Major Bioactive Components Research Articles

Effect of extraction and purification on the structure and activity of Flammulina velutipes polysaccharides: a review

SummaryFlammulina velutipes (F. velutipes) is one of the most widely consumed edible mushrooms worldwide. The growth of F. velutipes involves two primary stages: the mycelium and fruiting body. Unique polysaccharides are produced in each stage; mycelial polysaccharides (FVMPs) are produced during the mycelial fermentation stage, while fruiting body polysaccharides (FVFBPs) are produced during the fruiting stage. These polysaccharides, the major bioactive components of F. velutipes, have garnered significant attention due to their various functions and activities. Notably, they exert functional activities by mediating gut flora, including antioxidant, anti‐inflammatory, and immunomodulatory properties, reduce blood sugar and lipid levels, and enhance cognitive performance. This study examined the variations in FVMPs and FVFBPs resulting from different extraction and purification methods, with a specific focus on delineating their distinct structural characteristics. This study further explored the impact of the structural composition of FVMPs and FVFBPs on their health‐promoting properties, focusing on the relationship between their structures and their functional and biological effects. Finally, this study outlines future research avenues designed to contribute to the ongoing research in the field of bioactive FVMPs and FVFBPs.

Potential skincare benefits and self-healing properties of Lignosus rhinocerotis polysaccharides as affected by ultrasound-assisted H2O2/Vc treatment

Natural polysaccharides have been recognized as major bioactive components in skincare and wound care products. In this study, the skincare benefits and self-healing properties of Lignosus rhinocerotis polysaccharides (LRP) and its degraded products (DLRP-1, DLRP-2 and DLRP-3) by ultrasound assisted H2O2/Vc treatment (U-H/V) at different ultrasonic intensity (28.14, 70.35, and 112.56 W/cm2) were investigated. U-H/V altered the internal crystalline structure and microstructure of LRP, and enhanced the thermal stability. Due to the breakage of molecular chains after U-H/V, the moisture absorption of LRP was enhanced but the moisturizing property showed a different degree of reduction. U-H/V significantly improved the antioxidant, anti-tyrosinase and anti-inflammatory activities of LRP. Furthermore, the results of enzyme kinetic studies showed a mixed competitive-noncompetitive inhibition of tyrosinase activity by DLRP-3 and the inhibition constant of DLRP-3 on tyrosinase was 2.97 mg/mL. The apparent viscosity of LRP dispersions showed a first increasing followed by decreasing trend as ultrasonic intensity rose. U-H/V enhanced the viscoelastic properties of LRP gels without destroying their self-healing properties. This findings reveal that U-H/V is beneficial for improving the skincare efficacy of LRP, providing a theoretical foundation for the applicability of LRP in wound dressings.

Exploring the bioactive ingredients of three traditional Chinese medicine formulas against age-related hearing loss through network pharmacology and experimental validation.

Traditional Chinese medicine (TCM) formulas, including the Er-Long-Zuo-Ci pill, Tong-Qiao-Er-Long pill, and Er-Long pill, have long been utilized in China for managing age-related hearing loss (ARHL). However, the specific bioactive compounds, pharmacological targets, and underlying mechanisms remain elusive. This study aims to find the shared bioactive ingredients among these three formulas, uncover the molecular pathways they regulate, and identify potential therapeutic targets for ARHL. Furthermore, it seeks to validate the efficacy of these major components through both in vivo and in vitro experiments. Common bioactive ingredients were extracted from the TCMSP database, and their putative target proteins were predicted using the Swiss Target Prediction database. ARHL-related target proteins were collected from GeneCards and OMIM databases. Our approach involved constructing drug-target networks and drug-disease-specific protein-protein interaction networks and conducting clustering, topological property analyses, and functional annotation through GO and KEGG enrichment analysis. Molecular docking analysis was utilized to delineate interaction mechanisms between major bioactive ingredients and key target proteins. Finally, in vivo and in vitro experiments involving ABR recording, immunofluorescent staining, HE staining, and quantitative PCR were conducted to validate the treatment effects of flavonoids on the declining auditory function in DBA/2J mice. We identified 11 common chemical compounds across the three formulas and their associated 276 putative targets. Additionally, 3350 ARHL-related targets were compiled. As an intersection of the putative targets of the common compounds and ARHL-related proteins, 145 shared targets were determined. Functional enrichment analysis indicated that these compounds may modulate various biological processes, including cell proliferation, apoptosis, inflammatory response, and synaptic connections. Notably, potential targets such as TNFα, MAPK1, SRC, AKT, EGFR, ESR1, and AR were implicated. Flavonoids emerged as major bioactive components against ARHL based on target numbers, with molecular docking demonstrating diverse interaction models between these flavonoids and protein targets. Furthermore, baicalin could mitigate the age-related cochlear damage and hearing loss of DBA/2J mice through its multi-target and multi-pathway mechanism, involving anti-inflammation, modulation of sex hormone-related pathways, and activation of potassium channels. This study offers an integrated network pharmacology approach, validated by in vivo and in vitro experiments, shedding light on the potential mechanisms, major active components, and therapeutic targets of TCM formulas for treating ARHL.

