Semisynthesis of novel monacolin J derivatives: Hypocholesterolemic and neuroprotective activities

CampoyS.; SierraS.; SuarezB.; RamosM.C.; VelascoJ.; BurgosJ.S.; AdrioJ.L.

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Semisynthesis of novel monacolin J derivatives: Hypocholesterolemic and neuroprotective activities

机译：半合成新型莫纳可林J衍生物：降胆固醇和神经保护活性

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A fungal strain able to naturally accumulate large amounts of monacolin J was improved by N-methyl-N′-nitro-N-nitrosoguanidine mutagenesis and genetic disruption of the lovF gene. Semisynthesis was then used to produce novel statins by attaching different side chains at the C8 hydroxyl residue. In vitro hypocholesterolemic and neuroprotection assays showed that one derivative (NST0037) had a very low 3-hydroxy-3-methylglutaryl CoA reductase IC 50 and high protection rate for oxidative-stress-induced neuron cell death.

机译：N-甲基-N'-硝基-N-亚硝基胍的诱变和lovF基因的遗传破坏改善了能够自然积累大量莫纳可林J的真菌菌株。然后通过在C8羟基残基上连接不同的侧链，将半合成法用于生产新型他汀类药物。体外降胆固醇和神经保护实验表明，一种衍生物（NST0037）的3-羟基-3-甲基戊二酰辅酶A还原酶IC 50非常低，对氧化应激诱导的神经元细胞死亡具有很高的保护率。

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《The Journal of Antibiotics: An International Journal》 |2010年第8期|共7页
作者
CampoyS.; SierraS.; SuarezB.; RamosM.C.; VelascoJ.; BurgosJ.S.; AdrioJ.L.;
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正文语种 eng
中图分类药学;
关键词
hypocholesterolemic; monacolin J; neuroprotection; statins;

机译：降胆固醇;莫纳可林J;神经保护;他汀类;

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1. Semisynthesis of novel monacolin J derivatives: Hypocholesterolemic and neuroprotective activities [J] . CampoyS., SierraS., SuarezB., The Journal of Antibiotics: An International Journal . 2010,第8期

机译：半合成新型莫纳可林J衍生物：降胆固醇和神经保护活性
2. Hypocholesterolemic and hypolipidemic activity of some novel morpholine derivatives with antioxidant activity. [J] . Chrysselis MC, Rekka EA, Kourounakis PN Journal of Medicinal Chemistry . 2000,第4期

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3. Semisynthesis and Pesticidal Activities of Derivatives of the Diterpenoid Andrographolide and Investigation on the Stress Response of Aphis citricola Van der Goot (Homoptera: Aphididae) [J] . Hao Meng, Sun Zhiqiang, Xu Jianwei, Journal of Agricultural and Food Chemistry . 2020,第14期

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4. Stereospecific Synthesis of Tryptamine Derivatives of Alkaloid Securinine and Their Potential Neuroprotective Activity [C] . S.G. Klochkov, M.E. Neganova, S.A. Pukhov, International Conference on Modern Synthetic Methodologies for Creating Drugs and Functional Materials . 2019

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5. Neuroprotective activities of Nepalese and Native American traditional medicine in Parkinson's disease models. [D] . de Rus Jacquet, Aurelie. 2016

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6. Hypocholesterolemic Activity of Monascus Fermented Product in the Absence of Monacolins with Partial Purification for Functional Food Applications [O] . Zahra Ajdari, Maaruf Abd Ghani, Mohd Khan Ayob, -1

机译：在没有Monacolins且部分纯化的功能性食品应用中红曲菌发酵产物的降胆固醇活性
7. Semisynthesis of novel monacolin J derivatives: hypocholesterolemic and neuroprotective activities [O] . Sonia Campoy, Saleta Sierra, Beatriz Suarez, 2010

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8. Neuroprotective Ganglioside Derivatives [R] . Ullman, M. D. 2006

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Semisynthesis of novel monacolin J derivatives: Hypocholesterolemic and neuroprotective activities

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