Gynura procumbens aqueous extract alleviates nonalcoholic steatohepatitis through CFLAR-JNK pathway in vivo and in vitro Publication date: Available online 1 October 2019 Source: Chinese Herbal Medicines Author(s): Ya-yun Liu, Jiao-jiao You, Wei Xu, Ting Zhai, Chun-yuan Du, Yong Chen, Feng-mei Han Abstract Objective The present work was to investigate the protective effects of the aqueous extract of Gynura procumbens (GPAE) against nonalcoholic steatohepatitis (NASH) in mice and NCTC-1469 cells. Methods C57BL/6J mice were fed with methionine and choline-deficient (MCD) diet and administered simultaneously with GPAE (500 and 1000 mg/kg/d, respectively) by gavage for six weeks. The biomarkers of NASH in serum and liver were determined. NCTC-1469 cells were pretreated with 0.25 mmol/L palmitic acid (PA) plus 0.5 mmol/L oleic acid (OA) for 24 h or treated with adenovirus expressing short-hairpin RNA against CFLAR (Ad-shCFLAR) for 24 h and then treated with GPAE (80 and 160 µg/mL, respectively) for 24 h, and the content of cellular biomarkers of NASH was detected. Results In mice treated with MCD, GPAE could decrease the levels of serum ALT, AST, the content of hepatic TG, TC and MDA, repress the activities and protein expression of CYP2E1 and CYP4A and the phosphorylation of JNK, increase the activities of HO-1, CAT and GSH-Px, up-regulate the mRNA expression of PPARα, FABP5, CPT1α, ACOX, SCD-1, mGPAT, MTTP and the protein expression of CFLAR and NRF2. In NCTC-1469 cells treated with PA and OA, GPAE could decrease the content of cellular TG and ROS, promote the uptake of 2-NBDG, up-regulate the protein expression of CFLAR and NRF2. In NCTC-1469 cells treated with Ad-shCFLAR, GPAE up-regulated the mRNA and protein expression of CFLAR, down-regulated the phosphorylation of JNK, and increased the protein expression of NRF2 and pIRS1. Conclusion These results indicated that the activation on CFLAR-JNK pathway might be the main anti-NASH mechanism of GPAE, which on the one hand promote the β-oxidation and efflux of fatty acids in liver, and finally reduce hepatic lipid accumulation, on the other hand increase the activities of anti-oxidant enzymes and inhibit the activities of ROS generation enzymes by activating NRF2, and therefore attenuates hepatic oxidative stress damage.

Bioactivity of methanolic extract of Brassica juncea in animal model of diabetes mellitus Publication date: Available online 26 September 2019 Source: Chinese Herbal Medicines Author(s): Anuj Kumar, Akhilesh Kumar Rana, Amit Singh, Alok Singh Abstract Objective To study the bioactivity of methanolic extract of Brassica juncea on animal model of diabetes mellitus along with its effect on diabetic and metabolic parameters. Methods Diabetes mellitus was induced in rats by injecting streptozotocin (60 mg/kg) intraperitonealy. Blood glucose was measured on day 3 by GOD-POD method to confirm the diabetes mellitus. Rats having fasting blood glucose > 250 mg/dL were further selected for study and they were divided into four groups, control, control + streptozotocin, streptozotocin + metformin (75 mg/kg) and streptozotocin+ extract of B. juncea (450 mg/kg). Each group consisted of six rats of either sex. Metformin and experimental extract were administered for 21 d. Triglyceride, cholesterol level were measured on day 21 by commercially available kit. Blood glucose was measured on days 7 and 21. Anti-oxidant potential was assessed by estimating extent of lipid peroxidation (LPO) by malondialdehyde (MDA), nitric oxide (NO), superoxide dismutase (SOD) and glutathione (GSH) in liver, kidney, pancreas, muscle tissues on day 21. Unpaired and paired student's t-test was applied for statistical analysis. Results The extract of B. juncea showed significant decrease in blood glucose level on day 21. The treatment group showed significant difference in oxidative stress by increasing SOD and GSH and decreasing LPO and NO activity on day 21. The treatment did not show statistically significant difference of cholesterol, and triglycerides level on day 21. Conclusion The study showed anti-hyperglycemic and anti-oxidative properties of methanolic extract of B. juncea.