Phytochemical and Antioxidant Analysis of Artocarpus heterophyllus Peel Extracts

BACKGROUND: Plants have a diverse variety of bioactive compounds such as tannins, alkaloids, flavonoids, carbohydrates and steroids among many others that can offer significant physiological actions in the human body. Phytochemicals are naturally occurring chemical, biological and active compounds found in plants that are of benefit to human health apart from those that act as macronutrients and micronutrients. A. heterophyllus (Jackfruit) belongs to the family Moraceae. Jackfruit tree is native to India and is popular in several tropical and sub-tropical Countries. OBJECTIVE: The aim of this study is to determine the phytochemical constituents, antioxidant properties and gas chromatography mass spectroscopy (GC-MS) of the fruit peel of A. heterophyllus extracts using three different solvents. METHODS: Artocarpus heterophyllus fruits were collected from University of Ibadan botanical garden, identified at the Forestry Research Institute of Nigeria, Oyo State. The peel was extracted and dried at 35 ℃. Qualitative method and Gas Chromatography Mass Spectroscopy were used to determine the phytochemical and bioactive compounds present in the plant, whereas¬¬¬¬¬¬ 2, 2, Diphenylpicryl-1-hydrazyl (DPPH) was used for the antioxidant analysis. RESULTS: Secondary metabolites such as flavonoids, phenols, alkaloids, glycosides, saponins, tannins, steroids, and Terpenoids were present based on the solvents while anthraquinnes were absent. Flavonoid and phenol were abundant in the three extracts while saponin was moderate. Eight chemical compounds were observed in the plant extracts. Major bioactive components with highest and lowest retention peak were (65.55 %) bis(2- ethyl hexyl) phthalate and (6.06 %) Cis- 13(2- ethylhexyl)phthalate respectively. Antioxidant activity increased with increase in concentration of which acetone extract had the highest DPPH (75.00 %) at 100 μg/ml. CONCLUSION: The fundamental means of the usage of medicinal plants for medicine is due to their bioactive properties which are used as substrates for biochemical and enzymatic reactions. Phytochemical derivatives have antiviral, anti-inflammatory, anti-oxidant, immunomodulatory, anticancer, antimicrobial, antitumor, analgesic and many other properties harbor in them.

Comprehensive Isolation and Characterization of Theaflavins, Thearubigins and Caffeine as Bioactive Compounds from Darjeeling Black Tea

The present study aimed to isolate and characterize three major bioactive components viz. theaflavins, thearubigins and caffeine from Darjeeling black tea, which contribute significantly to the cup characteristics and health benefits of black tea. Theaflavins were isolated using Soxhlet extraction followed by column chromatography, HPLC and UV spectroscopy. HPLC showed effective separation of four major theaflavins. Thearubigins were isolated using liquid-liquid extraction and characterized through NMR, FTIR-ATR and UV spectroscopic techniques. The NMR spectral studies suggested thearubigins to be polymeric oxidation products of catechin groups, while FTIR spectral studies indicated similarity with proanthocyanidin-like polymers. Caffeine was isolated via a solid-liquid extraction followed by liquid-liquid extraction and identified using TLC, NMR, UV and SEM techniques. TLC showed an Rf value of 0.65, which is consistent with standard caffeine. The NMR confirmed the purity of isolated caffeine and SEM revealed its needle-shaped crystal morphology. The results show that these bioactive compounds may be efficiently isolated and characterized using chromatographic and spectroscopic methods.

