Radiolabeling and preliminary biological evaluation of a (99)mTc(CO)(3) labeled 3,3 '-(benzylidene)-bis-(1H-indole-2-carbohydrazide) derivative as a potential SPECT tracer for in vivo visualization of necrosis

Kristof Prinsen; Lixin Jin; Kathleen Vunckx; Marijke De Saint-Hubert; Lin Zhou; Jan Cleynhens; Johan Nuyts; Guy M. Bormans; Yicheng Ni; Alfons M. Verbruggen

doi:10.1016/j.bmcl.2010.10.102

Radiolabeling and preliminary biological evaluation of a (99)mTc(CO)(3) labeled 3,3 '-(benzylidene)-bis-(1H-indole-2-carbohydrazide) derivative as a potential SPECT tracer for in vivo visualization of necrosis

Kristof Prinsen
, Lixin Jin
, Kathleen Vunckx
, Marijke De Saint-Hubert
, Lin Zhou
, Jan Cleynhens
, Johan Nuyts
, Guy M. Bormans
, Yicheng Ni
, Alfons M. Verbruggen^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › Academic › peer-review

Abstract

N,N'-bis(diethylenetriamine pentaacetic acid)-3,3'-(benzylidene)-bis-(1H-indole-2-carbohydrazide) (bis-DTPA-BI) was radiolabeled with (99m)Tc(CO)(3). The resulting (99m)Tc(CO)(3)-bis-DTPA-BI was characterized (LC-MS) and evaluated as a potential SPECT tracer for imaging of necrosis in Wistar rats with a reperfused partial liver infarction and Wistar rats with ethanol induced muscular necrosis. To study the specificity, uptake of (99m)Tc(CO)(3)-bis-DTPA-BI was also studied in a mouse model of Fas-mediated hepatic apoptosis. The obtained results indicate that (99m)Tc(CO)(3)-bis-DTPA-BI displays selective uptake in necrotic tissue and can be used for in vivo visualization of necrosis by SPECT.

Original language	English
Pages (from-to)	502-505
Number of pages	4
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	21
Issue number	1
DOIs	https://doi.org/10.1016/j.bmcl.2010.10.102
Publication status	Published - Jan 2011

Keywords

Cell death
Necrosis
Tc-99m(CO)(3)
SPECT
Benzylidene-bis-indole

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Prinsen, K., Jin, L., Vunckx, K., De Saint-Hubert, M., Zhou, L., Cleynhens, J., Nuyts, J., Bormans, G. M., Ni, Y., & Verbruggen, A. M. (2011). Radiolabeling and preliminary biological evaluation of a (99)mTc(CO)(3) labeled 3,3 '-(benzylidene)-bis-(1H-indole-2-carbohydrazide) derivative as a potential SPECT tracer for in vivo visualization of necrosis. Bioorganic & Medicinal Chemistry Letters, 21(1), 502-505. https://doi.org/10.1016/j.bmcl.2010.10.102

@article{f9dc941e2cfc4e729dcb5052e679f098,

title = "Radiolabeling and preliminary biological evaluation of a (99)mTc(CO)(3) labeled 3,3 '-(benzylidene)-bis-(1H-indole-2-carbohydrazide) derivative as a potential SPECT tracer for in vivo visualization of necrosis",

abstract = "N,N'-bis(diethylenetriamine pentaacetic acid)-3,3'-(benzylidene)-bis-(1H-indole-2-carbohydrazide) (bis-DTPA-BI) was radiolabeled with (99m)Tc(CO)(3). The resulting (99m)Tc(CO)(3)-bis-DTPA-BI was characterized (LC-MS) and evaluated as a potential SPECT tracer for imaging of necrosis in Wistar rats with a reperfused partial liver infarction and Wistar rats with ethanol induced muscular necrosis. To study the specificity, uptake of (99m)Tc(CO)(3)-bis-DTPA-BI was also studied in a mouse model of Fas-mediated hepatic apoptosis. The obtained results indicate that (99m)Tc(CO)(3)-bis-DTPA-BI displays selective uptake in necrotic tissue and can be used for in vivo visualization of necrosis by SPECT.",

keywords = "Cell death, Necrosis, Tc-99m(CO)(3), SPECT, Benzylidene-bis-indole",

author = "Kristof Prinsen and Lixin Jin and Kathleen Vunckx and \{De Saint-Hubert\}, Marijke and Lin Zhou and Jan Cleynhens and Johan Nuyts and Bormans, \{Guy M.\} and Yicheng Ni and Verbruggen, \{Alfons M.\}",

