• Journal of Life Science
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• v.21 no.7
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• pp.923-931
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• 2011

In the present study, we investigated the effect of indole-3-carbinol (I3C), a natural compound present in vegetables, on the cell migration and invasion of OVCAR-3 ovarian cancer cells. Our results indicated that I3C inhibited the proliferation of OVCAR-3 cells, a process which was associated with inhibition of cell motility as determined by wound healing experiments and cell invasion studies. I3C treatment increased the tightness of the tight junctions (TJs), which was demonstrated by an increase in transepithelial electrical resistance and a decrease in paracellular permeability. The RT-PCR and immunoblotting results indicated that I3C repressed the levels of claudin-3 as well as claudin-4, proteins that comprise a major part of TJs and play a key role in the control and selectivity of paracellular transport. Furthermore, the activities of matrix metalloproteinase (MMP)-2 and MMP-9 were also decreased by treatment with I3C, which was connected with the down-regulation of their mRNAs and protein expression. The results suggest that I3C may be expected to inhibit cancer cell metastasis and invasion by restoring TJs and decreasing MMP activity in ovarian cancer cell line OVCAR-3.

• International Journal of Molecular Medicine
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• v.44 no.5
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• pp.1979-1987
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• 2019

Sargassum thunbergii is a brown alga from which various bioactive compounds can be extracted. Among these, the activities of indole derivatives, particularly as potential inhibitors of matrix metalloproteinases (MMPs), and their underlying mechanisms have been rarely investigated. Therefore, we evaluated the inhibitory effects of indole-6-carboxaldehyde (I6CA) on MMP-9 by gelatin zymography and western blot anlaysis. We used phorbol 12-myristate 13-acetate (PMA), which is known to induce MMP-9 expression and secretion, to stimulate HT1080 cells. Our results revealed that I6CA significantly inhibited MMP-9 expression and secretion, without significantly affecting the viability of PMA-stimulated HT1080 cells. Our mechanistic studies indicated that I6CA suppressed the phosphorylation and activation of two mitogen-activated protein kinases (MAPKs), c-Jun N-terminal kinase (JNK) and extracellular signal-regulated kinase 1/2 (ERK). Furthermore, I6CA inhibited the phosphorylation of inhibitor of κBα (IκBα) in response to PMA stimulation, which suppressed nuclear factor-κB (NF-κB) p65 subunit nuclear translocation. Collectively, I6CA was determined to suppress MMP-9 expression and secretion, and effects were proposed to be mediated via the inhibition of the MAPK and NF-κB p65 pathways. Therefore, we suggested I6CA to be a potential therapeutic agent for MMP-9-related processes, including tumor invasion and metastasis; however, further investigation is required.

• Journal of Environmental Science International
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• v.13 no.6
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• pp.513-518
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• 2004

3-weeks old Commelina was transferred to and grown in Hoagland solution (Control, $100\muM$ $Cd^{2+}$, $100\muM$ $Cd^{2+}$+ $100\muM$ IAA, $100\muM$ $Cd^{2+}$+ $100\muM$ IAA + 2 mM sucrose) for 3 weeks and then the effects of indole acetic acid (IAA) on the accumulation of $Cd^{2+}$ and growth of $Cd^{2+}$-treated Commelina were investigated. In the treatment of $Cd^{2+}$, $Cd^{2+}$ was uptaked to 1.74, and 51.36 ${\mu}g/g$ frwt. at the first week, but for three weeks, 0.51 and 34,53 ${\mu}g/g$ frwt, in leaf and stem respectively. When IAA was treated along with $Cd^{2+}$, $Cd^{2+}$ was uptaked to 0.18 and 8.63 ${\mu}g/g$ fiwt, at the first week, and for the incubation of 3 weeks, 0,51 and 45.0 ${\mu}g/g$ fiwt. in leaf and stem. In case of $Cd^{2+}$+IAA+sucrose, $Cd^{2+}$ was uptaked to 1.45 and 18.33 ${\mu}g/g$ frwt. at the first week, but for 3 weeks, 0,51 and 25.45 ${\mu}g/g$ fiwt. in leaf and stem. Likewise $Cd^{2+}$ uptake, the growth was also affected by $Cd^{2+}$ and IAA. During the incubation of 3 weeks, $Cd^{2+}$ reduced the stem growth about 8% in all weeks, but the treatment of IAA recovered the inhibition of stem growth caused by $Cd^{2+}$ to the degree of the control Therefore, it could be concluded that IAA altered the pattern of $Cd^{2+}$ uptake and the growth which were supposed to change $Cd^{2+}$ toxicity.

• Toxicological Research
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• v.7 no.2
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• pp.157-163
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• 1991

The effect of patulin, a mycotoxin, on the growth of Escherichia coli cell was investigated. E. coli cell elongation usually shown in SOS-response for DNA repair was induced by 20 mg of patulin per ml. After staining the E. coli chromosome with fluorescence dye(DAPI, 4', 6-diamino-2-phenyl-indole), chromosomal DNA partitioning was not affected by patulin. The observation indicateds that patulin acts as a DNA damaging agent which is effective for E. coli cell elongation introduced by the inhibition of septum formation.

