Combination of catechin, epicatechin, and rutin : Optimization of a novel complete antidiabetic formulation using a mixture design approach

Nowadays, synthetic chemical antidiabetic drugs, besides their therapeutic effects, present adverse effects that could be hard to handle over time. In the last decade, studies reported new alternative molecules with more health benefits and less adverse effects. The goal of this study is to optimize a new antidiabetic formulation using plant flavonoids: Catechin, Epicatechin, and Rutin. They are also a powerful antioxidant and anti-inflammatory molecules. A mixture design experiment will optimize their combination to obtain a new, safe multi-targets antidiabetic formulation making it a powerful combination for the management of diabetes and its complications. To study the variation of blood glucose level in response to the treatment over the time we performed an Oral Glucose Tolerance Test. The blood glucose level variations recorded as responses for the mixture design experiment. We used the molecules at a dose of 10 mg/kg. According to the software analysis, the prediction profiler showed us the optimum combination, and the result was a binary combination between Rutin and Epicatechin (25% and 75%, respectively). This combination prevented hyperglycemia and hypoglycemia, along with the best area under the curve, and after that, we validated it through a repeated oral administration on alloxan-induced diabetic mice for 28 d. Rutin, Catechin, and Epicatechin exhibit a potent antihyperglycemic activity, their synergistic combination validates a new formulation that could be a real candidate to conventional drugs. (C) 2020 Elsevier Inc. All rights reserved.Peer reviewe

Synthesis, molecular docking studies, and larvicidal activity evaluation of new fluorinated neonicotinoids against Anopheles darlingi larvae

Anopheles darlingi is the main vector of malaria in Brazil, characterized by a high level of anthropophilia and endophagy. Imidacloprid, thiacloprid, and acetamiprid are the most widespread insecticides of the neonicotinoid group. However, they produce adverse effects on the non-target insects. Flupyradifurone has been marketed as an alternative to non-fluorinated neonicotinoids. Neonicotinoids containing trifluoroacethyl substituent reveal increased insecticidal activity due to higher hydrophobicity and metabolic stability. We synthesized novel neonicotinoid insecticides containing fluorinated acceptor groups and their interactions were estimated with the nicotinic acetylcholine receptor (nAChR) binding site by molecular docking studies, to evaluate their larvicidal activity against A. darlingi, and to assess their outdoor photodegradation behavior. New neonicotinoid analogues were prepared and characterized by NMR and mass-spectrometry. The synthesized molecules were modelled by time-dependent density functional theory and analyzed, their interaction with nAChR was investigated by molecular docking. Their insecticide activity was tested on Anopheles larvae collected in suburban area of Manaus, Brazil. Four new fluorinated neonicotinoid analogs were prepared and tested against 3rd instars larvae of A. darlingi showing high larvicidal activity. Docking studies reveal binding modes of the synthesized compounds and suggest that their insecticidal potency is governed by specific interactions with the receptor binding site and enhanced lipophilicity. 2-Chloro-5-(2-trifluoromethyl-pyrrolidin-1-ylmethyl)pyridine 5 showed fast degradation in water maintaining high larvicidal activity. All obtained substances possessed high larvicidal activity in low concentrations in 48 hours of exposure, compared to commercial flupyradifurone. Such activity is connected to a unique binding pattern of the synthesized compounds to insect’s nAChR and to their enhanced bioavailability owing to introduction of fluorinated amino-moieties. Therefore, the compounds in question have a high potential for application as control agents for insects transmitting tropical diseases, and they will be less persistent in the environment.Peer reviewe

Ethnobotanical survey about the management of diabetes with medicinal plants used by diabetic patients in Region of Fez-Meknes, Morocco

Background: Diabetes mellitus is a major public health problem in Morocco with more than 1.6 million cases of diabetes in 2017 with an expectation to rise to over 2.7 million cases in 2045. The aim of this work is to provide ethnobotanical information on some of the medicinal plants used by diabetic patients to treat their illness in the region of Fez-Meknes (Morocco). Methods: A semi-structured and simple questionnaire was carried out. A total of 422 interviews were conducted with diabetic patients presented to diagnosis in the Hassan II Hospital center in Fez in Morocco. The data were analyzed through use value (UV) and relative frequency of citations (RFC). Results: In total, 50 plant species belonging to 27 families were reported. Lamiaceae (14%), Apiaceae (12%) and Fabaceae (12%) were reported as the most represented families. Among the collected species, 6 plants were reported for the first time as antidiabetic plants in Morocco. The most frequently cited plant species are Trigonella foenum graecum (8.41%), Olea europaea (7.71%) and runus amygdalus var. amara (7.71%). Almost 67% and 33% of diabetic patient use medicinal plants as a complement and alternatives to their medication respectively. Conclusion: This study showed the importance of medicinal plants in the healthcare system for treating diabetes. Knowledge of the use of medicinal plants that are used to manage diabetes may contribute to their preservation and to undertake further pharmacological studies.Peer reviewe

