Dracocephalum Rupestre Research Articles

Therapeutic potential of compound extract from Dracocephalum Rupestre Hance and Berberidis Radix against Salmonella-induced lamb diarrhea

Lamb diarrhea is primarily induced by bacterial infections, causing great economic and health challenges. Traditional antibiotic treatments raise concerns over drug resistance and environmental contamination. We explored the therapeutic potential of a compound extract from Dracocephalum rupestre Hance and Berberidis Radix against Salmonella-induced diarrhea in lamb. Twenty-five five-week-old Kunming mice (20 ± 5 g) were used. A controlled laboratory experiment, combing histological examinations, serum cytokine level analysis, gut microbiota composition analysis, and short-chain fatty acid quantification were conducted. Results demonstrated significant reparative effects on intestinal mucosal damage of the compound. Compound treatment notably reduced serum levels of inflammatory cytokines (IL-6, IL-8, sigA, and TNF-α), indicating an anti-inflammatory effect. Gene expression analysis of mucosal repair markers (PCNA, TGF, and EGFR) confirmed the positive impacts on intestinal recovery processes after treatment. Microbiota analysis revealed concentration-dependent alterations in gut microbial composition, with a notable increase in beneficial bacterial genera such as Muribaculum and Prevotella, suggesting the role of the compound in promoting gut health. Additionally, short-chain fatty acid analysis indicated an increase in beneficial acids, which are critical for the gut and overall health. This investigation highlights the potential therapeutic benefits of Dracocephalum rupestre Hance combining Berberidis Radix in lamb with Salmonella-induced diarrhea.

Identification of volatile and odor-active compounds in Maojian herbal tea (Dracocephalum rupestre Hance)

Maojian herbal tea originates from Xinzhou, Shanxi, China, and is renowned as one of the prominent northern Chinese herbal teas. However, the volatile and key odor-active compounds in Maojian herbal tea have not been reported. Using headspace-solid-phase microextraction coupled with gas chromatography–mass spectrometry, a total of 87 volatile compounds were identified. Thirteen aroma compounds were distinguished as the key odor-active compounds of Maojian herbal tea based on gas chromatography–olfactometry analysis, and odor activity values, including trans-β-ionone, cis-jasmone, β-caryophyllene, humulene, hexanal, nonanal, linalool, alloocimene B, β-cyclocitral, β-bourbonene, ylangene, δ-cadinene and indole. The results of partial least squares regression analysis demonstrate strong correlations between the odor-active compounds and odor properties. β-Caryophyllene is the main contributor to the woody aroma of Maojian herbal tea. The results of the present study offer a scientific insight into the aroma profile of Maojian herbal tea.

High-throughput MALDI-MSI metabolite analysis of plant tissue microarrays.

A novel metabolomics analysis technique, termed matrix-assisted laser desorption/ionization mass spectrometry imaging-based plant tissue microarray (MALDI-MSI-PTMA), was successfully developed for high-throughput metabolite detection and imaging from plant tissues. This technique completely overcomes the disadvantage that metabolites cannot be accessible on anintact plant tissue due to the limitations of the special structures of plant cells (e.g. epicuticular wax, cuticle and cell wall) through homogenization of plant tissues, preparation of PTMA moulds and matrix spraying of PTMA sections. Our study shows several properties of MALDI-MSI-PTMA, including no need of sample separation and enrichment, high-throughput metabolite detection and imaging (>1000 samples per day), high-stability mass spectrometry data acquisition and imaging reconstruction and high reproducibility of data. This novel technique was successfully used to quickly evaluate the effects of two plant growth regulator treatments (i.e. 6-benzylaminopurine and N-phenyl-N'-1,2,3-thiadiazol-5-ylurea) on endogenous metabolite expression in plant tissue culture specimens of Dracocephalum rupestre Hance (D.rupestre). Intra-day and inter-day evaluations indicated that the metabolite data detected on PTMA sections had good reproducibility and stability. A total of 312 metabolite ion signals inleaves tissues of D. rupestre were detected, of which 228 metabolite ion signals were identified, they were composed of 122 primary metabolites, 90 secondary metabolites and 16 identified metabolites of unknown classification. The results demonstrated the advantages of MALDI-MSI-PTMA technique for enhancing the overall detection ability of metabolites in plant tissues, indicating that MALDI-MSI-PTMA has the potential to become a powerful routine practice for high-throughput metabolite study in plant science.

