Fitoterapia最新文献

Twenty-eight chemical constituents including seven previously undescribed compounds [1, 2, 10, (+)16, and 17-19] were isolated from the fresh roots of Rehmannia glutinosa (Gaertn.) Libosch. ex DC. Their structures were determined by NMR and MS datas, distinct J coupling constants, and quantum chemical calculations. All the isolated compounds were screened for their cytotoxicity against MCF-7 and Hep-G2 cell lines. The results indicated that compounds 1, 10, (+)16, and 18 showed potent cytotoxicity against MCF-7 cell lines, with IC₅₀ values ranging from 17.2 ± 0.7 to 19.6 ± 0.7 μM, and compound 17 exhibited significant cytotoxicity against Hep-G2 cell lines, with IC₅₀ value of 25.8 ± 1.2 μM.

Four undescribed ecdysteroid glycosides (1-4) and ten known analogues (5-14) were isolated from the rhizomes of Paris yunnanensis and Paris mairei. Among them, compound 3 is a rare 14-deoxy derivative of ecdysteroid, while compounds 7-9, 11, 12, and 14 were reported from the genus Paris for the first time. Structural elucidation was performed through comprehensive spectroscopic analysis, including MS, NMR, chemical methods, and QM-NMR calculation. Furthermore, all isolated ecdysteroid derivatives were evaluated for anti-inflammatory activity. The results showed that compounds 3 and 7 displayed pronounced anti-inflammatory activity by inhibiting COX-2 expression, with IC₅₀ values of 11.59 and 12.66 μM, respectively.

Obesity is a complex metabolic disease caused by an energy imbalance, characterized by excessive weight gain, adiposity and disturbed lipid metabolism. Though several pharmacological anti-obesity drugs are available, their side effects have promoted interests towards natural alternatives. Edible mushrooms because of their rich bioactive constituents have emerged as capable anti-obesity agents. In this context, present study aims to examine the bioactive metabolite present in M. esculenta and its effects for managing diet-induced obesity in zebrafish. Preliminary phytochemical analysis confirmed the presence of different bioactive constituents, which were further characterized through Orbitrap High-Resolution Liquid Chromatography Mass Spectrometry (OHR-LCMS), leading to the identification of 38 different metabolites. In vitro pancreatic lipase inhibition assays confirmed concentration dependent enzyme suppression by aqueous extract of M. esculenta with IC₅₀ value of 130.31 ± 0.39 μg/mL. In vivo assessment using a diet-induced obese zebrafish model revealed significant reductions in body weight, size, body mass index (BMI) and fasting blood glucose level after dietary supplementation with M. esculenta fruiting bodies powder. Serum lipid profiling also depicted improvements by dropping levels of triglycerides (TG), total cholesterol (TC), low density lipoprotein (LDL) and very low density lipoprotein (VLDL) and increasing in high density lipoprotein (HDL). Histopathological examination of adipose tissue revealed decreased adipocyte hypertrophy and adipocyte count. Furthermore, ATR-FTIR spectroscopy of blood serum showed attenuated lipid and protein associated vibrational intensities in M. esculenta supplemented group. Collectively, these findings highlight the potential of M. esculenta supplementation as a natural, multi-target approach for management of obesity and related metabolic impairments.

This study aimed to elucidate the sedative-hypnotic effects of a stem-derived bioactive fraction from Syringa oblata Lindl. (ZDX) and to reveal its underlying mechanisms, thereby providing a theoretical and practical basis for the development of new sleep aid drugs. ZDX was prepared by optimizing the extraction and purification procedures. Using UPLC-Q-TOF-MS, the prototype compounds absorbed into the brain of insomnia mice were analyzed, and 15 bioactive compounds were identified or predicted, including Dihydrocubebin, (-)-Cubebin, Isoguamarol, and others. Its efficacy and mechanisms were investigated using network pharmacology, transcriptomics, metabolomics, and molecular docking, complemented by in vivo pharmacodynamic and molecular analyses. In an insomnia mouse model, ZDX significantly increased body weight, reduced sleep latency, and prolonged total sleep duration, while alleviating anxiety and depression-like behaviors and improving histopathological damage in the hippocampus and hypothalamus, showing significant sedative-hypnotic effects. Mechanistically, ZDX modulated key genes and proteins involved in the cAMP signaling pathway, enhanced superoxide dismutase activity, reduced malondialdehyde levels, decreased inflammatory cytokines (IL-6, IL-1β, and TNF-α), and restored neurotransmitter homeostasis in the brain. Collectively, ZDX exerts sedative-hypnotic effects, at least in part, by activating the cAMP/PKA-CREB-BDNF axis and coordinately regulating neurotransmission, oxidative stress, and inflammation.

This study investigated the effects and mechanisms of Cornus officinalis Siebold & Zucc. ethanol extract (COEE) on primary dysmenorrhea (PD). COEE administration dose-dependently reduced writhing times, prolonged writhing latency, decreased uterine prostaglandin F_2α (PGF_2α) levels and pro-inflammatory mediators, and improved histopathological signs of uterine inflammation. Furthermore, COEE suppressed the activation of the TLR4/MyD88/NF-κB/NLRP3 signaling axis. In ex vivo experiments, COEE inhibited spontaneous and agonist-induced uterine contractions, attenuated CaCl₂-induced contractile recovery, and reduced Bay K 8644 evoked Ca²⁺-mediated contractions. Collectively, our findings suggested that COEE alleviates PD by attenuating uterine inflammation and abnormal calcium-dependent contractions, supporting its potential use as a functional food source for managing PD.

