• Journal of Radiopharmaceuticals and Molecular Probes
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• v.5 no.1
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• pp.26-35
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• 2019

$^{188}Re$ is one of the most readily available generator derived and useful radionuclides for therapy emitting ${\beta}^-$ particles (2.12 MeV, 71.1% and 1.965 MeV, 25.6%) and imageable gammas (155 keV, 15.1%). The $^{188}W/^{188}Re$ generator is an ideal source for the long term (4-6 months) continuous availability of no carrier added (NCA) $^{188}Re$ suitable for the preparation of radiopharmaceuticals for radionuclide therapy. Rhenium-188 has been used for the preparation of therapeutic radiopharmaceuticals for the management of diseases such as bone metastasis, rheumatoid arthritis and primary cancers. Several early phase clinical studies using radiopharmaceuticals based on $^{188}Re$ -labeled phosphonates, antibodies, peptides, lipiodol and particulates have been reported. In this review, we addressed the current development status of $^{188}Re$ radiopharmaceuticals for liver cancer therapy and their applications.

• Korean Journal of Pharmacognosy
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• v.52 no.1
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• pp.41-48
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• 2021

This research was conducted to investigate the antibacterial and anti-inflammatory effects of MeOH Ex. of Salvia miltiorrhiza (MESM) against oral pathogenic bacteria. Minimum inhibitory concentration (MIC), removal effect of biofilm produced by Streptococcus mutans, effect of gene expression of proinflammatory cytokines and effect of production of proinflammatory cytokine of MESM were tested. MESM showed moderated antibacterial activity against oral pathogenic bacteria. About 89±8% of biofilms produced by S. mutans were removed by MESM at a concentration of 1 mg/mL. Gene expression of IL-1β and TNF-α induced by Porphyromonas gingivalis were 8~9 folds reduced by MESM. Gene expression of IL-8 induced by Fusobacterium nucelatum were 12 folds reduced by MESM. Production of IL-1β, TNF-α and IL-8 were significantly suppressed by MESM. Conclusively, MESM showed potent antibacterial and anti-inflammatory effect against oral pathogenic bacteria.

• Biomolecules & Therapeutics
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• v.32 no.5
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• pp.556-567
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• 2024

β-glucan, a polysaccharide found in various sources, exhibits unique physicochemical properties, yet its high polymerization limits clinical applications because of its solubility. Addressing this limitation, we introduce PPTEE-glycan, a highly purified soluble β-1,3/1,6-glucan derived from Aureobasidium pullulans. The refined PPTEE-glycan demonstrated robust immune stimulation in vitro, activated dendritic cells, and enhanced co-stimulatory markers, cytokines, and cross-presentation. Formulated as a PPTEE + microemulsion (ME), it elevated immune responses in vivo, promoting antigen-specific antibodies and CD8+ T cell proliferation. Intratumoral administration of PPTEE + ME in tumor-bearing mice induced notable tumor regression, which was linked to the activation of immunosuppressive cells. This study highlights the potential of high-purity Aureobasidium pullulans-derived β-glucan, particularly PPTEE, as promising immune adjuvants, offering novel avenues for advancing cancer immunotherapy.

• Bulletin of the Korean Chemical Society
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• v.14 no.2
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• pp.266-271
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• 1993

The reaction of $(CO_5$)M=C(OMe)Tol (M=Cr, Mo, W and $Tol=p-C_6H_4Me)$ and $BBr_3$ followed by treatment with tetramethylethylenediamine (TMEDA) yields a mixture of two diastereomers, trans, $cis-Br(CO)_2(tmeda)M{\equiv}$CTol [M=Cr(1a), Mo(2a), W(3a)] and cis, $trans-Br(CO)_2(tmeda)M{\equiv}$CTol [M=Cr(1b), Mo(2b), W(3b)], respectively. These compounds have been isolated as crystalline solids and characterized by spectroscopic (infrared, mass, $^1H$ and $^{13}C-NMR)$ data. The trans, cis-Br(CO)2(tmeda)Cr${\equiv}$CTol (1a), has been examine via a single crystal X-ray diffraction study : $BrCrO_2N_2C_{16}H_{23}$, Mr=407.27, triclinic, $P{\bar{1}},\;a=12.792(2),\;b=13.400(5),\;c= 11.645(4)\;{\AA},\;{\alpha}=101.26(2)^{\circ},\;{\beta}=103.04(2)^{\circ},\;{\gamma}=91.88(2)^{\circ},\;{\nu}=1907(1){\AA}^3,\;Z=2,\;{\rho}(calcd)=1.418\;gcm^{-3},\;{\lambda}(MoK{\alpha})=0.71069\;{\AA},\;{\mu}=26.25 cm^{-1},\;F(000)=831.97,\;T=295K,\;R=0.0977$ for 1332 significant reflections $[F_0>5{\sigma}(F_0)]$. There are two essentially equivalent molecules in the crystallographic asymmetric unit. Each molecule is octahedral with the bromide ligand trans to the alkylidyne carbon, the two cis-carbonyl ligands, and the bidentate TMEDA ligand.

