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Virtual screening and optimization of typeⅡ inhibitors of JAK2 from a natural product library

中国药理学与毒理学杂志 2015年第S1期29卷 98-99页

作者： Dik-LungMA DanielShiu-HinCHAN GuoWEI Hai-jingZHONG HuiYANG LaiToLEUNG ElizabethA.GULLEN PaulineChIU Yung-ChiCHENG Chung-hangLEUNG Department of Chemistry Hong Kong Baptist University Hong Kong China Department of Chemistry and the State Key Laboratory of Synthetic Chemistry University of Hong Kong Hong Kong China State Key Laboratory of Quality Research in Chinese Medicine Institute of Chinese Medical Sciences University of Macao Macao China Department of Pharmacology Yale University School of Medicine New Haven CT 06520 USA

OBJECTIVE To utilize a structure-based lead optimization approach to generate novel natural product-like typeⅡ inhibitors of JAK2 using the DOLPHIN protocol.METHODS Initially,the DOLHPIN computational protocol was employed to convert an active(DFG-in)conformation of JAK2 into a typeⅡ-compatible conformation,which was used as a model for the structure-based virtual screening of 150 000 natural product-like compounds in silico.The novel biflavonoid analogues were designed and synthesized based on the structure of lead compound and then tested for JAK2 and STAT3 inhibitory activity,cytotoxicity and HCV antiviral activity.RESULTS The top eleven highest-scoring compounds were generated from the initial high-throughput virtual screening.Amentoflavone 1a,a biflavonoid from the Chinese plant Gingko biloba,emerged as a promising candidate for further biological evaluation.In dose-response experiments,amentoflavone 1ainhibited JAK2 activity in a concentration dependent fashion with an IC50 value of 5μmol·L-1.As a proof-of-concept,we designed nine analogues 1b-1j with the addition of one or more aliphatic side chains to the biflavonoid scaffold of 1a.The octyl(C8)analogue 1bdisplayed superior potency against JAK2 activity and HCV activity compared to the parent compound 1a,validating the structure-based lead optimization approach used in this study.Moreover,kinetic analysis indicated that analogue 1bexhibited a non-competitive mode of inhibition,suggesting that this compound may be a putative typeⅡ inhibitor of JAK2.CONCLUSION Amentoflavone 1ahas been identified as a JAK2 inhibitor by structure-based virtual screening of a natural product library.In silico optimization using the DOLPHIN model yielded analogues with enhanced potency against JAK2 activity and HCV activity in cellulo.Molecular modeling and kinetic experiments suggested that the analogues may function as typeⅡ inhibitors of JAK2.

关键词： JAK2 natural products virtual screening structure-

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Integrative Medicine Demonstrates Advantage in COVID-19 Treatment

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Chinese Journal of Integrative Medicine 2020年第11期26卷 805-805,804页

作者： yung-Chi Cheng Henry Bronson Professor of Pharmacology Yale University Chairman and Founder of Consortium for the Globalization of Chinese Medicine

In December 2019,a cluster of patients in Wuhan,China with a new type of pneumonia with unknown etiology were found.The origin was subsequently discovered to be an infectious disease caused by a new coronavirus,SARS-C... 详细信息

关键词： Medicine etiology patients

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Effects of areca nut consumption on cell differentiation of osteoblasts, myoblasts, and fibroblasts

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BIOCELL 2023年第2期47卷 283-287页

作者： yung-FU CHANG Department of Biomedical Science and Environmental Biology Kaohsiung Medical UniversityKaohsiung807Taiwan Department of Medical Research Kaohsiung Medical University HospitalKaohsiung807Taiwan Translational Research Center of Neuromuscular Diseases Kaohsiung Medical University HospitalKaohsiung807Taiwan

Areca nut is used worldwide as a hallucinogenic addicting drug along the tropical belt.Arecoline,a toxic compound,is the most important alkaloid in areca nuts.The adverse effects of oral uptake and chewing of areca nut are well known.For example,the possibility of cancer caused by chewing areca nuts is widely discussed.Chewing areca nut has other adverse effects on other organs,including abnormal cell differentiation,oral cancer,and several other diseases.The use of areca nut is also associated with low birthweight.Skeletal musculature is the largest organ in the body and is attached to the bones.During embryo development,the differentiation of bone and muscle cells is critical.In this article,we reviewed the effects of areca nut and arecoline on embryonic cell differentiation,particularly osteoblasts,myoblasts,and fibroblasts.

