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1.
Vasanthakumar Rajappan Ramachandra S. Hosmane 《Bioorganic & medicinal chemistry letters》1998,8(24):756-3652
The synthesis of a novel planar, potentially aromatic, ring-expanded xanthine analogue (1), containing the 5:7-fused imidazo[4,5-e][1,4]diazepine ring system, along with guanase inhibition studies are reported. The compound was synthesized in six steps, starting from 1-benzyl-5-nitroimidazole-4-carboxylic acid (2), and was biochemically screened against rabbit liver guanase. Compound 1 is a moderate competitive inhibitor of the enzyme with a Ki of 2.27 ± 0.66 × 10−4 M. 相似文献
2.
AV Shevchenko IG Budzanivska TP Shevchenko VP Polischuk D Spaar 《Archives Of Phytopathology And Plant Protection》2013,46(2):139-146
The work was focused on the investigation of possible dependencies between the development of viral infection in plants and the presence of high heavy metal concentrations in soil. Field experiments have been conducted in order to study the development of systemic tobacco mosaic virus (TMV) infection in Lycopersicon esculentum L. cv. Miliana plants under effect of separate salts of heavy metals Cu, Zn and Pb deposited in soil. As it is shown, simultaneous effect of viral infection and heavy metals in tenfold maximum permissible concentration leads to decrease of total chlorophyll content in experiment plants mainly due to the degradation of chlorophyll a. The reduction of chlorophyll concentration under the combined influence of both stress factors was more serious comparing to the separate effect of every single factor. Plants' treatment with toxic concentrations of lead and zinc leaded to slight delay in the development of systemic TMV infection together with more than twofold increase of virus content in plants that may be an evidence of synergism between these heavy metal's and virus' effects. Contrary, copper although decreased total chlorophyll content but showed protective properties and significantly reduced amount of virus in plants. 相似文献
3.
Fabrizio Grandi Marcia M Colodel Lidianne N Monteiro João Rafael VP Leão Noeme S Rocha 《BMC veterinary research》2010,6(1):45
Backgroud
Extramedullary hematopoiesis (EMH) is defined as the presence of hematopoietic stem cells such as erythroid and myeloid lineage plus megakaryocytes in extramedullary sites like liver, spleen and lymph nodes and is usually associated with either bone marrow or hematological disorders. Mammary EMH is a rare condition either in human and veterinary medicine and can be associated with benign mixed mammary tumors, similarly to that described in this case. 相似文献4.
Wang G Sakthivel K Rajappan V Bruice TW Tucker K Fagan P Brooks JL Hurd T Leeds JM Cook PD 《Nucleosides, nucleotides & nucleic acids》2004,23(1-2):317-337
IMPDH inhibitors have potential antimicrobial, anticancer and immunomodulatory effects. Nucleoside inhibitors of IMPDH exert their inhibitory effects via nucleoside 5'-MPs. Conversion of nucleoside analogs to NMPs by cellular nucleoside kinases is not assured, and usually is inefficient. In order to bypass cellular phosphorylation, a series of azole nucleoside 5'-MP mimics (P1Ms) based on ribavirin, EICAR and bredinin were synthesized and screened against human and C. albicans IMP dehydrogenises. P1Ms 8, 16, 25, 28 and 29 demonstrated substantial IMPDH inhibition with Ki values in low micromolar range. 相似文献
5.
Deepa Indira Shankara Narayanan Varadarajan Santhik Subhasingh Lupitha Asha Lekshmi Krupa Ann Mathew Aneesh Chandrasekharan Prakash Rajappan Pillai Ishaque Pulikkal Kadamberi Indu Ramachandran Hari Sekar Anurup Kochucherukkan Gopalakrishnan Santhoshkumar TR 《European journal of cell biology》2018,97(1):1-14
The selective autophagic removal of mitochondria called mitophagy is an essential physiological signaling for clearing damaged mitochondria and thus maintains the functional integrity of mitochondria and cells. Defective mitophagy is implicated in several diseases, placing mitophagy as a target for drug development. The identification of key regulators of mitophagy as well as chemical modulators of mitophagy requires sensitive and reliable quantitative approaches. Since mitophagy is a rapidly progressing event and sub-microscopic in nature, live cell image-based detection tools with high spatial and temporal resolution is preferred over end-stage assays. We describe two approaches for measuring mitophagy in mammalian cells using stable cells expressing EGFP-LC3 – Mito-DsRed to mark early phase of mitophagy and Mitochondria-EGFP – LAMP1-RFP stable cells for late events of mitophagy. Both the assays showed good spatial and temporal resolution in wide-field, confocal and super-resolution microscopy with high-throughput adaptable capability. A limited compound screening allowed us to identify a few new mitophagy inducers. Compared to the current mitophagy tools, mito-Keima or mito-QC, the assay described here determines the direct delivery of mitochondrial components to the lysosome in real time mode with accurate quantification if monoclonal cells expressing a homogenous level of both probes are established. Since the assay described here employs real-time imaging approach in a high-throughput mode, the platform can be used both for siRNA screening or compound screening to identify key regulators of mitophagy at decisive stages. 相似文献
6.
