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

• 대한한방내과학회지
• /
• 제24권2호
• /
• pp.315-328
• /
• 2003

This study was performed to investigate the effect of Bunsimgieum on antitumor effect after sarcoma-180 cells transplantation into peritoneal cavity or left groin and immune responses on the depressed immunity induced by methotrexate in mice. The Bunsimgieum extract of 10mg/kg was orally administered 14 days for antitumor effects and 21 days for immune responses. 50% inhibitory concentration($IC_{50}$) of SUN-1, SUN-C4, and SUN-396 cancer cell, mean sunvival days and body weight of tumor bearing mice, and growth of tumor mass for antitumor effect; delayed type hypersentivity, hemagglutinin titer, hemolysis titer, rosette forming cells, natured killer cell activity, lymphocyte transformation, productivity of interleukin-2, and phagocytic activity for their immune responses were measured in ICR mice. Significance in antitumor effect is noted in the enlongation of mean life days and inhibition of tumor growth(p<0.01, respectively). Significance of immune responses is also noted in hemolysis titer, lymphocyte transfumotion, IL-2 productivity, phagocytic activity, and natural killer cell activity at E/T ratio 100:1(p<0.01, respectively). Significant in rosette cell formation was seen at dosage of 20mg/kg(p<0.01). However, Difference of body weight as antitumor effect, delayed type hypersensitivity, and hemagglutinin titer were not shown significantly. According to the above results, it could be suggested that Bunsimgieum has prominent antitumor and immunity enhancing effect.

• 고려인삼학회:학술대회논문집
• /
• 고려인삼학회 2002년도 학술대회지
• /
• pp.266-276
• /
• 2002

A red ginseng acidic polysaccharide(RGAP) with immunomodulating antitumor activities was isolated from Korean red ginseng, The molecular weight of RGAP was estimated to be 12-450 kDa by gel filtration chromatography, RGAP was found to increase survival rate and to inhibit of tumor growth significantly in a dose dependent manner in mice transplanted with tumor cells. RGAP significantly promoted nitric oxide(NO) production from peritoneal macrophages bothin vivo and in vitro. Western blot analysis exhibited a newly synthesized inducible nitric oxide synthase(iNOS) protein band in the RGAP treated group. It seems likely that immunomodulating antitumor activities of RGAP are mainly mediated by NO production of macrophage. RGAP was further purified by ultrafiltration and anion exchange chromatography on DEAE-sepharose, followed by gel filtration on Sephacryl S-300 to give an active fraction(GFP) with stronger NO production in murine macrophages. GFP increased survival rate ten times compared to RGAP in male ICR mice transplanted with sarcoma 180 and also showed more potent tumoricidal activities of natural killer cells than RGAP. Sugar $composition(mol\%)$ of GFP was found to be arabinose:rhamnose:xylose:galacturonic acid:mannose:galactose:glucose(10:9:1:25:8:20:27) by GC/MS. The results suggest that clinical trials of RGAP in immunotherapy against cancer are highly feasible.

• Plant Resources
• /
• 제3권1호
• /
• pp.1-45
• /
• 2000

To date many kinds of compounds have been obtained from plants kingdom as antineoplastic and anti-cancerous agents. However, there is no special type of compounds for cancer therapy. Various types of substances are effective for various types of cancers and tumors: for instance, alkaloids. lignans, terpenes and steroids etc. Curcumol obtained from Curcuma aromatica was tested and noticed to be effective against cancer of the uterine cervix clinically. Oridonin isolated from Rabdosia ssp. is now investigate for clinical trials in China. Moreover camptothecine isolated from Camptotheca acuminata is also antineoplastic alkaloid, but is very toxic. Chemical modification has been tried to decrease its toxicity This compound is now using as clinical agent. Harringtonin was investigated as an anticancerous drug in China. Taxol, a compound with a taxane ring isolated from the bark of Taxus brevifotia. has been demonstrated to have substantial anticancer activity in patients with solid tumors refractory standard chemotherapy. Supply of this drug has severely limited full exploration of its antineoplastic potential Some efforts are continued in National Cancer Institute(NCI) Washington for surveying various Taxus species for optimal taxol content, improvement in semi-synthesis from baccatin 111, improvement in method of extraction, and development of alternative renewable resources. Further, there are many compounds which have been reported as antineoplastic agents. On the other hand, we have screened on higher plants collected In Japan, China, Korea. Southeast Asia and South America for antineoplastic activity, which has been done using Sarcoma 180 ascites in mice, P388 Iymphocytic leukemia In mice, Chinese hamster lung V-79 cells, P388 cells and nasopharynx carcinoma(KB) cells in our laboratory, as primary screening. In this meeting, 1 will present on antitumor and cytotoxic substances of the higher plants(Rubis cordifolia, Ailanthus vilmoriniana, Aster tataricus, Taxus cuspidata var. nana, Cephalotaxus harringtonia var. drupacea, etc.) selected from above screening tests.

