RESUMO
Momordica cymbalaria Hook F. (MC), belonging to the family Cucurbitaceae, is a plant with several biological activities. This detailed, comprehensive review gathers and presents all the information related to the geographical distribution, morphology, therapeutic uses, nutritional values, pharmacognostic characters, phytochemicals, and pharmacological activities of MC. The available literature showed that MC fruits are utilized as a stimulant, tonic, laxative, stomachic, and to combat inflammatory disorders. The fruits are used to treat spleen and liver diseases and are applied in folk medicine to induce abortion and treat diabetes mellitus. The phytochemical screening studies report that MC fruits contain tannins, alkaloids, phenols, proteins, amino acids, vitamin C, carbohydrates, ß-carotenes, palmitic acid, oleic acid, stearic acid, α-eleostearic acid, and γ-linolenic acid. The fruits also contain calcium, sodium, iron, potassium, copper, manganese, zinc, and phosphorus. Notably, momordicosides are cucurbitacin triterpenoids reported in the fruits of MC. Diverse pharmacological activities of MC, such as analgesic, anti-inflammatory, antioxidant, hepatoprotective, nephroprotective, antidiabetic, cardioprotective, antidepressant, anticonvulsant, anticancer, antiangiogenic, antifertility, antiulcer, antimicrobial, antidiarrheal and anthelmintic, have been reported by many investigators. M. cymbalaria methanolic extract is safe up to 2,000 mg/kg. Furthermore, no symptoms of toxicity were found. These pharmacological activities are mechanistically interpreted and described in this review. Additionally, the microscopic, powder and physiochemical characteristics of MC tubers are also highlighted. In summary, possesses remarkable medicinal values, which warrant further detailed studies to exploit its potential benefits therapeutically.
Assuntos
Cucurbitaceae , Momordica , Feminino , Gravidez , Humanos , Compostos Fitoquímicos/farmacologia , Cafeína , VitaminasRESUMO
Prolonged exposure to high energy diets has been implicated in the development of pre-diabetes, a long-lasting condition that precedes type 2 diabetes mellitus (T2DM). A combination of pharmacological treatment and dietary interventions are recommended to prevent the progression of pre-diabetes to T2DM. However, poor patient compliance leads to negligence of the dietary intervention and thus reduced drug efficiency. Momordica balsamina (MB) has been reported to possess anti-diabetic effects in type 1 diabetic rats. However, the effects of this medicinal plant in conjunction with dietary intervention on pre-diabetes have not yet been established. Consequently, this study sought to evaluate the effects of MB on glucose homeostasis in a diet-induced pre-diabetes rat model in the presence and absence of dietary intervention. Pre-diabetes was induced on male Sprague Dawley rats by a high fat high carbohydrate (HFHC) diet for a period of 20 weeks. Pre-diabetic male Sprague Dawley rats were treated with MB (250 mg/kg p.o.) in both the presence and absence of dietary intervention once a day every third day for a period of 12 weeks. The administration of MB with and without dietary intervention resulted in significantly improved glucose homeostasis through reduced caloric intake, body weights, with reduced plasma ghrelin concentration and glycated hemoglobin by comparison to the pre-diabetic control. MB administration also improved insulin sensitivity as evidenced by the expression of glucose transporter 4 (GLUT 4) and glycogen synthase on the prediabetic treated animals. These results suggest that MB has the potential to be used to manage pre-diabetes and prevent the progression to overt type 2 diabetes as it demonstrated the ability to restore glucose homeostasis even in the absence of dietary and lifestyle intervention.
Assuntos
Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2 , Momordica , Estado Pré-Diabético , Humanos , Ratos , Animais , Glucose/metabolismo , Ratos Sprague-Dawley , Momordica/metabolismo , Diabetes Mellitus Experimental/tratamento farmacológico , Dieta Hiperlipídica , Insulina/uso terapêutico , Glicemia/metabolismoRESUMO
SUMMARY: Mormodica balsamina is a valuable medicinal plant that is used to treat wounds and inflammation; its leaves are also used as an antibiotic and in the treatment of stomach pain. This study was conducted to determine the anti-ulcer activity of methanolic leaf extract of Mormodica balsamina on ethanol-induced ulcer in albino rats. A total of 32 rats were used for the study. Groups I and II served as the baseline and negative controls respectively, while groups III-VII served as the test groups. Group I was untreated, while group II received 1ml/kg body weight of the vehicle (2 % DMSO). Three test groups (III - V) received methanol extracts (75 mg, 150 mg, 300 mg/kg body weight respectively) while the other three test groups (VI - VIII) received aqueous extracts (75 mg, 150mg, 300 mg/kg body weight respectively) via oral gavage for seven days prior to ulcer induction. The rats were sacrificed, stomachs excised and ulcers scored. Histological sections were produced and examined. Findings revealed that M. balsamina extracts protected the rats' gastric epithelia from ethanol induced ulceration to varying degree with the high dose (150 and 300 mg/kg) of both extracts offering the best preservation (42 % and 50 % ulcer protective index respectively) when compared to untreated animals. Histological findings correlated with calculated ulcer indices, with treated animals having less severe gastric mucosal lesions. In conclusion, extracts of M. balsamina may possess reasonable antiulcer activities in rats against ethanol induced gastric ulcer.
