Comparative analysis of root anatomical structure, chemical components and differentially expressed genes between early bolting and unbolting in Peucedanum praeruptorum Dunn.

Early bolting of Peucedanum praeruptorum Dunn severely affects its quality. In this study, we compared with the root structure of P. praeruptorum and its four coumarins content between early bolting (CT) and unbolting (WT) at different growth stages. We found that the proportion of area outside the root cambium (Rs) was higher in the WT plants than in the CT plants and correlated positively with the proximity to the root tip. Furthermore, the content of all four coumarins was also higher in the WT plants relative to the CT plants. In addition, we identified 15,524 differentially expressed genes (DEGs) between the two plant varieties. 11 DEGs are involved in the photoperiod and gibberellin pathways that regulate early bolting and 24 genes involved in coumarins biosynthesis were also identified. Nevertheless, early bolting of P. praeruptorum does affect its quality formation, and further studies are needed to confirm its mechanism.

The Root Extract of Peucedanum praeruptorum Dunn Exerts Anticancer Effects in Human Non-Small-Cell Lung Cancer Cells with Different EGFR Mutation Statuses by Suppressing MET Activity.

The aim of this study was to investigate the anticancer effects of the root extract of Peucedanum praeruptorum Dunn (EPP) in human non-small-cell lung cancer (NSCLC) cells and explore the mechanisms of action. We used four types of human lung cancer cell lines, including H1299 (epidermal growth factor receptor (EGFR) wild-type), PC9 (EGFR Glu746-Ala750 deletion mutation in exon 19; EGFR tyrosine kinase inhibitor (TKI)-sensitive), H1975 (EGFR L858R/T790M double-mutant; EGFR TKI-resistant), and PC9/ER (erlotinib-resistant) cells. EPP suppressed cell growth and the colony formation of NSCLC cells in a concentration-dependent manner. EPP stimulated chromatin condensation, increased the percentage of sub-G1 phase cells, and enhanced the proportion of annexin V-positive cells, demonstrating that EPP triggered apoptosis in NSCLC cells regardless of the EGFR mutation and EGFR TKI resistance status. The phosphorylation level of the signal transducer and activator of transcription 3 (STAT3) and AKT was decreased by EPP. The expression of STAT3 target genes was also downregulated by EPP. EPP reversed hepatocyte growth factor (HGF)-induced MET phosphorylation and gefitinib resistance. Taken together, our results demonstrate that EPP exerted anticancer effects not only in EGFR TKI-sensitive NSCLC cells, but also in EGFR TKI-resistant NSCLC cells, by suppressing MET activity.

Construction of graphene quantum dots-decorated EGFR cell membrane chromatography for screening active components from Peucedanum praeruptorum Dunn.

A novel stability-enhanced graphene quantum dot (GQD)-decorated epidermal growth factor receptor (EGFR) cell membrane chromatography was constructed to study the potential application of GQDs in bioaffinity chromatography, and to screen active components acting on EGFR from traditional Chinese medicine (TCM). The carboxyl groups on the surface of GQDs reacted with the amino groups of the amino-silica gel (SiO2-NH2) to form a covalent bond, thereby preparing the GQD-decorated silica gel (SiO2-GQDs). The EGFR cell membrane was further immobilized on the SiO2-GQDs through the same covalent binding method to obtain the GQD-decorated cell membrane stationary phase (SiO2-GQDs-CMSP). In this way, the cell membrane was firmly immobilized on the decorated silica carrier. The life span and stability of the GQD-decorated cell membrane chromatographic (SiO2-GQDs-CMC) column were both enhanced, and the optimal immobilization conditions of the EGFR cell membrane were also determined. This model was then verified by establishing a SiO2-GQDs-CMC online liquid chromatography-ion trap-time-of-flight (LC-IT-TOF) system to screen possible active components in Peucedanum praeruptorum Dunn. As a result, praeruptorin B (Pra-B) was screened out, and its inhibitory effect against EGFR cell growth was evaluated by the cell counting kit-8 (CCK-8) assay. Molecular docking assay was also conducted to further estimate the interaction between Pra-B and EGFR. Overall, this research indicated that GQDs may be a promising nanomaterial to be used in prolonging the life span of the CMC column, and Pra-B could be a potential EGFR inhibitor so as to treat cancer.

Tissue-Specific Metabolite Profiling on the Different Parts of Bolting and Unbolting Peucedanum praeruptorum Dunn (Qianhu) by Laser Microdissection Combined with UPLC-Q/TOF⁻MS and HPLC⁻DAD.

