• The Korean Journal of Nuclear Medicine
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• v.36 no.6
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• pp.333-343
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• 2002

Purpose: A new linker, hydrazino nicotinamide (HYNIC), was recently introduced for labelling of liposome with $^{99m}Tc$. In this study we synthesized HYNIC derivatized PEG (polyethylene glycol)-liposomes radiolabeled with $^{99m}Tc$. Materials and Methods: In order to synthesize HYNIC-DSPE (distearoyl phosphatidyl ethanolamine) which is a crucial component for $^{99m}Tc$ chelation, first of all succinimidyl 6-BOC-hydrazinopyridine-3-carboxylic acid was synthesized from 6-chloronicotinic acid by three sequential reactions. A DSPE derivative of succinimidyl 6-BOC-hydrazinopyridine-3-carboxylic acid was transformed into HYNIC-DSPE by HCI/dioxane. HYNIC-PEG-liposomes were prepared by hydration of the dried lipid mixture of EPC (egg phosphatidyl choline): PEG-DSPE : HYNIC-DSPE:cholesterol (1.85:0.15:0.07:1, molar ratio). The HYNIC-PEG-liposomes were labeled with $^{99m}Tc$ in the presence of $SnCl_2{\cdot}2H_2O$ (a reducing agent) and tricine (a coligand). To investigate the level of in vivo transchelation of $^{99m}Tc$ in the liposomes, the $^{99m}Tc$-HYNiC-PES-liposomes were incubated with a molar excess of DTPA, cysteine or glutathione solutions at $37^{\circ}C$ for 1 hour. The radiolabeled liposomes were also incubated in the presence of human serum at $37^{\circ}C$ for 24 hours. Results: 6-BOC-hydrazinopyridine-3-carboxylic acid was synthesized with 77.3% overall yield. The HYNIC concentration in the PEG-coated liposome dispersion was 1.08 mM. In condition of considering the measured liposomal size of 106 nm, the phospholipid concentration of $77.5\;{\mu}mol/m{\ell}$ and the liposomal particle number of $5.2{\times}10^{14}$ liposomes/ml, it is corresponded to approximate 1,250 nicotinyl hydrazine group per liposome in HYNIC-PEG-liposome. The removal of free $^{99m}Tc$ was not necessary because the labeling efficiency were above 99%. The radiolabeled liposomes maintained 98%, 96% and 99%, respectively, of radioactivity after incubation with transchelators. The radiolabeled liposomes possessed above 90% of the radioactivity in serum. Conclusion: These results suggest that the HYNIC can be synthesized easily and applied in labelling of PEG-liposomes with $^{99m}Tc$.

• The Korea Journal of Herbology
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• v.30 no.5
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• pp.15-21
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• 2015

Objectives : Methicillin-resistantStaphylococcus aureus(MRSA) is a human pathogen. New antibacterial agents are needed to treat MRSA-related infections. This study investigated the antibacterial activity of EtOH 70% extracts ofTonghyeonipal-dan(THD) which prescription is composed of oriental medicine against MRSA.Methods : The antibacterial activity of THD was evaluated against MRSA strains by using the Disc diffusion method, broth microdilution method, Checkerboard dilution test, and Time-kill test; its mechanism of action was investigated by bacteriolysis, detergent or ATPase inhibitors were used.Results : The minimum inhibitory concentration (MIC) of THD is 1,000~2,000 μg/mL against MRSA. In the checkerboard dilution test, fractional inhibitory concentration index (FICI) of THD in combination with antibiotics indicated synergy or partial synergism againstS. aureus. Furthermore, a time-kill assay showed that the growth of the tasted bacteria was considerably inhibited after 24 h of treatment with the combination of THD with selected antibiotics. For measurement of cell membrane permeability, THD 500 μg/mL along with concentration of Triton X-100 (TX) and Tris-(hydroxymethyl) aminomethane (TRIS) were used. In the other hand, N,N-dicyclohexylcarbodimide (DCCD) and Sodium azide (NaN3) were used as an inhibitor of ATPase. TX, TRIS, DCCD and NaN3 cooperation againstS. aureusshowed synergistic action.Conclusions : Accordingly, antimicrobial activity of THD was affected by cell membrane and inhibitor of ATPase were assessed. These results suggest that THD has antibacterial activity, and that THD extract offers great potential as a natural antibiotic against MRSA.

