Toxicological screening of 4-Phenyl-3,4-dihydrobenzoh]quinolin-2(1H)-one: A new potential candidate for Alzheimer's treatment

Anwar, Fareeha and Saleem, Uzma and Rehman, Atta Ur and Ahmad, Bashir and Ismail, Tariq and Mirza, Muhammad Usman and Kee, Lee Yean and Abdullah, Iskandar and Ahmad, Sarfraz (2021) Toxicological screening of 4-Phenyl-3,4-dihydrobenzoh]quinolin-2(1H)-one: A new potential candidate for Alzheimer's treatment. ACS Omega, 6 (16). pp. 10897-10909. ISSN 2470-1343, DOI https://doi.org/10.1021/acsomega.1c00654.

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Abstract

Toxicity studies are necessary for the development of a new drug. Naphthalene is a bicyclic molecule and is easy to derivatize. In our previous study, a derivative of naphthalene (4-phenyl,3,4-dihydrobenzoquinoline-2(H)one) was synthesized and reported its in vitro activity on different enzymes. This study was a probe to investigate the toxicity potential of that compound (SF3). Acute oral (425), subacute (407), and teratogenicity (414) studies were planned according to their respective guidelines given by organization of economic cooperation and development (OECD). Acute oral, subacute, and teratogenicity studies were carried out on 2000, 5-40, and 40 mg/kg doses. Blood samples were collected for hematological and biochemical analyses. Vital organs were excised for oxidative stress (superoxide dismutase, catalase, glutathione, and malondialdehyde) and histopathological analysis. LD50 of SF3 was higher than 2000 mg/kg. In acute and subacute studies, levels of alkaline phosphates and aspartate transaminase were increased. Teratogenicity showed no resorptions, no skeletal or soft tissue abnormalities, and no cleft pallet. Oxidative stress biomarkers were close to the normal, and no increase in the malondialdehyde level was seen. Histopathological studies revealed normal tissue architecture of the selected organs, except kidney, in acute oral and subacute toxicity studies at 40 mg/kg. The study concluded that SF3 is safer if used as a drug.

Item Type: Article
Funders: Malaya University (IIRG003A-2019)
Uncontrolled Keywords: Toxicological Screening; 4-Phenyl-3,4-dihydrobenzo[h]quinolin-2(1H)-one; Alzheimer's treatment
Subjects: Q Science > QD Chemistry
Divisions: Faculty of Science > Department of Chemistry
Depositing User: Ms Zaharah Ramly
Date Deposited: 05 Sep 2022 07:55
Last Modified: 05 Sep 2022 07:55
URI: http://eprints.um.edu.my/id/eprint/34145

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