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Background/Objectives: Plants species of the Epilobium genus are traditionally used to treat prostatitis and other urinary tract disorders and are particularly rich in ellagitannins and flavonol 3-O-glycosides. The aim of this work was to evaluate the inhibitory activity of different extracts from E. angustifolium L. and E. parviflorum Schreb. and their major bioactive compound, oenothein B, against a panel of Gram-positive (Enterococcus faecalis ATCC 29212, Enterococcus faecalis BS, Staphylococcus aureus ATCC 25923, Staphylococcus aureus ATCC 29213, and Staphylococcus aureus ATCC 43300) and Gram-negative (Escherichia coli ATCC 25922, Escherichia coli ATCC 35218, Escherichia coli BS, Klebsiella pneumoniae ATCC 13883, Klebsiella pneumoniae ATCC 70063, Klebsiella pneumoniae BS, Proteus mirabilis BS, and Pseudomonas aeruginosa ATCC 27853) bacteria responsible for prostatitis. Methods: Aqueous and ethanolic raw extracts were prepared, and the latter were further purified using the resin AmberliteTM XAD7HP. Then, an HPLC-MS/MS method was developed for the quantification of the marker bioactives and their levels were correlated with the antimicrobial activity. Results: Purified extracts were richer in polyphenols (330.80 and 367.66 mg/g of dry extract for E. angustifolium and E. parvifolium, respectively) than the raw extracts. Oenothein B was the predominant compound in all the extracts (119.98 to 327.57 mg/g of dry extract). The minimum inhibitory concentrations (MICs) in the range of µg/mL indicated significant antibacterial activity, which was higher for the purified extracts and oenothein B (MIC values from 4 to 16 and 8 to 1024 µg/mL on Gram-positive and Gram-negative strains, respectively). Conclusions: These results outline the outstanding potential of E. angustifolium and E. parviflorum extracts and oenothein B as therapeutic alternatives or complementary agents to conventional antibiotic treatments of prostatitis and other urinary tract infections. [ABSTRACT FROM AUTHOR] more...

Objectives: Five solvent extracts (n-hexane, ethyl acetate, ethanol, ethanol/water (70%), and water) of Gladiolus italicus Mill. from Turkey were evaluated for chemical and biological properties. Methods: Antioxidant activities, inhibitory properties against key enzymes involved in the etiology of chronic diseases were tested, as well as cytotoxic effects on different cell lines. Chemical characterization was also carried out to determine the most abundant compounds of each extract. Results: The highest total phenolic content (TPC) was observed in the water extract while highest TFC in ethanol/water extract. The most abundant compounds in the extracts were hyperoside (69041.06 mg kg−1), isoquercitrin (46239.49 mg kg−1), delphindin-3,5-diglucoside (42043.81 mg kg−1), myricetin (21486.61 mg kg−1), and kaempferol-3-glucoside (21199.76 mg kg−1). Molecular dynamic (MD) simulations confirmed the structural stability and dynamic conformational integrity of these complexes over a period of 100 ns. In network pharmacology, A total of 657 unique target genes were screened: 52 associated with programmed cell death-1 (PD-1), 85 with vascular endothelial growth factor receptor-2 (VEGFR2), and 130 with fibroblast growth factor receptor-2 (FGFR2), identifying crucial gene interactions for these proteins. Gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses were conducted, revealing significant interactions and pathways such as the advanced glycation end products (AGE) and their receptors (RAGE) signaling pathway in diabetic complications and T- helper 17 (Th17) cell differentiation, among others. This elucidation of complex networks involving key genes like AKT Serine/Threonine Kinase 1 (AKT1), MYC proto-oncogene (MYC), tumor protein 53 (TP53), Interleukin 6 (IL6), and tumor necrosis factor (TNF) provides a promising foundation for the development of targeted therapies in the treatment of non-communicable diseases. Conclusion: These results show that G. italicus could be a natural source of potent antioxidants and enzyme inhibitors which need to be further explored for the development of biopharmaceuticals. [ABSTRACT FROM AUTHOR] more...

