Acetogenins (
ACG) are naturally occurring compounds that are chemically one of the least investigated families. In the review, we have provided a comprehensive listing of 133 of these compounds for which anti-
tumor activity has been documented within the literature. We have compiled and studied their chemical structure, in-vitro as well as in-vivo anticancer
biological activity. We observed that the relative potency of
acetogenins can be categorized as adjacent bis-THF ACGs > nonadjacent bis-THF ACGs > mono-THF ACGs > linear-THF ACGs. Among adjacent bis-THF ACGs,
asiminocin (A100),
asiminecin (A101),
asiminacin (A102) and
asimin (A103) are the most active compounds with in-vitro activity (ED50) in the range of 10(-9) to 10(-12) μg/mL. For the nonadjacent bis-THF ACGs,
gigantecin (A53) exhibited better cytotoxicity as compared to others in the series with an ED50 in the range of 10(-6) to 10(-8) μg/mL. Similarly,
muricatetrocin-C (A36), a mono-THF and
coriadienin (A116) a linear
ACG has been reported to show promising cytotoxicity with an ED50 of 10(-5) μg/mL. Moreover, in-vivo studies indicate that compounds like
bullatacin (A83),
desacetyluvaricin (A76),
bullatalicin (A58) and
annonacin (A8) have demonstrated significant activity in mouse models and thereby exhibiting potential for lead development as a potential
anticancer agent/
drug. Also, globally oncologists are looking towards compounds from natural origin that inhibits the growth of resistant
tumor cells. We find that several
acetogenins like
bullatacin (A83), motrilin (A95),
asimicin (A77),
trilobacin (A96),
annonacin (A8),
gigantetronenin (A108) and
squamocin (A73) are efficacious in suppressing the proliferation of the MDR MCF-7/Adr cells. The present analysis suggests that
acetogenins can act as yet another important source for obtaining promising lead compounds in order to contribute to
cancer prevention, however, in future extensive in-vivo studies in animal models will be needed to provide insight for lead development.