Hamed A. Abosharaf, Aliaa Habib, Abdul Aziz Gad, Tarek M. Mohamed
{"title":"Peanut Resveratrol Inhibits COX-2 in Ehrlich Ascites Carcinoma In vivo Model","authors":"Hamed A. Abosharaf, Aliaa Habib, Abdul Aziz Gad, Tarek M. Mohamed","doi":"10.2174/1573408019666230726142647","DOIUrl":null,"url":null,"abstract":"\n\nThe primary goal of researchers interested in the field of oncology continues to be the development of a new anti-cancer medicine with minimal side effects. Due to their minimal toxicity and impressive performance, natural source-mediated anti-cancer treatments are attracting a lot of attention. Objective: The purpose of the current work was to extract and purify resveratrol from local Leguminosae, such as peanut, beans, cowpea, lupine, fava bean, and soybean, and then assess its cyclooxygenase-2 (COX-2) inhibition. The aim was then to evaluate the anticancer potential of extracted resveratrol individually or combined with doxorubicin against Ehrlich ascites carcinoma (EAC) model.\n\n\n\nResveratrol was extracted and purified using a silica gel column. The inhibition study of extracted resveratrol was conducted against COX-2 in vitro. Then, the anti-proliferation impact of resveratrol alone or combined with doxorubicin was evaluated against the previously established EAC model. Apoptotic/anti-apoptotic genes and cell cycle arrest were investigated.\n\n\n\nAfter being extracted from peanuts, resveratrol inhibited COX-2 in vitro competitively with an inhibition constant (Ki) of 0.545 µM, which is extremely close to the theoretically predicted value (0.48 µM) from molecular docking. Further, resveratrol obviously inhibited COX-2 in vivo. Importantly, resveratrol was able to cause apoptosis by upregulating Bax and downregulating the anti-apoptotic gene Bcl-2, either by itself or in combination with doxorubicin. Additionally, resveratrol's ability to stop the cell cycle is evidence of its COX-2-inhibiting antiproliferative properties.\n\n\n\nResveratrol exhibits anticancer potential via inhibition of COX-2, and it could be appropriate for combinational therapy in vivo.\n","PeriodicalId":35405,"journal":{"name":"Current Enzyme Inhibition","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2023-07-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Enzyme Inhibition","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/1573408019666230726142647","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
引用次数: 0
Abstract
The primary goal of researchers interested in the field of oncology continues to be the development of a new anti-cancer medicine with minimal side effects. Due to their minimal toxicity and impressive performance, natural source-mediated anti-cancer treatments are attracting a lot of attention. Objective: The purpose of the current work was to extract and purify resveratrol from local Leguminosae, such as peanut, beans, cowpea, lupine, fava bean, and soybean, and then assess its cyclooxygenase-2 (COX-2) inhibition. The aim was then to evaluate the anticancer potential of extracted resveratrol individually or combined with doxorubicin against Ehrlich ascites carcinoma (EAC) model.
Resveratrol was extracted and purified using a silica gel column. The inhibition study of extracted resveratrol was conducted against COX-2 in vitro. Then, the anti-proliferation impact of resveratrol alone or combined with doxorubicin was evaluated against the previously established EAC model. Apoptotic/anti-apoptotic genes and cell cycle arrest were investigated.
After being extracted from peanuts, resveratrol inhibited COX-2 in vitro competitively with an inhibition constant (Ki) of 0.545 µM, which is extremely close to the theoretically predicted value (0.48 µM) from molecular docking. Further, resveratrol obviously inhibited COX-2 in vivo. Importantly, resveratrol was able to cause apoptosis by upregulating Bax and downregulating the anti-apoptotic gene Bcl-2, either by itself or in combination with doxorubicin. Additionally, resveratrol's ability to stop the cell cycle is evidence of its COX-2-inhibiting antiproliferative properties.
Resveratrol exhibits anticancer potential via inhibition of COX-2, and it could be appropriate for combinational therapy in vivo.
期刊介绍:
Current Enzyme Inhibition aims to publish all the latest and outstanding developments in enzyme inhibition studies with regards to the mechanisms of inhibitory processes of enzymes, recognition of active sites, and the discovery of agonists and antagonists, leading to the design and development of new drugs of significant therapeutic value. Each issue contains a series of timely, in-depth reviews written by leaders in the field, covering a range of enzymes that can be exploited for drug development. Current Enzyme Inhibition is an essential journal for every pharmaceutical and medicinal chemist who wishes to have up-to-date knowledge about each and every development in the study of enzyme inhibition.