Insights into the Structure-Activity Relationship of Glycosides as Positive Allosteric Modulators Acting on P2X7 Receptors

Piyasirananda, Waraporn; Beekman, Andrew M.; Ganesan, A.; Bidula, Stefan; Stokes, Leanne

doi:10.1124/molpharm.120.000129

Cited by 9 publications

(3 citation statements)

References 38 publications

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“…1A shows the formulation processes for the preparation of Rg3/Lipo using ginsenoside Rg3(S) and SL via thin-film casting and hydration processes. Previous studies have reported that the stereoselectivity of the hydroxyl group on C-20 of ginsenoside Rg3 resulted in two types of Rg3 stereoisomers, Rg3(S) and Rg3(R), which are crucial for biological activity [ 16 - 18 ]. In particular, Rg3(S) showed a more promising reduction in ROS by UV radiation in human keratinocytes and fibroblasts than Rg3(R) [ 17 ].…”

Section: Resultsmentioning

confidence: 99%

Protection of Skin Fibroblasts from Infrared-A-Induced Photo-Damage Using Ginsenoside Rg3(S)-Incorporated Soybean Lecithin Liposomes

Jung

Song

You

et al. 2022

J. Microbiol. Biotechnol.

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Protection of skin cells from chronic infrared-A (IRA) irradiation is crucial for anti-photoaging of the skin. In this study, we investigated the protective activity of Rg3(S) and Rg3(S)-incorporated anionic soybean lecithin liposomes (Rg3/Lipo) with a size of approximately 150 nm against IRA-induced photodamage in human fibroblasts. The formulated Rg3/Lipo showed increased solubility in aqueous solution up to a concentration of 200 μg/ml, compared to free Rg3(S). In addition, Rg3/Lipo exhibited superior colloidal stability in aqueous solutions and biocompatibility for normal human dermal fibroblasts (NHDFs). After repeated IRA irradiation on NHDFs, elevated levels of cellular and mitochondrial reactive oxygen species (ROS) were greatly reduced by Rg3(S) and Rg3/Lipo. In addition, cells treated with Rg3/Lipo exhibited noticeably reduced apoptotic signals following IRA irradiation compared to untreated cells. Thus, considering aqueous solubility and cellular responses, Rg3/Lipo could serve as a promising infrared protector for healthy aging of skin cells.

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Section: Resultsmentioning

confidence: 99%

Protection of Skin Fibroblasts from Infrared-A-Induced Photo-Damage Using Ginsenoside Rg3(S)-Incorporated Soybean Lecithin Liposomes

Jung

Song

You

et al. 2022

J. Microbiol. Biotechnol.

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“…Certain single nucleotide polymorphisms have been shown to influence infection outcomes [23]. We recently showed that ginsenosides could potentiate ATP-mediated responses in the THP-1 human monocyte cell line which is known to carry the 1513A > C (rs3751143) polymorphism [24]. Therefore, we suggest that more work should be performed to determine whether boosting P2X7 responses in infection models is a useful therapeutic angle.…”

Section: Discussionmentioning

confidence: 97%

Ginsenosides enhance P2X7-dependent cytokine secretion from LPS-primed rodent macrophages

Dhuna

Helliwell

Luca

et al. 2023

Purinergic Signalling

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The activation of P2X7 is a well-known stimulus for the NLRP3-caspase 1 inflammasome and subsequent rapid IL-1β secretion from monocytes and macrophages. Here we show that positive allosteric modulators of P2X7, ginsenosides, can enhance the release of three important cytokines, IL-1β, IL-6 and TNF-α from LPS-primed rodent macrophages using the J774 mouse macrophage cell line and primary rat peritoneal macrophages. We compared the immediate P2X7 responses in un-primed and LPS-primed macrophages and found no difference in calcium response amplitude or kinetics. These results suggest that under inflammatory conditions positive allosteric modulators are capable of increasing cytokine secretion at lower concentrations of ATP, thus boosting the initial pro-inflammatory signal. This may be important in the control of intracellular infections.

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“…are rare in ginseng species ( Zhang H. et al, 2022 ). The experimental pharmacological research of ginsenosides have shown that the number of sugar residues contained in the branched, the position of glycosides, and their stereoselectivity all affect the pharmacological activity of ginsenoside monomers ( Piyasirananda et al, 2021 ; Yousof Ali et al, 2021 ; Ali et al, 2022 ). Oral administration of ginsenosides is the major approach, but they are not easily absorbed by themselves with low bioavailability ( Won et al, 2019 ).…”

Section: Introductionmentioning

confidence: 99%

Ginsenosides on stem cells fate specification—a novel perspective

Liu

Jiang

Song

et al. 2023

Front. Cell Dev. Biol.

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Recent studies have demonstrated that stem cells have attracted much attention due to their special abilities of proliferation, differentiation and self-renewal, and are of great significance in regenerative medicine and anti-aging research. Hence, finding natural medicines that intervene the fate specification of stem cells has become a priority. Ginsenosides, the key components of natural botanical ginseng, have been extensively studied for versatile effects, such as regulating stem cells function and resisting aging. This review aims to summarize recent progression regarding the impact of ginsenosides on the behavior of adult stem cells, particularly from the perspective of proliferation, differentiation and self-renewal.

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Insights into the Structure-Activity Relationship of Glycosides as Positive Allosteric Modulators Acting on P2X7 Receptors

Cited by 9 publications

References 38 publications

Protection of Skin Fibroblasts from Infrared-A-Induced Photo-Damage Using Ginsenoside Rg3(S)-Incorporated Soybean Lecithin Liposomes

Protection of Skin Fibroblasts from Infrared-A-Induced Photo-Damage Using Ginsenoside Rg3(S)-Incorporated Soybean Lecithin Liposomes

Ginsenosides enhance P2X7-dependent cytokine secretion from LPS-primed rodent macrophages

Ginsenosides on stem cells fate specification—a novel perspective

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