In vitro anti-inflammatory activity and ameliorative effects on gastric ulcers of Licania rigida benth seed extract.

Licania rigida Benth., a Brazilian endemic plant, has been traditionally used for treating inflammation and stomach pain. This work investigates the anti-inflammatory and gastroprotective activities of the ethanolic extract from L. rigida seeds (EELr) by in vitro and in vivo methods. The phytochemical profile was determined and the in vitro antioxidant activity was investigated by radical scavenging and thiobarbituric acid reactive substances methods. The ovalbumin denaturation method was used with sodium diclofenac as standard for the in vitro anti-inflammatory activity assessment. Acetylsalicylic acid was used to induce gastric ulcers in male mice and then to evaluate the preventive and therapeutic gastroprotective effect of EELr, using omeprazole as the reference drug. The extract exhibited relevant amount of phenolic compounds and flavonoids, in particular, demonstrating in vitro antioxidant capacity. EELr was able to inhibit almost 60% of ovalbumin denaturation at a concentration considered low. It also prevented the decrease of biochemical markers for oxidative stress such as superoxide dismutase (SOD) and reduced glutathione (GSH) in the stomach and SOD and catalase (CAT) in the liver. EELr also significantly decreased the number of lesions as well as reduced the ulcerated area when used as therapy. The observed effect may be due to its phenolic compounds, such as chlorogenic acid, caffeic acid and tannins, as previously reported. EELr is a potential source of compounds with anti-inflammatory activity, protects the liver from oxidative damage and improves healing of aspirin-induced ulcers. This work contributes to the knowledge of L. rigida species.

Phytochemical Characterizations of Maranthes polyandra (Benth.) Prance.

Two new ursane-type triterpenoids, named Polyanside A (1) and B (2), along with eleven known compounds (3-13), were isolated and elucidated from Maranthes polyandra (Benth.) Prance. The structures of these compounds were elucidated based on chemical evidence and multiple spectroscopic data. Isolated compounds were evaluated for anti-cancer, anti-inflammatory activities, and cytotoxicity on a normal human cell line (BJ). None of them showed activity and cytotoxicity. The hexane fraction was analyzed by GC-MS, resulting in the identification of forty-one compounds. This is the first comprehensive study on the phytochemistry of M. polyandra.

Licania rigida leaf extract: Protective effect on oxidative stress, associated with cytotoxic, mutagenic and preclinical aspects.

Brazilian plant biodiversity is a rich alternative source of bioactive compounds since plant-derived extracts and/or their secondary metabolites exhibit potential properties to treat several diseases. In this context, Licania rigida Benth (Chrysobalanaceae Family), a large evergreen tree distributed in Brazilian semi-arid regions, deserves attention for its widespread use in popular medicine, although its biological properties are still poorly studied. The aim of this study was to examine (1) acute and sub-chronic oral toxicity at 2000 mg/kg dose; (2) in vitro cytotoxicity at 0.1; 1; 10; 100 or 1000 µg/ml; (3) in vivo mutagenicity at 5, 10 or 20 mg/ml, and (4) potential antioxidant protective effect of L. rigida aqueous leaf extract of (AELr). No marked apparent toxic and genotoxic effects were observed using in vitro and in vivo assays after in vitro treatment of Chinese hamster ovary cell line (CHO-K1) with AELr or in vivo exposure of Wistar rats and Drosophila melanogaster to different extract concentrations. Concerning the antioxidant effect, the extract exhibited a protective effect by decreasing lipid peroxidation as determined by malondialdehyde levels. No significant changes were observed for glutathione (GSH) levels and activities of superoxide dismutase (SOD) and glutathione peroxidase (GPx). Data demonstrate the beneficial potential of AELr to be employed for therapeutic purposes. However, further studies are required to validate the pharmacological application of this plant extract to develop as a phytotherapeutic formulation.

Chrysobalanus icaco: A review of its phytochemistry and pharmacology.

