scholarly journals AcetylcholinesteraseInhibition by Biofumigant (Coumaran) from Leaves ofLantana camarain Stored Grain and Household Insect Pests

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Yallappa Rajashekar ◽  
Anjanappa Raghavendra ◽  
Nandagopal Bakthavatsalam
Keyword(s):  
Mode Of Action ◽  
Nervous Tissue ◽  
Insect Pests ◽  
Enzyme Inhibitor ◽  
Time Dependent ◽  
Stored Grain ◽  
Acetylthiocholine Iodide ◽  
Dose Dependent ◽  
Ellman's Reagent

Recent studies proved that the biofumigants could be an alternative to chemical fumigants against stored grain insect pests. For this reason, it is necessary to understand the mode of action of biofumigants. In the present study the prospectus of utilisingLantana camaraas a potent fumigant insecticide is being discussed. Inhibition of acetylcholinesterase (AChE) by Coumaran, an active ingredient extracted from the plantL. camara, was studied. The biofumigant was used as an enzyme inhibitor and acetylthiocholine iodide as a substrate along with Ellman’s reagent to carry out the reactions. Thein vivoinhibition was observed in both dose dependent and time dependent in case of housefly, and the nervous tissue (ganglion) and the whole insect homogenate of stored grain insect exposed to Coumaran. The possible mode of action of Coumaran as anacetylcholinesteraseinhibitor is discussed.

3,3′,5′-Triiodothyronine inhibits ontogenetic development of iodothyronine-5′-deiodinase in the liver of the neonatal mouse

1988 ◽  
Vol 119 (2) ◽  
pp. 181-188 ◽  
Author(s):  
Doo Chol Han ◽  
Kanji Sato ◽  
Yuko Fujii ◽  
Minoru Ozawa ◽  
Hidehito Imamura ◽  
...  
Keyword(s):  
Single Injection ◽  
Inhibitory Effect ◽  
Antagonistic Effect ◽  
Time Dependent ◽  
Dependent Manner ◽  
Neonatal Mice ◽  
Dose Dependent Decrease ◽  
Dose Dependent

Abstract. To elucidate the effect of rT3 on iodothyronine-5′-deiodinating activity (I-5′-DA) in the liver of neonatal mice, rT3 was injected sc on the 5–8th day after birth and I-5′-DA in the liver was determined. A single injection of rT3 (0.01–1 μg/g) inhibited the ontogenetically developing I-5′-DA in a dose- and time-dependent manner. The inhibitory effect was reversible and specific for I-5′-DA. Lineweaver-Burk analysis revealed that the time- and dose-dependent decrease in the enzyme activity was due to a decrease in Vmax with no alteration in Km values (5 × 10−8 mol/l). The maximal inhibitory effect was observed at a dose of 1 μg rT3/g, whereas the inhibitory effect was diminished at greater doses (4–10 μg/g), probably owing to a contamination with T4 of the rT3 preparation administered. Furthermore, consistent with our previous in vitro findings, rT3 inhibited the I-5′-DA induced by T3 in the liver of neonatal mice. These findings suggest that rT3 inhibited I-5′-DA in the liver of neonatal mice by decreasing the amount of enzyme available to the substrate and that rT3 also elicited an antagonistic effect against T3 in the induction of I-5′-DA in vivo.

scholarly journals Molecular docking analyses of CYP450 monooxygenases of Tribolium castaneum (Herbst) reveal synergism of quercetin with paraoxon and tetraethyl pyrophosphate: in vivo and in silico studies

2020 ◽  
Vol 9 (3) ◽  
pp. 212-221
Author(s):  
Ammarah Ghaffar ◽  
Sheikh Arslan Sehgal ◽  
Rida Fatima ◽  
Roya Batool ◽  
Ume Aimen ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Tribolium Castaneum ◽  
In Silico ◽  
Insect Pests ◽  
Food Contamination ◽  
Stored Grain ◽  
Residual Toxicity ◽  
Global Issue ◽  
In Silico Studies

