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Fitoterapia
Inverni della Beffa SpA
Fitoterapia

Inverni della Beffa SpA

0367-326X

Fitoterapia/Journal FitoterapiaSCIISTP
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    Lignanamides from the stems of Piper hancei maxim. and their anti-inflammatory and cytotoxic activities

    Yang F.Li H.Liang D.Yang Y.-Q....
    6页
    查看更多>>摘要：? 2022 Elsevier B.V.Four new lignanamides, hancamides A ? D (1–4), together with four known analogs (5–8), were isolated from the stems of Piper hancei Maxim. Their structures were determined based on 1D and 2D NMR, IR, UV, and HR-ESIMS spectroscopic analysis as well as by comparison with the reported data. All the isolates exhibited potential inhibitory effects on NO production in LPS-induced BV-2 microglial cells, with IC50 values of 4.26–40.68 μM. Moreover, compounds 2 and 8 displayed moderate cytotoxic activities against MGC-803, HepG2, SKOV-3, T24, and HeLa cells, with IC50 values ranging from 13.57 to 34.20 μM, respectively.
      原文链接:
    • NSTL
    • Elsevier

    Diterpenoids with α-glucosidase inhibitory activities from the fruits of Vitex trifolia Linn

    Djimabi K.Wang R.-Y.Li B.Chen X.-H....
    6页
    查看更多>>摘要：? 2022 Elsevier B.V.Viticis Fructus, known as “Man-jing-zi”, are the fruits of the traditional Chinese medicine Vitex trifolia Linn. and its variant Vitex trifolia Linn. var. simplicifolia. These fruits are used as folk medicines to treat various diseases. Although V. trifolia is useful for treating diabetes, the antidiabetic effect of its purified constituents is still under investigation. The phytochemical investigation on the ethanol extract of the fruits of V. trifolia yielded four new labdane diterpenoids vitetrolins A-D (1–4), together with seven (5–11) known analogs. The structures of these compounds were elucidated by spectroscopy techniques and the absolute configuration of 4 was determined by electronic circular dichroism (ECD) calculations. The isolated diterpenoids were evaluated for their α-glucosidase inhibitory activities. Compounds 5, 6, 8, and 9 exhibited moderate inhibitory activities against α-glucosidase with IC50 values ranging from 44.9 ± 6.1 to 70.5 ± 5.5 μM.
      原文链接:
    • NSTL
    • Elsevier

    Creating diverse glycosides of 2′-hydroxyflavone through microbial glycosylation

    Ren J.Barton C.D.Zhan J.
    9页
    查看更多>>摘要：? 2022 Elsevier B.V.Four new 2′-hydroxyflavone glycosides, namely hydroxyflavone-2′-O-β-D-glucuronide (1), hydroxyflavone-2′-O-α-L-rhamnoside (2), hydroxyflavone-2′-O-β-D-glucoside (3), and hydroxyflavone-2′-O-4″-O-methyl-β-D-glucoside (4), were biosynthesized through microbial glycosylation using Streptomyces coeruleorubidus NRRL B-2569, Streptomyces toxytricini NRRL 15443, Escherichia coli BL21(DE3)/pWZ8, and Beauveria bassiana ATCC 7159, respectively. Compounds 1–4 were structurally characterized through extensive analysis of 1D and 2D NMR spectroscopic data. The water solubility of glycosylated products 1–4 were enhanced by 7 to 15 times compared to the substrate 2′-hydroxyflavone. Moreover, antioxidant assays revealed that compounds 1 and 2 exhibited stronger 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity than the substrate, decreasing the logIC50 by 68.7% and 80.7%, respectively. Therefore, this research provides several effective biocatalysts that can be used for structural modification of flavonoids for enhanced water solubility and biological activities.
      原文链接:
    • NSTL
    • Elsevier

    Anti-inflammatory abietanes diterpenes and triterpenoids isolated from Clinopodium polycephalum

    Liu Y.Song H.Xu J.Bi G....
    7页
    查看更多>>摘要：? 2022 Elsevier B.V.Two previously undescribed diterpenes (1 and 2), as well as one curious triterpenoid were isolated from Clinopodium polycephalum, a medicinal plant distributed in southwestern and eastern China. Their structures were elucidated using MS analyses, UV spectrum, and extensive 2D-homo and heteronuclear NMR data interpretations. Among them, 1 had an unusual skeletal characteristic produced by a rare methyl migration pathway. All monomer compounds exhibited inhibitory effects on NO production in LPS-induced RAW 264.7 cells without affecting cell viabilities, which were comparable to that of positive control.
      原文链接:
    • NSTL
    • Elsevier

