squamosa seeds extract containing annonaceous acetogenin compounds

CHEN Yong; XU Shasha; CHEN Jianwei; WANG Yu; XU Huiqing; FAN Naibing; LI Xiang

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squamosa seeds extract containing annonaceous acetogenin compounds

CHEN Yong,XU Shasha,CHEN Jianwei,WANG Yu,XU Huiqing,FAN Naibing,LI Xiang * #

College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210046

*Correspondence author

#Submitted by

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Funding: Jiangsu Key Laboratory for Pharmacology and Safety Evaluation of Chinese Material Medica （No.No. P09018）, the Project Funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions （No.No. ysxk-2010）, Doctoral Fund of Ministry of Education of China （No.No. 20113237110009) and 2011 Program sponsored for scientific innovation research of college graduate in Jiangsu province）

Opened online:22 May 2012

Accepted by: none

Citation: CHEN Yong,XU Shasha,CHEN Jianwei.squamosa seeds extract containing annonaceous acetogenin compounds[OL]. [22 May 2012] http://en.paper.edu.cn/en_releasepaper/content/4478623

Seeds of Annona squamosa L. have been used in the south of China as a folk remedy to treat "malignant sores" (cancer). To investigate the chemical constituents and the anti-tumor activity of the standardized A. squamosa seeds extract in vitro and in vivo. Annonaceous acetogenin profiles of the standardized extract were determined by using Fourier transform infrared (FT-IR) and high performance liquid chromatography (HPLC) techniques. The anti-tumor activity of the extract was tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) cytotoxicity in vitro and H22 hepatoma cells transplantation tumor model in vivo. The FT-IR spectroscopy showed the presence of annonaceous acetogenin compounds in the extract. Two major annonaceous acetogenins: 12, 15-cis-squamostatin-A and bullatacin were identified and quantified by HPLC. The seed extract showed significant anti-tumor activity against four human tumor cell lines, especially for MCF-7 (IC50. 0.25 μg/ml) and Hep G2 (IC50. 0.36 μg/ml) cells in vitro. The extract inhibited the growth of H22 tumor cells in mice with a maximum inhibitory rate of 69.55% by oral administration. A. squamosa seed extract showed significant anti-tumor activities against human hepatoma cells in vitro and in vivo, indicating a potential for developing the extract as a novel anti-liver cancer drug.

Keywords:chemistry of Chinese Medicine; Annona squamosa; Anti-tumor; HPLC; Annonaceous acetogenin

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