The prevalence of obesity has increased and is a health concern worldwide.Due to the concerns regarding synthetic anti-obesity treatments,nowadays natural products become a trend.Previous studies proved that there is ...The prevalence of obesity has increased and is a health concern worldwide.Due to the concerns regarding synthetic anti-obesity treatments,nowadays natural products become a trend.Previous studies proved that there is a potential to use marine algae as anti-obesity agents.Therefore,in this study,the lipid inhibitory effect of crude polysaccharide of amyloglucosidase-assisted hydrolysate from Sargassum thunbergii(STAC)and its fucoidan fractions(STAFs)on 3T3-L1 cells and high-fat diet(HFD)-induced obese mice were investigated.According to the results,the STAF3,showed the highest xylose content and exhibited significant inhibitory effects on lipid accumulation by downregulating adipogenic and lipogenic proteins in 3T3-L1 cells.Furthermore,oral supplementation with STAC significantly declined gain in body weight and fat weight,and serum lipid contents in an HFD-induced obesity mouse model.Structural and chemical characterizations demonstrated that puritied STAF3 has consistent surface morphology and small particle size,with similar structural characteristics as commercial fucoidan.Together,these results indicate that STAC and purified STAF3 from Sargassum thunbergia is a potent source to develop as ananti-obesity agents or functional food products to counter obesity.展开更多
Although it is not generally a life-threatening disease,obesity is becoming a major health problem worldwide.It can be controlled by means of drugs,and,consequently,these are required to be safe as well as effective.I...Although it is not generally a life-threatening disease,obesity is becoming a major health problem worldwide.It can be controlled by means of drugs,and,consequently,these are required to be safe as well as effective.In this paper,we summarize the fate of various drugs that have been introduced for clinical use in the treatment of obesity.Fenfluramine and dexfenfluramine were withdrawn because of heart valve damage.Sibutramine suppresses appetite and increases heart rate and blood pressure.In the Sibutramine Cardiovascular OUTcomes trial,an increase in major adverse cardiovascular events prompted its withdrawal in Europe and the United States.Rimonabant is an endocannabinoid receptor antagonist that reduces body weight and ameliorates some cardiovascular risk factors.However,adverse psychiatric side effects led to its withdrawal as well.Orlistat is approved in Europe and the United States for the treatment of obesity,but its use is limited by gastrointestinal side-effects.Ephedrine and caffeine are natural ingredients in foods and supplements that may help the person to lose weight.In the light of several failed attempts,there is a clear need to develop drugs that are effective and safe in the long term in order to successfully combat the phenomenon of obesity.展开更多
Pu-erh tea, a traditional Chinese beverage, has been believed to have many benefits to human health and without side effects. In this study, we systematically analyzed the main active components of Pu-erh tea and inve...Pu-erh tea, a traditional Chinese beverage, has been believed to have many benefits to human health and without side effects. In this study, we systematically analyzed the main active components of Pu-erh tea and investigated its anti-obesity, anti-atherosclerotic and anti-oxidant effects using an obese rat model. Obesity was induced by feeding a high-fat diet and subsequently the experimental obese mice were fed with high-fat diet supplemented with low (2.5%), medium (5%) or high (7.5%) doses of Pu-erh tea powder for 6 weeks respectively. As result, the body weight gain of the rats was decreased by medium and high doses of Pu-erh tea treatments. Furthermore, the levels of serum total cholesterol (TC), triglyceride (TG) and atherosclerosis index (AI) were significantly lowered by Pu-erh tea compared to the control group. Conversely, high density lipoproteincholesterol (HDL-C) level of the rats was significantly elevated by Pu-erh tea treatments. In addition, Pu-erh tea treatments increased the activities of anti-oxidative enzymes such as superoxide dismutase (SOD) and glutathione peroxides (GSH-Px), whereas reduced the level of lipid peroxidation product malondialdehyde (MDA) in obese rats. Collectively, our find-ings revealed that Pu-erh tea exerts comprehensive benefits in anti-obesity, anti-atherosclerotic and anti-oxidant effects, therefore can be used as a promising functional food in obesity management.展开更多
Mesotherapy and anti-obesity medications are gradually gaining worldwide popularity for purposes of body contouring and weight loss.Their adverse effects are various,but there is a tendency to disregard them.Ischemic ...Mesotherapy and anti-obesity medications are gradually gaining worldwide popularity for purposes of body contouring and weight loss.Their adverse effects are various,but there is a tendency to disregard them.Ischemic colitis is one of the most common diseases associated with non-obstructive blood vessel disorders.However,there have been no case reports about the adverse effects resulting from mesotherapy only or in combination with anti-obesity medications.We report on an interesting case of ischemic colitis after mesotherapy combined with anti-obesity medications in a 39-year-old female who had no risk factors.展开更多
Objective To further explore associated effects of Lactobacillus plantarum dy-1(LFBE) on obesity and lipid metabolism at the gene expression level, the expression of micro RNAs(mi RNAs) was investigated in the liver o...Objective To further explore associated effects of Lactobacillus plantarum dy-1(LFBE) on obesity and lipid metabolism at the gene expression level, the expression of micro RNAs(mi RNAs) was investigated in the liver of high-fat diet(HFD) induced obese rats.Methods Three groups of animal models were established. Changes in mi RNA expression in the liver of each group were analyzed by microarray and RT-q PCR, complemented by bioinformatics. Palmitateinduced hepatocellular carcinoma(Hep G2) cells were used as a model to validate the test.Results LFBE treatment groups and HFD groups were observed to be distinctly different with respect to rates of increase in body weight and body fat percentage and triglyceride(TG) and total cholesterol(TC) levels in serum and liver. In addition, the LFBE group showed upregulation of ten mi RNAs and downregulation of five mi RNAs in the liver. Downregulation of mi R-34 a and mi R-212 was observed in the livers of the LFBE group. Gene ontology and kyoto encyelopedia of geues and genomes(KEGG)pathway analysis showed that possible target genes of the deregulated mi RNAs were significantly enriched in the adrenergic and HIF-1 signaling pathways.Conclusion These results demonstrate that LFBE might regulate the expression of mi RNAs in order to inhibit obesity and fatty liver.展开更多
