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PubMed2007

High-performance liquid chromatography and LC-ESI-MS method for the identification and quantification of two biologically active polyisoprenylated benzophenones xanthochymol and isoxanthochymol in different parts of Garcinia indica.

A reverse-phase high-performance liquid chromatographic method was developed for qualitative and quantitative analysis of xanthochymol (1), and isoxanthochymol (2) in the fruit rinds, leaves and seed pericarps of Garcinia indica with confirmation using PDA detection and electrospray ionization MS. Absorption at 276 nm was chosen as the measuring wavelength at which resolution and baseline separation of compounds (1) and (2) could be obtained. The identity of the above two isomeric compounds (1) and (2) in the samples was unambiguously determined by their respective quasi-molecular ion [M - H]- in ESI-MS. Compounds (1) and (2) were qualitatively and quantitatively analyzed in the above three samples of Garcinia indica. The overall analytical procedure is rapid and reproducible and is considered for the analysis of the above two compounds.

Benzophenones↗
PubMed2005

High dose of Garcinia cambogia is effective in suppressing fat accumulation in developing male Zucker obese rats, but highly toxic to the testis.

We investigated the ability of Garcinia cambogia extract containing (-)-hydroxycitric acid (HCA) to suppress body fat accumulation in developing male Zucker obese (fa/fa) rats. We also examined histopathologically the safety of its high doses. Diets containing different levels of HCA (0, 10, 51, 102 and 154 mmol/kg diet) were fed to 6-week-old rats for 92 or 93 days. Each diet group was pair-fed to the 154 mmol HCA/kg diet group. Epididymal fat accumulation and histopathological changes in tissues were observed. The highest dose of HCA-containing Garcinia cambogia (154 mmol HCA/kg diet) showed significant suppression of epididymal fat accumulation in developing male Zucker obese rats, compared with the other groups. However, the diets containing 102 mmol HCA/kg diet and higher (778 and 1244 mg HCA/kg BW/d, respectively) caused potent testicular atrophy and toxicity, whereas diets containing 51 mmol HCA/kg diet (389 mg HCA/kg BW/d) or less did not. Accordingly, 51 mmol HCA/kg diet (389 mg HCA/kg BW/d) was deemed to be the no observed adverse effect level (NOAEL).

ATP Citrate (pro-S)-Lyase↗
PubMed2005

Antiaflatoxigenic and antioxidant activities of Garcinia extracts.

The effect of hexane and chloroform extracts from the fruit rinds of Garcinia cowa and Garcinia pedunculata on the growth and aflatoxin production in Aspergillus flavus was studied using peanut powder as a model food system. The growth of A. flavus was completely inhibited by the hexane and chloroform extracts from G. cowa and chloroform extract from G. pedunculata at 3000 ppm concentration, which was considered as the minimum inhibitory concentration (MIC). The MIC for the hexane extract of G. pedunculata was at 4000 ppm. Both the extracts from G. cowa inhibited aflatoxin B1 production upto 100% at a lower concentration of 2000 ppm. It was observed that, at lower concentration of the extracts from G. cowa and G. pedunculata, the degree of inhibition of aflatoxin production was much higher than the inhibition of fungal growth. The hexane and chloroform extracts from G. cowa and G. pedunculata were also studied for their antioxidant capacity by the formation of phosphomolybdenum complex at 100 ppm concentration and reducing power by potassium ferricyanide reduction method at various concentrations. Hexane and chloroform extracts from G. cowa showed higher antioxidant capacity than G. pedunculata extracts. Similarly, both the extracts from G. cowa showed higher reducing power than the extracts from G. pedunculata. The antiaflatoxigenic activities of the extracts from G. cowa and G. pedunculata may be due to their effective antioxidative properties, which could suppress the biosynthesis of aflatoxin.

Aflatoxins↗
PubMed2004

Antiproliferation, antioxidation and induction of apoptosis by Garcinia mangostana (mangosteen) on SKBR3 human breast cancer cell line.

