The cyclodextrins (CDs) are cyclic oligomers of glucose that are water-soluble because of the large number of hydroxyl groups on CDs. They are biocompatible, non-immunogenic, and have low toxicities in animals and humans, and thus have been widely used to improve solubility of a variety of hydrophobic drugs as well as to enhance their bioavailability by forming water-soluble inclusion complexes via hydrophobic interactions between drugs and hydrophobic cavity of CDs.
Two hydrophobic coumarinolignans, cleomiscosins C and D were isolated from the heartwood of Acer mono, however, biological evaluation of these compounds was not carried out due to their low solubility in aqueous system. Therefore, their inclusion complex molecules with β-cyclodextrin were prepared for improvement of their very poor water solubility. Anti-proliferative effects of these complex molecules were successfully estimated on human colon cancer cells, HCT-116 in vitro. The inclusive complexes of cleomiscosins C and D with β-cyclodextrin exhibited excellent water solubility, which made it feasible to measure their cytotoxicity in cell-based assay system, and cleomiscosin D showed significant anti-proliferative effects with IC50 value of 6.6µg/mL.
