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Steroids

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https://www.readbyqxmd.com/read/28435038/a-convergent-synthesis-of-novel-alkyne-azide-cycloaddition-congeners-of-betulinic-acid-as-potent-cytotoxic-agent
#1
Nisar A Dangroo, Jasvinder Singh, Santosh K Rath, Nidhi Gupta, Arem Qayum, Shashank Singh, Payare L Sangwan
In an endeavour to develop potent anti-tumor agents from betulinic acid (BA), a series of C-28 derived 1,2,3-triazolyl derivatives were designed and synthesized by employing Cu(I) catalyzed Huisgen 1,3-dipolar cycloaddition reaction. All the derivatives were evaluated for cytotoxic activity by MTT assay against five different human cancer cell lines: lung (A549), colon (HCT116), prostate (PC3), pancreatic (MIA PaCa-2) and breast (T47D). The data revealed that compounds 11c, 11d, 11g, 11h and 13a possess most promising cytotoxic potential...
April 20, 2017: Steroids
https://www.readbyqxmd.com/read/28404456/biotransformation-of-anabolic-compound-methasterone-with-macrophomina-phaseolina-cunninghamella-blakesleeana-and-fusarium-lini-and-tnf-%C3%AE-inhibitory-effect-of-transformed-products
#2
Malik Shoaib Ahmad, SammerYousuf, Atia-Tul-Wahab, Almas Jabeen, Atta-Ur-Rahman, M Iqbal Choudhary
Microbial transformation of methasterone (1) was investigated with Macrophomina phaseolina, Cunninghamella blakesleeana, and Fusarium lini. Biotransformation of 1 with M. phaseolina yielded metabolite 2, while metabolites 3-7 were obtained from the incubation of 1 with C. blakesleeana. Metabolites 8-13 were obtained through biotransformation with F. lini. All metabolites, except 13, were found to be new. Methasterone (1) and its metabolites 2-6, 9, 10, and 13 were then evaluated for their immunomodulatory effects against TNF-α, NO , and ROS production...
April 9, 2017: Steroids
https://www.readbyqxmd.com/read/28396219/novel-synthesis-of-steroidal-oximes-and-lactams-and-their-biological-evaluation-as-antiproliferative-agents
#3
Roxana Martínez-Pascual, Socorro Meza-Reyes, José Luis Vega-Baez, Penélope Merino-Montiel, José M Padrón, Ángel Mendoza, Sara Montiel-Smith
A novel three-step methodology to obtain 6a-aza-B-homo steroidal lactams has been developed starting from the easily available cholesterol and pregnenolone. In addition, a new procedure for the synthesis of a 6a-aza-B-homo steroidal lactam analog of vespertilin, starting from diosgenin has been established. In both synthetic pathways, the key intermediate is a hydroxyimino derivative obtained in a one- or two-step sequence from the starting materials. These methods avoid the use of hazardous oxidant agents in the process...
April 7, 2017: Steroids
https://www.readbyqxmd.com/read/28377207/2-naphthoic-acid-ergosterol-ester-an-ergosterol-derivative-exhibits-anti-tumor-activity-by-promoting-apoptosis-and-inhibiting-angiogenesis
#4
Mingzhu Lin, Haijun Li, Yan Zhao, Enbo Cai, Hongyan Zhu, Yugang Gao, Shuangli Liu, He Yang, Lianxue Zhang, Guosheng Tang
Phytosterol is a natural component of vegetable oil and includes ergosterol (ER) and β-sitosterol. In this study, three new ergosterol monoester derivatives were obtained from the reflux reaction with ergosterol, organic acids (furoic acid, salicylic acid, and 2-naphthoic acid), EDCI, and DMAP in dichloromethane. The chemical structures were defined by IR and NMR. On the basis of the results, 2-naphthoic acid ergosterol ester (NE) had the highest tumor inhibition rate and was selected to study anti-tumor activity and its mechanism at doses of 0...
April 1, 2017: Steroids
https://www.readbyqxmd.com/read/28342744/synthesis-and-anti-cancer-activity-of-chiral-tetrahydropyrazolo-1-5-a-pyridine-fused-steroids
#5
Susana M M Lopes, Emanuel P Sousa, Luísa Barreira, Cátia Marques, Maria João Rodrigues, Teresa M V D Pinho E Melo
Regio- and stereoselective synthesis of novel chiral 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine-fused steroids via [8π+2π] cycloaddition of diazafulvenium methides with steroidal scaffolds is reported. The biological evaluation of the new family of hexacyclic steroids as anti-cancer agents was also carried out. Hexacyclic steroids bearing a benzyl group at C-22, derived from 16-dehydropregnenolone and 16-dehydroprogesterone, show considerable cytotoxicity against EL4 (murine T-lymphoma) in contrast with the corresponding C-22-unsubstituted derivatives showing low cytotoxicity...
