Evaluation of female sex hormones influence on the protein-transporter p-glycoprotein functioning in vitro

2020 ◽  
Vol 66 (6) ◽  
pp. 444-449
Author(s):  
A.V. Shchulkin ◽  
I.V. Chernykh ◽  
N.M. Popova ◽  
A.A. Slepnev ◽  
E.N. Yakusheva
Keyword(s):  
Sex Hormones ◽  
Constitutive Androstane Receptor ◽  
Direct Inhibition ◽  
Protein Activity ◽  
Transporter Protein ◽  
Female Sex ◽  
Female Sex Hormones ◽  
P Glycoprotein ◽  
Increased Activity

The effects of female sex hormones estradiol and progesterone on P-glycoprotein (Pgp) functioning have been investigated using Caco-2 cells. Pgp activity was analyzed in a transwell system by the transport of its substrate, fexofenadine. The amount of the transporter protein was analyzed by enzyme immunoassay. Incubation of Caco-2 cells with 10 μM estradiol and incubation for 3 days increased activity and synthesis of Pgp. Moreover, this effect was suppressed by the inhibitor of the constitutive androstane receptor (CAR) CINPA 1. Incubation of these cells with 100 μM progesterone for 3 days increased Pgp synthesis, but its activity remained unchanged due to non-genomic (direct) inhibition of Pgp molecule by gestagen. The pregnan-X receptor inhibitor (PXR), ketoconazole suppressed the inducing effect of progesterone on Pgp synthesis. The combination of 10 μM estradiol and 100 μM progesterone increased Pgp synthesis, but did not increase the transporter protein activity, due to direct inhibition of the Pgp molecule by progestogen. Thus, it was found that estradiol increased activity and synthesis of Pgp by stimulating CAR, and progesterone stimulated transporter protein synthesis by activating PXR.

scholarly journals INFLUENCE OF POLYSACCHARIDE COMPLEXES OF PLANTS OF CENTRAL RUSSIA ON THE P-GLYCOPROTEIN ACTIVITY IN VITRO

2020 ◽  
pp. 73-81
Author(s):  
Ivan Vladimirovich Chernykh ◽  
Aleksey Vladimirovich Shchul'kin ◽  
Yekaterina Yevgen'yevna Kirichenko ◽  
Sergey Konstantinovich Pravkin ◽  
Yelena Nikolayevna Yakusheva
Keyword(s):  
High Performance ◽  
Protein Activity ◽  
Apparent Permeability ◽  
Melilotus Officinalis ◽  
Polysaccharide Complex ◽  
Transport Medium ◽  
Transporter Protein ◽  
Central Russia ◽  
P Glycoprotein

The purpose of this work was to study the effect of polysaccharide complexes isolated from tansy flowers (Tanacetum vulgare L., fam. Asteraceae) and melilotus herb (Melilotus officinalis L., fam. Fabaceae) on P-glycoprotein (Pgp, ABCB1 protein) activity in vitro. On Caco-2 cell line the effect of polysaccharide complex isolated from tansy flowers and melilotus herb on Pgp activity was studied. In vitro Pgp activity was assessed by the transport of fexofenadine in the transwell system. High performance liquid chromatography with UV detection at wavelength 220 nm was used to determine fexofenadine concentration in the transport medium. It was revealed that when polysaccharide isolated from tansy flowers was added to the transport medium in concentrations 10 and 100 μM the ratio of the apparent permeability coefficients of fexofenadine b-a/a-b decreased by 1.81 and 2.65 times, respectively, compared with the series of isolated transport of fexofenadine, which indicated decreased Pgp functional activity under the polysaccharide action. The polysaccharide complex of the melilotus herb did not change the b-a/a-b ratio in any of the applied concentrations, thus it did not affect the activity of this transporter. It is advisable to continue the study of tansy flower polysaccharide complex as an inhibitor of Pgp transporter protein in order to assess the possibility of its clinical use for the treatment of pharmacoresistant forms of cancer by overcoming the phenomenon of multidrug resistance of cells.

Inhibition of lower esophageal sphincter circular muscle by female sex hormones.

