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The Komodo dragon is a unique reptile with an elongated tail that exhibits hitherto unknown adaptations and functions. This tail, composed of 60–86 vertebrae, serves diverse ecological and physiological roles. In juveniles, it is essential for an arboreal lifestyle and balance, while in adults, it functions as a tool for defense and offensive actions. It possesses characteristic haemal arches and a dorsal keel, along with well-developed muscles which enable precise tail control, influencing the Komodo dragon’s maneuverability and directional changes. The tail stores adipose tissue, providing Komodo dragons with the ability to regulate body temperature and independence from other seasonal variations. The tail adipose tissue impacts numerous biochemical processes and may play a crucial role in the animals’ metabolic strategies and reproductive capabilities. Its functions include providing essential mineral compounds for the organism, such as calcium, phosphorus, magnesium, iron, and zinc. Analysing the biochemical composition of tail fat is crucial for understanding the health of Komodo dragons.

The leaves of Ilex paraguariensis (known as Yerba mate), used as a popular beverage, are a very well-recognized plant material with various biological activities, including analeptic (because of caffeine), anti-obesity (phenolics, saponins), antimicrobial, and antiviral (phenolics, saponins). Here, the chemical compositions of the leaves of two European Ilex species (× meserveae and aquifolium) with three varieties each were investigated. The terpenoid, saponin, and polyphenolic fractions were submitted for LC-MS or GC-MS analysis against a standard Mate leaf. In addition, the aroma profiles of all the species were analysed using HS-SPME-Arrow prior to GC-MS analysis. All fractions were subjected to antiviral and cytotoxic assays. We found 86 compounds in all accessions, with limonene, linalool, and p-cymene being predominant. There were minor similarities between the volatile compositions of the European and South American species. We found ursolic and oleanolic acid to be the main compounds in the terpenoid fraction. Mono-caffeoylquinic acids and di-caffeoylquinic acids were the main constituents of the polar fractions. About 180 compounds from the saponin group were tentatively identified, of which 9 and 3 were selected as distinctive markers for I. meserveae and I. aquifolium, respectively. Based on chemical screening, I. aquifolium Silver Queen was chosen as the source of terpenoid and saponin fractions and polyphenol extracts. The most substantial inhibition of cancer cell growth was observed with saponin in the case of the MCF7 (human breast cancer) cell line, while for LoVo and L929 cell lines (human colorectal cancer and reference mouse fibroblasts), it was slightly weaker. These results should be analysed further as a promising chemoprevention of colorectal and gastrointestinal cancers. Saponin and polyphenolic extracts exhibited similar activities against HSV-1 and HAdV-5, with 4-log reduction in virus titres. This study focuses our attention on a field of potential antiviral formulations derived from European holly.

The aim of this study was to determine the content of mercury in impacted third molars from Legnica–Głogów Copper Area residents to emphasize the effects of environmental pollution on the human body. A group of 72 patients with an average age of 27.3 ± 6.9 years participated in the study. Within this study, the research group (Legnica–Głogów Copper Area residents) comprised 51 individuals, while the control group (residents of Wrocław) consisted of 21 participants. A higher number of female individuals participated in the research (55). The amount of mercury present in the samples was determined through atomic absorption spectrometry with the use of a SpectraAA atomic absorption spectrometer and a V2 AA240FS flame attachment that utilized an air–acetylene flame. The accumulation of Hg in the teeth of members of the control group residing in Wrocław was studied, with a focus on identifying the risk factors that contribute to this phenomenon. The final model analyzed the presence of various factors, including thyroid and parathyroid gland diseases, cardiac diseases, and interval-scale Vit. D3 concentration. Among these factors, the presence of cardiac diseases was deemed statistically significant in relation to an increase in Hg concentration in third molars (rate ratio = 2.27, p < 0.0001). The concentration of mercury increased with the age and time of residence in the L-G Copper District.

