LC–MS characterization, anti-kinetoplastide and cytotoxic activities of natural products from Eugenia jambolana Lam. and Eugenia uniflora

Objective To evaluate the trypanocidal, leishmanicidal and cytotoxic activity of Eugenia jambolana (E. jambolana) and Eugenia uniflora (E. uniflora) extracts and fractions. Methods The products were characterized by LC–MS. Antiparasitic assays were performed and cytotoxicity was evaluated in fibroblastos. In vitro assays were performed using spectrophotometric evaluation. All assays were performed in thrice. Results The results showed that the extracts and the tannic fraction from E. jambolana inhibited 100% of the epimastigote lines. The ethanolic extract was the most efficient in all concentrations tested against the three parasite strains. In the cytotoxicity assay the flavonoid fraction showed low toxicity. All E. uniflora samples showed cytotoxicity at the highest concentration tested, but the extract showed no toxic effect on the fibroblasts at the lowest concentration. The flavonoid and tannic fractions were more efficient against Leishmania braziliensis promastigotes compared to the extract. However, the extracts and the tannic fraction were more effective against Leishmania infantum strains. The effect on epimastigote cells was observed at all concentrations tested, with all E. uniflora samples. However, the samples were more effective at the highest concentration, where there was inhibition in 100% of the Trypanosoma cruzi strains. Conclusions The species E. jambolana and E. uniflora presented antiparasitic activity against all tested parasite strains, indicating that these species can serve as an alternative therapy as they were efficient in the tests performed. The E. uniflora extract and the E. jambolana flavonoid fraction presented a low cytotoxicity, opening the floor for new biological studies.

LC-MS characterization, anti-kinetoplastide and cytotoxic activities of natural products from Eugenia jambolana Lam.and Eugenia uniflora

Objective:To evaluate the trypanocidal,leishmanicidal and cytotoxic activity of Eugenia jambolana (E.jambolana) and Eugenia uniflora (E.uniflora) extracts and fractions.Methods:The products were characterized by LC-MS.Antiparasitic assays were performed and cytotoxicity was evaluated in fibroblastos.In vitro assays were performed using spectrophotometric evaluation.All assays were performed in thrice.Results:The results showed that the extracts and the tannic fraction from E.jambolana inhibited 100％ of the epimastigote lines.The ethanolic extract was the most efficient in all concentrations tested against the three parasite strains.In the cytotoxicity assay the flavonoid fraction showed low toxicity.All E.uniflora samples showed cytotoxicity at the highest concentration tested,but the extract showed no toxic effect on the fibroblasts at the lowest concentration.The flavonoid and tannic fractions were more efficient against Leishmania braziliensis promastigotes compared to the extract.However,the extracts and the tannic fraction were more effective against Leishmania infantum strains.The effect on epimastigote cells was observed at all concentrations tested,with all E.uniflora samples.However,the samples were more effective at the highest concentration,where there was inhibition in 100％ of the Trypanosoma cruzi strains.Contusions:The species E.jambolana and E.uniflora presented antiparasitic activity against all tested parasite strains,indicating that these species can serve as an altemative therapy as they were efficient in the tests performed.The E.uniflora extract and the E.jambolana flavonoid fraction presented a low cytotoxicity,opening the floor for new biological studies.

Efecto citoprotector de extractos de Eugenia jambolana y Psidium myrsinites DC. A. contra peroxidación lipídica inducida por hierro II / Citoprotective effect of Eugenia jambolana and Psidium myrsinites DC. A. against the lipid peroxidation induced by iron II

