• Archives of Pharmacal Research
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• 제22권3호
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• pp.279-287
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• 1999

Therapeutic use of anti-inflammatory steroids is limited due primarily to their systemic suppressive effects on pituitary function and the immune system.. To overcome the clinical limitation, a new approach toward the discovery of non-systemic anti-inflammatory steroids is based upon the antedrug concept introduced by this laboratory. The new concept describes locally active agents which are designed to undergo a predictable biotransformation to inactive metabolites upon entry into systemic circulation from the applied site. Thus, true antedrugs are devoid of systemic adverse effects. In a continuing effort, 16$\alpha$-carboxylate and isoxazoline derivatives of prednisolone have been synthesized and screened. In the croton oil-induced ear edema bioassay, the following relative potencies were obtained setting hydrocortisone=1.0; 3a, 1.5; 3b, 3.1; 4a, 4.0; 4b, 12.2; 5b, 8.2; 6b, 11.2; 7a, 1.9; 7b, 4.1; 8a, 3.3; 8b 6.8; 9a, 0.7; 9b 8.6; 10a 2.6; 10b, 7.4. Results of the five-day bioassay indicated that, in contrast to the parent compound, the novel steroidal antedrugs did not significantly alter body weight gain, thymus weights, adrenal weights or plasma corticosterone levels. Taken together, the antedrug concept appears to be a fundamentally sound strategy for the separation of local anti-inflammatory activity form systemic adverse effects.

• Asian Pacific Journal of Cancer Prevention
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• 제15권15호
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• pp.6343-6347
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• 2014

Multi-target drug design, in which drugs are designed as single molecules to simultaneously modulate multiple physiological targets, is an important strategy in the field of drug discovery. QT-011, a tamibarotene-furoxan derivative, was here prepared and proposed to exert synergistic effects on antileukemia by releasing nitric oxide and tamibarotene. Compared with tamibarotene itself, QT-011 displayed stronger antiproliferative effects on U937 and HL-60 cells and was more effective evaluated in a nude mice U937 xenograft model in vivo. In addition, QT-011 could release nitric oxide which might contribute to the antiproliferative activity. Autodocking assays showed that QT-011 fits well with the hydrophobic pocket of retinoic acid receptors. Taken together, these results suggest that QT-011 might be a highly effective derivative of tamibarotene and a potential candidate compound as antileukemia agent.

• 한국항해항만학회:학술대회논문집
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• 한국항해항만학회 2000년도 춘계학술대회논문집
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• pp.64-71
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• 2000

Yard cranes are very useful equipments for handling of heavy containers. But rope-driven yard cranes must have a little of sway and skew motion because ropes are passive mechanical device. So many researches have been concentrated on anti-sway algorithm controlling trolley speed. These approaches require sway angle. But it is very difficult to know sway angle and its derivative. Therefore control algorithm of trolley speed is not practical in general. On the contrary, control strategy using auxiliary rope is very useful to sway control of yard crane because rope length is shorter than quay-side container cranes. In this paper, we derive equations of motion of trolley system which have anti-sway controller to use auxiliary rope. And we propose the control strategy and analyse the behavior of the proposed system.

• 한국항해항만학회:학술대회논문집
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• 한국항해항만학회 2000년도 추계학술대회논문집
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• pp.143-151
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• 2000

Yard cranes are very useful equipments for handling of heavy containers. But rope-driven yard cranes must have a little of sway and skew motion because ropes are passive mechanical device. So many researches have been concentrated on anti-sway algorithm controlling trolley speed. These approaches require sway angle. But it is very difficult to know sway angle and its derivative. Therefore control algorithm of trolley speed is not practical in general. On the contrary, control strategy using auxiliary rope is very useful to sway control of yard crane because rope length is shorter than quay-side container cranes. In this paper, we derive equations of motion of trolley system which have anti-sway controller to use auxiliary rope. And we propose the control strategy and analyse the behavior of the proposed system.

• Natural Product Sciences
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• 제15권1호
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• pp.22-26
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• 2009

Phytochemical investigation of the roots of Echiochilon fruticosum resulted in the isolation of two naphthoquinone derivatives. Compound 1 was identified as anhydroalkanin while compound 2 was identified as a new derivative 5-hydroxy 8-methoxy 2-(4-methylpent-1,3-dienyl) naphthalene-1,4-dione named as echiochiloquinone. In addition, caffeic acid 3, caffeic acid methyl ester 4 were isolated. The structures were determined by physical, chemical and spectral methods. The anti-inflammatory activity of the root extracts and compound 2 was evaluated utilizing both cotton pellet-induced and carragenin-induced rat paw edema. The ulcerogenic effect was also studied.

• 한국산학기술학회:학술대회논문집
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• 한국산학기술학회 2001년도 춘계학술대회 발표논문집
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• pp.295-297
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• 2001

본 발명의 Puromycin 유도체인 Cystocin 화합물은 유기 합성에 의해 제조된 물질이 아니라 방선균 계열의 신균주인 Streptamyces sp GCA0001로부터 추출된 신규 물질로서, 항박테리아, 항종양 및 항바이러스 활성 등의 생물학적 미생물 활성면에서 종래의 Puromycin 화합물에 비해 현저히 뛰어난 효과를 지니고 있고 Streptomyces sp GCA0001로부터 추출, 분리 및 정제 과정을 통해 제조된 자연의 선택의 과정을 거친 화합물이므로, Puromycin을 대체할 수 있는 획기적인 물질로 볼 수 있다.

