Abstract
Piperine (PIP) is an active alkaloid of black and long peppers. An increasing amount of evidence is suggesting that PIP and its metabolite’s could be a potential therapeutic to intervene different disease conditions including chronic inflammation, cardiac and hepatic diseases, neurodegenerative diseases, and cancer. In addition, the omnipresence of PIP in food and beverages made this compound an important investigational material. It has now become essential to understand PIP pharmacology and toxicology to determine its merits and demerits, especially its effect on the central nervous system (CNS). Although several earlier reports documented that PIP has poor pharmacokinetic properties, such as absorption, bioavailability, and blood–brain barrier permeability. However, its interaction with metabolic enzyme cytochrome P450 superfamily and competitive hydrophobic interaction at Monoamine oxide B (MAO-B) active site have made PIP both a xenobiotics bioenhancer and a potential MAO-B inhibitor. Moreover, recent advancements in pharmaceutical technology have overcome several of PIP’s limitations, including bioavailability and blood–brain barrier permeability, even at low doses. Contrarily, the structure activity relationship (SAR) study of PIP suggesting that its several metabolites are reactive and plausibly responsible for acute toxicity or have pharmacological potentiality. Considering the importance of PIP and its metabolites as an emerging drug target, this study aims to combine the current knowledge of PIP pharmacology and biochemistry with neurodegenerative and neurological disease therapy.
Highlights
Piperine (PIP), an alkaloid, omnipresent in foods/beverages, is currently one of the compounds of interest for showing numerous pharmacological benefits
Earlier studies re-ported that PIP has poor bioavailability [2] owing to its lipophilic nature, it can inhibit metabolic enzymes like CYP3A4 and drug transporter P-glycoprotein and modulate xenobiotics metabolism in human liver [3]
Carbamazepine, a widely used anti-epileptic drug, has a very narrow therapeutic index, because carbamazepine is primarily metabolized by CYP3A4 and that yields carbamazepine-10,11-epoxide (CBZE) intermediate [4]
Summary
Piperine (PIP), an alkaloid, omnipresent in foods/beverages, is currently one of the compounds of interest for showing numerous pharmacological benefits. Co-treatment patients, enhancing the therapeutic window for carbamazepine in patients who rewith PIP has increased the carbamazepine area under the curve (AUC) and half-life in quire long-term therapy [6,7,8]. Several studies recently developed a PIPepileptic patients, enhancing the therapeutic window for carbamazepine in patients loaded nano-formulation, microemulsion, and intranasal delivery system to overcome who require long-term therapy [6,7,8]. PIP treatment showed reduced depressive-like [9]poor and loaded nano-formulation, microemulsion, and intranasal delivery system to overcome. The bioavailability enhancing property and the other pharmacological (AD) model [11], and halted neuronal cell death in a Parkinson’s (PD) model [12].activiAltoties of PIP, and its metabolites have made them a hot in recent research.
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