In vivo investigation of antimicrobial effects of cinnamaldehyde using immunosuppressed ICR mice with invasive pulmonary aspergillosis Publication date: Available online 25 September 2019 Source: Chinese Herbal Medicines Author(s): Xiao-jun Liu, Jing Luo, Jie-hua Deng, Ji-hong Li, Gang-sheng Wang Abstract Objective Invasive pulmonary Aspergillus infection has the characteristics of high morbidity, difficult to be treated, poor prognosis and high mortality. This study aims to investigate the effects of cinnamaldehyde on 1,3-β-D-glucans in the pulmonary Aspergillus fumigatus cell wall to provide a basis for developing novel antifungal drugs. Methods Immunosuppressed ICR mice were intranasally inoculated with 50 µL of A. fumigatus suspension (1 × 107 CFU/mL) and then separated into two groups, for the experimental group cinnamaldehyde was orally administered at 240 mg/kg/d consecutively for 14 d. While for the control group, voriconazole was used to treat the fungus infection. Pulmonary tissues were then extracted for 1,3-β-D-glucans assay and electron microscopy. Results The concentration of 1,3-β-D-glucans was significantly different between the cinnamaldehyde and voriconazole groups, which was (1160.89 ± 364.96) pg/mL and (3885.94 ± 845.45) pg/mL, respectively (P < 0.01). Electron microscopy showed that 2−3 outer layers (1,3-β-D-glucan layer) of A. fumigatus cell wall were damaged and fell off, resulting in serious defect of the cell wall, but the cell membrane was clear and intact. Conclusion Cinnamaldehyde has a significant influence on the integrity of 1,3-β-D-glucans in the pulmonary A. fumigatus cell wall, but the cell membrane is unaffected, suggesting that cinnamaldehyde has unique antifungal properties depending on its action against the 1,3-β-D-glucans on the pulmonary A. fumigatus cell wall.

New progress of interdisciplinary research between network toxicology, quality markers and TCM network pharmacology Publication date: Available online 24 September 2019 Source: Chinese Herbal Medicines Author(s): Shao Li, Qing-yang Ding

A phytochemical study on Dichocarpum auriculatum, an endangered medicinal plant peculiar to China Publication date: Available online 23 September 2019 Source: Chinese Herbal Medicines Author(s): Pei Li, Shuang-shuang Liu, Qing Liu, Jei Shen, Chun-nian He, Pei-gen Xiao ABSTRACT Objective Dichocarpum auriculatum, an endangered perennial herb, is endemic to China and has been used as folk medicines for the treatment of cough, hepatitis, scrofula, and epilepsy. However, there is no phytochemical report on this herbal so far. For the resource development and protective importance of this endangered medicinal plant, a phytochemical study was undertaken. Methods The chemical constituents were purified by silica gel column, Sephadex LH-20 column, and semi-preparative reversed phase HPLC. NMR and MS spectra were used for structural identification. Results Thirteen compounds were isolated from D. auriculatum. Their structures were characterized as jatrorrhizine (1), berberine (2), steponine (3), magnoflorine (4), coclauril (5), menisdaurin (6), menisdaurilide (7), aquilegiolide (8), (6R, 9S)-3-oxo-α-ionol-β-D-glucopyranoside (9), blumenol C glucoside (10), palmitic acid (11), dibutylphthalate (12), and auriculatum A (13). Conclusion Compound 13 is a new diester terephthalate derivative. All the compounds are obtained from the genus Dichocarpum for the first time, and compounds 9 and 10 have potential chemotaxonomic significance to the genus Dichocarpum.