Since the Komodo dragon has been included on The International Union for Conservation of Nature (IUCN) Red List of Threatened Species, it is crucial to know in detail its biology as there is a limited availability of research material on these animals—mainly those who died in zoos or whose remains were found in the wild. Anatomy is essential for understanding physiology, identification of diseases, adaptations in the environment, and behavior. In this dissection study, the relationship of individual anatomical structures was analyzed, the anatomy of the active and passive movement system of the thoracic limb was described, photographs were taken, and a radiographic examination was conducted. This species has its own differences, even within closely related lizard species. Varanus komodoensis possesses triceps muscles with three heads, and the wrist is extended with additional bones for greater flexibility of the hand. The muscles of the forelimb are analogous to the hind limb; however, they differ in the mass of individual muscles, especially those predisposed to perform the most important antigravity and locomotive functions.

Colorectal cancer is a major global health concern, and the need for effective chemopreventive agents is paramount. This study aimed to evaluate the potential of oils from transgenically modified flax for the prevention of colorectal cancer, in relation to the oil concertation. Flaxseed oils were obtained from traditional (Nike) and genetically modified flax lines (M and B). Cell viability assays were performed on various cancer cell lines, including colon adenocarcinoma cells. Flaxseed oil B exhibited the strongest anti-proliferative properties compared to the reference drugs and other oils. Additionally, M and B oils showed enhanced accumulation of Rhodamine 123 and increased apoptosis in colorectal cancer cells. M oil exhibited the highest levels of p53 protein. Notably, the tested transgenic oils did not induce metastasis and displayed stronger inhibition of COX-1 compared to COX-2. These data indicate the utility of flaxseed oils, especially from the M line, as adjuvants in colorectal cancer treatment, targeting the colon specifically.

Secure and efficient treatment of diverse pain and inflammatory disorders is continually challenging. Although NSAIDs and other painkillers are well-known and commonly available, they are sometimes insufficient and can cause dangerous adverse effects. As yet reported, derivatives of pyrrolo[3,4-d]pyridazinone are potent COX-2 inhibitors with a COX-2/COX-1 selectivity index better than meloxicam. Considering that N-acylhydrazone (NAH) moiety is a privileged structure occurring in many promising drug candidates, we decided to introduce this pharmacophore into new series of pyrrolo[3,4-d]pyridazinone derivatives. The current paper presents the synthesis and in vitro, spectroscopic, and in silico studies evaluating the biological and physicochemical properties of NAH derivatives of pyrrolo[3,4-d]pyridazinone. Novel compounds 5a-c–7a-c were received with high purity and good yields and did not show cytotoxicity in the MTT assay. Their COX-1, COX-2, and 15-LOX inhibitory activities were estimated using enzymatic tests and molecular docking studies. The title N-acylhydrazones appeared to be promising dual COX/LOX inhibitors. Moreover, spectroscopic and computational methods revealed that new compounds form stable complexes with the most abundant plasma proteins–AAG and HSA, but do not destabilize their secondary structure. Additionally, predicted pharmacokinetic and drug-likeness properties of investigated molecules suggest their potentially good membrane permeability and satisfactory bioavailability.

The purpose of this study was to determine tissue concentration of toxic metals, namely Mn, Cr, Ni, Cu, Fe, Cd, Pb, and Zn, in the removed third molars in patients from the Legnica-Głogów copper district. A group of 69 patients with an average age of 27.3 ± 6.9 years was enrolled into the study. There were 16 (23.2%) men and 53 (76.8%) women. Patients were divided into two groups according to the place of residence—residents of the Legnica-Głogów Copper Area (n = 49) and the control group, residents of Wrocław (n = 20). Determination of the Pb, Cd, Cr, Ni, Fe, Mn, Cu, Zn content was performed by atomic absorption spectrometry in an air–acetylene flame using the SpectraAA atomic absorption spectrometer with a V2 AA240FS flame attachment. The content of Fe and Pb in the third molars was higher among residents of the Legnica-Głogów Copper Area (p = 0.016 and p = 0.002, respectively). The significant risk factors that may contribute to the accumulation of toxic metals in teeth were identified. We showed a significant correlation between the level of Cr, Cu, and Zn and age, and between chromium and vitamin D3 concentration in the blood (p < 0.05 for all).

