• Title/Summary/Keyword: proliferative activity

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Synthesis of Flavokawain B and its Anti-proliferative Activity Against Gefitinib-resistant Non-small Cell Lung Cancer (NSCLC)

  • Seo, Young Ho;Oh, Yong Jin
    • Bulletin of the Korean Chemical Society
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    • v.34 no.12
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    • pp.3782-3786
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    • 2013
  • Non-small cell lung cancer (NSCLC) is the most common type of lung cancer and that accounts for 85% of lung cancer patients. Although several EGFR-targeted drugs have been developed in the treatment of NSCLC, the clinical efficacy of EGFR-targeted drugs in NSCLC is limited by the occurrence of drug resistance. In this regard, Hsp90 represents great promise as a therapeutic target of cancer due to its potential to simultaneously disable multiple signaling pathways. In this study, we discovered that a natural product, flavokawain B disrupted Hsp90 chaperoning function and impaired the growth of gefitinib-resistant non-small cell lung cancer (H1975). The result suggested that flavokawain B could serve as a potential lead compound to overcome the drug resistance in cancer chemotherapy.

Bizarre Parosteal Osteochondromatous Proliferation (Nora's lesion) of the Big Toe (A Report of Two Cases and Review) (무지에 발생한 기괴성 방골성 골연골성 증식증 (2예 보고))

  • Kim, Sang Woo;Suh, Jae Hee;Shin, Seung Myeong;Cho, Bum Keun
    • Journal of Korean Foot and Ankle Society
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    • v.17 no.1
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    • pp.68-73
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    • 2013
  • Bizarre parosteal osteochondromatous proliferation (BPOP) is an rare benign tumor which involve mostly tubular bones of feet and hand. BPOP has clinical, radiographic, and histologic similarities with osteochondroma.Radiologically, BPOP has not central continuity with underlying osseous medulla. Histologically, the lesion has marked proliferative activity, and enlarged, bizzare, and binucleated chondrocytes.Despite the high risk of recurrence, treatment of choice is surgical resection. This report presents two cases of BPOP of the big toe with reviews of clinical, radiographic, and histological characteristics.

Anti-proliferative Effects of Daidzein, Baicalein, Hesperidin and Ursolic Acid on Human Breast Cancer Cells Stimulated by Estrogenic Compounds (에스트로겐성 물질에 의해 자극된 인간 유방암 세포 증식에 대한 다이드제인, 바이칼레인, 헤스페리딘 및 우르솔산의 억제 효과)

  • Lee, Mi-Nam;Lee, Su-Yel;Lee, Hyun-Jae;Seok, Jeong-Ho;Lee, Choong-Jae
    • YAKHAK HOEJI
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    • v.54 no.3
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    • pp.168-173
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    • 2010
  • We investigated whether three flavonoids including daidzein, baicalein, hesperidin and ursolic acid, a triterpene acid, affect proliferation of MCF-7 human breast cancer cells stimulated by estrogenic compounds. Ursolic acid and baicalein inhibited proliferation of MCF-7 cells induced by PhIP, a food-derived carcinogen with estrogenic activity. Daidzein and hesperidin inhibited estradiol-induced proliferation of MCF-7 cells. These compounds should be further investigated for the possible involvement in signaling pathway after estrogen receptor binding in breast cancer cells.

The expression and functional roles of microRNAs in stem cell differentiation

  • Shim, Jiwon;Nam, Jin-Wu
    • BMB Reports
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    • v.49 no.1
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    • pp.3-10
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    • 2016
  • microRNAs (miRNAs) are key regulators of cell state transition and retention during stem cell proliferation and differentiation by post-transcriptionally downregulating hundreds of conserved target genes via seed-pairing in their 3' untranslated region. In embryonic and adult stem cells, dozens of miRNAs that elaborately control stem cell processes by modulating the transcriptomic context therein have been identified. Some miRNAs accelerate the change of cell state into progenitor cell lineages—such as myoblast, myeloid or lymphoid progenitors, and neuro precursor stem cells—and other miRNAs decelerate the change but induce proliferative activity, resulting in cell state retention. This cell state choice can be controlled by endogenously or exogenously changing miRNA levels or by including or excluding target sites. This control of miRNA-mediated gene regulation could improve our understanding of stem cell biology and facilitate their development as therapeutic tools. [BMB Reports 2016; 49(1): 3-10]

Synthesis and Anti-cancer Activity of Indirubin Derivatives as the CDK Inhibitors

