Compounds Caffeic Acid Research Articles

Neuroprotective Effects of Phenolic Constituents from Drynariae Rhizoma.

This study aimed to provide scientific data on the anti-Alzheimer's disease (AD) effects of phenolic compounds from Drynariae Rhizoma (DR) extract using a multi-component approach. Screening of DR extracts, fractions, and the ten phenolic compounds isolated from DR against the key AD-related enzymes acetylcholinesterase (AChE), butyrylcholinesterase (BChE), β-site amyloid precursor protein cleaving enzyme 1 (BACE1), and monoamine oxidase-B (MAO-B) confirmed their significant inhibitory activities. The DR extract was confirmed to have BACE1-inhibitory activity, and the ethyl acetate and butanol fractions were found to inhibit all AD-related enzymes, including BACE1, AChE, BChE, and MAO-B. Among the isolated phenolic compounds, compounds (2) caffeic acid 4-O-β-D-glucopyranoside, (6) kaempferol 3-O-rhamnoside 7-O-glucoside, (7) kaempferol 3-o-b-d-glucopyranoside-7-o-a-L-arabinofuranoside, (8) neoeriocitrin, (9) naringin, and (10) hesperidin significantly suppressed AD-related enzymes. Notably, compounds 2 and 8 reduced soluble Amyloid Precursor Protein β (sAPPβ) and β-secretase expression by over 45% at a concentration of 1.0 μM. In the thioflavin T assay, compounds 6 and 7 decreased Aβ aggregation by approximately 40% and 80%, respectively, and degraded preformed Aβ aggregates. This study provides robust evidence regarding the potential of DR as a natural therapeutic agent for AD, highlighting specific compounds that may contribute to its efficacy.

Estrogen-like Cell Proliferation Abilities of Korea Forest Plant Resources on MCF-7 Cells and Analysis of Active Compounds

This study conducted a comprehensive analysis of functional substances and explored their biological activities using colorimetric and chromatographic techniques to identify high-value materials from 14 species of forest plants native to Korea. Comparative analysis between plant species included calculating the total polyphenol and flavonoid contents and qualitative and quantitative analysis of the phytochemical compounds caffeic acid (1), p-coumaric acid (2), and quercetin (3) using HPLC, and antioxidant activity tests (DPPH and ABTS+) and menopausal symptom relief tests (E-screen assay) to investigate their biological activities. The results highlighted Cercidiphyllum japonicum (FR 4), Aruncus dioicus (FR 6), and Pseudocydonia sinensis (FR 8) as excellent forest plant resource materials among the 14 forest plant resources. Notably, FR 4 exhibited significant activity in the E-screen assay. On the basis of these findings, we propose the use of FR 4 as a valuable material. Further analysis identified the phytochemical compounds maltol (4), chlorogenic acid (5), ellagic acid (6), and quercitrin (7) in FR 4 and analyzed their biological activities. Compounds 2–6 found in FR 4 were confirmed to possess strong antioxidant activity, and an E-screen assay revealed an excellent cell proliferation rate for quercitrin (7). This suggests that quercitrin (7) in FR 4 may be a significant indicator of the alleviation of menopausal symptoms.

Exploring Caffeic Acid and Lignosulfonate as Key Phenolic Ligands for Metal-Phenolic Network Assembly.

Films formed by metals and phenols through a coordinative interaction have been extensively studied in previous years. We report the successful formation of MPN films from the phenolic compounds caffeic acid and lignosulfonate using Fe3+ ions for complexation. The likewise examined p-coumaryl alcohol showed some MPN film formation tendency, while for coniferyl alcohol and sinapyl alcohol, no successful film buildup could be observed. These newly formed films were compared to tannic acid-Fe3+ films as a reference. Film growth and degradation were tracked by using UV-vis absorption spectroscopy. The films were degradable under different conditions such as alkaline environments or in the presence of a strong chelator. Small hollow capsules with a diameter of 3 μm and thicknesses in the nanometer range were produced. Additionally, the prepared films showed varying colors and levels of wettability. By utilizing the films' coating properties, we successfully dyed human hair in various colors.

