Suppression of splenic lymphocyte proliferation by Eucommia ulmoides and genipin.

We investigated the modulation of innate and adaptive immune cell activation by Eucommia ulmoides Oliver extract (EUE) and its ingredient genipin. As an innate immunity indicator, the phagocytic activity of macrophages was determined by measuring engulfed, fluorescently labeled Escherichia coli. As a surrogate marker for the respective activation of cellular and humoral adaptive immunity, concanavalin A (Con A) and lipopolysaccharide (LPS) induction of primary splenocyte proliferation was assayed in in vitro and ex vivo systems. EUE and genipin suppressed the proliferation of primary splenic lymphocytes induced by Con A or LPS, but not macrophage phagocytosis. Oral administration of EUE and genipin to mice decreased splenic lymphocyte proliferation induced by Con A or LPS. These results revealed that E. ulmoides and genipin suppressed cellular and humoral adaptive immunity, and they suggest that E. ulmoides and genipin are promising candidates for immunosuppressive drugs that target diseases that involve excessive activation of adaptive immunity.

Neuroprotective effect of trans-cinnamaldehyde on the 6-hydroxydopamine-induced dopaminergic injury.

The anti-inflammatory and neuroprotective effects of trans-cinnamaldehyde (TCA) were investigated on the inflammatory cells and the dopaminergic degeneration in mice. TCA inhibited the up-regulation of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in the lipopolysaccharide (LPS)-induced inflammatory BV2 microglial cells. To investigate the TCA efficacy on the 6-hydroxydopamine (6-OHDA)-induced dopaminergic degeneration in mice, an intracerebroventricular injection of 6-OHDA was given to the mice, and TCA (30 mg/kg) was intraperitoneally administered. At 7 d after the 6-OHDA injection, 6-OHDA led to a severe loss of tyrosine hydroxylase (TH)-positive dopaminergic neurons in the striatum and substantia nigra (SN). On the other hand, TCA dramatically maintained the number of TH-positive dopaminergic neurons in the striatum and SN regions of the 6-OHDA-treated mice, which indicates that TCA is able to inhibit the 6-OHDA-induced reduction of TH expression in the dopaminergic neurons in the striatum and SN regions. TCA also inhibited the induction of iNOS and COX-2 in the 6-OHDA model, similarly as shown in the LPS-induced inflammatory BV2 microglial cells. These results indicate that TCA has a neuroprotective effect on dopaminergic neurons and that this effect may be associated with the inhibition of inflammatory responses. These findings suggest that TCA may be a therapeutic candidate for the prevention of inflammation-mediated neurodegenerative diseases.

Fabrication of nanosized Al2O3 coated reinforcing particle using electrostatic force.

Titanium carbide (TiC) particles have been coated with aluminum (Al) phase to enhance the compatibility with a metal matrix based on Al, expecting the homogenous dispersion of TiC particles into the matrix. The TiC particles were uniformly dispersed in the aqueous solution of pH 12. The aluminum nitrate as a precursor of Al phase was added to the solution dispersed with the TiC particles. The coating of Al phase onto the TiC particle was driven by the attractive force between the TiC particle with a negative charge and the Al cation in the aqueous solution. The TiC was not oxidized after heat treatment at 500 degrees C, whereas titanium dioxide peaks are detected after heat treatment at 1000 degrees C. In addition, the Al phase coated on the TiC surface was converted to amorphous alumina (Al2O3) and crystallized into alpha-Al2O3 during heat treatment at 500 and 1000 degrees C, respectively. The heat treatment condition such as atmosphere and temperature was an important factor in fabricating the reinforcing particles without degradation such as oxidation and phase transformation. The nano-sized Al2O3 coated reinforcing particles could be well fabricated using electrostatic force in the aqueous solution and by controlling the heat treatment condition.

Microencapsulation of alcohol solvents and high-content actives for efficient transdermal delivery.

The barrier function of the skin in effectively protecting the underlying tissue from the surrounding environment makes it challenging to achieve the efficient transdermal delivery of actives. Herein, we report on alcohol-solvent-encapsulated microcapsules to achieve enhanced skin efficacy. We show that using palm oil as the shell material allows for the microencapsulation of a broad range of alcohol solvents, including ethanol and dipropylene glycol (DPG), as well as on-demand release. Moreover, clinical trials reveal that the high-content actives in microcapsules result in enhanced skin efficacy, and the presence of DPG effectively mediates the transdermal delivery of these actives without causing any skin irritation. We envision that the alcohol-solvent microencapsulation strategy outlined in this work offers new possibilities in cosmetics, food, and drug delivery systems.

