Betulinic acid, a potent inhibitor of eukaryotic topoisomerase I: Identification of the inhibitory step, the major functional group responsible and development of more potent derivatives

Medical Science Monitor

Volumn 8, Issue 7, 2002, Pages

  Chowdhury, Arnab Roy ^a   Mandal, Suparna ^a   Mittra, Bidyottam ^a   Sharma, Shalini ^a   Mukhopadhyay, Sibabrata ^a   Majumder, Hemanta K ^a  

^a INDIAN INSTITUTE OF CHEMICAL BIOLOGY   (India)

Author keywords

Anti tumor compound; Betulinic acid; Catalytic Inhibitor; Cleavage antagonist; Topoisomerase I

Indexed keywords

ANTINEOPLASTIC AGENT; BETULIC ACID; CAMPTOTHECIN; DNA TOPOISOMERASE; DNA TOPOISOMERASE INHIBITOR; TRITERPENOID; DNA; DNA BINDING PROTEIN; ENZYME INHIBITOR; PLANT EXTRACT; TRITERPENE;

ANIMAL CELL; ANTIINFLAMMATORY ACTIVITY; ANTINEOPLASTIC ACTIVITY; ANTIVIRAL ACTIVITY; ARTICLE; CONTROLLED STUDY; DECARBOXYLATION; DNA CLEAVAGE; DRUG MECHANISM; DRUG POTENCY; ENZYME INHIBITION; IC 50; MOUSE; NONHUMAN; PROTEIN DNA INTERACTION; STRUCTURE ACTIVITY RELATION; ANIMAL; CHEMICAL STRUCTURE; CHEMISTRY; DRUG ANTAGONISM; HUMAN; ISOLATION AND PURIFICATION; MACROMOLECULE; METABOLISM; PROTEIN BINDING; RAT;

ANIMAL; ANTINEOPLASTIC AGENTS, PHYTOGENIC; CAMPTOTHECIN; DNA; DNA TOPOISOMERASES, TYPE I, EUKARYOTIC; DNA-BINDING PROTEINS; ENZYME INHIBITORS; HUMAN; MACROMOLECULAR SYSTEMS; MICE; MOLECULAR STRUCTURE; PLANT EXTRACTS; PROTEIN BINDING; RATS; SUPPORT, NON-U.S. GOV'T; TRITERPENES; ANIMALS; HUMANS; MACROMOLECULAR SUBSTANCES;

EID: 0036327903     PISSN: 12341010     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (29)

1. Anti-Aids Agents-XXVIII. Synthesis and anti HIV activity of betulinic acid and dihydro betulinic acid derivatives
2. Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis
3. Betulinic acid, isolation from Triphyophyllum peltatum and ancistrocladus heyneanus, antimalarial activity, and crystal structure of the benzyl ester
4. In vitro and in vivo evaluation of betulinic acid as antimalarial
5. Studies on the antiinflammatory activity of Nelumbo nucifera
6. Investigations on the steroidal anti-inflammatory activity of triterpenoids from diospyros Leucomelas
7. Sterol and triterpene derivatives from plants inhibit the effects of a tumor promoter, and sitosterol and betulinic acid inhibit tumor formation in mouse skin two-stage carcinogenesis
8. Betulinic acid induces apoptosis in human neuroblastoma call lines
9. Betulinic acid triggers CD95 (APO-I/Fas)-and p53 independent apoptosis via caspases in neuroectodermal tumors
10. Activation of mitochondria and release of mitochondrial apoptogenic factors by betulinic acid
11. Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I
12. Acetyl-11-keto-beta-boswellic acid induces apoptosis in HL-60 and CCRF-CEM cells and inhibits topoisomerase I
13. Acetyl-boswellic acids are novel catalytic inhibitors of human topoisomerase I ahd II Mol
14. Chemical examination of Bacopa monniera Wettst: Part I- Isolation of chemical constituents
15. The non alkaloidal constituents from the leaves of Alangium lamarckii Thw
16. Purification and Characterization of the DNA Untwisting Enzyme from Rat Liver
17. Diospyrin, a bisnapthaquinone: A novel inhibitor of type I DNA topoisomerase of Lesihmania donovani Mol
18. The characterization of a mammalian DNA structure-specific endonuclease
19. b-lapachone, a novel DNA topoisomerase I inhibitor with a Mode of Action Different from Camptothecin
20. DNA Damage by Antitumor Acridines Mediated by Mammalian DNA Topoisomerase II
21. ABA-specific response are I region restricted by the carriers used for immunization
22. Selected novel flavones inhibit the DNA binding or the DNA religation step of eukaryotic topoisomerase I
23. Differential actions of aclarubicin and doxorubicin: The role of topoisomerase I
24. Evidence for intercalation of chloroquine into DNA
25. Synthesis of betulinic acid derivatives with activity against human melanoma
26. Inhibitors of DNA topoisomerases
27. Topoisomerase-targeting antitumor drugs