Quinic acid is a cyclohexanecarboxylic acid contained in the extracts of several parts of medicinal plants including Haematocarpus validus, Hypericum empetrifolium, Achillea pseudoaleppica, Rumex ...nepalensis, Phagnalon saxatile subsp. saxatile, Coffea arabica, Ziziphus lotus L, and Artemisia annua L ... etc. Currently, in vitro and in vivo pharmacological studies showed that quinic acid exhibits various biological activities, such as antioxidant, antidiabetic, anticancer activity, antimicrobial, antiviral, aging, protective, anti-nociceptive and analgesic effects. Indeed, QA possesses an important antibacterial effect which could be explained by the fact that this molecule modules the functions of ribosomes and the synthesis of aminoacyl-tRNAs, modifications the levels of glycerophospholipids and fatty acids and disruption of the oxidative phosphorylation pathway thereby causing interference with membrane fluidity. The antidiabetic activity of AQ is achieved by stimulation of insulin secretion via the mobilization of Ca2+ from intracellular reserves and the increase in the NAD(P)H/NAD(P)+ ratio. Its anticancer effect is through the promotion of apoptosis, inhibition of activator protein 1 (AP-1) and signaling pathways involving protein kinase C (PKC) and certain mitogen-activated protein kinases (MAPKs), resulting in the downregulation of matrix metallopeptidase 9 (MMP-9) expression. Therefore, this review describes the main research work carried out on the biological properties of AQ and the mechanism of action underlying some of these effects, as well as the investigations of the main pharmacokinetic studies.
The aim of the present study was to investigate the changes in the content of phytochemical compounds and in vitro antioxidant, antibacterial, and anti-inflammatory activities of Teucrium polium L. ...aerial parts and root methanolic extracts at different phenological stages (vegetative, flowering, and seeding). The T. polium extracts were analyzed using gas chromatography−mass spectrometry (GC-MS), and their antioxidant properties were tested with the 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), ferrous ions (Fe2+), and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) methods. Forty-nine compounds were identified with the majority of germacrene D, t-cadinol, β-pinene, carvacrol, bicyclogermacrene, α-pinene, and limonene. The results show that the extracts significantly differ between different phenological stages of the plant material used in terms of the phytochemical composition (total phenolic compounds, total flavonoids, total alkaloids, and total saponin contents) and bioactivities (antioxidant, antibacterial, and anti-inflammatory) (p < 0.05). The highest total contents of phenolics (72.4 ± 2.5 mg gallic acid equivalent (GAE)/g dry weight), flavonoids (36.2 ± 3.1 mg quercetin equivalent (QE)/g dry weight), alkaloids (105.7 ± 2.8 mg atropine equivalent (AE)/g dry weight), and saponins (653 ± 6.2 mg escin equivalent (EE)/g dry weight), as well as antioxidant, antibacterial, and anti-inflammatory activities, were measured for the extract of the aerial parts obtained at the flowering stage. The minimum inhibitory concentration (MIC) values for the extracts were varied within 9.4−300 µg/mL, while the minimum bactericidal concentration (MBC) values were varied within 18.75−600 µg/mL. In addition, they were more active on Gram-positive bacteria than Gram-negative bacteria. The data of this work confirm that the T. polium extracts have significant biological activity and hence can be used in the pharmaceutical industry, clinical applications, and medical research, as well as cosmetic and food industries.
•Enzyme inhibitory activities of A. anatolica were tested in this study.•All extracts have remarkable enzyme inhibitory potentials.•Enzyme inhibitory activities varied significantly the plant parts ...and solvent used.•Therefore, this study may be useful for pharmaceutical and food areas.
Asphodeline species are traditionally used as food and medicines. The different extracts (acetone, methanol and water) from different parts (stem, root, seed and leaf) of Asphodeline anatolica were screened for inhibitory potentials on cholinesterase, tyrosinase, α-amylase and α-glucosidase. Enzyme inhibitory effects were investigated by using microplate reader. All studied extracts exhibited remarkable inhibitory effects on the tested enzymes. Generally, acetone and methanol extracts have higher potentials than water extracts. Also, the enzyme inhibitory activities of the extracts varied significantly according to the plant parts as well as the solvent used. R-Met (7.42mgGALAEs/g extract) and St-Ac (10.74mgGALAEs/g extract) had the highest acetylcholinesterase and butrylcholinesterase inhibitory activity, respectively. R-Met (22.48mgKAEs/g extract) exhibited the strongest tyrosinase inhibitory effects, while Se-Ac had the most potent activity on both α-amylase (2.53mmolACAEs/g extract) and α-glucosidase (6.70mmolACAEs/g extract). The results suggested that the A. anatolica extract may be useful for food and medicinal applications.
