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Fitoterapia
Inverni della Beffa SpA
Fitoterapia

Inverni della Beffa SpA

0367-326X

Fitoterapia/Journal FitoterapiaSCIISTP
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    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

    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

    Anti-TMV effects of seco-pregnane C21 steroidal glycosides isolated from the roots of Cynanchum paniculatum

    Wang D.Peng M.Yan X.Tang L....
    8页
    查看更多>>摘要：? 2022Tobacco mosaic virus (TMV) is known to infect a wide range of plants, resulting in reduced yield and productivity. Novel, effective, and plant-based pesticides are required to protect plants against TMV infection. To identify novel anti-TMV agents from natural sources, we systematically studied the roots of Cynanchum paniculatum and isolated six new seco-pregnane C21 steroidal glycosides, along with 14 known compounds. Their structures were elucidated by comprehensive spectroscopic data analysis. The anti-TMV activity of compounds were screened using the half-leaf method. Biological tests revealed that compounds 1, 2, 5, 9, 10, 15, and 16 displayed significant anti-TMV activities compared with the positive control ningnanmycin. In addition, reverse transcription-polymerase chain reaction (RT-PCR) and western blot analysis confirmed the antiviral activity of these compounds, as evident from reduced TMV coat protein (TMV-CP) gene replication and TMV-CP protein expression. These compounds downregulated the expression of NtHsp70–1 and NtHsp70–261, indicating that these steroidal glycosides possibly inhibit the TMV infection by suppressing the expression of NtHsp70–1 and NtHsp70–061 expression.
      原文链接:
    • NSTL
    • Elsevier

    Novel geranylhydroquinone derived meroterpenoids from the fungus Clitocybe clavipes and their cytotoxic activity

    Hou Y.Li Q.Chen M.Wu H....
    6页
    查看更多>>摘要：? 2022 Elsevier B.V.Three novel geranylhydroquinone derived meroterpenoids, named clavilactones J and K (1–2) and clavipol C (3), were isolated from the basidiomycete Clitocybe clavipes. Their structures were unambiguously identified by extensive spectroscopic data analysis, and the electronic circular dichroism (ECD) calculation, Gauge-Including Atomic Orbitals (GIAO) NMR calculations and Mo2(OAc)4-induced electronic circular dichroism experiments were used to establish their absolute configurations. Compound 1, with two epoxy groups located at the 10-membered carbocycle, is uncommon in the reported meroterpenoids from C. clavipes. All the obtained compounds (1–3) were tested for their cytotoxic activity against human tumor cell line HGC-27 by using the MTT assay. All the compounds exhibited moderate cytotoxic activities against HGC-27 cell with IC50 values ranging from 33.5 to 56.6 μM.
      原文链接:
    • NSTL
    • Elsevier

    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

    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

    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

    Syntheses and high selective cytotoxicity of dehydroabietylamine C-ring nitration derivatives

    Lu W.Xue H.Zhang J.Xu L....
    9页
    查看更多>>摘要：© 2022 Elsevier B.V.To find more effective anticancer agents, a series of novel dehydroabietylamine (DA) derivatives were synthesized, focusing on C-ring nitro modifications and C-18 imide introduction. Their cytotoxic activities against human tumor cell line HeLa (cervix), MCF-7 (breast), A549 (lung), HepG2 (liver), and nonmalignant cell line HUVEC (umbilical vein) in vitro were screened. The C-18 imide heterocyclic compounds 1, 2, and C-ring 14-nitro substituted 14 exhibited moderate to good cytotoxic activities and significant selectivity towards malignant cell lines. More importantly, they were significantly less cytotoxic to nonmalignant cells (HUVEC) than the parent compound and positive control doxorubicin hydrochloride (DOX). Meantime the mechanism of cytotoxicity of DA derivatives was studied. Annexin V-FITC/PI double-staining analysis suggested that cytotoxicity of compounds 2 and 14 was associated with early apoptosis induction. The interaction between compounds and DNA (herring sperm DNA) was studied using absorption spectral analysis and ethidium bromide (EB) fluorescence displacement experiments, the results exhibited that the binding of the compound to DNA was in the intercalative mode. The structure-activity relationship discussion implied that introduction of the nitro-group, especially the 14-nitro group, can significantly improve the cytotoxicity of dehydroabietylimide compounds. The relatively high cytotoxicity and significant high selectivity of compounds 2 and 14 indicated that they were particularly noteworthy. NO released amounts indicated that the amounts of NO released by the compounds bearing nitro-group were quite well associated positive correlation with their cytotoxic activity, which provide a new strategy for structure design of DA anticancer agents in the future.
      原文链接:
    • NSTL
    • Elsevier

    Diverse polyacetylenes from Atractylodes chinensis and their anti-osteoclastogenesis activity

    Zhang Y.Peng X.Sun Z.Hu C....
    6页
    查看更多>>摘要：© 2022 Elsevier B.V.The phytochemical investigation on Atractylodes chinensis afforded 15 polyacetylenes 1–15 and one meroterpenoid 16. Of the 16 isolates, compounds 4 and 9 are new ones, and compounds 8 and 16 are first reported from nature. In addition, the relative configuration of 1 and the available NMR data of compounds 1, 8, and 16 were first provided. Their structures were elucidated by extensive analysis of MS, UV, IR, and NMR spectroscopic data. Besides, all isolated compounds were evaluated for their effects on RANKL-induced osteoclastogenesis in BMMs. Among them, polyacetylenes 12–14 showed potent inhibitory activity with IC50 values of 0.67 ± 0.05 μM, 0.72 ± 0.31 μM, and 2.40 ± 0.41 μM, respectively. The current work demonstrates the polyacetylenes are the main active constituents of A. chinensis against osteoclastogenesis.
      原文链接:
    • NSTL
    • Elsevier