• The Korean Journal of Physiology and Pharmacology
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• v.18 no.2
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• pp.109-120
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• 2014

The epothilones are a class of microtubule inhibitors that exhibit a strong antitumor activity. UTD2 is a novel epothilone analog generated by genetic manipulation of the polyketide biosynthetic gene cluster. This study investigated the effects of UTD2 on the actin cytoskeleton and its critical regulators, and the signaling pathways which are essential for cell motility, growth and survival in MCF-7 breast cancer cells. Results showed that UTD2 inhibited the cellular functions of actin cytoskeleton, such as wound-closure, migration and invasion, as well as adhesion. Our study further demonstrated that UTD2 suppressed Rac1 GTPase activation and reduced the activity of PAK1, which is a downstream effector of Rac1, while the activity of Cdc42 was not affected. Additionally, the phosphorylation of p38 and ERK were significantly inhibited, but the phosphorylation of JNK remained the same after UTD2 treatment. Moreover, UTD2 inhibited the activity and mRNA expression of MMP-2, which plays a key role in cell motility. UTD2 also reduced the phosphorylation of Akt, which is an important signaling kinase regulating the cell survival through Rac1. Furthermore, UTD2 interrupted the synergy between Rac1 and Raf in focus formation assays. Taken together, these results indicated that UTD2 exerted multiple effects on the actin cytoskeleton and signaling pathways associated with Rac1. This study provided novel insights into the molecular mechanism of the antineoplastic and antimetastatic activities of epothilones. Our findings also suggest that the signaling pathways regulated by Rac1 may be evaluated as biomarkers for the response to therapy in clinical trials of epothilones.

• Journal of Life Science
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• v.24 no.12
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• pp.1378-1382
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• 2014

Phospholipase D (PLD) catalyzes the hydrolysis of phospholipid to phosphatidic acid (PA), a lipid secondary messenger. Two forms of PLD isozymes, phosphatidylcholine-specific PLD1 and PLD2, have been identified. PLD has emerged as a critical regulator of cell proliferation and survival signaling, and dysregulation of PLD occurs in a various illnesses, including cancer. PLD activity is essential for cell survival and protection from apoptosis. Overexpression of PLD isozymes or PLD-generated PA attenuates the expression of apoptotic genes and confers resistance to apoptosis. The apoptosis-related molecular mechanisms of PLD remain largely unknown. Recently, the dynamics of PLD turnover during apoptosis have been reported. The cleavage of PLD isozymes as specific substrates of caspase differentially regulates apoptosis. PLD1 is cleaved at one internal site, and PLD2 is cleaved two sites at the front of the N-terminus. The cleavage of PLD1 reduces its enzymatic activity, probably via the dissociation of two catalytic motifs, whereas the cleavage of PLD2 does not affect the catalytic motifs and its activity. Thus, PLD2 maintains antiapoptotic capacity, despite its cleavage. Therefore, the differential cleavage pattern of PLD isozymes by caspase affects its enzymatic activity and antiapoptotic function. Thus, PLD is considered a potential target for cancer therapy. We summarize recent studies regarding the functional role of PLD in apoptosis.

• Korean Journal of Acupuncture
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• v.18 no.1
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• pp.1-9
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• 2001

Artemisia asiatica Nakai aqua-acupuncture solution (ANAS) was administered once daily for 10 days before the tumor implantation ($1{\times}10^6\;cells$). Body weight, spleen weight and the number of ascitic tumor cells were measured at 6 days after tumor implantation. The change of body weight and the survival rate of mice were observed for 21 days. It was used three biomarkers (quinone reductase, glutathione, glutathione S-transferase) to test chemopreventive potentials of ANAS. ANAS exerted antitumor activity by inhibiting the growth of Ehrlich ascites tumor cells in vivo. Mice given Ehrlich cells and ANAS at $CV_{12}$ and $BL_{18}$ had 57.1% to 49.2% survival after 21 days. Quinone reductase activity and glutathione levels were increased with ANAS. However, glutathione S-transferase level was 1.1-fold with ANAS. These results suggest that ANAS has chemopreventive potential by inducing QR activity and increasing GSH level.

• Journal of Pharmacopuncture
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• v.14 no.1
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• pp.25-33
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• 2011

Objective : We investigate toxicity of Aconiti ciliare tuber and antioxidant activity of Aconiti ciliare tuber Pharmacopuncture to develop safe Aconiti ciliare tuber Pharmacopuncture and find out the effect. Methods : In order to investigate toxicity of Aconiti ciliare tuberm, we administered Aconiti ciliare tuberm orally to rats and examined the survival rate, comparing with the survival rate of rats administered by Radix aconitum simmered with Semen Glycine and Radix Glycyrrhizae. We examined the in vitro biological activity of Aconiti ciliare tuber Pharmacopuncture, including the total polyphenol content, and ABTS radical scavenging. Results and Conclusions : The $LD_{50}$ of Radix aconitum simmered with Semen Glycine and Radix Glycyrrhizae was 9.0g/kg, on the other hand, the $LD_{50}$ of Aconiti ciliare tuberm was more than 15g/kg. The total polyphenol contents of Aconiti ciliare tuberm Pharmacopuncture was 2.31mg/L. The 2,2'-azinobis-3-ehtlbezothiazoline-6-sulfonic acid radical decolorization (ABTS) was 10.26%. We conclude that Aconiti ciliare tuberm is not highly toxic, Aconiti ciliare tuber Pharmacopuncture has a little antioxidant effect.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2022.09a
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• pp.95-95
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• 2022

