Advances in Clinical and Experimental Medicine

Title abbreviation: Adv Clin Exp Med
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ISSN 1899–5276 (print)
ISSN 2451-2680 (online)
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Advances in Clinical and Experimental Medicine

2013, vol. 22, nr 3, May-June, p. 319–325

Publication type: original article

Language: English

Synthesis of 99mTc Labeled Temafloxacin Complex and Biodistribution in Male Wistar Rats Artificially Infected with Streptococci pneumonia

Synteza kompleksu temafloksacyny znakowanego 99mTc i biodystrybucja u samców szczurów szczepu Wistar sztucznie zakażonych szczepami Streptococcus pneumoniae

Syed Q. Shah1,A,D,E,F, Mohammad R. Khan2,E,F

1 Nuclear Medicine Research Laboratory (NMRL), University of Peshawar, Peshawar, KPK, Pakistan

2 Phytopharmaceutical & Neutraceuticals Research Laboratory (PNRL), University of Peshawar, Peshawar, KPK, Pakistan

Abstract

Background. Radiotracers techniques are offering a unique way to diagnosis deep tissue infection in its early stages. The radiotracers including radio-antibiotics have shown promising results in the early diagnosis of infection and its discrimination from infectious foci but wide ranges of microorganisms still poses threats.
Objectives. Synthesis of Technetium-99m (99mTc)-temafloxacin (TMC) complex for the localization of in vivo Streptococci pneumoniae infection in the early stages.
Material and Methods. The 99mTc-TMC complex was prepared by adding 50 µg of stannous chloride (SnCl2) with 4 37 MBq (0.5 mL) of sodium pertechnetate (Na99mTco -) at a pH of 5.2. Then 1 mg of the TMC was added to the mixture followed by incubation at room temperature for 10 min. The same procedure was repeated by changing the – amount of the SnCl2 from 50 to 250 µg along with the TMC from 2 to 5 mg and Na99mTco4 from 74 to 185 MBq. In higher concentrations of cysteine the stability of the 99mTc-TMC complex was evaluated. In vitro Streptococci pneumoniae uptake was investigated to validate the accuracy and preciseness of the 99mTc-TMC complex. In vivo uptake of the 99mTc-TMC complex was evaluated in ten (10) normal male Wistar rats (MWR) (140–160 g) divided into two groups (I and II).
Results. Maximum stability of 98.00 ± 0.34% at 30 min after reconstitution was observed by mixing 2.5 mg of TMC, – 100 µg of SnCl2 with 74 MBq of the Na99mTco4 . The stability of the complex remained 90% up to 4 hours. In serum the complex showed stability up to 16 hours. A saturated in vitro binding was noted with live Streptococci pneu- moniae. In the infected region (left thigh) of the MWR, almost five times higher uptake was observed as compared to the inflamed and normal muscles.
Conclusion. The above results confirm the suitability of the 99mTc-TMC complex as a potential Streptococci pneu- moniae infection localizing agent.

Streszczenie

Wprowadzenie.Techniki wykorzystujące radioznaczniki oferują unikalny sposób rozpoznawania zakażenia tkanek głębokich w jego początkowej fazie. Radioznaczniki, w tym antybiotyki, wykazały obiecujące wyniki w wczesnej diagnostyce infekcji i odróżnianie jej ognisk zakaźnych, ale szeroki zakres drobnoustrojów nadal stwarza zagrożenia.
Cel pracy. Synteza kompleksu technetu 99m (99mTc) i temafloksacyny (TMC) w celu umiejscowienia in vivo wczesnego zakażenia szczepami Streptococcus pneumoniae.
Materiał i metody. Kompleks 99mTc-TMC został przygotowany przez dodanie 50 µg chlorku cyny (SnCI2) do – 37 MBq (0,5 ml) nadtechnecjanu sodu (Na99mTco4 ) przy pH 5,2. Następnie 1 mg TMC dodano do mieszaniny, a następnie inkubowano w temperaturze pokojowej przez 10 minut. Tę samą procedurę powtórzono, zmieniając 4 ilość SnCl2 od 50 do 250 ug, TMC od 2 do 5 mg, Na99mTco – od 74 do 185 MBq. W większych stężeniach cysteiny oceniono stabilność kompleksu 99mTc-TMC. Badano wychwyt szczepów Streptococcus pneumoniae in vitro w celu sprawdzenia dokładności kompleksu 99mTc-TMC. Wychwyt kompleksu 99mTc-TMC oceniano in vivo u dziesięciu (10) zdrowych samców szczurów Wistar (MWR) (140–160 g), które podzielono na dwie grupy (I i II).
Wyniki. Maksymalną stabilność 98,00 ± 0,34% 30 minut po rozpuszczeniu obserwowano przez zmieszanie 2,5 mg 4 TMC, 100 ng SnCl2 z 74 MBq w Na99mTco –. Stabilność kompleksu pozostała na poziomie 90% do 4 godzin. W surowicy kompleks wykazał stabilność do 16 godzin. Nasycone wiązania in vitro stwierdzono u żywych Streptococcus pneumoniae. Z zakażonego obszaru ciała (lewe udo) MWR zaobserwowano prawie pięciokrotnie większy wychwyt w porównaniu do mięśni zdrowych i zmienionych zapalnie.
Wnioski. Powyższe wyniki potwierdzają przydatność kompleksu 99mTc-TMC jako środka do umiejscawiania potencjalnego zakażenia Streptococcus pneumoniae .

Key words

99mTc-Temafloxacin, Streptococci pneumoniae, infection localization.

Słowa kluczowe

99mTc-temafloksacyna, Streptococcus pneumoniae, umiejscawianie zakażenia.

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