Short Lecture “Novel neuroprotective metabolites produced via biotransformation of cyclocephagenol by Alternaria eureka 1E1BL1”
Makaleler > Tam Makale · 2022
Yazarlar: M Küçüksolak, G Üner, Petek BALLAR KIRMIZIBAYRAK, E Bedir
Planta Medica, Uluslararası, Wos, 2022, cilt 88, ss 1412-1413
Özet
Neurodegeneration refers to the loss of structure/function of neurons leading to neurological diseases including Alzheimerʼs and Parkinsonʼs. The discovery of novel therapeutics against neurodegenerative diseases has been an area of intense research as neurodegenerative diseases are a huge burden on society and the economy [ 1 ]. Numerous studies reported that natural products have the potential to prevent and treat neurodegeneration. Among these studies, the neuroprotective activities of cycloartane-type saponins are noteworthy [ 2 ], [ 3 ]. In our preliminary studies, the neuroprotective activity of cyclocephagenol, an aglycone of cyclocephaloside I from Astragalus microcephalus [ 4 ], was screened for H 2 O 2 -induced injury in SH-SY5Y cells. Based on the promising bioactivity of cyclocephagenol, the aims of this study were: i) to perform microbial transformation studies on cyclocephagenol using Alternaria eureka followed by isolation and structural characterization of the metabolites; ii) to investigate neuroprotective activities of the metabolites; iii) to understand structure-activity relationships towards neuroprotection. As a result, the biotransformation of cyclocephagenol by Alternaria eureka ([ Fig. 1 ]) yielded twenty-one new metabolites with modifications including monooxygenation, dehydration, methyl migration, epoxidation, and ring expansion. In addition to chemical diversity, biotransformation provided several novel compounds having potent neuroprotective activity against H 2 O 2 -mediated cell death. Further studies revealed that selected compounds reduced the amount of ROS and preserved the integrity of the mitochondrial membrane. Fig. 1 Biotransformation of cyclocephagenol by Alternaria eureka 1E1BL1 yielded new metabolites with neuroprotective activity. Acknowledgments We thank the Pharmaceutical Sciences Research Centre (FABAL, Ege University, Faculty of Pharmacy) for equipment support. We are very grateful to Bionorm Natural Products for providing cyclocephagenol. # Publication History Article published online: 12 December 2022 © 2022. Thieme. All rights reserved. Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, Germany