Linked Life Data

11900350

Source:http://linkedlifedata.com/resource/pubmed/id/11900350

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
5
pubmed:dateCreated
2002-3-19
pubmed:abstractText
Cepharanthine (12-O-methyl cepharanoline) is a plant alkaloid and has been shown to inhibit tumour necrosis factor-alpha- or phorbol 12-myristate 13-acetate-induced HIV-1 replication in the chronically infected promonocytic cell line, U1. Its mechanism of action is considered to be the inhibition of nuclear factor kappaB, a potent inducer of HIV-1 gene expression. In this study, we have synthesized 96 derivatives of cepharanoline, including cepharanthine, and examined their inhibitory effects on HIV-1 replication in U1 cells. Among the 12-O-alkyl derivatives, cepharanthine proved to be the most active, and the activity decreased as the length of the alkyl chain increased. All of the 12-O-acyl derivatives were totally inactive, while a few 12-O-carbamoyl derivatives displayed modest activity. Since 12-O-ethyl derivatives were found to be as active as cepharanthine against HIV-1 replication, we further synthesized various 12-O-ethyl derivatives of cepharanoline. Among the derivatives, five proved to be more active inhibitors than cepharanthine, and the most active compound was 12-O-ethylpiperazinyl cepharanoline. The 50% effective concentrations of this compound and cepharanthine were 0.0041 and 0.028 microg/ml (0.0060 and 0.046 microM), respectively.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0956-3202
pubmed:author
pubmed:issnType
Print
pubmed:volume
12
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
307-12
pubmed:dateRevised
2008-11-21
pubmed:meshHeading
pubmed:year
2001
pubmed:articleTitle
Anti-HIV-1 activity and structure-activity relationship of cepharanoline derivatives in chronically infected cells.
pubmed:affiliation
Division of Human Retroviruses, Center for Chronic Viral Diseases, Faculty of Medicine, Kagoshima University, Japan. baba@m.kufm.kagoshima-u.ac.jp
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't