• Proceedings of the PSK Conference
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• 2002.10a
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• pp.245.2-246
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• 2002

We studied on the antiproliferative effects of bile acids and their derivatives on HepG2 human hepatocellular carcinoma cells. Ursodeoxycholic acid (UDCA) and its synthetic derivative HS-1030. and chenodeoxycholic acid (CDCA) and its synthetic derivatives. HS-1199 and HS\ulcorner200, were used. We focused on the regulation of cell cycle and induction of apoptosis by these bile acid derivatives. (omitted)

• YAKHAK HOEJI
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• v.41 no.1
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• pp.94-98
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• 1997

Ceramide. a product of sphingomyelin hydrolysis, has been proposed as a lipid second messenger mediating antiproliferative activation. In this study, we examined the role of the cell cycle-related proteins in the ceramide-mediated growth suppression. Treatment of U-937 cells with C$_2$-ceramide(N-acetylsphingosine) resulted in growth suppression in a time- and concentration dependent manner. Ceramide induced concentration dependent dephosphorylation of retinoblastoma gene product (Rb). Rb remains hypophosphorylated in synchronized cells even after serum stimulation in the presence of ceramide. Ceramide decreased the expression of cyclin D$_1$ and cyclin E levels. These results suggest that antiproliferative effect of ceramide is associated with hypophosphorylation of Rb and decreased expression of cyclin D1 and cyclin E.

• Journal of Ginseng Research
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• v.17 no.3
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• pp.196-202
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• 1993

A study was performed to compare the anticancer effects of Korean and Chinese red ginseng roots. The whole crude extracts or chloroform, methanol and acetone fractions of the crude extracts were added in the culture medium of three cancer cell lines, a mouse leukemia cell line ($P_{388}$), a human colon carcinoma cell line (HT-29) and a human rectal carcinoma cell line (HRT-18), to screen the growth inhibition effects. The results are summarized as follows : 1. Crude extracts of both Korean and Chinese red ginseng roots inhibited the proliferation of all the three cancer cell lines tested in a dose dependent manner. However, the growth inhibition effects of Korean red ginseng extracts were significantly greater than that of Chinese red ginseng. 2. An acetone fraction showed the greatest antiproliferative effects among the 11'hole crude extracts, chloroform, methanol and acetone fractions of the crude extracts. 3. These results suggest that the active antiproliferative components of the crude extracts are present mostly in the acetone fraction.

• Bulletin of the Korean Chemical Society
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• v.33 no.11
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• pp.3635-3639
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• 2012

A series of new diarylureas possessing aminoisoquinoline scaffold was synthesized, and their in vitro antiproliferative activity against A375P human melanoma cell line was tested. Compounds 1d, 1l, 1n, 1p, 1q, and 1t showed superior potency against A375P to Sorafenib. The highest potency was shown by compound 1p possessing 3,5-bis(trifluoromethyl)phenyl terminal ring with $IC_{50}$ value of $0.41{\mu}M$.

• Bulletin of the Korean Chemical Society
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• v.34 no.8
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• pp.2480-2486
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• 2013

A new series of diarylamides and diarylureas having 2,3-dihydropyrrolo[3,2-b]quinoline scaffold was synthesized. Their in vitro antiproliferative activities were tested over NCI-60 cancer cell lines of nine different cancer types. Some target compounds showed good inhibition percentages over different cell lines. Among all the target compounds, compound 1f possessing 6,7-dimethoxy-2,3-dihydropyrrolo[3,2-b]quinoline nucleus, amide linker, and 4-chloro-3-(trifluoromethyl)phenyl terminal ring showed high selectivity against MCF7 and MDA-MB-468 breast cancer cell lines more than the other tested cell lines. Its inhibition percentages at $10{\mu}M$ concentration over those two cell lines were 84.97% and 87.13%, respectively.

• Journal of Ginseng Research
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• v.19 no.2
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• pp.114-116
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• 1995

Panax ginseng ginsenosides were examined for their affects on the DNA synthesis. The DNA 1 synthesis was measured by the thymidine incorporation into NIH3T3 cells. The ginsenoside, panaxytriol, $Rh_1$ and $Rh_2$ showed reduced [$^{3}H$]-thymidine incorporation. However, other ginsenosides of $Rh_1$, $Rh_2$ and $Rh_3$ did not inhibit DNA synthesis. Among the various ginsenosides, ginsenoside $Rh_2$ was found to be the most inhibitory on DNA synthesis. We suggest $Rh_2$ as one of the potential choice of antiproliferative drugs.