Mormodica balsamina es una valiosa planta medicinal que se utiliza para tratar heridas e inflamaciones; sus hojas también se utilizan como antibiótico y en el tratamiento del dolor de estómago. Este estudio se realizó para determinar la actividad antiulcerosa del extracto metanólico de hojas de Mormodica balsamina sobre la úlcera inducida por etanol en ratas albinas. Se utilizaron un total de 32 ratas para el estudio. Los grupos I y II sirvieron como referencia y controles negativos respectivamente, mientras que los grupos III-VII sirvieron como grupos de prueba. El grupo I no se trató, mientras que el grupo II recibió 1 ml/kg de peso corporal del vehículo (2% de DMSO). Tres grupos de prueba (III - V) recibieron extractos de metanol (75 mg, 150 mg, 300 mg/ kg de peso corporal respectivamente) mientras que los otros tres grupos de prueba (VI - VIII) recibieron extractos acuosos (75 mg, 150 mg, 300 mg/kg de peso corporal respectivamente) por sonda oral durante siete días antes de la inducción de la úlcera. Se sacrificaron las ratas, se extirparon los estómagos y se puntuaron las úlceras. Se realizaron y examinaron secciones histológicas. Los resultados revelaron que los extractos de M. balsamina protegieron el epitelio gástrico de las ratas de la ulceración inducida por etanol en diversos grados, y la dosis alta (150 y 300 mg/kg) de ambos extractos ofreció la mejor conservación (42 % y 50 % de índice de protección contra úlceras, respectivamente) en comparación con los animales no tratados. Los hallazgos histológicos se correlacionaron con los índices de úlcera calculados, y los animales tratados tenían lesiones de la mucosa gástrica menos graves. En extractos de M. balsamina puede poseer actividades antiulcerosas razonables en ratas contra la úlcera gástrica inducida por etanol.
Assuntos
Animais , Ratos , Úlcera Gástrica/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Momordica/química , Etanol/toxicidade , Antiulcerosos/administração & dosagem , Plantas Medicinais , Úlcera Gástrica/induzido quimicamente , Extratos Vegetais/química , Momordica balsamica , Folhas de Planta , Modelos Animais de Doenças , Mucosa Gástrica/efeitos dos fármacos , Antiulcerosos/químicaRESUMO
BACKGROUND: Plants are used in traditional healing practices of many cultures worldwide. Momordica balsamina is a plant commonly used by traditional African healers as a part of a treatment for HIV/AIDS. It is typically given as a tea to patients with HIV/AIDS. Water-soluble extracts of this plant were found to contain anti-HIV activity. METHODS: We employed cell-based infectivity assays, surface plasmon resonance, and a molecular-cell model of the gp120-CD4 interaction to study the mechanism of action of the MoMo30-plant protein. Using Edman degradation results of the 15 N-terminal amino acids, we determined the gene sequence of the MoMo30-plant protein from an RNAseq library from total RNA extracted from Momordica balsamina. RESULTS: Here, we identify the active ingredient of water extracts of the leaves of Momordica balsamina as a 30 kDa protein we call MoMo30-plant. We have identified the gene for MoMo30 and found it is homologous to a group of plant lectins known as Hevamine A-like proteins. MoMo30-plant is distinct from other proteins previously reported agents from the Momordica species, such as ribosome-inactivating proteins such as MAP30 and Balsamin. MoMo30-plant binds to gp120 through its glycan groups and functions as a lectin or carbohydrate-binding agent (CBA). It inhibits HIV-1 at nanomolar levels and has minimal cellular toxicity at inhibitory levels. CONCLUSIONS: CBAs like MoMo30 can bind to glycans on the surface of the enveloped glycoprotein of HIV (gp120) and block entry. Exposure to CBAs has two effects on the virus. First, it blocks infection of susceptible cells. Secondly, MoMo30 drives the selection of viruses with altered glycosylation patterns, potentially altering their immunogenicity. Such an agent could represent a change in the treatment strategy for HIV/AIDS that allows a rapid reduction in viral loads while selecting for an underglycosylated virus, potentially facilitating the host immune response.
Assuntos
Síndrome da Imunodeficiência Adquirida , HIV-1 , Momordica , Plantas Medicinais , Humanos , HIV-1/genética , Momordica/química , Momordica/metabolismo , Proteínas de Plantas/metabolismo , Proteína gp120 do Envelope de HIV/genética , Proteína gp120 do Envelope de HIV/metabolismo , Proteína gp120 do Envelope de HIV/farmacologiaRESUMO
Our lab investigates the anti-HIV-1 activity in Momordica balsamina (M. balsamina) leaf extract. Traditional Senegalese healers have used M. balsamina leaf extract as a part of a plant-based treatment for HIV/AIDS infections. Our overall goal is to define and validate the scientific basis for using M. balsamina leaf extract as a part of the traditional Senegalese treatment. As an initial characterization of this extract, we used activity-guided fractionation to determine the active ingredient's solubility and relative size. We found that M. balsamina leaf extract inhibits HIV-1 infection by >50% at concentrations of 0.02 mg/mL and above and is not toxic over its inhibitory range (0-0.5 mg/mL). We observed significantly more antiviral activity in direct water and acetonitrile extractions (p ≤ 0.05). We also observed significantly more antiviral activity in the aqueous phases of ethyl acetate, chloroform, and diethyl ether extractions (p ≤ 0.05). Though most of the antiviral activity partitioned into the aqueous layers, some antiviral activity was present in the organic layers. We show that the active agent in the plant extracts is at least 30 kD in size. Significantly more antiviral activity was retained in 3, 10, and 30 kD molecular weight cutoff filters (p ≤ 0.05). In contrast, most of the antiviral activity passed through the 100 kD filter (p ≤ 0.05). Because the active anti-HIV-1 agent presented as a large, amphiphilic molecule we ran the purified extract on an SDS-page gel. We show that the anti-HIV-1 activity in the leaf extracts is attributed to a 30 kDa protein we call MoMo30. This article describes how MoMo30 was determined to be responsible for its anti-HIV-1 activity.
