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关于仙女水母毒液中胆碱酯酶抑制化合物的研究。

Studies on the cholinesterases inhibiting compounds from the Cassiopea andromeda venom.

作者信息

Darabi Amir Hossein, Nabipour Iraj, Mohebbi Gholamhossein, Vazirizadeh Amir, Vatanpour Hossein, Maryamabadi Ammar

机构信息

The Persian Gulf Tropical Medicine Research Center, The Persian Gulf Biomedical Sciences Research institute, Bushehr University of Medical Sciences, Bushehr, Iran.

The Persian Gulf Marine Biotechnology Research Center, The Persian Gulf Biomedical Sciences Research Institute, Bushehr University of Medical Sciences, Bushehr, Iran.

出版信息

Bioinformation. 2020 Sep 30;16(9):702-709. doi: 10.6026/97320630016702. eCollection 2020.

Abstract

Cholinesterase inhibitors find application in the combat and care of several diseases, especially AD. Jellyfish venoms are the most promising sources of potent cholinesterase inhibitors. Therefore, it is of interest to study cholinesterases inhibiting compounds from the Cassiopea andromeda venom. We report bioactive compounds using the GC-MC method followed by molecular modeling and docking data analysis. The GC-MS analysis of the crude venom led to the identification of seven bioactive compounds (C1-C7), comprising the steroidal alkaloids, phenolic and carotenoid derivatives. The venom exhibited inhibitory activities against the cholinesterase enzymes. The compound C2, a Dioxolane steroid, displayed the strongest inhibition on both AChE and BChE activities for further consideration.

摘要

胆碱酯酶抑制剂在多种疾病的防治中有着应用,尤其是阿尔茨海默病(AD)。水母毒液是强效胆碱酯酶抑制剂最有前景的来源。因此,研究来自仙女水母毒液的胆碱酯酶抑制化合物具有重要意义。我们通过气相色谱 - 质谱联用(GC - MC)方法,随后进行分子建模和对接数据分析,报告了生物活性化合物。对粗毒液的GC - MS分析鉴定出七种生物活性化合物(C1 - C7),包括甾体生物碱、酚类和类胡萝卜素衍生物。该毒液对胆碱酯酶表现出抑制活性。化合物C2,一种二氧戊环甾体,对乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)的活性均表现出最强的抑制作用,值得进一步研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/798d/8457019/235a18a4514b/97320630016702F1.jpg

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