Article
Food Science & Technology
Bei Liu, Jinyu Yang, Jiatong Hao, Haifeng Xie, Kuniyoshi Shimizu, Renshi Li, Chaofeng Zhang
Summary: Mogrol from Siratia grosvenorii demonstrated anti-fibrotic effects by suppressing TGF-beta 1 pathway, restoring NOX4 expression, and promoting AMPK phosphorylation. The protective effect against lung fibrosis may be attributed to the activation of AMPK and amelioration of TGF-beta 1 signalling pathway.
JOURNAL OF FUNCTIONAL FOODS
(2021)
Article
Multidisciplinary Sciences
Kwadwo A. Opoku-Nsiah, Andres H. de la Pena, Sarah K. Williams, Nikita Chopra, Andrej Sali, Gabriel C. Lander, Jason E. Gestwicki
Summary: The study reveals the sequence preferences and gate-opening mechanisms of the human 20S proteasome (h20S). It shows that the recognition sequence of h20S is different from the archaeal system and is defined as the Y-F/Y (Y Phi) motif. The Y Phi sequence preferences can be tuned by valency, allowing multivalent proteasome activators to explore a greater sequence space. These findings expand the understanding of termini-mediated gating and provide insights for the design of h20S activators.
NATURE COMMUNICATIONS
(2022)
Article
Chemistry, Medicinal
Siming Wu, Zhihong Xiao, Junling Wei, Lei Zhang, Yuanyuan Cao, Zhuo Chen, Qianbin Li, Gaoyun Hu
Summary: A series of imidazo[1,2-a]pyridines were designed and synthesized as AMPK activators. The active compound showed good enzyme activation and hydrogen bonding interactions with key amino acids in the active site. It also demonstrated the ability to reduce ROS levels and increase p-AMPK and p-ACC levels in cells, while decreasing TGF-beta 1 levels. These findings provide new lead compounds for drug development.
Article
Chemistry, Medicinal
Jing-Ru Song, Na Li, Dian-Peng Li
Summary: Novel derivatives based on mogrol were designed and synthesized to improve anti-lung cancer activity, with compound 8f showing the strongest cytotoxicity against A549 cells by inhibiting STAT3 phosphorylation and compound 10a significantly enhancing cytotoxicity against NCI-H460 cells. This study suggests the potential development of therapeutic agents for lung cancer from natural mogrol.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Medicinal
Yuusuke Tamura, Ippei Morita, Yu Hinata, Eiichi Kojima, Yoshikazu Sasaki, Toshihiro Wada, Mutsumi Asano, Masahiko Fujioka, Yoko Hayasaki-Kajiwara, Takanori Iwasaki, Kenichi Matsumura
Summary: Diabetes is a global healthcare problem and targeting AMPK can be a potential treatment. However, finding direct AMPK activators with high potency for the 132-AMPK isoform and suitable chemical structure is challenging. In this study, we successfully designed a novel activator 14d which showed high in vitro potency, good pharmacokinetic profiles, and dose-dependent blood-glucose-lowering effects in a diabetic animal model. Chronic activation of AMPK with 14d also led to dose-dependent reduction in HbA1c.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Chemistry, Medicinal
Yuusuke Tamura, Ippei Morita, Yu Hinata, Eiichi Kojima, Hiroki Ozasa, Hidaka Ikemoto, Mutsumi Asano, Toshihiro Wada, Yoko Hayasaki-Kajiwara, Takanori Iwasaki, Kenichi Matsumura
Summary: AMP-activated protein kinase (AMPK) plays an important role in exercise-induced metabolic benefits. Activation of AMPK has been explored as a strategy for treating metabolic disorders, such as type 2 diabetes. Existing AMPK activators with different chemical structures have been reported, but direct activators for specific isoforms are limited. The newly designed 4-azaindole derivative 16g showed promising in vitro activity and demonstrated dose-dependent improvements in HbA1c and hepatic lipid accumulation in a diabetic animal model.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Chemistry, Multidisciplinary
Xiaoyu Hu, Chan Liu, Kaichun Wang, Lanxue Zhao, Yu Qiu, Hongzhuan Chen, Jiangmiao Hu, Jianrong Xu
Summary: This study discovered that both alpha-M and its derivative Zcbd-3 had similar effects in anti-Alzheimer's disease. The results also indicated that the 3-methyl-2-butenyl group at C-8 is important for the bioactivity of alpha-M, and modification of the double hydroxylation at the C-2 position may improve its anti-AD effects.
