Hypericum perforatum, widely cultivated in China for its substantial economic and medicinal advantages, is utilized in the pharmaceuticals, dietary supplements, and cosmetics industries. This study ...aimed to identify bioactive components with neuroprotective properties within the plant and to explore their underlying mechanisms. We isolated and identified seventeen compounds, including four novel ones (1−4) and thirteen known metabolites (5−17). The anti-neuroinflammatory and neuroprotective effects of these compounds were comprehensively assessed. Our results demonstrated that compounds 5, 6, and 9 effectively reduced nitric oxide (NO) release by inhibiting the expression of inducible nitric oxide synthase (iNOS), demonstrating notable anti-neuroinflammatory properties. Furthermore, compounds 4 and 5 were found to trigger the Nrf2/HO-1 pathway, indicating their considerable neuroprotective effects. Notably, the neuroprotective efficacy of the novel compound 4 was also preliminarily validated in a zebrafish model. These findings suggest that the prenylated flavonoids from H. perforatum may serve as potential neuroprotective agents for the prevention and treatment of neurodegenerative diseases.
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•First investigation of prenylated flavonoids from Hypericum perforatum L.•Four new compounds and thirteen known compounds were isolated and elucidated.•Compounds 5, 6 and 9 showed significantly anti-neuroinflammatory activities.•Compounds 4 and 5 exerted outstanding neuroprotective effects by activating Nrf2/HO-1 signaling pathway.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
Hypericum perforatum L. (Hypericaceae), popularly called St. John's wort (SJW), has a rich historical background being one of the oldest used and most extensively investigated medicinal herbs. Many ...bioactivities and applications of SJW are listed in popular and in scientific literature, including antibacterial, antiviral, anti-inflammatory. In the last three decades many studies focused on the antidepressant activity of SJW extracts. However, several studies in recent years also described the antinociceptive and analgesic properties of SJW that validate the traditional uses of the plant in pain conditions.
This review provides up-to-date information on the traditional uses, pre-clinical and clinical evidence on the pain relieving activity of SJW and its active ingredients, and focuses on the possible exploitation of this plant for the management of pain.
Historical ethnobotanical publications from 1597 were reviewed for finding local and traditional uses. The relevant data on the preclinical and clinical effects of SJW were searched using various databases such as PubMed, Science Direct, Scopus, and Google Scholar. Plant taxonomy was validated by the database Plantlist.org.
Preclinical animal studies demonstrated the ability of low doses of SJW dry extracts (0.3% hypericins; 3–5% hyperforins) to induce antinociception, to relieve from acute and chronic hyperalgesic states and to augment opioid analgesia. Clinical studies (homeopathic remedies, dry extracts) highlighted dental pain conditions as a promising SJW application. In vivo and in vitro studies showed that the main components responsible for the pain relieving activity are hyperforin and hypericin. SJW analgesia appears at low doses (5–100mg/kg), minimizing the risk of herbal-drug interactions produced by hyperforin, a potent inducer of CYP enzymes.
Preclinical studies indicate a potential use of SJW in medical pain management. However, clinical research in this field is still scarce and the few studies available on chronic pain produced negative results. Prospective randomized controlled clinical trials performed at low doses are needed to validate its potential efficacy in humans.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK, ZRSKP
Wound dressing materials are crucial for accelerating the healing period of chronic wounds. In this study, chitosan nanoparticles loaded with Hypericum perforatum (Hp) were modified with agarose to ...create wound-healing films and their antimicrobial potential was investigated in vitro. Chitosan (CS) nanoparticles and Hp-loaded nanoparticles were prepared using the ionic gelation method. The synthesized Hp-loaded CS nanoparticles were modified with agarose by the solvent-casting method. Antimicrobial assays were performed using the disk diffusion method and agar well diffusion method. The characterization of nanoparticles and films was performed by UV–Vis spectrophotometry, Dynamic Light Scattering (DLS), Fourier Transform Infrared Spectroscopy (FT-IR), mechanical testing, and swelling testing. The results showed that Hypericum perforatum was loaded into chitosan nanoparticles with a 90.1 ± 2.53 % yield. The sizes of the Hypericum perforatum-loaded chitosan nanoparticles and chitosan nanoparticles were 156 ± 22 nm and 69 ± 4.2 nm, respectively. The CS-Hp/Agarose film showed no cytotoxic effect on L929 fibroblast cells and maintained cell viability for 72 h. These results indicate that Hp might be used in wound healing due to its antimicrobial and cell growth-promoting properties.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
