RESUMO
Products derived from medicinal plants with antimicrobial activity are considered a promising alternative in the treatment of fungal infections. In this perspective, this study proposed to evaluate the antifungal activity of the dichloromethane fraction of Annona crassiflora Mart. against C. albicans strains. Tests were carried out to determine Minimum Inhibitory Concentration (MIC), Minimum Fungicide Concentration (MFC), microbial growth kinetics, fungal cell wall and membrane mechanisms of action, antifungal biofilm activity, and cytotoxic effects on human erythrocytes. The extract presented MIC and MFC values that ranged from 256 µg/mL to 1,024 µg/mL, with fungicidal activity in the microbial growth kinetics assay. The mechanism of action did not occur through damage to the cell wall or via binding to ergosterol in the membrane, though the fraction presents activity against biofilm and is not cytotoxic in human erythrocytes. The dichloromethane fraction of Annona crassiflora Mart. presented antifungal activity and reduced biofilm growth, without toxicity against human erythrocytes; however, further studies are needed to define its mechanism of action.
Assuntos
Annona , Antifúngicos , Biofilmes , Candida albicans , Cloreto de Metileno , Testes de Sensibilidade Microbiana , Extratos Vegetais , Annona/química , Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Humanos , Extratos Vegetais/farmacologia , Biofilmes/efeitos dos fármacos , Eritrócitos/efeitos dos fármacosRESUMO
The nematode Haemonchus contortus is, as a parasite, responsible for most mortality of small ruminants, causing significant economic losses. Numerous plant-derived compounds have exhibited promising anthelmintic activities against this nematode. Notably, the Annona genus stands out for demonstrated anthelmintic effects by extracts from several of its species against different nematodes. This study aimed to assess the effect of an Annona tomentosa fraction, rich in alkaloids, on H. contortus. This fraction, named Alk.F, is derived from the methanolic extract of the plant's stem bark. Chemical characterization of Alk.F was performed by liquid chromatography coupled with mass spectrometry. Among the nine predominant peaks obtained, seven alkaloids were identified: reticuline, reticuline N-oxide, reticuline N-oxide isomer, cyclanoline, asimilobine, tetrahydropalmatine and anonaine. Alk.F inhibited the larval development of H. contortus with an IC50 of 0.026â¯mg/mL, inhibited larval exsheathment with an IC50 of 0.38â¯mg/mL, and displayed low hemolytic activity towards sheep erythrocytes. Furthermore, atomic force microscopy revealed that Alk.F altered adhesive forces and the height profile on the surface of H. contortus larvae. In conclusion, A. tomentosa alkaloids alter the cuticle structure of H. contortus, inhibiting larval development and exsheathment, thus offering possibilities for contributing to the development of new anthelmintic drugs.
Assuntos
Alcaloides , Annona , Anti-Helmínticos , Haemonchus , Extratos Vegetais , Animais , Haemonchus/efeitos dos fármacos , Annona/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Anti-Helmínticos/farmacologia , Anti-Helmínticos/química , Alcaloides/farmacologia , Alcaloides/química , Larva/efeitos dos fármacos , Casca de Planta/química , Ovinos , Hemoncose/veterinária , Hemoncose/tratamento farmacológico , Hemoncose/parasitologiaRESUMO
This study aims to investigate the use of pond apple (Annona glabra) compounds as a novel strategy to prevent and treat acute hepatopancreatic necrosis disease (AHPND) as well as to better understand the mechanism of health improvement in shrimp. The A. glabra leaf extracts were extracted using various solvents and examined for in vitro and in vivo activity against Vibrio parahaemolyticus strains. In comparison with ethanol and water extracts, methanol extract showed the strongest bactericidal effect (MBC/MIC ratio of 2.50 ± 1.00), with minimal inhibitory concentration (MIC) of 0.023 ± 0.012 mg ml-1 and minimum bactericidal concentration (MBC) of 0.065 ± 0.062 mg ml-1. White leg shrimp (P. vannamei, body weight 10.37 ± 0.27 g) fed A. glabra methanol extracts-containing diets (AMEDs) at 1 %, 1.5 %, and 2.0 % demonstrated no deleterious effects on survival and were significantly increased in length and weight after 30 days of feeding. The level of total haemocyte, hyaline haemocyte on day 15 and granulocyte on day 30 remarkably increased (p < 0.05) in shrimps fed AMEDs groups compared to those in the control group. The finding demonstrates that granulocyte was induced time dependently. In particular, the survival rate of V. parahaemolyticus challenged shrimps under medication with AMEDs at 1.5 % and 2.0 % was significantly higher (p < 0.05) than that of the control group. The decrease in bacterial load of Vibrio spp. and V. parahaemolyticus was obviously recorded in hepatopancreas shrimp given AMEDs 1.5 % and 2.0 % and may be linked to herb characteristics such as antibacterial activity, enhancing innate immunity, and its potential to maintain the integrity of hepatopancreatic tissue. Our findings suggest that A. glabra extract might be used as a health enhancer in commercial farmed shrimp.
