1.Therapeutic effects of natural products on animal models of chronic obstructive pulmonary disease.
Xinru FEI ; Guixian YANG ; Junnan LIU ; Tong LIU ; Wei GAO ; Dongkai ZHAO
Journal of Central South University(Medical Sciences) 2025;50(6):1067-1079
Chronic obstructive pulmonary disease (COPD) currently lacks effective treatments to halt disease progression, making the search for preventive and therapeutic drugs a pressing issue. Natural products, with their accessibility, affordability, and low toxicity, offer promising avenues. Investigating the pharmacological effects and related signaling mechanisms of active components from natural products on COPD animal models induced by various triggers has become an important focus. In animal models induced by cigarette smoke, cigarette smoke combined with lipopolysaccharide (LPS), air pollution, elastase, bacterial or viral infections, the active compounds of natural products, such as flavonoids, terpenoids, and phenolics, can exert anti-inflammatory, antioxidant, mucus-regulating, and airway remodeling-inhibiting effects through key signaling pathways including nuclear factor-erythroid 2-related factor 2 (Nrf2)/heme oxygenase-1 (HO-1), nuclear factor-kappa B (NF-κB), and mitogen-activated protein kinase (MAPK). These findings not only provide a theoretical basis for the clinical diagnosis and treatment of COPD but also point to new directions for future scientific research.
Pulmonary Disease, Chronic Obstructive/etiology*
;
Animals
;
Disease Models, Animal
;
Biological Products/pharmacology*
;
Humans
;
NF-kappa B/metabolism*
;
Flavonoids/pharmacology*
;
Signal Transduction/drug effects*
;
Anti-Inflammatory Agents/pharmacology*
;
Heme Oxygenase-1/metabolism*
;
Terpenes/pharmacology*
;
Antioxidants/pharmacology*
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NF-E2-Related Factor 2/metabolism*
;
Smoke/adverse effects*
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Phenols/therapeutic use*
2.Applications of bioactive peptides in cosmeceuticals: a review.
Journal of Zhejiang University. Science. B 2025;26(6):527-545
The cosmetic sector is a multibillion-dollar industry that requires constant attention being paid to innovative product development and engagement. Notably, its market value is projected to exceed 750 billion U.S. dollars by 2025, and it is expanding as novel, climate-friendly, green, and sustainable components from natural sources are incorporated. This review is written based on the numerous reports on the potential applications of food-derived peptides while focusing on their possible uses in the formulation of cosmeceutical and skincare products. First, the production methods of bioactive peptides linked to cosmeceutical uses are described. Then, we discuss the obtainment and characterization of different anti-inflammatory, antimicrobial, antioxidant, anti-aging, and other pleiotropic peptides with their specific mechanisms, from various food sources. The review concludes with salient considerations of the cost of production and pilot scale operation, stability, compatibility, user safety, site-specificity, and delivery methods, when designing or developing biopeptide-based cosmeceutical products.
Cosmeceuticals/chemistry*
;
Peptides/pharmacology*
;
Humans
;
Antioxidants/pharmacology*
;
Anti-Inflammatory Agents/pharmacology*
;
Anti-Infective Agents/pharmacology*
;
Cosmetics
;
Skin Aging/drug effects*
3.EGCG as a therapeutic agent: a systematic review of recent advances and challenges in nanocarrier strategies.
Chee Ning WONG ; Yang Mooi LIM ; Kai Bin LIEW ; Yik-Ling CHEW ; Ang-Lim CHUA ; Siew-Keah LEE
Journal of Zhejiang University. Science. B 2025;26(7):633-656
Epigallocatechin-3-gallate (EGCG), a bioactive polyphenol abundant in green tea, has garnered significant attention for its diverse therapeutic applications, ranging from antioxidant and anti-inflammatory effects to potential anticancer properties. Despite its immense promise, the practical utilization of EGCG in therapeutic settings as a medication has been hampered by inherent limitations of this drug, including poor bioavailability, instability, and rapid degradation. This review comprehensively explores the current challenges associated with the application of EGCG and evaluates the potential of nanoparticle-based formulations in addressing these limitations. Nanoparticles, with their unique physicochemical properties, offer a platform for the enhanced stability, bioavailability, and targeted delivery of EGCG. Various nanoparticle strategies, including polymeric nanoparticle, micelle, lipid-based nanocarrier, metal nanoparticle, and silica nanoparticle, are currently employed to enhance EGCG stability and pharmacological activity. This review concludes that the particle sizes of most of these formulated nanocarriers fall within 300 nm and their encapsulation efficiency ranges from 51% to 97%. Notably, the pharmacological activities of EGCG-loaded nanoparticles, such as antioxidative, anti-inflammatory, anticancer, and antimicrobial effects, are significantly enhanced compared to those of free EGCG. By critically analyzing the existing literature and highlighting recent advancements, this article provides valuable insights into the promising prospects of nanoparticle-mediated EGCG formulations, paving the way for the development of more effective and clinically viable therapeutic strategies.
