Antioxidant and Antiproliferative Activities of Phenolic Extracts of Eriobotrya japonica (Thunb.) Lindl. Fruits and Leaves.

Increasing interest in new sources of secondary metabolites as biologically active substances has resulted in an advanced study of many plant species. Loquat (Eriobotrya japonica (Thunb.) Lindl. = Rhaphiolepis bibas (Lour.) Galasso & Banfi, Rosaceae family), an evergreen, subtropical fruit tree, native to China and Japan, but cultivated in southern countries of Europe, is a species commonly used in folk medicine and may be an excellent source of bioactive compounds. Therefore, the aim of the present study was to evaluate the profile of the phenolic constituents of E. japonica fruits and leaves originating from Tuscany (Italy), as well as their in vitro antioxidant and chemopreventive activities on human cancer cell lines breast adenocarcinoma (MCF-7), colon adenocarcinoma (Caco-2 and HT-29), and glioblastoma (U87MG). Results revealed that the extract of leaves displayed higher antioxidant and anticancer potential than the fruit extract and contained 25 individual phenolic compounds that have been characterized and quantified by the UPLC-PDA-MS method. The antiproliferative activity was correlated with the content of polyphenolic compounds indicating that both fruits and leaves are a good source of antioxidants and may be exploited as nutraceuticals enriching food or as components for the cosmetic/pharmaceutical industry.

Chemical Profiling, Bioactive Properties, and Anticancer and Antimicrobial Potential of Juglans regia L. Leaves.

The aim of this study was to assess the biological potential of the polyphenolic fraction isolated from J. regia leaves, collected in the Subcarpathian region (Poland). The phenolic profile was determined using the UPLC-PDA-MS/MS method. Biological activity was determined by evaluating the antioxidant, anticancer, antibacterial, and antifungal effects. Prior to this study, the purified polyphenolic fraction was not been tested in this regard. A total of 40 phenolic compounds (104.28 mg/g dw) were identified, with quercetin 3-O-glucoside and quercetin pentosides dominating. The preparation was characterized by a high ability to chelate iron ions and capture O2•- and OH• radicals (reaching IC50 values of 388.61, 67.78 and 193.29 µg/mL, respectively). As for the anticancer activity, among the six tested cell lines, the preparation reduced the viability of the DLD-1, Caco-2, and MCF-7 lines the most, while in the antibacterial activity, among the seven tested strains, the highest susceptibility has been demonstrated against K. pneumoniae, S. pyogenes, and S. aureus. Depending on the needs, such a preparation can be widely used in the design of functional food and/or the cosmetics industry.

Phenolic Profile and Antioxidant, Antibacterial, and Antiproliferative Activity of Juglans regia L. Male Flowers.

Juglans regia L., walnut, is a large, long-living tree, cultivated in temperate climates around the world. It is highly appreciated for its nutritional kernels and high-quality timber. Its barks, leaves, and husk are used as dyes and in folk medicine as herbal remedies for several diseases. From a biological and chemical standpoint, relatively little is known about the male flowers of the tree. Therefore, the aim of the study was to evaluate the phenolic profile as well as in vitro antioxidant, antimicrobial, and antiproliferative activity of male Juglans regia L. flowers. Phenolic content was determined by UPLC/PDA/MS/MS analyses; antioxidant activity was assessed by five different methods; antimicrobial activity was evaluated against the six most common pathogenic strains of Gram-positive and Gram-negative bacteria, and antiproliferative properties were assessed against six cell lines. Most of the analyses carried out in this study were performed for the first time for this raw material. J. regia flower extract was characterized by a strong ability to scavenge DPPH˙ free radicals, hydroxyl radicals, and chelating metal ions. Among the examined bacterial strains and neoplastic lines, the strongest antimicrobial activity was shown against S. aureus, L. monocytogenes, and B. cereus, and cytotoxic activity against breast cancer, glioblastoma, and astrocytoma cells. Male J. regia flowers have also been found to be a rich source of phenolic compounds. The content of polyphenols in the extract was 4369.73 mg/100 g d.w., and 24 compounds from the group of flavonoids, phenolic acids, and juglunosides were identified. Additionally, a strong correlation between the content of polyphenols and the antioxidant capacity and cytotoxic activity was observed. This is why the tested J. regia flowers are an excellent source of effective natural antioxidant, antibacterial, and chemopreventive compounds that have potential to be used in the pharmaceutical or food industries.

