Video Experimental Relacionado

Updated: Sep 9, 2025

Cellular Membrane Affinity Chromatography Columns to Identify Specialized Plant Metabolites Interacting with Immobilized Tropomyosin Kinase Receptor B

Cellular Membrane Affinity Chromatography Columns to Identify Specialized Plant Metabolites Interacting with Immobilized Tropomyosin Kinase Receptor B

Published on: January 19, 2022

Moléculas de base de Schiff derivadas del piperonal como agentes terapéuticos potenciales multi-objetivo contra el

Asif Ahmad¹, Uzma Salar², Musa Özil³

¹Third World Center for Science and Technology, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.

Future medicinal chemistry

|August 30, 2025

Resumen

Las nuevas bases de Schiff derivadas del piperonal muestran una inhibición de doble acción contra las enzimas de la diabetes y el Alzheimer. Estos compuestos ofrecen una estrategia prometedora para desarrollar nuevas terapias para ambas afecciones.

Área de la Ciencia:

Química medicinal
La neurociencia
Farmacología

Sus antecedentes:

La co-ocurrencia de la diabetes mellitus (DM) y la enfermedad de Alzheimer (AD) requiere el desarrollo de agentes terapéuticos multifuncionales.
Las bases de Schiff derivadas de Piperonal se exploran por su potencial para atacar enzimas implicadas tanto en DM como en AD.

Objetivo del estudio:

Sintetizar y caracterizar nuevos derivados de la base de Schiff derivados del piperonal.
Evaluar el potencial inhibidor de estos derivados contra las enzimas claves de la DM (α-amilasa y α-glucosidasa) y la AD (acetilcolinesterasa y butirilcolinesterasa).
Para evaluar las propiedades antioxidantes de los compuestos sintetizados.

Principales métodos:

Síntesis y caracterización estructural de los derivados de base de Schiff derivados del piperonal.
Ensayos de inhibición de enzimas in vitro contra la α-amilasa, la α-glucosidasa, la acetilcolinesterasa y la butirilcolinesterasa.
Análisis cinéticos y estudios de acoplamiento molecular.
Evaluación de la actividad antioxidante.

Principales resultados:

Los compuestos 7 y 17 exhibieron una potente inhibición contra la α- glucosidasa y la α- amilasa, respectivamente, superando al fármaco estándar acarbosa.
Los compuestos 7 y 9 demostraron efectos inhibidores significativos contra la acetilcolinesterasa y la butirilcolinesterasa, respectivamente, superando la eficacia del cloruro de donepezil.
Los derivados sintetizados también mostraron un notable potencial antioxidante.

Conclusiones:

Varios derivados de la base de Schiff derivados del piperonal muestran prometedores efectos inhibidores de doble acción contra objetivos relevantes tanto para la diabetes como para la enfermedad de Alzheimer.
Estos compuestos representan candidatos potenciales para el desarrollo de nuevos agentes terapéuticos para el tratamiento de la DM y la EA comórbidas.
Se justifica un mayor desarrollo de estos candidatos a éxito.

Palabras clave:

Bases de Schiff derivadas del piperonal Acarbosa y sus derivados antialzhéimer Antidiabético el antioxidante el donepezil

Más Videos Relacionados

A11-positive β-amyloid Oligomer Preparation and Assessment Using Dot Blotting Analysis

A11-positive β-amyloid Oligomer Preparation and Assessment Using Dot Blotting Analysis

Published on: May 22, 2018

Establishment of a Valuable Mimic of Alzheimer's Disease in Rat Animal Model by Intracerebroventricular Injection of Composited Amyloid Beta Protein

Establishment of a Valuable Mimic of Alzheimer's Disease in Rat Animal Model by Intracerebroventricular Injection of Composited Amyloid Beta Protein

Published on: July 29, 2018

Videos de Conceptos Relacionados

Alzheimer's Disease: Treatment

Alzheimer's Disease: Treatment

Alzheimer's Disease (AD), a neurodegenerative disorder, is pathologically identified by amyloid plaques and neurofibrillary tangles composed of tau protein. AD pharmacotherapy aims to manage cognitive symptoms, delay disease progression, and treat behavioral symptoms. The treatment is primarily symptomatic and palliative, with no definitive disease-modifying therapy available. Cholinesterase inhibitors, including donepezil (Aricept), rivastigmine (Exelon), and galantamine (Razadyne), are...

siRNA - Small Interfering RNAs

siRNA - Small Interfering RNAs

Small interfering RNAs, or siRNAs, are short regulatory RNA molecules that can silence genes post-transcriptionally, as well as the transcriptional level in some cases. siRNAs are important for protecting cells against viral infections and silencing transposable genetic elements.
In the cytoplasm, siRNA is processed from a double-stranded RNA, which comes from either endogenous DNA transcription or exogenous sources like a virus. This double-stranded RNA is then cleaved by the...

Targets for Drug Action: Overview

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...

Alzheimer's Disease: Overview

Alzheimer's Disease: Overview

Alzheimer's Disease (AD) is a continually advancing neurodegenerative disorder, distinguished by escalating memory loss, cognitive dysfunction, and dementia. The disease unfolds in three stages: preclinical, mild cognitive impairment (MCI), and dementia. Its onset is insidious, and the progression gradual, with the cause not well explained by other disorders.
The clinical diagnosis of AD hinges on the presence of memory and other cognitive impairments. Biomarkers, such as changes in Aβ...

Glucagon-like Receptor Agonists

Glucagon-like Receptor Agonists

Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...

G Protein-coupled Receptors

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...