Abstract

The peppers of the Capsicum species are exploited in many fields, as flavoring agents in food industry, or as decorative and therapeutic plants. Peppers show a diversified phytochemical content responsible for different biological activities. Synergic activity exerted by high levels of antioxidant compounds is responsible for their important anti-inflammatory property. A methanolic extract was obtained from a new pepper genotype and tested for anti-inflammatory activity. The extract was incorporated into phospholipid vesicles to increase the bioavailability of its bioactive components. Two types of phospholipid vesicles were produced, conventional liposomes and Penetration Enhancer containing Vesicles (PEVs). They were tested in human monoblastic leukemia U937 cell line, showing no cytotoxic effect. The intracellular reactive oxygen species (ROS) and nitric oxide (NO) levels were measured to value the in vitro efficacy of the vesicles in regulating inflammatory responses. Liposomal incorporation significantly reduced ROS levels in extract-treated LPS-activated cells. Furthermore, LC-MS/MS analyses demonstrated that liposomes facilitated the transport of the extract components across the cell membrane and their accumulation into the cytoplasm.

Highlights

  • Plants are an important source of chemical compounds mainly derived from their secondary metabolites with valuable properties to consumers [1].Peppers (Capsicum spp.) are among the oldest cultivated crops in warm climate regions worldwide and are a fundamental reservoir of bioactive compounds that contribute to the taste, color, and flavor of the fruits

  • In order to discriminate between the activity of the white Capsicum extract and the effect of the nanocarriers, WC-loaded liposomes and propylene glycol (PG)-Penetration Enhancer containing Vesicles (PEVs) were prepared, characterized, and compared with empty liposomes, empty PG-PEVs, and free WC extract

  • It is worth noting that an approximate 50-fold increase in capsaicin content was detected in cells treated with the higher WC concentration with respect to the lower concentration (25 vs. 5 μg/mL), which did not correspond to the only 5-fold more concentrated extract samples. This could be due to a matrix effect, which gave rise to a higher suppression of the capsaicin signal within the less concentrated sample (5 μg/mL) [55]. These results indicate that liposomes were more efficient than PG-PEVs in transporting the white Capsicum extract into the cells and promoting the accumulation of its components into the cytoplasm

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Summary

Introduction

Peppers (Capsicum spp.) are among the oldest cultivated crops in warm climate regions worldwide and are a fundamental reservoir of bioactive compounds that contribute to the taste, color, and flavor of the fruits. Antioxidants 2021, 10, 1683 conditions, the processing and storage practices [3,4]. Capsaicinoids are a group of alkaloids produced in variable amounts in hot peppers and their chemical structure influences the pungency of Capsicum species. They are probably produced as deterrents against certain herbivores and fungi, and major representatives are capsaicin and dihydrocapsaicin

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