• Title/Summary/Keyword: In vitro cytotoxicity

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Potent in Vitro Anticancer Activity of Metacycloprodigiosin and Undecylprodigiosin from a Sponge-Derived Actinomycete Saccharopolyspora sp. nov.

  • Liu, Rui;Cui, Cheng-Bin;Duan, Lin;Gu, Qian-Qun;Zhu, Wei-Ming
    • Archives of Pharmacal Research
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    • v.28 no.12
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    • pp.1341-1344
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    • 2005
  • Bioassay-guided fractionation of $CHCl_{3}$ extract from the fermentation broth of a sponge Mycale plumose-derived actinomycete Saccharopolyspora sp. nov., led to the isolation of two known prodigiosin analogs - metacycloprodigiosin (1) and undecylprodigiosin (2). These compounds exhibited significant cytotoxic activities against five cancer cell lines: P388, HL60, A-549, BEL­7402, and SPCA4. This is the first report on the significant cytotoxicity of metacycloprodigiosin (1) against human cancer cell lines.

Cytotoxic Effects of Hydrolysable Tannins from Some Euphorbia Plants on the Human Tumor Cell Lines (유포르비아속 식물로부터 단리한 가수분해형 탄닌의 인체고형암 세포에 대한 세포독성효과)

  • Lee, Seung-Ho;Park, Ji-Soo;Kim, So-Young;Chung, See-Ryun;Choi, Sang-Un
    • YAKHAK HOEJI
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    • v.41 no.4
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    • pp.524-529
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    • 1997
  • Seventy three hydrolysable tannins and related compounds were isolated from seven Euphorbia plants. Among them, 28 compounds including nine gallotannins, eleven ellagitannins and eight related compounds were selected according to the structural similarity. Cytotoxicity of them on the human tumor cell lines including A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT-15 were evaluated by the SRB method in vitro. 3,4,6-Tri-O-galloyl-D-glucose was shown to exhibit most potent cytotoxic effect($4.4{\mu}g/ml).

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Cannabidiol Induces Cytotoxicity and Cell Death via Apoptotic Pathway in Cancer Cell Lines

  • ChoiPark, Won-HyungHyun-Do;Baek, Seung-Hwa;Chu, Jong-Phil;Kang, Mae-Hwa;Mi, Yu-Jing
    • Biomolecules & Therapeutics
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    • v.16 no.2
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    • pp.87-94
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    • 2008
  • In view of obtaining potential anticancer compounds, we studied the inhibitory activity and the cytotoxic effects of a candidate compound in cancer cells. The cytotoxic effects of cannabidiol (CBD) in vitro were evaluated in NIH3T3 fibroblasts, B16 melanoma cells, A549 lung cancer cells, MDA-MB-231 breast cancer cells, Lenca kidney cells and SNU-C4 colon cancer cells. The cells were cultured in various concentrations of CBD for 48 h and 25 ${\mu}$M of CBD for 6-36 h. The cells were observed to exhibit inhibitory effects of the cell viability in their growth, and then cytotoxicity was estimated. The inhibitory activity of CBD was increased in all cancer cells and showed especially strong increment in breast cancer cells. The cytotoxicity of CBD increased in a dose- and time-dependent manner with growth inhibition in all cancer cell lines. Also, to assess the membrane toxicity induced by CBD, we investigated lactate dehydrogenase (LDH) release. After treatment with various concentrations of CBD, LDH release rate of cancer cells was accelerated. On the other hand, in the induction of cell death, caspase-3, -8 and -9 activations were detected in cancer cells after treatment with various concentrations of CBD, and CBD effectively induced activity of caspase-3, -8 and -9 in A549 lung cancer cells, MDAMB-231 breast cancer cells and Renca kidney cells. Therefore these results suggest that CBD has a possibility of anticancer agents and anticancer effects against cancer cells by modulation of apoptotic pathway in the range of 5-80 ${\mu}$M concentration.

The estimation of Draize score by in vitro cytotoxicity using continuous cell lines (In Vitro cytotoxicity에 의한 Draize score 측정 체계 수립)

