• 한국식품과학회지
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• 제54권2호
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• pp.126-133
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• 2022

본 연구에서는 달래의 특징적인 향 특성을 확인하기 위해 봄에 수확한 노지 재배 달래와 시설 재배 달래를 SAFE법으로 추출하고 GC-MS-O를 통해 휘발성 향기성분을 분석하였다. 달래는 알데하이드류와 황 함유 화합물의 함량이 높았으며, 휘발성 성분으로는 2-methyl-2-pentenal, 2-methyl-2-butenal 및 (E)-1-propenyl propyl trisulfide의 함량이 높았다. 달래의 향 특성에 기여하는 주요한 향 활성 화합물은 2-methyl-2-pentenal, (Z)-1-propenyl methyl disulfide, dipropyl disulfide, dimethyl trisulfide, (E)-1-propenyl propyl disulfide, dipropyl trisulfide, (E)-1-propenyl propyl trisulfide, 2-isopropyl-3-methoxypyrazine 및 2-sec-butyl-3-methoxypyrazine으로 총 9종이 확인되었다. 2-Isopropyl-3-methoxypyrazine와 2-sec-butyl-3-methoxypyrazine은 달래의 흙 냄새에 기여하는 화합물로 가장 강한 향 강도를 보였다. Dipropyl disulfide, dimethyl trisulfide 및 dipropyl trisulfide는 달래의 양파 및 마늘과 같은 향 특성에 기여하는 화합물로 향 강도가 피라진류 다음으로 강했고, 노지 재배 달래에서 시설 재배 달래보다 더 강하게 감지되었다. 2-Methyl-2-pentenal, (Z)-1-propenyl methyl disulfide 및 (E)-1-propenyl propyl disulfide는 달래에서 자른 양파와 같은 매운 향 특성에 기여하는 화합물로 노지 재배 달래에서 더 높은 함량과 강도를 보였다. (E)-1-Propenyl propyl trisulfide 와 (E)-1-propenyl methyl disulfide은 절인 야채 및 양배추 냄새에 기여하는 화합물로서 노지 재배 달래에서 낮은 함량과 향 강도를 보였다.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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• pp.185-185
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• 1998

As part of our continuing attempts to evaluate biologically active compounds from fruiting bodies of cultivated fungus of Paecilomyces japonicus Yasuda, we conducted series of experiments on various fractions and compounds isolated by systematic fractionations. Our main efforts were concentrated on searching for compounds showing antitumor activities, which were tested on mice carrying Sarcoma-180 ascitic tumor. The antitumor activity was assessed by the life spans after these mice were administered Lp. with test compounds for consecutive 20 days. One of two pure compounds, which we have isolated to date, demonstrated significant prolongation of life span. ( Mean Survival Time: 30.3 days compared to that of control: 23.6 days). Structural analysis showed that this compound corresponds to D-mannitol. On the other hand, Ergosterol, another isolated pure compound didn't show efficient antitumor activity. We also obtained water-soluble fractions containing protein-bound polysaccharides and n-butantol fractions, which showed strong antitumor activities, 35.4(150%) and 32.1(136.0%) days of MST, respectively. In SRB assay, however, the test materials didn't show any toxic effects, but the level of acid phosphatase increased significantly when they were applied in cultured macrophage in vitro. Therefore, we concluded that antitumour activities might be attributed to immunostimulating rather than cytotoxic effects. Further experiments are underway to purify and structurally characterize new antitumour compounds from the active fractions.

• Natural Product Sciences
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• 제28권2호
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• pp.45-52
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• 2022

The identification of Plasmodium falciparum enoyl acyl-carrier protein reductase (pfENR) is considered as a potential biological target against malaria. Trema orientalis is considered a rich source of phytochemicals useful in malaria treatment. This study evaluated the in-vitro inhibitory activity of the extract and isolated compounds of T. orientalis leaf; the isolated compounds and the analogues of the most active compound were subjected to in-silico molecular docking studies on pfENR. The methanolic extract of T. orientalis was subjected to repeated chromatographic separation which led to the isolation of some compounds. The isolated compounds from the plant were examined for their antimalarial activity using β-hematin inhibition assay. Virtual screening via molecular docking and ADMET studies were conducted to gain insight into the mechanism of binding of ligand and to identify effective pfENR inhibitors. The isolated compounds and the analogues of the most active isolates were gotten from PubChem library for use in docking study. Hexacosanol and β-sitosterol showed inhibition of the β-hematin formation. The docking results showed that hexacosanol, β-sitosterol and the analogues of β-sitosterol displayed binding energy ranging between -6.1 kcal/mol and -11.6 kcal/mol. Sitosterol glucoside has the highest docking score. Some of the ligands showed more binding affinity than known bioactive compounds used as reference. Analogues of β-sitosterol has been shown to be potential inhibitors of pfENR, therefore, the findings from this study suggest that sitosterol glucoside and ergosterol peroxide could act as antimalarial agents after further lead optimisation investigations.