Assuntos
Infecções por HIV , Soropositividade para HIV , HIV-1 , Momordica , Extratos Vegetais/farmacologia , Infecções por HIV/tratamento farmacológico , AntiviraisRESUMO
Diabetes mellitus is a typical life threatening of disease, which generate due to the dysfunction of ß cells of pancreas. In 2014, WHO stated that 422â million people were infected with DM. The current pattern of management of diabetes included synthetic or plant based oral hypoglycemic drugs and insulin but drug resentence is become a very big issues in antidiabetic therapy. Thus, it's very earnest to discover now medication for this disease. Now the days, it is well acknowledged that diabetic patients are more prone towards covid and related complications. Thus, medical practitioners reformed the methodology of prescribing medication for covid infected antidiabetic therapy and encouraging the medication contains dual pharmacological properties. It is also well know that polyphenols specifically hold a significant role in oxidative stress and reduced the severity of many inflammatory diseases. Cucumis melo has rich history as ethano-pharmacological use in Indian subcontinent. The fruit and seed are well-known for the treatment of various diseases due to the presence of phenolics. Therefore, in this study, the combined mixture of flower and seeds were used for the extraction of polyphenolic rich extract and tested for antidiabetic activity through the antioxidant and inâ vivo experiments. The antioxidant potential measurement exhibited that the selected plant extract has the significant competence to down-regulate oxidative stress (DPPH scavenging IC50 at 60.7±1.05â µg/mL, ABTS IC50 at 62.15±0.50â µg/mL). Furthermore, the major polyphenolic phyto-compounds derived from the Cucumis melo were used for inâ silico anticovid activity, docking, and complementarity studies. The anticovid activity prognosis reflected that selected phyto-compounds amentoflavone and vanillic acid have optimal possibility to interact with 3C-like protease and through this moderate anticovid activity can be exhibit. The docking experiments established that the selected compounds have propensity to interact with protein tyrosine phosphatase 1B, 11ß-Hydroxysteroid dehydrogenase, superoxide dismutase, glutathione peroxidase, and catalase ß-glucuronidase receptor. Inâ vivo experiments showed that 500â mg/kg, Cucumis melo extract ominously amplified body weight, plasma insulin, high-density lipoprotein levels, and biochemical markers. Furthermore, extract significantly downregulate the blood glucose, total cholesterol, triglycerides, low-density lipoprotein, and very low-density lipoprotein.
Assuntos
COVID-19 , Cucumis melo , Diabetes Mellitus Experimental , Momordica , 11-beta-Hidroxiesteroide Desidrogenases , Animais , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Biomarcadores , Glicemia , Catalase/metabolismo , Colesterol , Cucumis melo/metabolismo , Diabetes Mellitus Experimental/metabolismo , Glucuronidase , Glutationa Peroxidase/metabolismo , Humanos , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Insulina , Lipoproteínas HDL/uso terapêutico , Lipoproteínas LDL/uso terapêutico , Momordica/metabolismo , Peptídeo Hidrolases , Extratos Vegetais/química , Proteína Tirosina Fosfatase não Receptora Tipo 1 , Superóxido Dismutase/metabolismo , Triglicerídeos , Ácido VanílicoRESUMO
Aiming at overcoming multidrug resistance (MDR) in cancer, we have been studying Momordica balsamina, a vegetable known as African pumpkin. Five undescribed cucurbitane-type triterpenoids (balsaminaepoxide, balsaminatriol, balsaminoic acid, balsaminal, and balsaminol G) along with five known cucurbitacins were isolated from the methanol extract of Momordica balsamina aerial parts, whose structures were elucidated by spectroscopic data, mainly 1D and 2D NMR experiments. Compounds were evaluated for their ability as P-glycoprotein (P-gp/ABCB1) inhibitors in multidrug resistant human ABCB1-transfected mouse lymphoma cells (L5178Y, MDR) and resistant human colon adenocarcinoma cells (COLO 320), using the rhodamine-123 exclusion test, by flow cytometry. Several compounds, which were found to be non-cytotoxic, strongly inhibited P-gp efflux activity in a dose-dependent manner in both cell models. In MRD mouse lymphoma cells, balsaminol G and karavilagenin B were the most active, while in resistant colon adenocarcinoma cells, the strongest inhibitory activity was found for balsaminaepoxide, balsaminatriol and karavilagenin C, being several-fold more active than the positive control verapamil. In chemosensitivity assays, in a model of combination chemotherapy, selected compounds showed to interact synergistically with doxorubicin, thus substantiating their potential as MDR reversers. The strongest synergistic interaction was found for balsaminal and balsaminol G.