• Journal of Microbiology and Biotechnology
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• 제16권12호
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• pp.1968-1976
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• 2006

Recombinant E. coli ACV 1003 (recA:: lacZ) was used to measure low concentrations of DNA-damaging chemicals, which produce $\beta$-galactosidase via an SOS regulon system. Very low $\beta$-galactosidase activities of less than 0.01 unit/ml, $\beta$-galactosidase produced through an SOS response corresponding to the 10 ng/ml (ppb) of DNA damaging chemicals in the environment, can be rapidly determined by using an alternative interferometric biosensor with optically flat thin films of porous silicon rather than by the conventional time-consuming Miller's enzyme assay as well as the ELISA method. fu order to enhance the sensitivity in the interferometry, it needs to obtain more uniform distribution and higher biolinking efficiency, whereas interferometric sensing is rapid, cheap, and advantageous in high throughput by using a multiple-well-type chip. In this study, pore size adjusted to 60 nm for the target enzyme $\beta$-galactosidase to be bound on both walls of a Si pore and a calyx crown derivative was apllied as a more efficient biolinker. Furthermore, anti-$\beta$-galactosidase was previously functionalized with the biolinker for the target $\beta$-galactosidase to be specifically bound. When anti-$\beta$-galactosidase was bound to the calyx-crown derivative-linked surface, the effective optical thickness was found to be three times as high as that obtained without using anti-$\beta$-galactosidase. The resolution obtained was very similar to that afforded by the time-consuming ELISA method; however, the reproducibility was still unsatisfactory, below 1 unit $\beta$-galactosidase/ml, owing to the microscopic non-uniform distribution of the pores in the etched silicon surface.

• Journal of Ginseng Research
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• 제35권2호
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• pp.200-208
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• 2011

Ginsenoside (G) $Rp_1$ is a ginseng saponin derivative with anti-cancer and anti-inflammatory activities. In this study, we examined the mechanism by which G-$Rp_1$ inhibits inflammatory responses of cells. We did this using a strategy in which DNA constructs containing cyclooxygenase (COX)-2 and inducible nitric oxide synthase (iNOS) promoters were transfected into HEK293 cells. G-$Rp_1$ strongly inhibited the promoter activities of COX-2 and iNOS; it also inhibited lipopolysaccharide induced upregulation of COX-2 and iNOS mRNA levels in RAW264.7 cells. In HEK293 cells G-$Rp_1$ did not suppress TANK binding kinase 1-, Toll-interleukin-1 receptor-domain-containing adapter-inducing interferon-${\beta}$ (TRIF)-, TRIF-related adaptor molecule (TRAM)-, or activation of interferon regulatory factor (IRF)-3 and nuclear factor (NF)-${\kappa}$B by the myeloid differentiation primary response gene (MyD88)-induced. However, G-$Rp_1$ strongly suppressed NF-${\kappa}$B activation induced by I${\kappa}$B kinase (IKK)${\beta}$ in HEK293 cells. Consistent with these results, G-$Rp_1$ substantially inhibited IKK${\beta}$-induced phosphorylation of $I{\kappa}B{\alpha}$ and p65. These results suggest that G-$Rp_1$ is a novel anti-inflammatory ginsenoside analog that can be used to treat IKK${\beta}$/NF-${\kappa}$B-mediated inflammatory diseases.

• Biomolecules & Therapeutics
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• 제16권4호
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• pp.370-376
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• 2008

Ginsenoside Rp1 (G-Rp1) is a ginseng saponin derivative with chemopreventive and anti-cancer activities. In this study, we examined the regulatory activity of G-Rp1 on the functional activation of macrophages. G-Rp1 remarkably inhibited TNF-$\alpha$ production, LPS-induced cell cytotoxicity, NO production, ROS generation, and phagocytic uptake from lipopolysacchride (LPS)-activated RAW264.7 cells. According to structural feature study using several G-Rp1 analogs, two carbohydrates (glucose-glucose) at R1 position were observedto be highly effective, compared to other structural derivatives. Although the inhibitory activities of G-Rp1 on macrophage functions were not remarkable, several points that G-Rp1 was known to be safe, and that this compound was orally effective, suggest that G-Rp1 may be beneficial in treating macrophage-mediated immunological diseases.

• 한국식품영양학회지
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• 제28권5호
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• pp.880-893
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• 2015

Taurine is an abundant amino acid in many animals, including humans. Relatively large amounts of taurine are found in leukocytes, heart, muscles, retinas, kidneys, bones, and liver. Taurine has antioxidant effects; it reacts with hydrogen peroxide to prevent oxidation of the cell membrane. Taurine enhances the effects of anticancer drugs, while also reducing side effects, and taurolidine, a taurine derivative, has been shown to exhibit anti-cancer effects without notable side effects in several types of cancer. Taurine aids in cholesterol metabolism by increasing the rate of synthesis of bile acids, and, thus, reduces triglyceride levels. In addition, taurine is involved in the growth and differentiation of nerve cells and is associated with some neurological disorders. Taurine aids in bone formation and prevents bone dissolution. Moreover, taurine prevents liver damage from a variety of drugs and, thus, protects the liver. Taurine is involved in the development and function of the retina and lens. It also has anti-atherosclerotic and anti-thrombotic effects that protect against cardiovascular disease. Taurine may have additional physiological functions, and warrants further investigation.