Bioactive constituents from Flacourtia vogelii Hook.f. (Flacourtiaceae).

The chemical investigation of the methanolic root extract of Flacourtia vogelii led to the isolation of a new arylbenzoate derivative, vogelinal (1), together with thirteen known compounds (2-14). The structures of the isolates were elucidated by extensive spectroscopic and spectrometric analyses (1D and 2D NMR, ESI-MS) and by comparison with previously reported data. All the compounds were tested for their antioxidant, antifungal and antibacterial activities. Compound 7 exhibited the highest antioxidant potential, with RSa50of 11.80 ± 2.13 µg/mL, RSa50of 42.60 ± 6.32 µg/mL and RC50 of 51.60 ± 7.71 µg/mL for the DPPH, ABTS and FRAP assay, respectively. Compound 13 displayed weak antifungal effect with MIC value of 125 µg/mL against Candida parapsilosis. Compound 8 showed weak antibacterial effect with MIC value of 125 µg/mL, against Shigella dysenteria. The present study, conclude that this species could be a promising source of antioxidant and antibacterial constituents.

Homalium zeylanicum attenuates streptozotocin-induced hyperglycemia and cellular stress in experimental rats via attenuation of oxidative stress imparts inflammation.

ETHNOPHARMACOLOGICAL RELEVANCE: Homalium zeylanicum (Gardner) Benth (Salicaceae) leaves are being used as folklore medicine to treat diabetes by the local folk of Andhra Pradesh, India. The medicinal claim of this plant with hypoglycaemic effects was initially studied by the authors. Results demonstrated the important antioxidant activities of the hydroalcohol fraction of leaves of H. zeylanicum leaves (HAHZL) were positively correlated with phenols and flavonoids contents. AIM OF THE STUDY: Based on the previous findings, additional research is needed to examine the efficacy of using HAHZL to treat hyperglycemia. We therefore investigated in vitro and in vivo glycemic response of HAHZL, and evaluation of possible mechanism of bioactive molecules in mitigating streptozotocin-induced cellular stress in experimental rats via attenuation of oxidative stress imparts inflammation. METHODS: GC-MS/MS analysis of HAHZL was carried out to identify bioactive constituents. In vitro antidiabetic (α-glucosidase, α-amylase) and anti-inflammatory activities were investigated. HFD/low-STZ-prompted diabetic Wistar rats were administered with HAHZL (300 and 400 mg/kg; oral) for 28 days. Blood serum, oxidative stress, inflammation, DNA damage, and antidiabetic markers of pancreas and liver were determined. Histopathological studies of liver and pancreas were performed to assess the protective role of HAHZL. RESULTS: GC-MS/MS study revealed 7 bioactive compounds e.g., Phenol, 4-ethenyl-, acetate (28.68%), hydroquinone (9.10%), n-hexadecanoic acid (0.55%), phytol (0.57%), arbutin (17.65%), Vitamin E (1.04%), ß-Sitosterol (1.54%) which possess antioxidant, anti-inflammatory and anti-diabetic activities. HAHZL showed significant in vitro glycemic response as evidenced by the inhibition of α-amylase, and α-glucosidase activities. Lineweaver-Burk plot revealed that HAHZL exhibited competitive and mixed competitive inhibition towards α-amylase and α-glucosidase, respectively. HAHZL at 400 mg/kg modulated the pathophysiology associated with HFD/STZ-induced type2 diabetes mellitus and significantly (p < 0.001) improved antihyperglycemic (SG, SI, HOMA-IR, and HbA1C), antidyslipidemic (TC, HDL-C, LDL-C, and TG), antioxidative (MDA, SOD, CAT, GSH, and 8-OHdG) and anti-inflammatory (TNF-α, and CRP) markers in serum, pancreas and liver. In vitro and in vivo test results were corroborated by the improvement of pancreatic and hepatic tissue architecture in diabetic rats. CONCLUSION: HAHZL bearing bioactive components phenol, 4-ethenyl-,acetate, hydroquinone, n-hexadecanoic acid, arbutin, phytol, vitamin E and ß-sitosterol balanced glycemic level by normalising the levels of glycaemic indices, lipid profile, pancreas and liver functional markers in STZ-induced T2DM rats.