Alkaloids are a group of secondary metabolites that generate great interest since ancient times. Numerous Solanaceae plants are rich sources of tropane alkaloids as hyoscyamine and scopolamine which are obtained mainly from Hyoscyamus niger, Datura stramonium, Atropa belladonna, Mandragora officinarum. In the present study it was developed an HPLC-DAD using an XBridge Phenyl column for the quantification of scopolamine and hyoscyamine, molecules used in pharmaceutical industry to treat stomach or intestinal disorders. A. belladonna presented hyoscyamine and scopolamine, the first one ranged from 1466 to 5117 mg/Kg DW while the second one ranged from 140 to 1743 mg/Kg DW. In D. stramonium, hyoscyamine was not found while scopolamine ranged from 430 to 8980 mg/Kg DW. On the contrary H. niger and M. officinarum did not contain any trace of these alkaloids. This is the first work in which different parts of four Solanaceae were analysed for their hyoscyamine and scopolamine content. [ABSTRACT FROM AUTHOR] more...

The main cause of cancer death among women is breast cancer. The most common type of breast cancer is the estrogen receptor positive breast cancer. Discovery of estrogen receptor provided a highly effective target for treatment of hormone-dependent breast cancer. Selective estrogen receptor inhibitors are useful for halting the growth of breast cancer cells and inducing apoptosis. Tamoxifen, a popular selective estrogen receptor modulator, can treat breast cancer but also has unfavourable side effects due to its estrogenic activity in other tissues. Many herbal remedies and bioactive natural compounds, such as genistein, resveratrol, ursolic acid, betulinic acid, epigallocatechin-3-gallate, prenylated isoflavonoids, zearalenol, coumestrol, pelargonidin, delphinidin, and biochanin A, have the ability to specifically modulate the estrogen receptor alpha. Moreover, several of these compounds speed up cell death by supressing estrogen receptor gene expression. This opens wide avenue to introduce number of natural medicines with a revolutionary therapeutic impact and few side effects. [ABSTRACT FROM AUTHOR] more...

This study assessed the impact of full and late flowering stages on the polyphenols and enzyme inhibitory properties of Hypericum perforatum from Poland. Recognizing the significance of phenolic compounds in disease prevention and melatonin's emerging protective role, we employed an UHPLC-MS/MS system to quantify 38 phenolic compounds, not typical of St. John's wort, and to develop a new method for melatonin quantification. Afterward, the extracts were tested for their antioxidant capabilities (using phosphomolybdenum, DPPH, ABTS, FRAP, CUPRAC and ferrous chelating assays). Moreover, we investigated enzymes (acetylcholinesterase, butyrylcholinesterase and tyrosinase) involved in neurodegenerative disorders and (α-amylase and α-glucosidase) in diabetes. This study recognized the importance of phenolic compounds in disease prevention and explored the emerging protective role of melatonin, taking into account the floral ontogeny of the plant. Indeed, the full-flowering plant contained the greatest concentration of phenolic compounds (a total of 65,276.5 µg/g): hyperoside (18,726.59 µg/g), isoquercitrin (11,895.02 µg/g) and delphindin-3.5-diglucoside (10,619.51 µg/g), and showed the highest inhibitory enzyme activity. Moreover, only full-flowering St. John's wort contained melatonin (40 ng/g). Our results offer additional perspectives on the chemical-biological characteristics of H. perforatum and scientific knowledge that testifies to the importance of considering plant growth conditions for the development of nutraceuticals. [ABSTRACT FROM AUTHOR] more...

