Cytotoxicity and structure activity relationship studies of maplexins A-I, gallotannins from red maple (Acer rubrum)

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• 作者：Antonio Gonzá ; lez-Sarrí ; as ; Tao Yuan ; Navindra P. Seeramp> ; p>p>nseeram@uri.edup>
• 关键词：Acer rubrum ; Red maple ; Maplexins ; Antiproliferative ; Colon cancer cells ; Breast cancer cells
• 刊名：Food and Chemical Toxicology
• 出版年：2012
• 出版时间：May, 2012
• 年：2012
• 卷：50
• 期：5
• 页码：1369-1376
• 全文大小：829 K

文摘

Maplexins A-I are a series of structurally related gallotannins recently isolated from the red maple (Acer rubrum) species. They differ in number and location of galloyl derivatives attached to 1,5-anhydro-glucitol. Here, maplexins A-I were evaluated for anticancer effects against human tumorigenic (colon, HCT-116; breast, MCF-7) and non-tumorigenic (colon, CCD-18Co) cell lines. The maplexins which contained two (maplexins C-D) or three (maplexins E-I) galloyl derivatives each, inhibited cancer cell growth while those with only one galloyl group (maplexins A-B) did not. Moreover, maplexins C-D showed greater antiproliferative effects than maplexins E-I (IC₅₀ = 59.8-67.9 and 95.5-108.5 ¦ÌM vs. 73.7-165.2 and 115.5-182.5 ¦ÌM against HCT-116 and MCF-7 cells, respectively). Notably, the cancer cells were up to 2.5-fold more sensitive to the maplexins than the normal cells. In further mechanistic studies, maplexins C-D (at 75 ¦ÌM concentrations) induced apoptosis and arrested cell cycle (in the S-phase) of the cancer cells. These results suggest that the number of galloyl groups attached to the 1,5-anhydro-glucitol moiety in these gallotannins are important for antiproliferative activity. Also, this is the first in vitro anticancer study of maplexins.