Chicory supplementation improves growth performance in juvenile ostriches potentially by attenuating enteritis.

Enteritis and dysbiosis are the major causes of high morbidity and mortality of juvenile ostriches. Chicory (CC) has been proven to have excellent antioxidant, anti-inflammatory, and antibacterial activities. However, it's unclear whether CC could improve the survival rate of juvenile ostriches by relieving enteritis and correcting dysbiosis. South African ostrich hatchlings (Struthio camelus domesticus) were fed with and without a CC-supplemented diet, and the body weight gain and mortality were compared over 4 months of age. Fresh fecal samples of clinically healthy ostriches were collected, and 16S DNAs were analyzed. Moreover, ostrich chicks with LPS-induced enteritis were fed with different dosages (0, 20, 40, and 80 mg/kg) of chicoric acid (CA), a major bioactive component of CC, for five consecutive days. The expression levels of tight junction (TJ)-related proteins and inflammatory mediators in the ilea were detected with western blot and immunofluorescence. The ostrich chicks fed on the CC-supplemented diet began to increase in weight at the 1st month of age and became remarkably heavier at the fourth month (p < 0.01) compared with those fed on the non-CC-supplemented diet. Additionally, the mortality percentage was lower in the chicks fed on the CC-supplemented diet than those fed on the non-CC-supplemented diet (19% vs. 36%, respectively). The diet with the CC supplementation significantly increased the abundance of Phascolactobacteria (linear discriminant analysis; LDA >4) and Bacteroidota (26.7% vs. 17.7%, respectively) as well as decreased the enrichment of Clostridium (5.0% vs. 9.1%, respectively) in the ostrich ilea compared to the diet without CC. The supplementation of CA at a dose of 80 mg/kg significantly increased the expression level of ZO-1 and claudin-3 (p < 0.0001) and suppressed the levels of IL-1β, IL-6, and TNF-α (p < 0.0001) in ostriches with LPS-induced ileitis. Our results substantiate that CC or CA supplementation in a diet could effectively improve growth performance and reduce mortality in juvenile ostriches via modulating the gut microbiota and attenuating enteritis.

In vivo absorption, in vitro digestion, and fecal fermentation properties of non-starch polysaccharides from Chinese chestnut kernels and their effects on human gut microbiota

Non-starch polysaccharides are major bioactive components in chestnuts, and can serve as water-soluble polysaccharides with potential prebiotic properties. This study aims to establish an in vitro digestion and fermentation model to reveal the digestive and fermentative characteristics of Non-starch polysaccharides from chestnut kernels (NSPCK). The results indicated that under simulated digestion, NSPCK was partially digested in gastric juice but remained significantly undigested in saliva and intestinal juice, demonstrating considerable resilience against hydrolysis. After digestion, NSPCK still exhibited stable rough, lamellar, and porous structure and maintained strong antioxidant capacity. Animal experiments revealed positive effects of NSPCK on blood lipid level, and colon tissue of mice. Moreover, NSPCK enhanced the accumulation of short-chain fatty acids during fermentation, particularly acetic acid, propionic acid, and butyric acid. Furthermore, NSPCK intervention increased the abundance of beneficial bacteria such as Lactobacillus and Bifidobacterium, and at the same time reduced that of harmful bacteria such as Enterococcus.

TSG Extends the Longevity of Caenorhabditis elegans by Targeting the DAF-16/SKN-1/SIR-2.1-Mediated Mitochondrial Quality Control Process.

The improvement of mitochondrial function is described as a strategy for alleviating oxidative stress and intervening in the aging process. 2,3,5,4'-Tetrahydroxystilbene-2-O-β-D-glucoside (TSG) is one of the major bioactive components isolated from Polygonum multiflorum Thunb, and it exhibits multiple activities, including antioxidant and anti-inflammatory effects. In this study, we found that 200 μM TSG significantly extended the mean lifespan of Caenorhabditis elegans by 16.48% and improved health status by delaying age-associated physiological decline in worms. The longevity prolongation effect of TSG depended on the regulation of the mitochondrial quality control process mediated by DAF-16/FOXO, SKN-1/Nrf2 and SIR-2.1/SIRT1 to improve mitochondrial function. Moreover, TSG treatment obviously alleviated the proteotoxicity of β-amyloid and tau proteins in worms. Our findings indicated that TSG is a promising natural product for preventing aging and treating aging-associated neurodegenerative diseases by regulating the mitochondrial quality control process to improve mitochondrial function.

