Ten novel xanthones,garpedunxanthones A-G(1-5,6a/6b,7a/7b) and nujiangxanthone Q(8),along with sixteen known analogs(9-24),were isolated from Garcinia pedunculata and G.nujiangensis.Their structures were elucidated th...Ten novel xanthones,garpedunxanthones A-G(1-5,6a/6b,7a/7b) and nujiangxanthone Q(8),along with sixteen known analogs(9-24),were isolated from Garcinia pedunculata and G.nujiangensis.Their structures were elucidated through high-resolution electrospray ionization mass spectrometry(HR-ESI-MS) data,comprehensive nuclear magnetic resonance(NMR) spectroscopic analyses,and electronic circular dichroism(ECD) calculations.All compounds without cytotoxicity were assessed for anti-inflammatory properties by measuring the inhibition of nitric oxide(NO) production in lipopolysaccharide(LPS)-induced RAW264.7cells.Structure-activity relationships are also discussed.Compounds 7b,19,and 21 exhibited significant anti-inflammatory activity with IC_(50) values of 16.44±0.69,14.28±0.78,and 10.67±3.28 μmol·L^(-1),respectively.Enzyme-linked immunosorbent assay(ELISA) demonstrated that compounds 7b,19,and 21 inhibited the expression of pro-inflammatory cytokines TNF-α and IL-6 in a dose-dependent manner.The inhibitory effect of compo und 21 on IL-6 at 20 μmol·L^(-1)was comparable to that of the positive control.In network pharmacology studies,potential targets of compounds and inflammation were identified from PharmMapper and GeneCards databases.Gene Ontology(GO) and Kyoto Encyclopedia of Genes and Genomes(KEGG) enrichment analysis revealed that the overlapped targets were intricately associated with major pathogenic processes linked to inflammation,including positive regulation of mitogen-activated protein kinase(MAPK) cascade,protein kinase activity,NO synthase regulator activity,MAPK signaling pathway,and EGFR tyrosine kinase inhibitor resistance.展开更多
Two novel xanthones, 1,6-dihydroxy-4,5-dimethoxyxanthone （1） and 1,5,6-trihydroxy-7,8-di（3-methyl-2-butenyl）-6＇,6＇-dimethylpyrano（2＇,3＇：3,4）xanthone （2） were isolated from the bark of Garcinia xanthochymu...Two novel xanthones, 1,6-dihydroxy-4,5-dimethoxyxanthone （1） and 1,5,6-trihydroxy-7,8-di（3-methyl-2-butenyl）-6＇,6＇-dimethylpyrano（2＇,3＇：3,4）xanthone （2） were isolated from the bark of Garcinia xanthochymus by normal phase and reverse phase silica gel column chromatography. Their structures were elucidated by spectroscopic methods, especially 2D-NMR techniques.展开更多
The aim of the present study was to investigate the protective effects and underlying mechanisms of Garcinia xanthochymus, a perennial medicinal plant native to Yunnan, China, against H2 O2-induced oxidative damage in...The aim of the present study was to investigate the protective effects and underlying mechanisms of Garcinia xanthochymus, a perennial medicinal plant native to Yunnan, China, against H2 O2-induced oxidative damage in rat pheochromacytoma PC12 cells. Preincubation of PC12 cells with fruit Et OAc fraction(fruit-EFr., 12.5–50 μmol·L^(-1)) of G. xanthochymus for 24 h prior to H_2O_2 exposure markedly improved cell viability and increased the activities of antioxidant enzymes(superoxide dismutase, catalase, and heme oxygenase-1 [HO-1]), prevented lactate dehydrogenase release and lipid peroxidation malondialdehyde production, attenuated the decrease of matrix metalloproteinases(MMP), and scavenged reactive oxygen species(ROS). Fruit-EFr. also reduced BAX and cytochrome C expression and improved BCL-2 expression, thereby decreasing the ratio of BAX to BCL-2. Fruit-EFr. activated the nuclear translocation of NRF2 to increase HO-1 and induced the phosphorylation of AKT. Its cytoprotective effect was abolished by LY294002, a specific inhibitor of PI3 K. Taken together, the above findings suggested that fruit-EFr.of G. xanthochymus could enhance cellular antioxidant defense capacity, at least in part, through upregulating HO-1 expression and activating the PI3 K/AKT pathway and that it could suppress H_2O_2-induced oxidative damage via PI3 K/AKT and NRF2/HO-1 signaling pathways.展开更多
Objective:To study the chemical constituents of stembark of Garcinia malaccenm（G.malaccenm） together with apoptotic.antimicrobial and antioxidant activities.Methods:Purification and structure elucidation were carrie...Objective:To study the chemical constituents of stembark of Garcinia malaccenm（G.malaccenm） together with apoptotic.antimicrobial and antioxidant activities.Methods:Purification and structure elucidation were carried out by chromatographic and spectroscopic techniques, respectively.MTT and trypan blue exclusion methods were performed to study the cytotoxic activity.Antibacterial activity was conducted by dise diffusion and microdilulion methods, whereas antioxidant activities were done by ferric thiocyanate method and DPPH radical scavenging.Results:The phylochemical study led lo the isolation ofα,β-mangostin and cycloarl-24-en-3β-ol.α-Mangostin exhibited cytotoxic activity against HSC-3 cells with an IC<sub>50</sub> of 0.33μM.β- andα-mangostin showed activity against K562 cells with IC<sub>50</sub> of 0.40μM and 0.48μM,respectively,α-Mangostin was active against Gram-positive bacteria, Staphylococcus aureus（S.aureus） and Bacilus anthracis（B.anthmcis） with inhibition zone and MIC value of（19 mm;0.02S mg/mL） and（20 mm;0.013 mg/mL）,respectively.In antioxidant assay,α-mangostin exhibited activity as an inhibitor of lipid peroxidation.Conclusions:G.malaccenm presenceα- andβ-mangostin and cycloart-24-en-3β-ol.β-Mangostin was found very active against H.SC-3 cells and KS62.The results suggest that mangoslins derivatives have the potential to inhibit the growth of cancer cells by inducing apoptosis.In addition,α-andβ-mangostin was found inhibit the growth of Cram-positive pathogenic bacteria and also showed the activity as an inhibitor of lipid peroxidation.展开更多
