Moreno Cardenas Calisto, Kratzert Ren Ove, Hanifle Sofie, Gomes da Mata Kanzaki Elida Cleyse, Kanzaki Isamu, Kircher Brigitte, Çiçek Serhat Sezai
Department of Pharmaceutical Biology, Kiel University, Gutenbergstraße 76, 24118 Kiel, Germany.
Department of Biotechnology, Hamburg University of Applied Sciences, Ulmenliet 20, 21033 Hamburg, Germany.
Metabolites. 2025 Aug 9;15(8):542. doi: 10.3390/metabo15080542.
Multiple myeloma and acute myeloid leukemia are severe forms of blood cancer, which lack effective therapies for treatment. In our search for new chemical lead structures from nature, we were investigating the Brazilian medicinal plant arnica-do-cerrado ().
Repeated chromatography led to the isolation of four flavonoids and three sesquiterpenoids, which were evaluated for their cytostatic and cytotoxic properties against HL-60, MOLM-13, AMO-1, and KMS-12 PE cancer cells as well as the non-malignant HS-5 cell line.
Whereas the isolated flavonoids displayed only moderate activity, the three sesquiterpene lactones goyazensolide, centratherin, and lychnopholide exhibited pronounced effects against all four tested cell lines. Goyazensolide was the most effective compound, inhibiting proliferation and metabolic activity with IC values between 1.0 and 1.6 µM, as well as 1.0 to 2.0 µM, respectively. Centratherin and lychnopholide were somewhat less active but showed higher selectivity towards malignant cell lines, which was most pronounced for MOLM-13 cells.
The results of this study revealed interesting natural products that will be further evaluated for their potential as new lead compounds for the treatment of acute myeloid leukemia and multiple myeloma.
多发性骨髓瘤和急性髓系白血病是血癌的严重形式，缺乏有效的治疗方法。在我们从自然界寻找新的化学先导结构的过程中，我们对巴西药用植物阿尼卡-多-塞拉多（）进行了研究。
通过反复色谱法分离出四种黄酮类化合物和三种倍半萜类化合物，并评估了它们对HL-60、MOLM-13、AMO-1和KMS-12 PE癌细胞以及非恶性HS-5细胞系的细胞生长抑制和细胞毒性特性。
分离出的黄酮类化合物仅表现出中等活性，而三种倍半萜内酯戈亚泽索利德、森特拉辛和lychnopholide对所有四种测试细胞系均表现出显著作用。戈亚泽索利德是最有效的化合物，其抑制增殖和代谢活性的IC值分别在1.0至1.6μM以及1.0至2.0μM之间。森特拉辛和lychnopholide活性稍低，但对恶性细胞系表现出更高的选择性，这在MOLM-13细胞中最为明显。
本研究结果揭示了有趣的天然产物，将进一步评估它们作为治疗急性髓系白血病和多发性骨髓瘤新先导化合物的潜力。
