scholarly journals B-nor-methylene Colchicinoid PT-100 Selectively Induces Apoptosis in Multidrug-Resistant Human Cancer Cells via an Intrinsic Pathway in a Caspase-Independent Manner

ACS Omega ◽  
2022 ◽  
Author(s):  
Andreas Stein ◽  
Persefoni Hilken née Thomopoulou ◽  
Corazon Frias ◽  
Sina M. Hopff ◽  
Paloma Varela ◽  
...  
Oncotarget ◽  
2015 ◽  
Vol 6 (34) ◽  
pp. 36202-36218 ◽  
Author(s):  
Hak-Bong Kim ◽  
Su-Hoon Lee ◽  
Jee-Hyun Um ◽  
Won Keun Oh ◽  
Dong-Wan Kim ◽  
...  

1993 ◽  
Vol 54 (5) ◽  
pp. 851-857 ◽  
Author(s):  
Yuji Heike ◽  
Saburo Sone ◽  
Seiji Yano ◽  
Hiroyuki Seimiya ◽  
Takashi Tsuruo ◽  
...  

Author(s):  
Giusy Fiucci ◽  
Malgorzata Czarny ◽  
Yaakov Lavie ◽  
Di Zhao ◽  
Brygida Berse ◽  
...  

PLoS ONE ◽  
2013 ◽  
Vol 8 (4) ◽  
pp. e60975 ◽  
Author(s):  
Chiara Riganti ◽  
Barbara Castella ◽  
Joanna Kopecka ◽  
Ivana Campia ◽  
Marta Coscia ◽  
...  

2020 ◽  
Vol 13 (9) ◽  
pp. 218
Author(s):  
Yun Soo Jeong ◽  
Thuy Giang Lam ◽  
Seho Jeong ◽  
Sang-Gun Ahn

Multidrug resistance is a significant clinical crisis in cancer treatment and has been linked to the cellular expression of multidrug efflux transporters. The aim of this study was to examine the effects and mechanisms of the metformin derivative HL156A on human multidrug resistance (MDR) cancer cells. Here, HL156A significantly suppressed cell growth and colony formation through G2/M phase cell cycle arrest in MDR cancer cells. HL156A also reduced the wound closure rate and cell migration and induced caspase-3-dependent apoptosis. We found that HL156A inhibited the expression of MDR1 by inhibiting the HOXC6-mediated ERK1/2 signaling pathway and increased the sensitivity to paclitaxel or doxorubicin in MDR cells. Furthermore, HL156A significantly inhibited angiogenesis in a chicken chorioallantoic membrane (CAM) assay. These results suggest the potential of the metformin derivative HL156A as a candidate therapeutic modality for the treatment of human multidrug-resistant cancers.


Molecules ◽  
2019 ◽  
Vol 24 (16) ◽  
pp. 2968 ◽  
Author(s):  
Erjia Wang ◽  
Markus Santhosh Braun ◽  
Michael Wink

Multidrug resistance (MDR) causes challenging tasks in medicine. Human cancer cells, as well as microorganisms, can acquire multiresistance due to the up-regulation of efflux pumps (ABC transporters) and are difficult to treat. Here, we evaluated the effects of chlorophyll, the most abundant pigment on the globe, and its derivative, pheophytin, on cancer cells and methicillin-resistant Staphylococcus aureus (MRSA). We found that both substances have significant reversal effects on multidrug-resistant CEM/ADR5000 cells (RRpheophytin = 3.13, combination index (CI)pheophytin = 0.438; RRchlorophyll = 2.72, CIchlorophyll < 0.407), but not on drug-sensitive CCRF-CEM cells when used in combination with doxorubicin. This indicates that the porphyrins could interact with efflux pumps. Strong synergism was also observed in antimicrobial tests against MRSA when combining ethidium bromide with chlorophyll (FICI = 0.08). As there is a strong need for new drugs in order to reliably treat MDR cells, our research provides potential candidates for further investigation.


2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Mina Park ◽  
Jee Won Hwang ◽  
Yena Cho ◽  
Saegun Kim ◽  
Sang Hoon Han ◽  
...  

AbstractThe success of cancer chemotherapy is limited by multidrug resistance (MDR), which is mainly caused by P-glycoprotein (P-gp) overexpression. In the present study, we describe a novel microtubule inhibitor, 5-(N-methylmaleimid-3-yl)-chromone (SPC-160002), that can be used to overcome MDR. A synthetic chromone derivative, SPC-160002, showed a broad spectrum of anti-proliferative effects on various human cancer cells without affecting P-gp expression and its drug efflux function. Treatment with SPC-160002 arrested the cell cycle at the M phase, as evidenced using fluorescence-activated cell sorting analysis, and increased the levels of mitotic marker proteins, including cyclin B, pS10-H3, and chromosomal passenger complex. This mitotic arrest by SPC-160002 was mediated by promoting and stabilizing microtubule polymerization, similar to the mechanism observed in case of taxane-based drugs. Furthermore, SPC-160002 suppressed the growth and sphere-forming activity of cancer stem cells. Our data herein strongly suggest that SPC-160002, a novel microtubule inhibitor, can be used to overcome MDR and can serve as an attractive candidate for anticancer drugs.


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