99mTc-d-penicillamine-glucuronide: synthesis, radiolabeling, in vitro and in vivo evaluation
The current study was aimed at synthesizing a glucuronide derivative of D-penicillamine (D-PA) to be used for imaging purposes. First of all, D-PA-glucuronide (D-PA-Glu) was synthesized by experimental treatments starting with uridine 5'-diphospho-glucuronosyltransferase enzyme rich microsome p...
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| Veröffentlicht in: | Cancer biotherapy & radiopharmaceuticals 2011-10, Vol.26 (5), p.623-630 |
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| creator | Teksöz, Serap Içhedef, Ciğdem Acar Ozyüncü, Seniha Müftüler, Fazilet Zümrüt Biber Unak, Perihan Medine, Ilker Emin Ertay, Türkan Eren, Mine Şencan |
| description | The current study was aimed at synthesizing a glucuronide derivative of D-penicillamine (D-PA) to be used for imaging purposes. First of all, D-PA-glucuronide (D-PA-Glu) was synthesized by experimental treatments starting with uridine 5'-diphospho-glucuronosyltransferase enzyme rich microsome preparate. Then, the synthesized compound was labeled with technetium ((99m)Tc) by using a reduction method with stannous chloride. Quality controls were performed by using high-performance liquid chromatography and thin-layer radio chromatography (TLRC). Radiolabeling yield of (99m)Tc-D-PA-Glu was more than 98% according to TLRC results. In vitro evaluations of radiolabeled complexes were investigated on PC-3 human prostate cancer cells. (99m)Tc-D-PA-Glu exhibited more accumulation on PC-3 cells versus (99m)Tc-D-PA at 240 minutes. In order to determine its radiopharmaceutical potential, biodistribution studies were carried out in male Albino Wistar rats. The biodistribution results of (99m)Tc-D-PA-Glu, showed the highest uptake in prostate at 120 minutes postinjection with the main excretion route being through kidneys and bladder. (99m)Tc-D-PA-Glu and (99m)Tc-D-PA have exhibited different biodistribution results. |
| doi_str_mv | 10.1089/cbr.2010.0854 |
| format | Article |
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First of all, D-PA-glucuronide (D-PA-Glu) was synthesized by experimental treatments starting with uridine 5'-diphospho-glucuronosyltransferase enzyme rich microsome preparate. Then, the synthesized compound was labeled with technetium ((99m)Tc) by using a reduction method with stannous chloride. Quality controls were performed by using high-performance liquid chromatography and thin-layer radio chromatography (TLRC). Radiolabeling yield of (99m)Tc-D-PA-Glu was more than 98% according to TLRC results. In vitro evaluations of radiolabeled complexes were investigated on PC-3 human prostate cancer cells. (99m)Tc-D-PA-Glu exhibited more accumulation on PC-3 cells versus (99m)Tc-D-PA at 240 minutes. In order to determine its radiopharmaceutical potential, biodistribution studies were carried out in male Albino Wistar rats. The biodistribution results of (99m)Tc-D-PA-Glu, showed the highest uptake in prostate at 120 minutes postinjection with the main excretion route being through kidneys and bladder. (99m)Tc-D-PA-Glu and (99m)Tc-D-PA have exhibited different biodistribution results.</description><identifier>ISSN: 1084-9785</identifier><identifier>EISSN: 1557-8852</identifier><identifier>DOI: 10.1089/cbr.2010.0854</identifier><identifier>PMID: 21950558</identifier><language>eng</language><publisher>United States: Mary Ann Liebert, Inc</publisher><subject>Animals ; Cell Line, Tumor ; Chromatography, High Pressure Liquid ; Glucuronides - chemical synthesis ; Glucuronides - chemistry ; Glucuronides - pharmacokinetics ; Humans ; Male ; Mass Spectrometry ; Organotechnetium Compounds - chemical synthesis ; Organotechnetium Compounds - chemistry ; Organotechnetium Compounds - pharmacokinetics ; Penicillamine - analogs & derivatives ; Penicillamine - chemical synthesis ; Penicillamine - chemistry ; Penicillamine - pharmacokinetics ; Prostatic Neoplasms - metabolism ; Rats ; Rats, Wistar ; Technetium - chemistry ; Tissue Distribution</subject><ispartof>Cancer biotherapy & radiopharmaceuticals, 2011-10, Vol.26 (5), p.623-630</ispartof><rights>(©) Copyright 2011, Mary Ann Liebert, Inc.