Search Results (14)

There are two major global morbidity and mortality problems in the health sector: inflammation, which is the physiological process that, in acute and chronic conditions, gradually causes the loss of the body’s functionality, leading to severe damage to health; and microbial diseases, which are caused by pathogenic microorganisms such as bacteria. In the present study, the anti-inflammatory effects of three extracts of mesquite (Prosopis laevigata)—n-hexane (PH), dichloromethane (PD), and methanol (PM)—were assessed in a mouse model of 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ear oedema, and the antimicrobial effects against 14 microorganisms were assessed using the broth microdilution method. The extracts inhibited ear oedema by 60.81% (PH), 75.96% (PD), and 60.29% (PM). The most active anti-inflammatory extract (PD) was fractionated through chromatography, and three fractions (PDR3, PDR6, and PDR7) were evaluated. One of the most active fractions (PDR7) was purified via column chromatography, and ethyl veratrate (VE, 1) was isolated and identified. VE inhibited ear oedema by 85.1%. The anti-inflammatory effect is evidenced by the quantification of two pro-inflammatory cytokines (IL-10 and TNF-α). The PD extract, the PDR7 fraction, and the compound present an IL-10 concentration of 11.8, 18.9, and 36.5 pg/mg of protein, values significantly higher than the group that received only phorbol ester (* p < 0.05). These treatments also significantly decreased the concentration of TNF-α (* p < 0.05) to 197.6, 241.9, and 247.0 pg/mg protein, respectively. The PM extract showed the most pronounced antimicrobial effect, with a minimum inhibitory concentration (MIC) of <12.5 µg/mL for almost all the 14 tested strains, followed by the PD and PH extracts. Chromatographic fractionation of the PM extract yielded the PMR6, PMR7, and PMR10 fractions that inhibited all tested microorganisms with a MIC between 6.25 and 200 µg/mL. Compound 1 was active on five strains, with a concentration between 2 and 8 µg/mL. High-performance liquid chromatography analysis and comparison with commercial standards allowed for the identification of rutin (2) and quercetin 3-O-glucoside (3). Gas chromatography–mass spectrometry analysis of the PH and PD extracts allowed for the identification of fatty acids, terpenes, and phenols. Full article

The activation of hair follicle dermal papilla cells (HFDPCs), a critical target of hair loss relief, can be achieved through the upregulation of proliferation, the stimulation of hair inducibility, and the inhibition of cellular senescence. Veratric acid (VA) is a major benzoic acid found in fruits and vegetables. The biological activity of VA on HFDPCs remains to be elucidated. In this study, we investigated the capacity of VA for hair loss mitigation. An MTT assay, Ki67 staining, quantitative RT-PCR (qRT-PCR), and a Western blot analysis were performed to confirm the proliferative effect of VA. Hair inductivity was determined through a cell aggregation assay and ALP staining. Annexin V/PI staining was performed to confirm the anti-apoptotic effect of VA. The inhibitory effect of VA on cellular senescence was confirmed by a β-galactosidase (β-gal) assay and qRT-PCR using replicative senescence and oxidative stress-induced senescence models. As a result, VA dose-dependently upregulated the proliferation of HFDPCs, the expression of growth factors, and β-catenin protein levels. VA also dose-dependently increased ALP activity and cell aggregation and decreased apoptotic cells through the regulation of BCL2 and BAX expression. Moreover, VA reduced β-gal activity and the senescence-associated secretory phenotype (SASP) in a dose-dependent manner in senescent HFDPCs. These findings suggest that VA may serve as a potential therapeutic agent for alleviating hair loss by targeting multiple pathways involved in HFDPC activation. Full article

