Relationship between dichromate oxidizable and total soil organic carbon and distribution of different pools of organic carbon in Vertisols of Central India

Geo-referenced soil samples (0-15 cm) were collected from the farmers fields of Sehore (n = 120) and Vidisha (n = 156) district representing AESR 10.1 to establish the relationship between oxidizable SOC and total SOC in Vertisols of Central India and also to study the distribution of different pools of SOC as well as their relationship with crop yield. Total SOC was apportioned into different pools by using 5, 10 and 20 ml of concentrated H2SO4 that resulted in 3 acid-aqueous solution ratio of 0.5:1, 1:1 and 2:1. Also crop yields during the following winter season and rainy season from the geo-reference fields were recorded and were transformed to % relative yield. Oxidizable SOC (y) was related to total SOC (x) in the form of y = 0.825x – 0.086 (R2 = 0.958, n = 276), indicating that oxidizable SOC comprised 82.5% of the total SOC. Therefore it was recommended that a correction factor of 1.21 should be used to convert oxidizable SOC values to get the estimate of total SOC. The mean crop productivity was better related to oxidizable SOC (r = 0.5275) as compared to total SOC(r = 0.4886). The threshold and optimum values of oxidizable SOC were 3.2 and 11.2 g C/kg, respectively, whereas the threshold and optimum values for total SOC were 3.87 and 14.1 g C/kg, respectively. Among the different pools, less labile C was highly correlated (r = 0.5871) with the crop productivity, the computed threshold and optimum value for less labile C were 1.53 and 5.2 g C/kg, respectively

BPR1K653, a Novel Aurora Kinase Inhibitor, Exhibits Potent Anti-Proliferative Activity in MDR1 (P-gp170)-Mediated Multidrug-Resistant Cancer Cells

Over-expression of Aurora kinases promotes the tumorigenesis of cells. The aim of this study was to determine the preclinical profile of a novel pan-Aurora kinase inhibitor, BPR1K653, as a candidate for anti-cancer therapy. Since expression of the drug efflux pump, MDR1, reduces the effectiveness of various chemotherapeutic compounds in human cancers, this study also aimed to determine whether the potency of BPR1K653 could be affected by the expression of MDR1 in cancer cells.BPR1K653 specifically inhibited the activity of Aurora-A and Aurora-B kinase at low nano-molar concentrations in vitro. Anti-proliferative activity of BPR1K653 was evaluated in various human cancer cell lines. Results of the clonogenic assay showed that BPR1K653 was potent in targeting a variety of cancer cell lines regardless of the tissue origin, p53 status, or expression of MDR1. At the cellular level, BPR1K653 induced endo-replication and subsequent apoptosis in both MDR1-negative and MDR1-positive cancer cells. Importantly, it showed potent activity against the growth of xenograft tumors of the human cervical carcinoma KB and KB-derived MDR1-positive KB-VIN10 cells in nude mice. Finally, BPR1K653 also exhibited favorable pharmacokinetic properties in rats.BPR1K653 is a novel potent anti-cancer compound, and its potency is not affected by the expression of the multiple drug resistant protein, MDR1, in cancer cells. Therefore, BPR1K653 is a promising anti-cancer compound that has potential for the management of various malignancies, particularly for patients with MDR1-related drug resistance after prolonged chemotherapeutic treatments

Identification of Potent EGFR Inhibitors from TCM Database@Taiwan

Overexpression of epidermal growth factor receptor (EGFR) has been associated with cancer. Targeted inhibition of the EGFR pathway has been shown to limit proliferation of cancerous cells. Hence, we employed Traditional Chinese Medicine Database (TCM Database@Taiwan) (http://tcm.cmu.edu.tw) to identify potential EGFR inhibitor. Multiple Linear Regression (MLR), Support Vector Machine (SVM), Comparative Molecular Field Analysis (CoMFA), and Comparative Molecular Similarities Indices Analysis (CoMSIA) models were generated using a training set of EGFR ligands of known inhibitory activities. The top four TCM candidates based on DockScore were 2-O-caffeoyl tartaric acid, Emitine, Rosmaricine, and 2-O-feruloyl tartaric acid, and all had higher binding affinities than the control Iressa®. The TCM candidates had interactions with Asp855, Lys716, and Lys728, all which are residues of the protein kinase binding site. Validated MLR (r² = 0.7858) and SVM (r² = 0.8754) models predicted good bioactivity for the TCM candidates. In addition, the TCM candidates contoured well to the 3D-Quantitative Structure-Activity Relationship (3D-QSAR) map derived from the CoMFA (q² = 0.721, r² = 0.986) and CoMSIA (q² = 0.662, r² = 0.988) models. The steric field, hydrophobic field, and H-bond of the 3D-QSAR map were well matched by each TCM candidate. Molecular docking indicated that all TCM candidates formed H-bonds within the EGFR protein kinase domain. Based on the different structures, H-bonds were formed at either Asp855 or Lys716/Lys728. The compounds remained stable throughout molecular dynamics (MD) simulation. Based on the results of this study, 2-O-caffeoyl tartaric acid, Emitine, Rosmaricine, and 2-O-feruloyl tartaric acid are suggested to be potential EGFR inhibitors.National Science Council of Taiwan (NSC 99-2221-E-039-013-)Committee on Chinese Medicine and Pharmacy (CCMP100-RD-030)China Medical University (CMU98-TCM)China Medical University (CMU99-TCM)China Medical University (CMU99-S-02)China Medical University (CMU99-ASIA-25)China Medical University (CMU99-ASIA-26)China Medical University (CMU99-ASIA-27)China Medical University (CMU99-ASIA-28)Asia UniversityTaiwan Department of Health. Clinical Trial and Research Center of Excellence (DOH100-TD-B-111-004)Taiwan Department of Health. Cancer Research Center of Excellence (DOH100-TD-C-111-005