Contribution of Hydroxycinnamic Acids to Color Formation in Nonenzymatic Browning Reactions with Key Maillard Reaction Intermediates.

The Maillard reaction is a vital part of food processing, involving a vast number of complex reaction pathways, resulting in high-molecular-weight colorants. So far, studies have been focused on the conversion of carbohydrates and amino compounds, but the literature elaborating the contribution of phenolic compounds to the formation of the colored end-products is still rare. The aim of this study was to characterize early reactions, underlying the formation of phenol-containing melanoidins. For this purpose, binary model systems of the prominent phenolic compounds caffeic acid and ferulic acid combined with α-dicarbonyl compounds typically formed in the Maillard reaction such as glyoxal, methylglyoxal, and diacetyl were analyzed after heat treatment. High-resolution mass spectrometry revealed that decarboxylation, aromatic electrophilic substitution, and nucleophilic addition are important reaction steps that lead to colored heterogeneous oligomers. Polymerization was favored for phenolic compounds with a high electron density in the aromatic system and for α-dicarbonyl compounds carrying aldehyde functions.

Caffeic Acid, a Polyphenolic Micronutrient Rescues Mice Brains against Aβ-Induced Neurodegeneration and Memory Impairment.

Oxidative stress plays an important role in cognitive dysfunctions and is seen in neurodegeneration and Alzheimer's disease (AD). It has been reported that the polyphenolic compound caffeic acid possesses strong neuroprotective and antioxidant effects. The current study was conducted to investigate the therapeutic potential of caffeic acid against amyloid beta (Aβ1-42)-induced oxidative stress and memory impairments. Aβ1-42 (5 μL/5 min/mouse) was administered intracerebroventricularly (ICV) into wild-type adult mice to induce AD-like pathological changes. Caffeic acid was administered orally at 50 mg/kg/day for two weeks to AD mice. Y-maze and Morris water maze (MWM) behavior tests were conducted to assess memory and cognitive abilities. Western blot and immunofluorescence analyses were used for the biochemical analyses. The behavioral results indicated that caffeic acid administration improved spatial learning, memory, and cognitive abilities in AD mice. Reactive oxygen species (ROS) and lipid peroxidation (LPO) assays were performed and showed that the levels of ROS and LPO were markedly reduced in the caffeic acid-treated mice, as compared to Aβ-induced AD mice brains. Moreover, the expression of nuclear factor erythroid 2-related factor 2 (Nrf2) and heme oxygenase-1 (HO-1) were regulated with the administration of caffeic acid, compared to the Aβ-injected mice. Next, we checked the expression of ionized calcium-binding adaptor molecule 1 (Iba-1), glial fibrillary acidic proteins (GFAP), and other inflammatory markers in the experimental mice, which suggested enhanced expression of these markers in AD mice brains, and were reduced with caffeic acid treatment. Furthermore, caffeic acid enhanced synaptic markers in the AD mice model. Additionally, caffeic acid treatment also decreased Aβ and BACE-1 expression in the Aβ-induced AD mice model.

Ocimum sanctum L water extract: In-situ green synthesis of zinc oxide nanoparticles for treatment of rheumatoid arthritis: Preclinical study