This study was designed to determine the antiproliferative, apoptotic and antioxidative properties of crude methanolic extract (CME) from the pericarp of Garcinia mangostana (family Guttiferae) using human breast cancer (SKBR3) cell line as a model system. SKBR3 cells were cultured in the presence of CME at various concentrations (0-50 microg/ml) for 48 h and the percentage of cell viability was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-di phenyl tetrazolium bromide (MTT) assay. CME showed a dose-dependent inhibition of cell proliferation with ED(50) of 9.25+/-0.64 microg/ml. We found that antiproliferative effect of CME was associated with apoptosis on breast cancer cell line by determinations of morphological changes and oligonucleosomal DNA fragments. In addition, CME at various concentrations and incubation times were also found to inhibit ROS production. These investigations suggested that the methanolic extract from the pericarp of Garcinia mangostana had strong antiproliferation, potent antioxidation and induction of apoptosis. Thus, it indicates that this substance can show different activities and has potential for cancer chemoprevention which were dose dependent as well as exposure time dependent.

Antineoplastic Agents↗
PubMedDate not supplied

Possible anti-atherogenic effect of kolaviron (a Garcinia kola seed extract) in hypercholesterolaemic rats.

1. The hypolipidaemic effect of kolaviron, a mixture of Garcinia biflavonoid 1 (GB1), Garcinia biflavonoid 2 (GB2) and kolaflavanone, used in the treatment of various ailments in southern Nigeria, was investigated in rats. The ability of Questran (Bristol-Myers Squibb, Hounslow, UK), a hypolipidaemic therapeutic drug, to attenuate hypercholesterolaemia in rats was also examined. 2. In order to assess the hypolipidaemic effect of this extract in experimental animals, thiobarbituric acid-reactive substances (TBARS), cholesterol, phospholipid, low-density lipoprotein-cholesterol (LDL-C), high-density lipoprotein-cholesterol and triglyceride levels were determined in the plasma and liver. 3. Cholesterol administered orally to rats at a dose of 30 mg/0.3 mL five times a week for 8 consecutive weeks resulted in a significant increase (P<0.001) in the relative weight of the heart of hypercholesterolaemic animals compared with control. However, cotreatment with kolaviron and Questran ameliorated the cholesterol-induced enlargement of the heart. Kolaviron (100 and 200 mg/kg) elicited 88.5 and 87.4% reductions, respectively, in plasma cholesterol levels of pretreated animals compared with the cholesterol-fed group. In addition, kolaviron produced a significant decrease (P<0.05) in post-mitochondrial fraction (PMF) cholesterol levels in treated animals compared with untreated hypercholesterolaemic animals. Similarly, Questran significantly decreased (P<0.05) the cholesterol-induced increase in plasma cholesterol levels compared with untreated hypercholesterolaemic animals. In addition, (100 and 200 mg/kg) significantly (P<0.05) decreased plasma LDL-C levels by over 70% in treated animals compared with untreated hypercholesterolaemic animals. Similarly, kolaviron significantly decreased (P<0.05) PMF LDL-C levels by over 60% in treated animals compared with untreated hypercholesterolaemic animals. 4. The significantly (P<0.05) higher values of plasma and PMF triglycerides obtained in cholesterol-fed animals compared with control animals were unaltered following cotreatment with kolaviron and Questran. In the present study, there was a significant decrease (P<0.05) in plasma formation of malondialdehyde in kolaviron- and Questran-treated animals compared with untreated hypercholesterolaemic animals. 5. The results of the present study demonstrate that kolaviron exerts a hypocholesterolaemic effect and reduces the relative weight of the heart in cholesterol-fed animals. This reduction and the favourable lipid profile indicate a possible anti-atherogenic property of the extract.

Animals↗
PubMed2006

Antimicrobial activity in cultures of endophytic fungi isolated from Garcinia species.

