Molecular properties, structure, neurotrophic and anti-inflammatory activities of cultured secondary metabolites from the cultures of the mushroom Cyathus striatus CBPFE A06.

Two previously undescribed natural cyathane diterpenoids Me-dentifragilin A (1) and Epi-neocyathin O (2), and three known cyathane diterpenoids 3-5, cyathin O, neocyathin P, and cyathin I, were isolated from the rice medium of the Cyathus striatus CBPFE A06. Their structures were established by NMR spectra, and HR-ESI-MS. Compounds 1-5 displayed encouraging neurotrophic activity in PC-12 cells at doses of 5 µM. Meanwhile, 1-5 significantly inhibited LPS-induced NO generation in BV2 cells with the IC50 values ranging from 2.44 ± 0.16 to 4.33 ± 0.32 µM. Western blot analysis showed that 2 and 4 inhibited the expression of genes involved in nitric oxide (NO) production. Molecular docking revealed that five residues of inducible NO synthase (iNOS) are key residues affecting the interaction of 2 and 4 with iNOS. This study enriches the structural diversity of cyathane diterpenes and adds to the evidence that cyathane diterpenes prevent and treat neurodegenerative diseases.

Unprecedented Neoverrucosane and Cyathane Diterpenoids with Anti-Neuroinflammatory Activity from Cultures of the Culinary-Medicinal Mushroom Hericium erinaceus.

The culinary medicinal mushroom Hericium erinaceus holds significant global esteem and has garnered heightened interest within increasingly ageing societies due to its pronounced neuroprotective and anti-neuroinflammatory properties. Within this study, two novel diterpenes, 16-carboxy-13-epi-neoverrucosane (1) and Erinacine L (2); three known xylosyl cyathane diterpenoids, Erinacine A (3), Erinacine C (4), and Erinacine F (5); and four lanostane-type triterpenoids, and three cyclic dipeptides (10-12), in addition to orcinol (13), were isolated from the rice-based cultivation medium of H. erinaceus. Their structures were determined by NMR, HR-ESI-MS, ECD, and calculated NMR. Compound 1 marks a pioneering discovery as the first verrucosane diterpene originating from basidiomycetes, amplifying the scope of fungal natural product chemistry, and the intricate stereochemistry of Compound 5 has been comprehensively assessed for the first time. Compounds 2-5 not only showed encouraging neurotrophic activity in rat adrenal pheochromocytoma PC-12 cells, but also significantly inhibited lipopolysaccharide (LPS)-induced nitric oxide (NO) production in BV2 microglia cell cultures with IC50 values as low as 5.82 ± 0.18 µM. To elucidate the mechanistic underpinnings of these bioactivities, molecular docking simulation was used to analyze and support the interaction of 1 and 2 with inducible NO synthase (iNOS), respectively. In particular, compound 2, a cyathane-xyloside containing an unconventional hemiacetal moiety, is a compelling candidate for the prevention of neurodegenerative diseases. In summation, this investigation contributes substantively to the panorama of fungal diterpene structural diversity, concurrently furnishing additional empirical substantiation for the role of cyathane diterpenes in the amelioration of neurodegenerative afflictions.

Study of pre-treatment of quinoline in aqueous solution using activated carbon made from low-cost agricultural waste (walnut shells) modified with ammonium persulfate.

Activated carbon made from agricultural waste (walnut shells) was investigated as a suitable adsorbent for effectively removing quinoline from industrial wastewater. The activated carbon was treated with phosphoric acid and oxidized by ammonium persulfate and its ability to adsorb pyridine and quinoline in aqueous solution was investigated. Kinetic parameters for the adsorption process were determined through pseudo-first-order and pseudo-second-order kinetic models and intraparticle diffusion models. Equilibrium experiments and adsorption isotherms were analyzed using Langmuir and Freundlich adsorption isotherms. After reaching equilibrium, the activated carbon adsorbed quinoline in preference to pyridine: the equilibrium adsorptions from individual aqueous solutions (200 µL L-1) of quinoline and pyridine were 166.907 mg g-1 and 72.165 mg g-1, respectively. Thermodynamic studies of quinoline adsorption were conducted at different temperatures and indicated that quinoline adsorption was an endothermic and spontaneous process. The column-adsorption of quinoline and pyridine was consistent with the Thomas model and the Yoon-Nelson model. The removal efficiency of quinoline reached more than 97% for a velocity of 6 mL min-1 at the initial adsorption stage.

