Molecular and pharmacological aspects of piperine as a potential molecule for disease prevention and management: evidence from clinical trials

Tripathi, Amit Kumar; Ray, Anup Kumar; Mishra, Sunil Kumar

doi:10.1186/s43088-022-00196-1

Cited by 76 publications

(45 citation statements)

References 187 publications

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“…In addition, PPN is considered to be the first and most potent natural bioenhancer [ 8 ]. PPN has significant potential to inhibit CYP3A4 (a metabolizing enzyme) and P-glycoprotein (P-gp; an efflux transporter) [ 9 , 10 ]. P-gp is basically an efflux transporter that effluxes several drugs out of the cells after absorption from the intestine [ 11 ].…”

Section: Introductionmentioning

confidence: 99%

Formulation of Piperine Nanoparticles: In Vitro Breast Cancer Cell Line and In Vivo Evaluation

et al. 2022

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Piperine (PPN), one of the most investigated phytochemicals, is known to have excellent therapeutic efficacy against a variety of ailments including breast cancer. However, its physicochemical properties such as poor aqueous solubility restrict its clinical application. Therefore, the present investigation was designed to develop PPN encapsulated lipid polymer hybrid nanoparticles (PPN-LPHNPs) to overcome the limitation. The developed PPN-LPHNPs were optimized by the three-factor, three-level Box–Behnken design (33-BBD). The optimized PPN-LPHNPs were then evaluated for their drug release profile, cytotoxicity assay against MDA-MB-231 and MCF-7 cells, and gastrointestinal stability as well as colloidal stability. In addition, the optimized PPN-LPHNPs were evaluated for ex vivo intestinal permeation and in vivo pharmacokinetic in albino Wistar rats. As per the results, the optimized PPN-LPHNPs showed a small average particles size of <160 nm with a low (<0.3) polydispersity index, and highly positive surface charge (>+20 mV). PPN-LPHNPs revealed excellent gastrointestinal as well as colloidal stability and sustained release profiles up to 24 h. Furthermore, PPN-LPHNPs revealed excellent cytotoxicity against both MDA-MB-231 and MCF-7 cancer cells compared to the free PPN. Moreover, animal studies revealed that the PPN-LPHNPs exhibited a 6.02- and 4.55-fold higher intestinal permeation and relative oral bioavailability, respectively, in comparison to the conventional PPN suspension. Thus, our developed LPHNPs present a strong potential for improved delivery of PPN.

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Section: Introductionmentioning

confidence: 99%

Formulation of Piperine Nanoparticles: In Vitro Breast Cancer Cell Line and In Vivo Evaluation

et al. 2022

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“…This structural feature leads to characteristic ultraviolet (UV) absorptions [ 20 ]. A review reported in the literature this year (2022) gathered a set of studies of important targets that interact (experimental and computational results) with piperine [ 21 ]. This set of proteins is composed by inflammatory cytokines (IL-8, IL-10, IL-1 h, IL-6), transcriptional factors (AP-1, NF-κB, ATF-2), kinases (JNK, ERK1, ERK2, Akt, P38 MAPK), enzymes (NOS-2, COX-2, MMP-2, MMP-9), transporter genes (CYP3A4, RV1258c, MRP1, BCRP), and cell-cycle proteins (cyclin A/D/T, CDK-2, CDK-4), among others.…”

Section: Introductionmentioning

confidence: 99%

A Computational–Experimental Investigation of the Molecular Mechanism of Interleukin-6-Piperine Interaction

