4.5 Article

Antitumor activity of annonaceous acetogenins in HepS and S180 xenografts bearing mice

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 8, Pages 2717-2719

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.02.109

Keywords

Annonaceous acetogenins; In vivo; HepS; S180; Xenograft

Funding

  1. Jiangsu Key Laboratory for Pharmacology and Safety Evaluation of Chinese Materia Medica [P09018]
  2. Jiangsu Administration of Traditional Chinese Medicine [LZ09001]
  3. Priority Academic Program Development of Jiangsu Higher Education Institutions [ysxk-2010]
  4. Ministry of Education of China [20113237110009]
  5. Jiangsu province [790]

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Annonaceous acetogenins (ACGs), as one of the most powerful groups of mitochondrial complex I inhibitors, exhibit potent cytotoxic activity against a variety of human tumor cell lines. In this study, the antitumor activities of three main types of ACGs were investigated using S180 and HepS xenografts bearing mice simultaneously. The results revealed that select ACGs suppressed tumor growth in a dose-dependent fashion. Tested ACGs showed more selective antitumor activity against HepS. Furthermore, adjacent bis-THF ACGs were more active than mono-THF and nonadjacent bis-THF ACGs against HepS and S180; nonadjacent bis-THF ACGs were more active than mono-THF ACGs against S180, but mono-THF ACGs were more potent than nonadjacent bis-THF ACGs against HepS. (C) 2012 Elsevier Ltd. All rights reserved.

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