Radiolabeled somatostatin analogues, including octreotate have been used for targeted radiotherapy of neuroendocrine tumors
such as lymphoma, breast cancer, small-cell lung cancer and melanoma. In this paper, studies on the optimization of the production
of 177Lu, 166Ho and 153Sm radionuclides in Pakistan Atomic Research Reactor (PARR-I) and the investigations on the labeling of DOTA-Tyr-3 Octreotate
with 131I, 177Lu, 166Ho and 153Sm have been reported. The labeled DOTA-Tyr3-Octreotate complexes were found to be stable in acetate/ascorbate buffer and
saline at room temperature (18–22°C). The biodistribution studies of 177Lu-DOTA-Tyr-3 Octreotate in rat model indicated that the critical organ for this complex was the pancreas and the excretion
route was through kidney.
Onimaru, R., Shirato, H., Shimizu, S., et al.: Tolerance of organs at risk in small-volume, hypofractionated, image-guided radiotherapy for primary and metastatic lungcancers. Int. J. Radiat. Oncol. Biol. Phys., 2003, 56 (1), 126
Authors:Tamás Puskás, László Kovács, and Imre Henits
A szerzők négy beteg kórtörténetét ismertetik, akiknél az elmúlt két évben komputertomográfiás és mágneses rezonanciás vizsgálatokkal a pancreasban kialakult metasztázisokat diagnosztizáltak. Két betegnél a primer vesetumor felfedezése után több mint 10 évvel jelentek meg az áttétek a pancreasban. Egy nem kis sejtes tüdőtumoros és egy non-Hodgkin-lymphomában szenvedő betegnél a pancreasmetasztázist néhány hónappal a primer tumor felfedezését követően észlelték. A szerzők irodalmi adatok alapján megállapítják, hogy a pancreasban ritkák a metasztázisok. A pancreasmetasztázisok tünetei és radiológiai megjelenése változatos, ezért nem invazív képalkotó differenciáldiagnosztikájuk nehéz feladat. Ebben a beteg előzményeinek pontos ismerete és a funkcionális képalkotás jelent segítséget. Orv. Hetil., 2013, 154, 426–430.
Radon has been recognized to be one of the major contributors to the natural radiation causing even lung cancer if it is present
at enhanced levels. Its monitoring at highly confined locations such as underground caves, mines and tube-wells is very essential
for finding the health related hazards among the workers. This paper reports the investigations of the levels of radon, thoron
and their progeny monitored in the tube-wells of the Halls of residence at A.M.U., Aligarh, which lies in the subtropical
region of Indo-Gangetic plains situated in North India. The twin cup dosimeters were fixed for exposure at a depth of 5–35 feet
with a difference of 5 feet from the ground surface. The values of radon and thoron concentrations were found to vary from
6.58 to 1218.57 and 7.41–3226.61 Bq m−3, respectively. The preliminary results of this study for ‘bare mode’ detectors have been separately published and compared
with the recent data.
The development of pharmacological agents able to counteract the mechanisms of multidrug resistance (MDR) in oncology has remained a major goal for the past ten years. Several mechanisms are thought to be involved in drug resistance, including those associated with drug transport, detoxification and apoptosis. The first part of this thesis was focused on the inhibition of MDR through inhibition of the MDR P-glycoprotein (P-gp) in various cell lines. Six groups of compounds were involved in the P-gp efflux pump inhibitory studies: cinnamylidene ketones; 1,4-dihydropyridines derivatives; phenothiazines; HSP90 inhibitor peptide derivatives; Tylosin Betti base derivative and
diterpenes. The majority of the tested compounds were able to increase the R123 accumulation in cancer cell lines. Generally, the newly identified MDR modifiers were able to enhance the antiproliferative activity of selected anticancer drugs in a synergistic or additive way
on MDR cells. The
activity of TBN was confirmed in further
efficacy studies in DBA/2 mice. As an alternative way of antitumour effect, apoptosis inductions of resistance modifiers were studied. The substituted dihydropyridine 13 was the most promising apoptosis inducer on L 5178 Y cells. The human cytomegalovirus (CMV) was used in a modified
model for characterizing lathyrane compounds with antipromotion effect on human lung cancer cells. All the six macrocyclic lathyrane-type diterpenoids, except latilagascene D, could reduce the promotion
decreased IE-antigen expression of CMV to prevent progression of tumour malignancy.
