• Title/Summary/Keyword: in silica screening

Search Result 67, Processing Time 0.026 seconds

Screening of Microorganisms Having ACAT Inhibitor Activity from Soil and Characterization of AI-3, ACAT Inhibitor Produced by Streptomyces sp. A-3 (토양으로부터 ACAT 저해활성을 나타내는 미생물의 탐색과 방선균이 생산하는 ACAT 저해물질, AI-3의 특성)

  • 정태숙;김성욱;이항우;손광희;권용욱;최명언;복성해
    • Microbiology and Biotechnology Letters
    • /
    • v.21 no.6
    • /
    • pp.600-608
    • /
    • 1993
  • About 1, 300 strains isolated from soil were evaluated for acyl-CoA:cholesterol acyltransferase (ACAT) inhibition activity. About 4.0% of actinomycetes and 3.6% of fungi showed greater than 50% inhibition activity, respectively. However, none of the isolated bacteria exhibited inhibition activity more than 50%. Among them, one Streptomyces sp. A-3 showed a higher ACAT inhibition activity in culture broth. Isolation of the ACAT inhibitor (AI-3) was achieved by Amberlite XAD-7 column, silica-gel column, Sephadex LH-20 gel-filtration and reverse phase HPLC.

  • PDF

Screening Tests on the Constituents of the Xanthoxylum Drugs (산초류 생약의 성분 검색)

  • Kown, Chang-Ho;Hong, Nam-Doo;Kim, Chang-Min
    • Korean Journal of Pharmacognosy
    • /
    • v.4 no.4
    • /
    • pp.209-212
    • /
    • 1973
  • The pericarpia of Xanthoxylum piperitum D.C., X. coreanum $N_{AKAI}$ and Fagara mandshurica are used as an identical botanical drug in Korea. Although it is difficult to differentiate these three drugs on the basis of morphological characteristics, they can be easily identified by applying ethyl ether extracts of them on a silica gel thin-layer plate, using several developing solvent systems and color reagents, and comparing the component spots. The pericarpium of F. mandshurica gave the most spots and that of X. piperitum the least, which is also different from that of X. coreanum.

  • PDF

Anti-microbial and Anti-inflammatory Activity of New 4-methoxy-3-(methoxymethyl) Phenol and (E)-N'-(5-bromo-2-methoxybenzylidene)-4-methoxy Benzohydrazide Isolated from Calotropis gigantean white

  • Manivannan, R.;Shopna, R.
    • Natural Product Sciences
    • /
    • v.23 no.1
    • /
    • pp.69-74
    • /
    • 2017
  • A new phenol and hydrazide derivatives were obtained for the first time from the C. giganteawhite by silica gel column chromatography. The structure of the isolated compounds was identified by UV, IR NMR and MS. C. gigantea was scientifically reported for several medicinal properties viz. analgesic, antimicrobial and cytotoxic. In this screening work, anti-microbial activity of test compounds was found to be active against all organisms. Additionally, anti-inflammatory activity of the test groups has reduced the thickness of edema of the hind paw compared to the control group.

Novel Antioxidants, Stc-l and Stc-2, from Stereum ostrea

  • Kim, Young-Hee;Yun, Bong-Sik;Kim, Jong-Pyong;Moon, Suk-Sik;Yoo, Ick-Dong
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 1998.11a
    • /
    • pp.131-131
    • /
    • 1998
  • In the course of screening for new natural compounds having antioxidant activity from microbials, mushrooms as well as plants. We have isolated novel sesquiterpenoid and officinalic acid from methanolic extracts of Stereum ostrea. The dried fruit body( 450 g) of Stereum ostrea was extracted with methanol, then methanolic extract was partitioned between water and hexane, chloroform, and ethyl acetate, subsequently. The chloroform extract was subjected on silica gel, Sephadex LH-20 and RP-18 column chromatography, successively. And two compounds were isolated and identified as new triterpenoids and officinalic acid using $^1$H - NMR, $\^$13/C - NMR as well as Mass spectra.