Semicarbazide-sensitive amine oxidase ( SSAO) has been considered to be associated with the metabolism of glucose and fat,and elevated SSAO activity was observed in obese patients. In the present study,an in vitro SSA...Semicarbazide-sensitive amine oxidase ( SSAO) has been considered to be associated with the metabolism of glucose and fat,and elevated SSAO activity was observed in obese patients. In the present study,an in vitro SSAO activity-based method was developed to screen inhibitors from 1 5 anti-obesity drugs. Among the fifteen anti-obesity drugs,four drugs including caffeine,fenfluramine, bumetanide and amfebutamone inhibited SSAO activity,and caffeine was the most effective one. When the concentration of caffeine was 1 . 4 mmol / L,the inhibition ratio was 3 1 . 9 % and 1 8 . 8 % in rabbit serum and rat adipose tissue,respectively. Inhibition of SSAO activity by caffeine was also confirmed in the in vivo study,showing the inhibition ratio of 1 5 . 6 % on serum SSAO. Caffeine provides a natural source of inhibition of SSAO activity and may be a promising inhibitor for the study of SSAO.展开更多
As a dark tea,Pu-erh tea(PET)is produced from sun-dried leaves of Camellia sinensis var.assamica mainly in Yunnan Province of China.Many microorganisms are involved in the fermentation of PET.Among them,Aspergillus ni...As a dark tea,Pu-erh tea(PET)is produced from sun-dried leaves of Camellia sinensis var.assamica mainly in Yunnan Province of China.Many microorganisms are involved in the fermentation of PET.Among them,Aspergillus niger is most important.It is believed that the longer the preservation period,the better is the quality and taste of PET,which is commercially available as loose,compressed or instant tea leaves.Chemical components of PET include flavones,flavanols,flavonols,phenolic acids,alkaloids and methylxanthines.In this overview,the lipid-lowering and anti-obesity effects of PET were discussed based on animal models and human trials,and our study provided some insights into possible mechanisms of bioactive compounds,such as theabrownin,catechins,lovastatin and gallic acid.Other bioactivities of PET and some information on Fuzhuan brick tea were also included.Sources of information cited were from Google Scholar,Pub Med,Pub Med Central,Science Direct,J-Stage,Pub Chem,Directory of Open Access Journals(DOAJ),and China National Knowledge Infrastructure(CNKI).展开更多
This study investigated hypolipidemic,weight-reducing,and hepatoprotective effects of Antrodia cinnamomea mycelial extract obtained from solid-state culture(ACME)in an HFr D-induced obese/hyperlipidemic mouse model.Fo...This study investigated hypolipidemic,weight-reducing,and hepatoprotective effects of Antrodia cinnamomea mycelial extract obtained from solid-state culture(ACME)in an HFr D-induced obese/hyperlipidemic mouse model.Following 4-week ACME treatment,body weight,epididymal fat index,and some serum biochemical indices were measured.Expression levels of some related genes involved in cholesterol and lipid metabolism were analyzed by q RT-PCR.Moreover,histological studies of hepatic tissues were also conducted.After ACME treatment,body weight and epididymal fat index were significantly lower than that in model control group.ACME and simvastatin significantly reduced serum total cholesterol(T-CHO)and low-density lipoprotein cholesterol(LDL-C)levels,and increased high-density lipoprotein cholesterol(HDL-C)level.Subsequent experiments showed that:(i)ACME regulated transcriptional expression of 3-hydroxy-3-methylglutaryl-Co A reductase(HMGR),low-density lipoprotein receptor(LDLR),adipose triglyceride lipase(ATGL),and fatty acid synthase(FAS),with consequent reduction of blood lipid levels and body weight;(ii)ACME enhanced total antioxidant capacity(T-AOC)and superoxide dismutase(SOD)activity in hepatic tissues;(iii)ACME reduced malondialdehyde(MDA)level and ameliorated lipid oxidative damage in liver.Our findings indicate that ACME is a strong candidate for development as a novel anti-hyperlipidemia and anti-obesity health product.展开更多
This study aimed to elucidate the inhibition mechanism of apigenin against porcine pancreatic lipase(PPL),and,moreover,to comprehensively reveal the molecular basis of its anti-obesity via network pharmacology approac...This study aimed to elucidate the inhibition mechanism of apigenin against porcine pancreatic lipase(PPL),and,moreover,to comprehensively reveal the molecular basis of its anti-obesity via network pharmacology approach.The results showed that apigenin inhibited PPL with an IC50 value of 0.377±0.041 mM.Spectroscopic techniques combined molecular docking suggested that apigenin could bind into the PPL active pocket,affecting its normal spatial conformation.Moreover,molecular dynamic(MD)simulations revealed that the open conformation of PPL tended to transit to the closed in the presence of apigenin,which might one important reason for the inhibition of PPL catalytic ability.Network pharmacology analysis revealed that a total of 49 proteins could be identified as potential targets for the anti-obesity effects of apigenin.According to the protein-protein interaction(PPI)network analysis,six hub targets were extracted including IGF1,ESR1,MMP9,PPARA,MAPK14 and NR3C1.Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway enrichment indicated that the 49 potential targets could be mapped to 30 pathways(p<0.05).Among them,PI3K-Akt signaling pathway and insulin resistance can be considered as two major pathways regulated by apigenin.Further docking studies indicated that apigenin can bind into the binding pocket of the six hub target proteins identified according to the PPI network.The results indicated that in addition to inhibiting PPL,apigenin could exhibit anti-obesity benefit through the molecular mechanisms uncovered by network pharmacology.This study proposes a new strategy to reveal the mechanisms of dietary polyphenols at the level of network pharmacology.展开更多
The worldwide obesity epidemic has imposed human being a huge burden and attention had been drawn to manipulating the lactic acid bacteria (LAB) to improve obesity symptoms.In this study,a more comprehensive and relia...The worldwide obesity epidemic has imposed human being a huge burden and attention had been drawn to manipulating the lactic acid bacteria (LAB) to improve obesity symptoms.In this study,a more comprehensive and reliable in vitro method was established to screen LAB with greater potential against obesity.Firstly,twenty-eight human feces-derived LAB strains were selected by assessing bile salt-acid tolerance and cholesterol lowering capacity.Subsequently,the triglyceride lowering capacity,bile salt hydrolase (BSH) activity,α-glucosidase activity inhibition capacity and Enterobacter cloacae (E.cloacae) growth inhibition capacity were tested for further evaluating the anti-obesity properties of LAB strains.Principal component analysis (PCA) of these results indicated that Limosilactobacillus reuteri (L.reuteri) NCUH003,Lactiplantibacillus plantarum (L.plantarum) NCUH046 and Limosilactobacillus fermentum (L.fermentum) NCUH068 exhibited favorable anti-obesity properties.Besides,the LAB displayed good gastrointestinal adaptability and antioxidant activity but no hemolytic activity,and they were sensitive to various antibiotics.These results indicated that L.reuteri NCUH003,L.plantarum NCUH046 and L.fermentum NCUH068 are potential for application in obesity treatment.展开更多
