• Environmental Analysis Health and Toxicology
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• 제13권3_4호
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• pp.87-94
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• 1998

The use of cisplatin is limited by severe side effects such as renal toxicity. Our platinum-base drug discovery is aimed at developing drugs capable of diminishing toxicity and improving antitumor activity. We synthesized new Pt (II) complex analogue [Pt (cis-DACH)(DPPP)]. 2NO$_3$ (PC) containing cis-1,2-diaminocyclohexane as a carrier ligand and 1,3-bis(diphenylphosphino) propane as a leaving group. Furthermore, nitrate was added to improved the solubility. In this study, its structure was determined and its antitumor activity against SKOV-3 and NIH-OVCAR-3 human ovarian adenocarcinoma, and in vitro cytotoxicity was determined against primary cultured rabbit kidney proximal tubular and renal cortical cells of human kidney using colorimetric MTT assay. PC demonstrated acceptable antitumor activity against SKOV-3 and NIH-OVCAR-3 human ovarian adenocarcinoma and significant activity as compared with that of cisplatin. The toxicity of PC was found quite less than that of cisplatin using MTT and $^3$H-thymidine uptake tests in rabbit proximal tubular cells and human kidney cortical cells. PC was used for human cortical tissue in 7 weeks hitoculture by the glucose-consumption tests. We determined that the new platinum drug has lower nephrotoxicity than cisplatin. Based on these results, this novel platinum (II) complex compound (PC) represent a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low nephrotoxicity.

• Animal cells and systems
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• 제14권4호
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• pp.343-349
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• 2010

Ultrastructural studies of vitellogenesis in oocytes and follicle cells during oogenesis in female Protothaca (Notochione) jedoensis were investigated by histological and transmission electron microscope observations. In early vitellogenic oocytes, combined activities of the Golgi complex, mitochondria and rough endoplasmic reticulum in the cytoplasm are associated with autosynthetic vitellogenesis. Furthermore, at this time, many coated vesicles at the basal region of the oolemma of the oocyte lead to the formation of vesicles through endocytosis in the cytoplasm. Through the formation of the coated pits on oolemma during vitellogenesis, the uptake of extrafollicular precursors (nutritive materials) occurs in coated vesicles by endocytosis. Therefore, it is assumed that these exogenous materials are involved in heterosynthetic vitellogenesis. During late oogenesis, exogenous yolk precursors (yolk granules), lipid droplets and proteinaceous yolk granules are present in the cytoplasm of late vitellogenic oocytes. In mature oocytes, small yolk granules appear intermingled and form large mature yolk granules. Thus, two processes of vitellogenesis occur in oocytes by way of endogenous autosynthesis and exogenous heterosynthesis. The follicle cells attached to the oocytes appear to play an integral role in vitellogenesis in this study.

• Preventive Nutrition and Food Science
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• 제17권2호
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• pp.129-135
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• 2012

GPAR{elidium (G.) amansii is a red alga widely distributed in the shallow waters around East Asian countries. We investigated the effect of G. amansii on lipid accumulation and ROS (Reactive Oxygen Species) production in 3T3-L1 cells. G. amansii extracts dose-dependently inhibited lipid formation and ROS generation in cultured cells. Our results showed that anti-adipogenic effect of G. amansii was due to the reduction in mRNA expressions of PPAR${\gamma}$(peroxisome proliferator-activated receptor-${\gamma}$) and aP2 (adipocyte protein 2). G. amansii extracts significantly decreased mRNA levels of a ROS-generator, NOX4 (nicotinamide adenine dinucleotide phosphate hydrogen oxidase 4), and increased the protein levels of antioxidant enzymes including SOD1/2 (superoxide dismutases), Gpx (glutathione peroxidase), and GR (glutathione reductase), which can lead to the reduction of ROS in the cell. In addition, the G. amansii extract enhanced mRNA levels of adiponectin, one of the adipokines secreted from adipocytes, and GLUT4, glucose uptake protein. Taken together, our study shows that G. amansii extract inhibited lipid accumulation and ROS production by controlling adipogenic signals and ROS regulating genes.

