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Search results for: androstane

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#34509617   2021/09/09 To Up

Heterocyclic androstane and estrane D-ring modified steroids: microwave-assisted synthesis, steroid-converting enzyme inhibition, apoptosis induction, and effects on genes encoding estrogen inactivating enzymes.

D-ring-fused and D-homo lactone compounds in estratriene and androstane series were synthesized using microwave-assisted reaction conditions. Microwave-irradiated synthesis methods were convenient and effective, and provided high yields with short reaction times. Their inhibition of C-lyase and 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) activities were studied in in vitro enzyme assays. D-ring-fused triazolyl estrone analog 24 showed potent inhibition of NADH-complexed 17β-HSD1, with a binding affinity similar to that of the substrate estrone; its inhibition against NADPH-complexed 17β-HSD1 was markedly weaker. Compound 24 also significantly and selectively reduced proliferation of cancer cell lines of gynecological origin. This estrane triazole changed the cell cycle and induced apoptosis of HeLa, SiHa, and MDA-MB-231 cancer cells, measured by both increased subG1 fraction of cells and activation of caspase-independent signaling pathways. A third mode of anti-estrogenic action of 24 saw increased mRNA expression of the SULT1E1 gene in HeLa cells; in contrast, its 3-benzyloxy analog 23 increased mRNA expression of the HSD17B2 gene, thus showing pronounced pro-drug anti-estrogenic activity. Estradiol-derived D-ring triazole compound 24 thus acts at the enzyme, gene expression and cellular levels to decrease the production of active estrogen hormones, demonstrating its pharmacological potential.
Ágnes Erika Kulmány, Bianka Edina Herman, István Zupkó, Masa Sinreih, Tea Lanišnik Rižner, Marina Savić, Aleksandar Oklješa, Andrea Nikolić, Viktória Nagy, Imre Ocsovszki, Mihály Szécsi, Suzana Jovanović-Šanta

2541 related Products with: Heterocyclic androstane and estrane D-ring modified steroids: microwave-assisted synthesis, steroid-converting enzyme inhibition, apoptosis induction, and effects on genes encoding estrogen inactivating enzymes.

1000 tests96 wells (1 kit)25 mg1000 tests1000 tests1000 tests200 10 mg100.00 ul

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#34502180   2021/08/27 To Up

Activation of the Constitutive Androstane Receptor Inhibits Leukocyte Adhesiveness to Dysfunctional Endothelium.

Leukocyte cell recruitment into the vascular subendothelium constitutes an early event in the atherogenic process. As the effect of the constitutive androstane receptor (CAR) on leukocyte recruitment and endothelial dysfunction is poorly understood, this study investigated whether the role of CAR activation can affect this response and the underlying mechanisms involved. Under physiological flow conditions, TNFα-induced endothelial adhesion of human leukocyte cells was concentration-dependently inhibited by preincubation of human umbilical arterial endothelial cells with the selective human CAR ligand CITCO. CAR agonism also prevented TNFα induced VCAM-1 expression, as well as MCP-1/CCL-2 and RANTES/CCL-5 release in endothelial cells. Suppression of CAR expression with a small interfering RNA abrogated the inhibitory effects of CITCO on these responses. Furthermore, CITCO increased interaction of CAR with Retinoid X Receptor (RXR) and reduced TNFα-induced p38-MAPK/NF-κB activation. In vivo, using intravital microscopy in the mouse cremasteric microcirculation treatment with the selective mouse CAR ligand TCPOBOP inhibited TNFα-induced leukocyte rolling flux, adhesion, and emigration and decreased VCAM-1 in endothelium. These results reveal that CAR agonists can inhibit the initial inflammatory response that precedes the atherogenic process by targeting different steps in the leukocyte recruitment cascade. Therefore, CAR agonists may constitute a new therapeutic tool in controlling cardiovascular disease-associated inflammatory processes.
Mireia López-Riera, Rebeca Ortega, Luisa Hueso, María Carmen Montesinos, Mari Carmen Gomez-Cabrera, María Jesús Sanz, José T Real, Laura Piqueras

2373 related Products with: Activation of the Constitutive Androstane Receptor Inhibits Leukocyte Adhesiveness to Dysfunctional Endothelium.

96T100 96T100 100.00 ug100 μg

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#34495066   // To Up

Serum asprosin level in different subtypes of polycystic ovary syndrome: a cross-sectional study.

