Phenolic Glycosides Research Articles

Bioassay-guided isolation and identification of antimutagenic compounds from Morina coulteriana and evaluation of its therapeutic potential.

BackgroundIn the expanding field of cancer research, antimutagenic studies hold a promising ground. In recent times these studies have shown a shift towards the diverse flora of nature and its potential to treat cancer. Genus Morina has been extensively used in Chinese, Tibetan, and Indian traditional medicine to cure numerous diseases. The plant Morina coulteriana has been traditionally used to cure eye diseases. Nevertheless, it has been explored for the first time for its antimutagenic/antigenotoxic potential and phytochemical profile. PurposeThe present study aimed to determine the antimutagenic/antigenotoxic potential of Morina coulteriana and the bioassay-guided identification of its bioactive constituents. MethodsThe methanol crude extract and its subsequent fractions were tested for antimutagenic/antigenotoxic activity in vitro (Ames assay) and in vivo (Chromosomal aberration assay in Balb/c mice). The active (ethyl acetate) fraction was further investigated to isolate and identify its bioactive compounds utilizing chromatographic purification and detailed spectroscopic techniques respectively. ResultsThe results revealed that the plant and its fractions were neither mutagenic nor toxic. The ethyl acetate fraction showed significant antimutagenic/antigenotoxic activity (66.13%) in vitro and (88.15%) in vivo. Further, four identified major compounds which were also tested in vitro. Our results revealed that the plant is a potent antimutagen. It worked in a dose-dependent manner and its administration decreased the mutagenic load on the cells both in vitro and in vivo experiments. The 2 isolated compounds viz.; 4hydroxyacetophenone, a phenol and picein, a phenolic glycoside were reported for the first time from the genus Morina. ConclusionThe findings of the present investigation clearly show that the plant M. coulteriana Royle has a strong antimutagenic potential. Its administration decreased the mutagenic load on the cells both in vitro and in vivo experiments Thus the present study provides a platform for the exploration of new plants with potential antimutagenic properties.

Pharmacognostic standardization and phytochemical evaluation of Ficus rumphii blume leaves in Thailand

BackgroundFicus rumphii Blume has long been used in ethnomedicinal practices and is regarded as one of the medicinal plants in Thai traditional herbal formulas for diabetes treatment. At present, published data on pharmacognostic study of this plant for its identity, quality, and purity is still limited. ObjectiveThis study aimed to establish the pharmacognostic standardization parameters of Ficus rumphii leaves in Thailand. MethodsThe pharmacognostic study of F. rumphii leaves collected from 12 different sources throughout Thailand was conducted according to the methods described in WHO guidelines including macroscopic, microscopic, physicochemical parameters, phytochemical screening, and TLC fingerprint. ResultsMacroscopic and microscopic characteristics of F. rumphii leaves were reported in this study. Physicochemical parameters showed the value of loss on drying (6.87 ± 0.79 %), total ash (16.28 ± 5.76 %), acid insoluble ash (7.54 ± 4.53 %), water content (9.58 ± 2.49 %), water extractive matters (4.71 ± 1.75 %) and ethanol extractive matters (1.30 ± 0.52 %). Preliminary phytochemical screening of hexane, ethanol, and aqueous extracted revealed the presence of phenolic, flavonoid, diterpene, triterpene, steroid, saponin, and cardiac glycoside which were confirmed by TLC fingerprint profiles of ethanolic extract of this plant. ConclusionThis study is the first report on the pharmacognostic specification of F. rumphii leaves in Thailand, which could be used as a reference for quality control and the species identification of this plant material.

Antibacterial and Antioxidant Activities of Flavonoids, Phenolic and Flavonoid Glycosides from Gouania longispicata Leaves

