Enzyme Inhibitory Activity Research Articles

Kombucha beverages made from Camellia nitidissima Chi and Camellia sinensis flowers—physicochemical properties, sensory properties and bioactivity

Recently, various plant materials other than tea have been used as substrates for kombucha beverages. To improve the aroma and other qualities of kombucha, Camellia sinensis and Camellia nitidissima Chi flowers were used as raw materials to prepare novel kombucha beverages (marked as TFK and GFTK), which were systematically compared to traditional kombucha made from black tea. The results revealed that the biomass of kombucha made from TFK increased the most among all samples. TFK had the highest content of organic acids, with 9.03 g/L of acetic acid and 5.57 g/L of gluconic acid. Metabolomic analysis revealed that TFK showed the highest concentration of organic nitrogen compounds, whereas GFTK had the highest concentration of flavonoids. There were 183 kinds of volatile components identified in the 3 kombuchas, only 20 of which were common aroma components. Among the three kombucha beverages, TFK had the highest digestive enzyme inhibitory activity and was also second only to GFTK in terms of anti-oxidant properties. In terms of sensory properties, TFK had a higher fruit score compared to GFTK, but there was no significant difference in floral intensity between these two samples. Therefore, the C. sinensis flower is more suitable for preparing kombucha.

Synthesis, Characterization, Antibacterial Evaluation, and Enzyme Inhibition Activity of a Novel Nitrogen-containing Heterocyclic Sulfonamide

Synthesis, Characterization, Antibacterial Evaluation, and Enzyme Inhibition Activity of a Novel Nitrogen-containing Heterocyclic Sulfonamide

Discovery of Novel N-Phenyltriazinone Derivatives Containing Oxime Ether or Oxime Ester Moieties as Promising Protoporphyrinogen IX Oxidase Inhibitors.

Protoporphyrinogen IX oxidase (PPO, EC 1.3.3.4) is one of the most important targets for the discovery of green herbicides. In order to find novel PPO inhibitors with a higher herbicidal activity, a series of novel N-phenyltriazinone derivatives containing oxime ether and oxime ester groups were designed and synthesized based on the strategy of pharmacophore and scaffold hopping. Bioassay results revealed that some compounds showed herbicidal activities; especially, compound B16 exhibited broad-spectrum and excellent 100% herbicidal effects to Echinochloa crusgalli, Digitaria sanguinalis, Setaria faberii, Abutilon juncea, Amaranthus retroflexus, and Portulaca oleracea at a concentration of 37.5 g a.i./ha, which were comparable to trifludimoxazin. Nicotiana tabacum PPO (NtPPO) enzyme inhibitory assay indicated that B16 showed an excellent enzyme inhibitory activity with a value of 32.14 nM, which was similar to that of trifludimoxazin (31.33 nM). Meanwhile, compound B16 revealed more safety for crops (rice, maize, wheat, peanut, soybean, and cotton) than trifludimoxazin at a dose of 150 g a.i./ha. Moreover, molecular docking and molecular dynamics simulation further showed that B16 has a very strong and stable binding to NtPPO. It indicated that B16 can be used as a potential PPO inhibitor and herbicide candidate for application in the field.

Insight on Some Newly Synthesized Trisubstituted Imidazolinones as VEGFR-2 Inhibitors.

Two series of ten new 1,2,4-trisubstituted imidazolin-5-ones were synthesized and screened against MCF-7 breast cancer and A549 lung cancer cell lines to test their potential in vitro anticancer activity. The results revealed preferential activity of the tested compounds toward MCF-7 cell lines compared to A549 cell lines. The most promising ten compounds (3a, 3c, 3f, 3g, 3h, 3i, 3j, 6a, 6f, and 6i) were subjected to VEGFR-2 enzyme inhibitory activity testing to further explore their mechanism of action. The tested compounds showed remarkable enzyme inhibition in micromolar concentrations ranging from 0.07 to 0.36 μM, compared with Sorafenib and Sunitinib with IC50 values of 0.06 and 0.12 μM, respectively. The most promising candidate, 3j, was further evaluated for its cell cycle phases, apoptotic induction ability, as well as its antiproliferative activity and inhibitory potential for endothelial cell migration, analyzed by a cell scratch assay. Furthermore, in silico studies were also performed to identify and detect the stability of the binding poses.

