• Biomolecules & Therapeutics
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• 제7권1호
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• pp.1-6
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• 1999

Effects of Panax ginseng on the morphine toxicity were studied in relation to its effects on the opioid receptor-G protein interactions. Morphine treatments (3 days) reduced the body weight increment rate and the weight of the thymus and spleen. These changes were usually recovered by the concomitant administration of ginseng total saponin (GTS) but occasionally further deteriorated. This discrepancy was studied in relation to the opioid receptor coupling to G protein, that is, the effects of morphine and GTS on the opioid receptors were studied using the antagonist-agonist competitive binding studies. When GTS recovered the morphine toxicity, morphine shifted the striatal $\delta$ receptors to slightly higher affinity state, and this was partly recovered by the GTS treatment. However, morphine did not have any effect on the affinity state of $\delta$ receptor from NG108-15 cells, suggesting that additional factors were needed for the modulation of the affinity states of $\delta$ receptor. Effects of morphine and GTS on $\mu$ receptor were complicate and variable, and we could not reach a clear conclusion. The morphine toxicity might accompany complicate biological involvements, and the modulation of the affinity states of the opioid receptors might explain a part of the effects of GTS on the morphine toxicity.

• Bulletin of the Korean Chemical Society
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• 제18권9호
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• pp.939-945
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• 1997

Several types of 4-substituted-quinoline-2-carboxylic acid derivatives possessing different substituents at C4-position such as sulfonyl, phosphonyl, carbonyl groups, or a flexible alkyl chain have been synthesized and evaluated for their in vitro antagonistic activity at the glycine site on the N-methyl-D-aspartate (NMDA) receptor. Of them, 5,7-dichloro-4-(tolylsulfonylamino)-quinoline-2-carboxylic acid 9 was found to have the best in vitro binding affinity with IC50 of 0.57 μM. On the other hand, in compounds 21 and 22 the introduction of flexible alkyl chains on C4 of the quinoline mother nuclei caused a significant decrease of the in vitro binding affinity. In addition, replacement of polar carboxylic acid group on C2 by neutral bioisosteres in compounds 23a-d also seems to be disadvantageous to in vitro activity. In the structure-activity relationship (SAR) study of the 4-substituted quinoline-2-carboxylic acid acid derivatives, it was realized that the substitution pattern on C4 significantly influences on the binding affinity for the glycine site of NMDA receptor and the binding affinity might be increased by the introduction of a suitable electron rich substituent at C4 which has the ability of H-bonding donor.

• Archives of Pharmacal Research
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• 제20권6호
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• pp.579-585
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• 1997

To gain further insight into the mechanism of action of antiestrogens, we examined the interaction of antiestrogen with the estrogen receptor system and with estrogen- noncompetable antiestrogen binding sites. In addition to binding directly to the estrogen receptor, antiestrogens can be found associated with binding sites that are distinct from the estrogen receptor. In contrast to the restriction of estrogen receptors to estrogen target cells, such as those of uterus and mammary glands, antiestrogen binding sites are present in equal amounts in estrogen receptor-positive and -negative human breast cancer cell lines, such as MCF-7, T47D, and MDA-MB-231 that differ markedly in their sensitivity to antiestrogens. In order to gain greater insight into the role of these antiestrogen binding sites in the action of antiestrogens, we have examined the biopotency of different antiestrogens for the antiestrogen binding sites and that is CI628 > tamoxifen > trans-hydroxy tamoxifen > CI628M > H1285 > LY117018. This order of affinities does not parallel the affinity of these compounds for the estrogen receptor nor the potency of these compounds as antiestrogens. Indeed, compounds with high affinity for the estrogen receptor and greatest antiestrogenic potency have low affinities for these antiestrogen binding sites. Antiestrogenic potency correlates best with estrogen receptor affinity and not with affinity for antiestrogen binding sites. In summary, our findings suggested that interaction with the estrogen receptor is most likely the mechanism through which antiestrogens evoke their growth inhibitory effects.

• 문화기술의 융합
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• 제4권4호
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• pp.1-10
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• 2018

현재 화장품 시장은 새로운 변화를 모색하고 있다. 이에 소비자의 호감도에 대한 중요성은 부각되고 있는 실정이다. 그에 따른 대안에 대해서는 많은 관련 기업과 시장에서 노력하고 있을 것이다. 따라서 본 연구에서는 외부 캐릭터를 이용한 콜라보레이션 화장품의 캐릭터 특성에 대해 알아보고, 소비자의 호감도에 미치는 영향을 실증적으로 살펴보았다. 콜라보레이션 제품을 1회 이상 구매자를 대상으로 설문조사를 실시하였고 구조방정식을 통해 자료를 분석하였다. 분석결과 본 연구는 친숙성과 창의성이 소비자의 호감도에 통계적으로 유의한 영향을 미치고 있음을 확인할 수 있었다.

