[Pseudo-targeted metabolomics for differential components of Rhei Radix et Rhizoma from three plant species].

Rhei Radix et Rhizoma is common traditional Chinese medicine with multiple original plants. The content and proportion of the active components in Rhei Radix et Rhizoma from different plant species were compared to accurately evaluate the medicine qua-lity and provide a theoretical basis for precise use of this medicine in clinical practice. In this study, fresh Rhei Radix et Rhizoma samples were collected from the four-year-old plants of Rheum palmatum, R. tanguticum, and R. officinale. The relative content of 220 anthraquinones, anthrones, and tannins in the samples were determined by pseudo-targeted metabolomics, and the differential components were screened by multivariate statistical methods. The principal component analysis classified the samples into three clusters according to the original plants. The orthogonal partial least squares-discriminant analysis(OPLS-DA) screened out 117 differential components, including 8 free anthraquinones, 18 anthraquinone glycosides, 80 anthrones, and 11 tannins. Twenty-eight components had the highest content in R. tanguticum, mainly including sennosides, anthraquinone glycosides, and procyanidins. Thirty-five components showed the highest content in R. officinale, mainly including free anthraquinones and catechines. Fifty-four components showed the highest content in R. palmatum, mainly including dianthrones, while the structures of most of them cannot be determined temporarily. The content distribution of differential components in the three original plants indicates that R. tanguticum has the strongest effect of purging, while R. officinale has the strongest effect of clearing heat and purging fire, and both have stronger effects of resolvong stasis and dredging meridians than R. palmatum.

[Comparative study of purgative pharmacological effects and mechanisms of Moringa oleifera leaves and Rhei Radix et Rhizoma].

Moringa oleifera leaves are known for their "Virechana"(purgative) effect in Ayurvedic medicine in India. This study compared the purgative effects and mechanisms of M. oleifera leaves with the reference Rhei Radix et Rhizoma to establish a foundation for the further application of M. oleifera leaves in traditional Chinese medicine(TCM). Using network pharmacology and molecular docking methods, this study identified the material basis, common targets, and signaling pathways through which Rhei Radix et Rhizoma and M. oleifera leaves exerted their purgative pharmacological effects. A low-fiber diet-induced constipation mouse model was established to measure fecal parameters and small intestinal propulsion rate, and histological changes in the colon were observed using HE staining. Relative expression levels of relevant genes and target proteins were assessed using RT-qPCR and immunohistochemistry, respectively. The results showed that mapping the targets of Rhei Radix et Rhizoma and M. oleifera leaves onto the biological process network of constipation revealed close proximity, indicating that they may exert their therapeutic effects on constipation through similar biological processes. Molecular docking results indicated that compounds such as sennoside C and isoquercitrin could target serine/threonine protein kinases(AKT1) and mitogen-activated protein kinase 3(MAPK3), thereby affecting MAPK and calcium signaling pathways to promote defecation. Animal experiments demonstrated that both M. oleifera leaves and Rhei Radix et Rhizoma increased the number of fecal pellets and water content in constipated mice, improved small intestine motility, colon mucosal thickness, and muscle layer thickness, upregulated the gene expression levels of AKT1 and MAPK3 in the colon, and downregulated the expression of AQP3 protein. These findings suggest that M. oleifera leaves and Rhei Radix et Rhizoma share similarities in their therapeutic efficacy and mechanisms for treating constipation. Using Rhei Radix et Rhizoma as a reference can provide a better understanding of the characteristics of the "Virechana"(purgative) effect of M. oleifera leaves in TCM.

[Material basis of Rhei Radix et Rhizoma-Coptidis Rhizoma combination in alleviating "bitter-cold" properties based on supramolecular chemistry of Chinese medicine].

