Fitoterapia最新文献

Medicinal plants synthesize valuable active components, including terpenoids, alkaloids, and flavonoids, which exhibit significant potential for treating chronic diseases and immune disorders. The biosynthesis of these compounds is often regulated by bHLH transcription factors, a large and evolutionarily conserved family of regulatory proteins in plants. This review focuses on summarizing the research from the past decade concerning the roles of bHLH TFs in the biosynthesis of these bioactive compounds. It outlines the key regulatory networks within terpenoid, alkaloid, and flavonoid pathways, thereby enhancing our understanding of secondary metabolism and providing a basis for improving natural product yields.

Current antithrombotic therapies are associated with significant side effects, including gastrointestinal and intracranial bleeding, as well as interactions with diet and other medications. These limitations underscore the need for safer, more effective alternatives. Given the conservation of coagulation and platelet activation pathways between zebrafish and mammals, we investigated the utility of zebrafish as an in vivo model for screening plant-derived compounds with anti-platelet activity. Unlike conventional in vitro platelet aggregation assays, this approach allows simultaneous assessment of biological activity and systemic toxicity. A total of 41 plant tissue extracts were screened using a zebrafish-based thrombocyte aggregation assay, with five extracts showing significant inhibition of ADP-induced thrombocyte activation. These findings were validated using human whole blood impedance aggregation assays. Active extracts were then subjected to chromatographic fractionation, and select fractions retaining anti-platelet activity were further analyzed. From these, three compounds were isolated in sufficient quantity for structure elucidation using mass spectrometry and nuclear magnetic resonance spectroscopy. Structural analysis revealed three related compounds, two of which represent novel inhibitors of ADP-mediated platelet aggregation. This study highlights the zebrafish as a powerful platform for the in vivo screening of natural product libraries for antithrombotic agents and identifies two previously unreported plant-derived compounds with promising anti-platelet properties.

Saposhnikoviae Radix is commonly used in clinical practice to treat conditions such as the common cold, rheumatism, and pruritus caused by wind rash. However, the pharmacological mechanisms of its active constituents underlying the anti-inflammatory and immunomodulatory effects remain unclear. This study aimed to characterize the chemical constituent groups, including the alcohol supernatant, chromone-rich fraction, polysaccharides, and volatile oils of Saposhnikoviae Radix, using UPLC-MS and GC-MS, and investigate their anti-inflammatory and immunomodulatory effects in vitro and in vivo. Phytochemical analysis identified a total of 66, 32, and 113 major compounds in the alcohol supernatant, chromone-rich fraction, and volatile oil, respectively. Key chromones from Saposhnikoviae Radix, such as prim-O-hexosylcimifugin and 5-O-methylvisammioside, were characterized. The chromone-rich fraction and alcohol supernatant encompassed chromones, amino acids, organic acids, and coumarins, with key constituents including cimifugin and 3'-O-angeloylhamaudol identified. The volatile oil fraction comprised hydrocarbons, terpenes, aldehydes, ketones, and esters. A TNF-α/IFN-γ-induced HaCaT cell model was established. The results demonstrated that all constituent groups significantly reduced the concentrations of IL-1β, IL-6, IL-8, TARC, and MDC in a dose-dependent manner, while improving cell morphology. A murine model of atopic dermatitis (AD) was induced in BALB/C mice using 2,4-Dinitrochlorobenzene (DNCB). The findings revealed that the alcohol supernatant and polysaccharides from Saposhnikoviae Radix reduced mast cell infiltration, decreased serum IgE levels, and lowered IL-4 levels in the skin tissue of AD mice. These findings elucidated the potential mechanism of Saposhnikoviae Radix in treating AD and provided a theoretical and experimental basis for the material foundation of its therapeutic effects.

