PMID- 12208034
OWN - NLM
STAT- MEDLINE
DCOM- 20030417
LR  - 20190922
IS  - 1011-1344 (Print)
IS  - 1011-1344 (Linking)
VI  - 68
IP  - 1
DP  - 2002 Aug
TI  - Preparation and biological evaluation of the new chlorin photosensitizer T3,4BCPC 
      for detection and treatment of tumors.
PG  - 33-8
AB  - The new water-soluble photosensitizer 
      5,10,15,20-tetrakis[3,4-bis(carboxymethyleneoxy)phenyl]chlorin (T3,4BCPC) has 
      been prepared, characterized and labeled with 99mTc radionuclide. The radiotracer 
      was evaluated for tissue distribution in Wistar rats. Accumulation of 
      administrated activities in the liver, kidney, bladder and large intestine at 4 h 
      post-injection indicated that the labeled ligand was largely eliminated through 
      the renal and partly through the hepatobiliary system. In vivo biodistribution 
      studies of the labeled compound were carried out in rodent and murine tumor 
      models in comparison with other tumor-seeking radiopharmaceuticals such as 
      99mTc(V)-dimercaptosuccinic acid (DMSA), 201thallous chloride (TlCl) and 
      99mTc-citrate using a gamma camera computer system. In N-nitrosomethylurea 
      (NMU)-induced rat mammary tumors, the labeled ligand showed a five-fold tumor to 
      muscle (T/M) ratio compared to 99mTc(V)-DMSA (3-fold) and 201TlCl (3-fold). In 
      the case of C(3)H/J virus-induced spontaneous mammary tumors, the differences 
      were not marked. However, in the transplanted rat C(6)-glioma, the T/M ratio of 
      the labeled compound was appreciably higher (four-fold) than that noted with 
      99mTc(V)-DMSA (two-fold), 201TlCl (three-fold) and 99mTc-citrate (more than 
      three-fold). These findings suggest that the radiolabeled T3,4BCPC may have 
      potential for the detection of cancer. In order to ascertain the efficacy of the 
      compound for photodynamic therapy applications, a preclinical PDT study was 
      carried out in fibrosarcoma-bearing mice after injecting 5.0 mg/kg body weight of 
      the T3,4BCPC. A laser dose of 20 mW for 60 s resulted in 80% destruction of 
      tumors. These data suggest that this molecule could be useful for PDT of cancer. 
      The labeled agent could also be useful in monitoring the progression/regression 
      of tumors before, during, and after chemotherapy, radiation therapy or PDT.
CI  - Copyright 2002 Elsevier Science B.V.
FAU - Murugesan, S
AU  - Murugesan S
AD  - Radiation Medicine Centre, Bhabha Atomic Research Centre, Tata Memorial Hospital 
      Annexe, Parel, Mumbai 400012, India. smuru1999@yahoo.com
FAU - Shetty, S J
AU  - Shetty SJ
FAU - Srivastava, T S
AU  - Srivastava TS
FAU - Samuel, A M
AU  - Samuel AM
FAU - Noronha, O P D
AU  - Noronha OP
LA  - eng
PT  - Journal Article
PL  - Switzerland
TA  - J Photochem Photobiol B
JT  - Journal of photochemistry and photobiology. B, Biology
JID - 8804966
RN  - 0 (5,10,15,20-tetrakis(3,4-bis(carboxymethyleneoxy)phenyl)chlorin)
RN  - 0 (Anthracenes)
RN  - 0 (Photosensitizing Agents)
RN  - 0 (Porphyrins)
RN  - 0 (Radiopharmaceuticals)
RN  - 684-93-5 (Methylnitrosourea)
RN  - 7440-26-8 (Technetium)
SB  - IM
MH  - Animals
MH  - Anthracenes/chemical synthesis/*pharmacokinetics/*therapeutic use
MH  - Female
MH  - Glioma/*drug therapy
MH  - Isotope Labeling/methods
MH  - Male
MH  - Mammary Neoplasms, Experimental/chemically induced/*drug therapy
MH  - Methylnitrosourea
MH  - Neoplasms/diagnosis/*drug therapy
MH  - Photosensitizing Agents/chemical synthesis/*pharmacokinetics/*therapeutic use
MH  - Porphyrins/chemical synthesis/pharmacokinetics/*therapeutic use
MH  - Radiopharmaceuticals/chemical synthesis/therapeutic use
MH  - Rats
MH  - Rats, Wistar
MH  - *Technetium
MH  - Time Factors
MH  - Tissue Distribution
EDAT- 2002/09/05 10:00
MHDA- 2003/04/18 05:00
CRDT- 2002/09/05 10:00
PHST- 2002/09/05 10:00 [pubmed]
PHST- 2003/04/18 05:00 [medline]
PHST- 2002/09/05 10:00 [entrez]
AID - S1011134402003299 [pii]
AID - 10.1016/s1011-1344(02)00329-9 [doi]
PST - ppublish
SO  - J Photochem Photobiol B. 2002 Aug;68(1):33-8. doi: 10.1016/s1011-1344(02)00329-9.