HPLC/DAD, Antibacterial and Antioxidant Activities of Plectranthus Species (Lamiaceae) Combined with the Chemometric Calculations.

The increase in antibiotic resistance and the emergence of new bacterial infections have intensified the research for natural products from plants with associated therapy. This study aimed to verify the antibacterial and antioxidant activity of crude extracts of the genus Plectranthus species, being the first report on the modulation of aminoglycosides antibiotic activity by Plectranthus amboinicus extracts. The chemical composition was obtained by chemical prospecting and High-Performance Liquid Chromatography with diode arrangement detector (HPLC/DAD). The antibacterial activities of the extracts alone or in association with aminoglycosides were analyzed using the microdilution test. The antioxidant activity was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging. The phytochemical prospection allowed the flavonoids, saponins, tannins and triterpenoids to be identified. Quercetin, rutin, gallic acid, chlorogenic acid, caffeic acid, catechin, kaempferol, glycosylated kaempferol, quercitrin, and isoquercitrin were identified and quantified. The principal component analysis (PCA) observed the influence of flavonoids and phenolic acids from Plectranthus species on studied activities. Phytochemical tests with the extracts indicated, especially, the presence of flavonoids, confirmed by quantitative analysis by HPLC. The results revealed antibacterial activities, and synergistic effects combined with aminoglycosides, as well as antioxidant potential, especially for P. ornatus species, with IC50 of 32.21 µg/mL. Multivariate analyzes show that the inclusion of data from the antioxidant and antibacterial activity suggests that the antioxidant effect of these species presents a significant contribution to the synergistic effect of phytoconstituents, especially based on the flavonoid contents. The results of this study suggest the antibacterial activity of Plectranthus extracts, as well as their potential in modifying the resistance of the analyzed aminoglycosides.

Impact of drying processes on Bryophyllum pinnatum phenolic constituents and its anti-inflammatory and antioxidative activities in human erythrocytes.

The effect of drying on the phytoconstituents, antioxidative, and anti-inflammatory properties of Bryophyllum pinnatum leaves was investigated. The phenolic constituents were characterized using HPLC-DAD. The aqueous extraction was done and various assays (Inhibition of membrane stabilization, albumin Denaturation and heat-induced hemolysis, malondialdehyde (MDA), and reduced glutathione (GSH) contents, as well as superoxide dismutase (SOD) activity), were carried out on human erythrocytes. The fresh portion (89.12 µg/ml) exhibited the highest potential to inhibit heat-induced hemolysis compared to the standard drug-Diclofenac (91.51 µg/ml). Freeze-dried sample showed the highest inhibitory potential on albumin denaturation ([Freeze-dried-330.72 µg/ml], [Diclofenac-318.63 µg/ml]) and membrane destabilization ([Freeze-dried-331.93 µg/ml], [Diclofenac-289.57 µg/ml]) when compared with Diclofenac. Similarly, the freeze-dried sample showed the highest GSH and SOD level and lowest MDA level when human erythrocytes challenged with tertiary butyl hydroperoxide (tBHP) were treated with the extract. This study confirms the retention of a considerable quantity of bioactive constituents of plants when freeze-dried. PRACTICAL APPLICATIONS: The ideal method of drying Bryophyllum pinnatum and possible anti-inflammatory potential was investigated. This work may apply to the development of anti-inflammatory agents from a natural source with little or no side effect in managing inflammation.

Fluted pumpkin (Telfairia occidentalis) seed modulates some markers of erectile function in isolated rat's corpus cavernosum: Influence of polyphenol and amino acid constituents.

Pumpkin seeds are often used in traditional medicine in the management of erectile dysfunction. However, there is insufficient information about the possible biochemical rationale behind this practice. Hence, this study investigated the influence of fluted pumpkin seed on critical enzymes involved in erectile function in isolated rats' corpus cavernosum in vitro. The phenolics and amino acid contents of fluted pumpkin seed were determined using HPLC-DAD and GC-PFPD analyses respectively. The aqueous extract of the fluted pumpkin seed significantly (p < .05) scavenged free radicals and inhibited PDE-5, arginase, AChE, and ACE in rats' corpus cavernosum in a concentration-dependent pattern. Quercitrin and luteolin were the most dominant phenolics, while arginine, aspartate, and cysteine were the most aboundant amino acid constituents. The positive modulatory effect of the fluted pumpkin seed on these critical markers of erectile function could be attributed to its polyphenolics and amino acid constituents. PRACTICAL APPLICATIONS: This study brought to limelight the medicinal importance of fluted pumpkin seed in erectile functions. Therefore, this seed could be used as a functional food ingredient in the management of erectile dysfunctions and also in improving erectile functions in men. In addition, the dominant phenolics and amino acid constituents of this seed might be an effective nutraceutical in enhancing erections in men.

