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Chinese Chemical Letters 2014年第1期25卷 51-54页

作者： Min Han Guo-Cheng Wang Hong-Quan Duan tasly R&D Institute Tasly Holding Group Co.Ltd. tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics School of PharmacyTianjin Medical University

The self-assembly of cationic perylene diimide （PDI） and anionic cholesterol derivatives （CHOL） was conveniently achieved by the electrostatic attraction and π-π stacking interactions, exhibiting the weft-define... 详细信息

关键词： Perylene diimide Cholesterol Electrostatic attraction Supramolecular nanofibers

Xiao Ke Qing improves glycometabolism and ameliorates insulin resistance by regulating the PI3K/Akt pathway in KKAy mice

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Frontiers of Medicine 2018年第6期12卷 688-696页

作者： Xiaoqing Li Xinxin Li Genbei Wang Yan Xu Yuanyuan Wang Ruijia Hao Xiaohui Ma Department of Pharmacology and Toxicology Tasly Pharmaceutical Co.Ltd.Tianjin 300410China

Xiao Ke Qing (XKQ) granule has been clinically used to treat type 2 diabetes mellitus (T2DM) for 10 years in Chinese traditional medication. However, its mechanisms against hyperglycemia remain poorly understood. This study aims to investigate XKQ mechanisms on diabetes and diabetic liver disease by using the KKAy mice model. Our results indicate that XKQ can significantly reduce food and water intake. XKQ treatment also remarkably decreases both the fasting blood glucose and blood glucose in the oral glucose tolerance test. Additionally, XKQ can significantly decrease the serum alanine aminotransferase level and liver index and can alleviate the fat degeneration in liver tissues. Moreover, XKQ can ameliorate insulin resistance and upregulate the expression of IRS-1, PI3K (p85), p-Akt, and GLUT4 in the skeletal muscle of KKAy mice. XKQ is an effective drug for T2DM by ameliorating insulin resistance and regulating the PI3K/Akt signaling pathway in the skeletal muscle.

关键词： KKAy mice PI3K/Akt pathway XKQ diabetic liver disease type 2 diabetes mellitus

Sulfite as the substrate of C-sulfonate metabolism ofα,β-unsaturated carbonyl containing andrographolide:analysis of sulfite in rats'intestinal tract and the reaction kinetics of andrographolide with sulfite

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Chinese Journal of Natural Medicines 2021年第9期19卷 706-712页

作者： HUO Zhi-Peng FENG Xin-Chi WANG Yu TIAN Yu-Ting QIU Feng School of Chinese Materia Medica and State Key Laboratory of Component-based Chinese MedicineTianjin University of Traditional Chinese MedicineTianjin 301617China ~TCM Research Center Tasly AcademyTasly Holding Group Co.Ltd.Tianjin 300402China State Key Laboratory of Critical Technology in Innovative Chinese Medicine Tasly Pharmaceutical Co.Ltd.Tianjin 300402China Institute of Pharmacy China Pharmaceutical UniversityNanjing 210009China Institute of Pharmaceutical Science and Technology Tianjin UniversityTianjin 300072China

One-sixth of the currently known natural products containα,β-unsaturated carbonyl *** previous studies reported a rare C-sulfonate metabolic *** groups were linked to theβ-carbon ofα,β-unsaturated carbonyl-based natural compounds through this ***,the mechanism of this type of metabolism is still not fully understood,especially whether it is formed through enzyme-mediated biotransformation or direct sulfite *** this work,the enzyme-mediated and non-enzymatic pathways were ***,the sulfite content in rat intestine was determined by LC-MS/*** results showed that the amount of sulfite in rat intestinal contents was from 41.5 to 383μg·g^(-1),whereas the amount of sulfite in rat feed was lower than the lower limit of quantitation(20μg·g^(-1)).Second,the reaction kinetics of sulfite-andrographolide reactions in phosphate buffer solutions(pH 6-8)was *** half-lives of andrographolide ranged from minutes to *** was suggested that the C-sulfonate reaction of andrographolide was very ***,the C-sulfonate metabolites of andrographolide were both detected when andrographolide and L-cysteine-S-conjugate andrographolide were incubated with the rat small intestine contents or sulfite,indicating that the sulfite amount in rat intestine contents was high enough to react with andrographolide,which assisted a significant portion of andrographolide ***,the comparison of andrographolide metabolite profiles among liver homogenate(with NADPH),liver S9(with NADPH),small intestine contents homogenate(with no NADPH),and sulfite solution incubations showed that the C-sulfonate metabolites were predominantly generated in the intestinal tract by non-enzymatic *** summary,sulfite can serve as a substrate for C-sulfonate metabolism,and these results identified non-enzymatically nucleophilic addition as the potential mechanism for C-sulfonate metabolism of compounds containingα,β-unsaturated carbonyl moie

