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Taylor & Francis Health Sciences
Natural product research

Taylor & Francis Health Sciences

1478-6419

Natural product research/Journal Natural product researchSCIISTP
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    Multi-layered antimicrobial synergism of (E)-caryophyllene with minor compounds, tecleanatalensine B and normelicopine, from the leaves of Vepris gossweileri (I. Verd.) Mziray

    Moses K.,LangatYisau,MayowaNicholas,SadgroveMohammed,Danyaal...
    11页
    查看更多>>摘要：Abstract An aromatic alkaloid-rich ‘absolute’ extract from Vepris gossweileri inhibited Saccharomyces cerevisiae at 62.5?μg.mL?1 and Bacillus subtilis at 500?μg.mL?1 . A loss of activity upon fractionation indicated possible synergistic effects. Three new acridones, gossweicridone A (3), B (4) and C (5) and known compounds from the extract were inactive. Combinations of compounds showed that a sub-fraction containing mixtures of minor compounds with (Ε)-caryophyllene augmented activity by 50-folds, with MIC values of 19.6?μg.mL?1 for S. cerevisiae and 375.0?μg.mL?1 for B. subtilis, demonstrating potent ΣFIC values of 0.02 and 0.375 respectively. From the active sub-fraction, three compounds were assigned as tecleanatalensine B, 13S-hydroxy-9Z,11E,15E-octadecatrienoic acid and normelicopine. In combination with (Ε)-caryophyllene they separately demonstrated MIC values of 18?μg.mL?1, 34?μg.mL?1 and 16?μg.mL?1 , respectively against S. cerevisiae. The synergistic combinations were more potent with addition of pheophytin A, suggesting that the synergistic antifungal effect of the extract is multi-layered.
      原文链接:
    • NSTL
    • Taylor & Francis

    New piericidin derivatives from the marine-derived streptomyces sp. SCSIO 40063 with cytotoxic activity

    Jing,PengQingbo,ZhangXiaodong,JiangLiang,Ma...
    7页
    查看更多>>摘要：Abstract Two new piericidins A5 (1) and G1 (2), a previously synthesized piericidin G2 (3), and two known piericidins A1 (4) and A2 (5) were isolated from the marine-derived Streptomyces sp. SCSIO 40063. The structures of 1-5 were elucidated by HRESIMS, 1?D, 2?D NMR data analyses and comparisons with the known compounds. Compound 2 showed moderate cytotoxicities against four human tumor cell lines SF-268, MCF-7, HepG2 and A549 with IC50 values between 10.0 and 12.7?μM.
      原文链接:
    • NSTL
    • Taylor & Francis

    Two antibacterial spiro compounds from the roots of Artemisia pallens wall: evidence from molecular docking

    Varsha S.,HonmoreArun D.,NatuVijay M.,KhedkarManisha A.,Arkile...
    8页
    查看更多>>摘要：Abstract Bioassay-guided isolation from acetone extract of the roots of Artemisia pallens Wall yielded two spiro compounds (1 and 2). The structures of these compounds were determined on the basis of spectroscopic techniques such as IR, MS, 1?D and 2?D- NMR. The acetone extract, fractions and the isolated two compounds were investigated for their antibacterial activity against two gram negative (E. coli, P. aeruginosa) and two gram positive (S. aureus, B. subtilis) bacterial strains. Compound (2) showed the best spectra of activity with IC50 and MIC values between 2.48–3.08 and 12.78???21.77?μM and Compound (1) with 2.57–3.69 and 38.17???80.57?μM, respectively, for the four bacterial strains, whereas inactive against Mycobacterium tuberculosis. Molecular docking study could further help in understanding the various interactions between these compounds and DNA gyrase active site in detail and thereby could provide valuable insight into the mechanism of action.
      原文链接:
    • NSTL
    • Taylor & Francis

    Two new cytotoxic cycloartane triterpenoids from Aphanamixis polystachya (Wall.) R. N. Parker