Animals
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Humans
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Anti-Inflammatory Agents/administration & dosage*
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Antineoplastic Agents/administration & dosage*
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Antioxidants/administration & dosage*
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Biological Availability
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Catechin/analogs & derivatives*
;
Micelles
;
Particle Size
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Nanoparticle Drug Delivery System/chemistry*
4.Comparison of anti-inflammatory, antibacterial and analgesic activities of formulated granules versus traditional decoction of Yinqiao Powder.
Zhuolin GUO ; Zhiheng ZHANG ; Xindeng GUO ; Weiwei YANG ; Zhiqing LIANG ; Jinying OU ; Huihui CAO ; Zibin LU ; Linzhong YU ; Junshan LIU
Journal of Southern Medical University 2025;45(5):1003-1012
OBJECTIVES:
To compare the anti-inflammatory, antibacterial and analgesic effects of Yinqiao Powder (YQS) formulated granules and decoction.
METHODS:
We first evaluated the anti-inflammatory effects of the two dosage forms of YQS in a LPS-induced RAW 264.7 cell model using RT-qPCR and Western blotting. We further constructed zebrafish models of inflammation by copper sulfate exposure, caudal fin transection, or LPS and Poly (I:C) microinjection, and evaluated anti-inflammatory effects of YQS granules and decoction by examining neutrophil aggregation and HE staining findings. In a mouse model of acute lung injury (ALI) induced by intratracheal LPS instillation, the effects of YQS gavage at 10, 15, and 20 g/kg on lung pathologies were evaluated by calculating lung wet-dry weight ratio and using HE staining, ELISA and Western blotting. The microbroth dilution method was used to evaluate the antibacterial effect of YQS. Mouse pain models established by hot plate and intraperitoneal injection of glacial acetic acid were used to evaluate the analgesic effects of YQS at 10, 15, and 20 g/kg.
RESULTS:
Both YQS granules and decoction significantly reduced TNF-α, IL-6, and IL-1β expressions and p-STAT3 (Tyr 705) phosphorylation level in LPS-induced RAW 264.7 cells, and obviously inhibited neutrophil aggregation in the zebrafish models. In ALI mice, YQS granules and decoction effectively ameliorated lung injury, lowered lung wet-dry weight ratio, and reduced p-STAT3 (Tyr 705) expression and TNF-α and IL-6 levels. YQS produced obvious antibacterial effect at the doses of 15.63 and 31.25 mg/mL, and significantly reduced body torsion and increased pain threshold in the mouse pain models.
CONCLUSIONS
The two dosage forms of TQS have similar anti-inflammatory, antibacterial and analgesic effects with only differences in their inhibitory effect on TNF-α, IL-6 and IL-1β mRNA expressions in LPS-induced RAW 264.7 cells.
Animals
;
Mice
;
Drugs, Chinese Herbal/pharmacology*
;
Anti-Inflammatory Agents/pharmacology*
;
Analgesics/pharmacology*
;
RAW 264.7 Cells
;
Zebrafish
;
Anti-Bacterial Agents/pharmacology*
;
Powders
;
Tumor Necrosis Factor-alpha/metabolism*
;
Acute Lung Injury/drug therapy*
;
Interleukin-6/metabolism*
;
Lipopolysaccharides
5.Research progress on the potential mechanisms and effects of the cholinergic anti-inflammatory pathway in sepsis.
