Search Results (23)

Bupleurum scorzonerifolium Willd. is a commonly used bulk Chinese herbal remedy. Due to the large-scale mining of wild Bupleurum scorzonerifolium Willd., its natural resources are gradually exhausted. In addition, there are some problems in Bupleurum scorzonerifolium Willd. cultivation, such as lack of guidance, excessive application of fertilizers and so on, which lead to the yield and quality of Bupleurum to be below the standard value. Therefore, it is significant to clarify the regulation of quality and yield under different levels of fertilizers. In this study, three different levels of potassium fertilizer were applied; then, the metabolites in different parts of Bupleurum were analyzed by gas chromatography–mass spectrometry (GC–MS) to detect the alterations in the metabolic spectrum and recognize both the accumulation and distribution of key metabolites in response to each level of potassium fertilizer. The contents of various mineral elements, such as sodium, calcium, potassium, magnesium, manganese, zinc, iron, and copper, in different parts of Bupleurum under different potassium levels were determined. Potassium fertilizer had a significant impact on the absorption and distribution of these mineral elements. There were synergistic and antagonistic effects between each element and K⁺. The results showed that low and high potassium levels could promote the progression of main shoots and roots, but inhibited the accumulation of dry matter in lateral shoots and flowers. Low potassium levels stimulated the content of saikosaponin a in all plant parts, while high potassium levels inhibited the accumulation of most saikosaponin a,c and d. A total of 77 metabolites were identified by GC–MS, of which glycerol, d-glucose, silane and copper phthalocyanine were highlighted as the key metabolites in response to potassium fertilizer. The abovementioned metabolites are mapped into insulin signaling pathways, streptomycin biosynthesis, galactose metabolism and other metabolic pathways, sustaining the metabolic regulation of Bupleurum scorzonerifolium Willd. Full article

Douchi is a kind of soybean-fermented food in China. To explore the common and differential compounds in different Douchi, Douchi was fermented by Aspergillus niger, Rhizopus arrhizus, and Bacillus circulans, respectively, and co-fermented by the three strains in this study. The common and characteristic flavor compounds and common and characteristic non-volatile components of different strains of fermented Douchi were explored through GC×GC-TOFMS and UPLC–Q-TOFMS omics analysis. The result suggested that Pyrazines, ketones, and alkenes such as tetramethyl-pyrazine, 2,5-dimethyl pyrazine, furaneol, 2,3-butanedione, gamma-terpinene might contribute to the basic flavor of the Douchi fermented by A. niger, R. arrhizus, and B. circulans. Peptides, amines, and flavonoids, such as N–acetylhistamine, 7,3′,4′–trihydroxyflavone, (3S,8As)-3-isobutylhexahydropyrrolo[1,2-a]pyrazine-1,4-dione might contribute to the basic function of the above three Douchi. The common metabolic pathways involved in the fermentation were isoflavonoid biosynthesis, flavonoid biosynthesis, etc. Ketones and esters such as 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyran-4-one, 3-octanone, 5-methylfurfural and nonanal contributed to the unique flavor, while betaine, oleanolic acid, saikosaponin D and leucine might contribute to the unique function of A. niger fermented Douchi. Alkenes, pyrazine, and ketones such as α-terpinene, ethyl-pyrazine, dihydro-3-methyl-2(3H)-furanone, and linalool might contribute to unique flavor, while cordycepin, 2-Phenylacetamide might contributed to the unique function of R. arrhizus fermented Douchi. The unique flavor of B. circulans fermented Douchi might derived from ketones and esters such as 3-acetyl-2-butanone, 2-tridecanone, propionic acid-2-phenylethyl ester, while vitexin, astragalin, and phenethylamine might contribute to the unique function. Compared with single-strain fermented Douchi, the flavor substances and non-volatile components in multi-strain fermented Douchi were more abundant, such as hexadecanoic acid methyl ester, benzeneacetic acid ethyl ester, 9,12-octadecadienoic acid ethyl ester, nuciferine, and erucamide. It was speculated that there were common and differential substances in Douchi fermented by Aspergillus niger, Rhizopus arrhizus, and Bacillus circulans, which might contribute to the basic and unique flavor and function. Compared with single-strain fermented Douchi, the flavor substances and metabolites in multi-strain fermented Douchi were more abundant. This study provided a reference for the research of flavor and functional substances of Douchi. Full article

