da Costa-Silva Thais A, Conserva Geanne A Alves, Galisteo Andrés J, Tempone Andre G, Lago João Henrique G
Center of Natural Sciences and Humanities, Federal University of ABC (UFBAC), São Paulo, SP, Brazil.
Institute of Tropical Medicine, University of São Paulo (USP), São Paulo, SP, Brazil.
J Venom Anim Toxins Incl Trop Dis. 2019 Aug 19;25:e20190008. doi: 10.1590/1678-9199-JVATITD-2019-0008. eCollection 2019.
Visceral leishmaniasis is a complex neglected tropical disease caused by complex. Its current treatment reveals strong limitations, especially high toxicity. In this context, natural products are important sources of new drug alternatives for VL therapy. Therefore, the antileishmanial and immunomodulatory activity of compounds isolated from (Lauraceae) was investigated herein
The -hexane extract from twigs of were subjected to HPLC/HRESIMS and bioactivity-guided fractionation to afford compounds and which were evaluated against () and NCTC cells.
The -hexane extract displayed activity against () and afforded linderanolide E () and subamolide A (), which were effective against () promastigotes, with IC values of 57.9 and 24.9 µM, respectively. Compound was effective against amastigotes (IC = 10.5 µM) and displayed moderate mammalian cytotoxicity (CC = 42 µM). The immunomodulatory studies of compound suggested an anti-inflammatory activity, with suppression of IL-6, IL-10, TNF with lack of nitric oxide.
This study showed the antileishmanial activity of compounds and isolated from . Furthermore, compound demonstrated an antileishmanial activity towards amastigotes associated to an immunomodulatory effect.
内脏利什曼病是一种由寄生虫引起的复杂的被忽视的热带疾病。其目前的治疗方法存在很大局限性,尤其是毒性高。在此背景下,天然产物是内脏利什曼病治疗新药替代品的重要来源。因此,本文研究了从樟科植物中分离出的化合物的抗利什曼原虫和免疫调节活性。
对樟科植物嫩枝的正己烷提取物进行高效液相色谱/高分辨电喷雾电离质谱分析和生物活性导向分离,得到化合物1和2,并对其进行了抗杜氏利什曼原虫(Leishmania donovani)和NCTC细胞的活性评价。
正己烷提取物对杜氏利什曼原虫显示出活性,并得到了linderanolide E(1)和subamolide A(2),它们对杜氏利什曼原虫前鞭毛体有效,IC50值分别为57.9和24.9 μM。化合物2对无鞭毛体有效(IC50 = 10.5 μM),并显示出中等程度的哺乳动物细胞毒性(CC50 = 42 μM)。化合物2的免疫调节研究表明其具有抗炎活性,可抑制白细胞介素-6、白细胞介素-10、肿瘤坏死因子,且不产生一氧化氮。
本研究表明从樟科植物中分离出的化合物1和2具有抗利什曼原虫活性。此外,化合物2对无鞭毛体表现出抗利什曼原虫活性,并具有免疫调节作用。