• Journal of Ginseng Research
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• 제44권3호
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• pp.405-412
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• 2020

Background: Root rot is a serious destructive disease of Panax notoginseng, a famous cultivated araliaceous herb called Sanqi or Tianqi in Southwest China. Methods: The chemical substances of Sanqi rot roots were explored by chromatographic techniques. MS, 1D/2D-NMR, and single crystal X-ray diffraction were applied to determine the structures. Murine macrophage RAW264.7 and five human cancer cell lines were used separately for evaluating the antiinflammatory and cytotoxic activities. Results and Conclusion: Thirty dammarane-type triterpenes and saponins were isolated from the rot roots of P. notoginseng. Among them, seven triterpenes, namely, 20(S)-dammar-25-ene-24(S)-hydroperoxyl-3β,6α,12β,20-tetrol (1), 20(S)-dammar-3-oxo-23-ene-25-hydroperoxyl-6α,12β,20-triol (2), 20(S)-dammar-12-oxo-23-ene-25-hydroperoxyl-3β,6α,20-triol (3), 20(S)-dammar-3-oxo-23-ene-25-hydroperoxyl-12β,20-diol (4), 20(S),24(R)-epoxy-3,4-seco-dammar-25-hydroxy-12-one-3-oic acid (5), 20(S),24(R)-epoxy-3,4-seco-dammar-25-hydroxy-12-one-3-oic acid methyl ester (6), and 6α-hydroxy-22,23,24,25,26,27-hexanordammar-3,12,20-trione (7), are new compounds. In addition, 12 known ones (12-16 and 19-25) were reported in Sanqi for the first time. The new Compound 1 showed comparable antiinflammatory activity on inhibition of NO production to the positive control, whereas the known compounds 9, 12, 13, and 16 displayed moderate cytotoxicities against five human cancer cell lines. The results will provide scientific basis for understanding the chemical constituents of Sanqi rot roots and new candidates for searching antiinflammatory and antitumor agents.

• 한국식품위생안전성학회지
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• 제20권1호
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• pp.53-57
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• 2005

지하 943 m(3호공)로부터 취수한 경산 광천수의 유$\cdot$무기성분을 분석한 결과 총 17종류의 성분 중 무기물은 11 종류가 검출되었으며 무기성분 중에서는 나트륨과 칼슘 성분이 많이 함유되어 있는 것이 특징이었다. 그리고 구리와 납과 같은 중금속과 탄산가스 및 유화수소는 검출되지 않았다. 그리고 항산화 활성, 항돌연변이원성 및 인간암세포 성장억제 실험 결과 항산화 활성에서는 비교적 약한 활성을 나타내었다. MNNG, 4NQO, Trp-P-1및 $B({\alpha})P$와 같은 돌연변이원을 이용한 미생물 수준에서의 항돌연변이원성 실험 결과 S. typhimurium TA98에 대해서 간접변이원인 Trp-P-1은 시료 농도 $200{\mu}g/plate$ 첨가 시 $54\%$의 억제 활성을 나타내었다. 또한 S. typhimurium TA100 균주에서 4NQO 및 MNNG는 각각 $65.8\%$ 와 $58.6\%$의 억제활성을 보였으며 $B({\alpha})P$ 및 Trp-P-1에 대해서도 각각 67%와 63%의 높은 억제활성을 나타내었다. 그리고 광천수의 항암활성을 규명하기 위한 암세포 성장억제 효과에서는 시료농도 $50{\mu}g/well$ 첨가 시 A549, Hela, AGS 및 MCF-7에 대해서 각각 $66\%,\;45.6\%,\;37.7\%$ 및 $47.6\%$의 억제효과를 나타내었다. 또한 인간 정상 신세포 293에 대한 온천수 농도에 따른 세포독성 효과는 $20\%$ 이하의 낮은 생육 억제율을 보였으며 이것은 광천수가 정상세포에 대해서는 비교적 낮은 독성효과를 나타냄을 알 수 있었다.