Assuntos
Annona , Hepatopâncreas , Penaeidae , Extratos Vegetais , Vibrio parahaemolyticus , Animais , Penaeidae/microbiologia , Penaeidae/efeitos dos fármacos , Extratos Vegetais/farmacologia , Vibrio parahaemolyticus/efeitos dos fármacos , Annona/química , Hepatopâncreas/efeitos dos fármacos , Hepatopâncreas/patologia , Antibacterianos/farmacologiaRESUMO
INTRODUCTION: The leaves of Annona muricata L., known as "soursop" or "sirsak" in Indonesia, are used traditionally for cancer treatment. However, the bioactive components remain largely unidentified. OBJECTIVE: This study used untargeted liquid chromatography-tandem mass spectrometry (LC-MS/MS)-based metabolomics to identify potential cytotoxic compounds in A. muricata leaf extracts on MCF-7 breast cancer cells in vitro. METHODS: A. muricata leaves were macerated with water, 99% ethanol, and aqueous mixtures containing 30%, 50%, and 80% ethanol. Cytotoxic activity of the extracts against MCF-7 breast cancer cells was determined using the MTT assay. Ultra-high-performance liquid chromatography-Q-Orbitrap high-resolution mass spectroscopy (UHPLC-Q-Orbitrap-HRMS) was used to characterize the metabolite composition of each extract. The correlations between metabolite profile and cytotoxic activities were evaluated using orthogonal partial least square discriminant analysis (OPLS-DA). The binding of these bioactive compounds to the tumorigenic alpha-estrogen receptor (3ERT) was then evaluated by in silico docking simulations. RESULTS: Ninety-nine percent ethanol extracts demonstrated the greatest potency for reducing MCF-7 cell viability (IC50 = 22 µg/ml). We detected 35 metabolites in ethanol extracts, including alkaloids, flavonoids, and acetogenins. OPLS-DA predicted that annoreticuin, squadiolin C, and xylopine, and six unknown acetogenin metabolites, might reduce MCF-7 cell viability. In silico analysis predicted that annoreticuin, squadiolin C, and xylopine bind to 3ERT with an affinity comparable to doxorubicin. CONCLUSION: Untargeted metabolomics and in silico modeling identified cytotoxic compounds on MCF-7 cells and binding affinity to 3ERT in A. muricata leaf extracts. The findings need to be further verified to prove the screening results.
Assuntos
Annona , Antineoplásicos Fitogênicos , Metabolômica , Extratos Vegetais , Folhas de Planta , Espectrometria de Massas em Tandem , Humanos , Annona/química , Folhas de Planta/química , Células MCF-7 , Cromatografia Líquida de Alta Pressão/métodos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Metabolômica/métodos , Antineoplásicos Fitogênicos/farmacologia , Espectrometria de Massas em Tandem/métodos , Simulação de Acoplamento Molecular , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/metabolismoRESUMO
Lead (Pb) is a common pollutant that is not biodegradable and gravely endangers the environment and human health. Annona squamosa fruit has a wide range of medicinal uses owing to its phytochemical constituents. This study evaluated the effect of treatment with A. squamosa fruit extract (ASFE) on testicular toxicity induced in male rats by lead acetate. The metal-chelating capacity and phytochemical composition of ASFE were determined. The LD50 of ASFE was evaluated by probit analysis. Molecular docking simulations were performed using Auto Dock Vina. Forty male Sprague Dawley rats were equally divided into the following groups: Gp1, a negative control group; Gp2, given ASFE (350 mg/kg body weight (b. wt.)) (1/10 of LD50); Gp3, given lead acetate (PbAc) solution (100 mg/kg b. wt.); and Gp4, given PbAc as in Gp3 and ASFE as in Gp2. All treatments were given by oro-gastric intubation daily for 30 days. Body weight changes, spermatological parameters, reproductive hormone levels, oxidative stress parameters, and inflammatory biomarkers were evaluated, and molecular and histopathological investigations were performed. The results showed that ASFE had promising metal-chelating activity and phytochemical composition. The LD50 of ASFE was 3500 mg/kg b. wt. The docking analysis showed that quercetin demonstrated a high binding affinity for JAK-1 and STAT-3 proteins, and this could make it a more promising candidate for targeting the JAK-1/STAT-3 pathway than others. The rats given lead acetate had defective testicular tissues, with altered molecular, biochemical, and histological features, as well as impaired spermatological characteristics. Treatment with ASFE led to a significant mitigation of these dysfunctions and modulated the JAK-1/STAT-3/SOCS-1 axis in the rats.
