Anti-inflammatory Ingredients Research Articles

Solubility of dapsone in deep eutectic solvents: Experimental analysis, molecular insights and machine learning predictions.

Dapsone (DAP) is an anti-inflammatory and antimicrobial active pharmaceutical ingredient used to treat, e.g., AIDS-related diseases. However, low solubility is a feature hampering its efficient use. First, deep eutectic solvents (DES) were used as solubilizing agents for DAP as an alternative to traditional solvents. Second, intermolecular interactions in the systems were described and quantified. Finally, the solubility prediction model, previously created using the machine learning protocol, was extended and improved using new data obtained for eutectic systems. New DES were created by blending choline chloride (ChCl) with 6 selected polyols. The solubility of DAP in these solvents was measured spectrophotometrically. The impact of water dilution on the solubility curve was investigated. Experimental research was enriched with theoretical interpretations of intermolecular interactions, identifying the most probable pairs in the systems. Dapsone self-association and its ability to interact with components of the analyzed systems were considered. Thermodynamic characteristics of pairs were utilized as molecular descriptors in the machine learning process, predicting solubility in both traditional organic solvents and the newly designed DES. The newly formulated solvents demonstrated significantly higher efficiency compared to traditional organic solvents, and a small addition of water increased solubility, indicating its role as a co-solvent. The interpretation of the mechanism of DAP solubility highlighted the competitive nature of self-association and pair formation. Thermodynamic parameters characterizing affinity were instrumental in developing an efficient model for theoretical screening across diverse solvent classes. The study emphasized the necessity of retraining models when introducing new experimental data, as exemplified by enriching the model with data from DES. The research showcased the efficacy of developing new DES for enhancing solubility and creating environmentally and pharmaceutically viable systems, using DAP as an example. Molecular interactions proved valuable in understanding solubility mechanisms and formulating predictive models through machine learning processes.

Antioxidant and Anti-Inflammatory Activities of Lindera glauca Extracts

Introduction: The current study investigated the antioxidant and anti-inflammatory effects of ethanol extracts from Lindera glauca twig (LGT) and leaf/stem (LGLS). Methods: The antioxidant activities were measured by total content of polyphenol and flavonoid, DPPH radical scavenging, and ABTS+ radical scavenging activity. To evaluate the anti-inflammatory effect in the LPS-induced RAW 264.7 cells, protein and mRNA expression of major inflammatory factors were analyzed using Western blot analysis and RT-PCR. Results: The total polyphenol content of LGT and LGLS was 88.45 ± 11.74 and 115.75 ± 7.87 GA mg/g, respectively. The total flavonoid content was 66 ± 2.89 and 74.33 ± 2.89 QE mg/g. Both LGT and LGLS showed high DPPH and ABTS+ radical scavenging activities. Neither LGT nor LGLS was cytotoxic to RAW 264.7 cells. The anti-inflammatory activities were measured by LPS-induced RAW 264.7 cells. LGT and LGLS showed inhibition of the LPS-induced production of nitric oxide (NO), inducible NO synthase, cyclooxygenase-2 at the protein and mRNA levels, as determined by Western blotting and RT-PCR, respectively. In addition, the release of tumor necrosis factor-α and interleukin-6 mRNA expression levels of these cytokines was reduced by LGT and LGLS. Conclusion: These results suggest that LGT and LGLS extracts have potential for use as a functional antioxidant and anti-inflammatory ingredient in cosmetic industry.

Integrative analysis of the metabolome and transcriptome reveals the mechanism of polyphenol biosynthesis in Taraxacum mongolicum.