Objective:To investigate antioxidant and anti-obesity activity of flavonoids extracted by solvent cold percolation and preparative thin liquid chromatography from Dioscorea steriscus tubers.Methods:1-diphenyl-2-picryl...Objective:To investigate antioxidant and anti-obesity activity of flavonoids extracted by solvent cold percolation and preparative thin liquid chromatography from Dioscorea steriscus tubers.Methods:1-diphenyl-2-picrylhydrazyl(DPPH)antiradical activity was employed to investigate antioxidant activity while chromogenic method was used to determine alpha amylase inhibition activity and spectrophotometric methods using triolein as a substrate was used to investigate lipase activity.Results:Thin liquid chromatography profiling revealed eight different flavonoid types.Ethyl acetate extract yielded two types,R_(f) values 0.38 and 0.40;chloroform extract also yielded two types R_(f) values 0.06 and 0.51,while ethanol extract yielded four types with R_(f) values 0.16,0.33,0.65 and 0.96.All the extracted flavonoids exhibited antioxidant activity with ethanol extracts exhibiting the greatest antiradical activity.The order of enzyme inhibition capacity was ethyl acetate<chloroform<ethanol.Ethanol extract exhibited significantly greater anti-obesity activity as compared to herbex,a commercially anti-obesity medication sold in drug stores.Anti-α amylase activity and anti-lipase activity for herbex was(78.38±0.02)%and(76.07±0.09)%respectively,while that for ethanolic extract(R_(f)=0.96)was(93.66±0.00)%and(95.88±0.13)%.Conclusions:Results of the present study show that Dioscorea steriscus consists of bioactive compounds that can act as lipase andα-amylase inhibitors and therefore can be useful for the development of functional foods against obesity.It can also be used as a source of lead compounds for designing new ant-obesity therapeuticals.展开更多
Obesity is associated with several diseases,including mental health.Adipose tissue is distributed around the internal organs,acting in the regulation of metabolism by storing and releasing fatty acids and adipokine in...Obesity is associated with several diseases,including mental health.Adipose tissue is distributed around the internal organs,acting in the regulation of metabolism by storing and releasing fatty acids and adipokine in the tissues.Excessive nutritional intake results in hypertrophy and proliferation of adipocytes,leading to local hypoxia in adipose tissue and changes in these adipokine releases.This leads to the recruitment of immune cells to adipose tissue and the release of pro-inflammatory cytokines.The presence of high levels of free fatty acids and inflammatory molecules interfere with intracellular insulin signaling,which can generate a neuroinflammatory process.In this review,we provide an up-to-date discussion of how excessive obesity can lead to possible cognitive dysfunction.We also address the idea that obesity-associated systemic inflammation leads to neuroinflammation in the brain,particularly the hypothalamus and hippocampus,and that this is partially responsible for these negative cognitive outcomes.In addition,we discuss some clinical models and animal studies for obesity and clarify the mechanism of action of anti-obesity drugs in the central nervous system.展开更多
Objective:To explore the anti-obesity effects and the mechanism of action of Monascus pilosus(M.pilosus)-fermented black soybean(MFBS)extracts(MFBSE)and MFBS powders(MFBSP)in adipocytes and high-fat diet(HFD)-induced ...Objective:To explore the anti-obesity effects and the mechanism of action of Monascus pilosus(M.pilosus)-fermented black soybean(MFBS)extracts(MFBSE)and MFBS powders(MFBSP)in adipocytes and high-fat diet(HFD)-induced obese mice,respectively.Methods:Black soybean was fermented with M.pilosus,and the main constituents in MFBS were analyzed by HPLC analysis.In vitro,MFBSE were examined for anti-adipogenic effects using Oil-Red O staining.In vivo,mice were fed a normal-fat diet(NFD)control,HFD control or HFD containing 1 g/kg MFBSP for 12 weeks,and then body weight gain and tissues weight measured.Real-time PCR and western blot assay were used to determine the mechanism of anti-adipogenic effects.Results:MFBSE inhibited lipid accumulation in 3T3-L1 adipocytes without exerting cell cytotoxicity.MFBSP treatment in HFD-fed mice significantly decreased the body weight gain compared with the HFD control mice.MFBSE and MFBSP treatment resulted in significantly lower mRNA levels of adipogenesis-related genes,such as peroxisome proliferator-activated receptorγ(PPARγ),fatty acid-binding protein 4(FABP4),and fatty acid synthase(FAS),in adipocytes and in white adipose tissue(WAT)of HFD-induced obese mice.Conclusions:These results suggest that the anti-obesity effects of MFBS are elicited by regulating the expression of adipogenesis-related genes in adipocytes and WAT of HFDinduced obese mice.展开更多
High sucrose content in traditional hawthorn leathers limits the potential consumption, particularly for elders and diabetics. In this study, sucrose-free hawthorn leathers were formulated with 75% fructooligosacchari...High sucrose content in traditional hawthorn leathers limits the potential consumption, particularly for elders and diabetics. In this study, sucrose-free hawthorn leathers were formulated with 75% fructooligosaccharides(FOS) and 25% xylooligosaccharides(XOS)(HLF75), which exhibited comparable morphology and sensory properties to the traditional ones. Then, the anti-obesity activity of HLF75 was investigated using high-fat diet(HFD) fed C57BL/6J mice. Comparing with traditional hawthorn leathers, HLF75 supplementation in HFD significantly decreased the levels of blood glucose and serum lipid. The histomorphologies of liver and subcutaneous fat tissues were ameliorated by HLF75, as well as the down-regulated m RNA expression levels of IL-1β, Nos2 and Cox-2 in the liver. M oreover, the protein levels of M y D88 and NF-κB in the liver were suppressed by HLF75 treatment with decreased F4/80-positive macrophage number. Ho wever, the expression levels of PI3K, phosphorylated-AKT(Thr308), and phosphorylated-m TOR(Ser2448) proteins related to glucose metabolism were increased in the liver. Moreover, fat synthesis-related gene expression in HLF75-fed mice was suppressed while expressions of lipolysis genes were improved. Thus, HLF75 supplementation alleviated HFD-induced obesity through the alleviation of inflammation and restoration of the disturbed glucose and lipid metabolism. Functional oligosaccharides could be effective sucrose substitutes in hawthorn leathers and enable their potential utilization as functional foods.展开更多