Assuntos
Annona , Frutas , Compostos Organometálicos , Extratos Vegetais , Transdução de Sinais , Testículo , Animais , Masculino , Ratos , Annona/química , Frutas/química , Janus Quinase 1/metabolismo , Simulação de Acoplamento Molecular , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Ratos Sprague-Dawley , Transdução de Sinais/efeitos dos fármacos , Fator de Transcrição STAT3/metabolismo , Testículo/efeitos dos fármacos , Testículo/metabolismo , Testículo/patologiaRESUMO
The use of extracts rich in bioactive compounds is becoming increasingly common in the food, cosmetics, and pharmaceutical industries for the production of functional products. Araticum is a potential fruit to be analyzed due to its content of phenolic compounds, carotenoids and vitamins, with antioxidant properties. Therefore, this study aimed to investigate the effect of ultrasound on total phenolic compounds, total carotenoids, ascorbic acid, color, turbidity and rheology in araticum juice. Response surface methodology based on a central composite design was applied. Araticum juice was subjected to sonication at amplitude levels ranging from 20 to 100 % of the total power (400 W) at a constant frequency of 20 kHz for different durations (2 to 10 min). Morphological analysis was conducted to observe microscopic particles, and viscosity and suitability to rheological models (Newtonian, Power Law, and Herschel-Bulkley) were assessed. The ultrasonic probe extraction method was compared to the control juice. According to the responses, using the desirability function, the optimal conditions for extraction were determined to be low power (low amplitude) applied in a short period of time or low power applied in a prolonged time. These conditions allowed an ultrasonic probe to act on releasing bioactive compounds without degrading them. All three rheological models were suitable, with the Power Law model being the most appropriate, exhibiting non-Newtonian pseudoplastic behavior.
Assuntos
Reologia , Annona/química , Sucos de Frutas e Vegetais/análise , Carotenoides/química , Viscosidade , Ondas Ultrassônicas , Sonicação , Fenóis/química , Ácido Ascórbico/químicaRESUMO
Global aflatoxin contamination of agricultural commodities is of the most concern in food safety and quality. This study investigated the hepatoprotective effect of 80% methanolic leaf extract of Annona senegalensis against aflatoxin B1 (AFB1)-induced toxicity in rats. A. senegalensis has shown to inhibit genotoxicity of aflatoxin B1 in vitro. The rats were divided into six groups including untreated control, aflatoxin B1 only (negative control); curcumin (positive control; 10 mg/kg); and three groups receiving different doses (100 mg/kg, 200 mg/kg, and 300 mg/kg) of A. senegalensis extract. The rats received treatment (with the exception of untreated group) for 7 days prior to intoxication with aflatoxin B1. Serum levels of aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, lactate dehydrogenase, and creatinine were measured. Hepatic tissues were analysed for histological alterations. Administration of A. senegalensis extract demonstrated hepatoprotective effects against aflatoxin B1-induced toxicity in vivo by significantly reducing the level of serum aspartate aminotransferase and alanine aminotransferase and regenerating the hepatocytes. No significant changes were observed in the levels of alkaline phosphatase, lactate dehydrogenase, and creatinine for the AFB1 intoxicated group, curcumin+AFB1 and Annona senegalensis leaf extract (ASLE)+AFB1 (100 mg/kg, 200 mg/kg, and 300 mg/kg body weight [b.w.]) treated groups. Annona senegalensis is a good candidate for hepatoprotective agents and thus its use in traditional medicine may at least in part be justified.Contribution: The plant extract investigated in this study can be used in animal health to protect the organism from toxicity caused by mycotoxins.