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/21950558$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Teksöz, Serap</creatorcontrib><creatorcontrib>Içhedef, Ciğdem Acar</creatorcontrib><creatorcontrib>Ozyüncü, Seniha</creatorcontrib><creatorcontrib>Müftüler, Fazilet Zümrüt Biber</creatorcontrib><creatorcontrib>Unak, Perihan</creatorcontrib><creatorcontrib>Medine, Ilker Emin</creatorcontrib><creatorcontrib>Ertay, Türkan</creatorcontrib><creatorcontrib>Eren, Mine Şencan</creatorcontrib><title>99mTc-d-penicillamine-glucuronide: synthesis, radiolabeling, in vitro and in vivo evaluation</title><title>Cancer biotherapy & radiopharmaceuticals</title><addtitle>Cancer Biother Radiopharm</addtitle><description>The current study was aimed at synthesizing a glucuronide derivative of D-penicillamine (D-PA) to be used for imaging purposes. 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The biodistribution results of (99m)Tc-D-PA-Glu, showed the highest uptake in prostate at 120 minutes postinjection with the main excretion route being through kidneys and bladder. (99m)Tc-D-PA-Glu and (99m)Tc-D-PA have exhibited different biodistribution results.</description><subject>Animals</subject><subject>Cell Line, Tumor</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Glucuronides - chemical synthesis</subject><subject>Glucuronides - chemistry</subject><subject>Glucuronides - pharmacokinetics</subject><subject>Humans</subject><subject>Male</subject><subject>Mass Spectrometry</subject><subject>Organotechnetium Compounds - chemical synthesis</subject><subject>Organotechnetium Compounds - chemistry</subject><subject>Organotechnetium Compounds - pharmacokinetics</subject><subject>Penicillamine - analogs & derivatives</subject><subject>Penicillamine - chemical synthesis</subject><subject>Penicillamine - chemistry</subject><subject>Penicillamine - pharmacokinetics</subject><subject>Prostatic Neoplasms - metabolism</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Technetium - chemistry</subject><subject>Tissue Distribution</subject><issn>1084-9785</issn><issn>1557-8852</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>BENPR</sourceid><recordid>eNpdkM9LwzAcxYMobk6PXqV48bLMJE2Wb7zJ8BcMvOwolDRJZ0ab1KYd7L-34rx4-r4HHx7f9xC6pmRBCah7U3YLRkZHQPATNKVCSAwg2OmoCXCsJIgJukhpRwhZkqU8RxNGlSBCwBR9KNVsDLa4dcEbX9e68cHhbT2YoYvBW_eQpUPoP13yaZ512vpY69LVPmznmQ_Z3vddzHSwv2YfM7fX9aB7H8MlOqt0ndzV8c7Q5vlps3rF6_eXt9XjGrfAAOeltoLxpTSl45wCEA65ACmI_WmoZV4K5srKWOUoB6Eoq5ysrNZGachdPkN3v7FtF78Gl_qi8cm4sUtwcUgFKBCEcS5H8vYfuYtDF8bfRkgKxQnlI3RzhIaycbZoO9_o7lD8jZZ_A042bgk</recordid><startdate>201110</startdate><enddate>201110</enddate><creator>Teksöz, Serap</creator><creator>Içhedef, Ciğdem Acar</creator><creator>Ozyüncü, Seniha</creator><creator>Müftüler, Fazilet Zümrüt Biber</creator><creator>Unak, Perihan</creator><creator>Medine, Ilker Emin</creator><creator>Ertay, Türkan</creator><creator>Eren, Mine Şencan</creator><general>Mary Ann Liebert, Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>3V.</scope><scope>7QP</scope><scope>7T5</scope><scope>7TK</scope><scope>7X7</scope><scope>7XB</scope><scope>88A</scope><scope>88E</scope><scope>88I</scope><scope>8C1</scope><scope>8FE</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BHPHI</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>H94</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>LK8</scope><scope>M0S</scope><scope>M1P</scope><scope>M2P</scope><scope>M7P</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>Q9U</scope><scope>7X8</scope></search><sort><creationdate>201110</creationdate><title>99mTc-d-penicillamine-glucuronide: synthesis, radiolabeling, in vitro and in vivo evaluation</title><author>Teksöz, Serap ; Içhedef, Ciğdem Acar ; Ozyüncü, Seniha ; Müftüler, Fazilet Zümrüt Biber ; Unak, Perihan ; Medine, Ilker Emin ; Ertay, Türkan ; Eren, Mine Şencan</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p828-3bad52467cbe44188048358750d1089a73b52ebfcd9e1485912fe7fdaac9a83e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2011</creationdate><topic>Animals</topic><topic>Cell Line, Tumor</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Glucuronides - chemical synthesis</topic><topic>Glucuronides - chemistry</topic><topic>Glucuronides - pharmacokinetics</topic><topic>Humans</topic><topic>Male</topic><topic>Mass Spectrometry</topic><topic>Organotechnetium Compounds - chemical synthesis</topic><topic>Organotechnetium Compounds - chemistry</topic><topic>Organotechnetium Compounds - pharmacokinetics</topic><topic>Penicillamine - analogs & derivatives</topic><topic>Penicillamine - chemical synthesis</topic><topic>Penicillamine - chemistry</topic><topic>Penicillamine - pharmacokinetics</topic><topic>Prostatic Neoplasms - metabolism</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Technetium - chemistry</topic><topic>Tissue Distribution</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Teksöz, Serap</creatorcontrib><creatorcontrib>Içhedef, Ciğdem Acar</creatorcontrib><creatorcontrib>Ozyüncü, Seniha</creatorcontrib><creatorcontrib>Müftüler, Fazilet Zümrüt Biber</creatorcontrib><creatorcontrib>Unak, Perihan</creatorcontrib><creatorcontrib>Medine, Ilker Emin</creatorcontrib><creatorcontrib>Ertay, Türkan</creatorcontrib><creatorcontrib>Eren, Mine Şencan</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>ProQuest Central (Corporate)</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Immunology Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Biology Database (Alumni Edition)</collection><collection>Medical Database (Alumni Edition)</collection><collection>Science Database (Alumni Edition)</collection><collection>Public Health Database</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Natural Science Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>Biological Science Collection</collection><collection>ProQuest Central</collection><collection>Natural Science Collection</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>SciTech Premium Collection</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>ProQuest Biological Science Collection</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Science Database</collection><collection>Biological Science Database</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>ProQuest Central Basic</collection><collection>MEDLINE - 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First of all, D-PA-glucuronide (D-PA-Glu) was synthesized by experimental treatments starting with uridine 5'-diphospho-glucuronosyltransferase enzyme rich microsome preparate. Then, the synthesized compound was labeled with technetium ((99m)Tc) by using a reduction method with stannous chloride. Quality controls were performed by using high-performance liquid chromatography and thin-layer radio chromatography (TLRC). Radiolabeling yield of (99m)Tc-D-PA-Glu was more than 98% according to TLRC results. In vitro evaluations of radiolabeled complexes were investigated on PC-3 human prostate cancer cells. (99m)Tc-D-PA-Glu exhibited more accumulation on PC-3 cells versus (99m)Tc-D-PA at 240 minutes. In order to determine its radiopharmaceutical potential, biodistribution studies were carried out in male Albino Wistar rats. The biodistribution results of (99m)Tc-D-PA-Glu, showed the highest uptake in prostate at 120 minutes postinjection with the main excretion route being through kidneys and bladder. (99m)Tc-D-PA-Glu and (99m)Tc-D-PA have exhibited different biodistribution results.</abstract><cop>United States</cop><pub>Mary Ann Liebert, Inc</pub><pmid>21950558</pmid><doi>10.1089/cbr.2010.0854</doi><tpages>8</tpages></addata></record> |
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| issn | 1084-9785 1557-8852 |
| language | eng |
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| subjects | Animals Cell Line, Tumor Chromatography, High Pressure Liquid Glucuronides - chemical synthesis Glucuronides - chemistry Glucuronides - pharmacokinetics Humans Male Mass Spectrometry Organotechnetium Compounds - chemical synthesis Organotechnetium Compounds - chemistry Organotechnetium Compounds - pharmacokinetics Penicillamine - analogs & derivatives Penicillamine - chemical synthesis Penicillamine - chemistry Penicillamine - pharmacokinetics Prostatic Neoplasms - metabolism Rats Rats, Wistar Technetium - chemistry Tissue Distribution |
| title | 99mTc-d-penicillamine-glucuronide: synthesis, radiolabeling, in vitro and in vivo evaluation |
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