Morus alba, a Medicinal Plant for Appetite Suppression and Weight Loss.

The prevalence of obesity is expanding rapidly worldwide, making the disease a global burden with limited treatment options. The current obesity drug development trends suggest the possibility of reducing weight and reverse metabolic disturbances of obesity by controlling appetite. In this study, we screened more than 8000 plants from our plant library for the cannabinoid (CB1) receptor antagonists and identified Morus alba as a lead medicinal plant. Kuwanon G and Albanin G were isolated and identified from root-barks of Morus alba with 92% and 96% CB1 receptor ligand binding inhibitory activity, respectively. The bioflavonoid standardized extract was tested in the acute food intake study in rats at oral doses of 250 and 500 mg/kg for its appetite suppression activity. Diet-induced obesity in the C57BL/6J mice was used to evaluate the long-term food intake reduction activity and effect on the weight loss administered orally at 250 and 500 mg/kg for 7 weeks. Statistically significant and dose-dependent reduction in food intake was observed in both acute and long-term studies for the extract. Food intake reductions of 58.6% and 44.8% at 250 mg/kg and 50.1% and 44.3% at 500 mg/kg were observed at 1 and 2 h postfood provision, respectively. A 20% reduction in daily calorie intake was observed in the long-term study. Obese mice treated with the high dose of Morus root-bark extract showed 10.4 g (22.5%) and 7.1 g (16.5%) loss in body weight compared with the vehicle-treated obese animals (at week 7) and baseline, respectively. Statistically significant reductions in biochemical markers and visceral fat deposit were also observed. These results demonstrated that Morus alba extracts enriched in Kuwanon G, and Albanin G could be used alone to control appetite, manage body weight, and improve metabolic syndromes.

Evaluation of Natural Product Compositions for Appetite Suppression.

A change in homeostasis between food intake and energy expenditure is the hallmark of obesity. Many plant-based weight-management products are available in dietary supplement markets with no direct efficacy comparison. In this in vivo acute feed intake study in rats, the appetite suppression efficacy of well-known natural ingredients in the weight-loss market were evaluated. We tested pure caffeine, potato skin extract, Cissus quadrangularis extract, Garcinia cambogia extract, Crocus sativus extract, raspberry ketone isolated from Rubus idaeus, one commercial product (Appetrex), and one novel composition (UP601). Rats treated with potato skin extract, Crocus sativus bulb extract, and Cissus quadrangularis extracts showed statistically significant reduction in food consumption only at the 2-hour timepoint with 44.9%, 34.1%, and 44.3% reductions, respectively, after food provision at an equivalent human dosage of 2 g, 10 g, and 10 g, respectively. Garcinia cambogia fruit extract and raspberry ketone from Rubus idaeus showed statistically significant reduction in food consumption only at the 1-hour timepoint with 33.7% and 79.4% reductions, respectively, after food provision at an equivalent human dosage of 8 g and 5 g, respectively. UP601 and Appetrex were compared at 230 mg/kg. While 88.5%, 73.8%, and 63.1% reductions in food intake were observed for the UP601 treatment group, 64.2%, 27.5%, and 34.7% reductions in food intake were observed for rats treated with Appetrex at 1 h, 2 h, and 4 h after food provision. The composition UP601 demonstrated superior activity in food intake compared to any of the dietary supplements marketed for appetite suppression tested in this study.

A Botanical Composition from Morus alba, Ilex paraguariensis, and Rosmarinus officinalis for Body Weight Management.

