• 약학회지
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• 제51권6호
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• pp.463-468
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• 2007

Chong Myung Tang is consisted of three medicinal herbs (Acori Graminei Rhizoma, Polygalae Radix and Hoelen cum Radix). It has been used as a medicine for the purpose of learning and memory improvement. In this paper, Chong Myung Tang was screened the biological activities for Alzheimer's disease. The extract (70% ethanol) of Acari Graminei Rhizoma (1 mg/ml) showed that acetylcholinesterase (AChE) and amyloid beta ($A{\beta}$) peptide aggregation inhibitory potency are 43.1% and 76.5%, respectively. The extract of Polygalae Radix showed inhibitory activity against $A{\beta}_{1-42}$ peptide aggregation (51.5%). To predict the drug-likeness, oral absorption ability; blood-brain barrier (BBB) penetraion rate, mutagenecity and carcinogenicity; in silico screening was performed against 16 compounds in the three medicinal herbs. According to the results, all compounds have appropriate chemical structures as medicines. The six compounds in Acori Graminei Rhizoma and the five compounds in Hoelen cum Radix showed excellent oral absorption rate and BBB penetration rate. The four compounds in Polygalae Radix showed excellent oral absorption rate, but their BBB penetration was presented low rate. And, the extract of Hoelen cum Radix didn't show AChE and $A{\beta}_{1-42}$ peptide aggregation inhibitory activities in vitro. Therefore, their activity in brain may be other mechanism. According to all of the results, in silico prediction technology is convenient and effective to determine biological active compounds in medicinal herbs.

• 대한한의학회지
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• 제32권3호
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• pp.35-43
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• 2011

Objectives: This study was performed to screen target-specific inhibitors of ${\beta}$-catenin/TCF signaling whose functional activation plays an important role in early events in carcinogenesis. Methods: To investigate the activation or suppression of ${\beta}$-catenin/TCF transcription, we established a transiently transfected cell line with a constitutively active ${\beta}$-catenin mutant gene whose product is not degraded. This cell line was also co-transfected with luciferase reporter gene constructs containing either an optimized (TOPflash) or mutant (FOPflash) TCF-binding element. We investigated cytotoxic effects using a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium salt (MTS) assay. To find effective inhibitors of ${\beta}$-catenin/TCF signaling from medicinal herbs, the crude extracts of 99 types of medicinal herbs were screened using a luciferase assay system in HEK-293 and SH-SY5y cells. Results: At a concentration of $50{\mu}g$/ml, extracts of Angelica koreanae radix, Cannabis sativa semen, Ephedrae intermedia Schrenk radix, and Vitis rotundifolia fruit showed the following inhibitory effects on ${\beta}$-catenin/TCF signaling: $40{\pm}5.6%$, $23{\pm}6.1%$, $8{\pm}5.1%$, and $22{\pm}9.8%$ in ${\beta}$-catenin-activated HEK-293 cells and $9{\pm}4.7%$, $39{\pm}8.1%$, $39{\pm}6.4%$, and $42{\pm}10.1%$ in ${\beta}$-catenin-activated SH-SY5y cells, respectively. Crude extracts of E. radix were isolated by silica gel column chromatography, and two non-polar fractions of these extracts showed inhibitory effects on ${\beta}$-catenin/TCF signaling. Conclusions: In this study, we established a transiently transfected cell line as a screening system and found that various medicinal herb extracts had inhibitory effects on ${\beta}$signaling.

• 한국식물병리학회지
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• 제13권1호
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• pp.63-68
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• 1997

In the screening of antiviral materials produced by actinomycetes, an isolate named B25 was fond to produce an antibiotic substance ASA, which showed a strong inhibitory activity against tobacco mosaic virus (TMV) infection. ASA was purified from culture broth of B25 by silica gel column chromatography, preparative TLC, and reversed phase HPLC. Also MS, IR, UV spectrum, and melting point of ASA were determined and analysed. ASA was white powder soluble in dimethyl sulfoxide, chloroform, and ethyl acetate, having absorption peaks at 223 and 328 nm in UV-VIS spectrum, and had a molecular weight of 548. ASA showed strong inhibitory effect on TMV infection when it was applied as a mixture of TMV to the upper surface of leaves of a local lesion host (Nicotiana tabacum c. Xanthi-nc). It also showed antimicrobial effect against yeast and some phytopathogenic fungi.

• 약학회지
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• 제39권3호
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• pp.306-313
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• 1995

The aim of the present study was to produce low molecular weight cathepsin B inhibitor. A strain of Streptomyces aburabiensis isolated from soil in Korea was selected and the optimum condition for the production of the inhibitor was evaluated. Glucose and soytone were selected as best carbon and nitrogen sources, respectively. From the kinetic analysis in batch fermentation, it was found that the specific cathepsin B inhibitor production rate (q$_{p}$) was linearly related to specific growh rate ($\mu$). The inhibitor in culture filtrate was purified by adsorption on activated charcoal, butanot extraction, silica gel chromatography, ion exchange chromatography using Dowex-1 (Cl form) and Amberlite IRC-50 (H$^{+}$ form), and preparative TLC. From the UV, IR, Mass spectroscopy and $^{1}$H-NMR, the inhibitor was thought to be a new inhibitor of which molecular weight was 199.

