Bioactive Constituents Research Articles

Exploring the Potential Hepatoprotective Properties of Cactus (Cactaceae) in Liver Health and Disease Management: A Brief Review

Cacti are renowned for their resilience in arid environments and have been utilized as a valuable food source in various cultures for centuries. The potential effects of cactus (Cactaceae) consumption on liver health have garnered significant scientific interest in recent years. This review aimed to consolidate and analyze existing research findings regarding the relationship between cactus-derived compounds and their influence on liver function and health. Various cactus species, particularly Opuntia spp., are rich reservoirs of antioxidants, polyphenols, flavonoids, and betalains. In vitro and in vivo studies with animal models have shown that bioactive constituents of cactus exhibit anti-inflammatory, antioxidative, and antifibrotic properties, which potentially mitigate liver damage induced by oxidative stress, inflammation, and hepatotoxic agents. Understanding their mechanisms of action and conducting rigorous clinical studies with administration of cactus will ascertain their role in preventing and treating liver ailments, offering novel avenues in nutrition, hepatology, and natural medicine.

The safety and tolerability of Annona muricata leaf product in people living with cancer: Study protocol

ObjectivesThe objective of this study was to design a clinical study protocol to investigate the safety and tolerability of Annona muricata, in people living with advanced malignancy. Anecdotal clinical evidence suggests this herb has potential anti-cancer activity. There are numerous pre-clinical studies detailing Annona muricata’s main bioactive constituents. To date, clinical studies evaluating the efficacy, safety and tolerability are limited. DesignThis phase 1 open label study will involve people living with stage III and IV cancers of any type, who are not undergoing chemotherapeutic treatment. MethodsThe primary outcome is safety and tolerability of an Annona muricata leaf product as measured by participants’ self-reporting of adverse effects experienced and the proportion of participants completing the study. Secondary outcomes include biomarkers of inflammation and immune function, disease status and self-reported quality of life scores. Participants (n = 24) will be allocated to one of two groups for 12 weeks. Participants will commence at different timepoints and be assigned to either 530 mg or 1060 mg of Annona muricata daily. The study has been approved by the Human Research Ethics Committee Bellberry and will be reported in compliance with the SPIRIT statement. This study has been registered with the Australian New Zealand Clinical Trials Register. Results and conclusionsThe results of this study will provide safety and tolerability data for clinicians involved in the care of people living with cancer who choose to use Annona muricata products as an integrative approach to their healthcare. The results of this study will inform further research about the potential role of Annona muricata in cancer.

Comparative Bioactive Constituents, Radical Scavenging and Antidiabetic Properties of Fresh, Boiled and Air-Dried Momordica charantia Leaves

Comparative Bioactive Constituents, Radical Scavenging and Antidiabetic Properties of Fresh, Boiled and Air-Dried Momordica charantia Leaves

Spectral analysis and bioactive profiling of hot methanolic extracts from Phoenix dactylifera seeds: Antibacterial efficacy and in vitro cytotoxicity insights

Phoenix dactylifera, commonly called date palm, has great importance as a fruiting plant. The hot methanolic extract of date seeds (HMEDSE), was further fractionated into three fractions (F1, F2, and F3) through column chromatography. The three fractions were composed of various bioactive constituents which was analysed through GC-MS and FT-IR analysis. The results revealed remarkable antibacterial properties of crude HMEDSE against various pathogenic microorganisms affecting humans. The spectrum of activity of HMEDSE against various human pathogenic bacteria showed the following sequence based on its efficacy, Escherichia coli (17.6 ± 2.5 mm), Klebsiella pneumoniae (16.3 ± 2.5 mm), Staphylococcus aureus (16.3 ± 1.5 mm), Streptococcus pyogenes (15 ± 2.6 mm), Pseudomonas aeruginosa (15 ± 2 mm), and lastly, Bacillus subtilis (14.3 ± 2 mm). Furthermore, HMEDSE exhibited cytotoxicity, with an IC50 of 73.5 ± 0.5 µg/mL against MCF-7 ATCC breast cancer cells, leading to gradual apoptosis.

The Effect of Sargassum fusiforme and Fucus vesiculosus on Continuous Glucose Levels in Overweight Patients with Type 2 Diabetes Mellitus: A Feasibility Randomized, Double-Blind, Placebo-Controlled Trial.

