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Memantine (Mem) is a non-competitive N-methyl-d-aspartate (NMDA) receptor antagonist used in the treatment of Alzheimer's disease. However, side effects, including dizziness, headache and confusion, have been reported. Therefore, although it reduces the symptoms of dementia, such as memory loss, its use is limited by side effects for patients at risk of injury. In the present study, we investigated the effects of the Japanese Kampo medicine yokukansankachimpihange (YKSCH) on Mem-induced dizziness in a mouse model of memory impairment. Mem (20 mg/kg B.W., p.o.) reduced the performance score during the beam balance test and walking time on a rotarod, confirming the disrupted sense of balance and motor coordination. In contrast, YKSCH (750 mg/kg B.W., p.o.) significantly suppressed this disruption of balance and motor coordination in mice. Moreover, YKSCH did not attenuate the ameliorative effects of Mem on learning and memory impairment in the Y-maze test or step-through passive avoidance task. Spatial learning and memory significantly recovered in the Mem-treated group and Mem plus YKSCH-treated group, suggesting no pharmacological interaction between Mem and YKSCH in mice. Therefore, YKSCH may be effective at alleviating the Mem-induced equilibrium disturbance in mice with memory impairment without reducing its memory disorder improvement effects. Our study may be useful for future studies on the combined use of Mem and YKSCH in the treatment of Alzheimer's disease.

Disuse syndrome indicates psychosomatic hypofunction caused by excess rest and motionless and muscle atrophy is termed disuse muscle atrophy. Disuse muscle atrophy-induced muscle weakness and hypoactivity further induces muscle atrophy, leading to a vicious cycle, and this is considered a factor causing secondary sarcopenia and subsequently frailty. Since frailty finally leads to a bedridden state requiring nursing, in facing a super-aging society, intervention for a risk factor of frailty, disuse muscle atrophy, is important. However, the main treatment of disuse muscle atrophy is physical therapy and there are fewer effective preventive and therapeutic drugs. The objective of this study was to search for Kampo medicine with a disuse muscle atrophy-improving effect. Ninjin'yoeito is classified as a qi-blood sohozai (dual supplement) in Chinese herbal medicine, and it has an action supplementing the spleen related to muscle. In addition, improvement of muscle mass and muscle weakness by ninjin'yoeito in a clinical study has been reported. In this study, the effect of ninjin'yoeito on disuse muscle atrophy was investigated. A disuse muscle atrophy model was prepared using male ICR mice. After surgery applying a ring for tail suspension, a 1-week recovery period was set. Ninjin'yoeito was administered by mixing it in the diet for 1 week after the recovery period, followed by tail suspension for 14 days. Ninjin'yoeito administration was continued until autopsy including the hindlimb suspension period. The mice were euthanized and autopsied immediately after completion of tail suspension, and the hindlimb muscles were collected. The food and water intakes during the hindlimb unloaded period, wet weight of the collected muscle, and muscle synthesis and muscle degradation-related factors in blood and muscle were evaluated. Ingestion of ninjin'yoeito inhibited tail suspension-induced reduction of the soleus muscle wet weight. In addition, an increase in the blood level of a muscle synthesis-related factor, IGF-1, and promotion of phosphorylation of mTOR and 4E-BP1 in the soleus muscle were observed. It was suggested that ninjin'yoeito has a disuse muscle atrophy-improving action. Promotion of the muscle synthesis pathway was considered the action mechanism of this.

Kampo medicines are frequently used empirically to treat pain in clinical practice. Ninjin'yoeito (NYT), which is associated with few adverse effects, is often used to treat the elderly, but has not yet been examined in detail. We herein investigated the effects of NYT, at 500 and 1,000 mg/kg p.o. (NYT500/NYT1000 group) in single and repeated administrations for 14 days, on pain in rats with peripheral neuropathy induced by loose ligation of the sciatic nerve (chronic constriction injury: CCI). Untreated CCI rats given distilled water were used as a control group. To assess induced pain, the pain threshold was measured using the von Frey test. To evaluate spontaneous pain, the ground-contact area of the paw with neuropathic pain was measured using the Dynamic Weight Bearing test. Serum samples were collected after the test to elucidate the mechanism of action of NYT, and brain-derived neurotrophic factor (BDNF) and corticosterone protein levels, which have been reported to change due to chronic pain, were analyzed. After single administration of NYT, the pain threshold rose in the NYT500 and NYT1000 groups. The pain threshold tended to rise on day 14 of repeated administration in the NYT500 group (p = 0.08) and it significantly rose at NYT1000 group (p < 0.05) compared to Control group. In addition, the foot contact area increased (p = 0.09). Therefore, CCI-induced pain was significantly remitted and spontaneous pain was remitted after repeated administration of NYT. Serum BDNF levels were higher in untreated CCI rats than in normal rats (p = 0.05), but decreased after the repeated administration of NYT (NYT1000, p = 0.15), while serum corticosterone levels were lower (p = 0.12) than those in normal rats and increased after the repeated administration of NYT (NYT1000, p = 0.07). The blood BDNF level has been suggested to influence pain intensity. The findings demonstrated NYT effectively treats neuropathic pain, suggesting that a NYT-induced decrease in blood BDNF contributed to the mechanism of pain relief. In addition, the variation of corticosterone was observed, suggesting that normalization of responsiveness to stress by NYT contributed to the pain relief.

