Drug intelligence / Profile preview

imperialine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Imperialine is a **steroidal alkaloid** found primarily in the bulbs of plants in the Fritillaria genus, such as Fritillaria cirrhosa, Fritillaria imperialis, and Petilium eduardi. It is one of the major bioactive constituents of the traditional Chinese medicine chuanbeimu (Bulbus Fritillariae Cirrhosae), which has been widely used as an **antitussive and expectorant** in respiratory conditions such as cough, asthma, and other pulmonary diseases[1][3][6]. Imperialine possesses a cevan-type steroidal backbone, exhibits moderate alkalinity (pKa ≈ 8.5), and displays pharmacological effects including **mitigation of pulmonary impairment and suppression of inflammatory cytokines** (e.g., IL-1β, IL-6, IL-8, TNF-α) in COPD-like rat models[1]. The key mechanism appears to involve **passive membrane diffusion** across the intestinal wall, without evidence of active transporter involvement[3].

Other names
imperialineSipeimineKashmirineRaddeamine(3β,5α,17β)-3,20-dihydroxycevan-6-oneCevan-6-one, 3,20-dihydroxy-, (3β,5α,17β)-
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)IL1B (Interleukin-1 beta)IL-6 (Interleukin 6)NOS2 (Nitric Oxide Synthase 2)CHRM2 (M2)MMP9 (Matrix metalloproteinase-9)NF-κBTGFB1 (Transforming growth factor Beta-1 proprotein)TIMP1 (Metalloproteinase inhibitor 1)TNFA (Tumor necrosis factor alpha (soluble))

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