• 한국응용약물학회:학술대회논문집
• /
• 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
• /
• pp.174-174
• /
• 1994

항종양 물질의 탐색 및 연구 작업이 미생물을 대상으로 행해져 온것은 이미 오래전부터 이며, 기존의 연구 발표된 것들을 볼때 미생물 스크리닝의 증요성은 점차 증대되어가고 있다. 이에 본 연구에서는 국내 토양에서 방선균 약 1000여주를 분리하여 항종양 물질을 생산하는 방선군의 분리, 동전하고, 그 생산물질의 특성을 밝히고자 하였다. 방선균의 분리는 전국 각지에선 채집한 토양시료 각 1 g 씩을 80 $^{\circ}C$에서 90분간 건조처리한후 멸균된 증류수를 이용하여 각 단계별로 희석하여 Starch nitrate casein agar와 Glycerol asparagine agar를 사용하여 방선균을 분리하였다. 분리된 방선균을 Yeast extract-malt extract 액체 배지에서 7일간(160 rpm/28 $^{\circ}C$) 배양하였다. 여기에서 얻어진 배양액을 이용하여 항종양능을 확인한기 위해서 암세포주인 L1210주와 P388 D$_1$주, 정상 세포주로는 Vero 세포주를 이용한 MTT colorimetric assay를 이용하였다. 이들 실현에 대한 결과로써 S-104, 117, 409의 세 균주의 항종양물질 생산 균주를 분리하였다. 이들 균주가 생산하는 물질들은 기존의 시판 항암제인 Adriamycin에 비해 높게 나타났으며, 이들 균주의 동정은 ISP의 기준에 의하여 행하였다.

• Journal of Microbiology and Biotechnology
• /
• 제14권3호
• /
• pp.628-630
• /
• 2004

Antitumor activities of a peptide fraction isolated from traditional Korean soy sauce (SSP) were investigated in vitro and in vivo using cancer cell lines and F9 teratocarcinoma-bearing BALB/c mice. SSP exerted a dose-dependent antiproliferative effect on P388D1 mouse lymphoma, F9 mouse teratocarcinoma, and DLD-l human colon cancer cells with $IC_{50}$ values of 11, 50, and $50\mug/ml$, respectively. Tumor growth in F9 teratocarcinoma-bearing BALB/c mice, orally administered with 80 and 200 mg/kg/day of SSPs, was inhibited 10.3% and 52.4%, respectively, and survival days increased by 11.9% and 22.1%, respectively, compared to the control group. The results of antitumor activities exerted by SSP in vitro and in vivo suggest the feasibility of using SSP as an antitumor agent.

• Integrative Medicine Research
• /
• 제6권4호
• /
• pp.388-394
• /
• 2017

Background: The present study optimized ultrasound-assisted extraction conditions to maximize extraction yields of glycyrrhizic acid from licorice. Methods: The optimal extraction temperature ($X_1$), extraction time ($X_2$), and methanol concentration ($X_3$) were identified using response surface methodology (RSM). A central composite design (CCD) was used for experimental design and analysis of the results to obtain the optimal processing parameters. Results: Statistical analyses revealed that three variables and the quadratic of $X_1$, $X_2$, and $X_3$ had significant effects on the yields and were followed by significant interaction effects between the variables of $X_2$ and $X_3$ (p<0.01). A 3D response surface plot and contour plots derived from the mathematical models were applied to determine the optimal conditions. The optimum ultrasound-assisted extraction conditions were as follows: extraction temperature, $69^{\circ}C$; extraction time, 34?min; and methanol concentration, 57%. Under these conditions, the experimental yield of glycyrrhizic acid was 3.414%, which agreed closely with the predicted value (3.406%). Conclusion: The experimental values agreed with those predicted by RSM models, thus indicating the suitability of the model employed and the success of RSM in optimizing the extraction conditions.

