Cryptolepine, isolated from Sida acuta, sensitizes human gastric adenocarcinoma cells to TRAIL-induced apoptosis.
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.
Ahmed
Firoj
F
Graduate School of Pharmaceutical Sciences, Chiba University, Inage-ku, Chiba, Japan.
Toume
Kazufumi
K
Ohtsuki
Takashi
T
Rahman
Mahmudur
M
Sadhu
Samir Kumar
SK
Ishibashi
Masami
M
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*
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