Natural Product Research最新文献

The aim of this work was to explore the bioactive properties of Moringa stenopetala leaves (Baker f.) Cufod. Methanol and ethanol extracts showed the highest antioxidant activity with the lowest IC₅₀ values. MS leaves were found to be a good supplement for K, Fe and Ca. The obtained results indicated that ethanolic leaf extract exhibits growth inhibition of MDA-MB-231 cell line, and induction of apoptosis as well as cell cycle arrest. Also, there was a significant effect on cytotoxicity against a breast cell line when the ethanolic extract was combined with doxorubicin. At the molecular level, changes in gene expression were detected via qPCR. Thirty-two compounds were identified in the ethanolic extract using HPLC ESI-MS/MS and classified into: hydroxycinnamic acid derivatives, flavonoids, fatty acids, and other miscellaneous compounds. Molecular docking predicted that the main component in the ethanolic extract (apigenin-7-O-rutinoside) has multiple inhibitory effects on MDR-1, Raf-1 and Top-II proteins.

The medicinal and commercial value of pomegranate peel is attributed to its rich content of phenolic compounds, yet little is known about their concentrations and biological activity across different ripening stages. Pomegranate peels at different growth stages 1-3 (40, 80, and 120 days after fruit appearance respectively) were collected, dried, and macerated with 90% methanol. Stage 2 and stage 3 extract showed significant antimicrobial activity against S. aureus, and L. monocytogenes. Further, stage 2 extract showed highest efficacy against lung, breast, and liver cancer cells with IC₅₀ values of 19.76 ± 1.3, 24.28 ± 6.99, and 16.04 ± 2.78 µg/mL, respectively. Molecular docking, and simulation further confirmed the antimicrobial and cytotoxic activity of the most prominent stage 2 phytoconstituent (γ-Sitosterol). The study indicates that stage 2 pomegranate peel extract has potential as a safe and natural antimicrobial and cytotoxic agent. However, additional in vitro and in vivo testing is needed to validate these results.

One new acyclic norditerpenoid, lamellodysideol (1) was isolated from the Indonesian marine sponge Lamellodysidea herbacea together with known phytol (2). The structure of 1 was determined on the basis of spectral evidence and by comparison with known related molecules including optical rotation data. The relative configurations of 1d and 2b were proposed using quantum chemical calculation of NMR chemical shifts at DFT levels. In addition, the relative configuration of 2b was also supported by Newman's rule of six and confirmed through Hehre's protocol. Compounds 1d and 2b showed toxicity against NBT-T2 cells assay at 10 µg/mL.

To discover biorational natural product-based pesticides, a series of paeonol ester derivatives containing a Schiff base (6a-j, 7i,j, 8i,j, and 9i,j) were prepared, and their structures were well characterised by ¹H NMR and HRMS. Furthermore, bioactivities of these compounds as anti-oomycete and anti-fungal agents against two serious agricultural diseases, Phytophthora capsici and Fusarium graminearum we assessed. Amongst evaluated compounds, 1) Compounds 6a and 6e displayed good anti-oomycete against P. capsici, with EC₅₀ values of 116.50 and 88.86 mg/L, respectively. 2) Compounds 6e and 7i exhibited prominent anti-fungal against F. graminearum, with EC₅₀ values of 66.73 and 29.33 mg/L, respectively. 3) This study suggested that the introduction of nitro at the C5 position of paeonol could improve its bioactivity against P. capsici and F. graminearum. The results of this study pave the way for further design and development of paeonol derivatives as plant anti-oomycetes and anti-fungal agents in crop protection.

Propolis is a resinous material collected by different bee species from various plant exudates and used to seal holes in honeycombs, smoothen the internal walls, embalm intruders, improve health and prevent diseases. From its n-hexane extract, eight compounds were isolated and characterised as: mangiferonic acid (1); 1-hydroxymangiferonic acid (2), new natural product; mangiferolic acid(3); 27-hydroxymangiferolic acid (4), reported here for the first time as propolis constituent; 27-hydroxymangiferonic acid (5); α-amyrin (6); β-amyrin (7) and lupeol (8). The chemical structures of the isolated compounds were elucidated using spectroscopic methods, such as 1D and 2D-NMR, mass spectrometry and comparison with previous published reports. Compounds 6-8 and n-hexane extract were tested against Gram-negative and Gram-positive bacteria strains using agar disc diffusion and macrodilution techniques. Interestingly, n-hexane extract and compounds 6-8 had good inhibitory activities against Methicillin Resistant Staphylococcus aureus (MRSA) and the clinical Klebsiella pneumoniae isolates. The biological effects of n-hexane extract and its fraction against K. pneumoniae 12 CM and MRSA revealed in the present study suggest that the Cameroonian dark brown propolis could be a potential alternative management of biofilms on medical devices and respiratory skin or infections.