The complete chloroplast genome sequence of the medicinal plant, Dracocephalum rupestre (Lamiaceae)

Dracocephalum rupestre (tribe Mentheae; Lamiaceae) is a perennial herb from Korea and China with high ornamental and medicinal value. Here, we report its complete chloroplast genome to provide insight into the phylogenetic relationships of Dracocephalum. The genome is 151,230 bp long, with two inverted repeat regions (25,643 bp each) that separate a large single-copy region (82,536 bp) and a small single-copy region (17,408 bp). It contains 133 genes that encode 88 proteins, eight rRNAs, and 37 tRNAs. The maximum-likelihood phylogenetic analysis strongly supported Dracocephalum monophyly, showing that the genus forms a sister group with the subtribe Menthinae in the tribe Mentheae.

The complete chloroplast genome sequence of <i>Dracocephalum rupestre</i> (Lamiaceae)

<i>Dracocephalum rupestre</i> Hance is a perennial herb distributed across China, Mongolia, and Korea. This study reports the first complete chloroplast genome sequence of <i>D. rupestre</i>. The plastome is 151,230 bp long and exhibits a typical quadripartite structure comprising a large single-copy region of 82,536 bp, a small single-copy region of 17,408 bp, and a pair of identical inverted repeat regions of 25,643 bp each. It contains 130 genes, comprising 85 protein-coding genes, 37 tRNA genes, and eight rRNA genes. Phylogenetic analysis of <i>D. rupestre</i> and related species of Lamiaceae showed that the genus <i>Dracocephalum</i> is a monophyletic group, and <i>D. rupestre</i> is most closely related to <i>D. psammophilum</i>.

Metabolomic characterization of the chemical compositions of Dracocephalum rupestre Hance

Maojian tea (MJT) is a traditional Chinese herbal tea beverage manufactured from the leaves of the Dracocephalum rupestre Hance plant. In this study, a nontargeted metabolomics approach combined with absolute quantifications was applied to comprehensively investigate the chemical compositions of MJT and to determine the effects of the processing methods on compounds. Flavones (apigenin and luteolin, 0.06–1.35 mg/g), flavanones (eriodictyol and naringenin, 0.1–2.3 mg/g), flavone 7-O-glycosides (0.15–5.98 mg/g), flavanone 7-O-glycosides (0.28–19.41 mg/g), and triterpenoids were presumed to be characteristic components of MJT. Applying imitative green and black tea processing methods to MJT led to increases in flavone/flavanone aglycones, lipids, and triterpenoids and decreases in flavone/flavanone glycosides, amino acids, organic acids, and most phenolic acids. This study offers novel insights into the chemical compositions and the influences of processing methods on MJT and will be utilized for the quality control of MJT.

野生毛建草的引种驯化试验初报

毛建草是多年生草本植物，具有很高的药用价值和商业价值。由于野生毛建草资源缺失，因此野生毛建草的引种驯化是解决毛建草资源日益减少的根本途径。本研究以包头九峰山采集的野生毛建草种子为试验材料，在呼和浩特地区进行引种驯化栽培试验。结果表明：野生毛建草引种栽培方式简单，生长能力强，管理方便，抗性强，是适宜集约化、规模化、标准化栽培的野生品种。 Dracocephalum rupestre is a perennial herb with high medicinal value and commercial value. Because of the lack of wild Dracocephalum rupestre resources, the introduction and domestication of wild Dracocephalum rupestre is the fundamental way to solve the decreasing resources of Dracocephalum rupestre. In this study, the seeds of wild Dracocephalum rupestre collected by Baotou Jiufeng Mountain were used as test materials, and the introduction and domestication cultivation experiments were carried out in Hohhot area. The results showed that the introduction and cultivation of wild Dracocephalum rupestre was simple, the growth ability was strong, the management was convenient, the resistance was strong, and it was suitable for intensive, large-scale and standardized cultivation of wild varieties.

Antioxidant activities and hepatoprotective potential of Dracocephalum rupestre Hance extract against CCl4 -induced hepatotoxicity in Kunming mice

Antioxidant activities and hepatoprotective potential of <i>Dracocephalum rupestre</i> Hance extract against CCl₄ -induced hepatotoxicity in Kunming mice

Biomimetic synthesis and HPLC-ECD analysis of the isomers of dracocephins A and B.

Starting from racemic naringenin ((±)-1), a mixture of dracocephin A stereoisomers 6-(2”-pyrrolidinone-5”-yl)naringenin (±)-2a–d and its regioisomer, dracocephin B 8-(2”-pyrrolidinone-5”-yl)naringenin (±)-3a–d originally isolated from Dracocephalum rupestre, have been synthesized in a one-pot reaction. The separation of 2a–d and 3a–d was achieved by preparative HPLC. The four stereoisomers of each natural product were separated by analytical chiral HPLC and their absolute configuration was studied by the combination of HPLC–ECD measurements and TDDFT–ECD calculations. The synthesized flavonoid alkaloids were further characterized by physicochemical and in vitro pharmacological studies.

