Pharmacokinetics of ferulic acid following oral administration ethyl ferulate alone and in combination with piperine in rats

The amyloid plaques are a key hallmark of neurodegenerative diseases such as Alzheimer’s disease and Parkinson’s disease. Amyloidogenesis is a complex long-lasting multiphase process starting with the formation of nuclei of amyloid peptides: a process assigned as a primary nucleation. Curcumin (CU) is a well-known inhibitor of the aggregation of amyloid-beta (Aβ) peptides. Even more, CU is able to disintegrate preformed Aβ firbils and amyloid plaques. Here, we simulate by molecular dynamics the primary nucleation process of 12 Aβ peptides and investigate the effects of CU on the process. We found that CU molecules intercalate among the Aβ chains and bind tightly to them by hydrogen bonds, hydrophobic, π–π, and cation–π interactions. In the presence of CU, the Aβ peptides form a primary nucleus of a bigger size. The peptide chains in the nucleus become less flexible and more disordered, and the number of non-native contacts and hydrogen bonds between them decreases. For comparison, the effects of the weaker Aβ inhibitor ferulic acid (FA) on the primary nucleation are also examined. Our study is in good agreement with the observation that taken regularly, CU is able to prevent or at least delay the onset of neurodegenerative disorders.

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“…The linker length is 12 Å. FA contains only one aromatic ring and is a weaker inhibitor of Aβ aggregation than CU. [72].…”

Section: Discussionmentioning

confidence: 99%

“… a Calculated by ACD/Labs (ACD/ChemSketch, version 2020.1.0); b PubChem [ 44 ]; c [ 31 ]; d [ 43 ]; e DrugBank [ 71 ]; f [ 68 ]; g [ 72 ]. …”

Section: Figurementioning

confidence: 99%

Curcumin Inhibits the Primary Nucleation of Amyloid-Beta Peptide: A Molecular Dynamics Study

et al. 2020

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Two Metallic Nanoparticles Formulas of Phyllostachys heterocycla Extract Exhibited Potent Cytotoxicity against Ovarian Cancer Cells through Apoptosis Induction

Abdelhameed,

Nafie,

Ibrahim

et al. 2024

J Clust Sci

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Phyllostachys heterocycla is well-known for its high diversity of bioactive metabolites, which are the reason for its various potential medical uses for which anticancer activity has been proven. Herein, Phyllostachys heterocycla extract was prepared in two different metallic nanoparticle formulas such as iron oxide nanoparticle-boron, and iron oxide nanoparticle-humic acid (Fe2O3 NP-B and Fe2O3 NP-HA) with average particle sizes of 12.25 nm and 15.80 nm, respectively. Phyllostachys heterocycla extract and the two nano-formulas were investigated to obtain their cytotoxic activity. The crude extract exhibited potent cytotoxic activity against the ovarian (OVCAR-3) cancer cell line, with IC50 values of 16.3 µg/mL. In comparison, the two nano-loaded forms displayed a much more promising cytotoxic activity with IC50 values of 0.9 µg/mL for Fe2O3 NP-HA, and 6.4 µg/mL for Fe2O3 NP-B. Additionally, NP-HA and NP-B showed potent cytotoxic activities against prostate (PC-3) and pancreatic (Panc1) cancer cell lines with IC50 values of 2.31, 6.3 µg/mL for Fe2O3 NP-HA, and 14.9, 16.8 µg/mL for Fe2O3 NP-B. For apoptosis investigation, Fe2O3 NP-HA induced total ovarian apoptotic cell death by a 87.34-fold change, and necrosis by 1.29-fold change. Regarding cell cycle analysis, Fe2O3 NP-HA-PHE arrested the cell proliferation of OVCAR-3 cells in S-phase, with an increased cell population at S-phase of 42.6%. Additionally, it confirmed the apoptosis mechanism by inhibiting the antiapoptotic gene and activating the proapoptotic gene markers. Moreover, upon continuation of our phytochemical investigation of the plant, additional chemical components of the crude extract of Phyllostachys heterocycla were isolated using various chromatographic techniques. As a result, six compounds were isolated. By using different spectroscopic data, the chemical structures of the pure isolated compounds were assigned as stigmasterol (1), glyceryl monobehenate (2), vanillic acid (3), ferulic acid (4), catechin (5), and thymidine (6). These isolated compounds were previously reported for their potent cytotoxic activities against panel of cancer cell lines including pancreatic cancer and prostate cancer cell lines (Ferulic acid), beside the anti-tumor potential against ovarian cell lines (Stigmasterol). In addition to the cytotoxic activity against human larynx carcinoma HepG-2 cell lines (Catechin), human breast cancer MCF7 (Thymidine), and human colon cancer cell line HT-29 (Vanillic acid). Which may explain the significant cytotoxic and anticancer properities of the crude extract of Phyllostachysheterocycla.

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Pharmacokinetics of ferulic acid following oral administration ethyl ferulate alone and in combination with piperine in rats

Cited by 2 publications

References 13 publications

Curcumin Inhibits the Primary Nucleation of Amyloid-Beta Peptide: A Molecular Dynamics Study

Curcumin Inhibits the Primary Nucleation of Amyloid-Beta Peptide: A Molecular Dynamics Study

Two Metallic Nanoparticles Formulas of Phyllostachys heterocycla Extract Exhibited Potent Cytotoxicity against Ovarian Cancer Cells through Apoptosis Induction

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