The genus Chrysobalanus is one of the classes of medicinal plants used in the treatment and management of several diseases. This study is aimed at providing up-to-date information on the phytochemical composition and pharmacological uses of Chrysobalanus icaco. Current literature on the Chrysobalanus species was obtained by searching electronic databases such as PubMed, Google Scholar and Web of Science. Of the species in this genus, four have been reported in the literature, but only one (C. icaco) has been extensively studied. C. icaco is rich in several minerals, including potassium, magnesium, calcium and sodium. The plant also contains a host of phytochemicals, such as flavonoids, diterpenes and triterpenes, which have been shown to have pharmacological activity. It can be concluded that C. icaco is a good source of phytochemicals that contribute to its therapeutic uses. However, bioassay-guided isolation of its bioactive compounds is necessary for promoting the development of drugs from this medicinal plant.

Acute and repeated dose 28-day oral toxicity of Chrysobalanusicaco L. leaf aqueous extract.

Chrysobalanus icaco L. is a native plant of Brazil used as a food source and traditionally for the treatment of various diseases. The aim of study was performed the phytochemical analysis by UPLC-DAD-ESI-QTOF-MS/MS, and evaluated acute and repeated dose oral toxicities of the C. icaco L. leaf aqueous extract (AECi). The acute toxicity study was performed using a dose of AECi 2000 mg/kg, while the repeated dose toxicity study, the AECi was administered daily at doses of 100, 200 and 400 mg/kg, for 28 days. Behavior and mortality of animals were observed during the test period and body weight, as well water and eating consumption. Hematological, biochemical parameters and histopathological examinations were carried out. Phytochemical analysis of the AECi revealed the presence of flavonoids and tannins. Oral single dose of 2000 mg/kg of AECi resulted in no mortalities or abnormal clinical signs. Studies of repeated dose toxicity promoted a reduction in the body weight of treated animals and an increase of hepatic enzymes alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in both, males and females. Histopathological analyzes showed alterations in the livers of animals treated with AECi. Thus, this study recommends the population take care when using this species, especially during prolonged periods.

Chemical composition, nutritional properties, and antioxidant activity of Licania tomentosa (Benth.) fruit.

Licania tomentosa is a Brazilian plant species that produces edible fruits, yet there is little information available concerning their nutritional and/or bioactive composition. This study aimed to evaluate the nutritional and polyphenol composition of L. tomentosa fruits (pulp and seeds) and measure antioxidant activity in ethanolic extracts.The pulp and seeds were excellent sources of fiber (25.62%-41.70%) as well as minerals and vitamins. L. tomentosa contained no lectins or protease inhibitors (chymotrysin and trypsin) and 12 polyphenol compounds were identified in the seed extracts with a predominance of flavonoids. The seeds also presented antioxidant activities using the DPPH (SC5010.30-15.87 µg/mL), TBARS (IC50 18.46-20.84 µg/mL), and FRAP (RC50 0.203-0.309 µg/mL) assays. Due to its nutrient and antioxidant content, L. tomentosa may be used for food applications.

Anti-inflammatory activity of herb products from Licania rigida Benth.

