• 대한본초학회지
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• 제21권1호
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• pp.101-107
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• 2006

Objectives : It is well known that hexavalent chromium has toxic effect on normal cells. Recently, toxic effect of hexavalent chromium is diminished by the some extracts derived from herbs or plants. But, the toxic or protective mechanism of hexavalent chromium is well unknown. This study was performed to examine the protective effect of poncirin against $Na_2Cr_2O_7$-induced cytotoxicity on NIH3T3 fibroblasts. Methods : The protective effect of the cytotoxicity induced by $Na_2Cr_2O_7$ was measured by the cell viability after NIH3T3 fibroblasts were cultured with or without $Na_2Cr_2O_7$ for 48 hours. Antitoxic effects of poncirin on the cytotoxicity induced by $Na_2Cr_2O_7$ were examined by colorimetric assays such as MTT or XTT assay. Results : $Na_2Cr_2O_7$ decreased cell viability by the decreased absorbance in MTT or XTT assay, but, the poncirin increased cell viability which was decreased by $Na_2Cr_2O_7$-induced cytotoxicity on NIH3T3 fibroblasts. Conclusion : These results suggest that $Na_2Cr_2O_7$ showed cytotoxicity effect on NIH3T3 fibroblasts by the decrease of cell viavility, and poncirin was effective in the protection of $Na_2Cr_2O_7$-induced cytotoxicity in these cultures.

• Journal of Pharmaceutical Investigation
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• 제31권2호
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• pp.113-117
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• 2001

CKD602, a camptothecin derivative, is a synthetic and water-soluble anticancer agent possessing of topoisomerase I inhibiting activity. DPPC and DSPE-PEG liposomal formulations entrapped with CKD602 were developed. DSPE-PEG liposome, or PEGylated liposome, encapsulating CKD602 composed of dipalmitoylphosphatidylcholine (DPPC), cholesterol and distearoyl-N-monoethoxy poly (ethyleneglycol) succinylphosphatidylethanolamine $(DSPE-PEG_{2000})$ (22:11:2) was prepared by reverse-phase evaporation method. Formed liposomes were characterized in terms of the morphology, size and encapsulation efficiency. To elucidate the in vitro stability, PEGylated liposome was incubated in human plasma, and the adsorbed proteins onto the surface of liposomes were applied to the SDS-PAGE. In vitro cytotoxicity of CKD602 encapsulated in PEGylated liposome was studied in human cervical cancer cell line (HeLa). CKD602 in PEGylated liposome was found to be 40-fold more effective $(IC_{50}=1\;nM)$ than free CKD602 $(IC_{50}=40\;nM)$ in inhibiting the growth of HeLa cells in vitro.

• 생명과학회지
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• 제23권11호
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• pp.1381-1387
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• 2013

국내에서 식품으로 사용되고 있는 국화과 식물인 곤달비(Ligularia stenocephala) 잎과 뿌리의 생물활성을 과학적으로 검증하기 위하여 각 추출물에 대하여 항산화 활성 및 세포독성을 in vitro에서, 간보호 효과, 알코올 해독작용 및 기억증진 효능 등을 in vivo에서 평가하였으며 잎의 독특한 향기성분을 GC-MS로 분석하였다. 지질과산화 억제효과는 잎(20.4% 억제율)이 뿌리 보다 좋았으며, 유해 라디칼의 일종인 superoxide anion은 뿌리에서 생성 억제효과가 더 좋았고, DPPH 소거활성은 잎과 뿌리 모두 77~79%로 매우 뛰어났다. 사염화탄소로 유발된 급성 간독성 개선효과를 AST와 ALT 효소활성도를 지표로 확인한 결과, 잎의 ALT 억제활성이 대조군에 비해 약 78% 정도 감소하였으며 알코올을 투여한 mouse의 혈중 알코올 농도는 잎추출물 투여시 약 60% 가량 유의성 있게 감소되어 효과를 인정할 수 있었다. 세포독성은 뿌리에서 비교적 강하게 나타났는데, 흑색종의 경우, $IC_{50}=40.14mg/ml$이었으며, 잎의 세포독성은 비교적 약하였다. 기억증진 효과를 동물모델을 이용한 수동회피시험법으로 평가한 결과, 잎과 뿌리 모두 scopolamine에 의해 유도된 기억력 감소를 80% 이상 향상시킨 것으로 조사되었다. 곤달비 잎의 n-헥산 추출물을 GC-MS로 분석한 결과, 독특한 향기는 주로 terpene 화합물에서 유래되는 것으로 추정되었다.

