In Vitro Evaluation of a Stable Monomeric Gold(II) Complex with Hematoporphyrin IX: Cytotoxicity against Tumor and Kidney Cells, Cellular Accumulation, and Induction of Apoptosis
The antineoplastic potential of a stable monomeric Au(II) complex with hematoporphyrin IX (Hp), namely [Au(II)Hp-2H.(H2O)2], was investigated in a panel of tumor cell lines. The complex exhibits strong cytotoxicity, whereby the leukaemia- and lymphoma-derived cell lines are more sensitive, with IC50...
Saved in:
| Main Authors: | , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Wiley
2008-01-01
|
| Series: | Bioinorganic Chemistry and Applications |
| Online Access: | http://dx.doi.org/10.1155/2008/367471 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| _version_ | 1832562150917275648 |
|---|---|
| author | Georgi Momekov Dilyan Ferdinandov Spiro Konstantinov Sonja Arpadjan Daniela Tsekova Galina Gencheva Panayot R. Bontchev Margarita Karaivanova |
| author_facet | Georgi Momekov Dilyan Ferdinandov Spiro Konstantinov Sonja Arpadjan Daniela Tsekova Galina Gencheva Panayot R. Bontchev Margarita Karaivanova |
| author_sort | Georgi Momekov |
| collection | DOAJ |
| description | The antineoplastic potential of a stable monomeric Au(II) complex with hematoporphyrin IX (Hp), namely [Au(II)Hp-2H.(H2O)2], was investigated in a panel of tumor cell lines. The complex exhibits strong cytotoxicity, whereby the leukaemia- and lymphoma-derived cell lines are more sensitive, with IC50 values comparable to those of the reference anticancer drug cisplatin. In contrast, the solid tumor models are more sensitive to the platinum drug. A comparative assessment of both agents against the human kidney cell line 293T has shown that [Au(II)Hp-2H.(H2O)2] is less cytotoxic. The gold complex induces oligonucleosomal DNA fragmentation in tumour cells following 24-hour treatment and hence its cytotoxic effect is at least partly mediated by induction of apoptotic cell death. A prominent intracellular gold accumulation was detected after treating tumor cells with [Au(II)Hp-2H.(H2O)2] which shows that its putative pharmacological targets are readily accessible after a short incubation period. |
| format | Article |
| id | doaj-art-342c0a9fcfb44d518776dd13edb81ff8 |
| institution | Kabale University |
| issn | 1565-3633 1687-479X |
| language | English |
| publishDate | 2008-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Bioinorganic Chemistry and Applications |
| spelling | doaj-art-342c0a9fcfb44d518776dd13edb81ff82025-02-03T01:23:18ZengWileyBioinorganic Chemistry and Applications1565-36331687-479X2008-01-01200810.1155/2008/367471367471In Vitro Evaluation of a Stable Monomeric Gold(II) Complex with Hematoporphyrin IX: Cytotoxicity against Tumor and Kidney Cells, Cellular Accumulation, and Induction of ApoptosisGeorgi Momekov0Dilyan Ferdinandov1Spiro Konstantinov2Sonja Arpadjan3Daniela Tsekova4Galina Gencheva5Panayot R. Bontchev6Margarita Karaivanova7Laboratory of Molecular Pharmacology and Experimental Chemotherapy, Department of Pharmacology, Pharmacotherapy, and Toxicology, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav Street, 1000 Sofia, BulgariaLaboratory of Molecular Pharmacology and Experimental Chemotherapy, Department of Pharmacology, Pharmacotherapy, and Toxicology, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav Street, 1000 Sofia, BulgariaLaboratory of Molecular Pharmacology and Experimental Chemotherapy, Department of Pharmacology, Pharmacotherapy, and Toxicology, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav Street, 1000 Sofia, BulgariaDepartment of Analytical Chemistry, Faculty of Chemistry, “St. Kliment Ohridsky” University of Sofia, 1 J. Bourchier Boulevard, 1164 Sofia, BulgariaDepartment of Analytical Chemistry, Faculty of Chemistry, “St. Kliment Ohridsky” University of Sofia, 1 J. Bourchier Boulevard, 1164 Sofia, BulgariaDepartment of Analytical Chemistry, Faculty of Chemistry, “St. Kliment Ohridsky” University of Sofia, 1 J. Bourchier Boulevard, 1164 Sofia, BulgariaDepartment of Analytical Chemistry, Faculty of Chemistry, “St. Kliment Ohridsky” University of Sofia, 1 J. Bourchier Boulevard, 1164 Sofia, BulgariaLaboratory of Molecular Pharmacology and Experimental Chemotherapy, Department of Pharmacology, Pharmacotherapy, and Toxicology, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav Street, 1000 Sofia, BulgariaThe antineoplastic potential of a stable monomeric Au(II) complex with hematoporphyrin IX (Hp), namely [Au(II)Hp-2H.