Assuntos
Adenocarcinoma , Neoplasias do Colo , Cucurbita , Linfoma , Momordica , Triterpenos , Subfamília B de Transportador de Cassetes de Ligação de ATP , Animais , Linhagem Celular Tumoral , Neoplasias do Colo/tratamento farmacológico , Cucurbitacinas , Doxorrubicina/farmacologia , Resistencia a Medicamentos Antineoplásicos , Humanos , Metanol , Camundongos , Momordica/química , Extratos Vegetais/farmacologia , Rodaminas , Triterpenos/química , Triterpenos/farmacologia , VerapamilRESUMO
Natural compounds have been recognized as valuable sources for anticancer drug development. In this work, different parts from Momordica cochinchinensis Spreng were selected to perform cytotoxic screening against human prostate cancer (PC-3) cells. Chromatographic separation and purification were performed for the main constituents of the most effective extract. The content of the fatty acids was determined by Gas Chromatography-Flame Ionization Detector (GC-FID). Chemical structural elucidation was performed by spectroscopic means. For the mechanism of the apoptotic induction of the most effective extract, the characteristics were evaluated by Hoechst 33342 staining, sub-G1 peak analysis, JC-1 staining, and Western blotting. As a result, extracts from different parts of M. cochinchinensis significantly inhibited cancer cell viability. The most effective stem extract induced apoptosis in PC-3 cells by causing nuclear fragmentation, increasing the sub-G1 peak, and changing the mitochondrial membrane potential. Additionally, the stem extract increased the pro-apoptotic (caspase-3 and Noxa) mediators while decreasing the anti-apoptotic (Bcl-xL and Mcl-1) mediators. The main constituents of the stem extract are α-spinasterol and ligballinol, as well as some fatty acids. Our results demonstrated that the stem extract of M. cochinchinensis has cytotoxic and apoptotic effects in PC-3 cells. These results provide basic knowledge for developing antiproliferative agents for prostate cancer in the future.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , Momordica/química , Extratos Vegetais/farmacologia , Caules de Planta/química , Antineoplásicos Fitogênicos/química , Apoptose/genética , Biomarcadores Tumorais , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Humanos , Modelos Moleculares , Estrutura Molecular , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Relação Estrutura-AtividadeRESUMO
Targeting Bcr-Abl is the key to the treatment of chronic myeloid leukemia. Despite great progress in the treatment of patients with chronic CML, advanced CML patients are still unable to obtain effective and safe drugs. Momordica cochinchinensis seed is the dried ripe seed of Momordica cochinchinensis, which is a kind of fruit and consumed for dietary as well as medicinal uses. This study aimed to investigate the anticancer activity of Momordica cochinchinensis seed extract (MCSE) in CML cells. CML cells (KBM5 and KBM5-T315I) were treated with MCSE and analyzed for growth, apoptosis, and signal transduction. Nude mouse xenograft model was used to evaluate the antitumor activity of MCSE In Vivo. MCSE significantly reduced the cell viability of CML cells, triggered G0/G1 phase arrest in KBM5 cells and S phase arrest in KBM5-T315I cells. Concurrently, MCSE caused the activation of caspase-3, -8, -9, PARP and the degradation of Mcl-1, ultimately triggering endogenous and exogenous cell apoptosis. Meanwhile, MCSE downregulated Bcr-Abl levels and its downstream signaling pathways. Additionally, MCSE inhibited the growth of CML cells in nude mouse xenografts. Taken together, this study demonstrated the anticancer mechanism of MCSE, namely blocking Bcr-Abl and downregulating Mcl-1, and finally induced apoptosis of CML cells.