Background and objectiveRheumatoid arthritis is a chronic progressive autoimmune disorder, characterised by destruction of cartilage and under line bones. Though exact etiology of rheumatoid arthritis (RA) remains unknown. It is believed that alteration in control of cellular or molecular responses is involved in the chronic inflammation. Earlier in RA patients it was observed the circulating RA specific biomarkers and immunoglobulin deposits in the synovial joints. Zinc Oxide Nanoparticles (ZnO NPs) is used as an anti-inflammatory and anticancer agent, however there is nil/very less scientific data shows the anti-arthritic activity of green synthesis ZnO nanoparticles (Ocimum sanctum water extract in-situ synthesis of ZnO NPs having active compound Caffeic acid and Rosmerinic acid). Hence, the present activity was planned to assess the anti-arthritic activity of ZnO NPs in CIA rats. MethodsArthritis in rats were induced by subcutaneous injection of collagen type II (CII) (200 µl) at the base of tail on day 0 followed by booster dose on day 14. ZnO NPs were given (2 mg/kg b.wt./day) orally for 20 days. At the end of the study serum, joint homogenate was used to assess the level of biomarkers (RF, a-CCP, a-CII and CRP) and inflammatory mediators. In addition, m-RNA expression of various genes such as Nuclear factor-kB (NF-kB), inflammatory mediators like tumour necrosis factor-α (TNF-α), cyclooxygenase-2 (COX-2) etc. were assayed in joint tissue. Finally all these biochemical and molecular results were confirmed by microscopic study of joint tissue. ResultsZnO NPs, treated rats showed decrease in inflammation and clinical severity. This was related with decrease in the level of biomarkers (like RF, a-CCP and CRP), inflammatory mediators (TNF-α, COX-2) and activity of transcription factor NF-kB. All these findings were positively correlated with microscopic analysis of joint tissue that showed reduced inflammation and bone erosion in treated group. ConclusionThis study validates the anti-arthritic activity of ZnO NPs as it mitigates the arthritis related symptoms in CIA rats.

Phytochemical Investigation and in Vitro Antioxidant Activity of Panchavalkala Bark Extracts

Natural antioxidants have an important role in the prevention of many age-related diseases and promotion of health. Among natural antioxidants from plants, flavonoids and other phenolic compounds are potent antioxidants and chelating agents. Panchavalkala the barks of five trees i.e. Nyagrodha (Ficus benghalensis L.), Udumbara (Ficus racemosa L.), Ashwatha (Ficus religiosa L.), Plaksha (Ficus virens Aiton) and Parisha (Thespesiapopulnea (L.)Sol.ex Correa) are also known as Pancha Ksheeri Vrikshas in use since Vedic period. Barks of these trees are dried in shade and are used for different formulations (Pancha Kashaya Kalpanas), in different pathological conditions, especially as wound healing, gynecological disorders and etc. The plant samples were extracted using ethanol and water, and subjected for the phytochemical analysis. It was confirmed that samples contain many biologically active compounds like flavonoids, polyphenols, tannins, alkaloids, glycosides and terpinoids etc. The marker compound of each trial drug and the quantitative analysis has been carried out by high performance liquid chromatography. The antioxidant study was done by using in vitro method 1, 1­-diphenyl-2-picryl-hydrazyl (DPPH) radicle scavenging assay. The marker compounds caffeic acid and gallic acid were quantified in each extract for their quality and efficacy. PVK barks showed high free radicle scavenging activity as evidenced by the low IC50 values in DPPH (EE PVK- 20.46 µg/ml, AE PVK-37.79 µg/ml, EE T.poulenea-22µg/ml, AE T. poulenia- 23.31µg/ml AE F. benghalensis- 25.53µg/ml, EE F. benghalensis- 26.23µg/ml, EE F. religiosa – 34µg/ml). Quercetin- IC50 value 4.026µg/ml is used as standard.
 The results of the study demonstrated that PVK barks possess phyto-constituent’s viz. tannins, flavonoids, polyphenols etc. and has potential antioxidant activity. Thus these barks have good therapeutic potential as natural antioxidant and might be used in life style related conditions like hyperlipidemia, diabetes, obesity, cardiovascular disorders and etc.

Caffeic Acid Modified Nanomicelles Inhibit Articular Cartilage Deterioration and Reduce Disease Severity in Experimental Inflammatory Arthritis.

