Sesame (Sesamum indicum L.) seeds have been authenticated for its medicinal value in both
Chinese and Indian systems of medicine. Its numerous potential nutritional benefits are attributed to its
main bioactive constituents, sesamol. As a result of those studies, several molecular mechanisms are
emerging describing the pleiotropic biological effects of sesamol. This review summarized the most
interesting in vitro and in vivo studies on the biological effects of sesamol. The present work summarises
data available from Pubmed and Scopus database. Several molecular mechanisms have been elucidated
describing the pleiotropic biological effects of sesamol. Its major therapeutic effects have been
elicited in managing oxidative and inflammatory conditions, metabolic syndrome and mood disorders.
Further, compelling evidence reflected the ability of sesamol in inhibiting proliferation of the inflammatory
cell, prevention of invasion and angiogenesis via affecting multiple molecular targets and
downstream mechanisms. Sesamol is a safe, non‐toxic chemical that mediates anti‐inflammatory
effects by down‐regulating the transcription of inflammatory markers such as cytokines, redox status,
protein kinases, and enzymes that promote inflammation. In addition, sesamol also induces apoptosis
in cancer cells via mitochondrial and receptor‐mediated pathways, as well as activation of caspase cascades.
In the present review, several pharmacological effects of sesamol are summarised namely, antioxidant,
anti-cancer, neuroprotective, cardioprotective, anti-inflammatory, hypolipidemic, radioprotective,
anti-aging, anti-ulcer, anti-dementia, anti-depressant, antiplatelet, anticonvulsant, anti-anxiolytic,
wound healing, cosmetic (skin whitening), anti-microbial, matrix metalloproteinase (MMPs) inhibition,
hepatoprotective activity and other biological effects. Here we have summarized the proposed
mechanism behind these pharmacological effects.