Fitoterapia最新文献

In this study, the phytochemical profile of the roots and stems of Baliospermum yui was investigated for the first time, leading to the isolation of thirteen compounds, including four previously undescribed compounds: phenanthrene monomer baliosperol A (1) and heterodimer baliosperol B (2), and two tigliane-type diterpenoids baliospermins D-E (3-4). Their chemical structures were elucidated by 1D/2D NMR spectroscopy, HRESIMS, ECD calculations and GIAO NMR/DP4+ analysis. Compounds 1-12 were assessed in vitro for their inhibitory effects on nitric oxide (NO) production in lipopolysaccharide-induced RAW264.7 cells, and compounds 1, 2 and 5 showed moderate inhibitory activity with IC₅₀ values ranging from 21.83 ± 1.34 to 30.33 ± 1.48 μM. This study not only represents the first systematic chemical investigation of B. yui, but also highlights its potential as a rich source of tigliane-type diterpenoids.

A chemical investigation of Chloridium sp. P41, an endophytic fungus from Bufo melanostictus Schneider, led to the isolation of two new atranones (1-2). These complex metabolites feature a structural architecture, incorporating an eleven-membered ring fused to an enol-lactone moiety. Their structures were elucidated by comprehensive spectroscopic methods and single-crystal X-ray diffraction analysis. The analgesic activity of compounds 1 and 2 were evaluated using a zebrafish model. Specifically, compound 1 at 7.5 μM and compound 2 at 3.75 μM inhibited pain responses by 62.81 ± 8.57% and 57.30 ± 3.57%, respectively.

Cynaropicrin is a guaianolide-type sesquiterpene lactone primarily derived from plants within the Asteraceae family. Structurally, it features a distinctive 5-7-5 tricyclic framework, four exocyclic double bonds, and two hydroxyl groups. Due to its broad pharmacological activities, cynaropicrin garnered considerable scientific interest, with well-established protocols for its extraction and synthesis. Extensive studies have demonstrated that cynaropicrin exhibits remarkable antitumor activities by effectively inhibiting the proliferation of various malignancies, such as lung cancer, melanoma, and breast cancer. The underlying mechanisms are primarily associated with the regulation of cell cycle progression and apoptosis-related pathways. Moreover, cynaropicrin significantly enhances the efficacy of chemotherapeutic agents including temozolomide, cisplatin, and docetaxel, suggesting promising potential for combination therapy. Beyond its antitumor properties, cynaropicrin exhibits a broad spectrum of bioactivities, including antioxidant, antiviral, antiparasitic, and immunomodulatory effects, primarily via the modulation of signaling pathways like NF-κB. Structure-activity relationship (SAR) studies further indicate that the side chain, hydrophilicity of the OH-3 and OH-19 substituents, and the C17-C18 exo-olefin structure critically influence its NF-κB inhibitory activity. This review comprehensively synthesizes current knowledge regarding the mechanisms of action and SAR insight of cynaropicrin across various pathophysiological processes, evaluates its prospects for clinical application, and aims to provide a foundational framework to guide future research and development efforts involving this compound.

A phytochemistry investigation on the aerial parts of medicinal plant Sigesbeckia pubescens led to the discovery of three new ent-pimarane diterpenoids, sigesbecenes A-C (1-3), along with ten known analogues (4-13). The chemical structures of the new compounds were elucidated based on extensive spectroscopic techniques, chemical method, electronic circular dichroism (ECD) analysis, and single-crystal X-ray diffraction analysis. Among the isolates, compounds 1, 2, 4, 10, and 13 showed potential in vitro anti-vascular endothelial injury activity in oxidized low-density lipoprotein (ox-LDL)-induced human vein endothelial cells (HUVECs).

Astragalus membranaceus is used in traditional Chinese medicine for neuroinflammation-related conditions like ischemic stroke and Alzheimer's disease. A phytochemical investigation of its roots led to the isolation of three previously undescribed compounds, astragalusmonol A (1), astragalusmonosides A and B (2-3), along with seventeen known compounds (4-20). Their structures were confirmed by HRESIMS, NMR, IR, UV, electronic circular dichroism (ECD) calculations, X-ray crystallography, and chemical hydrolysis. All isolates were evaluated for anti-neuroinflammatory activity in lipopolysaccharide (LPS)-induced BV2 microglia. Fifteen of them exhibited significant activity, with compounds 12, 6, and 1 showing particularly potent effects (IC₅₀ values of 3.74, 9.71, and 26.47 μM, respectively). The most active compound, 12, also significantly attenuated thrombus formation in a zebrafish cerebral thrombosis model. This study not only enriches the chemical diversity of Astragalus membranaceus but also highlights the active compounds, notably compound 12, as promising candidates for targeting neuroinflammatory disorders.

Eight previously undescribed acetylenic acids (1-8) and one known acetylenic acid (9) were firstly isolated from Malania oleifera seed meal. The absolute configurations were determined by extensive spectral analysis, the bulkiness rule, and NMR calculations. All compounds were evaluated for their inhibitory effects on lipid accumulation in oleic acid (OA)-induced 3 T3-L1 cells. The results showed that compounds 1 and 2 exhibited moderate anti-adipogenesis effects than the positive control (LiCl, 10 mM), with IC₅₀ values of 40.45 μM and 25.20 μM, respectively.