The present study aimed to explore the material basis of Rhei Radix et Rhizoma-Coptidis Rhizoma combination in alleviating "bitter-cold" properties based on the supramolecular chemistry of Chinese medicine.Dynamic light scattering and scanning/transmission electron microscopy were used to characterize the morphological characteristics of supramolecules in the decoction of Rhei Radix et Rhizoma and Coptidis Rhizoma.The chemical composition of supramolecules, as well as the dissolution and release processes of supramolecules and the medicinal components of Coptidis Rhizoma decoction, was determined by the high-performance liquid chromatography-mass spectrometry.The differences in "bitter-cold" medicinal properties between Rhei Radix et Rhizoma decoction, Coptidis Rhizoma decoction, and co-decoction were analyzed by sensory evaluation, electronic tongue, mouse diarrhea model, and pathological indicators.The anthraquinones/tannins and alkaloids interacted to form supramolecules with a scale of about 400 nm when Rhei Radix et Rhizoma and Coptidis Rhizoma were decocted together, which delayed the dissolution and release of the active components represented by berberine. Compared with the consequence of single drug administration at 4 g·kg~(-1), the combination of the two drugs at 8 g·kg~(-1) significantly alleviated the "bitter-cold" properties.The effective components interacted to form supramolecules in the co-decoction of Rhei Radix et Rhizoma and Coptidis Rhizoma, which affected the dissolution and release of the effective components of Chinese medicinal decoction, thereby alleviating the "bitter-cold" properties.The findings of this study provide a new idea for revealing the scientific compatibility of Rhei Radix et Rhizoma and Coptidis Rhizoma.

[Botanical origin identification of Rhei Radix et Rhizoma based on color digitalization].

The color characteristic information of Rhei Radix et Rhizoma powder was obtained by spectrophotometer, the feasibility of rapid identification of Rhei Radix et Rhizoma origin based on chromaticity value was studied by statistical analysis. The results of rank correlation analysis showed that a~*(P<0.01), b~*(P<0.01) had significantly correlation with the origin of medicinal herbs, which could be used as two important parameters to distinguish the origin of Rhei Radix et Rhizoma, the larger the a~* value, the more red the powder color,and the greater the b~* value, the more yellow the powder color. Meanwhile, through Fisher discriminant analysis, the linear discriminant functions of different genus Rhei Radix et Rhizoma were established, which was Rheum tanguticum=40.666a~*+0.019b~*-213.303, Rh. palmatum=34.121a~*+0.061b~*-151.770, Rh. officinale=28.071a~*+0.113b~*-104.604 3, the coincidence rate of cross-validation was over 95%, among them, the discriminant rate of Rh. tanguticum and Rh. officinale reached 100%;In addition, using the percentile method to analyze the 90% reference value range of three different origin of Rhei Radix et Rhizoma, as a result, Rh. tanguticum a~*(10.236 5-10.604 7), b~*(32.294 8-34.841 7); Rh. palmatum a~*(8.602 7-8.770 0), b~*(27.534 8-28.968 6), and Rh. officinale a~*(6.825 7-7.464 3),b~*(21.001 6-27.716 4). According to this study, rank correlation analysis and Fisher discriminant analysis are feasible to distinguish the base of Rhei Radix et Rhizoma in a certain range, and provide some theoretical basis for the identification of Rhei Radix et Rhizoma. It also provides a new method and idea for the identification of other multi-base Chinese medicine.

[Research progress on processing history evolution as well as effect on chemical compositions and traditional pharmacological effects of Rhei Radix et Rhizoma].

Rhei Radix et Rhizoma(RRR) is a commonly used traditional Chinese medicine, with extensive pharmacological effects and clinical applications. This paper summarized processing history evolution of RRR and its effect on chemical compositions and pharmacological effects, and provided feasible insights for further studies on the chemical compositions and pharmacological effects of RRR before and after processing. Relevant information demonstrated that RRR has a long history of processing and various methods. At pre-sent, Chinese Pharmacopoeia mainly records four processing methods: cleaning(raw RRR), wine processing(RRR stir-fried with wine), steaming processing(RRR wine steaming), fried charcoal(RRR charring). RRR has a good effect in clearing heat effect, hemostatic effect and blood promoting effect, and its main chemical components are anthraquinone/anthrones, stilbene, phenylbutanone, chromogens, flavonoids and tannin compounds. This paper reviewed the history evolution of RRR and its effect on chemical composition and pharmacological changes, and put forward further study ideas, with the aim to provide a basic reference for processing mechanism, effective material basis and clinical application of RRR.