Saikosaponin D (SSD), derived from Bupleurum falcatum L., has various pharmacological properties, including immunoregulatory, anti-inflammatory, and anti-allergic effects. Several studies have investigated the anti-tumor effects of SSD on cancer in multiple organs. However, its role in colorectal cancer (CRC) remains unclear. Therefore, this study aimed to elucidate the suppressive effects of SSD on CRC cell survival and metastasis. SSD reduced the survival and colony formation ability of CRC cells. SSD-induced autophagy and apoptosis in CRC cells were measured using flow cytometry. SSD treatment increased LC3B and p62 autophagic factor levels in CRC cells. Moreover, SSD-induced apoptosis occurred through the cleavage of caspase-9, caspase-3, and PARP, along with the downregulation of the Bcl-2 family. In the in vivo experiment, a reduction in the number of metastatic tumor nodules in the lungs was observed after the oral administration of SSD. Based on these results, SSD inhibits the metastasis of CRC cells to the lungs by inducing autophagy and apoptosis. In conclusion, SSD suppressed the proliferation and metastasis of CRC cells, suggesting its potential as a novel substance for the metastatic CRC treatment. Full article

The incidence of depression has been steadily rising in recent years, making it one of the most prevalent mental illnesses. As the pursuit of novel antidepressant drugs captivates the pharmaceutical field, the therapeutic efficacy of Traditional Chinese Medicine (TCM) has been widely explored. Chaihu (Bupleurum) has been traditionally used for liver conditions such as hepatitis, liver inflammation, liver fibrosis, and liver cancer. It is believed to have hepatoprotective effects, promoting liver cell regeneration and protecting against liver damage. In addition, Bupleurum has also been used as a Jie Yu (depression-relieving) medicine in China, Japan, Republic of Korea, and other Asian countries for centuries. This review article aims to summarize the research conducted on the antidepressant properties and mechanisms of Bupleurum, as well as discuss the potential of TCM formulas containing Bupleurum. This review highlights various antidepressant ingredients isolated from Bupleurum, including saikosaponin A, saikosaponin D, rutin, puerarin, and quercetin, each with distinct mechanisms of action. Additionally, Chinese herb prescriptions and extracts containing Bupleurum, such as Chaihu Shugansan, Xiaoyaosan, and Sinisan, are also included due to their demonstrated antidepressant effects. This review reveals that these Bupleurum compounds exhibit antidepressant effects through the regulation of neurotransmitter mechanisms (such as 5-HT and DA), the NMDA (N-methyl-D-aspartate) system, brain-derived neurotrophic factor (BDNF), and other intracellular signaling pathways. Collectively, this comprehensive review provides insights into the multiple applications of Bupleurum in the treatment of depression and highlights its potential as an alternative or complementary approach to traditional therapies. However, it is essential to consider the potential adverse effects and clinical restrictions of Bupleurum despite its promising potential. Further research is needed to elucidate its specific mechanisms of action and evaluate its effectiveness in human subjects. Full article

