• Title/Summary/Keyword: and Antitumor activity

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Naphthazarin Derivatives (Ⅶ): Antitumor Action against ICR Mice Bearing Ascitic S-780 Cells

  • Song, Gyu-Yong;Kim, Yong;You, Young-Jae;Cho, Hoon;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • 제24권3호
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    • pp.190-193
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    • 2001
  • Various analogues of 5,8-dimethoxy-1,4-naphthoquinone (DMNQ) such as 2- or 6-(1-hydroxyiminoalkyl)-DMNQs were prepared and evaluated for the antitumor action. (1 -Hydroxyiminoalkyl)-DMNQs derivatives expressed greater antitumor action than (1-hydroxyalkyl) - or acyl-DMNQ derivatives. Moreover, 6-(1-hydroxyiminoalkyl)-DMNQ derivatives expressed higher antitumor action than 2-substituted ones, suggestive of a steric effect. Some of 6-(1-propyloxyalkyl)-DMNQ derivatives with an alkyl group of butyl to octyl moiety showed T/C values of >400%

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Syntheses and Evaluations of Antitumor and Antiangiogenic Phthalate Polymers Containing 5-Fluorouracil and Carboxylates

  • Lee, Sun-Mi;Jung, Sang-Wook;Ha, Chang-Sik;Chung, Il-Doo;Lee, Won-Ki;Park, Yong-Ho
    • 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.

Effects of Squalene on the Immune Responses in Mice(II):Cellular and Non-specific Immune Response and Antitumor Activity of Squalene

  • Ahn, Young-Keun;Kim, Joung-Hoon
    • Archives of Pharmacal Research
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    • 제15권1호
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    • pp.20-29
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    • 1992
  • Effects of squalene on cellular and non-specific immune responses and antitumor activity in mice were investigated. Cellular and non-specific immunological assay parameters adopted in the present study were delayed-type hypersensitivity reaction and resette forming cells (RFC) for cellular immunity, activities of natural killer (NK) cells and phagocyte for non-specific immunity. Squalene resulted in marked increases of cellular and non-specific immune functions and enhancement of host resistance to tumor challenge in dose-dependent manner.

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한의학의 항종양 면역치료에 관한 연구 -1990년 이후 발표된 실험논문을 중심으로- (Compilation of 104 Experimental Theses on the Antitumor and Immuno-activating therapies of Oriental Medicine)

  • 강연이;김태임;박종오;김성훈;박종대;김동희
    • 동의생리병리학회지
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    • 제17권1호
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    • pp.1-24
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    • 2003
  • This study was done to compile 104 experimental theses which are related to the antitumor and immuno-activating therapies between February 1990 through February 2002. Master's and doctoral theses were dassified by schools, degrees, materials, effects, experimental methods of antitumor and immunoactivity, and results. The following results were obtained from this study : 1. Classifying the theses by the school, 34.6% were presented by Daejeon University, 29.8% by Kyung-hee University and 11.5% by Won-kwang University. Of all theses, 51.0% were aimed for the doctoral degree and 43.3% were for the master's degree. All of three universities have their own cancer centers. 2. Classifying the theses by herb materials, complex prescription accounted for 60.3%, single herb accounted for 24.8% and herbal acupuncture accounted for 14.2%. Considering the key principles of the traditional medicine, complex prescription was much more thoroughly studied than single herb prescription. The results showed that the complex prescription had both antitumor activity and immuno-activating activity, which might reflects on multi-activation mechanisms by complex components. 3. Classifying the theses by the efficacy of herbs examined, in single herb, invigorating spleen and supplementing was 35.5%, expelling toxin and cooling was 29.0%, activating blood flow and removing blood stasis was 12.9%. In herbal acupuncture, invigorating spleen and supplementing was 52.9%, expelling toxin and cooling was 29.4%. In complex prescription, pathogen-free status was 41.9%, strengthening healthy qi to eliminate pathogen was 35.5%, strengthening healthy qi was 22.6%. It is presumed that the antitumor and immunoactivating therapy based on syndrome differentiation is the best way to develop oriental oncology. 4. Classifying the theses by antitumor experiments, cytotoxic effect was 48.1 %, survival time was 48.1 % and change of tumor size was 42.3%. Survival rate was not necessarily correlated with cytotoxicity. These data reflect the characteristic, wholistic nature of the oriental medicine which is based on BRM (biological response modifier). 5. Classifying the theses by immunoactivating experiments, hemolysin titer was 51.0%, hemagglutinin titer was 46.2% and NK cell's activity was 44.2%. In the future studies, an effort to elucidate specific molecular and cellular mechanisms of cytokine production in the body would be crucial. 6. Classifying the theses according to the data in terms of antitumor activity, 50% was evaluated good, 24.0% was excellent, and 15.5% have no effect. In an evaluation of immuno-activating activity, 35.9% was excellent and 18.0% showed a little effect. The index point, as described here, may helps to use experimental data for clinical trials. Changes in index points by varying dosage implicate the importance of oriental medical theory for prescription. 7. In 167 materials, IIP (immunoactivating index point, mean : 3.12±0.07) was significantly higher than AIP(antitumor index point, mean : 2.83±0.07). These data demonstrate that the effect of herb medicine on tumor activity depends more on immunoactivating activity than antitumor activity. This further implies that the development of herbal antitumor drugs must be preceded by the mechanistic understanding of immunoactivating effect. 8. After medline-searching tumor and herb-related articles from NCBI web site, we conclude that most of the studies are primarily focused on biomolecular mechanisms and/or pathways. Henceforth, we need to define the biomolecular mechanisms and/or pathways affected by herbs or complicated prescriptions. 9. Therefore, the most important point of oriental medical oncology is to conned between experimental results and clinical trials. For the public application of herbal therapy to cancer, it is critical to present the data to mass media. 10. To develop the relationship of experimental results and clinical trials, university's cancer clinic must have a long-range plan related to the university laboratories and, at the same time, a regular consortium for this relationship is imperative. 11. After all these efforts, a new type herbal medicine for cancer therapy which is to take care of the long-term administering and safety problem must be developed. Then, it would be expected that anti-tumor herbal acupuncture can improve clinical symptoms and quality of life (QOL) for cancer patients. 12. Finally, oriental medical cancer center must be constructed in NCC (National Cancer Center) or government agency for the development of oriental medical oncology which has international competitive power.

