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https://www.arca.fiocruz.br/handle/icict/36036
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2020-10-01
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- INI - Artigos de Periódicos [3397]
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TOXICITY OF TERPENES ON FIBROBLAST CELLS COMPARED TO THEIR HEMOLYTIC POTENTIAL AND INCREASE IN ERYTHROCYTE MEMBRANE FLUIDITY
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Universidade Federal de Goiás. Instituto de Física. Goiânia, GO, Brasil.
Universidade Federal de Goiás. Faculdade de Farmácia. Laboratório de Farmacologia e Toxicologia Celular. Goiânia, GO, Brasil.
Universidade Federal de Goiás. Instituto de Física. Goiânia, GO, Brasil.
Universidade Federal de Goiás. Faculdade de Farmácia. Laboratório de Farmacologia e Toxicologia Celular. Goiânia, GO, Brasil.
Universidade Federal de Goiás. Instituto de Física. Goiânia, GO, Brasil.
Universidade Federal de Goiás. Faculdade de Farmácia. Laboratório de Farmacologia e Toxicologia Celular. Goiânia, GO, Brasil.
Universidade Federal de Goiás. Instituto de Física. Goiânia, GO, Brasil.
Universidade Federal de Goiás. Faculdade de Farmácia. Laboratório de Farmacologia e Toxicologia Celular. Goiânia, GO, Brasil.
Universidade Federal de Goiás. Instituto de Física. Goiânia, GO, Brasil.
Abstract
erpenes are considered potent skin permeation enhancers with low toxicity. Electron paramagnetic res-onance (EPR) spectroscopy of the spin label 5-doxyl stearic acid (5-DSA) was used to monitor the effect ofsesquiterpene nerolidol and various monoterpenes on membrane fluidity in erythrocyte and fibroblastcells. In addition, the hemolytic levels and cytotoxic effects on cultured fibroblast cells were also mea-sured to investigate possible relationships between the cellular irritation potentials of terpenes andthe ability to modify membrane fluidity. All terpenes increased cell membrane fluidity with no significantdifferences between the monoterpenes, but the effect of sesquiterpene was significantly greater than thatof the monoterpenes. The IC50values for the terpenes in the cytotoxicity assay indicated that 1,8-cineoleshowed lower cytotoxicity anda-terpineol and nerolidol showed higher cytotoxicity. The correlationbetween the hemolytic effect and the IC50values for fibroblast viability was low (R= 0.61); however,in both tests, nerolidol was among the most aggressive of terpenes and 1,8-cineole was among the leastaggressive. Obtaining information concerning the toxicity and potency of terpenes could aid in the designof topical formulations optimized to facilitate drug absorption for the treatment of many skin diseases.
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