Phenolic glycosides from the stems of Homalium stenophyllum.

The phytochemical investigation of the stems of Homalium stenophyllum afforded seven new phenolic glycosides (1-5 and 8-9) and two known compounds (6 and 7). Their structures were elucidated by comprehensive analyses of NMR spectroscopic, mass spectrometric data and chemical hydrolysis. Additionally, their anti-inflammatory activities against the NO production in LPS-induced macrophages were evaluated.

Amelioration by Idesia polycarpa Maxim. var. vestita Diels. of Oleic Acid-Induced Nonalcoholic Fatty Liver in HepG2 Cells through Antioxidant and Modulation of Lipid Metabolism.

Idesia polycarpa Maxim. var. vestita Diels (I. polycarpa) is well known as an edible oil plant which contains abundant linoleic acid and polyphenols. The objective of this study was to maximize the by-product of defatted fruit of I. polycarpa. We found that the fraction D of ethyl acetate extract (EF-D) contained more polyphenols, which contribute to its strong antioxidant activity by antioxidant assays (DPPH, ABTS, and FRAP). Meanwhile, EF-D showed a significant lipid-lowering effect on oleic acid- (OA-) induced hepatic steatosis in HepG2 cells through enhancing antioxidant activity, reducing liver damage, and regulating lipid metabolism, antioxidant, and inflammation-related gene expression. The SOD and T-AOC levels significantly increased, but the levels of MDA, AST, and ALT decreased obviously when treated with EF-D. In general, EF-D improved the antioxidant enzyme activities and decreased the hepatic injury activities. Besides, treatment with EF-D for NAFLD influenced lipid metabolism and inflammation by activating PPARα which was associated with the increased expression of CPT1 and decreased expression of SCD, NF-κB, and IL-1. Moreover, EF-D improved the oxidative stress system through activation of the Nrf2 antioxidant signal pathways and upregulated its target genes of HO-1, NQO1, and GSTA2. The results highlighted the EF-D from the defatted fruit of I. polycarpa regarding lipid-lowering, proving it to be a potential drug resource of natural products for treating the nonalcoholic fatty liver disease (NAFLD).

The modulatory role of prime identified compounds in the bioactive fraction of Homalium zeylanicum in high-fat diet fed-streptozotocin-induced type 2 diabetic rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Homalium zeylanicum (Gardner) Benth. is a medicinal plant traditionally used in controlling diabetes which thus far has been assessed by the authors only to a very limited extent. PURPOSE: To fill the research gap in the literature review, we investigated the antihyperglycemic effects of hydro alcohol fraction of bark of H. zeylanicum (HAHZB) by modulating oxidative stress and inflammation in high-fat diet fed-streptozotocin (HFD/STZ)-induced type-2 diabetic rats. MATERIALS AND METHODS: To understand the antioxidant capacity of HAHZB, oxygen radical absorbance capacity (ORAC) and cell-based antioxidant protection in erythrocytes (CAP-e) were performed. GC-MS/MS analysis was performed to assess the bioactive components in HAHZB. HFD/STZ-induced diabetic rats were treated orally with HAHZB (300 and 400 mg/kg) for 28 days. After the end of the experiment, marker profiling and histopathological observation of blood and pancreas were examined. The study also highlights interaction between diabetes, oxidative stress and inflammation by examining the increased pro-inflammatory cytokines e.g. TNF-α and C-reactive protein (CRP) promotes DNA damage e.g. oxidation of 8-hydroxy-2-deoxyguanosine (8-OHdG) in chronic hyperglycaemia. RESULTS: In ex vivo cellular antioxidant capacity of -CAP-e and ORAC assays, HAHZB showed remarkable free radical scavenging ability in a dose dependent manner. GC-MS/MS analysis identified 28 no. of compounds and out of which, oleic acid (1.03%), ethyl tridecanoate (11.77%), phytol (1.29), 9,12-octadecadienoic acid, methyl ester, (E,E)-(5.97%), stigmasterol (1.30%) and ß-sitosterol (2.86%) have antioxidant, anti-inflammatory and anti-diabetic activities. HAHZB 400 mg/kg significantly (p < 0.001) improved the lipid profile (TC: 74.66 ± 0.59, HDL-C: 22.08 ± 0.46, LDL-C: 38.06 ± 0.69, and TG: 171.92 ± 1.01 mg/dL) as well as restoring antidiabetic markers (SG: 209.62 ± 1.05 mg/dL, SI: 15.07 ± 0.11 µIU/mL, HOMA-IR: 7.79 ± 0.04 %, and HbA1C: 8.93 ± 0.03 %) and renal functional markers (Tg: 291.26 ± 0.57 pg/mL, BUN: 23.79 ± 0.14 mg/dL, and Cr: 1.34 ± 0.04 mg/dL) in diabetic rats. Oxidative stress markers of pancreas (MDA: 3.65 ± 0.17 nM TBARS /mg protein, SOD: 3.14 ± 0.28 U/mg protein, CAT: 7.88 ± 0.23 U/mg protein, GSH: 12.63 ± 0.28 µM/g of tissue) were restored to normal as evidenced by histological architecture of pancreatic islet cells. The increased level of pro-inflammatory cytokines and oxidative DNA damage were significantly restored (TNF-α: 54.48 ± 3.19 pg/mL, CRP: 440.22 ± 7.86 ng/mL, and 8-OHdG: 63.65 ± 1.84 ng/mL) by HAHZB in diabetic rats. CONCLUSION: The present findings confirm that the presence of bioactive compounds in HAHZB exert therapeutic protective effect by decreasing oxidative, inflammation and pancreatic ß-cell damage in oxidative stress induced diabetic rats.