Synthesis of 4-(benzamide)- and 4-(phthalimide)-substituted phenoxypropanolamines and their beta1, beta2-adrenergic receptors binding studies

N-[4-(2-Hydroxy-3-isopropylaminopropoxy)phenyl-l-oxo-isoindoline 3 possess a cardioselective beta-adrenergic receptor binding affinity. Herein we attempted to synthesize the unreduced compound N-[4-(2-hydroxy-3-isopropylaminopropoxy)phenyl]phthalimide 4. But, reaction of N-[4-(2,3-epoxypropoxy)phenyl]plithalimide 10 with isopropylamine opened the phthalimide ring to give N-[4-(2-hydroxy-3-isopropylaminopeopoxy)phenyll-2-isopropylcarbamoylbenzainide 12 instead of 4 as expected. While treatment of 10 with tert-buitylamine gives N-[4-(3-tert-butylamino-2-hydroxypropoxy)phenyllphthalimide 15. Further, reaction of 15 with isopropylamine opened the phtlialimide ring to yield N-[4-(3-tertbutylamino-2-hydroxypropoxy)phenyl]-2-isopropylearbainoylbenzamide 16. Also, reaction of N-[4-(2,3-epoxypropoxy)phenyl]-5,6-dimethoxyphthalimide 11 with isopropylamine affords the phthalimide ring opened analogue N-[4-(2-hydroxy3-isopropylaminopropoxy)phenyl]-2-isopropylcarbamoyl-5,6-dimethoxybeiizamide 13. Compounds 12, 13, 15 and 16 have been tested for their in vitro beta(1)- and beta(2)-adrenergic receptor binding affinity using turkey erythrocyte-membrane (01) and lung homogenate of rats (beta(2)). The percentage inhibition of [H-3]DHA binding to both beta(1)-and beta(2)-adrenergic receptors are compared with that of the standard non-selective beta-adrenergic blocking agent propranolol 1 and selective agent atenolol. All the tested compounds exhibit binding affinity to PI-adrenergic receptors at the tested concentration [10(-5) M] and most of them (12, 15, 16) exhibit cardioselectivity (selectivity ratio > 1). The dimethoxy analogue 13 shows selectivity towards beta(2)-adrenergic receptor (selectivity ratio < 1)

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Not AvailableLong period of intensive crop cultivation deplete the available soil silicon (Si). Depletion of available Si in the soil could be one of the possible limiting factors amongst others contributing to declining yields. The lower values for Si in the soil can be justified due to (i) severe and frequent soil erosion and sediment transportation. (ii) Usually plants absorb Si almost equal to the concentration of most of macronutrients. (iii) Due to the desilication process, Si in the soil is continuously lost as the result of leaching process. Subtropical and tropical soils are generally low in available Si and would benefit from Si fertilization. The silicon content in some regions might be limited to sustainable crop production. Hence, improved Si management to increase yield and sustain crop productivity appears to be necessary in temperate as well in tropical countries. In order to address this problem of yield decline or stagnation, it seems necessary to survey the Si status of agriculturally important soils of different parts of the country and develop region-specific integrated nutrient management systems that include the Si element.Not Availabl

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Not AvailableChromium (Cr) is one of the toxic metals adversely affecting organisms including humans in the ecosystems, and it is present in considerable concentration in the tannery industrial effluent. Toxicity expression of Cr is suspected to be influenced considerably by other accompanying ions present in the effluent used for irrigation. In a screen house experiment, interactive effects of chloride and sulfate ions in a Vertisol on uptake of Cr by spinach crop were investigated and treatments imposed were three levels each of Cr (0, 50, 100 mg kg−1 ), chloride (Cl− ) (0, 25, 50 mM kg−1 ), and sulfur (S) (0, 4, 8 mM kg−1 ) in possible combinations. Plant growth parameters and leaf Cr concentrations were recorded to find out the effect of anions on Cr dynamics in the plant. Increasing the concentration of Cl− ions in soil reduced the Cr concentration in both root and shoot. Similarly, increasing the concentration of S from 4 to 8 mM kg−1 also reduced the concentration and uptake of Cr. Application of sulfate ions augmented the plant growth and counters the negative effect of Cl− ions and Cr. Thus, the study revealed that the addition of S fertilizers could minimize the Cr toxicity in high Cr contaminated soilsNot Availabl

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Not AvailableLong-term application of sewage for crop production accumulates significant amount of heavy metals in soil. Some of these metals are carcinogenic and affect the soil, plant, animal and human health adversely. Phytoremediation with mustard is a well known and regularly adopted practice for metal removal from contaminated areas. However, genetic potential of mustard cultivars may have much influence on phytoremediation potential of mustard. For this, four prominent mustard crop varieties (NRC DR 2, NRC HB 101, RH 749 and RH 119) were grown at sewage contributed metal contaminated agriculture fields of Islamnagar and Bheropura villages. Results showed that all the mustard varieties removed significant amount of Cu, Cd, Pb, Cr, Ni, Zn and Mn from soil. Mean data of all three locations showed that maximum removal of Cu (479 mg plant-1), Cd (2.80 mg plant-1), Cr (38.1 mg plant-1), Ni (9.96 mg plant-1), Zn (26.6 mg plant-1) and Mn (538 mg plant-1) was in NRC HB 101 except for Pb uptake which was highest in NRC DR 2 (1.53 mg plant-1). The NRC HB 101 showed higher phytoextraction potential compared to rest of the varieties. These results are very much useful for formulation of phytoremediation management strategies under metal contaminated agriculture areas.Not Availabl