Chinese Journal of Natural Medicines
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2025
·
IF 4.9
Yang Liu,Quanwei Sun,Xuefei Xu,Mengmeng Li,Wenheng Gao,Yunlong Li,Ye Yang,Dengke Yin
Ulcerative colitis (UC) is a chronic inflammatory disorder with a complex etiology, characterized by intestinal inflammation and barrier dysfunction. Platycodon grandiflorus polysaccharides (PGP), the primary component of Platycodon grandiflorus , and hesperidin (Hesp), a prominent active component in Citrus aurantium L. (CAL), have both demonstrated anti-inflammatory properties. This study aims to elucidate the underlying mechanism of the synergistic effect of PGP combined with Hesp on UC, focusing on the coordinated interaction between the phosphatidylinositol 3-kinase (PI3K)/protein kinase B (AKT) and Janus kinase 2 (JAK2)/signal transducer and activator of transcription 3 (STAT3) signaling pathways. A mouse model of UC induced by dextran sulfate sodium (DSS) and a cell model using lipopolysaccharide (LPS)-induced RAW264.7/IEC6 cells were employed to investigate the in vitro and in vivo anti-inflammatory effects of PGP combined with Hesp on UC and its potential mechanism of action. The results indicated that compared to the effects of either drug alone, the combination of PGP and Hesp significantly modulated inflammatory factor levels, inhibited oxidative stress, regulated colonic mucosal immunity, suppressed apoptosis, and restored intestinal barrier function in vitro and in vivo . Further in vitro studies revealed that PGP significantly inhibited the PI3K/AKT signaling pathway, while Hesp significantly inhibited the JAK2/STAT3 signaling pathway. The use of inhibitors and activators targeting both pathways validated the synergistic effects of PGP combined with Hesp on the PI3K/AKT and JAK2/STAT3 signaling pathways. These findings suggest that PGP combined with Hesp exhibits a synergistic effect on DSS-induced colitis, potentially mediated through the phosphatase and tensin homolog (PTEN)/PI3K/AKT and interleukin-6 (IL-6)/JAK2/STAT3 signaling pathways.
研究领域:
免疫学
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分子生物学
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药理学
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炎症性肠病研究
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信号转导
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2020
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IF 5.162
Jia-Qi He,Min-Xia Zheng,Hua-Zhong Ying,Yu-Sen Zhong,Huan-Huan Zhang,Min Xu,Chen-Huan Yu
Two polysaccharides (PRP1 and PRP2) were isolated from Platycodonis Radix . Preliminary structural analysis indicated that PRP1 was composed of glucose, fructose, and arabinose in a molar ratio of 1:1.91:1.59 with a molecular weight of 440 kDa, whereas PRP2 was composed of arabinose, fructose, and galactose in a molar ratio of 1:1.39:1.18 with a molecular weight of 2.85 kDa. Compared with PRP2, PRP1 exerted stronger anticancer activity in vitro. Treatment with 5–30 μg/ml of PRP1 significantly inhibited the proliferation of HepG2 cells in vitro, and oral administration at the doses of 75–300 mg/kg also reduced the tumor growth in vivo. The miRNA expression patterns of human liver cancer cells HepG2 in vivo under PRP1 treatment were established, and microRNA-21 (miR-21) as the onco-miRNA was appreciably downregulated. PRP1 repressed the expression of miR-21, which directly targeted and suppressed PTEN (a negative regulator of the PI3K/Akt signaling cascade), and subsequently upregulated the expression of PTEN but downregulated the PI3K/AKT pathway, thereby promoting liver cancer cell apoptosis. These findings indicated that PRP1 inhibited the proliferation and induced the apoptosis of HepG2 mainly via inactivating the miR-21/PI3K/AKT pathway. Therefore, PRP1 could be used as a food supplement and candidate for the treatment of liver cancer.