[Research progress of effect of Rhei Radix et Rhizoma and its anthraquinone in treatment of autoimmune diseases].

Rhei Radix et Rhizoma was first recorded in Shennong Ben Cao Jing, with a wide range of pharmacological activities. Autoimmune disease is a kind of disease that damages the tissue structure and function of immune cells and their components due to the impairment of immune tolerance function, including atherosclerosis, multiple sclerosis, gout, rheumatoid arthritis, autoimmune thyroiditis, ulcerative colitis, type 1 diabetes and IgA nephropathy. In recent years, clinical and experimental studies show that Rhei Radix et Rhizoma has potential therapeutic effects on autoimmune diseases. Under the guidance of the theory of traditional Chinese medicine, this paper reviews therapeutic and intervening effects of Rhei Radix et Rhizoma and its main active ingredient anthraquinone on autoimmune diseases. It also puts forward new study directions in view of the existing problems in studies of rhubarb and its anthraquinone, with the aim to provide reference for clinical treatment and scientific studies of effect of Rhei Radix et Rhizomaon autoimmune diseases.

[Research progress in original species identification in industry chain of Rhei Radix et Rhizoma].

Rhei Radix et Rhizoma is a kind of commonly used Chinese medicinal materials. Due to the overharvesting, the wild resource is endangering. Large market demand caused severely adulterant of commercial Rhei Radix et Rhizoma medicinal materials and decoction pieces. This manuscript reviewed the advances of the original species authentication in the industrial chain of Rhei Radix et Rhizoma during the latest decade, including characteristics and microscopic features, phytochemical analysis on anthraquinones, and molecular authentication based on DNA barcoding. Accordingly, an original species authentication route for the industrial chain of Rhei Radix et Rhizoma was summarized:(1)the identification of seeds and seedlings by DNA barcoding;(2) the selection of high variable sites based on the chloroplast genome;(3)biomonitoring of the Rhei Radix et Rhizoma medicinal materials and decoction pieces by two-dimensional DNA barcode;(4)traceability of Chinese patent medicines by third-generation sequencing. In conclusion, the combination of molecular identification and traditional identification methods provides a new idea for the identification of the original species of Rhei Radix et Rhizoma in the industrial chain and a essential guidance for the research of drug safety and efficacy of Rhei Radix et Rhizoma.

[Study on mechanism of Rhei Radix et Rhizoma-Persicae Semen in treatment of adenomyosis based on network pharmacology].

The aim of this paper was to screen the active targets of Rhei Radix et Rhizoma and Persicae Semen in the treatment of adenomyosis(AM) by means of network pharmacology, and to investigate their mechanism of action. The effective components of Rhei Radix et Rhizoma and Persicae Semen were screened out by using traditional Chinese medicine systematic pharmacological(TCMSP) database, with oral bioavilability(OB) ≥30% and drug-like(DL) ≥0.18 selected as the thresholds. A network was built between the main components and their corresponding targets. Ninety-five human genes corresponding to the medicine targets were obtained from Uniprot database; 220 genes corresponding to AM were obtained from GeneCards database. A total of 21 intersection genes were screened from disease genes and medicine genes, and the protein-protein interaction network interaction(PPI)analysis was conducted by using STRING tool. Disease-target PPI network was drawn by using Cytoscape software, and component-target-disease network was constructed. Twenty-five nodes and 74 connections were found, and then core networks and targets were screened for Kyoto encyclopedia of genes and genomes(KEGG) pathway enrichment analysis. The animal model of AM was established by feeding tamoxifen citrate mixed droplets to primary mice for verification of the mechanism. Twenty-three signaling pathways were involved in KEGG pathway enrichment. It was found that the therapeutic mechanism of Rhei Radix et Rhizoma and Persicae Semen on AM may involve multiple targets such as inflammation and immunity, proliferation and apoptosis, endocrine and oxidative stress. Among them, the P53 signaling pathway and the apoptotic signaling pathway which mediated the expression of P53 and BAX may be the important ones. Animal experiments proved that the effective components of Rhei Radix et Rhizoma and Persicae Semen can interfere with the P53 signaling pathway and the apoptotic signaling pathway at the junction of endometrial muscle layer, increase the expression of P53 and BAX in muscle layer cells, and promote the apoptosis of cells with abnormal proliferation ability.