Magnolia officinalis Rehder et Wilson (MRW) is a traditional herbal medicine with well-documented anti-inflammatory and antioxidative properties, yet its molecular basis in cancer therapy remains incompletely defined. This study aimed to elucidate the multi-target anticancer potential of MRW against pancreatic cancer through integrated in vitro and in silico analyses. LC-MS/MS profiling identified honokiol and magnolol as the major bioactive constituents, confirmed by retention time and UV spectra. MRW treatment suppressed cell viability and induced apoptosis in PANC-1 and MIA PaCa-2 cells by promoting reactive oxygen species (ROS) generation, mitochondrial membrane potential (∆Ψm) depolarization, and caspase activation, while sparing normal epithelial cells. Mechanistically, MRW inhibited DNA methyltransferase 1 (DNMT-1) and JAK2/STAT3 signaling while restoring undifferentiated embryonic cell transcription factor 1 (UTF-1) and miR-148a-3p expression, thereby reversing the epigenetic silencing and ROS overproduction characteristic of pancreatic cancer cells. Molecular docking further demonstrated strong binding affinities of honokiol, magnolol, and magnolin toward DNMT-1, UTF-1, STAT3, JAK2, IL-6, and Survivin, forming stable hydrogen-bond and π-π stacking interactions within catalytic pockets. These interactions suggest that MRW constituents' function as non-nucleoside DNMT-1 inhibitors and ROS-immune modulators that disrupt oncogenic feedback loops and re-activate apoptotic pathways. Collectively, these findings identify MRW as a multi-target phytomedicine integrating ROS-mediated oxidative stress, epigenetic remodeling, and immune-apoptotic signaling, supporting its translational potential as a low-toxicity adjunct strategy to conventional pancreatic cancer therapies.

Three previously undescribed sesquiterpenes, including one germacrane-type (1) and two guaiane-type (2 and 3), along with eighteen known sesquiterpenes (4-21), were isolated from the secondary rhizomes of Curcuma wenyujin. The structures of 1-3 were elucidated through comprehensive spectroscopic analysis, which integrated 1D/2D-NMR spectroscopic, high-resolution mass spectrometry (HRMS), electronic circular dichroism (ECD) spectra, and single-crystal X-ray diffraction (SC-XRD), together with DFT NMR calculations. Compounds 1-3 were evaluated for inhibitory effects on lipid accumulation in palmitic acid and oleic acid (PA/OA)-induced AML12 hepatocytes, and 3 exhibited a moderate inhibitory effect.

Rhododendron molle (Blume) G. Don is a plant of great significance in traditional Chinese medicine, particularly valued for its analgesic properties. This review systematically consolidates contemporary research on its phytochemistry, pharmacology, and structure-activity relationships. Over 200 compounds have been identified, with diterpenoids-notably those featuring 12 novel carbon skeletons-recognized as the principal bioactive and toxic constituents. These compounds underpin the plant's broad pharmacological profile, including marked anti-inflammatory, immunomodulatory, and potent antinociceptive activities. A central contribution of this review is a critical structure-activity relationships analysis that systematically identifies key functional groups (e.g., the C-2 and C-3 hydroxyls) as pivotal for the antinociceptive efficacy of grayanane diterpenoids. Promising lead compounds, such as Rhodojaponin III, are highlighted for their potential in developing new therapeutics for rheumatoid arthritis and neuropathic pain, as well as natural insecticides. By integrating traditional knowledge with modern science, this review not only validates the traditional uses of R. molle but also provides a foundational framework for future research, explicitly pointing to the need for in-depth mechanistic studies, comprehensive toxicity profiling, and rational drug development.

A new lupane- type triterpenoid and a new tirucallane- type nortriterpenoid, pekinenolone A (1) and pekinensin A (2), were isolated from the roots of Euphorbia pekinensis along with six known compounds (3-8). Their structures were established by spectroscopic analysis, NMR and ECD calculations, revealing 1 as the first new 13(18)-en-12,22-dione lupane-type triterpenoid. In anti-hepatocellular carcinoma (HCC) screenings, (3β,11β)-3,11-dihydroxylanosta-8,24-dien-7-one (8) exhibited potent cytotoxicity against Hepa1-6 cells (IC₅₀ = 4.29 ± 0.48 μM), while 1 was moderately active. Importantly, all isolates showed high selectivity, with no significant toxicity toward non-tumorigenic hepatocytes. The active compounds, 1 and 8, were found to induce apoptosis via caspase 3/7 activation. Furthermore, compound 8 inhibited cell metastasis in vitro and suppressed tumor growth in vivo, establishing it as a promising and selective lead structure for the development of new anti-HCC agents.

Background: The phagocytic function of macrophages is pivotal in regulating vascular inflammation and the progression of atherosclerosis (AS). Si-Miao-Yong-An Decoction (SMYAD), a traditional Chinese multi-herbal remedy, has been used in the treatment of vascular inflammation and AS. However, its impact on the phagocytic activity of macrophages remains unexplored.

