Oral tranexamic acid treats papulopustular rosacea by improving the skin barrier.

BACKGROUND: Papulopustular rosacea (PPR) is a chronic inflammatory disease with a significant impact on facial aesthetics. An impaired skin barrier is an important factor in the development and exacerbation of PPR. Tranexamic acid (TXA) has immune regulatory and anti-inflammatory effects, inhibits angiogenesis and endothelial hyperplasia, and promotes skin barrier repair. AIMS: We investigated the efficacy and safety of oral TXA for PPR treatment. PATIENTS/METHODS: In total, 70 patients were randomly assigned to receive traditional therapy plus oral TXA or traditional therapy alone for 8 weeks, with a 4-week follow-up period. The subjective improvement in rosacea was assessed using the clinical erythema assessment (CEA), investigator's global assessment (IGA), patient self-assessment (PSA) score, rosacea-specific quality of life (RQoL) score, and global aesthetic improvement score (GAIS). An objective improvement in rosacea was assessed using skin hydration, trans-epidermal water loss (TEWL), clinical photography, and an eight spectrum facial imager. RESULTS: CEA/IGA/PSA, dryness, and RQoL scores were significantly lower and GAIS was higher in the TXA group than in the traditional therapy group. Furthermore, oral TXA significantly improved skin barrier function, increased skin hydration, and decreased TEWL, with no significant side effects. Notably, we observed better outcomes and a greater improvement in skin barrier function with TXA treatment in patients with dry-type rosacea than in patients with oily skin. CONCLUSIONS: The addition of oral TXA to traditional therapy can lead to rapid and effective improvements in PPR, which may be attributed to improvements in skin barrier function.

Degradation kinetics of vitamins in different enteral feeding formulas during storage at different temperatures.

Vitamin degradation may be affected differently by various food matrices. In this study, the kinetics of vitamin A, B1, and C degradation were directly compared in two types of enteral feeding formulas (EFFs) with different energy densities over a nine-month storage period at 4, 25, and 30 °C. The content of vitamins A, B1, and C was measured in the initial and stored formulas. The results justified the finding that the content of these vitamins was gradually decreased with storage time or temperature increases during the period. At each temperature during storage, the degradation of vitamins A, B1, and C followed first-order kinetics, and the rate constants calculated indicated the degradation of vitamins was temperature-dependent. The EFF-B exhibited a higher activation energy for vitamin degradation than that in the EFF-A, and the activation energy indicated an inverse relationship with the fat content of EFFs. The outcomes might provide a reference for the development and application of EEFs.

Discrimination of untreated and sodium sulphite treated bean sprouts by Fourier transform infrared spectroscopy and chemometrics.

Sprouts of black beans (Phaseolus vulgaris L.), soybeans (Glycine max L.) and mung beans (Vigna radiata L.) are widely consumed foods containing abundant nutrients with biological activities. They are commonly treated with sulphites for the preservation and extension of shelf-life. However, our previous investigation found that immersing the bean sprouts in sulphite might convert the active components into sulphur-containing derivatives, which can affect both the quality and safety of the sprouts. This study explores the use of FTIR in conjunction with chemometric techniques to differentiate between non-immersed (NI) and sodium sulphite immersed (SI) black bean, soybean and mung bean sprouts. A total of 168 batches of raw spectra were obtained from NI and SI-bean sprouts using FTIR spectroscopy. Four pre-processing techniques, three modelling assessment techniques and four model evaluation indices were examined for differences in performance. The results show that the multiplicative scatter correction is the most effective pre-processing method. Among the models, the accuracy rate of the three models was as follows: radial basis function neural network (95%) > convolutional neural network (91%) > random forest (82%). The overall findings indicate that FTIR spectroscopy, in conjunction with appropriate chemometric approaches, has a high potential for rapidly determining the difference between NI and SI-bean sprouts.

Preparation and characterization of vitamin A microcapsules nutrient fortified salt.

