Antiproliferative activity of Rhinacanthus nasutus (L.) Kurz extracts and the active moiety, Rhinacanthin C.
Rhinacanthus nasutus (L.) Kurz (Acanthaceae) is a shrub widely distributed in South China and India. In this study, the antiproliferative activity of the ethanol extract of root and aqueous extract of leaves of R. nasutus, and the supposed active moiety rhinacanthin C was assessed in vitro using the human cervical carcinoma cell line HeLa, its MDR1-overexpressing subline Hvr100-6, human prostate carcinoma PC-3 cells and human bladder carcinoma T24 cells. Rhinacanthin C was chemically synthesized and its content in the R. nasutus extracts was determined by HPLC with a photodiode array detector. The antiproliferative activity of the R. nasutus extracts was also assessed in vivo using sarcoma 180-bearing mice. It was suggested that 1) the in vitro antiproliferative activity of rhinacanthin C was comparable with or slightly weaker than that of 5-FU, 2) rhinacanthin C showed antiproliferative activity for MDR1-overexpressing Hvr100-6 cells, similarly to parent HeLa cells, 3) the in vitro antiproliferative activity of the ethanol extract of root R. nasutus was due to rhinacanthin C, whereas that of the aqueous extract of leaves of R. nasutus was due to constituents other than rhinacanthin C, and 4) both of the R. nasutus extracts showed in vivo antiproliferative activity after oral administration once daily for 14 d.
Gotoh
Akinobu
A
Department of Clinical Genetics and International Center for Medical Research, School of Medicine, Kobe University, Japan.
Sakaeda
Toshiyuki
T
Kimura
Takashi
T
Shirakawa
Toshiro
T
Wada
Yoshitaka
Y
Wada
Atsushi
A
Kimachi
Tetsutaro
T
Takemoto
Yoshiji
Y
Iida
Akira
A
Iwakawa
Seigo
S
Hirai
Midori
M
Tomita
Hisako
H
Okamura
Noboru
N
Nakamura
Tsutomu
T
Okumura
Katsuhiko
K
D027901:Acanthaceae; D000818:Animals; D045744:Cell Line, Tumor; D006131:Growth Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D006367:HeLa Cells; D006801:Humans; D017705:Lignans / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D018515:Plant Leaves; D018517:Plant Roots; D023041:Xenograft Model Antitumor Assays / Q000379:methods
D006131:Growth Inhibitors; D017705:Lignans; D010936:Plant Extracts; C107781:rhinacanthin E