Investigation for anticancer activity of the newly synthesized p -Methoxyphenyl maleanilic acid and the diagnostic property of its 99m Tc-analogue

• Published in: International journal of radiation biology p. 1
• Main Authors: Farrag, Nourihan S, Khater, S I, Hassan, Fatma S M, Amin, Abeer M
• Format: Journal Article
• Language: English
• Published: England 07-03-2022
• Subjects: biodistribution; cancer monitoring; p-methoxyphenyl maleanilic acid; docking study; 99mTc-radiolabeling; cytotoxicity
• ISSN: 1362-3095

The limitations of the current chemotherapeutics are the main rational to develop and/or explore new anticancer agents and radiolabeled analogues for cancer early diagnosis.
The newly synthesized
-methoxyphenyl maleanilic acid (MPMA) was prepared, characterized and investigated for its anticancer activity. MPMA screened
against human hepatocellular carcinoma (HepG-2), human colon carcinoma (HCT-116) and human breast carcinoma (MCF-7) cell lines. Furthermore, the
screening was performed by radiolabeling of MPMA with technetium-99m (
Tc) and investigating its biological distribution in normal mice and solid tumor models. Moreover, MPMA and its radiolabeled analogue were docked to Y220C and Y220S mutants of p53 (p53
and p53
) in an effort to confirm their affinity to cancer as well as to investigate, virtually, the mechanism of action of MPMA.
The results revealed significant potency of MPMA against HepG-2 cell line (IC
= 56.2 ± 1.5 µg/mL) if compared to HCT-116 (IC
= 89.9 ± 1.8 µg/mL) and MCF-7 (IC
= 104 ± 2.7 µg/mL) cell lines. The radiolabeling yield was optimized to be 90.2 ± 2.1%. The radiolabeled MPMA showed a good localization in the site of solid tumor (15.1 ± 1.6%ID/g) at 2 h post intravenous administration to the tumor bearing mice.
Collectively, the findings confirmed the potential anticancer activity of MPMA and the possible use of
Tc-MPMA for cancer diagnosis and monitoring.