Current Advances in Chemistry and Biochemistry Vol. 5

2,9-diacetyl-7,14-diamino-5,5a,6a,7,12,12a-hexahydro-[1,2]thiazino[4',5':5,6]pyrido[2,3-g][1,2]thiazino[5,4-b]quinoline-1,6,8,13(2H,4H,9H,11H)-tetraone(2) was prepared by treatment of ,14-diamino-5,5a,12,12a-tetrahydro [1,2]thiazino[4',5':5,6]pyrido[2,3-g][1,2] thiazino[5,4-b]quinoline-1,6,8,13(2H,4H,9H,11H)-tetraone (1) with acetic anhydride and glacial acetic acid,  The reaction of thiazino quinoline (2) with aromatic aldehyde (3a-c) and piperdine catalyst provide arylidene derivatives( 4a-c).

N-acetylpyrazolo- derivatives (5a-c) and N-phenylpyrazolo derivatives (6a-c) were prepared via reaction of arylidene derivatives (4a-c) with an equimolar amount of hydrazine hydrate and/or phenylhydrazine in base catalyst. Also reaction of arylidene derivatives (4a-c) with an equimolar amount of hydroxylamine hydrochloride in ethanol with the presence of sodium hydroxide as a catalyst afford the corresponding isooxazolo pyrimidine derivatives(7a-c).The structure of the synthesized compounds were established by spectroscopic analysis (IR, ¹H-NMR,¹³CNMR and MS) and elemental analysis.

Human papillomavirus (HPV) infects keratinocytes of the skin and mucous membranes, causing a variety of afflictions. Cutaneous and genital warts are the most common HPV-related lesions. Recent studies have highlighted the involvement of oxidative stress as a cofactor in HPV pathogenesis. The relationship between the accumulation of advanced glycation end products (AGEs) and the development of mucocutaneous HPV-related lesions has not been confirmed yet. We have investigated the role of the AGEs-sRAGE axis in patients with HPV-related cutaneous lesions. We have included in the study 41 patients with warts (26 patients with palmoplantar warts and 15 patients with genital warts) and a control group including 28 healthy subjects. We have determined the serum levels of AGEs and circulating soluble receptor for AGEs (sRAGE) by ELISA method. sRAGE levels were lower in patients with palmoplantar warts (p<0.05) and in patients with genital warts (p>0.05) as compared to the control group. We have found higher levels of AGEs in patients with HPV-related cutaneous lesions versus controls, although with no statistical significance. We have obtained a negative correlation between sRAGE and AGEs in patients with palmoplantar warts (r= -0.43, p <0.02) and genital warts (r=-0.47, p>0.05). Our results suggest that the AGEs-sRAGE axis might be involved in the pathogenesis of HPV infection and its modulation could have beneficial therapeutic effects.

Apatite coatings on Titanium substrates have received widespread attention in the biomedical industry as implant devices for hip replacement and similar surgeries. The microstructural and mechanical properties of apatite films tend to play a very important role in enhancing the osteo-bonding capacities of surgical implants. Implants without such coatings are often dissociated from the host bones due to poor initial bone growth on its surface and stress and strain imbalance-related issues. In this investigation, an effort has been made to study the microstructural properties of the apatite grown on the titanium surfaces by non-destructive X-ray diffraction (XRD), Raman spectra, and FESEM. The analysis revealed that bone-like apatite could be grown successfully over titanium substrates used in the biomedical industry as bone implants. The biomimetic approach helps develop a bone-like apatite layer on the implants which would help in superior osteo-bonding.

Nanoparticles have unique, size-dependent properties, which means they are widely used in various branches of industry. The ability to control the properties of nanoparticles makes these nanomaterials very interesting for medicine and pharmacology. The application of nanoparticles in medicine is associated with the design of specific nanostructures, which can be used as novel diagnostic and therapeutic modalities. There are a lot of applications of nanoparticles, e.g., as drug delivery systems, radiosensitizers in radiation or proton therapy, in bioimaging, or as bactericides/fungicides. This paper aims to introduce the characteristics of noble metal-based nanoparticles with particular emphasis on their applications in medicine and related sciences. The development of nanotechnology has opened new doors for more effective treatment and diagnosis of various diseases.

