Decorporation dilemma: Interplay of prussian blue and potassium iodide in radioactive contamination.

The expansion of the nuclear industry has led to various radioactive effluents, originating from routine operations or catastrophic incidents such as those at Three Mile Island (USA), Chernobyl (Ukraine), and Fukushima (Japan). Research conducted after these events emphasizes Cesium-137 (137Cs) and iodine 131 (131I) as major contributors to harmful airborne dispersion and fallout. These isotopes infiltrate the human body via inhalation, ingestion, or wounds, posing significant health risks. Understanding contamination mechanisms and devising effective countermeasures are crucial in mitigating nuclear incident consequences. We propose that concurrent administration of Pru-Decorp™/Pru-Decorp-MG and potassium iodide (KI) could synergistically reduce the levels of 137Cs and block uptake of 131I, respectively, in nuclear incident scenarios. Pru-Decorp™ capsules contain insoluble ferric hexacyanoferrate(II) and are equivalent to USFDA-approved Radiogardase®-Cs, offering radiation exposure mitigation for Cs and Tl contamination. Pru-Decorp-MG capsules consist of insoluble PB and magnesium hydroxide, serving as a prophylactic measure to reduce the risk of internal Cs and Tl contamination for rescue responders. Pru-Decorp™/Pru-Decorp-MG binds Cs/Tl ions in the gastrointestinal tract, hindering absorption and promoting excretion, while KI saturates the thyroid gland with stable iodine, decreasing the uptake of radioactive iodine isotopes. Our hypothesis is supported by studies demonstrating the effectiveness of combination therapies, such as calcium alginate, iron(III) ferrocyanide, and KI, in decreasing the retention of radioisotopes in vital organs. To test this hypothesis, we propose a comprehensive research plan, including in vitro studies simulating gastrointestinal conditions, animal studies to evaluate the efficacy of both drugs simultaneously, and safety clinical trials comparing Pru-Decorp™/Pru-Decorp-MG alone, KI alone, and their combination. Expected outcomes include insights into the synergistic effects of Pru-Decorp™/Pru-Decorp-MG and KI, guiding the development of optimized treatment protocols for simultaneous administration during radioactive contamination incidents. This research aims to address significant critical gaps in nuclear incident preparedness by providing evidence-based recommendations for concurrent antidote use in scenarios involving multiple isotope contamination. Ultimately, this will enhance public health and safety during nuclear emergencies.

Light-induced antifungal activity of nanoparticles with an encapsulated porphyrin photosensitizer.

The strong antifungal effect of sulfonated polystyrene nanoparticles (NPs) with an encapsulated tetraphenylporphyrin (TPP) photosensitizer is reported here. TPP is activated by visible light, resulting in the generation of singlet oxygen. Its antifungal action is potentiated in the presence of potassium iodide, yielding I2/I3⁻, another antifungal species. The NPs exhibit no dark toxicity, but a broad spectrum of antifungal photodynamic effects. The efficiency of this rapid killing (on the order of minutes) depends on the concentration of TPP NPs, potassium iodide, yeast species and temperature. A strong antifungal activity of TPP NPs is demonstrated on eleven pathogenic and opportunistic pathogenic yeast species (six Candida species and other yeast species, including melanized Hortaea werneckii). The composition and architecture of yeast cell envelope structures clearly influence the efficacy of photodynamic therapy. Candida krusei is the most sensitive to photodynamic therapy. Despite expectations, melanin does not provide Hortaea cells with marked resistance compared to white yeast species. The kinetics of the interaction of NPs with yeast cells is also described. This study may inspire and promote the fabrication of a new type of antiseptic for various skin injuries in clinical medicine.

A novel tricationic fullerene C60 as broad-spectrum antimicrobial photosensitizer: mechanisms of action and potentiation with potassium iodide.

