Delving into the Latest Updates on Rutaecarpine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

MAPK x NF-κB x NLRP3 x TNFR1

Action

inhibitors

Mechanism

MAPKs inhibitors(Mitogen-activated protein kinase inhibitors), NF-κB inhibitors(Nuclear factor NF-kappa-B complex inhibitors), NLRP3 inhibitors(NACHT, LRR and PYD domains-containing protein 3 inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesNervous System Diseases+ [6]

Active Indication

Ischemic strokeCardiovascular DiseasesGout+ [1]

Inactive Indication-

Originator Organization

Chengdu University of Traditional Chinese Medicine

Active Organization

Chengdu University of Traditional Chinese Medicine

Chungnam National University

Chinese Medical Sciences China Academy

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC18H13N3O

InChIKeyACVGWSKVRYFWRP-UHFFFAOYSA-N

CAS Registry84-26-4

Increasing the expression of ATP-binding cassette transporter A1 (ABCA1) can lower cellular cholesterol levels and prevent foam cell formation. In this study, a series of 5, 6-dihydro-8H-isoquinolino[1, 2-b]quinazolin-8-one derivatives were synthesised and assessed for their ability to up-regulate ABCA1 expression. The structure-activity relationship was explored and summarised. Among the 28 derivatives, compound 3 exhibited the most potent activity in activating the ABCA1 promoter (2.50-fold), significantly up-regulating both ABCA1 mRNA and protein levels in RAW264.7 macrophage cells. Mechanism studies revealed that compound 3 acted by targeting the LXR-involved pathway. In a foam cell model, compound 3 reduced ox-LDL-induced lipid accumulation and thereby inhibited foam cell formation. Moreover, compared to the LXR agonist T0901317, compound 3 led to minimal accumulation of unwanted lipids and triglycerides in HepG2 cells. With little cytotoxicity towards all the tested cell lines, compound 3 holds promise as a novel potential anti-atherogenic agent for further exploration.

01 Oct 2025·CURRENT PHARMACEUTICAL DESIGN

Exploring the Therapeutic Potential of Evodia rutaecarpa in Early-Onset Pancreatic Cancer: A Network Pharmacology and Molecular Docking Approach

Article

Author: Park, Moon Nyeo ; Rahman, Md. Habibur ; Hasan, Md. Nahid ; Islam, Kh Mujahidul ; Kang, Han Na ; Kim, Bonglee ; Moon, Seungjoon ; Hasan, Md Imran ; Rahman, Md. Mizanur

Introduction::

Pancreatic cancer (PC) remains a formidable challenge in cancer, which requires innovative approaches to identify novel therapeutic strategies. Evodia rutaecarpa, a traditional herbal remedy known for its analgesic and antiemetic properties, has been reported to exhibit anticancer effects.

Methods::

We employed network pharmacology to elucidate the bioactive ingredients of Evodia rutaecarpa and their potential targets in the context of early-onset pancreatic cancer. By integrating data from public databases, we identified genes associated with PC and developed a protein-protein interaction (PPI) network. Topological analysis of the PPI network facilitated the identification of core targets, which were subsequently subjected to molecular docking with corresponding bioactive ingredients of Evodia rutaecarpa. The computational approach aimed to unveil the pharmacological mechanisms of basic putative crucial proteins and associated pathways implicated in early-onset PC. Pathway and GO analysis highlighted the significant involvement of Evodia rutaecarpa in pathways such as cAMP signaling, cytokine-cytokine receptor interaction, rheumatoid arthritis, interleukin signaling, bladder cancer, IL-17, IL-24 signaling, cytokine-mediated signaling, chemokine, and calcium-mediated signaling.

Results::

Further exploration focused on a hub protein module derived from PPIs, with molecular docking emphasizing strong binding interactions between Evodia rutaecarpa and ERBB2, a protein strongly implicated in PC management compared to other identified hub proteins (STAT1, ERBB2, CXCL10, INS, RACK1, FOS, HLA-DRB1, POMC, PRKAA1). Additionally, the pharmacokinetic analysis of Evodia rutaecarpa indicated its efficacy as a therapeutic agent with minimal adverse effects. Rutaecarpine, identified as the main bioactive ingredient, emerged as a potential inhibitor of PC growth through the suppression of ERBB2.

Conclusion::

These outcomes provide novel insights into the prevention and treatment of PC, presenting Evodia rutaecarpa as a promising candidate for further experimental validation and clinical exploration. The identified discovery has the potential to reduce the drug resistance of Evodia rutaecarpa by engaging with a new target in a specific manner, thus improving therapeutic effectiveness.

01 Sep 2025·EUROPEAN JOURNAL OF PHARMACOLOGY

Rutaecarpine alleviates aspirin-induced gastric injury via oxidative stress and ferroptosis inhibition

Article

Author: Zhu, Shishu ; Wei, Shizhang ; Jing, Manyi ; Chang, Lei ; Wang, Xin ; Wu, Wenbin ; Zhao, Yanling ; Li, Haotian ; Zhou, Xuelin

INTRODUCTION:

Rutaecarpine (RUT) has shown potential therapeutic benefits for gastrointestinal disorders, but its molecular mechanisms remain unclear. This study aimed to investigate the molecular mechanism of RUT in treating aspirin-induced acute gastric mucosal injury in rats.

METHODS:

SD rats received RUT for 7 consecutive days before aspirin-induced gastric damage. Metabolomics approaches were employed to identify differential metabolic signals and RUT-mediated protective mechanisms, validated by Western blotting.

RESULTS:

Compared to the model group, both RUT doses significantly alleviated gastric mucosal damage by enhancing tight junction-associated protein expression, suppressing inflammatory factors. Metabolomics revealed that the gastroprotective effects of RUT were primarily associated with lipid peroxidation and oxidative stress regulation. Furthermore, RUT treatment markedly reduced 4-HNE and MDA levels, and elevated GSH, SOD, and CAT activities, upregulated protein expression levels of Nrf2, HO-1, SLC7A11, GPX4, and FTH1.

CONCLUSION:

These findings demonstrate that RUT protects against aspirin-induced gastric mucosal injury by suppressing oxidative stress and inhibiting ferroptosis signaling pathways.

100 Deals associated with Rutaecarpine

Login to view more data

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Ischemic stroke	Preclinical	China	Chinese Medical Sciences China Academy	27 Jun 2025
Cardiovascular Diseases	Preclinical	South Korea	Chungnam National University	21 May 2025
Gout	Preclinical	China	Chengdu University of Traditional Chinese Medicine	08 May 2025
Peritonitis	Preclinical	China	Chengdu University of Traditional Chinese Medicine	08 May 2025