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신경팹티드, Achatin-1 유사체의 합성과 생리활성
홍남주,최청 영남대학교 자원문제연구소 1994 資源問題硏究 Vol.13 No.-
The structure activity relationships of neuroactive tetrapeptide. achatin-I (Gly-D-Phe-Ala-Asp) analogs were studied by neuro excitatory effect. Seven isomers of achatin-I were synthesi-zed using the solid phase method and bioactivities were tested with giant axon isolated both from American crayfish and cockroach. The sensitivity of the neuron to achatin-I and its isomers was strictly stereospecific : among the various isomers, Gly-D-Phe-Ala-Asp. Gly-D-Phe-Ala-Glu and Ac-Gly-0-Phe-Ala-Asp produced excitatory effects, while G3y-D-Phe-Ala-Asp, Gly-D-Phe-Gly-Asp, and Gly-Ala-D-Phe-Asp showed slight or no excitatory effects.
홍남주,진동훈,Eun Young Hong 대한화학회 2009 Bulletin of the Korean Chemical Society Vol.30 No.3
A series of conjugated cyclic and linear enkephalin analogs, Tyr-c[D-A2bu-Gly-Phe-Asp(NH-X)], where X = methyl, stearyl or PEG350, and Tyr-D-Ala-Gly-Phe-Cys(S-X), where X = methyl, octyl, or farnesyl, were synthesized in solution to investigate the receptor selectivity of opioids based on Schwyzer's membrane compartment concepts.5,6 Cyclizations of the target compounds were achieved in high yields (> 60%) employing BOP, NaHCO3 in DMF despite the steric hindrance of the bulky pendant groups. In the binding assay, the hydrophobic fatty acyl conjugates retained μ-receptor selectivity. The unsaturated farnesyl conjugate exhibited the increased binding affinity than the saturated stearyl conjugate for both μ-and δ-opioid receptors. The PEG conjugates displayed the δ-receptor selectivity. The low molecular weight PEG350 conjugate exhibited the increase selectivity than the high molecular weight PEG5000 conjugate to the δ-receptor. The results of this study support the membrane compartment concepts.
홍남주 대한화학회 2010 Bulletin of the Korean Chemical Society Vol.31 No.4
A series of 13- and 14-membered cyclic enkephalin analogs based on the moderately μ selective prototype compound Tyr-C[D-A2bu-Gly-Phe-Leu] 8a were synthesized to investigate the structure-activity relationship. The modifications of sequence were mainly focused on two positions 3 and 5, critical for the selective recognition for μ and δ opioid receptors. The substitution of hydrophobic Leu5 with hydrophilic Asp5 derivatives led to Tyr-C[D-A2bu-Gly-Phe-Asp(N-Me)] 7 and Tyr-C[D-Glu-Phe-gPhe-rAsp(O-Me)] 5, the peptides with a large affinity losses at both μ and δreceptors. The substitution of Phe3 with Gly3 led to Tyr-C[D-Glu-Gly-gPhe-rLeu] 3 and Tyr-C[D-Glu-Gly-gPhe-DrLeu]4, the peptides with large affinity losses at μ receptors, indicating the critical role of phenyl ring of Phe3 for μreceptor affinities. One atom reduction of the ring size from 14-membered analogs Tyr-C[D-Glu-Phe-gPhe-(L and D)-rLeu] 6a, 6b to 13-membered analogs Tyr-C[D-Asp-Phe-gPhe-(L and D)-rLeu] 1, 2 reduced the affinity at both μ and δ receptors, but increased the potency in the nociceptive assay, indicating the ring constrain is attributed to high nociceptive potency of the analogs. For the influence of D- or L-chirality of Leu5 on the receptor selectivity, regardless of chirality and ring size, all cyclic diastereomers displayed marked μ selectivity with low potencies at the δ receptor. The retroinverso analogs display similar or more active at μ receptor, but less active at δ receptor than the parent analogs.