In vitro digestibility and angiotensin converting enzyme (ACE) inhibitory activity of solid-state fermented fava beans (Vicia faba L.)

Reducing the content of quickly absorbed carbohydrates and saturated fats in snack formulations while increasing the consumption of high-quality proteins are effective strategies to prevent obesity in childhood. Thus, the nutritional value, digestibility, and functionality of fava beans (Vicia faba L.) fermented with Pleurotus ostreatus were examined as potential ingredients for food design. Solid-state fermentation enhanced the protein content by 16% with a rise in essential (25%) and non-essential (15%) amino acids while decreasing total carbohydrate content and tannin levels. Moreover, fermentation modified the amino acid profile released during digestion, increasing amino acids such as valine, isoleucine, and threonine, which are vital for health and development in childhood. Furthermore, the bioaccessible fraction of the fermented bean showed a 60% of ACE inhibition and improved magnesium bioaccessibility. Consequently, fava beans fermented with Pleurotus ostreatus emerged as a new ingredient in the development of new protein-rich snacks tailored for children and adolescents.

Development and Validation of a Liquid Chromatography-Tandem Mass Spectrometry Method for Screening Potential Citrate Lyase Inhibitors from a Library of Marine Compounds.

Tuberculosis, a persistent illness caused by Mycobacterium tuberculosis, remains a significant global public health challenge. The widespread use of anti-tuberculosis drugs has resulted in the emergence of drug-resistant strains, which complicates treatment efforts. Addressing this issue is crucial and hinges on the development of new drugs that can effectively target the disease. This involves identifying novel therapeutic targets that can disrupt the bacterium's survival mechanisms in various environments such as granulomas and lesions. Citrate lyase, essential for the survival of Mycobacterium species at lesion sites and in granulomatous conditions, is a potential target for the treatment of tuberculosis. This manuscript aimed to construct an efficient enzyme inhibitor screening platform using ultra-high performance liquid chromatography-quadrupole-time-of-flight mass spectrometry (UHPLC-QTOF MS). This system can accurately identify compounds with enzyme inhibitory activity from a library of marine terpenoids and phenolic compounds. Utilizing the screened herbal enzyme inhibitors as a starting point, we analyzed their chemical structures and skillfully built a library of marine compounds based on these structures. The results showed that all of the tested compounds from the phenolics library inhibited citrate lyase by more than 50%, and a significant portion of terpenoids also demonstrated inhibition, with these active terpenoids comprising over half of the terpenoids tested. The study underscores the potential of marine-derived phenolic and terpenoid compounds as potent inhibitors of citrate lyase, indicating a promising direction for future investigations in treating tuberculosis and associated disorders.

Valorization of various nut residues grown in Turkiye: Antioxidant, anticholinesterase, antidiabetic, and cytotoxic activities.

The utilization of plant-based residues has been extensively employed for the control of diverse illnesses, owing to their safety and minimal adverse effects. In the current study, it was aimed for the characterization of the bioactive, enzyme inhibitory, and cytotoxic activities of fresh pistachio shell skin (FPSS), green walnut husk and walnut membrane (GWH), almond outer shell and inner brown skin (ASIS), as well as peanut husk and inner skin (PHIS) to be used as industrial food processing by-products. The results showed that the samples exhibited different extraction yields, with GWH having the highest percentage at 15.18%, followed by FPSS at 12.81%, ASIS at 10.29%, and PHIS at 7.80%. FPSS had the highest total phenolic content (16.28 mg gallic acid equivalents (GAE)/g) as well as the best antioxidant capabilities for DPPH (8.96 mg Trolox equivalent (TE)/g), FRAP (11.46 mg TE/g), and ABTS (22.38 mg TE/g) assays. FPSS was followed by PHIS, ASIS, and GWH, respectively. Moreover, the extracts exhibited relatively low activity against acetylcholinesterase, α-glucosidase, and α-amylase compared to standard acarbose or galantamine. Furthermore, the extracts may have the potential to induce cytotoxic effects, varying from moderate to mild, on both cancerous (IC50 = 454.55-617.28 μg/mL) and healthy cells (IC50 = 438.60-490.20 μg/mL). The results of this research showed that shell residues of nut hold promise for a variety of industrial applications spanning the food, pharmaceutical, and cosmetic sectors.