• The Korea Journal of Herbology
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• v.22 no.4
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• pp.65-73
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• 2007

Objective : Salvia miltiorrhiza Bunge (Labiatae) (SM), an eminent herbal plant, has been widely used in traditional Chinese medicine for the treatment of vascular diseases such as hypertension. The aim of this study was to determine whether SM inhibits production of nitrite, an index of NO, and proinflammatory cytokines in lipopolysaccharide (LPS)-treated RAW 264.7 macrophages. And this study investigated whether or not SM could reduce tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$)-induced inflammatory response in human vascular aortic smooth muscle cells (HASMC) and umbilical vein endothelial cells (HUVEC). Methods : Cytotoxic activity of SM on RAW 264.7 cells was using 5-(3-caroboxymeth-oxy phenyJ)-2H-tetra-zolium inner salt (MTS) assay. We measured the NO production using Griess Reagent System. Production of Proliflammatory cytokines was measured by Enzyme-Linked Immunosorbent Assay (ELISA). Results : Our results indicated that SM significantly inhibited the LPS-induced NO production accompanied by an attenuation of tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), IL-6 and monocyte chemoattractant protein (MCP)-1 formation in macrophages. SM decreased TNF-${\alpha}$-induced IL-8, IL-6 production, and intracellular adhesion molecule (ICAM)-1 and vascular cell adhesion molecule (VCAM)-1 expression. Conclusion : These results indicate that SM has potential as an anti-inflammatory agent.

• Toxicological Research
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• v.31 no.3
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• pp.241-253
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• 2015

Furan ($C_4H_4O$) is a volatile compound formed mostly during the thermal processing of foods. The toxicity of furan has been well documented previously, and it was classified as "possible human carcinogen (Group 2B)" by the International Agency for Research on Cancer. Various pathways have been reported for the formation of furan, that is, thermal degradation and/or thermal rearrangement of carbohydrates in the presence of amino acids, thermal degradation of certain amino acids, including aspartic acid, threonine, ${\alpha}$-alanine, serine, and cysteine, oxidation of ascorbic acid at higher temperatures, and oxidation of polyunsaturated fatty acids and carotenoids. Owing to the complexity of the formation mechanism, a vast number of studies have been published on monitoring furan in commercial food products and on the potential strategies for reducing furan. Thus, we present a comprehensive review on the current status of commercial food monitoring databases and the possible furan reduction methods. Additionally, we review analytical methods for furan detection and the toxicity of furan.

• Korean Journal of Pharmacognosy
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• v.33 no.4 s.131
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• pp.343-351
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• 2002

Atherosclerosis is a progressive disease characterized by the accumulation of lipids and fibrous elements in the arteries. Monocyter/macrophages are involved in many aspects of the development of atherosclerotic plaques. It is known that the intercellular adhesion molecule-1(ICAM-1) expressed preferentially on endothelial cells of atherosclerotic plaque, promotes local adhesion and transendothelial migration of monocytes, neutrophils, and lymphocytes. Using the human promyelocytic leukemia HL-60 cell line, we investigated the inhibitory effects of methanol extracts of 175 natural plants on ICAM-1/LFA-1 mediated cell adhesion. Eight kinds of methanol extracts of tested plants inhibited PMA-induces homotypic aggregationof HL-60 cells without cytotoxicity at the concentration of $6.25\;{\mu}g/ml$. They were divided two fractions of $CHCI_3$ and $H_2O$ to use solvent partition. Among them, $CHCI_3$ extract $(1.0\;{\mu}g/ml)$ of Saururus chinensis and Chloranthus japonicus singificantly inhibited aggregation of HL-60 cells without cytotoxicity, respectively.

• Asian Pacific Journal of Cancer Prevention
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• v.17 no.7
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• pp.3559-3567
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• 2016

Background: In recent years, there has been considerable research on recycling of agro-industrial waste for production of bioactive compounds. The food processing industry produces large amounts of citrus peels that may be an inexpensive source of useful agents. Objective: The present work aimed to explore the phytochemical content, antioxidant, anticancer, antiproliferation, and antigenotxic activities of lemon, grapefruit, and mandarin peels. Materials and Methods: Peels were extracted using 98% ethanol and the three crude extracts were assessed for their total polyphenol content (TPC), total flavonoid content (TFC), and antioxidant activity using DPPH (1, 1-diphenyl-2-picrylhydrazyl). Their cytotoxic and mitogenic proliferation activities were also studied in human leukemia HL-60 cells and mouse splenocytes by CCK-8 assay. In addition, genotoxic/antigenotoxic activity was explored in mouse splenocytes using chromosomal aberrations (CAs) assay. Results: Lemon peels had the highest of TPC followed by grapefruit and mandarin. In contrast, mandarin peels contained the highest of TFC followed by lemon and grapefruit peels. Among the extracts, lemon peel possessed the strongest antioxidant activity as indicated by the highest DPPH radical scavenging, the lowest effective concentration 50% ($EC_{50}=42.97{\mu}g\;extract/mL$), and the highest Trolox equivalent antioxidant capacity (TEAC=0.157). Mandarin peel exhibited moderate cytotoxic activity ($IC_{50}=77.8{\mu}g/mL$) against HL-60 cells, whereas grapefruit and lemon peels were ineffective anti-leukemia. Further, citrus peels possessed immunostimulation activity via augmentation of proliferation of mouse splenocytes (T-lymphocytes). Citrus extracts exerted non-cytotoxic, and antigenotoxic activities through remarkable reduction of CAs induced by cisplatin in mouse splenocytes for 24 h. Conclusions: The phytochemical constituents of the citrus peels may exert biological activities including anticancer, immunostimulation and antigenotoxic potential.

