• Title/Summary/Keyword: Cytotoxicity

Search Result 4,596, Processing Time 0.214 seconds

Synthesis and in vitro Antitumor Activity of lsoazamitosene and lsoiminoazamitosene Derivatives

  • Ahn, Chan-Mug;Kim, Soo-Kie
    • Archives of Pharmacal Research
    • /
    • v.19 no.6
    • /
    • pp.535-542
    • /
    • 1996
  • Seven isoazamitosene derivatives, mitomycin analogues, were synthesized and tested for cytotoxicities against leukemia and gastric cancer cell lines. Preparation of a pyrrolo[1, 2-a]benzimidazole (3) (azamitosene ring system) was completed by utilizing the Lewis acid-catalized cyclization, with .omicron.-chloronitrotoluene as the starting material. Nitration of 3 produced a mixtue of two isomers (5-nitro isomer (4) and 7-nitro isomer (5)) in product ratio of 36 : 52. 4 was directly converted into quinone (7) by reduction and Fremy oxidaton. Finally, quinone derivatives (8, 9, 10, and 11) were synthesized by 1, 4-addition of 7 with cyclic secondary amines. From above-mentioned 5, 8-nitro compound (15) was prepared in 4 steps. At pH 3, Fremy oxidation of 15 produced quinone (16), whereas iminoquinone derivatives (17a and 17b) at pH 7. Isoazamitosene derivatives (8, 9, 10, and 11), containing cyclic amino groups at the 7-position, showed potent cytotoxicity on P388, SNU-1, and KHH tumor cell lines. Among them, 8 had stronger cytotoxicity against SNU-1 cell line than mitomycin and adriamycin. Considering these results, isoazamitosene derivatives may had unique cytotoxicity profiles. However, isoiminoazamitosene derivatives (17a and 17b) revealed very weak cytotoxicity.

  • PDF

Inhibitory Effect of Lichen Metabolites and their Synthetic Analogues on Melanin Biosynthesis in Cultured B-16 Mouse Melanoma Cells

  • Matubara, H.;Miharu, K.;Kinoshita, K.;Koyama, K.;Ye, Yang;Takahashi, K.;Yoshimura, I.;Yamamoto, Y.;Miura, Y.;Kinoshita, Y.
    • Natural Product Sciences
    • /
    • v.4 no.3
    • /
    • pp.161-169
    • /
    • 1998
  • The analogues of lichen components showing anti-tyrosinase activities were synthesized. 4-Alkylresorcinol derivatives showed both the inhibitory activity and cytotoxicity in B-16 melanoma cells at the doses of 10 mM to 1.2 mM. Resorcinol and 4-methylresorcinol showed the inhibitory effect with a low cytotoxicity at the doses of 2.5 mM and $600\;{\mu}M$ among 4-alkylresorcinols, respectively. Some diphenylmethane derivatives (Type A, B, and C) had strong activities with a low cytotoxicity. While xanthine derivatives had no effect. Glucosides of 4,5-alkylresorcinol and the diphenylmethane derivative (Type B) were prepared to decrease the cytotoxicity. As a result, no effect were observed. Liposome of the diphenylmethane derivative (Type B) was prepared for the same purpose, and the latter showed a remarkable effect at the dose of $15\;{\mu}M$ with a low cytotoxicity.

  • PDF

Physiological Effects and Utilization of Corbicula elatior Products -Effect of Cockle Extracts on Carcinogen-induced Cytotoxicity and Immune REsponse RElated to Its Antitumor Activity- (재첩가공품의 생리학적 특성과 이용 -재첩추출물의 항암효과와 면역활성증강 효과-)

