Degradation and inactivation efficacy of ozone water for antineoplastic drugs in hospital settings

2021 ◽  
pp. 107815522110425
Author(s):  
Ginjiro Kato ◽  
Hidemichi Mitome ◽  
Saki Shigematsu ◽  
Aya Utsunomiya ◽  
Miho Shimasaki ◽  
...  
Keyword(s):  
Ames Test ◽  
Active Sites ◽  
Structural Information ◽  
Human Cancer ◽  
Antineoplastic Drug ◽  
Ozone Treatment ◽  
Resonance Spectroscopy ◽  
Antineoplastic Drugs ◽  
Drug Formulations ◽  
Chemical Structures

Purpose Occupational exposure to antineoplastic drugs in hospital settings is recognized to be hazardous, and as such environmental decontamination including degradation and inactivation of such drugs is recommended. To data, although various agents such as oxidants have been reported to be useful for decontamination, simpler, safer, and more convenient methods are required. In this study, the degradation and inactivation efficacy of ozone water, which has newly been introduced for decontamination of antineoplastic drugs in spills, was investigated for formulations of gemcitabine, irinotecan, and paclitaxel. Methods Antineoplastic formulations (medicinal ingredient: ∼1.5 μmol) were mixed with 50 mL of ozone water (>4 mg/L). The reactions were monitored by high-performance liquid chromatography, and the degradation mixtures were analyzed by 1H nuclear magnetic resonance spectroscopy in order to obtain the structural information of the degradation products. The formulations of gemcitabine and irinotecan and those degradation mixtures were evaluated for their mutagenicity using the Ames test and cytotoxicity against human cancer cells. Results gemcitabine and irinotecan were found to be readily degraded by the ozone treatment, and their active sites were suggested to be degraded. In contrast, paclitaxel was hard to be decomposed, possibly owing to the consumption of ozone by the polyoxyethylene castor oil added as a pharmaceutical additive of the formulation. No significant mutagenic changes of Salmonella typhimurium strains used for the Ames test were observed for the samples within the concentration ranges examined. The ozone treatment showed obvious increases in cell viability for gemcitabine formulation, and mild increases for irinotecan formulation. Conclusions Ozone water was shown to be effective as a decomposition agent for the antineoplastic drug formulations examined, although the efficacy depends on the chemical structures of the drugs and the pharmaceutical additives. It was also suggested that ozone treatment has a tendency to decrease the toxicity of the antineoplastic drug formulations. As such, further studies are required in order to clarify the effects and application limitations of ozone water.

Pharmacological Uses of the Plants Belonging to the Genus Commiphora

2020 ◽  
Vol 18 ◽  
Author(s):  
Subbiah Latha ◽  
Palanisamy Selvamani ◽  
Thangavelu Prabha
Keyword(s):  
Secondary Metabolites ◽  
Plant Species ◽  
Dna Cleavage ◽  
Structural Information ◽  
Chemical Constituents ◽  
Future Research ◽  
Pharmacological Properties ◽  
Chemical Structures ◽  
Indigenous Uses ◽  
Available Information

: Natural products have a unique place in the healthcare industry. The genus Commiphora emerged as a potential medicinal with huge benefits as evidenced through its use in various traditional and modern systems of medicine. Therefore, we aimed to prepare a concise review on the pharmacological activities and the indigenous uses of various plant species belonging to the genus Commiphora along with the structural information of various active botanical ingredients present in these plants based on the published literatures and scientific reports. To collect the various published literatures on Commiphora in various journals; to study and classify the available information on the pharmacological uses and chemical constituents; and to present the gathered information as a precise review to serve as a potential reference for future research. Pharmacological and phytochemical data on Commiphora plant species were collected from various journals, books, reference materials, websites including scientific databases, etc for compilation. This review article describes the various pharmacological properties of plants of Commiphora species viz., Anti-arthritic and anti-inflammatory, Anti-atherogenic, Antibacterial, Anti-coagulant, Anti-dicrocoeliasis, Anti-epileptic, Anti-fascioliasis, Anti-fungal, Anti-heterophyidiasis, Anti-hyper cholesterolemic, Anti-hyperlipidemic, Anti-hypothyroidism, Anti-obesity, Anti-osteoarthritic, Anti-osteoclastogenesis, Anti-oxidant, Anti-parasitic, Anti-pyretic, Anti-schistosomiasis, Anti-septic, Anti-thrombotic, Anti-ulcer, Cardioprotective, COX enzyme inhibitory, Cytotoxic /Anti-carcinogenic/Anti-cancer, DNA cleavage, Hypotensive, Inhibits lipid peroxidation, Inhibits NO and NO synthase production, Insecticidal, Local anesthetic, Molluscicidal, Smooth muscle relaxant, Tick repellent activities along with toxicity studies. Furthermore, the review also included various secondary metabolites isolated from various species of Commiphora genus along with their chemical structures serve as a ready resource for researchers. We conclude that the plant species belonging to the genus Commiphora possesses abundant pharmacological properties with a huge treasure of diverse secondary metabolites within themselves. This review indicates the necessity of further in-depth research, pre-clinical and clinical studies with Commiphora genus which may help to detect the unidentified potential of the Commiphora plant species.

