Synthesis of l-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as potential prodrug of l-dopa

Cingolani, Gian Mario; Stefano, Antonio Di; Mosciatti, Barbara; Napolitani, F.; Giorgioni, Gianfabio; Ricciutelli, Massimo; Claudi, Francesco

doi:10.1016/s0960-894x(00)00249-3

Cited by 38 publications

(22 citation statements)

References 11 publications

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“…It acts as antioxidant, free radical scavenger and anti-lipid peroxidative agent (Elhabazi et al 2006;Beena and Rawat 2013;Aydin et al 2014). Natural antioxidants or antioxidant featured synthetic compounds have been found to protect various organs from oxidative injuries (Cingolani et al 2000;Cacciatore et al 2003;Rispoli et al 2004).…”

Section: Introductionmentioning

confidence: 99%

The carvacrol ameliorates acute pancreatitis-induced liver injury via antioxidant response

et al. 2015

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Acute pancreatitis (AP) may cause significant persistent multi-organ dysfunction. Carvacrol (CAR) possesses a variety of biological and pharmacological properties. The aim of the present study was to analyze the hepatic protection of CAR on AP induced by cerulein and to explore the underlying mechanism using in vivo studies. The rats were randomized into groups to receive (1) no therapy; (2) 50 lg/kg cerulein at 1-h intervals by four intraperitoneal injection (i.p.); (3) 50, 100 and 200 mg/kg CAR by one i.p.; and (4) cerulein ? CAR after 2 h of cerulein injection. 12 h later, serum was provided to assess the blood AST, ALT and LDH values. Also, liver tissues were obtained for histological and biochemical measurements. Liver oxidative stress markers were evaluated by changes in the amount of lipid peroxides measured as MDA and changes in tissue antioxidant enzyme levels, SOD, CAT and GSHPx. Histopathological examination was performed using scoring systems. Oxidative damage to DNA was quantitated in studied tissues of experimental animals by measuring the increase in 8-hydroxydeoxyguanosine (8-OHdG) formations. We found that the increasing doses of CAR decreased pancreatitisinduced MDA and 8-OH-dG levels. Moreover, the liver SOD, CAT and GSH-Px activities in the AP ? CAR group were higher than that of the rats in the AP group. In the treatment groups, AST, ALT and LDH were reduced. Besides, necrosis, coagulation and inflammation in the liver were alleviated (p \ 0.05). We suggest that CAR could be a safe and potent new drug candidate for treating AP through its antioxidative mechanism of action for the treatment of a wide range of disorders related to hepatic dysfunction.

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Section: Introductionmentioning

confidence: 99%

The carvacrol ameliorates acute pancreatitis-induced liver injury via antioxidant response

et al. 2015

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“…The exploratory investigations of new natural or synthetic antioxidants becomes a very popular in the world since the last 20 years (Geyikoglu and Turkez 2008); in addition, many efforts have been performed to explore novel antioxidant-natured compounds (Cingolani et al 2000;Cacciatore et al 2003Cacciatore et al , 2005Rispoli et al 2004;Turkez and Sisman 2007;Heuking et al 2009;Turkez and Dirican 2012). At this point, especially, in recent decades plant essential oils (EOs) and their components have attracted increased interest and consequently have been extensively investigated mainly in in vitro and in vivo systems (Turkez et al 2012a).…”

Section: Introductionmentioning

confidence: 99%

Carvacrol modulates oxidative stress and decreases cell injury in pancreas of rats with acute pancreatitis

et al. 2015

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Acute pancreatitis (AP) is considered as major problem around the world and the incidence of AP is increasing. Carvacrol (CAR), a monoterpenic phenol, has good antioxidant activity. This in vivo study was designed to evaluate whether CAR provide protection against AP that developed by pancreas injury. The rats were randomised into groups to receive (I) no therapy; (II) 50 lg/kg cerulein at 1 h intervals by four intraperitonally (i.p.) injections; (III) 50, 100 and 200 mg/kg CAR by one i.p. injection; and (IV) cerulein plus CAR after 2 h of cerulein administration. 12 h later, serum samples were obtained to assess pancreatic function, the lipase and amylase values. The oxidative stress markers were evaluated by changes in the amount of lipid peroxides measured as malondialdehyde (MDA) and changes in main tissue antioxidant enzyme levels including SOD, CAT and GSH-PX. Histopathological examination was performed using scoring systems. Additionally, oxidative DNA damage was determined by measuring the increases of 8-hydroxy-deoxyguanosine (8-OH-dG) formations. We found that the increasing doses of CAR decreased AP-induced MDA and 8-OH-dG levels. Moreover, the pancreas antioxidant enzyme activities were higher than that of the rats in the AP group when compared to the AP plus CAR group. In the treatment groups, the lipase and amylase were reduced. Besides, histopathological findings in the pancreatic tissue were alleviated (p \ 0.05). We suggest that CAR could be a safe and potent new drug candidate for treating AP through its antioxidative mechanism of action for the treatment of a wide range of disorders related to pancreas.

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“…The exploring of novel natural or synthetic antioxidants becomes a very popular research area in the World since the last 20 years ; in addition, many efforts have been performed to explore new antioxidantfeatured compounds (Cingolani et al 2000;Cacciatore et al 2003Cacciatore et al , 2005Rispoli et al 2004;Turkez and Sisman 2007;Heuking et al 2009;Di Stefano et al 2009a, b;Sozio et al 2010;Turkez et al 2012b). Newly, scientists and researchers are interested in the medical application of boron compounds.…”

Section: Introductionmentioning

confidence: 99%

Cytogenetic and oxidative alterations after exposure of cultured human whole blood cells to lithium metaborate dehydrate

et al. 2015

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Boron compounds have an ability of supporting antioxidant properties in human and animal tissues. Lithium metaborate dihydrate (LiBO 2-2H 2 O; LMD) is commonly used in nonlinear optic materials, cellular phones and pagers. But, there are limited data on the genotoxic and antioxidant effects of LMD in cultured human whole blood cells. The aim of this study was to evaluate for the genotoxicity and antioxidant/oxidant activity of LMD on human whole blood lymphocytes (n = 5). LMD was applied at various concentrations (0-1,280 lg/ml) to cultured blood samples. Antioxidant/oxidant activity was evaluated by measuring the total oxidant status (TOS) and total antioxidant capacity levels. Micronuclei and chromosomal aberration tests were used in genotoxicity studies. Our results clearly revealed that all tested concentrations of LMD were found to be non-genotoxic when compared to that of the control group. In addition, LMD exhibited antioxidant activities at low concentrations. In addition the TOS levels were not changed at all concentrations of LMD. Consequently, our results clearly demonstrated that LMD is non-genotoxic and it has an important antioxidant potential in vitro.

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Synthesis of l-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as potential prodrug of l-dopa

Cited by 38 publications

References 11 publications

The carvacrol ameliorates acute pancreatitis-induced liver injury via antioxidant response

The carvacrol ameliorates acute pancreatitis-induced liver injury via antioxidant response

Carvacrol modulates oxidative stress and decreases cell injury in pancreas of rats with acute pancreatitis

Cytogenetic and oxidative alterations after exposure of cultured human whole blood cells to lithium metaborate dehydrate

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