Open Medicinal Chemistry Journal最新文献_第10页

Cell engineering and molecular pharming for biopharmaceuticals. 用于生物制药的细胞工程和分子制药。

Open Medicinal Chemistry Journal Pub Date : 2008-05-14 DOI: 10.2174/1874104500802010049

M A Abdullah, Anisa Ur Rahmah, A J Sinskey, C K Rha

引用次数: 0

A new concept for smart drug delivery: adhesion induced nanovector implosion. 智能给药新概念:粘附诱导纳米载体内爆。

Open Medicinal Chemistry Journal Pub Date : 2008-05-14 DOI: 10.2174/1874104500802010062

Nicola M Pugno

引用次数: 7

Identification and characterization of skin biomolecules for drug targeting and monitoring by vibrational spectroscopy. 振动光谱技术用于药物靶向和监测的皮肤生物分子的鉴定和表征。

Open Medicinal Chemistry Journal Pub Date : 2008-05-08 DOI: 10.2174/1874104500802010038

Natalja Skrebova Eikje, Katsuo Aizawa, Takayuki Sota, Yukihiro Ozaki, Seiji Arase

{"title":"Identification and characterization of skin biomolecules for drug targeting and monitoring by vibrational spectroscopy.","authors":"Natalja Skrebova Eikje, Katsuo Aizawa, Takayuki Sota, Yukihiro Ozaki, Seiji Arase","doi":"10.2174/1874104500802010038","DOIUrl":"https://doi.org/10.2174/1874104500802010038","url":null,"abstract":"The article discusses the application of vibrational spectroscopy techniques for in vivo identification and characterization of glucose biomolecules monitored in the skin of healthy, prediabetes and diabetes subjects; for molecular characterization of water and proteins in in vivo monitored patch tested inflamed skin of the patients with contact dermatitis; for description of nucleic acids and proteins at the molecular level with progression to malignancy in skin cancerous lesions. The results of the studies show new possibilities to assess activity levels of glucose metabolism in the skin tissue of healthy, prediabetes and diabetes subjects; activity and severity of inflammation; activity of the processes of carcinogenesis with regard to benign, premalignant and malignant transformation. Based on our findings, we suggest that vibrational spectroscopy might be a rapid screening tool with sufficient sensitivity and specificity to identify and characterize skin biomolecules in described diseases for drug targeting and monitoring by the pharmacological community.","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2008-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1874104500802010038","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40019605","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 14

Microwave-Assisted Syntheses of Amino Acid Ester Substituted Benzoic Acid Amides: Potential Inhibitors of Human CD81-Receptor HCV-E2 Interaction. 微波辅助合成氨基酸酯取代苯甲酸酰胺：人类 CD81-受体 HCV-E2 相互作用的潜在抑制剂。

Open Medicinal Chemistry Journal Pub Date : 2008-04-15 DOI: 10.2174/1874104500802010021

Marcel Holzer, Sigrid Ziegler, Bernd Kronenberger, Christian D Klein, Rolf W Hartmann

引用次数: 0

Cyclobutane-containing alkaloids: origin, synthesis, and biological activities. 含环丁烷的生物碱：起源、合成和生物活性。

Open Medicinal Chemistry Journal Pub Date : 2008-04-15 DOI: 10.2174/1874104500802010026

Anastasia Sergeiko, Vladimir V Poroikov, Lumir O Hanus, Valery M Dembitsky

引用次数: 0

Molecular docking and analysis of survivin delta-ex3 isoform protein. survivin δ -ex3亚型蛋白的分子对接与分析。

Open Medicinal Chemistry Journal Pub Date : 2008-03-27 DOI: 10.2174/1874104500802010016

Z Ezziane

引用次数: 4

A New Generation Prothrombin Time Method for INR. 新一代凝血酶原时间法检测 INR。

Open Medicinal Chemistry Journal Pub Date : 2008-02-27 DOI: 10.2174/1874104500802010011

Juha Horsti, Helena Uppa, Juhani A Vilpo

{"title":"A New Generation Prothrombin Time Method for INR.","authors":"Juha Horsti, Helena Uppa, Juhani A Vilpo","doi":"10.2174/1874104500802010011","DOIUrl":"10.2174/1874104500802010011","url":null,"abstract":"Prothrombin time (PT) is the leading test for monitoring oral anticoagulation therapy (OAT). We sought to determine INR taking into account only active coagulation factors FII, FVII and FX without inhibition in patient plasmas and calibrator kits.We measured PT using a combined thromboplastin reagent. The calculation was based on a new PT method, which measures active coagulation factors (F II, F VII, FX) and corrects the errors caused by inactive coagulation factors.On this basis, an INR result with and without inhibition for individual patient samples was also calculated and applied to 200 plasma samples obtained from OAT patients. Conspicuous variation in inhibition between the four calibration kits was noted. The kinetics of this inhibition was closest to a noncompetitive pattern.The need of correction for INRs of single patients increases with higher INRs. At the same level of patient INRs the coagulation inhibiton varies markedly.It has been known that different thromboplastin reagents possess variable sensitivities, but this may depend on sensitivity in inactive coagulation factors. PT methods today measure the sum of active coagulation factors and inhibition of inactive coagulation factors. ISI calibrators contain variable amounts of inactive coagulation factors, which renders harmonisation of INR results.Application of the Acf-PT (INR(Acf)) presented in this work develops the PT methodology to measure the true coagulation activity in vivo for patient warfarin therapy without inhibition. INR(Inh) can evidently also be used for the diagnostics and follow-up of certain liver diseases.","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2008-02-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2709469/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40018582","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Important bioactive molecules of erythrocytes in colorectal cancer patients after colectomy. 结直肠癌患者结肠切除术后红细胞的重要生物活性分子。