  • 정민석;최종완
    • Proceedings of the SCSK Conference
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    • 1996.07a
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    • pp.33-51
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    • 1996
  • 화장품의 변질요인은 크게 물리적 또는 화학적 변화에 의한 요인과 미생물오염으로 인한 각종 문제점으로 대별될 수 있다. 이 중에서 미생물 오염문제는 제품의 상품가치에 미치는 영향 뿐만 아니라 지속적인 사용에 의한 피부의 위생적 측면때문에 그 중요성에 대한 인식이 높아지고 있다. 따라서, 제품개발시는 화장품 처방중의 영양성분의 배합, pH, 유화형태, 방부제의 혼합, 분배계수 및 그 안정성을 고려하여야 함은 물론이고 처방중의 모든 원료의 각각에 대한 항균능 및 피부자극여부를 사전에 미리 조사하여 각 제품별로 적당한 방부체계를 선택하는 것은 매우 중요한일이다. 독성실험방법에 있어서 in vivo 실험에 대체할 수 있는 새로운 in vitro 실험방법 수립 즉, 동물실험을 하지 않고 in vitro 실험결과로부터 in vivo 결과를 예측할 수 있도록 새로운 in vitro 실험체계의 가능성을 실험하였다. 4종의 cell line중 transformed mouse fibroblast L929가 본 실험에서 사용하기에 배양상의 용이성과 안정성, 재현성의 관점에서 가장 알맞은 cell line이었다. transformed mouse fibroblast L929를 사용한 NR$_{50}$ assay와 Draize score간의 regression coefficient ${\gamma}$값은 0.91이었다. 혈청은 시험물질의 세포에 대한 민감성에 영향을 주었다. 따라서, modified serum-free method를 이용함으로써 regression coefficient가 증가된 즉, 상관성 및 재현성이 높은 결과를 얻을 수 있었다. 이러한 기술은 독성실험에 실험동물을 사용하지 않고 in vivo test에 대체 할 수 있고, 또한 화학물질에 대한 prescreening으로 이용할 수 있을 것으로 판단된다.원과 섭식장소, 수중생물의 경우는 특히 수온, 수량 영양원등이다.(중략). 본 연구의 접근방법으로는 ASRS의 개념적인 Reference Model을 수립하고 이 Reference Model에 대한 Formal Model로 DEVS(Discrete Event System Specification)을 이용하여 시스템을 Modeling하였다. 이의 Computer Simulation을 위하여 DEVS형식론 환경에서의 Simulation Language인 DEVSim ++ⓒ를 이용하여 시스템을 구현하였다.. 실형 결과로는 먼저 선형 상미분방정식의 예로 mass-damper-spring system, 비선형 상미분방정식의 예로는 van der Pol 방정식, 연립 상미분방정식의 예로는 mixing tank problem 등을 보였으며, 그의 공학에서 일어나는 여러 가지 문제들도 다루었다.화물에 대한 방어력이 증가되어 나타난 결과로 여겨지며, 또한 혈청중의 ALT, ALP 및 LDH활성을 유의성있게 감소시키므로서 감잎 phenolic compounds가 에탄올에 의한 간세포 손상에 대한 해독 및 보호작용이 있는 것으로 사료된다.반적으로 홍삼 제조시 내공의 발생은 제조공정에서 나타나는 경우가 많으며, 내백의 경우는 홍삼으로 가공되면서 발생하는 경우가 있고, 인삼이 성장될 때 부분적인 영양상태의 불충분이나 기후 등에 따른 영향을 받을 수 있기 때문에 앞으로 이에 대한 많은 연구가 이루어져야할 것으로 판단된다.태에도 불구하고 [-wh]의미의 겹의문사는 병렬적 관계의 합성어가 아니라 내부구조를 지니지 않은 단순한 단어(minimal $X^{0}$ elements)로 가정한다. 즉, [+wh] 의미의 겹의문사는 동일한 구성요 소를 지닌 병렬적 합성어([$[W1]_{XO-}$ $[W1]_{XO}$ ]

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Screening Method for Antihepatotoxic Activity Using $CCl_4-induced$ Cytotoxicity in Primary Cultured Rat Hepatocytes (일차 배양 흰쥐 간세포에서 $CCl_4$ 유발 세포독성을 이용한 간보호 효과 검색방법)

  • Kim, Young-Sook;Park, Ki-Hyun
    • Korean Journal of Pharmacognosy
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    • v.26 no.1
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    • pp.51-56
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    • 1995
  • To devise an in vitro screening method for antihepatotoxic activity, $CCl_4-induced$ cytotoxicities in primary cultures rat hepatocytes were examined. When rat hepatocytes were intoxicated with 0.5, 1.0 or 1.5 mM $CCl_4$ for 1.5, 3 or 19hr, in order of LDH>GOT>GPT release form hepatocytes was increased in a dose-dependent manner. Treatment with 1.5 mM $CCl_4$ for 1.5 hr showed maximum increase in activity of LDH, GOT or GPT released in the medium compared with the control. At this experimental condition, well known antihepatotoxic substances, glycyrrhizin and silybin markedly inhibited $CCl_4-induced$ cytotoxicities. These results demonstrated that the screening method using $CCl_4-induced$ injury in primary cultured rat hepatocytes might be suitable in vitro assay for antihepatotoxic activity.