Boosted Antioxidant Effect Using a Combinatory Approach with Essential Oils from Origanum compactum, Origanum majorana, Thymus serpyllum, Mentha spicata, Myrtus communis, and Artemisia herba-alba: Mixture Design Optimization

Several studies have demonstrated the possible synergistic effect as an effective strategy to boost the bioactivity of essential oils. Using this framework, this study was conducted to effectively establish the ideal combination of six essential oils from different plants (Origanum compactum, Origanum majorana, Thymus serpyllum, Mentha spicata, Myrtus communis, and Artemisia herba-alba) that would express the best antioxidant activity. Each mixture was optimized using a mixture design approach to generate the most effective blend. The 2,2-diphenyl-1-picrylhydrazyl radical scavenging method was used as a reference method to assess the antioxidant activity. Each essential oil’s composition was identified using the GC/MS method. The single essential oil activities demonstrated variable antioxidant effects, and following the mixture design approach, the optimal antioxidant blend was revealed, as two mixtures demonstrated the best antiradical activity with 79.46% obtained with the mixture of O. majorana (28%) and M. spicata (71%) and 78.8% obtained with the mixture O. compactum (64%), O. majorana (13%), and T. serpyllum (21%). This study proposes a practical way to elaborate mixtures in the search for a boosting effect that can be oriented for the food or pharmaceutical industry

Boosted Antioxidant Effect Using a Combinatory Approach with Essential Oils from Origanum compactum, Origanum majorana, Thymus serpyllum, Mentha spicata, Myrtus communis, and Artemisia herba-alba: Mixture Design Optimization

Several studies have demonstrated the possible synergistic effect as an effective strategy to boost the bioactivity of essential oils. Using this framework, this study was conducted to effectively establish the ideal combination of six essential oils from different plants (Origanum compactum, Origanum majorana, Thymus serpyllum, Mentha spicata, Myrtus communis, and Artemisia herba-alba) that would express the best antioxidant activity. Each mixture was optimized using a mixture design approach to generate the most effective blend. The 2,2-diphenyl-1-picrylhydrazyl radical scavenging method was used as a reference method to assess the antioxidant activity. Each essential oil’s composition was identified using the GC/MS method. The single essential oil activities demonstrated variable antioxidant effects, and following the mixture design approach, the optimal antioxidant blend was revealed, as two mixtures demonstrated the best antiradical activity with 79.46% obtained with the mixture of O. majorana (28%) and M. spicata (71%) and 78.8% obtained with the mixture O. compactum (64%), O. majorana (13%), and T. serpyllum (21%). This study proposes a practical way to elaborate mixtures in the search for a boosting effect that can be oriented for the food or pharmaceutical industry

Optimized Antibacterial Effects in a Designed Mixture of Essential Oils of Myrtus communis, Artemisia herba-alba and Thymus serpyllum for Wide Range of Applications

Nowadays, the combination of molecules influences their biological effects, and interesting outcomes can be obtained from different component interactions. Using a mixture design method, this research seeks to simulate the efficacy of essential oil combinations against various bacteria and forecast the ideal combination. The chemical compositions of Myrtus communis, Artemisia herba-alba and Thymus serpyllum essential oils were analyzed using CG/MS. Then, the combined antibacterial effects were evaluated by testing mixture design formulations using the microdilution bioassay. The main compounds detected for M. communis essential oil were myrtenyl acetate (33.67%), linalool (19.77%) and 1,8-cineole (10.65%). A. herba-alba had piperitone as a chemotype, representing 85%. By contrast, the T. serpyllum oil contained thymol (17.29%), gamma-terpinene (18.31%) and p-cymene (36.15%). The antibacterial effect of the essential oils studied, and the optimum mixtures obtained were target strain-dependent. T. serpyllum alone ensured the optimal inhibition against S. aureus and E. coli, while a ternary mixture consisting of 17.1%, 39.6% and 43.1% of M. communis, A. herba-alba and T. serpyllum respectively, was associated with optimal inhibitory activity against B. subtilis. The outcome of this research supports the idea of the boosting effect of essential oil combinations toward better activities, giving better understanding of the usefulness of mixture designs for food, cosmetics, and pharmaceutical applications.Peer reviewe

Eco-friendly recycled polypropylene matrix composites incorporated with geopolymer concrete waste particles