• Journal of Ginseng Research
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• v.38 no.2
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• pp.154-159
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• 2014

Background: This study was carried out to investigate the effect of the steaming process on chemical constituents, free radical scavenging activity, and antiproliferative effect of Vietnamese ginseng. Methods: Samples of powdered Vietnamese ginseng were steamed at $120^{\circ}C$ for various times and thei extracts were subjected to chemical and biological studies. Results: Upon steaming, contents of polar ginsenosides, such as Rb1, Rc, Rd, Re, and Rg1, were rapidly decreased, whereas less polar ginsenosides such as Rg3, Rg5, Rk1, Rk3, and Rh4 were increased as reported previously. However, ocotillol type saponins, which have no glycosyl moiety at the C-20 position, were relatively stable on steaming. The radical scavenging activity was increased continuously up to 20 h of steaming. Similarly, the antiproliferative activity against A549 lung cancer cells was also increased. Conclusion: It seems that the antiproliferative activity is closely related to the contents of ginsenoside Rg3, Rg5, and Rk1.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.16
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• pp.7053-7060
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• 2015

In the present work, novel orange peel was extracted with 100%EtOH (ethanol) and fractionated into four fractions namely F1, F2, F3, F4 which were eluted from paper chromatographs using 100%EtOH, 80%EtOH, 50%EtOH and pure water respectively. The crude extract and its four fractions were evaluated for their total polyphenol content (TPC), total flavonoid content (TFC) and radical scavenging activity using DPPH (1,1-diphenyl-2-picrylhydrazyl) assay. Their cytotoxic activity using WST assay and DNA damage by agarose gel electrophoresis were also evaluated in a human leukemia HL-60 cell line. The findings revealed that F4 had the highest TPC followed by crude extract, F2, F3 and F1. However, the crude extract had the highest TFC followed by F4, F3, F2, and F1. Depending on the values of $EC_{50}$ and trolox equivalent antioxidant capacity, F4 possessed the strongest antioxidant activity while F1 and F2 displayed weak antioxidant activity. Further, incubation HL-60 cells with extract/fractions for 24h caused an inhibition of cell viability in a concentration-dependent manner. F3 and F4 exhibited a high antiproliferative activity with a narrow range of $IC_{50}$ values ($45.9-48.9{\mu}g/ml$). Crude extract exhibited the weakest antiproliferative activity with an $IC_{50}$ value of $314.89{\mu}g/ml$. Analysis of DNA fragmentation displayed DNA degradation in the form of a smear-type pattern upon agarose gel after incubation of HL-60 cells with F3 and F4 for 6 h. Overall, F3 and F4 appear to be good sources of phytochemicals with antioxidant and potential anticancer activities.

• Advances in Traditional Medicine
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• v.6 no.4
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• pp.286-292
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• 2006

In this study, we evaluated the antiproliferative effects of Panax notoginseng, ginsenoside Rb1, and notoginsenoside R1 in the human breast carcinoma MCF-7 cell line. Our results indicated that both Panax notoginseng radix extract (NRE) and Panax notoginseng rhizoma extract (NRhE) possess significant antiproliferative activities in MCF-7 cells. Compared to control group (100%), at the concentrations of 0.05, 0.5, and 1.0 mg/ml NRE, cell growth was concentration-dependently reduced to 81.0 ${\pm}$ 6.1 (P < 0.01), 34.2 ${\pm}$ 4.8 (P < 0.001), and 19.3 ${\pm}$ 1.9 (P < 0.001), respectively. Similar results with NRhE at concentrations of 0.5 and 1.0 mg/ml were obtained in these MCF-7 cells. To identify the responsible chemical constituent, we tested the antiproliferation effects of two representative saponins, ginsenoside Rb1 and notoginsenoside R1, on the MCF-7 cells. The data showed that ginsenoside Rb1 was endowed with antiproliferative properties, while notoginsenoside R1 did not have an inhibitory effect in the concentrations tested. Our studies provided evidence that Panax notoginseng extracts and ginsenoside Rb1 may be beneficial, as adjuvants, in the treatment of human breast carcinoma.

• Food Science and Biotechnology
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• v.15 no.6
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• pp.914-919
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• 2006

We investigated the catechin content in green tea leaf (GTL) and green tea seed (GTS), the antiproliferative and detoxifying phase II enzyme-inducing activities of the methanolic (80%, v/v) extracts from GTL and GTS. GTL and GTS contained $8,685{\pm}1,061$ and $108{\pm}32\;{\mu}g/g$ epigallocatechin gallate (EGCG), $11,486{\pm}506$ and $116{\pm}72\;{\mu}g/g$ epigallocatechin (EGC), $3,535{\pm}308$ and $821{\pm}95\;{\mu}g/g$ epicatechin gallate (ECG), and $1,429{\pm}177$ and $37{\pm}44\;{\mu}g/g$ epicatechin (EC), respectively. The methanolic extract of GTS showed a greater increase in quinone reductase activity and antiproliferation potential against mouse hepatoma cells than GTL extract did. GTS treatment resulted in the accumulation at sub-G1 phase of mouse hepatoma hepa1c1c7 cells as assessed by flow cytometry. Enhancement of phase II enzyme activity by GTS extract was shown to be mediated, directly or indirectly, via interaction with the antioxidant response element (ARE) sequence in the genes encoding the phase enzymes. As the catechin content in GTS was significantly lower than that in GTL, components other than catechins appear to be responsible for the anticarcinogenic activity of the seed. In summary, these results suggest that the 80% methanolic extract of GTS deserves further study to evaluate its potential as an anticarcinogenic agent and to investigate its mechanism of action.