Unidad de Investigación Médica Yucatán, Unidad Médica de Alta Especialidad, Centro Médico Ignacio García Téllez, Instituto Mexicano del Seguro Social (IMSS), Calle 41 No. 439, Col. Industrial, Mérida 97200, Mexico.
Unidad de Investigación Oncológica, Hospital de Oncología, Centro Médico Nacional, Instituto Mexicano del Seguro Social (IMSS), Avenida Cuauhtémoc 330, Ciudad de Mexico 06720, Mexico.
Molecules. 2022 Aug 31;27(17):5616. doi: 10.3390/molecules27175616.
Current antineoplastic agents present multiple disadvantages, driving an ongoing search for new and better compounds. Four lupane-type triterpenes, 3α,24-dihydroxylup-20(29)-en-28-oic acid (), 3α,23-dihydroxy-30-oxo-lup-20(29)-en-28-oic acid (), 3α,23--isopropylidenyl-3α,23-dihydroxylup-20(29)-en-28-oic acid (), and 3α,23-dihydroxylup-20(29)-en-28-oic acid (), previously isolated from , were evaluated on two cell lines of chronic (K562) and acute (HL60) myeloid leukemia. Compounds , , and decreased cell viability and inhibit proliferation, mainly in K562, and exhibited an apoptotic effect from 24 h of treatment. Of particular interest is compound , which caused arrest in active phases (G2/M) of the cell cycle, as shown by in silico study of the CDK1/Cyclin B/Csk2 complex by molecular docking. This compound [3α,23-dihydroxy-30-oxo-lup-20(29)-en-28-oic acid] s a promising candidate for incorporation into cancer treatments and deserves further study.
目前的抗肿瘤药物存在多种缺点，这促使人们不断寻找新的、更好的化合物。从 中分离得到的四种羽扇豆烷型三萜，3α,24-二羟基-20(29)-烯-28-酸（）、3α,23-二羟基-30-氧代-20(29)-烯-28-酸（）、3α,23--异亚丙基-3α,23-二羟基-20(29)-烯-28-酸（）和 3α,23-二羟基-20(29)-烯-28-酸（），对两种慢性（K562）和急性（HL60）髓性白血病细胞系进行了评估。化合物 、 和 降低了细胞活力并抑制增殖，主要在 K562 中，并表现出从 24 小时治疗开始的凋亡作用。特别有趣的是化合物 ，它通过分子对接对 CDK1/Cyclin B/Csk2 复合物进行计算机模拟研究，导致细胞周期的活性期（G2/M）停滞。该化合物 [3α,23-二羟基-30-氧代-20(29)-烯-28-酸]是一种很有前途的抗癌治疗候选药物，值得进一步研究。