  • 서재수;최명원;전순실;장명웅
    • Journal of the Korean Society of Food Science and Nutrition
    • /
    • v.29 no.2
    • /
    • pp.235-240
    • /
    • 2000
  • Inhibitory effects of cockle extracts on carcinogen-induced cytotoxicity in C3H/10T1/2 cells were studied. Soup (62$\mu\textrm{g}$/mL), solubility (28$\mu\textrm{g}$/mL) and liposolubility (9 $\mu\textrm{g}$/mL) of the cockle inhibited 3-methyl-cholanthrene(MCA)-induced cytotoxicity in C3H/10T1/2 cells by 53 and 94%, respectively. These results suggest that the extracts cockle might have anticarcinogen-induced cytotoxicity of C3H/10T1/2 cells. The effects of cockle extracts on the immune response related to its antitumor activity in vitro and in vivo were investigated. The cockle extracts showed a direct cytotoxic effect on sarcoma-180 cells, tumor cells in vitro. Soup (0.49 mg/mL), solubility (0.11 mg/mL) and liposolubiliy (0.05 mg/mL) of the cockle markedly decreased the total numbers of sarcoma-180 cells, but not their viability. The phagocytic acitivity of peritoneal macrophage of mice was significantly augmented by these extracts of the cockle compared with that of control in vivo. These extracts also raised the phagocuytic index, indicating that the number of phagocytize dmicrobes per macrophage increased. Thus, cockle extracts might show a antitumor activity by enhancing the phagocytic cell activities.

  • PDF

Protective Effect of Omega-3 of Polyunsaturated Fatty Acid Docosahexaenoic Acid on the Organic Mercury-Induced Cytotoxicity in Cultured NIH3T3 Fibroblasts

  • Ha, Dae-Ho;Lee, Jai-Kyoo
    • Biomedical Science Letters
    • /
    • v.14 no.3
    • /
    • pp.187-192
    • /
    • 2008
  • To clerify the protective effect of omega-3 of polyunsaturated fatty acid docosahexaenoic acid (DHA) on the cytotoxicity induced by organic mercury in cultured NIH3T3 fibroblasts. The measurement of cell viability on ogranic mercury wad done by XTT assay after NIH3T3 fibroblasts were cultured with various concentrations of methyl mercuric chloride (MMC). And also, the effect of DHA on the MMC-mediated cytotoxicity was examined by cell viability, and antioxidant effect of DHA was also assessed by superoxide dismutase (SOD)-like activity and the lipid peroxidation activity in cultured NIH3T3 fibroblasts. In this study, MMC decreased cell viability and $XTT_{50}$ value was determined at $50{\mu}M$ of MMC in these culture. In the effect of DHA against the cytotoxicity induced by MMC, DHA significantly increased the cell viability damaged by MMC in cultured NIH3T3 fibroblasts. And also, DHA showed the antioxidant effect by showing the increase of SOD-like activity and the decrease of lipid peroxidation activity. From these results, it is suggested that organic mercury such as MMC has highly toxic effect on cultured NIH3T3 fibroblasts, and also, omega-3 of polyunsaturated fatty acid, DHA showed the protection on MMC-induced cytotoxicity and antioxidant effect.

  • PDF

Effect of Kaempferol on the Cytotoxicity Induced Oxygen Free Radicals in Skin Fibroblast Derived from Human In Vitro

  • Lee, Jai-Kyoo;Ha, Dae-Ho
    • Biomedical Science Letters
    • /
    • v.14 no.3
    • /
    • pp.193-198
    • /
    • 2008
  • In order to evaluate on the effect of kaempferol on the cytotoxicity of oxygen tree radicals, XTT assay was performed to determine the cell viability after skin fibroblasts derived from human (Detroit 51) that were treated with various concentrations of hydrogen peroxide $(H_2O_2)$. And also, the effect of kaempferol on the cytotoxicity induced by H202 that was examined by cell viability, lactate dehydrogenase (LDH) activity and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity in these cultures. $H_2O_2$ decreased cell viability in dose-dependent manner in these cultures and the $XTT_{90}\;and\;XTT_{50}$ values were determined at concentration of $35{\mu}M\;and\;90{\mu}M$ of $H_2O_2$ after skin fibroblasts derived from human were treated with $15{\sim}90{\mu}M$ of $H_2O_2$ for 6 hours, respectively. $H_2O_2$ was highly toxic on cultured skin fibroblasts derived from human by toxic criteria of Brenfreund and Puerner (1984). In the protective effect of kaempferol on $H_2O_2$-induced cytotoxicity, kaempferol increased DPPH radical scavenging activity and significantly decreased LDH activity. From these results, it is suggested that oxygen tree radical, $H_2O_2$, was highly toxic on cultured skin fibroblasts derived from human, and also kaempferol of flavonoid showed the protection on $H_2O_2$-induced cytotoxicity.