The aim of the present study was to screen for antimicrobial activity in endophytic fungi isolated from surface sterilized leaves and branches of five Garcinia plants, G. atroviridis, G. dulcis, G. mangostana, G. nigrolineata and G. scortechinii, found in southern Thailand. Fermentation broths from 377 isolated fungi were tested for antimicrobial activity by the agar diffusion method. Minimum inhibitory concentrations (MICs) were obtained for crude ethyl acetate extracts. Seventy isolates (18.6%) displayed antimicrobial activity against at least one pathogenic microorganism, such as Staphylococcus aureus, a clinical isolate of methicillin-resistant S. aureus, Candida albicans and Cryptococcus neoformans. The results revealed that 6-10%, 1-2% and 18% of the crude ethyl acetate extracts inhibited both strains of S. aureus (MIC 32-512 microg mL(-1)), Ca. albicans and Cr. neoformans (MIC 64-200 microg mL(-1)), and Microsporum gypseum (MIC 2-64 microg mL(-1)), respectively. Isolates D15 and M76 displayed the strongest antibacterial activity against both strains of S. aureus. Isolates M76 and N24 displayed strong antifungal activity against M. gypseum. Fungal molecular identification based on internal transcribed spacer rRNA gene sequence analysis demonstrated that isolates D15 (DQ480353), M76 (DQ480360) and N24 (DQ480361) represented Phomopsis sp., Botryosphaeria sp. and an unidentified fungal endophyte, respectively. These results indicate that some endophytic fungi from Garcinia plants are a potential source of antimicrobial agents.

Anti-Infective Agents↗
PubMed2006

Hepatoprotection of D-galactosamine-induced toxicity in mice by purified fractions from Garcinia kola seeds.

The hepatoprotective effect of a biflavonoid complex, kolaviron, and its fractions from Garcinia kola seeds, together with the possible mechanisms involved was investigated in mice intoxicated with a single dose of D-galactosamine (GalNH(2)). Likewise, the ability of vitamin E to attenuate the toxicity was examined. Kolaviron, was separated by thin-layer chromatographic technique into three fractions; Fraction I, Fraction II and Fraction III with RF values of 0.48, 0.71 and 0.76, respectively. Pretreatment with kolaviron, fraction I and fraction II at a dose of 100 mg/kg for seven consecutive days before challenge with a single dose of GalNH(2) (800 mg/ kg) significantly (P<0.05) decreased serum alanine (ALT) and aspartate (AST) aminotransferases by 67%, 70%, 71% and 39%, 35%, 46%, respectively over GalNH(2)-only intoxicated mice. Vitamin E elicited respectively 65% and 39% reduction in the GalNH(2)-induced increase in the activities of these enzymes. In addition, pretreatment with kolaviron and fraction II significantly (P<0.05) decreased the activity of microsomal gamma-glutamyl transferase (gamma-GT) by 42% and 46%, respectively. Administration of kolaviron to GalNH(2)-intoxicated mice also restored glucose-6-phosphatase to level that was comparable to the control (P<0.05). These extracts except fraction III prevented the accumulation of serum and microsomal lipid peroxidation products, and also prevented the depletion of reduced glutathione (GSH) levels in the liver of GalNH(2)-intoxicated mice. Kolaviron, fraction I and fraction II at a dose of 100 mg/kg caused an induction of glutathione-S-transferase (GSH transferase) and uridyl glucuronosyl transferase (UDPGT) activities by 31%, 34%, 35% and 29%, 65%, 56%, respectively. GalNH(2)-induced toxicity was essentially prevented as indicated by a liver histopathologic study of liver slices from mice pretreated with kolaviron, fraction I and fraction II. This study shows that treatment with kolaviron, fraction I and fraction II (purified fractions from Garcinia kola) appeared to enhance the recovery from GalNH(2)-induced hepatotoxicity, and that the fractions I and II may therefore be responsible for the observed antihepatotoxic effect of kolaviron. This protection may be due to the ability of these extracts to induce the expression of phase II drug metabolizing enzymes.

Animals↗
PubMed2005

Screening for tyrosinase inhibitors among extracts of seashore plants and identification of potent inhibitors from Garcinia subelliptica.

