• Journal of Applied Biological Chemistry
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• 제49권3호
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• pp.110-113
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• 2006

Prolyl endopeptidase (PEP, EC 3.4.21.26, also referred to as prolyl oligopeptidase) degrades proline containing, biologically active neuropeptides such as vasopressin, substance P and thyrotropin-releasing hormone by cleaving peptide bonds on carboxyl side of prolyl residue within neuropeptides of less than 30 amino acids. Evaluation of PEP levels in postmortem brains of Alzheimer's disease patients revealed significant increases in PEP activity. Therefore, a specific PEP inhibitor can be a good candidate of drug against memory loss. Upon our examination for PEP inhibitory activity from micronutrients, ascorbic acid (vitamin C) showed small but significant PEP inhibition (13% PEP inhibition at $8{\mu}g{\cdot}ml^{-1}$). Palmitic acid showed almost no PEP inhibition. However, 6-O-palmitoyl ascorbic acid ($\underline{1}$) showed 70% PEP inhibition at $8{\mu}g{\cdot}ml^{-1}$ indicating that hydrophobic portion of the compound $\underline{1}$ may facilitate the inhibitory effect. $IC_{50}$ value of compound $\underline{1}$ was $12.6{\pm}0.2{\mu}M$. The primary and secondary Lineweaver Burk and Dixon plots for compound $\underline{1}$ indicated that it is a non-competitive inhibitor with inhibition constant (Ki) value of $23.7{\mu}M$.

• Journal of Ecology and Environment
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• 제29권4호
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• pp.337-342
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• 2006

The total monoterpenoid content of the pine litter layer and the availability of these compounds as inhibitors/stimulators on Polysphondylium violaceum of cellular slime molds were investigated. In order to determine the several monoterpenoids in the natural environment, we examined their concentrations in fresh, senescent, and decaying needles from 3 pine species (Pinus densiflora, P. thunbergii, P. rigida) by litter bag method. Total monoterpenoid content was highest in the fresh needles, but also remained relatively high in senescent needles. The effect of monoterpenoids identified from Pinus plants on the growth of P. violaceum was studied. We tested four concentrations (1, 0.1, 0.01, and $0.001\;{\mu}g/{\mu}L$) of each compound by using a disk volatilization technique. Each compound was treated after germination of spores of P. violaceum. All of the compounds at $1\;{\mu}g/{\mu}L$ concentration had a very strong inhibitory effect on cell growth of P. violaceum. Fenchone at all concentrations, myrcene, verbenone, bornyl acetate, and limonene at low concentrations stimulated the growth of P. violaceum. These results suggest that inhibitory or enhancing effects of selected monoterpenoids depend upon the concentration of the individual compound.

• 동의생리병리학회지
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• 제16권6호
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• pp.1157-1163
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• 2002

This experimental research has been done to study the effects of Gmibojungikgi-tang(GBJIKT) on the anti-allergic reaction. We found the several important results from the research which has been performed by two experiments toward immediately type and delayed type in order to study the effects of GBJIKT on hypersensitivity response to mice. The results obtained from our research are as following: The survival rate of one group to which we injected only the compound 48/80 is almost 0% according to its density and timing test. In the other hand, the survival rates of the other group to which we injected both of the compound 48/80 and GBJIKT are 10%, 10%, 20%, 30%, 20%, and 40% according to 0.025, 0.05, 0.1, 0.25 0.5 and 1(mg/g) of compound 48/80. Time dependency test also shows the 0% survival rates in 5 and 10 minutes. GBJIKT revealed the significantly inhibitory effect on Compound 48/80 induced Mast cell degranulation. GBJIKT showed the significantly inhibitory effect in the delayed type hypersensitivity response to picry1 chloride GBJIKT showed the significantly inhibitory effect in the delayed type hypersensitivity response to sheep red blood cell. Our research provides the important evidence that GBJIKT is benificial to the prevention and treatment of allergy related diseases.