• BMB Reports
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• 제34권3호
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• pp.237-243
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• 2001

Taxol, a natural product extracted from the Taxus brevifolia, is known to have significant anti-tumor activities against many common cancers, including ovarian and breast cancers. Despite the pronounced anti-tumor activity of this compound, its poor solubility in aqueous solutions hampers its clinical applications. We studied the anticancer mechanisms of the water-soluble taxol diethylenetriamine pentaacetate (DTPA) used for radiolabeling, and compared it to that of taxol. In vitro cytotoxicities of taxol and taxol-DTPA conjugate were tested in HT29 human colorectal cancer cells by the MTT method. As the result, the $IC_{50}$ value of the taxol-DTPA conjugate was about three fold higher than that of taxol. When analyzed by an agarose gel electrophoresis, the DNA ladders became evident after the incubation of cells with the taxol-DTPA conjugate for 24 h. We also found morphological changes of the cells undergoing apoptosis with electron microscopy Next, we examined the signal pathway of taxol-DTPA conjugate-induced apoptosis in HT29 cells. The activation of extracellular signal-regulated protein kinase (ERK1/2) occurred at 10, 30, 60 and 120 min after 200 nM taxol-DTPA conjugate treatment. The pretreatment of the MEK inhibitor (PD98059) completely blocked the taxol-DTPA conjugate-induced ERK1/2 activation. The activated ERK1/2 translocated into the nucleus at the same time and phosphorylated its transcriptional factor, c-Jun. These results suggest that the taxol-DTPA conjugate has an apoptotic activity in HT29 cells, and that its proapoptic activity might be related with the signal transduction via ERK1/2 and c-Jun similar to that of taxol.

• 대한한방내과학회지
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• 제31권3호
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• pp.650-666
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• 2010

Objectives : In this study, the author tried to investigate whether wood vinegar produced from Morus alba (MA) significantly affects the increase in airway epithelial mucosubstances and hyperplasia of tracheal goblet cells of rats, and in vitro airway mucin secretion and PMA- or EGF- or TNF-alpha-induced MUC5AC mucin production / gene expression from human airway epithelial cells. Materials and Methods : For the in vivo experiment, the author induced hypersecretion of airway mucus and goblet cell hyperplasia by exposure of rats to SO2 over 3 weeks. Effect of orally-administered MA over 2 weeks on increase in airway epithelial mucosubstances from tracheal goblet cells of rats and hyperplasia of goblet cells were assessed using histopathological analysis after staining the epithelial tissue with alcian blue. For the in vitro experiment, confluent RTSE cells were chased for 30 min in the presence of MA to assess the effect of MA on mucin secretion by enzyme-linked immunosorbent assay (ELISA). Also, effects of MA on PMA- or EGF- or TNF-alpha-induced MUC5AC mucin production and gene expression from human airway epithelial cells (NCI-H292) were investigated. Confluent NCI-H292 cells were pretreated for 30 min in the presence of MA and treated with PMA (10 ng/ml), EGF (25 ng/ml) or TNF-alpha (0.2 nm) for 24 hrs, to assess both effects of MA on PMA- or EGF- or TNF-alpha-induced MUC5AC mucin production by enzyme-linked immunosorbent assay (ELISA) and gene expression by reverse transcription-polymerase chain reaction (RT-PCR). Possible cytotoxicities of MA in vitro were assessed by examining LDH release from RTSE cells and the rate of survival and proliferation of NCI-H292 cells. In vivo liver and kidney toxicities of MA were evaluated by measuring serum GOT/GPT activities and serum BUN/creatinine concentrations of rats after administering MA orally. Results : 1. MA decreased the amount of intraepithelial mucosubstances of rats exposed to sulfur dioxide inhalationally. 2. MA decreased in vitro mucin secretion from cultured RTSE cells. 3. MA significantly inhibited PMA-, EGF-, and TNF-alpha-induced MUC5AC mucin productions and the expression levels of MUC5AC mRNA from NCI-H292 cells. 4. MA did not show either in vitro or in vivo hepatic or renal toxicities. Conclusion : The results from this study suggests that MA can regulate the secretion, production and gene expression of airway mucin observed in diverse respiratory diseases accompanied by mucus hypersecretion and does not show in vivo toxicity to liver and kidney functions after oral administration. Effects of MA should be further studied using animal experimental models that simulate the diverse pathophysiology of respiratory diseases via future research.

