Background: Many plants growing in Saudi Arabia are used in folk medicine for treatment of several diseases. Objective: Information of the chemical constituents and biological activities of plants is desirable for the discovery of therapeutic agents and discovering the actual value of folkloric remedies. Materials and Methods: The compounds were isolated and purified using silica gel column chromatography and preparative high-performance liquid chromatography-diode array detector (HPLC-DAD) Method. The alcoholic extracts of these plants were evaluated for biological activities. Results: Isolation and characterization of 1-feruloyl-β-D-glucopyranoside (1) as well as new secondary metabolite tryptophan methyl ester (2) were isolated for the 1^st time from the Horwoodia dicksoniae. The three flavones were isolated from Rumex cyprius identified as isoorientin (3), vitexin (4), and Cynarosid (5). The structures of these compounds were characterized by nuclear magnetic resonance and mass spectrometry analysis and comparing with literature. The compounds were isolated and purified using silica gel column chromatography and preparative HPLC-DAD Method. The alcoholic extracts of these plants were evaluated for antimicrobial activities against two Gram-positive bacteria, two Gram-negative bacteria, and four pathogenic fungi. Both plants showed good activities against Syncephalastrum racemosum and Streptococcus pneumoniae with minimal inhibitory concentrations (MICs) 0.98 and 1.95 μg/mL, respectively. H. dicksoniae showed good activity against Aspergillus fumigates with an MIC 1.95 μg/mL. The two extracts showed also effective free radical scavenging activities in the 1,1-diphenyl-2-picrylhydrazyl assay. H. dicksoniae exhibited remarkable cytotoxic activity against Human breast cancer mammary cancer cells-7, Human liver cancer human hepatoma carcinoma cells-2, and human lung carcinoma (A-549) cell lines. Conclusions: It was suggested that further work should be carried out to isolate, purify, and characterize the active constituents responsible for the activity of these plants. SUMMARY

• New secondary metabolite Tryptophane methyl ester as well as 1-feruloyl-β-D-glucopyranoside were isolated for the first time from the HD.
• Isoorientin, vitexin and Cynarosid were isolated from RC.
• HD exhibited good activity against Aspergillus fumigates with an MIC 1.95 μg mL^-1.
• HD showed significant cytotoxic activity against Human breast cancer (MCF-7), Human liver cancer (HepG-2) and Human lung carcinoma (A-549) cell lines.

Background: Investigation of selected plant extracts on multi-targets related to neurodegeneration, such as monoamine oxidases (MAO), cholinesterase enzymes, and antioxidant activities (AOA) is a useful tool for identification of new scaffolds. Objective: This work investigated biological effects of three Blechnum methanol extracts from Brazil and chemical profile of the most active sample. Materials and Methods: AOA included scavenging of hydroxyl and nitric oxide radicals, also lipid peroxidation inhibition. Enzymatic modulation of Blechnum binervatum, Blechnum brasiliense, and Blechnum occidentale extracts on MAO and cholinesterases was conducted. Moreover, total phenol content was performed with all samples, and high-performance liquid chromatography-diode array detection mass spectrometry HPLC-DAD-MS analysis was carried out with B. brasiliense. Possible toxic effects were evaluated on Wistar rats polymorphonuclear cells (PMN) and human stem cells. Results: B. brasiliense extract presented the highest phenolic amount (9.25 g gallic acid equivalent/100 g extract) and lowest IC₅₀values (112.3 ± 2.61 and 176.1 ± 1.19 μg/mL) against hydroxyl radicals and on lipid peroxidation, respectively, showing strong AO effects. On nitric oxide assay and cholinesterase inhibition, all extracts were considered inactive. MAO-A selective action was evidenced, being B. brasiliense powerful against this enzyme (IC₅₀: 72.7 μg/mL), followed by B. occidentale and B. binervatum (IC₅₀: 130.85 and 165.2 μg/mL). No cytotoxic effects were observed on PMN and human stem cells treated with Blechnum extracts. HPLC-DAD-MS analysis of B. brasiliense allowed the identification of chlorogenic and rosmarinic acids. Conclusion: Our results especially highlight B. brasiliense, with pronounced phenols content and strong effects on selected targets related to neurodegeneration, being characterized as a natural safe source of bioactive hydroxycinnamic acids. SUMMARY

