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Ahmed S Abdel-Razek, Abdelaaty Hamed, Marcel Frese, Norbert Sewald, Mohamed Shaaban
Penicisteroid C , a new polyoxygenated steroid was isolated from co-cultivation of Streptomyces piomogenus AS63D and Aspergillus niger using solid-state fermentation on rice medium. Additional diverse eleven known metabolites were identified: Fumigaclavine C, fumiquinazoline C, physcion, methylsulochrin, methyllinoleate, glycerol linoleate, cerebroside A, thymine, adenine, thymidine and adenosine. The structure of penicisteroid C was determined by HRESIMS, 1D and 2D NMR data. The antimicrobial and in vitro cytotoxic activities of the microbial extract and penicisteroid C were reported as well...
June 11, 2018: Steroids
Vladimir A D'yakonov, Regina A Tuktarova, Lilya U Dzhemileva, Svetlana R Ishmukhametova, Milyausha M Yunusbaeva, Usein M Dzhemilev
Synthetic analogues of natural 5Z,9Z-dienoic acids - hybrid molecules based on the oximes of cholesterol, pregnenolone, and androsterone with 1,14-tetradeca-5Z,9Z-dienedicarboxylic acid - were synthesized for the first time and studied for antitumor activity in vitro. The acid was prepared using catalytic cyclomagnesiation of O-containing 1,2-dienes with Grignard reagent in the presence of Cp2 TiCl2 as the key step. Using flow cytometry, it was shown for the first time that the new molecules are efficient apoptosis inducers in the HeLa, Hek293, U937, Jurkat, and K562...
June 9, 2018: Steroids
Vladimir A D'yakonov, Regina A Tuktarova, Lilya U Dzhemileva, Svetlana R Ishmukhametova, Milyausha M Yunusbaeva, Usein M Dzhemilev
Hybrid molecules based on a number of steroids (cholesterol, pregnenolone, androsterone) and 1,14-tetradeca-5Z,9Z-dienedicarboxylic acid linked via mono- and diethylene glycol spacers were synthesized for the first time and studied for antitumor activity in vitro. The acid was prepared using catalytic cyclomagnesiation of oxygenated 1,2-dienes with Grignard reagent in the presence of Cp2 TiCl2 as the key synthetic step. Using flow cytometry, the new molecules were shown for the first time to be efficient apoptosis inducers in the HeLa, Hek293, U937, Jurkat, and K562 cell cultures and to have dose-dependent effect on the S and G2 phases of the cell cycle...
June 8, 2018: Steroids
Therina du Toit, Martijn J J Finken, Henrike M Hamer, Annemieke C Heijboer, Amanda C Swart
The purpose of this study was to identify the C11-oxy C19 and C11-oxy C21 steroids in male and female neonate plasma. At birth, the most abundant C11-oxy steroids detected in neonatal plasma were 11β-hydroxyandrostenedione, ∼13 nM, and 11-ketoprogesterone, ∼23 nM. C11-oxy C19 steroids were higher than C19 steroids in neonatal plasma, 22.2 nM vs 5.4 nM. The inclusion of C11-oxy C19 and C21 steroid reference ranges in routine steroid analyses will assist the characterization of disorders associated with impaired steroidogenic enzyme expression and the identification of potential biomarkers...
June 5, 2018: Steroids
Rahel M Büttler, Esra Bagci, Henk S Brand, Martin den Heijer, Marinus A Blankenstein, Annemieke C Heijboer
BACKGROUND: Recently, measurements of steroids like testosterone, androstenedione, cortisol and cortisone in saliva are more and more applied in diagnostics and scientific studies. This is mainly due to the simple and non-invasive collection of saliva. We aimed to evaluate the optimal way to collect saliva for steroid hormone measurement. METHODS: We investigated in twenty volunteers whether there is a difference between steroid hormone concentrations in unstimulated and stimulated saliva collected while chewing, using cotton and synthetic Salivettes®, citric acid or chewing gum...
June 1, 2018: Steroids
Song Wang, Peng Xia, Nicholas A Cacalano, Haikun Xu, Dejun Li
Androgen insensitivity syndrome (AIS) is the most common cause of 46,XY disorders of sex development (46,XY DSD). This syndrome is an X-linked recessive genetic disease characterized by resistance to the actions of androgens in an individual with a male karyotype and it is caused by mutations in the androgen receptor (AR) gene. We evaluated two siblings with primary amenorrhea, normal secondary sex characteristics, absence of uterus and ovaries, intra-abdominal testis, and elevated testosterone levels. Sequence analysis of the AR gene revealed a splice acceptor site mutation in intron 2 (c...
