JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
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2023
·
IF 3.4
Quancheng Yang,Peng Cao,Yi Lv,Hua Peng,Xuejia Zhai
Pediatric heart failure (HF) is an important clinical disease with high hospitalization rates, morbidity, mortality and medical costs. Sacubitril/valsartan (also known as Entresto), was approved for the treatment of adult HF and is recently used in pediatrics. However, clinical therapy on children is more challenging than adults, and the pharmacokinetics of Entresto in children are still largely unknown and urgently needed. Herein, we aim to develop a simple and sensitive analytic method to monitor Entresto in pediatric patients, which is of great importance for individualized safe medication in children. Specifically, a liquid chromatography tandem mass spectrometry method for simultaneously quantification of valsartan, sacubitril and its bio-active metabolite sacubitrilat in human plasma has been developed and validated in pediatric patients. Plasma samples were pretreated with acetonitrile for protein precipitation. Elution was performed on X Select HSS T3 column (2.1 × 100 mm, 5 µm; Waters) column using an isocratic mobile phase process consisting of 0.1% formic acid aqueous solution and 0.1% formic acid acetonit rile with a total run time of 3.0 min. Valsartan-d3, sacubitrilin-d4 and sacubitrilat-d4 were used as the corresponding deuterium internal standards. According to the Bioanalytical Method Validation Guidance for Industry, the method was validated in the range of 0.5–5000 ng/mL. Intra- and inter-day accuracy of sacubitril,valsartan and sacubitrilat ranged from 93%− 108%, 98%− 109%, 91%− 102%, respectively, with relative standard deviation of precision ranging from 2.0% to 5.1%, 2.4%− 7.5%, 1,3%− 7.4%. The proposed method demonstrated good accuracy, precision and linearity. The matrix factors normalized by internal standard meet the acceptance criteria. The method was fully validated and applied in 39 children. Trough concentration of the three substances to be measured were: valsartan (11.3–938.0 ng/mL), sacubitril (0.5–395.5 ng/mL) and sacubitrilat (522.1–4890.0 ng/mL). Overall, this is the first study to simultaneously determined the plasma valsartan, sacubitril and sacubitrilat concentrations in children, which is believed to facilitate the clinical management of pediatric HF.
研究领域:
药理学
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儿科学
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临床医学
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DOI
PubMed
高影响因子
JOURNAL OF CHEMICAL THERMODYNAMICS
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2020
·
IF 2.888
Renren Sun,Haixia He,Yameng Wan,Liyuan Li,Jiao Sha,Gaoliang Jiang,Yu Li,Tao Li,Baozeng Ren
In this research, solubility of kojic acid in fourteen mono-solvents was obtained by laser monitoring approach at various temperatures under 0.1 MPa. The mole solubility of kojic acid exhibited a positive relation with temperature. Moreover, the solubility sequence of kojic acid at 298.15 K is: dimethyl sulfoxide (DMSO) > N-methylpyrrolidone (NMP) > N, N-dimethylacetamide (DMAC) > N, N-dimethylformamide (DMF) > 2-methoxyethanol > 2-ethoxyethanol > acetic acid > methanol > 1,4-dioxane > ethanol > water > n-propanol > acetone > ethyl acetate. The Hansen solubility parameter (HSP) and solvents polarity were applied to explore this solubility behaviour. The experimental solubility data was correlated with five thermodynamic models including two-Suffix Margules, NRTL-SAC, NRTL, modified Apelblat equation and UNIQUAC model, and the calculated results indicated that all of models had great fitting effects with the measured solubility data. Furthermore, the solution thermodynamic properties (Δ dis G o , Δ dis H o , Δ dis S o ) of kojic acid in investigated solvents were calculated by van’t Hoff equation. The positive values of Δ dis H o and Δ dis S o indicated that the dissolution process of kojic acid in all the measured solvents was endothermic and entropy-driven.