• Animal Bioscience
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• v.36 no.11
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• pp.1700-1708
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• 2023

Objective: The objective of this study was to determine the effects of β-mannanase on metabolizable energy (ME) and apparent total tract digestibility (ATTD) of protein in various feedstuffs including barley, copra meal, corn, corn distillers dried grains with solubles (DDGS), palm kernel meal, sorghum, and soybean meal. Methods: A basal diet was formulated with 94.8% corn and 0.77% amino acids, minerals, and vitamins and test diets replacing corn-basal diets with barley, corn DDGS, sorghum, soybean meal, or wheat (50%, respectively) and copra meal or palm kernel meal (30%, respectively). The basal diet and test diets were evaluated by using triplicated or quadruplicated 2×2 Latin square designs consisting of 2 diets and 2 periods with a total of 54 barrows at 20.6±0.6 kg (9 wk of age). Dietary treatments were levels of β-mannanase supplementation (0 or 800 U/kg of feed). Fecal and urine samples were collected for 4 d following a 4-d adaptation period. The ME and ATTD of crude protein (CP) in feedstuffs were calculated by a difference procedure. Data were analyzed using Proc general linear model of SAS. Results: Supplementation of β-mannanase improved (p<0.05) ME of barley (10.4%), palm kernel meal (12.4%), sorghum (6.0%), and soybean meal (2.9%) fed to growing pigs. Supplementation of β-mannanase increased (p<0.05) ATTD of CP in palm kernel meal (8.8%) and tended to increase (p = 0.061) ATTD of CP in copra meal (18.0%) fed to growing pigs. Conclusion: This study indicates that various factors such as the structure and the amount of β-mannans, water binding capacity, and the level of resistant starch vary among feedstuffs and the efficacy of supplemental β-mannanase may be influenced by these factors.

• The Korean Journal of Mycology
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• v.39 no.1
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• pp.57-67
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• 2011

Agaricus brasiliensis, one of edible mushroom belonging to Basidiomycota, has been used for curing gastric ulcer and stomach cancer of human beings and also known to have good inhibitory effects on sarcoma 180 and Ehrlich carcinoma of mice. Neutral saline soluble (0.9% NaCl), hot water soluble and methanol soluble substances (hereinafter referred to Fr. NaCl, Fr. HW and Fr. MeOH, respectively) were prepared from fruiting body of the mushroom. ${\beta}$-glucan and total protein contents were identify from fractions of edible mushrooms extract. The ${\beta}$-glucan and protein contents of all fractions of the mushrooms ranged from 21.54~32.31% and 0.16~9.34%, respectively. In vitro cytotoxicity tests, crude polysaccharides were not cytotoxic against cancer cell lines such as Sarcoma 180, HT-29, NIH3T3 and RAW 264.7 at the concentration of 10~2000 ${\mu}g/ml$. Intraperitoneal injection with crude polysaccharides exhibited life prolongation effect of 18.8~50.6% in mice previously inoculated with Sarcoma 180. Fr. HW increased the numbers of spleen cell by 1.2 fold at the concentration of 200 ${\mu}g/ml$ compared with control. Fr. MeOH and Na improved the immuno-potentiating activity of B lymphocyte by increasing the alkaline phosphatase activity by 1.6 fold compared with control at the concentration of 50~500 ${\mu}g/ml$. Fr. Na generated 15.9 ${\mu}M$ of nitric oxide (NO) when cultured with RAW 264.7 at the concentration of 200 ${\mu}g/ml$, while lipopolysaccharide, a positive control, produced 3.7 ${\mu}M$. The Fr. NaCl, Fr. HW and Fr. MeOH increased the secretion of TNF-${\alpha}$, IL-$1{\beta}$, Il-2 and IL-6 by 2.2 times compared with the control group. Fr. Na increased the numbers of peritoneal exudate cells by 4 folds at the concentration of 50mg/kg compared with control. Circulating leukocytes increased by 2.7 folds when Fr. HW from A. brasiliensis was inoculated at the concentration of 50 mg/kg body weight. The hematological and blood chemical analysis of the 3 fractions did not show any difference in blood compositions and enzyme activities compared with the control group (p<0.05). Therefore, the experimental results suggested that crude polysaccharides extracted from A. brasiliensis contain antitumor and immuno-potentiating activities against Sarcoma 180 in ICR mice.