Chinese Critical Care Medicine 2025;37(4):397-401
Sepsis is a common clinical syndrome in intensive care unit (ICU) with high morbidity and high mortality, making it a global health issue. The estimated global incidence of sepsis is 437/100 000, with an in-hospital mortality of 17%, which is higher in developing countries and underdeveloped regions. Despite some progress in sepsis treatment in recent years, the complexity of its pathophysiology limits therapeutic effectiveness. The cholinergic anti-inflammatory pathway (CAP), a neuro-immune regulatory pathway, plays a crucial role in sepsis through key components such as the vagus nerve, central M-type muscarinic receptor, the spleen and splenic sympathetic nerves, acetylcholine, and the α7 subunit of the nicotinic acetylcholine receptor (α7nAChR). This article explores the potential mechanisms and roles of CAP in sepsis, focusing on CAP-related cell signaling pathways, including nuclear factor-κB (NF-κB) signaling pathway, Janus kinase/signal transducer and activator of transcription 3 (JAK/STAT3) signaling pathway, phosphatidylinositol 3-kinase/protein kinase B (PI3K/Akt) signaling pathway, and cyclooxygenase (COX) and prostaglandin E2 (PGE2) signaling pathways. Potential applications of CAP in sepsis treatment include stimulating the vagus nerve (e.g., through pharmacological, electrical, or acupuncture stimulation), using α7nAChR agonists (e.g., nicotine, GTS-21, and PNU-282987), adrenergic receptor agonists (e.g., dexmedetomidine and salbutamol), or other drugs and bioactive substances (e.g., buprenorphine and traditional Chinese medicine components). These approaches aim to activate CAP, suppress inflammatory responses, and improve sepsis prognosis, providing a theoretical basis for treatment and promoting the development of related drugs.
Sepsis/metabolism*
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Humans
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Signal Transduction
;
alpha7 Nicotinic Acetylcholine Receptor
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NF-kappa B/metabolism*
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Anti-Inflammatory Agents
;
Acetylcholine
6.Curvularin derivatives from hydrothermal vent sediment fungus Penicillium sp. HL-50 guided by molecular networking and their anti-inflammatory activity.
Chunxue YU ; Zixuan XIA ; Zhipeng XU ; Xiyang TANG ; Wenjuan DING ; Jihua WEI ; Danmei TIAN ; Bin WU ; Jinshan TANG
Chinese Journal of Natural Medicines (English Ed.) 2025;23(1):119-128
Guided by molecular networking, nine novel curvularin derivatives (1-9) and 16 known analogs (10-25) were isolated from the hydrothermal vent sediment fungus Penicillium sp. HL-50. Notably, compounds 5-7 represented a hybrid of curvularin and purine. The structures and absolute configurations of compounds 1-9 were elucidated via nuclear magnetic resonance (NMR) spectroscopy, X-ray diffraction, electronic circular dichroism (ECD) calculations, 13C NMR calculation, modified Mosher's method, and chemical derivatization. Investigation of anti-inflammatory activities revealed that compounds 7-9, 11, 12, 14, 15, and 18 exhibited significant suppressive effects against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in murine macrophage RAW264.7 cells, with IC50 values ranging from 0.44 to 4.40 μmol·L-1. Furthermore, these bioactive compounds were found to suppress the expression of inflammation-related proteins, including inducible NO synthase (iNOS), cyclooxygenase-2 (COX-2), NLR family pyrin domain-containing protein 3 (NLRP3), and nuclear factor kappa-B (NF-κB). Additional studies demonstrated that the novel compound 7 possessed potent anti-inflammatory activity by inhibiting the transcription of inflammation-related genes, downregulating the expression of inflammation-related proteins, and inhibiting the release of inflammatory cytokines, indicating its potential application in the treatment of inflammatory diseases.
Penicillium/chemistry*
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Mice
;
Animals
;
Anti-Inflammatory Agents/isolation & purification*
;
RAW 264.7 Cells
;
Nitric Oxide/metabolism*
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Hydrothermal Vents/microbiology*
;
Macrophages/immunology*
;
Molecular Structure
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Nitric Oxide Synthase Type II/immunology*
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Cyclooxygenase 2/immunology*
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Geologic Sediments/microbiology*
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NF-kappa B/immunology*
;
NLR Family, Pyrin Domain-Containing 3 Protein/immunology*
7.Xanthones from Garcinia pedunculata and Garcinia nujiangensis and their anti-inflammatory activity.
