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Fitoterapia
Inverni della Beffa SpA
Fitoterapia

Inverni della Beffa SpA

0367-326X

Fitoterapia/Journal FitoterapiaSCIISTP
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    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

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

    Wang, JinWei, JieZhou, YaxinChen, Guoguang...
    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 1H 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((ER 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

    Rare cytochalasans isolated from the mangrove endophytic fungus Xylaria arbuscula

    Su, Jian-HuiWang, Ming-QiangLi, Yan-ZhenLin, Yin-Si...
    7页
    查看更多>>摘要：Four new cytochalasans, arbuschalasins A-D (1-4), along with thirteen known analogues (5-17), were isolated from the solid rice medium of endophytic fungus Xylaria arbuscula. Arbuschalasins A-B feature a rare 5/6/6/6 fused ring system while arbuschalasin D was characterized as the first example of natural cytochalasans that possesses a 5/5/11 fused scaffold. The structures of 1-4 were assigned by spectroscopic data, with their absolute structures being determined by electronic circular dichroism (ECD) calculations. All of the isolates were evaluated against the human colorectal adenocarcinoma cell lines (HCT15). Compounds 6 and 7 showed significant inhibitory effects (IC50 values were 13.5 and 13.4 mu M, respectively), being more active than those of the positive control, fluorouracil (103.1 mu M).
      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

    Petasin is the main component responsible for the anti-adipogenic effect of Petasites japonicus

    Uesugi, ShotaHakozaki, MayukaKanno, YukoShiraishi, Akiko...
    8页
    查看更多>>摘要：Petasites japonicus is one of the most popular edible wild plants in Japan. Many biological effects of P. japonicus have been reported, including anti-allergy, anti-inflammation, and anticancer effects. Although its anti-obesity effect has been reported in several studies, the most important component responsible for this activity has not been fully elucidated. On screening the components that suppress adipocyte differentiation in 3T3-F442A cells, we found that the extract of the flower buds of P. japonicus has anti-adipogenic effect. Among the known major components of P. japonicus, petasin exhibited a potent anti-adipogenic effect at an IC50 value of 0.95 mu M. Quantitative analysis revealed that the active component responsible for most of the anti-adipogenic effects of P. japonicus extract is petasin. Petasin suppressed the expression of markers of mature adipocytes (PPAR gamma, C/EBP alpha, and aP2). However, as isopetasin and petasol, analogs of petasin, did not exhibit these effects, it indicates that a double bond at the C11-C12 position and an angeloyl ester moiety were essential for the activity. Petasin affected the late stage of adipocyte differentiation and inhibited the expression of lipid synthesis factors (ACC1, FAS, and SCD1). Additionally, it was revealed that petasin could be efficiently extracted using hexane with minimal amount of pyrrolizidine alkaloids, the toxic components. These findings indicate that P. japonicus extract containing petasin could be a promising food material for the prevention of obesity.
      原文链接:
    • NSTL
    • Elsevier

    New ent-Kaurane and cleistanthane diterpenoids with potential cytotoxicity from Phyllanthus acidus (L.) Skeels

    Xin, YingXu, JiaLv, Jun-JiangZhu, Hong-Tao...
    5页
    查看更多>>摘要：Six diterpenoids including three ent-kauranes (1-2, 4) and three cleistanthanes (3, 5-6) were isolated from the roots and stems of Phyllanthus acidus (L.) Skeels. Of them, (165)-ent-16,17,18-tri-hydroxy-19-nor-kaur-4-en-3-one (1), phyllanthone A (2), and 6-hydroxycleistanthol (3) are new compounds, while the ent-kaurane diterpenoids were reported from the titled plant for the first time. Their structures were elucidated on the basis of the extensive spectroscopic analyses. Compounds 2 and 4-6 displayed cytotoxic potential with IC50 values ranging from 1.96 to 29.15 mu M. They also showed moderate anti-inflammatory activities (IC50 = 6.30-12.05 mu M). Particularly, the new ent-kaurane 2 displayed cytotoxic potential against HL-60 (IC50 = 2.00 mu M) and MCF-7 (IC50 = 3.55 mu M) cells, and anti-inflammatory activity (IC50 = 6.47 mu M).
      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

    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

    Myrsinane-type diterpenes from Euphorbia gedrosiaca with cell growth inhibitory activity and apoptotic effects on melanoma cancer cells

    Yazdiniapour, ZeinabMirian, MinaZolfaghari, BehzadMehdifar, Pegah...
    8页
    查看更多>>摘要：Phytochemical analysis of Euphorbia gedrosiaca Rech.f., Aellen & Esfand., an Iranian endemic spurge, afforded the isolation of four myrsinane types diterpene polyesters. Two new compounds (1-2) were based on a myrsinane skeleton while the others (3-4) were known diterpenes based on a cyclomyrsinane backbone. Their chemical structures were elucidated by spectroscopic methods, including 1D and 2D NMR and HRESIMS. The isolated compounds were tested to evaluate their cell growth inhibitory activity and apoptotic effects on melanoma cell lines, B16F10 and A375. The IC50 values for compounds 1-4 were 58.45, 55.43, 86.52 and 82.27 mu M, respectively, on B16F10, and 20.66, 21.88, 36.21 and 39.87 mu M, respectively, on A375 cells. Non-treated cells were used as negative control (100% cell growth) and 5 nM Taxol were considered as a positive control.
      原文链接:
    • NSTL
    • Elsevier

    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