Abstract Pest management in stored grain industry is a global issue due to the development of insecticide resistance in stored grain insect pests. Excessive use of insecticides at higher doses poses a serious threat of food contamination and residual toxicity for grain consumers. Since the development of new pesticide incurs heavy costs, identifying an effective synergist can provide a ready and economical tool for controlling resistant pest populations. Therefore, the synergistic property of quercetin with paraoxon and tetraethyl pyrophosphate has been evaluated against the larvae and adults of Tribolium castaneum (Herbst). Comparative molecular docking analyses were carried out to further identify the possible mechanism of synergism. It was observed that quercetin has no insecticidal when applied at the rate of 1.5 and 3.0 mg/g; however, a considerable synergism was observed when applied in combination with paraoxon. The comparative molecular docking analyses of CYP450 monooxygenase (CYP15A1, CYP6BR1, CYP6BK2, CYP6BK3) family were performed with quercetin, paraoxon and tetraethyl pyrophosphate which revealed considerable molecular interactions, predicting the inhibition of CYP450 isoenzyme by all three ligands. The study concludes that quercetin may be an effective synergist for organophosphate pesticides depending upon the dose and type of the compound. In addition, in silico analyses of the structurally diversified organophosphates can effectively differentiate the organophosphates which are synergistic with quercetin.

In Vitro and in Vivo Effect of Sodium Metaarsenite (KML001) in Non-Hodgkin's Lymphoma

Blood ◽  
2012 ◽  
Vol 120 (21) ◽  
pp. 1656-1656
Author(s):  
Jinsun Yoon ◽  
Eun Shil Kim ◽  
Sujung Kim ◽  
Young Lee
Keyword(s):  
Cell Cycle ◽  
Dna Damage ◽  
Malignant Lymphoma ◽  
Cell Lymphoma ◽  
Jurkat Cells ◽  
Time Dependent ◽  
Dependent Manner ◽  
Cycle Arrest ◽  
Dose Dependent

Abstract Abstract 1656 Arsenic trioxide has been used for treatment of hematological malignancies including acute promyelocytic leukemia (APL), multiple myeloma. Sodium metaarsenite (NaAs2O3: code name KML001) is an orally bio-available arsenic compound with potential anti-cancer activity. However, the effect of KML001 has not been well studied in non-Hodgkin's lymphoma. The aim of this study is to determine the anti-tumoral effect of KML001 and to investigate the mechanism of anti-tumoral effect of KML001 in malignant lymphoma. KML001 inhibited the cellular proliferation in all lymphoma cell lines as well as JurkatR cells (adriamycin-resistant Jurkat cells) in a dose-dependent manner with IC50 of 5 × 10−8M. KML001 induced G1 cell cycle arrest which was associated with decreased expression of cyclin B1, cyclin E1, CDK1 (cdc2p34), CDK2, CDK4, and CDK6. KML001- induced p27 was bound to CDK4 and CDK6 in Jurkat cells, and bound to CDK2, CDK4 and CDK6 in JurkatR cells. CDK4 and CDK6 kinase activities were reduced in Jurkat and JurkatR cells. KML001 increased early apoptotic fraction using annexin V-PI staining in a time-dependent manner. In addition, Apoptotic molecules of Bcl-2, Bcl-XL, Mcl-1, proform of caspase-3, caspase-8, and caspase-9 were decreased; in contrast, expressions of PARP active form and Bax, were increased in Jurkat and JurkatR cells treated with KML001 in a dose-dependent manner. In addition, KML001 inhibited the activation of STAT1, 3, 5, NF-κB (p65 and p50 subunits), pAKT, p-mTOR, p-GSK3 ß in a dose-dependent manner, but p-PTEN was up-regulated in KML001-treated Jurkat and JurkatR cells. In MAP kinase signaling, pERK was down regulated, while pp38 and pJNK were increased in a dose-dependent manner. Real-time PCR with RNA extracted from KML001-treated Jurkat and JurkatR cells showed a reduction of catalytic subunit of telomerase, hTERT, in a time- dependent manner. When treated KML001, DNA damage molecule (p-γ-H2AX) was increased in a time-dependent manner, and the telomere length was shorten in Jurkat and JurkatR cells. In vivo anti-tumoral activity of KML001 was confirmed using a xenograft-murine model of human lymphoma cell. Tumor burden was significantly reduced (P < 0.01) for 42 days. Especially, in-vivo anti-tumoral effect of 3.5 mg/Kg KML001 was comparable to that of doxorubicin (2.5 mg/Kg, P < 0.05). Furthermore, three refractory or relapsed malignant lymphoma patients (Diffuse large cell lymphoma, Follicular lymphoma. Mantle cell lymphoma) were treated with 10 mg of KML001 daily, resulting in decrease of lymphoma mass in 4 weeks without severe toxicities. In summary, KML001(sodium metaarsenite) demonstrated anti-tumoral effect via various mechanisms including cell cycle arrest, induction of apoptosis, and inhibition of JAK/STAT, PI3K and MAPK pathways. Especially, KML001 might target telomerase with DNA damage. Furthermore, it is probable that KML001 may overcome the resistance of chemotherapeutic agents. Collectively, KML001 may be a candidate agent for the treatment of de novo, refractory and relapsed malignant lymphoma. Disclosures: No relevant conflicts of interest to declare.