关键词： Sulfite C-Sulfonate metabolites α,β-Unsaturated carbonyl Reaction kinetics Andrographolide Non-enzymatic

Gastroprotective Effects of Ascaridole on Gastric Ulcer in Rats

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Chinese Herbal Medicines 2012年第1期4卷 58-62页

作者： Yong-hong ZHU[a][b] Xin-xin LI[b] Hong-mei MO[b] Li-hua ZHANG[b] Lan-lan ZHANG[b] Shui-ping ZHOU[b] Xiao-hui MA[b][c] Bo-li ZHANG[a] tianjin University of Traditional Chinese Medicine Tianjin 300193 China Department of Pharmacology and Toxicity Tasly R&D Institute Tianjin Tasly Group Co. Ltd. Tianjin 300410 China Department of Pharmacology and Toxicity Tasly R&D Institute Tianjin Tasly Group Co. Ltd. Tianjin 300410 China School of Pharmaceutical Science and Technology Tianjin University Tianjin 300072 China

Objective To evaluate the gastroprotective activity of ascaridole. Methods The gastroprotective effect of ascaridole was evaluated on ulcer healing in rats with acetic acid-induced chronic gastric ulcer, pylorus ligation- and Aspirin-induced gastric ulcer. Ascaridole was ig administered with the dosages of 10 and 20 mg/kg once daily for 7 d. Results Ascaridole showed the significant anti-ulcer effects. In acetic acid-induced gastric ulcer rats, the ulcer areas after 10 and 20 mg/kg of ascaridole treatment were (65.1 ± 20.0) and (50.6 ± 11.0) mm2, respectively, which were significant lower (P < 0.01) than that of the control group [(116.7 ± 35.8) mm2]. For pylorus ligation model, ascaridole showed a gastric ulcer healing effect in a dose-dependent manner. Ascaridole at the dose of 20 mg/kg showed 50% ulcer protection and had a significant (P < 0.05) gastroprotective activity since it decreased the total acidity and pepsin activity. Compared to the control group, the two dosages of ascaridole showed the significant reduction (P < 0.05) in the ulcer index on Aspirin-induced ulcer. Conclusion This study provides evidence that ascaridole shows potential efficacy on the healing of gastric ulcers induced by acetic acid, Aspirin, and pylorus ligation.

关键词： ascaridole Aspirin chronic gastric ulcer gastroprotective effect pylorus ligation

Systematic review and Meta-analysis of 26 randomized controlled clinical trials of Compound Danshen Dripping Pill for non-proliferating diabetic retinopathy

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Chinese Herbal Medicines 2022年第1期14卷 142-153页

作者： Yu Wang Lei Hao Zhipeng Huo Yuanxue Liu Yujing Sun Zhaohui Song State Key Laboratory of Core Technology in Innovative Chinese Medicine Tasly AcademyTasly Holding Group Co.Ltd.Tianjin 300410China

Objective:Diabetic retinopathy(DR) is the retinal consequence of chronic progressive diabetic microvascular leakage and ***-proliferating diabetic retinopathy(NPDR) is the early stage of *** eventually occurs to some degree in all patients with diabetes *** recent years,many clinical trials have shown that Compound Danshen Dripping Pill(CDDP) may be associated with the improvement of NPDR *** aim of this study was to quantitatively summarize the association between CDDP and the therapeutic effects of ***:It was conducted that a systematic literature search of Pub Med,Web of Science,CNKI,VIP and Wanfang Data updated in June 2020 with the following search terms:"diabetic retinopathy° or"retinopathy° or "DR° or "NPDR°,in combination with "Compound Danshen Dripping Pill° or "Salvia miltiorrhiza° or "Danshen°.Risk ratio(RR) and weighted mean difference(WMD) with their 95% confidence interval(CI) was calculated between treatment and control *** sensitivity analyses were undertaken by removing each individual study when high heterogeneity *** analysis,Metaregression,and publication bias analysis were also *** strength of evidence was evaluated with the Grading of Recommendation,Assessment,Development,and Evaluation(GRADE) ***:Twenty-six RCTs involving 2047 subjects were included to conduct a Meta-analysis after screening the studies,extracting the data,and assessing the study *** Stata15.0 software was utilized for ***-analysis indicated that curative effects of treatment group with CDDP was significantly better than control [RR = 0.54,95% CI(0.40,0.73);moderate-quality evidence].In addition,the results showed that CDDP was significantly associated with improving retinal hemorrhages[WMD =-0.62,95% CI(-0.78,-0.46);low-quality evidence],the vision [WMD = 0.14,and 95% CI(0.09,0.19),low-quality evidence],fundus fluorescence angiography [RR = 0.37 and 95% CI(0.23,0.60);low-qualit

