Frontiers in Pharmacology
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2026
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IF 5.4
Yanqing Wu,Xilin Qiao,Shuaiyu Chen,Yalan Lu,Bingyan Mao,Mengdie Zhu,Xinzhi Chen,Nipi Chen,Zhishan Ding,Bo Jin
Introduction MicroRNA-29b-3p (miR-29b-3p) plays a critical role in regulating endothelial apoptosis and autophagy. We previously demonstrated that protocatechualdehyde (PCA), a water-soluble phenolic acid derived from Salvia miltiorrhiza Bge., protects human umbilical vein endothelial cells (HUVECs) against oxygen-glucose deprivation/reoxygenation (OGD/R)-induced injury. However, whether miR-29b-3p mediates this protective effect remains unclear. Methods Using the OGD/R in vitro model of ischemia-reperfusion injury, we investigated the molecular mechanisms underlying ischemic damage at the cellular level. RT-qPCR was used to measure miR-29b-3p expression, Western blotting to assess autophagy- and apoptosis-related proteins, and MDC staining and flow cytometry to evaluate autophagy and apoptosis, respectively. Results The results showed that miR-29b-3p was downregulated in OGD/R-treated HUVECs, an effect that was reversed by PCA and the ROS inhibitor N-acetylcysteine (NAC). The miR-29b-3p mimic enhanced the promoting effects of PCA and NAC on miR-29b-3p expression, whereas miR-29b-3p inhibitor reversed these effects. Similarly, PCA-induced autophagy and inhibition of apoptosis were enhanced by the miR-29b-3p mimic and reversed by the inhibitor. To determine whether SIRT1 acts downstream of miR-29b-3p, we used EX527 (a SIRT1 inhibitor) and found that it attenuated the PCA-mediated upregulation of miR-29b-3p. The miR-29b-3p mimic enhanced PCA-induced SIRT1 activity and protein expression, while the inhibitor had the opposite effect. Additional experiments revealed that NAC suppressed ROS by upregulating miR-29b-3p, leading to increased SIRT1 expression and reduced apoptosis. Disscussion Collectively, these findings demonstrate that PCA ameliorates OGD/R-induced endothelial injury by promoting autophagy and inhibiting apoptosis via the ROS/miR-29b-3p/SIRT1 regulatory axis.
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CRYSTAL GROWTH & DESIGN
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2025
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IF 3.4
Detao Li,Zichen Ning,Feiqiang He,Zhi Gao,Limin Zhou,Li Xu,Zhijian Zheng,Jerry Heng,Shichao Du,Jinbo Ouyang
To enable efficient separation of chiral drugs and enhance their practical utility, this study investigates cocrystallization as a novel separation and purification strategy. Using R/S-mandelic acid and d/l-prolinamide as model compounds, we screened potential cocrystal/salt coformers and successfully synthesized seven novel chiral salts. The proton transfer was elucidated by analyzing molecular electrostatic potential differences at the hydrogen-bonding sites. Moreover, the formation mechanism of salts was explored through structural analyses, such as Hirshfeld surface calculations, energy framework assessments, and crystal void analysis. Considering the distinct properties of various chiral salts, we conducted competitive cocrystallization experiments, establishing a complementary chiral pairing principle that provides a theoretical foundation for cocrystallization-based chiral resolution. Based on these findings, we developed multiple processes for the separation of R- and S-mandelic acid as well as l- and d-prolinamide, achieving product purities exceeding 80%, which strongly demonstrate the feasibility of cocrystallization separation technology for chiral resolution. This work not only introduces a groundbreaking approach to chiral separation but also highlights the vast potential of cocrystallization technology in pharmaceutical purification and beyond.
