Drug discoveries & therapeutics最新文献_第5页

Purification of innate immunostimulant from green tea using a silkworm muscle contraction assay. 用蚕肌收缩法从绿茶中纯化天然免疫刺激剂。

IF 3.1

Drug discoveries & therapeutics Pub Date : 2011-02-01 DOI: 10.5582/ddt.v5.1.18

S Dhital, H Hamamoto, M Urai, K Ishii, K Sekimizu

引用次数: 15

Anti-influenza viral effects of novel nuclear export inhibitors from Valerianae Radix and Alpinia galanga. 缬草和高良姜新型核输出抑制剂的抗流感病毒作用。

IF 3.1

Drug discoveries & therapeutics Pub Date : 2011-02-01 DOI: 10.5582/ddt.v5.1.26

K Watanabe, H Takatsuki, M Sonoda, S Tamura, N Murakami, N Kobayashi

{"title":"Anti-influenza viral effects of novel nuclear export inhibitors from Valerianae Radix and Alpinia galanga.","authors":"K Watanabe, H Takatsuki, M Sonoda, S Tamura, N Murakami, N Kobayashi","doi":"10.5582/ddt.v5.1.26","DOIUrl":"https://doi.org/10.5582/ddt.v5.1.26","url":null,"abstract":"Many pathogenic viruses, such as the influenza virus and the Human Immunodeficiency Virus (HIV)-1, are a threat to humans, thus leading to thousands of deaths annually. The development of antiviral drugs is urgent, and it is an essential strategy for the suppression of these infectious diseases. However, regardless of the rapid emergence of many infectious diseases, the development of novel antiviral drugs has been slow, except for the case of the AIDS. In addition, several viruses can easily mutate and escape the inhibitory activity of anti-viral drugs. It was already well-established that HIV escapes from anti-viral drug effects because of the lack of proofreading activity in its reverse transcriptase. It is known that the influenza virus, which is resistant to Tamiflu, is already spread all over the world. Viruses utilize the host cell environment and cellular factors to propagate. Therefore, the development of novel drugs which inhibit viral protein-host protein interactions or cellular functions appear to be good candidates. The influenza virus is unique in replicating in host nuclei, and we therefore focused on the nuclear export processes for the development of anti-influenza viral drugs. We previously reported that leptomycin B (LMB), which inhibited the nuclear export processes via the nuclear export signal (NES) inhibited the nuclear export of influenza viral RNP (vRNP), and resulted in the inhibition of influenza viral propagation. We herein examined novel CRM1 inhibitors, valtrate from Valerianae Radix, and 1'-acetoxychavicol acetate (ACA) from Alpinia galanga as potent inhibitors for the influenza virus replication.","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"26-31"},"PeriodicalIF":3.1,"publicationDate":"2011-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5582/ddt.v5.1.26","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30543382","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 31

A sensitive near-infrared fluorescent probe for caspase-mediated apoptosis: Synthesis and application in cell imaging. caspase介导细胞凋亡的近红外荧光探针：合成及其在细胞成像中的应用。

Drug discoveries & therapeutics Pub Date : 2011-01-01 DOI: 10.5582/ddt.2011.v5.5.220

Yepeng Luan, Qiuhong Yang, Yumei Xie, Shaofeng Duan, Shuang Cai, M L Forrest

引用次数: 0

The Neuroprotective Effect of Antidepressant Drug via Inhibition of TIEG2-MAO B Mediated Cell Death. 抗抑郁药物通过抑制TIEG2-MAO B介导的细胞死亡的神经保护作用

Drug discoveries & therapeutics Pub Date : 2008-10-01

Deyin Lu, Chandra Johnson, Shakevia Johnson, Shawna Tazik, Xiao-Ming Ou

{"title":"The Neuroprotective Effect of Antidepressant Drug via Inhibition of TIEG2-MAO B Mediated Cell Death.","authors":"Deyin Lu, Chandra Johnson, Shakevia Johnson, Shawna Tazik, Xiao-Ming Ou","doi":"","DOIUrl":"","url":null,"abstract":"Alcohol use disorders are common in the world. However, the development of novel drugs to prevent alcohol-induced brain damage is based upon an improved neurobiological understanding on the cellular changes that take place in the brain. We previously reported that ethanol exposure lowered cell proliferation and increased cell apoptosis in all cell types, but affects brain cell lines the most, while ethanol and the anti-depressant drug deprenyl, an monoamine oxidase B (MAO B) inhibitor, exposure in unison increases cell viability. Here we investigated the molecular mechanism of the neuroprotective effect of deprenyl (0.25 nM) on ethanol (75 mM)-induced harmful effect. Transforming growth factor-beta-inducible early gene 2 (TIEG2) is an activator for MAO B. MAO B levels increase has been shown to contribute to neuronal cell death. This study uses the neuronal cell line to address whether ethanol induced cell death is through the activation of TIEG2-MAO B apoptotic pathway, and whether deprenyl protects cells from the effects of alcohol through the inhibition of this pathway. We have found that ethanol exposure increases the levels of mRNA and protein/catalytic activity for both TIEG2 and MAO B, while ethanol and deprenyl exposure in unison reduce the expression of both TIEG2 and MAO B, however it increases cell viability. Additionally, TIEG2-overexpressed cells display more cellular death-induced by ethanol than control cells. In summary, this study demonstrates the role of TIEG2 in ethanol induced cell death. The inhibition of the TIEG2-MAO B pathway may be one of the mechanisms for the neuroprotective effect of deprenyl.","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"289-295"},"PeriodicalIF":0.0,"publicationDate":"2008-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2782956/pdf/nihms78049.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"28536021","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

