• Archives of Pharmacal Research
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• v.25 no.3
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• pp.293-299
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• 2002

Cytotoxic and antimutagenic effects of a novel cis-$\varepsilon$-viniferin and five known stilbenes, transresveratrol, trans-$\varepsilon$-viniferin, gnetin H, suffruticosols A and B, isolated from the seeds of Paeonia lactiflora Pall. (Paeoniaceae) were determined against five different cancer cell lines, and mutagenicity of N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) in Salmonella typhimurium TA100, respectively. Six stilbenes showed cytotoxic activity in a dose-dependent manner, and especially did potent cytotoxic activity against C6 (mouse glioma) cancer cell with $IC_{50}$ values ranging from 8.2 to $20.5{\;}{\mu\textrm{g}}/ml$. trans-Resveratrol showed significant cytotoxic activity against HepG2 (liver hepatoma) and HT-29 (colon) human cancer cell lines with $IC_{50}$ values of 11.8 and 25.2 g/ml, respectively. In contrast, trans-$\varepsilon$-viniferin and cis--viniferin, and gnetin H exhibited marked cytotoxic activity against Hela (cervicse) and MCF-7 (breast) human cancer cell lines with $IC_{50}$ values of 20.4, 21.5, and $12.9{\;}{\mu\textrm{g}}/ml$, respectively. However, suffruticosol A and B had less cytotoxic effect against all cancer cells except C6. Meanwhile, six stilbenes exerted antimutagenic activity in a dose-dependent fashion. Of them, trans-resveratrol exhibited the strongest antimutagenic effect against MNNG with $IC_{50}$ value of $27.0{\;}{\mu\textrm{g}}/plate$, while other five resveratrol oligomers also did moderate antimutagenic activity with $IC_{50}$ values ranging from 31.7 to $35.2{\;}{\mu\textrm{g}}/plate$.

• Natural Product Sciences
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• v.28 no.1
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• pp.6-12
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• 2022

Five sesquiterpenoids, 7-epi-eudesm-4(15)-ene,1β,6α-diol (1), 7-epi-eudesm-4(15)-ene,1β,6α-diol (2), saniculamoid D (3), aphanamol I (4), and 4β,10α-dihydroxyaromadendrane (5), were isolated from the stem bark of Aglaia grandis. The compounds' (1-5) chemical structures were identified by spectroscopic data including, IR, NMR (¹H, ¹³C, DEPT 135°, HMQC, HMBC, ¹H-¹H COSY), and HRTOFMS, as well as by comparing with the previously reported spectral data. Therefore, this study described the structural elucidation of compounds 1-5 and evaluated their cytotoxic effects against Hela cervical and B16F10 melanoma cells for the first time, but no significant result was discovered.

• Proceedings of the Korean Society of Postharvest Science and Technology of Agricultural Products Conference
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• 2003.04a
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• pp.22-39
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• 2003

Biological activity of phenolic compounds in seeds and leaves of safflower (Carthamu tinctorius L.) were evaluated using several in vitro and in vivo assays. Six phenolic constituents were isolated from the seeds and identified as N-feruloylserotonia, N- (p-coumaroyl)serotonin, matairesinol, 8′-hydroxyarctigenin, acacetin 7-O-$\beta$-D-glucoside (tilianine) and acacetin. Six phenolic compounds exhibited considerable antioxidative activity, and especially two serotonins showed potent DPPH radical scavenging activity and antiperoxidative activity against rat liver microsomal lipid peroxidation induced by the hydroxyl radical generated via a Fenton-type reaction. Additionally, six phenolic compounds possessed comparable cytotoxicity against three cancer cells, Hela cell, MCF-7 and HepG2 cell, and particularly acacetin and its glycosides had the most potent cytotoxicity. Moreover, we found that feeding safflower seeds attenuated bone loss, and lowered levels of plasma and liver lipids in ovariectomized rats. Serotonins, lignans and flavones stimulated proliferation of the osteoblast-like cells in a dose-dependent manner (10$^{-15}$ ~10$^{-6}$ M), as potently as E$_2$ (17$\beta$-estradiol). Particularly, serotonins were mainly responsible for bone-protecting and lipid lowering effects in ovariectomized rats. Meanwhile, eight flavonoids, including a novel quercetin-7-O-(6"-O-acetyl)-$\beta$-D-glucopyranoside and seven kown flavonoids, luteolin quercetin, luteolin 7-O-$\beta$-D-glucopyranoside, luteolin-7-O-(6"-O-acetyl)-$\beta$-D-gluco-pyranoside, quercetin 7-O- -glucopyranoside, acacetin 7-O-$\beta$-D-glucuronide and apigenin-6-C-$\beta$-D-glucopyranosyl-8-C-$\beta$-D-glucopyranoside were first isolated and identified from safflower leaf. Among these flavonoids, luteolin-acetyl-glucoside and $\beta$quercetin- acetyl-glucoside showed potent antioxidative activities against 2-deoxyribose degradation and lipid peroxidation in rat liver microsomes. Luteolin, quercetin and their corresponding glycosides also exhibited strong antioxidative activity, while acacetin glucuronide and apigenin-6, 8-di-C-glucoside were relatively less active. Finally, changes in phenolic compositions were also determined by HPLC in the safflower seed and leaf during growth stages and roasting process to produce standardized supplement powerds. These results suggest that phenolic compounds in the roasted safflower seed and leaf may be useful as potential sources of therapeutic agents against several pathological disorders such as carcinogenesis, atherosclerosis and osteoporosis.