Dandelion is widely used in clinical practice due to its beneficial effects. Polyphenolic compounds are considered the main anti-inflammatory active ingredient of dandelion, but the gene expression patterns of polyphenolic compounds in different dandelion tissues are still unclear. In this study, we combined a nontargeted metabolome, PacBio Iso-seq transcriptome, and Illumina RNA-seq transcriptome to investigate the relationship between polyphenols and gene expression in roots, flowers, and leaves of flowering dandelion plants. Eighty-eight flavonoids and twenty-five phenolic acids were identified, and 64 candidate genes involved in flavonoid biosynthesis and 63 candidate genes involved in chicoric acid biosynthesis were identified. Most flavonoid and chicoric acid-related genes demonstrated the highest content in flowers. RNA-seq analysis revealed that genes involved in polyphenol biosynthesis pathways, such as CHS, CHI, F3H, F3'H, FLS, HQT, and CAS, which are crucial for the accumulation of flavonoids and chicoric acid, were upregulated in flowers. The combination of transcriptomic and metabolomic data can help us better understand the biosynthetic pathways of polyphenols in dandelion. These results provide abundant genetic resources for further studying the regulatory mechanism of dandelion polyphenol biosynthesis.

Electrospun dressings with a dual release functionality of two anti-inflammatory active ingredients

Electrospun dressings with a dual release functionality of two anti-inflammatory active ingredients

Characteristic and Formulation Turmeric Extract Nanoemulsion as Alternative Moisturizer in Atopic Dermatitis

Currently, many moisturizers are developed with anti-inflammatory ingredients intended for mild and moderate atopic dermatitis (AD). One of the ingredients that can be developed is turmeric (Curcuma longa), which has potent anti-inflammatory activity. However, turmeric topical treatments require nano formulas due to their limited skin absorption. This study aims to obtain the optimal formulation of turmeric extract nanoemulsion as an alternative moisturizer for AD. The nanoemulsions are made by a self-nanoemulsifying drug delivery system (SNEDDS) using a simplex lattice design (SLD). Based on the solubility test, the oil components were sunflower oil, tween 80 as a surfactant, and polyethylene glycol (PEG) 400 as cosurfactant with a ratio of 1:8:1. The SNEDDS formulation was analyzed using software design expert version 10.03. The optimum SNEDDS formulation characteristic included an average droplet size of 13.37nm, an average polydispersity index (PDI) of 0.179, an average transmittance of 81.53%, and an average zeta potential of -38.57mV. Based on these results, it can be concluded that the turmeric extract formula meets the nanoemulsion criteria because the average droplet size is <200nm, the droplet distribution is relatively homogeneous as illustrated by the small average PDI, the transmittancesare above 80%, and is relatively stable with a zeta potential >±30mV.

Dipotassium glycyrrhizate and hinokitiol enhance macrophage efferocytosis by regulating recognition, uptake, and metabolism of apoptotic cells invitro.

Efferocytosis is a process whereby macrophages remove apoptotic cells, such as neutrophils, that have accumulated in tissues, which is required for resolution of inflammation. Efferocytosis is impaired in individuals with increasing age and in those with various systemic diseases. Recently, efferocytosis has been reported to be related to the pathogenesis and progression of periodontitis, and enhancement of efferocytosis, especially in the subjects with impaired efferocytosis, was suggested to lead to periodontitis prevention and care. Various anti-inflammatory ingredients are used in oral care products, but their effect on efferocytosis is unclear. Here, we aimed to identify ingredients contained in oral care products that are effective for efferocytosis regulation. The ability of dead cells to induce inflammation in human gingival fibroblast (HGF) cells were evaluated by measuring IL-6 secretion. Six ingredients in oral care products used as anti-inflammatory agents were evaluated for their effect on efferocytosis using flow cytometry. The expression of various efferocytosis-related molecules, such as MERTK and LRP1 involved in recognition, and LXRα and ABCA1 that function in metabolism, were measured in RAW264.7 cells with or without ingredient treatment. Rac1 activity, which is related to the uptake of dead cells, was measured using the G-LISA kit. Dead cells elicited IL-6 secretion in HGF cells. Among the six ingredients, GK2 and hinokitiol enhanced efferocytosis activity. GK2 and hinokitiol significantly increased the expression of MERTK and LRP1, and also enhanced LXRα and ABCA1 expression after efferocytosis. Furthermore, they increased Rac1 activity in the presence of dead cells. Among the six ingredients tested, GK2 and hinokitiol promoted efferocytosis by regulating apoptotic cell recognition, uptake, and metabolism-related molecules. Efferocytosis upregulation may be one of the mechanisms of GK2 and hinokitiol in the treatment of inflammatory diseases, such as periodontitis.

