Sirignano, Carmina (2018) Phytochemical and synthetic studies on bioactive secondary metabolites from Apiaceae plants growing in Mediterranean and Middle-East regions. [Tesi di dottorato]

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Item Type: Tesi di dottorato
Lingua: English
Title: Phytochemical and synthetic studies on bioactive secondary metabolites from Apiaceae plants growing in Mediterranean and Middle-East regions
Creators:
CreatorsEmail
Sirignano, Carminacarmina.sirignano@unina.it
Date: 11 December 2018
Number of Pages: 151
Institution: Università degli Studi di Napoli Federico II
Department: Farmacia
Dottorato: Scienza del farmaco
Ciclo di dottorato: 31
Coordinatore del Corso di dottorato:
nomeemail
D'Auria, Maria Valeriamadauria@unina.it
Tutor:
nomeemail
Rigano, DanielaUNSPECIFIED
Date: 11 December 2018
Number of Pages: 151
Uncontrolled Keywords: Natural products, secondary metabolites, total synthesis, Daucus virgatus, Echinophora platyloba
Settori scientifico-disciplinari del MIUR: Area 05 - Scienze biologiche > BIO/15 - Biologia farmaceutica
Date Deposited: 19 Dec 2018 11:59
Last Modified: 23 Jun 2020 09:26
URI: http://www.fedoa.unina.it/id/eprint/12655

Abstract

Natural products represent a remarkable source of lead molecules for drug discovery, given their impressive structural diversity and their still unexplored potential. Considering that more than 90% of the world’s biodiversity still waits to be investigated, Nature continues to be a gold mine of new chemotypes and pharmacophores. Thus, taking into account all the potential sources, including plants, fungi, bacteria, and marine environment, approximately one-third of all New Molecular Entities (NMEs) approved by Food and Drug Administration (FDA) derives from natural products. In this context, the research work reported in this Ph.D. thesis has been focused on the phytochemical investigation of plants belonging to the Iranian and Northern African flora, in order to discover and rationalize their pharmacological potential. In particular, the first part of my work has been devoted to the characterization of the polyacetylene fraction of Echinophora platyloba, which pointed out a new interesting TRPA1 modulating activity of C14 polyacetylenes isolated from this Iranian endemic plant. Subsequently, the bio-guided fractionation of the apolar extract obtained from Daucus virgatus, a Tunisian endemic plant, led to the isolation of angeloylated germacranolides showing a promising Plasmodium transmission blocking activity. Moreover, the complete phytochemical characterization of D. virgatus apolar extract has resulted in the isolation of additional antiproliferative secondary metabolites. Part of my Ph.D. project has been spent at University College of Dublin (UCD), to design and initiate a synthetic strategy for the preparation of daucovirgolide G, the angeloylated germacranolide that showed the most promising anti-malarial activity, among all those isolated from D. virgatus. The total synthesis of daucovirgolide G, which is still in progress, will have as final goal the preparation of the active compound and of several analogues to be pharmacologically evaluated. The results obtained during my Ph.D. have been reported in nine papers already published or ready for publication.

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