The Yaobitong Capsule (YBTC) is a notable traditional Chinese medicine employed in the treatment of lumbar disc herniation (LDH). However, its therapeutic effective components are not well understood. This study aimed to systematically elucidate its pharmacodynamic basis by integrating comprehensive chemical analysis, bioactivity prediction, and experimental validation. Through UPLC-Q-TOF-MS analysis, 137 chemical constituents were tentatively identified in YBTC. Subsequent network pharmacology and molecular docking studies were conducted to prioritize candidate bioactive compounds, while serum pharmacochemistry analysis identified the components that were systematically absorbed. The analysis identified that four blood-entering components overlapped with the top predicted 25 effective components, specifically tetrahydropalmatine (Thp), corydaline, angelol A, and ligustilide. Among these, Thp exhibited the highest relative abundance in the bloodstream and demonstrated the strongest molecular docking affinity with the core targets. Furthermore, preliminary in vivo efficacy evaluations indicated that Thp possesses significant analgesic and tissue-protective properties, establishing it as the core pharmacodynamic component for further investigation. The findings suggest that Thp exerts neuroprotective and analgesic effects by inhibiting the activation of the p38 MAPK signaling pathway. Additionally, Thp significantly down-regulates the expression of key inflammatory mediators, such as iNOS and COX-2, as well as matrix metalloproteinases (MMPs), thereby producing synergistic pharmacological effects, including anti-inflammatory actions and inhibition of extracellular matrix degradation. In conclusion, this study systematically elucidates the pharmacodynamic effective components of YBTC in the treatment of LDH and identifies Thp as one of its principal active components.

Seven novel 2-(2-phenylethyl)chromone-sesquiterpene hybrids (1-7) were successfully isolated from the ethanol extract of Hainan agarwood of Aquilaria sinensis under HPLC-MS guidance. Their structures were determined by extensive spectroscopic analysis, including 1D and 2D NMR, HRESIMS, IR, and experimental and computed ECD data. Their anti-inflammatory, cytotoxic, and anti-Helicobacter pylori activities were evaluated. Compounds 1-4 demonstrated significant suppression of nitric oxide production in LPS-stimulated RAW264.7 cells, with IC₅₀ values ranged of 7.25-10.42 μM. Compounds 1-3, 5, 7 showed anti-H. pylori activity with MIC value of 20 μM, 4 and 6 exhibited MIC values of 40 μM. And every compound exhibited significant cytotoxicity in all five (K562, BEL-7402, SGC-7901, Hela and A549) human cancer cell lines examined, displaying overall IC₅₀ value is between 16.77 ± 0.21 to 47.58 ± 0.27 μM, demonstrating broad-spectrum anticancer potential.

Aim of study: Doxorubicin (Dox), as a common chemotherapeutic agent, induces cardiotoxicity by driving mitochondrial dysfunction and energy insufficiency. Yiqi Wenyang Formula (YQWYF) is an empirical prescription frequently used for treating heart failure (HF). This study aims to illustrate the therapeutic efficacy of YQWYF in treating Dox-induced cardiotoxicity, and the underlying mechanism.

Materials and methods: Dox-induced cardiotoxicity was modeled in mice and H9c2 cells. Active compounds of YQWYF-loaded heart tissues and YQWYF dry powder were screened by liquid chromatography-tandem mass spectrometry (LC-MS/MS). Morphological and functional changes in mitochondria of Dox-induced mice and H9c2 cells were examined via a series of examinations, including echocardiography, histological staining, transmission electron microscopy (TEM), Seahorse assay, JC-1 staining, and ATP content measurement. The regulatory effect of YQWYF on the SIRT1/PGC-1α signaling pathway was detected by Western blot, immunohistochemistry and immunofluorescence staining. Molecular docking of active compounds of YQWYF to SIRT1 was finally performed.

Results: Dox induction significantly resulted in ventricular remodeling, ultrastructural changes in myocardial mitochondria, and ATP decline in mouse heart tissues. Similarly, Dox treatment significantly decreased the viability of H9c2 cells by 25%, which also impaired the mitochondrial ultrastructure, mitochondrial membrane potential (MMP) and ATP production in vitro. YQWYF significantly reversed Dox-induced mitochondrial dysfunction and ATP depletion in mouse heart tissues and H9c2 cells by activating the SIRT1/PGC-1α signaling pathway. A total of 28 active compounds of YQWYF were identified, showing strong binding affinities to SIRT1.

Conclusion: YQWYF protects against Dox-induced cardiotoxicity by activating the SIRT1/PGC-1α signaling pathway.

Platycodin D is a triterpenoid saponin from Platycodon grandiflorus (balloon flower) that has emerged as a promising natural anticancer lead. This review synthesizes current evidence on its antitumor pharmacology and translational development, with emphasis on signaling mechanisms, active derivatives, bioanalytical quantification, and ADME/pharmacokinetics. Platycodin D suppresses tumor growth by engaging multiple cancer hallmarks, including induction of apoptosis and other programmed cell-death programs, inhibition of proliferation, and attenuation of invasion and metastasis. These effects are mediated, in part, through modulation of key oncogenic and stress-response pathways such as PI3K/Akt, NF-κB, and MAPK, alongside broader impacts on inflammatory and immune-regulatory networks. We further summarize structure-activity relationships and reported semisynthetic/natural analogs that inform lead optimization, as well as available evidence for chemosensitization and reversal of drug-resistance phenotypes in preclinical models. In addition, we overview current LC-MS/MS-based methods for bioanalysis of platycodin D in biological matrices and critically discuss major translational liabilities, including low oral bioavailability and ADME determinants (e.g., limited permeability, efflux, and metabolism), together with enabling formulation and delivery strategies. Collectively, the data support platycodin D as a multi-target anticancer scaffold while underscoring the need for rigorous in vivo validation, standardized pharmacokinetic characterization, safety evaluation, and well-designed clinical studies to define its therapeutic potential.