Diospyros Kaki Leaves Decoction Phytochemical Characterization and Bioactivities Evaluation: LC-MS-Qtof Identification, Antioxidant Activity, Enzyme Inhibition and Cytotoxicity Toward HepG2 and Mcf-7 Cell Lines

Abstract Diospyros kaki known as Persimmon has played an important role in Chinese medicine, and its leaves are used in pharmaceuticals, cosmetics, and beverages due to their biological properties. The aim of this study was to evaluate chemical composition, antioxidant activity, enzyme inhibition. The main compounds of Diospyros kaki leaves decoctions were identified using high-resolution liquid chromatography – high-resolution tandem mass spectrometry (LC-HRMS-MS) interfaced with a Quadrupole Time-of-Flight (Q-tof). The obtained results showed that the aqueous extract had a high content of total phenolsand flavonoids and showed strong antioxidant activity (EC50 between 3.79±0.19 and 12.05±0.11µg/mL). In addition, these extracts were able to inhibit3-hydroxy-3-methylglutaril-CoA (HMG-CoA) reductase and acetylcholinesterase (IC50 ranging from 58.35±0.69 to 210.21±28.9 µg/mL). The cytotoxicity against human liver cells HepG2 and breast MCF7 cell lines was also evaluated. No cytotoxicity to HepG2 and MCF7 cells was detected. These results indicate that Diospyros kaki leaves could be considered as attractive source of health-promoting ingredients and a promising plant for the development of new functional foods and pharmaceutical products.

Download Full-text

Comparative Phytochemical Profile and Biological Activity of Four Major Medicinal Halophytes from Qassim Flora

Plants ◽

10.3390/plants10102208 ◽

2021 ◽

Vol 10 (10) ◽

pp. 2208

Author(s):

Hamdoon A. Mohammed ◽

Hussein M. Ali ◽

Kamal A. Qureshi ◽

Mansour Alsharidah ◽

Yasser I. Kandil ◽

...

Keyword(s):

Antioxidant Activity ◽

Cell Lines ◽

Biological Properties ◽

Human Pancreatic Cancer ◽

Antioxidant Power ◽

Hydroalcoholic Extract ◽

Anabasis Articulata ◽

Ic50 Values ◽

Ferric Reducing Antioxidant Power ◽

Induced Apoptosis

Four halophytic plants, Lycium shawii, Anabasis articulata, Rumex vesicarius, and Zilla spinosa, growing in the central Qassim area, Saudi Arabia, were phytochemically and biologically investigated. Their hydroalcoholic extracts’ UPLC-ESIQ-TOF analyses demonstrated the presence of 44 compounds of phenolic acids, flavonoids, saponins, carbohydrates, and fatty acids chemical classes. Among all the plants’ extracts, L. shawii showed the highest quantities of total phenolics, and flavonoids contents (52.72 and 13.01 mg/gm of the gallic acid and quercetin equivalents, respectively), along with the antioxidant activity in the TAA (total antioxidant activity), FRAP (ferric reducing antioxidant power), and DPPH-SA (2,2-diphenyl-1-picryl-hydrazyl-scavenging activity) assays with 25.6, 56.68, and 19.76 mg/gm, respectively, as Trolox equivalents. The hydroalcoholic extract of the L. shawii also demonstrated the best chelating activity at 21.84 mg/gm EDTA equivalents. Among all the four halophytes, the hydroalcoholic extract of L. shawii exhibited the highest antiproliferative activity against MCF7 and K562 cell lines with IC50 values at 194.5 µg/mL and 464.9 µg/mL, respectively. The hydroalcoholic extract of A. articulata demonstrated better cytotoxic activity amongst all the tested plants’ extracts against the human pancreatic cancer cell lines (PANC1) with an IC50 value of 998.5 µg/mL. The L. shawii induced apoptosis in the MCF7 cell lines, and the percentage of the necrotic cells changed to 28.1% and 36.5% for the IC50 and double-IC50 values at 22.9% compared with the untreated groups. The hydroalcoholic extract of L. shawii showed substantial antibacterial activity against Bacillus cereus ATCC 10876 with a MIC value of 12.5 mg/mL. By contrast, the A. articulata and Z. spinosa exhibited antifungal activities against Aspergillus niger ATCC 6275 with MIC values at 12.5 and 50 mg/mL, respectively. These findings suggested that the L. shawii is a potential halophyte with remarkable biological properties, attributed to its contents of phenolics and flavonoid classes of compounds in its extract.