Inflammation plays an important role in the development of rheumatoid arthritis (RA). NR4A1 is an anti-inflammatory orphan nuclear receptor involved in protection from inflammatory stimuli in RA. In this study we have explored the anti-inflammatory potential of the FDA-approved drug 9-aminoacridine (9AA) and the natural compound caffeic acid (CA) conjugated to nanomicelles for the treatment of RA. We have synthesized methoxy polyethylene glycol polycaprolactone block copolymer (mPEG-b-PCL) by ring opening polymerization of ε-caprolactone. Then, we conjugated the hydrophilic caffeic acid (CA) with mPEG-b-PCL micelles via Steglich esterification and incorporated the 9AA drug. These nanomicelles were formulated by the solvent evaporation method with a size distribution around 190 nm and showed maximum drug loading capacity along with sustained drug release behavior. Furthermore, we tested the therapeutic potential of the formulated 9AA-encapsulated CA-conjugated nanomicelles (9AA-NMs) against an experimental RA model. We observed promising results which showed alleviation of arthritic symptoms by reducing inflammation, joint damage, bone erosion, and swelling. Further, collagen destruction was significantly reduced in articular cartilage, as shown by safranin-O and toluidine blue staining. The protective mechanism might be due to the simultaneous inhibition of NF-κB by 9AA and CA, whereas the activation of NR4A1 by 9AA leads to the suppression of HIF-1α. This combined therapeutic effect of 9AA and CA has enhanced the therapeutic efficacy of 9AA-NM and markedly reduced the severity of inflammatory arthritis. Unlike existing drugs for pain management and with limited efficacy, 9AA-NM exerted a disease-relevant activation/blockade that alleviated inflammation and exhibited marked therapeutic efficacy against RA.

Cytotoxic activity of ethanolic extracts of Lippia graveolens HBK leaves and stem against lung cancer cell line SK-LU-1

Lippia graveolens HBK (Verbenaceae) is an aromatic herb of economic importance in Mexico, known as oregano. The leaves are usedas condiments, and people use this species for respiratory and digestive disorders. The aim of this work was to evaluate the cytotoxic effect of ethanolic extracts obtained from free-oil leaves (L9) and stem (S15), against lung cancer cell line SK-LU-1, through tetrazolium salt (MTT) assay. Extracts concentrations of 0.3 to 300 μg/mL were used and HFF-1 as normal control cells. Both L9 and S15 extracts, showed cytotoxic effect, although stem was stronger than leaves and without damage to normal cell control. The phenolic compounds caffeic acid and acacetin werein higher concentration in L9, whereas naringenin, taxifolin, eriodictyol, luteolin, and apigenin had higher concentrations in S15. The ethanolic extracts of L. graveolens have excellent cytotoxic activity, and have a wide possibility of use in lung cancer treatment.

Disinfectant activities of extracts and metabolites from Baccharis dracunculifolia DC.

The concern regarding the harm caused by biocides to human health has been increasing over the years, making the natural products an alternative to less toxic and more efficient biocides. Therefore, this paper reports the investigation of the disinfectant potential of extracts and isolated compounds from Baccharis dracunculifolia. For this purpose, extracts of aerial parts (BD-C), tricomial wash (BD-L) and roots (BD-R) of B. dracunculifolia were obtained by maceration. The extracts were submitted to different chromatographic techniques, including high-speedy countercurrent chromatography (HSCCC) furnishing nine isolated compounds. The extracts and isolated compounds were evaluated regarding their antimicrobial activity by the broth microdilution method, according to the Clinical and Laboratory Standards Institute, and regarding their sanitizing activity according to Standard Operating Procedure No. 65·3210·007 (INCQS, 2011), developed by the National Institute for Quality Control in Health (INCQS) - Oswaldo Cruz Foundation (FIOCRUZ). In the antimicrobial evaluation the BD-C extract showed minimum inhibitory concentration (MIC) values of 200 and 100 µg/ml against Staphylococcus aureus and Tricophyton mentagrophytes, respectively. BD-L extract showed MIC value of 200 µg/ml against S. aureus. The isolated compounds caffeic acid (MBC 2·22 µmol l-1 ), ferulic acid (MBC 2·06 µmol l-1 ) and baccharin (MBC 0·27 µmol l-1 ) showed significant inhibitory activity against S. aureus. All B. dracunculifolia isolated compounds were active with exception of aromadrendin-4´-O-methyl-ether for T. mentagrophytes. Additionally, isosakuranetin was active against Salmonella choleraesuis (MIC 1·4 µmol l-1 ). Regarding the sanitizing activity, the hydroalcoholic solution containing 0·2% of B. dracunculifolia extract in 40°GL ethanol was effective in eliminating the microbial contamination on all carrier cylinders and against all microorganisms evaluated in the recommended exposure time of 10 min. Therefore, B. dracunculifolia has potential for the development of sanitizing agents to be used in hospitals, food manufactures and homes.