Saikosaponins (SS) are the main active components of Bupleuri Radix. In this study, the yields of SS a, b₁, b₂, c, d, e, and f were simultaneously determined using the HPLC-DAD dual wavelength method, and the ultrasound-assisted extraction process of saikosaponins was optimized using the response surface methodology. The antioxidant effect of saikosaponins was investigated using the scavenging rate of 1, 1-diphenyl-2-picrylhydrazyl (DPPH), 2, 2-diazo-bis (3-ethyl-benzothiazole-6-sulfonic acid) diammonium salt (ABTS), and hydroxyl (-OH) groups, and the mechanism was clarified via network pharmacological analysis. The results showed that the optimal extraction process of SS was a 5% ammonia–methanol solution as an extraction solvent, a material–liquid ratio of 1:40, a temperature of 46.66 °C, an extraction time of 65.07 min, and an ultrasonic power of 345.56 W. The total content of the seven saikosaponins under this condition was up to 6.32%, which was close to the model’s predicted value of 6.56%, where the yields of the seven saikosaponins a, b₁, b₂, c, d, e, and f were 1.18%, 0.11%, 0.26%, 1.02%, 3.02%, 0.38%, and 0.44%, respectively. The saikosaponins have an obvious scavenging ability for DPPH, ABTS, and -OH radicals. The interactions of seven saikosaponins with antioxidant targets were studied, and a database was used to collate the core of saikosaponins and antioxidants through network pharmacology. The mechanisms of the antioxidant effects of the saikosaponins were derived via GO enrichment analysis and KEGG pathway analysis. Finally, the binding energy of the saikosaponins to the antioxidant targets was found to be less than −5.0 kcal·mol⁻¹ via molecular docking, indicating that the antioxidant capacity of the saikosaponins are good. Therefore, this study developed a rapid and efficient method for the extraction of saikosaponins, which provides a theoretical basis for an in-depth understanding of the rational utilization of saikosaponins and the development of their medicinal value. Full article

The purpose of this work was to illustrate the effect of processing with vinegar on saikosaponins of Bupleurum chinense DC. (BC) and the protective effects of saikosaponin A (SSA), saikosaponin b1 (SSb1), saikosaponin b2 (SSb2), and saikosaponin D (SSD) in lipopolysaccharide (LPS)-induced acute lung injury (ALI) mice. We comprehensively evaluated the anti-inflammatory effects and potential mechanisms of SSA, SSb1, SSb2, and SSD through an LPS-induced ALI model using intratracheal injection. The results showed that SSA, SSb1, SSb2, and SSD significantly decreased pulmonary edema; reduced the levels of IL-6, TNF-α, and IL-1β in serum and lung tissues; alleviated pulmonary pathological damage; and decreased the levels of the IL-6, TNF-α, and IL-1β genes and the expression of NF-κB/TLR4-related proteins. Interestingly, they were similar in structure, but SSb2 had a better anti-inflammatory effect at the same dose, according to a principal component analysis. These findings indicated that it may not have been comprehensive to only use SSA and SSD as indicators to evaluate the quality of BC, especially as the contents of SSb1 and SSb2 in vinegar-processed BC were significantly increased. Full article

Saikosaponin D (SSD), an active compound derived from the traditional plant Radix bupleuri, showcases potential in disease management owing to its antioxidant, antipyretic, and anti-inflammatory properties. The toxicological effects of SSD mainly include hepatotoxicity, neurotoxicity, hemolysis, and cardiotoxicity. SSD exhibits antitumor effects on multiple targets and has been witnessed in diverse cancer types by articulating various cell signaling pathways. As a result, carcinogenic processes such as proliferation, invasion, metastasis, and angiogenesis are inhibited, whereas apoptosis, autophagy, and differentiation are induced in several cancer cells. Since it reduces side effects and strengthens anti-cancerous benefits, SSD has been shown to have an additive or synergistic impact with chemo-preventive medicines. Regardless of its efficacy and benefits, the considerations of SSD in cancer prevention are absolutely under-researched due to its penurious bioavailability. Diverse studies have overcome the impediments of inadequate bioavailability using nanotechnology-based methods such as nanoparticle encapsulation, liposomes, and several other formulations. In this review, we emphasize the association of SSD in cancer therapeutics and the discussion of the mechanisms of action with the significance of experimental evidence. Full article

