Antileishmanial activity and immunomodulatory effect of seco subamolide, a butanolide isolated from Nectandra oppositifolia (Lauraceae)

从樟科植物油藤中分离的丁酸内酯 seco subamolide 的抗利什曼原虫活性和免疫调节作用

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作者:Thais A da Costa-Silva, Geanne A Alves Conserva, Andrés J Galisteo Jr, Andre G Tempone, João Henrique G Lago

Background

Visceral leishmaniasis is a complex neglected tropical disease caused by Leishmania donovani 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 Nectandra oppositifolia (Lauraceae) was investigated herein.

Conclusion

This study showed the antileishmanial activity of compounds 1 and 2 isolated from N. oppositifolia. Furthermore, compound 2 demonstrated an antileishmanial activity towards amastigotes associated to an immunomodulatory effect.

Methods

The n-hexane extract from twigs of N. oppositifolia were subjected to HPLC/HRESIMS and bioactivity-guided fractionation to afford compounds 1 and 2 which were evaluated in vitro against Leishmania (L.) infantum chagasi and NCTC cells.

Results

The n-hexane extract displayed activity against L. (L.) infantum chagasi and afforded isolinderanolide E (1) and secosubamolide A (2), which were effective against L. (L.) infantum chagasi promastigotes, with IC50 values of 57.9 and 24.9 µM, respectively. Compound 2 was effective against amastigotes (IC50 = 10.5 µM) and displayed moderate mammalian cytotoxicity (CC50 = 42 µM). The immunomodulatory studies of compound 2 suggested an anti-inflammatory activity, with suppression of IL-6, IL-10, TNF with lack of nitric oxide.

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