A novel amphiphilic photosensitizing agent based on a tricationic fullerene C60 (DMC603+) was efficiently synthesized from its non-charged analogue MMC60. These fullerenes presented strong UV absorptions, with a broad range of less intense absorption up to 710 nm. Both compounds showed low fluorescence emission and were able to photosensitize the production of reactive oxygen species. Furthermore, photodecomposition of L-tryptophan sensitized by both fullerenes indicated an involvement of type II pathway. DMC603+ was an effective agent to produce the photodynamic inactivation (PDI) of Staphylococcus aureus, Escherichia coli and Candida albicans. Mechanistic insight indicated that the photodynamic action sensitized by DMC603+ was mainly mediated by both photoprocesses in bacteria, while a greater preponderance of the type II pathway was found in C. albicans. In presence of potassium iodide, a potentiation of PDI was observed due to the formation of reactive iodine species. Therefore, the amphiphilic DMC603+ can be used as an effective potential broad-spectrum antimicrobial photosensitizer.

Bifunctional Therapeutic Application of Low-Frequency Ultrasound Associated with Zinc Phthalocyanine-Loaded Micelles.

PURPOSE: Sonodynamic therapy (SDT) is a new therapeutic modality for the noninvasive cancer treatment based on the association of ultrasound and sonosensitizer drugs. Topical SDT requires the development of delivery systems to properly transport the sonosensitizer, such as zinc phthalocyanine (ZnPc), to the skin. In addition, the delivery system itself can participate in sonodynamic events and influence the therapeutic response. This study aimed to develop ZnPc-loaded micelle to evaluate its potential as a topical delivery system and as a cavitational agent for low-frequency ultrasound (LFU) application with the dual purpose of promoting ZnPc skin penetration and generating reactive oxygen species (ROS) for SDT. METHODS: ZnPc-loaded micelles were developed by the thin-film hydration method and optimized using the Quality by Design approach. Micelles' influence on LFU-induced cavitation activity was measured by potassium iodide dosimeter and aluminum foil pits experiments. In vitro skin penetration of ZnPc was assessed after pretreatment of the skin with LFU and simultaneous LFU treatment using ZnPc-loaded micelles as coupling media followed by 6 h of passive permeation of ZnPc-loaded micelles. The singlet oxygen generation by LFU irradiation of the micelles was evaluated using two different hydrophilic probes. The lipid peroxidation of the skin was estimated using the malondialdehyde assay after skin treatment with simultaneous LFU using ZnPc-loaded micelles. The viability of the B16F10 melanoma cell line was evaluated using resazurin after treatment with different concentrations of ZnPc-loaded micelles irradiated or not with LFU. RESULTS: The micelles increased the solubility of ZnPc and augmented the LFU-induced cavitation activity in two times compared to water. After 6 h ZnPc-loaded micelles skin permeation, simultaneous LFU treatment increased the amount of ZnPc in the dermis by more than 40 times, when compared to non-LFU-mediated treatment, and by almost 5 times, when compared to LFU pretreatment protocol. The LFU irradiation of micelles induced the generation of singlet oxygen, and the lipoperoxidation of the skin treated with the simultaneous LFU was enhanced in three times in comparison to the non-LFU-treated skin. A significant reduction in cell viability following treatment with ZnPc-loaded micelles and LFU was observed compared to blank micelles and non-LFU-treated control groups. CONCLUSION: LFU-irradiated mice can be a potential approach to skin cancer treatment by combining the functions of increasing drug penetration and ROS generation required for SDT.

Characteristics of Dye-Sensitized Solar Cell Assembled from Modified Chitosan-Based Gel Polymer Electrolytes Incorporated with Potassium Iodide.

In the present work, phthaloyl chitosan (PhCh)-based gel polymer electrolytes (GPEs) were prepared using dimethylformamide (DMF) as a solvent, ethyl carbonate (EC) as a co-solvent, and a set of five quaternaries of potassium iodide (KI) as a doping salt, which is a mixed composition of iodine (I2). The prepared GPEs were applied to dye-sensitized solar cells (DSSC) to observe the effectiveness of the electrolyte, using mesoporous TiO2, which was sensitized with N3 dye as the sensitizer. The incorporation of the potassium iodide-based redox couple in a polymer electrolyte is fabricated for dye-sensitized solar cells (DSSCs). The number of compositions was based on the chemical equation, which is 1:1 for KI:I2. The electrical performance of prepared GPE systems have been assessed using electrical impedance spectroscopy (EIS), and dielectric permittivity. The improvement in the ionic conductivity of PhCh-based GPE was observed with the rise of salt concentration, and the maximum ionic conductivity (4.94 × 10-2 S cm-1) was achieved for the 0.0012 mol of KI:I2. The study of dielectric permittivity displays that ions with a high dielectric constant are associated with a high concentration of added ions. Furthermore, the gel polymer electrolyte samples were applied to DSSCs to detect the conversion effectiveness of the electrolytes. For electrolytes containing various content of KI:I2 the highest conversion efficiency (η%) of DSSC obtained was 3.57% with a short circuit current density (Jsc) of 20.33 mA cm-2, open-circuit voltage (Voc) of 0.37 V, fill factor (FF) of 0.47, as well as a conductivity of 2.08 × 10-2 S cm-1.