Chemical composition and physical parameters of the implant surface, such as roughness, regulate the cellular response leading to implant bone osseointegration. Possible implant surface modifications include anodization or the plasma electrolytic oxidation (PEO) treatment process that produces a thick and dense oxide coating superior to normal anodic oxidation. Experimental modifications with Plasma Electrolytic Oxidation (PEO) titanium and titanium alloy Ti6Al4V plates and PEO additionally treated with low-pressure oxygen plasma (PEO-S) were used in this study to evaluate their physical and chemical properties. Cytotoxicity of experimental titanium samples as well as cell adhesion to their surface were assessed using normal human dermal fibroblasts (NHDF) or L929 cell line. Moreover, the surface roughness, fractal dimension analysis, and texture analysis were calculated. Samples after surface treatment have substantially improved properties compared to the reference SLA (sandblasted and acid-etched) surface. The surface roughness (Sa) was 0.59–2.38 µm, and none of the tested surfaces had cytotoxic effect on NHDF and L929 cell lines. A greater cell growth of NHDF was observed on the tested PEO and PEO-S samples compared to reference SLA sample titanium.

Protozoa, in both humans and animals, are one of the leading causes of disease. International programmes introduced in many countries have helped reduce the incidence of disease. However, it has recently become increasingly difficult to achieve the goals set for the coming years. One of the main reasons for this, as with other pathogenic organisms, such as bacteria and fungi, is the increasing resistance to current methods of treating and preventing infection. Therefore, new therapies with high efficacy are needed. In the present study, the novel mixtures of essential oils (EOs), clove, garlic, Ceylon cinnamon, and rosemary with organic acids (acetic, propionic, lactic) and metal ions (Cu, Mn, Zn) were tested against five selected model protozoa (Euglena gracilis, Gregarina blattarum, Amoeba proteus, Paramecium caudatum, Pentatrichomonas hominis). The cytotoxicity and potential anticancer activity of the obtained combinations were tested on the human fibroblasts (NHDF) and human cancer cell lines (A549, MCF7, LoVo, HT29). All of the mixtures showed very good antiprotozoal properties. The most efficient were the combination of clove and rosemary essential oils, mixtures of acids, and Mn ions. The LD50 values were in the range of 0.001–0.006% and the LD100 values were 0.002–0.008%. All of the tested mixtures did not show cytotoxicity against normal cells, but did show growth inhibition against cancer cell lines. The most cytotoxic against cancer cells were combinations with cinnamon essential oil. Nevertheless, the proposed combinations containing essential oils, organic acids, and metal ions have high antiprotozoal activity, with low toxicity to healthy human cells.

The characteristics such as microtopography, physical and chemical properties influence the behavior of an implant in a soft tissue. Anodization—as a potent method of titanium alloy surface modification—of the transgingival abutment or healing screw, has achieved some improvement. One of the possible surface treatment method is low-pressure radiofrequency oxygen plasma treatment. The aim of the study was to evaluate the chemical properties and cytocompatibility of the experimental surface. Titanium discs made of grade-23 titanium alloy (Ti-6Al-4V) anodized (A sample) with different voltage parameters (28, 67, 78, and 98 V) were included in the study. Half of the samples regarded as the “S” group were additionally treated with low-pressure radiofrequency oxygen plasma treatment. The surfaces were characterized using scanning electron microscopy, X-ray spectroscopy and Raman spectroscopy, and electrochemically investigated via a corrosion test. Furthermore, two cell lines were used, including the CHO-compatible reference line and a primary human fibroblast line for the MTT assay; direct (contact) cytotoxicity of the materials was tested with the cells, and the growth of fibroblasts on the surfaces of the different materials was tested. The morphology of the “S”-treated samples did not differ from the morphology of only-anodized samples. However, the oxygen concentration on the surface in that group slightly increased by about 1% as a result of post-trial treatment. The highest corrosion resistance was observed for both A-78 V and S-78 V samples. The cytotoxicity assay revealed no changes in cell morphology or vitality. The MTT test proved comparable culture viability among all groups; however, the “S” samples showed statistically significantly higher fibroblast proliferation and adhesion scores compared to the “A” samples. Through the in vitro study, the low-pressure radiofrequency oxygen plasma treatment of the anodized Ti-6Al-4V alloy presented itself as an auspicious option in the field of transgingival element surface modification of implants.