AIM:To investigate the growth inhibitory mechanism of four caged xanthones from Garcinia hanburyi in cholangiocarcinoma(CCA) KKU-100 and KKU-M156 cells.METHODS:Four caged xanthones,selected on the basis of their antic...AIM:To investigate the growth inhibitory mechanism of four caged xanthones from Garcinia hanburyi in cholangiocarcinoma(CCA) KKU-100 and KKU-M156 cells.METHODS:Four caged xanthones,selected on the basis of their anticancer potency and chemical structure diversities(i.e.isomorellin,isomorellinol,forbesione and gambogic acid) were used in this study.Growth inhibition of these caged xanthones was determined using the sulforhodamine B assay.Induction of apoptosis was assessed by observing cell morphology,ethidium bromide and acridine orange staining and DNA fragmentation assay.Levels of apoptotic-related gene and protein expressions were determined by a real-time reverse transcriptase polymerase chain reaction and Western blotting analysis,respectively.RESULTS:The compounds were found to inhibit growth of both cell lines in a dose-dependent manner and also showed selective cytotoxicity against the cancer cells when compared with normal peripheral blood mononuclear cells.Growth suppression by these compounds was due to apoptosis,as evidenced by the cell morphological changes,chromatin condensation,nuclear fragmentation,and DNA ladder formation.At the molecular level,these compounds induced down-regulation of Bcl-2 and survivin proteins with up-regulation of Bax and apoptosisinducing factor proteins,leading to the activation of caspase-9 and-3 and DNA fragmentation.The functional group variations did not appear to affect the anticancer activity with regard to the two CCA cell lines;however,at a mechanistic level,isomorellinol exhibited the highest potency in increasing the Bax/Bcl-2 protein expression ratio(120 and 41.4 for KKU-100 and KKU-M156,respectively) and in decreasing survivin protein expression(0.01 fold as compared to control cells in both cell lines).Other activities at the molecular level indicate that functional groups on the prenyl side chain may be important.CONCLUSION:Our findings for the first time demonstrate that four caged xanthones induce apoptosis in CCA cells which is mediated through a mitochondriadependent signaling pathway.展开更多
Objective: To isolate a-mangostin(AMG) from the peels of mangosteen(Garcinia mangostana L.), grown in Vietnam, and to investigate antibiofilm activity of this compound against three Staphylococcus aureus(S. aureus) st...Objective: To isolate a-mangostin(AMG) from the peels of mangosteen(Garcinia mangostana L.), grown in Vietnam, and to investigate antibiofilm activity of this compound against three Staphylococcus aureus(S. aureus) strains, one of which was methicillin-resistant S. aureus(MRSA) and the other two strains were methicillinsensitive S. aureus(MSSA).Methods: AMG in n-hexane fraction was isolated on a silica gel column and chemically analyzed by HPLC and NMR. The antibiofilm activity of this compound was investigated by using a 96-well plate model for the formation of biofilms. Biofilm biomass was quantified using crystal violet. The viability of cells was observed under confocal microscopy using LIVE/DEAD Bac Light stains. Biofilm composition was determined using specific chemical and enzyme tests for polysaccharide, protein and DNA. Membranedamaging activity was assayed by measuring the hemolysis of human red blood cells in presence of AMG.Results: The results indicated that the isolated AMG, with a purity that exceeded 98%,had minimal inhibitory concentrations in the range of 4.6–9.2 mmol/L for the three strains tested. Interestingly, the MSSA strains were more sensitive to AMG than the MRSA strain. Minimal bactericidal concentrations were 2-fold higher than the minimal inhibitory concentration values for the three strains, indicating that AMG was a bactericidal compound. AMG also prevented biofilm formation effectively, albeit that again the MRSA strain was the most resistant. Interestingly, biofilms of the MRSA strain contained protein as a main component of the extracellular matrix, whereas this was polysaccharide in the MSSA strains. This might relate to the resistance of the MRSA 252 strain to AMG.Assays using human red blood cells indicated that AMG caused significant membrane damage with 50% of cell lysis occurred at concentration of about 36 mmol/L.Conclusions: Our results provide evidence that the isolated AMG has inhibitory activity against biofilm formation by S. aureus, including MRSA. Thus, isolated AMG proposes a high potential to develop a novel phytopharmaceutical for the treatment of MRSA.展开更多
A new caged polyprenylated xanthone, gambogic aldehyde （1）, was isolated from the resin of Garcinia hanburyi. Its structure was elucidated on the basis of spectral data including 1D and 2D NMR data. In addition, the...A new caged polyprenylated xanthone, gambogic aldehyde （1）, was isolated from the resin of Garcinia hanburyi. Its structure was elucidated on the basis of spectral data including 1D and 2D NMR data. In addition, the antiproliferative ability of compound 1 was determined in mouse leukemia P388 and P388/ADR cells.展开更多
AIM: To investigate long-term effects of Garcinia Cambogia (GC), weight-loss supplement, on adiposity and non-alcoholic fatty liver disease in obese mice. METHODS: Obesity-prone C57BL/6J mice were fed a high-fat diet ...AIM: To investigate long-term effects of Garcinia Cambogia (GC), weight-loss supplement, on adiposity and non-alcoholic fatty liver disease in obese mice. METHODS: Obesity-prone C57BL/6J mice were fed a high-fat diet (HFD, 45 kcal% fat) with or without GC (1%, w/w) for 16 wk. The HFD contained 45 kcal% fat, 20 kcal% protein and 35 kcal% carbohydrate. They were given free access to food and distilled water, and food consumption and body weight were measured daily and weekly, respectively. Data were expressed as the mean ± SE. Statistical analyses were performed using the statistical package for the social science software program. Student's t test was used to assess the differences between the groups. Statistical significance was considered at P < 0.05. RESULTS: There were no significant changes in body weight and food intake between the groups. However, the supplementation of GC significantly lowered visceral fat accumulation and adipocyte size via inhibition of fatty acid synthase activity and its mRNA expression in visceral adipose tissue, along with enhanced enzymatic activity and gene expression involved in adipose fatty acid β-oxidation. Moreover, GC supplementation resulted in significant reductions in glucose intolerance and the plasma resistin level in the HFD-fed mice. However, we first demonstrated that it increased hepatic collagen accumulation, lipid peroxidation and mRNA levels of genes related to oxidative stress (superoxide dismutase and glutathione peroxidase) and inflammatory responses (tumor necrosis factor-α and monocyte chemoattractant protein-1) as well as plasma alanine transaminase and aspartate transaminase levels, although HFD-induced hepatic steatosis was not altered. CONCLUSION: GC protects against HFD-induced obesity by modulating adipose fatty acid synthesis and β-oxidation but induces hepatic fibrosis, inflammation and oxidative stress.展开更多
A novel caged-prenylxanthone xanthone,neobractatin(1),was isolated from the twig of Garcinia bracteata.Its structure was elucidated by spectroscopic methods,especially 2D NMR techniques.
