyfen, Methoxyfenozide, and Tebufenozide) and two oil-extracts of neem and bitter gourd seeds] against Bemisia tabaci and their selectivity for its parasitoid, Encarsia formosa were evaluated in laboratory and field conditions for 2 years (2018-2019) in Pakistan. Toxicity results demonstrate that Pyriproxyfen, Buprofezin, and Fenoxycarb proved to be effective (80-91% mortality and 66.3-84.2% population-reduction) against B. tabaci followed by Methoxyfenozide, Tebufenozide (50-75% mortality and 47.8-52.4% population-reduction), and then oil-extracts of neem and bitter gourd (25-50% mortality and 36.5-39.8% population-reduction) in the laboratory [72 h post-application exposure interval (PAEI)] and field trails (168 h PAEI), respectively. All tested biorationals, except Methoxyfenozide [(slightly-harmful/Class-II), i.e., causing mortality of parasitoids between a range of 25-50%] and Tebufenozide [(moderately-harmful/Class-III), i.e., causing mortality of parasitoids between the ranges of 51-75%], proved harmless/Class-I biorationals at PAEI of 7-days in the field (parasitism-reduction < 25%) and 3-days in the lab (effect < 30%). In laboratory bioassays, exposure of parasitized-pseudopupae and adult-parasitoids to neem and bitter gourd oils demonstrated that these compounds proved harmless/Class-I biorationals (< 30% mortality). Alternatively, Pyriproxyfen, Buprofezin, Fenoxycarb, Methoxyfenozide, and Tebufenozide were slightly-harmful biorationals (30-79% mortality) against the respective stages of E. formosa. We conclude that most of the tested biorationals proved harmless or slightly harmful to E. formosa, except tebufenozide after PAEI of 7-days (168 h) in the field and, therefore, may be used strategically in Integrated Pest Management (IPM) of B. tabaci.


Assuntos
Gossypium/parasitologia , Hemípteros/fisiologia , Inseticidas/toxicidade , Controle Biológico de Vetores/métodos , Vespas/fisiologia , Animais , Azadirachta/química , Gossypium/genética , Interações Hospedeiro-Parasita/efeitos dos fármacos , Hidrazinas/toxicidade , Hormônios Juvenis/toxicidade , Larva/efeitos dos fármacos , Larva/fisiologia , Momordica charantia/química , Fenilcarbamatos/toxicidade , Extratos Vegetais/toxicidade , Plantas Geneticamente Modificadas , Piridinas/toxicidade , Tiadiazinas/toxicidade , Resultado do Tratamento
18.
J Agric Food Chem ; 69(6): 1816-1830, 2021 Feb 17.
Artigo em Inglês | MEDLINE | ID: mdl-33406828

RESUMO

Qualitative analysis of cucurbitane-type triterpenoids of bitter melon (fruit of Momordica charantia L.) using ultraperformance liquid chromatography quadrupole time-of-flight mass spectrometry revealed 27 promising cucurbitane-type triterpenoids, and LC/MS-guided chemical analysis of M. charantia fruit extract led to the isolation and structural characterization of 22 cucurbitane-type triterpenoids (1-22), including 8 new cucurbitane-type triterpenoidal saponins, yeojoosides A-H (1-8). The structures of the new compounds (1-8) were elucidated by spectroscopic methods, including 1D and 2D NMR and high-resolution electrospray ionization mass spectrometry. Their absolute configurations were assigned by quantum chemical electronic circular dichroism calculations, chemical reactions, and DP4+ analysis using gauge-including atomic orbital NMR chemical shift calculations. All isolated compounds (1-22) were examined for inhibitory activity against protein tyrosine phosphatases relevant to insulin resistance. Nine compounds (7, 8, 9, 11, 14, 15, 19, 20, and 21) showed selective inhibitory effects of over 70% against PTPN2. The present results suggested that these compounds would be potential antidiabetic agents.


