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Staphylococcus aureus is a bacterium responsible for resistance to multiple drugs and the efflux system is widely studied among the resistance mechanisms developed by this species. The present study evaluates the inhibition of the MepA efflux pump by thiadiazine-derived compounds. For this purpose, thiadiazine-derived compounds (IJ-14 to IJ-20) were tested against S. aureus K2068 strains. Microdilution tests were initially conducted to assess the Minimum Inhibitory Concentration (MIC) of the compounds and their efflux pump inhibition activity. In addition, fluorimetry tests were performed using BrEt emission and tests were conducted to inhibit the expression of the mepA gene. This involved comparing the bacterial gene expression with the antibiotic alone to the gene expression after combining compounds (IJ-17 and IJ-20) with the antibiotic. Furthermore, membrane permeability assessment tests and in silico molecular docking tests were performed. It was observed that the IJ17 and IJ20 compounds exhibited direct activity against the tested strain. The IJ17 compound produced significant results in the gene inhibition tests, which was also evidenced through the membrane permeability alteration test. These findings suggest that thiadiazine-derived compounds have promising effects against one of the main resistance mechanisms, with the IJ17 compound presenting observable mechanisms of action.
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Coumarins are compounds with scientifically proven antibacterial properties, and modifications to the chemical structure are known to improve their effects. This information is even more relevant with the unbridled advances of antibiotic resistance, where Staphylococcus aureus and its efflux pumps play a prominent role. The study's objective was to evaluate the potential of synthetic coumarins with different substitutions in the C-3 position as possible inhibitors of the NorA and MepA efflux pumps of S. aureus. For this evaluation, the following steps took place: (i) the determination of the minimum inhibitory concentration (MIC); (ii) the association of coumarins with fluoroquinolones and ethidium bromide (EtBr); (iii) the assessment of the effect on EtBr fluorescence emission; (iv) molecular docking; and (v) an analysis of the effect on membrane permeability. Coumarins reduced the MICs of fluoroquinolones and EtBr between 50% and 87.5%. Coumarin C1 increased EtBr fluorescence emission between 20 and 40% by reinforcing the evidence of efflux inhibition. The molecular docking results demonstrated that coumarins have an affinity with efflux pumps and establish mainly hydrogen bonds and hydrophobic interactions. Furthermore, C1 did not change the permeability of the membrane. Therefore, we conclude that these 3-substituted coumarins act as inhibitors of the NorA and MepA efflux pumps of S. aureus.
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In this review, we discuss the advantages of vegetable sprouts in the development of food products as well as their beneficial effects on a variety of disorders. Sprouts are obtained from different types of plants and seeds and various types of leafy, root, and shoot vegetables. Vegetable sprouts are enriched in bioactive compounds, including polyphenols, antioxidants, and vitamins. Currently, different conventional methods and advanced technologies are used to extract bioactive compounds from vegetable sprouts. Due to some issues in traditional methods, increasingly, the trend is to use recent technologies because the results are better. Applications of phytonutrients extracted from sprouts are finding increased utility for food processing and shelf-life enhancement. Vegetable sprouts are being used in the preparation of different functional food products such as juices, bread, and biscuits. Previous research has shown that vegetable sprouts can help to fight a variety of chronic diseases such as cancer and diabetes. Furthermore, in the future, more research is needed that explores the extraordinary ways in which vegetable sprouts can be incorporated into green-food processing and preservation for the purpose of enhancing shelf-life and the formation of functional meat products and substitutes.
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Alimentos Funcionales , Verduras , Polifenoles/farmacología , Polifenoles/análisis , Antioxidantes/farmacología , Antioxidantes/análisis , Semillas/químicaRESUMEN
Pectin is an acidic heteropolysaccharide found in the cell walls and the primary and middle lamella of land plants. To be authorized as a food additive, industrial pectins must meet strict guidelines set forth by the Food and Agricultural Organization and must contain at least 65% polygalacturonic acid to achieve the E440 level. Fruit pectin derived from oranges or apples is commonly used in the food industry to gel or thicken foods and to stabilize acid-based milk beverages. It is a naturally occurring component and can be ingested by dietary consumption of fruit and vegetables. Preventing long-term chronic diseases like diabetes and heart disease is an important role of dietary carbohydrates. Colon and breast cancer are among the diseases for which data suggest that modified pectin (MP), specifically modified citrus pectin (MCP), has beneficial effects on the development and spread of malignancies, in addition to its benefits as a soluble dietary fiber. Cellular and animal studies and human clinical trials have provided corroborating data. Although pectin has many diverse functional qualities, this review focuses on various modifications used to develop MP and its benefits for cancer prevention, bioavailability, clinical trials, and toxicity studies. This review concludes that pectin has anti-cancer characteristics that have been found to inhibit tumor development and proliferation in a wide variety of cancer cells. Nevertheless, further clinical and basic research is required to confirm the chemopreventive or therapeutic role of specific dietary carbohydrate molecules.
