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<p>Quinazolinone derivatives possess a privileged scaffold with variable pharmacological activities. This study conducted an <i>in vitro</i> evaluation of the pyrazine-linked quinazolinone sulfonamide derivative (<b>PQS</b>) to assess its anticancer activity, following confirmation of its safety in a normal cell line. Results revealed that <b>PQS</b> has a noteworthy cytotoxic effect on HepG-2 and HeLa cells, indicating its potential anticancer activity. Additionally, <b>PQS</b> is quite safe on normal Vero cells. Furthermore, <i>in vivo</i> biological activity of <b>PQS</b> was evaluated for its radioprotective properties&#xa0;in (5&#xa0;Gy) irradiated mice. <b>PQS</b> 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 <b>PQS</b> treatment in irradiated mice. These results were confirmed by histopathological examination of kidney tissues. Besides, <i>in-silico</i> ADME studies revealed that compound <b>PQS</b> showed drug-like properties, confirmed by its physicochemical and pharmacokinetic properties. In conclusion, the results of the present study demonstrated that <b>PQS</b> 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 <i>in vivo </i>study.</p>

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

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年4月9日

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

摘要

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.