Methods: ApoE^-/- mice were divided into normal control groups. Model, SMYAD-treated (35.1 or 70.2 g/kg), colchicine-treated (0.102 m g/kg) (n = 6), and fed a high-fat diet (HFD) for 10 weeks in vivo. Several parameters were assessed, including aortic plaque area, lipid accumulation, inflammatory cytokine levels, and macrophage efferocytosis. Potential core targets of SMYAD in restoring macrophage efferocytosis were predicted through network pharmacology. In vitro, RAW264.7 macrophages were exposed to oxidized low-density lipoprotein (ox-LDL) and SMYAD-containing serum. Macrophage efferocytosis was evaluated via Western blot (WB), RT-qPCR, and co-culture assays with apoptotic cells. Predicted targets were further validated through in vitro experiments.

Results: SMYAD reduced lipid deposition and plaque area in ApoE^-/- mice, lowered the levels of inflammatory cytokines, and restored macrophage efferocytosis. Network pharmacology analysis identified PPAR-γ as the key mediator of SMYAD's effects on macrophage efferocytosis. In cell-based assays, SMYAD upregulated MerTK expression, enhanced macrophage efferocytosis, and, through siRNA interference, confirmed that this effect is mediated via the PPAR-γ pathway.

Conclusions: This study, combining in vivo and in vitro experiments with network pharmacology, elucidates that SMYAD restores macrophage efferocytosis and mitigates vascular inflammation via the PPAR-γ/MerTK signaling pathway, offering potential therapeutic benefits for AS.

The increasing use of herbal electronic cigarettes raises concerns regarding their biological impact beyond conventional nicotine delivery. Although marketed as "natural" alternatives, their phytochemical vapors interact with molecular pathways that may influence respiratory health. This review summarizes current evidence on the molecular crosstalk between herbal phytochemicals and microRNAs (miRNAs) in the context of electronic cigarette vapor exposure, emphasizing their roles in oxidative stress, inflammation, and tissue remodelling. Literature was systematically examined to evaluate in vitro, in vivo, and bioinformatics findings on phytochemicals commonly incorporated in herbal e-liquids. Key molecular pathways (NF-κB, Nrf2/HO-1, MAPK, PI3K/Akt/mTOR, and TGF-β/Smad) and miRNA regulators were analyzed to elucidate mechanisms of lung injury and protection. The search strategy involved PubMed, Web of Science, and Scopus databases, using the keywords "herbal e-liquid," "phytochemicals," "lung injury," "miRNA," and "molecular pathway." Evidence indicates that bioactive phytochemicals such as quercetin, linalool, and EGCG can modulate the expression of miRNAs (e.g., miR-21, miR-146a, miR-155, miR-210), thereby regulating inflammatory and oxidative responses. Crosstalk between these phytochemicals and miRNAs contributes to dual effects: mitigating reactive oxygen species and cytokine overproduction, while in some cases promoting pro-inflammatory or fibrotic signalling under chronic exposure. This bidirectional modulation highlights the complex balance between potential therapeutic benefits and risks of herbal vapor inhalation. Herbal electronic cigarettes cannot be considered risk-free. Their phytochemicals engage in intricate interactions with miRNA networks and molecular pathways that may influence respiratory health. Understanding this molecular crosstalk is essential for evaluating safety, guiding regulatory strategies, and identifying therapeutic prospects of phytochemical-based inhalation systems.

Cancer stem cells (CSCs) play a pivotal role in cancer initiation, development, metastasis, and recurrence. They exhibit inherent resistance to conventional chemotherapy, posing a significant challenge to the complete eradication of tumors. Traditional Chinese medicine (TCM) and its bioactive compounds exhibit remarkable potential in selectively targeting cancer stem cells owing to their low toxicity and ability to regulate multiple molecular targets. In this review, we provide a comprehensive analysis of the biological characteristics of cancer stem cells and their role in tumor initiation and progression. We also evaluate therapeutic strategies targeting cancer stem cells and recent core molecular mechanisms, and highlight their limitations. Additionally, we explore the molecular mechanisms through which TCM active components (such as curcumin, berberine, and resveratrol) effectively target cancer stem cells via seven distinct pathways, as well as the multi-level, multi-mechanistic targeting of TCM on CSCs. Furthermore, we propose fabricating nanomedicines to solve the challenges of low bioavailability and insufficient targeting of active components in TCM. These nanomedicines, such as physically loaded nanomedicines, covalently coupled nanomedicines, and self-assembled nanomedicines, can precisely target drugs, enhance stability, and promote the synergistic effect of multiple components, thereby significantly improving the clearance efficiency of cancer stem cells. Finally, we explore the potential of intelligent-responsive nanomedicines and multimodal combination therapies in addressing tumor heterogeneity and advancing clinical translation. This will provide a theoretical foundation and methodological framework for integrating traditional medicine with modern technology.