研究领域:
药理学
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肿瘤学
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分子生物学
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DOI
PubMed
高影响因子
Journal of Traditional Chinese Medicine
·
2025
·Vol. 45
·期 5
·1040
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IF 2.2
Yuanmei ZHANG,Heqing LIU,Shaowen WANG,Lele WANG,Yawen GAO,Rui SUN,Jihui TANG
OBJECTIVE: To investigate whether Jiegeng ( Radix Platycodi , RP) has a Yin - Jing potentiating effect on Jingjie ( Herba Schizonepetae Tenuifoliae, ST). We investigated the pharmacokinetics and tissue distribution of pulegone, the active ingredient in ST volatile oil, in rats to verify the scientific validity of the Yin - Jing doctrine, the basic theory of Traditional Chinese Medicine (TCM). METHODS: The volatile oil and aqueous extract of ST were extracted by hydrodistillation. RP's aqueous extract underwent aqueous extraction. After individual and co-administration, we conducted pharmacokinetic and tissue distribution studies on Sprague-Dawley male rats. RESULTS: Peak concentration (Cmax), mean retention time from 0 to ∞ (MRT0→∞), and area under the curve (AUC0→10), (AUC0→∞) were 1.51, 1.14, 2.34, and 3.86 times higher in the co-administration group than in the individual administration group, respectively ( P < 0.05). In addition, half-life (T1/2) was significantly prolonged in the co-administration group ( P < 0.05). Meanwhile, the clearance and elimination rate constant (Ke) in the co-administration group were significantly lower than those in the individual administration group, just 50% of those in the individual administration group ( P < 0.05). After co-administration of the drug, the pulegone content in all tissues of the rats was elevated to varying degrees, especially a significant increase in the drug content in lung tissues ( P < 0.05). CONCLUSION: After co-administration, the retention of pulegone in the body was prolonged, the elimination of pulegone from the body was delayed, and the accumulation of pulegone in the lungs was facilitated. Therefore, using RP as a Yin - Jing drug concoction has a significant cumulative effect of inducing upward mobilization and targeting lung tissues.
研究领域:
中药药理学
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药物代谢
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药代动力学
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传统中医药理论
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组织分布
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天然药物化学
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药物相互作用
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PubMed
高影响因子
CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY
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2019
·Vol. 46
·期 12
·1194-1200
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IF 2.336
Di Wu,Wei Zhang,Ying Chen,Hong Ma,Mengchang Wang
Multiple myeloma (MM) is a malignancy characterized by the proliferation of malignant plasma cells. Platycodin D (PLD) is a triterpenoid saponin that exerts anti-tumour activity through multiple mechanisms. However, the role of PLD in MM remains unknown. Here, we investigated the effect of PLD on MM cell lines NCI-H929 and U266B1, and elucidated the underlying molecular mechanism. Cell Counting Kit-8 assay showed that the proliferation of NCI-H929 and U266B1 cells was significantly decreased after PLD treatment. Transwell assay confirmed that PLD treatment suppressed migration of NCI-H929 and U266B1 cells. Flow cytometry results indicated that the apoptotic rates of bortezomib (BTZ)-treated NCI-H929 and U266B1 cells were markedly increased after PLD treatment. Western blot analysis revealed that bcl-2 expression was decreased, while bax expression was increased in PLD-treated NCI-H929 and U266B1 cells compared with that in BTZ-treated cells. Furthermore, PLD treatment blocked the activation of nuclear factor-kappa B (NF-κB) and Janus kinase 2 (JAK2)/signal transducer and activator of transcription 3 (STAT3) signalling pathways in NCI-H929 cells. Taken together, these data showed that PLD inhibited proliferation and migration, and enhanced chemosensitization to BTZ through inactivation of the NF-κB and JAK2/STAT3 pathways in MM cell lines. These findings indicated that PLD might serve as a novel therapeutic agent for the treatment of MM.
