Tan Mario A, An Seong Soo A
Bionano Research Institute, Gachon University, Seongnam-si, Republic of Korea.
College of Science and Research Center for the Natural and Applied Sciences, University of Santo Tomas, Manila, Philippines.
3 Biotech. 2020 Dec;10(12):517. doi: 10.1007/s13205-020-02535-4. Epub 2020 Nov 9.
The purified oxindole alkaloids, isomitraphylline and mitraphylline from , revealed their ability to break amyloid aggregates in vitro suggesting their therapeutic potentials in Alzheimer's disease (AD). Thioflavin-T assay for assessing amyloid- (Aβ) aggregation of these alkaloids exhibited inhibitions at 60.321% ± 2.61 (50 μM) for isomitraphylline and 43.17% ± 3.48 (50 μM) for mitraphylline. Neuroprotective effects were elaborated against Aβ-induced SH-SY5Y cells at 20 μM and 10 μM for isomitraphylline, and 20 μM for mitraphylline. In addition, both alkaloids attenuated and protected the HO-induced SH-SY5Y cell cytotoxicity at 20 μM. The intracellular ROS levels of SH-SY5Y cells from HO-induced oxidative stress were reduced at 20 μM and 10 μM, and the mitochondrial membrane potentials of Aβ-induced SH-SY5Y cells were protected at 20 μM. The overall results suggested the potentials of both alkaloids to target certain pathological biomarkers of AD and could be further investigated as therapeutic or preventive drug leads against AD.
从[来源未提及]中纯化得到的氧化吲哚生物碱异帽柱木碱和帽柱木碱,在体外显示出分解淀粉样聚集体的能力,表明它们在阿尔茨海默病(AD)治疗方面具有潜力。用于评估这些生物碱淀粉样β蛋白(Aβ)聚集的硫黄素-T检测显示,异帽柱木碱在50μM时抑制率为60.321%±2.61,帽柱木碱在50μM时抑制率为43.17%±3.48。在20μM和10μM浓度下,异帽柱木碱对Aβ诱导的SH-SY5Y细胞具有神经保护作用,帽柱木碱在20μM时具有此作用。此外,两种生物碱在20μM时均能减轻并保护过氧化氢(HO)诱导的SH-SY5Y细胞毒性。在20μM和10μM浓度下,HO诱导的氧化应激导致的SH-SY5Y细胞内活性氧水平降低,在20μM时,Aβ诱导的SH-SY5Y细胞的线粒体膜电位得到保护。总体结果表明这两种生物碱有针对AD某些病理生物标志物的潜力,可作为治疗或预防AD的药物先导物作进一步研究。