The tyrosinase inhibitory activity of methanol extracts of the leaves of 39 plant species growing on the seashore of Iriomote island (Okinawa, Japan) was investigated. The extracts of Hibiscus tiliaceus, Carex pumila, and Garcinia subelliptica showed potent activity among them. The inhibitors in the extract of Garcinia subelliptica were purified by assay-guided fractionation to give two biflavonoids. These were known compounds (2R,3S-5,7,4',5'',7'',3''',4'''-heptahydroxy flavanone[3-8''] flavone and 5,7,4',5'',7'',3''',4'''-heptahydroxy[3-8''] biflavanone), although their strong inhibitory activity toward tyrosinase is revealed for the first time in this work. One of these biflavonoids (2R,3S-5,7,4',5'',7'',3''',4'''-heptahydroxy flavanone[3-8''] flavone) showed much stronger activity (IC50 2.5 microM) than that of kojic acid (IC50 9.1 microM) when L-tyrosine was used as the substrate.

Flavanones↗
PubMed2002

Brief chewing of Garcinia manii stick reverses reduced saliva pH after a glucose rinse.

BACKGROUND: A popular variety of wood, pieces of which are chewed as an oral hygiene practice in Southern Ghana, was tested for its capacity to reverse experimentally lowered pH of saliva. This was done to determine whether (Garcinia manii) stick-chewing neutralizes acidogenic challenge to teeth, and thereby potentially affords dental caries prevention benefit. MATERIAL/METHODS: Seventy-two volunteer medical students gave (baseline) saliva samples by spitting 3-4 times into a 25 ml conical flask. They then rinsed their mouths with a five-percent aqueous solution of glucose. Subsequent to the glucose rinse, half of the subjects (chewers), pre-selected by drawing lots, chewed a popular chewing stick Garcinia manii for five minutes, while the other half (controls) did not. The pH of saliva samples given by the volunteers at various time intervals was measured using a Kent EIL 7020 pH meter, and the results were analysed by the Analysis of Variance (Anova) method. RESULTS: As expected, saliva pH was reduced in both groups after the glucose rinse, but increased significantly faster in stick chewers compared with controls. CONCLUSIONS: It is suggested from this study that brief (Garcina manii) stick-chewing confers a caries prevention/control benefit by reversing acidogenic challenge to teeth.

Adult↗
PubMed2007

Reduction of adipose tissue and body weight: effect of water soluble calcium hydroxycitrate in Garcinia atroviridis on the short term treatment of obese women in Thailand.

Fifty obese women with a body mass index (BMI) over 25 kg/m(2) were randomly allocated into two groups, 25 in each. Group 1, with a mean (+/-SEM) age of 40.0+/-2 years, received water soluble calcium hydroxycitrate (HCA) as Garcinia atroviridis. Group 2, with a mean age of 35.6+/-1.8 years, received placebo. All subjects were recommended a similar diet with 1000 Kcal/day. The trial lasted for 2 months. At baseline the means BMI of Group 1 and Group 2 were 27.5+/-0.2 kg/m(2) and 26.7+/-0.5 kg/m(2), respectively. Group 1 lost significantly more weight (2.8 vs. 1.4 kg, p<0.05) and at a greater rate than Group 2 throughout the study. The decrease in their body weight was due to a loss of fat storage as evidenced by a significant decrease in the triceps skin fold thickness. On a short-term basis, HCA in Garcinia atroviridis was an effective for weight management.

Adipose Tissue↗
PubMed1998

Garcinia cambogia (hydroxycitric acid) as a potential antiobesity agent: a randomized controlled trial.