Assuntos
Resistência à Insulina , Momordica charantia , Triterpenos , Frutas/química , Cromatografia Gasosa-Espectrometria de Massas , Glicosídeos , Proteínas Tirosina Fosfatases , Triterpenos/análise , Triterpenos/farmacologia
19.
Molecules ; 26(3)2021 Jan 22.
Artigo em Inglês | MEDLINE | ID: mdl-33499307

RESUMO

Cutibacterium acnes (formerly Propionibacterium acnes) is one of the major bacterial species responsible for acne vulgaris. Numerous bioactive compounds from Momordica charantia Linn. var. abbreviata Ser. have been isolated and examined for many years. In this study, we evaluated the suppressive effect of two cucurbitane-type triterpenoids, 5ß,19-epoxycucurbita-6,23-dien-3ß,19,25-triol (Kuguacin R; KR) and 3ß,7ß,25-trihydroxycucurbita-5,23-dien-19-al (TCD) on live C. acnes-stimulated in vitro and in vivo inflammatory responses. Using human THP-1 monocytes, KR or TCD suppressed C. acnes-induced production of interleukin (IL)-1ß, IL-6 and IL-8 at least above 56% or 45%, as well as gene expression of these three pro-inflammatory cytokines. However, a significantly strong inhibitory effect on production and expression of tumor necrosis factor (TNF)-α was not observed. Both cucurbitanes inhibited C. acnes-induced activation of the myeloid differentiation primary response 88 (MyD88) (up to 62%) and mitogen-activated protein kinases (MAPK) (at least 36%). Furthermore, TCD suppressed the expression of pro-caspase-1 and cleaved caspase-1 (p10). In a separate study, KR or TCD decreased C. acnes-stimulated mouse ear edema by ear thickness (20% or 14%), and reduced IL-1ß-expressing leukocytes and neutrophils in mouse ears. We demonstrated that KR and TCD are potential anti-inflammatory agents for modulating C. acnes-induced inflammation in vitro and in vivo.


Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Cucurbitacinas/química , Cucurbitacinas/farmacologia , Inflamação/tratamento farmacológico , Momordica charantia/química , Triterpenos/química , Triterpenos/farmacologia , Acne Vulgar/tratamento farmacológico , Acne Vulgar/imunologia , Acne Vulgar/microbiologia , Animais , Citocinas/biossíntese , Citocinas/genética , Modelos Animais de Doenças , Glicosídeos/química , Glicosídeos/farmacologia , Infecções por Bactérias Gram-Positivas/tratamento farmacológico , Infecções por Bactérias Gram-Positivas/imunologia , Infecções por Bactérias Gram-Positivas/microbiologia , Humanos , Inflamação/imunologia , Inflamação/microbiologia , Masculino , Camundongos , Camundongos Endogâmicos ICR , Monócitos/efeitos dos fármacos , Monócitos/imunologia , Monócitos/metabolismo , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Propionibacteriaceae/patogenicidade , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Células THP-1
20.
Phytother Res ; 35(2): 637-656, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-32929814

RESUMO

Type 2 diabetes mellitus is a chronic hyperglycemic condition due to progressively impaired glucose regulation. Momordica charantia L. could potentially improve hyperglycemia because its fruit extracts can alleviate insulin resistance, beta-cell dysfunction, and increase serum insulin level. We evaluated the effect of M. charantia L. in comparison with a vehicle on glycemic control in animal models of type 2 diabetes mellitus. MEDLINE, Web of Science, Scopus, and CINAHL databases were searched without language restriction through April 2019. About 66 studies involving 1861 animals that examined the effect of M. charantia L. on type 2 diabetes mellitus were included. Fruits and seed extracts reduced fasting plasma glucose (FPG) and glycosylated hemoglobin A1c in comparison to vehicle control: (42 studies, 815 animals; SMD, -6.86 [95% CI; -7.95, -5.77], 3 studies, 59 animals; SMD; -7.76 [95% CI; -12.50, -3.01]) respectively. Also, the extracts have hepato-renal protective effects at varying doses and duration of administration. Despite the observed significant glycemic control effect, poor methodological quality calls for future researches to focus on standardizing extract based on chemical markers and adopt measures to improve the quality of preclinical studies such as sample size calculation, randomization, and blinding.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Momordica charantia , Extratos Vegetais/uso terapêutico , Animais , Fitoterapia
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