研究领域:
药物化学
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晶体工程
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手性分离技术
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超分子化学
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材料科学
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JOURNAL OF ETHNOPHARMACOLOGY
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2024
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IF 4.8
Danilo de Souza Costa,Rayssa A. Cajas,Carla Monteiro Leal,Lara S. Aleixo de Carvalho,Lara Cruz de Souza,Lucas Fukui-Silva,Josué de Moraes,Ademar A. Da Silva Filho
Ethnopharmacological relevance Acmella oleracea (L.) R. K. Jansen, commonly referred to as “Jambu”, is a valuable medicinal plant native to the Amazon regions. Inflorescences of A. oleracea is utilized as local anesthetic properties and for its insecticidal, antiparasitic, and anthelmintic attributes. Aims of this study This study aimed to evaluate the in vitro and in vivo antiparasitic properties of A. oleracea extract and spilanthol (SPL) against Schistosoma mansoni . Materials and methods The ethanolic extract of A. oleracea inflorescences (AoE) was prepared, analyzed by HPLC-DAD, and characterized by UHPLC-HRMS/MS. SPL was isolated from AoE by chromatographic fractionation. The antischistosomal properties of AoE and SPL were evaluated in vitro against adult schistosomes and in preclinical assays using murine models of patent S. mansoni infection. Results Through UHPLC-HRMS/MS analysis, 14 alkamides were annotated in AoE. HPLC-DAD analysis of AoE revealed a peak with a substantial relative area of ∼85%, which was isolated and identified as SPL. AoE and SPL caused mortality of adult schistosomes ex vivo , showing EC 50 values of 32.6 μg/mL and 27.8 μM, respectively, without affected Vero cells or Caenorhabditis elegans . In preclinical studies, the oral administration (400 mg/kg) of AoE and SPL resulted in significant reductions in worm burden of 28% and ∼42%, respectively. Additionally, SPL exhibits remarkable effects on oogram, decreasing egg burden and the number of immature eggs by over 80%, while also promoting significant reductions in hepato- and splenomegaly. Conclusions The research underscores the antischistosomal activity of A. oleracea highlighting the potential of SPL as a lead for the development of new schistosomicidal drugs and encouraging further studies to validate the traditional anthelmintic use of A. oleracea inflorescences.
研究领域:
药理学
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寄生虫学
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药物开发
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高影响因子
SPECTROSCOPY LETTERS
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2025
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IF 1.6
Ju Wei,Bingyu Luo,Jiao Fu,Shunli Zhou,E. Li,Xiaodong Su,Xiaotong Gao,Zhenfu Jia,Xiaojiang Li
To overcome the interference caused by the inner filter effect, this study optimally selected red fluorescence carbon dots as the signal source and constructed a novel dual-mode Ag@Red-CDs nanoprobe for the highly selective detection of Fe³+ using fluorescence and colorimetry. This probe is based on a unique reaction between Fe3+ and silver nanoparticles (AgNPs) that weakens the static quenching effect of AgNPs on R-CDs; at the same time, the depletion of AgNPs induces a change in the absorbance of the system. Under optimal conditions, the probe exhibited a linear fluorescence response in the Fe³+ concentration range of 0.10–25.00 μg/mL and a linear colorimetric response of 0.18–8.00 μg/mL. The detection limits for fluorescence and colorimetry were 0.31 μg/mL and 0.56 μg/mL, respectively. In spiked real samples, the fluorescence method achieved Fe³+ recovery rates of 99.10–102.34%, while the colorimetric method showed recovery rates of 99.83–101.42%. Overall, this research significantly broadened the potential applications of R-CDs-based materials for the quantitative detection of heavy metal ions in water bodies.