CONTEXT: Hydroxycitric acid, the active ingredient in the herbal compound Garcinia cambogia, competitively inhibits the extramitochondrial enzyme adenosine triphosphate-citrate (pro-3S)-lyase. As a citrate cleavage enzyme that may play an essential role in de novo lipogenesis inhibition, G cambogia is claimed to lower body weight and reduce fat mass in humans. OBJECTIVE: To evaluate the efficacy of G cambogia for body weight and fat mass loss in overweight human subjects. DESIGN: Twelve-week randomized, double-blind, placebo-controlled trial. SETTING: Outpatient weight control research unit. PARTICIPANTS: Overweight men and women subjects (mean body mass index [weight in kilograms divided by the square of height in meters], approximately 32 kg/m2). INTERVENTION: Subjects were randomized to receive either active herbal compound (1500 mg of hydroxycitric acid per day) or placebo, and both groups were prescribed a high-fiber, low-energy diet. The treatment period was 12 weeks. Body weight was evaluated every other week and fat mass was measured at weeks 0 and 12. MAIN OUTCOME MEASURES: Body weight change and fat mass change. RESULTS: A total of 135 subjects were randomized to either active hydroxycitric acid (n = 66) or placebo (n = 69); 42 (64%) in the active hydroxycitric acid group and 42 (61%) in the placebo group completed 12 weeks of treatment (P = .74). Patients in both groups lost a significant amount of weight during the 12-week treatment period (P<.001); however, between-group weight loss differences were not statistically significant (mean [SD], 3.2 [3.3] kg vs 4.1 [3.9] kg; P = .14). There were no significant differences in estimated percentage of body fat mass loss between treatment groups, and the fraction of subject weight loss as fat was not influenced by treatment group. CONCLUSIONS: Garcinia cambogia failed to produce significant weight loss and fat mass loss beyond that observed with placebo.

Adult↗
PubMed2001

Impact of certain flavonoids on lipid profiles--potential action of Garcinia cambogia flavonoids.

Flavonoids from Cocos nucifera, Myristica fragrance, Saraka asoka and Garcinia cambogia exerted hypolipidaemic activity in rats. Lipid lowering activity was maximum in rats administered flavonoids (10 mg/kg BW/day) from Garcinia cambogia. A dose response study revealed biphasic activity. Higher doses were less effective in reducing lipid levels in serum and tissues, although devoid of toxic effects.

Animals↗
PubMed1985

Antihepatoxic constituents of Garcinia kola seeds.

Kolaviron, a fraction of defatted methanolic extract and biflavanones of Garcinia kola seeds significantly antagonized the lethal poisoning of mice with phalloidin. Garcinia biflavanones GB1, GB2 and kolaflavanone were isolated as the active constituents.

Animals↗
PubMed2000

Chemoprevention of 2-acetylaminofluorene-induced hepatotoxicity and lipid peroxidation in rats by kolaviron--a Garcinia kola seed extract.

The effect of kolaviron, a mixture of Garcinia biflavonoid 1 (GB1), Garcinia biflavonoid 2 (GB2) and kolaflavanone, used in the treatment of various ailments in southern Nigeria on hepatotoxicity and lipid peroxidation induced by 2-acetylaminofluorene (2-AAF) in rats was investigated. The ability of butylated hydroxyanisole (BHA) to attenuate the toxic effect of 2-AAF was also examined. Kolaviron administered orally to rats at a dose of 100mg/kg body weight twice a day for 1 week before challenge with 2-AAF (200mg/kg feed) and continuously for 3 weeks at a single dose of 200mg/kg body weight reversed the 2-AAF-mediated decrease in final body weight and relative organ weights, especially the liver. BHA was administered at a dose of 7.5g/kg feed to the animals for 4 weeks. The extract decreased significantly the 2-AAF-mediated increase in the activity of aspartate aminotransferase, alanine aminotransferase, gamma-glutamyl transferase and ornithine carbamyl transferase by 58%, 62%, 60% and 67%, respectively. BHA elicited respectively 55%, 63%, 57% and 65% reduction in the 2-AAF induced-increase in the activities of these enzymes. Histological examination of the liver slices correlated with the changes in serum enzyme alterations. Similarly, kolaviron decreased the 2-AAF reduction of 5'-nucleotidase and glucose-6-phosphatase activities by 63% and 60%, respectively while BHA elicited 59% and 61% decrease in the activities of these enzymes. Simultaneous administration of kolaviron with 2-AAF inhibited microsomal lipid peroxidation as assessed by the thiobarbituric acid reacting substances (TBARS) formation by 66%. BHA produced a 64% reduction in TBARS formation. In the present study, kolaviron appears to act as an in vivo natural antioxidant and an effective hepatoprotective agent and is as effective as BHA.

