二氢杨梅素(Dihydromyricetin) - 药物靶点：PB2_在研适应症：2型糖尿病，酒精相关疾病，酒精性肝疾病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

(+)-ampelopsin、(+)-dihydromyricetin、Ampelopsin

+ [2]

靶点

PB2

作用机制

PB2抑制剂(流感病毒PB2蛋白抑制剂)

治疗领域

内分泌与代谢疾病消化系统疾病其他疾病+ [2]

在研适应症

2型糖尿病酒精相关疾病酒精性肝疾病+ [1]

非在研适应症-

原研机构

University of Guadalajara

在研机构

University of Southern California

University of Guadalajara

南方医科大学

非在研机构-

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)临床前

特殊审评-

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结构

分子式C15H12O8

InChIKeyKJXSIXMJHKAJOD-LSDHHAIUSA-N

CAS号27200-12-0

关联

4

项与二氢杨梅素相关的临床试验

NCT05623501 / Not yet recruiting临床1期IIT

Phase I, Dose-Escalation Study of Dihydromyricetin (DHM) to Treat Alcohol-Associated Liver Disease

The current proposal is designed as a first-in-human Phase 1 open-label, dose-escalation study to assess the safety, pharmacokinetics, and the maximum tolerated dose of DHM among healthy volunteers using a purified form of DHM from a local cGMP compliant source (Master Herbs, Inc).

开始日期2024-09-15

申办/合作机构

University of Southern California

JPRN-UMIN000042938 / Completed

Investigation of ampelopsin absorption by different dosage forms: An open-label, randomized, three-drug, three-period, Latin square design, crossover study - Investigation of ampelopsin absorption by different dosage forms

开始日期2021-01-07

申办/合作机构

FANCL Corp.

NCT03606694 / Active, not recruiting临床2期IIT

Effect of Dihydromirycetin Administration on Glycemic Control, Insulin Sensitivity and Insulin Secretion in Patients With Type 2 Diabetes Mellitus

Dihydromyricetin has demonstrated promising effects in glycemic control, insulin sensitivity and insulin secretion, that above mentioned findings show that dihydromyricetin has an excellent potential effect in the treatment of type 2 diabetes mellitus patients.

开始日期2019-10-30

申办/合作机构

University of Guadalajara

100 项与二氢杨梅素相关的临床结果

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100 项与二氢杨梅素相关的转化医学

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100 项与二氢杨梅素相关的专利（医药）

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673

项与二氢杨梅素相关的文献（医药）

2025-02-01·Non-coding RNA Research

Molecular insight of miRNA-217 role in the pathogenesis of myocardial infarction: Promising diagnostic biomarker and therapeutic target

Article

作者: Zaafan, Mai A ; Zaafan, Mai A. ; Abdelhamid, Amr M. ; Abdelhamid, Amr M

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.

2025-01-01·Food Chemistry

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

Article

作者: 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.

2024-12-31·Journal of Enzyme Inhibition and Medicinal Chemistry

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

Article

作者: 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 项与二氢杨梅素相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
2型糖尿病	临床2期	墨西哥	University of Guadalajara	2019-10-30
酒精相关疾病	临床1期	-	University of Southern California	2024-09-15
酒精性肝疾病	临床1期	-	University of Southern California	2024-09-15
流感病毒感染	临床前	中国	南方医科大学	2020-07-01