Diabetes is a widely existing disease in patients at risk of pancreatic cancer. It originates from pancreatic endocrine gland whereas pancreatic cancer develops from exocrine glands. Leukocyte cell surface glycans are involved in leukocyte-endothelial cell adherence and retinal endothelial cell death in diabetic retinopathy. A stimulation of hexosamine biosynthesis pathway occurs in diabetes and in pancreatic cancer controlled by oncogene KRAS variant. The present study found a significant elevation of \(\alpha\)1-3 and \(\alpha\)1-4fucosyltransferase activities in pancreatic cancer serum. We examined 5 pancreatic non-tumor and 14 pancreatic tumor tissue specimens for quantitative changes in glycosyltransferse (GTs) activities in pancreatic tumorigenesis by following the incorporation of ¹⁴C or ³H monosaccharide (CPM) from ¹⁴C or ³H monosaccharide donors into specific acceptor catalyzed by 1 mg protein of TritonX-100 solubilized tissue extract. As compared to pancreatic non-tumor tissue specimens with a very low level of GTs activities, pancreatic tumor specimens on average contained 26.0, 42.9, 331.7, 121.0 and 62.8-fold of \(\alpha\)1-2, \(\alpha\)1-3, \(\alpha\)1-4, \(\alpha\)1-6 FTs and FT VI activities respectively. The major sialyltransferase \(\alpha\)2-3 (O)ST and sialomucin glycoproteins increased 95.4 and 4.0-fold; N-glycan \(\alpha\)Man: \(\beta\)1-2GlcNAc-T, chain elongating \(\beta\)Gal: \(\beta\)1-3 GlcNAc-T and N-glycan GalNAc capping \(\beta\)1-3/1-4 GalNAc-T were respectively 95.0, 2.7 and 14.8-fold and the mRNAs of FUT-4, \(\beta\)1-3 and \(\beta\)1-4 GalNAc-Ts were 8.3, 12.0 and 2.4-fold respectively. The increase in activity in neutrophils of retinopathy vs. normal was: \(\beta\)1-2- GlcNAc-T (9.0 fold), \(\beta\)1-3-GlcNAc-T (2.5), \(\alpha\)1-3- FT (3.5), \(\alpha\)1-6-FT (3.3), FTVII (1.9), \(\alpha\)GalNAc: \(\beta\)1-3-GalT (1.4), \(\beta\)GlcNAc: \(\beta\)1-4-Gal-T (2.1), \(\alpha\)2-3-(O)ST (2.1), \(\alpha\)2-3-(N)ST (4.5), \(\alpha\)2-6-(N)ST (8.1). GalNAc replacing Gal in LacNAc terminals results in changes of glycosyltransferase specificities and the modified GalNAc \(\beta\)1-4GlcNAc by FTs and STs bind to lectins such as WGA and SNA. In contrast to a low-level expression-difference of glycosyltransferases between tumor and non-tumor specimens from stomach, prostate and colon, a multifold increase in GTs in pancreatic tumor would indicate their significant role in invasion and intractability of pancreatic cancer. The high-level GT activities in diabetic neutrophils could contribute to the alterations in cell-cell interactions in diabetic retinopathy.

Reduction of 1-aryl-3-(4-aryl-5-arylimino-\(\Delta\)2 -1,2,4-thiadiazol-3-yl) thiourea with ammonical hydrogen sulphide yielded 1,3,5-triazine-2-thiones by intramolecular eliminative cyclisation

This study addresses the individual decontamination of chemical warfare agents (CWA) and other hazardous substances. The individual decontamination applies to contaminated body surfaces, protective clothing and objects immediately after contamination, performed individually or by mutual assistance using prescribed or improvised devices. The article evaluates the importance of individual decontamination, security level for Fire and Rescue Service Units of the Czech Republic (FRS CR) and demonstrates some of the devices. The decontamination efficiency of selected methods (sorbent, glove and sponge, two-chamber foam device and wiping with alcohol) was evaluated for protective clothing and painted steel plate contaminated with O-ethyl-S-(diisopropylaminoethyl)-methylthiophosphonate (VX), sulfur mustard, o-cresol and acrylonitrile. The methods were assessed from an economic point of view and with regard to specific user parameters, such as the decontamination of surfaces or materials with poor accessibility and vertical surfaces, the need for a water rinse as well as toxic waste and its disposal. The improvised Czech fire-fighter System for Individual Decontamination of Fire-fighters was most effective when comparing decontamination methods used by FRS CR. For CWA and other hazardous chemicals, this improvised process had a high decontamination quality of comparable efficiency to commercial goods.

In this present study, Mannich bases 1-[(2,5-Dioxopyrrolidin-1-yl)(phenyl)methyl] urea (USB) and 1-[(2,5-Dioxopyrrolidin-1-yl)(phenyl)methyl] thiourea (TSB) formed by the condensation of succinimide, benzaldehyde and urea/thiourea and its Mn^II, Co^II, Cu^II, Zn^II, Cd^II and Hg^II complexes have been synthesized. Urea and related compounds have long been studied for their biological activities. Analytical, magnetic, electrical conductivity, and spectral studies, as well as elemental analysis, were used to deduce their structures.Geometries of the complexes include octahedral, tetrahedral, and tetragonally distorted octahedral. Magnetic susceptibility and conductance data show that the complexes are monomeric and non-electrolytic. In the presence of metal ions in the ligand system, antimicrobial screening experiments yielded positive results.

