title: Discovery of a new function of curcumin which enhances its anticancer therapeutic potency.
abstract: Curcumin has received immense attention over the past decades because of its diverse biological activities and recognized as a promising drug candidate in a large number of diseases. However, its clinical application has been hindered due to extremely low aqueous solubility, chemical stability, and cellular uptake. In this study, we discovered quite a new function of curcumin, i.e. pH-responsive endosomal disrupting activity, derived from curcumin's self-assembly. We selected anticancer activity as an example of biological activities of curcumin, and investigated the contribution of pH-responsive property to its anticancer activity. As a result, we demonstrated that the pH-responsive property significantly enhances the anticancer activity of curcumin. Furthermore, we demonstrated a utility of the pH-responsive property of curcumin as delivery nanocarriers for doxorubicin toward combination cancer therapy. These results clearly indicate that the smart curcumin assemblies act as promising nanoplatform for development of curcumin-based therapeutics.
authors.affiliation: Department of Nanobiochemistry, Frontiers of Innovative Research in Science and Technology, Konan University, 7-1-20 Minatojima-Minamimachi, Kobe 650-0047, Japan.
authors.forename: Koji
authors.initials: K
authors.lastname: Nagahama
authors.affiliation: Department of Nanobiochemistry, Frontiers of Innovative Research in Science and Technology, Konan University, 7-1-20 Minatojima-Minamimachi, Kobe 650-0047, Japan.
authors.forename: Tomoya
authors.initials: T
authors.lastname: Utsumi
authors.affiliation: Department of Nanobiochemistry, Frontiers of Innovative Research in Science and Technology, Konan University, 7-1-20 Minatojima-Minamimachi, Kobe 650-0047, Japan.
authors.forename: Takayuki
authors.initials: T
authors.lastname: Kumano
authors.affiliation: Department of Nanobiochemistry, Frontiers of Innovative Research in Science and Technology, Konan University, 7-1-20 Minatojima-Minamimachi, Kobe 650-0047, Japan.
authors.forename: Saeko
authors.initials: S
authors.lastname: Maekawa
authors.affiliation: Department of Nanobiochemistry, Frontiers of Innovative Research in Science and Technology, Konan University, 7-1-20 Minatojima-Minamimachi, Kobe 650-0047, Japan.
authors.forename: Naho
authors.initials: N
authors.lastname: Oyama
authors.affiliation: Department of Nanobiochemistry, Frontiers of Innovative Research in Science and Technology, Konan University, 7-1-20 Minatojima-Minamimachi, Kobe 650-0047, Japan.
authors.forename: Junji
authors.initials: J
authors.lastname: Kawakami
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D003474:Curcumin / Q000494:pharmacology*; D004337:Drug Carriers / Q000737:chemistry; D006801:Humans; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000201:enzymology / Q000473:pathology; D014407:Tumor Cells, Cultured; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D003474:Curcumin