Separation of major bioactive components by GC-MS and antioxidant studies on Solanum nigrum extract

Separation of major bioactive components by GC-MS and antioxidant studies on Solanum nigrum extract

Astragaloside IV attenuates fatty acid-induced renal tubular injury in diabetic kidney disease by inhibiting fatty acid transport protein-2

BackgroundRenal tubular injury induced by free fatty acid bound to albumin is the key pathological basis for the progression of diabetic kidney disease. However, effective interventions are limited. Astragaloside IV, as a major bioactive component purified from Astragalus membranaceus (Fisch.) Bunge, possesses pharmacological properties of lowering blood glucose and proteinuria, and renal tubular protection in diabetic kidney disease. Further work is needed to understand the underlying molecular mechanisms. PurposeThis study was designed to investigate the mechanism of renal tubular protection by astragaloside IV in diabetic kidney disease. MethodsRats receiving high-fat diet combined with streptozotocin (30 mg/kg, i.p.) were gavaged with astragaloside IV (10 mg/kg/d or 20 mg/kg/d) or empagliflozin (1.72 mg/kg/d) for 8 weeks. In vitro, the NRK-52E cells were treated with free fatty acid-deleted BSA or palmitic acid-bound BSA in the presence or absence of astragaloside IV (5 μM, 10 μM, 20 μM) or 5 μM of mcc950. The effects of astragaloside IV on mitochondrial function, NLRP3/ASC/IL-18/IL-1β inflammatory cascade, and renal tubular injury were detected by pathological staining, immunoblotting, MitoSOX Red staining. Next, to investigate the mechanism of renal tubular protection by astragaloside IV, we transfected Fatp2 siRNA into BSA-PA-treated NRK-52E cells and injected lipofermata (a FATP2 inhibitor) intraperitoneally into free fatty acid-bound BSA overloaded rats with concomitant astragaloside IV treatment. ResultsTreatment with astragaloside IV for 8 weeks dose-dependently attenuated the blood glucose, ratio of urinary albumin to creatinine, disorder of lipid metabolism, and pathological injury in diabetic kidney disease rats. In addition, astragaloside IV dose-dependently attenuated mitochondrial-derived reactive oxygen species and subsequent inhibiting NLRP3-mediated inflammatory cascade in diabetic kidney disease rats and palmitic acid-bound BSA-treated NRK-52E cells, thereby exerting renal tubular protection. More importantly, the effects of astragaloside IV on restoration of mitochondrial function, inhibition of inflammatory response and amelioration of renal tubular injury in vivo and in vitro were further enhanced when used in combination with Fatp2 siRNA or lipofermata. ConclusionAstragaloside IV exerts antioxidant and anti-inflammatory effects in diabetic kidney disease by inhibiting FATP2-mediated fatty acid transport, thereby attenuating renal tubular injury.

Mechanisms of Yiai Fuzheng formula in the treatment of triple-negative breast cancer based on UPLC-Q-Orbitrap-HRMS, network pharmacology, and experimental validation