Antioxidant, antimicrobial, and molecular docking studies of novel chalcones and Schiff bases bearing 1, 4-naphthoquinone moiety

2021 ◽  
Vol 19 ◽  
Author(s):  
Nadia Ali Ahmed Elkanzi ◽  
Hajer Hrichi ◽  
Rania B. Bakr
Keyword(s):  
Molecular Docking ◽  
Schiff Bases ◽  
Active Sites ◽  
Radical Scavenging ◽  
Docking Studies ◽  
Antimicrobial Compounds ◽  
Molecular Docking Studies ◽  
Fungal Strains ◽  
Chemical Structures

Background: The 1,4-naphthoquinone ring has attracted prominent interest in the field of medicinal chemistry due to its potent pharmacological activity as antioxidant, antibacterial, antifungal, and anticancer. Objective: Herein, a series of new Schiff bases (4-6) and chalcones (8a-c & 9a-d) bearing 1,4-naphthoquinone moiety were synthesized in good yields and were subjected to in-vitro antimicrobial, antioxidant, and molecular docking testing. Methods: A facile protocol has been described in this study for the synthesis of new derivatives (4-7, 8a-c, and 9a-d) bearing 1,4-naphthoquinone moiety. The chemical structures of all the synthesized compounds were identified by 1H-NMR, 13C-NMR, MS, and elemental analyses. Moreover, these derivatives were assessed for their in-vitro antimicrobial activity against gram-positive, gram-negative bacteria, and fungal strains. Further studies were conducted to test their antioxidant activity using DPPH (2,2-diphenyl-1-picrylhydrazyl) scavenging assay. Molecular docking studies were realized to identify the most likely interactions of the novel compounds within the protein receptor. Results: The antimicrobial results showed that most of the compounds displayed good efficacy against both bacterial and fungal strains. The antioxidant study revealed that compounds 9d, 9a, 9b, 8c, and 6 exhibited the highest radical scavenging activity. Docking studies of the most active antimicrobial compounds within GLN- 6-P, recorded good scores with several binding interactions with the active sites. Conclusion: Based on the obtained results, it was found that compounds 8b, 9b, and 9c displayed the highest activity against both bacterial and fungal strains. The obtained findings from the DPPH radical scavenging method revealed that compounds 9d and 9a exhibited the strongest scavenging potential. The molecular docking studies proved that the most active antimicrobial compounds 8b, 9b and 9c displayed the highest energy binding scores within the glucosamine-6-phosphate synthase (GlcN-6-P) active site.

scholarly journals Natalenamides A–C, Cyclic Tripeptides from the Termite-Associated Actinomadura sp. RB99

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 3003 ◽  
Author(s):  
Seoung Rak Lee ◽  
Dahae Lee ◽  
Jae Sik Yu ◽  
René Benndorf ◽  
Sullim Lee ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Cyclic Peptides ◽  
Culture Broth ◽  
Resonance Spectroscopy ◽  
Ionization Mass ◽  
Inhibitory Effects ◽  
Associated Bacteria ◽  
Chemical Structures ◽  
New Compounds ◽  
Powerful Strategy

In recent years, investigations into the biochemistry of insect-associated bacteria have increased. When combined with analytical dereplication processes, these studies provide a powerful strategy to identify structurally and/or biologically novel compounds. Non-ribosomally synthesized cyclic peptides have a broad bioactivity spectrum with high medicinal potential. Here, we report the discovery of three new cyclic tripeptides: natalenamides A–C (compounds 1–3). These compounds were identified from the culture broth of the fungus-growing termite-associated Actinomadura sp. RB99 using a liquid chromatography (LC)/ultraviolet (UV)/mass spectrometry (MS)-based dereplication method. Chemical structures of the new compounds (1–3) were established by analysis of comprehensive spectroscopic methods, including one-dimensional (1H and 13C) and two-dimensional (1H-1H-COSY, HSQC, HMBC) nuclear magnetic resonance spectroscopy (NMR), together with high-resolution electrospray ionization mass spectrometry (HR-ESIMS) data. The absolute configurations of the new compounds were elucidated using Marfey’s analysis. Through several bioactivity tests for the tripeptides, we found that compound 3 exhibited significant inhibitory effects on 3-isobutyl-1-methylxanthine (IBMX)-induced melanin production. The effect of compound 3 was similar to that of kojic acid, a compound extensively used as a cosmetic material with a skin-whitening effect.