year = "2011",

month = jan,

doi = "10.1016/j.bmcl.2010.10.102",

language = "English",

volume = "21",

pages = "502--505",

journal = "Bioorganic \& Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd",

number = "1",

}

Prinsen, K, Jin, L, Vunckx, K, De Saint-Hubert, M, Zhou, L, Cleynhens, J, Nuyts, J, Bormans, GM, Ni, Y & Verbruggen, AM 2011, 'Radiolabeling and preliminary biological evaluation of a (99)mTc(CO)(3) labeled 3,3 '-(benzylidene)-bis-(1H-indole-2-carbohydrazide) derivative as a potential SPECT tracer for in vivo visualization of necrosis', Bioorganic & Medicinal Chemistry Letters, vol. 21, no. 1, pp. 502-505. https://doi.org/10.1016/j.bmcl.2010.10.102

Radiolabeling and preliminary biological evaluation of a (99)mTc(CO)(3) labeled 3,3 '-(benzylidene)-bis-(1H-indole-2-carbohydrazide) derivative as a potential SPECT tracer for in vivo visualization of necrosis. / Prinsen, Kristof; Jin, Lixin; Vunckx, Kathleen et al.
In: Bioorganic & Medicinal Chemistry Letters, Vol. 21, No. 1, 01.2011, p. 502-505.

Research output: Contribution to journal › Article › Academic › peer-review

TY - JOUR

T1 - Radiolabeling and preliminary biological evaluation of a (99)mTc(CO)(3) labeled 3,3 '-(benzylidene)-bis-(1H-indole-2-carbohydrazide) derivative as a potential SPECT tracer for in vivo visualization of necrosis

AU - Prinsen, Kristof

AU - Jin, Lixin

AU - Vunckx, Kathleen

AU - De Saint-Hubert, Marijke

AU - Zhou, Lin

AU - Cleynhens, Jan

AU - Nuyts, Johan

AU - Bormans, Guy M.

AU - Ni, Yicheng

AU - Verbruggen, Alfons M.

PY - 2011/1

Y1 - 2011/1

N2 - N,N'-bis(diethylenetriamine pentaacetic acid)-3,3'-(benzylidene)-bis-(1H-indole-2-carbohydrazide) (bis-DTPA-BI) was radiolabeled with (99m)Tc(CO)(3). The resulting (99m)Tc(CO)(3)-bis-DTPA-BI was characterized (LC-MS) and evaluated as a potential SPECT tracer for imaging of necrosis in Wistar rats with a reperfused partial liver infarction and Wistar rats with ethanol induced muscular necrosis. To study the specificity, uptake of (99m)Tc(CO)(3)-bis-DTPA-BI was also studied in a mouse model of Fas-mediated hepatic apoptosis. The obtained results indicate that (99m)Tc(CO)(3)-bis-DTPA-BI displays selective uptake in necrotic tissue and can be used for in vivo visualization of necrosis by SPECT.

AB - N,N'-bis(diethylenetriamine pentaacetic acid)-3,3'-(benzylidene)-bis-(1H-indole-2-carbohydrazide) (bis-DTPA-BI) was radiolabeled with (99m)Tc(CO)(3). The resulting (99m)Tc(CO)(3)-bis-DTPA-BI was characterized (LC-MS) and evaluated as a potential SPECT tracer for imaging of necrosis in Wistar rats with a reperfused partial liver infarction and Wistar rats with ethanol induced muscular necrosis. To study the specificity, uptake of (99m)Tc(CO)(3)-bis-DTPA-BI was also studied in a mouse model of Fas-mediated hepatic apoptosis. The obtained results indicate that (99m)Tc(CO)(3)-bis-DTPA-BI displays selective uptake in necrotic tissue and can be used for in vivo visualization of necrosis by SPECT.

KW - Cell death

KW - Necrosis

KW - Tc-99m(CO)(3)

KW - SPECT

KW - Benzylidene-bis-indole

U2 - 10.1016/j.bmcl.2010.10.102

DO - 10.1016/j.bmcl.2010.10.102

M3 - Article

C2 - 21075631

SN - 0960-894X

VL - 21

SP - 502

EP - 505

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 1

ER -

Prinsen K, Jin L, Vunckx K, De Saint-Hubert M, Zhou L, Cleynhens J et al. Radiolabeling and preliminary biological evaluation of a (99)mTc(CO)(3) labeled 3,3 '-(benzylidene)-bis-(1H-indole-2-carbohydrazide) derivative as a potential SPECT tracer for in vivo visualization of necrosis. Bioorganic & Medicinal Chemistry Letters. 2011 Jan;21(1):502-505. doi: 10.1016/j.bmcl.2010.10.102