Planta Med 2010; 76(1): 82-85
DOI: 10.1055/s-0029-1185971
Pharmacology
Letters
© Georg Thieme Verlag KG Stuttgart · New York

Antiproliferative and Apoptotic Activities of Linear Furocoumarins from Notopterygium incisum on Cancer Cell Lines

Shi-Biao Wu1 , Fei Pang2 , Ying Wen3 , Hong-Feng Zhang2 , Zheng Zhao3 , Jin-Feng Hu1
  • 1Key Laboratory of Brain Functional Genomics, East China Normal University, Shanghai, P. R. China
  • 2Department of Biomedicine, School of Life Science, East China Normal University, Shanghai, P. R. China
  • 3Department of Neuropharmacology and Toxicology, Key Laboratory of Brain Functional Genomics, Ministry of Education and Shanghai Key Laboratory of Brain Functional Genomics, East China Normal University, Shanghai, P. R. China
Further Information

Publication History

received February 24, 2009 revised June 18, 2009

accepted June 19, 2009

Publication Date:
03 August 2009 (online)

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 (19). 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-[(2E,5Z)-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 IC50 values of 7.7–24.8 µg/mL (5-FU: ca. 5 µg/mL). Compounds 13 also showed moderate cytotoxicity against the MCF-7 cancer cell line, with IC50 values of 39.4–61.3 µg/mL (5-FU: 17.3 µg/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.

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Prof. Dr. Jin-Feng Hu

Department of Natural Products for Chemical Genetic Research
Key Laboratory of Brain Functional Genomics
Ministry of Education and
Shanghai Key Laboratory of Brain Functional Genomics
East China Normal University

3663 Zhongshan Road N

Shanghai 200062

People's Republic of China

Phone: + 86 21 62 23 75 10

Fax: + 86 21 62 60 67 91

Email: jfhu@brain.ecnu.edu.cn

Dr. Hong-Feng Zhang Associate Professor

Department of Biomedicine
School of Life Science
East China Normal University

3663 Zhongshan Road N

Shanghai 200062

People's Republic of China

Phone: + 86 21 62 23 35 49

Fax: + 86 21 62 23 37 54

Email: hfzhang@bio.ecnu.edu.cn

Dr. Zheng Zhao Associate Professor

Department of Neuropharmacology and Toxicology
Key Laboratory of Brain Functional Genomics
Ministry of Education and Shanghai Key Laboratory of Brain Functional Genomics
East China Normal University

3663 Zhongshan Road N

Shangahi 200062

People's Republic of China

Phone: + 86 21 62 23 80 05

Fax: + 86 21 62 60 19 53

Email: zzhao@brain.ecnu.edu.cn