In Vitro and In Vivo Biological Evaluation of Novel 1,4‐Naphthoquinone Derivatives as Potential Anticancer Agents DOI
Palanisamy Ravichandiran, Aleksandra Martyna, Elżbieta Kochanowicz

и другие.

ChemMedChem, Год журнала: 2024, Номер unknown

Опубликована: Авг. 13, 2024

Abstract A novel library of naphthoquinone derivatives ( 3–5 aa ) was synthesized and evaluated for their anticancer properties. Specifically, compounds 5 i, l, o, q, r, s, t , v demonstrated superior cytotoxic activity against the cancer cell lines that were studied. All studied exhibited a higher selectivity index (SI) favourable safety profile than standard drug doxorubicin. Notably, compound displayed greater effect on MCF‐7 cells (IC 50 =1.2 μM, 0.9 μM at 24 h 48 h, respectively) compared to doxorubicin =2.4 2.1 respectively). To further investigate mechanism effect, additional studies conducted with in cells. The are including morphological changes, AO/EB (acridine orange/ethidium bromide) double staining, apoptosis analysis, colony assay, SDS‐PAGE Western blotting, cycle detecting reactive oxygen species (ROS) assay. findings showed triggered effects through initiation arrest G1/S phase necrosis. In vivo ecotoxicity indicated had lower toxicity towards zebrafish larvae (LC =50.15 μM) an insignificant impact cardiac functions. xenotransplantation significant reduction tumour volume xenograft. Approximately 95 % xenografts survived after 10 days treatment. Finally, computational modelling study four protein receptors, namely ER, EFGR, BRCA1, VEFGR2. highlight importance aminonaphthoquinone moiety, amide linkage, propyl thio moiety enhancing drug‐likeness features docking scores (−9.1, −7.1, −8.9, −10.9 kcal/mol) (−7.2, −6.1, −6.9, −7.3 VEGFR2 respectively. Therefore, notable antitumor suggest these molecular frameworks may play role development promising agents

Язык: Английский

Intracellular metal ion-based chemistry for programmed cell death DOI
Y You, Zhongying Guo, Tyler Wolter

и другие.

Chemical Society Reviews, Год журнала: 2025, Номер unknown

Опубликована: Янв. 1, 2025

Intracellular metal ions play essential roles in multiple physiological processes, including catalytic action, diverse cellular intracellular signaling, and electron transfer. It is crucial to maintain ion homeostasis which achieved by the subtle balance of storage release intracellularly along with influx efflux at interface cell membrane. Dysregulation has been identified as a key mechanism triggering programmed death (PCD). Despite importance initiating PCD, molecular mechanisms within these processes are infrequently discussed. An in-depth understanding review role PCD may better uncover novel tools for cancer diagnosis therapy. Specifically, calcium (Ca

Язык: Английский

Процитировано

0

Recent Advances in Metal Complexes Based on Biomimetic and Biocompatible Organic Ligands against Leishmaniasis Infections: State of the Art and Alternatives DOI Creative Commons
Sandra Jiménez-Falcao, José M. Méndez‐Arriaga

Inorganics, Год журнала: 2024, Номер 12(7), С. 190 - 190

Опубликована: Июль 12, 2024

Leishmaniasis is a complex disease present in variety of manifestations listed by the World Health Organization (WHO) as one neglected diseases with worse prognosis if not treated. Medicinal inorganic chemistry has provided drugs based on metal–organic complexes synthesized different metal centers and organic ligands to fight against great number parasite maladies specifically Leishmaniasis. Taking advantage natural properties that many metals for biotechnological purposes, nanotechnology offered, recent years, new approach consisting application nanoparticles treat parasitic diseases, drug vehicle or treatment themselves. The aim this review gather most widely used metallic strategies proposed antileishmanial agents.

Язык: Английский

Процитировано

3

Photoactivated Anticancer Activity of Cobalt(III) Complexes with Naturally Occurring Flavonoids Chrysin and Silibinin DOI

Jyotirmoy Dutta,

Arpan Bera, Aarti Upadhyay

и другие.

ChemBioChem, Год журнала: 2024, Номер unknown

Опубликована: Авг. 22, 2024

Abstract Photoactive metal complexes of bioessential transition ions with natural chelators are gaining interest as photocytotoxic agents for cancer photodynamic therapy (PDT). We report six new cobalt(III) a mixed‐ligand formulation [Co(B) 2 (L)](ClO 4 ) ( Co1 – Co6 ), where B represents N,N‐donor α ‐diimine ligand, namely, phenanthroline (phen; , Co2 dipyrido[3,2‐ d :2’,3’‐ f ]quinoxaline (dpq; Co3 Co4 and c ]phenazine (dppz; Co5 L is the monoanionic form naturally occurring flavonoids chrysin (chry; silibinin (sili; ). Complexes displayed d‐d absorption band within 500–700 nm exhibited excellent dark photostability in solution. Cytotoxicity studies indicated significant activity against cervical (HeLa) lung (A549) cells under visible light (400–700 nm) irradiation giving low micromolar IC 50 values (2.3–3.4 μM, phototoxicity index~15–30). The demonstrated notably toxicity normal HPL1D epithelial cells. Flow cytometry assay revealed an apoptotic mode cell damage triggered by when irradiated. ROS generation involvement singlet oxygen species death mechanism irradiated light. Overall, coordinated dipyridophenazine flavonoid ligands potential candidates PDT applications.

Язык: Английский

Процитировано

2

In Vitro and In Vivo Biological Evaluation of Novel 1,4‐Naphthoquinone Derivatives as Potential Anticancer Agents DOI
Palanisamy Ravichandiran, Aleksandra Martyna, Elżbieta Kochanowicz

и другие.

ChemMedChem, Год журнала: 2024, Номер unknown

Опубликована: Авг. 13, 2024

Abstract A novel library of naphthoquinone derivatives ( 3–5 aa ) was synthesized and evaluated for their anticancer properties. Specifically, compounds 5 i, l, o, q, r, s, t , v demonstrated superior cytotoxic activity against the cancer cell lines that were studied. All studied exhibited a higher selectivity index (SI) favourable safety profile than standard drug doxorubicin. Notably, compound displayed greater effect on MCF‐7 cells (IC 50 =1.2 μM, 0.9 μM at 24 h 48 h, respectively) compared to doxorubicin =2.4 2.1 respectively). To further investigate mechanism effect, additional studies conducted with in cells. The are including morphological changes, AO/EB (acridine orange/ethidium bromide) double staining, apoptosis analysis, colony assay, SDS‐PAGE Western blotting, cycle detecting reactive oxygen species (ROS) assay. findings showed triggered effects through initiation arrest G1/S phase necrosis. In vivo ecotoxicity indicated had lower toxicity towards zebrafish larvae (LC =50.15 μM) an insignificant impact cardiac functions. xenotransplantation significant reduction tumour volume xenograft. Approximately 95 % xenografts survived after 10 days treatment. Finally, computational modelling study four protein receptors, namely ER, EFGR, BRCA1, VEFGR2. highlight importance aminonaphthoquinone moiety, amide linkage, propyl thio moiety enhancing drug‐likeness features docking scores (−9.1, −7.1, −8.9, −10.9 kcal/mol) (−7.2, −6.1, −6.9, −7.3 VEGFR2 respectively. Therefore, notable antitumor suggest these molecular frameworks may play role development promising agents

Язык: Английский

Процитировано

1