scholarly journals The Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation

Antioxidants ◽  
2021 ◽  
Vol 10 (11) ◽  
pp. 1826
Author(s):  
Sandra Flory ◽  
Romina Männle ◽  
Jan Frank
Keyword(s):  
Cell Culture ◽  
Inhibitory Activity ◽  
Important Determinant ◽  
Biological Activities ◽  
Intestinal Cells ◽  
Free Medium ◽  
Clear Effect ◽  
P Glycoprotein ◽  
Pre Treatment ◽  
Culture Supernatants

The biological activities of curcumin in humans, including its antioxidative and anti-inflammatory functions, are limited by its naturally low bioavailability. Different formulation strategies have been developed, but the uptake of curcumin from these galenic formulations into and efflux from intestinal cells, which may be critical processes limiting bioavailability, have not been directly compared. Furthermore, little is known about their effect on P-glycoprotein activity, an important determinant of the pharmacokinetics of potentially co-administered drugs. P-glycoprotein activity was determined in LS180 cells, incubated with 30 or 60 µmol/L of curcumin in the form of seven different formulations or native curcuma extract for 1 h. All formulations inhibited P-glycoprotein activity at both concentrations. Curcumin uptake, after 1 h incubation of LS180 cells with the formulations (60 µmol/L), showed significant variability but no consistent effects. After 1 h pre-treatment with the formulations and further 8 h with curcumin-free medium, curcumin in cell culture supernatants, reflecting the efflux, differed between individual formulations, again without a clear effect. In conclusion, curcumin inhibits P-glycoprotein activity independently of its formulation. Its uptake by and efflux from intestinal cells was not significantly different between formulations, indicating that these processes are not important regulatory points for its bioavailability.

scholarly journals The Coconut Water Antimicrobial Peptide CnAMP1 Is Taken up into Intestinal Cells but Does Not Alter P-Glycoprotein Expression and Activity

2020 ◽  
Vol 75 (3) ◽  
pp. 396-403
Author(s):  
Katya Anaya ◽  
Maren Podszun ◽  
Octavio Luiz Franco ◽  
Carlos Alberto de Almeida Gadelha ◽  
Jan Frank
Keyword(s):  
Antimicrobial Peptide ◽  
Cellular Uptake ◽  
Biological Activities ◽  
Cocos Nucifera ◽  
Coconut Water ◽  
Intestinal Cells ◽  
Glycoprotein P ◽  
P Glycoprotein ◽  
Physiological Relevance ◽  
Expression And Activity

AbstractCoconut antimicrobial peptide-1 (CnAMP1) is a naturally occurring bioactive peptide from green coconut water (Cocos nucifera L.). Although biological activities have been reported, the physiological relevance of these reports remains elusive as it is unknown if CnAMP1 is taken up into intestinal cells. To address this open question, we investigated the cytotoxicity of CnAMP1 in intestinal cells and its cellular uptake into human intestinal cells. Considering the importance of the P-glycoprotein (P-gp) to the intestinal metabolism of xenobiotics, we also investigated the influence of CnAMP1 on P-gp activity and expression. Both cell lines showed intracellular fluorescence after incubation with fluorescein labelled CnAMP1, indicating cellular uptake of the intact or fragmented peptide. CnAMP1 (12.5–400 μmol/L) showed no signs of cytotoxicity in LS180 and differentiated Caco-2 cells and did not affect P-gp expression and activity. Further research is required to investigate the identity of CnAMP1 hydrolysis fragments and their potential biological activities.

Screening of Actinomycetes For α-amylase Inhibitors Production

2019 ◽  
Vol 15 (1) ◽  
pp. 41-45
Author(s):  
Shivabai Chandwad ◽  
Sudhakar Gutte
Keyword(s):  
Inhibitory Activity ◽  
Enzyme Inhibitors ◽  
Spectroscopic Method ◽  
Solid Material ◽  
Soil Samples ◽  
Assay Method ◽  
Novel Drugs ◽  
Pre Treatment ◽  
Diabetic Treatment ◽  
Amylase Inhibitors