May 30, 2018: Steroids
B Sreelatha, G ShyamPrasad, V Koteshwar Rao, S Girisham
Mesophilic fungi are well recognized as models of mammalian drug metabolism. Thermophilic fungi remained unexplored despite having a unique mechanism of growing at higher temperatures and performing wide diverse reactions. The present investigation is directed to isolate a promising thermophilic fungal strain capable of biotransformation using spironolactone as a model drug. Two-stage fermentation protocol was followed for the process. The transformation of spironolactone was identified by HPLC and structure elucidation of the metabolites was done with the help of LC-MS/MS analysis and previous reports...
May 24, 2018: Steroids
Heidi Laderoute, Christine Bone, E James Squires
Porcine sulfotransferase 2A1 (pSULT2A1) is a key enzyme involved in the testicular and hepatic sulfoconjugation of steroids such as dehydroepiandrosterone (DHEA) and potentially androstenone. This latter steroid is a major cause of boar taint, which is an unpleasant off-odour and off-flavour in pork from male pigs. Sulfotransferase 2B1 (pSULT2B1) may also be important, although no direct evidence exists for its involvement in sulfoconjugation of steroids. The purpose of this study was to investigate the sulfoconjugation activity of human and porcine sulfotransferases towards DHEA and androstenone...
May 22, 2018: Steroids
Muafia Jabeen, Muhammad Iqbal Choudhry, Ghulam Abbas Miana, Khondaker Miraz Rahman, Umer Rashid, Hidayat-Ullah Khan, Arshia, Abdul Sadiq
Steroidal hormones progesterone and testosterone play a vital role in breast and prostate cancers. In this research, we have synthesized and characterized a total of thirty-one (31) new nitrogenous derivatives of progesterone and testosterone. The synthesized derivatives (1-31) were screened for their anti-cancer potential against MCF-7 and PC-3 cell lines of breast using MTT assay. The compounds 1-31exhibited significant inhibitory potentials against MCF-7 and PC-3 cell lines. In MCF-7 assay, compound 17 displayed IC50 value of 04 ±0...
May 14, 2018: Steroids
Nora Al-Kazaale, Phuong T Tran, Farhad Haidari, Eirik Johansson Solum, Sandra Liekens, Peter Vervaeke, Ingebrigt Sylte, Jing-Jy Cheng, Anders Vik, Trond Vidar Hansen
The endogenous steroid 2-methoxyestradiol (1) has attracted a great interest as a lead compound towards the development of new anti-cancer drugs. Herein, the synthesis, molecular modeling, anti-proliferative and anti-angiogenic effects of ten 2-ethyl and four 2-methoxy analogs of estradiol are reported. The ethyl group was introduced to the steroid A-ring using a novel Friedel-Crafts alkylation protocol. Several analogs displayed potent anti-proliferative activity with IC50 -values in the submicromolar range towards the CEM human leukemia cancer cell line...
May 14, 2018: Steroids
Song-Wei Li, Wen-Ting Chen, Li-Gong Yao, Yue-Wei Guo
Two new steroids, ximaosteroid E (1) and ximaosteroid F (2), along with two known related compounds (3 and 4), were isolated from the Chinese soft coral Sinularia sp. Notably, 1 possesses an uncommon dihydrofuran group. Their structures were established from extensive spectroscopic analyses and comparisons of their spectral data with those reported in the literature. The absolute configuration of 2 was determined by applying the modified Mosher's method. In bioassay, compounds 1, 2, and 4 showed significant cytotoxicity against the HL-60 tumor cell line with IC50 values of 1...
May 14, 2018: Steroids
Michaël Levy, Ala-Eddine Deghmane, Myriam Aouiti-Trabelsi, Stéphane Dauger, Albert Faye, Patricia Mariani-Kurkdjian, Muhamed-Kheir Taha
Invasive meningococcal disease (IMD) is usually associated with intense inflammatory response that is correlated with severe infection. Corticosteroids may regulate this inflammatory response through an early but transient induction of IL-10 that is suggested to improve the outcome of IMD. We explored the mechanism of action of corticosteroids as an adjuvant treatment to antibiotics. Transgenic mice expressing the human transferrin were infected by a hyperinvasive meningococcal strain and transcriptomic analysis were then performed in the blood for all conditions of infection and treatment...