Curcumin-loaded a-lactalbumin nanoparticles neuroprotective effects against permethrine-induced neurotoxicity

Curcumin, as is well known, plays the role of an antioxidant, anti-inflammatory and neuroprotective ingredient. Permethrine is a synthetic type I pyrethroidal neurotoxic pesticide that has been involved in causing neurotoxicity in dopaminergic cells and is currently the subject of extensive study in the fight against Parkinson's disease (PD). In the current study, curcumin loaded α-lactalbumin (α-LA) nanoparticles prepared by desolvation technique were used to protect dopaminergic cell line SH-SY5Y against permethrine induced neurotoxicity. These curcumin-loaded nanoparticles, according to transmission electron microscopy, and dynamic light scattering analysis, have the diameters of 100–150 nm, respectively. The encapsulation efficiency was 60.23 % ±3.1 %.The cellular uptake of curcumin was demonstrated to be mediated by these nanoparticles by spectrofluorimetric and Confocal imaging investigations. The α-lactalbumin nanoparticles loaded with curcumin exhibited greater intracellular drug absorption, extended retention, and neuroprotection compared to their corresponding curcumin concentrations. Neuroprotective effect was established by viability experiments and ROS level measurement. Furthermore, in permethrine-induced PD-like features, a-synuclein expression rose and tyrosine hydroxylase expression fell. To further shield dopaminergic neurons from neurotoxicity, curcumin-loaded lactalbumin nanoparticles would be a powerful therapeutic delivery vehicle.

Natural Topical Treatment Contributes to a Reduction of Dry Scalp Symptoms in Children.

Dry scalp conditions affect a significant portion of the population, including children. Emerging evidence indicates the potential for improvement of atopic symptoms through altering the skin microbiome. Therefore, a topical treatment consisting of probiotic extracts, honey, turmeric, and vitamin B12 was manufactured to improve dry scalp symptomology through sustained balance of the microbiome. This interventional clinical study aims to determine the safety and efficacy of the topical treatment in reducing dry scalp symptomology in children 1-17 years old with dry scalp symptoms. Participants applied the topical dry scalp treatment 2-3 times per week for two weeks. Safety and efficacy of the topical treatment was determined through physician assessment using the validated Investigator's Global Assessment (IGA) scale and the Total Severity Scale (TSS) during pre- and post-treatment clinic visits as well as parent reports at baseline, 1-week midpoint, and 2-week exit. Use of the topical treatment was associated with reduced symptoms of itchiness, dryness, irritation, and flakiness in children. The average IGA score was 3.0 at baseline and 2.0 after treatment, corresponding to a score difference of 1.0 (p < 0.001, 95% CI: 0.7, 1.2). The TSS score difference was 1.9 (p < 0.001, 95% CI: 1.4, 2.4). The total parent-reported scalp severity score decreased from 16.6 (95% CI: 14.8, 18.4) to 12.4 (p < 0.001, 95% CI: 11.0, 13.7) at 2-week exit. Study results mirror those reported in a study conducted in adults and point to the safety and efficacy of this natural topical treatment in reducing dry scalp symptomology in children. Based on our data, the combination of probiotic extracts and other anti-inflammatory ingredients appears to improve overall scalp health and appearance, though further studies will need to be conducted to further elucidate the link between clinical improvement and a balanced scalp microbiome.

Optimal compatibility proportional screening of Trichosanthis Pericarpium - Trichosanthis Radix and its anti - Inflammatory components effect on experimental zebrafish and coughing mice