研究领域:
肿瘤学
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药理学
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细胞生物学
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分子生物学
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DOI
PubMed
高影响因子
ACS Omega
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2023
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IF 4.1
Zhihai Wu,Zhiqiang Luo,Wen Sun,Yuanyuan Shi,Qi Ding
Allergic asthma is a prevalent form of asthma that is characterized primarily by airway inflammation. Jiegeng decoction (JGT) is a traditional Chinese herbal formula known for its anti-inflammatory properties and has been used to treat respiratory diseases for centuries. This study aimed to investigate the biological effects and mechanisms of action of JGT in improving allergic asthma. An experimental allergic asthma mouse model was established using ovalbumin. The results showed that JGT significantly improved inflammation cell infiltration in the lung tissue of allergic asthmatic mice and the inflammatory environment of Th2 cells in the bronchoalveolar lavage fluid while also reducing serum IgE levels. Subsequently, 38 components of JGT were identified through liquid chromatography–mass spectrometry. Network pharmacology revealed that regulating inflammation and immune responses is the primary biological process by which JGT improves allergic asthma, with Th2 cell differentiation and the JAK-STAT signaling pathway being the key mechanisms of action. Finally, qPCR, flow cytometry, and Western blotting were used to validate that JGT inhibited Th2 cell differentiation by blocking the JAK1-STAT6 signaling pathway in CD4+ T cells, ultimately improving allergic asthma. This study provides a novel perspective on the therapeutic potential of JGT in the treatment of allergic asthma.
研究领域:
药理学
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免疫学
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中医
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分子生物学
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DOI
PubMed
高影响因子
DRUG DELIVERY
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2022
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IF 6.819
Chunjing Guo,Yanguo Su,Hui Wang,Min Cao,Ningning Diao,Zhongxin Liu,Daquan Chen,Ming Kong
Liposomes have been widely used for targeted drug delivery, but the disadvantages caused by cholesterol limit the application of conventional liposomes in cancer treatment. The compatibility basis of couplet medicines and the compatibility principle of the traditional Chinese medicine principle of ‘monarch, minister, assistant and guide’ are the important theoretical basis of Chinese medicine in the treatment of tumor and the important method to solve the problem of high toxicity. In this study, the active ingredients of the couplet medicines Platycodon grandiflorum and Glycyrrhiza uralensis were innovatively utilized, and glycyrrhizic acid (GA) was encapsulated in liposomes constructed by mixing saponin and lecithin, and cholesterol was replaced by platycodin and ginsenoside to construct saponin liposomes (RP-lipo) for the drug delivery system of Chinese medicine. Compared with conventional liposomes, PR-lipo@GA has no significant difference in morphological characteristics and drug release behavior, and also shows stronger targeting of lung cancer cells and anti-tumor ability in vitro, which may be related to the pharmacological properties of saponins themselves. Thus, PR-lipo@GA not only innovatively challenges the status of cholesterol as a liposome component, but also provides another innovative potential system with multiple functions for the clinical application of TCM couplet medicines.
