• Title/Summary/Keyword: inhibitory compounds

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Evaluation of Two Biologically Active Compounds for Control of Wheat Root Rot and its Causal Pathogens

  • Hashem, Mohamed;Hamada, Afaf M.
    • Mycobiology
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    • v.30 no.4
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    • pp.233-239
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    • 2002
  • The main aim of this study is to evaluate the efficiency of two biologically active compounds(Strom and F-760) in control of wheat root rot disease and its causal organisms. Fusarium graminearum, F. oxysporum, F. solani and Bipolaris sorokiniana were used as target organisms. In vitro, the two compounds showed fungicidal effect on all investigated pathogens resulted in suppression of radial growth and mycelial dry weight of them. Under greenhouse conditions, treatment of wheat grains with either Strom or F-760 before cultivation significantly reduced the percent of disease distribution as well as the mean disease rating of plants in both seedling and flowering stages. Fresh and dry weights of plants as well as water maintenance capacity were increased as the result of applying these compounds as seed dressing. Also data showed that the membrane stability of plants was injured as a result of infection with all investigated organisms, while this injury was alleviated when F-760 and Strom were applied. The $K^+$ efflux and the leakage of UV absorbing metabolites was stimulated with fungal infection. However, F-760 and Storm treatment partially retarded the stimulatory effect on leakage of $K^+$ and UV-absorbing metabolites of fungal infected plants. On the other side, the fungal infection had inhibitory effects on pigment fractions(chlorophyll a, b, and carotenoids) biosynthesis in wheat leaves. This retarding effect was partially or completely alleviated as the grains were treated with the applied compounds.

Cytotoxic Compounds from the Flowers of Paulownia coreana (오동나무꽃의 항암성분)

  • Oh, Joa-Sub;Zee, Ok-Pyo;Moon, Hyung-In
    • Korean Journal of Pharmacognosy
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    • v.31 no.4
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    • pp.449-454
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    • 2000
  • In search for plant-derived cytotoxic compounds, it was found that the $CHCl_3$ and EtOAC extracts obtained from the flowers of Paulownia coreana Uyeki (Scrophulariaceae) exhibited significant cytotoxic activity against human tumor cell lines, A549, SK-OV-3, SK-MEL-2, XF498, and HCT15. Activity-guided fractionation on the basis of the inhibitory activity against the growth of human tumor cell lines, in vitro, and repeated column chromatography afforded several cytotoxic compounds from P. coreana. The structures and stereochemistry of these compounds were established, on the basis of analysis of spectra including IR, UV, EI-MS, $^{1}H-NMR,\;^{13}C-NMR$ and some chemical transformations, as Compound PCCl $(2-hydroxy-4(15),11(13)-eudesmadien-8{\beta},12-olide)$, Compound $PCC2(2,3-dihydro-4-hydroxy-1(15),11(13)-xanthadien-8{\beta},12-olide)$, Compound PCE1 (chrysophanol), Compound PCE2 (emodin), Compound PCE3 (physcion). Cytotoxic activity of compounds obtained from P. coreana. on five tumor cells lines was evaluated by procedure of SRB methods.

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Secondary Metabolites Isolated from Ganoderma lucidum and Their Anti-inflammatory Activity (영지버섯(Ganoderma lucidum)으로 부터 분리한 이차대사산물 및 이들의 항 염증 활성)

  • Kim, Hye Ji;Koo, Man Hyung;Lee, Jun Hyuck;Suh, Sung-Suk;Youn, Ui Joung
    • Korean Journal of Pharmacognosy
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    • v.50 no.3
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    • pp.232-238
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    • 2019
  • Phytochemical study of Ganoderma lucidum (Polyporaceae) let to the isolation of five lanostane triterpenoid (1-5), along with two nitrogen derived phenolic compounds, N-phenylethylformamide (6) and N-acetylphenethylamine (7). The structures of the compounds were determined by 1D and 2D NMR, and MS experiments, as well as by comparison of their data with published values. Compounds 6 and 7 were isolated for the first time from the genus Ganoderma and this species. All the compounds were evaluated for cancer chemopreventive potential based on their ability to inhibit nitric oxide (NO) production induced by lipopolysaccharide (LPS) in mouse macrophage RAW 264.7 cells in vitro. Among the isolates, compounds 2 and 3 showed moderate inhibitory activity against NO production.

