Saucernetin-8 isolated from Saururus chinensis induced the differentiation of human acute promyelocytic leukemia HL-60 cells.
The present work was performed to investigate the effects of saucernetin-8 on proliferation and differentiation of human leukemia HL-60 cells as well as the underlying mechanisms for these effects. Saucernetin-8 exhibited a potent antiproliferative activity against HL-60 cells. This compound was also found to be a potent inducer of differentiation in human leukemia derived HL-60 cells through the examination of differentiation markers, as assessed by nitroblue tetrazolium reduction test, esterase activity assay, phagocytic activity assay, morphology change, and expression of CD14 and CD66b surface antigens. These results suggest that saucernetin-8 induces the differentiation of human leukemia cells to granulocytes and monocytes/macrophages lineage. Moreover, DNA flow-cytometry indicated that saucernetin-8 induced a G1 phase arrest of HL-60 cells. The protein and mRNA expression levels of p21 were up-regulated during saucernetin-8-dependent HL-60 cell differentiation, whereas the level of c-myc was down-regulated. Taken together, our results suggest that saucernetin-8 may have potential as a therapeutic agent in human leukemia.
College of Pharmacy, Kyung-Hee University, Dongdaemun-Ku, Seoul, Korea.
Bo-Rim
BR
Seo
Chae-Bin
CB
Yoo
Hee-Juhn
HJ
Park
Jong-Won
JW
Choi
Kyungwon
K
Seo
Seung-Ki
SK
Choi
Kyung-Tae
KT
Lee
D000970:Antineoplastic Agents / Q000302:isolation & purification / Q000494:pharmacology*; D018797:Cell Cycle Proteins / Q000096:biosynthesis / Q000235:genetics; D002454:Cell Differentiation / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D050759:Cyclin-Dependent Kinase Inhibitor p21; D015536:Down-Regulation; D005663:Furans / Q000302:isolation & purification / Q000494:pharmacology*; D016259:Genes, myc / Q000187:drug effects; D018922:HL-60 Cells; D006801:Humans; D017705:Lignans / Q000302:isolation & purification / Q000494:pharmacology*; D010936:Plant Extracts / Q000494:pharmacology; D012333:RNA, Messenger / Q000096:biosynthesis; D020133:Reverse Transcriptase Polymerase Chain Reaction; D032134:Saururaceae; D015854:Up-Regulation
D000970:Antineoplastic Agents; C493956:CDKN1A protein, human; D018797:Cell Cycle Proteins; D050759:Cyclin-Dependent Kinase Inhibitor p21; D005663:Furans; D017705:Lignans; D010936:Plant Extracts; D012333:RNA, Messenger; C481155:saucernetin-8