Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.2.1.21 (beta-glucosidase)
 3,280 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A procedure for the estimation of D- and D,L-amygdalin in urine is described. Amygdalin is hydrolyzed by beta-glucosidase and base to benzaldehyde, glucose and cyanide. Benzaldehyde is extracted with methylene chloride and the ultraviolet (UV) absorbence determined at 243 nm. The response of human urine "spiked" with amygdalin was linear between 10 and 75 microgram/ml. Mice administered 100 mg/kg of amygdalin intravenously or orally excreted about 70 and 20% of the administered dose, respectively, over 96 hours. In each instance more than 96% of excreted drug equivalents were obtained within the first 24 hours.
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PMID:A simple method for the estimation of amygdalin in the urine. 56 46

Amygdalin MF was evaluated alone and in combination with an activating agent, beta-glucosidase, against three transplantable rodent tumors; Ridgway osteogenic sarcoma, Lewis lung carcinoma, and P388 leukemia. In dose-response studies up to the LD20 in normal mice, amygdalin MF alone did not demonstrate significant antitumor activity against any of these three tumor systems. Similarly, at doses not exceeding the LD10 in normal mice, amygdalin MF plus beta-glucosidase did not demonstrate antitumour activity against any of these three tumor systems. Potentiation of the lethal toxicity of amygdalin MF by beta-glucosidase was observed in all studies where the two agents were given in simultaneous combination.
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PMID:Experimental studies of the antitumor activity of amygdalin MF (NSC-15780) alone and in combination with beta-glucosidase (NSC-128056). 106 May 11

Experiments are described in which four transplantable rodent tumors (L1210 lymphoid leukemia, P388 lymphocytic leukemia, B16 melanoma, and Walker 256 carcinosarcoma) were used to investigate the antitumor activity of amygdalin MF. Amygdalin MF was given alone and in combination with beta-glucosidase which was administered 1/2 hour prior to amygdalin MF, starting 24 hours after tumor implantation. No antitumor activity was observed in any of the four tumor systems tested with the drug alone or in combined therapy. The combined therapy showed potentiation of toxicity with doses of amygdalin MF greater than or equal to 100 mg/kg.
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PMID:Antitumor activity of amygdalin MF (NSC-15780) as a single agent and with beta-glucosidase (NSC-128056) on a spectrum of transplantable rodent tumors. 120 98

The mean lethal dose (LD50) of amygdalin in rats was found to be 880 mg/kg body weight (BW) by oral administration. However, when 600 mg/kg BW was administered orally with beta-glucosidase, all the rats died. Total and Mg ATPase activities of the heart decreased with increasing levels of administered amygdalin. When 200 mg/kg BW amygdalin was administered 2.3 mg (11.7% of the dose) was excreted intact over 48 h. Amygdalin, 7.4 mg (18.5% of the dose) was excreted when the dose was 400 mg/kg BW, while 7.5 mg (12.4% of the dose) was excreted as intact amygdalin when the dosage was increased to 600 mg/kg BW. Thiocyanate excreted within the same 48-h period was 7.0, 9.1, and 9.5 mumol representing 18, 11.2, and 7.8% of the 200, 400, and 600 mg/kg BW oral dosage, respectively. With 300 mg/kg BW amygdalin administered intraperitoneally, 4.1 mg amygdalin and 3.9 mumol thiocyanate representing 13.7 and 6.5% of the dose, respectively, was excreted. Excretion of intact amygdalin and thiocyanate was uniform when the dose was low (200 mg), but with higher doses over 70% of the excreted products were detected in the urine during the first 24 h.
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PMID:On the metabolism of amygdalin. 1. The LD50 and biochemical changes in rats. 293 6

The evidence for the claims that laetrile (amygdalin) can prevent or control cancers has been reviewed. The beta-glucosidase content of cancer tissues is low compared to that of normal liver and small intestine. Cancer tissues contain the enzyme rhodanese in amounts comparable to that of liver and kidney and hence, cannot be attacked selectively by cyanide release through beta-glucosidase action on amygdalin. Amygdalin does not have the properties of a vitamin. Rats have been reared for several generations on diets devoid of cyanogenic glycosides, without developing neoplasms. Experiments with tumor-bearing rodents have demonstrated no curative properties by amygdalin administration. Amygdalin is not as non-toxic as claimed, particularly when ingested orally, and especially when taken with plant material high in beta-glucosidase. The claims for cure and control of cancers in humans have been refuted by distinguished physicians who specialize in the treatment of cancer patients. The writings of laetrile proponents are filled with erroneous and absurd statements. The propaganda for the doctrine of "freedom of choice in cancer treatment" deludes many individuals with treatable cancer to reject proven methods of treatment.
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PMID:The case against laetrile: the fraudulent cancer remedy. 698 71

We describe a novel version of antibody-directed enzyme prodrug therapy (ADEPT), with the use of amygdalin as prodrug. Amygdalin is a naturally occurring cyanogenic glycoside, which can be cleaved by sweet almond beta-glucosidase to yield free cyanide. If amygdalin could be activated specifically at the tumour site, then malignant cells would be killed without the systemic toxicity usually associated with chemotherapy. To this end, we have conjugated beta-glucosidase to a tumour-associated monoclonal antibody (MAb) (HMFG1) and the conjugate has been tested in vitro for specificity and cytotoxicity subsequent to activation of amygdalin. Amygdalin was cytotoxic to HT1376 bladder cancer cells only at high concentrations, whereas the combination of amygdalin with HMFG1-beta-glucosidase enhanced the cytotoxic effect of amygdalin by 36-fold. When 2 concentrations of HMFG1-beta-glucosidase were compared, the toxic effect was dose dependent. The cytotoxicity of amygdalin was also enhanced by the MAb-enzyme conjugate even when the unbound conjugate was removed from the medium prior to exposure to amygdalin and the cells were washed. In addition to the cytotoxic effect, we also demonstrated specificity, using a MAb-enzyme conjugate that does not recognise the HT1376 bladder cancer cells. Finally, we studied the cytotoxic effect of the conjugate in co-culture of HMFG1-positive and-negative cell lines (HT 1376 and U87MG cells). We demonstrated that the rate of surviving cells corresponds well to the percentage of U87MG (HMFG1-negative) cells in the flask. Our findings indicate that ADEPT is more effective than non-directed enzyme activation of a prodrug and can result in a non-toxic cancer therapy.
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PMID:In vitro cytotoxicity following specific activation of amygdalin by beta-glucosidase conjugated to a bladder cancer-associated monoclonal antibody. 983 64

Tonin(Persicae Semen) is the herb medicine that contains amygdalin as a major ingredient. Amygdalin in water is decomposed into benzaldehyde, HCN, and glucose by emulsin, a hydrolysis enzyme in tonin. A useful and practical method for the optimum extraction condition of amygdalin without enzymatic hydrolysis is required. The extraction yield of amygdalin of natural formula tonin was 0.1% from crude powders, 1.4% from small pieces, 3.5% from half pieces and 2.4% from whole pieces. The extraction yield of amygdalin of outer shell-eliminated tonin was 0.3% from crude powders, 1.4% from small pieces, and 3.5% from half pieces and whole pieces respectively. The extraction yield of amygdalin was most high when using the size larger than half.
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PMID:Development of quantitative extraction method of amygdalin without enzymatic hydrolysis from tonin(Persicae Semen) by high performance liquid chromatography. 1221 55