Anti-Allergic Effects of the Subcritical Water Extract Powder of in Mouse and Guinea Pig Models.

We evaluated the effects of unripe mandarin orange () extract powder (unripe mandarin extract powder [UMEP]) treated with subcritical water on allergic diseases by using animal models. High performance liquid chromatography (HPLC) analysis revealed that subcritical water is a more effective solvent than alcohol and hot water, as it quickly extracted approximately 90% of the functional compounds narirutin (1) and hesperidin (2) from whole fruits. Repeated oral administration of UMEP significantly reversed the peripheral blood flow decline observed during the promotion of allergies after sensitization with the antigen, hen egg-white lysozyme (HEL).

Effect of polyphenols from on blood stasis syndrome.

In this study, we employed a previously developed assay system to determine whether the flowers and leaves of (; commonly known as "lilac") can prevent blood stasis syndrome, known as in Japanese. This syndrome is considered an important pathology in traditional Chinese and Japanese medicine, and is related to diseases such as peripheral vascular disorders, blood vessel inflammation, and platelet aggregation, whose severities are augmented owing to lipid peroxidation, free radicals, and oxidative stress. The assay system employed in this study monitored the blood flow decrease in the tail vein of mice subjected to sensitization with hen egg white lysozyme.

Allergy-preventive effects of linarinic acid and its tetrahydropyrrolo[2,1-b]quinazoline derivatives isolated from Linaria vulgaris.

Linarinic acid, (-)-1,2,3,9-tetrahydropyrrolo[2,1-b]quinazoline-1-carboxylic acid (4a), was isolated from the ethanol extract of Linaria vulgaris Mill. In our previous study, a series of tetrahydropyrrolo[2,1-b]quinazoline derivatives 4b, 4c, 5a, 5b, 6a and 6b that were structurally related to 4a and evaluated as neuroprotective agents were synthesized. The aim of the present study was to investigate the novel features of these compounds.

Development of an Assay Method to Search for Compounds Inhibiting Stress-Enhanced Allergy.

Stress exacerbates allergic disorders such as atopic dermatitis and asthma. It is also an important factor affecting blood flow (BF). Allergic reactions also affect blood flow.

Allergy-preventive effects of chlorogenic acid and iridoid derivatives from flower buds of Lonicera japonica.

Allergy-preventive activity of flower buds of Lonicera japonica THUNB. was found in the 35% EtOH extract (LJ) using an in vivo assay, The assay system uses monitoring of a decrease in blood flow (BF) in the tail vein of mice subjected to sensitization with hen-egg white lysozyme (HEL). Bioassay-guided fractionation of the 35% EtOH extract led to isolation of chlorogenic acid (1) and three known iridoid derivatives, loganin (2), secoxyloganin (3) and sweroside (4), all of which inhibited the BF decrease.

Preventive effects of the extract of kinka-cha, a folk tea, on a rat model of metabolic syndrome.

Kinka-cha (dried leaf of Camellia nitidissima) is used as a folk tea for detoxication, diuresis and antihypertension. In the present study, we evaluated the extract of kinka-cha on metabolic, vascular and oxidative stress parameters in a model of metabolic syndrome, SHR/NDmcr-cp/cp (SHR/cp) rats that manifest hypertension, obesity, glucose intolerance and hyperlipidemia. Treatment with the extract of kinka-cha alleviated the increase in blood pressure, decrease in tail blood flow and elevated serum oxidative stress marker levels including lipid peroxides, 8-hydroxy-2'-deoxyguanosine, 3-nitrotyrosine and 3-chlorotyrosine.

Uptake of AMP, ADP, and ATP in Escherichia coli W.

The uptake activity ratio for AMP, ADP, and ATP in mutant (T-1) cells of Escherichia coli W, deficient in de novo purine biosynthesis at a point between IMP and 5-aminoimidazole-4-carboxiamide-1-β-D-ribofuranoside (AICAR), was 1:0.43:0.19.

Allergy-preventive effects of the flowers of Impatiens textori.

The allergy-preventive activity of a 35% EtOH extract (IT) of flowers of Impatiens textori MIQ. was demonstrated in a continuing search for allergy-preventive substances from natural sources. The evaluation of its activity used an in vivo assay method for monitoring the blood flow decrease in the tail vein microcirculation of mice subjected to sensitization with hen-egg white lysozyme.

Allergy-preventive effects of Hibiscus mutabilis 'versicolor' and a novel allergy-preventive flavonoid glycoside.

Allergy-preventive activity was demonstrated for the MeOH extract (HM) of the petals of Hibiscus mutabilis L. 'versicolor' MAKINO in a continuing search for allergy-preventive substances from natural sources, using the in vivo assay method. This assay system uses monitoring of a decrease in the blood flow at the tail vein of mice subjected to hen egg-white lysozyme (HEL) sensitization.

