title: Cryptolepine, isolated from Sida acuta, sensitizes human gastric adenocarcinoma cells to TRAIL-induced apoptosis.
abstract: Bioassay guided separation of Sida acuta whole plants led to the isolation of an alkaloid, cryptolepine (1), along with two kaempferol glycosides (2-3). Compound 1 showed strong activity in overcoming TRAIL-resistance in human gastric adenocarcinoma (AGS) cells at 1.25, 2.5 and 5 μm. Combined treatment of 1 and TRAIL sensitized AGS cells to TRAIL-induced apoptosis at the aforementioned concentrations.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Chiba University, Inage-ku, Chiba, Japan.
authors.forename: Firoj
authors.initials: F
authors.lastname: Ahmed
authors.forename: Kazufumi
authors.initials: K
authors.lastname: Toume
authors.forename: Takashi
authors.initials: T
authors.lastname: Ohtsuki
authors.forename: Mahmudur
authors.initials: M
authors.lastname: Rahman
authors.forename: Samir Kumar
authors.initials: SK
authors.lastname: Sadhu
authors.forename: Masami
authors.initials: M
authors.lastname: Ishibashi
mesh_terms: D000230:Adenocarcinoma / Q000473:pathology; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D053148:Caspase 3 / Q000378:metabolism; D053179:Caspase 7 / Q000378:metabolism; D045744:Cell Line, Tumor; D019008:Drug Resistance, Neoplasm; D004789:Enzyme Activation / Q000187:drug effects; D006027:Glycosides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D026121:Indole Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D019660:Malvaceae / Q000737:chemistry*; D011804:Quinolines / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013274:Stomach Neoplasms / Q000473:pathology; D053221:TNF-Related Apoptosis-Inducing Ligand / Q000494:pharmacology*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D006027:Glycosides; D026121:Indole Alkaloids; D011804:Quinolines; D053221:TNF-Related Apoptosis-Inducing Ligand; C024015:cryptolepine; D053148:Caspase 3; D053179:Caspase 7