查看更多>>摘要：? 2022 Elsevier B.V.Seven undescribed thermopsine-based alkaloids (1–7), including one undescribed biogenetically related intermediate (7), were isolated from the seeds of Thermopsis lanceolata R. Br. Compound 1 possessed a 6/6–6 tricyclic skeleton, while compounds 2–6 represented three rare dimerization patterns constructed by quinolizidine alkaloids. Their structures were elucidated by comprehensive spectroscopic data analysis as well as ECD calculations. Biologically, compound 6 displayed significant anti-Tomato spotted wilt virus (TSWV) activity compared with the positive control ningnanmycin. Moreover, compound 1 exhibited good insecticidal activity against Aphis fabae with LC50 value of 25.2 mg/L.
查看更多>>摘要：? 2022Four undescribed sesquiterpenes (1–4) and 20 known sesquiterpenes (5–24) were obtained from the fruits of Litsea lancilimba Merr. by Small Molecule Accurate Recognition Technology (SMART). The gross structures and the relative configurations of the new compounds were deduced by spectroscopic data analysis. The absolute configurations were defined by comparison of their experimental and calculated electronic circular dichroism (ECD) spectra data. All compounds were screened for their neuroprotective effects against H2O2-induced SH-SY5Y cells injury. Compounds 2, 3, 7, 8 and 13 exhibited comparable neuroprotective activity to the positive trolox at 50 μM.
查看更多>>摘要：? 2022 Elsevier B.V.Twelve dihydro-β-agarofuran-type sesquiterpenoids, including five new ones (1–5), were purified from the seeds of Celastrus virens (Wang et Tang) C. Y. Chent et T. C. Kao. Their chemical structures were characterized via comprehensive spectroscopic analysis, single-crystal X-ray diffraction analysis, and computational prediction of ECD, as well as comparison of observed and reported NMR spectral data. Among the isolates, nine abundant dihydro-β-agarofuran-type sesquiterpenoids were evaluated for their lifespan-extending activity using the nematode Caenorhabditis elegans model. As a result, compounds 1, 2, 5, 6, 8, and 9 (50 μM) significantly extended the mean survival time of C. elegans, respectively, compared with the blank control group (p < 0.05). Further Quantitative RT-PCR showed that the prolonging of lifespan mediated by compounds 1, 6, 8, and 9 were dependent on the transcription factors skn-1 and hsf-1.
查看更多>>摘要：? 2022Nine new sesquiterpenes wenyujinones A-I (1–9), along with ten known ones (10–19), were isolated from the rhizomes of Curcuma wenyujin Y. H. Chen et C. Ling (C. wenyujin). The chemical structures of compounds 1–9 were elucidated by NMR spectroscopic and mass spectrometric data, electronic circular dichroism (ECD) spectra analysis. Furthermore, all compounds were evaluated for the protective effects against hydrogen peroxide (H2O2)-induced injury in human hepatic L02 cells, for the inhibitory effects on nitric oxide (NO) production in RAW 264.7 cells, and for their cytotoxicity against three human cancer cell lines A549, HL60, and MCF7 in vitro. As a result, compounds 2, 4, 14 markedly weakened the oxidative damage induced by H2O2 in L02 cells via strengthening the cell viability.
查看更多>>摘要：? 2022 Elsevier B.V.Ginsenosides, characterized by triterpenoid, are one of the active components of ginseng. Among them, PPD-type ginsenosides have potent and diverse pharmacological activities, while the effective applications and clinical studies are limited by the poor stability, water solubility and oral bioavailability. In this review, we have attempted to demonstrate the structural-activity relationship of chemical modifications on the dammarane-type skeleton and the C-17 side chain, noting that certain structurally modified derivatives exhibit satisfactory pharmacological activity. This review will provide ideas for the design and synthesis of novel PPD derivatives, and valuable help for the further study of PPD derivatives to make it realize clinical application.