Construction of Novel Bifunctional Chimeric Proteins Possessing Antitumor and Thrombolytic Activities

  • Hui, Jing;Dai, Youjin;Bian, Yuanyuan;Li, Hui;Cui, Xiaojin;Yu, Xiaojie;You, Song;Hu, Fengqing
    • Journal of Microbiology and Biotechnology
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    • 제22권7호
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    • pp.894-901
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    • 2012
  • Based on their respective antitumor and thrombolytic activities, the superantigen staphylococcal enterotoxin C2 (SEC2) and staphylokinase (Sak) were chosen for the construction of the novel chimeric proteins Sak-linker-SEC2 and SEC2-linker-Sak using a linker composed of nine Ala residues. Both chimeric proteins possessed nearly the same PBMC proliferation stimulating activity and antitumor activity as SEC2 and thrombolytic activity as Sak. Neither the SEC2 or Sak component of each chimeric protein affected the activity of the other component. The results presented in this study provide a possible strategy to prevent and cure tumor thrombus.

Enhanced Antitumor Efficacy with Combined Administration of Astragalus and Pterostilbene for Melanoma

  • Huang, Xin-Yan;Zhang, Song-Zhao;Wang, Wen-Xi
    • Asian Pacific Journal of Cancer Prevention
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    • 제15권3호
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    • pp.1163-1169
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    • 2014
  • Astragalus, a commonly used traditional Chinese medicine, has exhibited antitumor actions in patients. In this study, in vitro and in vivo antitumor effects of astragalus and synergistic antitumor efficacy in combination with pterostilbene were investigated. Melanoma cells were treated with pterostilbene (Pt), graduated doses of astragalus injection (AI), or these in combination. Cell viability was measured using a MTT assay. Released nucleosomes and caspase activity were measured using enzyme-linked immunosorbent assay. Growth inhibition in vitro and in vivo was also assessed. Analysis of variance and t tests were used for statistical analysis. Significant reduction (p<0.05) in cellular proliferation were observed with AI and AI-Pt in a time- and concentration-dependent manner. Apoptosis and caspase-3/7 activity were significantly increased by AI and AI-Pt treatment (p<0.05). In vivo, AI inhibited melanoma tumor growth, with inhibition rates ranging from 36.5 to 62.3%, by inducing apoptosis via up-regulation Bax expression and the Bax/Bcl-2 ratio and down-regulating Bcl-2 expression. AI significantly inhibits the growth of melanoma in vitro and in vivo by inducing apoptosis. These data suggest that combined treatment of astragalus with pterostilbene enhances antitumor efficacy.

Pyrimidine Nucleoside 유도체들의 합성 및 약물학적 효능 검색 (Synthesis of Pyrimidine Nucleoside Analogues and Screening of Their Biological Effects)

  • 신혜순;이희주
    • Biomolecules & Therapeutics
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    • 제3권3호
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    • pp.217-222
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    • 1995
  • Several acyclonucleoside analogues of pyrimidine base and N$^1$-derivatives of 5-fluorouracil have been synthesized and evaluated for their biological effects. When tested with in vitro Lekemia L1210 cells, the 5-fluorouracil derivatives exhibited slightly higher antitumor activity than the parent 5-fluorouracil. When tested against Herpes Simplex Virus type 1 and type 2 cultured in the Vero cell, the 5-fluorouracil derivatives showed weak antiviral activity.