Brown seaweed is promising for the treatment of type 2 diabetes mellitus (T2DM). Its bioactive constituents can positively affect plasma glucose homeostasis in healthy humans. We investigated the effect of the brown seaweeds Sargassum (S.) fusiforme and Fucus (F.) vesiculosus in their natural form on glucose regulation in patients with T2DM. We conducted a randomized, double-blind, placebo-controlled pilot trial. Thirty-six participants with T2DM received, on a daily basis, either 5 g of dried S. fusiforme, 5 g of dried F. vesiculosus, or 0.5 g of dried Porphyra (control) for 5 weeks, alongside regular treatment. The primary outcome was the between-group difference in the change in weekly average blood glucose levels (continuous glucose monitoring). The secondary outcomes were the changes in anthropometrics, plasma lipid levels, and dietary intake. The data were analyzed using a linear mixed-effects model. The change in weekly average glucose levels was 8.2 ± 2.1 to 9.0 ± 0.7 mmol/L (p = 0.2) in the S. fusiforme group (n = 12) and 10.1 ± 3.3 to 9.2 ± 0.7 mmol/L (p = 0.9) in the F. vesiculosus group (n = 10). The between-group difference was non-significant. Similarly, no between-group differences were observed for the changes in the secondary outcomes. A daily intake of 5 g of fresh, dried S. fusiforme or F. vesiculosus alongside regular treatment had no differential effect on weekly average blood glucose levels in T2DM.

A Review on Therapeutic Potential of <i>Rosmarinus officinalis</i> L

Rosemary (Rosmarinus officinalis L.) is an aromatic evergreen shrub with a long history of culinary and medicinal applications. This review aims to provide a comprehensive overview of the therapeutic potential of rosemary and its bioactive constituents. The plant's essential oil and extracts are rich in potent antioxidant compounds, including carnosic acid, carnosol, rosmarinic acid, and ursolic acid. These phytochemicals have been extensively investigated for their diverse biological activities. Numerous studies have demonstrated the remarkable antioxidant, anti-inflammatory, and antimicrobial properties of rosemary extracts, attributable to their ability to neutralize reactive oxygen species and inhibit pathogenic microorganisms. Moreover, rosemary has shown promising anticancer effects, inducing apoptosis and inhibiting the proliferation of various cancer cell lines, including breast, colon, and leukemia. Emerging evidence also highlights the potential of rosemary in managing metabolic disorders, such as diabetes and hyperlipidemia. Its bioactive compounds have been found to modulate glucose and lipid metabolism through the activation of AMPK and PPAR pathways, thus improving glucose homeostasis and lipid profiles. Moreover rosemary has garnered significant interest for its neuroprotective and cognitive-enhancing properties. Compounds like rosmarinic acid have exhibited cholinergic and neuroprotective effects, inhibiting acetylcholinesterase activity and mitigating oxidative stress in the brain, thereby potentially benefiting neurodegenerative disorders like Alzheimer's and Parkinson's diseases. This review discusses about the vast therapeutic potential of rosemary and its constituents, highlighting the need for further research to elucidate their mechanisms of action, bioavailability, and potential synergistic effects, paving the way for their future application in modern medicine

The effect of date (Phoenix dactylifera L.) varieties on bioactive compounds, phenolic constituents, fatty acids and element contents of date seed and oils

AbstractIn this study, the oil amounts, bioactive components, fatty acid profiles and element quantities of the date kernels (Osailah, Rothanh Qassim, Rushudiah, Nabtat‐Ali, Sbakah) were determined. The oil quantities of the date seeds were altered to be between 3.50 (Osailah) and 5.55% (Nabtat‐Ali). The total phenolic quantities of the seeds were assigned to be between 330.83 (Rothanh Qassim) to 365.42 mg GAE/100 g (Osailah) while antioxidant activities of date seeds are assessed to be between 13.89 (Rothanh Qassim) and 38.74% (Nabtat‐Ali). The total flavonoid quantities of the date seeds were displayed to be between 4824.83 (Osailah) and 9133.17 mg/100 g (Sbakah). The (+)‐ Catechin and 1,2‐dihydroxy benzene quantities of the date seeds were established to be between 75.01 (Rothanh Qassim) and 186.02 mg/100 g (Sbakah) to 67.43 (Rothanh Qassim) and 199.89 mg/100 g (Sbakah), respectively. Oleic acid amounts of the seed oils were altered to be between 45.89 (Rothanh Qassim) and 52.55% (Nabtat‐Ali). K, P, S, Ca and Mg were the key minerals of the date seeds. Considering the bioactive components, polyphenol contents, fatty acid composition and mineral content of date kernels, it is thought that date kernel powders can be added to some foods as a food supplement.

