title: Naphthoquinone components from Alkanna tinctoria (L.) Tausch show significant antiproliferative effects on human colorectal cancer cells.
abstract: Our research to seek active compounds against human colorectal cancer from the root of Alkanna tinctoria (L.) Tausch led to the isolation of two naphthoquinones, alkannin (1) and angelylalkannin (2). The antiproliferative effects of the two compounds on human colon cancer cells HCT-116 and SW-480 were determined by the 3,4-(5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium salt (MTS) method. Cell cycle profile and cell apoptosis were determined using flow cytometry. Both of the two compounds showed significant inhibitory effects on the cancer cells. For alkannin (1) and angelylalkannin (2), the median inhibitory concentration (IC₅₀) values were 2.38 and 4.76 µM for HCT-116 cells, while for SW-480 cells they were 4.53 and 7.03 µM, respectively. The potential antiproliferative mechanisms were also explored. At concentrations between 1-10 µM, both compounds arrested the cell cycle at the G1 phase and induced cell apoptosis.
authors.affiliation: Faculty of Pharmaceutical Sciences, Nagasaki International University, 2825-7 Huis Ten Bosch, Sasebo, Nagasaki 859-3298, Japan.
authors.forename: Nguyen
authors.initials: N
authors.lastname: Huu Tung
authors.forename: Guang-Jian
authors.initials: GJ
authors.lastname: Du
authors.forename: Chong-Zhi
authors.initials: CZ
authors.lastname: Wang
authors.forename: Chun-Su
authors.initials: CS
authors.lastname: Yuan
authors.forename: Yukihiro
authors.initials: Y
authors.lastname: Shoyama
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D028082:Boraginaceae / Q000737:chemistry*; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects*; D015179:Colorectal Neoplasms; D045325:HCT116 Cells; D006801:Humans; D009285:Naphthoquinones / Q000494:pharmacology*; D010936:Plant Extracts / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry; D051381:Rats
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D009285:Naphthoquinones; D010936:Plant Extracts; C018204:alkannin; C580562:angelylalkannin