Acid Compounds Research Articles

Atmospheric implications of hydrogen bonding between methanesulfonic acid and 12 kinds of N-containing compounds

The hydrogen bonding interactions between methanesulfonic acid (MSA) and NHx compounds, such as ammonia (A), alkylamines (aNHx), and cyclic amino compounds (cNHx), were investigated using density functional theory, atoms in molecules, localized molecular orbitals-based energy decomposition analysis, and atmospheric clusters dynamic code methods. The results revealed that these dimers exhibit hydrogen bonds by SOH⋯N interactions. MSA–cNHx dimers showed higher binding energies compared to MSA–aNHx/A dimers. Topological analysis using AIM confirmed the presence of hydrogen bonding in these dimers by ρ(r) and ∇2ρ(r). The results of IRI indicate that there are different strength types of hydrogen bonding interactions in these dimers. LMO–EDA highlighted electrostatic interactions as the main attractive force, particularly in MSA–cNHx dimers. ACDC results showed a low evaporation rate for MSA–cNHx dimers compared to others. These findings suggest that MSA plays a crucial role in NPF events, and MSA–cNHx clusters could potentially act as nucleation nuclei in the atmosphere.

Chemical Composition, In vitro and In silico Evaluation of Essential Oil Extracted from Mentha Piperita L. for Lung Cancer

Background: Mentha piperita, a naturally occurring herb, is utilized in medicinal formulations. It possesses abundant bioactive elements, including flavonoids and phenolic acid compounds,that exhibit various properties such as antioxidants, anti-inflammatory and anti-cancer. Objective: In the present study, chemical constituents of essential oil extracted from Mentha piperita were analyzed and identified through GC-MS. In vitro antiproliferative activity was performed on A549 lung cancer cell line lines. In silico study was conducted by Schrodinger’s Maestro’s software to identify chemical constituents in the plant as potential EGFR (Epidermal Growth Factor Receptors) inhibitors Methods: Hydro-distilled essential oil was analyzed by GC-MS to identify chemical components based on the retention index and mass fragmentation pattern, which was then tested for its antiproliferative activity by MTT assay against human lung cancer cell lines. All the identified constituents were investigated in silico for their affinity towards EGFR (Epidermal Growth Factor Receptors). Results: A total of thirty constituents were identified where D-carvone (56.69%), L-limonene (12.36%), squalene (3.36%), cis-carveol (2.93%), and α-amorphene (2.36%) were observed as major constituents of the essential oil. The essential mentha oil also exhibited antiproliferative activity against lung cancer cell lines with an IC50 value of 86.05 µg/ml. Furthermore, from the in silico study, five constituents were identified to have a better affinity for EGFR (Epidermal Growth Factor Receptors) than that of the standard drug Osimertinib. Conclusion: In the present study, the aerial part of the plant Mentha piperita was hydrodistilled.Thirty phytoconstituents were identified through GC-MS data. An in-silico study was performed using Schrodinger software, and a further in vitro study was performed in which essential oil showedgood antiproliferative activity against the A549 cancer cell line.

Molecular docking study of modified isoniazid compounds on mycolic acid synthase in the cell wall of mycobacterium tuberculosis

Using the isoniazid in antituberculosis therapy can lead to mutations in the KatG and inhA genes of Mycobacterium tuberculosis, resulting in the development of resistance and necessitating modifications to the isoniazid compound. This study aims to assess the potential and level of toxicity of modified compounds, namely 4-pyridine carboxylic acid, pyridine aldehyde, and methyl pyridine, on the mycolic acid receptor through a molecular docking approach. PyRx was employed for the docking process using a protocol with an exhaustiveness of 106 and a center grid box at X=42.424, Y=22.4321, and Z=46.6391. Additionally, the ProTox-II website was used to determine the toxicity level of the test compounds. The results obtained from this research consist of the respective affinity values of the test compounds: -6, -5.4, and -5.2 kcal/mol. The toxicity levels of the test compounds are as follows: class 5, class 4, and class 4. All test compounds interact with amino acids on the target protein, specifically with residue numbers Histidine (HIS A:8), Phenylalanine (PHE A:142) through hydrogen bonding, Leucine (LEU A:95) through pi-Sigma (π) bonding, and Valine (VAL A:12) through pi-Alkyl (π) bonding. In conclusion, the 4-pyridine carboxylic acid compound exhibits potential as a promising drug candidate but comes with a high level of toxicity

