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Plants (Basel, Switzerland) May 2024Medicinal plant tissue cultures are potential sources of bioactive compounds. In this study, we report the chemical characterization of the callus cultures of three...
Medicinal plant tissue cultures are potential sources of bioactive compounds. In this study, we report the chemical characterization of the callus cultures of three medicinal spp. (, and ), along with the comparison to bracts and flowers of the same species. Our aim was to show that calli of spp. are good alternatives to the calli of for the production of polyphenols and are better sources of a subset of polyphenolic metabolites, compared to the original organs. Calli were initiated from young bracts and grown on woody plant medium containing 1 mg L 2,4-D and 0.1 mg L BAP. For chemical characterization, a quality-controlled untargeted metabolomics approach and the quantification of several bioactive compounds was performed with the use of LC-ESI-MS/MS. While bracts and flowers contained flavonoid glycosides (astragalin, isoquercitrin) as major polyphenols, calli of all species contained catechins, coumarins (fraxin, esculin and scopoletin) and flavane aglyca. calli contained 5397 µg g DW catechin, 201 µg g DW esculin, 218 µg g DW taxifolin and 273 µg g DW eriodictyol, while calli from other species contained lower amounts. and flowers were rich in isoquercitrin, containing 8134 and 6385 µg g DW, respectively. The currently tested species contained many of the bioactive metabolites described from . The production of catechin was shown to be comparable to the most efficient tissue cultures reported. Flowers and bracts contained flavonoid glycosides, including tiliroside, resembling bioactive fractions of . In addition, untargeted metabolomics has shown fingerprint-like differences among species, highlighting possible chemotaxonomic and quality control applications, especially for bracts.
PubMed: 38794359
DOI: 10.3390/plants13101288 -
BMC Infectious Diseases May 2024In November 2019, the world faced a pandemic called SARS-CoV-2, which became a major threat to humans and continues to be. To overcome this, many plants were explored to...
BACKGROUND
In November 2019, the world faced a pandemic called SARS-CoV-2, which became a major threat to humans and continues to be. To overcome this, many plants were explored to find a cure.
METHODS
Therefore, this research was planned to screen out the active constituents from Artemisia annua that can work against the viral main protease Mpro as this non-structural protein is responsible for the cleavage of replicating enzymes of the virus. Twenty-five biocompounds belonging to different classes namely alpha-pinene, beta-pinene, carvone, myrtenol, quinic acid, caffeic acid, quercetin, rutin, apigenin, chrysoplenetin, arteannunin b, artemisinin, scopoletin, scoparone, artemisinic acid, deoxyartemisnin, artemetin, casticin, sitogluside, beta-sitosterol, dihydroartemisinin, scopolin, artemether, artemotil, artesunate were selected. Virtual screening of these ligands was carried out against drug target Mpro by CB dock.
RESULTS
Quercetin, rutin, casticin, chrysoplenetin, apigenin, artemetin, artesunate, sopolin and sito-gluside were found as hit compounds. Further, ADMET screening was conducted which represented Chrysoplenetin as a lead compound. Azithromycin was used as a standard drug. The interactions were studied by PyMol and visualized in LigPlot. Furthermore, the RMSD graph shows fluctuations at various points at the start of simulation in Top1 (Azithromycin) complex system due to structural changes in the helix-coil-helix and beta-turn-beta changes at specific points resulting in increased RMSD with a time frame of 50 ns. But this change remains stable after the extension of simulation time intervals till 100 ns. On other side, the Top2 complex system remains highly stable throughout the time scale. No such structural dynamics were observed bu the ligand attached to the active site residues binds strongly.
CONCLUSION
This study facilitates researchers to develop and discover more effective and specific therapeutic agents against SARS-CoV-2 and other viral infections. Finally, chrysoplenetin was identified as a more potent drug candidate to act against the viral main protease, which in the future can be helpful.