Vitamin A, also known as retinol, is a fat-soluble vitamin that plays crucial role in various physiological functions In vivo. However, factors such as light, oxygen, and others may impact the stability of VA. To enhance its stability. This study microencapsulated VA, Gelatin, carboxymethyl cellulose, and salt were mixed in a ratio of 5:1:0.1 as the shell material. Additionally, 12% TG and 3.5% sucrose ester were added with core-shell ratio of 1:8. The experimental results indicated that VA microcapsules exhibited an encapsulation efficiency of 81.12%, after 9 weeks of storage this rate decreased to 75.38%, and the encapsulated VA oil did not exhibit extravasation. The addition of an appropriate amount of salt to the shell material enhanced the mechanical properties of the shell material, compared to the shell material without added salt, the leakage of VA in the salt-added sample decreased by 5.8% for 30 min and 14.5% for 60 min. In vitro release experiments showed that after 3 h of incubation in simulated gastric fluid, the microcapsules had an 18.52% release rate. In simulated intestinal fluid, this increased to 66.58%, indicating strong enteric solubility. Supplementary Information: The online version contains supplementary material available at 10.1007/s13197-024-05962-w.

Antitumor Activity and Mechanism of Terpenoids in Seaweeds Based on Literature Review and Network Pharmacology.

Seaweeds are a treasure trove of natural secondary metabolites. Terpenoids extracted from seaweeds are shown to possess a variety of antitumor cellular activities. However, due to the complex and diverse structures of terpenoids, their therapeutic targets and complex mechanisms of action have not been clarified. The present study summarises the research on terpenoids from seaweeds in oncological diseases over the last 20 years. Terpenoids show different degrees of inhibitory effects on different types of tumor cells, suggesting that terpenoids in seaweeds may have potential antitumor disease potential. Terpenoids with potential antitumor activity and their mechanism of action are investigated using network pharmacology. A total of 125 terpenoids and 286 targets are obtained. Proto-oncogene tyrosine-protein kinase Src(SRC), Signal transducer and activator of transcription 3 (STAT3), Mitogen-activated protein kinase (MAPK3, MAPK1), Heat shock protein HSP 90-alpha (HSP90AA1), Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (PIK3CA), and RAC-alpha serine/threonine-protein kinase (AKT1) are defined as core targets. According to GO function and Kyoto encyclopedia of genes and genomes(KEGG) enrichment analysis, terpenoids may affect the Phoshatidylinositol 3'-kinase (PI3K)-Akt signaling pathway, Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor resistance, Prostate cancer, MAPK signaling pathway, and Proteoglycans in cancer. In addition, the molecular docking results show that the selected terpenoids are all able to bind strongly to the active protein. Terpenoids may slow down the progression of cancer by controlling apoptosis, proliferation, and protein and enzyme binding.

Biosynthesis of resveratrol by an endophytic Priestia megaterium PH3 via the phenylpropane pathway.

Resveratrol (RES) is a secondary metabolite synthesized by plants in response to environmental stress and pathogen infection, which is of great significance for the industrial production of RES by fermentation culture. In this study, we aimed to explore the biosynthesis pathway of RES and its key enzymes in the Priestia megaterium PH3, which was isolated and screened from peanut fruit. Through Liquid Chromatography-Mass Spectrometry (LC-MS) analysis, we quantified the RES content and distribution in the culture medium and determined that Priestia megaterium PH3 mainly secreted RES extracellularly. Furthermore, the highest production of RES was observed in YPD, yielding an impressive 127.46 ± 6.11 µg/L. By optimizing the fermentation conditions, we achieved a remarkable RES yield of 946.82 ± 24.74 µg/L within just 2 days, which represents the highest reported yield for a natural isolate produced in such a short time frame. Our investigation revealed that the phenylpropane pathway is responsible for RES synthesis in this bacterium, with cinnamate 4-hydroxylase (C4H) identified as the main rate-limiting enzyme. Overall, our findings highlight the robust RES production capabilities of Priestia megaterium PH3, offering novel insights and potential applications for bacterial fermentation in RES production. KEY POINTS: • RES synthesized by the bacterium was confirmed through the phenylpropane pathway. • The key rate-limiting enzyme for biosynthesis-RES is C4H. • RES reached 946.82 ± 24.74 µg/L after fermentation for 2 days.