Antidiabetic activity of Helicteres angustifolia root.

Context The root of Helicteres angustifolia L. (Sterculiaceae) has been used as folk herbal drug to treat cancer, bacterial infections, inflammatory, and flu in China. However, there is no report on its antidiabetic activity. Objective This study evaluates the antidiabetic activity of ethanol extract from H. angustifolia root. Materials and methods The promoting effect of H. angustifolia root ethanol extract (25, 50, and 100 µg/mL) on glucose uptake was evaluated using HepG2 cell, differentiated C2C12 myotubes, and differentiated 3T3-L1 adipocytes. The antidiabetic activity of the extract was assessed in vivo using STZ-induced diabetic rats by orally administration of the extract (200 and 400 mg/kg b.w.) once per day for 28 d. Blood glucose, TG, TC, TP, HDL-C, UA, BUN, AST, ALT, insulin, and HOMA-IR were analyzed. Results The results showed that the extract increased glucose uptake in C2C12 myotubes and 3T3-L1 adipocytes with an IC50 value of 79.95 and 135.96 µg/mL, respectively. And about 12%, 19%, and 10% (p < 0.05) in HepG2 cells when compared with the control at the concentration of 25, 50, and 100 µg/mL, respectively. After 28 days' treatment with the extract, significant reduction was observed in blood glucose, HOMA-IR, TC, TG, UA, BUN, AST, and ALT levels, while the levels of TP and HDL cholesterol increased. Discussion and conclusion These results suggest that H. angustifolia root ethanol extract possess potent antidiabetic activity, which is the first report on antidiabetic activity of this plant.

Evaluation of anti-hyperglycemic effect of Actinidia kolomikta (Maxim. etRur.) Maxim. root extract.

This study aimed to evaluate the anti-hyperglycemic effect of ethanol extract from Actinidia kolomikta (Maxim. etRur.) Maxim. root (AKE).An in vitro evaluation was performed by using rat intestinal α-glucosidase (maltase and sucrase), the key enzymes linked with type 2 diabetes. And an in vivo evaluation was also performed by loading maltose, sucrose, glucose to normal rats. As a result, AKE showed concentration-dependent inhibition effects on rat intestinal maltase and rat intestinal sucrase with IC(50) values of 1.83 and 1.03mg/mL, respectively. In normal rats, after loaded with maltose, sucrose and glucose, administration of AKE significantly reduced postprandial hyperglycemia, which is similar to acarbose used as an anti-diabetic drug. High contents of total phenolics (80.49 ± 0.05mg GAE/g extract) and total flavonoids (430.69 ± 0.91mg RE/g extract) were detected in AKE. In conclusion, AKE possessed anti-hyperglycemic effects and the possible mechanisms were associated with its inhibition on α-glucosidase and the improvement on insulin release and/or insulin sensitivity as well. The anti-hyperglycemic activity possessed by AKE maybe attributable to its high contents of phenolic and flavonoid compounds.

In vitro and in vivo bioactivities of aqueous and ethanol extracts from Helicteres angustifolia L. root.

