Abstract：
:Inflammatory cytokines and human immunodeficiency virus type 1 (HIV-1) gp120 are considered to play an important role in the pathogenesis of HIV-1-associated CNS disorders. These substances are produced predominantly by HIV-1-infected or activated macrophages and microglia in the brain and induce neural cell death. Cepharanthine is a biscoclaurine alkaloid isolated from Stephania cepharantha Hayata and has been shown to have anti-inflammatory, anti-allergic, and immunomodulatory activities in vivo. We previously reported that this compound could inhibit tumor necrosis factor (TNF)-alpha- or phorbol 12-myristate 13-acetate-induced HIV-1 replication in latently infected U1 cells through the inhibition of nuclear factor-kappaB, a potent inducer of HIV-1 gene expression. In the present study, we demonstrated that cepharanthine suppresses the production of inflammatory cytokines and a chemokine, i.e. TNF-alpha, interleukin (IL)-1beta, IL-6, and IL-8, in human monocytic cell cultures, including primary monocyte/macrophage cultures. This effect of cepharanthine was concentration-dependent, and significant suppression was observed at 0.1 microg/mL. Furthermore, the compound also inhibited TNF-alpha- and gp120-induced death of differentiated human neuroblastoma cells at a concentration of 0.04 to 0.2 microg/mL. It penetrates the blood-brain barrier, and a medicine containing cepharanthine as a major component has been used in Japan for the treatment of patients with chronic inflammatory diseases. Thus, cepharanthine should be investigated further for its therapeutic and prophylactic potential in HIV-1-associated CNS disorders.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Okamoto M,Ono M,Baba Mdoi
10.1016/s0006-2952(01)00692-xsubject
Has Abstractpub_date
2001-09-15 00:00:00pages
747-53issue
6eissn
0006-2952issn
1873-2968pii
S0006-2952(01)00692-Xjournal_volume
62pub_type
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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更新日期：1991-06-21 00:00:00
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pub_type： 杂志文章
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更新日期：1994-07-05 00:00:00
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doi：10.1016/s0006-2952(99)00369-x
更新日期：2000-03-15 00:00:00