In antiquity, flax was used as a dressing for healing wounds. Currently, work is underway on the genetic modification of flax fibers to improve their properties. Genetic modifications have resulted in an increased content of antioxidants and more favorable mechanical properties. The works published so far have presented independent tests of fibers and dressings after appropriate technological treatments in cell cultures. This study aimed to compare the properties of the fibers and the dressing produced in cell cultures—hamster fibroblasts—V79. The research material was traditional NIKE fibers; genetically modified M, B, and MB fibers; and linen dressings obtained from these fibers. The extract from 48-h incubation of 40 mg of fiber in the culture medium, which was desolved into 10, 20, and 30 mg, was administered to the cell culture. On the other hand, a linen dressing was placed on cells with an area of 0.5 cm2, 1 cm2, 1.5 cm2, and 2 cm2. Cells with fiber or dressing were incubated for 48 h, and then, biological tests were performed, including cell viability (in propidium iodide staining), cell proliferation (in the SRB assay), evaluation of the intracellular free radical level (in the DCF-DA assay), genotoxicity (in the comet assay), assessment of the apoptotic and necrotic cells (in staining anexin-V and iodide propidium), the course of the cell cycle, and the scratch test. The correlation between apoptosis and genotoxicity and the levels of free radicals and genotoxicity were determined for the tested linen fibers and fabrics. The tests presented that the fibers are characterized by the ability to eliminate damaged cells in the elimination phase. However, the obtained fabrics gain different properties during the technological processing of the fibers into linen dressings. Linen fabrics have better regenerative properties for cells than fibers. The linseed dressing made of MB fiber has the most favorable regenerative properties.

This study evaluated in vitro antibacterial, antifungal, anticancer and antioxidant activities of methanolic leaf and root extracts from Solanum nigrum L. and determined its chemical composition. The chemical profile of S. nigrum L. extract was tested using liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS). Disc diffusion and microdilution assays were used for the antibacterial activities. Antifungal activity was measured using the poisoned food technique. In vitro activity on the cell culture model was assessed by MTT assay, viability measurement and by determination of cellular ROS by DCFDA assay. The minimal inhibitory concentrations for extracts from aerial parts ranged from 125 to 500 μg/mL for gram-positive cocci and Pectobacterium strains. The growth inhibition coefficient ranged from 17–56%, depending on the dosage. The antifungal effect of S. nigrum extracts on the tested filamentous fungi depended on the dose. An inhibitory effect of 50–56% on fungi was observed against Alternaria alternata and Chaetomium globosum. The study showed a reduction in cellular vitality of THP1, A549, MCF7 and HeLa cancer lines using both extracts. In addition, there was a decrease in the number of viable cells in cultures incubated with the extract of aerial parts and a reduction in oxygen radicals in the cells. The obtained results indicate the possibility of using S. nigrum extracts from the aerial part as antimicrobial factors. Both extracts show chemopreventive properties by inhibiting the growth of cancer cells and reducing the level of free radicals. Both extracts show chemopreventive properties by inhibiting cancer cell growth and lowering free radical levels. The broad biological activity of the studied extracts can be used in agriculture, veterinary usages and medicine.

