Phenylpropionic Acid Research Articles

Secondary Metabolite Profile and Pharmacological Opportunities of Lettuce Plants following Selenium and Sulfur Enhancement.

Selenium (Se) is an essential trace nutrient for humans and animals owing to its role in redox regulation, thyroid hormone control factors, immunity, inflammatory reactions, brain activities, and carbohydrate regulation. It is also important to support muscle development, as well as for reproductive and cardiovascular well-being. Furthermore, sulfur is known to be a healing element, due to the remarkable function of specialized and secondary S-containing compounds. The scope of the current study was to determine the impact of Se and S enrichment on the secondary metabolite accumulation and antibacterial and NO inhibition activities in green and red leaf lettuce (V1 and V2, respectively). The plants were grown in a hydroponic system supplied with different S concentrations (S0: 0, S1: 1 mM and S2: 1.5 mM K2SO4) via the nutrient solution and foliar-applied varying levels of Se (0, 0.2 and 2.6 µM). Electrospray ionization-quadrupole time-of-flight mass spectrometry (ESI-QTOF/MS) combined with ultra-performance liquid chromatography (UPLC) was used to identify the secondary metabolites in green and red lettuce. The results indicated that extracts of the biofortified lettuce were not cytotoxic to Vero kidney cells at the highest concentration tested of 1 mg/mL. The ESI/MS of the tentatively identified metabolites showed that the response values of 5-O-caffeoylquinic acid, cyanidin 3-O-galactoside, quercetin 3-O-(6''-acetyl-glucoside) and quercetin 3-O-malonylglucoside were induced synergistically under higher Se and S levels in red lettuce plants. The acetone extract of red lettuce had antibacterial activity against Pseudomonas aeruginosa, with a minimum inhibitory concentration (MIC) of 0.156 and 0.625 μg/mL under S2/Se1 and S2/Se2 treatments, respectively. As with antibacterial activity, the acetone extract of green (V1) lettuce treated with adequate (S1) and higher S (S2) under Se-limiting conditions showed the ability to inhibit nitric oxide (NO) release from macrophages. NO production by macrophages was inhibited by 50% at respective concentrations of 106.1 ± 2.4 and 101.0 ± 0.6 μg/mL with no toxic effect on the cells, in response to S1 and S2, respectively, under Se-deficient conditions (Se0). Furthermore, the red cultivar (V2) exhibited the same effect as the green cultivar (V1) regarding NO inhibition, with IC50 = 113.0 ± 4.2 μg/mL, in response to S1/Se2 treatments. Collectively, the promising NO inhibitory effect and antibacterial activity of red lettuce under the above-mentioned conditions might be attributed to the production of flavonoid glycosides and phenylpropanoic acid esters under the same condition. To the best of our knowledge, this is the first report to show the novel approach of the NO inhibitory effect of Se and S enrichment in food crops, as an indicator for the potential of Se and S as natural anti-inflammatory agents.

Green diastereospecific synthesis of various medicine analogues containing dipeptides and release of the medicines by Baker's yeast

We have succeeded green and economical synthesis of various dipeptides in 76–99% yields with 70–>99% de and dipeptides-containing medicine analogues in 74–99% yields with 79–97% de in aqueous THF at −15 °C via the mixed carbonic carboxylic anhydrides by the activation of the corresponding carboxylic acids. We observed that the anilide l-Phe-l-Phe-NHC6H4-4-OH, one of the deprotecting medicine analogues, was cleaved at the C-terminal of l-phenylalanine (l-Phe) by Baker's yeast under starvation conditions followed by treatment of a freshly prepared PhCH2CH2CO2CO2Et from 3-phenylpropanoic acid, ClCO2Et, and Et3N in MeCN to afford PhCH2CH2CONHC6H4-4-OH and PhCH2CH2CO-l-Phe-NHC6H4-4-OH in 46% and 42% yields, respectively. Interestingly, biocatalytic hydrolysis of l-Phe-d-Phe-NHC6H4-4-OH by Baker's yeast gave PhCH2CH2CO-d-Phe-NHC6H4-4-OH in 20% yield and PhCH2CH2CO-l-Phe-d-Phe-NHC6H4-4-OH 60% recovery yield.

