Journal of ethnopharmacology最新文献

Ethnopharmacological relevance: Bergenia ciliata (Haw.) Sternb. (Family Saxifragaceae) remains mentioned as Pashanbheda in Ayurveda and Zakhmehayat in Unani. In North Waziristan, Pakistan, indigenous communities use this plant in ethnodentistry to treat tooth decay and toothaches. However, scientific evidence on its mode of action is still lacking.

Aim of the study: To evaluate the effect of extracts and fractions of B. ciliata flower against oral bacteria and elucidate the possible antibacterial and antibiofilm mechanism.

Materials and methods: Prepared extract of B. ciliata flowers were checked for its antibacterial activity against oral (S. mutans, S. pyogenes, S. oralis) and opportunistic bacteria (Staphylococcus aureus, Citrobacter clonae and Achromobacter insolitus). Preparative TLC-bioautography and silica gel column chromatography was used to isolate bioactive compounds. HRESI-MS and NMR studies were employed for its structural elucidation. Antibacterial and antibiofilm activities of extracts and isolated compounds were studied against S. mutans. Scanning Electron Microscope studies indicated membrane damage. Reactive Oxygen Species production (ROS), lipid peroxidation and cytoplasmic leakage were also assessed.

Results: The most active ethyl acetate extract (EA) showed potent inhibitory effect against S. mutans (0.390 μg/μl). TLC-bioautography indicated spots F1 & F2 to show inhibition zones. F1 was identified as kaempferol. This is the first report on flowers of B. ciliata against oral infection. The mode of action of F1 can be attributed to its ability to destroy the membrane integrity, reducing and disrupting biofilm. It also produced ROS within the bacterial cell, leading to lipid peroxidation and subsequently causing death of the bacteria.

Conclusion: Kaempferol is the active compound in bioactive spot F1 which showed antibacterial and antibiofilm activity. The antibacterial activity can be linked with the membrane disrupting properties of kaempferol and producing ROS inside S. mutans. Thus, phytochemicals derived from B. ciliata can be used in the development of pharmaceutical dental products.

Ethnopharmacological relevance: Zuojin formula (ZJF) is a well-known herbal medicine in Pharmacopoeia of China, which is widely used for gastritis. Modified Zuojin formula (MZJF) was adapted based on traditional Chinese medicine (TCM) theories concerning gastric atrophy and dysplasia, along with extensive clinical experience, has been clinically employed to treat chronic atrophic gastritis (CAG). However, the underlying mechanisms by which MZJF intervenes in CAG remain to be fully elucidated.

Aim of the study: The aim of this study was to evaluate the effects of MZJF intervention in CAG and explore its potential mechanisms.

Methods: Four induction factors were used to establish a CAG rat model. HE and AB-PAS staining was utilized to assess the effects of MZJF in the intervention of CAG. The stomach weight index and gastric acid pH was used to assess the overall state of stomach. ELISA was used to assess the gastric mucosal inflammatory response. Using transmission electron microscopy to observe chief cells and parietal cells, we evaluate the improvement of ultrastructure by MZJF. Through network pharmacology analysis, the possible regulatory mechanism of MZJF in CAG was preliminarily explored. Binding interactions between MZJF components and predicted targets were explored using molecular docking. Subsequently, quantitative real-time PCR (qRT-PCR), Western blot, biochemical analysis and TUNEL staining were applied to validate the effect of MZJF on predicted pathways.

Results: MZJF treatment ameliorated gastric mucosal pathology, inflammation, cellular ultrastructural damage and PG levels, halted the exacerbation of CAG in rats, along with a reduction in stomach weight index and gastric acid pH. A total of 79 compounds in MZJF targeting 203 CAG-related molecules were identified through network pharmacology. Enrichment analysis of the core targets was focused on the hypoxia inducible factor-1α (HIF-1α) signaling pathway. Molecular docking results identified HIF-1α as stable binding targets for MZJF primary components. Subsequently, PCR, WB, and biochemical results showed that MZJF suppressed the gene and protein expression levels of HIF-1α and its downstream molecules including glycolytic enzymes and transporters, modulated glucose, pyruvic acid and lactate levels in gastric mucosal tissue. Moreover, MZJF induced apoptosis of gastric epithelial cells, as evidenced by the upregulation of cleaved caspase-3, Bax, Bax/Bcl-2 and TUNEL positive cells ratio.

