The development of new and effective antitumor agents is one of the main goals of medicinal and biochemical research at present. The present study is concerned with the evaluation of the previously synthesized N-Butyl...The development of new and effective antitumor agents is one of the main goals of medicinal and biochemical research at present. The present study is concerned with the evaluation of the previously synthesized N-Butylpyridoquinoxaline 1,4-dioxide (NBPQD) as an antitumor agent against Ehrlich ascites carcinoma (EAC). The first part of the study (tumor imaging) was to investigate the biodistribution of NBPQD in the organs of EAC-bearing mice using iodine-125 isotope stressing on its distribution in the main organs (stomach, liver, spleen, kidney) in addition to blood and ascetic fluid. The second part was the assessment of the antitumor activity of NBPQD by estimating the tumor volume and the contents of total protein, total lipid, DNA and RNA in liver tissues. In addition, liver function tests and the redox status were assessed. Tumor volume and DNA, RNA, urea and malondialdehyde (MDA) levels and the liver enzymes activity were highly significantly increased (P < 0.001) in untreated EAC-bearing mice compared to control. However, total lipid and total protein in liver tissues in addition to serum albumin, glucose, reduced glutathione (GSH) as well as activities of glutathione reductase (GSH-R) and superoxide dismutase (SOD) all were highly significantly decreased in untreated EAC-bearing mice compared to controls. All these decreased parameters were highly significantly restored to their normal levels in NBPQD treated mice compared to the untreated EAC-bearing mice. The survival time of the NBPQD treated mice was longer than that of the untreated ones. It is thus, evident that NBPQD had a remarkable antitumor activity against EAC in Swiss albino mice.展开更多
Chloroquine (CQ) was and still considered as the most common agent in </span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style=&quo...Chloroquine (CQ) was and still considered as the most common agent in </span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">the </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">treatment and prophylaxis of malaria, it also possesses many different pharmacological and biological activities that make it able to be used as a therapy or adjuvant therapy for many types of diseases. CQ exhibits anticancer activity alone or as adjuvants with other agents against many kinds of tumors. Its activities also were approved as </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">an </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">anti-inflammatory agent in rheumatoid and other autoimmune diseases like systemic lupus and rheumatic arthritis. Its</span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">’</span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;"> important role in the improvement of many metabolic disorders like hypertension, hyperglycemia, and lipid profile disturbances was also established. CQ can act against different microbial infections such as many types of virus</span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">es</span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">, bacteria and fungus by different mechanisms of action. Furthermore, its dermatological role in </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">the </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">treatment of many skin diseases was demonstrated. Recently, CQ showed </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">a </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">very responsive role in curing and prevention of </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">the </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">covoid-19 virus. This review summarizes intensively the multiple therapeutic applications of CQ and discusses the possible mechanisms of action for these applications.展开更多
文摘The development of new and effective antitumor agents is one of the main goals of medicinal and biochemical research at present. The present study is concerned with the evaluation of the previously synthesized N-Butylpyridoquinoxaline 1,4-dioxide (NBPQD) as an antitumor agent against Ehrlich ascites carcinoma (EAC). The first part of the study (tumor imaging) was to investigate the biodistribution of NBPQD in the organs of EAC-bearing mice using iodine-125 isotope stressing on its distribution in the main organs (stomach, liver, spleen, kidney) in addition to blood and ascetic fluid. The second part was the assessment of the antitumor activity of NBPQD by estimating the tumor volume and the contents of total protein, total lipid, DNA and RNA in liver tissues. In addition, liver function tests and the redox status were assessed. Tumor volume and DNA, RNA, urea and malondialdehyde (MDA) levels and the liver enzymes activity were highly significantly increased (P < 0.001) in untreated EAC-bearing mice compared to control. However, total lipid and total protein in liver tissues in addition to serum albumin, glucose, reduced glutathione (GSH) as well as activities of glutathione reductase (GSH-R) and superoxide dismutase (SOD) all were highly significantly decreased in untreated EAC-bearing mice compared to controls. All these decreased parameters were highly significantly restored to their normal levels in NBPQD treated mice compared to the untreated EAC-bearing mice. The survival time of the NBPQD treated mice was longer than that of the untreated ones. It is thus, evident that NBPQD had a remarkable antitumor activity against EAC in Swiss albino mice.
文摘Chloroquine (CQ) was and still considered as the most common agent in </span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">the </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">treatment and prophylaxis of malaria, it also possesses many different pharmacological and biological activities that make it able to be used as a therapy or adjuvant therapy for many types of diseases. CQ exhibits anticancer activity alone or as adjuvants with other agents against many kinds of tumors. Its activities also were approved as </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">an </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">anti-inflammatory agent in rheumatoid and other autoimmune diseases like systemic lupus and rheumatic arthritis. Its</span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">’</span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;"> important role in the improvement of many metabolic disorders like hypertension, hyperglycemia, and lipid profile disturbances was also established. CQ can act against different microbial infections such as many types of virus</span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">es</span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">, bacteria and fungus by different mechanisms of action. Furthermore, its dermatological role in </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">the </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">treatment of many skin diseases was demonstrated. Recently, CQ showed </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">a </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">very responsive role in curing and prevention of </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">the </span></span></span><span style="font-family:Verdana;"><span style="font-family:Verdana;"><span style="font-family:Verdana;">covoid-19 virus. This review summarizes intensively the multiple therapeutic applications of CQ and discusses the possible mechanisms of action for these applications.