The diversity of endophytic fungi in Tartary buckwheat (Fagopyrum tataricum) and its correlation with flavonoids and phenotypic traits.

Tartary buckwheat (Fagopyrum tataricum) is a significant medicinal crop, with flavonoids serving as a crucial measure of its quality. Presently, the artificial cultivation of Tartary buckwheat yields low results, and the quality varies across different origins. Therefore, it is imperative to identify an effective method to enhance the yield and quality of buckwheat. Endophytic fungi reside within plants and form a mutually beneficial symbiotic relationship, aiding plants in nutrient absorption, promoting host growth, and improving secondary metabolites akin to the host. In this study, high-throughput sequencing technology was employed to assess the diversity of endophytic fungi in Tartary buckwheat. Subsequently, a correlation analysis was performed between fungi and metabolites, revealing potential increases in flavonoid content due to endophytic fungi such as Bipolaris, Hymenula, and Colletotrichum. Additionally, a correlation analysis between fungi and phenotypic traits unveiled the potential influence of endophytic fungi such as Bipolaris, Buckleyzyma, and Trichosporon on the phenotypic traits of Tartary buckwheat. Notably, the endophytic fungi of the Bipolaris genus exhibited the potential to elevate the content of Tartary buckwheat metabolites and enhance crop growth. Consequently, this study successfully identified the resources of endophytic fungi in Tartary buckwheat, explored potential functional endophytic fungi, and laid a scientific foundation for future implementation of biological fertilizers in improving the quality and growth of Tartary buckwheat.

In vitro combination effects of plant-derived quercetin with synthetic bicalutamide on prostate cancer and normal cell lines: in silico comparison.

Prostate cancer is the second most frequent and the fifth greatest cause of death in men. Although diet has been connected to the prevalence of cancer in addition to other factors, the relation between cancer and prevention is weak. Treatment options are at risk due to cell resistance. To identify new combinations, we tried plant-derived quercetin with bicalutamide on cell lines. To determine the cytotoxicity and apoptotic potential of plant-derived quercetin and its combination, MTT [3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyl tetrazolium bromide] and dual stain assays were performed. In silico protein-ligand interaction was performed to support the in vitro findings. A thin layer, column, and high-performance chromatography were used to purify quercetin along with an authentic sample. In the cytotoxic study, quercetin was minimized by 80% similar to bicalutamide and a combination of quercetin and bicalutamide by 50% when compared to controls by 2%. Quercetin and bicalutamide showed a similar binding affinity for androgen receptors (9.7 and 9.8), hub genes (10.8 and 10.0), and a few other PCa-related genes (9.4 and 9.1). We propose to conclude that the combination of quercetin plus bicalutamide can be used for chemotherapy if additional in vivo studies are conducted. The intake of foods high in polyphenolic compounds can help to prevent prostate cancer. Examination of quercetin on several cell lines will provide a definite conclusion to combat cancers.

Propolis-loaded liposomes: characterization and evaluation of the in vitro bioaccessibility of phenolic compounds.

Background and purpose: Propolis has low water solubility, poor stability, and limited bioaccessibility of phenolic constituents when subjected to in vitro digestion. To overcome these drawbacks, the liposomal encapsulation method can be employed. Experimental approach: Soybean phosphatidylcholine lecithin mixed with Tween 80 (T80) and ammonium phosphatides (AMP) was used to produce propolis extract (PE)-loaded liposomes. The mean particle size, zeta potential, encapsulation efficiency values, and transmission electron microscopy analysis were used to characterize liposomes. Individual phenolics were determined for digested and nondigested propolis-loaded liposomes and propolis extract. Key results: Tween 80 incorporation reduced the size of unloaded liposomes, whereas AMP inclusion yielded larger liposomes. In both formulations, PE loading significantly increased the size and reduced the zeta potential values and homogeneity of the size distribution. In free PE, the most bioaccessible polyphenols were phenolic acids (3.20 to 5.63 %), and flavonoids such as caffeic acid phenethyl ester, galangin, pinobanksin, and pinocembrin (0.03 to 2.12 %) were the least bioaccessible. Both liposomal propolis provided significantly higher bioaccessibility of phenolic compounds. The liposomes with T80 and AMP in their compositions recovered 52.43 and 185.90 % of the total amount of phenolic compounds in the nondigested samples, respectively. The liposomes containing AMP not only exhibited high solubility for PE but also provided protection to the phenolic compounds during in vitro digestion. Conclusion: Liposomal encapsulation could be a promising approach to improving the solubility and stability of PE in digestive fluids, making it suitable for the delivery of propolis in oral formulations.

