ISOLATION AND IDENTIFICATION OF 6β, 17α, 21-TRIHYDROXY-6α-METHYL-Δ4-PREGNENE-3,20-DIONE (21-ACETATE) FROM THE URINE OF HUMAN SUBJECTS TREATED WITH 6α-METHYL-17α-ACETOXYPROGESTERONE

1962 ◽  
Vol 24 (4) ◽  
pp. 445-452 ◽  
Author(s):  
E. CASTEGNARO ◽  
G. SALA
Keyword(s):  
Infrared Spectra ◽  
Human Subjects ◽  
Metabolic Process ◽  
Isolation And Identification ◽  
Men And Women ◽  
Adrenal Tissue ◽  
Degradation Reactions ◽  
Normal Men

SUMMARY A new tetrazolium reducing compound, present as a conjugate which could be hydrolysed by β-glucuronidase, has been isolated from the urine of normal men and women and oophorectomized-adrenalectomized women, all of whom had received 100 mg./day 6α-methyl-17α-acetoxyprogesterone (MAP) either subcutaneously or orally. Detailed studies of its characteristics, including degradation reactions, ultraviolet and infrared spectra, combined with studies on known steroids, suggest that the new compound is 6β,17α,21-trihydroxy-6α-methyl-Δ4-pregnene-3,20-dione (21-acetate). It is suggested that MAP in vivo undergoes hydroxylation at C-21 in the absence of ovarian and adrenal tissue which up to the present have been considered essential for this metabolic process.

FORMATION OF EPITESTOSTERONE BY HUMAN BLOOD AND ADRENAL TISSUE

1967 ◽  
Vol 54 (2) ◽  
pp. 208-214 ◽  
Author(s):  
Jorge Blaquier ◽  
Ralph I. Dorfman ◽  
Enrico Forchielli
Keyword(s):  
Venous Blood ◽  
Endocrine Gland ◽  
Men And Women ◽  
Peripheral Venous Blood ◽  
Adrenal Tissue ◽  
Idiopathic Hirsutism ◽  
Normal Human ◽  
Normal Men ◽  
Peripheral Production

ABSTRACT Whole peripheral venous blood from normal men and women, and from females with idiopathic hirsutism was incubated in vitro with labelled testosterone, androstenedione and dehydroepiandrosterone. Epitestosterone was formed consistently from added testosterone, in some cases from androstenedione but not from dehydroepiandrosterone. The rate of formation of epitestosterone from testosterone by blood of normal men and women is similar, whereas the rate of formation in blood from female idiopathic hirsutes was several fold greater. In a similar manner, normal human adrenal tissue also formed epitestosterone from added testosterone but not from androstenedione nor dehydroepiandrosterone. These results suggest that the origin of urinary epitestosterone can be the resultant of both peripheral production and endocrine gland secretion.

INTERCONVERSION OF PROGESTERONE AND 20α-DIHYDROPROGESTERONE AND OF ANDROSTENEDIONE AND TESTOSTERONE IN VITRO BY BLOOD AND ERYTHROCYTES

1968 ◽  
Vol 58 (3) ◽  
pp. 419-444 ◽  
Author(s):  
H. J. van der Molen ◽  
D. Groen
Keyword(s):  
Dehydrogenase Activity ◽  
Venous Blood ◽  
Hydroxysteroid Dehydrogenase ◽  
Linear Increase ◽  
Equivalent Amount ◽  
Men And Women ◽  
Peripheral Venous Blood ◽  
Normal Men

