Liposome-Mediated Inhibition of Inflammation by Hydroxycitrate
Hydroxycitrate (HCA), a main organic acid component of the fruit rind of <i>Garcinia cambogia</i>, 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...
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-10-01
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| Series: | Nanomaterials |
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| Online Access: | https://www.mdpi.com/2079-4991/10/10/2080 |
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| author | Antonio Vassallo Valentina Santoro Ilaria Pappalardo Anna Santarsiero Paolo Convertini Maria De Luca Giuseppe Martelli Vittoria Infantino Carla Caddeo |
| author_facet | Antonio Vassallo Valentina Santoro Ilaria Pappalardo Anna Santarsiero Paolo Convertini Maria De Luca Giuseppe Martelli Vittoria Infantino Carla Caddeo |
| author_sort | Antonio Vassallo |
| collection | DOAJ |
| description | Hydroxycitrate (HCA), a main organic acid component of the fruit rind of <i>Garcinia cambogia</i>, 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 E<sub>2</sub> (PGE<sub>2</sub>)) 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 PGE<sub>2</sub> 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 PGE<sub>2</sub> increase. This suggests that liposomal HCA can be exploited to target the citrate pathway involved in inflammatory processes. |
| first_indexed | 2024-03-10T15:27:03Z |
| format | Article |
| id | doaj.art-e0bf93539c464d2a82143a327394f93a |
| institution | Directory Open Access Journal |
| issn | 2079-4991 |
| language | English |
| last_indexed | 2024-03-10T15:27:03Z |
| publishDate | 2020-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Nanomaterials |
| spelling | doaj.art-e0bf93539c464d2a82143a327394f93a2023-11-20T17:58:02ZengMDPI AGNanomaterials2079-49912020-10-011010208010.3390/nano10102080Liposome-Mediated Inhibition of Inflammation by HydroxycitrateAntonio Vassallo0Valentina Santoro1Ilaria Pappalardo2Anna Santarsiero3Paolo Convertini4Maria De Luca5Giuseppe Martelli6Vittoria Infantino7Carla Caddeo8Department of Science, University of Basilicata, Viale dell’Ateneo Lucano 10, 85100 Potenza, ItalyDepartment of Pharmacy, University of Salerno, Via Giovanni Paolo II 132, 84084 Salerno, ItalyDepartment of Science, University of Basilicata, Viale dell’Ateneo Lucano 10, 85100 Potenza, ItalyDepartment of Science, University of Basilicata, Viale dell’Ateneo Lucano 10, 85100 Potenza, ItalyDepartment of Science, University of Basilicata, Viale dell’Ateneo Lucano 10, 85100 Potenza, ItalyDepartment of Science, University of Basilicata, Viale dell’Ateneo Lucano 10, 85100 Potenza, ItalyDepartment of Science, University of Basilicata, Viale dell’Ateneo Lucano 10, 85100 Potenza, ItalyDepartment of Science, University of Basilicata, Viale dell’Ateneo Lucano 10, 85100 Potenza, ItalyDepartment of Scienze della Vita e dell’Ambiente, Sezione di Scienze del Farmaco, University of Cagliari, Via Ospedale 72, 09124 Cagliari, ItalyHydroxycitrate (HCA), a main organic acid component of the fruit rind of <i>Garcinia cambogia</i>, 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 E<sub>2</sub> (PGE<sub>2</sub>)) 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 PGE<sub>2</sub> 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 PGE<sub>2</sub> increase. This suggests that liposomal HCA can be exploited to target the citrate pathway involved in inflammatory processes.https://www.mdpi.com/2079-4991/10/10/2080hydroxycitrateliposomesmacrophagesinflammationantioxidant |
| spellingShingle | Antonio Vassallo Valentina Santoro Ilaria Pappalardo Anna Santarsiero Paolo Convertini Maria De Luca Giuseppe Martelli Vittoria Infantino Carla Caddeo Liposome-Mediated Inhibition of Inflammation by Hydroxycitrate Nanomaterials hydroxycitrate liposomes macrophages inflammation antioxidant |
| title | Liposome-Mediated Inhibition of Inflammation by Hydroxycitrate |
| title_full | Liposome-Mediated Inhibition of Inflammation by Hydroxycitrate |
| title_fullStr | Liposome-Mediated Inhibition of Inflammation by Hydroxycitrate |
| title_full_unstemmed | Liposome-Mediated Inhibition of Inflammation by Hydroxycitrate |
| title_short | Liposome-Mediated Inhibition of Inflammation by Hydroxycitrate |
| title_sort | liposome mediated inhibition of inflammation by hydroxycitrate |
| topic | hydroxycitrate liposomes macrophages inflammation antioxidant |
| url | https://www.mdpi.com/2079-4991/10/10/2080 |
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