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Ganoderic acid ameliorates ulcerative colitis by improving intestinal barrier function via gut microbiota modulation

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Ganoderic acid ameliorates ulcerative colitis by improving i...

第十二届药用真菌学术研讨会

作者： Yuwei Ye baoxue yang Department of Pharmacology School of Basic Medical Sciences Peking University

Background Ulcerative colitis (UC) is a chronic and recurrent gastrointestinal disease that affects millions of humans worldwide and imposes a huge social and economic burden. It is necessary to find safe and efficient drugs for preventing and treating UC. Aim The aim of this study was to determine whether ganoderic acid (GA), the main bioactive component of Ganoderma lucidum, has preventive and therapeutic effect on UC in a dextran sulfate sodium (DSS)-induced UC mouse model.

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Discovery of a novel urea transporter inhibitor using computer aided drug design and its pharmacological study

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Discovery of a novel urea transporter inhibitor using comput...

第十一届海峡两岸心血管科学研讨会、2017年全国心脑血管药理学术会议、中国卒中学会第一次新药研讨会

作者： Li Min yang baoxue Peking University Health Science Center

Objective:Urea transporters B(UT-B) is a transmembrane protein selectively permeable to urea and play an important role in urine *** work showed UT-B knockout resulted as the urea selective urine concentrating defect, but did not affect electrolyte balance,which suggests that UT-B inhibitors have the potential to be developed into novel *** objective of this study

关键词： Discovery of a novel urea transporter inhibitor using computer aided drug design and its pharmacological study

Aquaporin-1 retards renal cyst development in polycystic kidney disease by inhibition of Wnt signaling

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Aquaporin-1 retards renal cyst development in polycystic kid...

中国生理学会第24届全国会员代表大会暨生理学学术大会

作者： Weiling Wang Hong Zhou baoxue yang Department of Pharmacology School of Basic Medical SciencesPeking University

Objective:Water channel aquaporin-1(AQP1)is expressed at epithelial cell plasma membranes in renal proximal tubules and thin descending limb of ***,AQP1 was identified to interact with β-*** dominant polycystic kidney disease(ADPKD)is one of the most common human monogenic diseases in which canonical Wnt pathway was *** we investigated the relationship between AQP1 and Wnt ***:Expression of β-catenin,E-cadherin and other Wnt signaling related proteins were detected in MDCK and AQP1 over-expression MDCK ***-immunoprecipitation was used to determine the interaction between AQP1 and β-catenin,GSK3β,LRP6 and *** we used matrix-grown MDCK cells,embryonic kidney organ cultures and Aqp1/Pkd1 double knockout mice to investigate the role of AQP1 in ***:AQP1 transfection decreased β-catenin and cyclin D1 expression and increased p-β-catenin,suggesting down-regulation of Wnt ***-immunoprecipitation showed AQP1 interaction with β-catenin,GSK3β,LRP6 and *** matrix-grown MDCK cells,AQP1 transfection inhibited cystdevelopment and promoted *** embryonic kidney cultures,AQP1 deletion increased cyst development by up to0%.Kidney size and cyst number were significantly greater in AQP1 null PKD mice than in AQP1-expressing PKD mice,with the difference due mainly to a greater number proximal tubule *** analysis revealed decreased β-catenin phosphorylation and increased β-catenin expression in Aqp1/Pkd1 double knockout mice,suggesting enhanced Wnt ***:These results suggested that AQP1 may be involved in maintaining the stability of the"destruction complex"to promote β-catenin phosphorylation and suppress the Wnt signaling ***1 as a novel determinant in renal cyst development that may involve inhibition of Wnt signaling by an AQP1-macromolecular signaling complex.

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Discovery of novel diarylamides as orally active diuretics targeting urea transporters

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Acta Pharmaceutica Sinica B 2021年第1期11卷 181-202页

作者： Shun Zhang Yan Zhao Shuyuan Wang Min Li Yue Xu Jianhua Ran Xiaoqiang Geng Jinzhao He Jia Meng Guangying Shao Hong Zhou Zemei Ge Guangping Chen Runtao Li baoxue yang Department of Pharmacology School of Basic Medical SciencesPeking UniversityBeijing 100191China State Key Laboratory of Natural and Biomimetic Drugs Peking UniversityBeijing 100191China Key Laboratory of Molecular Cardiovascular Sciences Ministry of EducationBeijing 100191China School of Pharmaceutical Sciences Peking UniversityBeijing 100191China College of Pharmacy Inner Mongolia Medical UniversityHohhot 010110China Department of Anatomy and Neuroscience Center Chongqing Medical UniversityChongqing 400016China Department of Physiology Emory University School of MedicineAtlantaGA 30322USA