Download Full-text

Effect of High Hydrostatic Pressure Extraction on Biological Activities and Phenolics Composition of Winter Savory Leaf Extracts

Antioxidants ◽

10.3390/antiox9090841 ◽

2020 ◽

Vol 9 (9) ◽

pp. 841

Author(s):

Sílvia A. Moreira ◽

Sara Silva ◽

Eduardo Costa ◽

Soraia Pinto ◽

Bruno Sarmento ◽

...

Keyword(s):

Antioxidant Activity ◽

Cell Lines ◽

Biological Activities ◽

Cell Metabolism ◽

Biological Properties ◽

Leaf Extracts ◽

Assisted Extraction ◽

Cancerous Cell ◽

Pressure Extraction ◽

Satureja Montana

Satureja montana L. has several biological properties related to its diverse composition of secondary metabolites. Nevertheless, it has been mainly studied for its essential oil, with only a few studies on the profile and bioactivities of the bioactive compounds from its leaf extracts being reported. This work aimed to study the antioxidant activity (by oxygen radical absorbance capacity (ORAC) assay), antimicrobial minimum inhibitory and bactericidal concentrations (MIC and MBC) determination, antibiofilm (by colorimetry), impact upon DNA (anti- and pro-oxidant assay), and cytotoxicity (by cell metabolism viability assays) of S. montana extracts obtained by high-pressure-assisted extraction (HPE). The extract obtained at 348 MPa, 35% (v/v) ethanol presented the highest concentration of individual phenolic compounds, and a minimum bactericidal concentration of 20 mg/mL against Listeria monocytogenes. HPE extracts showed antioxidant activity not only in ORAC but they were also able to prevent/attenuate peroxide-induced damage upon DNA. Moreover, on its own, HPE extract induced less oxidative damage than the control extract. Concerning the cytotoxicity, HPE extracts (at 0.5 and 1.0 mg/mL) were not harmful to HT29 cell lines, while control extracts (obtained at atmospheric pressure) at higher concentrations (>1.0 mg/mL) slightly reduced the metabolism of the cells. Finally, all extracts showed inhibition of the viability of 3 cancerous cell lines (>2.0 mg/mL for Caco-2, HeLa, and TR146) to below 15%.

Download Full-text

Seasonal Effect on the Biological Activities of Litsea glaucescens Kunth Extracts

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2018/2738489 ◽

2018 ◽

Vol 2018 ◽

pp. 1-11 ◽

Cited By ~ 3

Author(s):

Julio César López-Romero ◽

Humberto González-Ríos ◽

Aida Peña-Ramos ◽

Carlos Velazquez ◽

Moises Navarro ◽

...

Keyword(s):

Antioxidant Activity ◽

Cell Lines ◽

Antiproliferative Activity ◽

Biological Activities ◽

Antimicrobial Activities ◽

Inhibitory Effect ◽

Biological Properties ◽

Seasonal Effect ◽

Microdilution Method ◽

High Antioxidant Activity

This study shows the seasonal effect on the antioxidant, antiproliferative, and antimicrobial activities of L. glaucescens Kunth (LG) leaves extracts. Their antioxidant activity was evaluated through the DPPH, FRAP, and ORAC assays. Their phenolic content (PC) was determined by means of the Folin-Ciocalteu method, and the main phenolic compounds were identified through a HPLC-DAD analysis. Antiproliferative activity was determined by MTT assay against HeLa, LS 180, M12.C3.F6, and ARPE cell lines. Antimicrobial potential was evaluated against Staphylococcus aureus and Escherichia coli using a microdilution method. All the LG extracts presented high antioxidant activity and PC, with quercitrin and epicatechin being the most abundant. Antioxidant activity and PC were affected by the season; particularly autumn (ALGE) and summer (SULGE) extracts exhibited the highest values (p<0.05). All extracts presented moderate antiproliferative activity against the cell lines evaluated, HeLa being the most susceptible of them. However, ALGE and SULGE were the most active too. About antimicrobial activity, SULGE (MIC90<800 μg/mL; MIC50 < 400 μg/mL), and SLGE (MIC50 < 1000 μg/mL) showed a moderate inhibitory effect against S. aureus. These findings provide new information about the seasonal effect on the PC and biological properties of LG extracts. Clearly, antioxidant activity was the most important with respect to the other two.

