Testosterone and Aromatase Inhibition

CLINICAL PEARLS: Testosterone and Aromatase inhibition Restoring and maintaining adequate Testosterone levels is important for overall health and wellbeing. Restoring Testosterone levels is commonly achieved by hormone replacement therapy and can be maintained by following a healthy diet, maintaining a healthy weight, exercising regularly, and practicing good sleep hygiene. Before initiating hormone replacement therapy, it is important that all hormone levels are evaluated by saliva testing to aid in choosing the safest and most effective treatment plan and to ensure that a therapeutic Testosterone level is accurately achieved. The Aromatase Enzyme When restoring testosterone levels with exogenous hormone replacement therapy, it’s important to understand that one may experience unwanted side effects including feeling tired, developing male breasts, abdominal weight gain, loss of muscle mass, and emotional/mood disturbances. The cause of these side effects is not specific to any preparation (gel, cream, troche, pellets, etc.), but are caused more specifically by the way that Testosterone is metabolized within in the body. When Testosterone is replaced, the hormone becomes free in the body and is available for the catalyzing the aromatase enzyme to covert the Testosterone into Estrogen. This biochemical process is referred to as aromatization. Aromatase inhibitors Currently, there is drug therapy available to prevent these unwanted side effects. Prescription medications such as Progesterone and Anastrozole are available to suppress Estrogen production and mitigate unwanted side effects by inhibiting the aromatase enzyme. Moreover, Chrysin and Saw Palmetto are both natural supplements that inhibit the conversion of Testosterone to Estrogen and are commonly used to improve prostate health. These pharmaceutical grade products are relatively affordable and available over the counter. Furthermore, Saw Palmetto is said to increase libido, prevent hair loss, and alleviate stress, which, in turn, aid in relieving symptoms of andropause. Consult with our Pharmacists about developing a rational treatment plan that aims to provide positive outcomes to your health and wellbeing while on Testosterone replacement therapy. By: Jason Solano, PharmD candidate 2020, UNM College of Pharmacy .

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DHEA: Dehydroepiandrosterone
DHEA: Dehydroepiandrosterone Joseph Pepping, Pharm.D. [Am J Health-Syst Pharm 57(22):2048-2056, 2000. © 2000 ASHP, Inc.] Introduction Dehydroepiandrosterone (DHEA) and its active metabolite, DHEA sulfate (DHEAS), are endogenous hormones synthesized and excreted primarily by the zona reticularis of the adrenal cortex in response to adrenocorticotropic hormone. The exact mechanism of action and clinical role, if any, of DHEA and DHEAS remain unclear. Epidemiological data indicate an inverse relationship between serum DHEA and DHEAS levels and the frequency of cancer, cardiovascular disease (in men only), Alzheimer's disease and other age-related disorders, immune function, and progression of HIV infection. [1] Animal (primarily rodent) studies have suggested many beneficial effects of DHEA, including improved immune function and memory and prevention of atherosclerosis, cancer, diabetes, and obesity. Many of the benefits seen in animal studies have yet to be shown in humans. [1-3] Uses Clinically substantiated (yet still controversial) uses of DHEA include replacement therapy in patients with low serum DHEA levels secondary to chronic disease, adrenal exhaustion, or corticosteroid therapy; treating systemic lupus erythematosus (SLE), improving bone density in postmenopausal women; improving symptoms of severe depression; improving depressed mood and fatigue in patients with HIV infection; and increasing the rate of reepithelialization in patients undergoing autologous skin grafting for burns. [1,4-8] Other possible uses (with some supporting clinical studies) include enhancing the immune response and sense of well-being in the elderly, decreasing certain cardiovascular risk factors, and treating male erectile dysfunction. [4,8-12] Use of DHEA to slow or reverse the aging process, improve cognitive function, promote weight loss, increase lean muscle mass, or slow the progression of Parkinson's disease and Alzheimer's disease is clinically unsubstantiated.
