The Therapeutic and Diagnostic Value of Fluorine

2020 ◽  
Vol 4 (1) ◽  
pp. 17-29
Author(s):  
Isma Attique ◽  
Shabbir Hussain ◽  
Muhammad Amjad ◽  
Khalida Nazir ◽  
Muhammad Shahid Nazir

Fluorine has a useful positron transmitting isotope and it enjoys broad application in the medical field. It is utilized in fluorinated agents,therapeutic sciences and steroid field. Fluorine incorporation viafluoroalkylation is a useful approach in the development of new functional materials and in drug design. Fluorine also plays its role as an anticancer agent and is a successful chemotherapeutic agent for certain sorts of malignant growth. 5-fluorouracil plays a vital role in the treatment of cancer. 18 Facts as a radio label tracer atom in PET imaging. 19 F has the second most sensitive and stable NMR-active nucleus.

Cells ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 178
Author(s):  
Jiann Ruey Ong ◽  
Oluwaseun Adebayo Bamodu ◽  
Nguyen Viet Khang ◽  
Yen-Kuang Lin ◽  
Chi-Tai Yeh ◽  
...  

Hepatocellular carcinoma (HCC) is one of the most diagnosed malignancies and a leading cause of cancer-related mortality globally. This is exacerbated by its highly aggressive phenotype, and limitation in early diagnosis and effective therapies. The SUMO-activating enzyme subunit 1 (SAE1) is a component of a heterodimeric small ubiquitin-related modifier that plays a vital role in SUMOylation, a post-translational modification involving in cellular events such as regulation of transcription, cell cycle and apoptosis. Reported overexpression of SAE1 in glioma in a stage-dependent manner suggests it has a probable role in cancer initiation and progression. In this study, hypothesizing that SAE1 is implicated in HCC metastatic phenotype and poor prognosis, we analyzed the expression of SAE1 in several cancer databases and to unravel the underlying molecular mechanism of SAE1-associated hepatocarcinogenesis. Here, we demonstrated that SAE1 is over-expressed in HCC samples compared to normal liver tissue, and this observed SAE1 overexpression is stage and grade-dependent and associated with poor survival. The receiver operating characteristic analysis of SAE1 in TCGA−LIHC patients (n = 421) showed an AUC of 0.925, indicating an excellent diagnostic value of SAE1 in HCC. Our protein-protein interaction analysis for SAE1 showed that SAE1 interacted with and activated oncogenes such as PLK1, CCNB1, CDK4 and CDK1, while simultaneously inhibiting tumor suppressors including PDK4, KLF9, FOXO1 and ALDH2. Immunohistochemical staining and clinicopathological correlate analysis of SAE1 in our TMU-SHH HCC cohort (n = 54) further validated the overexpression of SAE1 in cancerous liver tissues compared with ‘normal’ paracancerous tissue, and high SAE1 expression was strongly correlated with metastasis and disease progression. The oncogenic effect of upregulated SAE1 is associated with dysregulated cancer metabolic signaling. In conclusion, the present study demonstrates that SAE1 is a targetable cancer metabolic biomarker with high potential diagnostic and prognostic implications for patients with HCC.


2019 ◽  
Author(s):  
Anna Notaro ◽  
Marta Jakubaszek ◽  
Severin Koch ◽  
Riccardo Rubbiani ◽  
Orsolya Dömötör ◽  
...  

