Pro-Apoptotic Activity of Epi -Obtusane against Cervical Cancer: Nano Formulation, In Silico Molecular Docking, and Pharmacological Network Analysis.

Autor: Abdelhafez OH; Department of Pharmacognosy, Faculty of Pharmacy, Deraya University, Universities Zone, New Minia 61111, Egypt., Abdel-Rahman IM; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Deraya University, New-Minia 61111, Egypt., Alaaeldin E; Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia 61519, Egypt.; Department of Pharmaceutics, Faculty of Pharmacy, Deraya University, Universities Zone, New Minia 61111, Egypt., Refaat H; Department of Pharmaceutical Sciences and Experimental Therapeutics, College of Pharmacy, University of Iowa, Iowa City, IA 52246, USA., El-Sayed R; Department of Chemistry, University College in Al-Jamoum, Umm Al-Qura University, Makkah 24231, Saudi Arabia.; Chemistry Department, Faculty of Science, Benha University, Benha 13518, Egypt., Al-Harbi SA; Department of Chemistry, University College in Al-Jamoum, Umm Al-Qura University, Makkah 24231, Saudi Arabia., Shawky AM; Science and Technology Unit (STU), Umm Al-Qura University, Makkah 21955, Saudi Arabia., Hegazy MF; Chemistry of Medicinal Plants Department, National Research Centre, El-Tahrir Street, Dokki, Giza 12622, Egypt., Moustafa AY; Zoology Department, Faculty of Science, Sohag University, Sohag 82524, Egypt., Shady NH; Department of Pharmacognosy, Faculty of Pharmacy, Deraya University, Universities Zone, New Minia 61111, Egypt.
Jazyk: angličtina
Zdroj: Pharmaceuticals (Basel, Switzerland) [Pharmaceuticals (Basel)] 2023 Nov 08; Vol. 16 (11). Date of Electronic Publication: 2023 Nov 08.
DOI: 10.3390/ph16111578
Abstrakt: Cancer is a major disease that threatens human health all over the world. Intervention and prevention in premalignant processes are successful ways to prevent cancer from striking. On the other hand, the marine ecosystem is a treasure storehouse of promising bioactive metabolites. The use of such marine products can be optimized by selecting a suitable nanocarrier. Therefore, epi -obtusane, previously isolated from Aplysia oculifera , was investigated for its potential anticancer effects toward cervical cancer through a series of in vitro assays in HeLa cells using the MTT assay method. Additionally, the sesquiterpene was encapsulated within a liposomal formulation (size = 130.8 ± 50.3, PDI = 0.462, zeta potential -12.3 ± 2.3), and the antiproliferative potential of epi -obtusane was investigated against the human cervical cancer cell line HeLa before and after encapsulation with liposomes. Epi -obtusane exhibited a potent effect against the HeLa cell line, while the formulated molecule with liposomes increased the in vitro antiproliferative activity. Additionally, cell cycle arrest analysis, as well as the apoptosis assay, performed via FITC-Annexin-V/propidium iodide double staining (flow cytofluorimetry), were carried out. The pharmacological network enabled us to deliver further insights into the mechanism of epi -obtusane, suggesting that STAT3 might be targeted by the compound. Moreover, molecular docking showed a comparable binding score of the isolated compound towards the STAT3 SH2 domain. The targets possess an anticancer effect through the endometrial cancer pathway, regulation of DNA templated transcription, and nitric oxide synthase, as mentioned by the KEGG and ShinyGo 7.1 databases.
Databáze: MEDLINE
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