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Brine Shrimp Bioassay를 이용한 해양생물의 세포독성검색
손병화(Byeng Wha Son),조용진(Yong Jin Cho),이대령(Dae Ryoung Yi),노연숙(Yeon Suk Roh),이선미(Sun Mi Lee),최홍대(Hong Dae Choi) 대한약학회 1993 약학회지 Vol.37 No.5
As a part of chemical study on the bioactive metabolites from marine organisms, we have investigated cytotoxicity using brine shrimp bioassay for each solvent fractions of the marine algae(12 species), marine sponges(3 species), coelenterates(2 species), echinoderms(4 species), marine molluscs(17 species), and ascidians(2 species), respectively. As the results, chloroform extract of Stichopus japonicus (LC50 : 274 mcg/ml), ethyl acetate extract of Anthocidaris crassispina(LC50 : 121mcg/ml), n-butanol extract of Undaria pinnatifida (LC50 : 178mcg/ml), and water extract of Thais clavigera (LC50 : 61mcg/ml) displayed the most significant cytotoxic activity against brine shrimp. Among the marine organisms tested, echinoderms and marine molluscs were thought to be the most active Phylums on screening of new bioactive compounds.
홍조 꼬시래기(Gracilaria verrucosa) 유래의 글리세로당 Floridoside의 화학구조
노연숙,손병화,임광식,최홍대,Roh, Yeon-Suk,Son, Byeng-Wha,Im, Kwang-Sik,Choi, Hong-Dae 한국생약학회 1994 생약학회지 Vol.25 No.2
As part of search for new biologically active substances from marine organism, we have isolated a glyecrol glycoside from the marine red alga Gracilaria verrucosa. The structure of the glycerol glycoside was elucidated as 2-O-${\alpha}-_D$-galactopyranosylglycerol[floridoside(4)] on the basis of spectroscopic and physicochemical evidences.
조용진,정동윤,최홍대,박종희,손병화,Cho, Yong-Jin,Jeong, Dong-Youn,Choi, Hong-Dae,Park, Jong-Hee,Son, Byeng-Wha 한국생약학회 1998 생약학회지 Vol.29 No.3
Two isoflavonoids were isolated from the flowers of Pueraria lobata (Flos puerariae) guided initially fractionation based on brine shrimp lethality assay. The structures were identified as 4',5,7-trihydroxy-6-methoxyisoflavone (tectorigenin) and 4',7-dihydroxy-6-methoxyisoflavone (glycitein), respectively, on the basis of their spectroscopic and physicochemical evidences.
Chul Woo Jeong(정철우),Byeng Wha Son(손병화),Jae Du Ha(하재두),Gun-Do Kim(김군도) 한국생명과학회 2011 생명과학회지 Vol.21 No.3
EGFR kinase의 활성을 억제할 수 있는 억제제는 암뿐만이 아니라 성장성 질환에도 효과적인 치료제가 될 수 있다. 본 연구는 새로운 퀴나졸린계 물질인 화합물 63013과 63033의 EGFR kinase 활성억제 효과를 분석하였다. 이들 물질들은 기존의 디알콕시퀴나졸린의 용해성을 증가시키기 위하여 [1,4]-다이옥시노 퀴나졸린 구조를 가지며 알콕시 곁사슬로 연결되어있다. 화합물 63013과 63033은 A431 인간 피부암세포에서 EGF에의해 유도되는 EGFR의 kinase 활성을 저해, 세포 내에서 EGFR 신호체계에 관여하는 MEK1/2, MAPK p44/42, AKT, STAT3과 같은 하위 분자들의 활성저해 효과를 유도하였다. 이러한 활성저해 효과는 현재 상용화되어 있는 Gefitinib (Iressa<SUP>®</SUP>)와의 비교연구에서 화합물 63013과 63033이 보다 더 낮은 처리 농도에서 EGFR kinase의 활성을 저해하며 암세포의 성장을 억제함을 관찰 할 수 있었다. 따라서 본 연구는 이들 신규 물질들의 EGFR-연관 질환에 대한 EGFR kinase 선택적 억제제로서의 이용 가능성을 제시하고 있다. Inhibitors of EGFR (epidermal growth factor receptor) kinase activity may prove useful to therapeutically intervene in cancer and to treat other proliferative diseases. In this study, we investigated the inhibitive effects of two compounds named 63013 and 63033 possess a [1,4]-dioxino quinazoline structure that links the alkoxy side chains together and their structural characteristics are considered to allow better solubility than the dialkoxyquinazoline derivatives. The EGFR kinase activities of A431 human epidermoid carcinoma cells, stimulated by EGF were inhibited by treatment with 63013 and 63033 in a dose-dependent manner respectively. Consistent with the compound-mediated EGFR kinase suppression, the major EGF-related downstream target molecules, such as MEK1/2, MAPK p44/42, AKT and STAT3, were also suppressed by both compounds. Interestingly, both compounds led to cell growth inhibition at a lower concentration than that of Gefitinib (Iressa<SUP>®</SUP>). Collectively, our study showed that both compounds may have good therapeutic potential as an EGFR kinase specific inhibitor to treat EGFR-related diseases.