• Molecules and Cells
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• v.26 no.5
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• pp.443-453
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• 2008

The Bric-a-brac, Tramtrack, Broad-complex (BTB) domain is a protein-protein interaction domain that is found in many zinc finger transcription factors. BTB containing proteins play important roles in a variety of cellular functions including regulation of transcription, regulation of the cytoskeleton, protein ubiquitination, angiogenesis, and apoptosis. Here, we report the cloning and characterization of a novel human gene, KLHL31, from a human embryonic heart cDNA library. The cDNA of KLHL31 is 5743 bp long, encoding a protein product of 634 amino acids containing a BTB domain. The protein is highly conserved across different species. Western blot analysis indicates that the KLHL31 protein is abundantly expressed in both embryonic skeletal and heart tissue. In COS-7 cells, KLHL31 proteins are localized to both the nucleus and the cytoplasm. In primary cultures of nascent mouse cardiomyocytes, the majority of endogenous KLHL31 proteins are localized to the cytoplasm. KLHL31 acts as a transcription repressor when fused to GAL4 DNA-binding domain and deletion analysis indicates that the BTB domain is the main region responsible for this repression. Overexpression of KLHL31 in COS-7 cells inhibits the transcriptional activities of both the TPA-response element (TRE) and serum response element (SRE). KLHL31 also significantly reduces JNK activation leading to decreased phosphorylation and protein levels of the JNK target c-Jun in both COS-7 and Hela cells. These results suggest that KLHL31 protein may act as a new transcriptional repressor in MAPK/JNK signaling pathway to regulate cellular functions.

• Journal of the Korean Society of Food Science and Nutrition
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• v.31 no.1
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• pp.143-148
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• 2002

We investigated the cytotoxicity effects of Lycii fructus (LF) on HePG2, MCF7 and C6 cell lines by the MTT assay. We extracted the methanol (LFM) and fractionated to five partition layers. Among partition layers, the ethylether partition layer (LFMEE) was showed the strongest cytotoxic effects on all cancer cell lines. The hexane partition layer (LFMH) also was showed significant cytotoxic activities on Hela and MCF-7 cell lines. We also determined the induction of intracellular quinone reductase (QR) activity on HepG2 cells. Among various partition layers of Lycii fructus; LFMH was showed the most effective such induced effect such as 1.85 to the control value of 1.0. And we also determined the enhancement of anticarcinogenic effect by combination of Lycii fructus with vitamin C on all cell lines. These results suggest that potentially useful anticarcinegenic chemicals could be isolated from LFMEE and LFMH of the Lycii frutus and also we found the enhanced effect by the combination of various partition layers of LFM with vitamin C.

• The Journal of Korean Obstetrics and Gynecology
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• v.24 no.3
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• pp.14-27
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• 2011

Objectives: This study was designed to investigate the effects of Acanthopanacis Cortex Radicis extract(ACRE) on the apoptosis in HeLa cell and MCF-7 cell. Methods: After treatment with various concentration of ACRE, cell growth was evaluated in HeLa cell and MCF-7 cell. Hoechst 33342 staining was performed to estimate DNA fragment effect of ACRE on the apoptosis in HeLa cell and MCF-7 cell. Annexin V/PI apoptosis assay was used to estimate the effects of ACRE on the early apoptosis in HeLa cell and MCF-7 cell. RT-PCR was used to estimate the apoptosis gene expression effect of ACRE on Hela cell MCF-7 cell. Results: Under $0.1mg/m\ell$ of ACRE, cytotoxic effect was not found per NIH3T3 cell. The viability of HeLa cell and MCF-7 cells was significantly decreased ACRE ($100{\mu}g/m\ell$) in HeLa cell and MCF-7 cell, ACRE ($50{\mu}g/m\ell$) in HeLa cell 3 days after treatment, in MCF-7 cell 1&3 days after treatment (p<0.01). DNA fragmentation was observed 3 days after treatment of cl of ACRE on HeLa cell and MCF-7 cell. In Annexin V/PI apoptosis assay, after treatment of $100{\mu}g/m\ell$ of ACRE, the early apoptotic cell increased both in HeLa cell and MCF-7 cell. In RT-PCR analysis, after treatment of $100{\mu}g/m\ell$ of ACRE, bcl-2 were decreased and bax, caspase-3 were increased both in HeLa cell and MCF-7 cell. Conclusions: ACRE appears to have considerable activity on the apoptosis in HeLa cell and MCF-7 cell.

