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Pinellia tuber, the dried tuber of Pinellia ternata , causes a very strong acridity sensation in the oral and laryngopharynx mucosa when taken orally in its unprocessed form. In traditional Chinese medicine (TCM), this sensation has been called \"toxicity\", and Pinellia tuber must be processed using ginger extract, licorice, or alum. In Japanese traditional Kampo medicine, since “toxicity” can be eliminated by decocting, it should not be processed. However, little is known about the mechanism underlying the \"detoxification\" of Pinellia tubers. In this study, we produced murine antiserum using recombinant P. ternata lectin (PTL), developed an immuno-fluorescence staining method for PTL in the needle-shaped crystals (raphides) that were prepared by petroleum ether extraction (PEX) from Pinellia tuber, and elucidated the mechanism of the processing of Pinellia tuber using heat or ginger extract. After heating the raphides in water, the amount of PTL contained in the raphides was significantly reduced by the immunostaining, although the shape of the raphides was not changed. Incubating raphides with dried ginger extract also significantly reduced the amount of PTL in the raphides in a concentration-dependent manner. By the activity-guided fractionation of ginger extract, the active ingredients in the ginger extract were oxalic acid, tartaric acid, malic acid, and citric acid. Among these four organic acids, oxalic acid mainly contributed to the effect of dried ginger extract by its content in ginger extract and its activity. These results exhibit scientific evidences for the traditional theories of processing to \"detoxify\" Pinellia tuber in TCM and Kampo medicine. Graphical abstract

Pinelliae Rhizoma (PR), a highly esteemed traditional Chinese medicinal herb, is widely applied in clinical settings due to its diverse pharmacological effects, including antitussive, expectorant, antiemetic, sedative-hypnotic, and antitumor activities. Pinellia ternata exhibits morphological variation in its leaves, with types resembling peach, bamboo, and willow leaves. However, the chemical composition differences among the corresponding rhizomes of these leaf phenotypes remain unelucidated. This pioneering research employed Matrix-Assisted Laser Desorption/Ionization Mass Spectrometry Imaging (MALDI-MSI) to conduct the in situ identification and spatial profiling of 35 PR metabolites in PR, comprising 12 alkaloids, 4 organic acids, 12 amino acids, 5 flavonoids, 1 sterol, and 1 anthraquinone. Our findings revealed distinct spatial distribution patterns of secondary metabolites within the rhizome tissues of varying leaf types. Orthogonal Partial Least Squares Discriminant Analysis (OPLS-DA) effectively differentiated between rhizomes associated with different leaf morphologies. Furthermore, this study identified five potential differential biomarkers—methylophiopogonanone B, inosine, cytidine, adenine, and leucine/isoleucine—that elucidate the biochemical distinctions among leaf types. The precise tissue-specific localization of these secondary metabolites offers compelling insights into the specialized accumulation of bioactive compounds in medicinal plants, thereby enhancing our comprehension of PR’s therapeutic potential.

The present study investigates the chemical composition variances among Pinelliae Rhizoma, a widely used Chinese herbal medicine, and its common adulterants including Typhonium flagelliforme, Arisaema erubescens, and Pinellia pedatisecta. Utilizing the non-targeted metabolomics technique of employing UHPLC-Q-Orbitrap HRMS, this research aims to comprehensively delineate the metabolic profiles of Pinelliae Rhizoma and its adulterants. Multivariate statistical methods including PCA and OPLS-DA are employed for the identification of differential metabolites. Volcano plot analysis is utilized to discern upregulated and downregulated compounds. KEGG pathway analysis is conducted to elucidate the differences in metabolic pathways associated with these compounds, and significant pathway enrichment analysis is performed. A total of 769 compounds are identified through metabolomics analysis, with alkaloids being predominant, followed by lipids and lipid molecules. Significant differential metabolites were screened out based on VIP > 1 and p-value < 0.05 criteria, followed by KEGG enrichment analysis of these differential metabolites. Differential metabolites between Pinelliae Rhizoma and Typhonium flagelliforme, as well as between Pinelliae Rhizoma and Pinellia pedatisecta, are significantly enriched in the biosynthesis of amino acids and protein digestion and absorption pathways. Differential metabolites between Pinelliae Rhizoma and Arisaema erubescens are mainly enriched in tyrosine metabolism and phenylalanine metabolism pathways. These findings aim to provide valuable data support and theoretical references for further research on the pharmacological substances, resource development and utilization, and quality control of Pinelliae Rhizoma.

