Synthesis of 3-(2, 8, 9-trioxa-5-aza-1-germatricyclo [3.3.3.0] Undecane-1- yl)-3-(4-hydroxyl-3-methoxyphenyl)-propionic Acid and its Inhibitory Effect on the Cervical Tumor U14 in vitro and in vivo

Abstract

In this study, the novel germatrane compound, 3-(2, 8, 9-trioxa-5-aza-1- germatricyclo [3.3.3.0] undecane-1-yl)-3-(4-hydroxy-3- methoxyphenyl)-propionic acid (1), has been synthesized and its activities against cervical tumor U14 were evaluated in vitro and in vivo. The results have demonstrated that the compound posed significant inhibition on U14 tumor with IC(50) values of 48.57 mg/L in cell-based assay and tumor inhibitory rates of 38.50%, 47.17% and 64.02% (from low dose to high dose) in animal experiment.

Physiological Activity of Trace Element Germanium Including Anticancer Properties

“…Based on caffeic acid 3-germatranyl-3-(4-hydroxy-3-methoxyphenyl) propionic acid ( 3 ) was synthesized, which showed strong activity against cervical tumor U14 (in vitro and in vivo). This had inhibitory activity against cervical cancer cell line U14 with an IC50 as high as 48.57 mg/L (117.32 µM), whereas the degree of inhibition of the tumor growth is 64% in the animal experiment [ 114 ]. 2-aminoethoxy-substituted germatrane ( 1 , R = OCH 2 CH 2 NH 2 ) inhibits the activity of mononuclear alkaline phospholipase A2, and may serve for the development of new antisclerotic drugs to prevent lipid metabolism disorders [ 115 ].…”

Physiological Activity of Trace Element Germanium Including Anticancer Properties

“…Based on caffeic acid 3-germatranyl-3-(4-hydroxy-3-methoxyphenyl) propionic acid (3) was synthesized, which showed strong activity against cervical tumor U14 (in vitro and in vivo). It had inhibitory activity against cervical cancer cell line U14 with IC50 as high as 48.57 mg/L (117.32 µM), whereas the degree of inhibition of the tumor growth is 64% in the animal experiment [119]. 2-aminoethoxy-substituted germatrane (1, R = OCH2CH2NH2) inhibits the activity of mononuclear alkaline phospholipase A2, and may serve for the development of new antisclerotic drugs to prevent lipid metabolism disorders [120].…”