In Vitro Evaluation of Extracts From Ixora Species for a Potential Phytosomal Formulation.

Background Ixora species are perennial shrubs and flowering plants belonging to the family Rubiaceae. The leaf and flower parts of Ixora coccinea (I. coccinea) andIxora alba (I. alba) were aimed at isolating their active fractions. The present study was to determine in vitro antitumor activity against malignant melanoma cell lines for phytosome formulation. Materials and methods Two species, I. coccinea (red flowers and leaves) and I. alba (white flowers and leaves), were selected, and this study focused on determining the active fraction by comparing the in vitro antimicrobial and antioxidant potentials of petroleum ether, chloroform, ethyl acetate, and hydroalcoholic (ethanol:water, 70:30 v/v) extracts. The identified potent extract was subjected to in vitro anticancer activity in malignant melanoma cell lines. Results A phytochemical study revealed phytosterols, flavonoids, proteins, amino acids, alkaloids, carbohydrates, phenols, tannins, and diterpenes. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay was used to evaluate the antioxidant effect of I. coccinea and I. alba leaf and flower extracts. In the DPPH assay, I. coccinea flower hydroalcoholic extract (ICFHA) had an IC50 value of 248.99 µg/mL, and I. coccinea leaf hydroalcoholic extract (ICLHA) had an IC50 value of 268.87 µg/mL. These two extracts had a lower value with a higher antioxidant effect. In the total antioxidant assay, I. coccinea leaf ethyl acetate extract (ICLEA) and I. coccinea leaf chloroform extract (ICLCE) have 77.4 ± 0.05 and 68.9 ± 0.03 mg of ascorbic acid equivalent per gm of extract, respectively. These two extracts exhibited a high antioxidant effect. The antimicrobial potential was evaluated using selected bacterial and fungal strains using the agar-well diffusion method. Petroleum ether and chloroform extracts of I. coccinea and I. alba leaves and flowers did not possess antimicrobial activity with any of the bacterial or fungal strains. An ethyl acetate extract and a hydroalcoholic extract of I. coccinea leaves and flowers showed antimicrobial activity against Enterococcus faecalis, Candida albicans, and Staphylococcus aureus. An ethyl acetate extract of I. coccinea flower and a hydroalcoholic extract of I. alba leaf showed a significant zone of inhibition when compared with standard chloramphenicol for all three selected strains, which may be due to the presence of active phytoconstituents. ICLHA showed a MIC of ≤300 µg/mL for Enterococcus faecalis and Staphylococcus aureus and ≤400 µg/mL for Candida albicans microbial strains. The high total flavonoid content was reported in ICLEA at 771.31 µg/mL and in I. coccinea flower ethyl acetate extract (ICFEA) at 694.69 µg/mL. High-performance thin layer chromatography (HPTLC) analysis showed a high quercetin (QCE) content in the ICLEA extract. To prove the in vitro skin anticancer activity, an MTT assay was performed for the ICLEA extract in a malignant melanoma cell line, and the IC50 value was reported as 7.96 µg/mL. Conclusion I. coccinea leaf ethyl acetate extract revealed a significant total flavonoid content in analysis through the aluminum chloride method, and the presence of a high QCE content was confirmed by HPTLC analysis. The in vitro skin anticancer activity of ICLEA was confirmed by the MTT assay; therefore, it was concluded that the ICLEA extract was a potent fraction and was selected to develop a phytosome.

Flavonoids and Alzheimer's disease: reviewing the evidence for neuroprotective potential.