Novel Aryl Phosphate for Improving Fire Safety and Mechanical Properties of Epoxy Resins

Epoxy resins (EPs) are highly flammable, and traditional flame retardant modifications often lead to a significant reduction in their mechanical performance, limiting their applications in aerospace and electrical and electronic fields. In this study, a novel flame retardant, bis(4-(((diphenylphosphoryl)oxy)methyl)phenyl)phenyl phosphate (DMP), was successfully prepared and introduced into the EP matrix. When the addition of DMP was 9 wt%, the EP/9 wt% DMP thermosets passed the UL-94 V-0 rating, and their LOI was increased from 24.5% of EP to 35.0%. With the introduction of DMP, the phosphoric acid compounds from the decomposition of DMP promoted the dehydration and charring of the EP matrix, and the compact, dense char layer effectively exerted the shielding effect in the condensed phase. Meanwhile, the produced phosphorus-containing radicals played a quenching effect in the gas phase. As a result, the peak heat release rate (PHRR) and total heat release (THR) of EP/9 wt% DMP were reduced by 68.9% and 18.1% compared to pure EP. In addition, the polyaromatic structure of DMP had good compatibility with the EP matrix, and the tensile strength, flexural strength and impact strength of EP/9 wt% DMP were enhanced by 116.38%, 17.84% and 59.11% in comparison with that of pure EP. This study is valuable for expanding the application of flame-retardant EP/DMP thermosets in emerging fields.

Amino Acid Compound 2 (AAC2) Treatment Counteracts Insulin-Induced Synaptic Gene Expression and Seizure-Related Mortality in a Mouse Model of Alzheimer’s Disease

Diabetes is a major risk factor for Alzheimer’s disease (AD). Amino acid compound 2 (AAC2) improves glycemic and cognitive functions in diabetic mouse models through mechanisms distinct from insulin. Our goal was to compare the effects of AAC2, insulin, and their nanofiber-forming combination on early asymptomatic AD pathogenesis in APP/PS1 mice. Insulin, but not AAC2 or the combination treatment (administered intraperitoneally every 48 h for 120 days), increased seizure-related mortality, altered the brain fat-to-lean mass ratio, and improved specific cognitive functions in APP/PS1 mice. NanoString and pathway analysis of cerebral gene expression revealed dysregulated synaptic mechanisms, with upregulation of Bdnf and downregulation of Slc1a6 in insulin-treated mice, correlating with insulin-induced seizures. In contrast, AAC2 promoted the expression of Syn2 and Syp synaptic genes, preserved brain composition, and improved survival. The combination of AAC2 and insulin counteracted free insulin’s effects. None of the treatments influenced canonical amyloidogenic pathways. This study highlights AAC2’s potential in regulating synaptic gene expression in AD and insulin-induced contexts related to seizure activity.

Encapsulation of ɣ-Aminobutyric Acid Compounds Extracted from Germinated Brown Rice by Freeze-Drying Technique

Gamma-aminobutyric acid (GABA) from plants has several bioactivities, such as neurotransmission, anti-cancer cell proliferation, and blood pressure control. Its bioactivities vary when exposed to pH, heat, and ultraviolet. This study analyzed the protective effect of the GABA encapsulation technique using gum arabic (GA) and maltodextrin (MD) and the freeze-drying method. The impact of different ratios of the wall material GA and MD on morphology, GABA content, antioxidant activity, encapsulation efficiency, process yield, and physical properties were analyzed. Results showed that the structure of encapsulated GABA powder was similar to broken glass pieces of various sizes and irregular shapes. The highest GABA content and encapsulation efficiency were, respectively, 90.77 mg/g and 84.36% when using the wall material GA:MD ratio of 2:2. The encapsulated powder’s antioxidant activity was 1.09–1.80 g of encapsulation powder for each formula, which showed no significant difference. GA and MD as the wall material in a 2:2 (w/w) ratio showed the lowest bulk density. The high amount of MD showed the highest Hausner ratio (HR), and Carr’s index (CI) showed high encapsulation efficiency and process yield. The stability of encapsulated GABA powder can be kept in clear glass with a screw cap at 35 °C for 42 days compared to the non-encapsulated one, which can be preserved for only 18 days under the same condition. In conclusion, this study demonstrated that the freeze-drying process for GABA encapsulation preserved GABA component extracts from brown rice while increasing its potential beneficial properties. Using a wall material GA:MD ratio of 2:2 resulted in the maximum GABA content, solubility, and encapsulation efficiency while having the lowest bulk density.

