• Title/Summary/Keyword: IC-MS/MS

Search Result 256, Processing Time 0.027 seconds

MT-2007, Protein Kinase C Inhibitor from Aetinomycetes Isolate No. 2007-18 (방선균 분리주 No 2007-18이 생산하는 Protein Kinase C 저해물질, MT-2007)

  • 안종석;박문수;박찬선;윤병대;민태익;안순철;오원근;이현선;윤병대
    • Microbiology and Biotechnology Letters
    • /
    • v.21 no.1
    • /
    • pp.54-58
    • /
    • 1993
  • During the screening of inhibitors against protein kinase CCPKC) and the bleb formation of K562 cell induced by phorbol ester from microbial secondary metabolites, MT-2007 was purified by solvent extraction, and chromatographic techniques from Actinomycetes isolate No. 2007-18. It showed completely suppression of bleb formation of K562 cell surface induced by phorbol 12.13dibutylate at the concentration of 503.9 11M and ICso on PKC was 31.4 11M. Its structure was postulated as lasalocid A sodium salt by physico-chemical properties and UV, IR. MS, IH-NMR.

  • PDF

Methyl-Branched Fatty Acids, Inhibitors of Enoyl-ACP Reductase with Antibacterial Activity from Streptomyces sp. A251

  • Zheng, Chang-Ji;Sohn, Mi-Jin;Chi, Seung-Wook;Kim, Won-Gon
    • Journal of Microbiology and Biotechnology
    • /
    • v.20 no.5
    • /
    • pp.875-880
    • /
    • 2010
  • Bacterial enoyl-ACP reductase (FabI) has been demonstrated to be a novel antibacterial target. In the course of our screening for FabI inhibitors, we isolated two methyl-branched fatty acids from Streptomyces sp. A251. They were identified as 14-methyl-9(Z)-pentadecenoic acid and 15-methyl-9(Z)-hexadecenoic acid by MS and NMR spectral data. These compounds inhibited Staphylococcus aureus FabI with $IC_{50}$ values of 16.0 and $16.3\;{\mu}M$, respectively, but did not affect FabK, an enoyl-ACP reductase of Streptococcus pneumonia, at $100\;{\mu}M$. Consistent with their selective inhibition for FabI, they blocked intracellular fatty acid synthesis as well as the growth of S. aureus, but did not inhibit the growth of S. pneumonia. Additionally, these compounds showed reduced antibacterial activity against fabI-overexpressing S. aureus, compared with the wild-type strain. These results demonstrate that the methylbranched fatty acids show antibacterial activity by inhibiting FabI in vivo.

Anti-complement Activity of Triterpenoids from the Whole Plant of Patrinia saniculaefolia

  • An, Ren-Bo;Na, Min-Kyun;Min, Byung-Sun;Lee, Hyeong-Kyu;Bae, Ki-Hwan
    • Natural Product Sciences
    • /
    • v.14 no.4
    • /
    • pp.249-253
    • /
    • 2008
  • Two oleanane-type triterpenes (1, 2) and their glycosides (4-6), and one ursane-type triterpene (3) have been isolated from a methanolic extract of Patrinia saniculaefolia Hemsley (Valerianaceae) through repeated silica gel and reversed-phase C-18 column chromatography. Their chemical structures were determined as oleanolic acid (1), oleanonic acid (2), 23-hydroxyursolic acid (3), 3-O-${\alpha}$-L-arabinopyranosyl-oleanolic acid (4), 3-O-${\beta}$-D-glucopyranosyl-oleanolic acid (5), and oleanolic acid 3-O-[${\alpha}$-D-xylopyranosyl-($1{\rightarrow}3$)-${\beta}$-D-glucuronopyranoside-6-O-butyl-ester] (6) on the basis of their MS, $^1H$-, and $^{13}C$-NMR spectral data. All compounds were isolated from the whole plant of the P. saniculaefolia for the first time. These compounds were examined for their anti-complement activity against the classical pathway of the complement system. Among them, compounds 1 - 3 exhibited anti-complement activity with $IC_{50}$ values of 470.1, 212.2, and 121.0 ${\mu}M$, respectively, whereas compounds 4 - 6 were inactive. These results suggest that the carbonyl or hydroxy group at C-3 in the oleananeand/or ursane-triterpenes are important for the anti-complement activity against the classical pathway.

Xylaroisopimaranin A, a New Isopimarane Derivative from an Endophytic Fungus Xylaralyce sp.