    Bi-juan,YangXiao-jiang,HaoDuo-zhi,ChenYi-ting,Wang...
    6页
    查看更多>>摘要：Abstract Two new cycloartane triterpenoids, (24?R)-cycloartane-3β,24,25,30-tetrol (1) and (24?R)-24,25,30-trihydroxy-9,19-cycloartane-3-one (2), along with three known compounds (3-5) were isolated from leaves and twigs of Aphanamixis polystachya. The new compounds were elucidated based on comprehensive spectroscopic analysis, including 1?D, 2?D NMR and HREIMS. The in?vitro cytotoxic activities evaluation of five human cancer cell lines revealed that compound 1 exhibited cytotoxic activity on all of tested human cancer cell lines, while compound 2 only had specific activity on SMMC-7721 cell line.
      原文链接:
    • NSTL
    • Taylor & Francis

    Salprzesides A and B: two novel icetexane diterpenes with antiangiogenic activity from Salvia przewalskii Maxim

    Bei-Ming,QiuPan,WangJie,Li
    7页
    查看更多>>摘要：Abstract Two novel icetexane diterpenes were isolated from Salvia przewalskii Maxim., namely Salprzesides A (1) and B (2), together with two known abietane-type diterpenes respectively identified as sahandinone (3) and miltirone (4). The structures of isolated compounds were determined by UV, IR, HR-ESI-MS, 1D and 2D NMR analysis. The in vitro antiangiogenic activities of compounds 1–4 were studied against human umbilical vascular endothelial cells (HUVECs). The IC50 values of compounds 1–4 ranged from 4.22?±?1.07 to 39.31?±?2.17?μM against HUVECs.
      原文链接:
    • NSTL
    • Taylor & Francis

    Non-ulcerogenic pyrazolyl 2-hydroxychalcones and pyrazolylpyrazolines derived from naturally existing furochromone (khellin): semi-synthesis, docking study and anti-inflammatory activity

    Fatma Abd El-Fattah,RagabYassin Mohammed,NissanM. Alaraby,SalemMamdouh Moawad,Ali...
    9页
    查看更多>>摘要：Abstract Novel pyrazolyl 2-hydroxychalcone derivatives 3a–e and pyrazolylpyrazoline derivatives 4a–e and 5a–j derived from the naturally existing furochromone (Khellin) were synthesized and evaluated for their in?vivo anti-inflammatory activity. Most of the synthesized compounds showed better or comparable activity to that of Diclofenac as reference drug. Twelve compounds were evaluated for their ulcerogenic potential and exhibited no ulcerogenic effect. In addition compounds 3c, 5c and 5h as examples showed PGE2 inhibition % 88.86, 65.87 and 44.06, respectively and TNFα inhibition % 48.62, 31.11 and 16.02, respectively in rat serum samples. Compounds 3c, 5c, 5h and Celecoxib were subjected to in?vitro COX-1 and COX-2 inhibition assay, showed selectivity index 45.04, 102.04, 131.58 and 185.18, respectively. The computational finding supported those of in?vitro, where the pyrazolylpyrazolines interacted with the COX-2 enzyme in a similar orientation to that of Celecoxib, while chlacones were found to exhibit similar orientation to that of Diclofenac.
      原文链接:
    • NSTL
    • Taylor & Francis

    A hederagenin-type triterpene saponin, sumbulianoside a from Cephalaria sumbuliana and its potent immunomodulatory activity against seasonal flu virus H3N2

    Huseyin,AbaciGulsah,AkagacAyse,NalbantsoyNazli Boke,Sarikahya...
    9页
    查看更多>>摘要：Abstract A new hederagenin-type triterpene saponin; hederagenin 28-O-β-D-galactopyranosyl-(1→6)-β-D-glucopyranosyl ester named sumbulianoside A (1), together with twelve known saponins were isolated from the n-butanol extract of Cephalaria sumbuliana (Caprifoliaceae) from which, one known saponin, dipsacus saponin A (2) was isolated, for the first time from Cephalaria species. The structures of the isolated compounds were elucidated by 1?D and 2?D NMR and HRESIMS analyses. Cytotoxic activities were investigated on A549, Hela, PANC1, SHSY5Y cells and non-cancerous cell HEK293 by MTT method and immunomodulatory activities were evaluated against activated H3N2 seasonal virus in whole blood by measuring IL-4, IFN-γ, IL-1β cytokine level with ELISA. According to the cytotoxicity results, compounds 1 and 2 did not possess significant cytotoxicity, while only compound 2 induced significant IL-4 production (** p<.001) against H3N2 showing a possible Th2 response and antibody production. All compounds had no effect on cytokine release (p?>?0.5).
      原文链接:
    • NSTL
    • Taylor & Francis

