scholarly journals Study of Suggested Chemotherapy Agent of bis ((S) -3-methoxycarbamoyl pentanoate) di chloride bis (ethyl amine) platinum (IV))MPP) using DFT

2021 ◽  
Vol 0 (0) ◽  
pp. 0-0
Author(s):  
Nasir Kazim
Author(s):  
Elnaz Asgharkhani ◽  
Aazam Najmafshar ◽  
Mohsen Chiani

This study aims to investigate the effects of different non-ionic surfactants on physicochemical properties of ART niosomes. ART is a natural compound that is used as an antimalarial and chemotherapy agent in medicine. ART has low bioavailability, stability and solubility. In order to solve these problems and enhancing the efficiency of the drug, nanotechnology was used. In the present study, several niosomal formulations of ART prepared using different molar ratios of Span 60 : Tween 60 : PEG-600: ART in PBS. These three formulations were FI (1:1:0.5:0.5), FII (2:1:0.5:0.5) and FIII (1:2:0.5:0.5), respectively. The encapsulation efficiency was measured by HPLC and the drug release was evaluated by dialysis method. The cytotoxicity test was determined by MTT assay. The size, zeta potential and polydispersity index of the vesicles was measured by Zeta Sizer. Stability study was performed within two months. The MTT assay results showed that cytotoxicity effect of these formulations on MCF-7 cell line is better than C6 cell line and the FIII had the best results for both of them. The entrapment efficiencies of the formulations I, II and III were obtained 82.2±1.88%, 75.5±0.92% and 95.5±1.23%, respectively. The results of size, zeta potential and polydispersity index indicated that the size of the vesicles is below 200 nm, their surface charge is about -35 mV and they were monodisperse. Stability and release study indicated that the formulation III has the best stability and release pattern. Therefore, the use of PEGylated niosomal ART can effectively improve its therapeutic index, stability and solubility.


2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Wang Yin ◽  
Dongxi Xiang ◽  
Tao Wang ◽  
Yumei Zhang ◽  
Cuong V. Pham ◽  
...  

AbstractTwo ATP-binding cassette transporters, ABCB1/MDR1 and ABCG2/BCRP, are considered the most critical determinants for chemoresistance in hepatocellular carcinoma. However, their roles in the chemoresistance in liver cancer stem cells remain elusive. Here we explored the role of inhibition of MDR1 or ABCG2 in sensitizing liver cancer stem cells to doxorubicin, the most frequently used chemotherapeutic agent in treating liver cancer. We show that the inhibition of MDR1 or ABCG2 in Huh7 and PLC/PRF/5 cells using either pharmacological inhibitors or RNAi resulted in the elevated level of intracellular concentration of doxorubicin and the accompanied increased apoptosis as determined by confocal microscopy, high-performance liquid chromatography, flow cytometry, and annexin V assay. Notably, the inhibition of MDR1 or ABCG2 led to the reversal of the chemoresistance, as evident from the enhanced death of the chemoresistant liver cancer stem cells in tumorsphere-forming assays. Thus, the elevation of effective intracellular concentration of doxorubicin via the inhibition of MDR1 or ABCG2 represents a promising future strategy that transforms doxorubicin from a traditional chemotherapy agent into a robust killer of liver cancer stem cells for patients undergoing transarterial chemoembolization.


Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3532
Author(s):  
Ibrahim M. El-Deeb ◽  
Valeria Pittala ◽  
Diab Eltayeb ◽  
Khaled Greish

Triple-negative breast cancer (TNBC) is a heterogeneous subtype of tumors that tests negative for estrogen receptors, progesterone receptors, and excess HER2 protein. The mainstay of treatment remains chemotherapy, but the therapeutic outcome remains inadequate. This paper investigates the potential of a duocarmycin derivative, tafuramycin A (TFA), as a new and more effective chemotherapy agent in TNBC treatment. To this extent, we optimized the chemical synthesis of TFA, and we encapsulated TFA in a micellar system to reduce side effects and increase tumor accumulation. In vitro and in vivo studies suggest that both TFA and SMA–TFA possess high anticancer effects in TNBC models. Finally, the encapsulation of TFA offered a preferential avenue to tumor accumulation by increasing its concentration at the tumor tissues by around four times in comparison with the free drug. Overall, the results provide a new potential strategy useful for TNBC treatment.


1988 ◽  
Vol 37 (15) ◽  
pp. 2979-2985 ◽  
Author(s):  
Alistair J. Benson ◽  
Carl N. Martin ◽  
R.Colin Garner
Keyword(s):  

2007 ◽  
Vol 6 (3-4) ◽  
pp. 155-168 ◽  
Author(s):  
Deborah C. Bebout ◽  
Wei Lai ◽  
Sarah M. Stamps ◽  
Steven M. Berry ◽  
Raymond J. Butcher

2017 ◽  
Vol 15 (14) ◽  
pp. 3046-3059 ◽  
Author(s):  
Trieu N. Trinh ◽  
Eileen A. McLaughlin ◽  
Christopher P. Gordon ◽  
Ilana R. Bernstein ◽  
Victoria J. Pye ◽  
...  

Leveraging our quinolone-1-(2H)-one based Hedgehog signalling pathway (HSP) inhibitors we have developed two new classes of HSP inhibitors based on: l-tryptophan and benzo[1,3]dioxol-5-ylmethyl-[2-(1H-indol-3-yl)-ethyl]-amine.


2018 ◽  
Vol 14 (8) ◽  
pp. 1430-1447 ◽  
Author(s):  
Jing Xin ◽  
Sijia Wang ◽  
Jing Wang ◽  
Jiazhuang Wang ◽  
Lei Fu ◽  
...  

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