Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 5, Pages 2645-2650Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.11.041
Keywords
HBS; HIV-1; lignin; LTR; NF-kappa B; TNF-alpha
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Human immunodeficiency virus type 1 (HIV-1) is a cytopathic retrovirus and the primary etiological agent of acquired immunodeficiency syndrome (AIDS) and related disorders. In cells chronically infected with HIV-1, nuclear factor-kappa B (NF-kappa B) activation by external stimuli such as tumor necrosis factor alpha (TNF alpha) augments replication of HIV-1. NF-kappa B involves in many diseases such as inflammation, cancer, and. Crohn's disease. In this paper, we exhibit that (i) HIV-1 gene expression was inhibited by lignin, (ii) fraction of small molecular mass in HBS lignin (less than 0.5 kDa) had stronger inhibitory effects than large molecular mass (more than 1.3 kDa), (iii) lignin also inhibited activation of NF-kappa B induced by TNF alpha, (iv) among six lignin dimer-like compounds, compound 6 containing beta-5 bond has more potent inhibitory activity than compounds 1, 2, 3, 4 and 5, which contain beta-1, beta-O-4, 5-5, or beta-beta structural units. These results suggested that small molecules of lignin inhibit HIV-1 replication through suppression of HIV-1 transcription from LTR including activation via NF-kappa B. Low molecular lignin may be a beneficial material or drug leads as a new class for AIDS and NF-kappa B-related diseases. (C) 2008 Published by Elsevier Ltd.
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