Background:Chinese medicine has been proposed as a novel approach to the prevention of metabolic disorders such as obesity.Danggui Buxue decoction,a decoction prepared from Huangqi(Astragali Radix)and Danggui(Angelica...Background:Chinese medicine has been proposed as a novel approach to the prevention of metabolic disorders such as obesity.Danggui Buxue decoction,a decoction prepared from Huangqi(Astragali Radix)and Danggui(Angelicae Sinensis Radix),has been used to nourish vitality and enhance blood circulation in traditional Chinese medicine.However,the effect of Danggui Buxue decoction on obesity is still primarily unknown.Methods:Cell proliferation,differentiation,and apolipoprotein-IV transcription were investigated to explore the function of Danggui Buxue decoction by methyl thiazolyl tetrazolium assay,alkaline phosphatase assay,and luciferase assay,respectively.Results:Danggui Buxue decoction promoted cell growth by up to 15%(P=0.034)and induced cell differentiation by up to 38%(P=0.006)at 0.3 mg/mL.Moreover,Danggui Buxue decoction enhanced the transcription of apolipoprotein-IV by 2.4 times(P=0.027),activating its promoter by 28.9%(P=0.031)at 0.3 mg/mL.In addition,Danggui Buxue decoction functioned in a dose-dependent manner.Conclusion:These results suggest that Danggui Buxue decoction promotes cell differentiation by enhancing apolipoprotein-IV transcription and alkaline phosphatase activity,and it may also have a potential anti-obesity effect because apolipoprotein-IV transcription is closely related to the reduction of food intake.展开更多
The methanol extract of grains of paradise (GP), the seed of Aframomum melegueta, which is distributed throughout West Africa, was administered during an animal breeding test. The extract suppressed body weight gain a...The methanol extract of grains of paradise (GP), the seed of Aframomum melegueta, which is distributed throughout West Africa, was administered during an animal breeding test. The extract suppressed body weight gain and decreased the weight of adipose tissues in breeding mice, with a greater effect on mice fed a high-fat diet (HFD) than on those fed a normal diet (ND). Other significant effects of GP intake included increased serum triglyceride (TG) concentration and reduced hepatic total cholesterol (TC) and TG concentrations. GP intake markedly prevented fat accumulation and improved hepatic lipid metabolism in HFD-fed mice. In addition, GP extract at a dosage of 5 mg/kg body weight decreased sympathetic nerve activity (SNA) in brown adipose tissue (BAT), while capsaicin, a major component of chili pepper, activated BAT SNA. This suggested that GP exerts a potential anti-obesity effect by a different mechanism from that of capsaicin.展开更多
The main aim of this study is to determine the anti-hyerlipidemic and anti-obesity activity of Canephora robusta in hyperlipidemia induced rats. Prepared coffee bean extract (GCE) was procured from the market which is...The main aim of this study is to determine the anti-hyerlipidemic and anti-obesity activity of Canephora robusta in hyperlipidemia induced rats. Prepared coffee bean extract (GCE) was procured from the market which is unroasted and contains more quantity of caffeine and chlorogenic acid when compared to roasted coffee. Male albino Wister rats are fed with high fat diet (HFD) for weeks to induce hyperlipidemia in rats, which are divided into 4 groups with 4 animals in each group. Test GCBE was given in doses of 200 mg/kg and 400 mg/kg to III and IV groups which are fed with HFD for 30 days. Then blood samples were collected through retro-orbital sinus by capillaries and serum is separated for analysis. The result obtained from lipid profile which includes total cholesterol, triglycerides, very low density lipoproteins, and low density lipoproteins shows the decreased level when compared to the hyperlipidemic control. This shows the significant reduction of total body weight (p < 0.05) when given with dose of 200 mg/kg and 400 mg/kg. The present study suggests that GCBE has anti-obesity and anti-hyperlipidemic activity, where 400 mg/kg is more effective to reduce the total body weight and lipid levels when compared to 200 mg/kg. Further studies on this extract may lead to identify the possible mechanism of action and isolation of active principle from the same.展开更多
Obesity,characterized by the dysregulation of energy balance in adipose tissue and other metabolic organs,is frequently accompanied by chronic low-grade inflammation.As long-acting insulin sensitizers,the organically-...Obesity,characterized by the dysregulation of energy balance in adipose tissue and other metabolic organs,is frequently accompanied by chronic low-grade inflammation.As long-acting insulin sensitizers,the organically-derivatized polyoxovanadates(POVs),can extend the dosing interval of antidiabetic drugs from hourly to almost daily.In this work,the protective activity of POVs is investigated by an eight-week in vivo experiment,in which a small amount of POVs was administrated orally to a mouse model of dietinduced obesity every day.The present study shows that administration of POVs significantly decreases the body weight of mice,reduces adipose tissue accumulation,and simultaneously reduces adipose tissue inflammation.In addition,the anti-obesogenic population of i NKT cells is protected potentially by POVs,which subsequently alleviates visceral adipose tissue inflammation in high-fat-diet(HFD)-fed mice against diet-induced obesity.By contrast,the change in body weight after POV treatment is the result of a substantial reduction in fat mass,with no obvious effects on lean body mass.These findings demonstrate that supplementary of POVs would be an effective way to combat obesity and metabolic disorders while lowering metabolic inflammation.展开更多
5-Hydroxytryptamine 2C(5-HT2C) receptor is one of the major targets of anti-obesity agents, due to its role in regulation of appetite. In the present study, the 70% EtO H extract of the roots of Bupleurum chinense was...5-Hydroxytryptamine 2C(5-HT2C) receptor is one of the major targets of anti-obesity agents, due to its role in regulation of appetite. In the present study, the 70% EtO H extract of the roots of Bupleurum chinense was revealed to have agonistic activity on 5-HT2 C receptor, and the subsequent bioassay-guided isolation led to identification of several saikosaponins as the active constituents with 5-HT2 C receptor agonistic activity in vitro and anti-obesity activity in vivo. The new compound, 22-oxosaikosaponin d(1), was determined by extensive spectroscopic analyses(HR-ESI-MS, IR, and 1D and 2D NMR). The primary structure-activity relationship study suggested that the intramolecular ether bond between C-13 and C-28 and the number of sugars at C-3 position were closely related to the 5-HT2 C receptor agonistic activity. Saikosaponin a(3), the main saponin in B. chinense, showed obviously agonistic activity on 5-HT2 C receptor with an EC50 value of 21.08 ± 0.33 μmol×L^(–1) in vitro and could reduce food intake by 39.1% and 69.2%, and weight gain by 13.6% and 16.4%, respectively, at 3.0 and 6.0 mg×kg^(–1) in vivo. This investigation provided valuable information for the potential use of B. chinense as anti-obesity agent.展开更多