关键词： Areca nut Cell differentiation Osteoblast Myoblast Fibroblast

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Hair growth-promotion effects and antioxidant activity of the banana flower extract HappyAngel^(■):double-blind, placebo-controlled trial

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Food Science and Human Wellness 2023年第5期12卷 1917-1923页

作者： Chia-Hua Liang yung-Hsiang Lin yung-Kai Lin Chi-Fu Chiang Department of Cosmetic Science and Institute of Cosmetic Science Chia Nan University of Pharmacy and ScienceTainan 71710China Research&Design Center TCI CO.Ltd.Taipei 114722China Institute of Food Safety and Risk Management Department of Food ScienceTaiwan Ocean UniversityKeelung 202301China Graduate Institute of Biomedical Engineering Chung Hsing UniversityTaichung 202301China

Banana flowers contain various bioactive components, including several antioxidants with anti-inflammatory effects. However, it is unclear whether they can reduce and prevent hair loss. This study examines the effect of banana flower extracts on preventing hair loss and strengthening hair roots. The banana flower extract(HappyAngel^(■))was used to treat human hair follicle dermal papilla cells(HFDPCs)and the expression of reactive oxygen species(ROS), dihydrotestosterone(DHT), and hair-related genes(SRD5A1, SRD5A2, AR, and KROX20)were monitored. Fifty subjects were divided into a placebo group and a banana flower group. The experimental group consumed banana flower extract daily for twelve weeks and then underwent hair testing, hair-related genes analysis, collection of hair loss, and questionnaires. The results showed that the banana flower extract significantly increased hair cell growth and decreased the expression of ROS, DHT, and hair follicle growth inhibition-related SRD5A1, SRD5A2, and AR genes, and significantly increased the expression of hair growth-related KROX20 gene in HFDPCs. Consuming banana flower extract for twelve weeks increased the hair root diameter and reduced hair loss and scalp redness compared to the placebo group. Thus, banana flower extract(HappyAngel^(■))can stimulate hair growth and inhibit the activation of hair loss genes.

关键词： Banana flower Dihydrotestosterone Hair loss ROS Follicle dermal papilla cells

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Sensitivity and specificity of hearing tests for screening hearing loss in older adults

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Journal of Otology 2023年第1期18卷 1-6页

作者： Hsin-Chen Ting yung-Yao Huang PSA Charitable Foundation New Taipei CityTaiwanChina Department of Audiology and Speech-Language Pathology MacKay Medical CollegeNew Taipei CityTaiwanChina

Objectives: The study aimed to determine the most appropriate hearing screening test to identify disabling hearing loss for adults aged 65 years or older.Methods: This study included 577 older adults. Four hearing screening tests were considered in the study, including the Hearing Handicap Inventory for Elderly Screening(HHIE-s), three single question tests, the whisper test, and the finger rub test. The sensitivity and specificity of these tests referenced to the hearing threshold of disabling hearing loss were estimated.Results: Among all tests, only the single self-perception question(0.7064 for sensitivity;0.7225 for specificity) and whisper test(0.7833 for sensitivity;0.7708 for specificity) could obtain both sensitivity and specificity higher than 70% for adults aged ≥65 years.Conclusion: Overall, we suggest using the whisper test to identify disabling hearing loss(>40 dB HL at the better ear) for adults aged 65 years or older. However, if the conditions do not permit, the single selfperception question is also acceptable. Moreover, HHIE-s might not be a good test to detect disabling hearing loss for adults aged 80 years or older.