The Yellow River has been managed by Chinese more than 2,000 years. In Qing Dynasty (AD 1644–1911), the relationship between environment change and management style could be revealed based on GIS and historical records. In this part, (1) the design mind and function of “Digital Historical Yellow River” system, (2) the example of this system used in the Yellow River finance research. The change of the Yellow River is not only a result of environment changing, but also a management methods problem. The Yellow River hydrological changing in 1820–1840s made the Yellow River management Based on Digital Humanities and GIS, more materials could be used, more details will be revealed, and more questions will be answered.

Objective Light injury-induced apoptosis of retinal photoreceptor cells can lead to vision loss. The mechanism underlying such injury remains unclear, and there are no effective therapies at present. The aim of this study was to examine the potential antiapoptotic role of the cellular repressor of E1A-stimulated genes (CREG) in retinal cells in a rat model of light-induced retinal damage. Methods CREG proteins were injected into the vitreous space of rats in which light retinal injury was induced. An equal volume of PBS was injected into the vitreous space of a control group. Retinas were collected for H&E staining and Western blotting analysis 1, 3, and 7 days later. Inhibitors or agonist for P38, JNK, and AKT were injected into the vitreous space to verify CREG function. Results In rats with light-induced retinal injury, the CREG treatment inhibited the expression of apoptosis-related proteins caspase-3, caspase-8, and caspase-9 and signaling proteins phosphorylated ERK (P-ERK), phosphorylated JNK (P-JNK), phosphorylated P38 (P-P38), and phosphorylated AKT (P-AKT). An inhibitor of PI3K-AKT and an agonists of P38 and JNK abrogated the inhibitory effect of CREG on caspase-3 expression. Conclusion CREG protected retinal cells against apoptosis by inhibiting P38/MAPK and JNK/MAPK signaling pathways and activating the PI3K-AKT signaling pathway.

Herbal medicines, acupuncture and moxibustion are often used for unidentified complaints. It is well known that catecholamine secreted by the sympatho-adrenal medullary system primarily functions to increase cardiac output and raise glucose levels in the blood during acute stress. In the present study, the effects of yokukansankachimpihange (YKSKCH, a Kampo medicine) on urinary catecholamine in mice that were repeatedly stressed by restraining were examined. Restraint stress (240 min/d×3 d×3 cycles, daytime: 12:00-16:00) induced a marked increase in noradrenaline (NA) and adrenaline (A) levels in the urine. Oral administration of YKSKCH (750 mg/kg of body weight) significantly inhibited the increase in urinary NA and A levels in mice after repeated restraint stress. In addition, the NA/dopamine (physical stress) and A/dopamine (mental stress) ratios were lower in the 750 mg/kg YKSKCH-treated group than in the control group. The tail suspension test was also performed and locomotor activity was investigated. Oral administration of YKSKCH at 750 mg/kg significantly reduced the immobility time, which was longer in mice after repeated restraint stress. Furthermore, oral administration of YKSKCH at 750 mg/kg increased locomotor activity, which was lower in mice after repeated restraint stress. These results suggest that YKSKCH has positive effects on mental and physical stress after repeated restraint stress, without reducing locomotor activity.

Yokukansankachimpihange (YKSCH) is a Chinese formula proven in Japan to be an effective treatment for pruritus in patients with atopic dermatitis or chronic urticaria and dry eczema with psychoneurotic symptoms, such as insomnia. Sodium dodecyl sulfate (SDS) may cause skin irritation in both humans and animals. Adverse effects, such as skin dryness, barrier destruction, dermatitis, and pruritus, developed following the repeated application of 10% SDS to a local site. Therefore, the present study investigated the antipruritic effects of YKSCH on skin irritation induced by a repeated SDS stimulation in mice and attempted to elucidate the underlying mechanism of action. ICR mice were stimulated with 10% SDS and co-treated with oral YKSCH extract for four days. Only oral YKSCH extract was administered on the fifth day. Scratching behavior was observed 24 h after the last application of SDS. Intraepidermal nerve growth was investigated by an immunofluorescence analysis. NGF concentrations in the epidermis were measured using an enzyme-linked immunosorbent assay. The expression of amphiregulin (Areg) and semaphorin 3A (Sema3A) was assessed by quantitative real-time PCR. The oral administration of YKSCH (200-400 mg/kg) dose-dependently suppressed pruritus, significantly reduced intraepidermal nerve growth, and down-regulated epidermal Areg mRNA expression in SDS-treated mice. These results suggest that YKSCH exerts antipruritic effects against SDS-induced pruritus in mice. The mechanism of action of YKSCH may involve reductions in intraepidermal nerve density due to the down-regulated expression of Areg.

The Tb complex C6H14O19Tb2has been synthesized from a hydrothermal reaction and the crystal structure has been determined by means of single-crystal X-ray diffraction. The Tb atom is coordinated by nine O atoms. The molecular structure stabilized by the O-H…O hydrogen-bonding interactions.

Arginyl-fructose (AF) and arginyl-fructosyl-glucose (AFG) are products of the Maillard reaction between arginine and reducing sugars during the thermal treatment of Asian ginseng ( Panax ginseng C.A. Meyer). AF and AFG are widely distributed in red ginseng. Because there is no AFG in fresh Asian ginseng, the objective of the present study was to identify the arginine derivatives present in fresh Panax quinquefolius L. Two compounds obtained from P. quinquefolius L. were identified as AF and AFG by comparing the 13 C NMR and MS (mass spectrometry) spectra with those of standards. We propose that the Maillard reaction may exist in the fresh plant and not only during the thermal processing of ginseng. The antioxidant activities of AF and AFG were investigated in vitro . The data indicate that the Maillard reaction products AF and AFG contribute to the antioxidant activity of P. quinquefolius L.