• 한국수산과학회지
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• 제42권5호
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• pp.434-441
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• 2009

This study was conducted to compare the biological activities of 7 melania snails from the family Pleuroceridae (Semisulcospira coreana, Koreanomelania nodifila, Semisulcospira forticosta, Koreoleptoxis globus ovalis, Semisulcospira libertina, Semisulcospira tegulata and Semisulcospira gottschei) in Korea. Among the 7 species, S. coreana, Korean. nodifila, S. forticosta and S. gottschei showed over 80% cytotoxicities on three cancer cell lines (SNU-1, A549 and Hep 3B) compared to the non-treatment, whereas S. libertina and S. tegulata showed almost no growth inhibition activities on the same cancer cell lines. In relation to ACE inhibition activity, only S. coreana, Korean. nodifila, and S. forticosta showed over 60% ACE inhibition activities, whereas other melania snails exhibited inhibition activities of lower than 25%. DPPH radical scavenging activities were also determined, and used to categories melania snails into three groups based on Duncan's multiple range test at P<0.05. The amount of TNF-${\alpha}$ produced by in vitro mouse peritoneal macrophage was determined according to bioactivity on L-929 cells. Three melania snails, S. coreana, Korean. nodifila and S. gottschei, exhibited 95.2%, 89.7% and 93.7% cell death(%) on L-929 cells, respectively. Glucose-6-phosphate dehydrogenase inhibitory activity was also obtained in the extract of S. coreana (31.9%) and Korean. nodifila (28.1%), showing that these extracts can be used as supplemental dietary health foods. In conclusion, we believe that the extracts of melania snails should be given due consideration in functional health food development.

• Journal of Korean Neurosurgical Society
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• 제38권2호
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• pp.126-131
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• 2005

Objective : The choice of tumor antigen for dendritic cell[DC]-loading has still been an unresolved problem in the DC-based vaccine strategies against malignant gliomas that has not been found well-characterized tumor specific antigens. In this study, we compare tumor-specific T cell response induced by glioma apoptotic body[GAB]-pulsed DCs to response induced by glioma cell lysate-pulsed ones quantitatively. Methods : DCs generated in the presence of granulocyte macrophage-colony stimulating factor and interleukin[IL]-4 from peripheral blood mononuclear cells[PBMCs] of HLA-A2 positive healthy donors were cultured. Each GABs and glioma cell lysate generated from HLA-A2 positive T98G glioblastoma cells were co-incubated with DCs. $CD8^+$ T lymphocytes isolated from PBMCs of same donors were cultured in media containing IL-2 and either stimulated by GAB- or lysate-pulsed DCs three times at a weekly interval. The interferon[IFN]-${\gamma}$ concentrations of each cell culture supernate were measured by enzyme immunoassay technique. Cytolytic activity of the generated cytotoxic $CD8^+$ T cells either stimulated with GAB- or lysate-pulsed DCs was determined by a standard 4-h $^{51}Cr$-release assay. Results : IFN-${\gamma}$ production and cytolytic activity of effector T cells stimulated by GAB-pulsed DCs were significantly higher than those of T cells stimulated by lysate-pulsed ones. Conclusion : These results indicate the choice of antigen is a critical determinant in the induction of antitumor immunity against malignant glioma. Antigen preparations from GABs represent a promising alternative to glioma cell lysate in DC-based glioma vaccine strategies.