Hypericum perforatum L. (HPL), also known as St. John's wort, is one of the extensively researched domestically and internationally as a medicinal plant. In this study, non-targeted metabolomics ...combined with machine learning methods were used to identify reasonable quality indicators for the holistic quality control of HPL. First, the high-resolution MS data from different samples of HPL were collected, and visualized the chemical compounds through the MS molecular network. A total of 122 compounds were identified. Then, the orthogonal partial least squares-discriminant analysis (OPLS-DA) model was established for comparing the differences in metabolite expression between flower, leaf, and branches. A total of 46 differential metabolites were screened out. Subsequently, analyzing the pharmacological activities of these differential metabolites based on protein-protein interaction (PPI) network. A total of 25 compounds associated with 473 gene targets were retrieved. Among them, 13 highly active compounds were selected as potential quality markers, and five compounds were ultimately selected as quality control markers for HPL. Finally, three different classifiers (support vector machine (SVM), random forest (RF), and K-nearest neighbor (KNN)) were used to validate whether the selected quality control markers are qualified. When the feature count is set to 122 and 46, the RF model demonstrates optimal performance. As the number of variables decreases, the performance of the RF model degrades. The KNN model and the SVM model also exhibit a decrease in performance but still manage to satisfy the intended requirements. The strategy can be applied to the quality control of HPL and can provide a reference for the quality control of other herbal medicines.
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•A custom-built database was built to visualized the compounds present in HPL.•An OPLS-DA model was established to selected differential metabolites.•The PPI network was established to selected the active compounds.•Three classifiers were used to assess the qualification of quality markers.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
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•The coupling process is an effective strategy to prepare high purity products.•The total recovery ratio of hypericin was 80.6 % in the coupling process.•Hypericin with the purity of ...98.7 % was obtained from the extracts efficiently.•XAD16 N column chromatography showed an excellent stability and reproducibility.
Hypericin has shown promising potential for the prevention and treatment of cancer. Here we report facile strategy for the separation and purification of natural products from the extracts by demonstrating hypericin isolation from Hypericum perforatum L. extract using macroporous resin column chromatography (MRCC) followed by preparative liquid chromatography (PLC). Effect of various parameters including the kinds of resins, loading extract concentration, loading flow rate, types of eluent, and elution flow rate on the separation efficiency of MRCC for hypericin was investigated. The purity and purification ratio of hypericin was 71.8 % and 2.4 respectively, optimized by XAD16 N MRCC with a high stability and reproducibility. PLC parameters were determined by optimizing stationary phase, mobile phase, and injection sample amount. The high purity hypericin (98.7 %) was achieved by PLC and the total recovery ratio of hypericin was 80.6 % in the coupling process.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
Hypericum perforatum is a perennial plant, with worldwide distribution, commonly known as St. John's wort. It has been used for centuries in traditional medicine for the treatment of several ...disorders, such as minor burns, anxiety, and mild to moderate depression. In the past years, its antidepressant properties have been extensively studied. Despite that, other H. perforatum biological activities, as its neuroprotective properties have also been evaluated. The present review aims to provide a comprehensive summary of the main biologically active compounds of H. perforatum, as for its chemistry, pharmacological activities, drug interactions and adverse reactions and gather scattered information about its neuroprotective abilities. As for this, it has been demonstrated that H. perforatum extracts and several of its major molecular components have the ability to protect against toxic insults, either directly, through neuroprotective mechanisms, or indirectly, through is antioxidant properties. H. perforatum has therefore the potential to become an effective neuroprotective therapeutic agent, despite further studies that need to be carried out.
Saint John's wort (
L., HP) is commonly registered in Europe under the THR scheme (Traditional Herbal Registration) or licensed as a medicine. Nonetheless unregulated medical products and food ...supplements are accessible through the internet which are often of poor quality. The species' natural distribution stretches through large regions of Europe to China and four subspecies have been distinguished. When compared to the European Pharmacopoeia reference, the presence of additional compounds was linked to so-called Chinese HP.
