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Herbal mixture extracts (HME) comprised of Semen Sojae Nigrum, Fructus Cnidii, Radix Glycyrrhizae, and Cornu Cervi. Herein, we employed three mouse models, including hot-plate test, acetic acid (AA)-induced writhing test and AA-induced vascular permeability test, to determine analgesic and anti-inflammatory effects of HME. Results revealed that HME exhibited analgesic effects in hot-plate test and in AA-induced writhing test, as evidenced by increasing the latency to lick paws and decreasing AA-induced writhing counts, respectively. HME also significantly and dose-dependently decreased AA-induced vascular permeability, indicating HME exhibited anti-inflammatory effects. Similar improvement can be observed in aspirin treatment that used as positive control in this study. Most of medicinal effects of Fructus Cnidii are considered to attribute to coumarins, such as osthol (OST) and imperatorin (IMP) with several pharmacological activities. We then used OST and IMP as bioactive components in HME. The content of OST and IMP in HME was 3.57 ± 0.10 mg/g and 1.20 ± 0.02 mg/g, respectively, from three independent batches. Only OST possessed inhibitory effects in three mouse models, suggesting that OST may partially involve in protective effects of HME. These results demonstrated that HME has a potential on anti-analgesic effects and anti-inflammatory actions.

The aim of this study was to investigate and compare the effects of three herbal mixture extracts on obesity induced by high-fat diet (HFD) in rats. The prescriptions— Pericarpium citri reticulatae and Fructus crataegi —were used as matrix components and mixed with Ampelopsis grossedentata , Salvia miltiorrhiza , and epigallocatechin-3-gallate (EGCG) to form T1, T2, and T3 complexes, respectively. Results revealed that HFD feeding significantly increased body weight gain, fat deposition, plasma lipid profiles, hepatic lipid accumulation, and hepatic vacuoles formation, but decreased plasma levels of adiponectin in rats. Only the T1 complex showed the tendency, although not significantly so, for decreased HFD-induced body weight gain. T1 and T3 complexes significantly reduced HFD-induced fat deposition, and plasma levels of triglyceride, total cholesterol, and low-density lipoprotein cholesterol. Only the T1 complex significantly increased HFD-reduced adiponectin levels in plasma, but decreased HFD-increased triglyceride content in liver tissues. All complexes effectively inhibited HFD-induced vacuoles formation. The content of dihydromyricetin, salvianolic acid B, and EGCG in T1, T2, and T3 complexes was 18.25 ± 0.07%, 22.20 ± 0.10%, and 18.86 ± 0.04%, respectively. In summary, we demonstrated that herbal mixture extracts, especially T1 complex, exhibit antiobesity activity in HFD-fed rats.

Dihydromyricetin (DHM)-rich herbal mixture extracts, also called APF complex, comprised of Ampelopsis grossedentata, Pericarpium citri reticulatae, and Fructus crataegi. The content of DHM in APF complex was 362.7 ± 12.5 mg/g. The aims of this study were to investigate the therapeutic effects of APF complex on metabolic syndrome in rats fed a high-fat diet (HFD) and evaluate the subacute toxicity of APF complex in rats. HFD significantly increased body weight gain, fat tissue (epididymal fat, mesenteric fat, and perirenal fat) deposition, body fat index, and hepatic triglyceride (TG) and total cholesterol (TC) accumulation as well as caused abnormal blood biochemical parameters, including TC, TG, low-density lipoprotein-cholesterol (LDL-C), free fatty acid (FFA), and glucose. APF complex has a tendency but not significance to limit HFD-induced body weight gain. APF complex also significantly improved HFD-induced body fat accumulation, as evidenced by decreasing fat tissue deposition and body fat index. In addition, APF complex significantly ameliorated HFD-induced hyperlipidemia and hyperglycemia, as evidenced by reducing levels of blood TG and TC as well as blood glucose and FFA, respectively. Furthermore, APF complex significantly decreased HFD-induced hepatic TG and TC accumulation. In subacute toxicity assessment, APF complex exhibited no toxicological signs, as evidenced by without affecting mortality, food and water consumption, body weight changes, absolute organ weights, hematological system, blood lipids and nutritional status, and electrolyte balance as well as non-toxic to liver and renal function. Overall, APF complex was considered as a non-toxic herbal prescription and could act as adjuvant therapy for metabolic syndrome. Keywords: Dihydromyricetin, Herbal mixture extracts, High-fat diet, Metabolic syndrome, Subacute toxicity

The tyrosinase inhibitory and antioxidant activities of four nicotinic acid derivatives, namely, nicotinamide, methyl nicotinate, nicotinic acid hydroxamate (NAH), N -methyl nicotinic acid hydroxamate (NAH-M), and kojic acid, were studied. The tyrosinase inhibitory activity was found to follow the trend: NAH > kojic acid > NAH-M > methyl nicotinate > nicotinamide. The concentrations of half-inhibition (IC 50 ) of NAH against monophenolase and diphenolase activity were 2 and 1 μM, respectively; the inhibition mode was a mixed-type in the former and an uncompetitive type in the latter. In the antioxidant activity assays, NAH and NAH-M, but not nicotinamide or methyl nicotinate, showed dose-dependent DPPH radical scavenging activity, and their corresponding IC 50 values were 65.81 and 125 μM, respectively. NAH and NAH-M also showed hydroxyl radical scavenging activity and anti-low-density-lipoprotein peroxidation. These results indicate that NAH and NAH-M have the potential to be useful in cosmetics or food processing, and therefore, they should be investigated further.