BACKGROUND: Qianhu is a traditional Chinese medicine. It is thought that Qianhu roots will harden after bolting and not be suitable for medicinal purposes. Bolting Qianhu and unbolting Qianhu are referred to as "Xiong Qianhu" and "Ci Qianhu," respectively. In this study, the properties, microscopic and chemical characteristics of Ci Qianhu and Xiong Qianhu roots were compared using fluorescence microscopy, laser microdissection coupled with ultra-high-performance liquid chromatography-quadrupole/time-of-flight mass spectrometry, and high-performance liquid chromatography with diode-array detection. RESULTS: Microscopy results showed that the area of secondary xylem in the root increased after bolting, with the cork and secretory canals showing strong fluorescence intensity. A total of 34 peaks, mostly pyranocoumarins, were identified in the tissues of Ci Qianhu and Xiong Qianhu. The secretory canals contained the highest variability of coumarins, whereas the secondary xylem contained the least coumarins. Moreover, seven coumarins, especially the pyran- coumarin, decreased after bolting. Generally, both before and after bolting, coumarin level was the highest in the bark, followed by the middle part, and the lowest in the inner part. CONCLUSION: Thus, it was indicated that the area of secondary xylem increased after bolting, however the coumarin variant and content decreased in the secondary xylem of Qianhu. The result shows that the quality of Qianhu decreases after bolting, which supports the viewpoint that Xiong Qianhu is not suitable for medicinal use.

Streptomyces castaneus sp. nov., a novel actinomycete isolated from the rhizosphere of Peucedanum praeruptorum Dunn.

During an investigation of microbial diversity in medicinal herbs, a novel actinomycete, strain NEAU-QHHV11T was isolated from the rhizosphere of Peucedanum praeruptorum Dunn collected from Xianglu Mountain in Heilongjiang Province, northeast China and characterized using a polyphasic approach. The organism was found to have typical characteristics of the genus Streptomyces. Phylogenetic analysis based on 16S rRNA gene sequence also indicated that strain NEAU-QHHV11T belongs to the genus Streptomyces and was most closely related to Streptomyces graminilatus NBRC 108882T (98.7 % sequence similarity) and Streptomyces turgidiscabies NBRC 16080T (98.7 % sequence similarity). The results of DNA-DNA hybridization and some phenotypic characteristics indicated that strain NEAU-QHHV11T could be distinguished from its close phylogenetic relatives. Thus, strain NEAU-QHHV11T represents a novel species of the genus Streptomyces, for which the name Streptomyces castaneus sp. nov. is proposed. The type strain is NEAU-QHHV11T (=CGMCC 4.7235T = DSM 100520T).

Comparative pharmacokinetic study of pyranocoumarins and khellactone in normal and acute lung injury rats after oral administration of Peucedanum praeruptorum Dunn extracts using a rapid and sensitive liquid chromatography-tandem mass spectrometry method.

Pyranocoumarins are the main constitutes in Peucedanum praeruptorum Dunn and possess various biological activities. In this article, we developed and validated a rapid and sensitive liquid chromatography-tandem mass spectrometry method for the targeted quantification of the pyranocoumarins, praeruptorin A, praeruptorin B and praeruptorin E, and khellactone, which is a common metabolite of these pyranocoumarins in rat plasma samples. We then performed a comparative pharmacokinetic study of these pyranocoumarins and khellactone in normal and lipopolysaccharide-induced acute lung injury (ALI) in rats following oral administration of P. praeruptorum Dunn extracts. Calibration curves gave desirable linearity (r > 0.99) and the lower limit of quantifications were sufficient for quantitative analysis. The precision and accuracy were assessed by intra-batch and inter-batch assays, and the relative standard deviations were all within 10.23% and the accuracy (relative error) was between -5.52% and 8.68%. The extraction recoveries, matrix effects and stability were also acceptable. The pharmacokinetic study revealed that the area under the concentration-time curve (0-t) of khellactone in ALI rats was significantly decreased compared with the normal rats. Meanwhile, the systemic exposures of these pyranocoumarins were slightly higher in the ALI rats than those in normal rats were. The pharmacokinetic study in the pathological state might provide information that was more comprehensive to guide the clinical usage of P. praeruptorum Dunn.

A chromosome-scale genome of Peucedanum praeruptorum provide insights into Apioideae evolution and medicinal ingredient biosynthesis.