Ethnopharmacological relevanceYiai Fuzheng formula (YAFZF), as a Traditional Chinese Medicine (TCM) prescription, has been used widely at Zhongnan Hospital of Wuhan University for its therapeutic effects and high safety on triple-negative breast cancer (TNBC). ObjectiveIn this study, we employed ultra-high-performance liquid chromatography-quadrupole/orbitrap high-resolution mass spectrometry (UPLC-Q-Orbitrap-HRMS), network pharmacology, and experimental validation to elucidate the underlying action mechanism of YAFZF in the treatment of TNBC. MethodsThe key active ingredients in YAFZF were analyzed using UPLC-Q-Orbitrap-HRMS, and then the potential components, target genes and signalling pathways of YAFZF were predicted using the network pharmacological method. We then used molecular docking to visualize the combination characteristics between major active components and macromolecules in the crucial pathway. In vitro experiments were conducted to investigate the inhibitory effects of YAFZF treatment on the cell viability, invasion, and migration of 4T1 and MDA-MB-231 cells. The xenograft TNBC models were constructed using female Balb/c mice, and their body weights, tumour volumes, and weights were monitored during YAFZF treatment. Quantitative real-time PCR (qRT-PCR), Hematoxylin-eosin (HE), immunohistochemistry (IHC) staining, Western blot (WB), and terminal deoxynucleotidyl transferase (TdT)-dUTP nick-end labeling (TUNEL) staining were used for further experimental validation. ResultsBased on UPLC-Q-Orbitrap-HRMS and network pharmacology analysis, 6 major bioactive components and 153 intersecting genes were obtained for YAFZF against TNBC. Functional enrichment analysis identified that the phosphatidylinositol 3-kinase (PI3K)-protein kinase B (Akt) signalling pathway might be the mechanism of action of YAFZF in the treatment of TNBC. Molecular docking results suggested that the main active compounds in YAFZF had strong binding energies with the proteins in the PI3K/Akt pathway. In vitro experiments showed that YAFZF inhibited the cell viability, invasion, and migration abilities of TNBC cells. Animal experiments confirmed that YAFZF treatment suppressed tumour cell proliferation and increased apoptotic cells. PCR, HE, WB, and IHC results indicated that YAFZF could suppress xenograft tumour metastases by inhibiting the PI3K/AKT/mTOR pathway regulating the epithelial-mesenchymal transition (EMT) process. ConclusionYAFZF therapy showed its potential for reducing proliferation, invasion, and migration abilities, increasing apoptosis of TNBC cells. Furthermore, YAFZF treated TNBC by inhibiting xenograft tumour distant metastases via the regulation of EMT by the PI3K/Akt/mTOR pathway, suggesting that it may be useful as an adjuvant treatment.

Early Preclinical Studies of Ergosterol Peroxide and Biological Evaluation of Its Derivatives.

Ganoderma lucidum is a medicinal mushroom that produces various pharmacological compounds, including triterpenoids. A major bioactive component of G. lucidum is ergosterol peroxide (EP), which is attributed to its anticancer effects. The current study focuses on the in vitro ADME (absorption, distribution, metabolism, and elimination), in vivo efficacy and toxicity of EP, and the synthesis of new EP derivatives to improve aqueous solubility. It was found that EP is metabolically stable in liver microsomes and plasma. In vivo studies showed that EP inhibits tumor growth in murine cancer models, and it is well tolerated by mice. The maximum tolerated dose was investigated in mice at escalating doses with a defined maximum amount of 500 mg/kg, which indicated no signs of toxicity, confirmed by plasma chemistry and analysis of harvested tissues. Complementary organ toxicity assays including cardio and hepatotoxicity assays of EP demonstrated no inhibitory effects. Next, a focused library of EP derivatives was developed to investigate the iterative addition of heteroatoms to improve the aqueous solubility properties of EP. Significant solubility improvement was observed by the introduction of hydrogen bonding promoting groups, particularly the sulfate group. Superior aqueous solubility properties are directly correlated with the biological activity of the compound against triple-negative breast cancer cellular (TNBC) models. The EP derivatives maintain ample therapeutic index at the tested concentrations, indicating they engage with the same biological target(s) as the parental compound (EP). The combined studies indicate that EP and its derivatives are selective TNBC cell death inducers, while sparing noncancerous tissue.

Pharmacokinetics of two triterpenoid saponins and three flavonoids in Astragalus membranaceus leaves by UHPLC-MS/MS

