Radiomodulatory and antioxidant properties of a novel pyrazine-linked quinazolinone sulfonamide derivative: Insights into renal apoptosis.

Heba M Karam, Mai H Mekkawy, Amira Abd-ElRaouf, Aiten M Soliman, Mostafa M Ghorab

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Article in Naunyn-Schmiedeberg's archives of pharmacology, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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5 authors.

Heba M KaramDrug Radiation Research Department, National Center for Radiation Research and Technology (NCRRT), Egyptian Atomic Energy Authority, Cairo, 11787, Egypt.

Mai H MekkawyDrug Radiation Research Department, National Center for Radiation Research and Technology (NCRRT), Egyptian Atomic Energy Authority, Cairo, 11787, Egypt.

Amira Abd-ElRaoufDrug Radiation Research Department, National Center for Radiation Research and Technology (NCRRT), Egyptian Atomic Energy Authority, Cairo, 11787, Egypt.

Aiten M SolimanDrug Radiation Research Department, National Center for Radiation Research and Technology (NCRRT), Egyptian Atomic Energy Authority, Cairo, 11787, Egypt. Aiten_mahmoud@yahoo.com.

Mostafa M GhorabDrug Radiation Research Department, National Center for Radiation Research and Technology (NCRRT), Egyptian Atomic Energy Authority, Cairo, 11787, Egypt.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Quinazolinone derivatives possess a privileged scaffold with variable pharmacological activities. This study conducted an in vitro evaluation of the pyrazine-linked quinazolinone sulfonamide derivative (PQS) to assess its anticancer activity, following confirmation of its safety in a normal cell line. Results revealed that PQS has a noteworthy cytotoxic effect on HepG-2 and HeLa cells, indicating its potential anticancer activity. Additionally, PQS is quite safe on normal Vero cells. Furthermore, in vivo biological activity of PQS was evaluated for its radioprotective properties in (5 Gy) irradiated mice. PQS showed mitigation of gamma radiation-induced oxidative stress, verified by the decline in MDA, ROS and NO levels, while GSH levels and GST activities were improved in kidney tissues. The apoptotic pathway was also assessed, where weak expression of caspase-3 and Bcl2-associated X protein (Bax) was noticed paired with higher expression of B-cell lymphoma 2 (Bcl2) after PQS treatment in irradiated mice. These results were confirmed by histopathological examination of kidney tissues. Besides, in-silico ADME studies revealed that compound PQS showed drug-like properties, confirmed by its physicochemical and pharmacokinetic properties. In conclusion, the results of the present study demonstrated that PQS has dual activity as a potential anticancer on HepG-2 and HeLa cancer cell lines and radio-protective activity through its anti-apoptotic and antioxidant action in the in vivo study.

Indexed as

Antineoplastic AgentsAntioxidantsKidneyPyrazinesQuinazolinonesRadiation-Protective AgentsSulfonamidesAnimalsApoptosisChlorocebus aethiopsGamma RaysHeLa CellsHep G2 CellsHumansMaleMiceAntineoplastic AgentsAntioxidantsPyrazinesQuinazolinonesRadiation-Protective AgentsReactive Oxygen SpeciesSulfonamidesAntioxidantApoptosisGamma radiationKidney damageQuinazolinoneScavenging

Identifiers

PMID41951844

DOI10.1007/s00210-026-05248-2

PMCPMC13357621

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.