In order to obtain an integrated picture of the entire chemoprofile, the chemical composition of HP
was studied using a combination of techniques well-established in the relevant industries. The impact of phytogeographic factors on the
can shed light on whether the variability of the final products is strongly influenced by these factors of whether they relate to poor processing, adulteration, or other factors linked to the processing of the material.
Eighty-six
samples (77
.
) were collected from 14 countries. Most were authenticated and harvested in the wild; others came as roughly ground material from commercial cultivations, markets and pharmacies. The samples were analyzed using HPTLC and
H-NMR-based principal component analysis (PCA).
Limited chemical variability was found. Nonetheless, the typical fingerprint of Chinese HP was observed in each specimen from China. Additional compounds were also detected in some samples collected in Spain. Rutin is not necessarily present in the crude material. The variability previously found in the marketed products can be ascribed only partially to the geographical origin of harvested material, but mainly to the plant part harvested, closely related to harvesting techniques, processing and probably time of harvest.
HP can be sourced in a consistent composition (and thus quality) from different geographical sources. However, chemical variability needs to be accounted for when evaluating what is considered authentic good material. Therefore, the processing and good practice are all stages of primary importance, calling for a better (self-)regulation and quality assurance along the value chain of an herbal medical product or botanical.
urpose: Nanostructured lipid carriers (NLC) can improve the stability of various phytochemicals, so this research aimed to develop and employ such delivery systems for Hypericum perforatum extract ...containing the light- and oxygen-sensitive phloroglucinol hyperforin. Materials and methods: By varying the processing parameters and the solid and liquid lipids used, different NLC models were obtained via emulsification, followed by high-shear homogenization and ultrasonication. After characterization of the elaborated nanocarriers, those that exhibited optimal properties were loaded with St. John's wort extract by incorporating it in the lipid phase before emulsification and also studied. Results: The NLC models developed by prolonged ultrasonication demonstrated favorable characteristics regarding particle size, polydispersity index (PDI), and zeta potential (ZP). The physically stable during long-term storage nanosystems, which also showed a reduced degree of crystallinity of the solid lipid included, were loaded with St. John's wort extract. Of the carriers so-obtained, those developed by ultrasonication at ambient temperatures can be described as acceptably uniform systems (PDI from 0.23±0.01 to 0.27±0.01), comprising particles with dimensions below 200 nm, favorable ZP values (ζ > |30 mV|), and superior entrapment efficacy (EE) greater than 85%. Conclusion: In this research, different stable NLC dispersions were successfully developed. After the inclusion of the St. John's wort extract, the model possessing the highest EE (87.77±0.64%) was chosen as a carrier to conduct further studies evaluating its wound-healing potential.
Background: Colorectal cancer (CRC) continues to be a leading cause of cancer related death in the world and approximately 70 to 75 % of patients with metastatic colorectal cancer survive for up to 1 ...year after diagnosis. Curcumin (CUR) is a potential chemotherapeutic agent used to treat cancer. There is ample evidence of the inhibitory effects of Hypericum perforatum L. extract (HPE) on cell proliferation and its effects on the induction of apoptosis in various human cancer cell lines. Objective: The purpose of this study was to investigate the proapoptotic effect of HPE and its nanoliposomes (HPE-Lip) and to scrutinize the synergistic and therapeutic potential of HPE/CUR-loaded nanoliposome (HPE/CUR-Lip). Methods: In the present in vitro study, SW1116 and SW48 cell lines were cultured and then treated with different doses of HPE, CUR, bare liposome solely (Lip-Sol), and nanoliposomes loaded with HPE (HPE-Lip), CUR (CUR-Lip) and CUR/HPE (HPE/CUR-Lip) for 24, 48 and 72 hours. Cytotoxicity was measured by MTT assay and apoptosis rate by an annexin-V FITC/propidium iodide double-staining method using flow cytometry. Results: The results showed that cell viability was inhibited in a dose-dependent and time-dependent manner in all groups compared to the control group. The use of nanoliposomes improved the outcomes. HPE/CUR-Lip exhibited higher in vitro cytotoxic and proapoptotic activity against SW1116 and SW48 cell lines (P < 0.05). Conclusion: The findings of this study suggest that the HPE/CUR-Lip complex could provide a potential strategy to achieve a synergistic effect of HPE and CUR in the treatment of colorectal cancer.
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