Identification of Allelochemicals with Differential Modes of Phytotoxicity against Cuscuta campestris

Cuscuta campestris is a parasitic weed species with noxious effects in broadleaf crops worldwide. The control of Cuscuta in the majority of crops affected is limited or non-existing. We tested, for the first time, the effect of eighteen metabolites in in vitro-grown Cuscuta seedlings. We found that 2-benzoxazolinone, hydrocinnamic acid and pisatin caused the strongest inhibition of seedling growth. In addition to seedling growth, pisatin caused necrosis of the Cuscuta seedling, occurring mostly at the seedling shoot. Scopoletin and sesamol treatments caused toxicity, observed as a black staining, only at the Cuscuta root apices, while caffeic acid, ferulic acid and vanillic acid caused toxicity, observed as brown staining, in the root apices. The structure–activity relationships in four structural derivatives of 2-benzoxazolinone, and five structural derivatives of hydrocinnamic acid, were also studied. The identification of new herbicidal modes of action against Cuscuta is the first step in creating new alternatives to sustainable chemical control of parasitic weeds.

Moldavica acid A, a new salicylic acid derivative from Dracocephalum moldavica

In this paper, we present the discovery of a novel salicylic acid derivative, moldavica acid A (1), and a new natural dibenzo[b,f]oxepin, moldavica acid B (2), together with four known phenylpropionic acids (3-6) and protocatechuic acid (7) that were isolated from Dracocephalum moldavica L. Their structures were elucidated by comprehensive spectroscopic methods, including infrared and nuclear magnetic resonance. Compound 1 is the first example of salicylic acid linking a carboxylated α-pyrone via an ethyl bridge. Beyond expanding the knowledge of the chemical diversity of D. moldavica, both compounds 1 and 2 were shown to upregulate the expression of Kruppel-like factor 2, which could serve as a prospective therapeutic target for the treatment of atherosclerosis.

Asymmetric Remote meta-C–H Activation Controlled by a Chiral Ligand

The use of a chiral ligand for stereocontrol has assisted the development of a number of asymmetric functionalization of proximal C–H bonds. Herein, we report a chiral ligand-controlled, asymmetric remote meta-C–H activation of arenes, leading to asymmetric C–H olefination and arylation of hydrocinnamic acid derivatives through desymmetrization with Ac-L-Phe-OH as the chiral ligand using a Pd(II) catalyst. The origins of the enantioselectivity were explained with density functional theory calculations. The larger distortion energy of the substrate part in the C–H bond activation transition structure S-TS1 is the major controlling factor that disfavors the formation of the S-enantiomer product.

Isocitrate binds to the itaconic acid–responsive LysR-type transcriptional regulator RipR in Salmonella pathogenesis

Macrophages produce itaconic acid in phagosomes in response to bacterial cell wall component lipopolysaccharide to eliminate invading pathogenic bacteria. Itaconic acid competitively inhibits the first enzyme of the bacterial glyoxylate cycle. To overcome itaconic acid stress, bacteria employ the bacterial LysR-type transcriptional regulator RipR. However, it remains unknown which molecule activates RipR in bacterial pathogenesis. In this study, we determined the crystal structure of the regulatory domain of RipR from the intracellular pathogen Salmonella. The RipR regulatory domain structure exhibited the typical dimeric arrangement with the putative ligand-binding site between the two subdomains. Our isothermal titration calorimetry experiments identified isocitrate as the physiological ligand of RipR, whose intracellular level is increased in response to itaconic acid stress. We further found that 3-phenylpropionic acid significantly decreased the resistance of the bacteria to an itaconic acid challenge. Consistently, the complex structure revealed that the compound is antagonistically bound to the RipR ligand-binding site. This study provides the molecular basis of bacterial survival in itaconic acid stress from our immune systems. Further studies are required to reveal biochemical activity, which would elucidate how Salmonella survives in macrophage phagosomes by defending against itaconic acid inhibition of bacterial metabolism.

Quantification of Gut Microbiota Dysbiosis-Related Organic Acids in Human Urine Using LC-MS/MS.

