Drug intelligence / Profile preview

baohuoside I

Development stage
Preclinical
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral, Not Established For Clinical Use
01

Overview

Baohuoside I is a **flavonoid glycoside** (glycosyloxyflavone) isolated primarily from plants of the genus Epimedium (notably Epimedium koreanum and Epimedium pubescens), a key constituent in the herbal "Epimedii Folium". It acts as an **anti-cancer**, **anti-inflammatory**, **anti-osteoclastic**, and **apoptosis-inducing** agent, with demonstrated activity in vitro and in vivo. Mechanistically, it downregulates proteins such as survivin and cyclin D1, induces apoptosis via inhibition of NF-κB pathway, and inhibits major signaling cascades (MAPK, NF-κB, CXCR4, PPARγ/VEGF) involved in tumor progression, angiogenesis, and osteoclast differentiation[1][4][6][7][10][13][14]. Baohuoside I also exhibits **cytoprotective, neuroprotective, and antiproliferative effects** and has been shown to act as a chemosensitizer (e.g., enhancing the efficacy of paclitaxel in breast cancer or overcoming cisplatin resistance in ovarian cancer). It is not an approved pharmaceutical but is being investigated in preclinical models for esophageal cancer, breast cancer, hepatocellular carcinoma, nasopharyngeal carcinoma, ovarian cancer, multiple myeloma, and osteoporosis[3][6][7][10][11][13]. It also inhibits CYP3A4 and CYP2C19, potentially altering the metabolism of drugs such as tofacitinib, indicating a risk for drug–drug interactions[3].

Other names
baohuosideIcarisidIcariside IIBaohuside IBaohuosideⅠBaohuoside-1Baohuoside1Baohuoside 1baohuoside IBahoroside IIcariside II-RM
02

Targets

NF-κBCXCR4 (C-X-C motif chemokine receptor 4)PPARG (Peroxisome proliferator-activated receptor gamma)CYP3A4 (Cytochrome P450 3A4)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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