关键词： Sensitivity and specificity Hearing screening Questionnaire Whisper test Finger rub test

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Quantum supremacy: some fundamental concepts

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National Science Review 2019年第1期6卷 22-23页

作者： Man-Hong yung Shenzhen Institute for Quantum Science and Engineering and Department of Physics Southern University of Science and Technology Shenzhen Key Laboratory of Quantum Science and Engineering Southern University of Science and Technology

Quantum computation was envisioned by Feynman as a valuable means of solving quantum problems [1]. The question is, how do we prove the superiority of quantum computing over classical devices? A common misconception in describing the power of a quantum computer over a classical computer is that quantum bits can be prepared in a superposition of an exponential number of states, which cannot be achieved with classical bits. This statement is certainly true, but it does not tell us, specifically,what problems quantum computers can

关键词： Quantum supremacy some fundamental concepts

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Honokiol attenuates oxidative stress-induced cytotoxicity in human keratinocytes via activating AMPK signaling

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Asian Pacific Journal of Tropical Biomedicine 2021年第5期11卷 222-230页

作者： yung Hyun Choi Anti-Aging Research Center Dong-eui UniversityBusan 47340Republic of Korea Department of Biochemistry College of Korean MedicineDong-eui UniversityBusan 47227Republic of Korea

Objective:To investigate the effect of honokiol on oxidative damage in HaCaT human keratinocytes.Methods:HaCaT cells were exposed to hydrogen peroxide(H_(2)O_(2)),following pretreatment with various concentrations of honokiol.The alleviating effects of honokiol on HaCaT cell viability and cell death,reactive oxygen species(ROS)production,DNA damage,mitochondrial dynamics,and inhibition of adenosine triphoaphate production against H_(2)O_(2)were investigated.Western blotting analysis was used to analyze the expression levels of specific proteins.Results:Honokiol suppressed H_(2)O_(2)-induced cytotoxicity and DNA damage by blocking abnormal ROS accumulation.Honokiol also prevented apoptosis by inhibiting loss of mitochondrial membrane potential and release of cytochrome c from the mitochondria into the cytosol,decreasing the Bax/Bcl-2 ratio,and reducing the activity of caspase-3 in H_(2)O_(2)-stimulated HaCaT cells.In addition,honokiol attenuated H_(2)O_(2)-induced reduction of adenosine triphosphate content,and activation of AMP-activated protein kinase(AMPK)was markedly promoted by honokiol in H_(2)O_(2)-stimulated cells.Importantly,the anti-apoptosis and anti-proliferative activity of honokiol against H_(2)O_(2)was further enhanced by adding an activator of AMPK,indicating that honokiol activated AMPK in HaCaT keratinocytes to protect against oxidative damage.Conclusions:The present results indicate that honokiol may be useful as a potential therapeutic agent against various oxidative stress-related skin diseases.

关键词： Honokiol ROS DNA damage Apoptosis AMPK

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A new biomimicry marine current turbine: Study of hydrodynamic performance and wake using software OpenFOAM

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Journal of Hydrodynamics 2016年第1期28卷 125-141页

作者： yung-Jeh CHU Department of Civil Engineering Faculty of Engineering University of Malaya

