• Bulletin of the Korean Chemical Society
• /
• v.30 no.7
• /
• pp.1463-1469
• /
• 2009

Eleven novel oxiranyl and thiiranyl phenolic compounds were synthesized as potential antitumor agents using epichlorohydrin and epithiohydrin in the presence of $K_2CO_3$. Cytotoxicities were found in range of I$C_{50}$ values of 2.5-14.8 $\mu$M, which was partially attributed to topoisomerase II inhibition. Bis-thiiranyl anthraquinone analog, 19 showed more cytotoxicity against MDA-MB-231 (breast cancer cell) and PC3 (prostate cancer cell) after 24 and/or 48 h and more potent topoisomerase II inhibitory activity than etoposide.

• Journal of Life Science
• /
• v.23 no.11
• /
• pp.1388-1396
• /
• 2013

This study used an S-180 cell-injected mouse model to evaluate the antitumor effects of the acute and subacute toxicity of Keumsa (Phellinus linteus) extract intravenously administrated in ICR mice. When administered intravenously (31.3-250 mg/kg body weight), Keumsa (Phellinus linteus) extract significantly inhibited the growth of the solid tumor cell. The antitumor activity of Keumsa (Phellinus linteus) extract increased in a dose-dependent manner. The highest dose (250 mg/kg body weight) was highly effective, reducing tumor formation by 42.7% compared with the control group. In the acute toxicity test, $LD_{50}$ of the Keumsa (Phellinus linteus) extract showed 632.84 mg/kg (♂) and 814.48 mg/kg (♀) after intravenous administration. In addition, liver and spleen weight were increased in a dose-dependent manner. In the subacute toxicity test, the mice were intravenously administered over the course of 28 days. The $LD_{50}$ of the Keumsa (Phellinus linteus) extract showed 355.41 mg/kg (♂) and 383.53 mg/kg (♀) after intravenous administration. The liver and spleen weight also increased in a dose-dependent manner. In the case of the group that received more than 125 mg/kg of intravenous administration, exercise capacity, such as jumping ability and agility, were significantly increased. These results suggest that Keumsa (Phellinus linteus) extract can be regarded as a potent enhancer of the innate immune response, and it can be considered as a new natural product with low toxicity that may be used as a candidate for antitumor action.

• Proceedings of the Ginseng society Conference
• /
• 1990.06a
• /
• pp.102-110
• /
• 1990

Antitumor polyacetylenlc alcohol, panaxytriol (Ci7 H2603), was isolated and purified from a Powder of the root of Panax ginseng C.A. Meyer. Panaxytriol Possesses unusual Property of being soluble in both water and organic solvents. Panaxytriol inhibited the growth of various kinds of human cultured cell lines in dose-dependent fashion in vitro. The in vivo effects of panaxytriol were tested against C57BU6 mice transplanted with Bl6 melanomas. Panaxytriol (8 and 40 mg/kg) administered intramuscularly (im) produced significant tumor growth delays in mice. Although a detailed mechanism of growth inhibition by panaxytriol is unknown, preliminary results appear to implicate a surface membrane site of action. And its action seems to be more dose-dependent than time-dependent. Finally, panaxytriol pharmacokinetics was evaluated in mice given single 8 mgrkg doses intraperitoneally(ip) or im. Serum panaxytriol content was measured using both tumor growth inhibitory assay and a gas chromatographic method. The maximum serum panaxytriol content after ip and im administration was 35.0 and 1.61 ug/ml respectively. These results indicate that the compound may act as cytotoxic substance even in-patients. Keywords Panax ginseng, panaxytriol, tumor growth inhibition

• Journal of Ginseng Research
• /
• v.14 no.2
• /
• pp.244-252
• /
• 1990

Antitumor polyacetylenic alcohol, panaxytriol (Cl7 H26O3), was isolated and purified from a powder of the root of Pnnnx tin.1.encl C.A. Meyer. Panaxytriol possesses unusual property of being soluble in both water and organic solvents. Panaxytriol inhibited the growth of various kinds of human cultured cell lines in dose-dependent fashion in vitro. The in vivo effects of panaxytriol were tested against C57BL/6 mice transplanted with Bl6 melanomas. Panaxytriol (8 and 40 mg/kg) administered intra-muscularly(im) produced significant tumor growth delays in mice. Although a detailed mechanism of growth inhibition by panaxytriol is unknown, preliminary results appear to implicates a surface membrane site of action. And its action seems to be more dose-dependent than time-dependent. Finally, panaxytriol pharmacokinetics was evaluated in mice given single 8 mg/kg doses intraperitoneally (ip) or im. Serum panaxytriol content was measured using both tumor growth inhibitory assay and a gas chromatographic method. The maximum serum panaxytriol content after ip and im administration was 35.0 and 1.6 $\mu$g/ml respectively. These results indicate that the compound may act as cytotoxic substance even in patients.

