In vivo antimalarial activities of a derivative of secochiliolide acid from Nardophyllum bryoides

In this study, researchers from Argentina and Belgium evaluated the anti-parasitic properties of the derivatives of a compound isolated from Nardophyllum bryoides, a South American flowering plant from the sunflower family. Their results were published in the journal Chemical Biology & Drug Design.

• The researchers synthesized a series of new esters derived from secochiliolide acid (SA), a diterpene from N. bryoides.
• They tested the compounds for anti-parasitic activity using Plasmodium falciparum and Trypanosoma brucei, and cytotoxicity using normal mammalian cells.
• The researchers reported that the SA esters displayed moderate anti-trypanosomal activity, with IC50 values ranging between 2.55 and 18.14 microMolar (uM). However, they showed low antiplasmodial effects, with IC50 values greater than 29 uM.
• The only exception was the n?hexyl ester of SA, which showed strong and selective antiplasmodial activity (IC50 = 1.99 uM).
• Using the 4-day suppressive test of Peters in mice, the researchers assessed the antimalarial efficacy of the n?hexyl ester of SA in vivo.
• Intraperitoneal treatment with the compound at 50mg/kg per day reduced parasitemia by 56 percent, which was statistically significant four days post-infection.
• The compound also increased the survival time of the mice.

Based on these findings, the researchers concluded that the n-hexyl ester of SA from N. bryoides can be used as a potent antimalarial agent.

Journal Reference:

Ronchi RJ, Beaufay C, Bero J, Robirosa JB, Mazzuca M, Palermo JA, Quetin?Leclercq J, Sanchez M. SECOCHILIOLIDE ESTER DERIVATIVES: PREPARATION AND EVALUATION OF THEIR ANTITRYPANOSOMAL AND ANTIMALARIAL EFFICACY. Chemical Biology & Drug Design. 14 September 2018;93(2):147-153. DOI: 10.1111/cbdd.13392