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Fitoterapia
Inverni della Beffa SpA
Fitoterapia

Inverni della Beffa SpA

0367-326X

Fitoterapia/Journal FitoterapiaSCIISTP
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    Euphzycopias A-I, macrocyclic diterpenes with NLRP3 inflammasome inhibitory activity from Euphorbia helioscopia L.

    Zhang, YuXiong, FengZhang, Jing-JingYue, Chen-Fang...
    12页
    查看更多>>摘要：A phytochemical investigation was conducted on Euphorbia helioscopia, resulting in the isolation of thirteen compounds, including nine undescribed diterpenoids, Euphzycopias A - I (1-9), of which the skeletons of compounds 1-4 were found in E. helioscopia L. Compounds 1-3 had 5/7/6 cyclic systems, while compound 4 had a 4/11 polycyclic system with a 4,7-cyclic ether between C-4 and C-7. The anti-inflammasome test using the isolated compounds (1-6, 8-13) showed that the diterpenes from E. helioscopia L. had a strong inhibitory effect on NLRP3 inflammasomes with IC50 values of 3.34-14.92 mu M.
      原文链接:
    • NSTL
    • Elsevier

    Monoterpene indole alkaloids from Melodinus cochinchinensis (Lour.) Merr.

    Wang, Xiao-FengWei, Ren-JieFang, Qiang-QiangHe, Wan-Ying...
    4页
    查看更多>>摘要：Melodicochinines A - D (1-4), four new monoterpene indole alkaloids (MIAs), along with 21 known ones, were isolated from the stems and twigs of Melodinus cochinchinensis. Their structures were elucidated on the basis of extensive spectroscopic analysis. A ubiquitin-rhodamine 110 assay showed that 11-methyloxytabersonine had potential inhibitory effect against ubiquitin-specific protease 7 (USP7).
      原文链接:
    • NSTL
    • Elsevier

    Bioactive lipids from the fruits of Solanum xanthocarpum and their anti-inflammatory activities

    Xu, Zhen-PengAlgradi, Adnan MohammedLiu, YanWang, Si-Yi...
    9页
    查看更多>>摘要：Bioactive lipids widely found in daily consumed plants and animals are essential or beneficial to health and some of them are important physiological regulators in the human body. In our current investigation, 18 bioactive lipids (1-18), including 8 sphingolipids (1-8), 7 oxylipins (9-15), 3 phenolic lipids (16-18) were isolated from the fruits of Solanum xanthocarpum. And compounds 1, 9, 15, 16, and 18 were new lipids. In this study, homologues (4-8, 16, and 17) and configuration isomers (2 and 3) of bioactive lipids were separated, and NMR combined with MS/MS2 was an effective method to identify these compounds. These findings provided the reference for the separation and structural identification of bioactive lipids. The anti-inflammatory activities of all isolated lipids were evaluated by their inhibition of the NO release of LPS-induced RAW 264.7 cells. Aglycone components of sphingolipids, oxylipids with free carboxylic acid groups, phenylpmpionic acid-fatty acid glyceride polymer exhibited significant anti-inflammatory activities. Further analysis by molecular docking revealed the interactions of bioactive compounds with the iNOS protein.
      原文链接:
    • NSTL
    • Elsevier

    Leonurine hydrochloride-a new drug for the treatment of menopausal syndrome: Synthesis, estrogen-like effects and pharmacokinetics

    Wei, JieZhou, YaxinChen, GuoguangRen, Lili...
    10页
    查看更多>>摘要：This research aimed to investigate the estrogen-like effects of Leonurine hydrochloride (Leo). First, we developed a total synthesis of Leo from 3,4,5-trimethoxy-benzoic acid and the structure was confirmed through H-1 NMR and mass spectrometry (MS). Then the estrogenic activity of Leo in vitro and in vivo was studied. The proliferation and proliferation inhibitory effects of Leo on MCF-7 cells and MDA-MB-231 cells indicate that Leo exerts estrogen-like effects through estrogen receptor alpha (ER alpha) and estrogen receptor beta((RER beta) in vitro. Uterotrophic assay in juvenile mice showed that Leo has an estrogen-like effect in vivo, as it can promote the development of the uterus of juvenile mice, increase its uterine coefficient and the size of the uterine cavity, as well as the increased number of uterine glands and the thickened uterine wall. For further research, cyclophosphamide (CTX) was used to establish a mouse model of ovarian function decline. Through this model, we found that Leo can restore the estrous cycle of mice, increase the number of primordial and primary follicles in the ovaries of mice, and regulate the disordered hypothalamic-pituitary-ovarian (HPOA) axis of mice. Finally, the pharmacokinetics of Leo was studied and oral bioavailability of Leo was calculated to be 2.21%. Leo was synthesized and the estrogen-like effect in vitro and in vivo was confirmed as well as its pharmacokinetics.
      原文链接:
    • NSTL
    • Elsevier

