Synthesis and Importance of Bulky Aromatic Cap of Novel SAHA Analogs for HDAC Inhibition and Anticancer Activity

Chun, Pu-Soon,Kim, Won-Hee,Kim, Jung-Su,Kang, Jin-Ah,Lee, Hye-Jin,Park, Ji-Young,Ahn, Mee-Young,Kim, Hyung-Sik,Moon, Hyung-Ryong Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.6

On the basis of potent HDAC-inhibitory activity and anticancer activity of SAHA, novel SAHA derivatives 3a-d and 7 with a bulky cap such as p-dimethylaminophenyl, 4-phenylaminophenyl, 4-phenyloxyphenyl, 9H-fluorenyl or naphthalenyl ring were synthesized starting from the corresponding aryl amines or naphthalenyl acetic acid using an EDC-mediated amide coupling reaction in the presence of HOBt followed by a nucleophilic addition-elimination reaction with hydroxylamine. Compounds 3b, 3c and 3d showed more potent inhibitory activity on total HDACs (14~27-fold), HDAC1 (8~15-fold), HDAC2 (1.3~25-fold) and HDAC7 (1~3-fold) and more potent anticancer activity (2~22-fold) against MCF-7, MDA-MB-231, MCF-7/Dox, MCF-7/Tam, SK-OV-3, LNCaP and PC3 human cancer cell lines than SAHA.

한국, ECERS-R, NAEYC의 유아교육기관 평가지표 비교

이순례(Lee Soon Lye),이현옥(Lee Hyun-Ok),부성숙(Pu Sung Sook) 한국육아지원학회 2009 육아지원연구 Vol.4 No.2

본 연구의 목적은 우리나라 유치원 평가 영역 중 ‘교육환경 영역’의 평가지표를 외국의 ECERS-R, NAEYC 평가지표와 비교․분석하여 차이점을 살펴보는 것이다. 차이점을 분석한 결과, 한국의 지표 내용은 추상적이고 포괄적이면서도 특정 요소 또는 한 두가지 측면을 부분적, 중점적으로 강조한 반면, 외국 지표는 구체적이고 상세하게 평가사항을 기술하면서도 다양한 요소, 다양한 측면을 종합적으로 고려하여 평가하고 있었다. 또한 한국의 지표는 개인적 공간, 교사(성인)나 장애아를 위한 환경 고려 사항이 없는 반면, 외국의 지표는 개인적 공간을 강조함으로써 집단 내에서의 개인적 권리를 강조하고 있었고, 교사와 장애아를 위한 공간 및 시설을 필수적으로 고려하고 있었으며, 다문화 가족도 고려하고 있었다. 그리고 한국의 지표에서는 교육환경과 관련된 건강, 안전 사항이 독립된 다른 영역(건강․안전영역)에서 다루어지고 있는 것에 비해 외국의 지표에서는 교육환경 영역 내에 건강, 안전 사항이 포함되어 다루어지고 있었다. 특히 ‘환경안전’을 강조하여 환경 호르몬, 공기오염, 수질오염 등의 위험으로부터 유아의 안전을 도모하고 있었다. The aim of this study is to compare and analyze differences between Korean Kindergarten accreditation index and ECERS-R and NAEYC's ones in the area of the environment of facilities. The study found that the Korean index was abstract and general and it focused on several factors. However, the foreign indexes were more specific and detailed. At the same time, they evaluated various factors and aspects comprehensively. Although the Korean index didn't consider personal space and environment for teachers and disabled children, the foreign indexes considered individual rights in a group by emphasizing personal space as well as space and facilities for teachers and disabled children. They also considered environments for multi-cultural families. The Korean index included environmental-related health and safety in the health and safety area, which was different from the area of the educational environment. However, the foreign indexes included environmental-related health and safety in the area of the educational environment . Especially, it emphasized 'environmental safety' to reduce the risks of environmental hormones, air pollution, and water pollution and protect children's safety.

REPRODUCTION STUDIES WITH PRANOPROFEN, A NONSTEROIDAL ANTI-INFLAMMATORY AGENT IN RATS-TERATOLOGY TEST

Moon, Hwa-Hwey,Kim, Pu-Young,Cho, Dae-Hyun,Heo, Ok-Soon,Lee, Sung-Hee,Yoon, Tae-Bo,Kim, Soon han The Korean Society of Toxicology Korea Environment 1986 Toxicological Research Vol.2 No.1

Teratological study on pranoprofen, as antiinflammatory agent, was conducted by oral intubation in Sprague-Dawley rats. Pranoprofen was administered doses of 1.0, 2.5 and 5.0mg/kg/day and doze of 0.5mg/kg/day of Indomethacin was used as positive control. The rats were dosed from day 7 to 17 of gestation. At necropsy on day 20 of gestation, pathologically changes of gastroin-testinal system, liver and adrenal gland were examined at the high dose administered group. There were no differences between control and treated group on the number of implantations, the number of alive and dead fetuses, tail length, and external visceral and skeletal malformations.