Obesity is the largest and fastest growing public health catastrophe in the world affecting both adults and children with a prevalence impacting more than one-third of United States (US) adult population. Although the long-term solution lies in lifestyle changes in the form of dieting and exercise, intervention is required for those who are already obese. Unfortunately, treatment options remain quite limited due to associated side effects of conventional therapeutics. As a natural alternative, in this study we describe the beneficial effect of a standardized composition (UP603) comprised of extracts from Morus alba, Ilex paraguariensis, and Rosmarinus officinalis in improving metabolic disorders in high fat diet (HFD) and high fat & high fructose diet (HFFD) induced obese C57BL/6J mice. Mice treated with UP603 showed dose-correlated decrease in body weight gains compared to vehicle treated HFFD group. Following 7 weeks of treatment, the changes in body weight gains from baseline were found as 6.4%, 27.3%, 2.0%, 3.1%, 0.4%, and -2.9% for normal control diet, HFFD, Orlistat, 450, 650, and 850 mg/kg UP603 treated animals, respectively. Reductions of 7.9-21.1% in total cholesterol, 25.4-44.6% in triglyceride, and 22.5-38.2% in low-density lipoprotein were observed for mice treated with 450-850 mg/kg of UP603. In a dual energy X-ray absorptiometry scan, percentage body fat of 18.9%, 47.8%, 46.1%, and 40.4% were found for mice treated with normal control, HFD, Orlistat, and UP603, respectively. Reductions of 65.5% and 16.4% in insulin and leptin, respectively, and 2.1-fold increase in ghrelin level were also observed for the UP603 group. Statistically significant improvements in nonalcoholic steatohepatitis scores were also observed from liver histology for mice treated with UP603. Hence, UP603, a standardized botanical composition from M. alba, I. paraguariensis, and R. officinalis could potentially be considered as a natural alternative to maintain healthy body weight and to manage metabolic syndrome.

UP601, a standardized botanical composition composed of Morus alba, Yerba mate and Magnolia officinalis for weight loss.

BACKGROUND: The prevalence of obesity is surging in an alarming rate all over the world. Pharmaceutical drugs are considered potential adjunctive therapy to lifestyle modification. However, for most, besides being too expensive, their long term usages are hindered by their severe adverse effects. Here we describe the effect of UP601, a standardized blend of extracts from Morus alba, Yerba mate and Magnolia officinalis, in modulating a number of obesity-related phenotypic and biochemical markers in a high-fat high-fructose (HFF)-induced C57BL/6J mouse model of obesity. METHOD: Adipogenesis activity of the composition was assessed in 3T3-L1 cells in vitro. Effects of UP601 on body weight and metabolic markers were evaluated. It was administered at oral doses of 300 mg/kg, 450 mg/kg and 600 mg/kg for 7 weeks. Orlistat (40 mg/kg/day) was used as a positive control. Body compositions of mice were assessed using dual energy X-ray absorptiometry (DEXA). Serum biomarkers were measured for liver function and lipid profiling. Relative organ weights were determined. Histopathological analysis was performed for non-alcoholic steatohepatitis (NASH) scoring. RESULTS: UP601 at 250 µg/ml resulted in 1.8-fold increase in lipolysis. Statistically significant changes in body weight (decreased by 9.1, 19.6 and 25.6% compared to the HFF group at week-7) were observed for mice treated with UP601 at 300, 450 and 600 mg/kg, respectively. Reductions of 9.1, 16.9, and 18.6% in total cholesterol; 45.0, 55.0, 63.6% in triglyceride; 34.8, 37.1 and 41.6% in LDL; 3.2, 21.6 (P = 0.03) and 33.7% (P = 0.005) in serum glucose were observed for UP601 at 300, 450 and 600 mg/kg, respectively. Body fat distribution was found reduced by 31.6 and 17.2% for the 450 mg/kg UP601 and orlistat, respectively, from the DEXA scan analysis. Up to an 89.1% reduction in mesenteric fat deposit was observed for UP601 in relative organ weight. Statistically significant improvements in NASH scores were observed for mice treated with UP601. CONCLUSION: UP601, a standardized botanical composition from Morus alba, Yerba mate and Magnolia officinalis could potentially be used for achieving healthy weight loss and maintenance.

Appetite Suppression and Antiobesity Effect of a Botanical Composition Composed of Morus alba, Yerba mate, and Magnolia officinalis.

