• 제목/요약/키워드: cytotoxicities

검색결과 191건 처리시간 0.025초

행소탕(杏蘇湯) 및 가미팔미환(加味八味丸)이 호흡기(呼吸器) 배상세포(杯狀細胞)로부터의 뮤신 분비(分泌)에 미치는 영향 (Effects of HaengSoTang(HST), Gami-PalMiHwan(GPMH) on mucin secretion from airway goblet cells)

  • 임도희;이정은;한영주;황지호;조철준;배한호;채은영;박양춘
    • 대한한방내과학회지
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    • 제26권1호
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    • pp.221-228
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    • 2005
  • The intent of this study is to investigate whether two oriental medical prescriptions named haengsotang(HST) and gami-palmihwan(GPMH) significantly effect mucin release from cultured hamster tracheal surface epithelial(HTSE) cells, Confluent HTSE cells were metabolically radiolabeled with $^3H-glucosamine$ for 24 hrs and chased for 30 min in the presence of HST or GPMH to assess the effect of each agent on $^3H-mucin$ release. Possible cytotoxicities of each agent were assessed by measuring lactate dehydrogenase(LDH) release. Also, the effects of HST and GPMH on contractility of isolated tracheal smooth muscle were investigated. The results are consistant with the following assertions: (1) HST significantly inhibited mucin release from cultured HTSE cells, without cytotoxicity; (2) GPMH did not effect mucin release without cytotoxicity; (3) HST and GPMH did not effect contractility of isolated tracheal smooth muscle. These results suggest a need for further investigation of HST and its components, for its potential in oriental medicine prescriptions and novel agents that effectively regulate (inhibit) mucin secretion from airway goblet cells.

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Antitumor Activities of Spray-dried Powders with Different Molecular Masses Fractionated from the Crude Protein-bound Polysaccharide Extract of Agaricus blazei Murill

  • Hong, Joo-Heon;Kim, Seok-Joong;Ravindra, Pogaku;Youn, Kwang-Sup
    • Food Science and Biotechnology
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    • 제16권4호
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    • pp.600-604
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    • 2007
  • In this study, we first prepared 3 kinds of powders with different molecular masses from the crude protein-bound polysaccharide extract of Agraricus blazei Murill through ultrafiltration, followed by spray-drying. Then, the antitumor activities of the powders were analyzed. Size exclusion chromatography coupled with a multi-angle laser-light-scattering system showed the 3 powders had the following molecular ranges: below 10 kDa (SD-1), 10 to 150 kDa (SD-2), and above 150 kDa (SD-3), representing peak molecular weights of $8.26{\times}10^3,\;9.65{\times}10^4$, and $5.94{\times}10^6\;g/mol$, respectively. All the powders stimulated macrophage RAW264.7 cells to produce nitric oxide, of which SD-2 and SD-3 were superior to the crude extract powder (CP-SD), while SD-1 showed the lowest activity. Similar results were found for their cytotoxicities against human cancer cell lines (A549, MCF-7, and AGS), where the highest activity was obtained with the SD-2 treatment for 72 hr at $1,000\;{\mu}g/mL$. The MCF-7 cell line was less sensitive to the powders than the other cells. From this research we found that ultrafiltration, in combination with spray-drying, is applicable for preparing protein-bound polysaccharide powders with higher antitumor activities.

Methanolic Extract of Plumbago Zeylanica - A Remarkable Antibacterial Agent Against Many Human and Agricultural Pathogens