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Exerts Anxiolytic-Like Effects Through GABAA Receptors in a Surgical Menopause Model in Rats
Biomedicine & Pharmacotherapy 109 (2019) 2387–2395 Contents lists available at ScienceDirect Biomedicine & Pharmacotherapy journal homepage: www.elsevier.com/locate/biopha Original article Chrysin (5,7-dihydroxyflavone) exerts anxiolytic-like effects through GABAA receptors in a surgical menopause model in rats T ⁎ Juan Francisco Rodríguez-Landaa,b, , Fabiola Hernández-Lópezc, Jonathan Cueto-Escobedoa, Emma Virginia Herrera-Huertad, Eduardo Rivadeneyra-Domínguezb, Blandina Bernal-Moralesa,b, Elizabeth Romero-Avendañod a Laboratorio de Neurofarmacología, Instituto de Neuroetología, Universidad Veracruzana, Xalapa, Veracruz, Mexico b Facultad de Química Farmacéutica Biológica, Universidad Veracruzana, Xalapa, Veracruz, Mexico c Hospital General de Zona con Medicina Familiar No. 28, Delegación Veracruz Norte, Instituto Mexicano del Seguro Social (H.G.Z. c/mf. No. 28, Delegación Veracruz Norte, IMSS), Martínez de la Torre, Veracruz, Mexico d Facultad de Ciencias Químicas, Universidad Veracruzana, Orizaba, Veracruz, Mexico ARTICLE INFO ABSTRACT Keywords: The present study investigated the effects of the flavonoid chrysin (5,7-dihydroxyflavone) on anxiety-like be- Anxiolytics havior in rats in a model of surgical menopause and evaluated the participation of γ-aminobutyric acid-A Chrysin (GABAA) receptors in these actions. At 12 weeks post-ovariectomy, the effects of different doses of chrysin (0.5, GABAA 1, 2, and 4 mg/kg) were evaluated in the elevated plus maze, light/dark test, and locomotor activity test, and Oophorectomy comparisons were made with the clinically effective anxiolytic diazepam. The participation of GABA receptors Ovariectomy A in the actions of chrysin was explored by pretreating the rats with the noncompetitive GABA chloride ion Surgical menopause A channel antagonist picrotoxin (1 mg/kg). The results showed that chrysin (2 and 4 mg/kg) reduced anxiety-like behavior in both the elevated plus maze and light/dark test, and these effects were similar to diazepam.
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2020 Formulary: List of Covered Drugs
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DHEA) and Androstenedione Has Minimal Effect on Immune Function in Middle-Aged Men
Original Research Ingestion of a Dietary Supplement Containing Dehydroepiandrosterone (DHEA) and Androstenedione Has Minimal Effect on Immune Function in Middle-Aged Men Marian L. Kohut, PhD, James R. Thompson, MS, Jeff Campbell, BA, Greg A. Brown, MS, Matthew D. Vukovich, PhD, Dave A. Jackson, MS, Doug S. King, PhD Department of Health and Human Performance, Iowa State University, Ames, Iowa Key words: aging, cytokines, lymphocyte, hormones, androstenedione, DHEA Objective: This study investigated the effects of four weeks of intake of a supplement containing dehydro- epiandrosterone (DHEA), androstenedione and herbal extracts on immune function in middle-aged men. Design: Subjects consumed either an oral placebo or an oral supplement for four weeks. The supplement contained a total daily dose of 150 mg DHEA, 300 mg androstenedione, 750 mg Tribulus terrestris, 625 mg chrysin, 300 mg indole-3-carbinol and 540 mg saw palmetto. Measurements: Peripheral blood mononuclear cells were used to assess phytohemagglutinin(PHA)-induced lymphocyte proliferation and cytokine production. The cytokines measured were interleukin (IL)-2, IL-4, IL-10, IL-1␤, and interferon (IFN)-␥. Serum free testosterone, androstenedione, estradiol, dihydrotestosterone (DHT) were also measured. Results: The supplement significantly increased serum levels of androstenedione, free testosterone, estradiol and DHT during week 1 to week 4. Supplement intake did not affect LPS or ConA proliferation and had minimal effect on PHA-induced proliferation. LPS-induced production of IL-1beta, and PHA-induced IL-2, IL-4, IL-10, or IFN-gamma production was not altered by the supplement. The addition of the same supplement, DHEA or androstenedione alone to lymphocyte cultures in vitro did not alter lymphocyte proliferation, IL-2, IL-10, or IFN-␥, but did increase IL-4.
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Antidotal Or Protective Effects of Honey and Chrysin, Its Major Polyphenols
Acta Biomed 2019; Vol. 90, N. 4: 533-550 DOI: 10.23750/abm.v90i4.7534 © Mattioli 1885 Debate Antidotal or protective effects of honey and chrysin, its major polyphenols, against natural and chemical toxicities Saeed Samarghandian1, Mohsen Azimi-Nezhad1, Ali Mohammad Pourbagher Shahri2, 3 Tahereh Farkhondeh 1Department of Basic Medical Sciences, Neyshabur University of Medical Sciences, Neyshabur, Iran; 2Cardiovascular Diseases Research Center, Birjand University of Medical Sciences, Birjand, Iran; 3Faculty of Medicine, Birjand University of Medical Sciences, Birjand, Iran Summary. Objective: Honey and its polyphenolic compounds are of main natural antioxidants that have been used in traditional medicine. The aim of this review was to identify the protective effects of honey and chrysin (a polyphenol available in honey) against the chemical and natural toxic agents. Method: The scientific data- bases such as MEDLINE, PubMed, Scopus, Web of Science and Google Scholar were searched to identify studies on the antidotal effects of honey and chrysin against toxic agents. Results: This study found that honey had protective activity against toxic agents-induced organ damages by modulating oxidative stress, inflam- mation, and apoptosis pathways. However, clinical trial studies are needed to confirm the efficacy of honey and chrysin as antidote agents in human intoxication. Conclusion: Honey and chrysin may be effective against toxic agents. (www.actabiomedica.it) Key words: honey, chrysin, natural toxic agent, chemical toxic agent 1. Introduction the two types of sugar: glucose and fructose. Refined fructose, which is found in sweeteners, is metabolized Nowadays, antioxidants are used for reducing risk by the liver and has been associated with: obesity. Al- of various diseases such as cancer, cardiovascular, neu- though, Sugar is sugar, however, honey is (mostly) sug- rodegenerative, renal failure, gastrointestinal, and res- ar.