研究领域:
化学
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物理化学
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热力学
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DOI
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2023
·Vol. 24
·期 7
·6013
·
IF 5.6
Wei Wang,Lijuan Yang,Weiwei Wang,Jianyong Zhang,Ulrich H. Engelhardt,Heyuan Jiang
The inhibition of tyrosinase (TYR) activity is an effective measure to inhibit melanin synthesis. At present, there are many methods with discrepant details that study the TYR inhibitory activity of samples. Under the same experimental conditions, this paper systematically studies whether enzyme species and sample addition methods are the key factors that determine the TYR inhibitory activity of samples. TYRs extracted from B16F10 cells, apple and mushroom, called BTYR, ATYR and MTYR, respectively, were selected to implement this study. Results showed that TYR inhibitory activities of samples were obviously affected by the above two factors. It was necessary to select the appropriate enzyme according to the problems to be explained. It was speculated that indirectly inhibitory activity reflected the comprehensive effects of samples on TYR catalytic activity and intracellular TYR synthesis pathway, while directly inhibitory activity reflected the effects of samples on TYR catalytic activity. Additionally, kojic acid could be used as a positive control for both B16F10 cells and MTYR models. The TYR inhibitory activity of β-arbutin was complicated and fickle, while that of epigallocatechin gallate (EGCG) was universal and stable, which is to say, EGCG always inhibited TYR activity in a dose-dependent manner. In conclusion, the TYR inhibitory activities of samples were affected by enzyme species and sample addition methods. Compared with the unstable β-arbutin, EGCG was more valuable for clinical research.Keywords:tyrosinase;species;sample addition methods;EGCG;kojic acid;β-arbutin
研究领域:
生物化学
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药理学
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皮肤病学
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DOI
PubMed
高影响因子
Cosmetics
·
2025
·Vol. 12
·期 4
·174
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IF 3.2
Jian-Ye Zhu,Zeng-Yue Ge,Qi-Bin Yang,Cai-Fu Jiang,Lei Wu,Xin-Yuan Jiang,Lin-Fu Liang
Natural tyrosinase inhibitors are currently a hot research topic due to their potential application in cosmetic and medicinal products. For the plantLycopodiastrum casuarinoides, the chemical constituents with a tyrosinase inhibitory effect have not been investigated yet. Bioassay-guided isolation was conducted on the aboveground parts, resulting in the isolation of 10 compounds (1–10). Their chemical structures were confirmed by their spectral data and comparison with literature data. It might be worth pointing out that compounds3–9were isolated from the genusLycopodiastrumfor the first time. The bioassay revealed that compounds6and7displayed moderate mushroom tyrosinase inhibitory activity (IC50= 1.90 and 2.43 mM, respectively), which was close to the positive control kojic acid (IC50= 0.17 mM). Moreover, the in silico experiments disclosed that Lys180, His178 and other amino residues played key roles in the binding modes between compounds6and7and mushroom tyrosinase (PDB: 2Y9X). These findings suggested potential for further investigation on this species as a source of cosmetic ingredients.
研究领域:
天然产物化学
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生药学
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生物化学
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化妆品科学
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结构生物学
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DOI
高影响因子
JOURNAL OF FOOD QUALITY
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2023
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IF 3.3
Jing-Xin Ye,Yun-Fang Qian,Wei-Qing Lan,Jing Xie
Biofilms composed of microbes and extracellular polymeric substances (EPSs) pose a significant risk to human health and lead to economic loss in the food industry. In this study, the antimicrobial and antibiofilm properties of kojic acid (KA) against Aeromonas sobria (A. sobria) and Staphylococcus saprophyticus (S. saprophyticus) were investigated by determining the leakage of DNA and protein, cell morphology, biofilm formation, the metabolic activity of biofilms, excretion of EPS, and biofilm architecture. The results indicated that the values of minimum inhibitory concentration (MIC) of A. sobria and S. saprophyticus after KA treatment were 0.4 mg/mL and 1.6 mg/mL, respectively. 1 × MIC KA showed unignorable antimicrobial activity against the two bacteria, leading to alterations in the bacterial physicochemical characteristics and cell death. Sub-MICs of KA can inhibit biofilm formation and decrease the metabolic activity and excretion of EPS, and these inhibition effects were in a dose-dependent manner. These results were further confirmed by the visual images obtained from scanning electron microscopy (SEM) and confocal laser scanning microscopy (CLSM). Moreover, S. saprophyticus is more susceptible to KA in inhibiting biofilm formation, and for A. sobria, changes in the cell structure and the permeability of the cell membrane were more obvious. This research highlighted the antibacterial and antibiofilm activity of KA against A. sobria and S. saprophyticus.