  • Singh, Mukesh Kumar;Pandey, Ajit;Sawarkar, Hemant;Gupta, Anshita;Gidwani, Bina;Dhongade, Hemant;Tripathi, Dulal Krishna
    • 대한약침학회지
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    • 제20권1호
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    • pp.18-22
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    • 2017
  • Objectives: The current investigation was carried out to determine the cytotoxic and the antimicrobial activities of methanolic extracts of Plumbago zeylanica. Methods: The stems, leaves, and whole plants were air dried and extracted with methanol by using a Soxhlet extractor for 72 hours at $55-60^{\circ}C$. The antimicrobial activities were determined from the zones of inhibition, which were measured by using the agar well diffusion method, and the cytotoxicity assays were performed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay method. Results: The methanolic extracts of the stem and the leaves of Plumbago zeylanica were tested against six bacterial species and nine fungal species, and both extracts showed antimicrobial activity in a dose-dependent manner. The leaf extract of Plumbago zeylanica showed maximum antimicrobial activity against both Staphylococcus aureus sub sp aureus and Fusarium oxysporum. The stem extract was found to be more antimicrobial against the Pseudomonas aeruginosa and the Penicillium expansum species. MTT assays were used to test the cytotoxicity of the whole plant extract in the HCT-116 and the K-562 cell lines, and that extract was shown to have weak cytotoxicity in both cell lines. Conclusion: In the present study, the methanolic stem extracts of Plumbago zeylanica were found to possess remarkable antibacterial activities against many human and agricultural pathogens. The extracts were also found to possess significant antifungal activities, but the antifungal activities were less than the antibacterial activities. Finally, the extracts were found to have weak cytotoxicities in the HCT-116 and the K-562 cell lines.

상엽(桑葉) 추출물의 미백활성 및 피부섬유구조 형성에 미치는 효과 (Effect of Mori Follium Extract on the Melanogenesis and Skin Fibril Matrix)

  • 권오준
    • 대한본초학회지
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    • 제31권5호
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    • pp.41-46
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    • 2016
  • Objectives : The Skin is composed of multiple layers, including the epidermis, dermis, and hypodermis. It provides a vital barrier structure that protects vertebrates from external environmental antigens, solvents, ultraviolet light, microorganisms, toxins, and weather conditions. Although several biological effects of Mori Follium have been reported, beneficial effects of Mori Follium in skin health remain unclear. In this study, we prepared water extract of Mori Follium (MLE) and evaluated the effects on melanin accumulation and expression levels of skin fibril-related proteins.Methods : The cytotoxicities of MLE in B16F10 melanoma and human skin fibroblasts (HSF) were examined by MTT assay. Inhibitory effect of MLE on the α-MSH- and IBMX-induced melanosis in B16F10 melanoma was examined. The expression levels of fibronectin, collagen 1α2, and CCN2 in MLE-treated HSF were analyzed by reverse transcription-polymer chain reaction (RT-PCR) and western blotting.Results : The MLE treatment for 24 h did not affect to the B16F10 and HSF at concentrations of 1, 10, 50, 100, 200, 400 and 800 ㎍/ml. The MLE treatment for 72 h significantly and dose dependently suppressed melanin accumulation in B16F10 melanoma. In addition, the MLE treatment up-regulated expression levels of skin fibril-related genes such as fibronectin, collagen 1α2, and CCN2 in HSF. Our western blot analysis revealed MLE-induced up-regulation of skin fibril-related genes required the activation of CCN2 protein.Conclusions : In conclusion, these findings suggest that the MLE could be used in development of cosmetic natural material of maintaining healthy skin.

Structure-Related Cytotoxicity and Anti-Hepatofibric Effect of Asiatic Acid Derivatives in Rat Hepatic Stellate Cell-Line, HSC-T6

  • Dong, Mi-Sook;Jung, Seung-Hyun;Kim, Hyun-Jung;Kim, Jeong-Ran;Zhao, Long-Suan;Lee, Eung-Seok;Lee, Eun-Joo;Yi, Jung-Bum;Lee, Nam-Kyu;Cho, Yong-Baik;Kwak, Wie-Jong;Park, Young-In
    • Archives of Pharmacal Research
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    • 제27권5호
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    • pp.512-517
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    • 2004
  • The structural relationship of 16 asiatic acid (AA) derivatives, including AA and asiaticoside (AS) to cytotoxicity and anti-hepatofibrotic activity in HSC-T6 cells, were investigated. Cytotoxicities of AA derivatives varied from 5.5 $\mu$M to over 2000 $\mu$M of $IC_{50}$/ depending on AA functional group modifications. Substituting the hydroxyl group at the C(2) to N≡C and substituting bulky groups for dihydroxyl groups at (3), (23) of the A-ring increased the cytotoxicity, but keto group at C(11) and benzoyl ester at C(2) were greatly reduced it. Modification of the carboxylic acid group at C28 also reduced the cytotoxicity. The collagen synthesis determined by hydroxyproline content in the cells was inhibited from a maximum of 48% (Zlx-i-85 and 87) to 15% (AS) by AA derivatives. The anti-hepatofibrotic effect of these compounds might be due to the reduced expression of prolyl 4-hydroxylase $\alpha$ and $\beta$ subunits and TIMP2. However, the inhibition of collagen by asiaticoside derivatives did not show any structural-activity relationship.