Effects of Water Stress, Defoliation and Crop Thinning on Vitis vinifera L. cv. Solaris Must and Wine Part II: 1H NMR Metabolomics.

Proton nuclear magnetic resonance (1H NMR) metabolomics was employed to investigate the impact of water deficit, defoliation, and crop thinning on the chemical composition of must and wines from the cool-climate white grape variety Solaris. The obtained results show that viticultural practices (defoliation and crop thinning) affected the amino acid and sugar content of Solaris must and thereby the quality of the final wine—mainly in terms of compounds normally related to fruity aroma (i.e., isopentanol), non-sugar sweetness (i.e., proline and glycerol), and alcohol content. The content of tyrosol, a natural phenolic antioxidant with a high bioavailability, was increased in the final wine by a combination of defoliation and crop thinning. The results of the metabolomics analysis performed on the must and wine samples from the water stress experiment showed that short-term water deficit significantly affected the concentration of several flavor-related compounds, including glutamate, butyrate and propanol, of the organic acids lactate and fumarate, and of the phenolic compounds caffeic acid and p-coumaric acid. ANOVA simultaneous component analysis showed that the effect of water deficit accounted for 11% (p < 0.001) and 8% (p < 0.001) of the variability in the metabolite concentrations in must and wines, respectively, while viticultural practices accounted for 38% (p < 0.001) and 30% (p < 0.001) of the metabolite variability in must and wines, respectively.

Review on Lemon Balm Herb and its Evaluation

The development of drugs from medicinal herbs may be good to find novel therapeutic agents in the treatment of anxiety. Melissa officinalis L. (lemon balm) belongs to the Lamiaceae family and grows widely in the Mediterranean region, western Asia, southwestern Siberia, and northern Africa. Melissa officinalis L. has been used in traditional medicine to treat headaches, indigestion, colic, nervousness, cardiac failure and depression. In addition, it has been reported in several researches that lemon balm had many beneficial effects such as anti-inflammatory and ant nociceptive, Antioxidant. leaves contain several classes of constituents including polyphenolic compounds (rosmarinic acid, caffeic acid and protocatechuic acid), essential oils (geranial, neral, citronellal, geraniol, beta-pinene, alpha-pinene, beta-caryophyllene, germacrene D, and ocimene), monotherpenoid aldehydes, sesquiterpenes, flavonoids (luteolin) and tannins. The aims of this study were to evaluate the phytochemical screening of ethanolic extract of Melissa officinalis L. One study examined a chemically-validated essential oil derived from Melissa and found that Melissa inhibited binding of GABAA to receptor channel in the rat forebrain, but had no effect on or nicotinic acetylcholine receptors (Abuhamdah et al., 2008). They also found that Melissa elicited a significant dose-dependent reduction in both inhibitory and excitatory transmission.. The aromatic balm leaves are often used in beverages and as a seasoning in salads, dressings and sauces, as well as in cooked foods, e.g., in soups and stews. Some vernacular names are balm, common balm, blue balm, dropsy plant, honey plant, Herzkraut, citronelle, cytria, cedronella.

Caffeic acid phenethyl ester suppresses intestinal FXR signaling and ameliorates nonalcoholic fatty liver disease by inhibiting bacterial bile salt hydrolase activity.