Kinetic control aspects and mechanisms in oriented membrane processes for extraction and recovery of ascorbic acid compound.

Ascorbic acid comprises four enantiomers, with only one of them, L-ascorbic acid, recognized as vitamin C. The modern industries place significant importance on obtaining this compound in its purest form. The challenge is to recover L-ascorbic acid, which requires specific processes within these industries. To satisfy this condition, purification is needed, a process that requires large quantities of solvents and high energy consumption. To overcome these limitations, we conducted a study on the facilitated extraction of L-ascorbic acid using three affinity polymer membranes, including supported liquid membrane (SLM), polymer inclusion membrane (PIM), and grafted polymer membranes (GPM) with cholic acid as the extractive agent. Following the characterization of the membranes using IR spectroscopy and SEM techniques, we investigated various parameters associated with substrate diffusion through the organic membrane phase. Regarding the biologically active L-ascorbic acid, our research findings indicated that kinetic factors drove the mechanisms of the studied processes.

Bioisosteric Replacement in the Search for Biologically Active Compounds: Design, Synthesis and Anti-Inflammatory Activity of Novel [1,2,4]triazino[2,3-c]quinazolines

Background: Designing novel biologically active compounds with anti-inflammatory properties based on condensed quinazolines is a significant area of interest in modern medicinal chemistry. In the present study, we describe the development of promising new bioactive molecules through the bioisosteric replacement of a carbon atom with a sulfur atom in anti-inflammatory agents, specifically 3-methyl-2-oxo-2H-[1,2,4]triazino[2,3-c]quinazolin-6-yl)butanoate. Methods: Design and synthetic studies have led to the series of previously unknown substituted 2-[((3-R-2-oxo-2H-[1,2,4]triazino[2,3-c]quinazolin-6-yl)methyl)thio]carboxylic acids and their esters. These compounds were synthesized by reacting 6-chloroalkyl-3-R-2H-[1,2,4]triazino[2,3-c]quinazolin-2-ones with sulfanylalkyl carboxylic acids and their functional derivatives. The purity and structure of the obtained compounds were confirmed using a set of physicochemical methods, including elemental analysis, HPLC-MS, and 1H NMR spectroscopy. Molecular modeling, predicted toxicity, drug-likeness, and pharmacokinetics data were used to select compounds for evaluation of their effects on acute aseptic inflammation (carrageenan-induced paw edema test) and on markers of the inflammatory process. Results: The compound 2-((1-(3-methyl-2-oxo-2H-[1,2,4]triazino[2,3-c]quinazolin-6-yl)ethyl)thio)acetic acid (compound 2e) was identified as the most active anti-inflammatory agent (AA = 53.41%), demonstrating significant inhibition of both paw edema development and the generation of pro-inflammatory cytokines and mediators. Conclusions: Results from docking studies and analysis of “structure-affinity” correlations revealed that these compounds are promising candidates for further modification and detailed investigation of their anti-inflammatory activity

Silver Nanoparticles (AgNPs) Act as Nanoelicitors in Melissa officinalis to Enhance the Production of Some Important Phenolic Compounds and Essential Oils

ABSTRACTNanoparticles (NPs) are well‐known biostimulants in plant biotechnology, utilised to enhance the physical properties of plants and exhibit positive effects on them. The important key role is the most suitable type, effective dose and size of NP to be used in plant tissue culture systems. In this study, various concentrations of silver nanoparticles (AgNPs; 0, 25, 50, 75 and 100 μg L−1) were tested as elicitors in callus culture with the aim of enhancing secondary metabolite production in lemon balm (Melissa officinalis L.). According to the results obtained, callus formation rates have shown an increase in all applications compared to the control group. The highest callus formation, weight and diameter were observed in 50 μg L−1 application. In this application, the callus structure was compact and its colour was green. However, the aromatic compounds, neral and geranial increased significantly in 25 μg L−1 application. The maximum increase in phenolic compounds such as caffeic acid, chlorogenic acid, proto‐catechic acid, hesperidin and p‐coumaric acid was observed in the 75 μg L−1 AgNP and the highest increase in rosmarinic acid compound was determined in the 50 μg L−1 application. The study found that AgNP applications are an effective method for increasing the production of secondary metabolites in medicinal and aromatic plants, such as lemon balm, in vitro.

