Antidiabetic Effect of Passiflora ligularis Leaves in High Fat-Diet/Streptozotocin-Induced Diabetic Mice.

Type 2 diabetes mellitus (T2DM) is a major global public health concern, prompting the ongoing search for new treatment options. Medicinal plants have emerged as one such alternative. Our objective was to evaluate the antidiabetic effect of an extract from the leaves of Passiflora ligularis (P. ligularis). For this purpose, T2DM was first induced in mice using a high-fat diet and low doses of streptozotocin. Subsequently, an aqueous extract or an ethanolic extract of P. ligularis leaves was administered for 21 days. The following relevant results were found: fasting blood glucose levels were reduced by up to 41%, and by 29% after an oral glucose overload. The homeostasis model assessment of insulin resistance (HOMA-IR) was reduced by 59%. Histopathologically, better preservation of pancreatic tissue was observed. Regarding oxidative stress parameters, there was an increase of up to 48% in superoxide dismutase (SOD), an increase in catalase (CAT) activity by 35% to 80%, and a decrease in lipid peroxidation (MDA) by 35% to 80% in the liver, kidney, or pancreas. Lastly, regarding the lipid profile, triglycerides (TG) were reduced by up to 30%, total cholesterol (TC) by 35%, and low-density lipoproteins (LDL) by up to 32%, while treatments increased high-density lipoproteins (HDL) by up to 35%. With all the above, we can conclude that P. ligularis leaves showed antihyperglycemic, hypolipidemic, and antioxidant effects, making this species promising for the treatment of T2DM.

Flavonoids and saponins from Passiflora edulis f. edulis leaves (purple passion fruit) and its potential anti-inflammatory activity.

OBJECTIVES: The objective of this work was to evaluate the anti-inflammatory activity of the aqueous extract, fractions and major compounds, which are isolated and identified from Passiflora edulis f. edulis (purple passion fruit) leaves extract. METHODS: For the isolation of the major compounds, reversed-phase chromatography and normal phase countercurrent chromatography were used. The separation was followed by thin layer chromatography and HPLC-DAD-ELSD. One-dimensional and two-dimensional NMR and ESI-TOF-MS/MS were used for structural elucidation. The anti-inflammatory activity was evaluated on a TPA multiple dose model of skin chronic inflammation in mice. Additionally, myeloperoxidase (MPO) and nitric oxide synthase (NOS) activity assays were performed as possible mechanisms of action studies. KEY FINDINGS AND CONCLUSIONS: The study of the butanolic fraction mainly showed the presence of saponins and flavonoids. Three minor flavonoids were detected; and three known saponins, cyclopassiflosides IX, XI and III were isolated and identified. This is the first unequivocal report of the presence of these compounds in P. edulis f. edulis leaves. The most favourable results of anti-inflammatory activity were obtained for the flavonoid-rich fraction. All the fractions and isolated compounds evaluated, presented high percentages of inhibition of nitric oxide synthase activity.

Adjustable conduits for guided peripheral nerve regeneration prepared from bi-zonal unidirectional and multidirectional laminar scaffold of type I collagen.

Shortness of donor nerves has led to the development of nerve conduits that connect sectioned peripheral nerve stumps and help to prevent the formation of neuromas. Often, the standard diameters of these devices cannot be adapted at the time of surgery to the diameter of the nerve injured. In this work, scaffolds were developed to form filled nerve conduits with an inner matrix with unidirectional channels covered by a multidirectional pore zone. Collagen type I dispersions (5 mg/g and 8 mg/g) were sequentially frozen using different methods to obtain six laminar scaffolds (P1 to P5) formed by a unidirectional (U) pore/channel zone adjacent to a multidirectional (M) pore zone. The physicochemical and microstructural properties of the scaffolds were determined and compared, as well as their biodegradability, residual glutaraldehyde and cytocompatibility. Also, the Young's modulus of the conduits made by rolling up the bizonal scaffolds from the unidirectional to the multidirectional zone was determined. Based on these comparisons, the proliferation and differentiation of hASC were assessed only in the P3 scaffolds. The cells adhered, aligned in the same direction as the unidirectional porous fibers, proliferated, and differentiated into Schwann-like cells. Adjustable conduits made with the P3 scaffold were implanted in rats 10 mm sciatic nerve lesions to compare their performance with that of autologous sciatic nerve grafted lesions. The in vivo results demonstrated that the tested conduit can be adapted to the diameter of the nerve stumps to guide their growth and promote their regeneration.

Phytochemical analysis, antioxidant and anti-inflammatory activity of calyces from Physalis peruviana.

