• Title/Summary/Keyword: Cytoxicity

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Haloacetylshikonin Derivatives : Synthesis and Evaluation of Antitumor Activity (할로아세틸시코닌 유도체의 합성 및 항암성 평가)

  • Zheng, Xiang-Guo;Jin, Guang-Zhu;Song, Gyu-Yong;Cho, Hoon;Ahn, Byung-Zun
    • YAKHAK HOEJI
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    • v.42 no.2
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    • pp.159-164
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    • 1998
  • The secondary hydroxy group at side chain of shikonin structure was selectively acylated with various haloacetic acids in presence of dicyclohexylcarbodiimide and 4-dimethylamin opyridine to produce haloacetylshikonin derivatives. The cytotoxicity of monohaloacetylshikonin derivatives against L1210 cells increased in the following order; monochloroacetylshikonin ($ED_{50}$, 0.142${\mu}$g/ml) > monobromoacetylshikonin ($ED_{50}$. 0.158${\mu}$g/ml) > monoiodoacetylshikonin ($ED_{50}$, 0.173${\mu}$g/ml). Introduction of larger halogen atoms decreased the cytotoxic activity, presumably due to steric hinderance. The cytotoxicity of chloroacetylshikonin derivatives was dependent on the number of chlorine atom, thus increasing in the following order; trichloroacetylshikonin (0.032${\mu}$g/ml) > dichloroacetylshikonin (0.059${\mu}$g/ml) > monochloroacetylshikonin ($ED_{50}$, 0.142${\mu}$g/ml). Thus, the electron withdrawing effect seems to be important for the cytotoxicity of chloroacetylshikonin derivatives. Consistent with the above, dichloroacetylshikonin (T/C. 182%) and trifluoroacetylshikonin (195%) showed higher T/C values than monochloroacetyl-(T/C, 122%), monobromoacetyl-(T/C, 154%) and monoiodoacetylshikonin (T/C, 117%) derivatives. Haloacetylshikonin derivatives showing lower cytoxic activities against L1210 cells exhibited lower T/C values. It seems that there is a relationship between the cytoxicity of haloacetylshikonin and their antitumor activity.

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Studies on the Immuno Modulating Acitivity of Fermented Artemisiae Argyi Folium Extract (애엽(艾葉) 발효 추출물의 면역활성에 관한 연구)

  • Han, Hyo-Sang;Park, Wan-Su;Lee, Young-Jong
    • The Korea Journal of Herbology
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    • v.23 no.3
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    • pp.103-112
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    • 2008
  • Objectives : This research aimed to study the cytotoxicity and immuno modulating activity of fermented Artemisia argyi Lev. et Vant.(Compositae). Methods : Effect of fermented Artemisiae Argyi Folium extracts, which were fermented by Sacchromyces cerevisiae STV89(AFS), on cell viability, generation of ROS within cells, generation of NO and the level of cytokines($TNF-{\alpha}$ and IL-6) was measured using mouse macrophage RAW 264.7 cell. Results : 1. Result of MTT assay conducted to verify the cytotoxicity of fermented Artemisiae argyi folium extract illustrated that, when fermented Artemisiae argyi folium extract was processed for each concentration, there was no excessive induction of cytoxicity in the RAW 264.7 cell. 2. Fermented Artemisiae Argyi Folium extract increased the generation of H2O2 within RAW 264.7 cell as well as significantly increased inhibition of generation of H2O2 in macrophage induced by LPS. 3. Fermented Artemisiae Argyi Folium extract inhibited generation of NO in RAW 264.7 cell, and significantly inhibited increase in generation of NO of macrophage induced by LPS. 4. Fermented Artemisiae Argyi Folium extract, AFS has significantly reduced the increase in the generation of $TNF-{\alpha}$ above 10 ${\mu}g/mL$. 5. Fermented Artemisiae Argyi Folium extract, AFS has significantly reduced the increase in generation of IL-6 above 50 ${\mu}g/mL$. Conclusions : AFS fermented extract produced from Artemisiae Argyi Flium, have increased generation of ROS and reduced generation of NO in RAW 264.7 cell without excessively inducing cytotoxicity of RAW 264.7 cell. In addition, they displayed significant immuno modulating activities including inhibition of generation of $TNF-{\alpha}$ and IL-6 in macrophage, induced by LPS.