Dragendorff's reagent: Historical perspectives and current status of a versatile reagent introduced over 150 years ago at the University of Dorpat, Tartu, Estonia.

The well-known Dragendorff's reagent (DR) was introduced by an Estonian-German Professor Johann Georg Noel Dragendorff (1836-1898) in the middle of the 19th century (1866). Dragendorff, who was a full-time professor in pharmacy at the university of Dorpat (Tartu) used his reagent originally for the rapid screening of herbal products to find traces of alkaloids. DR is a solution of potassium bismuth iodide composing of basic bismuth nitrate (Bi(NO3)3), tartaric acid, and potassium iodide (KI), and when contact with alkaloids DR produces an orange or orange red precipitate. In this review article, we make a short historical overview on the biography and scientific research work of Professor Dragendorff at the University of Dorpat. The chemistry, method of preparation, mechanism of action, and practical uses of DR in various disciplines in various European countries including the Baltic countries (Estonia, Latvia, Lithuania), Finland, Ukraine, Moldova, and in Asia (Vietnam), are also discussed. Over several decades, DR and its modifications have found uses in many new applications and disciplines, and a number of commercial DRs are also currently available on the market. Today, DR is used for example in the production of surfactants, where non-ionic surfactant is precipitated in water solution with modified DR (KBiI4+BaCl2+glacial acetic acid). Total six different potassium iodobismuthate (DR) solutions are also presented in the European Pharmacopoeia. In conclusion, DR (after more than 150 years of its invention in Estonia) has still an important role in pharmaceutical and related sciences all over the world.

Efficient photodynamic inactivation of Candida albicans by porphyrin and potassium iodide co-encapsulation in micelles.

Photodynamic inactivation of bacterial and fungal pathogens is a promising alternative to the extensive use of conventional single-target antibiotics and antifungal agents. The combination of photosensitizers and adjuvants can improve the photodynamic inactivation efficiency. In this regard, it has been shown that the use of potassium iodide (KI) as adjuvant increases pathogen killing. Following our interest in this topic, we performed the co-encapsulation of a neutral porphyrin photosensitizer (designated as P1) and KI into micelles and tested the obtained nanoformulations against the human pathogenic fungus Candida albicans. The results of this study showed that the micelles containing P1 and KI displayed a better photodynamic performance towards C. albicans than P1 and KI in solution. It is noteworthy that higher concentrations of KI within the micelles resulted in increased killing of C. albicans. Subcellular localization studies by confocal fluorescence microscopy revealed that P1 was localized in the cell cytoplasm, but not in the nuclei or mitochondria. Overall, our results show that a nanoformulation containing a photosensitizer plus an adjuvant is a promising approach for increasing the efficiency of photodynamic treatment. Actually, the use of this strategy allows a considerable decrease in the amount of both photosensitizer and adjuvant required to achieve pathogen killing.

Preparation of KI/Hydroxyapatite Catalyst from Phosphate Rocks and Its Application for Improvement of Biodiesel Production.

The main aim of this work was to investigate the suitability of a KI/KIO3 impregnated hydroxyapatite (HAP) catalyst derived from natural phosphate rocks for biodiesel production. This study evaluated the effect of impregnation concentrations (1-6% w/w) on the catalyst performance in biodiesel production. The biodiesel was produced from waste cooking oil (WCO) under simultaneous esterification-transesterification reactions at 60 °C for 6 h. The results showed that the biodiesel yield increased by increasing impregnation concentration and the maximum yield (91.787%) was achieved at an impregnation concentration of 5% w/w. The KI/HAP catalyst showed better performance (91.78% biodiesel yield, 59.1% FAME yield and surface area of 13.513 m2/g) as compared to the KIO3/HAP catalyst (90.07% biodiesel yield, 55.0% FAME yield and surface area of 10.651 m2/g).

