• Archives of Pharmacal Research
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• 제25권2호
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• pp.158-164
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• 2002

In the course of searching immunomodulators from natural sources, the protein-bound polysaccharide, CM-Ala, has been isolated from the water extract of Chelidonium majus L. (Papaveraceae). The immunostimulatory characteristics have been investigated in several experiments such as generation of activated killer (AK) cells, proliferation of splenocytes, activation of macrophages and granulocyte macrophage-colony forming cell (GM-CFC) assay. Of the fractions obtained using Sephacryl S200 column chromatography, CM-Ala was the most effective fraction that augmented the cytotoxicity against Yac-1 tumor cells from 0.88% to 34.18% by culturing with splenocytes for 5 days. CM-Ala also enhanced nitric oxide production by two fold in peritoneal macrophages and exhibited antitumor activity. It showed mitogenic activity on both spleen cells and bone marrow cells. CM-Ala induced proliferation of splenocytes by 84 fold and increased GM-CFC numbers by 1.48 fold over than the non-treated. On the contrary, CM-Ala had cytotoxic activity to a diverse group of tumor cells. From the above results, we proposed that CM-Ala has a possibility of an effective antitumor immunostimulator.

• 한국식품영양과학회지
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• 제39권2호
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• pp.179-185
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• 2010

하이아미의 정조와 현미상태에 대해 일품벼를 대조구로 하여 항산화성분의 함량과 에탄올 추출물에 대한 in vitro 항산화활성 및 항암활성을 측정하였다. 하이아미의 정조 및 현미 추출물의 총 폴리페놀 함량은 각각 6.31 및 3.75 mg/g으로 나타났으며, 일품은 각각 5.66 및 3.47 mg/g으로 나타나 하이아미가 약간 높은 것을 알 수 있었다. 하이아미의 정조와 현미 추출물의 $\gamma$-oryzanol 함량은 각각 33.53 및 39.47 mg/100 g으로 나타났으며, 일품의 경우 각각 24.33 및 28.68 mg/100 g으로 나타나 일품에 비해 하이아미에서 높은 함량을 보이는 것으로 나타났다. 하이아미와 일품벼 정조 및 현미의 70% 에탄올 추출물에 대한 DPPH radical, hydrogen peroxide, superoxide radical 및 hydroxyl radical 소거활성을 5 mg/mL의 농도에서 측정한 결과 하이아미가 일품에 비해 높은 것으로 나타났으며, 정조 추출물이 현미 추출물보다 높은 radical 소거활성을 보이는 것으로 나타났다. 70% 에탄올 추출물에 대한 in vitro 항암활성을 측정한 결과 정조 및 현미 추출물의 억제 활성은 용량 의존적으로 증가하는 것으로 나타났으며, 특히 하이아미는 위암 및 유방암세포에 높은 활성을 보였으며, 일품은 대장암 및 간암세포에 대해 높은 활성을 보였다.

• 산업기술연구
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• 제25권B호
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• pp.241-251
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• 2005

Exopolysaccharide (CBP) from submerged culture broth of Ganoderma lucidum mycelium and the water soluble (BWS) and water insoluble (BWI) fractions of CBP were prepared by gel filtration. Antitumor activity and effects on proliferation and differenciation of human cancer cells and mouse NIH 3T3 cells were studied. Cytotoxicity test of CBP, BWS and BWI fractions on human cancer cell lines was performed by using sulforhodamine B (SRB) assay. A549 (lung carcinoma), Colo320 DM and HSR (colon carcinoma), and NIH 3T3 cells were used. BWI fraction showed the strongest cytotoxicity (maximum 20% survival) to all human cells tested. However it did not induced apoptosis. Interestingly BWI fraction did not exert cytotoxic effect on NIH 3T3 cells at low concentration of cells ($5{\times}10^4$) but strong toxic effect at high concentration of cells($5{\times}10^5$) which showed transformed morphology. These results suggest that BWI may have cancer cell specific anticancer activity. However, BWI fraction did not effect the amount of pRb and c-myc protein, which implied that BWI fraction did not act at the early stage of signal transduction pathway. CBP fraction induced differenciation of human leukemic cell line, HL-60 cells suggesting the carcinogenesis prevention of normal cell and possible induction of normalization for cancer cell.