[Study on potential hepatotoxicity of rhein in Rhei Radix et Rhizoma based on liver metabolism].

The bilirubin metabolism mediated by the phase Ⅱ metabolizing enzyme UGT1A1 in the liver was evaluated to study the potential hepatotoxicity risk based on investigation on the inhibitory effect of rhein and its metabolites on the UGT1A1 enzyme in Rhei Radix et Rhizoma. Firstly, in vitro liver microsomes incubation was used to initiate the phase Ⅱ metabolic reaction to investigate the inhibitory effect of rheinon UGT1A1 enzyme. Secondly, the phase Ⅰ and phase Ⅱ metabolic reactions were initiated to investigate the hepatotoxicity risk of rhein metabolites. It was found that the rhein and its phase Ⅱ metabolites had no significant inhibitory effect on UGT1A1 enzyme, but its phase Ⅰ metabolites significantly reduced UGT1A1 enzyme activity. Based on the metabolites analysis, it is speculated that the rhein phase Ⅰ metabolite rheinhydroxylate and its tautomers have certain hepatotoxicity risks, while the toxicity risk induced by the prototype and phase Ⅱ metabolites of rheinglucoside, rheinglucuronic acid and rhein sulfate is small.

[Quality evaluation of Rhei Radix et Rhizoma decoction].

Decoction of single medicinal herb is a reference for the standardization of different dosage forms of Chinese medicine and it provides a new direction for solving the problems existing in the quality of Chinese medicinal granules such as no uniform dosage form and no clear quality standard. In this paper, the quality evaluation method of standard decoction of rhubarb was established to provide reference for the quality control of common dosage forms such as clinical decoction and formula granule. 10 batches of representative Rhei Radix et Rhizoma were collected to establish UPLC fingerprints were established. The chemical structures of main peaks were identified with ultra-performance liquid chromatography with quadrupole-time-of-flight mass spectrometry (UPLC-Q-TOF-MS) and the main components in the decoction were Anthraquinones. The extraction ratio of the standard decoction was (28.1±3.8)% and the transfer rate was (19.9±6.3)%. The method for the quality evaluation of standard decoction of Rhei Radix et Rhizoma was established in this study, providing reference for the quality control method of terminal products from decoction of Rhei Radix et Rhizoma.

[Simultaneous content determination of 14 components in Rhei Radix et Rhizoma by high performance liquid chromatography method].

To establish an HPLC (high performance liquid chromatography) method for the simultaneous content determination of gallic acid, (+)-catechin, (－)-epicatechin-3-O-gallate, isolindleyin, 4-(4'-hydroxyphenyl)-2-butanone, emodin, chrysophanol, physcion, aloe-emodin, rhein, lindleyin, 4-(4'-hydroxyphenyl)-2-butanone-4'-O-ß-D-(2″-O-galloyl-6″-O-cinnamoyl)-glucopyranoside, sennoside A and sennoside B in Rhei Radix et Rhizoma. The analysis was performed on Agilent Zorbax SB-C18 (4.6 mm×150 mm, 5 µm) with 0.05% phosphoric acid solution (A) - acetonitrile (B) as mobile phase for gradient elution. The flow rate was 1 mL•min⁻¹, with column temperature of 40 ℃ and the wavelength was set at 268 nm. All calibration curves showed good linearity (r > 0.999 9) within the concentration range. Both the intra- and inter-day precision for 14 analytes was less than 3.1%, with the mean recovery at the range of 91.80%-104.1%. Meanwhile, quantitative determination was carried out for 10 qualified samples from Rheum palmatum and 10 qualified samples from R. tanguticum, respectively. It was found that the content of 4-(4'-hydroxyphenyl)-2-butanone and aloe-emodin were higher in the R. tanguticum and R. palmatum, respectively, and the content of all the compounds was different in each sample. The established HPLC method for simultaneous content determination of 14 compounds from Rhei Radix et Rhizoma could be used for quantitative assessment and quality control of Rhei Radix et Rhizoma.