Assuntos
Annona , Curcumina , Ratos , Animais , Aflatoxina B1/toxicidade , Curcumina/farmacologia , Alanina Transaminase/farmacologia , Fosfatase Alcalina/farmacologia , Creatinina/farmacologia , Fígado , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Aspartato Aminotransferases/farmacologia , Lactato DesidrogenasesRESUMO
The obtained seeds from fruit processing are considered by-products containing proteins that could be utilized as ingredients in food manufacturing. However, in the specific case of soursop seeds, their usage for the preparation of protein isolates is limited. In this investigation a protein isolate from soursop seeds (SSPI) was obtained by alkaline extraction and isoelectric precipitation methods. The SSPI was sonicated at 200, 400 and 600 W during 15 and 30 min and its effect on the physicochemical, functional, biochemical, and structural properties was evaluated. Ultrasound increased (p < 0.05) up to 5 % protein content, 261 % protein solubility, 60.7 % foaming capacity, 30.2 % foaming stability, 86 % emulsifying activity index, 4.1 % emulsifying stability index, 85.4 % in vitro protein digestibility, 423.4 % albumin content, 83 % total sulfhydryl content, 316 % free sulfhydryl content, 236 % α-helix, 46 % ß-sheet, and 43 % ß-turn of SSPI, in comparison with the control treatment without ultrasound. Furthermore, ultrasound decreased (p < 0.05) up to 50 % particle size, 37 % molecular flexibility, 68 % surface hydrophobicity, 41 % intrinsic florescence spectrum, and 60 % random coil content. Scanning electron microscopy analysis revealed smooth structures of the SSPI with molecular weights ranging from 12 kDa to 65 kDa. The increase of albumins content in the SSPI by ultrasound was highly correlated (r = 0.962; p < 0.01) with the protein solubility. Improving the physicochemical, functional, biochemical and structural properties of SSPI by ultrasound could contribute to its utilization as ingredient in food industry.
Assuntos
Annona , Proteínas de Plantas , Sementes , Solubilidade , Sementes/química , Proteínas de Plantas/química , Proteínas de Plantas/isolamento & purificação , Annona/química , Ondas Ultrassônicas , Fenômenos Químicos , SonicaçãoRESUMO
Vulvovaginal candidiasis, mostly caused by Candida albicans, remains a prevalent concern in women's health. Annona muricata L. (Annonaceae), a plant native from Brazil, is well-known for its therapeutic potential, including antitumor, anti-inflammatory, and antimicrobial properties. This study presents an innovative hydrogel formulation containing the ethanolic extract from A. muricata leaves designed to control C. albicans in an in vivo model of vulvovaginal candidiasis. Here, we report the development, thermal, physicochemical and rheological characterization of a Carbopol®-based hydrogel containing A. muricata extract. Furthermore, we evaluated its activity in a vulvovaginal candidiasis in vivo model. Thermal analyses indicated that the addition of the extract increased the polymer-polymer and polymer-solvent interactions.Rheological analysis showed a decrease in the viscosity and elasticity of the formulation as the A. muricata extract concentration increased, suggesting a liquid-like behavior. After treatment with the Carbopol®-based hydrogel with A. muricata, our in vivo results showed a significant reduction in vulvovaginal fungal burden and infection, as well as a reduction in mucosal inflammation. The current research opens up possibilities for the application of the Carbopol®-based hydrogel with A. muricata as a natural therapeutic option for the treatment of vulvovaginal candidiasis.
Assuntos
Annona , Antifúngicos , Candida albicans , Candidíase Vulvovaginal , Hidrogéis , Extratos Vegetais , Folhas de Planta , Annona/química , Candidíase Vulvovaginal/tratamento farmacológico , Candidíase Vulvovaginal/microbiologia , Antifúngicos/farmacologia , Antifúngicos/química , Feminino , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Hidrogéis/química , Hidrogéis/farmacologia , Candida albicans/efeitos dos fármacos , Animais , Reologia , Testes de Sensibilidade Microbiana , CamundongosRESUMO
This review aimed to critically and comparatively analyze the physicochemical, proximate, nutritional, phytochemical composition, and bioactivities of araticum (Annona crassiflora Mart.) (AAc), a fruit from the Brazilian Cerrado. Additionally, the potential applications of this fruit in the food industry were reviewed. Data and information were collected from the Scopus, Web of Science, and Google Scholar databases. AAc, a fruit mainly studied in the Brazilian regions of Minas Gerais and Goiás, has well-documented physicochemical, proximate, and nutritional characteristics. It is rich in fiber, sugars, vitamins A and C, minerals, and oil, making it attractive to the food industry. However, there are research gaps, such as the impact of climatic conditions on the AAc chemical composition. Additional studies are needed, especially for the peel and seeds, and investigations of pre-treatments effect on the chemical composition are recommended. The application of AAc in food products is mainly limited to pulp, but there is potential for using peels and seeds. AAc is a rich source of phytochemical compounds with various biological properties, such as antioxidants, hepatoprotective, and antimicrobial activities. Future studies should explore other phytochemicals present in the fruit beyond phenolic compounds. The consumption of AAc can contribute to combating food insecurity malnutrition, and promoting the conservation of the Brazilian Cerrado.
