Storage Stability of Atheroglitatide, an Echogenic Liposomal Formulation of Pioglitazone Targeted to Advanced Atheroma with a Fibrin-Binding Peptide

Authors

Khalid Alghamdi
Zeyad Alehaideb
Ashok Kumar
Hamad Al-Eidi
Sahar S Alghamdi
Rasha Suliman
Rizwan Ali
Feras Almourfi
Saleh M Alghamdi
Mohamed Boudjelal
Sabine Matou-Nasri

Language

English

Publication Date

1-1-2023

Journal

Frontiers in Pharmacology

DOI

10.3389/fphar.2023.1169812

PMID

37197407

PMCID

PMC10184183

PubMedCentral® Posted Date

April 2023

PubMedCentral® Full Text Version

Post-print

Abstract

There is no first-line treatment for vitiligo, a skin disease characterized by a lack of melanin produced by the melanocytes, resulting in an urgent demand for new therapeutic drugs capable of stimulating melanocyte functions, including melanogenesis. In this study, traditional medicinal plant extracts were tested for cultured human melanocyte proliferation, migration, and melanogenesis using MTT, scratch wound-healing assays, transmission electron microscopy, immunofluorescence staining, and Western blot technology. Of the methanolic extracts, Lycium shawii L. (L. shawii) extract increased melanocyte proliferation at low concentrations and modulated melanocyte migration. At the lowest tested concentration (i.e., 7.8 μg/mL), the L. shawii methanolic extract promoted melanosome formation, maturation, and enhanced melanin production, which was associated with the upregulation of microphthalmia-associated transcription factor (MITF), tyrosinase, tyrosinase-related protein (TRP)-1 and TRP-2 melanogenesis-related proteins, and melanogenesis-related proteins. After the chemical analysis and L. shawii extract-derived metabolite identification, the in silico studies revealed the molecular interactions between Metabolite 5, identified as apigenin (4,5,6-trihydroxyflavone), and the copper active site of tyrosinase, predicting enhanced tyrosinase activity and subsequent melanin formation. In conclusion, L. shawii methanolic extract stimulates melanocyte functions, including melanin production, and its derivative Metabolite 5 enhances tyrosinase activity, suggesting further investigation of the L. shawii extract-derived Metabolite 5 as a potential natural drug for vitiligo treatment.

Keywords

Lycium shawii, human melanocyte, melanogenesis, melanin, natural product, skin depigmentation, vitiligo

Published Open-Access

yes

Recommended Citation

Alghamdi, Khalid; Alehaideb, Zeyad; Kumar, Ashok; et al., "Storage Stability of Atheroglitatide, an Echogenic Liposomal Formulation of Pioglitazone Targeted to Advanced Atheroma with a Fibrin-Binding Peptide" (2023). Faculty, Staff and Student Publications. 2485.
https://digitalcommons.library.tmc.edu/uthmed_docs/2485