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公开(公告)号：KR1020000066932A
公开(公告)日：2000-11-15
申请号：KR1019990014355
申请日：1999-04-22
Applicant: 한국과학기술연구원
IPC: A61K31/34
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。
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公开(公告)号：KR1020000056561A
公开(公告)日：2000-09-15
申请号：KR1019990005977
申请日：1999-02-23
Applicant: 한국과학기술연구원
IPC: C07H15/24
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。
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公开(公告)号：KR100314906B1
公开(公告)日：2001-11-23
申请号：KR1019990006025
申请日：1999-02-24
Applicant: 한국과학기술연구원
IPC: C12Q1/68
Abstract: 본발명은 NF-κB 활성의존적리포터유전자가발현된세포주를이용하여전사인자인 NF-κB의활성을측정하고또한 TNF-α등의다양한 NF-κB 활성화인자들의활성및 양을측정하는방법에관한것으로서, 상세하게는 NF-κB가결합하는 DNA 염기서열을 9개반복적으로연결한 DNA 단편, SV40 바이러스의최소프로모터, 리포터진 및선택표지로구성되는발현벡터로형질전환된 RAW-NF-AP 또는 HeLa-NF-AP 세포주를이용하여 NF-κB 또는 TNF-α의활성을특정하는방법으로서, NF-κB 또는 TNF-α의기전연구, NF-κB 활성화조절물질의검색및 TNF-α합성을조절하는물질의검색등에매우유용하게사용될수 있다.
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Patent Agency Ranking
公开(公告)号：KR1019990074024A
公开(公告)日：1999-10-05
申请号：KR1019980007348
申请日：1998-03-05
Applicant: 한국과학기술연구원
IPC: C07C69/738 , C07C69/013
Abstract: 본 발명은 사상자로부터 분리, 동정된 토릴린이 내성세포주 막에서 p-gp ATPase의 활성을 증가시켜 항암제의 유출을 억제하므로써 항암제를 세포내에 축척시킨 결과, 세포독성을 증가시켜 항암제의 활성을 증강시키는 방법과 항암제로서의용도에 관한 것이다. 본 발명의 토릴린 화합물은 혈관신생에 관여하는 내피세포의 증식을 억제하고 계배를 이용한 CAM assay에서 혈관신생을 억제할 뿐만아니라 암세포가 분비하는 막분해 효소인 matrix metalloprotease의 활성과 그 유전자 발현을 억제하여 암세포의 침윤을 저해하는 뛰어난 효과가 있어 다기능 항암제로 이용가치가 높다.
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公开(公告)号：KR100293258B1
公开(公告)日：2001-06-15
申请号：KR1019990005977
申请日：1999-02-23
Applicant: 한국과학기술연구원
IPC: C07H15/24
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.
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公开(公告)号：KR100273657B1
公开(公告)日：2000-12-15
申请号：KR1019980007348
申请日：1998-03-05
Applicant: 한국과학기술연구원
IPC: C07C69/738 , C07C69/013
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。
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公开(公告)号：KR1020000056573A
公开(公告)日：2000-09-15
申请号：KR1019990006025
申请日：1999-02-24
Applicant: 한국과학기술연구원
IPC: C12Q1/68
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。
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公开(公告)号：KR100321312B1
公开(公告)日：2002-03-18
申请号：KR1019990014355
申请日：1999-04-22
Applicant: 한국과학기술연구원
IPC: A61K31/34
Abstract: 본발명은태산목 (L.)의잎에서추출한세스퀴테르펜락톤 (sesquiterpene lactone) 화합물로서염증질환및 면역질환치료제로이용될수 있는, 화학식 1의구조를갖는코스투놀라이드 (costunolide)에관한것으로, 상기화합물들은인체의면역체계를조절하는중요한인자인산화질소 (nitric oxide, NO)나종양괴사인자-알파 (TNF-α)의생성을억제하고, 염증매개인자의발현에중요한전사인자인 NF-κB의활성화를억제함으로써, 산화질소나종양괴사인자-알파의과잉생성또는 NF-κB의활성화에의해야기되는염증관련질환및 면역질환의효과적인치료제로이용될수 있다. 코스투놀라이드
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