Synthesis, radiolabeling, biodistribution and fluorescent imaging of histidine-coupled hematoporphyrin.
BACKGROUND
Hematoporphyrin (Hp) and hematoporphyrin derivatives (HpDs) have been widely used as photosensitizers in photodynamic therapy (PDT). Radiolabeling of HpDs is helpful for preclinical and clinical studies of PDT.


METHODS
The histidine-coupled hematoporphyrin (His-Hp) was synthesized and radiolabeled with [(99m)Tc(CO)(3)(H(2)O)(3)](+). Biodistribution of the radioligand and fluorescent imaging of His-Hp in mice bearing S180 tumor were investigated.


RESULTS
[(99m)Tc(CO)(3)](+)-labeled His-Hp was electrically neutral, hydrophilic and stable. The biodistribution of the radioligand in S180 tumor-bearing mice was similar with that of nonlabeled HpD in the literature. The uptake of His-Hp in tumors and livers was confirmed by fluorescent imaging.


CONCLUSIONS
The complex [(99m)Tc(CO)(3)](+)-His-Hp might be suitable for in vivo dose evaluation of HpD in PDT.
Beijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, College of Chemistry and Molecular Engineering, Peking University, Beijing, P.R. China.
Yupeng
Y
Liu
Bo
B
Shen
Fei
F
Liu
Bin
B
Zhang
Taiwei
T
Chu
Jing
J
Bai
Shanglian
S
Bao
D000818:Animals; D045744:Cell Line, Tumor; D060326:Chemistry Techniques, Synthetic; D006415:Hematoporphyrins / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use; D006639:Histidine / Q000737:chemistry*; D007553:Isotope Labeling; D008297:Male; D051379:Mice; D057054:Molecular Imaging / Q000379:methods*; D015609:Organotechnetium Compounds / Q000737:chemistry; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use; D013050:Spectrometry, Fluorescence
D006415:Hematoporphyrins; D015609:Organotechnetium Compounds; D017319:Photosensitizing Agents; D006639:Histidine