• Archives of Pharmacal Research
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• 제19권1호
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• pp.62-65
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• 1996

A homologous series of twenty, hitherto unreported, analogues of 5-halosubstituted $1, 3-Bis(\omega-cyanoalkyl)uracil$acyclic nucleosides were synthesized by the series of alkylation reactions of 5-halouracils with the corresponding chloroacetonitrile, chloropropionitrile, chlorobutyronitrile and 5-chlorovaleronitrile $(Cl-(C_ 2)_n-CN: n=l, 2, 3, 4)\; in\; anhydrous\; DMSO\; (or DMF)/K_2CO_3(or NaH)\; under\; 75^{\circ}C$ temperature. Antitumor activities for the synthesized compounds were determined against three cell lines (FM-3A cell, P-388 cell and U-938 cell lines). The compounds that exhibited moderate activity to significant activity, included la-b, 2a-b, 3a-c, and 4a, whose compounds were active against P-388, FM-3A and U-937 cell lines with the compounds la, lb, and 2a, showing significant antitumor activity (inhibitory concentrations $(IC_{50})$ ranged from 2.2 to $7.0\mug/ml$). Their strucrure-activity relationship did not show any activity differences in their effective chain length (methyl, ethyl, propyl, butyl) in 1, 3-bis(.omega.-cyanoalkyl) uracils.

• 한국미생물·생명공학회지
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• 제22권3호
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• pp.322-328
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• 1994

Antitumor and immunoadjuvant activities of Bifidobacterium adolesentis ATCC-15703 were investigated against the ascites and solid forms of tumor induced by Sarcoma 180(S-180) in ICR mice. When 100 $\mu$g of the bacterium was intraperitonealy administered in the mice, the survival rate(T/C %) of the mice was 132% for 50 days after the inoculation of S-180, however the increment of their body weights was suppressed. When the 100 $\mu$g was subcutaneously adminis- tratered at the right grion, the suppresion rate of the tumor growth on the 21st day after inoculation of S-180 were 62.3%. Complete supression of the tumor growth was observed from 2 out of 8 test mice. The bacterium itself appeared to have noncytotoxic substance against the S-180 in vitro. The bacteria] administration markedly enhanced the activity of peritoneal macrophages. The num- ber of peritoneal macrophages at one day after the administration of the 100 $\mu$g increased about 8 times as much as that of the control, and the highest activity of acid phosphatase appeared at 2 days.

• Food Science and Biotechnology
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• 제17권5호
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• pp.976-982
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• 2008

The 10 species of marine green algae was collected from Jejudo(Island) in Korea. Methanolic and aqueous extracts were prepared and screened for inhibition activities against tumor cell growth. Of the tested samples, the sea staghorn (Codium fragile) aqueous extract (CFAE) showed the highest activity on CT-26 cell growth. Therefore, CFAE was selected for further experiments and the possibility to induce apoptosis by the CFAE was investigated. Flow cytometric analysis revealed that it dose-dependently increased apoptotic cells with hypodiploid DNA contents in CT-26 cell line. These results indicated that CFAE can suppress the growth of CT-26 cells through apoptosis. The CFAE decreased the protein expression of anti-apoptotic Bcl-xL and led to the activation of caspase-3 and -7. A crude polysaccharide was separated from CFAE and it mainly constituted with 61.2% galactose and 30.5% arabinose as analyzed by high performance liquid chromatography (HPLC).

• Bulletin of the Korean Chemical Society
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• 제32권7호
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• pp.2397-2404
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• 2011

Variable selection k nearest neighbor QSAR modeling approach was applied to a data set of 80 3-arylisoquinolines exhibiting cytotoxicity against human lung tumor cell line (A-549). All compounds were characterized with molecular topology descriptors calculated with the MolconnZ program. Seven compounds were randomly selected from the original dataset and used as an external validation set. The remaining subset of 73 compounds was divided into multiple training (56 to 61 compounds) and test (17 to 12 compounds) sets using a chemical diversity sampling method developed in this group. Highly predictive models characterized by the leave-one out cross-validated $R^2$ ($q^2$) values greater than 0.8 for the training sets and $R^2$ values greater than 0.7 for the test sets have been obtained. The robustness of models was confirmed by the Y-randomization test: all models built using training sets with randomly shuffled activities were characterized by low $q^2{\leq}0.26$ and $R^2{\leq}0.22$ for training and test sets, respectively. Twelve best models (with the highest values of both $q^2$ and $R^2$) predicted the activities of the external validation set of seven compounds with $R^2$ ranging from 0.71 to 0.93.

