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Nripendra Vikram Singh Shilpa Parashuram Jyotsana Sharma Roopa Sowjanya Potlannagari Dhinesh Babu Karuppannan Ram Krishna Pal Prakash Patil Dhananjay M. Mundewadikar Vipul R. Sangnure P.V. Parvati Sai Arun Naresh V.R. Mutha Bipin Kumar Abhishek Tripathi Sathish Kumar Peddamma Harish Kothandaraman Sailu Yellaboina Dushyant Singh Baghel Umesh K. Reddy 《Saudi Journal of Biological Sciences》2020,27(12):3514-3528
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Rajyalaxmi RS Sowjanya TN Kiranmayi P Mohan MP 《Indian journal of experimental biology》2004,42(11):1117-1122
A cobalt-resistant wall-less mutant of N. crassa (Cor-sl) characterized previously was also found to be 3-fold more resistant to nickel when compared to the parent wall-less mutant (W-sl). The Cor-sl strain accumulates relatively lower amounts of nickel when compared to W-sl. Sub-cellular fractionation showed significant quantities of nickel to be associated with nuclear and mitochondrial fractions in both the wall-less mutants. However significant differences were observed in vacuolar fractions of W-sl and Cor-sl strains. Fractionation of cell-free extracts on Sephadex G-10 column resolved nickel into two peaks, of which the peak II in Cor-sl constituted 70% of nickel, while the same in W-sl was about 30%. A 3-fold increase in histidine content was observed in case of Cor-sl as compared to W-sl strain, suggesting its role in Ni-resistance. 相似文献
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Early prenatal or post natal exposure to environmental insults such as valproic acid (VPA), thalidomide and ethanol could
induce behavioral alterations similar to autistic symptoms. Bacopa monniera, a renowned plant in ayurvedic medicine is useful in several neurological disorders. The purpose of the present study was
to evaluate the effect of B. monniera on VPA induced autism. On 12.5 day of gestation the female pregnant rats were divided into control and VPA treated groups.
They were administered saline/VPA (600 mg/kg, i.p.) respectively and allowed to raise their own litters. Group I—male pups
of saline treated mothers. On postnatal day (PND) 21 VPA induced autistic male pups were divided into two groups (n = 6);
Group II—received saline and Group III—received B. monniera (300 mg/kg/p.o.) from PND 21–35. Behavioral tests (nociception, locomotor activity, exploratory activity, anxiety and social
behavior) were performed in both adolescence (PND 30–40) and adulthood (PND 90–110) period. At the end of behavioral testing
animals were sacrificed, brain was isolated for biochemical estimations (serotonin, glutathione, catalase and nitric oxide)
and histopathological examination. Induction of autism significantly affected normal behavior, increased oxidative stress
and serotonin level, altered histoarchitecture of cerebellum (decreased number of purkinje cells, neuronal degeneration and
chromatolysis) when compared with normal control group. Treatment with B. monniera significantly (p < 0.05) improved behavioral alterations, decreased oxidative stress markers and restored histoarchitecture of cerebellum.
In conclusion, the present study suggests that B. monniera ameliorates the autistic symptoms possibly due to its anti-anxiety, antioxidant and neuro-protective activity. 相似文献
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M Ravinder B Mahendar S Mattapally KV Hamsini TN Reddy C Rohit K Srinivas SK Banerjee VJ Rao 《Bioorganic & medicinal chemistry letters》2012,22(18):6010-6015
Twenty-six 2-pyridone derivatives (8a-8z), which are structurally analogous to amrinone and milrinone two important cardiotonic drugs, are synthesized and characterized. The synthesis of 2-pyridone derivatives involves addition, followed by cyclization between Baylis-Hillman acetates (7a-7k) and enamino esters or nitriles (3a-3e). Thus synthesized pyridones were subjected to PDE3 inhibitory activity, 14 pyridones were found to be hits out of 26 pyridones synthesized and out of 14 hits, there are 5 pyridones found to be lead compounds having excellent PDE3 inhibitory activity. Further we have carried out computational analysis to understand protein/enzyme and 2-pyridone derivative interactions to identify amino acid residues involved in the vicinity of binding and compared with milrinone drug. 相似文献
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Manda Sathish Sabanis Chetan Dushantrao Shalini Nekkanti Ramya Tokala Soujanya Thatikonda Yellaiah Tangella Gunda Srinivas Shirisha Cherukommu Namballa Hari Krishna Nagula Shankaraiah Narayana Nagesh Ahmed Kamal 《Bioorganic & medicinal chemistry》2018,26(17):4916-4929
A series of new C3-trans-cinnamide linked β-carboline conjugates has been synthesized by coupling between various β-carboline amines and substituted cinnamic acids. Evaluation of their anti-proliferative activity against a panel of selected human cancer cell lines such as A549 (lung cancer), MCF-7 (breast cancer), B16 (melanoma), HeLa (cervical cancer) and a normal cell line NIH3T3 (mouse embryonic fibroblast cell line), suggested that the newly designed conjugates are considerably active against all the tested cancer cell lines with IC50 values 13–45?nM. Moreover, the conjugates 8v and 8x were the most active against MCF-7 cells (14.05?nM and 13.84?nM respectively) and also even potent on other cell lines tested. Further, detailed investigations such as cell cycle analysis, apoptosis induction study, topoisomerase I inhibition assay, DNA binding affinity and docking studies revealed that these new conjugates are DNA interactive topoisomerase I inhibitors. 相似文献