Propolis is commonly used in traditional Chinese medicine. Studies have demonstrated the therapeutic effects of propolis extracts and its major bioactive compound caffeic acid phenethyl ester (CAPE) on obesity and diabetes. Herein, CAPE was found to have pharmacological activity against nonalcoholic fatty liver disease (NAFLD) in diet-induced obese mice. CAPE, previously reported as an inhibitor of bacterial bile salt hydrolase (BSH), inhibited BSH enzymatic activity in the gut microbiota when administered to mice. Upon BSH inhibition by CAPE, levels of tauro-β-muricholic acid were increased in theintestine and selectively suppressed intestinal farnesoid X receptor (FXR) signaling. This resulted in lowering of the ceramides in theintestine that resulted from increased diet-induced obesity. Elevated intestinal ceramides are transported to the liver where they promoted fat production. Lowering FXR signaling was also accompanied by increased GLP-1 secretion. In support of this pathway, the therapeutic effects of CAPE on NAFLD were absent in intestinal FXR-deficient mice, and supplementation of mice with C16-ceramide significantly exacerbated hepatic steatosis. Treatment of mice with an antibiotic cocktail to deplete BSH-producing bacteria also abrogated the therapeutic activity of CAPE against NAFLD. These findings demonstrate that CAPE ameliorates obesity-related steatosis at least partly through the gut microbiota-bile acid-FXR pathway via inhibiting bacterial BSH activity and suggests that propolis enriched with CAPE might serve as a promising therapeutic agent for the treatment of NAFLD.

Promoting Angiogenesis Effect and Molecular Mechanism of Isopropyl Caffeate (KYZ), a Novel Metabolism-Derived Candidate Drug, Based on Integrated Network Pharmacology and Transgenic Zebrafish Models.

Aim of the study: Ischemic diseases have a huge impact on people’s health, which can cause blood supply blockage or restriction in specific tissues. Researchers must develop novel drugs with great efficacy and low toxicity for the prevention and treatment of such diseases. Isopropyl caffeic acid (KYZ) was one of the metabolites of caffeic acid in vivo. This study is to explore the protective effect and mechanism of KYZ on ischemic disease from the perspective of angiogenesis in vivo and in vitro, providing support for the treatment of ischemic diseases and the discovery of a new candidate drug. Methods: The network pharmacology and molecular docking were used to predict the targets of KYZ. In addition, the effects of KYZ on damaged and normal blood vessels were evaluated using the Tg (fli1: EGFP) transgenic zebrafish. The HUVECs model was used to study the effects of KYZ on proliferation, migration, and tube formation. The same dosage of caffeic acid (CA) was also administered in vitro and in vivo at the same time to assess the pharmacodynamic difference between the two compounds. Western Blot and ELISA methods were used to detect the expression of related target proteins. Results: The result from the network pharmacology indicated that the targets of KYZ were related to angiogenesis. It was also found that KYZ could repair the vascular damage induced by the PTK787 and promote the growth of subintestinal vessels in normal zebrafish. The result also indicated that KYZ’s angiogenic ability is better than the precursor compound CA. In HUVECs, KYZ could promote cell proliferation, migration, and tube formation. Further mechanistic study suggested that the KYZ could induce the release of VEGF factor in HUVECs, up-regulate the expression of VEGFR2, and activate the PI3K/AKT and MEK/ERK signaling pathways. Conclusions: These data show that KYZ may promote angiogenesis through VEGF, PI3K/AKT, and MEK/ERK signaling pathways, suggesting that KYZ exhibited great potential in the treatment of ischemic cardio-cerebrovascular diseases.

Antioxidant, Hypoglycemic and Molecular Docking Studies of Methanolic Extract, Fractions and Isolated Compounds from Aerial Parts of Cymbopogon citratus (DC.) Stapf.