Microwave processing effects on physico-chemical, functional properties, phenolic profile, and Maillard products of flaxseed flour and flaxseed press cake flour

Microwave processing (MwP) is an energy-efficient and impressive method for modifying the functional properties and enhancing the availability of nutrients and bioactive constituents in flaxseeds (FS). The comprehensive and comparative evaluation of FS flour and flaxseed press cake (FPC) flour after MwP is required for large-scale industrial processing and utilization of flaxseeds. In this study, the changes in phenolic composition, Maillard products, physicochemical and functional properties of FS flour and FPC flour after MwP of flaxseeds at 180 W, 360 W, and 540 W for 5, 10, and 15 min were investigated. The unprocessed FS and FPC flour differed in the level of ash, fat, minerals, phenolics, flavonoids, and functional properties. The oil absorption capacity, protein, zinc, and copper augmented in FPC flour and declined in FS flour upon increasing MwP conditions. The phenolic acids (free gallic, protocatechuic, syringic, and caffeic acid, bound protocatechuic and vanillic acid), flavonoids (free rutin, bound epicatechin, and kaempferol), Maillard products, and browning index augmented in FS and FPC flours upon MwP at 540 W for 15 min. However, the L* and b* values, magnesium, potassium, selenium, bound catechin, free epicatechin, and free quercetin declined in FS and FPC flours upon MwP at higher power and time. The FPC flour obtained after MwP at 540 W for 15 min exhibited higher ash (5.71 %), protein (29.46 %), and water absorption (7.17 g/g), lowest emulsifying activity (20.03 m2/g), emulsifying stability (14.66 min) and water solubility (3.95 %) indexes. While the FS flour obtained upon MwP at 540 W for 15 min showed the highest fat content (37.52 %) and water solubility (6.20 %), lowest protein content (24.03 %), minerals, color values, oil absorption (1.69 g/g), emulsifying activity (41.38 m2/g) and stability (21.82 min). In conclusion, the MwP of flaxseeds can be used in industries to improve phenolic profile, Maillard products and modify functional properties of FS and FPC flour for possible utilization in food products.

Protein Tyrosine Phosphatase 1B Inhibitors of Pueraria lobata Based on the Spectrum-Effect Relationship by Q-Marker Selection.

Pueraria lobata (P. lobata), a traditional anti-diabetic medicine mainly composed of flavonoids and isoflavones, has a long history in diabetes treatment in China. However, the anti-diabetic active component is still unclear. Recently, protein tyrosine phosphatase 1B (PTP1B) has been a hot therapeutic target by negatively regulating insulin signaling pathways. In this study, the spectrum-effect relationship analysis method was first used to identify the active components of P. lobata that inhibit PTP1B. The fingerprints of 12 batches of samples were established using high-performance liquid chromatography (HPLC), and sixty common peaks were identified. Meanwhile, twelve components were identified by a comparison with the standards. The inhibition of PTP1B activity was studied in vitro by using the p-nitrophenol method, and the partial least squares discriminant analysis, grey relational analysis, bivariate correlation analysis, and cluster analysis were used to analyze the bioactive compounds in P. lobata. Peaks 6, 9 (glycitin), 11 (genistin), 12 (4'-methoxypuerarin), 25, 34, 35, 36, 53, and 59 were considered as potentially active substances that inhibit PTP1B. The in vitro PTP1B inhibitory activity was confirmed by glycitin, genistin, and 4'-methoxypuerarin. The IC50s of the three compounds were 10.56 ± 0.42 μg/mL, 16.46 ± 0.29 μg/mL, and 9.336 ± 0.56 μg/mL, respectively, indicating the obvious PTP1B inhibitory activity. In brief, we established an effective method to identify PTP1B enzyme inhibitors in P. lobata, which is helpful in clarifying the material basis of P. lobata on diabetes. Additionally, it is evident that the spectrum-effect relationship method serves as an efficient approach for identifying active compounds, and this study can also serve as a reference for screening bioactive constituents in traditional Chinese medicine.