The leaves of Gouania longispicata Engl. (GLE) have been traditionally used to treat more than forty ailments in Uganda, including stomachache, lung and skin cancers, syphilis, toothache, and allergies. In this study, pure compounds were isolated from the methanolic extract of GLE leaves and their structures elucidated using ultraviolet visible spectroscopy, liquid chromatography–tandem mass spectrometry, high performance liquid chromatography, and 1D and 2D NMR techniques. The antibacterial and antioxidant activities of the compounds were assessed using the broth dilution and DPPH assays, respectively. Two known flavonoid glycosides (kaempferol-3-O-α-rhamnopyranoside and rutin), a phenolic glycoside (4,6-dihydroxy-3-methylacetophenone-2-O-β-D-glucopyranoside), and flavonoids (kaempferol and quercetin) were characterized. This is the first time that the kaempferol derivative, the acetophenone as well as free forms of quercetin, kaempferol, and rutin, are being reported in GLE and the Gouania genus. The compounds exhibited antibacterial activity against Streptococcus pneumoniae and Escherichia coli with minimum inhibitory concentrations between 16 µg/mL and 125 µg/mL. The radical scavenging activities recorded half-minimum inhibitory concentrations (IC50) ranging from 18.6 ± 1.30 µg/mL to 28.1 ± 0.09 µg/mL. The IC50 of kaempferol and quercetin were not significantly different from that of ascorbic acid (p > 0.05), highlighting their potential as natural antioxidant agents. These results lend credence to the use of GLE leaves in herbal treatment of microbial infections and oxidative stress-mediated ailments.

Metabolomics analysis of Cucumis melo var. flexuosus organs in correlation to its anti-inflammatory activity aided by chemometrics

Snake melon (Cucumis melo var. flexuosus, CM) is a gourd with health-promoting nutritional traits and unexplored phytochemicals. This study aims to comprehensively investigate the phytoconstituents in the fruits, leaves, roots, seeds, and stems of CM, using liquid chromatography-quadrupole time-of-flight tandem mass spectrometry. Consequently, 118 metabolites were identified, encompassing phenolic compounds, flavonoids, megastigmanes, lignans, cucurbitacins, and fatty acids. Multivariate data analysis revealed differences in the metabolite composition of CM organs and correlated these variations with the potential in-vitro anti-inflammatory properties assessed against RAW 264.7 macrophages through the down-regulation of cyclo-oxygenase-Ⅱ, nuclear factor-kappa B, and tumor necrosis factor-α. The results indicated that leaf and seed extracts showed the highest anti-inflammatory activity due to their enrichment in several flavonoids, phenolic glycosides, and a megastigmane. These findings emphasize the health benefits of CM organs as potential functional foods and functional food by-products, serving as a natural source for developing new anti-inflammatory agents.

Six new phenolic glycosides from the roots of Scrophularia ningpoensis

Six new phenolic glycosides (1–6) and thirteen known compounds (7–19) were isolated from the roots of Scrophularia ningpoensis. Their structures were determined through comprehensive analyses of the physicochemical properties and spectroscopic data (1D NMR, 2D NMR, and HR-ESI-MS). The anti-inflammatory potential of all compounds was evaluated by determining their ability to inhibit lipopolysaccharide (LPS) induced NO production in RAW 264.7 macrophage cells. In addition, the cytotoxicity of all compounds on HepG2, 4 T1 and A549 cell lines was also evaluated.

Pelargonium graveolens: Towards In-Depth Metabolite Profiling, Antioxidant and Enzyme-Inhibitory Potential.

Pelargonium graveolens L'Hèr. (Geraniaceae) is renowned for its traditional use as a flavor, ornamental and medicinal plant. This work aimed at an in-depth study of the phytochemical profiling and in vitro antioxidant and enzyme inhibition assessment of a methanol-aqueous extract from P. graveolens leaves. A UHPLC-HRMS analysis revealed more than 110 secondary metabolites, including 8 acyltartaric and 11 acylcitric/acylisocitric acids; 8 gallotannins; 36 flavonols, flavanones and methoxylated flavonoids together with 17 phenolic and aliphatic acids; and 21 phenolic acid glycosides. For the first time, acylcitric acids along with feruloyl- and coumaroyltartaric acids are reported in the species. The leaf extract actively scavenged 2,2-diphenyl-1-picrylhydrazyl DPPH (273.45 mg trolox equivalent (TE/g)) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS•+) radicals (531.97 mgTE/g) and showed a high reducing power: 431.32 mg TE/g Cupric reducing antioxidant capacity (CUPRAC) and 292.21 mg TE/g Ferric reducing antioxidant power (FRAP). It possessed a metal chelating capacity (13.44 ethylenediaminetetraacetic acid equivalent (EDTAE)/g) and contained 2.71 mmol TE/g in the phosphomolybdenum assay. The rose geranium extract exhibited high inhibition towards acetyl- and butyrylcholinesterase (2.80 and 2.20 mg galantamine equivalent (GALAE)/g, respectively) and tyrosinase (75.49 mg kojic acid equivalent (KAE)/g). It inhibited α-glucosidase and α-amylase (3.75 mmol and 0.79 acarbose equivalent (ACAE)/g, respectively) and lipase (28.91 mg orlistat equivalent (OE)/g). This study sheds light into the future potential application of the rose geranium in pharmaceutical and nutraceutical products.

