TESTING OF ANTI-HIV COMPOUNDS FROM MEDICINAL PLANTS

描述：（改编自申请人摘要）。 在本提案中， 证明了几种来自植物的水和有机馏分， 玻利维亚民间药物具有抗艾滋病毒活性。 这些分数将是 使用各种化学技术进一步纯化。 化合物将 基于极性和酸/碱与有机溶剂进行分配 特性. 类似化合物的组将通过以下方法进一步纯化： 色谱手段，直到获得纯化合物。 化学 结构将由核磁共振、质量 光谱法或其它化学或仪器方法。 的方法 抗HIV化合物的作用将在体外测定中表征。 gp 120-CD 4相互作用（受体结合）抑制试验， 将进行去包被或逆转录酶活性。 额外 评价化合物是否诱导产生 干扰素或抑制细胞过程，如糖基化， 考察 一旦发现纯化的化合物， 这些药物将在人体内进行抗艾滋病毒活性测试， 单核细胞在体外和在HIV感染的动物模型中， vivo. 研究人员声称，这些研究已经导致了 在几种粗馏分中发现抗HIV活性。 此夕h 申请人相信，通过进一步纯化， 医学上重要的抗艾滋病毒药物可能会被发现，从而改善我们的 治疗人类艾滋病毒感染的能力。

DESCRIPTION: (Adapted from Applicant's Abstract). In this proposal, it is demonstrated that several aqueous and organic fractions from plants used in Bolivian folk medicine have anti-HIV activity. These fractions will be further purified using various chemical techniques. Compounds will be partitioned against organic solvents based on polarity and acid/base properties. Groups of similar compounds will be further purified by chromatographic means until pure compounds are obtained. Chemical structures will be determined by nuclear magnetic resonance, mass spectrometry, or other chemical or instrumental means. The methods of action of anti-HIV compounds will be characterized in in vitro assays. Assays for the inhibition of the gp120-CD4 interaction (receptor binding), uncoating, or reverse transcriptase activity will be performed. Additional studies to evaluate whether the compounds induce the production of interferon or inhibit cellular processes, such as glycosylation, will be examined. Once purified compounds are discovered and their modes of action have been defined, the drugs will be tested for anti-HIV activity in human mononuclear cells in vitro and in an animal model for HIV infection in vivo. The investigators claim that these studies have already lead to the discovery of anti-HIV activity in several crude fractions. Further, the applicants believe that with further purification, it is possible that medicinally important anti-HIV agents may be discovered thus improving our ability to treat HIV infections in humans.