Functional and Structural Properties of Type V Collagen from the Skin of the Shortbill Spearfish (Tetrapturus angustirostris).

Type V collagen is considered to be a crucial minor collagen in fish skin with unique physiological functions. In this research, the cDNAs of three procollagens (Tacol5a1, Tacol5a2, and Tacol5a3) in type V collagen were cloned from the skin of shortbill spearfish (Tetrapturus angustirostris). The open reading frames (ORFs) of Tacol5a1, Tacol5a2, and Tacol5a3 contained 5991, 4485, and 5607 bps, respectively, encoding 1997, 1495, and 1869 amino acid residues. Each of the deduced amino acid sequences of procollagens contained a signal peptide and a fibrillar collagen C-terminal domain (COLFI). A conserved thrombospondin-like N-terminal domain (TSPN) was found at the N-terminus of Tacol5a1 and 5a3 procollagens, whereas a von Willebrand factor (VWC) was found at the N-terminus of Tacol5a2 procollagen. Tacol5a1, Tacol5a2, and Tacol5a3 had their theoretical isoelectric points of 5.06, 6.75, and 5.76, respectively, and predicted molecular weights of 198,435.60, 145,058.48, and 189,171.18, respectively. The phylogenetic tree analysis revealed that Tacol5a1 of shortbill spearfish clustered with that of yellow perch (Perca flavescens) instead of broadbill swordfish (Xiphias gladius). In addition, type V collagen was extracted from the shortbill spearfish skin. The in silico method demonstrated that shortbill spearfish type V collagen has a high potential for angiotensin-converting enzyme (ACE) inhibition activity (79.50%), dipeptidyl peptidase IV inhibition (74.91%) activity, and antithrombotic activity (46.83%). The structural clarification and possible functional investigation in this study provide the foundation for the applications of exogenous type V collagen derived from fish sources.

Skin anti-aging potential of Launaea procumbens extract: Antioxidant and enzyme inhibition activities supported by ADMET and molecular docking studies

Aging is a natural process that occurs in all living organisms. Particularly, the skin embodies aging since it serves as a barrier between the body and its surroundings. Previously, we reported the wound healing effect of Launaea procumbens and identified compounds therein. The study aims to explore the skin anti-aging properties of the plant extract. To that effect, the antioxidant potential of L. procumbens methanolic extract (LPM) was assessed using two complementary DPPH and FRAP assays. The enzyme inhibitory effect of the extract on collagenase, elastase, hyaluronidase, and tyrosinase was evaluated to assess the direct skin anti-aging effects. Similarly, the anti-inflammatory activity was evaluated to explore the indirect anti-aging effects via the assessment of extract inhibitory effects on cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). In addition, ADMET and molecular docking studies were performed to explore the interaction mechanisms of identified compounds in LPM with target enzymes. LPM demonstrated significant antioxidant activity in DPPH (IC50 = 29.08 µg/mL) and FRAP (1214.67 µM FeSO4/g extract) assays. Plant extract showed significant inhibition of collagenase, elastase, hyaluronidase, and tyrosinase (IC50 = 52.68, 43.76, 31.031, and 37.13 µg/mL, respectively). The extract demonstrated significant COX-2 and 5-LOX inhibition capacity with IC50 values of 8.635 and 10.851 µg/mL, respectively. The molecular docking study revealed the high potential of the identified compounds to bind to the active sites of enzymes crucially involved in the skin aging process. ADMET analysis of the compounds revealed their good absorption, distribution, and metabolism profiles, and they were found to be safe as well. Study findings suggest L. procumbens as a promising source for the development of natural skin anti-aging and antioxidant compounds. This, in turn, may facilitate its incorporation into cosmetic formulations after further investigation.

