• Applied Biological Chemistry
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• v.51 no.3
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• pp.212-218
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• 2008

This study was performed to determine the antimutagenic and anticancer effects of ethanol extract of buckwheat sprout using Ames test and SRB assay, respectively. An ethyl acetate fraction (200 ${\mu}/plate$) from the ethanol extract of buckwheat sprout showed inhibition rate of 80.6% against the mutagenesis induced by N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) in Salmonella typhimurium TA100 strain. Also the ethyl acetate fraction (200 ${\mu}/plate$) showed higher antimutagenic activity than other fractions against the mutagenesis induced by 4-nitroquinoline-1-oxide (4NQO) in Salmonella typhimurium TA98 and TA100. In addition, the ethyl acetate fraction (200 ${\mu}/plate$) showed high antimutagenic effect of 80.9% and 85.9% against the mutation of TA98 and TA100 strains induced by 3-amino-1,4-dimethyl-5H-pyrido-(4,3-b)indol (Trp-P-1), respectively. The cytotoxic effects of each solvent fraction from the ethanol extract of buckwheat sprout against human cancer cell lines including lung carcinoma (A549), gastric carcinoma (AGS), breast adenocarcinoma (MCF-7), hepatocellular carcinoma (Hep3B), and colon adenocarcinoma (Colo 205) were investigated. The ethyl acetate fraction of buckwheat sprout ethanol extract at the concentration of 1.0 mg/ml showed strong cytotoxic activities of 70.3, 94.8, 79.6, 82.3, and 73.2% against A549, AGS, MCF-7, Hep3B and Colo 205 cancer cell lines, respectively.

• Journal of Korean Biological Nursing Science
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• v.12 no.3
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• pp.127-132
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• 2010

Purpose: The aim of this study is to evaluate the effect of Xanthium sibiricum Patr. on carcinogenesis. Method: Water extract from Xanthium sibiricum Patr. (XPW) was prepared and investigated for the potential antitumor activity and inhibition of benzo[a]pyrene-DNA adduct formation and free radical formation. Result: It was shown that the water possess considerable toxicity toward tumor cell lines. Concentration of XPW at 1.0 mg/mL and 2.5 mg/mL resulted in more than 30% inhibition of growth in HeLa cells. Toxicity of XPW to A549 revealed that 54% inhibition of growth at concentration of 2.5 mg/mL. At concentrations of 0.5 mg/mL, 1.0 mg/mL and 2.5 mg/mL of XPW, the binding of [$^3H$]B[a]P metabolites to DNA of human Chang cell was inhibited by 19%, 33%, and 41%, respectively. There 18% and 32% inhibition in the free radical formation with XPW at the concentration of 1.0 mg/mL and 2.5 mg/mL, respectively. Conclusion: Water extract from Xanthium sibiricum Patr. (XPW) has antitumor and cancer chemopreventive activities.

• BMB Reports
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• v.48 no.10
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• pp.549-558
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• 2015

Cellular senescence is a process by which cells enter a state of permanent cell cycle arrest. It is commonly believed to underlie organismal aging and age-associated diseases. However, the mechanism by which cellular senescence contributes to aging and age-associated pathologies remains unclear. Recent studies showed that senescent cells exert detrimental effects on the tissue microenvironment, generating pathological facilitators or aggravators. The most significant environmental effector resulting from senescent cells is the senescence-associated secretory phenotype (SASP), which is constituted by a strikingly increased expression and secretion of diverse pro-inflammatory cytokines. Careful investigation into the components of SASPs and their mechanism of action, may improve our understanding of the pathological backgrounds of age-associated diseases. In this review, we focus on the differential expression of SASP-related genes, in addition to SASP components, during the progress of senescence. We also provide a perspective on the possible action mechanisms of SASP components, and potential contributions of SASP-expressing senescent cells, to age-associated pathologies.

• Korean Journal of Pharmacognosy
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• v.43 no.1
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• pp.6-9
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• 2012

The $CH_2Cl_2$ soluble part of the leaves of Helianthus tuberosus L. (Compositae) exhibited a potent cytotoxic activity against the cultured human tumor cell lines including A-549, SK-OV-3, SK-MEL-2, XF498 and HCT-15 in vitro. Bioassaydirected fractionation of the $CH_2Cl_2$ soluble part of this plant led to the isolation of four cytotoxic sesquiterpene lactones having ${\alpha}$-methylene-${\gamma}$-lactone ring in the molecule. On the basis of physical and spectral evidences, their structures were characterized as ${\Delta}^{4,15}$-isoatripliciolide tiglate (1), ${\Delta}^{4,15}$-isoatripliciolide methacrylate (2), budlein A isobutylate (3) and budlein A tiglate (4). The ${\Delta}^{4,15}$-isoatripliciolide tiglate (1) showed the most potent cytotoxic activity ($0.26{\mu}M<ED_{50}<2.16{\mu}M$) against all of the cell lines tested.