Antinociceptive and anti-inflammatory activities of Philodendron bipinnatifidum Schott ex Endl (Araceae).

ETHNOPHARMACOLOGICAL RELEVANCE: Popular medicine use stems of Philodendron bipinnatifidum (Araceae) in inflammation cases, such as in erysipelas, as well as orchitis and rheumatism treatment. The present study, conducted for the first time in literature, investigate the antinociceptive and anti-inflammatory activities of P. bipinnatifidum stems ethyl acetate extract (EPB). MATERIALS AND METHODS: GC/MS and HPLC analysis were performed for EPB extract. We used EPB at 250, 375 and 500 mg/kg (oral route, p.o.) in male Swiss mice. The antinociceptive activity of the plant extract assessed by acetic acid induced writhing and formalin tests. To investigate the possible participation of opioid system in EPB-mediated effects, we previously administered naloxone to the mice. Anti-inflammatory activity was evaluated using carrageenan-induced paw oedema. The open-field test aimed to investigate the possible EPB effects on the locomotor and exploratory activities. To assess the protective role of EPB on carrageenan-induced oxidative stress, the levels of NPSH, TBARS, as well as SOD and CAT activities were evaluated in blood and paw tissue. The acute toxicity of the EPB was investigated using OECD 423 guideline. RESULTS: The EPB chemical analysis by GC/MS and HPLC revealed the presence of flavonoids (luteolin and quercetin) and phytosterols (ß-sitosterol and stigmasterol). The oral treatment with the EPB inhibited mice abdominal writhings (P < 0.01) at 375 and 500 mg/kg, and reduced the formalin effect at the first-phase (500 mg/kg, P < 0.05) and also at the second-phase (500 mg/kg, P < 0.001) of the test. EPB (375 and 500 mg/kg) did not alter spontaneous locomotion in open field test, however the number of fecal bolus was significantly lower for the EPB group at 500 mg/kg when compared to the vehicle group (P < 0.05). The pretreatment with naloxone caused significant inhibition of antinociceptive activity induced by EPB in the formalin test, revealing the possible involvement of opioid receptors. EPB extract administered at 500 mg/kg (p.o.) prevented carrageenan-induced paw oedema (P < 0.05 and 0.01) until 6 h after carragenan injection. Evaluation of TBARS and NPSH levels, SOD and CAT activities in the blood and paw tissue of animals submitted to the carrageenan assay suggested that the anti-inflammatory effect of EPB may be linked to oxidative stress inhibition. The acute administration of the EPB (2000 mg/kg, p.o.) caused no mortality, demonstrating low toxicity. CONCLUSIONS: The extract of P. bipinnatifidum displays antinociceptive and anti-inflammatory activities, causing no toxicological effects. The pharmacological activity of this vegetal species may be related to the presence of flavonoids and phytosterols. Our results support the ethnomedical use of this vegetal species as analgesic and anti-inflammatory agent.