Background:Diabetes mellitus is the most common and fastest growing disease in the world. One of the therapies to treat diabetes is the inhibition of α-amylase activity by inhibitors from microbial and plant source. Actinomycetes are potential sources of enzyme inhibitors, drugs, amino acids, vitamins etc.Objective:Our work mainly highlights the isolation of actinomycetes from soil samples of different habitats and screening of α -amylase inhibitors.Methods:Actinomycetes were isolated from soil samples of different habitats by different methods; these include a variety of pre-treatment of soil samples in combination with an appropriate supplement medium with selective antibacterial agents. Isolated actinomycetes grown in fermentation condition and metabolites were extracted with Isopropyl alcohol and concentrated to obtain solid material. The extract of each isolate was tested for α -amylase inhibition using starch Iodine plate method and DNS- spectroscopic method.Results:Total 110 actinomycetes strains were isolated from various sources. Among 110 extracts of actinomycetes, eight extracts have shown positive results for α-amylase inhibition in starch Iodine plate assay method. Extracts selected from primary results were used for the confirmation of inhibitory activity using DNS- spectroscopic method. Out of eight extracts, six extracts showed Porcine pancreatic α -amylase inhibitory activity ranging from 40-86%. The actinomycetes strains that produce α -amylase inhibitory activity are A-24, A-29, B-5, B-18, C-15 and D-24.Conclusion:These results show that actinomycetes are a potential source for α -amylase inhibitors, which may lead to valuable novel drugs for diabetic treatment.

Nω-Hydroxy-L-arginine and Its Homologues. Chemical and Biological Properties. A Review

2004 ◽  
Vol 69 (3) ◽  
pp. 499-510 ◽  
Author(s):  
Petra Beranová ◽  
Karel Chalupský ◽  
Gustav Entlicher
Keyword(s):  
Inhibitory Activity ◽  
Biological Activities ◽  
Biological Effects ◽  
Biological Properties ◽  
No Synthase ◽  
Point Of View ◽  
No Donor ◽  
Good Substrate ◽  
No Formation ◽  
Vasorelaxant Activity

Nω-Hydroxy-L-arginine (NOHA) is a stable intermediate in NO formation from L-arginine catalyzed by NO synthase (NOS). Apparently, NOHA can be released and serve as a stable reserve NO donor (as a substrate of NOS) or transported and exert its own biological effects. It shows endothelium-dependent as well as endothelium-independent vasorelaxant activity. The latter case indicates that NOHA can be metabolized by pathways independent of NOS. These possibilities are discussed in detail. Of the available NOHA homologues homo-NOHA is a good substrate of NOS while nor-NOHA seems to be a very poor substrate of this enzyme. On the contrary, nor-NOHA exerts arginase inhibitory activity 20 times higher than NOHA whereas homo-NOHA is inactive. Detailed investigation of biological activities of NOHA and its homologues seems to be promising from the pharmacological point of view. A review with 43 references.

scholarly journals Volatile terpenoids as potential drug leads in Alzheimer’s disease

2017 ◽  
Vol 15 (1) ◽  
pp. 332-343 ◽  
Author(s):  
Karolina A. Wojtunik-Kulesza ◽  
Katarzyna Targowska-Duda ◽  
Katarzyna Klimek ◽  
Grażyna Ginalska ◽  
Krzysztof Jóźwiak ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Mtt Assay ◽  
Inhibitory Activity ◽  
Biological Activities ◽  
Plant Metabolites ◽  
Secondary Plant Metabolites ◽  
Docking Simulations ◽  
Ache Inhibitory Activity ◽  
Volatile Terpenoids

AbstractAlzheimer’s disease (AD) is by far the most prevalent of all known forms of dementia. Despite wide-spread research, the main causes of emergence and development of AD have not been fully recognized. Natural, low-molecular, lipophilic terpenoids constitute an interesting group of secondary plant metabolites, that exert biological activities of possible use in the prevention and treatment of AD. In order to identify secondary metabolites possessing both antioxidant activity and the potential to increase the level of acetylcholine, selected terpenoids have been screened for possible acetylcholinesterase inhibitory activity by use of two methods, namely Marston (chromatographic assay) and Ellman (spectrophotometric assay). In order to describe the interaction between terpenes and AChE active gorge, molecular docking simulations were performed. Additionally, all analyzed terpenes were also evaluated for their cytotoxic properties against two normal cell lines using MTT assay. The obtained results show that: carvone (6), pulegone (8) and γ-terpinene (7) possess desirable AChE inhibitory activity. MTT assay revealed low or lack of cytotoxicity of these metabolites. Thus, among the investigated terpenes, carvone (6), pulegone (8) and y-terpinene (7) can be recognized as compounds with most promising activities in the development of multi-target directed ligands.