  • Bao, Shang-Song;Liu, Hui-Hui;Zhang, Xue-Qing;Liu, Cheng-Xiong;Li, Xiao-Cong;Guo, Zhi-Yong
    • Natural Product Sciences
    • /
    • v.25 no.3
    • /
    • pp.228-232
    • /
    • 2019
  • Five secondary metabolites, including a new isopimarane derivative xylaroisopimaranin A (1), were isolated from the endophytic fungus Xylaralyce sp. (HM-1), and their structures were elucidated by 1D, 2D NMR, MS and CD spectra. Their bioactivities were performed to antibacterial, Hep G2 cells cytotoxicity and brine shrimp inhibition. The biological evaluation results showed that the xylaroisopimaranin A (1), xylabisboein B (2), griseofulvin (3), 5-methylmellein (4) and mellein-5-carboxlic acid (5) displayed no significant Hep G2 cells cytotoxicity and antibacterial acitivity, but they inhibited the brine shrimp with $IC_{50}$ from 0.5 to $25{\mu}mol/mL$.

Diels-Alder Type Adducts from Hairy Root Cultures of Morus macroura

  • Happyana, Nizar;Hakim, Euis H.;Syah, Yana M.;Kayser, Oliver;Juliawaty, Lia D.;Mujahidin, Didin;Ermayanti, Tri M.;Achmad, Sjamsul A.
    • Natural Product Sciences
    • /
    • v.25 no.3
    • /
    • pp.233-237
    • /
    • 2019
  • Three Diels-Alder type adducts, guangsangon E (1), chalcomoracin (2) and sorocein I (3) were isolated from hairy root cultures of Morus macroura. The structures of the isolated compounds (1-3) were determined by spectroscopic method (NMR and MS), and spectral comparison to literature. Cytotoxic activities of the isolated compounds (1 - 3) were investigated against P-388 murine leukemia cell line. Guangsangon E (1) showed the most potent cytotoxicity against P-388 murine leukemia cell line with $IC_{50}$ value of $2.75{\pm}0.32{\mu}g/mL$. To the best of our knowledge, guangsangon E (1) and sorocein I (3) were reported for the first time from the tissue cultures of M. macroura.

Chemical Constituents of Impatiens balsamina Stems and Their Biological Activities

  • Kim, Dong Hyun;Lee, Tae Hyun;Subedi, Lalita;Kim, Sun Yeou;Lee, Kang Ro
    • Natural Product Sciences
    • /
    • v.25 no.2
    • /
    • pp.130-135
    • /
    • 2019
  • The purification of the MeOH extract from Impatiens basamina by repeated column chromatography led to the isolation of one new tetrahydronaphthalene (1), together with eleven known compounds (2 - 12). The structure of the new compound (1) was determined by spectral data analysis ($^1H$ and $^{13}C$-NMR, $^1H-^1H$ COSY, HSQC, HMBC, NOESY, and HR-ESI-MS). Isolated compounds (1 - 12) were evaluated for their inhibitory effects on NO production in LPS-activated murine microglial BV-2 cells and their effects on NGF secretion from C6 glioma cells. Compounds 3, 7, and 10 reduced NO levels in LPS-activated murine microglial cells with $IC_{50}$ values of 26.89, 25.59, and $44.21{\mu}M$, respectively. Compounds 1, 5, and 9 upregulated NGF secretion to $153.09{\pm}4.66$, $156.88{\pm}8.86$, and $157.34{\pm}3.30%$, respectively.

Anticancer Activity and Chemical Composition of a Non-Polar Fraction from Asiasari Radix et Rhizoma (세신 비극성 분획의 항암 활성 및 성분 분석)

  • Cho, Seung-Sik;Kang, Bok Yun;Bae, Min-Suk;Shim, Jung-Hyun;Kim, Hyun Jung;Yoon, Goo
    • Korean Journal of Pharmacognosy
    • /
    • v.51 no.4
    • /
    • pp.264-269
    • /
    • 2020
  • The study aimed to characterize chemical composition and anticancer property of the n-hexane fraction derived from Asiasari Radix et Rhizoma. The anticancer activity was evaluated on a panel of cancer cell lines including HN22, HSC2, HSC3, and HSC4 cells (human oral cancer), HCC827 and HCC827GR cells (human lung cancer), and KYSE30 and KYSE450 (human esophageal cancer) by MTS assay. As a result, The least polar subfraction from n-hexane-soluble layer displayed notable cytotoxicity on the tumor cell lines with IC50 ranging from 1.20 to 17.0 ㎍/ml. The chemical composition of constituents in the active subfraction was determined by gas chromatography-mass spectrometry (GC-MS). The essential oils comprised of sesquiterpenes including β-gurjunene (7.45%), γ-amorphene (6.61%), guaia-6,9-diene (6.40%), δ-guaiene (5.21%) and a phenylpropanoid, safrole (0.49%) were mainly identified in addition to long-chain hydrocarbons including n-heptadecane (24.60%), 7-hexadecene (4.44%) and a diterpenoid, ent-kaur-16-ene (6.57%).