The concept of foam as a drug carrier for intraperitoneal chemotherapy, feasibility, cytotoxicity and characteristics.

For decades, intraperitoneal chemotherapy (IPC) was delivered into the abdominal cavity as a liquid solution. This preliminary study aims to evaluate foam as a potential new drug carrier for IPC delivery. Foam-based intraperitoneal chemotherapy (FBIC) was produced with taurolidine, hydrogen peroxide, human serum, potassium iodide and doxorubicin/ oxaliplatin for both ex vivo and in vitro experiments. Analysis of FBIC efficacy included evaluation of cytotoxicity, tissue penetration, foam stability, temperature changes and total foam volume per time evaluation. FBIC showed penetration rates of about 275 ± 87 µm and higher cytotoxicity compared to controls and to conventional liquid IPC (p < 0.005). The volume of the generated foam was approximately 50-times higher than the initial liquid solution and temporarily stable. Foam core temperature was measured and increased to 47 °C after 9 min. Foam ingredients (total protein content) were evenly distributed within different locations. Our preliminary results are quite encouraging and indicate that FBIC is a feasible approach. However, in order to discuss a possible superior effect over conventional liquid or aerosolized chemo applications, further studies are required to investigate pharmacologic, pharmacodynamic and physical properties of FBIC.

Multi-spectroscopic, voltammetric and molecular docking studies on binding of anti-diabetic drug rosigiltazone with DNA.

The binding of an anti-diabetic drug rosiglitazone (RG) with calf-thymus DNA (CT-DNA) in physiological buffer (pH 7.4) has been investigated using various spectral techniques such as UV-Vis, fluorescence, 1H NMR and circular dichroism (CD) coupled with viscosity measurement and molecular docking studies. The binding of RG with CT-DNA results in small hypochromism without any change in absorption maximum and fluorescence quenching with hardly any shifts in emission maximum suggesting groove binding mode of interaction. The binding constant is found to be 4.2 × 102 M-1 at 298 K. Thermodynamic analysis reveal that the binding is spontaneous and H-bonding and van der Waals forces play predominant role in the binding of RG with CT-DNA. Competitive interaction between RG and ethidium bromide with CT-DNA, viscosity measurements, KI quenching, 1H NMR and CD studies substantiate the prosed mode of binding. Voltammetric investigations suggest that the electro-reduction of RG is an adsorption controlled process and shift of reduction peak to more negative potential, with a binding constant of 3.4 × 103 M-1, validates the groove binding mode of interaction between RG and CT-DNA. Molecular docking reveals that RG binds in the minor groove of DNA and the dominating interaction forces are H-bonding and hydrophobic interactions.

Iodine/potassium iodide catalyst for the synthesis of trifluoromethylated quinazolines via intramolecular cyclization of 2,2,2-trifluoro-N-benzyl-N'-arylacetimidamides.

An efficient and simple protocol for the synthesis of trifluoromethylated quinazolines has been described by I2-/KI-promoted oxidative C(sp3)-C(sp2) bond under the optimal oxidative cyclization reaction conditions. The required 2,2,2-trifluoro-N-benzyl-N'-arylacetimidamides are readily prepared from the corresponding acetimidoyl chlorides and benzylamines under a nucleophilic substitution reaction in the form of in situ. The merits of this protocol are the use of inexpensive molecular iodine, metal-free oxidative coupling and good to excellent yields.

Potassium Stimulation of IAA Transport Mediated by the Arabidopsis Importer AUX1 Investigated in a Heterologous Yeast System.