Background. Obesity and its comorbidities continue to challenge the world at an alarming rate. Although the long term solution lies on lifestyle changes in the form of dieting and exercising, drug, medical food, or dietary supplement interventions are required for those who are already obese. Here we describe a standardized blend composed of extracts from three medicinal plants: Morus alba, Yerba mate, and Magnolia officinalis for appetite suppression and metabolic disorders management. Method. Extracts were standardized to yield a composition designated as UP601. Appetite suppression activity was tested in acute feed intake rat model. Efficacy was evaluated in C57BL/6J mouse models treated with oral doses of 1.3 g/kg/day for 7 weeks. Orlistat at 40 mg/kg/day was used as a positive control. Body compositions of mice were assessed using a dual energy X-ray absorptiometry (DEXA). ELISA was done for insulin, leptin, and ghrelin level quantitation. Nonalcoholic steatohepatitis (NASH) scoring was conducted. Results. Marked acute hypophagia with 81.8, 75.3, 43.9, and 30.9% reductions in food intake at 2, 4, 6, and 24 hours were observed for UP601. Decreases in body weight gain (21.5% compared to the HFD at weeks 7 and 8.2% compared to baseline) and calorie intake (40.5% for the first week) were observed. 75.9% and 46.8% reductions in insulin and leptin, respectively, 4.2-fold increase in ghrelin level, and reductions of 18.6% in cholesterol and 59% in low-density lipoprotein were documented. A percentage body fat of 18.9%, 47.8%, 46.1%, and 30.4% was found for mice treated with normal control, HFD, Orlistat, and UP601, respectively. 59.3% less mesenteric fat pad and improved NASH scores were observed for UP601. Conclusion. UP601, a standardized botanical composition from Morus alba, Yerba mate, and Magnolia officinalis could be used as a natural alternative for appetite suppression, maintaining healthy body weight and metabolism management.

UP1306, a Botanical Composition with Analgesic and Anti-inflammatory Effect.

BACKGROUND: Pain, one of the cardinal signs of inflammation, is the most common clinical manifestations of arthritis. Conventional pain relief therapy heavily relies on the use of prescription and over the counter nonsteroidal anti-inflammatory drugs as the first line of defense where their long-term usage causes deleterious gastrointestinal and cardiovascular-related side-effects. Hence, there is an equivocal need for evidence-based safer and efficacious alternatives from natural sources to overcome the most prominent and disabling symptoms of arthritis. MATERIALS AND METHODS: Carrageenan-induced rat paw edema and abdominal constriction (writhing's) assays in mouse were used to evaluate the anti-inflammatory and analgesic effects of UP1306, a composition that contains a standardized blend of extracts from the heartwood of Acacia catechu and the root bark of Morus alba administered orally at dose ranges of 100-300 mg/kg. Cyclooxygenase (COX) and lipoxygenase (LOX) inhibition assays were carried out to determine the IC50 of Acacia and Morus extracts. The merit of combining these two extracts was also assessed. RESULTS: Statistically significant improvement in pain resistance and suppression of edema were observed in animals treated with UP1306, when compared to vehicle-treated diseased rats and mice. Results from the high dose of UP1306 (300 mg/kg) were similar to those achieved by ibuprofen treatment at a dose of 200 mg/kg in early hours of treatment. In vitro, UP1306 showed dose-dependent inhibition of the enzymatic activities of COX and LO with IC50 values of 20.9 µg/mL, 49.2 µg/mL, and 11.1 µg/mL in COX-1, COX-2, and 5'-LO, respectively. CONCLUSIONS: These data suggest that UP1306, analgesic, and anti-inflammatory agent of botanical origin with dual COX-LO inhibition activity, could potentially be used to alleviate symptom associated to osteoarthritis. SUMMARY: Pain is the most common clinical manifestations of arthritisCarrageenan-induced rat paw edema and abdominal constriction (writhing's) assays in mouse are among the widely used models to evaluate the anti-inflammatory and analgesic effects of nutraceuticalsCyclooxygenase and lipoxygenase (LO) inhibition assays were carried out to determine the IC50 of Acacia and Morus extracts.Efficacy of UP1306, a composition containing a blend of two standardized extracts from the heartwood of Acacia catechu and root bark of Morus alba, was evaluated in the above models.UP1306 demonstrated its enhanced significance by improving the major cardinal signs of arthritis in vivo and inflammation markers in vitro.UP1306 could potentially be considered as a dietary supplement product for the management of arthritis.

Hepatoprotective Activity of Herbal Composition SAL, a Standardize Blend Comprised of Schisandra chinensis, Artemisia capillaris, and Aloe barbadensis.