• 미생물학회지
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• 제49권2호
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• pp.211-214
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• 2013

비스페놀 A (BPA)는 내분비계 장애물질의 하나로서 인간에게 큰 위협이 되고 있는 물질이다. 따라서 BPA의 분석 및 제거를 위해 BPA에 대해 선택적 친화성을 보이는 특정 리간드 탐색이 요구되고 있다. 본 연구에서는 초음파 처리를 동반한 바이오패닝 기법을 이용하여 파지 표면 디스플레이 라이브러리로부터 BPA에 친화성이 높은 펩타이드 서열을 탐색하였다. BPA 입자에 대한 6라운드의 positive 스크리닝과 에펜도르프 튜브 표면 재질에 대한 negative 스크리닝 과정을 실시하였고, 이를 통해 BPA에 선택적 친화성이 높은 CysLysSerLeuGluAsnSerTyrCys (CKSLENSYC) 서열을 스크리닝하였다. 또한 확보된 서열의 선택적 친화성을 검증하기 위해 BPA와 구조가 유사한 비스페놀 F (BPF), 비스페놀 S (BPS)에 대해서 교차 친화성이 있는지 평가하였고, 앞에서 선택된 서열이 BPS, BPF에 비하여 상대적으로 BPA에 대한 친화성이 높다는 것을 확인하였다.

• Asian-Australasian Journal of Animal Sciences
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• 제28권10호
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• pp.1442-1448
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• 2015

The objectives of this study were to determine the molecular weight of condensed tannins (CT) extracted from mangosteen (Garcinia mangostana L) peel, its protein binding affinity and effects on fermentation parameters including total gas, methane ($CH_4$) and volatile fatty acids (VFA) production. The average molecular weight ($M_w$) of the purified CT was 2,081 Da with a protein binding affinity of 0.69 (the amount needed to bind half the maximum bovine serum albumin). In vitro gas production declined by 0.409, 0.121, and 0.311, respectively, while CH4 production decreased by 0.211, 0.353, and 0.549, respectively, with addition of 10, 20, and 30 mg CT/500 mg dry matter (DM) compared to the control (p<0.05). The effects of CT from mangosteen-peel on in vitro DM degradability (IVDMD) and in vitro N degradability was negative and linear (p<0.01). Total VFA, concentrations of acetic, propionic, butyric and isovaleric acids decreased linearly with increasing amount of CT. The aforementioned results show that protein binding affinity of CT from mangosteen-peel is lower than those reported for Leucaena forages, however, the former has stronger negative effect on IVDMD. Therefore, the use of mangosteen-peel as protein source and $CH_4$ mitigating agent in ruminant feed requires further investigations.

• Bulletin of the Korean Chemical Society
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• 제35권5호
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• pp.1365-1374
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• 2014

Thirteen analogs of tridecapeptide ${\alpha}$-factor (WHWLQLKPGQPMY) of Saccharomyces cerevisiae with C- or N-terminal Trp extension and isosteric replacement by Aib at position 8 and 11, Trp at position 13, D-Ala at position 9, and Orn and Glu at position 6 were synthesized and assayed for their biological activity. Receptor binding assay was carried out using our newly developed spectrophotometric method with detector peptide 14. C- or N-terminal extended analogs, ${\alpha}$-factor-$[Trp]_n$ (n =1-5) 1-5 and $[N-Trp]_1$-${\alpha}$-factor 6, were all less active than native ${\alpha}$-factor and gradual decreases in both activity and receptor affinity were observed with greater Trp extension. Trp-substituted analog at position 13, $[Trp^{13}]{\alpha}$-factor 7, exhibited about 2-fold reductions in both activity and receptor affinity. Aib-substituted analogs, $[Aib^8]{\alpha}$-factor 8 and $[Aib^{11}]{\alpha}$-factor 9, showed 5- to 10-fold reduction in activity as well as 3-fold reduction in receptor affinity compared to native ${\alpha}$-factor. $[Orn^6]{\alpha}$-factor 10 demonstrated strong potency with a 7.0-fold increase in halo activity as well as 1.8-fold increase in receptor affinity compared to native ${\alpha}$-factor. For two double substituted analogs, [$Glu^6,{\small{D}}-Ala^9$]${\alpha}$-factor 12 showed the slightly decreased potency in halo activity compared to analog 10, whereas [$Orn^6,{\small{D}}-Ala^9$]${\alpha}$-factor 11 exhibited 15-fold higher halo activity as well as nearly 3-fold higher receptor affinity compared to native ${\alpha}$-factor.

