Direct Inhibition of the First PDZ Domain of ZO-1 by Glycyrrhizin is a Possible Mechanism of Tight Junction Opening of Caco-2 Cells.

2022 ◽  
Author(s):  
Emi Hibino ◽  
Natsuko Goda ◽  
Misaki Hisada ◽  
Takeshi Tenno ◽  
Hidekazu Hiroaki
Keyword(s):  
Tight Junction ◽  
Drug Absorption ◽  
Pdz Domain ◽  
Direct Inhibition ◽  
Pharmacological Activities ◽  
Intestinal Drug Absorption ◽  
Anti Inflammation

Glycyrrhizin (GL) is known to exhibit a variety of useful pharmacological activities, including anti-inflammation, anti-hepatotoxicity, and enhancement of intestinal drug absorption. GL has been reported to modify the assembly of...

scholarly journals Regional Intestinal Drug Absorption: Biopharmaceutics and Drug Formulation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 272
Author(s):  
Arik Dahan ◽  
Isabel González-Álvarez
Keyword(s):  
Drug Absorption ◽  
Unmet Needs ◽  
Drug Formulation ◽  
Fluid Composition ◽  
Mucosal Cell ◽  
Special Issue ◽  
Junction Resistance ◽  
Intestinal Drug Absorption ◽  
Carrier Mediated Transport ◽  
Mechanistic Basis

The gastrointestinal tract (GIT) can be broadly divided into several regions: the stomach, the small intestine (which is subdivided to duodenum, jejunum, and ileum), and the colon. The conditions and environment in each of these segments, and even within the segment, are dependent on many factors, e.g., the surrounding pH, fluid composition, transporters expression, metabolic enzymes activity, tight junction resistance, different morphology along the GIT, variable intestinal mucosal cell differentiation, changes in drug concentration (in cases of carrier-mediated transport), thickness and types of mucus, and resident microflora. Each of these variables, alone or in combination with others, can fundamentally alter the solubility/dissolution, the intestinal permeability, and the overall absorption of various drugs. This is the underlying mechanistic basis of regional-dependent intestinal drug absorption, which has led to many attempts to deliver drugs to specific regions throughout the GIT, aiming to optimize drug absorption, bioavailability, pharmacokinetics, and/or pharmacodynamics. In this Editorial we provide an overview of the Special Issue "Regional Intestinal Drug Absorption: Biopharmaceutics and Drug Formulation". The objective of this Special Issue is to highlight the current progress and to provide an overview of the latest developments in the field of regional-dependent intestinal drug absorption and delivery, as well as pointing out the unmet needs of the field.

scholarly journals Robotic screening of intestinal drug absorption

2020 ◽  
Vol 4 (5) ◽  
pp. 485-486
Author(s):  
Abdul W. Basit ◽  
Christine M. Madla ◽  
Francesca K. H. Gavins
Keyword(s):  
Drug Absorption ◽  
Intestinal Drug Absorption

scholarly journals High dose of baicalin or baicalein can reduce tight junction integrity by partly targeting the first PDZ domain of zonula occludens-1 (ZO-1)

2020 ◽  
Vol 887 ◽  
pp. 173436 ◽  
Author(s):  
Misaki Hisada ◽  
Minami Hiranuma ◽  
Mio Nakashima ◽  
Natsuko Goda ◽  
Takeshi Tenno ◽  
...  
Keyword(s):  
Tight Junction ◽  
Pdz Domain ◽  
High Dose ◽  
Zonula Occludens ◽  
Zonula Occludens 1

scholarly journals Strategies to Enhance Drug Absorption via Nasal and Pulmonary Routes

Pharmaceutics ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 113 ◽  
Author(s):  
Maliheh Ghadiri ◽  
Paul Young ◽  
Daniela Traini
Keyword(s):  
Nucleic Acid ◽  
Tight Junction ◽  
Drug Absorption ◽  
Therapeutic Agents ◽  
Nasal Administration ◽  
Absorption Enhancers ◽  
Non Invasive ◽  
Basic Concepts ◽  
Transmucosal Administration ◽  
Poor Absorption