REPRODUCTION STUDIES WITH PRANOPROFEN: A NONSTEROIDAL ANTINFLAMMATORY AGENT IN RATS-PERINATAL AND POSTNATAL TEST.

Moon, Hwa-Hwey,Kim, Pu-Young,Cho, Dae-Hyun,Heo, Ok-Soon,Park, Sook-Hee,Yoon, Tae-Bo,Kim, Soon han The Korean Society of Toxicology Korea Environment 1986 Toxicological Research Vol.2 No.2

prenatal and postanatal study on pranoprofen, as an antiinflammatory agent, was conducted by oral administration in Sprague-Dawley pregnancy rats from day 17 of gestation to day 21 of after delivery. Pranoprofen was intubated doses of 1.0, 2.5 and 5.0 mg/kg/day and dose of 5.0mg/kg/day of Indomethacin was used as positive control. After delivery, several study indexes such as length of gestation, No. of implantations, No. of live pups, No. of perinatal deaths, sex ratio and No. of malformation were checked and then all the newborns were feeded and investigated physical and behavioral changes.

MUTAGENIC EVALUATION OF PRANOPROFEN, A NEW ANTI-INFLAMMATORY AGENT

Moon, Hwa-Hwey,Kim, Pu-Young,Yun, Tai-Bo,Jo, Dae-Hyun,Park, Han-Soo,Heo, Ok-Soon,Kim, Soon-Han,Choi, Suk-Hee The Korean Society of Toxicology Korea Environment 1987 Toxicological Research Vol.3 No.1

The mutagenicity of pranoprofen, a new antiinflammatory agent primarily used in Japan, was evaluated by employing several different methods such as the Ames test, micronucleus test, and the sister chromatid exchange test. For the Ames test, various doses of pranoprofen (5 and 1 mg, 100, 10, and 1 ${\mu}$g per plate) were applied, with or without the mammalian liver S-9 fraction, to the S. typhimurium LT2. For the micronucleus test, 24 hours after administering the various doses of pranoprofen (200, 100, and 50 mg/kg) to male mice by aral intubation, the femura of each group were isolated and the bone marrow samples were prepared. The micronucleated red cells and the ratio of the polychromatic versus the normochroomatic cells were counted. For the sister chromatid exchange test, the maximal non-cytotoxic concentrations (10 to 0.1 mM pranoprofen) were applied to the culture media of the Chinese Hamster Ovary (CHO) cells for 24 hrs. The numbers of revertant colonies did not increase with the increasing doses of pranoprofen when teseted with various strains of S. typhimurium. In the micronucleus test employing mice, the pranoprofen was identkfied to be a non-clastogen and a non-spindle poison. In the sister chromatid exchange test employing the cultured CHO cells, the pranoprofen did not increase the incidences of chromosomal abnormality. Based on these results, pranoprofen was found to have no mutagenic activity.

벤조[b][1,4]옥사진-3(4H)-치온 유도체의 합성과 이들의 타이로시네이즈 저해 활성

김도현(Do Hyun Kim),천부순(Pu soon Chun),정해영(Hae Young Chung),문형룡(Hyung Ryong Moon) 대한약학회 2017 약학회지 Vol.61 No.1

To investigate whether a “β-phenyl-α,β-unsaturated thiocarbonyl” scaffold can play a key role in tyrosinase inhibition, benzo[b][1,4]oxazine-3(4H)-thione derivatives bearing the scaffold were synthesized through a three-step reaction including Knoevenagel condensation. Four compounds showed not only high binding affinity with tyrosinase on docking simulation but also greater inhibitory activity against mushroom tyrosinase than arbutin. These results indicate that a “β- phenyl-α,β-unsaturated thiocarbonyl” may serve as an important chemical scaffold for potent tyrosinase inhibitors.