  • Ju, Moon-Myoung;Kim, Yong-Chul;Lee, Sang-Kook;Lee, Jong-Won
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.187.2-187.2
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    • 2003
  • The cyclin-dependent kinases (CDKs), a group of serine/threonine kinases that form active heterodimeric complexes binding to cyclins, are key regulators of the cell cycle. The role of cyclin dependent kinases(CDKs) in cell cycle regulation has stimulated an interest in them as potential targets for proliferative diseases such as cancer, psoriasis, and chemotherapeutic agent-induced alopecia. Indirubin, an active ingredient of a traditional Chinese recipe Danggui Longhui Wan, are potent CDK inhibitors competing with ATP for binding to the catalytic site of the CDKs. (omitted)

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Molecular docking study of nuciferine as a tyrosinase inhibitor and its therapeutic potential for hyperpigmentation

  • Veerabhuvaneshwari Veerichetty;Iswaryalakshmi Saravanabavan
    • Genomics & Informatics
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    • v.21 no.3
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    • pp.43.1-43.13
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    • 2023
  • Melanin is synthesized by tyrosinase to protect the skin from ultraviolet light. However, overproduction and accumulation of melanin can result in hyperpigmentation and skin melanoma. Tyrosinase inhibitors are commonly used in the treatment of hyperpigmentation. Natural tyrosinase inhibitors are often favoured over synthetic ones due to the potential side effects of the latter, which can include skin irritation, allergies, and other adverse reactions. Nuciferine, an alkaloid derived from Nelumbo nucifera, exhibits potent antioxidant and anti-proliferative properties. This study focused on the in silico screening of nuciferine for anti-tyrosinase activity, using kojic acid, ascorbic acid, and resorcinol as standards. The tyrosinase protein target was selected through homology modeling. The residues of the substrate binding pocket and active site pockets were identified for the purposes of grid box optimization and docking. Therefore, nuciferine is a potent natural tyrosinase inhibitor and shows promising potential for application in the treatment of hyperpigmentation and skin melanoma.

Phenolic Glycosides Isolated from Safflower (Carthamus tinctorius L.) Seeds Increase the Alkaline Phosphatase (ALP) Activity of Human Osteoblast-like Cells

  • Kim, Dong-Hyun;Lee, Jin-Hee;Ahn, Eun-Mi;Lee, Youn-Hyung;Baek, Nam-In;Kim, In-Ho
    • Food Science and Biotechnology
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    • v.15 no.5
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    • pp.781-785
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    • 2006
  • The chemical compositions of the seeds of the safflower (Carthamus tinctorius L.) plant were evaluated to determine possible compound having proliferative effects on human osteoblast cells. Three-[4,5-dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide (MTT) test and alkaline phosphatase (ALP) activity were used to assess the effects of the isolates on the human osteoblast-like line (Saos-2). Activity guided fractionation led to the isolation of ALP activating lignin and alkaloid glycosides through the extraction of the seeds, solvent partitioning and repeated silica gel and octadecyl silica (ODS) column chromatographic separations. The data from Nuclear Magnetic Resonance (NMR), Mass (MS), and Infrared (IR) analyses enabled the determination of the chemical structure and characterization of two compounds as a tracheloside and an N-(p-coumaroyl)-serotonin mono-${\beta}$-D-glucopyranoside. These two compounds showed respectively $149.2{\pm}4.2$ and $138.9{\pm}3.5%$ ALP activity compared to the control when evaluated at a concentration of $100\;{\mu}g/mL$.

Combination of Potassium Pentagamavunon-0 and Doxorubicin Induces Apoptosis and Cell Cycle Arrest and Inhibits Metastasis in Breast Cancer Cells

  • Putri, Herwandhani;Jenie, Riris Istighfari;Handayani, Sri;Kastian, Ria Fajarwati;Meiyanto, Edy
    • Asian Pacific Journal of Cancer Prevention
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    • v.17 no.5
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    • pp.2683-2688
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    • 2016
  • A salt compound of a curcumin analogue, potassium pentagamavunon-0 (K PGV-0) has been synthesized to improve solubility of pentagamavunon-0 which has been proven to have anti-proliferative effects on several cancer cells. The purpose of this study was to investigate cytotoxic activity and metastasis inhibition by K PGV-0 alone and in combination with achemotherapeutic agent, doxorubicin (dox), in breast cancer cells. Based on MTT assay analysis, K PGV-0 showed cytotoxic activity in T47D and 4T1 cell lines with $IC_{50}$ values of $94.9{\mu}M$ and $49.0{\pm}0.2{\mu}M$, respectively. In general, K PGV-0+dox demonstrated synergistic effects and decreased cell viability up to 84.7% in T47D cells and 62.6% in 4T1 cells. Cell cycle modulation and apoptosis induction were examined by flow cytometry. K PGV-0 and K PGV-0+dox caused cell accumulation in G2/M phase and apoptosis induction. Regarding cancer metastasis, while K PGV-0 alone did not show any inhibition of 4T1 cell migration, K PGV-0+dox exerted inhibition. K PGV-0 and its combination with dox inhibited the activity of MMP-9 which has a pivotal role in extracellular matrix degradation. These results show that a combination of K PGV-0 and doxorubicin inhibits cancer cell growth through cell cycling, apoptosis induction, and inhibition of cell migration and MMP-9 activity. Therefore, K PGV-0 may have potential for development as a co-chemotherapeutic agent.