• 한국식품과학회지
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• 제20권6호
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• pp.762-768
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• 1988

우유의 지방분해 효소인 리파제를 분리 연구하기 위하여 홀몬처리 되지 않은 정상유와 홀몬 처리된 비정상유에서 리파제를 Heparin-Sepharose-CL-6B를 이용하여 분리 정제하였다. Heparin-Sepharose에 친화력을 조사한 결과 두 개의 효소활성이 있는 성분이 구분되었으며 한 성분은 Heparin-Sepharose-CL-6B에 결합되었고 다른 한 성분은 결합되지 않은 채 분리되었다. 친화성 크로마토그램에 결합되어 분리 정제된 리파제의 최적 온도, 최적 pH, 기질 특이성, 분자량 및 BSA의 활성제로서의 작용등 여러 가지 효소특성은 모두 동일한 것으로 나타났다. 그러나 홀몬처리된 소에서 얻은 우유의 경우에는 또 다른 호소활성 성분이 나타나 있음을 알았다. 이 lipolytic activity가 있는 성분은 Heparin-Sepharose-CL-6B에 친화력을 보이지 않았으므로 정상적인 milk lipase와는 구별된다. 따라서 홀몬처리된 소에서 얻은 우유에 함유된 성분중 Heparin-Sepharose에 결합된 효소는 유지방 자동산화에 영향을 끼치지 않으며 Heparin-Sepharose에 결합되자 않은 활성이 있는 성분은 자동산패에 영향을 크게 미친다고 볼 수 있다. 그 이유는 hormone의 불균형 상태로 인하여 생유에 자동산패가 일어날 수 있으며 이것은 비정상적으로 분비된 리파제 출현 사이에 연관관계가 있음을 의미한다.

• 멤브레인
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• 제1권1호
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• pp.34-43
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• 1991

물에 대해 수착선택성이 높은 아세트산 셀룰로오스 치밀막(CA막)과 에탄올에 대해 수착선택성이 높은 실리콘 고무막(SR막)을 통한 물(1)/에탄올(2) 이성분 혼합액의 투과증발에 있어서 막의 친화성과 최적 조업조건의 관계를 조사하였다. CA막과 SR막을 제조하여, 이들 막에서의 수착량, 수착선택도, 투과증발 분리도 및 투과증발 속도를 실험으로 구하고 서로 비교하였다. 하류압력의 영향을 Thompson다이아그램을 써서 분석하였고, 공급액 농도와 조업 온도 변화에 따른 수착 및 투과증발 특성을 활동도 계수, 가소화 효과, 활성화에너지 등으로 설명할 수 있었다. CA막을 사용한 물의 분리의 경우에는 물에 대한 투과증발 분리도 ($[\alpha^2_1]_{PV}$) 및 투과증발 속도 모두 하류압력이 낮고, 공급액의 농도가 중간 정도이고, 온도가 높은 조업조건이 유리하였다. 그러나 SR막을 사용한 에탄올의 분리의 경우에는 에탄올에 대한 투과증발 분리도 ($[\alpha^2_1]_{PV}$) 는 하류압력이 높을수록, 공급액 중의 에탄올 농도가 낮을수록, 조업온도가 낮을수록 증가하였지만, 투과증발 속도는 반대의 경향을 나타내었다.

• BMB Reports
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• 제39권5호
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• pp.586-594
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• 2006

Germinal centers (GCs) have been identified as site at which the somatic mutation of immunoglobulins occurs. However, somatic mutations in immunoglobulins have also been observed in animals that normally do not harbor germinal centers. This clearly indicates that somatic mutations can occur in the absence of germinal centers. We therefore attempted to determine whether or not GCs exist in TNFR1-deficient mice, and are essential for the somatic mutation of immunoglobulins, using (4-hydroxy-3-nitropheny)acetyl-ovalbumin (NP-OVA). Both wild-type and TNFR1-deficient mice were immunized with NPOVA, and then examined with regard to the existence of GCs. No typical B-cell follicles were detected in the TNFR1-deficient mice. Cell proliferation was detected throughout all splenic tissue types, and no in vivo immune-complex retention was observed in the TNFR1-deficient mice. All of these data strongly suggest that no GCs were formed in the TNFR1-deficient mice. Although TNFR1-deficient mice are unable to form GCs, serological analyses indicated that affinity maturation had been achieved in both the wild-type and TNFR1-deficient mice. We therefore isolated and sequenced several DNA clones from wild-type and the TNFR1-deficient mice. Eight out of 12 wild-type clones, and 11 out of 14 clones of the TNFR-1-deficient mice contained mutations at the CDR1 site. Thus, the wild-type and TNFR1-deficient mice were not extremely different with regard to types and rates of somatic mutation. Also, high-affinity antibodies were detected in both types of mice. Collectively, our data appear to show that affinity maturation may occur in TNFR1-deficient mice, which completely lack GCs.