    Vlasouliodes A-D, four new C30 dimeric sesquiterpenes exhibiting potential inhibition of MCF-7 cells from Vladimiria souliei

    Wu Z.-L.Li H.-L.Zhang W.-D.Li J.-Y....
    9页
    查看更多>>摘要：? 2022 Elsevier B.V.As our ongoing interest to search bioactive dimeric sesquiterpenes from the genus Vladimiria (Asteraceae), the plant of Vladimiria souliei was studied. Based on the repetitive chromatographic fractionation, a chemical investigation on the roots of Vladimiria souliei led to the isolation and the identification of four previously undescribed sesquiterpene dimers, vlasouliodes A-D (1–4). Their chemical structures were elucidated by comprehensive analysis of spectroscopic data, including HRESIMS, 1D and 2D NMR spectroscopic data. The absolute configurations of them were unambiguously established by the experimental and calculated ECD data. In the in vitro biological activity evaluation, 1 and 3 displayed pronounced inhibitory activity against human breast adenocarcinoma cell lines (MCF-7) with IC50 values of 17.12 ± 0.42 μM and 13.12 ± 0.10 μM, respectively. Additionally, treatment with 1 and 3 induced cell apoptosis in MCF-7 cells, down-regulated the expression of Caspase-3 and up-regulated the expression of Cleaved-caspase-3.
      原文链接:
    • NSTL
    • Elsevier

    Chemical constituents from the bulbs of Lilium davidii var. unicolor and anti-insomnia effect

    Zhang H.Niu T.Chang J.Jin L....
    7页
    查看更多>>摘要：? 2022 Elsevier B.V.In this work, twenty-five water-soluble constituents were isolated from the bulbs of Lilium davidii var. unicolor, including two new compounds termed liliumtides A and B (1–2), and seventeen known compounds (3–4, 6–13, 15, 17, 21–25) isolated from the genus of Lilium for the first time. Their structures were established using high-resolution electrospray ionization mass spectroscopy and 1D and 2D nuclear magnetic resonance data. To confirm furtherly the absolute configuration of liliumtide A, and to accumulate enough sample to study the anti-insomnia effect, a total synthesis for liliumtide A was achieved by four steps. The pentobarbital-induced sleeping time test showed that compared with the blank control group, the liliumtide A decreased sleep latency and significantly increased the sleep time. These results suggested that liliumtide A could be investigated as a natural anti-insomnia lead compound in the pharmaceutical and food industries.
      原文链接:
    • NSTL
    • Elsevier

    Acylated sucroses and butenolide analog from the leaves of Tripterygium wilfordii Hook. f. and their potential anti-tyrosinase effects

    Ai Y.-F.Dong S.-H.Huang X.-X.Song S.-J....
    7页
    查看更多>>摘要：? 2022 Elsevier B.V.Three undescribed acylated sucroses (1–3), one undescribed butenolide analog (4) along with three known compounds (5–7) were isolated from the aqueous EtOH extract of the dried leaves of Tripterygium wilfordii. Their structures were elucidated on the basis of spectroscopic analyses, electron circular dichroism (ECD) techniques, and saccharide hydrolysis. All the isolated compounds were tested for their anti-tyrosinase effects. Among them, 6 exhibited similar inhibitory effects on tyrosinase with IC50 values of 0.073 mM comparing to arbutin. Additionally, the possible mechanism of the interaction between 6 and the active site of tyrosinase was explored by molecular docking.
      原文链接:
    • NSTL
    • Elsevier