Characterization of the Principal Constituents of Danning Tablets, a Chinese Formula Consisting of Seven Herbs, by an UPLC-DAD-MS/MS Approach.

Danning Tablets are a traditional Chinese formula showing broad clinical applications in hepatobiliary diseases and containing a diversity of bioactive chemicals. However, the chemical profiling of the formula, which serves as the material foundation of its efficacy, is really a big challenge as Danning Tablets consist of seven herbs from different origins. An ultra-performance liquid chromatography coupled to diode array detection and electrospray ionization mass spectrometry (UPLC-DAD-ESI-MS/MS) approach was developed to characterize the principal polyphenol constituents in the formula. As a result, a total of 32 constituents, including 14 anthraquinones and their glucosides, four anthrones, two naphthalene glycosides, two stilbenes and 10 flavonoids were identified based on their retention time, UV absorption and MS/MS fragmentation patterns. The sources of these compounds were also illustrated. Most of the bioactive anthraquinone derivatives were found in Rhei Radix et Rhizoma or Polygoni Cuspidati Rhizoma et Radix, which are the Emperor drugs in the formula for its clinic usage. These findings indicate the merit of using this integrated UPLC-DAD-ESI-MS/MS approach to rapidly illustrate the chemical foundation of complex formulas. The present study will facilitate the quality control of Danning Tablet formulas as well as the individual herbs.

[Mechanism of Rhei Radix et Rhizoma combined with Scutellariae Radix on liver inflammation in rats with endotoxin disease based on p38MAPK pathway].

To explore the mechanism of Rhei Radix et Rhizoma combined with Scutellariae Radix in regulatory lipopolysaccharide (LPS)-induced liver inflammation in rats with endotoxin blood, 50 male SD rats were selected and randomly divided into blank group, model group, dexamethasone group, herbal pair high dose group, herbal pair low dose group, with 10 in each group. Rats in each were given preventive drugs for 7 consecutive days. At 0.5 h after the final administration, the model was built through the tail vein injection with LPS (5 mg•kg⁻¹). Then, animal anal temperatures were determined and recorded once every 0.5 h. The rats were killed at 4 h after the modeling to determine spleen thymus coefficient. ELISA method was used to detect cytokines interleukin-1ß (IL-1ß) and tumor necrosis factor-alpha (TNF-α) in liver tissues. The colorimetric method was applied in determination of oxidation nitrogen (NO) content in liver tissues. Western Blot method was adopted to detect Toll-like receptor protein 4, p38MAPK p38MAPK, phosphorylated p38MAPK (p-p38MAPK) and nitric oxide synthase (iNOS) protein expressions. The results showed that compared with the blank group, in the model group, TLR4 protein expression, iNOS protein expression and p38 phosphorylation expression, IL-1ß, NO and TNF-α content increased significantly in liver tissues (P<0.05 or P<0.01). And compared with the model group, the herbal pair high dose group showed significantly reduction in IL-1ß, NO and TNF-α expressions in rat liver tissues (P<0.05 or P<0.01), down-regulation in iNOS protein expression and p38 phosphorylation expression in rat liver tissues (P<0.05), but without significant up-regulation in TLR4 protein. Low-dose herbal pair can significantly reduce IL-1ß and NO expression in model rat liver tissues (P<0.01), significantly down-regulate iNOS protein expression (P<0.01), with a slight down-regulation in phosphorylation of p38 but no statistical significance, and no reduction in TLR4 expression. In conclusion, the compatibility of Rhei Radix et Rhizoma combined with Scutellariae Radix may reduce the expression of iNOS protein and the release of inflammatory cytokines IL-1ß, NO and TNF-α by decreasing p38 protein phosphorylation expression and blocking p38MAPK signaling pathways, so as to alleviate the inflammation reaction and protect the liver.

