scholarly journals Reduction of the Double Bond of 6-Arylvinyl-1,2,4-trioxanes Leads to a Remarkable Increase in Their Antimalarial Activity against Multidrug-Resistant Plasmodium yoelii nigeriensis in a Swiss Mice Model

ACS Omega ◽  
2021 ◽  
Author(s):  
Mohammad Hassam ◽  
Ajit Shankar Singh ◽  
Dinesh Kumar Yadav ◽  
Chandan Singh ◽  
Sunil K. Puri ◽  
...  
Keyword(s):  
Double Bond ◽  
Antimalarial Activity ◽  
Multidrug Resistant ◽  
Plasmodium Yoelii ◽  
Mice Model ◽  
Remarkable Increase ◽  
Swiss Mice

Plasmodium yoelii nigeriensis (MDR)—Efficacy of Oral Pyronaridine against Multidrug-Resistant Malaria in Swiss Mice

2000 ◽  
Vol 94 (3) ◽  
pp. 190-193 ◽  
Author(s):  
Renu Tripathi ◽  
Aseem Umesh ◽  
Meenu Mishra ◽  
S.K. Puri ◽  
G.P. Dutta
Keyword(s):  
Multidrug Resistant ◽  
Plasmodium Yoelii ◽  
Swiss Mice

Pyrrolidine-Acridine hybrid in Artemisinin-based combination: a pharmacodynamic study

Parasitology ◽  
2016 ◽  
Vol 143 (11) ◽  
pp. 1421-1432 ◽  
Author(s):  
SWAROOP KUMAR PANDEY ◽  
SUBHASISH BISWAS ◽  
SARIKA GUNJAN ◽  
BHAVANA SINGH CHAUHAN ◽  
SUNIL KUMAR SINGH ◽  
...  
Keyword(s):  
Malaria Parasite ◽  
Lethal Dose ◽  
Parasite Clearance ◽  
Multidrug Resistant ◽  
Mice Model ◽  
Artemisinin Derivatives ◽  
Swiss Mice ◽  
Function Test

SUMMARYAiming to develop new artemisinin-based combination therapy (ACT) for malaria, antimalarial effect of a new series of pyrrolidine-acridine hybrid in combination with artemisinin derivatives was investigated. Synthesis, antimalarial and cytotoxic evaluation of a series of hybrid of 2-(3-(substitutedbenzyl)pyrrolidin-1-yl)alkanamines and acridine were performed and mode of action of the lead compound was investigated. In vivo pharmacodynamic properties (parasite clearance time, parasite reduction ratio, dose and regimen determination) against multidrug resistant (MDR) rodent malaria parasite and toxicological parameters (median lethal dose, liver function test, kidney function test) were also investigated. 6-Chloro-N-(4-(3-(3,4-dimethoxybenzyl)pyrrolidin-1-yl)butyl)-2-methoxyacridin-9-amine (15c) has shown a dose dependent haem bio-mineralization inhibition and was found to be the most effective and safe compound against MDR malaria parasite in Swiss mice model. It displayed best antimalarial potential with artemether (AM) in vitro as well as in vivo. The combination also showed favourable pharmacodynamic properties and therapeutic response in mice with established MDR malaria infection and all mice were cured at the determined doses. The combination did not show toxicity at the doses administered to the Swiss mice. Taken together, our findings suggest that compound 15c is a potential partner with AM for the ACT and could be explored for further development.

Synthesis and antimalarial activity of novel bicyclic and tricyclic aza-peroxides

RSC Advances ◽  
2016 ◽  
Vol 6 (28) ◽  
pp. 23718-23725 ◽  
Author(s):  
Lalit Yadav ◽  
Mohit K. Tiwari ◽  
Bharti Rajesh Kumar Shyamlal ◽  
Manas Mathur ◽  
Ajit K. Swami ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Antimalarial Activity ◽  
Oral Route ◽  
Plasmodium Yoelii ◽  
Swiss Mice

Bicyclic and tricyclic aza-peroxides were synthesized and assessed for theirin vitroandin vivoantimalarial activities againstPlasmodium falciparum(3D7 strain) andPlasmodium yoelii nigeriensisin Swiss mice by an oral route, respectively.

scholarly journals Immune responses in liver and spleen against Plasmodium yoelii pre-erythrocytic stages in Swiss mice model

2020 ◽  
Vol 24 ◽  
pp. 29-41 ◽  
Author(s):  
Arif Jamal Siddiqui ◽  
Jyoti Bhardwaj ◽  
Manish Goyal ◽  
Kirtika Prakash ◽  
Mohd Adnan ◽  
...  
Keyword(s):  
Immune Responses ◽  
Plasmodium Yoelii ◽  
Mice Model ◽  
Swiss Mice

6-(4′-Aryloxy-phenyl)vinyl-1,2,4-trioxanes: A new series of orally active peroxides effective against multidrug-resistant Plasmodium yoelii in Swiss mice

2010 ◽  
Vol 20 (15) ◽  
pp. 4459-4463 ◽  
Author(s):  
Chandan Singh ◽  
Ved Prakash Verma ◽  
Niraj Krishna Naikade ◽  
Ajit Shankar Singh ◽  
Mohammad Hassam ◽  
...  
Keyword(s):  
Multidrug Resistant ◽  
Plasmodium Yoelii ◽  
Swiss Mice ◽  
Orally Active ◽  
Phenyl Vinyl

Poly ICLC Enhances the Antimalarial Activity of Chloroquine Against Multidrug-Resistant Plasmodium yoelii nigeriensis in Mice

1997 ◽  
Vol 17 (7) ◽  
pp. 419-423 ◽  
Author(s):  
A AWASTHI ◽  
S. MEHROTRA ◽  
V. BHAKUNI ◽  
G.P. DUTTA ◽  
H.B. LEVY ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Multidrug Resistant ◽  
Plasmodium Yoelii

scholarly journals Overcoming multidrug-resistance in vitro and in vivo using the novel P-glycoprotein inhibitor 1416

2012 ◽  
Vol 32 (6) ◽  
pp. 559-566 ◽  
Author(s):  
Yan Xu ◽  
Feng Zhi ◽  
Guangming Xu ◽  
Xiaolei Tang ◽  
Sheng Lu ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Cancer Chemotherapy ◽  
Antitumour Activity ◽  
Multidrug Resistant ◽  
The Novel ◽  
Mice Model ◽  
P Glycoprotein ◽  
Channel Currents

MDR (multidrug-resistance) represents a major obstacle to successful cancer chemotherapy and is usually accomplished by overexpression of P-gp (P-glycoprotein). Much effort has been devoted to developing P-gp inhibitors to modulate MDR. However, none of the inhibitors on the market have been successful. 1416 [1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane hydrochloride (phenoprolamine hydrochloride)] is a new VER (verapamil) analogue with a higher IC50 for blocking calcium channel currents than VER. In the present paper, we examined the inhibition effect of 1416 on P-gp both in vitro and in vivo. 1416 significantly enhanced cytotoxicity of VBL (vinblastine) in P-gp-overexpressed human multidrug-resistant K562/ADM (adriamycin) and KBV cells, but had no such effect on the parent K562 and KB cells. The MDR-modulating function of 1416 was further confirmed by increasing intracellular Rh123 (rhodanmine123) content in MDR cells. Human K562/ADM xenograft-nude mice model verified that 1416 potentiates the antitumour activity of VBL in vivo. RT-PCR (reverse transcriptase-PCR) and FACS analysis demonstrated that the expression of MDR1/P-gp was not affected by 1416 treatment. All these observations suggest that 1416 could be a promising agent for overcoming MDR in cancer chemotherapy.

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