scholarly journals The Uridine Diphosphate Glucuronosyltransferase 2B15 D85Y and 2B17 Deletion Polymorphisms Predict the Glucuronidation Pattern of Androgens and Fat Mass in Men

2007 ◽  
Vol 92 (12) ◽  
pp. 4878-4882 ◽  
Author(s):  
Charlotte Swanson ◽  
Dan Mellström ◽  
Mattias Lorentzon ◽  
Liesbeth Vandenput ◽  
Jenny Jakobsson ◽  
...  

Abstract Context: Previous in vitro studies have demonstrated that the UDP glucuronosyltransferase (UGT)2B15 and UGT2B17 glucuronidate androgens and their metabolites. Objective: Our objective was to determine in vivo whether the UGT2B15 D85Y and the UGT2B17 deletion polymorphisms predict androgen glucuronidation and body composition. Participants: Two population-based cohorts including young adult (n = 1068; age = 18.9 yr) and elderly (n = 1001; age = 75.3 yr) men were included in the study. Main Outcome Measures: Serum and urine levels of testosterone (T) and dihydrotestosterone (DHT) were measured by gas chromatography-mass spectrometry, and serum levels of the major glucuronidated androgen metabolites androstane-3α,17β-diol(androstanediol)-3-glucuronide, androstanediol-17-glucuronide, and androsterone-glucuronide were measured by liquid chromatography-tandem mass spectrometry. Body composition was measured by dual-energy x-ray absorptiometry. Results: Both the UGT2B15 D85Y and the UGT2B17 deletion polymorphisms were associated with serum levels of androstanediol-17-glucuronide (P < 0.001) but not with levels of androstanediol-3-glucuronide or androsterone-glucuronide in both cohorts. Glucuronidation of T and DHT was associated with the UGT2B17 deletion but not with the UGT2B15 D85Y polymorphism, suggested by strong associations between the deletion polymorphism and urine levels of these two hormones. Both polymorphisms were associated with several different measures of fat mass (P < 0.01). The UGT2B17 deletion polymorphism was associated with insulin sensitivity (P < 0.05) as indicated by the homeostasis model assessment index. Conclusions: The UGT2B15 D85Y and the UGT2B17 deletion polymorphisms are both predictors of the glucuronidation pattern of androgens/androgen metabolites. Our findings indicate that UGT2B17 is involved in 17-glucuronidation of mainly T but also of DHT and androstanediol and that UGT2B15 is involved in the 17-glucuronidation of androstanediol. Furthermore, these two polymorphisms are predictors of fat mass in men.

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1555
Author(s):  
Enas E. Eltamany ◽  
Usama Ramadan Abdelmohsen ◽  
Dina M. Hal ◽  
Amany K. Ibrahim ◽  
Hashim A. Hassanean ◽  
...  

Chemical investigation of the methanolic extract of the Red Sea cucumber Holothuria spinifera led to the isolation of a new cerebroside, holospiniferoside (1), together with thymidine (2), methyl-α-d-glucopyranoside (3), a new triacylglycerol (4), and cholesterol (5). Their chemical structures were established by NMR and mass spectrometric analysis, including gas chromatography–mass spectrometry (GC–MS) and high-resolution mass spectrometry (HRMS). All the isolated compounds are reported in this species for the first time. Moreover, compound 1 exhibited promising in vitro antiproliferative effect on the human breast cancer cell line (MCF-7) with IC50 of 20.6 µM compared to the IC50 of 15.3 µM for the drug cisplatin. To predict the possible mechanism underlying the cytotoxicity of compound 1, a docking study was performed to elucidate its binding interactions with the active site of the protein Mdm2–p53. Compound 1 displayed an apoptotic activity via strong interaction with the active site of the target protein. This study highlights the importance of marine natural products in the design of new anticancer agents.


2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Kajsa Roslund ◽  
Markku Lehto ◽  
Pirkko Pussinen ◽  
Kari Hartonen ◽  
Per-Henrik Groop ◽  
...  