• Blechnum crude extracts showed high phenolic amounts and valuable IC₅₀ values on targets related with neurodegenerative disorders
• Blechnum brasiliense was the most active sample, with strong radical scavenging and lipid peroxidation inhibition, also with monoamine oxidases: A selective modulation
• No cytotoxic effects were observed on polymorphonuclear cells rat cells and human stem cells treated with Blechnum extracts
• High-performance liquid chromatography-diode array detection-mass spectrometry analysis of Blechnum brasiliense allowed the identification of hydroxycinnamic derivatives: Chlorogenic and rosmarinic acids.

Abbreviations used: IC₅₀: half maximal inhibitory concentration; MAO: monoamine oxidase; MAO-A: monoamine oxidase isoform A; MAO-B: monoamine oxidase isoform B; HO^•: hydroxyl radical.

Context: Twigs and leaves of Juniperus sabina L. have been traditionally used as the medicinal herb in China for the treatment of many ailments including rheumatoid arthritis (RA). Aims: To confirm the therapeutic effect of total flavonoids from J. sabina (JSTF) on RA-induced by Complete Freund's Adjuvant (CFA) in rats. Settings and Design: Wistar rats (200 ± 20 g) were immunized by intradermal injection of 0.1 mL of CFA into the right hind metatarsal footpad. JSTF was administered orally at the dose of 125,250 and 500 mg/kg on 14 days after the induction of adjuvant arthritis. Tripterygium glycoside (20 mg/kg) was used as a positive control. Paw swelling, arthritic score, body weight loss, serum cytokines, inflammatory mediators, and histological change were measured. Results: We found that JSTF could ameliorate paw swelling of CFA rats, and significantly inhibit arthritic score (P < 0.05). The overproduction of tumor necrosis factor alpha and interleukin 1beta were remarkably suppressed in the serum of JSTF (125,500 mg/kg) treated rats (P < 0.05). Histopathological studies also showed a marked decrease of synovial inflammatory infiltration and synovial lining hyperplasia in the joints of JSTF-treated animals. Six flavonoids were isolated and from JSTF by various chromatographic methods and identified as follows: Catechin, quercitrin, isoquercitrin, isoscutellarein 7-O-β-D-xylopyranoside, isoscutellarein 7-O-β-D-xylopyranose-(1 → 3)-α-L-rhamnoside, and rutin. Conclusions: These results suggest the potential therapeutically effect of JSTF as an anti-arthritis agent toward CFA-induced arthritis in rats, and verified therapeutic applications of J. sabina on RA in folk medicine. SUMMARY

• Twigs and leaves of Juniperus sabina L. have been traditionally used as the medicinal herb in China for the treatment of rheumatoid arthritis
• JSTF could ameliorate paw swelling of CFA rats, and significantly inhibit arthritic score
• Histopathological studies showed a marked decrease of synovial inflammatory infiltration and synovial lining hyperplasia in the joints of JSTF-reated animals
• Six flavonoids were isolated and from JSTF including: Catechin, quercitrin, isoquercitrin, isoscutellarein 7-O-β-D-xylopyranoside, isoscutellarein 7-O-βD-xylopyranose.(1→3).αL-rhamnoside, and rutin.

Abbreviations used: JSTF: Total flavonoids from Juniperus sabina; CFA: Complete Freund's Adjuvant; TG: Tripterygium glycoside; TNF-α: Tumor necrosis factor alpha; IL-1β: Interleukin 1beta; IL-6: Interleukin 6; H and E: Hematoxylin and eosin.

