• Archives of Pharmacal Research
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• 제24권6호
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• pp.524-526
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• 2001

Four prostate-type triterpenes were isolated from a methanol extract of Alismatis Rhizoma by bioassay-guided isolation using in vitro cytotoxic assay. The compounds were identified as alisol B 23-acetate (1), alisol C 23-acetate (2), alisol B (3), alisol A 24-acetate (4) by spectroscopic methods. Amongst the compounds, alisol B (3) showed significant cytotoxicity against SK-OV3, B16-F10, and HT1080 cancer cell lines with $ED_50$ values of 7.5, 7.5, $4.9\mu\textrm{g}/ml$, respectively.

• Archives of Pharmacal Research
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• 제27권5호
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• pp.478-484
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• 2004

The novel 1-(1-benzoylindoline-5-sulfonyl)-4-phenyl-4,5-dihydroimidazolones 2 shows highly potent and broad cytotoxicities. Their cytotoxicities against human lung carcinoma A549, human chronic myelogenous leukemia K562, and human ovarian adenocarcinoma SK-OV-3 are compatible with doxorubicin. Compound 2p (1-[(4-aminobenzoyl)indoline-5-sulfonyl])-4-phenyl-4,5-dihydroimidazolone) exhibits a cytotoxicity that is far more potent than doxorubicin and also exhibits highly effective antitumour activities against murine (3LL, Colon 26) and human xenograft (NCI-H23, SW620) tumor models.

• 동의생리병리학회지
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• 제16권3호
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• pp.452-457
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• 2002

Galla Rhois is a gallnut of Rhus javanica Linne used for treatment of diarrhea, hemorrhage, cough, leukorrhea and toxic tumor etc in oriental medicine. For the evaluation of antitumor effect of Galla Rhois, activity based fractionation was done. We isolated an effective compound and identified 1,2,3,4,6-penta-O-galloyl-β-D-glucose(PGG) by photometric analysis such as NMR and MASS. Then, we studied the angiogenic activity of PGG. It showed a cytotoxicity against SK-OV-3, SK-OV-3, HT1080 with IC/sub 50/ of 50 ug/ml approximately. It also effectively inhibited proliferation of HUVEC cells treated by bFGF to 30% of control at 20 ug/ml and cell migration to 80% at 10 ug in a dose dependent fashion. Tube formation of HUVEC cells on matrigel was effectively suppressed from 2.5 ug/ml of concentration by PGG. Moreover, it effectively recovered the dysfunction of gap junctional intercellular communication in WB-F344 rat liver epithelial cells caused by hydrogen peroxide at 4 ug/ml suggesting it potently can inhibit tumor promotion. Taken together, it indicates 1,2,3,4,6-penta-O-galloyl- β -D-glucose has antiangiogenic activity.

• 대한약리학회지
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• 제31권1호
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• pp.103-114
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• 1995

일부 malignant tumor에 Pt-complex의 일상 응용 과정에서 신장독성등의 심한 부작용이 문제점으로 지적되고 있다. 이 연구에서는 기존의 cisplatin보다 항암효과는 우수하면서, 부작용을 감소시킨 새로운 Pt-complex의 개발에 역점을 두었다. 본 연구에서 합성한 Pt(Ⅱ) complex는 carrier ligand로서 1,2-diaminocyclohexane(dach)을 사용하였고, leaving group으로는 diophosphine류인 1,2-bisdiphenylphosphinoethane(DPPE)을 도입하였으며, 물에 대한 용해도를 높이기 위해 dinitrate로 만들었다. 새로이 합성한 [Pt(Ⅱ)(trans-d-dach)(DPPE)]$(NO_3)_2$는 원소 분석, IR 및 $^{13}C-NMR$ 분석 data에 의하여 위의 물질임이 확인되었다. MTT assay method에 의한 항암활성 연구를 통하여 P-388, L-1210 lymphocytic leukemia cell과 SK-OV3 난소암세포에서 항암효과가 인정되었으며, 이 항암효과는 대조 약물로 사용된 cisplatin과 유사하였다. 토끼의 신세뇨관 세포와 인체의 신피질 세포를 이용한 cytotoxity 및 thymidine 섭취율과 인체 신피질 조직 배양을 이용한 glucose consumption 실험을 통하여 모두 cisplatin보다 신장독성이 현저히 감소되었다. 이상의 결과로 보아 Pt(Ⅱ)complexes는 carrier ligand와 leaving group의 선택에 따라 항암활성의 증가와 신독성의 감소를 일으키는 요인으로 보여지며, 이 연구에서 만들어진 Pt(Ⅱ)complex는 앞으로 다각적인 검토를 거쳐 새로운 항암화학요법제로 개발될 가능성이 있을 것으로 생각된다.

• 생약학회지
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• 제31권1호
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• pp.77-81
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• 2000

The MeOH extract of Notopterygium incisum showed a strong cytotoxicity against B16 murine melanoma cell line. From this extract three furanocoumarins including bergamottin, isoimperatorin, notopterol and one polyacetylenic compound (falcarindiol) together with one phenylpropanoid (caffeic acid methyl ester) and one triterpenoid (pregnenolone) were isolated. The isolated compounds were evaluated for cytotoxic activity against four kinds of cancer cell lines, e.g. P388 (murine lymphocytic leukemia), B16 (murine melanoma), A549 (human lung carcinoma) and SK-OV-3 (human ovarian cancer). Among the isolates, falcarindiol and caffeic acid methyl ester expressed a significant antiproliferative activity against all tested cell lines.