In this paper, capillary zone electrophoresis method was used for the analysis of ceftezole sodium and cefpiramide sodium. 20 mmol/L borax solutio, 16 kV voltage, 254 nm UV detection wavelength was chosen for electrophoretic analysis.

An efficient pressurized liquid extraction (PLE) technique was employed in extracting chromones from the roots of Saposhnikovia divaricata (Radix Saposhnikoviae). Chromones were quantified and analyzed by LC-ESI/MS. The PLE procedure was optimized, validated and compared with the other conventional extraction techniques. PLE gained the best result due to the highest extraction efficiency within the shortest extraction time. The optimal conditions of PLE were employing 50% ethanol as the extraction solvent at a temperature of 140°C and an extraction pressure of 1500 psi, using one extraction cycle with a static extraction time of 8 min. A good LC separation was achieved using a Hypersil ODS2 column and methanol/water as the mobile phase at a flow rate of 0.8 mL/min. MS coupling with an ESI interface in the positive ion mode was used as the detection technique. This is the first report on combining PLE with LC-ESI/MS for the extraction and quantification of chromones in Radix Saposhnikoviae. The elaborated PLE method also provided a good alternative for the chromone extraction from other plant substances.

We reported that ginger prevented obesity in mice fed a high-fat diet in previous study. In this experiment, we examined the effects of zingerone, the major pungent component of ginger on fat storage in ovariectomized (Ovx) rats. Oral administration of 170 mg/kg zingerone significantly reduced body weight and the final parametrail adipose tissue weight in ovariectomized rats. Blood glucose levels after oral administration of glucose were lower in zingerone-treated Ovx-rats than in the Ovx-rats (control). Basal lipolysis in zingerone-treated Ovx-rats was increased compared with that in the Ovx-rats. Zingerone significantly increased norepinephrine-induced lipolysis associated with the translocation of hormone-sensitive lipase (HSL) from the cytosol to lipid droplets in adipocytes. These results indicate that zingerone may prevent the fat storage through increasing norepinephrine-induced lipolysis in adipocytes.

To investigate the anti-obesity effects of escins extracted from the seeds of Aesculus turbinata BLUME, anti-obesity models in vitro and in vivo were employed. In a preliminary experiment, different solvent fractions of Aesculus turbinata BlUME as well as two isolated compounds were tested for their effects on pancreatic lipase (PL) in vitro. Subsequently, female ICR mice were fed a high fat diet with or without different concentrations of total escins for 11 weeks to examine body weight, parametrial adipose tissue weight, and hepatic triacylglycerol (TG) and total cholesterol (TC) contents. Plasma triacylglycerol levels (TG) after oral administration of lipid emulsions to rats were also investigated. The results showed that total escins (1 mg/ml) as well as two compounds isolated from total escins, namely escin Ib and IIa, showed inhibitory effects on PL activity. In vivo, total escins suppressed the increase in body weight, parametrial adipose tissue weight, TG content, and TC content in mice's liver; TG content in rat plasma was also reduced at 1, 2 and 3 h after oral administration of the lipid emulsion plus different concentrations of escins compared to those in the lipid emulsion groups. Meanwhile, mice fed a high fat diet plus 2% total escins for 3 d had an increased TG level in the feces compared to the HF group. The reason for this may be due to a delay in the intestinal absorption of dietary fat by inhibiting PL activity.

To optimize ginsenosides hydrolyzing beta-glucosidase production from Aspergillus niger, response surface methodology was carried out in two stages. The Plackett-Burman design was achieved to screen the important variables that influence beta-glucosidase production. Among 10 variables (wheat bran, soybean powder, CaCl(2), ginsenosides, KH(2)PO(4), MgSO(4), polyethylene glycol (PEG), medium volume, inoculum size, and stirring speed), it was found that wheat bran, KH(2)PO(4), and stirring speed had significant effect on beta-glucosidase activity due to very low p-values (p

The fresh fruit (Japanese name, Tonburi) of Kochia scoparia has been used as a food garnish in Japanese-style dishes from ancient times, and may prevent metabolic syndromes such as hyperlipidemia, hypertension, obesity and atherosclerosis. This study was performed to clarify whether an ethanol extract of K. scoparia fruit prevented obesity induced in mice by a high-fat diet for 9 weeks. The ethanol extract of K. scoparia fruit prevented the increases in body weight and parametrial adipose tissue weight induced by the high-fat diet. Furthermore, consumption of a high-fat diet containing 1% or 3% K. scoparia extract significantly increased the fecal content and the fecal triacylglycerol level at day 3 compared with those in the high-fat diet group. The ethanol extract (250 mg/kg) and total saponins (100 mg/kg) of K. scoparia inhibited the elevation of the plasma triacylglyccerol level 2 or 3 h after the oral administration of the lipid emulsion. Total saponins, momordin Ic, 2′-O-β-d-glucopyranosyl momordin Ic and 2′-O-β-d-glucopyranosyl momordin IIc isolated from K. scoparia fruit inhibited the pancreatic lipase activity (in vitro). These findings suggest that the anti-obesity actions of K. scoparia extract in mice fed a high-fat diet may be partly mediated through delaying the intestinal absorption of dietary fat by inhibiting pancreatic lipase activity. Copyright © 2006 John Wiley & Sons, Ltd.

