scholarly journals Transport of Corilagin, Gallic Acid, and Ellagic Acid from Fructus Phyllanthi Tannin Fraction in Caco-2 Cell Monolayers

2016 ◽  
Vol 2016 ◽  
pp. 1-10 ◽  
Author(s):  
Xin Mao ◽  
Ling-Fang Wu ◽  
Hai-juan Zhao ◽  
Wen-Yi Liang ◽  
Wen-Jing Chen ◽  
...  
Keyword(s):  
Tight Junction ◽  
Gallic Acid ◽  
Ellagic Acid ◽  
Organic Anion ◽  
Multidrug Resistance Proteins ◽  
Apparent Permeability ◽  
Glycoprotein P ◽  
Sodium Glucose Cotransporter ◽  
Apparent Permeability Coefficient

Objective. To investigate the absorption property of the representative hydrolyzable tannin, namely corilagin, and its hydrolysates gallic acid (GA) and ellagic acid (EA) from the Fructus Phyllanthi tannin fraction (PTF)in vitro.Methods. Caco-2 cells monolayer model was established. Influences of PTF on Caco-2 cells viability were detected with MTT assay. The transport across monolayers was examined for different time points, concentrations, and secretory directions. The inhibitors of P-glycoprotein (P-gp), multidrug resistance proteins (MRPs), organic anion transporting polypeptide (OATP) and sodium/glucose cotransporter 1 (SGLT1), and tight junction modulators were used to study the transport mechanism. LC-MS method was employed to quantify the absorption concentration.Results. The apparent permeability coefficient(Papp)values of the three compounds were below 1.0 × 10−6 cm/s. The absorption of corilagin and GA were much lower than their efflux, and the uptake of both compounds was increased in the presence of inhibitors of P-gp and MRPs. The absorption of EA was decreased in the company of OATP and SGLT1 inhibitors. Moreover, the transport of corilagin, GA, and EA was enhanced by tight junction modulators.Conclusion. These observations indicated that the three compounds in PTF were transported via passive diffusion combined with protein mediated transport. P-gp and MRPs might get involved in the transport of corilagin and GA. The absorption of EA could be attributed to OATP and SGLT1 protein.

Bicarbonate secretion in rat distal colon in vitro: a measurement technique

1988 ◽  
Vol 254 (3) ◽  
pp. C383-C390 ◽  
Author(s):  
G. M. Feldman ◽  
S. F. Berman ◽  
R. L. Stephenson
Keyword(s):  
Short Circuit ◽  
Distal Colon ◽  
Apparent Permeability ◽  
Chemical Gradients ◽  
Acid Generation ◽  
Rat Distal Colon ◽  
Tissue Surfaces ◽  
Apparent Permeability Coefficient ◽  
Transepithelial Voltage

To study HCO3- secretion in rat distal colon, we utilized a technique that permits control of electrical and chemical transepithelial gradients. With symmetrical solutions (pH 7.4, [HCO3-] 25 mM, and CO2 tension 40 mmHg) bathing both tissue surfaces and under short-circuit conditions, HCO3- secretion remained stable for greater than 4 h at 1 mueq. h-1.cm-2. As the mucosal solution was alkalinized, the serosal solution was acidified at 3.1 mueq.h-1.cm-2. Ninety-four percent of serosal acidification was accounted for by the rate of metabolic lactic acid generation and transepithelial HCO3- secretion. Clamping transepithelial voltage reversibly affected net HCO3- secretion, and a linear relationship existed between clamped mucosal voltage and net HCO3- flux (r = 0.99); mucosal voltage of -68 mV completely inhibited net secretion. The apparent permeability coefficient of the colon to HCO3- is 2.8 X 10(-6) cm/s. One millimolar ouabain completely inhibited net HCO3- secretion. Acetazolamide (10(-4) M) inhibited secretion by approximately 50%, whereas a 10(-3) M concentration inhibited secretion by 90%. These data demonstrate that net colonic HCO3- secretion can be measured without imposed electrical and chemical gradients and that this flux is voltage sensitive and depends on carbonic anhydrase and Na+-K+-ATPase activities.

scholarly journals Development and In Vitro Evaluation of a Mucoadhesive Oral Deliverv System for Antisense Oliaonucleotides

2003 ◽  
Vol 71 (3) ◽  
pp. 165-177 ◽  
Author(s):  
Andreas Bernkop-Schnürch ◽  
Julia Telsnig ◽  
Margit Hornof
Keyword(s):  
Delivery System ◽  
Permeability Coefficient ◽  
Enzymatic Degradation ◽  
Phosphorothioate Oligonucleotide ◽  
Apparent Permeability ◽  
Release Studies ◽  
Apparent Permeability Coefficient ◽  
Permeation Studies ◽  
Membrane Bound