Topics: SARS-CoV-2; Artemisia annua; Molecular Docking Simulation; Coronavirus 3C Proteases; Humans; Phytochemicals; COVID-19 Drug Treatment; Antiviral Agents; Plant Extracts; Computer Simulation; Protease Inhibitors; COVID-19; Molecular Dynamics Simulation
PubMed: 38750422
DOI: 10.1186/s12879-024-09387-w -
Metabolites Apr 2024Sweet potato ( (L.) Lam.) belongs to family Convolvulaceae. The plant is distributed worldwide and consumed, especially for its edible tubers. Many studies have proved...
A Comparative Analysis of Polysaccharides and Ethanolic Extracts from Two Egyptian Sweet Potato Cultivars, Abees and A 195: Chemical Characterization and Immunostimulant Activities.
Sweet potato ( (L.) Lam.) belongs to family Convolvulaceae. The plant is distributed worldwide and consumed, especially for its edible tubers. Many studies have proved that the plant has variable biological activities such as antidiabetic, anti-cancer, antihypertensive, antimicrobial, and immunostimulant activities. The roots of sweet potatoes are rich in valuable phytochemical constituents that vary according to the flesh color. Our investigation focused on the chemical profiling of two Egyptian sweet potato cultivars, Abees and A 195, using UPLC-QTOF and the analysis of their polysaccharide fractions by GC-MS. Furthermore, we assessed the immunostimulant properties of these extracts in immunosuppressed mice. The study revealed that sweet potato roots contain significant concentrations of phenolic acids, including caffeoylquinic, caffeic, caffeoyl-feruloyl quinic, and p-coumaric acids, as well as certain flavonoids, such as diosmin, diosmetin, and jaceosidin, and coumarins, such as scopoletin and umbelliferone. Moreover, polysaccharides prepared from both studied cultivars were analyzed using GC-MS. Further biological analysis demonstrated that all the tested extracts possessed immunostimulant properties by elevating the level of WBCs, IL-2, TNF, and IFN-γ in the immunosuppressed mice relative to the control group with the highest values in polysaccharide fractions of A195 (the ethanolic extract showed a higher effect on TNF and IFN-γ, while its polysaccharide fraction exhibited a promising effect on IL-2 and WBCs). In conclusion, the roots of the Egyptian sweet potato cultivars Abees and A 195 demonstrated significant immunostimulant activities, which warrants further investigation through clinical studies.
PubMed: 38668350
DOI: 10.3390/metabo14040222 -
Frontiers in Pharmacology 2024Scopoletin is a coumarin synthesized by diverse medicinal and edible plants, which plays a vital role as a therapeutic and chemopreventive agent in the treatment of a... (Review)
Review
Scopoletin is a coumarin synthesized by diverse medicinal and edible plants, which plays a vital role as a therapeutic and chemopreventive agent in the treatment of a variety of diseases. In this review, an overview of the pharmacology, pharmacokinetics, and toxicity of scopoletin is provided. In addition, the prospects and outlook for future studies are appraised. Scopoletin is indicated to have antimicrobial, anticancer, anti-inflammation, anti-angiogenesis, anti-oxidation, antidiabetic, antihypertensive, hepatoprotective, and neuroprotective properties and immunomodulatory effects in both and experimental trials. In addition, it is an inhibitor of various enzymes, including choline acetyltransferase, acetylcholinesterase, and monoamine oxidase. Pharmacokinetic studies have demonstrated the low bioavailability, rapid absorption, and extensive metabolism of scopoletin. These properties may be associated with its poor solubility in aqueous media. In addition, toxicity research indicates the non-toxicity of scopoletin to most cell types tested to date, suggesting that scopoletin will neither induce treatment-associated mortality nor abnormal performance with the test dose. Considering its favorable pharmacological activities, scopoletin has the potential to act as a drug candidate in the treatment of cancer, liver disease, diabetes, neurodegenerative disease, and mental disorders. In view of its merits and limitations, scopoletin is a suitable lead compound for the development of new, efficient, and low-toxicity derivatives. Additional studies are needed to explore its molecular mechanisms and targets, verify its toxicity, and promote its oral bioavailability.
