Caffeic acid esters and lignans from Piper sanguineispicum

Area of Science:

• Natural Product Chemistry
• Pharmacognosy
• Parasitology

Background:

• Piper species are a rich source of bioactive natural products.
• Leishmaniasis remains a significant global health concern, necessitating novel therapeutic agents.

Purpose of the Study:

• To isolate and characterize novel compounds from Piper sanguineispicum leaves.
• To evaluate the antileishmanial potential of isolated compounds against Leishmania amazonensis.

Main Methods:

• Isolation of compounds using chromatographic techniques.
• Structure elucidation via 1D and 2D NMR, HRCIMS, and CD spectroscopy.
• Antileishmanial activity assay against axenic amastigote forms of Leishmania amazonensis.

Main Results:

• Three new caffeic acid esters (1-3) and four new lignans (4-7) were identified.
• Caffeic acid esters 1 and 3 demonstrated potent antileishmanial activity with IC(50) values of 2.0 μM and 1.8 μM, respectively.
• Compounds 1 and 3 exhibited moderate cytotoxicity against murine macrophages.

Conclusions:

• Piper sanguineispicum is a valuable source of novel bioactive compounds.
• Caffeic acid esters 1 and 3 show significant potential as lead compounds for antileishmanial drug development.
• Further investigation into the mechanism of action and toxicity profile of these compounds is warranted.