  • PDF

Screening of Antioxidants to Human Low Density Lipoprotein (LDL) from Marine Resources (수산자원으로부터 Human Low Density Lipoprotein (LDL)에 대한 항산화제의 탐색)

  • 류병호
    • Journal of Food Hygiene and Safety
    • /
    • v.14 no.2
    • /
    • pp.153-159
    • /
    • 1999
  • This study was undertaken to evaluate antioxidative activities of substances isolated from marine resources against human low density lipoprotein (LDL). Methanol-water extract(80 : 20, v/v) of Sargassum ringgoldianum had the highest antioxidant activity and the active substance was purified by silica gel column chromatography by eluting chlorform : methanol mixture (80 : 20 v/v). The active fraction was seperated to several spots on the TLC in chlorofrom : methanol (10 : 1, v/v) mixture. Antioxidative activity of band 4 of fraction 2 on TLC was highest than that of $\alpha$-tocopherol against human LDL oxidation by the method of thiobarbituric acid reactive substance (TBARS). The band 4 of fraction 2 inhibited the copper mediated oxidation of human LDL with almost completely at 1 or 2 mg/ml.

  • PDF

PAF Antagonistic Activity of 2-hydroxy-3-methoxybenzoic Acid Glucose Ester from Gentiana scabra

  • Huh, Hoon;Kim, Hye-Kyong;Lee, Hern-Ku
    • Archives of Pharmacal Research
    • /
    • v.21 no.4
    • /
    • pp.436-439
    • /
    • 1998
  • In order to find out anti-platelet activating factor (PAF) from natural resources, Korean medicinal plants used for the treatments of peripheral circulation disorders were tested for their possible protective effects on PAF-induced anaphylactic shock. From the above screening, the methanol extract of Gentiana scabra showed a potent antagonistic activity against PAF. Water suspension of the extract was partitioned with $CH_2$$CI_2$ and EtOAc, successively. The EtOAc fraction which showed the highest activity was chromatographed on silica gel to yield 6 fractions. From the fraction which showed higher PAF-antagonistic activity than the other fractions, compound 1 was isolated by recrystallization. On the basis of spectral data, compound 1 was identified as 2-hydroxy-3-methoxybenzoic acid glucose ester. The compound prevented the mice from the PAF-induced death at a dose of 300 $\mu\textrm{g}$/mouse.

  • PDF

Screening and Purification of an Anti-Prostate Cancer Compound, Deoxypodophyllotoxin, from Anthriscus sylvestris Hoffm (전호(Anthriscus sylvestris Hoffm)로부터 전립선 암세포 저해물질인 deoxypodophyllotoxin 의 탐색 및 분리)

  • Cho, Hyo-Jin;Yu, Sun-Nyoung;Kim, Kwang-Youn;Sohn, Jae-Hak;Oh, Hyun-Cheol;Ahn, Soon-Cheol
    • Journal of Life Science
    • /
    • v.19 no.1
    • /
    • pp.9-14
    • /
    • 2009
  • The prostate cancer is the critical health problem, increasing of its related death in worldwide. Unfortunately present surgery and chemotherapeutic choices seem to be impossible in curing or controlling prostate cancer, because metastasis occasionally advances even after these potentially curative therapies. Therefore, there is immediate need to alternative chemoprevention and chemotherapeutic agents. Over one hundred species of dried medicinal herbs were tested for proliferation inhibitory effects on prostate cancer cell line, PC-3. One of them, Anthriscus sylvestris was selected because of potent anti-proliferation effect. The dried root of A. sylvestris was extracted with 100% methanol for 2-3 days and its extract was fractionated by using ethyl acetate. And ethyl acetate layer was subjected to column chromatographies on silica gel, reverse phase-18 (RP-18) and Sephadex LH-20, in turn. Finally, the pure compound was obtained by crystallization in methanol at $4^{\circ}C$ for overnight and identified as deoxypodophyllotoxin by NMR spedorscopic and physico-chemical analyses. In addition, it was confirmed that deoxypodophyllotoxin clearly inhibits the proliferation of PC-3 cells in a dose and time-dependent manner.

Antibacterial Activity of Salvia Miltiorrhiza against Methicillin-resistant Staphylococcus aureus (丹參의 methicillin 내성 황색포도구균에 대한 효과)