PubMed: 38464713
DOI: 10.3389/fphar.2024.1268464 -
Frontiers in Genetics 2024Litchi () is an important sub-tropical fruit in the horticulture market in China. Breeding for improved fruit characteristics is needed for satisfying consumer demands....
Litchi () is an important sub-tropical fruit in the horticulture market in China. Breeding for improved fruit characteristics is needed for satisfying consumer demands. Budding is a sustainable method for its propagation. During our ongoing breeding program, we observed a litchi mutant with flat leaves and sharp fruit peel cracking in comparison to the curled leaves and blunt fruit peel cracking fruits of the mother plant. To understand the possible molecular pathways involved, we performed a combined metabolome and transcriptome analysis. We identified 1,060 metabolites in litchi leaves and fruits, of which 106 and 101 were differentially accumulated between the leaves and fruits, respectively. The mutant leaves were richer in carbohydrates, nucleotides, and phenolic acids, while the mother plant was rich in most of the amino acids and derivatives, flavonoids, lipids and organic acids and derivatives, and vitamins. Contrastingly, mutant fruits had higher levels of amino acids and derivatives, carbohydrates and derivatives, and organic acids and derivatives. However, the mother plant's fruits contained higher levels of flavonoids, scopoletin, amines, some amino acids and derivatives, benzamidine, carbohydrates and derivatives, and some organic acids and derivatives. The number of differentially expressed genes was consistent with the metabolome profiles. Gene Ontology and Kyoto Encyclopedia of Genes and Genomes pathway-enriched gene expressions showed consistent profiles as of metabolome analysis. These results provide the groundwork for breeding litchi for fruit and leaf traits that are useful for its taste and yield.
PubMed: 38463170
DOI: 10.3389/fgene.2024.1360138 -
Plant Physiology and Biochemistry : PPB Mar 2024Plants produce a myriad of specialized compounds in response to threats such as pathogens or pests and different abiotic factors. The stress-related induction of...
Plants produce a myriad of specialized compounds in response to threats such as pathogens or pests and different abiotic factors. The stress-related induction of specialized metabolites can be mimicked using silver nitrate (AgNO) as an elicitor, which application in conservation agriculture has gained interest. In Arabidopsis thaliana, AgNO triggers the accumulation of indole glucosinolates (IGs) and the phytoalexin camalexin as well as pheylpropanoid-derived defensive metabolites such as coumaroylagmatins and scopoletin through a yet unknown mechanism. In this work, the role of jasmonic (JA) and salicylic acid (SA) signaling in the AgNO-triggered specialized metabolite production was investigated. To attain this objective, AgNO, MeJA and SA were applied to A. thaliana lines impaired in JA or SA signaling, or affected in the endogenous levels of IGs and AGs. Metabolomics data indicated that AgNO elicitation required an intact JA and SA signaling to elicit the metabolic response, although mutants impaired in hormone signaling retained certain capacity to induce specialized metabolites. In turn, plants overproducing or abolishing IGs production had also an altered hormonal signaling response, both in the accumulation of signaling molecules and the molecular response mechanisms (ORA59, PDF1.2, VSP2 and PR1 gene expression), which pointed out to a crosstalk between defense hormones and specialized metabolites. The present work provides evidence of a crosstalk mechanism between JA and SA underlying AgNO defense metabolite elicitation in A. thaliana. In this mechanism, IGs would act as retrograde feedback signals dampening the hormonal response; hence, expanding the signaling molecule concept.
Topics: Arabidopsis; Plant Growth Regulators; Arabidopsis Proteins; Silver Nitrate; Oxylipins; Cyclopentanes; Salicylic Acid; Gene Expression Regulation, Plant; Plant Diseases
PubMed: 38457948
DOI: 10.1016/j.plaphy.2024.108483 -
Chinese Medicine Mar 2024Liver cirrhosis is a chronic liver disease with hepatocyte necrosis and lesion. As one of the TCM formulas Wuling Powder (WLP) is widely used in the treatment of liver...