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Malus , Neoplasias , Animales , Humanos , Pectinas/farmacología , Pectinas/uso terapéutico , Frutas , Neoplasias/prevención & control , Carbohidratos de la DietaRESUMEN
Tuberculosis has become a major health problem globally. This is worsened by the emergence of resistant strains of Mycobacterium tuberculosis showing ability to evade the effectiveness of the current antimycobacterial therapies. Therefore, the efforts carried out to explore new entities from many sources, including marine, are critical. This review summarizes several marine-derived macrolides that show promising activity against M. tuberculosis. We also provide information regarding the biosynthetic processes of marine macrolides, including the challenges that are usually experienced in this process. As most of the studies reporting the antimycobacterial activities of the listed marine macrolides are based on in vitro studies, the future direction should consider expanding the trials to in vivo and clinical trials. In addition, in silico studies should also be explored for a quick screening on marine macrolides with potent activities against mycobacterial infection. To sum up, macrolides derived from marine organisms might become therapeutical options for tackling antimycobacterial resistance of M. tuberculosis.
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Mycobacterium tuberculosis , Tuberculosis , Humanos , Macrólidos/farmacología , Antituberculosos/farmacología , Antituberculosos/uso terapéutico , Farmacorresistencia Bacteriana , Tuberculosis/tratamiento farmacológico , Pruebas de Sensibilidad MicrobianaRESUMEN
Moringa oleifera and strawberry are cultivated extensively worldwide and are divinely blessed with an enormous amount of nutritional and medicinal constituents, such as vitamin C, vitamin E, iron, potassium, and phenolic antioxidants that play a pivotal role in treating, confining, and preventing diabetes and many kinds of cancer. The focus of the study is to develop different samples of highly acceptable ready to serve (RTS) Moringa strawberry juice blend by underutilizing Moringa and strawberry juice in different proportions. Moringa oleifera's bitter taste and green color steeply limits its acceptability and counter this drawback utilized with strawberry juice. The physicochemical analysis of blended juice was performed to investigate the suitability and keeping quality of the juice mixture. The collected data signify that pH titratable acidity (TA) and total soluble solids (TSS) the slight modification after the inclusion of Moringa juice extract and throughout the storage. The Moringa treatment positively improved the total phenolic content (TPC), antioxidant, and vitamin C from 12 to 49.17 mg GAE/100g, 61.41 to 87.69%, and 64.03 to 86.65 mg/100 mL, respectively, but there was a slight decline in antioxidant quantity while stored under refrigerated conditions for one month. An assimilative trend was noticed in TPC and vitamin C, which collapsed from 49.17-36.32 mg GAE to 86.65-79.19 mg, respectively. In accordance with sensory analysis T 2 (90% strawberry juice and 10% Moringa extract), the juice blend was rated best in context to flavor, color, and taste. This juice blend proved to be greatly effective especially for children suffering from malnutrition as well as women to counter with its appreciable number of nutritional constituents.
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Cancer is still one of the world's deadliest health concerns. As per latest statistics, lung, breast, liver, prostate, and cervical cancers are reported topmost worldwide. Although chemotherapy is most widely used methodology to treat cancer, poor pharmacokinetic parameters of anticancer drugs render them less effective. Novel nano-drug delivery systems have the caliber to improve the solubility and biocompatibility of various such chemical compounds. In this regard, cyclodextrins (CD), a group of natural nano-oligosaccharide possessing unique physicochemical characteristics has been highly exploited for drug delivery and other pharmaceutical purposes. Their cup-like structure and amphiphilic nature allows better accumulation of drugs, improved solubility, and stability, whereas CDs supramolecular chemical compatibility renders it to be highly receptive to various kinds of functionalization. Therefore combining physical, chemical, and bio-engineering approaches at nanoscale to specifically target the tumor cells can help in maximizing the tumor damage without harming non-malignant cells. Numerous combinations of CD nanocomposites were developed over the years, which employed photodynamic, photothermal therapy, chemotherapy, and hyperthermia methods, particularly targeting cancer cells. In this review, we discuss the vivid roles of cyclodextrin nanocomposites developed for the treatment and theranostics of most important cancers to highlight its clinical significance and potential as a medical tool.