Peucedanum praeruptorum Dunn, a traditional Chinese medicine rich in coumarin, belongs to the Apiaceae family. A high-quality assembled genome of P. praeruptorum is lacking, which has posed obstacles to functional identification and molecular evolution studies of genes associated with coumarin production. Here, a chromosome-scale reference genome of P. praeruptorum, an important medicinal and aromatic plant, was first sequenced and assembled using Oxford Nanopore Technologies and Hi-C sequencing. The final assembled genome size was 1.83 Gb, with a contig N50 of 11.12 Mb. The entire BUSCO evaluation and second-generation read comparability rates were 96.0 % and 99.31 %, respectively. Furthermore, 99.91 % of the genome was anchored to 11 pseudochromosomes. The comparative genomic study revealed the presence of 18,593 orthogroups, which included 476 species-specific orthogroups and 1211 expanded gene families. Two whole-genome duplication (WGD) events and one whole-genome triplication (WGT) event occurred in P. praeruptorum. In addition to the γ-WGT shared by core eudicots or most eudicots, the first WGD was shared by Apiales, while the most recent WGD was unique to Apiaceae. Our study demonstrated that WGD events that occurred in Apioideae highlighted the important role of tandem duplication in the biosynthesis of coumarins and terpenes in P. praeruptorum. Additionally, the expansion of the cytochrome P450 monooxygenase, O-methyltransferase, ATP-binding cassette (ABC) transporter, and terpene synthase families may be associated with the abundance of coumarins and terpenoids. Moreover, we identified >170 UDP-glucosyltransferase members that may be involved in the glycosylation post-modification of coumarins. Significant gene expansion was observed in the ABCG, ABCB, and ABCC subgroups of the ABC transporter family, potentially facilitating the transmembrane transport of coumarins after bolting. The P. praeruptorum genome provides valuable insights into the machinery of coumarin biosynthesis and enhances our understanding of Apiaceae evolution.

Peucedanum praeruptorum Dunn leaf aqueous extract protects against alcoholic gastric injury by inhibiting inflammation and oxidative stress in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Peucedanum praeruptorum Dunn (PPD) was used to treat gastrointestinal disease in China before the Tang Dynasty, and it was considered a "Top-grade" herb in Shennong Bencaojing, known for its ability to relieve the stomach Qi and indigestion. AIM OF THE STUDY: Alcohol consumption can induce severe gastric mucosal injury that lacks effective and safe interventions. We aimed to investigate the gastroprotective effects of Peucedanum praeruptorum Dunn leaf (PPL) after bolting in alcohol-induced gastric damage in mice. MATERIALS AND METHODS: Mice were orally administered PPL aqueous extract at doses of 2.5, 5, and 10 g/kg for 5 consecutive days prior to the induction of gastric damage model with ethanol. Gastric tissue was stained by hematoxylin and eosin (H&E), and the levels of pro-inflammatory cytokines and oxidative stress indicators were determined using ELISA and RT-qPCR. RNA-seq was used to detect differentially expressed genes (DEGs) in the gastric tissue, while Western blotting was employed to measure the expressions of IL-17, TNF-a, and AKT pathways. RESULTS: Treatment with PPL alleviated alcohol-induced gastric damage in mice, whereas dried root (PPD) and stem (PPS) of Peucedanum praeruptorum Dunn had no gastroprotective function. The content of peucedanocoumarin I was higher in the dried PPL compared to PPD and PPS, with an increase in peucedanocoumarin I content in PPL after boiling. Additionally, PPL administration (5, 10 g/kg) decreased pro-inflammatory factors, such as interleukin-6 (IL-6), IL-8, IL-4, IL-1ß, IL-18, and tumor necrosis factor (TNF-a) in alcohol-induced gastric injury mice (p < 0.05), and improved oxidative stress markers, including superoxide dismutase enzymes (SOD), catalase (CAT), and malondialdehyde (MDA) (p < 0.05). RNA-seq data revealed that PPL treatment inhibited alcohol-induced inflammation-related signals, including IL-17 and TNF pathways, and restored alcohol-inhibited gastric digestive and metabolic functions, such as xenobiotics metabolism of cytochrome P450, and protein digestion and absorption pathways. Notably, treatment with PPL downregulated the expressions of IL-17 A, TNF-a, monocyte chemoattractant protein-1 (MCP-1), and AKT-phosphorylation induced by ethanol exposure (p < 0.05). Thus, the aqueous extract of PPL provided protection against alcohol-induced gastric injury by mitigating inflammation and oxidative stress in mice, suggesting a potential novel therapeutic approach for alcohol-induced gastric damage.