ABSTRACT Peripheral venous blood and erythrocytes from normal men and women, as well as from dogs, rabbits and sheep were incubated with 14C-labeled progesterone*, 20α-dihydroprogesterone, androstenedione and testosterone. The presence in blood and erythrocytes of a 20α-hydroxysteroid dehydrogenase activity, catalyzing the interconversion progesterone ⇄ 20α-dihydroprogesterone, and of a 17β-hydroxysteroid dehydrogenase activity, catalyzing the interconversion androstenedione ⇆ testosterone was observed. Incubation with washed erythrocytes in the presence of glucose and several co-factors favoured the formation of the reduced compounds: 20α-dihydroprogesterone or testosterone. Incubations with washed erythrocytes, without addition of glucose and co-factors, favoured the formation of the oxidized compounds: progesterone and androstenedione. Incubation of steroids with whole blood, resulted in metabolism of progesterone to 20α-dihydroprogesterone and of androstenedione to testosterone. The formation of the product during incubation in vitro increased linearly with time of incubation (15—180 min). Incubations of 20 ml blood or the equivalent amount of erythrocytes with substrate amounts of steroids varying from 0.5 to 3000 μg, gave a linear increase in the amount of product formed. The possible significance of these observations in vitro for steroid metabolism in vivo is discussed.

ÉTUDES IN VIVO SUR LE MÉTABOLISME DES ANDROGÉNES APRES ADMINISTRATION DE STÉROÏDES INHIBITEURS DE L'OVULATION

1965 ◽  
Vol 50 (1) ◽  
pp. 131-144 ◽  
Author(s):  
P. Mauvais-Jarvis ◽  
M. F. Jayle ◽  
J. Decourt ◽  
J. Louchart ◽  
J. Truffert
Keyword(s):  
Luteinizing Hormone ◽  
Urinary Excretion ◽  
Normal Subjects ◽  
Hormone Activity ◽  
Testosterone Production ◽  
Normal Men ◽  
Ethinyl Oestradiol

ABSTRACT Normal subjects and hirsute women with micropolycystic ovaries were treated with ethinyl-oestrenol + 3-methoxy-ethinyl-oestradiol (Lyndiol®), in view of studying the action of this compound on the production of androgens and on the urinary excretion of their metabolites. In normal men, the production of testosterone and the excretion of androsterone and aetiocholanolone are suppressed, whereas the excretion of other 17-ketosteroids and the production of dehydroepiandrosterone sulphate are unchanged. Moreover, the luteinizing hormone activity (LH) in plasma is depressed. It seems that the preparation inhibits specifically the testicular androgen production, by suppressing the hypothalamo-hypophyseal control of LH. Testosterone production and urinary 17-ketosteroid excretion are modified in the same way in women with Stein-Leventhal's syndrome. Physiopathological and therapeutical implications which come from these results are discussed.

ATYPICAL ADRENAL HYPERFUNCTION: IN VIVO STUDIES AND INCUBATIONS OF ADRENAL TISSUE WITH 4-14C PROGESTERONE

1968 ◽  
Vol 58 (3_Suppl) ◽  
pp. S5-S34
Author(s):  
Joseph W. Goldzieher ◽  
Leonard R. Axelrod ◽  
Arthur S. Weissbein
Keyword(s):  
Urinary Excretion ◽  
Clinical Features ◽  
In Vivo Studies ◽  
Acth Stimulation ◽  
Adrenal Tissue ◽  
Adrenal Hyperfunction

ABSTRACT Six women with atypical forms of adrenal cortical hyperfunction were studied by means of urinary excretion of 17-ketosteroids and 17-hydroxycorticoids and their response to ACTH stimulation and corticosteroid suppression. Unusual responses were observed, particularly with respect to the independence of 17-KS and 17-OHCS excretion. The adrenals of 3 patients were anatomically normal whereas the others showed hyperplasia. Minced adrenal tissue was incubated with 4-14C progesterone and the metabolites isolated and definitively identified. The pattern of biosynthesized corticosteroids showed great variation, and in some instances clarified certain clinical features. The pattern of certain C19-metabolites could not be studied adequately because of the use of a Δ4 rather than a Δ5 substrate.

