scholarly journals Modulating the Chemical and Biological Properties of Cancer Stem Cell-Potent Copper(II)-Nonsteroidal Anti-Inflammatory Drug Complexes

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1677 ◽  
Author(s):  
Shin ◽  
Eskandari ◽  
Suntharalingam
Keyword(s):  
Three Dimensional ◽  
Biological Properties ◽  
Culture Studies ◽  
Apoptosis Pathway ◽  
Cytotoxicity Studies ◽  
Ic50 Value ◽  
Low Toxicity ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Micromolar Range

Copper(II) complexes bearing nonsteroidal anti-inflammatory drugs (NSAIDs) are known to potently kill cancer stem cells (CSCs), a subpopulation of tumour cells with high metastatic and relapse fidelity. One of the major disadvantages associated to these copper(II) complexes is their instability in the presence of strong cellular reductants (such as ascorbic acid). Here we present a biologically stable copper(II)-NSAID complex containing a bathocuproinedisulfonic acid disodium ligand and two indomethacin moieties, Cu(bathocuproinedisulfonic acid disodium)(indomethacin)2, 2. The copper(II) complex, 2 kills bulk breast cancer cells and breast CSC equally (in the sub-micromolar range) and displays very low toxicity against non-tumorigenic breast and kidney cells (IC50 value > 100 µM). Three-dimensional cell culture studies show that 2 can significantly reduce the number and size of breast CSC mammospheres formed (from single suspensions) to a similar level as salinomycin (an established anti-breast CSC agent). The copper(II) complex, 2 is taken up reasonably by breast CSCs and localises largely in the cytoplasm (>90%). Cytotoxicity studies in the presence of specific inhibitors suggest that 2 induces CSC death via a reactive oxygen species (ROS) and cyclooxygenase isoenzyme-2 (COX-2) dependent apoptosis pathway.

An Ultrasensitive Electrochemical Sensor for the Detection of Acetaminophen via a Three-Dimensional Hierarchical Nanoporous Gold Wire Electrode

The Analyst ◽  
2021 ◽  
Author(s):  
Lanting Qian ◽  
Reem Elmahdy ◽  
Antony Raj Thiruppathi ◽  
Aicheng Chen
Keyword(s):  
Electrochemical Sensor ◽  
Three Dimensional ◽  
Gold Wire ◽  
Nanoporous Gold ◽  
Wire Electrode ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Acetaminophen is one of the most commonly used non-steroidal anti-inflammatory drugs worldwide. However, due to the increasing popularity of this drug, overdosing and the contamination of ambient waterways have emerged...

scholarly journals Therapeutic Applications of Terpenes on Inflammatory Diseases

2021 ◽  
Vol 12 ◽  
Author(s):  
María Luisa Del Prado-Audelo ◽  
Hernán Cortés ◽  
Isaac H. Caballero-Florán ◽  
Maykel González-Torres ◽  
Lidia Escutia-Guadarrama ◽  
...  
Keyword(s):  
Inflammatory Diseases ◽  
Interleukin 1 ◽  
Biological Properties ◽  
Global Perspective ◽  
Necrosis Factor Alpha ◽  
Factor Alpha ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Anticonvulsant Activities ◽  
Necrosis Factor

In the last decades, the search for natural products with biological applications as alternative treatments for several inflammatory diseases has increased. In this respect, terpenes are a family of organic compounds obtained mainly from plants and trees, such as tea, cannabis, thyme, and citrus fruits like lemon or mandarin. These molecules present attractive biological properties such as analgesic and anticonvulsant activities. Furthermore, several studies have demonstrated that certain terpenes could reduce inflammation symptoms by decreasing the release of pro-inflammatory cytokines for example, the nuclear transcription factor-kappa B, interleukin 1, and the tumor necrosis factor-alpha. Thus, due to various anti-inflammatory drugs provoking side effects, the search and analysis of novel therapeutics treatments are attractive. In this review, the analysis of terpenes’ chemical structure and their mechanisms in anti-inflammatory functions are addressed. Additionally, we present a general analysis of recent investigations about their applications as an alternative treatment for inflammatory diseases. Furthermore, we focus on terpenes-based nanoformulations and employed dosages to offer a global perspective of the state-of-the-art.

