Anti-tumor 12-deoxyphorbol esters from Euphorbia cornigera.

Full Abstract

Nine (1-8 and 10) new and two (9 and 11) known compounds have been isolated from roots of Euphorbia cornigera Boiss. Their structure and relative stereochemistry were acquired through NMR ((1)H, (13)C, COSY-45, HOHAHA, HMQC, HMBC, NOE and HMBC) spectroscopic measurements. Compounds 1-10 were identified as diesters of 13,20-O-diacyl and 11 as 13-O-acetyl of 12-deoxyphorbol. Cytotoxic activity of the compounds was investigated on human KB cells by reduction of MTT. Compounds 8-10 displayed IC(50) of 0.8, 0.5, and 1.0 microg mL(-1), respectively, whereas the activity of rest of the compounds (1-7) was either very low or (11) zero even up to 1000 microg mL(-1). The inhibition of DNA synthesis through Trypan blue exclusion and Brd-U assay was investigation to figure out the role of compounds 8-10 and concluded that these were responsible for the death of KB cells. Significant correlation has been found between the cytotoxicity and DNA cross-link and DNA strand-break formation.

Author information

Author/s: Baloch, Imam Bakhsh (IB); Baloch, Musa Kaleem (MK); Saqib, Qazi Najam us (QN);

Affiliation: Department of Chemistry, Gomal University, Dera Ismail Khan, Pakistan.

Journal and publication information

Publication Type: Journal Article

Journal: European journal of medicinal chemistry (Eur J Med Chem), published in France. (Language: eng)

Reference: 2008-Feb; vol 43 (issue 2) : pp 274-81

Dates: Created 2008/02/15; Completed 2008/06/19;

PMID: 17512094, status: MEDLINE (last retrieval date: 2/18/2009, IMS Date: )

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