Malignant melanoma is an aggressive cancer requiring new therapeutic options. Isodonal, a known spirolactone type ent-kauranoid, was obtained in high abundance from Isodon oresbius. Phenotypic screening of isodonal revealed its antiproliferative activity against A375 melanoma cells. In the structural modification to prompt its selection for optimization, we synthesized a focused library of thirty new ester derivatives (8-37) at C-6 position of isodonal. All analogues exhibited enhanced potency (IC₅₀ = 0.73-4.43 μM) over isodonal, with the C-6 4-fluorocinnamate ester 29 being most potent (IC₅₀ = 0.73 μM; ∼10-fold improvement). Structure-activity relationship analysis revealed that conjugated systems (e.g., cinnamoyl) boost activity, and that specific substitutions in benzoate derivatives can modulate selectivity between melanoma and normal cells. Compound 29 was found to suppress proliferation, induce apoptosis and G2/M phase arrest, and elevate ROS levels in A375 cells. This study delivers a potent lead compound and a framework for the natural product-inspired development of anti-melanoma therapeutics.

Andrographolide (AG), a natural diterpenoid compound derived from Andrographis paniculata, exhibits potential against non-alcoholic steatohepatitis (NASH). However, its therapeutic utility is limited by poor solubility, short half-life, and low bioavailability. This study aimed to enhance AG's efficacy by encapsulating it into exosome-like nanoparticles (ELNs) isolated from Nauclea officinalis (N. officinalis, Rubiaceae family) and evaluating its anti-NASH activity in WRL68 cells. This study isolated Nauclea officinalis-derived ELNs (N-ELNs) via ultracentrifugation. Loganin, andrographolide, and asiatic acid were detected in N-ELNs using the HPLC method. RNA sequencing and target gene analysis identified miRNAs in N-ELNs and their cross-kingdom targets in the human genome. AG-loaded N-ELNs (AG-N-ELNs) were prepared using a passive loading method and characterized by transmission electron microscopy, nanoparticle tracking analyzer, and high-performance liquid chromatography. Their effects were tested in free fatty acid (FFA)-exposed WRL68 cells. As for the results, AG suppressed Nuclear Factor kappa-B p50 (NF-κB p50) activation, downregulated NLRP3 expression, and reduced pro-inflammatory cytokines (IL-1β, IL-6, TNF-α) in WRL68 cells. It also restored mitochondrial membrane potential and decreased reactive oxygen species (ROS). N-ELNs targeted the ACC/ CPT1 axis to alleviate lipid deposition, reducing total cholesterol and triglyceride levels. AG-N-ELNs outperformed both AG and N-ELNs individually, demonstrating superior anti-NASH activity through synergistic effects of AG's anti-inflammatory/antioxidant properties and N-ELNs' miRNA-mediated metabolic regulation. In conclusion, AG-N-ELNs effectively alleviate NASH-like pathological features in vitro through multi-target regulation, offering a promising strategy for NASH treatment. Further in vivo validation and formulation optimization are warranted.

The plant kingdom is estimated to produce at least 250,000 distinct natural products, a significant proportion of which remain structurally and biologically uncharacterized, representing a vast, underexplored reservoir of chemical diversity. Withania adpressa Coss. ex Batt is an endemic species of the Moroccan Sahara and a member of the Solanaceae family. Traditionally, nearly all parts of the plant, including roots, leaves, flowers, and fruits have been used to treat digestive disorders, gastritis, colds, rheumatoid arthritis, and for their purported diuretic and aphrodisiac effects. The plant is notably rich in bioactive secondary metabolites, particularly withanolides, which are largely responsible for its diverse pharmacological properties, including antitumor, anticancer, antioxidant, antimicrobial, and anti-inflammatory activities. Despite promising findings supporting its anticancer potential, no W. adpressa based-extract has yet been developed into a commercially available traditional medicine. In this line, further studies and clinical trials are needed to confirm the plant's therapeutic potential and explore additional applications. This review consolidates, for the first time, current chemical, and biological research on W. adpressa, with a focus on its most bioactive extracts, fractions, and compounds, aiming to support their development into phytopharmaceutical development.

(±)-Aquilarines G-L (1-6), undescribed racemic heteropolymers 2-phenylchromone-phenylpropanoid were isolated from the agarwood of Aquilaria sinensis, and chiral HPLC separation resulted in six pairs of optically pure compounds. The structures of racemates and their enantiomers were elucidated by spectroscopic methods and ECD calculations. Biological evaluation on renal fibrosis were carried out, revealing that the enantiomers of compounds (±)-3-(±)-5, especially (±)-4 and (±)-5, could reduce the expression of fibrotic markers fibronectin and collagen I in TGF-β1 induced NRK-52e cells. Interestingly, the dextro-isomers [(+)-4 and (+)-5] showed more prominent activities than laevo-isomers [(-)-4 and (-)-5].

Andrastin meroterpenoids and gregatin polyketides are two widely distributed classes of structurally distinct natural products (NPs); however, hybrids containing both frameworks, termed andrastin-gregatin hybrids (AGHs), remain exceptionally rare. In our search for anti-inflammatory NPs from natural sources, six AGHs (1-6) and three known monomers (7-9) were isolated from Penicillium sp. KYS-21, of which andragatins A-C (1-3) were identified as new compounds. All AGHs potently inhibit the production of nitric oxide (NO) in LPS-stimulated macrophages with IC₅₀ values within 10 μM, while the monomers are inactive. Andragatin A (1) suppresses inflammatory responses in vitro by concurrently inhibiting the NF-κB and MAPK pathways and exhibits dose-dependent anti-inflammatory activity in an LPS-induced zebrafish model. This work expands the chemical and biological diversity of the rare AGH family and highlights the hybrid scaffold as a promising pharmacophore for anti-inflammatory drug discovery.