Urine organic acid contains water-soluble metabolites and/or metabolites—derived from sugars, amino acids, lipids, vitamins, and drugs—which can reveal a human’s physiological condition. These urine organic acids—hippuric acid, benzoic acid, phenylacetic acid, phenylpropionic acid, 4-hydroxybenzoic acid, 4-hydroxyphenyl acetic acid, 3-hydroxyphenylpropionic acid, 3,4-dihydroxyphenyl propionic acid, and 3-indoleacetic acid—were the eligible candidates for the dysbiosis of gut microbiota. The aim of this proposal was to develop and to validate a liquid chromatography–tandem mass spectrometry (LC-MS/MS) bioanalysis method for the nine organic acids in human urine. Stable-labeled isotope standard (creatinine-d3) and acetonitrile were added to the urine sample. The supernatant was diluted with deionized water and injected into LC-MS/MS. This method was validated with high selectivity for the urine sample, a low limit of quantification (10–40 ng/mL), good linearity (r > 0.995), high accuracy (85.8–109.7%), and high precision (1.4–13.3%). This method simultaneously analyzed creatinine in urine, which calibrates metabolic rate between different individuals. Validation has been completed for this method; as such, it could possibly be applied to the study of gut microbiota clinically.

Expression of a Hydroxycinnamoyl-CoA Shikimate/Quinate Hydroxycinnamoyl Transferase 4 Gene from Zoysia japonica (ZjHCT4) Causes Excessive Elongation and Lignin Composition Changes in Agrostis stolonifera.

Hydroxycinnamoyl-CoA shikimate/quinate hydroxycinnamoyl transferase (HCT) is considered to be an essential enzyme for regulating the biosynthesis and composition of lignin. To investigate the properties and function of ZjHCT4, the ZjHCT4 gene was cloned from Zoysia japonica with a completed coding sequence of 1284-bp in length, encoding 428 amino acids. The ZjHCT4 gene promoter has several methyl jasmonate (MeJA) response elements. According to analysis of expression patterns, it was up-regulated by MeJA, GA3 (Gibberellin), and SA (Salicylic acid), and down-regulated by ABA (Abscisic acid). Ectopic ZjHCT4 expression in creeping bentgrass causes excessive plant elongation. In addition, the content of G-lingnin and H-lingnin fell in transgenic plants, whereas the level of S-lingnin increased, resulting in a considerable rise in the S/G unit ratio. Analysis of the expression levels of lignin-related genes revealed that the ectopic expression of ZjHCT4 altered the expression levels of a number of genes involved in the lignin synthesis pathway. Simultaneously, MeJA, SA, GA3, IAA, BR (Brassinosteroid), and other hormones were dramatically enhanced in transgenic plants relative to control plants, whereas ABA concentration was significantly decreased. Expression of ZjHCT4 impacted lignin composition and plant growth via altering the phenylpropionic acid metabolic pathway and hormone response, as revealed by transcriptome analysis. HCTs may influence plant lignin composition and plant development by altering hormone content. These findings contributed to a deeper comprehension of the lignin synthesis pathway and set the stage for further investigation and application of the HCTs gene.