• The Korean Journal of Pharmacology
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• v.23 no.2
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• pp.57-75
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• 1987

Two modalities of gonadotropin secretion, pulsatile gonadotropin and preovulatory gonadotropin surge, have been identified in the mammals. Pulsatile gonadotropin secretion is modulated by the pulsatile pattern of GnRH release and complex ovarian steroid feedback actions. The neural mechansim that regulates the pulsatile release of GnRH in the hypothalamus is called "GnRH pulse generator". Ovarian steroids, estradiol and progesterone, appear to exert thier feedback effects both directly on the pituitary to modulate gonadotropin release and on a hypothalamic site to modulate GnRH release; estradiol primarily affects the amplitude while progesterone decreases the frequency of the pulsatile GnRH. Steroid hormones are known to affect catecholamine transmission in brain. MBH-POA is richly innervated by NE systems and close apposition of NE terminals and GnRH cell bodies occurs in the MBH as well as in the POA. NE normally facilitates pulsatile LH release by acting through ${\alpha}-receptor$ mechanism. However, precise nature of facilitative role of NE transmission in maintaining pulsatile LH has not been clearly understood. Close apposition of DA and GnRH terminals in ME might permit DA to influence GnRH release. Action of DA transmission probably is mediated by axo-axonic contacts between GnRH and DA fibers in the ME. Dopamine transmission does not normally regulate pulsatile LH release, but under certain conditions, increased DA transmission inhibit LH pulse. Endogenous opioid acts to suppress the secretion of GnRH into hypophysial portal circulation, thereby inhibiting gonadotropin secretion. However, an interaction between endogenenous opioid peptides and gonadotropin release is a complex one which involves ovarian hormones as well. LH secretion appears to be most suppressed by endogenenous opioids during the luteal phase, at a time of elevated progesterone secretion. The arcuate nucleus contains not only cell bodies for GnRH and ${\beta}-endorphin$ but also a dense aborization of fibers suggesting that GnRH release is changed by the interactions between GnRH and ${\beta}-endorphin$ cell bodies within the arcuate nucleus. The frequency and amplitude of pulsatile LH release seem to be increased during the preovulatory gonadotropin surge. Estradiol exerts positive feedback action on the hypothalamo-pituitary axis to trigger preovulatory LH surge. GnRH is also crucial hormonal stimulus for preovulatory LH surge. It is unlikely, however, that increased secretion of GnRH during the preovulatory gonadotropin surge represents an obligatory neural signal for generation of the LH discharge in primates including human. Modulation of preovulatory LH surge by catecholamines has been studied almost exclusively in rats. NE and E may be involved in distinct way to accumulate GnRH in the MBH and its release into the hypophysial portal system during the critical period for LH surge on proestrus in rats. However, the mechanisms whereby augmented adrenergic transmission may facilitate the formation and accumulation of GnRH in the ME-ARC nerve terminals before the LH surge have not been clearly understood.

• Bulletin of the Korean Chemical Society
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• v.14 no.4
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• pp.439-444
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• 1993