Objective:To investigate the antimalarial activity and toxicity of the crude ethanolic extract of its pericarp both in vitro and in vim.Methods:The antimalarial activity of Gareinja mangostana(G.mangostana)Linn.extrac...Objective:To investigate the antimalarial activity and toxicity of the crude ethanolic extract of its pericarp both in vitro and in vim.Methods:The antimalarial activity of Gareinja mangostana(G.mangostana)Linn.extract against 3D7 and Kl Plasmodium falciparum(P.falciparum)clone were assessed using SYBR green I-based assay.A 4-day suppressive test of Plasmodium berghei{P.berghei)infected mouse was performed to investigate in vivo antimalarial activity.Results:The in vitro antimalarial activity was seleclive(SI>5?and classified as weak and good lo moderate activity against both 3D7 and K1 P.falciparum,clones with median IC_(50)(range)values of 11.12(10.94-11.29)and 7.54(6.80-7.68)μg/mL,respectively.The extract was considered nontoxic to mice.The maximum tolerated doses for acute and subacute toxicity in mice were 5 000and 2 000 mg/kg,respectively.Median(range)parasite density on day 4 of the negative control group(25%Tween-80),mice treated with 250,500,1000,and 2 000 mg/kg body weight of the extract,and 10 mg/kg body weight of chloroquine for 14 d were 12.8(12.2-13.7),11.4(9.49-13.8),11.6(9.9-12.5),11.7(10.6-12.8),10.9(9.4-11.6)and 0(0-0)%respectively.Parasite density on day 4in the control group treated with Tween-80 was higher than the groups treated with chloroquine and all dose levels of the extract.Conclusions:G.mangostana linn,showed weak antimalarial activity of the extract both in vitro and in vivo could be due to limitation of absorption of the active compounds.展开更多
BACKGROUND Herbal supplements(HS)for weight loss are perceived to be“safe”and“natural”,as advertised in ads,however,hepatotoxicity can be associated with consumption of some HS.Use of HS may be missed,as the patie...BACKGROUND Herbal supplements(HS)for weight loss are perceived to be“safe”and“natural”,as advertised in ads,however,hepatotoxicity can be associated with consumption of some HS.Use of HS may be missed,as the patient may not report these unless specifically asked about these products,since they are often not thought of as medications with potential side effects or interaction potential.CASE SUMMARY We reported a case of a 21-year-old female with morbid obesity who presented with abdominal pain for 1 wk associated with nausea,vomiting,anorexia and myalgias.She denied smoking tobacco,drinking alcohol,usage of illicit drugs,hormonal contraceptives,or energy drinks.There was no significant past medical or family illnesses.Her laboratory workup revealed acute liver failure.The workup for possible etiologies of acute liver failure was unremarkable.She was using a weight loss herbal supplement“Garcinia cambogia”for 4 wks.This case demonstrates the association of acute liver failure with Garcinia cambogia.CONCLUSION Medical reconciliation of HS should be performed in patients with suspected acute liver failure and early discontinuation of HS can prevent further progression of drug induced hepatoxicity.展开更多
Objective:To assess the neuroprotective effects of aqueous extract of Garcinia kola on neurotoxin administered malnourished mice adopting histological procedure.Methods:The study was carried out using thirty-two adult...Objective:To assess the neuroprotective effects of aqueous extract of Garcinia kola on neurotoxin administered malnourished mice adopting histological procedure.Methods:The study was carried out using thirty-two adult malnourished mice which were randomly assigned into four groups(n=8):A,B,C and D.Group A served as control,while the other groups served as the experimental groups.Animals in group A were fed malnourished diet ad libitum and given water liberally.Animals in group B were administered with 3-Nitropropionic acid(3-NP)(neurotoxin)only at 20 rag/kg body weight,group C were given only Garcinia kola extracts,and group D were pre-treated with Garcinia kola extracts at 200 mg/kg for seven days prior to administration of neurotoxin at 20 mg/kg body weight.After three days of neurotoxins administration in the relevant groups,the brains were excised and fixed in formal calcium for histological processing.Results:The study showed that hippocampal and cerebellar neurons of animals in group B exhibited some cellular degeneration and blood vessel blockage,which were not seen in groups A,C and D.Cresyl violet staining was least intense in group B than in groups A,C and D.Despite the fact that animals in group D has equal administration of 3-Nitropropionic acid concentration,there were no traces of neural degeneration as it was evidenced in group B.Conclusions:It is concluded that Garcinia kola has protective effects on the neurons of the hippocampus and cerebellum of malnourished mice.展开更多
Objective:To investigate the cytotoxic effect of ethanol extract of the stem bark of asam kandis[Garcinia cowa Roxb.(G.cowa)]on T47 D breast cancer cell line.Methods:The cytotoxicity of ethanol extract was carried out...Objective:To investigate the cytotoxic effect of ethanol extract of the stem bark of asam kandis[Garcinia cowa Roxb.(G.cowa)]on T47 D breast cancer cell line.Methods:The cytotoxicity of ethanol extract was carried out against human breast cancer cell line(T47D) by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide colorimetric assay.The extract was added at various concentrations(0.1.1,10 and 100 μg/mL).The level of cytotoxicity was determined by calculating the level of IC_(50),that was based on the percentage of the cell death after 24 h treatment with the extract.Cell morphological changes were observed by using inverted microscope.Results:The 3-(4.5-dimelhylthiazol-2-yl)-2.5-diphenyltelrazolium bromide assay showed that ethanol extract of G.cowa exhibited significant cytotoxic effect on T47 D with IC_(50) value of(5.10+1.68) μg/mL.Morphological alteration of the cell lines after exposure to ethanol extract of G.cowa was observed under phase contrast microscope in a dosc-dependent manner.ConclusionsThe results suggest the possible use of ethanol extract of asam kandis for preparing herbal medicine for cancer-related ailments.展开更多