Multi-omics combined to explore the purging mechanism of Rhei Radix et Rhizoma and Magnoliae Officinalis Cortex.

Rhei Radix et Rhizoma and Magnoliae Officinalis Cortex have been used together to treat constipation in the clinical practices for more than 2000 years. Nonetheless, their compatibility mechanism is still unclear. In this study, the amelioration of Rhei Radix et Rhizoma combined with Magnoliae Officinalis Cortex on constipation was systematically and comprehensively evaluated. The results showed that their compatibility could markedly shorten gastrointestinal transport time, increase fecal water content and frequency of defecation, improve gastrointestinal hormone disorders and protect colon tissue of constipation rats compared with the single drug. Furthermore, according to 16S rRNA sequencing in conjunction with UPLC-Q-TOF/MS, the combination of two herbal medications could greatly raise the number of salutary bacteria (Lachnospiraceae, Romboutsia and Subdoligranulum) while decreasing the abundance of pathogenic bacteria (Erysipelatoclostridiaceae). And two herb drugs could markedly improve the disorder of fecal metabolic profiles. A total of 7 different metabolites associated with constipation were remarkably shifted by the compatibility of two herbs, which were mainly related to arachidonic acid metabolism, alpha-linolenic acid metabolism, unsaturated fatty acid biosynthesis and other metabolic ways. Thus, the regulation of intestinal microbiome and its metabolism could be a potential target for Rhei Radix et Rhizoma and Magnoliae Officinalis Cortex herb pair to treat constipation. Furthermore, the multi-omics approach utilized in this study, which integrated the microbiome and metabolome, had potential for investigating the mechanism of traditional Chinese medicines.

Effect of Rhei Radix et Rhizoma and Eupolyphaga Steleophaga on liver protection mechanism based on pharmacokinetics and metabonomics.

Objective: Based on metabonomics technology of high-performance liquid chromatography-mass spectrometry (HPLC-MS/MS) and hydrogen nuclear magnetic resonance spectroscopy (1H NMR), the pharmacokinetic characteristics and therapeutic mechanism of Rhei Radix et Rhizoma (RhRR, Dahuang in Chinese), Eupolyphaga Steleophaga (EuS, Tubiechong in Chinese) combined with RhRR acting on acute liver injury were explored. Methods: Models of acute liver injury were established, and the pharmacokinetic methods of five components of RhRR-EuS in rats were found by HPLC-MS/MS. The liver tissues of different groups of mice were analyzed by 1H NMR spectroscopy combined with multivariate statistical analysis to investigate the metabolomics of RhRR-EuS and RhRR. Results: Pharmacokinetic results showed there were different levels of bimodal phenomenon in different groups, and the absorption of free anthraquinone in RhRR increased after compatibility with EuS. In addition, the pathological state of acute liver injury in rats can selectively promote the absorption of emodin, chrysophanol, physcion and aloe emodin. Through 15 differential metabolites in the liver tissue of acute liver injury mice, it was revealed that RhRR-EuS and RhRR could protect the liver injury by regulating the metabolism of glutamine and glutamic acid, alanine, aspartic acid and glutamic acid, and phosphoinositide. However, the regulation of RhRR was weaker than that of RhRR-EuS. Conclusion: For the first time, we studied the pharmacokinetics and metabolomics differences of RhRR-EuS and RhRR in rats and mice with acute liver injury, in order to provide theoretical reference for clinical treatment of liver disease by DHZCP.

Scorch processing of rhubarb (Rheum tanguticum Maxim. ex Balf.) pyrolyzed anthraquinone glucosides into aglycones and improved the therapeutic effects on thromboinflammation via regulating the complement and coagulation cascades pathway.