Bupleurum chinense is an important medicinal plant in China; however, little is known regarding how this plant transcribes and synthesizes saikosaponins under drought stress. Herein, we investigated how drought stress stimulates the transcriptional changes of B. chinense to synthesize saikosaponins. Short-term drought stress induced the accumulation of saikosaponins, especially from the first re-watering stage (RD_1 stage) to the second re-watering stage (RD_2 stage). Saikosaponin-a and saikosaponin-d increased by 84.60% and 75.13%, respectively, from the RD_1 stage to the RD_2 stage. Drought stress also stimulated a rapid increase in the levels of the hormones abscisic acid, salicylic acid, and jasmonic acid. We screened 49 Unigenes regarding the terpenoid backbone and triterpenoid biosynthesis, of which 33 differential genes were significantly up-regulated during drought stress. Moreover, one P450 and two UGTs are possibly involved in the synthesis of saikosaponins, while some transcription factors may be involved in regulating the expression of key enzyme genes. Our study provides a reference for the cultivation of B. chinense and a practical means to ensure the quality (safety and effectiveness) of B. chinense for medicinal use, as well as insights into the modernization of the China Agriculture Research System. Full article

The saponins of Bupleurum falcatum L., saikosaponins, are the major components responsible for its pharmacological and biological activities. However, the anti-cancer effects of prosaikogenin and saikogenin, which are glycoside hydrolyzed saikosaponins, are still unknown due to its rarity in plants. In this study, we applied two recombinant glycoside hydrolases that exhibit glycoside cleavage activity with saikosaponins. The two enzymes, BglPm and BglLk, were cloned from Paenibacillus mucilaginosus and Lactobacillus koreensis, and exhibited good activity between 30–37 °C and pH 6.5–7.0. Saikosaponin A and D were purified and obtained from the crude B. falcatum L. extract using preparative high performance liquid chromatography technique. Saikosaponin A and D were converted into saikogenin F via prosaikogenin F, and saikogenin G via prosaikogenin G using enzyme transformation with high β-glycosidase activity. The two saikogenin and two prosaikogenin compounds were purified using a silica column to obtain 78.1, 62.4, 8.3, and 7.5 mg of prosaikogenin F, prosaikogenin G, saikogenin F, and saikogenin G, respectively, each with 98% purity. The anti-cancer effect of the six highly purified saikosaponins was investigated in the human colon cancer cell line HCT 116. The results suggested that saikosaponins and prosaikogenins markedly inhibit the growth of the cancer cell line. Thus, this enzymatic technology could significantly improve the production of saponin metabolites of B. falcatum L. Full article

Phosphorus (P) deficiency affects plant yield and quality, yet at the same time, excessive phosphorus application does not necessarily promote the growth of plants. How to maintain a balance between biomass accumulation and phosphorus application is a problem. Therefore, the purpose of this research was to explore the relationship between yield and quality of Bupleurum and phosphorus fertilization, based on three phosphorus fertilization levels (20 kg∙ha⁻¹; 10 kg∙ha⁻¹; and 0 kg∙ha⁻¹). We adopted gas chromatography-mass spectrometry to assess the response of primary metabolites of different plant tissues (flowers, main shoots, lateral shoots and roots) to phosphorus fertilization. At the same time, high-performance liquid chromatography was used to quantify saikosaponin A and saikosaponin D, the main active ingredients of Bupleurum. Our research showed that low phosphorus level application has a positive impact on the yield and quality of Bupleurum, especially the above-ground parts increasing the fresh weight of flowers and lateral shoots and the length of main shoots, and moreover, increasing the saikosaponins content in all above-ground parts while decreasing the content in roots which show no significance increase in fresh weight and length. However, high phosphorus level showed a negative impact as it decreases the saikosaponins content significantly in flowers and roots. Furthermore, phosphorus application changed the proportion of saikosaponins, promoting the content of saikosaponin A and inhibiting the content of saikosaponin D in most organs of Bupleurum. Therefore, we can say that high phosphorus application is not preferable to the yield and quality of Bupleurum. To identify the metabolic pathways and special key metabolites, a total of 73 metabolites were discovered, and four differential metabolites—ether, glycerol, chlorogenic and L-rhamnose—were considered to be the key metabolites of Bupleurum’s response to phosphorus fertilization. Furthermore, Bupleurum’s response to phosphorus fertilization was mainly related to metabolic pathways, such as starch and sucrose metabolism and galactose metabolism. Under the phosphorus level, the content of sugars, organic acids and their derivatives, polyols and their derivatives and alkyl were upregulated in flowers. Furthermore, the contents of compounds in the main shoot and lateral shoots showed the same upward trend, except glycosides and polyols and their derivatives. Full article

