Piperine: Chemical, biological and nanotechnological applications

Abstract

Piperine (PIP) is an alkaloid present in several species of piper, mainly Piper nigrum Linn. and P. longum, among other species. The present article provides a comprehensive review of PIP research in the last years concerning its chemical properties, synthesis, absorption, metabolism, bioavailability and toxicity. The reviewed PIP literature has shown many pharmacological properties, such as antidiabetic, antidiarrheal, antioxidant, antibacterial, and anti-parasitic activity of PIP. However, its low solubility and absorption make its application challenging. This review also includes advances in the development of nanosystems containing PIP, including liposomes, micelles, metal nanoparticles, nanofibers, polymeric nanoparticles, and solid-lipid nanoparticles. Finally, we discuss different in vitro and in vivo studies to evaluate the biological activity of this drug, as well as some methods for the synthesis of nanosystems and their physical characteristics.

Piperine-Loaded Chitosan Nanoparticles: Preparation and Characterization

“…PIP has many pharmacological properties, such as antidiabetic, antidiarrheal, antioxidant, antibacterial, and antiparasitic activity [5]. It also reduces cholesterol uptake and enhances translocation of cholesterol transporter proteins, as reported by Christian Rafael Quizia et al [5]. PIP-loaded NPs showed a more significant inhibitory effect on seizure-related behavioral signs compared to the free PIP [6].…”

“…and P. longum. PIP has many pharmacological properties, such as antidiabetic, antidiarrheal, antioxidant, antibacterial, and antiparasitic activity [5]. It also reduces cholesterol uptake and enhances translocation of cholesterol transporter proteins, as reported by Christian Rafael Quizia et al [5].…”

“…Hypertension and hypercholesterolemia are the main factors of morbidity and mortality in today's society since they are two key risk factors for the emergence and development of cardiovascular diseases. Both CTS and PIP could reduce cholesterol uptake and enhance translocation of cholesterol transporter proteins [2,3,5]. The preparation of NPs intended to be used as functional food to support for the treatment of hypercholesterolemia rarely been reported before.…”

Recent Strategies for Improving Solubility and Oral Bioavailability of Piperine

“…Other traditional medicine systems, such as TCM, use black pepper to treat various pains (e. g. muscle aches and headaches), rheumatism, and infections such as strep throat and influenza, as well as to improve blood circulation [3]. Based on its utilisation in traditional medicine, extensive in vitro and in vivo studies regarding the bioactivity of piperine have been conducted and reported: a very wide range of bioactivity, including anti-inflammatory, antimicrobial, anticancer, anti-diabetic, anti-obesity, antihyperlipidemia, anticonvulsant, antidepressant, antiepileptic, neuroprotective, and hepatoprotective [1,2,4,5]. Recent studies on piperine by in silico method showed that piperine has antiviral activity against the SARS-CoV-2 virus that caused COVID-19, through inhibition of virus replication and the ACE-2 receptor [6,7].…”

In Vitro Phenotypic Activity and In Silico Analysis of Natural Products from Brazilian Biodiversity on Trypanosoma cruzi

“…fasciculata (Solanaceae) have promising activity against Leishmania amazonensis [ 11 ]; (ii) extracts from leaves and stem bark of Crescentia cujete (Binoniacea) have anti-inflammatory and antibacterial in vitro activities; possibly related to tannins, flavonoids, flavones and flavonols [ 12 ]; (iii) extracts from Clusia (Clusiaceae) species and Malpighia glabra (Malpighiaceae) rich in carotenoids and flavonoids present potent antioxidant activity [ 13 , 14 , 15 ]; and (iv) aqueous extract pf Rheedia longifolia (Clusiaceae) leaves has analgesic and anti-inflammatory in vivo activities and low toxicity [ 16 ]. Additionally, natural products from Piper species (Piperaceae) display broad biological roles [ 17 , 18 , 19 , 20 , 21 ], including antiprotozoal effects [ 22 ]. Additionally, a chalcone isolated from inflorescences of P. aduncum [ 23 ] and an essential oil and the ethanolic extract from leaves of P. marginatum [ 24 ] also present promising in vitro effect against L. amazonensis .…”