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生物增强剂胡椒碱至少具有三种形态。

The Bioenhancer Piperine is at Least Trimorphic.

作者信息

Pfund Laura Y, Chamberlin Brianna L, Matzger Adam J

机构信息

Department of Chemistry and the Macromolecular Science and Engineering Program, University of Michigan, 930 North University Avenue, Ann Arbor, Michigan 48109, United States.

出版信息

Cryst Growth Des. 2015 May 6;15(5):2047-2051. doi: 10.1021/acs.cgd.5b00278. Epub 2015 Mar 23.

DOI:10.1021/acs.cgd.5b00278
PMID:28529462
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5436616/
Abstract

Polymer-induced heteronucleation (PIHn), a powerful crystalline polymorph discovery method, has revealed two novel polymorphs of the low solubility bioenhancer piperine. Both of these forms exhibit enhanced solubility when compared to the commercial polymorph, thereby potentially improving the efficacy of piperine as a bioenhancer. Structural comparison of the three forms reveals that π-π interactions are only present in the two newly discovered forms. Combined with the stability data this reveals that despite the extended conjugation present in the moleculesuch interactions are not preferred in thesolid state.

摘要

聚合物诱导异相成核(PIHn)是一种强大的晶体多晶型发现方法,它揭示了低溶解度生物增强剂胡椒碱的两种新型多晶型。与市售多晶型相比,这两种形式均表现出更高的溶解度,从而有可能提高胡椒碱作为生物增强剂的功效。三种形式的结构比较表明,π-π相互作用仅存在于两种新发现的形式中。结合稳定性数据表明,尽管分子中存在扩展共轭,但这种相互作用在固态中并非首选。

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本文引用的文献

1
Piperine inhibits the growth and motility of triple-negative breast cancer cells.胡椒碱抑制三阴性乳腺癌细胞的生长和运动能力。
Cancer Lett. 2015 Feb 1;357(1):129-140. doi: 10.1016/j.canlet.2014.11.017. Epub 2014 Nov 13.
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Piperine inhibits IL-1β-induced IL-6 expression by suppressing p38 MAPK and STAT3 activation in gastric cancer cells.胡椒碱通过抑制胃癌细胞中p38丝裂原活化蛋白激酶(MAPK)和信号转导子与转录激活子3(STAT3)的激活来抑制白细胞介素-1β(IL-1β)诱导的白细胞介素-6(IL-6)表达。
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Impact of polymers on the crystallization and phase transition kinetics of amorphous nifedipine during dissolution in aqueous media.
胡椒碱及其包合物在生物相关介质中的溶解度及其对减轻小鼠回肠收缩的作用。
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Evaluation of the Molecular State of Piperine in Cyclodextrin Complexes by Near-Infrared Spectroscopy and Solid-State Fluorescence Measurements.通过近红外光谱和固态荧光测量评估胡椒碱在环糊精复合物中的分子状态。
Int J Med Chem. 2019 Feb 11;2019:7530480. doi: 10.1155/2019/7530480. eCollection 2019.
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Survey and analysis of crystal polymorphism in organic structures.有机结构中晶体多晶型的调查与分析。
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Mol Pharm. 2014 Oct 6;11(10):3565-76. doi: 10.1021/mp500333v. Epub 2014 Sep 18.
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Investigation of the efficacy of adjunctive therapy with bioavailability-boosted curcuminoids in major depressive disorder.生物利用度增强的姜黄素类化合物辅助治疗重度抑郁症的疗效研究。
Phytother Res. 2015 Jan;29(1):17-21. doi: 10.1002/ptr.5211. Epub 2014 Aug 4.
5
Brain-derived neurotrophic factor signalling mediates the antidepressant-like effect of piperine in chronically stressed mice.脑源性神经营养因子信号传导介导了胡椒碱对慢性应激小鼠的抗抑郁样作用。
Behav Brain Res. 2014 Mar 15;261:140-5. doi: 10.1016/j.bbr.2013.12.020. Epub 2013 Dec 19.
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7
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