Cancer is one of the main causes of death worldwide. Chemotherapy, despite its severe side effects, is to date one of the leading strategies against cancer. Metal-based drugs present several potential advantages when compared to organic ones and gained trust from the scientific community after the approval on the market of the drug cisplatin. Recently, we reported a ruthenium complex ([Ru(DIP)2(sq)](PF6), where DIP is 4,7- diphenyl-1,10-phenantroline and sq is the semiquinonate), with a remarkable potential as chemotherapeutic agent against cancer, both in vitro and in vivo. In this work, we analyse a structurally similar compound, namely [Ru(DIP)2(mal)](PF6), carrying the flavour-enhancing agent approved by the FDA, maltol (mal). To possess an FDA approved ligand is crucial for a complex, whose mechanism of action might include ligand exchange. Herein, we describe the synthesis and characterisation of [Ru(DIP)2(mal)](PF6), its stability in solutions and in conditions which resemble the physiological ones, and its in-depth biological investigation. Cytotoxicity tests on different cell lines in 2D model and on HeLa MultiCellular Tumour Spheroids (MCTS) demonstrated that our compound has higher activity compared to the approved drug cisplatin, inspiring further tests. [Ru(DIP)2(mal)](PF6) was efficiently internalised by HeLa cells through a passive transport mechanism and severely affected the mitochondrial metabolism. <br>


2019 ◽  
Author(s):  
Anna Notaro ◽  
Marta Jakubaszek ◽  
Severin Koch ◽  
Riccardo Rubbiani ◽  
Orsolya Dömötör ◽  
...  

Cancer is one of the main causes of death worldwide. Chemotherapy, despite its severe side effects, is to date one of the leading strategies against cancer. Metal-based drugs present several potential advantages when compared to organic ones and gained trust from the scientific community after the approval on the market of the drug cisplatin. Recently, we reported a ruthenium complex ([Ru(DIP)2(sq)](PF6), where DIP is 4,7- diphenyl-1,10-phenantroline and sq is the semiquinonate), with a remarkable potential as chemotherapeutic agent against cancer, both in vitro and in vivo. In this work, we analyse a structurally similar compound, namely [Ru(DIP)2(mal)](PF6), carrying the flavour-enhancing agent approved by the FDA, maltol (mal). To possess an FDA approved ligand is crucial for a complex, whose mechanism of action might include ligand exchange. Herein, we describe the synthesis and characterisation of [Ru(DIP)2(mal)](PF6), its stability in solutions and in conditions which resemble the physiological ones, and its in-depth biological investigation. Cytotoxicity tests on different cell lines in 2D model and on HeLa MultiCellular Tumour Spheroids (MCTS) demonstrated that our compound has higher activity compared to the approved drug cisplatin, inspiring further tests. [Ru(DIP)2(mal)](PF6) was efficiently internalised by HeLa cells through a passive transport mechanism and severely affected the mitochondrial metabolism. <br>


2018 ◽  
Vol 2 ◽  
Author(s):  
K.K. Asanka Sanjeewa ◽  
You-Jin Jeon

Seaweeds play a vital role as a source of food and ingredients in traditional Korean medicine. Koreans consume seaweed as fresh vegetables, salad, soups, or snacks. There are several edible brown seaweed species are abundant along the shores of the Korean peninsula, such as Ecklonia cava, Hizikia fusiforme, Laminaria japonica, Pelvetia siliquosa, Sargassum fulvellum, and Undaria pinnatifida. With the growing body of scientific evidence, it is clear that these brown seaweeds are not only good substitutes for land vegetables but also a good source of bioactive secondary metabolites. The secondary metabolites identified from edible Korean brown seaweeds (phlorotannins, sulfated polysaccharides, pigments, and sterols) have the potential to be developed as functional food ingredients. However, seaweeds consumption and their industrial level applications as functional materials are limited compared to the land vegetables. Insufficient awareness about health benefits of seaweeds might be the reason for this issue. Thus, in this review health promotion properties associated with edible Korean brown seaweeds are summarized. The present study might therefore increase consumption and industrial use of brown seaweeds.


1958 ◽  
Vol 70 (12supplement) ◽  
pp. 130-136
Author(s):  
Ryoichi Uemura ◽  
Shigeru Iwamori ◽  
Kensaku Hirano ◽  
Tadanobu Okimoto ◽  
Akira Fujii

2021 ◽  
Author(s):  
Yang Dinglong ◽  
Chen Shuai ◽  
Chen Yujing ◽  
Wang Beiyang ◽  
Zhang Guohao ◽  
...  