Tabernaemontana catharinensis leaves effectively reduce the irritant contact dermatitis by glucocorticoid receptor-dependent pathway in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Tabernaemontana catharinensis, popularly known as snakeskin, is used in traditional medicine to treat skin inflammatory disorders. To confirm the topical anti-inflammatory effect of T. catharinensis leaves, we evaluated the therapeutic effect of crude extract (TcE) and its different fractions on irritant contact dermatitis model in mice and verified its anti-inflammatory action mechanism. MATERIALS AND METHODS: The qualitative phytochemical analysis of TcE and its dichloromethane, n-butanol and ethyl acetate fractions was performed by UHPLC-ESI-HRMS. The gel accelerated stability was performed to ensure the effectiveness formulation. We investigated the TcE' inhibitory effect, its fractions and a gel formulation containing TcE in irritant contact dermatitis models induced by unique (1000 µg/ear) and multiple (400 µg/ear) croton oil application, evaluated by the ear edema formation, inflammatory cell infiltration (MPO activity measurement and histological procedure) and pro-inflammatory cytokines levels. The action glucocorticoid-like of TcE was investigated using a glucocorticoid receptor antagonist (mifepristone; 50 mg/kg, s.c.). RESULTS: The treatments (10 µg/ear) reduced the ear edema and MPO activity by 100% and 94 ± 3% (TcE) 85 ± 4% and 88 ± 3% (dichloromethane fraction), 83 ± 6% and 73 ± 11% (n-butanol fraction) and 86 ± 6% and 93 ± 4% (ethyl acetate fraction) and 100% (dexamethasone solution), respectively to the acute ICD model. The TcE and dexamethasone gel (15 mg/ear) also reduced by 66 ± 6% and 70 ± 5% the ear edema and by 58 ± 14% and 84 ± 4% the MPO activity, respectively. To the chronic ICD model, the TcE and dexamethasone (10 µg/ear) also reduced the ear edema (66 ± 6% and 70 ± 5%) and the MPO activity (58 ± 14% and 84 ± 4%); on the 9th day of the experiment. TcE and dexamethasone also reduced the pro-inflammatory cytokines (MIP-2, IL-1ß and TNF-α) levels in acute ICD model induced by croton oil. Besides, mifepristone prevented the topical anti-edematogenic effect of TcE' and dexamethasone' solutions by 97 ± 9% to TcE and 75 ± 15% to dexamethasone. The accelerated stability study of T.catharinensis gels showed no relevant changes at low temperatures. The dereplication of the TcE and fractions revealed the presence of indole alkaloids, triterpenes, and flavonoids by UHPLC-ESI-HRMS. These classes of compounds are known in the literature for present potential anti-inflammatory action, supporting the results obtained. CONCLUSION: The results confirm the topical popular use ofT.catharinensis leaves in the treatment of skin inflammation and demonstrate the TcE' potential for the development of a promising topical anti-inflammatory agent to treat inflammatory disorders.

Tabernaemontana catharinensis leaves exhibit topical anti-inflammatory activity without causing toxicity.

BACKGROUND: Tabernaemontana catharinensis, popularly known as snake skin, has been empirically used as an anti-inflammatory to treat cutaneous skin disorders. However, no study proves its effectiveness as a topical anti-inflammatory. STUDY DESIGN: We investigated the topical anti-inflammatory effect of T.catharinensis leaves crude extract (TcE) in irritant contact dermatitis models in mice and its preliminary toxicity profile. METHODS: The topical anti-inflammatory effect was evaluated by ear thickness measurement, inflammatory cell infiltration (MPO activity measurement and histological procedure) and cytokines levels. TcE qualitative phytochemical analysis was performed by UHPLC-ESI-HRMS and the TcE effect (therapeutic dose; 10 µg/ear) on preliminary toxicological parameters was also evaluated (on the 14°â€¯day of experiment). RESULTS: TcE (10 µg/ear) prevented the development of ear edema induced by cinnamaldehyde, capsaicin, arachidonic acid, phenol, and croton oil with maximum inhibition of 100% to cinnamaldehyde, arachidonic acid, phenol, and croton oil and 75 ±â€¯6% to capsaicin. Besides, the TcE (10 µg/ear) also prevented the increase of MPO activity by 96 ±â€¯2%, 48 ±â€¯7%, 100%, 87 ±â€¯8%, and 93 ±â€¯4%, respectively, to the same irritant agents. The positive controls also prevented both ear edema and the increased of MPO activity by 100% and 42 ±â€¯8% (HC-030031), 54 ±â€¯6% and 80 ±â€¯4% (SB-366791), 100% and 54 ±â€¯5% (indomethacin), 100% and 80 ±â€¯4% (dexamethasone in skin inflammation model induced by phenol) and 100% and 97 ±â€¯3% (dexamethasone in inflammation model induced by croton oil), respectively. TcE also prevented the inflammatory cells infiltration and the increase of MIP-2, IL-1ß and TNF-α levels irritant agents-induced. TcE topical anti-inflammatory effect may be attributed to the combined effect of indole alkaloids, terpenes, and phenolic compounds found in the extract and identified by dereplication method. The TcE' therapeutic dose proved to be safe in preliminary toxicological tests. CONCLUSION: Our results suggest that TcE could be an interesting strategy for the treatment of inflammatory diseases.

Drying alters the phenolic constituents, antioxidant properties, α-amylase, and α-glucosidase inhibitory properties of Moringa (Moringa oleifera) leaf.