Synthesis, Docking Study and In-vitro Evaluation of Anti-Tuberculosis Activity of Tri Substituted Imidazoles Containing Quinoline Moiety

  • Sahana, S.;Vijayakumar, G.R.;Sivakumar, R.;Sriram, D.;Saiprasad, D.V.
    • Journal of the Korean Chemical Society
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    • v.66 no.3
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    • pp.194-201
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    • 2022
  • A simple, efficient, and cost-effective method has been employed for the synthesis of 2,4,5-trisubstituted imidazole derivatives (3a-j) containing quinoline substituent at 2nd position. Title compounds were obtained by multicomponent reaction (MCR), involving aryl substituted 1,2-diketone, quinoline carbaldehyde and ammonium acetate in the presence of acetic acid solvent under mild reaction conditions. The newly synthesized quinoline containing imidazole derivatives were confirmed through FT-IR, 1H-NMR, 13C-NMR and mass spectral analysis. In-vitro microplate alamar blue assay (MABA) to determine the MIC (minimum inhibitory concentration) values against Mycobacterium tuberculosis H37Rv was performed for the synthesized compounds. The synthesized compounds exhibited activity against Mycobacterium tuberculosis and among which compounds, 3d, 3f and 3i showed good activity. The highest activity was showed with compound 3i. The anti-mycobacterial activity results are well correlated with the computational molecular docking analysis, which was performed for the synthesized compounds prior to the evaluation of the activity.

12,13-Dihydroxyfumitremorgin C, Fumitremorgin C, and Brevianamide F, Antibacterial Diketopiperazine Alkaloids from the Marine-Derived Fungus Pseudallescheria sp.

  • Zhang, Dahai;Noviendri, Dedi;Nursid, Muhammad;Yang, Xiu-Dong;Son, Byeng-Wha
    • Natural Product Sciences
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    • v.13 no.3
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    • pp.251-254
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    • 2007
  • Dioxopiperazine alkaloids, 12R,13S-dihydroxyfumitremorgin C (1), fumitremorgin C (2), and brevianamide F (3), were isolated from the marine-derived fungus Pseudallescheria, and the absolute stereostructures of compounds 1 - 3 were elucidated on the basis of chemical and physicochemical evidence. Compounds 1 - 3 showed an antibacterial activity against Staphylococcus aureus, methicillin-resistant S. aureus, and multidrug-resistant S. aureus. The MIC (minimum inhibitory concentration) values of compounds 1 - 3 were 125 ${\mu}g/mL$ for all strains.

The Design and Synthesis of 1,4-Substituted Piperazine Derivatives as Triple Reuptake Inhibitors

  • Han, Min-Soo;Han, Young-Hue;Song, Chi-Man;Hahn, Hoh-Gyu
    • Bulletin of the Korean Chemical Society
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    • v.33 no.8
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    • pp.2597-2602
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    • 2012
  • Novel 1,4-substituted piperazine derivatives 5, Series A and B were designed by fragment analysis and molecular modification of 4 selected piperazine-containing compounds which possess antidepressant activity. We synthesized new 39 analogues of Series A and 10 compounds of Series B, respectively. The antidepressant screening against DA, NE, and serotonin neurotransmitter uptake inhibition was carried out using the Neurotransmitter Transporter Uptake Assay Kit. The compounds in Series B showed relatively higher reuptake inhibitory activity for SERT, NET, and DAT than those in Series A. The length of spacer between the central piperazine core and the terminal phenyl ring substituted at the piperazine ring in Series B seems to exert an important role in the activity.

