• International Journal of Oral Biology
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• v.38 no.4
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• pp.155-160
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• 2013

The major issue in the development of nucleic acid based therapeutics is the inefficient delivery of these agents into cells. We prepared cholesterol conjugated spermine and evaluated its usefulness as a delivery modality for antisense oligonucleotides in HeLa-Luc cells. A 2'-O-methyl antisense oligonucleotide sequence, designed to correct splicing at an aberrant intron inserted into a normal luciferase reporter gene, was used for complex formation with cholesterol conjugated spermine. Effective delivery of this antisense agent into nucleus would results in the expression of a luciferasereporter gene product. The cholesterol-spermine formed stable complexes with the antisense oligonucleotide and showed modest delivery activity. Furthermore, this delivery activity was maintained even in the presence of serum proteins, mimicking in vivo conditions. Cholesterol-spermine thus has potential as a delivery system for antisense oligonucleotides into cells.

• Journal of Plant Biology
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• v.37 no.4
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• pp.397-402
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• 1994

Possible roles of polyamines in the inhibition of cell elongation in Ranunculus petioles were investigated. Exogenously apoplied polyamines greatly inhibited the auxin-induced petiole growth, while treatment of the tissue with $\alpha$-difluoromethylarginine, the inhibitor of putrescine biosynthesis, further enhanced the growth in the presence of IAA. Inhibitory effect of spermine can also be apparent for fusicoccin-induced elongation, but not for growth induced by a low pH. Spermine also suppressed the ethylene-enhanced growth in the presence of auxin. Using computer-based video digitizer system, the inhibitory effects of spermine on petiole growth were kinetically analyzed. Auxin-induced growth was characterized by an initial and transient growth with a highly elevated rate followed by a steady growth with a slightly reduced rate. Spermine treatment was found to shorten the duration of the initial phase of growth, and to reduce the rates of both the initial and steady growth as well. The latent period for auxin induction was not affected by spermine.

• YAKHAK HOEJI
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• v.43 no.4
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• pp.535-540
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• 1999

Glutamate (Glu) receptor-mediated excitoxicity has been implicated in many acute and chronic types of neurological disorders. Exposure of mature rat cortical neurons (15-18 days in culture) to the various concentrations of Glu resulted in a marked neuronal death, whereas immature rat cortical neurons (4∼5 days in culture) were resistant to the Glu-induced toxicity. Glu receptor subtype-specific agonists showed differential extent of toxicity in the immature neurons. The neurons treated with NMDA or kainate (KA) did not exhibit damage. However, quisqualate (QA) treatment induced a considerable cell death (36.1%) in immature enurons. The non-NMDA antagonist DNQX did not reduce this response. Interestingly, the QA-induced toxicity was potentiated by spermine in a concentration-dependent manner. Again, the spermine-enhanced damage was not altered by the polyamine antagonist ifenprodil. Taken together, unlike NMDA or KA, QA can induce neurotoxicity in immature rat cortical neurons and the QA-induced toxicity was potentiated by spermine. The lack of antagonizing effects of DNQX and ifenprodil on QA-induced toxicity and the potentiated toxicity by spermine, respectively, implies that both QA receptor and the polyamine site of NMDA receptor may not mediate the neurotoxicity observed in this study, and that a distinct mechanism(s) may be involved in excitotoxicity in immature neurons.

• Journal of the Korean Chemical Society
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• v.29 no.3
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• pp.304-310
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• 1985

Effect of spermine on the susceptibility of calf thymus nucleohistone to DNase 1, in relation to the structural change of the nucleohistone, and cooperativity of the interaction of the nucleohistone with DNase 1 was investigated. Dansylated nucleohistone, in which the histone moiety had been derivatized by dansylation, was also used to investigate functional roles of the histone moiety on the cooperativity. The data here indicate the possibility that the nucleohistone, in contrast with the DNA, may not undergo monomolecular condensation, whereas intermolecular aggregation and enhancement of the positive cooperativity of the interaction of nucleohistone with DNase 1 may be brought about by spermine. The interaction of the DNS-nucleohistone with DNase 1 showed negative cooperativity. Based on the data here, it can be speculated that the cooperativity of the nucleohistone is influenced by the histone moiety of the nucleohistone.

• Korean Journal of Plant Tissue Culture
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• v.21 no.4
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• pp.207-213
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• 1994

In order to study the effect of cyclohexylamine (CHA) and polyamines during adventitious root formation, the correlation of adventitious root formation with endogenous polyamine content was investigated in inoculated soybean cotyledons at the rooting medium supplemented with CHA, spermidine and spermine. Adventitious root formation was inhibited in medium containing 10$^{-3}$ -10$^{-2}$ M CHA. Adventitious root formation was not formed in treatment with 10$^{-2}$ M CHA plus polyamine. It was inhibited in 2.5 $\times$ 10$^{-3}$ M CHA alone and reverved in 2.5 $\times$ 10$^{-3}$ M CHA plus 10$^{-4}$ M spermine. Putrescine content was lower in 10$^{-2}$ M CHA and 10$^{-2}$ M CHAplus 10$^{-4}$ M spermine treatment than in control after 3 days of incubation. However, it was higher in 2.5 $\times$ 10$^{-3}$ M CHA and 2.5 $\times$ 10$^{-3}$ M CHA plus 10$^{-4}$ M spermine treatment than in control. Spermine content was higher in all CHA treatments than in control, while spermidine content was lower than in control.