Citridones E-G (1-3), three new phenylpyridone derivatives together with two known curvularins (4 and 5) were isolated from the solid culture of the endophytic fungus Penicillium sumatrense GZWMJZ-313 in Garcinia mult...Citridones E-G (1-3), three new phenylpyridone derivatives together with two known curvularins (4 and 5) were isolated from the solid culture of the endophytic fungus Penicillium sumatrense GZWMJZ-313 in Garcinia multiflora. The structures of new compounds were determined in the light of spectroscopic data,X-ray and ECD calculation. Compounds 1 and 3 are racemates, while compound 2 is optically pure.Compounds 1 and 4 showed antibacterial and antifungal activities against Staphylococcus aureus,Pseudomonas aeruginosa, Clostridium perfringens, Escherichia coli and Candida albicans with MIC values ranging from 8 μg/mL to 64 μg/mL.展开更多
Insecticidal effects of different doses of the dust and methanol extracts of Garcinia kolae on Callosobruchus maculatus and Sitophilus zeamais were tested. The dust had no significant effect on the two insects, none o...Insecticidal effects of different doses of the dust and methanol extracts of Garcinia kolae on Callosobruchus maculatus and Sitophilus zeamais were tested. The dust had no significant effect on the two insects, none of them died even at 3 d after treatment. The methanol extracts, however, had rapid lethal effects on both C. maculatus and S. zeamais. The mortality of C. maculatus by the lowest concentration of methanol extracts ranged from 95%-100% whereas in S. zeamais, the mortality ranged from 87.5%-100% and 70%-100% in concentrations of 1 g extract＋3 ml methanol and 1 g extract＋5 ml methanol, respectively, from 24 to 48 h. The least concentration of 1 g extract＋l 5 ml methanol had no significant lethal effect on Sitophilus zeamais.展开更多
Objectives: Garcinia kola seeds (EAgk) (Clusiaceae) contain coagulant components use to pretreat aquaculture wastewater in Nigeria. This work was undertaken to assess the effects of EAgk on blood coagulation because o...Objectives: Garcinia kola seeds (EAgk) (Clusiaceae) contain coagulant components use to pretreat aquaculture wastewater in Nigeria. This work was undertaken to assess the effects of EAgk on blood coagulation because of its contents. Methods: Five groups of four rats of both sexes (200 ± 5 g) received orally distilled water, phytomenadione (15 mg/kg b.w.) and garcinia kola seeds extract (250, 500 and 1000 mg/kg b.w.) for four days and after this period, bleeding time was measured by tail hemorrhage model. Activated partial thromboplastin time (aPTT) and platelet count were determined by coagulometer and hematological analyzer respectively. Blood red cells protection of EAgk was measured by the methods of 2,2’-Azobis(2-methylpropionamidine) dihydrochloride (AAPH)-induced hemolysis and inhibition of 2,2-Diphenyl-1-picryl hydrazyl (DPPH) radical and hydrogen peroxide. Results: EAgk at 1000 mg/kg b.w. induced a significant decrease in bleeding time from 420 ± 27.3 s to 157.5 ± 18.9 s. The platelet count of group of rat treated with EAgk (1000 mg/kg b.w.) increased significantly (p 0.05, n = 4). EAgk inhibited hemolysis, DPPH radical and hydrogen peroxide with IC50 values of 1.02 ± 0.2;3.2 × 10?2 ± 0.12 and 1.01 ± 0.5 mg/mg respectively. Conclusions: EAgk exhibits hemostatic effects, which could justify the presence of coagulant components in the extract. Erythrocytes’ protective activity of Garcinia kola seeds may be due to free radicals and hydrogen peroxide inhibition.展开更多
<em>Garcinia kola</em> Heckel, called “petit cola” in C<span style="white-space:nowrap;">ô</span>te d’Ivoire and “bitter kola” in Nigeria, is a Non-Timber Forest Product...<em>Garcinia kola</em> Heckel, called “petit cola” in C<span style="white-space:nowrap;">ô</span>te d’Ivoire and “bitter kola” in Nigeria, is a Non-Timber Forest Product of great socioeconomic importance. Unfortunately, this species is threatened due to overexploitation and deforestation. This study tested the effect of leaf area on stem cuttings to regenerate vegetatively in a non-mist poly-propagator without using exogenous hormones. Three stem cuttings types: greenwood, softwood and hardwood (12 - 15 cm in length) were collected from 24-month years old seedlings. The two top leaves of each cutting type were conserved at different leaf area: 0 cm<sup>2</sup>, 28.25 cm<sup>2</sup>, 56.5 cm<sup>2</sup>, 84.75 cm<sup>2</sup> and 113 cm<sup>2</sup> (entire leaf area). Observations were made on rooting, sprouting and leafing abilities of cuttings depending to treatments applied. Results showed that all cutting types have presented good ability to shooting and rooting. Cuttings with 113 cm<sup>2</sup> leaf areas presented the best rooting (94.44% ± 2.42%) and shouting (95.55% ± 2.42%) percentage and longest primary root length (12.03 ± 0.50 cm). Hardwood, softwood and greenwood cuttings with 113 cm<sup>2</sup> leaf area had the best rooting percentage (96.66% ± 3.33%, 96.66% ± 5.77% and 90.00% ± 5.77% respectively). The longest primary root length (13.50 ± 0.97 cm) was observed to greenwood cuttings with 113 cm<sup>2</sup> leaf area. Regenerated plants in the forest presented well survival percentage (96.66%). This study shows that it is possible to regenerate entire plants by cuttings without using external hormones in non-mist poly-propagator.展开更多