The Complex permittivity spectra e* = e'-je" of binary mixtures of Diethylene Glycol Monomethyl Ether with aromatic compounds at different temperatures have been measured in the frequency range of 10 MHz to 20 GHz using the time domain reflectometry technique. Dielectric parameters viz. dielectric constant (e₀), relaxation time (t) were obtained from complex permittivity spectra using nonlinear least squares fit method.  Using these parameters excess permittivity (e₀^E), excess inverse relaxation time (1/t)^E, Bruggeman factor (f_B), Kirkwood correlation factor (g^eff) were determined. On the basis of above parameters, intermolecular interaction and dynamics of molecules at molecular level are predicated. Study of Dielectric relaxation of binary mixture in microwave frequencies has become very important tool to get information regarding intermolecular and intramolecular interaction between mixing components.

The kinetics and dynamic profiles of monomer conversion for various situations of: blue-light only, 2-light (red and UV), and 3-light (red, blue, UV) are presented. Higher oxygen concentration leads to a lower conversion, which could be enhanced by reducing the S-inhibition via a red or blue light pre-irradiation. The system under UV-only leads to a conversion lower than that of blue-only. However, conversion could be improved by the dual-light (blue and UV), and further enhanced by the pre-irradiation of red-light. The two competing factors, N-inhibition and S-inhibition, could be independently and selectively tailored to achieve: (i) high conversion of blue-light (without UV-light), enhanced by red-light pre-irradiation for minimal S-inhibition; and (ii) efficient PC initiated by UV-light produced N-inhibition for reduced confinement thickness and for high print speed. For a dual-wavelength (UV and blue), the UV-light initiated inhibition effect is strongly monomer-dependent due to different C=C bond rate constants and conversion efficacies. Without the UV-light, for a given blue-light intensity, higher initiator concentration and rate constant lead to higher conversion, Conversion of blue-only are much higher than that of UV-only and UV-blue combined. For example, UV-light controlled methacrylate conversion of a glycidyl dimethacrylate resin is formulated with a tertiary amine co-initiator, and butyl nitrite. The system is subject to a continuous exposure of a blue light, but an on-off exposure of a UV-light. Finally, we developed a theoretical new finding for the criterion of a good material/candidate governed by a double ratio of light-intensity and concentration, [I₂₀C₂₀]/ [I₁₀C₁₀].

A new alcohol was isolated from the aqueous methanol extract of the leaves of Cissus javana DC which is widely used in Manipur, India for dissolution and expulsion of kidney stones. In addition, known compounds Stigmasterol, Stigmasterol glucoside, Onocer-7-ene 3\(\alpha\),21\(\beta\)-diol, \(\beta\)-amyrin-[olean12(13)-en-3-one] were also isolated from the same methanol extract. Analysis of trace element contents of the plant leaf reflects its role in the ethno medicinal property of the plant. It was found that the plant leaf have exceptionally high calcium (2960 mg/100 g), magnesium (465 mg/100 g) and iron (520 mg/100 g) content.

Lately, several studies have demonstrated the health benefits associated with natural compounds consumption. Fruit phenolics, lycopene and ascorbic acid, have strong antioxidant, anti-inflammatory, antimugenic and anticarcinogenic activities. In the present study parameters related to fruit quality and climacteric conditions, such as color, moisture, pH, water activity, total phenolic compounds, ascorbic acid and lycopene content were analyzed. Diospyros kaki cv. chocolate fruits were extracted with different solvents, such as methanol, ethanol and water. Total polyphenolics of each extract determined by Folin-Ciocalteu method were found to be higher in methanolic extract and lower in ethanol considering Diospyros fruits with peel. Significant variations were found in the levels of these parameters according to different geographic regions. Results support the importance of Diospyros kaki cv. chocolate fruits, Portuguese cultivar, as a functional food with high antioxidant potential that may have beneficial effects against oxidative human damage.

Is a cell a complex coacervate with distribution coefficients and adsorption coefficients as prime physical–chemical parameters allowing a low-entropy-driven bioenergetics based on coherence, as first proposed by Schrödinger in 1944? Or does a cell have ordinary water in solution with small solutes such as K+, separated by a membrane containing ion-pumps that must constantly oppose passive leaks? The latter viewpoint is known as "membrane-(pump)-theory" (MPT) which is still generally accepted in current physiology and cell biology, but is incompatible with many recent observations on intrinsically disordered proteins, membrane-less organelles, the (quantum) coherence of living systems, and with many crucial old observations. It is not yet generally known that MPT was fully falsified by Ling during the 60^ties and 70^ties and that Ling developed an adsorption and coherence based coacervate model for the living cell, with a whole set of experimentally approved new equations. All basic tenets of his so-called ‘association-induction-hypothesis’ (AIH) are experimentally approved. It is the aim of this review to demonstrate that the AIH is a good guide to interpret many contemporary physiological, physical-chemical and physical data of living cells and sub-cellular systems, particularly those on coherent behaviour, which are incompatible with MPT. It will be shown that we very much need Ling’s new bio-energetics and have to abandon that of MPT.