Neuroinflammatory response to experimental stroke is inhibited by eriodictyol

BackgroundCerebral ischemia is a common disease and one of the most common causes of death and disability worldwide. The lack of glucose and oxygen in neuronal tissue leads to a series of inflammatory events, culminating in neuronal death. Eriodictyol is a flavonoid isolated from the Chinese herb Dracocephalum rupestre that has been proven to have anti-inflammatory properties. Hypothesis/PurposeThus, the present study was designed to explore whether eriodictyol has neuroprotective effects against the neuronal damage, motor and memory deficits induced by permanent middle cerebral artery occlusion (pMCAO) in mice. Study DesignAnimals were orally treated with eriodictyol (1, 2 and 4mg/kg) or vehicle (saline) 30min before pMCAO, 2h after, and then once daily for the following five days. MethodsThe parameters studied were neuronal viability, brain infarcted area; sensorimotor deficits; exploratory activity; working and aversive memory; myeloperoxidase (MPO) activity; TNFα, iNOS and GFAP immunoreactivity. ResultsThe treatment with eriodictyol prevented neuronal death, reduced infarct area and improved neurological and memory deficits induced by brain ischemia. The increase of MPO activity and TNF-α, iNOS and GFAP expression were also reduced by eriodictyol treatment. ConclusionThese findings demonstrate that eriodictyol exhibit promising neuroprotection effects against the permanent focal ischemia cerebral injury in the mice experimental model and the underlying mechanisms might be mediated through inhibition of neuroinflammation.

Eriodictyol Attenuates β-Amyloid 25–35 Peptide-Induced Oxidative Cell Death in Primary Cultured Neurons by Activation of Nrf2

Oxidative stress plays an important role in the pathogenesis of neurodegenerative diseases, including Alzheimer's disease (AD). Eriodictyol, a flavonoid isolated from the Chinese herb Dracocephalum rupestre, has long been established as an antioxidant. The present study was designed to investigate the effect of eriodictyol on β-amyloid 25-35 peptide (Aβ25-35)-induced oxidative cell death in primary neurons and to explore the role of the nuclear factor erythroid-2-related factor 2/antioxidant response element (Nrf2/ARE) pathway in this process. For this purpose, primary cultures of cortical neurons were exposed to 15μM Aβ25-35 in the absence or presence of eriodictyol (20, 40 and 80μM). The results revealed that Aβ25-35-induced cytotoxicity and apoptotic characteristics such as activation of JNK/p38 apoptotic signaling pathway were effectively attenuated by eriodictyol pretreatment. Eriodictyol treatment also resulted in an increase in Nrf2 protein levels and subsequent activation of ARE pathway genes in primary cultured neurons. The protective effects of eriodictyol were attenuated by RNA interference-mediated knockdown of Nrf2 expression. Taken together, these results clearly demonstrate that eriodictyol protects neurons against Aβ25-35-induced cell death partially through Nrf2/ARE signaling pathway, which further supports that eriodictyol might be a promising novel therapeutic agent for AD.

Eriodictyol protects against H2O2-induced neuron-like PC12 cell death through activation of Nrf2/ARE signaling pathway

Eriodictyol, a flavonoid isolated from the Chinese herb Dracocephalum rupestre has long been established as an antioxidant. The present study was designed to explore the protective effects of eriodictyol against hydrogen peroxide (H2O2)-induced neurotoxicity with cultured rat pheochromocytoma cells (PC12 cells) and the possible mechanisms involved. For this purpose, differentiated PC12 cells were cultured and exposed to 200μM H2O2 in the absence or presence of eriodictyol (20, 40 and 80μM). In addition, the potential contribution of the Nrf2/ARE neuroprotective pathway in eriodictyol-mediated protection against H2O2-induced neurotoxicity was also investigated. The results showed that H2O2-induced cell death can be inhibited in the presence of eriodictyol as measured by assays for MTT and apoptosis. Further study revealed that eriodictyol induced the nuclear translocation of Nrf2, enhanced the expression of heme oxygenase (HO-1) and γ-glutamylcysteine synthetase (γ-GCS), and increased the levels of intracellular glutathione. Treatment of PC12 cells with Nrf2 small interference RNA abolished eriodictyol-induced HO-1 and γ-GCS expression and its protective effects. In conclusion, these results suggest that eriodictyol upregulates HO-1 and γ-GCS expression through the activation of Nrf2/ARE pathway and protects PC12 cells against H2O2-induced oxidative stress.