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The Inhibitory Effect of Leek (Buchu) Kimchi Extracts on MCA-induced Cytoxicity and Transformation in C3H-10T1/2 Cells

  • Jung, Keun-Ok;Park, Kun-Young
    • Preventive Nutrition and Food Science
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    • v.4 no.4
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    • pp.255-259
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    • 1999
  • The anticarcinogenic effects of the methanol extracts from leek (buchu in Korean) kimchi and Korean cabbage kimchi were evaluated using cytotoxicity and transformation tests in C3H/10T1/2 cells. Various fractions of the 6-day fermented leek kimchi at 15$^{\circ}C$, hexane, methanol soluble, dichloromethane, ethyl acetate, butanol and aqueous fraction, were also studied in the same system. The inhibitory effect of the leek kimchi(6-day fermented at 15$^{\circ}C$, pH 4.29) was higher than that of the Korean cabbage kimchi(4-day fermented at 15$^{\circ}C$, pH 4.21) on the cytotoxicity induced by 3-methylcholanthrane (MCA) in the C3H/10T1/2 cell system. While the MCA-treated culture(control) formed 21.0 foci of type II plus III in C3H/10T1/2 cells, 100$\mu\textrm{g}$/ml of the methanol extract of the leek kimchi and that of the 4-day fermented Korean cabbage kimchi treated cultures reduced the formation of type II plus III foci to 7.4 and 11.3, respectively. Among the fractions of the leek kimchi, the dichloromethane fraction showed the highest inhibitory effect on MCA-induced cytotoxicity in C3H/10T1/2 cells. Fifty $\mu\textrm{g}$/ml of dichloromethane fraction from the leek kimchi suppressed the MCA-induced cytotoxicity by 77%. On the transformation test using MCA, the dichloromethane fraction considerably reduced the formation of type II plus III foci, especially thpe III foci. When 50$\mu\textrm{g}$/ml of dichloromethane fraction from the leek kimchi was treated, the numbers of type III foci mediated by MCA were decreased to 1.7 compared to 10 for the control. These results indicate that leek kimchi has stronger anticarcinogenic effects than Korean cabbage kimchi and that the dichloromethane fraction of the leek kimchi may contain the major compound(s) that suppress the carcinogenesis in the eukaryotic cells.

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Anti-inflammatory Activity of Herbal Extracts through Inhibition of TNF-α, IL-6 and IL-8 (TNF-α, IL-6, IL-8 저해를 통한 천연약용식물 추출물의 항염증 특성)

  • Kim, Yong-Soo;Gwon, Hui-Jeong;Park, Jong-Seok;Lim, Youn-Mook;Nho, Young-Chang
    • Journal of Radiation Industry
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    • v.5 no.3
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    • pp.273-277
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    • 2011
  • This study evaluated the cytotoxicity and anti-inflammatory activities of natural herbal extracts including Houttuynia cordata and Eucommia ulmoides against human mast cell (HMC-1). Houttuynia cordata (HC) and Eucommia ulmoides(EU) were extracted with distilled water (at $75^{\circ}C$) and then freeze-dried for 5 days. Finally, the mixture of HC and EU were sterilized by ${\gamma}$-rays irradiation. Cytotoxicity of the mixture against HMC-1 cell was measured using cell counting kit-8 (CCK-8) assay. In addition, inflammatory mediator cytokines such as TNF-${\alpha}$, IL-6 and IL-8 were evaluated by ELISA kit on the HMC-1 cells with calcimycin A23187 and phorbol 12-myristate 13-acetate (PMA). The results showed that mixture of HC and EU had no cytoxicity and reduced TNF-${\alpha}$, IL-6, IL-8 response on HMC-1 cells.

SAL 10-6 and Cytotoxicity of Sanitary Aid Products Utilizing Gamma Sterilization Technology (감마선 멸균기술을 이용한 의약외품의 무균보증수준(SAL 10-6) 확보 및 세포독성 평가)

  • Kim, Kwang Hoon;Eom, Yong Woon;Lee, Hoo Chul;Park, Sung Hyun;Kim, Soo Jin;Kim, Kwan Soo;Park, Soon Youn;Jeong, Ill Yun
    • Journal of Radiation Industry
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    • v.8 no.2
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    • pp.133-140
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    • 2014
  • The sterilization of health care products is widely used to choose conventional Ethylene Oxide gas sterilization in South Korea. But the method has brought serious issues because of the toxic residual gas and global warming of $CO_2$ evacuation after the sterilization process. This study is carried out to confirm the application possibility of gamma sterilization instead of Ethylene Oxide in sanitary aid products. Four kinds of products (gauze, menstrual pad, bandage, menstrual tampon) were treated with gamma irradiation of 15 kGy, then analyzed the achievement of the sterility assurance level (SAL) $10^{-6}$ through BI test. The cytotoxicity of accelerated samples of 6 months elapse evaluated by means of colony forming rate at various concentration of the extracts. pH and UV measurements at extract concentrations were tested according to the MFDS (Ministry of food & drug safety) guideline to verify a stability & safety of product sterilized. The results revealed that the extracts did not show any significant changes in cytoxicity assay as well as pH and UV values by gamma sterilization. All extract concentration was observed high cell viability, pH and UV values were calculated within the acceptable range prescribed by the guideline. It indicates that gamma sterilization could effectively substitute for conventional sterilization such as Ethylene Oxide sterilization in the sanitary aid products.