• Archives of Pharmacal Research
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• 제23권5호
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• pp.450-454
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• 2000

Eight 2-alkylaminosubstituted 5,8-dimethoxy-4-methylquinolines and nine 2-alkylaminosub-stituted or 2,6-disubstituted 4-methylquinoline-5,8-diones were synthesized and evaluated in vitro cytotoxicity against four human cancer cell lines (HOP62, SK-OV-3, HCT15 and SF295).

• Archives of Pharmacal Research
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• 제29권4호
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• pp.276-281
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• 2006

A series of 8-alkyl-and 8-aryl-8,9-dihydro-7H-isoindolo[5,6-g]quinoxaline-7,9-diones were synthesized using sultine chemistry as a key step in good yield. These compounds were evaluated for their in vitro cytotoxicity against six human cancer cell lines (HCT15, SK-OV-3, A549, SNB19, MCF7 and MCF7/ADR).

• Archives of Pharmacal Research
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• 제25권4호
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• pp.421-427
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• 2002

For probing the importance of planarity of imidazolidinone motif of 4-phenyl-1-(N-acylindoline-5-sulfonyl)imidazolidinones 1 for their cytotoxicity, 4-phenyl-1-(N-acylindoline-5-sulfonyl)[1,2,5]thiadiazolidine-1,1-dioxides 2 were prepared and their cytotoxicity were measured against human lung carcinoma (A549), human colon carcinoma (COLO205), human ovarian cancer (SK-OV-3), human leukemic cancer (K562), and murine colon adenocarcinoma (Colon26) cell lines in vitro. Although only carbonyl moiety of imidazolidinone ring was replaced with sulfonyl group, compounds 2 do not show any activity against all five cancer cell lines unlike 1. Therefore the planarity of imidazolidinone ring of 1 should be an important factor for their cytotoxic activity.

• 한국식품과학회지
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• 제37권1호
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• pp.108-112
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• 2005

본 연구는 폐기되는 차나무 열매를 이용하여 향균활성과 항종양활성을 비교하고 이용가능성에 대하여 탐색하고자 하였다. 항균활성과 항종양활성을 알아보기 위하여 70% 에탄올과 물 추출물의 활성을 측정하였다. 항균활성은 식중독균과 몇 종의 병원균, 효모, 곰팡이 등 17균주에 대하여 추정하였고, 항종양 활성은 6종류의 인체 암세포주, 1종류의 정상세포주에 대하여 조사하였다. 차나무 잎, 종자와 과피의 항균활성을 비교한 결과는 종자의 70% 에탄올과 물 추출물에서 효모에 대하여 항균활성이 높게 나타났다. 특히, candida albicans, Cryptococcus neoformans에 대하여 항균활성을 보였다. 종자 물 추출물을 $80,\;100^{\circ}C$에서 30분, $121^{\circ}C$에서 15분간 열처리 후 항균활성을 검색한 결과 가열온도에 따른 차이는 크게 나타나지 않았다. 항종양 활성을 검색하기 위하여 MTI assay를 통해 활성을 측정하였다. 과피 추출물에서 전혀 활성이 없었지만 종자 추출물에서는 큰 활성을 나타내었다. 극성용매인 70% 에탄올과 물 추출물의 종양세포 증식억제효과가 높게 나타났으며 그중에서 물 추출물이 70% 에탄올 추출물 보다 높게 항종양 활성이 나타났다. 차나무 종자로부터 추출한 활성물질의 종양세포와 정상 세포에 대한 세포독성을 MTT assay로 비교한 결과 $50{\mu}g/mL$의 농도에서 난소암 세포인 SK-OV-3는 70%의 억제율을 나타낸 반면 정상세포에서는 10% 미만으로 나타나 정상세포보다 종양세포에 대하여 보다 큰 선택 독성을 나타내는 것으로 보인다.

• Archives of Pharmacal Research
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• 제19권4호
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• pp.286-291
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• 1996

Phenolic compounds are prevalent as toxins or environmental pollutants, but they are also widely used as drugs for various purpose including anticancer agent. A novel biphenolic compound, bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methane (GERI-BPO02-A) was isolated from the fermentation broth of Aspergillus fumigatus F93 previously, and it has revealed cytotoxicity against human solid tumor cells. Its effective doses that cause 50% inhibition of cell growth in vitro against non-small cell lung cancer cell A549, ovarian cancer cell SK-OV-3, skin cancer cell SK-MEL-2 and central nerve system cancer cell XF498 were 8.24, 10.60, 8.83, $9.85\mug/ml$ respectively. GERI-BPO02-A has also revealed cytotoxicity against P-glycoproteinexpressed human colon cancer cell HCT15 and its multidrug-resistant subline HCT15/CL02, and its cytotoxicity was not affected by P-glycoprotein. We have also tested cytotoxicities of structurally related compounds of GERI-BPO02-A such as diphenylmethane, 1,1-bis(3,4dimethylphenyl)ethane, 2,2-diphenylpropane, 2-benzylpyridine, 3-benzylpyridine, $4,4^I-di-tert-butylphenyl$, bibenzyl, $2,2^I-dimethylbibenzyl$, cis-stilbene, trans-stilbene, 3-tert-butyl-4-hydroxy-5-methylphenyisulfide, sulfadiazine and sulfisomidine for studying of structure and activity relationship, and from these data we could suppose that hydroxyl group of GERI-BPO02A conducted important role in its cytotoxicity.