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International Journal of Ophthalmology(English edition) 2017年第2期10卷 310-314页

作者： Zhi-Hua Cui Yan Zhang Ling-Ling Liang Zhao-Hui Li Inna Abramova Qian Hao First Hospital of Jilin University Changchun 130021Jilin ProvinceChina People's Hospital of Changchun City Changchun 130000Jilin ProvinceChina pharm.d.candidate 2016Long Island UniversityBrooklyn NY 11201USA

INTROdUCTION Non-small cell lung cancer（NSCLC）is a common malignant disease with an extremely poor *** cancer has been reported to metastasize to the eye in 0.2%to7%of patients based on clinical studies,and in 6%to ... 详细信息

关键词： lung development of a new choroidal metastasis in resistance to crizotinib therapy in anaplastic lymphoma kinaserearranged non-small cell lung cancer NSCLC cell

Synthesis of a highly hydrophobic cyclic decapeptide by solid-phase synthesis of linear peptide and cyclization in solution

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Chinese Chemical Letters 2010年第4期21卷 391-394页

作者： Chen, Jian Zhang, Bei Xie, Cao Lu, Yi Wu, Wei Fudan Univ Sch Pharm Shanghai 201203 Peoples R China

A general method was described to synthesize a highly hydrophobic cyclic peptide,cyclo[LWLWLWLWLQ]where underlines indicate d-configuration of the amino acid,by a two-step solid-phase/solution synthesis *** linear decapeptide was assembled by standard Boc chemistry on solid-phase and subsequently cyclized in solution with high efficiency and reproducibility. In subsequent purification by semi-preparative HPLC,50%(v/v) dMF/H_2O was employed as the solvent to overcome the difficulty of solubilization...

关键词： Cyclic peptide decapeptide cyclo[LWLWLWLWLQ] Solid-phase synthesis Cyclization Purification

Phenolic and nuntritional profiles, and antioxidant activity of grape pomaces and seeds from Lacrima di Morro d'Alba and Verdicchio varieties

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FOOd BIOSCIENCE 2023年第3期53卷 2731-2740页

作者： Abouelenein, doaa Mustafa, Ahmed M. Caprioli, Giovanni Ricciutelli, Massimo Sagratini, Gianni Vittori, Sauro Univ Camerino Sch Pharm Chem Interdisciplinary Project CHIP Via Madonna Carceri I-62032 Camerino Italy Zagazig Univ Fac Pharm Dept Pharmacognosy Zagazig 44519 Egypt

Grape pomace contains high amounts of bioactive compounds, mainly polyphenols, with different concentrations depending on several factors: grape variety, vinification procedures, even within the same cultivar variation may be due to the geographic regions and wine vintage. Therefore, phenolic, antioxidant, macro- and micronutritional composition of wine waste (pomace and seed) originating from Lacrima di Morro d'Alba red grape variety and pomace of Verdicchio white variety were evaluated for the first time. LC-MS/MS analysis showed the presence of 32 phenolic compounds. The phenolic profile was different in pomace of both varieties: white grape pomaces showed the predominance of flavan-3-ols, while anthocyanins were predominant in red pomaces. Comparing seeds and pomace of Lacrima di Morro d'Alba, catechin and epicatechin are representative compounds in red grape seeds, while malvidin-3-galactoside and petunidin-3-glucoside are the most abundant compounds in pomace of all wineries. Highest TPC and antioxidant activities determined by UV-vis spectrophotometer were observed in seed samples. High dietary fibers, polyunsaturated fatty acids, minerals and protein contents were observed in all samples. Wine byproducts of both grape varieties appeared to be a good source of phenolic and nutritional compounds;therefore, they could be a cheap alternative for phenolics production and development of new functional foods.

关键词： Lacrima di Morro d 'Alba Red grape variety White grape variety Verdicchio Grape pomace Grape seeds Phenolic profile Nutritional profile Antioxidant

Clinical Utility of Respiratory Fluoroquinolones from pharmacokinetic-pharmacodynamic Viewpoint

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Clinical Utility of Respiratory Fluoroquinolones from Pharma...

