Lapachol, a naphthoquinone, was obtained from the methanol extract of the root of Kigelia africana (sausage tree) (Lam.) Benth. and structurally modified to improve anticancer specificity. The structures of the lapachol and derivatives were elucidated following the consideration of spectra data which included mass spectrometry and nuclear magnetic resonance (NMR) techniques. The in vitro cytotoxic activities of the lapachol and its derivatives were evaluated on healthy human prostate (PC-3), human cervical cancer (Hela) and mouse fibroblast (3T3) cell lines using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Lapachol exhibited higher cytotoxicity on the Hela cells (IC₅₀ = 6.15 μg mL⁻¹) compared to the derivative molecules. The lapachol was cytotoxic to both cancer and normal cell, while the derivatized conjugates lost the cytotoxic potency to cancer cell. This work provides evidence that supports lapachol as one of the major cytotoxic compounds present in the root of K. africana of Nigerian origin and it is recommended that the extract of the plant should be consumed with caution owing to general cellular toxicity of the major phytoconstituent.

Lapachol是一种萘醌，是从非洲基格里亚（香肠）（Bamth ）Benth的甲醇提取物中获得的。并进行结构修饰以提高抗癌特异性。考虑到包括质谱法和核磁共振（NMR）技术在内的光谱数据，阐明了拉帕胆及其衍生物的结构。使用3-（4,5-二甲基噻唑-2-基）对健康的人前列腺（PC-3），人宫颈癌（Hela）和小鼠成纤维细胞（3T3）细胞系评估了lapachol及其衍生物的体外细胞毒性活性）-2,5-二苯基四唑溴化物（MTT）分析。Lapachol对Hela细胞表现出更高的细胞毒性（IC ₅₀  = 6.15μgmL ^-1）与衍生分子相比。拉帕酚对癌细胞和正常细胞均具有细胞毒性，而衍生的结合物则对癌细胞失去细胞毒性。这项工作提供了证据证明拉帕酚是存在于尼日利亚起源的非洲假单胞菌根中的主要细胞毒性化合物之一，并且由于主要植物成分的一般细胞毒性，因此建议谨慎食用植物提取物。