Povinelli

Zazeri

Jones

et al. 2022

IJMS

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Herein, we elucidate the biophysical aspects of the interaction of an important protein, Interleukin-6 (IL6), which is involved in cytokine storm syndrome, with a natural product with anti-inflammatory activity, piperine. Despite the role of piperine in the inhibition of the transcriptional protein NF-κB pathway responsible for activation of IL6 gene expression, there are no studies to the best of our knowledge regarding the characterisation of the molecular interaction of the IL6-piperine complex. In this context, the characterisation was performed with spectroscopic experiments aided by molecular modelling. Fluorescence spectroscopy alongside van’t Hoff analyses showed that the complexation event is a spontaneous process driven by non-specific interactions. Circular dichroism aided by molecular dynamics revealed that piperine caused local α-helix reduction. Molecular docking and molecular dynamics disclosed the microenvironment of interaction as non-polar amino acid residues. Although piperine has three available hydrogen bond acceptors, only one hydrogen-bond was formed during our simulation experiments, reinforcing the major role of non-specific interactions that we observed experimentally. Root mean square deviation (RMSD) and hydrodynamic radii revealed that the IL6-piperine complex was stable during 800 ns of simulation. Taken together, these results can support ongoing IL6 drug discovery efforts.

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“…The pharmacological significance of the metabolites present in DSV, particularly their anti-inflammatory properties, are well documented ( Semaming et al, 2015 ; Semwal et al, 2015 ; Correa et al, 2016 ; Graebin, 2018 ; Rios et al, 2018 ; Kahkeshani et al, 2019 ; Ruwizhi and Aderibigbe, 2020 ; Li C.-X. et al, 2021 ; Nisar et al, 2021 ; Sharifi-Rad et al, 2021 ; Tripathi et al, 2022 ). Recently, DSV has also been reported to ameliorate S protein-induced inflammatory response in A549 xenotransplanted zebrafish by reducing IL-6 and TNF-α, pro-inflammatory cytokine levels and rescuing fever-driven swimming behavioural patterns ( Balkrishna et al, 2020c ).…”

Section: Introductionmentioning

confidence: 99%

Herbo-mineral formulation, Divya-Swasari-Vati averts SARS-CoV-2 pseudovirus entry into human alveolar epithelial cells by interfering with spike protein-ACE 2 interaction and IL-6/TNF-α /NF-κB signaling

et al. 2022

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The herbo-mineral formulation, Divya-Swasari-Vati (DSV), is a well-known Ayurvedic medication for respiratory ailments. In a recent pre-clinical study, DSV rescued humanized zebrafish from SARS-CoV-2 S-protein-induced pathologies. This merited for an independent evaluation of DSV as a SARS-CoV-2 entry inhibitor in the human host cell and its effectiveness in ameliorating associated cytokine production. The ELISA-based protein-protein interaction study showed that DSV inhibited the interactions of recombinant human ACE 2 with three different variants of S proteins, namely, Smut 1 (the first reported variant), Smut 2 (W436R variant) and Smut 3 (D614G variant). Entry of recombinant vesicular stomatitis SARS-CoV-2 (VSVppSARS-2S) pseudovirus, having firefly luciferase and EGFP reporters, was assessed through luciferase assay and fluorescent microscopy. DSV exhibited dose-dependent inhibition of VSVppSARS-2S pseudovirus entry into human lung epithelial A549 cells and also suppressed elevated levels of secreted pro-inflammatory cytokines such as interleukin-6 (IL-6), interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α) induced by viral infection mimicking Poly I:C-, S-protein- and VSVppSARS-2S pseudovirus. In human immune cells, DSV also moderated TNF-α-mediated NF-κB induction, in a dose-dependent manner. The observed anti-viral effect of DSV against SARS-CoV-2 is attributable to the presence of different metabolites Summarily, the observations from this study biochemically demonstrated that DSV interfered with the interaction between SARS-CoV-2 S-protein and human ACE 2 receptor which consequently, inhibited viral entry into the host cells and concomitant induction of inflammatory response.

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Molecular and pharmacological aspects of piperine as a potential molecule for disease prevention and management: evidence from clinical trials

Cited by 76 publications

References 187 publications

Formulation of Piperine Nanoparticles: In Vitro Breast Cancer Cell Line and In Vivo Evaluation

Formulation of Piperine Nanoparticles: In Vitro Breast Cancer Cell Line and In Vivo Evaluation

A Computational–Experimental Investigation of the Molecular Mechanism of Interleukin-6-Piperine Interaction

Herbo-mineral formulation, Divya-Swasari-Vati averts SARS-CoV-2 pseudovirus entry into human alveolar epithelial cells by interfering with spike protein-ACE 2 interaction and IL-6/TNF-α /NF-κB signaling

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