The present study was designed to synthesize and evaluate a series of benzylisoquinoline derivatives. These compounds were synthesized by Bischler-Napieralski cyclization to yield 1-benzyl-3,4-dihydroisoquinolines, an...The present study was designed to synthesize and evaluate a series of benzylisoquinoline derivatives. These compounds were synthesized by Bischler-Napieralski cyclization to yield 1-benzyl-3,4-dihydroisoquinolines, and the products were obtained by reductions. All these compounds were identified by MS, 1H NMR and 13 C NMR. The inhibitory activities on pancreatic lipase and preadipocyte proliferation for the synthesized compounds and alkaloids from Nulembo nucifera were assessed in vitro. Most of the compounds showed inhibitory activities on both pancreatic lipase and preadipocyte proliferation. Particularly, compounds 7p-7u and 9d-9f exhibited significant inhibitory activity on pancreatic lipase while compounds 7c, 7d, 7f, 7g, 7i, and 7j potently inhibited the proliferation of 3T3-L1 preadipocytes. Our results provided a basis for future evaluation and development of these compounds as leads for therapeutics for human diseases.展开更多
基金The“Basic Science Research Program”extended its support via the National Research Foundation of Korea (NRF),which is sponsored through the Ministry of Education (2018R1C1B6004780)supported by Main Research Program (E0211200-03)of the Korea Food Research Institute (KFRI)funded by the Ministry of Science and ICT。
文摘The prevalence of obesity has increased and is a health concern worldwide.Due to the concerns regarding synthetic anti-obesity treatments,nowadays natural products become a trend.Previous studies proved that there is a potential to use marine algae as anti-obesity agents.Therefore,in this study,the lipid inhibitory effect of crude polysaccharide of amyloglucosidase-assisted hydrolysate from Sargassum thunbergii(STAC)and its fucoidan fractions(STAFs)on 3T3-L1 cells and high-fat diet(HFD)-induced obese mice were investigated.According to the results,the STAF3,showed the highest xylose content and exhibited significant inhibitory effects on lipid accumulation by downregulating adipogenic and lipogenic proteins in 3T3-L1 cells.Furthermore,oral supplementation with STAC significantly declined gain in body weight and fat weight,and serum lipid contents in an HFD-induced obesity mouse model.Structural and chemical characterizations demonstrated that puritied STAF3 has consistent surface morphology and small particle size,with similar structural characteristics as commercial fucoidan.Together,these results indicate that STAC and purified STAF3 from Sargassum thunbergia is a potent source to develop as ananti-obesity agents or functional food products to counter obesity.
文摘Although it is not generally a life-threatening disease,obesity is becoming a major health problem worldwide.It can be controlled by means of drugs,and,consequently,these are required to be safe as well as effective.In this paper,we summarize the fate of various drugs that have been introduced for clinical use in the treatment of obesity.Fenfluramine and dexfenfluramine were withdrawn because of heart valve damage.Sibutramine suppresses appetite and increases heart rate and blood pressure.In the Sibutramine Cardiovascular OUTcomes trial,an increase in major adverse cardiovascular events prompted its withdrawal in Europe and the United States.Rimonabant is an endocannabinoid receptor antagonist that reduces body weight and ameliorates some cardiovascular risk factors.However,adverse psychiatric side effects led to its withdrawal as well.Orlistat is approved in Europe and the United States for the treatment of obesity,but its use is limited by gastrointestinal side-effects.Ephedrine and caffeine are natural ingredients in foods and supplements that may help the person to lose weight.In the light of several failed attempts,there is a clear need to develop drugs that are effective and safe in the long term in order to successfully combat the phenomenon of obesity.
文摘Pu-erh tea, a traditional Chinese beverage, has been believed to have many benefits to human health and without side effects. In this study, we systematically analyzed the main active components of Pu-erh tea and investigated its anti-obesity, anti-atherosclerotic and anti-oxidant effects using an obese rat model. Obesity was induced by feeding a high-fat diet and subsequently the experimental obese mice were fed with high-fat diet supplemented with low (2.5%), medium (5%) or high (7.5%) doses of Pu-erh tea powder for 6 weeks respectively. As result, the body weight gain of the rats was decreased by medium and high doses of Pu-erh tea treatments. Furthermore, the levels of serum total cholesterol (TC), triglyceride (TG) and atherosclerosis index (AI) were significantly lowered by Pu-erh tea compared to the control group. Conversely, high density lipoproteincholesterol (HDL-C) level of the rats was significantly elevated by Pu-erh tea treatments. In addition, Pu-erh tea treatments increased the activities of anti-oxidative enzymes such as superoxide dismutase (SOD) and glutathione peroxides (GSH-Px), whereas reduced the level of lipid peroxidation product malondialdehyde (MDA) in obese rats. Collectively, our find-ings revealed that Pu-erh tea exerts comprehensive benefits in anti-obesity, anti-atherosclerotic and anti-oxidant effects, therefore can be used as a promising functional food in obesity management.
文摘Mesotherapy and anti-obesity medications are gradually gaining worldwide popularity for purposes of body contouring and weight loss.Their adverse effects are various,but there is a tendency to disregard them.Ischemic colitis is one of the most common diseases associated with non-obstructive blood vessel disorders.However,there have been no case reports about the adverse effects resulting from mesotherapy only or in combination with anti-obesity medications.We report on an interesting case of ischemic colitis after mesotherapy combined with anti-obesity medications in a 39-year-old female who had no risk factors.
基金supported by the priority academic program development of Jiangsu Higher Education institutionsthe National Natural Science Foundation of China [31801538]
文摘Objective To further explore associated effects of Lactobacillus plantarum dy-1(LFBE) on obesity and lipid metabolism at the gene expression level, the expression of micro RNAs(mi RNAs) was investigated in the liver of high-fat diet(HFD) induced obese rats.Methods Three groups of animal models were established. Changes in mi RNA expression in the liver of each group were analyzed by microarray and RT-q PCR, complemented by bioinformatics. Palmitateinduced hepatocellular carcinoma(Hep G2) cells were used as a model to validate the test.Results LFBE treatment groups and HFD groups were observed to be distinctly different with respect to rates of increase in body weight and body fat percentage and triglyceride(TG) and total cholesterol(TC) levels in serum and liver. In addition, the LFBE group showed upregulation of ten mi RNAs and downregulation of five mi RNAs in the liver. Downregulation of mi R-34 a and mi R-212 was observed in the livers of the LFBE group. Gene ontology and kyoto encyelopedia of geues and genomes(KEGG)pathway analysis showed that possible target genes of the deregulated mi RNAs were significantly enriched in the adrenergic and HIF-1 signaling pathways.Conclusion These results demonstrate that LFBE might regulate the expression of mi RNAs in order to inhibit obesity and fatty liver.