Background: The central nervous system is easily damaged by oxidative stress due to high oxygen consumption and poor defensive capacity. Hence, multiple studies have demonstrated that inhibiting oxidative stress-induced damage, through an antioxidant-rich diet, might be a reasonable approach to prevent neurodegenerative disease. Objective: In the present study, response surface methodology was utilized to optimize the extraction for neuro-protective constituents of Camellia japonica byproducts. Materials and Methods: Rat pheochromocytoma cells were used to evaluate protective potential of Camellia japonica byproducts. Results: Optimum conditions were 33.84 min, 75.24%, and 75.82°C for time, ethanol concentration and temperature. Further, we demonstrated that major organic acid contents were significantly impacted by the extraction conditions, which may explain varying magnitude of protective potential between fractions. Conclusions: Given the paucity of information in regards to defatted C. japonica seed cake and their health promoting potential, our results herein provide interesting preliminary data for utilization of this byproduct from oil processing in both academic and industrial applications. SUMMARY

• Neuro-protective potential of C. japonica seed cake on cell viability was affected by extraction conditions
• Extraction conditions effectively influenced on active constituents of C. japonica seed cake
• Biological activity of C. japonica seed cake was optimized by the responsive surface methodology.

Abbreviations used: GC-MS: Gas chromatography-mass spectrometer, MTT: 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, PC12 cells: Pheochromocytoma, RSM: Response surface methodology. Eui-Cheol Shin

Background: Gegen (Puerariae Labatae Radix) is one of the important medicines in Traditional Chinese Medicine. The studies showed that Gegen and its preparation had effective actions for atherosclerosis. Objective: Near-infrared (NIR) was used to develop a method for rapid determination of puerarin during percolation and concentration process of Gegen. Materials and Methods: About ten batches of samples were collected with high-performance liquid chromatography analysis values as reference, calibration models are generated by partial least-squares (PLS) regression as linear regression, and artificial neural networks (ANN) as nonlinear regression. Results: The root mean square error of prediction for the PLS and ANN model was 0.0396 and 0.0365 and correlation coefficients (r²) was 97.79% and 98.47%, respectively. Conclusions: The NIR model for the rapid analysis of puerarin can be used for on-line quality control in the percolation and concentration process. SUMMARY

• Near-infrared was used to develop a method for on.line quality control in the percolation and concentration process of Gegen
• Calibration models are generated by partial least.squares.(PLS) regression as linear regression and artificial neural networks.(ANN) as non.linear regression
• The root mean square error of prediction for the PLS and ANN model was 0.0396 and 0.0365 and correlation coefficients.(r²) was 97.79% and 98.47%, respectively.

Abbreviations used: NIR: Near-Infrared Spectroscopy; Gegen: Puerariae Loabatae Radix; TCM: Traditional Chinese Medicine; PLS: Partial least-squares; ANN: Artificial neural networks; RMSEP: Root mean square error of validation; R2: Correlation coefficients; PAT: Process analytical technology; FDA: The Food and Drug Administration; Rcal: Calibration set; RMSECV: Root mean square errors of cross-validation; RPD: Residual predictive deviation; SLS: Straight Line Subtraction; MLP: Multi-Layer Perceptron; MSE: Mean square error. Wan Guangrui

