Apoptosis-inducing activity of synthetic intermediates of halichlorine.
Synthetic intermediates of alkaloid halichlorine with the azaspiro core structure have been found to induce apoptosis of cultured human cells including an acute monocytic leukemia cell line (THP-1) at micromolar concentrations. The novel biological activity of the intermediates was suggested to depend on the skeletal structure and silyloxymethyl functionality on the five-membered ring.
Itoh
Midori
M
Institute for Medicinal Resources, University of Tokushima, Sho-machi 1-78, 770-8505, Tokushima, Japan.
Kuwahara
Jun
J
Itoh
Kohji
K
Fukuda
Yu ichi
Yi
Kohya
Mikiko
M
Shindo
Mitsuru
M
Shishido
Kozo
K
D000470:Alkaloids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D017209:Apoptosis / Q000187:drug effects*; D053148:Caspase 3; D053179:Caspase 7; D020169:Caspases / Q000378:metabolism; D002843:Chromatin / Q000187:drug effects / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004789:Enzyme Activation / Q000187:drug effects; D006801:Humans; D015394:Molecular Structure; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013997:Time Factors; D014407:Tumor Cells, Cultured
D000470:Alkaloids; D002843:Chromatin; D013141:Spiro Compounds; C412666:halichlorine; C505407:CASP3 protein, human; C505520:CASP7 protein, human; D053148:Caspase 3; D053179:Caspase 7; D020169:Caspases