Chemical Constituents and Pharmacological Activities of Family Flacourtiaceae: A Class of Important Phytomedicine.

Flacourtiaceae plants are widely used as folk medicines in traditional medicine systems for its chemical diversity and pharmacological activities. In many different areas, Flacourtiaceae plants are used as traditional medicines for the treatment of ulcers, malaria, rheumatism. The Flacourtiaceae plants contain a very plentiful chemical composition, and phytochemical studies show that the Flacourtiaceae plants contained terpenoids, aromatic glycosides, flavnoids, phenylpropanoids, alkaloids, fatty hydrocarbon, and other compounds. In pharmacological studies, various extract and isolated individual compounds exhibited antitumor, anti-oxidation, and anti-inflammatory activities. In this review, the literature data on the chemical constituents and pharmacological investigations of the Flacourtiaceae plants are summarized, to provide information about a more comprehensive chemical composition and detailed pharmacological activities of Flacourtiaceae plants, with a view of further development of clinical medication. However, research on quantitative analysis, toxicity, and drug safety in vitro and in vivo is still insufficient, and further research is required.

Computational and experimental validation of free radical scavenging properties of high-performance thin-layer chromatography quantified phenyl myristate in Homalium nepalense.

Phenyl myristate was isolated from Homalium nepalense, which is known for its therapeutic virtues in traditional medicine. However, the study of radical scavenging-capacity of phenyl myristate is limited by its relatively low abundance in medicinal plants. We have studied the isolation, structure-elucidation, and bioactivities of high-performance thin-layer chromatography validated phenyl myristate from hydroalcohol-extract of bark of H. nepalense. The chemical structure of phenyl myristate was elucidated by spectroscopic methods. The chromatography was performed on high-performance thin-layer chromatography aluminum plates coated with silica-gel 60 F254 . Determination and quantitation of phenyl myristate were performed by densitometric-scanning at 254 nm (chloroform-methanol, 9:1, v/v; Rf 0.49). The method was validated according to International Council for Harmonisation guidelines in terms of linearity, specificity, sensitivity, accuracy, precision, robustness, and stability. Linearity-range of phenyl myristate was 100-500 ng/5 µL with correlation-coefficient r2  = 0.9997. Limits of detection and quantitation were 3.35 and 10.17 ng, respectively. Phenyl myristate showed significant free-radical-scavenging activities in 2,2-diphenyl-1-picrylhydrazyl, oxygen-radical-absorbance-capacity, and ex vivo cell-based-antioxidant-protection-in-erythrocytes assays. Molecular-docking approach of phenyl myristate showed effective binding at active sites of human serum albumin (HSA) with the lowest binding energy (-8.4 kcal/mol) that was comparable with ascorbic acid (-5.0 kcal/mol). These studies provide mechanistic insight into the potential free radical scavenging activities of phenyl myristate.