Civil construction wastes have been incorporated into polymers for recycling as novel engineering composites. In the present work eco-friendly composites with recycled polypropylene (rPP) matrix incorporated with geopolymer concrete waste particles, wither plain (GCW) or surface-modified with oleic acid (AGC) were investigated. The geopolymer concrete waste particles were mixed with polymer powder to provide an effective dispersion between the different materials. Composites were produced by an initial reactive extrusion processing followed by injection molding. These novel composites with amount of 20, 40 and 50 wt% of GCW particles, both plain as-received and surface-modified, were technically evaluated by tensile tests, statistically analyzed by ANOVA, as well as by water absorption as per ASTM standards. Surface dispersion of nanoparticles was revealed by atomic force microscopy. Microstructural analysis was performed by scanning electron microscopy. The results indicated that these sustainable GCW particles incorporated into rPP matrix exhibit superior processability and water absorption less than 0.01%. The rPP/AGC composites present relatively higher elastic modulus, 629 MPa, as compared to the neat rPP, with 529 MPa. These properties suggest potential sustainable applications in building construction using waste materials.Peer reviewe

Ethnobotanical Survey of Medicinal Plants Used in the Traditional Treatment of Depression and Anxiety in Fez-Meknes Region

Depression and anxiety represent a major mental health problem in the world. The majority of Moroccan people use traditional medicine for their health needs, including various forms of depression and anxiety. The aim of this work is to make an inventory of plant species used in folk medicine for the management of depression and anxiety in Fez-Meknes regions. Established questionnaires were administered to 243 interviews in 4 communities within Fez-Meknes region. With traditional health practitioners, herbalists and consumer. Plant species belonging to 31 families were reported. The most frequently cited families are Lamiaceae followed by Asteraceae, Apiaceae and Verbenaceae. Leaves were the major plant parts used forming 58% solely and 73 mixed with other parts. This was followed by seeds 17%, flowers 6%, roots 2% and fruits, bark (1% each). The current survey represents a useful documentation, which can use to preserving knowledge on the use of medicinal plants in this region and to explore the phytochemical and pharmacological potential of medicinal plants.Peer reviewe

Optimized Antibacterial Effects in a Designed Mixture of Essential Oils of Myrtus communis, Artemisia herba-alba and Thymus serpyllum for Wide Range of Applications

Nowadays, the combination of molecules influences their biological effects, and interesting outcomes can be obtained from different component interactions. Using a mixture design method, this research seeks to simulate the efficacy of essential oil combinations against various bacteria and forecast the ideal combination. The chemical compositions of Myrtus communis, Artemisia herba-alba and Thymus serpyllum essential oils were analyzed using CG/MS. Then, the combined antibacterial effects were evaluated by testing mixture design formulations using the microdilution bioassay. The main compounds detected for M. communis essential oil were myrtenyl acetate (33.67%), linalool (19.77%) and 1,8-cineole (10.65%). A. herba-alba had piperitone as a chemotype, representing 85%. By contrast, the T. serpyllum oil contained thymol (17.29%), γ-terpinene (18.31%) and p-cymene (36.15%). The antibacterial effect of the essential oils studied, and the optimum mixtures obtained were target strain-dependent. T. serpyllum alone ensured the optimal inhibition against S. aureus and E. coli, while a ternary mixture consisting of 17.1%, 39.6% and 43.1% of M. communis, A. herba-alba and T. serpyllum respectively, was associated with optimal inhibitory activity against B. subtilis. The outcome of this research supports the idea of the boosting effect of essential oil combinations toward better activities, giving better understanding of the usefulness of mixture designs for food, cosmetics, and pharmaceutical applications

Marketing and legal status of phytomedicines and food supplements in Morocco

Publisher Copyright: © 2020 Walter de Gruyter GmbH, Berlin/Boston.The Phytomedicine (PM) and Food supplements (FS) Market is considerably growing in Morocco a review of state is necessarily to structure and improve it. Information was collected directly from the pharmacist through a questionnaire-based survey who was conducted in 284 pharmacies in the region of Fez-Meknes in Morocco. Data were analyzed and classified using relative frequency of citations (RFC). More than 98% of the pharmacies commercialized the PM and FS, 80% of the pharmacists deny the existence of a real area dedicated to them, the majority (94%) of them prefer phytomedicine rather than classic drugs. This study reported about 64 products as the most used by the population of the region of Fez-Meknes among them 48 FS (75%) and 16 PM (25%) and the most marketed products are used for Transit Disorders (28.34%), then Anxiety (22.17%) and ENT Disease (20.18%). Despite the fact that Morocco is a country where people use medicinal plants daily, the commercialization of the PM and FS is still unstructured. Due to legal problem the PM Sold in the market are mainly exported. To assure development and also valorization of this sector the regulation of this market is highly required.Peer reviewe