RESUMO
The incidences of endocrine and metabolic disorders like diabetes have increased worldwide. Several proposed molecular pathways mechanisms for the management of diabetes have been identified, but glycaemic control is still a challenging task in the drug discovery process. Most of the drug discovery processes lead to numerous scaffolds that are prominent in natural products. The review deals with the natural bioactives as an α-amylase inhibitors, α-glucosidase inhibitors, protein tyrosine phosphatase-1B inhibitors, dipeptidyl peptidase-IV inhibitors, G-protein coupled receptors-40 agonists, PPAR-γ agonists and the activators of 5'-adenosine monophosphate-activated protein kinase and glucokinase. So, in this review, we focused on the hypoglycaemic bioactives, which will assist scientific developers, traditional medicinal practitioners, and readers to discover some potent antidiabetic molecules. Strategies like chemometric approaches, scaffold hopping, and total synthesis of natural products by group modification or ring opening/closing mechanism could be useful for the development of novel hit/lead antidiabetic molecules. The study concludes that each phyto molecule inherits a potential to get explored by repurposing techniques for various antidiabetic targets and offer an alternative antidiabetic therapeutic medicinal potential.
RESUMO
With the aim of developing multidrug solids through a tuned crystal engineering approach, we have selected two antiurinary infective drugs, namely, nitrofurantoin (NF) and trimethoprim (TMP) and isolated eight binary drug-drug solid solvates along with a nonsolvated cocrystal. Crystal structure analyses were performed for eight of these solids and rationalized in terms of known supramolecular synthons formed by pyrimidine, imide, and amine functionalities. Notably, the TMP-NF anhydrous cocrystal and its ionic cocrystal hydrate exhibit enhanced equilibrium solubilities compared to pure NF or the simple NF hydrate. Furthermore, the ionic cocrystal hydrate exhibits greater antibacterial activity against the Gram-negative bacteria, E. coli, compared to the parent TMP and NF at the lowest concentration of 3.9 µg/mL. This study indicates initial pathways using the cocrystal methodology that would help to eventually arrive at an antiurinary cocrystal with optimal properties.
Assuntos
Anti-Infecciosos Urinários/química , Composição de Medicamentos/métodos , Nitrofurantoína/química , Trimetoprima/química , Anti-Infecciosos Urinários/farmacologia , Anti-Infecciosos Urinários/uso terapêutico , Química Farmacêutica/métodos , Cristalização , Combinação de Medicamentos , Escherichia coli/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Nitrofurantoína/farmacologia , Nitrofurantoína/uso terapêutico , Solubilidade , Trimetoprima/farmacologia , Trimetoprima/uso terapêutico , Infecções Urinárias/tratamento farmacológico , Infecções Urinárias/microbiologiaRESUMO
Balanites aegyptiaca Delile (BA) is an enduring xerophytic woody and spinous flowering tree and is commonly known as desert date or Ingudi (Hingot). It belongs to the family Zygophyllaceae, which is specific to be drought areas of Nigeria, Africa, South Asia and India (Rajasthan). In Ayurveda, this traditional medicinal plant is reported for the management of jaundice, syphilis, yellow fever, metabolic disorders, liver, and spleen problems. The main aim of the review is to compile its medicinal uses and further advancements to showcase the promises inherited in various parts of the plant for the benefit of mankind. As per the literature survey, various researchers have focused on the detailed investigation of BA including the phytopharmacological evidence, chemical constituents, nano-formulations, commercialized products, and clinical trials. Several remarkable scaffolds and isolated compounds like diosgenin, yamogenin, balanitin1/2, balanitin 3, bal4/5, bal6/7, rutin-3-glycosides, 3,7-diglycosides, (3, 12, 14, 16)-(12-hydroxycholest-5-ene-3,16-diyl-bis)-D-glucopyranoside and balanitoside have been identified. Additionally, this traditional plant has been scientifically proven by in vitro and in vivo. Based on the complete review of this plant, most of the compounds have been isolated from the fruit and kernel part. Additionally, based on the literature, a histogram was developed for pharmacological activity in which antidiabetic study was found to be more compared to other pharmacological activity. As a spinous desert dates, this plant needs to be explored more to bring out newer phytochemicals in the management of various diseases.
RESUMO
Vegetables, fruits, and spices have a pivotal role in maintaining the metabolism and have diversified health welfares. The food products have medicinal values (Medifood) and benefitted prophylactically and simultaneously; health experts recommend them due to their synergistic effect on medicine. Therefore, research thrusts have developed medifood and counted in the field of pharma-nutrition. Type II diabetes mellitus is one of the foremost progressive metabolic disorders, which affects several millions of people around the globe due to ignorance of food habits. Improvement in lifestyle and intake of habitual food may improve the diabetic conditions. In the present study, we performed in silico studies of fatty acids on the free fatty acid 1 receptor to identify fatty acids readily available in daily food content. Additionally, molecular dynamic simulation study to recognize the dynamic behavior of protein-fatty acid complex. The in silico results suggest that 04 fatty acids may be promising in which behenic acid was most potential and showed binding energy of - 110.857 kcal/mol. The stability of the protein-ligand complex is confirm in simulation studies, with occupancy of 95% and 84%, respectively. Behenic acid is present in different parts of the Moringa tree and may serve as medifood in type II diabetes mellitus.
Assuntos
Diabetes Mellitus Tipo 2 , Simulação de Dinâmica Molecular , Diabetes Mellitus Tipo 2/tratamento farmacológico , Ácidos Graxos , Humanos , VerdurasRESUMO
Due to changed lifestyle and other reasons, diabetes has become one of the common metabolic disorder of the globe. Numerous therapeutic options are available, which controls the plasma glucose levels. However, most of the drugs are associated with some undesired side effects. Owing to the side effects and enhanced understanding of the phytochemicals, an inclination toward herbal medicine is seen in the population. These herbal products are also associated with concerns like poor aqueous solubility, compromised permeation, and a low degree of bioavailability. So, the emergence of nanotechnology in the herbal medicine is required to nullify the associated concerns of conventional antidiabetic drugs. The present review aims to compile the literature available for the nano-interventions pertinent to herbal products for diabetes management.