Glycyrrhiza glabra (licorice) belongs to the family Fabaceae and has a long story in traditional medicines and folk remedies to treat inflammation, arthritis, gastrointestinal problems and dyspepsia, Consequently, there is ongoing research into novel plants and herbal compounds possessing anti-inflammatory properties, aiming to uncover more potent alternatives while mitigating the potential toxicities associated with conventional anti-inflammatory medications.

The aim of the present study was to evaluate the anti-inflammatory activity of Hydroalcoholic extract of Glycyrrhiza glabra root, in order to find new and more effective agents for the treatment of degenerative and inflammatory diseases.

The activity of anti-inflammatory was assessed by the protein denaturation method using the standard drug Diclofenac.

The phytochemical constituents identified were flavonoids, alkaloids, phenols, saponins, steroids, and terpenoids, with flavonoids, alkaloids, and phenols being the most abundant.

The results showed that the Hydroalcoholic extract of G. glabra root have a very good inhibitory effect, with percentages of 81 %, at a concentration of 10 g/L compared to Diclofenac (61.3 %).

Hydroalcoholic extract of roots exhibit attractive property anti-inflammatory, which can be attributed to the presence of secondary metabolites of different classes of compounds and can therefore, be considered a promising candidate for future application as alternative therapeutic agents, particularly in the development of anti-inflammatory drugs.

Introduction: Globimetula oreophila belongs to the family Loranthaceae, and it is a hemiparasitic shrub that grows on dicotyledonous trees like neem trees, rubber trees, citrus trees, cocoa trees, and kola nuts. In traditional medicine, it is used to treat conditions like malaria, diarrhea, headaches, and insomnia. The G. oreophila genus and family (Loranthaceae) are poorly studied regarding their secondary metabolite constituents. This research study aims to isolate and characterize some of the bioactive secondary metabolites present in the butanol fraction of G. oreophila. Method: the powdered plant material was extracted with 70% ethanol using cold maceration which afforded the crude ethanol extract. Partitioning of the crude ethanol extract with n-hexane, chloroform, ethyl acetate, and n-butanol produced the corresponding fractions, where the n-butanol fraction was subjected to silica gel column chromatography and repeated gel filtration. Results: column chromatographic separation of the n-butanol fraction led to the isolation of a yellowish amorphous substance as flavonol (1) and flavonol glycoside (2). Physical and chemical tests, spectroscopic analysis, and literature data led to the elucidation of compounds 1 and 2 as quercetin (5, 7, 3’, 4’-tetrahydroxy-quercetin-3-O-α-L-rhamnopyranoside) and quercetin rhamnoside (3, 5, 7, 3’, 4’-pentahydroxy flavone), respectively. Conclusion: Compounds 1 and 2 were isolated for the first time from the plant and contributed to the chemical taxonomy of the plant.

Phthalates are a group of chemical compounds used primarily as plasticizers to increase the flexibility, transparency, durability, and longevity of plastics. Consequently, they are commonly found in products such as plastic food packaging, clothing, cosmetics, PVC-based toys, and medical devices, among others. However, the use of phthalates poses various health risks, including endocrine disruption and reproductive toxicity, and can also have harmful effects on the environment. Therefore, rapid analytical methods with good analytical figures of merit are needed to detect them.

This study describes the development of a liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS) method for the detection of phthalates in different samples based on precursor ion scan. LC-MS/MS was chosen due to its high sensitivity and selectivity. The precursor ion mode enhances analysis specificity by identifying phthalates through their precursor ions, specifically the 149-precursor ion, which is characteristic of phthalates due to their common fragmented structure.

The developed method was successfully applied to different sample types (such as plastics, clothing, and cosmetics), demonstrating its applicability. The obtained results were compared with those produced by a similar gas chromatography coupled with tandem mass spectrometry (GC-MS/MS) method. This approach allows for an effective initial screening of phthalates in quality control laboratories, facilitating the rapid identification of potential contamination and ensuring regulatory compliance.

1-Hydroxy-N-phenylnaphthalene-2-carboxamide and a series of other seventeen carboxanilides in the anilide part of dichlorinated, trichlorinated and dibrominated, tribrominated and chlorinated/brominated have recently been reported as biologically active compounds mainly with antibacterial, antimycobacterial and anticancer effects. Since lipophilicity is one of the factors influencing the bioavailability (absorption, distribution, metabolism, elimination) and activity and even toxicity of bioactive compounds, all the derivatives were investigated for their lipophilic and hydrophilic properties. All eighteen compounds were analyzed by reversed-phase high-performance liquid chromatography (RP-HPLC). The procedure was performed under isocratic conditions with methanol as the organic modifier in the mobile phase using an end-capped non-polar C18 stationary reversed-phase column. The lipophilicity values are expressed as the logarithm of the capacity factor k (for the mobile phase water : methanol) and the distribution coefficients D at pH values of 6.5 and 7.4 (for the mobile phase buffer : methanol), as well as the calculated values of log P/Clog P by various methods. The unsubstituted derivative is the least lipophilic, 1-hydroxy-N-(3,4,5-trichlorophenyl)naphthalene-2-carboxamide and N-(4-bromo-3-chlorophenyl)-1-hydroxynaphthalene-2-carboxamide are the most lipophilic. The mutual correlations between the experimental and predicted lipophilicity values are low, in addition, there are large deviations in the cross-correlations between log k and log D, which is due to the presence of a free ionizable phenolic group in the molecule.

