Planta medica最新文献

Alzheimer's disease (AD) is a neurodegenerative condition with marked cognitive loss and impaired thinking abilities as well as spatial memory, working memory, and communication skills. Numerous studies have found that both type 1 and type 2 diabetes lead to neuropathological and neurobehavioral problems, which lead to notable cognitive dysfunction and deterioration in memory. The aims of this study are to find out the neuroprotective potential of eupalitin on memory in streptozotocin-induced diabetic rats and to evaluate its in silico binding affinity on acetylcholinesterase by using molecular docking studies. Eupalitin (dose 1 mg/kg/day) was used to study the behavior model and other biochemical parameters measurement in acute as well as chronic streptozotocin (STZ)-induced diabetic rats. Eupalitin treatment increased the level of acetylcholinesterase (AChE) and lipid peroxidation and decreased glutathione in STZ-infused diabetic rat's brain tissue, suggesting that this substance may modulate cognitive function that is altered by oxidative stress. Results were comparable to standard drugs metformin and donepezil. Docking score and molecular mechanics generalized born surface area (MMGBSA) study results of eupalitin in comparison with donepezil possess superior predicted binding affinity toward AChE. The level of Aβ _(1 - 42) was considerably lower in the eupalitin-treated group than in the STZ-treated group during both the acute and chronic phases of treatment, but results were more prominent in the case of chronic-level treatment. In silico studies showed the binding affinity toward AChE. This result concluded that eupalitin antioxidant potential may be utilized as a therapy for diabetes mellitus (DM)-related cognitive impairment.

Nitidine (NIT) was isolated from the bark of Zanthoxylum myriacanthum and assessed for anti-proliferative effects on NTERA-2 cancer stem cells using 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay, spheroid assay, DNA and lysosome staining, flow cytometry, caspase assay, immunoblotting, and molecular docking studies. Moreover, nitidine suppresses stemness properties like in vitro tumorsphere forming, c-myc, Oct4, Nanog proteins of NTERA-2 cancer stem cells after 48-hour treatment. Nitidine selectively induced anti-survival activities by triggering the intrinsic apoptotic process through p53 signaling and lysosome-dependent cell death (LDCD). The mechanism of action of nitidine on cancer stem cells was also investigated using molecular docking studies to provide physical insights. Molecular docking studies revealed that nitidine induces LDCD by effectively inhibiting the MHR1/2 domain of the TRPM2 protein on liposome membrane. These results suggested the potential capacity of nitidine in inhibiting cancer stem cells or tumor-initiating cells for therapeutic cancer application.

Rauvolfia serpentina produces a number of indole alkaloids and has long been used in the traditional treatment of arrhythmia. Given the shortage of natural resources, the K-27M strain of R. serpentina tissue culture was established. The aim was to evaluate the antiarrhythmic activity of extracts with different compositions and ratios of indole alkaloids derived from the cell biomass of the K-27M strain. Chemical analysis was conducted using HPLC-MS. Adrenaline-induced (rats) and ischemia-reperfusion arrhythmia (isolated guinea pig hearts) models were used to study the antiarrhythmic activity of the extracts. Extracts were obtained from dry (extracts 1, 2, and 3) and fresh biomass (fractions 1 and 2 of extract 4). Extract 1 contained ajmaline and acetylajmaline (the total indole alkaloid content (TIAC) was 2.2% of the dry biomass); extract 2-ajmaline, acetylajmaline, and raucaffricine (TIAC 6.4%); extract 3-ajmaline and raucaffricine (TIAC 29.0%). Fraction 1 of extract 4 was dominated by vomilenine, methylajmalicine, ajmalicine, and raufloridine (TIAC 65.0%), and fraction 2 of extract 4 contained acetylajmaline (TIAC 47.4%). Extracts 1 and 2 containing negligible amounts of indole alkaloids showed a weak proarrhythmic effect. Fractions 1 and 2 of extract 4 had a pronounced antiarrhythmic effect in the adrenaline-induced arrhythmia model. In addition, fraction 2 of extract 4 had an antiarrhythmic effect in the ischemia-reperfusion arrhythmia model. The level of this activity depended on the composition and ratio of alkaloids in the extract. Thus, the K-27M strain of R. serpentina tissue culture is a promising source of indole alkaloids with antiarrhythmic activity.

