Molecular cloning of a gene coding for cephalexin semisynthesizing enzyme

학위논문(석사) - 한국과학기술원 : 생물공학과, 1988.2, [ vi, 54 p. ]한국과학기술원 : 생물공학과

방선균이 생산하는 신규 항종양 항생물질 및 하이브리드 안스라사이크린의 특성과 화학구조

학위논문(박사) - 한국과학기술원 : 생물과학과, 1996.8, [ x, 211 p. ]The Streptomyces sp. MCH79 was selected from the cytotoxicity assay against tumor cells to search for novel antitumor compound from microbial metabolites. This strain was identified as Streptomyces ostreogriseus on the basis of its cultural, morphological and physiological properties. The active compounds, MCH-14 (40.1 mg), MCH-15 (26.9 mg), MCH-16 (20.1 mg), MCH-17 (91.7 mg), MCH-18 (21.6 mg), MCH-22 (135.2 mg), MCH-31 (52.2 mg), MCH-23 (25.4 mg), MCH-32 (19.6 mg), MCH-Vi (9600 mg) and MCH-Vj (143.4 mg), were recovered from the mycelium of fermentation broth (120ℓ)with acetone extraction followed by purification on a silica gel column chromatography and reverse-phase HPLC chromatography. The structure of MCH compounds were determined by spectroscopic methods of UV, FT-IR, $^1H$-NMR, $^{13}C$-NMR, DEPT, $^1H-^1H$ COSY, $^{13}C-^1H$ COSY, HMBC and FAB-MS as well as physicochemical data such as melting point and optical rotation. Structural studies revealed that there were seven novel oligomycin analogues, 41-demethyl-29 -hydroxy-homooligomycin A, 41-demethyl-oligomycin E, 41-demethyl-44-hydroxy-homooligomycin A, 41-demethyl-homooligomycin E, 41-demethyl-homooligomycin B, homooligomycin E, 41-demethyl-homooligomycin A and four known oligomycins, 44-homooligomycin B, 44-homooligomycin A, oligomycin A, 44-homooligomycin C. The MCH compounds showed selective growth inhibition against cell lines such as RHEK-1 (human epidermal keratinocyte cell line), RHEK-1/pSV2 ras (cell line transformed with $pSV_2$ras), NIH-3T3 (NIH Swiss mouse embryo fibrolast), F25 (oncogene ras transformed NIH-3T3) and human tumor cell lines, SNU-1 (human stomach cancer) and SNU-354 (human liver cancer), with the $IC_{50}$ values range of 0.073-19.0, 0.025-6.50, 1.17-159.75, 0.22-0.75, 0.17-0.63, 0.19-1.05㎍/ml, respectively. The MCH compounds showed stronger cytotoxic effect on RHEK-1/pSVras and F25 than on their parent cells, RHEK-1 and NIH-3T3, indicating that the compounds conferred differe...한국과학기술원 : 생물과학과

Natural substance of torilin and the use thereof as an inhibitor of tumor growth

본 발명은 사상자로부터 분리한 토릴린 화합물의 항암제로서의 용도에 관한 것이다. 본 발명의 토릴린 화합물은 혈관신생에 관여하는 내피세포의 증식을 억제하고 혈관신생을 억제할 뿐만아니라, 암세포가 분비하는 막분해 효소인 매트릭스 메탈로프로테아제의 활성과 그 유전자 발현을 억제하여 암세포의 침윤을 저해하는 뛰어난 효과가 있어 다기능 항암제로서의 이용가치가 높다