beta glucuronidase/neoplasms

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Induction of β-glucuronidase release by cytostatic agents in small tumors.

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Extracellular β-glucuronidase (β-GUS) in tumors has been investigated as a target enzyme for prodrug therapy. However, despite encouraging preclinical results, animal studies also indicate that the success of prodrug therapy might be limited by the insufficient prodrug-converting enzyme activity,

Comparison of two anthracycline-based prodrugs for activation by a monoclonal antibody-beta-glucuronidase conjugate in the specific treatment of cancer.

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Antibody-directed enzyme prodrug therapy (ADEPT) may improve the therapeutic index of cytostatic agents. We compared two prodrugs, epirubicin-glucuronide (Epi-glu) and doxorubicin-spacer-glucuronide (Dox-sp-glu), for their cytotoxicity on activation by a monoclonal antibody-enzyme conjugate bound to

Soy Saponins Meditate the Progression of Colon Cancer in Rats by Inhibiting the Activity of β -Glucuronidase and the Number of Aberrant Crypt Foci but Not Cyclooxygenase-2 Activity.

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Objective. The effect of extracted crude soybean saponins on preneoplastic lesions, aberrant crypt foci (ACF), and the related mechanism were investigated. Research Methods and Procedures. Rats were assigned into five groups according to different doses of extracted crude soybean saponins and

[A study on activity of beta-glucuronidase in serum and secretion from upper respiratory tract in patients with head and neck malignant tumors].

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Beta-glucuronidase (beta-GD) activity in serum and upper respiratory tract (URT) secretion in patients with head and neck malignant tumors (HNMT) was studied. Subjects included 40 HNMT patients, 40 healthy volunteers and 40 patients with benign tumors of the head and neck region. The results showed

Therapeutic trial of aniline mustard in patients with advanced cancer. Comparison of therapeutic response with cytochemical assessment of tumor cell beta-glucuronidase activity.

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Seventy-eight patients with advanced cancer received an adequate therapeutic trial with aniline mustard (NSC 18429). Significant anticancer activity with clinical benefit was demonstrated in five patients with cancer of the prostate and one patient with renal cancer. beta-glucuronidase levels in

A minimal toxicity approach to cancer therapy: possible role of beta-glucuronidase.

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Most cancer cells differ from normal cells in that they show higher beta-glucuronidase activity and lower pH of their cytoplasm. Anti-cancer drugs can be designed which take advantage of these gradients to deliver maximal toxicity to tumors and minimal toxicity to normal tissue. Many design criteria

Enhanced uptake of doxorubicin into bronchial carcinoma: beta-glucuronidase mediates release of doxorubicin from a glucuronide prodrug (HMR 1826) at the tumor site.

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Lack of tumor selectivity is a severe limitation of cancer chemotherapy. Consequently, reducing dose-limiting organ toxicities such as the cardiac toxicity of doxorubicin (Dox) is of major clinical relevance. Approaches that would facilitate a more tumor-selective anticancer therapy by using

Enhancement of CPT-11 antitumor activity by adenovirus-mediated expression of β-glucuronidase in tumors.

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CPT-11 is a clinically important prodrug that requires conversion into the active metabolite SN-38, a potent topoisomerase I poison, for antitumor activity. However, SN-38 is rapidly metabolized to the inactive SN-38 glucuronide (SN-38G) in the liver, which reduces the amount of SN-38 available for

Dose optimization of a doxorubicin prodrug (HMR 1826) in isolated perfused human lungs: low tumor pH promotes prodrug activation by beta-glucuronidase.

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HMR 1826 (N-[4-beta-Glucuronyl-3-nitrobenzyl-oxycarbonyl]doxorubicin) is a nontoxic glucuronide prodrug from which active doxorubicin is released by beta-glucuronidase. Preclinical studies aimed at dose optimization of HMR 1826, based on intratumoral pharmacokinetics, are important to design

Selective and augmented β-glucuronidase expression combined with DOX-GA3 application elicits the potent suppression of prostate cancer.

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The present study was carried out to evaluate the specific and amplified β-glucuronidase (βG) expression in prostate cancer cells by using a prostate‑specific antigen (PSA) promoter-controlled bicistronic adenovirus and to evaluate the specific killing of prostate cancer cells after the application

Enterolactone glucuronide and β-glucuronidase in antibody directed enzyme prodrug therapy for targeted prostate cancer cell treatment.

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Evidence from preclinical and animal studies demonstrated an anticancer effect of flaxseed lignans, particularly enterolactone (ENL), against prostate cancer. However, extensive first-pass metabolism following oral lignan consumption results in their systemic availability primarily as glucuronic

Facile and ultrasensitive fluorescence sensor platform for tumor invasive biomaker β-glucuronidase detection and inhibitor evaluation with carbon quantum dots based on inner-filter effect.

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Early detection and diagnosis have great practical significances for the effective prevention and treatment of cancer. In this study, we developed a novel, facile and ultra-sensitive fluorescence assay for the determination of tumor invasive biomarker β-glucuronidase (GLU) based on the inner-filter

Effect of Cocos nucifera and red chilli on intestinal b-glucuronidase and mucinase activity in experimental colon cancer.

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Effect of Cocos nucifera and red chilli on intestinal B-glucuronidase and faecal mucinase activity, was studied in rats given 1 ,2-dimethylhydrazine (DMH) . The average weight gain by the animals given coconut kernel was more than the DMH and chilli treated groups. The activity of B-glucuronidase

Synthesis of pyrimidine-2,4,6-trione derivatives: Anti-oxidant, anti-cancer, α-glucosidase, β-glucuronidase inhibition and their molecular docking studies.

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This paper describes a facile protocol, efficient, and environmentally benign for the synthesis a series of barbiturate acid substituted at C5 position 3a-o. The desired compounds subjected in vitro for different set of bioassays including against anti-oxidant (DPPH and super oxide scavenger

β-Glucuronidase-responsive prodrugs for selective cancer chemotherapy: an update.

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The design of novel antitumor agents allowing the destruction of malignant cells while sparing healthy tissues is one of the major challenges in medicinal chemistry. In this context, the use of non-toxic prodrugs programmed to be selectively activated by beta-glucuronidase present at high

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