Fabric Fiber as a Biofilm Carrier for Halomonas sp. H09 Mixed with Lactobacillus rhamnosus GG.

Biofilm bacteria have stronger resistance to the adverse external environment compared to planktonic bacteria, and biofilms of non-pathogenic bacteria have strong potential for applications in food. In this experiment, Halomonas sp. H09 and Lactobacillus rhamnosus GG, which have film-forming ability in monoculture and better film-forming ability in mixed culture than the two strains alone, were selected as the target strains for mixed culture. According to SEM observation and bacterial dry weight measurement, the target strain formed a dense biofilm on a 0.1 g/L chitosan-modified cellulose III carrier. Furthermore, the presence of extracellular polymeric substances in biofilms was verified by EDS and FTIR. The results showed that 0.1 g/L chitosan-modified cellulose III was an ideal carrier material for immobilization of Halomonas sp. H09 with Lactobacillus rhamnosus GG biofilm. This research provided a basis for the selection of non-pathogenic mixed-bacteria biofilm carriers.

Preparation and functional characteristics of protein from Ginkgo endophytic Pseudomonas R6 and Ginkgo seed.

Ginkgo seed protein (GSP) has excellent processing characteristics and antioxidant properties. In this study, Gingko endophytic protein (GEP) was synthesized by Ginkgo endophytic Pseudomonas R6. SDS-PAGE analysis indicated that the molecular weights of GSP and GEP were mainly distributed at 17 KDa and 48 KDa, respectively. FTIR showed that GEP and GSP exhibited characteristic absorption in the amide I, II, and III bands, and absorption in amide A and B indicated the presence of hydrogen bonding. HPLC analysis showed that both proteins had 17 amino acids, but their relative abundance was different, with GSP having the highest Ser content (74.713 mg/g) and GEP having the highest Val content (35.905 mg/g). Stomata were observed on the surface of both proteins by SEM, and there were lamellar and some spherical structures on GEP, while the opposite was observed on GSP. GEP had superior solubility, OHC, FC and EC, while GSP showed good WHC. Both proteins exhibited antioxidant activities, with GSP exhibiting stronger hydroxyl radical scavenging ability than GEP, with IC50 of 0.46 mg/mL and 1.54 mg/mL, respectively. This work demonstrates the antioxidant potential of GEP as an alternative to GSP in the food industry.

JAK1 inhibitor abrocitinib for the treatment of steroid-induced rosacea: case series.

Background: Steroid-induced rosacea is a severe withdrawal reaction which can occur after the frequent and excessive topical use of steroids on the face. The Janus kinase (JAK)-signal transducers and activators of transcription signaling pathway is involved in many biological processes and may play a role in the development of steroid-induced rosacea. Objective: To observe the efficacy and safety of the JAK1 inhibitor abrocitinib in the treatment of steroid-induced rosacea. Methods: Four Chinese female patients were treated with orally-administered abrocitinib, a selective JAK1 inhibitor with a good safety profile, for steroid-induced rosacea. Results: Abrocitinib treatment resulted in improved skin condition and lowered Dermatology Life Quality Index scores in each of the four patients. No discomfort was reported and no adverse effects were observed. Conclusion: The JAK1 inhibitor abrocitinib is a promising potential treatment for steroid-induced rosacea.

Investigation of the Potential Phlorotannins and Mechanism of Six Brown Algae in Treating Type II Diabetes Mellitus Based on Biological Activity, UPLC-QE-MS/MS, and Network Pharmacology.