Kalopanax septemlobus (K. septemlobus) has been documented for therapeutic efficacy against scabies, but with fewer modern studies. In this paper, the inhibitory effects of K. semtemlobus extract and monomeric compounds on Trichophyton mentagrophytes and Trichophyton rubrum were studied, and the mechanism of action was preliminarily discussed. The chemical constituents of the ethyl acetate layer of K. semtemlobus were isolated and purified under the trace of antifungal activity (microdilution method). The structure was characterized by nuclear magnetic resonance spectroscopy (NMR) and mass spectrometry (MS); in vitro antifungal activity was investigated by microdilution (MIC, MFC), spore germination suppression, serum induced culture, extracellular protein determination, intracellular nucleic acid release, and PI fluorescence staining. Two compounds were isolated and elucidated, hederagenin (1: ) and kalopanaxsaponin A (2: ), respectively. The antifungal study showed that kalopanaxsaponin A had strong activity and could inhibit fungal growth from growth appreciation, transformation, and cell membrane (protein, nucleic acid leakage). The above data show that kalopanaxsaponin A has a strong antifungal effect (MIC₅₀=7.8 µg/mL), but in vivo and clinical experiments are needed to verify whether it has a curative effect. This study provides a potential compound for the development of natural antifungal drugs.

Wild garlic (Allium ursinum) is a wild plant growing in Middle and Eastern Europe that has been traditionally applied in local cuisine and herbal medicine practices. The leaves of the plant contain numerous bioactive compounds, i.e., flavonols, flavanols, phenolic acids, and thiopolysulfides. The aim of the study is to present the antioxidant, anti-inflammatory, and antimicrobial properties of this plant. The leaves of Allium ursinum possess strong antioxidant activity, which varies depending on extractant use and plant origin. The plant has limited capacity for ferric ion reduction in a FRAP test, as well. The previous studies showed that the high content of phenolic compounds was prevalently responsible for the high antiradical capacity. On the other hand, the thiopolysulfides present in the plant are responsible for its anti-inflammatory effect, observed as inhibition of TNF-α and interleukins, and as a bactericidal effect against skin pathogenic microflora. Wild garlic has a negative effect on cancer cell line viability, while it enhances the viability of non-cancerogenic tissue cells. All these effects clearly show that wild garlic is an interesting and potent raw material that should be more often applied in today's functional foods, as well as a novel additive for dietary supplements, herbal remedies, or materials with topical anti-bacterial action.

Parkinson's disease is characterized by an abnormal accumulation of alpha synuclein (α-syn) in different regions of the central nervous system. At present, only palliative pharmacological treatments are available for Parkinson´s disease. Immunotherapy is considered an alternative to treat Parkinson's disease, and plants are a convenient alternative platform for biopharmaceutical production. When compared to other systems, plants are particularly attractive because they offer cost-effectiveness, large-scale production, and enhanced safety. Therefore, this study aimed to establish a carrot cell suspension culture for the production of cLTB-Syn, a vaccine candidate against Parkinson's disease. The convenience of MS medium optimization was demonstrated. Transgenic callus cultures were maintained and adapted on solid MSU9 medium without phytohormones, followed by growth kinetics in suspension cultures. The maximum biomass yield was 15.8 ± 0.35 g/L DW at 14 days of culture, with a growth rate of µ = 0.1034/d and td = 6.7 days. The cLTB-Syn protein production reached a maximum value of 2.62 ± 0.03 µg/g DW, representing a 1.6-fold increase over the initial culture time. Finally, the presence of the transgene was confirmed by PCR, and the integrity of cLTB-Syn protein was determined by dot blot assays. This study presents evidence of a promising system for a toxin-free biopharmaceutical production, which has the potential to be scaled up for large manufacturing, at a low cost.

