A randomized, double-blind, placebo-controlled crossover clinical trial to evaluate the anti-diabetic effects of Allium hookeri extract in the subjects with prediabetes.

Background: Allium hookeri is widely consumed as a vegetable and herbal medicine in Asia. A. hookeri has been reported anti-inflammatory, anti-obesity, osteoblastic, anti-oxidant, and anti-diabetic effects in animal studies.

Changes in volatile flavor compounds in steam-dried root.

This study was carried out to identify volatile flavor compounds in root (AHR) and steam-dried AHR. The volatile compounds were extracted using a simultaneous steam distillation and extraction (SDE) method and identified by gas chromatography/mass spectrometry (GC/MS) analysis. Forty volatile compounds, present at a concentration of 76.

Allium hookeri root protects oxidative stress-induced inflammatory responses and β-cell damage in pancreas of streptozotocin-induced diabetic rats.

Background: Water extract from the root of Allium hookeri (AH) shows anti-inflammatory, antioxidant, and free radical scavenging effects. In this study, the ameliorating effects of AH on oxidative stress-induced inflammatory response and β-cell damage in the pancreas of streptozotocin (STZ)-induced type 1 diabetic rats were investigated.

Methods: AH (100 mg/kg body weight/day) was orally administered every day for 2 weeks to STZ-induced diabetic rats.

Inhibitory activities of anthraquinones from Rubia akane on phosphatase regenerating liver-3.

The methanolic extract of the roots of Rubia akane (Rubiaceae) was found to show inhibitory activity on phosphatase of regenerating liver-3 (PRL-3). Bioassay-guided fractionation of the methanolic extract resulted in the isolation of two anthraquinone compounds, 2-methyl-1,3,6-trihydroxy-9,10-anthraquinone-3-O-(6'-O-acetyl)-α-rhamnosyl(1→2)-β-glucoside and 2-methyl-1,3,6-trihydroxy-9,10-anthraquinone, as inhibitors on PRL-3. These compounds inhibited PRL-3 in a dose-dependent manner with IC₅₀ values of 5.

Therapeutic effects of Baicalein on atopic dermatitis-like skin lesions of NC/Nga mice induced by dermatophagoides pteronyssinus.

The present study was conducted to investigate the effects of Baicalein (BE), which is hydrolyzed product of Baicalin (BA), on atopic dermatitis (AD). AD was induced in NC/Nga mice by DPE treatment. BE hydrogels treatment reduced the levels of skin severity scores.

Effects of isolated compounds from Catalpa ovata on the T cell-mediated immune responses and proliferation of leukemic cells.

Three compounds were isolated from the ethyl acetate soluble fraction of the methanolic extract of the leaves of Catalpa ovata (Bignoniaceae) through repeated column chromatography. We investigated the effects of these compounds on T cell-mediated responses for tumor surveillance and proliferation in U937, HL60, and Molt-4 leukemia cells. Compounds 1-3 inhibited proliferation of those cells in a dose-dependent manner.

Cytotoxic germacranolide sesquiterpenes from the bark of Magnolia kobus.

A new (3) and three known germacrane-type sesquiterpenoids were isolated from the chloroform-soluble fraction of the methanolic extract of the bark of Magnolia kobus (Magnoliaceae) through repeated silica gel and Sephadex LH-20 column chromatography. Their chemical structures were elucidated as costunolide (1), parthenolide (2), isobisparthenolidine (3), and bisparthenolidine (4) by spectroscopic analysis. Compounds 1-4 exhibited cytotoxicity against human A549, SK-OV-3, SK-MEL-2, and HCT15 tumor cells.

Farnesyl protein transferase inhibitory components of Polygonum multiflorum.

The methanolic extract of the roots of Polygonum multiflorum (Polygonaceae) was found to show inhibitory activity towards farnesyl protein transferase (FPTase). Bioassay-guided fractionation of the methanolic extract resulted in the isolation of two anthraquinone glycosides, as inhibitors of FPTase. These compounds inhibited the FPTase activity in a dose-dependent manner.

The effects of ketorolac tromethamine and baicalein on the levels of inflammatory factors in human synoviocytes.

