• Journal of the Korean Chemical Society
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• v.54 no.1
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• pp.158-164
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• 2010

• Proceedings of the Plant Resources Society of Korea Conference
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• 2011.10a
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• pp.19-19
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• 2011

예비실험 중 한국의 울릉도에 자생하고 취나물로 이용되고 있는 섬쑥부쟁이(Aster glehni Franchet et Sckmidt, Compositae)가 페놀성 화합물 함량이 높고 peroxynitrite 소거효과가 높았기 때문에 이를 이용한 추출물의 제조를 통한 건강기능식품을 창출하고자 하였다. 건강식품을 위한 추출물 제조를 위하여 물과 에탄올만을 이용하여 페놀성 화합물 고함유 추출물의 제조가 가능하고 높은 peroxynitrite 소거효과를 나타내는 추출물을 결정하고자 하였다. 즉, 추출용매로 Water-EtOH 비율을 조절하여 추출하여 추출물의 함량, HPLC를 이용한 caffeoylquinic acid(CQ) 화합물의 함량분석 및 peroxynitrite 소거효과를 비교하였다. Water-EtOH (7:3)으로 추출한 섬쑥부쟁이 추출물은 CQ 함량이 높고, 높은 peroxynitrite 소거효과, 항경련효과, 진정효과 및 항비만효과 등이 나타났다. 건강기능식품을 위한 추출물 제조시 한국에서는 물과 에탄올만이 허용되기 때문에 CQ 함량이 높은 추출물의 제조가 가능하고 높은 peroxynitrite 소거효과를 유지할 수 있는가에 관한 실험 이외에 마우스에서 선택된 추출물의 진정효과 및 항경련효과 실험을 수행하였다. 진정효과와 항경련효과를 위하여 마우스에서 각각 pentobarbital로 유도한 수면연장효과와 PTZ로 유도한 경련에 대한 효과를 측정하여 유의성있는 활성이 확인되었으므로 이 추출물을 이용한 건강기능식품으로의 이용이 가능하다고 생각된다.

• YAKHAK HOEJI
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• v.48 no.3
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• pp.182-188
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• 2004

This study aimed to synthesize new anticonvulsive agents as potential dual acting prodrugs. For the synthesis of ester or amide prodrug types, p-hydroxybenzaldehyde or valproic acid was coupled with clinically usable anticonvulsants or GABAmimetics with use of DCC/DMAP coupling methods. Also their anticonvulsive activities were evaluated.

• Applied Biological Chemistry
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• v.43 no.1
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• pp.72-77
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• 2000

The repeated silica gel colum chromatographies of EtOAc fraction, showing anticonvulsant activity, obtained from MeOH extracts of Schizandra chinensis B. fruits led to isolation of a sesquiterpenoid, four lignans and a sterol glycoside. Their chemical structures were determined to be chamigrenal, gomisin A, gomisin H, gomisin N. schizandrin and daucosterol. Among them, schizandrin and daucosterol inhibited GABA degrative enzymes, succinic semialdehyde dehydrogenase and succinic semialdehyde reductase, respectively. It is postulated that the schizandrin and daucosterol are able to elevate the neurotransmitter GABA levels in central nervous system by inhibitory action on GABA degrative enzymes and act as anticonvulsant drugs.

• YAKHAK HOEJI
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• v.45 no.1
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• pp.7-15
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• 2001

For the purpose of defining the effects of N-acyl groups on the anticonvulsant activities of N-acyl-$\alpha$-amino-glutarimides, various (R)- and (S)-N-acyl-$\alpha$-aminoglutarimide were prepared from the corresponding N-Cbz-glutamic acid and were evaluated their anticonvulsant activities in the MES and PTZ test, including their neurotoxicities. Among the tested compounds, only (R) N-cinnamoyl-$\alpha$-amino-N-methylglutarimide showed anticonvulsant activity in the MES and PTZ test. And the other tested compounds was active in the only PTZ test. The order of anticonvulsant activities in the PTZ test was as followes; for the (R) series, N-4-methoxycinnamoyl = cinnamoyl > N-4-nitrobenzoyl > N-benzoyl > N-phenylacetyl; for the (S) series, N-4-methoxycinnamoyl = N-3-nitrobenzoyl > N-4-nitrobenzoyl = N-cinnamoyl = N-phenylacetyl. From the above results, it was conceivable that the substituted N-acyl group had important effects on the anticonvulsant activities of these compounds. However stereoisomeric deferences in the anticonvulsant activities were not exhibited clearly.

• Journal of Applied Biological Chemistry
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• v.59 no.4
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• pp.323-330
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• 2016

Pinellia ternata Breitenbach, the natural medicinal plant of the Araceae family, is a perennial plant originated from the East Asia, but also widely distributed in Europe and North America. Its tuber is used as traditional medicine for treatment of various diseases such as vomiting, inflammation, and traumatic injury. Pharmacological studies revealed that P. ternata possesses anticonvulsant, anti-tumor, insecticidal, and cytotoxic activities. Despite being well-known as the useful medicinal plant, there is no reliable, standardized method for origin discrimination. Ultra performance liquid chromatography-photodiode array detector and quadrupole time of flight-mass spectrometry based metabolite-profiling was applied to explore significant metabolite for origin discrimination between Korean and Chinese P. ternata. One compound was isolated from Korean P. ternata using repeated ODS column chromatography by bioactivity guided fractionation, and determined as [6]-gingerol according to the results of spectroscopic data including nuclear magnetic resonance and MS. This compound was selected as cosmeceutical biomarker by fingerprints, and it was associated to melanin inhibitory effect determining its origin authenticity. Furthermore, the calibration curve of biomarker was prepared using validated method for the comparison of content between Korean and Chinese P. ternata. This is the report to address the selection and successful validation of the discriminant metabolite for confirmation of Korean P. ternata.

• Journal of Life Science
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• v.14 no.1
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• pp.91-97
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• 2004

As a part of our study on the improvement of anticonvulsant, here we report the synthesis of N-acyl-$\alpha$-aminosuc-cinimides 1 and N-acyl-$\alpha$-aminoglutarimides 2. (R)-Benzoic acid 4-benzyloxycarbonylamino-2-oxo-pyrrolidin-1-ylester 6a, (R)-4-nifro-benzoic acid 4-benzyloxycarbonylamino-2- oxo-pyrrolidin-1-yl ester 6b, (R) -4-nitro-benzoic acid 4-benzyloxycarbonylamino-2-oxo-pyrrolidin-1-yl ester 6c, and (R)-propionic acid 4-benzyloxycarbonylamino-2-oxo-pyrrolidin-1-yl ester 6d were synthesized from (R)-2-benzyloxy carbonylamino-succinic acid 3 as a starting meterial. (R)-(3- Benzyloxycarbonylamino-2,6-dioxo-piperidin-1-yloxy)-acetic acid methyl ester 10a, (R)-(3-benzyloxycarbonylamino-2,6-dioxo-piperidin-1-yloxy)-acetic acid ethy1 ester 10b, an d (R)-2-(3-benzyloxycarbonylamino-2,6- diox o-piperidin-1-yl oxy)-propionic acid methyl ester l0c were synthesized from (R)- 3-carbobenzyloxy-amino-glutarmic acid 7 as a starting meterial. The yield, mp, IR, $^1H-NMR,\; and^{13}C$- NMR spectra of the products 6a, 6b, 6c, 6d, 10a, l0b, l0c are summarized in footnote. The biological studies of these compounds are in progress and will be reported in future.