    Six new triterpenoids from the root of Potentilla reptans and their cardioprotective effects in silico

    Ayesheh,EnayatiAref,SalehiMostafa,AlilouHermann,Stuppner...
    9页
    查看更多>>摘要：Abstract Tormentic acid ester glucosides derivatives (1, 2 and 4), 3-oxoursane ester glycoside (3) and 11-methoxy-ursane ester glycosides (5, 6) as six new triterpenoids, along with catechin were isolated from the ethyl acetate fraction of Potentilla reptans root (Et) methanolic extract. The structures of the compounds were elucidated by 1D, 2D NMR, IR and MS spectroscopy. Additionally, isolated triterpenoid compounds (1–6) and catechin were evaluated for their cardioprotective effects via glycogen synthase kinase 3β (GSK-3β) and glucocorticoid regulated kinase-1 (SGK1) protein kinase inhibition by Molecular Docking. Compound 1 and catechin (compound 7) exhibited significant inhibitory effects against GSK-3β and SGK1 protein kinases with a binding energy value ?9.1 and ?8.8?kcal/mol, respectively. Hence, Et can be a suitable natural candidate to protect cardiomyocytes injury.
      原文链接:
    • NSTL
    • Taylor & Francis

    Nitric oxide production inhibitory activity of clerodane diterpenes from Monoon membranifolium

    Isaraporn,PolbupphaVirayu,SuthiphasilpTharakorn,ManeeratRawiwan,Charoensup...
    5页
    查看更多>>摘要：Abstract A new clerodane diterpene, 2β-methoxyhardwickiic acid (1), and four known compounds (2–5) were isolated from the twigs of Monoon membranifolium. The structure of the new compound was determined by extensive spectroscopic methods and ESITOFMS data. The absolute configuration of 1 was established by a comparison of its ECD spectrum and specific rotation with those of related previously reported compounds. All compounds were evaluated for their nitric oxide (NO) production inhibitory activities in RAW264.7 macrophage cells. Compounds 3 and 5 inhibited NO production with IC50 values of 16.1 and 28.9?μM, respectively, which were better than that of standard compound, indomethacin (IC50 = 32.2?μM).
      原文链接:
    • NSTL
    • Taylor & Francis

    Cytotoxic alkaloids from the root of Zanthoxylum paracanthum (mildbr) Kokwaro

    Leonidah Kerubo,OmosaVaderament-A,Nchiozem-NgnitedemJustus,MukaviBrenda,Atieno Okoko...
    8页
    查看更多>>摘要：Abstract Chemical investigation of the root of Zanthoxylum paracanthum afforded 1 new alkamide derivative, (2E,4E)-6-oxo-N-isobutyldeca-2,4-dienamide (1) together with 10 known congeners including one phenolic amide (2), four benzophenanthridines (3???6), three indolonaphthyridines (7???9) and two lignans (10 and 11). Their structures were elucidated by a combination of spectroscopic and spectrometric data. Using resazurin reduction assay, the crude extract (10?μg/mL) and isolates (10?μM) were screened for their cytotoxic activities against the drug-sensitive (CCRF-CEM) leukemia cell line and its multidrug-resistant counterpart (CEM/ADR5000). Compounds 3, 4 and 6 showed cytotoxicity against CCRF-CEM with IC50 values of 2.00?±?0.33, 2.31?±?0.20 and 0.11?±?0.04?μM, respectively. Only compound 6 exhibited strong cytotoxic activity against CEM/ADR5000 with an IC50 value of 2.34?±?0.34?μM in comparison with the standard drug doxorubicin which showed IC50 values of 0.01?±?0.14 (CCRF-CEM) and 26.78?±?3.30?μM (CEM/ADR5000).
      原文链接:
    • NSTL
    • Taylor & Francis