March 22, 2017: Steroids
https://www.readbyqxmd.com/read/28327355/cytotoxic-and-apoptosis-inducing-activity-of-c21-steroids-from-the-roots-of-cynanchum-atratum
#6
Jian Zhang, Lin Ma, Zheng-Feng Wu, Shu-Le Yu, Lei Wang, Wen-Cai Ye, Qing-Wen Zhang, Zhi-Qi Yin
Two new (1-2) and two known C21 steroids (3-4) were isolated from the roots of Cynanchum atratum. Their structures were elucidated by detailed 1D and 2D spectroscopic. The MTT assay showed that compounds 1-4 displayed obvious cytotoxic activities against HepG2 cells with IC50 values ranging from 10.19μM to 76.12μM. Compounds 1-3 also exhibited cytotoxic effects in A549 cells with IC50 values of 30.87-95.39μM. Compound 3 showed the antiproliferative activity via G0/G1 cell cycle arrest and proapoptosis in HepG2 cells by Flowcytometry analysis...
March 19, 2017: Steroids
https://www.readbyqxmd.com/read/28322864/water-soluble-derivatives-of-25-och3-ppd-and-their-anti-proliferative-activities
#7
Wu-Xi Zhou, Yuan-Yuan Sun, Wei-Hui Yuan, Yu-Qing Zhao
(20R)-25-Methoxyl-dammarane-3β,12β,20-triol (25-OCH3-PPD, AD-1) is a dammarane-type sapogenin showing anti-tumor potential. In the search for new anti-tumor agents with higher potency than our previously identified compound 25-OCH3-PPD, 11 novel sulfamic acid and diacid derivatives that could improve water solubility and contribute to good drug potency and pharmacokinetic profiles were designed and synthesized. Their in vitro anti-tumor activities in MCF-7, A-549, HCT-116, and BGC-823 cell lines and one normal cell line were tested by standard MTT assay...
March 18, 2017: Steroids
https://www.readbyqxmd.com/read/28300583/synthesis-of-new-c-25-and-c-26-steroidal-acids-as-potential-ligands-of-the-nuclear-receptors-daf-12-lxr-and-gr
#8
María V Dansey, María C Del Fueyo, Adriana S Veleiro, Pablo H Di Chenna
A new methodology to obtain C-25 and C-26 steroidal acids starting from pregnenolone is described. Construction of the side chain was achieved by applying the Mukaiyama aldol reaction with a non-hydrolytic work-up to isolate the trapped silyl enol ether with higher yields. Using this methodology we synthesized three new steroidal acids as potential ligands of DAF-12, Liver X and Glucocorticoid nuclear receptors and studied their activity in reporter gene assays. Our results show that replacement of the 21-CH3 by a 20-keto group in the side chains of the cholestane scaffold of DAF-12 or Liver X receptors ligands causes the loss of the activity...
March 11, 2017: Steroids
https://www.readbyqxmd.com/read/28288896/age-and-menopause-related-differences-in-subcutaneous-adipose-tissue-estrogen-receptor-mrna-expression
#9
Young-Min Park, Christopher Erickson, Dan Bessesen, Rachael E Van Pelt, Kimberly Cox-York
OBJECTIVES: Changes in estrogen receptor (ER) expression likely underlie differential metabolic effects of estrogen in pre- and postmenopausal women. The aim of the current study was to determine whether ER gene expression in abdominal and femoral subcutaneous adipose tissue (SAT) was associated with age, menopause, or regional adiposity. METHODS: We studied pre- and post-menopausal (n=23 and 22, respectively; age 35-65y) normal weight (mean±SD; BMI 23.7±2.5kg/m(2)) women with similar total fat mass...
March 10, 2017: Steroids
https://www.readbyqxmd.com/read/28267564/development-of-17%C3%AE-hydroxysteroid-dehydrogenase-type-3-as-a-target-in-hormone-dependent-prostate-cancer-therapy
#10
REVIEW
Xiaohui Ning, Yan Yang, Hong Deng, Qihao Zhang, Yadong Huang, Zhijian Su, Yongmei Fu, Qi Xiang, Shu Zhang
17β-Hydroxysteroid dehydrogenase type 3 (17β-HSD3) is expressed almost exclusively in the testes and specifically converts the weak androgenic androstenedione to active testosterone (T) in the presence of NADPH. Additionally, studies have demonstrated that 17β-HSD3 is over-expressed in hormone-dependent prostate cancer. T, which interacts with the androgen receptor (AR), eventually stimulates the growth of prostate cancer cells. Defects in T synthesis or action impair the development of the male phenotype during embryogenesis and cause the autosomal recessive disorder male pseudohermaphroditism...