Two new phenolic glycosides from the roots of Iris domestica (L.) Goldblatt & Mabb and their cytotoxic activity

Two new phenolic glycosides, Diplostephioside D (1) and Diplostephioside E (2) together with ten known phenols (3–12) were isolated from the dried roots of Iris domestica (L.) Goldblatt & Mabb. Among them, compounds 4–9 have not been reported previously from the family Iridaceae. The chemical structures were elucidated based on extensive spectroscopic experiments, including 1D and 2D NMR as well as HR-ESI-MS, and comparison with those reported in the literature. All of the isolated compounds were evaluated for their cytotoxic activity against HeLa cells. Compounds 1, 2, 4, 8 and 12 showed cytotoxic activities with IC50 values ranging from 13.52 ± 1.52 to 53.33 ± 1.40 μM.

Comparative Proteomic Analysis Reveals the Effect Mechanisms of Glucose on the Biomass and Phenolic Glycoside Esters Synthesis Activity of Candida Parapsilosis ACCC 20221 Whole-Cell Catalyst.

A new Candida parapsilosis ACCC 20221 (C. parapsilosis ACCC 20221) whole-cell catalyst with a high phenolic glycoside esters synthesis activity and large biomass was obtained after culture with glucose. The possible mechanisms were revealed by using comparative proteomics. It found the expression of proteins involved in post-translational modification, protein turnover, and chaperone, and RNA processing and modification was upregulated, which ensured the metabolic balance and accurate translation, correct folding, and post-translational modification of proteins, thus enhancing the production of lipases in C. parapsilosis ACCC 20221 cultured with glucose. Moreover, the glycolysis pathway, tricarboxylic acid cycle, and fatty acids synthesis were enhanced, while the β-oxidation of fatty acids was weakened in C. parapsilosis ACCC 20221 cells cultured with glucose, which led to an increase in energy generation and cell membrane synthesis; thus, large biomass was obtained. In addition, CCE40476.1 and CAC86400.1, which were likely to exert arbutin esters synthesis activity in C. parapsilosis ACCC 20221, were screened, and it was found that vinyl propionate could easily enter the catalytic pocket of CCE40476.1 and form hydrogen bonding interactions with Leu191 and Ser266.

Ecological factors impacting genetic characteristics and metabolite accumulations of Gastrodia elata

ObjectiveThe investigation of the correlation between ecological factors and the genetic characteristics or metabolites of plants offers valuable insights into the regional causes of genetic and metabolic diversity. Here, Gastrodia elata, a medicinal plant, is employed as a model to explore the environmental factors that influence its genetic characteristics and metabolic accumulations. MethodsA total of 23 G. elata populations from six cultispecies and 11 cultivated regions were selected based on the predictions of the global geographic information system. The genetic characteristics of these populations were evaluated using highly polymorphic simple sequence repeat markers. Additionally, the metabolic accumulations and antioxidant capacity of mature tubers were measured employing colorimetry and high performance liquid chromatography (HPLC). Ecological data of each region were obtained from the WorldClim-global climate database and harmonized world soil database. To assess the influence of ecological factors on the genetic characteristics and metabolic profiles of G. elata, Pearson’s correlation analysis was conducted. ResultsGenetic variation among G. elata populations exceeded that within populations. Genetic diverisity, distance and structure manifested regional and species-specific patterns. Metabolic profiling and antioxidant capacity exhibited regional variations. Notably, the Lueyang region demonstrated that a content range of total polysaccharide, total protein, and phenolic glycosides was 9.34 %−189.67 % higher than the average. Similarly, in the Hubei region, total phenolic content, p-hydroxybenzyl alcohol content, and antioxidant indicators were observed to be higher than the average levels, by 106.57 %, 136.47 % and 12.50 %−91.14 %, respectively. Furthermore, ecological factors had a significant comprehensive impact on G. elata genetic characteristics (r > 0.256 and P<0.05). Multivariate metabolite accumulations in G. elata were influenced by dominant ecological factors. Temperature notably impacted the accumulation of total protein (|r| > 0.528 and P<0.05). Moisture, encompassing precipitation and soil content, significantly affected the production of phenolic glycosides (|r| > 0.503 and P<0.05). ConclusionThe genetic characteristics of G. elata manifested regional and species-specific patterns, with the metabolic accumulations and antioxidant capacity of mature tubers exhibited regional variations. Specifically, multivariate ecological factors comprehensively influenced genetic characteristics. Temperature and moisture played pivotal roles in regulating the accumulations of proteins and phenolic glycosides, respectively. These findings underscore the significant impact of ecological factors on the shaping of G. elata, highlighting their crucial role in enhancing the quality of Chinese medicinal materials.