Synergistic effect of α-mangostin on antibacterial activity of tetracycline, erythromycin, and clindamycin against acne involved bacteria Publication date: Available online 21 September 2019 Source: Chinese Herbal Medicines Author(s): Md Iftekhar Ahmad, James E Keach, Tapan Behl, Pharkphoom Panichayupakaranant Abstract Objective To evaluate the synergistic effect of α-mangostin with tetracycline, erythromycin, and clindamycin against bacteria involved in acne production. Methods A broth microdilution method was used to determine the minimum inhibitory concentration (MIC) of α-mangostin and a range of antibiotics. Synergistic effects on antibacterial activity were determined based on their own MIC, and then using a checkerboard method and a time-kill assay at 37 °C for 24 h. Results α-Mangostin exhibited antibacterial activity against Propionibacterium acnes, Staphylococcus aureus, S. epidermidis and S. pyogenes with MIC values of 0.78, 3.13, 0.78, and 6.25 µg/mL, respectively. The results of the checkerboard assay showed that α-mangostin produced synergistic effects with tetracycline, erythromycin, and clindamycin against all tested bacteria, with a fractional inhibitory concentration index (FICI) between 0.09 and 0.32. Moreover, time-kill curve data indicated that α-mangostin increased the antibacterial activity of tetracycline, erythromycin, and clindamycin. Conclusion These findings suggested that α-mangostin may be used to enhance the antibacterial activity of some antibiotics against bacteria involved in acne production.

Monosaccharide analysis and fingerprinting identification of polysaccharides from Poria cocos and Polyporus umbellatus by HPLC combined with chemometrics methods Publication date: Available online 17 September 2019 Source: Chinese Herbal Medicines Author(s): Jie Liu, Jing Zhou, Qian-qian Zhang, Min-hang Zhu, Mo-li Hua, Yun-hui Xu Abstract Objective Poria cocos and Polyporus umbellatus are similar medicinal fungi in traditional Chinese medicines. A method for fingerprint analysis of monosaccharide composition of polysaccharides by HPLC combined with chemometrics methods has been developed for characterization and discrimination of them in this research. Methods The polysaccharides were extracted by decocting in water, and then completely hydrolyzed with hydrochloride. Monosaccharides in the hydrolyzates were derivatized with 1-phenyl-3-methyl-5-pyrazolone (PMP) for HPLC analysis. More than 20 batches of P. cocos and P. umbellatus from different regions were analyzed. Results The fingerprints of P. cocos showed five common characteristic peaks, which were identified by comparing with the reference substances. The five peaks corresponded to the derivatives of mannose, ribose, glucose, galactose, and fucose. At the same time, the fingerprints of P. umbellatus showed eight common characteristic peaks, of which seven were identified as the derivatives of mannose, ribose, rhamnose, glucose, galactose, xylose, and fucose. Moreover, the similarity of their fingerprints was respectively calculated by the Similarity Evaluation System for Chromatographic Fingerprint of TCM published by China Pharmacopoeia Committee (Version 2004A). And the data were further processed by hierarchical cluster analysis (HCA) and principal component analysis (PCA). The similarity evaluation and HCA indicated that there were no significant difference in P. cocos or P. umbellatus samples from different geographical regions, but PCA was performed to characterize the difference in monosaccharide constituents between P. cocos and P. umbellatus, and linear discriminant analysis (LDA) showed the overall correct classification rate was 100%. Conclusion The fingerprint analysis method of monosaccharide composition of water-soluble polysaccharides can distinguish P. cocos and P. umbellatus, and can be applied for the authentication or quality control for P. cocos and P. umbellatus.

In vitro anti-Helicobacter pylori activity of aqueous extract from Persian Oak testa Publication date: Available online 16 September 2019 Source: Chinese Herbal Medicines Author(s): Asghar Sharifi, Mohsen Azizi, Parastoo Moradi-Choghakabodi, Shapour Aghaei, Arsalan Azizi Abstract Objective Growing problem of antibiotic resistance in Helicobacter pylori, as a common cause of chronic gastritis and even stomach cancer, demands searching for novel candidates of herbal sources. This study is aimed at assessing the antimicrobial activity of aqueous extract obtained from Quercus brantii var. persica seed coat (Testa) on H. pylori isolated from gastric biopsy specimens. Methods Such specimens were collected from 100 patients presenting with endoscopic gastroduodenal findings. Testa extracts were prepared from Persian Oak forests in the province of Kohgiluyeh and Boyer-Ahmad, IRAN. H. pylori isolates were obtained by a series of standard bacteriology tests and cell culture, then were confirmed by PCR. The activity of testa extracts towards 25 H. pylori isolates was assessed by well diffusion method, microdilution assay, and a disk diffusion assay in vitro. Results were analyzed statistically by one-way ANOVA analysis. Results Aqueous extract of testa demonstrated an antimicrobial activity with zone diameters of inhibition ranged from 0 mm to 40 mm. Its inhibitory activity increased simultaneously with increasing extract concentration. The lowest MIC and MBC were both recorded as 2 µg/mL. Anti-H. pylori activity of testa extract was approximately close to tetracycline and metronidazole and less than amoxicillin. A potent extract of testa possessed significant inhibitory activity (P < 0.05). Conclusion Testa extract is suggested as a natural therapeutic source against the gastric H. pylori infection. However, evaluating the in vivo activity of this extract is necessary too.