    Bioactive polycyclic polyprenylated acylphloroglucinols from Hypericum scabrum

    Zhou Z.-B.Mou P.-Y.Zeng H.Wei X....
    6页
    查看更多>>摘要：? 2022Eighteen polycyclic polyprenylated acylphloroglucinols were isolated from the whole plant of Hypericum scabrum Linn., including six new compounds (1–6). Their structures were elucidated by comprehensive spectroscopic analyses. The evaluation of their cytotoxic activities was carried out against SMMC-7721 and MGC-803 cell lines. We found that most tested compounds exhibited moderate cytotoxic activities against SMMC-7721 cell line except for 11 and 12, while compounds 1, 5–7, 13 and 16 also showed cytotoxic activities on MGC-803 cells. Besides, Bacillus subtilis, MRSA and MDPRA were also used to test inhibitory activity of these compounds. Our results showed that only compounds 12 and 13 presented weak inhibitory activity against Bacillus subtilis, while compounds 7, 13 and 14 also inhibited MRSA weakly.
      原文链接:
    • NSTL
    • Elsevier

    Design, synthesis and cytotoxic activity studies of alkyne linked analogues of Nimbolide

    Manga B.Venkateswara Rao B.Ramalingam V.Suresh Babu K....
    9页
    查看更多>>摘要：? 2022 Elsevier B.V.A series of novel nimbolide derivatives bearing various substitutions on 28th position was designed and synthesized using Sonogashira (2a-2p) and Glaser coupling (3a-3e) reactions. The synthesized derivatives were assessed for in vitro cytotoxic activity against four different human cancer cell lines (A549 cells, MCF-7 cells, MDA-MB-231 cells, and HCT15 cells) and normal cell line (HEK cells) using MTT assay. Among the screened derivatives, the compound 3a showed potent activity against A549 cells with IC50 value of 0.23 μM as comparing with parent molecule 1 (1.48 μM) and the standard drug doxorubicin (0.82 μM). As well, the flow cytometry analysis confirmed that the compounds 1 and 3a arrest the cell cycle progress at S phase and induce the early apoptosis in the lung cancer. The qRT-PCR analysis revealed that the compounds 1 and 3a downregulate the BcL2 expression and upregulates the Bax gene expression level in A549 cells. The strong binding affinity of the compounds 1 and 3a with BcL2 was also confirmed using molecular docking analysis. Together, the results suggested that the compound 3a is a promising anticancer agent against lung cancer is deserved for further investigation.
      原文链接:
    • NSTL
    • Elsevier

    Schisandraceae triterpenoids: A review of phytochemistry, bioactivities and synthesis

    Zhang Y.-Q.Liu Y.Zhang Z.-P.Wu D.-D....
    26页
    查看更多>>摘要：? 2022Ethnopharmacological relevance: Plants of the Schisandraceae family have a rich and medicinal history dating back to ancient times. Many of them are used as folk medicine in the treatment of chronic coughs, asthma, nocturnal emission, spontaneous sweating, night sweats, palpitation, insomnia and thirst. Aim of the review: The current review is carried out on triterpenoids from the Schisandraceae family, aiming to comprehensively summarize their phytochemistry, pharmacology and synthesis and provide new insights to the chemical and pharmacological study and rational utilization on medicinal plants of the Schisandarceae family. Materials and methods: The information was searched from the scientific literature published from June 2014 to November 2021 on the online databases (including PubMed, CNKI, Elsevier, SciFinder and Web of Science) and other bibliography (e.g. the Chinese Pharmacopoeia, 2020 edition, Chinese herbal books). The scientific literature related to phytochemistry, pharmacology, biological activites and synthesis of triterpenoids from the Schisandraceae family was gathered. Results: From June 2014 to November 2021, there were approximately 211 novel triterpenoids isolated and identified from 18 species of the Schisandraceae family. These compounds exhibit tremendous diversity in their structures, and some of them possess promising pharmacological activities, including anti-viral, anti-tumor, anti-inflammatory, hepatoprotective, immunosuppressive activities and neuroprotective effects. In the attempt to synthesize active compounds, the total synthesis of 13 schinortriterpenoids belonging to five structural types was successfully completed. Conclusions: Studies of triterpenoids from the Schisandraceae family are well documented in this review (from June 2014 to November 2021), and it is also well acknowledged that they are valuable resources with medicinal efficacy. However, relevant pharmacological studies are limited to in vitro tests, and data from in vivo studies and toxicology are lacking or unavailable. Fortunately, there is growing interest in the synthesis of active compounds, which should serve as an approach for accessing active compounds to develop in vivo or toxicity studies, with a view of clarifying their in vitro and vivo mechanisms for more effective and safe natural drugs.
      原文链接:
    • NSTL
    • Elsevier