Isolation and purification of four phenolic glycoside isomers from the leaves of Idesia polycarpa Maxim. by high-speed counter-current chromatography and preparative high-performance liquid chromatography.

We established an efficient method using high-speed counter-current chromatography (HSCCC) combined with preparative high-performance liquid chromatography (prep-HPLC) for isolating and purifying phenolic glycoside isomers. The method involves a rapid and sensitive ultra-performance liquid chromatography-under voltage(UPLC-UV) technique using a sub-2 µm core-shell particle column for qualitative and quantitative analysis of four phenolic glycoside isomers from Idesia polycarpa Maxim. leaves. The partially purified samples from ethyl acetate extraction of ethanol extracts of I. polycarpa Maxim. leaves were obtained by HSCCC with a two-phase solvent system composed of n-hexane-ethyl acetate-methanol-water solution (3:5:3:5, v/v/v/v) to obtain fractions I and II, which contain two phenolic glycoside isomers. The two fractions were further isolated by prep-HPLC to yield compounds 1, 2, 3, and 4 with purities of 98.29%, 98.71%, 98.49% and 98.52%, and total recoveries of 93.5%, 72.2%, 75.5% and 88.3%, respectively. Compound 1 was first isolated from I. polycarpa Maxim., while compound 2 was reported to be a new phenolic glycoside, which is 1-[(6'-O-(Z)-p-coumaroyl)-ß-D-glucopyranosyl]-oxy-2-phenol. The chemical structures of the four phenolic glycoside isomers were analyzed and confirmed by UPLC, UV, electrospray ionization mass spectrometry (ESI-MS), fourier transform infra-red (FT-IR), 1H-nuclear magnetic resonance (1H NMR), 13C-nuclear magnetic resonance (13C NMR) and 2D nuclear magnetic resonance (2D NMR) spectra. This study opens prospects for broad industrial applications of HSCCC/prep-HPLC for the isolation and purification of isomers.

Ethnobotanical uses, biological activities and chemical properties of Kei-apple [Dovyalis caffra (Hook.f. & Harv.) Sim]: An indigenous fruit tree of southern Africa.

ETHNOPHARMACOLOGICAL RELEVANCE: Dovyalis caffra (Hook.f. & Harv.) Sim (commonly called Kei-apple) is an indigenous fruit tree that has medicinal values for various ethnic groups in southern Africa. AIM OF THE REVIEW: This review aims to provide a critical appraisal of the existing knowledge on the ethnobotanical value, biological activities and phytochemicals of Dovyalis caffra. In addition, the potential of producing a functional health product from Kei-apple due to its therapeutic effects and rich pool of phytochemicals was explored. METHODS: A detailed literature search was conducted using various online search engines, such as Scopus, Google Scholar, Mendeley and Web of Science. Additional information was sourced from ethnobotanical literature focusing on southern African flora. RESULTS: Dovyalis caffra has diverse uses in local and popular medicine, specifically for relieving pain and rheumatism in humans. Ethno-veterinary potential of Kei-apple has also been documented in East Africa. Non-medicinal uses of the tree include its role in biological hedging and as a traditional herb for African magical purpose. Regarding its biological activities, polar extracts from the seeds exhibited noteworthy antibacterial (minimum inhibitory concentration of 1 µg/ml against Staphylococcus aureus) activity. Quantitative analysis (e.g. GC-MS, HPLC) indicated the presence of a rich (>80) pool of chemicals, including sterols, phenolic acids and fatty acids from different parts of the plant while 11 compounds have been isolated from its leaves and twigs. CONCLUSIONS: Dovyalis caffra has been tested for various biological activities and the extracts (seeds in particular) demonstrated promising antibacterial potential. A lack of alignment between the ethno-medicinal uses and existing biological screenings was observed, indicting the need for anti-inflammatory and anti-rheumatism potential of Dovyalis caffra to be explored. In vivo validation of antibacterial and anti-parasitic activities against clinical bacterial strains and parasites, respectively is required. Other areas that need investigation are safety evaluations and development of integrated cultivation approach in order to fully explore the plant's potential.