Assuntos
Antineoplásicos , Leucemia Mielogênica Crônica BCR-ABL Positiva , Momordica , Animais , Antineoplásicos/farmacologia , Apoptose , Linhagem Celular Tumoral , Proliferação de Células , Resistencia a Medicamentos Antineoplásicos , Proteínas de Fusão bcr-abl , Humanos , Mesilato de Imatinib/farmacologia , Mesilato de Imatinib/uso terapêutico , Leucemia Mielogênica Crônica BCR-ABL Positiva/patologia , Camundongos , Momordica/metabolismo , Proteína de Sequência 1 de Leucemia de Células Mieloides , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ensaios Antitumorais Modelo de XenoenxertoRESUMO
BACKGROUND: Non-small cell lung cancer (NSCLC) is a major subtype of lung cancer with a higher mortality rate. Both apoptosis and autophagy are crucial processes in the pathophysiology of NSCLC. Muyin extract (MSE) is a combination of Momordica cochinchinensis (Lour.) Spreng seeds and Epimedium brevicornu Maxim extract, with an optimal ratio of 1:1. Our previous research has firstly shown that MSE exerts a good anti-tumor activity, especially for NSCLC. PURPOSE: This study aims to evaluate the inhibitory effect of MSE on NSCLC and explore the underlying mechanism. METHODS: In vitro, cell proliferation was examined by MTT and colony formation. Apoptosis was detected by annexin V-FITC/PI assay while autophagy was assessed by Acridine orange (AO) and Monodansylcadaverine (MDC) staining. In vivo, Lewis lung cancer cell transplanted mice model was established to measure the effect of MSE on tumor growth. Hematoxylin eosin (H & E) staining was used to observe the pathological changes of the tumor after MSE treatment. The apoptosis in tumor tissue was detected by TUNEL assay. Meanwhile, the cellular proliferation marker Ki67 and autophagy marker LC3â ¡ were observed by immunohistochemistry staining. The IL-4 and IFN-γ concentrations in blood were tested by Elisa. The apoptosis related factors (Bcl-2, Bax Caspase-3, cleaved Caspase-3, Caspase-9 and p53), autophagy marker proteins (Atg-5, Becline-1, LC3â ¡/â and p62) as well as Akt/mTOR pathway were detected by western blotting. RESULTS: Present study showed that MSE greatly inhibited the proliferation of NSCLC in vitro and in vivo, together with apoptotic rate increasing. P53 and cleaved Caspase-3 levels were up-regulated while Bcl-2/Bax ratio, Caspase-3 and Caspase-9 levels were significantly down-regulated treated with MSE. Meanwhile, MSE activated autophagy, Atg-5, Becline-1 as well as the ratio of LC3â ¡/â were notably up-regulated while p62 was down-regulated after MSE treatment. Importantly, MSE significantly blocked Akt/mTOR pathway, which is a common upstream signal triggered by autophagy and apoptosis. Furthermore, when co-treated with specific autophagy inhibitor, the inhibitory rate and anti-apoptotic Bcl-2 level were significantly reversed. Impressively, MSE remarkably increased IFN-γ/ IL-4 ratio while VP16 did not in animal model, and the inhibition rate in tumor weight after MSE treatment was higher than xiaojin pill. CONCLUSION: Taken together, it is proved that MSE may be a promising oral TCM candidate for NSCLC therapy with immunity improvement. The underlying mechanisms could be associated with the induction of apoptosis and autophagy through blocking Akt/mTOR pathway, meanwhile, it may promote crosstalk between autophagy and apoptosis.
Assuntos
Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Animais , Apoptose , Autofagia , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Linhagem Celular Tumoral , Epimedium/química , Neoplasias Pulmonares/tratamento farmacológico , Camundongos , Momordica/química , Extratos Vegetais/farmacologia , Proteínas Proto-Oncogênicas c-akt/metabolismo , Transdução de SinaisRESUMO
Abstract The purpose of this research was to develop a hydrogel containing the extract of Gac fruit (Momordica cochinchinensis Spreng) with appropriate physicochemical properties and good dermatological efficacy. The Gac aril fruit was extracted by maceration in dichloromethane, and its antioxidant activity was determined through a DPPH assay. The very low water-solubility of the Gac extract is responsible for its incompatibility with the hydrogel. To overcome this drawback, LabrafacTM PG and Tween 60 were used to develop the hydrogel due to their potent potential for solubilizing the Gac extract. The prepared hydrogels displayed good physical properties, a homogenous orange gel, appropriate pH, and viscosity. After storage in an accelerated condition for six months, the hydrogels of the Gac extract had physical stability and high remaining amounts of beta-carotene and lycopene within the range of 90.25 - 94.61%. The skin efficacy of hydrogel containing the Gac fruit extract was found using 14 healthy female volunteers over a 30-day period of daily application. Topical application of the hydrogel containing the Gac fruit extract, which contains antioxidants, significantly moisturizes the skin and enhanced its elasticity (p ≤ 0.05; ANOVA). This makes it suitable for use as a skin care product
Assuntos
Humanos , Feminino , Adulto , Extratos Vegetais/efeitos adversos , Eficácia , Hidrogéis/análise , Frutas/efeitos adversos , Pele , Análise de Variância , Higiene da Pele , Momordica , Antioxidantes/farmacologiaRESUMO
Whitening research is of particular interest in the cosmetics market. The main focus of whitening research is on melanogenesis inhibition through tyrosinase activity. The mechanism of melanogenesis is involved with tyrosinase activity and p-PKC signaling. In this study, we used Momordica cochinchinensis (Lour.) spreng, a tropical fruit found throughout Southeast Asia, to investigate the inhibitory effect of melanogenesis. M. cochinchinensis contains a high concentration of polyphenols, flavonoids, and unsaturated fatty acids, which might be related to antioxidant activity. This study aimed to determine whether M. cochinchinensis extracts inhibit melanin synthesis in melan-A cells by inhibiting tyrosinase activity and p-PKC signaling. M. cochinchinensis was divided into pulp and aril and extracted under various conditions, and it was confirmed that all pulp and aril extracts have high contents of both phenols and flavonoids. Melan-A cells were treated with PMA for three days to induce melanin synthesis. After PMA treatment, M. cochinchinensis extracts were added to cultured media in a dose-dependent manner. Melanin contents and MTS were used to determine the amount of melanin in live cells. M. cochinchinensis extracts were evaluated for their effects on tyrosinase activity and p-PKC signaling pathways by Western blotting. It was found that M. cochinchinensis extract treatment decreased the amount of melanin and suppressed p-PKC expression. Additionally, tyrosinase activity was reduced after M. cochinchinensis extract treatment in a dose-dependent manner. Therefore, it was concluded that M. cochinchinensis could be used in antimelanogenesis and functional cosmetic materials to improve whitening.