La evaluación de la actividad antioxidante ha sido una cuestión relevante teniendo en cuenta su importancia para la salud humana. Estudios recientes muestran que el uso de plantas en forma de jugos o tés como fuentes de antioxidantes naturales, que se pueden utilizar como complemento para el tratamiento de diversas enfermedades. En este contexto, evaluado el potencial antioxidante in vitro, de extractos de Eugenia jambolana Lam y Psidium myrsinites DC. A. y cuantificar fenoles y flavonoides presentes en los extractos. La peroxidación lipídica ha sido evaluada por la técnica de TBARS (sustancias reactivas al ácido tiobarbitúrico). De acuerdo con los resultados, mostraron una mejor actividad antioxidante del extracto de psidium myrsinites DC. A. Para poner a prueba TBARS con fosfolípido de huevo extrae redujo los niveles basales en el proceso de peroxidación de lípidos, la CI50 del extracto etanolico de Euguenia jambolana (EEFEJ) mostró los mejores resultados, con un más bajo valor de la CI50 en comparación con el extracto hidroetanolico de Psidium mirsinites, demostrado ser más efectivo. Por lo tanto, a través de estas pruebas se puede ver que los extractos de las hojas de la especie, Eugenia jambolana Lam y Psidium myrsinites DC. A., la actividad antioxidante de exposiciones, sustancias fenólicas directamente relacionados producidos a partir de su metabolismo secundario.

The evaluation of the antioxidant activity has been a relevant and important issue to human health. Recent studies show that the use of plants juices or teas as sources of natural antioxidants, which can be used as an adjuvant in the treatment of several diseases. In this context, was evaluated the in vitro antioxidant potential of the extracts of Psidium myrsinites DC. and Eugenia jambolana Lam. The total of phenols and flavonoids were quantified in the extracts. Lipid peroxidation was evaluated by the technique of TBARS (thiobarbituric acid reactive substances). According to the results, was showed a better antioxidant activity in the extract of Psidium myrsinites DC. A. In the TBARS assay with egg phospholipid the extracts reduced the basal levels in the process of lipid peroxidation and the IC50 of ethanol extract of Eugenia jambolana (EEFEJ) showed the best results with a lower value of IC50 compared with hydroethanol extract of Psidium mirsinites, demonstrating be more effective. Therefore, through these tests can be seen that extracts from the leaves of the species, Eugenia and Psidium jambolana Lam myrsinites DC. A., exhibit antioxidant activity, directly related phenolic substances produced from the secondary metabolism.

In vitro antioxidant activity and total phenolic content of endophytic fungi isolated from Eugenia jambolana Lam

OBJECTIVE@#To elucidate the antioxidant activity and total phenolic content (TPC) of ethyl acetate extracts of endophytic fungi isolated from Eugenia jambolana by three different antioxidant assays.@*METHODS@#Twenty one different endophytic fungal extracts were screened for presence of various phytochemicals, TPC and in vitro antioxidant activity. TPC was tested by Folin-Ciocalteau reagent based assay. DPPH free radical scavenging, hydrogen peroxide scavenging and reducing power assays were used to evaluate the antioxidant activity.@*RESULTS@#Alkaloids, phenols, flavonoids, saponins, and terpenes were the main phytochemicals presents in all 21 endophytes. A significant positive correlation was found between antioxidant activity and TPC in fungal extracts. There is 36% endophytic extracts having high phenolic content exhibited potent antioxidant activity. Chaetomium sp., Aspergillus sp., Aspergillus peyronelii and Aspergillus niger strain showed the highest antioxidant activity ranging from 50% to 80% having 58 mg/g to 60 mg/g GAE total phenolics. Ascorbic acid used as a standard showed 90% reducing potential.@*CONCLUSIONS@#The results reveal that metabolites produced by endophytic fungi isolated from Eugenia jambolana can be a potential source of novel natural antioxidant compounds.

In vitro antioxidant activity and total phenolic content of endophytic fungi isolated from Eugenia jambolana Lam

Objective: To elucidate the antioxidant activity and total phenolic content (TPC) of ethyl acetate extracts of endophytic fungi isolated from Eugenia jambolana by three different antioxidant assays. Methods: Twenty one different endophytic fungal extracts were screened for presence of various phytochemicals, TPC and in vitro antioxidant activity. TPC was tested by Folin-Ciocalteau reagent based assay. DPPH free radical scavenging, hydrogen peroxide scavenging and reducing power assays were used to evaluate the antioxidant activity. Results: Alkaloids, phenols, flavonoids, saponins, and terpenes were the main phytochemicals presents in all 21 endophytes. A significant positive correlation was found between antioxidant activity and TPC in fungal extracts. There is 36% endophytic extracts having high phenolic content exhibited potent antioxidant activity. Chaetomium sp., Aspergillus sp., Aspergillus peyronelii and Aspergillus niger strain showed the highest antioxidant activity ranging from 50% to 80% having 58 mg/g to 60 mg/g GAE total phenolics. Ascorbic acid used as a standard showed 90% reducing potential. Conclusions: The results reveal that metabolites produced by endophytic fungi isolated from Eugenia jambolana can be a potential source of novel natural antioxidant compounds.