• 약학회지
• /
• 제35권6호
• /
• pp.497-503
• /
• 1991

Six novel 5-substituted-1-[2-(3-methoxy-2-hydroxyphenyl)-1-methoxyethyl]uracils 2a-f were prepared by condensation of 2,4-bis(trimethylsilyloxy)-5-substituted uracils with 2,7-dimethoxy-2,3-dihydrobenzofuran (9) in the presence of Lewis acid. The 2,3-dihydrobenzofuran derivative 9 was obtained by intramolecular acetalization of 2-acetoxy-3-methoxyphenyl acetaldehyde (8) which was synthesized by oxidative cleavage of 1-allyl-2-acetoxy-3-methoxybenzene (7) using osmium tetroxide followed by $NaIO_4$. Compounds 2a-f were evaluated for in vitro antiviral activity against HSV-1, HSV-2 and HRV. None of these compounds showed activity with $ID_{50}$ values up to $100\;{\mu}g/ml$ except for 5-chlorouracil derivative 2d which exhibited antiviral activity against HSV-1 with $ED_{50}$ $30\;{\mu}g/ml$. In the antitumor activity against L1210 and P388 leukemia cell lines, 2d showed activity with $ID_{50}$ values of $14\;{\mu}g/ml$ and $11.6\;{\mu}g/ml$, and 2c with $ID_{50}$ values of $22.9\;{\mu}g/ml$ and $8.8\;{\mu}g/ml$, respectively.

• Archives of Pharmacal Research
• /
• 제18권6호
• /
• pp.449-453
• /
• 1995

The search for patinum (II)-based compounds with improved therapeutic properties was prompted to design and synthesize a new family of water-soluble, third generation cis-diamminedichlorplatinum (II) complexes linked to uracil and uridine. Six heretofore undescribed uracil and uridine-platinum (II) complexes are ; [N-(2-aminoethyl)uracil-5-carboxamide]dichloroplatinum (II)(3a), [N-2(2-aminoethyl)uracil-6-carboxmide]dichloroplatinum (II) (3b),[5-(2-aminorthyl)carbamoyl-2',3',5',-tri-O-acetyluridine] dichloroplatinum (II) (6b), [5-(2-aminoethyl)-carbamoyl]-2',3',5',-tri-O-acetyluridine] dichloroplatinum (II) (6b), [5-(2-aminoethyl)carbamoylu-ridine]dihloroplatinum (II) (7a), [6-(2-aminoethyl)carbamoyluridine]dichloroplatinum (II) (7b). These analogues were prepared from the key starting materials, 5-carboxyuracil (1a) and 6-carboxyuracil (1b) which were reacted with ethylenediamine to afford the respective N-(2-aminoethyl)uracil-5-carboxmide (2a) land N-(2-aminoethyl)uracil-6-carboxamide (2b). The cisplatin complexes 3a and 3b were obtained through the reaction of the respective 2a and 2b ficiently introduced on the .betha.-D-ribose ring via a Vorbruggen-type nucleoside coupling procedure with hexamethyldisilazane, trimethylchlorosilane and stannicchloride under anhydrous acetonitfile to yield the sterospecific .betha.-anomeric 5-carboxy-2',3',5'-tri-O-acetyluridine (4a) and 6-carboxy-2',3',5'-tri-O-acetyluridine (4b), respective 5-(2-aminoethyl)carbamoyl-2',3',5'-tri-O-acetyluridine (5a) and 6-(2-aminoethyl)carbamoyl-2',3',5'-tri-O-acetyluridine (5b). The diamino-uridines 5a and 5b were reacted with potassium tetrachloroplatinate (II) to give the novel nucleoside complexes, 6a and 6b respectively which were deacetylated into the free nucleosides, 7a and 7b by the treatment with CH/sub 3/ONa. The antitumor activities were evaluated against three cell lines (K-562, FM-3A and P-388).

• Fisheries and Aquatic Sciences
• /
• 제14권4호
• /
• pp.379-388
• /
• 2011

The mechanism by which gonadotropin-releasing hormone (GnRH) and dopamine (DA) control gonadotropin (GTH) release was studied in male and female rainbow trout using cultured pituitary cells obtained at different reproductive stages. The mechanisms of follicle-stimulating hormone (FSH) release by GnRH and DA could not be determined yet. However, basal and salmon-type GnRH (sGnRH)- or chicken-II-type GnRH (cGnRH-II)- induced luteinizing hormone (LH) release increased with gonadal maturation in both sexes. LH release activity was higher after sGnRH stimulation than cGnRH-II stimulation at maturing stages in both sexes. The GnRH antagonist ([Ac-3, 4-dehydro-$Pro^1$, D-p-F-$Phe^2$, D-$Trp^{3,6}$] GnRH) suppressed LH release by sGnRH stimulation in a dose-dependent manner, although the effect was weak in maturing fish. The role of DA as a GTH-release inhibitory factor differs during the reproductive cycle: the inhibition of sGnRH-stimulated LH release by DA was stronger in immature fish than in maturing, ovulating, or spermiated fish. DA did not completely inhibit sGnRH-stimulated LH release, and DA alone did not alter basal LH release. Relatively high doses ($10^{-6}$ or $10^{-5}M$) of domperidone (DOM, a DA D2 antagonist) increased LH release, which did not change with reproductive stage in either sex. The potency of DOM to enhance sGnRH-stimulated LH release was higher in maturing and ovulated fish than in immature fish. These data suggest that LH release from the pituitary gland is controlled by dual neuroendocrine mechanisms by GnRH and DA in rainbow trout, as has been reported in other teleosts. The mechanism of control of FSH release, however, remains unknown.