Protective effect of Peucedanum praeruptorum Dunn extract on oxidative damage of LLC­PK1 cells induced by H2O2.

Peucedanum praeruptorum Dunn extract (PPDE) is a well-known treatment used in traditional Chinese medicines, where it is most commonly used to treat coughs and symptoms such as headaches and fever. In the present study, the antioxidant capacity of PPDE in vitro was determined by scavenging experiments using DPPH, ABTS+·, ·OH, and ·O2-. The cell survival rate was determined by MTT assay. The MDA, SOD, CAT, GSH, and GSH-Px content were determined by colorimetry assays. The expression levels of antioxidant genes SOD, CAT, GSH, and GSH-Px were assessed by reverse transcription-quantitative PCR. HPLC was used to identify the PPDE components. The results suggested that PPDE had scavenging effects on DPPH, ABTS, hydroxyl, and superoxide anion radicals in a concentration-dependent manner; H2O2 treatment resulted in oxidative stress in LLC-PK1 cells, and the degree of injury of LLC-PK1 cells following PPDE treatment was improved, which was positively correlated with its concentration. Peucedanum praeruptorum Dunn extract treatment reduced the content of MDA and increased the content of CAT, SOD1, GSH, and GSH-Px. The mRNA expression levels of antioxidant genes detected by quantitative PCR were consistent with changes in CAT, SOD, GSS, and GSH-Px. Additionally, the trend in CAT, SOD1, GSH, and GSS protein expression levels was also consistent at the mRNA level. PPDE was found to consist of isochlorogenic acid C, myricetin, baicalin, luteolin, and kaempferol. Therefore, PPDE, which was formed of products derived from natural substances, functioned in the inhibition of oxidative damage. The present study aimed to obtain a better understanding of the traditional Chinese medicine Peucedanum praeruptorum Dunn and preliminarily elucidate its antioxidant mechanism at the cellular level. Further animal or human experiments are required to verify the antioxidant effects of PPDE for further development and utilization.

Effects of plant growth-promoting rhizobacteria on growth indicators and physiological characteristics of Peucedanum praeruptorum Dunn leaves.

As a kind of medicinal plant, Peucedanum praeruptorum Dunn has been over-harvested in the wild population, which leads to its artificial cultivation. The present study aims to analyze the effects of different plant growth-promoting rhizobacteria (PGPR) on the growth and physiological characteristics of P. Praeruptorum leaves. Compared with the CK, the content of malondialdehyde (MDA) was drastically reduced in the leaves of P. Praeruptorum in different treatment groups (P < 0.05), and with S6 showing the most significant reduction in MDA content (content was only about 1/3 that of the CK). The indicators of leaf area, length and width were found to be the highest in group S9, reaching a level that is 3.75, 3.08 and 1.48 times higher than those in group CK, respectively. Group S8 has the largest plant height, which is 1.22 times higher than that in group CK. S2 has the largest stem diameter, which is 1.69 times higher than that in group CK. Group S1 has the largest petiole length, which is 1.74 times higher than that in group CK. Group S6 has the largest chlorophyll content, which is 1.63 times higher than that in group CK. Group S2 has the highest content of soluble sugar and soluble protein, which are 2.02 times and 3.82 times higher than those in group CK. Group S9 exhibits the strongest CAT activity, which is 3.71 times higher than that in group CK. S5 exhibits the strongest SOD activity, which is 2.32 times higher than group CK. Group S1 exhibits the strongest POD activity, which is 5.94 times higher than that in group CK. In conclusion, the inoculation with PGPR is effective in improving the growth of P. Praeruptorum leaves and their physiological indicators, which provides guidance on the application of PGPR to achieve the high quality and yield of P. Praeruptorum.

Peucedanum praeruptorum Dunn polysaccharides regulate macrophage inflammatory response through TLR2/TLR4-mediated MAPK and NF-κB pathways.

