Anti-retroviral activity of lavendamycin analogs

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dc.contributor.advisor Behforouz, Nancy en_US
dc.contributor.author Wang, Aiqin en_US
dc.date.accessioned 2011-06-03T19:37:31Z
dc.date.available 2011-06-03T19:37:31Z
dc.date.created 1996 en_US
dc.date.issued 1996
dc.identifier LD2489.Z78 1996 .W36 en_US
dc.identifier.uri http://cardinalscholar.bsu.edu/handle/handle/185633
dc.description.abstract Lavendamycin, an aminoquinolinedione antibiotic is similar to streptonigrin, an antibiotic with known antiretroviral activity. Their applicability as drugs is limited due to their high toxicity to mammalian cells. A series of novel analogs of lavendamycin has been recently synthesized. In initial screening, three of the analogs showed significant inhibitory activity toward the reverse transcriptase (RT) of the avian myeloblastosis virus (AMV) and exhibited little or no animal toxicity and relatively low cellular cytotoxicity.In this study, we determined the anti-retroviral activity of nine analogs by assessing their anti-reverse transcriptase(anti-RT) activity in comparison to streptonigrin. Using both the human immunodeficiency virus (HIV) and AMV reverse transcriptase in vitro we found that the analogs exhibited significant anti-RT activity. The inhibitory activity of the analogs was dose dependent, and they had different effects on the two enzymes. At 30 µM seven of the analogs inhibited HIV-RT activity by 50% or more. At this concentration, two of the analogs were significantly more effective than streptonigrin. AMV-RT was more sensitive toward both streptonigrin and several of the analogs than was HIV-RT. Furthermore, combination of azidothymidine (AZT)-triphosphate (TP) and several of analogs showed synergistic inhibitory effects at low doses.
dc.description.sponsorship Department of Biology
dc.format.extent v, 82 leaves : ill. ; 28 cm. en_US
dc.source Virtual Press en_US
dc.subject.lcsh Antineoplastic antibiotics -- Testing. en_US
dc.subject.lcsh Esters. en_US
dc.subject.lcsh Retroviruses. en_US
dc.subject.lcsh HIV infections -- Treatment. en_US
dc.title Anti-retroviral activity of lavendamycin analogs en_US
dc.description.degree Thesis (M.S.)
dc.identifier.cardcat-url http://liblink.bsu.edu/catkey/1036177 en_US


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  • Master's Theses [5510]
    Master's theses submitted to the Graduate School by Ball State University master's degree candidates in partial fulfillment of degree requirements.

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