• Journal of Microbiology and Biotechnology
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• 제29권11호
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• pp.1799-1805
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• 2019

Doxorubicin (DOX) is one of the most effective anticancer agents used for the treatment of multiple cancers; however, its use is limited by its short half-life and adverse drug reactions, especially cardiotoxicity. In this study, we found that the conjugate of DOX with APTA12 (Gemcitabine incorporated G-quadruplex aptamer) was significantly more cancer selective and cytotoxic than DOX. The conjugate had an affinity for nucleolin, with higher uptake and retention into the cancer cells than those of DOX. Further, it was localized to the nucleus, which is the target site of DOX. Owing to its mechanism of action, DOX has the ability to intercalate into the nucleotides thus making it a suitable drug to form a conjugate with cancer selective aptamers such as APTA12. The conjugation can lead to selectively accumulate in the cancer cells thus decreasing its potential nonspecific as well as cardiotoxic side effects. The aim of this study was to prepare a conjugate of DOX with APTA12 and assess the chemotherapeutic properties of the conjugate specific to cancer cells. The DOX-APTA12 conjugate was prepared by incubation and its cytotoxicity in MCF-10A (non-cancerous mammary cells) and MDA-MB-231 (breast cancer cells) was assessed. The results indicate that DOX-APTA12 conjugate is a potential option for chemotherapy especially for nucleolin expressing breast cancer with reduced doxorubicin associated side effects.

• 대한약침학회지
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• 제20권3호
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• pp.207-212
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• 2017

Objectives: Study of the mechanisms involved in cancer progression suggests that cyclooxygenase enzymes play an important role in the induction of inflammation, tumor formation, and metastasis of cancer cells. Thus, cyclooxygenase enzymes could be considered for cancer chemotherapy. Among these enzymes, cyclooxygenase 2 (COX-2) is associated with liver carcinogenesis. Various COX-2 inhibitors cause growth inhibition of human hepatocellular carcinoma cells, but many of them act in the COX-2 independent mechanism. Thus, the introduction of selective COX-2 inhibitors is necessary to achieve a clear result. The present study was aimed to determine the growth-inhibitory effects of new analogues of chalcone epoxide as selective COX-2 inhibitors on the human hepatocellular carcinoma (HepG2) cell line. Methods: Estimation of both cell growth and the amount of prostaglandin E2 (PGE2) production were used to study the effect of selective COX-2 inhibitors on the hepatocellular carcinoma cell. Cell growth determination has done by MTT assay in 24 h, 48 h and 72 h, and PGE2 production has estimated by using ELYSA kit in 48 h and 72 h. Results: The results showed growth inhibition of the HepG2 cell line in a concentration and time-dependent manner, as well as a reduction in the formation of PGE2 as a product of COX-2 activity. Among the compounds those analogues with methoxy and hydrogen group showed more inhibitory effect than others. Conclusion: The current in-vitro study indicates that the observed significant growth-inhibitory effect of chalcone-epoxide analogues on the HepG2 cell line may involve COX-dependent mechanisms and the PGE2 pathway parallel to the effect of celecoxib. It can be said that these analogues might be efficient compounds in chemotherapy of COX-2 dependent carcinoma specially preventing and treatment of hepatocellular carcinomas.

• The Korean Journal of Pain
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• 제24권4호
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• pp.179-184
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• 2011

Background: The analgesic mechanisms of cyclooxygenase (COX)-2 inhibitors have been explained mainly on the basis of the inhibition of prostaglandin biosynthesis. However, several lines of evidence suggest that their analgesic effects are mediated through serotonergic or adrenergic transmissions. We investigated the roles of these neurotransmitters in the antinociception of a selective COX-2 inhibitor at the spinal level. Methods: DUP-697, a selective COX-2 inhibitor, was delivered through an intrathecal catheter to male Sprague-Dawley rats to examine its effect on the flinching responses evoked by formalin injection into the hindpaw. Subsequently, the effects of intrathecal pretreatment with dihydroergocristine, prazosin, and yohimbine, which are serotonergic, ${\alpha}1$ adrenergic and ${\alpha}2$ adrenergic receptor antagonists, respectively, on the analgesia induced by DUP-697 were assessed. Results: Intrathecal DUP-697 reduced the flinching response evoked by formalin injection during phase 1 and 2. But, intrathecal dihydroergocristine, prazosin, and yohimbine had little effect on the antinociception of intrathecal DUP-697 during both phases of the formalin test. Conclusions: Intrathecal DUP-697, a selective COX-2 inhibitor, effectively relieved inflammatory pain in rats. Either the serotonergic or adrenergic transmissions might not be involved in the analgesic activity of COX-2 inhibitors at the spinal level.

• Composites Research
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• 제32권1호
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• pp.13-20
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• 2019

본 연구에서는 전기 자동차의 주요 부품 중 하나인, Battery Module의 품질 Issue 및 부품특성 개선을 위해 복합재료를 사용하여 구조보강 하였으며, 단일소재의 단점을 극복할 수 있는 Hybrid 개념의 기구 구조 최적화를 수행하고 성능을 비교하였다. 이를 위해 고전 적층 판 이론(Classical Laminated Plate Theory, CLPT)에 따른 복합재료 주요 설계 변수 도출 및 복합재료 물성 예측 알고리즘에 대해 연구하였으며, 설계된 복합재료의 기계적 물성을 바탕으로 유한요소해석(FEM)을 통해 Battery Module의 성능을 검증하였다. 이를 통해 자동차 Battery 부품의 안정성 및 경량화 등의 부품 특성 개선 여부를 확인할 수 있었다. 최종적으로 검증결과에 따르면 Selective Composite Patch로 보강된 Hybrid Battery Module은 기존 Al Battery Module에 비해 30%의 중량 감소 및 제품 두께 32.5%를 줄일 수 있고, 충격 성능 유지 등 Hybrid 구조의 장점을 입증하였다.