Evaluation of antinociceptive and anti-inflammatory activities of extract and fractions of Eugenia jambolana root bark and isolation of phytoconstituents

Eugenia jambolana Lam., Myrtaceae, is a widely distributed and traditionally well known plant in India. The root bark of the plant was extracted with ethanol and then successively fractionated into petroleum ether fraction, chloroform fraction, n-butanol fraction and methanol fraction. The extract and fractions of the plant material were evaluated for the antinociceptive activity by acetic acid-induced writhing test and formalin-induced nociception test, and anti-inflammatory activity was screened by carrageenan-induced rat paw edema, cotton pellet induced granuloma formation and adjuvant induced arthritis in rat models. The test materials showed the antinociceptive and anti-inflammatory effect in dose dependent manner and the petroleum ether fraction was found to be most potent among the test materials. At 400 mg/kg b.w., p.o. dose petroleum ether fraction significantly inhibited 54.28% writhing response and 73.77% formalin induced nociception in mice. The fraction with same dose showed significant 79.31% inhibition of carrageenan-induced rat paw edema, 57.78% anti-proliferative effect and 77.93% inhibition of adjuvant induced arthritis. The bioactive petroleum ether fraction was then subjected to column chromatography which led to isolate three compounds, namely, β-sitosterol, stigmasterol and lupeol. These compounds were characterized and identified by IR, ¹H NMR, 13C NMR and mass spectroscopy.

Spray-dried extracts from Syzygium cumini seeds: physicochemical and biological evaluation

Aqueous extract from seeds of Syzygium cumini (L.) Skeels, Myrtaceae, obtained by dynamic maceration was spray-dried and characterized by its physico-chemical and antihyperglycaemic action. The extract showed to possess high amount of polyphenols, significant in vitro free radical scavenger activity using the DPPH method and an antihyperglycaemic effect in alloxan-induced experimental diabetes. S. cumini spray-dried extracts were obtained using silicon dioxide and cassava starch as adjuvants. The powders showed acceptable flowability, compactability, and low hygroscopicity at 43% relative humidity. Besides, the spray-dried extracts showed in vivo antihyperglycaemic and in vitro scavenger activity comparable to the lyophilized extract. Thus, experimental data indicates that the extract from S. cumini has a relevant activity and that spray-drying could be adequately used to perform the technological processing of S. cumini fluid extracts.

Anticancer activity of sclerotiorin, isolated from an endophytic fungus Cephalotheca faveolata Yaguchi, Nishim. & Udagawa.

Biodiversity provides critical support for drug discovery. A significant proportion of drugs are derived, directly or indirectly, from biological sources. Through high throughput screening (HTS) and bioassay-guided isolation, bioactive compound sclerotiorin has been isolated from an endophytic fungus Cephalotheca faveolata. Sclerotiorin was found to be potent anti-proliferative against different cancer cells. In this study sclerotiorin has been found to induce apoptosis in colon cancer (HCT-116) cells through the activation of BAX, and down-regulation of BCL-2, those further activated cleaved caspase-3 causing apoptosis of cancer cells.

Antiviral activity of crude extracts of Eugenia jambolana Lam. against highly pathogenic avian influenza (H5N1) virus.

