신규 아클라비논 유도체 및 그의 제조방법
    1.
    发明公开
    신규 아클라비논 유도체 및 그의 제조방법 失效
    新型AKLAVINONE衍生物及其生产方法

    公开(公告)号:KR1020000067074A

    公开(公告)日:2000-11-15

    申请号:KR1019990014564

    申请日:1999-04-23

    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 translation: 目的:提供通过用链霉菌sp和发酵变压器分离的含有aklavinone C-11羟化酶基因的载体转化生物合成变体制备的新型aklavinone衍生物及其生产方法,其可有效用于抗生素。 构成:式1的2,11-二羟基喹喔啉通过生物转化用于制备各种新的蒽环类抗生素。 因此,通过使用该化合物作为前体制备作为蒽环类抗生素的2,11-二羟基喹诺酮类,对细胞毒性低,比常规抗生素更安全。

    세스퀴테르펜 락톤 화합물 코스투놀라이드의 염증질환 치료제로서의 용도
    2.
    发明公开
    세스퀴테르펜 락톤 화합물 코스투놀라이드의 염증질환 치료제로서의 용도 失效
    使用化学复合物COSTUNOLIDE作为抗炎药物

    公开(公告)号:KR1020000066932A

    公开(公告)日:2000-11-15

    申请号:KR1019990014355

    申请日:1999-04-22

    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 translation: 目的:提供倍半萜内酯化合物,其可以抑制一氧化氮(NO)或肿瘤坏死因子-α(TNF-α)的产生(它们是控制人体免疫系统的重要因素); 并抑制NF-κB的活性,NF-κB是代表炎症介导因子的重要转录因子; 因此可用作炎症相关疾病和免疫疾病的药物。 成分法:通过甲醇提取法,从大兰木兰获得木贼多糖,其可以通过口服或肠胃外给药,并且可以用作常见药物制剂的形式,例如片剂,丸剂,颗粒剂,粉剂,胶囊剂,悬浮液 口服液剂,乳剂,糖浆,注射用灭菌溶液,栓剂。 有效剂量的倍半萜内酯化合物,肋骨瓜内酯为5-50mg / kg,理想的为5-20mg / kg,可以每天施用1-3次。

    프레그난 배당체 화합물 및 그들의 항암제로서의 용도
    3.
    发明公开
    프레그난 배당체 화합물 및 그들의 항암제로서의 용도 失效
    PREGNANE GLYCOSIDE及其作为防治剂的用途

    公开(公告)号:KR1020000056561A

    公开(公告)日:2000-09-15

    申请号:KR1019990005977

    申请日:1999-02-23

    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 translation: 目的:提供从仙妮兰(Cynanchum wilfordii)中分离得到的式(1)和/或式(2)的芸香苷及其作为抗癌剂的用途。 构成:通过以下步骤制备由茜草(Cynanchum wilfordii)分离的由式(1)表示的孕烷苷,其中提取枸杞子的根,用甲醇在阴凉处干燥,并将提取物真空浓缩,得到 甲醇提取物; 分馏成二氯甲烷和水; 进行硅胶柱色谱,然后使用正己烷乙酸乙酯梯度系统获得活性级分; 在RPMPLC柱上进行色谱至活性级分; 并用甲醇重结晶。 该化合物通过防止抗癌剂从具有多重耐药性的细胞系中释放而增加抗癌剂的活性,抑制血管生成所必需的内皮细胞的复制,并通过降低基质的活性来抑制癌细胞浸润 金属蛋白酶和编码该酶的基因的表达。

    프레그난 배당체 화합물 및 그들의 항암제로서의 용도
    4.
    发明授权
    프레그난 배당체 화합물 및 그들의 항암제로서의 용도 失效
    前脑糖苷的制备及其作为抗癌剂的用途