• 동의생리병리학회지
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• 제17권2호
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• pp.308-315
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• 2003

This experimental research has been done to study the effects of Sipjeondaebo-tang(SOT) on the anti-allergic reaction. We found the several important results from the research which has been performed by two experiments toward immediately type and delayed type in order to study the effects of SDT on hypersensitivity response to mice. The results obtained from our research are as following. The survival rate of one group to which we injected only the compound 48/80 is almost 0% according to its density and timing test. In the other hand, the survival rates of the other group to which we injected both of the compound 48/80 and SDT are 20%, 10%, 30%, 10%, 40% and 70% according to 0.025, 0.05, 0.1, 0.25 0.5 and 1 (mg/g) of compound 48/80. Time dependency test also shows the 30% and 20% survival rates in 5 and 10 minutes. SDT revealed the significantly inhibitory effect on Compound 48/80 induced Mast cell degranulation. SDT showed the significantly inhibitory effect in the delayed type hypersensitivity response to picry1 chloride. SDT showed the significantly inhibitory effect in the delayed type hypersensitivity response to sheep red blood cell. Our research provides the important evidence that SDT is benificial to the prevention and treatment of allergy related diseases.

• 한국환경과학회지
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• 제28권11호
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• pp.993-1004
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• 2019

Chrysanthemum boreale Makino (C. boreale) is widely distributed in Asian countries, and has traditionally been used to treat various inflammatory diseases including bronchitis. In this study, we aimed to isolate biologically active compounds from leaves and stems of C. boreale. Chemical components were purified by column chromatograpy and recyclic HPLC, and characterized from their spectral data (IR, MS, NMR). Biological activity experiments were conducted for Farnesyl-protein transferase (FPTase) activity, apoptosis and nitirc oxide (NO) release. As a results, three sesquiterpene lactones were isolated. Compound 1 (4-methoxy-8-O-acetyl-10-hydroxy-2,11(13)-guaiadiene-12,6-olide) showed strong cytotoxic activities having an average growth inhibition of 50% ($GI_{50}$) value of $1.89{\mu}g/m{\ell}$ against human colon adenocarcinoma cells. Compound 1 also showed a low half maximal inhibitory concentration ($IC_{50}$) value of $10{\mu}g/m{\ell}$ for NO release. In the caspase 3 activity, compound 1 and compound 2 (8-O-(2-carbonyl-2-butyl)-3,10-dihydroxy-4,11(13) -guaiadiene-12,6-olide) exhibited 94% and 90% apoptosis inhibition activity, respectively. Compound 3 (4,8-O-diacetyl -10-hydroxy-2(3),11(13)-guaiadiene-12,6-olide) showed a strong inhibitory effect on FPTase activity with 90% inhibitory activity at a concentration of $100{\mu}g/m{\ell}$. These results clearly show the presence of lactone compounds in the leaves and stems, which may partially contribute to the pharmacological activity of C. boreale.

• Archives of Pharmacal Research
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• 제23권1호
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• pp.46-49
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• 2000

Two neolignan compound, magnolol $(5,5^{l}-diallyl-2,2^{l}-dihydroxybiphenyl, 1)$ and honokiol $(5,5^{l}-diallyl-2,4^{l}-dihydroxybiphenyl, 2)$ were isolated from the stem bark of Magnolia obovata and evaluated for antifungal activity against various human pathogenic fungi. Compound 1 and 2 showed significant inhibitory activities against Trichophyton mentagrophytes, Microsporium gypseum, Epidermophyton floccosum, Aspergillus niger, Cryptococcus neoformans, and Candida albicans with minimum inhibitory concentrations (MIC) in a range of $25-100{\mu}g/ml$. Therefore, compound 1 and 2 could be used as lead compounds for the development of novel antifungal agents.

• Applied Biological Chemistry
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• 제50권3호
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• pp.204-209
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• 2007