• Asian-Australasian Journal of Animal Sciences
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• v.31 no.8
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• pp.1325-1335
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• 2018

Objective: This study investigated whether spermine supplementation could regulate cell cycle, apoptosis, and amino acid transporter-related genes expression in the thymus and spleen of early weaned piglets. Methods: Eighty female piglets were randomly distributed to receive adequate nutrients supplemented with spermine (0.4 mmol/kg body weight/24 h) or to be provided with restricted nourishment supplemented with normal saline for 7 h or 3, 6, or 9 d in pairs. Results: Regardless of administration time, spermine supplementation significantly up-regulated cyclin A2 gene expression but down-regulated p21 and cyclin D3 mRNA levels in the thymus and spleen and reduced cyclin E2 gene expression in the thymus of piglets (p<0.05). Irrespective of the treatment period, the reduced Bax and caspase-3 gene expressions and improved Bcl-2 mRNA level were observed in the thymus and spleen of spermine-administrated piglets (p<0.05). Regardless of supplementation time, spermine intake significantly enhanced the expressions of amino acid transporter-related genes (SLC1A1, SLC1A5, SLC7A1, SLC7A7, and SLC15A1) in both thymus and spleen, as well as SLC7A9 in the spleen of piglets (p<0.05). In addition, extended spermine administration also markedly promoted cell proliferation, depressed apoptosis and modulated amino acid transport (p<0.05), and such effects were the greatest during prolonged spermine supplementation (6 d) compared to the other time periods (p<0.05). Conclusion: Spermine supplementation may regulate cell cycle during the G1/S phase, suppress apoptosis and modulate amino acid transport. A period of 6 d of spermine supplementation is required to produce the optimal effects on nutritional implications.

• The Korean Journal of Physiology and Pharmacology
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• v.24 no.1
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• pp.101-110
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• 2020

Transient receptor potential canonical 4 (TRPC4) channel is a nonselective calcium-permeable cation channels. In intestinal smooth muscle cells, TRPC4 currents contribute more than 80% to muscarinic cationic current (mIcat). With its inward-rectifying current-voltage relationship and high calcium permeability, TRPC4 channels permit calcium influx once the channel is opened by muscarinic receptor stimulation. Polyamines are known to inhibit nonselective cation channels that mediate the generation of mIcat. Moreover, it is reported that TRPC4 channels are blocked by the intracellular spermine through electrostatic interaction with glutamate residues (E728, E729). Here, we investigated the correlation between the magnitude of channel inactivation by spermine and the magnitude of channel conductance. We also found additional spermine binding sites in TRPC4. We evaluated channel activity with electrophysiological recordings and revalidated structural significance based on Cryo-EM structure, which was resolved recently. We found that there is no correlation between magnitude of inhibitory action of spermine and magnitude of maximum current of the channel. In intracellular region, TRPC4 attracts spermine at channel periphery by reducing access resistance, and acidic residues contribute to blocking action of intracellular spermine; channel periphery, E649; cytosolic space, D629, D649, and E687.

• Journal of Plant Biology
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• v.33 no.4
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• pp.217-223
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• 1990

Restriction enzyme inhibiting substance (REIS) extracted from spinach chloroplast and Chlamydomonas seems not to be proteinaceous, because its inhibiting activity was not lost by heat or trypsin treatment. And it seems not to be lipid or polysacchride, because its inhibiting activity was not lost by lipase or $\alpha$-amylase treatment, respectively. In Chlamydomonas, putrescine, spermidine and spermine were present. The amount of putrescine was the smallest and that of spermie was the greatest. But only spermine was contained in REIS and the activity of REIS. It was proportional to the amount of spermine in REIS and it was hindered by Na+ ion. So, the inhibiting activity of REIS seems to be deeply related to spermine contained in REIS. But restriction enzyme inhibiting activity remained to the some extent although salts and spermine were eliminated by dialysis.

• Journal of Microbiology
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• v.35 no.4
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• pp.315-322
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• 1997

The effects of a polyamine, spermine, on the differentiation of Naegleria gruberi amebas into flagellates were tested. Addition of spermine at early stages of differentiation (until 40 min after the initiation of differentiation) completely inhibited the differentiation. To understand the inhibition mechanism, we examined the effect of spermine treatment on the transcription and translation of differentiation-specific genes during differentiation. Addition of spermine at early stages did not inhibit the accumulation of two differentiation-specific mRNAs, ${\alpha}$-tubulin and Class I mRNA, significantly, but rather prevented the rapid degradation of the mRNAs in later overall protein synthesis partially and gradually. However, translation of the ${\alpha}$-tubulin mRNA was completely inhibited. These data suggest that the inhibition of differentiation of N. gruberi by spermine treatment did not result from the inhibition of transcription of differentiation-specific genes but from the specific inhibition of translation of the mRNAs during the differentiation.

• Journal of the Korean Chemical Society
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• v.29 no.5
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• pp.533-538
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• 1985

To investigate the importance of the hydrophobic interaction in the spermine-induced collapse of DNA to a compact structure, the effect of urea on the anomalous absorbance-temperature profile of calf thymus DNA has been investigated. With the increase of the urea concentration, the trough phase of the anomalous absorbance-temperature profile was eliminated eventually. The cooperativity, enthalpy, and the midpoint of the transition to the trough region are more sensitive to urea than those of the Tm-region transition. The present data of the adverse effect of urea, a hydrophobic environmental reagent, on the thermal stabilization of the condensed state of DNA, suggest that hydrophobic interaction may play an important role in the stabilization of the tertiary structure of the collapsed state of DNA.