研究领域:
分析化学
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环境科学
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材料科学
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CANCER LETTERS
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2025
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IF 10.1
Hongchengcheng Chen,Guihui Yu,Haodong Lin,Xiao Albert Zhou,Jiansong Liu,Haoyun Liu,Yefei Luo,Kaiqi Cheng,Zuchao Mao,Yujie Ma,Jun Wang,Kezhong Chen,Jiadong Wang,Yun Li
R-loop accumulation has emerged as a critical factor that induces DNA damage and compromises genomic integrity. However, the regulatory mechanisms governing the R-loop-induced DNA damage remain unclear. Here, FTSJ3 was determined to be a pivotal regulator of R-loop homeostasis and genomic stability. We demonstrated that FTSJ3 was specifically recruited to R-loop structures, where it prevented DNA damage by suppressing excessive R-loop formation. FTSJ3 expression was significantly upregulated in multiple cancer types, and its elevated expression levels correlated with unfavorable survival in patients with lung adenocarcinoma (LUAD). FTSJ3 depletion increased R-loop-dependent DNA damage. Inhibiting FTSJ3 expression sensitized lung cancer cells to cisplatin both in vitro and in vivo . FTSJ3 could be a genome guardian that limits R-loop-associated damage, suggesting its potential role as a cancer intervention therapeutic target and a predictive biomarker for chemotherapy responsiveness.
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Bioresources and Bioprocessing
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2019
·Vol. 6
·期 1
·1-12
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IF 0
Zhang Can,Song Wei,Liu Jia,Chen Xiulai,Liu Liming
( R )- or ( S )-2-Hydroxy-4-(methylthio)butanoic acid (HMTBA) is used as a poultry nutritional supplement and to treat renal failure disease. Herein, we report an artificially designed biocatalytic cascade process, which uses l -methionine to synthesize ( R )- or ( S )-HMTBA. This biocatalysis cascade comprises a basic module and two different extender modules and operates in a modular assembly manner. The basic module responsible for the transformation of l -methionine to α-keto-γ-methylthiobutyric acid (KMTB) is comprised of the l -amino acid deaminase. Two different extender modules responsible for the transformation of KMTB to ( R )- or ( S )-HMTBA are comprised of the R/S-specific lactate dehydrogenase in combination with the formate dehydrogenase, respectively. Engineered Escherichia coli catalysts, one containing the basic module, the other containing the one of two different extender modules, produced 97.6 g L −1 ( R )-HMTBA and 96.4 g L −1 ( S )-HMTBA with a yield of 96.9% and 95.8% at the large scale (1 L) using a two-stage strategy in one pot, respectively. Therefore, this biocatalytic process lays the foundation for the industrial-scale conversion of low-cost l -amino acids to corresponding high-value enantiopure chiral 2-hydroxy acids.
研究领域:
生物技术
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酶工程
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代谢工程
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合成生物学
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Journal of Ginseng Research
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2022
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IF 5.735
Hong-Yan Guo,Yue Xing,Yu-Qiao Sun,Can Liu,Qian Xu,Fan-Fan Shang,Run-Hui Zhang,Xue-Jun Jin,Fener Chen,Jung Joon Lee,Dongzhou Kang,Qing-Kun Shen,Zhe-Shan Quan
Background Ginseng possesses antitumor effects, and ginsenosides are considered to be one of its main active chemical components. Ginsenosides can further be hydrolyzed to generate secondary saponins, and 20( R )-panaxotriol is an important sapogenin of ginsenosides. We aimed to synthesize a new ginsengenin derivative from 20( R )-panaxotriol and investigate its antitumor activity in vivo and in vitro . Methods Here, 20( R )-panaxotriol was selected as a precursor and was modified into its derivatives. The new products were characterized by 1 H-NMR, 13 C-NMR and HR-MS and evaluated by molecular docking, MTT, luciferase reporter assay, western blotting, immunofluorescent staining, colony formation assay, EdU labeling and immunofluorescence, apoptosis assay, cells migration assay, transwell assay and in vivo antitumor activity assay. Results The derivative with the best antitumor activity was identified as 6,12-dihydroxy-4,4,8,10,14-pentamethyl-17-(2,6,6-trimethyltetrahydro-2 H -pyran-2-yl)hexadecahydro-1 H -cyclopenta[a]phenanthren-3-yl( tert -butoxycarbonyl)glycinate ( A11 ). The focus of this research was on the antitumor activity of the derivatives. The efficacy of the derivative A11 (IC 50 < 0.3 μM) was more than 100 times higher than that of 20( R )- panaxotriol (IC 50 > 30 μM). In addition, A11 inhibited the protein expression and nuclear accumulation of the hypoxia-inducible factor HIF-1α in HeLa cells under hypoxic conditions in a dose-dependent manner. Moreover, A11 dose-dependently inhibited the proliferation, migration, and invasion of HeLa cells, while promoting their apoptosis. Notably, the inhibition by A11 was more significant than that by 20( R )-panaxotriol ( p < 0.01) in vivo . Conclusion To our knowledge, this is the first study to report the production of derivative A11 from 20( R )-panaxotriol and its superior antitumor activity compared to its precursor. Moreover, derivative A11 can be used to further study and develop novel antitumor drugs.
