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1.
Chem Biodivers ; : e202401268, 2024 Aug 23.
Artículo en Inglés | MEDLINE | ID: mdl-39177000

RESUMEN

Water hyacinth (Eichhornia crassipes (Mart.) Solms) is a highly invasive aquatic weed native to the Amazonia basin, known for its rapid propagation, adaptability and utilization in traditional medicine. The study aims to unveil the therapeutic potential of water hyacinth flowers methanolic extract (EC-CME) and its four kupchan fractions (EC-PESF, EC-DCMSF, EC-EASF, EC-ASF) through diversified chemical-pharmacological approaches. GC-MS/MS of EC-CME uncovered a rich tapestry of 72 phytochemical components. In vitro DPPH scavenging assay and total phenolic content determination assay deciphered promising antioxidant assays with remarkably low IC50 values of 0.353 and 0.485 µg/mL, respectively for EC-ESF and EC-ASF. Besides, different in vivo tests, including tail emersion, acetic acid-induced writhing, and thiopental-induced sleeping test of EC-CME, yielded a remarkable 8.61 ± 0.29 minutes of tail immersion time compared to the control's 2.05 ± 0.11 minutes at the highest dose (600 mg/kg). The best % inhibition of writhing was recorded as 47.96% accrued in 400 mg/kg dose, indicating robust pain-relieving properties. The onset and duration of sleep are significantly ameliorated for EC-CME, unveiling its antidepressant potential. Besides, molecular docking studies along with ADME/T analysis also validated the wet lab findings as well as their safety, efficacy and drug-likeliness profile.

2.
Heliyon ; 10(6): e27533, 2024 Mar 30.
Artículo en Inglés | MEDLINE | ID: mdl-38496846

RESUMEN

Flavonoids are organic compounds characterized by a range of phenolic structures, which are abundantly present in various natural sources such as fruits, vegetables, cereals, bark, roots, stems, flowers, tea, and wine. The health advantages of these natural substances are renowned, and initiatives are being taken to extract the flavonoids. Apigenin, galangin, hesperetin, kaempferol, myricetin, naringenin, and quercetin are the seven most common compounds belonging to this class. A thorough analysis of bibliographic records from reliable sources including Google Scholar, Web of Science, PubMed, ScienceDirect, MEDLINE, and others was done to learn more about the biological activities of these flavonoids. These flavonoids appear to have promising anti-diabetic, anti-inflammatory, antibacterial, antioxidant, antiviral, cytotoxic, and lipid-lowering activities, according to evidence from in vitro, in vivo, and clinical research. The review contains recent trends, therapeutical interventions, and futuristic aspects of flavonoids to treat several diseases like diabetes, inflammation, bacterial and viral infections, cancers, and cardiovascular diseases. However, this manuscript should be handy in future drug discovery. Despite these encouraging findings, a notable gap exists in clinical research, hindering a comprehensive understanding of the effects of flavonoids at both high and low concentrations on human health. Future investigations should prioritize exploring bioavailability, given the potential for high inter-individual variation. As a starting point for further study on these flavonoids, this review paper may promote identifying and creating innovative therapeutic uses.

3.
Front Pharmacol ; 15: 1359815, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38487168

RESUMEN

Introduction: Plants and their extracts have been integral to the development of medicinal treatments throughout history, offering a vast array of compounds for innovative therapies. Baccaurea motleyana Müll. Arg., commonly known as Rambai, is an evergreen tree with economic importance in the Old-World Tropics. Method: The study investigates its phytochemical composition through Gas Chromatography-Mass Spectrometry (GC-MS) and evaluates its pharmacological properties, including antidiabetic, antidiarrheal, antimicrobial, and antidepressant effects. Result and Discussion: The GC-MS analysis revealed 15 bioactive compounds in the methanol extract, with Phenol, 3,5-bis(1,1-dimethylethyl)-, Methyl stearate, and Hexadecanoic acid, methyl ester being the predominant ones. The cytotoxicity assay demonstrated significant activity in the ethyl acetate fraction. Antimicrobial assays indicated mild to moderate antibacterial activity. In vivo studies on mice revealed significant hypoglycemic, antidiarrheal, and antidepressant properties. Molecular docking studies against EGFR, DHFR, GLUT-3, KOR, and MOA identified promising compounds with potential therapeutic effects. The identified compounds exhibited favorable ADME/T properties, emphasizing their potential for drug development. The study underscores the promising therapeutic potential of Baccaurea motleyana, showcasing its diverse bioactive compounds with significant medicinal properties. Conclusion: These findings lay the groundwork for future research, emphasizing the exploration of B. motleyana as a source of natural remedies for addressing prevalent health conditions.

4.
Biomed Res Int ; 2015: 731292, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-26579539

RESUMEN

The blood-brain barrier (BBB) is a dynamic and highly selective permeable interface between central nervous system (CNS) and periphery that regulates the brain homeostasis. Increasing evidences of neurological disorders and restricted drug delivery process in brain make BBB as special target for further study. At present, neurovascular unit (NVU) is a great interest and highlighted topic of pharmaceutical companies for CNS drug design and delivery approaches. Some recent advancement of pharmacology and computational biology makes it convenient to develop drugs within limited time and affordable cost. In this review, we briefly introduce current understanding of the NVU, including molecular and cellular composition, physiology, and regulatory function. We also discuss the recent technology and interaction of pharmacogenomics and bioinformatics for drug design and step towards personalized medicine. Additionally, we develop gene network due to understand NVU associated transporter proteins interactions that might be effective for understanding aetiology of neurological disorders and new target base protective therapies development and delivery.


Asunto(s)
Barrera Hematoencefálica/metabolismo , Sistemas de Liberación de Medicamentos/métodos , Diseño de Fármacos , Modelos Biológicos , Acoplamiento Neurovascular/fisiología , Farmacocinética , Animales , Simulación por Computador , Humanos , Acoplamiento Neurovascular/efectos de los fármacos
5.
Bioinformation ; 11(2): 67-72, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-25848166

RESUMEN

Normal blood glucose level depends on the availability of insulin and its ability to bind insulin receptor (IR) that regulates the downstream signaling pathway. Insulin sequence and blood glucose level usually vary among animals due to species specificity. The study of genetic variation of insulin, blood glucose level and diabetics symptoms development in Aves is interesting because of its optimal high blood glucose level than mammals. Therefore, it is of interest to study its evolutionary relationship with other mammals using sequence data. Hence, we compiled 32 Aves insulin from GenBank to compare its sequence-structure features with phylogeny for evolutionary inference. The analysis shows long conserved motifs (about 14 residues) for functional inference. These sequences show high leucine content (20%) with high instability index (>40). Amino acid position 11, 14, 16 and 20 are variable that may have contribution to binding to IR. We identified functionally critical variable residues in the dataset for possible genetic implication. Structural models of these sequences were developed for surface analysis towards functional representation. These data find application in the understanding of insulin function across species.

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