Delving into the Latest Updates on Pinocembrin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

5,7-Dihydroxyflavanone, 7-Dihydroxyflavanone

Target

5α-reductase x AR

Mechanism

5α-reductase inhibitors(Steroid 5 alpha reductase inhibitors), AR agonists(Androgen Receptor agonists)

Therapeutic Areas

Nervous System DiseasesCardiovascular Diseases

Active Indication

Acute Ischemic Stroke

Inactive Indication

Brain Infarction

Originator Organization

Chinese Academy of Medical Sciences

Active Organization

CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.

Inactive Organization

CSPC Pharmaceutical Group Ltd.

CSPC Zhongqi Pharmaceutical Technology (Tianjin) Co., Ltd.

Chinese Academy of Medical Sciences

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC15H12O4

InChIKeyURFCJEUYXNAHFI-UHFFFAOYSA-N

CAS Registry68745-38-0

The iron-sulfur domain (CISD) proteins of CDGSH are classified into three classes: CISD1, CISD2, and CISD3. During premature ageing, mutations that affect these proteins, namely their binding sites, could result in reduced protein production and an inability to preserve cellular integrity. Consequently, this leads to the development of conditions such as diabetes. Notably, CISD3 plays a crucial role in the management of age-related disorders such as Wolfram syndrome, which is often referred to as DIDMOAD (diabetes insipidus, diabetes mellitus, optic atrophy, and deafness). Computational analyses have predicted that CISD3 regulates the redox state, safeguards the endoplasmic reticulum and mitochondria, and maintains intracellular calcium levels. CISD3, a member of a recently discovered gene family associated with the CDGSH iron protein apoptotic compensatory response, fulfils a crucial function in mitigating the effects of accelerated ageing. The compound "(-)-(2S)-7,4'-Dihydroxyflavanone" has been discovered by computational drug design as a possible activator of CISD3. It shows potential therapeutic benefits in ameliorating metabolic dysfunction and enhancing glucose regulation. The ligand binds to the binding pocket of the CISD3 protein, increasing the stability of the protein and enhancing its functionality. The current research investigates the binding processes of the molecule in various structures and its anticipated effects on these tissues, therefore providing valuable insights into the mitigation of age-related diabetes and metabolic dysfunction. The projected tripling of the worldwide population of individuals aged 50 and above by 2050 necessitates the urgent development of immunoinformatics-based approaches, including pharmaceutical therapies that target CISD3, to prevent age-related pathologies. The stimulation of CISD3, namely by compounds such as "(-)-(2S)-7,4'-Dihydroxyflavanone", has the potential to counteract telomere shortening and improve metabolic pathways.

01 Jan 2025·Neuroscience Letters

Effects of lateral ventricle injection of 5,7-dihydroxytryptamine on neurons in the medial prefrontal cortex of rats: An electrophysiology study

Article

Author: Liu, Yuanyuan ; Hao, Xueqin ; Deng, Bo ; Fan, Lingling ; Qiu, Xiangjun

The medial prefrontal cortex (mPFC) is closely associated with various psychopathologies in humans, and its dysfunction is invariably accompanied by abnormalities in the serotonin (5-hydroxytryptamine, 5-HT) system of the brain. In this study, in-vivo extracellular recording techniques were used to investigate changes in the excitability of pyramidal neurons and interneurons in the rat mPFC following injection of 5,7-dihydroxytryptamine (5,7-DHT) into the bilateral lateral ventricles to damage the serotoninergic neurons. The levels of 5-HT in the mPFC and dorsal raphe nucleus of rats were determined by high-performance liquid chromatography. The results showed that the levels of 5-HT were significantly reduced in the mPFC and dorsal raphe nucleus two weeks after injection of 5,7-DHT into the bilateral lateral ventricles, relative to the normal group. The discharge frequency of pyramidal neurons in the mPFC was markedly increased compared to the normal group, with a significant rise in burst discharge, while the average discharge frequency of interneurons was significantly reduced and tended towards irregular activity. The results of the study indicated that the brain's 5-HT neurotransmitter system not only directly affects the activity of mPFC pyramidal neurons but also modulates the electrical activity of interneurons, thereby regulating the local microcircuitry within the mPFC and participating in its function.

01 Jan 2025·Fitoterapia

Development of therapeutic and cosmetic cream based on flavonoids

Article

Author: Savchenko, D L ; Adekenov, S M ; Kenzhebekov, A.O. ; Zhabaeva, A.N. ; Zhabaeva, A N ; Adekenova, A.S. ; Polyakov, V V ; Savchenko, D.L. ; Polyakov, V.V. ; Adekenov, S.M. ; Kenzhebekov, A O ; Adekenova, A S

The article discusses the results of the development of a cream based on Populus balsamifera L. bud flavonoids, which have anti-inflammatory, skin-regenerating effects. A cream's anti-inflammatory and wound-healing activity based on a flavonoid substance has been studied. In an experiment on a model of an incised skin wound, it was determined that a cream based on the sum of flavonoids from balsam poplar buds, containing pinostrobin, pinocembrin, tectochrysin, exhibits anti-inflammatory and wound-healing activities. Considering that the effectiveness of local wound treatment mainly depends on the rational treatment of the first phase of the wound process, we have developed a 1 % flavonoid cream and its production technology. The technology for the production of flavonoid cream includes extraction and isolation of the sum of flavonoids from the raw material of Populus balsamifera L. buds, preparation of flavonoid substance and excipients, preparation of the cream base and cream, packaging and labelling of cream. Based on the results of our experiments, a pilot industrial regulation for the production of a new cream based on the sum of flavonoids of Populus balsamifera L. buds has been developed, and pilot production of an original medicinal and cosmetic cream was organised.

100 Deals associated with Pinocembrin

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External Link

KEGG	Wiki	ATC	Drug Bank
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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute Ischemic Stroke	Phase 2	CN	CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.	02 Dec 2013
Ischemic stroke	Phase 1	CN	CSPC Zhongqi Pharmaceutical Technology (Tianjin) Co., Ltd.	01 Jun 2013
Brain Infarction	Discovery	CN	CSPC Pharmaceutical Group Ltd.	-
Brain Infarction	Discovery	CN	Chinese Academy of Medical Sciences	-