Synthesis of benzo-condensed cyclic cathinone derivatives

Recently, the number of new psychoactive substances (NPS), which are sold as legal alternatives to conventional or misused drugs, has been growing on the market. Via small chemical modifications in the basic structure of the already banned substances, new derivatives are made. Although they pose a real threat to human health, they do circumvent regulation system. This fact led us to formulate the aim of this work, which is the synthesis of cyclic derivatives of cathinones, substances that are derived from natural substance S-cathinone. All commercial reagents and solvents were used without additional purification. 1H NMR and 13 C NMR spectra measured for structure conformation were acquired on an Agilent 400-MR DDR2 spectrometer with CDCl3 or CH3OD as the solvent. Cyclic derivatives of cathinone with different size of benzo-condensed ring were prepared using different synthetic approaches optimised to maximum possible yields. The first intermediate with a six membered condensed ring was synthesised using a nucleophilic addition of an aryllithium on cyclobutanone to form corresponding cyclobutanol derivative. This alcohol was transferred to an α-tetralone system using a radical cyclization reaction with potassium peroxodisulfate and silver nitrate. A cycliclization reaction of differently substituted 4-arylbutanoic acids employing polyphosphoric acid was used as a second approach. Also, five and four membered condensed ring derivatives were synthesised using two different approaches. The first approach was based on Friedel-Crafts acylation, where phenylpropanoic and phenylethanoic acid were converted to chlorides using oxalyl chloride, then using aluminium (III) chloride as a catalyst the intramolecular ring-closing reaction was completed. The second approach was cyclization of acids by means of thionyl chloride and trifluoromethanesulfonic acid. The benzocycloheptane ring was prepared using all cyclization reactions mentioned above. All the above-described intermediates were subsequently subjected to the sequence of reactions to prepare the final derivatives. A reaction of cyclic ketones with isoamyl nitrite provided oximes which were reduced with zinc dust in acetic acid to form acetamides. These acetamides were hydrolysed using hydrochloric acid yielding corresponding amines. These amines were transformed to trifluoroacetamides, which were methylated using iodomethane and the final step, acid hydrolysis gave rise to the target N-methylated cyclic derivatives. Different approaches towards the synthesis of benzocondensed bicyclic ketones with various sizes of the aliphatic ring are presented. These compounds have been used as intermediates to prepare new cyclic cathinones and their formal metabolites (N-demethylated derivatives). All the novel substances are fully characterized and, moreover, the possibility of their chiral separation using HPLC is being studied to assign their absolute configuration and study the biological activity of enantiomers.

Enhancing the prebiotic and antioxidant effects of exopolysaccharides derived from Cordyceps militaris by enzyme-digestion

Cordyceps militaris is an edible and potentially medicinal mushroom. It contains various biologically active compounds, including exopolysaccharides. In this study, the abilities as antioxidants and prebiotics of exopolysaccharides of C. militaris (CMP) and its low-molecular-weight polysaccharide of CMP (LCMP) obtained using glycoside hydrolase digestion were investigated. CMP and LCMP had obvious DPPH, ABTS, and hydroxyl radical scavenging activities of 13.71%, 38.33% and 23.94%, and 30.36%, 69.32% and 43.82%, respectively, at a concentration of 1 mg/mL. In the gut microbiota consortium, treatment with CMP or LCMP increased Bacteroidetes growth and decreased Firmicutes/Bacteroidetes ratios, compared with the negative or glucose-treated controls. Based on changes in the consortium, the media treated with CMP and LCMP had increases in acetic, lactic, and 2-hydroxyisocaproic acid metabolites. In particular, LCMP-treated media had increases in production of two phenolic acids, benzoic acid and hydrocinnamic acid. Prebiotic activity tests found that CMP and LCMP had growth-promoting activities (mean values 0.34–0.77 and 0.46–0.95, respectively) similar to those of inulin (mean values 0.43–1.11). These results indicated that LCMP was a beneficial antioxidant and an excellent prebiotic that enhanced proliferation of probiotics and phenolic acid abundance. This may provide a basis for the understanding of the effects of prebiotics on health. KeywardsCordyceps militaris, Exopolysaccharides (EPS), Prebiotics, Short-chain fatty acids (SCFAs), Phenolic acids.

Two dimers generated by lithospermic decarboxylation coupling from Danshen

To further reveal the active ingredients of Danshen, we systematically studied its chemical components and obtained two new lithospermic acid derivatives (compounds 1 and 2) together with five known phenylpropionic acids (compounds 3–7) from the dried rhizomes of Salvia miltiorrhiza. The structures of the two new compounds were determined by multiple spectral analyses (UV, IR, HR-ESI-MS, NMR, and ECD). In addition, the absolute configurations were established by chiral analysis and calculated and experimental circular dichroism spectra. Biological research indicated that compound 1 could significantly inhibit the proliferation of isoproterenol (ISO)-treated cardiac fibroblasts (AC16 cells), and MMP9 was found to be the most likely target of compound 1. The protein expression and mRNA levels of MMP9 were increased in ISO-induced AC16 cells, which could be reversed by treatment with compound 1. Furthermore, this treatment could alleviate the migration and activation of ISO-induced cardiac fibroblasts.