Assuntos
Antioxidantes/farmacologia , Melaninas/biossíntese , Momordica , Monofenol Mono-Oxigenase/antagonistas & inibidores , Extratos Vegetais/farmacologia , Transdução de Sinais/efeitos dos fármacos , Flavonoides/farmacologia , Humanos , Fenóis/farmacologiaRESUMO
The African pumpkin (Momordica balsamina) contains bioactive phenolic compounds that may assist in reducing oxidative stress in the human body. The leaves are mainly consumed after boiling in water for a specific time; this hydrothermal process and conditions of the gastrointestinal tract may affect the presence and bioactivity of phenolics either positively or negatively. In this study, the effects of hydrothermal processing (boiling) and in vitro simulated human digestion on the phenolic composition, bioaccessibility and bioactivity in African pumpkin were investigated in comparison with those of spinach (Spinacia oleracea). A high-resolution ultra-performance liquid chromatography, coupled with diode array detection, quadrupole time-of-flight and mass spectrometer (UPLC-DAD-QTOF-MS) was used to profile phenolic metabolites. Metabolites such as 3-caffeoylquinic acid, 5-caffeoylquinic acid, 3,4-dicaffeoylquinic acid, 3,5-dicaffeoylquinic acid and 4,5-dicaffeoylquinic acid were highly concentrated in the boiled vegetable extracts compared to the raw undigested and all digested samples. The majority of African pumpkin and spinach extracts (non-digested and digested) protected Deoxyribonucleic acid (DNA), (mouse fibroblast) L929 and human epithelial colorectal adenocarcinoma (Caco-2) cells from 2,2'-Azobis(2-methylpropionamidine) dihydrochloride (AAPH)-induced oxidative damage. From these results, the consumption of boiled African pumpkin leaves, as well as spinach, could be encouraged, as bioactive metabolites present may reduce oxidative stress in the body.
Assuntos
Cucurbita/química , Digestão/efeitos dos fármacos , Momordica/química , Fenóis/química , Fenóis/farmacologia , Folhas de Planta/química , Animais , Antioxidantes/química , Células CACO-2 , Linhagem Celular Tumoral , Flavonoides/química , Humanos , Camundongos , Oxirredução/efeitos dos fármacos , Extratos Vegetais/química , Polifenóis/química , Ácido Quínico/análogos & derivados , Ácido Quínico/química , Spinacia oleracea/química , Verduras/químicaRESUMO
PURPOSE: To determine the prevalence of crude herbs' use in the self-management of hypertension and the health-related quality of life (HRQOL) in patients with hypertension. METHODS: This cross-sectional study was performed among patients with hypertension attending a government health clinic. Socio-demographic characteristics, lifestyle modifications, medical history and predictors of crude herbs users were obtained. The diversity of crude herbs used was assessed using a modified international complementary and alternative medicine questionnaire (I-CAM-Q) and the HRQOL was assessed using the SF36 instrument. RESULTS: Out of the 294 patients recruited, 52.4% were female, 41.5% were Malay and 38.8% were within the 60 to69 age category. The prevalence of crude herbs users was 30.6% and the most common herbs used were pegaga (Centella asiatica), peria (Momordica charantia) and betik (Carica papaya). Using the regression analysis, significantly higher odds of using crude herbs are noted among Malay or Indian patients who have these characteristics: attained secondary education, experienced falls or muscle pain, and had systolic blood pressure of more than 140 mmHg. There was no significant difference in HRQOL domains between the crude herb users and non-users (p>0.05). CONCLUSION: Besides taking allopathic medications, certain patients with hypertension use crude herbs as a form of self-management. Although patients are adamant about integrating crude herbs as a form of self-management, the effects of doing so have not been properly investigated. This implies that the healthcare staff members need to communicate with the patients regarding the use of crude herbs together with conventional drugs.
Assuntos
Hipertensão/psicologia , Hipertensão/terapia , Preparações de Plantas/uso terapêutico , Qualidade de Vida , Autogestão , Idoso , Carica , Centella , Estudos Transversais , Feminino , Humanos , Hipertensão/epidemiologia , Estilo de Vida , Malásia/epidemiologia , Malásia/etnologia , Masculino , Pessoa de Meia-Idade , Momordica , Prevalência , Atenção Primária à Saúde/organização & administração , Análise de Regressão , População Suburbana , Inquéritos e QuestionáriosRESUMO
Plant-derived compounds and/or extracts have proven to be beneficial for the treatment of a broad spectrum of cancers with minimal side effects. In this study, we investigated whether a crude acetone extract of Momordica balsamina (MBE) can interfere with the metastatic ability of HT-29 colorectal cancer (CRC) cells. The phytochemical composition of MBE was determined by ultra-performance liquid chromatography and cytotoxic effects by the MTT and acridine orange/ethidium bromide staining assays. The effect of MBE on the formation of reactive oxygen species was assessed using the DCFH2 -DA assay. Wound healing assay, transwell cell invasion assay, cell adhesion assay, and the extracellular matrix-cell adhesion array were used to assess the antimetastatic effects of MBE. The effect of MBE on the expression of TNF-α, NF-κB, TIMP-3, MMP-2, and MMP-9 was assessed by western blot analysis. Our results showed that MBE consists of a mixture of compounds without a known anticancer activity in CRC and exhibits cytotoxicity against HT-29 cells. MBE also suppressed reactive oxygen species formation, cell invasion, cell migration, and cell adhesion. The reduction of cell invasion was associated with the downregulation of TNF-α, NF-κB, MMP2, and MMP9 and upregulation of TIMP-3 proteins. We concluded that MBE inhibits the metastatic ability of HT-29 CRC cells in vitro.