• 대한정형외과학회지
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• 제55권1호
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• pp.9-28
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• 2020

비스테로이드 소염제(non-steroidal anti-inflammatory drugs, NSAIDs)는 세계적으로 관절염과 같은 만성 통증에 가장 흔히 사용되는 약물이며 성분 및 기전에 따라 다양한 종류가 있다. 장기간 사용 시에는 소화기계 및 심혈관계 합병증 등의 다양한 부작용이 발생할 수 있는 것으로 알려져 있다. 기존의 비선택적 NSAID와 유사한 진통 효과를 지니면서 위장관계 내약성을 보완해줄 수 있는 cyclooxygenase-2 (COX-2) 선택적 NSAID가 많은 기대를 모았으나 2004년 및 2005년도에 심혈관계 안전성에 대한 우려로 rofecoxib과 valdecoxib의 허가가 취하되면서 NSAID 약물의 부작용에 관한 관심은 더욱 증가하고 있다. 따라서 각 약물의 부작용 및 상호작용을 고려하여 필요한 약물을 최소한으로 사용하는 것이 매우 중요하다. 본 논문에서는 NSAID 약물을 복용할 때 발생할 수 있는 부작용 및 각 약물의 특성을 숙지하며 비선택적 NSAID 및 COX-2 선택적 NSAID의 사용과 관련된 최근 연구 및 지침에 대해 알아보고자 한다.

• 공업화학
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• 제28권6호
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• pp.619-625
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• 2017

본 연구에서는 하이드로퍼옥시 라디칼 생성단계에서 반응 부산물로 생성되는 과산화수소를 정량하여 수산화라디칼의 생성 및 비스페놀 A (BPA)의 분해특성을 조사하였다. 라디칼 연쇄반응이 일어나지 않는 조건에서는 Criegee mechanism과 동일하게 오존에 의한 직접산화반응만이 BPA를 분해시키는 것으로 나타났다. 라디칼 연쇄반응이 일어나는 pH 6.5 및 9.5의 조건에서는 비선택적 산화반응이 일어나 수산화라디칼의 생성을 간접적으로 확인할 수 있었다. 투입된 촉매에 의한 BPA의 분해효율은 $O_3$/PAC ${\geq}$ $O_3/H_2O_2$ > $O_3$/high pH > $O_3$ alone 공정 순으로 나타났다. 오존/촉매공정들의 산화반응 동안에는 0.03~0.08 mM의 과산화수소가 지속적으로 측정되었다. $O_3$/high pH 공정의 경우, BPA가 반응시작 50 min 만에 완전히 분해되었지만, TOC (총유기탄소) 제거율은 29%로 산화반응 중 생성된 중간물질을 충분히 산화시키지 못하는 것으로 나타났다(선택적 산화반응). $O_3/H_2O_2$ 및 $O_3$/PAC 공정에서는 BPA가 반응시작 40 min 만에 완전히 분해되었으며, TOC 제거율은 각각 57% 및 66% 정도로 반응 중간체들을 산화(비선택적 산화반응)시키는 것으로 나타났다.

• 한국정보처리학회:학술대회논문집
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• 한국정보처리학회 2004년도 춘계학술발표대회
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• pp.1355-1358
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• 2004

This paper describes a modification to the SACK (Selective Acknowledgement) Transmission Control Protocol's (TCP), called SACK TCP with Probing Device, SACK works in conjunction with Probing Device, for improving SACK TCP performance when more than half a window of data lost that is typical in handoff as well as unreliable media. It shows that by slightly modifying the congestion control mechanism of the SACK TCP, it can be made to better performance to multiple packets lost from one window of data.

• 셀메드
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• 제9권2호
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• pp.2.1-2.1
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• 2019

Depression is common psychiatric diseases characterized by diverse physical and emotional symptoms including low mood, loss of interest in pleasurable activities, and feelings of worthlessness. Depression causes of death and disability. The first antidepressant was created by the idea that central serotonin mechanism. Selective serotonin reuptake inhibitor, fluoxetine is the first-line drug in the treatment of depressive disorder and their few side effects as opposed to tricyclic antidepressants. Not all people with depression respond adequately to standard treatments. Korean music playing/listening actions appear to be a reliable approach to developing recovery from depression.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.75.2-75.2
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• 2003

The present study was designed to compare the effects of conotoxin GVIA, a selective blocker of N-type voltage-dependent calcium channels (VDCC) and cilnidipine, a blocker of both L- and N-type VDCC, on the secretion of catecholamines (CA) evoked by cholinergic stimulation and membrane-depolarization in the isolated perfused rat adrenal gland, and also to establish the mechanism of action. 1. The inhibition of the CA secretory response evoked by acetylcholine (5.32 x 10$\^$-3/ ${\mu}$M) was stronger in cilnidipine-treated glands than in conotoxin GVIA-treated glands. (omitted)

• Asian Pacific Journal of Cancer Prevention
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• 제16권2호
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• pp.761-767
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• 2015

Background: In this study, we used Daucus carota oil extract (DCOE) to target acute myeloid leukemia (AML) cells. All the AML cell lines tested were sensitive to the extract while peripheral mononuclear cells were not. Analysis of mechanism of cell death showed an increase in cells positive for annexinV and for active caspases, indicating that DCOE induces apoptotic cell death in AML. Inhibition of the MAPK pathway decreased sensitivity of AML cells to DCOE, indicating that cytotoxicity may be dependent on its activity. In conclusion, DCOE induces selective apoptosis in AML cells, possibly through a MAPK-dependent mechanism.