BACKGROUND Acquired immunodeficiency syndrome (AIDS) is caused by the Human immunodeficiency virus type-1 (HIV-1). HIV-1 protease (HIV-1 PR) is an essential enzyme for the HIV replication, and therefore, it is an important target for antiretroviral drugs development, particularly from natural products. Auricularia polytricha (AP) is an edible mushroom with several important therapeutic properties. These properties will be investigated as HIV-1 PR inhibitors. METHODS The sequential hexane (APH), ethanol (APE) and water (APW) extracts from AP were screened for inhibitory activity against HIV-1 PR. The extract that consistently showed the strong HIV-1 PR inhibition was further investigated for its phytochemical constituents. The compounds were purified by column chromatography. The isolated compounds were structurally elucidated using 1D and 2D NMR, HRMS, FTIR, and GC/MS techniques. Each compound was screened against HIV-1 PR to determine its inhibitory activity and to provide an explanation for the activity found in the extract. RESULTS Hexane crude extract of AP (APH) exhibited significant inhibition on HIV-1 PR activity. Four major compounds isolated from APH fraction were identified to be two triacylglycerols, linoleic acid and ergosterol. Moreover, all four compounds showed significant inhibition of HIV-1 PR activity. CONCLUSION The findings from this study suggest that AP is a good source of fatty esters, fatty acids and ergosterol. These natural products exhibit anti-HIV-1 properties by blocking HIV-1 PR. These important biological results warrant further development of AP as an alternative antiretroviral drug.

中文翻译：

---

多毛木耳的粗提物和分离化合物的抗HIV-1蛋白酶活性。

背景技术获得性免疫缺陷综合症（AIDS）是由人类1型免疫缺陷病毒（HIV-1）引起的。HIV-1蛋白酶（HIV-1 PR）是HIV复制所必需的酶，因此，它是抗逆转录病毒药物特别是天然产物研发的重要目标。多毛木耳（AP）是一种可食用的蘑菇，具有多种重要的治疗特性。这些特性将作为HIV-1 PR抑制剂进行研究。方法筛选从AP中提取的己烷，乙醇（APE）和水（APW）顺序提取物对HIV-1 PR的抑制活性。对提取物始终表现出强烈的HIV-1 PR抑制作用，对其植物化学成分进行了进一步研究。化合物通过柱色谱法纯化。使用1D和2D NMR对分离出的化合物进行结构解析，HRMS，FTIR和GC / MS技术。筛选每种化合物抗HIV-1 PR的方法，以确定其抑制活性，并为提取物中的活性提供解释。结果AP的己烷粗提取物（APH）对HIV-1 PR活性具有明显的抑制作用。从APH馏分中分离出的四种主要化合物被鉴定为两种三酰基甘油，亚油酸和麦角固醇。此外，所有四种化合物均显示出对HIV-1 PR活性的显着抑制作用。结论从这项研究中发现，AP是脂肪酯，脂肪酸和麦角固醇的良好来源。这些天然产物通过阻断HIV-1 PR表现出抗HIV-1的特性。这些重要的生物学结果保证了AP作为抗逆转录病毒替代药物的进一步发展。筛选每种化合物抗HIV-1 PR的方法，以确定其抑制活性，并为提取物中的活性提供解释。结果AP的己烷粗提取物（APH）对HIV-1 PR活性具有明显的抑制作用。从APH馏分中分离出的四种主要化合物被鉴定为两种三酰基甘油，亚油酸和麦角固醇。此外，所有四种化合物均显示出对HIV-1 PR活性的显着抑制作用。结论从这项研究中发现，AP是脂肪酯，脂肪酸和麦角固醇的良好来源。这些天然产物通过阻断HIV-1 PR表现出抗HIV-1的特性。这些重要的生物学结果保证了AP作为抗逆转录病毒替代药物的进一步发展。筛选每种化合物抗HIV-1 PR的方法，以确定其抑制活性，并为提取物中的活性提供解释。结果AP的己烷粗提取物（APH）对HIV-1 PR活性具有明显的抑制作用。从APH馏分中分离出的四种主要化合物被鉴定为两种三酰基甘油，亚油酸和麦角固醇。此外，所有四种化合物均显示出对HIV-1 PR活性的显着抑制作用。结论从这项研究中发现，AP是脂肪酯，脂肪酸和麦角固醇的良好来源。这些天然产物通过阻断HIV-1 PR表现出抗HIV-1的特性。这些重要的生物学结果保证了AP作为抗逆转录病毒替代药物的进一步发展。