文摘Ten novel xanthones,garpedunxanthones A-G(1-5,6a/6b,7a/7b) and nujiangxanthone Q(8),along with sixteen known analogs(9-24),were isolated from Garcinia pedunculata and G.nujiangensis.Their structures were elucidated through high-resolution electrospray ionization mass spectrometry(HR-ESI-MS) data,comprehensive nuclear magnetic resonance(NMR) spectroscopic analyses,and electronic circular dichroism(ECD) calculations.All compounds without cytotoxicity were assessed for anti-inflammatory properties by measuring the inhibition of nitric oxide(NO) production in lipopolysaccharide(LPS)-induced RAW264.7cells.Structure-activity relationships are also discussed.Compounds 7b,19,and 21 exhibited significant anti-inflammatory activity with IC_(50) values of 16.44±0.69,14.28±0.78,and 10.67±3.28 μmol·L^(-1),respectively.Enzyme-linked immunosorbent assay(ELISA) demonstrated that compounds 7b,19,and 21 inhibited the expression of pro-inflammatory cytokines TNF-α and IL-6 in a dose-dependent manner.The inhibitory effect of compo und 21 on IL-6 at 20 μmol·L^(-1)was comparable to that of the positive control.In network pharmacology studies,potential targets of compounds and inflammation were identified from PharmMapper and GeneCards databases.Gene Ontology(GO) and Kyoto Encyclopedia of Genes and Genomes(KEGG) enrichment analysis revealed that the overlapped targets were intricately associated with major pathogenic processes linked to inflammation,including positive regulation of mitogen-activated protein kinase(MAPK) cascade,protein kinase activity,NO synthase regulator activity,MAPK signaling pathway,and EGFR tyrosine kinase inhibitor resistance.
基金the National Natural Science Foundation of China （No. 30670215）
文摘Two novel xanthones, 1,6-dihydroxy-4,5-dimethoxyxanthone （1） and 1,5,6-trihydroxy-7,8-di（3-methyl-2-butenyl）-6＇,6＇-dimethylpyrano（2＇,3＇：3,4）xanthone （2） were isolated from the bark of Garcinia xanthochymus by normal phase and reverse phase silica gel column chromatography. Their structures were elucidated by spectroscopic methods, especially 2D-NMR techniques.
基金supported by the National Natural Science Foundation of China(No.31370379)the National Natural Science Foundation Youth Project Financing(No.81201610)+1 种基金State Ethnic Affairs Commission Research Project(No.CMZY13012)Universities of Hubei Province Outstanding Youth Scientific Innovation Team Plan(No.T201220)
文摘The aim of the present study was to investigate the protective effects and underlying mechanisms of Garcinia xanthochymus, a perennial medicinal plant native to Yunnan, China, against H2 O2-induced oxidative damage in rat pheochromacytoma PC12 cells. Preincubation of PC12 cells with fruit Et OAc fraction(fruit-EFr., 12.5–50 μmol·L^(-1)) of G. xanthochymus for 24 h prior to H_2O_2 exposure markedly improved cell viability and increased the activities of antioxidant enzymes(superoxide dismutase, catalase, and heme oxygenase-1 [HO-1]), prevented lactate dehydrogenase release and lipid peroxidation malondialdehyde production, attenuated the decrease of matrix metalloproteinases(MMP), and scavenged reactive oxygen species(ROS). Fruit-EFr. also reduced BAX and cytochrome C expression and improved BCL-2 expression, thereby decreasing the ratio of BAX to BCL-2. Fruit-EFr. activated the nuclear translocation of NRF2 to increase HO-1 and induced the phosphorylation of AKT. Its cytoprotective effect was abolished by LY294002, a specific inhibitor of PI3 K. Taken together, the above findings suggested that fruit-EFr.of G. xanthochymus could enhance cellular antioxidant defense capacity, at least in part, through upregulating HO-1 expression and activating the PI3 K/AKT pathway and that it could suppress H_2O_2-induced oxidative damage via PI3 K/AKT and NRF2/HO-1 signaling pathways.
基金partially supported by the Intermtional Islamic University Malaysia(HUM)through EDWB1002-350
文摘Objective:To study the chemical constituents of stembark of Garcinia malaccenm（G.malaccenm） together with apoptotic.antimicrobial and antioxidant activities.Methods:Purification and structure elucidation were carried out by chromatographic and spectroscopic techniques, respectively.MTT and trypan blue exclusion methods were performed to study the cytotoxic activity.Antibacterial activity was conducted by dise diffusion and microdilulion methods, whereas antioxidant activities were done by ferric thiocyanate method and DPPH radical scavenging.Results:The phylochemical study led lo the isolation ofα,β-mangostin and cycloarl-24-en-3β-ol.α-Mangostin exhibited cytotoxic activity against HSC-3 cells with an IC<sub>50</sub> of 0.33μM.β- andα-mangostin showed activity against K562 cells with IC<sub>50</sub> of 0.40μM and 0.48μM,respectively,α-Mangostin was active against Gram-positive bacteria, Staphylococcus aureus（S.aureus） and Bacilus anthracis（B.anthmcis） with inhibition zone and MIC value of（19 mm;0.02S mg/mL） and（20 mm;0.013 mg/mL）,respectively.In antioxidant assay,α-mangostin exhibited activity as an inhibitor of lipid peroxidation.Conclusions:G.malaccenm presenceα- andβ-mangostin and cycloart-24-en-3β-ol.β-Mangostin was found very active against H.SC-3 cells and KS62.The results suggest that mangoslins derivatives have the potential to inhibit the growth of cancer cells by inducing apoptosis.In addition,α-andβ-mangostin was found inhibit the growth of Cram-positive pathogenic bacteria and also showed the activity as an inhibitor of lipid peroxidation.
