Acute Toxicity of Several Organophosphorous Insecticides and Protection by Cholinergic Antagonists and 2-PAM on Artemia salina Larvae

Sánchez-Fortún, S.; Sanz, Marta

doi:10.1007/s002449900123

Cited by 4 publications

(9 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Thus, these data suggest that the functional group oxime is crucial for the effectiveness of these compounds against the mortality induced by malathion. In agreement with this, Sánchez‐Fórtun et al demonstrated that the lethal action of OPs is completely prevented by the pre‐treatment of A salina with the oxime 2‐pyridine aldoxime methochloride (2‐PAM), and this result has been confirmed afterwards by Barahona and Sánchez‐Fórtun and Sánchez‐Fórtun and Barahona …”

Section: Discussionsupporting

confidence: 52%

“…However, the validity of using A salina as a screen has not been fully established for oxime‐type compounds, so there may not be a direct correlation of the toxicological or pharmacological effects of oximes among A salina and other species. Importantly, AChE activity assessment is widely used as a biomarker of OP poisoning in the A salina model and these assays were critical to identify the ideal oxime and test in rats, respecting the principle of the 3Rs of vertebrates.…”

Section: Discussionmentioning

confidence: 99%

“…In another series of experiments to determine the synergic effect of atropine and PHBO or Cℓ‐HIN or Cℓ‐OXHS, groups of ten 24‐hour‐old A salina were incubated with malathion (30 µmol/L) and atropine (1 and 10 µmol/L), and different concentrations of each compound (0.01 and 1 µmol/L) or vehicle were immediately added (5‐6 independent experiments). Concentrations of atropine were based on the previous results of Sánchez‐Fortún and Barahona . Survival rate was assessed 24 hours later.…”

Section: Methodsmentioning

confidence: 99%

“…Several studies have evaluated the toxicity of OP as well as the protective effects of atropine and oximes in Artemia salina as a convenient alternative to toxicity screening . Moreover, this biological model has been chosen as the testing organism considering its availability, short life cycle, high adaptability to varied nutrient resources, low cost and low variability in the population. In fact, estimation of the medium lethal dose in A salina uses a bioassay for preliminary assessment in toxicology and pharmaceutical studies by following the 3Rs policy (reduction, refinement and replacement) …”

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Pre‐clinical evidence of safety and protective effect of isatin and oxime derivatives against malathion‐induced toxicity

Savall

Fidélis

Gutierrez

et al. 2019

Basic Clin Pharma Tox

View full text Add to dashboard Cite

The inhibition of acetylcholinesterase (AChE) is a common outcome caused by organophosphorus (OPs) intoxication. Although inconsistent, the standard treatment consists of a muscarinic receptor antagonist (atropine) and AChE‐reactivating molecules such as oximes. This study proposes to test unpublished compounds which contain the moieties of isatin and/or oxime have protective effects against the toxicity induced by malathion in two animal models: Artemia salina and Rattus norvegicus (Wistar rats). The lethality was assessed in A salina, and the calculated LD50 to (3Z)‐5‐chloro‐3‐(hydroxyimino) indolin‐2‐one oxime (Cℓ‐HIN) and 2‐(5‐chloro‐2‐oxoindolin‐3‐ylidene)‐hydrazinecarbothioamide (Cℓ‐OXHS) was higher than 1000 µM while to 3‐(phenylhydrazono) butan‐2‐one oxime (PHBO) was 38 µM. Our screening showed that Cℓ‐HIN seems to be the most promising molecule, with low toxicity to A salina, protection against mortality (with or without atropine) and AChE inhibition induced by malathion. Similarly, the oral administration of 300 mg/kg of Cℓ‐HIN induced low or no toxicity in rats. The plasma butyrylcholinesterase (BChE) and cortical AChE activities were reactivated by Cℓ‐HIN (50 mg/kg, p.o.) in rats exposed to malathion (250 mg/kg, i.p). No difference was observed in paraoxonase‐1 (PON‐1) activity among groups treated. In conclusion, Cℓ‐HIN restored the cholinesterase activities inhibited by malathion in A salina and rats with low toxicity in both. Thus, the data provide evidence that Cℓ‐HIN, a compound that combines isatin and oxime functional groups, is safe and has important properties to reactivate the cholinesterases inhibited by malathion. In addition, we demonstrate the importance of a preliminary assessment in an alternative model in order to reduce the use of mammalians in drug discovery.