Conclusions: MZJF suppressed the HIF-1α-mediated glycolytic pathway, and promoted cell apoptosis, thereby halting the malignant transformation of CAG. The study provides a valuable reference point for applying TCM in preventing and treating CAG.

Ethnopharmacological relevance: Cardiac apoptosis has been reported to be involved in the development of Heart failure (HF) after Myocardial infarction (MI). As a traditional Chinese medicine with cardioprotective properties, Gualou Xiebai Banxia Decoction (GXBD) is therapeutically effective in treating MI. However, whether GXBD regulates cardiac apoptosis in HF after MI remains unknown, and the underlying mechanisms still unclear.

Aim of the study: This study aimed to explore the effects and potential mechanisms of GXBD on cardiac apoptosis after MI.

Materials and methods: The MI model was constructed by ligating the left anterior descending coronary artery (LAD) in mice. The cardioprotective effects of GXBD were determined by echocardiography, masson staining, and hematoxylin and eosin (HE) staining. Bioinformatics analysis and network Pharmacology were used to explore the underlying molecular mechanisms of GXBD in MI. The effects of GXBD on apoptosis as well as the ALDH2 were examined by TUNEL staining, Immunohistochemistry (IHC), and Western blot (WB). Additionally, the effects of GXBD on oxidative stress, apoptosis and the ALDH2 in cardiomyocytes (H9c2) were investigated using reactive oxygen species (ROS) detection, Hoechst33342/PI stainingand and WB. Moreover, the effects of suppressing and overexpressing ALDH2 in H9c2 cells were further examined.

Results: Target prediction analysis showed that ALDH2 was a key target of GXBD which could ameliorate myocardial infarction. GXBD dose-dependently reduced cardiomyocyte apoptosis and ventricular dysfunction. In vivo experiments, GXBD activated ALDH2 enzymatic activity and inhibited the expression levels of Bax, Bcl-2, Cleaved Caspase 3, and Caspase 9. In vitro experiments, GXBD inhibited apoptosis in H9c2 cells. ALDH2 activation enhanced these inhibitory effects of GXBD while silencing of ALDH2 significantly reversed these inhibitory effects of GXBD.

Conclusion: GXBD exerts inhibitory effects on oxidative stress and cardiomyocyte apoptosis in mice after MI, suppresses H9c2 oxidative stress and apoptosis through activation of the enzyme activity of ALDH2.

Ethnopharmacological relevance: Safflower, the florets of Carthamus tinctorius L., is a widely used traditional Chinese medicine for promoting circulation and improving dysmenorrhea. Polysaccharides is one of the principal water-soluble components in Safflower, which recently endowed with a variety of biological activities, thus making them have important research significance in the field of ethnopharmacology.

Aim of the study: This review summarized the latest research progress on the preparation technology, structural characteristics, and pharmacological effects of Safflower polysaccharides. Moreover, by comparing the structural characteristic of Safflower polysaccharides, the potential structure-activity relationship of Safflower polysaccharides was also discussed.

Materials and methods: This article used keywords including Safflower polysaccharide, Carthamus tinctorius L polysaccharide, Safflower polysaccharide extraction and separation, Safflower polysaccharide structure, and Safflower polysaccharide anti-tumor effects to search for all relevant literature in PubMed, Web of Science, Google Scholar, ScienceDirect, CNKI and other databases from the establishment of the database to July 2024.

Results: Summarizing current research findings, seventeen homogeneous Safflower polysaccharides have been obtained. Their structural characteristics, including molecular weights, monosaccharide composition, sugar residue types, glycosidic bond configuration, and the linkage sequence, were initially researched. In terms of pharmacological activity, Safflower polysaccharides exhibit a wide range of biological activities, including immune regulation, anti-tumor effects, and antioxidant properties. Furthermore, the structural characteristics of Safflower polysaccharides significantly influence its biological activities, encompassing factors such as molecular weight, monosaccharide composition, and degree of branching.