• 한국산림과학회지
• /
• 제79권4호
• /
• pp.388-397
• /
• 1990

1979년 촬영한 흑백항공사진(黑白航空寫眞)과 1988년 촬영한 흑백적외선항공사진(黑白赤外線航空寫眞)을 이용하여 금오산지역(金烏山地域)의 토지이용변화(土地利用變化)와 임분재적(林分材積)의 변화(變化)에 관하여 얻은 결과는 다음과 같다. 1. 항공사진상의 임상구분에 있어서 색조(色調)가 어두운 것은 침엽수림(針葉樹林), 색조(色調)가 밝고 수관이 매우 불규칙한 것은 활엽수림(闊葉樹休)으로 구분되었다. 2. 칩엽수림중 수관이 좁은 원추형이고 감촉(感觸)이 조(粗)하고 끝이 둥근 것은 소나무림, 감촉(感觸)이 세(細)하고 끝이 뾰족한 것은 리기다소나무림으로 구분되었고, 수관이 불규칙하고 넓은 원추형은 낙엽송림으로 구분되었다. 3. 임지(林地)의 면적변화(面積變化)를 살펴보면 혼효림에서 678ha가 소나무림으로, 130ha가 리기다소나무림으로 변화되었고 219ha가 활엽수림으로 변화되었다. 활엽수림은 279ha가 혼효림으로 변화되었다. 4. 수관직경(樹冠直徑)과 흉고직경(胸高直徑)과의 회귀식(回歸式)을 구하여 F-test한 결과, 모든 수종의 임분에서 유의성(有意性)이 있었고, 소나무림과 혼효림과 활엽수림에서는 $H=a+bD+cD^2$, 리기다소나무림과 낙엽송림에서는 logD=loga+blogCD 식이 $R^2$값이 높았다. 모든 수종의 임분에서 D=a+bCD의 식이 좋아 흉고직경계산시(胸高直徑計算時) 이 식을 이용하였다. 5. 수고(樹高)를 구하기 위하여 수고곡선식(樹高曲線式)을 유도하여 F-test를 한 결과 모두 유의성(有意性)이 있었고, 소나무림과 낙엽송림에서는 logH=loga+blogD, 리기다소나무림, 활엽수림 및 흔효림에서는 $H=a+bD+cD^2$이 좋았다. 6. ha당 재적(材積)이 가장 좋은 임분은 낙엽송림이고, 성장률(成長率)이 가장 좋은 임분은 혼효림이었다. 활엽수림은 ha당 재적과 성장율에 있어 가장 낮았다. 연간성장량(年間成長量)은 낙엽송림이 $4.005m^3/ha$로 가장 좋았고, 활엽수림이 $0.682m^3/ha$로 가장 낮았다.

• 생약학회지
• /
• 제32권1호통권124호
• /
• pp.55-60
• /
• 2001

The comparison of $IC_{50}$ values of Salvia plebeia R. Br. extracts on L1210, $P388D_1$ cancer and Vero normal cell lines showed that the n-hexane soluble extract of S. plebeia R. Br. retains the most growth-inhibitory activity against tumor cell lines. The minimum inhibitory concentration (MIC) of the extract against microorganisms were also examined. Antimicrobial activity of amocla and ketoconazole as references was compared to those of other solvent extracts such as $H_2O$, n-hexane, chloroform, ethyl acetate and methanol. The antimicrobial activity of extract had growth inhibition activity against gramnegative bacteria, gram-positive bacteria and fungi $(MIC\;>\;200\;{\mu}g/ml)$ except for n-hexane extract. Seven bacterial strains were tested for in vitro susceptibility to the extract of S. plebeia R. Br. However the n-hexane extract of S. plebeia R. Br. inhibited the growth of several bacterial strains (MIC values between 100 and $200\;{\mu}g/ml$ for gram positive bacteria, $25\;{\mu}g/ml$ for P. putida).

