Pterostilbene-isothiocyanate impedes RANK/TRAF6 interaction to inhibit osteoclastogenesis, promoting osteogenesis in vitro and alleviating glucocorticoid induced osteoporosis in rats

Kumar, Viney; Haldar, Swati; Ghosh, Souvik; Chauhan, Samrat; Sharma, Abhishek; Dhankhar, Poonam; Kumar, Amit; Jaiswal, Satish; Saini, Saakshi; Gupta, Somesh; Lahiri, Debrupa; Roy, Partha

doi:10.1016/j.bcp.2022.115284

Cited by 4 publications

(4 citation statements)

References 78 publications

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“…Molecular docking (MD) stands as a pivotal technique in structural molecular biology, a consensus affirmed by numerous citations in the literature [109][110][111][112][113][114]. In our study, MD was used to observe and confirm possible interactions between FIS and AChE/BChE.…”

Section: Bchementioning

confidence: 96%

Mechanochemical Approach to Obtaining a Multicomponent Fisetin Delivery System Improving Its Solubility and Biological Activity

Rosiak,

Tykarska,

Cielecka-Piontek

2024

IJMS

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In this study, binary amorphous solid dispersions (ASDs, fisetin-Eudragit®) and ternary amorphous solid inclusions (ASIs, fisetin-Eudragit®-HP-β-cyclodextrin) of fisetin (FIS) were prepared by the mechanochemical method without solvent. The amorphous nature of FIS in ASDs and ASIs was confirmed using XRPD (X-ray powder diffraction). DSC (Differential scanning calorimetry) confirmed full miscibility of multicomponent delivery systems. FT-IR (Fourier-transform infrared analysis) confirmed interactions that stabilize FIS’s amorphous state and identified the functional groups involved. The study culminated in evaluating the impact of amorphization on water solubility and conducting in vitro antioxidant assays: 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)—ABTS, 2,2-diphenyl-1-picrylhydrazyl—DPPH, Cupric Reducing Antioxidant Capacity—CUPRAC, and Ferric Reducing Antioxidant Power—FRAP and in vitro neuroprotective assays: inhibition of acetylcholinesterase—AChE and butyrylcholinesterase—BChE. In addition, molecular docking allowed for the determination of possible bonds and interactions between FIS and the mentioned above enzymes. The best preparation turned out to be ASI_30_EPO (ASD fisetin-Eudragit® containing 30% FIS in combination with HP-β-cyclodextrin), which showed an improvement in apparent solubility (126.5 ± 0.1 µg∙mL−1) and antioxidant properties (ABTS: IC50 = 10.25 µg∙mL−1, DPPH: IC50 = 27.69 µg∙mL−1, CUPRAC: IC0.5 = 9.52 µg∙mL−1, FRAP: IC0.5 = 8.56 µg∙mL−1) and neuroprotective properties (inhibition AChE: 39.91%, and BChE: 42.62%).

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Section: Bchementioning

confidence: 96%

Mechanochemical Approach to Obtaining a Multicomponent Fisetin Delivery System Improving Its Solubility and Biological Activity

Rosiak,

Tykarska,

Cielecka-Piontek

2024

IJMS

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“…PTR’s antioxidant capabilities have been associated with its role in preventing cancer, influencing neurological conditions, reducing inflammation, mitigating vascular diseases, and improving diabetes outcomes [ 2 , 21 , 39 ]. Moreover, the in silico study of PTR activity has been of interest in various biomedical applications [ 40 , 41 , 42 , 43 , 44 , 45 ]. PTR has been investigated for, among other reasons, (i) the binding mode with the Keap1 Kelch domain [ 41 ], (ii) a telomerase inhibitor [ 43 ], and (iii) to confirm whether PTR binds to the MMP-9 proteins [ 42 ].…”

Section: Introductionmentioning

confidence: 99%

Enhanced Antioxidant and Neuroprotective Properties of Pterostilbene (Resveratrol Derivative) in Amorphous Solid Dispersions