Some botanicals have been reported to possess antioxidative activities acting as scavengers of free radicals rendering their usage in herbal medicine. Here we describe the potential use of "SAL," a standardized blend comprised of three extracts from Schisandra chinensis, Artemisia capillaris, and Aloe barbadensis, in mitigating chemically induced acute liver toxicities. Acetaminophen and carbon tetrachloride induced acute liver toxicity models in mice were utilized. Hepatic functional tests from serum collected at T24 and hepatic glutathione and superoxide dismutases from liver homogenates were evaluated. Histopathology analysis and merit of blending 3 standardized extracts were also confirmed. Statistically significant and dose-correlated inhibitions in serum ALT ranging from 52.5% (p = 0.004) to 34.6% (p = 0.05) in the APAP and 46.3% (p < 0.001) to 29.9% (p = 0.02) in the CCl4 models were observed for SAL administered at doses of 400-250 mg/kg. Moreover, SAL resulted in up to 60.6% and 80.2% reductions in serums AST and bile acid, respectively. The composition replenished depleted hepatic glutathione in association with an increase of hepatic superoxide dismutase. Unexpected synergistic protection from liver damage was also observed. Therefore, the composition SAL could be potentially utilized as an effective hepatic-detoxification agent for the protection from liver damage.

UP1304, a Botanical Composition Containing Two Standardized Extracts of Curcuma longa and Morus alba, Mitigates Pain and Inflammation in Adjuvant-induced Arthritic Rats.

BACKGROUND: Though, the initial etiologies of arthritis are multifactorial, clinically, patients share pain as the prime complaints. Present day pain relief therapeutics heavily relies on the use of prescription and over the counter nonsteroidal anti-inflammatory drugs as the first line of defense where their long-term usage causes gastrointestinal and cardiovascular-related side effects. Hence, the need for evidence-based safer and efficacious alternatives from natural sources to overcome the most prominent and disabling symptoms of arthritis is an overdue. Here, we evaluated the anti-inflammatory and analgesic effect of UP1304, a composition that contains a standardized blend of two extracts from the rhizome of Curcuma longa and the root bark of Morus alba in adjuvant-induced arthritis models in rats. MATERIALS AND METHODS: The anti-inflammatory and analgesic effects of the botanical composition were demonstrated in adjuvant-induced arthritis models in rats with oral dose ranges of 50-200 mg/kg. Ibuprofen at a dose of 100 mg/kg was used as a reference compound. Ex vivo sulfated glycosaminoglycan inhibition assays were performed. RESULTS: Statistically significant improvements in pain resistance, suppression of paw edema and ankle thickness were observed in animals treated with UP1304 compared to vehicle-treated diseased rats. These results were similar to those achieved by ibuprofen treatment. Inhibitions of proteoglycan degradation were observed in a range of 37.5-61.7% for concentration of UP1304 at 50-200 µg/mL when compared to interleukin-1α-exposed untreated explants. CONCLUSIONS: These data suggest that UP1304, for its analgesic and anti-inflammatory effects, could potentially be considered agent of botanical origin for the improvement of arthritis associated symptoms. SUMMARY: Pain is one of the cardinal signs of arthritis.Long term applications of commonly used non-steroidal anti-inflammatory drugs for pain relief are associated with cardiovascular and gastrointestinal side effects.Cartilage degradation evidenced as glycosaminoglycan loss from articular cartilage into the synovial fluid has been reported in arthritis patients.Adjuvant-induced arthritis model in rats are among the widely used models for efficacy evaluation of nutraceuticals.Efficacy of UP1304, a composition containing a blend of two standardized extracts from the rhizome of Curcuma longa and root bark of Morus alba, was evaluated in adjuvant-induced arthritis model in rats and in glycosaminoglycan releasing inhibition assays.UP1304 demonstrated its enhanced significance by improving the major cardinal signs of arthritis in vivo and ex vivo.UP1304 could potentially be considered as a dietary supplement product for the management of arthritis.

Analgesic and anti-inflammatory effects of UP1304, a botanical composite containing standardized extracts of Curcuma longa and Morus alba.