ETHNOPHARMACOLOGICAL RELEVANCE: Helicteres angustifolia L. (H. angustifolia L.) has been used as traditional medicine in the treatment of cancer in China and Laos. Its medical benefits, however, are still lacking of scientific evidence. Two extracts successively obtained from the root of H. angustifolia L., namely the aqueous root extract (ARE) and the ethanolic root extract (ERE), were used to evaluate the antioxidant and anticancer activities in vitro, and the antitumor efficacy of ARE was examined in vivo, respectively. MATERIALS AND METHODS: ARE and ERE were extracted successively from H. angustifolia L. root with water and ethanol. In vitro antioxidant activities were assessed by radicals scavenging assay, ferrous chelating assay and reducing power assay. In vitro anticancer activities of ARE and ERE were evaluated by their cytotoxic effects against three human cancer cell lines. In addition, the anti-tumor activities of ARE in vivo were assessed by using Ht1080 (human fibrosarcoma cell line Ht1080) tumor xenografts mice. BALB/c nude mice were orally administrated with 200mg/kg/d of ARE. The tumor inhibition rate was determined on day 42 after treatment by using histopathology analysis of the tumor tissues. Furthermore, relevant biochemical parameters in blood were analyzed to monitor their cytotoxic effect. RESULTS: In vitro assays indicated that ARE possessed relatively higher antioxidant and anticancer activities than ERE, with IC50 values of 82.31 ± 9.62, 62.50 ± 6.99, and 127.49 ± 2.9 µg/mL against DLD-1, A549, and HepG2 cells, respectively. In vivo tumor inhibition experiments suggested that ARE possessed significant antitumor efficacy in BALB/c nude mice with a tumor inhibition rate of 49.83 ± 14.38% (p<0.05) and little toxicity was observed to the host. CONCLUSION: ARE from H. angustifolia L. possessed high antioxidant activities is active against liver cancer HepG2, lung cancer A549 and colon cancer DLD-1 cells in vitro and tumor xenografts bearing BALB/c nude mice in vivo. Further studies on elucidation of the mechanisms involved and isolation of the active components may provide more valuable information for the development of functional products from H. angustifolia L. and their application in cancer treatment.

Fucoxanthin induces growth arrest and apoptosis in human bladder cancer T24 cells by up-regulation of p21 and down-regulation of mortalin.

Fucoxanthin, a natural carotenoid, has been reported to have anti-cancer activity in human colon cancer cells, human prostate cancer cells, human leukemia cells, and human epithelial cervical cancer cells. This study was undertaken to evaluate the molecular mechanisms of fucoxanthin against human bladder cancer T24 cell line. MTT analysis results showed that 5 and 10 µM fucoxanthin inhibited the proliferation of T24 cells in a dose- and time-dependent manner accompanied by the growth arrest at G0/G1 phase of cell cycle, which is mediated by the up-regulation of p21, a cyclin-dependent kinase (CDK)-inhibitory protein and the down-regulation of CDK-2, CDK-4, cyclin D1, and cyclin E. In addition, 20 and 40 µM fucoxanthin induced apoptosis of T24 cells by the abrogation of mortalin-p53 complex and the reactivation of nuclear mutant-type p53, which also had tumor suppressor function as wild-type p53. All these results demonstrated that the anti-cancer activity of fucoxanthin on T24 cells was associated with cell cycle arrest at G0/G1 phase by up-regulation of p21 at low doses and apoptosis via decrease in the expression level of mortalin, which is a stress regulator and a member of heat shock protein 70, followed by up-regulation of cleaved caspase-3 at high doses.

Effect of ultrasonic extraction conditions on antioxidative and immunomodulatory activities of a Ganoderma lucidum polysaccharide originated from fermented soybean curd residue.

A crude Ganoderma lucidum polysaccharide (GLPL) was extracted from fermented soybean curd residue by ultrasonic assisted extraction. The optimal extraction conditions were 30 min at 80 °C with 80 W and water to solid ratio of 10, and with this method 115.47 ± 2.95 mg/g of GLPL yield was obtained. Additionally, the antioxidant and immunomodulatory activities of GLPL were investigated. The results showed that GLPL exhibited strong antioxidant effects, which included scavenging activities against DPPH radicals, hydrogen oxide and ABTS radicals with IC50 values of 0.23, 0.48 and 0.69 mg/mL, respectively. For immunomodulatory activities, GLPL was shown to strongly stimulate the proliferation of macrophages (158.02 ± 13.12%), the production of nitric oxide and phagocytosis (21.16 ± 1.65 µM), and, at 40.00 µg/mL, protected macrophage from Doxorubicin (DOX) (0.16 ± 0.003).