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Liposome-mediated inhibition of inflammation by hydroxycitrate

Title: Liposome-mediated inhibition of inflammation by hydroxycitrate
Authors: Vassallo A.; Santoro V.; Pappalardo I.; Santarsiero A.; Convertini P.; De Luca M.; Martelli G.; Infantino V.; Caddeo C.
Contributors: Vassallo, A.; Santoro, V.; Pappalardo, I.; Santarsiero, A.; Convertini, P.; De Luca, M.; Martelli, G.; Infantino, V.; Caddeo, C.
Publication Year: 2020
Collection: Università degli Studi di Cagliari: UNICA IRIS
Subject Terms: Hydroxycitrate; Liposome; Macrophage; Inflammation; Antioxidant
Description: Hydroxycitrate (HCA), a main organic acid component of the fruit rind of Garcinia cambogia, is a natural citrate analog that can inhibit the ATP citrate lyase (ACLY) enzyme with a consequent reduction of inflammatory mediators (i.e., nitric oxide (NO), reactive oxygen species (ROS), and prostaglandin E2 (PGE2)) levels. Therefore, HCA has been proposed as a novel means to prevent, treat, and ameliorate conditions involving inflammation. However, HCA presents a low membrane permeability, and a large quantity is required to have a biological effect. To overcome this problem, HCA was formulated in liposomes in this work, and the enhancement of HCA cell availability along with the reduction in the amount required to downregulate NO, ROS, and PGE2 in macrophages were assessed. The liposomes were small in size (~60 nm), monodispersed, negatively charged (−50 mV), and stable on storage. The in vitro results showed that the liposomal encapsulation increased by approximately 4 times the intracellular accumulation of HCA in macrophages, and reduced by 10 times the amount of HCA required to abolish LPS-induced NO, ROS, and PGE2 increase. This suggests that liposomal HCA can be exploited to target the citrate pathway involved in inflammatory processes.
Document Type: article in journal/newspaper
Language: English
Relation: info:eu-repo/semantics/altIdentifier/pmid/33096779; info:eu-repo/semantics/altIdentifier/wos/WOS:000585221000001; volume:10; issue:10; firstpage:1; lastpage:9; numberofpages:9; journal:NANOMATERIALS; https://hdl.handle.net/11584/299844
DOI: 10.3390/nano10102080
Availability: https://hdl.handle.net/11584/299844; https://doi.org/10.3390/nano10102080; https://www.mdpi.com/2079-4991/10/10/2080
Rights: info:eu-repo/semantics/openAccess
Accession Number: edsbas.9C0923F3
Database: BASE