• Archives of Pharmacal Research
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• v.27 no.1
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• pp.44-47
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• 2004

Loranthus tanakae Fr. et Sav. (Loranthaceae) is a species of mistletoe, a semiparasitic plant growing on the branches of Quercus and Betula species as host trees. In our ongoing search for bioactive compounds from endemic species in Korea, we have investigated to isolate the chemical constituents responsible for the antitumor effect of the MeOH extract of L. tanakae. The ethyl acetate soluble part of the MeOH extract demonstrated a marginal inhibition on the proliferation of the tumor cell lines such as A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system), and HCT-15 (colon) in vitro. Thus, the activity-guided isolation procedure upon the ethyl acetate soluble part of the extract has been carried out and finally four flavonoid rhamnopyranosides (1-4) were isolated as active principle. The structures of 1-4 were elucidated by the physicochemical and spectral data as rhamnetin 3-O-$\alpha$-L-rhamnoside (1), quercetin 3-O-$\alpha$-L-rhamnoside (2), rhamnocitrin 3-O-$\alpha$rhamnoside (3), and kaempferol 3-O-$\alpha$-L-rhamnoside (4).

• Proceedings of the Plant Resources Society of Korea Conference
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• 2019.04a
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• pp.33-33
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• 2019

The AKT signaling pathway is a highly regulated cell signaling system that forms a network with other cell signaling pathways. Hence, the AKT signaling pathway mediates several important cellular functions that include cell survival, proliferation, cell migration, and et cetera. Irregularities that led overactive AKT signaling have been linked to many diseases such as cancer and metabolic-associated diseases. Hence, modulating the overactive AKT signaling pathway via inhibitor is a tantalizing prospect for treatment of cancer and metabolic-associated diseases. Two inhibitors of the AKT signaling pathway will be presented in this symposium: 1) Bisleuconothine A (BisA), a bisindole alkaloid that inhibit autophagy and 2) Ceramicine B (CerB), a limonoid that inhibit adipogenesis. The first topic is on a bisindole alkaloid, BisA and its mechanism in inducing autophagosome formation in lung cancer cell line, A549.(1) Since most autophagy inducing agents generally induce apoptosis, we found that BisA does not induce apoptosis even in high dose. BisA up-regulation of LC3 lipidation is achieved through mTOR inactivation. The phosphorylation of PRAS40, a mTOR repressor was suppressed by BisA. This observation suggested that BisA inactivates mTOR via suppression of PRAS40 phosphorylation. Interestingly, the phosphorylation of AKT, an upstream regulator of PRAS40 phosphorylation was also down-regulated by BisA. These findings suggested that Bis-A induces autophagosomes formation by interfering with the AKT-mTOR signaling pathway. The second topic is on CerB and its mechanism in inhibiting adipogenesis in preadipocytes cell line, MC3T3-G2/PA6.(2,3) CerB inhibits the phosphorylation of protein kinase B (AKT) at the Thr308 position but not the Ser473. Consequently, the phosphorylation of FOXO3 which is located downstream of AKT is also inhibited. Considering that FOXO3 is an important regulator of PPARγ which is a key factor in adipogenesis, CerB may inhibit adipogenesis via the AKT-FOXO3 signaling pathway. Taken together, both BisA and CerB highlighted the potential of AKT signaling pathway modulation as an approach to induce autophagy and inhibit the formation of fat cells, respectively.

• Journal of the Korean Wood Science and Technology
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• v.46 no.2
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• pp.166-177
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• 2018

Plant essential oils are defined as fragrant volatile oils extracted from leaves, stems, fruits, flowers, and roots of a plant. Such oils are composed of multiple components and multiple functions. By accumulation of inductive information, various plant essential oils have been studied for using in therapeutic medicine for various diseases. Despite of the apparent advantages of essential oils as a source of therapeutic medicines, plant essential oils have many limitations, including cytotoxic side effects. Therefore, it is necessary to evaluate the toxicity and the mechanisms of cytotoxicity of such oils. In this study, we evaluated the cytotoxicity to human-derived cell lines of 10 plant essential oils provided by National Institute of Forest Science (i.e., Larix kaempferi; Abies holophylla; Zanthoxylum ailanthoides; Pinus parviflora; Tsuga sieboldti; Chamaecyparis pisifera; Cryptomeria japonica; Pinus densiflora; Illicium anisatum; Pinus thunbergii). Cytotoxicity evaluations were accomplished by using CCK-assays and PCR-based cytotoxicity-related marker gene analyses with A549 cell line, and the Detroit551 cell line which are lung and skin cell line. The genes were analyzed included caspase-3 has a role in cell apoptosis, and the other cyclinA, cyclinB, cyclinD, and cyclinE regulated cell cycling for the cell proliferation. By examining the five cytotoxicity-related marker genes by performing real-time PCR and examined the cytostatic gene regulation associated with the various essential oils. The results of this study showed that the degree of cytotoxicity and the cytostatic gene regulation which could give precious information for using the plant essential oil for the clinical usages.