The present study was to investigate the molecular mechanisms underlying macrophage inflammatory response to polysaccharides from Peucedanum praeruptorum Dunn (PPDs) and elucidate the receptors and signaling pathways associated with PPDs-mediated macrophage activation. MTT and Griess method were performed to investigate the effects of PPDs on cell viability and NO production. Neutral red and FITC-dextran were used to determine the pinocytic and phagocytic activity. RT-qPCR and ELISA were employed to analyze the mRNA expression of inflammatory factors and production of cytokines and chemokines. RNA-seq and bioinformatics analysis were conducted to determine the underlying molecules, regulators and pathways, which were further validated by pathway inhibition and neutralization assays. The results indicated that PPDs significantly enhanced pinocytic and phagocytic activity, promoted the expression and secretion of inflammatory factors and chemokines, and boosted the expression of accessory and costimulatory molecules. RNA-Seq analysis identified 1343 DEGs, 405 GO terms and 91 KEGG pathways. IL6 and TNF were identified as hubs of connectivity in PPDs-mediated macrophage activation. "Cytokine-cytokine receptor interaction", "TNF signaling pathway", "NF-kappa B signaling pathway", "JAK-STAT signaling pathway" and "MAPK signaling pathway" were the most significant pathways. The pathway inhibition assay revealed that MAPK and NF-κB pathways were essential to macrophage activation by PPDs. TLR2 and TLR4 were uncovered to be the functional receptors and involved in recognition of PPDs. These results indicated that PPDs modulated macrophage inflammatory response mainly through TLR2/TLR4-dependent MAPK and NF-κB pathways.

Fungal isolates influence the quality of Peucedanum praeruptorum Dunn.

The symbiotic relationship between beneficial microorganisms and plants plays a vital role in natural and agricultural ecosystems. Although Peucedanum praeruptorum Dunn is widely distributed, its development is greatly limited by early bolting. The reason for early bolting in P. praeruptorum remains poorly characterized. We focus on the plant related microorganisms, including endophytes and rhizosphere microorganisms, by combining the traditional isolation and culture method with metagenomic sequencing technology. We found that the OTUs of endophytes and rhizosphere microorganisms showed a positive correlation in the whole growth stage of P. praeruptorum. Meanwhile, the community diversity of endophytic and rhizosphere fungi showed an opposite change trend, and bacteria showed a similar change trend. Besides, the microbial communities differed during the pre- and post-bolting stages of P. praeruptorum. Beneficial bacterial taxa, such as Pseudomonas and Burkholderia, and fungal taxa, such as Didymella and Fusarium, were abundant in the roots in the pre-bolting stage. Further, a strain belonging to Didymella was obtained by traditional culture and was found to contain praeruptorin A, praeruptorin B, praeruptorin E. In addition, we showed that the fungus could affect its effective components when it was inoculated into P. praeruptorum. This work provided a research reference for the similar biological characteristics of perennial one-time flowering plants, such as Saposhnikovia divaricate, Angelica sinensis and Angelica dahurica.

Comparative analysis and chemical profiling of different forms of Peucedani Radix.

Peucedani Radix, derived from roots of Peucedanum praeruptorum Dunn, is a well-known herb used for centuries in traditional Chinese medicine, which is rich in various coumarins. Four different forms including "earthworm head", "bamboo-like", taproots and multi-branched roots have occurred in current producing areas, but the differences in their external features and chemistry have not been concerned till now. In this study, the morphological and microscopic characters of "earthworm head" and "bamboo-like" roots were compared in detail, and qualitative and quantitative characterization of main active coumarins in different forms of Peucedani Radix have been developed by UPCL-Q/TOF-MS and HPLC-DAD, respectively. The results showed that both "earthworm head" and "bamboo-like" consisted of rhizome and root, exhibiting distinct features from normal taproots. Moreover, 53 coumarins including simple coumarins, furanocoumarins and pyranocoumarins were identified or putatively characterized from the four forms samples under the established UPLC-Q/TOF-MS conditions. In addition, the developed quantitative method was successfully applied to simultaneously determine eight main coumarins in 24 batches of four forms Peucedani Radix and 12 batches of dissected "earthworm head" and "bamboo-like" samples. The quantitative results proved that wild "earthworm head" showed higher content of active coumarins and the "bamboo-like" was a rich source of coumarins in cultivated samples, especially for furanocoumarins. These findings would provide reasonable basis for further quality evaluation, grades classification and comprehensive utilization of P. praeruptorum resources.

The complete plastome of Peucedanum praeruptorum (Apiaceae).