Moringa oleifera leaf is a popular green leafy vegetable which has found its usefulness in the preparation of traditional stews and soups. Like most green leafy vegetable which are not around year-round, the leaf is usually dried and pulverized for storage and easier handling, and despite the popularity of this processing technique, there is dearth of information on how drying affects the health-promoting properties of the leaves. Hence, this study sought to investigate the effect of some drying methods (freeze-drying, sun, air and oven drying) on the phytoconstituents, antioxidant properties, and biological activities of moringa leaf. This study revealed that drying methods significantly altered the phytoconstituents (phenolics, flavonoids, vitamin C, tannin, saponin, phytate, oxalate, alkaloid, cardenolides, and cardiac glycosides), antioxidant capacities (reducing power, Fe2+chelating, ABTS •+, DPPH, and • OH scavenging abilities), and enzyme inhibitory (α-amylase and α-glucosidase) effects of the leaf, with freeze-drying being the most promising method for preserving the nutraceutical properties of moringa leaf. However, for practical application, the order of preference of the drying methods which ensures adequate retention of phytoconstituents and possibly biological activities of the leaf as observed in this study is freeze-drying > air drying > sun drying > oven drying, in the order of decreasing magnitude.

In vitro antioxidant activities and inhibitory effects of phenolic extract of Senecio biafrae (Oliv and Hiern) against key enzymes linked with type II diabetes mellitus and Alzheimer's disease.

The phenolic extract of Senecio biafrae leaves was investigated to determine the in vitro antioxidant, phenolic profiles, and inhibition of key enzymes relevant to type II diabetes mellitus (α-amylase and α-glucosidase) and Alzheimer's disease (acetylcholinesterase and butrylcholinesterase). The phenolic extract demonstrated significant scavenging abilities against all in vitro antioxidant parameters assessed. Reversed-phase HPLC of the extract revealed the presence of gallic acid, chlorogenic, caffeic acid, rutin, quercetin, and kaempferol. The extract also inhibited activities of α-amylase (IC 50 = 126.90 µg/ml), α-glucosidase (IC 50 = 139.66 µg/ml), acetylcholinesterase (IC 50 = 347.22 µg/ml), and butrylcholinesterase (IC 50 = 378.79 µg/ml), which may be attributed to the antioxidant potential of the extract and its phenolic composition. Therefore, this study suggests that the leaves of S. biafrae may be useful in the management of diabetes mellitus and Alzheimer's disease.

Effect of dietary supplement from mono-culture fermentation of Moringa oleifera seeds by Rhizopus stolonifer on hematology and markers linked to hypercholesterolemia in rat model.

Mono-culture fermentation by Rhizopus stolonifer could promote the healthiness of immune systems and cholesterol levels. Hence, we examined the effect of diet from mono-culture fermentation of Moringa oleifera seeds by R. stolonifer (MCF-MORS) on hematological parameters and fundamental indicators of hypercholesterolemia in rat. The animals were divided into six groups (n = 6). Group 1 was placed on basal diet. Group II, III, IV and V were placed on a basal diets supplemented with 7.5%, 15%, 22.5% and 30%, respectively, of MCF-MORS. Group VI was placed on basal diet fed with unfermented M. oleifera seeds (UF-MOS). The experiment lasted for eight weeks. The results revealed 7.5% MCF-MORS as better biological method to augment PCV, RBC and Hb count in animal model. Also, 7.5% and/or 15% MCF-MORS demonstrated highest levels in centrophils, neutrophils and eosinophils, whereas the levels of lymphocytes, basophils and monocytes showed no significant difference. Similarly, 7.5% and 15% MCF-MORS modulated LDL and HDL, respectively, better than UF-MOS; but showing no difference in cholesterol level. MCF-MORS also maintained architectural integrity of villi and splenocytes better than UF-MOS. We therefore concluded that diet from MCF-MORS at 7.5% and 15% modulates HDL, LDL, cholesterol and immune system-related disorders better than UF-MOS in rat model.

Protective role of jaboticaba Plinia peruviana peel extract in copper-induced cytotoxicity in Allium cepa.