Astragalus membranaceus (A. membranaceus) leaves can be used both as a medicine and food material. Their main chemical components are flavonoids and triterpenoid saponins. The pharmacokinetics of A. membranaceus leaves are rarely reported in the literature. This study aimed to investigate the pharmacokinetics of five major bioactive components of A. membranaceus leaves [rhamnocitrin 3-glucoside (RCG), tiliroside (TIL), rhamnocitrin 3-neohesperidoside (RNH), huangqiyenin R (HuR), and huangqiyenin I (HuI)]. Simultaneously using ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method. The extract of A. membranaceus leaves was administered orally to rats, and the rat plasma was subjected to a fast, sensitive, and specific UHPLC-MS/MS method. Butylparaben served as the internal standard. The plasma samples were pretreated using isopropanol/ethyl acetate (1:1, v/v) liquid–liquid extraction. Chromatographic separations were performed at a flow rate of 0.3 mL/min on a Waters ACQUITY HSS T3 Column (2.1 mm × 100 mm, 1.8 μm) using mobile phases of 0.1 % formic acid/water and 0.1 % formic acid/acetonitrile. Mass spectrometry detection was performed using an electrospray ionization ion source in the negative-ion mode and the multiple reaction monitoring mode. All analytes had an intraday and interday relative standard deviation of less than 14.10 %. The range of accuracy was –11.94–6.920 % and –15.22–5.800 %. The lower limits of quantification for RCG, TIL, RNH, HuR, HuI was 10.24, 10.27, 10.12, 5.137, and 5.841 ng/mL, respectively. The criteria were met by stability, matrix effects, and extraction recovery. The pharmacokinetic parameters of A. membranaceus leaf extract were ultimately obtained using this analytical method. The study provides a theoretical basis for future pharmacological research, clinical application, and development of healthy food from A. membranaceus leaves.

Protective effects and regulatory mechanisms of Platycodin D against LPS-Induced inflammatory injury in BEAS-2B cells

Platycodin D (PLD), a major bioactive component of triterpene saponins found in Platycodon grandiflora, is renowned for its anti-inflammatory and antioxidant properties. This study aims to explore the protective effects and regulatory mechanisms of PLD in an LPS-induced inflammation injury model of BEAS-2B cells. Initially, PLD was identified from Platycodon grandiflora extracts utilizing UPLC-Q-TOF-MS/MS technology. The effects of PLD on the viability, morphology, ROS levels, and inflammatory factors of LPS-induced BEAS-2B cells were then investigated. The results showed that PLD significantly alleviated LPS-induced oxidative stress and inflammatory injury. Further analysis revealed that PLD positively influenced apoptosis levels, mitochondrial morphology, and related gene expression, indicating its potential to mitigate LPS-induced apoptosis and alleviate mitochondrial dysfunction. Using molecular docking technology, we predicted the binding sites of PLD with mitochondrial autophagy protein. Gene expression levels of autophagy-related proteins were measured to determine the impact of PLD on mitochondrial autophagy. Additionally, the study examined whether the mitochondrial autophagy agonists rapamycin (RAPA) could modulate the upregulation of inflammasome-related factors NLRP3 and Caspase-1 in LPS-induced BEAS-2B cells. This was done to evaluate the regulator mechanisms of PLD in pulmonary inflammatory injury. Our findings suggest that PLD’s mechanism of action involves the regulation of mitochondrial autophagy, which in turn modulates inflammatory responses.

Analysis of the Spatholobus suberectus full-length transcriptome identified an R2R3-MYB transcription factor-encoding gene SsMYB158 that regulates flavonoid biosynthesis

Spatholobus suberectus Dunn (Leguminosae) has been used for medicinal purposes for a long period. Flavonoids are the major bioactive components of S. suberectus. However, there is still limited knowledge of the exact method via which transcription factors (TFs) regulate flavonoid biosynthesis. The full-length transcriptome of S. suberectus was analyzed using SMRT sequencing; 61,548 transcripts were identified, including 12,311 new gene loci, 53,336 novel transcripts, 44,636 simple sequence repeats, 36,414 complete coding sequences, 871 long non-coding RNAs and 6781 TFs. The SsMYB158 TF, which is associated with flavonoid biosynthesis, belongs to the R2R3-MYB class and is localized subcellularly to the nucleus. The overexpression of SsMYB158 in Nicotiana benthamiana and the transient overexpression of SsMYB158 in S. suberectus resulted in a substantial enhancement in both flavonoids and catechin levels. In addition, there was a remarkable upregulation in the expression of essential enzyme-coding genes associated with the flavonoid biosynthesis pathways. Our study revealed SsMYB158 as a critical regulator of flavonoid biosynthesis in S. suberectus and laying the foundation for its molecular breeding.

