Rapid screening of brain-penetrable antioxidants from natural products by blood-brain barrier specific permeability assay combined with DPPH recognition

2018 ◽  
Vol 151 ◽  
pp. 42-48 ◽  
Author(s):  
Junfeng Zhu ◽  
Xiaojiao Yi ◽  
Jinghui Zhang ◽  
Shuqing Chen ◽  
Yongjiang Wu
Keyword(s):  
Natural Products ◽  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Rapid Screening ◽  
Blood Brain ◽  
Specific Permeability ◽  
Permeability Assay

scholarly journals Can Natural Products Exert Neuroprotection without Crossing the Blood–Brain Barrier?

2021 ◽  
Vol 22 (7) ◽  
pp. 3356
Author(s):  
Manon Leclerc ◽  
Stéphanie Dudonné ◽  
Frédéric Calon
Keyword(s):  
Natural Products ◽  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Brain Diseases ◽  
Omega 3 ◽  
Indirect Pathway ◽  
Brain Functions ◽  
Blood Brain ◽  
The Central Nervous System ◽  
Peripheral Metabolism

The scope of evidence on the neuroprotective impact of natural products has been greatly extended in recent years. However, a key question that remains to be answered is whether natural products act directly on targets located in the central nervous system (CNS), or whether they act indirectly through other mechanisms in the periphery. While molecules utilized for brain diseases are typically bestowed with a capacity to cross the blood–brain barrier, it has been recently uncovered that peripheral metabolism impacts brain functions, including cognition. The gut–microbiota–brain axis is receiving increasing attention as another indirect pathway for orally administered compounds to act on the CNS. In this review, we will briefly explore these possibilities focusing on two classes of natural products: omega-3 polyunsaturated fatty acids (n-3 PUFAs) from marine sources and polyphenols from plants. The former will be used as an example of a natural product with relatively high brain bioavailability but with tightly regulated transport and metabolism, and the latter as an example of natural compounds with low brain bioavailability, yet with a growing amount of preclinical and clinical evidence of efficacy. In conclusion, it is proposed that bioavailability data should be sought early in the development of natural products to help identifying relevant mechanisms and potential impact on prevalent CNS disorders, such as Alzheimer’s disease.

Anin vitrotransport model for rapid screening and predicting the permeability of candidate compounds at blood–brain barrier

2011 ◽  
Vol 13 (12) ◽  
pp. 1087-1097 ◽  
Author(s):  
Zhi-Hong Yang ◽  
Xiao Sun ◽  
Chao Mei ◽  
Xiao-Bo Sun ◽  
Xiao-Dong Liu ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Rapid Screening ◽  
Blood Brain

High throughput artificial membrane permeability assay for blood–brain barrier

2003 ◽  
Vol 38 (3) ◽  
pp. 223-232 ◽  
Author(s):  
Li Di ◽  
Edward H Kerns ◽  
Kristi Fan ◽  
Oliver J McConnell ◽  
Guy T Carter
Keyword(s):  
Membrane Permeability ◽  
Blood Brain Barrier ◽  
High Throughput ◽  
Brain Barrier ◽  
Artificial Membrane ◽  
Blood Brain ◽  
Permeability Assay

scholarly journals Rapid Screening of Blood-Brain Barrier Penetration of Drugs Using the Immobilized Artificial Membrane Phosphatidylcholine Column Chromatography

2005 ◽  
Vol 11 (1) ◽  
pp. 13-20 ◽  
Author(s):  
Chi Ho Yoon ◽  
Soo Jin Kim ◽  
Beom Soo Shin ◽  
Kang Choon Lee ◽  
Sun Dong Yoo
Keyword(s):  
Blood Brain Barrier ◽  
Prediction Method ◽  
Brain Barrier ◽  
Rapid Screening ◽  
Artificial Membrane ◽  
Immobilized Artificial Membrane ◽  
Blood Brain ◽  
Cns Penetration

The chromatographic capacity factors (kIAM) of 23 structurally diverse drugs were measured by the immobilized artificial membrane (kIAM) phosphatidylcholine chromatography for the prediction of blood-brain barrier (BBB) penetration. The kIAM was determined using themobile phase consisting of acetonitrile:DPBS (20:80 v/v) and corrected for the molar volume of the solutes (kIAM/MWn). The correlation between kIAM/MWn and CNS penetration was highest when measured at pH 5.5 with the power function of n = 4. This in vitro predictionmethod was validated with 7 newly synthesized PDE-4 inhibitors. The relationship between in vivo plasma-to-brain concentration ratios and in vitro CNS penetration was excellent ( r= 0.959). The developed in vitro prediction method may be used as a rapid screening tool for BBB penetration of drugs with passive transport mechanism, with high success, low cost, and reproducibility.

The Protective Effects of Natural Products on Blood-Brain Barrier Breakdown

2012 ◽  
Vol 19 (12) ◽  
pp. 1830-1845 ◽  
Author(s):  
A. Kam ◽  
K. M. Li ◽  
V. Razmovski-Naumovski ◽  
S. Nammi ◽  
K. Chan ◽  
...  
Keyword(s):  
Natural Products ◽  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Protective Effects ◽  
Blood Brain ◽  
Barrier Breakdown ◽  
Blood Brain Barrier Breakdown
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