基金Supported by Grants from the Center of Excellence for Innovation in Chemistry,Commission on Higher Education,No 48-03-3-00-144Faculty of Medicine,No 51-03-2-00-008 and Khon Kaen University,No 50-03-1-01-005,Research Funds,Khon Kaen University,Thailand
文摘AIM:To investigate the growth inhibitory mechanism of four caged xanthones from Garcinia hanburyi in cholangiocarcinoma(CCA) KKU-100 and KKU-M156 cells.METHODS:Four caged xanthones,selected on the basis of their anticancer potency and chemical structure diversities(i.e.isomorellin,isomorellinol,forbesione and gambogic acid) were used in this study.Growth inhibition of these caged xanthones was determined using the sulforhodamine B assay.Induction of apoptosis was assessed by observing cell morphology,ethidium bromide and acridine orange staining and DNA fragmentation assay.Levels of apoptotic-related gene and protein expressions were determined by a real-time reverse transcriptase polymerase chain reaction and Western blotting analysis,respectively.RESULTS:The compounds were found to inhibit growth of both cell lines in a dose-dependent manner and also showed selective cytotoxicity against the cancer cells when compared with normal peripheral blood mononuclear cells.Growth suppression by these compounds was due to apoptosis,as evidenced by the cell morphological changes,chromatin condensation,nuclear fragmentation,and DNA ladder formation.At the molecular level,these compounds induced down-regulation of Bcl-2 and survivin proteins with up-regulation of Bax and apoptosisinducing factor proteins,leading to the activation of caspase-9 and-3 and DNA fragmentation.The functional group variations did not appear to affect the anticancer activity with regard to the two CCA cell lines;however,at a mechanistic level,isomorellinol exhibited the highest potency in increasing the Bax/Bcl-2 protein expression ratio(120 and 41.4 for KKU-100 and KKU-M156,respectively) and in decreasing survivin protein expression(0.01 fold as compared to control cells in both cell lines).Other activities at the molecular level indicate that functional groups on the prenyl side chain may be important.CONCLUSION:Our findings for the first time demonstrate that four caged xanthones induce apoptosis in CCA cells which is mediated through a mitochondriadependent signaling pathway.
基金Supported by the TWAS research grant 14-062 RG/BIO/AS_GNAFOSTED grant 106-NN.02–2016.19National Research Council of Thailand(NRCT)and Center of Excellence for Innovation in Chemistry(PERCH-CIC)
文摘Objective: To isolate a-mangostin(AMG) from the peels of mangosteen(Garcinia mangostana L.), grown in Vietnam, and to investigate antibiofilm activity of this compound against three Staphylococcus aureus(S. aureus) strains, one of which was methicillin-resistant S. aureus(MRSA) and the other two strains were methicillinsensitive S. aureus(MSSA).Methods: AMG in n-hexane fraction was isolated on a silica gel column and chemically analyzed by HPLC and NMR. The antibiofilm activity of this compound was investigated by using a 96-well plate model for the formation of biofilms. Biofilm biomass was quantified using crystal violet. The viability of cells was observed under confocal microscopy using LIVE/DEAD Bac Light stains. Biofilm composition was determined using specific chemical and enzyme tests for polysaccharide, protein and DNA. Membranedamaging activity was assayed by measuring the hemolysis of human red blood cells in presence of AMG.Results: The results indicated that the isolated AMG, with a purity that exceeded 98%,had minimal inhibitory concentrations in the range of 4.6–9.2 mmol/L for the three strains tested. Interestingly, the MSSA strains were more sensitive to AMG than the MRSA strain. Minimal bactericidal concentrations were 2-fold higher than the minimal inhibitory concentration values for the three strains, indicating that AMG was a bactericidal compound. AMG also prevented biofilm formation effectively, albeit that again the MRSA strain was the most resistant. Interestingly, biofilms of the MRSA strain contained protein as a main component of the extracellular matrix, whereas this was polysaccharide in the MSSA strains. This might relate to the resistance of the MRSA 252 strain to AMG.Assays using human red blood cells indicated that AMG caused significant membrane damage with 50% of cell lysis occurred at concentration of about 36 mmol/L.Conclusions: Our results provide evidence that the isolated AMG has inhibitory activity against biofilm formation by S. aureus, including MRSA. Thus, isolated AMG proposes a high potential to develop a novel phytopharmaceutical for the treatment of MRSA.
文摘A new caged polyprenylated xanthone, gambogic aldehyde （1）, was isolated from the resin of Garcinia hanburyi. Its structure was elucidated on the basis of spectral data including 1D and 2D NMR data. In addition, the antiproliferative ability of compound 1 was determined in mouse leukemia P388 and P388/ADR cells.