Effects of Sagunjatang-Gami on Uterine and Ovarian Function in the Ovariectomized Rat Postmenopause Model (사군자탕가미방(四君子湯加味方)이 난소적출 폐경 병태 모델의 자궁 및 난소 기능에 미치는 영향)

  • Maeng, Yu-Sook;Choi, Min-Sun;Ahn, In-Suk;Kim, Dong-Il
    • The Journal of Korean Obstetrics and Gynecology
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    • v.25 no.4
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    • pp.12-26
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    • 2012
  • Objectives: The purpose of this study is to examine the effects of Sagunjatang-Gami(SGJT) on uterine and ovarian function in the ovariectomized rat postmenopause model. Methods: SGJT was administered in ovariectomized Wister albino female rats for three month. After that, uterine weight, uterine index, serum estradiol-$17{\beta}$ levels and phosphorylation of ERK or AKT, and histological analysis of uterus were measured to assess the impact on uterine and ovarian function in ovariectomized rats. In addition, phosphorylation of $ER{\alpha}$, ERK, AKT by SGJT in MDA-MB-231 cells were measured. To identify safety of SGJT, the cell cytoxicity in MDA-MB-231 cells and serum GOT, GPT levels were measured in ovariectomized rats. Results: The results were as follows. 1. SGJT decreased the viability of MDA-MB-231 cells in a dose-dependent manner. 2. The level of serum GOT, GPT in SGJT-treated group showed significant decrease in comparison with control group. 3. Phosphorylation of $ER{\alpha}$, ERK, AKT by SGJT in MDA-MB-231 cells were increased. 4. Uterus index in SGJT-treated group showed significant increase in comparison with control group. The level of serum estradiol-$17{\beta}$ in SGJT-treated group showed significant increase in comparison with control group. Phosphorylation of ERK or AKT by SGJT in the uterus of ovariectomized rats was increased significantly. 5. Uterus index and the level of serum estradiol-$17{\beta}$ in SGJT-treated group increased at higher rates in comparison with estrogen-treated group. Conclusions: Taken together, we suggest that SGJT has been shown to be effective in preventing postmenopausal uterine and ovarian degeneration and curing postmenopausal low estrogen related symptoms.

A Literatural Study on Medicinal Herbs used in Cancer Therapy (악성종양(惡性腫瘍) 치료(治療)에 응용(應用)되는 약물(藥物)에 대(對)한 문헌적(文獻的) 고찰(考察))

  • Park, Ryung-Joon;Park, Yong-Ki
    • The Journal of Dong Guk Oriental Medicine
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    • v.9
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    • pp.139-154
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    • 2000
  • This studies were examined in orther to investigate the object and the method of animal experimental papers on medicinal herbs of cancer therapeutic activities from the reported 23 literatures containing anti-cancer effects of medicinal herbs. The results were obtained as follows: 1. The oriental medicinal therapies on cancer were Pujeung(扶正法), Kuesa(祛邪法), Pujeungkuesa(扶正法邪法). 2. The experimental medicinal herbs of cancers therapy were 103 species, which was used for experimental cancer single or combine. Among then, Houttuyniae herba, Polyporus, Manitis squama, Evodiae fructus, Aucklandiae radix and Pharbitidis semen were effective for cancer treatment, while Houttuyniae herba inhibited tumor cells, but not normal cells. Also, Evodiae fructus, Aucklandiae radix and Pharbitidis semen showed strong cytoxicities on 20 different tumor cell lines, whereas Saururi herba seu rhizoma showed cytoxicity against HT-29 cell, melanoma, SK-MEL-5 cell, and Anemarrhenae rhizoma against ovarian tumor cell only, and Schizonepetae herba against HT-29 cell line only with a potent inhivitory activities. 3. P815 cell, Yac-1 cell, Sarcoma 180 cell, K 562 cell, and SNU-1 cells were frequently used as experimental cancer therapy.

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Whitening Effect of Green Tea Seed Shell Ethanol Extracts (녹차씨 껍질 에탄올 추출물의 미백 활성)

  • Song, Ha-Yeon;Sung, Nak-Yun;Jung, Pil-Mun;Kang, Min-Soo;Park, Won-Jong;Byun, Eui-Hong
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.44 no.10
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    • pp.1470-1475
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    • 2015
  • The objective of this study was to evaluate the whitening effect of green tea seed shell as an industrial byproduct. Green tea seed shell extract (GTSE) was obtained by ethanol extraction, and the yield was 1.24%. 1,1-Diphenyl-2-picrylhydrazyl radical scavenging and tyrosinase inhibitory activity of GTSE increased dose-dependently. To estimate inhibition of melanin synthesis, viability was tested in B16BL6 melanoma cells. GTSE treatment induced cytotoxicity at a concentration higher than $125{\mu}g/mL$ but did not induce cytoxicity lower than $62.5{\mu}g/mL$. Thus, we fixed the optimal concentration at $62.5{\mu}g/mL$. Using this optimal concentration, melanin synthesis inhibition was measured, and GTSE treatment significantly reduced melanin synthesis induced by ${\alpha}$-melanin stimulating hormone. Therefore, the results indicate that green tea seed shell extracts may have potential melanin synthesis inhibitory activity and may be useful for development of whitening material as a natural ingredient.

