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송규용,배기환,명창선,김문일,박용진,윤미영,김동희,Song Gyu Yong,Bae Ki Whan,Myung Chang-Seon,Jin Wen Yi,Park Yong Jin,Yun Mi Young,Kim Dong Hee 대한동의생리학회 2005 동의생리병리학회지 Vol.19 No.3
Antitumor and anti-metastatic effects of mineral powder(MP) were studied. In the present study, MP did not exhibit the any cytotoxic activity against leukemic cells such as L1210 and U937 tumor cell lines in vitro. Also, MP did not exhibit the any cytotoxic activity against solid cells such as A549 and B16-BL6 tumor cell lines in vitro. However, in vivo, MP exhibit a significant antitumor activity in BDF1 mice bearing Lewis lung carcinoma cells(LLC) with inhibition rates of 46 and $23\%$ at 200 and 100 mg/kg/day, respectively. Furthermore, in pulmonary colonization assay, MP exhibit the inhibitory effect of tumor metastasis. From these results, it was concluded that MP had antitumor and anti-metastatic activity suggesting its application for the prevention and treatment of cancer.
2-Propylthio-5,8-dimethoxy-1,4-naphthoquinone의 항암활성에 관한 연구
송규용 충남대학교 약학대학 의약품개발연구소 2004 藥學論文集 Vol.19 No.-
In a continuation of the search for novel antitumor agent, 5,8-dimethoxy-1,4-naphthoquinone was selected as a lead compound and 2-alkylthio-5,8-dimethoxy-1,4-naphthoquinone derivatives were synthesized from 1,5-dihydroxynaphthalene in 5 steps. Among them, 2-propylthio-5,8-dimethoxy-1,4-naphthoquinone (2-PropylthioDMNQ) exhibited the strongest cytotoxicity (ED_(50), 2.02±0.89 and 9.44±199 μM) against L1210 and A549 cells, respectively. Also, 2-propylthioDMNQ (6C) strongly inhibited adhesion of B16-BL6 cells to gelatin and matrigel coated matrices and exhibited anti-invasive effect of B16-BL6 cells. The T/C value of 2-propylthioDMNQ (6c) treated group was 123±2.65 % in S-180 bearing ICR mice.
Flavone의 합성 중간체인 2-Aroyloxyacetophenone류의 새로운 합성법
송규용,안병준 충남대학교 약학대학 의약품개발연구소 1994 藥學論文集 Vol.10 No.-
We have synthesized some 2-(2-benzyloxybenzoyloxy)-and 2-(2,6-dibenzyloxybenzoyloxy)-acetophenones as intermediates for flavone synthesis. The reaction of polyoxygenated 2-hydroxyacetophenones with 2-benzyloxybenzoic acid or 2,6-dibenzyloxybenzoic acid in the presence of dicyclohexylcarbodiimide and p-dimethylaminopyridine resulted in a good yield(70~89%) of 2-(2-benzyloxybenzoyloxy)-acetophenones or 2-(2,6-dibenzyloxybenzoyloxy)-acetophenones under milder conditions and in shorter time than the previous methods. This new methods using benzoic acids instead of benzoyl chlorides saves one reaction step of acid chlorination in comparision of the previous methods.
Flavone의 합성 중간체인 2-Aroxyloxyacetophenone류의 새로운 합성법
송규용(Gyu Yong Song),안병준(Byung Zun Ahn) 대한약학회 1994 약학회지 Vol.38 No.1
We have synthesized some 2-(2-benzyloxybenzoyloxy)-and 2-(2,6-dibenzyloxybenzoyloxy)-acetophenones as intermediates for flavone synthesis. The reaction of polyoxygenated 2-hydroxyacetophenones with 2-benzyloxybenzoic acid or 2,6-dibenzyloxybenzoic acid in the presence of dicyclohexylcarbodiimide and p-dimethylaminopyridine resulted in a good yield(70-89%) of 2-(2-benzvloxybenzovloxy)-acetophenones or 2-(2,6-dibenzyloxybenzoyloxy)-acetophenones under milder conditions and in shorter time than the previous methods. This new methods using benzoic acids instead of benzoyl chlorides saves one reaction step of acid chlorination in comparision of the previous methods.
