title: A potential in vitro and in vivo anti-HIV drug screening system for Chinese herbal medicines.
abstract: Chinese herbal medicines are often applied as an alternative therapy for viral diseases. However, the development of anti-HIV herbal drugs has proceeded slowly, partly because of the lack of a high-throughput system for screening these drugs. The present study evaluated 16 herbal medicines for anti-HIV activities in vitro and in vivo. Herbal medicines were first screened for the ability to regulate C-X-C receptor 4 (CXCR4) and C-C receptor 5 (CCR5) promoter activities. A single-round pseudotyped HIV-luciferase reporter virus system (HIV-Luc) was used to identify potential anti-HIV mechanisms. CD4+ T cells from healthy volunteers were examined for changes in CXCR4 and CCR5 levels. HIV-1 replication was evaluated by ELISA. Spica Prunellae and Herba Andrographitis were found to down-regulate the activities of both the CXCR4 and CCR5 promoters. Also, Spica Prunellae and Herba Andrographitis (>1000 μM) inhibited HIV-1 in a dose-dependent manner. CXCR4 and CCR5 levels were reduced in CD4+ T cells from healthy volunteers (p<0.05). Spica Prunellae and Herba Andrographitis (EC₅₀: 3.18 and 5.49 μg/mL, respectively) could suppress cell fusion and decrease p24 antigen. In conclusion, the data demonstrated that Spica Prunellae and Herba Andrographitis possessed anti-HIV-1 capabilities, perhaps through the inhibition of the CXCR4 and CCR5 promoters and HIV-1 replication.
authors.affiliation: Department of Pathogenic Organism Biology, Henan University of TCM, Zhengzhou 450008, Henan, P.R. China.
authors.forename: Long
authors.initials: L
authors.lastname: Feng
authors.forename: Li
authors.initials: L
authors.lastname: Wang
authors.forename: Yun-yun
authors.initials: YY
authors.lastname: Ma
authors.forename: Min
authors.initials: M
authors.lastname: Li
authors.forename: Guo-Qiang
authors.initials: GQ
authors.lastname: Zhao
mesh_terms: D000328:Adult; D035685:Andrographis / Q000737:chemistry; D000818:Animals; D019380:Anti-HIV Agents / Q000494:pharmacology*; D065100:CCR5 Receptor Antagonists; D015496:CD4-Positive T-Lymphocytes / Q000378:metabolism / Q000821:virology; D002470:Cell Survival; D004305:Dose-Response Relationship, Drug; D004341:Drug Evaluation; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000494:pharmacology* / Q000592:standards; D004789:Enzyme Activation; D057075:Enzyme Assays / Q000379:methods; D004797:Enzyme-Linked Immunosorbent Assay; D005260:Female; D017930:Genes, Reporter; D057809:HEK293 Cells; D016655:HIV Core Protein p24 / Q000378:metabolism; D015658:HIV Infections / Q000821:virology; D015497:HIV-1 / Q000187:drug effects* / Q000472:pathogenicity / Q000502:physiology; D006801:Humans; D007963:Leukocytes, Mononuclear / Q000187:drug effects; D008156:Luciferases / Q000737:chemistry / Q000235:genetics; D008297:Male; D011401:Promoter Regions, Genetic; D031347:Prunella / Q000737:chemistry; D012333:RNA, Messenger / Q000235:genetics / Q000378:metabolism; D051381:Rats; D019713:Receptors, CCR5 / Q000378:metabolism; D019718:Receptors, CXCR4 / Q000235:genetics / Q000378:metabolism; D014162:Transfection; D014779:Virus Replication; D055815:Young Adult
chemical_list: D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; C527276:CXCR4 protein, human; D004365:Drugs, Chinese Herbal; D016655:HIV Core Protein p24; D012333:RNA, Messenger; D019713:Receptors, CCR5; D019718:Receptors, CXCR4; C514799:p24 protein, Human Immunodeficiency Virus Type 1; D008156:Luciferases