scholarly journals SYNTHESIS AND ANTITUMOR ACTIVITY OF NEW MULTIFUNCTIONAL COUMARINS

2020 ◽  
Vol 17 (36) ◽  
pp. 871-883
Author(s):  
Moath Kahtan BASHIR ◽  
Yasser Fakri MUSTAFA ◽  
Mahmood Khudhayer OGLAH
Keyword(s):  
Schiff Base ◽  
Antitumor Activity ◽  
Human Cancer ◽  
Biological Activities ◽  
Cell Viability Assay ◽  
Chemical Structures ◽  
Viability Assay ◽  
Schiff Base Formation ◽  
Mcf 7

Cancer constitutes one of the most severe public health menaces worldwide. It is imperative to synthesize new compounds and explore their antitumor activity to find a potential resolution to this health problem. Synthesis of new scaffolds and evaluating their antitumor activity is a relevant approach for combating cancer development. Coumarins can exhibit diverse biological activities, and one of these is the antitumor activity. This study aimed to synthesize new coumarins by grafting their precursors to the aromatic amines via Schiff base formation and evaluating their introductory antitumor activity. New multifunctional coumarins (MC1-MC9) were prepared by integrating a functionalized coumarin with different toluidine derivatives via a Schiff-base linkage. Spectral characterization inspired by FTIR, 1H- and 13C- NMR spectroscopies has established the chemical structures of the synthesized products. The antitumor activity was explored in vitro versus four dominant human cancer lines, including HeLa, SKG, MCF-7, and AMN3. The outcomes acquired from the cell viability assay inspected by applying MTT dye have revealed that the synthesized multifunctional coumarins, particularly MC3, have a hopeful activity. It can be concluded that a similar trend of activity against the test cell lines was observed for the synthesized coumarins, with the best action being versus MCF-7 and the least one versus AMN3. This study not only affords a new scaffold of a significant antitumor activity but also provides some insights into its structureactivity relationship.

scholarly journals Synthesis and Pharmacological Evaluation of Novel 2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole Derivatives as Promising Anxiolytic and Analgesic Agents

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 6049
Author(s):  
Dmitriy V. Maltsev ◽  
Alexander A. Spasov ◽  
Pavel M. Vassiliev ◽  
Maria O. Skripka ◽  
Mikhail V. Miroshnikov ◽  
...  
Keyword(s):  
In Silico Analysis ◽  
Chloroacetic Acid ◽  
Benzimidazole Derivatives ◽  
Neutral Medium ◽  
Tail Flick ◽  
Resonance Spectroscopy ◽  
Chemical Structures ◽  
Motor Activities ◽  
Allosteric Sites ◽  
Analgesic Agents

A number of novel 2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole derivatives 2 were obtained by alkylation mainly in the 1H-tautomeric form of 2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole or its 8,9-dimethyl-substituted analog 4-chlorobenzyl bromide, 4-chloroacetic acid fluoroanilide, and 4-tert-butylphenacyl bromide in neutral medium. Compounds 3 were cyclized and synthesized earlier with 11-phenacyl-substituted diazepino[1,2-a]benzimidazoles upon heating in conc. HBr. The chemical structures of the compounds were clarified by using the 1H Nuclear Magnetic Resonance Spectroscopy (1H-NMR) technique. Anxiolytic properties were evaluated using the elevated plus maze (EPM) and open field (OF) tests. The analgesic effect of compounds was estimated with the tail flick (TF) and hot plate (HP) methods. Besides, possible the influence of the test compounds on motor activities of the animals was examined by the Grid, Wire, and Rotarod tests. Compounds 2d and 3b were the most active due to their prominent analgesic and anxiolytic potentials, respectively. The results of the performed in silico analysis showed that the high anxiolytic activity of compound 3b is explained by the combination of a pronounced interaction mainly with the benzodiazepine site of the GABAA receptor with a prominent interaction with both the specific and allosteric sites of the 5-HT2A receptor.

