Antiproliferative Activity of Rhinacanthus nasutus (L.) K<small>URZ</small> Extracts and the Active Moiety, Rhinacanthin C

Akinobu Gotoh; Toshiyuki Sakaeda; Takashi Kimura; Toshiro Shirakawa; Yoshitaka Wada; Atsushi Wada; Tetsutaro Kimachi; Yoshiji Takemoto; Akira Iida; Seigo Iwakawa; Midori Hirai; Hisako Tomita; Noboru Okamura; Tsutomu Nakamura; Katsuhiko Okumura

doi:10.1248/bpb.27.1070

Regular Articles

Antiproliferative Activity of Rhinacanthus nasutus (L.) KURZ Extracts and the Active Moiety, Rhinacanthin C

Akinobu Gotoh, Toshiyuki Sakaeda, Takashi Kimura, Toshiro Shirakawa, Yoshitaka Wada, Atsushi Wada, Tetsutaro Kimachi, Yoshiji Takemoto, Akira Iida, Seigo Iwakawa, Midori Hirai, Hisako Tomita, Noboru Okamura, Tsutomu Nakamura, Katsuhiko Okumura

Author information

Akinobu Gotoh
Department of Clinical Genetics and International Center for Medical Research, School of Medicine, Kobe University
Toshiyuki Sakaeda
Department of Hospital Pharmacy, School of Medicine, Kobe University
Takashi Kimura
Department of Hospital Pharmacy, School of Medicine, Kobe University
Toshiro Shirakawa
Department of Organs Therapeutics, Faculty of Medicine, Kobe University Graduate School of Medicine
Yoshitaka Wada
Department of Organs Therapeutics, Faculty of Medicine, Kobe University Graduate School of Medicine
Atsushi Wada
Department of Hospital Pharmacy, School of Medicine, Kobe University
Tetsutaro Kimachi
Faculty of Pharmaceutical Sciences, Mukogawa Women's University
Yoshiji Takemoto
Graduate School of Pharmaceutical Sciences, Kyoto University
Akira Iida
Graduate School of Pharmaceutical Sciences, Kyoto University
Seigo Iwakawa
Kobe Pharmaceutical University
Midori Hirai
Kobe Pharmaceutical University
Hisako Tomita
Kobe Pharmaceutical University
Noboru Okamura
Department of Hospital Pharmacy, School of Medicine, Kobe University
Tsutomu Nakamura
Department of Hospital Pharmacy, School of Medicine, Kobe University
Katsuhiko Okumura
Department of Hospital Pharmacy, School of Medicine, Kobe University

Keywords: Rhinacanthus nasutus (L.), rhinacanthin C, MDR1

JOURNAL FREE ACCESS

2004 Volume 27 Issue 7 Pages 1070-1074

DOI https://doi.org/10.1248/bpb.27.1070

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Abstract

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.

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