• Macromolecular Research
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• 제9권5호
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• pp.277-284
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• 2001

Poly(exo-3,6-epoxy-1,2,3,6-tetrahydrophthalic anhydride)s [poly(ETA)s] and poly($\alpha$-ethoxy-exo-3,6-epoxy-1,2,3,6-tetrahydrophthaloyl-5-fluorouracil)s [poly(EETFU)s ] with various average molecular weights were prepared by photopolymerizations. The number average molecular weights of the fractionated poly(ETA)s and poly(EETFU)s determined by GPC were in the range of 3,600∼21,000 and 3,600-33,400, respectively. The release rate of 5-FU from poly(EETFU) decreased with increasing average molecular weight. The in vitro cytotoxicity of poly(ETA) against a normal cell line was lower than that of 5-fluorouracil(5-FU), The in vivo antitumor activities of the synthesized samples at dosage of 0.8 mg/kg against mice bearing sarcoma 180 tumor cell line decreased in the following order: poly(EETFU) > poly(ETA) > EETFU > ETA > 5-FU. The antiangiogenic activities of the poly(ETA)s were better than those of 5-FU.

• KSBB Journal
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• 제6권1호
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• pp.45-54
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• 1991

The aims of this study were investigated the antitumor effects and immunological activities of lipopolysaccharides (LPS) extracted from Proteus vulgaris RH-90 toward sarcoma-180 cells. LPS extracted from Proteus vulgris RH-90 was irradiated with gamma ray for detoxification. The tumor incidence of sarcoma-180 occurs all group which injected with gamma ray irradiated LPS and tumor of sarcoma-180 was necrotized with breeding in the injected group of l0$\mu\textrm{g}$ LPS. The inhibition ratio of tumor growth showed at the highest level of 60.88% when 5$\mu\textrm{g}$ gamma ray irradiated LPS was injected into mice. The prolongation ratio of life showed 20.72% when injected into mice with gamma ray irradiated LPS of 5$\mu\textrm{g}$. In the effect of immunological activity, the number of circurating leucocyte and peritoneal exudate cells were increased significantly in the treatment group than that control group, and dose-dependent response indicated by the increase of weights of immunorgans which revealed the improvement of immunity. The effect of macrophage on phagocytes, there were not found the differences between phagocytic and corrected phagocytic index.

• 한국식품조리과학회지
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• 제29권5호
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• pp.573-580
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• 2013

We investigated the physiological activities of extracts from Lindera obtusiloba Blume leaf and twig (LLW: water extract from Lindera obtusiloba Blume leaf, LLE: 50% ethanol extract from Lindera obtusiloba Blume leaf, LTW: water extract from Lindera obtusiloba Blume twig, LTE: 50% ethanol extract from Lindera obtusiloba Blume twig). Total polyphenol and total flavonoid contents of LTE were 445.38 mg/g and 302.09 mg/g, respectively. The electron donating ability (95.38%) of LTE was higher than that of the LLE (93.76%), LTW (88.09%), and LLW (82.06%). The oxygen radical absorbance capacity of extracts were improved with 50% ethanol condition, rather than hot water. Superoxide radical scavenging activity and FRAP activity of the extracts were improved with an increase of treatment concentration. All the extracts($1,000{\mu}g/mL$) stimulated a production of nitric oxide (NO) in macrophage RAW264.7 cells. In particular, the NO stimulating activity of LTE was superior to that of LLE, LTW, and LLW. The antitumor activity of LTE ($500{\mu}g/mL$) in A549, HeLa and SNU719 was 55.63%, 83.87% and 68.11%, respectively. The UVB-induced MMP-1 production in HS68 cells was suppressed by the treatment of LTE (88.28%), LLE (83.96%), LTW (80.59%) and LLW (76.08%).