Ellipticine is an indole alkaloid with proven antitumor activity against various tumors in vitro and a diverse mechanism of action, which includes topoisomerase II inhibition, intercalation, and cell cycle impact. Olivacine—ellipticine’s isomer—shows similar properties. The objectives of this work were as follows: (a) to find a new path of olivacine synthesis, (b) to study the cytotoxic properties of olivacine and ellipticine in comparison to doxorubicin as well as their impact on the cell cycle, and (c) to investigate the cellular pharmacokinetics of the tested compounds to understand drug resistance in cancer cells better. SRB and MTT assays were used to study the anticancer activity of olivacine and ellipticine in vitro. Both compounds showed a cytotoxic effect on various cell lines, most notably on the doxorubicin-resistant LoVo/DX model, with olivacine’s cytotoxicity approximately three times higher than doxorubicin. Olivacine proved to be less effective against cancer cells and less cytotoxic to normal cells than ellipticine. Olivacine proved to have fluorescent properties. Microscopic observation of cells treated with olivacine showed the difference in sensitivity depending on the cell line, with A549 cells visibly affected by a much lower concentration of olivacine than normal NHDF cells. An increased percentage of cells in G0/G1 was observed after treatment with olivacine and ellipticine, suggesting an impact on cell cycle progression, potentially via higher p53 protein expression, which blocks the transition from G0/G1 to the S phase. Ellipticine induced apoptosis at a concentration as low as 1 μM. It has been proved that the tested compounds (ellipticine and olivacine) undergo lysosomal exocytosis. Reducing exocytosis is possible through the use of compounds that inhibit the activity of the proton pump. Olivacine and ellipticine exhibited diverse cytotoxicity against a panel of cancer cells. Analysis of the lysosomal exocytosis of olivacine and ellipticine shows the need to look for derivatives with comparable anticancer activity but reduced weak base character.

Laser-induced periodic surface structures (LIPSS) are the sub-wavelength periodic nanostructures generated by the femtosecond laser. Implant topography and its nanostructural changes can be important for biomedical applications. In order to compare the surface topography of different implants, appropriate mathematical and physical descriptive methods should be provided. The aim of the study was to evaluate the experimental LIPSS-based—Low Spatial Frequency LIPSS (LSFL) dental implant surfaces. Novel methods of surface analysis, such as Fractal Dimension Analysis and Texture Analysis, were compared to the standard surface roughness evaluation. Secondary, cell viability, and attachment tests were applied in order to evaluate the biological properties of the new titanium surface and to compare their correlation with the physical properties of the new surfaces. A Normal Human Dermal Fibroblast (NHDF) cytotoxicity test did not show an impact on the vitality of the cells. Our study has shown that the laser LIPSS implant surface modifications significantly improved the cell adhesion to the tested surfaces. We observed a strong correlation of adhesion and the growth of cells on the tested surface, with an increase in implant surface roughness with the best results for the moderately rough (2 μm) surfaces. Texture and fractal dimension analyses are promising methods to evaluate dental implants with complex geometry.

To date, chronic inflammation is involved in most main human pathologies such as cancer, and autoimmune, cardiovascular or neurodegenerative disorders. Studies suggest that different prostanoids, especially prostaglandin E2, and their own synthase (cyclooxygenase enzyme-COX) can promote tumor growth by activating signaling pathways which control cell proliferation, migration, apoptosis, and angiogenesis. Non-steroidal anti-inflammatory drugs (NSAIDs) are used, alongside corticosteroids, to treat inflammatory symptoms particularly in all chronic diseases. However, their toxicity from COX inhibition and the suppression of physiologically important prostaglandins limits their use. Therefore, in continuation of our efforts in the development of potent, safe, non-toxic chemopreventive compounds, we report herein the design, synthesis, biological evaluation of new series of Schiff base-type hybrid compounds containing differently substituted N-acyl hydrazone moieties, 1,3,4-oxadiazole ring, and 4,6-dimethylpyridine core. The anti-COX-1/COX-2, antioxidant and anticancer activities were studied. Schiff base 13, containing 2-bromobenzylidene residue inhibited the activity of both isoenzymes, COX-1 and COX-2 at a lower concentration than standard drugs, and its COX-2/COX-1 selectivity ratio was similar to meloxicam. Furthermore, the results of cytotoxicity assay indicated that all of the tested compounds exhibited potent anti-cancer activity against A549, MCF-7, LoVo, and LoVo/Dx cell lines, compared with piroxicam and meloxicam. Moreover, our experimental study was supported by density functional theory (DFT) and molecular docking to describe the binding mode of new structures to cyclooxygenase.