Integrative analysis of the transcriptome and metabolome provides insights into polysaccharide accumulation in Polygonatum odoratum (Mill.) Druce rhizome.

Polygonatum odoratum (Mill.) Druce is a traditional Chinese herb that is widely cultivated in China. Polysaccharides are the major bioactive components in rhizome of P. odoratum and have many important biological functions. To better understand the regulatory mechanisms of polysaccharide accumulation in P. odoratum rhizomes, the rhizomes of two P. odoratum cultivars 'Y10' and 'Y11' with distinct differences in polysaccharide content were used for transcriptome and metabolome analyses, and the differentially expressed genes (DEGs) and differentially accumulated metabolites (DAMs) were identified. A total of 14,194 differentially expressed genes (DEGs) were identified, of which 6,689 DEGs were down-regulated in 'Y10' compared with those in 'Y11'. KEGG enrichment analysis of the down-regulated DEGs revealed a significant enrichment of 'starch and sucrose metabolism', and 'amino sugar and nucleotide sugar metabolism'. Meanwhile, 80 differentially accumulated metabolites (DAMs) were detected, of which 52 were significantly up-regulated in 'Y11' compared to those in 'Y10'. The up-regulated DAMs were significantly enriched in 'tropane, piperidine and pyridine alkaloid biosynthesis', 'pentose phosphate pathway' and 'ABC transporters'. The integrated metabolomic and transcriptomic analysis have revealed that four DAMs, glucose, beta-D-fructose 6-phosphate, maltose and 3-beta-D-galactosyl-sn-glycerol were significantly enriched for polysaccharide accumulation, which may be regulated by 17 DEGs, including UTP-glucose-1-phosphate uridylyltransferase (UGP2), hexokinase (HK), sucrose synthase (SUS), and UDP-glucose 6-dehydrogenase (UGDH). Furthermore, 8 DEGs (sacA, HK, scrK, GPI) were identified as candidate genes for the accumulation of glucose and beta-D-fructose 6-phosphate in the proposed polysaccharide biosynthetic pathways, and these two metabolites were significantly associated with the expression levels of 13 transcription factors including C3H, FAR1, bHLH and ERF. This study provided comprehensive information on polysaccharide accumulation and laid the foundation for elucidating the molecular mechanisms of medicinal quality formation in P. odoratum rhizomes.

Comparisons of pharmacokinetics and tissue distribution of six major bioactive components of the herbal pair Alpinia officinarum-Cyperus rotundus in normal and primary dysmenorrhea rats

The Liangfu formula, as described in 'Liangfang Jiye', is well-known for its efficacy in treating stomach pain, abdominal pain, and dysmenorrhea. This research aimed to investigate the pharmacokinetics and tissue distribution of 5-hydroxy-7-(4-hydroxy-3-methoxyphenyl)-1-phenyl-3-heptanone (DPHA), Galangin, Kaempferide, 5-Hydroxy-1,7-diphenyl-3-heptanone (DPHC), α-Cyperone, and Nootkatone in vivo using an LC-MS/MS method. The method successfully separated the six active components and internal standards (Chrysin and Yakuchinone-A) on an XB-C18 column with a mobile phase of 0.2 ‰ formic acid water-acetonitrile. It demonstrated good linearity with a correlation coefficient (r2) ≥ 0.9911 and a lower limit of quantification (LLOQ) of 5–80 ng/mL for the different components. Precision, accuracy, matrix effects, and recovery rates were within acceptable ranges. Pharmacokinetic analysis revealed significant differences in parameters between primary dysmenorrhea (PD) and normal rats (especially AUC, Tmax, and CLz/F). Tissue distribution showed that the six active components of the herbal pair Alpinia officinarum Hance-Cyperus rotundus L. (HPAC) extract was primarily distributed in the liver, lung, and kidney. This study offers valuable insights into the potential mechanisms of action and drug development for treating PD.

Sesamol Alleviates Sarcopenia via Activating AKT/mTOR/FoxO1 Signal Pathway in Aged Obese Mice.

