Abstract

GARCIA-PUPO, Laura; NUNEZ FIGUEREDO, Yanier; TACORONTE MORALES, Juan Enrique  and  DELGADO HERNANDEZ, René. Effect of a new series of synthetic spiroteroids on the PC12 cell line viability. Rev Cubana Farm [online]. 2013, vol.47, n.1, pp. 77-85. ISSN 0034-7515.

Introduction: diosgenin and its derivatives have been described as potent anti-proliferative compounds in several tumor cell lines. However, other structurally-related compounds are reported to exert neuroprotective activity and are also included in food for human consumption. Objective: to evaluate the effect of a novel series of diogesin-derived synthetic spirosteroids on cellular viability of neuron-like PC12 cell line. Methods: cellular viability was determined by the MTT assay along with some theorical molecular descriptors, such as lipophilicity and polar surface area, in order to establish the structure-activity relationships. Results: the results demonstrated that only taurodeoxycholic acid significantly decrease PC12 cell culture viability. Moreover, this molecule presents lower virtual logP values and higher polar surface area values than the rest of spirosteroid series. Conclusions: those results endorse future studies of taurodeoxycholic acid as a potential anti-tumor candidate and of the rest of the molecules in this series as potential neuroprotective agents to be evaluated in this PC12 cell line and similar therapeutic dose.

Keywords : spirosteroids; cytotoxicity; taurodeoxycholic acid; structure-activity relationship.

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