• Bulletin of the Korean Chemical Society
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• v.33 no.9
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• pp.2985-2990
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• 2012

New thiazoline derivatives 7a-c, and thiophenes 9a-c linked to indole moiety were easily prepared via the reaction of the acrylamide derivative 3 with phenacyl bromides 4a-c, depending on the reaction conditions. In addition, the reaction of compound 3 with hydrazonoyl chlorides 11a-f afforded a series of 1,3,4-thiadiazole derivatives 13a-f. Moreover, coupling of 3-(3-methyl-1H-indol-2-yl)-3-oxopropanenitrile (2) with the diazonium salts of 3-phenyl-5-aminopyrazole 16 or 3-amino-1,2,4-triazole 17 gave the corresponding hydrazones 18 and 19, respectively. Cyclization of the latter hydrazones yielded the corresponding pyrazolo[5,1-c]-1,2,4-triazine and 1,2,4-triazolo[5,1-c]-1,2,4-triazine derivatives 20 and 21, respectively. The structures of the synthesized compounds were assigned on the basis of elemental analysis, IR, $^1H$ NMR and mass spectral data. All the synthesized compounds were tested for in vitro activities against certain strains of fungi such as Aspergillus niger, Aspergillus nodulans, Alternaria alternate. Compounds showed marked inhibition of fungal growth nearly equal to the standards.

• Journal of Food Hygiene and Safety
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• v.10 no.3
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• pp.133-138
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• 1995

In vitro antimutagenic activity of methanol extract from brrwn rice and its physico-chemical characteristics were investigated using Salmonella typhimurium reversion assay and SOS chromotest. Methanol extracts of brown rice were not mutagenic compared with direct and indirect, mutagenicities of 4NQO (4-nitroquinoline oxide), 2NF(2-nitrofluorene), Trp-p-1(3-Amino-1,4-dimethyl-5H-pyrido-[4,3-b]indole), and Trp-p-2(3-Amino-1-methy-5H-pyrido-[4,3-b]indole). Antimutagenic activity against the indirect mutagenicties induced by Trp-p-1, Trp-p-2 and AFB1 (aflatoxin B1) was found in methanol extract. Even though antimutagenic activity showed dose-dependent, it remained constant at inhibition rate ranging 60~90% when the concentration was abov 3mg/plate in the S. typhimurium reversion assay and 0.2~0.6 mg/assay in the SOS chromotest. The antimutagenic activity of the methanol extracts was stable at various pH (2, 7 and 10), temperatures (60, 80 and 10$0^{\circ}C$)and heation times (2, 4, 6, 8, 10 min at 10$0^{\circ}C$).

• Journal of the East Asian Society of Dietary Life
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• v.7 no.4
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• pp.527-537
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• 1997

This study was performed to determine the effects of antimutagenicity of Porturaca oleracea L. in Korea. In Ames test, the ethanol extract of Poturaca oleracea L. inhibited mutagenic activity of N-methyl-N'-nitro-N-nitrosoguanidine(MNNG), , 4-nitroquinoline-1-oxide(4NQO), benzo($\alpha$)pyrene (B($\alpha$)P) and 3-amino-1,4-dimethyl-5H-pyrido-(4,3-b)indole (Trp-P-1) in Salmonella typhimurium TA98 and TA100. But hot-water extract Poturaca oleracea L. only Inhibited mutagenic activity of MNNG in Salmonella typhimurium TA100, On 4NQO, the ethanol extract 100-1,600$\mu\textrm{g}$/plate of Porturaca oleracea L. showed a slight inhibitory effect of 13-48%, 4-47% in TA98 and TA100, respectively, but on MNNG, it showed higher inhibitory effect of 6-86% in TA100, And the treatment of 1,600$\mu\textrm{g}$/plate of ethanol extract of Porturacea L. had strong antimutagenicity with 74-87% inhibition against TA98 and TA100 induced by B(a)P and with 85-93% inhibition against TA98 and TA100 induced by Trp-P-1. The ethanol extract was fractionated with ether. chloroform, ethylacetate, butanol and water. Among them, most of the fraction except water fraction showed strong antimutagenicity effects against mutation induced by 4-NQO, MNNG, B(a)P and Trp-P-1. Chloroform fraction had strong antimutagenicity with 91% inhibition against TA100 induced by MNNG, diethyl etherfraction had strong antimutagenicity with 92%, 98% inhibition against TA98 and TA100 induced by 4NQO, Chloroform fraction had strong antimutagenicity with 97% inhibition against TA100 induced by B (a)P and diethyl etherfraction had strong antimutagenicity with 98% inhibition against both strain Induced by Trp-P-1, respectively.