Xiaojie FAN ; Yufeng JIA ; Jiaxin GUO ; Jinyuan YANG ; Dahong LI ; Huiming HUA
Chinese Journal of Natural Medicines (English Ed.) 2025;23(2):225-233
Ten novel xanthones, garpedunxanthones A-G (1-5, 6a/6b, 7a/7b) and nujiangxanthone Q (8), along with sixteen known analogs (9-24), were isolated from Garcinia pedunculata and G. nujiangensis. Their structures were elucidated through high-resolution electrospray ionization mass spectrometry (HR-ESI-MS) data, comprehensive nuclear magnetic resonance (NMR) spectroscopic analyses, and electronic circular dichroism (ECD) calculations. All compounds without cytotoxicity were assessed for anti-inflammatory properties by measuring the inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW264.7 cells. Structure-activity relationships are also discussed. Compounds 7b, 19, and 21 exhibited significant anti-inflammatory activity with IC50 values of 16.44 ± 0.69, 14.28 ± 0.78, and 10.67 ± 3.28 μmol·L-1, respectively. Enzyme-linked immunosorbent assay (ELISA) demonstrated that compounds 7b, 19, and 21 inhibited the expression of pro-inflammatory cytokines TNF-α and IL-6 in a dose-dependent manner. The inhibitory effect of compound 21 on IL-6 at 20 μmol·L-1 was comparable to that of the positive control. In network pharmacology studies, potential targets of compounds and inflammation were identified from PharmMapper and GeneCards databases. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analysis revealed that the overlapped targets were intricately associated with major pathogenic processes linked to inflammation, including positive regulation of mitogen-activated protein kinase (MAPK) cascade, protein kinase activity, NO synthase regulator activity, MAPK signaling pathway, and EGFR tyrosine kinase inhibitor resistance.
Xanthones/therapeutic use*
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Garcinia
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Anti-Inflammatory Agents/therapeutic use*
;
Plant Preparations/therapeutic use*
;
Structure-Activity Relationship
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Nitric Oxide/metabolism*
;
RAW 264.7 Cells
;
Animals
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Mice
;
Enzyme-Linked Immunosorbent Assay
;
Mitogen-Activated Protein Kinase Kinases/metabolism*
;
Circular Dichroism
8.Ent-pimarane and ent-kaurane diterpenoids from Siegesbeckiapubescens and their anti-endothelial damage effect in diabetic retinopathy.
Mengjia LIU ; Tingting LUO ; Rongxian LI ; Wenying YIN ; Fengying YANG ; Di GE ; Na LIU
Chinese Journal of Natural Medicines (English Ed.) 2025;23(2):234-244
Diabetic retinopathy, a prevalent and vision-threatening microvascular complication of diabetes mellitus, is the leading cause of blindness among middle-aged and elderly individuals. Natural diterpenoids isolated from Siegesbeckia pubescens demonstrate potent anti-inflammatory properties. This study aimed to identify novel bioactive diterpenoids from S. pubescens and investigate their effects on oxidative stress and inflammatory responses in diabetic retinopathy, both in vitro and in vivo. Three new ent-pimarane-type diterpenoids (1-3) and six known compounds (4-9) were isolated from the aerial parts of S. pubescens. Their structures were elucidated through spectroscopic data interpretation, and absolute configurations were determined by comparing calculated and experimental electronic circular dichroism (ECD) spectra. Among these compounds, 14β,16-epoxy-ent-3β,15α,19-trihydroxypimar-7-ene (5) exhibited the most potent protective effect against high glucose and interleukin-1β (IL-1β)-stimulated human retinal endothelial cells. Mechanistically, compound 5 promoted endothelial cell survival while ameliorating oxidative stress and inflammatory response in diabetic retinopathy, both in vivo and in vitro. These findings not only suggest that diterpenoids such as compound 5 are important anti-inflammatory constituents in S. pubescens, but also indicate that compound 5 may serve as a lead compound for preventing or treating vascular complications associated with diabetic retinopathy.
Diabetic Retinopathy/metabolism*
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Humans
;
Oxidative Stress/drug effects*
;
Animals
;
Diterpenes, Kaurane/administration & dosage*
;
Asteraceae/chemistry*
;
Male
;
Endothelial Cells/drug effects*
;
Abietanes/administration & dosage*
;
Molecular Structure
;
Mice
;
Anti-Inflammatory Agents/chemistry*
;
Plant Extracts/chemistry*
;
Mice, Inbred C57BL
9.The prospect and underlying mechanisms of Chinese medicine in treating periodontitis.
