Parthenin—A Sesquiterpene Lactone with Multifaceted Biological Activities: Insights and Prospects

Abstract

Parthenin, a sesquiterpene lactone of pseudoguaianolide type, is the representative secondary metabolite of the tropical weed Parthenium hysterophorus (Asteraceae). It accounts for a multitude of biological activities, including toxicity, allergenicity, allelopathy, and pharmacological aspects of the plant. Thus far, parthenin and its derivatives have been tested for chemotherapeutic abilities, medicinal properties, and herbicidal/pesticidal activities. However, due to the lack of toxicity–bioactivity relationship studies, the versatile properties of parthenin are relatively less utilised. The possibility of exploiting parthenin in different scientific fields (e.g., chemistry, medicine, and agriculture) makes it a subject of analytical discussion. The present review highlights the multifaceted uses of parthenin, on-going research, constraints in the practical applicability, and the possible workarounds for its successful utilisation. The main aim of this comprehensive discussion is to bring parthenin to the attention of researchers, pharmacologists, natural product chemists, and chemical biologists and to open the door for its multidimensional applications.

Sesquiterpene Lactone-Rich Extract of Tithonia diversifolia (Hemsley) A. Gray (Asteraceae) suppresses Trypanosoma brucei brucei in both In Vivo and In Vitro Experimental Models

“…This class of phytochemical constituent of plants has been implicated to possess anti-trypanosomal activities against different strains of Trypanosoma species. 23,24 However, the present study did not isolate, quantify or characterize the STLs from the VLC sub-fractions responsible for the moderate cytostatic and strong anti-trypanosomal activities against human foreskin fibroblast and Trypanosoma brucei brucei respectively. To further confirm the consistency in the strong antitrypanosomal activity of the STL constituents of T. diversifolia,…”

“…The efficacy of the STLs-rich extracts against AAT-causing animal trypanosomiasis complements several other pharmacological properties of T. diversifolia towards discovering potent phyto-molecules. [7][8][9][10][11][12][13][14][15][16][17][18][19]21,23,28 This study identified the abundance of STLs in the extract of T. diversifolia and examined their potential as a promising source of anti-trypanosomal leads.…”

“…20,21 Like many other plants in the Asteraceae family, its richness in sesquiterpene lactones (STLs) has continued to generate a prospect as well as diverse pharmacological activities, structure-activity relationships, and pharmacokinetics. [22][23][24] Studies have shown that through non-selective off-targets binding as a Michael acceptor, the interaction of the thiol (-SH) of proteins and enzymes with the nucleophilic alpha-methylenegamma-lactone of STLs could be responsible for their diverse activities. 22,24 This uniqueness compared with other secondary metabolites has continued to serve as the major focus for the progression and translation of STLs and their diverse pharmacological activities to clinical trials.…”

Semisynthesis of Novel Dispiro-pyrrolizidino/thiopyrrolizidino-oxindolo/indanedione Natural Product Hybrids of Parthenin Followed by Their Cytotoxicity Evaluation

“…hysterophorus) by using it as a rich source of chemicals such as parthenin, a sesquiterpene lactone. Parthenin shows medicinal properties such as antileishmanial, anticancer, microbicidal, anti-inflammatory, antiviral, and trypanocidal activities. − …”

“…Parthenin shows medicinal properties such as antileishmanial, anticancer, microbicidal, anti-inflammatory, antiviral, and trypanocidal activities. 36 − 38 …”