The effect of free fatty acids on the in-vitro binding of testosterone in human plasma

1993 ◽  
Vol 136 (2) ◽  
pp. 327-330 ◽  
Author(s):  
M. J. Diver
Keyword(s):  
Fatty Acids ◽  
Free Fatty Acids ◽  
Pregnant Women ◽  
Human Plasma ◽  
Sex Hormone Binding Globulin ◽  
Hormone Binding ◽  
In Vitro Binding ◽  
Vitro Binding ◽  
Significant Difference

ABSTRACT The effect of supraphysiological levels of free fatty acids (FFA) on the binding of testosterone to sex-hormone binding globulin (SHBG) and on non-SHBG binding in both male plasma and plasma from pregnant women was studied. Six FFAs were added to plasma as individual acids. No alteration in testosterone binding to SHBG could be demonstrated with any of the FFAs in either male plasma or plasma from pregnant women. When the same plasma was heated to destroy SHBG binding, a highly significant (P <0·01) increase in non-SHBG binding was seen in both male plasma and plasma from pregnant women when the unsaturated FFAs oleic, linoleic and linolenic acids were added. No significant difference was demonstrated with the saturated FFAs, palmitic, stearic and arachidic acids. Journal of Endocrinology (1993) 136, 327–330

Inhibition of binding of gonadal steroids to serum binding proteins by non-esterified fatty acids: the influence of chain length and degree of unsaturation

1989 ◽  
Vol 120 (2) ◽  
pp. 175-179 ◽  
Author(s):  
C. Street ◽  
R. J. S. Howell ◽  
L. Perry ◽  
S. Al-Othman ◽  
T. Chard
Keyword(s):  
Fatty Acids ◽  
Protein Binding ◽  
Unsaturated Fatty Acids ◽  
Late Pregnancy ◽  
Sex Hormone Binding Globulin ◽  
Partial Purification ◽  
Normal Female ◽  
Esterified Fatty Acids ◽  
Vitro Binding

Abstract. The effect of non-esterified fatty acids (NEFA) on the in vitro binding of testosterone, 5-alpha dihydrotestosterone and estradiol E2 to sex hormone binding globulin (SHBG) was examined using pooled normal female serum, and SHBG and albumin fractions obtained from the partial purification of late pregnancy serum. A range of saturated and unsaturated fatty acids were examined for their effect on steroid-protein binding. In normal female serum, NEFA added at physiological concentrations disrupted steroid-protein binding. The shorter chain (C8–C12) saturated acids and the poly-unsaturated acids proved to be more effective inhibitors than the longer chain saturated or mono-unsaturated acids. The greatest inhibition was obtained with E2 whereas the binding of dihydrotestosterone was least affected. With partially purified SHBG, the same concentrations of NEFA were less effective at inhibiting the binding of dihydrotestosterone and testosterone but elicited the same effect with E2. The binding of steroids to albumin appeared to be unaffected by these concentrations of NEFA.

scholarly journals Fatty Acids with in Vitro Binding Affinity for Human Opioid Receptors from the Fungus Emericella nidulans

2013 ◽  
Vol 61 (44) ◽  
pp. 10476-10480 ◽  
Author(s):  
Amer H. Tarawneh ◽  
Francisco León ◽  
Mohamed M. Radwan ◽  
Xiaoning Wang ◽  
Olivia R. Dale ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Binding Affinity ◽  
Opioid Receptors ◽  
Emericella Nidulans ◽  
In Vitro Binding ◽  
Vitro Binding

In vitro Binding of MX2 (KRN8602) and Epirubicin to Human Plasma Protein

Pharmacology ◽  
1997 ◽  
Vol 55 (6) ◽  
pp. 279-284
Author(s):  
Wei-zheng. Zhang ◽  
Walter Cosolo ◽  
John Zalcberg
Keyword(s):  
Human Plasma ◽  
Plasma Protein ◽  
In Vitro Binding ◽  
Human Plasma Protein ◽  
Vitro Binding

Postprandial free fatty acids stimulate activity of human corticosteroid binding globulin

1995 ◽  
Vol 269 (6) ◽  
pp. E1067-E1075 ◽  
Author(s):  
M. Haourigui ◽  
S. Sakr ◽  
M. E. Martin ◽  
N. Thobie ◽  
A. Girard-Globa ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Free Fatty Acids ◽  
Binding Activity ◽  
Affinity Constant ◽  
Binding Studies ◽  
Vitro Binding ◽  
Corticosteroid Binding Globulin ◽  
High Concentrations ◽  
Mixed Oil