AbstractWe have measured the volatile fingerprints of four pathogenic oral bacteria connected to periodontal disease and dental abscess: Porphyromonas gingivalis (three separate strains), Prevotella intermedia, Prevotella nigrescens and Tannerella forsythia. Volatile fingerprints were measured in vitro from the headspace gas of the bacteria cultured on agar. Concrete identification of new and previously reported bacterial volatiles were performed by a combination of solid phase microextraction (SPME) and offline gas chromatography–mass spectrometry (GC–MS). We also studied the effect of the reduced electric field strength (E/N) on the fragmentation patterns of bacterial volatiles in online proton-transfer-reaction time-of-flight mass spectrometry (PTR-ToF-MS). We aimed to discover possible new biomarkers for the studied oral bacteria, as well as to validate the combination of GC–MS and PTR-MS for volatile analysis. Some of the most promising compounds produced include: 1-Methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ), indole, and a cascade of sulphur compounds, such as methanethiol, dimethyl disulphide (DMDS) and dimethyl trisulphide (DMTS). We also found that several compounds, especially alcohols, aldehydes and esters, fragment significantly with the PTR-MS method, when high E/N values are used. We conclude that the studied oral bacteria can be separated by their volatile fingerprints in vitro, which could have importance in clinical and laboratory environments. In addition, using softer ionization conditions can improve the performance of the PTR-MS method in the volatile analysis of certain compounds.


2021 ◽  
Vol 17 (5) ◽  
pp. 54
Author(s):  
RaghavendraLakshmana Shetty Hallur ◽  
ChaitanyaV. N L. Motamarri ◽  
PrashithKekuda T. Ramamoorthy ◽  
ChetanD Murthy ◽  
RavikumarPatil H. Siddappa ◽  
...  

2016 ◽  
Vol 88 (1) ◽  
pp. 281-292 ◽  
Author(s):  
CHARLENE S.C. GARCIA ◽  
CAROLINE MENTI ◽  
ANA PAULA F. LAMBERT ◽  
THIAGO BARCELLOS ◽  
SIDNEI MOURA ◽  
...  

ABSTRACT Salvia officinalis (Lamiaceae) has been used in south of Brazil as a diary homemade, in food condiment and tea-beverage used for the treatment of several disorders. The objective of this study was to characterize chemical compounds in the hydroalcoholic (ExtHS) and aqueous (ExtAS) extract from Salvia officinalis (L.) by gas chromatography-mass spectrometry (GC-MS) and by high-resolution electrospray ionization mass spectrometry (ESI-QTOF MS/MS), evaluate in vitro ability to scavenge the free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH•) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS•+), catalase (CAT-like) and superoxide dismutase (SOD-like) activity, moreover cytotoxic by MTT assay, alterations on cell morphology by giemsa and apoptotic-induced mechanism for annexin V/propidium iodide. Chemical identification sage extracts revealed the presence of acids and phenolic compounds. In vitro antioxidant analysis for both extracts indicated promising activities. The cytotoxic assays using tumor (Hep-2, HeLa, A-549, HT-29 and A-375) and in non-tumor (HEK-293 and MRC-5), showed selectivity for tumor cell lines. Immunocytochemistry presenting a majority of tumor cells at late stages of the apoptotic process and necrosis. Given the results presented here, Brazilian Salvia officinalis (L.) used as condiment and tea, may protect the body against some disease, in particularly those where oxidative stress is involved, like neurodegenerative disorders, inflammation and cancer.