    Anti-inflammatory sesquiterpenoids from the heartwood of Juniperus formosana Hayata

    Liu, ShunzhiZhang, JianyuHe, FengmingFu, Wenhao...
    9页
    查看更多>>摘要：Juniperus formosana Hayata (J. formosana) is a commom needlebush cultivar growing in China. Six new compounds (1-6), including four cadinene sesquiterpenoids (1-4), one abietane diterpenoid (5), and one (3-naphthol derivative (6), along with 18 known compounds (7-24) were isolated and identified through phytochemical investigation on the heartwood of J. formosana. The structures of these compounds were fully elucidated by their 1D and 2D NMR, HR-ESI-MS, UV, and IR spectral data analyses. The absolute configurations of compounds 1,3, and 5 were confirmed by experimental and calculated electronic circular dichmism (ECD) data. Moreover, X-ray crystallographic analysis was carried out to characterize the structure of compound 4. The inhibitory effects on the nitric oxide (NO) production of all the isolated compounds were initially examined in RAW264.7 macrophages induced by lipopolysaccharide (LPS). The results showed that compounds 3 and 12 possessed significant inhibitory potency on NO generation with IC50 values of 3.41 mu M and 6.15 mu M among the new and known compounds, respectively. The expressions of IL-1 beta, IL-6, and TNF-alpha were measured in LPS-stimulated RAW264.7 cells to evaluate the anti-inflammatory effects of compounds 1-24. Compounds 1-6 and 9-12 exhibited potent anti-inflammatory effects. Additionally, the expressions of p38, Erk, and I kappa B alpha proteins were further determined to explore the anti-inflammatory mechanism of the most potent compounds 3 and 12. Overall, our findings indicate the potential of J. formosana for developing medicine candidates as the treatments of inflammation.
      原文链接:
    • NSTL
    • Elsevier

    Structural characterization of the carbohydrate and protein part of arabinogalactan protein from Basella alba stem and antiadhesive activity of polysaccharides from B. alba against Helicobacter pylori

    Nguyen, H. T.Herrmann, F.Koenig, S.Goycoolea, F. M....
    10页
    查看更多>>摘要：Background: Increasing drug resistance of Helicobacter pylori has highlighted the search for natural compounds with antiadhesive properties, interrupting the adhesion of H. pylori to stomach epithelia. Basella alba, a plant widely used in Asian traditional medicine, was investigated for its antiadhesive activity against H. pylori. Methods: B. alba extract FE was prepared by aqueous extraction. Polysaccharides were isolated from FE by ethanol precipitation and arabinogalactan-protein (AGP) was isolated with Yariv reagent. Carbohydrate analyses was performed by standard methods and sequence analysis of the protein part of AGP by LC-MS. In vitro adhesion assay of fluorescent-labelled H. pylori J99 to human AGS cells was performed by flow cytometric analysis. Results: Raw polysaccharides (BA1) were isolated and 9% of BA1 were identified as AGP (53.1% neutral carbohydrates L-arabinose, D-galactose, rhamnose, 5.4% galacturonic acid, 41.5% protein). After deglycosylation of AGP, the protein part (two bands at 15 and 25 kDa in tricine SDS-PAGE) was shown to contain peptides like ribulose-bisphosphate-carboxylase-large-chain. Histological localization within the stem tissue of B. alba revealed that AGP was mainly located at the procambium ring. Functional assays indicated that neither FE nor BA1 had significant influence on viability of AGS cells or on H. pylori. FE inhibited the bacterial adhesion of H. pylori to AGS cells in a dose dependent manner. Best anti-adhesive effect of similar to 67% was observed with BA1 at 2 mg/mL. Conclusion: The data obtained from this study characterize in part the mucilage and isolated polysaccharides of B. alba. As the polysaccharides interact with the bacterial adhesion, a potential uses a supplemental antiadhesive entity against the recurrence of H. pylori after eradication therapy may be discussed.
      原文链接:
    • NSTL
    • Elsevier

    New anti-influenza A viral norsesquiterpenoids isolated from feces-residing Streptomyces sp