FRONTIERS IN CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Denis A. Babkov, Olga N. Zhukovskaya, Anastasia A. Brigadirova, Diana R. Prilepskaya, Alexandra A. Kolodina, Abbas Haider S. Abbas, Anatolii S. Morkovnik, M. Elizabeth Sobhia, Ketan Ghosh, Alexander A. Spasov
Summary: This study describes the synthesis of a series of hydrobromides of N-(4-biphenyl)methyl-N'-dialkylaminoethyl-2-iminobenzimidazoles, which are considered as bi-privileged structures due to the presence of two privileged structural fragments. Compound 7a was shown to activate AMP-activated kinase (AMPK) and simultaneously inhibit protein tyrosine phosphatase 1B (PTP1B) with similar potency, making it an interesting prototype of potential antidiabetic agents with a dual-target mechanism of action. Through proof of concept in vivo study, it was demonstrated that the dual-targeting compound 7a has a disease-modifying effect in a rat model of type 2 diabetes mellitus by improving insulin sensitivity and lipid metabolism.
CHEMICAL BIOLOGY & DRUG DESIGN
(2023)
Article
Biochemistry & Molecular Biology
Na Li, Jingru Song, Dianpeng Li
Summary: By modifying the mogrol core with ester derivatives, the antiproliferative activity against human cancer cells was significantly enhanced, with some derivatives showing even higher activity than the positive drug. The cytotoxicity of certain derivatives was much more potent than the control drug, indicating promising anticancer potential.
CHEMISTRY & BIODIVERSITY
(2022)
Article
Biochemistry & Molecular Biology
Jian Zhang, Keman Mu, Peng Yang, Xinqian Feng, Di Zhang, Xiangyu Fan, Qiantao Wang, Shengjun Mao
Summary: The study found that electron-donating methoxy groups on the 3,4,5 position of the phenyl ring enhanced the antiepileptic effects, while other groups at different positions decreased activity. Additionally, either an allyl or a 1-butenyl group in conjunction with the benzene ring showed optimal activity in the allyl moiety. Compounds 5 and 19 exhibited better neuroprotective effects against epilepsy in both in vitro and in vivo models.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Kevin M. Gayler, Jeremy M. Quintana, Jordan Mattke, Michael A. Plunk, Jessica H. Kostyo, Johann W. Karunananthan, Harold Nguyen, Mina Shuda, Liam D. Ferreira, Hannah Baker, Alexandra L. Stinchcomb, Iraida Sharina, Robert R. Kane, Emil Martin
Summary: Previous studies have shown that the anti-hyperlipidemic drug gemfibrozil can activate the NO receptor soluble guanylyl cyclase independently of NO and heme. New gemfibrozil derivatives were synthesized and evaluated for sGC activation, identifying positions in gemfibrozil's structure that are important for activation. Compounds 7c and 15b were found to be more potent activators of purified sGC's cGMP-forming activity compared to gemfibrozil, showing enhanced relaxation of preconstricted mouse thoracic aorta rings. These findings provide insights for further optimization of sGC activators based on the gemfibrozil scaffold.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Nermin S. S. Ahmed, Heba E. E. El-Nakib, Marian M. M. Ramsis, Nouran O. O. Albably, Jannette Wober, Jan J. J. Weigand, Kai Schwedtmann, Oliver Zierau, Ashraf H. H. Abadi
Summary: This study presents a new class of potent Tamoxifen (TAM) analogues with both anticancer and antiviral activity, without increasing the risk of uterine cancer.
Article
Biochemistry & Molecular Biology
Jun Sato, Hiroki Kusano, Toshiaki Aoki, Satoru Shibuya, Katsuki Yokoo, Kazuo Komano, Takuya Oguma, Shuhei Matsumoto, Takafumi Sato, Kazuya Yasuo, Kenji Yamawaki
Summary: A series of tricyclic beta-lactams were synthesized and evaluated for antibacterial activities against carbapenem-resistant Enterobacterales (CBEs). Introducing sulfoxide resulted in potent antibacterial activities and strong therapeutic efficacy in a neutropenic mouse lung infection model. The tricyclic beta-lactam skeleton may serve as a promising scaffold for new antibacterial agents against CREs.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Applied
Wen Xu, Jiaying Li, Jia Chen, Jialin Xu, Dan Zheng, Mengxia Wu, Yu Mu, Xueshi Huang, Liya Li
Summary: This study investigated the chemical characteristics and hypolipidemic effects of alkylphenols in the fruit of Syzygium jambos. Cardanols and alkylresorcinols were isolated and identified, and cardanols were found to suppress lipids accumulation and reduce triglyceride content via the activation of AMPK/PPARα signaling pathways. Furthermore, the distribution of cardanols in mice after oral intake was studied. The findings highlight the potential usage of cardanols and Syzygium jambos fruit for the management of dyslipidemia.
