Drug intelligence / Profile preview

epimedin b

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Epimedin B is a naturally occurring flavonoid glycoside found predominantly in species of the genus *Epimedium* (notably *Epimedium brevicornu* and *Epimedium koreanum*) and is a major active constituent of Herba Epimedii. It has demonstrated multiple biological activities including anti-inflammatory[1][2], antioxidant[2], antiosteoporotic[1][4][8][10], and immunostimulatory effects[5]. Mechanistically, epimedin B exerts its antiosteoporotic effect by stimulating osteoblast activity and modulating bone turnover markers. In animal models of osteoporosis it increases N-terminal propeptide of type I procollagen (P1NP), decreases C-telopeptide of type I collagen (CTX1), improves bone microarchitecture parameters such as connectivity density and trabecular number while reducing trabecular separation[10]. Transcriptomic analyses indicate that its action involves regulation of the PI3K-Akt signaling pathway as well as MAPK and PPAR pathways in bone tissue[4][10]. In immunology studies it has been shown to enhance activation of the NLRP3 inflammasome—promoting caspase‑1 cleavage and IL‑1β secretion in macrophages—without affecting TNF‑α or IL‑6 production at effective doses for inflammasome activation[5]. Its poor oral bioavailability is attributed to low intrinsic permeability and efflux by apical transporters such as BCRP in intestinal cells[7].

Other names
110623-73-93-\[(2S,3R,4R,5R,6S)-4,5-dihydroxy-6-methyl-3-\[(2S,3R,4S,5R)-3,4,5-trihydroxyoxan-2-yloxy\]oxan\-2\-yl\]oxy\-5-hydroxy\-2-(4-methoxyphenyl)\ -8-(3-methylbut\-2-enyl)\ -7-\[(2S,\ 3R,\ 4S,\ 5S,\ 6R)\ -3,\ 4,\ 5-trihydroxy\-6-(hydroxymethyl)oxan\-2-yloxy\]chromen\-4-oneDTXSID40149341DTXSID-40149341DTXSID 40149341
02

Targets

NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)PPAR (PPAR family)

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