New therapeutic agents such as proteins, peptides, and nucleic acid-based agents are being developed every year, making it vital to find a non-invasive route such as nasal or pulmonary for their administration. However, a major concern for some of these newly developed therapeutic agents is their poor absorption. Therefore, absorption enhancers have been investigated to address this major administration problem. This paper describes the basic concepts of transmucosal administration of drugs, and in particular the use of the pulmonary or nasal routes for administration of drugs with poor absorption. Strategies for the exploitation of absorption enhancers for the improvement of pulmonary or nasal administration are discussed, including use of surfactants, cyclodextrins, protease inhibitors, and tight junction modulators, as well as application of carriers such as liposomes and nanoparticles.

scholarly journals ANTIOXIDANT ACTIVITY TEST OF ANDROGRAPHOLIDE IN BITTER HERBS USING DPPH SCAVENGING

2017 ◽  
Vol 1 (1) ◽  
pp. 9
Author(s):  
Ni Made Pitri Susanti ◽  
Ni Kadek Warditian ◽  
I Made Agus Gelgel Wirasuta
Keyword(s):  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Free Radical Scavenging ◽  
Scavenging Activity ◽  
Pharmacological Activities ◽  
Inhibition Effect ◽  
Activity Test ◽  
Ic50 Value ◽  
Dpph Scavenging ◽  
Anti Inflammation

Abstract Bitter herbs (Sambiloto) have many pharmacological activities including antioxidant, antidiabetic, anticancer, antihyperlipidemic and anti-inflammation. Andrographolide is a diterpene compounds contained in bitter herbs. It is known that andrographolide compound responsible for the pharmacological activity of the bitter herbs. This study investigated DPPH free radical scavenging activity from andrographolide diterpene lactone. This study was initiated with the isolation of andrographolide compound from bitter herbs and then testing their DPPH free radical scavenging. The results suggested that andrographolide had IC50 value of 5.45 mg. This means andrographolide has 50% DPPH inhibition effect, i.e 5.45 mg.

scholarly journals The Multifunctional Effects of Nobiletin and Its MetabolitesIn VivoandIn Vitro

2016 ◽  
Vol 2016 ◽  
pp. 1-14 ◽  
Author(s):  
Hao Huang ◽  
Linfu Li ◽  
Weimei Shi ◽  
Hai Liu ◽  
Jianqiong Yang ◽  
...  
Keyword(s):  
Biological Activities ◽  
Signaling Cascades ◽  
Pharmacological Effects ◽  
Pharmacological Activities ◽  
Promising Candidate ◽  
Beneficial Effects ◽  
Pharmaceutical Agent ◽  
Intracellular Targets ◽  
Anti Inflammation

Nobiletin (NOB) chemically known as 5,6,7,8,3′,4′-hexamethoxyflavone is a dietary polymethoxylated flavonoid found inCitrusfruits. Recent evidences show that NOB is a multifunctional pharmaceutical agent. The various pharmacological activities of NOB include neuroprotection, cardiovascular protection, antimetabolic disorder, anticancer, anti-inflammation, and antioxidation. These events may be underpinned by modulation of signaling cascades, including PKA/ERK/MEK/CREB, NF-κB, MAPK, Ca2+/CaMKII, PI3K/Akt1/2, HIF-1α, and TGFβsignaling pathways. The metabolites may exhibit stronger beneficial effects than NOB on diseases pathogenesis. The biological activities of NOB have been clarified on many systems. This review aims to discuss the pharmacological effects of NOB with specific mechanisms of actions. NOB may become a promising candidate for potential drug development. However, further investigations of NOB on specific intracellular targets and clinical trials are still needed, especially forin vivomedical applications.

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