Open Medicinal Chemistry Journal Pub Date : 2008-02-27 DOI: 10.2174/1874104500802010006

Anna Blázovics, Agnes Szilvás, György Székely, Eniko Tordai, Edit Székely, Gábor Czabai, Zsolt Pallai, Eva Sárdi

{"title":"Important bioactive molecules of erythrocytes in colorectal cancer patients after colectomy.","authors":"Anna Blázovics, Agnes Szilvás, György Székely, Eniko Tordai, Edit Székely, Gábor Czabai, Zsolt Pallai, Eva Sárdi","doi":"10.2174/1874104500802010006","DOIUrl":"https://doi.org/10.2174/1874104500802010006","url":null,"abstract":"Formaldehyde (HCHO) and protoporphyrin, are in connection with redox homeostasis. Data show the importance of HCHO in proliferative as well as in apoptotic processes. Free protoporphyrin can be detected near the Zn-protoporphyrin in cancer and it has pro- and antioxidant forms depending on concentrations. The aim was to determine the amount of HCHO and protoporphyrin concentrations of erythrocytes in colorectal cancer after colectomy and to estimate redox homeostasis. Total 32 adult patients after 5-10 years of colectomy and 9 healthy volunteers were drawn into this study. Tumor markers, redox parameters, HbA1c, HCHO and protoporphyrin concentrations were measured. Erytrocyte HCHO was significantly lower in colectomysed patients, than in controls. Protoporphyrin concentration was low in patients, but in metastasis its concentration was significant. HbA1c correlated significantly with free radicals and decreased the antioxidant status of erythrocytes. HCHO and protoporphyrin concentrations of erythrocytes and the total scavenger capacity are very important indexes in cancer.","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2008-02-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2709480/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40018581","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 14

Chronic experimental diabetes accelerates urinary elimination of deprenyl and its metabolites. 慢性实验性糖尿病会加速去甲肾上腺素及其代谢物在尿液中的排出。

Open Medicinal Chemistry Journal Pub Date : 2008-01-10 DOI: 10.2174/1874104500802010001

Ernest Adeghate, Péter Sótonyi, Huba Kalász

{"title":"Chronic experimental diabetes accelerates urinary elimination of deprenyl and its metabolites.","authors":"Ernest Adeghate, Péter Sótonyi, Huba Kalász","doi":"10.2174/1874104500802010001","DOIUrl":"10.2174/1874104500802010001","url":null,"abstract":"Many diabetic patients take several medications to treat diabetes-associated complications and other ailments. The mode of elimination of these drugs and their metabolites are poorly understood. The elimination of deprenyl, a MAO-B inhibitor, used for the treatment of the early stage of Parkinson's disease and senile dementia was investigated using thin layer chromatography.Male Wistar rats (180-200 g) were rendered diabetic by streptozotocin (STZ) treatment (60 mg/kg, i.v.). Rats having at least three times higher plasma glucose level than the normal were considered diabetic. Rats were treated with a single oral dose of 5 mg/kg (14)C-(methyl)-labeled (-)-deprenyl, 98 microCi/mg. Diabetic rats excreted the majority of urinary radioactivity in 8 hours, while control rats did it in 16 hours. The approximate ratio of major metabolites as determined using thin-layer chromatography did not change. In conclusion, diabetic rats excreted radiolabelled-deprenyl more rapidly compared to control animals. Increased elimination of deprenyl should be taken into account in the management of patients suffering from diabetes.","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2008-01-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2709476/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40018580","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Heteroarotinoids with anti-cancer activity against ovarian cancer cells. 对卵巢癌细胞具有抗癌活性的类杂胡萝卜素。

Open Medicinal Chemistry Journal Pub Date : 2007-10-24 DOI: 10.2174/1874104500701010011

Thanh C Le, K Darrell Berlin, Stacy D Benson, Margaret A Eastman, Gianna Bell-Eunice, Anna C Nelson, Doris M Benbrook

{"title":"Heteroarotinoids with anti-cancer activity against ovarian cancer cells.","authors":"Thanh C Le, K Darrell Berlin, Stacy D Benson, Margaret A Eastman, Gianna Bell-Eunice, Anna C Nelson, Doris M Benbrook","doi":"10.2174/1874104500701010011","DOIUrl":"https://doi.org/10.2174/1874104500701010011","url":null,"abstract":"The Flex-Het compound 10a (SHetA2-NSC 721689) {[4-nitrophenylamino][(2,2,4,4-tetramethylthiochroman-6-yl)amino]methane-1-thione]} has shown promise in preclinical testing as an anti-cancer agent without evidence of toxicity, skin irritancy, or teratogenicity. One objective of this study was to synthesize a series of heteroarotinoids structurally related to SHetA2 and to measure the effect of structural alterations on the cytotoxicity activities of the compounds on A2780 ovarian cancer cells. Alterations included comparisons of activity of an NO2 end group versus a CO2Et end group, a thiourea linker versus a urea linker, and a distorted, thiochroman ring unit versus a planar quinoline ring unit. Cytotoxicity assays demonstrated the thiourea linker compounds to be similar in potency to the urea linker counterparts, the NO2 substitutions were slightly more potent than the CO2Et substitutions, and replacement of the thiochroman group with a planar quinoline fused ring system markedly reduced activity. The mechanism of cytotoxicity through apoptosis was confirmed for the compounds. The optimal combination of structural features for enhancing potency consisted of a urea linker, a NO2 substitution, and a flexible thiochroman unit. Extensive H-bonding in the more active urea derivative was confirmed by X-ray and NMR analyses. This is the first example in which the biological activity of flexible, thiochroman units is compared to that of fused aryl units in a heteroarotinoid molecule.","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2007-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2709466/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40018579","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 16