Traditionally, Cymbopogon citratus is used to treat a variety of ailments, including cough, indigestion, fever, and diabetes. The previous chemical and bioactive research on C. citratus mainly focused on its volatile oil. In this study, 20 non-volatile known compounds were isolated from the dried aerial part of C. citratus, and their structures were elucidated by MS, NMR spectroscopy, and comparison with the published spectroscopic data. Among them, 16 compounds were reported for the first time from this plant. The screening results for antioxidant and α-glucosidase inhibitory activities indicated that compounds caffeic acid (5), 1-O-p-coumaroyl-3-O-caffeoylglycerol (8), 1,3-O-dicaffeoylglycerol (9) and luteolin-7-O-β-D-glucopyranoside (12) had potent antioxidant capacities, with IC50 values from 7.28 to 14.81 μM, 1.70 to 2.15 mol Trolox/mol and 1.31 to 2.42 mol Trolox/mol for DPPH, ABTS, and FRAP, respectively. Meanwhile, compounds 8 and 9 also exhibited significant inhibitory activities against α-glucosidase, with IC50 values of 11.45 ± 1.82 μM and 5.46 ± 0.25 μM, respectively, which were reported for the first time for their α-glucosidase inhibitory activities. The molecular docking result provided a molecular comprehension of the interaction between compounds (8 and 9) and α-glucosidase. The significant antioxidant and α-glucosidase inhibitory activities of compounds 8 and 9 suggested that they could be developed into antidiabetic drugs because of their potential regulatory roles on oxidative stress and digestive enzyme.

Medicinal benefits of lemon balm (Melissa officinalis) for human health

Melissa officinalis L, also known as lemon balm, bee balm, honey balm, is a perennial herb. Lemon balm occurs naturally in sandy and scrubby areas but also grown on damp wasteland, at elevations ranging from sea level to the mountains. Melissa officinalis is cost-effective, and compared with the economic indicators of traditional crops grown on fertilized land; this herb provides much higher profits. The leaf of Melissa officinalis contains flavonoids (quercitrin, rhamnocitrin, luteolin), polyphenolic compounds (rosmarinic acid, caffeic acid, and protocatechuic acid), monoterpenoid aldehyde, monoterpene glycosides, triterpenes (ursolic and oleanolic acids), sesquiterpenes, tannins, and essential oils (citral). Antimicrobial activities of the extracts and of rosmarinic acid of this plant were evaluated and were confirmed. The essential oil of Melissa officinalis L was shown to have anti-inflammatory activities, in treating various diseases associated with inflammation and pain. Melissa officinalis L relieves stress-related effects. Extract have the potential to prevent oxidative damage by preventing free radical– mediated oxidative stress. Melissa officinalis showed strong reducing power and exhibited a significant inhibition of deoxyribose degradation. The high phenolic content and radical scavenging activities of extracts of Melissa officinalis L was confirmed.

Effect of drought stress on metabolite synthesis in Actinidia Arguta Leaves

In the context of global climatic changes, water stress, which causes drought, is one of the limiting factors affecting the environment and negatively affects the growth and development of cultivated plants. The stressful impact of dry conditions causes changes in the biochemical processes of plants. Herein, we studied the change in antioxidant activity, the amount of phenolic compounds and the peculiarities of the synthesis of some metabolites in Actinidia. argutа leaves, Taezhny Dar variety, under drought stress. All parameters were measured in leaves of control plants and after drought stress. Biennial plants were grown in separate pots and kept in an open area under a canopy to keep out the rain. Antioxidant activity and the amount of phenolic compounds were determined spectrophotometrically. Under conditions of moisture deficiency, the antioxidant activity and the amount of phenolic compounds in the leaves are higher than in the control. The composition of metabolites in the leaf extract was determined by gas chromatography-mass spectrometry. Under drought stress, changes in the synthesis of primary and secondary metabolites occur. In the leaves of control plants, 14 substances were identified, of which 6 are organic acids and 8 are carbohydrate substances. In the leaves of plants under drought stress, 37 compounds were recorded, that is, more than 2 times more than in the leaves of control plants, 23 substances of a carbohydrate nature were identified, including Myo-Inositol, which has antioxidant properties. The main carbohydrates in the leaves of the control plants of actinidia were turanose and mannobiose; under drought conditions, sucrose; its content increased 15 times in comparison with the control plants. The phenolic compounds Quininic acid and Caffeic acid are synthesized in the leaves of Actinidia arguta plants subjected to drought.

