title: Multiple effects of berberine derivatives on colon cancer cells.
abstract: The pharmacological use of the plant alkaloid berberine is based on its antibacterial and anti-inflammatory properties; recently, anticancer activity has been attributed to this compound. To exploit this interesting feature, we synthesized three berberine derivatives, namely, NAX012, NAX014, and NAX018, and we tested their effects on two human colon carcinoma cell lines, that is, HCT116 and SW613-B3, which are characterized by wt and mutated p53, respectively. We observed that cell proliferation is more affected by cell treatment with the derivatives than with the lead compound; moreover, the derivatives proved to induce cell cycle arrest and cell death through apoptosis, thus suggesting that they could be promising anticancer drugs. Finally, we detected typical signs of autophagy in cells treated with berberine derivatives.
authors.affiliation: Istituto di Genetica Molecolare CNR, 27100 Pavia, Italy ; Departamento de Ciencias de la Salud, Universidad Técnica Particular de Loja, San Cayetano Alto, Calle París, 1101608 Loja, Ecuador.
authors.forename: Luis Miguel
authors.initials: LM
authors.lastname: Guamán Ortiz
authors.affiliation: Istituto di Genetica Molecolare CNR, 27100 Pavia, Italy.
authors.forename: Micol
authors.identifier: 0000-0003-3330-2112
authors.initials: M
authors.lastname: Tillhon
authors.affiliation: Istituto di Genetica Molecolare CNR, 27100 Pavia, Italy.
authors.forename: Michael
authors.identifier: 0000-0001-8240-0603
authors.initials: M
authors.lastname: Parks
authors.affiliation: Istituto di Genetica Molecolare CNR, 27100 Pavia, Italy.
authors.forename: Ilaria
authors.initials: I
authors.lastname: Dutto
authors.affiliation: Istituto di Genetica Molecolare CNR, 27100 Pavia, Italy.
authors.forename: Ennio
authors.identifier: 0000-0001-5391-5157
authors.initials: E
authors.lastname: Prosperi
authors.affiliation: Department of Molecular Medicine, Immunology and General Pathology Unit, University of Pavia, Via Ferrata 9, 27100 Pavia, Italy.
authors.forename: Monica
authors.identifier: 0000-0003-0437-7027
authors.initials: M
authors.lastname: Savio
authors.affiliation: Naxospharma srl, Via Giuseppe Di Vittorio 70, 20026 Novate Milanese, Italy.
authors.forename: Andrea G
authors.initials: AG
authors.lastname: Arcamone
authors.affiliation: Naxospharma srl, Via Giuseppe Di Vittorio 70, 20026 Novate Milanese, Italy.
authors.forename: Franco
authors.initials: F
authors.lastname: Buzzetti
authors.affiliation: Naxospharma srl, Via Giuseppe Di Vittorio 70, 20026 Novate Milanese, Italy.
authors.forename: Paolo
authors.identifier: 0000-0002-7971-7404
authors.initials: P
authors.lastname: Lombardi
authors.affiliation: Istituto di Genetica Molecolare CNR, 27100 Pavia, Italy.
authors.forename: Anna Ivana
authors.identifier: 0000-0003-3484-9881
authors.initials: AI
authors.lastname: Scovassi
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000138:chemical synthesis; D017209:Apoptosis / Q000187:drug effects; D001343:Autophagy / Q000187:drug effects; D001599:Berberine / Q000008:administration & dosage* / Q000031:analogs & derivatives / Q000138:chemical synthesis; D049109:Cell Proliferation / Q000187:drug effects*; D003110:Colonic Neoplasms / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology; D045325:HCT116 Cells; D006801:Humans; D016159:Tumor Suppressor Protein p53 / Q000235:genetics
chemical_list: D000970:Antineoplastic Agents; D016159:Tumor Suppressor Protein p53; D001599:Berberine