• 제목/요약/키워드: biochemical compound

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초임계유체를 이용한 우르솔산 함유 고체 가용화 제제의 제조 (Preparation of Water-Soluble Solid Forms Containing Ursolic Acid Using Supercritical Fluid)

  • 이상윤;정주희;정인일;최문재;박의훈;유종훈;임교빈
    • KSBB Journal
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    • 제22권5호
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    • pp.328-335
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    • 2007
  • 본 연구에서는 뛰어난 주름개선효능을 가지고 있지만 수용액상에서의 낮은 용해도로 인해 사용에 제약이 있는 UA의 용해도를 향상시키기 위하여 HP-$\beta$-CD와의 포접체를 형성하는 UA함유 제제를 제조하고자 하였으며 특히 초임계유체 공정기술을 포접화합물 제조에 도입하여 초임계 기술의 적용의 가능성을 조사하였다. UA의 용해도를 증가시키기 위한 제조방법으로 HP-$\beta$-CD와의 혼합물을 반죽법, 용매증발법 및 초임계유체공정을 이용하여 제조하고, 각 제조시료들의 용해도 증가 및 특성을 확인한 결과 용매증발법과 초임계 ASES공정에 의해 물에 대한 용해도가 증가된 UA/HP-$\beta$-CD 제제를 얻을 수 있었다. 각 방법에 의해 제조된 UA 함유 제제의 화장품 제형에서의 안정도 실험을 수행하였으며 실험결과 유화제형에서는 모든 제제가 시간 및 온도에 대한 안정성을 보였으나 가용화제형에서는 ASES 제제와 Ursolisome 제제의 경우 시간이 경과하거나 함유 UA농도가 증가함에 따라 화장품 제형의 현탁도가 증가함을 확인할 수 있었다.

항장효법에 의한 옥병풍산가미의 즉각형 알레르기 반응 억제 효과 (Inhibitory Effects of Immediate-Type Allergic Reaction of Okbyungpoongsan-Gami by Anal Therapy)

  • 조정연;문구원;문석재;원진희;유경태;이종덕
    • 동의생리병리학회지
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    • 제16권2호
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    • pp.239-244
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    • 2002
  • Okbyungpoongsan-Gami (OG) has been used for the treatment of excessive sweating with general weakness and allergic rhinitis recently. Anal therapy is another way of taking Oriental medicine. It is an important pathway but not available in common clinical situation. This experiment was performed in order to study the inhibitory effect of immediate-type allergic reaction of OG by anal therapy. In addition, the experiment was practised by 1 H-NMR spectroscopy to examine molecular structure of OG. The results were obtained as follows : OG concentration-dependently inhibited compound 48/80- induced immediate type systemic allergic reaction with concentrations of 0.01-1.0g/kg by anal administration 1 h before injection of compound 48/80. OG also concentration-dependently inhibited compound 48/80- induced ear swelling response with concentrations of 0.01-1g/kg by anal administration 1h before injection of compound 48/80. OG also inhibited the passive cutaneous anaphylaxis activated by anti-dinitrophenyl (DNP) IgE antibody concentration- dependently at concentrations ranging from 0.01 to 1g/kg. When OG was pretreated at concentrations ranging from 0.01 to 1g/ℓ, the histamine release from the rat peritoneal mast cells induced by compound 48/80 was reduced in a concentration-dependent manner. OG (0.1-1g/ℓ) had a significant inhibitory effect on histamine release from IgE-induced activated mast cells. OG is seen to be a biochemical compound certainly by 1 H-NMR spectroscopy According to above results, anal therapy of OG may be beneficial in the treatment of systemic and local immediate-type allergic reactions by inhibition of histamine release from mast cells.

랫드를 이용한 할로겐 화합물의 흡입독성 연구 (Study on Inhalation Toxicity of Halogen Compound Using Rats)

  • 김현영;유일재;임칠홍;정용현;맹승희;이준연;이성배;한정희;이종윤;이용묵
    • 한국산업보건학회지
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    • 제10권2호
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    • pp.109-123
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    • 2000
  • Inhaled halogen compound was examined through micronucleus tests and toxicity tests using SD (Sprague-Dawley) rats with repeated dosages for six hours a day, five days a week, during four weeks. In four-week repeated exposure, no specific sign caused by the $CF_3I$ compound was observed on the clinical symptoms, body weight variation, feed consumption, and urinalysis data in the testing groups with reference to the control group. In hematological and biochemical blood tests of the testing groups, the significant, but in their normal ranges, value dependencies of glucose, aspartate aminotransferase, alanine aminotransferase and etc., on the halogen carbohydride concentration was observed. In histo-pathological tests, no specific lesion or concentration dependent change due to the $CF_3I$ compound dosage was observed in both sexes of the female and male in the tested animals. But, micronucleus tests on marrow cells extracted from the tested animals which were repeatedly exposed in the $CF_3I$ compound during four weeks, the frequencies of micronuclei were significantly increased dose-dependently compared to the control groups.

