• Preventive Nutrition and Food Science
• /
• 제11권4호
• /
• pp.273-277
• /
• 2006

Recently, Rhei Rhizoma extracts (RRE) have begun to receive more attention as potential biological response modifiers. In the present study, we studied the antiproliferative effect of RRE on tumor cells and the effect of RRE on macrophage function. A variety of tumor cells and macrophages were treated with RRE at various concentrations. The effect of RRE on cell proliferation was measured by MTT assay and the effect of RRE on the production of nitric oxide (NO) was determined in the macrophage-like cell lines Raw264.7, C6 and peritoneal macrophages (pMQ). RRE inhibited the growth of tumor cells (e.g., B16, HOS). However, the effects of RRE on the production of NO varied with macrophage types. RRE had no effect on C6 cell growth and slightly increased the growth of Raw264.7 cells. In addition, treatment of normal pMQ with RRE enhanced NO production in a concentration-dependent manner, whereas RRE suppressed NO production at $50\;{\mu}g/mL$ in both Raw264.7 and C6 cells. However, RRE suppressed NO production in LPS/IFN-$\gamma$-stimulated C6 cells. Overall, these results suggest that RRE elicits an antiproliferative property and differentially modulates NO production in various macrophages, and have a potential for therapeutic application.

• Bulletin of the Korean Chemical Society
• /
• 제31권10호
• /
• pp.2854-2860
• /
• 2010

Synthesis of a new series of pyrimidinyl-imidazo[2,1-b]thiazole derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the pyrimidinyl ring side chain was investigated. The biological results indicated that most of the newly synthesized compounds showed moderate activity against A375, compared with Sorafenib. Among all of these derivatives, the cyclic sulfamide derivatives IIIa, IIIb, and IIIe showed the most potent antiproliferative activity against A375 human melanoma cell line. The IC50 values of compounds IIIa,b were in nanomolar scale. In addition, compound IIIe ($IC_{50}=1.9\;{\mu}M$) also demonstrated more potent antiproliferative activity compared with Sorafenib ($IC_{50}=5.6\;{\mu}M$).

• 한국미생물·생명공학회지
• /
• 제50권2호
• /
• pp.218-227
• /
• 2022

Glycosylation of aesculetin was performed using amylosucrase from the hyperthermophilic bacterium Deinococcus geothermalis DSM 11300 to improve the solubility and biological activity of aesculetin. A newly synthesized aesculetin glycoside was identified as α-cichoriin (aesculetin 7-α-D-glucoside) by nuclear magnetic resonance analysis. The solubility of α-cichoriin was 11 times higher than that of aesculetin because of the attached glucose moiety. Aesculetin and α-cichoriin had no significant effect on the proliferation of normal cells, such as RAW 264.7, but they showed a cell proliferation inhibitory effect on B16F10 melanoma cells. Unlike treatment with aesculetin and α-cichoriin, aesculin (aesculetin 6-β-D-glucoside) showed no antiproliferative activity in B16F10 cells. Based on the molecular structures of aesculin and α-cichoriin, the position where glucose binds to aesculetin and the anomeric configuration between glucose and aesculetin are thought to be important for exerting an antiproliferative effect on the B16F10 cell line. Based on these results, we propose that α-cichoriin, the α-glycosylated form of aesculetin, may serve as a model for developing phytochemical analogs with therapeutic potential for the treatment of diseases associated with tumor cell proliferation without cytotoxicity to normal cells.

• 대한본초학회지
• /
• 제27권4호
• /
• pp.17-23
• /
• 2012

Objectives : Schisandrae Fructus (SF) has traditionally been used to balance level of body fluid and to strengthen kidney function. It has been reported that the SF extract has antioxidant, hepatoprotective, neuroprotective and anticancer effects. This study investigated an antiproliferative effect of SF extract on PC-3 human prostate cancer cells and analyzed active ingredients of SF extract qualitatively and quantitatively. Methods : We examined the antiproliferative effect of SF extract with MTT assay, DAPI staining and annexin-V/7-AAD double staining. The active ingredients of SF extract were identified by using HPTLC and HPLC/DAD system. Results : SF-chloroform fraction inhibited growth of PC-3 cells and changed the morphology of nucleus in a dose dependent manner. A dose-dependent apoptotic cell death was also measured by flow cytometry analysis. It was analyzed that SF-chloroform fraction contained more schizandrin than other fractions by using HPTLC and HPLC/DAD system. Conclusions : These results suggest that SF extract and schizandrin may be a potential chemotherapeutic agent for the control of PC-3 human prostate cancer cells.

• Bulletin of the Korean Chemical Society
• /
• 제32권3호
• /
• pp.821-828
• /
• 2011

Design and synthesis of new 3,4-diarylpyrazole-1-carboxamide derivatives are described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The pharmacological results indicated that most of the synthesized compounds showed moderate activity against A375, compared with Sorafenib. On the other hand, compounds Ia, Ie, IIb, and IIh were more potent than Sorafenib. In addition, compound IIa was equipotent to Sorafenib. Among all of these derivatives, compound IIb which has diethylamino and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line. Virtual screening was carried out through docking of the most potent compound IIb into the domain of V600E-b-Raf and the binding mode was studied.