Jaboticaba Plinia peruviana (Poir.) Govaerts is a Brazilian berry that presents high levels of polyphenols, which may play a key role in preventing cytotoxic and genotoxic effects of harmful agents. Although copper is an essential micronutrient that plays an important role in organisms, high copper concentrations may trigger toxicity to animals and plants. Here, we investigated whether Plinia peruviana hydroalcoholic extract prevents copper-induced cytotoxicity in Allium cepa root cells. Five different anthocyanins and phenolic compounds were identified in Plinia peruviana extract. Importantly, the exposure to 1.53 mg/L copper for 24 h impaired mitotic index, as well as increased mitosis disturbances and triggered DNA damage. Pre-incubation with Plinia peruviana extract (0.25 g/L and 0.75 g/L) for 3 h prevented copper-induced changes in the mitotic index and reduced the number of abnormal cells. In conclusion, we suggest that Plinia peruviana peel extract has protective effects against cellular and genetic disturbances induced by copper.

Insecticidal and repellent effect of cinnamon oil on flies associated with livestock / Efecto insecticida y repelente del aceite de canela sobre moscas asociadas con el ganado

Abstract Objective. Due to the increased parasitic resistance, there is a need to explore alternative insecticides, including natural products, such essential oils. In this sense, the aim of this study was to evaluate, for the first time, the insecticidal and repellent effect of Cinnamomun zeylanicum (free and nanoemulsion forms) in vitro and in vivo. Materials and methods. For that, the insecticidal effect of the free form was tested at 1.0, 5.0 and 10%, while the nanoemulsion form was tested at 0.5, 1.0 and 5.0% against adult house flies, Musca domestica. For validation of the test, the flies were sprayed with the diluent (water and triton 10%) and with blank nanoemulsion (without C. zeylanicum essential oil). Moreover, in vivo test was performed using cows naturally infested with Haemotobia irritans. Results. The results demonstrated that cinnamon oil (10%) and the nanoemulsion (5%) were 100% effective against M. domestica after 90 minutes of exposure. The repellent effect was tested in vivo using 5% of cinnamon oil on Holstein cows naturally infested by Haemotobia irritans. The flies were counted at 0, 1, 2, 3, 9 and 24 h after cinnamon oil treatment. It was verified significant decrease (p<0.05) in the number of flies on cows sprayed with cinnamon in all times. Conclusions. Based on these results, C. zeylanicum showed insecticidal effect (in vitro) against domestic flies and repellent effect (in vivo) against the horn fly.

Resumen Objetivo. Debido a la mayor resistencia parásita, hay una necesidad de explorar insecticidas alternativos, incluidos los productos naturales, tales como aceites esenciales. En este sentido, el objetivo de este estudio fue evaluar, para el primer equipo, el efecto insecticida y repelente de Cinnamomum zeylanicum (formas libres y nanoemulsión) in vitro e in vivo. Materiales y métodos. Para ello, el efecto insecticida de la forma libre se ensayó a 1.0, 5.0 y 10%, mientras que la forma nanoemulsión se ensayó a 0.5, 1.0 y 5.0% frente a las moscas domésticas adultas, Musca domestica. Para la validación de la prueba, las moscas fueron rociados con el diluyente (agua y triton 10%) y con nanoemulsión en blanco (sin aceite esencial de C. zeylanicum). También, fueron realizados pruebas in vivo usando vacas naturalmente infestadas con Haemotobia irritans. Resultados. Los resultados demostraron que el aceite de canela (10%) y la nanoemulsión (5%) fueron 100% eficaz contra M. domestica después de 90 minutos de exposición. El efecto repelente se ensayó in vivo usando 5% de aceite de canela en vacas Holstein, naturalmente infestados por Haemotobia irritans. Se contaron las moscas a las 0, 1, 2, 3, 9 y 24 h después del tratamiento el aceite de canela. Se verificó disminución significativa (p<0.05) en el número de moscas vivas de vacas canela pulverizada en todo momento. Conclusiones. En base a estos resultados, C. zeylanicum mostró un efecto insecticida (in vitro) contra las moscas domésticas y efecto repelente (in vivo) contra la mosca de los cuernos.

Protective effect of Uncaria tomentosa extract against oxidative stress and genotoxicity induced by glyphosate-Roundup® using zebrafish (Danio rerio) as a model.

Oxidative stress and DNA damage are involved in the glyphosate-based herbicide toxicity. Uncaria tomentosa (UT; Rubiaceae) is a plant species from South America containing bioactive compounds with known beneficial properties. The objective of this work was to evaluate the antioxidant and antigenotoxic potential of UT extract in a model of acute exposure to glyphosate-Roundup® (GR) in zebrafish (Danio rerio). We showed that UT (1.0 mg/mL) prevented the decrease of brain total thiols, the increase of lipid peroxidation in both brain and liver, and the decrease of liver GPx activity caused after 96 h of GR (5.0 mg/L) exposure. In addition, UT partially protected against the increase of micronucleus frequency induced by GR exposure in fish brain. Overall, our results indicate that UT protects against damage induced by a glyphosate-based herbicide by providing antioxidant and antigenotoxic effects, which may be related to the phenolic compounds identified in the extract.