Screening of potent α-glucosidase inhibitory and antioxidant polyphenols in Prunella vulgaris L. by bioreaction-HPLC-quadrupole-time-of-flight-MS/MS and in silico analysis.

Prunella vulgaris L. is a well-known traditional Chinese medicine for blood glucose homeostasis and antioxidant potential. Ethyl acetate fraction of P. vulgaris L. demonstrated higher phenolic content (85.53 ± 6.74mg gallic acid equivalents per gram dry weight), α-glucosidase inhibitory (IC50 , 69.13 ± 2.86 μg/ml), and antioxidant (IC50 , 8.68 ± 1.01 μg/ml) activities. However, the bioactive polyphenols responsible for the beneficial properties remain unclear. Here, bioreaction-HPLC-quadrupole-time-of-flight-MS/MS method was developed for rapid, accurate, and efficient screening and identification of polyphenols with α-glucosidase inhibitory and antioxidant activities from P. vulgaris L. Bioactive polyphenols can specifically bind with α-glucosidase or react with 1,1-diphenyl-2-picryl-hydrazyl radical, which was easily discriminated from nonactive compounds. Subsequently, 20 bioactive polyphenols (16 phenyl propionic acid derivatives and four flavonoids) were screened and identified. Furthermore, molecular docking analysis revealed that screened 20 polyphenols bind with the active sites of α-glucosidase through hydrogen bonding and π-π stacking. Density functional theory calculations demonstrated their electron transport ability and chemical reactivity. The in silico analysis confirmed the screened results. In summary, this study provided a valuable strategy for rapid discovering bioactive compounds from complex natural products and offered scientific evidence for further development and application of P. vulgaris L.

A complementary chromatographic strategy for integrated components characterization of Imperatae Rhizoma based on convergence and liquid chromatography combined with mass spectrometry and molecular network

The complexity of natural ingredients and the diversity of preparations are the major obstacles to the quality evaluation of traditional Chinese medicines (TCMs). A more comprehensive characterization of herbal compounds using different types of chromatographic separation techniques and covering a diverse polarity range can help evaluate the quality of TCMs. In this study, we first proposed a comprehensive method for characterizing compounds derived from Imperatae Rhizoma by combining the complementary strengths of UPCC-QTOF-MS (ultra-performance convergence chromatography coupled with quadrupole-time of flight mass spectrometry) with UPLC-QTOF-MS (ultra-performance liquid chromatography coupled with quadrupole-time of flight mass spectrometry). The method based on the UNIFI scientific platform significantly shortened the analysis time and enabled a more comprehensive characterization of known and unreported compounds. Meanwhile, a feature-based molecular network (FBMN) was established on the Global Natural Product Social (GNPS) to infer potential compounds by rapidly classifying and visualizing these components. A total of 62 compounds in Imperatae Rhizoma were jointly characterizedand classified into six types. In comparison, the UPCC-QTOF-MS technology individually characterized 17 components, including lactones, phenols, aldehydes, phenylpropanoids, and small polar organic acids. The UPLC-QTOF-MS technology characterized 16 compounds mainly phenylpropionic acids, flavonoid glycosides, and chromone glycosides. Furthermore, three types of characteristic compounds could be well aggregated into an FBMN approach. Five possible potential new compounds were detected through the supplementary identification of GNPS and the correlation analysis of vicinal known compounds. The strategy was first applied to Imperatae Rhizoma and facilitated the characterization of a large quantity of data to provide comprehensive chemical composition results. This approach can be easily extended to the study of the material basis of other herbs or preparations in order to improve the accuracy of herb quality evaluation.

Intrinsic Ability of the β-Oxidation Pathway To Produce Bioactive Styrylpyrones.

