Fitoterapia最新文献

Three new monoterpenes compounds (5S, 8S)-5-(2E-butenyl)-8-methyl propionate-cyclopentanone (1), 1-Oxy, 10-keto-α-myrcene hydroxide (2), (3R,4R)-3-hydroxy-4-isobutenyl-cyclopentyl ester (3), along with eleven known small molecular compounds such as monoterpenes (1-7, 14), coumarin (10), and other small molecular compounds (8, 9, 11-13) were isolated from Seriphidium terrae-albae. The structures were elucidated by NMR, HRESIMS, ECD calculations, and X-ray crystallography. Anti-inflammatory activity test results showed that 9 compounds were detected to inhibit NO secretion by mouse macrophage Raw 264.7. Among them, the IC₅₀ value of compound 1 (9.56 ± 0.66 μM) was relatively close to the positive control drug Andrographolide (AG) (2.70 ± 0.39 μM). Molecular docking predicted that the target of compound 1 may be the STAT3 proteins. Further mechanism studies have revealed that compound 1 acted on the STAT3 target in the JAK/STAT signaling pathway, indicating the activation of M2 macrophages, exerted anti-inflammatory effects. Additionally, it could also reduce the cytoplasmic NF-κB content achieve the anti-inflammatory effect. Therefore, compound 1 has the potential to become an anti-inflammatory lead compound. This study provides reference value for the research and development of small-molecule natural product anti-inflammatory drugs.

Previously undescribed benzophenone rhamnosides, triadenosides A-F (1-6), were isolated from the aerial parts of Triadenum japonicum (Blume) Makino (Hypericaceae), where known compounds including benzophenone rhamnosides (7 and 8), benzophenone C-glucoside (9), flavonols and their glycosides (10-17), and biflavone (18) were also isolated and identified. Detailed spectroscopic analysis revealed that triadenoside A (1) was 2,3',5'-trihydroxy-4,6-dimethoxybenzophenone 2-O-α-L-rhamnopyranoside, while the absolute configuration of the rhamnosyl moiety was confirmed by HPLC analysis. Triadenosides B-E (2-5) were assigned as acetyl derivatives of 1 in their rhamnosyl moieties. In contrast, triadenoside F (6) was elucidated to be 2,3',5',6-tetrahydroxy-4-methoxybenzophenone 2-O-α-L-(4″-O-acetyl)rhamnopyranoside. Compounds 1-18 isolated from T. japonicum as well as some benzophenone derivatives (5a-5e, 6a, and 8a) prepared from 5, 6, and 8 were evaluated for their inhibitory activity against RSL3-induced ferroptosis on human hepatoma Hep3B cells, showing significant inhibitory effects of triadenosides A-E (1-5) and their derivatives (5c, 5d, and 5e) with EC₅₀ values ranging from 18.0 to 41.4 nM comparable to that of a ferroptosis inhibitor, ferrostatin-1, whereas triadenoside F (6) did not exhibit such activity.

Euodia Fruit is a crude drug used to treat migraine and headaches and is well-known to contain indole alkaloids, which may contribute to the observed pharmacological activities. A methanolic extract of Euodia Fruit exhibited pancreatic lipase inhibitory activity (IC₅₀ 13.9 mg/mL). Bioassay-guided fractionation of the extract led to the isolation of 14 quinolone alkaloids (1-14), three indole alkaloids: rutaecarpine (15), evodiamine (16), and dehydroevodiamine (17), and a limonoid: rutaevine acetate (18), among which three quinolone alkaloids (12-14) have been previously undescribed. The structures of 12-14 were determined by extensive spectroscopic analyses, including two-dimensional (2D) NMR. Compounds 2, 3, 6-9, 13, and 14 exhibited pancreatic lipase inhibitory activity, with IC₅₀ values ranging from 1.40 to 7.37 mM. The results revealed that the length of the aliphatic side chain and the presence of an olefinic bond at the C-2 side chain of the quinolone alkaloids could impact lipase inhibitory activity. In soybean oil-loaded mice, orally administered evocarpine (8) reduced serum triglyceride levels in a dose-dependent manner. Furthermore, 8-14 at 5.0 and 50 μM exhibited peroxisome proliferator-activated receptor (PPAR)-γ ligand-binding activity.

