Risk factors of disease activity and renal damage in patients with systemic lupus erythematosus.

PURPOSE: To evaluate the clinical features of patients with Systemic Lupus Erythematosus (SLE) and explore the risk factors of disease activity and renal damage. METHODS: A retrospective study involving 194 patients were performed. Patients were divided into lupus nephritis (LN) group (63.40%) and non-LN group (36.60%), different disease activity group, and different renal function group according to the clinical data. Multivariate logistic regression analysis showed that albumin (ALB), uric acid (UC), total cholesterol (TC), and anti-dsDNA antibodies were the influencing factors of LN in patients with SLE (P < 0.05); ALB, UC, and complement 3(C3) were the influencing factors of lupus disease activity (P < 0.05); UC, C3, and hemoglobin (HB) were the influencing factors of abnormal renal function in SLE patients. RESULTS: The results of the ROC curve showed that ALB, UA, and TC had certain predictive value for combined LN in patients with SLE, and the predictive value of ALB was greater than that of TC (P < 0.05); ALB, UA, and C3 being predictors of the activity of patients with SLE; BUN, UA, and HB all had certain predictive value for the abnormal renal function in patients with LN. SLE patients have the high incidence of renal impairment. CONCLUSION: The results of this study suggest that patients with SLE should regularly monitor the levels of ALB, UA, TC, C3, and HB, as well as pay attention to the intervention of hyperlipidemia and hyperuricemia in patients with SLE to better control disease progression.

Bioinspired ion channel receptor based on hygroelectricity for precontact sensing of living organism.

Tactile sensors play an important role in human-machine interaction (HMI). Compared to contact tactile sensing, which leaves physical hardware vulnerable to wear and tear, proximity sensing is better at reacting to remote events before physical contact. The apteronotus albifrons possess ion channel receptors for remote surroundings perception. Inspired by the relevant ion channel structure and self-powered operation mode, we designed a new proximity sensor with ion rectification characteristics and self-powered capability. This bio-inspired ion channel receptor exploits the hygroelectric effect to convert the humidity information into a series of current signals when the living organism approaches, and it is insensitive to non-aquatic non-organisms. The sensor offers high sensitivity (2.3 mm-1), a suitable range (0-10 mm) for close object detection, fast response (0.3 s), and fast recovery (2.5 s). The unique combination of bio-sensitivity, non-contact detection characteristics, and humidity-based power generation capabilities enriches the functionality of future HMI electronics. As a proof of concept, the sensor has been successfully applied in different scenarios such as human health management, early warning systems, non-contact switches to prevent virus transmission, object recognition, and finger trajectory detection.

Evaluating Earplug Performance over a 2-Hour Work Period with a Fit-Test System.

Workers rely on hearing protection devices to prevent occupational noise-induced hearing loss. This study aimed to evaluate changes in attenuation over time for properly fit devices when worn by workers exposed to hazardous noise. Earplug fit testing was accomplished on 30 workers at a brewery facility with three types of foam and three types of premolded earplugs. The personal attenuation ratings (PARs) were measured before and after a 2-hour work period while exposed to hazardous noise levels. The minimum acceptable initial PAR was 15 dB. Average decreases in PAR ranged from -0.7 to -2.6 dB across all six earplug types. Significant changes in PAR were observed for the Foam-1 ( p = 0.009) and Premold-3 ( p = 0.004) earplugs. A linear mixed regression model using HPD type and study year as fixed effects and subject as random effect was not significant for either fixed effect ( α = 0.05). Ninety-five percent of the final PAR measurements maintained the target attenuation of 15 dB. Properly fitting earplugs can be effective at reducing worker's noise exposures over time. The potential for a decrease in attenuation during the work shift should be considered when training workers and establishing the adequacy of protection from hazardous noise exposures.

Investigation on the Modeling and Reconstruction of Head Injury Accident Using ABAQUS/Explicit.