基金Supported by the Ministry of Science and Technology of China(2008AA12A218 2009BAK59B01)
文摘Semicarbazide-sensitive amine oxidase ( SSAO) has been considered to be associated with the metabolism of glucose and fat,and elevated SSAO activity was observed in obese patients. In the present study,an in vitro SSAO activity-based method was developed to screen inhibitors from 1 5 anti-obesity drugs. Among the fifteen anti-obesity drugs,four drugs including caffeine,fenfluramine, bumetanide and amfebutamone inhibited SSAO activity,and caffeine was the most effective one. When the concentration of caffeine was 1 . 4 mmol / L,the inhibition ratio was 3 1 . 9 % and 1 8 . 8 % in rabbit serum and rat adipose tissue,respectively. Inhibition of SSAO activity by caffeine was also confirmed in the in vivo study,showing the inhibition ratio of 1 5 . 6 % on serum SSAO. Caffeine provides a natural source of inhibition of SSAO activity and may be a promising inhibitor for the study of SSAO.
文摘As a dark tea,Pu-erh tea(PET)is produced from sun-dried leaves of Camellia sinensis var.assamica mainly in Yunnan Province of China.Many microorganisms are involved in the fermentation of PET.Among them,Aspergillus niger is most important.It is believed that the longer the preservation period,the better is the quality and taste of PET,which is commercially available as loose,compressed or instant tea leaves.Chemical components of PET include flavones,flavanols,flavonols,phenolic acids,alkaloids and methylxanthines.In this overview,the lipid-lowering and anti-obesity effects of PET were discussed based on animal models and human trials,and our study provided some insights into possible mechanisms of bioactive compounds,such as theabrownin,catechins,lovastatin and gallic acid.Other bioactivities of PET and some information on Fuzhuan brick tea were also included.Sources of information cited were from Google Scholar,Pub Med,Pub Med Central,Science Direct,J-Stage,Pub Chem,Directory of Open Access Journals(DOAJ),and China National Knowledge Infrastructure(CNKI).
基金Fundamental Research Funds for the Central Universities of China(2662019PY066,2662016PY132)。
文摘This study investigated hypolipidemic,weight-reducing,and hepatoprotective effects of Antrodia cinnamomea mycelial extract obtained from solid-state culture(ACME)in an HFr D-induced obese/hyperlipidemic mouse model.Following 4-week ACME treatment,body weight,epididymal fat index,and some serum biochemical indices were measured.Expression levels of some related genes involved in cholesterol and lipid metabolism were analyzed by q RT-PCR.Moreover,histological studies of hepatic tissues were also conducted.After ACME treatment,body weight and epididymal fat index were significantly lower than that in model control group.ACME and simvastatin significantly reduced serum total cholesterol(T-CHO)and low-density lipoprotein cholesterol(LDL-C)levels,and increased high-density lipoprotein cholesterol(HDL-C)level.Subsequent experiments showed that:(i)ACME regulated transcriptional expression of 3-hydroxy-3-methylglutaryl-Co A reductase(HMGR),low-density lipoprotein receptor(LDLR),adipose triglyceride lipase(ATGL),and fatty acid synthase(FAS),with consequent reduction of blood lipid levels and body weight;(ii)ACME enhanced total antioxidant capacity(T-AOC)and superoxide dismutase(SOD)activity in hepatic tissues;(iii)ACME reduced malondialdehyde(MDA)level and ameliorated lipid oxidative damage in liver.Our findings indicate that ACME is a strong candidate for development as a novel anti-hyperlipidemia and anti-obesity health product.
基金supported by[National Natural Science Foundation of China](Grant number 32001702).
文摘This study aimed to elucidate the inhibition mechanism of apigenin against porcine pancreatic lipase(PPL),and,moreover,to comprehensively reveal the molecular basis of its anti-obesity via network pharmacology approach.The results showed that apigenin inhibited PPL with an IC50 value of 0.377±0.041 mM.Spectroscopic techniques combined molecular docking suggested that apigenin could bind into the PPL active pocket,affecting its normal spatial conformation.Moreover,molecular dynamic(MD)simulations revealed that the open conformation of PPL tended to transit to the closed in the presence of apigenin,which might one important reason for the inhibition of PPL catalytic ability.Network pharmacology analysis revealed that a total of 49 proteins could be identified as potential targets for the anti-obesity effects of apigenin.According to the protein-protein interaction(PPI)network analysis,six hub targets were extracted including IGF1,ESR1,MMP9,PPARA,MAPK14 and NR3C1.Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway enrichment indicated that the 49 potential targets could be mapped to 30 pathways(p<0.05).Among them,PI3K-Akt signaling pathway and insulin resistance can be considered as two major pathways regulated by apigenin.Further docking studies indicated that apigenin can bind into the binding pocket of the six hub target proteins identified according to the PPI network.The results indicated that in addition to inhibiting PPL,apigenin could exhibit anti-obesity benefit through the molecular mechanisms uncovered by network pharmacology.This study proposes a new strategy to reveal the mechanisms of dietary polyphenols at the level of network pharmacology.
基金supported by National Natural Science Foundation of China(Project No.32160547)Central Government Guide Local Special Fund Project(Project No.20212ZDD02008)+2 种基金Vegetable Industry Technology System Post Expert Project of Jiangxi Province(Project No.JXARS-06)State Key Laboratory of Food Science and Technology Nanchang University(Project No.SKLF-ZZA-201910)State Key Laboratory of Food Science and Technology Nanchang University(Project No.SKLF-ZZB-202132).
文摘The worldwide obesity epidemic has imposed human being a huge burden and attention had been drawn to manipulating the lactic acid bacteria (LAB) to improve obesity symptoms.In this study,a more comprehensive and reliable in vitro method was established to screen LAB with greater potential against obesity.Firstly,twenty-eight human feces-derived LAB strains were selected by assessing bile salt-acid tolerance and cholesterol lowering capacity.Subsequently,the triglyceride lowering capacity,bile salt hydrolase (BSH) activity,α-glucosidase activity inhibition capacity and Enterobacter cloacae (E.cloacae) growth inhibition capacity were tested for further evaluating the anti-obesity properties of LAB strains.Principal component analysis (PCA) of these results indicated that Limosilactobacillus reuteri (L.reuteri) NCUH003,Lactiplantibacillus plantarum (L.plantarum) NCUH046 and Limosilactobacillus fermentum (L.fermentum) NCUH068 exhibited favorable anti-obesity properties.Besides,the LAB displayed good gastrointestinal adaptability and antioxidant activity but no hemolytic activity,and they were sensitive to various antibiotics.These results indicated that L.reuteri NCUH003,L.plantarum NCUH046 and L.fermentum NCUH068 are potential for application in obesity treatment.