Constituent-taste relationship of Kuding tea fermented by Aspergillus neoniger and Aspergillus cristatus: Unveiling taste characteristics through untargeted metabolomics

Kuding tea (KDT), known for its medicinal and edible attributes, currently faces limited application due to its unfavorable taste. Thus, we aimed to improve KDT flavor using fungal fermentation and elucidate the mechanism of flavor change through the constituent-taste relationship. In this study, an electronic tongue was utilized to assess the flavor profiles of unfermented and fermented teas by Aspergillus neoniger (AN) and Aspergillus cristatus (AC). A constituent-taste relationship method combining untargeted metabolomics and taste sensors was employed to analyze the taste-related differential metabolites. The analysis of metabolic pathways further elucidated the potential taste-altering mechanisms. Fermentation of both AN and AC led to changes in the umami and sweetness of KDT. Additionally, AN fermentation impacted bitterness and sourness, while AC fermentation influenced saltiness. Based on the strategy of constituent-taste relationship, 31 and 30 metabolites predominantly including lipids, phenolic acids, flavonoids, amino acids and phenolic glycosides were discovered to be significantly correlated with the flavor characteristics of KDT. During fermentation, AN and AC participated in 5 and 4 metabolic pathways, respectively, showing distinct regulatory mechanisms in altering KDT flavor. AN led to pronounced deglycosylation of glycosides, while AC impacted the degradation of phenolic acids and lipids. Together, this study advances the understanding of metabolic changes in fermented KDT and provides valuable insights into the enhancement of flavor characteristics.

Effects of Strawberry Tree (Arbutus unedo L.) Aqueous Leaf Extract and Arbutin on PK-15 and HepG2 Cells.

The antioxidant properties of the leaves of the Mediterranean strawberry tree (Arbutus unedo L.) are mainly attributed to the main bioactive compound, the phenolic glycoside arbutin. In this study, the safety profile of strawberry tree aqueous leaf extract (STE) and arbutin at the DNA level was assessed in vitro using porcine PK-15 kidney cells and HepG2 cells derived from human hepatomas. To examine the effects on cell viability and DNA damage, cells were treated for 24 h with STE or arbutin at three concentrations presumed to be non-toxic (400, 200, and 11.4 µg/mL). Assessments were performed using the MTS viability assay, dual acridine orange/ethidium bromide fluorescent staining, and alkaline comet assay. Results showed that the highest concentration (400 µg/mL) of both tested compounds had no significant cytotoxic effects on either PK-15 or HepG2 cells. Apoptosis was the predominant type of cell death and the total amount of DNA damage in treated cells was within acceptable limits. These results on the in vitro cytocompatibility of arbutin and STE with PK-15 and HepG2 cells could serve to make more reliable judgements about safe levels of arbutin in cosmetic products and functional foods, given the increased popularity of the compound in recent years.

Isolation, Purification of Phenolic Glycoside 1 from Moringa oleifera Seeds and Formulation of Its Liposome Delivery System.