Background: Linen dressings were invented a few years ago but are still being worked on. Methods: The obtained fabrics from the traditional variety of flax (Nike), two transgenic types of flax (M50 and B14) and the combination of these two flax fibers (M50 + B14) were tested in direct contact in cell cultures. Cell viability tests were performed, and the proliferation potential of cells on Balb3T3 and NHEK cell lines was checked using the Sulforhodamine-B (SRB) test. Moreover, the effect of new linen fabrics on apoptosis of THP-1 cells, as well as on the cell cycle of NHEK, HMCEV and THP-1, cells after 24 h of incubation was assessed. Results: All tested linen fabrics did not raise the number of necrotic cells. The tested fabrics caused a statistically significant decrease in the total protein content in skin cancer (except for 0.5 cm of Nike-type fabrics). The smallest cells in the apoptotic phase were in cultures treated with M50 fiber on an area of 0.5 cm. After 48 h of incubation of HEMVEC, NHEK and THP-1 cells with the tested fabrics, the growth of S-phase cells was noticed in all cases. At the same time, the greatest increase was observed with the use of B14 fabric. Necrosis is not statistically significant. Conclusions: All the obtained flax fibers in the form of flax dressings did not lose their wound-healing properties under the influence of the technological process. New dressings made of genetically modified flax are a chance to increase the effectiveness of treatment of difficult healing wounds.

Olivacine and ellipticine are model anticancer drugs acting as topoisomerase II inhibitors. Here, we present investigations performed on four olivacine derivatives in light of their antitumor activity. The aim of this study was to identify the best antitumor compound among the four tested olivacine derivatives. The study was performed using CCRF/CEM and MCF-7 cell lines. Comet assay, polarography, inhibition of topoisomerase II activity, histone acetylation, and molecular docking studies were performed. Each tested compound displayed interaction with DNA and topoisomerase II, but did not cause histone acetylation. Compound 2 (9-methoxy-5,6-dimethyl-1-({[1-hydroxy-2-(hydroxymethyl)butan-2-yl]amino}methyl)-6H-pyrido[4,3-b]carbazole) was found to be the best candidate as an anticancer drug because it had the highest affinity for topoisomerase II and caused the least genotoxic damage in cells.

Huculs (Equus caballus) are an old breed of primitive mountain horses, originating from the Carpathian Mountains. To the best of our knowledge, data concerning the epidemiology of viral infections observed within this breed are sparse. The objective of this study was to estimate the serological status of a semi-isolated, unvaccinated Hucul herd, with respect to both common equine viral infections and horse-infecting arboviruses, the presence of which was previously reported in Poland. Twenty horses of the Hucul breed, living in a remote area in Poland, were studied in 2018 from March to May. Using nasal secretion swabs as a specimen source, isolation attempts were negative regarding ERAV, EHV-1, EAV, and EIV. According to the virus neutralisation method, in the sera obtained from the animals, antibodies against the following viruses were detected: EHV-1 in 12 horses (60%; with titres from 1:8 to 1:64), EIV A/H7N7 in 13 (65%; titres from 1:20 to 1:80), EIV A /H3N8 in 12 (60%; titres from 1:20 to 1:80), USUV in 5 (25%; titres from 1:10 to 1:80), and ERAV in 1 (5%; titre 1:32). Antibodies against EAV, EIAV, and WNV were not present in the tested sera. The detected presence of specific antibodies associated with five out of the eight equine viruses investigated indicates that the Hucul herd, due to its partial separation and lack of specific prophylaxis, could serve as a sentinel animal group for the detection of equine viruses/arboviruses present within the local ecosystem. The detection of common equine viral infections within the herd provides additional epidemiological data concerning the breed.