• 약학회지
• /
• 제55권2호
• /
• pp.116-120
• /
• 2011

Abnormal proliferation of vascular smooth muscle cells (VSMCs) plays an important role in the development and progression of proliferative cardiovascular diseases, including hypertension and atherosclerosis. To find antiproliferative agent (A)-8 had inhibitory effect on VSMCs proliferation. Therefore, we examined the antiproliferative effect of A-8, a newly synthesized obovatol derivative. To investigate the antiproliferative effect of A-8, we examined cell counting and [$^3H$]-thymidine incorporation assays. The pre-incubation of A-8 (1~4 ${\mu}M$) significantly inhibited proliferation and DNA synthesis of 5% fetal bovine serum (FBS)-stimulated rat aortic VSMCs in concentration-dependent manner. Whereas, A-8 did not show any cytotoxicity in rat aortic VSMCs in this experimental condition by WST-1 assay. In addition, A-8 significantly inhibited 5% FBS-induced cell cycle progression in rat aortic VSMCs. These results show that A-8 may be developed as a potential antiproliferative agent for treatment of angioplasty restenosis and atherosclerosis. Furthermore, A-8 should be examined for further clinical application either as a single agent or in combination with other angioplasty restenosis or atherosclerosis agents.

• Journal of Ginseng Research
• /
• 제39권3호
• /
• pp.274-278
• /
• 2015

Background: Steaming of ginseng is known to change its chemical composition and biological activity. This study was carried out to investigate the effect of different steaming time-scales on chemical constituents and antiproliferative activity of Vietnamese ginseng (VG). Methods: VG was steamed at $105^{\circ}C$ for 2-20 h. Its saponin constituents and antiproliferative activity were studied. The similarity of chemical compositions between steamed samples at $105^{\circ}C$ and $120^{\circ}C$ were compared. Results: Most protopanaxadiol and protopanaxatriol ginsenosides lost the sugar moiety at the C-20 position with 10-14 h steaming at $105^{\circ}C$ and changed to their less polar analogues. However, ocotillol (OCT) ginsenosides were reasonably stable to steaming process. Antiproliferative activity against A549 lung cancer cells was increased on steaming and reached its plateau after 12 h steaming. Conclusion: Steaming VG at $105^{\circ}C$ showed a similar tendency of chemical degradation to the steaming VG at $120^{\circ}C$ except the slower rate of reaction. Its rate was about one-third of the steaming at $120^{\circ}C$.

• Bulletin of the Korean Chemical Society
• /
• 제30권9호
• /
• pp.2027-2031
• /
• 2009

The synthesis of a new series of diarylureas and amides having a 1-substituted-3-(3-chloro-5-methoxyphenyl)-4- pyridinylpyrazole scaffold is reported here. The in vitro antiproliferative activities of these diaryl derivatives against human melanoma cell line A375 were tested and the effect of substituents on the phenyl ring was investigated. Most of the newly synthesized compounds generally showed superior or similiar activity against A375 to Sorafenib. Among these compounds, IId, IIg and IIh showed excellent activity against A375 compared to Sorafenib.

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

• 치위생과학회지
• /
• 제7권1호
• /
• pp.31-35
• /
• 2007

Caesalpinia sappan L. (Leguminosae) is an oriental medicinal herb distributed in China and Taiwan, and its heartwood has been traditionally used as an analgesic, a therapy for thrombosis or tumor. This study was to investigate the proliferation and inhibition effects of Caesalpinia sappan extracts against human epithelial cell and cancer cell lines. The methanol extract of dried C. sappan heartwood was evaporated (KS-6), and then sequentially extracted by hexane (KS-01), chloroform (KS-02), ethyl acetate (KS-03), n-butanol (KS-04), and water (KS-05). After 48 hr of exposure, these fractions at a concentration of $50{\mu}g/ml$ significantly increased, and reduced cell proliferation in both human normal epithelial and cancer cell lines. The ethyl acetate fraction (KS-03) among organic solvent fractions was 120.2% of the most proliferation activity ($50{\mu}g/ml$) against HaCaT human epithelial cell. However, fractions from chloroform, butanolic and methanolic extract had 7.2, 28.7 and 20.8% of antiproliferative effect on HaCaT cell, respectively. In cell proliferation effects of C. sappan extract on HeLa, SiHa and C33A human cervical cancer cells, chloroform fraction (KS-2) was the most antiproliferative activity, its antiproliferative rate (dosage, $50{\mu}g/ml$) relative to control was 25.8, 12.2 and 17.4% for SiHa, HeLa and C33A, respectively. The results indicated that the six extract fractions could induce cell cycle stimulate or arrest in some way. Finally, further investigation is needed to assess the molecular mechanisms mediated anticancer activities of this plant.