Free flow electrophoresis allows quick preparation of extracellular vesicles from cell culture supernatants and human plasma

Cytotherapy ◽  
2021 ◽  
Vol 23 (5) ◽  
pp. S118
Author(s):  
S. Staubach ◽  
T. Tertel ◽  
V. Börger ◽  
C. Grätz ◽  
M. Pfaffl ◽  
...  
Keyword(s):  
Cell Culture ◽  
Human Plasma ◽  
Extracellular Vesicles ◽  
Free Flow ◽  
Culture Supernatants

Treatment of Groundwater with Slow Sand Filtration

1988 ◽  
Vol 20 (3) ◽  
pp. 141-147 ◽  
Author(s):  
T. Hatva
Keyword(s):  
Biological Activities ◽  
Treatment Phase ◽  
Purification Process ◽  
Sand Filtration ◽  
Sand Filters ◽  
Slow Sand Filtration ◽  
Filtration Method ◽  
Pre Treatment ◽  
Full Scale Tests ◽  
Iron Manganese

The purification process and techniques of the slow sand filtration method for treatment of groundwater was studied on the basis of pilot plant and full scale tests and studies of waterworks, to obtain guidelines for construction and maintenance. The purification process consists in general of two principal phases which are pre-treatment and slow sand filtration. Both are biological filters. The main purpose of the pre-treatment is to reduce the iron content of raw water, in order to slow down the clogging of the slow sand filters. Different types of biofilters have proved very effective in the pre-treatment phase, with reduction of total iron from 50 % to over 80 %. During the treatment, the oxidation reduction conditions gradually change becoming suitable for chemical and biological precipitation of iron, manganese and for oxidation of ammonium. Suitable environmental conditions are crucial in the oxidation of manganese and ammonium which, according to these studies, mainly occurs in slow sand filters, at the end of the process. Low water temperature in winter does not seem to prevent the biological activities connected with the removal of iron, manganese and ammonium, the chief properties necessitating treatment of groundwater in Finland.

scholarly journals Constituents of Acacia nilotica (L.) Delile with Novel Kinase Inhibitory Activity

2017 ◽  
Vol 4 (03) ◽  
pp. e108-e113 ◽  
Author(s):  
Augustine Ahmadu ◽  
Abdulkarim Agunu ◽  
Thi-Ngoc-Dung Nguyen ◽  
Blandine Baratte ◽  
Béatrice Foll-Josselin ◽  
...  
Keyword(s):  
Protein Kinases ◽  
Anticancer Agents ◽  
Inhibitory Activity ◽  
Ethyl Acetate Extract ◽  
Biological Activities ◽  
Bone Cancer ◽  
Acacia Nilotica ◽  
Tropical Africa ◽  
Ic50 Value ◽  
Kinase Inhibitory Activity

Abstract Acacia nilotica (L.) Delile belongs to the genus Acacia, which includes about 1400 species in subtropical and tropical Africa including Nigeria, Senegal, Egypt, and Mozambique as well as Asia from India to Burma. This plant is traditionally used to treat several pathologies such as mouth, ear, and bone cancer. Moreover, it possesses many other biological activities (antidiarrheal, anti-inflammatory, antimicrobial, and antifungal). We report here the extraction, purification, and identification of two known compounds [ethylgallate and (+)-catechin] from the bark of the tree that were further tested for their inhibitory activities against a panel of disease-related protein kinases. Both compounds were active, and (+)-catechin showed the best activity by inhibiting nine out of fourteen protein kinases with an IC50 value in the µg/mL range. This compound gave the highest activity against CLK1 with an IC50 of 2.1 µg/mL. The ethyl acetate extract and its components, such as catechins and other polyphenols, which also had protein kinase inhibitory activity, can be exploited in the research for anticancer agents.

scholarly journals The Effects of Maternal Smoking on Pregnancy and Offspring: Possible Role for EGF?