Involvement of inducible nitric oxide synthase in blood flow decrease in vein induced by hen-egg white lysozyme.

Our in vivo assay system developed to search for allergy-preventive substances, assesses the blood flow decrease in tail vein microcirculation of mice subjected to sensitization with hen-egg white lysozyme (HEL). The blood flow decrease appears to be regulated by various factors such as nitric oxide (NO), thromboxane (TX) A(2), prostacyclin (PGI(2)) and endothelin (ET)-1 together with cyclooxygenase (COX)-1, COX-2, inducible nitric oxide synthase (iNOS), and constitutive nitric oxide synthase (cNOS). In this study, we examined in detail the roles of iNOS in this assay system using an iNOS knockout (KO) mouse.

Allergy-preventive flavonoids from Xanthorrhoea hastilis.

Allergy-preventive activity was demonstrated for an extract of resins from Xanthorrhoea hastilis R. BR. in a search for allergy-preventive substances from natural sources.

Allergy-preventive phenolic glycosides from Populus sieboldii.

Allergy-preventive activity was demonstrated for an extract of the bark of Populus sieboldii in a continuing search for allergy-preventive substances from natural sources. By bioassay-directed fractionation of this plant bark, two new phenolic glycosides, siebolside A {2-hydroxy-5-[(benzoyloxy)methyl]phenyl (6'-O-acetyl) beta-D-glucopyranoside} (1) and siebolside B {2-hydroxy-5-[(benzoyloxy)methyl]phenyl beta-D-glucopyranoside} (2), were isolated, together with three known compounds, salicin (3), sakuranin (4), and neosakuranin (5). The structures of 1 and 2 were elucidated by spectroscopic methods.

Garcinone B reduces prostaglandin E2 release and NF-kappaB-mediated transcription in C6 rat glioma cells.

In the course of our survey of natural compounds inhibiting prostaglandin E2 release and/or lipopolysaccharide (LPS)-induced transcriptional stimulation via NF-kappaB, a central regulator of inflammatory genes, from natural resources, we found garcinone B, a xanthone from callus tissue culture of Hypericum patulum, as a compound with such pharmacological activities, that is a derivative of gamma-mangostin which potently inhibits COX-1 and COX-2 activities to reduce PGE2 release from C6 rat glioma cells, and inhibits IKK activity to prevent NF-kappaB-dependent COX-2 gene transcription. Garcinone B, to a lesser extent, reduced A23187-induced increase in prostaglandin E2 release than gamma-mangostin and its structurally related compound, patulone, in C6 cells. This compound also prevented LPS-induced stimulation of NF-kappaB-dependent transcription.

Antianaphylactic and antipruritic effects of the flowers of Impatiens textori MIQ.

The anti-anaphylactic and anti-pruritic activities of a 35% EtOH extract (IT) of the flowers of Impatiens textori MIQ. were investigated by in vivo assay. IT and apigenin (1), apigenin 7-glucoside (2) and luteolin (3), principal compounds from IT, inhibited compound 48/80 (COM)-induced by blood pressure (BP) decrease, which was an immunoglobulin (Ig)E-independent anaphylaxis-like response.

Development of an in vivo bioassay method for allergy-preventive substances using hen-egg white lysozyme (HEL)-induced blood flow decrease.

We discovered a phenomenon in which the blood flow in vein microcirculation markedly decreases in response to hen-egg white lysozyme (HEL)-sensitization without any change in blood pressure. Using this blood flow decrease as a guide, we developed an in vivo assay method to search for substances, which can prevent allergies. Antagonists of histamine, serotonin and platelet activating factor (PAF) did not affect the blood flow decrease in response to HEL-sensitization.

Inhibitory effects of xanthones from guttiferae plants on PAF-induced hypotension in mice.

The inhibitory effects of 22 xanthones from three Guttiferae plants (Hypericum patulum, Calophyllum inophyllum and C. austroindium) on exogenous platelet activating factor (PAF)-induced hypotension were examined using a blood pressure monitoring in vivo assay method. Guanandin (2), caloxanthone E (3), 1,3,5,6-tetrahydroxy-2-isoprenylxanthone (8), 6-deoxyjacareubin (11) and patulone (18) showed strong inhibition of PAF-induced hypotension, with inhibitory effects of more than 60 %.

Alpha-mangostin induces Ca2+-ATPase-dependent apoptosis via mitochondrial pathway in PC12 cells.

We investigated the cell death effects of eight xanthones on PC12 rat pheochromocytoma cells. Among these compounds, alpha-mangostin, from the fruit hull of Garcinia mangostana L., had the most potent effect with the EC(50) value of 4 microM.

Effects on blood pressure decrease in response to PAF of Impatiens textori MIQ.