• Molecules and Cells
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• v.42 no.3
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• pp.270-283
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• 2019

This study was aimed to explore if lncRNA MALAT1 would modify chemo-resistance of non-small cell lung cancer (NSCLC) cells by regulating miR-197-3p and p120 catenin (p120-ctn). Within this investigation, we totally recruited 326 lung cancer patients, and purchased 4 NSCLC cell lines of A549, H1299, SPC-A-1 and H460. Moreover, cisplatin, adriamycin, gefitinib and paclitaxel were arranged as chemotherapies, and half maximal inhibitory concentration (IC50) values were calculated to evaluate the chemo-resistance of the cells. Furthermore, mice models of NSCLC were also established to assess the impacts of MALAT1, miR-197-3p and p120-ctn on tumor growth. Our results indicated that MALAT1 and miR-197-3p were both over-expressed within NSCLC tissues and cells, when compared with normal tissues and cells (P < 0.05). The A549, H460, SPC-A-1 and SPC-A-1 displayed maximum resistances to cisplatin ($IC50=15.70{\mu}g/ml$), adriamycin ($IC50=5.58{\mu}g/ml$), gefitinib ($96.82{\mu}mol/L$) and paclitaxel (141.97 nmol/L). Over-expression of MALAT1 and miR-197-3p, or under-expression of p120-ctn were associated with promoted viability and growth of the cancer cells (P < 0.05), and they could significantly strengthen the chemo-resistance of cancer cells (P < 0.05). MALAT1 Wt or p120-ctn Wt co-transfected with miR-197-3p mimic was observed with significantly reduced luciferase activity within NSCLC cells (P < 0.05). Finally, the NSCLC mice models were observed with larger tumor size and weight under circumstances of over-expressed MALAT1 and miR-197-3p, or under-expressed p120-ctn (P < 0.05). In conclusion, MALAT1 could alter chemo-resistance of NSCLC cells by targeting miR-197-3p and regulating p120-ctn expression, which might assist in improvement of chemo-therapies for NSCLC.

• Biomolecules & Therapeutics
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• v.5 no.2
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• pp.215-221
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• 1997

In an effort to screen new selective antitumor agents from the broth of soil microorganism, cytotoxicity oriented screening was performed against tumor cells and 3 compounds (Compound 1, 2 and 3) were isolated from Sreptomyces parvullus ISP 5048 and their chemical structures were determined. Among these compounds, Compound 2 showed the highest cytotoxicity against P388Dl and L1210. While the $IC_{50}$/ values of compound 2 against P388Dl and L1210 were 0.073$\mu$g/ml and 0.07$\mu$g/ml, respectively, and the $IC_{50}$/ value of Compound 3 was 0.17$\mu$g/ml against human lung cancer cells, A549, the cytotoxicity of Compound 2 and 3 against normal cell line, Vero E6 cell was about 4- and 8-fold lower than that of adriamycin. Based on the chemical analysis data, Compound 3 was octacosamicine A, a known antibiotic, which was reported by Dobasih et al. (1988). Taken together the results demonstrated that Compound 2 and Compound 3 has the possibility to be developed as antitumor agent because of its potent cytotoxicity as well as high selectivity against various cancer cell lines.

• Journal of Mushroom
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• v.20 no.3
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• pp.93-101
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• 2022

Cordyceps militaris mycelium extracts containing high amounts of cordycepin were evaluated in vitro for their anti-inflammatory and tumor cell growth-inhibitory activities. All extracts dose dependently inhibited the increased production of inflammatory mediators including reactive oxygen species (ROS), nitric oxide (NO), and 𝛽-hexosaminidase in lipopolysaccharide (LPS)-stimulated inflammatory cells. All extracts were evaluated for anti-proliferative activity against normal RBL-2H3 cells and diverse types of cancer cell lines, including HCT, MC5-7, U-87MG, AGS, and A549 cells. The extract showed the strongest growth inhibition (IC₅₀ = 28.13 ㎍/mL) relative to vehicle-treated control cells against fibrosarcoma (MC5-7). We have demonstrated anti-inflammatory activity of C. militaris via inhibition of NO, ROS production, and 𝛽-hexosaminidase release in activated cells. C. militaris mycelium extract was also evaluated mechanistically and found to exert six types of anti-cancer activity, confirming its pharmacological potential. Our study suggests C. militaris use as a potential source of anti-inflammatory and anti-cancer agents. C. militaris may also be considered a functional food.