Ethnopharmacological relevanceThe herbal pair of Trichosanthis Pericarpium (TP) - Trichosanthis Radix (TR) can be seen in the famous formula “Beimu Gualou San”. It is a commonly selected combination of medicinal herbs for the treatment of cough with lung heat. Both drugs are derived from Trichosanthes kirilowii Maxim, a medicinal plant known for its ability to clear heat, resolve phlegm, produce saliva, and alleviate dryness. However, the optimal combination ratio and active ingredients of TP-TR have yet to be determined. Aim of the studyThis study aims to investigate the optimal combination ratio of TP-TR and its anti-inflammatory active ingredients in cough treatment. Materials and methodsA zebrafish (Danio rerio) inflammatory injury model and response surface method were applied in the present study to determine the appropriate proportion of TP-TR. Chemical constituents in TP-TR were identified using HPLC-ELSD and UPLC-MS/MS methods. Subsequently, a cough mouse model was created using an ammonia solution to evaluate the effectiveness of the optimal TP-TR ratio. Network pharmacology and intestinal flora sequencing were used to validate the anti-inflammatory components of TP-TR. ResultsThe herbal pair of TP - TR at the ratio of 1:2 showed an optimal anti-inflammatory effect, with a composite inflammatory factor score of 119.645 in the zebrafish experiment. TP-TR combination facilitated the dissolution of glutamine, inosine, cytosine, isoquercetin, and other substances. In the animal model, the TP-TR (1:2) treatment significantly reduced the frequency of coughs and prolonged cough latency compared to the model group. Results of the network pharmacology indicated that inflammatory-related factors such as TLR4, STAT3, EGFR, and AKT1 played crucial roles in cough treatment with TP-TR, consistent with the validation experiment. The 16s rDNA sequencing results revealed a significant increase in the abundance of Clostridia_UCG-014, Lachnospiraceae, Christenella, Ruminococcus, and other species in the intestinal tract of mice after modelling. TP-TR (1:2) reduced the abundance of pro-inflammatory flora such as Clostridium_UCG-014 and Lachnospira, which were closely associated with L-lysine and trans-4-hydroxy-L-proline present in TP-TR according to correlation analysis. ConclusionTP-TR may promote the dissolution of glutamine, thymidine, inosine, cytosine, isoquercetin, and other components through their combination, thereby regulating the abundance of Clostridium_UCG-014 and Lachnospira and exerting an antitussive effect. This study, for the first time, showed that TP-TR at a 1:2 ratio exhibits superior anti-inflammatory effects. In addition to inflammatory mediators like EGFR, TLR4, AKT1, and STAT3, gut microbes could also serve as potential regulatory targets of TP-TR in the treatment of cough. 2'-Deoxyguanosine monohydrate, L-lysine, L-leucine, γ-aminobutyric acid, L-valine, L-tryptophan, L-proline, trans-4-hydroxy-L-proline, L-methionine, uridine, 2'-deoxyinosine, guanosine, cucurbitacin B and cucurbitacin D were identified as its anti-inflammatory active ingredients.

Development and Characterization of Inula britannica Extract-Loaded Liposomes: Potential as Anti-Inflammatory Functional Food Ingredients.

We investigated the potential of Inula britannica extract encapsulated in liposomes as a functional food ingredient with enhanced bioavailability and stability. Inula britannica, known for its anti-inflammatory properties and various health benefits, was encapsulated using a liposome mass production manufacturing method, and the physical properties of liposomes were evaluated. The liposomes exhibited improved anti-inflammatory effects in lipopolysaccharide-activated RAW 264.7 macrophages, suppressing the production of pro-inflammatory mediators such as nitric oxide and prostaglandin E2 and downregulating the expression of iNOS and COX-2 transcription factors. Additionally, we observed reduced production of pro-inflammatory cytokines TNF-α, IL-6, and IL-1β, and modulation of the NF-κB and mitogen-activated protein kinase signaling pathways. These findings suggest that Inula britannica extract encapsulated in liposomes could serve as a valuable functional food ingredient for managing and preventing inflammation-related disorders, making it a promising candidate for incorporation into various functional food products. The enhanced absorption and stability provided by liposomal encapsulation can enable better utilization of the extract's beneficial properties, promoting overall health and well-being.

Protopine Alleviates Dextran Sodium Sulfate-Induced Ulcerative Colitis by Improving Intestinal Barrier Function and Regulating Intestinal Microbiota.