Pharmacokinetics of tolfenamic acid in ducks (Anas platyrhynchos domestica) after different administration routes

ABSTRACT 1. The objective of this research was to compare the pharmacokinetics and bioavailability of tolfenamic acid, analgesic, antipyretic and anti-inflammatory compound, after administration through different routes to Pekin ducks. The investigation was carried out over four time periods using a randomised cross-pharmacokinetic design. 2. Tolfenamic acid was administered to ducks intravenously, intramuscularly, subcutaneously and orally at a dose of 2 mg/kg. Tolfenamic acid analysis was performed using HPLC-UV and pharmacokinetic data were conducted by non-compartmental analysis. 3. The total clearance, volume of distribution at steady state and terminal elimination half‐life after intravenous administration were 0.14 l/h/kg, 0.29 l/kg and 1.80 h, respectively. The peak plasma concentration and bioavailability for intramuscular, subcutaneous and oral administration were 4.59, 3.55 and 2.23 μg/ml and 93.62, 74.30 and 43.43%, respectively. 4. Tolfenamic acid was absorbed rapidly, eliminated quickly and exhibited a small distribution volume in Pekin ducks. Pharmacokinetic parameters, including maximum concentration, area under the plasma concentration – time curve and bioavailability, were found to be different in ducks from other bird species.

Benzylpiperazinyl derivatives of alepterolic acid: Synthesis and cytotoxic evaluation.

Natural products play a significant role in the development of modern drugs. Alepterolic acid, a labdane-type diterpenoid firstly isolated from Aleuritopteris argentea (Gmél.) Fée, has been identified as a valuable template for the synthesis of potent anticancer agents by structural modification. In this study, a series of new derivatives was obtained by coupling alepterolic acid with benzylpiperazines. It was found that (3,4-dichlorobenzyl)piperazinyl alepterolic acid (compound 6p) displayed the most toxic against MCF-7 cell line, with IC50 value of 8.31±0.67 μM. Further investigations demonstrated that compound 6p induced morphological changes in MCF-7 cells, inhibited proliferation in a time- and dose-dependent manner. Furthermore, western blot analysis revealed that compound 6p induced a significant increase in cleaved caspase-9, cleaved caspase-3, cleaved poly (ADP-ribose) polymerase (PARP) and Bax/Bcl2 ratio in MCF-7 cells. All of these results confirmed that compound 6p induced endogenous apoptosis in MCF-7 cells. Conclusively, the findings suggest that the incorporation of benzylpiperazine to alepterolic acid represents a promising approach for the discovery of new drug candidates.

Experimental evaluation of acid number effect on interfacial tension between nitrogen and mixtures of petroleum fractions including diesel fuel and gasoline at different pressures

Crude oil is made up of very complex compounds, which are found in polar organic substances especially organic acid compounds in the majority. Although organic acid content in crude oil is low, the presence of organic acids affects the interfacial tension (IFT) in oil reservoirs thereby altering the enhancement of oil recovery using nitrogen gas (N2) injection. Therefore, in this study, the effects of pressure (1 to 35 bar), the percentage of aromatic compounds (0.0 to 100 vol%) in the aliphatic hydrocarbon samples and the organic acid (benzoic acid) content (0.0 to 0.8 g.L− 1) on IFT between a mixture of gasoline/diesel fuel and N2 were investigated at a temperature of 298 K. IFT does not necessarily decrease as pressure increases for the sake of existence of aromatic compounds. IFT alteration for gasoline was more (about 8 dyne.cm− 1) than for diesel fuel (approximately 4 dyne.cm− 1) during pressure increased from 1 to 35 bar due to the replacement of heavy long chain aliphatic compounds instead of light aromatic matters. The effect of IFT alteration between N2 and diesel fuel during increasing the organic acid content was little (approximately 1.5 dyne.cm− 1), in contrast, this effect was more noticeable for N2/gasoline (about 8 dyne.cm− 1). In addition, a reduced cubic model for estimating IFT between N2 and petroleum fractions in terms of pressure, petroleum fraction composition and organic acid content was proposed with an average relative error of less than 2.6%.