산마늘 추출물의 항돌연변이원성 및 세포독성 효과 (Antimutagenic and Cytotoxic Effects of Allium victorialis Extracts)

  • 함승시;최승필;최형택;이득식
    • 한국식품저장유통학회지
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    • 제11권2호
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    • pp.221-226
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    • 2004
  • 산마늘 에탄올 추출물과 각종 유기용매 분획물에 대하여 항돌연변이원성과 세포독성을 검토하였다. 시료자체는 돌연변이원성이 없는 것으로 나타났다. 직접 변이원인 MNNG에 대한 항돌연변이 효과에서 S. typhimurium TA100 균주에 대해 산마늘 에탄올 추출물(200$\mu\textrm{g}$/plate)에서 88.2%의 억제효과를 나타내었다. 동일 시료 농도에서 4NQO에 대해서는 S. typhimurim TA98과 TA100 두 균주 모두에서 각각 76.4%와 83.0%의 비교적 높은 억제효과를 나타내었다. 암세포 성장 억제 효과를 검토한 실험에서는 에탄올 추출물이 다른 분획물보다 높은 억제활성을 나타내었다. 시료농도의 증가와 함께 억제활성도 증가하는 경향을 나타내었으며 시료농도 50 $\mu\textrm{g}$/plate에서 A549가 74.2%, MCF-7이 71.3% 그리고 KATOIII에 대하여 67.4%의 암세포 성장억제효과를 나타내었다.

Selective Cytotoxicity of a Novel Platinum (II) Coordination Complex on Human Gastric Cancer Cell Lines and Normal Kidney Cells

  • Jung, Jee-Chang;Kim, Young-Kyu;Yim, Sung-Vin;Park, Seung-Joon;Chung, Joo-Ho;Chang, Sung-Goo;Lee, Kyung-Tae;Rho, Young-Soo
    • The Korean Journal of Physiology and Pharmacology
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    • 제3권3호
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    • pp.283-291
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    • 1999
  • We have synthesized novel platinum (II) coordination complex containing cis-1,2-diaminocyclohexane (DACH) as a carrier ligand and 1,2-bis(diphenylphosphino)ethane (DPPE) as leaving group. Furthermore, nitrate was added to improve the water-solubility. A new series of [Pt(cis-DACH)(DPPE)] $2NO_3(PC)$ was evaluated its antitumor activity on various MKN-45 human gastric adenocarcinoma cell-lines and normal primary cultured kidney cells. The new platinum complex demonstrated high efficacy in the cytotoxicity on MKN-45 cell-lines as well as adriamycin-resistant (MKN-45/ADR) and cisplatin-resistant (MKN-45/CDDP) cells. The cytotoxicities of PC were found quite less than those of cisplatin in rabbit proximal renal tubular cells, human renal cortical cells and human renal cortical tissues using MTT assay, $[^3H]-thymidine$ uptake and glucose consumption tests. Based on these results, this novel platinum (II) coordination complex, was considered as better a valuable lead for improving antitumor activities with low nephrotoxicities in the development of a new clinically available anticancer chemotherapeutic agents.

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Polyoxygenated Flavones; Synthesis, Cytotoxicities and Antitumor Activity against ICR Mice Carrying S-180 Cells