Authors:S. Shirmardi, M. Gandomkar, M. Mazidi, M. Shafiei, and M. Ghannadi Maragheh
Tumors such as prostate, small cell lung cancer, breast, gastric and colon cancer are known to overexpress receptors to bombesin
(BBN). In this study, a new bombesin analogue was labeled with 99mTc via HYNIC and tricine/EDDA as coligands and investigated further. HYNIC-GABA-Bombesin (7–14) NH2 was synthesized using a standard Fmoc strategy. Labeling with 99mTc was performed at 100 °C for 10 min and radiochemical analysis involved ITLC and HPLC methods. The stability of radiopeptide
was checked in the presence of humane serum at 37 °C up to 24 h. The receptor bound internalization and externalization rates
were studied in GRP receptor expressing PC-3 cells. Biodistribution of radiopeptide was studied in nude mice bearing PC-3
tumor. Labeling yield of >98% was obtained corresponding to a specific activity of ~2.6 MBq/nmol. Peptide conjugate showed
good stability in the presence of human serum. The radioligand showed high and specific internalization into PC-3 cells (14.63 ± 0.41%
at 4 h). In biodistribution studies, a receptor-specific uptake was observed in GRP-receptor-positive organs so that after
4 h the uptakes in mouse tumor and pancreas were 1.31 ± 0.18 and 1.2 ± 0.13% ID/g, respectively.
Authors:O. Althunibat, B. Ridzwan, M. Taher, J. Daud, S. Jauhari Arief Ichwan, and H. Qaralleh
Sea cucumbers are marine invertebrates of the phylum of Echinodermata that have been used in Asian traditional medicine since ancient times. This study was conducted to investigate the antioxidant and cytotoxic properties of aqueous and organic extracts from two sea cucumber species, Holothuria edulis Lesson (Holothuriidae) and Stichopus horrens Selenka (Stichopodidae). Antioxidant activities of the extracts were evaluated by DPPH· and β-carotene bleaching assays, while MTT and trypan blue exclusion assays were used to demonstrate the cytotoxic effects of the extracts against two human cancer cell lines, non-small cell lung cancer cells (A549) and esophageal cancer cells (TE1). The results showed that both aqueous and organic extracts of H. edulis were able to scavenge DPH radical (IC50 at 2.04 mg/ml and 8.73 mg/ml, respectively). Aqueous and organic extracts of S. horrens inhibited 79.62% and 46.66% of β-carotene oxidation by linoleate free radical. On the other hand, the organic extract of S. horrens exhibited the highest cytotoxic effects against A549 and TE1 cancer cells giving IC50 at 15.5 and 4.0 μg/ml, respectively. In conclusion, the present study revealed that H. edulis and S. horrens contain promising levels of antioxidant and cytotoxic natural products that might be used for cancer prevention and treatment.
Inhalation of tobacco smoke is ranked second to food as a source of210Pb and210Po exposure to man. Assay of210Pb and210Po in commercially available tobacco collected from many countries have been carried out to assess the potential risk from210Po present in tobacco.The range of210Po contained in the tobacco grands varied from 10.08 to 15.0 mBq/tob or 13.0 to 20.1 mBq/g and the mean was 11.6 mBq/tob or 15.4 mBq/g. During the International Standard Smoking process about 50% of210Po present in tobaccos was transferred into the smoke and the other 50% remained in the ash and butt. About 10% of the total210Po of tobacco was inhaled by smoke through mainstream smoke. One pack-a-day smoker inhaled 24 mBq of210Po per day through smoking and the annual inhalation was 8.8 Bq. The risk of mortality from lung cancer caused by210Po in tobaccos was 18 per million persons for the above model.
The importance of angiogenesis in tumor growth and metastasis has led to develop new imaging tracers to understand angiogenic
vasculature. Based on the previous study, we further focused on the tumor molecular imaging application of the novel peptide
Arginine-Arginine-Leucine (Tyr-Cys-Gly-Gly-Arg-Arg-Leu-Gly-Gly-Cys, tRRL) in this study. The cytotoxicity of raioiodinated
tRRL (131I-tRRL) in HepG2 cells was assessed by tested cell viability using kit. tRRL was conjugated with fluorescein FITC to observe
its binding with tumor cells and human aortic endothelial cells (HAEC) in vitro. Whole body SPECT imaging of varied tumors
xenograftes was performed after intravenous injection of 131I-tRRL for 24 h in BALB/c nude mice. Compared with negative control PBS, small peptide tRRL was of non-cytotoxicity. 131I-tRRL could lead to significant cytotoxicity on HepG2 cells when the radioactivity was greater than 370 kBq. In vitro binding
experiment and cellular uptake results revealed that tRRL could adhere to tumor cells besides tumor derived endothelial cells.
In vivo SPECT imaging, 131I-tRRL mainly accumulated in various tumor tissues, including melanoma, liver cancer and lung cancer bearing mice. In breast
cancer xenografte imaging, the tumor has no significant radionuclide accumulation at 24 h after injected of 131I-tRRL. Radioiodinated tRRL offers a noninvasive nuclear imaging method for functional molecular imaging of tumors, and may
be a promising candidate carrier for tumor targeted therapy.