Taraxinic acid, a hydrolysate of sesquiterpene lactone glycoside from the Taraxacum coreanum NAKAI, induces the differentiation of human acute promyelocytic leukemia HL-60 cells.
The present work was performed to elucidate the active moiety of a sesquiterpene lactone, taraxinic acid-1'-O-beta-D-glucopyranoside (1). from Taraxacum coreanum NAKAI on the cytotoxicity of various cancer cells. Based on enzymatic hydrolysis and MTT assay, the active moiety should be attributed to the aglycone taraxinic acid (1a). rather than the glycoside (1). Taraxinic acid exhibited potent antiproliferative activity against human leukemia-derived HL-60. In addition, this compound was found to be a potent inducer of HL-60 cell differentiation as assessed by a nitroblue tetrazolium reduction test, esterase activity assay, phagocytic activity assay, morphology change, and expression of CD 14 and CD 66 b surface antigens. These results suggest that taraxinic acid induces the differentiation of human leukemia cells to monocyte/macrophage lineage. Moreover, the expression level of c-myc was down-regulated during taraxinic acid-dependent HL-60 cell differentiation, whereas p21(CIP1) and p27(KIP1) were up-regulated. Taken together, our results suggest that taraxinic acid may have potential as a therapeutic agent in human leukemia.
Choi
Jung-Hye
JH
College of Pharmacy, Kyung-Hee University, Seoul, Korea.
Shin
Kyung-Min
KM
Kim
Na-Young
NY
Hong
Jung-Pyo
JP
Lee
Yong Sup
YS
Kim
Hyoung Ja
HJ
Park
Hee-Juhn
HJ
Lee
Kyung-Tae
KT
D000818:Animals; D002454:Cell Differentiation / Q000187:drug effects / Q000502:physiology; D006027:Glycosides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018922:HL-60 Cells / Q000166:cytology / Q000187:drug effects*; D006801:Humans; D007783:Lactones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D051379:Mice; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D018514:Plant Structures / Q000737:chemistry; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D031205:Taraxacum / Q000737:chemistry; D014407:Tumor Cells, Cultured / Q000166:cytology / Q000187:drug effects
D006027:Glycosides; D007783:Lactones; D010936:Plant Extracts; D012717:Sesquiterpenes