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리포좀에 봉입된 아클라루비신의 약물동태, 세포독성, 항암효과 및 비장/혈구 세포독성 (Pharmacokinetics, Cell Toxicity, Antitumor Activity and Spleen/Blood Cell Toxicity of Aclarubicin-entrapped Liposomes)

  • 박목순;박진규;이계원;명평근;석대은;황성주;지웅길
    • 약학회지
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    • 제42권3호
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    • pp.274-274
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    • 1998
  • Aclarubicin(ACL)-entrapped freeze dried liposomes were prepared using Microfludizer to attain a sustained release at targeted organs in a prolonged time so that it can reduce th e side effect and maximize the therapeutic effect. The freeze-dried liposomes were evaluated for pharmacokinetics, antitumor activity against Sarcoma 180, cytotoxicity against L1210 and A549 tumor cells, spleen toxicity and myelosuppressive action. The AUC0->8hr values were 122+/-42, 382+/-140, 419+/-171, 835+/-206 and 443+/-309mcg min/ml for free ACL. ACL-liposome formulation I, II, III and IV, respectively. Cytotoidcity of ACL-entrapped liposomes against L1210 and A549 tumor cells was 2-4 times higher than that of free aclarubicin. ACL-liposome formulation I(PC/CHOL/TA) showed the most potent antitumor activity against Sarcoma 180 in mice. The loss of body weight was much smaller with ACL-entrapped liposomes than free ACL after I.p. injection at a dose of 2 mg/kg/day. Compared to free ACL, ACL-entrapped liposomes expressed a lower and delayed spleen toxicity up to 5th day after I.v. administration. Myelosupperssion seemed to be lower with ACL-entrapped liposome of PC/PC-hydrate/CHOL/TA (formulation III) than free aclarubicin.

갓버섯의 항균 분석 (Antitumor Components of the Cultured Mycelia of Lepiota procera)

  • 김병각;심미자;김옥남;김하원;최응칠
    • 한국식품위생안전성학회지
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    • 제4권2호
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    • pp.109-118
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    • 1989
  • 한국산 담자균류인 갓버섯 Lepiota procera의 균사를 액내 배양하여 항암성분인 단백성 다당체를 분리하였다. 이 성분은 DEAE-Sephadex A-50 이온교환수지와 Sepharose-4B gel Filtration을 이용하여 정제하여 Fraction C1을 얻었으며 이 Fr, Cr은 단백질과 다당체로 구성되어 있으며 항암 효과는 10mg/kg/day 투여군에서 64%의 저지유을 나타내었다. 이러한 항암작용의 기전을 밝히기 위한 연구의 일환으로 면역에 미치는 영향을 실험함 결과 이 단백다당체는 용혈반형성 세포수를 증가시켰으며, 저하된 지연성 과민반응을 회복시켰을 뿐만 아니라, carrageenan 투여에 의해 억제된 면역능을 다시 증강시켰음을 알 수 있었다. 이러한 결과들은 이 버섯의 항암작용이 세포독성에 의한 것이 아니라 종양에 대한 면역능을 강화시켜 발휘됨을 제시하고 있다.

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들깻잎에서 동정한 Phytol의 항암 및 면역활성증강 효과 (Antitumor Activity of Phytol Identified from Perilla Leaf and its Augmentative Effect on Cellular Immune Response)

  • 김광혁
    • Journal of Nutrition and Health
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    • 제26권4호
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    • pp.379-389
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    • 1993
  • Several studies have shown that extracts from yellow-green vegetables reveal antitumor activities. In the present study we investigated the effect of phytol in order to elucidate the immunological mechanism of antitumor activity of this substance. The results obtained from the experiment as follows: 1) Phytol showed cytotoxic effect on sarcoma 180 cells in vitro. 2) When phytol was injected into the peritoneal cavity of mice transplanted with sarcoma 180 cells, the average survival time (24.0 days) tended to increase as compared with the nontreated control (19.2 days). 3) When sarcoma 180 cells were injected subcutaneously into the right groin of mice, and then phytol was injected into the peritoneal cavity, the tumor inhibition ratio was 33%. 4) The natural killer(NK) cell activity was significantly augmented by phytol in vitro and in vivo. Similar augmentations of NK cell activity were obtained with culture supernatants of phytol exposed spleen cells and peripheral blood mononuiclear cells. 5) Phytol on the macrophage from peritoneal cavity showed a higher effectiveness in vivo than in vitro. These results indicate that phytol shows the inhibitory effect for growth of sarcoma 180 cells in vitro, also it can augment macrophage and NK cell activities in vivo.

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