Bioorganic & Medicinal Chemistry 2007-02-01

Rotenoids and flavonoids with anti-invasion of HT1080, anti-proliferation of U937, and differentiation-inducing activity in HL-60 from Erycibe expansa.

Hisashi Matsuda, Kazutoshi Yoshida, Katsutoshi Miyagawa, Yasunobu Asao, Saya Takayama, Souichi Nakashima, Fengming Xu, Masayuki Yoshikawa

Index: Bioorg. Med. Chem. 15 , 1539-46, (2007)

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Abstract

Principal rotenoids (deguelin, tephrosin, rotenone, and 12a-hydroxyrotenone) (3-30microM) isolated from the stems of Erycibe expansa significantly inhibited invasion of human fibrosarcoma HT1080 cells through Matrigel-coated filters and release of proMMPs-2 and 9. In addition, deguelin and tephrosin showed differentiation-inducing activity in human promyelocytic leukemia HL-60 cells. Furthermore, effects of various constituents isolated from the ethyl acetate-soluble fraction on proliferation of human leukemia U937 cells were examined. As a result, most of isoflavones and several flavans as well as rotenoids showed moderate or substantial anti-proliferative activities.