Neurodegeneration, which manifests as several chronic and incurable diseases, is an age-related condition that affects the central nervous system (CNS) and poses a significant threat to the public's health for the elderly. Recent decades have experienced an alarming increase in the incidence of neurodegenerative disorders (NDDs), a severe public health issue due to the ongoing development of people living in modern civilizations. Alzheimer's disease (AD) is a leading trigger of age-related dementia. Currently, there are no efficient therapeutics to delay, stop, or reverse the disease's course development. Several studies found that dietary bioactive phytochemicals, primarily flavonoids, influence the pathophysiological processes underlying AD. Flavonoids work well as a supplement to manufactured therapies for NDDs. Flavonoids are effective in complementing synthetic approaches to treat NDDs. They are biologically active phytochemicals with promising pharmacological activities, for instance, antiviral, anti-allergic, antiplatelet, anti-inflammatory, antitumor, anti-apoptotic, and antioxidant effects. The production of nitric oxide (NO), tumor necrosis factor (TNF-α), and oxidative stress (OS) are downregulated by flavonoids, which slow the course of AD. Hence, this research turned from preclinical evidence to feasible clinical applications to develop newer therapeutics, focusing on the therapeutic potential of flavonoids against AD.

Utilising UPLC-QTOF-MS/MS to determine the phytochemical profile and in vitro cytotoxic potential of Ziziphora capitata L. with molecular docking simulation.

Ziziphora capitata (Lamiaceae family) aerial parts extract contains 57 metabolites, including flavonoids, phenolic acids, anthocyanins, and coumarins, as assessed by UPLC-QTOF-MS/MS. Successive extracts (hexane, chloroform, ethyl acetate, ethanol 95%, and water) were tested in vitro cytotoxic activity against HepG-2, MCF-7, HCT-116, A549, and PC3 cell lines. The results revealed that hexane extract exhibited the most potent cytotoxic activity among PC3 and A549 cell lines, IC50 = 47.1 ± 1.75 and 49.2 ± 1.08 µg/mL compared to Vinblastine IC50 = 42.47 ± 1.95 and 24.64 ± 1.18 µg/mL, respectively, and had a moderate impact on the remaining cell lines. Moreover, the chloroform and ethyl acetate extracts exhibited moderate affinity among all tested cell lines. Furthermore, the total phenolic and flavonoid contents were assessed. The molecular docking simulation was performed inside the effective sites of VEGFR-2 and TS as anticancer targets for the top ten phytochemicals. The results showed higher binding energy values for VEGFR-2 than for TS compared to vinblastine and co-crystallized ligands.

Chemical composition and biological activities of the Algerian Cymbalaria muralis aerial parts.

In the present study we report data about antioxidant (DPPH, ß-Carotene, reducing power), anti-inflammatory (xylene-induced ear oedema in mice (76 ± 1.0%) and membrane stabilisation (100%)) and antimicrobial (Escherichia coli ATCC25922, Staphylococcus aureus ATCC25923, Pseudomonas arugenosa ATCC27853 and Fusarium oxysporum ATCC62506) activities of the ethanolic extract from the Algerian Cymbalaria muralis P. Gaertn., B. Mey. & Scherb (CME). The LC-ESIMS analysis of CME chemical profile allowed to identify antirrhinoside (1), catalpol (2), linarioside (3), glucosyringic acid (4), angoroside C (5), apigenin 7-O-glucoside (6), acacetin 7-O-ß-D-glucopyranoside (7), apigenin (8), chrysoeriol 7-rutinoside (9), diosmin (10) and linarin (11). The evaluated total phenolic and flavonoid contents support the biological activities.

The effects of citrus flavonoids supplementation on endothelial function: A systematic review and dose-response meta-analysis of randomized clinical trials.

The present systematic review and dose-response meta-analysis was conducted to synthesize existing data from randomized clinical trials (RCTs) concerning the impact of citrus flavonoids supplementation (CFS) on endothelial function. Relevant RCTs were identified through comprehensive searches of the PubMed, ISI Web of Science, and Scopus databases up to May 30, 2023. Weighted mean differences and their corresponding 95% confidence intervals (CI) were pooled utilizing a random-effects model. A total of eight eligible RCTs, comprising 596 participants, were included in the analysis. The pooled data demonstrated a statistically significant augmentation in flow-mediated vasodilation (FMD) (2.75%; 95% CI: 1.29, 4.20; I2 = 87.3%; p < 0.001) associated with CFS compared to the placebo group. Furthermore, the linear dose-response analysis indicated that each increment of 200 mg/d in CFS led to an increase of 1.09% in FMD (95% CI: 0.70, 1.48; I2 = 94.5%; p < 0.001). The findings from the nonlinear dose-response analysis also revealed a linear relationship between CFS and FMD (Pnon-linearity = 0.903, Pdose-response <0.001). Our findings suggest that CFS enhances endothelial function. However, more extensive RTCs encompassing longer intervention durations and different populations are warranted to establish more precise conclusions.