Mice were fed either a high fat diet or a high fat diet containing 1% mannooligosaccharides (MOS) for twelve weeks. The effects of MOS on fat accumulation and excretion were examined. After twelve weeks, the percentage weight of the fat and hepatic triglyceride level were significantly lower in the MOS group than that of the control group (p < 0.05 and p < 0.01 respectively). Furthermore, the serum triglyceride level had a decreasing tendency in the MOS group (p = 0.058). On the other hand, the fecal triglyceride level as well as the amount of fat excreted significantly increased in the MOS group (p < 0.05). This study showed that the administration of MOS lessened the fat accumulation in the parametrial adipose tissue and the liver while at the same time increased the amount of fat being excreted. These results indicate that MOS may prevent the fat storage through inhibiting the intestinal absorption of dietary fat in a high fat diet.

The antiobesity effects of Coleus forskohlii were investigated in ovariectomized (ovx) rats. Eight-week-old female Wistar rats were assigned to four groups: a sham-operated group fed the control diet (MF, sham-m) ; an ovx-m group fed the control diet; a sham-operated group fed the control diet containing 50 g/kg of Coleus forskohlii extract (sham-c) ; and an ovx-c group fed the control diet containing 50 g/kg of Coleus forskohlii extract. The body weight, adipose tissues, and cell diameter were investigated in ovx rats after Coleus forskohlii extract treatment. Administration of Coleus forskohlii extracts reduced body weight, food intake, and fat accumulation in ovx rats. Our results suggest that Coleus forskohlii may be useful in the treatment of obesity.

In the process of investigating anti-obesity effect of Platycodi Radix, we found that aqueous extract of Platycodi Radix might inhibit intestinal absorption of dietary fat by inhibiting pancreatic lipase (PL) activity. In order to clarify the anti-obesity mechanism of Platycodi Radix, activity-guided isolation was performed to find active components. The total saponin fraction of Platycodi Radix appeared to have a potent inhibitory activity against the hydrolysis of triolein emulsified with phosphatidycholine by pancreatic lipase in vitro. Based on these results, further purification of active components yielded 10 known triterpenoidal saponins, among these compounds, platycodin A, C, D, and deapioplatycodin D exhibited significant inhibitory effects on PL at the concentration of 500 microg/mL with 3.3, 5.2, 34.8, and 11.67% pancreatic lipase activity vs control, respectively. Platycodin D was found to inhibit the PL activity in a dose-dependent manner. Therefore, the anti-obesity effect of Platycodi Radix might be due to the inhibition of pancreatic lipase by its saponins.

Zingiber officinale Roscoe has been used as a folk medicine in China. An aqueous extract of Z. officinale Roscoe inhibited the hydrolysis of triolein emulsified with phosphatidylcholine by pancreatic lipase in vitro and it reduced the elevation of rat plasma triacylglycerol levels 1 and 2 h after oral administration of a lipid emulsion containing corn oil. These results suggest that the aqueous extract of Z. officinale Roscoe might inhibit the intestinal absorption of dietary fat by inhibiting its hydrolysis. Therefore we investigated the antiobesity effects of the aqueous extract of Z. officinale Roscoe by feeding a high-fat diet to mice for 8 weeks. Body weights at 2-8 weeks and final parametrial adipose tissue weights were significantly lower in mice fed the high-fat diet containing 3% aqueous extract of Z. officinale Roscoe than in the controls fed the high-fat diet. Feeding a high-fat diet containing 1% aqueous extract of Z. officinale Roscoe also significantly reduced final parametrial adipose tissue weights that were elevated in mice fed the high-fat diet alone. Our data suggest that the antiobesity effect of aqueous extract of Z. officinale Roscoe in mice fed a high-fat diet may be due in part to the inhibition of intestinal absorption of dietary fat by the active compounds of Z. officinale Roscoe.

The present study investigated the effects of Ginkgo biloba extract and its flavonoid fractions on alpha-amylase and alpha-glucosidase activity in vitro. Ginkgo biloba extracts and their flavonoid fraction significantly inhibited alpha-amylase and alpha-glucosidase activity in vitro. Furthermore, Ginkgo biloba extracts and their flavonoid fraction reduced the elevation of rat plasma glucose level after oral administration of various saccharinity agents. In addition, we examined the effects of the flavonoid fraction isolated from Ginkgo biloba extracts on the plasma glucose level in streptozotocin-induced diabetic rats. When flavonoid fractions were orally administered to the rats three times daily for 9 days, plasma glucose concentrations were decreased compared with those in the water treatment group. Furthermore, flavonoid fractions reduced the elevation of rat plasma glucose levels after oral administration of sucrose and glucose in streptozotocin-induced diabetic rats.

The inhibitory effects were examined of a hot-water extract of coffee beans on Kud: Wistar rats by an in vivo oral saccharinity tolerance test (OST), and the in vitro suppression of alpha-amylase and alpha-glucosidase activity. The hot-water extract of coffee beans strongly inhibited the activities of alpha-amylase and alpha-glucosidase, and reduced the postprandial blood glucose concentration by OST. Chlorogenic acid and acarbose strongly inhibited the activity of alpha-glucosidase, and reduced the postprandial blood glucose concentration by OST. However, caffeine, which is a major component of coffee beans, had no such effect. These results suggest that the inhibitory effect of the hot-water extract of coffee beans on postprandial hyperglycemia may have been due in part to the inhibition of alpha-glucosidase by chlorogenic acid which is a major component of coffee beans.

