Antiproliferative activity of semisynthetic xylopic acid derivatives

被引:4
作者
Soh, Desire [1 ,2 ,3 ]
Ernestine, Nkwengoua [3 ]
Tchana Satchet, Emmanuella Marthe [3 ]
Defokou, Ulrich Dzo [3 ]
Schneider, Bernd [4 ]
Giovanni, Vidari [5 ,6 ]
Nyasse, Barthelemy [3 ]
机构
[1] Univ Bamenda, Higher Teacher Training Coll, Dept Chem, Bambili, Cameroon
[2] Univ Bamenda, TWAS Res Unit TRU, Bamenda, Cameroon
[3] Univ Yaounde I, Dept Organ Chem, Lab Med Chem & Pharmacognosy, Fac Sci, Yaounde, Cameroon
[4] Max Planck Inst Chem Ecol, Jena, Germany
[5] Univ Pavia, Dept Chem, Pavia, Italy
[6] Tishk Int Univ, Dept Med Anal, Fac Sci, Erbil, Kurdistan Regio, Iraq
关键词
Xylopia aethiopica; annonaceae; ent-kaurane diterpenoids; xylopic acid; antiproliferative activity; semisynthesis;
D O I
10.1080/14786419.2021.1876045
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
Two ent-kaurene diterpenoids, ent-15- beta -acetyloxy-kaur-16-en-19-oic acid (xylopic acid) 1 and ent-7-oxo-kaur-16-en-19-oic acid 2 were isolated from the fruits of Xylopia aethiopica. Chemical manipulation of xylopic acid yielded ent-kaurane derivatives 3, 4, 5, and 6. Their structures were elucidated by spectroscopic analysis, including 1 D- and 2 D-NMR spectroscopies. The antiproliferative activities of compounds 1, 2, 3, 4, and 6 were tested on breast MCF7 and SkBr3, endometrial Ishikawa, ovarian BG-1, mesothelioma IST-MES1 and hepatocellular HepG2 human tumor cells, and on mammalian MRC-10 fibroblast cells. Ketone 2 showed significant antiproliferative activity against MFC7 human breast cancer cells (IC50 = 3 +/- 1 mu M) and A549 pulmonary adenocarcinoma (8 +/- 1 mu M), that was higher than the well-known anti-cancer agent cisplatin (IC50 = 19 +/- 3 and 15 +/- 4 mu M, respectively).
引用
收藏
页码:1288 / 1295
页数:8
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