Download Full-text

Antioxidant Activity and Lipase Enzyme Inhibition of Gynura procumbens (Lour.) Merr and Curcuma xanthorrhiza Roxb and their Correlation with Chemometric Methods

International Journal of Pharmaceutical Research ◽

10.31838/ijpr/2020.sp2.294 ◽

2020 ◽

Vol 12 (sp2) ◽

Keyword(s):

Antioxidant Activity ◽

Enzyme Inhibition ◽

Chemometric Methods ◽

Lipase Enzyme ◽

Curcuma Xanthorrhiza

Download Full-text

Apoptosis Caused by Triterpenes and Phytosterols and Antioxidant Activity of an Enriched Flavonoid Extract from Passiflora mucronata

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520618666180315090949 ◽

2019 ◽

Vol 18 (10) ◽

pp. 1405-1416 ◽

Cited By ~ 4

Author(s):

Isabel C.V. da Silva ◽

Goran N. Kaluđerović ◽

Pollyana F. de Oliveira ◽

Denise O. Guimarães ◽

Carla H. Quaresma ◽

...

Keyword(s):

Antioxidant Activity ◽

Cell Lines ◽

Oleanolic Acid ◽

Folk Medicine ◽

Hexane Fraction ◽

Cytotoxicity Test ◽

B16f10 Cell ◽

Dpph Method ◽

Melanoma B16f10 ◽

First Time

Background: P. mucronata (Pm) comes from South America, Brazil and is characterized as “Maracujá de Restinga”. It is used in folk medicine for its soothing properties and in treating insomnia. Objective: The present study for the first time analyzed the antioxidant and cytotoxicity of the hydroalcoholic leaves extract and fractions from Pm. Method: The cytotoxicity test will be evaluated by different assays (MTT and CV) against human prostate cancer (PC3) and mouse malignant melanoma (B16F10) cell lines, and the antioxidant test by DPPH method. Results: β-Amyrin, oleanolic acid, β-sitosterol and stigmasterol were isolated of the most active, hexane fraction. These substances were tested against the tumor cell lines: β-sitosterol and stigmasterol showed the most relevant activity to PC3 in CV assay and, oleanolic acid to B16F10 by the MTT assay. In addition, it was possible to indicate that the mode of cell death for stigmasterol, presumably is apoptosis. In terms of antioxidant activity, the hydroalcoholic leaves extract presented higher activity (EC50 133.3 µg/mL) compared to the flower (EC50 152.3 µg/mL) and fruit (EC50 207.9 µg/mL) extracts. By the HPLC-MS, it was possible to identify the presence of flavones in the leaf extract (isoschaftoside, schaftoside, isovitexin, vitexin, isoorientin, orientin). Conclusions: P. mucronata hexane fraction showed promising cytotoxic effect against cancer cell lines, and stigmasterol contributes to this activity, inducing apoptosis of these cells. Furthermore, as other Passiflora species, Pm extract showed antioxidant activity and flavones are its major phenolic compounds.

Download Full-text

Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

Molecules ◽

10.3390/molecules26123579 ◽

2021 ◽

Vol 26 (12) ◽

pp. 3579

Author(s):

Svetlana A. Popova ◽

Evgenia V. Pavlova ◽

Oksana G. Shevchenko ◽

Irina Yu. Chukicheva ◽

Aleksandr V. Kutchin

Keyword(s):

Antioxidant Activity ◽

Antioxidant Properties ◽

Biological Properties ◽

High Reactivity ◽

Biologically Active ◽

Brain Lipids ◽

Wide Range ◽

Privileged Structure ◽

Vitro Model

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.

Download Full-text

Tea as a Source of Biologically Active Compounds in the Human Diet

Molecules ◽

10.3390/molecules26051487 ◽

2021 ◽

Vol 26 (5) ◽

pp. 1487

Author(s):

Joanna Klepacka ◽

Elżbieta Tońska ◽

Ryszard Rafałowski ◽

Marta Czarnowska-Kujawska ◽

Barbara Opara

Keyword(s):