研究领域:
药理学
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肿瘤学
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有机化学
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生物化学
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INTERNATIONAL JOURNAL OF HYDROGEN ENERGY
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2020
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IF 4.939
Wenzhuo Chen,Liping Sun,Qiang Li,Lihua Huo,Hui Zhao
Defect-rich MoS 2 /r-GO hybrids are successfully synthesized via microwave-assisted solvothermal process, and their electrocatalytic properties for hydrogen evolution reaction (HER) are evaluated. The hybrids exhibit low overpotential of 86 mV at 10 mA cm −2 , with a Tafel slope of 44 mV dec −1 as well as promising long-term stability. The activation energy required by HER is 25.4 kJ/mol, and the faraday efficiency reaches 86.3% at −0.16 V (vs. RHE). The attractive performance can be attributed to the abundant defects generated in highly disordered MoS 2 phase, which help to expose a large number of active sites. In addition, the interaction between r-GO and MoS 2 particles promotes the charge transfer process. This work provides a simple strategy for the rational design and mass fabrication of defect-rich MoS 2 -based electrocatalysts for hydrogen evolution reaction.
研究领域:
材料科学
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电化学
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纳米技术
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催化
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高影响因子
FOOD CHEMISTRY
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2024
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IF 8.5
Huajian Xu,Zhongtao Hu,Zongwei Hao,Changyue Deng,Xiaowen Pi,Binjia Zhang
The effects of amino acids with different R-groups, namely glutamic acid (GLU), glutamine (GLN), and theanine (THE), on the pasting and structure properties of corn starch (CS) were investigated. During gelatinization, GLU decreased viscosity of CS. GLN and THE increased pasting enthalpy of CS from 7.62 to 8.72 and 9.50 J/g, respectively. All starch-amino acid systems had higher storage and loss modulus. Amino acids could adhere to starch granule surface. After co-gelatinization, GLU increased short-range order degree of starch, while GLN and THE decreased. Both infrared spectroscopy and quantum computation showed that non-covalent interaction occurred between amino acids and starch. Molecular dynamics revealed that the interaction between GLU and starch weakened hydrogen bonding between starch and water, promoting cross-linking between starch chains. GLN and THE changed dihedral angle torsion of glycoside bonds, and mainly interacted with starch by electrostatic interaction (50.06 kJ/mol) and van der Waals force (50.30 kJ/mol), respectively.