Effect of Water Extract of Carthamus tinctorious L. on In Vitro Activity of T and B Lymphocytes (시험관내에서 홍화의 물 추출물이 T 및 B 림프구의 활성에 미치는 영향)

  • Choi, Youn-Hwa;Do, Jeong-Su;Nam, Sang-Yun
    • Korean Journal of Pharmacognosy
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    • v.35 no.4 s.139
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    • pp.330-337
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    • 2004
  • Based on the traditional application of Carthamus tinctorious L. (CF) as a component of Korean medicinal decoctions, in the present study, we investigated in vitro an immunomodulatory activity of water extract of CF(WECF). Water extract of CF significantly increased the in vitro proliferative responses of spleen cells (SPC). However, addition of WECF during anti-CD3 activation resulted in a significant decrease in SPC proliferation. Flow cytometric analysis showed that WECF addition chanced T and B cell frequencies in anti-CD3-activated spleen cell populations. Using purified cells, it was revealed that WECF is mitogenic to B cells but rather inhibitory to T cell Proliferation. Upon anti-CD3 stimulation, high concentration (1 mg/ml) of WECF significantly inhibited T cell proliferation until day 2 of stimulation. At day 3, anti-CD3-activated cells exposed to WECF recovered their proliferation to the level comparable to control. Although B cell proliferation was also inhibited in proliferation at day 1, it recovered sooner and then was rather augmented by WECF at day 3. These data indicate that WECF down-regulates lymphocyte proliferation at early phase of activation but T cells are more vulnerable than B cells to WECF, However, CD4+ and CD8+ T cells did not differ in WECF-mediated immunotoxicity. Data of propidium iodide (PI) staining showed that WECF accelerates activated T cell, but not B cell, apoptosis and WECF concurrently inhibited cytokine production of activated T cells. Taken together, WECF exhibits B cell mitogenic activity and differential toxicity more pronounced to T cells, suggesting a possible in vivo application of WECF for specific control of T cells without alteration of B cell activity.

Exopolysaccharide Produced by Pediococcus acidilactici M76 Isolated from the Korean Traditional Rice Wine, Makgeolli

  • Song, Young-Ran;Jeong, Do-Youn;Cha, Youn-Soo;Baik, Sang-Ho
    • Journal of Microbiology and Biotechnology
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    • v.23 no.5
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    • pp.681-688
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    • 2013
  • This work is aimed to increase knowledge of the functional exopolysaccharide (EPS) from lactic acid bacteria (LAB) in makgeolli, a Korean fermented rice wine. Among LAB strains isolated from makgeolli, strain M76 was selected as a functional strain producing a bioactive EPS, based on its antioxidative activity on the DPPH radical. The 16S rRNA gene sequencing analysis showed a high sequence similarity (99.0%) with P. acidilactici, but had different biochemical properties with the already known P. acidilactici type strains in the aspect of carbohydrates utilization. The obtained P. acidilactici M76 produced a soluble EPS above 2 g/l. One-step chromatography using gel filtration after ethanol precipitation from the supernatant of P. acidilactici M76 was enough to obtain purified EPS with a single peak, showing a molecular mass of approximately 67 kDa. Componential and structural analyses of EPS by TLC, HPLC, and FT-IR indicated that the EPS is a glucan, consisting of glucose units. The purified EPS had antioxidant activity on the DPPH radical of 45.8% at a concentration of 1 mg/ml. The purified EPS also showed proliferative effect on the pancreatic RIN-m5F cell line and remarkable protection activity on alloxan-induced cytotoxicity. This potent antioxidant and antidiabetic EPS by LAB in makgeolli may contribute to understanding the functionality of makgeolli.