Article
Immunology
Renquan Zhang, Hui Liang, Gaoli Liu, Wanli Jiang, Zheng Tang, Qinglu Fan, Zhihao Nie, Haifeng Hu, Ganjun Kang, Songping Xie
Summary: This study found that Nesfatin-1 has significant protective effects against pulmonary fibrosis by blocking the TGF-beta 1/Smad pathway in an AMPKa-dependent manner.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2023)
Article
Construction & Building Technology
Bing Cui, Huanling Wu, Canhui Zhao, Jiaping Liu, Zhiming Guo
Summary: Nanjing Jiangxinzhou Yangtze River Bridge is an innovative cable-stayed bridge in China with a unique steel-concrete composite structure. With the use of new materials, such as coarse aggregate reactive powder concrete, it has significantly improved the manufacturing speed and performance of the bridge, making significant contributions to the development of cable-stayed bridges.
STRUCTURAL ENGINEERING INTERNATIONAL
(2023)
Article
Construction & Building Technology
Yang Zhou, Yuan Chen, Ming Jin, Jiaping Liu, Changwen Miao
Summary: In this study, molecular dynamics simulations were used to investigate the effects of irradiation on cementitious materials. The results showed that irradiation led to a transformation in structure and a reduction in mechanical performance of calcium silicate hydrates. Additionally, an increase in ductility was observed, which could be beneficial for designing more radiation-resistant cement materials.
JOURNAL OF SUSTAINABLE CEMENT-BASED MATERIALS
(2023)
Article
Clinical Neurology
Shuiwei Xia, Yajie Wang, Xianli Lv, Chunmiao Chen, Junguo Hui, Xulu Wu, Zufei Wang, Huijun Chen, Jiansong Ji
Summary: This study compared the abilities of vessel wall magnetic resonance imaging techniques, SNAP sequence and T1-weighted volumetric isotropic turbo spin echo acquisition (T1-w VISTA) sequence, in evaluating cervical artery dissection (CAD). The results showed that both SNAP and T1-w VISTA sequences had the same diagnostic performance in CAD diagnosis, and their consistencies with the final diagnosis were good. Additionally, SNAP showed better intramural hematoma (IMH)-wall contrast than T1-w VISTA.
INTERVENTIONAL NEURORADIOLOGY
(2023)
Article
Green & Sustainable Science & Technology
Gang Liu, Zhitao Han, Jiawei Li, Zhen Wang, Shaosi Cheng, Yubin Liu, Jing Yu, Xinxiang Pan
Summary: A novel method for removing pre-oxidized NOx using Na2SO3/THS composite solution is proposed in this study, aiming to achieve high NOx absorption efficiency and low nitrate concentration in scrubbed wastewater simultaneously.
ENVIRONMENTAL PROGRESS & SUSTAINABLE ENERGY
(2023)
Article
Environmental Sciences
Nianping Chi, Jiajun Liu, Minghua Lei, Li Feng
Summary: The introduction of amphiphilic CPAM TP-ADB with cationic microblock structure and hydrophobic association improves the dewatering performance of PD sludge.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2023)
Article
Environmental Sciences
Jiawei Li, Guoqiang Song, Zhenzhen Mu, Xiaoou Lan, Fan Yang, Lin Li, Xiuping Han
Summary: Several studies have shown a relationship between short-term exposure to air pollution and worsening of certain skin conditions. This study in Shenyang, China, from 2016 to 2018, expands on these findings by exploring the potential association between exposure to air pollutants including particulate matter, sulfur dioxide, and ozone and the incidence of acute and chronic urticaria. The results suggest that short-term exposure to ozone, PM2.5, and PM10 can increase the risk of acute and chronic urticaria.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2023)
Article
Oncology
Honghui Zhao, Dan Li, Jiayin Liu, Xinliang Zhou, Jing Han, Long Wang, Zhisong Fan, Li Feng, Jing Zuo, Yudong Wang
Summary: This study analyzed the characteristics of gut microbes in lung cancer patients and found that the differences in gut microbes are related to the effectiveness of anti-PD-1 therapy combined with chemotherapy. In particular, Bifidobacterium breve was identified as a potential biomarker for predicting efficacy.
Article
Chemistry, Applied
Niuniu Cui, Jiawei Li, Ziwen Xie, Xiaofei Yan, Dongming Qi
Summary: The study introduces a novel pigment dyeing technology that uses charge attractions between cationic nanoscale pigment and cotton fabrics. This technology offers advantages such as no salt, recyclable dyebath, high uptake, and good wet fastness. The research explores the synthesis of cationic copolymer nanoparticle dispersants and the preparation of nanoscale pigment dispersion. The results demonstrate the excellent dispersion performance and colloid stability of the nanoscale pigment dispersion, as well as the higher coloring intensity and color fastness achieved in the dyeing of cotton fabrics. The recyclability of the dyebath significantly reduces dyeing effluent discharge, providing a promising and ecologically sustainable dyeing technology for cotton fabrics.
