It is generally believed that high-quality Bupleurum scorzonerifolium roots possess specific morphological characteristics, being red, robust, and long with strong odor. However, the scientific connotation of these characteristics has not been elucidated. According to the theory of "quality evaluation through morphological identification", we studied the correlations between appearance traits(the RGB value of root surface, root length, root diameter, dry weight, and ratio of phloem to xylem) and content of main chemical components(volatile oils, total saponins, total flavonoids, total polysaccharides, and seven saikosaponins) of B. scorzonerifolium roots. Epson Scanner and ImageJ were used to scan the root samples and measure the appearance traits. Ultraviolet spectrophotometry and HPLC were employed to determine the content of chemical components. The correlation, regression, and cluster analyses were performed to study the correlations between the appearance traits and the content of chemical components. The results showed that the content of volatile oils and saikosaponins were significantly correlated with RGB value, root length, and root diameter, indicating that within a certain range, the roots being redder, longer, and thicker had higher content of volatile oils and saikosaponins. According to the appearance traits and chemical component content, the 14 samples from different producing areas were classified into four grades, and the differences in morphological traits and chemical component content were consistent among different grades. The findings in this study demonstrate that appearance traits(RGB value, root length, and root diameter) can be used to evaluate the quality of B. scorzonerifolium roots. Meanwhile, this study lays a foundation for establishing an objective quality evaluation method for B. scorzonerifolium roots.
Bupleurum/chemistry* ; Saponins/analysis* ; Oleanolic Acid/analysis* ; Oils, Volatile/analysis* ; Plant Roots/chemistry*

Through consulting the herbs and medical books of past dynasties, combining with modern literature and field investigation, this paper made textual research on the name, origin, producing area, harvesting and processing of Bupleuri Radix used in the Catalogue of Ancient Classical Prescriptions(the first batch).From Han to the Southern and Northern Dynasties, the source of Bupleuri Radix was a mixture of Bupleurum and Peucedanum, it's hard to define the origin of authentic products.In Tang Dynasty, Caryophyllaceae had been used as Bupleuri Radix. In Song Dynasty, it was clear that the genuine production area of Bupleuri Radix was Yinzhou, its origin was B. corzonerifolium and B. yinchowense.After the Ming Dynasty, B. chinense gradually became the mainstream. It has been confirmed that there were differences in the efficacy between Stellaria dichotoma in Caryophyllaceae and Bupleurum in Umbelliferae, however, the use of S. dichotoma is still attributed to Bupleuri Radix. In the Qing Dynasty, S. dichotoma was distinguished from Bupleuri Radix as another medicine. Among the prescriptions containing Bupleuri Radix included in the Catalogue of Classical Prescriptions in Ancient China(the first batch), the mainstream of genuine Bupleuri Radix should be B. scorzonerifolium and B. chinense. It is suggested that the genuine base of Bupleuri Radix should be selected according to the current resources and industrial development of Bupleuri Radix, and it should conform to the Chinese Pharmacopoeia.
Bupleurum/chemistry* ; China ; Drugs, Chinese Herbal ; Medicine, Chinese Traditional ; Plant Roots/chemistry* ; Prescriptions

UPLC-Q-TOF-MS was used to analyze the chemical differences in Bupleurum. chinense,B. marginatum,B. marginatum var. stenophyllum and B. smithii var. parvifolium. Chromatographic separation was carried out on an Acquity HSS T3 C_(18) column( 2. 1 mm ×100 mm,1. 8 μm,Waters) with the mobile phase composed of 0. 1% formic acid in water-acetonitrile in the gradient elution. A hybrid quadrupole time-of-flight tandem mass spectrometry( Q-TOF-MS~E) was used for mass spectrometric analysis. Finally,25 peaks were identified based on their exact mass data and fragmentation characteristics. B.chinense,B.marginatum,B. marginatum var. stenophyllum and B. smithii var. parvifolium were obviously clustered into 3 types through processing by principal component analysis( PCA). There was almost no difference between B. chinense and B. marginatum. However,the compounds existed in B. chinense were different from those in B. marginatum var. stenophyllum,and B. smithii var. parvifolium.
Bupleurum ; chemistry ; classification ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; Phytochemicals ; analysis ; Tandem Mass Spectrometry

