• 대한환경공학회지
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• 제31권2호
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• pp.147-152
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• 2009

본 연구에서는 톨루엔 계열 화합물로 오염된 환경에 대해 고정화한 유전자 재조합 균주 KG1206의 적용 가능성에 대해 조사하였다. 재조합 균주 KG1206은 직접 유도제인 m-toluate, benzoate 뿐만 아니라 톨루엔, 자일렌 이성질체가 간접 유도제로서 발광 활성을 나타낸다. 연구에 의해 결정된 고정화 프로토콜의 최적 조건은 다음과 같다: 균주 농도(1 : 1 (v/v)), 오염원 용액(인산염 완충액), 발광 측정에 필요한 비드 수(4개), 5가지 오염원에 대한 최대 발광 활성은 일반적으로 m-toluate > p-xylene > 톨루엔 > o-xylene > m-xylene 순으로 나타났다. 생물발광과 오염원 감소는 HPLC로 확인하였으며, 고정 균주에 의해 초기 5 mM m-toluate는 5시간 배양 후 약 48%의 감소율을 나타내었으며 계속 분해되는 경향이 관찰되었다. 알긴산 균주 고정화에 대한 본 연구 결과는 톨루엔 계열 화합물을 함유한 석유계 탄화수소에 오염된 특정 환경을 생물학적 모니터링에 유용한 방법으로 사용할 수 있을 것이다.

• 약학회지
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• 제42권2호
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• pp.165-169
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• 1998

Inhibitory effects of 16 cinnamic acid analogs on formyl-Met-Leu-Phe(fMLP)-induced chemotaxis of rat polymorphonuclear leukocytes were determined by using a microchemotaxis appa ratus. 3,4-Dlhydrocinnamic acid called as caffeic acid exhibited the highest inhibitory effect on the chemotaxis among cinnamic acid analogs tested in this study. Hydroxycinnamic acids exhibited stronger inhibitory effects on the chemotaxis than cinnnamic acid. Hydroxycinnamic acids with one hydroxy group at ortho, meta or para position exhibited similar inhibitory effects on the chemotaxis with corresponding methoxy cinnamic acids, but 3,4-dihydroxycinnamic acid did stronger inhibitory effects than 3,4-dimethoxycinnamic acid. 3,4-Dimethoxycinnamic acid exhibited weaker inhibitory effects on the chemotaxis than 1,2-dimethoxy-4-propenylbenzene and 3,4-dimethoxy cinnamonitrile with -CH=CHCN or -CH=$CHCH_3$, group instead of -CH=CHCOOH group. 4-Hydroxy cinnamic acid and 3,4-dihydroxycinnamic acid exhibited stronger exhibitory effects on the chemotaxis than 3-(4-hydroxyphenyl) propionic acid and 3,4-dihydroxyhydrocinnamic acid with -$CH_2CH_2$COOH group instead of -CH=CHCOOH group.

• Genomics & Informatics
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• 제19권4호
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• pp.48.1-48.10
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• 2021

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) encodes small envelope protein (E) that plays a major role in viral assembly, release, pathogenesis, and host inflammation. Previous studies demonstrated that pyrazine ring containing amiloride analogs inhibit this protein in different types of coronavirus including SARS-CoV-1 small envelope protein E (SARS-CoV-1 E). SARS-CoV-1 E has 93.42% sequence identity with SARS-CoV-2 E and shared a conserved domain NS3/small envelope protein (NS3_envE). Amiloride analog hexamethylene amiloride (HMA) can inhibit SARS-CoV-1 E. Therefore, we performed molecular docking and dynamics simulations to explore whether amiloride analogs are effective in inhibiting SARS-CoV-2 E. To do so, SARS-CoV-1 E and SARS-CoV-2 E proteins were taken as receptors while HMA and 3-amino-5-(azepan-1-yl)-N-(diaminomethylidene)-6-pyrimidin-5-ylpyrazine-2-carboxamide (3A5NP2C) were selected as ligands. Molecular docking simulation showed higher binding affinity scores of HMA and 3A5NP2C for SARS-CoV-2 E than SARS-CoV-1 E. Moreover, HMA and 3A5NP2C engaged more amino acids in SARS-CoV-2 E. Molecular dynamics simulation for 1 ㎲ (1,000 ns) revealed that these ligands could alter the native structure of the proteins and their flexibility. Our study suggests that suitable amiloride analogs might yield a prospective drug against coronavirus disease 2019.

• Journal of Dairy Science and Biotechnology
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• 제41권1호
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• pp.26-33
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• 2023

Eugenol, which can be extracted from clove oil, is a phenolic aromatic compound and has been found to have antibacterial, antiviral, antifungal, anticancer, anti-inflammatory, and antioxidant functions. Consequently, clove oil has long been used in several fields (food, medicine, skincare). Hence, in this study, the sensory profile of clove oil contained in milk analogs (almond, oat, and soy milks) was evaluated at different amounts (added at 0.25%-0.5% increments from 0% to 1.5%). Because of the strong scent of clove oil, the value of the evaluation for sensory profile determined in this study tended to be low. However, compared with the control group, good values in the evaluation for the sensory profile were found in all samples containing 0.25% of clove oil. We evaluated clove oil contained in milk analogs to help increase their sales through products with improved functionality.

• Journal of Microbiology and Biotechnology
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• 제26권1호
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• pp.56-60
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• 2016

Two new glucosides (1 and 2) of geldanamycin (GA) analogs were obtained from in vitro glycosylation by UDP-glycosyltransferase (YjiC). Based on spectroscopic (HR-ESI-MS, 1D, and 2D-NMR) analyses, the glucosides were elucidated as 4,5-dihydro-7-O-descarbamoyl-7-hydroxyl GA-7-O-β-D-glucoside (1) and ACDL3172-18-O-β-D-glucoside (2). Furthermore, the water solubility of compounds 1 and 2 was about 215.2 and 90.7 times higher respectively, than that of the substrates. Among compounds 1-4, only 3 showed weak antiproliferative activity against four human tumor cell lines: MDA-MB-231, SMMC7721, HepG2, and SW480 (IC₅₀: 13.6, 15.1, 31.8, and 22.7 μM, respectively).