In this work, a green process for the synthesis and characterization of hybrid nanoflowers was proposed, wherein Tribulus terrestris L. extract functioned as the organic component and Cu (II), Zn ...(II) and Co (II) metal ions as the inorganic element during the formation of the nanoflowers. To characterize the synthesized hybrid nanoflowers (hNFs), the morphologies were investigated using SEM, EDX, FT-IR analysis, elemental mapping, and XRD spectroscopy. The cytotoxic effect of hNFs was investigated to test biological activity. A549 cell lines and the MTT staining method were used for the anticancer activity of T. terrestris L. extract and hNFs. Differences in SEM images were observed as the metal content changed. Cytotoxic evaluations have shown that Co nanoflower may be a safer therapeutic alternative than plant extracts and other nanoflowers. It was observed that Zn and Cu hybrid nanoflowers were influential on the cell line up to a specific concentration, but as the concentration increased, they increased cell viability. It was observed that metal hybrid nanoflowers increased the anticancer activity compared to T. terrestris L. extract. These results can contribute to developing adequate new-generation preparations for A549 (lung cancer) problems of nanoflowers synthesized using T. terrestris L. extract. In summary, this study has been conducted for the first time.
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•Tribulus terrestris L.-Cu(II), Co(II), Zn(II) hybrid nanoflowers synthesis were carried out.•Characterization was carried out using SEM, EDX, XRD and elemental mapping.•A549 cell lines and the MTT staining method were used for the anticancer activity.•Cytotoxic evaluations have shown that Co nanoflower may be a safer therapeutic alternative than plant extracts.
One of the main causes of atherosclerosis is a disruption in cellular cholesterol hemostasis. The low-density lipoprotein receptor (LDLR) is an important factor in maintaining cholesterol homeostasis ...by the receptor-mediated endocytosis of LDL particles. Defective hepatic LDLR activity and uptake of LDL particles lead to elevated blood levels of low-density lipoprotein cholesterol (LDL-C), which is associated with a higher risk of atherosclerotic cardiovascular disease. LDLR expression can be affected by microRNAs (miRNAs). Some miRNAs, like miR-148a, miR-185, miR-224, miR-520, miR-128-1, miR-27a/b, miR-130b, and miR-301 seem to be important post-transcriptional regulators of LDLR related genes. These findings indicate the critical role of miRNAs in regulating LDL metabolism. The aim of this review was to provide insight into the miRNAs involved in LDLR activity and their potential roles in the treatment of cardiovascular disease.
Triterpene acid and phenolic constituents from nine ancient varieties of apple (
) fruits cultivated in Fanna, Friuli Venezia Giulia region, northeast Italy, were analyzed and compared with four ...commercial apples ('Golden Delicious', 'Red Delicious', 'Granny Smith' and 'Royal Gala'). Total phenolic and flavonoid contents were measured by spectrophotometric assays. The quali-quantitative fingerprint of secondary metabolites including triterpene acid was obtained by LC-DAD-(ESI)-MS and LC-(APCI)-MS, respectively. Based on the two LC-MS datasets, multivariate analysis was used to compare the composition of ancient fruit varieties with those of four commercial apples. Significant differences related mainly to the pattern of triterpene acids were found. Pomolic, euscaphyc, maslinic and ursolic acids are the most abundant triterpene in ancient varieties pulps and peels, while ursolic and oleanolic acids were prevalent in the commercial fruits. Also, the content of the phenolic compounds phloretin-2-
-xyloglucoside and quercetin-3-
-arabinoside was greater in ancient apple varieties. The antioxidant (radical scavenging, reducing power, metal chelating and phosphomolybdenum assays) and enzyme inhibitory effects (against cholinesterase, tyrosinase, amylase and glucosidase) of the samples were investigated in vitro. Antioxidant assays showed that the peels were more active than pulps. However, all the samples exhibited similar enzyme inhibitory effects. Ancient Friuli Venezia Giulia apple cultivars can be a source of chlorogenic acid and various triterpene acids, which are known for their potential anti-inflammatory activity and beneficial effects on lipid and glucose metabolism. Our results make these ancient varieties suitable for the development of new nutraceutical ingredients.