Since biological applications and toxicity of graphene-based materials are structure dependent, studying their interactions with the biological systems is very timely and important. We studied short-term (1, 24, and 48 h) effects of ultrapure (GO) and Mn2+-contaminated (GOS) graphene oxide on normal human dermal fibroblasts (NHDF) and adenocarcinomic human alveolar basal epithelial cells (A549) using selected oxidative stress markers and cytokines: glutathione reductase (GR) and catalase (CAT) activity, total antioxidative capacity (TAC), and malondialdehyde (MDA) concentration, levels of vascular endothelial growing factor (VEGF), tumor necrosis factor-alpha (TNF-α), platelet-derived growth factor-BB (PDGF-BB), and eotaxin. GOS induced higher levels of oxidative stress, measured with CAT activity, TAC, and MDA concentration than GO in both cell lines when compared to control cells. GR activity decreased in time in NHDF cells but increased in A549 cells. The levels of cytokines were related to the exposure time and graphene oxide type in both analyzed cell lines and their levels comparably increased over time. We observed higher TNF-α levels in NHDF and higher levels of VEGF and eotaxin in the A549 cell line. Both types of cells showed similar susceptibility to GO and GOS. We concluded that the short-time exposure to GOS induced the stronger response of oxidative stress markers without collapsing the antioxidative systems of analysed cells. Increased levels of inflammatory cytokines after GO and GOS exposure were similar both in NHDF and A549 cells.

Numerous studies have confirmed the coexistence of oxidative stress and inflammatory processes. Long-term inflammation and oxidative stress may significantly affect the initiation of the neoplastic transformation process. Here, we describe the synthesis of a new series of Mannich base-type hybrid compounds containing an arylpiperazine residue, 1,3,4-oxadiazole ring, and pyridothiazine-1,1-dioxide core. The synthesis was carried out with the hope that the hybridization of different pharmacophoric molecules would result in a synergistic effect on their anti-inflammatory activity, especially the ability to inhibit cyclooxygenase. The obtained compounds were investigated in terms of their potencies to inhibit cyclooxygenase COX-1 and COX-2 enzymes with the use of the colorimetric inhibitor screening assay. Their antioxidant and cytotoxic effect on normal human dermal fibroblasts (NHDF) was also studied. Strong COX-2 inhibitory activity was observed after the use of TG6 and, especially, TG4. The TG11 compound, as well as reference meloxicam, turned out to be a preferential COX-2 inhibitor. TG12 was, in turn, a non-selective COX inhibitor. A molecular docking study was performed to understand the binding interaction of compounds at the active site of cyclooxygenases.

Inhibition of cyclooxygenase is the way of therapeutic activities for anti-inflammatory pharmaceuticals. Serum albumins are the major soluble protein able to bind and transport a variety of exogenous and endogenous ligands, including hydrophobic pharmaceuticals. In this study, a novel N-substituted 1H-pyrrolo[3–c]pyridine-1,3(2H)-diones derivatives were synthesized and biologically evaluated for their inhibitory activity against cyclooxygenases and interactions with BSA. In vitro, COX-1 and COX-2 inhibition assays were performed. Interaction with BSA was studied by fluorescence spectroscopy and circular dichroism measurement. The molecular docking study was conducted to understand the binding interaction of compounds in the active site of cyclooxygenases and BSA. The result of the COX-1 and COX-2 inhibitory studies revealed that all the compounds potentially inhibited COX-1 and COX-2. The IC50 value was found similar to meloxicam. The intrinsic fluorescence of BSA was quenched by tested compounds due to the formation of A/E–BSA complex. The results of the experiment and molecular docking confirmed the main interaction forces between studied compounds and BSA were hydrogen bonding and van der Waals force.