The effect of bittern on a mouse IgE-mediated dermatitis model was examined. Both the immediate- and delayed-type responses elicited by the IgE-antigen treatment were significantly suppressed in mice treated with bittern. On the other hand, MgCl2, the main component of bittern, failed to suppress either the immediate-or delayed-type response. Furthermore, bittern was found to inhibit IgE production in mice treated with ovalbumin. These results suggest that bittern may improve the pathological state of human atopic dermatitis.

The results of this study clarify the physiological significance of the variation in skin temperature at the shoulder. The skin temperature was found to be reduced by shoulder stiffness, indicating that this decrease in the skin temperature might have been caused by disturbance of the peripheral blood flow. In addition to the effect from shoulder stiffness, ingesting miso soup called “asage” also reduced the skin temperature at shoulder. The addition of bittern prepared at Indonesia to the miso soup accelerated the reduction of skin temperature, suggesting that the salty taste of the miso soup might have been responsible for this reduction. Experiments were conducted to clarify whether or not the bittern increased the salty taste of the miso soup to indicate that the reduction in skin temperature might have been induced by the salty taste. The experimental results clearly indicated that the bittern increased the salty taste of NaCl solution and show that MgCl2 in the bittern was the active principle. These results collectively suggest that reduction in skin temperature associated with shoulder stiffness might have been induced by the reduction of peripheral blood flow and that the addition of the bittern to the miso soup accelerated this reduction in skin temperature.

In preliminary experiments, polyphenol fractions prepared from the leaves of Salix matsudana reduced the elevation of the rat plasma triacylglycerol level at 3 and 4 h after oral administration of a lipid emulsion containing corn oil, at a dose of 570 mg/kg. The present study examined the anti-obesity action of polyphenol fractions of S. matsudana leaves by testing whether the polyphenol fractions prevented the obesity induced by feeding a high-fat diet to female mice for 9 weeks. Body weights at 2-9 weeks and the fi nal parametrial adipose tissue weights were significantly lower in mice fed the high-fat diet with 5% polyphenols of S. matsudana leaves than in those fed the high-fat diet alone. The polyphenols of S. matsudana leaves also significantly reduced the hepatic total cholesterol content, which was elevated in mice fed the high-fat diet alone. In addition, the polyphenol fractions of S. matsudana leaves inhibited palmitic acid uptake into brush border membrane vesicles prepared from rat jejunum and alpha-amylase activity, and their fractions enhanced norepinephrine-induced lipolysis in fat cells. In conclusion, it is suggested that the inhibitory effects of the flavonoid glycoside fraction of S. matsudana leaves on high-fat diet-induced obesity might be due to the inhibition of carbohydrate and lipid absorption from small intestine through the inhibition of alpha-amylase and palmitic acid uptake into small intestinal brush border membrane or by accelerating fat mobilization through enhancing norepinephrine-induced lipolysis in fat cells.

Previously, it was reported that polyphenol fractions prepared from the leaves of Salix matsudana reduced the elevation of the rat plasma triacylglycerol level at 3 and 4 h after oral administration of a lipid emulsion containing corn oil, at a dose of 570 mg/kg. Moreover, body weights at 2-9 weeks and the fi nal parametrial adipose tissue weights were significantly lower in mice fed the high-fat diet with 5% polyphenol fractions of S. matsudana leaves than in those fed the high-fat diet alone. The polyphenol fractions of S. matsudana leaves also significantly reduced the hepatic total cholesterol content, which was elevated in mice fed the high-fat diet alone. In addition, the polyphenol fractions of S. matsudana leaves inhibited palmitic acid uptake into brush border membrane vesicles prepared from rat jejunum and alpha-amylase activity, and their fractions enhanced norepinephrine-induced lipolysis in fat cells. To clarify the active substances inhibiting the palmitic acid uptake into small intestinal brush border membrane, the alpha-amylase activity or enhancing the norepinephrine-induced lipolyis in fat cells, the isolation of the active substances from polyphenol fraction was attempted using the above three assay systems. Compounds 1, 2 and 3 were isolated from the polyphenol fractions and identified as apigenin-7-O-d-glucoside, luteolin-7-O-d-glucoside and chrysoeriol-7-O-d-glucoside, respectively. Among three flavonoids, apigenin-7-O-d-glucoside inhibited alpha-amylase activity, and luteolin-7-O-d-glucoside and chrysoeriol-7-O-d-glucoside inhibited palmitic acid uptake into small intestinal brush border membrane. Furthermore, three flavonoid glucosides enhanced norepinephrine-induced lipolysis in fat cells.

The aim of this experimental trial was to study the effect of ultrasound application on the lipolysis in adipose tissue. Rats were administered to pentobarbital (Nembutal) anesthesia and their abdomens were shaved. Rat abdomen was subjected to 24 kHz-1 MHz ultrasound for 10 min to investigate frequency and power-intensity dependency for fat mobilization. Blood was taken from the tail vein to estimate plasma free fatty acids (FFA). For frequency dependency two regions around 100 kHz and 300-500 kHz were effective for fat mobilization. For power-intensity dependency, effective regions were found to be from 24 to 1090 kHz. In the effective regions on frequency and power-intensity, application of ultrasound caused increases in plasma FFA and norepinephrine concentration of extra-cellular fluid of perirenal adipose tissue. These results suggest that ultrasound application stimulates fat mobilization through a local increase in norepinephrine secretion under the conditions of effective frequency and intensity.