• 한국식품영양학회지
• /
• 제37권1호
• /
• pp.30-39
• /
• 2024

Black chestnut (BC) was obtained through aging of fresh chestnut (FC) at 80℃ for 15 days. Proximate and mineral compositions along with colors of FC and BC were evaluated. With aging, moisture contents decreased by 50%, whereas sugar contents, carbohydrate contents, and calories increased. Contents of minerals (Fe, P, Ca, Na, Mg, K) were significantly higher in FC than in BC, showing an order of Mg < Ca < P < K in both FC and BC. Using a Hunter color system, it was found that lightness (L), redness (a), and yellowness (b) values of FC were higher than those of BC. Antioxidant and cytotoxic activities of hot water and ethanol (50, 80, 100%) extracts prepared from FC and BC were evaluated. Extraction yields were lower with FC than with BC. Among water and ethanol extracts, water extract showed the highest DPPH radical scavenging activity for both FC and BC. IC₅₀ values for ABTS+ radical scavenging activities increased after aging. Cytotoxicities of FC and BC extracts were similar to each other. They were different against various cell lines (3T3, HeLa, and Sarcoma-180). These results suggest that BC could be used as a new processed food using chestnut.

• 한국식품영양과학회지
• /
• 제44권4호
• /
• pp.516-523
• /
• 2015

도라지 추출물과 그것의 분획물들(헥산, 클로로포름, 에틸아세테이트, 부탄올 및 물)의 발암물질 N-nitrosodimethylamine(NDMA)과 유전독성에 대항하는 안전성, 항돌연변이 및 항암 효과를 연구하였다. 도라지 추출물과 그것의 분획물들의 유전독성학적 안전성 평가를 위한 복귀돌연변이 시험은 S. Typhimurium TA98과 TA100의 복귀변이 집락수를 조사하는 Ames test로 수행하였다. 도라지 추출물과 그것의 분획물들은 복귀변이 집락수를 유의적으로 변화시키지 않았고, N-methyl-N'-nitro-N-nitroso-guanidine과 4-nitroquinoline 1-oxide에 의해 유발된 돌연변이에 대해 농도 의존적으로 돌연변이 억제 효과가 있었다. 도라지 추출물과 그것의 분획물들 중에 에틸아세테이트 분획물이 가장 높은 항돌연변이 효과를 나타내었다. 도라지 70% 에탄올 추출물 및 분획물들은 인간 자궁경부암세포(HeLa), 인간 간암세포(HepG2), 인간 유방암세포(MCF-7) 및 인간 폐암세포(A549) 성장 억제 효과를 나타내었고, 인간 신장정상세포(293)는 암세포보다 억제 효과가 낮았다. 더하여 in vivo에서 도라지 70% 에탄올 추출물 및 분획물의 항암 효과를 검토하기 위하여 Balb/c 마우스에 sarcoma-180 종양세포로 고형암을 유발시키면서 도라지 추출물과 그것의 분획물들의 고형암 성장 억제 효과를 알아본 결과 농도 의존적으로 고형암 성장 억제 효과를 나타냈고 도라지 에틸아세테이트 분획물이 가장 높은 억제 효과를 보였다. 그리고 도라지 에틸아세테이트 분획물은 NDMA 생성을 억제하였다. 따라서 도라지 에틸아세테이트 분획물은 항돌연변이 및 항암 효과가 있었고 현재 실험 조건에서 안전한 새로운 항암 소재 후보라는 것을 알 수 있었다.