A process of modeling and reconstructing human head injuries involved in traffic crashes based on ABAQUS/Explicit is presented in this paper. A high-fidelity finite element (FE) model previously developed by the authors is employed to simulate a real accident case that led to head injury. The most probable head impact position informed by CT images is used for the FE modeling and simulation since the head impact position is critical for accident reconstruction and future analysis of accidents that involve human head injuries. Critical von Mises stress on the skull surface of the head model is chosen as the evaluation criterion for the head injury and FE simulations on 60 cases with various human head-concrete ground impact conditions (impact speeds and angles) were run to obtain those stress values. The FE simulation results are compared with the CT images to determine the minimum speed that will cause skull fracture and the corresponding contact angle at that speed. Our study shows that the minimum speed that would cause skull fracture is 3.5 m/s when the contact angle between the occipital position of the injured head and the ground is about 30°. Effects of the impact speed and the contact angle on the maximum von Mises stress of the head model are revealed from the simulations. The method presented in this paper will help forensic pathologists to examine the head impact injuries and find out the real reasons that lead to those injuries.

Alterations of Renal Function in Patients with Diabetic Kidney Disease: A BOLD and DTI Study.

Objectives: Our study aims to determine the patterns of renal oxygenation changes and microstructural changes by BOLD and DTI with deteriorating kidney function in patients with diabetic kidney disease (DKD). Methods: Seventy-two patients with type 2 diabetes mellitus (DM) and twenty healthy controls (HCs) underwent laboratory examinations, and renal BOLD and DTI images were obtained on a 3T-MRI machine. R2 ∗ , fractional anisotropy (FA), and average diffusion coefficient (ADC) values were evaluated. DM patients were divided into three subgroups (Group-DI/DII/DIII, based on urinary albumin-creatinine ratio (UACR)) and a nondiabetic kidney disease group (Group-NDKD). D-value and MCR of R2 ∗ and FA were proposed to evaluate the differentiation between medulla and cortex of the individual kidney among HCs and three subgroups for reducing individual differences. Comparisons were made between NDKD and kidney function-matched DKD patients. Correlations between MRI parameters and renal clinical indices were analyzed. Results: Compared with Group-HC/DI, medullary R2 ∗ and FA values were significantly different in Group-DII/III. The D-value of R2 ∗ and FA in Group-III were significantly smaller than that in Group-HC. However, only MCR of R2 ∗ in Group-III was significantly smaller than that in HCs. Medullary R2 ∗ and FA were negatively associated with serum creatinine (SCr) and cystatin C (Cys C) and positively associated with eGFR. Conclusions: With renal function declining, BOLD and DTI could capture alterations including the first rising and then falling medullary R2 ∗ , continuously declining medullary FA, and apparent cortex-medullary differentiation in DKD patients. The MRI parameters showed renal changes accompanied by varying degrees of albuminuria, sharing common involvement in DKD and NDKD patients, but it was hard to distinguish between them. BOLD seemed more sensitive than DTI in identifying renal cortex-medullary differentiation.

Association Between Passive Smoking and Menstrual Discomfort: A Cross-Sectional Study of 2,571 Non-smoking Chinese Nurses.

