Loliolide, is a natural bioactive monoterpenoid lactone extracted from a variety of plants including marine algae, medicinal plants such as psychoactive plant Salvia divinorum, Acalypha, Brachystemma calycinum, Calendula officinalis L. flowers and many more. Loliolide exerted inhibitory activity against cellular senescence in human dermal fibroblasts diminishing senescence-associated β-galactosidase activity (SA-β-gal), the level of p21 protein, and the level of reactive oxygen species in senescent cells induced by adriamycin treatment. These findings imply that loliolide might be useful for the development of dietary supplements or cosmetics that ameliorate tissue aging or age-associated diseases. As a selective estrogen receptor modulator, which can activate ERβ and ERα and simultaneously express estrogenic activity loliolide can be applied as medical or food compositions to improve estrogen deficiency-related symptoms and can be used as selective estrogen receptor modulator (SERM) in menopause women. Recently loliolide was characterized as a potent hepatitis C virus (HCV) entry inhibitor, which merit further evaluation for development as candidate antiviral agents against hepatitis C.