Synthesis of Caffeic Acid Derivatives: Identification of (E)-N-(4-Cyanobenzyl)-3-(3,4-dihydroxyphenyl)acrylamide as an Anticancer Agent against Human Cervical Cancer Cells

A novel series of natural compound-caffeic acid derivatives were synthesized by coupling with different substituted amines and alkyl halides in an effort to enhance the anticancer activity and explore the structure-activity relationship. The structures of the compounds were determined by 1H NMR and mass spectroscopy analysis. Compounds were evaluated for inhibition against HeLa-cervical cancer cell proliferation and results revealed that compound (E)-N-(4-cyanobenzyl)-3-(3,4- dihydroxyphenyl)acrylamide (SHC5) exhibited potent antiproliferative activity with 5.2 μM concentration and it is further confirmed by Hoechst/PI double staining and Annexin V/PI double staining assay. Further, compound SHC5 was screened against other cancer cell lines namely K562, Jurkat, HCT116 and MiaPaCa2 to test the specificity of the molecule and found to be ineffective.

Cytocompatibility of Caffeic Acid‐Silica Hybrid Materials on NIH‐3T3 Fibroblast Cells

AbstractThe hydroxycinnamoyl compound caffeic acid (CA), broadly occurring in plants, is receiving special attention in materials science thanks to its antioxidant, anti‐inflammatory, and antimicrobial activities that make it promising for application use in various sectors. In this context, CA–based peptide biomaterials are recently developed as eco‐friendly and multifunctional free radical scavengers useable in a wide range of consumer manufacture, ranging from cosmetics to household products, as well as clinical applications, including imaging, drug delivery, and disinfection. Furthermore, a water‐soluble chitosan‐caffeic acid conjugate, effective in delaying lipid oxidation, is also synthetized. Herein, exploiting sol‐gel route versatility, CA/silica materials are synthetized. Hybrids, chemically characterized mainly through spectroscopic techniques, varied in their relative CA content, which represented 5%, 10%, 15%, or 20% of materials’ weight. The synthetized materials are able to elicit anti‐radical properties. The CA amount appeared to be determinant in anti‐radical activity, as well as in biocompatibility assessment. To this latter purpose, mouse embryonic fibroblast cell line NIH‐3T3 cells are utilized and directly exposed to hybrid materials. Redox mitochondrial activity is evaluated by means of the MTT test, whose results are in accordance with the materials’ biocompatibility.

Optimization for the extraction of polyphenols from Inonotus obliquus and its antioxidation activity

In order to study the extraction process and antioxidative activity of Inonotus obliquus polyphenols (IOP), the optimal extraction process was determined by orthogonal experiment optimization. The clearance rate of DPPH and hydroxyl radicals were used as indicators to evaluate the antioxidant activity of IOP. The results showed that the optimum extraction conditions were as follows: ethanol concentration of 50%, solid–liquid ratio of 1:20, temperature of 60 °C, and 90 min. Under these conditions, the extraction yield of IOP was 2.84%. The antioxidant capacity of extracts appeared to be IOP dose-dependent, while it also presented stronger ferric reducing antioxidant power (FRAP). High Performance Liquid Chromatography (HPLC-MS) analysis indicated that the major identified polyphenol compounds extracted at the optimal conditions were ten compounds (procyanidin, caffeic acid, p-coumaric acid, isorhamnetin-3-O-glucoside, astilbin, tangeretin, gallic acid, kaempferol, quercetin, and catechin 7-xyloside). These findings indicate that I. obliquus polyphenols have the potential to be developed as a natural antioxidant and have a good application prospect.