This research work investigates the effects of the concentration and treatment of chopped false banana (Ensete ventricosum) fibres on the mechanical properties of a polypropylene matrix. The chopped false banana fibres (FBFs) were modified using Aloe Vera gel following treatment with 5% NaOH for 12 h at room temperature, with 1% acetic acid used to neutralise the remaining NaOH. FBF-reinforced polypropylene composite plates were then manufactured with 10, 20, 30, and 40 wt.% of chopped FBF. The mechanical properties were investigated using the compressive, impact, and three-point bending tests. Regarding the mechanical properties of the FBF-reinforced polypropylene composites, it was found that they have a maximum average compressive strength of 17.2 MPa. A maximum bending strength of 12.109 MPa was found for the Aloe Vera gel-treated composite with 30 wt.% of FBF. The maximum average compressive strength for this composite was 17.19 MPa. A maximum bending strength of 9.97 MPa for untreated composites was recorded for the composite with 10 wt.% of FBF. Finally, Aloe Vera-treated FBF-reinforced composites have better mechanical properties than untreated ones. The mechanical properties of Aloe Vera-treated FBF-reinforced polypropylene composites, as determined via impact, compressive and flexural tests, were superior for composites with 30 wt.% of FBF. Full article

(1) Background: this study describes bioactive compounds in the following halophytes: Sarcocornia (S. alpini, S. pruinosa, and S. perennis) and Arthrocnemum (A. macrostachyum). The material comes from: coastal marshes in Tinto River, Guadiana River, and some interior provinces from the Iberian Peninsula. (2) Methods: the techniques used were Folin–Ciocalteu, GC-MS, and ESI-MS/MS. (3) Results: Five phenolic acids were found in Sarcocornia: trans-cinnamic, salicylic, veratric, coumaric, and caffeic acids. In addition, in Arthronemum, ferulic acid was also detected. The obtained flavonoids were cyanidin-3-O-arabinoside, luteolin-7-glucoside, dihydroquercetin, and p-coumaroyl-glucoside. They also presented fatty acids, such as palmitic, linoleic, and oleic acids in Sarcocornia, while palmitic, linolenic, and stearic acids were the main fatty acids in A. macrostachyum. (4) Conclusions: the high diversity of the compounds identified confirms the relation between nutritional interest and salt tolerance in halophytes. Full article

Phenolic acids possess many beneficial biological activities, including antioxidant and anti-inflammatory properties. Unfortunately, their low bioavailability restricts their potential medical uses, as it limits the concentration of phenolic acids achievable in the organism. The conjugation with phospholipids constitutes one of the most effective strategies to enhance compounds bioavailability in biological systems. In the present study, the conjugates of anisic (ANISA) and veratric acid (VA) with phosphatidylcholine (PC) were investigated. Since both ANISA and VA are inhibitors of tyrosinase, a melanocyte enzyme, the expression of which increases during tumorigenesis, anticancer potential of the conjugates was tested in several metastatic melanoma cell lines. The conjugates proved to be antiproliferative, apoptosis-inducing and cell-cycle-affecting agents, selective for cancerous cells and not affecting normal fibroblasts. The conjugates substituted by ANISA and VA, respectively, at both the sn-1 and sn-2 positions of PC, appeared the most promising, since they were effective against the vast majority of metastatic melanoma cell lines. Additionally, the conjugation of phenolic acids to PC increased their antioxidant activity. Molecular modeling was employed for the first time to estimate the features of the investigated conjugates relevant to their anticancer properties and membrane permeation. Again, the conjugates substituted by phenolic acid at both the sn-1 and sn-2 positions of PC seemed to be presumably most bioavailable. Full article

Many halophytes have great nutritional and functional potential, providing chemical compounds with biological properties. Salicornia patula Duval-Jouve is a common euhalophyte from saline Mediterranean territories (Spain, Portugal, France, and Italy). In the present work we quantified for the first time the bioactive compounds in S. patula (total phenolic compounds and fatty acids), from Iberian Peninsula localities: littoral-coastal Tinto River basin areas (southwest Spain, the Huelva province), and mainland continental territories (northwest and central Spain, the Valladolid and Madrid provinces). Five phenolic acids including caffeic, coumaric, veratric, salicylic, and transcinnamic have been found with differences between mainland and coastal saltmarshes. S. patula contain four flavonoids: quercetin-3-O-rutinoside, kaempferol/luteolin, apigenin 7-glucoside, and pelargonidin-3-O-rutinoside. These last two glycosylated compounds are described for the first time in this genus of Chenopodiaceae. The fatty acid profile described in S. patula stems contains palmitic, oleic, and linoleic acids in high concentrations, while stearic and long-chain fatty acids were detected in low amounts. These new findings confirm that S. patula is a valuable source of bioactive compounds from Mediterranean area. Full article