Ulcerative colitis (UC) is an inflammatory bowel disease (IBD), and its pathogenesis is related to intestinal mucosal barrier damage and gut microbiota imbalance. Protopine (PRO), an isoquinoline alkaloid, is one of the main anti-inflammatory ingredients of traditional Chinese medicine Macleaya cordata(Willd.) R. Br. This study investigated the effects of PRO on the intestinal mucosal barrier and gut microbiota in dextran sodium sulfate (DSS)-induced colitis mice. C57BL/6J mice were treated with 3% DSS in drinking water to induce acute colitis, while PRO was administered orally once daily for 7 days. The results showed that PRO administration significantly alleviated the symptoms of DSS-induced colitis in mice and inhibited the expression of inflammation-related genes. In addition, PRO restored the integrity of the intestinal barrier in colitis mice by restoring colonic mucin secretion and promoting the expression of tight junction proteins. Furthermore, PRO alleviated the DSS-induced gut microbiota dysbiosis by decreasing the abundance of Proteobacteria, Escherichia-Shigella and Enterococcus, as well as enhancing the abundance of beneficial bacteria, such as Firmicutes and Akkermansia. These findings suggested that PRO effectively alleviated DSS-induced ulcerative colitis by suppressing the expression of inflammation-related genes, maintaining the intestinal mucosal barrier and regulating the intestinal microbiota.

Essential oil from the stems of Croton kongensis Gagnep.: chemical composition, antimicrobial and anti-inflammatory activities

The current study describes the chemical compositions, antimicrobial and anti-inflammatory activities of the essential oil (EO) from the stems of Croton kongensis Gagnep., collected from two wild-growing populations in Thanh Hoa province, Vietnam, namely Nhu Xuan and Thuong Xuan. According to gas chromatography/mass spectrometry (GC/MS) analyses, the major components in the Nhu Xuan EO sample were (E)-caryophyllene (10.62%), bornyl acetate (9.81%), (E)-nerolidol (9.15%), and linalool (8.10%). In contrast, linalool (15.05%), bornyl acetate (9.52%), (E)-caryophyllene (7.91%), bicyclogermacrene (7.36%), 1,8-cineole (6.53%), and (E)-nerolidol (6.00%) were the dominant components in the Thuong Xuan EO sample. The two EO samples were screened for antimicrobial activity against a panel of pathogenic bacteria and fungi using a broth microdilution assay and showed promising antimicrobial activities with minimum inhibitory concentration (MIC) ≤ 200 μg/mL. Among them, the Nhu Xuan EO sample exhibited better activity against four bacteria and three fungi compared to the Thuong Xuan EO sample, which only showed activity against one bacterium and three fungi. Additionally, the anti-inflammatory study demonstrated that the EO samples from Nhu Xuan and Thuong Xuan inhibited nitric oxide production in lipopolysaccharide-stimulated RAW 264.7 macrophage cells, with IC50 values of 105.71 ± 0.96 μg/mL and 94.93 ± 1.31 μg/mL, respectively. In conclusion, this is the first report describing the antimicrobial and anti-inflammatory effects of the EO from C. kongensis stems. Our results suggest that the EO from C. kongensis stems in both regions could be potentially utilized as new natural antimicrobial and anti-inflammatory ingredients in the medicine and food industries.

The extraction and anti-inflammatory screening of Onosma glomeratum Y. L. Liu

“Zicao” has a long medicinal history and has a variety of pharmacological activities. As the main resource of “zicao” in Tibet, Onosma glomeratum Y. L. Liu (tuan hua dian zi cao), usually used for treating pneumonia in Tibet, has not been reported deeply. In order to determine the main anti-inflammatory active ingredients of Onosma glomeratum Y. L. Liu, in this study, the extracts enriched in naphthoquinones and polysaccharides were optimized prepared form Onosma glomeratum Y. L. Liu by ultrasonic extraction, and reflux extraction, respectively, with Box-Behnken design effect surface method. And their anti-inflammatory abilities were screened on LPS induced A549 cells model, for figuring out the anti-inflammatory active ingredients from Onosma glomeratum Y. L. Liu. The extract enriched naphthoquinone was obtained under following condition: extract with 85% ethanol in a liquid to material ratio of 1:40 g/mL at 30 °C for 30 minutes using ultrasound, leading to the extraction rate of total naphthoquinone as 0.98 ± 0.017%; the extract enriched polysaccharides was prepared as follows: extract 82 minutes at 100 °C with distilled water in a liquid to material ratio of 1:50 g/mL, with extraction rate of polysaccharide as 7.07 ± 0.02%. On the LPS-induced A549 cell model, the polysaccharide extract from Onosma glomeratum Y. L. Liu showed better anti-inflammatory effects than the naphthoquinone extract, indicating the extract enriched in polysaccharides is the anti-inflammatory extract of Onosma glomeratum Y. L. Liu, which could serve as a potential anti-inflammatory extract in medical and food industries in the future.

