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Fitoterapia
Inverni della Beffa SpA
Fitoterapia

Inverni della Beffa SpA

0367-326X

Fitoterapia/Journal FitoterapiaSCIISTP
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    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.

    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.

    Synthesis of 4-thiosubstituted flavan derivatives and their hypoglycemic activities

    Zhang X.Yang Y.-N.Feng Z.-M.Jiang J.-S....
    7页
    查看更多>>摘要:? 2022A series of 4-thiosubstituted flavan derivatives (1–44) were designed and synthesized. The target compounds were assayed for inhibitory activity against α-glucosidase in vitro, and the results indicated that all compounds displayed significant effects in the range of IC50 = 1.03–7.48 μM compared to that of acarbose, the positive control drug. Structure-activity relationship (SAR) studies indicated that the hydroxyl groups in the flavan B ring, the electron withdrawing groups, and the length of the alkyl chains are important for this biological activity. In addition, some compounds were tested for their tolerance to sucrose in mice, and compound 44 exhibited activity comparable to that of acarbose. Docking analysis indicated that compound 44 binds to the enzyme in a pocket close to the catalytic site, similar to acarbose.

    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.

    (±)-Hyperpyran A: Terpenoid-based bicyclic dihydropyran enantiomers with hypoglycemic activity from Hypericum perforatum (St. John's wort)

    Zhao X.Guo Y.Xu Q.Shi Z....
    5页
    查看更多>>摘要:? 2022(±)-Hyperpyran A (1a/1b), a pair of new terpenoid-based bicyclic dihydropyran enantiomers, were isolated from the aerial parts of Hypericum perforatum (St. John's wort). Their structures and absolute configurations were elucidated by NMR spectroscopic analyses, ECD comparison, and X-ray crystal diffraction. Compounds 1a/1b possess hexahydrocyclopenta[c]pyran ring system and a plausible biosynthetic pathway was also proposed. In addition, compound 1a exhibited a moderate promotion of glucose uptake activity in hepatocytes.

    Sugar easters and xanthones from the roots of Polygala tenuifolia Willd. and their cytoprotective activity

    Wang M.-K.Li X.-J.Yu K.Yang B.-B....
    8页
    查看更多>>摘要:© 2022 Elsevier B.V.Six new sugar esters (1–6), named tenuifolisides F-G (1–2) and tenuifolioses W-Z (3–6), together with 16 known compounds (7–22) were isolated from the roots of Polygala tenuifolia. The chemical structures of the new compounds were elucidated by 1D, 2D NMR and HRESIMS techniques together with chemical methods. All the compounds were evaluated for the cytoprotective activity against hydrogen peroxide (H2O2)-induced oxidative stress in human keratinocyte HaCaT cells. Compounds 4, 5, 13, 20 and 22 showed strong cytoprotective effect.

    Secondary metabolites of the genus Nigrospora from terrestrial and marine habitats: Chemical diversity and biological activity

    Xu T.Song Z.Hou Y.Liu S....
    22页
    查看更多>>摘要:? 2022 Elsevier B.V.Secondary metabolites produced by the ascomycetes have attracted wide attention from researchers. Their diverse chemical structures and rich biological activities are essential in medicine, food, and agriculture. The monophyletic Nigrospora genus belongs to the Apiosporaceae family and is a rich source of novel and diverse bioactive metabolites. It occurs as a common plant pathogen, endophyte, and saprobe distributed in many ecosystems worldwide. Researchers have focused on discovering new species and secondary metabolites in the past ten years. The host diseases caused by Nigrospora species are also investigated. This review describes 50 references from Web of Science, CNKI, Google Scholar and PubMed related to the secondary metabolites from Nigrospora. Here, a total of 231 compounds isolated from five known species and 21 unidentified species of Nigrospora from January 1991 to June 2022 are summarized. Their structures are attributed to polyketides, terpenoids, steroids, N-containing compounds, and fatty acids. Meanwhile, 77 metabolites exhibited various biological activities like cytotoxic, antifungal, antibacterial, antiviral, antioxidant, anti-inflammatory, antileukemic, antimalarial, phytotoxic, enzyme inhibitory, etc. Notably, this review presents a comprehensive literature survey focusing on the chemistry and bioactivity of secondary metabolites from Nigrospora.

    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.

    Geraniol and β-citronellol participate in the vasorelaxant effects of Rosa damascena Miller essential oil on the rat thoracic aorta

    Demirel S.
    8页
    查看更多>>摘要:? 2022 Elsevier B.V.Aim: This study aimed to investigate the vasoactive effects of Rosa damascena Miller essential oil and its major components, geraniol and β-citronellol, on the rat thoracic aorta. Methods: Isolated tissue bath model and Wistar rats were used to perform the experiments. Two-fold increasing concentrations (20–160 μg/mL) of rose oil were administered to determine its vasoactive effects. Submaximal contractions were induced by PE or KCl in both endothelium-intact and -denuded segments. Time-matched control groups were also formed. To evaluate the role of geraniol and β-citronellol, concentrations in the range of 0.4–3.2 μg/mL and 0.8–6.4 μg/mL were applied respectively. The statistical significance level was considered as p < 0.05. Results: All doses of rose oil applied led to vasorelaxation in thoracic aortas precontracted with PE. In precontracted thoracic aortas with KCl, the significant effect of rose oil persisted, albeit slightly diminished. When the endothelium was removed, the relaxant effect of rose oil was partially reduced, but still significant. Besides, although geraniol relaxed aortic segments at all concentrations (0.4 to 3.2 μg/mL), β-citronellol caused vasorelaxation at doses of 1.6, 3.2, and 6.4 μg/mL. Conclusion: In conclusion, the first findings were obtained that rose oil can cause a vasorelaxant effect in a concentration-dependent manner in rat thoracic aorta. This effect substantially persisted in vascular segments without endothelium or precontracted with KCl. It was further shown for the first time that geraniol and β-citronellol exert vasodilatory effects on the rat thoracic aorta. These results suggest that rose oil exhibits its vasorelaxant effect through geraniol and β-citronellol.

    Corrigendum to “Prenylated indole alkaloids and lignans from the flower buds of Tussilago farfara” [Fitoterapia 146 (2020) 104729] (Fitoterapia (2020) 146, (S0367326X20303117), (10.1016/j.fitote.2020.104729))

    Song X.-Q.Sun J.Yu J.-H.Zhang J.-S....
    1页
    查看更多>>摘要:© 2022 Elsevier B.V.The authors regret that the absolute configuration for compound 5 in Fig. 1 was improperly drawn and should be inverted as shown below. Thus, the absolute configuration description for compound 5 should be corrected to ‘7S,8R,7′S,8′R’.[Formula presented] The authors would like to apologise for any inconvenience caused to the scientific community.