Antioxidant Activity ◽

Phenolic Compounds ◽

Daily Intake ◽

The Body ◽

Biologically Active ◽

Sodium Potassium ◽

Tea Infusions ◽

Copper Manganese ◽

Health Promoting ◽

Average Consumption

Due to the different levels of bioactive compounds in tea reported in the literature, the aim of this study was to determine whether commercially available leaf teas could be an important source of phenolics and selected minerals (copper, manganese, iron, zinc, magnesium, calcium, sodium, potassium) and if the differences in the content of these components between various types of tea are significant. It was found that both the amount of these compounds in tea and the antioxidant activity of tea infusions were largely determined by the origin of tea leaves as well as the processing method, which can modify the content of the studied components up to several hundred-fold. The group of green teas was the best source of phenolic compounds (110.73 mg/100 mL) and magnesium (1885 µg/100 mL) and was also characterised by the highest antioxidant activity (59.02%). This type of tea is a great contributor to the daily intake of the studied components. The average consumption of green tea infusions, assumed to be 3–4 cups (1 L) a day, provides the body with health-promoting polyphenol levels significantly exceeding the recommended daily dose. Moreover, drinking one litre of an unfermented tea infusion provides more than three times the recommended daily intake of manganese. Tea infusions can be a fairly adequate, but only a supplementary, source of potassium, zinc, magnesium, and copper in the diet. Moreover, it could be concluded that the antioxidant activity of all the analysed types of tea infusions results not only from the high content of phenolic compounds and manganese but is also related to the presence of magnesium and potassium.

Download Full-text

Advances in Processing, Quality, Safety, Authenticity, Nutrition, Health, and Oral Health of Extra Virgin Olive Oil

Proceedings ◽

10.3390/foods_2020-07668 ◽

2020 ◽

Vol 70 (1) ◽

pp. 107

Author(s):

Maria Antoniadou ◽

Theodoros Varzakas

Keyword(s):

Oral Health ◽

Olive Oil ◽

Review Paper ◽

Safety Management ◽

Virgin Olive Oil ◽

Extra Virgin Olive Oil ◽

Biological Properties ◽

Management Systems ◽

Health Promoting ◽

Effect Of Food

Olive fruit exerts great socioeconomic impact. Many studies have shown the multiple benefits of healthy olive oil for the human body. The increase in consumption of extra virgin olive oil is mainly due to its unique sensory, nutritive qualities, biological properties, and health-promoting effects. In this review paper recent advances in quality, safety, authenticity, processing, nutrition, health, and oral health of extra virgin olive oil (EVOO) have been discussed and outlined. Regarding safety, the effect of food safety management systems in EVOO has been reported along with the use of different tools such as FMEA and Ishikawa.

Download Full-text

Synthesis and Cytotoxic Analysis of Novel Myrtenyl Grafted Pseudo-Peptides Revealed Potential Candidates for Anticancer Therapy

Molecules ◽

10.3390/molecules25081911 ◽

2020 ◽

Vol 25 (8) ◽

pp. 1911 ◽

Cited By ~ 1

Author(s):

Odette Concepción ◽

Julio Belmar ◽

Alexander F. de la Torre ◽

Francisco M. Muñiz ◽

Mariano W. Pertino ◽

...

Keyword(s):

T Cells ◽

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Anticancer Agents ◽

Cd4 T Cells ◽

Dermal Fibroblast ◽

Colon Adenocarcinoma ◽

Cancer Cell Lines ◽

Biological Properties

Myrtenal is a natural monoterpene isolated from essential oils of several plants and their derivates have shown to have several biological properties including cytotoxicity. The cytotoxic activity of these derivates are being investigated for their antitumor effect leading to the development of potential anticancer agents. In this study, novels Myrtenyl grafted pseudo-peptides were designed, synthesized and functionally characterized as possible therapeutic agents for cancer treatment. Thirteen novel Myrtenyl grafted pseudo-peptides were prepared in high atom economy and efficiency by a classic Ugi-4CR and sequential post-modification. Their structures were confirmed by NMR, and ESI-MS, and its cytotoxic activity was evaluated in three cancer cell lines and primary CD4+ T cells at different proliferative cycles. Our results revealed that some of these compounds showed significant cytotoxicity against human gastric, breast and colon adenocarcinoma cells lines, but not against human dermal fibroblast cell line. Moreover, from the thirteen novel myrtenyl synthesized the compound (1R,5S)-N-{[1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl]methyl}-N-[2-(cyclohexylamino)-2–oxoethyl]-6,6-dimethylbicyclo[3.1.1]hept-2-ene-2-carboxamide (3b) proved to be the best candidate in terms of acceptable EC50, and Emax values in cancer cell lines and at inducing cytotoxicity in CD4+ T cells undergoing active proliferation, without affecting non-proliferating T cells. Overall, the synthesis and characterization of our Myrtenyl derivates revealed novel potential anticancer candidates with selective cytotoxic activity.

Download Full-text