Prodrug Approach for Increasing Cellular Glutathione Levels

Cacciatore, Ivana; Cornacchia, Catia; Pinnen, Francesco; Mollica, Adriano; Stefano, Antonio Di

doi:10.3390/molecules15031242

Cited by 103 publications

(93 citation statements)

References 130 publications

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“…The absence of a metabolising organ-the liver-in the present in vitro study may explain why NAC did not elevate BuChE and AChE activities in comparison to cysteine. 20 Thus, in clinical situations in which liver function is normal, NAC treatment may still be effective. The results of the present work indicate that therapeutic plasma concentrations of cysteine (or, potentially, NAC) for the treatment of OP poisoning strongly depends on OP plasma concentrations.…”

Section: Discussionmentioning

confidence: 99%

“…deacetylated) by the liver into its active metabolite cysteine and serves as a cysteine donor. 20 The thiol group of cysteine is reactive toward xenobiotics and seems to be responsible for its beneficial effects in poisoning cases. 21 In the present study, the reactivation effect of equimolar concentrations of 2-PAM, NAC and cysteine on dichlorvos-induced BuChE and AChE inhibition was investigated.…”

Section: Discussionmentioning

confidence: 99%

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In Vitro Cysteine Reactivates Organophosphate Insecticide Dichlorvos-Inhibited Human Cholinesterases

Mohammadi

Jalilian

Karimi

et al. 2017

SQUMJ

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Objectives: Organophosphate (OP) pesticides inhibit both red blood cell (RBC) and plasma cholinesterases (ChEs). Oximes, especially pralidoxime (2-PAM), are widely used as antidotes to treat OP poisoning. In addition, N-acetylcysteine (NAC) is sometimes used as an adjuvant antidote. The current study aimed to assess the feasibility of using NAC as a single therapeutic agent for OP poisoning in comparison to in vitro 2-PAM. Methods: This study was carried out at the Razi Drug Research Center of Iran University of Medical Sciences, Tehran, Iran, between April and September 2014. A total of 22 healthy human subjects were recruited and 8 mL citrated blood samples were drawn from each subject. Dichlorvos-inhibited blood samples were separately exposed to low and high doses (final concentrations of 300 and 600 μmol.L-1 , respectively) of 2-PAM, NAC and cysteine. Plasma and RBCs were then separated by centrifugation and their ChE activity was measured using spectrophotometry. Results: Although cysteine-and not NAC-increased the ChE activity of both plasma and RBCs over those of dichlorvos, it did not increase them over those of a high dose of 2-PAM. Conclusion: These results suggest that the direct reactions of 2-PAM and cysteine with dichlorvos and the reactivation of phosphorylated ChEs occurr via an associative stepwise addition-elimination process. High therapeutic blood concentrations of cysteine are needed for the elevation of ChE activity in plasma and RBCs; however, both this agent and NAC may still be effective in the reactivation of plasma and RBC ChEs.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

In Vitro Cysteine Reactivates Organophosphate Insecticide Dichlorvos-Inhibited Human Cholinesterases

Mohammadi

Jalilian

Karimi

et al. 2017

SQUMJ

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“…Reduced glutathione (GSH) is the most abundant cytosolic thiol playing important role in protection of cells against electrophiles-initiated damages [17]. Earlier we have demonstrated that chalcones (open-chain α,β-unsaturated carbonyls) [18] and cyclic chalcone analogues [19,20] possess intrinsic reactivity towards GSH resulting in formation of the expected adducts.…”

Section: Resultsmentioning

confidence: 99%

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2018

MOJBOC

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“…The depletion of glutathione appears to be liable for the generation of lipid peroxide 20 . Reduced glutathione is a extremely sensitive indicator of cell functionality and visibility.…”

Section: Discussionmentioning

confidence: 99%

Anti Inflammatory Effect of Poly Herbal Formulation on Carrageenan Induced Acute Inflammation in Albino Rats

Shobana¹,

John²,

Jothi³

et al. 2018

Int. Res. J. Pharm.

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ABSTARCTInflammation is defined as the local response of living mammalian tissues to injury due to any agent. It is a body defense reaction in order to eliminate or limit the spread of injurious agents as well as to remove the consequent necrosed cells and tissue and it is manifestation of the body's response to tissue damage and infection. Most currently used drugs for the treatment of inflammation-related diseases are the steroidal and nonsteroidal drugs. In addition, these drugs are known to have several adverse effects, and this has encouraged the use of medicinal plants with very little side effects to substitute for this chemical therapeutics. The present study has been undertaken to evaluate the anti inflammatory potentials of poly herbal formulation on carrageenan induced paw enema in albino rats. The polyherbal formulation was prepared from Calendula officinalis L, Lantana camara L. and Desmodium gangeticum Linn. were selected under study and it can be used for the preparation of poly herbal formulation. The anti inflammatory activity was studied by using carrageenan induced paw edema model. The aqueous extracts of polyherbal formulation were administered orally at dose level of 100, 200 and 300mg/kg bw for 28 days. Indomethacin was used as a standard. After the experimental period, the blood and edematous tissue samples were collected for analysing antioxidant and biochemical parameters. The paw thickness, levels of lipid peroxide, interleukin -6, C -reactive protein, total and differential leucocytes count were significantly increased and the superoxide dismutase, reduced glutathione and total protein levels were decreased in the carrageenan induced animals. Administration of poly herbal formulation restored the levels of above parameters near to normal. The present study concludes that poly herbal formulation prepared from Calendula officinalis L, Lantana camara L. and Desmodium gangeticum Linn. has significant anti inflammatory activity against carrageenan induced paw edema in preclinical models.

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Prodrug Approach for Increasing Cellular Glutathione Levels

Cited by 103 publications

References 130 publications

In Vitro Cysteine Reactivates Organophosphate Insecticide Dichlorvos-Inhibited Human Cholinesterases

In Vitro Cysteine Reactivates Organophosphate Insecticide Dichlorvos-Inhibited Human Cholinesterases

Untitled

Anti Inflammatory Effect of Poly Herbal Formulation on Carrageenan Induced Acute Inflammation in Albino Rats

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