Polycystic ovary syndrome can be divided into different subtypes, including insulin resistance and hyperandrogenism. The aim of this study was to investigate the relationship between serum asprosin levels and polycystic ovary syndrome subtypes.
Yonghui Jiang, Yue Liu, Zhiheng Yu, Ping Yang, Shigang Zhao

2549 related Products with: Serum asprosin level in different subtypes of polycystic ovary syndrome: a cross-sectional study.



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#34486432   // To Up

Effects of a blood flow restriction exercise under different pressures on testosterone, growth hormone, and insulin-like growth factor levels.

To investigate the changes in serum growth hormone (GH), testosterone, and insulin-like growth factor 1 (IGF-1) during low-intensity resistance exercise under different cuff pressures.
Li Yinghao, Yang Jing, Wang Yongqi, Zhou Jianming, Gao Zeng, Tang Yiting, Li Shuoqi

1027 related Products with: Effects of a blood flow restriction exercise under different pressures on testosterone, growth hormone, and insulin-like growth factor levels.

50 ug5 x 50 ug100.00 ug2 Pieces/Box0.1ml (1mg/ml)100.00 ug100.00 ug20 ug100.00 ug100.00 ug100.00 ug0.2 mg

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#34482297   2021/08/20 To Up

Two crystallographic forms and the absolute structure of 5α,14α-androstane.

5α,14α-Androstane (CH) crystallizes in two different polymorphic forms in the same vapor diffusion experiment. The major form (Form I) crystallizes as thin plates in the space group P2, with Z = 4. These plates are twinned along a long c axis of length 43 Å and readily suffer from radiation damage when diffracted. The minor form (Form II) crystallizes as fine needles in the space group P222, Z = 3. In the minor form, 5α,14α-androstane cocrystallizes with 5α,14α-androstan-17-one, an oxidation product of 5α,14α-androstane. The presence of 5α,14α-androstan-17-one in the minor form of the crystals was confirmed by HR-MS. Form II can be crystallized as a pure form without the ketone impurity using a different solvent system. High level density functional theory (DFT) lattice free energy calculations were performed and show that both pure forms are isoergic within the estimated error of the calculations.
Christopher M Crittenden, Antonio G DiPasquale

1349 related Products with: Two crystallographic forms and the absolute structure of 5α,14α-androstane.

25 mg1000 tests1000 tests96 wells (1 kit)1000 tests1000 tests 1 kit(s) 25 mg10

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#34478830   2021/08/31 To Up

Biological evaluation of antiproliferative and anti-invasive properties of an androstadiene derivative on human cervical cancer cell lines.

Gynaecological cancers are leading cause of death: breast cancer is the most frequently diagnosed type of malignancies, and cervical neoplasms rank fourth for both incidence and mortality among women worldwide. In one of our previous studies, favourable antiproliferative and antimetastatic properties of a newly synthesized androstane derivative, 17APAD have been demonstrated on breast cancer cell lines with different expression patterns of hormone receptors. The aim of the current study was to investigate the antitumoral potential of this molecule in cervical cancer cell lines, including SiHa cells positive for human papilloma virus (HPV) type 16 and HPV-negative C33A cells. 17APAD exerted pronounced growth-inhibition (with IC values ranging from 0.76 to 1.72 μM with considerable cancer selectivity), while cisplatin used as a reference agent yielded higher IC values (ranging from 3.69 to 12.43) and less selectivity, as evidenced by MTT assay. The proapoptotic effect and morphological changes induced by 17APAD were detected by Hoechst 33258-propidium iodide or Annexin V-Alexa488-propidium iodide fluorescent double staining methods, supplemented with a caspase-3 activity assay to identify the mechanism behind the programmed cell death induced by 17APAD. Additionally, significant and concentration-dependent elevation of the ratio of cells in the G2/M phase, on the expense of G0/G1 phase, was observed after 48 h of exposure to 17APAD. Besides its potent antiproliferative properties against both cervical cancer cell lines, 17APAD elicited a remarkable inhibition of cell migration and invasion as detected in wound-healing and Boyden chamber assays, respectively. The mechanisms of action underlying the effects of 17APAD on cell proliferation and motility were independent of androgenic activity, as demonstrated by the Yeast Androgen Screen method. Our results provide new evidence for the proapoptotic and anti-invasive properties of 17APAD, suggesting that it is worth of further research, as a promising prototype for designing novel anticancer agents.
Ágnes E Kulmány, Éva Frank, Dóra Papp, András Szekeres, Gábor J Szebeni, István Zupkó

2458 related Products with: Biological evaluation of antiproliferative and anti-invasive properties of an androstadiene derivative on human cervical cancer cell lines.