Depression is a kind of mental illness accompanied by complex etiology and pathogenesis in clinic. With the quickening pace of circadian rhythm and increase of life pressure in modern society, the incidence of depression is increasing year by year. Nowadays, some typical antidepressant Western medicines, such as selective serotonin re-uptake inhibitors (SSRI) and tricyclic antidepressants (TCA), have been used as the main therapeutic drugs in clinic. Unfortunately, administration of these drugs will result in severe adverse reactions, slow treatments, and low cure rates, thus obviously they can not be used for a long term. Sini San, which originated from written by Zhang zhongjing, is a prescription widely applied in clinic for curing mental illness and also a basic Chinese herbal formula for modern treatment of depression. This article would review the research progress on antidepressant effects of Sini San based on single herbs of Bupleuri Radix and Paeoniae Radix Alba, herb-pair of Bupleuri Radix-Paeoniae Radix Alba, and formula of Sini San, providing directions and ideas for future research on complicated Chinese herbal formulae.
Antidepressive Agents ; pharmacology ; Bupleurum ; chemistry ; Depression ; drug therapy ; Drugs, Chinese Herbal ; pharmacology ; Humans ; Paeonia ; chemistry

Epoxy ether type and isophthalene type saponin are the main saponins of Bupleurum chinense. However,due to the difference of their UV spectrum,there is no quantitative method for simultaneous determination of these two kinds of saponins. In this paper,a dual-wavelength high performance liquid chromatography(HPLC) was developed for simultaneous determination of five saponins in epoxidized ether(saikosaponin a,c,d) and isosorbide type(saikosaponin b1,b2). The mobile phase was eluted with acetonitrile-water(0.1% phosphoric acid) gradient at a column temperature of 30 °C and a flow rate of 1.0 mL·min⁻¹. The detection wavelengths were 208 nm for saikosaponins a,c, and d, and 254 nm for saikosaponins b₁ and b₂. The results showed that the separation of five kinds of saikosaponin was good, with the linear range of 9.70-1 935.00(=0.999 4),8.20-1 380.00(=0.999 3),6.90-1 640.00(=0.999 0),5.25-630.00(=0.999 4), and 5.15-618.00 mg·L⁻¹(=0.999 5), respectively. The average recoveries were 97.70%-100.2% and the RSD was less than 3%(=6). The method is simple,rapid and reproducible. It can be used for the determination of five kinds of saikosaponins in B. chinense.
Bupleurum ; chemistry ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; Oleanolic Acid ; analogs & derivatives ; isolation & purification ; Plant Roots ; chemistry ; Saponins ; isolation & purification

The present study aimed to investigate the effects of polysaccharides extracted from Bupleurum chinense DC (BCPs) on macrophage functions. In the in vivo experiment, 1 mL of 5% sodium thioglycollate was injected into the abdomen of the mice on Day 0 and macrophages were harvested on Day 4. The macrophages were cultured in plates and treated with different concentrations of BCPs and stimulus. Effects of BCPs on macrophage functions were assessed by chemotaxis assay, phagocytosis assay and Enzyme-Linked Immunosorbent Assay (ELISA). Our results showed the enhanced chemotaxis, phagocytosis and secretion of nitric oxide (NO) and inflammatory cytokines by macrophages when treated with BCPs. However, when chemotaxis and phagocytosis were up-regulated by complement components or opsonized particles, BCPs inhibited these effects. Also, the NO production induced by lipopolysaccharides (LPS) was suppressed by BCPs mildly. Moreover, BCPs had an inhibitory effect on the [Ca] elevation of macrophages. These results suggested that BCPs exerted modulatory effects on macrophage functions, which may contribute to developing novel approaches to treating inflammatory diseases.
Animals ; Bupleurum ; chemistry ; Chemotaxis ; drug effects ; Cytokines ; analysis ; metabolism ; Immunologic Factors ; pharmacology ; Immunomodulation ; drug effects ; Macrophages ; drug effects ; Mice ; Mice, Inbred BALB C ; Nitric Oxide ; analysis ; metabolism ; Phagocytosis ; drug effects ; Plant Extracts ; chemistry ; isolation & purification ; pharmacology ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Polysaccharides ; isolation & purification ; pharmacology

