Bioactivities and the structural modification of Parthenolide: a review

Wu, Jie; Wang, Xiaoqian; Hou, Yunlei; Gong, Ping

doi:10.1007/s00044-023-03181-0

Cited by 3 publications

(1 citation statement)

References 76 publications

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“…In contrast, the nature of the molecular target (s) of parthenolide and related sesquiterpene lactones is less clear; in fact, parthenolide has been described as having a “ …promiscuous bioactivity profile… ” [40]. Most studies on the molecular effects of parthenolide and related compounds focus on their impact on IkB kinases and nuclear factor kappa-B (NF-κB) and several classes of cytokines downstream of it, which may account for parthenolide’s antitumoral and anti-inflammatory properties [68,69]. Additionally, parthenolide interferes with microtubule physiology [70,71] and, intriguingly, has been proposed as an agent that promotes functional nervous tissue regeneration [72], in contrast to results obtained from our laboratory (in preparation).…”

Section: Discussionmentioning

confidence: 99%

Schild analysis of the interaction between parthenolide and cocaine suggests an allosteric relationship for their effects on planarian motility

Kakuturu

O'Brien

Pagán

2022

Preprint

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One of the best-characterized planarian behaviors induced by various compounds is the change in locomotor velocity. Previous work from our laboratory showed that the sesquiterpene lactone parthenolide and the local anesthetic cocaine, reduce planarian motility. Parthenolide reverses the cocaine-induced motility decrease and vice versa. However, the exact mechanism of the cocaine/parthenolide antagonism for this specific planarian behavior is still unknown. Here we report the results of a Schild analysis to determine whether the parthenolide/cocaine relationship is orthosteric or allosteric. Our results suggest an orthosteric relationship between these two compounds in the planarian Girardia tigrina. The simplest interpretation of our data is a shared binding site for cocaine and parthenolide. Still, we cannot rule out the possibility of distinct yet overlapping binding sites with the data available.

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Section: Discussionmentioning

confidence: 99%

Schild analysis of the interaction between parthenolide and cocaine suggests an allosteric relationship for their effects on planarian motility

Kakuturu

O'Brien

Pagán

2022

Preprint

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Schild Analysis of the Interaction between Parthenolide and Cocaine Suggests an Allosteric Relationship for Their Effects on Planarian Motility

Kakuturu,

O’Brien,

Pagán

2024

Biomolecules

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The freshwater planarian is an emerging animal model in neuroscience due to its centralized nervous system that closely parallels closely parallels the nervous system of vertebrates. Cocaine, an abused drug, is the ‘founding member’ of the local anesthetic family. Parthenolide, a sesquiterpene lactone, acts as a behavioral and physiological antagonist of cocaine in planarians and rats, respectively. Previous work from our laboratory showed that both parthenolide and cocaine reduced planarian motility and that parthenolide reversed the cocaine-induced motility decrease at concentrations where parthenolide does not affect the movement of the worms. However, the exact mechanism of the cocaine/parthenolide antagonism is unknown. Here, we report the results of a Schild analysis to explore the parthenolide/cocaine relationship in the planarian Girardia tigrina. The Schild slopes of a family of concentration–response curves of parthenolide ± a single concentration of cocaine and vice versa were −0.55 and −0.36, respectively. These slopes were not statistically different from each other. Interestingly, the slope corresponding to the parthenolide ± cocaine (but not the cocaine ± parthenolide) data set was statistically different from −1. Our data suggest an allosteric relationship between cocaine and parthenolide for their effect on planarian motility. To the best of our knowledge, this is the first study about the mechanism of action of the antagonism between cocaine and parthenolide. Further studies are needed to determine the specific nature of the parthenolide/cocaine target(s) in this organism.

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Insights into Tissue-Specific Specialized Metabolism in Wampee (Clausena lansium (Lour.) Skeels) Varieties

Zhang,

Zhou,

Zhang

et al. 2024

Foods

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Wampee (Clausena lansium (Lour.) Skeels) has natural bioactive components with diverse health benefits, but its detailed metabolism and tissue distribution are not fully understood. Here, widely targeted metabolomics analysis methods were employed to analyze the wampee fruit (peel, pulp, and seed) of 17 different varieties. A total of 1286 metabolites were annotated, including lipids, flavonoids, polyphenols, carbazole alkaloids, coumarins, and organic acids, among others. The quantitative analysis and matrix-assisted laser desorption/ionization–mass spectrometry imaging (MALDI-MSI) analysis indicated remarkable variations in metabolite categories and content in the peel, pulp, and seed of wampee fruit. Additionally, the difference analysis found that the metabolic components of peel contributed dominantly to the differences among varieties, and 7 potential biomarkers were identified. In this study, a comprehensive metabolome landscape of wampee fruit was established, which provided important information for the isolation and identification of functional components, food industry application, and nutritional improvement breeding.

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Bioactivities and the structural modification of Parthenolide: a review

Cited by 3 publications

References 76 publications

Schild analysis of the interaction between parthenolide and cocaine suggests an allosteric relationship for their effects on planarian motility

Schild analysis of the interaction between parthenolide and cocaine suggests an allosteric relationship for their effects on planarian motility

Schild Analysis of the Interaction between Parthenolide and Cocaine Suggests an Allosteric Relationship for Their Effects on Planarian Motility

Insights into Tissue-Specific Specialized Metabolism in Wampee (Clausena lansium (Lour.) Skeels) Varieties

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