호박(Cucurbita pepo L.) 종자의 자엽조직을 이용한 체세포배형성
홍남주,박현용 조선대학교 부설생명과학 연구소 1999 생명과학 연구 Vol.7 No.-
호박종자의 자엽절편체를 20μM 2,4-dichlorophenoxy acetic acid (2,4-D)가 첨가된 Murashige와 Skoog(MS) 배지에 치상한 후, 24시간 낮은 광조건(3000Lux)에서 배양하여 callus와 체세포배형성을 유도하였다. 2,4-D가 첨가된 MS배지에서 유도된 캘러스를 동일 배지에 계대배양하는 동안 치밀하게 생장하는 embryogenic callus는 계대배양 횟수의 증가와 함께 더 높은 빈도로 출현하였다. 이러한 callus로부터 somatic embryos의 생성은 3차 계대배양 후, 생장조절제가 첨가되지 않은 MS 배지에 2주 배양 후에 embryo의 형성이 관찰되었으며, 계속되는 배양에서 embryo 형성이 증가되었다. Somatic embryogensis was induced from seed cotyledons of pumpkin (Cucurbita pepo L.). Seed cotyledonary explants were cultured on MS medium supplemented with 20μM 2,4-dichlorophenoxey acetic acid(2,4-D) by incubating at 25 ± 2℃ under 24 hrs photoperiod (3000 Lux) for 4 weeks. The explants were transferred (subcultured) to same medium and to growth regulator-free MS medium for 4 weeks. Three times subculture on the same medium containing 20μM 2,4-D was required for somatic embryogenesis. Somatic embryos was only observed on growth regulator-free MS medium after 2 week cultures in the 4th subculture.
촉매로서 Silver Oxide를 이용한 Serine의 결사슬기 보호
홍남주 嶺南大學校附設 基礎科學硏究所 1988 基礎科學硏究 Vol.8 No.-
In peptide synthesis, especially using the solid phase method, N-tert-butoxy-carbonyl-O-benzyl-L-Serine has been proved to be a useful intermediate to incorporate serine into the synthetic peptide analongues. O-Benzylation of serine using silver oxide as the catalyst was attempt and the result was compared with that of the conventional method using sodium hydride. O-Benzylation was performed with benzyl bromide and benzyl chloride in MeCN and DMF. tert-Butoxycarbonyl group, phthalyl group and copper complex method were used for the protections of serine α-amino group. The best result was obtained with Boc-Ser, benzyl bromide, and acetonitrile. Silver oxide method gave superior result (yield: >20%) over NaH method. The optimum reaction times for O-benzylation procedure of Pht-Ser and Boc-Ser (Fig.1) under the silver oxide catalyst were 18 hrs.
C - 말단이 증가된 Dermorphin 유도체의 합성과 생물학적 활성도
홍남주,정재규,국순웅 ( Nam Joo Hong,Chae Kyu Cheong,Soon Uoong Koock ) 생화학분자생물학회 1988 BMB Reports Vol.21 No.4
Dermorphinoyl (DMR)-arginine, DMR-arginyl-arginine, DMR-arginylarginyl-valine, DMR-arginyl-prolyl-glutamic acid, (Sar⁴) DMR-arginine, (Sar⁴) DMR-arginyl-arginine, (Sar⁴) DMR-arginylarginyl-valine and (Sar⁴) DMR-arginyl-prolyl-glutamic acid have been prepared in order to examine the effect of C-terminal extension of dermorphin (H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH₂) on opioid activity. The dermorphin analogues were synthesized by the solid phase method. Following intravenous administration in mice (hot-plate test), the percent analgesic activities of compounds showed the following trend, morphin$gt; (Sar⁴) DMR-Arg-Arg-Val = DMR-Arg-Arg-Val $gt; (Sar⁴) DMR-Arg-Pro-Glu = DMR-Arg-Pro-Glu $gt; (Sar⁴) DMR-Arg-Arg = DMR-Arg-Arg $gt; (Sar⁴) DMR-Arg = DMR-Arg.
Hydrophobic peptide의 소수성과 구조의 관계에 관한 회귀해석
홍남주 영남대학교 자원문제연구소 1989 資源問題硏究 Vol.8 No.-
To study of structure-activity relationship (SAR) of the artificial endogeneous morphine like peptides, lopophilicity is one of the most important factor determining opioid activity among lipophilicity, electronic property and steric factor due to the drug transport in biological system as well as binding mode of action to receptor site. A variety of mono, dipeptide analogues were synthesized by the solution method. As the physical data to analyze quantitatively SAR of these class of compounds on the basis of hydrophobicity, log P values were determined from the octanol-water system. Then, we exploited that the hydrophobic parameter (πR), steric bulkiness (Es) of amino acid side chain and amide bond parameter (Ipep), these are how to quantitatively affect overall hydrophobicity (log P) of peptide molecule. Regression equation gave the quantitative information about the relationship between structure and *hydrophobicity of Peptide.