基金Supported by Bindura University of Science Education(Grant No.2013/6).
文摘Objective:To investigate antioxidant and anti-obesity activity of flavonoids extracted by solvent cold percolation and preparative thin liquid chromatography from Dioscorea steriscus tubers.Methods:1-diphenyl-2-picrylhydrazyl(DPPH)antiradical activity was employed to investigate antioxidant activity while chromogenic method was used to determine alpha amylase inhibition activity and spectrophotometric methods using triolein as a substrate was used to investigate lipase activity.Results:Thin liquid chromatography profiling revealed eight different flavonoid types.Ethyl acetate extract yielded two types,R_(f) values 0.38 and 0.40;chloroform extract also yielded two types R_(f) values 0.06 and 0.51,while ethanol extract yielded four types with R_(f) values 0.16,0.33,0.65 and 0.96.All the extracted flavonoids exhibited antioxidant activity with ethanol extracts exhibiting the greatest antiradical activity.The order of enzyme inhibition capacity was ethyl acetate<chloroform<ethanol.Ethanol extract exhibited significantly greater anti-obesity activity as compared to herbex,a commercially anti-obesity medication sold in drug stores.Anti-α amylase activity and anti-lipase activity for herbex was(78.38±0.02)%and(76.07±0.09)%respectively,while that for ethanolic extract(R_(f)=0.96)was(93.66±0.00)%and(95.88±0.13)%.Conclusions:Results of the present study show that Dioscorea steriscus consists of bioactive compounds that can act as lipase andα-amylase inhibitors and therefore can be useful for the development of functional foods against obesity.It can also be used as a source of lead compounds for designing new ant-obesity therapeuticals.
基金supported by the Brazilian funding agencies CNPq,and FUNDECT (to LM)
文摘Obesity is associated with several diseases,including mental health.Adipose tissue is distributed around the internal organs,acting in the regulation of metabolism by storing and releasing fatty acids and adipokine in the tissues.Excessive nutritional intake results in hypertrophy and proliferation of adipocytes,leading to local hypoxia in adipose tissue and changes in these adipokine releases.This leads to the recruitment of immune cells to adipose tissue and the release of pro-inflammatory cytokines.The presence of high levels of free fatty acids and inflammatory molecules interfere with intracellular insulin signaling,which can generate a neuroinflammatory process.In this review,we provide an up-to-date discussion of how excessive obesity can lead to possible cognitive dysfunction.We also address the idea that obesity-associated systemic inflammation leads to neuroinflammation in the brain,particularly the hypothalamus and hippocampus,and that this is partially responsible for these negative cognitive outcomes.In addition,we discuss some clinical models and animal studies for obesity and clarify the mechanism of action of anti-obesity drugs in the central nervous system.
基金the support of the "Cooperative Research Program for Agriculture Science & Technology Development (Project No.PJ009582)" of the Rural Development Administration.Republic of Korea
文摘Objective:To explore the anti-obesity effects and the mechanism of action of Monascus pilosus(M.pilosus)-fermented black soybean(MFBS)extracts(MFBSE)and MFBS powders(MFBSP)in adipocytes and high-fat diet(HFD)-induced obese mice,respectively.Methods:Black soybean was fermented with M.pilosus,and the main constituents in MFBS were analyzed by HPLC analysis.In vitro,MFBSE were examined for anti-adipogenic effects using Oil-Red O staining.In vivo,mice were fed a normal-fat diet(NFD)control,HFD control or HFD containing 1 g/kg MFBSP for 12 weeks,and then body weight gain and tissues weight measured.Real-time PCR and western blot assay were used to determine the mechanism of anti-adipogenic effects.Results:MFBSE inhibited lipid accumulation in 3T3-L1 adipocytes without exerting cell cytotoxicity.MFBSP treatment in HFD-fed mice significantly decreased the body weight gain compared with the HFD control mice.MFBSE and MFBSP treatment resulted in significantly lower mRNA levels of adipogenesis-related genes,such as peroxisome proliferator-activated receptorγ(PPARγ),fatty acid-binding protein 4(FABP4),and fatty acid synthase(FAS),in adipocytes and in white adipose tissue(WAT)of HFD-induced obese mice.Conclusions:These results suggest that the anti-obesity effects of MFBS are elicited by regulating the expression of adipogenesis-related genes in adipocytes and WAT of HFDinduced obese mice.
基金supported by the National Natural Science Foundation of China (31630096)。
文摘High sucrose content in traditional hawthorn leathers limits the potential consumption, particularly for elders and diabetics. In this study, sucrose-free hawthorn leathers were formulated with 75% fructooligosaccharides(FOS) and 25% xylooligosaccharides(XOS)(HLF75), which exhibited comparable morphology and sensory properties to the traditional ones. Then, the anti-obesity activity of HLF75 was investigated using high-fat diet(HFD) fed C57BL/6J mice. Comparing with traditional hawthorn leathers, HLF75 supplementation in HFD significantly decreased the levels of blood glucose and serum lipid. The histomorphologies of liver and subcutaneous fat tissues were ameliorated by HLF75, as well as the down-regulated m RNA expression levels of IL-1β, Nos2 and Cox-2 in the liver. M oreover, the protein levels of M y D88 and NF-κB in the liver were suppressed by HLF75 treatment with decreased F4/80-positive macrophage number. Ho wever, the expression levels of PI3K, phosphorylated-AKT(Thr308), and phosphorylated-m TOR(Ser2448) proteins related to glucose metabolism were increased in the liver. Moreover, fat synthesis-related gene expression in HLF75-fed mice was suppressed while expressions of lipolysis genes were improved. Thus, HLF75 supplementation alleviated HFD-induced obesity through the alleviation of inflammation and restoration of the disturbed glucose and lipid metabolism. Functional oligosaccharides could be effective sucrose substitutes in hawthorn leathers and enable their potential utilization as functional foods.
基金supported by Natural Science Foundation of Guangdong Province of China(2018A030307074)Project of Educational Commission of Guangdong Province of China(2019KQNCX080)。
文摘Background:Chinese medicine has been proposed as a novel approach to the prevention of metabolic disorders such as obesity.Danggui Buxue decoction,a decoction prepared from Huangqi(Astragali Radix)and Danggui(Angelicae Sinensis Radix),has been used to nourish vitality and enhance blood circulation in traditional Chinese medicine.However,the effect of Danggui Buxue decoction on obesity is still primarily unknown.Methods:Cell proliferation,differentiation,and apolipoprotein-IV transcription were investigated to explore the function of Danggui Buxue decoction by methyl thiazolyl tetrazolium assay,alkaline phosphatase assay,and luciferase assay,respectively.Results:Danggui Buxue decoction promoted cell growth by up to 15%(P=0.034)and induced cell differentiation by up to 38%(P=0.006)at 0.3 mg/mL.Moreover,Danggui Buxue decoction enhanced the transcription of apolipoprotein-IV by 2.4 times(P=0.027),activating its promoter by 28.9%(P=0.031)at 0.3 mg/mL.In addition,Danggui Buxue decoction functioned in a dose-dependent manner.Conclusion:These results suggest that Danggui Buxue decoction promotes cell differentiation by enhancing apolipoprotein-IV transcription and alkaline phosphatase activity,and it may also have a potential anti-obesity effect because apolipoprotein-IV transcription is closely related to the reduction of food intake.