Inonotus obliquus is widely recognized as the Chaga mushroom. Chaga contains various bioactive compounds, including polysaccharides, triterpenoids, polyphenols, and melanin. To address the characterization and quantitative analysis of triterpenoids and phenolics in Chaga, a multi-analytical approach has been developed combining LC-PDA-ELSD and LC-DAD-QToF. These methods were designed to quantify 11 compounds, comprising seven triterpenoids and four fatty acids, using LC-PDA-ELSD, and four phenolics using the LC-DAD-QToF method. Calibration curves for these compounds demonstrated excellent linearity within the tested range. The methods exhibited high precision, with intra- and inter-day relative standard deviations below 3% and recoveries ranged from 91% to 104%. The validated methods were applied to analyze eleven sclerotia samples, one mycelium sample, three grain-based samples, and eighteen dietary supplements. Results revealed that eight of the eighteen supplements (44%) contained ground mycelium, which primarily showed the presence of fatty acids but lacks detectable levels of triterpenoid and phenolic markers characteristic of Chaga. Triterpenoids and hispidin, identified as key bioactive compounds, were detected in eight (44%) of the eighteen supplements; however, these products also contained fatty acids and/or betulin. Two (11%) of the 18 supplements showed the presence of phenolic compounds only; no triterpenoids were detected. Additionally, untargeted metabolomic screening using LC-DAD-QToF tentatively identified 103 compounds from diverse chemical groups, including nine reference compounds. These findings provide valuable insights for the quality assessment of dietary or food supplements marketed as containing Chaga.

Six previously undescribed polycyclic polyprenylated acylphloroglucinols (PPAPs) with a vicinal diol moiety (1: -6: ) were isolated from the whole plant of Hypericum himalaicum. Their structures were established through a comprehensive analysis of HRMS and 1D and 2D NMR data, while the absolute configurations were determined using the Mo₂(OAc)₄-induced circular dichroism (ICD), ECD, and NMR calculations. Compound 1: attenuated the secretion of NO, TNF-α, and IL-6, downregulated the protein expression of COX-2 and iNOS, and inhibited the release of ROS in LPS-induced RAW264.7 macrophages. Further investigation revealed that the anti-inflammatory effects may be attributed to the inhibition of the NF-κB and NLRP3 signaling pathways.

Saikosaponins, bioactive compounds derived from Bupleurum falcatum roots, have limited applications due to their low bioavailability and the absence of efficient large-scale separation methods. To address this, an enzymatic transformation in vitro with cellulase was employed to remove glucose at the C-3 position, producing lipophilic prosaikogenins. These metabolites were separated using countercurrent chromatography (CCC) and preparative HPLC. The optimal CCC solvent system was determined to be dichloromethane/methanol/water (4 : 3 : 2, v/v/v). Prosaikogenin F and prosaikogenin G (PSG G) were isolated from the deglycosylated fraction, and the effect of rotation speed on compound retention was examined. Further enzymatic biotransformation using α-L-rhamnosidase and cellulase resulted in the isolation of prosaikogenins E₁ and E₃. The efficient separation of these four prosaikogenins was achieved through a combination of enzymatic transformation and CCC. Of these, PSG G demonstrated the strongest anticancer activity against the cancer cell lines MDA-MB-468, HepG2, and HCT116, while exhibiting lower toxicity in normal cells, supporting its potential as an effective anticancer agent. This study presents a highly efficient enzymatic transformation and separation strategy that can aid in the pharmaceutical development of saikosaponin derivatives.

There is growing evidence highlighting the pivotal role of cellular metabolic adaptation in governing diverse immune responses, as well as the capacity of immune cells to alter metabolic preferences. In both scenarios, the prospect of leveraging bioactive compounds to induce metabolic reprogramming emerges as a novel adjuvant strategy for clinical immunotherapy. Rg1, a major active ginsenoside found in ginseng roots, has the potential to function as a glucocorticoid receptor agonist. Unraveling the intricate relationship between anti-inflammatory functions and the metabolic effects of ginsenosides and glucocorticoids may contribute to the identification of metabolic biomarkers associated with anti-inflammation. This research aims to determine endogenous metabolic response differences evoked by Rg1 and glucocorticoids underlying in vivo anti-inflammatory responses. The metabolic impact, particularly on primary metabolites, was assessed in zebrafish embryos using gas chromatography-mass spectrometry (GC-MS) in conjunction with metabolic pathways analysis via the KEGG pathway database. Our results indicated that Rg1 possesses a similar effect in alleviating inflammation in treating injured zebrafish as beclomethasone. The anti-inflammatory effects of Rg1 are achieved by inhibiting the neutrophils and macrophages toward the amputated edges and upregulating gene expression associated with pro-inflammatory cytokines. The anti-inflammatory effects of Rg1 also include changes in fatty-acid metabolism and downstream aromatic amino acids in the TCA cycle. Therefore, Rg1 may be a promising drug candidate for treating inflammatory responses and a valuable supplement for enhancing immune regulation.