OBJECTIVE: Though the initial etiologies of arthritis are multifactorial, clinically, patients share the prime complaints of the disease, pain. Here the authors assessed the analgesic and anti-inflammatory effects of UP1304, a composite that contains a standardized blend of extracts from the rhizome of Curcuma longa and the root bark of Morus alba, on rats with carrageenan-induced paw edema. METHODS: A plant library was screened for bradykinin receptor antagonists. In vivo, the anti-inflammatory and analgesic effects of the standardized composite, UP1304, were evaluated in rats with carrageenan-induced paw edema using oral dose ranges of 100-400 mg/kg. Ibuprofen, at a dose of 200 mg/kg, was used as a reference compound. In vitro, cyclooxygenase (COX) and lipoxygenase (LOX) inhibition assays were performed to evaluate the degree of inflammation. RESULTS: Statistically significant improvements in pain resistance and paw edema suppression were observed in animals treated with UP1304, when compared to vehicle-treated rats. Results from the highest dose of UP1304 (400 mg/kg) were similar to those achieved by ibuprofen treatment at 200 mg/kg. In vitro, UP1304 showed dose-dependent inhibition of the enzymatic activities of COX and LOX. A half-maximal inhibitory concentration of 9.6 µg/mL for bradykinin B1 inhibition was calculated for the organic extract of C. longa. Curcumin showed Ki values of 2.73 and 58 µg/mL for bradykinin receptors B1 and B2, respectively. CONCLUSION: Data presented here suggest that UP1304, analgesic and anti-inflammatory agent of botanical origin, acted as a bradykinin receptor B1 and B2 antagonist, and inhibited COX and LOX enzyme activities. This compound should be considered for the management of symptoms associated with arthritis.

Analgesic and anti-Inflammatory effect of UP3005, a botanical composition Containing two standardized extracts of Uncaria gambir and Morus alba.

BACKGROUND: Osteoarthritis (OA) is a chronic debilitating degenerative joint disease characterized by cartilage degradation and synovial inflammation exhibited by clinical symptoms such as joint swelling, synovitis, and inflammatory pain. Present day pain relief therapeutics heavily relies on the use of prescription and over the counter nonsteroidal anti-inflammatory drugs as the first line of defense where their long-term usage causes detrimental gastrointestinal and cardiovascular-related side-effects. As a result, the need for evidence based safer and efficacious alternatives from natural sources to overcome the most prominent and disabling symptoms of arthritis is a necessity. MATERIALS AND METHODS: Describe the anti-inflammatory and analgesic effect of UP3005, a composition that contains a standardized blend of two extracts from the leaf of Uncaria gambir and the root bark of Morus alba in carrageenan-induced rat paw edema, abdominal constriction (writhing's) and ear swelling assays in mouse with oral dose ranges of 100-400 mg/kg. RESULTS: In vivo, statistically significant improvement in pain resistance, and suppression of paw edema and ear thickness in animals treated with UP3005 were observed compared with vehicle-treated diseased rats and mice. Ibuprofen was used a reference compound in all the studies. In vitro, enzymatic inhibition activities of UP3005 were determined with IC50 values of 12.4 µg/ml, 39.8 µg/ml and 13.6 µg/ml in cyclooxygenase-2 (COX-1), COX-2 and lipoxygenase (5-LOX) enzyme activity assay, respectively. CONCLUSIONS: These data suggest that UP3005, analgesic and anti-inflammatory agent of botanical origin with balanced dual COX-LOX inhibition activity, could potentially be used for symptom management of OA.

UP3005, a Botanical Composition Containing Two Standardized Extracts of Uncaria gambir and Morus alba, Improves Pain Sensitivity and Cartilage Degradations in Monosodium Iodoacetate-Induced Rat OA Disease Model.

