• 약학회지
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• 제54권5호
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• pp.328-333
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• 2010

Comparative molecular field analyses (CoMFA) on the antiproliferative activity of N-substituted (R) 2-amino-5-(2,4-dihydroxyphenyl)-1,3,4-thiadiazole analogues (ADTs: 1-17) against bladder cancer (HCV29T) and rectal cancer (SW707) cells were studied quantitatively. The statistical predictability and fitness of CoMFA A1 model for bladder cancer cells were better than those of CoMFA F1 model for rectal cancer cells and the antiproliferative activity of ADTs depends on steric field (HCV29T: 93.1% & SW707: 83.8%). Also, from the contour maps of optimized CoMFA models, the activity for bladder cancer cells had predicted to increase when sterically favored groups were substituted on meta- and para-position, and sterically disfavored groups were substituted on one ortho-position of phenyl ring. The activity for rectal cancer cells had predicted to increase when sterically favored groups were substituted on para-position, and sterically disfavored groups were substituted on two ortho-position of phenyl ring as R-group.

• 대한화학회지
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• 제64권1호
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• pp.7-18
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• 2020

An efficient and facile procedure has been developed for the synthesis of novel bichalcone derivatives (4a, 4b). The key step contains the solvent-free aldol synthesis of bichalcones based on quinones. Bichalcones (4a, 4b) were used as precursors for the synthesis of some interesting heterocyclic compounds like, diazepines (5a, 5b), pyrazolo-pyrimidines (7a, 7b), and pyrazoline derivatives (8a, 8b). Moreover, new thioxopyrimidine derivatives (9a, 9b) were furnished and used as a functionalizing agent to produce the triazole-pyrimidines (11, 12) and the carbonitrile derivative (14). All the synthesized compounds were fully characterized using physical and spectral data like, FT-IR, ¹H NMR, ¹³C NMR, and MS. Bichalcones (4a, 4b) and diazepines (5a, 5b) were screened for their anticonvulsant activity, where compounds (4a, 5a, and 5b) revealed potent anticonvulsant activity compared to diazepam. On the other hand, some of the prepared compounds were screened for their antiproliferative activity and they showed significant cytotoxic effects on most of the cancer cell lines with regard to broad spectrum antitumor activity.

• Journal of Microbiology and Biotechnology
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• 제20권4호
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• pp.693-699
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• 2010

An antiproliferative ribonuclease with a new N-terminal sequence was purified from fruiting bodies of the edible wild mushroom Russula delica in this study. This novel ribonuclease was unadsorbed on DEAE-cellulose, but absorbed on SP-Sepharose and Q-Sepharose. It had a molecular mass of 14 kDa, as judged by fast protein liquid chromatography on Superdex 75 and SDS-polyacrylamide gel electrophoresis. Its optimal pH and optimal temperature were pH 5 and $60^{\circ}C$, respectively. The ranking of its activity toward various polyhomoribonucleotides was poly C> poly G>poly A>poly U. It could inhibit proliferation of HepG2 and MCF-7 cancer cells with an $IC_50$ value of $8.6\;{\mu}M$ and $7.2\;{\mu}M$, respectively. It was devoid of antifungal and HIV-1 reverse transcriptase inhibitory activity.

• Food Science and Biotechnology
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• 제18권1호
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• pp.207-212
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• 2009

Celandine (Chelidonium majus, family Papaveraceae) is an herb used extensively in traditional Korean medicine. To investigate its antioxidant and antiproliferative activities, the methanolic extract of celandine was introduced. The antioxidant properties of the extract were tested using various in vitro systems, including hydroxyl radical scavenging assay, DNA damage protection assay, 1,1-diphenyll-2-2-pricylhydrazyl (DPPH) free radical scavenging activity, metal chelating activity, and reducing power assay. The extract exhibited stronger antioxidant activity ($IC_{50}=7.92{\mu}g/mL$) against hydroxyl radicals in the Fenton system than butylated hydroxyanisole ($IC_{50}=51.46{\mu}g/mL$) and $\alpha$-tocopherol ($IC_{50}=67.48{\mu}g/mL$). Likewise, damage to the plasmid pBR 322 induced by hydroxyl radicals was found to be protected by the extract at a concentration of $400{\mu}g/mL$. Cellular proliferation and the induction of apoptosis were also examined by a cellular proliferation assay, flow cytometry, and mRNA expression analysis. Taken together, the extract significantly inhibited the growth of HT-29 cells in a concentration- and time-dependent manner, and gradually increased both the proportion of apoptotic cells and the expression of caspase-3. Overall, our research suggests that celandine possesses antioxidant and antiproliferative properties.

• Archives of Pharmacal Research
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• 제27권5호
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• pp.554-561
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• 2004

Trichostatin A, an antifungal antibiotics, and HC-toxin are potent and specific inhibitors of histone deacetylase activity. Histone deacetylase inhibitors are new class of chemotherapeutic drugs able to induce tumor cell apoptosis and/or cell cycle arrest. In this study, the antiproliferative activities of trichostatin A and HC-toxin were compared between estrogen receptor positive human breast cancer cell MCF-7 and estrogen receptor negative human breast cancer cell MDA-MB-468. Trichostatin A and HC-toxin showed potent antiproliferative activity in both MCF-7 and MDA-MB-468 cells. In MCF-7 cells that contain high level estrogen receptor, trichostatin A and HC-toxin brought about three-times more potent cell growth inhibitory effect than estrogen receptor negative MDA-MB-468 cells. Both trichostatin A and HC-toxin showed cell cycle arrest at G$_2$/M phases of MCF-7 and MDA-MB-468 cells in a dose- and time- depen- dent manner. Trichostatin A and HC-toxin also induced apoptosis from MCF-7 and MDA-MB-468 cells in a dose- and time-dependent manner. Results of this study suggested that antipro-liferative effects of trichostatin A and HC-toxin might be involved in estrogen receptor signaling pathway, but cell cycle arrest and apoptosis of trichostatin A and HC-toxin might not be involved in estrogen receptor system of human breast cancer cells.