Effect of drug-polymer binary mixtures on the in-vitro release of ibuprofen from transdermal drug-in-adhesive layers. 药物-聚合物二元混合物对布洛芬经皮药物-黏附层体外释放的影响。

IF 3.1

Drug discoveries & therapeutics Pub Date : 2008-10-01

K Y Ho, M Ord, K Dodou

{"title":"Effect of drug-polymer binary mixtures on the in-vitro release of ibuprofen from transdermal drug-in-adhesive layers.","authors":"K Y Ho, M Ord, K Dodou","doi":"","DOIUrl":"","url":null,"abstract":"We report on the formation of eutectic mixtures of ibuprofen using two different polymers together with investigations on the in-vitro release of ibuprofen from drug-in-adhesive layers. Ibuprofen, literature melting point (m.p.) = 73.5-76.5°C, was tested together with Pluronic F127, literature m.p. = 54.4-60.5°C, and polyethylene glycol 1000 (PEG 1000), literature m.p. = 37-40.9°C, as second components in binary mixtures, incorporated into an acrylic adhesive, either as solid physical mixtures (PM) or molten mixtures (MM). Studies of how the type of mixture preparation (PM versus MM) and the ratio of components in binary mixtures affecting the in-vitro drug release of ibuprofen, compared with ibuprofen-adhesive layers without polymer addition were conducted. Ibuprofen release did not improve using the eutectic composition with Pluronic F127, possibly due to increased ibuprofen solubilisation in the adhesive and a subsequent decrease in the thermodynamic activity of the formulation. A significant increase in ibuprofen release (P < 0.05) was shown for compositions adjacent to the eutectic one, with ibuprofen: Pluronic F127 (40:60) and ibuprofen: PEG 1000 (20:80, 25:75, 30:70), from both PM- and MM-adhesive formulations, compared to the ibuprofen-adhesive formulations.","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"277-81"},"PeriodicalIF":3.1,"publicationDate":"2008-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30576208","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Pulmonary drug delivery: Implication for new strategy for pharmacotherapy for neurodegenerative disorders. 肺给药:神经退行性疾病药物治疗新策略的意义。

IF 3.1

Drug discoveries & therapeutics Pub Date : 2008-10-01

N Islam, S Rahman

引用次数: 0

Effect of benzyl-N-acetyl-α-galactosaminide on KL-6 mucin expression and invasive properties of a human pancreatic carcinoma cell line. 苄基- n -乙酰-α-半乳糖胺对人胰腺癌细胞株KL-6粘蛋白表达及侵袭特性的影响

IF 3.1

Drug discoveries & therapeutics Pub Date : 2008-10-01

H L Xu, Y Inagaki, F S Wang, N Kokudo, M Nakata, W Tang

引用次数: 0

Regulation of the nitric oxide synthesis pathway and cytokine balance contributes to the healing action of Myristica malabarica against indomethacin-induced gastric ulceration in mice. 一氧化氮合成途径和细胞因子平衡的调节参与了黑豆蔻对消炎痛诱导的小鼠胃溃疡的愈合作用。

IF 3.1

Drug discoveries & therapeutics Pub Date : 2008-10-01

B Maity, D Banerjee, S K Bandyopadhyay, S Chattopadhyay

{"title":"Regulation of the nitric oxide synthesis pathway and cytokine balance contributes to the healing action of Myristica malabarica against indomethacin-induced gastric ulceration in mice.","authors":"B Maity, D Banerjee, S K Bandyopadhyay, S Chattopadhyay","doi":"","DOIUrl":"","url":null,"abstract":"The role of the ariginine-metabolism in the healing action of the methanol extract of Myristica malabarica (rampatri) (RM) and omeprazole (Omez) against indomethacin-induced stomach ulceration in mouse was investigated. Indomethacin (18 mg/kg) was found to induce maximum stomach ulceration in Swiss albino mice on the 3rd day of its administration, which was associated with reduced arginase activity (38.5%, p < 0.05), eNOS expression, along with increased iNOS expression, total NOS activity (5.37 fold, p < 0.001), NO generation (55.1%, p < 0.01), and ratio of pro-/anti-inflammatory cytokines. Besides providing comparable healing as Omez (3 mg/kg × 3 d), RM (40 mg/kg × 3 d, p.o.) shifted the iNOS/NO axis to the arginase/polyamine axis as revealed from the increased arginase activity (59.5%, p < 0.01), eNOS expression, and reduced iNOS expression, total NOS activity (73%, p < 0.001), and NO level (49.8%, p < 0.01). These could be attributed to a favourable anti/pro inflammatory cytokines ratio, generated by RM. The healing by Omez was however, not significantly associated with those parameters.","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"296-304"},"PeriodicalIF":3.1,"publicationDate":"2008-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30576211","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Antioxidant activity of wild plants collected in Beni-Sueif governorate, Upper Egypt. 上埃及Beni-Sueif省野生植物抗氧化活性研究。

IF 3.1

Drug discoveries & therapeutics Pub Date : 2008-10-01

S Abouzid, A Elshahaat, S Ali, M I Choudhary

引用次数: 0