• Biomolecules & Therapeutics
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• 제8권3호
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• pp.228-234
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• 2000

We have synthesized a novel platinum(II) coordination complex containing trans-ι-1,2-diaminocy-clohexane (DACH) as a carrier ligand and 1,2-dichloroethane (DCE) as a leaving group. A new series of [Pt(trans-ι-DACH)(DCE)](PC) was evaluated for its cytotoxic activity on MKN-45 human gastric adenocar-cinoma cells and normal primary cultured kidney cells. The new platinum complex has demonstrated high efficacy in the cytotoxicity against MKN-45/P, MKN-45/ADM and MKN-45/CDDP cell-lines. The cytotoxicity of PC against rabbit proximal renal tubular cells, human renal cortical cells and human renal cortical tissues, determined by MTT assay, the [$^3H$]-thymidine uptake arid glucose consumption tests, was found to be quite less than those of cisplatin. Based on these results, this novel platinum(II) coordination complex appears to be better for improving antitumor activities with low nephrotoxicity and is a valuable lead in the development of new, clinically available anticancer chemotherapeutic agents.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 2007년도 Proceedings of The Convention
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• pp.129-139
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• 2007

Many modalities of treatment for acquired skin hyperpigmentation are available including chemical agents or physical therapies, but none are completely satisfactory. The ideal depigmenting compound should have a potent. rapid and selective bleaching effect on hyperactivated melanocytes, carry no short- or long-term side-effects and lead to a permanent removal of undesired pigment. acting at one or more steps of the pigmentation process. Depigmentation can be achieved by regulating (i) the transcription and activity of tyrosinase, tyrosinase related protein-1 (TRP-1), tyrosinase related protein-2 (TRP-2), and/or peroxidase; (ii) the uptake and distribution of melanosomes in recipient keratinocytes and (iii) melanin and melanosome degradation and turnover of pigmented keratinocytes. One of the interesting point for development of skin whitening agent is Mitf(Microphthalmia-associated transcription factor). Mitf belongs to the basic helix-loop-helix-zip family of trabscription factors and it is crucial as it regulates both melanocyte proliferation as well as melanogenesis and is the major regulator of tyrosinase and the related enzymes (TRPs), as well as many melanosome structural proteins such as pMel17. Recently, we developed MITF-down-regulating agents from natural and synthetic sources, which have anti-melanogenic effect on in vitro and in vivo. We suggested that potent MITF-down regulating agents might be used for skin whitening cosmeceuticals.

• 약학회지
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• 제44권5호
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• pp.399-405
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• 2000

We have synthesized a novel platinum (II) coordination complex containing trans-ι-1,2-diaminocyclohexane (DACH) as a carrier ligand and 1,2-bis (diphenylphosphino)ethane (DPPE) as a leaving group. In addition, nitrate was added to improve the water-solubility. A new series of [Pt (trans-ι-DACH) (DPPE)].2NO$_3$(PC) was evaluated for its cytotoxic activity on MKN-45 human gastric adenocarcinoma cells and normal primary cultured kidney cells. PC has demonstrated high levels of cytotoxicity against MKN-45/S, MKN-45/ADR and MKN-45/CDDP cells. The cytotoxicity of PC against rabbit proximal renal tubular cells, human renal cortical cells, and human renal cortical tissues, determined using the MTT assaying technique, the ($^3$H)-thymidine uptake and the glucose consumption tests, was found to be quite less than those of cisplatin. Based on these results, this novel platinum (II) coordination complex appears to be better for improving antitumor activities with low nephrotoxicity and is a valuable lead in the development of new clinically available anticancer chemotherapeutic agents.

• 한국약용작물학회:학술대회논문집
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• 한국약용작물학회 2006년도 Proceedings of The Convention of The Korean Society of Applied Pharmacology
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• pp.23-39
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• 2006

The application of the knowledge from the Human Genome Project to clinical medicine will be through both industrial drug development and the application of pharmacogenomics (PG) to patient care. The slow uptake of clinical innovations into clinical practice can be frustrating, but understanding the history of acceptance and sustaining medical innovation is critically important to position PG to succeed. This primarily means that PG tests must have legitimacy; they must be thoroughly validated, must be cost-effective, must be widely accepted by medical practitioners, must be supported by public policy, and must have a way of being easily incorporated into current medical practice. They must also lead to actionalble decisions by health care providers for their patients. Innovative PG assays should be tested in the best US laboratories, and reimbursement for testing must be accepted at the federal and state level. The companies providing these PG tests should be capable of supporting the interpretation and use of the test throughout medical practice. Advances such as the addition of PG information to drug labeling and the routine use of validated biomarkers to determine choice of cancer chemotherapy have been made. The PG research community must pay attention to the principles that have been previously described for acceptance and sustaining medical innovations in order for PG to be widely accepted in clinical medical practice.

