• 제목/요약/키워드: $In$ $vitro$ degradation

검색결과 348건 처리시간 0.024초

$Cu^{2+}$-Anthraquinone Complexes : Formation, Interaction with DNA, and Biological Activity

  • Ko, Thong-Sung;Maeng, Hack-Young;Park, Mi-Kyeong;Park, Il-Hyun;Park, In-Sang;Kim, Byoung-Sun
    • Bulletin of the Korean Chemical Society
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    • 제15권5호
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    • pp.364-368
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    • 1994
  • Growth inhibition potency of the anthraquinones, anthraquinone-1,5-disulfonic acid and carminic acid, for Sarcoma 180 and L1210 leukemia cells in vivo and in vitro, was induced by the divalent transition metal ion, $Cu^{2+}$. On the other hand spectroscopic titration data show that the anthraquinone drugs form $Cu2^+$ chelate complexes (carminic acid : $Cu^{2+}$ = 1 : 6; anthraquinone-1,5-disulfonic acid : $Cu^{2+}$ = 1 : 3). Furthermore the $Cu^{2+}$-drug complexes associate with DNA to form the $Cu^{2+}$-anthraquinone-DNA ternary complexes. The formation of the complexes was further supported by the $H_2O_2-dependent$ DNA degradation, which can be inhibited by ethidium bromide, caused by the $Cu^{2+}$-drug complexes. It is likely that the $Cu^{2+}$-mediated cytotoxicity of the anthraquinone drugs is related with the $Cu^{2+}-mediated$ binding of the anthraquinone drugs to DNA and DNA degradation.

Evaluation of In Vitro Release Profiles of Fentanyl-Loaded PLGA Oligomer Microspheres

  • Gilson Khang;Seo, Sun-Ah;Park, Hak-Soo;John M. Rhee;Lee, Hai-Bang
    • Macromolecular Research
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    • 제10권5호
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    • pp.246-252
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    • 2002
  • In order to the development of the delivery device of long-acting local anesthetics for postoperative analgesia and control of chronic pain of cancer patient, fentnyl-loaded poly (L-lactide-co-glycolido) (PLGA, molecular weight, 5,000 g/mole; 50 : 50 mole ratio by lactide to glycolide) microspheres (FMS) were studied. FMS were prepared by an emulsion solvent-evaporation method. The influence of several preparation parameters such as initial drug loading, PLGA concentration, emulsifier concentration, oil phase volume, and fabrication temperature has been investigated on the fentanyl release profiles. Generally, the drug showed the biphasic release patterns, with an initial diffusion followed by a lag period before the onset of the degradation phase, but there was no lag time in our system. Fentanyl was slowly released from FMS over 10 days in vitro with a quasi-zero order property. The release rate increased with increasing drug loading as well as decreasing polymer concentration with relatively small initial burst effect. From the results, FMS may be a good formulation to deliver the anesthetic for the treatment of chronic pain.

Characterization of Biocompatible Polyelectrolyte Complex Multilayer of Hyaluronic Acid and Poly-L-Lysine

  • Hahn, Sei-Kwang;Allan S. Hoffman
    • Biotechnology and Bioprocess Engineering:BBE
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    • 제9권3호
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    • pp.179-183
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    • 2004
  • A biocompatible polyelectrolyte complex multilayer (PECML) film consisting of poly-L-lysine (PLL) as a polycation and hyaluronic acid (HA) as a polyanion was developed to test its use for surface modification to prevent cell attachment and protein drug delivery. The formation of PECML through the electrostatic interaction of HA and PLL was confirmed by contact angle measurement, ESCA analysis, and HA content analysis. HA content increased rapidly up to 8 cycles for HA/PLL deposition and then slightly increased with an increasing number of deposition cycle. In vitro release of PLL in the PECML continued up to 4 days and ca. 25% of HA remained on the chitosan-coated cover glass after in vitro release test for 7 days. From the results, PECML of HA and PLL appeared to be stable for about 4 days. The surface modification of the chitosan-coated cover glass with PECML resulted in drastically reduced peripheral blood mononuclear cell (PBMC) attachment. Concerned with its use for protein drug delivery, we confirmed that bovine serum albumin (BSA) as a model protein could be incorporated into the PECML and its release might be triggered by the degradation of HA with hyaluronidase.