• 대한약침학회지
• /
• 제5권2호
• /
• pp.120-136
• /
• 2002

Objectives : The purpose of this study is to investigate Acute and Subacute Toxicity, and Anti-cancer Effect of H Herbal-acupuncture on mice and rats. Methods : Balb/c mice were injected intraperitoneally with H Herbal-acupuncture for $LD_{50}$ and acute toxicity test. Sprague-Dawley rats were experimented in the same way for subacute toxicity test. H Herbal-acupuncture was injected into abdomen of mice having S-180 cancer cell line. Result : 1. During the test, $LD_{50}$ could not be counted since there was no expired subjects. 2. In an acute toxicity test, the loss of motility and reflex action was observed, but weight increased in the treatment group, compared with those in the normal group (P<0.05). 3. In an acute toxicity test of serum biochemical values of mice, glucose increased in the treatment group II while total cholesterol was increased in the all treatment groups (P<0.05). 4. In a subacute toxicity test, a little loss of motility and reflex action was observed in the treatment group. Weight of mice in the treatment group decreased on the 28th day. 5. In a subacute toxicity test, liver weight was decreased but lung weight of mice increased in the all treatment groups (P<0.05). 6. As a result of measuring Complete Blood Count test (CBC) of rat, HCT was decreased in treatments even though it was not significant, compared with the normal group (P<0.05). 7. In a serum biochemical value test of subacute toxicity, total protein and albumin decreased in the all treatment groups. Creatinine, glucose, GOT increased in the treatment group I compared with the control group. Alkaline phos-phatase decreased in treatment II group, compared with the control group (P<0.05). 8. Median survival time that was measured in the rats treated with sarcoma-180 cancer cell Median decreased in the treatment group, compared with the control group (P<0.05). 9. Natural killer cell activity showed significant reduction at 100:1 and 10:1 E/T ratio while it increased at 50:1 E/T ratio. It is inferred that there was an error in the experiment (P<0.05). 10. In an interleukin-2 productivity test, even though it decreased in lung cancer, and increased in abdomen cancer, but it was only a small difference (P<0.005). 11. After injecting B16F10 cell into a capillary vessel of C57BL/6 mice and generating metastasized lung cancer, the lung was examined with the naked eye. It was not possible to see metastasized cancer in the all groups on the seventh day but the cancer was viewed on the fourteenth day. The number and volume of metastasized cancer in the treatment group enlarged in the treatment group, compared with the control group. Conclusion : According to the results, H herbal-acupuncture took no effects in cancer.

• 대한한방종양학회지
• /
• 제9권1호
• /
• pp.1-14
• /
• 2003

Objective : Ikiyangeumhaedoc-tang(IYHT) has an effect of nourishing Yin(陰) and Jin(津), and has been used to cancer patient effectively. In order to prove the anticancer's and antimetastic effect of IYHT experimentally, studies were done. Methods : We evaluated the cytotoxic activity on HT-1080 cells as well as inhibitory effect on activity of DNA topoisomerase Ⅰ, cell adhesion, cell invasion and proliferation of HUVEC cells induced by bFGF and measured the expression of mRNA(uPA, MMP2, TIMP2), p-ERK protein, recovery effect of gap junctional intercellular communication by $H_{2}O_2$ and survival time of ICR mice bearing sacoma-180. Results : IYHT showed the inhibitory effect on DNA topoisomerase Ⅰ in the concentration of $100{\mu}g/ml,\;500{\mu}g/ml$ and the dosage-dependent inhibitory effect on the adhesion of HT-1080. The concentration of 1mg/ml of IYHT inhibited 15% of adhesion compared with control. IYHT decreased the expression of uPA, but not in MMP2, TIMP2 by RT-PCR and inhibited the expression of p-ERK effectively in the concentration of more than $500{\mu}g/ml.$ IYHT recovered the inhibited gap junctional intercellular communication by $H_{2}O_2$ to the level of 60% of normal control in the concentration of $400{\mu}g/ml$ but, did not extended the mean survival time of sarcoma 180-bearing mouse. Conclusions : It was concluded that IYHT could be applied usefully for prevention and treatment of human cancer, And also experimental study for the evaluation of molecular biological study and antimetastatic research would be recommended in the near future.

