In Vitro Effects of the Neolignan 2,3-Dihydrobenzofuran Against Leishmania Amazonensis

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• 作者：Luciano Gomes de Castro Oliveira ; Lucas Moreira Brito ; Michel Muá ; lem de Moraes Alves ; Layane Valé ; ria Amorim ; Enoque Pereira Costa Sobrinho-Jú ; nior ; Camila Ernanda Sousa de Carvalho ; Klinger Antonio da Franca Rodrigues ; Daniel Dias Rufino Arcanjo ; Antô ; nia Maria das Graç ; as Lopes Citó ; and Fernando Aé ; cio de Amorim Carvalho
• 刊名：Basic & Clinical Pharmacology & Toxicology
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：120
• 期：1
• 页码：52-58
• 全文大小：462K
• ISSN：1742-7843

文摘

Leishmaniasis is an infectious disease complex caused by protozoa from the Leishmania genus, which presents a broad spectrum of clinical manifestations: cutaneous, mucocutaneous and visceral forms. The current treatments are unsatisfactory considering that few drugs are available and present some level of toxicity. Many lignans and neolignans have been used for the development of new antileishmania drugs. The capability in vitro of the neolignan 2,3-dihydrobenzofuran (2,3-DBF), a commonly found constituent of propolis and other plants, to inhibit the growth of promastigote and macrophage-internalized amastigote forms of Leishmania amazonensis was investigated. The cytotoxicity of this compound was assessed by MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) test in BALB/c murine macrophages and human erythrocyte lysis assay. The 2,3-DBF was active against promastigote (IC₅₀=1.042 μM) and amastigote (IC₅₀=1.43 μM) forms, indicating a potent antileishmanial effect. There was no evidence of cytotoxicity to macrophages or erythrocytes at concentrations ranging from 13 to 0.5 μM, after 48 hr of exposure. The antileishmanial activity is probably mediated by the activation of macrophages, because treatment with 2,3-DBF increases both phagocytic and lysosomal activities, as well as the nitrite (NO₂^−) levels. These results suggest that 2,3-DBF may be a potential candidate for the development of a new promising antileishmanial drug. Further studies are needed to determine its potential in vivo effect as well as additional mechanisms underlying the antileishmanial and immunomodulatory activities.