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| 1 | Hewei Jiangni granule alleviates visceral hypersensitivity in a rat model of non-erosive reflux disease via transient receptor potential channel signaling显示文摘Objective:To uncover the underlying mechanism of Hewei Jiangni granule(HWJNG)on non-erosive reflux disease(NERD)treatment by examining histological changes,gastrointestinal neurochemicals release and visceral hypersensitivity-related receptor expression in NERD model rats.Methods:A NERD rat model was established via a combination of basal sensitization and acid perfusion.HWJNG treatments at different doses were then administered.Pathological changes to tissues,mast cell(MC)activation,serum levels of esophageal visceral hypersensitivity-related neurochemicals,and transient receptor potential(TRP)receptor mRNA and protein levels were investigated.Results:Compared with the control group,the expression of tryptase in MCs,the changes of intercellular space,and the serum levels of substance P(SP),calcitonin gene-related peptides(CGRP)and proteinaseactivated receptor 2(PAR2)increased in the model group(all P<.05).The expression of TRP vanilloid 1(Trpv1)mRNA decreased in esophagus and dorsal root ganglia(DRG)of the model group(P=.030&P=.013),and the expression of TRP melastatin channel subfamily member 8(Trpm8)mRNA decreased in the esophagus of model group(P<.01).The level of esophageal TRPV1 protein increased in the model group(P<.01)and the level of TRPM8 protein decreased in esophagus and DRG of the model group(both P<.05).Compared with the model group,the serum levels of SP,CGRP,and PAR2 in the mediumdose HWJNG group showed significant decreases(all P<.05).The expression of Trpv1 mRNA in esophagus and DRG of the HWJNG groups and the Omeprazole group remarkably decreased(all P<.05),as was the expression of Trpm8 mRNA in esophagus of the HWJNG groups(all P<.05).Conclusion:HWJNG alleviated visceral hypersensitivity in NERD model rats by regulating TRP-mediated signaling.Our results indicate that HWJNG has potential as a therapeutic agent for NERD. | Jiali Liu Fushun Kou Xiang Tan Yi Dai Chune Xie Xiaohong Li Lei Shi Tangyou Mao Xiaojun Shi Junxiang Li | 2020 | Journal of Traditional Chinese Medical Sciences2020，7，2： | 1 |
| 2 | Research progress of Chinese medicine treatment of Helicobacter pylori associated gastric diseases 显示文摘 | Xie Chune Xue Xiaoxuan | 2013 | Journal of Beijing University of Chinese Medicine (TCM clinical Edition)2013，20，1： | 1 |
| 3 | Isomerization and bioaccessibility of cypermethrin and fenpropathrin in Pacific oyster during simulated digestion as influenced by domestic cooking methods显示文摘Pyrethroids can be ingested by humans through eating contaminated oysters,which is potentially harmful to health.This study aimed to investigate the effects of raw,steaming,and roasting on cypermethrin(CP)and fenpropathrin(FP)in oysters during simulated digestion.Results showed that the amount of released CP and FP was different from raw(CP:0.617μg·g−1,FP:0.266μg·g−1),steaming(CP:0.498μg·g−1,FP:0.660μg·g−1),and roasting(CP:1.186μg·g−1,FP:0.588μg·g−1)at the end of simulated digestion.The share of cis-CP and low-efficiency CP increased significantly(p<0.05),and the share of high-efficiency trans-CP did not maintain a high level for a long time during simulated digestion.The fluorimetric titration and isothermal titration calorimetry confirmed that CP and FP could spontaneously interact with oyster actin,and CP could bind with oyster actin more tightly than FP.This study reveals that cooking methods affect the binding capacity of CP and FP to oyster tissues and influence the changes of CP and FP in oysters during digestion.Furthermore,the current study provides a reference for assessing the potential harm of pyrethroids in oysters to consumers. | Hangtao Xie Yadan Jiao Tian Li Tuo Zhang Yanyan Zheng Yongkang Luo Yuqing Tan Chune Liu Hui Hong | 2023 | Food Innovation and Advances2023，2，1： | 0 |
| 4 | Discovery of novel covalent selective estrogen receptor degraders against endocrine-resistant breast cancer显示文摘Endocrine-resistance remains a major challenge in estrogen receptorαpositive(ERα^(+))breast cancer(BC)treatment and constitutively active somatic mutations in ERαare a common mechanism.There is an urgent need to develop novel drugs with new mode of mechanism to fight endocrineresistance.Given aberrant ERαactivity,we herein report the identification of novel covalent selective estrogen receptor degraders(cSERDs)possessing the advantages of both covalent and degradation strategies.A highly potent cSERD 29c was identified with superior anti-proliferative activity than fulvestrant against a panel of ERa+breast cancer cell lines including mutant ERα.Crystal structure of ERα-29c complex alongside intact mass spectrometry revealed that 29c disrupted ERa protein homeostasis through covalent targeting C530 and strong hydrophobic interaction collied on H11,thus enforcing a unique antagonist conformation and driving the ERαdegradation.These significant effects of the cSERD on ERαhomeostasis,unlike typical ERαdegraders that occur directly via long side chains perturbing the morphology of H12,demonstrating a distinct mechanism of action(MoA).In vivo,29c showed potent antitumor activity in MCF-7 tumor xenograft models and low toxicity.This proof-of-principle study verifies that novel cSERDs offering new opportunities for the development of innovative therapies for endocrine-resistant BC. | Yubo Wang Jian Min Xiangping Deng Tian Feng Hebing Hu Xinyi Guo Yan Cheng Baohua Xie Yu Yang Chun-Chi Chen Rey-Ting Guo Chune Dong Hai-Bing Zhou | 2023 | Acta Pharmaceutica Sinica B2023，13，12： | 0 |
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