March 4, 2017: Steroids
https://www.readbyqxmd.com/read/28237768/steroidal-saponins-from-datura-metel
#11
Nguyen Thi Mai, Nguyen Thi Cuc, Hoang Le Tuan Anh, Nguyen Xuan Nhiem, Bui Huu Tai, Chau Van Minh, Tran Hong Quang, Kwan Woo Kim, Youn-Chul Kim, Hyuncheol Oh, Phan Van Kiem
Datura metel L. (Solanaceae) is an annual herb that has been widely used in the traditional medicine for the treatment of coughs, bronchial asthma, and rheumatism. Chemical investigation of an acidic methanol extract of the whole plants of D. metel resulted in the isolation of five new steroidal saponins (1-3, 5, and 6), named metelosides A-E, and four known compounds (4, 7-9). Their structures were elucidated by extensive spectroscopic methods, including 1D and 2D NMR and MS spectra. The structures of metelosides A and B were found to be unusual among the reported spirostane-type steroidal saponins due to the presence of the acetamide groups in the molecules...
February 22, 2017: Steroids
https://www.readbyqxmd.com/read/28300584/synthesis-of-side-chain-oxysterols-and-their-enantiomers-through-cross-metathesis-reactions-of-%C3%AE-22-steroids
#12
David P Brownholland, Douglas F Covey
A synthetic route that utilizes a cross-metathesis reaction with Δ(22) steroids has been developed to prepare sterols with varying C-27 side-chains. Natural sterols containing hydroxyl groups at the 25 and (25R)-26 positions were prepared. Enantiomers of cholesterol and (3β,25R)-26-hydroxycholesterol (27-hydroxycholesterol) trideuterated at C-19 were prepared for future biological studies.
May 2017: Steroids
https://www.readbyqxmd.com/read/28192128/antitumor-activity-of-newly-synthesized-oxo-and-ethylidene-derivatives-of-bile-acids-and-their-amides-and-oxazolines
#13
Srđan Bjedov, Dimitar Jakimov, Ana Pilipović, Mihalj Poša, Marija Sakač
Bile acid derivatives with modifications in side chain and modifications on steroid skeleton were synthetized and their antitumor activity against five human cancer cell lines was investigated. Modifications in side chain include amid group, formed in reaction with 2-amino-2-methylpropanol, and 4,4-dimethyloxazoline group, obtained after cyclization of amides. In the steroid skeleton oxo groups were introduced in position 7 (2, 2a, 2b) and 7,12 (3, 3a, 3b). Ethylidene groups were introduced regio- and stereoselectively on C-7, and/or without stereoselectivity on C-3 by Wittig reaction...
April 2017: Steroids
https://www.readbyqxmd.com/read/28192127/long-term-treatment-with-nandrolone-decanoate-impairs-mesenteric-vascular-relaxation-in-both-sedentary-and-exercised-female-rats
#14
Izabela F Caliman, Cristian S Bernabe, Antônio F de Melo, Girlândia A Brasil, Andrews M do Nascimento, Ewelyne M de Lima, Suely G Figueiredo, Tadeu U de Andrade, Nazaré S Bissoli
Nandrolone Decanoate (ND) is an Anabolic Androgenic Steroid (AAS) that under abusive regimen can lead to multiple physiological adverse effects. Studies of AAS-mediated cardiovascular (CV) alterations were mostly taken from male subjects, even though women are also susceptible to the effects of AAS and gender-specific differences in susceptibility to vascular diseases exist. Here we investigate ND-induced vascular reactivity alterations in both sedentary and exercised female rats and whether these alterations depend on endothelium-derived factors...
April 2017: Steroids
https://www.readbyqxmd.com/read/28189541/adhesive-blood-microsampling-systems-for-steroid-measurement-via-lc-ms-ms-in-the-rat
#15
Kirsten Heussner, Manfred Rauh, Nada Cordasic, Carlos Menendez-Castro, Hanna Huebner, Matthias Ruebner, Marius Schmidt, Andrea Hartner, Wolfgang Rascher, Fabian B Fahlbusch
INTRODUCTION: Liquid Chromatography Tandem Mass Spectrometry (LC-MS/MS) allows for the direct analysis of multiple hormones in a single probe with minimal sample volume. Rodent-based animal studies strongly rely on microsampling, such as the dry blood spot (DBS) method. However, DBS suffers the drawback of hematocrit-dependence (non-volumetric). Hence, novel volumetric microsampling techniques were introduced recently, allowing sampling of fixed accurate volumes. We compared these methods for steroid analysis in the rat to improve inter-system comparability...