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Repeat-induced point mutation (RIP) is a sexual stage-specific mutational process of Neurospora crassa and other fungi that alters duplicated DNA sequences. Previous studies from our laboratory showed that chromosome segment
duplications (Dps) longer than ~300 kbp can dominantly suppress RIP, presumably by titration of the RIP machinery, and that although Dps <200 kbp did not individually suppress RIP, they could do so in homozygous and multiply heterozygous crosses, provided the
sum of the duplicated DNA exceeds ~300 kbp. Here we demonstrate suppression of RIP in a subset of progeny carrying the normally
sub-threshold 154 kbp Dp(R2394) from a cross of T(R2394) to the wild isolated Carrefour Mme. Gras strain (CMG). Thus, the CMG strain contains a factor that together with Dp(R2394) produces a synthetic RIP suppressor phenotype. It is possible that the factor is a cryptic Dp that together with Dp(R2394) can exceed the size threshold for titration of the RIP machinery and thereby causes RIP suppression. 相似文献
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Sharma S Sowjanya A Kumari M Suryaprakash R Cynthia G Suresh J Chakrabarti R 《Life sciences》2006,80(3):235-244
The current goal in the treatment of diabetes is not only to enhance the glycemic control but also to improve the associated cardiovascular risk factors. Among many of the strategies available, a co-ligand of PPARalpha and gamma in a single molecule which combines the insulin sensitizing potential of PPARgamma and the beneficial lipid modulating properties of PPARalpha agonism, has gained attention in the recent past. Here we report the biochemical mechanism by which a dual PPAR alpha/gamma agonist Ragaglitazar (Raga) achieves this goal. The PPARalpha component of Raga appears to contribute to a significant increase in beta oxidation, ApoA1 secretion and inhibition of TG biosynthesis in HepG2 cells. These effects of Raga at 60 microM were similar to that shown by Fenofibrate (Feno) at 250 microM. The PPARgamma component of Raga showed significant G3PDH activity and TG accumulation with a corresponding increase in aP2 expression in 3T3L1 cells. Significantly reduced levels of IL-6 and TNFalpha were observed in the culture supernatants of Raga treated 3T3L1 cells. Raga resulted in significant insulin dependent glucose uptake in 3T3L1 with a corresponding increase in GLUT4 expression. Further, Raga showed a significant cholesterol efflux with a corresponding increase in ABCA1 protein expression in THP-1 macrophages. In conclusion, Raga activates both PPARalpha and gamma regulated pathway in adipocytes as well as in hepatocytes which together contributes for its insulin sensitizing and lipid lowering activity. In addition the dual activation of PPAR alpha/gamma also shows an athero-protective potential by inducing reverse cholesterol efflux and inhibiting the pro-inflammatory cytokines. 相似文献
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Opposing Effects of CREBBP Mutations Govern the Phenotype of Rubinstein-Taybi Syndrome and Adult SHH Medulloblastoma 总被引:1,自引:0,他引:1
Daniel J. Merk Jasmin Ohli Natalie D. Merk Venu Thatikonda Sorana Morrissy Melanie Schoof Susanne N. Schmid Luke Harrison Severin Filser Julia Ahlfeld Serap Erkek Kaamini Raithatha Thomas Andreska Marc Weißhaar Michael Launspach Julia E. Neumann Mehdi Shakarami Dennis Plenker Ulrich Schüller 《Developmental cell》2018,44(6):709-724.e6
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Niggula Praveen Kumar Yogesh Vanjari Sowjanya Thatikonda Venkatesh Pooladanda Pankaj Sharma Balasubramanian Sridhar Chandraiah Godugu Ahmed Kamal Nagula Shankaraiah 《Bioorganic & medicinal chemistry letters》2018,28(22):3564-3573
A facile method for the construction of double bond between 3-ylidene oxindoles and α-azido ketones has been successfully accomplished with a mild base. This method features azido reduction with concomitant double bond formation to provide the new class of bioactive enamino-2-oxindoles. These new compounds were screened for their in vitro cytotoxic potential on selected human cancer cell lines such as colon, lung, breast, and cervical cancer cells. Among them, representative compounds 3a, 3h, 3k, 3p, 3w and 3x showed notable cytotoxicity profile with IC50 values ranging from 1.40?±?0.10 to 28.7?±?0.36?µM. Compound 3k displayed most potent cytotoxicity against lung cancer (NCI-H460) cells with an IC50 value of 1.40?±?0.10?µM. 3k also arrested the G2/M phase of the cell cycle and induced distinctive apoptotic features on lung cancer cells. The apoptosis induction is supported by various cellular assays such as AO/EB, DAPI, and DCFDA staining studies including clonogenic assay. Extent of apoptosis was also analyzed by Annexin binding and JC-1 staining. Moreover, this method is amenable for the generation of a library of new class of stable bioactive enamino-2-oxindoles. 相似文献