In this study, N, N '-bis {4- [(α-L- rhamnosyloxy) benzyl]} thiourea (PG-1), a phenolic glycoside compound was purified from Moringa seed. The PG-1 has attracted extensive attention due to its anti-cancer, antioxidant, anti-inflammatory and hypoglycemic properties. However, some of its physicochemical properties such as oral bioavailability has not been studied. Herein, a highly purified PG-1 was extracted and incorporated in multiple layered liposomes (PG-1-L) to avoid its burst release and enhance oral bioavailability. After appropriate characterization, it was discovered that the obtained PG-1-L was stable, homogeneous and well dispersed with the average particle size being 89.26 ± 0.23 nm. Importantly, the in vitro release and in vivo oral bioavailability of PG-1-L were significantly improved compared with PG-1. In addition, MTT results showed that compared with the free PG-1, PG-1-L displayed obvious inhibitory effect on the HepG2 cells, while the inhibitory effect on healthy non-malignant 3T6 and LO-2 cells was not significant, indicating that PG-1-L had high safety. In conclusion, PG-1-L can be used as a promising delivery system and an ideal novel approach to improve the oral bioavailability and anticancer activity of PG-1.

Exploring Vernonia amygdalina’s leaf extracts for phytochemical screening and its anti-bacterial activities

ABSTRACT The aim of this study was to screen the phytochemicals and assess the antibacterial properties of crude extracts from Vernonia amygdalina leaves against specific pathogenic bacteria. Qualitative and qauntitave analysis was performed on both ethanol and ethyl acetate crude extracts using standardized techniques. The analysis revealed the presence of alkaloids, phenol, flavonoids, terpenoids, saponins, tannins, and cardiac glycosides in the ethanol extract, while saponins and glycosides were absent in the ethyl acetate extract. The quantities of phenols, flavonoids, and alkaloids were determined using Gallic acid, quercetin, and atropine assays, respectively. The ethanol extract contained 154.7 ± 3.6 (mg GAE/g) of total phenols, 33.3 ± 1.8 (mg QE/g) of flavonoids, and 2.4 ± 0.08 (mg AE) of alkaloids, whereas the ethyl acetate extract contained 93.7 ± 3.9 (mg GAE/g) of total phenols, 30.7 ± 8.3 (mg QE/g) of flavonoids, and 1.57 ± 0.3 (mg GAE/g) of alkaloids. This study identified 44 components in the ethanol crude extract and 10 components in the ethyl acetate crude extract. The presence of alkanes, alkenes, amines, carboxylic acids, and alcohols was confirmed by FT-IR analysis. Each crude extract was tested at concentrations of 500 mg/mL, 250 mg/mL, 125 mg/mL, and 62.5 mg/mL using the same method. A concentration of 0.001 mg/mL of Penicillin capsule standard drugs and dimethyl sulfoxide were used as positive and negative controls, respectively. Overall, the results of the study indicated that both crude extracts exhibited antibacterial activity at higher concentrations.

Enhanced Curculigoside and Phenolic Compounds Elevate Antioxidant Activity in C. orchioides Gaertn In Vitro Under Exogenous Augmentation with Elicitors Salicylic Acid (SA) and Polyethylene Glycol (PEG) 6000

Abstract Introduction Curculigo orchioides Gaertn, an endangered medicinal plant, possesses a bioactive compound known as curculigoside (phenolic glycoside) in addition to other phenolic compounds. Curculigoside has multifunctional pharmacological properties including antioxidant and anti-inflammatory. Advances in plant tissue culture provide us with tools for the in vitro propagation of medicinal plants in addition to a well-founded system to enhance pharmacologically bioactive compounds through the use of elicitors. Objective The study evaluates the effect of exogenous application of salicylic acid (SA) and polyethylene glycol 6000 (PEG 6000) to in vitro cultures of C. orchioides for enhanced curculigoside, phenolic compounds production followed by an increase in antioxidant activity (AA). Method Eight-week-old subcultured plants grown in one-fourth strength Murashige and Skoog media were subjected to elicitors treatment. SA (10, 100, and 1,000 ppm) and a PEG 6000 (1,000, 5,000, and 10,000 ppm) were used as elicitors for a period of 1, 2, and 4 weeks. Plants without treatment were considered as control. The treated plants were subjected to 80% acetone solvent for efficient phenolic extract preparation. High-performance liquid chromatography was used for the analysis of curculigoside content (CC), and total phenolic content (TPC) was determined using the Folin–Ciocalteu colorimetric method. AA was evaluated by 1,1-diphenyl-2-picrylhydrazyl assay. Results SA treatment increased CC, TPC, and biological activity of AA properties compared to the control, with the maximum value observed at 10 ppm treatment after week 1 elicitation. CC, TPC, and AA gradually decreased after week 2 elicitation, and the lowest values were observed after week 4 elicitation. In the PEG 6000 treatment, 10,000 ppm elicited the highest CC and TPC, with the maximum AA observed after week 2 elicitation. The treatment also elicited higher CC, TPC, and AA in both the 1st and 4th weeks compared to the control. Conclusion SA and PEG 6000 successfully enhanced CC, TPC, and improved AA in C. orchioides in vitro. The study also offers insightful information for the neutraceutical, cosmeceutical, and pharmaceutical industries about how to potentially manipulate medicinal plants in vitro to increase the synthesis of bioactive compounds.