Synthesis of Hydroxylactams and Esters Derived from Thalidomide and Their Antitumor Activities

  • Sun, Guanglong;Liu, Xiangchao;Zhou, Heng;Liu, Zenglu;Mao, Zhenmin
    • Bulletin of the Korean Chemical Society
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    • v.35 no.5
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    • pp.1337-1342
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    • 2014
  • A novel and convenient route for the synthesis of a series of thalidomide derivatives is described. Compound 2 was cyclized with different amines under alkaline condition to obtain 4-nitro substituted phthalimidines 3a-d. Hydroxylactams 4a-d were produced via bromination and hydroxylation. Different acyl chlorides were reacted with hydroxylactams to provide the desired esters 5a-d. All compounds were evaluated by MTT assay for their inhibitory activities against HCT-116, MG-63, MCF-7, HUVEC and HMVEC cell lines in vitro. Most of them showed no obvious cytotoxic effect on normal human cells, compounds 4a-d, $5a_2$, $5a_4$, $5a_5$, $5b_2$, $5c_2$ and $5d_2$ exhibited potent antitumor activities, among which compounds $5a_2$ and $5b_2$ were more effective than 5-FU.

Two p-Terphenyls from Mushroom Paxillus panuoides with Free Radical Scavenging Activity

  • Yun, Bong-Sik;Lee, In-Kyoung;Kim, Jong-Pyung;Yoo, Ick-Dong
    • Journal of Microbiology and Biotechnology
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    • v.10 no.2
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    • pp.233-237
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    • 2000
  • As part of a continuing investigation to identify free radical scavengers from the fruit bodies of basidiomycetes, we isolated two p-terphenyl compounds, designated as PAl and PA2l, from cethanolic extract of the fruit body of Pasillus panuoides. The methanolic extract was processed by ethyl acetate extraction and silica gel column chromatography to yield two active fraction. PAl was obtained from one of the fractions through Sephadex LH-20 and silica gel column chromatographies and reverse-phase HPLC. The other fraction was purified by Sephadex LH-20 and reverse-phase column chromatographies to produce PA2. The compounds PA1 and PA2 were identified as leucomentin-4 and leucomentin-2, respectively, on the basis of various spectroscopic analyses. These compounds exhibited strong inhibitory activities against lipid peroxidation in rat liver microsomes with IC_{50}$ values of 0.10 and $0.06{\;}\mu\textrm{g}ml$, respectively.

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Natural Compounds from Danshen Suppress the Activity of Hepatic Stellate Cells

  • Oh, Seong-Hwan;Cho, Kyung-Hwan;Yang, Beom-Seok;Roh, Yong-Kyun
    • Archives of Pharmacal Research
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    • v.29 no.9
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    • pp.762-767
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    • 2006
  • Danshen is an herbal medication frequently used in oriental medicine to treat liver or kidney malfunction. In the course of our studies, we observed that compounds purified from Danshen exhibit an inhibitory activity against Discoidin Domain Receptor 2 (DDR2) tyrosine kinase. Through this inhibition, these compounds also inhibited the growth of HSC T6 cells and suppressed the expression of alpha-smooth muscle actin and MMP2, as well as collagen synthesis, all of which are increased in activated liver stellate cells. Given that activation of liver stellate cells is the hallmark of liver fibrosis and that DDR2 plays a critical role in this activation, these results suggest that one of the pharmacological activities of Danshen extract that protects the liver is the inhibition of key cell-signaling kinases, such as DDR2, in liver stellate cells.

Bioactive Metabolites from Selected Sponges of Korean and Tropical Waters

  • Shin, Jong-Heon;Park, Jung-Rae;Seo, Young-Wan;Lee, Hyi-Seung;Cho, Ki-Woong
    • Proceedings of the PSK Conference
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    • 2001.04a
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    • pp.90-94
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    • 2001
  • Wondonins A and B, aromatic alkaloids of an unprecedented skeletal class have been isolated form and association of the sponges Poecillastra wondoensis and Jaspis sp. In addition, four novel bromotyrosine-derived metabolites, psammaplins $A_1$ and $A_2$, aplysinellins A and B, have been isolated from the tropical sponge Aplysinella rhax. The structures of these compounds have been determined on the basis of combined chemical and spectral analyses. The new compounds exhibited significant cytotoxicity and antiangiogenic activity as well as inhibitory activities against farnesyl protein transferase and leucine aminopeptidase. In addition to these compounds, several bioactive metabolites have been isolated from sponges of Korean and tropical waters.

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