Lipopolysaccharides (LPS) contamination in herbal crude polysaccharides is inevitable. The present study was performed to explore the effect of polymyxin B on abolishing the influence of LPS contamination in mononuclear cells. LPS was pretreated with polymyxin B sulfate (PB) at different concentrations for 1, 5 or 24 h, and then used to stimulate RAW264.7 and mouse peritoneal macrophages (MPMs). The nitric oxide (NO) and tumor necrosis factor-α (TNF-α) in cell culture supernatant, as the indications of cell response, were assayed. Bupleurum chinensis polysaccharides (BCPs) with trace amount contamination of LPS was treated with PB. 30 μg·mL of PB, treating LPS (10 and 1 000 ng·mL in stimulating RAW264.7 and MPMs respectively) at 37 °C for 24 h, successfully abolished the stimulating effect of LPS on the cells. When the cells were stimulated with LPS, BCPs further promoted NO production. However, pretreated with PB, BCPs showed a suppression of NO production in MPMs and no change in RAW264.7. In the in vitro experiments, LPS contamination in polysaccharide might bring a great interference in assessing the activity of drug. Pretreatment with PB (30 μg·mL) at 37 °C for 24 h was sufficient to abolish the effects of LPS contamination (10 and 1 000 ng·mL).
Animals ; Bupleurum ; chemistry ; Drug Contamination ; Drugs, Chinese Herbal ; analysis ; pharmacology ; Lipopolysaccharides ; analysis ; antagonists & inhibitors ; Macrophages ; drug effects ; metabolism ; Mice ; Nitric Oxide ; metabolism ; Polymyxin B ; analysis ; pharmacology ; Polysaccharides ; analysis ; pharmacology ; Tumor Necrosis Factor-alpha ; metabolism

5-Hydroxytryptamine 2C (5-HT) receptor is one of the major targets of anti-obesity agents, due to its role in regulation of appetite. In the present study, the 70% EtOH extract of the roots of Bupleurum chinense was revealed to have agonistic activity on 5-HT receptor, and the subsequent bioassay-guided isolation led to identification of several saikosaponins as the active constituents with 5-HT receptor agonistic activity in vitro and anti-obesity activity in vivo. The new compound, 22-oxosaikosaponin d (1), was determined by extensive spectroscopic analyses (HR-ESI-MS, IR, and 1D and 2D NMR). The primary structure-activity relationship study suggested that the intramolecular ether bond between C-13 and C-28 and the number of sugars at C-3 position were closely related to the 5-HT receptor agonistic activity. Saikosaponin a (3), the main saponin in B. chinense, showed obviously agonistic activity on 5-HT receptor with an EC value of 21.08 ± 0.33 μmol·Lin vitro and could reduce food intake by 39.1% and 69.2%, and weight gain by 13.6% and 16.4%, respectively, at 3.0 and 6.0 mg·kgin vivo. This investigation provided valuable information for the potential use of B. chinense as anti-obesity agent.
Animals ; Anti-Obesity Agents ; chemistry ; isolation & purification ; pharmacology ; Biological Assay ; Bupleurum ; chemistry ; Male ; Oleanolic Acid ; analogs & derivatives ; chemistry ; isolation & purification ; pharmacology ; Rats ; Rats, Sprague-Dawley ; Saponins ; chemistry ; isolation & purification ; pharmacology ; Serotonin 5-HT2 Receptor Agonists ; chemistry ; isolation & purification ; pharmacology ; Structure-Activity Relationship

OBJECTIVETo analyze the effect of Chinese herbs used by Prof. LI Tao on peripheral blood T subsets in treating multiple sclerosis (MS) by using association rules and statistical methods, thereby providing evidence for optimizing prescriptions.

METHODSData of MS inpatients and outpatients recorded by data collecting system, Xiyuan Hospital, China Academy of Chinese Medical Sciences were resorted. The relationship between Chinese herbs and T cell subsets were analyzed using SPSS17.0 and Aprior module in SPSS Clementine 12.0.