A new phenolic glycoside from the Idesia polycarpa Maxim. leaves.

Phytochemical investigation on the ethyl acetate extract of Idesia polycarpa Maxim. Leaves led to the isolation of four phenolic glycoside isomers (1-4). Compound 2 appeared to be new reported phenolic glycoside, while compound 1 was the first time isolated from the titled species. Their structures were established by IR, UV, HRESI-MS and 1D and 2D NMR spectroscopies analysis and comparison of spectral data with previously reported data. The compounds 3 and 4 showed stronger activity of scavenging the DPPH free radical than the other two compounds, while the compounds 1 and 2 showed a significant activity of scavenging the ABTS free radical. Compounds 2 and 4 exhibited stronger cytotoxicity against HepG2 cell lines compared to compounds 1 and 3. Moreover, compound 3 presented the highest cytotoxicity against MCF cell lines with IC50 value of 37.17 ± 0.26 µg/mL than compounds 1, 2 and 4.

The ameliorative effect of Homalium nepalense on carbon tetrachloride-induced hepatocellular injury in rats.

The purpose of this study was to evaluate ameliorative effects of Homalium nepalense Benth. (Flacourtiaceae) on CCl4-induced hepatocellular injury in rats. Oxygen-radical absorbance-capacity (ORAC) and cell-based-antioxidant-protection-in-erythrocytes (CAP-e) were performed and found that the ethyl acetate fractions of bark (HNEB) and leaf (HNEL) showed a remarkable degree of antioxidant activities in a dose dependent manner. Antioxidant potential HNEB was higher than HNEL and was comparable with trolox. HNEB and HNEL at 300 and 400 mg/kg showed significant hepatoprotective activities against CCl4-induced hepatotoxicity as evidenced by restoration of SGOT, SGPT, ALP, TB and TP level. The level of TBARS, SOD, CAT and GSH were significantly improved and restored towards normal value. Both fractions at 400 mg/kg showed remarkable improvements in marker levels as comparable to silymarin. Histopathological observations of liver tissues revealed the reduction of necrosis with appearance of sinusoidal space, central vein, and bile duct both in case of HNEB and HNEL. GC-MS and LC-MS confirmed occurrence of a total 53 no. of phytocompounds in HNEB and HNEL. Based on their retention times-(RT) and mass-to-charge-ratios-(m/z), some of the major bioactive compounds were catechol (5.89%), 5-hydroxymethylfurfural (5.87%), salicylic acid (4.89%), eugenol (1.60%), doconexent (0.31%), ß-sitosterol (1.59%), 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyran-4-one (1.15%), coniferyl alcohol (2.99%), hexadecanoic acid methyl ester (1.05%), and betulin (1.20%). H. nepalense possesses significant hepatoprotection effect because of its antioxidant constituents.

A phenolic glycoside from Flacourtia indica induces heme mediated oxidative stress in Plasmodium falciparum and attenuates malaria pathogenesis in mice.

BACKGROUND: Flacourtia indica is especially popular among the various communities of many African countries where it is being used traditionally for the treatment of malaria. In our previous report, we have identified some phenolic glycosides from the aerial parts of F. indica as promising antiplasmodial agents under in vitro conditions. PURPOSE: Antimalarial bioprospection of F. indica derived phenolic glycoside in Swiss mice (in vivo) with special emphasis on its mode of action. METHODS: Chloroquine sensitive strain of Plasmodium falciparum was routinely cultured and used for the in vitro studies. The in vivo antimalarial potential of phenolic glycoside was evaluated against P. berghei in Swiss mice through an array of parameters viz., hematological, biochemical, chemo-suppression and mean survival time. RESULTS: 2-(6-benzoyl-ß-d-glucopyranosyloxy)-7-(1α, 2α, 6α-trihydroxy-3-oxocyclohex-4-enoyl)-5-hydroxybenzyl alcohol (CPG), a phenolic glycoside isolated from the aerial parts of F. indica was found to exhibit promising antiplasmodial activity by arresting the P. falciparum growth at the trophozoite stage. Spectroscopic investigations reveal that CPG possesses a strong binding affinity with free heme moieties. In addition, these interactions lead to the inhibition of heme polymerization in malaria parasite, augmenting oxidative stress, and delaying the rapid growth of parasite. Under in-vivo condition, CPG exhibited significant antimalarial activity against P. berghei at 50 and 75mg/kg body weight through chemo-suppression of parasitemia and ameliorating the parasite induced inflammatory and oxidative (hepatic) imbalance in the experimental mice. CONCLUSION: CPG was found to be a potential antimalarial constituent of F. indica with an explored mechanism of action, which also offers the editing choices for developing CPG based antimalarial chemotypes.