• Asian Pacific Journal of Cancer Prevention
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• 제13권12호
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• pp.6073-6076
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• 2012

Discovery of anticancer drugs that kill or disable tumor cells in the presence of normal cells without undue toxicity is a potential challenge for therapeutic care. Several papers in the literature have emphasized the potential implications of marine products such as seaweeds which exhibit antitumor activity. Study attempts to screen the antitumor effect of Sargassum sp, against chosen cell lines such as MCF-7 (Breast cancer) and Hep-2 (Liver Cancer). Ethanol extract of Sargassum sp. was concentrated using a Soxhlet apparatus and dissolved in DMSO. In vitro cytotoxic activity of Sargassum sp at various concentrations ($100{\mu}g/ml-300{\mu}g/ml$) screened for antitumor effect against the chosen cell lines using MTT assay (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide, a yellow tetrazole). The study documented that the percentage of cell viability has been reduced with increased concentration, as evidenced by cell death. Sargassum sp extract shows potential cytotoxic activity ($P{\leq}0.05$) with $IC_{50}$ of $200{\mu}g/ml$ and $250{\mu}g/ml$ against Hep-2 and MCF-7 cell lines respectively. The ethanol fraction of Sargassum sp induced cell shrinkage, cell membrane blebbing and formation of apoptotic bodies with evidence of bioactive components as profound influencing factors for anti-tumor effects. Further research need to be explored for the successful application of Sargassum sp as a potent therapeutic tool against cancer.

• Asian Pacific Journal of Cancer Prevention
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• 제13권5호
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• pp.2015-2020
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• 2012

Oleanolic acid (OA) is a naturally occurring triterpenoid in food materials and is a component of the leaves and roots of Olea europaea, Viscum album L., Aralia chinensis L. and more than 120 other plant species. There are several reports validating its antitumor activity against different cancer cells apart from its hepatoprotective activity. However, antitumor activity against skin cancer has not beed studied well thus far. Hence the present study of effects of OA against HaCaT (immortalized keratinocyte) cells - a cell-based epithelial model system for toxicity/ethnopharmacology-based studies - was conducted. Radical scavenging activity ($DPPH{\cdot}$) and FRAP were determined spectrophotometrically. Proliferation was assessed by XTT assay at 24, 48 and 72 hrs with exposure to various concentrations (12.5-200 ${\mu}M$) of OA. Apoptotic induction potential of OA was demonstrated using a cellular DNA fragmentation ELISA method. Morphological studies were also carried out to elucidate its antitumor potential. The results revealed that OA induces apoptosis by altering cellular morphology as well as DNA integrity in HaCaT cells in a dose-dependent manner, with comparatively low cytotoxicity. The moderate toxicity observed in HaCaT cells, with induction of apoptosis, possibly suggests greater involvement of programmed-cell death-mediated mechanisms. We conclude that OA has relatively low toxicity and has the potential to induce apoptosis in HaCaT cells and hence provides a substantial and sound scientific basis for further validation studies.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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• pp.73-73
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• 1993

As part of a research program to develope 3rd generation anti tumor platinum complexes, a series of platinum complexes which have 4, 5-bis-(aminomethyl)- 1, 3-dioxolane derivatives as bidenate amine ligands, represented by the general structual formula was prepared. The R$_1$ and/or R$_2$ substituents in this series of platinum complexes can be hydrogen. alkyl, of jointly formed cyclohexane. Two Xs can be a bidenate leaving ligand such as 1, 1-cyclobutanedicarboxylate, malonate, dimethylmalonate, ethylmalonate, glycolate, L-lactate, or N-methyliminodiacetate. From based on the pharmacological and toxicological studies, we have chosen SKI 2053R, cis-malonato[(4R, 5R)-4, 5-bis(aminomethyl)-2-isopropyl-1, 3-dioxolane] platinum(II) complex (NSC D644591) as a candidate for clinical evaluation. The antitumor activity of a new anti tumor platinum complex, cis-malonato [(4R, 5R)-4, 5-bis(aminomethyl)-2-isopropyl-1, 3-dioxolane] platinum(II) (SKI 2053R, NSC D644591), was compared with those of cisplatin and carboplatin using murine tumors. We evaluated three platinum complexes against L1210/CPR, a subline of L1210 leukemia resistant to cisplatin for their abilities to overcome tumor resistance to cisplatin. The in vitro cytotoxicity of SKI 2053R to L1210 cell line was 2.5-fold less potent thann that of cisplatin, and was 10-fold more cytotoxic than that of carboplatin. SKI 2053R retained similar cytotoxic effect and anti tumor activity to L1210/CPR cell line, like the cytotoxicity of SKI 2053R to L1210 cell line, while either cisplatin or carboplatin had not property to overcome the acquired cisplatin-resistance. SKI 2053R exhibited greater or comparable antitumor activity than cisplatin or carboplatin in murine tumor models.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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• pp.74-74
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• 1993