• BMB Reports
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• 제31권6호
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• pp.560-564
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• 1998

Echinomycin-7 is an echinomycin derivative, Smethylated sulfonium perchlorate of echinomycin. We studied the in vitro cytotoxicity and in vivo antitumor activity of echinomycin-7 against P388 leukemia cells and compared the results with echinomycin. With respect to the cytotoxic effects, echinomycin-7 had cell line-dependent $IC_{50}$ values while echinomycin had similar values to several tumor cell lines. Also, in vivo antitumor activities were observed in tumor-bearing mice treated with both agents, which showed that echinomycin-7 had a broad therapeutic dose range. We also observed the apoptosis on leukemia cells treated with echinomycin-7 which exihibited the ladder pattern of DNA on electrophoresis. In addition to apoptosis, echinomycin-7 arrested $G_1/S$ phases of the cell cycle at the same time. We then examined the signaling pathway of echinomycin-7-induced apoptosis and showed that ERK of the MAP kinase family was activated and translocated into the nucleus by echinomycin-7 stimulation. This study suggests that echinomycin-7 acts as an antitumor agent through in vitro cytotoxicity and has in vivo antitumor activity against leukemia cells, and that the echinomycin-7- induced apoptosis might involve signal transduction via MAP kinases.

• Toxicological Research
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• 제16권1호
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• pp.77-82
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• 2000

This study was conducted to assess a possible alternative method as replacements for in vivo test. The human fibroblasts were exposed to several photoxic chemicals (promethazine, neutral red, chlortetracyclone, amiodatone, bithional, 8-methyooxypsorale) and non-phototoxi substance, ammonium laureth sulfate and irradiatied with 5 J/$cm^2$ of UVA (3320~420nm). The cell viability was measured by NRU (neutral red uptake) assay. The photoxic potential of test chemicals in the NRU PT (phototoxicity test) was assessed by determining the PIF (photoirritancy Factor) by using a cut-off value of 5. The NRU PT responses of most chemicals showed a close agreement with in vivo response except bithinol. There was a relatively good agreement between in vitro NRU assay and in vivo data. These results suggest that NRU assay using fibroblast could be used to predict the phototoxicity.

• 약학회지
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• 제53권1호
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• pp.41-44
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• 2009

A series of 2-alkyl-2,3-dihydro-1H-2-azacyclopenta[b]anthracene-5,10-diones ($3a{\sim}h$) were synthesized and evaluated in vitro cytotoxicity against colon cancer cell lines (HCT116 and SW620) and nuroblastoma cell lines (SK-N-SH and SK-N-MC). Among them, compound 3f showed significant cytotoxic activity ($IC_{50}$ against SK-N-SH; $14.8{\mu}M$, $IC_{50}$ against SK-N-MC; $11.3{\mu}M$).

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1997년도 춘계학술대회
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• pp.111-111
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• 1997

As part of a drug discovery program to develope more effective platinum-based anticancer drugs, a series of platinum complexes trans-diaminocyclohexane platinum bi sdiphenylphosphino - ethane ( KHPC- 002) cis-diaminocyclohexane platinum bi sdiphenylphosphino - ethane ( KHPC- 006) has been evaluated in vitro against 4 human carcinoma cell lines with those of cisplatin using a tetrazolium-based colorimetric assay (MTT assay). The cell lines were two human bladder carcinoma cell lines, HT-1197 and HT-1376, human colon carcinoma cell line, HCT-116, and prostate cancer cell line DU-145. in vitro cytotoxic potential of each platinum complex was expressed as the cytotoxicity index (Cl, %).