• Archives of Pharmacal Research
• /
• 제21권4호
• /
• pp.458-464
• /
• 1998

Search for a new $\alpha$-methylene-$\gamma$-butyrolactone-bearing 6-substituted purine as a potental antitumor agent has led to synthesize seven, hitherto unreported, $5^1$-Methyl-$5^1$-[(6-substituted-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$- methylenetetrahydrofurans (H, Cl, l, $CH_3$, $NH_2$, SH, >C=O) (6a-g). These include $5^1$-Methyl-$5^1$-[(9H-purin-9-yl)methyll-$2^1$-oxo-$3^1$ -methylenetetrahydrofurans (6a), $5^1$-Methyl-$5^1$-[(6-chloro-9H-purin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydr ofurans (6b), $5^1$-Methyl-$5^1$-[(6-chloro-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6c), $5^1$-Methyl-$5^1$-[(6-methyl-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6d), $5^1$-Methyl-$5^1$-[(9H-adenin-9-yl)methyll-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6e), $5^1$-Methyl-$5^1$-[(6-mercapto-9H-purin-9-yl) methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofurans (6f) and $5^1$-Methyl-$5^1$-[(9H-hypoxanthin-9-yl)methyll-$2^1$-oxo-$3^1$-methylenetetrahydrof urans (6g) which were made by the Reformatsky-type reaction of ethyl $\alpha$-(bromomethyl) acrylate with the corresponding (6-substituted-9H-purin-9-yl)-2-propanone intermediates (5a-g). These ketone intermediates 5a-g, 1-(9H-purin-9-yl)-2-propanone (5a), 1-(6-chloro-9H-purin-9-yl)-2-propanone (5b), 1-(6-iodo-9H-purin-9-yi)-2-propanone (5c), 1-(6-methyl-9H-purin-9-yl)-2-propanone (5d), 1-(9H-adenin-9-yl)-2-propanone (Se), 1-(6-mercapto-9H-purin-9-yl)-2-propanone (5f), and 1-(9H-hypoxanthin-9-yl)-2-propanone (5g) were directly obtained by the alkylation of the 6-substituted purine bases with the chloroacetone in the presence of $K_2$$CO_3$ (or NaH) under DMF (or DMSO). The preliminary in vitro cytotoxcity assay for the synthetic .alpha.-methylene-y-butyro-lactone compounds (6a-g) were determined against three cell lines (PM-3A, P-388, and K-562) and showed the moderate antitumor activity ($IC_50$ ranged from 1.4 to 4.3 $\mu\textrm{g}$/ml) with the compound $5^1$-methyl-$5^1$ -[(9H-hypoxanthin-9-yl)methyl]-$2^1$-oxo-$3^1$-methylenetetrahydrofuran (6g) showing the least antitumor activity.

• 대한방사선기술학회지:방사선기술과학
• /
• 제13권2호
• /
• pp.37-42
• /
• 1990

The paper is based on the record of researching the patients with cancer in the Chun-nam National University Hospital from September 1985 to December 1988. The results are the as follows ; 1. Among the total O.P.D. 921, 028, the patients of Therapeutic Radiology (Opening the Therapeutic Radiology in September) are classified into 27,159(2.95%), (186 in 1985, 2,388 in 1986, 10,511 in 1987, and 14,074 in 1988) 2. Among the 4,925 cancer patients, cervix and uterus cancer patients are 1,138(23.10%), stomach cancer patients are 592(12.02%), brain and thyroid cancer patients are 565(11.47%), liver cancer patients are 400 (8.12%), lung cancer patients are 355 (7.20%) and sexual ratio appeared 1 : 1.13. Therefore, female patients are a slightly more than the male patients. 3. The age distribution of cancer was that of $45{\sim}54$ ages are 1,244(25.26%), $55{\sim}64$ ages are 1,119(22.72%) and $35{\sim}44$ ages are 773(15.70%) and the half of all the cancer patients are $45{\sim}64$ ages. 4. Among the 2,519 cancer patients, 742(29.46%) are in the uterus system, 620(24.62%) are in the brain and thyroid part, 402 (15.96%) are in the lungs. Therefore, these three kinds of cancer consist of 70%. 5. The occupational distribution of 3,067 cancer patients ($87{\sim}88\;year$) house wives are 636 (20.73%), orderly farmers are 622 (20.28%) public service personnells are 193 (6.29%), salarymen are 162(5.28%) and businessmen are 159(5.18%).