Recently reported multihalogenated (CF₃/Cl) anilides of 1-hydroxynaphthalene-2-carboxanilides showed significant activity against both the reference strain Staphylococcus aureus ATCC 29213 and clinical isolates of methicillin-resistant S. aureus (MRSA). This fact inspired further investigation of the effect of these compounds on staphylococci. Chemoproteomics is a tool for investigating protein targets of potential drugs. It makes it possible to understand the effect of a bioactive molecule on a living system. An activity-based protein profiling (ABPP) method was employed using highly active, moderately active, and inactive ring-substituted 1-hydroxynaphthalene-2-carboxanilides as probes. The experiment was performed on the universally sensitive collection strain S. aureus ATCC 29213. Tryptic cleavage of proteins was performed prior to HPLC-MS/MS analysis. Protein profiles of control samples (S. aureus cells) and profiles of S. aureus treated with inactive/active derivatives were investigated and compared to each other. More than 1000 proteins were analyzed, with approximately 70% of the proteins was increased and 30% of the proteins was decreased after treatment with the investigated compounds. Under the influence of highly active compounds, the bacteria did not survive, although the expression of some life-supporting proteins (e.g., serine-aspartate repeat protein D) was observed; on the contrary, staphylococcal collagenase was one of the most inhibited enzymes. The functions of a set of proteins increased/decreased by the studied derivatives were characterized, on the basis of which the effect of bioactive agents against S. aureus can be monitored.

The data obtained by the author in the field of chemistry of carbon clusters, namely, the chemical binding of C₆₀ fullerene with 5Z,9Z-dienoic acids by nucleophilic addition to the carbon cluster of α halocarbanions generated in situ from their malonic acid esters are summarized. Based on ethyl, benzyl, acetylene and triazole esters of malonic acid containing 5Z,9Z-dienoic acids and C₆₀ fullerene, new hybrid methanofullerenes were synthesized under the conditions of the Bingel-Hirsch reaction. The synthesized methanofullerenes exhibit high cytotoxic activity towards tumor cells of the Jurkat, K562, U937, HL60 lines, and it has also been established that they are effective inducers of apoptosis, exerting a phase-specific cytotoxic effect on the cell cycle of tumor cells.

Next, by the method of intermolecular esterification of malonic acid with α,ω-diols, in the presence of hafnium triflate Hf(OTf)4, previously undescribed macrodiolides containing a 1Z,5Z-diene fragment in the structure were synthesized in high yields and stereoselectivity.Under the conditions of the Bingel-Hirsch reaction, chemical binding of the synthesized macrodiolides with C₆₀ fullerene was carried out to obtain the corresponding methanofullerenes. The cytotoxic activity of macrodiolides and methanofullerenes in relation to tumor cell lines Jurkat, K562, U937, HL60 and normal fibroblasts was studied. It was found that the cytotoxicity of the hybrid molecule is higher compared to the original macrodiolide (from 5 to 170 times). In addition, the synthesized hybrid molecules initiate apoptosis by uncoupling oxidation and phosphorylation of the mitochondrial membrane of tumor cells.

Essential oils (EOs) are complex mixtures of terpenic and phenolic volatiles, although other groups of compounds can be present in high proportions. Due to their strong biological activities, EOs have been increasingly screened for nematicidal activity against plant parasitic nematodes of crops and forest species. Direct-contact bioassays can provide important data on the properties of anti-nematodal chemical structures. In previous studies, the EO of Satureja montana, winter savory, revealed a high nematicidal activity against the pinewood nematode (PWN), a dangerous phytoparasite that attacks pine trees and causes pine wilt disease in susceptible trees. The bioactivity of S. montana EO was attributed to its oxygen-containing molecules, while the hydrocarbon molecules showed only a weak activity. However, the interactions between EO compounds was not ascertained. In the present study, the main compounds of winter savory EO, i.e., the phenol carvacrol (64%), and the hydrocarbons γ-terpinene (18%) and p-cymene (8%) were tested solely to pinpoint the main responsible for the nematicidal strength of the EO; and in binary combinations to assess synergistic or antagonistic interactions. Direct-contact bioassays were performed for the compounds and their binary combinations at the proportions they presented in the original EO. Carvacrol, induced the strongest response, inducing complete PWN mortality at a concentration as low as 0.5 mg/mL, however, γ-terpinene and p-cymene appear to influence its activity, even though they induced a low PWN mortality at 1 mg/mL. Uncovering the interactions between the components of nematicidal EOs can provide clues to formulate more effective sustainable alternatives to traditional pesticides.