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The quest for novel anti-diabetic medication from medicinal plants is very important since they contain bioactive phytochemicals that offer better activity and safety compared to conventional therapy. In the present study, in vitro, in vivo and in silico approaches were explored to evaluate the anti-inflammatory, antioxidants, and hypoglycemic activities of the crude methanol extract of Azanza garckeana pulp. Our in vitro analysis revealed that the extract contains total phenols (260.80⯱â¯2.23â¯mg/100â¯g) and total flavonoids (10.28⯱â¯1.29â¯mg/100â¯g) contents, and demonstrated dose-dependent in vitro antioxidants activities in; DPPH (IC50 =141.30⯱â¯1.64⯵g/mL), FRAP (IC50 =155.07⯱â¯1.03⯵g/mL), LPO (IC50 =184.96⯱â¯2.01⯵g/mL), and ABTS (IC50 =162.56⯱â¯1.14⯵g/mL) assays; anti-inflammatory activities in: membrane stabilization (IC50 =141.34⯱â¯0.46⯵g/mL), protein denaturation (IC50 =203.61⯱â¯2.35⯵g/mL) and proteinase activities (IC50=f 171.35⯱â¯1.56⯵g/mL) assays; and hypoglycemic activities in: α- amylase (IC50 277.85⯱â¯2.51⯵g/mL), and glucose uptake by yeast cells assays. In vivo analysis revealed that the extract exhibited dose-dependent anti-inflammatory, hypoglycemic activities and improved the weight gain in STZ-induced diabetic rats. In addition, the extract attenuated oxidative stress and increased the activities of SOD, catalase, GSH while depleting the level of LPO in STZ induced diabetic rats. Consequently, the liquid chromatography mass spectrometry (LC-MS) characterization of A. garckeana pulp, revealed the presence of 2-Hexadecen-1-ol,3,7,11,15-tetramethyl-,(2E,7â¯R,11â¯R)-, nonyl flavanone, testolactone and 6-(Benzyloxy)-â¯4,4-Dimethyl-2-Chromanone. These compounds were subjected to pharmacoinformatics analysis among which testolactone and 6-(Benzyloxy)-â¯4,4-Dimethyl-2-Chromanone demonstrated the best drug-likeness, pharmacokinetics, and also exhibited potential hypoglycemic and anti-inflammatory properties. Altogether, the present study provides preclinical evidence of the antioxidant, anti-inflammatory and antidiabetic activities of A. garckeana extract suggesting its potential applications for the development of alternative therapy for diabetes and its associated inflammatory condition.
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Diabetes Mellitus Experimental , Malvaceae , Animales , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Antioxidantes/uso terapéutico , Glucemia , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/química , Hipoglucemiantes/farmacología , Hipoglucemiantes/uso terapéutico , Extractos Vegetales/uso terapéutico , Ratas , Testolactona/uso terapéuticoRESUMEN
Colorectal cancer (CRC) is one of the most common and reoccurring diseases, as well as the world's second largest cause of mortality. Despite existing preventative, diagnostic, and treatment methods, such as chemotherapy, the number of instances rises year after year. As a result, new effective medications targeting specific checkpoints should be developed to combat CRC. Natural compounds, such as curcumin, have shown significant anti-colorectal cancer characteristics among medications that can be used to treat CRC. These chemicals are phenolic compounds that belong to the curcuminoids category. Curcumin exerts its anti-proliferative properties against CRC cell lines in vitro and in vivo via a variety of mechanisms, including the suppression of intrinsic and extrinsic apoptotic signaling pathways, the stoppage of the cell cycle, and the activation of autophagy. Curcumin also has anti-angiogenesis properties. Thus, this review is aimed at emphasizing the biological effect and mode of action of curcumin on CRC. Furthermore, the critical role of these substances in CRC chemoprevention was emphasized.
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In recent years, many studies have been conducted to develop functional meat products, focusing on strategies to maximize health-promoting compounds and reduce the presence of those that may cause negative impacts on the consumer's health. As such, the use of prebiotic, probiotic, and synbiotic agents in meat products has grown considerably. In addition, the use of new generation probiotics in meat products is a novel field that can be explored. With the most recent paraprobiotics/postbiotics update, several components could be tested in meat products. Some interventional studies using meat products added with biotic agents have shown great potential as functional foods by reducing the formation of nitrous compounds in the gut and improving the functionality of the gut microbiota. Although there are few studies focusing on synbiotic meat products, the results are also very promising in this field. As such, this review seeks to describe how probiotics, prebiotics, paraprobiotics and postbiotics can be employed in meat products to give them functional properties, as well as some of the major issues that may arise when using these agents.