A novel Mediterranean diet-inspired supplement ameliorates cognitive, microbial, and metabolic deficits in a mouse model of low-grade inflammation

ABSTRACT The Mediterranean diet (MD) and its bioactive constituents have been advocated for their neuroprotective properties along with their capacity to affect gut microbiota speciation and metabolism. Mediated through the gut brain axis, this modulation of the microbiota may partly contribute to the neuroprotective properties of the MD. To explore this potential interaction, we evaluated the neuroprotective properties of a novel bioactive blend (Neurosyn240) resembling the Mediterranean diet in a rodent model of chronic low-grade inflammation. Behavioral tests of cognition, brain proteomic analysis, 16S rRNA sequencing, and 1H NMR metabolomic analyses were employed to develop an understanding of the gut-brain axis interactions involved. Recognition memory, as assessed by the novel object recognition task (NOR), decreased in response to LPS insult and was restored with Neurosyn240 supplementation. Although the open field task performance did not reach significance, it correlated with NOR performance indicating an element of anxiety related to this cognitive change. Behavioral changes associated with Neurosyn240 were accompanied by a shift in the microbiota composition which included the restoration of the Firmicutes: Bacteroidota ratio and an increase in Muribaculum, Rikenellaceae Alloprevotella, and most notably Akkermansia which significantly correlated with NOR performance. Akkermansia also correlated with the metabolites 5-aminovalerate, threonine, valine, uridine monophosphate, and adenosine monophosphate, which in turn significantly correlated with NOR performance. The proteomic profile within the brain was dramatically influenced by both interventions, with KEGG analysis highlighting oxidative phosphorylation and neurodegenerative disease-related pathways to be modulated. Intriguingly, a subset of these proteomic changes simultaneously correlated with Akkermansia abundance and predominantly related to oxidative phosphorylation, perhaps alluding to a protective gut-brain axis interaction. Collectively, our results suggest that the bioactive blend Neurosyn240 conferred cognitive and microbiota resilience in response to the deleterious effects of low-grade inflammation.

Geniposide dosage and administration time: Balancing therapeutic benefits and adverse reactions in liver disease treatment

Gardenia jasminoides Ellis, a staple in herbal medicine, has long been esteemed for its purported hepatoprotective properties. Its primary bioactive constituent, geniposide, has attracted considerable scientific interest owing to its multifaceted therapeutic benefits across various health conditions. However, recent investigations have unveiled potential adverse effects associated with its metabolite, genipin, particularly at higher doses and prolonged durations of administration, leading to hepatic injury. Determining the optimal dosage and duration of geniposide administration while elucidating its pharmacological and toxicological mechanisms is imperative for safe and effective clinical application.This study aimed to evaluate the safe dosage and administration duration of geniposide in mice and investigate its toxicological mechanisms within a comprehensive dosage-duration-efficacy/toxicity model. Four distinct mouse models were employed, including wild-type mice, cholestasis-induced mice, globally farnesoid X-activated receptor (FXR) knock out mice, and high-fat diet-induced (HFD) NAFLD mice. Various administration protocols, spanning one or four weeks and comprising two or three oral doses, were tailored to each model's requirements. Geniposide has positive effects on bile acid and lipid metabolism at doses below 220 mg/kg/day without causing liver injury in normal mice. However, in mice with NAFLD, this dosage is less effective in improving liver function, lipid profiles, and bile acid metabolism compared to lower doses. In cholestasis-induced mice, prolonged use of geniposide at 220 mg/kg/day worsened liver damage. Additionally, in NAFLD mice, this dosage of geniposide for four weeks led to intestinal pyroptosis and liver inflammation. These results highlight the lipid-lowering and bile acid regulatory effects of geniposide, but also warn of potential negative impacts on intestinal epithelial cells, particularly with higher doses and longer treatment durations. Therefore, achieving optimal therapeutic results requires a decrease in treatment duration as the dosage increases, in order to maintain a balanced approach to the use of geniposide in clinical settings.