• Korean Journal of Pharmacognosy
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• v.36 no.4 s.143
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• pp.263-272
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• 2005

To develop safe and new anticoagulation agents from natural resources, the inhibitory activities of 291 methanol extracts, which were prepared from different parts of 197 medicinal and wild plants, against human thrombin were evaluated. Based in anti-coagulation activity determined by thrombin time and activated partial thromboplastin time, the extract of leaf of Myrica rubra was finally selected. The extract of M. rubra showed a strong thrombin inhibitory activity (above 1,819%) at 0.5 mg/ml as a final concentration, whereas aspirin showed 337% inhibition at concentration of 1.5 mg/ml. The activity of the extract remained more than 85% and 60% by heat treatment at $100^{\circ}C$ for 30min, and acid treatment at pH 2 for 60 min, respectively. Our results suggested that the extract of Myrica rubra could be the potential source as thrombin inhibitor.

• Archives of Pharmacal Research
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• v.28 no.8
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• pp.923-929
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• 2005

Methanol extracts of domestic plants of Korea were evaluated as a potential inhibitor of neutral pH optimum and membrane-associated 60 kDa sphingomyelinase (N-SMase) activity. In this study, we partially purified N-SMase from bovine brain membranes using ammonium sulfate. It was purified approximately 163-fold by the sequential use of DE52, Butyl-Toyopearl, DEAE-Cellulose, and Phenyl-5PW column chromatographies. The purified N-SMase activity was assayed in the presence of the plant extracts of three hundreds species. Based on the in vitro assay, three plant extracts significantly inhibited the N-SMase activity in a time- and concentration-dependent manner. To further examine the inhibitory pattern, a Dixon plot was constructed for each of the plant extracts. The extracts of Abies nephrolepis, Acer tegmentosum, and Ginkgo biloba revealed a competitive inhibition with the inhibition constant (Ki) of $11.9 {\mu}g/mL,\;9.4{\mu}g/mL,\;and\;12.9{\mu}g/mL$, respectively. These extracts also inhibited in a dose-dependent manner the production of ceramide induced by serum deprivation in human neuroblastoma cell line SH-SY5Y.

• Korean Journal of Pharmacognosy
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• v.35 no.3 s.138
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• pp.255-258
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• 2004

Chinese cabbage (Brassica campestris ssp pekinensis) is one of the most popular green vegetables in Cruciferae family, which consisted in many Korean food. All kinds of Chinese cabbage are used both fresh and cooked with certain varieties being more suitable than others for some uses. A unique dish, Kimchi, has been developed in Korea and elsewhere by fermenting Chinese cabbage and pickling it in salt solution. Though lots of beneficial effect of Kimchi on human health has been published before, it is still debatable and in vague on the active origin of the Kimchi or of the Chinese cabbage responsible for the corresponding biological activities. We have recently conducted photochemical investigation of the Chinese cabbage, which is the main ingredient of the Korean traditional food, Kimchi. The MeOH extract of Chinese cabbage was partitioned with ethylacetate and BuOH, successively. The ethyl acetate soluble part was subjected to column chromatography with silica gel and RP-18, which gave finally five minor components, i.e., ${\beta}-sitosterol$ (1), indole-3-acetonitrile (2), 4-methoxyindole-3-acetonitrile (3), methyl ferulate (4), glycerol 1-(9,12,15-octadecatrienoate) (5). The structures of them were established on the basis of spectral $(^1H-NMR,\;^{13}C-NMR)$ evidences.

• International Journal of Oral Biology
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• v.36 no.2
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• pp.59-64
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• 2011

Anthocyanins are naturally occuring phytochemicals and the main components of the coloring of plants, flowers and fruits. They are known to elicit antioxidative, anti-inflammatory and cancer preventive activity. In this study, we investigated anthocyanins in black / yellow soybean seedcoats using different methods of detection - thin layer chromatography (TLC), capillary zone electrophoresis (CZE) and HPLC analysis. The anthocyanins in soybean seedcoats were extracted by five independent methods of extraction and the aglycons (anthocyanidins) of the corresponding anthocyanins were prepared by acid mediated hydrolysis. The anthocyanin / anthocyanidin in black soybean seedcoat showed characteristic TLC mobility, CZE electrophoretic retention and HPLC migration time while little of anthocyanins were detected from yellow soybean seedcoat. The extracted anthocyanins showed pH dependent retention time in CZE and spectral change in UV-Vis spectrum. HPLC analysis of the hydrolyzed extract of black soybean seedcoat identified the presence of four anthocyanidins. The major anthocyanin in black soybean seedcoat was cyanin (cyanidin-3-O-glucoside), with the relative order of anthocyanidin in cyanidin > delphinidin > petunidin > pelargonidin.