OBJECTIVE: Based on the inhibitory effects of teasaponin on pancreatic lipase activity in vitro, this study was performed to clarify whether teasaponin prevented obesity induced in mice by a high-fat diet for 11 weeks. DESIGN: For in vitro experiments, assay for the inhibitory effects of teasaponin on pancreatic lipase activity was performed by measuring the rate of release of oleic acid from triolein in an assay system using triolein emulsified with lecithin, gum arabic, Triton X-100 or 4-methylumbelliferyloleate. For in vivo experiments, female ICR mice were fed a high-fat diet with or without 0.5% teasaponin for 11 weeks. RESULTS: Teasaponin competitively inhibited the hydrolysis of triolein emulsified with lecithin, gum arabic, Triton X-100 or 4-methylumbelliferyloleate. Teasaponin inhibited the elevations of plasma triacylglycerol levels 3, 4 and 5 h after oral administration of lipid emulsion containing corn oil. Teasaponin suppressed the increases in body, parametrial adipose tissue weights and diameter in adipose cell size induced by a high-fat diet. Furthermore, feeding a high-fat diet plus teasaponin had no effect on stool frequency and content, but significantly increased triacylglycerol contents in feces as compared to feeding a high-fat diet. CONCLUSIONS: The anti-obesity effects of teasaponin in high-fat diet-treated mice may be partly mediated through delaying the intestinal absorption of dietary fat by inhibiting pancreatic lipase activity.

We suggested a strategy for identifying anti-obesity drugs. The strategy aimed to prevent obesity through inhibiting intestinal absorption of dietary fat. Intestinal absorption of dietary fat was found to be reduced by tea saponin and chitosan through inhibiting pancreatic lipase activity, by chondroitin sulfate through inhibiting both pancreatic lipase activity and fatty acid absorption, and by lactosucrose through inhibiting beta-monoglyceride absorption. All these functional substances reduced plasma triglyceride levels previously elevated by oral administration of a lipid emulsion containing corn oil. Furthermore, these substances were found to cause reduction in perimetrial adipose tissue weight, which had been elevated by oral administration of a high fat diet (containing 40% of beef tallow) to female mice. Based on these results, a strategy for identifying anti-obesity drugs was discussed.

Objective Chitin and chitosan are polymers containing more than 5000 acetylglucosamine and glucosamine units, respectively, and their molecular weights are over one million Daltons. The present study assessed the effects of chitin-chitosan on the activity of pancreatic lipase in vitro and on the degree of fat storage induced in mice by the oral administration of a high-fat diet for nine weeks. Design Mice were fed a high-fat diet and treated with chitin-chitosan for nine weeks. Experiments were also carried out to clarify whether or not chitin-chitosan inhibited pancreatic lipase activity in assay systems using triolein emulsified with lecithin, gum arabic or Triton X-100. Results Chitin-chitosan prevented the increase of body weight, hyperlipidaemia and fatty liver induced by a high-fat diet. Chitin-chitosan inhibited hydrolysis of triolein, emulsified with phosphatidylcholine, but not that of triolein emulsified with gum arabic and Triton X-100. These results suggest that the site of inhibitory action of chitin-chitosan may not be the enzyme but its substrate. Conclusion The anti-obesity effects of chitin-chitosan in high-fat diet-treated mice might be partly due to the inhibition of intestinal absorption of dietary fat. Consequently, chitin-chitosan might cause improvement of the fatty liver and hyperlipidaemia in mice fed a high fat diet through inhibiting intestinal absorption of dietary fat.

OBJECTIVE: Oolong tea is traditionally reported to have anti-obesity and hypolipidaemic effects. The present study was performed to clarify whether oolong tea prevented obesity induced in mice by the oral administration of a high-fat diet for 10 weeks. DESIGN: High-fat diet-induced obese mice were treated with oolong tea for 10 weeks. The effects of various active fractions isolated from oolong tea on noradrenaline-induced lipolysis were examined with isolated fat cells and a cell-free system consisting of lipid droplets and hormone-sensitive lipase (HSL). RESULTS: The mean food consumption was not significantly different between high-fat diet-treated mice and high-fat plus oolong tea diet-treated mice. Oolong tea prevented the obesity and fatty liver induced by a high-fat diet. A water extract of oolong tea enhanced noradrenaline-induced lipolysis, and the active substance was identified as caffeine. Caffeine enhanced noradrenaline-induced lipolysis in fat cells without a concomitant increase in HSL activity and also accelerated the hormone-induced lipolysis in a cell-free system consisting of lipid droplets and HSL, but not in the cell-free system with sonicated lipid droplets and HSL. Oolong tea extract inhibited pancreatic lipase activity. CONCLUSION: It was demonstrated that the anti-obesity effects of oolong tea in high-fat diet-treated mice might be due partly to the enhancing effect of caffeine isolated from oolong tea on noradrenaline-induced lipolysis in adipose tissue, and to the inhibitory action of some other substance in oolong tea on pancreatic lipase activity. Caffeine was found to enhance lipolysis through acting on lipid droplets but not on HSL. The results suggest that oolong tea may be an effective crude drug for the treatment of obesity and fatty liver caused by a high-fat diet.

