The abnormal proliferation and
hypertrophy of adipocytes mediate the expansion of adipose tissue and then cause
obesity-related diseases. Theoretically, an approach for preventing and curing
obesity is to inhibit cell proliferation during the mitotic clonal expansion (MCE) progression of adipocyte differentiation. Polycyclic polyprenylated acylphloroglucinols (
PPAPs) are mainly found from Hypericum and Garcinia genus, which have been reported to have various
biological activities such as anti-depressant,
anti-oxidant, and anti-
tumor. Previously, our group has reported that
adamantane-type
PPAPs exhibited blunting activity in adipogenesis. In this study, another six
adamantane PPAPs were screened to investigate their anti-adipogenesis activities and then discussed the structure-activity relationship. Particularly, sampsonione F, one of the
PPAPs dramatically suppressed adipogenesis dose-dependently in vitro, along with decreased expressions of C/EBPβ, C/EBPα, PPARγ, FABP4, and FAS. Moreover, sampsonione F upregulated the expression of p27 by activating p53 pathway and then downregulated the expressions of key regulators during G1/S phase arrest. Our data support that sampsonione F suppressed adipogenesis by activating p53 pathway, regulating
cyclins, and resulting in G1/S phase arrest during the MCE progression of adipogenesis. This work provides a new
adamantane-type
PPAPs in the regulation of adipogenesis and extends our knowledges on the mechanism of the type
PPAPs in regulation of adipogenesis.