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Review
. 2023 Dec 29;13(1):70.
doi: 10.3390/cells13010070.

Gentiopicroside-An Insight into Its Pharmacological Significance and Future Perspectives

Lemonia Antoniadi  1 , Magdalena Bartnik  2 , Apostolis Angelis  1 , Anna Wawruszak  3 , Maria Halabalaki  1 , Wirginia Kukula-Koch  2 , Leandros A Skaltsounis  1
Affiliations
Review

Gentiopicroside-An Insight into Its Pharmacological Significance and Future Perspectives

Lemonia Antoniadi et al. Cells. .

Abstract

Gentiopicroside (GPS) is a leading component of several plant species from the Gentianaceae botanical family. As a compound with plenty of biological activities and a component of herbal drugs, GPS has an important role in the regulation of physiological processes in humans. The results of recently published scientific studies underline a meaningful role of this molecule as an active factor in metabolic pathways and mechanisms, which may have an influence in the treatment of different diseases, including digestive tract disorders, malignant changes, neurological disorders, microbial infections, bone formation disorders, inflammatory conditions, and others. This review aims to collect previously published reports on the biological properties of GPS as a single compound that were confirmed by in vitro and in vivo studies, and to draw attention to the newly discovered role of this bitter-tasting secoiridoid. Thanks to these properties, the research on this substance could be revisited.

Keywords: Gentiana; Gentianaceae; gentiopicroside; health benefits; in vitro; in vivo; molecular mechanism of bioactivity; pharmacological activity; semisynthetic derivatives of gentiopicroside.

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Conflict of interest statement

The authors declare no conflicts of interest.

Figures

Figure 1
Figure 1
Chemical structure of gentiopicroside.
Figure 2
Figure 2
Structures of two main metabolites of GPS: gentiopicral (A) and erythrocentaurin (B).
Figure 3
Figure 3
Biological properties of gentiopicroside.
Figure 4
Figure 4
The main targets for anti-inflammatory activity of GPS (COX-2—cyclooxygenase 2; IL-1β—interleukin 1β; IL-6—interleukin 6; IL-8—interleukin 8; iNOS—inducible nitric oxide synthase; GPS—gentiopicroside; TNF-α—tumor necrosis factor α; PGE2—prostaglandin E2; NO—nitric oxide).
Figure 5
Figure 5
The effects of GPS on the metabolism of glucose (EGFR1—epidermal growth factor receptor 1; FoxO1—Forkhead box O1; PI3K—phosphoinositide 3-kinase).
Figure 6
Figure 6
Mechanisms of the anti-cancer activity of GPS in various cancer cell lines.
Figure 7
Figure 7
Biological effects of GPS, proven in in vivo studies.
See this image and copyright information in PMC

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