2021 ◽  
Vol 9 ◽  
Author(s):  
Hamed Janbazacyabar ◽  
Marthe van Daal ◽  
Thea Leusink-Muis ◽  
Ingrid van Ark ◽  
Johan Garssen ◽  
...  
Keyword(s):  
Cell Culture ◽  
Immune Responses ◽  
Spleen Cell ◽  
Cigarette Smoke ◽  
Mammary Glands ◽  
Smoke Exposure ◽  
Cigarette Smoke Exposure ◽  
Positive Correlation ◽  
Spleen Cell Culture ◽  
Culture Supernatants

Cigarette smoke exposure during pregnancy and lactation is associated with adverse pregnancy outcomes. Here, we investigated the effects of maternal smoke exposure on pregnancy and offspring immunity and explored whether, epidermal growth factor (EGF), an important growth-promoting factor in human colostrum and milk, might be a possible missing link in maternal smoke exposure and changes in infants’ immune responses. Pregnant BALB/c mice were exposed to either cigarette smoke or air during gestation and lactation, and effects on pulmonary inflammation in dams and immune responses in offspring were examined. Maternal smoke exposure increased airway hyperresponsiveness and accumulation of inflammatory cells in the lungs of pregnant dams compared to non-pregnant dams. The E-cadherin protein expression was reduced in mammary glands of cigarette smoke-exposed pregnant dams. EGF levels were higher in mammary glands and serum of smoke-exposed pregnant dams compared to air-exposed pregnant dams. Offspring from cigarette smoke-exposed dams exhibited elevated levels of IL-17A, MCP-1, IL-22, and IL-13 in anti-CD3 stimulated spleen cell culture supernatants. EGF levels were also increased in serum of offspring from smoke-exposed dams. A positive correlation was observed between serum EGF levels and neutrophil numbers in bronchoalveolar lavage fluid of the dams. Interestingly, IL-17A, MCP-1, IL-22, IL13, and IFN-γ levels in anti-CD3 stimulated spleen cell culture supernatants of male pups also showed a positive correlation with EGF serum levels. In summary, our results reveal that maternal smoke exposure predisposes dams to exacerbated airway inflammation and offspring to exacerbated immune responses and both phenomena are associated with elevated EGF concentrations.

scholarly journals Transport of Alzheimer’s associated amyloid-β catalyzed by P-glycoprotein

PLoS ONE ◽  
2021 ◽  
Vol 16 (4) ◽  
pp. e0250371
Author(s):  
James W. McCormick ◽  
Lauren Ammerman ◽  
Gang Chen ◽  
Pia D. Vogel ◽  
John G. Wise
Keyword(s):  
Cell Culture ◽  
Atp Hydrolysis ◽  
Amyloid Β ◽  
Md Simulations ◽  
Membrane Transporter ◽  
Biochemical Activity ◽  
Glycoprotein P ◽  
P Glycoprotein ◽  
Hydrolysis Activity

P-glycoprotein (P-gp) is a critical membrane transporter in the blood brain barrier (BBB) and is implicated in Alzheimer’s disease (AD). However, previous studies on the ability of P-gp to directly transport the Alzheimer’s associated amyloid-β (Aβ) protein have produced contradictory results. Here we use molecular dynamics (MD) simulations, transport substrate accumulation studies in cell culture, and biochemical activity assays to show that P-gp actively transports Aβ. We observed transport of Aβ40 and Aβ42 monomers by P-gp in explicit MD simulations of a putative catalytic cycle. In in vitro assays with P-gp overexpressing cells, we observed enhanced accumulation of fluorescently labeled Aβ42 in the presence of Tariquidar, a potent P-gp inhibitor. We also showed that Aβ42 stimulated the ATP hydrolysis activity of isolated P-gp in nanodiscs. Our findings expand the substrate profile of P-gp, and suggest that P-gp may contribute to the onset and progression of AD.

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