Amino acids and flavonoids analysis reveals quality constituents difference among different albino tea resources.

Albino tea has attracted increased attention due to its unique flavor. To reveal the difference in key metabolites constituting the important quality of different tea resources, amino acids and flavonoids profiles in three albino resources with different degrees of albinism and one normal green variety were comprehensively investigated. K-means analysis revealed 35 amino acids were significantly enriched in 'Jibai', while 3 and 2 were specifically accumulated in 'Huangjinya' and 'Anjibaicha', respectively. Based on OPLS-DA models, 40, 31 and 45 significantly differential flavonoids were determined in 'Huangjinya', 'Anjibaicha' and 'Jibai' compared to 'Fudingdabaicha', and most were down-regulated. Among them, 10, 5 and 13 differential flavonoids were exclusively found in 'Huangjinya', 'Anjibaicha' and 'Jibai', respectively, which may contribute to unique quality for different resources. The differential flavonoids and amino acids involved in their metabolic pathways were obviously different among four resources, resulting in the difference in tea quality and flavor.

Ocimum kilimandscharicum 4CL11 negatively regulates adventitious root development via accumulation of flavonoid glycosides.

4-Coumarate-CoA Ligase (4CL) is an important enzyme in the phenylpropanoid biosynthesis pathway. Multiple 4CLs are identified in Ocimum species; however, their in planta functions remain enigmatic. In this study, we independently overexpressed three Ok4CL isoforms from Ocimum kilimandscharicum (Ok4CL7, -11, and -15) in Nicotiana benthamiana. Interestingly, Ok4CL11 overexpression (OE) caused a rootless or reduced root growth phenotype, whereas overexpression of Ok4CL15 produced normal adventitious root (AR) growth. Ok4CL11 overexpression in N. benthamiana resulted in upregulation of genes involved in flavonoid biosynthesis and associated glycosyltransferases accompanied by accumulation of specific flavonoid-glycosides (kaempferol-3-rhamnoside, kaempferol-3,7-O-bis-alpha-l-rhamnoside [K3,7R], and quercetin-3-O-rutinoside) that possibly reduced auxin levels in plants, and such effects were not seen for Ok4CL7 and -15. Docking analysis suggested that auxin transporters (PINs/LAXs) have higher binding affinity to these specific flavonoid-glycosides, and thus could disrupt auxin transport/signaling, which cumulatively resulted in a rootless phenotype. Reduced auxin levels, increased K3,7R in the middle and basal stem sections, and grafting experiments (intra and inter-species) indicated a disruption of auxin transport by K3,7R and its negative effect on AR development. Supplementation of flavonoids and the specific glycosides accumulated by Ok4CL11-OE to the wild-type N. benthamiana explants delayed the AR emergence and also inhibited AR growth. While overexpression of all three Ok4CLs increased lignin accumulation, flavonoids, and their specific glycosides were accumulated only in Ok4CL11-OE lines. In summary, our study reveals unique indirect function of Ok4CL11 to increase specific flavonoids and their glycosides, which are negative regulators of root growth, likely involved in inhibition of auxin transport and signaling.

Effect of quinoa (Chenopodium quinoa W.) flour supplementation in breads on the lipid profile and glycemic index: an in vivo study.

