Antiproliferative and apoptotic activities of linear furocoumarins from Notopterygium incisum on cancer cell lines.

Abstract

Bioassay-guided fractionation of the antiproliferative chloroform extract of the traditional Chinese medicine Qiang-Huo (Notopterygium incisum) led to the isolation of nine linear furocoumarins (1- 9). All the isolates were tested against two human cancer cell lines (HepG-2 and MCF-7) and a rat cancer cell line (C6) using the MTT assay method. Among them, notopol (1), notopterol (2), 5-[(2 E,5 Z)-7-hydroxy-3,7-dimethyl-2,5-octadienoxy]psoralene (3), and 5-[(2,5)-epoxy-3-hydroxy-3,7-dimethyl-6-octenoxy]psoralene (4) showed significant antiproliferative activity against the HepG-2 and C6 cancer cell lines, with IC(50) values of 7.7-24.8 microg/mL (5-FU: ca. 5 microg/mL). Compounds 1- 3 also showed moderate cytotoxicity against the MCF-7 cancer cell line, with IC(50) values of 39.4-61.3 microg/mL (5-FU: 17.3 microg/mL). The cell cycle-specific inhibition and apoptosis induced by compounds 1 and 2 were determined using flow cytometry. The structure-activity relationship (SAR) is briefly discussed herein. It was found that the presence of a free hydroxy at the lipophilic side chain linked to C-5 of the linear furocoumarins was essential for their in vitro antiproliferative activity.

• Authors: Shi-Biao Wu, Fei Pang, Ying Wen, Hong-Feng Zhang, Zheng Zhao, Jin-Feng Hu
• Journal: Planta medica (Planta Med) Vol. 76 Issue 1 Pg. 82-5 (Jan 2010) ISSN: 1439-0221 [Electronic] Germany
• PMID: 19653148 (Publication Type: Letter, Research Support, Non-U.S. Gov't)
• Copyright: Copyright Georg Thieme Verlag KG Stuttgart . New York.

Chemical References

• Antineoplastic Agents, Phytogenic
• Drugs, Chinese Herbal
• Furocoumarins

Topics

• Animals
• Antineoplastic Agents, Phytogenic (pharmacology, therapeutic use)
• Apiaceae (chemistry)
• Apoptosis (drug effects)
• Cell Cycle (drug effects)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Drugs, Chinese Herbal (chemistry, pharmacology, therapeutic use)
• Furocoumarins (chemistry, pharmacology, therapeutic use)
• Humans
• Inhibitory Concentration 50
• Neoplasms (drug therapy)
• Phytotherapy
• Rats
• Rhizome
• Structure-Activity Relationship