In vitro and in vivo exploitation of cell stress pathways using methanolic extracts of Phlomis stewartii in diabetic rat’s model

Various bioactive constituents present in plants are used to treat metabolic disorders linked to oxidative stress and obesity. Low-grade to chronic inflammation and IR are considered as main causes of obesity, which is strongly correlated with the prevalence and incidence of Type-2 Diabetes Mellitus (T2DM). In this study, the biological influence of Phlomis stewartii extracts was evaluated in vitro and in vivo using rat diabetic models. The biological effects included anti-inflammatory, anti-proliferative, anti-apoptotic, metabolic hormonal via molecular signaling pathways, and antioxidant potential. The extracts from P. stewartii exhibited the strongest DPPH and FRAP potential for LM (38.92 µg/mL) and (45.28 µg/mL) respectively. Moreover, the high absorbance for reducing power was observed in leaves methanol (LM) 1.36 which is greater than flower methanol (FM) 1.12, and whole plant methanol (WPM) 1.21 at a concentration of 500 µg/mL when comparing treated groups to the negative control (NC), and positive control (PC) groups. The results of an Enzyme-linked Immunosorbent Assay (ELISA) study measuring a metabolic hormonal profile that includes Triiodothyronine (T3), Thyroxine (T4), Thyroid Stimulating Hormone (TSH), insulin, leptin, and glucokinase showed that LM has been greatly recovered. The study examined the gene expression analysis of cell stress pathways, and it found that the PC groups had higher levels of Janus kinase (JAK), Signal Transducer and Activator of Transcription (STATS) pathways through JAK (JAK-2 and STAT-1), G protein-Coupled Receptor Kinase 2 (GRK-2), Calmodulin 2 (CALM-2), Proteins Inhibitor of Activated STAT 1 (PIAS-1), Forkhead Box 01, 03, 04, (FOXO-1, FOXO-3, FOXO-4), Bcl-2 Associated X-protein (BAX), B-cell Lymphoma 2 (BCL-2), Interleukins (IL-6, IL-1β), and Tumour Necrosis Factor-α (TNF-α). On the other hand, downregulation was observed in NC groups and P. stewartii extract-treated groups. The outcome of this study suggests a strong relationship towards ameliorative effects.

Anti-acute gastric ulcer resistance of Aurantii Fructus Immaturus juice processing Atractylodis Macrocephalae Rhizoma by regulating PTGS2, MAPK1, and KDR targets based on metabolomics and integrated network pharmacology analysis

Abstract Background Currently, traditional methods of treating acute gastric ulcer (AGU) have many drawbacks, necessitating an alternative therapy with fewer adverse effects. Atractylodis Macrocephalae Rhizoma (BZ) is known for strengthening the spleen and harmonizing the stomach. BZ processed with Aurantii Fructus Immaturus juice (ZSZBZ), a classic decoction since the Han Dynasty, can enhance the efficacy of BZ. However, the key active components and targets of action of ZSZBZ remain undiscovered. Aim of the study This study aimed to investigate the bioactive chemical constituents of ZSZBZ against AGU and their possible mechanisms of action, elucidating the scientific content of ZSZBZ processing. Materials and methods Initially, we examined rat stomach histopathology and conducted ELISA for oxidative stress and inflammation. Subsequently, we investigated underlying mechanisms using metabolomics. Further analysis of potent components and key targets in ZSZBZ was conducted through liquid chromatography-mass spectrometry analysis combined with network pharmacology. Finally, key targets were analyzed by Western blot. Results ZSZBZ improved gastric histopathology, reversing high alcohol-induced oxidative stress (SOD, CAT) and inflammatory level (TNF-α, IL-6) disorders. This is associated with ZSZBZ’s regulation of amino acid metabolism, energy metabolism, and inflammatory response-related metabolic pathways, along with key targets PTGS2, MAPK1, and KDR. The significant increase in potency of ZSZBZ may be attributed to elevated levels of naringenin, hesperidin, hesperidin, and rhamnoceroside after concoction. Conclusions Combining metabolomics and network pharmacology, this study elucidated that ZSZBZ enhanced gastroprotection by modulating amino acid metabolism, antioxidant, and inflammation-related targets and pathways, providing insights into the bioactive compounds and potential mechanisms of herbal concoctions.

Exploring the anti-gastric cancer mechanism of action of Bidentis Bipinnatae Herba based on network pharmacology, molecular docking, and cellular experimental validation.