Brassinolide (BR) is the “sixth class” plant hormone, which plays an important role in various physiological and biochemical processes of plants. The wide variety of functions of Pinellia ternata means that there is huge demand for it and thus it is in short supply. This paper mainly assessed the changes of yield and quality in P. ternata at different stages after BR treatments by principal component analysis, in order to improve the yield and quality of P. ternata and at the same time determine the best harvest time. The results showed that the tuber yield of P. ternata was significantly increased by BR treatments at different stages (except for the 15th day). After the 15th, 45th, 60th, 75th, 90th, and 105th day of treatments, the tuber yield of P. ternata reached peak values at 0.10 (0.65 g), 0.50 (1.97 g), 0.50 (1.98 g), 1.00 (2.37 g), 1.00 (2.84 g), and 2.00 mg/L (3.76 g) BR treatment, respectively. The optimal harvest time was the 75th day after 0.10, 0.50, and 1.00 mg/L BR treatments, which not only significantly improved the yield of P. ternata, but also retained high level of total alkaloids in the tubers (20.89, 5.37, and 13.44%) and bulbils (9.74, 20.42, and 13.62%), high total flavone content in the tubers (17.66, 16.26, and 12.74%) and bulbils (52.63, 12.79, and 38.69%), and high β-sitosterol content in the tubers (25.26, 16.65, and 0.62%) of P. ternata, compared with the control, respectively.

Tetramethylpyrazine (TMP), a pharmacologically active component isolated from the rhizome of the Chinese herb Rhizoma Chuanxiong (Chuanxiong), has been clinically used in China and Southeast Asian countries for the prevention and treatment of cardiovascular diseases (CVDs) for about fifty years. The pharmacological effects of TMP on the cardiovascular system have attracted great interest. Emerging experimental studies and clinical trials have demonstrated that TMP prevents atherosclerosis as well as ischemia-reperfusion injury. The cardioprotective effects of TMP are mainly related to its antioxidant, anti-inflammatory, or calcium-homeostasis effects. This review focuses on the roles and mechanisms of action of TMP in the cardiovascular system and provides a novel perspective on TMP’s clinical use.

Pinelliae Rhizoma (PR) is a commonly used Chinese medicinal herb, but it has been frequently reported about its toxicity. According to the traditional Chinese medicine theory, processing can reduce the toxicity of the herbs. Here, we aim to determine if processing reduces the toxicity of raw PR, and to explore the underlying mechanisms of raw PR-induced toxicities and the toxicity-reducing effect of processing. Biochemical and histopathological approaches were used to evaluate the toxicities of raw and processed PR. Rat serum metabolites were analyzed by LC-TOF-MS. Ingenuity pathway analysis of the metabolomics data highlighted the biological pathways and network functions involved in raw PR-induced toxicities and the toxicity-reducing effect of processing, which were verified by molecular approaches. Results showed that raw PR caused cardiotoxicity, and processing reduced the toxicity. Inhibition of mTOR signaling and activation of the TGF-β pathway contributed to raw PR-induced cardiotoxicity, and free radical scavenging might be responsible for the toxicity-reducing effect of processing. Our data shed new light on the mechanisms of raw PR-induced cardiotoxicity and the toxicity-reducing effect of processing. This study provides scientific justifications for the traditional processing theory of PR, and should help in optimizing the processing protocol and clinical combinational application of PR.

Pinelliae Rhizoma Praeparatum cum Alumine (PRPCA) is an important traditional processed herbal medicine mainly used for treating phlegm in China for more than 2000 years. In our previous studies, extraction optimization, characterization, and bioactivities of total polysaccharides from PRPCA were investigated. In this study, further purification of these polysaccharides was performed. Two polysaccharides named neutral fraction of total polysaccharides-II (TPN-II) and acidic fraction of total polysaccharides-II (TPA-II) were obtained by gradient ion-exchange chromatography followed by gel-permeation chromatography. Results of scanning electron microscopy (SEM) analysis in the present study showed that TPN-II had a tight structure with a rough and uneven surface, while TPA-II had a relative homogeneous surface and a loose structure. Further studies indicated that TPN-II was a homosaccharide mainly composed by glucose with a molecular weight of 8.0 kDa. TPA-II was mainly composed of mannose, rhamnose, glucuronic acid, galacturonic acid, glucose, galactose and arabinose in a molar ratio of 2.1, 2.3, 1.7, 10.6, 2.6, 14.2, and 2.5, with a molecular weight of 1250 kDa. The nuclear magnetic resonance (NMR) results indicated that α and β form glycoside bonds existed in TPN-II and TPA-II, and TPN-II was composed of α-glucopyranose. In addition, both purified polysaccharides have significant anti-inflammatory effects on mucus secretion of human airway epithelial NCI-H292 cells without cytotoxicity. Compared with TPN-II, TPA-II exhibited more significant anti-inflammatory effects on lipopolysaccharide (LPS)-induced airway inflammation by regulating levels of interleukin-4 (IL-4) and interferon-γ (IFN-γ) and inhibiting mucus secretion. The results suggest that polysaccharides from PRPCA could be explored as therapeutic agents in treating inflammation and over secretion of mucus in asthma.

