Protein Information

Name P gp
Synonyms ABC20; MDR1; ABCB 1; ABCB1; ATP binding cassette sub family B member 1; CD243; CD243 antigen; CLCS…

Compound Information

Name anthraquinone
CAS 9,10-anthracenedione

Reference List

PubMed Abstract RScore(About this table)
17949858 Cui XR, Tsukada M, Suzuki N, Shimamura T, Gao L, Koyanagi J, Komada F, Saito S: Comparison of the cytotoxic activities of naturally occurring hydroxyanthraquinones and hydroxynaphthoquinones. Eur J Med Chem. 2008 Jun;43(6):1206-15. Epub 2007 Sep 14.

The cytotoxicity of the anthraquinone and naphthoquinone derivatives on P-gp-underexpressing HCT 116 cells and P-gp-overexpressing Hep G2 cells was examined by MTT assay.
81(1,1,1,1) Details
12883032 Pors K, Paniwnyk Z, Teesdale-Spittle P, Plumb JA, Willmore E, Austin CA, Patterson LH: Alchemix: a novel alkylating anthraquinone with potent activity against anthracycline- and cisplatin-resistant ovarian cancer. Mol Cancer Ther. 2003 Jul;2(7):607-10.

This indicates that Alchemix can evade both P-glycoprotein efflux pump and DNA mismatch repair-mediated resistance.
1(0,0,0,1) Details
10739007 Fukushima T, Yamashita T, Takemura H, Suto H, Kishi S, Urasaki Y, Ueda T: Effect of PSC 833 on the cytotoxicity and pharmacodynamics of mitoxantrone in multidrug-resistant K562 cells. Leuk Res. 2000 Mar;24(3):249-54.

We examined the effect of PSC 833, a nonimmunosuppressive cyclosporin analogue, on the cytotoxicity, accumulation and retention of an anthraquinone antileukemia drug mitoxantrone (MIT).
This was done in P-glycoprotein (PGP)-overexpressing multidrug-resistant K562/D1-9 cells and compared with the effect of cyclosporin A (CsA).
1(0,0,0,1) Details
18035333 Hsiao CJ, Li TK, Chan YL, Hsin LW, Liao CH, Lee CH, Lyu PC, Guh JH: WRC-213, an l-methionine-conjugated mitoxantrone derivative, displays anticancer activity with reduced cardiotoxicity and drug resistance: identification of topoisomerase II inhibition and apoptotic machinery in prostate cancers. Biochem Pharmacol. 2008 Feb 15;75(4):847-56. Epub 2007 Oct 22.

Moreover, the assessment of cytotoxicity in H9c2 cardiomyocytes and drug resistance in NCI/ADR-RES cells demonstrated that WRC-213 showed much lower cardiotoxicity and P-glycoprotein-related resistance than those of mitoxantrone, etoposide and doxorubicin.
Several l- and d-form amino acids were introduced into the anthraquinone skeleton and numerous derivatives were synthesized for the evaluation of anticancer activity.
1(0,0,0,1) Details
11906965 Tarasiuk J, Stefanska B, Plodzich I, Tkaczyk-Gobis K, Seksek O, Martelli S, Garnier-Suillerot A, Borowski E: Anthrapyridones, a novel group of antitumour non-cross resistant anthraquinone analogues. Br J Pharmacol. 2002 Mar;135(6):1513-23.

The interaction of these derivatives with erythroleukemia K562 sensitive and K562/DOX resistant (overexpressing P-glycoprotein) cell lines has been examined.
4(0,0,0,4) Details
16458007 Dzieduszycka M, Bontemps-Gracz MM, Stefanska B, Martelli S, Piwkowska A, Arciemiuk M, Borowski E: Synthesis of 7-oxo-7H-naphtho [1,2,3-de] quinoline derivatives as potential anticancer agents active on multidrug resistant cell lines. Bioorg Med Chem. 2006 May 1;14(9):2880-6. Epub 2006 Feb 2.

Following our earlier finding that tetracyclic anthraquinone analogs with a fused pyridone ring exhibit cytotoxic activity toward multidrug resistant tumor cells, a series of new potential antitumor agents, 7-oxo-7H-naphtho [1,2,3-de] quinoline derivatives (3, 6-8, 10-12, 14, 15, and 18), bearing one or two basic side chains and various substituents at the pyridone ring, have been synthesized.
The compounds exhibited cytotoxic activity toward sensitive human leukemia cell line HL-60 and against its resistant sublines HL-60/VINC (MDR1 type) and HL-60/DX (MRP1 type).
1(0,0,0,1) Details
16521213 Akimoto M, Yoshikawa M, Ebara M, Sato T, Fukuda H, Kondo F, Saisho H: Relationship between therapeutic efficacy of arterial infusion chemotherapy and expression of P-glycoprotein and p53 protein in advanced hepatocellular carcinoma. World J Gastroenterol. 2006 Feb 14;12(6):868-73.

When only the data from the 11 patients treated with anthraquinone drug, mitoxantrone, were analyzed, however, the number of patients who showed poor response to treatment was significantly higher among the p53-positive patients (P=0.012), irrespective of the survival outcome.
1(0,0,0,1) Details