Conclusion: Safflower polysaccharides have seen significant advancements in recent years regarding preparation methods, structural characterization, and pharmacological studies. These achievements would provide a theoretical basis for the application of Safflower polysaccharide in the field of ethnopharmacology. While Safflower polysaccharides exhibit diverse biological activities and significant potential for development and utilization, further in-depth research is needed to enhance our understanding of their mechanisms of action and optimize their clinical applications.

Ethnopharmacological relevance: Phyllanthus amarus is ethnomedicinally used to treat gallbladder stones, kidney stones and chronic liver diseases. P. amarus is gaining popularity as an ingredient in many botanical dietary supplements.

Aim of the study: To evaluate the interaction of P. amarus extract and its lignans with human xenobiotic sensing receptors (PXR and AhR) and their downstream genes.

Materials and methods: Activation of PXR and AhR was measured by reporter gene assays. Gene expression analysis was performed in hepatic (HepG2) and intestinal (LS174T) cells by RT-PCR. CYP inhibition assays were carried out in baculosomes. The inhibitory effect on the ABC transporters (P-gp and BCRP) was investigated via rhodamine-123 and Hoechst 33342 uptake assays in Caco-2 and MDR-MDCK cells. Effect on CYP3A4 and CYP1A2 enzyme activity was measured in primary human hepatocytes.

Results: P. amarus extract and its lignans activated AhR and PXR in respective reporter cells. Tested extract and lignans significantly increased CYP3A4 mRNA but inhibited CYP3A4 enzyme activity when tested in primary human hepatocytes and CYP3A4-specific baculosomes. In contrast, increased CYP1A2 mRNA was associated with increased CYP1A2 enzyme activity in hepatocytes. No inhibition of CYP1A2 activity was detected in baculosomes. A weak inhibitory effect on ABC-transporters was observed.

Conclusions: Results suggest that overconsumption of P. amarus or P. amarus-containing botanical supplements may change CYP homeostasis which could alter the pharmacokinetics of substrate drugs, thereby elevating the risk of herb-drug interactions (HDIs) when taken concomitantly with conventional medications. Further studies are warranted to strengthen the clinical relevance of these findings.

Ethnopharmacological relevance: Mentha longifolia L. has been employed to treat cough, lung inflammation, and bronchial asthma disorders.

Aim of the study: Our study was carried out to investigate the medicinal effect of the flavonoids derived from M. longifolia, specifically didymin, linarin, rutin, and TMF, as well as the whole extracts of M. longifolia subsp. typhoides and M. longifolia subsp. schimperi, in comparison to dexa, in a mice model of ovalbumin-allergic asthma (OVA).

Methods: After inhaling OVA, the mice developed acute asthma symptoms. Mice were subjected orally to Dexa and/or isolated flavonoids. The study assessed total and differential leukocyte counts, LDH concentration, and total protein concentration in BALF, reduced levels of GSH and total NOx products in lung tissues and analyzed the lung specimens by staining them with haematoxylin and eosin (H & E).

Results: Histopathological analysis of the right lung lobes demonstrated that the isolated flavonoids exhibited a significant anti-inflammatory effect higher than Dexa as shown by decreasing the overall and distinct leukocyte counts, LDH levels, and total protein levels in BALF, as compared to the OVA group (p< 0.05). TMF was the most effective and the other tested flavonoids are more effective than Dexa but less than TMF. In addition, all tested flavonoids and Dexa significantly (p< 0.05) mitigated OVA-induced oxidative stress as evidenced by diminished lung NOx level and elevated GSH level. Computational docking studies proved recognition of didymin, linarin, rutin, and TMF to the leukotriene esterase binding sites.

Conclusion: The tested flavonoids; didymin, linarin, rutin, and TMF successfully inhibit Ova-induced allergic asthma in mice through their anti-inflammatory and antioxidant activities and may represent promising candidate as a remedy for allergic asthma.

Ethnopharmacological relevance: Fallopia aubertii (L. Henry) Holub (F. aubertii), a traditional Tibetan medicine, is used in China for treating respiratory inflammatory diseases, including acute lung injury (ALI). However, the chemical constituents of F. aubertii and its anti-inflammatory mechanisms in the lungs remain poorly understood.

Aim of the study: This study aimed to identify the chemical constituents of the F. aubertii extract (FAE), evaluate its effectiveness in reducing ALI in mice, and elucidate the underlying mechanisms of its action.