研究领域:
微生物学
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生物技术
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食品科学
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DOI
高影响因子
EXPERIMENTAL AND MOLECULAR PATHOLOGY
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2025
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IF 3.7
Jinpeng Lv,Kun Zou,Chuanwei Yin,Wenhui Xu,Duo Meng,Huansha Zhang,Wenhao Yu,Peiwen Jiang,Changjun Yun,Hui Xue,Nan Hu,Rongyin Gao
Daidzin, a prominent isoflavone found in soybeans, Pueraria lobata , and various legumes, has been extensively investigated for its diverse pharmacological activities, which include anticancer, antioxidant, anti-inflammatory, antiepileptic, and alcohol detoxification properties. Previous studies have shown that the dichloromethane fraction of Pueraria lobata stem (DCM-PLS) exhibits significant anti-melanogenic activity, with daidzin identified as the principal active compound. However, the precise role of daidzin in pigmentation remains incompletely understood. This study aimed to investigate the effects of daidzin on pigmentation and to elucidate the underlying mechanisms. Our findings revealed that daidzin not only inhibited basal melanin production but also reduced melanin synthesis induced by α-MSH, ACTH, and UV exposure. The effects of daidzin were primarily mediated through the activation of the extracellular signal-regulated protein kinase (ERK) and protein kinase B (AKT) pathways. Upon activation, these pathways facilitated the ubiquitination and degradation of Melanocytes Inducing Transcription Factor (MITF), resulting in decreased expression of tyrosinase, TRP-1, and TRP-2, ultimately inhibiting melanogenesis. Importantly, our research further demonstrated that daidzin reduced pigmentation in both zebrafish and human skin explants, highlighting its potential application as a therapeutic approach for disorders related to skin pigmentation.
研究领域:
药理学
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皮肤科学
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生物化学
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分子生物学
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植物学
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细胞生物学
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DOI
PubMed
高影响因子
Food Bioscience
·
2024
·
IF 4.8
Zhengming Xu,Xi Zhu,Jiayi Lian,Yuan Guan,Zhengang Zhao
Exploiting efficient tyrosinase inhibitors and utilizing the inhibition mechanism are of great significance to avoid enzymatic browning in food and skin melanogenesis. Polydatin had excellent tyrosinase inhibitory activity in vitro with IC 50 value of 24.90 μM; however, it exhibited unsatisfactory inhibitory activity intracellularly, which was associated with poor cellular uptake. Fortunately, 6″- O -lauryl polydatin was green-efficiently synthesized by lipase-catalyzed acylation under microwave irradiation. 6″- O -lauryl polydatin exhibited superior mono-/diphenolase inhibitory activity within 100 μM than kojic acid, which had IC 50 of 221 μM. Neither polydatin nor 6″- O -lauryl polydatin bound to the catalytic site, but rather bound noncovalently to the allosteric site 2 of tyrosinase through hydrogen bonds and hydrophobic interactions according to molecular simulations, thereby inducing secondary structure unfolding and reducing tyrosinase activity. 6″- O -lauryl polydatin showed stronger anti-browning effects than polydatin in the natural storage of potato and apple pieces. Polydatin and kojic acid did not induce apoptosis, but 6″- O -lauryl polydatin inhibited human melanin A375 cell proliferation by stimulating ROS overproduction and regulating cell cycle and apoptotic pathways. In addition, lipophilic 6″- O -lauryl polydatin had greater cellular uptake though suffered from intracellular hydrolysis, and exerted better tyrosinase and melanogenesis inhibitory activity than polydatin and kojic acid based on mouse B16F10 melanoma cell model. The results suggested polydatin and 6″- O -lauryl polydatin were promising tyrosinase inhibitors for anti-browning in foods or cosmetics fields.