研究领域:
食品科学
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化学
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材料科学
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Pharmaceutics
·
2020
·Vol. 12
·期 1
·35
·
IF 4.421
Rui Zhang,Jie Wu,Siyu Liu,LiangJun Deng,Junhua Hu,Xi Chen,Wen Tan
Recent studies have shown that β2-Adrenoreceptor is a regulator of the a-synuclein gene driving risk of Parkinson’s disease. The β2-AR agonist (R)-salbutamol, eutomer of rac-salbutamol, may hold therapeutic potential for Parkinson’s disease (PD) following nasal administration. In this study, we use desorption electrospray ionization mass spectrometry (DESI-MS) to analyze spatial distribution of (R)-salbutamol in rat brain following nasal and intravenous administration. Here, we report that (R)-salbutamol efficiently deliver to the brain and had more drug dosage exposure in rat’s brain through nasal route administration than that of intravenous route administration. In conclusion, administering (R)-salbutamol through nasal route of administration may hold advantages in improving spatial distribution and increased exposure of drug in brain.Keywords:Parkinson’s disease;β2-adrenergic receptor;salbutamol;nasal administration;desorption electrospray ionization
研究领域:
神经科学
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药物学
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JOURNAL OF APPLIED POLYMER SCIENCE
·
2018
·Vol. 136
·期 7
·47068
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IF 1.901
N.-C. Wang,L.-F. Fang,J. Wang,P. Zhang,W.-B. Wang,C.-E. Lin,L. Xiao,C. Chen,B. Zhao,H. Abdallah,H. Matsuyama,B.-K. Zhu
Carboxyl groups in the membranes usually contribute the hydrophilicity and antifouling properties. However, membrane performance including permeation and separation properties is not stable at different pH environments due to pH sensitivity of carboxyl groups. In this work, a series of membranes from random copolymers poly(vinyl chloride- r -acrylic acid) [P(VC- r -AA)] were fabricated via nonsolvent induced phase separation process. The morphology and surface properties were investigated. The pH-dependent property of carboxyl groups contained ultrafiltration membranes were studied in detail. The results indicated that pH sensitivity of these membrane was restrained, which was mainly attributed to the random sequential structure of VC and AA repeating unit in P(VC- r -AA) copolymer. The probable arched structures on the pore surface/wall at alkaline environment limited the obvious change of the pore size, which resulted in the stable permeation and separation properties at the varied pH environments. Therefore, it indicated that P(VC- r -AA) was a kind of promising membrane material which would be widely applied in water treatment field. © 2018 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2019 , 136 , 47068.
研究领域:
材料科学
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环境科学
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化学工程
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高影响因子
INORGANICA CHIMICA ACTA
·
2017
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IF 2.002
Jie Chai,Yanfei Liu,Jinglong Dong,Bin Liu,Binsheng Yang
The worldwide use of chromium(III) picolinate Cr(pic) 3 as nutrition additives has aroused more and more controversies. To reevaluate the safety and validity of Cr(pic) 3 , seven new derivatives Cr(R-pic) 3 (pic = picolinic acid, R = H ( 1 ), 5-Br ( 2 ), 5-CF 3 ( 3 ), 4-Cl ( 4 ), 5-COOH ( 5 ), 3-CH 3 ( 6 ), 5-OH ( 7 ), 3-OH ( 8 )) were synthesized and characterized by X-ray crystal diffraction, ESI-MS, IR and elemental analysis. It was found that different substituent group affected physicochemical activities of the complex such as the Fenton-like reaction and oxidation reaction. Especially, –OH group derivatives lose their hydroxyl radical-generation and Cr(VI)-generation abilities comparing with halogen group in tube experiment. Even so, these differences in chemistry properties may be ignored in live cells and animal tests: no obvious cellular damage (MTT assay) and tissue injury (acute toxicity study) were observed for both Cr(pic) 3 and its derivatives. In addition, hypoglycemic activity study indicated that these Cr(III) complexes have no significant influence than CrCl 3 salt on the blood glucose, serum insulin, total cholesterol, triglyceride, high density lipoprotein and low density lipoprotein of diabetic mice through two months’ study. Therefore, these substituent group is unable to improve the biological activities of Cr(pic) 3 obviously and the validity of Cr(pic) 3 used as a nutrition additives is doubted.
研究领域:
无机化学
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生物化学
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药理学
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高影响因子
危险品化学品经营许可证（带存储）