Modular Synthesis and Cytotoxicity Evaluation of Dragocins A—C and Their Analogues: Discovery of a Potential Anticancer Agent DOI Open Access
Ziqiang Wang, Jianjun Wang, Peng Wang

et al.

Chinese Journal of Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 11, 2025

Comprehensive Summary Dragocins A—C are structurally unique marine natural products featuring an uncommon tri‐oxa‐tricyclic[6.2.1]undecane moiety. However, their extremely low abundance has hindered extensive screening of bioactivities. We hereby describe efficient and modular approach to synthesizing dragocins analogues using commercially available inexpensive anisomycin D‐ribosyl thioglycoside derivative as the starting materials. A key feature our synthesis is construction skeleton. This challenging architecture achieved by stereocontrolled formation β‐ribofuranosidic bond DDQ (2,3‐dichloro‐5,6‐dicyano‐1,4‐benzoquinone)‐promoted intramolecular cross‐dehydrogenative etherification at benzylic position. Our also characterized successful installation a chlorine atom methoxy group tertiary C‐4' position via late‐stage silver‐catalyzed decarboxylative chlorination reaction electrophilic enol intermediate. Cytotoxicity evaluations synthesized compounds revealed demethyl dragocin A, N ‐demethylated potential anticancer candidate due its strong cytotoxicity against A549 lung, HCT116 colorectal MCF7 breast cancer cell lines. work demonstrated preliminary structure‐activity relationship this compound, setting solid foundation for developing novel candidates.

Language: Английский

Unraveling the Mechanism of Carbonic Anhydrase IX Inhibition by Alkaloids from Ruta chalepensis: A Synergistic Analysis of In Vitro and In Silico Data DOI
Haifa A. Alqhtani,

Sarah I. Othman,

Faris F. Aba Alkhayl

et al.

Biochemical and Biophysical Research Communications, Journal Year: 2024, Volume and Issue: 733, P. 150685 - 150685

Published: Sept. 11, 2024

Language: Английский

Citations

7

Historical Perspective and Current Trends in Anticancer Drug Development DOI Open Access
Katarzyna Gach, Joanna Drogosz-Stachowicz, Anna Janecka

et al.

Cancers, Journal Year: 2024, Volume and Issue: 16(10), P. 1878 - 1878

Published: May 15, 2024

Cancer is considered one of the leading causes death in 21st century. The intensive search for new anticancer drugs has been actively pursued by chemists and pharmacologists decades, focusing either on isolation compounds with cytotoxic properties from plants or screening thousands synthetic molecules. Compounds that could potentially become candidates must have ability to inhibit proliferation and/or induce apoptosis cancer cells without causing too much damage normal cells. Some were discovered accident, others as a result long-term research. In this review, we presented brief history development most important groups drugs, pointing fact they all many side effects.

Language: Английский

Citations

5

Marine seaweed endophytic fungi-derived active metabolites promote reactive oxygen species-induced cell cycle arrest and apoptosis in human breast cancer cells DOI

Jeyamanikandan Venkatachalam,

Veronica Shalini Jeyadoss,

Kabilan Subash Chandra Bose

et al.

Molecular Biology Reports, Journal Year: 2024, Volume and Issue: 51(1)

Published: May 5, 2024

Language: Английский

Citations

4

Synthesis and characterization of innovative GA@Ag-CuO nanocomposite with potent antimicrobial and anticancer properties DOI Creative Commons
Amr H. Hashem, Mostafa A. Abdel-Maksoud, Sabiha Fatima

et al.

Scientific Reports, Journal Year: 2025, Volume and Issue: 15(1)

Published: Jan. 3, 2025

Cancer and microbial infections place a significant burden on the world's health systems can increase rate of disease mortality. In current study, novel nanocomposite based Gum Arabic, silver copper oxide nanoparticles (GA@Ag-CuO nanocomposite) was synthesized to overcome problem infection in cancer treatment. Characterization using UV-Vis. spectrophotometer reveals that, observed peak spectrum formed by O.D. at 0.755, confirmed that produced GA@Ag-CuO small discernible 360 nm. The particles' diameters varied from 9.5 nm 49.5 nm, with mean diameter 25.53 ± 1.4 created Arabic filtrate rich active functional groups, provided polydisperse NPs were intended reduce, stabilize, act as capping agents. Based XRD data, crystallized had face-centered (fcc) crystal structure. Biosafety assessed toward Wi 38 normal cell line, where it showed safety tested line IC50 154.2 µg/mL. Antimicrobial results has antibacterial activity MICs 15.6, 125, 31.25 125 µg/mL against S. epidermis, aureus, L. plantrum, typhimurium, respectively. Likewise, antifungal C. albicans neoformans 62.5 15.62 µg/ml, Moreover, displayed promising anticancer 26.11 59.5 µg/ml MCF-7 Hep-G2, conclusion, demonstrated antibacterial, antifungal, activities.