研究领域:
食品科学
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药学
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化妆品化学
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酶学
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DOI
高影响因子
JOURNAL OF FOOD SCIENCE
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2024
·Vol. 89
·期 12
·8398-8409
·
IF 3.2
Junguo Wang,Hongyue Wang,Keshuang Guo,Xindi Zhang,Xiangrong Zhang
The purpose of this study was to prepare and evaluate the formulation of nanoemulsions (NEs) to encapsulate phloretin (PT) to improve its stability, antioxidant, and tyrosinase inhibitory competence. The aim of this study was to improve the stability, antioxidant, and tyrosinase inhibitory effects of PT via NEs. The formulations were prepared using low energy emulsification method for PT-VE-NEs, α -tocopherol (Vitamin E) and medium chain triglycerides (MCT) were used as the oil phase, and Tween 60 was used as the emulsifier and PEG-400 as the co-emulsifier. The droplet size and zeta potential of oil-in-water NEs were evaluated using dynamic light scattering. The PT-VE-NEs were also characterized by transmission electron microscopy and Fourier transform infrared spectroscopy. The mean droplet diameter was 14.85 ± 0.14 nm, with a zeta potential of −2.47 ± 0.51 mV. Fourier transform infrared spectroscopy revealed the formation of molecular interactions in the NEs formulations. PT-VE-NEs size was maintained the same during the in vitro digestion study. The particle size of PT-VE-NE remained stable during in vitro digestion. The addition of VE significantly improved the antioxidant, tyrosinase inhibitory effects, as well as thelion and physical stability of PT-VE-NE. The results revealed that NEs is a promising strategy to improve the functionality and stability of PT and VE. PT-VE-NEs will be applied for the preservation of fruits.
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PubMed
高影响因子
Chemistry Africa-A Journal of the Tunisian Chemical Society
·
2024
·
IF 2.3
Wang Wenchao,An Lianhao,Lei Junrong,Li Dan,Shen Zheluan,Wang Hong,Li Qingyong
Pearl powder has been used in medicine and beauty treatment since ancient times in China. However, it is still unclear whether the biological activities of pearl powder are affected by different extraction methods or not. In this study, we determine the total protein yield, protein molecular weight and biological activities including antioxidant, tyrosinase inhibition and melanogenesis inhibition activities and cytotoxicity of different pearl powder extracts prepared by five different preparation methods. The ultrasonic-assisted extraction (UAE) and microwave-assisted extraction (MAE) of pearl powder were optimized by the response surface method based on total protein yield. Compared with solid-liquid extraction (SLE), the optimized UAE and MAE increased the total protein yield without changing protein molecular weight. In addition, the extract by MAE enhanced the tyrosinase inhibition activity and anti-melanogenesis activity slightly. Acidolysis hydrolyzes macromolecular protein into small molecules with obvious cytotoxicity and low activities. Enzymolysis can hydrolyze macromolecular protein into small molecules with high protein yield and improvement of bioactivities. In the determination of the antioxidant assay, the extract prepared by the enzymolysis showed significant activity. These results suggest that protein molecules of the pearl powder extract are degraded appropriately by enzymolysis to smaller molecules to obtain the enhanced biological activities that can be applied in the cosmetic industry.
研究领域:
药学
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化妆品科学
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生物化学
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产品关联
DOI
高影响因子
FOOD CHEMISTRY
·
2024
·
IF 8.5
Jinfeng Zhang,Wei Yang,Min He,Zhiyun Peng,Guangcheng Wang
Tyrosinase (Polyphenol oxidase), a key enzyme in enzymatic browning, is an attractive target for developing new anti-browning agents in the food industry. In this work, twenty pyrazole-1,2,4-triazole derivatives ( 3a-3n, 4a-4f) were synthesized and tested in vitro, most of compounds showed potent anti-tyrosinase activity. Of these, 3c (IC 50 = 1.02 ± 0.08 μM) was found to be 14 folds stronger than kojic acid (IC 50 = 14.74 ± 1.23 μM) and behaved as a mixed type inhibitor. Besides, the disappeared peak of dopaquinone in the HPLC assay intuitively validated the inhibitory effect of 3c . Copper ions chelating, fluorescence quenching and molecular docking assays showed that coordination with copper is the key to play a role. Furthermore, 3c exhibited excellent anti-browning ability for the Rosa roxburghii Tratt, the non-enzymatic browning experiment showed that 3c could prevent browning in non-enzymatic ways. It is suggested that these derivatives could serve as the leading compounds to find more efficient anti-browning agents in the future.