Naturally occurring α‐pyrones with biological activities are mostly synthesised by polyketide synthases (PKSs) via iterative decarboxylative Claisen condensation steps. Remarkably, we found that some enzymes related to the fatty acid β‐oxidation pathway in Escherichia coli, namely the CoA ligase FadD and the thiolases FadA and FadI, can synthesise styrylpyrones with phenylpropionic acids in vivo. The two thiolases directly utilise acetyl‐CoA as an extender unit for carbon‐chain elongation through a non‐decarboxylative Claisen condensation, thus making the overall reaction more efficient in terms of carbon and energy consumption. Moreover, using a cell‐free approach, different styrylpyrones were synthesised in vitro. Finally, targeted feeding experiments led to the detection of styrylpyrones in other species, demonstrating that the intrinsic ability of the β‐oxidation pathway allows for the synthesis of such molecules in bacteria, revealing an important biological feature hitherto neglected.

Intrinsic Ability of the β‐Oxidation Pathway To Produce Bioactive Styrylpyrones

AbstractNaturally occurring α‐pyrones with biological activities are mostly synthesised by polyketide synthases (PKSs) via iterative decarboxylative Claisen condensation steps. Remarkably, we found that some enzymes related to the fatty acid β‐oxidation pathway in Escherichia coli, namely the CoA ligase FadD and the thiolases FadA and FadI, can synthesise styrylpyrones with phenylpropionic acids in vivo. The two thiolases directly utilise acetyl‐CoA as an extender unit for carbon‐chain elongation through a non‐decarboxylative Claisen condensation, thus making the overall reaction more efficient in terms of carbon and energy consumption. Moreover, using a cell‐free approach, different styrylpyrones were synthesised in vitro. Finally, targeted feeding experiments led to the detection of styrylpyrones in other species, demonstrating that the intrinsic ability of the β‐oxidation pathway allows for the synthesis of such molecules in bacteria, revealing an important biological feature hitherto neglected.

Enhanced degradation of quinoline in near-neutral pH aqueous solution by magnetically recoverable biochar: Performance, mechanism and variables effects

BackgroundQuinoline is a highly toxic nitrogen-containing heterocyclic organic compound. Iron-carbon microelectrolysis is a potential method for treating quinoline in aqueous solution, but commercially available iron-carbon fillers (ICF) are difficult to recover from aqueous solution and have extremely poor degradation effects on near-neutral pH quinoline solution. MethodsIn this study, the magnetically recoverable biochar (MR-BC) was prepared by impregnation-pyrolysis method and used to enhance the degradation of quinoline in near-neutral pH aqueous solution. Significant findingsThe highest removal rate of 1.00 g MR-BC to 50 mg·L−1 quinoline wastewater can reach 99.98% within one hour, while ICF only removes 7.03% of quinoline. Nontoxic hydro-cinnamic acid and cinnamic acid are the main degradation products of quinoline by the MR-BC in near-neutral pH aqueous solution. It is supposed that the degradation process is a result of synergistic effects between MR-BC and quinoline molecules, such as chemical adsorption (π-π and hydrogen bond), electrostatic attraction, reactive oxygen species (ROS) oxidation and atomic hydrogen ([H]) reduction. In addition, the kinetic fitting results indicated that the degradation of quinoline by MR-BC is more consistent with pseudo-second-order kinetics.

Biocatalytic hydrolysis of various esters using Baker’s yeast under neutral conditions without sucrose

We have found that biocatalytic hydrolysis of various esters using Baker’s yeast proceeds efficiently under neutral conditions without sucrose. Hydrolysis of ethyl, methyl, propyl, isopropyl, benzyl, allyl, prenyl, and vinyl esters of 3-phenylpropanoic acid using Baker’s yeast gave easily 3-phenylpropanoic acid in 52–86% yields. In contrast, Baker’s yeast did not hydrolyze the rigid structural esters such as cinnamyl and phenyl 3-phenylpropanoates. Then, Baker’s yeast hydrolyzed various ethyl esters of 3-arylpropanoic acids, 4-phenylbutanoic acid, and fatty acids to afford the corresponding acids in 29–85% yields.