• Journal of Haehwa Medicine
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• v.25 no.1
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• pp.71-86
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• 2016

Objective : Hongyi (Formica yessensis) is the dried insect of fomicidae. In previous studies, it appeared possibilities on anti-thrombosis, preventing atherosclerosis, treating rheumatoid disease, and inhibiting hela cell. In this study, we investigated anti-inflammatory effects and mechanism of Hongyi. Methods : Hongyi A was extracted by water and made dried powder. Hongyi B was extracted by ethanol and made dried powder. We measured Nitric Oxide (NO) production on the mouse macrophages (RAW 264.7), mouse vascular endothelial cell (MOVAS) and human vascular endothelial cell (HUVEC) for anti-inflammatory effect. In addition, we conducted reverse transcription reaction (RT-PCR) for investigating the mechanism. Results : In RAW 264.7 macrophages stimulated by LPS, Hongyi A ($100{\mu}g/m{\ell}$) decreased NO production compared with LPS $2{\mu}g/ml$ control group with statistical significance (p<0.05). Hongyi A (50, $100{\mu}g/m{\ell}$) also decreased NO production compared with LPS $4{\mu}g/ml$ control group with statistical significance (p<0.01). Hongyi B (50, $100{\mu}g/m{\ell}$) decreased NO production compared with LPS $2{\mu}g/ml$ control group with statistical significance (p<0.01). Hongyi B (10, 50, $100{\mu}g/m{\ell}$) also decreased NO production compared with LPS $4{\mu}g/ml$ control group with statistical significance (p<0.01, p<0.001, p<0.001). In the MOVAS, Hongyi A and B increased NO production compared with control group. In the HUVEC, Hongyi B increased NO production compared with control group. The expression of NF-${\kappa}B$ in 12-hours MOVAS culture was decreased by Hongyi A and B (10, $50{\mu}g/ml$) compared with control group, but expression of $I{\kappa}B$ was increased. In the 24-hours MOVAS culture, expression of $I{\kappa}B$ was significantly increased. The expression of NF-${\kappa}B$ in 12-hours HUVEC culture was decreased by Hongyi A and B compared with control group, but expression of $I{\kappa}B$ was increased. Hongyi B also increased eNOS mRNA gene expression. Conclusions : Hongyi A and B showed anti-inflammatory effect in mouse macrophages with the activation of vascular endothelial cell through NO production in MOVAS and HUVEC repectively. Honyi B showed superior effect than Hongyi A, but additonal mechanism study should be conducted.

• The Korean Journal of Zoology
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• v.23 no.4
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• pp.203-218
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• 1980

Unscheduled DNA synthesis, chromosome aberrations, sister chromatid exchanges and DNA replication inhibition induced by the combined treatments with ara-C and UV-light or MMS in $HF_1$, CHO and $HelaS_3$ cells were studied, and the results obtained were as follows: (1) Ara-C was found to inhibit UV-or MMS-induced unscheduled DNA synthesis and the inhibitory effect of ara-C was more remarkable in its post-treatment. (2) Ara-C enhanced the rate of chromosome aberrations induced by MMS or UV-light. Post-treatment with ara-C exhibited the synergistic effect on MMS-induced chromosome aberrations mainly by increases of chromatid deletions. (3) Contrarily, ara-C did not increase the rate of sister chromatid exchanges, particularly in the pre-treatment with MMS, although it was found to induce sister chromatid exchanges. (4) The rate of DNA synthesis was declined immediately after are-C treatment and then recovered. The combined treatments with ara-C and UV-light or MMS showed that the initial response on replication inhibition was similar to that of ara-C, but later responses were similar to that of UV-light or MMS treated group.

• Korean Journal of Clinical Laboratory Science
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• v.49 no.4
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• pp.446-454
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• 2017

Human papillomaviruses (HPVs) are major causes of cervical cancer. Sixteen high risk HPVs, including HPV 16, HPV 18, HPV31, HPV 33, HPV 35, HPV 39, HPV 45, HPV 51, HPV 52, HPV 53, HPV 56, HPV 58, HPV 59, HPV 66, HPV 68, and HPV 69 are found in cervical cancer. HPVs 16 and 18 are mainly presented in 70% of cervical cancer. Therefore, identifying the presence of these high-risk HPVs is crucial. The objective of this study is to establish the HPV ViroCheck for detecting 16 HR-HPVs and genotypes of HPVs 16 and 18, as well as to analyze the analytical performance of HPV ViroCheck. We performed the analytical sensitivity of HPV E6 / E7 genes of 16 high risk HPVs to confirm the limit of detection. Then, a cross reactivity of HPV ViroCheck with microorganisms and viruses related to the cervix were analyzed for analytical specificity. Analytical sensitivity of high risk HPV genotypes ranged from 1 to 100 copies when using cloned DNAs. The limit of detection was 10 cells for both SiHa and HeLa cells. Cervical-related microorganisms and viruses did not show cross-reactivity to HPV DNA. Moreover, the intra- and inter-assay coefficient variations (CVs) were below 5%. In conclusion, HPV Virocheck will be useful for the detection of 16 HR HPVs, as well as HPV 16 and HPV 18 genotypes rapidly.