Effectiveness of different methods for the extraction of principle actives and phytochemicals content in medicinal herbals / Efectividad de diferentes métodos para la extracción de principios activos y contenido de fitoquímicos en hierbas medicinales

In this present study, we investigated the influence of various extraction methods including maceration, sonication, infusion, decoction, and microwave extraction, on the chemical and biological potential of phytochemicals extracted from three medicinal plants (Ageratum conyzoides, Plantago majorand Arctium lappa L). The results were subsequently analyzed by variance analysis. Our results suggested that sonication is the most effective extraction method among the five methods tested herein, for the extraction of phytochemicals that have a high antioxidant potential and high phenolic content. The three plants employed for this study had a high concentration of flavonoids and phenolics which was compatible with the chemosystematics of the species. All the samples possessed a Sun Protection Factor (SPF) of less than 6. Interestingly, a maximum reaction time of approximately 20 min was noted for the complexation of AlCl3 with the flavonoids present in the phytochemical extract during analyses of the kinetic parameters. We finally identified that the Ageratum conyzoides extract, prepared by sonication, possessed a significant pharmacological potential against hepatocarcinoma tumour cells, whose result can guide further studies for its therapeutic efficacy.

En el presente estudio, investigamos la influencia de varios métodos de extracción, incluyendo maceración, sonicación, infusión, decocción y extracción por microondas, sobre el potencial químico y biológico de los fitoquímicos extraídos de tres plantas medicinales (Ageratum conyzoides, Plantago majory Arctium lappa L). Los resultados se analizaron posteriormente mediante análisis de varianza. Nuestros resultados sugieren que la sonicación es el método de extracción más eficaz entre los cinco métodos aquí probados, para la extracción de fitoquímicos que tienen un alto potencial antioxidante y un alto contenido fenólico. Las tres plantas empleadas para este estudio tenían una alta concentración de flavonoides y fenólicos que era compatible con la quimiosistemática de las especies. Todas las muestras poseían un factor de protección solar (SPF) menor a 6. Curiosamente, se observó un tiempo máximo de reacción de aproximadamente 20 min para la complejación de AlCl3con los flavonoides presentes en el extracto fitoquímico durante los análisis de los parámetros cinéticos. Finalmente, identificamos que el extracto de Ageratum conyzoides, elaborado por sonicación, posee un importante potencial farmacológico frente a las células tumorales del hepatocarcinoma, cuyo resultado puede orientar nuevos estudios sobre su eficacia terapéutica.

Phenolic profile and antioxidant activity from peels and seeds of melon (Cucumis melo L. var. reticulatus) and their antiproliferative effect in cancer cells

Melon (Cucumis melo L.) has high economic value and in recent years, its production has increased; however, part of the fruit is wasted. Usually, inedible parts such as peel and seeds are discarded during processing and consumption. Extracts of melon residues were prepared and their phenolic compounds, antioxidants and antiproliferative activities were evaluated. Total phenolic compounds were found in hydroethanolic, hydromethanolic, and aqueous extracts, especially for melon peel (1.016 mg gallic acid equivalent/100 g). Flavonoids total content found for melon peel aqueous extract was 262 µg of catechin equivalent (CA)/100 g. In all extracts of melon peel significant amounts of gallic acid, catechin, and eugenol were found. For total antioxidant capacity, reported as ascorbic acid equivalent, the hydroethanolic and hydromethanolic extracts in peels and hydromethanolic in seeds were 89, 74, and 83 mg/g, respectively. Different extracts of melon showed iron and copper ions chelating activity at different concentrations, especially melon peel aqueous extract, reaching values of 61% for iron and 84% for copper. The hydroethanolic extract of melon peel presented a significant ability for hydroxyl radicals scavenging (68%). To assess the antiproliferative potential in human cancer cell lines, such as kidney carcinoma, colorectal carcinoma, cervical adenocarcinoma and cervical carcinoma, MTT assay was performed. The proliferation was inhibited by 20-85% at extracts concentrations of 0.1-1.0 mg/mL in all cancer cell lines. The results suggest that melon residues extracts display a high antioxidant activity in in vitro assays and have effective biological activity against the growth of human tumor cells.