Auxin regulates diverse processes involved in plant growth and development. AUX1 is the first identified and most widely investigated auxin importer, and plays an important role in root gravitropism and the development of lateral root and root hair. However, the regulation of auxin transport by AUX1 is still not well understood. In this study, we examined the effect of metal ions on AUX1 transport function and found that the activity could be specifically stimulated four times by K+. Further experiments revealed the preference of KF on the enhancement of transport activity of AUX1 over KCl, KBr, and KI. In addition, the interaction between K+ and AUX1 confers AUX1 more resistant to thermal stress but more vulnerable to proteolysis. Conventional chemical modification indicated that the extracellular acidic amino acids of AUX1 play a key role in the K+ stimulation. Site-specific mutagenesis showed that the replacement of Asp166, Asp293, and Asp312 of AUX1 to alanine deteriorated the K+-stimulated auxin transport. By contrast, when these residues were mutated to glutamate, lysine, or asparagine, only the D312E variant restored the IAA transport activity to the wild-type level. It is thus convinced that D312 is presumably the most promising residue for the K+ stimulation on AUX1.

Oxidation of cystatin imparted by riboflavin generated free radicals: Spectral analysis.

Thiol Protease inhibitors (cystatins) are endogenous natural inhibitors of cysteine proteases. They are present in all mammalians cells and body fluids. Cystatin are allocated into three major families. Family -I stefins, family -II cystatins and family -III kininogens, according to their amino acid sequence, molecular weight, carbohydrate content and disulphide bonds. It has been investigated that thiol proteases (cathepsin) and their endogenous inhibitor, cystatins have been closely associated with diseases like Alzheimer's, Prions, neurodegenerative diseases, cancer and diabetes. Photodynamic effect of various sensitizers' have long been applied to delineate structural and functional properties of biologically active proteins. Flavins are well known to photo oxidize amino acids which effects conformation of proteins. Riboflavin (Vit B2) with a recommended daily requirement of approximately 2-3 mg is a yellow pigment, It is widely distributed in human tissues and blood, in both free and conjugated forms. In the present Study it has been shown that cystatin purified from buffalo brain (BC) is susceptible to reactive oxygen species generated by photo activation of riboflavin. It was observed that Photo activated riboflavin leads to inactivation of BC. Major Loss of tryptophan intensity was observed in the presence of purified thiol protease inhibitor upon incubation with 50 µM of riboflavin. In order to inspect the type of reactive oxygen species involved in inactivation of the inhibitor, different scavenger's were used namely glucose, potassium Iodide, sodium azide, manitol, thiourea, sodium benzoate, curcumin, quercetin, ascorbic acid and uric acid. It was found that Glucose, Potassium Iodide and sodium azide, have preventive effect on photo inactivation of the purified cystatin whilst other scavengers illustrated diminutive defensive effect.

Comparison of two functionalized fullerenes for antimicrobial photodynamic inactivation: Potentiation by potassium iodide and photochemical mechanisms.

A new fullerene (BB4-PPBA) functionalized with a tertiary amine and carboxylic acid was prepared and compared with BB4 (cationic quaternary group) for antimicrobial photodynamic inactivation (aPDI). BB4 was highly active against Gram-positive methicillin resistant Staphylococcus aureus (MRSA) and BB4-PPBA was moderately active when activated by blue light. Neither compound showed much activity against Gram-negative Escherichia coli or fungus Candida albicans. Therefore, we examined potentiation by addition of potassium iodide. Both compounds were highly potentiated by KI (1-6 extra logs of killing). BB4-PPBA was potentiated more than BB4 against MRSA and E. coli, while for C. albicans the reverse was the case. Addition of azide potentiated aPDI mediated by BB4 against MRSA, but abolished the potentiation caused by KI with both compounds. The killing ability after light decayed after 24 h in the case of BB4, implying a contribution from hypoiodite as well as free iodine. Tyrosine was readily iodinated with BB4-PPBA plus KI, but less so with BB4. We conclude that the photochemical mechanisms of these two fullerenes are different. BB4-PPBA is more Type 2 (singlet oxygen) while BB4 is more Type 1 (electron transfer). There is also a possibility of direct bacterial killing by electron transfer, but this will require more study to prove.

Antimicrobial photodynamic therapy mediated by methylene blue and potassium iodide to treat urinary tract infection in a female rat model.

