Inhibition of thymidylate synthase by pergularinine, tylophorinidine and deoxytubulosine
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Title |
Inhibition of thymidylate synthase by pergularinine, tylophorinidine and deoxytubulosine
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Creator |
Rao, K Narasimha
Bhattacharya, R K Veankatachalam, S R |
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Description |
442-448
The activity of thymidylate synthase (TS) purified in our laboratory from Lactobacillus leichmannii was inhibited by pergularinine (PGL) and tylophorinidine (TPD) and deoxytubulosine (DTB) isolated froml the Indian medicine plants Pergularia pallida and Alanguml lamarckii respectively. Cytotoxicity studies showed that cell growth of L. leichmannii was inhibited (IC50) = 40-45 μM) by all the three alkaloids, the concentrations > 80-90 μM resulting in complete loss of the enzyme activit y. Ki values of the enzyme calculated from Lineweaver-Burk and Dixon plots for PGL, TPD and DTB were l0× 10-6M, 9× 10-6M and 7× 10-6M respectively. These are typed as ‘non-competitive’ inhibitors of TS. All the three alkaloids, inhibited (IC50 = 50 μM) the elevated TS activity of leukocytes in cancer patients with clinically diagnosed chronic myelocytic leukemia (n= 10), acute lymphocytic leukemia (n=8) and metastatic solid tumours (n=3). |
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Date |
2012-12-31T20:09:49Z
2012-12-31T20:09:49Z 1999-12 |
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Type |
Article
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Identifier |
0975-0959 (Online); 0301-1208 (Print)
http://hdl.handle.net/123456789/15477 |
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Language |
en_US
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Rights |
CC Attribution-Noncommercial-No Derivative Works 2.5 India
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Publisher |
NISCAIR-CSIR, India
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Source |
IJBB Vol.36(6) [December 1999]
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