Adipocyte-specific transcription factors and antioxidants are considered the best target of obesity. Aruncus dioicus var. kamtschaticus (A. dioicus, Samnamul) is easily available owing to edible and inexpensive. However, the anti-adipogenic effects of the underlying mechanism of A. dioicus extract (ADE) have not yet been reported. In the present study, we evaluate anti-adipogenic pathway in 3T3-L1 adipocytes, antioxidant activities and quantified phenolics using high-performance liquid chromatography of ADE. The results revealed ADE had reduced adipocyte differentiation (0.72-fold vs. MDI (media of differentiation) control), triglyceride (TG; 0.50-fold vs. MDI control, p < 0.001), and total cholesterol contents (0.77-fold vs. MDI control) by regulating adipocyte-specific transcription factors (C/EBPα, PPARγ, and SREBP1) and their downstream mRNA (AdipoQ, Ap2, SREBP1-c, and FAS) levels. Furthermore, ADE has higher total phenol and flavonoid contents and scavenging assay in the DPPH and ABTS+. In particularly, ADE contains chlorogenic acid (7.04 mg/kg), caffeic acid (20.14 mg/kg), ferulic acid (1.74 mg/kg), veratric acid (29.31 mg/kg), cinnamic acid (4.70 mg/kg), and quercetin (4.18 mg/kg). In conclusion, since these phenols, especially quercetin, in the ADE appear to reduce differentiation, TG and cholesterol content by regulating adipocyte-specific transcription factors in adipocytes, ADE has the potential to be developed into a new antioxidant and anti-obesity therapeutics. Full article

There is increasing interest in the application of bioherbicides because they are less destructive to the global ecosystem than synthetic herbicides. Research has focused on reducing the dependence upon synthetic herbicides by substituting them with environmentally and economically sustainable bioproducts. Allelopathic phytochemicals may be an efficient method for controlling weeds, benefitting both the environment and human health. This study addressed the allelopathic potential of Miscanthus sacchariflorus (MS) extracts on the germination, plant growth, biomass, and biochemical parameters (electrolyte leakage, photosynthetic pigments, and antioxidant enzyme activities) of weeds using laboratory and field experiments. Liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS) showed the presence of 22 phenolic compounds, including Orientin, Luteolin, Veratric acid, Chlorogenic acid, Protocatechuic acid, p-Coumaric acid, and Ferulic acid. Leaf extracts of M. sacchariflorus either completely suppressed or partially reduced seed germination and affected the development of weed seedlings (root and shoot length), in a dose-dependent manner. Aqueous extracts of M. sacchariflorus reduced the fresh weight and dry weight, affected the photosynthetic pigment content (chlorophylls, carotenoids), influenced the electrolyte ion leakage, and stimulated the activity of antioxidant enzymes in a species-specific manner. Pearson’s correlation analysis showed that the phenolic compound composition of M. sacchariflorus correlated with the variables tested, indicating that the phytochemicals present in the plant extracts of M. sacchariflorus are a potential source of bio-herbicides. Full article

