State Key Laboratory of Biotherapy, Collaborative Innovation Center of Biotherapy and Cancer Center, West China Hospital of Sichuan University, Chengdu, P. R. China.
Translational Skin Cancer Research, German Cancer Consortium (DKTK), Dermatology, University Duisburg-Essen, Essen, Germany.
Am J Chin Med. 2022;50(5):1173-1196. doi: 10.1142/S0192415X22500483. Epub 2022 Jul 2.
Acquired immunodeficiency syndrome (AIDS) caused by human immunodeficiency virus (HIV) infection is a serious public problem threatening global health. At present, although "cocktail therapy" has achieved significant clinical effects, HIV still cannot be completely eradicated. Furthermore, long-term antiviral treatment has caused problems such as toxic side effects, the emergence of drug-resistant viruses, and poor patient compliance. Therefore, it is highly necessary to continue to search for high-efficient, low-toxic anti-HIV drugs with new mechanisms. Natural products have the merits of diverse scaffolds, biological activities, and low toxicity that are deemed the important sources of drug discovery. Thus, finding lead compounds from natural products followed by structure optimization has become one of the important ways of modern drug discovery. Nowadays, many natural products have been found, such as berberine, gnidimacrin, betulone, and kuwanon-L, which exert effective anti-HIV activity through immune regulation, inhibition of related functional enzymes in HIV replication, and anti-oxidation. This paper reviewed these natural products, their related chemical structure optimization, and their anti-HIV mechanisms.
获得性免疫缺陷综合征（AIDS）是由人类免疫缺陷病毒（HIV）感染引起的严重威胁全球健康的公共卫生问题。目前，尽管“鸡尾酒疗法”取得了显著的临床效果，但 HIV 仍不能被完全清除。此外，长期的抗病毒治疗导致了毒性副作用、耐药病毒的出现和患者顺应性差等问题。因此，继续寻找具有新机制的高效、低毒的抗 HIV 药物是非常必要的。天然产物具有多样的骨架、生物活性和低毒性等优点，被认为是药物发现的重要来源。因此，从天然产物中寻找先导化合物并进行结构优化已成为现代药物发现的重要途径之一。目前，已经发现了许多具有抗 HIV 活性的天然产物，如小檗碱、 gnidimacrin、桦木酮酸和 kuwanon-L 等，它们通过免疫调节、抑制 HIV 复制过程中的相关功能酶以及抗氧化作用发挥有效的抗 HIV 活性。本文综述了这些天然产物及其相关的化学结构优化和抗 HIV 机制。
