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Phenylthioalkylamines in experimental tumor treatment in mice
Abstract:
Two phenylthioalkylamines, phenylthioethylamine (PTEA) and phenylthiopropylamine (PTPA), were prepared and tested for cytotoxicity in vitro and as antitumor agents in (C57BL X DBA/2)F1 (BDF1) mice. Low concentrations of PTEA (median effective concentrations of 8.0, 12.0, and 1.3 micrograms PTEA/ml) inhibited the growth of P388 murine lymphoma, L1210 leukemia, and B16 melanoma cells in culture. PTPA was more effective; concentrations of 0.80, 0.56, and 0.35 micrograms PTPA/ml inhibited the growth of P388, L1210, and B16 in vitro by 50%. PTEA and PTPA treatment increased survival times in BDF1 mice bearing the P388 lymphoma, L1210 leukemia, B16 melanoma, and Lewis lung tumors. Multiple daily administrations of the test compounds were more effective than single daily injections in increasing the life-span in mice bearing the P388 lymphoma and B16 melanoma. Both PTEA and PTPA inhibited the enzyme copper-zinc superoxide dismutase.
Insights
Phenylthioethylamine (PTEA) and phenylthiopropylamine (PTPA) show promising antitumor activity against various cancers in vitro and in vivo. These compounds effectively inhibited tumor cell growth and increased survival rates in mice, suggesting therapeutic potential.
Area of Science:
- Pharmacology
- Medicinal Chemistry
- Oncology
Background:
- Phenylthioalkylamines are a class of compounds with potential biological activity.
- Superoxide dismutase is an enzyme involved in cellular protection against oxidative stress.
Purpose of the Study:
- To evaluate the in vitro cytotoxicity and in vivo antitumor efficacy of phenylthioethylamine (PTEA) and phenylthiopropylamine (PTPA).
- To investigate the effect of PTEA and PTPA on survival rates in tumor-bearing mice.
Main Methods:
- In vitro cytotoxicity assays were performed on P388 murine lymphoma, L1210 leukemia, and B16 melanoma cell lines.
- In vivo antitumor activity was assessed in (C57BL X DBA/2)F1 (BDF1) mice bearing various tumors.
- Enzyme inhibition assays were conducted for copper-zinc superoxide dismutase.
Main Results:
- Both PTEA and PTPA demonstrated significant inhibition of tumor cell growth in vitro, with PTPA being more potent.
- Treatment with PTEA and PTPA increased survival times in mice with P388 lymphoma, L1210 leukemia, B16 melanoma, and Lewis lung tumors.
- Multiple daily administrations were more effective than single injections for certain tumor models.
- Both compounds were found to inhibit copper-zinc superoxide dismutase activity.
Conclusions:
- Phenylthioethylamine (PTEA) and phenylthiopropylamine (PTPA) exhibit significant antitumor properties.
- The observed efficacy suggests potential for these compounds as novel anticancer agents.
- Further research is warranted to explore their therapeutic applications and mechanisms of action.