Plant Constituents Interfering with Human Sex Hormone-Binding Globulin. Evaluation of a Test Method and Its Application to Urtica dioica Root Extracts

1995 ◽  
Vol 50 (1-2) ◽  
pp. 98-104 ◽  
Author(s):  
Dietmar Ganßer ◽  
Gerhard Spiteller

Abstract A test system is described, which allows the search for compounds interfering with human sex hormone-binding globulin (SHBG) even in complex plant extracts. The method has been evaluated and applied to Urtica dioica root extracts. The lignan secoisolariciresinol (5) as well as a mixture of isomeric (11 E)-9,10,13-trihydroxy-11-octadecenoic and (10 E)-9 ,12,13-trihydroxy-10-octadecenoic acids (3 and 4, resp.) were demonstrated to reduce binding activity of human SHBG. Methylation of the mixture of 3 and 4 increased its activity about 10-fold.

1986 ◽  
Vol 112 (4) ◽  
pp. 603-608 ◽  
Author(s):  
G. L. Hammond ◽  
M. S. Langley

Abstract. Sex hormone binding globulin (SHBG) and corticosteroid binding globulin (CBG) were detected by specific immunoassays in mixed-saliva taken from normal men and women. The immunochemical identity of both proteins was demonstrated by parallelism between dose response curves generated by serial dilutions of saliva and standards in the immunoassays. In addition, the specific removal of both proteins by incubation with steroid affinity-chromatography gels demonstrated the integrity of their steroid binding activity. The mean ± sd concentrations of SHBG (pmol/l) and CBG (μg/l) in mixed-saliva taken from normal volunteers were as follows: men (n = 6) 19 ± 10 and 38 ± 18; women (n = 6) 63 ± 60 and 72 ± 71 and women during late pregnancy (n = 6) 282 ± 168 and 92 ± 80, respectively. The data indicate that the concentrations of SHBG and CBG in saliva represent ∼ 0.1% of plasma concentrations. It is suggested that these proteins pass from the blood to saliva in a non-specific manner, and may influence the steroid content of saliva under certain physiological circumstances.


Author(s):  
S K Cunningham ◽  
T J McKenna

It is possible that alterations in sex hormone-binding globulin (SHBG) binding capacity are due to changes in binding kinetics rather than changes in concentration and, therefore, the immunoreactivity of SHBG may not reflect the binding activity. In this study an immunoradiometric (IRMA) assay was evaluated and the results compared with those of an established binding capacity assay. The correlation between the results of the IRMA ( y) and binding assay ( x) for 179 specimens was r=0·984, y=0·95 x+5·9. Irrespective of the method used, SHBG values in normal non-pregnant women were significantly ( P<0·05) higher than those in normal men, hirsute women, women with polycystic ovary syndrome, hyperprolactinaemic women and obese women, and were significantly less than those in pregnant women; SHBG levels in hirsute women rose during treatment with certain anovulants and fell in genetic males during the second decade of life independent of androgen levels or activity. While being technically simpler SHBG-IRMA provides comparable results to the classical binding assay, indicating that immunoreactivity is an excellent index of binding activity.


2019 ◽  
Vol 295 (5) ◽  
pp. 1202-1211 ◽  
Author(s):  
Phillip Round ◽  
Samir Das ◽  
Tsung-Sheng Wu ◽  
Kristiina Wähälä ◽  
Filip Van Petegem ◽  
...  

Sex hormone–binding globulin (SHBG) determines the equilibrium between free and protein-bound androgens and estrogens in the blood and regulates their access to target tissues. Using crystallographic approaches and radiolabeled competitive binding-capacity assays, we report here how two nonsteroidal compounds bind to human SHBG, and how they influence androgen activity in cell culture. We found that one of these compounds, (−)3,4-divanillyltetrahydrofuran (DVT), present in stinging nettle root extracts and used as a nutraceutical, binds SHBG with relatively low affinity. By contrast, a synthetic compound, 3-(1H-imidazol-1-ylmethyl)-2phenyl-1H-indole (IPI), bound SHBG with an affinity similar to that of testosterone and estradiol. Crystal structures of SHBG in complex with DVT or IPI at 1.71–1.80 Å resolutions revealed their unique orientations in the SHBG ligand-binding pocket and suggested opportunities for the design of other nonsteroidal ligands of SHBG. As observed for estradiol but not testosterone, IPI binding to SHBG was reduced by ∼20-fold in the presence of zinc, whereas DVT binding was almost completely lost. Estradiol-dependent fibulin-2 interactions with SHBG similarly occurred for IPI-bound SHBG, but not with DVT-bound SHBG. Both DVT and IPI increased the activity of testosterone in a cell culture androgen reporter system by competitively displacing testosterone from SHBG. These findings indicate how nonsteroidal ligands of SHBG maybe designed to modulate the bioavailability of sex steroids.


1989 ◽  
Vol 1 (4) ◽  
pp. 289 ◽  
Author(s):  
SM Campo ◽  
PA Rogers ◽  
JK Findlay

Androgen binding activity, indistinguishable from sex-hormone-binding globulin (SHBG) in serum, has been identified in human follicular fluid by binding analyses (saturation and Scatchard analyses and binding specificity), immunoradiometric assay and Con-A Sepharose chromatography. Follicular fluid was obtained at the time of oocyte recovery from either individual follicles (range 2-7) from seven patients, or as a pool obtained from follicles of several patients who had received a Clomid-human menopausal gonadotrophin treatment to stimulate follicular growth as part of an in vitro fertilization program. Concentrations of SHBG in follicular fluid varied between individual follicles (750 +/- 202 fmol mg-1 protein; mean +/- s.d.; n = 14) and ranged above and below concentrations of SHBG in serum (948 +/- 171 fmol mg-1 protein; n = 5) taken 4 h before oocyte recovery and harvest of follicular fluid. There were strong correlations (r = 0.7-0.9) between the steroid and SHBG contents in individual follicular fluids of two patients. However, the concentration of SHBG in follicular fluid was generally 100-fold lower than that of oestradiol or progesterone, suggesting that SHBG may play some role other than determining the concentration of unbound steroid in the follicle.


1982 ◽  
Vol 101 (2) ◽  
pp. 248-253 ◽  
Author(s):  
Viveca Odlind ◽  
Kerstin Elamsson ◽  
Doris E. Englund ◽  
Arne Victor ◽  
Elof D. B. Johansson

Abstract. Sex hormone binding globulin (SHBG) levels were studied for possible effects of oestradiol-17β on SHBG. No change in SHBG plasma was recorded during normal menstrual cycles or during treatment with oestradiol-17β to menopausal women. However, gonadotrophin treatment to amenorrhoeic women to induce ovulation resulted in high oestradiol concentrations and a pronounced increase in SHBG was found during the luteal phase of these cycles. A marked increase of SHBG was also recorded in a woman with pronounced fluctuations of oestradiol during treatment with levonorgestrel sc implants for contraception. In conclusion, effects on SHBG were only found when extraordinarily high levels of plasma oestradiol were recorded.


1987 ◽  
Vol 116 (3_Suppl) ◽  
pp. S144 ◽  
Author(s):  
G. SINNECKER ◽  
E. LUDWIG ◽  
A. KRENZ ◽  
R.P. WILLIG

Sign in / Sign up

Export Citation Format

Share Document