Crude extracts of leaves and bark of E. jambolana were tested for antiviral activity against highly pathogenic avian influenza virus (H5N1) by CPE reduction assay in three different layouts to elucidate virucidal, post-exposure and pre-exposure antiviral activity of the extracts. The cold and hot aqueous extracts of bark and hot aqueous extract of leaves of E. jambolana showed significant virucidal activity (100% inhibition) which was further confirmed in virus yield reduction assay (~98 to 99% reduction) and by egg based in ovo assay. The selective index (CC50/EC50) of hot aqueous extract (248) and cold aqueous extract (43.5) of bark of E. jambolana showed their antiviral potential against H5N1 virus. The significant virucidal activity of leaves and bark of E. jambolana merits further investigation as it may provide alternative antiviral agent for managing avian influenza infections in poultry farms and potential avian-human transmission.

Syzygium cumini (L.) Skeels：A review of its phytochemical constituents and traditional uses

Syzygium cumini (S. cumini) (L.) Skeels (jambolan) is one of the widely used medicinal plants in the treatment of various diseases in particular diabetes. The present review has been primed to describe the existing data on the information on botany, phytochemical constituents, traditional uses and pharmacological actions of S. cumini (L.) Skeels (jambolan). Electronic database search was conducted with the search terms of Eugenia jambolana, S. cumini, jambolan, common plum and java plum. The plant has been viewed as an antidiabetic plant since it became commercially available several decades ago. During last four decades, numerous folk medicine and scientific reports on the antidiabetic effects of this plant have been cited in the literature. The plant is rich in compounds containing anthocyanins, glucoside, ellagic acid, isoquercetin, kaemferol and myrecetin. The seeds are claimed to contain alkaloid, jambosine, and glycoside jambolin or antimellin, which halts the diastatic conversion of starch into sugar. The vast number of literatures found in the database revealed that the extracts of different parts of jambolan showed significant pharmacological actions. We suggest that there is a need for further investigation to isolate active principles which confer the pharmacological action. Hence identification of such active compounds is useful for producing safer drugs in the treatment of various ailments including diabetes.

Wound healing activities of eugenia jambolana lam. Bark extracts in albino rats.

Wound healing is physiological process, which takes place by body's natural regenerative capacity. Due to various reasons there may be delay in healing and this prolonged healing may sometimes lead to scar formation. Currently attention has been focused on natural products to prevent infection and to promote healing. In the present study, Eugenia jambolana bark extracts was taken to investigate its wound healing property. Full thickness deep burn wound model in Albino rats, were used to study the healing efficiency. Formulations (10% ointment) of crude ethanolic extract of the Eugenia jambolana bark was applied tropically over thermal wound. It was found that ointment treated rats showed accelerated healing than the control. It was observed that 10% extract of the Eugenia jambolana bark has progressive effects on wound healing in the experimental groups. This study suggests that Eugenia jambolana bark powder could be developed as a therapeutic agent for wound healing.

Attenuation of renal dysfunction by anti-hyperglycemic compound isolated from fruit pulp of Eugenia jambolana in streptozotocin-induced diabetic rats.

The renal protective effect of an active principle isolated from the aqueous extract of fruit pulp of Eugenia jambolana was investigated in streptozotocin(45 mg/kg body weight)-induced severely diabetic rats (FBG ≥ 300 mg/dl). For isolation of active principle, crude aqueous extract of E. jambolana fruit pulp was subjected to purification by ion-exchange column chromatography, which yielded a partially purified compound (FII), which on further purification by rechromatography gave a purified active compound (FIIc). Purity of FIIc was confirmed by high pressure liquid chromatography. Detailed UV, NMR, IR spectra suggested that FIIc is a small aliphatic organic compound having molecular formula C4H7O4N. Oral administration of FIIc to diabetic rats (10, 15 and 20 mg/kg body weight per day for a period of 60 days) produced significant (P<0.001) fall in fasting blood glucose (FBG) in a dose-dependent manner. Treatment with FIIc (15 mg/kg body wt.) showed significant (P<0.001) improvement in body weight, blood urea, plasma creatinine levels, urinary volume, urinary sugar and microalbuminuria. Renal hypertrophy, assessed as the ratio of the weight of the two kidneys to total body weight was also significantly (P<0.05) improved after treatment with FIIc. The above results suggest that FIIc possesses significant nephroprotective activity.

Antidiabetic and antiulcer effects of extract of eugenia jambolana seed in mild diabetic Rats : Study on gastric mucosal offensive acid-pepsin secretion.

