Thyroid peroxidase inhibition by Kalanchoe brasiliensis aqueous extract.
Flavonoids are known inhibitors of thyroid peroxidase (TPO) and some are components of Kalanchoe brasiliensis, a plant used in popular medicine to treat tissue injuries, enlarged ganglia and peptic ulcer. As K. brasiliensis extract is currently used, the present study was designed to evaluate the effects of K. brasiliensis aqueous extract on TPO activity. We show here that TPO iodide-oxidation activity was significantly inhibited by K. brasiliensis aqueous extract and that TPO inhibition seems to be competitive, since the enzyme V(max) was unchanged and K(m) for iodide was significantly increased in the presence of the plant extract. Furthermore, TPO inhibitory activity produced by K. brasiliensis extract was unchanged after boiling or by incubation with hepatic enzymes (activated S9 fraction), suggesting that at least the antithyroid component of this plant infusion could probably reach systemic circulation. We also report that K. brasiliensis aqueous extract is able to scavenge H(2)O(2), in vitro. As H(2)O(2) is an essential TPO cofactor, it is possible that the H(2)O(2) trapping effect of K. brasiliensis may be responsible, at least in part, for the inhibition of the iodide-oxidation reaction catalysed by this enzyme. Thus, K. brasiliensis aqueous extract has antithyroid effects in vitro, suggesting that its chronic consumption could contribute to the development of goitre and hypothyroidism, mainly in areas of low iodine intake.
Ferreira
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Laboratório de Fisiologia Endócrina, Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil.
Rosenthal
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Carvalho
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D000818:Animals; D000975:Antioxidants / Q000494:pharmacology; D013956:Antithyroid Agents / Q000494:pharmacology*; D001938:Brazil; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D016166:Free Radical Scavengers / Q000494:pharmacology; D006358:Hot Temperature; D006801:Humans; D006861:Hydrogen Peroxide / Q000378:metabolism; D066298:In Vitro Techniques; D007453:Iodide Peroxidase / Q000037:antagonists & inhibitors*; D007454:Iodides / Q000737:chemistry; D008713:Methimazole / Q000494:pharmacology; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism; D016877:Oxidants / Q000378:metabolism; D010084:Oxidation-Reduction; D010936:Plant Extracts / Q000494:pharmacology*; D010946:Plants, Medicinal / Q000737:chemistry*; D011441:Propylthiouracil / Q000494:pharmacology; D051381:Rats
D000975:Antioxidants; D013956:Antithyroid Agents; D004791:Enzyme Inhibitors; D016166:Free Radical Scavengers; D007454:Iodides; D016877:Oxidants; D010936:Plant Extracts; D008713:Methimazole; D011441:Propylthiouracil; D006861:Hydrogen Peroxide; D007453:Iodide Peroxidase