Launaea taraxacifolia (Willd.) Amin ex C. Jeffrey inhibits oxidative damage and econucleotidase followed by increased cellular ATP in testicular cells of rats exposed to metropolitan polluted river water.

BACKGROUND: Humans are directly/indirectly exposed to hazardous chemicals from the aquatic environment. We investigated the protection of the Launea taraxacifolia methanolic extract (LTME) on the hydroxyl steroid dehydrogenases [(∆5-3ß-hydroxyl steroid dehydrogenase (∆5-3ß-HSD) and the ∆5-17ß-hydroxyl steroid dehydrogenase (∆5-17ß-HSD), testicular 5'-nucleotidase and lactate dehydrogenase (LDH)] activities as well as the key indicators of oxidative stress in germinal epithelial cells of rats induced with surulere polluted river water (SPRW). METHODS: The animals were divided into six groups (n=8). Group I was given 1 mL of distilled water only, Group II received 1 mL of SPRW only, Group III received 200 mg/kg LTME before+1 mL of SPRW after, Group IV received 200 mg/kg LTME+1 mL of SPRW, Group V received 1 mL of SPRW before+200 mg/kg LTME after and Group VI received 200 mg/kg LTME only. The treatment was done via oral administration for 28 days. RESULTS: The HPLC results showed the abundance of quercetin and quercitrin. The SPRW increased 5'-nucleotidase with the concomitant decrease of ∆5-3ß-HSD, ∆5-17ß-HSD and LDH activities in rats exposed in relation to the control. Similarly, the administration of the SPRW caused a systemic oxidative damage along with adverse histopathological changes in germinal epithelial cells. CONCLUSIONS: Interestingly, these alterations were differentially reversed by LTME via the elevation of steroidogenic enzymes and cellular ATP.

HPLC and in vitro evaluation of antioxidant properties of fruit from Malpighia glabra (Malpighiaceae) at different stages of maturation.

Malpighia glabra L. is indicated for the treatment of diseases due presenting several medicinal properties. The aim of the present study was quantify phenolic compounds and carotenoids, additionally, evaluate the antioxidant potential of different methanolic fractions (mature stage, intermediate stage and green maturity stage) of Malpighia glabra. Methanolic fractions of the three stages of maturation were characterized using HPLC-DAD. The antioxidant activity of fractions was evaluated using in vitro assay systems: iron-chelating activity (Fe2+), inhibition of the radical 1-1-diphenyl-2-picrylhydrazyl (DPPH) and inhibition of production of thiobarbituric acid reactive substances (TBARS). In quantifying compounds by HPLC-DAD showed that the compounds rutin and quercetin showed the highest peaks in the three samples tested. Regarding carotenoids, the ß-carotene stood in the analyze. The methanolic fraction of lyophilized pulp of green fruits showed better results for iron chelation and DPPH tests; TBARS by the methanolic fraction of the ripe fruits showed lower IC50 as the basal. When in the presence of iron as an inducer of peroxidation, the methanolic fraction of the pulp of green fruits showed the lowest IC50. Our research indicates that the o fruits of M. glabra good potential in scavenging free radicals and can be an important source of antioxidant phytochemical.

Syzygium cumini leaf extract inhibits LDL oxidation, but does not protect the liproprotein from glycation.