The purpose of this study is to explore the potential molecular mechanism of Bidentis Bipinnatae Herba against gastric cancer by using network pharmacology methods, molecular docking, and cellular experimental validation. Medicinal plants related to gastric cancer were queried through TCMSP, SymMap, and Herb databases. The TCSMP database (drug-likeness ≥ 0.18) was used to retrieve the bioactive constituents. TCSMP, SwissTargetPrediction, and Herb databases were used to retrieve the target genes, and Cytoscape software was used to construct the "active ingredient-target" network. After protein interaction analysis using String 11.0 platform, the hub genes were screened using CytoHubba. The obtained hub genes were uploaded to the cBioPortal for pathway enrichment. The genes involved in gastric cancer-related RTK-RAS pathway were molecularly docked and experimentally validated. Bidentis Bipinnatae Herba was common to TCMSP, SymMap, and Herb databases. A total of nine active ingredients were obtained in Bidentis Bipinnatae Herba, acting on 192 targets. Seven hub genes were obtained from these target genes and enriched in the RTK-RAS pathway in gastric cancer. MAPK1 and EGFR had good molecular docking results with their corresponding chemicals. Cellular experiments showed that the treatment of luteolin, quercetin, and Okanin reduced the expression of EGFR in AGS cells; the treatment of luteolin and quercetin could reduce the expression of MAPK1. Bidentis Bipinnatae Herba contained active components, which may be anti-gastric cancer in a multi-target (MAPK1 and EGFR) manner.

Response of Yield, Quality, and Bioactive Constituents of Green Onion to Foliar Spraying with Moringa oleifera Leaf Extract and Yeast Extract

Response of Yield, Quality, and Bioactive Constituents of Green Onion to Foliar Spraying with Moringa oleifera Leaf Extract and Yeast Extract

Pharmaceutical prospects of pomegranate antioxidants in combating microbial infections

ABSTRACT Pomegranates, which are renowned for their diverse bioactive phytochemicals with antioxidant, anti-inflammatory, and antimicrobial properties, have garnered significant interest in the field of natural medicine. This study aimed to systematically investigate the phytochemical content, bioavailability, and antimicrobial effects of extracts derived from different parts of three Jordanian pomegranate cultivars, Kodari, Qerati, and Black. Comprehensive quantitative analyses revealed significantly higher phenolic content and antioxidant capacities in peel extracts, particularly in the Black and Qerati cultivars. The total phenolic content was determined using the Folin-Ciocalteu colorimetric assay, and the antioxidant activity was evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay. Bioavailability was determined using stimulated gastrointestinal digestion assays, revealing controlled release in gastric fluid compared to more substantial release in intestinal fluid, thereby suggesting potential implications for bioavailability. Furthermore, antimicrobial assays showed promising antibacterial effects against Staphylococcus aureus in a time-dependent manner, although the efficacy varied among the cultivars and components. These findings underscore the multifaceted bioactive potential of pomegranate extracts, particularly those derived from optimized peel extracts, positioning them as promising natural preservatives or functional ingredients. However, further research is warranted to delve into specific bioactive constituents, absorption mechanisms, and their potential applications in diverse fields, such as foods, nutraceuticals, and pharmaceuticals. By expanding the current understanding of the factors influencing pomegranate bioactivities, this study lays the groundwork for tailored utilization of pomegranate fractions based on ideal phytochemical profiles and targeted effects.

A Review on Divine Tree Nyctanthes Arbor-Tristis Linn – A Treasure House of Therapeutic Components

Nyctanthes arbor-tristis Linn is a short ancient tree believed to be a divine tree in India. The tree bears beautiful white flowers known for its aura. It is extensively cultivated in tropical and subtropical regions across the world. Since time immemorial, crude extracts of each part of the tree is used as a classical medicine in treatment of organ disorders, fevers, infections, expectorant, allergies, gynaecological problems, and various other diseases. Nyctanthes arbor-tristis Linn possess phytochemicals such as Alkaloids, steroids, Glycosides, flavonoids, Terpenes, essential oils, proteins that exhibit pharmacological activities like anti-inflammatory, anti-cancer, anti-diabetic, hepato-protective, CNS depressant, anti-anaemic, antipyretic, sedative and many more. This review article has included all the possible details about the plant, its distribution phytochemical constituents, and pharmacological activities. Phytochemical studies and Nyctanthes arbor-tristis Linn’s pharmacological activities indicated it as a potential medicinal plant for various elements. However, more research is crucial to investigate the mode of action of the plant’s bioactive constituents and its therapeutic potential.