• Macromolecular Research
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• 제16권6호
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• pp.510-516
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• 2008

New antitumor active polymers, poly(methacryloyl-2-oxy-1,2,3-propanetricarboxylic acid-co-exo-3,6-epoxy-l,2,3,6-tetrahydrophthalic acid) [poly(MTCA-co-ETAc)], poly(methacryloyl-2-oxy-l,2,3-propanetricarboxylic acid-co-hydrogen ethyl-exo-3,6-epoxy-l,2,3,6-tetrahydrophthalate) [poly(MTCA-co-HEET)], and poly(methacryloyl-2-oxy-l,2,3-propanetricarboxylic acid-co-a-ethoxy-exo-3,6-epoxy-1,2,3,6-tetrahydrophthaloyl-5-fluorouracil) [poly(MTCA-co-EETFU)] were synthesized and characterized. Their antitumor activity, inhibition of DNA replication and antiangiogenesis were examined. The structures of the polymers were identified by FT-IR, $^1H$ and $^{13}C$-NMR spectroscopy. The number average molecular weights of the fractionated polymers determined by GPC ranged from 9,400 to 14,900, and polydispersity indices were less than 1.7. The in vitro cytotoxicity of these polymers was determined and their antitumor activity was evaluated. The $IC_{50}$ values (the drug concentration at inhibition of 50% tumor growth) indicated that the synthesized polymers were much better inhibitors of cancer cells and showed lower cytotoxicity than the free 5-FU. The in vivo antitumor activity of the conjugates was examined using mice bearing the sarcoma 180 tumor cell line. The life spans (TIC) of the mice treated with the conjugates were higher than those treated with the free 5-FU. In addition, the synthesized conjugates showed excellent antiangiogenic activity based on an embryo chorioallantoic membrane assay.

• 대한수의학회지
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• 제33권4호
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• pp.701-710
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• 1993

The pine needles, Pinus densiflow Sieb. et Zucc., which is a feed for goats showing a low incidence rate of cancer were evaluated to confirm the potent anticancer effects, with or without several conventional anticancer drugs. The pine needles collected from Mt. Buk-Han located near Seoul were extracted with 95% methanol and methand and concentrated. From the methanol extract, SOM-A, was extracted dichlormethane and SOM-B was extracted with ethyl acetate. SOM-C was extracted with distilled water. These extracts were tested for their antitumor activities in vitro and in vivo. Among them, SOM-A and SOM-C exhibited potent antitumor activities described as belows. 1. The cytotoxic effects of SOM-A and SOM-C were examined against in vitro cultured murine and humman tumor cells. SOM-A showed strong cytotoxicity against human tumor cell lines and SOM-C showed strong cytotoxicity against murine tumor cell lines tested. 2. The antitumor effects of SOM-A and SOM-C were examined against P388 and L1210 of mouse ascitic tumors. The highest mean survival time(MST) ration was 151%(P388) for SOM-C(90mg/kg). 3. To compare the antitumor effects of SOM-A, SOM-B, and SOM-C against solid tumors, S-180 and Ehrlich carcinoma were implanted subcutaneously to mice on Day O. The drugs were given intraperitoneally to mice once a day on Days 1-20, and the tumor weights were measured on Day 21. SOM-A showed inhibition of tumor growth more than 50% in the experiment on S-180 and Ehrlich, and SOM-C also markedly inhibited tumor growth. However, SOM-B had no effect. 4. SOM-C combined with ${\alpha}$-interferon and SOM-C combined with Mitomycin-C enhanced the antitumor activities against murine ascitic tumors P388 leukemia.

• 생약학회지
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• 제27권1호
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• pp.42-46
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• 1996

The medicinal formula, Kilkyungtang (KKT) and two modified Kilkyungtangs (KKT-1 and KKT-2), which were supplemented by the additional crude drug, Houttuyniae herba (KKT-1), and Oldenlandiae diffusae herba (KKT-2) to KKT, had been applied widely as decoctions for the treatment of malignant tumors. Cytotoxic activities against two tumor cell lines, A549 and $B16-F_0$ were investigated. However, none of them were found to exhibit significant cytotoxicity upon tested tumor cells below the concentration of $1000{\mu}g/ml$. However, cytotoxic activities of three reputed antitumor agents, i.e., mitomycin C (MMC), cisplatin (CPT) and 5-fluorouracil (5-FU) was significantly potentiated by the combined treatment of them with KKT, KKT-1 and KKT-2 respectively, especially against A549 (human non small cell lung adenocarcinoma), in vitro.