ETNOPHARMACOLOGICAL RELEVANCE: Syzygium cumini (L.) Skeels is a plant widely used in folk medicine to treat diabetes mellitus (DM). The tea from its leaves is frequently used by diabetics for lowering hyperglycemia. There is a close relationship between DM and atherosclerosis, a chronic immuno-inflammatory disease, were the early stages encompass oxidative and glycative modifications in the structure of low density lipoprotein (LDL). AIM OF THIS STUDY: To investigate the potential protective effects of aqueous-leaf extract from Syzygium cumini (S.cExt) against CuSO4-induced oxidation and methylglyoxal (MG)-induced glycation of human LDL in vitro. MATERIALS AND METHODS: LDL oxidative changes were evaluated by measuring conjugated dienes (CD) formation, thiobarbituric acid reactive substances (TBARS) levels, quenching of tryptophan (Trp) fluorescence and structural modifications in LDL particle. In LDL glycated by MG (glyLDL), we determined the levels of fluorescent advanced glycation end products (AGEs) and mobility by agarose gel electrophoresis. RESULTS: S.cExt blocked oxidative events induced by CuSO4 in human LDL, plasma and serum. Fourier transform infrared spectroscopy (FT-IR) revealed that specific regions of apoB100 were oxidized by CuSO4 in human LDL and that S.cExt reduced these oxidations. Unlike, the increased AGEs levels and eletrophoretic mobility observed in LDL MG-glycated were not modified by S.cExt. CONCLUSION: The findings herein indicate that S.cExt could be tested in atherogenesis models as potential protective agent against LDL oxidation.

Angiotensin-1-converting enzyme inhibition, antioxidant activity, and modulation of cerebral Na+/K+ ATPase by free phenolics of African locust bean (Parkia biglobosa).

AIMS: To investigate the antioxidant activities and effects of free phenols (FPPB) and bound phenols (BPPB) of Parkia biglobosa leaves on some enzymes of neuro-cardiovascular relevance. METHODS AND RESULTS: HPLC-DAD fingerprinting of FPPB and BPPB, and the antihemolytic, radical (1,1-diphenyl-2 picrylhydrazyl, DPPH; 2,2-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid), ABTS) scavenging and ferric reducing antioxidant properties of extracts, were assessed. In addition, the effects of the phenolics on angiotensin-1-converting enzyme (ACE), cerebral acetylcholinesterase/butyrylcholinesterase (AChE/BuChE), and Na+/K+ATPase were determined in vitro. FPPB was more potent than BPPB in terms of ABTS (EC50:4.06 ± 0.3 vs 24.07 ± 2.1 µg/mL) and DPPH (EC50:3.82 ± 0.2 vs 10.22 ± 0.1 µg/mL) radicals scavenged, respectively. The free phenolic extract was a better DPPH. scavenger than ascorbic acid (EC50 = 12.58 ± 0.4 µg/mL; DPPH reference) and compared well with Trolox (EC50:4.44 ± 0.08 µg/mL; ABTS reference). The anti-hemolytic effect of FPPB (36%) and BPPB (53%) was highest at 15 µg/mL but lower than that recorded for ascorbic acid (67% at 10 µg/mL). Even though FPPB (IC50 = 15.35 ± 4.0 µg/mL) and BPPB (IC50 = 46.85 ± 3.3 µg/mL) showed considerably lower ACE-inhibitory effect than ramipril (IC50:0.173 ± 0.04 µg/mL), both extracts demonstrated dose-dependent, significant (p < 0.01/p < 0.05) inhibition of the enzyme. FPPB increased cerebral Na+/K+ATPase activity but neither phenolic extract affects cerebral AChE/BuChE activities. HPLC-DAD revealed catechin, caffeic acid, and quercetin, respectively, as the major phenolics (mg/g) in FPPB (29.85, 30.29, and 17.10) and BPPB (32.70, 30.51, and 19.25). CONCLUSION: The effects of P biglobosa on ACE and cerebral ATPase are related to its constituent phenolics. ACE inhibition could be an important mechanism underlying the documented hypotensive effect of the plant.

Phenolic constituents and modulatory effects of Raffia palm leaf (Raphia hookeri) extract on carbohydrate hydrolyzing enzymes linked to type-2 diabetes.

