Neuroprotective Potential of Indole-Based Compounds: A Biochemical Study on Antioxidant Properties and Amyloid Disaggregation in Neuroblastoma Cells DOI Creative Commons
Tania Ciaglia, Maria Rosaria Miranda, Simone Di Micco

et al.

Antioxidants, Journal Year: 2024, Volume and Issue: 13(12), P. 1585 - 1585

Published: Dec. 23, 2024

Based on the established neuroprotective properties of indole-based compounds and their significant potential as multi-targeted therapeutic agents, a series synthetic indole–phenolic was evaluated multifunctional neuroprotectors. Each compound demonstrated metal-chelating properties, particularly in sequestering copper ions, with quantitative analysis revealing approximately 40% chelating activity across all compounds. In cellular models, these hybrid exhibited strong antioxidant cytoprotective effects, countering reactive oxygen species (ROS) generated by Aβ(25–35) peptide its oxidative byproduct, hydrogen peroxide, showing average 25% increase cell viability reduction ROS levels to basal states. Further using thioflavin T fluorescence assays, circular dichroism, computational studies indicated that synthesized derivatives effectively promoted self-disaggregation fragment. Taken together, findings suggest unique profile actions for derivatives, combining chelating, antioxidant, anti-aggregation which position them promising development agents Alzheimer’s disease therapy. The methods used provide reliable vitro data, although further vivo validation assessment blood–brain barrier penetration are needed confirm efficacy safety.

Language: Английский

Modulation of the Neuro–Cancer Connection by Metabolites of Gut Microbiota DOI Creative Commons
Alice Njolke Mafe, Dietrich Büsselberg

Biomolecules, Journal Year: 2025, Volume and Issue: 15(2), P. 270 - 270

Published: Feb. 12, 2025

The gut-brain-cancer axis represents a novel and intricate connection between the gut microbiota, neurobiology, cancer progression. Recent advances have accentuated significant role of microbiota metabolites in modulating systemic processes that influence both brain health tumorigenesis. This paper explores emerging concept metabolite-mediated modulation within connection, focusing on key such as short-chain fatty acids (SCFAs), tryptophan derivatives, secondary bile acids, lipopolysaccharides (LPS). While microbiota's impact immune regulation, neuroinflammation, tumor development is well established, gaps remain grasping how specific contribute to neuro-cancer interactions. We discuss with potential implications for neurobiology cancer, indoles polyamines, which yet be extensively studied. Furthermore, we review preclinical clinical evidence linking dysbiosis, altered metabolite profiles, tumors, showcasing limitations research gaps, particularly human longitudinal studies. Case studies investigating microbiota-based interventions, including dietary changes, fecal transplantation, probiotics, demonstrate promise but also indicate hurdles translating these findings therapies. concludes call standardized multi-omics approaches bi-directional frameworks integrating microbiome, neuroscience, oncology develop personalized therapeutic strategies patients.

Language: Английский

Citations

1
From Infection to Tumor: Exploring the Therapeutic Potential of Ciprofloxacin Derivatives as Anticancer Agents DOI Creative Commons

Hesham M. Hassan,

Roket Hassan,

Ranya Mohammed Elmagzoub

et al.

Pharmaceuticals, Journal Year: 2025, Volume and Issue: 18(1), P. 72 - 72

Published: Jan. 9, 2025

Ciprofloxacin, a widely used second-generation fluoroquinolone for treating bacterial infections, has recently shown notable anticancer properties. This review explores progress in developing ciprofloxacin derivatives with properties, emphasizing key structural changes that improve their therapeutic effectiveness by modifying the basic group at position 7, carboxylic acid 3, or both. It further investigates mechanisms which these fight cancer, such as inducing apoptosis, arresting cell cycle, inhibiting topoisomerase I and II, preventing tubulin polymerization, suppressing interleukin 6, blocking thymidine phosphorylase, multidrug resistance proteins, hindering angiogenesis. Additionally, it outlines future directions, enhancing efficacy, selectivity, investigating potential synergy other chemotherapeutic agents, offering promising avenue new therapies cancer.

Language: Английский

Citations

0
Pancreatic lipase inhibitors as anti-obesity agents: a review of recent chemical scaffolds and their pancreatic lipase inhibitory potential DOI
Noor ul Amin Mohsin, Matloob Ahmad, Maryam Farrukh

et al.