• 대한약침학회지
• /
• 제6권1호
• /
• pp.76-94
• /
• 2003

Objectives : The purpose of this study was to investigate Acute$\cdot$Subacute Toxicity and Anti-cancer Effect of K-Herbal-acupuncture in mice and rats. Methods : Balb/c mice were injected intraperitoneally with K-herbal-acupuncture for $LD_{50}$ and acute toxicity test. Sprague-Dawley rats were injected intraperitoneally with K-herbal-acupuncture for subacute toxicity test. K-Herbal-acupuncture was injected on abdomen of mice with S-180 cancer cell line. Result : 1. $LD_{50}$ of K-Herbal-acupuncture was limited $4{\times}10^{-3}$ml/kg~$2{\times}10^{-3}$ml/kg by the test. 2. In acute toxicity test, all of mice were down to the moving reflex, but the weight of mice was increased in treatment group, compared with the normal group. (P<0.05) 3. In acute toxicity test of serum biochemical values of mice, glucose was increased in treatment II group, total cholesterol was increased both treatments.(P<0.05) 4. In subacute toxicity test, the clinical signs of toxication was down to the moving reflex, but it is not severe like acute toxicity test, and observed weight loss at the treatments. 5. In subacute toxicity test, liver weight was decreased compared with the normal group. (P<0.05) 6. In subacute toxicity test of complete blood count test (CBC) of rat, HCT was decreased in treatments, compared with the normal group.(P<0.05) 7. In subacute toxicity test of serum biochemical values of rat, uric acid and triglyceride were decreased, and glucose was increased in treatment groups compared with the control group. (P<0.05) 8. Median survival time was increased about $45\%$ in treatment groups compared with the control group.(P<0.05) 9. Natural killer cell activity was increased in B16F10 lung cancer model, but it was not in sarcoma-180 abdomen cancer. 10. In interleukin-2 productivity test, treatment groups didn't show significant change in lung cancer and abdomen cancer, compared with the normal group.(P<0.005) 11. In making an examination of metastatic cancer with the naked eye, melanoma metastasized in the Lung of C57BL/6 mice. The treated group showed more Melanoma than the control in the numbers and volume. Conclusion : According to the result, K-herbal-acupuncture need further study to know the function and effect in cancer.

• 대한한의학회지
• /
• 제19권1호
• /
• pp.234-250
• /
• 1998

Bujeonghangamtang(扶正抗癌湯) has been used for cure of tumor as a traditional medicine without any experimental evidence to support the rational basis for its clinical use. This study was carroed out to evaluate the possible therapeutic or antitumoral effects of Bujeonghangamtang extract against tumor, and to carry out some mechanisms responsible for its effect. Some kinds of tumor were induced by .the typical application of 3-methylcholanthrene (MCA) or by the implantation(s.c) of malignant tumor cells such as leukemia cells(3LL cells) or sarcoma cells(Sl80 cells). Treatment of the Bujeonghangamtang water-extract (dailly 1mg/mouse, i. p.) was continued for 7 days prior to tumor induction and after that the treatment was lasted for 20 days. Against squamous cell carcinoma induced by MCA, Bujeonghangamtang decreased not only the frequency of tumor production but also the number and the weight of tumors per tumor bearing mice (TBM). Bujeongmngamtang also significantly suppressed the development of 3LL cell and S180 cell-implanted tumors in occurence-frequency and their size, and some developed tumors were regressed by the continuous treatment of Bujeonghangamtang extract into TBM. In vitro, treatment of Bujeonghangamtang extract had no effect on the growth of some kinds of cell line such as FsaII, A431 strain but significantly inhibited the proliferation of 3LL, S180 cells and augmented the DNA synthesis of mitogen-activated lymphocytes. Bujeonghangamtang also stimulated the migrative ability of leukocyte, the MIF and IL-2 production of T lymphocytes, but not IL 6 production of B cells. Bujeonghangamtang-administration to mice enhanced NK cells attivities. These results demonstrated that Bujeonghangamtang extract exhibited a significant prophylactic benefits against tumors and its antitumor activity was manifested depending on the type of tumor cells. And these results also suggested that effect of Bujeonghangamtang might be chiefly due to nonspecific enhancement of NK cell activities and cell-mediated immune responses.