• 한국자원식물학회지
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• 제9권1호
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• pp.47-54
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• 1996

할미꽃의 뿌리에 함유되어 있는 제초활성물질의 확인과 동정을 위하여 이들을 추출 정제하고 활성성분 및 제초활성을 조사하여 다음과 같은 결과를 얻었다. 1. 각종 칼럼크로마토그래피법과 Prep. HPLC의 순차적인 적용에 의해 제초활성물질이 포함된 할미꽃 뿌리의 메타놀추출물을 정제하여 2개의 활성분획을 획득하였다. 2. 최종적으로 얻어진 활성분획들을 100ppm의 농도로 조제하여 처리한 결과, 식용피 유근의 생장 억제율은 대조구에 비해 각각 48% 및 60%로 나타났다. 3. GC-MS Spectrometry에 의해 분리된 활성분획 중의 성분들을 기존자료들과 비교하여 수종의 지방산 에스테르, 2종의 탄화수소류, squalene, evidonol 및 1종의 diazepin 관련 화합물이 동정되었다.

• Archives of Pharmacal Research
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• 제29권12호
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• pp.1119-1124
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• 2006

The methanol extract from the aerial parts of Dictamnus albus was active in inhibiting monoamine oxidase (MAO) from the mouse brain. Activity-guided fractionation led to the isolation of four known coumarins, 7-(6'R-hydroxy-3', 7'-dimethyl-2'E, 7'-octadienyloxy) coumarin (1), auraptene (2), umbelliferone (3), and xanthotoxin (4), as active compounds along with an inactive alkaloid, skimmianine (5). Compounds 1 and 2 inhibited MAO activity in a concentration-dependent manner with $IC_{50}$ values of 0.7 and $1.7\;{\mu}M$, respectively. Compounds 1 and 2 showed a slight and potently selective inhibitory effect against MAO-B ($IC_{50}\;0.5\;and\;0.6\;{\mu}M,\;respectively$) compared to MAO-A ($IC_{50}\;1.3\;and\;34.6\;{\mu}M,\;respectively$). According to kinetic analyses derived by Lineweaver-Burk reciprocal plots, compounds 1 and 2 exhibited a competitive inhibition to MAO-B.

• KSBB Journal
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• 제11권5호
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• pp.536-542
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• 1996

충치 예방 물질의 탐색 연구 일환으로, Cacao bean husk(CBH) 추출물로부터 얻어진, gluco-syltransferase(Gtase) 저해 활성 분획을 분리하였 다. 이를 다시 MCI-gel CHP-20와 Sephadex LH 20의 column chromatography법으로 분리, 정제하였으며, 이로부터 얻어진 2개의 GTase 활성 저해 물질에 대한 구조 해석을 행하였다. 분리.정제된 2개의 GTase 저해 활성 물질은 anisaldehyde-$H_2SO_4$ 및 FeCb에서 각각 갈색 및 청색 반응을 하며, 또 TLC상에서 dimer의 flavan-3-ol $R_r$값을 나타내는 단일 물질이었다. NMR(PMR, C CMR) 빛 mass spectrum으로 두 정제 분획에 대 한 화학 구조를 분석한 결과, G Tase 저해능을 나타 내는 단물질은 (-)-epicatechin-($\beta\rightarrow8$)-catechin 으로 결합된 procyanidin B-1 ($C_{30}H_{26}O_{12}$) 및 cate chin의 2량체인 procyanidin B一3($C_{30}H_{26}O_{12}$)이었다.