Phenolic Constituents from Balanophora laxiflora with their Anti-inflammatory and Cytotoxic Effects

  • Anh, Nguyen Thi Hong;Duong, Nguyen Thuy;Vinh, Pham Duc;Ha, Do Thi
    • Natural Product Sciences
    • /
    • v.27 no.1
    • /
    • pp.49-53
    • /
    • 2021
  • Balanophora laxiflora Hemsl. (Balanophoraceae) is a traditional medicinal plant with a diverse array of biological activities. In our exploration of new bioactive constituents from B. laxiflora, we isolated five compounds, including a new lignan, balanophorone (5), and four known phenolic compounds (1-4). The chemical structures of these compounds were determined by extensive spectroscopic analyses, including 1D and 2D NMR, HR-ESI-MS, and CD. In addition, we evaluated the effects of each of the isolates (1-5) on the messenger RNA expression levels of tumor necrosis factor (TNF)-α and cyclooxygenase (COX)-2 in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages and cytotoxicity against MCF-7 and MDA-MB-231 breast cancer cells. Compound 2 showed significant inhibition of LPS-induced COX-2 and TNF-α expression in RAW 264.7 macrophages, while compound 4 showed moderate cytotoxicity against MCF-7 and MDA-MB-231 breast cancer cells, with IC50 values of 18.3 and 30.7 µM, respectively. No significant effects on the viability of normal mammary epithelial cells were observed.

Molecular Networking-based De-replication Strategy Leads to the Isolation of a New Chromone from Pleosporales sp.

  • Kwon, Haeun;Kim, Jun Gu;Oh, Jeong-Joo;Kim, Jae-Jin;Kim, Gyu-Hyeok;Hwang, Bang Yeon;Yim, Joung Han;Lee, Dongho
    • Natural Product Sciences
    • /
    • v.26 no.4
    • /
    • pp.340-344
    • /
    • 2020
  • A new chromone analogue (1) was isolated from an EtOAc-extract of Pleosporales sp. culture medium, together with five known chromones (2 - 6). The isolation workflow was guided by a Molecular Networking-based dereplication strategy. The chemical structure of the new compound was elucidated using NMR and MS spectroscopy, and the absolute configuration was established by the Mosher's method. All isolated compounds were evaluated for their inhibitory effects on lipopolysaccharide-induced nitirc oxide production in RAW 264.7 macrophages. Compound 1 showed marginal inhibitory activity with an IC50 value of 118.7 μM.

Chemical Composition of Leaves, Stem bark and Fruit Essential Oil from Premna foetida Linn

  • UMARU, Isaac John;AHMED, Maryam Usman;HABIBU, Bilyaminu;EMOCHONE, Yohanna Roy
    • The Korean Journal of Food & Health Convergence
    • /
    • v.7 no.6
    • /
    • pp.1-8
    • /
    • 2021
  • Premna foetida is a woody plant with short and twisted trunk. P. foetida is a scandent, erect shrub or small tree, thorny on the trunk and large branches. Leaves are opposite or whorled and entire or serrate. Premna foetida is a wild plant locally known as "Daun Sebuas". P. foetida is used for it nutritive and as traditional treatment. The fruit and leaves of P. foetida are prepared for salad. The study aimed at the hydrodistillation and antioxidant activity of leaves, stem-bark and fruits essential oil from Premna foetida Linn, they were analysed by capillary GC and GC-MS. Ninety eight compounds representing 81.68±0.02, 37.31±0.05 and 93.45±0.03 of the isolates of leaves, stem-bark and fruits respectively were identified, the most abundant were α -Duprezianene (77.27±0.03, leaves, α-Gurjunene (36.06±0.05) fruits and Hinesol acetate (77.19±0.03) stem-bark. Components among which sesquiterpenoids dominated. The total volatiles were assayed for antioxidant potentials using 2, 2-diphenyl-1-picrylhydrazyl (DPPH). The total volatiles showed strong activity with IC50 of 11.74±0.82㎍/ml, 9.63±0.34 ㎍/ml and 49.73±1.12 ㎍/ml for leaves fruits and stem-bark respectively.