Language: Английский

Citations

0

Phytochemical Profile and Anticancer Potential of Helichrysum arenarium Extracts on Glioblastoma, Bladder Cancer, and Breast Cancer Cells DOI Creative Commons
İhsan Nalkıran, Hatice Sevim Nalkıran

Pharmaceuticals, Journal Year: 2025, Volume and Issue: 18(2), P. 144 - 144

Published: Jan. 22, 2025

Background/Objectives: Cancer is the second leading cause of death globally. Medicinal plants have emerged as fundamental sources bioactive compounds with anticancer potential, largely attributed to their diverse secondary metabolites. This study aimed investigate cytotoxic effects Helichrysum arenarium extracts from two distinct regions Turkiye, Mersin, and Artvin, on cancerous (MDA-MB-231, RT4, T98G) non-cancerous (ARPE-19, hGF) cell lines identify responsible for these effects. Methods: H. plant were prepared using ethanol methanol solvents, followed by lyophilization dissolution in DMSO. The evaluated Hoechst staining MTS assays assess viability. IC50 values selectivity indices calculated. Phytochemical composition was analyzed Quadrupole Time-of-Flight mass spectrometry. Results: extract Mersin (HAE-M) demonstrated superior cytotoxicity, particularly against breast bladder cancer cells, while showing minimal impact cells. HAM-M, HAE-A, HAM-A exhibited comparatively less potent analysis HAE-M identified 16 compounds, including Naringenin, Luteolin, Quercitrin, known antioxidant properties. Conclusions: These findings highlight potential extracts, HAE-M, a source agents. novel its comprehensive different extraction methods regional sources, combined phytochemical profiling, selective Further investigations into mechanisms action could contribute development plant-derived therapies.

Language: Английский

Citations

0

Investigation of Aframomum melegueta compounds as ERK5 inhibitor related to breast cancer via molecular docking and dynamic simulation DOI

Paul Olamide Ottu,

Olorunfemi Oyewole Babalola, Oluwamodupe Cecilia Ejelonu

et al.

In Silico Pharmacology, Journal Year: 2025, Volume and Issue: 13(1)

Published: Jan. 25, 2025

Language: Английский

Citations

0

Potential Molecular Interactions and In Vitro Hyperthermia, Thermal, and Magnetic Studies of Bioactive Nickel-Doped Hydroxyapatite Thin Films DOI Open Access

Muhammad Sohail Asghar,

Uzma Ghazanfar,

Muhammad Rizwan

et al.

International Journal of Molecular Sciences, Journal Year: 2025, Volume and Issue: 26(3), P. 1095 - 1095

Published: Jan. 27, 2025

The treatment of bone cancer often necessitates the surgical removal affected tissues, with artificial implants playing a critical role in replacing lost structure. Functionalized represent an innovative approach to improve bio-integration and long-term effectiveness surgery treating cancer-damaged bones. In this study, nickel-substituted hydroxyapatite (Ni:HAp) nanoparticles were deposited as thin films using laser pulses range 30,000–60,000. Comprehensive structural, infrared, optical, morphological, surface, magnetic evaluations conducted on synthesized Ni:HAp films. hysteresis (M-H) loop demonstrated increase saturation magnetization higher number pulses. A minimum squareness ratio 0.7 was observed at 45,000 pulses, M-H characteristics indicated shift toward ferromagnetic behavior, achieving desired thermal response through alternating field application within 80 s. Thermogravimetric analysis revealed distinct stability, material structure exhibiting 46% degradation 800 °C. incorporation bioactive film holds significant promise for hyperthermia treatment. Using HDOCK simulations, interactions between ligand molecules proteins also explored. Strong binding affinities docking score −67.73 thus observed. presence Ca2+ ions enhances electrostatic interactions, providing valuable insights into biochemical roles therapeutic applications. Intravenous administration nanoparticles, which subsequently aggregate tumor tissue, combined applied field, enable targeted heating 45 This focused selectively targets cells while preserving surrounding healthy thereby potentially enhancing therapy

Language: Английский

Citations

0

Preparation, characterization, and in vitro release studies of multifunctional nanoformulations designed by functionalized graphene nanosheets with natural compounds DOI
Khaled AbouAitah, Yingjie Bu, Mukesh Sharma

et al.

FlatChem, Journal Year: 2025, Volume and Issue: unknown, P. 100824 - 100824

Published: Jan. 1, 2025

Language: Английский

Citations

0

In vitro and in silico studies of Vallisneria spiralis for breast cancer treatment. DOI Creative Commons
Ravindra Waykar,

Srinivasakumar Kumarapillai

Research Square (Research Square), Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 28, 2025

Abstract This research article investigates the anticancer potential of Vallisneria spiralis Linnaeus (Vallisneria L.) for human breast cancer management. The in vitro experiments demonstrated that increasing concentrations silver nanoparticles (AgNPs) and iron oxide (IONPs) resulted greater cytotoxicity against MCF-7 cells. antioxidant L. was assessed using 2-diphenyl-1-picryl-hydroxyl (DPPH) radical scavenging assay, which showed promising results. In silico analysis involved molecular docking phytocompounds with target protein (PDB ID: 3CZH). study presents a novel approach to treatment by developing nanoparticle-based drug delivery system derived from

Language: Английский

Citations

0

Apoptosis Induction and S-Phase Cell Cycle Blockade in Human Lung Adenocarcinoma Cell Line (A549) by Chlorophytum comosum (Thunb.) Jaques DOI Creative Commons
Shehla Adhami, Humaira Farooqi, Asrar Ahmad Malik

et al.

Research Square (Research Square), Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 29, 2025

Abstract Methods The ethanolic roots (CCRE) and leaves (CCLE) extracts were interrogated for their apoptotic potential against human lung adenocarcinoma cell line (A549) using DNA fragmentation, Annexin V-FITC/PI staining apoptosis assay cycle analysis flow cytometry. Results Our results revealed significant damage induced death in A549 on treatment with active concentrations (40 µg/ml 80 µg/ml) of the S phase arrest. Conclusions This is first study demonstrating inducing chemically characterized bioactive compounds present from Chlorophytum comosum non-small line. concludes that can be a candidate natural isolated, clinically evaluated development novel naturally derived anti-cancer drugs cancer.

Language: Английский

Citations

0