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Antiprogestins with a 4′ para imidazolylphenyl moiety were synthesized and their biochemical interactions with the progesterone and glucocorticoid receptor were investigated. Depending on the substitution pattern at the 17 position partial progesterone receptor (PR)-agonistic derivatives like compounds EC339 and EC336 or pure antagonists like compound EC317 were obtained. EC317 was investigated in...
Breast cancer is the second leading cause of cancer deaths in women in the United States. Diethylstilbestrol (DES) is a synthetic estrogen that has been shown to cause cancer in animals and humans, altering cell viability as well as inducing DNA damage. Diallyl sulfide (DAS) is a garlic organosulfide that has been shown to inhibit both the initiation and promotion phases of cancer in vivo and in vitro,...
Certified reference materials (CRMs) can be used as a valuable tool to validate the trueness of measurement methods and to establish metrological traceability of analytical results. Diosgenin has been selected as a candidate reference material. Characterization of the material relied on two different methods, mass balance method and Coulometric titration method (CT). The certified value of diosgenin...
Transformation of Finasteride (I) by cell suspension cultures of Ocimum sanctum L. was investigated. Fermentation of compound (I) with O. sanctum afforded three oxidized derivatives, 16β-hydroxyfinasteride (II), 11α-hydroxyfinasteride (III) and 15β-hydroxyfinasteride (IV). Among these metabolites, compound (II) was a new metabolite. Compound (I) and its derivatives were studied for their tyrosinase...
β-d-Glucopyranoside,(3β,12β,20E)-12,25-dihydroxydammar-20(22)-en-3-yl (pseudo-ginsenoside Rh2) and its 20Z-isomer were synthesized from ginsenoside Rh2 under a mild condition, via a simple three-step called acetylation, elimination–addition and saponification. In addition, their activities were evaluated by eight different human tumor cells, compared with ginsenoside Rh2 group. Results indicated that...
In order to utilize and protect the resources of Rhizoma Paridis rationally, we carried out a phytochemical investigation on the non-medicinal (aerial) parts of Paris verticillata that led to the isolation of fifteen steroidal saponins. Among them, three are new spirostanol saponins, named parisverticosides A–C (1–3), as well as one new cholestane glycoside, named parisverticoside D (4). Their structures...
Increased exposure to estrogens and estrogen metabolites is linked with increased rates of breast, ovarian and other human cancers. Metabolism of estrogen can led to formation of electrophilic o-quinones capable of binding to DNA. In order to gain insight into the mechanism of estrogen-induced DNA damage, estrone and catechol estrogens derived from estrone, have been regioselectively labeled with...
The microbial transformations of testosterone and testosterone heptanoate by four fungi: Absidia griseolla var. igachii PTCC 5260, Acremonium chrysogenu PTCC 5271, Fusarium fujikuroi PTCC 5144, and Fusarium solani complex PTCC 5285 were investigated for the first time. Incubation of testosterone heptanoate with F. fujikuroi and F. solani yielded three metabolites, which were isolated and characterized...
Cortisol is involved in many physiological processes, including immunosuppressive and anti-inflammatory actions, and therefore cortisol and its synthetic analogs are widely used to treat a large number of diseases. In glucocorticoid treatment, a large variability of clinical responses is observed. This variability may, in part, be ascribed to genetic variation in the glucocorticoid receptor (GR) gene...
Steroid sulfates are a major class of steroid metabolite that are of growing importance in fields such as anti-doping analysis, the detection of residues in agricultural produce or medicine. Despite this, many steroid sulfate reference materials may have limited or no availability hampering the development of analytical methods. We report simple protocols for the rapid synthesis and purification of...
A new 9,11-secosteroid, 25(26)-dehydrosarcomilasterol (1), two new polyhydroxylated steroids, 7α-hydroxy-crassarosterol A (2) and 11-acetoxy-7α-hydroxy-crassarosterol A (3), together with three known related ones (4–6), were isolated from the South China Sea soft corals Sarcophyton trocheliophorum and Sinularia flexibilis, respectively. The structures of the new steroids were elucidated on the basis...
Taking pregnenolone as the starting material, two series of pyrazolinyl and pyrazolyl pregnenolones were synthesized through different routes. The synthesis of the analogs of both series is multistep and proceeds in good overall yields. While the key step in the synthesis of pyrazolinyl pregnenolones is the heterocyclization of benzylidine derivatives (3) in presence of hydrazine hydrate, it is the...
In teleosts, the levels of steroids during critical period of sex differentiation are critical for gonadogenesis. Hence, steroidogenesis and expression of steroidogenic enzyme genes are very critical for gonadal development and function. In this regard, 17β-HSDs are important as they are involved in both 17β-estradiol (E 2 ) and testosterone (T) biosynthesis. Full length cDNAs of 17β-HSD 1...
Although accumulating evidence indicates high expression of CYP17A1(P45017A1) allows castration resistant prostate cancer (CRPC) to maintain high intratumoral androgen levels, the potential P45017A1 activity has not been characterized yet. The aim of this study was to examine the potential CYP17A1 activity including 17α-hydroxylase and 17,20-lyase activities in human CRPC and the effect of a CYP17A...
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