Centrosymmetric homo- and heteroleptic core paddle-wheel copper(II) carboxylates; Syntheses, crystal structures, antioxidant, anticancer and enzyme inhibition activity

Synthesis and characterization of homo- (C5H7N2)2[Cu2(3,5-F2C6H3CH2COO)6] (1) and heteroleptic [Cu2(3,5-F2C6H3CH2COO)4(2-CH3Py)2] (2) core paddle-wheel copper(II) carboxylates is reported in the present work. The characterization was made by spectroscopic techniques, elemental and single crystal XRD analyses. The single crystal XRD analysis revealed a rare homoleptic anionic copper(II) carboxylate complex (1) consisting 2-aminopyridinium counter cations and a neutral heteroleptic copper(II) carboxylate complex (2) consisting 2-methyl pyridine as a co-ligand. The copper ions adopted a distorted square pyramidal geometry in both the paddle-wheel dimeric complexes. To evaluate the biological potency of the synthesized complexes, in vitro antioxidant, enzymes inhibition and anticancer activities were performed. The synthesized complexes have shown overall better biological activity compared to the ligand acid. Complex 2 was the most potent DPPH (IC50 =180.96 ± 9.04 µg/mL) and •OH (IC50 = 189.51 ± 9.33 µg/mL) radicals scavenger, α-amylase (IC50 = 441.86 µg/mL) and acetylcholinesterase (IC50 = 88.62 µg/mL) inhibitor. Furthermore, complex 2 activity against malignant glioma U-87 cell line (IC50 = 21.95 µg/mL) was also highest among the tested compounds. However, complex 1 with an IC50 value of 51.83 µg/mL has shown somewhat better inhibition of the butyrylcholinesterase enzyme compared to the complex 2 (IC50 = 56.36 µg/mL).

Exploring the Composition and Bioactivity of Hedychium flavum Leaf and Stem Essential Oil: In Vitro Assessment of Antibacterial, Antioxidant, Cytotoxicity, and Enzyme Inhibitory Activities

Hedychium flavum is an edible, medicinal, and aromatic plant widely cultivated for its essential oil. So far, little studies have been done on its phytoconstituents and bioactivities. Hence, the research aimed to determine the chemical constituents of leaf essential oil (L-EO) and stem essential oil (S-EO) of H. flavum and first estimate their antibacterial, antioxidant, cytotoxic, and enzyme inhibitory activities. According to gas chromatography-flame ionization detector/mass spectrometer (GC-FID/MS) assay, L-EO was mainly composed of β-pinene (33.4%), α-pinene (10.4%), humulene (6.8%), β-caryophyllene (6.0%), eucalyptol (6.0%), caryophyllene oxide (5.5%), endo-borneol (3.8%), humulene epoxide II (3.7%), and D-limonene (3.2%). The predominant components of S-EO were β-pinene (17.2%), eucalyptol (9.7%), nerolidol (7.8%), α-phellandrene (6.7%), α-pinene (5.8%), β-caryophyllene (5.4%), terpinen-4-ol (4.5%), D-limonene (4.4%), p-cymene (3.7%), endo-borneol (3.5%), and α-terpineol (3.5%). For the bioactivities, L-EO and S-EO showed strong antibacterial activity against Escherichia coli, Enterococcus faecalis, and Bacillus subtilis with the minimum inhibitory concentration (MIC) of 9.77–625.00 µg/mL and the minimum bactericidal concentration (MBC) of 9.77–1250.00 µg/mL. Both L-EO and S-EO exhibited moderate antioxidant activity in the DPPH (14.52 ± 0.93 mg/mL and 4.73 ± 0.15 mg/mL, respectively) and ABTS (4.05 ± 0.75 mg/mL and 2.38 ± 0.14 mg/mL, respectively) free radical scavenging capacity. S-EO showed selective cytotoxicity on human leukemic K562 cell line (IC50 = 93.94 ± 0.91 µg/mL), which was nearly three times that of noncancer L929 cell line (IC50 = 294.49 ± 9.40 µg/mL). In enzyme inhibitory properties, L-EO exerted a potent inhibition on α-glucosidase (IC50 = 1.03 ± 0.02 mg/mL), and both essential oils had weak inhibition against cholinesterase and tyrosinase. Thus, H. flavum L-EO and S-EO possess antibacterial, antioxidant, cytotoxic, and enzyme inhibitory activities with potential for exploitation in the food, cosmetic, and pharmaceutical industries.