Involvement of 5-Hydroxytryptamine in Platelet Aggregation In Vivo in Rats and Guinea Pigs

1989 ◽  
Vol 61 (03) ◽  
pp. 463-467 ◽  
Author(s):  
G M Smith
Keyword(s):  
Platelet Count ◽  
Guinea Pigs ◽  
Platelet Adhesion ◽  
Adenosine Diphosphate ◽  
Rate Of Return ◽  
Low Doses ◽  
Dose Dependent ◽  
Higher Doses ◽  
Rat Platelets

SummaryIn this study, 5-hydroxytryptamine (5-HT) caused a dose- dependent fall in the circulating platelet count suggesting that 5-HT receptors are activated in rat platelets to cause platelet adhesion and aggregation. When low doses of adenosine diphosphate (ADP) were simultaneously injected with 5-HT, there was a significant potentiation of the responses to ADR Ketanserin significantly reduced the potentiated responses. When higher doses of ADP were infused with bolus injections of 5-HT there was no potentiation and ketanserin did not reduce these responses. Ketanserin did not inhibit the collagen-induced fall in circulating platelet count, but did significantly increase the rate of return to the basal platelet count compared with control. 5-HT did not cause a fall in platelet count in guinea-pigs

Effects of NO-Donors on Thrombus Formation and Microcirculation in Cerebral Vessels of the Rat

1996 ◽  
Vol 76 (01) ◽  
pp. 111-117 ◽  
Author(s):  
Yasuto Sasaki ◽  
Junji Seki ◽  
John C Giddings ◽  
Junichiro Yamamoto
Keyword(s):  
Blood Flow ◽  
Thrombus Formation ◽  
Dependent Manner ◽  
Red Cell ◽  
Cell Velocity ◽  
Red Cell Velocity ◽  
The Mean ◽  
Wall Shear ◽  
Dose Dependent

SummarySodium nitroprusside (SNP) and 3-morpholinosydnonimine (SIN-1), are known to liberate nitric oxide (NO). In this study the effects of SNP and SIN-1 on thrombus formation in rat cerebral arterioles and venules in vivo were assessed using a helium-neon (He-Ne) laser. SNP infused at doses from 10 Μg/kg/h significantly inhibited thrombus formation in a dose dependent manner. This inhibition of thrombus formation was suppressed by methylene blue. SIN-1 at a dose of 100 Μg/kg/h also demonstrated a significant antithrombotic effect. Moreover, treatment with SNP increased vessel diameter in a dose dependent manner and enhanced the mean red cell velocity measured with a fiber-optic laser-Doppler anemometer microscope (FLDAM). Blood flow, calculated from the mean red cell velocity and vessel diameters was increased significantly during infusion. In contrast, mean wall shear rates in the arterioles and venules were not changed by SNP infusion. The results indicated that SNP and SIN-1 possessed potent antithrombotic activities, whilst SNP increased cerebral blood flow without changing wall shear rate. The findings suggest that the NO released by SNP and SIN-1 may be beneficial for the treatment and protection of cerebral infarction