白花蛇舌草 헥산分劃과 多糖體가 抗癌 및 抗轉移 活性에 미치는 影響 : Ursolic acid와 Asperuloside 병용투여시 항암 및 항전이 효과에 관한 연구
宋圭鏞,柳時容,金聖勳 대한동의병리학회 1999 동의생리병리학회지 Vol.13 No.1
산업기술의 발달로 인한 삶의 질의 향상과 더불어 현대의학의 발달에도 불구하고 아직도 불치의 병으로 여겨지고 있는 암에 의한 사망률은 계속 증가되고 있는 추세로 암을 치유하기 위한 연구가 활발히 전개되고 있다. 백화사설초는 항암 본초로 분류되어 암치료를 위해 한방처방에 가미되어 응용되고 있다. 그러나 백화사설초의 성분에 대한 연구는 미흡한 실정이다. 이런 점을 감안하여 본 연구실에서는 백화사설초의 용매 분획 중 헥산 분획이 수종의 암세포에 대해서 세포독성이 있음을 발견하고 물질분리를 실시하여 물질을 단리한 후 물리·화학적인 방법을 통하여 구조를 확인 한 결과 ursolic acid(UA)가 효과를 나타내는 물질이라는 것을 밝혔다. 따라서 UA의 구체적인 항암 및 항전이 효과를 검증하기 위하여 수종의 암세포에 대한 세포독성, 부착저지효과, 폐암전이 억제효과, 혈관형성 억제효과, 암전이에 관련된 유전자인 MMP-2의 발현 정도를 살펴보았고 면역세포에 미치는 영향은 물론 배당체인 asperuloside(AS)를 분리하여 UA와 병용투여하므로써 항암 및 항전이 활성의 변화를 관찰하여 항암제로서의 가능성을 타진하고자 하였다. 실험결과 UA는 수종의 암세포에 농도의존적으로 암의 성장을 억제하였으며, AS의 병용투여시 상승적인 세포독성 효과를 발휘하지 않았다. 그러나 세포부착 저지효과, 혈관형성 억제효과 및 폐암전이 효과와 같은 암전이에 관련된 실험에서 AS는 UA의 효과를 상승적으로 증가시켰을 뿐만아니라 면역세포에 대해서도 증가효과를 나타냈다. 이상의 결과로부터 UA는 항암 및 항전이 효과가 있음을 발견하였으며, AS와 같은 배당체의 병용투여는 이러한 항암 및 항전이 효과를 증가시키는 것으로 보아 암에 유효하게 사용될 수 있으리라 사료된다. Ursolic acid(UA), isolated from the Oldenlandia diffusa(Rubiaceae), is a triterpenoid compound that exist widely in food, medicinal herbs, and other plants and has been recognized to have a wide spectrum of pharmacological activity such as antiinflammatory effect, anti-HIV activity, antihyperlipidemic activity, and antitumor activity. Ursolic acid was treated either alone or in combination with asperuloside(AS), irridoidal glycoside, for the evaluation of antitumor and antimetastatic effects by several experimental parameters, for example, cytotoxicity against various cancer cell line, clonogenic assay, antiadhesion assay, CAM assay, pulmonary colonization assay, MMP-2 expression, and immunological analysis by FACS. The results were obtained as follows; Ursolic acid showed a potent cytotoxic activity in a dose dependent manner against SF295, SK-OV-3, HCT15, and UN-2 cancer cell lines, while combined treatmenmt of UA & AS didn't. However, UA & AS were more effectiv than UA only in inhibitory effect on cell adhesion of A549 cells to complex extracellular matrix in vitro and pulomonary colonization assay by B16BL/6 in vivo. In the clonogenic assay UA & AS more effectively inhibited colony formation by A549 synergistically to 97% than UA to 78%. By analysis by FACS UA & AS activated CD4(T helper cell) and CDB(cytotoxic T cell) as well as macrophage while UA activated macrophage only. UA and AS suppressed MMP-2 gene expression more effectively than UA only in a dose dependent manner. These results suggest that combined therapy of ursolic acid and asperuloside showed antitumor and antimetastatic effects than ursolic aicd only so that Oldenlandiae diffusae Herba can be effectively applied for the prevention and treatment of cancer. It also is very necessary that biological activities and their mechanism should be kept studying between different constituents isolated from same plant.
정상 식이 수컷 흰쥐에서 흑삼이 체중 및 지질에 미치는 영향
송규용(Gyu Yong Song),오한진(HAn Jin Oh),노성수(Seong Soo Roh),서영배(Young Bae Seo),박용진(Yong Jin Park),명창선(Chang-Seon Myung) 대한약학회 2006 약학회지 Vol.50 No.6
Previously, we have reported that black ginseng was produced by nine-time repeated steaming 5-year fresh ginsengs at 95℃ for 3 hr in pottery apparatus and drying at 60℃ for 12~36 hr and had an outstanding anticancer activity. This study was designed to examine the ability of black ginseng to suppress body weight gain and appetite, and to investigate the effect of black ginseng on lipid profile in male rats fed normal diets. The extract of black ginseng was administered daily for 3 weeks, and the changes of body weight and food intake were measured. After administering the extracts for 3 weeks, the fat weight and serum lipid levels were also measured. Black ginseng persistently suppressed weigh gain and food intake was also reduced, but not significantly. The weight of both epididymal and abdominal fats was decreased in black ginseng-treated rats. Serum triglyceride level in rats administered with black ginseng was also significantly lowered. Therefore, these results reveal that the repeated administration of black ginseng causes a suppression body weigh gain by decreasing triglyceride level in blood and body fat deposit.