A simple, sensitive, and rapid UHPLC-MS/MS method was developed for the simultaneous determination of veratraldehyde and its metabolite veratric acid in rat plasma. Cinnamaldehyde was used as an internal standard (IS) and the one-step protein precipitation method with 0.2% formic acid in acetonitrile (mobile phase B) was used for the sample extraction. Reversed C18 column (YMC-Triart C18 column, 50 mm × 2.0 mm, 1.9 µm) was used for chromatographic separation and was maintained at 30 °C. The total run time was 4.5 min and the electrospray ionization in positive mode was used with the transition m/z 167.07 → 139.00 for veratraldehyde, m/z 183.07 → 139.00 for veratric acid, and m/z 133.00 → 55.00 for IS. The developed method exhibited good linearity (r²  ≥  0.9977), and the lower limits of quantification ranged from 3 to 10 ng/mL for the two analytes. Intra-day precision and accuracy parameters met the criteria (within ±15%) during the validation. The bioanalytical method was applied for the determination of veratraldehyde and veratric acid in rat plasma after oral and percutaneous administration of 300 and 600 mg/kg veratraldehyde. Using the analytical methods established in this study, we can confirm the absorption and metabolism of veratraldehyde in rats for various routes. Full article

Lipase-catalyzed acidolysis reactions of egg-yolk phosphatidylcholine (PC) with anisic (ANISA) and veratric (VERA) acids were investigated to develop a biotechnological method for the production of corresponding biologically active O-methylated phenophospholipids. Screening experiments with four commercially available immobilized lipases indicated that the most effective biocatalyst for the incorporation of ANISA into phospholipids was Novozym 435. None of the tested enzymes were able to catalyze the synthesis of PC structured with VERA. The effects of different solvents, substrate molar ratios, temperature, enzyme loading, and time of the reaction on the process of incorporation of ANISA into the phospholipids were evaluated in the next step of the study. The mixture of toluene/chloroform in the ratio 9:1 (v/v) significantly increased the incorporation of ANISA into PC. The acidolysis reaction was carried out using the selected binary solvent system, 1/15 substrate molar ratio PC/ANISA, 30% (w/w) enzyme load, and temperature of 50 °C afforded after 72 h anisoylated lysophosphatidylcholine (ANISA-LPC) and anisoylated phosphatidylcholine (ANISA-PC) in isolated yields of 28.5% and 2.5% (w/w), respectively. This is the first study reporting the production of ANISA-LPC and ANISA-PC via a one-step enzymatic method, which is an environmentally friendly alternative to the chemical synthesis of these biologically active compounds. Full article

A considerable amount of bioactive compounds have been used for the biopharmaceutical engineering to help human health and nutrition. Hairy root culture (HRC) or transgenic root is a favourable alternative technique for phytochemical production. Ligularia fischeri is a significant source of pharmaceutically important active compounds with an enormous range of health care applications. HRC of L. fischeri was developed using Agrobacterium rhizogenes for the production of polyphenolic compounds with antioxidant, antimicrobial, antidiabetic, anticancer and anti-inflammatory pharmaceutical activities. Hairy roots (HRs) were selected by morphological assessment, genetic and molecular analyses. The maximum accumulation of fresh mass (94.15 g/L) and dry mass (9.45 g/L) was recorded in MS liquid medium supplemented with 30 g/L sucrose at 28 days. Furthermore, HRs successfully produced numerous polyphenolic compounds, including six hydroxycinnamic acids, seven flavonols, seven hydroxybenzoic acids, vanillin, resveratrol, pyrogallol, homogentisic, and veratric acids, which were identified by UHPLC analysis. HRs produced higher total phenolic (185.65 mg/g), and flavonoid (5.25 mg/g) contents than non-transformed roots (125.55 mg/g and 3.75 mg/g). As a result of these metabolic changes, pharmaceutical activities were found higher in HRs than non-transformed roots (NTRs). The present study indicates that HRC has the potential to increase the content of beneficial polyphenolic compounds with higher potential pharmaceutical activities. To the best of our knowledge, the present study is the first report on enhancing the production of polyphenolic compounds with pharmaceutical activities from the HRCs of L. fischeri. Full article

