scholarly journals Sensitive, High-Throughput Liquid Chromatography-Tandem Mass Spectrometry Analysis of Atorvastatin and Its Pharmacologically Active Metabolites in Serum for Supporting Precision Pharmacotherapy

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1324
Author(s):  
Gellért Balázs Karvaly ◽  
István Vincze ◽  
István Karádi ◽  
Barna Vásárhelyi ◽  
András Zsáry

The antihyerlipidemic drug atorvastatin (ATR) is used worldwide as part of the strategy to prevent cardiovascular events. The high prevalence of patient nonadherence remains an important challenge which could be addressed efficiently by precision pharmacotherapy based on therapeutic drug monitoring (TDM). ATR is metabolized to pharmacologically active metabolites, and evidence shows that the sums of ATR acid and lactone form concentrations (ATR + ATRL), or of ATR and hydroxylated metabolites (ATR + MET) should be assayed. A method is presented for the analysis of these substances in serum. Method validation included the estimation of the quantitative relationship between the concentrations and the standard deviations (SD), which supports the optimal incorporation of TDM results into nonparametric pharmacokinetic models. The concentrations of the analytes were evaluated in human subjects receiving ATR. The method’s performance improved by taking the sums of acid and lactone concentrations into account. The concentration–SD relationship was linear, and we recommend applying Theil’s regression for estimating the assay error. All analytes could be detected by 2 h post dose in the samples of human subjects. The changes in metabolite/parent drug concentration ratios in time depended on the dose. The method is suitable for the TDM of ATR with a focus on precision pharmacotherapy.

Author(s):  
ANITA ROY A ◽  
ANGEL MARY ◽  
INDU SABAPATHY ◽  
MANIKKAM RAJALAKSHMI

Objective: The present study was aimed to evaluate the anticancer property of eremanthin isolated from Costus speciosus against breast cancer using in vitro and in silico approaches and thereby to develop eremanthin as a typical phytotherapeutic drug against cancer. Methods: The presence of specific biologically active extract was confirmed under GC–MS/MS (gas chromatography–mass spectrometry) analysis. The cell proliferation inhibitory effect of the eremanthin was confirmed by MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) and LDH (lactate dehydrogenase) assay. In silico studies were performed to predict the targeted interaction of eremanthin with cancer proteins. Results: The GC–MS/MS analysis confirmed the presence of eremanthin with peak value of RA: 20.03. The MTT and LDH assays revealed the antiproliferative activity of eremanthin on MCF-7 and MDA-MB-231 breast cancer cell lines. The results provide stable interaction between eremanthin and cancer target proteins. Conclusion: Thus, the compound can be used as an effective herbal therapeutic molecule to treat cancer with further explorations.


2019 ◽  
Vol 16 (04) ◽  
pp. 779-787 ◽  
Author(s):  
Anan Kalakattawi ◽  
Sana G. Al Attas ◽  
Sherif Edris ◽  
Ahmed Z. Abdel Azeiz ◽  
Ahmad F. AlGuthami ◽  
...  

ABSTRACT: Candida albicans is a common human yeast that infect several epithelial tissues including vagina. The increase of drug-resisting C. albicans encouraged the researchers to find alternative treatment. Honey medical signatures such as bactericidal, antifungal and anti-candida made it a possible candidate for disease treatment. In addition, rose essential oil possesses a wide range of biochemical activities in folkloric medicine including anti-microbial activities. The present research utilizes honey alone or in conjunction with Taifi rose (Rosa damascena) oil as anti-candida agent to treat vaginal candidiasis. Three local monof oral honeys from different flower sources and/or geographic origins were tested with four concentrations (50, 80 and 95%), while two concentrations of the Taifi rose oil (1 and 2%). anti-candida activity of honey alone or in conjunction with Taifi rose oil was determined as well as phenolic and flavonoids contents were determined. Also, GC-MS analysis of volatile oils and alkaloids were evaluated. The results of this study indicated that acidity is within the allowed range for commercialization and long-lasting storage. All honeys tested inhibited completely the C. albicans growth at concentrations 80% and 95% either incubation after 48 or 72 h. Also, only Markh and Manuka honeys were completely inhibited C. albicans growth at 50% concentration. Also, C. albicans growth inhibited completely at 2% Taifi rose oil after the incubation periods of 48 and 72 h. The phenolic compounds and flavonoids were analysed by mass spectrometry analysis which revealed the Markh honey showed the presence of gallic acid and quercetin that proved to have antifungal activity. It could be concluded that mixed Markh honey and Taifi rose oil treatment was capable to inhibit C. albicans growth completely. Further research is required to determine the anti-candida activity of the mixture of Markh honey and Taifi rose oil in the human body as a new therapeutic drug to treat vaginal candidiasis.


2019 ◽  
Vol 20 (10) ◽  
pp. 2576 ◽  
Author(s):  
Cristina Alexandra Ciocan-Cartita ◽  
Ancuța Jurj ◽  
Mihail Buse ◽  
Diana Gulei ◽  
Cornelia Braicu ◽  
...  

Mass spectrometry (MS) is an essential analytical technology on which the emerging omics domains; such as genomics; transcriptomics; proteomics and metabolomics; are based. This quantifiable technique allows for the identification of thousands of proteins from cell culture; bodily fluids or tissue using either global or targeted strategies; or detection of biologically active metabolites in ultra amounts. The routine performance of MS technology in the oncological field provides a better understanding of human diseases in terms of pathophysiology; prevention; diagnosis and treatment; as well as development of new biomarkers; drugs targets and therapies. In this review; we argue that the recent; successful advances in MS technologies towards cancer omics studies provides a strong rationale for its implementation in biomedicine as a whole.


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