Preferential dissolution behaviour of the austenite phase in Fe-27Cr-xC high chromium cast iron.

Preferential dissolution behaviour of the austenite (γ) phase in Fe-27Cr-xC high chromium cast irons (HCCIs) immersed in 0.1 mol dm-3 H2SO4 + 0.05 mol dm-3 HCl was investigated. Potentiodynamic and potentiostatic polarisation revealed that the primary and eutectic γ phases dissolved preferentially at -0.35 and 0.00 VSilver Silverchloride Electrode potential in sat. KCl (SSE), respectively. The immersion of the HCCIs in the solution showed that the dissolution of the primary γ phase dominated for ca. 1 h, while the primary and eutectic γ phases dissolved after ca. 1 h. However, the carbide phases remained undissolved during the dissolution of the γ phases. Furthermore, the corrosion rate of the HCCIs increased with the increasing C content owing to the increase in the contact potential difference values of the γ and carbide phases. The change in electromotive force due to C addition was related to the accelerated corrosion rate of the γ phases.

Passivation of precipitation-hardened UNS N07718 in a shallow sour aqueous solution.

Passivation of precipitation-hardened UNS N07718 in 5 wt% NaCl + 0.5 wt% CH3COOH was investigated. Cyclic potentiodynamic polarisation revealed that the alloy surface was passivated without active-passive transition behaviour. The alloy surface was in a stable passive state during potentiostatic polarisation at 0.5 VSSE for 12 h. Bode and Mott-Schottky plots showed that the passive film became electrically resistive and less defective with n-type semiconductive properties during the polarisation. X-ray photoelectron spectra revealed that Cr- and Fe-enriched hydro/oxide layers were formed on the outer and inner layers of the passive film, respectively. The thickness of the film was almost constant with the increase of the polarisation time. The outer Cr-hydroxide layer changed into a Cr-oxide layer during the polarisation, resulting in a decreased donor density in the passive film. The film's composition change during the polarisation should be related to the corrosion resistance of the alloy in the shallow sour conditions.

Effect of carbon addition on the passivity of hypoeutectic high chromium cast irons.

The effect of adding C on the passivity of hypoeutectic high chromium cast iron (HCCI) was investigated in a pH 8.4 boric-borate buffer solution. The microstructure of HCCI is composed of austenite and carbide phases, whose fractions and chemical compositions are influenced by the amount of C added. Electrochemical and surface analyses revealed that the addition of C in the HCCI increased the defect densities in the n-type and p-type semiconductive oxide layers on the austenite and carbide phases, respectively.

Analysis of saikosaponins in Bupleuri Radix and Caihu-shugan-san using reversed-phase HPLC with pulsed amperometric detection.

A simple and sensitive reversed-phase (RP) HPLC coupled with pulsed amperometric detection (PAD) method was developed to determine the saikosaponin content in Bupleuri Radix or Caihu-shugan-san. Four saikosaponins in Bupleuri Radix and Caihu-shugan-san were extracted with a 6:4 solution of 10 mM sodium phosphate buffer (pH 8)/100% ethanol. Pulsed amperometric detection of carbohydrates in four major saikosaponins was highly sensitive when used with a water-acetonitrile gradient on an alkaline RP column with a post-column delivery system. The limits of detection (S/N=3) and of quantification (S/N=10) of saikosaponins were 0.01-0.02 and 0.03-0.05 µg/mL, respectively. The intra- and inter-day precision (RSDs) were each <9.7% and the average recoveries were 95.0-97.6% in Bupleuri Radix. This method can be used to analyze saikosaponins in Bupleuri Radix and Caihu-shugan-san.

A new polyoxygenated triterpene and two new aeginetic acid quinovosides from the roots of Rehmannia glutinosa.

A new minor polyoxygenated triterpene named glutinolic acid (1) and two new aeginetic acid quinovosides (2, 3) were isolated from the roots of Rehmannia glutinosa LIBOSCH. (Scrophulariaceae) cultivated in Gunwi-gun, Korea. The structures of these compounds were established as 3α,19α,20ß,24,30-pentahydroxyurs-12-en-28-oic acid (1, glutinolic acid), aeginetic acid 5-O-ß-D-quinovoside (2) and aeginetoyl ajugol 5″-O-ß-D-quinovoside (3) on the basis of chemical and spectroscopic evidence.