• Microbiology and Biotechnology Letters
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• v.29 no.3
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• pp.181-185
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• 2001

The naturally occurring chemical indole-3-carbinol (13C), found in vegetables of the Brassica genus, is a promising anticancer agent that was shown previ- ously to induce a Gl cell cycle arrest of human breast cancer cell lines, independent of estrogen receptor signaling. The anticancer activity of 13C and the possible mechanisms of its action were explored in a human hepatocellular carcinoma cell line, HepG2. Treatment of HepG2 cells with 13C suppressed the growth of the cells. The growth sup- pression caused by 13C ($IC_{50}$/: 444$\mu$M) was found to be partially due to its ability to stop the cell cycle in HepG2 cells. Western blot analysis for the Gl phase artiest demonstrated that the expression-levels of cyclin-dependent kinase (Cdk4, Cdk6) and cyclic D were reduced strongly after treatment of Hep72 cells with 13C (4007M) for 24- 72 hrs. Furthermore, I3C selectively abolished the expression of Cdk6 in a dose- and time-dependent manner, and accordingly, inhibited the phosphorylation of retinoblastoma. Interestingly, after the HepG2 cells reached their max- imal growth arrest, the level of the p21, a well-known Cdk inhibitor, increased significantly. Therefore, it could be considered that the Gl arrest of HepG2 cells treated with 13C was due to the indirect inhibition of Cdk4/6 activities by p21 Western blot analysis for G2/M phase arrest of demonstrated the levels of Cdc2 and cyclin Bl werer reduced dramatically after the treatment of HepG2 cells with 13C ($40\mu$M) for 24-72 hrs. flow cytometry of propidium iodide-stained HepG2 cells revealed that 13C induces a Gl (53%,72hr incubation) and G2 (25%,24hr incubation) cell cycle arrest. Thus, our observations have uncovered a previously undefined antiproliferative pathway for r3C that implicates Cdk4/6 and Cdc2 as a target for cell cycle control in human HepG2 cells. However, the 13C-medi- ated cell cycle arrest and repression of Cdk4/6 production did not affect the apoptotic induction of HepG2 cell.

• Preventive Nutrition and Food Science
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• v.2 no.3
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• pp.232-235
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• 1997

This study was investigated to determine antimutagenic effects of enzymatic browning reaction products (PEBRPs) obtained by reaction of polyphenol compouns with oxidase extracted from potato. Catechol (Ca) PEBRPs showed the strongeest inhibitor effects with 90% inhibition on benzo-($\alpha$)-pyrene(B($\alpha$)P) induced mutagenesis in Salmonella typhimurium TA98, but he least with40% inhibition on the 2-aminofluorene (2-AF) induced mutagenesis in TA98. The strong antimutagenic activities with 80% inhibition were observed in the presence of 100$\mu\textrm{g}$/plate of hydroquinone(HQ)-PEBRP on the B($\alpha$)P or 3-amino-1,4-dimethyl-5H-pyrido[4,3-b]indole(Trp-P-1) induced mutagenesis in TA98, whereas HQ-PEBRP showed the least antimutagenic effect on 2-AF-induced mutagenesis. The addition of 100$\mu\textrm{g}$ hydroxyhydroquinone(HHQ)-PEBRP to the plate led to approximately 82% inhibitory effects on 2-AF or Trp-P-1 induced mutagenesis in TA98, whereas the least antimutagenicity was obsrved in the4-nitroquinoline-1-oxide(4-NQO) induced mutagenesis in the presence of 100$\mu\textrm{g}$/plate of HHQ-PEBRP. More than 80% inhibiton were observed in the presence of 200$\mu\textrm{g}$/plate of Pyrogalol(Py)-PEBRP on the B($\alpha$)P or Trp-P-1 induced mutagenesis in TA98, but the least with 38% inhibition on 4-NQO induced mutagenesis in TA98. The results indicate that enzymatic browing reaction products of potato have a strong modulatory effect on mutagen induced mutagenesis in TA98.

• Mycobiology
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• v.36 no.2
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• pp.93-98
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• 2008

Two Schiff base ligands $L_1\;and\;L_2$ were obtained by the condensation of glycylglycine respectively with imidazole-2-carboxaldehyde and indole-3-carboxaldehyde and their complexes with Zn(II) were prepared and characterized by microanalytical, conductivity measurement, IR, UV-Vis., XRD and SEM. The molar conductance measurement indicates that the Zn(II) complexes are 1:1 electrolytes. The IR data demonstrate the tetradentate binding of $L_1$ and tridentate binding of $L_2$. The XRD data show that Zn(II) complexes with $L_1\;and\;L_2$ have the crystallite sizes of 53 and 61 nm respectively. The surface morphology of the complexes was studied using SEM. The in vitro biological screening effects of the investigated compounds were tested against the bacterial species Staphylococcus aureus, Escherichia coli, Klebsiella pneumaniae, Proteus vulgaris and Pseudomonas aeruginosa and fungal species Aspergillus niger, Rhizopus stolonifer, Aspergillus flavus, Rhizoctonia bataicola and Candida albicans by the disc diffusion method. A comparative study of inhibition values of the Schiff base ligands and their complexes indicates that the complexes exhibit higher antimicrobial activity than the free ligands. Zinc ions are proven to be essential for the growth-inhibitor effect. The extent of inhibition appeared to be strongly dependent on the initial cell density and on the growth medium.