May 10, 2018: Steroids
Yu Chen, Yi Dong, Yuanlong Chi, Qiang He, Hui Wu, Yao Ren
A novel microbial procedure was proposed for diosgenin production from Dioscorea zingiberensis C.H. Wright (DZW) tubers via employing Aspergillus awamori for the first time. The optimal conditions of fermenter cultivation were established as inoculation dosage of 8%, fermentation temperature of 30 °C, cultivation time of 8 days, initial pH of 7.0 and a stirring rate of 180 rpm when the converted diosgenin content reached a peak value of 74.26±3.23 mg/g substrate. The product was purified by silica gel column and then confirmed as diosgenin (purity: 96...
May 8, 2018: Steroids
Seth Guller
No abstract text is available yet for this article.
May 8, 2018: Steroids
Ching-Chung Tsai, Shu-Leei Tey, Li-Ching Chang, Yu-Tsun Su, Kai-Jen Lin, Shih-Che Huang
Most pregnant women have symptoms of gastroesophageal reflux disease (GERD) during pregnancy. Postmenopausal hormone replacement therapy is associated with GERD. The effects of estradiol on lower esophageal sphincter (LES) motility and GERD are not clearly known. The purpose of this study is to investigate the effects of estradiol on the motility of the porcine LES. Relaxations of clasp and sling strips of porcine LES caused by estradiol were measured using isometric transducers. We investigated the mechanism of estradiol-induced relaxation of the porcine LES using tetraethylammonium, apamine, iberiotoxin, glibenclamide, KT5720, KT5823, NG-nitro-l-arginine, tetrodotoxin, and ω-conotoxin GVIA...
May 5, 2018: Steroids
Panida Loutchanwoot, Tina Vortherms
Effects of puerarin on the hypothalamic gonadotropin-releasing hormone (GnRH) pulse generator function is investigated, for the first time, in ovariectomized rats at the level of mRNA expression of estrogen-responsive genes, e.g., estrogen receptor (ER), GnRH and its receptor (GnRHR). Rats were treated orally for 90 days either with a soy-free diet containing two different doses of puerarin (low dose of 600 mg/kg and high dose of 3000 mg/kg) or estradiol benzoate (E2B) at either low dose (4.3 mg/kg) or high dose (17...
May 4, 2018: Steroids
Vladimir A Zolottsev, Yaroslav V Tkachev, Alexandra S Latysheva, Vladimir A Kostin, Roman A Novikov, Vladimir P Timofeev, Galina E Morozevich, Alexey V Kuzikov, Victoria V Shumyantseva, Alexander Y Misharin
No abstract text is available yet for this article.
August 2018: Steroids
Christina Wang, Steve Shiraishi, Andrew Leung, Sima Baravarian, Laura Hull, Victor Goh, Paul W N Lee, Ronald S Swerdloff
No abstract text is available yet for this article.
July 2018: Steroids
Bentley J Hanish, Jennifer F Hackney Price, Ichiro Kaneko, Ning Ma, Arjan van der Vaart, Carl E Wagner, Peter W Jurutka, Pamela A Marshall
Rexinoids are powerful ligands that bind to retinoid-X-receptors (RXRs) and show great promise as therapeutics for a wide range of diseases, including cancer. However, only one rexinoid, bexarotene (Targretin TM) has been successfully transitioned from the bench to the clinic and used to treat cutaneous T-cell lymphoma (CTCL). Our goal is to develop novel potent rexinoids with a less untoward side effect profile than bexarotene. To this end, we have synthesized a wide array of rexinoids with EC50 values and biological activity similar to bexarotene...
July 2018: Steroids
Tresha E Dobson, Anderson R Maxwell, Adesh Ramsubhag
Six cholic acid derivatives (1-6) were isolated from broth cultures of Bacillus amyloliquefaciens UWI-W23, an isolate from the Trinidad Pitch Lake. The compounds were extracted via solvent extraction and/or XAD resin adsorption and purified using silica gel column chromatography. Their structures were elucidated using 1D, 2D NMR and ESI-MS spectrometry and FT-IR spectrophotometry. One of the compounds, taurodeoxycholate (2) is for the first time being reported from a bacterial source while deoxycholate (4) is for the first time being reported from a Gram-positive bacterium...
July 2018: Steroids
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