The present study was designed to determine the phenolic constituents, antioxidant, and enzyme inhibition activities of aerial parts and bulbs of Allium lycaonicum (family Amaryllidaceae). Extracts were prepared by maceration and Soxhlet/infusion using hexane, methanol, and water as extraction solvents. Generally, extracts from the aerial parts showed higher total phenolic and individual components and antioxidant activity than their respective bulb extracts. Maceration with water was the best to extract total phenolic content from the aerial parts (29.00 mg gallic acid equivalents (GAE)/g), while the Soxhlet extraction with hexane (22.29 mg GAE/g) was the best for the bulb. Maceration with methanol recovered the highest total flavonoid content from both the aerial parts (41.95 mg (rutin equivalents (RE)/g) and bulb (1.83 mg RE/g). Polar extracts of aerial parts were characterized by higher abundance of kaempferol-3-glucoside (≤20,624.27 µg/mg), hyperoside (≤19,722.76 µg/g), isoquercitrin (≤17,270.70 µg/g), delphindin-3,5-diglucoside (≤14,625.21 µg/g), and rutin (≤10,901.61 µg/g) than the bulb. Aerial parts' aqueous extract, prepared by maceration, exerted the highest anti-ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical activity (64.09 mg trolox equivalents (TE)/g), Cu++ (83.03 mg TE/g) and Fe+++ (63.03 mg TE/g) reducing capacity while that prepared by infusion recorded the highest anti-DPPH (2,2-diphenyl-1-picrylhydrazyl) radical (31.70 mg TE/g) and metal chelating (27.66 mg EDTAE/g) activities. The highest total antioxidant activity (1.46 mmol TE/g) was obtained by maceration of the bulb with water. Extracts obtained by organic solvents showed remarkable enzyme inhibition properties against the tested enzymes. Soxhlet extraction of the bulb with hexane and methanol recorded the highest acetylcholinesterase inhibition (4.75 mg galanthamine equivalents (GALAE)/g) and tyrosinase inhibition (139.95 mg kojic acid equivalents/g) activities, respectively. Extracts obtained by maceration of the bulb with methanol and the aerial parts with hexane exerted the highest glucosidase inhibition (3.25 mmol acarbose equivalents/g) and butyrylcholinesterase inhibition (20.99 mg GALAE/g) activities, respectively. These data indicated that A. lycaonicum is a source of bioactive molecules with potential antioxidant and enzyme inhibition properties. Nonetheless, the extracts obtained through various solvents and extraction techniques showed variations in their phytoconstituent composition and biological properties. [ABSTRACT FROM AUTHOR] more...

AbstractLamium orientale E.H.L. Krause is a herbaceous annual plant species in the Lamiaceae family. In the present study, anticancer, antioxidant, antibacterial, enzyme inhibitory, and quorum sensing inhibitory (on the inhibition of biofilm formation and violacein pigment production) activities of infusion and methanol (MeOH) extracts of roots, stems, leaves, and flowers of L. orientale were evaluated. The total phenolic-flavonoid contents and the phytochemical profiles of the extracts were determined using colorimetric assays and high-performance liquid chromatography-electrospray ionization tandem mass spectrometry (HPLC-ESI-MS/MS), respectively. The leaf extracts had the maximal levels of flavonoids and phenolics. Chlorogenic acid was most concentrated in the extracts. Based on several antioxidant activity assays, the MeOH extract of the flowers and infusion extract of the leaves had potent antioxidant activities. The MeOH extract of the stems exhibited the highest activities against acetylcholinesterase and butyrylcholinesterase, while the MeOH extract of the roots demonstrated the highest activities against tyrosinase, amylase, and glycosidase. The highest anticancer activity was determined for the MeOH extract of the roots against the MCF-7 cells (IC50=425.7 µg/mL). The MeOH extract of leaves and all infusion extracts significantly inhibited biofilm formation in Pseudomonas aeruginosa. The results suggested that L. orientale extracts may have significant potential for developing new therapeutic approaches owing to their high content of bioactive molecules. [ABSTRACT FROM AUTHOR] more...

Boscia coriacea Graells (BC), Grewia erythraea (Schweinf.) Chiov. (GE), Ochradenus baccatus Delile (OB), and Orthosiphon pallidus Royle ex Benth. (OP) are medicinal plants used in Djibouti. They were evaluated to determine their total phenolic content (TPC), flavonoid content (TFC), and phytochemical profile using HPLC-MS/MS. Additionally, their antioxidant capacity was assessed through five various methods. Enzymatic activities were also measured, focusing on acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-amylase, α-glucosidase, and tyrosinase. OP extract had the highest TPC and exhibited the best antioxidant capacity, whereas OB and BC extracts had the highest TFC. Twenty-seven compounds were identified and quantified by LCMS. GE extract demonstrated the highest AChE activity, whereas OP extract had the highest BChE activity. BC was most active against α-amylase and α-glucosidase, and only GE and OP extracts showed tyrosinase inhibition in vitro. In silico analysis, the compounds were optimized and docked to the human tyrosinase-related protein 1 using AutoDock Vina, with absorption, distribution, metabolism, and elimination to evaluate their suitability based on key therapeutic criteria. Chlorogenic, neochlorogenic, gallic acids, and quercetin emerged as promising tyrosinase inhibitors. These plants can be a viable source in the prevention and treatment related to tyrosinase enzyme inhibition., (© 2024 Wiley‐VHCA AG, Zurich, Switzerland.) more...