• 대한화학회지
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• 제55권4호
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• pp.719-722
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• 2011

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.188.1-188.1
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• 2003

The antiparasitic agent apicidin, which was recently isolated from cultures of Fusarium Pallidoroseum, belongs to a rare group of cyclictetrapeptide fungal metabolites. Apicidin inhibits protozoal HDAC and is orally active against Plasmodium berghei malaria in mice. The biological activity of apicidin appears to be attributable to inhibition of apicomplexan HDAC at low nanomolar concentrations. In the present, we have worked about the synthesis of new apicidin derivatives and discovered that apicidin and some derivatives have mild antitumor activity. (omiited)

• 대한약학회:학술대회논문집
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• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
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• pp.187.2-187.2
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• 2001

• 생약학회지
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• 제28권4호
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• pp.209-214
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• 1997

This study was carried out to find new antitumor agents from plant resource. Three cytotoxic agents were isolated from the root of Dictamnus albus by hexane extraction, silica gel column chromatography and HPLC. They were identified to be dictamnine $(C_{12}H_9NO_2)$, preskimmianine $(C_{17}H_{21}NO_4)$ and fraxinellone $(C_{14}H_{16}O_3)$ on the basis of spectroscopic evidences. In this study, it was newly found that these compounds possess a cytotoxic activity against lung lymphoma L1210 cell line. Among them. Preskimmianine was the most potent against the lymphoma L1210 with a $IC_{50}$ of $3.125\;{\mu}g/ml\;(10.3\;{\mu}M)$. Toxicity of preskimmianine against normal Iymphocyte was observed at the concentration of $50\;{\mu}g/ml\;(165\;{mu}M)$. These results support the pharmacological role of D. albus, a herb known as Paeksun in Korea and used as an anticancer agent in folk medicine.

• Journal of Microbiology and Biotechnology
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• 제15권5호
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• pp.1140-1145
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• 2005

MJM383, a rare actinomycete sp. strain originated from Chinese soils, was isolated through an antimicrobial screening system. The analysis of 16S rDNA sequences and biochemical characterization determined the strain to belong to genus Kitasatospora. Both NMR and ESI mass data of its purified bioactive compounds revealed Kitasatospora sp. MJM383 to produce two antitumor agents, streptonigrin and oxopropaline G, which have been known to be produced from Streptomyces species. This is the first report to demonstrate the presence of antitumor agents produced by genus Kitasatospora.

• Archives of Pharmacal Research
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• 제27권5호
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• pp.471-477
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• 2004

In this study, a series of 4-amino-5-cyano-3-substituted-2,3-dihydrothiazol-2-thiones (1a-c), as well as their triazolo and triazinopyrimidine derivatives such as 8-substituted-3-benzyl-5-meth-ylthiazolo[5,4-e][1,2,4] triazolo[1,5-c]pyrimidin-2-thiones (4-6, 10) and 3-benzyl-5-methyl thiazolo[5,4-e]pyrimidino[3,4-b][1,2,4]triazin-2-thiones (7a-b) were prepared as potential antimicrobial and antitumor agents. Some of the tested compounds showed promising antimicrobial activity and non of them showed any appreciable antitumor activity.

• 한국자원식물학회지
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• 제5권2호
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• pp.73-84
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• 1992

Many types of compounds have been isolated from higher plants till now, that is, alkaloids, terpenes, lignans, steroids and so on. One of them, named as RA series Cyclic hexapeptides isolated from Rubia akane and R. cordijofia also have strong antineoplastic activity against various types of tumors. Till now 10 kinds ofRA series compounds were isolated and named as RA - I, II, III, IV, V, VI, VII, VIII, IX and X. Moreover,monogl-ucoside of RA - V newly Isolated from same plant. Many kinds of derivatives including natural RAcompounds were tested for QSAR, and one of them, RA - VII was screened up as a most suitable substance asan antitumor agent. RA - VII(=RA-700) has strong cytotoxic activity against KB cells, P388 Iymphocyticleukemia and MM2 mammary carcinoma cells. RA - VII has been under investigation for Phase I clinical trials.

• 한국자원식물학회지
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• 제5권2호
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• pp.95-103
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• 1992

Present anticancer drugs in the clinical side have not showed a conclusive effect of the chemotherapy for cancer patients. In order to find much more efficient antitumor agents fromnatural resources, various screening methods vivo and in vitro have been developed by manyresearchers. The intention of this paper is to provide an outline of some background on the tumorsystem in drug development of natural products, to review some screening programs for theevaluation of antitumor activity and to introduce the practical procedures of some antitumorscreening methods in vivo and in vitro. At the end of this paper, the current literatures related toantitumor natural products from higher plants at our laboratory are described.Key words'anticancer drugs, screening methods.

• Archives of Pharmacal Research
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• 제22권6호
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• pp.575-578
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• 1999

Derivatives of elema-1,3-diene were synthesized in several steps as polar analogs of $\beta$-elemene, antitumor agent under clinical phase. The lactone ring of compound 1 was opened by LiAlH4 to give diol 2 which was selectively protected by TBDPSCI. After acetylation of the secondary alcohol, the acetylated product was ozonolyzed and reduced to give elemene derivative 4 which was converted to diolefin 8 via selenides subsequent deprotection by tetrabutylammonium fluoride gave two compounds 9, 10.

• 동의생리병리학회지
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• 제20권5호
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• pp.1196-1199
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• 2006

Tripterygium regelii SPRAGUE is distributed in Korea and Northern China. This extract has been used as a herb medicine, especially antiparasitic, anti-inflammatory and detoxifying agent in East asia. During our research to develop new antitumor agents from natural products, Dichlorornethane (CH$_2$Cl$_2$) extract of Tripterygium regelii SPRAGUE (DTR) showed the potent apoptotic effects in A-549 lung cancer, HeLa-3 cervical cancer, SKMEL-2 melanoma cells in a dose-dependent manner. in order to purify major compounds from DTR, column chromatography was carried out gradually. Silica gel and RP-18 column chromatography for active fractions led to the isolation of a compound. The compound determined by 1 H-NMR was turned out to De Celastrol known to have antitumor activity.