PURPOSE: The objective of the present study was to evaluate the systemic anti-inflammatory activity of the hydroalcoholic extract of the leaves of Licania rigida Benth (EHFLR) on models of systemic inflammation in mice. METHODS: The quantitative chemical profiles of phenolic acids and flavonoids were performed by High-Performance Liquid Chromatography (HPLC). Systemic anti-inflammatory activity was determined from carrageenan and dextran-induced paw edema models and the animals were orally treated (p.o.) with EHFLR at doses of 25, 50, 100 mg/kg, indomethacin (10 mg/kg) for carrageenan-induced paw edema and promethazine (6 mg/kg) for dextran-induced paw edema. The possible mechanisms involved in the anti-inflammatory action of the extract were evaluated by the paw edema models induced by histamine and arachidonic acid, and by the model of carrageenan-induced peritonitis, where vascular permeability and leukocyte migration to the peritoneal cavity were evaluated. RESULTS: The results of the HPLC identified the presence of phenolic acids and flavonoids, with chlorogenic acid (1.16%) and Caempferol (0.81%) as the main constituents. From the results, it was concluded that the extract has an LD50 ≥5000 mg/kg when administered orally in mice as this dose did not trigger deaths in any of the observed groups. EHFLR (25 mg/kg) showed a significant antiderematogenic effect on histamine and arachidonic acid-induced paw edema at the third hour of the tests, with a percentage of inhibition of 46.64% and 18.33%, respectively. The extract (25 mg/kg, p.o.) also significantly reduced vascular permeability and leukocyte migration in the peritoneal cavity. CONCLUSIONS: It is concluded that EHFLR exerts a systemic anti-inflammatory action, which seems to depend, at least in part, on the inhibition of arachidonic acid metabolism and the action of vasoactive amines. In addition, the extract reduced the leukocyte migration in the peritoneal cavity, indicating that its action may be linked to the inhibition of pro-inflammatory cytokines.

Mass Spectral Similarity Networking and Gas-Phase Fragmentation Reactions in the Structural Analysis of Flavonoid Glycoconjugates.

Flavonoids represent an important class of natural products with a central role in plant physiology and human health. Their accurate annotation using untargeted mass spectrometry analysis still relies on differentiating similar chemical scaffolds through spectral matching to reference library spectra. In this work, we combined molecular network analysis with rules for fragment reactions and chemotaxonomy to enhance the annotation of similar flavonoid glyconjugates. Molecular network topology progressively propagated the flavonoid chemical functionalization according to collision-induced dissociation (CID) reactions, as the following chemical attributes: aglycone nature, saccharide type and number, and presence of methoxy substituents. This structure-based distribution across the spectral networks revealed the chemical composition of flavonoids across intra- and interspecies and guided the putatively assignment of 64 isomers and isobars in the Chrysobalanaceae plant species, most of which are not accurately annotated by automated untargeted MS2 matching. These proof of concept results demonstrate how molecular networking progressively grouped structurally related molecules according to their product ion scans, abundances, and ratios. The approach can be extrapolated to other classes of metabolites sharing similar structures and diagnostic fragments from tandem mass spectrometry.

The new plant Parinari kerstingii Engl.: Toxicity studies and anti-inflammatory properties.

ETHNOPHARMACOLOGICAL RELEVANCE: Parinari kerstingii Engl. extract is traditionally used for the treatment of inflammation, bronchopneumonia, feverish pains, and breast cancer. However, there have not been any scientific reports regarding the medicinal properties of this plant, and no experiments have been done to ascertain the safety of the extract. AIM OF THE STUDY: The objective of this work was to evaluate the toxicity of Parinari kerstingii Engl. extracts as an herbal remedy and to investigate its anti-inflammatory potential in vivo. MATERIALS AND METHODS: Sprague-Dawley albino male rats were used in these experiments. 100, 300 and 600 mg/kg of body weight doses of Parinari kerstingii Engl. water extract (PKWE) were used for a 14 day toxicity study. For the anti-inflammatory studies, the carrageenan-induced paw edema model was used to investigate the effect of four fractions of Parinari kerstingii Engl. ethanol extract [petroleum ether (fraction A), ethyl acetate (fraction B), n -butanol (fraction C) and water (fraction D)] on the paw size of rats and to investigate the inhibitory effects of Parinari kerstingii Engl. water (PKWE) and Parinari kerstingii Engl. ethanol extract (PKEE). RESULTS: The administration of 100 mg/kg and 300 mg/kg of body weight doses of Parinari kerstingii Engl. water extract showed no sign of toxicity. However, the 600 mg/kg of body weight dose showed a very significant increase in creatinine concentration. All the fractions of Parinari kerstingii Engl. extract demonstrated anti-inflammatory effects, as shown by a significant reduction in carrageenan-induced paw edema and by a significant decrease in the production of IL-1, TNF-α, COX-2, NF-кB, and PGE2. Moreover, fraction A and B showed enhanced in vivo anti-inflammatory effects compared to aspirin. Furthermore, PKEE was demonstrated to be more effective than PKWE. CONCLUSION: We present the first report on the plant Parinari kerstingii Engl. Based on our findings, PKWE at a dose of up to 300 mg/kg of body weight for 14 days is considered safe, and our anti-inflammatory results support its traditional use. Overall, Parinari kerstingii Engl. has been demonstrated to be a potential drug candidate. Thus, further experiments, such as isolation/structural elucidation of the phytochemicals and biological screening of this plant, need to be done.

