Delving into the Latest Updates on Arecoline with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

mAChRs

Action

agonists

Mechanism

mAChRs agonists(Muscarinic acetylcholine receptor agonists)

Therapeutic Areas

Nervous System Diseases

Active Indication

Autistic Disorder

Inactive Indication

Alzheimer Disease

Originator Organization

Ferrosan Medical Devices A/S

Active Organization

Xiamen Xianyue Hospital

Inactive Organization

Ferrosan Medical Devices A/S

Cogent Elliott Ltd.

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC8H13NO2

InChIKeyHJJPJSXJAXAIPN-UHFFFAOYSA-N

CAS Registry63-75-2

To develop novel mosquito control agents, we designed and synthesized a series of derivatives based on the natural alkaloid arecoline as a lead compound, targeting muscarinic acetylcholine receptors (mAChRs). Using computer-aided drug design and docking techniques focused on mAChRs, we designed piperidine derivatives and screened for synthetically accessible candidates. The compounds were synthesized, structurally characterized, and evaluated for activity via a Fluo-4 calcium fluorescence assay using Chinese Hamster Ovary-K1 (CHO-K1) cells expressing the muscarinic acetylcholine receptor M1. Most compounds showed potent mAChRs agonist activity, with Half Maximal Effective Concentration (EC₅₀) values below 10 μM. In subsequent insecticidal activity tests, these piperidine derivatives exhibited strong larvicidal effects against Aedes aegypti. The Median Lethal Concentration (LC₅₀) values for compounds 1a, 2a, 3a, 4a, 13a, 22a, 2b, and 9b were 58.4, 29.6, 11.4, 21.7, 42.0, 61.7, 125.9, and 81.6 mg/L, respectively. Notably, compound 13a maintained high insecticidal activity even against pyrethroid-resistant mosquitoes, indicating a mode of action different from conventional neurotoxic insecticides. These results demonstrate that mAChR-targeting derivatives derived from betel alkaloids represent a promising strategy for developing new mosquito control agents and offer a novel approach to combating insecticide resistance.

01 Mar 2026·JOURNAL OF ORAL PATHOLOGY & MEDICINE

Stem Cell Secretome Reverse Areca Nut Extract Induced Fibrosis in Human Fibroblast and Patient‐Derived Biopsies

Article

Author: Pande, Nikhil ; Bhonde, Ramesh ; Sanap, Avinash ; Kheur, Supriya ; Potdar, Pranjali ; Takbhate, Bhagyashri ; Mante, Nishant ; Monga, Nitika ; Kharat, Avinash

ABSTRACT:

Background:

Oral submucous fibrosis is a progressive, oral potentially malignant condition that can affect the oral cavity and is often linked to areca nut consumption. This study aimed to investigate the potential of dental pulp mesenchymal stem cells secretome (DPMSCs‐S) in the reversal of areca nut‐induced fibrosis in human fibroblast cells and patient‐derived buccal mucosa tissues.

Materials and Methods:

The cytokine and growth factor levels in DPMSCs‐S were analyzed by flow cytometry. Cytotoxicity and apoptotic features were analyzed using a cell viability assay and microscopy, respectively. Cellular senescence and reactive oxygen species generation were assessed in human fibroblast cells using a β‐galactosidase assay and 2′,7′‐dichlorodihydrofluorescein diacetate probe, respectively. Fibrosis‐related gene expression (COL15A1, COL1, COL3, α‐SMA, TGFβ1, and TGFβ2) and protein expression (COL1 and Ki67) were assessed by RT‐PCR and fluorescence microscopy, respectively.

Results:

Areca nut extract and arecoline resulted in a dose‐dependent reduction in cell viability. Secretome treatment reduced cell death, apoptotic and senescent features in fibroblast cells exposed to areca nut extract and arecoline, decreased ROS levels, and significantly downregulated areca nut‐induced fibrotic gene expressions (COL15A1, COL3, α‐SMA, TGFβ2), and protein expression of COL1. Heat‐inactivated secretome retained the activity, implying the involvement of heat‐stable biomolecules in the reversal of fibrosis. Ex vivo results corroborated these findings, with reduced expression of COL15A1, COL3, and α‐SMA in buccal tissues from oral submucous fibrosis patients treated with DPMSCs‐S.

Conclusion:

Secretome exhibited promising cytoprotective and anti‐fibrotic properties, reduction in cell death, senescence, collagen expression, and oxidative stress. These findings support the potential of secretome as a novel therapeutic candidate for oral submucous fibrosis, meriting further investigation in preclinical and clinical trials.

01 Feb 2026·INTERNATIONAL DENTAL JOURNAL

Curcumin suppresses EMT to alleviate oral submucous fibrosis progression through XIST/miR-25-3p-mediated inactivation of the TGF-β1/Smads signalling pathway

Article

Author: Liu, Yao ; Liu, Jian ; Min, Qian ; Zhao, Yue ; Qin, Jian

BACKGROUND:

Oral submucous fibrosis (OSF) is a chronic oral disease with a tendency to carcinogenesis. At present, the treatment of OSF is limited and ineffective, and there is an urgent need to find new effective drugs and mechanisms of action.

METHODS:

Arecoline was used to induce human oral mucosal fibroblasts (HOFs) to establish OSF cell model. The effects of curcumin on the proliferation, migration and invasion of HOFs were detected by CCK-8 and Transwell. Western blot (WB) was used to detect the effect of curcumin on epithelial-mesenchymal transition (EMT) process and TGF-β1/Smads signalling pathway. The regulation of XIST and miR-25-3p expression by curcumin was detected by qRT-PCR, and the role of XIST/miR-25-3p axis in curcumin function was investigated by rescue assay to detect cell viability, EMT progression and TGF-β1/Smads signalling pathway.

RESULTS:

Curcumin significantly inhibited HOF cell viability (about 58%) and EMT process, down-regulate the expression of mesenchymal markers N-cadherin and Vimentin (over 40%), up-regulate the expression of epithelial marker E-cadherin (twice), and inhibit the activation of TGF-β1/Smads signalling pathway (about 50%). Curcumin regulated the expression levels of XIST (downregulated by approximately 58%) and miR-25-3p (increased by more than twice), and XIST regulated the expression of miR-25-3p through sponge adsorption. Further studies confirmed that curcumin regulated HOF cell activity, EMT process and TGF-β1/Smads signalling pathway through the XIST/miR-25-3p axis.

CONCLUSIONS:

Curcumin effectively inhibits EMT by inactivating the TGF-β1/Smads pathway through regulating XIST/miR-25-3p, and thereby alleviating the progression ofOSF. The study results further reveal the mechanisms underlying the function of curcumin, and may provide novel targets and ideas for OSF therapy.

100 Deals associated with Arecoline

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB04365

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	Phase 1	-	Cogent Elliott Ltd.	-
Alzheimer Disease	Phase 1	-	Ferrosan Medical Devices A/S	-
Autistic Disorder	Preclinical	China	Xiamen Xianyue Hospital	01 Sep 2025