Molecular Docking Appraisal of Pleurotus ostreatus Phytochemicals as Potential Inhibitors of PI3K/Akt Pathway for Breast Cancer Treatment DOI Creative Commons
Magdalene Eno Effiong, Mercy Bella-Omunagbe, Israel Sunmola Afolabi

et al.

Bioinformatics and Biology Insights, Journal Year: 2025, Volume and Issue: 19

Published: Jan. 1, 2025

Introduction: Breast cancer (BC) is a heterogeneous disease involving network of numerous extracellular signal transduction pathways. The phosphoinositide 3-kinase (PI3K)/serine/threonine kinase (Akt)/mechanistic target rapamycin (mTOR) pathway crucial for understanding the BC development. Phosphoinositide 3-kinase, phosphatase and tensin homolog (PTEN), mTOR, Akt, 3-phosphoinositide-dependent 1 (PDK1), FoxO1, glycogen synthase 3 (GSK-3), mouse double minute 2 (MDM2), H-Ras, proapoptotic B-cell lymphoma (BCL-2) family protein (BAD) proteins are key drivers this potential therapeutic targets. Pleurotus ostreatus an edible mushroom that rich in flavonoids phenols can serve as inhibitors PI3K/Akt/mTOR pathway. Aim: This study evaluated anticancer properties P through structure-based virtual screening 22 biologically active compounds present mushroom. Method: Model optimization was carried out on PI3K, PTEN, PDK1, GSK-3, MDM2, BAD molecular docking compounds/control binding pocket were simulated AutoDock Vina PyRx. drug likeness, pharmacokinetic, pharmacodynamic features prospective leads all anticipated. Result: Several potent selected driver identified from ostreatus. Ellagic acid with affinities −8.0, −8.1, −8.2, −6.2, −7.1 kcal/mol BAD, respectively, had better affinity compared their reference drugs. Likewise, apigenin (−7.8 kcal/mol), chrysin quercetin (−6.4 chlorogenic (−6.2 kcal/mol) to H-Ras proteins, respectively. Conclusion: acid, apigenin, luteolin, quercetin, chrysin, naringenin phytochemicals seen lead molecules due ability strongly bind under Analogs these also be designed

Language: Английский

Development and Validation of Microwave-assisted Extraction for Phenolic Compound Profiling in Diverse Oyster Mushrooms (Pleurotus spp.) Sourced from Various Geographical Regions DOI Creative Commons

M Umar Harun,

Miguel Palma, Widiastuti Setyaningsih

et al.

Journal of Agriculture and Food Research, Journal Year: 2025, Volume and Issue: unknown, P. 101754 - 101754

Published: Feb. 1, 2025

Language: Английский

Citations

1

Punica granatum L. Peel: Anticancer Activity on Hep3B, Drug‐likeness, ADMET Prediction, and Molecular Docking with EGFR‐TK DOI
Dua Danjolli‐Hashani,

Şebnem Selen İşbilir,

Ayşen Şuekinci Yılmaz

et al.

ChemistrySelect, Journal Year: 2025, Volume and Issue: 10(3)

Published: Jan. 1, 2025

Abstract The side effects of the cancer treatment medications that have sparked renewed interest in herbal formulation research. Due to its high phytochemical content, Punica granatum L. (different parts pomegranate), a basic traditional medicine source, is an excellent option for anticancer In this study, activity (Hicaz variety) peel extract on Hep3B cell line was determined by MTT test. results showed P. cytotoxic effect (cancer) but no AML12 (healthy). To explain effect, main bioactive components peel, which are ellagic acid, abscisic ethyl gallate, phlorizin, gallic and myricetin, were performed docking study with EGFR‐TK (PDB ID: 1M17). poses all selected compounds bind same site as inhibitor erlotinib, while acid (−8.8 kcal/mol), myricetin (−8.9 phlorizin (−8.7 kcal/mol) lower binding energy. Also, drug similarity, physicochemical, ADMET properties these phenolic evaluated. All indicated could be potential therapeutic candidate against liver cancer.