Objective: In order to investigate the antioxidant activities of polysaccharides (BPL-1 and BPL-2), one of the most important functional constituents in Brasenia schreberi was isolated from the external mucilage of B. schreberi (BPL-1) and the plant in vivo (BPL-2). This paper examines the relationship between the content of sulfuric radicals and uronic acid in BPL and the antioxidant activity of BPL. Materials and Methods: The free radicals, 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS+) and 1,1-diphnyl-2-picrylhydrazyl (DPPH-), were used to determine the antioxidant activity of BPL. The Fourier-transform infrared spectroscopy of BPL-1 and BPL-2 revealed typical characteristics of polysaccharides. Results: The two sample types had different contents. This was proved by their different adsorption peak intensities. The IC50 values of BPL-1 (31.189 mg/ml) and BPL-2 (1.863 mg/ml) showed significant DPPH radical scavenging activity. Based on the quantification of ABTS radical scavenging, the IC50 value of BPL-1 (5.460 mg/ml) was higher than that of BPL-2 (0.239 mg/ml). Therefore, in terms of the reducing power, the IC50 value of BPL-1 was too high to determine, and the IC50 value of BPL-2 was found to be 50.557 mg/ml. Hence, the antioxidant activity and total reducing power were high, and they were greater in BPL-2 than in BPL-1. In addition, BPL-2 was found to have more sulfuric radicals and uronic acid than BPL-1. Conclusion: The contents of sulfuric radicals and uronic acid are significantly correlated to the antioxidant activity and reducing power of BPL; the more sulfuric radicals and uronic acid, the more antioxidant activity and reducing power BPL has. SUMMARY

• The water-soluble crude polysaccharides obtained from the external mucilage and the Brasenia schreberi plant in vivo were confirmed to have high contents of sulfuric radicals and uronic acid
• Both BPL-1 and BPL-2 exhibited antioxidative activity and reducing power, and their antioxidative activity gradually improved with increasing concentrations
• The content of sulfuric radicals and uronic acid in BPL-1 and BPL-2 might explain their high antioxidant activity.

Abbreviations used: BPL-1:Polysaccharide were isolated from the external mucilage of B. Schreberi; BPL-2: Polysaccharide were isolated from the plant in vivo of B. schreberi; BPL:Polysaccharide were isolated from B. Schreberi.

Context: Recent studies have demonstrated that baicalin has antihyperglycemic effects by inhibiting lipid peroxidation. Baicalin is low hydrophilic and poorly absorbed after oral administration. Thus, a suitable formulation is highly desired to overcome the disadvantages of baicalin. Objective: The objective of this work was to prepare baicalin-loaded nanostructured lipid carriers (B-NLCs) for enhanced antidiabetic effects. Materials and Methods: B-NLCs were prepared by high-pressure homogenization method using Precirol as the solid lipid and Miglyol as the liquid lipid. The properties of the NLCs, such as particle size, zeta potential (ZP), and drug encapsulation efficiency (EE), were investigated. The morphology of NLCs was observed by transmission electron microscopy. In addition, drug release and antidiabetic activity were also studied. Results: The results revealed that B-NLCs particles were uniformly in the nanosize range and of spherical morphology with a mean size of 92 ± 3.1 nm, a ZP of −31.35 ± 3.08 mV, and an EE of 85.29 ± 3.42%. Baicalin was released from NLCs in a sustained manner. In addition, B-NLCs showed a significantly higher antidiabetic efficacy compared with baicalin. Conclusion: B-NLCs described in this study are well-suited for the delivery of baicalin. SUMMARY

• Currently, herbal medicines have attracted increasing attention as a complementary approach for type 2 diabetes
• Baicalin has antihyperglycemic effects by inhibiting lipid peroxidation
• A suitable formulation is highly desired to overcome the disadvantages (poor solubility and low bioavailability) of baicalin
• Nanostructured lipid carriers could enhance the antidiabetic effects of baicalin.

Abbreviations used: B-NLCs: Baicalin-Loaded Nanostructured Lipid Carriers, B-SUS: Baicalin Water Suspension, EE: Encapsulation Efficiency, FBG: Fasting Blood Glucose, HbAlc: Glycosylated Hemoglobin, HPLC: High-performance Liquid Chromatography; NLCs: Nanostructured Lipid Carriers, PI: Polydispersity Index, SD: Sprague-Dawley, SLNs: Solid lipid nanoparticles, STZ: Streptozotocin, TC: Total cholesterol, TEM: Transmission Electron Microscope, TG: Total Triglyceride, ZP: Zeta Potential.