    Lu, ShengshengXie, XiHu, JiananLin, Haixing...
    8页
    查看更多>>摘要：Three novel norsesquiterpenoids, (2R,45,8aR)-8,8a,1,2,3,4-hexahydro-2-hydroxy-4,8a-dimethyl-2(2H)-naphthalenone (1), (15,35,45,4aS,8aR)-4,8a-dimethyloctahydronaphthalene-1,3,4a(3H)-triol(2), (4S,4aS,8aS)-octahydro-4a-hydroxy-4, 8a-dimethyl-1(2H)-naphthalenone (3), as well as six other known analogues (4-9), were isolated from the culture broth of Streptomyces sp. XM17, an actinobacterial strain inhabiting the fresh feces of the giant panda Ailuropoda melanoleuca. The chemical structures of 1-3 were elucidated comprehensively by NMR spectroscopic and MS analyses, furthermore, the stereochemical configurations were resolved by NOESY experiments, along with ECD spectral and single-crystal X-ray crystallographic analyses. These compounds were then tested for their antiviral activities using the "pretreatment of virus" approach, which showed that most of these compounds were potent in inhibiting the entry of influenza A virus, with IC50 values ranging from 5 to 49 nM and selectivity indices all above 500.
      原文链接:
    • NSTL
    • Elsevier

    Erianin suppresses proliferation and migration of cancer cells in a pyruvate carboxylase-dependent manner

    Wang, SiyuGuo, YuanbiaoHuang, XinheHong, Jing...
    10页
    查看更多>>摘要：Erianin is a natural small molecule dibenzyl compound extracted from Dendrobium officinale or Dendrobium chrysotoxum. Studies show erianin has many pharmacological functions such as antioxidant, antibacterial, antiviral, improving diabetic nephmpathy, relaxing bronchial smooth muscle and anti-tumor. However, the erianin-mediated molecular mechanism is elusive, and the target protein of erianin is not clear yet. Here, we screened and identified that the target protein of erianin in human hepatoma HepG2 cells is human pyruvate carboxylase, and explored the anti-tumor signal pathway regulated by erianin in several cell lines. Firstly, the interaction between human pyruvate carboxylase and erianin was studied by bioinformatics and biochemical methods. Secondly, in vitro, erianin can specifically inhibit the activity of human pyruvate carboxylase, and the purified human pyruvate carboxylase can specifically bind to the activity probe of erianin. Thirdly, human pyruvate carboxylase is highly expressed in a variety of malignant tumors, and the inhibitory effect of erianin on tumor cells is positively correlated with the expression of human pyruvate carboxylase, and erianin can selectively inhibit the activity of pyruvate carboxylase. Finally, erianin can regulate the pyruvate carboxylasemediated Wnt/ beta- Catenin pathway. All of which provide important data for the further study of the anticancer mechanism of erianin, and lay a solid foundation for the further development and utilization of erianin.
      原文链接:
    • NSTL
    • Elsevier

    The triterpenoids and sesquiterpenoids from the plant of Agrimonia pilosa

    Zhang, JiaYang, Ya-NanFeng, Zi-MingYuan, Xiang...
    5页
    查看更多>>摘要：A phytochemistry of the whole plant of Agrimonia pilosa led to the discovery of two new nortriterpenoids, agrimonorterpenes A and B (1 and 2), together with one known triterpenoid fupenzic acid (3) and seven known sesquiterpenoids (4-10). The new structures were determined as 19 alpha-hydroxy-2-oxo-nor-A (3)-urs-11,12-dien-28-oic acid (1) and 2, 19 beta-dihydroxy-3-oxo-23-noroleana-1, 4, 12-trien-28-oic acid (2) by the spectroscopic data of UV, IR, HR-ESI-MS, and NMR. Notably, the structure of 1 possessed a rare five-membered A- ring. And this is the first time to discover the sesquiterpenoids (4-10) from A. pilosa. Compound 3 displayed the selective cytotoxicity against HCT116, BGC823, and HepG2 cell lines with the IC50 values of 16.31 mu M, 21.94 mu M, and 23.40 mu M, respectively.
      原文链接:
    • NSTL
    • Elsevier

    Eurobusones A-D, four antibacterial formyl phloroglucinol meoterpenoids from Eucalyptus robusta

    Liu, RuiLiu, Xiang-YueLi, MinLiu, Juan...
    7页
    查看更多>>摘要：Four antibacterial formyl phloroglucinol memterpenoids (FPMs), eurobusones A-D (1-4), as well as six known analogues (5-10), were isolated from the leaves of Eucalyptus robusta. Their structures were determined by the analysis of spectroscopic data and electron circular dichroism (ECD) calculation, along with the application of Snatzke helicity rules. Among them, compounds 2 and 8-10 showed good activity against Staphylococcus aureus, Pseudomonas aeruginosa and Bacillus subtilis with MIC50 values less than 1.00 mu g/mL.
      原文链接:
    • NSTL
    • Elsevier