Embelin derivatives and their anticancer activity through microtubule disassembly.
Biological activities of the 1,4-benzoquinone derivatives 5- O-ethylembelin ( 1) and 5- O-methylembelin ( 2) were investigated. Both of them showed antiproliferative activity against a panel of human tumor cell lines upon comparison to normal marsupial kidney cells (PtK2). They arrested HL-60 cells in the G(0)/G(1) phase of the cell cycle in a dose- and time-dependent manner. In HeLa cells, exposure to 100 microM of 1 or 2 for 6 h induced a complete disassembly of the microtubule network and an increased number of cells blocked in mitotic stages. Treatment with 10 microM of 1 and 2 for 24 h induced apoptosis in HL-60 cells. This evidence suggests that both 1 and 2 are promising novel antimitotic and anticancer molecules targeting microtubular proteins.
Xu
Minjuan
M
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Xueyuan Road 38, 100083 Beijing, P.R. China.
Cui
Jingrong
J
Fu
Hongzheng
H
Proksch
Peter
P
Lin
Wenhan
W
Li
Min
M
D000818:Animals; D050256:Antimitotic Agents / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D016227:Benzoquinones / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D018922:HL-60 Cells / Q000187:drug effects; D006367:HeLa Cells / Q000187:drug effects; D006801:Humans; D051379:Mice; D008870:Microtubules / Q000187:drug effects; D008938:Mitosis / Q000187:drug effects; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D018547:Plant Stems; D029623:Primulaceae
D050256:Antimitotic Agents; D000972:Antineoplastic Agents, Phytogenic; D016227:Benzoquinones; D010936:Plant Extracts; C010945:embelin