• Bulletin of the Korean Chemical Society
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• 제32권spc8호
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• pp.3009-3016
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• 2011

To investigate the possible isosteric replacement of imidazolidinone moiety in 4-phenyl-N-arylsulfonylimidazolidinone for broad and potent anticancer agents, a series of 4-phenyl-l(N)-arylsulfonylimidazolidinones 6a-k, imidazolidinethione analogs 7a-i, and imidazolidine oxime analogs 8a-c were prepared and evaluated for their in vitro anticancer activity against four human cancer cell lines (human lung A549, human colon COLO205, human leukemia K562, human ovary SK-OV-3). Among all the derivatives of N-arylsulfonylimidazolidinone 6a-k, compounds 6f and 6g showed the best inhibition comparable to doxorubicin against all cancer cell lines. Increasing the carbon chain on alkyl moieties of carbamates as shown in 6c-g did not alter the activity. The imidazolidinethione analogs 7a-i and imidazolidin-2-one oxime derivatives 8a-c did not possess any good activity. Therefore, imidazolidinone moiety is the best pharmacophore among the 4-phenyl-Narylsulfonylimidazolidinone derivatives.

• 대한화학회지
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• 제55권5호
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• pp.765-775
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• 2011

Novel analogs of bortezomib were designed, synthesized and in vitro biological evaluation was carried out using human tumor cell lines A549 and PC3. Docking studies of these analogs of bortezomib was discussed. According to biological investigations, the inhibitors 4, 6, and 8 were found to be more potent than reference drug candidate bortezomib. A549 cell line showed significant sensitivity towards 4, 6, and 8 with $IC_{50}$ values 14.03, 18.5, and 12.4 nM, respectively, and PC3 cell line showed IC50 values 26.1, 37.0, and 21.2 nM, respectively. The $IC_{50}$ values of bortezomib in these cell lines are 27.3 nM and 42.0 nM.

• BMB Reports
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• 제30권6호
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• pp.415-420
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• 1997

Although $CD4^+$ T cell responses to protein-derived antigen have well been understood, the epitopes recognized by hapten-specific $CD4^+$ T cells have not been fully defined. In this study, we characterized the response of a T cell hybridoma (5Di0.1B8) which is specific for a hapten. N-hydroxysuccinimidyl-4-azidobenzoate (HSAB) restricted by MHC class II $I-A^d$. Using three different antigen presenting cells (APCs) expressing $I-A^d$, the role of class II MHC proteins in haptenic antigen presentation and subsequent activation of 5D10.1B8 has been examined. Activation of 5D10.1B8 T cells by HSAB analogs was also performed. Our results show that each APC activated T cells differentially and that interleukin-2 (IL-2) augmented antigen-presenting ability of all the APCs, suggesting that increased expression of class II MHC protein by IL-2 played an important role in HSAB presentation and T cell activation. Finally, early T cell receptor-dependent signals induced by HSAB or its analogs were examined by phosphotyrosine immunoblot analysis, and showed that tyrosine phosphorylation level of a 18-20 kD protein increased upon stimulation.

• KSBB Journal
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• 제27권2호
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• pp.121-126
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• 2012

In order to explore structural features of minoxidil analogs with a view of enhancing lysyl hydroxylase (LH) inhibitory activity, molecular holographic QSAR (HQSAR) and CoMSIA (comparative molecular similarity indices analysis) were performed. The results from the atomic contributions with optimized the HQSAR 6-2 model indicated that, in case of pyrimidine-1-N-oxide substituent, C2 atom of pyrimidine ring and C'3-C'4 bond of 4-piperidinol group showed the highest impact on the inhibitory activity towards LH enzyme. It was also evident from the information of the optimized CoMSIA F5 model that the inhibitory activity mainly depended on the hydrophobic field contribution (36%) and the hydrogen bond (H-bond) field contribution (49.2%) of substrate molecule. Particularly, it is predicted that the functional groups which disfavor H-bond acceptors in large space around the piperidinol group and also the functional groups which favor the H-bond acceptors at C'4 (& C'5) atom in $R_5$ group play a role for increased inhibitory activity. With this in mind, it is likely that a novel candidate having more improved inhibitory activity on hair growth could be designed in the future.

• 한국응용과학기술학회지
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• 제25권3호
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• pp.380-387
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• 2008

The effects of the applied stretch and MgADP binding on the structure of the actin and myosin cross-bridges in rabbit fibers in the rigor state have been investigatedwith improved resolution by x-ray diffraction using synchrotron radiation. To clarify the structure of the ATP hydrolysis intermediates formed by actin and myosin cross-bridges,the effects of various phosphate analogs in the of MgADP on the structure of the thin and thick filaments in glycerinated rabbit muscle fibers in the rigor state investigated by x-ray diffraction with a short exposure time using synchrotron radiation. These results strongly suggest that when MgADP and phosphate analogs such as metallofluorides(BeF3 and AlF4)and vanadate(VO4(Vi)) were added the rigor fibers in the presence of the ATP-depletion backup system, the intensities of the actin-based layer lines were markedly weakened. We found that the intensity of the 14.5 nm-based meridional reflections increase by 20-50% when phosphate analogs such as metallofluorides(BeF3 and AlF4) and vanadate(VO4(Vi)) was added to the rigor muscle.