Free radicals play a critical role in causing hemorheologic abnormality which is highly correlated with cardiovascular disease and stroke. In this study, we established an in vitro model to evaluate the influence of free radical attacks on hemorheological parameters. A well-sealed chamber with hyperbaric oxygen was used to simulate an environment of free radical attacks. Hemorheological parameters, including whole blood viscosity, erythrocyte membrane lipid peroxidation, and erythrocyte deformability, were investigated. We then used the in vitro model to evaluate the anti-free radical effects of some well-known catechin antioxidants, such as epigallocatechin gallate (EGCG), (-)-epicatechin 3-gallate (ECG), and (-)-epigallocatechin (EGC) on abnormal hemorheological parameters induced by hyperbaric oxygen. The results show that an increase in oxygen partial pressure (1.0, 1.5, 2.0 and 2.5 atm) and exposure time (4, 8, 12 and 16 h) resulted in elevated free radical formation and viscosity of whole blood, enhanced lipid peroxidation in erythrocyte membranes, but decreased erythrocyte deformability. In addition, EGCG, ECG, and EGC (0.1, 0.5 and 1.0 μM) effectively ameliorated hemorheologic abnormality and enhanced erythrocyte deformability. Therefore, this study has provided an in vitro hyperbaric oxygen model to rapidly screen or assess the efficacy of functional foods and drugs in the prevention or improvement of hemorheologic abnormality.

Osteoporosis is a reduction in skeletal mass due to an imbalance between bone resorption and bone formation. Bone morphogenetic protein (BMP) plays important roles in osteoblastic differentiation and bone formation. Therefore, components involved in BMP activation are good targets for the development of anti-osteoporosis drugs. In this study, imperatorin and bergapten, two coumarin derivatives, were shown to enhance alkaline phosphatase (ALP) activity, type I collagen synthesis and bone nodule formation in primary cultured osteoblasts. Imperatorin and bergapten increased mRNA levels of BMP-2 using quantitative RT-PCR, whereas the BMP-2 antagonist noggin attenuated the increase of ALP activity induced by imperatorin and bergapten, indicating that BMP-2 expression is required for the action of imperatorin and bergapten in osteoblastic maturation. Both imperatorin and bergapten enhanced the phosphorylation of SMAD (transcription factors activated by TGF-beta) 1/5/8, p38 and extracellular signal-regulated protein (ERK). Pretreatment of osteoblasts with p38 inhibitor (SB203580) or mitogen-activated protein kinase inhibitor (PD98059) or transfected with dominant negative mutant of p38 or ERK antagonized the elevation of BMP-2 expression and ALP activity induced by imperatorin and bergapten. Local administration of imperatorin or bergapten into the metaphysis of the tibia via the implantation of a needle cannula significantly increased the BMP-2 immunostaining and bone volume of secondary spongiosa in tibia. Taken together, our results provide evidence that coumarin derivatives increase BMP-2 expression and enhance bone formation in rat via the p38 and ERK-dependent signaling pathway.

A mycelial mattress of Rhizopus stolonifer obtained from a liquid static culture was utilized for wound dressing and biomedical use. Following screening of mutants induced by UV radiation, F6, exhibiting delayed sporangium formation was selected because its sporangium maturation exhibited a 5-day delay without significant loss of mycelial weight compared to the wild type. The sporangium-free mycelial mattress from the sporangiospore culture of F6 was treated with 1N sodium hydroxide NaOH at 85°C for 2 h to produce a sponge-like membrane named Rhizochitin. The trifluoroacetic acid hydrolysate of Rhizochitin contained 36% N-acetylglucosamine and 53% hexose respectively detected by the Elson-Morgen and phenol-sulfuric acid methods. Results indicated the wound area in rats covered with Rhizochitin was 40% less than that of the uncovered group. Rhizochitin decreased the expression of PDGF in the proliferation stage, increased the expression of TGF-β in the inflammation and proliferation stages, and increased the expression of VEGF in the inflammation and proliferation stages. Rhizochitin inhibited secretion of matrix metalloproteinase-9 on days 1, 7, 9, and 12 and matrix metalloproteinase-2 on days 3, 7, 9, and 12. It was concluded that Rhizochitin has beneficial properties of biocompatible, biodegradable, and wound healing.

LUFFACHITINobtained from the residue of the sponge-like dried fruit ofLuffa aegyptiacawas developed as a weavable skin substitute in this study. A chemical analysis revealed thatLUFFACHITINwas composed of a copolymer containing N-acetyl-glucosamine (~40%) as a major monomer with a filamentary structure as demonstrated by both optical and scanning electron microscopy. The pulp-like white residue of the sponge-like dried fruit ofLuffa aegyptiacaafter treatment was then woven into a thin, porous membrane by filtration and lyophilization as a skin substitute for conducting wound-healing study on rats. The results indicated that theLUFFACHITINmembrane showed significant wound-healing enhancement (25 days to complete healing) compared to cotton gauze (>30 days), but not inferior to that ofSACCHACHITIN. Furthermore, theLUFFACHITINmembrane had advantages of having a high yield, better physical properties for fabrication, and a more attractive appearance.