(H2O)2], was investigated in a panel of tumor cell lines. The complex exhibits strong cytotoxicity, whereby the leukaemia- and lymphoma-derived cell lines are more sensitive, with IC50 values comparable to those of the reference anticancer drug cisplatin. In contrast, the solid tumor models are more sensitive to the platinum drug. A comparative assessment of both agents against the human kidney cell line 293T has shown that [Au(II)Hp-2H.(H2O)2] is less cytotoxic. The gold complex induces oligonucleosomal DNA fragmentation in tumour cells following 24-hour treatment and hence its cytotoxic effect is at least partly mediated by induction of apoptotic cell death. A prominent intracellular gold accumulation was detected after treating tumor cells with [Au(II)Hp-2H.(H2O)2] which shows that its putative pharmacological targets are readily accessible after a short incubation period.http://dx.doi.org/10.1155/2008/367471 |
| spellingShingle | Georgi Momekov Dilyan Ferdinandov Spiro Konstantinov Sonja Arpadjan Daniela Tsekova Galina Gencheva Panayot R. Bontchev Margarita Karaivanova In Vitro Evaluation of a Stable Monomeric Gold(II) Complex with Hematoporphyrin IX: Cytotoxicity against Tumor and Kidney Cells, Cellular Accumulation, and Induction of Apoptosis Bioinorganic Chemistry and Applications |
| title | In Vitro Evaluation of a Stable Monomeric Gold(II) Complex with Hematoporphyrin IX: Cytotoxicity against Tumor and Kidney Cells, Cellular Accumulation, and Induction of Apoptosis |
| title_full | In Vitro Evaluation of a Stable Monomeric Gold(II) Complex with Hematoporphyrin IX: Cytotoxicity against Tumor and Kidney Cells, Cellular Accumulation, and Induction of Apoptosis |
| title_fullStr | In Vitro Evaluation of a Stable Monomeric Gold(II) Complex with Hematoporphyrin IX: Cytotoxicity against Tumor and Kidney Cells, Cellular Accumulation, and Induction of Apoptosis |
| title_full_unstemmed | In Vitro Evaluation of a Stable Monomeric Gold(II) Complex with Hematoporphyrin IX: Cytotoxicity against Tumor and Kidney Cells, Cellular Accumulation, and Induction of Apoptosis |
| title_short | In Vitro Evaluation of a Stable Monomeric Gold(II) Complex with Hematoporphyrin IX: Cytotoxicity against Tumor and Kidney Cells, Cellular Accumulation, and Induction of Apoptosis |
| title_sort | in vitro evaluation of a stable monomeric gold ii complex with hematoporphyrin ix cytotoxicity against tumor and kidney cells cellular accumulation and induction of apoptosis |
| url | http://dx.doi.org/10.1155/2008/367471 |
| work_keys_str_mv | AT georgimomekov invitroevaluationofastablemonomericgoldiicomplexwithhematoporphyrinixcytotoxicityagainsttumorandkidneycellscellularaccumulationandinductionofapoptosis AT dilyanferdinandov invitroevaluationofastablemonomericgoldiicomplexwithhematoporphyrinixcytotoxicityagainsttumorandkidneycellscellularaccumulationandinductionofapoptosis AT spirokonstantinov invitroevaluationofastablemonomericgoldiicomplexwithhematoporphyrinixcytotoxicityagainsttumorandkidneycellscellularaccumulationandinductionofapoptosis AT sonjaarpadjan invitroevaluationofastablemonomericgoldiicomplexwithhematoporphyrinixcytotoxicityagainsttumorandkidneycellscellularaccumulationandinductionofapoptosis AT danielatsekova invitroevaluationofastablemonomericgoldiicomplexwithhematoporphyrinixcytotoxicityagainsttumorandkidneycellscellularaccumulationandinductionofapoptosis AT galinagencheva invitroevaluationofastablemonomericgoldiicomplexwithhematoporphyrinixcytotoxicityagainsttumorandkidneycellscellularaccumulationandinductionofapoptosis AT panayotrbontchev invitroevaluationofastablemonomericgoldiicomplexwithhematoporphyrinixcytotoxicityagainsttumorandkidneycellscellularaccumulationandinductionofapoptosis AT margaritakaraivanova invitroevaluationofastablemonomericgoldiicomplexwithhematoporphyrinixcytotoxicityagainsttumorandkidneycellscellularaccumulationandinductionofapoptosis |