Chemical Constituents of the Marine Traditional Chinese Medicine of Pegasus laternarius Cuvier (Hai-E Yu)

Pegasus laternarius Cuvier (Hai-E Yu) is a marine traditional Chinese medicine that has been used to treat cancers and reduce inflammation. Previous chemical investigations have only revealed the occurrence of high levels of protein, fatty acids, and a large number of steroids, thus more active compounds in P. laternarius still need to be further discovered. The present study aims to search for new bioactive constituents of P. laternarius with cytotoxic effects and nitric oxide (NO) inhibitory activities. In this work, 16 pure compounds from the ethyl acetate fraction of Pegasus laternarius Cuvier were successively obtained by various chromatographic techniques, and the structure of the isolates was elucidated by spectroscopic analyses. The isolated and identified compounds included one 2H-1,2,3-triazole-4-carboxylate derivative (1), two oxadiazines (2, 3), two amino acids (4, 5), three nucleosides (6–8), three steroids (9–11), and five others (12–16). All the obtained compounds were evaluated for their antitumor activity on A549 and HCT-116 cell lines along with their inhibitory effects on lipopolysaccharide-induced NO production in RAW264.7 cells. The triazole compound 1 was found to exhibit moderate cytotoxicity against two human cell lines (A549 and HCT-116) with IC50 values of 44.5 and 32.9 μmol/L, respectively. The steroid compound 10 inhibited NO production with IC50 values lower than 50 μmol/L. Consequently, this study provides insight into the cytotoxic and NO inhibitory activities of the marine traditional Chinese medicines in Hai-E-Yu.

Antibacterial, anti-invasive, and anti-inflammatory activity of bovine lactoferrin extracted from milk or colostrum versus whole colostrum.

Lactoferrin (Lf), a multifunctional cationic glycoprotein extracted from milk or colostrum, is able to chelate two ferric ions per molecule, inhibit the formation of reactive oxygen species, interact with the anionic components of bacteria or host cells, and enter inside host cell nucleus, thereby exerting antibacterial, anti-invasive, and anti-inflammatory activities. By virtue of Lf presence, bovine colostrum is expected to perform analogous functions to pure Lf, along with additional activities attributable to other bioactive constituents. The present research aims to compare the antibacterial, anti-invasive, and anti-inflammatory activities of bovine Lf purified from milk (mbLf) and colostrum (cbLf) in comparison to those exhibited by whole bovine colostrum (wbc). The results demonstrated a major efficacy of mbLf in inhibiting pathogenic bacteria and in exerting anti-invasive and anti-survival activities with respect to cbLf and wbc. Furthermore, mbLf lowered IL-6 levels to those of uninfected cells, while a less evident decrease was observed upon cbLf treatment. Conversely, wbc managed to slightly lower IL-6 levels compared to those synthesized by infected cells. These data demonstrate that, to obtain maximum effectiveness in such activities, Lf should be formulated/used without addition of other substances and should be sourced from bovine milk rather than colostrum.

Elevated PINK1/Parkin-Dependent Mitophagy and Boosted Mitochondrial Function Mediate Protection of HepG2 Cells from Excess Palmitic Acid by Hesperetin.

Deregulation of mitochondrial functions in hepatocytes contributes to many liver diseases, such as nonalcoholic fatty liver disease (NAFLD). Lately, it was referred to as MAFLD (metabolism-associated fatty liver disease). Hesperetin (Hst), a bioactive flavonoid constituent of citrus fruit, has been proven to attenuate NAFLD. However, a potential connection between its preventive activities and the modulation of mitochondrial functions remains unclear. Here, our results showed that Hst alleviates palmitic acid (PA)-triggered NLRP3 inflammasome activation and cell death by inhibition of mitochondrial impairment in HepG2 cells. Hst reinstates fatty acid oxidation (FAO) rates measured by seahorse extracellular flux analyzer and intracellular acetyl-CoA levels as well as intracellular tricarboxylic acid cycle metabolites levels including NADH and FADH2 reduced by PA exposure. In addition, Hst protects HepG2 cells against PA-induced abnormal energetic profile, ATP generation reduction, overproduction of mitochondrial reactive oxygen species, and collapsed mitochondrial membrane potential. Furthermore, Hst improves the protein expression involved in PINK1/Parkin-mediated mitophagy. Our results demonstrate that it restores PA-impaired mitochondrial function and sustains cellular homeostasis due to the elevation of PINK1/Parkin-mediated mitophagy and the subsequent disposal of dysfunctional mitochondria. These results provide therapeutic potential for Hst utilization as an effective intervention against fatty liver disease.