Biocompatible Wax-Based Microcapsules with Hermetic Sealing for Thermally Triggered Release of Actives.

We present a microfluidic approach that utilizes temperature-responsive and biocompatible palm oil as the shell material in microcapsules to simultaneously achieve hermetic sealing as well as on-demand temperature-triggered release of the encapsulated actives. Unlike common paraffin waxes (e.g., eicosane), microcapsule shells comprising palm oil do not form pores or cracks during freezing and provide a hermetic seal, a nearly perfect seal that separates the core containing the actives from the surrounding environment over a prolonged period of time. This allows effective isolation and protection of complex cargoes such as small molecules with high diffusivity, strong acids, and cosmetic actives including niacinamide. Moreover, the palm oil shell melts above the defined melting temperature, allowing the on-demand release of the encapsulated actives. Furthermore, palm oil is biocompatible, is edible, and leaves a minimal footprint when used in personal care and cosmetic products, offering new perspectives in the design of microcapsules for cosmetic applications.

Identification of antiadipogenic constituents of the rhizomes of Anemarrhena asphodeloides.

Three new phenolic compounds, (E)-4'-demethyl-6-methyleucomin (1), anemarcoumarin A (2), and anemarchalconyn (3), were isolated from an ethyl acetate extract of the rhizomes of Anemarrhena asphodeloides, together with seven known compounds (4-10). The structures of the new compounds (1-3) were determined on the basis of spectroscopic data interpretation. Compound 3 exhibited a potent inhibitory effect against the differentiation of preadipocyte 3T3-L1 cells with an IC50 value of 5.3 microM.

Anti-Alzheimer and antioxidant activities of Coptidis Rhizoma alkaloids.

Coptidis Rhizoma and its isolated alkaloids are reported to possess a variety of activities, including neuroprotective and antioxidant effects. Thus, the anti-Alzheimer and antioxidant effects of six protoberberine alkaloids (berberine, palmatine, jateorrhizine, epiberberine, coptisine, and groenlandicine) and one aporphine alkaloid (magnoflorine) from Coptidis Rhizoma were evaluated via beta-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) assays, along with peroxynitrite (ONOO(-)) scavenging and total reactive oxygen species (ROS) inhibitory assays. Six protoberberine alkaloids exhibited predominant cholinesterases (ChEs) inhibitory effects with IC(50) values ranging between 0.44-1.07 microM for AChE and 3.32-6.84 microM for BChE; only epiberberine (K(i)=10.0) and groenlandicine (K(i)=21.2) exerted good, non-competitive BACE1 inhibitory activities with IC(50) values of 8.55 and 19.68 microM, respectively. In two antioxidant assays, jateorrhizine and groenlandicine exhibited significant ONOO(-) scavenging activities with IC(50) values of 0.78 and 0.84 microM, respectively; coptisine and groenlandicine exhibited moderate total ROS inhibitory activities with IC(50) values of 48.93 and 51.78 microM, respectively. These results indicate that Coptidis Rhizoma alkaloids have a strong potential of inhibition and prevention of Alzheimer's disease (AD) mainly through both ChEs and beta-amyloids pathways, and additionally through antioxidant capacities. In particular, groenlandicine may be a promising anti-AD agent due to its potent inhibitory activity of both ChEs and beta-amyloids formation, as well as marked ONOO(-) scavenging and good ROS inhibitory capacities. As a result, Coptidis Rhizoma and the alkaloids contained therein would clearly have beneficial uses in the development of therapeutic and preventive agents for AD and oxidative stress-related disease.

Cholinesterase and BACE1 inhibitory diterpenoids from Aralia cordata.