Kadsura heteroclita (Roxb.) Craib and Eichhornia crassipes (Mart.) Solms. have been known to give effects on pimple. Jatropha gossypiifolia L., Anisomeles indica (L.) Kuntze, Kadsura heteroclita (Roxb.) Craib extracts have been used for cough cold for a long time. To test whether Jatropha, Anisomeles, Kadsura and Eichhornia have anti-oxidant acitivity, we performed DPPH assay. Jatropha showed 91.98% anti-oxidant activity and Anisomeles, Eichhornia and Kasuda showed 47.91%, 47.35% and 32.00% anti-oxidant activity, respectively, compared to Ascorbic acid control. To further determine whether these extracts have any cytotoxic effects, we used MTT assay with these extracts in Raw264.7 cells. Jatropha showed 45.10% survival rate and Anisomeles, Eichhornia and Kasuda showed 76.78%, 86.24% and 82.88% survival rate, respectively, compared to negative control. Taken together, these results suggest that Jatropha showed higher anti-oxidant activity than other plant extracts, however it has cytotoxic effect. Therefore, we consider Anisomeles, Eichhornia and Kasuda extracts might be a good candidate to develop as a therapeutic agent with higher anti-oxidant acitivity and lower cytotoxic effects among the tested plant extracts.

• Journal of Nutrition and Health
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• v.26 no.4
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• pp.379-389
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• 1993

Several studies have shown that extracts from yellow-green vegetables reveal antitumor activities. In the present study we investigated the effect of phytol in order to elucidate the immunological mechanism of antitumor activity of this substance. The results obtained from the experiment as follows: 1) Phytol showed cytotoxic effect on sarcoma 180 cells in vitro. 2) When phytol was injected into the peritoneal cavity of mice transplanted with sarcoma 180 cells, the average survival time (24.0 days) tended to increase as compared with the nontreated control (19.2 days). 3) When sarcoma 180 cells were injected subcutaneously into the right groin of mice, and then phytol was injected into the peritoneal cavity, the tumor inhibition ratio was 33%. 4) The natural killer(NK) cell activity was significantly augmented by phytol in vitro and in vivo. Similar augmentations of NK cell activity were obtained with culture supernatants of phytol exposed spleen cells and peripheral blood mononuiclear cells. 5) Phytol on the macrophage from peritoneal cavity showed a higher effectiveness in vivo than in vitro. These results indicate that phytol shows the inhibitory effect for growth of sarcoma 180 cells in vitro, also it can augment macrophage and NK cell activities in vivo.

• Journal of the Korean Society of Food Science and Nutrition
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• v.30 no.2
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• pp.372-376
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• 2001

The effect of garlic extract and vitamin C mixture on the various cancer cell lines in vitro and in vivo have been examined. Proliferation of human colon cancer (HT-29), human rectal cancer (HRT-18) and human hepatoma (HepG2) cells was inhibited by garlic extract and vitamin C, respectively. Based on the cytotoxic activity, mixture of garlic extract and vitamin C was demonstrated to possess a synergistic growth inhibition on HT-29, HRT-18 and HepG2 cancer cells. Mixture of garlic extract and vitamin C significantly arrested G2/M phase cells in the HepG2 cell cycle. Oral administration of mixture of garlic extract and vitamin C to sarcoma-180 tumor-bearing mice prolonged survival time compared to that of control group. These results suggested that addition of vitamin C enhances anticancer activity of garlic extract in vitro, and mixture of garlic extract and vitamin C has antitumor effect in vivo.

• Journal of Veterinary Clinics
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• v.15 no.1
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• pp.36-40
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• 1998

This experiment was carried out in order to evaluate the immunomodulatory activity of levamisole (LMS) in 5. fgrjn challenged eels with different treatment regimens: 7-day LMS treatment before the challenge, 7-day LMS treatment started simultaneously with the challenge, 14-day treatment before and after the challenge. The antibacterial effect was activated in all treated groups, with the best being obtained in the simultaneously treated group. LMS stimulated the defense mechanisms of the eel as demonstrated by increase in the level of total protein, albumin, trypsin inhibitor capacity, lysozyme activity, antibody titers antibacterial activity and survival rate. These results suggest that antibacterial effects of LMS was achieved by not only non-specific immune response but also specific one in eel.

• YAKHAK HOEJI
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• v.24 no.2
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• pp.123-134
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• 1980

A new glycoside was isolated from Acanthopanax chiisanensis Nakai (Araliaceae) leaves and its biological activity was investigated. The new glycoside was tentatively assigned the structure of Asecotriterpenoid glycoside, $C_{48}H_{76}O_{19}$ m.p. $208~209^{\circ}$ and named chiisanoside. Chiisanoside exhibited non-toxic effects and significant antihistaminic activity. It was found that chiisanoside showed the antidiabetic activity against epinehrine-and alloxan-induced diabetes, decreased the toxicity of $LD_{50}$ by ephedrine hydrochloride and promoted the elimination of chloramphenicol from blood. Chiisanoside also increased the survival rate in rats intoxicated by carbon tetrachloride from death and led to re-establishment of normal enzymatic function. In the histopathological studies, chiisanoside improved fatty degeneration and parenchymal cell necrosis of the liver induced by carbon tetrachloride in rats.

• The Korean Journal of Malacology
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• v.26 no.4
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• pp.255-260
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• 2010

This study was conducted to investigate protocol standardization for spermatozoa cryopreservation of the Scapharca broughtonii (Schrenck). Among the freezing rates, freezing at a height of 2 cm above liquid nitrogen surface for 5 minute gave higher activity and survival rate. Among the various diluents, Ringer's solution was the best for S. broughtonii sperm cryopreservation. The suitability of cryoprotectants dimethylsulfoxide (DMSO), dimethylacetamide (DMA), glycerol and methanol were tested against three freezing rates. DMSO gave significantly higher activity and survival rates than others.