β-Lapachone is an ortho-naphthoquinone originally isolated from the heartwood of Handroanthus impetiginosus and can be obtained through synthesis from lapachol, naphthoquinones, and other aromatic compounds. β-Lapachone is well known to inhibit topoisomerase I and to induce NAD(P)H: quinone oxidoreductase 1. Currently, phase II clinical trials are being conducted for the treatment of pancreatic cancer. In view of ever-increasing scientific interest in this naphthoquinone, herein, the authors present a review of the synthesis, physicochemical properties, biological activities, and toxicity of β-lapachone. This natural compound has shown activity against several types of malignant tumors, such as lung and pancreatic cancers and melanoma. Furthermore, this ortho-naphthoquinone has antifungal and antibacterial activities, underscoring its action against resistant microorganisms and providing anti-inflammatory, antiobesity, antioxidant, neuroprotective, nephroprotective, and wound-healing properties. β-Lapachone presents low toxicity, with no signs of toxicity against alveolar macrophages, dermal fibroblast cells, hepatocytes, or kidney cells.

β-Lapachone 是一种邻位萘醌，最初从Handroanthus impetiginosus的心材中分离出来，可由拉帕酚、萘醌和其他芳香族化合物合成得到。众所周知，β-Lapachone 可抑制拓扑异构酶 I 并诱导 NAD(P)H：醌氧化还原酶 1。目前，正在进行 II 期临床试验以治疗胰腺癌。鉴于对这种萘醌的科学兴趣与日俱增，在此，作者对 β-拉帕醌的合成、理化性质、生物活性和毒性进行了综述。这种天然化合物已显示出对多种类型的恶性肿瘤的活性，例如肺癌和胰腺癌以及黑色素瘤。此外，这个邻-萘醌具有抗真菌和抗菌活性，强调其对耐药微生物的作用，并提供抗炎、抗肥胖、抗氧化、神经保护、肾保护和伤口愈合特性。β-Lapachone 毒性低，对肺泡巨噬细胞、真皮成纤维细胞、肝细胞或肾细胞没有毒性迹象。