  • PDF

Synthesis and In Vitro Cytotoxicity of Cinnamaldehydes to Hyman Solid Tumor Cells

  • Kwon, Byoung-Mog;Lee, Seung-Ho;Choi, Sang-Un;Park, Sung-Hee;Lee, Chong-Ock;Cho, Young-Kwon;Sung, Nack-Do;Bok, Song-Hae
    • Archives of Pharmacal Research
    • /
    • v.21 no.2
    • /
    • pp.147-152
    • /
    • 1998
  • Cinnamaldehydes and related compounds were synthesized from various cinnamic acids based on the $2^{I}$-hydroxycinnamaidehyde isolated from the bark of Cinnamomum cassia Blume. The cytotoxicity to human solid tumor cells such as A549, SK-OV-3, SK-MEL-2, XF498 and HCT15 were measured. Cinnamic acid, cinnamates and cinnamyl alcohols did not show any cytotoxicity against the human tumor cells. Cinnamaldehydes and realted compounds were resistant to A549 cell line up to 15 .mu.g/ml. In contrast, HCT15 and SK-MEL-2 cells were much sensitive to these cinnamaidehyde analogues which showed $ED{50} values 0.63-8.1{\mu}g/ml.$Cytotoxicity of the saturated aldehydes was much weak compared to their unsaturated aldehydes. From these studies, it was found that the key functional group of the cinnamaldehyde-related compounds in the antitumor activity is the propenal group.p.

  • PDF

Preparation and Characterization of Water-Soluble Glass Through Melting Process(II) : Dissolution Characteristics, Bactericidal Effects and Cytotoxicity (용융법에 의한 수용성 유리의 제조 및 특성(II) : 용해 특성, 살균 효과 및 세포 독성)

  • 오승한;조종호;최세영;오영제
    • Journal of the Korean Ceramic Society
    • /
    • v.34 no.1
    • /
    • pp.13-22
    • /
    • 1997
  • Water-soluble phosphate glasses containing Ag and Cu ion were prepared through melting process. Dis-solution characteristics, bactericidal effect and cytotoxicity were investigated with composition and time in D. I. water using the powdered sample. Surface change were observed with increasing dissolution time us-ing the bulk specimen. Dissolution amount was maximum at the molar Ag:Cu ratio of 1 and increased with increasing time. The behavior of dissolution was total dissolution from the early stage. But no new layer was observed at the glass surface during dissolution. The bactericidal effect for pseudomonas sp, e. coli, sta-phylococcus aureus, and salmonella increased with increasing dissolution amount and therefore great bac-tericidal effect appeared. The result of cytotoxicity experiment to L929 showed that solution with more than 10 ppm of Ag ion had strong cytotoxicity.