• 한국식품저장유통학회지
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• 제15권2호
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• pp.274-279
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• 2008

해양심층수 간장 및 일반간장을 제조하여 항돌연변이원성과 세포독성을 측정하였으며 sarcoma-180 cell을 이용하여 in vivo에서 항암효과를 살펴보았다. S. typhimurium TA98과TA100 균주를 이용한 실험에서 모든 시료에서 돌연변이원성이 없었으며, 항돌연변이원성 실험에서는 직접변이원인 MNNG($0.4{\mu}g$/plate)의 경우 TA100 균주에서 해양심층수간장의 시료농도 $200{\mu}g$/plate에서 90.9%의 높은 억제효과를 나타내었으며 4NQO($0.15{\mu}g$/plate)에 대해서는 같은 시료농도에서 62.0%의 억제효과를 나타내었다. 그리고 4NQO의 경우 TA98 균주에 대해서 해양심층수 간장은 61.7%의 억제효과를 나타내었으며 모든 시료는 농도 의존적으로 억제하는 것으로 나타났다. 세포독성 효과를 알아보기 위하여 HeLa, Hep3B, AGS, A549와 MCF-7을 사용하였다. 각 시료 추출물의 암세포 성장효과를 조사한 결과, 해양심층수 간장이 1 mg/mL의 농도에서 각각 69.4%, 70.5%, 55.6%, 82.1% 및 73.2%의 억제율을 나타내었다. 그리고 해양심층수 간장은 고형암 성장 억제 실험에서 대조군에 비해서 40.9%의 고형암 성장 억제효과를 나타내었다.

• 대한한의학회지
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• 제29권3호
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• pp.63-75
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• 2008

Objectives: In the present study, the author intended to investigate whether Gamijinhae-tang (Jiaweizhenke-tang) (GJHT) significantly affects both contractility of tracheal smooth muscle and mucin secretion from airway epithelial cells. Materials and Methods: Effect of GJHT on contractility of isolated tracheal smooth muscle of rabbit was investigated. Confluent hamster tracheal surface epithelial (HTSE) cells were metabolically radiolabeled with 3H-glucosamine for 24 hrs and chased for 30 min in the presence of GJHT to assess the effect of the agent on 3H-mucin secretion. At the same time, confluent NCI-H292 cells were chased for 30 min in the presence of GJHT to assess the effect of the agent on MUC5AC secretion by ELISA. Total elution profiles of control spent media and treatment sample (radioactive mucin) through Sepharose CL-4B column were analyzed. Also, effect of the agent on MUC5AC gene expression in cultured NCI-H292 cells was investigated. Possible cytotoxicities of the agent were assessed by measuring both lactate dehydrogenase (LDH) release from HTSE cells and examining the rate of survival and proliferation of NCI-H292 cells. Results: (1) GJHT inhibited Ach-induced contraction of isolated tracheal smooth muscle; (2) GJHT significantly increased mucin secretion from cultured HTSE cells. However, it did not affect MUC5AC secretion from NCI-H292 cells, only chiefly affecting the 'mucin' secretion; (3) GJHT did not significantly affect the expression levels of MUC5AC gene in cultured NCI-H292 cells; (4) GJHT did not significantly inhibit the survival and proliferation of NCI-H292 cells. However, it slightly increased LDH release from HTSE cells. Conclusion: The author suggests that effects of GJHT with their components should be further investigated and it is valuable to find, from oriental medical prescriptions, novel agents which might regulate mucin secretion from airway epithelial cells.