In this study, the ultrasound-assisted extraction of polysaccharides (PSA) from Pinelliae Rhizoma Praeparatum Cum Alumine (PRPCA) was optimized by response surface methodology (RSM). The structural characteristics of PSA were analyzed by UV-vis spectroscopy, infrared spectroscopy, scanning electron microscopy, high performance gel permeation chromatography and high performance liquid chromatography, respectively. In addition, antioxidant and antimicrobial activities of PSA were studied by different in vitro assays. Results indicated that the optimal extraction conditions were as follows: the ratio of water to raw of 30 mL/g, extraction time of 46.50 min, ultrasonic temperature of 72.00 °C, and ultrasonic power of 230 W. Under these conditions, the obtained PSA yield (13.21 ± 0.37%) was closely agreed with the predicted yield by the model. The average molecular weights of the PSA were estimated to be 5.34 × 103 and 6.27 × 105 Da. Monosaccharide composition analysis indicated that PSA consisted of mannose, galactose uronic acid, glucose, galactose, arabinose with a molar ratio of 1.83:0.55:75.75:1.94:0.45. Furthermore, PSA exhibited moderate antioxidant and antibacterial activities in vitro. Collectively, this study provides a promising strategy to obtain bioactive polysaccharides from processed products of herbal medicines.

Sleep disorder (SD) has a high incidence and seriously affects quality of life, mental health and even the manifestation of physical diseases. The combination of Pinellia ternata (Chinese name: banxia) and Prunella vulgaris  (Chinese name: xiakucao), known as the Banxia–Xiakucao Chinese herb pair (BXHP), is a proven Chinese herbal medicine that has been used to treat SD for thousands of years due to its significant clinical effects. However, its active pharmacological components and sedative–hypnotic mechanisms have not been fully elucidated. Thus, the present study used a systematic pharmacological approach to develop pharmacokinetic screens and target predictions via construction of a protein–protein interaction network and annotation database for SD-related and putative BXHP-related targets. Visualization, screening and integrated discovery enrichment analyses were conducted. The BXHP chemical database contains 166 compounds between the two herbal ingredients, and of these, 22 potential active molecules were screened by pharmacokinetic evaluation. The targets of 114 of the active molecules were predicted, and 34 were selected for further analysis. Finally, gene ontology and Kyoto Encyclopedia of Genes and Genomes pathway analyses suggested that BXHP can reduce inflammatory responses. and mediate immune-related and central nervous system neurotransmitters via regulation of multiple targets and pathways. The use of a systematic pharmacology-based approach in the present study further elucidated the mechanisms of action underlying BXHP for the treatment of SD from a holistic perspective and sheds light on the systemic mechanisms of action of Chinese herbal medicines in general.

Objective: A model of Near Infrared Diffuse Reflectance Spectroscopy (NIR-DRS) was established for the first time to determine the content of Shengmaxinside I in the honey-fried processing of Rhizoma Cimicifugae. Methods: Shengmaxinside I content was determined by high-performance liquid chromatography (HPLC), and the data of the honey-fried processing of Rhizoma Cimicifugae samples from different batches of different origins by NIR-DRS were collected by TQ Analyst 8.0. Partial Least Squares (PLS) analysis was used to establish a near-infrared quantitative model. Results: The determination coefficient R2 was 0.9878. The Cross-Validation Root Mean Square Error (RMSECV) was 0.0193%, validating the model with a validation set. The Root Mean Square Error of Prediction (RMSEP) was 0.1064%. The ratio of the standard deviation for the validation samples to the standard error of prediction (RPD) was 5.5130. Conclusion: This method is convenient and efficient, and the experimentally established model has good prediction ability, and can be used for the rapid determination of Shengmaxinside I content in the honey-fried processing of Rhizoma Cimicifugae.