Cocoplum (Chrysobalanus icaco L.) decreases doxorubicin-induced DNA damage and downregulates Gadd45a, Il-1ß, and Tnf-α in vivo.

DNA damage and inflammation are promising targets in disease prevention studies. Since these pathways have shown to be modulated by dietary components, investigating the molecular effects of food becomes relevant. This study aimed at investigating the protective effects of cocoplum (Chrysobalanus icaco L.) against doxorubicin (DXR)-induced damage. Rats were treated with cocoplum (100, 200 or 400mg/kg/day) for 14days, associated or not with DXR (15mg/kg b.w.). Tissue-targeted comet assay and the oxidative stress parameters oxidized/reduced glutathione and catalase were investigated in liver, kidney, and heart. The expressions of DNA damage/repair (Gadd45a, Parp1, Xrcc2) and proinflammatory genes (Il-1ß, Il-6, Nf-κb, Tnf-α) were performed by real-time quantitative PCR. Cocoplum decreased DNA damage and the expressions of Gadd45a, Il-1ß, and Tnf-α induced by DXR. These findings demonstrate that cocoplum fruits possess antigenotoxic and anti-inflammatory effects against DXR-induced damage and encourage other in vivo/clinical studies with this fruit.

Comprehensive Dual Liquid Chromatography with Quadruple Mass Spectrometry (LC1MS2 × LC1MS2 = LC2MS4) for Analysis of Parinari Curatellifolia and Other Seed Oil Triacylglycerols.

Online two-dimensional (2D) comprehensive liquid chromatography (LC × LC) has become increasingly popular. Most LC × LC separations employ one or more detectors at the outlet of the second dimension, 2D, with very short runs to avoid undersampling. We used six detectors, including dual parallel mass spectrometry (LC1MS2), for detection of the first dimension, 1D. We made an argentation (silver-ion) UHPLC column from a strong cation exchange column for 2D, coupled with UV and LC1MS2 detection. LC1MS2 in 1D combined with LC1MS2 in 2D, plus five other detectors, constituted LC2MS4 in a comprehensive LC1MS2 × LC1MS2 2D-LC separation. Electrospray ionization (ESI) high resolution accurate mass (HRAM) mass spectrometry (MS) and atmospheric pressure chemical ionization (APCI) MS were used in parallel for 1D detection, while atmospheric pressure photoionization (APPI) MS and ESI-MS were used for detection of 2D. The LC1MS2 used for 1D allowed quantification of triacylglycerol (TAG) molecular species of Parinari curatellifolia and other seed oils, while the 2D allowed isomers of TAG containing 18:3 fatty acyl chains as well as TAG regioisomers to be separated and identified. The LC1MS2 in 1D allowed identification of oxo-TAG species by HRAM MS and quantification of 806.3 ± 1.3 and 1101 ± 22 µg/g of α- and γ- tocopherols, respectively, in P. curatellifolia by APCI-MS. It is now feasible to use silver-ion UHPLC as the 2D separation in LC × LC and to use multiple mass spectrometers across both dimensions to perform conventional quantitative analysis and to take advantage of the newest LC × LC separation technology to identify isomers that are otherwise difficult to separate.