First Report on Salvia Sahendica Boiss & Buhs roots biocomponents characterization by GC-MS and HPLC and Antibacterial Potency

Treatment of bacterial infections with antibiotic resistance is complicated. For this reason, new therapeutic methods are needed to control bacterial infections. Therefore, it is necessary to discover new antibiotics from medicinal plants that can destroy drug-resistant bacteria. Essential oils (EO) of some medicinal plants have antimicrobial effects and can be used as antimicrobial agents in the treatment of infections and food industries. The aim of this study was to determine the EO composition and antimicrobial effects of EO and polyphenols profile of Salvia Sahendica roots for the first time. Chemical compounds and antibacterial activity of EOs against Staphylococcus aureus and Bacillus cereus as gram-positive and Escherichia coli and Pseudomonas aeruginosa as gram- negative bacteria were evaluated using microtiter broth dilution method. Studied organs of S. sahendica showed significant diversity in terms of type and percentage of essential oil and polyphenol compounds. Overall, 44, 46, 42, and 45 compounds were identified in the essential oil of leaves, flowers, stems, and roots of this plant, which constituted 99.6, 99.3, 98.2, and 99.4% of total oil composition, respectively. The current study collectively demonstrated inhibitory effects ranged from strong (S. aureus) to low inhibition (P. aeruginosa). According to the HPLC result, the amounts of coumaric acid, chlorogenic acid, and gallic acid compounds in the root are higher than in other plant parts, which indicate that the root can be a suitable source for the production of these valuable polyphenol compounds. Due to the results, it is possible to hope for the application of EO from S. sahendica as natural antibacterial in the pharmaceutical and food industries.

Preservation with Different Smoking Techniques to Extend the Shelf Life of “Urutan” Chicken

“Urutan” chicken is one of the processed meat products processed through the manufacture of meat dough, fat and complete Balinese spices ("Basa Genep"). Extending the shelf life of “urutan” chicken can be done by smoking process either by cold smoking method or hot smoking. Smoke can preserve food ingredients due to the presence of acid, phenolic and carbonyl compounds. The method used in this study is Randomized Block Design (RBD) with a factorial pattern consisting of 2 factors, namely Factor I is Hot Smoking Technique consisting of 3 levels and Factor II is Smoking Time consisting of 4 levels so that 12 treatment combinations are obtained and 2 repetitions are carried out so that 24 experimental units are obtained. The parameters observed include phenol content, water content, ash content, fat content, protein content, Esherichia coli and Salmonella sp. Statistical analysis shows that smoking time has a significant effect (sig <0.05) on the phenol content of “urutan” chicken, but does not have a significant effect (sig> 0.05) on the fat and protein content of “urutan” chicken. The fat content of “urutan” chickens in the smoking duration treatment at a temperature of 100 ° C ranged from 9.798 - 11.870%. The lowest fat content was obtained in 2 hours of smoking, which was 9.798% which was not significantly different from other treatments. The protein content of “urutan” chickens in the smoking treatments of 0.5, 1, 1.5 and 2 hours ranged from 11.788 -12.197%. The smoking duration did not have a significant effect on the protein content of “urutan” chickens, which was probably because the smoking duration of 0.5 -2 hours had not denatured the protein sequence. The phenol content of “urutan” chickens in the smoking treatments of 0.5, 1, 1.5 and 2 hours ranged from 0.206 - 0.312%. The highest phenol content was obtained in 2 hours of smoking at a smoking temperature of 100 ° C, which was 0.312%. The results showed that the longer the smoking, the higher the phenol content of “urutan” chickens. The lowest pH value was obtained in the 100 °C 2-hour smoking treatment of 5.16, which was significantly different from other treatments. The highest water content was obtained in the 100 °C 2-hour temperature treatment of 63.19%, which was significantly different from other treatments

Optimization of Germination Conditions for Enriched γ-Aminobutyric Acid and Phenolic Compounds of Foxtail Millet Sprouts by Response Surface Methodology.