研究领域:
药学
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肿瘤学
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中医药
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药物递送系统
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DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
·
2025
·
IF 5.4
Shasha Han,Zichen Luo,Shihang Bao,Zihan Xiao,Weichen Xu,Tong Xie,Chen Shi,Jin Wang,Jinjun Shan
Ethnopharmacological relevance Platycodon grandiflorus root, is a widely used herb in East Asia for treating respiratory diseases, but research on its oral safety is limited. Aim of the study This study examines the potential adverse gastrointestinal reactions resulting from excessive consumption of Platycodon grandiflorus root (PR) and its effects on gut microbiota and host co-metabolism. Materials and methods This study evaluated the effects of different doses (1.5, 4.5, and 7.5 g/kg/day) of PR on ICR mice through gavage. Select the 7.5 g/kg/day dosage group and the control group to assess intestinal morphology and conduct histopathological studies. Examine inflammation-related factors and tight junction proteins using WB, qPCR, and ELISA. Additionally, perform 16S rDNA sequencing and metabolomic analyses to evaluate changes in gut microbiota and endogenous metabolites. Finally, the clearance of gut microbiota with antibiotics, the effects of excessive PR on mice were investigated. Results Excessive intake of PR can lead to mortality in mice, as well as symptoms such as intestinal flatulence and slowed intestinal transit, suggesting the occurrence of chronic intestinal pseudo-obstruction accompanied by endotoxemia. It altered both α-diversity and β-diversity in the gut microbiota of mice, with increased relative abundances of Pseudomonadota, Verrucomicrobiota, Escherichia-Shigella , Akkermansia , Bacteroides , and Klebsiella , closely linked to intestinal obstruction and bacterial overgrowth. Excessive intake of PR also resulted in metabolic disturbances in mice, particularly in the levels of metabolites such as bate-hydroxybutyrate, 5,6-dihydrouracil, uridine, isoleucine, mannitol, bate-alanine, L-cysteine, L-tyrosine, and orotic acid, which may provide insights into the side effects associated with excessive consumption of PR. Clearing the gut microbiota significantly mitigated adverse effects on the intestines and restored metabolite levels. Conclusions This study demonstrates that excessive PR induces gut microbiota and metabolic disruption in normal mice, with the overgrowth of Gram-negative bacteria releasing LPS that impair smooth muscle contraction, leading to adverse effects such as chronic intestinal pseudo-obstruction.
研究领域:
药理学
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微生物学
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代谢组学
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PubMed
高影响因子
BIOMEDICINE & PHARMACOTHERAPY
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2023
·
IF 7.5
Tao Long,Xue Chen,Yue Zhang,Yu-Jia Zhou,Yan-Ni He,Yun-Fei Zhu,Hai-Jun Fu,Lu Yu,Chong-Lin Yu,Betty Yuen-Kwan Law,Jian-Ming Wu,Da-Lian Qin,An-Guo Wu,Xiao-Gang Zhou
Enhancing the clearance of proteins associated with Alzheimer's disease (AD) emerges as a promising approach for AD therapeutics. This study explores the potential of Radix Stellariae , a traditional Chinese medicine, in treating AD. Utilizing transgenic C. elegans models of AD, we demonstrated that a 75% ethanol extract of Radix Stellariae (RSE) (at 50 µg/mL) effectively diminishes Aβ and Tau protein expression, and alleviates their induced impairments including paralysis, behavioral dysfunction, neurotoxicity, and ROS accumulation. Additionally, RSE enhances the stress resistance of C. elegans . Further investigations revealed that RSE promotes autophagy, a critical cellular process for protein degradation, in these models. We found that inhibiting autophagy-related genes negated the neuroprotective effects of RSE, suggesting a central role for autophagy in the actions of RSE. In PC-12 cells, we observed that RSE not only inhibited Aβ fibril formation but also promoted the degradation of AD-related proteins and reduced their cytotoxicity. Mechanistically, RSE was found to induce autophagy via modulating PI3K/AKT/mTOR and AMPK/mTOR signaling pathways. Importantly, inhibiting autophagy counteracted the beneficial effects of RSE on the clearance of AD-associated proteins. Moreover, we identified Dichotomine B, a β-carboline alkaloid, as a key active constituent of RSE in mitigating AD pathology in C. elegans at concentrations ranging from 50 to 1000 µM. Collectively, our study presents novel discoveries that RSE alleviates AD pathology and toxicity primarily by inducing autophagy, both in vivo and in vitro. These findings open up new avenues for exploring the therapeutic potential of RSE and its active component, Dichotomine B, in treating neurodegenerative diseases like AD.