ETHNOPHARMACOLOGICAL RELEVANCE: The pathophysiological mechanism of thromboinflammation involves the intricate interplay between the inflammatory responses and coagulation cascades. Rhubarb is frequently used in traditional Chinese medicine to treat thromboinflammatory diseases. The scorched rhubarb (prepared by stir-baking the dried raw rhubarb till it partly turns to charcoal) is believed to possess enhanced blood-cooling and stasis-removing functions compared to the raw rhubarb, thereby augmenting the therapeutic effects on thromboinflammation. AIM OF THE STUDY: This study aimed to explore the chemical and pharmacological foundations of the scorch processing of rhubarb in order to ensure and enhance the efficacy and safety of the scorched rhubarb for treating thromboinflammatory diseases. MATERIALS AND METHODS: The dried raw rhubarb pieces were subjected to stir-baking at 180 °C for 10∼80 min to obtain the rhubarbs with varying degrees of scorching. Typical ingredients present in rhubarb pieces and extracts were determined by high-performance liquid chromatography. The therapeutic effects of the raw and scorched rhubarb on thromboinflammation were evaluated using a rat model. Proteomics analysis was employed to screen potential biological pathways associated with thromboinflammation treatment by the raw and scorched rhubarb, which were further verified using a cell model. RESULTS: Morphological properties indicated that the rhubarb baked at 180 °C for 50 min in this research showed the optimal degree of scorching. Compared to the raw rhubarb, the properly scorched rhubarb exhibited lower levels of anthraquinone glucosides, higher levels of anthraquinone aglycones, superior anti-thromboinflammatory effects, and no purgative side effects. Proteomics analysis revealed that the complement and coagulation cascades pathway played a significant role in mediating the therapeutic effects of the raw and scorched rhubarb on thromboinflammation. Furthermore, it was found that anthraquinone aglycones were more effective than their glucoside counterparts in restoring the impaired vascular endothelial cells as well as regulating the complement and coagulation cascades pathway. CONCLUSIONS: Proper scorch processing may augment the therapeutic effects of rhubarb on thromboinflammation via relieving inflammation and oxidative stress, repairing vascular endothelial cells, restoring coagulation cascades and blood rheology, and regulating some other biological processes. This may be partly caused by the scorch-induced thermolysis of anthraquinone glucosides into their aglycone counterparts that seemed to perform better in regulating the complement and coagulation cascades pathway.

Rhei Radix et Rhizoma and its anthraquinone derivatives: Potential candidates for pancreatitis treatment.

BACKGROUND: Pancreatitis is a common exocrine inflammatory disease of the pancreas and lacks specific medication currently. Rhei Radix et Rhizoma (RR) and its anthraquinone derivatives (AQs) have been successively reported for their pharmacological effects and molecular mechanisms in experimental and clinical pancreatitis. However, an overview of the anti-pancreatitis potential of RR and its AQs is limited. PURPOSE: To summarize and analyze the pharmacological effects of RR and its AQs on pancreatitis and the underlying mechanisms, and discuss their drug-like properties and future perspectives. METHODS: The articles related to RR and its AQs were collected from the Chinese National Knowledge Infrastructure, Wanfang data, PubMed, and the Web of Science using relevant keywords from the study's inception until April first, 2024. Studies involving RR or its AQs in cell or animal pancreatitis models as well as structure-activity relationship, pharmacokinetics, toxicology, and clinical trials were included. RESULTS: Most experimental studies are based on severe acute pancreatitis rat models and a few on chronic pancreatitis. Several bioactive anthraquinone derivatives of Rhei Radix et Rhizoma (RRAQs) exert local protective effects on the pancreas by maintaining pancreatic acinar cell homeostasis, inhibiting inflammatory signaling, and anti-fibrosis, and they improve systemic organ function by alleviating intestinal and lung injury. Pharmacokinetic and toxicity studies have revealed the low bioavailability and wide distribution of RRAQs, as well as hepatotoxicity and nephrotoxicity. However, there is insufficient research on the clinical application of RRAQs in pancreatitis. Furthermore, we propose effective strategies for subsequent improvement in terms of balancing effectiveness and safety. CONCLUSION: RRAQs can be developed as either candidate drugs or novel lead structures for pancreatitis treatment. The comprehensive review of RR and its AQs provides references for optimizing drugs, developing therapies, and conducting future studies on pancreatitis.