Quinoa is a gluten-free pseudocereal, with an excellent nutrient profile containing considerable amounts of fiber and minerals and rich in antioxidants such as polyphenols. The purpose of this research was to investigate the effects of quinoa bread on physical, chemical, bioactive components, glycaemic index (GI), and biochemical parameters. Human subjects aged between 20 and 50 years with the absence of morbid factors were fed daily with quinoa bread for 3 months in order to study its pre-and post-treatment effects on blood glucose, glycosylated haemoglobin, and lipid profile. The effort was made to incorporate the maximum amount of quinoa into the bread without compromising the acceptability of the bread. Of the 14 formulations, TQ13, containing 20% quinoa flour with 3% wheat bran, was selected for further analysis. The GI study revealed that quinoa bread peaked at 45 min with a gradual increase after ingestion of the bread and a steady decline thereafter. The observed value for blood glucose levels, before and after supplementation with quinoa-incorporated bread, was 86.96 ± 15.32 mg/dL and 84.25 ± 18.26 mg/dL, respectively. There was a statistically significant (p ≤ 0.05) decrease in levels of triglycerides, total cholesterol, low-density lipoprotein (LDL), and very-LDL (VLDL) level before and after supplementation. However, non-significant changes were observed for high-density lipoprotein levels from the pre- and post-treatment with the quinoa-incorporated bread. Quinoa-incorporated bread possessed low GI (42.00 ± 0.83) compared to control (69.20 ± 1.84) and long-term consumption proved to contain functional efficacies in terms of hypolipidemic effect.

Simultaneous assessment of absorption and pharmacokinetic characteristics of four active flavonoids from Chimonanthus nitens Leaf Granules using LC-MS determination: in vivo and in vitro.

A sensitive UPLC-HRMS method was developed and validated for simultaneous quantification of four active flavonoids from Chimonanthus nitens Leaf Granules (CNLG) in biological matrix. The method was utilized in pharmacokinetic study of the four flavonoids in rats as well as other evaluation assays in vitro. It was revealed that rutin, nicotiflorin, and astragalin had poor oral bioavailability in rats possibly due to low intestinal permeability and metabolism in intestinal flora. Kaempferol underwent rapid glucuronidation and sulphation in rat plasma with medium permeability coefficient. The results provided valuable data for future research and development of CNLG flavonoids.

Assessment of the botanical origin of Saudi Arabian honey samples to identify pollen with chromatographic tools and packing and storage.

The increasing demand for honey purification and authentication necessitates the global utilization of advanced processing tools. Common honey processing techniques, such as chromatography, are commonly used to assess the quality and quantity of valuable honey. In this study, 15 honey samples were authenticated using HPLC and GC-MS chromatographic methods to analyze their pollen spectrum. Various monofloral honey samples were collected, including Acacia, Hypoestes, Lavandula, Tamarix, Trifolium, and Ziziphus species, based on accurate identification by apiarists in 2023 from the Kingdom of Saudi Arabia. Honey analysis revealed the extraction of pollen from 20 different honeybee floral species. Pollen identified from honey samples using advanced chromatographic tools revealed dominant vegetation resources: Ziziphus species (23%), Acacia species (25%), Tamarix species (34%), Lavandula species (26%), Hypoestes species (34%), and Trifolium species (31%). This study uses HPLC to extract phenolic compounds, revealing dominant protocatechuic acid (4.71 mg g-1), and GC-MS to analyze organic compounds in honey pollen. Specifically, 2-dodecanone was detected with a retention time of 7.34 min. The utilization of chromatographic tools in assessing honey samples for pollen identification provides a reliable and efficient method for determining their botanical origins, thereby contributing to the quality control and authentication of honey products.

Luteolin Is More Potent than Cromolyn in Their Ability to Inhibit Mediator Release from Cultured Human Mast Cells.

INTRODUCTION: Mast cells are known for their involvement in allergic reactions but also in inflammatory reactions via secretion of numerous pro-inflammatory chemokines, cytokines, and enzymes. Drug development has focused on antiproliferative therapy for systemic mastocytosis and not on inhibitors of mast cell activation. The only drug available as a "mast cell blocker" is disodium cromoglycate (cromolyn), but it is poorly absorbed after oral administration, is a weak inhibitor of histamine release from human mast cells, and it develops rapid anaphylaxis. Instead, certain natural flavonoids, especially luteolin, can inhibit mast cell activation. METHODS: Here, we compared pretreatment (0-120 min) with equimolar concentration (effective dose for 50% inhibition = 100 mm for inhibition of histamine release by cromolyn) of cromolyn and luteolin on release of mediators from the cultured human LADR mast cell line stimulated either by immunoglobulin E (IgE) and anti-IgE or with IL-33. RESULTS: We show that luteolin is significantly more potent than cromolyn inhibiting release of histamine, tryptase, metalloproteinase-9, and vascular endothelial growth factor. Moreover, while luteolin also significantly inhibited release of IL-1ß, IL-6, and IL-8 (CXCL8) and TNF, cromolyn had no effect. CONCLUSION: These findings support the use of luteolin, especially in liposomal form to increase oral absorption, may be a useful alternative to cromolyn.