This study sought to investigate the effects of Raffia palm (Raphia hookeri) leaf extract on enzymes linked to type-2 diabetes mellitus (T2DM) and pro-oxidant induced oxidative stress in rat pancreas. The extract was prepared and its α-amylase and α-glucosidase inhibitory effects were determined. Radical [2,2-diphenyl-1-picrylhydrazyl (DPPH)] scavenging and Fe2+-chelating abilities, and inhibition of Fe2+-induced lipid peroxidation in rat pancreas homogenate were assessed. Furthermore, total phenol and flavonoid contents, reducing property, and high performance liquid chromatography diode array detector (HPLC-DAD) fingerprint of the extract were also determined. Our results revealed that the extract inhibited α-amylase (IC50 = 110.4 µg/mL) and α-glucosidase (IC50 = 99.96 µg/mL) activities in concentration dependent manners which were lower to the effect of acarbose (amylase: IC50 = 18.30 µg/mL; glucosidase: IC50 = 20.31 µg/mL). The extract also scavenged DPPH radical, chelated Fe2+ and inhibited Fe2+-induced lipid peroxidation in rat pancreas all in concentration dependent manners with IC50 values of 402.9 µg/mL, 108.9 µg/mL and 367.0 µg/mL respectively. The total phenol and flavonoid contents were 39.73 mg GAE/g and 21.88 mg QAE/g respectively, while the reducing property was 25.62 mg AAE/g. The HPLC analysis revealed the presence of chlorogenic acid (4.17 mg/g) and rutin (5.11 mg/g) as the major phenolic compounds in the extract. Therefore, the ability of the extract to inhibit carbohydrate hydrolyzing enzymes and protect against pancreatic oxidative damage may be an important mechanisms supporting its antidiabetic properties and could make Raffia palm leaf useful in complementary/alternative therapy for management of T2DM. However, further studies such as in vivo should be carried out.

Phenolic extracts and amino acids content from Cucumeropsis mannii naudin and Citrullus lanatus inhibit relevant enzymes of erectile dysfunction in rat's penile tissue.

•A focused on the erectogenic potentials of two tropical pumpkin seeds was established.•The antioxidant properties of these seed varieties were also discussed.•The inhibitory effects of the seeds on key enzymes relevant to ED were critically explored.•The potentials of the seeds to manage ED were recommended.

Assessment of the antiproliferative and antigenotoxic activity and phytochemical screening of aqueous extracts of Sambucus australis Cham. & Schltdl. (ADOXACEAE).

The purpose of this study was to evaluate the antiproliferative and antigenotoxic activity of Sambucus australis Cham. & Schltdl. aqueous extracts on the cell cycle of Allium cepa L. as well as determine the phenolic compounds in such extracts. S. australis inflorescences and leaves of two accessions were used for aqueous extract preparation at concentrations: 0.003 g/ml and 0.012 g/ml. A. cepa bulbs were rooted in distilled water and, subsequently, placed in treatments for 24 hours. Rootlets were collected and fixed in modified Carnoy's solution for 24 hours and kept. The squash technique was performed for slide preparation. Root tips were smashed and stained with 2% acetic orcein, and a total of 4000 cells per treatment were analyzed. The phenolic compounds were determined using high-performance liquid chromatography and data was analyzed using the Scott-Knott test. The results show that S. australis aqueous extracts have antiproliferative potential. Besides, the extracts prepared from S. australis leaves of both accessions at a concentration of 0.012 g/ml have shown antigenotoxic activity. The phytochemical analysis allowed us to determine the presence of flavonoids and phenolic acids, of which kaempferol and chrologenic acid were the most predominant compounds in the extracts from the inflorescences and leaves, respectively.

Nanostructured cinnamon oil has the potential to control Rhipicephalus microplus ticks on cattle.

The aim of this study was to evaluate the capacity of pure and nanostructured cinnamon oil to control the infestation and reproductive efficiency of Rhipicephalus microplus on dairy cows. In vitro (stage I)-engorged female ticks were immersed in concentrations of 1.0, 5.0 and 10% of cinnamon oil on its pure form, and 0.5, 1.0, and 5.0% of the nanostructured form. 10% cinnamon oil (pure form) showed 100% efficacy, whereas concentrations of 1 and 5% were 62 and 97% efficacious, respectively. Nanocapsules and nanoemulsions containing cinnamon oil at 5% showed 95 and 97% efficacy, respectively. In vivo (stage II)-16 naturally tick-infested cows were divided into four groups of four animals each: Group A was composed of dairy cows sprayed with Triton (control); Group B was composed of dairy cows sprayed with cinnamon oil in its pure form (5%), whereas groups C and D were composed of dairy cows sprayed with nanocapsules and nanoemulsions, respectively, containing cinnamon oil at 0.5%. The ticks on each animal were counted on days 0, 1, 4 and 20 after spraying. Animals sprayed with pure and nanoencapsulated cinnamon oil carried significantly fewer ticks on days 1 and 4 post-treatment and were free of ticks on day 20 post-treatment. Ticks collected from these dairy cows (24 h after application) had impaired oviposition and larval inhibition, resulting in 90.5 and 100% efficacy when using pure and nanocapsules, respectively. In conclusion, the pure and nanostructured forms of cinnamon oil interfered with tick reproduction, whereas a significant acaricidal effect was found when applied onto cattle.