Bioprofiling of Salicaceae bud extracts through high-performance thin-layer chromatography hyphenated to biochemical, microbiological and chemical detections.

The buds of poplars (Populus L.) and willows (Salix L.), both from the same family (Salicaceae Mirbel), are increasingly used in gemmotherapy and importantly contribute to the production of the physiologically active propolis by European bee Apis mellifera L. In order to study their phenolic profiles, polar extracts of buds from P. nigra L. were compared to those of P. alba L. and S. alba L. through high-performance thin-layer chromatography (HPTLC). Five chemotypical patterns were distinguished after derivatisation with the Natural Product reagent and confirmed by principal component analysis. The HPTLC analysis was directly hyphenated to various microbiological and biochemical assays as well as spectrometric techniques, directly linking to active molecules in the chromatograms. At a glance, polyvalent compounds were evident when all derivatisation and activity assays, to which HPTLC was hyphenated at ease, were combined together. In Populus buds, at least three antimicrobial compound zones were detected using Aliivibrio fischeri and Bacillus subtilis bioassays, and one phyto-œstrogen with the planar yeast œstrogen screen. In all samples, several inhibitors of acetyl- and butyrylcholinesterase and rabbit liver esterase were detected. Hyphenation to high resolution mass spectrometry supported the assignment of bioactive compounds, as shown for chrysin as selective cholinesterase inhibitor as well as caffeic acid and galangin as antimicrobials in P. nigra and P. alba. This fast and cost-efficient method can be appropriately extended and applied to the botanical origin determination and quality control of bud extracts and propolis samples.

Effects of Aphloia theiformis on key enzymes related to diabetes mellitus.

CONTEXT: Aphloia theiformis (Vahl.) Benn. (Flacourtiaceae) (AT) is traditionally used for the management of diabetes mellitus (DM), but there is no scientific data regarding activity against enzymes linked to this condition. OBJECTIVE: To evaluate the kinetics of AT on key enzymes inhibition related to DM, and establish the antioxidant profile of AT. MATERIALS AND METHODS: Dried powdered AT leaves were used to prepare crude methanol extract (70% v/v) (CME). Kinetics of CME (5000 to 156.25 µg/mL) on α-amylase, α-glucosidase, and lipase inhibition were studied. CME was partitioned using solvents of increasing polarity and kinetics of enzyme inhibition of each fraction (1000-31.25 µg/mL) was evaluated. Potent fractions were combined to assess any synergistic effect. Total phenol, flavonoid, tannin, anthocyanin contents, and antioxidant capacity of AT was evaluated using standard spectrophotometric methods. RESULTS: CME, ethyl acetate, and n-butanol fractions showed potent inhibitory activities against the enzymes with IC50 ranging from 22.94-939.97 µg/mL. Significant (p < 0.05) reduction in IC50 (15.72 and 157.03 µg/mL against α-amylase and lipase, respectively) was observed when ethyl acetate and n-butanol fractions were combined; showing synergism. The extracts showed noncompetitive inhibition against α-amylase and α-glucosidase. Ethyl acetate, n-butanol fractions, and CME showed highest antioxidant capacities (0.44-1.41 µg GAE/mg sample), and phenol content (211.74-675.53 µg GAE/mg sample). CONCLUSION: This study supports the use of AT in the management of DM and provides the rationale for bioactivity guided isolation and characterization of compounds from the ethyl acetate and n-butanol fractions.

A New Benzophenanthridine Alkaloid from Caloncoba glauca.