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Isolation and Identification of Antifungal Compounds from $Bacillus$ $subtilis$ C9 Inhibiting the Growth of Plant Pathogenic Fungi

  • Islam, Md. Rezuanul;Jeong, Yong-Tae;Lee, Yong-Se;Song, Chi-Hyun
    • Mycobiology
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    • 제40권1호
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    • pp.59-65
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    • 2012
  • Antagonistic microorganisms against $Rhizoctonia$ $solani$ were isolated and their antifungal activities were investigated. Two hundred sixteen bacterial isolates were isolated from various soil samples and 19 isolates were found to antagonize the selected plant pathogenic fungi with varying degrees. Among them, isolate C9 was selected as an antagonistic microorganism with potential for use in further studies. Treatment with the selected isolate C9 resulted in significantly reduced incidence of stem-segment colonization by $R.$ $solani$ AG2-2(IV) in Zoysia grass and enhanced growth of grass. Through its biochemical, physiological, and 16S rDNA characteristics, the selected bacterium was identified as $Bacillus$ $subtilis$ subsp. $subtilis$. Mannitol (1%) and soytone (1%) were found to be the best carbon and nitrogen sources, respectively, for use in antibiotic production. An antibiotic compound, designated as DG4, was separated and purified from ethyl acetate extract of the culture broth of isolate C9. On the basis of spectral data, including proton nuclear magneric resonance ($^1H$ NMR), carbon nuclear magneric resonance ($^{13}C$ NMR), and mass analyses, its chemical structure was established as a stereoisomer of acetylbutanediol. Application of the ethyl acetate extract of isolate C9 to several plant pathogens resulted in dose-dependent inhibition. Treatment with the purified compound (an isomer of acetylbuanediol) resulted in significantly inhibited growth of tested pathogens. The cell free culture supernatant of isolate C9 showed a chitinase effect on chitin medium. Results from the present study demonstrated the significant potential of the purified compound from isolate C9 for use as a biocontrol agent as well as a plant growth promoter with the ability to trigger induced systemic resistance of plants.

Curcumin Induces Apoptosis and Inhibits Growth of Human Burkitt's Lymphoma in Xenograft Mouse Model

  • Li, Zai-xin;Ouyang, Ke-qing;Jiang, Xv;Wang, Dong;Hu, Yinghe
    • Molecules and Cells
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    • 제27권3호
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    • pp.283-289
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    • 2009
  • Curcumin, a natural compound extracted from rhizomes of curcuma Curcuma species, has been shown to possess potent anti-inflammatory, anti-tumor and anti-oxidative properties. However, the mechanism of action of the compound remains poorly understood. In this report, we have analyzed the effects of curcumin on the cell proliferation of Burkitt's lymphoma Raji cells. The results demonstrated that curcumin could effectively inhibit the growth of Raji cells in a dose- and time-dependent manner. Further studies indicated that curcumin treatment resulted in apoptosis of cells. Biochemical analysis showed that the expression of Bax, Bid and cytochrome C were up-regulated, while the expression of oncogene c-Myc was down regulated after curcumin treatment. Furthermore, poly (ADP-ribose) polymerase (PARP) cleavage was induced by the compound. Interestingly, the antiapoptotic Bcl-2 expression was not significantly changed in Raji cells after curcumin treatment. These results suggested that the mechanism of action of curcumin was to induce mitochondrial damage and therefore led to Raji cell apoptosis. We further investigated the in vivo effects of curcumin on the growth of xenograft tumors in nude mice. The results showed that curcumin could effectively inhibit tumor growth in the xenograft mouse model. The overall results showed that curcumin could suppress the growth of Burkitt's lymphoma cells in both in vitro and in vivo systems.

Novel Mononuclear Ruthenium(II) Compounds in Cancer Therapy

  • Anchuri, Shyam Sunder;Thota, Sreekanth;Yerra, Rajeshwar;Devarakonda, Krishna Prasad;Dhulipala, Satyavati
    • Asian Pacific Journal of Cancer Prevention
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    • 제13권7호
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    • pp.3293-3298
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    • 2012
  • The present study was conducted to evaluate in vivo anticancer activity of two novel mononuclear ruthenium(II) compounds, namely Ru(1,10-phenanthroline)$_2$(2-nitro phenyl thiosemicarbazone)$Cl_2$(Compound $R_1$) and Ru (1,10-phenanthroline)$_2$(2-hydroxy phenyl thiosemicarbazone)$Cl_2$(Compound $R_2$) against Ehrlich ascites carcinoma (EAC) mice and in vitro cytotoxic activity against IEC-6 (small intestine) cell lines and Artemia salina nauplii using MTT [(3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide)] and BLT [brine shrimp lethality] assays respectively. The tested ruthenium compounds at the doses 2 and 4 mg/kg body weight showed promising biological activity especially in decreasing the tumor volume, viable ascites cell counts and body weights. These compounds prolonged the life span (% ILS), mean survival time (MST) of mice bearing-EAC tumor. The results for in vitro cytotoxicity against IEC-6 cells showed the ruthenium compound $R_2$ to have significant cytotoxic activity with a $IC_{50}$ value of $20.0{\mu}g/mL$ than $R_1$ ($IC_{50}=78.8{\mu}g/mL$) in the MTT assay and the $LC_{50}$ values of $R_1$ and $R_2$ compounds were found to be 38.3 and $43.8{\mu}g/mL$ respectively in the BLT assay. The biochemical and histopathological results revealed that there was no significant hepatotoxicity and nephrotoxicity associated with the ruthenium administration to mice.