2-Acetylaminofluorene↗
PubMed1990

Histological alterations by a diet containing seeds of Garcinia kola: effect on liver, kidney, and intestine in the rat.

Histological examination of liver, kidney, and duodenum of rats fed a diet containing 10% (w/w) dry powdered seeds of Garcinia kola for 6 weeks revealed cellular changes that were not observed in pair-fed control animals. The main cellular changes observed in the rats fed on Garcinia kola diet included vacuolation of duodenal villous epithelial cells, numerous intracytoplasmic vacuoles in hepatocytes, and mild hydropic degeneration in cells of the renal proximal tubular epithelium. These changes are probably due to the flavonoids contained in G. kola seeds.

Animals↗
PubMed1993

The bronchodilator effect of Garcinia Kola.

This work investigated the bronchodilator effect of Garcinia Kola (Bitter Kola) in normal Nigerians. Nineteen undergraduate male students (17-25 years) were used for the study which involved the consumption of Garcinia Kola (15 grammes per subject) and the measurement of peak expiratory flow rate (PEFR), forced expiratory volume in one second (FEV1) and forced vital capacity (FVC) at intervals of 30 minutes up to a maximum of 90 minutes. Each subject served as his own control. There was time-dependent increases in the measured parameters. However, only the PEFR showed significant (p < 0.05) increase and this was observed at the 60th minute. This probably shows a mild bronchodilator effect of this Kola.

Adolescent↗
PubMed2003

Novel and anti-inflammatory constituents of Garcinia subelliptica.

Four novel phloroglucinol derivatives, garcinielliptones A (1), B (2), C (3), D (4), a novel triterpenoid, garcinielliptone E (5), and three known compounds were isolated from the seeds of Garcinia subelliptica. The structures, including relative configurations, were elucidated by means of spectroscopic data. Known compounds garsubellin A (6) and garcinielliptin oxide (7) showed potent inhibitory effects on the release of beta-glucuronidase, and beta-glucuronidase and histamine, respectively, from peritoneal mast cells stimulated with compound 48/80 in a concentration-dependent manner with IC(50) values of 15.6+/-2.5, and 18.2+/-3.6 and 20.0+/-2.7 microM, respectively. Compound 7 showed potent inhibitory effects on the release of beta-glucuronidase and lysozyme from neutrophils stimulated with formyl-Met-Leu-Phe(fMLP)/cytochalasin B (CB) in a concentration-dependent manner with IC(50) values of 15.7+/-3.0 and 23.9+/-3.2 microM, respectively. Compound 7 also showed potent inhibitory effect on superoxide formation from neutrophils stimulated with fMLP/CB also in a concentration-dependent manner with an IC(50) value of 17.9+/-1.5 microM.

Animals↗
PubMed2003

Terpenoids with a new skeleton and novel triterpenoids with anti-inflammatory effects from Garcinia subelliptica.

Three novel phloroglucinol derivatives, garcinielliptones F (1), H (3), and I (4), and two novel terpenoids, garcinielliptones G (2) and J (5), with a new skeleton have been isolated from the seeds of Garcinia subelliptica. Their structures, including relative configurations, were elucidated by spectroscopic methods and computer-generated molecular modeling. Compound 1 showed potent inhibitory effects on the release of beta-glucuronidase and lysozyme from rat neutrophils that had been stimulated with formyl-Met-Leu-Phe (fMLP)/cytochalasin B (CB). This effect was concentration-dependent with IC(50) values of 26.9+/-2.6 and 20.0+/-1.3 microM, respectively. Compound 1 also showed a potent concentration-dependent inhibitory effect on superoxide anion generation in rat neutrophils stimulated with fMLP/CB, with an IC(50) value of 17.0+/-0.9 microM. Compound 4 showed a potent inhibitory effect on NO production in culture media of N9 cells in response to lipopolysaccharide (LPS)/interferon-gamma (IFN-gamma) in a concentration-dependent manner with an IC(50) value of 7.4+/-0.2 microM.

Animals↗