Synthesis of novel anticancer iridoid derivatives and their cell cycle arrest and caspase dependent apoptosis

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• 作者：Sukanya Pandeti^a ; Komal Sharma^b ; Surendar Reddy Bathula^b ; ^{bsreddy@cdri.res.in" class="auth_mail} ; Narender Tadigoppula^a ; ^{t_narendra@cdri.res.in" class="auth_mail} ; ^{tnarender@rediffmail.com" class="auth_mail}
• 关键词：7-O-trans-cinnamoyl 6尾-hydroxyloganin derivatives ; Arbortristoside-A ; Anticancer agents ; Apoptosis ; Nyctanthes arbortristis
• 刊名：Phytomedicine
• 出版年：15 February, 2014
• 年：2014
• 卷：21
• 期：3
• 页码：333-339
• 全文大小：1281 K

文摘

Nyctanthes arbortristis Linn (Oleaceae) is widely distributed in sub-Himalayan regions and southwards to Godavari, India commonly known as Harsingar and Night Jasmine. In continuation of our drug discovery programme on Indian medicinal plants, we isolated arbortristoside-A (1) and 7-O-trans-cinnamoyl 6尾-hydroxyloganin (2) from the seeds of N. Arbortristis, which exhibited moderate in vitro anticancer activity. Chemical transformation of 2 led to significant improvement in the activity in derivative 8 and 15 against HepG2 (human hepatocellular carcinoma), MCF-7 (breast adenocarcinoma) cell lines. The compounds 8 and 15 were also capable of cell cycle arrest and caspase dependent apoptosis in HepG2 cell lines. These iridoid derivatives hold promise for developing safer alternatives to the marketed drugs.