The optimum germination conditions for foxtail millet sprouts enriched with γ-aminobutyric acid (GABA) and antioxidant polyphenols were investigated. From single-factor experimental results, both the GABA level and total phenolic content (TPC) were more significantly affected by soaking temperature and time, and concentration of sucrose culture solution. Response surface methodology (RSE) was used to optimize the germination conditions of foxtail millet sprouts, where the interaction between soaking temperature and sucrose concentration exhibited a significant (p < 0.05) effect on TPC, and the interaction between soaking time and sucrose concentration displayed a significant (p < 0.05) effect on GABA content. The optimal germination conditions for TPC and GABA enrichment of foxtail millet sprouts were soaking at 31 °C for 4.5 h and germinating at 35 °C with 4.5 g/L sucrose solution for 5 days. Under the optimized conditions, the TPC and GABA content of foxtail millet sprouts were 926.53 milligrams of ferulic acid equivalents per 100 g dry weight (mg FAE/100 g DW) and 259.13 mg/kg, separately, with less difference from the predicted values of 929.44 mg FAE/100 g DW and 263.60 mg/kg, respectively. Collectively, all the individual phenolic compounds increased significantly (p < 0.05) by optimization, except for cis-p-coumaric acid and cis-ferulic acid in bound. The results provide a practical technology for suitable germination conditions to improve the health components of foxtail millet sprouts and increase their added value.

Bacterial inhibition and biofilm eradication ability of low-toxic deep eutectic solvents prepared from lactic acid and quaternary ammonium compounds

In the present communication, the preparation of deep eutectic solvents (DESs) based on an aqueous solution of lactic acid (LA) and two different quaternary ammonium compounds, choline chloride (ChCl) and tetraethylammonium chloride (TEAC), is proposed for the application as an antibacterial agent. The antibacterial and cytotoxic properties of the DESs obtained were studied and found to be highly effective in inhibiting both Gram-positive and Gram-negative bacteria and eradicating bacterial biofilms. Moreover, the DESs obtained exhibited reduced cytotoxicity towards soft tissue cells compared to the aqueous LA solution. The excellent antibacterial properties and low cytotoxicity of the DESs prepared make them a promising candidate for the development of novel antimicrobial agents or antibacterial eutectogels for delivery systems and tissue engineering applications.

Investigation on induced smectic phases in double hydrogen bond liquid crystal complexes derived from aromatic carboxylic acids: Experimental and quantum chemical approaches

In the present study, double Hydrogen bond liquid crystal (HBLC) complexes in different mole ratio (1:1 and 1:2) have been isolated from symmetrical aromatic dicarboxylic acid of non-mesogenic compound 1,3-Phenylenediacetic acid (1,3-PDA) and mesogenic compound 4-n-dodecyloxybenzoic acid (12 OBA). Fourier transform infrared Spectroscopy (FTIR) explores the presence of functional groups in the title complexes. Formation of H-bond between 1,3-PDA and 12 OBA is experimentally confirmed by observing the FTIR peak at 3639 cm−1 (1:1 ratio). Induced mesophases and its textures along with transition temperatures are analyzed using polarizing optical microscope (POM) and differential scanning calorimetry (DSC). The layered structures (smectic phases) and their molecular mechanism has been analyzed using density functional theory (DFT). Further, the establishment of H-bond in the title complex has been investigated with the aid of optimized geomentry, molecular electrostatic potential (MEP) and reduced density gradient (RDG) analysis. The band gap energy of title complex (1:1) is calculated by UV–Vis spectrometer and the same has been justified by HOMO-LUMO studies. Maximum absorption in the UV region and moderate bandgap energy (Eg = 4.22 eV) of the title complex clearly indicates its potential application in NLO, optoelectronics and laser tuning devices. In addition to that, LC parameters and its effect on mesophase are reported using experimental and computational methods.

Discovery and Development of Caffeic Acid Analogs as Versatile Therapeutic Agents

Caffeic acid (CA) is a polyphenolic acid compound widely distributed in plant seeds. As natural compounds with high research interest, caffeic acid and its derivatives show good activity in the treatment of tumors and inflammation and have antibacterial properties. In recent years, caffeic acid derivatives have been studied extensively, and these derivatives fall roughly into three categories: (1) caffeic acid ester derivatives, (2) caffeic acid amide derivatives, (3) caffeic acid hybrids. These caffeic acid analogues exert mainly antibacterial and antioxidant activities. Among the caffeic acid analogues summarized in this paper, compounds 1g and CAP10 have good activity against Candida albicans, and their MIC50 is 32 µg/mL and 13 μM, respectively. In a DPPH assay, compounds 3k, 5a, CS2, Phellinsin A and 8j showed strong antioxidant activity, and their IC50 values are 18.6 μM, 67.85 μM, 40.29 μM, 0.29 ± 0.004 mM, 4774.37 ± 137.20 μM, respectively. Overall, compound CAP10 had the best antibacterial activity and compound 3k had the best antioxidant activity. This paper mainly summarizes and discusses some representative caffeic acid analogs, hoping to provide better drug design strategies for the subsequent development of caffeic acid analogs.