Introduction: Menstrual discomfort affects women's quality of life, which is an important public health issue. Evidence confirming the link between passive smoking and menstrual discomfort is limited. Therefore, the aim of this study is to investigate the aforementioned topic on the basis of a cross-sectional study of 2,571 non-smoking Chinese nurses. Methods: Demographic information and passive smoking were assessed using a self-administered questionnaire. Menstrual discomfort was characterized as dysmenorrhea, illness or weakness, bed rest, and restlessness during menstruation, which was assessed using a modified version of the Cornell Medical Index-Health Questionnaire. Multivariate-adjusted odds ratio (OR) and 95% confidence intervals (CIs) were estimated using the logistic regression model. Results: A total of 1:195 nurses (46.48%) were exposed to passive smoking. Compared with non-passive smoking nurses, passive smoking nurses were more likely to have menstrual discomfort symptoms (72.38 vs. 64.39%), especially symptoms of dysmenorrhea (49.54 vs. 42.08%), illnesses or weakness (48.28 vs. 42.08%), and restlessness during menstruation (53.05 vs. 46.22%). Exposure to passive smoking was significantly associated with menstrual discomfort (OR = 1.41, 95%CI: 1.19-1.67), especially symptoms of dysmenorrhea (OR = 1.32, 95%CI: 1.13-1.56), illness or weakness (OR = 1.24, 95%CI: 1.06-1.46), and restlessness (OR = 1.26, 95%CI: 1.08-1.48) during menstruation. The subgroup analyses, stratified by age, children, and marital status, agreed with the main findings. Conclusions: Exposure to passive smoking was related to symptoms of dysmenorrhea and menstrual discomfort.

Analysis of the correlation between the severity of neonatal hypoxic ischemic encephalopathy and multiple organ dysfunction.

OBJECTIVE: To evaluate the hypoxic ischemic encephalopathy (HIE) and multiple organ dysfunction (MOD) in neonates and analyze the correlation between the two disorders. METHODS: From January 2018 to January 2020, infants with HIE who were born in our hospital at or above 37 weeks of gestation, and those with ischemic hypoxic encephalopathy at or above 2000 grams were selected as study subjects. HIE and MOD monitoring were performed for three days. HIE severity was graded according to reported scores including amplitude integrated EEG. Multiple organ dysfunction was also assessed. The correlation between neonatal hypoxic ischemic encephalopathy and multiple organ dysfunction was analyzed. RESULTS: Children with HIE were divided into three grades: mild, moderate and severe. There were statistically significant differences among the three groups in emergency caesarean section, Apgar 5 minutes, systemic hypothermia and neonatal mortality. Differences in MOD scores were found in three HIE stages per day from Day 1 to Day 3. Among children with mild HIE grading, the most common mildly affected organ systems are pH, electrolyte imbalance and liver system, and the least affected organs are kidney and blood systems. Among children with HIE grade of mild and severe, there was no significant difference in moderate-severe organ involvement, and the number of severely affected children was small. CONCLUSION: With the increase of HIE severity, multi-organ involvement is aggravated. The organ involvement of HIE children with different degrees of severity is different.

Association Between Passive Smoking and Health Among Chinese Nurses: A Cross-Sectional Study.

This study aimed to investigate the association between passive smoking and physical and psychological health in Chinese nurses. Participants of this cross-sectional study comprised 2,484 non-smoking nurses. Passive smoking and demographic information were assessed using a self-administered questionnaire. Physical, psychological, and overall health status of nurses were measured using the Cornell Medical Index (CMI) health questionnaire. Multivariate-adjusted odds ratio (OR) and 95% confidence interval (CI) for nurses' health were estimated by exposure to passive smoking using unconditional logistic regression models. A total of 1,219 nurses (49.07%) were exposed to passive smoking. Of these, 609 (24.52%), 160 (6.44%), and 587 (23.63%) nurses had poorer physical, mental, and overall health, respectively. After adjusting for other confounding factors, compared with the non-passive smoking group, passive smoking was associated with poor physical (OR = 1.51, 95% CI: 1.25-1.83), mental (OR = 1.48, 95% CI: 1.07-2.07), and overall (OR = 1.58, 95% CI: 1.30-1.93) health of nurses, respectively. We also carried out subgroup analyses stratified by age, department, and professional title, which showed that most findings supported the main results. This study demonstrated that exposure to passive smoking was a risk factor for overall decreased physical and mental health status among Chinese nurses.

Evaluating the Effectiveness of Earplugs in Preventing Noise-Induced Hearing Loss in an Auto Parts Factory in China.

