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

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. Thi...

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Main Authors: Anwar, Fareeha, Saleem, Uzma, Rehman, Atta Ur, Ahmad, Bashir, Ismail, Tariq, Mirza, Muhammad Usman, Kee, Lee Yean, Abdullah, Iskandar, Ahmad, Sarfraz
Format: Article
Published: American Chemical Society 2021
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QD Chemistry
Online Access:http://eprints.um.edu.my/34145/
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spelling my.um.eprints.341452022-09-05T07:55:22Z http://eprints.um.edu.my/34145/ Toxicological screening of 4-Phenyl-3,4-dihydrobenzoh]quinolin-2(1H)-one: A new potential candidate for Alzheimer's treatment Anwar, Fareeha Saleem, Uzma Rehman, Atta Ur Ahmad, Bashir Ismail, Tariq Mirza, Muhammad Usman Kee, Lee Yean Abdullah, Iskandar Ahmad, Sarfraz QD Chemistry 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. American Chemical Society 2021-04-27 Article PeerReviewed 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 <https://doi.org/10.1021/acsomega.1c00654>. 10.1021/acsomega.1c00654
institution Universiti Malaya
building UM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Malaya
content_source UM Research Repository
url_provider http://eprints.um.edu.my/
topic QD Chemistry
spellingShingle QD Chemistry
Anwar, Fareeha
Saleem, Uzma
Rehman, Atta Ur
Ahmad, Bashir
Ismail, Tariq
Mirza, Muhammad Usman
Kee, Lee Yean
Abdullah, Iskandar
Ahmad, Sarfraz
Toxicological screening of 4-Phenyl-3,4-dihydrobenzoh]quinolin-2(1H)-one: A new potential candidate for Alzheimer's treatment
description 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.
format Article
author Anwar, Fareeha
Saleem, Uzma
Rehman, Atta Ur
Ahmad, Bashir
Ismail, Tariq
Mirza, Muhammad Usman
Kee, Lee Yean
Abdullah, Iskandar
Ahmad, Sarfraz
author_facet Anwar, Fareeha
Saleem, Uzma
Rehman, Atta Ur
Ahmad, Bashir
Ismail, Tariq
Mirza, Muhammad Usman
Kee, Lee Yean
Abdullah, Iskandar
Ahmad, Sarfraz
author_sort Anwar, Fareeha
title Toxicological screening of 4-Phenyl-3,4-dihydrobenzoh]quinolin-2(1H)-one: A new potential candidate for Alzheimer's treatment
title_short Toxicological screening of 4-Phenyl-3,4-dihydrobenzoh]quinolin-2(1H)-one: A new potential candidate for Alzheimer's treatment
title_full Toxicological screening of 4-Phenyl-3,4-dihydrobenzoh]quinolin-2(1H)-one: A new potential candidate for Alzheimer's treatment
title_fullStr Toxicological screening of 4-Phenyl-3,4-dihydrobenzoh]quinolin-2(1H)-one: A new potential candidate for Alzheimer's treatment
title_full_unstemmed Toxicological screening of 4-Phenyl-3,4-dihydrobenzoh]quinolin-2(1H)-one: A new potential candidate for Alzheimer's treatment
title_sort toxicological screening of 4-phenyl-3,4-dihydrobenzoh]quinolin-2(1h)-one: a new potential candidate for alzheimer's treatment
publisher American Chemical Society
publishDate 2021
url http://eprints.um.edu.my/34145/
_version_ 1744649159120519168
score 13.211869

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