Nitric Oxide-induced Protein S-nitrosylation Causes Mitochondrial Dysfunction and Accelerates Post-ovulatory Aging of Oocytes in Cattle

  • Niu, Ying-Jie;Zhou, Dongjie;Zhou, Wenjun;Nie, Zheng-Wen;Kim, Ju-Yeon;Oh, YoungJin;Lee, So-Rim;Cui, Xiang-Shun
    • 한국동물생명공학회지
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    • 제35권1호
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    • pp.102-111
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    • 2020
  • Nitric oxide (NO)-induced protein S-nitrosylation triggers mitochondrial dysfunction and was related to cell senescence. However, the exact mechanism of these damages is not clear. In the present study, to investigate the relationship between in vitro aging and NO-induced protein S-nitrosylation, oocytes were treated with sodium nitroprusside dihydrate (SNP), and the resultant S-nitrosylated proteins were detected through biotin-switch assay. The results showed that levels of protein S-nitroso thiols (SNO)s and expression of S-nitrosoglutathione reductase (GSNOR) increased, while activity and function of mitochondria were impaired during oocyte aging. Addition of SNP, a NO donor, to the oocyte culture led to accelerated oocyte aging, increased mitochondrial dysfunction and damage, apoptosis, ATP deficiency, and enhanced ROS production. These results suggested that the increased NO signal during oocyte aging in vitro, accelerated oocyte degradation due to increased protein S-nitrosylation, and ROS-related redox signaling.

Effects of Defaunation on Fermentation Characteristics, Degradation of Ryegrass Hay and Methane Production by Rumen Microbes In Vitro When Incubated with Plant Oils

  • Qin, Wei-Ze;Li, Cheng-Yun;Choi, Seong-Ho;Jugder, Shinekhuu;Kim, Hyun-Ju;Lee, Sang-Suk;Song, Man-Kang
    • 한국초지조사료학회지
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    • 제34권3호
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    • pp.193-201
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    • 2014
  • This study was conducted to examine the effects of defaunation (removal of live protozoa) on fermentation characteristics, degradation of ryegrass hay and $CH_4$ (methane) production by rumen microbes when incubated with plant oils (SO, sunflower oil and LO, linseed oil) in vitro. Sodium lauryl sulfate (0.000375 g/ml) as a defaunation reagent was added into the culture solution and incubated anaerobically up to 24 h at $39^{\circ}C$. pH from defaunation was increased for all treatments from 6 h incubation times (p<0.01-0.001) compared with those from fauantion. Concentration of ammonia-N from defaunation is higher than that from faunation at 3 h (p<0.001), 12 h (p<0.05) and 24 h (p<0.001) incubation times. Defaunation decreased (p<0.01-0.001) total volatile fatty acid concentration at all incubation times. Molar proportions of $C_2$ (acetate, p<0.05-0.001) and butyrate (p<0.01-0.001) were also decreased by defaunation at all incubation times. Molar proportion of $C_3$ (propionate), however, was increased by defaunation at all incubation times (p<0.001). Thus the rate of $C_2$ to $C_3$ was decreased by defaunation at all incubation times (p<0.001). Defaunation decreased ED (effective degradability) of dry matter (p<0.001) and ED of neutral detergent fiber (p<0.001) of ryegrass hay. Defaunation decreased total gas, $CH_4$ production, $CH_4$ % in total gas and $CH_4/CO_2$ at all incubation times (p<0.001). Oil supplementation decreased total gas (p<0.05-0.001), $CH_4$ production (p<0.001) and $CH_4$ % in total gas (p<0.001) compared with control at all incubation times. The result of this study showed that defaunation combined with oil supplementation may cause an alteration of microbial communities and further medicate the fermentation pattern, resulting in both reduction of degradation of ryegrass hay and $CH_4$ production. No difference, however, was observed in all the examinations between SO and LO.