It was the aim of this study to develop an oral phosphorothioate oligodeoxynucleotide (PS-ODN) drug delivery system and to evaluate its properties in vitro. Results demonstrated that the 16-mer phosphorothioate oligonucleotide used was completely stable towards enzymatic degradation by secreted and membrane bound intestinal enzymes. Permeation studies with freshly excised intestinal mucosa showed a comparatively high uptake of the PS-ODN with an apparent permeability coefficient (Papp) of 8.35 ± 1.24 x 10-6 cm/sec. The PS-ODN was incorporated in a poly(acrylic acid)-cysteine carrier matrix system exhibiting high cohesive and mucoadhesive properties. Release studies demonstrated that a controlled and sustained PS-ODN release out of this delivery system could be achieved. Because of these features, the dosage form developed within this study seems to represent a promising novel tool for oral PS-ODN delivery.

scholarly journals Preliminary Report on the Effect of Savanna Plants Leucaena leucocephala, Parkia platycephala and Senna alata against Eggs and Immature Stages of Trichostrongylid Nematodes In Vitro

Pathogens ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 986
Author(s):  
Benta Natânia Silva Figueiredo ◽  
Marcello Otake Sato ◽  
Laiane Teixeira Sousa Moura ◽  
Sandra Maria Botelho Mariano ◽  
Tarso da Costa Alvim ◽  
...  
Keyword(s):  
Gallic Acid ◽  
Ellagic Acid ◽  
Leucaena Leucocephala ◽  
Phytochemical Analysis ◽  
Active Components ◽  
Active Metabolites ◽  
Egg Hatching ◽  
Senna Alata ◽  
Anthelmintic Effect

The current study evaluated the anthelmintic effect of different extracts of Leucaena leucocephala, Parkia platycephala, and Senna alata on trichostrongylid eggs and infective larvae and determined the potential active components of each plant. Dried and macerated plant material was concentrated using rotaevaporation to obtain the crude extract (CE), followed by solvent partitioning to obtain hexanic (HexE), acetatic (AcE), and butanolic (BuE) extracts used for phytochemical analysis and anthelmintic efficacy testing in vitro. All the crude and partitioned extracts tested showed inhibition activity in the hatching of trichostrongylid eggs. Larvicidal efficacy was observed at CE concentrations of 2.5, 5.0, and 7.5 mg/mL for P. platycephala and S. alata. However, L. leucocephala CE did not significantly reduce the number of living larvae in the tested concentrations. Chromatographic analysis revealed several active metabolites; gallic acid, ellagic acid, naringin, morin, and kaempferol on AcE of P. platycephala; gallic acid, rutin, and ellagic acid on BuE of P. platycephala; and gallic acid and naringin on BuE of L. leucocephala. The extracts of P. platycephala, L. leucocephala, and S. alata leaves showed egg hatching inhibition and larvicidal activity, probably produced by tannins and flavonoids, which may act alone or by synergism.

scholarly journals Antiulcer Activity and Potential Mechanism of Action of the Leaves of Spondias mombin L.

2018 ◽  
Vol 2018 ◽  
pp. 1-20 ◽  
Author(s):  
Samara Alves Brito ◽  
Cynthia Layse Ferreira de Almeida ◽  
Temístocles Italo de Santana ◽  
Alisson Rodrigo da Silva Oliveira ◽  
Jéssica Carla Bezerra do Nascimento Figueiredo ◽  
...  
Keyword(s):  
Gastric Mucosa ◽  
Gallic Acid ◽  
Ellagic Acid ◽  
Antioxidant Activities ◽  
Chronic Ulcer ◽  
Antiulcer Activity ◽  
Spondias Mombin ◽  
Sh Groups ◽  
Ulcer Model

