Boluda Carlos J, Trujillo Juan M, Pérez José A, López Hermelo, Aragón Zulma, Díaz Raquel G
Instituto Universitario de Bioorgáinica Antonio González, Universidad de La Laguna, Avda. Astrofisico F. Sánchez, 2, 38206 La Laguna, Tenerife, Canary Islands, Spain.
Nat Prod Commun. 2009 Feb;4(2):235-8.
The dioxo-lignans of the arylnaphthalene-type named justicidone (2) and elenodione (3) were obtained from elenoside (1) through a short and efficient semisynthetic process. Justicidone (2), one of its synthetic precursors, 4-(benzo[d][1,3]dioxol-5-yl)-5,6,8-trimethoxy-3a,4-dihydronaphtho[2,3-c]furan-1(3H)-one (9), and the aglycone of elenoside (5) showed cytotoxic activity towards the HL-60 cell line (IC50 = 7.25 miroM, 5.41 microM and 2.06 miroM, respectively).
通过一个简短而高效的半合成过程，从elenoside（1）中获得了芳基萘型的二氧代木脂素，即justicidone（2）和elenodione（3）。Justicidone（2）、其合成前体之一4-(苯并[d][1,3]二氧杂环戊烯-5-基)-5,6,8-三甲氧基-3a,4-二氢萘并[2,3-c]呋喃-1(3H)-酮（9）以及elenoside（5）的苷元对HL-60细胞系显示出细胞毒性活性（IC50分别为7.25 μM、5.41 μM和2.06 μM）。