Inhibitory Effects of β-Glycyrrhetinic Acid on Tumor Necrosis Factor-α Production in RAW 264.7 Cells

  • Park, Kyoung-Sik
    • Journal of Applied Biological Chemistry
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    • 제53권3호
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    • pp.147-153
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    • 2010
  • $\beta$-glycyrrhetinic acid (GA), the active principle of licorice (Glycyrrhiza glabra L.) has been reported to exhibit anti-inflammatory properties in different animal models. In this study, the effects of GA on the production of inflammatory mediators including tumor necrosis factor (TNF)-$\alpha$, interleukin (IL)-6, nitric oxide (NO), and prostaglandin E (pGE)-2 were examined in RAW 264.7 cells in vitro. Furthermore, to elucidate a possible mechanism for the inhibitory effect of GA on the production of TNF-$\alpha$, it was investigated whether the treatment of GA affects the I-${\kappa}B{\alpha}$ degradation and subsequent nuclear translocation of NF-${\kappa}B$. Various inflammatory responses were induced in the culture system by treating with a lipopolysaccharide (LPS). GA showed anti-inflammatory activities in dose-dependant manner with $IC_{50}$ of $5.4{\mu}M$ by inhibiting the production of TNF-$\alpha$ in RAW 264.7 cells. In addition, the treatment of GA blocked both I-${\kappa}B{\alpha}$ degradation and the nuclear translocation of NF-${\kappa}B$ from cytosol to nucleus. However, it did not affect the production of IL-6, NO, and PGE-2, implying the direct blocking of the production of TNF-$\alpha$ resulting from both the I-${\kappa}B{\alpha}$ degradation and the nuclear translocation of NF-${\kappa}B$. This finding might provide the underlying mechanism to explain the reported anti-inflammatory activities of GA in animal models.

새로운 반응기구에 의한 bradykinin 유사물의 합성 (Synethesis of bradykinin analogues by new reaction vessel)

  • 최청
    • Applied Biological Chemistry
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    • 제34권4호
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    • pp.334-338
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    • 1991
  • 고상법으로 새로운 반응기구에 의한 bradykinin 및 $(D-Phe7\;-Leu^8)$ bradykinin을 합성하였다. Coupling은 N, N'-dicyclohexylcarbodiimide로 행하였으며 HBr 용액으로 cleavage한 후 조펩티드는 high pressure liquid chromatography로 정제하였다. 이들 펩티드의 순도는 paper chromatography, thin layer chromatography, paper electrophoresis, 융점측정기 및 아미노산기분석기에 의하여 분석하였다. Endopeptidase인 ${\alpha}-chymotrypsin$과 trysin, exopeptidase인 carboxypeptidase A와 leucine aminopeptidase를 사용하여 in vitro 상에서 이들 펩티드의 분해실험을 하였다. ${\alpha}-Chymotrypsine$ 및 carboxypeptidase A에 의하여 이들 펩티드는 빠르게 분해하였으나 leucine aminopeptidase는 N-말단의 2번 위치에 proline의 imino결합 때문에 분해하지 않았다.

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In Vitro Activities of 2,2'-Dipyridyl Against Trichomonas vaginalis, Candida albicans, and Gardnerella vaginalis

