A Potential In Vitro and In Vivo anti-HIV Drug Screening System for Chinese Herbal Medicines

• Published in: Phytotherapy research 2012-06, Vol.26 (6), p.899-907
• Main Authors: Feng, Long, Wang, Li, Ma, Yun-yun, Li, Min, Zhao, Guo-Qiang
• Format: Article
• Language: English
• Subjects: Adult; Andrographis - chemistry; Animals; Anti-HIV Agents - pharmacology; anti-HIV drugs; Biological and medical sciences; CCR5 promoter; CCR5 Receptor Antagonists; CD4-Positive T-Lymphocytes - metabolism; CD4-Positive T-Lymphocytes - virology; Cell Survival; Chinese herbal medicines; CXCR4 promoter; Dose-Response Relationship, Drug; Drug Evaluation; Drug Evaluation, Preclinical - methods; Drugs, Chinese Herbal - chemistry; Drugs, Chinese Herbal - pharmacology; Drugs, Chinese Herbal - standards; Enzyme Activation; Enzyme Assays - methods; Enzyme-Linked Immunosorbent Assay; Female; General pharmacology; Genes, Reporter; HEK293 Cells; Herba Andrographitis; HIV Core Protein p24 - metabolism; HIV Infections - virology; HIV-1 - drug effects; HIV-1 - pathogenicity; HIV-1 - physiology; Humans; Leukocytes, Mononuclear - drug effects; Luciferases - chemistry; Luciferases - genetics; Male; Medical sciences; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; Promoter Regions, Genetic; Prunella - chemistry; Rats; Receptors, CCR5 - metabolism; Receptors, CXCR4 - genetics; Receptors, CXCR4 - metabolism; RNA, Messenger - genetics; RNA, Messenger - metabolism; Spica Prunellae; traditional Chinese medicine; Transfection; Virus Replication; Young Adult
• ISSN: 0951-418X; 1099-1573
• DOI: 10.1002/ptr.3658

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