Soluble Thrombomodulin Purified from Human Urine Exhibits a Potent Anticoagulant Effect In Vitro and In Vivo

1995 ◽  
Vol 73 (05) ◽  
pp. 805-811 ◽  
Author(s):  
Yasuo Takahashi ◽  
Yoshitaka Hosaka ◽  
Hiromi Niina ◽  
Katsuaki Nagasawa ◽  
Masaaki Naotsuka ◽  
...  
Keyword(s):  
Human Urine ◽  
Specific Activity ◽  
Anticoagulant Activity ◽  
Rabbit Lung ◽  
Soluble Thrombomodulin ◽  
Molecular Weights ◽  
Dose Dependent Fashion ◽  
Dose Dependent

SummaryWe examined the anticoagulant activity of two major molecules of soluble thrombomodulin purified from human urine. The apparent molecular weights of these urinary thrombomodulins (UTMs) were 72,000 and 79,000, respectively. Both UTMs showed more potent cofactor activity for protein C activation [specific activity >5,000 thrombomodulin units (TMU)/mg] than human placental thrombomodulin (2,180 TMU/mg) and rabbit lung thrombomodulin (1,980 TMU/mg). The UTMs prolonged thrombin-induced fibrinogen clotting time (>1 TMU/ml), APTT (>5 TMU/ml), TT (>5 TMU/ml) and PT (>40 TMU/ml) in a dose-dependent fashion. These effects appeared in the concentration range of soluble thrombomodulins present in human plasma and urine. In the rat DIC model induced by thromboplastin, administration of UTMs by infusion (300-3,000 TMU/kg) restored the hematological abnormalities derived from DIC in a dose-dependent fashion. These results demonstrate that UTMs exhibit potent anticoagulant and antithrombotic activities, and could play a physiologically important role in microcirculation.

Adenosine Diphosphate (ADP)-Induced ⍺-Granules Release from Platelets of Native Whole Blood Is Reduced by Ticlopidine but Not by Aspirin or Dipyridamole

1986 ◽  
Vol 56 (02) ◽  
pp. 147-150 ◽  
Author(s):  
V Pengo ◽  
M Boschello ◽  
A Marzari ◽  
M Baca ◽  
L Schivazappa ◽  
...  
Keyword(s):  
Whole Blood ◽  
Light Transmission ◽  
Ex Vivo ◽  
Early Stage ◽  
Shape Change ◽  
Adenosine Diphosphate ◽  
Dose Dependent ◽  
Plateletderived Growth Factor ◽  
Platelet Shape

SummaryA brief contact between native whole blood and ADP promotes a dose-dependent release of platelet a-granules without a fall in the platelet number. We assessed the “ex vivo” effect of three widely used antiplatelet drugs, aspirin dipyridamole and ticlopidine, on this system. Aspirin (a single 800 mg dose) and dipyridamole (300 mg/die for four days) had no effect, while ticlopidine (500 mg/die for four days) significantly reduced the a-granules release for an ADP stimulation of 0.4 (p <0.02), 1.2 (p <0.01) and 2 pM (p <0.01). No drug, however, completeley inhibits this early stage of platelet activation. The platelet release of α-granules may be related to platelet shape change of the light transmission aggregometer and may be important “in vivo” by enhancing platelet adhesiveness and by liberating the plateletderived growth factor.

Insulinomimetic properties of trace elements and characterization of their in vivo mode of action

Diabetes ◽  
1990 ◽  
Vol 39 (10) ◽  
pp. 1243-1250 ◽  
Author(s):  
L. Rossetti ◽  
A. Giaccari ◽  
E. Klein-Robbenhaar ◽  
L. R. Vogel
Keyword(s):  
Trace Elements ◽  
Mode Of Action
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