Pharmacological treatment with L-DOPA may reduce striatal dopamine transporter binding in in vivo imaging studies

2016 ◽  
Vol 55 (01) ◽  
pp. 21-28 ◽  
Author(s):  
C. Antke ◽  
H. Hautzel ◽  
H.-W. Mueller ◽  
S. Nikolaus
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Binding Sites ◽  
Human Subjects ◽  
Synaptic Cleft ◽  
Presynaptic Terminal ◽  
Imaging Studies ◽  
Psychiatric Conditions ◽  
Da Release

SummaryNumerous neurologic and psychiatric conditions are treated with pharmacological compounds, which lead to an increase of synaptic dopamine (DA) levels. One example is the DA precursor L-3,4-dihydroxyphenylalanine (L-DOPA), which is converted to DA in the presynaptic terminal. If the increase of DA concentrations in the synaptic cleft leads to competition with exogenous radioligands for presynaptic binding sites, this may have implications for DA transporter (DAT) imaging studies in patients under DAergic medication.This paper gives an overview on those findings, which, so far, have been obtained on DAT binding in human Parkinson’s disease after treatment with L-DOPA. Findings, moreover, are related to results obtained on rats, mice or non-human primates. Results indicate that DAT imaging may be reduced in the striata of healthy animals, in the unlesioned striata of animal models of unilateral Parkinson’s disease and in less severly impaired striata of Parkinsonian patients, if animal or human subjects are under acute or subchronic treatment with L-DOPA. If also striatal DAT binding is susceptible to alterations of synaptic DA levels, this may allow to quantify DA reuptake in analogy to DA release by assessing the competition between endogenous DA and the administered exogenous DAT radioligand.

Genetic Engineering of AAV Capsid Gene for Gene Therapy Application

2020 ◽  
Vol 20 (5) ◽  
pp. 321-332
Author(s):  
Yunbo Liu ◽  
Xu Zhang ◽  
Lin Yang
Keyword(s):  
Gene Therapy ◽  
Neutralizing Antibodies ◽  
Human Subjects ◽  
Genetic Diseases ◽  
Capsid Gene ◽  
Human Populations ◽  
Stable Gene ◽  
Efficient Gene ◽  
Gene Therapy Application

Adeno-associated virus (AAV) is a promising vector for in vivo gene therapy because of its excellent safety profile and ability to mediate stable gene expression in human subjects. However, there are still numerous challenges that need to be resolved before this gene delivery vehicle is used in clinical applications, such as the inability of AAV to effectively target specific tissues, preexisting neutralizing antibodies in human populations, and a limited AAV packaging capacity. Over the past two decades, much genetic modification work has been performed with the AAV capsid gene, resulting in a large number of variants with modified characteristics, rendering AAV a versatile vector for more efficient gene therapy applications for different genetic diseases.

scholarly journals Lightening Effect of Skin Lightening Cream Containing Piper betle L. Extract in Human Volunteers

Cosmetics ◽  
2021 ◽  
Vol 8 (2) ◽  
pp. 32
Author(s):  
Sharifah Shakirah Syed Omar ◽  
Hazrina Hadi ◽  
Nadzira Mohd Hanif ◽  
Hawa Mas Azmar Ahmad ◽  
Shiow-Fern Ng
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Human Subjects ◽  
Skin Barrier ◽  
Skin Tone ◽  
In Vivo Studies ◽  
Piper Betle ◽  
Melanin Content ◽  
Skin Lightening

Hyperpigmentation affects people globally with negative psychological impacts. Piper betle L. leaf (PBL) extract has many benefits including skin lightening which may reduce hyperpigmentation. The objective of this study was to develop an effective skin-lightening cream containing PBL with ideal characteristics. A formulation of base cream and PBL cream was prepared and characterized by centrifugation, particle size and zeta potential analysis, rheological profile studies and physical properties’ observation. In vivo studies on 30 human subjects tested the effects of base and PBL cream on skin-lightening, hydration, trans-epidermal water loss (TEWL) and elasticity through weekly tests 4 weeks in duration. Base and PBL creams had a non-Newtonian property with acceptable color, odor, texture, zeta potential, particle size and showed no phase separation. The in vivo study indicated a significant reduction in melanin content and an improvement in skin tone for PBL cream but not in base cream. TEWL and elasticity also showed significant reduction for both formulations, indicating a healthier skin barrier and supple skin with consistent use, although hydration fluctuated with no significant changes. The developed PBL cream showed significant results in the reduction in melanin content and improving skin tone, which shows the formulation can confer skin-lightening effect.

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