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, Yucatán, Mexico.
Unidad de Biotecnología, Centro de Investigación Científica de Yucatán (CICY), Calle 43 No. 130, Col. Chuburná de Hidalgo, Mérida 97205, Yucatán, Mexico.
Molecules. 2022 Nov 26;27(23):8263. doi: 10.3390/molecules27238263.
Leukemia is one of the most frequent types of cancer. No effective treatment currently exists, driving a search for new compounds. Simple structural modifications were made to novel triterpenes isolated from . Of the three resulting derivatives, 3α-methoxy-24-hydroxylup-20(29)-en-28-oic acid () caused a decrease in the median inhibitory concentration (IC) on the K562 cell line. Its mode of action was apparently apoptosis, ROS generation, and loss of mitochondrial membrane potential (MMP). Molecular docking analysis showed to produce lower binding energies than its precursor for the Bcl-2 and EGFR proteins. Small, simple, and viable modifications to triterpenes can improve their activity against leukemia cell lines. is a potentially promising element for future research. Clarifying the targets in its mode of action will improve its applicability.
白血病是最常见的癌症类型之一。目前尚无有效的治疗方法，因此正在寻找新的化合物。对从 中分离出的新型三萜类化合物进行了简单的结构修饰。在这三种衍生化合物中，3α-甲氧基-24-羟基羽扇豆-20(29)-烯-28-酸 () 导致对 K562 细胞系的半数抑制浓度 (IC) 降低。其作用模式显然是细胞凋亡、ROS 生成和线粒体膜电位 (MMP) 丧失。分子对接分析表明，与前体相比， 对 Bcl-2 和 EGFR 蛋白的结合能更低。对三萜类化合物进行微小、简单和可行的修饰可以提高其对白血病细胞系的活性。 是未来研究的一个有前途的候选物。阐明其作用模式中的靶标将提高其适用性。