Spondias mombin L. is used in folk medicine for the treatment of inflammation and gastrointestinal diseases. Our study investigated the antiulcer activity of S. mombin ethanolic extract (SmEE) and its majority compounds gallic acid (GA) and ellagic acid (EA). Phytochemical characterization was performed by HPLC. The SmEE was screened for in vitro antioxidant activities using phosphomolybdenum, ABTS, DPPH, and FRAP assays. The antiulcer activity of SmEE, GA, EA, or GA + EA was evaluated by gastric lesion models induced by absolute ethanol and indomethacin. Following this, it is capable of stimulating mucus production, antisecretory capacity, and the influence of −SH groups and NO in the effect of SmEE. Its healing activity was demonstrated by acetic acid-induced chronic ulcer model. Anti-Helicobacter pylori activity was assessed by determining the MIC of the SmEE (64–1024 μg/mL). The HPLC results identified the presence of gallic acid and ellagic acid in SmEE. The extract showed antioxidant activity in vitro. SmEE (50, 100, and 200 mg/kg) reduced the area of ulcerative lesions induced by ethanol in 23.8, 90.3, and 90.2%, respectively. In NSAID model, the SmEE induced protection of 36.8, 49.4, and 49.9%, respectively. GA (10 mg/kg) or EA (7 mg/kg) or the association of GA + EA (10 + 7 mg/kg) inhibited the ethanol-induced lesions in 71.8, 70.9, and 94.9%, respectively, indicating synergistic action. SmEE (100 mg/kg) decreased acid secretion and H+ concentration in the gastric contents, increased levels of mucus, and showed to be dependent of −SH groups and NO on the protection of the gastric mucosa. In chronic ulcer model, SmEE reduced the gastric area lesion. SmEE showed anti-H. pylori activity. In conclusion, our study showed that SmEE has antiulcerogenic activity. GA and EA are isolated gastric protectors and, when associated, acted synergistically to protect the gastric mucosa.

scholarly journals Quantitative Analysis and In vitro Anti-inflammatory effects of gallic acid, ellagic acid, and quercetin from radix sanguisorbae

2016 ◽  
Vol 12 (46) ◽  
pp. 104 ◽  
Author(s):  
Hyeun-Kyoo Shin ◽  
Chang-Seob Seo ◽  
Soo-Jin Jeong ◽  
Sae-Rom Yoo ◽  
Na-Ri Lee
Keyword(s):  
Quantitative Analysis ◽  
Gallic Acid ◽  
Ellagic Acid ◽  
Anti Inflammatory

scholarly journals Phenolic Compounds Isolated and Identified from Amla (Phyllanthus emblica) Juice Powder and their Antioxidant and Neuroprotective Activities

2018 ◽  
Vol 13 (10) ◽  
pp. 1934578X1801301 ◽  
Author(s):  
Kenneth Rose ◽  
Chunpeng Wan ◽  
Amber Thomas ◽  
Navindra P. Seeram ◽  
Hang Ma
Keyword(s):  
Gallic Acid ◽  
Ellagic Acid ◽  
Chemical Constituents ◽  
Butylated Hydroxytoluene ◽  
Neuroprotective Activity ◽  
Control Group ◽  
Phyllanthus Emblica ◽  
Neuroprotective Effects ◽  
Potential Health

The edible fruit of Phyllanthus emblica (known as amla and Indian gooseberry) is widely used in Eastern traditional medicinal systems for a variety of ailments. Our group has previously reported that an amla juice powder shows neuroprotective effects in several in vitro and in vivo assay models but its chemical constituents and their neuroprotective activity remain unknown. Therefore, we conducted a phytochemical investigation of amla juice powder and evaluated the antioxidant and neuroprotective effects of the isolates. Ten phenolics (1–10), including gallic acid (1), five gallic acid derivatives (2–6), ellagic acid (7), and three ellagic acid derivatives (8–10), were isolated and identified with compounds 8–10 being reported from amla for the first time. All of the isolates showed antioxidant effects in the DPPH assay with IC50 values ranging from 6-158.9 μM superior to the synthetic commercial antioxidant, butylated hydroxytoluene (IC50 = 371.4 μM). In addition, compound 8 reduced β-amyloid-induced neurotoxicity in a transgenic Caenorhabditis elegans model by increasing their survival rate by 28.3% compared to the control group. This study adds to the growing body of evidence supporting the potential health benefits of amla and supports the functional food and nutraceutical applications of amla juice powder.

scholarly journals Effect of two surfactants on in vitro permeation of butorphanol through horse nasal mucosa

Uniciencia ◽  
2021 ◽  
Vol 35 (2) ◽  
pp. 1-10
Author(s):  
María Inés Velloso ◽  
Héctor Alfredo Andreeta ◽  
María Fabiana Landoni
Keyword(s):  
Nasal Mucosa ◽  
Tween 80 ◽  
Ionic Surfactant ◽  
Apparent Permeability ◽  
In Vitro Permeation ◽  
Apparent Permeability Coefficient ◽  
Dose Control ◽  
Franz Diffusion Cells ◽  
Cetrimonium Bromide