Assuntos
Annona , Indústria Alimentícia , Frutas , Sementes , Compostos FitoquímicosRESUMO
Annona montana mucilage (AMM) is a novel mucilage with unique but limited information. This study investigated the effects of AMM addition on the pasting and rheological properties of wheat starch (WS), corn starch (CS), water caltrop starch (WCS), and lotus rhizome starch (LRS). The addition of AMM generally increased the pasting temperature and peak viscosity, but reduced the setback value of all starches to varying degrees, and the initiation of viscosity-increase for cereal starch/AMM systems during pasting occurred at lower temperatures, accompanied with a distinctive two-stage swelling process as well as lower peak and final hot paste viscosity at 50 °C. AMM significantly increased the pseudoplasticity and entanglement of the systems to varying degrees (LRS > WS > WCS > CS). Under a constant shear rate of 50 s-1, the consistency level was found to fall in honey-like for cereal starch/AMM groups, and honey-like to extremely thick levels for WCS and LRS/AMM groups. Except for the WCS/AMM systems, the storage and loss modulus as well as tan increased with increasing AMM concentration. Short-term retrogradation of starch at 4 °C was pronouncedly retarded by the addition of AMM for WS, CS and WCS groups, but was less affected for LRS group.
Assuntos
Annona , Lotus , Lythraceae , Zea mays , Triticum , Montana , Rizoma , Amido , Polissacarídeos , ViscosidadeRESUMO
Fruit peels might be a valuable source of active ingredients for cosmetics, leading to more sustainable usage of plant by-products. The aim of the study was to evaluate the phytochemical content and selected biological properties of hydroglycolic extracts from peels and pulps of Annona cherimola, Diospyros kaki, Cydonia oblonga, and Fortunella margarita as potential cosmetic ingredients. Peel and pulp extracts were compared for their antiradical activity (using DPPH and ABTS radical scavenging assays), skin-lightening potential (tyrosinase inhibitory assay), sun protection factor (SPF), and cytotoxicity toward human fibroblast, keratinocyte, and melanoma cell lines. The total content of polyphenols and/or flavonoids was significantly higher in peel than in pulp extracts, and the composition of particular active compounds was also markedly different. The HPLC-MS fingerprinting revealed the presence of catechin, epicatechin and rutoside in the peel of D. kaki, whereas kaempferol glucoside and procyanidin A were present only in the pulp. In A. cherimola, catechin, epicatechin and rutoside were identified only in the peel of the fruit, whereas procyanidins were traced only in the pulp extracts. Quercetin and luteolinidin were found to be characteristic compounds of F. margarita peel extract. Naringenin and hesperidin were found only in the pulp of F. margarita. The most significant compositional variety between the peel and pulp extracts was observed for C. oblonga: Peel extracts contained a higher number of active components (e.g., vicenin-2, kaempferol rutinoside, or kaempferol galactoside) than pulp extract. The radical scavenging potential of peel extracts was higher than of the pulp extracts. D. kaki and F. margarita peel and pulp extracts inhibited mushroom and murine tyrosinases at comparable levels. The C. oblonga pulp extract was a more potent mushroom tyrosinase inhibitor than the peel extract. Peel extract of A. cherimola inhibited mushroom tyrosinase but activated the murine enzyme. F. margarita pulp and peel extracts showed the highest in vitro SPF. A. cherimola, D. kaki, and F. margarita extracts were not cytotoxic for fibroblasts and keratinocytes up to a concentration of 2% (v/v) and the peel extracts were cytotoxic for A375 melanoma cells. To summarize, peel extracts from all analyzed fruit showed comparable or better cosmetic-related properties than pulp extracts and might be considered multifunctional active ingredients of skin lightening, anti-aging, and protective cosmetics.