基金Supported by The Basic Science Research Program, No.2011-0022387the SRC program, Center for Food and Nutritional Genomics: No. 2012-0000644 through the National Research Foundation of Korea funded by the Ministry of Education,Science and Technology
文摘AIM: To investigate long-term effects of Garcinia Cambogia (GC), weight-loss supplement, on adiposity and non-alcoholic fatty liver disease in obese mice. METHODS: Obesity-prone C57BL/6J mice were fed a high-fat diet (HFD, 45 kcal% fat) with or without GC (1%, w/w) for 16 wk. The HFD contained 45 kcal% fat, 20 kcal% protein and 35 kcal% carbohydrate. They were given free access to food and distilled water, and food consumption and body weight were measured daily and weekly, respectively. Data were expressed as the mean ± SE. Statistical analyses were performed using the statistical package for the social science software program. Student's t test was used to assess the differences between the groups. Statistical significance was considered at P < 0.05. RESULTS: There were no significant changes in body weight and food intake between the groups. However, the supplementation of GC significantly lowered visceral fat accumulation and adipocyte size via inhibition of fatty acid synthase activity and its mRNA expression in visceral adipose tissue, along with enhanced enzymatic activity and gene expression involved in adipose fatty acid β-oxidation. Moreover, GC supplementation resulted in significant reductions in glucose intolerance and the plasma resistin level in the HFD-fed mice. However, we first demonstrated that it increased hepatic collagen accumulation, lipid peroxidation and mRNA levels of genes related to oxidative stress (superoxide dismutase and glutathione peroxidase) and inflammatory responses (tumor necrosis factor-α and monocyte chemoattractant protein-1) as well as plasma alanine transaminase and aspartate transaminase levels, although HFD-induced hepatic steatosis was not altered. CONCLUSION: GC protects against HFD-induced obesity by modulating adipose fatty acid synthesis and β-oxidation but induces hepatic fibrosis, inflammation and oxidative stress.
基金support of this work by the National Natural Science Foundation of China (No.20702061)
文摘A novel caged-prenylxanthone xanthone,neobractatin(1),was isolated from the twig of Garcinia bracteata.Its structure was elucidated by spectroscopic methods,especially 2D NMR techniques.
基金supported by The National Research Couneil of Thailand.(Grant No.034/2556)Thammasat University and the Cammission on Higher Education,Ministry of Education of Thailand(NRI Project)
文摘Objective:To investigate the antimalarial activity and toxicity of the crude ethanolic extract of its pericarp both in vitro and in vim.Methods:The antimalarial activity of Gareinja mangostana(G.mangostana)Linn.extract against 3D7 and Kl Plasmodium falciparum(P.falciparum)clone were assessed using SYBR green I-based assay.A 4-day suppressive test of Plasmodium berghei{P.berghei)infected mouse was performed to investigate in vivo antimalarial activity.Results:The in vitro antimalarial activity was seleclive(SI>5?and classified as weak and good lo moderate activity against both 3D7 and K1 P.falciparum,clones with median IC_(50)(range)values of 11.12(10.94-11.29)and 7.54(6.80-7.68)μg/mL,respectively.The extract was considered nontoxic to mice.The maximum tolerated doses for acute and subacute toxicity in mice were 5 000and 2 000 mg/kg,respectively.Median(range)parasite density on day 4 of the negative control group(25%Tween-80),mice treated with 250,500,1000,and 2 000 mg/kg body weight of the extract,and 10 mg/kg body weight of chloroquine for 14 d were 12.8(12.2-13.7),11.4(9.49-13.8),11.6(9.9-12.5),11.7(10.6-12.8),10.9(9.4-11.6)and 0(0-0)%respectively.Parasite density on day 4in the control group treated with Tween-80 was higher than the groups treated with chloroquine and all dose levels of the extract.Conclusions:G.mangostana linn,showed weak antimalarial activity of the extract both in vitro and in vivo could be due to limitation of absorption of the active compounds.
文摘BACKGROUND Herbal supplements(HS)for weight loss are perceived to be“safe”and“natural”,as advertised in ads,however,hepatotoxicity can be associated with consumption of some HS.Use of HS may be missed,as the patient may not report these unless specifically asked about these products,since they are often not thought of as medications with potential side effects or interaction potential.CASE SUMMARY We reported a case of a 21-year-old female with morbid obesity who presented with abdominal pain for 1 wk associated with nausea,vomiting,anorexia and myalgias.She denied smoking tobacco,drinking alcohol,usage of illicit drugs,hormonal contraceptives,or energy drinks.There was no significant past medical or family illnesses.Her laboratory workup revealed acute liver failure.The workup for possible etiologies of acute liver failure was unremarkable.She was using a weight loss herbal supplement“Garcinia cambogia”for 4 wks.This case demonstrates the association of acute liver failure with Garcinia cambogia.CONCLUSION Medical reconciliation of HS should be performed in patients with suspected acute liver failure and early discontinuation of HS can prevent further progression of drug induced hepatoxicity.
文摘Objective:To assess the neuroprotective effects of aqueous extract of Garcinia kola on neurotoxin administered malnourished mice adopting histological procedure.Methods:The study was carried out using thirty-two adult malnourished mice which were randomly assigned into four groups(n=8):A,B,C and D.Group A served as control,while the other groups served as the experimental groups.Animals in group A were fed malnourished diet ad libitum and given water liberally.Animals in group B were administered with 3-Nitropropionic acid(3-NP)(neurotoxin)only at 20 rag/kg body weight,group C were given only Garcinia kola extracts,and group D were pre-treated with Garcinia kola extracts at 200 mg/kg for seven days prior to administration of neurotoxin at 20 mg/kg body weight.After three days of neurotoxins administration in the relevant groups,the brains were excised and fixed in formal calcium for histological processing.Results:The study showed that hippocampal and cerebellar neurons of animals in group B exhibited some cellular degeneration and blood vessel blockage,which were not seen in groups A,C and D.Cresyl violet staining was least intense in group B than in groups A,C and D.Despite the fact that animals in group D has equal administration of 3-Nitropropionic acid concentration,there were no traces of neural degeneration as it was evidenced in group B.Conclusions:It is concluded that Garcinia kola has protective effects on the neurons of the hippocampus and cerebellum of malnourished mice.