研究领域:
食品科学
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药物化学
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生物化学
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产品关联
DOI
PubMed
高影响因子
FITOTERAPIA
·
2024
·
IF 2.5
Yuan Wei,Wen-Hua Dong,Wei Li,Jun Zeng,Hui-Qin Chen,Sheng-Zhuo Huang,Li Yang,Wen-Li Mei,Ya-Li Wang,Zhi-Yong Guo,Hao-Fu Dai,Hao Wang
Six new dimeric 2-(2-phenylethyl)chromones ( 1 – 6 ) were successfully isolated from the ethanol extract of agarwood of Aquilaria filaria from Philippines under HPLC-MS guidance. Compounds 1 – 6 are all dimers formed by linking 5,6,7,8-tetrahydro-2-(2-phenylethyl)chromone and flindersia 2-(2-phenylethyl)chromone via a single ether bond, and the linkage site (C5-O-C8′′) of compound 2 is extremely rare. A variety of spectroscopic methods were used to ascertain their structures, including extensive 1D and 2D NMR spectroscopic analysis, HRESIMS, and comparison with literature. The in vitro tyrosinase inhibitory and anti-inflammatory activities of each isolate were assessed. Among these compounds, compound 2 had a tyrosinase inhibition effect with an IC 50 value of 27.71 ± 2.60 μM, and compound 4 exhibited moderate inhibition of nitric oxide production in lipopolysaccharide-stimulated RAW264.7 cells with an IC 50 value of 35.40 ± 1.04 μM.
研究领域:
植物化学
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药理学
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产品关联
DOI
PubMed
高影响因子
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
·
2025
·
IF 3
Yilu Sun,Jia Zhao,Jianhui Rong
Skin hyperpigmentation due to UV-induced tyrosinase activation and melanin overproduction is an ongoing challenge in cosmetic and dermatological applications. While resveratrol analogues show anti-melanogenic potential, the structure-activity relationships of their glycosylated derivatives remain underexplored. Here, we investigate how the vinyl moiety in the food-derived stilbenoid glycoside piceid (resveratrol-3- O -β-glucoside) affects tyrosinase inhibition. We reduced the vinyl moiety to yield dihydropiceid by catalytic hydrogenation and systematically assessed both compounds for anti-melanogenic effects. As results, piceid exhibited superior monophenolase inhibition over dihydropiceid in enzyme kinetics, while both compounds showed comparable diphenolase inhibition. Cellular assays revealed that piceid reduced melanin production by 59.2 % at 25 μM in α-MSH-stimulated B16F10 melanoma cells, whereas dihydropiceid showed weaker activity (<25 % reduction). MolgpKa analysis indicated that the vinyl moiety lowered the 4′-OH pKa (9.7 vs. 9.9), while UV–vis spectroscopy validated that the vinyl moiety enhanced the copper chelation capacity of piceid (ΔOD: 0.459) over dihydropiceid (ΔOD: 0.233). Molecular docking revealed that 4′-OH in piceid closely coordinated the tyrosinase binuclear copper center, whereas molecular dynamics simulation validated that hydrogen bonding supports the binding of both compounds to tyrosinase. Collectively, this study establishes the vinyl moiety in dietary stilbenoids as a critical pharmacophore for tyrosinase inhibition and thereby provides a molecular basis for developing natural anti-hyperpigmentation functional foods or cosmeceuticals.
研究领域:
化妆品科学
·
分子生物学
·
药理学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）