This study examined the effects of ketorolac tromethamine (KT) and baicalein (BE) on the levels of inflammatory factors in human synoviocytes. The fibroblast-like synoviocytes (FLS) cells were used to determine the possible regulatory effects of KT and BE (KTBE) on the levels of inflammatory factors in FLS cells. In addition, the levels of TNF-alpha, IL-6, and IL-1beta mRNA expression in FLS cells induced by a TNF-alpha and IL-1beta co-treatment were largely inhibited by a KTBE treatment.

Anti-hyperalgesic and anti-inflammatory effects of ketorolac tromethamine gel using pulsed ultrasound in inflamed rats.

The aim of this study was to determine if a ketorolac tromethamine (KT) gel solution could be administered in vivo via phonophoretic transdermal delivery using pulsed ultrasound by examining its anti-hyperalgesic and anti-inflammatory effects in a rat carrageenan inflammation model. 1% carrageenan was injected into the plantar surface of the right hindpaw of a rat, and anti-hyperalgesic and anti-inflammatory effects of KT via phonophoretic transdermal delivery were examined. The changes in the mechanical and thermal hyperalgesia, nociceptive flexor reflex (NFR), as well as the swelling changes were determined.

Prostaglandin E2-mediated dysregulation of proinflammatory cytokine production in pristane-induced lupus mice.

Systemic lupus erythematosus (SLE) is characterized by inflammatory and dysregulatory immune responses including overactive B cells, overproduction of proinflammatory cytokines, and T cell hyperactivity. PGE(2) modulates a variety of immune processes at sites of inflammation, including production of inflammatory cytokines. However, the role of PGE(2) in dysregulatory inflammatory and immune responses in lupus remains unclear.

Cytotoxic components from the dried rhizomes of Zingiber officinale Roscoe.

Five compounds were isolated from the chloroform-soluble fraction of the methanolic extract of the dried rhizomes of Zingiber officinale (Zingiberaceae) through repeated column chromatography. Their chemical structures were elucidated as 4-, 6-, 8-, and 10-gingerols, and 6-shogaol using spectroscopic analysis. Among the five isolated compounds, 6-shogaol exhibited the most potent cytotoxicity against human A549, SK-OV-3, SK-MEL-2, and HCT15 tumor cells.

Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abeta1-42 aggregation for Alzheimer's disease therapeutics.

With the goal of developing Alzheimer's disease therapeutics, we have designed and synthesized new piperidine derivatives having dual action of acetylcholinesterase (AChE) and beta-amyloid peptide (Abeta) aggregation inhibition. For binding with the catalytic site of AChE, an ester with aromatic group was designed, and for the peripheral site, another aromatic group was considered. And for intercalating amyloid-beta oligomerization, long and linear conformation with a lipophilic group was considered.

Anesthetic effects of lidocaine hydrochloride gel using low frequency ultrasound of 0.5 MHz.

Purpose: Low-frequency ultrasound has a significant effect on the transdermal permeation of high molecular weight drugs. However, the rate of permeation in pulsed mode is quite low necessitating considerable time to apply the ultrasound. 0.

A new cytotoxic prenylated chalcone from Sophora flavescens.

We have isolated a new prenylated chalcone from the roots of Sophora flavescens (Leguminosae). We determined that structure of this compound is 7,9,2',4'-tetrahydroxy-8-isopentenyl-5-methoxychalcone (1) on the basis of spectroscopic analysis (1D and 2D NMR data). Compound 1 exhibited potent cytotoxicity against human acute promyelocytic (HL60), mouse lymphocytic (L1210) and human histiocytic (U937) leukemia cells.

Cytotoxic isoquinoline alkaloids from the aerial parts of Corydalis incisa.

Three known isoquinoline alkaloids were isolated from the chloroform-soluble fraction of the methanolic extract of the aerial parts of Corydalis incisa (Papaveraceae) through repeated column chromatography. Their chemical structures were elucidated as corynoline (1), corynoloxine (2) and 6-oxocorynoline (3) using spectroscopic analysis. Compounds 1-3 exhibited cytotoxicity against human A549, SK-OV-3, SK-MEL-2 and HCT15 tumor cells.

