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Asian Pacific Journal of Tropical Biomedicine 2019年第2期9卷 53-59页

作者： Da Eun Kim Yeon Sil Hwang Bo Yoon Chang Dae Sung Kim Hyoung Kwon Cho Sung Yeon Kim Institute of pharmaceutical Research and Development College of PharmacyWonkwang University hanpoong pharm.co. Ltd

Objective: To investigate cosmetic potential of Syzygium aromaticum L.(S. aromaticum L.) and to determine its antioxidant and anti-wrinkling effects. Methods: Using highperformance liquid chromatography, eugenol component was quantitated. The antioxidant activity of S. aromaticum L. was analyzed by 2,2-diphenyl-1-picrylhydrazyl radical scavenging and superoxide dismutase like activities. To determine cell viability, elastase and matrix metalloproteinase-1(MMP-1) activity, human dermal fibroblasts(HS68) were treated with S. aromaticum L. The inhibitory effect of S. aromaticum L. on tumor necrosis factor alpha induced MMPs expression in HS68 was analyzed by realtime-PCR. Results: The eugenol content was confirmed in S. aromaticum L. S. aromaticum L. was observed to have high 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity and superoxide dismutase like activity. S. aromaticum L. had no cytotoxicity against the HS68 and dose-dependently increased elastase inhibition. Moreover, S. aromaticum L. significantly decreased MMP-1 content and inhibited gene levels of MMP-1, MMP-2, MMP-3 and MMP-9. conclusions: The findings suggest that S. aromaticum L. has great potential as a cosmeceutical ingredient with antioxidant and antiwrinkling effects.

关键词： Syzygium aromaticum L Antioxidant Anti-aging Elastase Matrix metalloproteinase-1

Risk of ischaemic stroke in patients with transient global amnesia: a propensity-matched cohort study

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Stroke & Vascular Neurology 2022年第2期7卷 101-107页

作者： Sang Hun Lee Keon-Yeup Kim Jeong-Woo Lee So-Jeong Park Jin-Man Jung Department of Neurology Korea University Ansan HospitalKorea University College of MedicineAnsanRepublic of Korea Data Science Team Hanmi Pharm.Co.LtdSeoulRepublic of Korea Korea University Zebrafish Translational Medical Research Center AnsanRepublic of Korea

Background The exact pathophysiological mechanism of transient global amnesia(TGA)is *** is debatable whether TGA is a risk factor for ***,here we investigated the possibility of TGA as a risk factor for stroke in a real-world setting using large-scale nationwide health claims *** We used health claims data from the Korean National Health Insurance Service(NHIS).Patients diagnosed with TGA between 2007 and 2013 were *** initially extracted patients without TGA who were preferentially matched for age and sex with the patients with TGA at a ratio of 10:1 from the whole ***,we performed 1:2 propensity score matching analysis to balance the baseline characteristics between the two *** the propensity score-matched dataset,we performed multivariable cox regression analysis to investigate the association between TGA and stroke type,including ischaemic,haemorrhagic and all stroke *** Patients with TGA(n=14673)were selected from the NHIS *** extracting from the whole database(n=140486)and propensity score matching their data at a 1:2 ratio,a total of 10448 and 20442 patients were finally assigned to the TGA and control groups,*** multivariable cox regression analysis demonstrated that the TGA group had a higher risk of ischaemic stroke and all types of stroke(adjusted HR=1.194;95%CI:1.043 to 1.368;and HR=1.197;95%CI:1.056 to 1.357,respectively).conclusions Analysis of the nationwide claims database showed that TGA could be an important risk factor for stroke,especially for ischaemic stroke.

关键词： patients matched transient

Influence of physical properties of carrier on the performance of dry powder inhalers

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Acta pharmaceutica Sinica B 2016年第4期6卷 308-318页

作者： Tingting Peng Shiqi Lin Boyi Niu Xinyi Wang Ying Huang Xuejuan Zhang Ge Li Xin Pan Chuanbin Wu School of pharmaceutical Sciences Sun Yat-Sen University Guangzhou Neworld pharm. co. Ltd. Guangdong Research Center for Drug Delivery Systems

Dry powder inhalers(DPIs) offer distinct advantages as a means of pulmonary drug delivery and have attracted much attention in the field of pharmaceutical science. DPIs commonly contain micronized drug particles which, because of their cohesiveness and strong propensity to aggregate, have poor aerosolization performance. Thus carriers with a larger particle size are added to address this problem. However, the performance of DPIs is profoundly influenced by the physical properties of the carrier, particularly their particle size, morphology/shape and surface roughness. Because these factors are interdependent, it is difficult to completely understand how they individually influence DPI *** purpose of this review is to summarize and illuminate how these factors affect drug–carrier interaction and influence the performance of DPIs.