• IMMUNE NETWORK
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• 제13권1호
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• pp.30-33
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• 2013

Previously we showed that biodegradable nanoparticles containing poly-IC or CpG oligodeoxynucleotide (ODN) together with ovalbumin (OVA) were efficient at inducing MHC-restricted presentation of OVA peptides in dendritic cells. The CTL-inducing activities of the nanoparticles were examined in the present study. Nanoparticles containing poly-IC or CpG ODN together with OVA were prepared using biodegradable polymer poly(D,L-lactic acid-co-glycolic acid), and then were opsonized with mouse IgG. The nanoparticles were injected into the tail vein of mice, and 7 days later the OVA-specific CTL activities were measured using an in vivo CTL assay. Immunization of mice with the nanoparticles containing poly-IC or CpG ODN together with OVA elicited potent OVA-specific CTL activity compared to those containing OVA only. In accordance with these results, nanoparticles containing poly-IC or CpG ODN together with OVA exerted potent antitumor activity in mice that were subcutaneously implanted with EG7.OVA tumor cells. These results show that encapsulation of poly-IC or CpG ODN together with antigen in biodegradable nanoparticles is an effective approach for the induction of potent antigen-specific CTL responses in vivo.

• Advances in Traditional Medicine
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• 제1권2호
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• pp.36-44
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• 2000

The polysaccharide fractions were isolated and purified from Phellodendron chinese SCHNEID, and antitumor activities using the melanoma B-16-derived metastatic tumors were examined at dosages of 2, 5 and 10 mg/100 g. F-7 and F-8 showed the highest tumor metastatic inhibitory activities (inhibition ratio 60 and 80% in 2 mg/100 g), and in dose of 5 mg/100 g, the inhibitory ratios were 85 and 70%, respectively. Furthermore, 10 mg/100 g of intraperitoneal (i.p.) injection gave 90 and 95% of inhibition. When the effects of polysaccharides on hypersensitivity were examined, the inhibitory activities were not markedly observed in oral administration, indicating that the polysaccharides are directly acting to immune system. Also, the polysaccharides increased the number of circulating blood leukocytes and total peritoneal exudate cells. Although implantation of tumor cells greatly decreased the productivity of antibody (antibody-mediated) and T lymphocyte reactivity (delayed-type) as 6.3 from 9.3 and 5.9 from 7.7, represented by the increase of footpad thickness, respectively. the polysaccharides elevated the reactivity of T lymphocyte in tumor-bearing mice, which were rapidly recovered by discontinuance of sample treatments. Especially, F-2, F-5, F-7 and F-8 remarkably recovered the decreased sensitivity. These results clearly indicated that the i.p. injection is much effective to suppress tumor growth than oral administration.

• 약학회지
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• 제14권1_2호
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• pp.1-14
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• 1970

Seventeen N,N/sup I/-disubstituted thiourea derivatives were synthesized by the Hugershof reaction and reported. Antitumor activities of the synthesized compounds against ascitic Ehrlich Carcinoma and ascitic sarcoma 180 were reported. It was found that 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis (2-carboxyphenyl)-2,2/sup I/-dithiourea was considerably active against ascitic Ehrlich Carcinoma and Sarcoma 180 respectively. 1-(2-Carboxyphenyl)-3-(p-ethoxyphenyl)-2 thiourea was active against ascitic Sarcoma 180. 1-Salicyloyl-3-(p-ethoxyphenyl)-2-thiourea and 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis(2-hydroxyethyl)-2,2/sup I/-dithiourea were active against ascitic Ehrlich Carcinoma. Antitubercular activities of the synthesized compounds against Mycobacterium tuberculosis H/sub 37/ R/sub v/ were also reported. It was found that 1-Isonicotinyl-4-cyclohexyl-3-thiosemicarbazide was considerably active at 100 .mu.g/ml. 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis(2-hydroxyethyl)-2,2/sup I/-dithiourea and 1-Salicyloyl-3-(p-ethoxyphenyl)-2-thiourea were active at 1000 .mu.g/ml respectively. Antibacterial activities of nine compounds of the synthesized compounds against S. aureus and E. Coli were reported. It was found that 1,1-(p-Phenylene)-4,4/sup I/-bis(isonicotinyl)-2,2/sup I/-dithiosemicarbazide and 1-Isonicotinyl-4-cyclohexyl-3-thiosemicarbazide were considerably active against S. aureus and E. Coli respectively. 1-(6-Methyl-2-benzothiazolyl)-3-(1-naphthyl)-2-thiourea was active against S. aureus. 1,1/sup I/-(p-Phenylene)-3,3/sup I/-bis (2-hydroxyethyl)-2,2/sup I/-dithiourea was active against E. Coli.