Peucedanum praeruptorum is an important traditional herbal medicine unique to China. The complete chloroplast genome of P. praeruptorum was generated here using high-throughput sequencing. The plastome was 147,197 bp in size, which consisted of a pair of inverted repeats (IRs; 18,713 bp), a large single copy (LSC; 92,161 bp) and a small single copy (SSC; 17,610 bp). The GC content of the plastome was 37.6%, with 44.5%, 36.0%, and 31.1% in IRs, LSC, and SSC, respectively. A total of 128 genes were annotated, including 84 protein-coding genes, 35 tRNAs, eight rRNAs, and one pseudogene (Ψycf1). The phylogenomic analysis indicated that P. praeruptorum formed a monophyletic clade with Peucedanum japonicum.

[Factors influencing the quality of Peucedanum Praeruptorum Dunn and "assessment of quality based on its features"].

The factors influencing the evaluation of the quality of Peucedanum praeruptorum Dunn, called "Qianhu" in Chinese, include the botanical origin, places of production, harvesting time and its nature of "Ci Xiong" (bolting and unbolting) etc. The orthodox products are derived from Peucedanum praeruptorum Dunn in successive dynasties, especially the unbolting one produced in Anhui and Zhejiang Provinces picked up during the Beginning of Winter. The "assessment of quality based on its features" includes the "Earthworm head" , "black skin of the root" , "gold inlaid with white jade" , "soft texture like sweet rice" and "strong fragrant smell" . Therefore, the "assessment of quality based on its features" is the summary of all its properties, including the morphology, color, flavor, and property, and it's also the background for evaluating its quality and embodying the wisdom of distinguishing experiences of ancient herbologists.

Reduced allergic lung inflammation by root extracts from two species of Peucedanum through inhibition of Th2 cell activation.

ETHNOPHARMACOLOGICAL EVIDENCE: Peucedani Radix (PR), the root of Peucedanum praeruptorum Dunn (PPD) or Peucedanum decursivum (Miq.) Maxim. (PDM), has long been used in Korea to eliminate sputum, relieve cough, and reduce bronchus contraction. Furthermore, these therapeutic strategies are recognized as general and effective methods in western medicine as well as traditional Korean medicine. AIM OF THE STUDY: To determine and compare the anti-inflammatory effects of PPD extracts (PPDE) and PDM extracts (PDME) on allergic lung inflammation, using in vivo OVA-induced airway inflammation in mice and in vitro primary cell culture systems. MATERIALS AND METHODS: Eight-week-old female C57BL/6 mice were placed into four groups (n=4 per group): saline control, OVA-induced allergic lung inflammation with vehicle, or PPDE (200mg/kg) or PDME (200mg/kg) treatment. PR extracts (PRE) were administered from 1 week before 1st OVA sensitization to the day before sacrifice. Mice were sacrificed 18h after last OVA intra-nasal challenge followed by histological and biochemical analyses. RESULTS: Inflammatory phenotypes were alleviated with oral administration of PRE. PRE treatment decreased mucus production in airway epithelium, inflammatory cell number, eosinophilia, type 2 cytokines, and histamine in bronchoalveolar lavage fluid (BALF). Mice with PRE administration showed diminished activated CD4 T cell (CD4+CD25+ cell) and GATA-3 level in the lung. In addition, PRE treatment reduced Th2 cell activation in vitro, using Th2 polarization system. CONCLUSION: Our findings indicate that the anti-inflammatory effects of PRE arise from reduced Th2 cell activation and validate the clinical use of PR in traditional Korean medicine.

Cell membrane chromatography coupled with UHPLC-ESI-MS/MS method to screen target components from Peucedanum praeruptorum Dunn acting on α1A adrenergic receptor.

Peucedanum praeruptorum Dunn (BaiHuaQianHu in Chinese) is a traditional Chinese medicine that has a long history of use in China. In this study, HEK 293 α1A adrenergic cell membrane chromatography was coupled with UHPLC-ESI-MS/MS and successfully used to identify active components from Peucedanum praeruptorum Dunn. Paeruptorin A, paeruptorin B, and paeruptorin C were identified with α1A adrenergic receptor activity. Pharmacological assays showed that tamsulosin hydrochloride, paeruptorin A, paeruptorin B, and paeruptorin C in concentrations of 1×10(-8) to 1×10(-4)mol/mL could relax prostate strips pre-contracted with adrenalin in a concentration dependent manner. Therefore, the HEK293 α1A cell membrane chromatography coupled UHPLC-ESI-MS/MS system may be a potentially useful drug discovery method for screening for medicinal herbal components with α1A adrenergic receptor inhibitory activity.