Assuntos
Annona , Catequina , Diospyros , Melanoma , Rosaceae , Rutaceae , Camundongos , Animais , Humanos , Catequina/análise , Antioxidantes/farmacologia , Diospyros/química , Quempferóis/análise , Monofenol Mono-Oxigenase , Polegar , Frutas/química , Rosaceae/química , Rutina/análise , Compostos Fitoquímicos/análise , Extratos Vegetais/químicaRESUMO
INTRODUCTION: Soursop (Annona muricata L.) is a crop with medicinal properties and numerous bioactive compounds. Ripening is a complex process that regulates fruit quality and changes in metabolite content, such as flavonoids, polyphenols, and organic acids. OBJECTIVES: This study aimed to analyze the phenolic profiling of soursop fruit ripening. METHODS: The metabolic changes in different days of storage of soursop fruits were investigated using a semi-metabolomic approach based on ultra-performance liquid chromatography coupled to electrospray ionization quadrupole-time of flight mass spectrometry (UPLC-ESI-QTOF-MS). Further, multivariate analysis such as supervised partial least squares discriminant analysis (PLS-DA) was conducted to identify differential metabolites. RESULTS: A total of 68 metabolites were identified in soursop fruit during postharvest storage. A higher number of metabolites were identified in the Day zero (D0) compared to the Day one (D1), Day three (D3), and Day five (D5), belonging to flavonoids, other polyphenols, phenolic acids, and organic acids. The Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis showed that the pathways of flavone and flavonol biosynthesis, flavonoid biosynthesis, and biosynthesis of secondary metabolites were mostly enriched. Additionally, we included all the compounds and their postharvest storage in the public Phenolics profile database. CONCLUSIONS: Here, we show that the stage of ripening has a significant effect on the phenolic content, highlighting the point of cut (D0) and the onset of senescence (D5). The findings of this study provide new insights into the soursop fruit quality and may contribute to the identification of metabolic markers for its storage.
Assuntos
Annona , Metabolômica , Frutas , Fenóis , Polifenóis , FlavonoidesRESUMO
Chemical exploration of the total extract derived from Epicoccum nigrum Ann-B-2, an endophyte associated with Annona squamosa fruits, afforded two new metabolites, epicoccofuran A (1) and flavimycin C (2), along with four known compounds namely, epicocconigrone A (3), epicoccolide B (4), epicoccone (5) and 4,5,6-trihydroxy-7-methyl-1,3-dihydroisobenzofuran (6). Structures of the isolated compounds were elucidated using extensive 1D and 2D NMR along with HR-ESI-MS. Flavimycin C (2) was isolated as an epimeric mixture of its two diastereomers 2a and 2b. The new compounds 1 and 2 displayed moderate activity against B. subtilis, whereas compounds (2, 3, 5, and 6) showed significant antiproliferative effects against a panel of seven different cancer cell lines with IC50 values ranging from 1.3 to 12 µM.
Assuntos
Annona , Antineoplásicos , Ascomicetos , Benzofuranos , Annona/química , Frutas , Benzofuranos/farmacologia , Ascomicetos/química , Antineoplásicos/química , Estrutura MolecularRESUMO
CONTEXT: The present study aims to investigate the therapeutic potential of phytocompounds derived from Annona reticulata leaves for the treatment of hypertension, utilizing computational methodologies. Gaining a comprehensive understanding of the molecular interactions between neophytadiene and γ-sitosterol holds significant importance in the advancement of innovative therapeutic approaches. This study aims to examine the inhibitory effects of neophytadiene and γ-sitosterol using molecular docking and dynamics simulations. Additionally, we will evaluate their stability and predict their drug-like properties as well as their ADME/toxicity profiles. Neophytadiene and γ-sitosterol have a substantial binding affinity with 1O8A, as shown by the docking study. The stability of the complexes was confirmed through molecular dynamics simulations, while distinct clusters were identified using PCA. These findings suggest the presence of potential stabilizers. The drug-likeness and ADME/toxicity predictions revealed positive characteristics, such as efficient absorption rates, limited distribution volume and non-hazardous profiles. The neophytadiene and γ-sitosterol exhibit potential as hypertension medication options. Computational investigations reveal that these compounds exhibit high affinity for binding, stability and favourable pharmacokinetic properties. The results of this study lay the groundwork for additional experimental verification and highlight the promising prospects of utilizing natural compounds in the field of pharmaceutical research. METHODS: Target proteins (1O8A) were used to perform molecular docking with representative molecules. Stability, conformational changes and binding energies were assessed through molecular dynamics simulations lasting 100 ns. Principal component analysis (PCA) was utilized to analyze molecular dynamics (MD) simulation data, to identify potential compounds that could stabilize the main protease. The safety and pharmacokinetic profiles of the compounds were evaluated through drug-likeness and ADME/toxicity predictions.