Background: Thymelaea microphylla Coss. et Dur. (Thymelaeaceae) (TM) is a rare medicinal plant endemic to Algeria. Leaves decoction is used in folk medicine for anticancer, anti-inflammatory, and antidiabetic properties. Objective: Herein, the antioxidant and anti-inflammatory properties of different extracts from leaves and flowers of Algerian TM were evaluated. Materials and Methods: The study was carried out by in vitro cell-free assays (antioxidant/radical properties), ex vivo experiments (inhibition of prostaglandin E2 and thromboxane B2 release in human whole blood) and in vitro experiments on cell systems (cytotoxicity on peripheral blood mononuclear cells, and protective effects on human vein endothelial cells exposed to TNF-α). Results: The acetone TM extract showed significant antioxidant properties and excellent anti-inflammatory and cyclooxygenase-inhibitory activity, together with lack of toxicity on normal human blood cells; furthermore, it was able to protect endothelial cells against dysfunction induced by TNF-α, as shown by decrease in cell death, e-selectin expression and leukocyte adhesion. Conclusion: On these bases, TM leaves and flowers appear to be a good source of bioactive compounds with significant antioxidant and antiinflammatory capability, and potentially effective in prevention and treatment of pathological conditions related to oxidative stress and inflammation, such as endothelial dysfunction. SUMMARY

• Thymelaea microphylla leaves and flowers are a good source of bioactive compounds with significant antioxidant/free radical scavenger and anti-inflammatory activity.
• The acetone extract from leaves and flowers of Algerian Thymelaea microphylla possesses excellent cyclooxygenase-inhibitory activity.
• This extract is able to protect against endothelial dysfunction, an early event in development of atherosclerosis and vascular diseases.

Abbreviations used: TM: Thymelaea microphylla; BCB: Beta-carotene bleaching; AcE: Acetone extract; PGE2: Prostaglandin E2; TxB2: Thromboxane B2; FL: Fluorescein; Cat: Catechin; DPPH: 2,2-diphenyl-1-picrylhydrazyl; ABTS: 2,2'-azinobis-(3-ethyl-benzothiazolin-6-sulfonic acid)+; Que: Quercetin; ORAC: Oxygen radical absorbance capacity; AAPH: 2,2'-azobis (2-methylpropionamidine)dihydrochloride; PMS/NADH: Phenazine methosulfate/nicotinamide adenine dinucleotide; HUVECs: Human umbilical vein endothelial cells. Antonio Speciale

Objective: The purpose of this study was to investigate the potential influences of Socheongryong-tang(SCRT) on the messenger ribonucleic acid (mRNA) and protein expression of cytochrome P450 (CYP450) in vivo. Materials and Methods: SCRT was orally administered to either male or female Sprague-Dawley rats once daily at doses of 0, 1000, 2000, or 5000 mg/kg/day for 13 weeks. The mRNA expression of CYP450s (CYP1A1, 1A2, 2B1/2, 2C11, 2E1, 3A1, 3A2, and 4A1) in liver tissues was measured by reverse transcription polymerase chain reaction. And then, the protein expression of CYP1A1 and CYP2B1/2 in liver tissues was analyzed by the Western blot. Results: We found no significant influence in the mRNA expression of hepatic CYP1A2, 2C11, 2E1, 3A1, 3A2, and 4A1 after repeated administration of SCRT for 13 weeks. By contrast, the mRNA and protein expression of hepatic CYP1A1 was increased by repeated SCRT treatment in male rats, but not in female rats. The mRNA and protein expression of hepatic CYP2B1/2 in both genders was increased by administration of SCRT. Conclusion: A caution is needed when SCRT is co-administered with substrates of CYP2B1/2 for clinical usage. In case of male, an attention is also required when SCRT and drugs metabolized by CYP1A1 are taken together. Our findings provide information regarding the safety and effectiveness of SCRT when combined with conventional drugs. SUMMARY

• Oral administration of Socheongryong-tang for 13 weeks did not affect the mRNA expression of hepatic CYP1A2, 2C11, 2E1, 3A1, 3A2, and 4A1
• In male rats, oral administration of Socheongryong-tang for 13 weeks induced the mRNA and protein expression of hepatic CYP1A1 and CYP2B1/2
• In female rats, oral administration of Socheongryong-tang for 13 weeks induced the mRNA and protein expression of hepatic CYP2B1/2.