April 2017: Steroids
https://www.readbyqxmd.com/read/28167101/quinone-related-hexacyclic-by-products-in-the-production-process-of-exemestane
#16
Giovanni Battista Giovenzana, Norberto Masciocchi, Roberto Negri, Giovanni Palmisano, Andrea Penoni, Lucio Toma
Exemestane, a 3rd-generation aromatase inhibitor, is clinically used in the treatment of breast cancer in postmenopausal women. The key step of the industrial synthetic process, i.e., a dehydrogenation to introduce the Δ(1)-unsaturation, is normally performed with quinones such as p-chloranil or DDQ. We observed the formation of two different hexacyclic by-products, depending on the quinone used in the oxidation step. These compounds arise from an initial [4+2] cycloaddition between the precursor 6-methylenandrost-4-ene-3,17-dione and the quinone reagent, followed by a twofold dehydrohalogenation (with p-chloranil) or dehydrogenation (with DDQ)...
April 2017: Steroids
https://www.readbyqxmd.com/read/28163026/engineering-of-cyp106a2-for-steroid-9%C3%AE-and-6%C3%AE-hydroxylation
#17
Julia Nikolaus, Kim Thoa Nguyen, Cornelia Virus, Jan L Riehm, Michael Hutter, Rita Bernhardt
CYP 106A2 from Bacillus megaterium ATCC 13368 has been described as a 15β-hydroxylase showing also minor 11α-, 9α- and 6β-hydroxylase activity for progesterone conversion. Previously, mutant proteins with a changed selectivity towards 11α-OH-progesterone have already been produced. The challenge of this work was to create mutant proteins with a higher regioselectivity towards hydroxylation at positions 9 and 6 of the steroid molecule. 9α-hydroxyprogesterone exhibits pharmaceutical importance, because it is a useful intermediate in the production of physiologically active substances which possess progestational activity...
April 2017: Steroids
https://www.readbyqxmd.com/read/27998756/effects-of-24-epibrassinolide-and-green-light-on-plastid-gene-transcription-and-cytokinin-content-of-barley-leaves
#18
Marina V Efimova, Radomira Vankova, Victor V Kusnetsov, Raisa P Litvinovskaya, Ilya E Zlobin, Petre Dobrev, Nina P Vedenicheva, Alina L Savchuk, Raisa A Karnachuk, Natalia V Kudryakova, Vladimir V Kuznetsov
In order to evaluate whether brassinosteroids (BS) and green light regulate the transcription of plastid genes in a cross-talk with cytokinins (CKs), transcription rates of 12 plastid genes (ndhF, rrn23, rpoB, psaA, psaB, rrn16, psbA, psbD, psbK, rbcL, atpB, and trnE/trnY) as well as the accumulation of transcripts of some photoreceptors (PHYA, CRY2, CRY1A, and CRY1B) and signaling (SERK and CAS) genes were followed in detached etiolated barley leaves exposed to darkness, green or white light ±1μm 24-epibrassinolide (EBL)...
April 2017: Steroids
https://www.readbyqxmd.com/read/28119081/neuroprotective-effect-and-mechanism-of-daucosterol-palmitate-in-ameliorating-learning-and-memory-impairment-in-a-rat-model-of-alzheimer-s-disease
#19
Zhi-Hong Ji, Zhong-Qi Xu, Hong Zhao, Xin-Yu Yu
Alzheimer's disease (AD) is an age-related neurodegenerative disorder characterized by progressive memory decline and cognitive impairment. Amyloid beta (Aβ) has been proposed as the causative role for the pathogenesis of AD. Accumulating evidence demonstrates that Aβ neurotoxicity is mediated by glutamate excitotoxicity. Daucosterol palmitate (DSP), a plant steroid with anti-glutamate excitotoxicity effect, was isolated from the anti-aging traditional Chinese medicinal herb Alpinia oxyphylla Miq. in our previous study...
March 2017: Steroids
https://www.readbyqxmd.com/read/28041951/the-role-of-sex-hormones-and-steroid-receptors-on-female-reproductive-cancers
#20
REVIEW
Luiz Gustavo de Almeida Chuffa, Luiz Antonio Lupi-Júnior, Aline Balandis Costa, João Paulo de Arruda Amorim, Fábio Rodrigues Ferreira Seiva
Sex steroids have been widely described to be associated with a number of human diseases, including hormone-dependent tumors. Several studies have been concerned about the factors regulating the availability of sex steroids and its importance in the pathophysiological aspects of the reproductive cancers in women. In premenopausal women, large fluctuations in the concentration of circulating estradiol (E2) and progesterone (P4) orchestrate many events across the menstrual cycle. After menopause, the levels of circulating E2 and P4 decline but remain at high concentration in the peripheral tissues...
February 2017: Steroids
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