LC/MS/MS Phenolic Profile, Antioxidant Capacity, Angiotensin-Converting Enzyme (ACE) and Glutathione S Transferase (GST) Inhibitory Properties of Ultrasound-Assisted Propolis Extracts.

Resinous beehive product propolis has many biological activities. It contains various aromatic substances that have great differences in their chemical composition depending on the natural flora. Thus, chemical characterization and biological properties of propolis samples is an important subject for the pharmaceutical industry. In this study, the propolis samples collected from three cities in Turkey were prepared as methanol (MEP), ethanol (EEP), chloroform (ChlEP), hexane (HxEP), and ethyl acetate (EAEP) extracts using an ultrasonic assisted technique. The antioxidant capacities of the samples were evaluated by free radical scavenging activity (DPPH), cation radical scavenging activity (ABTS), and reducing activity (CUPRAC) and (FRAP). The strongest biological activities were detected in ethanol and methanol extracts. Enzyme inhibition of the propolis samples were determined against the human glutathione S-transferase (GST) and angiotensin converting enzyme (ACE). IC50 values of MEP1, MEP2, and MEP3 samples against the ACE were found as 13.9 µg/mL, 14.8 µg/mL, and 12.8 µg/mL, while against the GST IC50 values of MEP1, MEP2, and MEP3 samples were as 5.92 µg/mL, 9.49 µg/mL, and 5.72 µg/mL. To know the possible causes of the biological test results advanced LC/MS/MS method was applied. trans-ferulic acid, kaempferol, and chrysin were found as the most abundant phenolic compounds in each sample. The propolis extracts obtained using the proper solvent have a good potential to be used in pharmaceuticals to treat the diseases related to oxidative damage, hypertension, and inflammation. Finally, the interactions between chrysin, trans-ferulic acid and kaempferol molecules with ACE and GST receptors were analyzed using molecular docking study. Selected molecules interact with active residues by binding to the active site of the receptors.

The effects of Daucus carota extract against PC3, PNT1a prostate cells, acetylcholinesterase, glutathione S-transferase, and α-glycosidase; an in vitro-in silico study.

Daucus carota L. ssp. major (DCM) plant is widely used in traditional medicine to treat some types of cancer and various diseases. Therefore, we evaluated the biological activities of this plant to define its effects against prostate cancer (PCa), Alzheimer's disease (AD), oxidation, and diabetes mellitus (DM) as well as identified its phenolic composition. To determine the anti-cancer properties of the plant extract, we treated PCa cells with the extract at a concentration range of 0.25, 0.5, 1, 2, and 4 mg/ml. Significant results were obtained against the PC3 cells compared to normal PNT1a prostate epithelial cells. As a result of precise measurements at the millimolar level, it was observed that the plant extract showed an effective inhibition (IC50 ) against glutathione S-transferase (GST; 12.84 mM), acetyl cholinesterase (AChE; 15.07 mM), and α-Gly (11.75 mM) enzymes when compared with standard inhibitors. Antioxidant activities of DCM methanol extract were determined via two well-known in vitro techniques. The extracts showed antioxidant activities against the DPPH and ABTS+ . The LC-ESI-MS/MS was used to determine the phenolic compounds of methanol extract from DCM. Chlorogenic acid (2,089.096 µg/g), shikimic acid (193.14 µg/g), and coumarin (113.604 µg/g) were characterized as major phenolic compounds. In addition, the interactions of chlorogenic acid, chrysin, coumarin, and shikimic acid with the used three enzymes have been calculated using molecular docking simulation. PRACTICAL APPLICATIONS: Plant natural phenolic compounds have protective effects such as anti-inflammatory, antioxidant, anticarcinogen, and enzyme inhibitory. Therefore, it has an important place in the food and pharmaceutical industry. The present study aims to reveal the enzyme inhibitory, antioxidant, and anticarcinogenic properties of the Daucus carota ssp. Major (DCM) plant extract. Significant results were obtained against the PC3 cells compared to normal PNT1a prostate epithelial cells. DCM extract demonstrated considerable antioxidant activity and inhibitory potential on used metabolic enzymes. These biological effects are thought to have a relationship with rich chemical composition.

Chemical constituent and radical scavenging antioxidant activity of Anthemis kotschyana Boiss.

