Abstract:
PURPOSE: Novel aklavinone derivatives prepared by transforming biosynthetic variants with a vector containing aklavinone C-11 hydroxylase gene separated from Streptomyces sp and fermenting transformer thereof and process for producing the same are provided which can be effectively used for an antibiotic. CONSTITUTION: 2,11-Dihydroxyaklavinone of formula 1 is used in the manufacture of various new anthracycline antibiotics through bioconversion. Thus, 2,11-dihydroxyaklavinonecycline as anthracycline antibiotics is prepared by using the compound as a precursor, has low toxicity against a cell and is safer than conventional antibiotics.
Abstract:
PURPOSE: A sesquiterpene lactone compound, costunolide is provided, which inhibits production of nitric oxide(NO) or tumor necrosis factor-alpha(TNF-alpha)(they are important factor for controling of human immune system); and inhibits activity of NF-kappaB, the important transcription factor in representation of inflammation-mediate-factor; so which can be used as a medicine for inflammation-related disease and immune-disease. CONSTITUTION: The costunolide is gained from Magnolia grandiflora L. by methanol-extracting, which can be administrated by oral or parenteral, and can be used as a form of common pharmaceutical preparation, e.g., tablets, pills, granules, powders, capsules, suspension, liquid preparation for oral, emulsion, syrup, sterilized solution for injection, suppositories. An effective dosage of sesquiterpene lactone compound, the costunolide is 5-50mg/kg, desirably 5-20mg/kg, which can be administrated 1-3times per day.
Abstract:
PURPOSE: Pregnane glycoside of formula (1) and/or formula (2) which is isolated from Cynanchum wilfordii and its use as an anticancer agent are provided. CONSTITUTION: A pregnane glycoside represented by formula (1), isolated from Cynanchum wilfordii, is prepared by carrying out the following steps of: extracting the roots of Cynanchum wilfordii ground and drying in a shade with methanol and concentrating the extract under vacuum to obtain the methanol extract; fractionating to dichloromethane and water; performing a silica gel column chromatography and then obtaining an active fraction using n-hexane ethylacetate step gradient system; performing chromatography on a RPMPLC column to the active fraction; and recrystallizing with methanol. The compound increases the activities of the anticancer agent by preventing the anticancer agent from being released from a cell line having a multi-drug resistance, inhibits the replication of an endothelial cell necessary to the angiogenesis and inhibits cancer cellular infiltration by decreasing the activities of matrix metalloprotease and the expression of the gene encoding the enzyme.
Abstract:
PURPOSE: A natural torilin compound useful as an anticancer drug is provided for enhancing the efficiency of the anticancer drug, inhibiting increase of endothelial or blood vessel neoplasm, preventing activity of the matrix metallo-protease and reducing the gene expression thereof. CONSTITUTION: The natural torilin compound useful as the anticancer drug having excellent anti-tumor activity and abilities for inhibiting the increase of endothelial and blood vessel neoplasm and the reaction of matrix metallo-protease and form reducing the expression of the gene thereof is defined by the formula I and is separated and purified from Torilidis Fluctus as a medical plant. The anti-tumor composition, that is, the anticancer drug comprising pharmaceutically effective amount of the natural torilin compound is particularly used to inhibit blood vessel neoplasm and infiltration of tumor cells.
Abstract:
PURPOSE: A measuring process for an activity of genes transcription factor NF-kappaB, and activity and quantity of TNF-alpha is provided, which can be used in an investigation for process of NF-kappaB or TNF-alpha; in an inspection of NF-kappaB activation controlling material; and in an inspection of TNF-alpha synthesis controlling material. CONSTITUTION: A process for the measurement of activity of NF-kappaB and TNF-alpha comprises of: preparing the plasmid(pNF-SEAP) comprising NF-kappaB binding DNA fraction; culturing HeLa cells and RAW264.7 cells; precipitating the pNF-SEAP DNA with calcium phosphate, and sprinkling the solution on two cells; culturing the cells in DEME plate, and moving to antibiotics-contained plate; selecting the cells still alive to get RAW-NF-AP cells and HeLa-NP-AP cells; measuring NF-kappaB activity induced by LPS in RAW-NF-AP cells; examining inhibition effect of dexamethasone on NF-kappaB activity; measuring the NF-kappaB activity induced by TNF-alpha in the HeLa-NP-AP cells; and measuring quantity of TNF-alpha using the HeLa-NP-AP cells.
Abstract:
본 발명은 하기 화학식 1의 아클라시노마이신 X, 하기 화학식 2의 11-히드록시 아클라시노마이신 X 및 스트렙토마이세스 갈릴레우스( Streptomyces galilaeus ) ATCC 31133을 배양하여 균사체를 분리한 후 상기 균사체로부터 아클라시노마이신 X를 추출함을 포함하는, 아클라시노마이신 X의 제조방법에 관한 것이다. 화학식 1
Abstract:
본 발명은 아클라비논 11-히드록실라제를 암호화하는 유전자, 이를 포함하는 발현벡터 및 이러한 발현벡터에 의해 형질전환된 숙주세포를 제공하며, 또한 상기 유전자를 세포내에서 발현시켜 하이브리드 안트라사이클린계 항생제를 제조하는 방법을 제공한다. 또한 야생형 균주가 생산하는 새로운 항생제 아클라시노마이신 X(2"-amino aclacinomycin Y) 및 이의 제조방법을 제공한다.
Abstract:
본 발명은 안트라사이클린계 항생제를 생산하는 변이 균주 및 이를 혼합 배양하여 독소루비신 (doxorubicin)을 대량 생산하는 방법에 관한 것이다. 구체적으로, 본 발명은 독소루비신의 생합성 과정 중에 돌연변이가 유발되어 독소루비신은 생산하지 못하지만 생합성 중간체인 ε-로도마이시논 (ε-rhodomycinone) 이후의 중간체들의 생합성에 필요한 효소들의 활성은 보유한 스트렙토마이세스 푸세티우스 변이 균주, 바우마이신 (baumycin)의 생합성 과정에 돌연변이가 유발되어 중간체인 ε-로도마이시논을 고수율로 생산하는 스트렙토마이세스 속 변이 균주, 상기 균주들 및 이들의 형질전환체를 혼합 배양하여 독소루비신을 생산하는 발효 방법에 관한 것으로서, 상기 방법을 이용하면 항암 효과가 우수한 독소루비신을 대량 생산하여 용이하게 정제할 수 있다.
Abstract:
본 발명은 노박덩굴 추출물 및 이로부터 얻은 하기의 구조식(I),(II),(III)의 새로운 세스퀴테르펜 에스테르 화합물에 관한 것이다.
본 발명은 구조식(I),(II),(III)의 새로운 세스퀴테르펜 에스테르 화합물을 노박덩굴(Celastrus orbiculatus)의 뿌리로부터 분리·정제하는 방법에 관한 것이다. 또한 본 발명은 세스퀴테르펜 에스테르 화합물 및 이의 유도체를 유효 성분으로 하는 약학적 조성물을 다제내성(multi-drug resistance) 조절제로서 사용하는 용도에 관한 것이다.