The effect of postprandial variation of free fatty acids (FFA) on serum corticosteroid binding globulin (CBG) properties and cortisol (hydrocortisone) concentrations were explored in 11 women (20-30 yr) during 8 h after an oral load of tallow (26% C16:0, 18% C18:0, and 43% C18:1), oleic-sunflower (oleic-SF; 73% C18:1), sunflower (SF; 67% C18:2), and mixed oil (MO; 39% C18:1 and 48% C18:2). Serum FFA increased little after SF and MO but more than doubled in the late postprandial period (6 and 8 h) after oleic-SF (due to monounsaturated FFA) or tallow (due to saturated and monounsaturated FFA). CBG concentrations remained unchanged, but in relation with the postprandial elevation of serum FFA, CBG binding activity was increased after tallow or oleic-SF as a result of a combined two- to threefold increase in affinity constant and a 50% reduction in binding sites. Immunological and in vitro binding studies showed the changes in CBG behavior to be conformational and to be mediated mainly by monounsaturated FFA, especially C18:1. The modifications of CBG properties were associated with sustained high concentrations of cortisol (suppression of midday decrease) 6 and 8 h after tallow or oleic-SF. Thus dietary FFA may have an impact on bioavailability of glucocorticoids.

scholarly journals Plasma free fatty acids in hyperemesis gravidarum pregnancy

Open Medicine ◽  
2017 ◽  
Vol 12 (1) ◽  
pp. 70-75 ◽  
Author(s):  
Mustafa Ulubay ◽  
Mustafa Ozturk ◽  
Ozlem Ozturk ◽  
Ugur Keskin ◽  
Ulas Fidan ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Free Fatty Acids ◽  
Pregnant Women ◽  
Gestational Age ◽  
Neural Development ◽  
Plasma Levels ◽  
Hyperemesis Gravidarum ◽  
Saturated Fatty Acids ◽  
Nervonic Acid ◽  
Significant Difference

AbstractWe evaluated the free fatty acids differences in plasma between hyperemesis gravidarum(HG) and healthy pregnant in first trimester pregnancy.ObjectiveWe aimed to compare the plasma levels of DHA, AA and EPA, between HG patients and healthy pregnant womenDesignFifty-two pregnants were involved in the study. Twenty-six pregnants of them were HG as study group, and twenty-six pregnants were enrolled as healthy pregnant women at the similar gestational age. The saturated fatty acids C14, C15, C16, C18, C20, C22, and C24; the omega-3 fatty acids eicosapentaenoic acid, (EPA) and docosahexaenoic acid, (DHA); the omega-6 fatty acids linoleic acid, arachidonic acid (AA), and homo-gamma-linolenic acid; and the omega-9 fatty acids oleic acid, erucic acid, and nervonic acid were analysed by gas chromatography.ResultsStatistically differences was not seen between the groups with maternal age, gestational age, or plasma levels of EPA, DHA, and AA. Statistically significant difference was seen between the groups with plasma levels of C20 and C22(p<0.05). C20 was declined but C22 was rised in the HG patients.ConclusionEPA, DHA, or AA, which related to placental and fetal neural development are not changing from Hyperemesis gravidarum.

Fatty Acids with In Vitro Binding Affinity for Human Opioid Receptors from the Fungus UK-101

Planta Medica ◽  
2012 ◽  
Vol 78 (05) ◽  
Author(s):  
AH Tarawneh ◽  
MM Radwan ◽  
X Wang ◽  
O Dale ◽  
A Husni ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Binding Affinity ◽  
Opioid Receptors ◽  
In Vitro Binding ◽  
Vitro Binding

Discovery of New AKT1 Inhibitors by Combination of In silico Structure Based Virtual Screening Approaches and Biological Evaluations

2019 ◽  
Author(s):  
Filip Fratev ◽  
Denisse A. Gutierrez ◽  
Renato J. Aguilera ◽  
suman sirimulla
Keyword(s):  
Virtual Screening ◽  
Success Rate ◽  
Protein Interactions ◽  
In Silico ◽  
Biological Data ◽  
In Vitro Binding ◽  
Vitro Binding ◽  
Screening Protocol ◽  
Screening Approaches

AKT1 is emerging as a useful target for treating cancer. Herein, we discovered a new set of ligands that inhibit the AKT1, as shown by in vitro binding and cell line studies, using a newly designed virtual screening protocol that combines structure-based pharmacophore and docking screens. Taking together with the biological data, the combination of structure based pharamcophore and docking methods demonstrated reasonable success rate in identifying new inhibitors (60-70%) proving the success of aforementioned approach. A detail analysis of the ligand-protein interactions was performed explaining observed activities.<br>

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