복합항생제 SP-102(설박탐.픽페라실린)의 랫드 복강내 투여에 의한 아급성 독성 (Subacute Toxicity of SP-102 (Sulbactam. Piperacilline) in Rats Administered Intraperitoneally)

  • 서경원;박기숙;신동환;김창옥;한형미;박인원;김효정
    • Biomolecules & Therapeutics
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    • 제1권2호
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    • pp.251-261
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    • 1993
  • The subacute toxicity of combined antibiotics, SP-102 (Sulbactam.Piperacilline), was examined in S.D.rats. Four groups of rats were administered intraperitoneally with 0, 512, 1280 and 3200 mg/kg/day of SP-102 for 30 days. Hain clinical sign related to the compound was soft stool. The body weight gain was slightly decreased in male rats treated with 1280, 3200 mg/kg and in female rats treated with 1280 mg/kg of SP-102. Water consumption was significantly increased in rats administered with SP-102. There were no dose-related changes of urinalysis, biochemical examination and hematological findings in all the groups treated with SP-102. Gross necropsy and histopathology revealed no evidence of specific toxicity related to SP-102. Our data indicate that no-observed effect level of SP-102 is below 512 mg/kg in male and female rats. Maximum tolerated dose of SP-102 was estimated to be above 3200 ma/kg in this study.

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Voltammetric Studies of Cu-Adriblastina Complex and its Effect on ssDNA-Adriblastina Interaction at In Situ Mercury Film Electrode

  • D.Abd El Hady;M.Ibrahim Abdel Hamid;M.Mahmoud Sellem;N.Abo E Maali
    • Archives of Pharmacal Research
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    • 제27권11호
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    • pp.1161-1167
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    • 2004
  • Adriblastina, a cancerostatic anthracycline antibiotic, causes considerable oxidative damage to DNA molecules. The interaction of this compound with DNA was investigated using Osteryoung square wave stripping voltammetry (OSWSV) and cyclic voltammetry (CV) at an in situ mercury film electrode. It was found that the equilibrium constant of the bonded oxidized form of the drug was 63 times bigger more important than that of the bonded reduced form. Copper forms 1 metal: 2 drug stoichiometry complex which is highly stable compared to ssDNA-drug interaction and consequently inhibited the drug biochemical damaging effects. Copper complex offered sub-nanogram determination of adriblastina in aqueous and urine media.

A Potential Target of Tanshinone IIA for Acute Promyelocytic Leukemia Revealed by Inverse Docking and Drug Repurposing

  • Chen, Shao-Jun
    • Asian Pacific Journal of Cancer Prevention
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    • 제15권10호
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    • pp.4301-4305
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    • 2014
  • Tanshinone IIA is a pharmacologically active ingredient extracted from Danshen, a Chinese traditional medicine. Its molecular mechanisms are still unclear. The present study utilized computational approaches to uncover the potential targets of this compound. In this research, PharmMapper server was used as the inverse docking tool andnd the results were verified by Autodock vina in PyRx 0.8, and by DRAR-CPI, a server for drug repositioning via the chemical-protein interactome. Results showed that the retinoic acid receptor alpha ($RAR{\alpha}$), a target protein in acute promyelocytic leukemia (APL), was in the top rank, with a pharmacophore model matching well the molecular features of Tanshinone IIA. Moreover, molecular docking and drug repurposing results showed that the complex was also matched in terms of structure and chemical-protein interactions. These results indicated that $RAR{\alpha}$ may be a potential target of Tanshinone IIA for APL. The study can provide useful information for further biological and biochemical research on natural compounds.

Efficiency of Lamarckian Genetic Algorithm in Molecular Docking of Phenylaminopyrimidine (PAP) Derivatives: A Retrospect Study

  • Ratilla, Eva Marie A.;Juan, Amor A. San
    • 한국생물정보학회:학술대회논문집
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    • 한국생물정보시스템생물학회 2004년도 The 3rd Annual Conference for The Korean Society for Bioinformatics Association of Asian Societies for Bioinformatics 2004 Symposium
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    • pp.203-209
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    • 2004
  • Molecular docking using Lamarckian genetic algorithm of AutoDock 3.0 (AD3) was employed to understand in retrospect the selectivity of phenylaminopyrimidine (PAP) derivatives against the kinase domain c-Abl, implicated in chronic myelogenous leukemia (CML). The energetics of protein-ligand complex was scored using AD3 to identify active drug conformations while Ligplot and ligand protein contact (LPC) programs were used to probe schematic molecular recognition of the bound inhibitor to the protein. Results signify correlation between model and crystal structures of STI-571 compound or Imatinib (IM), a PAP derivative and now clinically proven for its efficacy in CML. A prospect active form Abl inhibitor scaffold from matlystatin class of compounds will be published elsewhere.

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