Chemical composition and antioxidant, enzyme inhibition and cytoprotective activity of two Antarctic lichens of the genus Psoroma (Pannariaceae)

Lichens contain different types of chemical compounds with multiple biological activities that demonstrate their potential pharmacological use. This research aims to report the metabolomic identification of the ethanolic extracts of P. antarcticum and P. hypnorum, their antioxidant, enzyme inhibitory, and their cytoprotection activity. Sixteen metabolites were identified in P. antarcticum and twelve in P. hypnorum; the extracts reported variable antioxidant activity with IC50 >350 µg/mL in DPPH·, values >18 µmol Trolox/g in ORAC and >40 µmol Trolox/g in FRAP and a phenolic compound content >10 mg GAE/g, as well as significant results in cholinesterases, α-glucosidase, pancreatic lipase, α-amylase, and tyrosinase enzyme inhibition activities with IC50 ranging from 18 to 510 µg/mL, and which were complemented by molecular docking experiments. Both extracts showed improved cytoprotection at the concentrations of 0.5 to 1.0 μg/mL. This study contributes to the knowledge of the chemical diversity of Antarctic lichen extracts and their effectiveness in the evaluation of biological activities related to neurodegenerative diseases and metabolic syndrome.

Analyzing the Chemical Constituents and In Vitro Biological Effects of Extracts Artemisia absinthium L. Extracts Obtained Using Different Methodologies and Solvents.

The present study aimed to investigate the chemical constituents of different extracts from aerial parts of A. absinthium and to evaluate their antioxidant and enzyme inhibition activity. Extracts were prepared by maceration, infusion or Soxhlet techniques. Results showed that the highest total phenolic and flavonoids contents was recorded respectively from the hexane extract prepared by maceration and ethyl acetate extract obtained by Soxhlet method. The characteristic compounds of Artemisia species artemetin, casticin, sesartemin and yangambin in addition to coumarins were identified in all extracts. Aqueous extract obtained by infusion exerted the highest radical scavenging and ions reducing properties while that prepared by maceration displayed the highest chelating power. Methanol extracts obtained by the two methods of extraction exerted the highest anti-Tyr activity while that obtained by maceration showed the best α-glucosidase inhibition activity. These findings indicated that A. absinthium is a rich source of bioactive molecules with possible therapeutic applications.

Modification of Bioactive Properties in Food Protein Hydrolysates by Alcalase and Trypsin

Abstract Background Protein hydrolysates are the fragments of proteins that form during the hydrolysis with promised bioactive properties. Enzymatic hydrolysis produces bioactive peptides with specific amino acid profile. Among all the properties, angiotensin-I converting enzyme (ACE-I) inhibitory activity of the protein hydrolysates attained maximum attention to combat life-threatening disease like hypertension. Methodology In the present study 10 protein-rich food sources (> 20% protein content on dry basis) were used to prepare protein hydrolysates using alcalase and trypsin to investigate the effect of enzymes on ACE-I inhibitory and antioxidant activity. Results Among all the sources, the highest degree of hydrolysis was observed in sardine (62.89%) followed by soybean (61.24%) when hydrolyzed by alcalase. Kidney pea exhibited highest ACE-I inhibitory activity with IC50 value of 0.517 and 0.521 when hydrolyzed using both trypsin and alcalase, respectively. All the sources selected showed nonsignificant changes in ACE-I inhibitory activity between alcalase and trypsin (p < 0.05) except Bengal gram and chicken. Antioxidant activity was higher in alcalase hydrolyzed egg yolk (43.08%). Conclusion Among the sources, all animal proteins hydrolyzed using alcalase exhibited significantly higher (p < 0.05) antioxidant activity than trypsin. However, protein hydrolysates prepared from sardine using alcalase would yield bioactive peptides with higher ACE-I inhibitory and antioxidant activity. Therefore, use of alcalase as a substitution for trypsin would be economical for large-scale production. Henceforth, food protein hydrolyzed by alcalase can be used as a functional ingredient for the development of functional or nutraceutical foods to combat lifestyle diseases.