Assuntos
Neoplasias do Colo , Momordica , Acetona , Linhagem Celular Tumoral , Movimento Celular , Proliferação de Células , Neoplasias do Colo/tratamento farmacológico , Células HT29 , Humanos , Extratos Vegetais/farmacologiaRESUMO
Momordica balsamina leaf extracts originating from three different geographical locations were analyzed using reversed-phase liquid chromatography (RP-LC) coupled to travelling wave ion mobility (TWIMS) and high-resolution mass spectrometry (HRMS) in conjunction with chemometric analysis to differentiate between potential chemotypes. Furthermore, the cytotoxicity of the three individual chemotypes was evaluated using HT-29 colon cancer cells. A total of 11 molecular species including three flavonol glycosides, five cucurbitane-type triterpenoid aglycones and three glycosidic cucurbitane-type triterpenoids were identified. The cucurbitane-type triterpenoid aglycones were detected in the positive ionization mode following dehydration [M + H - H2O]+ of the parent compound, whereas the cucurbitane-type triterpenoid glycosides were primarily identified following adduct formation with ammonia [M + NH4]+. The principle component analysis (PCA) loadings plot and a variable influence on projection (VIP) analysis revealed that the isomeric pair balsaminol E and/or karavilagen E was the key molecular species contributing to the distinction between geographical samples. Ultimately, based on statistical analysis, it is hypothesized that balsaminol E and/or karavilagen E are likely responsible for the cytotoxic effects in HT-29 cells.
Assuntos
Antineoplásicos Fitogênicos/química , Flavonóis/química , Glicosídeos/química , Momordica/química , Triterpenos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Cromatografia de Fase Reversa , Flavonóis/isolamento & purificação , Flavonóis/farmacologia , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Células HT29 , Humanos , Concentração Inibidora 50 , Espectrometria de Massas/métodos , Extratos Vegetais/química , Folhas de Planta/química , Análise de Componente Principal , Relação Estrutura-Atividade , Triterpenos/isolamento & purificação , Triterpenos/farmacologiaRESUMO
Obesity and its associated conditions, such as type 2 diabetes mellitus (T2DM) and nonalcoholic fatty liver disease (NAFLD), are a particular worldwide health problem at present. Momordica cochinchinensis (MC) is consumed widely in Southeast Asia. However, whether it has functional effects on fat-induced metabolic syndrome remains unclear. This study was conducted to examine the prevention effect of Momordica cochinchinensis aril (MCA) on obesity, non-alcoholic fatty liver and insulin resistance in mice. MCA protected the mice against high-fat diet (HFD)-induced body weight gain, hyperlipidemia and hyperglycemia, compared with mice that were not treated. MCA inhibited the expansion of adipose tissue and adipocyte hypertrophy. In addition, the insulin sensitivity-associated index that evaluates insulin function was also significantly restored. MCA also regulated the secretion of adipokines in HFD-induced obese mice. Moreover, hepatic fat accumulation and liver damage were reduced, which suggested that fatty liver was prevented by MCA. Furthermore, MCA supplementation suppressed hepatic lipid accumulation by activation of the AMP-activated protein kinase (AMPK) and peroxisome proliferator-activated receptor-alpha (PPAR-alpha) signaling pathway in the human fatty liver HuS-E/2 cell model. Our data indicate that MCA altered the microbial contents of the gut and modulated microbial dysbiosis in the host, and consequently is involved in the prevention of HFD-induced adiposity, insulin resistance and non-alcoholic fatty liver disease.
