• 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.

• Archives of Pharmacal Research
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• 제27권9호
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• pp.893-900
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• 2004

2- or 6-Substituted BZT-N derivatives were synthesized, and their cytotoxic activity against can-cer L1210 and SNU-1 cells was examined. The antitumor action was also assessed in mice bearing S-180 cells in peritoneal cavity. In a comparison, it was found that 6-substituted BZT-N derivatives exhibited higher potencies in both bioactivities than 2-substituted BZT-N derivatives against L1210 cells in in vitro and S-180 in vitro tests exception of compound 36. Interestingly, it was observed that 2-substituted compound 36, which has methyl group at RI position, exhib-ited a better antitumor activity than 6-substituted compounds against L1210 and SNU-1 in vitro. The EDso value of 2-substituted compound 36 against L1210 was found to be comparable to the EDso value of adriamycin and was even better against the solid cancer cell line SNU-1. It was also observed that 2-substituted compound 36 showed better antitumor activity in mice bearing S-180 cells in the peritoneal cavity. The T/C (％) value of 2-substituted compound 36 was simi-lar to that of adriamycin. Quantitative structure-activity relationship (QSAR) tests reveal that the experimental E $D_{50}$ values against SNU-1 closely correlate with both the calculated HOMO ener-gies ( $E_{HOMO}$) and the measured H-NMR chemical shift of 3-H ($\delta$$_{H}$). The results suggests that a compound having higher $E_{HOMO}$ and $\delta$$_{H}$ values usually should have a lower E $D_{50}$ (SNU-1) value.lue.lue.lue.

• Archives of Pharmacal Research
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• 제23권4호
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• pp.283-287
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• 2000

A series of 2-(1-hydroxyiminoalkyl)-1,4-dimethoxy-9,10-anthraquinones (oximes) was synthesized and evaluated for cytotoxicity against L1210 cells and A549 cells. These oximes showed a greater cytotoxic activity compared to those of 2-(1-hyd roxyalkyl)-1,4-dimethoxy-9,10-anthraquinones as the hydroxyalkyl bioisosteres. The enhanced cytotoxiciy assumed to be due to the improved water solubility of the hydroxyimino group. Moreover, it was found that the cytotoxicity of the oximes decreased with elongation of alkyl groups at the side chain. All of the synthesized compounds showed higher cytotoxicity against L1210 cells than A549 cells.

• Natural Product Sciences
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• 제15권4호
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• pp.250-255
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• 2009

Seven compounds including hederagenin 3-[(O-${\alpha}$-L-rhamnopyranosyl-($1{\rightarrow}2$)-${\alpha}$-L-arabinopyranosyl) (1), $3{\beta}$-[(O-${\alpha}$-L-rhamnopyranosyl-($1{\rightarrow}2$)-${\alpha}$-L-arabinopyranosyl)oxy]olean-12-en-28-oic acid (2), caffeic acid methyl ester (3), ferulic acid (4), orebiusin A (5), latifonicinin C (6) and 5-(hydroxymethyl)-2-furfuraldehyde (7) were isolated from the ethyl acetate fraction of the roots of Pulsatilla koreana. Their chemical structures were established based on physicochemical and spectroscopic data analyses. All isolates were investigated for their cytotoxic activity against cancer cell lines. Among them, compound 1 showed inhibitory activity against A549, COLO 205, and L1210 cancer cell lines with $IC_{50}$ values of 15.8, 36.5, and 22.8 ${\mu}g$/mL, respectively.

• Biomolecules & Therapeutics
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• 제5권2호
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• pp.215-221
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• 1997

In an effort to screen new selective antitumor agents from the broth of soil microorganism, cytotoxicity oriented screening was performed against tumor cells and 3 compounds (Compound 1, 2 and 3) were isolated from Sreptomyces parvullus ISP 5048 and their chemical structures were determined. Among these compounds, Compound 2 showed the highest cytotoxicity against P388Dl and L1210. While the $IC_{50}$/ values of compound 2 against P388Dl and L1210 were 0.073$\mu$g/ml and 0.07$\mu$g/ml, respectively, and the $IC_{50}$/ value of Compound 3 was 0.17$\mu$g/ml against human lung cancer cells, A549, the cytotoxicity of Compound 2 and 3 against normal cell line, Vero E6 cell was about 4- and 8-fold lower than that of adriamycin. Based on the chemical analysis data, Compound 3 was octacosamicine A, a known antibiotic, which was reported by Dobasih et al. (1988). Taken together the results demonstrated that Compound 2 and Compound 3 has the possibility to be developed as antitumor agent because of its potent cytotoxicity as well as high selectivity against various cancer cell lines.