Biosynthetic pathway analysis combined with feature-based molecular networking to comprehensively characterize the chemical constituents in seeds of Sterculia lychnophora.

The seeds of Sterculia lychnophora Hance, commonly known as Pangdahai (PDH) in Chinese, have found extensive use in both culinary and traditional medicinal practices. However, a comprehensive understanding of the chemical composition of PDH has been lacking. This study proposes a strategy that integrates biosynthetic pathway analysis with feature-based molecular networking (FBMN), aiming for a thorough and global characterization of the chemical compositions of PDH. The FBMN map reveals potential compounds with structural similarity, and the MS/MS fragments could be annotated based on library matches, which could predict the plausible biosynthetic pathways in PDH, accomplishing the annotation of compounds clustered in FBMN by integrating biosynthetic pathways. Consequently, 126 compounds were plausibly or unambiguously identified, including 37 phenolic acids and glycosides, 20 flavonoids and glycosides, 12 procyanidins, 21 alkaloids, 22 lipids, and 14 others. Leveraging the information, 40 compounds, including 1 unique isoquinoline alkaloid and 2 rare linear furocoumarins, were isolated and confirmed. This study not only demonstrates a highly effective approach for identifying compounds within complex herbal mixtures but also establishes a robust foundation for the further development of PDH.

A Comparison Analysis of Quality and Metabolic Compounds in Lilies with Different Drying Treatments.

The present study aimed to investigate the variations in the nutritional composition, antioxidant capacity, and metabolite profile of lilies subjected to different drying treatments, including vacuum freeze drying (VFD), hot air drying (HAD), vacuum drying (VD), and infrared drying (ID). The results show that VFD provided better preservation of the original coloration and displayed the highest levels of total amino acid content, total phenolic content, total flavonoid content, and polysaccharide and alkaloid content. Our results reveal that VFD treatment can be employed to obtain high-quality lilies with desirable appearance characteristics and nutrient compositions. Metabolomics analysis identified a total of 464 metabolites from various dried lilies. Differential metabolite screening found 150 differential metabolites across all pairwise comparisons. Hierarchical clustering analysis (HCA) indicated that lilies subjected to VFD treatment exhibited a higher abundance of steroids, saponin, flavonoids, and phenolic glycoside, whereas those subjected to HAD, VD, or ID treatments showed relatively elevated levels of specific amino acids or derivatives. This study elucidates the significant impact of various drying treatments on the quality and metabolic profile of lilies, thereby providing valuable insights for enhancing the nutritional quality of processed lilies.

Anti-inflammatory phenolic glycosides from endemic Marrubium rotundifolium Boiss.

Marrubium rotundifolium Boiss. is an endemic plant distributed in Aegean Region of Türkiye. It’s traditionally used in Anatolian medicine for treatment of cold and flu, dyspepsia, costiveness and intestinal spasms. However, phytochemical studies on the plant are limited. In the present study, five phenolic glycosides 4’,5,6,7-tetramethoxy scutellarein (1), apigenin-7-O-(3”-O-E-p-coumaroyl)-β-d-glucopyranoside (2), tiliroside (3), 4-(β-d-glucopyranosyloxy) benzoic acid (4), and astragalin (5) were isolated from the aerial parts of M. rotundifolium and their structures were elucidated on the basis of spectroscopic methods (1D and 2D NMR, and MALDI-TOF/MS). Moreover, anti-­inflammatory activities of the isolated compounds were evaluated by measurements of interleukins (IL-1β, IL-6) and tumour necrosis factor-alpha (TNF-α) levels. Tiliroside exhibited the highest potency in all pathways. At concentrations of 3 and 6 µg/mL, it significantly decreased the levels of pro-inflammatory cytokines IL-1β (192.53 and 175.54 pg/mL), IL-6 (925.52 and 946.81 pg/mL), and TNF- α (6465.86 and 6267.67 pg/mL). This is the first report on phenolic profile of endemic M. rotundifolium. The anti-inflammatory and antidiabetic activity potential of the plant should be investigated in further studies.