Polyphenolic Compounds of Crataegus Berry, Leaf, and Flower Extracts Affect Viability and Invasive Potential of Human Glioblastoma Cells.

Crataegus contains numerous health-promoting compounds that are also proposed to have anti-cancer properties. Herein, we aimed at a contemporaneous evaluation of the effects of polyphenol-rich extracts of berries, leaves, and flowers of six Crataegus species on the viability and invasive potential on the highly aggressive human glioblastoma U87MG cell line. The treatment with the extracts evoked cytotoxic effects, with the strongest in the berry extracts. All extracts not only promoted the apoptosis-related cleavage of poly (ADP-ribose) polymerase 1 (PARP1) but also substantially inhibited the activity of pro-survival kinases, focal adhesion kinase (FAK), and protein kinase B (PKB; also known as Akt), thus indicating the suppression of proliferative and invasive potentials of the examined glioblastoma cells. The qualitative and quantitative characterization of the extracts' content was also performed and revealed that amongst 37 polyphenolic compounds identified in the examined Crataegus extracts, the majority (29) was detected in berries; the leaf and flower extracts, exerting milder cytotoxic effects, contained only 14 and 13 compounds, respectively. The highest polyphenol content was found in the berries of C. laevigata x rhipidophylla x monogyna, in which flavan-3-ols and phenolic acids predominated. Our results demonstrated that a high content of polyphenolic compounds correlated with the extract cytotoxicity, and especially berries were a valuable source of compounds with anti-cancer potential. This might be a promising option for the development of an effective therapeutic strategy against highly malignant glioblastomas in the future.

The Content of Phenolic Acids and Flavonols in the Leaves of Nine Varieties of Sweet Potatoes (Ipomoea batatas L.) Depending on Their Development, Grown in Central Europe.

The aim of the study was the qualitative and quantitative analysis of the bioactive components present in the leaves of 9 sweet potato cultivars grown in the moderate climate in Poland, which were harvested at different growth stages according to the BBCH (Biologische Bundesanstalt, Bundessortenamt und Chemische Industrie) scale (14, 51, 89). It was found that sweet potato leaves contained 7 polyphenolic compounds, including 5 chlorogenic acids-neochlorogenic acid (5-CQA), chlorogenic acid (3-CQA), 4-cryptochlorogenic acid (4-CQA), 34-di-O-caffeoylqunic acid (3,4-CQA), 3,5-di-O-caffeoylqunic acid (3,5-CQA)-and 2 flavonoids, quercetin-3-O-galactoside (Q-3-GA) and quercetin-3-O-glucoside (Q-3-GL). Their content depended on the genotype of the examined cultivars and on the stage of leaf development. The mean content of the identified polyphenolic compounds in the examined cultivars ranged from 148.2 to 14.038.6 mg/100 g-1 DM for the leaves harvested at growth stage 14 according to the BBCH scale. In the case of leaves harvested at BBCH stage 51, the concentration of polyphenolic compounds ranged from 144.76 to 5026.8 mg/100 g-1 DM and at BBCH stage 89 from 4078.1 to 11.183.5 mg/100 g-1 DM. The leaves of the Carmen Rubin cultivar collected at stage 14 contained the highest amount of polyphenolic compounds, while Okinava leaves had the highest amount of these compounds at stage 51. The highest content of polyphenolic compounds in leaves at BBCH growth stage 89 was found in the Radiosa variety. The highest concentration levels were found for 3-CQA at all stages of leaf development. Significant correlations between polyphenol content and antioxidant activity measured by 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing/antioxidant power (FRAP) were found. The results of this experiment revealed that the growth stages and genetic properties of cultivars have a very significant influence on the content of phenolic acids and flavonols in sweet potato leaves. The results are innovative and can have a practical application, as the knowledge of the content of the substances under study makes it possible to determine the optimal management practice of sweet potato leaf harvest in order to obtain more top-quality raw material.