Language: Английский

Citations

0

Mechanistic Insights into the Anticancer Potential of Methoxyflavones Analogs: A Review DOI Creative Commons

Mohammad Aidiel,

Maisarah Abdul Mutalib, Rajesh Ramasamy

et al.

Molecules, Journal Year: 2025, Volume and Issue: 30(2), P. 346 - 346

Published: Jan. 16, 2025

2-phenylchromen-4-one, commonly known as flavone, plays multifaceted roles in biological response that can be abundantly present natural sources. The methoxy group naturally occurring flavones promotes cytotoxic activity various cancer cell lines by targeting protein markers, facilitating ligand-protein binding mechanisms and activating cascading downstream signaling pathways leading to death. However, the lipophilic nature of these analogs is a key concern it impacts drug membrane transfer. While lipophilicity crucial for efficacy, excessive effects flavonoids reduce water solubility hinder transport target sites. Recent vitro studies suggest incorporation polar hydroxyl groups which form hydrogen bonds stabilize free radicals may help overcome challenges associated with while maintaining their essential properties. Naturally coexisting methoxyflavones, this review explores synergistic role hydroxy moieties through bonding capacity maximizing cytotoxicity against lines. physicochemical analysis revealed potential intramolecular interaction favorable electron delocalization region between both improve levels. Together, provides useful strategy structure-activity relationship (SAR) flavonoid distinct suggesting optimal functional positioning achieve balanced lipophilicity, effective bonding, simultaneously minimized steric hindrance specific types.

Language: Английский

Citations

0

Molecular Docking Appraisal of Pleurotus ostreatus Phytochemicals as Potential Inhibitors of PI3K/Akt Pathway for Breast Cancer Treatment DOI Creative Commons
Magdalene Eno Effiong, Mercy Bella-Omunagbe, Israel Sunmola Afolabi

et al.

Bioinformatics and Biology Insights, Journal Year: 2025, Volume and Issue: 19

Published: Jan. 1, 2025

Introduction: Breast cancer (BC) is a heterogeneous disease involving network of numerous extracellular signal transduction pathways. The phosphoinositide 3-kinase (PI3K)/serine/threonine kinase (Akt)/mechanistic target rapamycin (mTOR) pathway crucial for understanding the BC development. Phosphoinositide 3-kinase, phosphatase and tensin homolog (PTEN), mTOR, Akt, 3-phosphoinositide-dependent 1 (PDK1), FoxO1, glycogen synthase 3 (GSK-3), mouse double minute 2 (MDM2), H-Ras, proapoptotic B-cell lymphoma (BCL-2) family protein (BAD) proteins are key drivers this potential therapeutic targets. Pleurotus ostreatus an edible mushroom that rich in flavonoids phenols can serve as inhibitors PI3K/Akt/mTOR pathway. Aim: This study evaluated anticancer properties P through structure-based virtual screening 22 biologically active compounds present mushroom. Method: Model optimization was carried out on PI3K, PTEN, PDK1, GSK-3, MDM2, BAD molecular docking compounds/control binding pocket were simulated AutoDock Vina PyRx. drug likeness, pharmacokinetic, pharmacodynamic features prospective leads all anticipated. Result: Several potent selected driver identified from ostreatus. Ellagic acid with affinities −8.0, −8.1, −8.2, −6.2, −7.1 kcal/mol BAD, respectively, had better affinity compared their reference drugs. Likewise, apigenin (−7.8 kcal/mol), chrysin quercetin (−6.4 chlorogenic (−6.2 kcal/mol) to H-Ras proteins, respectively. Conclusion: acid, apigenin, luteolin, quercetin, chrysin, naringenin phytochemicals seen lead molecules due ability strongly bind under Analogs these also be designed

Language: Английский

Citations

0