Evaluation of potential anti-aging effects of Achillea phrygia Boiss. & Balansa (Asteraceae)

This study aims to determine the anti-aging effects of Achillea phrygia, an endemic plant, by evaluating its sun protection factor (SPF) level, antioxidant activity, total phenolic content, extracellular matrix-degrading enzymes (ECM) inhibition, genotoxic/anti-genotoxic, and cytotoxic activities. The SPF level was assessed using an in vitro quantitative method, while antioxidant capacity was determined through DPPH, β-carotene, and hydroxyl-radical (H2O2) scavenging assays. The total phenolic content was quantitatively conducted using the Folin Ciocalteu reagent. The inhibition of ECM-degrading enzymes was determined using matrix metalloproteinase-1 (MMP-1), hyaluronidase, and elastase enzymes. Genotoxic/anti-genotoxic properties were assessed using the AMES Salmonella/microsome assay, and cytotoxicity effects were assessed through the MTT assay. The results indicated that A. phrygia showed moderate SPF activity (SPF = 4.013) and exhibited IC50 values of 0.183 ± 0.03, 0.079 ± 0.51, and 1.18 ± 0.35 mg/mL for DPPH, β-carotene, and hydroxyl-radicals, respectively. The total phenolic content was measured to be 23.56 ± 1.42 mg GAE/g dry extract. Furthermore, the extract demonstrated inhibition of MMP-1 (47.98%) and elastase (39.2%) activities. Importantly, it did not induce DNA damage and showed antigenotoxic activity ranging from 10% to 65.6%. The cytotoxicity assay revealed an IC50 value of 42.41±4.05 µg/mL. These findings suggest that A. phrygia could be utilized as a cosmetic ingredient in skincare products due to its ability to protect against UV radiation, exhibit antioxidant properties, prevent extracellular matrix degradation, and inhibit DNA damage.

Chemical profiling and biological activities of the roots of Allochrusa gypsophiloides

Allochrusa gypsophiloides is one of the best-known endemic saponin bearing food plants of Central Asia. However, the plant’s secondary metabolites remain unmapped. The current study aimed to chemical profile of the metabolite in the plant roots by an untargeted UHPLC-ESI-MS, together with the isolation of the major compounds followed by a 2D NMR and HR-MS for identification and evaluation of the antioxidant and enzyme inhibitory activity of the extracts. The results revealed the presence of 48 putatively annotated metabolites comprising triterpene glycosides, phenolic compounds and their derivatives, organic acid glycosides, and lignan glycosides. The chromatographic separation and purification of the extract resulted in the isolation of four compounds where two new compounds and along with two known triterpenes were reported. The ethanol/water extracts showed a maximum effect in antioxidant assays, while the ethyl acetate extract achieved the best effect in the enzyme inhibitory assays.

AN INVESTIGATION OF THE ACE INHIBITORY ACTIVITY, ANTIOXIDANT CAPACITY, AND PHYTOCHEMICAL CONSTITUENTS OF POLAR AND NON-POLAR EXTRACTS OF ZIZIPHUS JUJUBA FRUIT: STATISTICAL SCREENING THE MAIN COMPONENTS RESPONSIBLE FOR BIOACTIVITY

Herein, the angiotensin I-converting enzyme (ACE) inhibitory activity, antioxidant capacity, total polyphenol contents (TPC), and phytochemical profiles of polar and non-polar extracts of dried Ziziphus jujuba fruits were investigated, along with the statistical determination of the main components responsible for ACE inhibitory activity. The non-polar extract expressed the strongest ACE inhibitory activity (99.81%) among the extracts. The non-polar extract also exhibited the highest DPPH scavenging activity (IC50 of 30.63), linoleic acid/β-carotene bleaching capacity (89.31%), and TPC (59.47 mg GAE/g). The phenolic profiles of the extracts were identified by LC-MS/MS, and the presence of seven triterpenoid species in the extracts was examined using GC-MS techniques. The principal constituents included 19 phenolics, 2 organic acids, and 4 triterpenoids. A Pearson correlation and principal component analysis were conducted to find the correlation between individual phenolic compounds and ACE inhibitory activity.