20 1000 100 μg1 ml200 25 1 mg1 mg200 200

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#34477163   // To Up

Anaphylactic shock in a patient with severe aortic stenosis treated with adrenaline and landiolol for circulatory management: A case report.

We present the first case of a patient with severe aortic stenosis who developed anaphylactic shock and was successfully treated with adrenaline and landiolol, a highly selective β1-receptor blocker, to prevent disruption of the myocardial oxygen supply-demand balance caused by tachycardia.
Akihiro Yokoyama, Motohiro Sekino, Taiga Ichinomiya, Hironori Ishizaki, Keiko Ogami-Takamura, Takashi Egashira, Rintaro Yano, Sojiro Matsumoto, Ushio Higashijima, Tetsuya Hara

1510 related Products with: Anaphylactic shock in a patient with severe aortic stenosis treated with adrenaline and landiolol for circulatory management: A case report.

100 μg

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#34475067   2021/09/01 To Up

Renal Function Improves After the Discontinuation of Androgen Deprivation Therapy in Japanese Patients With Prostate Cancer.

Androgen deprivation therapy (ADT) is one of the most effective treatments for advanced prostate cancer (PCa). However, it has been reported that the use of ADT is significantly associated with an increased risk of acute kidney injury (AKI) among patients with newly diagnosed non-metastatic PCa. We investigated changes in renal function that occurred in Japanese patients with PCa after ADT was discontinued.
Hiroshi Masuda, Ayumi Fujimoto, Manato Kanesaka, Kyokusin Hou, Takahito Suyama, Kazuhiro Araki, Satoko Kojima, Yukio Naya

2501 related Products with: Renal Function Improves After the Discontinuation of Androgen Deprivation Therapy in Japanese Patients With Prostate Cancer.



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#34472702   2021/09/02 To Up

Nuclear receptor HR96 upregulates cytochrome P450 for insecticide detoxification in Tribolium castaneum.

Red flour beetle, Tribolium castaneum, is a major agricultural pest that causes significant damage to stored grains and products. Although hormone receptor 96 (HR96) is known to be the single ortholog corresponding to mammalian constitutive androstane receptor and pregnane X receptor, structural feature of Tribolium HR96 (TcHR96) and its role in insecticide-mediated transcription control of cytochrome P450 enzyme genes in T. castaneum have not been elucidated yet.
In-Young Kim, Byungyoon Choi, Woo-Ram Park, Yu-Ji Kim, Bo-Eun Kim, Seulgi Mun, Hueng-Sik Choi, Don-Kyu Kim

1101 related Products with: Nuclear receptor HR96 upregulates cytochrome P450 for insecticide detoxification in Tribolium castaneum.

2 Pieces/Box2 Pieces/Box100ug Lyophilized100ug50 ug100ug Lyophilized8 inhibitors 1 G100ug Lyophilized100ug100 μg

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#34470165   2021/06/07 To Up

Spermiogenesis toxicity of imidacloprid in rats, possible role of CYP3A4.

This study evaluated the adverse effects of low-dose imidacloprid (IMI) on the characteristics of sperm from male Wistar rats. Thirty mature male rats were equally divided into three groups and orally administered vehicle (Control Group), acceptable daily intake (ADI) concentration of IMI (Group 1), and IMI at a dose 10-fold that of the ADI (Group 2) for 90 days. The findings revealed that IMI caused abnormalities in sperm concentrations and morphologies, accompanied by an imbalance of the gonadal hormone testosterone. Histopathological damage and decrease of testosterone levels were observed in testes from rats treated with IMI. However, estradiol and gonadotropin levels were unchanged after IMI treatment. IMI inhibited the activity of cytochrome P450 3A4 (CYP3A4) and left itself existed in the organism of rats. The indicators relating to sperms and CYP3A4 activity were recovered when rats were co-treated with IMI and CYP3A4 inducer rifampicin together. These results indicated that low-dose IMI exposure caused sperm abnormalities through affecting on the spermiogenesis in testis. Inhibition of CYP3A4 activity by IMI largely contributed to its sperm toxicity. Thus, IMI exposure at doses close to real-world settings resulted in sperm toxicity on rats, which might be a potential risk factor for human reproductive diseases.
Guo-Ping Zhao, Jin-Wang Li, Fang-Wei Yang, Xue-Feng Yin, Fa-Zheng Ren, Bing Fang, Guo-Fang Pang

2184 related Products with: Spermiogenesis toxicity of imidacloprid in rats, possible role of CYP3A4.

100 UG100 μg 5 G100ug Lyophilized20mg1 mg11 inhibitors100 μg200 96 assays

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