Materials and methods: The chemical composition of FAE was determined using UPLC-LTQ Velos Pro-Orbitrap Elite. Network pharmacology was employed to predict the mechanisms by which FAE might mitigate ALI. Mice were administered FAE orally for seven days, followed by intratracheal instillation of lipopolysaccharide (LPS) to induce ALI. On the final day, the mice were euthanized, and their lungs were collected for transcriptome analysis, proteomics, pharmacodynamic evaluation, and mechanistic studies. Hematoxylin and eosin (H&E) staining assessed lung pathology. Transcriptome and proteomic analyses, along with real-time quantitative PCR (RT-qPCR) and western blotting, were used to investigate FAE's effects on lung inflammation and related signaling pathways. In vitro experiments further explored the anti-ALI mechanisms of FAE. Immunofluorescence assays in RAW264.7 cells examined the nuclear translocation of NF-κB.

Results: Fifty-one compounds were identified in FAE, predominantly flavonoid glycosides. Network pharmacology suggested that FAE may inhibit ALI by modulating the NF-κB pathway and Th17 differentiation. RNA-seq analysis indicated that FAE might suppress inflammation through the IL-17 signaling pathway, with these findings corroborated by mRNA level measurements in vivo and in vitro. FAE alleviated LPS-induced ALI by modulating the IL-17A signaling pathway, which was confirmed through proteomic analysis. Western blotting revealed that FAE reduced the expression of IL-17A, Act1, TRAF6, and p-NF-κB, while immunofluorescence assays showed FAE inhibited LPS-induced NF-κB nuclear translocation.

Conclusion: FAE attenuates inflammation-mediated ALI by inhibiting the IL-17A/NF-κB signaling pathway. This study highlights the anti-ALI effects of FAE and provides a theoretical foundation for its potential use in ALI treatment.

Ethnopharmacological relevance: Shenling Baizhu San (SLBZS) is a Traditional Chinese Medicine (TCM) formula composed of 10 medicinal herbs, historically used to strengthen the spleen, replenish qi, and alleviate fatigue-related symptoms. SLBZS originates from the 'Taiping Huimin Heji Ju Fang' of the Song Dynasty. Central fatigue (CF), a subtype of fatigue, is considered in TCM to be closely associated with spleen deficiency. However, there is currently a lack of research on SLBZS's therapeutic effects on CF and the pharmacological mechanisms underlying its potential benefits.

Aim of the study: This study aims to assess the effects of SLBZS on CF in rats induced by the Modified Multiple Platform Method (MMPM) and to elucidate the underlying mechanisms, focusing on mitochondrial biogenesis and SIRT1/PGC-1α pathway regulation.

Materials and methods: CF was induced in male Wistar rats using MMPM, involving intermittent sleep deprivation over 21 days. SLBZS was administered at low(LSLBZS), medium(MSLBZS), and high doses(HSLBZS). Chemical components of SLBZS were identified and quantified using Liquid Chromatography-Tandem Mass Spectrometry(LC-MS/MS). Behavioral tests evaluated physical performance, emotional state, and cognitive function, while serum biochemical markers, mitochondrial morphology, and the protein and gene expression levels of the SIRT1/PGC-1α pathway were analyzed to explore underlying mechanisms.

Results: A total of 141 main compounds in SLBZS were identified, comprising various components such as flavonoids, phenylpropanoids, terpenoids, among others. SLBZS significantly improved physical performance, alleviated negative emotions, and enhanced cognitive function in CF rats. Biochemically, SLBZS increased serum ATP levels and reduced fatigue-related markers. Mitochondrial analysis demonstrated that SLBZS reversed mitochondrial degeneration, increased mitochondrial number, and increased mtDNA copy number in the hippocampus. Furthermore, SLBZS upregulated SIRT1 /PGC-1α pathway expression at both the protein and gene levels in the hippocampus. Notably, the HSLBZS group demonstrated particularly pronounced effects.

Conclusion: SLBZS significantly alleviates CF symptoms enhances mitochondrial function via upregulating the SIRT1/PGC-1α pathway, positioning it as a promising alternative for CF management by addressing both its physiological and symptomatic aspects.