scholarly journals Molecular Analysis of Murine Leukemia Cell Lines Resistant to 5,10-Dideazatetrahydrofolate Identifies Several Amino Acids Critical to the Function of Folylpolyglutamate Synthetase

2000 ◽  
Vol 275 (34) ◽  
pp. 26599-26606 ◽  
Author(s):  
Rongbao Zhao ◽  
Steven Titus ◽  
Feng Gao ◽  
Richard G. Moran ◽  
I. David Goldman
1999 ◽  
Vol 77 (1-2) ◽  
pp. 47-50 ◽  
Author(s):  
John D. Roberts ◽  
John Peroutka ◽  
G. Beggiolin ◽  
C. Manzotti ◽  
L. Piazzoni ◽  
...  

2021 ◽  
Vol 89 (2) ◽  
pp. 21
Author(s):  
Kartini Hasballah ◽  
Murniana Sarong ◽  
Renzavaldy Rusly ◽  
Herdina Fitria ◽  
Dewi Rara Maida ◽  
...  

Calotropis gigantea has been known to produce bioactive secondary metabolites with antiproliferative activities against cancer cells. Herein, we extracted the secondary metabolites using ethyl acetate from its root bark and further tested its antiproliferative activities against P388 murine leukemia cell lines. The subfractions from the ethyl acetate extract was obtained from Vacuum Liquid Column Chromatography (VLCC), and followed by Gravity Column Chromatography (GCC). The subfraction C2 and D1 were identified to contain triterpenoids and steroids with the most potent cytotoxicity against Brine Shrimp Lethality Test (BSLT). A 3-(4,5-dimethylthiazol-2-yl) -2-5 diphenyl tetrazolium bromide (MTT) assay suggested that ethyl acetate extract has the highest antiproliferative activities against P388 murine leukemia cell lines (IC50 = 21.79 μg/mL), as opposed to subfraction C2 (IC50 = 50.64 µg/mL) and subfraction D1 (IC50 = 49.33 µg/mL). The compound identified in subfraction C2 and D1 are taraxerol acetate and calotropone, respectively. Though taraxerol acetate and calotropone were active in inhibiting the leukemic cell lines, their IC50s were lower than the ethyl acetate extract, which is probably due to the synergism of the secondary metabolites.


1988 ◽  
Vol 12 (9) ◽  
pp. 763-771 ◽  
Author(s):  
Hitoshi Sawada ◽  
Katsuhiko Itoh ◽  
Teruo Kirikae ◽  
Hiroto Sakoda ◽  
Hiroaki Tezuka ◽  
...  

2015 ◽  
Vol 50 (1) ◽  
pp. 33 ◽  
Author(s):  
Sol-Rim Jeon ◽  
Jae-Wook Lee ◽  
Pil-Sang Jang ◽  
Nack-Gyun Chung ◽  
Bin Cho ◽  
...  

Blood ◽  
2004 ◽  
Vol 104 (11) ◽  
pp. 4369-4369
Author(s):  
Freidoun Albertioni ◽  
Gerrit Jansen ◽  
Kambiz Fotoohi ◽  
Yehuda G. Assaraf ◽  
Lilah Rothem ◽  
...  

Abstract Methotrexate (MTX) is one of the leading drugs in the treatment of leukemia, but extensive metabolism to 7-hydroxymethotrexate (7-OHMTX) can limit its therapeutic efficacy. In this study we investigated whether 7-OHMTX itself can provoke antifolate resistance that may further disrupt MTX efficacy. For this purpose we developed resistance to 7-OHMTX as well as MTX in two human leukemia cell lines (CCRF-CEM and MOLT-4) by stepwise exposure to increasing concentrations of 7-OHMTX and MTX. Consequently, both leukemia cell lines displayed marked levels of resistance to 7-OHMTX (>10 fold) and MTX (>75 fold), respectively. The underlying mechanism of resistance in the MTX-exposed cells was a marked decrease (>10-fold) in reduced folate carrier (RFC)-mediated cellular uptake of MTX. This was associated with transcriptional silencing of the RFC gene in MTX-resistant CCRF-CEM cells. In contrast, the molecular basis for the resistance to 7-OHMTX was solely due to a marked decreased (> 95%) in folylpolyglutamate synthetase (FPGS) activity which conferred >100-fold MTX resistance upon a short term exposure to this drug. This is the first demonstration that 7-OHMTX can provoke distinct modalities of antifolate resistance as compared to the parent drug MTX.


1993 ◽  
Vol 53 (3) ◽  
pp. 457-462 ◽  
Author(s):  
T. Miyagi ◽  
J. Ohyashiki ◽  
K. Yamato ◽  
H. P. Koeffler ◽  
I. Miyoshi

2019 ◽  
Vol 35 (1) ◽  
pp. 134-139
Author(s):  
Desi Harneti ◽  
Asep Supriadin ◽  
Rani Maharani ◽  
Nurlelasari Nurlelasari ◽  
Tri Mayanti ◽  
...  

Four dammarane-type triterpenoids, dammardienon (1), aglaiabbreviatin E (2), dammar-20,25-dien-3b,24-diol (3) and dammar-24-en-3b,20-diol (4) were isolated from methanolic extract of the bark of Aglaia glabrata. The structures of all triterpenoids were elucidated by 1D-, 2D-NMR, and comparison with previously reported data. All triterpenoids were applied into in vitro bioassay against P-388 murine leukemia cell. Dammar-24-en-3b,20-diol (4) has cytotoxic activity with IC50 value of 9.45 mM towards P-388 murine leukemia cell lines.


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