Magnetic-stirring-enhanced mechanical amorphous dispersion extraction for the hydrophobic phytochemical constituents using an aqueous solution from a medicinal plant.

A method involving chitosan-assisted magnetic-stirring-enhanced mechanical amorphous dispersion extraction was developed and utilized to extract hydrophobic anthraquinones from Rhei Radix et Rhizoma prior to ultrahigh performance liquid chromatography analysis. Incorporating natural chitosan as a dispersant facilitated the extraction of hydrophobic anthraquinones using purified water, considerably enhancing the eco-friendliness of the extraction methodology. To optimize extraction efficiency, an extensive evaluation of the crucial parameters influencing rhubarb yield was conducted. Furthermore, a response surface methodology was applied to optimize the extraction conditions. Under these optimized conditions, the method exhibited linearity ranges of 0.1-100 µg/mL, with correlation coefficients between 0.9990 and 0.9998. The method's intraday (n = 6) and interday (n = 6) precision levels were maintained at ≤3.58%, which was considered to be within acceptable limits. The computed detection and quantification limits were 16.54-24.60 and 54.91-82.04 ng/mL, respectively. Consequently, this optimized method was effectively employed to extract five specific compounds (aloe-emodin, emodin, rhein, chrysophanol, and physcion) from Rhei Radix et Rhizoma, achieving recoveries ranging from 86.43% to 102.75%.

The Rhei radix rhizoma-based carbon dots ameliorates dextran sodium sulphate-induced ulcerative colitis in mice.

As an autoimmune disease of the colon, the incidence of ulcerative colitis (UC) remains high. Carbon dots (CDs), a new type of nanomaterials, display excellent biological activity and are expected to inspire a new treatment for UC. A green method was used to carbonise rhei radix rhizoma (RRR) and extract CDs to study their anti-ulcer activity. The RRR-based carbon dots (RRR-CDs) were characterised by electron microscopy, optical techniques, and other techniques. The results indicated RRR-CDs have abundant chemical groups, excellent solubility and tiny size (1.374 nm-4.533 nm), which may be conducive to the exertion of inherent activity. Using a classic dextran sodium sulphate (DSS)-induced UC mouse model, for the first time, it was demonstrated RRR-CDs have significant anti-ulcerative activity in improving DAI score (from 2.8 to 1.6), colon length (4.15 to 6.08), and histopathology in mice. The underlying mechanisms of anti-ulcerative activity may be related to haemostatic, antioxidant, and anti-inflammatory activities to protect the mucosal barrier. RRR-CDs have symptomatic and potential mechanisms of treatment and are expected to become a candidate drug for the treatment of UC. This not only further expands the basis for the biological activity of CDs, but provides a potential treatment plan for solving thorny diseases in clinical practice.

Separation and purification of glycosides from medicinal plants based on strong polar separation medium with online closed-loop mode.

Natural glycosides widely distributed in medicinal plants are valuable sources of therapeutic agents, showing various pharmacological effects. The separation and purification of natural glycosides are meaningful for their pharmacological research, which face with great challenges due to the complex of medicinal plants samples. In this work, two kinds of functional monolithic separation mediums A and S were fabricated and fully applied in the online extraction, separation and purification of active glycoside components from medicinal plants with a simple-procedure closed-loop mode. Chrysophanol glucoside and physcion glucoside were detected and separated from Rhei Radix et Rhizoma using separation medium A as a solid-phase extraction adsorbent. Rhapontin was isolated and purified from Rheum hotaoense C. Y. Cheng et Kao using separation medium S as the stationary phase of high-performance liquid chromatography. Compared to the reported literatures, high yield of 5.68, 1.20 and 4.76 mg g-1 of these three products were obtained with high purity. These two online closed-loop mode methods were carried out using high-performance liquid chromatography system, in which the sample injection, isolation and purification procedures are all online mode, and reduced loss compared to offline extraction and purification procedures, thus achieving high recovery and high purity.