scholarly journals Cytotoxicity Studies of Lycorine Alkaloids of the Amaryllidaceae

2014 ◽  
Vol 9 (8) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Jerald J. Nair ◽  
Johannes van Staden
Keyword(s):  
Structural Diversity ◽  
Biological Properties ◽  
Cytotoxic Agents ◽  
Plant Family ◽  
Cytotoxic Effects ◽  
Naturally Occurring ◽  
Cytotoxicity Studies ◽  
Privileged Status ◽  
Low Toxicity ◽  
Widespread Interest

The plant family Amaryllidaceae is renowned for its unique alkaloid constituents which possess a significant array of structural diversity. Several of these alkaloids are known for their interesting biological properties, of which galanthamine and pancratistatin have acquired a privileged status due to their relevance in the pharmaceutical arena. In particular, galanthamine represents the first prescription drug emanating from the Amaryllidaceae after its approval by the FDA in 2001 for the treatment of Alzheimer's disease. Following on this commercial success there have been sustained projections for the emergence of an anticancer agent related to pancratistatin due to the potency, selectivity, low toxicity and high tolerability typifying targets of this series of alkaloids. The lycorine series of alkaloids have also garnered widespread interest as cytotoxic agents and were amongst the earliest of the Amaryllidaceae constituents to exhibit such activity. To date over 100 of such naturally-occurring or synthetically-derived alkaloids have been screened for cytotoxic effects against a number of cancer cell lines. This survey examines the cytotoxic properties of lycorine alkaloids, highlights the outcomes of structure-activity relationship orientated studies and affords plausible insights to the mechanistic rationale behind these effects.

scholarly journals Gold Nanoclusters Display Low Immunogenic Effect in Microglia Cells

Nanomaterials ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 1066
Author(s):  
Joanna Sobska ◽  
Magdalena Waszkielewicz ◽  
Anna Podleśny-Drabiniok ◽  
Joanna Olesiak-Banska ◽  
Wojciech Krężel ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Interleukin 1 ◽  
Gold Nanoclusters ◽  
Biological Properties ◽  
The Body ◽  
Great Promise ◽  
Low Toxicity ◽  
Anti Inflammatory

Gold nanoparticles hold a great promise for both clinical and preclinical applications. The major factors impeding such applications are toxicity of new nanomaterials including e.g., pro-apoptotic activities or inflammatory effects, but also their potential to accumulate in the body or inadequate absorption, distribution, metabolism and excretion (ADME) profiles. Since such adverse effects depend on the size, form and coating of nanomaterials, the search for new, less toxic nanomaterials with low tendency to accumulate is highly active domain of research. Here, we describe optical and biological properties of Au18 gold nanoclusters (NCs), small gold nanoparticles composed of 18 atoms of gold and stabilized with glutathione ligands. These nanoclusters may be suitable for in vivo applications owing to their low toxicity and biodistribution profile. Specifically, using lactate dehydrogenase (LDH) test in P19 cell line we found that Au18 NCs display low toxicity in vitro. Importantly, using primary microglial cells we showed that at low concentrations Au18 NCs display anti-inflammatory signaling on evidence of reduced interleukin 1-β (IL1-β) levels and unchanged levels of tumor necrosis factor (TNF-α) or Ym1/2. Such effect was dose dependent as higher concentrations of Au18 NCs induced expression of pro-inflammatory cytokines and suppression of anti-inflammatory cytokine Ym1/2, pointing, thus, to global inflammatory activity. Finally, we also showed that within 3 days Au18 NCs can be completely eliminated from the liver reported as the major target organ for accumulation of gold nanoparticles. These data point to a potential of gold nanoparticles for further biomedical studies.

scholarly journals Synthesis of 1,2,3-triazole derivatives based on propargyl ester of a saturated single-basic carbonic acid and para-azidobenzoic acid