BACKGROUND
Liver cirrhosis is a chronic liver disease with hepatocyte necrosis and lesion. As one of the TCM formulas Wuling Powder (WLP) is widely used in the treatment of liver cirrhosis. However, it's key functional components and action mechanism still remain unclear. We attempted to explore the Key Group of Effective Components (KGEC) of WLP in the treatment of Liver cirrhosis through integrative pharmacology combined with experiments.
METHODS
The components and potential target genes of WLP were extracted from published databases. A novel node importance calculation model considering both node control force and node bridging force is designed to construct the Function Response Space (FRS) and obtain key effector proteins. The genetic knapsack algorithm was employed to select KGEC. The effectiveness and reliability of KGEC were evaluated at the functional level by using gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis. Finally, the effectiveness and potential mechanism of KGEC were confirmed by CCK-8, qPCR and Western blot.
RESULTS
940 effective proteins were obtained in FRS. KEGG pathways and GO terms enrichments analysis suggested that effective proteins well reflect liver cirrhosis characteristics at the functional level. 29 components of WLP were defined as KGEC, which covered 100% of the targets of the effective proteins. Additionally, the pathways enriched for the KGEC targets accounted for 83.33% of the shared genes between the targets and the pathogenic genes enrichment pathways. Three components scopoletin, caryophyllene oxide, and hydroxyzinamic acid from KGEC were selected for in vivo verification. The qPCR results demonstrated that all three components significantly reduced the mRNA levels of COL1A1 in TGF-β1-induced liver cirrhosis model. Furthermore, the Western blot assay indicated that these components acted synergistically to target the NF-κB, AMPK/p38, cAMP, and PI3K/AKT pathways, thus inhibiting the progression of liver cirrhosis.
CONCLUSION
In summary, we have developed a new model that reveals the key components and potential mechanisms of WLP for the treatment of liver cirrhosis. This model provides a reference for the secondary development of WLP and offers a methodological strategy for studying TCM formulas.
PubMed: 38429802
DOI: 10.1186/s13020-024-00896-z -
Ultrasonics Sonochemistry Feb 2024Solanum pseudocapsicum (PC) and Capsicum annum (CA) belongs to the family of Solanaceae. CA have been reported a rich source of phenolics whereas, the phenolics content...
BACKGROUND
Solanum pseudocapsicum (PC) and Capsicum annum (CA) belongs to the family of Solanaceae. CA have been reported a rich source of phenolics whereas, the phenolics content of GA (gallic acid), SC (scopoletin), RA (rosmarinic acid), and RV (resveratrol) are yet to be reported for the PC-fruit. This study comparatively evaluates the phenolics profile for different parts (seeds and skin) and colors (green and red) of the PC- and CA-fruits using the green solvents of ethanol (ET), acetone (AC), water (HO), and different combinations of these solvents.
METHODOLOGY
Ultrasonics extraction (US) and UHPLC analysis were employed for phenolics evaluation.
RESULTS
The USMD (method development) revealed the highest extract yield of 62 mg/100 mg for the PC-skin in ET:AC (70:30) solvent whereas, more phenolics (ppm) were observed for PC-seeds in ET:AC (50:50) solvent, particularly the SC (29.46) and GA (16.92). The UHPLCMDMV exhibited significant accuracies (100.70-114.14 %) with r-values (0.9993-0.9997) in the linearity range of 1-200 ppm. The USMV (method validation) in PC- and CA-fruit parts and colors revealed more extract yields for the red skin part of the PC- (180.5 mg) and CA-fruit (126.2 mg). The phenolics were seen more in the green seeds of the PC-fruit (ppm); SC (276), GA (147.36), RV (28.54), and RA (23.87) followed by the green PC-skin, and red/green CA-seeds. The statistical models of mean differences, ANOVA, and Pearson's correlation showed significant differences for the PC-fruit parts (seeds and skin) and colors (red and green) vs extract yield and phenolics content (P = 0.05).
CONCLUSION
PC-and CA-fruits were successfully evaluated where the seeds for the green fruits exhibited more phenolics amount.