RESULTSRadix bupleuri, Radix Paeoniae alba, Fructus Aurantii, Atractylodes, and Radix Glycyrrhizae were most commonly used herbal combinations.Radix Aconiti lateralis preparata and Rhizoma Smilacis glabrae were often added. Radix Aconiti lateralis preparata was associated with decreased Th1 cells (confidence level 83.78%, supportive level 36.26%). Decreased Th1 cell was associated with Radix Aconiti lateralis preparata (confidence level 71.26%, supportive level 36.26%).Radix Aconiti lateralis preparata was obviously associated with decreased Th1 cells. Radix Bupleuri, Radix Paeoniae alba, bitter orange, Atractylodes , Radix glycyrrhizae, and Radix Aconiti lateralis preparata could reduce peripheral blood Th1 subsets of MS patients and elevate Th2 subsets (all P < 0.01).

CONCLUSIONSThe herbal combination of Radix Bupleuri, Radix Paeoniae alba, Fructus Aurantii, Atractylodes, Radix Glycyrrhizae, Rhizoma Smilacis glabrae, and Radix Aconiti lateralis preparata could lower peripheral blood Th1 cells and elevate Th2 cells, and prevent the relapse of MS possibly by reducing Th1 cells and elevating Th2 cells. Especially Radix Aconiti lateralis preparata played important roles in aforesaid changes of Th1 and Th2.

Aconitum ; chemistry ; Atractylodes ; chemistry ; Bupleurum ; chemistry ; China ; Drugs, Chinese Herbal ; therapeutic use ; Fruit ; chemistry ; Glycyrrhiza ; chemistry ; Humans ; Multiple Sclerosis ; therapy ; Paeonia ; chemistry ; Plant Roots ; chemistry ; Rhizome ; chemistry ; Smilacaceae ; chemistry ; T-Lymphocyte Subsets ; drug effects

We revisited the "Xiao Chaihu Decoction event (XCHDE)" occurred in late 1980s in Japan and the Bupleuri Radix related adverse drug reaction (ADR) reports in China After careful review, comparison, analysis and evaluation, we think the interstitial pneumonitis, drug induced Liver injury (DILI) and other severe adverse drug envents (ADEs) including death happened in Japan is probably results from multiple factors, including combinatory use of XCHDE with interferon, Kampo usage under modern medicine theory guidance, and use of XCHD on the basis of disease diagnosis instead of traditional Chinese syndrome complex differentiation. There are less ADE case reports related to XCHD preparation in China compared to Japan, mostly manifest with hypersensitivity responses of skin and perfuse perspiration. The symptoms of Radix Bupleuri injection related ADEs mainly manifest hypersensitivity-like response, 2 cases of intravenous infusion instead of intramuscular injection developed hypokalemia and renal failure. One case died from severe hypersensitivity shock. In Chinese literatures, there is no report of the interstitial pneumonitis and DILI associated with XCHDG in Japan. So far, there is no voluntary monitoring data and large sample clinical research data available. The author elaborated the classification of "reevaluation" and clarified "re-evaluation upon events" included the reaction to the suspected safety and efficacy events. Based on the current status of the clinical research on the Radix Bupleuri preparations, the author points out that post-marketing "re-evaluation upon suspected event" is not only a necessity of continuous evaluation of the safety, efficacy of drugs, it is also a necessity for providing objective clinical research data to share with the international and domestic drug administrations in the risk-benefit evaluation. It is also the unavoidable pathway to culture and push the excellent species and famous brands of TCM to the international market, in that it enhances the pharmaceutical manufactures the ability to control enterprise risk and eliminate the negative impact on traditional Chinese medicine. With the widely used and ADR report concentrated Radix Bupleuri injection as an example, the author provide a new approach to post-marketing clinical research.
Bupleurum ; chemistry ; Drug Compounding ; Drug-Related Side Effects and Adverse Reactions ; etiology ; Drugs, Chinese Herbal ; adverse effects ; Humans ; Product Surveillance, Postmarketing ; methods ; Safety