Eriodictyol-7-O-glucoside, a novel Nrf2 activator, confers protection against cisplatin-induced toxicity

Eriodictyol-7-O-glucoside, a flavonoid isolated from Dracocephalum rupestre, is among the most potent free radical scavenger. In the present study, we identified eriodictyol-7-O-glucoside as a novel nuclear factor E2-related factor 2 (Nrf2) activator using a high-throughput cellular screening method. This compound activated Nrf2 signaling pathway and was able to stabilize Nrf2 by delaying Nrf2 degradation, resulting in accumulation of Nrf2 protein and activation of the Nrf2-dependent protective response. Recent studies have suggested that activation of Nrf2 pathway would confer protection against cisplatin-induced toxicity. The protective role of eriodictyol-7-O-glucoside in cisplatin-induced toxicity was investigated in a human renal mesangial cell line, HRMC. Cotreatment of HRMC cells with eriodictyol-7-O-glucoside significantly improved cell survival under cisplatin exposure. These findings demonstrated the feasibility of using natural compounds targeting Nrf2 as a therapeutic approach to subvert the side effects of cisplatin in normal cells.

Protective effect of naringenin-7-O-glucoside against oxidative stress induced by doxorubicin in H9c2 cardiomyocytes

Doxorubicin (DOX) is one of the most effective chemotherapeutic agents, but cardiotoxicity limits its clinical use. Although the mechanisms are not entirely understood, reactive oxygen species (ROS) and cardiomyocyte apoptosis appear to be involved in DOX cardiotoxicity. Protection or alleviation of DOX cardiotoxicity can be achieved by administration of natural phenolic compounds via activating endogenous defense systems and antiapoptosis. Naringenin-7-O-glucoside (NARG), isolated from Dracocephalum rupestre Hance, could protect from cardiomyocyte apoptosis and induce endogenous antioxidant enzymes against DOX toxicity, but the effects on intracellular ROS generation and cell membrane stability were not demonstrated. In the present study, we investigated the effects of NARG on H9c2 cell morphology, viability, lactate dehydrogenase (LDH) and creatine kinase (CK) leakage, glutathine peroxidase (GSH-Px) activity, intracellular Ca2+ concentration, and ROS generation. Compared with DOX alone treatment group, the morphological injury of the cells in groups treated by DOX plus NARG was alleviated, cell viability was increased, the amount of released LDH and CK was significantly decreased, the activity of GSH-Px was increased, the content of intracellular Ca2+ and ROS generation was lowered remarkably. These results suggest that NARG could prevent cardiomyocytes from DOX-induced toxicity by their property of stabilizing the cell membrane and reducing ROS generation.

(1S*,2R*,4aS*,6aS*,6bR*,10S*,12aR*,14aS*)-10-Hydroxy-1,2,6a,6b,9,9,12a-heptamethylperhydropicene-4a,14a-carbolactone

The title compound, C30H48O3, was extracted from the plant Dracocephalum rupestre Hance. The mol­ecule contains five fused cyclo­hexane rings and one five-membered lactone ring. Inter­molecular O—H⋯O hydrogen bonds between the hydroxyl and carbonyl groups link the mol­ecules into chains along [010]. The absolute structure has not been determined.

Simultaneous determination of nine major active compounds in Dracocephalum rupestre by HPLC

A new method was developed for the simultaneous determination of nine major constituents in Dracocephalum rupestre, including 5,7-dihydroxychromone ( 1), eriodictyol-7- O-β- d-glucoside ( 2), luteolin-7- O-β- d-glucoside ( 3), naringenin-7- O-β- d-glucoside ( 4), apigenin-7- O-β- d-glucoside ( 5), eriodictyol ( 6), luteolin ( 7), naringenin ( 8) and apigenin ( 9). The quantitative determination was conducted by reversed phase high-performance liquid chromatography with photodiode array detector (LC–PDA). Separation was performed on an Agilent Eclipse XDB-C 18 column (150 mm × 4.6 mm i.d., 5 μm) with gradient elution of acetonitrile and 0.5% aqueous acetic acid. The components were identified by retention time, ultraviolet (UV) spectra and quantified by LC–PDA at 260 nm. All calibration curves showed good linearity ( r 2 > 0.999) within test ranges. The reproducibility was evaluated by intra- and inter-day assays and R.S.D. values were less than 3.0%. The recoveries were between 95.15 and 104.45%. The limits of detection (LOD) ranged from 0.002 to 0.422 μg/ml and limits of quantification (LOQ) ranged from 0.005 to 1.208 μg/ml, respectively. The identity of the peaks was further confirmed by high-performance liquid chromatography with triple-quadrupole mass spectrometry system coupled with electrospray ionization (ESI) interface. The developed method was applied to the determination of nine constituents in 14 samples of D. rupestre collected at various harvesting times. Most compounds accumulated at much higher amounts in about June–July. The satisfactory results indicated that the developed method was readily utilized as a quality control method for D. rupestre.