Bupleurum (Apiaceae) is widely used in traditional Chinese medicine to treat inflammatory and infectious diseases. Although roots are the only used parts in China, other countries use the whole plant. The yield and quality of Bupleurum depend mainly on fertilizers, especially nitrogen. The current study aimed to assess the relationship between the nitrogen fertilization level and the quality and metabolomic response of different parts (flowers, main shoots, lateral shoots and roots) of Bupleurum to three nitrogen fertilization levels (control group: 0 kg·ha⁻¹; low-nitrogen group: 55 kg·ha⁻¹; high-nitrogen group: 110 kg·ha⁻¹). The results showed that a high nitrogen level increases Bupleurum yield and quality parameters only in aerial parts, especially flowers, but has no significant effect on roots. The HPLC method was exploited for simultaneous quantification of three saikosaponins (A, C and D), which are the main bioactive components in the plant. It was found that the total content of saikosaponins decreased with high nitrogen fertilization in roots but significantly increased in flowers. Moreover, nitrogen fertilizer promoted the content of saikosaponin A but inhibited saikosaponins C and saikosaponins D in most parts of the plant. To study the response of primary metabolites, we adopted gas chromatography–mass spectrometry (GC−MS) analysis; 84 metabolites were identified that were mostly up-regulated with a high nitrogen level in flowers but down-regulated in roots. Four differential metabolites—D-fructose, lactose, ether and glycerol—were recognized as key metabolites in Bupleurum under nitrogen fertilization. Meanwhile, The Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment results explained that the impact of nitrogen fertilization on Bupleurum was attributed to the C-metabolism, N-metabolism, and lipids metabolism. This research put forward new insights into potential mechanisms and the relationship between the quality and yield of Bupleurum and nitrogen fertilization. Full article

Obesity is a lipid metabolism disorder caused by genetic, medicinal, nutritional, and other environmental factors. It is characterized by a complex condition of excess lipid accumulation in adipocytes. Adipogenesis is a differentiation process that converts preadipocytes into mature adipocytes and contributes to excessive fat deposition. Saikosaponin A (SSA) and saikosaponin D (SSD) are triterpenoid saponins separated from the root of the Bupleurum chinensis, which has long been used to treat inflammation, fever, and liver diseases. However, the effects of these constituents on lipid accumulation and obesity are poorly understood. We investigated the anti-obesity effects of SSA and SSD in mouse 3T3-L1 adipocytes. The MTT assay was performed to measure cell viability, and Oil Red O staining was conducted to determine lipid accumulation. Various adipogenic transcription factors were evaluated at the protein and mRNA levels by Western blot assay and quantitative reverse transcription polymerase chain reaction (qRT-PCR). Here, we showed that SSA and SSD significantly inhibited lipid accumulation without affecting cell viability within the range of the tested concentrations (0.938–15 µM). SSA and SSD also dose-dependently suppressed the expression of peroxisome proliferator-activated receptor gamma (PPARγ), CCAAT/enhancer binding protein alpha (C/EBPα), sterol regulatory element binding protein-1c (SREBP-1c), and adiponectin. Furthermore, the decrease of these transcriptional factors resulted in the repressed expression of several lipogenic genes including fatty acid binding protein (FABP4), fatty acid synthase (FAS), and lipoprotein lipase (LPL). In addition, SSA and SSD enhanced the phosphorylation of adenosine monophosphate-activated protein kinase (AMPK) and its substrate, acetyl-CoA carboxylase (ACC), and inhibited the phosphorylation of extracellular-regulated kinase 1/2 (ERK1/2) and p38, but not c-Jun-N-terminal kinase (JNK). These results suggest that SSA and SSD inhibit adipogenesis through the AMPK or mitogen-activated protein kinase (MAPK) pathways in the early stages of adipocyte differentiation. This is the first study on the anti-adipogenic effects of SSA and SSD, and further research in animals and humans is necessary to confirm the potential of saikosaponins as therapeutic agents for obesity. Full article