Dendrobium orchid polysaccharide extract: Preparation, characterization and in vivo skin hydrating efficacy Publication date: Available online 11 September 2019 Source: Chinese Herbal Medicines Author(s): Mayuree Kanlayavattanakul, Tamonpatch Pawakongbun, Nattaya Lourith Abstract Objective Dendrobium spp., the major globally commercializing tropical orchid, has been continuously used in Chinese medicine. However, preparation and standardization of this therapeutic orchid including its clinical evidence for topical application are sparely to be exploited. Methods Maceration of the white orchid (Dendrobium cv. Khao Sanan) in water was varied on the extraction time. The extraction yields and total polysaccharide content of the extracts were compared. The best extract condition was selected, standardized, and evaluated on safety and skin hydrating efficacy in human volunteers. Results The extraction for 3 h gave the extract with polysaccharide content that significantly (P < 0.001) greater than the other extraction times with the following specification: yield [(35.60 ± 2.51)%], moisture content [(7.65 ± 0.21)%], total polysaccharide, sugar, reducing sugar and ash content [(72.95 ± 2.37)%, (34.38 ± 0.00)%, (16.28 ± 0.00)%, and (0.12 ± 0.00)%], pH (4.42 ± 0.01), viscosity [(15.07 ± 0.12) cps] swelling and water absorption capacities [(10.00 ± 0.00)%, (1.19 ± 0.24) g/g]. This antioxidative polysaccharide caused no skin irritation with a better skin hydrating efficacy than the untreated skin and the benchmark as examined in 22 Thai volunteers. Conclusion White Dendrobium is ready to be supplied as a specialty ingredient with a safe and efficient profile for skin dryness therapy. This innovative application of the identified traditional Chinese medicinal herb flows in the main stream of the consumers’ preferences and demand upon natural derived products.

Chemical constituents from heartwoods of Caesalpinia sappan with antiplatelet aggregation activities Publication date: Available online 10 September 2019 Source: Chinese Herbal Medicines Author(s): Yu Ji, Ya-qiong Zhang, Tong-dan Liu, Meng-yuan Xia, Chun-lin Long, Li Wang, Yue-hu Wang, Yi Kong Abstract Objective To clarify the active constituents of the heartwoods of Caesalpinia sappan, a traditional Chinese medicine with the functions of promoting blood circulation (Huoxue in Chinese) and removing blood stasis (Quyu in Chinese). Methods The chemical constituents were isolated and purified by combination of silica gel and Sephadex LH-20 column chromatography, along with semipreparative HPLC. Their chemical structures were established by multiple spectroscopic methods and comparison with literature data. The in vitro antiplatelet aggregation activities were evaluated using mouse platelet induced by AYPGKF-NH2, a gold agonist of protease-activated receptor 4 (PAR4). Results Two new phenols, methyl 2-(4,4′,5′-trihydroxy-2′-(methoxymethyl) biphenyl-2-yloxy) acetate (1) and 1′-methylcaesalpin J (2), together with 24 known compounds (3–26), were isolated from the heartwoods of C. sappan. Among them, sappanchalcone (16) and brazilin (20) showed inhibitory activities against mouse platelet aggregation with IC50 values of 114.8 µmol/L and 100.8 µmol/L, respectively. Conclusion Antiplatelet compounds from C. sappan targeting at PAR4 are reported for the first time.