Untargeted metabolomic profiling of Prinsepia utilis Royle leaves by Ultra-Performance Liquid Chromatography-Quadrupole-Time of Flight-Mass Spectrometry.

Prinsepia utilis Royle, native to the Himalayas, is esteemed in Chinese and Indian folk medicine for its diverse medicinal benefits, targeting arthritis, pain relief, bone disorders, and joint discomfort. This study examined the 25% aqueous methanol extract of P.utilis leaves using UPLC-Q-TOF-MS/MS, identifying 78 metabolites, 76 of which were reported for the first time in P.utilis. These included 64 phenolics represented by 56 flavonoids, 5 phenolic acids, 3 phenolic glycosides, 4 terpenoids, 2 lignan glycosides, and 8 other compounds, expanding the knowledge of its chemical composition. These findings lay a foundation for further research, providing insights into potential bioactive compounds and opening avenues for applications in natural product drug discovery, traditional medicine, and nutraceutical development, leveraging the plant's established traditional uses.

The lipase inhibitory effect of mulberry leaf phenolic glycosides: The structure-activity relationship and mechanism of action

The present study found for the first time that phenolic glycosides were an important material basis for mulberry leaves to inhibit lipase. The corresponding IC50 for hyperoside, rutin, astragalin and quercetin were 68, 252, 385 and 815 μg/mL respectively. The inhibitory effect was ranked as monoglycosides > phenolic hydroxyl groups > disaccharides on the benzone ring. Hyperoside bound to lipase in competitive inhibition type with one binding site, while the others bound to lipase in a mixed inhibition type by two similar sites. All four compounds altered the microenvironment and secondary conformation of lipase through static quenching. The docking score, stability, and binding energy were consistent with the compound inhibitory activity. The main binding between compounds and lipase amino acid residues were spontaneously though hydrophobic interactions and hydrogen bonding. The strong hydrogen bonds formed with SER-152 inside the lipase pocket, might be important for the strong inhibitory activity of hyperoside.

Gastrodin Ameliorates Learning and Memory Impairments Caused by Long-Term Noise Exposure.

The developing brain is significantly affected by long-term exposure to noise at an early age, leading to functional disorders such as learning and memory impairments. Gastrodin (GAS), a natural organic compound, is an extraction of phenolic glycoside from the rhizome of Gastrodia elata. Clinically, GAS is extensively utilised for the treatment of neurological disorders. This study aimed to explore the effect and mechanism of GAS on noise exposure-induced learning and memory impairments. Rats aged 21 days were exposed to a 90 dB noise environment for 4 weeks and divided into the noise group, the noise + GAS group, and the control group to establish a noise exposure model. After noise exposure treatment, the improvement effect of GAS on the memory of rats was evaluated by Y-maze and Morris water maze. Enzyme-linked immunosorbent assay was utilised to determine the effect of GAS on neurotransmitter levels in the hippocampal tissue of noise-exposed rats. Western blot was applied for the detection of the protein levels of neurotrophic factors. The GAS treatment significantly improved spatial memory and increased the levels of key neurotransmitters (norepinephrine, dopamine and serotonin) and neurotrophic factors (neurotrophin-3 and brain-derived neurotrophic factor) in the hippocampal tissues of noise-exposed rats. These alterations correlate with enhanced cognitive functions, suggesting a neuroprotective effect of GAS against noise-induced cognitive impairments. This study supports the potential of GAS to treat noise-induced learning and memory impairments by modulating neurotransmitter secretion and enhancing the expression levels of neurotrophic factors. These findings offer potential therapeutic avenues for cognitive impairments induced by noise exposure.