A new triterpenoid saponin, 3- O -β- d -glucopyranosyl 16-oxo-platycodigenin 28- O -β- d -apiofuranosyl-(1 → 3)-β- d -xylopyranosyl-(1 → 4)-α- l -rhamnopyranosyl-(1 → 2)-α- l -arabinopyra-nosyl ester, was isolated from the roots of Platycodon grandiflorum , together with three known saponins, including platycodin D, deapio platycoside E and platycoside E. The structure of the new compound, named 16-oxo-platycodin D, was elucidated on the basis of spectroscopic data.

An EtOAc-soluble fraction from a 80% Me2CO extract of the rhizomes of Astilbe thunbergii enhanced norepinephrine-induced lipolysis in rat fat cells, while an EtOAc-insoluble fraction had no effect. The active substances isolated from the EtOAc-soluble fraction of the rhizomes were identified as eucryphin (1), bergenin (2), and astilbin (3), which enhanced norepinephrine-induced lipolysis at concentrations of 10-1000 microgram/mL, while they themselves did not cause lipolysis. Furthermore, these compounds slightly stimulated adrenocorticotrophic hormone-induced lipolysis and inhibited insulin-induced lipogenesis from glucose.

The water extract of Juglans mandshurica fruit has been shown to strongly inhibit pancreatic lipase in vitro in a dose-dependent manner. The extract was observed to inhibit the normal elevation in the level of plasma triacylglycerol in rats 2–4 h after oral administration of a lipid emulsion. Fourteen compounds isolated from J. mandshurica fruit were evaluated for their inhibitory activity against pancreatic lipase. Of these, 1,4,8-trihydroxynaphthalene-1-O-β-d-[6′-O-(3″,4″,5″-trihydroxybenzoyl)]glucopyranoside (1) showed the strongest inhibitory activity.

Introduction – Radix Saposhnikoviae is one of the most famous Chinese herbal medicines with many pharmacological activities towards inflammatory symptoms and antioxidation. Chromones are considered as one of the effective components. It is important to find a reasonable method to extract the chromones in S. divaricata. Objective – To develop an ultrasonic-assisted extraction (UAE) to extract chromones in Radix Saposhnikoviae and to optimise extraction conditions. Methodology – Four chromones (prim-O-glucosylcimifugin, cimifugin, 5-O-methylvisammioside and sec-O-glucosylhamaudol) were extracted by the UAE method combined with response surface methodology (RSM). Box–Behnken design (BBD) was applied to evaluate the effects of three independent variables (ethanol concentration, extraction time and extraction temperature) on the chromones yield of Radix Saposhnikoviae. Results – Correlation analysis of the mathematical-regression model indicated that a quadratic polynomial model could be employed to optimise the extraction of chromones by UAE method. The optimal conditions to obtain the highest chromones yield of Radix Saposhnikoviae were a solvent of 75% ethanol, an extraction time of 48 min and an extraction temperature of 67°C. Conclusion – Under these optimal conditions, the experimental values agreed closely with the predicted values. The analysis of variance indicated a high goodness of model fit and the success of RSM method for optimising chromones extraction in Radix Saposhnikoviae. Copyright © 2011 John Wiley & Sons, Ltd.

The present study was performed to clarify whether the crude saponins from stems and leaves of Panax quinquefolium inhibited lipase activity in vitro, and prevented obesity induced in mice by feeding a high-fat diet for 8 weeks. For in vitro experiments, assay for the inhibitory effects of saponins from stems and leaves of Panax quinquefolium on pancreatic lipase activity was performed by measuring the rate of release of oleic acid from triolein. For in vivo experiments, female ICR mice were fed a high-fat diet with or without saponins from stems and leaves of Panax quinquefolium for 8 weeks. The crude saponins inhibited pancreatic lipase activity in vitro. Furthermore, crude saponins (lg/kg body weight) inhibited the elevations of plasma triacylglycerol in rats administered the oral lipid emulsion tolerance test. In addition, long-term administration of crude saponins, the parametrial adipose tissue weight was decreased by feeding a high-fat diet containing l% or 3% crude saponins compared to those of high-fat diet group. It is demonstrated that the anti-obesity effects of the crude saponins from stems and leaves of Panax quinquefolium in high-fat diet-treated mice may be due to the inhibition of intestinal absorption of dietary fat by ginsenosides Rc, Rb(1) and Rb(2).

Three new triterpenoid saponins, gypsosaponins A-C (1-3), were isolated from the roots of Gypsophila oldhamiana (Caryophyllaceae). Their structures were established as 3-O-beta-D-galactopyranosyl-(1-->2)-[beta-D-xylopyranosyl-(1-->3)]-beta-D-glucuronopyranosyl quillaic acid 28-O-alpha-L-arabinopyranosyl-(1-->2)-alpha-L-arabinopyranosyl-(1-->3)-beta-D-xylopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->2)-beta-D-fucopyranoside (1), 3-O-beta-D-galactopyranosyl-(1-->2)-[beta-D-xylopyranosyl-(1-->3)]-methyl-beta-D-glucuronopyranosyl gypsogenin 28-O-beta-D-glucopyranosyl-(1-->3)-[beta-D-xylopyranosyl-(1-->4)]-alpha-L-rhamnopyranosyl-(1-->2)-beta-D-fucopyranoside (2), and 23-O-beta-D-glucopyranosyl gypsogenic acid 28-O-beta-D-glucopyranosyl-(1-->3)-[beta-D-glucopyranosyl-(1-->6)]-beta-D-glucopyranoside (3), on the basis of various spectroscopic analyses and chemical degradations. The biological activities of 1-3 were examined inhibitory activity against pancreatic lipase, which showed inhibition of 58.2%, 99.2% and 50.3% at concentration of 1 mg/ml, respectively.