Drug-resistant urinary tract infections (UTIs) are difficult and sometimes impossible to treat. Many UTIs are caused by uropathogenic Escherichia coli (UPEC). We developed an intact rat model of UTI, by catheterizing female rats and introducing a bioluminescent UPEC strain into the female rat bladder which lasted for up to six days. We recently showed that antimicrobial photodynamic inactivation (aPDI) of a bacterial infection mediated by the well-known phenothiazinium salt, methylene blue (MB) could be strongly potentiated by addition of the non-toxic salt potassium iodide (KI). In the intact rat model we introduced MB into the bladder by catheter, followed by KI solution and delivered intravesicular illumination with a diffusing fiber connected to a 1 W 660 nm laser. Bioluminescent imaging of the bacterial burden was carried out during the procedure and for 6 days afterwards. Light-dose dependent loss of bioluminescence was observed with the combination of MB followed by KI, but recurrence of infection was seen the next day in some cases. aPDT with MB + KI gave a significantly shorter duration of infection compared to untreated controls. aPDT with MB alone was the least effective. No signs of aPDT damage to the bladder lining were detected. This procedure to treat urinary tract infections without antibiotics by using already approved pharmaceutical substances (MB and KI) may have clinical applicability, either initially as a stand-alone therapy, or as an adjunct to antibiotic therapy by a rapid and substantial reduction of the bacterial burden.

Binding studies of guggulsterone-E to calf thymus DNA by multi-spectroscopic, calorimetric and molecular docking studies.

Guggulsterone, a sterol found in plants is used as an ayurvedic medicine for many diseases such as obesity, internal tumors, ulcers etc. E and Z are two isoforms of guggulsterone, wherein guggulsterone-E (GUGE) has also been shown to have anticancer potential. Most of the anticancer drugs target nucleic acids. Therefore, we studied the mode of interaction between ctDNA and GUGE using UV-Vis, fluorescence and CD spectroscopy, isothermal calorimetry along with molecular docking studies. Hoechst 3325, ethidium bromide and rhodamine-B displacement experiments confirms that GUGE binds in the minor groove of DNA. ITC results further suggest these interactions to be feasible and spontaneous with hydrogen bond formation and van der waals interactions. Lastly, molecular docking also suggests GUGE to be a minor groove binder interacting through a single hydrogen bond formation between OH group of GUGE and nitrogen (N3) of adenosine (A6).

Chitosan: A macromolecule as green corrosion inhibitor for mild steel in sulfamic acid useful for sugar industry.

The present investigation aims at investigation of low cost nontoxic carbohydrate biopolymer chitosan as corrosion inhibitor alone and in combination with KI for mild steel in 1M sulfamic acid medium using gravimetric, electrochemical and surface analysis techniques. It is found that chitosan alone exhibits inhibition efficiency of 73.8% at 200ppm concentration. However, in combination with KI (5ppm), it gave more than 90% inhibition efficiency. The significant increase in the inhibition performance of chitosan has been explained by the synergistic mechanism. The results of Potentiodynamic polarization study shows that chitosan and its blend with KI decreases both anodic and cathodic reactions occurring at mild steel surface in 1M sulfamic acid medium by blocking active sites of the metal and acts as mixed type inhibitor. EIS study reveals that the polarization resistance increases with increase in the concentration of inhibitors which increases charge transfer resistance across the metal/solution interface. The adsorption of chitosan followed the Langmuir adsorption isotherm. The formation of inhibitor film on metal surface was supported by scanning electron microscopy (SEM) and atomic force microscopy (AFM) surface studies.

Potentiation by potassium iodide reveals that the anionic porphyrin TPPS4 is a surprisingly effective photosensitizer for antimicrobial photodynamic inactivation.