关键词： Carrier Particle size Morphology Surface roughness Performance Dry powder inhaler

UPLCeMS/MS for the determination of azilsartan in beagle dog plasma and its application in a pharm.co.inetics study

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Asian Journal of pharmaceutical Sciences 2015年第3期10卷 247-253页

作者： Cheng Gong Junfeng Wang Yinghua Sun Dawei Ding Lu Zhong Meng Zhu Jin Sun Xiangrong Zhang Shenyang pharmaceutical University No.103Wenhua RoadShenyang 110016China Shandong Weigao pharm.co.Ltd. Weihai 264200China

The purpose of the study is to develop an ultra performance liquid chromatographytandem mass spectrometry(UPLCeMS/MS)to determinate the concentration of azilsartan in the dog *** precipitated by methanol,the plasma sample containing azilsartan and diazepam(internal standard,IS)was determined by UPLCeMS/*** mobile phase consisted of acetonitrile-water was pumped at a flow rate of 0.3 ml/min in gradient *** 2.6 m XB-C18 column(502.1 mm,100Å;Phenomenex,USA)were used for LC *** column temperature was 30℃ and the injection volume was 5 *** electrospray ionization(ESI)and multiple reaction monitoring(MRM)were applied at the transitions of m/z 457/279(azilsartan)and m/z 285/193(diazepam),*** developed method was identified a good linearity over a concentration range of 2.5e5000 ng/*** lower limit of quantitation(LLOQ)was 2.5 ng/*** intraday and inter-day precision(relative standard deviation,RSD%)were less than 10%and accuracy(relative error,RE%)was less than 5%at three quality control *** extraction recovery of azilsartan at three quality control levels were 82.41±0.68%,98.66±11.00%,102.43±0.82%.And the recovery for IS(100 ng/ml)was 91.75±0.54%.A validated UPLCeMS/MS method was firstly developed for the quantification of azilsartan in dog plasma and it was applied to the pharm.co.inetics study.

关键词： Azilsartan UPLCeMS/MS pharm.co.inetics study

Total Synthesis of (-)-Tetrahydrolipstatin by the Tandem Mukaiyama-aldol Lactonization

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Chinese Chemical Letters 2005年第11期16卷 1448-1450页

作者： Jian YIN Xiao Bo YANG Zai Xin CHEN Yi Hua ZHANG Center of Drug Discovery China Pharmaceutical University Nanjing 210009 Jiangsu Yabang pharm. Res. ＆ Dev. co. Ltd Nanjing 210004

（-）-Tetrahydrolipstatin 1 was synthesized in three steps and 33.8% overall yield from aldehyde 6 by tandem Mukaiyama-aldol lactonization, which offered a concise, efficient and highly diastereoselective route to this antiobesity drug. We also presented a resolution method for preparation of the crucial intermediate, β- （t-butyldimethylsilyloxy）tetradecanal.

关键词： Tetrahydrolipstatin tandem Mukaiyama-aldol lactonization asymmetric synthesis,(R)-β-hydroxy tetradecanal resolution.

Development of an eco-friendly and fast HPLC method for quantitative analysis of four nucleosides in cordyceps and related products

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Chinese Journal of Natural Medicines 2021年第12期19卷 954-960页

作者： QIAN Zheng-Ming WU Zi HUANG Qi WANG Chuan-Xi TAN Guo-Yin LI Wen-Jia SUN Wan-Yang LV Gen-Pin GAO Hao Institute of Traditional Chinese Medicine and Natural Products College of PharmacyJinan UniversityGuangzhou 510632China Ruyuan HEC pharm.co. Ltd.Shaoguan 512700China