Aili XING ; Feng WANG ; Jinzhong LIU ; Yuan ZHANG ; Jingya HE ; Bin ZHAO ; Bin SUN
Chinese Journal of Natural Medicines (English Ed.) 2025;23(3):269-285
Inflammation represents a critical immune response triggered by cellular activities and inflammatory mediators following tissue damage. It plays a central role in the pathological progression of diverse diseases, including psychiatric disorders, cancer, and immunological conditions, rendering it an essential target for therapeutic intervention. Periodontitis, a prevalent oral inflammatory disease, is a leading cause of tooth loss and poses significant health challenges globally. Traditionally, inflammatory diseases such as periodontitis have been treated with systemic administration of synthetic chemicals. However, recent years have witnessed challenges, including drug resistance and microbial dysbiosis associated with these treatments. In contrast, natural products derived from Chinese medicine offer numerous benefits, such as high safety profiles, minimal side effects, innovative pharmacological mechanisms, ease of extraction, and multiple targets, rendering them viable alternatives to conventional antibiotics for treating inflammatory conditions. Numerous effective anti-inflammatory natural products have been identified in traditional Chinese medicine (TCM), including alkaloids, flavonoids, terpenoids, lignans, and other natural products that exhibit inhibitory effects on inflammation and are potential therapeutic agents. Several studies have confirmed the substantial anti-inflammatory and immunomodulatory properties of these compounds. This comprehensive review examines the literature on the anti-inflammatory effects of TCM-derived natural products from databases such as PubMed, Web of Science, and CNKI, focusing on terms like "inflammation", "periodontitis", "pharmacology", and "traditional Chinese medicine". The analysis systematically summarizes the molecular pharmacology, chemical composition, and biological activities of these compounds in inflammatory responses, alongside their mechanisms of action. This research seeks to deepen understanding of the mechanisms and biological activities of herbal extracts in managing inflammatory diseases, potentially leading to the development of promising new anti-inflammatory drug candidates. Future applications could extend to the treatment of various inflammatory conditions, including periodontitis.
Humans
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Periodontitis/immunology*
;
Drugs, Chinese Herbal/chemistry*
;
Medicine, Chinese Traditional
;
Animals
;
Anti-Inflammatory Agents/chemistry*
10.Total alkaloids from Thesium chinense inhibit lipopolysaccharide-induced respiratory inflammation by modulating Nrf2/NF-κB/NLRP3 signaling pathway.
Guohui LI ; Yueqin GUAN ; Lintao XU ; Guangcheng PENG ; Qingtong HAN ; Tian WANG ; Zhenpeng XU ; Xuesen WEN ; Hongxiang LOU ; Tao SHEN
Chinese Journal of Natural Medicines (English Ed.) 2025;23(4):421-430
Inflammation plays a pivotal role in the etiology and progression of various diseases. In traditional Chinese medicine, the whole plants of Thesium chinense Turcz. and its preparations (e.g. Bairui Granules) have been employed to manage inflammatory conditions. While flavonoids were previously considered the primary anti-inflammatory components, other potentially active constituents have been largely overlooked and not thoroughly investigated. This study presents a novel finding that the total alkaloids of T. chinense (BC-Alk) are potent active substances underlying the traditional and clinical applications of T. chinense and Bairui Granules as anti-inflammatory agents. UPLC-MS/MS analysis identified the composition of BC-Alk as quinolizidine alkaloids. The anti-inflammatory efficacy of BC-Alk was evaluated using a lipopolysaccharide (LPS)-induced lung inflammation model in mice. Results demonstrated that BC-Alk significantly mitigated LPS-induced lung inflammation, attenuated the overproduction of IL-1β and the overproduction of inflammatory factors (TNF-α), and ameliorated lung tissue hyperplasia in mice in vivo. Mechanistic studies in vitro revealed that BC-Alk upregulated the expression of Nrf2 and its downstream proteins NQO1 and glutamate-cystine ligase and modifier subunit (GCLM), inhibited NF-κB phosphorylation, and suppressed NLRP3 activation. Collectively, these findings indicate that BC-Alk exerts potent inhibitory effects against lung inflammation by modulating Nrf2, NF-κB, and NLRP3 pathways. This study provides new insights into the anti-inflammatory constituents of T. chinense and Bairui Granules.
Animals
;
Lipopolysaccharides/adverse effects*
;
Alkaloids/pharmacology*
;
NF-kappa B/metabolism*
;
NF-E2-Related Factor 2/metabolism*
;
NLR Family, Pyrin Domain-Containing 3 Protein/metabolism*
;
Mice
;
Signal Transduction/drug effects*
;
Anti-Inflammatory Agents/pharmacology*
;
Male
;
Mice, Inbred C57BL
;
Humans
;
Drugs, Chinese Herbal/administration & dosage*
;
Pneumonia/genetics*

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