Chemotaxonomic study of Chrysobalanus icaco Linnaeus (Chrysobalanaceae) using ultra-high performance liquid chromatography coupled with diode array detection fingerprint in combination with multivariate analysis.

We investigated a strategy for the chemotaxonomy study of Chrysobalanus icaco Linnaeus (Chrysobalanaceae) based on ultra-high performance liquid chromatography coupled with diode array detection fingerprint in combination with multivariate analysis. Two models using principal component analysis and partial least squares discriminant analysis were developed, and the samples could be successfully classified into two classes: Class 1 (red morphotype) and Class 2 (white and black morphotypes). Furthermore, ultra-high performance liquid chromatography coupled with diode array and electrospray ionization tandem mass spectrometry was used to identify the main compounds responsible for class separation. The partial least squares discriminant analysis model accurately classified the C. icaco samples using an external validation subset with prediction ability of 100% and revealed the existence of two chemotypes. The most important finding obtained in this study is that the three morphotypes distinguished by the mature fruit color (white, red, and black) are not all phytoequivalent to each other.

Cocoplum (Chrysobalanus icaco L.) anthocyanins exert anti-inflammatory activity in human colon cancer and non-malignant colon cells.

Cocoplum (Chrysobalanus icaco L.) (CP) is an anthocyanin-rich fruit found in tropical areas around the globe. CP polyphenols are associated with beneficial effects on health, including reduction of inflammation and oxidative stress. Due to its functional properties, the consumption of this fruit may be beneficial in the promotion of human health and reduce the risk for chronic diseases. The objective of this study was to assess the anti-inflammatory and anti-proliferative activities of anthocyanins extracted from CP (1.0 to 20.0 µg ml-1 gallic acid equivalents [GAE]) in CCD-18Co non-malignant colonic fibroblasts and HT-29 colorectal adenocarcinoma cells. Tumor necrosis factor alpha (TNF-α, 10 ng mL-1) was used to induce inflammation in CCD-18Co cells. CP anthocyanins were identified and quantified using HPLC-ESI-MSn. The chemical analysis of CP extract identified delphinidin, cyanidin, petunidin and peonidin derivatives as major components. Cell proliferation was suppressed in HT-29 cells at 10.0 and 20.0 µg ml-1 GAE and this was accompanied by increased intracellular ROS production as well as decreased TNF-α, IL-1ß, IL-6, and NF-κB1 expressions at 20.0 µg ml-1 GAE. Within the same concentration range, there was no cytotoxic effect of CP anthocyanins in CCD-18Co cells and TNF-α-induced intracellular ROS-production was decreased by 17.3%. IL-1ß, IL-6 and TNF-α protein expressions were also reduced in TNF-α-treated CCD-18Co cells by CP anthocyanins at 20.0 µg ml-1 GAE. These results suggest that cocoplum anthocyanins possess cancer-cytotoxic and anti-inflammatory activities in both inflamed colon and colon cancer cells.

Polyphenol Composition, Antioxidant Activity and Cytotoxicity of Seeds from Two Underexploited Wild Licania Species: L. rigida and L. tomentosa.

Studies have shown the benefit of antioxidants in the prevention or treatment of human diseases and promoted a growing interest in new sources of plant antioxidants for pharmacological use. This study aimed to add value to two underexploited wild plant species (Licania rigida) and L. tomentosa) from Brazilian flora. Thus, the phenolic compounds profile of their seed ethanol extract and derived fractions were elucidated by HPLC, the antioxidant capacity was assessed by in vitro chemical tests and the cytotoxicity determined using the human carcinoma cell lines MCF-7 and Caco-2. Eleven phenolic compounds were identified in the extracts of each species. The extracts and fractions showed excellent antioxidant activity in the DPPH assay (SC50, ranging from 9.15 to 248.8 µg/mL). The aqueous fraction of L. rigida seeds was most effective in preventing lipid peroxidation under basal conditions (IC50 60.80 µg/mL) whereas, in the presence of stress inducer, the methanolic fraction of L. tomentosa performed best (IC50 8.55 µg/mL). None of the samples showed iron chelating capacity. Ethanolic seed extracts of both species did not reveal any cytotoxicity against MCF-7 and Caco-2 cells. Both plant species showed a promising phenolic profile with potent antioxidant capacity and deserve attention to be sustainably explored.