Osteoarthritis (OA) is a multifactorial disease primarily noted by cartilage degradation in association with inflammation that causes significant morbidity, joint pain, stiffness, and limited mobility. Present-day management of OA is inadequate due to the lack of principal therapies proven to be effective in hindering disease progression where symptomatic therapy focused approach masks the actual etiology leading to irreversible damage. Here, we describe the effect of UP3005, a composition containing a proprietary blend of two standardized extracts from the leaf of Uncaria gambir and the root bark of Morus alba, in maintaining joint structural integrity and alleviating OA associated symptoms in monosodium-iodoacetate- (MIA-) induced rat OA disease model. Pain sensitivity, micro-CT, histopathology, and glycosaminoglycans (GAGs) level analysis were conducted. Diclofenac at 10 mg/kg was used as a reference compound. UP3005 resulted in almost a complete inhibition in proteoglycans degradation, reductions of 16.6% (week 4), 40.5% (week 5), and 22.0% (week 6) in pain sensitivity, statistically significant improvements in articular cartilage matrix integrity, minimal visual subchondral bone damage, and statistically significant increase in bone mineral density when compared to the vehicle control with MIA. Therefore, UP3005 could potentially be considered as an alternative therapy from natural sources for the treatment of OA and/or its associated symptoms.

Antiplatelet and antithrombotic effect of Phyllostachys pubescens leaves and Mume Fructus combination.

BACKGROUND: Agents currently used for the treatment and prevention of thrombosis have a number of side effects. We conducted this study to develop antithrombotic agents from herbs that are used in food. METHODS: The 80% (v/v) ethanol extracts of Phyllostachys pubescens leaf (PL) and Mume Fructus (MF) and their combinations-2:1 (PM21), 1:1 (PM11), and 1:2 (PM12)-were evaluated on rat platelet aggregation induced by adenosine diphosphate (ADP) in vitro and on arteriovenous shunt thrombosis after 3 days of oral treatment in rats in vivo. RESULTS: At 100 µg/mL, PM21 and PM11 inhibited in vitro ADP-induced aggregation by 44.0 ± 4.3% and 30.0 ± 3.2%, respectively, whereas PL, MF, and PM12 weakly or scarcely inhibited ADP-induced aggregation by 3.9 ± 3.2%, 13.0 ± 2.7%, and 5.2 ± 1.3%, respectively. The IC50 values of PM21 on ADP-, collagen-, and thrombin-induced platelet aggregations were 135.6 ± 7.4 µg/mL, 142.7 ± 5.8 µg/mL, and 186.5 ± 9.7 µg/mL, respectively. In an in vivo rat arteriovenous-shunt thrombosis model, thrombus weight was significantly decreased after the oral administration of 400 mg/kg PL (27.8 ± 3.0%, p < 0.01) or MF (35.2 ± 2.1%, p < 0.01), and with a good accord to the in vitro results, the combination of PL and MF in the ratio of 2:1, PM21 (60.9 ± 1.2%, p < 0.001), showed a superior antithrombotic effect to those of individual extracts. At dosages of 200 mg/kg, 100 mg/kg, and 50 mg/kg, PM21 dose-dependently decreased thrombosis weight (ED50, 314 mg/kg). CONCLUSION: These results suggest that combination preparations of PL and MF, especially their 2:1 combination, can increase antiplatelet and antithromboticeffects more than PL and MF alone, offering evidence for a potential novel combination antithrombotic therapy.

Antiallergic herbal composition from Scutellaria baicalensis and Phyllostachys edulis.

We aimed to find antiallergic agents from natural sources using mast cells activated during allergic reaction. We screened over 2000 plants for blockade of histamine release and identified two of them, S. baicalenesis and P. edulis. Bioassay-guided fractionation led to two main constituent flavonoids, baicalin from S. baicalenesis roots and isoorientin from P. edulis leaves. Based on these two compounds, two standardized extracts (SSBE and SPEE) and a combined standardized herb composition (SHC) were developed. SSBE, SPEE, and SHC remarkably inhibited histamine and leukotriene release from mast cells activated by anti-OVA/OVA binding, and SHC showed a stronger inhibition than either extract alone. SHC also showed greater inhibition potency than either aspirin or cromolyn, which are known antiallergic agents. Our results suggest that SHC reduce degranulation during mast cell activation and could be a promising candidate for the treatment of immune/allergic diseases related to mast cells.

Water-soluble polysaccharide from Eleutherococcus senticosus stems attenuates fulminant hepatic failure induced by D-galactosamine and lipopolysaccharide in mice.