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Characterization of Acharan Sulfate Binding Proteins in Murine Lewis Lung Carcinoma Cell

  • Joo, Eun-Ji;Hahn, Bum-Soo;Kim, Yeong-Shik
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.150.2-151
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    • 2003
  • We have focused on various biological activities of acharan sulfate (AS) isolated from the giant African snail Achatina fulica. In a previous study, AS showed antiangiogenic and immunomodulating activity. We also investigated antitumor activity of AS. In vitro AS had no cytotoxicity within 0 to 200 ug/ml in tumor cells such as Lewis lung carcinoma(LLC) , KM1214 (human colon cancer cell) and Caki-1 (human kidney cancer cell) by both MTT and SRB assay. In vivo AS was used to treat C57BL/6 mice bearing LLC by subscutaneous injection. (omitted)

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Phospholipid polymer can reduce cytotoxicity of poly (lactic acid) nanoparticles in a high-content screening assay

  • Kim, Hyung Il;Ishihara, Kazuhiko
    • Biomaterials and Biomechanics in Bioengineering
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    • v.1 no.2
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    • pp.95-104
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    • 2014
  • The objective of this study was to evaluate the cytotoxicity of poly (lactic acid) (PLA) nanoparticles. We used a water-soluble, amphiphilic phospholipid polymer, poly (2-methacryloyloxyethyl phosphorylcholine-co-n-butyl methacrylate) (PMB30W), as a stabilizer for the PLA nanoparticles. The PLA nanoparticles and PMB30W-modified PLA (PLA/PMB30W) nanoparticles were prepared by evaporating tetrahydrofuran (THF) from its aqueous solution. Precipitation of the polymers from the aqueous solution produced PLA and PLA/PMB30W nanoparticles with a size distribution of $0.4-0.5{\mu}m$. The partial coverage of PMB30W on the surface of the PLA/PMB30W nanoparticles was confirmed by X-ray photoelectron spectroscopy (XPS) and dynamic light-scattering (DLS). A high-content automated screening assay (240 random fields per group) revealed that the PLA nanoparticles induced apoptosis in a mouse macrophage-like cell line (apoptotic population: 73.9% in 0.8 mg PLA/mL), while the PLA/PMB30W nanoparticles remained relatively non-hazardous in vitro (apoptotic population: 13.8% in 0.8 mg PLA/mL). The reduction of the apoptotic population was attributed to the phosphorylcholine groups in the PMB30W bound to the surface of the nanoparticle. In conclusion, precipitation of PLA in THF aqueous solution enabled the preparation of PLA nanoparticles with similar shapes and size distribution but different surface characteristics. PMB30W was an effective stabilizer and surface modifier, which reduced the cytotoxicity of PLA nanoparticles by enabling their avoidance of the mononuclear phagocyte system.

Studies on Immunomodulatory and Antioxidant Activities of Astragali membranacei Radix according to the Cultivated Years (황기(黃芪)의 재배 년수에 따른 면역 및 항산화 활성 연구)

  • Jung, Chul
    • Korean Journal of Korean Medical Institute of Dermatology and Aesthetics
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    • v.1 no.1
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    • pp.53-90
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    • 2005
  • Purpose: Contents of astragaloside I, II and IV, cytotoxicity, anticancer activity, immunomodulatory activity and antioxidant capacity were to be compared as a function of the cultivated years as one, three, five and seven years. Method: Major components of Astragali membranacei Radix were separated as astragaloside I, astragaloside II, astragaloside IV by HPLC analysis. Cytotoxicity and anticancer activities were measured by MTT and SRB assay. For immunomodulatory activity, the secretion of IL -6 and $TNF-{\alpha}$, NK cell activation and macrophage activation were observed as well as kinetics of responding to human T cells by a microphysiometer. In vitro antioxidant activities were measured by several radical scavenging activities of superoxide anion radican, DPPH, LDL and linoleic acid. For in vivo activity, the activation of SOD, GSH-px, catalase, ALDH and ADH was measured as well the relative weight of liver. Result : 1. For HPLC analysis, the contents of all of astragaloside I, astragaloside II, astragaloside IV were in order of three, five, one and seven years. 2. The cytotoxicity of normal human lung cell line, HEL299 showed lower than 18% in adding 0.25 mg/ml, and 28.9% in adding 1.0 mg/ml of water extract of seven year root. For methanol extracts, three year root showed highest cytotoxicity as 35.2 % and there was no difference between the cultivated years. 3. For anticancer activities, methanol extracts of one and three year roots showed relatively high inhibition of human stomach cancer cells, AGS, breast cancer cells, MCF-7, lung cancer cells, A549 and liver cancer cell, Hep3B as well as high selectivities. 4. The water extract of seven year root could yield high secretion of IL-6 from both human Band T cells while the methanol extracts of three and five year roots secreted high amounts of IL-6 and $TNF-{\alpha}$ from both Band T cells. 5. As a result of in vitro antioxidant activities, both water and methanol extracts from five and seven year roots showed high activities for superoxide anion radical scavenging activity, inhibiting linoleic acid peroxide and contents of total phenols. 6. For in vivo tests, Mn-SOD and GSH-px activities and weight of liver were better in adding seven year root. For ALDH activity one year root was better and for ADH activity five year root. Overall speaking, seven year root showed relatively better antioxidant activities. Conclusion:There was difference of the contents of astragaloside I, astragaloside II, astragaloside IV according to cultivation year. Methanol extract showed better activities of anticancer and immune activation rather than water extract Interestingly enough, for methanol extracts, overall activities were improved as the cultivation year increased. There might be further investigation required for the clinical uses of the results as several biological activities varied according to the cultivated year of Astragali membranacei Radix.