We recently reported that addition of the non-toxic salt, potassium iodide can potentiate antimicrobial photodynamic inactivation of a broad-spectrum of microorganisms, producing many extra logs of killing. If the photosensitizer (PS) can bind to the microbial cells, then delivering light in the presence of KI produces short-lived reactive iodine species, while if the cells are added after light the killing is caused by molecular iodine produced as a result of singlet oxygen-mediated oxidation of iodide. In an attempt to show the importance of PS-bacterial binding, we compared two charged porphyrins, TPPS4 (thought to be anionic and not able to bind to Gram-negative bacteria) and TMPyP4 (considered cationic and well able to bind to bacteria). As expected TPPS4+light did not kill Gram-negative Escherichia coli, but surprisingly when 100mM KI was added, it was highly effective (eradication at 200nM+10J/cm2 of 415nm light). TPPS4 was more effective than TMPyP4 in eradicating the Gram-positive bacteria, methicillin-resistant Staphylococcus aureus and the fungal yeast Candida albicans (regardless of KI). TPPS4 was also highly active against E. coli after a centrifugation step when KI was added, suggesting that the supposedly anionic porphyrin bound to bacteria and Candida. This was confirmed by uptake experiments. We compared the phthalocyanine tetrasulfonate derivative (ClAlPCS4), which did not bind to bacteria or allow KI-mediated killing of E. coli after a spin, suggesting it was truly anionic. We conclude that TPPS4 behaves as if it has some cationic character in the presence of bacteria, which may be related to its delivery from suppliers in the form of a dihydrochloride salt.

Synthesis of novel coumarin nucleus-based DPA drug-like molecular entity: In vitro DNA/Cu(II) binding, DNA cleavage and pro-oxidant mechanism for anticancer action.

Despite substantial research on cancer therapeutics, systemic toxicity and drug-resistance limits the clinical application of many drugs like cisplatin. Therefore, new chemotherapeutic strategies against different malignancies are needed. Targeted cancer therapy is a new paradigm for cancer therapeutics which targets pathways or chemical entities specific to cancer cells than normal ones. Unlike normal cells, cancer cells contain elevated copper which plays an integral role in angiogenesis. Copper is an important metal ion associated with chromatin DNA, particularly with guanine. Thus, targeting copper via copper-specific chelators in cancer cells can serve as an effective anticancer strategy. New pharmacophore di(2-picolyl)amine (DPA)-3(bromoacetyl) coumarin (ligand-L) was synthesized and characterized by IR, ESI-MS, 1H- and 13C-NMR. Binding ability of ligand-L to DNA/Cu(II) was evaluated using a plethora of biophysical techniques which revealed ligand-L-DNA and ligand-L-Cu(II) interaction. Competitive displacement assay and docking confirmed non-intercalative binding mode of ligand-L with ctDNA. Cyclic voltammetry confirmed ligand-L causes quasi reversible Cu(II)/Cu(I) conversion. Further, acute toxicity studies revealed no toxic effects of ligand-L on mice. To evaluate the chemotherapeutic potential and anticancer mechanism of ligand-L, DNA damage via pBR322 cleavage assay and reactive oxygen species (ROS) generation were studied. Results demonstrate that ligand-L causes DNA cleavage involving ROS generation in the presence of Cu(II). In conclusion, ligand-L causes redox cycling of Cu(II) to generate ROS which leads to oxidative DNA damage and pro-oxidant cancer cell death. These findings will establish ligand-L as a lead molecule to synthesize new molecules with better copper chelating and pro-oxidant properties against different malignancies.

Field-effect transition sensor for KI detection based on self-assembled calixtube monolayers.

A series of novel calixarene-based tubes comprising different numbers of silatrane anchoring groups was synthesized. For the first time, a self-assembled monolayer (SAM) derived from calixtubes was formed on a SiO2 surface. The formation of the SAM was confirmed by X-ray photoelectron spectroscopy, scanning electron microscopy-energy dispersive X-ray analysis, and contact angle measurements. Modification of the sensitive surface of a conventional ion-selective field effect transistor (ISFET) with the afforded SAM resulted in the production of a KI-sensitive sensor. This sensor selectively determined KI compare to different alkali metal iodides: NaI, RbI, CsI; also investigation of different potassium salts (acetate, iodide, nitrate, chloride, dihydrophosphate, perchlorate) showed the highest response to KI. This sensor was successfully employed to determine the presence of KI in artificial saliva with a limit of detection of ~3 × 10-8 М. In addition, it was found that the detection limit of the sensor could be increased by combining the sensor with a microfluidic system. Due to the obtained sensor sensitivity and its ability to detect KI in artificial saliva, we could conclude that this sensor shows great potential for application in the determination of KI in different media, such as the human body and in biological liquids, such as saliva or urine.