Roles of Anti-Inflammatory Active Ingredients of Saussurea costus in Silico approach as Adjuvant Therapy in COVID-19 Cases

SARS-CoV-2 (COVID-19) remains a very high risk to this date. The COVID-19 mortality rate is relatively high since it potentially causes various complications and cytokine storms, thereby increasing the mortality rate of those infected. Consumption of healthy food/drink is one of the means to boost the immune system and prevent COVID-19 infection. One of the interesting plants to use in this case is Saussurea costus. This plant contains active ingredients that can serve as anti-inflammatory, antitumor, antibacterial, antiseptic, antifungal agents, etc. However, studies on the role of the active ingredients as an anti-inflammatory agent to treat COVID-19, prevent cytokine storms, and improve COVID-19 patient outcomes are rarely found. In this in silico study, a total of 75 compounds in Saussurea costus were analized and five of which showed the greatest potential as the drug candidates, namely isoalantolactone, isozaluzanin C, arbusculin a, β-costic acid, and picriside B. Three target proteins were utilized in this study, including IL-6R, NFKB1, and TNFR1. The ligand samples were minimized before the molecular simulation process, and then the target proteins were sterilized. Furthermore, biological activity tests were conducted on the (anti-inflammatory and immunosuppressant) drug candidate compounds, followed by a druglikeness analysis, and ended with blind dockings to screen the potential compounds of the natural ingredients. The analysis of the docking results was performed using LigPlot+. The analysis results signified that according to the predicted probability with medium confidence (Pa &gt; 0.3), all of the drug candidate compounds of Saussurea costus in silico indicated biological activities as anti-inflammatory and immunosuppressant agents, which could be categorized as drug-like molecules. In addition, the molecular docking analysis results in this study suggested that the five active compounds of Saussurea costus showed an affinity for the aforementioned target proteins. Among the five active compounds, picriside B had the lowest binding affinity for IL-6R, NFKB1, and TNFR1, with total energies of -6.3kcal/mol, - 6.5kcal/mol, and -9.0 kcal/mol, respectively. In addition, picriside B also demonstrated the most interactions with all of the target proteins. This compound was able to form hydrophobic and hydrogen bonds with the three target proteins. The other four active compounds could be potentially utilized as adjuvant therapy for COVID-19 because these compounds had an affinity for and many chemical bond interactions with the three target proteins.

Golden berry leaf extract containing withanolides suppresses TNF-α and IL-17 induced IL-6 expression in HeLa Cells.

Inflammation, characterized by the overexpression of IL-6 in various tissues, has been reported as a symptom of coronavirus disease 2019. In this study, we established an experimental system for overexpression of IL-6 in HeLa cells stimulated by TNF-α and IL-17, along with identification of anti-inflammatory materials and components from local agricultural, forestry, and fishery resources. We constructed a library of extracts from natural sources, of which 111 samples were evaluated for their anti-inflammatory activities. The MeOH extract of Golden Berry (Physalis peruviana L) leaf was found to exhibit strong anti-inflammatory properties (IC50=4.97µg/mL). Preparative chromatography identified two active constituents, 4β-hydroxywithanolide E (4β-HWE) (IC50=183nM) and withanolide E (WE) (IC50=65.1nM). Withanolides are known anti-inflammatory ingredients of Withania somnifera, an Ayurvedic herbal medicine. P. peruviana leaves containing 4β-HWE and WE should be considered as useful natural resources for anti-inflammatory products.