Three alkaloids including a new one, N-formyldihydrochelerythrine (1), together with four other known compounds were isolated from the stem bark of Caloncoba glauca. The structure of the new compound was elucidated from spectroscopic and mass spectrometric evidence. This is the first report of alkaloids from the genus Caloncoba. Sesamin (4) [MIC = 256 µg/mL (Candida albicans) and dihydrochelerythrine (2) [MIC = 32 (C. albicans and C. parapsilosis), and 128 µg/mL (C. krusei)] had moderate to weak antifungal activity.

A mechanism-based pharmacological evaluation of efficacy of Flacourtia indica in management of dyslipidemia and oxidative stress in hyperlipidemic rats.

BACKGROUND: Flacourtia indica (Burm. f.) Merr. is a medicinal plant indigenous to India and is broadly used worldwide for the treatment of a variety of health ailments. The present study was experimented on hyperlipidemic Charles Foster rats with the aim to explore the possible mechanism responsible for the antidyslipidemic activity of the hydromethanolic extract from F. indica leaves (FIL). METHODS: Hyperlipidemia was induced by a single intraperitoneal dose of Triton WR-1339 in Charles Foster rats. The plasma lipid levels were estimated in control and treated groups. The antioxidant potential of F. indica was assessed in both enzymatic and non-enzymatic systems. An acute toxicity study of high-performance liquid chromatography (HPLC)-fingerprinted extract was carried out in Swiss albino mice. RESULTS: The F. indica extract at a dose of 150 mg/kg significantly lowers the plasma level of total cholesterol (17%), triglycerides (13%), and phospholipids (16%) by increasing post-heparin lipolytic activity (19%) and lecithin-cholesterol-acyltransferase activity (20%) in Triton-induced hyperlipidemic rats. In addition, the F. indica extract showed significant in vitro antioxidant and anti-adipogenic activity. HPLC analysis indicates the presence of flavanones and flavones in the extract, and the extract was found to be non-toxic up to a dose of 2000 mg/kg body weight in the acute oral toxicity study. CONCLUSIONS: These finding suggest that F. indica holds significant potential in preventing clinical deterioration induced by dyslipidemia along with oxidative stress.

Biochemical Characterization of Dovyalis hebecarpa Fruits: A Source of Anthocyanins with High Antioxidant Capacity.

UNLABELLED: Dovyalis hebecarpa, which is also known as the Ceylon gooseberry, is an attractive exotic purple berry that is produced in the southwest of Brazil with high yields. Current literature lacks information about the nutritional composition and antioxidant capacity of this fruit. As such, this work aimed to evaluate and compare the proximate composition, phytochemical content, and antioxidant capacity of D. hebecarpa over two seasons through the application of a range of different methods, including FRAP, ABTS, and ORAC assays. The proximate composition and biometric parameters were monitored for quality purposes. The results significantly changed between seasons in accordance with variations in rain incidence and average temperatures. The Ceylon gooseberry contained a similar or higher content of anthocyanins (ACY) than other berries commonly consumed in human diet. These ACY were identified at higher levels in the fruit's skin (284 to 351 mg of cyanidin-3-glucoside equivalents/100 g of fresh weight [FW]) than in its pulp (49 to 69 mg/100 g of FW). The use of an ORAC assay identified higher antioxidant activity (145 µmol of Trolox equivalents [TE]/g in the skins and 179 µmol of TE/g in the pulp on a FW basis) than all other methods used to determine antioxidant activity. Thus, D. hebecarpa is a rich source of ACY that demonstrates high antioxidant activity against the peroxyl radicals formed in ORAC assay conditions. PRACTICAL APPLICATION: Ceylon gooseberry fruit is a source of phytochemicals that could be used in the human diet providing defense against free radicals damage. Moreover, the skins of the fruit, which are not typically consumed, contained higher levels of polyphenols than the pulp. This indicates that the skins of the Ceylon gooseberry may represent a promising source of natural pigments and antioxidants for industrial applications.

Antimicrobial and antioxidant flavonoids from the leaves of Oncoba spinosa Forssk. (Salicaceae).