Urea transporters(UT)play a vital role in the mechanism of urine concentration and are recognized as novel targets for the development of salt-sparing ***,UT inhibitors are promising for development as novel *** the present study,a novel UT inhibitor with a diarylamide scaffold was discovered by high-throughput *** of the inhibitor led to the identifi-cation of a promising preclinical candidate,N-[4-(acetylamino)phenyl]-5-nitrofuran-2-carboxamide(1 H),with excellent in vitro UT inhibitory activity at the submicromolar *** half maximal inhibitory concentrations of 1 H against UT-B in mouse,rat,and human erythrocyte were 1.60,0.64,and0.13 mmol/L,*** investigation suggested that 8 mmol/L 1 H more powerfully inhibited UT-A1 at a rate of 86.8%than UT-B at a rate of 73.9%in MDCK cell *** interestingly,we found for the first time that oral administration of 1 H at a dose of 100 mg/kg showed superior diuretic effect in vivo without causing electrolyte imbalance in ***,1 H did not exhibit apparent toxicity in vivo and in vitro,and possessed favorable pharmacokinetic characteristics.1 H shows promise as a novel diuretic to treat hyponatremia accompanied with volume expansion and may cause few side effects.

关键词： Urea transporter inhibitor Diuretic Structure optimization Oral administration

Research on accurate quantitation technique using liquid chromatography coupled with triple quadrupole mass spectrometry and experiment optimization—take a novel diuretic as an example

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Journal of Chinese Pharmaceutical Sciences 2022年第3期31卷 184-191页

作者： Wen Ma Yue Xu Shuyuan Wang Jun Li baoxue yang State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking University Health Science CenterBeijing 100191China Department of Pharmacology School of Basic Medical SciencesPeking University Health Science CenterBeijing 100191China

Liquid chromatography coupled with the triple quadrupole mass spectrometry(LC-QQQ MS)technique is the most commonly used technique for quantitative *** is widely used in pharmacology,targeted metabolomics,Chinese medicine quality control,and other research *** technique monitors only characteristic precursors and product ions through multiple reaction monitoring(MRM)mode and can detect targeted molecules in complex matrix with high specificity and *** the present study,a diarylamide derivative diuretic was used as an example to introduce the method establishment and parameter optimization of this liquid chromatography-mass spectrometry *** and its internal standard could be completely separated within a 5-min gradient,and the quantitative linear range was 1–1000 ng/mL with R2=0.9996 in practical *** study showed that the key to the method development for LC-QQQ MS was the selection of the LC mobile phase,the elution gradient,the declustering potential,and the collision energy of compounds in MS.

关键词： Liquid chromatography Triple quadrupole mass spectrometry Method establishment Diuretic

AMPK activation enhances the anti-atherogenic effects of high-density lipoproteins in apoE-/- mice

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AMPK activation enhances the anti-atherogenic effects of hig...

首届东方药理论坛暨2018年全国心脑血管药理学术会议、上海市药理学会第十九届学术年会

作者： Ang Ma Jing Wang Liu yang Yuanyuan An baoxue yang Haibo Zhu State Key Laboratory for Bioactive Substances and Functions of Natural Medicines Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Studyand Institute of Materia MedicaChinese Academy of Medical Sciences & Peking Union Medical College State Key Laboratory of Natural and Biomimetic Drugs Department of PharmacologySchool of Basic Medical SciencesPeking University

HDL plays crucial roles at multiple stages of the pathogenesis of ***-activated protein kinase（AMPK） is a therapeutic candidate for the treatment of cardiovascular ***,the effect of AMPK activation on HDL functionality has not been established in *** assessed the effects of pharmacological AMPK activation using,A-769662（30 mg/kg,i.p.）,AICAR（200 mg/kg, i.p.）,metformin（260 mg/kg,by gavage）,and IMM-H007（200 mg/kg, by gavage） on the atheroprotective functions of HDL in apoE-deficient(apoE) mice fed with a1.2% cholesterol+10% lard *** treated with AMPK activators showed significantly enhanced in vivo reverse cholesterol transport from macrophages to the plasma,liver,and feces versus *** activation also increased the expression of ABCA1 and ABCG1 in macrophages and SR-BI and LCAT in the *** from AMPK activation mice exhibited a lower HDL inflammatory index and myeloperoxidase activity,and a higher paraoxonasel activity,than HDL from untreated mice,implying superior antioxidant and anti-inflammatory *** AMPK activation also reduced plasma lipid peroxidation,inflammatory cytokine production,and atherosclerotic plaque formation in *** observations suggest that pharmacological AMPK activation enhances the anti-atherogenic properties of HDL in *** likely represents a key mechanism by which AMPK activation attenuates atherosclerosis.