基金Supported by Hibah Doktor scheme of Directorate General of Higher Education,Ministry of Education and Culture,Republic of Indonesia(Grant No.DIPA 09/UN.16/D-DD/2014)
文摘Objective:To investigate the cytotoxic effect of ethanol extract of the stem bark of asam kandis[Garcinia cowa Roxb.(G.cowa)]on T47 D breast cancer cell line.Methods:The cytotoxicity of ethanol extract was carried out against human breast cancer cell line(T47D) by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide colorimetric assay.The extract was added at various concentrations(0.1.1,10 and 100 μg/mL).The level of cytotoxicity was determined by calculating the level of IC_(50),that was based on the percentage of the cell death after 24 h treatment with the extract.Cell morphological changes were observed by using inverted microscope.Results:The 3-(4.5-dimelhylthiazol-2-yl)-2.5-diphenyltelrazolium bromide assay showed that ethanol extract of G.cowa exhibited significant cytotoxic effect on T47 D with IC_(50) value of(5.10+1.68) μg/mL.Morphological alteration of the cell lines after exposure to ethanol extract of G.cowa was observed under phase contrast microscope in a dosc-dependent manner.ConclusionsThe results suggest the possible use of ethanol extract of asam kandis for preparing herbal medicine for cancer-related ailments.
基金financially supported by the 100 Leading Talents of Guizhou Province (fund for W. Zhu and X. Hao)the Science and Technology Project of Guizhou (No. QKHT Z-20144007)the Academician Workstation of Guizhou (No. QKH YSZ2015-4009)
文摘Citridones E-G (1-3), three new phenylpyridone derivatives together with two known curvularins (4 and 5) were isolated from the solid culture of the endophytic fungus Penicillium sumatrense GZWMJZ-313 in Garcinia multiflora. The structures of new compounds were determined in the light of spectroscopic data,X-ray and ECD calculation. Compounds 1 and 3 are racemates, while compound 2 is optically pure.Compounds 1 and 4 showed antibacterial and antifungal activities against Staphylococcus aureus,Pseudomonas aeruginosa, Clostridium perfringens, Escherichia coli and Candida albicans with MIC values ranging from 8 μg/mL to 64 μg/mL.
文摘Insecticidal effects of different doses of the dust and methanol extracts of Garcinia kolae on Callosobruchus maculatus and Sitophilus zeamais were tested. The dust had no significant effect on the two insects, none of them died even at 3 d after treatment. The methanol extracts, however, had rapid lethal effects on both C. maculatus and S. zeamais. The mortality of C. maculatus by the lowest concentration of methanol extracts ranged from 95%-100% whereas in S. zeamais, the mortality ranged from 87.5%-100% and 70%-100% in concentrations of 1 g extract＋3 ml methanol and 1 g extract＋5 ml methanol, respectively, from 24 to 48 h. The least concentration of 1 g extract＋l 5 ml methanol had no significant lethal effect on Sitophilus zeamais.
文摘Objectives: Garcinia kola seeds (EAgk) (Clusiaceae) contain coagulant components use to pretreat aquaculture wastewater in Nigeria. This work was undertaken to assess the effects of EAgk on blood coagulation because of its contents. Methods: Five groups of four rats of both sexes (200 ± 5 g) received orally distilled water, phytomenadione (15 mg/kg b.w.) and garcinia kola seeds extract (250, 500 and 1000 mg/kg b.w.) for four days and after this period, bleeding time was measured by tail hemorrhage model. Activated partial thromboplastin time (aPTT) and platelet count were determined by coagulometer and hematological analyzer respectively. Blood red cells protection of EAgk was measured by the methods of 2,2’-Azobis(2-methylpropionamidine) dihydrochloride (AAPH)-induced hemolysis and inhibition of 2,2-Diphenyl-1-picryl hydrazyl (DPPH) radical and hydrogen peroxide. Results: EAgk at 1000 mg/kg b.w. induced a significant decrease in bleeding time from 420 ± 27.3 s to 157.5 ± 18.9 s. The platelet count of group of rat treated with EAgk (1000 mg/kg b.w.) increased significantly (p 0.05, n = 4). EAgk inhibited hemolysis, DPPH radical and hydrogen peroxide with IC50 values of 1.02 ± 0.2;3.2 × 10?2 ± 0.12 and 1.01 ± 0.5 mg/mg respectively. Conclusions: EAgk exhibits hemostatic effects, which could justify the presence of coagulant components in the extract. Erythrocytes’ protective activity of Garcinia kola seeds may be due to free radicals and hydrogen peroxide inhibition.
文摘<em>Garcinia kola</em> Heckel, called “petit cola” in C<span style="white-space:nowrap;">ô</span>te d’Ivoire and “bitter kola” in Nigeria, is a Non-Timber Forest Product of great socioeconomic importance. Unfortunately, this species is threatened due to overexploitation and deforestation. This study tested the effect of leaf area on stem cuttings to regenerate vegetatively in a non-mist poly-propagator without using exogenous hormones. Three stem cuttings types: greenwood, softwood and hardwood (12 - 15 cm in length) were collected from 24-month years old seedlings. The two top leaves of each cutting type were conserved at different leaf area: 0 cm<sup>2</sup>, 28.25 cm<sup>2</sup>, 56.5 cm<sup>2</sup>, 84.75 cm<sup>2</sup> and 113 cm<sup>2</sup> (entire leaf area). Observations were made on rooting, sprouting and leafing abilities of cuttings depending to treatments applied. Results showed that all cutting types have presented good ability to shooting and rooting. Cuttings with 113 cm<sup>2</sup> leaf areas presented the best rooting (94.44% ± 2.42%) and shouting (95.55% ± 2.42%) percentage and longest primary root length (12.03 ± 0.50 cm). Hardwood, softwood and greenwood cuttings with 113 cm<sup>2</sup> leaf area had the best rooting percentage (96.66% ± 3.33%, 96.66% ± 5.77% and 90.00% ± 5.77% respectively). The longest primary root length (13.50 ± 0.97 cm) was observed to greenwood cuttings with 113 cm<sup>2</sup> leaf area. Regenerated plants in the forest presented well survival percentage (96.66%). This study shows that it is possible to regenerate entire plants by cuttings without using external hormones in non-mist poly-propagator.