Effects of different extraction methods on the structure and function of blackberry seed polysaccharides

SummaryThe different extraction methods including hot‐water extraction, ultrasound‐assisted extraction, and microwave‐assisted extraction, enzyme‐assisted extraction, ultrasound and microwave‐assisted extraction, and ultrasound and enzyme‐assisted extraction (UEE) methods were carried out to extract blackberry seed polysaccharides (BSPs). The extraction yield, structure, antioxidant capacity, and glucometabolic enzyme inhibition activities of BSPs were determined in this work. Extraction methods have no influence on the monosaccharide composition of BSPs but affected the molar ratio of monosaccharides. Fourier transform infrared spectroscopy and X‐ray diffraction results showed that the extraction method cannot effect on the functional groups and crystal forms of BSPs. The findings also revealed that UEE led to the highest BSP extraction yield (4.56%), highest antioxidant capacities, and highest α‐amylase (48.49%) and α‐glucosidase (67.33%) inhibitory rates, which may because of the dispersed molecular weight distribution and loose microstructure of BSPs. These results suggest that UEE may be used in the industry to obtain BSPs with high functional activities.

Modulatory Effects of the Kuwanon-Rich Fraction from Mulberry Root Bark on the Renin-Angiotensin System.

In this study, we investigated the anti-hypertensive properties of mulberry products by modulating the renin-angiotensin system (RAS). Comparative analysis showed that the ethyl acetate fractions, particularly from the Cheongil and Daeshim cultivars, contained the highest levels of polyphenols and flavonoids, with concentrations reaching 110 mg gallic acid equivalent (GE)/g and 471 mg catechin equivalent (CE)/g of extract, respectively. The ethyl acetate fraction showed superior angiotensin-converting enzyme (ACE) inhibitory activity, mainly because of the presence of the prenylated flavonoids kuwanon G and H. UPLC/Q-TOF-MS analysis identified kuwanon G and H as the primary active components, which significantly contributed to the pharmacological efficacy of the extract. In vivo testing of mice fed a high-salt diet showed that the ethyl acetate fraction substantially reduced the heart weight and lowered the serum renin and angiotensinogen levels by 34% and 25%, respectively, highlighting its potential to modulate the RAS. These results suggested that the ethyl acetate fraction of mulberry root bark is a promising candidate for the development of natural ACE inhibitors. This finding has significant implications for the management of hypertension through RAS regulation and the promotion of cardiovascular health in the functional food industry.

Fatty Acid Composition, Antioxidant, and Enzyme Inhibition Activities of Cachrys Crassiloba (Boiss.) Meikle Fruit and Leaf Extracts

The genus Cachrys L. (Apiaceae) is distributed in the Mediterranean region and contains 11 species. C. crassiloba (Boiss.) Meikle is a species that grows in Southwest and Western Anatolia. Considering the literature studies, there were not enough studies on C. crassiloba. In this study, fatty acid composition, total phenol/flavonoid contents, antioxidant and acetyl-butrylcholinesterase, tyrosinase, and α-glucosidase enzyme inhibition activities of n-hexane and ethanol extracts prepared from C. crassiloba fruits and leaves were investigated by spectrophotometric methods at different concentrations. When the results were evaluated, it was found that the hexane extract of C. crassiloba leaf (123.92 ± 4.62 GA mg/g extract) had the highest total phenol content, while the ethanol extract of C. crassiloba fruit (134.38 ± 0.98 QE mg/g extract) had the highest flavonoid content. C. crassiloba hexane and ethanol leaf extracts (IC50= 8.04 ± 1.31 µg/mL; 10.30 ± 3.15 µg/mL) showed good antioxidant activity com-pared to the ascorbic acid (IC50= 14.59 ± 1.96 µg/mL) in DPPH assay. C. crassiloba leaf ethanol extract (IC50= 17.38 ± 5.02 µg/mL) has the highest ABTS scavenging activity. C. crassiloba extracts have mod-erate cholinesterase inhibitory activity. C. crassiloba leaf ethanol extract (IC50= 196.65 ± 1.94 µg/mL) has good tyrosinase enzyme inhibition activity. C. crassiloba leaf hexane extract (36.35% ± 1.13) was found to have significant inhibitory activity against α-glucosidase. In conclusion, besides its antioxidant activity, C. crassiloba may be effective against neurodegenerative diseases and skin disorders such as hyperpigmentation and diabetes mellitus, but further phytochemical analysis studies are required.