Abstract Background: Despite cumulative evidence shows osteonecrosis of the femoral head (ONFH) could result in the progressive collapse of the femoral head. The pathogenesis of ONFH remains unclear. Early ONFH is difficult to diagnose due to the lack of effective biomarkers. Method: In Gene Expression Omnibus (GEO) database, we searched the Microarray datasets for serum (GSE123568) in ONFH and normal controls to identify differentially expressed genes (DEGs) by R software. The enrichment analyses were performed to enrich pathways of DEGs. Protein–protein interaction (PPI), miRNA-mRNA co-expression, ceRNA networks were constructed using Cytoscape to identity top15 hub genes, target miRNAs of hub genes and potential regulatory pathways. Furthermore, hub genes validated in GSE74089 with high diagnostic value for ONFH were selected as key genes. The Human Protein Atlas (HPA) and Bgee Database were used to find out the subcellular and tissue distribution of key genes.Results: A total of 568 DEGs were identified between 30 ONFH samples and 10 normal controls. Kyoto Encyclopedia of Genes and Genomes (KEGG) and Gene Ontology (GO) enrichment analysis showed that DEGs are mostly enriched in innate immune responses, thrombosis and signal transduction. Fifteen hub genes were identified by PPI network using Cytoscape. The 15 hub genes were almost all positively correlated with each other. The expression of PLEK (P<0.001), TLR2 (P<0.05), and TREM1 (P<0.001) were validated in dataset GSE74089 and they had high diagnostic value (AUC>0.8) for ONFH. MALAT1-miR-146b-5p-TLR2, MALAT1-miR-664b-3p-PLEK, NORAD-miR-106b-5p-TLR2, and MSMO1-miR-106b-5p-TLR2 might be potential RNA regulatory pathways in the disease progression of ONFH. PLEK mainly expressed in nucleus, TREM1 in dictyosome, and TLR2 in nucleoplasm and mitochondria.Conclusions: In this study, we found that PLEK, TLR2, and TREM1 might be potential biomarkers in diagnostic and play a vital role in the progression of ONFH.


2019 ◽  
Author(s):  
Jiaran Shi ◽  
Shi Chen ◽  
Bifeng Wu ◽  
Kun Yang ◽  
Xiaosheng Hu

Abstract Background Long noncoding RNA (LncRNA) played a vital role in pathophysiology of cardiovascular diseases. However, its role in the diagnosis of atrial fibrillation (AF) remains unknown. The aim of this study is to identify the diagnostic value of lncRNA GAS5 for AF patients.Methods Four lncRNAs (NEAT1, GAS5, UCA1, and TUG1) were selected as potential biomarkers of AF. The circulating expression of lncRNAs were measured by qRT-PCR. Receiver operating characteristic curve (ROC) and area under the ROC curve (AUC) were applied to assess their diagnostic value for AF.Results In screening trial, LncRNA GAS5 was down-regulated in AF patients, with no significant differences in other three lncRNAs. Then a total of 128 participants were enrolled including 85 AF patients and 43 controls. Circulating levels of GAS5 in AF patients were remarkably reduced compared with controls ( P <0.001). The AUC was 0.858, with 81.2% sensitivity and 86.0% specificity. Further, the downregulation of GAS5 was more significant in persistent rather than paroxysmal AF. Correlation analysis showed that GAS5 was negatively correlated with CHA2DS2-VASc score and several echocardiography indexes.Conclusions Circulating lncRNA GAS5 is a potential biomarker for AF diagnosis and may prognose AF progression and stroke risk.


Author(s):  
Usharani B.

