Calculation of Lipophilicity of Organophosphate Pesticides Using Density Functional Theory

Магомедов, К. Э.; Zeynalov, R. Z.; Suleymanov, S.I.; Tataeva, S. D.

doi:10.3390/membranes12060632

Cited by 5 publications

(2 citation statements)

References 37 publications

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“…32 A chemical with a higher lipophilicity can pass through lipid cell membranes, the blood-brain barrier, and protein binding. 50 This lipophilic property is predicted to enable temephos to penetrate The values were expressed using mean ± SEM LSD (* = Significantly different at 5% level of significance) -: no damage, +: there is damage the mouth or cuticle and eventually enter the midgut cells. This study is still limited to histological studies.…”

Section: Discussionmentioning

confidence: 99%

Another Mode of Action of Temephos Against Aedes aegypti Larvae: A Stomach Poison Investigation

Adrianto¹,

Subekti²,

Arwati³

et al. 2023

Pharmacogn J.

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Introduction: Aedes aegypti is a key vector for the spread of several severe arboviral infections. The Indonesian Ministry of Health launched Temephos as a national effort to limit the Aedes aegypti larvae population. The old theory has been passed down for generations that the principle of the mechanism of action of temephos as a neurotoxin. The main aim of this study was to investigate the mechanism of action of temephos as a stomach poison by using histopathology study. Method: There are two treatments with three replications: a container containing only 100 ml of water with tween 20 and a container containing 100 ml of water with 1 ppm of temephos 8G. The 20 third-instar Ae. aegypti larvae in containers containing 100 ml of water with 1 ppm of temephos 8G were compared with those in 100 ml of water containing Tween-20. The experiment was done in three replications. The number of dead larvae was recorded after 24 hours of treatment. Histological sections of the larval midgut were prepared and stained with hematoxylin-eosin (HE). Light microscopy was used to examine changes in the length of the midgut lumen and the epithelium. Data were analyzed using a one-way ANOVA. The appearances of the nucleus of the epithelial cell and the degree of damage were qualitatively observed. Results: The results showed that no dead larvae were found in the control group, however, 100% mortality was found in the temephos group. The changes in midgut lumen length and in the epithelium length were significantly different from those in the control group (p<0.05). Nuclei of epithelial cells were lost and midgut cells were damaged in the temephos group. Conclusions: This study reports the first discovery of the mechanism of action of temephos other than a neurotoxin, namely stomach poison.

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Section: Discussionmentioning

confidence: 99%

Another Mode of Action of Temephos Against Aedes aegypti Larvae: A Stomach Poison Investigation

Adrianto¹,

Subekti²,

Arwati³

et al. 2023

Pharmacogn J.

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“…e lipophilicity parameter (log P) is a crucial factor in membrane transport [36,37]. Here, the log P value of DBPP was determined as water-octanol partition coefficients using the shake-flask method.…”

Section: Lipophilicity and Cellular Uptakementioning

confidence: 99%

Synthesis and Antitumor Activity of a GSH Inert Bisphosphonate Platinum (II) Complex

Liu

et al. 2022

Journal of Chemistry

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Osteosarcoma is a highly aggressive neoplasm. Traditional platinum chemotherapeutic agents for osteosarcoma inevitably have acquired drug resistance and serious side effects, which have limited their utility. To slow down the reaction of platinum drugs with glutathione (GSH) is a strategy to overcome the resistance of platinum chemotherapeutic agents. Herein, the unique design of a GSH inert bisphosphonate platinum complex cis-{di(amino)platinum[tetraethyl 2,2-bis(2-pyridinylmethyl)methylidene-1,1-bisphosphonate]} (DBPP) is reported. MTT assay demonstrates that DBPP showed moderate inhibition towards human osteosarcoma cell line U2OS cells. The cytostatic action of DBPP is related to conformational conversion from B-DNA to A-DNA and the unwinding of pUC19 DNA. DBPP could also destroy the tertiary structure of human serum albumin (HSA). Notably, 31P NMR and 1H NMR indicate that DBPP can hardly chelate with GSH, which could overcome the GSH-induced side effects. We envision that this unique design of the platinum complex would open up new ways to overcome GSH-induced resistance.

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Cypermethrin and/or sulfamethoxazole exposure effect on apoptosis and endoplasmic reticulum of grass carp cardiomyocyte

Xing

Bai

et al. 2023

Ecotoxicology and Environmental Safety

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Calculation of Lipophilicity of Organophosphate Pesticides Using Density Functional Theory

Cited by 5 publications

References 37 publications

Another Mode of Action of Temephos Against Aedes aegypti Larvae: A Stomach Poison Investigation

Another Mode of Action of Temephos Against Aedes aegypti Larvae: A Stomach Poison Investigation

Synthesis and Antitumor Activity of a GSH Inert Bisphosphonate Platinum (II) Complex

Cypermethrin and/or sulfamethoxazole exposure effect on apoptosis and endoplasmic reticulum of grass carp cardiomyocyte

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