Abstract Hyperacidified tumors having high β-glucuronidase activity can be treated with glucuronides with aglycones toxic to the tumor cells with great safety toward the rest of the body by first administering an alkalinizing agent in an amount sufficient to maintain the pH level of non-tumor tissues at approximately 7.4 during the glucuronide treatment. This will cause inactivation of β-glucuronidase activity in the rest of the body. Novel glucuronides are disclosed the aglycones of which exert a higher toxic effect in an acid environment or is water-soluble only in an alkaline environment. Such compounds have particular utility with the above process. By substituting radioisotopes into the aglycone, diagnosis and in situ radiation therapy may be accomplished. Bacterial cells having β-glucuronidase activity may also be diagnosed and treated in accordance with the present invention. A urine test is disclosed to determine the amount of free glucuronic acid in the urine which is an indication of the presence of a tumor in the body having high β-glucuronidase activity.
A process for treating infections caused by bacteria having β-glucuronidase activity, comprising: intravenously or orally administering to the patient an alkalinizing agent in an amount sufficient to maintain the pH of the internal tissues of the patient at a level of approximately 7.4; and parenterally administering a glucuronide compound, the aglycone of which is toxic to bacterial cells, in an anti-bacteria effective amount, whereby the β-glucuronidase activity of the bacterial cells causes deconjugation of the glucuronide at the site of the infection and release of the aglycone thereat.
Claim 2
Dependent Claim
88 words
A process for treating infections caused by bacteria having β-glucuronidase activity, comprising: intravenously or orally administering to the patient an alkalinizing agent in an amount sufficient to maintain the pH of the internal tissues of the patient at a level of approximately 7.4; and parenterally administering a glucuronide compound, the aglycone of which is toxic to bacterial cells, in an anti-bacteria effective amount, whereby the β-glucuronidase activity of the bacterial cells causes deconjugation of the glucuronide at the site of the infection and release of the aglycone thereat.
Claim 3
Dependent Claim
19 words
A process in accordance with claim 1, wherein said bacterial infection comprises an infection of streptococci, staphylococci, or E-coli.
Claim 4
Dependent Claim
87 words
A process for the diagnosis of the presence of bacterial cells having β-glucuronidase activity, comprising: intravenously or orally administering to the patient an alkalinizing agent in an amount sufficient to maintain the pH of the patient at a level of approximately 7.4; parenterally administering glucuronide compound the aglycone of which contains a radioisotope capable of emitting sufficient radiation to be detected by a full body radiation scan; and scanning the entire body of the patient to determine the presence and location of any radioactive aglycone immobilized therein.
Claim 5
Dependent Claim
87 words
A process for the diagnosis of the presence of bacterial cells having β-glucuronidase activity, comprising: intravenously or orally administering to the patient an alkalinizing agent in an amount sufficient to maintain the pH of the patient at a level of approximately 7.4; parenterally administering glucuronide compound the aglycone of which contains a radioisotope capable of emitting sufficient radiation to be detected by a full body radiation scan; and scanning the entire body of the patient to determine the presence and location of any radioactive aglycone immobilized therein.