The clinical benefit of a multimodal topical approach to treating skin dyspigmentation

The recent removal of hydroquinone from the over-the-counter market has created a need for modern skin lightening formulations. An effective pigment lightening formulation must be non-irritating to prevent skin darkening from post-inflammatory hyperpigmentation, penetration enhanced to reach the epidermal/dermal junction, contain anti-inflammatory ingredients, and address multiple mechanisms of pigment production. The objective of this research was to demonstrate the efficacy of a topical multimodal pigment lightening preparation containing tranexamic acid, niacinamide, and licorice. Fifty female subjects 18+ years of all Fitzpatrick skin types with mild to moderate facial dyspigmentation were enrolled. Subjects were provided with the study product for twice daily use on the entire face and an SPF50 sunscreen with evaluations occurring at Week 4, Week 8, Week 12, and Week 16. The investigator used a face map to identify a pigmented target site on the face for dermaspectrophotometer (DSP) measurement. The dermatologist investigator completed a baseline facial efficacy and tolerability assessment. The subjects completed a tolerability assessment. 48/50 subjects completed the study without tolerability issues. The DSP readings demonstrated a statistically significant reduction in target spot pigmentation at Week 16. The investigator assessed a 37% decrease in pigment intensity, a 31% decrease in pigment extent, a 30% decrease in pigment homogeneity, a 45% improvement in brightness, a 42% improvement in clarity, and a 32% improvement in overall facial skin dyspigmentation at Week 16. The combination of penetration enhanced tranexamic acid, niacinamide, and licorice was effective in inducing facial pigment lightening.

Mechanisms affecting the biopharmacological properties of saffron active ingredients based on anti-inflammatory activity

ABSTRACT To explore the mechanisms affecting the biopharmacological properties of the active components of saffron. Ultrasonic extraction technique was applied to extract the active components from safflower materials and combined with molecular docking technique to screen four safflower anti-inflammatory active components, naiophenol-3–0-rutinoside, kaempferol-3-O-glucoside, quercetin and lignan. In order to understand the mechanism of the influence of its biopharmaceutical properties, the changes of the solubility and permeability parameters of the anti-inflammatory active components of safflower were obtained by using the classical shaking bottle method and the body enteric irrigation method. The compound environment had a great influence on the solubility of single active ingredient. The calculated results of the dose number of all ingredients were greater than 1, and the solubility properties were all high solubility. The absorption parameters and osmotic coefficients of kaempferol-3-O-glucoside and lignan varied insignificantly under different concentration conditions, while each osmotic coefficient of kaempferol-3-O-rutinoside and quercetin showed a positive proportional decreasing trend. In addition, the osmotic coefficients of the three components except kaempferol-3-O-glucoside did not change with environmental changes, and the overall anti-inflammatory active ingredient absorption mechanisms included both passive diffusion and active transport. The two biopharmaceutical properties of the solubility and permeability of the active ingredients of Safflower can be changed under the influence of the application environment and drug concentration. In the pharmaceutical process, the preparation means can be optimized from this aspect to achieve the purpose of improving the clinical efficacy of Safflower anti-inflammatory drugs.

Development of an online UPLC-PDA-ESI-Q-TOF-MS-LOX-FLD system for rapid screening of anti-inflammatory compounds in Polygala tenuifolia Willd

In this study, the first ultra-high performance liquid chromatography-photo-diode array-electrospray ionization-quadrupole-time-of-flight-mass spectrometry-lipoxygenase-fluorescence detector (UPLC-PDA-ESI-Q-TOF-MS-LOX-FLD) online system was developed for the identification and evaluation of anti-inflammatory active ingredients in Polygala tenuifolia Willd. Using this system, the UPLC fingerprints, mass fragments and LOX-binding peak profiles in the samples were rapidly and simultaneously obtained. A total of 101 compounds were isolated and identified and 38 compounds (11 oligosaccharide esters, nine xanthones, 17 saponins, and one glycosyloxyflavone) showed strong LOX-binding activity. Six compounds were selected to study their LOX-binding ability, and the results indicated that the content of the six compounds had a good linear relationship with the LOX-binding ability, and it was found that the substitution position, the type of substituent and the number of glycosyl groups all had a certain influence on the LOX-binding ability of the compounds. The LOX-binding activities of 10 compounds were verified by the surface plasmon resonance (SPR) technique and the activity results were consistent with the online system. After validation, we identified 7 active compounds that combined with LOX to exert anti-inflammatory effects for the first time. All the results fully demonstrate the efficiency, stability and reliability of the online system and this work provides an exemplary and useful method for the rapid screening of potential anti-inflammatory active compounds in P. tenuifolia and other traditional Chinese medicines. At the same time, it provides a new direction for screening small molecule inhibitors of enzymes like LOX.