Discovery of components in honeysuckle for treating COVID-19 and diabetes based on molecular docking, network analysis and experimental validation.

Molecular docking screening identified ochnaflavone, madreselvin B and hydnocarpin as key components for treating COVID-19 with diabetes in honeysuckle using 3 C-like protease (Mpro), angiotensin-converting enzyme 2 (ACE2), and dipeptidyl peptidase 4 (DPP4) as molecular docking targets, ACE2, DPP4, IL2, NFKB1, PLG, TBK1, TLR4 and TNF were the core targets, and multiple antiviral and anti-inflammatory signalling pathways were involved. Further, the levels of IL-1ß and DPP4 in cell supernatant that had been activated by LPS was decreased by hypnocarpin, and ACE2 protein and DPP4 mRNA in cells were down-regulated. Overall, we have identified three components from honeysuckle that have potency to treat COVID-19 combined with diabetes. SARS-CoV-2 transcription may be inhibited by these components in honeysuckle, reducing virus invasion, inhibiting inflammatory factors, and improving immune response. Our findings could provide a basis for the clinical application and further development of honeysuckle.

Exploring the Therapeutic Potential of Flavonoids in the Management of Cancer.

Flavonoids are a class of polyphenolic compounds that can be classified into six distinct categories, namely isoflavonoids, flavanones, flavanols, flavonols, flavones, and anthocyanidins. These compounds are naturally occurring and can be found in a diverse range of plant species. Flavonoids, a class of bioactive compounds, are mostly obtained through the consumption of vegetables, fruits and plant-derived beverages such as wine, cocoa-based products and green tea. Flavonoids have been demonstrated to exhibit a diverse range of anticancer properties. These include the modulation of activities of enzymes involved in scavenging reactive oxygen species, involvement in cell cycle arrest, induction of apoptosis and autophagy, as well as suppression of cancer cell proliferation and invasiveness. Flavonoids exhibit a dual role in maintaining reactive oxygen species balance. They function as antioxidants in regular physiological conditions, while also demonstrating significant pro-oxidant properties in cancer cells. This prooxidant activity induces apoptotic pathways and downregulates pro-inflammatory signalling pathways. The paper explores the biochemical characteristics, bioavailability, anticancer efficacy, and modes of action of flavonoids.

Effect of total flavonoids of Dracocephalum moldavica L. On neuroinflammation in Alzheimer's disease model amyloid-ß (Aß1-42)-peptide-induced astrocyte activation.

One of the main pathological features noted in Alzheimer's disease (AD) is the presence of plagues of aggregated ß-amyloid (Aß1-42)-peptides. Excess deposition of amyloid-ß oligomers (AßO) are known to promote neuroinflammation. Sequentially, following neuroinflammation astrocytes become activated with cellular characteristics to initiate activated astrocytes. The purpose of this study was to determine whether total flavonoids derived from Dracocephalum moldavica L. (TFDM) inhibited Aß1-42-induced damage attributed to activated C8-D1A astrocytes. Western blotting and ELISA were used to determine the expression of glial fibrillary acidic protein (GFAP), and complement C3 to establish the activation status of astrocytes following induction from exposure to Aß1-42. Data demonstrated that stimulation of C8-D1A astrocytes by treatment with 40 µM Aß1-42 for 24 hr produced significant elevation in protein expression and protein levels of acidic protein (GFAP) and complement C3 accompanied by increased expression and levels of inflammatory cytokines. Treatment with TFDM or the clinically employed drug donepezil in AD therapy reduced production of inflammatory cytokines, and toxicity initiated following activation of C8-D1A astrocytes following exposure to Aß1-42. Therefore, TFDM similar to donepezil inhibited inflammatory secretion in reactive astrocytes, suggesting that TFDM may be considered as a potential compound to be utilized in AD therapy.