Inhibitory Effect on RANKL-Induced Osteoclast Differentiation by Water Extract of Zizyphus Jujuba Mill (대추 물 추출물이 RANKL에 의해 유도되는 파골세포 분화에 미치는 영향)

  • Yoon, Kang Hugh;Baek, Jong Min;Kim, Ju Young;Kwak, Seong Cheoul;Cheon, Yoon Hee;Jeon, Byung Hoon;Lee, Chang Hoon;Choi, Min Kyu;Oh, Jaemin;Lee, Myeung Su;Kim, Jeong Joong
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.28 no.1
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    • pp.29-34
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    • 2014
  • Bone homeostasis is maintained by balance between bone resorbing-osteoclasts and bone forming-osteoblasts. Excessive osteoclastic bone resorption plays a critical role in bone destruction in pathological bone diseases such as osteoporosis, rheumatoid arthritis, and periodontal disease. Many compounds derived from natural products have pharmacological applications and have therapeutic value for treating or preventing several bone diseases characterized by excessive bone resorption. To discover new compounds that can act as anti-resorptive agents, we screened for natural compounds that regulate osteclast differentiation, and found that water extract of Ziziphus Jujuba Mill (WEZJ) has inhibitory effects on osteoclast differentiation. In this study, WEZJ clearly inhibits the osteoclast differentiation in the presence of receptor activator of nuclear factor kB (RANKL), macrophage colony-stimulating factor (M-CSF) without cytoxicity by blocking activation of nuclear factor of activated T cells (NFAT)c1, and c-Fos. In signaling pathway, the phosphorylation of Akt, p38, c-Jun N-terminal kinases (JNK), extracellular signal-regulated kinases (ERK) and the expression of osteoclast-associated receptor (OSCAR), tartrate-resistant acid phosphates (TRAP), Integrin av, Integrin b3, Cathepsin K are suppressed, too. These result suggest that WEZJ may have therapeutic value for treating or preventing several bone diseases characterized by excessive bone destruction.

Comparative Study on the Toxic Mechanism of Oxidant-Induced Neurotoxicity and Protective Effects of Several Herb Extracts as a Nerve Growth Factor in Spinal Motor Neurons Damaged by Oxygen Radicals (신경성장인자(神經成長因子)로서의 약류별(藥類別) 한약제(韓藥劑)가 척수(脊髓) 운동신경세포(運動神經細胞)의 손상(損傷)에 미치는 효능(效能) 및 기전(機轉)에 관(關)한 비교(比較) 연구(硏究))

  • Park Seung-Taeck;Yoon Hyang-Suk;Hyoung Keon-Young;Cho Chung-Gu;Lee Kang-Chang;Kim Won-Shin;Kim Hyung-Min;Jeon Byung-Hoon;Yun Young-Gap
    • Herbal Formula Science
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    • v.7 no.1
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    • pp.131-141
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    • 1999
  • In order to eludidate the mechanism of oxidative stress in cultured spinal motor neurons damaged by oxygen free radicals, cytoxicity was assesed by MTT assay and NR assay after spinal motor neurons from mouse were cultured in media containing various concentrations of xanthine oxidase(XO) and hypoxanthine(HX) for 3 hours. In addition, neuroprotective effects of several herb extracts on oxidant-induced neurotoxicity were examined in these cultures, compared with nerve growth factors such as basic fibroblast growth factor(bFGF). XO/HX decreased cell viability in dose- and time dependent manners on cultured mouse spinal motor neurons, and MTT50 and NR50 values were measured at 20mU/ml XO and 0.1mM HX for 3 hours in these cultures. bFGF significantlt increased cell viability. In neuroprotective of herb extracts, Epimedium Koreanum Nakai(EK) and Alpinia oxphylla Mig(IJI) was very effective in the prevention of the neurotoxicity induced by XO/HX in cultured mouse spinal motor neurons. From the above results, it is suggested that XO/HX shows toxic effect in cultured mouse spinal motor neurons and selective herb extracts such as Epimedium Koreanum Nakai(EK) and Alpinia oxphylla Mig(IJI) were very effective in the increase of cell viability against the neurotoxicity induced by oxygen radicals in these cultures.

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