• 한국미생물·생명공학회지
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• 제24권3호
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• pp.321-326
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• 1996

In the course of screening for new bioactive compounds from oligotrophs in soil, a microorganism, designated as SA-246 and now identified as Micromonospora sp., has been shown to produce a strong antibacterial compound. The active compound was purified from broth filtrate by ethylacetate extraction, silica gel column chromatography, preparative TLC and HPLC, and was identified as crisamicin A based on mass and NMR spectral data. The compound SA- 246 exhibited not only strong antibacterial activity against Gram-positive bacteria but also cytotoxicity against cancer cell lines such as A549 (lung), SK-OV-3 (ovarian), SK-MEL-2 (melanoma), XF498 (central nervous system) and HCT15 (colon).

• 한국미생물·생명공학회지
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• 제21권4호
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• pp.322-328
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• 1993

During the screening of antifungal compounds from microbial secondary metabolites to control phytophthora blight of red pepper caused by Phytophthora capsici, a soil isolate, strain 38D10 was selected. Based on taxonomic studies, this strain was identified as Streptomyces neyagawaensis. The antifungal compound was purified from culture broth by HP-20 column chromatography, ethyl acetate extraction, silica gel column chromatography, HPLC and identified as concanamycin B by UV. $^1H$-NMR, $^{13}C$-NMR, SIMS analysis. Concanamycin B has strong antifungal activity against some phytopathogenic fungi but not antivacterial activity and preventive value were 50% and 100% at 125ppm and 250ppm in pot assay.

• Journal of Microbiology and Biotechnology
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• 제19권3호
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• pp.286-290
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• 2009

In the course of screening for substances inhibiting apoptosis of U937 human leukemia cells induced by etoposide ($10\;{\mu}g/ml$), Forsythiae fructus, which showed a high level of inhibition, was selected. The regulating compounds were purified from the ethyl acetate extract by silica gel column chromatography and HPLC. The active substance was purified and identified as rengyolone by spectroscopic methods. This compound showed inhibitory activity on caspase-3 induction, a major protease of the apoptosis cascade, with an $IC_{50}$ value of $38.96\;{\mu}M$ after 8 h of etoposide treatment in U937 cells. The expression level of caspase-3 and poly(ADP-ribose) polymerase (PARP) were dose-dependently inhibited by the compound, suggesting that rengyolone inhibits etoposide-induced apoptosis via downregulation of caspases.

• 한국미생물·생명공학회지
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• 제24권5호
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• pp.574-578
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• 1996

In the course of screening for the antifungal compounds against Candida albicans, an antifungal compound (F1480) was isolated from the culture broth of Aspergillus candidus F1484. Isolation and purification of compound F1484 were performed using ethyl acetate extraction, silica gel column chromatography, ODS column chromatography, and preparative HPLC. The structure of compound F1484 was determined by the spectroscopic analyses of EI-MS, $^{13}$C, $^{1}$H-NMR, DEPT, HMQC, and HMBC. This compound appeared to have a structure of antifungal agent, chloroflavonin. In addition to antifungal activities against the yeast phase of Candida species, compound F1484 showed cytotoxic effect against various human tumor cell lines.

• 약학회지
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• 제50권6호
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• pp.367-371
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• 2006

Phellinus pini (Hymenocaetaceae) has been used for the immunomodulating activity hypolipidemic effect, gastric cancer non-insulin dependant diabetes, diarrhea, and menstrual irregularity. From the screening of each fraction for the inhibitory activity of NO production in lipopolysaccaride (LPS) activated RAW 264.7 cells, methanol extract of Phellinus pini and hexane soluble fraction exhibited inhibition of NO production compared with LPS control without toxicity. The hexane soluble fraction showed dose dependent inhibition of NO production. According to activity guided fractionation, the active hexane fr. was repeatedly chromatographed over silica gel, ergosta-4,6,8(14),22- tetraen-3-one was isolated. The compound inhibited NOS activation (IC$_{50}$ = 29.7 uM) and NO production of activated macrophage at 30 uM.

• 한국미생물·생명공학회지
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• 제23권1호
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• pp.98-103
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• 1995

During the screening of antifungal antibiotics from microbial metabolites, we selected Pseudomonas aeruginosa KGM-100 showing powerful antagonistic activity against various phytopathogenic fungi. Antibiotics KGM-100A and KGM-100B were purified from the culture broth of Pseudomonas aeruginosa KGM-100 by diaion HP-20 column chromatography, ethyl acetate extraction, silica gel column chromatography, preparative TLC and recrystallization. KGM-100A which was recrystallized in MeOH showed antimicrobial activities against a broad spectrum of fungi and bacteria. Physico-chemical properties of KGM-100A were determined and identified to be phenazine-l-carboxylic acid by UV, IR, $^{1}$H-NMR, $^{13}$C-NMR, mass spectrum, and elemental analyses.