Sesamol is a major bioactive component extracted from sesame seeds and has various medicinal properties. However, the effects of sesamol on sarcopenia associated with aging and obesity remains unclear. Therefore, the protective effects and underlying mechanisms of sesamol on sarcopenia was evaluated in aged and obese C57BL/6J male mouse models fed a high fat diet and C2C12 myotubes co-treated with D-gal and PA in this study. Our in vivo data showed that sesamol activated AKT/mTOR/FoxO1 signal pathway, and then upregulated p-p70S6K and p-4EBP1 to promote myoprotein synthesis, and downregulated Atrogin-1 and MuRF1 to inhibit myoprotein degradation, thus ameliorating sarcopenia related to aging and obesity. Furthermore, our in vitro results confirmed the protective effect and aforementioned mechanisms of sesamol on sarcopenia. Collectively, sesamol could alleviate sarcopenia associated with aging and obesity via activating the AKT/mTOR/FoxO1 signal pathway. Our findings highlight the therapeutic potentials of sesamol for aging and obesity-related metabolic muscular complications.

Mycobiota contaminating some market cake samples with reference to their toxin and enzyme

Fungi can spoil the majority of baked products. Spoilage of cake during storage is commonly associated with fungi. Therefore, this study aimed to assess the quality of different types of cakes sold in the market. The most predominant fungal genera in the tested cake samples (14 samples) were Aspergillus spp., and Penicillium spp. On Potato Dextrose Agar (PDA), the medium fungal total count was 43.3 colonies /g. Aspergillus was the most dominant genus and was isolated from six samples of cake. Aspergillus was represented by 3 species namely, A. flavus, A. niger, and A. nidulans, represented by 13.32, 19.99, and 3.33 colonies /g respectively. On Malt Extract Agar (MEA) Medium, the fungal total count was 123.24 colonies / g. Aspergillus was the most dominant isolated genus from 11 samples of cake and was represented by 5 species, namely, A. flavus, A. niger, A. ochraceous, A. terreus, and A. versicolor (26. 65, 63.29, 3.33, 6.66, and 3.33 colonies / g , respectively). Twenty-four isolates (88.88 %) of the total tested twenty-seven filamentous fungi showed positive results for amylase production. Ten isolates (37.03%) of the total tested filamentous fungi showed positive results for lipase production, and finally eleven isolates (40.74 %) of the total fungal isolates showed positive results for protease production. Aflatoxins B1, B2, G1, G2, and ochratoxin A were not detected in fourteen collected samples of cake. In this study, clove oil was the best choice overpeppermint oil and olive oil for preventing mold development when natural agents were compared. It might be due to the presence of a varietyof bioactive chemical compounds in clove oil, whose major bioactive component is eugenol, which acts as an antifungal reagent. Therefore, freshly baked cake should be consumed within afew days to avoid individuals experiencing foodborne illnesses.

Novel Approaches for the Analysis and Isolation of Benzylisoquinoline Alkaloids in Chelidonium majus

AbstractBenzylisoquinoline alkaloids are the major bioactive components in Chelidonium majus, a plant that has a long usage history for the treatment of gastrointestinal ailments in European and Asian phytomedicine. This study reports on the development and application of a supercritical fluid chromatography technique for the simultaneous qualitative and quantitative determination of seven benzylisoquinoline alkaloids in under six minutes using a Viridis BEH 2-EP column and a modifier comprising methanol with 30% acetonitrile and 20 mM ammonium formate. The method was fully validated according to ICH guidelines showing, e.g., excellent linearity (≥ 0.9997) and maximum deviations for intraday and inter-day precision of 2.99 and 2.76%, respectively. The new supercritical fluid chromatography assay was not only employed for the analysis of several C. majus samples but was also used for the subsequent development of a fast centrifugal partition chromatography technique, whereby five benzylisoquinoline alkaloids could be isolated within approximately 2.5 h, with only two of them, protopine and chelidonine, requiring an additional purification step. To achieve this, a solvent system composed of chloroform/methanol/0.3 M hydrochloric acid was used in descending mode. By injecting 500 mg of crude extract, stylopine (1.93 mg), sanguinarine (0.57 mg), chelidonine (1.29 mg), protopine (1.95 mg), and coptisine (7.13 mg) could be obtained. The purity of compounds was confirmed by supercritical fluid chromatography and MS.