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排序方式: 共有189条查询结果,搜索用时 15 毫秒
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Sheunopa C. Mzezewa Sylvester I. Omoruyi Luke S. Zondagh Sarel F. Malan Okobi E. Ekpo Jacques Joubert 《Journal of enzyme inhibition and medicinal chemistry》2021,36(1):1607
Multitarget directed ligands (MTDLs) are emerging as promising treatment options for Alzheimer’s disease (AD). Coumarin derivatives serve as a good starting point for designing MTDLs due to their inherent inhibition of monoamine oxidase (MAO) and cholinesterase enzymes, which are complicit in AD’s complex pathophysiology. A preliminary series of 3,7-substituted coumarin derivatives were synthesised and evaluated for enzyme inhibitory activity, cytotoxicity as well as neuroprotective ability. The results indicated that the compounds are weak cholinesterase inhibitors with five compounds demonstrating relatively potent inhibition and selectivity towards MAO-B with IC50 values between 0.014 and 0.498 hx00B5;µM. Significant neuroprotective effects towards MPP+-compromised SH-SY5Y neuroblastoma cells were also observed, with no inherent cytotoxicity at 10 µM for all compounds. The overall results demonstrated that substitution of the phenylethyloxy moiety at the 7-position imparted superior general activity to the derivatives, with the propargylamine substitution at the 3-position, in particular, displaying the best MAO-B selectivity and neuroprotection. 相似文献
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Bryce, J. H. and ap Rees, T. 1985. Comparison of the respiratorymetabolism of Plantago lanceolata L. and Plantago major L.J.exp. Bot. 36 15591565. The aim of this work was to discover if the respiratory metabolismof the roots of Plantago lanceolata L. differed from that ofthe roots of Plantago major L. Measurements of oxygen uptakeand dry weight of excised root systems during growth of seedlingsprovided evidence that the two species differed in the amountof respiration needed to support a given increase in dry weight.Excised root systems were given a 6-h pulse in [U-14C]sucrosefollowed by a 16.5-h chase in sucrose. The detailed distributionof 14C amongst the major components of the roots at the endof the pulse and the chase revealed no significant differencebetween the two species. Patterns of 14CO2 production from [1-14C],[2-14C], [3,4-14C], and [6-14C]glucose of excised root systemsfrom plants of three ages were similar for the two species.It is suggested that there is no conclusive evidence for anysignificant inherent difference in the respiratory metabolismof the roots of the two species. Key words: 14C sugar metabolism, respiration, roots, Plantago 相似文献
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M C Kruger J Booyens N T Malan 《Prostaglandins, leukotrienes, and essential fatty acids》1988,33(1):41-47
Discontinuous sucrose gradients were used to determine the degree of association between arachidonic acid and sarcoplasmic reticulum vesicle membranes. Fraction analyses showed that arachidonic acid migrated to a different region of the sucrose gradient in the presence of sarcoplasmic reticulum membranes. This could suggest that arachidonic acid was complexed into the membranes. Arrhenius curves representing the temperature dependency of Ca2+-Mg2+-ATPase activity and calcium uptake in the presence and absence of arachidonic acid were constructed. The activation energy for ATPase did not change significantly due to the presence of arachidonic acid. The curve representing control calcium uptake did not show a discontinuity. However, the curve representing calcium uptake in the presence of arachidonic acid showed discontinuities at 18 degrees C and 21 degrees C. Activation energy increased sharply between these temperatures. The results suggest that arachidonic acid reached the critical micellar concentration between these temperatures. Enthalpy decreased in the presence of arachidonic acid. This observation could suggest a transition of the protein-phospholipid complex to a less rigid state since decreased order in the membrane would decrease the energy barrier for activation of ATPase. 相似文献
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Opute M. Yvette Sarel F. Malan Dale Taylor Erika Kapp Jacques Joubert 《Bioorganic & medicinal chemistry letters》2018,28(8):1287-1291
Previously we have shown that pentacycloundecylamine-chloroquinoline (PCU-CQ) conjugates possess significant chemosensitizing abilities and can circumvent the resistance associated with chloroquine (CQ) resistant plasmodia. In order to further explore structurally related polycyclic compounds as reversed CQ agents we synthesized a series of eight aza-adamantanol (1–4) and adamantane-imine (5–8) CQ conjugates. All conjugates showed limited cytotoxicity against CHO cells (IC50?>?37?µM). Compounds 1, 2 and 5 were highly active (K1 IC50?<?100?nM) exhibiting a 3–4-fold increase in antiplasmodial activity against CQ resistant strain K1 compared to CQ. Reduced cross-resistance (resistance index, RI: 2–4.3) relative to CQ (RI?=?38) was also observed for these compounds. Compound 1 which showed an 18-fold enhancement at retaining its activity against the K1 strain compared to CQ is a promising candidate to substitute CQ in P. falciparum resistant malaria. 相似文献
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Rapid recycling of triose phosphates in oak stem tissue 总被引:10,自引:3,他引:7
S. A. HILL J. S. WATERHOUSE E. M. FIELD V. R. SWITSUR T. AP REES 《Plant, cell & environment》1995,18(8):931-936
We report the carbon-13 and oxygen-18 isotope ratios in cellulose from the early and late wood of pedunculate oak (Quercus robur L.). The δ13 C value of the early wood correlates best with that of the late wood of the previous year. The δ18O value of the early wood correlates best with that of the late wood of the same year. We suggest that a biochemical explanation of these data is that there is a rapid cycle between hexose monophosphates and triose phosphates in oak stem tissue during cellulose synthesis. Evidence in support of this explanation is provided by the intramolecular distribution of 14C in labelled fructose extracted from cores of wood that had been supplied with [1?14C]- and [6-14C]glucose. 相似文献
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CM Ward AP Wilkinson S Bramham HA Lee HW-S Chan GW Butcher A Hutchings MRA Morgan 《Mycotoxin Research》1990,6(2):73-83
From a single aflatoxin B1 oxime — bovine serum albumin conjugate, polyclonal and monoclonal antibody preparations were produced. The four rabbit polyclonal antisera were specific for aflatoxin Bi in a microtitration plate enzyme — linked immunosorbent assay. The monoclonal antibodies showed a wide range of differing specificities, recognizing, for example, aflatoxins B1, B2, G1 and G2; B1 and B2; B1 and G1; and G1 alone. No antibody preparations reacted with aflatoxin M1. The significance of these results to the strategy of anti-aflatoxin antibody production for use in quantitative enzyme immunoassays is discussed. 相似文献
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