The aim of this study was to investigate whether Eleutherococcus senticosus stems could attenuate D-galactosamine/lipopolysaccharide-induced fulminant hepatic failure in mice. E. senticosus, known as Siberian ginseng, is a popular folk medicine used as a tonic in Asia. Preparations of E. senticosus used in this study were as follows; (i) 70% ethanol extract (ii) water extract (iii) ethanol-soluble part of the water extract (iv) polysaccharide obtained as an 80% ethanol insoluble of the water extract. Preparations were given by intraperitoneal (300 mg/kg and 50 mg/kg) or oral (300 mg/kg) injection at 12 hr and 1 hr before a D-galactosamine/lipopolysaccharide injection. The intraperitoneal injection of water extract and polysaccharide significantly lowered serum levels of tumour necrosis factor-alpha, aspartate transaminase and alanine transaminase, improved the histologic changes in liver, inhibited hepatocyte apoptosis confirmed by the terminal deoxynucleotidyl transferase-mediated dUTP nick end-labeling method and DNA fragmentation assay, and suppressed the lethality induced by D-galactosamine/lipopolysaccharide. The oral administration of water extract and polysaccharide also reduced serum aspartate transaminase, alanine transaminase and tumour necrosis factor-alpha levels. In contrast 70% ethanol extract and ethanol-soluble part of the water extract had no protective effect when treated intraperitoneally or orally. These results indicate E. senticosus stems attenuate fulminant hepatic failure induced by D-galactosamine/lipopolysaccharide in mice and the protective effect is due to water-soluble polysaccharides in E. senticosus stems.

Effect of Acanthopanax koreanum Nakai (Araliaceae) on D-galactosamine and lipopolysaccharide-induced fulminant hepatitis.

The hepatoprotective effects of Acanthopanax koreanum Nakai (Araliaceae) were evaluated in D-galactosamine/lipopolysaccharide-induced fulminant hepatic failure in mouse. Preparations of Acanthopanax koreanum used were an ethanol extract, a water extract, and the ethanol-soluble and ethanol-insoluble components of the water extract of roots or stems of the plant. Mice were pretreated with various extracts by intraperitoneal injection or orally, 12 and 1 h before intraperitoneal injection of D-galactosamine and lipopolysaccharide (LPS). Intraperitoneal pretreatment with the water extract or the ethanol-insoluble component of the water extract markedly reduced the elevated levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), and tumor necrosis factor-alpha (TNF-alpha), reduced the histological changes in the liver, and attenuated hepatocyte apoptosis confirmed by the terminal deoxynucleotidyl transferase-mediated dUTP nick end-labeling method and DNA fragmentation assay. Oral pretreatment with the ethanol-insoluble component of the water extract also reduced serum AST, ALT, and TNF-alpha levels. The present study shows that the ethanol-insoluble component of a water extract from Acanthopanax koreanum has a protective effect against the induction of fulminant hepatitis in mice by D-galactosamine and lipopolysaccharide.

Lignans from Saururus chinensis inhibiting the transcription factor NF-kappaB.

The sesquineolignans, saucerneol D and saucerneol E were isolated from the roots of Saururus chinensis together with four known lignans, manassantin A, manassantin B, (-)-saucerneol methyl ether, and (+)-saucernetin. Structure elucidation was based on the analysis of spectroscopic data and anti-inflammatory activity was studied using HeLa cells transfected with NF-kappaB reporter construct. All compounds except for (+)-saucernetin inhibited NF-kappaB dependent reporter gene expression with IC50 values of 2.5-16.9 microM.

Two new furanoditerpenes from Saururus chinenesis and their effects on the activation of peroxisome proliferator-activated receptor gamma.

Two new acyclic furanoditerpene compounds, saurufuran A (1) and B (2), were obtained from the root of Saururus chinensis, and their structures were elucidated by means of 1D and 2D NMR spectroscopic analyses. Saurufuran A (1) is effective on the activation of peroxisome proliferator-activated receptor gamma (PPARgamma) with an EC(50) value of 16.7 microM; however, saurufuran B (2), with an EC(50) value of >100 microM, weakly activated the PPARgamma.