Assuntos
Frutas/química , Microbioma Gastrointestinal/efeitos dos fármacos , Momordica/química , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Obesidade/tratamento farmacológico , Extratos Vegetais/farmacologia , Animais , Dieta Hiperlipídica/efeitos adversos , Masculino , Camundongos , Hepatopatia Gordurosa não Alcoólica/induzido quimicamente , Hepatopatia Gordurosa não Alcoólica/metabolismo , Hepatopatia Gordurosa não Alcoólica/patologia , Obesidade/induzido quimicamente , Obesidade/metabolismo , Obesidade/patologia , Extratos Vegetais/químicaRESUMO
Momordica cochinchinensis (Lour.) Spreng is an indigenous South Asian edible fruit, and seeds of Momordica cochinchinensis have been used therapeutically in traditional Chinese medicine. Previous studies have shown that M. cochinchinensis seed (Momordicae Semen) has various pharmaceutical properties such as antioxidant and anti-ulcer effects as well as contains secondary metabolites with potential anticancer activities such as triterpenoids and saponins. Recent studies reported that water extract and ethanol extract of M. cochinchinensi seed were tested on mammals using an acute toxic classic method as OECD guidelines 420. No matter injected intravenously or intramuscularly, animals died within several days. In this study, zebrafish embryos were exposed to various doses of Cochinchina momordica seed extract (CMSE) from 2 dpf (days post fertilization, dpf) to 3 dpf. CMSE-induced cardiotoxicity such as pericardial edema, cardiac apoptosis, increased ROS production, cardiac neutrophil infiltration, decreased blood flow velocity, and reduced expression of three marker genes of cardiac functions were found in zebrafish roughly in a dose-dependent manner. These results suggest that CMSE may induce cardiotoxicity through pathways involved in inflammation, oxidative stress, and apoptosis.
Assuntos
Cardiotoxicidade/etiologia , Momordica/química , Extratos Vegetais/toxicidade , Sementes/química , Animais , Apoptose/efeitos dos fármacos , Embrião não Mamífero/efeitos dos fármacos , Coração/efeitos dos fármacos , Hemodinâmica/efeitos dos fármacos , Momordica/toxicidade , Sementes/toxicidade , Peixe-ZebraRESUMO
BACKGROUND: Momordica saponin extract (MSE) was found to not only improve longevity and neuroprotection but also alleviate fat accumulation in Caenorhabditis elegans in our previous study. However, the lipid-lowering activity of MSE alone could not fully explain its ability to improve health, so the antistress effects of MSE were further studied. METHODS: Using C. elegans as an in vivo animal, the lifespan of MSE-treated C. elegans under various stressors (H2O2, paraquat and heat) and normal conditions was studied. Furthermore, the antioxidant activities of MSE were discussed. To study the underlying mechanisms, the expression of stress resistance genes and the resistance of related mutants to H2O2 stress were tested. RESULTS: MSE significantly improved the lifespan of C. elegans under stress and normal conditions. Meanwhile, the mobility of C. elegans was also improved. Moreover, the activities of SOD and CAT and the ratio of GSH/GSSG were elevated. Consistently, the levels of ROS and lipid oxidation (the NEFA and MDA content) were reduced. Furthermore, MSE treatment upregulated the expression of the sod-3, sod-5, clt-1, clt-2, hsp-16.1 and hsp-16.2 genes. All biomarkers indicated that the antistress and anti-aging activities of MSE were due to its strong antioxidant activities. Finally, MSE induced nuclear DAF-16::GFP localization. Studies with mutants revealed that skn-1 and hsf-1 were involved in the activity of MSE, which might upregulate the expression of downstream stress-responsive genes. CONCLUSIONS: Therefore, in addition to its lipid-lowering property, the ability of MSE to improve healthspan was also attributed to the stress resistance effect. Together, MSE might serve as a lead nutraceutical in geriatric research.
Assuntos
Proteínas de Caenorhabditis elegans , Momordica , Saponinas , Envelhecimento , Animais , Antioxidantes/farmacologia , Caenorhabditis elegans/metabolismo , Proteínas de Caenorhabditis elegans/genética , Proteínas de Caenorhabditis elegans/metabolismo , Fatores de Transcrição Forkhead/metabolismo , Peróxido de Hidrogênio , Longevidade , Momordica/metabolismo , Estresse Oxidativo , Extratos Vegetais/farmacologia , Espécies Reativas de Oxigênio , Saponinas/farmacologiaRESUMO
BACKGROUND: Momordica cochinchinensis (Cucurbitaceae) is a nutritionally and medicinally important fruit restricted to South East Asia with diverse morphological and genetic variations but there is limited information on its medicinal potential. METHODS: M. cochinchinensis aril from 44 different samples in Australia, Thailand and Vietnam were extracted using different solvents and tested for its anticancer potential. Anticancer activity of M. cochinchinensis aril on breast cancer (MCF7 and BT474) and melanoma (MM418C1 and D24) cells were compared to control fibroblasts (NHDF). The cytotoxicity of the cells following treatment with the aril extract was determined using CCK-8 assay. Biochemical and morphological changes were analysed using flow cytometry, confocal and transmission electron microscopy to determine the mechanism of cell death. RESULTS: The water extract from the aril of M. cochinchinensis elicited significantly higher cytotoxicity towards breast cancer and melanoma cells than the HAE extract. The IC50 concentration for the crude water extract ranged from 0.49 to 0.73 mg/mL and induced both apoptotic and necrotic cell death in a dose- and time-dependant manner with typical biochemical and morphological characteristics. The greatest cytotoxicity was observed from Northern Vietnam samples which caused 70 and 50% melanoma and breast cancer cell death, respectively. CONCLUSIONS: The water extract of M. cochinchinensis aril caused significant apoptosis and necrosis of breast cancer and melanoma cells, with varieties from Northern Vietnam possessing superior activity. This highlights the potential of this fruit in the development of novel anticancer agents against such tumours, with specific regions on where to collect the best variety and extraction solvent for optimum activity.