Fourteen diterpenes were isolated from the n-hexane fraction of the roots of Aralia cordata (syn. = A. continentalis). Through spectroscopy, the chemical structures were determined as: ent-pimara-8(14),15-diene-19-oic acid (1); ent-kaur-16-en-19-oic-acid (2); 18-nor-ent-pimara-8(14),15-diene-4beta-ol (3); 18-nor-ent-kaur-16-ene-4beta-ol (4); ent-pimara-8(14),15-diene-19-ol (5); 7alpha-hydroxy-ent-pimara-8(14),15-diene-19-oic acid (6); 7beta-hydroxy-ent-pimara-8(14),15-diene-19-oic acid (7); ent-pimar-15-en-8alpha,19-diol (8); 7-oxo-ent-pimara-8(14),15-diene-19-oic acid (9); 16alpha-hydroxy-17-isovaleroyloxy-ent-kauran-19-oic acid (10); 17-hydroxy-ent-kaur-15-en-19-oic acid (11); 15alpha,16alpha-epoxy-17-hydroxy-ent-kauran-19-oic acid (12); 16alpha,17-dihydroxy-ent-kauran-19-oic acid (13); and 16alpha-methoxy-17-hydroxy-ent-kauran-19-oic acid (14). Compounds 4, 5, 8, 12, and 14 were first isolated from this plant. The anti-Alzheimer and antioxidant effects of ent-pimarane-type diterpenes 1, 3, 5, 8, and 9, as well as ent-kaurane-type diterpenes 2, 4, and 10-13, were evaluated via beta-site amyloid precursor protein cleaving enzyme 1 (BACE1), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), peroxynitrite (ONOO(-)), and nitric oxide (NO*) assays. Of the compounds tested, 8 exerted the most effective BChE inhibition with an IC(50) value of 7.58 microM, followed by 3, 13, 11, 2, and 10. Compounds 9-11 exhibited good BACE1 inhibitory activities with IC(50) values of 18.58-24.10 microM. However, 11 showed marginal AChE inhibitory effect, and all compounds tested showed no scavenging activities on ONOO(-) and NO* at a concentration of 100 microM.

Rat growth-hormone release stimulators from fenugreek seeds.

Bioassay-guided fractionation of MeOH extract from fenugreek (Trigonella foenum-graecum L.) seeds resulted in the isolation of two rat growth-hormone release stimulators in vitro, fenugreek saponin I (1) and dioscin (9), along with two new, i.e., 2 and 3, and five known analogues, i.e., 4-8. The structures of the new steroidal saponins, fenugreek saponins I, II, and III (1-3, resp.), were determined as gitogenin 3-O-beta-D-xylopyranosyl-(1-->6)-beta-D-glucopyranoside, sarsasapogenin 3-O-beta-D-xylopyranosyl-(1-->6)-beta-D-glucopyranoside, and gitogenin 3-O-alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranoside, respectively. Fenugreek saponin I (1) and dioscin (9) caused ca. 12.5- and 17.7-fold stimulation of release, respectively, of rat growth hormone from rat pituitary cells, whereas gitogenin (5) showed moderate activity. To our knowledge, this is the first study to demonstrate that steroidal saponins stimulate rat growth-hormone release in rat pituitary cells.

Norditerpenoid and dianthramide glucoside alkaloids from cultivated Aconitum species from korea.

A new norditerpene alkaloid named 8-O-methylhypaconine (1) was isolated along with twelve known alkaloids from the underground parts of an unknown species of Aconitum plant culti vated in Korea. Among the known alkaloids, two dianthramide glucosides, N-(2'-beta-glucopyra nosyl-5'-hydroxysalicyl)-5-hydroxyanthranilic acid methyl ester (2) and N-(2'-beta-glucopyranosyl-5'-hydroxysalicyl)-5-hydroxy-6-methoxyanthranilic acid methyl ester (3), were isolated from Aconitum plants for the first time. The structures were established on the basis of chemical and spectroscopic methods.

Effect of processing method on platycodin D content in Platycodon grandiflorum roots.

Platycodon grandiflorum root is a traditional medicine and food material rich in triterpenoid saponins. Its major constituent, platycodin D (PD), is known to have various pharmacological properties, but processing methods may influence the PD content. In this study, a fully validated HPLC-ELSD method was developed for the quantification of PD in various states of 73 P. grandiflorum root samples from East Asia, and it exhibited a marked variation of the content. Furthermore, the effects of processing procedures such as peeling and drying temperature on the PD content were investigated using UPLC-ELSD analysis, and as a result, a significant influence of processing methods such as peeling and heating of samples on the content was confirmed. Specifically, unpeeled samples that were dried at 40 °C showed the greatest PD content. The obtained results could facilitate the reliable standardization of P. grandiflorum for precise authentication and efficacious applications.

High performance liquid chromatographic analysis of isoflavones in medicinal herbs.