Multiple cellular effects of leaf extracts from Parinari curatellifolia.

BACKGROUND: Parinari curatellifolia is a prominent plant in folk medicine in Sub-Saharan Africa. The plant decoctions are used to treat various ailments, including the treatment of cancer, pneumonia, fever, microbial infections and anti-inflammation. The aims of the study were to investigate the effects of P. curatellifolia leaf extracts on cell inflammatory and proliferative activity. METHODS: Parinari curatellifolia fresh leaves were collected from Centenary in Mashonaland Central Province of Zimbabwe. Plant extracts were prepared using methanol, water, acetone and ethanol. Firstly, the effects of the extracts were determined on xanthine oxidase activity. Kinetic constants were determined for the extracts that showed inhibitory effects. Then the effects of Parinari curatellifolia water extract on LPS, menadione and hydrogen peroxide-activated nitric oxide production in RAW 264.7 cells was determined by quantifying the amount of nitrites formed. Finally, the effects of P. curatellifolia on the proliferation of Jurkat-T cells as well as its modulation of cisplatin-induced cell- cytotoxicity was investigated on a Jurkat human T-cell lymphoma cell line. RESULTS: There was significant XO inhibitory activity by the ethanol and methanol extracts at 15.6 µg/ml and 3.9 µg/ml respectively. The IC50 determination for allopurinol, ethanol extract and methanol extract were 0.43 µg/ml, 1.38 µg/ml and 2.19 µg/ml respectively. The kinetic results showed that the ethanol and methanol extracts were allosteric inhibitors of XO. The water extract of P. curatellifolia inhibited NO production in RAW cells when LPS was used as an activator. P. curatellifolia and cisplatin showed dose-dependent cytotoxicity on Jurkat-T cells. Isolated DNA from the cells showed that there was DNA cleavage on cells exposed to P. curatellifolia indicating that apoptosis may be a mechanism by which P. curatellifolia exerts its cytotoxicity on Jurkat-T cells. CONCLUSIONS: These results scientifically support the use of P. curatellifolia leaf extracts in the management of pain, inflammatory and neoplastic conditions. P. curatellifolia thus has multiple biological effects, thus, validating its use in traditional medical uses.

Chrysobalanus icaco L. fruits inhibit NADPH oxidase complex and protect DNA against doxorubicin-induced damage in Wistar male rats.

Chrysobalanus icaco L. is an underexplored plant found in tropical areas around the globe. Currently, there is no apparent information regarding the effects C. icaco fruits may exert in vivo or potential role in health promotion. This study aimed at providing evidence regarding the in vivo influence of this fruit on antigenotoxicity, antimutagenicity, and oxidative stress in rats. Male Wistar rats were treated with 100, 200, or 400 mg/kg body weight (bw)/d C. icaco fruit for 14 d. Doxorubicin (DXR, 15 mg/kg bw, ip) was used for DNA damaging and as an oxidant to generate reactive oxygen species (ROS). Genomic instability was assessed by the comet assay and micronucleus (MN) test, while antioxidant activity was determined by oxidative burst of neutrophils. Chrysobalanus icaco fruit polyphenols were quantified and characterized by high-performance liquid chromatography coupled to a diode array detector and tandem mass spectrometer (HPLC-DAD-MS/MS). The concentrations of 19 chemical elements were determined by inductively coupled plasma-mass spectroscopy (ICP-MS). Significant amounts of polyphenols, magnesium, and selenium were found in C. icaco fruit. This fruit displayed in vivo antioxidant activity against DXR-induced damage in rat peripheral blood neutrophils, antigenotoxicity in peripheral blood cells, and antimutagenicity in bone-marrow cells and peripheral blood cells. Correlation analyses between endpoints examined indicated that the mechanism underlying chemopreventive actions of C. icaco fruit was attributed to inhibition of NADPH oxidase complex manifested as low levels of DNA damage in animals exposed to DXR. Data indicate that phytochemicals and minerals in C. icaco fruit protect DNA against damage in vivo associated with their antioxidant properties.

