Delving into the Latest Updates on Dihydromyricetin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(+)-ampelopsin, (+)-dihydromyricetin, Ampelopsin

+ [2]

Target

PB2

Mechanism

PB2 inhibitors(polymerase basic protein 2 (PB2) inhibitors)

Therapeutic Areas

Endocrinology and Metabolic DiseaseDigestive System DisordersOther Diseases+ [2]

Active Indication

Diabetes Mellitus, Type 2Alcohol-Related DisordersLiver Diseases, Alcoholic+ [1]

Inactive Indication-

Originator Organization

University of Guadalajara

Active Organization

University of Southern California

University of Guadalajara

Southern Medical University

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC15H12O8

InChIKeyKJXSIXMJHKAJOD-LSDHHAIUSA-N

CAS Registry27200-12-0

BackgroundGlobally, myocardial infarction (MI) is one of the main causes of death. This study aims to investigate the role of miR-217 in the pathogenesis through targeting MAPK and PI3K/AKT signaling pathways in experimental model of myocardial infarction and studying the possible cardioprotective role of dihydromyricetin (DHM) through modulation of this pathway.MethodsDihydromyricetin was injected (100 mg/kg; p.o.) in isoprenaline induced myocardial infarction rat model for 14 days. Rats were anaesthetized and blood samples were taken for serum separation, estimation of creatine kinase-MB (CK-MB), and troponin-I levels after 24 h had passed since the last isoprenaline injection. In addition, the hearts were also used for the other biochemical studies and the histological evaluation.ResultsDHM resulted in a significant suppression of the elevated levels miR-217 and MAPK compared to the MI control group and restored the normal level of serum CK-MB. Furthermore, DHM successfully restored the oxidative balance and halted the pro-inflammatory mediators in the cardiac tissue.ConclusionAccordingly, our experiment emphasizes the anti-ischemic property that has been demonstrated through modulation of expression level of miR-217 and consequent deactivation of MAPK and PI3K/AKT signaling pathways, and this was assured by halting downstream pro-inflammatory markers.

01 Jan 2025·Food Chemistry

Natural α-glucosidase inhibitors from Aquilaria sinensis leaf-tea: Targeted bio-affinity screening, identification, and inhibition mechanism

Article

Author: Fei, Tao ; Lin, Xue ; Liu, Yingxin ; Li, Fangliang ; Wang, Lu ; Liu, Zhonghua

Aquilaria sinensis leaves have long been consumed as a popular replacement tea for lowering postprandial blood glucose levels, but their specific functional components remain unclear. In this study, Aquilaria sinensis leaf-tea 70 % ethanol extract (ALTE) exhibited excellent anti-α-glucosidase activity (IC₅₀ = 6.93 ± 1.91 μg/mL) and promoted glucose consumption ability in 3 T3-L1 preadipocyte cells. Subsequently phenolic compositions of ALTE were identified for the first time. After that, five potential α-glucosidase inhibitors (α-GIs) including cynaroside-3,5-diglucose, malvidin 3-glucose, epicatechin, epigallocatechin gallate, and dihydromyricetin in ALTE were screened using a targeted bio-affinity ultrafiltration-HPLC/MS method. Moreover, these five α-GIs all showed good anti-α-glucosidase effects and glucose consumption-promoting ability. Furthermore, the binding properties and inhibition mechanisms of five α-GIs to α-glucosidase were further analyzed via enzyme inhibition kinetics, molecular docking, and molecular dynamics simulation. This study confirms that Aquilaria sinensis leaf-tea is effective in preventing post-hyperglycemia in vitro models, suggesting potential for future research in human trials.

31 Dec 2024·Journal of Enzyme Inhibition and Medicinal Chemistry

Design, synthesis, and biological activity evaluation of dihydromyricetin derivatives against SARS-CoV-2-Omicron virus

Article

Author: Wu, Cong ; Liu, Chao ; Jiang, Qi ; Wang, Wei ; Pan, Tong ; Sheng, Wenbing ; Liu, Leping ; Zhou, Xudong ; Zhong, Hui

An oxidising and substituting one-pot reaction strategy has been developed to synthesise dihydromyricetin derivatives with the aim of enhancing the inhibitory activity of dihydromyricetin against SARS-CoV-2. Different ω-methoxy-ω-oxeylkyl was introduced in C₇-OH site and yielded eight analogs, all of them showed good inhibitory activity against SARS-CoV-2 3CL^pro with IC₅₀ values ranging from 0.72 to 2.36 μM. In the Vero E6-cell, compound 3 has a good activity of anti-SARS-CoV-2 virus (Omicron virus BA.5) in the prevention model, with an EC₅₀ of 15.84 μM, and so do compound 10 in the therapeutic model, with an EC₅₀ of 11.52 μM. The results suggest that the introduction of long chain ω-oxeylkyl at C₇-OH facilitate the inhibition of viral replication in the therapeutic model, which is consistent with the binding energies predicted from molecular docking conclusions. It implies that dihydromyricetin derivatives have the potential to become effective inhibitors of SARS-CoV-2 Omicron and other viruses.

100 Deals associated with Dihydromyricetin

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	Phase 2	MX	University of Guadalajara	30 Oct 2019
Alcohol-Related Disorders	Phase 1	-	University of Southern California	15 Sep 2024
Liver Diseases, Alcoholic	Phase 1	-	University of Southern California	15 Sep 2024
Influenza, Human	Preclinical	CN	Southern Medical University	01 Jul 2020