Isophthaloylbis (Azanediyl) Dipeptide Ligand and Its Complexes: Structural Study, Spectroscopic, Molecular Orbital, Molecular Docking, and Biological Activity Properties

The ligand 2,2′-(isophthaloylbis(azanediyl))bis(3-phenylpropanoic acid; H2L) was used to build novel metal complexes of Co(II), Ni(II), Fe(III), and Zn(II) metal ions. Elemental analyses, thermal, infrared, mass, electronic spectra, magnetic moments, X-ray diffraction analysis, and conductivity measurements were used to predict the nature of bonding and the stereochemistry of the complexes. The complexes were proposed to have the general formula [M(H2L)(H2O)2]Cl n , where M = Co(II), Ni(II), and Zn(II) (n = 2) and Fe(III) (n = 3), based on the elemental analyses data. All of the complexes were electrolytes, according to the molar conductivity measurements. The FT-IR spectra revealed that the dipeptide ligand is tetradentately coordinated to metal ions, with NNOO donor atoms participating in coordination with metal (II)/(III) ions, resulting in octahedral complexes. Using the recommended programme, the structural formula for the investigated ligand was optimized. Using the density-functional theory (DFT) approach, the energy gaps and other essential theoretical parameters were calculated. The agar diffusion method was used to test the in vitro biological characteristics of the ligand (H2L) and its transition metal complexes against Gram(+) bacteria (Bacillis subtilis and Staphylococcus aureus) and Gram(−) bacteria (Escherichia coli and Pseudomonas aeruginosa). The title compounds were found to be more biologically active than the parent dipeptide ligand. The title compounds have a good interaction with the crystal structures of 3t88-Escherichia coli, 3ty7-S. aureus, 5h67-Bacillus subtilis, and 5i39-Pseudomonasaeruginosa, according to molecular docking study.

Ibuprofen Nanoemulsion as a Promising Drug Delivery Strategy

Phenyl propionic acid derivative drug Ibuprofen was selected for the study’s model medication. It is hypothesized that nanoemulsion might be a useful medication delivery method for enhancing oral absorption. According to the findings, the nanoemulsion formulation greatly enhanced the drug’s anti-inflammatory capabilities when compared to the Ibuprofen solution. Ibuprofen’s solubility and oral bioavailability are enhanced using nanoemulsion technology. To evaluate and pinpoint nanoemulsion area’s are made of glycerol, olive oil, and various sucrose esters, a pseudo ternary phase diagram was created (co-surfactant). Following the discovery of such a nanoemulsion zone, a colloidal system was created to serve as an ibuprofen carrier system. Droplet size, polydispersity index, zeta potential, and morphological measurements were made to determine the characteristics of the chosen nanoemulsion (NE) area.

DAF-16 is involved in colonic metabolites of ferulic acid-promoted longevity and stress resistance of Caenorhabditis elegans.

Ferulic acid (FA) is a dietary polyphenol widely found in plant tissues. It has long been considered to have health-promoting qualities. However, the biological properties of dietary polyphenols depend largely on their absorption during digestion, and the effects of their intestinal metabolites on human health have attracted the interest of researchers. This study evaluated the effects of three main colonic metabolites of FA - 3-(3,4-dihydroxyphenyl)propionic acid (3,4diOHPPA), 3-(3-hydroxyphenyl)propionic acid (3OHPPA) and 3-phenylpropionic acid (3PPA) - on longevity and stress resistance in Caenorhabditis elegans. Our results showed that 3,4diOHPPA, 3OHPPA and 3PPA extended the lifespan under normal conditions in C. elegans whereas FA did not. High doses of 3,4diOHPPA (0.5 mmol L-1 ), 3OHPPA (2.5 mmol L-1 ) and 3PPA (2.5 mmol L-1 ) prolonged the mean lifespan by 11.2%, 13.0% and 10.6%, respectively. Moreover, 3,4diOHPPA, 3OHPPA and 3PPA treatments promoted stress tolerance against heat, UV irradiation and paraquat. Furthermore, three metabolites ameliorated physical functions, including reactive oxygen species and malondialdehyde levels, motility and pharyngeal pumping rate. The anti-aging activities mediated by 3,4diOHPPA, 3OHPPA and 3PPA depend on the HSF-1 and JNK-1 linked insulin/IGF-1 signaling pathway, which converge onto DAF-16. The current findings suggest that colonic metabolites of FA have the potential for use as anti-aging bioactivate compounds. © 2022 Society of Chemical Industry.