Diabetes mellitus is a global chronic metabolic disease and the prevalence of diabetes mellitus is increasing dramatically every year. Berberine (BBR) from Coptidis Rhizoma has potent hypoglycemic effects, however, the specific proteins targeted by berberine that contribute to its hypoglycemic action remain to be elucidated. In this work, TIGAR (TP53-induced glycolysis and apoptosis regulator) was identified as a direct target protein for berberine using activity-based protein profiling (ABPP) and other chemical proteomics techniques with active photoaffinity probes as chemical tools. In addition, the study revealed that berberine-targeted TIGAR attenuated the conversion of fructose-2, 6-bisphosphate to fructose-6-phosphate. This study demonstrated an innovative mechanism by which berberine directly targets TIGAR and its hypoglycemic effects. Therefore, TIGAR emerges as a novel target for the treatment of diabetes mellitus, with TIGAR inhibitors offering a new and promising therapeutic strategy for managing the disease.

Seven diterpenoids including five ent-cleistanthanes (1, 2, 4-6) and two ent-pimaranes (3, 7) were isolated for the first time from the aerial part of Phyllanthus franchetianus H. Lév. Their structures were elucidated on the basis of the extensive spectroscopic analyses, single-crystal X-ray diffraction and ECD analysis. Phyllanthanes A-C (1-3) are new compounds. Notably, the ent-cleistanthanes 1 and 4-5 exhibited moderate cytotoxicity against five human cancer (HL-60, A549, HepG2, MDA-MB-231, SW480) (IC₅₀ = 5.01-32.41 μM) and one normal BEAS-2B (IC₅₀ = 20.45-24.33 μM) cell lines.

Two populations of Physalis patula Miller collected in different localities (Querétaro and Teotihuacán) of Central México were analyzed. Eight new compounds including three withanolides, physapatolides A-C (1-3), two labdanes, 12-epi-physacoztomatin (10) and physapatulone (12), besides three 12-O-glucosyl labdanes, patulosides A-C (13-15), were isolated from these collections. A series of known withanolides, flavonoids, labdanes, sucrose esters, and sterols were also isolated. Withanolides isolated of each population exhibited different substitution patterns of ring D, thus while 15,16-dioxygenated withanolides were found in the Querétaro population, oxygenation occurs at C-14 and C-15 in those isolated from Teotihuacán population. The structures of all the isolated compounds were determined by analysis of their spectroscopic and spectrometric data. The absolute configuration assigned to physapatolide A (1) was confirmed by X-ray diffraction analysis of its acetyl derivative 1a, while those of labdane diterpenoids were based on chemical correlations. The antibacterial activity of 16 of the isolated compounds (1-3, 5-9, 13, 14, and 16-21) and two derivatives (13a, 14a) was evaluated against five ATCC bacterial strains (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus subtilis). Compounds 1-3 inhibited around 100 % the growth of S. aureus at 250 μg/mL (w/v). The minimum inhibitory concentrations (MIC) of compounds 1, 2, and 3, against S. aureus were 62.5, 125 and 62.5 μg/mL, respectively, whereas their MIC's against a Methicillin-resistant S. aureus (MRSA) clinical isolate were 125, 62.5 and 62.5 μg/mL, respectively.

This study investigated the antihyperglycemic potential of a hydroalcoholic extract from Syzygium malaccense leaves (E-SM) and isolate phenolic compounds with antioxidant and cytotoxic activities through a bioguided assay. The aim was to explore the therapeutic properties of S. malaccense in managing hyperglycemia and oxidative stress-related conditions. E-SM was prepared using ethanol-water (40:60 v/v) and purified through a solid-liquid procedure with increasing polarity solvents, yielding the acetone fraction (AceFr). Previous studies showed Ace-Fr had potent antioxidant and cytotoxic properties. Chromatographic techniques further purified AceFr, producing three bioactive subfractions (SF-1, SF-2, and SF-3). Flavonoids myricitrin (C1) and a mixture of quercitrin and mearnsitrin (M1) were isolated from SF-2 and SF-3 using TLC preparative. HPLC-DAD quantified phenolic compounds, including myricitrin, gallic acid, myricetin, and quercetin. HPLC-ESI-QTOF-MS/MS analysis identified ten compounds, primarily flavonols quercetin and myricetin and their glycosides. SF-1 exhibited a 30 % reduction in cell viability in cutaneous melanoma cells at 100 and 250 mg L^-1, while SF-2 and SF-3 displayed enhanced antioxidant potential and reduced cancer cell locomotion proportional to concentration. In diabetic rats treated with E-SM (400 mg/kg), kidney tissue showed restored catalase activity similar to the control group, with consistent NPSH levels. Increased GST activity indicated tissue protection, while lower MDA levels suggested reduced lipid peroxidation across tissues. Our results indicate that three phenolic compounds with high antioxidant activity were isolated, and the chemical composition of the E-SM extract, rich in glycosylated flavonoids, could be related to its antihyperglycemic action.