Abbreviations used: SCRT: Socheongryong-tang, CYP450: Cytochrome P450, HPLC: High performance liquid chromatography, RT-PCR: Reverse transcription polymerase chain reaction. Soo-Jin Jeong

Background: The aim of this study is to determine the antifatigue active fraction from Abelmoschus esculentus. The in vivo antifatigue effects of ethanol extracts and polysaccharides from A. esculentus fruit have been determined. The polysaccharides of A. esculentus were determined as the best effective fractions of antifatigue effects. Materials and Methods: About 360 Kunming male mice were randomly divided into nine subgroups: normal control subgroup, model subgroup, positive subgroup and the ethanol extracts of A. esculentus with high dose (3.2 g/kg) subgroup, medium dose (1.6 g/kg) subgroup and low dose (0.8 g/kg) subgroup, the polysaccharides of high dose (3.2 g/kg) subgroup, medium dose (1.6 g/kg) subgroup, and the low dose (0.8 g/kg) subgroup. The antifatigue effects of ethanol extracts and polysaccharides form A. esculentus were measured by comparing body weight, food intake, swimming time, liver glycogen, serum urea, blood lactic acid as well as visceral parameter in mice. Results: Compared with the model subgroup, other subgroups significantly prolonged swimming time, and high dose polysaccharides administration was the most effective (P < 0.01). High dose polysaccharides significantly increased liver glycogen, serum lactic acid, and serum urea (P < 0.01) in mice. In contrast with model group, the high dose polysaccharides administration could also significantly elevated the parameters of testicles and epididymis (P < 0.01). The study established that the ethanol extracts and polysaccharides of A. esculentus both have antifatigue effects. Conclusions: The results demonstrated that both the ethanol extracts and polysaccharides of A. esculentus have antifatigue effects. The high dosage polysaccharides have significant antifatigue properties. The results will provide the basis for further development and utilization of this plant. SUMMARY

1. The high dosage polysaccharides have restoration ability on kidney yang deficiency mice.
2. The high dosage polysaccharides have significant effects of relieving body fatigue of mice.
3. The polysaccharide of Abelmoschus esculentus showed better antifatigue effects than the ethanol extracts.

Abbreviations used: A. esculentus: Abelmoschus esculentus, BUN: Blood urine nitrogen, LD: Lactic Acid dehydrogenase, AE: Abelmoschus esculentus ethanol extracts, AP: Abelmoschus esculentus polysaccharides, LAC: Lactic acid content.

Background: Baicalin is a bioactive ingredient extracted from the root of Scutellariae radix, which is used to treat ulcerative colitis (UC). Objective: We investigated the activity of baicalin on lipopolysaccharide-stimulated RAW264.7 cells and 2,4,6-trinitrobenzene sulfonic acid-induced rats, including the attenuation of oxidant stress and apoptosis. Materials and Methods: The severity of colitis was assessed by disease activity index. The activities of catalase (CAT), glutathione peroxidase (GSH-PX), superoxide dismutase (SOD), and the content of malondialdehyde (MDA) were determined by their corresponding kits. The terminal deoxynucleotidyl transferase-mediated dUTP nick end-labeling (TUNEL) was performed to study whether experimental colitis was associated with intestinal epithelial cell (IEC) apoptosis and the effect of baicalin on IEC apoptosis. Western blot analysis and immunocytochemistry assay were applied to determine the protein expressions. The reactive oxygen species (ROS) level in the colon of UC rats treated with baicalin was determined by ROS assay kit. Results: Baicalin remarkably upregulated the activities of CAT, GSH-PX, and SOD and decreased the content of MDA in a dose-dependent manner in vitro and in vivo. The TUNEL-positive cells in rats treated baicalin were remarkably reduced. Both Western blot analysis and immunocytochemistry assay indicated that baicalin significantly decreased the expressions of transforming growth factor beta-1, Bax protein and upregulated the expression of Bcl-2 protein. In addition, the expressions of total and cleaved caspase-3, total and cleaved caspase-9 protein, Fas, and FasL in vitro were downregulated by the treatment with baicalin. Baicalin of different doses reduced the generation of ROS in UC rats. Conclusion: Taken together, these evidences provide scientific basics for the application of baicalin in the treatment of UC and suggest that baicalin exerts its effect via suppression of oxidant stress and apoptosis. SUMMARY

