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Synthesis, Cytotoxicity, and Antitumor Activity of Lantadene‐A Congeners
Author(s) -
Sharma Manu,
Sharma Pritam Dev,
Bansal Mohinder Pal,
Singh Jaswant
Publication year - 2007
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.200790082
Subject(s) - chemistry , dmba , lantana camara , cytotoxicity , in vivo , stereochemistry , terpene , cell culture , oleanolic acid , pharmacology , triterpene , carcinogenesis , 12 o tetradecanoylphorbol 13 acetate , in vitro , biochemistry , phorbol ester , biology , enzyme , botany , medicine , genetics , microbiology and biotechnology , alternative medicine , pathology , gene , protein kinase c
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 μ M , 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.