Inspired by Dryobalanops aromatica seed, a new biomimicry marine current turbine is proposed. Hydrodynamic performance and wake properties are two key factors determining whether a new marine current turbine design is practical or not. Thus, a study of hydrodynamic performance and wake of the proposed biomimicry turbine is conducted. The computational fluid dynamics（CFD） software, Open FOAM is used to generate the required results for the mentioned study. The hydrodynamic performance and wake properties of the proposed biomimicry turbine is compared to two conventional turbines of Bahaj et al. and Pinon et al. respectively. The simulation results showed that the proposed biomimicry marine current turbine gives optimum power output with its power coefficient, 0.376 PC ≈ at the tip speed ratio（TSR） of 1.5. Under the same boundary conditions, the maximum torque produced by the proposed biomimicry turbine at zero rotational speed is 38.71 Nm which is 1110% greater than the torque generated by the turbine of Bahaj et al.. The recovery distance for the wake of the biomimicry turbine is predicted to be 10.6% shorter than that of IFREMER-LOMC turbine. The above-mentioned results confirm the potential application of the proposed biomimicry marine current turbine in the renewable energy industry.

关键词： marine current turbine wake biomimicry computational fluid dynamics（CFD） Open FOAM

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Generating Synthetic Data to Reduce Prediction Error of Energy Consumption

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Computers, Materials & Continua 2022年第2期70卷 3151-3167页

作者： Debapriya Hazra Wafa Shafqat yung-Cheol Byun Department of Computer Engineering Jeju National UniversityJeju-siKorea

Renewable and nonrenewable energy sources are widely incorporated for solar and wind energy that produces electricity without increasing carbon dioxide emissions.Energy industries worldwide are trying hard to predict future energy consumption that could eliminate over or under contracting energy resources and unnecessary financing.Machine learning techniques for predicting energy are the trending solution to overcome the challenges faced by energy companies.The basic need for machine learning algorithms to be trained for accurate prediction requires a considerable amount of data.Another critical factor is balancing the data for enhanced prediction.Data Augmentation is a technique used for increasing the data available for training.Synthetic data are the generation of new data which can be trained to improve the accuracy of prediction models.In this paper,we propose a model that takes time series energy consumption data as input,pre-processes the data,and then uses multiple augmentation techniques and generative adversarial networks to generate synthetic data which when combined with the original data,reduces energy consumption prediction error.We propose TGAN-skip-Improved-WGAN-GP to generate synthetic energy consumption time series tabular data.We modify TGANwith skip connections,then improveWGANGPby defining a consistency term,and finally use the architecture of improved WGAN-GP for training TGAN-skip.We used various evaluation metrics and visual representation to compare the performance of our proposed model.We also measured prediction accuracy along with mean and maximum error generated while predicting with different variations of augmented and synthetic data with original data.The mode collapse problemcould be handled by TGAN-skip-Improved-WGAN-GP model and it also converged faster than existing GAN models for synthetic data generation.The experiment result shows that our proposed technique of combining synthetic data with original data could significantly reduce the prediction error rate and increase the p

关键词： Energy consumption generative adversarial networks synthetic data time series data TGAN WGAN-GP TGAN-skip prediction error augmentation

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Unraveling Iterative Control Structures from Business Processes

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Journal of Computer Science & Technology 2021年第1期36卷 158-190页

作者： Yain-Whar Si Weng-Hong yung Department of Computer and Information Science University of MacaoMacaoChina

Iterative control structures allow the repeated execution of tasks,activities or sub-processes according to the given conditions in a process model.Iterative control structures can significantly increase the risk of triggering temporal exceptions since activities within the scope of these control structures could be repeatedly executed until a predefined condition is met.In this paper,we propose two approaches to unravel iterative control structures from process models.The first approach unravels loops based on zero-one principle.The second approach unravels loops based on branching probabilities assigned at split gateways.The proposed methods can be used to unfold structured loops,nested loops and crossing loops.Since the unfolded model does not contain any iterative control structures,it can be used for further analysis by process designers during the modeling phase.The proposed methods are implemented based on workflow graphs,and therefore they are compatible with modeling languages such as Business Process Modelling Notation(BPMN).In the experiments,the execution behavior of unfolded process models is compared against the original models based on the concept of runs.Experimental results reveal that runs generated from the original models can be correctly executed in the unfolded BPMN models that do not contain any loops.

关键词： business process management iterative control structure unravelling zero-one principle branching probability

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