A survey was administered to 385 noise-exposed workers from an auto parts factory and 1268 non-noise-exposed health department employees in China. Individual 8 h A-weighted equivalent sound levels (LAeq,8h), earplug personal attenuation ratings (PARs), and pure-tone audiometric tests were performed. The average LAeq,8h of noise-exposed workers was 87 dB (A) with a mean PAR of 7 dB. The prevalence of high-frequency hearing loss was 65% for noise-exposed workers and 33% for the non-noise-exposed employees. The use of earplugs had no observable effect on the prevalence of high-frequency hearing loss of the study participants (OR 0.964, 95% CI 0.925-1.005, p = 0.085). No significant relationship between the effectiveness offered by earplug use and high-frequency hearing thresholds at 3, 4, and 6 kHz was found (t = -1.54, p = 0.125). The mandatory requirement of earplug use without individualized training on how to wear HPDs correctly had no detectable effect on the prevention of hearing loss at the auto parts factory. The hearing conservation program at the surveyed factory was not effective. Periodic hearing tests, earplug fit testing, expanding the offer of different types of hearing protection, and employee education about the importance of protecting their hearing were recommended to the occupational health and safety program.

Association between night shift and sleep quality and health among Chinese nurses: A cross-sectional study.

AIM: To explore the sleep quality among Chinese nurses and identify the association between night shift and sleep quality and health. BACKGROUND: Chinese nurses have many night shifts; the effect of it regarding nurses' sleep quality and health is still not being explored. METHODS: This was a cross-sectional study. There were 3,206 nurse participants. The participants self-completed a sociodemographic questionnaire, the Pittsburgh Sleep Quality Index (PSQI) and the Cornell Medical Index (CMI). RESULTS: Night shift nurses demonstrated relatively worse sleep quality (55.1%) and more health problems (20.7%). Night shift work was significantly associated with poor sleep quality (ß = 0.96, confidence interval [CI] = 0.67-1.26) and poor health (ß = 2.01, CI = 0.15-3.88). Except for sleep medication (ß = 0.02, CI = -0.01, 0.05) and psychological health (ß = 0.38, CI = -0.27, 1.03), night shift work was significantly associated with other PSQI domains and physical health. CONCLUSION: Night shift work was a risk factor for nurses' sleep quality and health. Night shift nurses have more sleep disorders and physical health problems. IMPLICATIONS FOR NURSING MANAGEMENT: Nurse managers should pay attention to the impact of shift work on nurses' sleep quality and health and reform the rotating shift work system to improve nurses' occupational health.

Empagliflozin Regulates the AdipoR1/p-AMPK/p-ACC Pathway to Alleviate Lipid Deposition in Diabetic Nephropathy.

BACKGROUND: Abnormal lipid deposition in the progress of diabetic nephropathy (DN) plays an important role in a number of studies that have shown that SGLT2 inhibitor (SGLT2i) empagliflozin plays an important role in lipid metabolism, but its mechanism is still unclear. METHODS: We aimed to explore the effect of empagliflozin on lipid levels in kidney cancer patients with DN and postoperative patients without DN kidney carcinoma; the patients with DN showed ectopic lipid deposition. In type 2 diabetes model mice induced by streptozotocin (STZ) and a high-fat diet, combined AMPK plus empagliflozin or empagliflozin inhibitor plus compound C was applied, followed by analyses of the blood, urine and kidney indexes to observe the correlation between SGLT2i and AMPK and lipid metabolism in diabetic kidney disease. We determined whether DN in patients with renal tubular atrophy involved lipid metabolism. RESULTS: In clinical specimens, the adiponectin receptor AdipoR1 was reduced, and the phosphorylation acetyl-CoA carboxylase (p-ACC) was increased. In vitro and in vivo pathological immunofluorescence and Western blotting confirmed that, under the condition of high glucose, malpighian tubules displayed ectopic lipid deposition and expressed related lipid parameters accompanied by fibrosis. Empagliflozin intervention reduced lipid deposition fibrosis and renal tubular atrophy, and the addition of compound C promoted disease progression. Moreover, siAdipoR1 transfection proved that AdipoR1 affected P-AMPK and then p-ACC affected lipid metabolism in renal tubular cells. CONCLUSION: According to the above experimental results, empagliflozin could reduce lipid metabolism of DN through AdipoR1/P-AMPK/P-ACC pathway and delay DN progress.