Mahendra Seervi Praveen K. Sobhan Krupa Ann Mathew Jeena Joseph Prakash Rajappan Pillai T. R. Santhoshkumar 《Apoptosis : an international journal on programmed cell death》2014,19(1):269-284
Despite the use of new generation target specific drugs or combination treatments, drug-resistance caused by defective apoptosis signaling remains a major challenge in cancer treatment. A common apoptotic defect in drug-resistant tumor is the failure of cancer cells to undergo Bax/Bak-dependent mitochondrial permeabilization due to impaired signaling of Bcl-2 family proteins. Therefore, Bax and Bak-independent caspase-activating compounds appear to be effective in killing such tumor cells. An image-based cellular platform of caspase sensors in Bax and Bak deficient background allowed us to identify several potential Bax/Bak-independent caspase-activating compounds from a limited high-throughput compound screening. FRET-based caspase sensor probe targeted at the nucleus enabled accurate and automated segmentation, yielding a Z-value of 0.72. Some of the positive hits showed promising activity against drug-resistant human cancer cells expressing high levels of Bcl-2 or Bcl-xL. Using this approach, we describe thiolutin, CD437 and TPEN as the most potentially valuable drug candidates for addressing drug-resistance caused by aberrant expression of Bcl-2 family proteins in tumor cells. The screen also enables the quantification of multiparameter apoptotic events along with caspase activation in HTS manner in live mode, allowing characterization of non-classical apoptosis signaling. 相似文献
7.
Vasanthakumar P. Rajappan Ramachandra S. Hosmane 《Nucleosides, nucleotides & nucleic acids》2013,32(4-5):835-836
Abstract In an effort to explore the biochemical mode of guanase inhibition as well as the structure-activity relationships of azepinomycin, five analogues (I-V) of azepinomycin were synthesized and screened against guanase from rabbit liver. Our results suggest that while the 6-hydroxy group of azepinomycin is crucial for activity, its putative transition state mode of inhibition of guanase is questionable. The additional H-bonding sites at position 5, and hydrophobic groups in and around position 3 of azepinomycin appear to be tolerated, and may in fact enhance the potency of inhibition. 相似文献
8.
A synthesis and an antiviral analysis of the linear extended derivative of aristeromycin (2) is described. 相似文献
9.
V Geetha Das Moumita Zarei Mehrdad VP Mayookha Harohally Nanishankar V G Suresh Kumar 《Glycoconjugate journal》2022,39(4):525-542
Glycoconjugate Journal - Glycosaminoglycans (GAGs) are bioactive polysaccharides or glycoconjugates found in the fish waste having significant health impacts. In the present study it has been... 相似文献
10.
The objective of the present study was to develop membrane-moderated transdermal systems of ampicillin sodium and to evaluate
them with respect to various in vitro and in vivo parameters. The membrane-type transdermal systems were prepared using a
drug with various antinucleant polymers— hydroxypropyl methylcellulose (HPMC), methylcellulose (MC), cellulose acetate phthalate,
chitosan, sodium alginate (SA), and sodium carboxymethylcellulose—in an ethanol: pH 4.7 buffer volatile system by the solvent
evaporation technique with HPMC as the rate-controlling membrane for all the systems. The swelling properties of the polymers
were studied, and drug-polymer interaction studies were performed. The patches were subjected to various physicochemical studies,
in vitro release studies, permeation studies, and skin irritation studies. The best patch among the formulations was selected
for further in vivo studies. Compared to the other patches, SA exhibited the highest moisture content at 16%; a 21% moisture
uptake was found with MC. The release and permeation of the drug from the SA patch was found to be the maximum. The in vivo
study of the SA patch exhibited a peak plasma concentration Cmax of 126 μg/mL at Tmax 4 hours. Hence, it can be concluded that hydrophilic ampicillin sodium can be developed as a transdermal delivery system
with SA that is an alternative to intravenous administration and has minimal adverse effects.
Published: January 26, 2007 相似文献