One of the first adamantane derivatives used in medicine was amantadine (1-aminoadamantane), which showed good activity against the influenza virus. The introduction of an adamantane fragment into the structures of known drugs leads to an increase in lipophilicity and a noticeable improvement in pharmacological properties. Many adamantane derivatives have a wide range of biological activities, including antiviral, antidiabetic, antibacterial, antimalarial, anticancer, and anti-inflammatory properties. A hybrid molecule based on 5Z,9Z-eicosa-5,9-dienoic acid and 1-aminoadamantane was synthesized in high yield. The Ti-catalyzed cross-cyclomagnesiation reaction of 2-(hepta-5,6-dien-1-yloxy)tetrahydro-2H-pyran and trideca-1,2-diene produced dialkylidenemagnesacyclopentane, the hydrolysis of which and subsequent removal of tetrahydropyranyl protection led to ( 5Z,9Z)-eicosa-5,9-dien-1-ol. By oxidation of the resulting diene alcohol, (5Z,9Z)-eicosa-5,9-dienoic acid was obtained. The reaction of 1-aminoadamantane with dienoic acid was carried out in the presence of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC HCl) and catalytic amounts of N,N-4-dimethylaminopyridine (DMAP) to give (5Z,9Z)-N -(adamantan-1-yl)eicosa-5,9-dienamide. The synthesized amide was tested for the viability of human tumor cells using the HEK293, Jurkat and K562 tumor lines as an example. Drugs known as topoisomerase I and II inhibitors, camptothecin and etoposide, were taken as controls. Our data show that the synthesized hybrid molecule based on (5Z,9Z)-eicosa-5,9-dienoic acid and 1-aminoadamantane is a promising inducer of apoptosis in tumor cells.

Enteric coating plays a crucial role in preventing the disintegration of pharmaceutical dosage forms in the stomach. This is particularly important for drugs that are unstable at an acidic pH or are designed to act in the small intestine. While conventional synthetic polymers have been widely used for enteric coatings, there is growing interest in exploring naturally derived proteins as an alternative. This study focused on two natural polymers: soya protein and whey protein isolates, first by determining the gastro-resistance properties of films prepared from these proteins. Then, appropriate casting solutions will be developed to create polymeric films, and their resistance to acidic pH will be evaluated using disintegration tests. Second, crate drug pellets coated with the most effective protein-based film were previously prepared, and their performance was assessed using the USP apparatus I (basket). The results demonstrated that the coated pellets (SA and SAG) exhibited excellent gastro-resistance properties. Specifically, the percentage release of the coated pellets met the USP criteria: less than 10% release in the first 2 hours under acidic conditions, followed by at least 80% release within 45 minutes in the buffer phase. In contrast, uncoated pellets showed immediate release, with over 69% of the dye released during the initial 2 hours. Notably, the SA and SAG-coated pellets demonstrated remarkable resistance to acidic pH, releasing only 1% and approximately 2% of the dye faster than uncoated pellets. These findings highlight the potential of SA and SAG coating films for efficient delayed release or enteric coating applications.

1Z,5Z-diene compounds containing biologically active 3,4-dimethoxyphenyl fragments were synthesized. Molecules containing this moiety have attracted the attention of medicinal chemistry researchers due to their biological activities, including anti-inflammatory and antioxidant, anticancer, fungicidal and neuroprotective activities. The presence of methoxy groups in these structures enhances their biological activity as they participate in various interactions that are critical for their binding affinity and selectivity towards certain biological targets. The intermolecular homo-cyclomagnesiation reaction of 4-(buta-2,3-dien-1-yl)-1,2-dimethoxybenzene catalyzed by Cp2TiCl2 with the help of EtMgBr produced dialkylidenemagnesacyclopentane, the acid hydrolysis of which led to the production of (2Z,6Z)-1,8 -bis(3,4-dimethoxyphenyl)octa-2,6-diene with a yield of 74%. Also, Ti-catalyzed cross-intermolecular cyclomagnesiation of 4-(buta-2,3-dien-1-yl)-1,2-dimethoxybenzene with octadeca-1,2-diene produces the corresponding dialkylidenemagnesacyclopentane, acid hydrolysis of which gives the target 1,2- dimethoxy-4-((2Z,6Z)-pentacose-2,6-dien-1-yl)benzene in 68% yield. Cyclomagnesiation reactions were carried out in an inert atmosphere of argon. The resulting products were isolated using column chromatography. The structures of the synthesized compounds were determined using elemental analysis, IR, 1H-NMR, 13C-NMR spectral data and mass spectroscopy. The resulting 1Z,5Z-dienes containing 3,4-dimethoxyphenyl fragments are of great interest as objects for studying their biological activity.