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For decades now, compounds in the cycloartane-type series have been shown to
have versatile pharmacological activities. However, no extensive review has been written
to summarize these health-beneficial activities. Therefore, the purpose of this paper is to
systematically highlight the biological activities of these compounds, including their antitumor
and anti-osteoporosis effects, their effects on receptors, cytokine release, and
chronic renal failure, as well as their tyrosinase inhibitory, anticomplement, anti-parasite,
anti-HIV, and antituberculosis activities. In this review, we have summarized the structures
of over 200 compounds based on their characteristics and described their structureactivity
relationships (SARs), and potential mechanisms of action.