The in vitro cytotoxicity of SKI 2053R was evaluated against human tumor cell lines along with those of cisplatin and carboplatin using MTT assay. The cell lines tested were two human lung cancer cell lines and five human stomach cancer celt lines. The level of cytotoxic effects of SKI 2053R against two human lung cancer cell lines was located between cisplatin and carboplatin. However, the cytotoxic activity of SKI 2053R against five human stomach cancer cell lines was similar to that of cisplatin. SKI 2053R is considered to be selectively cytotoxic toward human stomach cancer cell lines. We carried out pharmacokinetic and ex vivo phrmacodynamic studies of SKI 2053R in beagle dogs to predict the clinical antitumor effect of SKI2053R, comparing with those of cisplatin and carboplatin. In ex vivo pharmacodynamics which used MTT assay as bioassay on the 2 lung and 5 stomach cancer cell, mean antitumor indexes (ATIs) of SKI 2053R were highest among three compounds in both lung and stomach cancer cell lines, especially in stomach cancer cell. Much higher ATI profile and maximal inhibition rates of SKI 2053R appeared in the stomach cancer cells will give desirable advantages to clinical trial s against gastric carcinoma. The anti tumor activity and target organ toxicity of SKI 2053R were compared with those of cisplatin on stomach cancer cell line, KATO III xenografted into nude BALB/c(nu/nu) mice. All groups of cisplatin and SKI 2053R showed active tumor regression. The inhibition rates(IR) of SKI 2053R were higher than that of cisplatin on the basis of mean IR. Though the loss of body weight was observed in all groups from the first week, the SKI 2053R group recovered it soon from the third week after the initiation of treatment, maintaining the most active anti tumor activity among three groups.

• 혜화의학회지
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• 제8권1호
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• pp.403-424
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• 1999

To evaluate the antitumor activity, antimetastatic and radioprotective effects of Kamisasammaekmundongtang(KSMT), studies were done experimentally. The results were obtained as follows: 1. In cytotoxicity against P388, A549 and B16-F10, KSMT was not showed satisfiable cytotoxicity as compared with control. 2. In Inhibitory effect on activity of DNA topoisomerase I, KSMT has strong inhibitory effect. 3. The inhibitory effect on adhesion of A549 to complex extracellular matrix was significantly increased at 0.5mg/ml, 1mg/ml of KSMT. 4. The T/C% was 122 in KSMT treated group in S-180 bearing ICR mice. 5. In antiangiogenetic effect on CAM assay, inhibitory rate was 33% in KSMT treated group. 6. In pulmonary colonization assay, a number of colonies in the lungs were decreased significantly in KSMT treated group as compared with control group. 7. By FACS analysis of splenic leukocyte after exposure to radiation by linear accelerator, T-helper cell, B cell and macrophage in KSMT treated group were significantly increased while splenocytes were decreased in control group. 8. In histological changes of jejunum of $Bald{\setminus}C$ mice after exposure to radiation by linear accelerator, exclusion and fusion of villi were decreased as compared with control group. But in duodenum and ileum, exclusion and fusion of villi were not decreased as compared with control group. 9. WBC, PLT were increased in KSMT treated group as compared with control group after exposure to radiation by linear accelerator, but the increasing effect was not significant. Above results suggest that KSMT may be useful in prevention of cancer metastasis and protection from damage by radiotherapy. But the further study of KSMT would be demanded.

• 한국축산식품학회:학술대회논문집
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• 한국축산식품학회 2002년도 제30차 추계 학술대회
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• pp.174-174
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• 2002

• Archives of Pharmacal Research
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• 제25권6호
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• pp.781-785
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• 2002

A series of pyrazoloxyphenyl benzoyl urea derivatives was designed and synthesized for cytotoxic evaluation as potential antitumor agents. The synthetic compounds were evaluated for in vitro cytotoxicity against five human tumor cell lines, including A-549, SKOV-3, SK-MEL-2, XF-498 and HCT-15. Among others, compound 11 exhibited 50∼100 times greater antitumor activities than the commercial product, Cisplatin.