In vivo and in vitro inhibition of rat liver glutathione transferases activity by extracts from Combretum zeyheri (Combretaceae) and Parinari curatellifolia (Chrysobalanaceae).

BACKGROUND: Parinari curatellifolia and Combretum zeyheri are medicinal plants used in Zimbabwe and other Southern African countries for stomach ailments, fever, body aches, wound healing, cancer and tuberculosis. Glutathione transferases (GSTs) are mammalian enzymes that play a significant role in the detoxification and metabolism of many xenobiotic and endogenous compounds and as such can interact with many exogenous compounds including herbal medicines. The effects of Parinari curatellifolia and Combretum zeyheri leaf extracts on glutathione transferases of male Sprague-Dawley rats were investigated in vivo and in vitro after oral administration of either leaf ethanol or water extracts of each plant. METHODS: For Parinari curatellifolia, 18 male Sprague-Dawley rats were administered with 0, 500 and 1000 mg/kg body weight of the leaf extracts in corn oil or saline. Animals were sacrificed after 96 h and the kidney and liver samples were removed and used to prepare the cytosolic fractions. GST activity was determined using 1-chloro-2, 4-dinitrobezene. For Combretum zeyheri, twenty four male Sprague-Dawley rats were randomly divided into two groups. These two groups were further divided into three groups of four animals each. They were given either the aqueous or ethanol extract at doses of C. zeyheri at 0, 50 mg/kg body weight and 200 mg/kg body weight. The extracts were administered orally by oral gavage for four consecutive days and the rats were sacrificed by cervical dislocation on the fifth day. RESULTS: In animals administered with C. zeyheri, GST activity was significantly increased by the 200 mg/kg aqueous extract in the kidneys and livers in vivo whilst the ethanolic extract at 200 mg/kg decreased enzyme activity significantly both organs. Both the ethanol and aqueous extracts inhibited GST activity in vitro with the ethanol extract being more potent inhibitor than ethacrynic acid, a standard GST inhibitor. The increased GST activity in vivo and versus inhibition in vitro suggests that metabolites may be responsible for the effects observed in vivo. For P. curatellifolia, a dose-dependent decrease in GST activity was observed in vivo for the animals given the aqueous extract but no changes were observed with the ethanol extract. There was a concentration-dependent inhibition of cytosolic GSTs when P. curatellifolia leaf extracts in vitro. The ethanol extract of P. curatellifolia exhibited GST-inhibitory activity in the liver with an IC50 value of 12 µg/mL and for ethacrynic acid, the IC50 was found to be 10 µg/mL. This showed that this extract was a potent inhibitor of GSTs in vitro. CONCLUSIONS: C. zeyheri had an inductive effect on GST activity when administered in aqueous solution but inhibited GST in vitro whilst P. curatellifolia inhibited GST activity in vivo. Induction of GSTs would be cytoprotective against the toxic effects electrophilic chemicals. Since GSTs are responsible for the synthesis of prostaglandins, the inhibition of GST activity of by these two plants in vivo maybe one of the reasons that makes the plants important for use in the treatment pain and fever in ethnopharmacology.

A New Ceramide and Biflavonoid from the Leaves of Parinari hypochrysea (Chrysobalanaceae).