The aerobic oxidation of the Fe(II) complex of 1,4,8,11-tetraazacyclotetradecane, [Fe(cyclam)$(CH_3CN)_2](ClO_4)_2$, in MeCN in the presence of a few drops of $HClO_4$ leads to low spin Fe(III) species [Fe(cyclam)$(CH_3CN)_2](ClO_4)_3$. The Fe(III) cyclam complex is further oxidized in the air in the presence of a trace of water to produce the deep green binuclear bismacrocyclic Fe(II) complex $[Fe_2(C_{20}H_{36}N_8)(CH_3CN)_4](ClO_4)_4{\cdot}2CH_3CN$. The Fe(II) ions of the complex are six-coordinated and the bismacrocyclic ligand is extensively unsaturated. $[Fe_2(C_{20}H_{36}N_8)(CH_3CN)_4](ClO_4)_4{\cdot}2CH_3CN$ crystallizes in the monoclinic space group $P2_1/n$ with a= 13.099 (1) ${\AA}$, b= 10.930 (1) ${\AA}$, c= 17.859 (1) ${\AA}$, ${\beta}$= 95.315 $(7)^{\circ}$, and Z= 2. The structure was solved by heavy atom methods and refined anisotropically to R values of R= 0.0633 and $R_w$= 0.0702 for 1819 observed reflections with F > $4{\sigma}$ (F) measured with Mo K${\alpha}$ radiation on a CAD-4 diffractometer. The two macrocyclic units are coupled through the bridgehead carbons of ${\beta}$-diimitie moieties by a double bond. The double bonds in each macrocycle unit are localized. The average bond distances of $Fe(II)-N_{imine}$, $Fe(II)-N_{amine}$, and $Fe(II)-N_{MeCN}$ are 1.890 (5), 2.001 (5), and 1.925 (6) ${\AA}$, respectively. The complex is diamagnetic, containing two low spin Fe(II) ions in the molecule. The complex shows extremely intense charge transfer band in the near infrared at 868 nm with ${\varepsilon}$= 25,000 $M^{-1}cm^{-1}$. The complex shows a one-electron oxidation wave at +0.83 volts and two one-electron reduction waves at -0.43 and-0.72 volts vs. Ag/AgCl reference electrode. The complex reacts with carbon monoxide in $MeNO_2$ to form carbonyl adducts, whose $v_{CO}$ value (2010 $cm^{-1}$) indicates the ${\pi}$-accepting property of the present bismacrocyclic ligand.

• Physical Therapy Korea
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• v.15 no.4
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• pp.70-79
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• 2008

The purpose of this study was to find out the effects of electroencephalograph (EEG) power and coherence on cognitive function in normal elderly, non-demented elderly with mild cognitive impairment, and demented elderly during working cognition tasks. Forty elderly women (19 demented elderly, 10 non-demented elderly with mild cognitive impairment, 11 norma1 elderly) participated in this study, All subjects performed working cognition tasks with Raven's CPM while EEG signal was recorded, EEGs were measured continuously at rest and during the working cognition task. EEG power and coherence was computed over 21 channels: right and left frontal, central, parietal, temporal and occipital region. We found that there were more correct answers among normal elderly women than in other groups Owing the working cognition task, ${\Theta}$ wave at Fp1, Fp2 and F8, a wave at Fp2, ${\beta}$ wave at Fp1, Fp2. F4 and F8 of the frontal region was increased significantly in the demented elderly group. On the other hand. ${\Theta}$ wave at Fp1, Fp2 and F7, ${\beta}$ wave at Fp1, Fp2, F3 and F7 of the frontal region was increased significantly in the group of non-demented elderly with mild cognitive impairment. In contrast. in the normal elderly group, all of the ${\Theta}$ wave and ${\beta}$ wave at Fp1, Fp2, F3, F4, F7 and F8 of the frontal region (except ${\beta}$ wave at F3) was increased significantly, These results suggest that the nerves in prefrontal and right hemisphere regions were most active in the demented elderly group during problem solving, and the nerves in the prefrontal and left hemisphere lobe were most active in the group of non-demented elderly with mild cognitive impairment. In contrast, me majority of nerves in the frontal region were active in the normal elderly group.

• Journal of Applied Biological Chemistry
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• v.50 no.4
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• pp.275-280
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• 2007

Dried unripe fruits of Rubus coreanus Miq. were extracted with 80% aqueous MeOH and the concentrated extract was partitioned with EtOAc and $H_2O$. From the EtOAc fraction, four triterpenoids were isolated through repeated silica gel, ODS and Sephadex LH-20 column chromatographies. From the result of physico-chemical data including NMR, MS aud IR, the chemical structures of the compounds were determined as tormentic acid (1), myrianthic acid (2), hovenic acid (3) and 2${\alpha}$,3${\beta}$,19${\beta}$,23-tetrahydroxylolean-12-en-28-oic acid (4). Compounds 3 and 4 were isolated for the first time from this plant. All isolated compounds were evaluated for cytotoxic activity against human colon carcinoma cells using in vitro three-[4,5-dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay, compound 3 showed a higher cytotoxicity ($IC_{50}$ = 7.8 ${\mu}M$) than doxorubicin ($IC_{50}$= 50 ${\mu}M$).