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Conclusion
Published in Linda M. Castell, Samantha J. Stear (Nottingham), Louise M. Burke, Nutritional Supplements in Sport, Exercise and Health, 2015
Samantha J. Stear, Linda M. Castell, Louise M. Burke
In Figure 48, the supplements reviewed in this book that we have assigned to the ‘Caution’ category are: androstenediol (prohormone); androstenedione (DIONE); DHEA (Didehydroepiandrosterone); prohormones (19-nor steroid group); DMAA; Jack3D; oxyElite Pro; colostrum-bovine; ephedra; γ-hydroxybutyrate and γ-butyrolactone (GHB and GBL); glucuronolactone; glycerol; Hydroxycut; melamine; pangamic acid; peptides-synthetic; tribulus; weight loss supplements: herbal; and yohimbine. The rationale for the rating of caution for each product is explained in the summary and comments section of the table.
Hormones and Cancer
Published in Peter G. Shields, Cancer Risk Assessment, 2005
Heather Spencer Feigelson, Roberta McKean-Cowdin
There are two androgen synthesis pathways that occur in the adrenals and the testes. The 5-delta pathway is most common in humans, whereas the 4-delta pathway is common in rodents. Both pathways begin with the rate-limiting conversion of cholesterol to prenenolone through the action of CYP11A1, as previously described. The 5-delta pathway consists of the conversion of pregnenolone to 17-alpha hydroxy-pregnenolone and subsequently dehydroepiandrosterone (DHEA) through the action of CYP17 in either the testes or the adrenals. Dehydroepiandrosterone is then converted to androstenediol in the testes by HSD17B3. The final step of the 5-delta pathway, also limited to the testes, is the metabolism of androstene-diol to testosterone by the enzyme HSD3B2.
Formation and Metabolism of Steroid Conjugates: Effect of Conjugation on Excretion and Tissue Distribution
Published in Ronald Hobkirk, Steroid Biochemistry, 1979
P. I. Musey, K. Wright, J. R. K. Preedy, D. C. Collins
Other androgen sulfates have been identified in human peripheral plasma by gasliquid chromatography after chromatography and solvolysis. Laatikainen et al.132 found androstenediol monosulfate (40 to 90 ng/mℓ free steroid) and disulfate (80 to 160 ng/mℓ free steroid). Similar values for the monosulfate (30 to 190 ng/mℓ free steroid) and disulfate (70 to 580 ng/mℓ free steroid) were found by Jänne et al.124 In addition, they measured epiandrosterone-3β-sulfate (30 to 430 ng/mℓ free steroid) and 5-androstene-3β, 17α-diol disulfate (30 to 150 ng/mℓ free steroid).124
A prospective study examining isolated acne and acne with hyperandrogenic signs in adult females
Published in Journal of Dermatological Treatment, 2021
Prekshi Bansal, Kabir Sardana, Lokesh Sharma, Umesh Chandra Garga, Gauri Vats
Androgen excess in adult females can manifest either biochemically or clinically or both. Clinical hyperandrogenism in form of acne, hirsutism, alopecia and irregular menses could exist even in the absence of raised serum androgens due to end organ hypersensitivity (22). The dichotomy between the high proportion of women with clinician signs of androgen excess without concomitant laboratory values has been reported previously (23) and can be explained by the role of tissue derived androgens. Cutaneous 5 alpha reductase converts testosterone to a more potent pure androgen called DHT (dihydrotestosterone) which exerts androgenic effects via its metabolite 3 alpha androstenediol glucuronide (3alpha-diol) which is a surrogate marker of peripheral androgen excess (24). Studies have shown that high levels of alpha androstenediol glucuronide and androsteroneglucuronide have been reported in women with acne with normal circulating hormones (25,26) and can explain our finding.
Lead optimization of 4-(thio)-chromenone 6-O-sulfamate analogs using QSAR, molecular docking and DFT – a combined approach as steroidal sulfatase inhibitors
Published in Journal of Receptors and Signal Transduction, 2021
The role of estrogens in breast cancer involves two different mechanisms i) Estrogens synthesized in the ovaries and a Luteinizing Hormone Releasing Hormone (LHRH) agonist suppresses the function of pituitary hormone to promote estrogen synthesis in pre-menopausal women, ii) In post-menopausal women, androgen secreted from adrenal glands synthesize estrogens [9,10]. In recent years, studies have been carried out to predict the mechanism by which estrogens are biosynthesized; intensive research is being done in identifying a novel target that prevents the synthesis of estrogens. In mammary gland an enzyme Steroidal Sulfatase (STS) plays a major role in the biosynthesis of estrogen. STS catalyzes the conversion of biologically inactive steroid sulfates (steroid-3-sulfate) into biologically active unsulfated derivatives (3-hydroxy steroid). The three major advantage of targeting STS are i) at molecular level, 87% of breast cancer patients showed higher expression of STS mRNA levels in malignant tissues [11] ii) the activity of STS in cancer tissue is several hundred times more than that of aromatase pathway [12] iii) 5-androstenediol, a steroid circulates in postmenopausal women binds to ER and stimulates the growth of ER + breast cancer cells. Thus, STS would be a more promising target in discovering novel candidate for the treatment of breast cancer.
KMRC011, an agonist of toll-like receptor 5, mitigates irradiation-induced tissue damage and mortality in cynomolgus monkeys
Published in Journal of Immunotoxicology, 2020
Hong-Soo Lee, Doo-Wan Cho, Ji-Seok Han, Su-Cheol Han, Sang Keun Woo, Soo-Youn Jun, Woo-Jong Lee, Susie Yoon, Son-Il Pak, Sang-Jin Lee, Eunsol Seong, Eun-Jung Park
Only a few medical radiation countermeasures (MRC), e.g. 5-androstenediol/Neumune (Hollis-Eden Pharmaceuticals, San Diego, CA), beclomethasone dipropionate (BDP)/OrbeShield (Soligenix, Princeton, NJ), BIO 300/Genistein (Humanetics Pharmaceuticals, Edina, MN), CBLB502/Entolimod (Cleveland BioLabs, Buffalo, NY), HemaMax/NMIL 12-1 (Neumedicines, Pasadena, CA), and ON01210/Ex-RAD/Recilisib (Onconova Therapeutics, Newtown, PA) have to date been granted investigational new drug (IND) status (Singh et al. 2015). Three types of therapeutics, e.g. Filgrastim/Neupogen (Amgen, Thousand Oaks, CA), Pegfilgrastim-Neulasta (Amgen), and Sargramostim/Leukine (Sanofi-Aventis, Bridgewater, NJ), were recently approved by the US FDA based on a successful strategy. For example, BDP/OrbeShield was shown to significantly improve survival rates/mitigate gastrointestinal damage among canines with ARS caused by exposure to lethal doses of TBI (Singh et al. 2015). Even so, the use of these MRC candidates has been limited to patients with radiation-induced myelosuppression (ARS hemato-poietic sub-syndrome). To date, although a few MRC have been approved for use in treating patients with hematopoietic ARS, no MRC has been approved by the US FDA for general use to treat gastrointestinal ARS sub-syndrome (Shi et al. 2017; US Food and Drug Administration 2019).