An eco-friendly and fast HPLC method was developed for the determination of adenosine, inosine, guanosine and uridine in cordyceps and related products(fermented mycelia of Hirsutella sinensis and Paecilomyces hepiali). The sample was ultrasonically extracted using 0.5% phosphoric acid solutions for 2.5 min. Sample separation was performed on a Poroshell SB-Aq column(50 mm × 4.6 mm, 2.7 μm) using eco-friendly mobile phase consisting of formic acid and ammonium formate aqueous solution at a flow rate of 1.0 m L·min;. The detection wavelength was 260 nm. The developed HPLC method showed good linearity with correlation coefficients of 1.0000 in the test range. Good precision, repeatability and stability of this method were also observed(RSD ≤ 2.81%).The recovery ranged from 91.84%-105.19%(RSD ≤ 2.59%). compared with reported methods, the current method did not use harmful organic solvent and took only 10.5 min. It obtained a high eco-score of 91 by the "Analytical Eco-Scale" tool. The developed method is eco-friendly and fast, which is suitable for the quality evaluation of cordyceps and related products.

关键词： Adenosine Inosine Guanosine Uridine cordyceps

Increased susceptibility of ethanol-treated gastric mucosa to naproxen and its inhibition by DA-9601, an Artemisia asiatica extract

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World Journal of Gastroenterology 2005年第47期11卷 7450-7456页

作者： Tae Young Oh Gook Jun Ahn Seul Min Choi Byoung Ok Ahn Won Bae Kim Research Laboratories Dong-A Pharm. Co.Ltd.47-5SanggalKiheungYonginKyunggi449-905South Korea

AIM： To examine the effect of DA-9601, a new gastroprotective agent, on the vulnerability of ethanoltreated rat＇s stomach to naproxen （NAP）. METHODS： Male Sprague-Dawley rats were pretreated with 1 mL of 50% ethanol twice a day for 5 d and then NAP （50 mg/kg） was administered. DA-9601 was admin- istered 1 h before NAP. Four hours after NAP, the rats were killed to examine gross injury index （mm2）, histologic change and to determine mucosal levels of malondialdehyde （MDA）, prostaglandin E2 （PGE2）, glutathione （GSH） and myeloperoxidase （MPO）. RESULTS： Pretreatment of ethanol significantly increased NAP-induced gastric lesions, as well as an increase in NDA and MPO. On the contrary, mucosal PGE2 and GSH contents were decreased dramatically by ethanol pretreatment, which were aggravated by NAR DA-9601 significantly reduced NAP-induced gastric injury grossly and microscopically, regardless of pretreatment with ethanol. DA-9601 preserved, or rather, increased mucosal PGE2 and GSH in NAP-treated rats （P〈0.05）, with reduction in mucosal MDA and MPO levels. coNCLUSION： These results suggest that repeated alcohol consumption renders gastric mucosa more susceptible to NSAIDs though, at least in part, reduction of endogenous cytoprotectants including PGE2 and GSH, and increase in MPO activation, and that DA-9601, a new gastroprotectant, can reduce the increased vulnerability of ethanol consumers to NSAIDs-induced gastric damage via the mechanism in which PGE2 and GSH are involved.

关键词： DA-9601 Alcohol Naproxen Gastric damage Malondialdehyde Prostaglandin E2 Glutathione Myeloperoxidase NSAIDS

DLX5 promotes col10a1 expression and chondrocyte hypertrophy and is involved in osteoarthritis progression

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Genes & Diseases 2023年第5期10卷 2097-2108页

作者： Jinnan Chen Fangzhou Chen Xuan Wu Huiqin Bian Chen Chen Xiaojing Zhang Ruoxuan Hei Xiaotong Yang Haochun Yuan Qian Wang Yaojuan Lu Longwei Qiao Qiping Zheng Department of Laboratory Medicine School of MedicineJiangsu UniversityZhenjiangJiangsu 212013China Department of Pathology The Affiliated People's Hospital of Jiangsu UniversityZhenjiangJiangsu 212002China The Affiliated Suzhou Hospital of Nanjing Medical University NanjingJiangsu 215008China Shenzhen Walgenron Bio-pharm.co.Ltd. ShenzhenGuangdong 518118China