研究领域:
神经科学
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药理学
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中药学
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细胞生物学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
Food & Function
·
2022
·Vol. 13
·期 7
·3946-3956
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IF 6.317
Zhe Wang,Chunhai Li,Xi He,Kang Xu,Zhipeng Xue,Ting Wang,Zhenshang Xu,Xinli Liu
The effect of Platycodon grandiflorum (PG) on colitis and its underlying mechanism were rarely studied. In this study, Lactobacillus rhamnosus 217-1 was used to ferment PG roots, and the concentrations of platycodin-D, flavonoids, and polyphenols and the DPPH free radical scavenging rate were significantly increased. Treatment with a PG root fermentation broth (PGRFB) could reduce dextran sulfate sodium (DSS) induced ulcerative colitis (UC) in mice. Meanwhile, the PGRFB significantly reduced the content of inflammatory factors in mouse serum and the expression of inflammatory factor mRNA in the intestinal tract, regulated the polarization of M1/M2 macrophages, and increased the expression of tight junction protein mRNA in intestinal epithelial cells. In summary, it was proved that the PGRFB could inhibit the nuclear factor kappa B (NF-κB) signaling pathway and the expression of Nod-like receptor protein 3 (NLRP3) inflammasomes by activating AMP-activated protein kinase (AMPK) and lowering the release of pro-inflammatory cytokines.
研究领域:
药理学
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免疫学
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微生物学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2019
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IF 3.414
Yining Liu,Zhuping Hong,Jing Qian,Yi Wang,Shufang Wang
Ethnopharmacological relevance Jie-Geng-Tang (JGT), a famous traditional Chinese medicine prescription, consists of Platycodonis Radix and Glycyrrhizae Radix et Rhizoma . According to traditional medicinal theory, JGT exerts various effects, including apocenosis, detoxifying, moisturizing the lung and relieving sore throat. It is often used to treat throat inflammation and lung diseases. Aim of the study To determine the protective effect of JGT on Staphylococcus aureus ( S. aureus )-induced acute lung injury (ALI) in mice and to identify the compounds in the prescription that may be responsible for antibacterial activity . Materials and methods The protective effect of JGT was assessed using S. aureus -induced ALI mice (i.g., 2.7 g/kg/day). Bacterial burden, pathological morphology, cytokine levels of TNF-α, IL-1β, KC, and MIP-2 were evaluated in the lung and bronchoalveolar lavage fluid at 24 h post-infection, respectively. Twenty three compounds in the prescription were evaluated for their minimum inhibitory concentration (MIC) in vitro by means of microbroth dilution method against S. aureus . The antibacterial effects in vitro of licochalcone A and isoliquiritigenin were also investigated by transmission electron microscopy . In vivo antibacterial activities of licochalcone A and isoliquiritigenin were evaluated by survival rates, bacterial burden, and pathological morphology of lung tissues on S. aureus -induced ALI in mice (i.p., 160 mg/kg/day). Results Pretreatment with JGT significantly improved the pathological morphology of lung tissues on S. aureus -induced ALI in mice, accompanied with the reduced bacterial burden in the lungs and inhibited expression of inflammatory cytokine levels at 24 h post-infection. Five compounds, namely licochalcone A, licoisoflavone B, glyasperin A, isoliquiritigenin, and licochalcone B from Jie-Geng-Tang displayed good antibacterial activities against S. aureus (MIC < 128 μg/mL). Furthermore, applications of licochalcone A and isoliquiritigenin resulted in the increased survival rates, reduced bacterial burden in the lungs, and improved pathological morphology of lung tissues in S. aureus infected mice. Conclusion The study demonstrated that Jie-Geng-Tang presented protective role of acute lung injury, which supported its traditional use for the treatment of lung diseases. Licochalcone A, isoliquiritigenin, licoisoflavone B, glyasperin A, and licochalcone B might contribute to the antibacterial activity of JGT on S. aureus -induced acute lung injury. The anti- S. aureus activity of licoisoflavone B, glyasperin A, and licochalcone B in vitro , as well as the anti- S. aureus activity of licochalcone A in vivo , were first reported in this study.