    公开(公告)号:KR100293258B1

    公开(公告)日:2001-06-15

    申请号:KR1019990005977

    申请日:1999-02-23

    Abstract: 본발명은백하수오로부터분리한화학식 1 (별명 CW-1)의프레그난배당체(gagaminin 3-&0&-β-D-cymaropyranosyl-(1→4)-β-D-oleandropyranosyl- (1→4)-β-D-cymaropyranosyl-(1→4)-β-D-cymaropyranoside) 및그의용도에관한것으로서, 상기화합물은항암제내성세포주에서항암제의세포내축적을증가시키고유출을억제함으로써항암제의활성을증강시키는다중약제내성억제제, 혈관신생에관여하는내피세포의증식을억제하고내피세포의튜브로의분화를억제하는혈관신생억제제, 암세포가분비하는세포외기질 (extra-cellular matrix) 분해효소인매트릭스메탈로프로테아제 (matrix metalloprotease)의활성과그 유전자발현을억제하는활성에의한암세포의침윤억제제로서의용도를가지며, 또한본 발명은백하수오로부터분리한화학식 2의프레그난배당체화합물의혈관신생억제제, 암세포침윤억제제로서의용도에관한것이다. 상기한화학식 1 및화학식 2의프레그난배당체화합물은다기능항암제로서이용가치가높다.

    천연물질토릴린화합물및그의항암제로서의용도
    5.
    发明授权

    公开(公告)号:KR100273657B1

    公开(公告)日:2000-12-15

    申请号:KR1019980007348

    申请日:1998-03-05

    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 translation: 目的:提供用作抗癌药物的天然罗替林化合物,用于提高抗癌药物的效率,抑制内皮或血管肿瘤的增加,防止基质金属蛋白酶的活性和降低其基因表达。 构成:可用作具有优异的抗肿瘤活性和抑制内皮和血管肿瘤增加的能力的抗癌药物和基质金属蛋白酶的反应以及减少其基因表达的形式的天然罗替林化合物由 并将其作为医用植物从Torilidis Fluctus中分离和纯化。 抗肿瘤组合物,即包含药学有效量的天然罗替林化合物的抗癌药物特别用于抑制血管肿瘤和肿瘤细胞浸润。

    유전자 전사인자 NF-κB의 활성 및 TNF-α의 활성 및 양을측정하는 방법
    6.
    发明公开
    유전자 전사인자 NF-κB의 활성 및 TNF-α의 활성 및 양을측정하는 방법 失效
    基因转录因子NF-KAPPAB的活性测定及TNF-α的活性和数量

    公开(公告)号:KR1020000056573A

    公开(公告)日:2000-09-15

    申请号:KR1019990006025

    申请日:1999-02-24

    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 translation: 目的:提供基因转录因子NF-κB活性的测定方法,以及TNF-α的活性和数量,可用于NF-κB或TNF-α过程的研究。 检查NF-kappaB激活控制材料; 并检测TNF-α合成控制材料。 构成:测量NF-κB和TNF-α活性的方法包括:制备包含NF-κB结合DNA级分的质粒(pNF-SEAP); 培养HeLa细胞和RAW264.7细胞; 用磷酸钙沉淀pNF-SEAP DNA,并将溶液洒在两个细胞上; 培养DEME板中的细胞,移至含抗生素的板上; 选择细胞仍然存活以获得RAW-NF-AP细胞和HeLa-NP-AP细胞; 测量RAW-NF-AP细胞中LPS诱导的NF-κB活性; 检测地塞米松对NF-κB活性的抑制作用; 测量HeLa-NP-AP细胞中TNF-α诱导的NF-κB活性; 并使用HeLa-NP-AP细胞测量TNF-α的量。

    안트라사이클린계 항생제를 생산하는 변이균주 및 이를 혼합배양하여 독소루비신을 생산하는 방법
    9.
    发明授权
    안트라사이클린계 항생제를 생산하는 변이균주 및 이를 혼합배양하여 독소루비신을 생산하는 방법 失效
    产生蒽环类抗生素的突变株和通过混合培养生产阿霉素的方法

    公开(公告)号:KR100266435B1

    公开(公告)日:2006-01-27

    申请号:KR1019970069309

    申请日:1997-12-16

    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.

    새로운 세스퀴테르펜 에스테르 화합물
    10.
    发明授权
    새로운 세스퀴테르펜 에스테르 화합물 失效
    新型SESQUITERPENE ESTER化合物

    公开(公告)号:KR100191901B1

    公开(公告)日:1999-06-15

    申请号:KR1019960009782

    申请日:1996-04-01

    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.

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