  • Seo, Myung-won;Jeong, Seung-il;Shin, Chol-gyun;Ju, Young-sung;Kim, Hong-jun;Ko, Byoung-seob
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
    • /
    • v.16 no.1
    • /
    • pp.94-99
    • /
    • 2003
  • Objectives : Gram-positive bacteria have became increasing resistant to antibacterial agents, and hence multi-drug-resistant bacterial pathogens are now a major problem in clinical medicine. There is, therefore, a need for new antibacterial agents. In the course of our screening program for potent antibacterial agent from medicinal plants, the extract of Salvia miltiorrhiza (S. miltiorrhiza) showed antibacterial activity against methcillin resistant Staphylococcus aureus (MRSA) and antibiotic-resistant S. aureus. Methods : S. miltiorrhiza was extracted with 80$\%$ EtOH. The extract was suspended in H2O and fractionated successively with hexane chloroform, ethyl acetate, and n-buthanol. The chloroform fraction, which showed the highest antibacterial activity(MICs, 78㎍/ml) against MRSA, was chromatographed on a silica gel column and recycling prep-LC to give the pure antibacterial component. Results and Conclusions : The second fraction among the chloroform soluble portion of an aqueous EtOH extract of S. miltiorrhiza root showed outstanding antibacterial activity against MRSA and antibiotic-resistant S. aureus compared to the other fraction. An active compound was isolated from the second fraction using silica gel column chromatoraphy and recycling prep-LC. Based on these data together with the IH-, 13C-NMR, mass and mp, the active compounds were identified tanshinone Ⅰ, dehydrotanshinone Ⅰ and cryptotanshinone. Among tanshinones, cryptotanshinone and dihydrotanshinone Ⅰ MICs against MRSA and antibiotics-resistant S. aureus were 12.5, 12.5 and 6.3㎍/ml, respectively.

  • PDF

Screening of Leukotriene $B_4$ Receptor Antagonist Activity from the Herbal Drugs (생약의 류코트리엔 $B_4$ 수용체결합 저해작용 검색)

  • Lee, Hwa-Jin;Ryu, Jae-Ha
    • Korean Journal of Pharmacognosy
    • /
    • v.31 no.3
    • /
    • pp.273-279
    • /
    • 2000
  • Leukotriene $B_4\;(LTB_4)$ is a pro-inflammatory mediator synthesized in myeloid cells from arachidonic acid. Elevated levels of $LTB_4$ have been found in a number of inflammatory diseases and levels are related to disease activity in some of these. Because $LTB_4$ interacts with cells through specific cell surface receptors, $LTB_4$ receptor blockade is the most specific approach to reduce the pathogenic role of $LTB_4$. In order to find $LTB_4$ receptor antagonist from plants, we screened the $LTB_4$ receptor antagonistic activity of the methanol extract and solvent fractions of herbal drugs. The ability of samples to inhibit specific binding of $[^3H]-LTB_4$ to human peripheral neutrophils was used as assay to evaluate the antagonistic activity of plant materials. Among the tested methanol extracts of herbal drugs, Mori Radicis Cortex, Perillae Semen, Armeniacae Semen and Sophorae subprostratae Radix showed potent inhibitory activity above 70% at the concentration of $100\;{mu}g/ml$. The inhibitory activities of $LTB_4$ binding to human neutrophils were evaluated for several solvent fractions at three different concentrations. Especially, hexane soluble fractions of Anemarrhenae Rhizoma and Embeliae Radix, and ethyl acetate soluble fractions of Aristolochiae Fructus, Magnoliae Cortex and Zingiberis Rhizoma crudus showed moderate activity at $25\;{mu}g/ml$. These fractions were promising candidates for the study of the activity-guided chromatographic purification of active compounds. Silica gel column chromatography of hexane soluble fractions of Anemarrhenae Rhizoma and Embeliae Radix gave very active sub-fractions, AA-4 and ES-4, and their inhibition activities of $LTB_4$ binding to human neutrophil at $30\;{mu}g/ml$ were 78% and 62%, respectively. From these results we could anticipate new $LTB_4$ receptor antagonist from herbal drugs, and the block of $LTB_4$ effects may provide beneficial in neutrophil mediated diseases such as inflammation and bronchial asthma.

  • PDF

A Caspase Inducing Inhibitor Isolated from Caesalpinia sappan (소목(Caesalpinia sappan)으로부터 분리한 caspase 유도 저해 물질)

  • Son, Eun-Jung;Kim, Jin-Hee;Kim, Hyun-A;Baek, Seung-Hwa;Kho, Yung-Hee;Kim, Mee-Ree;Lee, Choong-Hwan
    • Korean Journal of Food Science and Technology
    • /
    • v.35 no.4
    • /
    • pp.680-683
    • /
    • 2003
  • Through the screening of caspase-3 inducing inhibitors in U937 human monocytic leukemia cell from natural sources, Caesalpiniae sappan, which showed a high level of inhibition, was selected. The inhibition compound was purified from methanol extract by silica gel column chromatography and HPLC. The inhibitor was identified as brazilin by spectroscopic methods of ESI-MS, $^1H-NMR$, and $^{13}C-NMR$. Brazilin showed inhibitory activity of caspase-3 induction, a major protease of apoptosis cascade, with $IC_{50}$ value of $4.5\;{\mu}g/mL$ after 7 hr of treatment in U937 cells.