查看更多>>摘要：? 2022 Elsevier B.V.Inflammation is a critical defense mechanism for body which is crucial for wound healing. However, when it spirals out of control and becomes chronic, it possesses a risk for diseases such as metabolic disorders or cancer. Scutellaria L. species are known with their potent anti-inflammatory effects. We aim to investigate the potential anti-inflammatory effects of Scutellaria brevibracteata Stapf and its active principles with underlying mechanisms using both in vitro and in vivo methods. Aqueous extract of S. brevibracteata (SB) was chromatographed on several columns to get 6 main fractions and 2 pure compounds. The levels of IL-6, NO, and TNF-α were measured in LPS-induced RAW 264.7 cells. In vivo carrageenan-induced paw edema test and immunoblotting in these paws were performed. SB was significantly reduced the inflammation in LPS-induced RAW cells via IL-6 and TNF-α cytokines at 200 μg/mL (P < 0.001) and paw edema via COX-2 and iNOS (P < 0.001). 3-O-methyl kaempferol, isolated from SB, reduced the production of NO, IL-6 and TNF-α in LPS-stimulated macrophages at 50 μM (P < 0.001); it significantly diminished inflammation-induced edema and COX-2, iNOS, and NF-κB protein levels were reduced compared to control group (P < 0.001). It was noticed that the methoxylation of C3 position has no effect on the anti-inflammatory mechanism of action comparing with kaempferol. In vivo studies indicated 3-O-methyl kaempferol was as effective as indomethacin. Considering the side effects caused by indomethacin, this compound can be evaluated as a novel drug candidate in inflammatory diseases with fewer side effects.
查看更多>>摘要：? 2022 Elsevier B.V.Four undescribed secocycloartane monoglycosides (1–4) were isolated from an ethanolic extract of the dry flowers of Cordia lutea Lam. Their structural assignment is based on NMR and MS analysis. Their stereochemistry is confirmed by molecular modelling studies using DFT-NMR calculations done for compound 3. In vitro antibacterial activity of the four compounds was moderate on Helicobacter pylori (MIC = 15.6 μg/mL), and much weaker on Staphylococcus aureus, Pseudomonas aeruginosa or Escherichia coli (MIC >125 μg/mL). Toxicity evaluated against RAW 264.7 cells was weak (IC50 values ranging from 24 to 41 μM i.e. 15 to 24 μg/mL), but in the same range as anti-Helicobacter activity.
查看更多>>摘要：? 2022Grossheimin 1 is a polyfunctionalized sesquiterpene, featuring, in addition to the exomethylene-γ-lactone group, also an additional exocyclic double bond, a hydroxyl, and a ketone carbonyl. These functional groups have been modified, generally in an orthogonal way, by arylation of the exomethylene, by the introduction of heteroatoms associated to oxygen-, nitrogen- and phosphorous functionalities, and by acylation. A selection of the analogues was investigated for bioactivity, showing that the introduction of a substituent at C-13 is not detrimental, and can modulate potency independently from retention or reduction of the C-11 – C-13 exomethylene double bond and the effect of this maneuver on Michael reactivity. In vivo experiments of 26 samples made it possible to establish that grossheimin 1 and its five new derivatives have a pronounced antitumor activity against alveolar liver cancer, Pliss lymphosarcoma, Walker's carcinosarcoma, sarcoma 45, M-1 sarcoma, P-388 leukemia.
查看更多>>摘要：? 2022A pair of enantiomers with a rearranged dimeric phenylethanol skeleton, namely (±)-disyringol A (1a and 1b), were isolated from the stem barks of Syringa pinnatifolia. The structures were established using IR, UV, MS, and NMR data, and their absolute configurations were resolved by experimental and calculated ECD data analysis. Their biosynthetic pathway was speculated on the basis of a phenylethanoid precursor and was proved by a total synthesis. Compounds 1a and 1b showed the inhibition against NO production in LPS-induced RAW264.7 cells with their IC50 values of 27.28 and 24.64 μM, respectively, however no protective effect was observed against the hypoxia-induced injuries to H9c2 cells.
查看更多>>摘要：? 2022 The Author(s)The CH2Cl2/MeOH (1:1) extract of the stems of Tephrosia uniflora yielded the new β-hydroxydihydrochalcone (S)-elatadihydrochalcone-2'-methyl ether (1) along with the three known compounds elongatin (2), (S)-elatadihydrochalcone (3), and tephrosin (4). The structures were elucidated by NMR spectroscopic and mass spectrometric data analyses. Elongatin (2) showed moderate antibacterial activity (EC50 of 25.3 μM and EC90 of 32.8 μM) against the Gram-positive bacterium Bacilus subtilis, and comparable toxicity against the MCF-7 human breast cancer cell line (EC50 of 41.3 μM). Based on the comparison of literature and predicted NMR data with that obtained experimentally, we propose the revision of the structures of three β-hydroxydihydrochalcones to flavanones.
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