Journal
MOLECULES
Volume 27, Issue 4, Pages -Publisher
MDPI
DOI: 10.3390/molecules27041151
Keywords
piperaceae; lignans; medicinal plants; secondary metabolites; vascular reactivity
Funding
- CAPES
- FAPERJ
- PROEP-CNPQ
- Pharmaceutical Institute of Technology at Oswaldo Cruz Foundation
- Botanical Garden Research Institute of Rio de Janeiro
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Piper species, especially Piper tectoniifolium Kunth, are potential natural sources of the bioactive compound (-)-grandisin. A new method for identifying (-)-grandisin was developed, and the molecule was found to have a vasorelaxant effect. These findings suggest that P. tectoniifolium has the potential to be a renewable source of grandisin and a template for the development of new drugs.
The Piper species are a recognized botanical source of a broad structural diversity of lignans and its derivatives. For the first time, Piper tectoniifolium Kunth is presented as a promising natural source of the bioactive (-)-grandisin. Phytochemical analyses of extracts from its leaves, branches and inflorescences showed the presence of the target compound in large amounts, with leaf extracts found to contain up to 52.78% in its composition. A new HPLC-DAD-UV method was developed and validated to be selective for the identification of (-)-grandisin being sensitive, linear, precise, exact, robust and with a recovery above 90%. The absolute configuration of the molecule was determined by X-ray diffraction. Despite the identification of several enantiomers in plant extracts, the major isolated substance was characterized to be the (-)-grandisin enantiomer. In vascular reactivity tests, it was shown that the grandisin purified from botanical extracts presented an endothelium-dependent vasorelaxant effect with an IC50 of 9.8 +/- 1.22 mu M and around 80% relaxation at 30 mu M. These results suggest that P. tectoniifolium has the potential to serve as a renewable source of grandisin on a large scale and the potential to serve as template for development of new drugs for vascular diseases with emphasis on disorders related to endothelial disfunction.
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