Identification of anti-HIV agent(s) from Sophora Alkaloids

苦参生物碱中抗 HIV 药物的鉴定

• 批准号: 7576764
• 负责人: LI HUANG
• 金额: $ 19.5万
• 依托单位: DUKE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2008
• 资助国家: 美国
• 起止时间: 2008-04-01 至 2011-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7576764
• 关键词: AIDS therapy; Acquired Immunodeficiency Syndrome; Adverse effects; Alkaloids; Anti-HIV Agents; Anti-Inflammatory Agents; Anti-inflammatory; China; Chinese Herbs; Chinese People; Chinese Traditional Medicine; Communicable Diseases; Country; Drug usage; Drug-sensitive; Effectiveness; Escape Mutant; Fractionation; Genotype; Goals; HIV; HIV-1; Herbal Medicine; Highly Active Antiretroviral Therapy; Lead; Lipopolysaccharides; Medicine; Modern Medicine; Morbidity - disease rate; Multi-Drug Resistance; Patients; Phase; Production; RNA-Directed DNA Polymerase; Reporting; Screening procedure; Severe Acute Respiratory Syndrome; Sophora; TNF gene; Testing; Viral; Virus; Virus Diseases; drug development; improved; mortality; novel; public health relevance; small molecule

DESCRIPTION (provided by applicant): Highly active anti-retroviral therapy has successfully reduced the morbidity and mortality of AIDS patients. However, the side effects associated with long term drug usage and the emerging of multi-drug resistance viruses have undermined the effectiveness of current treatment. Therefore, new anti-HIV-1 agents with novel mechanism of action have the potential to improve current AIDS therapy. The goal of this study is to identify novel anti-HIV-1 agents from traditional Chinese herb medicines. We have screened many Chinese medicines for anti-HIV activity and found one that possessed potent anti-HIV activity. This anti-HIV Chinese medicine, Sophora Alkaloids Tannate (SAT), was used widely for its anti-inflammatory activity as an over the counter medicine in China. We hypothesized that SAT contains one or several anti-HIV compounds that can inhibit HIV-1 replication. This hypothesis will be tested by pursuing the following specific aims: 1. Identify the active components in SAT that are responsible for the anti-HIV activity. 2. Determine the mechanisms of anti-HIV-1 action of each active compound in SAT. Results derived from this study are expected to provide useful information to determine whether the anti-HIV compounds isolated from SAT has the potential to be developed into anti-HIV drugs for AIDS therapy. PUBLIC HEALTH RELEVANCE: The objective of this R21 application is to identify the active component(s) from a Chinese traditional herbal medicine "Sophora Alkaloids Tannate" that has shown potent anti-HIV activity.

描述（申请人提供）：高效抗逆转录病毒疗法已成功降低艾滋病患者的发病率和死亡率。然而，与长期药物使用相关的副作用和多重耐药病毒的出现破坏了当前治疗的有效性。因此，具有新作用机制的新型抗HIV-1药物具有改善当前AIDS治疗的潜力。本研究的目的是从中草药中筛选新型抗HIV-1药物。我们筛选了许多具有抗HIV活性的中药，并发现了一种具有强效抗HIV活性的中药。苦参碱鞣酸盐是一种抗HIV的中药，因其抗炎活性而在中国被广泛用作非处方药。我们假设SAT含有一种或几种可以抑制HIV-1复制的抗HIV化合物。这一假设将通过追求以下具体目标进行测试：1。确定SAT中负责抗HIV活性的活性成分。2.确定SAT中每种活性化合物的抗HIV-1作用机制。本研究的结果将为确定从SAT中分离的抗HIV化合物是否有潜力开发成用于治疗艾滋病的抗HIV药物提供有用的信息。 公共卫生关系：该R21申请的目的是鉴定来自中国传统草药“苦参碱鞣酸盐”的活性成分，该活性成分已显示出有效的抗HIV活性。