Type 2 diabetes mellitus (T2DM) has developed into an important health concern worldwide. The discovery of phlorotannins and their efficacy in the treatment of T2DM has become a hotspot for research in various fields. In this study, the potential phlorotannins and mechanism of six brown algae against T2DM were in-depth investigated using biological activity assays, LC-MS, and network pharmacology. First, the ethyl acetate fraction (EA frac.) showed high polyphenolic content and possessed significantly antioxidant and enzyme inhibitory abilities. Further, a total of fifty-nine peaks were obtained from six EA fracs. via UPLC-QE-MS/MS analysis, and fifteen of them were identified as phlorotannins and their isomers or derivatives. In detail, the chemical structures of six phlorotannins were inferred as dibenzodioxine-1,3,6,8-tetraol, bifuhalol, dioxinodehydroeckol, eckol, fucofurodiphlorethol, and fucotriphlorethol; three phlorotannin isomers were deduced to be fucophlorethol, trifucol, triphlorethol A, or triphlorethol B; and the phlorotannin derivative of m/z 263 was determined to be dibenzodioxine-1,2,3,6,8-pentanol or dibenzodioxine-1,2,4,5,7-pentanol. Moreover, 43 T2DM-related targets acted on by these chemicals were identified, and the function of phlorotannin to prevent and treat T2DM was elucidated in a holistic way based on the established compound-target-disease network, and GO function and KEGG pathway enrichment analysis.

A study of the efficacy and safety of plaque psoriasis treatment by TNF-α and IL-17A inhibitor biologics in patients who received the inactivated SARS-CoV-2 vaccine.

BACKGROUND: Vaccination is an important method for the prevention of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) transmission. There is currently a lack of real-world clinical data regarding the safety and efficacy of coronavirus disease 2019 (COVID-19) vaccines with respect to plaque psoriasis treatment involving tumor necrosis factor-α (TNF-α) and interleukin-17A (IL-17A) inhibitors. METHODS: We longitudinally analyzed 152 patients with plaque psoriasis, 86 of whom received two doses of inactivated COVID-19 vaccine (either BBIBP-CorV or CoronaVac). Comparisons were made between patients undergoing treatment with biologics (TNF- α inhibitors or IL-17A inhibitors) or acitretin. Routine blood tests were used to assess safety; the psoriasis area and severity index (PASI) and dermatology life quality index (DLQI) were used to assess efficacy. RESULTS: After inactivated COVID-19 vaccination, biologics retained considerable advantages in terms of improving skin lesions (measured by PASI) and quality of life (measured by DLQI), compared with conventional treatment (p < 0.05 and p < 0.01, respectively). Routine blood tests and hepatorenal function analyses suggested that inactivated SARS-CoV-2 vaccines did not alter the safety of biologics treatment (p > 0.05). CONCLUSIONS: Inactivated SARS-CoV-2 vaccines do not have significant impacts on the safety and efficacy of biologics (TNF-α inhibitors or IL-17A inhibitors) in patients with moderate to severe plaque psoriasis.

Characterization of lipopeptide produced by Bacillus altitudinis Q7 and inhibitory effect on Alternaria alternata.

This study identified the antifungal metabolites produced by Bacillus altitudinis Q7 against Alternaria alternata and investigated the antifungal activity and antifungal action. Lipopeptide, the important secondary metabolites were identified by Fourier transform infrared (FTIR) and liquid chromatography-mass spectrometry as lichenysin. The antifungal activity of lipopeptide on A. alternata was determined by microdilution technique, and its minimum inhibitory concentration was 1.2 mg/ml. Stability test showed that lipopeptide had excellent temperature and pH resistance. To investigate whether lichenysin acted on the cell membrane and changed its permeability, the ultra-violet absorption of protein and nucleic acid were measured using a colorimetric method. The antifungal metabolites produced by B. altitudinis Q7 was lichenysin, which showed stable antifungal activity in the extreme environments. Lichenysin could inhibit A. alternata by altering the permeability of cell membrane, leading to the outflow of proteins and nucleic acids from the cytoplasm. This research suggests the lipopeptide from B. altitudinis Q7 is a potential biological control agent against A. alternata.

Isolation and purification of 12 flavonoid glycosides from Ginkgo biloba extract using sephadex LH-20 and preparative high-performance liquid chromatography.