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Characterization of ginsenoside compound K loaded ionically cross-linked carboxymethyl chitosan-calcium nanoparticles and its cytotoxic potential against prostate cancer cells

  • Zhang, Jianmei;Zhou, Jinyi;Yuan, Qiaoyun;Zhan, Changyi;Shang, Zhi;Gu, Qian;Zhang, Ji;Fu, Guangbo;Hu, Weicheng
    • Journal of Ginseng Research
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    • v.45 no.2
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    • pp.228-235
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    • 2021
  • Backgroud: Ginsenoside compound K (GK) is a major metabolite of protopanaxadiol-type ginsenosides and has remarkable anticancer activities in vitro and in vivo. This work used an ionic cross-linking method to entrap GK within O-carboxymethyl chitosan (OCMC) nanoparticles (Nps) to form GK-loaded OCMC Nps (GK-OCMC Nps), which enhance the aqueous solubility and stability of GK. Methods: The GK-OCMC Nps were characterized using several physicochemical techniques, including x-ray diffraction, transmission electron microscopy, zeta potential analysis, and particle size analysis via dynamic light scattering. GK was released from GK-OCMC Nps and was conducted using the dialysis bag diffusion method. The effects of GK and GK-OCMC Nps on PC3 cell viability were measured by using the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide assay. Fluorescent technology based on Cy5.5-labeled probes was used to explore the cellular uptake of GK-OCMC Nps. Results: The GK-OCMC NPs had a suitable particle size and zeta potential; they were spherical with good dispersion. In vitro drug release from GK-OCMC NPs was pH dependent. Moreover, the in vitro cytotoxicity study and cellular uptake assays indicated that the GK-OCMC Nps significantly enhanced the cytotoxicity and cellular uptake of GK toward the PC3 cells. GK-OCMC Nps also significantly promoted the activities of both caspase-3 and caspase-9. Conclusion: GK-OCMC Nps are potential nanocarriers for delivering hydrophobic drugs, thereby enhancing water solubility and permeability and improving the antiproliferative effects of GK.

Pathogenicity of Korean isolates of Acanthamoeba by observing the experimental infection and zymodemes of five isoenzymes

  • Im, Kyung-Il;Shin, Ho-Joon;Seo, Dong-Whan;Jeon, Soung-Hoo;Kim, Tae-Eun
    • Parasites, Hosts and Diseases
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    • v.37 no.2
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    • pp.85-92
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    • 1999
  • To determine the pathogenicity of Acanthamoeba spp. isolated in Korea and to develop a isoenzymatic maker, the mortality rate of infected mice, in vitro cytotoxicity against target cells and isoenzyme band pattern were observed. Five isolates of Acanthamoeba spp. (YM-2, YM-3, YM-4, YM-5 and YM-7) were used in this study as well as three reference Acanthamoeba spp. (A. culbertsoni, A. hatchetti, and A. royreba). According to the mortality rate of infected mice, Korean isolated could be categorized into three groups: high virulent (YM-4), low virulent (YM-2, YM-5, YM-7) and the nonpathogenic group (YM-4), In addition, the virulence of Acanthamoeba spp. was enhanced by brain passage in mice. In the cytotoxicity assay against chinese hamster ovary cells, especially, the cytotoxicity of brain-passaged amoebae was relatively higher than the long-term cultivated ones. The zymodeme patterns of glucose-6-phosphate dehydrogenase (G6PD), malate dehydrogenase (MDH), hexokinase (HK), glutamate oxaloacetate transaminase (GOT) and malic enzyme (ME)of Acanthamoeba spp. were different among each isolate, and also between long-term cultrued amoebae and brain passaged ones. In spites of the polymorphic zymodemes, a slow band of G6PD and K, and an intermediate band of MDH were only observed in pathogenic Acanthamoeba spp., which should be used as isoenzymatic makers.

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