• 대한한의학방제학회지
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• 제22권2호
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• pp.35-43
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• 2014

Objectives : The purpose of this study was to identify antiproliferative effects of Salviae miltiorrhizae Radix(SM) extracts against cancer cell lines. Methods : We used 2 kinds of cancer cell lines such as colon cancer cells(HT-29), human oral epitheloid carcinoma cells(KB). MTT assay was performed to examine the efficacy of SM extracts on the cytostaticity of cancer cells in proportion to time and doses. Apoptosis was evaluated by DNA laddering and DAPI nuclei staining. Results : The MTT absorbances against HT-29 and KB of SM extracts were significantly decresed. DNA ladders could be identified in KB of SM extracts. The morphological change were observed and number of cells were decreased by SM extracts. Conclusions : SM extracts is considered to be effective to induce apoptosis and inhibit cancer cell proliferation.

• 한국식품영양학회지
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• 제35권6호
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• pp.464-472
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• 2022

The present study was designed to investigate the antiproliferative activity and molecular mechanisms of Bibimbap in HT-29 human colorectal adenocarcinoma cells. Bibimbap extract inhibited the proliferation of HT-29 cells by 50% at a concentration of 10.1±0.17 mg/mL for 48 h. The population of live cells decreased slightly, and the morphology changed with a reduction in cell volume (pyknosis) with Bibimbap. Treatment with 5 mg/mL of Bibimbap resulted in slight cell shrinkage. Furthermore, as the Bibimbap dose increased to 10 mg/mL, these characteristics were more evident, and HT-29 cells exhibited partial detachment by staining with the DNA-binding dye Hoechst 33342. Flow cytometric analysis by Annexin V and PI double staining showed that Bibimbap increased the levels of apoptosis. Analysis of the mechanism of these events showed that Bibimbap-treated cells exhibited a mitochondria-dependent apoptotic pathway through the modulation of caspase-3, caspase-8, caspase-9, and poly-ADP ribose polymerase, as well as Bax and Bcl-2 expression in dose- and time-dependent manners. Consequently, Bibimbap exerts a significant antiproliferative effect on HT-29 human colorectal adenocarcinoma cells.

• Journal of Korean Neurosurgical Society
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• 제46권4호
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• pp.389-396
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• 2009

Objective : Triptolide (TP) has been reported to suppress the expression of mitogen-activated protein kinase (MAPK) phosphatase-1 (MKP-1), of which main function is to inactivate the extracellular signal-regulated kinase-1/2 (ERK-1/2), the p38 MAPK and the c-Jun N-terminal kinase-1/2 (JNK-1/2), and to exert antiproliferative and pro-apoptotic activities. However, the mechanisms underlying antiproliferative and pro-apoptotic activities of TP are not fully understood. The purpose of this study was to examine whether the down-regulation of MKP-1 expression by TP would account for antiproliferative activity of TP in immortalized HT22 hippocampal cells. Methods : MKP-1 expression and MAPK phosphorylation were analyzed by Western blot. Cell proliferation was assessed by $^3H$-thymidine incorporation. Small interfering RNA (siRNA) against MKP-1, vanadate (a phosphatase inhibitor), U0126 (a specific inhibitor for ERK-1/2), SB203580 (a specific inhibitor for p38 MAPK), and SP600125 (a specific inhibitor for JNK-1/2) were employed to evaluate a possible mechanism of antiproliferative action of TP. Results : At its non-cytotoxic dose, TP suppressed MKP-1 expression, reduced cell growth, and induced persistent ERK-1/2 activation. Similar growth inhibition and ERK-1/2 activation were observed when MKP-1 expression was blocked by MKP-1 siRNA and its activity was inhibited by vanadate. The antiproliferative effects of TP, MKP-1 siRNA, and vanadate were significantly abolished by U0126, but not by SB203580 or SP600125. Conclusion : Our findings suggest that TP inhibits the growth of immortalized HT22 hippocampal cells via persistent ERK-1/2 activation by suppressing MKP-1 expression. Additionally, this study provides evidence supporting that MKP-1 may play an important role in regulation of neuronal cell growth.

• 한국생명과학회:학술대회논문집
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• 한국생명과학회 2002년도 제35회 학술심포지움 및 춘계학술대회
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• pp.72-72
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• 2002

• 한국응용과학기술학회지
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• 제26권2호
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• pp.161-170
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• 2009

In this work, a novel series of aminoisoquinolinylamide derivatives 1a-c and 2a-f were synthesized via several reaction steps, starting from 2-methyl-4-nitrobenzonitrile (3) and 1-chloro-5-nitroquinoline (8). And their antiproliferative activities were screened against A375 human melanoma cell line compared to Sorafenib as a reference compound. Among them, compound 1b and 1c exhibited meaningful inhibitory activities. These results demonstrated that aminoisoquinolinylamide scaffold possesses the possibility as the treatment for melanoma.