Phenolic content and antioxidant activity of Anthemis kotschyana Boiss. var. discoidea (A. kotschyana) were reported in this study. The ethanol extract of Anthemis kotschyana (EEA) and the water extract of Anthemis kotschyana (WEA) were prepared and used for biochemical analyses. Radical scavenging antioxidant capacities of EEA and WEA were evaluated by DPPH (1,1-diphenyl-2-picrylhydrazyl) free radical scavenging method. Another goal of the study was to evaluate the phenolic compositions of A. kotschyana by liquid chromatography and tandem mass spectrometry (LC-MS/MS). Rhamnetin (5.484 ± 0.020 ppm; µg/g extract) and quinic acid (2.251 ± 0.012 ppm; µg/g extract) were identified as major two compounds in the plant sample. This study will be a scientific base for further studies about A. kotschyana for plant biochemistry and plant-based pharmacological industry.

Phytochemical Content, Antidiabetic, Anticholinergic, and Antioxidant Activities of Endemic Lecokia cretica Extracts.

The aim of this work was to investigate the enzyme inhibition, antioxidant activity, and phenolic compounds of Lecokia cretica (Lam.) DC. Acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glycosidase enzymes were strongly inhibited by the L. cretica extracts. IC50 values for the three enzymes were found as 3.21 mg/mL, 2.1 mg/mL, and 2.07 mg/mL, respectively. Antioxidant activities were examined in both aqueous and ethanol (EtOH) extracts using CUPRAC, FRAP, and DPPH method. Also, the phenolic compounds of the endemic plant were identified and quantified by using HPLC/MS/MS. According to the results, the extracts have remarkable antioxidant activities. The most abundant phenolic acids of L. cretica in EtOH extract were determined as quinic acid (12.76 mg/kg of crude extract), chlorogenic acid (3.39 mg/kg), and malic acid (2.38 mg/kg).

Phytochemical content, antioxidant activity, and enzyme inhibition effect of Salvia eriophora Boiss. & Kotschy against acetylcholinesterase, α-amylase, butyrylcholinesterase, and α-glycosidase enzymes.

Many taxa of Salvia genus have been used in herbal beverages, food flavoring, cosmetics, and pharmaceutical industry. In this paper, chemical compounds of Salvia eriophora (S. eriophora) leaves were determined by LC-MS/MS (Liquid Chromatography tandem Mass Spectrometry). Salvigenin (158.64 ± 10.8 mg/kg), fumaric acid (123.09 ± 8.54 mg/kg), and quercetagetin-3.6-dimethylether (37.85 ± 7.09 mg/kg) were detected as major compounds in the ethanol extract, whereas fumaric acid (555.96 ± 38.56 mg/kg), caffeic acid (103.62 ± 20.51 mg/kg), and epicatechin (83.19 ± 8.43 mg/kg) were detected as major compounds in the water extract. Furthermore, enzyme inhibition of S. eriophora against acetylcholinesterase (AChE), α-amylase (AM), butyrylcholinesterase (BChE), and α-glycosidase (AG) enzymes were detected. AChE, BChE, AG, and AM enzymes were very strongly inhibited by S. eriophora water extract (WES) and S. eriophora methanol extract (MES). Additionally, antioxidant potential of S. eriophora was determined by in vitro analytical methods. IC50 values of WES and MES were performed for radicals. PRACTICAL APPLICATIONS: Metabolic enzymes have crucial functions on living systems due to inhibition or activation of them mainly attributed with some health disorders. AChE, BChE, AM, and AG enzymes have important roles on carbohydrate metabolism or cholinergic pathways. The relation between enzyme inhibition effect and phenolic compounds or antioxidant activity need to be confirmed. Thus, many studies tested to clarify this relation for pure samples or plant extracts. To the best of our knowledge, this is the first report about inhibition effects of Salvia eriophora extracts against AChE, BChE, AM, and AG enzymes as well as their phenolic contents and antioxidant activities.

Evaluation of antioxidant capacity of endemic plant Marrubium astracanicum subsp. macrodon: Identification of its phenolic contents by using HPLC-MS/MS.

Antioxidant properties of Marrubium astracanicum subsp. macrodon solvent extracts were measured by both cupric ion reducing antioxidant capacity (CUPRAC) and ferric reducing antioxidant power (FRAP) methods. According to the results, ethanol extract of the plant has high potential of reducing antioxidant activity on CUPRAC method. However, water extract of the plant has lower antioxidant potential. Furthermore, both water and ethanol extracts showed lower reducing antioxidant activity compare to standards on FRAP method. Moreover, the composition and content of plant leaves were detected by UHPLC-ESI-MS/MS. High concentrations of quinic acid, p-coumaric acid and malic acid were determined.