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Updated: Jul 17, 2026
07:20
Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
The study of possibility to elevate antitumor activity and decrease of systemic toxic effects of cisplatin by its
L A Sakhno1, V V Sarnatskaya, L A Yushko
1Department of Physico-chemical Mechanisms of Sorption Detoxification, R.E. Kavetsky Institute of Experimental Pathology, Oncology and Radiobiology, NAS of Ukraine, Kyiv, Ukraine. lara7@onconet.kiev.ua
Experimental Oncology
|February 8, 2007
Summary
Cisplatin bound to deliganded albumin (CP-dHSA) enhances antitumor effects against Guerin carcinoma and reduces toxicity compared to cisplatin alone. This novel complex offers improved cancer treatment potential.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Background:
- Cisplatin (CP) is a widely used chemotherapy drug.
- Albumin is a potential carrier for drug delivery.
- Understanding CP-albumin interactions is crucial for optimizing cancer therapy.
Purpose of the Study:
- To evaluate the antitumor and toxic effects of cisplatin (CP) alone and complexed with deliganded albumin (dHSA).
- To investigate the complex formation between CP and albumin.
- To assess the efficacy and safety of a novel CP-dHSA complex.
Main Methods:
- Complex formation studied using differential scanning and isothermic flow microcalorimetry.
- Albumin-bound CP quantified via ultrafiltration.
- Platinum concentration determined by atomic-absorption spectral analysis.
- In vivo antitumor and toxic effects evaluated in a Guerin carcinoma (GC) model.
Main Results:
- Cisplatin binds to the III domain of albumin.
- Deliganded albumin (dHSA) exhibits enhanced complex-forming ability with CP.
- The CP-dHSA complex demonstrated superior Guerin carcinoma growth inhibition compared to CP alone.
- CP-dHSA administration resulted in a 15% increase in blood creatinine, versus 40% for CP.
Conclusions:
- The CP-dHSA complex enhances antitumor activity.
- The CP-dHSA complex reduces the toxic effects of cisplatin.
- CP-dHSA is a promising therapeutic complex for cancer treatment.
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