scholarly journals Low Molecular Weight (poly)Phenol Metabolites Across the Blood-Brain Barrier: The Underexplored Journey

2020 ◽  
pp. 1-22 ◽  
Author(s):  
Rafael Carecho ◽  
Diogo Carregosa ◽  
Cláudia Nunes dos Santos
Keyword(s):  
Molecular Weight ◽  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Low Molecular Weight ◽  
Blood Brain

scholarly journals Recent Advances in Synthesis, Bioactivity, and Pharmacokinetics of Pterostilbene, an Important Analog of Resveratrol

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 5166
Author(s):  
Yeju Liu ◽  
Yuyang You ◽  
Juan Lu ◽  
Xi Chen ◽  
Zhihong Yang
Keyword(s):  
Molecular Weight ◽  
Blood Brain Barrier ◽  
The Body ◽  
Brain Barrier ◽  
Low Molecular Weight ◽  
Pharmacological Activities ◽  
Therapeutic Applications ◽  
Blood Brain ◽  
Pass Through ◽  
Anti Inflammation

Pterostilbene is a natural 3,5-dimethoxy analog of resveratrol. This stilbene compound has a strong bioactivity and exists widely in Dalbergia and Vaccinium spp. Besides natural extraction, pterostilbene can be obtained by biosynthesis. Pterostilbene has become popular because of its remarkable pharmacological activities, such as anti-tumor, anti-oxidation, anti-inflammation, and neuroprotection. Pterostilbene can be rapidly absorbed and is widely distributed in tissues, but it does not seriously accumulate in the body. Pterostilbene can easily pass through the blood-brain barrier because of its low molecular weight and good liposolubility. In this review, the studies performed in the last three years on resources, synthesis, bioactivity, and pharmacokinetics of pterostilbene are summarized. This review focuses on the effects of pterostilbene on certain diseases to explore its targets, explain the possible mechanism, and look for potential therapeutic applications.

Monitoring Blood-Brain Barrier Status in a Rat Model of Glioma Receiving Therapy: Dual Injection of Low-Molecular-Weight and Macromolecular MR Contrast Media

Radiology ◽  
2010 ◽  
Vol 257 (2) ◽  
pp. 342-352 ◽  
Author(s):  
Benjamin Lemasson ◽  
Raphaël Serduc ◽  
Cécile Maisin ◽  
Audrey Bouchet ◽  
Nicolas Coquery ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Contrast Media ◽  
Blood Brain Barrier ◽  
Rat Model ◽  
Brain Barrier ◽  
Low Molecular Weight ◽  
Blood Brain ◽  
Dual Injection ◽  
Mr Contrast Media

Accessing the Blood-Brain Barrier to Treat Brain Disorders

2019 ◽  
Vol 9 (3) ◽  
pp. 198-209
Author(s):  
M. Sureshkumar ◽  
A. Pandian
Keyword(s):  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Low Molecular Weight ◽  
Brain Disorders ◽  
Permeable Membrane ◽  
Drug Molecules ◽  
Blood Brain ◽  
Therapeutic Molecules ◽  
Pass Through ◽  
The Brain

: Crossing the blood-brain barrier (BBB) and treating brain disorders by delivering therapeutic agents to specific regions of the brain is a challenge. The BBB, naturally evolved, protective physiological barrier acts as a selective permeable membrane in such a way that it allows only nonionic molecules and molecules of low molecular weight to pass through. Treating brain tumor has become a great challenge as the drug molecules of larger size are not able to cross the BBB and reach the target site. The incompetence of techniques for brain-specific delivery of therapeutic molecules has led researchers to increasingly explore the diagnosis and treatment of disorders incurable with present techniques. This article is to discuss the various techniques or methods to deliver drugs to the brain crossing the BBB.

scholarly journals Rapid and Reversible Enhancement of Blood–Brain Barrier Permeability Using Lysophosphatidic Acid

2013 ◽  
Vol 33 (12) ◽  
pp. 1944-1954 ◽  
Author(s):  
Ngoc H On ◽  
Sanjot Savant ◽  
Myron Toews ◽  
Donald W Miller
Keyword(s):  
Drug Delivery ◽  
Molecular Weight ◽  
Blood Brain Barrier ◽  
Lysophosphatidic Acid ◽  
Near Infrared ◽  
Brain Barrier ◽  
Small Molecular Weight ◽  
Blood Brain ◽  
Bbb Permeability ◽  
The Brain