Rosiak,

Tykarska,

Cielecka-Piontek

2024

IJMS

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In this study, amorphous solid dispersions (ASDs) of pterostilbene (PTR) with polyvinylpyrrolidone polymers (PVP K30 and VA64) were prepared through milling, affirming the amorphous dispersion of PTR via X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). Subsequent analysis of DSC thermograms, augmented using mathematical equations such as the Gordon–Taylor and Couchman–Karasz equations, facilitated the determination of predicted values for glass transition (Tg), PTR’s miscibility with PVP, and the strength of PTR’s interaction with the polymers. Fourier-transform infrared (FTIR) analysis validated interactions maintaining PTR’s amorphous state and identified involved functional groups, namely, the 4′–OH and/or –CH groups of PTR and the C=O group of PVP. The study culminated in evaluating the impact of amorphization on water solubility, the release profile in pH 6.8, and in vitro permeability (PAMPA-GIT and BBB methods). In addition, it was determined how improving water solubility affects the increase in antioxidant (ABTS, DPPH, CUPRAC, and FRAP assays) and neuroprotective (inhibition of cholinesterases: AChE and BChE) properties. The apparent solubility of the pure PTR was ~4.0 µg·mL−1 and showed no activity in the considered assays. For obtained ASDs (PTR-PVP30/PTR-PVPVA64, respectively) improvements in apparent solubility (410.8 and 383.2 µg·mL−1), release profile, permeability, antioxidant properties (ABTS: IC50 = 52.37/52.99 μg·mL−1, DPPH: IC50 = 163.43/173.96 μg·mL−1, CUPRAC: IC0.5 = 122.27/129.59 μg·mL−1, FRAP: IC0.5 = 95.69/98.57 μg·mL−1), and neuroprotective effects (AChE: 39.1%/36.2%, BChE: 76.9%/73.2%) were confirmed.

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“…25 Recently, the effect of PT on bone homeostasis has been reported, demonstrating that pterostilbene-isothiocyanate suppresses osteoclastogenesis and promotes osteogenesis to ameliorate osteoporosis. 26 In addition, PT has been found to inhibit ROS generation and inflammation, exerting an antiarthritic effect on rheumatoid arthritis (RA). 27 Based on these findings, PT could be a potential strategy for the prevention and therapy of OA.…”

Section: ■ Introductionmentioning

confidence: 99%

“…Furthermore, PT has been reported to improve nonalcoholic fatty liver disease (NAFLD) by reducing lipid accumulation and inflammation . Recently, the effect of PT on bone homeostasis has been reported, demonstrating that pterostilbene-isothiocyanate suppresses osteoclastogenesis and promotes osteogenesis to ameliorate osteoporosis . In addition, PT has been found to inhibit ROS generation and inflammation, exerting an antiarthritic effect on rheumatoid arthritis (RA) .…”

Section: Introductionmentioning

confidence: 99%

Pterostilbene Protects against Osteoarthritis through NLRP3 Inflammasome Inactivation and Improves Gut Microbiota as Evidenced by In Vivo and In Vitro Studies

Lee,

Chang,

Cheng

et al. 2024

J. Agric. Food Chem.

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Osteoarthritis (OA) is a persistent inflammatory disease, and long-term clinical treatment often leads to side effects. In this study, we evaluated pterostilbene (PT), a natural anti-inflammatory substance, for its protective effects and safety during prolonged use on OA. Results showed that PT alleviated the loss of chondrocytes and widened the narrow joint space in an octacalcium phosphate (OCP)-induced OA mouse model (n = 3). In vitro experiments demonstrate that PT reduced NLRP3 inflammation activation (relative protein expression: C: 1 ± 0.09, lipopolysaccharide (LPS): 1.14 ± 0.07, PT: 0.91 ± 0.07, LPS + PT: 0.68 ± 0.04) and the release of inflammatory cytokines through NF-κB signaling inactivation (relative protein expression: C: 1 ± 0.03, LPS: 3.49 ± 0.02, PT: 0.66 ± 0.08, LPS + PT: 2.78 ± 0.05), ultimately preventing cartilage catabolism. Interestingly, PT also altered gut microbiota by reducing inflammation-associated flora and increasing the abundance of healthy bacteria in OA groups. Collectively, these results suggest that the PT can be considered as a protective strategy for OA.

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Pterostilbene-isothiocyanate impedes RANK/TRAF6 interaction to inhibit osteoclastogenesis, promoting osteogenesis in vitro and alleviating glucocorticoid induced osteoporosis in rats

Cited by 4 publications

References 78 publications

Mechanochemical Approach to Obtaining a Multicomponent Fisetin Delivery System Improving Its Solubility and Biological Activity

Mechanochemical Approach to Obtaining a Multicomponent Fisetin Delivery System Improving Its Solubility and Biological Activity

Enhanced Antioxidant and Neuroprotective Properties of Pterostilbene (Resveratrol Derivative) in Amorphous Solid Dispersions

Pterostilbene Protects against Osteoarthritis through NLRP3 Inflammasome Inactivation and Improves Gut Microbiota as Evidenced by In Vivo and In Vitro Studies

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