산사 추출물로부터 ${\alpha}-amylase$, ${\alpha}-glucosidase$ 저해활성을 탐색하고 Sephadex LH-20($5{\times}45$ cm)와 MCI-gel CHP-20를 이용하여 저해활성 물질을 정제하고 구조분석을 하였다. 산사 추출물의 페놀화합물의 함량은 물 추출물에서 22.5 mg/g, 60% ethanol 추출물에서 19.2 mg/g으로 나타났으며, 산사 물 추출물 (200 ${\mu}g/ml$)에서 ${\alpha}-amylase$, ${\alpha}-glucosidase$ 저해활성이 각각 100%와 82.6%로 나타났으나, 60% ethanol 추출물(200 ${\mu}g/ml$)에서는 ${\alpha}-glucosidase$ 저해활성이 12%로 낮은 저해활성을 나타내어 산사 물 추출물을 Sephadex LH-20를 이용하여 분획한 결과 I, II, III, IV의 4가지 분획물을 획득하고 다시 Sephadex LH-20과 MCI-gel을 이용하여 nomal phase type인 $EtOH{\rightarrow}H_2O$와 reverse phase type인 $H_2O{\rightarrow}MeOH$로 유기용매의 농도를 증가 시키며 용출하여 A, B, C, D의 compounds를 얻었다. 4가지 compound 중 compound C(200 ${\mu}g/ml$)가 ${\alpha}$-amylase, ${\alpha}$-glucosidase 저해활성이 각각 97.6%, 97.7%로 가장 높게 나타났으며, FAB-MS, NMR과 IR spectrum을 분석한 결과 chlorogenic acid로 동정되었다.

• Mycobiology
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• 제37권1호
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• pp.31-36
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• 2009

A phytochemical study on the flower of Calotropis gigantea (Linn.) using silica gel column chromatography and preparative thin layer chromatography, led to the first time isolation of Di-(2-ethylhexyl) phthalate (compound 1) and anhydrosophoradiol-3-acetate (compound 2). The structures of these compounds were confirmed by spectroscopic analyses (IR, HRTOFMS and NMR). The antibacterial and antifungal activities of ethyl acetate extract, compound 1 and compound 2 were measured using the disc diffusion method. Ethyl acetate extract and compound 1 presented better results than compound 2. The minimum inhibitory concentrations (MICs) of the extract and compounds were found to be in the range of $16{\sim}128{\mu}g/ml$. The cytotoxicity ($LC_{50}$) against brine shrimp nauplii (Artemia salina) were also evaluated and found to be 14.61 ${\mu}g/ml$ for ethyl acetate, 9.19 ${\mu}g/ml$ for compound 1 and 15.55 ${\mu}g/ml$ for compound 2.

• Archives of Pharmacal Research
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• 제24권5호
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• pp.441-445
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• 2001

Resveratrol, a trihydroxystilbene found in grapes and several plants, has been shown to be active in inhibiting multistage carcinogenic process. Using resveratrol as the prototype, we synthesized several analogs and evaluated their growth inhibitory effect using cultured human cancer cells. In the present report we show that one of the resveratrol analogs, 3, 5,2',4'-tetramethoxy-trans-stilbene, potentiated the inhibition of cancer cell growth. Prompted by the strong growth Inhibitory activity of the compound ($IC_{50}$; $0.8{\mu}$ g/ml) compared to resveratrol ($IC_{50}$; $18{\mu}$ug/ml) in cultured human colon cancer cells (Col2), we performed an action mechanism study using the compound. The compound induced the accumulation of cellular DNA contents in the sub-CO phase DNA contents of the cell cycle by in a time-dependent manner. The morphological changes were also consistent with an apoptotic process. This result indicated that the compound induced apoptosis of cancer cells, and may be a candidate for use in the development of potential cancer chemotherapeutic or cancer chemopreventive agents.

• 통합자연과학논문집
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• 제11권2호
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• pp.107-112
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• 2018

p38 MAP kinase belongs to the Mitogen-activated protein (MAP) kinase family; a serine/threonine kinase. It plays an important role in intracellular signal transduction pathways. It is associated with the development and progression of various cancer types making it a crucial drug target. Present study involves the HQSAR analysis of recently reported imidazo[1,2-b]pyridazine derivatives as p38 MAP kinase antagonists. The model was generated with Atom (A), bond (B), chirality (Ch), and hydrogen (H) parameters and with different set of atom counts to improve the model. An acceptable HQSAR model ($q^2=0.522$, SDEP=0.479, NOC=5, $r^2=0.703$, SEE=0.378, BHL=97) was developed which exhibits good predictive ability. A contribution map for the most active compound (compound 17) illustrated that hydrogen and nitrogen atoms in the ring A and ring B, as well as nitrogen atom in ring C and the hydrogen atom in the ring D provided positive activity in inhibitory effect while, the least active compound (compound 05) possessed negative contribution to inhibitory effect. Hence, analysis of produced HQSAR model can provide insights in the designing potent and selective p38 MAP kinase antagonists.