Liver disorders are a major health concern. Saikosaponin-d (SSd) is an effective active ingredient extracted from Bupleurum falcatum, a traditional Chinese medicinal plant, with anti-inflammatory and antioxidant properties. However, its hepatoprotective properties and underlying mechanisms are unknown. We investigated the effects and underlying mechanisms of SSd treatment for thioacetamide (TAA)-induced liver injury and high-fat-diet (HFD)-induced non-alcoholic fatty liver disease (NAFLD) in male C57BL/6 mice. The SSd group showed significantly higher food intake, body weight, and hepatic antioxidative enzymes (catalase (CAT), glutathione peroxidase (GPx), and superoxide dismutase (SOD)) and lower hepatic cyclooxygenase-2 (COX-2), serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), interleukin (IL)-1β, tumor necrosis factor (TNF)-α, and fibroblast growth factor-21 (FGF21) compared with controls, as well as reduced expression of inflammation-related genes (nuclear factor kappa B (NF-κB) and inducible nitric oxide synthase (iNOS)) messenger RNA (mRNA). In NAFLD mice, SSd reduced serum ALT, AST, triglycerides, fatty acid–binding protein 4 (FABP4) and sterol regulatory element–binding protein 1 (SREBP1) mRNA, and endoplasmic reticulum (ER)-stress-related proteins (phosphorylated eukaryotic initiation factor 2α subunit (p-eIF2α), activating transcription factor 4 (ATF4), and C/EBP homologous protein (CHOP). SSd has a hepatoprotective effect in liver injury by suppressing inflammatory responses and acting as an antioxidant. Full article

Insamyangpye decoction (ISYPD) is an oriental herbal prescription used in Korea to treat lung-related diseases such as chronic obstructive pulmonary disease. ISYPD is a complex prescription consisting of 13 herbal medicines, and ISYPD sample was obtained by adding 50 L of distilled water to a mixture (5 kg) of 13 herbal medicines, extracting at 100 °C for 2 h using an electric extractor, and freeze-drying. In this study, an accurate and sensitive liquid chromatography tandem mass spectrometry (LC–MS/MS) method based on multiple reaction monitoring (MRM) was developed and verified for quality assessment of ISYPD using 10 marker components: mulberroside A (1), amygdalin (2), liquiritin apioside (3), naringin (4), poncirin (5), platycodin D (6), ginsenoside Rb1 (7), glycyrrhizin (8), saikosaponin A (9), and schizandrin (10). These marker compounds were separated using an Acquity UPLC BEH C₁₈ column (2.1 mm × 50 mm, 1.7 μm) maintained at 30 °C with a mobile phase elution gradient of acetonitrile in distilled water, both containing 0.1% (v/v) trifluoroacetic acid. Marker components were quantified using the LC–MS/MS MRM method developed and validated, and found at 0.09–7.47 mg/g. Full article

Saikosaponin A (SSa) and D (SSd) are typical oleanane-type saponins featuring a unique 13,28-epoxy-ether moiety at D ring of the aglycones, which exhibit a wide range of biological and pharmacological activities. Herein, we report the first synthesis of saikosaponin A/D (1–2) and their natural congeners, including prosaikosaponin F (3), G (4), saikosaponin Y (5), prosaikogenin (6), and clinoposaponin I (7). The present synthesis features ready preparation of the aglycones of high oxidation state from oleanolic acid, regioselective glycosylation to construct the β-(1→3)-linked disaccharide fragment, and efficient gold(I)-catalyzed glycosylation to install the glycans on to the aglycones. Full article