The aim of the present study was to evaluate the effect of two surfactants on in vitro permeation of butorphanol through equine nasal mucosa. Franz diffusion cells and equine nasal mucosa were used. Three formulations were developed based on citric acid, sodium citrate, sodium chloride, and butorphanol tartrate and administered at a 24.4 g cm-3 dose. Control formulation lacked any penetration enhancer. Formulation 1 (F1) had a cationic surfactant (cetrimonium bromide) and formulation 2 (F2) had a non-ionic surfactant (Tween 80). Statistically comparing flux values at the steady state (Jss), apparent permeability coefficient (Kp), and lag-time from control, F1 and F2 for the respiratory region does not show statistically significant differences (α= 0.05). However, statistically significant differences were found on the Jss and Kp, values from control, F1, and F2 in olfactory mucosa. A statistical analysis on the latter showed significant differences between the Jss values of F1 and F2 and between control and F2. Based on this, Tween 80 proved to be a promising excipient in developing intranasal butorphanol formulations in equines since it increases its passage through the nasal mucosa. These results are very promising to continue with the development of intranasal butorphanol formulation in equines.

scholarly journals Partial Least Square Model (PLS) as a Tool to Predict the Diffusion of Steroids Across Artificial Membranes

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1387
Author(s):  
Eleni Tsanaktsidou ◽  
Christina Karavasili ◽  
Constantinos K. Zacharis ◽  
Dimitrios G. Fatouros ◽  
Catherine K. Markopoulou
Keyword(s):  
Animal Experiments ◽  
Pharmaceutical Research ◽  
Partial Least Square ◽  
Least Square ◽  
Predictive Tool ◽  
Apparent Permeability ◽  
Internal Validation ◽  
Candidate Drug ◽  
Apparent Permeability Coefficient

One of the most challenging goals in modern pharmaceutical research is to develop models that can predict drugs’ behavior, particularly permeability in human tissues. Since the permeability is closely related to the molecular properties, numerous characteristics are necessary in order to develop a reliable predictive tool. The present study attempts to decode the permeability by correlating the apparent permeability coefficient (Papp) of 33 steroids with their properties (physicochemical and structural). The Papp of the molecules was determined by in vitro experiments and the results were plotted as Y variable on a Partial Least Squares (PLS) model, while 37 pharmacokinetic and structural properties were used as X descriptors. The developed model was subjected to internal validation and it tends to be robust with good predictive potential (R2Y = 0.902, RMSEE = 0.00265379, Q2Y = 0.722, RMSEP = 0.0077). Based on the results specific properties (logS, logP, logD, PSA and VDss) were proved to be more important than others in terms of drugs Papp. The models can be utilized to predict the permeability of a new candidate drug avoiding needless animal experiments, as well as time and material consuming experiments.

scholarly journals Inhibitory Effect of Berberine on Broiler P-glycoprotein Expression and Function: In Situ and In Vitro Studies

2019 ◽  
Vol 20 (8) ◽  
pp. 1966 ◽  
Author(s):  
Yujuan Zhang ◽  
Li Guo ◽  
Jinhu Huang ◽  
Yong Sun ◽  
Fang He ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Inhibitory Effect ◽  
In Vitro Models ◽  
Apparent Permeability ◽  
Glycoprotein P ◽  
P Glycoprotein ◽  
And Function ◽  
Xenobiotic Receptor

Overcoming P-glycoprotein (P-gp) efflux is a strategy to improve the absorption and pharmacokinetics of its substrate drugs. Berberine inhibits P-gp and thereby increases the bioavailability of the P-gp substrate digoxin in rodents. However, the effects of berberine on P-gp in chickens are still unclear. Here, we studied the role of berberine in modulating broilers P-gp expression and function through both in situ and in vitro models. In addition, molecular docking was applied to analyze the interactions of berberine with P-gp as well as with chicken xenobiotic receptor (CXR). The results showed that the mRNA expression levels of chicken P-gp and CXR decreased in the ileum following exposure to berberine. The absorption rate constant of rhodamine 123 increased after berberine treatment, as detected using an in situ single-pass intestinal perfusion model. Efflux ratios of P-gp substrates (tilmicosin, ciprofloxacin, clindamycin, ampicillin, and enrofloxacin) decreased and the apparent permeability coefficients increased after co-incubation with berberine in MDCK-chAbcb1 cell models. Bidirectional assay results showed that berberine could be transported by chicken P-gp with a transport ratio of 4.20, and this was attenuated by verapamil (an inhibitor of P-gp), which resulted in a ratio of 1.13. Molecular docking revealed that berberine could form favorable interactions with the binding pockets of both CXR and P-gp, with docking scores of −7.8 and −9.5 kcal/mol, respectively. These results indicate that berberine is a substrate of chicken P-gp and down-regulates P-gp expression in chicken tissues, thereby increasing the absorption of P-gp substrates. Our findings suggest that berberine increases the bioavailability of other drugs and that drug-drug interactions should be considered when it is co-administered with other P-gp substrates with narrow therapeutic windows.

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