• 한국식품저장유통학회지
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• 제12권2호
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• pp.179-183
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• 2005

솔잎 열수 증류액에 대한 항산화 활성은 $RC_{50}$ 값이 $18.4\;{\mu}L$로서 매우 강한 항산화 활성을 나타내었다. 솔잎 열수 증류액에 대한 항돌연변이 활성은 S. typhimurium TA98과 TA100 균주를 이용한 돌연변이성 실험 결과 솔잎 열수 증류액 자체로서는 변이원성이 없었으며 항돌연변이원성 실험에서는 직접변이원인 WNNG $(0.4\;{\mu}L/plate)$의 경우 S. typhimurium TA100 균주에서 시료농도 $200\;{\mu}L/plate$에서 $45.9\%$의 억제활성을 나타내었으며 4NQO $(0.15\;{\mu}g/plate)$에 대해서는 동일 농도에서 $85.5\%$의 높은 억제활성을 나타내었다. 그리고 간접변이원인 $B(\alpha)P\;(10\;{\mu}g/plate)$에 대해서는 시료농도 $200\;{\mu}g/plate$의 시료농도에서 $88\%$의 높은 억제 활성을 나타내었다. 한편 Trp-P-1 $0.15\;{\mu}g/plate$에 대해서는 $50\;{\mu}g/plate$의 낮은 시료농도에서도 $85\%$의 높은 억제활성을 나타내었으며 모두 농도 의존적으로 억제하는 것으로 나타났다. 솔잎 열수 증류액의 암세포 성장억제효과를 검토한 결과, 폐암세포, 유방암세포에 대해서 각각 $78.7\%$, $62.3\%$의 비교적 높은 억제효과를 보였으며, 특히 위암세포, 자궁암세포, 간암세포에서 각각 $90.8\%,\;93.7\%,\;90.0\%$의 높은 억제효과를 나타내었다.

• 한국식품영양학회지
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• 제23권1호
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• pp.118-123
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• 2010

유전자 발현 조절 수준에서 멜라닌 색소의 생합성을 조절하는 천연물질을 탐색하고자 황금으로부터 유용성 물질을 추출 및 분획하여 티로시나아제 프로모터 부위를 도입하여 형질전환된 B16 melanoma cell에 처리한 결과, 그 메탄올 추출물의 티로시나아제 유전자 발현율은 $10\;{\mu}g/m{\ell}$와 $100\;{\mu}g/m{\ell}$의 농도에서 대조군 세포에 비해 각각 약 231과 256%로 매우 크게 증진하는 효과를 보여 주었다. 극성도가 서로 다른 용매 분획물들을 형질전환된 세포에 처리하였을 때 methylene chloride와 ethyl acetate 용매 분획물들은 $10\;{\mu}g/m{\ell}$의 농도에서, butyl alcohol 용매 분획물은 $10\;{\mu}g/m{\ell}$와 $100\;{\mu}g/m{\ell}$의 농도에서, 그리고 물 용매 분획물은 $500\;{\mu}g/m{\ell}$의 고농도에서 티로시나아제 유전자의 발현을 증진시키는 효과를 보여 주었다. 그러나 그들의 티로시나아제 발현 증진 효과는 메탄올 추출물보다 낮았다. 황금 메탄올 추출물을 B16 melanoma cell에 처리한 다음 MTT assay를 실시한 결과, $10\;{\mu}g/m{\ell}$와 $100\;{\mu}g/m{\ell}$의 농도에서는 대조군 세포와 세포활성능이 유사할 정도로 세포독성이 매우 낮게 나타났다. 그러나 그 이상의 농도에서는 세포 활성능이 현저하게 낮았으며, 특히 $1,000\;{\mu}g/m{\ell}$의 농도에서는 세포 독성이 심하여 세포의 활성능을 측정하는 것이 불가능하였다. 본 연구결과, 황금 메탄올 추출물 내에는 티로시나아제 유전자의 발현을 증진시키는 데에 관여하는 성분들이 함유되어 있는 것으로 추측된다. 따라서 황금 추출물은 멜라닌 색소의 생합성에 관여하는 유전자의 발현하는 증진시키는 목적으로 이용함이 바람직하며, 이를 산업적으로 응용하기 위해서는 앞으로도 보다 많은 연구가 필요하다.