ABCB1 C3435T가 신장이식 수혜자에서 tacrolimus의 최저혈중농도에 미치는 영향: 체계적 문헌고찰 및 메타분석

신혜연(Hye Yeon Sin),천부순(Pu soon Chun) 대한약학회 2018 약학회지 Vol.62 No.5

A large number of studies have investigated the influence of ABCB1 C3435T polymorphism on blood trough concentrations of tacrolimus in kidney transplant recipients. However, the results are inconsistent. The aim of the present study was to clarify the effects of ABCB1 C3435T on trough blood levels of tacrolimus in renal transplant recipients at different post-transplantation times. The databases of PubMed, Embase, Ovid, and Cochrane Library were searched for all published studies from inception to March 2018. In addition, reference lists of articles were also examined. Using the Review Manager 5, weighted mean differences of dose-adjusted trough concentration of tacrolimus were pooled to estimate the effects of ABCB1 C3435T on tacrolimus levels. A total of 11 studies (968 recipients) were included in the present metaanalysis. The adult recipients with CC genotype had lower dose-adjusted trough concentration of tacrolimus than the CT and TT carriers at the first week after kidney transplantation (CC vs CT, WMD: -14.82; 95% CI: -24.73, -4.90; p=0.003; CC vs TT, WMD: -30.73; 95% CI: -47.9, -13.57; p=0.0004). Similar results were observed in adult recipients at the first month after transplantation (CC vs CT, WMD: -19.61; 95% CI: -27.66, -11.56; p<0.00001; CC vs TT, WMD: -25.45; 95% CI: -47.68, -3.22; p=0.02). Furthermore, at 3 months, the pediatric and adult recipients with CC or CT genotype had lower dose-adjusted trough concentration than the TT carriers (CT vs TT, WMD: -11.85; 95% CI: -18.65, -5.04; p=0.0006; CC vs TT, WMD: -30.98; 95% CI: -37.46, -24.50; p<0.00001). In addition, at the time of 6 months, the adult recipients carrying 3435C allele had lower dose-adjusted trough concentration than the TT carriers (CC vs CT, WMD: -19.00; 95% CI: -23.60, -14.39; p<0.00001; CT vs TT, WMD: -6.57; 95% CI: -12.87, -0.28; p=0.04; CC vs TT, WMD: -26.46; 95% CI: -32.04, -20.88; p<0.00001). These results imply that the adult recipients carrying ABCB1 3435C allele need higher dose of tacrolimus to prevent acute rejection after kidney transplantation.

포스트 코로나 시대 온라인 플랫폼 프로젝트중심학습을 활용한 전문직 간 교육 프로그램 개발 : 보건계열 대학생을 중심으로

주현정 ( Hyun-jung Ju ),윤보영 ( Bo-young Yoon ),천부순 ( Pu-soon Chun ),김상희 ( Sang-hee Kim ) 대한설비관리학회 2021 대한설비관리학회지 Vol.26 No.2

Online learning has been provided to students in universities due to the spread of COVID-19. Online collaborative learning can support interaction between learners and develop problem-solving and self-directed learning abilities. Interprofessional education (IPE) develops healthcare students as future interprofessional team members by learning together about each others’ roles and practicing collaboration and teamwork, which can provide quality patient care. The purpose of this study is to develop an IPE program utilizing online platform project-based learning. In the IPE program, participants are faculty members and students from three departments―medicine, nursing, and pharmacy. At the phase of design, we defined three core competencies―communication, collaboration, and professionalism―and course objectives, organized student groups and matched the groups with faculty members using a team-teaching model, and selected online platform project-based learning as instructional methods. At the phase of development, we developed learning processes and content for a fifteen-week-long course, including six steps: preparing, selecting, planning, executing, creating, and presenting, and evaluating. We also developed a guide for instructors and strategies for students’ team projects. For instructors to play a role facilitators in an online learning environment, faculty development systems and resources will be needed. Future studies will need to conduct program evaluations to investigate the effectiveness of the IPE program.

DA-125 의 국소자극성

김원배,양중익,이종권,이순복,김대병,김부영,안병옥,백남기 한국응용약물학회 1993 Biomolecules & Therapeutics(구 응용약물학회지) Vol.1 No.1

DA-125, a new anthracycline derivative, shows significant anticancer activities. We conducted a study to examine the local irritating effect of DA-125 using mice and rabbits. In the skin test in mice, intradermal injection of 0.4 ㎎ of DA-125, compared to a dosage of 0.2 ㎎ of adriamycin, had weak irritating potentials to induce skin ulceration and erythematous induration. A dosage of 0.6 ㎎ of DA-125 produced similar degree of lesions in perivascular irritation model to that of 0.2 ㎎ of adriamycin, but the healing time was shorter in the case of mice treated with DA-125. In ocular irritation study in rabbit, the highest M.O.I.(mean ocular irritation index) of 0.5% DA-125 solution was 0.67, therefore DA-125 could be considered as a practically non-irritating anticancer agent. These results suggest that substitution of DA-125 for Adriamycin would reduces the possibility of outbreaks of local irritation and the severity of the lesions.

기니픽을 이용한 자가중합형 레진의 피하이식 독성연구

이종권(Jong-Kwon Lee),류승렬(Seung-Rel Ryu),김대병(Dai-Byung Kim),이선희(Sun-Hee Lee),김부영(Pu-Young Kim),이영순(Yong-Soon Lee) 한국실험동물학회 1997 Laboratory Animal Research Vol.13 No.2