show abstract

Section: Discussionsupporting

confidence: 52%

Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Pre‐clinical evidence of safety and protective effect of isatin and oxime derivatives against malathion‐induced toxicity

Savall

Fidélis

Gutierrez

et al. 2019

Basic Clin Pharma Tox

View full text Add to dashboard Cite

show abstract

“…It has been shown that Artemia is highly vulnerable to toxins at the early developmental stages [12,13]. In contrast, in the brine shrimp lethality test, maximum sensibility was reached after 48 h of exposure (the oldest age class tested by us) [14]. At this stage in their life cycle the nauplii have reached their second and third instar and exhibit their greatest sensitivity to test compounds [15].…”

Section: Resultsmentioning

confidence: 99%

Untitled

Carballo¹,

Hernández-Inda²,

Pérez³

et al. 2002

BMC Biotechnol

270

View full text Add to dashboard Cite

Background: The brine shrimp lethality assay is considered a useful tool for preliminary assessment of toxicity. It has also been suggested for screening pharmacological activities in plant extracts. However, we think that it is necessary to evaluate the suitability of the brine shrimp methods before they are used as a general bio-assay to test natural marine products for pharmacological activity.

show abstract

The use of carbamates, atropine, and 2‐pyridine aldoxime methoiodide in the protection of Artemia salina against poisoning by carbophenothion

Sánchez-Fortún

Barahona

2001

Enviro Toxic and Chemistry

View full text Add to dashboard Cite

The acute toxicity of carbophenothion to three age classes of Artemia salina was evaluated. An increase in toxicity of carbophenothion was found following longer development of A. salina. The effect of pretreatment with the nonselective muscarinic antagonist atropine, the two reversible acetylcholinesterase-inhibitors physostigmine and pyridostigmine, and the cholinesterase-reactivating oxime 2-pyridine aldoxime methochloride (2-PAM) on carbophenothion-induced lethality in 24-h-old A. salina was also investigated. The lethal action of carbophenothion was completely prevented by pretreatment of A. salina with 2-PAM. Atropine and pyridostigmine afforded a maximal protection of approximately 87% and 72%, respectively, compared to control values. In contrast, physostigmine was ineffective. The inhibitory effects of combinations of 10(-5) M atropine with physostigmine, pyridostigmine, or 2-PAM were greater than those elicited by either drug alone, with the maximum protection afforded being 92.58%, 100%, and 100%, respectively. In the presence of 10(-7) M atropine, neither pyridostigmine nor 2-PAM provided additional inhibition of the lethality compared to that with either drug alone, whereas the protection afforded by 10(-7) M atropine plus physostigmine increased as the concentration of carbamate increased (up to 10(-3) M). Pretreatment with pyridostigmine or physostigmine plus 2-PAM (10(-6) M) slightly enhanced the maximal inhibition of carbophenothion lethality compared to that with either drug alone. It is suggested that the most active combined pretreatment studied here was physostigmine plus atropine.

show abstract

Acute Toxicity of Several Organophosphorous Insecticides and Protection by Cholinergic Antagonists and 2-PAM on Artemia salina Larvae

Cited by 4 publications

References 0 publications

Pre‐clinical evidence of safety and protective effect of isatin and oxime derivatives against malathion‐induced toxicity

Pre‐clinical evidence of safety and protective effect of isatin and oxime derivatives against malathion‐induced toxicity

Untitled

The use of carbamates, atropine, and 2‐pyridine aldoxime methoiodide in the protection of Artemia salina against poisoning by carbophenothion

Contact Info

Product

Resources

About