Naringenin-7- O-glucoside protects against doxorubicin-induced toxicity in H9c2 cardiomyocytes by induction of endogenous antioxidant enzymes

Doxorubicin, a widely used chemotherapeutic agent, can give rise to severe cardiotoxicity that limits its clinical use by generation of reactive oxygen species (ROS) and apoptosis. Protection or alleviation of doxorubicin cardiotoxicity can be achieved by administration of natural phenolic compounds via activating endogenous defense systems and antiapoptosis. Naringenin-7- O-glucoside (NARG), isolated from Dracocephalum rupestre Hance, has been demonstrated to protect against cardiomyocyte apoptosis. In the present study, we investigated the effects of NARG on endogenous antioxidant enzymes against doxorubicin toxicity and the potential role of extracellular signal-regulated kinase (ERK) in regulation of NARG-induced Nrf2-dependent gene expression in H9c2 cardiomyocytes. The mRNA expression of glutamate-cysteine ligase modifier subunit (GCLM) and glutamate-cysteine ligase catalytic subunit (GCLC) was upregulated by NARG as detected by RT-PCR. NARG (10, 20, and 40 μM) pretreatment increased NAD (P) H: quinone oxidoreductase (NQO1), ERK, and Nrf2 protein levels in cardiomyocytes as detected by Western blotting. These results suggest that NARG could prevent cardiomyocytes from doxorubicin-induced toxicity by induction of endogenous antioxidant enzymes via phosphorylation of ERK1/2 and nuclear translocation of Nrf2.

Stereochemistry of flavonoidal alkaloids from Dracocephalum rupestre

Phytochemical studies on the aerial parts of Dracocephalum rupestre led to the isolation of four groups of flavonoidal alkaloids, dracocephins A–D. They were elucidated as conjugates of flavanone with pyrrolidin-2-one on the basis of extensive spectroscopic analysis. The two stereogenic centers rendered each group of the dracocephins as two pairs of enantiomers simultaneously. All of the sixteen isomers were separated successfully by chiral HPLC and their stereochemical features were determined by their CD data and single-crystal X-ray diffraction analysis of one stereoisomer. The additive relation of the chiroptical contributions resulting from the two stereogenic centers was generalized. The CD contribution of the chiral carbon in the pyrrolidin-2-one ring was proposed by subtraction of their respective contributions.

Protective effects of naringenin-7- O-glucoside on doxorubicin-induced apoptosis in H9C2 cells

Doxorubicin, a widely used chemotherapeutic agent, can give rise to severe cardiotoxicity by inducing cardiomyocyte apoptosis. Dracocephalum rupestre Hance, a Chinese traditional herb, has therapeutic potential for cardiovascular diseases. Naringenin-7- O-glucoside is the main active constituent of D. rupestre and there is increasing interest in its therapeutic applications. The aim of this study was to evaluate the effects of naringenin-7- O-glucoside on cardiomyocyte apoptosis induced by doxorubicin. Cell viability was detected by MTT assay. Naringenin-7- O-glucoside (10, 20, and 40 μM) significantly enhanced cardiomyocyte proliferation relative to that of doxorubicin. Furthermore, naringenin-7- O-glucoside increased the protein levels of heme oxygenase-1 (HO-1) and Bcl-2 in cardiomyocytes (as detected by Western blotting) and suppressed the mRNA expression of caspase-3 and caspase-9 (as detected by RT-PCR). These results suggest that naringenin-7- O-glucoside has protective effects against doxorubicin-induced apoptosis, effects which could underlie the use of naringenin-7- O-glucoside therapeutic agent for treating or preventing cardiomyopathy associated with doxorubicin.

Separation and structure determination of two diastereomeric pairs of enantiomers from Dracocephalum rupestre by high-performance liquid chromatography with circular dichroism detection

All of the four stereoisomers of an unprecedented type of flavanones, the dracorupesins, were separated from the aerial parts of Dracocephalum rupestre simultaneously. The dracorupesins were characterized as two diastereomeric pairs of enantiomers by on-line chiral high-performance liquid chromatography-circular dichroism (HPLC-CD) analysis, which was a reliable stereoanalytical tool for natural products. The planar structures of the compounds were elucidated by means of spectroscopic methods including IR, MS, one-dimensional NMR (1D-NMR) and two-dimensional NMR (2D-NMR) techniques.