Special metabolites isolated from Urochloa humidicola (Poaceae)

ABSTRACT This study aims to identify special metabolites in polar extracts from Urochloa humidicola (synonym Brachiaria humidicola) that have allelopathic effects and induce secondary photosensitization in ruminants. The compounds were isolated and identified via chromatographic and spectroscopic techniques. The compounds 4-hydroxy-3-methoxy-benzoic acid, trans-4-hydroxycinnamic acid, and p-hydroxy-benzoic acid; the flavonols isorhamnetin-3-O-β-d-glucopyranoside and methyl quercetin-3-O-β-d-glucuronate; and kaempferitrin, quercetin-3-O-α-l-rhamnopyranoside, and tricin were identified in the extract from the leaves of Urochloa humidicola. Two furostanic saponins, namely, dioscin and 3-O-α-l-rhamnopyranosyl-(1-4)-[α-l-rhamnopyranosyl-(1-2)]-β-d-glucopyranosyl-penogenin, as well as catechin-7-O-β-d-glucopyranoside were identified in the methanolic extract obtained from the roots of this plant. This species features a range of metabolites that may be toxic for animals if used in food and may interfere with the growth medium, thereby inhibiting the development of other species.

Tridax procumbens flavonoids: a prospective bioactive compound increased osteoblast differentiation and trabecular bone formation

BACKGROUND: The Tridax procumbens extracts (TPE) are known for their ethno-medicinal properties to increase osteogenic functioning in mesenchymal stem cells. Recently, we found that the T. procumbens flavonoids (TPF) significantly suppressed the RANKL-induced osteoclasts differentiation and bone resorption. The TPF also promoted osteoblasts differentiation and bone formation demonstrated by increasing bone formation markers in cultured mouse primary osteoblasts. However, the effects of the TPF on in vivo bone formation remain unclear. In this study, we investigated the effects of the TPF on in vivo bone formation, injected the TPF (20 mg/kg) twice a day in the low calcium diet mice and killed them after 21 day. Radiographic and histomorphometric analyses were performed on the dissected bones to determine the anabolic effects of the TPF. RESULTS: Bone mineral density and bone mineral content of the TPF-treated mice were significantly increased compared to the control mice. Bone formation-related indices like osteoblast number, osteoblast surface, bone volume, mineralizing surface, mineral apposition rate and bone formation rate were significantly increased in the TPF-treated mice compared to the control mice. CONCLUSION: Our findings point towards the stimulation of bone formation by TPF, suggested that the TPF could be a potential natural anabolic agent to treat patients with bone loss-associated diseases such as osteoporosis.

Sandfly (Diptera: Psychodidae: Phlebotominae) species diversity in an urban area of the municipality of Tapachula, Chiapas, Mexico

Monitoring phlebotomine sandflies in urban areas is key for epidemiological studies in susceptible populations. This paper describes sandfly fauna that were present in an urban area of the municipality of Tapachula, Chiapas, Mexico, and were captured with Shannon and CDC light traps. During February and March of 2014, 1,442 sandflies were captured, specifically Lutzomyia cruciata (Coquillet) (98.8%), Lutzomyia cayennensis cayennensis (Floch and Abonnenc) (0.8%), Lutzomyia chiapanensis (Dampf) (0.3%) and Lutzomyia atulapai (De León) (0.1%). Lu. cruciata was the most abundant and the most frequently trapped species. This is the first record of its remarkable ability to adapt to urban green areas. The three other species trapped represent new records of geographic distribution for the study region. These results indicate the need to establish measures for reducing both human contact with this vector and the risk of possible sites of infection.

Flavonoids isolated from Tridax procumbens (TPF) inhibit osteoclasts differentiation and bone resorption

BACKGROUND: The Tridax procumbens flavonoids (TPF), are well known for their medicinal properties among local natives. The TPF are traditionally used for dropsy, anaemia, arthritis, gout, asthma, ulcer, piles, and urinary problems. It also used in treating gastric problems, body pain, and rheumatic pains of joints. The TPF have been reported to increase osteogenic functioning in mesenchymal stem cells. However, their effects on osteoclastogenesis remain unclear. The TPF isolated from T. procumbens and investigated the effects of the TPF inhibit on osteoclast differentiation and bone resorption activities using primary osteoclastic cells. Osteoclast formation was assessed by counting the number of tartrate resistant acid phosphatase (TRAP) positive multinucleated cells and by measuring both TRAP activities. RESULTS: The TPF significantly suppressed the RANKL-induced differentiation of osteoclasts and the formation of pits in primary osteoclastic cells. The TPF also decreased the expression of mRNAs related to osteoclast differentiation, including Trap, Cathepsin K, Mmp-9, and Mmp-13 in primary osteoclastic cells. The treatment of primary osteoclastic cells with the TPF decreased Cathepsin K, Mmp-9, and Mmp-13 proteins expression in primary osteoclastic cells. CONCLUSION: These results indicated that TPF inhibit osteoclastogenesis and pits formation activities. Our results suggest that the TPF could be a potential anti-bone resorptic agent to treat patients with bone loss-associated diseases such as osteoporosis.