Bacterial extracellular polysaccharides

1988 ◽  
Vol 34 (4) ◽  
pp. 415-420 ◽  
Author(s):  
Chris Whitfield
Keyword(s):  
Pathogenic Bacteria ◽  
Structural Information ◽  
Extracellular Polysaccharides ◽  
Natural Environments ◽  
Chemical Structures ◽  
Technological Advances ◽  
Wide Range ◽  
Surface Polysaccharides ◽  
Surface Location ◽  
Commercial Applications

The synthesis of extracellular polysaccharides has been recognized in certain bacterial cultures since the 1880s. It is now apparent that a wide range of bacteria produce these polymers and an equally wide range of chemical structures are possible. Their surface location, together with the range of available monosaccharide combinations, noncarbohydrate substituents, and linkage types, make extracellular polysaccharides excellent agents of diversity. As a result, much effort has been directed towards elucidating their structure in pathogenic bacteria and in enteric organisms in particular. Commercial applications of microbial polysaccharides have now broadened the scope of structural information. Most recently, technological advances in molecular biology have created the possibility of manipulating desired polymer characteristics, and with these advances, our knowledge of the mechanisms of synthesis and regulation of cell surface polysaccharides has improved. Ultimately more information regarding the function of extracellular polysaccharides in natural environments may result.

Preparation and properties of shape-stabilized phase change material cellulose benzoate-g-polyoxyethylene (2) hexadecyl ether with potential for thermal energy storage

2018 ◽  
Vol 89 (8) ◽  
pp. 1512-1521
Author(s):  
Na Han ◽  
Wenxin Zhang ◽  
Xiufang Wang ◽  
Xingxiang Zhang ◽  
Wei Li ◽  
...  
Keyword(s):  
Phase Transition ◽  
Energy Storage ◽  
Phase Change ◽  
Thermal Energy ◽  
Thermal Energy Storage ◽  
Solid Phase ◽  
Resonance Spectroscopy ◽  
Thermal Reliability ◽  
Scanning Calorimetry ◽  
Chemical Structures

It is a worldwide challenge to efficiently use renewable resources to solve the current energy shortage. The existing cellulose-based material is incapable of proper power storage. In this study, a series of cellulose benzoate-g-polyoxyethylene (2) hexadecyl ether (CB-g-E2C16) solid–solid phase change materials were synthesized with cellulose as the skeleton and polyoxyethylene (2) hexadecyl ether (E2C16) as a functional side chain. The skeleton cellulose and benzoyl chloride restrict the free movement of the molecular chains of E2C16 above the phase transition temperature, leading to a solid–solid phase change. Fourier transform infrared spectroscopy and nuclear magnetic resonance spectroscopy were performed to investigate the chemical structures. The thermal energy-storage properties, thermal reliability and thermal stability of the CB-g-E2C16 were investigated by differential scanning calorimetry and thermogravimetry (TG) methods. The analysis results indicated that the E2C16 chains were successfully grafted onto the cellulose benzoate (CB) backbone and the copolymers exhibited typical solid–solid phase transition behavior. The enthalpy and degree of substitution of graft copolymers CB-g-E2C16 could be adjusted by changing the feeding ratio of the raw materials, reaction temperature and post-processing methods of CB. TG analysis results showed that the CB-g-E2C16 copolymers possessed good thermostability and they keep their stability up to 278℃. Compared with pure cellulose, CB-g-E2C16 copolymers could be dissolved in dimethyl sulfoxide and most of them could be dissolved in N, N-dimethylformamide.

scholarly journals New Discorhabdin Alkaloids from the Antarctic Deep-Sea Sponge Latrunculia biformis

Marine Drugs ◽  
2019 ◽  
Vol 17 (8) ◽  
pp. 439 ◽  
Author(s):  
Li ◽  
Peifer ◽  
Janussen ◽  
Tasdemir
Keyword(s):  
Anticancer Activity ◽  
Deep Sea ◽  
Topoisomerase I ◽  
Active Sites ◽  
Binding Potential ◽  
Chemical Structures ◽  
Ic50 Values ◽  
Ft Ir ◽  
The Antarctic