A new ceramide and a new biflavonoid named parinaramide (1) and sparinaritin (2), respectively, have been isolated along with ten known compounds, kaempferol, quercetin, taxifolin, taxifolin-3-O-rhamnoside, lupeol, betulinic acid, ursolic acid, 2α-hydroxy-ursolic acid, 2,3-dihydroxy-1-(4-hydroxy-3,5-dimethoxyphenyl)-1-propanone, and sucrose, from the leaves of Parinari hypochrysea (Chrysobalanaceae). Structures were determined using 1D- and 2D-NMR, MS and by chemical analysis. The methanol extract of leaves, stem bark and roots of P. hypochrysea were screened for their antioxidant and lipoxygenase inhibition potential and found to be inactive.

Chrysobalanus icaco L. Leaves Normalizes Insulin Sensitivity and Blood Glucose and Inhibits Weight Gain in High-Fat Diet-Induced Obese Mice.

Chrysobalanus icaco L. is a medicinal plant present in the Brazilian coastline and known for its hypoglicemic and antioxidant properties. Here, we assessed the beneficial metabolic effects of the aqueous extract of C. icaco (AECI) leaves in diet-induced obese mice. Swiss mice were fed standard chow (SC used as controls) or high-fat diet (HFD) to induce obesity. After 10 weeks, mice on each diet were divided into two groups with one group used as control while the other group treated with AECI for 4 weeks resulting in four groups of mice: SC; SC treated with AECI (SC + AECI); HFD; and HFD treated with AECI (HFD + AECI). AECI was administered drinking water at about 200 mg/kg. AECI was able to normalize insulin (13,682 ± 1090 vs. 9828 ± 485 AU, P < .05) and fasting blood glucose (192.8 ± 14.2 vs. 132.3 ± 6.4 mg/dL, P < .05) and inhibit weight gain (39 ± 5.7%) and fat storage in liver (72.60 ± 3.83%, P < .0001), despite the high-fat intake. These findings reinforce the use of AECI in hyperglycemia and highlight the potential extract's effect in preventing weight gain and fat accumulation in liver of diet-induced obese mice.

Aqueous extract of Chrysobalanus icaco leaves, in lower doses, prevent fat gain in obese high-fat fed mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Due to the rise in obesity, the necessity for resources and treatments that could reduce the morbidity and mortality associated to this pandemia has emerged. The development of new anti-obesity drugs through herbal sources has been increasing in the past decades which are being used not only as medicine but also as food supplements. Previous studies with the aqueous extract of Chrysobalanus icaco L (AECI) have demonstrated activity on lowering blood glucose levels and body weight. AIM OF THE STUDY: Investigate C. icaco effects in overall adiposity and glycemic homeostasis. MATERIAL AND METHODS: C57BL/6J mice were randomly assigned to standard chow (SC) or high-fat diet (HFD) and treated with AECI in 0.35mg/mL or 0.7mg/mL concentrations ad libitum. Food intake, feed efficiency, metabolic efficiency, body, fat pads and gastrocnemius weight, adiposity index, serum lipids, fecal lipid excretion, locomotor activity in the open field test and insulin and glucose tolerance tests were analyzed and compared. The major components of the extract were demonstrated through HPLC and its antioxidant activity analyzed through DPPH and lipid peroxidation. RESULTS: The AECI in the 0.35mg/mL concentration did not affect food intake or body weight. However, it promoted lower adipose tissue gain, TG levels, and fecal lipid excretion, increased locomotor activity and lean mass weight, and normalized insulin sensitivity and glucose tolerance. Moreover, AECI showed the presence of myricetin 3-O-glucuronide, rutin, quercitrin and myricitrin and demonstrated high-antioxidant activity. CONCLUSIONS: AECI in lower concentrations can prevent fat storage or enhance fat utilization through the increase of locomotor activity. Also, this reinforces its ability to maintain glucose homeostasis through the normalization of insulin sensitivity and glucose tolerance despite the high-fat diet intake. These activities could be associated to the extract's polyphenol content.