关键词： AMP-activated protein kinase atherosclerosis high-density lipoprotein reverse cholesterol transport

High urea induces depression and LTP impairment through mTOR signaling suppression caused by carbamylation

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High urea induces depression and LTP impairment through mTOR...

首届东方药理论坛暨2018年全国心脑血管药理学术会议、上海市药理学会第十九届学术年会

作者： Hongkai Wang Weiling Wang Boyue Huang Jianhua Ran baoxue yang Department of Pharmacology School of Basic Medical Sciencesand State Key Laboratory of Natural and Biomimetic DrugsPeking University

Background:Depression is one of the main factors lowering quality of life for patients with chronic physical *** is unknown whether a biological factor is implicated in ***,the end product of protein metabolism,has been considered to have negligible toxicity for a *** previous study showed depression phenotype in urea transporter (UT) B knockout mice,which suggests that

关键词： LTP High urea induces depression and LTP impairment through mTOR signaling suppression caused by carbamylation

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灵芝多糖的药理学研究进展

菌物研究 2024年第1期22卷 22-38页

作者：张玉坤姚阳杨宝学重庆三峡医药高等专科学校重庆404120 北京大学基础医学院药理系北京100191

灵芝入药在我国有着悠久的历史。灵芝多糖(Ganoderma lucidum polysaccharides, GLPs)是灵芝中的主要活性成分之一,因提取方法相对简单,具有理想的开发应用前景,因此受到越来越多研究者的重视。文献表明,GLPs具有调节免疫、抗炎、抗氧... 详细信息

灵芝入药在我国有着悠久的历史。灵芝多糖(Ganoderma lucidum polysaccharides, GLPs)是灵芝中的主要活性成分之一,因提取方法相对简单,具有理想的开发应用前景,因此受到越来越多研究者的重视。文献表明,GLPs具有调节免疫、抗炎、抗氧化等广泛药理作用,对神经系统、心血管系统和消化系统等多种疾病具有改善作用。文中以药理学为基础,结合实验数据和结果,概述了灵芝中多糖类活性成分的药理作用和对疾病潜在的治疗作用。GLPs的药理作用是多方面、多途径的,可以影响疾病进展的多条信号通路,其作用方式更倾向于将机体调节到一个健康积极的状态,间接改善或抑制疾病进程,机制上主要与其抗氧化和调节免疫的作用密切相关。近年来,随着对不同品种、不同培养底物、不同提取方式获得GLPs药理作用研究的报道日益增多,也反映了研究者对GLPs构效关系研究的迫切需求。后续,对GLPs建立统一的质量控制标准、保证GLPs提取物结构的稳定性、明确其构效关系将有助于GLPs的临床应用,推进其国际化进程。

关键词：灵芝多糖药理作用机制

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灵芝三萜的药理学研究进展

菌物研究 2024年第1期22卷 60-78页

作者：卢烽姜涛杨宝学北京大学基础医学院药理学系北京100191 血管稳态与重构全国重点实验室北京100191 北华大学基础医学院吉林132013

灵芝是药食同源的大型真菌,可用于预防和治疗多种疾病。灵芝三萜是灵芝的重要活性成分,其含量是评价灵芝品质的重要指标。灵芝三萜的化学结构决定其多样的生物学活性,包括抗炎、抗氧化、抗肿瘤、抗衰老、调节免疫功能以及调节代谢等。... 详细信息

灵芝是药食同源的大型真菌,可用于预防和治疗多种疾病。灵芝三萜是灵芝的重要活性成分,其含量是评价灵芝品质的重要指标。灵芝三萜的化学结构决定其多样的生物学活性,包括抗炎、抗氧化、抗肿瘤、抗衰老、调节免疫功能以及调节代谢等。文中基于相关研究文献对灵芝三萜的药理作用及其机制进行总结和论述,以期为灵芝三萜在创新药物研发与功能性食品开发领域的基础研究和转化应用提供系统参考资料。

关键词：灵芝三萜药理活性功能性食品灵芝酸