Liposome-Encapsulated Bioactive Guttiferone E Exhibits Anti-Inflammatory Effect in Lipopolysaccharide-Stimulated MH-S Macrophages and Cytotoxicity against Human Cancer Cells

Background. Guttiferone E is a naturally occurring polyisoprenylated benzophenone exhibiting a wide range of remarkable biological activities. But its therapeutic application is still limited due to its poor water solubility. This study is aimed at preparing guttiferone E-loaded liposomes and assess...

Full description

Saved in:
Bibliographic Details
Published in:Mediators of inflammation 2022-08, Vol.2022, p.1-10
Main Authors: Dzoyem, Jean Paul, Pinnapireddy, Shashank Reddy, Fouotsa, Hugues, Brüßler, Jana, Runkel, Frank, Bakowsky, Udo
Format: Article
Language:English
Subjects:
Anti-inflammatory drugs
Atomic force microscopy
Benzophenone
Cancer
Cancer cells
Cancer therapies
Cytotoxicity
Dielectric films
Efficiency
Enzymes
Ethylenediaminetetraacetic acid
Health aspects
Inflammation
Lasers
Light scattering
Lipids
Lipopolysaccharides
Liposomes
Macrophages
Microscopy
Morphology
Natural products
Nitric oxide
Nonsteroidal anti-inflammatory drugs
Prostaglandin endoperoxide synthase
Silicon nitride
Thin films
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Background. Guttiferone E is a naturally occurring polyisoprenylated benzophenone exhibiting a wide range of remarkable biological activities. But its therapeutic application is still limited due to its poor water solubility. This study is aimed at preparing guttiferone E-loaded liposomes and assessing their in vitro cytotoxicity and anti-inflammatory effect. Methods. Liposomes containing guttiferone E were prepared by the thin film hydration method, and the physicochemical characteristics were determined using dynamic light scattering, laser Doppler velocimetry, and atomic force microscopy. The cytotoxicity was assessed by the MTT assay. The fluorometric cyclooxygenase (COX) activity assay kit was used to assess the COX activity while the nitric oxide production was evaluated by the Griess reagent method. Results. The liposomes with a mean size of 183.33±17.28 nm were obtained with an entrapment efficiency of 63.86%. Guttiferone E-loaded liposomes successfully decreased the viability of cancer cells. The overall IC50 values varied between 5.46 μg/mL and 22.25 μg/mL. Compared to the untreated control, guttiferone E-loaded liposomes significantly reduced the nitric oxide production and the activity of COX in a concentration-dependent manner. Conclusion. This study indicates that liposomes can be an alternative to overcome the water insolubility issue of the bioactive guttiferone E.
ISSN:0962-9351
1466-1861
DOI:10.1155/2022/8886087