1978 ◽  
Vol 234 (3) ◽  
pp. E243 ◽  
Author(s):  
R S Fisher ◽  
G S Roberts ◽  
C J Grabowski ◽  
S Cohen
Keyword(s):  
Lower Esophageal Sphincter ◽  
Sex Hormones ◽  
Circular Muscle ◽  
Response Curves ◽  
Circular Smooth Muscle ◽  
Female Sex ◽  
Female Sex Hormones ◽  
Esophageal Sphincter ◽  
Muscle Responses

To determine the effect of estrogenic and progesteronic activity on lower esophageal sphincter (LES) circular muscle, studies were performed on 20 adult opossums. Does-response curves on circular smooth muscle strips from the LES were constructed for gastrin and acetylcholine alone, and with 17beta-estradiol and/or progesterone added. Each female hormone significantly decreased the maximal LES muscle responses to gastrin and acetylcholine. A combination of 17beta-estradiol and progesterone abolished the response to gastrin. In contrast, the male sex hormone, dihydrotestosterone, had no effect. In conclusion, administration of estrogen and progesteron, but not dihydrotestosterone, in vitro reduced LES muscle responses to gastrin and acetylcholine. These studies suggest that the female sex hormones can alter LES function and potentially may be of importance in the pathogenesis of heartburn of pregnancy.

scholarly journals Sex Disparities in Cystic Fibrosis: Review on the Effect of Female Sex Hormones on Lung Pathophysiology and Outcomes

2020 ◽  
pp. 00475-2020
Author(s):  
G.Y. Lam ◽  
J. Goodwin ◽  
P.G. Wilcox ◽  
B.S. Quon
Keyword(s):  
Cystic Fibrosis ◽  
Sex Differences ◽  
Sex Hormones ◽  
Mucociliary Clearance ◽  
Therapeutic Interventions ◽  
Female Sex ◽  
Female Sex Hormones ◽  
Sex Disparities

Sex differences in morbidity and mortality have been reported in the cystic fibrosis (CF) population worldwide. However, it is unclear why CF women have worse clinical outcomes than men. In this review, we focus on the influence of female sex hormones on CF pulmonary outcomes and summarise data from in vitro and in vivo experiments on how estrogen and progesterone might modify mucociliary clearance, immunity and infection in the CF airways. The potential for novel sex hormone related therapeutic interventions is also discussed.

Effects of female sex hormones on mitochondria: possible role in acute fatty liver of pregnancy

1995 ◽  
Vol 268 (1) ◽  
pp. G107-G115 ◽  
Author(s):  
S. Grimbert ◽  
C. Fisch ◽  
D. Deschamps ◽  
A. Berson ◽  
B. Fromenty ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Fatty Liver ◽  
Palmitic Acid ◽  
Sex Hormones ◽  
Tricarboxylic Acid Cycle ◽  
Liver Mitochondria ◽  
Female Sex ◽  
Female Sex Hormones ◽  
Acute Fatty Liver

Acute fatty liver of pregnancy occurs in some women. As other cases of microvesicular steatosis are due to impaired mitochondrial oxidation of fatty acids, we investigated the effects of female sex hormones on liver mitochondria in female mice. Three hours after administration of both estradiol (36 mumol/kg) and progesterone (150 mumol/kg), the in vitro beta-oxidation of [U-14C]palmitic acid and the activity of the tricarboxylic acid cycle decreased 49 and 54%, whereas the in vivo oxidation of [U-14C]palmitic acid decreased 38%. One week of treatment with both sex hormones produced ultrastructural lesions of mitochondria, decreased the recovery of mitochondrial proteins by 34%, increased state 4 respiration by 54-77%, and decreased the activities per gram of liver of several enzymes involved in the activation, mitochondrial uptake, and oxidation of fatty acids by 34-54%. We conclude that female sex hormones have deleterious effects on liver mitochondria and suggest that these effects, together with other factors, may contribute to the development of acute fatty liver of pregnancy in some women.

Female Sex Hormones and Epilepsy

2015 ◽  
Vol 10 (01) ◽  
pp. 65-71
Author(s):  
Chakorn Chansakul
Keyword(s):  
Sex Hormones ◽  
Female Sex ◽  
Female Sex Hormones

scholarly journals The modulation of social behavior and empathy via oral contraceptives and female sex hormones

2021 ◽  
pp. 105250
Author(s):  
Julia Strojny ◽  
Gregor Domes ◽  
Urs Fischbacher ◽  
Bernadette von Dawans
Keyword(s):  
Social Behavior ◽  
Sex Hormones ◽  
Oral Contraceptives ◽  
Female Sex ◽  
Female Sex Hormones
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