2021 ◽  
Vol 12 (1) ◽  
pp. 13-17
Author(s):  
Ibragimdjan Аbdugafurov Azizovich ◽  
Fazliddin Qirgizov Bakhtiyarovich ◽  
Ilhom Оrtikov Sobirovich
Keyword(s):  
Carbonic Acid ◽  
Effect Of Temperature ◽  
Reaction Yield ◽  
Factors Affecting ◽  
Low Toxicity ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
First Time ◽  
Derivatives Of ◽  
Membered Heterocycle

The development of highly effective and low-toxicity nonsteroidal anti-inflammatory drugs (NSAIDs) is one of the important challenges facing modern pharmacology. To overcome this problem, many studies have been conducted on compounds containing a five-membered heterocycle containing three nitrogen atoms. The pharmacodynamics of these compounds are mainly due to their anti-inflammatory effect. Therefore, it is important to synthesize new derivatives of 1,2,3-triazoles, to determine their structure and to look for substances with anti-inflammatory activity on their basis. For the first time, the corresponding derivatives of 4-(4-(exchangeable)-1H-1,2,3-triazole-1-yl)-benzoic acid were synthesized by cycloaddition of propargyl esters of saturated carboxylic acids and para-azidobenzoic acid in the presence of copper (I) iodide. The structure of the obtained substances was analyzed by IR, 1H NMR, and MS techniques. It is proved that under the action of the catalyst in the reaction, only 1,4-isomers are formed. Factors affecting the course of the reaction were identified. Only one isomer is formed in the reaction of cyclic addition under the action of a catalyst and the effect of temperature, duration of time, and nature of the solvent on the reaction yield was studied.

scholarly journals Efektivitas Suplementasi Glukosamin pada Tatalaksana Osteoartritis

2019 ◽  
Vol 8 (2) ◽  
pp. 59-66
Author(s):  
Shinta Melia Desiana ◽  
Jessica Sindy Sirait
Keyword(s):  
Alternative Therapy ◽  
Degenerative Joint Disease ◽  
Google Scholar ◽  
Joint Disease ◽  
Symptomatic Therapy ◽  
Literature Study ◽  
Pharmacological Management ◽  
Low Toxicity ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Osteoartritis merupakan penyakit sendi degeneratif yang paling umum ditemukan yang mengakibatkan disabilitas, terutama pada lansia. Angka kejadian osteoartritis setiap tahunnya semakin bertambah dikarenakan pertambahan kejadian obesitas serta usia tua sebagai faktor risiko osteoartritis. Penatalaksanaan osteoartritis secara farmakologis hingga saat ini hanya berupa terapi simtomatik yaitu dengan pemberian antinyeri seperti analgesik dan Non-Steroidal Anti-Inflammatory Drugs (NSAID), namun penggunaan obat-obat tersebut dalam jangka panjang akan menimbulkan efek samping, dari yangringan hingga berat. Karena itulah diperlukan terapi alternatif yang efektif untuk tatalaksana osteoartritis. Glukosamin merupakan komponen glikosaminoglikan pada kartilago dan berfungsi untuk mempertahankan fleksibilitas, elastisitas serta pemeliharaan sendi. Hal ini membuat banyak orang yang yakin bahwa glukosamin dapat memberi manfaat sebagai terapi komplementer dalam penatalaksanaan osteoartritis. Metode yang digunakan menggunakan kumpulan sumber pustaka sejumlah 28 artikel dari tahun 2008 hingga 2019, dimana proses pencarian menggunakan Pubmed, Google Scholar, Medline dan Science Direct. Hasil yang didapatkan dari telaah kepustakaan menunjukkan bahwa pemberian suplementasi glukosamin maupun dengan penambahan beberapa senyawa mungkin efektif untuk digunakan dalam penatalaksanaan osteoartritis.   Kata kunci: glukosamin, osteoartritis, tatalaksana   EFFECTIVITY OF GLUCOSAMINE SUPLEMENT IN OSTEOARTHRITIS MANAGEMENT   ABSTRACT Osteoarthritis is the most common degenerative joint disease which can lead to disability, especially in elderly. The number of people affected is increasing every year due to obesity and aging of the population, as the risk factors. To this day, pharmacological management of osteoarthritis has only been symptomatic therapy, including administration of painkillers such as analgesics and Non-Steroidal Anti-Inflammatory Drugs. However, the use of these drugs in long term will cause various adverse effects. Thus, alternative therapy with high efficacy and low toxicity are needed. Glucosamine is a component of glycosaminoglycans in cartilages that serves to maintain strength and elasticity of the joints. This makes many people believe that glucosamine could provide benefits as an additional therapy in managing osteoarthritis. The method uses a collection of research articles as many as 28 articles from 2008 to 2019, where the search process uses the Pubmed, Google Scholar, Medline and Science Direct. The results obtained from the literature study indicate that the administration of glucosamine supplementation and the addition of several compounds might be effective in managing osteoarthritis.   Keywords: glucosamine, osteoarthritis, management