关键词： Compound Danshen Dripping Pill diabetic retinopathy Meta-analysis randomized controlled clinical trial systemic review

Analysis of pesticide residues in commercially available chenpi using a modified QuEChERS method and GC-MS/MS determination

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Journal of Pharmaceutical Analysis 2020年第1期10卷 60-69页

作者： Shuang Li Peipei Yu Ceng Zhou Ling Tong Dongxiang Li Zhiguo Yu Yunli Zhao School of Pharmacy Shenyang Pharmaceutical UniversityShenyang110016China Baoding No.1 Central Hospital BaodingHebei Province 071000China State Key Laboratory of Core Technology in Innovative Chinese Medicine Tasly Pharmaceutical Analysis InstituteTasly AcademyTianjin 300402China

To ensure the safety of the commercially available chenpi,a convenient and fast analytical method was developed for the determination of 133 pesticide residues in chenpi using gas chromatography-tandem mass spectrometry(GC-MS/MS).In this study,different extraction solvents,redissolution solvents and adsorbents were tested according to the recovery and purification effect to obtain a modified QuEChERS *** samples were extracted with *** the clean-up step,octadecyl-modified silica(C18)and graphitized carbon black(GCB)were selected,and aminopropyl(NH2)was used instead of primary secondary amine(PSA)because of its weaker ion exchange capacity which had little effect on the recovery of *** were quantified by matrix-matched calibration with internal *** pesticides showed good linearity in the respective range,both with values of r2>*** average recoveries of the pesticides spiked samples ranged from 70.0% to 112.2% with the RSDs of 0.2%–14.4%.The modified QuEChERS method was validated and applied to twenty real *** pesticides were found in eight batches,but no pesticide exceeded the maximum residue limits(MRL,MRL reference to European commission).

关键词： Pesticide residues Chenpi GC-MS/MS QuEChERS

Identification of metabolites of Radix Paeoniae Alba extract in rat bile, plasma and urine by ultra-performance liquid chromatography–quadrupole time-of-flight mass spectrometry

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Journal of Pharmaceutical Analysis 2014年第1期4卷 14-25页

作者： Zheng-Wei Chen Ling Tong Shu-Ming Li Dong-Xiang Li Ying Zhang Shui-Ping Zhou Yong-Hong Zhu He Sun Department of Pharmaceutical Analysis China Pharmaceutical University tasly R&D Institute Tianjin Tasly Group Co. Ltd. Center of Drug Metabolism and Pharmacokinetics China Pharmaceutical University

Ultra-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry （UPLC-Q-TOF/MS） was developed to identify the absorbed parent components and metabolites in rat bile, plasma and urine after oral administration of Radix Paeoniae Alba extract （RPAE）. A total of 65 compounds were detected in rat bile, plasma and urine samples, including 11 parent compounds and 54 metabolites. The results indicated that glucuronidation, hydroxylation and methylation were the major metabolic pathways of the components of RPAE. Furthermore, the results of this work demonstrated that UPLC-Q-TOF/MS combined with MetaboLynx？ software and mass defect filtering （MDF） could provide unique high throughput capabilities for drug metabolism study, with excellent MS mass accuracy and enhanced MSE data acquisition. With the MSE technique, both precursor and fragment mass spectra can be simultaneously acquired by alternating between high and low collision energy during a single chromatographic run.

关键词： Radix Paeoniae Alba Metabolite profiling UPLC-Q-TOF/MS Monoterpene glycosides

Simultaneous Determination of Silybin A and Silybin B in Rat Plasma and Pharmacokinetic Study

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Chinese Herbal Medicines 2011年第4期3卷 304-309页

作者： CHU Yang,LI Wei,LI Zhi-wen,LI Xin-xin,MA Xiao-hui,ZHOU Shui-ping,ZHU Yong-hong Department of Pharmacology,tianjin tasly Institute,tianjin 300410,China Department of Pharmacology Tianjin Tasly Institute Tianjin 300410 China

Objective To investigate the bioavailability and pharmacokinetics of silybin A and silybin B in rats,respectively. Methods Following iv and ig administration of silybin to 20 Wistar rats,the plasma samples were collected at different time points up to 12 *** pretreatment was involved in one-step protein precipitation with acetonitrile. Silybin A and silybin B were simultaneously determined by LC-MS/*** After ig dosing silybin 28,56,and 112 mg/kg to rats,the t1/2βvalues were 5.48,5.08,and 5.73 h for silybin A,and 4.56,4.12,and 5.53 h for silybin B; The Cmax were 674.3,1349.4,and 2042.5 ng/mL for silybin A,and 671.0,1365.4,and 2066.2 ng/mL for silybin B; The Tmax were 0.20,0.23,and 0.20 h for silybin A,and 0.20,0.23,and 0.20 h for silybin B;The AUC were 454.4, 845.9,and 1219.5 h·ng/mL for silybin A,and 432.0,817.1,and 1153.6 h·ng/mL for silybin *** absolute bioavailabilities of silybin A and silybin B were 2.86%and 1.93%,*** Silybin A and silybin B have very low bioavailability after ig administration,and there is no significant difference in the pharmacokinetic parameters between silybin A and silybin B,which indicates that the two diastereoisomers have similar pharmacokinetic behavior in rats.