Topics: Capsicum; Solanum; Ultrasonics; Chromatography, High Pressure Liquid; Plant Extracts; Phenols; Solvents; Fruit; Antioxidants; Ethanol; Camphor; Menthol; Acetone
PubMed: 38309047
DOI: 10.1016/j.ultsonch.2024.106789 -
ACS Earth & Space Chemistry Dec 2023Coumarins are exuded into the soil environment by plant roots in response to iron (Fe) deficiency. Previous studies have shown that coumarins can increase the Fe...
Coumarins are exuded into the soil environment by plant roots in response to iron (Fe) deficiency. Previous studies have shown that coumarins can increase the Fe solubility upon interaction with sparsely soluble Fe(III) (hydr)oxide. However, the chemical mechanisms of Fe(III) (hydr)oxide dissolution by coumarins remain unclear. The high redox instability of dissolved coumarins and the interference of coumarins in determining the Fe redox state hinder the quantitative and mechanistic investigation of coumarin-induced Fe mobilization. In this study, we investigated the oxidative stability of three coumarins that have been found in root exudates, esculetin, scopoletin, and fraxetin, over a broad pH range under oxic and anoxic conditions. Our results show that the oxidation of coumarins is irreversible under oxic conditions and that oxidative degradation rates increased with increasing pH under both oxic and anoxic conditions. However, the complexation of Fe protects coumarins from degradation in the circumneutral pH range even under oxic conditions. Furthermore, we observed that Ferrozine, which is commonly used for establishing Fe redox speciation, can facilitate the reduction of Fe(III) complexed by coumarins, even at circumneutral pH. Reduction rates increased with decreasing pH and were larger for fraxetin than for scopoletin and esculetin. Based on these observations, we optimized the Ferrozine method for determining the redox state of Fe complexed by coumarins. Understanding the stability of dissolved coumarins and using a precise analytical method to determine the redox state of Fe in the presence of coumarins are critical for investigating the mechanisms by which coumarins enhance the availability of Fe in the rhizosphere.
PubMed: 38148994
DOI: 10.1021/acsearthspacechem.3c00199 -
Journal of Experimental Botany Feb 2024Production of the phytoalexins scopoletin and scopolin is regulated by jasmonate (JA) and ethylene signaling in Nicotiana species in response to Alternaria alternata,...
Production of the phytoalexins scopoletin and scopolin is regulated by jasmonate (JA) and ethylene signaling in Nicotiana species in response to Alternaria alternata, the necrotrophic fungal pathogen that causes brown spot disease. However, how these two signaling pathways are coordinated to control this process remains unclear. In this study, we found that the levels of these two phytoalexins and transcripts of their key enzyme gene, feruloyl-CoA 6'-hydroxylase 1 (NaF6'H1), were synergistically induced in Nicotiana attenuata by co-treatment with methyl jasmonate (MeJA) and ethephon. By combination of RNA sequencing and virus-induced gene silencing, we identified a WRKY transcription factor, NaWRKY70, which had a similar expression pattern to NaF6'H1 and was responsible for A. alternata-induced NaF6'H1 expression. Further evidence from stable transformed plants with RNA interference, knock out and overexpression of NaWRKY70 demonstrated that it is a key player in the synergistic induction of phytoalexins and plant resistance to A. alternata. Electrophoretic mobility shift, chromatin immunoprecipitation-quantitative PCR, and dual-luciferase assays revealed that NaWRKY70 can bind directly to the NaF6'H1 promoter and activate its expression. Furthermore, the key regulator of the ethylene pathway, NaEIN3-like1, can directly bind to the NaWRKY70 promoter and activate its expression. Meanwhile, NaMYC2s, important JA pathway transcription factors, also indirectly regulate the expression of NaWRKY70 and NaF6'H1 to control scopoletin and scopolin production. Our data reveal that these phytoalexins are synergistically induced by JA and ethylene signaling during A. alternata infection, which is largely mediated by NaWRKY70, thus providing new insights into the defense responses against A. alternata in Nicotiana species.
Topics: Nicotiana; Phytoalexins; Scopoletin; Ethylenes; Cyclopentanes; Oxylipins; Transcription Factors
PubMed: 37870145
DOI: 10.1093/jxb/erad415