Essential oils are extracted from diverse plants and used in medicinal field for diverse conditions. The presence of unique aromatic compounds imparts aroma and medicinal values. Essential oil plays a vital role in pharmaceutical, cosmetics and also acts as rejuvenate. Though there are various plants from which essential oil are extracted, our study focuses on the extraction and comparison of the phytochemicals released from the fresh leaves of Cymbopogon citratus using two different organic solvents; (a). hexane (b) hexane and toluene in the ratio 1:1. Extraction was performed for 16 hours in Soxhlet extractor. The amount of oil obtained was weighed in both extractions and subjected to GC MS for phytochemical analysis. Results revealed that when the solvents hexane and toluene in the ratio 1:1 was used it gave a better yield of 3% from 5 gram of fresh leaves, while hexane yielded only 1.5%. The GC-MS analysis revealed that the compound released from both extractions are of diverse medicinal values and can be used in aromatherapy as rejuvenate. The compounds nerol (2,6 octadienal, 3,7 dimethyl.Z) and geraniol (2,6 octadienal, 3,7 dimethyl) are the common phytochemicals extracted .Nerol and geraniol are geometric isomers. Geraniol is reported as an efficient anticancer agent with additional properties of analgesic, antinflammatory and antiseptic values. Nerol is used as a fragrance. The compound 1 acetyl 4 hydroxy pyrrolidine 2 one is extracted when hexane and toluene were used for extraction in the ratio 1:1. It is reported to be anti-rheumatic and effective in the treatment of hips and joints. Hence it can be concluded that hexane and toluene in the ratio 1:1 can be used for extraction of oil considering its medicinal values and the increased % of extraction rather than using hexane alone.


Author(s):  
◽  
◽  

Liver plays a vital role in the human body that performs several crucial life functions. A number of liver diseases exist and it is a challenging task to diagnose the liver disease at its early stage. In recent years, several data mining techniques have been used in medical field for prediction but there can be further improvements for quick and accurate diagnose of liver disease. In this paper, a variety of Classifiers have been experimented on Indian liver disease patients dataset which is publicly available on Kaggle. Attribute subset selection is performed to identify significant attributes and the resulting dataset is named as Selected Attributes Dataset (SAD). SAD provides more accuracy in less computation time using Random forest classification algorithm and improved system including these parameters i.e., the efficiency of the system can be increased, early decision making, less time and space required. This research work will provide help to predict liver disease with less amount of data, i.e., number of attributes.


2019 ◽  
Vol 2019 ◽  
pp. 1-13
Author(s):  
Chung Pin Lim ◽  
Mun Fei Yam ◽  
Mohd. Zaini Asmawi ◽  
Voon Kin Chin ◽  
Nurul Hayah Khairuddin ◽  
...  

Medicinal plants have been considered as promising sources of drugs in treating various cancers. Crinum amabile (C. amabile), a plant species from the Amaryllidaceae family, is claimed to be a potential source for cancer chemotherapeutic compounds. Here, we aimed to investigate the potential of C. amabile as an anticancer agent. Dried leaves of C. amabile were serially extracted and our findings showed that chloroform extract (CE) was shown to exhibit cytotoxic effect against all cancer cell lines used. This active extract was further fractionated in which F5 fraction was shown to possess the highest cytotoxicity among all fractions. F5 fraction was then tested in-depth through Annexin V/FITC apoptosis and DNA fragmentation assays to determine its apoptotic effect on MCF-7 cells. Results revealed that F5 fraction only showed induction of cell apoptosis starting at 72-hour treatment while DNA fragmentation was not detected at any of the concentrations and treatment periods tested. Meanwhile, cell proliferation assay revealed that F5 fraction was able to inhibit normal cell proliferation as well as VEGF-induced cell proliferation of normal endothelial cell (HUVECs). In conclusion, F5 fraction from C. amabile leaf CE was able to exhibit cytostatic effect through antiproliferation activity rather than induction of cell apoptosis and therefore has the potential to be further investigated as an anticancer agent.


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