关键词： bioavailability LC-MS/MS pharmacokinetics silybin A silybin B

A network pharmacology approach to explore the mechanism of action of Yiqi Fumai lyophilized injection in the treatment of novel coronavirus disease

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Traditional Medicine Research 2023年第3期8卷 1-9页

作者： Yan Zhou Lei Fan Du-Hong Xie Xiao-Ying Han Bo-Xuan Zhao Yi Zhang De-Kun Li Ai-Chun Ju Hai-Xia Ji Ou Qiao Xin-Yu Zhang Wen-Zhe Wang Chang-Xiao Liu Wen-Yuan Gao School of Pharmaceutical Science and Technology Tianjin UniversityTianjin 300072China School of International Education Tianjin UniversityTianjin 300072China Clinical School of Changsha Health Vocational College Changsha 410100China tasly Pride Pharmaceutical Company Limited Tianjin 300410China tianjin Pharmaceutical Research Institute Tianjin 300072China

Background:Shengmai decoction,which has been included in the diagnosis and treatment of coronavirus disease 2019(COVID-19),is effective in the early treatment of patients with severe *** Fumai lyophilized injection(YQFM)is a modern Chinese medicine preparation of the Shengmai *** mechanism of its intervention at the molecular level in the severe stage of COVID-19 remains ***,it is necessary to investigate the mechanism of YQFM in the treatment of patients with severe ***:The corresponding target genes of the main active ingredients in YQFM and COVID-19 were obtained by using multiple databases and literature retrieval.A protein-protein interaction network was constructed,and enrichment analysis of the target was performed using Cytoscape ***,the docking of all the identified compounds with angiotensin-converting enzyme II was confirmed by applying molecular docking ***:YQFM has anti-inflammatory effects on RAW267.4 *** main active compounds of YQFM are all effective anti-inflammatory agents,and these active compounds also show beneficial physiological functions,such as anti-oxidation,anti-bacterial,and anticancer *** Ontology analysis showed enrichment in the following pathways:lipopolysaccharides,interleukins,NF-kappa B,interleukin-2 and others,revealing that YQFM may play a role in the treatment of patients with severe COVID-19 through these ***:YQFM has multicomponent and multitarget characteristics,and it could reduce lung injury by inhibiting inflammatory reactions,promoting antiviral activities,and regulating immunity,among other functions,to treat patients with severe COVID-19.

关键词： network pharmacology novel corona virus traditional Chinese medicine natural compounds inflammation

Reducing oxidative stress and hepatoprotective effect of water extracts from Pu-erh tea on rats with high-fat diet

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Food Science and Human Wellness 2016年第4期5卷 199-206页

作者： Jingjing Su Xueqing Wang Wenjun Song Xiaoli Bai Changwen Li tianjin Key Laboratory of Food Biotechnology College of Biotechnology and Food ScienceTianjin University of CommerceTianjin 300134China Yunnan tasly Deepure Biological Tea Group Company Limited Pu ErhYunnan 665100China

Reducing oxidative stress and hepatoprotective effect of Pu-erh tea water extracts on rats fed with high-fat diet were researched for explaining health care of Pu-erh *** SD rats were divided into five *** body weight was measured once a *** malondialdehyde(MDA)and glucose(Glu)levels and the activities of alanine aminotransferase(ALT),aspartate aminotransferase(AST),nitric oxide synthase(NOS),and pyruvate kinase(PK)in serum were ***,the hepatic glycogen level(HGL)and the activities of hepatic total superoxide dismutase(T-SOD),catalase(CAT),and glutathione peroxidase(GSH-Px)were also measured after continuous administration for 12 *** result demonstrated that Pu-erh extract caused the decreases in body weight,fat index,MDA and NOS levels,and the increases in hepatic T-SOD,CAT and GSH-Px activities,indicating that the extract may be due to inhibiting the increases of body weight and fat index,reducing oxidant stress state and inhibiting lipid peroxidation,thus decreasing the activities of ALT and AST,and protecting the liver in ***,the extracts could increase the production of hepatic glycogen and the activity of PK,and reduce glucose level,protecting the liver from the diseases associated with type II diabetes.

关键词： Pu-erh tea extracts Oxidative stress Hepatoprotective effect