Metabolites of Icariin in Rat Bile Following Oral Administration

第六届全国抗菌药物临床药理学术会议

作者： Keith A．Rodvold Colleges of pharmacy and Medicine University of Illinois at Chicago Pharm．D．

Why pharmacokinetics-pharmacodynamics? Traditional Predictor of Antimicrobial Potency Minimum Inhibitory concentration (MIC) is a good indicator of the potency of antimicrobial activity Alone, MIC does not provide information about the time course of antimicrobial activity Rates of Bactericidal Activity with Increasing drug Concentrations Anti-Infective Activity: Concept # 1 Effect of drug concentration on the rate of bactericidal activity Concentration-dependent: rate and extend of antimicrobial killing is enhanced by increasing drug concentrations Concentration-Independent (or time-dependent): higher drug concentrations do not increase the rate or extend of antimicrobial killing;often saturation of the killing rate occurs at low multiples of the MIC (eg., 4-5 x MIC) Anti-Infective Concentrations & MIC

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Chinese Chemical Letters 1998年第6期9卷 549-552页

作者： Feng QIU Qing Song TAN Ying Jie CHEN Yoshihiro KANO Xin Sheng YAO(Shenyang pharmaceutical University, Shenyang 110015Hokkaido College of pharmacy, Japan) Shenyang pharmaceut Univ Shenyang 110015 Peoples R China Hokkaido Coll pharm Otaru Hokkaido Japan

The biliary metabolites of orally administered icariin in rats were investigated. Two metabolites B-l and B-2 were isolated and identified as icaritin 3-O-alpha-L-rhamnopyranosyl-7-O-beta-d-glucopyranuronoside and ica... 详细信息

关键词： icariin icariside II icaritin 3-O-alpha-L-rhamnopyranosyl-7-O-beta-d-glucopyranuronoside metabolite

Epigenetic regulation of ABCG2 promoter methylation in adolescents with hyperuricemia

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BIOCELL 2024年第12期48卷 1805-1813页

作者： Huang, Xueting Xu, Chaojie Li, Chen Pan, Zhixian Yantian dist Peoples Hosp Dept Nephrol & Rheumatol Shenzhen 518000 Peoples R China Zhengzhou Univ Affiliated Hosp 5 Dept Urol Zhengzhou 450000 Peoples R China Free Univ Berlin Dept Biol Chem Pharm D-14195 Berlin Germany

Background: Hyperuricemia is a metabolic disorder which is characterized by increased serum uric acid levels, which can contribute to serious health issues such as gout, cardiovascular disease, and kidney damage. Epigenetic modifications, for example, dNA methylation, exert a crucial function in gene regulation and have been implicated in various metabolic disorders. The ATP-Binding Cassette Subfamily G Member 2 (ABCG2) gene is involved in uric acid excretion, and its expression can be influenced by methylation of its promoter region. Methods: This study involved the design of three guide RNA (gRNA) sequences targeting specific CpG sites within the ABCG2 promoter region. Using the Clustered Regularly Interspaced Short Palindromic Repeats/dead Cas9-Ten-Eleven Translocation 1 (CRISPR/dCas9-TET1) system, these gRNAs were employed to guide targeted demethylation of the ABCG2 promoter in cell models. A non-targeting gRNA served as a negative control. The methylation status of the ABCG2 promoter and its effect on gene expression were assessed using bisulfite sequencing and qRT-PCR. Results: Among the gRNAs tested, gRNA2 and gRNA3 effectively guided the dCas9-TET1 complex to the ABCG2 promoter, resulting in significant demethylation. gRNA2 showed the most pronounced effect, leading to a substantial increase in ABCG2 expression. Clinical data analysis revealed that adolescents with hyperuricemia had higher uric acid levels compared to healthy controls, and a higher proportion of the hyperuricemia group reported a high-protein diet, suggesting a link between diet and ABCG2 methylation. Conclusion: The findings demonstrate that targeted demethylation of the ABCG2 promoter can significantly upregulate its expression, which may help modulate uric acid levels. These results indicate that dietary factors, such as a high-protein diet, could influence ABCG2 methylation and thus impact hyperuricemia. Advanced research is necessary to explore the therapeutic potential of aiming at ep

关键词： Hyperuricemia ABCG2 Methylation CRISPR/dCas9-TET1

Improved Trial designs and drug development Using Modeling and Simulation

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Improved Trial Designs and Drug Development Using Modeling a...