  • PDF

A study on cytotoxicity of Ti-Nb alloys (Ti-Nb계 합금의 세포독성에 관한 연구)

  • Park, Hyo-Byeong
    • Journal of Technologic Dentistry
    • /
    • v.25 no.1
    • /
    • pp.89-94
    • /
    • 2003
  • The use of titanium alloys as biomaterials is increasing due to their superior biocompatibility and enhanced corrosion resistance compared to conventional stainless steels and cobalt-based alloys. Ti-6Al-4V ($\alpha+\beta$type) alloy instead of pure titanium ($\alpha$type) is being widely used as biomaterials has some characteristics such as high fatigue strength, tensile strength and corrosion resistance. It also has similar characteristics to Ti in inducing bony ingrowth. But it has been reported recently that the vanadium element expresses cytotoxicity and carcinogenicity and the aluminium element is related with dementia of Alzheimer type and neurotoxicity. In order to overcome their detrimental effects, $\beta$-phase stabilizer Nb was chosen in the present study. CP-Ti(ASTM grade 2), Ti-3wt.%Nb($\alpha$type), Ti-20wt.%Nb ($\alpha+\beta$type) and Ti-40 wt.%Nb($\beta$type) alloys were melted by vacuum arc furnace. Biocompatibility of Ti-Nb alloys was evaluated by cytotoxicity test. The results can be summarized as follows: 1. For the cytotoxicity test, Ti-Nb alloys showed excellent biocompatibility compared to CP-Ti(ASTM grade 2), 316L STS and Co-Cr alloys.

  • PDF

Inhibitory Effects of Leachianone A from Sophora fIavescens Ait. against Cadmium Induced Cytotoxicity (고삼으로부터 분리된 Leachianone A의 카드뮴에 대한 독성억제 효과)

  • Young, Hee-Tae;Choi, Hwa-Jung;Baek, Seung-Hwa
    • Journal of Physiology & Pathology in Korean Medicine
    • /
    • v.22 no.5
    • /
    • pp.1163-1167
    • /
    • 2008
  • In this study, cytotoxicity of cadmium on NIH 3T fibroblasts was utilized in order to discover antitoxic compound in methanol extract of Sophora fIavascens Ait. There were treatment groups; control (medium only), $MTT_{50}$ group and five experimental groups. MTT {3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H- tetrazoliumbromide} assay was performed to evaluate the cytotoxicity of cell organelles and $IC_{50}$ was also measured. Accordingly we have examined the detoxification effects of methanol extract of S. flavescens Ait. and leachianone A (LA) on cadmium-treated NIH 3T3 fibroblasts ($IC_{50}=\;12.5{\mu}M$) to observe morphological changes by the light microscopy. Both S. flavescens Ait. methanol extract and LA showed inhibitory effects on cadmium-induced cytotoxicity. Furthermore, LA showed dose-dependency in detoxication. From these results, it is conceivable to suggest that LA from S. flavescens Ait. methanol extract is a potential antitoxic agent.

Selective Cytotoxicity of Novel Platinum(II) Coordination Complexes on Human Bladder Cancer Cell-Lines and Normal Kidney Cells

  • Kim, Jung-Tae;Rho, Young-Soo;Jung, Jee-Chang
    • The Korean Journal of Physiology and Pharmacology
    • /
    • v.7 no.2
    • /
    • pp.111-117
    • /
    • 2003
  • Cisplatin is often effective in cancer treatment, but its clinical use is limited because of its nephrotoxicity. We have synthesized new platinum(II) coordination complexes (PC-1 & PC-2) containing trans-${\iota}$ and cis-1,2-diaminocyclohexane (DACH) as carrier ligands and L-3 -phenyllactic acid (PLA) as a leaving group with the aim of reducing nephrotoxicity but maintaining its anticancer activity. In this study, new platinum(II) complex compounds were evaluated for selective cytotoxicity on cancer cell-lines and normal kidney cells. The new platinum complexes have demonstrated high efficacy in the cytotoxicity against human bladder carcinoma cell-lines (T-24/HT-1376). The cytotoxicity of these compounds against rabbit proximal renal tubular cells and human renal cortical tissues, was determined by MTT assay, the [3H]-thymidine uptake and glucose consumption test, and found to be quite less than those of cisplatin. Based on our results, these novel platinum compounds appear to be valuable lead compounds with high efficacy and low nephrotoxicity.