Condensed Tannins from Longan Bark as Inhibitor of Tyrosinase: Structure, Activity, and Mechanism.

In this study, the content, structure, antityrosinase activity, and mechanism of longan bark condensed tannins were evaluated. The findings obtained from mass spectrometry demonstrated that longan bark condensed tannins were mixtures of procyanidins, propelargonidins, prodelphinidins, and their acyl derivatives (galloyl and p-hydroxybenzoate). The enzyme analysis indicated that these mixtures were efficient, reversible, and mixed (competitive is dominant) inhibitor of tyrosinase. What's more, the mixtures showed good inhibitions on proliferation, intracellular enzyme activity and melanogenesis of mouse melanoma cells (B16). From molecular docking, the results showed the interactions between inhibitors and tyrosinase were driven by hydrogen bond, electrostatic, and hydrophobic interactions. In addition, high levels of total phenolic and extractable condensed tannins suggested that longan bark might be a good source of tyrosinase inhibitor. This study would offer theoretical basis for the development of longan bark condensed tannins as novel food preservatives and medicines of skin diseases.

Proanthocyanidins purified from fruit pericarp of Clausena lansium (Lour.) Skeels as efficient tyrosinase inhibitors: structure evaluation, inhibitory activity and molecular mechanism.

Fruit pericarp of Clausena lansium (Lour.) Skeels, a food waste, was selected as a raw material for proanthocyanidins. The proanthocyanidins' structures were integrally analyzed using three methods: matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS), high performance liquid chromatography electrospray ionization mass spectrometry (HPLC-ESI-MS) and 13C nuclear magnetic resonance (NMR). The results elucidated that these compounds were composed of prodelphinidin (75%) and procyanidin (25%) with a degree of polymerization (DP) up to the 20-mers. They were proved to be remarkable, reversible and mixed competitive inhibitors of tyrosinase according to results from enzyme experiments. The IC50 values were calculated to be 23.6 ± 1.2 and 7.0 ± 0.2 µg mL-1 for the monophenolase and diphenolase activities, respectively. In addition, the proanthocyanidins had a good inhibitory effect on cell proliferation, cellular tyrosinase activity and melanin production of B16 mouse melanoma cells. Chelation between the hydroxyl group on the B ring of the proanthocyanidins and dicopper irons of the enzyme provided one of the feasible mechanisms for the inhibition on the basis of fluorescence quenching and molecular docking analyses. This research would supply the scientific basis to these compounds application in the pharmaceutical, insecticides, and preservative fields.

Structure characterization and anti-tyrosinase mechanism of polymeric proanthocyanidins fractionated from kiwifruit pericarp.

To provide information on the structure, activity, and structure-activity relationship of kiwifruit (Actinidia chinensis) pericarp proanthocyanidins (PAs), they were separated into three fractions. These fractions were further identified by MALDI-TOF MS and HPLC-ESI-MS methods. Spectra results revealed that they are complex mixtures of B-type propelargonidins, procyanidins, procyanidins gallate, and prodelphinidins. Enzymatic activity analysis showed that these compounds strongly inhibit the activity of tyrosinase, indicating that they are reversible and mixed-type inhibitors of the enzyme. The results obtained from fluorescence quenching showed PAs inhibit the enzyme activity by interacting with substrate and enzyme. This study confirmed that the mean degree of polymerization (mDP) of PAs produces a positive effect on their anti-tyrosinase activity. In addition, the antioxidant analysis indicated that PAs possess potent antioxidant activity. These conclusions mean kiwifruit pericarp PAs may be explored as insecticides, food preservatives, and cosmetic additives.