The present study characterizes the effects of lysophosphatidic acid (LPA) on blood–brain barrier (BBB) permeability focusing specifically on the time of onset, duration, and magnitude of LPA-induced changes in cerebrovascular permeability in the mouse using both magnetic resonance imaging (MRI) and near infrared fluorescence imaging (NIFR). Furthermore, potential application of LPA for enhanced drug delivery to the brain was also examined by measuring the brain accumulation of radiolabeled methotrexate. Exposure of primary cultured brain microvessel endothelial cells (BMECs) to LPA produced concentration-dependent increases in permeability that were completely abolished by clostridium toxin B. Administration of LPA disrupted BBB integrity and enhanced the permeability of small molecular weight marker gadolinium diethylenetriaminepentaacetate (Gd-DTPA) contrast agent, the large molecular weight permeability marker, IRdye800cwPEG, and the P-glycoprotein efflux transporter probe, Rhodamine 800 (R800). The increase in BBB permeability occurred within 3 minutes after LPA injection and barrier integrity was restored within 20 minutes. A decreased response to LPA on large macromolecule BBB permeability was observed after repeated administration. The administration of LPA also resulted in 20-fold enhancement of radiolabeled methotrexate in the brain. These studies indicate that administration of LPA in combination with therapeutic agents may increase drug delivery to the brain.

Quantifying blood-brain-barrier leakage using a combination of evans blue and high molecular weight FITC-Dextran

2019 ◽  
Vol 325 ◽  
pp. 108349
Author(s):  
Yangyang Xu ◽  
Qi He ◽  
Mengqi Wang ◽  
Xin Wang ◽  
Feilong Gong ◽  
...  
Keyword(s):  
Molecular Weight ◽  
High Molecular Weight ◽  
Blood Brain Barrier ◽  
Evans Blue ◽  
Brain Barrier ◽  
Blood Brain

scholarly journals Extracellular Vesicle Delivery of Neferine for the Attenuation of Neurodegenerative Disease Proteins and Motor Deficit in an Alzheimer’s Disease Mouse Model

2022 ◽  
Vol 15 (1) ◽  
pp. 83
Author(s):  
Bin Tang ◽  
Wu Zeng ◽  
Lin Lin Song ◽  
Hui Miao Wang ◽  
Li Qun Qu ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Neurodegenerative Disease ◽  
Blood Brain Barrier ◽  
Natural Compounds ◽  
Brain Barrier ◽  
Motor Deficit ◽  
Cellular Models ◽  
Blood Brain

Exosomes are nano-extracellular vesicles with diameters ranging from 30 to 150 nm, which are secreted by the cell. With their role in drug cargo loading, exosomes have been applied to carry compounds across the blood–brain barrier in order to target the central nervous system (CNS). In this study, high-purity exosomes isolated by the ultra-high-speed separation method were applied as the natural compound carrier, with the loading efficiency confirmed by UHPLC-MS analysis. Through the optimization of various cargo loading methods using exosomes, this study compared the efficiency of different ways for the separation of exosomes and the exosome encapsulation of natural compounds with increasing molecular weights via extensive in vitro and in vivo efficacy studies. In a pharmacokinetic study, our data suggested that the efficiency of compound’s loading into exosomes is positively correlated to its molecular weight. However, with a molecular weight of greater than 1109 Da, the exosome-encapsulated natural compounds were not able to pass through the blood–brain barrier (BBB). In vitro cellular models confirmed that three of the selected exosome-encapsulated natural compounds—baicalin, hederagenin and neferine—could reduce the level of neurodegenerative disease mutant proteins—including huntingtin 74 (HTT74), P301L tau and A53T α-synuclein (A53T α-syn)—more effectively than the compounds alone. With the traditional pharmacological role of the herbal plant Nelumbo nucifera in mitigating anxiety, exosome-encapsulated-neferine was, for the first time, reported to improve the motor deficits of APP/PS1 (amyloid precursor protein/ presenilin1) double transgenic mice, and to reduce the level of β-amyloid (Aβ) in the brain when compared with the same concentration of neferine alone. With the current trend in advocating medicine–food homology and green healthcare, this study has provided a rationale from in vitro to in vivo for the encapsulation of natural compounds using exosomes for the targeting of BBB permeability and neurodegenerative diseases in the future.

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