• Archives of Pharmacal Research
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• 제27권5호
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• pp.495-501
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• 2004

A series of N-substituted-1,3-isoindolinedione derivatives (2-16) were synthesized for the purpose of defining the effect of N-substitution on the anticonvulsant activity of these derivatives. The target compounds (2-16) were obtained by condensation of phthalic anhydride with the corresponding amine derivative. The structures of the synthesized derivatives (2-16) were confirmed by means of IR, $^1$H-NMR, $^{13}$ C-NMR, MS and elemental analyses. The anticonvulsant activity of all compounds (2-16) were evaluated by subcutaneous pentylenetetrazole seizure threshold test at doses of 0.2, 0.4 and 0.8 mmol/kg compared with sodium valproate as a positive control. Their neurotoxicity were determined by the rotorod test. Many of the present series of compounds showed good anticonvulsant activity at the tested doses, as compared to sodium valproate. Three of them (4, 6 and 11) exhibited 100 % protection against convulsions, neurotoxicity and death at all tested doses. Out of the series, two compounds (12 and 13) were completely inactive with 100% mortality. 3-(p-chlorophenyl)-4-(1 ,3-dioxo-2,3-dihydro-1 H-2-isoindolyl) butanoic acid derivative (11) has emerged as the most active compound which is 20 times more active than valproate with ED$_{50}$ 8.7, 169 mg/kg; TD$_{50}$ 413, 406 mg/kg and PI 47.5, 2.4. The results revealed the importance of the combination of baclofenic and phthalimide moieties (compound 11) as a promising anticonvulsant candidate.

• 한국해양바이오학회지
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• 제2권4호
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• pp.209-223
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• 2007

Nature is one of the most important sources of pharmacologically active compounds in the search for drugs against life threatening diseases. Even though plants and terrestrial microorganisms have played as an important source for the new drug candidates from nature, marine organisms such as tunicates, sponges, soft corals, sea horses, sea snakes, marine mollusks, seaweeds, nudibranches, sea slugs and marine microorganisms are increasingly attracting attention in recent years. Marine organisms also have the potential to develop into future drugs against important diseases, such as cancer, a range of bacterial and viral diseases, malaria, and inflammations. Even though the mechanism of action in the molecular level of most metabolites is still unclear, the mechanisms by which they interfere with the pathogenesis of a wide range of diseases have been reported. The knowledge of this is one of the key factors necessary to develop bioactive compounds into medicines. This is due to their structurally unique and pharmacologically active compounds. The potential pharmaceutical, medicinal and research applications of some of these compounds are discussed in hundreds of scientific papers, and are reviewed here.

• 한국미생물·생명공학회지
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• 제19권3호
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• pp.235-241
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• 1991

Streptomyces melanosporofaciens로 동정된 strain 88-GT-161 균주는, 그람양성세균 및 식물병원성 곰팡이에 각각 항균활성을 나타내는 phthalate 유도체 및 염기성 마크로라이드의 새로운 항생물질을 생산하는 것으로 밝혀졌다. 이들 활성물질들의 분리. 정제과정에서 in vitro 및 in vivo(포트 시험) 항균활성을 조사하였으며, phtahalate 유도체 항생물질은 IR, NMR, 질량분석 스펙트럼 조사를 통하여 bis(2-ethylexyl) phthalate(dioctyl phthalate)로 동정하였다. Dioctyl phthalate가 Streptomyces sp.에 의하여 생산되며 생합성된 이 화합물이 항균활성을 가진다는 사실이 보고된 것은 이것이 처음이다.

• Archives of Pharmacal Research
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• 제28권8호
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• pp.892-896
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• 2005

In order to isolate substances that inhibit the hemolytic activity of human serum against eryth-rocytes, we have evaluated whole plants of the Orostachys japonicus species with regard to its anti-complement activity, and have identified its active principles following activity-guided isolation. A methanol extract of the O. japonicus, as well as its n-hexane soluble fraction, exhibited significant anti-complement activity on the complement system, which was expressed as total hemolytic activity. A bioassay-guided chromatographic separation of the constituents resulted in the isolation of three known compounds 1-3 from the active n-hexane fraction. The structure of these compounds were analyzed, and they were identified as hydroxyhopanone (1), $\beta-sitosteryl-3-O-\beta-D-glucopyranosyl-6'-O-palmitate$ (2), and $\beta-sitosteryl-3-O-\beta-D-glucopyranoside$ (3), respectively. Of these compounds, compound 2 exhibited potent anti-complement activity $(IC_{50}=1.0\pm0.1{\mu}M)$ on the classical pathway of the complement, as compared to tiliroside $(IC_{50}=76.5\pm1.1{\mu}M)$, which was used as a positive control. However, compounds 1 and 3 exhibited no activity in this system.