Article
Environmental Sciences
Hongyi Wu, Ling Xie, Yuchen Wu, Liwei Chen, Bian Jiang, Xiaohai Chen, Yinglin Wu
Summary: This study investigated the accumulation of total petroleum hydrocarbons (TPHs) on the coast of Leizhou Peninsula in Southern China. Land-based discharge, sea traffic, and sediment type were found to significantly influence TPHs distribution. The concentration of TPHs increased by 1.036 μg/g with the addition of one more boat on the wharf. 'Blue Carbon' ecosystems, such as mangroves, were more severely polluted. Cleaner production policies should be implemented to mitigate TPHs discharge from coastal areas.
MARINE POLLUTION BULLETIN
(2023)
Article
Engineering, Multidisciplinary
Jun Li, Jia Wei Li, Jia Rui Zhang, Kuo Li, Tian Ma, Wei Feng Wang, Xiao Wei Zhai, William N. MacPherson, Robert R. J. Maier, Duncan P. Hand
Summary: In this paper, we demonstrate the design and fabrication of 45 degrees micro-mirrors using focused ion beam (FIB) processing. The mirrors are accurately aligned with optical fibre cores, eliminating the need for alignment of external turning mirror components. Experimental results show that the fabricated structure is capable of measuring two-axis acceleration with a linear response range of 0.2 to 4 g and an rms. error of 0.03 g. Frequency response up to 700 Hz and cross-sensitivity of approximately 4.3% are also demonstrated.
MEASUREMENT SCIENCE AND TECHNOLOGY
(2023)
Article
Spectroscopy
Qi Xiao, Huajian Luo, Huishan Cao, Bo Li, Jiajia Liu, Yi Liu, Shan Huang
Summary: Ti3C2 quantum dots were synthesized and successfully applied for fluorescent imaging of living cells. The binding interaction between Ti3C2 QDs and trypsin was comprehensively studied using spectroscopic strategies and molecular modeling technique. The results show that Ti3C2 QDs can quench the intrinsic fluorescence of trypsin and significantly inhibit its enzymatic activity on human serum albumin and cells.
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
(2023)
Article
Spectroscopy
Ling Lin, Meiling Fan, Muhammad Ijaz, Leiyang Cheng, Gang Li
Summary: In the LED multi-spectral imaging (LEDMSI) system, modulation using square wave frequency division with a frequency ratio of 2 can improve image quality and acquisition speed, but it occupies a wide frequency band. This paper proposes a modulation method using multiple square wave signals with different phases as carrier signals to solve the above problems. Experimental results show that the proposed method improves the quality of multi-spectral images, indicating its significance in improving the performance of the LEDMSI system.
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
(2023)
Article
Computer Science, Artificial Intelligence
Yiyang Liu, Hua Dai, Jiawei Li, Yu Chen, Geng Yang, Jun Wang
Summary: This paper proposes a BP-Model-based convoy mining algorithm that optimizes mining by adopting the divide-and-conquer methodology. The performance of the algorithms is evaluated on real-world datasets, showing that they are more efficient than existing convoy mining algorithms.
EXPERT SYSTEMS WITH APPLICATIONS
(2023)
Article
Nanoscience & Nanotechnology
Jia-Wei Li, Jian-Gang Guo, Li-Jun Zhou
Summary: Many studies have shown that the nanotwinned structure and graphene reinforcing phase can improve the mechanical properties of aluminum. However, the synergistic effect of the two on the strengthening and toughening mechanisms of aluminum matrix composites has rarely been reported. In this work, molecular dynamics simulations are used to study the mechanical properties and microscopic deformation mechanisms of graphene/nanotwinned aluminum matrix composites. The effects of graphene distribution patterns, twin boundaries (TBs), their angles, and the number of graphene layers on the mechanical behaviors of the composites are analyzed.
PHYSICA E-LOW-DIMENSIONAL SYSTEMS & NANOSTRUCTURES
(2023)
Article
Computer Science, Artificial Intelligence
Xiang Shi, Yinpeng Liu, Jiawei Liu, Qikai Cheng, Wei Lu
Summary: Scientific papers are crucial for academic communication, but many of them lack in-depth research and present core content ambiguously, hindering the progression of science and technology. To address this challenge, the INTEGrity vERification (INTEGER) task is introduced to help researchers assess the integrity of their papers and verify the clarity of each knowledge unit. A multi-task learning model utilizing Tucker decomposition and span-level attention mechanism is proposed to accurately identify terms and their integrity. Experimental results show the effectiveness of the model.
EXPERT SYSTEMS WITH APPLICATIONS
(2024)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