Transdermal delivery system of triamcinolone acetonide from a gel using phonophoresis.

Triamcinolone acetonide (TA) is a corticosteroid that is used in the systemic and topical treatment of many inflammatory diseases. In this study, a phonophoretic drug delivery system was designed to enhance the TA permeability and the influence of ultrasound was examined. In order to establish the transdermal delivery system for TA, a hydrophilic carbopol gel containing TA was prepared after adopting phonophoresis.

Guaiane sesquiterpenoids from Torilis japonica and their cytotoxic effects on human cancer cell lines.

A new compound 2 and two known guaiane-type sesquiterpenoids were isolated from the methylene chloride-soluble fraction of the methanolic extract of the fruits of Torilis japonica (Umbelliferae) through repeated silica gel and Sephadex LH-20 column chromatography. Their chemical structures were elucidated as torilin (1), 11-acetoxy-8-angeloyloxy-1beta-hydroxy-4-guaien-3-one (1beta-hydroxytorilin, 2), and 11-acetoxy-8-angeloyloxy-1alpha-hydroxy-4-guaien-3-one (1alpha-hydroxytorilin, 3) by spectroscopic analysis. Compounds 1-3 exhibited cytotoxicity against human A549, SK-OV-3, SK-MEL-2, and HCT15 tumor cells.

Inhibitory activity of 6-O-angeloylprenolin from Centipeda minima on farnesyl protein transferase.

The methanolic extract of the aerial parts of Centipeda minima was found to show inhibitory activity on farnesyl protein transferase (FPTase). Bioassay-guided fractionation of the methanolic extract resulted in the isolation of 6-O-angeloylprenolin, as an inhibitor on FPTase. This compound inhibited FPTase activity in a dose-dependent manner, and the IC50 value of 6-O-angeloylprenolin was 18.

Anti-inflammatory effects by transdermal application of triamcinolone acetonide gel using phonophoresis in rats.

The present study was carried out to determine the feasibility of using gel formulations for the transdermal delivery of triamcinolone acetonide (TA), which is one of the synthetic glucocorticoids, in conjunction with phonophoresis, and to develop the carbopol gels of TA. For this purpose, the anti-inflammatory effects of the gel containing TA after the adoption of ultrasound were evaluated by investigating the in vivo change in the serum creatine phosphokinase (CPK) and histological findings. Following a muscle injury, the serum CPK activity decreased significantly in the TA gel group with phonophoresis, comparing with that in the control group and the commercial gel group given ultrasound.

Acetylcholinesterase inhibitors from the aerial parts of Corydalis speciosa.

In a bioassay-guided search for acetylcholinesterase inhibitors from Korean natural resources, four isoquinoline alkaloids, corynoxidine (1), protopine (2), palmatine (3), and berberine (4) have been isolated from the methanolic extract of the aerial parts of Corydalis speciosa. Structures of these compounds were elucidated on the basis of spectroscopic techniques. These compounds inhibited acetylcholinesterase activity in a dose-dependent manner, and the IC50 values of compounds 1-4 were 89.

Acetylcholinesterase inhibitors from the twigs of Vaccinium oldhami Miquel.

In the course of finding Korean natural products with acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the twigs of Vaccinium oldhami significantly inhibited AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of two compounds, taraxerol (1) and scopoletin (2), as active constituents. These compounds inhibited AChE activity in a dose-dependent manner, and the IC50 values of compounds 1 and 2 were 33.

Acetylcholinesterase inhibitors from the roots of Angelica dahurica.

In the course of finding Korean natural products for acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the roots of Angelica dahurica showed significant inhibitory effects on AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of three furanocoumarins, isoimperatorin (1), imperatorin (2) and oxypeucedanin (3), as active principles. These compounds inhibited AChE activity in a dose-dependent manner, and the IC50 values of compounds 1-3 were 74.

Preparation and evaluation of aceclofenac microemulsion for transdermal delivery system.

To develop novel transdermal formulation for aceclofenac, microemulsion was prepared for increasing its skin permeability. Based on solubility and phase studies, oil and surfactant was selected and composition was determined. Microemulsion was spontaneously prepared by mixing ingredients and the physicochemical properties such was investigated.