Diabetes has been reported to increase propensity to peptic ulceration through its effect both on offensive and defensive mucosal factors. Seeds of Eugenia jambolana (EJ) have been reported to have both antidiabetic as well as ulcer protective effects. The present study evaluates the antidiabetic effects of ethanolic extract of dried seed kernel of Eugenia jambolana (EJE) and its comparative effect on gastric ulceration and acidpepsin secretion with standard antisecretory FL-blocker. Ranitidine and antidiabetic glibenclamide with a premise that Eugenia jambolana may show better ulcer healing effects by promoting defensive or reducing offensive mucosal factors in mild diabetes (MD) rats. MD was produced in adult rats by administration of streptozotocin (45 mg/kg, ip). EJE was given orally in the doses of 100–400 mg/kg for 10 days and in the dose of 200 mg/kg for 30 days respectively to study its dose- and time-dependent effects on various diabetic parameters like blood glucose, serum cholesterol and triglycerides, insulin level and glycosylated hemoglobin. For ulcer protective and gastric secretion studies, EJE (200 mg/kg) was given orally for 10 days against 2 h cold restraint stress (CRS)-, 4 h pylorus ligation (PL), aspirin (ASP, 200 mg/kg, 4 h) – and 95% ethanol (EtOH, 1 ml/200 g, 1 h)-induced gastric ulcers and offensive acid-pepsin secretion after 4 h PL with cooccurring MD in rats. EJE showed dose-dependent decrease in blood glucose level in MD rats. Blood glucose level remained stable in mild diabetic rats from 3rd day onwards after streptozotocin administration (taken as 1st day for treatment) and EJE (200 mg/kg) showed anti-hyperglycemic effect on 10th day of its administration. Further, EJE in the above dose also decreased cholesterol level with little or no effect on triglycerides level and reversed the decrease and increase in insulin and glycosylated hemoglobin level near to the normal level as observed alter 30 days treatment in MD rats. MD rats exhibited an increased propensity to gastric ulceration induced by CRS, ASP, EtOH and PL and caused increase in acid-pepsin secretion. EJE was not only effective in reversing the increased propensity to ulceration in diabetic rats but also decreased the acid-pepsin output better than glibenclamide. The ulcer protective effect of Eugenia Jambolana seems to be due to its antidiabetic and gastric antisecretory effects.

Caracterização farmacognóstica do jambolão (Syzypiam cumini (L. ) Skeels)

A padronização de um fitoterápico é etapa imprescindível para garantia da qualidade de medicamentos contendo plantas medicinais. Objetivou-se padronizar Syzygiam cumini (L.) Skeels e para tanto se estabeleceram parametros tais como, avaliação morfoanatômica das folhas, morfológica das flores e dos frutos, avaliação granulométrica da droga rasurada (frutos), determinação da umidade, avaliação dos processos de secagem, determinação do teor de extrativos e do teor de taninos (monômeros e polimeros). O estudo anatômico das folhas revelou a inexistência de pêlos no sistema dérmico, assim como a ocorrência de glândulas secretoras, drusas, colênquima e esclerênquima. As flores são hermafroditas, com androceu polistêmone e gineceu com ovário ínfero, gamocarpelar, bilocular com placentação axial. Observou-se elevado teor extrativo (38,57 por cento). O diâmetro médio de partícula dos frutos secos moídos ficou em 0,630 mm. O processo de secagem dos frutos influenciou o teor de taninos totais. O teor de taninos determinado ficou em 5,10 por cento para monômeros e 11,30 por cento para os polimeros.

The phytotherapics standardization is an important step for the warranty of the quality of the drugs contends medicinal plants. The aim of this paper was to standardize and establish parameters seeking the characterization of the drug, according to technical pharmacopoeias and in some cases, other techniques were developed. Morphologic description of leaves, flowers and fruits, granulometric analysis of the ground drugs, dry residues, evaluations in the drying methods, determination of the extractive drift and tannins values (monomers and polymers) were executed, being the monomers in the range of 5,10 percent and 11,30 percent for the polymeric ones.