• International Journal of Oral Biology
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• 제49권1호
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• pp.10-17
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• 2024

Glutamate-mediated oxidative stress causes neuronal cell death by increasing intracellular Ca²⁺ uptake, reactive oxidative species (ROS) generation, mitogen-activated protein kinase (MAPK) activation, and translocation of apoptosis-inducing factor (AIF) to the nucleus. In the current study, we demonstrated that corydaline exerts potent neuroprotective effects against glutamate-induced neurotoxicity. Treatment with 5 mmol/L glutamate increased cellular Ca²⁺ influx, ROS generation, MAPK activation, and AIF translocation. In contrast, corydaline treatment decreased cellular Ca²⁺ influx and ROS generation. Western blot analysis revealed that glutamate-mediated MAPK activation was attenuated by corydaline treatment. We further demonstrated that corydaline treatment inhibited the glutamate-mediated translocation of AIF to the nucleus. We propose that corydaline is a promising lead structure for the development of safe and effective neuroprotectants.

• 한국환경농학회지
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• 제28권2호
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• pp.131-138
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• 2009

비오염 지역인 '06년 "탑라이스(Top-rice)" 생산단지 논토양에서 채취한 토양, 볏짚, 정조, 왕겨, 현미, 쌀겨 및 백미를 분석한 결과 다음과 같다. 논토양 중 비소 1.235 mg/kg, 카드뮴 0.094 mg/kg, 구리 4.412 mg/kg, 납 4.728 mg/kg 및 수은 0.0279 mg/kg으로 우리나라 토양환경보전법상 중금속 오염 우려 및 대책기준을 초과하는 지역은 없었다. 백미 중 비소 0.051 mg/kg, 카드뮴 0.040 mg/kg, 구리 0.345 mg/kg, 납 0.065 mg/kg 및 수은 0.0015 mg/kg으로 잔류허용기준을 초과하는 시료는 없었다. 벼에 흡수.이행된 중금속은 대부분 볏짚에 높게 분포하였고 그 다음으로 쌀겨 부위가 약간 높게 분포 하였다. 그 밖에 정조, 왕겨, 현미 및 백미 중에는 비슷한 농도로 낮게 분포하는 것을 알 수 있었다. 토양 중 중금속과 백미 중 중금속간 흡수기울기는 카드뮴(Cd 0.431) > 구리(Cu 0.054) ${\fallingdotseq}$ 수은(Hg 0.052) > 비소(As 0.021) >> 납(Pb 0.008) 순으로 토양 중 카드뮴이 벼에 흡수되어 쌀로 쉽게 이행되어 축적될 가능성이 제일 컸다. 벼에 흡수된 구리와 수은도 흡수이행이 용이하였고, 비소와 납은 거의 쌀로 이행되지 않았다. 벼의 지상부로 흡수.이행된 중금속 중 63.3-93.4%는 볏짚에 존재하였으며, 정조에 6.6-36.7%, 왕겨에 0.6-5.7%, 현미에 3.2-31.3%, 쌀겨에 0.8-4.6% 그리고 백미에 1.1-26.7%가 분포하는 것으로 나타났다. 카드뮴의 경우 지상부로 흡수된 양의 26.7-31.3%가 백미 또는 현미에 분포하였다.

• 한국환경농학회지
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• 제19권3호
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• pp.213-217
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• 2000

중금속 오염토양에 대한 식물복원법(phytoremediation)중 phytoextraction을 적합한 식물종의 탐색을 위하여 비식용식물인 섬유류 3종, 화훼류 3종 및 수목류 5종을 대상으로 Cd과 Pb을 각각 15, $100\;mg\;kg^{-1}$ 으로 조절하여 처리한 토양에서 pot 재배한 후 식물중에 흡수된 함량 및 그 흡수량을 조사하였다. 식물의 건물생산량은 양황철, 물푸레나무, 사철나무 등 수목류가 섬유류 및 화훼류보다 높게 나타났다. 식물의 부위별 Cd 및 Pb함량은 줄기와 잎보다 뿌리에서 높았고, 식물별 Cd 함량은 채송화, 메리골드, 목화, 아마 순으로 높았으며 Pb 함량은 대마 및 아마에서 높게 나타났다. 식물의 Cd 및 Pb 총 흡수량은 양황철, 사철나무, 물푸레나무, 영산홍 순으로 높게 나타났다. 식물의 Cd 및 Pb 총 흡수량은 시험후 토양에 잔류한 Cd, Pb 함량과 고도의 부의 상관을 보였다. 식물의 건물생산량 및 흡수량을 볼 때 양황철, 사철나무, 물푸레나무 및 영산홍 등이 토양정화식물로의 가치가 있다고 생각된다.