Two new compounds including one benzaldehyde (1) and one azaphilone (2) were isolated from the marine-derived fungus Penicillium sclerotiorum PSU-AMF89 together with nine known compounds (3-11). Their structures were determined by spectroscopic evidences. The absolute configuration of 2 was established by comparison of the ECD data with those of the previously reported data of compound 7 as well as the biosynthetic consideration. Compound 1 displayed potent cytotoxic activity against MCF-7 cells with an IC₅₀ value of 9 µM, compared with the standard drugs, tamoxifen and doxorubicin, whereas compounds 3 and 8 were moderately active against Cryptococcus neoformans and methicillin-resistant Staphylococcus aureus, respectively, with equal MIC values of 64 µg/mL. In addition, they were non-cytotoxic to noncancerous Vero cells.

Mushrooms have proven to be a valuable source of diverse bioactive compounds that can hold substantial potential for preventing and managing various diseases. This research focused on examining the numerous bioactive compounds found in Pisolithus albus (P. albus) (Cooke & Massee) Priest mushrooms, particularly those obtained from ethyl acetate and dichloromethane extracts. Polyphenols, flavonoids, tannins, and alkaloids were also evaluated by chemical analysis. Furthermore, the bioactive compounds of extracts were identified using thin-layer chromatography (TLC), gas chromatography-mass spectrometry (GC-MS), and Liquid Chromatography Mass Spectrometry (LC-MS). Evident diversity in the phytochemical composition was noted between the ethyl acetate (EtOAc) and dichloromethane (DCM) extracts, identifying through spectrometric methods interesting bioactive compounds that exhibit potential utility across medicinal and agricultural domains, including their application as herbicides. This study not only shed light on the bioactive constituents within the two types of extracts but also underscored the advantageous compounds inherent in P. albus mushrooms.

Diabetes mellitus is a rising global health issue, necessitating effective and affordable treatments. This study aimed to develop marker-based quantification methods for Diospyros montana Roxb using a DoE approach and conduct in-silico anti-diabetic screening of its phytoconstituents. Methanolic extracts of the plant underwent fractionation, with the chloroform fraction used for simultaneous HPLC quantification of Plumbagin and Juglone. The in-vitro anti-diabetic effects were evaluated through alpha-amylase and alpha-glucosidase inhibition assays. Cytoscape 3.7.2 was used to construct networks linking phytoconstituents to Type-2 diabetes targets and pathways, while docking studies involved proteins 1SO2, 3H1V, and 5DXU. A validated HPLC method quantified Plumbagin (Rt: 4.618) and Juglone (Rt: 3.998). The chloroform fraction showed significant enzyme inhibition with IC50 values of 36.775 and 33.124. Gene network analysis highlighted 8-hydroxyisodiospyrin, and docking revealed Astragalin's strong binding to 3H1V (score: -10.537). This study underscores Diospyros montana Roxb potential in diabetes management, warranting further research.

Seventeen compounds were isolated from the aerial parts of Ceratocarpus arenarius L., including 1 previously undescribed xanthone and 6 firstly isolated compounds. The structures of compounds were identified by Mass spectrometry and NMR spectroscopy. In addition, the in vitro cytotoxicity of the isolates against human oesophageal squamous carcinoma KYSE-150 and KYSE-70 cell were investigated by MTT to identify Genistein (8) and 1,4-dihydroxy-2-naphthoic acid (9) as the most effective compounds, which could exhibit anti-proliferation activity with IC₅₀ values of 39.11 μg/mL and 5.71 μg/mL against KYSE-150, 34.07 μg/mL and 4.51 μg/mL KYSE-70, respectively. Swiss target prediction and Molecular docking were applied to reveal the action mechanism of the effective compounds and provide guidance for the potential use of the C. arenarius L. in antitumor treatment.