  • Song, Gyu-Yong;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • 제18권6호
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    • pp.440-448
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    • 1995
  • Fitty two flavones were synthesized from polyoxygenated dibenzoylmethanes which were obtained by a modified Baker-Venkatarman rearrangement, of 2-benzoyl oxyacetophenones. The following flavones among them showed good cytotoxic activities against L1210 and HL60 cells ; 2'-benzoyloxy-5,7-dimethoxyflavone $(8.2{\mu}g/ml,{\;}5.0 {\mu}g/ml)$, 2'-benzyloxy-5,7,8-trimethoxyflavone $(5,9 {\mu}g/ml,{\;}11.0{\mu}g/ml,{\;}2.7{\mu}g/ml)$, 2'-hydroxy-5,7,8-trimethoxyflavone $(9.8{\mu}/ml,{\;}6.2{\mu}g/ml)$, 2'-benzyloxy-5-hydroxyflavone $(5.2 {\mu}g/ml,{\;}3.6{\mu}g/ml)$, and 5,2'-dihydroxyflavone $(5.1{\mu}g/ml,{\;}4.0{\mu}g/ml)$. Presence of 5-methoxy group potentiated the cytotoxic activity, while the existence of 7-methoxy group decreased the activity. 5-Hydroxy or methoxy activates 4-carbonyl group, while 7-methoxy group deactivates the acrbonyl group. From these observation it was concluded that the activation of carbonyl group at C-4 of a flavone is important for the enahncement of the cytotoxic activity. The presence of both 5-hydroxy and 2-benzyloxy-or 2-hydroxy group enhanced the antitumor activity; 2'-benzyloxy-5-hydroxy-7-methoxyflaone 9T/C=144%), 5.2'-dihydroxy-7-methoxyflavone (T/C=132%) and 5,2'-dihydroxy-6,78,6' trtramethoxyflvone (T/C = 172%) 2'hexanolytion of 5,2'-dihydroxy-flavones did not improve the natitumor activity; 2' hexanoyloxy-5-hydroxy-7-methoxyflavone showed T/C = 132%, about the same as that of 5,2'-dihydroxy-7-methoxyflvone (T/C=130%)

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천연물화학(天然物化學)에서 보는 동의약(東醫藥) (The Oriental Materia Medica in viewpoint of natural products chem)

  • 안병준
    • 혜화의학회지
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    • 제4권2호
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    • pp.309-329
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    • 1996
  • There are the Seven Effect of Drugs and unique processing methods in Chinese traditional medicine. The Seven Effects are single effrect(單行), additive effect(相加, 相須), synergic effect(上乘, 相使), antagonistic effect(相畏, 拮抗), inhibitory effect(相惡), neutralizing effect(相殺) and opposite effect(相反). We are interested in synergic effects of some drugs and components ; Addition of OLDENLANDIA DIFFUSA to Kilkyungtang combanation enhanced the cytotoxic activity of Kilkyungtang against A549 and B16-Fo eells by 20% and 50%, respectively. The Oldenlandia-added kilkyungtang also potentiated the cytotoxicities of mitomycine Cand 5-fluorouracil. ar-tunnerone. isolated from the root of Curcuma longa, potentiated the cytotoxic activity of sesquiphellandrene(isolated from the same root), aurapten(isolated from Aurantii semen)or cyclophosphamide by 10 times. The purpose of the processing(修治) of Chinese grugs is to remove unusable parts of plants and to eliminate toxicities as well as to produse new active components in drugs. On a occasion of study on the anthelmintic drugs against the chinese fluke(Clonorchis sinesis, (肝디스토마), we have observed that the processed mume fruit(鳥梅) possessed a very very potent clonorchicidal effect, while the methanol extract of the non-processed fruit inactive. The active component was isolated from the processed mume and identified as 5-hydroxymethylfurfuryl aldehyde. This substance dose not occur in the immature fruit and was found only in the processed one. Wehave heated the immature fruit in an oven at $90^{\circ}C$ for 52 hrs and found that the heated fruit eame clonorchidal. As demonstrated in these and other example cited in this presentation, the natural products chemistry is contributory to univeiling the drug effect ensued from the processing and the synergic effect of Oriental medical drug combinations, and to rationalization or modernization of the traditional medicine.

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Design, Synthesis, Antitumor Activity and Mode of Action of Novel Oxiranyl and Thiiranyl Phenol Derivatives

  • Yang, Zunhua;Kang, Jin-Ah;Kim, Won-Hee;Park, Ah-Young;Kim, Hyung-Sik;Kim, Jung-Su;Kim, Jin-Ah;Gong, Ping;Jeong, Lak-Shin;Moon, Hyung-Ryong
    • Bulletin of the Korean Chemical Society
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    • 제30권7호
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    • pp.1463-1469
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    • 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.