Medicinal Chemistry Research, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 18, 2025

Language: Английский

Citations

0
Development of indole hybrids for potential lung cancer treatment-part I: nitrogen-containing six-membered aromatic heterocycles DOI

Shijia Zhao,

Zhi Xu

Future Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 17

Published: March 29, 2025

Lung cancer is the most prevalent invasive malignancy and leading cause of cancer-related death. Chemotherapy vital for lung therapy, but multidrug resistance responsible majority fatalities, creating an imperative demand to develop novel chemotherapeutics. Indole a valuable anti-lung pharmacophore since its derivatives could act on cells through various mechanisms. Notably, indole hybrids inhibit multiple targets simultaneously have potential overcome shortcomings traditional Moreover, many such as indole-pyrimidine hybrid osimertinib indole-hydroxamic acid panobinostat, are either under clinical evaluations or already been approved therapy. This indicates that rational design represents highly prospective approach development new chemotherapeutic agents. review focuses exploring therapeutic delves into their action mechanisms well structure-activity correlations, covering articles published between 2021 present. The ultimate goal offer foundation in future.

Language: Английский

Citations

0
Development of indole hybrids for potential lung cancer treatment - part II DOI
Shanshan Huang,

Zhi Xu,

Yafei Zhuang

et al.

Future Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 17

Published: March 30, 2025

Lung cancer has become the most prevalent for past three decades, and 5-years survival rate of lung is only ~20% nowadays. Chemotherapy mainstay therapy, especially non-small cell cancer. However, drug resistance represents a principal cause therapeutic failure in leading to insensitivity, tumor recurrence, disease progression. Indole hybrids have potential conquer resistance, enhance efficacy, reduce adverse events, improve pharmacokinetic properties due their capacity inhibit multiple targets simultaneously. Moreover, indole osimertinib, mobocertinib, cediranib, vizimpro are currently applied clinics demonstrating that valuable scaffolds treatment eradication This review provides comprehensive overview evolving landscape with vitro vivo efficacy against cancer, structure–activity relationships as well mechanisms action also discussed, covering articles published from 2021 onward.

Language: Английский

Citations

0
An insight into the therapeutic impact of quinoxaline derivatives: Recent advances in biological activities (2020–2024) DOI Creative Commons

Aly M. Waseem,

Ranya Mohammed Elmagzoub,

Mervat Mohammed Mazhar Abdelgadir

et al.

Results in Chemistry, Journal Year: 2024, Volume and Issue: unknown, P. 101989 - 101989

Published: Dec. 1, 2024

Language: Английский

Citations

3
Bisindole Compounds—Synthesis and Medicinal Properties DOI Creative Commons
Maria Marinescu

Antibiotics, Journal Year: 2024, Volume and Issue: 13(12), P. 1212 - 1212

Published: Dec. 13, 2024

The indole nucleus stands out as a pharmacophore, among other aromatic heterocyclic compounds with remarkable therapeutic properties, such benzimidazole, pyridine, quinoline, benzothiazole, and others. Moreover, series of recent studies refer to strategies for the synthesis bisindole derivatives, various medicinal antimicrobial, antiviral, anticancer, anti-Alzheimer, anti-inflammatory, antioxidant, antidiabetic, etc. Also, natural are mentioned in literature their biological properties starting point related bisindoles. Drawing from these data, we have proposed this review provide an overview techniques qualities bisindolic that been 2010 2024 well numerous uses chemistry materials, nanomaterials, dyes, polymers, corrosion inhibitors.

Language: Английский

Citations

1
Neuroprotective Potential of Indole-Based Compounds: A Biochemical Study on Antioxidant Properties and Amyloid Disaggregation in Neuroblastoma Cells DOI Creative Commons
Tania Ciaglia, Maria Rosaria Miranda, Simone Di Micco

et al.

Antioxidants, Journal Year: 2024, Volume and Issue: 13(12), P. 1585 - 1585

Published: Dec. 23, 2024

Based on the established neuroprotective properties of indole-based compounds and their significant potential as multi-targeted therapeutic agents, a series synthetic indole–phenolic was evaluated multifunctional neuroprotectors. Each compound demonstrated metal-chelating properties, particularly in sequestering copper ions, with quantitative analysis revealing approximately 40% chelating activity across all compounds. In cellular models, these hybrid exhibited strong antioxidant cytoprotective effects, countering reactive oxygen species (ROS) generated by Aβ(25–35) peptide its oxidative byproduct, hydrogen peroxide, showing average 25% increase cell viability reduction ROS levels to basal states. Further using thioflavin T fluorescence assays, circular dichroism, computational studies indicated that synthesized derivatives effectively promoted self-disaggregation fragment. Taken together, findings suggest unique profile actions for derivatives, combining chelating, antioxidant, anti-aggregation which position them promising development agents Alzheimer’s disease therapy. The methods used provide reliable vitro data, although further vivo validation assessment blood–brain barrier penetration are needed confirm efficacy safety.

Language: Английский

Citations

1