Three new triterpenoid saponins, acanthopanaxosides A (1), B (7), and C (13), were isolated from the leaves of Acanthopanax senticosus, together with 12 known saponins. The structures of these new saponins were established as 3-O-beta-D-glucopyranosyl-(1-->2)-alpha-L-arabinopyranosyl-30-nor-olean-12,20(29)-dien-28-oic acid 28-O-alpha-L-rhamnopyranosyl-(1-->4)-6-O-acetyl-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl ester (1), 3-O-beta-D-glucopyranosyl-(1-->2)-alpha-L-arabinopyranosyl oleanolic acid 28-O-alpha-L-rhamnopyranosyl-(1-->4)-6-O-acetyl-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl ester (7), and 3-O-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranosyl-3beta-hydroxyolean-12-ene-28,29-dioic acid (13), on the basis of spectroscopic analysis and chemical degradation. Among the known compounds, sessiloside and tauroside H1 are reported for the first time from A. senticosus. The biological activity of compounds 1-15 was examined against pancreatic lipase. Ciwujianoside C1 (6), tauroside H1 (11), 3-O-alpha-rhamnopyranosyl-(1-->2)-alpha-arabinopyranosyl mesembryanthemoidigenic acid (12), acanthopanaxoside C (13), sessiloside (14), and chiisanoside (15) inhibited pancreatic lipase activity in vitro. In turn, ciwujianosides C2 (3), D2 (5), C4 (8), and C3 (10) and hederasaponin B (9) enhanced this enzyme.

The fresh fruit (Japanese name, Tonburi) of Kochia scoparia has been used as a food garnish in Japanese-style dishes from ancient times, and may prevent metabolic syndromes such as hyperlipidemia, hypertension, obesity and atherosclerosis. This study was performed to clarify whether an ethanol extract of K. scoparia fruit prevented obesity induced in mice by a high-fat diet for 9 weeks. The ethanol extract of K. scoparia fruit prevented the increases in body weight and parametrial adipose tissue weight induced by the high-fat diet. Furthermore, consumption of a high-fat diet containing 1% or 3% K. scoparia extract significantly increased the fecal content and the fecal triacylglycerol level at day 3 compared with those in the high-fat diet group. The ethanol extract (250 mg/kg) and total saponins (100 mg/kg) of K. scoparia inhibited the elevation of the plasma triacylglyccerol level 2 or 3 h after the oral administration of the lipid emulsion. Total saponins, momordin Ic, 2'-O-beta-d-glucopyranosyl momordin Ic and 2'-O-beta-d-glucopyranosyl momordin IIc isolated from K. scoparia fruit inhibited the pancreatic lipase activity (in vitro). These findings suggest that the anti-obesity actions of K. scoparia extract in mice fed a high-fat diet may be partly mediated through delaying the intestinal absorption of dietary fat by inhibiting pancreatic lipase activity.

In the process of investigating the hypolipidemic effects of Spirulina platensis, we found that the aqueous extract of S. platensis may inhibit the intestinal absorption of dietary fat by inhibiting pancreatic lipase activity. The aqueous extract of S. platensis (500 m/kg) reduced the elevation of rat plasma triacylglycerol levels after oral administration of the lipid emulsion 2 h after administration. To clarify the hypolipidemic effects of S. platensis, the active component was isolated and designated 1'-O-(palmitonyl)-2'-O-(caprylonyl) glyceryl-beta-alpha-D-galactopyranoside (glycolipid H-b2). Glycolipid H-b2 was found to inhibit pancreatic lipase activity in a dose-dependent manner. The fractions containing glycolipid H-b2 (250 mg/kg) reduced the elevation of rat plasma triacylglycerol levels after oral administration of the lipid emulsion 2 h after administration. Furthermore, we examined the effects of phycocyanin isolated from S. platensis on pancreatic lipase activity. Phycocyanin inhibited the pancreatic lipase activity in a dose-dependent manner. These results suggest that the inhibitory effects of S. platensis on postprandial triacylglycerolemia may be due in part to the inhibition of pancreatic lipase activity by glycolipid H-b2 and phycocyanin.

The antiobesity effects of Coleus forskohlii were investigated in ovariectomized (ovx) rats. Eight-week-old female Wistar rats were assigned to four groups: a sham-operated group fed the control diet (MF, sham-m) ; an ovx-m group fed the control diet; a sham-operated group fed the control diet containing 50 g/kg of Coleus forskohlii extract (sham-c) ; and an ovx-c group fed the control diet containing 50 g/kg of Coleus forskohlii extract. The body weight, adipose tissues, and cell diameter were investigated in ovx rats after Coleus forskohlii extract treatment. Administration of Coleus forskohlii extracts reduced body weight, food intake, and fat accumulation in ovx rats. Our results suggest that Coleus forskohlii may be useful in the treatment of obesity.