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Oreochromis Niloticus)
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Natural Substitutes for Aromatase Inhibitors by Dr
Natural Substitutes for Aromatase Inhibitors by Dr. Sam Schikowitz ND, LAc Natural, Integrative, and Holistic Health Solutions Combining Eastern and Western Healing Traditions www.WholeFamilyMedicine.com [email protected] (845) 594-6822 Sam Schikowitz ND LAc, [email protected], Naturopathic Medicine • Blends modern medical sciences with centuries-old natural, approaches. • Concentrates on the whole-patient wellness • Attempts to find the underlying cause of the patient's condition rather than focusing on symptomatic treatment. • Work as a team with patients to empower them to keep themselves healthy Sam Schikowitz ND LAc, [email protected], 845-594-6822 Naturopathic Medical Training • 4 years pre-medical bachelors o General, Organic, and Biochemistry o Zoology, Botany, Cell Biology o Statistics, Psychology, Physics, etc • 4 to 5 year medical training • 2 to 3 year supervised clinical internship o Over 600 patient visits • 1 or 2 year residencies Sam Schikowitz ND LAc, [email protected], 845-594-6822 Naturopathic Allopathic Medical School Medical School • Bachelor’s Degree • Outpatient • Pre-med Coursework • Hospital Rotations Rotations • Biomedical Sciences • Surgical Rotations • Diet Therapy • Pre-Clinical Medicine • Nutrient • Pharmacology Therapy • Minor Surgery • Pediatrics • Manipulative • Geriatrics Therapy • Gynecology • Counseling • Cardiology • Botanical • Endocrinology Medicine • Immunology • Homeopathy • Clinical Rotations Sam Schikowitz ND LAc, [email protected],
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The Role of Chrysin Against Harmful Effects of Formaldehyde Exposure on the Morphology of Rat Fetus Liver and Kidney Development
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Inhibitory Effect of Sauchinone on UDP-Glucuronosyltransferase (UGT) 2B7 Activity
molecules Article Inhibitory Effect of Sauchinone on UDP-Glucuronosyltransferase (UGT) 2B7 Activity Byoung Hoon You, Eun Chae Gong and Young Hee Choi * College of Pharmacy and Intergrated Research Institute for Drug Development, Dongguk University-Seoul, 32 Dongguk-lo, Ilsandong-gu, Goyang, Gyonggi-do 10326, Korea; [email protected] (B.H.Y.); [email protected] (E.C.G.) * Correspondence: [email protected]; Tel.: +82-31-961-5212 Received: 4 January 2018; Accepted: 7 February 2018; Published: 9 February 2018 Abstract: Herb–drug interaction (HDI) limits clinical application of herbs and drugs, and inhibition of herbs towards uridine diphosphate (UDP)-glucuronosyltransferases (UGTs) has gained attention as one of the important reasons to cause HDIs. Sauchinone, an active lignan isolated from aerial parts of Saururus chinensis (Saururacease), possesses anti-oxidant, anti-inﬂammatory, and anti-viral activities. In pharmacokinetics of sauchinone, sauchinone is highly distributed to the liver, forming extensive metabolites of sauchinone via UGTs in the liver. Thus, we investigated whether sauchinone inhibited UGTs to explore potential of sauchinone–drug interactions. In human liver microsomes (HLMs), sauchinone inhibited activities of UGT1A1, 1A3, 1A6, and 2B7 with IC50 values of 8.83, 43.9, 0.758, and 0.279 µM, respectively. Sauchinone also noncompetitively inhibited UGT1A6 and 2B7 with Ki values of 1.08 and 0.524 µM, respectively. In in vivo interaction study using mice, sauchinone inhibited UGT2B7-mediated zidovudine metabolism, resulting in increased systemic exposure of zidovudine when sauchinone and zidovudine were co-administered together. Our results indicated that there is potential HDI between sauchinone and drugs undergoing UGT2B7-mediated metabolism, possibly contributing to the safe use of sauchinone and drug combinations.
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Centene Employee
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