Antioxidant and antityrosinase proanthocyanidins from Polyalthia longifolia leaves.

In the present study the structure of proanthocyanidins from Polyalthia longifolia leaves was characterized with (13)C nuclear magnetic resonance, high performance liquid chromatography electrospray ionization mass spectrometry, and matrix-assisted laser desorption/ionization time-of-flight mass spectrometry analyses. The results showed that the proanthocyanidins were mixture of homopolymers of B-type procyanidins with degree of polymerization up to 14-mer. Furthermore, the antioxidant activity of the proanthocyanidins was studied through 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) free-radical scavenging activities, and ferric reducing/antioxidant power assays. In addition, antityrosinase activity of the proanthocyanidins was investigated. The IC50 for 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) free-radical scavenging activity of the proanthocyanidins were 89.32 ± 12.07 and 76.79 ± 5.88 µg/mL, respectively; the ferric reducing/antioxidant power value was 710.54 ± 142.82 mg ascorbic acid equivalent/g dry weight. The IC50 for antityrosinase activity was 773.09 ± 1.47 µg/mL. In conclusion, the proanthocyanidins from P. longifolia leaves exhibited potent antioxidant and antityrosinase activities. This research would provide scientific evidence for the use of proanthocyanidins from P. longifolia leaves as antioxidant and antityrosinase agents.

Structure characterization of proanthocyanidins from Caryota ochlandra Hance and their bioactivities.

Proanthocyanidins (PAs) from Caryota ochlandra fruit pericarp and fruit flesh were characterized by (13)C nuclear magnetic resonance, high performance liquid chromatography-electrospray ionization mass spectrometry, and matrix-assisted laser desorption/ionization time-of-flight mass spectrometry techniques. The fruit pericarp and flesh PAs were complex mixtures of homo- and heteropolymers of B-type procyanidins and prodelphinidins both with degrees of polymerization up to dodecamer. Their antioxidant and antityrosinase activities were investigated. The fruit pericarp PAs exhibited potent antioxidant activity with IC50 values of 142.86 ± 1.53 and 80.51 ± 0.4 µg/ml for DPPH and ABTS free-radical scavenging assays; with FRAP value of 373.09 ± 5.02 mg ascorbic acid equivalent/g dry weight. Furthermore, the fruit pericarp PAs had antityrosinase activity while the fruit flesh PAs could be oxidized by tyrosinase. The structure and antioxidant activities of the C. ochlandra fruit PAs together with their effects on tyrosinase activity would lay scientific foundation for their utilization in food and nutrition industry.

Condensed tannins from Ficus virens as tyrosinase inhibitors: structure, inhibitory activity and molecular mechanism.

Condensed tannins from Ficus virens leaves, fruit, and stem bark were isolated and their structures characterized by 13C nuclear magnetic resonance spectrometry, high performance liquid chromatography electrospray ionization mass spectrometry, and matrix-assisted laser desorption/ionization time-of-flight mass spectrometry. The results showed that the leaves, fruit, and stem bark condensed tannins were complex mixtures of homo- and heteropolymers of B-type procyanidins and prodelphinidins with degrees of polymerization up to hexamer, dodecamer, and pentadecamer, respectively. Antityrosinase activities of the condensed tannins were studied. The results indicated that the condensed tannins were potent tyrosinase inhibitors. The concentrations for the leaves, fruit, and stem bark condensed tannins leading to 50% enzyme activity were determined to be 131.67, 99.89, and 106.22 µg/ml on monophenolase activity, and 128.42, 43.07, and 74.27 µg/ml on diphenolase activity. The inhibition mechanism, type, and constants of the condensed tannins on the diphenolase activity were further investigated. The results indicated that the condensed tannins were reversible and mixed type inhibitors. Fluorescence quenching, copper interacting, and molecular docking techniques were utilized to unravel the molecular mechanisms of the inhibition. The results showed that the hydroxyl group on the B ring of the condensed tannins could chelate the dicopper irons of the enzyme. Moreover, the condensed tannins could reduce the enzyme product o-quinones into colourless compounds. These results would contribute to the development and design of antityrosinase agents.