Physalis peruviana calyces are used extensively in folk medicine. The crude ethanolic extract and some fractions of calyces were evaluated in order to explore antioxidant and anti-inflammatory activities. The anti-inflammatory activity was evaluated by the TPA-induced ear edema model. The antioxidant in vitro activity was measured by means of the superoxide and nitric oxide scavenging activity of the extracts and fractions. The butanolic fraction was found to be promising due to its anti-inflammatory and antioxidant activities. Therefore, a bio-assay guided approach was employed to isolate and identify rutin (1) and nicotoflorin (2) from their NMR spectroscopic and MS data. The identification of rutin in calyces of P. peruviana supports the possible use of this waste material for phytotherapeutic, nutraceutical and cosmetic preparations.

Sucrose esters from Physalis peruviana calyces with anti-inflammatory activity.

Physalis peruviana is a native plant from the South American Andes and is widely used in traditional Colombian medicine of as an anti-inflammatory medicinal plant, specifically the leaves, calyces, and small stems in poultice form. Previous studies performed by our group on P. peruviana calyces showed potent anti-inflammatory activity in an enriched fraction obtained from an ether total extract. The objective of the present study was to obtain and elucidate the active compounds from this fraction and evaluate their anti-inflammatory activity in vivo and in vitro. The enriched fraction of P. peruviana was purified by several chromatographic methods to obtain an inseparable mixture of two new sucrose esters named peruviose A (1) and peruviose B (2). Structures of the new compounds were elucidated using spectroscopic methods and chemical transformations. The anti-inflammatory activity of the peruvioses mixture was evaluated using λ-carrageenan-induced paw edema in rats and lipopolysaccharide-activated peritoneal macrophages. Results showed that the peruvioses did not produce side effects on the liver and kidneys and significantly attenuated the inflammation induced by λ-carrageenan in a dosage-dependent manner, probably due to an inhibition of nitric oxide and prostaglandin E2, which was demonstrated in vitro. To our knowledge, this is the first report of the presence of sucrose esters in P. peruviana that showed a potent anti-inflammatory effect. These results suggest the potential of sucrose esters from the Physalis genus as a novel natural alternative to treat inflammatory diseases.

Anti-inflammatory R-prostaglandins from Caribbean Colombian soft coral Plexaura homomalla.

OBJECTIVES: This study aims to evaluate the effect of prostaglandins isolated from soft coral Plexaura homomalla, collected in Colombian Caribbean Sea, on in vivo and in vitro inflammation models. METHODS: Extracts from P. homomalla were fractionated and sequentially chromatographed to obtain the prostaglandins: (15R)-PGA2 (1), (15R)-PGA2 -Me (2), (15R)-O-Ac-PGA2 (3), (15R)-O-Ac-PGA2 -Me (4) and (15R)-PGE2 (5) in addition to three semi-synthetic prostaglandins obtained by transformations of the natural products. The anti-inflammatory properties of natural and semi-synthetic compounds were determined in vivo using 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear oedema model and in vitro leucocyte degranulation, myeloperoxidase (MPO) and elastase enzymatic activities from human polymorphonuclear cells (PMNs). The cell viability was evaluated by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. KEY FINDINGS: In the in vivo assay, (15R)-PGE2 (1) and (15R)-O-Ac-PGA2 (3) showed anti-inflammatory activity, as well as in vitro inhibition of elastase release from PMNs. In the PMNs degranulation assay, (15R)-PGE2 (5), was the most active compound in the inhibition of MPO release. Finally, all the tested prostaglandins showed moderate inhibition for elastase enzyme activity, whereas none of the prostaglandins exhibit significative inhibition on MPO activity. CONCLUSION: (15R)-PGE2 (1) and (15R)-O-Ac-PGA2 (3) present significant inhibition on three important events related to the topical inflammatory response induced by TPA: the oedema formation, the PMNs degranulation, events that modulate MPO and elastase levels at inflammation site, and the inhibition of the enzyme activity.

Fuscoside E: a strong anti-inflammatory diterpene from Caribbean octocoral Eunicea fusca.

The screen of 10 soft coral extracts collected from the Colombian Caribbean Sea in the TPA-induced ear edema model allowed us to identify Eunicea fusca extract among others as an interesting source of active compounds. The new diterpene, fuscoside E (1), along with the known fuscoside B (2), fuscol (3), (+)-germacrene D (4) and a mixture of six sterols (5-10), were isolated from this soft coral. Their structures were elucidated by 1D and 2D NMR spectroscopy techniques. Fuscoside E (1) absolute stereochemistry was determined by chiroptical methods. Fuscoside E (1) and B (2) showed strong anti-inflammatory in the above mentioned bioassay. Additionally, fuscoside E (1) and the sterol mixture (5-10) presented antifouling activity against bacterial strains involved in surface colonization.