• 한국약용작물학회지
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• 제13권2호
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• pp.80-84
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• 2005

Five known anthraquinones, physcion (1), I-O-methylemodin (2), emodin (3), $physcion-8-O-{\beta},-D-glucopyranoside$ (5), $emodin-8-O-{\beta},-D-glucopyranoside$ (6) and two known stilbenes, trans-resveratrol (4), $trans-resveratrol-3-O-{\beta},-D-glucopyranoside$ (7) were isolated from MeOH extract of Reynoutria sachalinensis (Polygonaceae). All structures were unambiguously established by 1D and 2D NMR and MS data and the compounds were evaluated for their cytotoxicity against L1210, HL-60, BI6F10 tumor cell lines in MTT assay. Among the compounds, trans-resveratrol (4) exhibited significant cytotoxic activity with $IC_{50}$ values of 9.2, 6.7 and $9.8\;{\mu}g/ml$, against the test cell lines respectively, but compounds 1-3 exhibited the moderate cytotoxic activity.

• 한국식품조리과학회지
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• 제21권3호
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• pp.311-318
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• 2005

Echinacea angustifolia의 부위별(꽃봉오리, 잎, 줄기 및 뿌리) 메탄을 추출물의 암세포(HepG2, 3LL, HL60, L1210)를 대상으로 한 항암 활성과 전자공여능을 검색한 결과는 다음과 같다. 1. 에키네시아 메탄을 추출물의 간암세포인 HepG2 cell 대한 MTT assay는 농도의존적으로 세포독성 효과가 증가하였으며, 인간유래 백혈암세포인 HL60 cell의 경우에 잎과 뿌리 추출물은 저농도에서부터 독성효과가 컸고, 줄기와 꽃봉오리는 저농도에서는 독성효과가 낮았으나 고농도로 갈수록 독성효과가 커짐을 알 수 있었다 폐암세포인 3LL cell과 마우스 유래 백혈암세포인 L1210 cell에 대한 경우는 세포독성효과가 없었다. 2. Hemacytometer에 의한 HepG2 cell의 암세포 성장에 미치는 효과는 배양기간이 증가함에 따라 농도의존적으로 증식억제 효과가 증가되었다. 3. HepG2 세포주의 형태학적 변화에서 대조군은 암세포가 조밀하게 중첩되어 증식되었으나 시료를 0.5 mg/mL 이상의 농도로 첨가하였을 때 세포의 결속력이 감소되어 세포주위가 흐트러지고 세포가 사멸된 것을 관찰 할 수가 있었다. 4. 전자공여능의 수준은 부위에 따라 최고의 EDA를 나타내는 농도가 달랐으며, 뿌리와 줄기부위는 저농도에서도 매우 높은 전자공여능을 나타내었다.

• 한국식품과학회지
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• 제30권1호
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• pp.13-21
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• 1998

도라지의 물과 석유에테르 추출물의 세포 증식 억제효과를 mouse DBA/2 strain유래의 백혈병성 임파모세포인 L1210과 인체 결장 암세포인 HCT-48 및 직장암세포인 HRT-18를 대상으로 분석하였다. 수용성 추출물보다는 석유에텔 추출물이 모든 항암세포에 대하여 현저히 높은 항암효과를 나타내었다. 도라지 석유에테르 추출물을 실리카겔 컬럼크로마토그라피에서 석유에테르과 에틸에테르 혼합을(7:3)로 얻은 분획은 더욱 높은 활성을 나타냈으며 L1210에서는 0.3mg/mL, HCT-48는 1.2mg/mL의 농도에서 대조군에 비해 -99%, -55%의 증식억제효과를 보였다.

• Natural Product Sciences
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• 제1권1호
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• pp.43-49
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• 1995

Two cucurbitane-compounds were isolated from the roots of Bryonia alba L. and the chemical structures were established as 19-norlanost-5-ene-3,1l,22-trione-$2{\beta}$, $16{\alpha}$,$20{\beta}$,25-tetrahydroxy-9-methyl (23,24-dihydrocucurbitacin D) and 2-O-${\alpha}$-D-glucopyranosyl 19-norlanost-5-ene-3,11,22-trione-$2{\beta}$,$16{\alpha}$,$20{\beta}$,25-tetrahydroxy-9-methyl (arvenin IV), respectively, on the basis of chemical and spectral methods. Both of the compounds showed cytotoxic activity against cancer cell lines, A549, SK-MEL-2, COLO 205 and L1210.

• 약학회지
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• 제40권2호
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• pp.117-125
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• 1996

3'-Deamino-3-hydroxy-4'-fluoro- or 3'-deamino-3'-hydroxy-4'-azido-daunorubicin(6,8) and -doxorubicin(7,9) have been synthesized, respectively. Compounds 7,8 and 9 were mo re cytotoxic than daunorubicin(1) and doxorubicin(2) against L1210 murine leukemic cell in vitro. When administered intraperitoneally for 9 days starting 1 day after tumor inoculation, compounds 7(T/C 605%) and 9(T/C 488%) showed significant antitumor activity for ip-inoculuated L1210 murine leukemia at wide range of doses.