Phenolic acids and its methoxy derivatives are known to induce caspase-mediated apoptosis activity and exhibit cytotoxic effect towards various cancer cell lines. However, their low stability and poor bioavailability in the human organism extensively restrict the utility of this group of compounds as anticancer and health-promoting agents. In this report, a series of eight novel phosphatidylcholines (3a-b, 5a-b, 7a-b, 8a-b) containing anisic or veratric acids (1a-b) at sn-1 and/or sn-2 positions were synthesized. The phenoylated phospholipids were obtained in good yields 28–66%. The structures of novel compounds were determined by their spectroscopic data. All synthesized compounds were evaluated for their antiproliferative activity towards six cancer cell lines and normal cell line Balb/3T3. Lipophilization of phenolcarboxylic acids significantly increased their anticancer properties. The asymmetrically substituted phenoylated phosphatidylcholines exhibited higher antiproliferative effect than free acids. Lysophosphatidylcholine (7b) effectively inhibited the proliferation of human leukaemia (MV4-11), breast (MCF-7), and colon (LoVo) cancer cell lines at concentrations of 9.5–20.7 µm and was from 19 to 38-fold more active than corresponding free veratric acid. The conjugation of anisic/veratric acids with the phosphatidylcholine have proved the anticancer potential of these phenolcarboxylic acids and showed that this type of lipophilization is an effective method for the production of active biomolecules. Full article

Ultraviolet (UV) radiation induces DNA damage, oxidative stress, and inflammatory processes in human epidermis, resulting in inflammation, photoaging, and photocarcinogenesis. Adequate protection of skin against the harmful effect of UV irradiation is essential. In recent years naturally occurring herbal compounds such as phenolic acids, flavonoids, and high molecular weight polyphenols have gained considerable attention as beneficial protective agents. The simple phenolic veratric acid (VA, 3,4-dimethoxybenzoic acid) is one of the major benzoic acid derivatives from vegetables and fruits and it also occurs naturally in medicinal mushrooms which have been reported to have anti-inflammatory and anti-oxidant activities. However, it has rarely been applied in skin care. This study, therefore, aimed to explore the possible roles of veratric acid in protection against UVB-induced damage in HaCaT cells. Results showed that veratric acid can attenuate cyclobutane pyrimidine dimers (CPDs) formation, glutathione (GSH) depletion and apoptosis induced by UVB. Furthermore, veratric acid had inhibitory effects on the UVB-induced release of the inflammatory mediators such as IL-6 and prostaglandin-E2. We also confirmed the safety and clinical efficacy of veratric acid on human skin. Overall, results demonstrated significant benefits of veratric acid on the protection of keratinocyte against UVB-induced injuries and suggested its potential use in skin photoprotection. Full article

A bulk polymerization method was used to easily and efficiently prepare homo-veratric acid (3,4-dimethoxyphenylacetic acid)-imprinted polymers from eight basic monomers: 2-vinylpyridine, 4-vinylpyridine, 1-vinylimidazole, N-allylaniline, N-allylpiperazine, allylurea, allylthiourea, and allylamine, in the presence of homoveratric acid as a template in N,N-dimethylformamide as a porogen. The imprinted polymer prepared from allylamine had the highest affinity to the template, showing an imprinting factor of 3.43, and allylamine polymers MIP8/NIP8 were selected for further studies. Their binding properties were analyzed using the Scatchard method. The results showed that the imprinted polymers have two classes of heterogeneous binding sites characterized by two pairs of K_d, B_max values: K_d(1) = 0.060 μmol/mL, B_max(1) = 0.093 μmol/mg for the higher affinity binding sites, and K_d(2) = 0.455 μmol/mL, B_max(2) = 0.248 μmol/mg for the lower affinity binding sites. Non-imprinted polymer has only one class of binding site, with K_d = 0.417 μmol/mL and B_max = 0.184 μmol/mg. A computational analysis of the energies of the prepolymerization complexes was in agreement with the experimental results. It showed that the selective binding interactions arose from cooperative three point interactions between the carboxylic acid and the two methoxy groups in the template and amino groups in the polymer cavities. Those results were confirmed by the recognition studies performed with the set of structurally related compounds. Allylamine polymer MIP8 had no affinity towards biogenic amines. The obtained imprinted polymer could be used for selective separation of homoveratric acid. Full article