An efficient and rapid preparative method for the separation and purification of flavonoid glycosides from the Ginkgo biloba extract (GBE) was developed by sephadex LH-20 and preparative high-performance liquid chromatography (HPLC). 40 g GBE of 24% flavonoids were loaded onto the sephadex LH-20 column and five fractions (1.15, 2.57, 1.32, 4.45, and 3.31 g) at flavonoid content of 72.3, 54.2, 63.5, 51.2, and 59.2% were produced. Ultimately, 12 flavonoid glycosides that are at least purities of 97.7% were obtained from 100 mg of each fraction by preparative HPLC. The fraction A, B, and D each contained two flavonoids, yielded 35, 30, 23, 20, 25, and 25 mg, respectively. The fraction C and E each contained three flavonoids, produced 20, 13, 15, 18, 15, and 20 mg, respectively. The chemical structures of the purified compounds were identified by nuclear magnetic resonance (NMR) and electrospray ionization mass spectrometry (ESI/MS).

Systems pharmacology-based drug discovery and active mechanism of phlorotannins for type 2 diabetes mellitus by integrating network pharmacology and experimental evaluation.

Phlorotannins, polyphenolic compounds that exist only in brown algae, have an effect on T2DM. However, the structure of phlorotannins is complex and diverse, and the complex role of therapeutic targets and active compounds has not been revealed. In this study, the potential targets and pharmacological effects of phlorotannins in the treatment of T2DM were identified based on network pharmacology and enzyme activity inhibition experiment. In total, 15 phlorotannins and 53 associated targets were yielded. Among them, SRC, ESR1, AKT1, HSP90AB1, and AR were defined as core targets. 527 GO biological processes items and 101 KEGG pathways were obtained, including EGFR tyrosine kinase inhibitor resistance, thyroid hormone signaling pathway, AGE-RAGE signaling pathway in diabetic complications, and VEGF signaling pathway. Phlorotannins could enable resistance against T2DM by inflammatory, survival, gene transcription, proliferation, apoptosis, and atherosclerosis. Finally, α-glucosidase inhibition assay and molecular docking proved the effect of selected phlorotannins on T2DM. PRACTICAL APPLICATIONS: Phlorotannins are a kind of polyphenol compounds that only exists in brown algae. Its structure is polymerized by aromatic precursors phloroglucinol (1,3,5-trihydroxybenzene). They have aroused great interest due to their excellent and valuable biological activities. However, the structure of phlorotannins is complex and diverse, and the complex role of therapeutic targets and active compounds has not been revealed. In this study, the potential targets and pharmacological effects of phlorotannins in the treatment of T2DM were determined basis on network pharmacology and enzyme activity inhibition experiment. In conclusion, the results showed the value of phlorotannins treating on T2DM. Moreover, this study has great significance for improving the medicinal value of phlorotannins and screening natural products for the treatment of T2DM.

Systems pharmacology-based drug discovery and active mechanism of natural products for coronavirus pneumonia (COVID-19): An example using flavonoids.

BACKGROUND: Recently, the value of natural products has been extensively considered because these resources can potentially be applied to prevent and treat coronavirus pneumonia 2019 (COVID-19). However, the discovery of nature drugs is problematic because of their complex composition and active mechanisms. METHODS: This comprehensive study was performed on flavonoids, which are compounds with anti-inflammatory and antiviral effects, to show drug discovery and active mechanism from natural products in the treatment of COVID-19 via a systems pharmacological model. First, a chemical library of 255 potential flavonoids was constructed. Second, the pharmacodynamic basis and mechanism of action between flavonoids and COVID-19 were explored by constructing a compound-target and target-disease network, targets protein-protein interaction (PPI), MCODE analysis, gene ontology (GO), and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment. RESULTS: In total, 105 active flavonoid components were identified, of which 6 were major candidate compounds (quercetin, epigallocatechin-3-gallate (EGCG), luteolin, fisetin, wogonin, and licochalcone A). 152 associated targets were yielded based on network construction, and 7 family proteins (PTGS, GSK3ß, ABC, NOS, EGFR, and IL) were included as central hub targets. Moreover, 528 GO items and 178 KEGG pathways were selected through enrichment of target functions. Lastly, molecular docking demonstrated good stability of the combination of selected flavonoids with 3CL Pro and ACEⅡ. CONCLUSION: Natural flavonoids could enable resistance against COVID-19 by regulating inflammatory, antiviral, and immune responses, and repairing tissue injury. This study has scientific significance for the selective utilization of natural products, medicinal value enhancement of flavonoids, and drug screening for the treatment of COVID-19 induced by SARS-COV-2.