The sponge genus Latrunculia is a prolific source of discorhabdin type pyrroloiminoquinone alkaloids. In the continuation of our research interest into this genus, we studied the Antarctic deep-sea sponge Latrunculia biformis that showed potent in vitro anticancer activity. A targeted isolation process guided by bioactivity and molecular networking-based metabolomics yielded three known discorhabdins, (−)-discorhabdin L (1), (+)-discorhabdin A (2), (+)-discorhabdin Q (3), and three new discorhabdin analogs (−)-2-bromo-discorhabdin D (4), (−)-1-acetyl-discorhabdin L (5), and (+)-1-octacosatrienoyl-discorhabdin L (6) from the MeOH-soluble portion of the organic extract. The chemical structures of 1–6 were elucidated by extensive NMR, HR-ESIMS, FT-IR, [α]D, and ECD (Electronic Circular Dichroism) spectroscopy analyses. Compounds 1, 5, and 6 showed promising anticancer activity with IC50 values of 0.94, 2.71, and 34.0 µM, respectively. Compounds 1–6 and the enantiomer of 1 ((+)-discorhabdin L, 1e) were docked to the active sites of two anticancer targets, topoisomerase I-II and indoleamine 2,3-dioxygenase (IDO1), to reveal, for the first time, the binding potential of discorhabdins to these proteins. Compounds 5 and 6 are the first discorhabdin analogs with an ester function at C-1 and 6 is the first discorhabdin bearing a long-chain fatty acid at this position. This study confirms Latrunculia sponges to be excellent sources of chemically diverse discorhabdin alkaloids.

scholarly journals Analysis of Bio-Based Fatty Esters PCM’s Thermal Properties and Investigation of Trends in Relation to Chemical Structures

2019 ◽  
Vol 9 (2) ◽  
pp. 225 ◽  
Author(s):  
Rebecca Ravotti ◽  
Oliver Fellmann ◽  
Nicolas Lardon ◽  
Ludger Fischer ◽  
Anastasia Stamatiou ◽  
...  
Keyword(s):  
Thermal Properties ◽  
Phase Change ◽  
Energy Demand ◽  
Phase Change Materials ◽  
Arachidic Acid ◽  
Resonance Spectroscopy ◽  
Scanning Calorimetry ◽  
Fatty Esters ◽  
Latent Heat Storage ◽  
Chemical Structures

As global energy demand increases while primary sources and fossil fuels’ availability decrease, research has shifted its focus to thermal energy storage systems as alternative technologies able to cover for the mismatch between demand and supply. Among the different phase change materials available, esters possess particularly favorable properties with reported high enthalpies of fusion, low corrosivity, low toxicity, low supercooling, thermal and chemical stability as well as biodegradability and being derived from renewable feedstock. Despite such advantages, little to no data on the thermal behavior of esters is available due to low commercial availability. This study constitutes a continuation of previous works from the authors on the investigation of fatty esters as novel phase change materials. Here, methyl, pentyl and decyl esters of arachidic acid, and pentyl esters of myristic, palmitic, stearic and behenic acid are synthesized through Fischer esterification with high purities and their properties are studied. The chemical structures and purities are confirmed through Attenuated Total Reflectance Infrared Spectroscopy, Gas Chromatography coupled with Mass Spectroscopy and Nuclear Magnetic Resonance Spectroscopy, while the determination of the thermal properties is performed through Differential Scanning Calorimetry and Thermogravimetric Analysis. In conclusion, some correlations between the melting temperatures and the chemical structures are discovered, and the fatty esters are assessed based on their suitability as phase change materials for latent heat storage applications.

scholarly journals Interactions and Dissociation Constants of Galactomannan Rendered Cellulose Films with Concavalin A by SPR Spectroscopy

Polymers ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 3040
Author(s):  
Pilar Vilaró ◽  
Carina Sampl ◽  
Gundula Teichert ◽  
Werner Schlemmer ◽  
Mathias Hobisch ◽  
...  
Keyword(s):  
Active Sites ◽  
Dissociation Constants ◽  
Resonance Spectroscopy ◽  
Irreversible Adsorption ◽  
Force Microscopy ◽  
Cellulose Films ◽  
The Past ◽  
Physiological Processes ◽  
Atomic Force ◽  
Dissociation Constant Kd

Interactions of biomolecules at interfaces are important for a variety of physiological processes. Among these, interactions of lectins with monosaccharides have been investigated extensively in the past, while polysaccharide-lectin interactions have scarcely been investigated. Here, we explore the adsorption of galactomannans (GM) extracted from Prosopis affinis on cellulose thin films determined by a combination of multi-parameter surface plasmon resonance spectroscopy (MP-SPR) and atomic force microscopy (AFM). The galactomannan adsorbs spontaneously on the cellulose surfaces forming monolayer type coverage (0.60 ± 0.20 mg·m−2). The interaction of a lectin, Concavalin A (ConA), with these GM rendered cellulose surfaces using MP-SPR has been investigated and the dissociation constant KD (2.1 ± 0.8 × 10−8 M) was determined in a range from 3.4 to 27.3 nM. The experiments revealed that the galactose side chains as well as the mannose reducing end of the GM are weakly interacting with the active sites of the lectins, whereas these interactions are potentially amplified by hydrophobic effects between the non-ionic GM and the lectins, thereby leading to an irreversible adsorption.

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