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Synthesis, Cytotoxicity, and Antitumor Activity of Lantadene-A Congeners

✍ Scribed by Manu Sharma; Pritam Dev Sharma; Mohinder Pal Bansal; Jaswant Singh

Publisher
John Wiley and Sons
Year
2007
Tongue
English
Weight
138 KB
Volume
4
Category
Article
ISSN
1612-1872

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✦ Synopsis

Abstract

Five new derivatives of the pentacyclic triterpenoid lantadene A (=22__β__‐angeloyloxy‐3‐oxoolean‐12‐en‐28‐oic acid; 1) from the leaves of Lantana camara L. were synthesized, characterized, and screened for their cytotoxicities against four human cancer cell lines. The three most‐potent compounds, i.e., 1, 4, and 6, with IC~50~ values in the range of ca. 20–29 μM, were further studied for their in vivo tumor‐inhibitory potential upon oral administration in two‐stage squamous cell carcinogenesis, using female Swiss albino mice, papilloma being induced by 7,12‐dimethylbenz[a]anthracene (DMBA), and promoted by 12‐O‐tetradecanoylphorbol‐13‐acetate (TPA). The results are discussed in terms of structure–activity relationship.

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