文摘The methanol extract of grains of paradise (GP), the seed of Aframomum melegueta, which is distributed throughout West Africa, was administered during an animal breeding test. The extract suppressed body weight gain and decreased the weight of adipose tissues in breeding mice, with a greater effect on mice fed a high-fat diet (HFD) than on those fed a normal diet (ND). Other significant effects of GP intake included increased serum triglyceride (TG) concentration and reduced hepatic total cholesterol (TC) and TG concentrations. GP intake markedly prevented fat accumulation and improved hepatic lipid metabolism in HFD-fed mice. In addition, GP extract at a dosage of 5 mg/kg body weight decreased sympathetic nerve activity (SNA) in brown adipose tissue (BAT), while capsaicin, a major component of chili pepper, activated BAT SNA. This suggested that GP exerts a potential anti-obesity effect by a different mechanism from that of capsaicin.
文摘The main aim of this study is to determine the anti-hyerlipidemic and anti-obesity activity of Canephora robusta in hyperlipidemia induced rats. Prepared coffee bean extract (GCE) was procured from the market which is unroasted and contains more quantity of caffeine and chlorogenic acid when compared to roasted coffee. Male albino Wister rats are fed with high fat diet (HFD) for weeks to induce hyperlipidemia in rats, which are divided into 4 groups with 4 animals in each group. Test GCBE was given in doses of 200 mg/kg and 400 mg/kg to III and IV groups which are fed with HFD for 30 days. Then blood samples were collected through retro-orbital sinus by capillaries and serum is separated for analysis. The result obtained from lipid profile which includes total cholesterol, triglycerides, very low density lipoproteins, and low density lipoproteins shows the decreased level when compared to the hyperlipidemic control. This shows the significant reduction of total body weight (p < 0.05) when given with dose of 200 mg/kg and 400 mg/kg. The present study suggests that GCBE has anti-obesity and anti-hyperlipidemic activity, where 400 mg/kg is more effective to reduce the total body weight and lipid levels when compared to 200 mg/kg. Further studies on this extract may lead to identify the possible mechanism of action and isolation of active principle from the same.
基金supported by the National Natural Science Foundation of China(Nos.22101086,and 21225103)Natural Science Foundation of Guangdong Province(No.2021A1515010271)+1 种基金Tsinghua University Initiative Foundation Research Program(No.20131089204)the State Key Laboratory of Natural and Biomimetic Drugs(No.K20160202)。
文摘Obesity,characterized by the dysregulation of energy balance in adipose tissue and other metabolic organs,is frequently accompanied by chronic low-grade inflammation.As long-acting insulin sensitizers,the organically-derivatized polyoxovanadates(POVs),can extend the dosing interval of antidiabetic drugs from hourly to almost daily.In this work,the protective activity of POVs is investigated by an eight-week in vivo experiment,in which a small amount of POVs was administrated orally to a mouse model of dietinduced obesity every day.The present study shows that administration of POVs significantly decreases the body weight of mice,reduces adipose tissue accumulation,and simultaneously reduces adipose tissue inflammation.In addition,the anti-obesogenic population of i NKT cells is protected potentially by POVs,which subsequently alleviates visceral adipose tissue inflammation in high-fat-diet(HFD)-fed mice against diet-induced obesity.By contrast,the change in body weight after POV treatment is the result of a substantial reduction in fat mass,with no obvious effects on lean body mass.These findings demonstrate that supplementary of POVs would be an effective way to combat obesity and metabolic disorders while lowering metabolic inflammation.
基金supported by the National Science Foundation of China(No.81573322)the Hundred-Talent Program of CAS+1 种基金the CAS"Light of West China"Programthe Youth Innovation Promotion Association of CAS
文摘5-Hydroxytryptamine 2C(5-HT2C) receptor is one of the major targets of anti-obesity agents, due to its role in regulation of appetite. In the present study, the 70% EtO H extract of the roots of Bupleurum chinense was revealed to have agonistic activity on 5-HT2 C receptor, and the subsequent bioassay-guided isolation led to identification of several saikosaponins as the active constituents with 5-HT2 C receptor agonistic activity in vitro and anti-obesity activity in vivo. The new compound, 22-oxosaikosaponin d(1), was determined by extensive spectroscopic analyses(HR-ESI-MS, IR, and 1D and 2D NMR). The primary structure-activity relationship study suggested that the intramolecular ether bond between C-13 and C-28 and the number of sugars at C-3 position were closely related to the 5-HT2 C receptor agonistic activity. Saikosaponin a(3), the main saponin in B. chinense, showed obviously agonistic activity on 5-HT2 C receptor with an EC50 value of 21.08 ± 0.33 μmol×L^(–1) in vitro and could reduce food intake by 39.1% and 69.2%, and weight gain by 13.6% and 16.4%, respectively, at 3.0 and 6.0 mg×kg^(–1) in vivo. This investigation provided valuable information for the potential use of B. chinense as anti-obesity agent.
基金supported by the Graduate Students Scientific Research Innovation Projects of Jiangsu Province(No:CXZZ11-0804)
文摘The present study was designed to synthesize and evaluate a series of benzylisoquinoline derivatives. These compounds were synthesized by Bischler-Napieralski cyclization to yield 1-benzyl-3,4-dihydroisoquinolines, and the products were obtained by reductions. All these compounds were identified by MS, 1H NMR and 13 C NMR. The inhibitory activities on pancreatic lipase and preadipocyte proliferation for the synthesized compounds and alkaloids from Nulembo nucifera were assessed in vitro. Most of the compounds showed inhibitory activities on both pancreatic lipase and preadipocyte proliferation. Particularly, compounds 7p-7u and 9d-9f exhibited significant inhibitory activity on pancreatic lipase while compounds 7c, 7d, 7f, 7g, 7i, and 7j potently inhibited the proliferation of 3T3-L1 preadipocytes. Our results provided a basis for future evaluation and development of these compounds as leads for therapeutics for human diseases.
