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

苦参生物碱中抗 HIV 药物的鉴定

基本信息

批准号：
7494340
负责人：
LI HUANG
金额：
$ 19.2万
依托单位：
DUKE UNIVERSITY
依托单位国家：
美国
项目类别：
财政年份：
2008
资助国家：
美国
起止时间：
2008-04-01 至 2010-03-31
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/7494340
关键词：
2-cyclopentyl-5-(5-isoquinolylsulfonyl)-6-nitro-1H-benzo(D)imidazole AIDS therapy Acquired Immunodeficiency Syndrome Adverse effects Alkaloids Anti-HIV Agents Anti-Inflammatory Agents Anti-inflammatory Biological Factors China Chinese Herbs Chinese People Chinese Traditional Medicine Communicable Diseases Coumarins Country Development Drug usage Drug-sensitive Effectiveness Escape Mutant Flavonoids Fractionation Genotype Goals HIV HIV-1 Herbal Medicine Highly Active Antiretroviral Therapy Inhibitory Concentration 50 Lead Malignant Neoplasms Medicine Modern Medicine Morbidity - disease rate Multi-Drug Resistance Patients Phase Public Health RNA-Directed DNA Polymerase Reporting Screening procedure Severe Acute Respiratory Syndrome Sophora Testing Viral Virus Virus Diseases alpha benzopyrone base drug development improved mortality novel pandemic disease small molecule

项目摘要

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（由申请人提供）：高度活跃的抗逆转录病毒疗法已成功降低了艾滋病患者的发病率和死亡率。但是，与长期药物使用和多药耐药性病毒的出现有关的副作用破坏了当前治疗的有效性。因此，具有新型作用机理的新型抗HIV-1药物具有改善当前艾滋病疗法的潜力。这项研究的目的是从传统的中含中药力植物中识别出新型的抗HIV-1药物。我们已经筛选了许多用于抗HIV活性的中药，并发现一种具有有效的抗HIV活性的中药。这种抗HIV中药，Sophora生物碱单酸酯（SAT），被广泛用于其抗炎活性，作为中国的反药物。我们假设SAT包含一种或几种可以抑制HIV-1复制的抗HIV化合物。该假设将通过追求以下特定目的来检验：1。确定SAT中负责抗HIV活性的主动组成部分。 2。确定SAT中每种活性化合物的抗HIV-1作用的机制。预计从这项研究中得出的结果将提供有用的信息，以确定从SAT分离的抗HIV化合物是否有可能发展为抗HIV药物进行艾滋病治疗。公共卫生相关性：该R21应用程序的目的是确定中国传统草药“ Sophora生物碱单抗”中的活跃成分，该成分显示出有效的抗HIV活动。