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Molecules 2014, 19(1), 581-594;

Gastroprotective Mechanisms of Action of Semisynthetic Carnosic Acid Derivatives in Human Cells

Laboratorio de Cultivo Celular, Facultad de Ciencias de la Salud, Universidad de Talca, Casilla 747, Talca 3460000, Chile
Laboratorio de Química de Productos Naturales, Instituto de Química de Recursos Naturales, Universidad de Talca, Casilla 747, Talca 3460000, Chile
Author to whom correspondence should be addressed.
Received: 2 December 2013 / Revised: 30 December 2013 / Accepted: 30 December 2013 / Published: 6 January 2014
(This article belongs to the Section Medicinal Chemistry)
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Carnosic acid (CA) and its semisynthetic derivatives display relevant gastroprotective effects on HCl/ethanol induced gastric lesions in mice. However, little is known on the mechanisms of action of the new compounds. The aim of the present work was to assess the gastroprotective action mechanisms of CA and its derivatives using human cell culture models. A human gastric adenocarcinoma cell line (AGS) and lung fibroblasts (MRC-5) were used to reveal the possible mechanisms involved. The ability of the compounds to protect cells against sodium taurocholate (NaT)-induced damage, and to increase the cellular reduced glutathione (GSH) and prostaglandin E2 (PGE2) content was determined using AGS cells. Stimulation of cell proliferation was studied employing MRC-5 fibroblasts. Carnosic acid and its derivatives 1018 raised GSH levels in AGS cells. While CA did not increase the PGE2 content in AGS cells, all derivatives significantly stimulated PGE2 synthesis, the best effect being found for the 12-O-indolebutyrylmethylcarnosate 13. A significant increase in MRC-5 fibroblast proliferation was observed for the derivatives 7 and 1618. The antioxidant effect of the compounds was assessed by the inhibition of lipid peroxidation in human erythrocyte membranes, scavenging of superoxide anion and DPPH discoloration assay. The new CA derivatives showed gastroprotective effects by different mechanisms, including protection against cell damage induced by NaT, increase in GSH content, stimulation of PGE2 synthesis and cell proliferation. View Full-Text
Keywords: action mechanisms; gastroprotective; carnosic acid; diterpenes action mechanisms; gastroprotective; carnosic acid; diterpenes

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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Theoduloz, C.; Pertino, M.W.; Schmeda-Hirschmann, G. Gastroprotective Mechanisms of Action of Semisynthetic Carnosic Acid Derivatives in Human Cells. Molecules 2014, 19, 581-594.

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