Characterization and functional properties of conjugates of rice protein with exopolysaccharides from Arthrobacter ps-5 by Maillard reaction.

The study examined the potential nutritive value of rice protein (RP) through Maillard reaction. Structures and properties of synthetic conjugates of RP and exopolysaccharide (EPS) from Arthrobacter ps-5 were investigated systematically. Fluorescence characteristics and high molecular weight compounds appeared in Maillard reaction products (MRPs). Moreover, EPS or its degradation products in the form of covalent bond cross-linked with RP were identified, where -NH2 disappeared and C=O, C=N and C-N increased. Determination of free -SH residues suggested mutual conversion between disulfide bonds and sulfhydryl groups occurred during Maillard reaction. HPLC analysis identified conjugates with different molecular weight, where melanoprotein was formed by covalent bonds. As RP conjugated with EPS, the molecules spread out and changed the spatial structure. Functional properties of MRPs, including solubility, foaming activity, emulsifying ability and resistance to oxidation, were greatly improved. The study has discovered an efficient method for increasing the application value of plant protein.

Biosynthesis of selenoproteins by Saccharomyces cerevisiae and characterization of its antioxidant activities.

The study investigated biosynthesis of selenoproteins by Saccharomyces. cerevisiae using inorganic selenium. Selenium supplement via two stages was carried out during fermentation and the physicochemical characteristics of selenoproteins and its antioxidant activities were examined through in vitro assessment procedures. After fermentation, dry cells weight (7.47 g/L) and selenium content (3079.60 µg/kg) in the yeast were achieved when fermentation time points at the 6th hour and the 9th hour were chosen to supplement 30% and 70% of 30 µg/mL Na2SeO3 respectively. A maximal yield of selenium content in selenoproteins reached 1013.07 µg/g under optimized culture conditions and was 133-fold higher than the control. One new band with molecular weight of 26.76 KDa appeared in conjugated selenoproteins of sodium dodecyl sulphate-polyacrylamide gel electrophoresis. Surface structure of selenoproteins and the control was different by Scanning electron microscopy images. Infrared spectrometry analysis demonstrated that groups of HSe, SeO and C-Se-O involved in selenoproteins were important pieces of evidence showing presence of Se embedded in the protein molecule. Selenoproteins showed strong antioxidant activities on DPPH·, OH and ·O2-, which was much higher than the control proteins. Therefore, the study provided an efficient selenium-enriched culture method of inorganic selenite to organic selenium and basis for selenoproteins applications.

Biosynthesis of selenium rich exopolysaccharide (Se-EPS) by Pseudomonas PT-8 and characterization of its antioxidant activities.

Biosynthesis of organo-selenium is achieved by submerged fermentation of selenium-tolerant Pseudomonas PT-8. The end product of metabolic process is selenium-bearing exopolysaccharide (Se-EPS), which contains a higher content of uronic acid than the exopolysaccharide (EPS) by the strain without selenium in the culture medium. Selenium content in Se-EPS reached a maximum yield of 256.7 mg/kg when using an optimized culture condition. Crude Se-EPS was purified into two fractions-a pH neutral Se-EPS-1 and an acidic Se-EPS-2. Structure and chemical composition of Se-EPS-2 were investigated by chromatographic analyses. Results showed that Se-EPS-2 was a homogenous polysaccharide with molecular weight of 7.3 kDa, consisting of monosaccharides, rhamnose, arabinose, xylose, mannose, glucose and galactose with a molar ratio of 19.58:19.28:5.97:18.99:23.70:12.48, respectively. Compared to the EPS, the content of rhamnose in Se-EPS increased and molecular weight decreased. The Se-EPS had strong scavenging actions on DPPH•, •OH and •O2(-), which is much higher than the EPS.