  • Ryu, Jae-Sook;Min, Duk-Young;Kim, Myeong-Cheol;Kim, Nam-Sik;Shin, Myeong-Heon
    • Journal of Microbiology and Biotechnology
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    • 제11권1호
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    • pp.124-130
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    • 2001
  • The in vitro activities of 2,2'-dipyridyl, an iron-chelator, against clinical isolates of Trichomonas vaginalis, Candida albicans, and Gardnerella vaginalis was evaluated and compared with those of four other vaginal suppositories, ornidazole, clotrimazole, povidone-iodine, and $Cenacert^{\circledR}$ (Methylbezethonium Chloride mixed with 9-aminoacrydine undecylenate and hydrochloric acid N-myristyl-3-hydroxy butyl amine). The 2,2'-dipyridyl killed T. vaginalis and G. vaginalis at concentrations of $410\;{\mu}g/ml$ and $205\;{\mu}g/ml$, respectively, however, ths agent was less active against C. albicans (80% of which was inhiited at $410\;{\mu}g/ml$). The inhibition of these three pathogens by 2,2'-dipyridyl was similar to clotrimazole. In addition, the effect of 2,2'-dipyridyl on the ultrastructure of T. vaginalis, C. albicans, an G. vaginalis was examined. Transmission electron microscopy indicated that 2,2'-dipyridyl induced modifications of the cellular contents and cell envolope concumitant with the degradation of the three pathogens. These results suggest that 2,2'-dipyridyl has an inhibitory effect on C. albicans and G. vaginalis, as well as T. vaginalis.

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담배 형질전환 식물체를 이용한 γ-Benzenehexachloride의 분해 (The γ-Benzenehexachloride Degradation Using Transgenic Tobacco Plant)

  • 이정경;박순기;정일경
    • Journal of Plant Biotechnology
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    • 제30권1호
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    • pp.103-108
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    • 2003
  • 본 연구는 난분해성 농약의 자연분해를 유도하기 위하여 ${\gamma}$-BHC를 탄소원으로 이용하여 호기적으로 자화하는 미생물 (Sphingomonas paucimobilis)에서 분리된 탈염소화효소 중 ${\gamma}$-BHC분해의 첫단계에 관여하는 linA유전자를 담배에 도입하여 BHC에 활성을 나타내는 형질전환 시물체를 만들었다. LinA 유전자를 함유한 pJK 108 백터를 제작하여. Agrobacterium를 이용한 leaf disk transformation 방법으로 담배에 형질전환시켰으며, northern분석 및 Southern분석을 통해 형질전환 개체에서 linA유전자의 도입과 linA유전자 유래의 mRNA가 전사됨을 확인하였다. Western 분석에서 linA단백질의 발현을 확인하였고, gas chromatography를 이용하여 담배 형질전환 개체에서 BHC가 ${\gamma}$-PCCH와 1,2.4-TCB로 분해되는 것을 확인하였다.

Comparative study of some analytical methods to quantify lignin concentration in tropical grasses

  • Velasquez, Alejandro V.;Martins, Cristian M.M.R.;Pacheco, Pedro;Fukushima, Romualdo S.
    • Asian-Australasian Journal of Animal Sciences
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    • 제32권11호
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    • pp.1686-1694
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    • 2019
  • Objective: Lignin plays a relevant role in the inhibition of cell wall (CW) structural carbohydrate degradation. Thus, obtaining accurate estimates of the lignin content in tropical plants is important in order to properly characterize the mechanism of lignin action on CW degradation. Comparing conflicting results between the different methods available for commercial use will bring insight on the subject. This way, providing data to better understand the relationship between lignin concentration and implications with tropical forage degradation. Methods: Five grass species, Brachiaria brizantha cv $Marand{\acute{u}}$, Brachiaria brizantha cv $Xara{\acute{e}}s$(MG-5), Panicum maximum cv Mombaça, Pennisetum purpureum cv Cameroon, and Pennisetum purpureum cv Napier, were harvested at five maturity stages. Acid detergent lignin (ADL), Klason lignin (KL), acetyl bromide lignin (ABL), and permanganate lignin (PerL) were measured on all species. Lignin concentration was correlated with in vitro degradability. Results: Highly significant effects for maturity, lignin method and their interaction on lignin content were observed. The ADL, KL and ABL methods had similar negative correlations with degradability. The PerL method failed to reliably estimate the degradability of tropical grasses, possibly due to interference of other substances potentially soluble in the $KMnO_4$ solution. Conclusion: ADL and KL methods use strong acid ($H_2SO_4$) and require determination of ash and N content in the lignin residues, therefore, increasing time and cost of analysis. The ABL method has no need for such corrections and is a fast and a convenient method for determination of total lignin content in plants, thus, it may be a good option for routine laboratory analysis.