Salidroside attenuates LPS-induced kidney injury through activation of SIRT1/Nrf2 pathway.

Salidroside (SAL) is an anti-inflammatory, antioxidant, anticancer, neuroprotective, and renal protective active ingredient extracted from the Chinese herb. Rhodiola Rosea. However, the role of SAL in kidney injury has not yet been elucidated. The study investigates SAL's protective effect and mechanism in lipopolysaccharide (LPS)-induced kidney injury. Male C57BL/6 wild-type mice (6-8weeks old) were intraperitoneally injected with 10mg/kg LPS for 24h and SAL (50mg/kg) 2h before the LPS injection. Biochemical and TUNNEL staining assay analyses were carried out to assess kidney injury. The Elisa assay analyzed the mRNA expression of NGAL and KIM-1. RT-qPCR and Western blotting measured the mRNA and protein expression of HO-1, NQO1, Beclin1, P62, SIRT1, Nrf2, and PNCA, respectively. Our study found that mice co-treated with SAL had significantly reduced blood urea nitrogen (BUN), serum creatinine (Scr), neutrophil gelatinase-associated lipocalin (NGAL), and kidney injury molecule-1 (KIM-1) levels in serum of LPS-induced mice. SAL cotreatment potentially decreased the apoptosis rate of kidney tissue and podocytes induced by LPS. SAL significantly reduced the content of malondialdehyde (MDA) and increased superoxide dismutase (SOD) in LPS-treated mice. Autophagy-related proteins Beclin-1 increased but decreased P62 protein expression by cotreatment of SAL in LPS-injected mice. SAL enhanced the Sirtuin 1 (SIRT1) and nuclear factor erythroid 2-related factor 2 (Nrf2) protein expression in LPS-induced kidney tissues. Our results speculate that SAL protects against LPS-induced kidney injury through activation of the SIRT1/Nrf2 pathway.

Protective effect of Allium scorodoprasum L. ethanolic extract in cyclophosphamide-induced hepatotoxicity model in rats.

Cyclophosphamide is a chemotherapeutic agent and immunosuppressant drug; however, it damages the liver. This study investigates the protective effect of ethanolic extract of Allium scorodoprasum (ASE) on cyclophosphamide-induced liver injury. Twenty-eight Wistar albino rats were randomly divided into four groups (n = 7 per group): healthy rats, cyclophosphamide (200 mg/kg), cyclophosphamide (200 mg/kg) + ASE (100 mg/kg) and cyclophosphamide (200 mg/kg) + ASE (200 mg/kg). ASE was administered for 14 days, and the rats were euthanized 24 h after cyclophosphamide administration. Cyclophosphamide treatment leads to an increase in serum levels of alanine aminotransferase, aspartate aminotransferase, lactate dehydrogenase, total cholesterol, triglycerides, low-density lipoprotein and very low-density lipoprotein, as well as an increase in the liver levels of malondialdehyde, tumour necrosis factor, interleukin (IL)-1β and IL-6, while high-density lipoprotein levels decrease. Treatment with cyclophosphamide caused liver necrosis and postnecrotic cell infiltration; however, pathological changes were prevented by ASE. 8-Hydroxy-2'-deoxyguanosine, anti-4-hydroxynenal antibody and anti-dityrosine levels increased in rats treated with cyclophosphamide and decreased in the groups treated with ASE. These changes were dose dependent in the ASE-treated groups. Treatment with cyclophosphamide caused liver damage due to oxidative stress and inflammation. ASE regulated the damage at high doses because it has potent antioxidant and anti-inflammatory ingredients. In future studies, it may be beneficial to administer ASE in higher doses or for longer periods of time.