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  • Title: Selective toxicity of gossypol against epithelial tumors and its detection by magnetic resonance spectroscopy.
    Author: Benz C, Keniry M, Goldberg H.
    Journal: Contraception; 1988 Mar; 37(3):221-8. PubMed ID: 3370994.
    Abstract:
    The antitumor toxicity of gossypol was measured in 6 human carcinoma cell lines and compared with its toxicity against human bone marrow stem cells. Marrow cells were more resistant than any of the tumor cell lines, and tumor cell sensitivity depended on the content of intracellular LDH-M. [31P]-Magnetic resonance spectroscopy showed decline in tumor ATP levels occurring within 24 hours of treatment, suggesting that this non-invasive technique may serve as an early biochemical monitor of gossypol toxicity. The antiproliferative activity of gossypol was measured in 6 human carcinoma cell lines and compared with its toxicity against human bone narrow stem cells. Marrow cells were more resistant than any of the tumor cell lines, and tumor cell sensitivity depended on the content of intracellular lactate dehydrogenase (LDH)-M. Magnetic resonance spectroscopy showed a decline in tumor ATP levels occurring within 24 hours of treatment, suggesting that this noninvasive technique may serve as an early biochemical monitor of gossypol toxicity. The qualitative differences in mitochondria and cellular energy metabolism between normal and malignant cells represent a potential new target for selective chemotherapy. The antimitochondrial properties of gossypol may prove useful in treating proliferative epithelial tumors, especially those rich in cathodal LDH isozymes. Overall, these preclinical studies suggest that gossypol should be administered on the basis of an individual tumor's LDH isozyme profile and can be monitored by magnetic resonance spectroscopy for biochemical effectiveness within hours of its administration.
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