Phytoestrogens have been used as a food supplement to prevent osteoporosis. The isoflavones in the phytoestrogens are daidzein, genistein and formononetin which are present in various herbs. This study examined the quantity of isoflavones in medicinal herbs, which can be used as a phytoestrogen supplement; soybean. These isoflavones were quantified using high performance liquid chromatography (HPLC) with a UV/VIS detector. The concentration of daidzein in Puerariae Radix was 10,436.16 +/- 2,143.83 mg/kg of the dried herb, which was much higher than that extracted from soybeans, 341.47 +/- 18.96 mg/kg. The amount of genistein in Sophorae flavescentis Radix (336.09 +/- 50.89 mg/kg) was approximately 11 times higher than that extracted from soybean (30.03 +/- 7.17 mg/kg). The level of formononetin in Dalbergiae odoriferae Lignum, 2,189.14 +/- 136.46 mg/kg, was the highest among the herbs tested. The total isoflavone content of Puerariae Radix was approximately 30 times higher than that extracted from soybean. Therefore, plants from the family Leguminosae, particularly Puerariae Radix, can be a good source of phytoestrogens.

Prevention of epimerization and quantitative determination of amygdalin in Armeniacae Semen with Schizandrae Fructus solution.

Armeniacae Semen not only contains amygdalin, but emulsin also, which is an enzyme that hydrolyzes amygdalin. The extraction yield of amygdalin from Armeniacae Semen was low, due to the presence of emulsin, when extracted with water. When Schizandrae Fructus solution was used as the extractant; however, amygdalin was almost completely extracted, regardless of the cutting size, due to the absence of the influence of emulsin. In addition, when the crude powder or small piece forms were used with Schizandrae Fructus solution, on epimerization of the D-amygdalin into neoamygdalin occurred. D-amygdalin and its conversion product, neoamygdalin, were quantitatively analyzed by reverse-phase, high-performance liquid chromatography (HPLC), with an optimized eluent of 10 mM sodium phosphate buffer (pH 2.3), containing 11.5% acetonitrile. The concentration and detector response were linearly correlated over the range 0.05 to 2 mM. The detection limits for both D-amygdalin and neoamygdalin were approximately 5 microM for the amount injected.

Identification of cytoprotective constituents of the flower buds of Tussilago farfara against glucose oxidase-induced oxidative stress in mouse fibroblast NIH3T3 cells and human keratinocyte HaCaT cells.

A new cytoprotective compound, 1-[(4S)-3,4-dihydro-4-hydroxy-2,2-dimethyl-2H-1-benzopyran-6-yl]-ethanone (1) was isolated from the flower buds of Tussilago farfara L. (Compositae), together with eight known compounds, 3,4-dicaffeoyl isoquinic acid (2), trans-cinnamic acid (3), 4-hydroxyacetophenone (4), 4,5-dicaffeoylquinic acid methyl ester (5), 3,5-dicaffeoylquinic acid methyl ester (6), 4-hydroxybenzoic acid (7), isoquercetrin (8), and ligucyperonol (9). Compounds 2-4 were found in this plant for the first time. The isolates 1-9, were tested for their cytoprotective activities against glucose oxidase-induced oxidative stress in mouse fibroblast NIH3T3 cells and human keratinocyte HaCaT cells. Among them, 1 and 3 showed significant cytoprotective activities as determined by MTT assay and lactate dehydrogenase leakage, indicating their possibility as the potent cytoprotective agents. The structure of 1 was determined by spectroscopic data analysis including 1D- and 2D-NMR experiments, and its absolute configuration was elucidated by a circular dichroism.

Quantitative determination of amygdalin epimers from armeniacae semen by liquid chromatography.

D-amygdalin and its conversion product, neoamygdalin, were quantitatively analyzed on reverse-phase, high-performance liquid chromatography with an optimized eluent of 10 mM sodium phosphate buffer (pH 3.1) containing 8.5% acetonitrile. Linearity between concentrations and detector responses was obtained in the range from 0.05 to 0.5 mM. The detection limits for D-amygdalin and neoamygdalin were approximately 5 microM per injected amount. Armeniacae semen contains not only amygdalin but also emlusin, which is an enzyme that hydrolyzes amygdalin. When extracting amygdalin from a whole piece of armeniacae semen in boiling water, there was almost no influence of emulsin; which increased the extraction efficiency. However, conversion of d-amygdalin into neoamygdalin at high temperature was found. In this report, we solved this problem by using 4% citric acid as an extractant. This solution also prevented the extraction process from being affected by emulsin. In addition, the extraction efficiency remained the same as that when methanol was used as an extractant, regardless of the cutting size.