Isolation and purification of condensed tannins from flamboyant tree and their antioxidant and antityrosinase activities.

Flamboyant tree, a kind of medicinal plant, was studied as a source of condensed tannins. The antioxidant activities of the condensed tannins from the leaf, fruit, and stem bark of flamboyant tree were screened by ABTS radical and hydroxyl radical scavenging activity methods. The results indicated that these compounds possessed potent antioxidant activity. Their structures were then characterized by high-performance liquid chromatography-electrospray ionization mass spectrometry (HPLC-ESI-MS) after thiolytic degradation. The results showed that the leaf condensed tannins were composed of afzelechin/epiafzelechin, catechin/epicatechin, and gallocatechin/epigallocatechin, while the fruit and stem bark condensed tannins had afzelechin/epiafzelechin and catechin/epicatechin. In addition, the condensed tannins were evaluated for their antityrosinase ability. They were found to have significant antityrosinase activity. The IC50 values were 35 ± 2.0 and 40 ± 0.5 µg/ml for the condensed tannins of fruit and stem bark, respectively. Further, fluorescence quenching and copper interacting techniques were utilized to unravel the molecular mechanisms of the inhibition. The results showed that the hydroxyl group of the condensed tannins could chelate the dicopper center of the enzyme and interact with tryptophan residues. Our studies revealed that condensed tannins might be suitable for use in food, agriculture, cosmetic, nutraceutical, and pharmaceutical applications.

Structural analysis of proanthocyanidins isolated from fruit stone of Chinese hawthorn with potent antityrosinase and antioxidant activity.

Proanthocyanidins were isolated from fruit stone of Chinese hawthorn (Crataegus pinnatifida Bge. var. major N.E.Br.). Their structures were analyzed and elucidated by methods of matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS) and high performance liquid chromatography electrospray ionization mass spectrometry (HPLC-ESI-MS). The results demonstrated that these compounds are complicated mixtures of homo- and heteropolymers consisting of procyanidin/procyanidin gallate and prodelphinidin. They possessed structural heterogeneity in monomer units, polymer length, and interflavan linkage (A-type and B-type). Their antityrosinase and antioxidant activity were then investigated. The results revealed that they can inhibit tyrosinase activities, including the monophenolase activity and the diphenolase activity. In addition, proanthocyanidins possessed potent antioxidant activity. Our studies revealed that proanthocyanidins isolated from fruit stone of Chinese hawthorn may be applied in food, agriculture, pharmaceutical, and cosmetic industries.

Reversible and competitive inhibitory kinetics of amoxicillin on mushroom tyrosinase.

In the present work, we investigated the inhibitory effects of amoxicillin, a bacteriolytic ß-lactam antibiotic drug, on the rate of monophenol hydroxylation and o-diphenol oxidation catalyzed by mushroom tyrosinase. The results showed that amoxicillin could inhibit both monophenolase and diphenolase activities. For monophenolase activity, the inhibition on reaction rate was dose-dependent, while the influence on lag period was not obvious. For diphenolase activity, amoxicillin was found to be a reversible inhibitor, with an IC50 value of 9.0 ± 1.8 mM. Kinetics analysis showed that amoxicillin was a mixed type inhibitor of the enzyme with KI and KIS values of 8.30 mM and 44.79 mM, respectively. Further, the molecular mechanism underlying the inhibition of tyrosinse by amoxicillin was investigated by means of fluorescence quenching and molecular docking techniques. The results showed that amoxicillin could form static interaction with the catalytic pocket of the enzyme through the interaction of amoxicillin with the dicopper irons and amino acid residues in the enzyme active center. Our results contributed to the usage of amoxicillin as a potential tyrosinase inhibitor in the field of medicinal industry and could also provide guidance in the design of novel tyrosinase inhibitors.