• Korean Journal of Plant Resources
• /
• v.33 no.3
• /
• pp.183-193
• /
• 2020

Recently, as a natural substance has been emphasized interest in research to enhance the immune function. Green lettuce (Lactuca sativa L.) is a popular vegetable used fresh and it contains various phytochemicals and antioxidant compounds, and has been reported to have various physiological activities such as antibacterial, antioxidant, antitumor and anti-mutagenic. However, only a few studies have investigated on the mechanism of action of immune-enhancing activity of lettuce. Therefore, in this study, the immunomodulatory activities and potential mechanism of action of Green lettuce extracts (GLE) were evaluated in the murine macrophage cell line RAW264.7. GLE significantly increased NO levels by RAW264.7 cells, as well as expressions of immunomodulators such as iNOS, COX-2, IL-1β, IL-6, IL-12, TNF-α and MCP-1. Although GLE activated ERK1/2, p38, JNK and NF-κB, GLE-mediated expressions of immunomodulators was dependent on p38, JNK and NF-κB. In addition, TLR4 inhibition blocked GLE-mediated expressions of immunomodulators and activation of p38, JNK and NF-κB. Taken together, these results demonstrated that TLR4-MAPK/NF-κB signalling pathways participated in GLE-induced macrophage activation and GLE could be developed as a potential immunomodulating functional food.

• Korean Journal of Pharmacognosy
• /
• v.29 no.4
• /
• pp.331-337
• /
• 1998

Most Annonaceous acetogenins are potently bioactive and offer exciting potential as new antitumor, pesticidal and other bioactivites. The major mode of action of the acetogenin is inhibition of electron transport in the mitochodria. Two known cytotoxic ketolactone Annonaceous acetogenins, (2,4-cis)-isoannonacin (compound 1) and (2,4-trans)-isoannonacin (compound 2), have been isolated from Asimina triloba (Annonaceae) by bioactivity directed fractionation. The structures were characterized on the basis of chemical and spectral data. Compounds 1 and 2, which are known but are first isolated from the seeds of this species, were ob-tained. In brine shrimp lethality test (BST), 1 and 2 exhibited cytotoxicity.

• Proceedings of the PSK Conference
• /
• 2003.04a
• /
• pp.245.3-246
• /
• 2003

S-Adenosylhomocysteine hydrolase (SAH) catalyzes the hydrolysis of S-adenosylhomocysteine to adenosine and L-homocysteine and has been an attractive target for the development of broad spectrum antiviral agents. Based on the potent inhibitory activity of neplanocin A against SAH, we have reported the synthesis and novel mechanism of action of fluoro-neplanocin A. (omitted)

• Proceedings of the Korean Society of Applied Pharmacology
• /
• 2003.11a
• /
• pp.86-86
• /
• 2003

In a continuous effort to develop novel anticancer agents we newly synthesized and evaluated the antitumor activity of nucleoside analogues. One analogue, 4 - ［2-Chlor-6- (3-iodo- benzy lamino) -purin -9-yl］- 2,3-dihydroxy-cyclopentanecarbo xylic acid methylamide (LJ-331), has been shown to exert a potent inhibition of human cancer cell growth in vitro including human lung (A549), stomach (SNU-638) and leukemia (HL-60) cancer cells. Following mechanism of action study revealed that LJ - 331induces cell cycle arrest at the G1 phase in HL-60 cells and evokes apoptotic phenomena such as an increase in DNA ladder intensity and chromatin condensation by a dose- and time-dependent manner. LJ-331 also activated the caspase-3 activity in HL-60. This result suggests that the growth inhibition of human cancer cells by LJ-331 might be related to the cell cycle arrest and induction of apoptosis.

• Journal of Ginseng Research
• /
• v.33 no.3
• /
• pp.165-176
• /
• 2009

Korean ginseng, which contains ginsenosides and polysaccharides as its main constituents, is orally administered to humans. Ginsenosides and polysaccharides are not easily absorbed by the body through the intestines due to their hydrophilicity. Therefore, these constituents which include ginsenosides Rb1, Rb2, and Rc, inevitably come into contact with intestinal microflora in the alimentary tract and can be metabolized by intestinal microflora. Since most of the metabolites such as compound K and protopanaxatriol are nonpolar compared to the parental components, these metabolites are easily absorbed from the gastrointestinal tract. The absorbed metabolites may express pharmacological actions, such as antitumor, antidiabetic, anti-inflammatory, anti-allergic, and neuroprotective effects. However, the activities that metabolize these constituents to bioactive compounds differ significantly between individuals because all individuals possess characteristic indigenous strains of intestinal bacteria. Recently, ginseng has been fermented with enzymes or microbes to develop ginsengs that contain these metabolites. However, before using these enzymes and probiotics, their safety and biotransforming activity should be assessed. Intestinal microflora play an important role in the pharmacological action of orally administered ginseng.

• Biomolecules & Therapeutics
• /
• v.6 no.3
• /
• pp.303-311
• /
• 1998

The general pharmacological properties of new platinum (II) coordination complexes, SA : [Pt(trans-ι-DACH)(DPPE)] . 2NO$_3$, SB : [Pt(cia-DACH)(DPPP)] 2NO$_3$ and SC : [Pt(cia-DACH)(DPPE)] 2NO$_3$on central nervous, respiratory, cardiovascular and digestive systems were studied in various experimental animals. These platinum (II) anticancer agents had no effects on analgesia, thiopental-induced sleeping time, body temperature, strychnine-induced convulsion, inflammation and local anesthetic action in mice and rats. Intestinal motility, stomach-ulcer induced by serotonin and bile-secretion of rats were not influenced by the dose of 30 mg/kg. However SB and SC induced a mild decrease in heart rate in anesthetized rats. Based on these results, these new platinum (II) complexes may be regarded as a valuable lead compound in the development of new anticancer chemotherapeutic agents with marked antitumor activity and low toxicity.