Drug intelligence / Profile preview

sesamin

Development stage
Preclinical
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Sesamin is a naturally occurring lignan compound found predominantly in sesame seeds and sesame oil. It is widely used as a dietary supplement due to its antioxidant, anti-inflammatory, and lipid-lowering properties. Mechanistically, sesamin acts as a fatty acid metabolism modifier by inhibiting delta-5-desaturase (Δ5-desaturase), an enzyme involved in polyunsaturated fatty acid biosynthesis, leading to reduced levels of eicosapentaenoic acid (EPA) and arachidonic acid. Sesamin also inhibits tocopherol-ω-hydroxylation, the rate-limiting step in vitamin E metabolism, resulting in increased levels of γ-tocopherol and γ-tocotrienol. Additionally, it modulates drug-metabolizing enzymes by acting as an inhibitor of cytochrome P450 3A4 (CYP3A4) through antagonism of the pregnane X receptor (PXR), potentially affecting drug interactions[1][2][5]. Sesamin has demonstrated anti-cancer effects via suppression of NF-κB activation pathways and modulation of estrogen receptor activity[6][7]. It is not developed or marketed by any specific pharmaceutical company but is available as a nutritional supplement.

Other names
sesamin
02

Targets

CYP3A4 (Cytochrome P450 3A4)FADS1 (Fatty acid desaturase 1)NFKB1 (NF-κB1)PXR (Pregnane X receptor)

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