A 35% EtOH extract of flowers of Impatiens textori MIQ. showed an inhibitory effect on blood pressure decrease in response to platelet activating factor (PAF) measured with a blood pressure monitoring system. Bioassay-guided fractionation of the 35% EtOH extract (IT) led to isolation of the flavones apigenin (1) and luteolin (3), which significantly inhibited blood pressure decrease in response to PAF.

Antipruritic effects of the fruits of Chaenomeles sinensis.

A 35% EtOH extract of the fruits of Chaenomeles sinensis, long utilized as a folk medicine for cough, significantly inhibited the pruritogenic agent compound 48/80 (COM)-induced scratching behavior in mice. Antipruritic activity-guided fractionation and purification yielded active quercetin, apigenin, and catechin derivatives, which exhibited significant inhibitory effects on COM-induced scratching behavior. To the best of our knowledge, apigenin (5), apigenin 7-glucronide (6), and apigenin 4'-methoxy-7-glucronide (acacetin 7-glucronide) (7) were isolated from the fruits of C.

Effects of conjugated linoleic acid on anaphylaxis and allergic pruritus.

The effects of conjugated linoleic acid (CLA) against anaphylaxis and allergic pruritus were investigated using a in vivo assay. Inhibitory effects of CLA were observed on the immediate (type 1) hypersensitivity reaction, with CLA significantly suppressing the decrease in blood pressure (BP) and blood flow (BF) induced by the hen egg-white lysozyme (HEL)-anaphylactic reaction in ddY mice. After oral administration, CLA showed antipruritic activity, with significant inhibition of scratching behavior induced by compound 48/80 (COM), a histamine-release agent.

Anti-inflammatory and anti-allergic activities of hydroxylamine and related compounds.

The anti-inflammatory activities of several novel oximes and O-acyl oximes that we synthesized have been reported based on carrageenan-induced rat foot-pad swelling assay and histamine-induced rat vascular permeability assay. A cyclooxygenase (COX)-1 inhibitory effect has also been reported for 4'-piperidinoacetophenone and 4'-morpholinoacetophenone oximes and their O-acyl derivatives. To further search for more effective non-steroidal anti-inflammatory or anti-allergic drugs, 1-hydroxylamino-1-(4'-piperidinophenyl) ethane (P-HA) and 1-hydroxylamino-1-(4'-morpholinophenyl) ethane (M-HA) were synthesized from the corresponding oximes with sodium cyanoborohydride, and N,O-diacetyl hydroxylamines (P-HA-Ac and M-HA-Ac) were prepared from these hydroxylamines using acetyl chloride.

Cyclooxygenase-2 inhibitory 1,4-naphthoquinones from Impatiens balsamina L.

Significant selective cyclooxygenase-2 (COX-2) inhibitory activities were observed for two new 1,4-naphthoquinone sodium salts, sodium 3-hydroxide-2[[sodium 3-hydroxide-1,4-dioxo(2-naphthyl)]ethyl]naphthalene-1,4-dione (impatienolate) (1) and sodium 2-hydroxide-3-(2-hydroxyethyl)naphthalene-1,4-dione (balsaminolate) (2), which were isolated from the corolla of Impatiens balsamina L. (Balsaminaceae). Their structures were elucidated by spectral techniques.

Preventive effects of Impatiens balsamina on the hen egg-white lysozyme (HEL)-induced decrease in blood flow.

Monitoring the blood flow of unanesthesized mice was found to be a reliable and effective method for studying their anaphylactic responses, in addition to the known method of monitoring blood pressure. Hen egg-white lysozyme (HEL)-specific anaphylaxis in mice was estimated by monitoring the decrease in blood flow with a Doppler blood flow meter. This method is convenient for searching for both anaphylaxis and anti-anaphylactic substances from natural products.

Bisxanthones from Hypericum japonicum: inhibitors of PAF-induced hypotension.

The CHCl3-soluble part (HJ) of the MeOH extract from Hypericum japonicum afforded new bisxanthones, jacarelhyperols A (1) and B (2). The structures were elucidated by spectral methods. These compounds and HJ showed significant inhibitory effects against PAF-induced hypotension by an in vivo evaluation method, which can reveal the pharmacological action of the test material.

Antipruritic effects of 1,4-naphthoquinones and related compounds.

The antipruritic effects of orally administered 1,4-naphthoquinone derivatives and related compounds on compound 48/80-induced scratching behavior in mice were studied. 2-Hydroxy-3-(2-hydroxyethyl)-1,4-naphthoquinone, ferulic acid, 2,2'-methylenebis(3-hydroxy-1,4-naphthoquinone), and 2,2'-ethylidenebis(3-hydroxy-1,4-naphthoquinone) (impatienol) all exhibited significant antipruritic activity. However, 2-methoxy-3-(2-hydroxyethyl)-1,4-naphthoquinone (balsaquinone), which was isolated from a natural source for the first time, did not show any activity.