Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades, 2º Piso, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Mexico City CP 06725, Mexico.
CONACYT-Consorcio de Investigación, Innovación y Desarrollo para las Zonas Áridas, Instituto Potosino de Investigación Científica y Tecnológica A. C., San Luis Potosí CP 78216, Mexico.
Molecules. 2021 Nov 2;26(21):6646. doi: 10.3390/molecules26216646.
Incomptine A () is a sesquiterpene lactone isolated from that induces apoptosis, reactive oxygen species production, and a differential protein expression on the U-937 (diffuse histiocytic lymphoma) cell line. In this work, the antitumor potential of was investigated on Balb/c mice inoculated with U-937 cells and through the brine shrimp lethality (BSL) test. Furthermore, was subjected to molecular docking study using as targets proteins associated with processes of cancer as apoptosis, oxidative stress, and glycolytic metabolism. In addition to determining the potential toxicity of in human, its acute toxicity was performed in mice. Results reveals that showed high antilymphoma activity and BSL with an EC of 2.4 mg/kg and LC 16.7 µg/mL, respectively. The molecular docking study revealed that has strong interaction on all targets used. In the acute oral toxicity, had a LD of 149 mg/kg. The results showed that the activities of including antilymphoma activity, BSL, acute toxicity, and in silico interactions were close to the methotrexate, an anticancer drug used as positive control. These findings suggest that may serve as a candidate for the development of a new drug to combat lymphoma.
枯茗醛 A () 是从 中分离得到的一种倍半萜内酯,可诱导 U-937(弥漫性组织细胞淋巴瘤)细胞系凋亡、产生活性氧物质和差异蛋白表达。在这项工作中,研究了枯茗醛 A 对接种 U-937 细胞的 Balb/c 小鼠的抗肿瘤潜力,并通过卤虫致死(BSL)试验进行了研究。此外,还使用与凋亡、氧化应激和糖酵解代谢等癌症相关过程相关的蛋白作为靶标,对枯茗醛 A 进行了分子对接研究。除了确定枯茗醛 A 在人类中的潜在毒性外,还在小鼠中进行了其急性毒性试验。结果表明,枯茗醛 A 表现出高抗淋巴瘤活性和 BSL,EC 为 2.4mg/kg,LC 为 16.7μg/mL。分子对接研究表明,枯茗醛 A 与所有使用的靶标均具有强烈的相互作用。在急性口服毒性试验中,枯茗醛 A 的 LD 为 149mg/kg。结果表明,枯茗醛 A 的活性包括抗淋巴瘤活性、BSL、急性毒性和计算机模拟相互作用与用作阳性对照的抗癌药物甲氨蝶呤相近。这些发现表明,枯茗醛 A 可能作为开发治疗淋巴瘤的新药的候选药物。