In vitro anti-tumor effect of methotrexate modified by peptide / 药学学报
Acta Pharmaceutica Sinica
;
(12): 452-458, 2012.
Article
in Chinese
| WPRIM
| ID: wpr-323020
ABSTRACT
This study is to investigate the anti-tumor effect in vitro of methotrexate modified by LH-RH peptide (LH-RH-MTX). LH-RH receptors highly expressing MCF-7 human breast carcinoma cell line and lowly expressing K562 human erythroleukemia cell line were served as the tested cells. The cell proliferation inhibition rates of LH-RH-MTX were detected by MTT colorimetric assay. The effects of LH-RH-MTX on the cell cycle and apoptosis rates were detected by flow cytometry. The inhibition rate of LH-RH-MTX on MCF-7 cells was much higher than that on K562 cells, and the inhibition rate of LH-RH-MTX on MCF-7 cells was much higher than that of free MTX at the same concentration. The inhibition rate of LH-RH-MTX on rat bone marrow mononuclear cells was less than that of free MTX. The number of MCF-7 cells in S phase increased after administration of LH-RH-MTX. The apoptosis rate of LH-RH-MTX group significantly increased compared with that of the control group and MTX group. The relative expression of LHRHR mRNA of LH-RH-MTX group markedly decreased compared with that of the control group and MTX group. LH-RH-MTX is realizable to reduce drug side effects, increase the therapeutic index and achieve tumor-targeted therapy.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
RNA, Messenger
/
Bone Marrow Cells
/
Leukocytes, Mononuclear
/
Cell Cycle
/
Cells, Cultured
/
Chemistry
/
Methotrexate
/
Gonadotropin-Releasing Hormone
/
Drug Delivery Systems
Limits:
Animals
/
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2012
Type:
Article
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