研究领域:
药理学
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免疫学
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中医
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微生物学
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病理学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2022
·
IF 8.025
Yi Li,Chunjing Guo,Qiang Chen,Yanguo Su,Huimin Guo,Ruoyang Liu,Changgang Sun,Shuqi Mi,Jinqiu Wang,Daquan Chen
Pneumonia can lead to high morbidity and mortality secondary to uncontrolled inflammation of the lung tissue. Blocking cytokine storm storms may be the key to saving the life of patients with severe pneumonia. According to the medicinal guide theory of Traditional Chinese Medicine (TCM) and the inherent affinity with macrophages for the site of inflammation, we constructed the drug delivery platform (MNPs) derived from macrophage-membrane encapsulated reaction oxygen species (ROS)-responsive Platycodon grandiflorum polysaccharides (PGP) nanoparticles (PNPs) to calm the cytokine storm and improve lung inflammation. By loading the anti-inflammatory agent Curcumin (Cur), we demonstrated that [email protected] significantly attenuated inflammation and cytokine storm syndrome in acute lung injury (ALI) mice by suppressing pro-inflammatory factor production and inflammatory cell infiltration. Interestingly, we observed that the PNPs also have potent pulmonary targeting ability compared to other polysaccharide carriers, which is in line with the medicinal guide theory of TCM. Our study revealed the rational design of drug delivery platforms to improve the treatment of lung injury, which inherits and develops the important theories of TCM through the perfect combination of guide theory and biomimetic nanotechnology and provides the experimental scientific basis for the clinical application of channel ushering drugs.
研究领域:
药理学
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纳米技术
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中医
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免疫学
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肺科学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2024
·
IF 5.7
Wenting Wang,Zi Wang,Zhaojie Meng,Shuang Jiang,Zhi Liu,Hong-yan Zhu,Xin-dian Li,Jing tian Zhang,Wei Li
The current study aimed to assess the effectiveness of pharmacological intervention with Platycodin D (PD), a critically active compound isolated from the roots of Platycodon grandiflorum, in mitigating cardiotoxicity in a murine model of type 2 diabetes-induced cardiac injury and in H9c2 cells in vitro. Following oral administration for 4 weeks, PD (2.5 mg/kg) significantly suppressed the elevation of fasting blood glucose (FBG) levels, improved dyslipidemia, and effectively inhibited the rise of the cardiac injury markers creatine kinase isoenzyme MB (CK-MB) and cardiac troponin T (cTnT). PD treatment could ameliorate energy metabolism disorders induced by impaired glucose uptake by activating AMPK protein expression in the DCM mouse model, thereby promoting the GLUT4 transporter and further activating autophagy-related proteins. Furthermore, in vitro experiments demonstrated that PD exerted a concentration-dependent increase in cell viability while also inhibiting palmitic acid and glucose (HG-PA)-stimulated H9c2 cytotoxicity and activating AMPK protein expression. Notably, the AMPK activator AICAR (1 mM) was observed to upregulate the expression of AMPK in H9c2 cells after high-glucose and -fat exposure. Meanwhile, we used AMPK inhibitor Compound C (20 μM) to investigate the effect of PD activation of AMPK on cells. In addition, the molecular docking approach was employed to dock PD with AMPK, revealing a binding energy of −8.2 kcal/mol and indicating a tight interaction between the components and the target. PD could reduce the expression of autophagy-related protein p62, reduce the accumulation of autophagy products, promote the flow of autophagy, and improve myocardial cell injury. In conclusion, it has been demonstrated that PD effectively inhibits cardiac injury-induced type 2 diabetes in mice and enhances energy metabolism in HG-PA-stimulated H9c2 cells by activating the AMPK signaling pathway. These findings collectively unveil the potential cardioprotective effects of PD via modulation of the AMPK signaling pathway.
研究领域:
药理学
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糖尿病
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心脏病学
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细胞生物学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）