A preliminary investigation into the activity and toxicity of an amyloid-based Emodin formulation

IF 2.6 4区医学 Q2 PHARMACOLOGY & PHARMACY

Toxicon Pub Date : 2025-03-01 DOI:10.1016/j.toxicon.2025.108308

Anderson Gattis , Alejandro Hinojosa , Maytham Ismail , Venkateshwar G. Keshamouni , Mathumai Kanapathipillai

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Abstract

Emodin is a natural plant derivative with many therapeutic properties including anti-cancer, anti-apoptosis, and anti-inflammatory effects. However, the delivery of Emodin is quite challenging due to its superhydrophobic properties. Furthermore, conventional systemic delivery approaches often result in side effects. Thus, alternative strategies are important for the successful delivery of Emodin. The goal of this study was to develop a novel Emodin drug depot utilizing peptide amyloids. For the peptides, an aggregation-prone amino acid domain of receptor-interacting serine/threonine-protein kinase 3 (RIP3) protein was used. The RIP3/Emodin amyloid aggregates physicochemical characterization, cellular uptake, effects on toxicity, oxidative stress, and inflammation were investigated. Studies reveal that Emodin-encapsulated RIP3 peptide amyloid aggregates were able to induce significant lung cancer cell toxicity compared to free Emodin. Further, aggregates alone did not exhibit toxicity and or oxidative stress. In addition, the formulation was able to inhibit lipopolysaccharide (LPS) mediated inflammation in macrophage cells. Overall, the studies indicate the potential of RIP3 peptide amyloids as hydrophobic drug depots.

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来源期刊

Toxicon 医学-毒理学

CiteScore

4.80

自引率

10.70%

发文量

358

审稿时长

68 days

期刊介绍： Toxicon has an open access mirror Toxicon: X, sharing the same aims and scope, editorial team, submission system and rigorous peer review. An introductory offer Toxicon: X - full waiver of the Open Access fee. Toxicon''s "aims and scope" are to publish: -articles containing the results of original research on problems related to toxins derived from animals, plants and microorganisms -papers on novel findings related to the chemical, pharmacological, toxicological, and immunological properties of natural toxins -molecular biological studies of toxins and other genes from poisonous and venomous organisms that advance understanding of the role or function of toxins -clinical observations on poisoning and envenoming where a new therapeutic principle has been proposed or a decidedly superior clinical result has been obtained. -material on the use of toxins as tools in studying biological processes and material on subjects related to venom and antivenom problems. -articles on the translational application of toxins, for example as drugs and insecticides -epidemiological studies on envenoming or poisoning, so long as they highlight a previously unrecognised medical problem or provide insight into the prevention or medical treatment of envenoming or poisoning. Retrospective surveys of hospital records, especially those lacking species identification, will not be considered for publication. Properly designed prospective community-based surveys are strongly encouraged. -articles describing well-known activities of venoms, such as antibacterial, anticancer, and analgesic activities of arachnid venoms, without any attempt to define the mechanism of action or purify the active component, will not be considered for publication in Toxicon. -review articles on problems related to toxinology. To encourage the exchange of ideas, sections of the journal may be devoted to Short Communications, Letters to the Editor and activities of the affiliated societies.