Olivacine is an alkaloid-containing pyridocarbazole structure. It is isolated from the bark of the evergreen timber tree, Aspidosperma olivaceum. Its well-documented anticancer activity led to the synthesis of new derivatives, which are semisynthetic and fully synthetic pyridocarbazoles. This study aimed to evaluate the potential antineoplastic activity of four newly synthesized olivacine derivatives. Multidrug resistance is a common phenomenon causing failure in the chemotherapy of many tumors. It is mainly related to increased function of P-glycoprotein, an efflux pump removing cytostatic out of the cells. The cell lines used in the study were colorectal carcinoma cell lines: LoVo (doxorubicin-sensitive) and LoVo/DX (doxorubicin-resistant). The NHDF cell line was used to assess cell viability. First, the cells were incubated with olivacine derivatives. In the next step, the following assays were performed: DCF-DA assay, MTT assay, rhodamine 123 assay, detection of apoptosis, proliferation inhibition-mitotic index. The tested compounds showed higher antineoplastic potential and lower toxicity than the reference compound ellipticine. The results indicate that the new olivacine derivatives are good candidates for future anticancer drugs.

Cyclooxygenase inhibitors as anti-inflammatory agents can be used in chemoprevention. Many in vitro and in vivo studies on human and animal models have explained the mechanisms of the chemopreventive effect of COX inhibitors such as: induction of apoptosis, inhibition of neoplasia, angiogenesis suppression, induction of cell cycle inhibition and inhibition of the expression of peroxisome proliferator-activated receptors. Here, biological evaluation of twelve different Schiff base derivatives of N-(2-hydrazine-2-oxoethyl)-4,6-dimethyl-2-sulfanylpyridine- 3-carboxamide are presented. Their in vitro anti-COX-1/COX-2, antioxidant and anticancer activities were studied. The molecular docking study was performed in order to understand the binding interaction of compounds in the active site of cyclooxygenases. Compounds PS18 and PS33 showed a significant inhibitory activity on COX-1 at lower concentrations compared to meloxicam and piroxicam. The IC50 of COX-1 of these compounds was 57.3 µM for PS18 and 51.8 µM for PS33. Out of the tested compounds, the highest therapeutic index was demonstrated by PS18, PS19, PS33, PS40 and PS41. Lower molar concentrations of these compounds inhibit the growth of cancer cells while not inhibiting the healthy cells. Compounds PS18, PS19 and PS33 simultaneously demonstrated a statistically-significant inhibition of COX-1 or COX-2. This opens up the possibility of applying these compounds in the chemoprevention of cancer.

Graphene has been one of the most tested materials since its discovery in 2004. It is known for its special properties, such as electrical conductivity, elasticity and flexibility, antimicrobial effect, and high biocompatibility with many mammal cells. In medicine, the antibacterial, antiviral, and antitumor properties of graphene have been tested as intensively as its drug carrying ability. In this study, the protective effect of graphene oxide against Rubella virus infection of human lung epithelial carcinoma cells and human chondrocyte cells was examined. Cells were incubated with graphene oxide alone and in combination with the Rubella virus. The cytopathic effect in two incubation time periods was measured using DAPI dye as a percentage value of the changed cells. It was shown that the graphene oxide alone has no cytopathic effect on any of tested cell lines, while the Rubella virus alone is highly cytopathic to the cells. However, in combination with the graphene oxide percentage of the changed cells, its cytotopathicity is significantly lower. Moreover, it can be concluded that graphene oxide has protective properties against the Rubella virus infection to cells, lowering its cytopathic changes to the human cells.