Abstract
The inhibition of cell proliferation by methyl (2Z,4E)-2-methylsulfanyl-5-(1-naphthyl)-4-nitro-2,4-pentadienoate (1-Naph-NMCB) and (1E,3E)-1,4-bis(2-naphthyl)-2,3-dinitro-1,3-butadiene (2-Naph-DNB) has been studied in vitro against four cell lines selected for their resistance to doxorubicin, cisplatin, taxol and 5-fluorouracil. In previous experiments both compounds showed good in vitro antiproliferative, cytotoxic and pro-apoptotic activities against cell lines of different histologic origin. The results of the experiments presented here suggest that 1-Naph-NMCB is able to overcome all of the different mechanisms of resistance showed by the resistant cell lines used for our experiments. On the contrary, when we used the taxol-resistant A549-T12 cell line, characterized by a mechanism of resistance due to a mutation of the target site of taxol on microtubules, it displayed a partial but significant cross-resistance to 2-Naph-DNB. Although the actual mechanism of this cross-resistance has not yet been definitively elucidated, our results from immunostaining of microtubules suggest that it may be linked to the presence of a shared target site for taxol and 2-Naph-DNB on microtubules.
| Original language | English |
|---|---|
| Pages (from-to) | 47-51 |
| Number of pages | 5 |
| Journal | European Journal of Pharmacology |
| Volume | 588 |
| Issue number | 1 |
| DOIs | |
| Publication status | Published - Jun 24 2008 |
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Keywords
- 1-Naph-NMCB
- 2-Naph-DNB
- Drug-resistance
- Mechanism of resistance
ASJC Scopus subject areas
- Cellular and Molecular Neuroscience
- Pharmacology
Cite this
Sensitivity of different resistant tumour cell lines to the two novel compounds (2Z,4E)-2-methylsulfanyl-5-(1-naphthyl)-4-nitro-2,4-pentadienoate and (1E,3E)-1,4-bis(2-naphthyl)-2,3-dinitro-1,3-butadiene. / Viale, Maurizio; Petrillo, Giovanni; Maccagno, Massimo; Castagnola, Patrizio; Aiello, Cinzia; Cordazzo, Cinzia; Mariggiò, Maria A.; Jadhav, Sushilkumar A.; Bianchi, Lara; Leto, Giuseppe; Rizzato, Egon; Poggi, Alessandro; Spinelli, Domenico.
In: European Journal of Pharmacology, Vol. 588, No. 1, 24.06.2008, p. 47-51.Research output: Contribution to journal › Article
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TY - JOUR
T1 - Sensitivity of different resistant tumour cell lines to the two novel compounds (2Z,4E)-2-methylsulfanyl-5-(1-naphthyl)-4-nitro-2,4-pentadienoate and (1E,3E)-1,4-bis(2-naphthyl)-2,3-dinitro-1,3-butadiene
AU - Viale, Maurizio
AU - Petrillo, Giovanni
AU - Maccagno, Massimo
AU - Castagnola, Patrizio
AU - Aiello, Cinzia
AU - Cordazzo, Cinzia
AU - Mariggiò, Maria A.
AU - Jadhav, Sushilkumar A.
AU - Bianchi, Lara
AU - Leto, Giuseppe
AU - Rizzato, Egon
AU - Poggi, Alessandro
AU - Spinelli, Domenico
PY - 2008/6/24
Y1 - 2008/6/24
N2 - The inhibition of cell proliferation by methyl (2Z,4E)-2-methylsulfanyl-5-(1-naphthyl)-4-nitro-2,4-pentadienoate (1-Naph-NMCB) and (1E,3E)-1,4-bis(2-naphthyl)-2,3-dinitro-1,3-butadiene (2-Naph-DNB) has been studied in vitro against four cell lines selected for their resistance to doxorubicin, cisplatin, taxol and 5-fluorouracil. In previous experiments both compounds showed good in vitro antiproliferative, cytotoxic and pro-apoptotic activities against cell lines of different histologic origin. The results of the experiments presented here suggest that 1-Naph-NMCB is able to overcome all of the different mechanisms of resistance showed by the resistant cell lines used for our experiments. On the contrary, when we used the taxol-resistant A549-T12 cell line, characterized by a mechanism of resistance due to a mutation of the target site of taxol on microtubules, it displayed a partial but significant cross-resistance to 2-Naph-DNB. Although the actual mechanism of this cross-resistance has not yet been definitively elucidated, our results from immunostaining of microtubules suggest that it may be linked to the presence of a shared target site for taxol and 2-Naph-DNB on microtubules.
AB - The inhibition of cell proliferation by methyl (2Z,4E)-2-methylsulfanyl-5-(1-naphthyl)-4-nitro-2,4-pentadienoate (1-Naph-NMCB) and (1E,3E)-1,4-bis(2-naphthyl)-2,3-dinitro-1,3-butadiene (2-Naph-DNB) has been studied in vitro against four cell lines selected for their resistance to doxorubicin, cisplatin, taxol and 5-fluorouracil. In previous experiments both compounds showed good in vitro antiproliferative, cytotoxic and pro-apoptotic activities against cell lines of different histologic origin. The results of the experiments presented here suggest that 1-Naph-NMCB is able to overcome all of the different mechanisms of resistance showed by the resistant cell lines used for our experiments. On the contrary, when we used the taxol-resistant A549-T12 cell line, characterized by a mechanism of resistance due to a mutation of the target site of taxol on microtubules, it displayed a partial but significant cross-resistance to 2-Naph-DNB. Although the actual mechanism of this cross-resistance has not yet been definitively elucidated, our results from immunostaining of microtubules suggest that it may be linked to the presence of a shared target site for taxol and 2-Naph-DNB on microtubules.
KW - 1-Naph-NMCB
KW - 2-Naph-DNB
KW - Drug-resistance
KW - Mechanism of resistance
UR - http://www.scopus.com/inward/record.url?scp=44449169296&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=44449169296&partnerID=8YFLogxK
U2 - 10.1016/j.ejphar.2008.04.020
DO - 10.1016/j.ejphar.2008.04.020
M3 - Article
C2 - 18495109
AN - SCOPUS:44449169296
VL - 588
SP - 47
EP - 51
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
SN - 0014-2999
IS - 1
ER -