Osteoarthritis(OA)has been considered non-reversible as articular cartilage wears down with limited repair *** chondrocyte hypertrophy and increased type X collagen gene(coL10A1)expression have been associated with ***,regulators controlling collagen X expression and chondrocyte hypertrophy may play a role in OA ***,we investigated how Distal-less homeobox 5(DLX5),the distal-less homeobox family member,controls murine col10a1 gene expression and chondrocyte hypertrophy in chondrogenic cell models and its role in a murine OA *** qRT-PCR and Western blot analyses,we detected significantly increased levels of coL10A1 and DLX5 in hypertrophic MCT and ATDC5 cells compared to their proliferative *** expression of Dlx5 further increases,while knockdown of Dlx5 decreases coL10A1 expression in hypertrophic MCT *** have performed dual-luciferase reporter and ChiP assays and demonstrated that DLX5 promotes reporter activity through direct interaction with col10a1 *** established a murine OA model and detected markedly increased coL10A1 and DLX5 in the articular cartilage and subchondral bone of the OA mice compared with the ***,forced overexpression of DLX5 in hypertrophic MCT cells up-regulates RUNX2,and adjacent DLX5 and RUNX2 binding sites have previously been found within the col10a1 ***,our data suggest that DLX5 may cooperate with RUNX2 to control cell-specific col10a1 expression and chondrocyte hypertrophy and is involved in OA pathogenesis.

关键词： Chondrocyte hypertrophy col10a1expression DLX5 Osteoarthritis RUNX2

Synthesis of cyclic peptide reniochalistatin E and conformational isomers

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Chinese Chemical Letters 2018年第7期29卷 1143-1146页

作者： Huiyun Luo Hongli Yin Chaojun Tang Ping Wang Feng Liang The State Key Laboratory of Refractories and Metallurgy School of Chemistry and Chemical Engineering Wuhan University of Science and TechnologyWuhan 430081 China Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs School of Chemistry and Chemical Engineering Shanghai Jiao Tong University Shanghai200240 China Chonqqing Huapont pharm. co. Ltd. Chongqing 401121 China

Here, we report a convenient and efficient synthesis strategy for the total synthesis of cyclic peptide reniochalistatin E and its conformational isomers with 32% overall yield. We found the linear peptide precursor w... 详细信息

关键词： Cyclic peptide Reniochalistatin E Solid-phase peptide synthgesis conformational isomers

Oral bacteria colonize and compete with gut microbiota in gnotobiotic mice

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International Journal of Oral Science 2019年第3期11卷 192-200页

作者： Bolei Li Yang Ge Lei Cheng Benhua Zeng Jinzhao Yu Xian Peng Jianhua Zhao Wenxia Li Biao Ren Mingyun Li Hong Wei Xuedong Zhou State Key Laboratory of Oral Diseases & National Clinical Research Center for Oral Diseases Sichuan UniversityChengduChina Department of Cariology and Endodontics West China Hospital of StomatologySichuan UniversityChengduChina Department of Laboratory Animal Science College of Basic Medical SciencesThird Military Medical UniversityChongqingChina Shanghai Majorbio Bio-pharm Technology co. LtdShanghaiChina

The oral microbiota is associated with oral diseases and digestive systemic ***,the causal relationship between them has not been completely elucidated,and colonisation of the gut by oral bacteria is not clear due to the limitations of existing research *** aim of this study was to develop a human oral microbiota-associated (HOMA) mouse model and to investigate the ecological invasion into the *** transplanting human saliva into germ-free (GF) mice,a HOMA mouse model was first constructed.16S rRNA gene sequencing was used to reveal the biogeography of oral bacteria along the cephalocaudal axis of the digestive *** the HOMA mice,84.78% of the detected genus-level taxa were specific to the *** component analysis (PCA) revealed that the donor oral microbiota clustered with those of the HOMA mice and were distinct from those of specific pathogen-free (SPF) *** HOMA mice,OTU counts decreased from the stomach and small intestine to the distal *** distal gut was dominated by Streptococcus,Veillonella,Haemophilus,Fusobacterium,Trichococcus and *** mice and human microbiota-associated (HMA) mice along with the GF mice were then *** communities of cohoused mice clustered together and were significantly separated from those of HOMA mice and HMA *** Source Tracker analysis and network analysis revealed more significant ecological invasion from oral bacteria in the small intestines,compared to the distal gut,of cohoused *** conclusion,a HOMA mouse model was successfully *** overcoming the physical and microbial barrier,oral bacteria colonised the gut and profiled the gut microbiota,especially in the small intestine.

关键词： microbiota germ-free component analysis