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K.-H. Lam et al. / European Journal of Medicinal Chemistry 45 (2010) 5527e5530
Human hepatocellular carcinoma Hep3B cell line was used for
Appendix. Supplementary data
preliminary in vitro anti-cancer screening of the organophosphine
compounds, and cisplatinum was used as the positive reference.
Athymic nude mice Hep3B hepatocellular carcinoma xenograft
Supplementary data associated with this article can be found, in
experiment was then performed using racemic
3 (rac-3).
We observed that rac-3 exhibited significant in vivo antitumor
activity. Intraperitoneal injection of rac-3 at 10 mg/kgBW for 4
consecutive days showed a statistically significant retardation of
Hep3B xenograft tumor growth when compared to the vehicle
control (please refer to the Supplementary Material for details).
Further autopsy study of the vital organs demonstrated that the
current rac-3 treatment protocol did not exert necrotic features on
vital organs including kidney and liver. Interestingly, the rac-3
resulted in significant necrotic induction on the Hep3B cancer cell
xenograft, suggesting the effective in vivo therapeutic activity of
rac-3 (Fig. 2) [23,24].
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Dr. C.H. Chui would like to acknowledge the financial support
from Institute of Textiles and Clothing, the Hong Kong Polytechnic
University (1ZV-5L from ITC, HKPU). Dr. C.H. Chui is supported by
the Assistant Professorship from ITC, HKPU, and Prof. R. Gambari is
sponsored by AIRC (Italian Association for Cancer Research). The
authors wish to dedicate to Professor Albert Sun-Chi Chan on his
occasion of his 60th birthday, and to acknowledge Areas of Excel-
lence Scheme established under the University Grants Committee
of the Hong Kong Special Administrative Region, P.R. China (Project
No. AoEP-10/01)