Prunella vulgaris is a medicinal and edible homologous plant, commonly used as a folk medicine to treat diseases. The Prunella vulgaris polysaccharides (PVPs) are reported with the antioxidant activity. This work was designed to isolate, characterize, and test the antioxidant activity of purified PVPs from P. vulgaris. A new homogeneous polysaccharide (PVP-1) was prepared by the DEAE column from PVPs, and diverse chromatography/spectroscopy and chemical methods were simultaneously employed to characterize the fine structure of PVP-1. The result showed PVP-1 had a triple helix structure, and the repeating structural unit of PVP-1 was composed of →6)-β-D-Galp-(1→6)-β-D-Galp-(3,1→6)-β-D-Galp-(1→6)-β-D-Galp-(1→ as the main chain, together with →6)-β-D-Galp-(1,3→1)-α-D-Araf-(5→1)-β-D-Galp-(4→1)-α-D-Galp-(2→ and →6)-β-D-Galp-(1,3→1)-α-D-GlcAp-(4→1)-α-D-Glcp-(4→1)-α-D-Galp as the branch chains. The main monosaccharides of PVP-1 were galactose (Gal, 41.25 %), galactose-OMe (Gal-OMe, 27.73 %), arabinose (Ara, 10.63 %), mannose (Man, 9.86 %), glucose (Glc, 3.88 %), glucuronic acid (GlcA, 2.86 %), ribose (Rib, 1.79 %), and xylose (Xyl, 1.76 %). In addition, the scanning electron microscopy (SEM) displayed that the surface of PVP-1 was rough and porous. PVP-1 gave the scavenging rates of the DPPH, ABTS, and hydroxyl radical lower than vitamin C at the same concentration, with the highest scavenging rate of DPPH radical at 82.71 % ± 4.19 % (5 mg/mL).

Ethnopharmacological relevance: Hypertension is a serious health problems and a leading cause of adult mortality worldwide. Foeniculum. vulgare Mill, a plant traditionally used for various ailments, including cardiovascular disorders such as hypertension.

Aim of the study: The objective of the study is to verify the vasorelaxant effect of fennel seeds on the isolated and perfused mesenteric vascular beds in rats.

Materials and methods: The vasorelaxant effect of the aqueous extract of F. vulgare (AEFv) seeds was tested on mesenteric arteries, both intact and denuded, precontracted with phenylephrine. Extracts from liquid-liquid extraction of F. vulgare were screened to find the active fraction. The mechanism of action of the active butanolic fraction (BFFv) was studied using inhibitors like L-NAME (nitric oxide synthase inhibitor), ODQ (guanylate cyclase inhibitor), indomethacin (cyclooxygenase inhibitor), potassium channel blockers (tetraethylammonium TEA, and glibenclamide), and atropine (a muscarinic receptor antagonist). Moreover, the antioxidant properties of AEFv and BFFv were evaluated using DPPH radical scavenging, β-carotene linoleic acid, and ferric-reducing power assays; total flavonoids and phenolics of AEFv and BFFv were measured using Folin-Ciocalteu and aluminum chloride colorimetric assays; HPLC-DAD analysis and acute toxicity of BFFv in mice were also performed.

Results: AEFv caused a concentration-dependent vasodilatory response in intact mesenteric arteries (E_max = 81.73 ± 0.36 %). This effect was significantly reduced after endothelium removal. The butanolic fraction showed the highest vasorelaxant effect. The vasodilatory effect was attenuated by L-NAME, ODQ, indomethacin, TEA, glibenclamide, and atropine, indicating involvement of the NO/GMPc pathway, potassium channels, and muscarinic receptors. Additionally, fennel extracts demonstrated excellent antioxidant activity and high concentrations of flavonoids and phenolic compounds. HPLC-DAD analysis of the butanolic fraction revealed an abundance of phenolic acids. Acute toxicity studies of BFFv showed no toxic effects.

Conclusion: Our findings support the traditional use of Foeniculum vulgare seeds for preventing cardiovascular disorders associated with vascular dysfunction, highlighting their vasorelaxant and antioxidant properties.

Three novel compounds, including an aromatic amino acid, dimorine A (1), a suncheonoside derivative, dimoroside A (2), and a phenylpropanoid glycoside, dimoroside B (3), together with four known compounds (4-7) were separated from Umbelopsis dimorpha VDG10, the predominant endophytic fungus found in the roots of Vaccinium dunalianum Wight (Ericaceae). Their structures were elucidated by spectroscopic methods, and the ECD spectrum confirmed the absolute configuration of 3. In addition, the antifungal activities of novel compounds against five phytopathogenic fungi were evaluated. The results indicated that compound 3 has a better inhibitory effect on Alternaria brassicicola than the broad-spectrum antifungal agent thiabendazole, and its MICs of 15.63-7.82 μg/mL.