Abstract Benzene sulfonamides are an important biological substituent for several activities. In this study, hybridization of benzene sulfonamide with piperazine derivatives were investigated for ...their antioxidant capacity and enzyme inhibitory potencies. Six molecules were synthesized and characterized. DPPH, ABTS, FRAP, CUPRAC, chelating and phosphomolybdemum assays were applied to evaluate antioxidant capacities. Results show that compounds have high antioxidant capacity and compound 4 has the best antioxidant activity among them. Compound 4 has higher antioxidant activity than references for FRAP (IC 50 : 0.08 mM), CUPRAC (IC 50 : 0.21 mM) and phosphomolybdenum (IC 50 : 0.22 mM) assays. Besides this, compound 4 has moderate DPPH and ABTS antioxidant capacity. Furthermore, enzyme inhibition activities of these molecules were investigated against AChE, BChE, tyrosinase, α -amylase and α -glucosidase enzymes. It was revealed that all compounds have good enzyme inhibitory potential except for α -amylase enzyme. The best inhibitory activities were observed for AChE with compound 5 the same value (IC 50 : 1.003 mM), for BChE with compounds 2 and 5 the same value (IC 50 : 1.008 mM), for tyrosinase compound 4 (IC 50 : 1.19 mM), and for α -glucosidase with compound 3 (IC 50 : 1.000 mM). Docking studies have been conducted with these molecules, and the results correlate well with the inhibitory assays.
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•Imbalance of the immune system is associated with a range of chronic.•Phytochemical intake impedes the inflammatory and autoimmune disorders.•Phytochemicals are the potential source ...of immunomodulators.•Natural immunostimulants have ability to activate humoral and cell-mediated responses.
A well-functioning immune system of the host body plays pivotal role in the maintenance of ordinary physiological and immunological functions as well as internal environment. Balanced immunity enhances defense mechanism against infection, diseases and unwanted pathogens to avoid hypersensitivity reactions and immune related diseases. The ideal immune responses are the results of corrective interaction between the innate immune cells and acquired components of the immune system. Recently, the interest towards the immune system increased as significant target of toxicity due to exposure of chemicals, drugs and environmental pollutants. Numerous factors are involved in altering the immune responses of the host such as sex, age, stress, malnutrition, alcohol, genetic variability, life styles, environmental-pollutants and chemotherapy exposure. Immunomodulation is any modification of immune responses, often involved induction, amplification, attenuation or inhibition of immune responses. Several synthetic or traditional medicines are available in the market which promptly have many serious adverse effects and create pathogenic resistance. Phytochemicals are naturally occurring molecules, which significantly play an imperative role in modulating favorable immune responses. The present review emphasizes on the risk factors associated with alterations in immune responses, and immunomodulatory activity of phytochemicals specifically, glycosides, alkaloids, phenolic acids, flavonoids, saponins, tannins and sterols and sterolins.
Due to renewed interest in the cultivation and production of Italian
L., we proposed a multi-methodological approach to explore chemically and biologically both the essential oil and the aromatic ...water of this plant. We reported the chemical composition in terms of cannabinoid content, volatile component, phenolic and flavonoid pattern, and color characteristics. Then, we demonstrated the ethnopharmacological relevance of this plant cultivated in Italy as a source of antioxidant compounds toward a large panel of enzymes (pancreatic lipase, α-amylase, α-glucosidase, and cholinesterases) and selected clinically relevant, multidrug-sensible, and multidrug-resistant microbial strains (
,
,
, and
spp.), evaluating the cytotoxic effects against normal and malignant cell lines. Preliminary in vivo cytotoxicity was also performed on
larvae. The results corroborate the use of this natural product as a rich source of important biologically active molecules with particular emphasis on the role exerted by naringenin, one of the most important secondary metabolites.
Oxidative stress is a common phenomenon of many liver disorders; it both affects patient survival and directly influences the applicability, effectiveness, and toxicity of drugs. In the pursuit of ...reliable natural remedies for hepatoprotection, this study reports on the complete phytochemical characterization, antioxidant, and hepatoprotective activities of the Prenanthes purpurea methanol-aqueous extract in an in vitro model of diclofenac-induced liver injury (DILI). An ultra high-performance liquid chromatography–high-resolution mass spectrometry analysis (UHPLC-HRMS) was conducted, delineating more than 100 secondary metabolites for the first time in the species, including a series of phenolic acid-hexosides, acylquinic, acylhydroxyquinic and acyltartaric acids, and flavonoids. Quinic acid, chlorogenic, 3,5-dicaffeoylquinic and 5-feruloylhydroxyquinic acid, caffeoyltartaric and cichoric acids, eryodictiol-O-hexuronide, and luteolin O-hexuronide dominated the phytochemical profile and most likely contributed to the observed hepatoprotective activity of the studied P. purpurea leaf extract. The potency and molecular basis of cellular protection were investigated in parallel with pure caffeoylquinic acids in a series of pretreatment experiments that verified the antiapoptotic and antioxidant properties of the natural products.
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