scholarly journals A novel compound isolated from Sclerochloa dura has anti-inflammatory effects

2016 ◽  
Vol 81 (1) ◽  
pp. 1-12 ◽  
Author(s):  
Syed Bukhari ◽  
Astrid Feuerherm ◽  
Hanna Tunset ◽  
Stian Isaksen ◽  
Mari Sæther ◽  
...  
Keyword(s):  
Methanol Extract ◽  
Preparative Hplc ◽  
Enzymatic Conversion ◽  
Effective Inhibitor ◽  
Aerial Parts ◽  
Ic50 Value ◽  
Release Assay ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Pro Inflammatory Cytokines

The activation of PLA2 by means of pro-inflammatory cytokines results in the subsequent release of arachidonic acid (AA) and generates eicosanoids, which further propagate inflammation. By 6the cyclooxygenases (COX1/2) responsible for the enzymatic conversion of AA to eicosanoids, the non-steroidal anti-inflammatory drugs are effective in relieving the pain and discomfort of inflammation. By using AA release assay as a guide for biological and anti-inflammatory activity, novel compound 1-O-(3-O-linolenoyl-6-deoxy-6-sulfo-?-D-glucopyranosyl)-glycerol (1) together with five known compounds isovitexin, byzantionoside B, tricin 4?-O-(erythro-?-guaiacylglyceryl) ether 7-O-?-glucopyranoside, 1-O-feruloyl glycerol and tricin 7-glucoside were isolated from the methanol extract of the aerial parts of Sclerochloa dura using LC techniques (Sephadex LH-20 column chromatography, preparative HPLC and semi-preparative HPLC). All isolated compounds were identified using spectroscopic NMR spectroscopy and MS spectrometry. Novel compound (1) was found to be an effective inhibitor of AA release with an IC50 value of 0.09 ? 0.03 mg mL-1.

Three Dimensional structure and organization of diploid chromosomes by optical section microscopy

1987 ◽  
Vol 45 ◽  
pp. 633-635
Author(s):  
David A. Agard ◽  
Yasushi Hiraoka ◽  
John W. Sedat
Keyword(s):  
Dimensional Space ◽  
Three Dimensional ◽  
Developmental State ◽  
Mitotic Cell ◽  
Biological Properties ◽  
Dimensional Structure ◽  
Specific Gene ◽  
Three Dimensional Structure ◽  
Complementary Techniques ◽  
Dynamic Structures

In an effort to understand the complex relationship between structure and biological function within the nucleus, we have embarked on a program to examine the three-dimensional structure and organization of Drosophila melanogaster embryonic chromosomes. Our overall goal is to determine how DNA and proteins are organized into complex and highly dynamic structures (chromosomes) and how these chromosomes are arranged in three dimensional space within the cell nucleus. Futher, we hope to be able to correlate structual data with such fundamental biological properties as stage in the mitotic cell cycle, developmental state and transcription at specific gene loci.Towards this end, we have been developing methodologies for the three-dimensional analysis of non-crystalline biological specimens using optical and electron microscopy. We feel that the combination of these two complementary techniques allows an unprecedented look at the structural organization of cellular components ranging in size from 100A to 100 microns.

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