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Acute effect of [beta]-sitosterol on calcium uptake mediates anti-inflammatory effect in murine activated neutrophils.
Liz, Rafael 1; Zanatta, Leila 2; dos Reis, Gustavo Oliveira 1; Horst, Heros 3; Pizzolatti, Moacir Geraldo 3; Silva, Fatima Regina Mena Barreto 2; Frode, Tania Silvia 1
[Article] Journal of Pharmacy & Pharmacology. 65(1):115-122, January 2013.

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Objectives: To evaluate the effect of [beta]-sitosterol on 45Ca2 uptake in activated murine neutrophils, and upon myeloperoxidase and adenosine deaminase activity, and interleukin-1[beta] (IL-1[beta]) and tumour necrosis factor-[alpha] (TNF-[alpha]) levels, in carrageenan-induced inflammation in the mouse air pouch model.

Methods: Dried Esenbeckia leiocarpa bark was macerated and extracted resulting in a crude hydroalcoholic extract (CHE) that was partitioned to obtain an alkaloid fraction. The alkaloid was then partitioned in polar and nonpolar subfractions. [beta]-Sitosterol was isolated from the nonpolar subfraction and identified by comparison with the literature. The effect of [beta]-sitosterol on 45Ca2 uptake in activated murine neutrophils, and upon myeloperoxidase and adenosine deaminase activity, IL-1[beta] and TNF-[alpha] levels in carrageenan-induced inflammation in mice were evaluated.

Key findings: [beta]-Sitosterol promoted a time- and dose-dependent increase of the calcium uptake in activated neutrophils that was promptly reversed by nifedipine, BAPTA-AM, LY294002, and colchicine. [beta]-Sitosterol inhibited myeloperoxidase and adenosine deaminase activity, and IL-1[beta] and TNF-[alpha] levels.

Conclusions: [beta]-Sitosterol inhibited either myeloperoxidase and adenosine deaminase activity or IL-1[beta] and TNF-[alpha] levels. This effect seemed to be mediated by the calcium uptake in activated neutrophils in a time- and concentration-dependent manner through L-type voltage dependent calcium channels, intracellular calcium, phosphoinositide kinase-3, and microtubule modulation.