麦角甾醇--一种来自 Phormidium retzii 的乙酰胆碱酯酶抑制剂,与阿尔茨海默氏症治疗有关。

IF 1.5 Q3 MEDICINE, RESEARCH & EXPERIMENTAL International Journal of Molecular and Cellular Medicine Pub Date : 2023-01-01 DOI:10.22088/IJMCM.BUMS.12.2.100
Rincy Yesudas, Vinoth Kumar Thirumalairaj, Geetharamani Durairaj, Amrutha Chacko, Lakshmanasenthil Shanmugaasokan, Suja Gunasekaran
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引用次数: 0

摘要

本研究观察了从微藻 Phormidium retzii 中提取的胆碱酯酶抑制剂的体外筛选、纯化和鉴定过程。从淡水样本中筛选出混合微藻培养物 Phormidium sp.乙酰胆碱酯酶(AChE)是从 hRBC 幽灵中纯化出来的。使用有机溶剂对 P. retzii 进行了连续提取。然后测试了胆碱酯酶的活性以及各种提取物对其的抑制作用。然后对活性馏分进行部分纯化和表征。P. retzii 的石油醚提取物对 AChE 的最大抑制率为 68.6%,而其他溶剂提取物则没有抑制作用。使用薄层色谱法从活性提取物中获得了七个馏分。其中 5 号馏分对 AChE 的最大抑制率为 86.37%。对 5 号馏分进行 GC-MS 分析后,确定其活性成分为豆固醇。豆固醇(0.45µM)的最大抑制率为 81.2±0.08%,IC50 值为 0.214。从 P. retzii 中提取的豆固醇可抑制 AChE,从而成为治疗阿尔茨海默病的更安全药物,且副作用极小。
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Stigmasterol- an Acetylcholinesterase Inhibitor from Phormidium retzii with relevance to Alzheimer's disease Therapy.

This study observed in vitro screening, purification and identification of cholinesterase inhibitors from the microalgae Phormidium retzii. Mixed microalgal culture was screened from freshwater samples for Phormidium sp. Single colony was purified and authenticated as P. retzii. Acetylcholinesterase (AChE) enzyme was purified from hRBC ghost. Sequential extraction of P. retzii was performed using organic solvents. Cholinesterase enzyme activity and its inhibition by various extracts were then tested. The active fractions were then subjected to partial purification and characterization. Petroleum ether extract of P. retzii showed maximum inhibition of 68.6 % against AChE while other solvent extracts showed no inhibition. Seven fractions were obtained from the active extract using thin layer chromatography. Among which fraction no. 5 showed maximum inhibition of 86.37 % towards AChE. Fraction no. 5 when subjected to GC-MS led to determination of the active principle as stigmasterol. The maximum inhibition of stigmasterol (0.45µM) was 81.2±0.08% with IC50 value of 0.214. Stigmasterol from P. retzii inhibited AChE projecting itself as safer drug for Alzheimer's disease with minimal side effects.

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期刊介绍: The International Journal of Molecular and Cellular Medicine (IJMCM) is a peer-reviewed, quarterly publication of Cellular and Molecular Biology Research Center (CMBRC), Babol University of Medical Sciences, Babol, Iran. The journal covers all cellular & molecular biology and medicine disciplines such as the genetic basis of disease, biomarker discovery in diagnosis and treatment, genomics and proteomics, bioinformatics, computer applications in human biology, stem cells and tissue engineering, medical biotechnology, nanomedicine, cellular processes related to growth, death and survival, clinical biochemistry, molecular & cellular immunology, molecular and cellular aspects of infectious disease and cancer research. IJMCM is a free access journal. All open access articles published in IJMCM are distributed under the terms of the Creative Commons Attribution CC BY. The journal doesn''t have any submission and article processing charges (APCs).
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