Delving into the Latest Updates on Pinocembrin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

5,7-Dihydroxyflavanone, 7-Dihydroxyflavanone, DL-0108

Target

5α-reductase x AR

Action

inhibitors, agonists

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

License Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC15H12O4

InChIKeyURFCJEUYXNAHFI-UHFFFAOYSA-N

CAS Registry68745-38-0

After stroke, there is a high incidence of acute lung injury and impairment of intestinal barrier function. In this research, the effects of pinocembrin on organ injuries induced by cerebral ischemia-reperfusion were investigated in mice with middle cerebral artery occlusion/reperfusion (MCAO/R) and further explored the possible mechanism. The potential targets of pinocembrin against MCAO/R were obtained by online tools. An MCAO/R model was developed in C57BL/6 J mice, in combination with pinocembrin administration and lentivirus-mediated gene intervention. Pinocembrin alleviated neurological impairment, reduced the volume of cerebral infarction, attenuated pathological injury of brain tissues in MCAO/R-induced mice by promoting the expression of dipeptidyl peptidase 9 (DPP9), and blocked the nucleotide-binding domain leucine-rich repeat pyrin domain containing 1 (NLRP1) inflammasome activation. Moreover, pinocembrin attenuated the infiltration of inflammatory cells in the lungs and intestinal histopathological injury induced by MCAO/R. The above effects of pinocembrin were reversed by knocking down DPP9. These findings indicated that pinocembrin inhibits NLRP1 inflammasome activation by inducing DPP9, thus mitigating brain, lung, and intestinal injuries induced by MCAO/R.

01 Jul 2025·ARCHIVES OF ORAL BIOLOGY

Comparison of dose and time effects of flavonoids, alone or in combination, on the induction of mineralization markers in human osteoblast-like cells

Article

Author: de Souza, Maria Eduarda ; Peres, Geórgia Rondó ; Duque, Cristiane ; Rabelo, Rafaela Laruzo ; Rios, Rafael Araújo ; Braga, Gabriela Pacheco de Almeida ; Nunes, Gabriel Pereira

OBJECTIVE:

This study compared the cytotoxicity, alkaline phosphatase (ALP) activity, and mineralization-inducing effects of flavonoids on human osteoblast-like Saos-2 cells.

DESIGN:

Saos-2 cells were treated with quercetin, myricetin, pinocembrin, kaempferol, isoquercitrin (Iso), rutin (Rut), taxifolin (Tax), ampelopsin (Amp), epigallocatechin-3-gallate (EGCG), and chrysin at 100, 50, and 25 µM for 48 h. Metabolic activity, ALP activity and mineral deposition were assessed via resazurin, thymolphthalein and Alizarin Red S staining assays, respectively, after 8 and 14 days. Calcium hydroxide was used as positive control, and untreated cells (DMEM) as negative control. Based on initial screening, Tax, Iso, Rut and Amp were selected for double combination treatments (at 50/50 µM and at 25/25 µM), and the same assays were performed. Data were analyzed using ANOVA and Tukey's test (α = 0.05).

RESULTS:

Comparing the flavonoids, regardless of time and concentration, only chrysin at 100 µM and 50 µM significantly reduced cell viability. Iso, Rut, Tax, and Amp exhibited the highest ALP activity and mineralized nodules formation, significantly outperforming the other flavonoids and DMEM control, particularly at 50 and 25 µM (p < 0.05). Among the combinations, Tax+Iso, Tax+Amp and Tax+Rut, at 25/25 µM demonstrated higher ALP activity and enhanced mineral deposition compared to the other flavonoid combinations and DMEM (p < 0.05).

CONCLUSIONS:

Based on this preliminary in vitro model, Tax, Iso, Rut, and Amp, both individually and in combination, effectively promote biomineralization in Saos-2 cells, without inducing cytotoxic effects. These flavonoids hold significant potential for osteogenic applications, warranting further in vivo studies and clinical trials to optimize their therapeutic use.

01 May 2025·JOURNAL OF ETHNOPHARMACOLOGY

Identification of potential markers of elevated anticandidal activity of propolis extracts

Article

Author: Okińczyc, Piotr ; Szweda, Piotr ; Kuś, Piotr Marek ; Van Dijck, Patrick ; Bollin, Piotr

ETHNOPHARMACOLOGICAL RELEVANCE:

For centuries, propolis has been one of the most important and popular antimicrobial (antibacterial and antifungal) agents used in traditional medicine worldwide, including Central and Eastern Europe. Despite centuries of use of this product, the molecular mechanisms of its activity remain not fully recognized, and the components that determine its biological activity have not been identified.

AIM OF THE STUDY:

Hence, the main goal of the present study was to identify propolis ingredients that are crucial for the antifungal activity of this product.

MATERIALS AND METHODS:

A serial two-fold microdilution method was applied to evaluate the activity of 83 ethanolic extracts of propolis (EEP) samples collected in different regions of Poland. The chemical composition of all EEPs was determined using UHPLC-DAD and UHPLC-QqTOF-MS methods. Advanced chemometric analysis of the correlation between antifungal activity and chemical composition was performed to identify the components related to the increased antifungal potential of propolis. Subsequently, the antifungal activities of pure "active ingredients" and their combinations were determined.

RESULTS:

Only seven extracts (8.4 %) exhibited high anticandidal potential with MIC (Minimum Inhibitory Concentration) values between 32 and 256 μg/mL. The identified most important potential markers related to increased antifungal activity of propolis collected in East Europe are: pinocembrin, pinobanksin-3-acetate, chrysin, galangin, pinobanksin, techtochrysin, genkwanin, pinostrobin and sakuranetin isomer. However, the pure compounds did not inhibit the growth of Candida spp. up to a concentration of 256 μg/mL (MIC >256 μg/mL). Much better activity was observed for combinations of these ingredients. The highest activity was observed for a mixture of five compounds: chrysin, galangin, pinocembrin, pinobanksin, and pinobanksin-3-acetate, with MIC and MFC (Minimal Fungicidal Concentration) values 64 and 128 μg/mL (summary concentration of all compounds - 12.8 or 25.6 of each μg/mL), respectively.

CONCLUSIONS:

The relatively low number of propolis samples collected in Poland exhibit considerable activity against Candida spp. Markers of elevated antifungal potential have been identified. Moreover, it has been proved, that only the composition of these compounds (not pure ingredients alone) is effective in the treatment of Candida spp. Mixtures of these ingredients can be considered as potential antifungal agents (artificial propolis). Moreover, UHPLC-DAD and UHPLC-QqTOF-MS methods of determining the chemical composition of EEPs have been optimized.

100 Deals associated with Pinocembrin

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External Link

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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	China	CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.	02 Dec 2013
Ischemic stroke	Phase 2	China	CSPC Zhongqi Pharmaceutical Technology (Tianjin) Co., Ltd.	01 Jun 2013
Brain Infarction	Phase 2	China	Chinese Academy of Medical Sciences	-
Brain Infarction	Phase 2	China	CSPC Pharmaceutical Group Ltd.	-