Synthesis, Characterization, and Antimicrobial Evaluation of Thiadiazole Derivatives Derived from 2-Amino-5-Thio-1,3,4-Thiadiazole

This manuscript introduces a series of novel Schiff base and heterocyc-licring compounds, focusing on derivatives of 1,3-oxazepine and thiazo-lidinone.The derivative (2-Hydroxy-N-(5-mercapto-[1,3,4] thiadiazol-2-yl)-2-phenyl-acetamide was created by reacting ethyl mandelate ester[M1] and 2-amino-5-thio-1,3,4-thiadiazole compound to produce new compound [M2] and after that, compound [M2] was reacted with hydrazine hydrate 99% in dry DMF solvent, yielding the compound (N-(5-Hydrazino-[1,3,4]thiadiazol-2-yl)-2-hydroxy-2-phenyl-acetamide [M3]. In contrast , the Schiff base compound [M4] were synthesized by reacting compound [M3] with aromatic heterocyclic aldehyde (furan-2-carbaldehyde) in the presence of glacial acetic acid as a catalyst, and then Schiff base [M4] was reacted with maleic anhydride in dry benzene as a solvent to produce (1,3-Oxazepine) derivative [M5]. Additionally, the thiazolidinone derivative [M6] was synthesized through the reaction of equimolar amounts of (N-[5-(N'-Furan-2-yl-methylene-hydrazino)-[1,3,4]thiadiazol-2-yl]-2-hydroxy-2-phenyl-acetamide [M4] with thioacetic acid compound in chloroform as a solvent. The structural formula of all derivatives was confirmed by FT-IR and (1HNMR, 13CNMR) spectroscopy. The synthesized derivatives [M1-M6] were screened for their evaluated for antibacterial activity against S. aureus, S. epidermidis, E. coli, Klebsiella sp., and the fungus Candida albicans. Dimethyl sulfoxide (DMSO) was used as the solvent. Also, the ampicillin compound was used as the standard drug for comparison.

Anti-Bacterial Potential of Multi-strain Probiotics Lactiplantibacillus plantarum (Strain Dad-13 and FNCC-0250) and Lacticaseibacillus paracasei GMRMP-001 against Escherichia coli FNCC-0091 In Vitro and In Vivo

Lactiplantibacillus plantarum Dad-13, Lactiplantibacillus plantarum FNCC-0250 and Lacticaseibacillus paracasei GMRMP-001 are probiotics strain isolated from Indonesian local and traditional fermented foods. This study aims to evaluate the administration of multi-strain probiotics at dose of 109 CFU/mL/day for 14 days against the diarrhea-causing bacteria Escherichia coli FNCC-0091 at a dose of 1011 CFU/mL/day. Thirty rats were randomized and the divided into 5 groups, including control group, skim milk group, single-strain group, multi-strain group and E. coli group. Antibacterial activity was analyzed in vitro, feed intake, body weight were analyzed, microbial analysis was carried out on feces and cecum, short chain fatty acids were analyzed and intestinal morphology was measured. The result showed that the single-strain and multi-strain inhibition zone in in vitro test produces a very strong inhibitory potential (&gt; 9 mm). The number of L. plantarum and L. paracasei increased and the number of E. coli decreased significantly in the feces and cecum of Rat indicating the survival rate of the probiotic bacteria in the digestive tract and their ability to fight pathogenic bacteria. The concentration of acetic acid, propionic acid and butyric acid compounds also increased, indicating that the digestive tract is at a low pH so that it can inhibit the growth of pathogenic bacteria in rats. In addition, consumption of multi-strain probiotics does not have a negative effect on intestinal morphology. The conclusion is that multi-strain probiotics are able to inhibit pathogenic bacteria in vivo and in vitro. HIGHLIGHTS Multi-strain probiotics isolated from traditional Indonesian fermented foods can reduce the potential for diarrhea. Single-strain and multi-strain have the same effectiveness in inhibiting pathogenic bacteria as seen from the growth of the bacteria. Digestive conditions were damaged in rat that were not given probiotic intervention, but when they received probiotic intervention, digestive conditions improved. GRAPHICAL ABSTRACT