Assuntos
Annona , Fármacos Cardiovasculares , Inibidores da Enzima Conversora de Angiotensina , Simulação de Acoplamento Molecular , Compostos Fitoquímicos/farmacologiaRESUMO
OBJECTIVE: To study the antibacterial and phytochemical activities of bioactive elements in the leaves of Annona reticulata Linn, a historically used Bangladeshi medicinal plant. METHODS: Shade-dried and crushed plant leaves were soaked with various solvents to obtain samples for different chemical analyses. All extracts were selected for antimicrobial, physicochemical, and Pharmacological investigations. The antimicrobial activity was evaluated using disc diffusion assay, and broth microdilution methods determined potentiation of the activities of the antibiotic antibacterial activity of the plant extracts was investigated using either gram-positive or gram-negative pathogenic wild-type bacteria. RESULTS: From the initial phytochemical and pharmacological studies, it was clear that all extracts, methanol, chloroform, and ethyl acetate, of the leaves of A. reticulata, were proven to process potent bioactive constituents. While differential antimicrobial properties were found to be possessed by all extracts, methanolic extract was the most potent one against all tested microorganisms. It also has potentiated the activities of antibiotics in E. coli. CONCLUSION: Bioactive constituents in the plant extracts were shown to possess phytochemical and antimicrobial activities. More investigation is needed to segregate the chemical components responsible for the respective phytochemical and antimicrobial activities.
Assuntos
Annona , Anti-Infecciosos , Antibacterianos/química , Bactérias , Escherichia coli , Extratos Vegetais/química , Anti-Infecciosos/farmacologia , Bactérias Gram-Negativas , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Metanol , Folhas de Planta/química , Testes de Sensibilidade MicrobianaRESUMO
Soursop (Annona muricata) is a tropical tree whose decoction derived from bark, root, seed, or leaf has been used for medicinal uses. In addition, the fruit itself is considered a food, and the juice is utilized to treat heart and liver diseases. The aim of this study was to determine the phenolic content. In addition, a water-soluble fraction of the soursop fruit pulp (WSSP) was examined for the following properties: antioxidant, mutagenic, and antimutagenicity. UV-visible spectrophotometry determined total phenolic content by the Folin-Ciocalteu method to be 11.22 ± 0.6 mg of gallic acid equivalent per gram dried extract, and free-radical scavenging activity by the 2,2'-diphenyl-1-picryl-hydrazyl (DPPHâ¢) showed an EC50 of 1032 µg/ml. In the Salmonella/microsome assay, no marked mutagenicity was induced following WSSP treatment, and a chemopreventive capacity was observed in the antimutagenic assay. The cytotoxicity assays were carried out using the water-soluble tetrazolium salt and lactate dehydrogenase (LDH) assays demonstrated that WSSP induced significant cytotoxicity in MCF-7 and Caco-2 cells, indicating greater effectiveness of cytotoxic action by destroying cell membrane integrity. Data suggest that WSSP may exert beneficial effects as a DNA chemopreventive and antitumor agent.