BACKGROUND: Naturally occurring flavonoids have been reported to possess various pharmacological properties. The aim of this study was to evaluate the antimicrobial and antioxidant activities of the MeOH extract and flavonoids from the leaves of Oncoba spinosa, a plant used for the treatment of syphilis, wounds and sexual impotence. METHODS: The plant extract was prepared by maceration in methanol and sequentially fractionated by column chromatography. The structures of isolated compounds were elucidated on the basis of spectral studies and comparison with published data. The MeOH extract and its isolated compounds were evaluated for their antibacterial and antifungal activities by broth microdilution method. The 1,1-diphenyl-2-picrylhydrazyl (DPPH) and trolox equivalent antioxidant capacity (TEAC) assays were used to detect the antioxidant activity. The samples were tested spectrophotometrically for their hemolytic properties against human red blood cells. RESULTS: The fractionation of the MeOH extract afforded five known flavonoids including kaempferol (1), quercetin (2), apigenin-7-O-ß-D-glucuronopyranoside (3), quercetin 3-O-ß-D-galactopyranoside (4) and quercetin 3-O-α-L-rhamnopyranosyl (1 → 6) ß-D-glucopyranoside (5). The MeOH extract displayed weak to moderate antimicrobial activities (MIC = 256-2048 µg/ml). Quercetin 3-O-α-L-rhamnopyranosyl (1 → 6) ß-D-glucopyranoside (5) and quercetin (2) were respectively the most active compounds against bacteria (MIC = 8-64 µg/ml) and fungi (MIC = 64 - 128 µg/ml). These tested samples also showed high radical-scavenging activities (EC50 = 5.08 - 70.56 µg/ml) and gallic acid equivalent antioxidant capacities (TEAC = 53.76 - 89.86 µg/ml) when compared with vitamin C (EC50 = 4.72 µg/ml). The MeOH extract and compounds 2-5 were non-toxic to human red blood cells indicating their high selectivity to be used as antimicrobial and antioxidant drugs. CONCLUSION: The MeOH extract of O. spinosa as well as compounds 2 - 5 could be a potential source of natural antimicrobial and antioxidant products.

Free radical-scavenging activities of Homalium species--An endangered medicinal plant of Eastern Ghats of India.

Three species of the genus Homalium - e.g. Homalium nepalense, Homalium tomentosum and Homalium zeylanicum (Flacourtiaceae) - are recorded in India which are confined to the Eastern Ghat hill ranges. While H. zeylanicum is the IUCN red-listed medium-sized tree, the other two are endangered species of medicinal significance. The antioxidant potential of leaf and bark of the plants was evaluated through successive extraction methods by using hexane, chloroform, ethyl acetate and methanol. The extracts were subjected to in vitro assays as DPPH, hydroxyl, nitric oxide and superoxide along with its biochemical estimation. Amongst all, the ethyl acetate extracts of bark is found to be most potent compared with that of the leaves. H. nepalense has the highest amount of total phenolic and flavonoid contents followed by H. tomentosum and H. zeylanicum, respectively, and significant antioxidant behaviour.

First chemical evaluation and toxicity of Casinga-cheirosa to Balb-c male mice.

Laetia suaveolens, known as "casinga-cheirosa", crude extract EB719 has previously shown cytotoxic activity against prostate cancer and squamous cell carcinoma. For the first time, seven molecules were isolated from its apolar-α-tocopherol (1) and sitosterol (2)-and polar-3-O-caffeoylquinic acid (3), 4-O-caffeoylquinic acid (4), 5-O-feruloylquinic acid (5), hyperoside (6), and isoquercitrin (7)-fractions. Acute toxicity was determined in a two-stage experiment: (1) a reduced number of Balb-c male mice received 5000 mg/kg of EB719 to allow evaluation of general activity and other 27 parameters, plus death, up to the establishment of non-lethal dose (NLD), as well as lethal dose 50% (LD50); (2) NLD was administered and diazepam introduced as reference drug. EB719 showed LD50=178.0 mg/kg, and NLD 156.3 mg/kg. In stage one EB719 did not influence general activity, but provoked impairment in grasp reflexes, tail squeeze and breathing; piloerection and cyanosis were increased. In stage two, alterations occurred in auricular reflex, piloerection and breathing after diazepam administration, but not in response to EB719. Intestinal hemorrhage caused by local bleeding was observed after necropsy, and may be the main cause of animals' death other than a systemic effect of the extract. Although the isolated compounds are biologically and pharmacologically active in both men and animal systems, it is premature to relate their occurrence in EB719 to the observed intestine hemorrhage in mice.