Cardiac biomakers for the evaluation of acute coronary syndrome.

The traditional diagnosis of myocardial infarction relies primarily within the exhibited patient's clinical presentation, electrocardiographic changes, and elevation in cardiac markers. Since the clinical presentation can be highly variable and EKG changes are not readily present for all patients, the use of markers of cardiac injury to support the diagnosis of myocardial infarction has become a fundamental part of the evaluation of a patient with suspected acute coronary syndrome. In 2007 the Joint European Society of Cardiology/ American College of Cardiology Committee for the Redefinition of Myocardial Infarction concluded that the main criteria for myocardial infarction should be a rise or fall of cardiac biomarkers (namely cardiac troponins and CK-MB) along with: (1) ischemic symptoms, (2) ischemic changes in EKG, (3) Q waves in EKG, or (4) imaging evidence of loss of myocardial viability or (5) wall motion abnormalities. These changes have increased search interests for more sensitive and specific markers of acute myocardial injury; furthermore, dedicated research has commenced in order to specifically allocate markers that could even predict myocardial ischemia. Therefore this article will review traditional employment of cardiac markers, providing current insight, information and experimental data with respect to emerging markers of myocardial ischemia.

[Antiinflammatory activity of extracts and fractions obtained from Physalis peruviana L. calyces]. / Actividad antinflamatoria de extractos y fracciones obtenidas de cálices de Physalis peruviana L.

INTRODUCTION: Cape gooseberry calyces (Physalis peruviana) have been used in folk medicine for their medicinal properties including anticancer, antimycobacterial, antipyretic, diuretic, immunomodulatory and antiinflammatory properties. OBJECTIVE: The antiinflammatory effect was evaluated for extracts and fractions obtained from Physalis peruviana calyces in a mice model of acute inflammation. The fractions responsible for antiinflammatory activity were extracted for possible identification. MATERIALS AND METHODS: The Physalis peruviana calyces were extracted by percolation with organic solvents. The primary hydroalcoholic fraction was purified by column chromatography. The antiinflammatory effect of extracts and fractions was evaluated using the 12-O-tetradecanoylphorbol-13-acetate-induced mouse model of ear edema. RESULTS: Thirty-eight secondary fractions were obtained by column chromatography of primary hydroalcoholic fraction. Six fractions, evaluated in 12-O-tetradecanoylphorbol-13-acetate-induced inflammation assay, showed significant antiinflammatory activity (p<0.05). The major fraction, Pp-D28-LF, showed a significant dose-dependent response at doses over 250 microg/ear. CONCLUSION: The antiinflammatory activity attributed to Physalis peruviana calyces was confirmed and validated its use in folk medicine. Fractions responsible for the antiinflammatory action were identified and seem promising for phytomedicinal development. Further studies are needed to isolate and identify the active constituents of these fractions as well as to ascertain the mechanisms involved in the antiinflammatory effect.

Hyperinsulinemic-euglycemic therapy for intoxication with calcium channel blockers.

Conventional therapy for intoxication with calcium channel blockers consists of crystalloid solutions, calcium gluconate, glucagon and vasopressor agents. These therapies often fail to improve hemodynamic function in intoxicated patients. The pathophysologic mechanism proposed for intoxication with these agents, suggest hypoinsulinemia as the determinant factor. We will describe the case of a 77 years old man treated for an overdose of nifedipine and atenolol who arrived at our institution with hypotension and bradycardia. After conventional therapy failed to improve the patient's hemodynamic status, hyperinsulinemia and euglycemia contributed to the improvement of the patient's neurologic and hemodynamic condition. Thus, hyperinsulinemic-euglycemic therapy was of benefit in this patient with hemodynamic compromise secondary to intoxication with calcium channel blocker not responding to conventional therapy. We will review the mechanism of action of calcium channel blocker drugs as well as the clinical presentation and treatment options for calcium channel blocker intoxication.

Alcaloides isoquinolínicos de la corteza y flores de Erythrina fusca Loureiro / Isoquinolinic alcaloids from the bark and flowers of the Erythrina fusca Loureiro

De la corteza y flores de Erythrina fusca Loureiro se aislaron los alcaloides isoquinolínicos (+) -epieritratidina y 8-(+)-oxoerisodina, los cuales fueron identificados con base en sus constantes espectroscópicas. Se determinó la actividad antimicrobiana de extractos crudos y fracciones frente a bacterias y hongos. Se evaluó la actividad farmacólogica de extractos crudos y fracciones frente a ratas tipo WISTAR