1995 ◽  
Vol 88 (3) ◽  
pp. 319-324 ◽  
Author(s):  
Susan A. Jebb ◽  
Gail R. Goldberg ◽  
Graham Jennings ◽  
Marinos Elia

1. There are few data regarding the accuracy of Hologic QDR-1000W dual-energy X-ray absorptiometry for the measurement of body composition. In two studies, one in an in vitro experimental system using oil and water mixtures and the other in samples of pork meat, the effect of depth and tissue thickness on the measured composition was assessed. In the latter study the measured fat mass was compared with that measured by direct analysis. 2. All data indicated a trend in the measured fat mass with depth, such that more fat was measured at extremes of depth (<10 cm and >25 cm) than at intermediate depths. 3. In samples of meat weighing approximately 55 kg, dual X-ray absorptiometry significantly underestimated the absolute fat mass compared with direct analysis (mean 20.4 ± 1.65%) by 5–8% or 1–4 kg of fat. 4. These findings are of direct relevance to both clinical and research work using this technique to measure body composition, in particular in circumstances in which changes in body composition and/or tissue thickness are anticipated.


Author(s):  
Krishnavignesh L Krishnavignesh ◽  
Mahalakshmipriya A ◽  
Ramesh M

  Objective: Continued resistance toward the antibiotics urges us to explore newer antibiotics. Plants are being the safer source of antibiotics with lesser or no side effects. This study was designed to study the presence of phytochemical constituents and antibacterial activity of leaf and flower extracts of Wedelia glauca against urinary tract infection causing pathogens.Methods: The plant leaves were extracted with five different solvents based on the polarity. The extraction was done using soxhalation. Antimicrobial activity was determined by agar well diffusion method for both the sample and standard. The acetone plant extract was subjected to gas chromatography-mass spectrometry (GC-MS) analysis for screening phytoconstituents.Results: Preliminary phytochemical screening revealed the presence of diverse phytoconstituents in the plant. The different extracts exhibited a considerable antimicrobial potential. Among the solvents used acetone extract showed comparably better antimicrobial activity with 100% of inhibition rate with the maximum zone of inhibition of 1.6±0.77 mm against Staphylococcus sp. and Aspergillus sp. at the concentration of 5 mg. GC-MS analysis provided 8 major peaks which revealed the existence of a variety of bioactive compounds which may attribute to the efficacy of the plant.Conclusion: W. glauca leaf and flower extracts displayed a broad spectrum of antibacterial and antifungal activity and can be considered as a potential source of newer antibiotic compounds.


2020 ◽  
Vol 10 (5) ◽  
pp. 307-316
Author(s):  
Mohammad Sanad Abu-Darwish ◽  
Célia Cabral ◽  
Zulfigar Ali ◽  
Mei Wang ◽  
Shabana I. Khan ◽  
...  

Abstract In Jordan, Salvia ceratophylla L. is traditionally used in the treatment of cancer, microbial infections, and urinary disorders. This study aimed: (1) to chemically characterize S. ceratophylla essential oil (EO) from South Jordan, by gas chromatography (GC) and gas chromatography-mass spectrometry (GC–MS); and (2) to evaluate in vitro the cytotoxic, anti-inflammatory, and antiprotozoal activities of the EO, it’s predominant components, and the hexane (A), ethyl acetate (B), methanol (C) and crude-methanol extracts (D). The analysis revealed that the EO has 71 compounds, with linalool (54.8%) as main constituent. Only the hexane extract (A) showed some cytotoxic activity against SK-MEL, KB, BT-549, SK-OV-3, LLC-PK1 and VERO cells lines with IC50 between 60 and > 100 µg/mL. The EO inhibited NO production (IC50 90 µg/mL) and NF-κB activity (IC50 38 µg/mL). The extracts A, B, and D inhibited NO production and NF- κB activity with IC50 between 32 and 150 µg/mL. Linalool considerably inhibited NO production (IC50 18 µg/mL). The extracts tested did not exhibit antileishmanial activity. Regarding antitrypanosomal activity, the EO exhibited significant results with IC50 2.65 µg/mL. In conclusion, Jordan S. ceratophylla EO represents a rich source of linalool and bears a promising therapeutic potential for further antitrypanosomal drug development.


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