rutaecarpine

Rutaecarpine is a natural pentacyclic indolopyridoquinazolinone alkaloid isolated primarily from the fruit of Evodia rutaecarpa, a traditional Chinese medicinal herb[1][4][5][2]. It is known for diverse pharmacological properties, including vasodilatory, anti-thrombotic, anti-platelet aggregation, anti-inflammatory, analgesic, anti-obesity, and anticancer activities[1][3][5]. Mechanistically, rutaecarpine acts through multiple targets: it is a known inhibitor of cyclooxygenase-2 (COX-2)[5][12][13] and also inhibits COX-1[10]. It can induce degradation of the ABCB1 transporter via upregulation of E3 ubiquitin ligase MARCH8, thereby reversing ABCB1-mediated multidrug resistance (MDR) in cancer cells[1]. Additionally, it activates transient receptor potential vanilloid 1 (TRPV1), leading to increased calcitonin gene-related peptide (CGRP) release and vasodilation, contributing to antihypertensive effects[3]. It shows anti-inflammatory activity by inhibiting NADPH oxidase-dependent production of reactive oxygen species (ROS), inducible nitric oxide synthase (iNOS), and suppression of pro-inflammatory cytokines[3][5]. Rutaecarpine has also demonstrated anti-atherosclerotic, anti-Alzheimer's, antitumor, and anti-obesity properties in multiple preclinical models[1][5].

Other names

rutaecarpineRutacarpineRHETINERutaccarpine