• Baicalin remarkably upregulated the activities of catalase, glutathione peroxidase, and superoxide dismutase and decreased the content of MDA, both in vivo and in vitro
• The terminal deoxynucleotidyl transferase-mediated dUTP nick end-labeling-positive cells in rats treated baicalin remarkably reduced in a concentration-dependent manner
• Western blot analysis and immunocytochemistry assay indicated that baicalin significantly decreased the expressions of transforming growth factor beta-1, Bax protein, and upregulated the expression of Bcl-2 protein
• The expressions of total and cleaved caspase-3, total and cleaved caspase-9 protein, Fas, and FasL in vitro were downregulated by the treatment with baicalin.

Abbreviations used: UC: Ulcerative colitis, LPS: Lipopolysaccharide, TNBS: 2,4,6-trinitrobenzene sulfonic acid, DAI: Disease activity index, CAT: Catalase, GSH-PX: Glutathione peroxidase, SOD: Superoxide dismutase, MDA: Malondialdehyde, TUNEL: Terminal deoxynucleotidyl transferase-mediated dUTP nick end-labeling, ROS: Reactive oxygen species, IEC: Intestinal epithelial cell, SD: Sprague-Dawley, HE: H and E, DNTB: 5,5'-dithiobis-2-nitrobenzoic acid, TBA: Thiobarbituric acid, TBARS: Thiobarbituric acid-reactive substances, S.D: Standard deviation, and PBS: Phosphate-buffered saline.

Objective: Dioscorea nipponica Makino is one of the most common used traditional Chinese drugs which are used to treat gouty arthritis (GA). Nuclear factor-κB (NF-κB) pathway plays an important role during this process. In the present study, we investigated the effects of total saponins from D. nipponica Makino (TDN) on NF-κB pathway in interleukin-1β (IL-1β) induced fibroblast-like synoviocytes (FLS). Materials and Methods: FLS were divided into three groups: Normal group, model group, which was given 10 μg/L IL-1β to induce the proliferation, and TDN group (10 μg/L IL-1β +100 μg/L TDN). 1 h, 24 h, 48 h, and 72 h after treating, immune fluorescence method was used to detect the cell location of NF-κB p65. Electrophoretic mobility shift assay was used to detect the activation of NF-κB p65. Western blot method was used to detect the protein expressions of NF-κB p65, IκBα, and p-IκBα. Results: TDN could inhibit the activation and transfer of NF-κB p65. As time went on, the expression of NF-κB p65 in the cytoplasm was decreased while it was increased in the nucleus. The expression of p-IκBα was increased, whereas the expression of IκBα was not changed. TDN could regulate these abnormal expressions. Conclusion: TDN may treat GA by regulating NF-κB signal pathway. SUMMARY

• TDN could inhibit the transfer of NF-κB p65.
• TDN could inhibit the activation of NF-κB p65.
• TDN could inhibit the expression of p-IκBα

Abbreviations used: TDN: Total saponins from Dioscorea nipponica Makino, GA: Gouty arthritis, FLS: Fibroblast-like synoviocytes, IL-1β: Interleukin-1 beta, IF: Immune fluorescence, EMSA: Electrophoretic mobility shift assay, WB: Western blot.