SOLUTION PROPERTIES OF ANTITUMOR CARBOXYMETHYLATEd dERIVATIVES OF α-(1→3)-d-GLUCAN FROM GANOdERMA LUCIdUM

第十二次全国临床药理学学术会议

作者： Richard Lalonde pharm.d.Vice President and Global Head of Clinical pharmacology Pfizer

Overview Current challenges and opportunities in drug development Modeling and simulation based on clinical pharmacology principles Examples of modeling and simulation in drug development at Pfizer Impact on trial des...

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Chinese Journal of Polymer Science 2001年第3期19卷 283-289页

作者： Li-na Zhang Mei Zhang Jing-hua Chen Fan-bo Zeng department of Chemistry Wuhan University, Wuhan 430072, China pharmacy College, Tongji Medical University, Wuhan 430072, China Wuhan Univ Dept Chem Wuhan 430072 Peoples R China Tongji Med Univ Coll Pharm Wuhan 430072 Peoples R China

Fractions of a water insoluble α-(1→3)-d-glucan (GL) extracted from Ganoderma lucidum were carboxy-methylated (CM) to obtain water-soluble carboxymethylated derivatives (CM-GL) having a degree of substitution (dS) of0.38～0.51. Weight-average molecular weight M_w and intrinsic viscosity [η] of the samples CM-GL were measured by gelpermeation chromatography combined with laser light scattering (GPC-LLS) and viscometry. The CM-GL exhibits a stifferchain in aqueous solution at 25℃ than the original glucan, The antitumor activities against Ehrlich ascites carcinoma (EAC,5×10~6) of the carboxymethylated derivatives from the α-glucan and curdlan, a β-glucan, are significantly higher than thoseof the original glucans. The effects of the relatively low molecular weight, expanded chains and better water-solubility of theCM-GL on the enhancement of antitumor activity could not be neglected. The chain stiffness decreased speedily withincrease of temperature from 40 to 60℃ or NaOH concentration from 0.1 to 0.4 in the solution, respectively, and the changeof the chain stiffness is reversible.

关键词： Solution properties Antitumor activity Carboxymethylated derivative α-d-glucan Ganoderma lucidum

Evaluation of antiplasmodial properties in 15 selected traditional medicinal plants from India

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Journal of Integrative Medicine 2020年第1期18卷 80-85页

作者： Yogesh Subhash Biradar Swathi Bodupally Harish Padh department of pharmacognosy and Phytochemistry Bharat School of PharmacyMangalpallyIbrahimpatnamHyderabad 501510TelanganaIndia department of pharm d Bharat School of PharmacyMangalpallyIbrahimpatnamHyderabad 501510TelanganaIndia department of Biotechnology B.V.Patel Pharmaceutical Education and Research Development CentreThaltej-Gandhinagar HighwayThaltejAhmedabad 380054GujaratIndia

Objective:The objective of this study was to evaluate the in vitro antiplasmodial properties against malaria parasite in 15 plants mentioned in Indian traditional medicine ***:In vitro antiplasmodial activity of methanolic extracts obtained from Indian traditional medicinal plants was evaluated on Plasmodium falciparum of FCK2 and INdO strains using schizont maturation inhibition assay and parasite lactate dehydrogenase inhibition ***:Methanolic extracts of Adhatoda zeylanica,Embelia ribes,Piper nigrum and Plumbago zeylanica exhibited more than 50%inhibition in both the stains in schizont maturation inhibition *** extracts of seven medicinal plants exhibited antiplasmodial activity at half maximal inhibitory concentration(IC50)d methanolic extracts of five medicinal plants exhibited antiplasmodial activity at IC50dehydrogenase(PfLdH)inhibition ***,*** and *** exhibited promising antiplasmodial activity in PfLdH inhibition *** and *** exhibited improved activity against resistant in comparison to sensitive ***:*** and *** were the most promising extracts from this study and deserve further investigation of their antiplasmodial properties.

关键词： Medicinal plants Plasmodium falciparum Schizont maturation inhibition assay Lactate dehydrogenase inhibition assay Cytotoxicity

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新药给糖尿病患者带来希望

中国处方药 2006年第11期5卷 72-73页

作者： Kathy Hitchens 菅鑫妍 pharm.d. MSBA

竞争已经拉开了序幕.对1型和2型糖尿病,各个制药厂家都希望通过研发可以更好的治疗疾病、改善患者生活质量以及最终能彻底的预防糖尿病并发症发生的新治疗方法来获得在这一领域内的重要位置.

关键词：糖尿病患防糖尿病并发症新药患者生活质量治疗方法 2型糖尿病