Mechanistic studies on protective effects of total flavonoids from Ilex latifolia Thunb. on UVB-radiated human keratinocyte cell line (HaCaT cells) based on network pharmacology and molecular docking technique.

The aim of the present research is to investigate anti-UVB radiation activity of total flavonoids from Ilex latifolia Thunb. (namely large-leaved Kuding tea) on human keratinocyte cell line (HaCaT cells) based on network pharmacology and molecular docking technique. Network pharmacology was used to screen target genes of active ingredients from Ilex latifolia Thunb. associated with UVB irradiation. The possible signaling pathways were analyzed by KEGG enrichment and verified by cellular experiments. Molecular docking was used to assess the affinity between the active ingredients and the core targets. The prediction of network pharmacology and molecular docking was identified by series experiment in UVB-irradiated HaCaT cells. Network pharmacology results showed that the active ingredients of Ilex latifolia Thunb. for anti-UVB irradiation were mainly flavonoids, and the possible signaling pathways were involved in PI3K-AKT, apoptosis, MAPKs, NF-κB, and JAK-STAT3. Molecular docking indicated key binding activity between AKT1-Glycitein, STAT3-Formononetin, CASP3-Formononetin, TNF-Kaempferol, CASP3-Luteolin, and AKT1-Quercetin. The total flavonoid pretreatment (0.25-1.0 mg/mL) down-regulated the expression of IL-6, IL-1ß, and TNF-α in the cells determined by ELISA. The expression of phosphor PI3K, phosphor AKT, phosphor JAK, phosphor STAT3, phosphor JNK, and phosphor p38 MAPKs and COX-2 proteins in cytosolic and NF-κB p65 protein in nucleus were down-regulated and determined by western blot. It also protected UVB-irradiated cells from apoptosis by reducing apoptosis rate and down-regulating active-caspase 3. In a word, the total flavonoid treatment protected HaCaT cells from UVB injuries effectively, and the potential mechanism involves PI3K-AKT, JAK-STAT3, MAPK, and NF-κB pathway by anti-inflammatory and apoptosis action in cells. The mechanism in vivo experiment needs to be further confirmed in future.

Phytochemical potential and GC-MS analysis of propolis from Punjab region of India.

Propolis is a beehive product produced from honeybees by mixing ß-glycosidase enzyme and beeswax with exudate collected from plant resins. The main goal of this study was to investigate the phytochemical potential and GC-MS profiling of the main constituents of propolis. The antioxidant activity was assessed by using 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay, total phenolic content and total flavonoid content were analysed by Folin-Ciocalteu reagent method and aluminium chloride method respectively. Methanolic extract exhibited highest antioxidant activities, ethanolic extract had the highest total phenolic content, and maximum amount of flavonoid was observed in the chloroform extract. GC-MS analysis revealed the presence of flavonoids, fatty acids and phenolic compounds. Results revealed that propolis from Derra Bassi can be used as natural antioxidant, also extracting solvents had a significant impact on the phytochemical activities and with its standardisation can be used for prevention of diseases related with free radicals.

A new benzoquinone and a new stilbenoid from Paphiopedilum exul (Ridl.) Rolfe.

One new alkyl benzoquinone, paphionone (1), one new trans-stilbenoid, (E)-6,5'-dihydroxy-2,3'-dimethoxystilbene (2), and eight known stilbenoids and flavonoids (3-10) were isolated from the leaves and roots of Paphiopedilum exul (Orchidaceae). Their chemical structures were determined based on IR, ECD, MS and NMR analyses. Cytotoxicity of all isolated compounds towards human hepatocellular carcinoma (HepG2) cell line was examined in vitro by MTT assay. The para-hydroxybenzyl substituted stilbene 10 was potently cytotoxic to the cancer cells, with an IC50 value of 4.80 ± 1.10 µM (selectivity index = 20.83). All compounds were non-toxic to normal human embryo fibroblast (OUMS-36) cell line.