Assuntos
Annona , Humanos , Annona/química , Frutas/química , Células CACO-2 , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Fenóis/análise , Antioxidantes/farmacologiaRESUMO
The seeds of Annona glabra L., an invasive plant in Vietnam, were first employed as a new biosorbent for the adsorption of methylene blue (MB) from aqueous media. The characterizations of the material using FT-IR, SEM, nitrogen adsorption-desorption analysis, and point of zero charge reveals that it possesses a rough and irregular surface, various polar functional groups, and pHpzc of 5.5. Certain adsorption conditions including adsorbent dose, solution pH, contact time, and initial concentration of MB were found to affect adsorption efficiency. The kinetic data are well fitted with pseudo-second-order model with the adsorption rate of 0.002 g mg-1 min-1 and initial rate of 4.46 mg g-1 min-1. For the adsorption isotherm, three nonlinear models were used to analyze the experiment data, including Langmuir, Freundlich, and Temkin. The results indicate that the Langmuir model best describes the adsorption of Annona glabra L. seeds powder (AGSP) with a maximum adsorption capacity of 98.0 mg g-1. The investigation underpins the adsorption mechanism, whereby the electrostatic attraction between positively charged MB and negatively charged surface of AGSP is expected to be the predominant mechanism, together with hydrogen bonding and pi-pi interaction. These results make AGSP an interesting biosorbent concerning its environmental friendliness, cost-effectiveness, and relatively high dye adsorption capacity.
Assuntos
Annona , Poluentes Químicos da Água , Azul de Metileno/análise , Azul de Metileno/química , Espectroscopia de Infravermelho com Transformada de Fourier , Poluentes Químicos da Água/análise , Concentração de Íons de Hidrogênio , Sementes/química , Adsorção , CinéticaRESUMO
Because of their low ecological impact, plant molluscicides have garnered much attention. The work aimed to find out if Annona squamosa (AS) seed extract has a molluscicidal impact on Biomphalaria alexandrina snails and enhances this extract by adding CuO nanoparticles (NPs). Using a scanning electron microscope (SEM), transmission electron microscope (TEM), and PANalytical X'Pert PRO X-ray diffractometer (XRD), the presence of the green A. squamosa-based CuO NPs (AS-CuO NPs) was confirmed. After 24 h of exposure, the half-lethal concentration (LC50) of AS-CuO NPs was more toxic to mature B. alexandrina than the aqueous extract of AS seeds (LC50: 119.25 mg/L vs. 169.03 mg/L). The results show that snails exposed to sublethal doses of AS-CuO NPs at LC10 or LC25 (95.4 or 106.7 mg/L, respectively) had much higher glucose levels and alkaline phosphatase activity than those not exposed. Nevertheless, there was no discernible change in the protein content in general or glycogen phosphorylase production. Histological and immunohistochemical analysis showed that snails exposed to A. squamosa-derived CuO NPs LC10 had shrinking digestive tubules and degeneration as well as vacuolation of many digestive, secretory, ova, and sperm cells, with PCNA expressing positively in the hermaphrodite gland and digestive tubule cells. The toxic profile of green CuO NPs produced by A. squamosa may damage the biological activity of B. alexandrina snails; thus, this compound could be used as a molluscicidal base. Furthermore, B. alexandrina proved to be a useful biomarker of nanomaterial contamination.
Assuntos
Annona , Biomphalaria , Moluscocidas , Nanopartículas , Animais , Cobre/farmacologia , Sementes , Moluscocidas/toxicidade , Extratos Vegetais/farmacologia , Comportamento Alimentar , ÓxidosRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Multi-Drug Resistance (MDR), mediated by P-glycoprotein (P-gp) is one of the barriers to successful chemotherapy in colon cancer patients. Annona muricata L. (A.muricata), commonly known as soursop/Graviola, is a medicinal plant that has been traditionally used in treating diverse diseases including cancer. Phytochemicals of A.muricata (Annonaceous Acetogenins-AGEs) have been well-reported for their anti-cancer effects on various cancers. AIM OF THE STUDY: The study aimed to examine the effect of AGEs in reversing MDR in colorectal cancer cells. METHODS: Based on molecular docking and molecular dynamic simulation, the stability of annonacin upon P-gp was investigated. Further in vitro studies were carried in oxaliplatin-resistant human colon cancer cells (SW480R) to study the biological effect of annonacin, in reversing drug resistance in these cells. RESULTS: Molecular docking and simulation studies have indicated that annonacin stably interacted at the drug binding site of P-gp. In vitro analysis showed that annonacin was able to significantly reduce the expression of P-gp by 2.56 folds. It also induced apoptosis in the drug-resistant colon cancer cells. Moreover, the intracellular accumulation of P-gp substrate (calcein-AM) was observed to increase in resistant cells upon treatment with annonacin. CONCLUSION: Our findings suggest that annonacin could inhibit the efflux of chemotherapeutic drugs mediated by P-gp and thereby help in reversing MDR in colon cancer cells. Further in vivo studies are required to decipher the underlying mechanism of annonacin in treating MDR cancers.