Investigations of anticholinestrase and antioxidant potentials of methanolic extract, subsequent fractions, crude saponins and flavonoids isolated from Isodon rugosus

BACKGROUND: Based on the ethnomedicinal uses and the effective outcomes of natural products in various diseases, this study was designed to evaluate Isodon rugosus as possible remedy in oxidative stress, alzheimer's and other neurodegenerative diseases. Acetylecholinestrase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of crude methanolic extract (Ir.Cr), resultant fractions (n-hexane (Ir.Hex), chloroform (Ir.Cf), ethyl acetate (Ir.EtAc), aqueous (Ir.Aq)), flavonoids (Ir.Flv) and crude saponins (Ir.Sp) of I. rugosus were investigated using Ellman's spectrophotometric method. Antioxidant potential of I. rugosus was determined using DPPH, H2O2 and ABTS free radicals scavenging assays. Total phenolic and flavonoids contents of plant extracts were determined and expressed in mg GAE/g dry weight and mg RTE/g of dry sample respectively. RESULTS: Among different fractions Ir.Flv and Ir.Cf exhibited highest inhibitory activity against AChE (87.44 ± 0.51, 83.73 ± 0.64%) and BChE (82.53 ± 0.71, 88.55 ± 0.77%) enzymes at 1 mg/ml with IC50 values of 45, 50 for AChE and 40, 70 µg/ml for BChE respectively. Activity of these fractions were comparable to galanthamine causing 96.00 ± 0.30 and 88.61 ± 0.43% inhibition of AChE and BChE at 1 mg/ml concentration with IC50 values of 20 and 47 µg/ml respectively. In antioxidant assays, Ir.Flv, Ir.Cf, and Ir.EtAc demonstrated highest radicals scavenging activities in DPPH and H2O2 assays which were comparable to ascorbic acid. Ir.Flv was found most potent with IC50 of 19 and 24 µg/ml against DPPH and H2O2 radicals respectively. Whereas antioxidant activates of plant samples against ABTS free radicals was moderate. Ir.Cf, Ir.EtAc and Ir.Cr showed high phenolic and flavonoid contents and concentrations of these compounds in different fractions correlated well to their antioxidant and anticholinestrase activities. CONCLUSION: It may be inferred from the current investigations that the Ir.Sp, Ir.Flv and various fractions of I. rugosus are good sources of anticholinesterase and antioxidant compounds. Different fractions can be subjected to activity guided isolation of bioactive compounds effective in neurological disorders.

In Vitro Trypanocidal Activity of Macela (Achyrocline satureioides) Extracts against Trypanosoma evansi

The aim of this study was to verify the trypanocidal effectiveness of aqueous, methanolic, and ethanolic extracts of Achyrocline satureioides against Trypanosoma evansi in vitro. A. satureioides extracts, known as macela, were used on trypomastigotes at different concentrations (1, 5, 10, 50, 100, 500, and 1,000 microg/ml) and exposure times (0, 1, 3, 6, and 9 hr). A dose-dependent effect was observed when the 3 extracts were tested. The concentrations of 1, 5, and 10 microg/ml were not able to kill trypomastigotes until 3 hr after exposure, and the highest concentrations (500 and 1,000 microg/ml) were able to kill all trypomastigotes after 1 hr. When the time of exposure was increased up to 9 hr, the concentrations at 50 and 100 microg/ml were 100% effective to 3 extracts. The chemical analysis of the extracts revealed the presence of flavonoids, a trypanocidal compound already described. Based on the results, we can conclude that the A. satureioides extracts exhibit trypanocidal effects.

Anti-carcinogenic potential of Euphorbia neriifolia leaves and isolated flavonoid against N-Nitrosodiethylamine-induced renal carcinogenesis in mice.

Anti-carcinogenic potential of hydro-ethanolic extract of Euphorbia neriifolia (EN) leaves and an isolated flavonoid (ENF) was investigated against N-Nitrosodiethylamine (DENA)-induced renal carcinogenesis in mice. Experimental mice were pretreated with 150 and 400 mg/kg body wt of EN, 0.5% and 1% mg/kg body wt of butylated hydroxylanisole (BHA) as a standard antioxidant and 50 mg/kg body wt of ENF for 21 days prior to the administration of a single dose of 50 mg/kg body wt of DENA. Levels of renal markers (urea and creatinine), xenobiotic metabolic enzymes (Cyt P450 and Cyt b5), lipid peroxidation (LPO), antioxidants (SOD, CAT, GST and GSH) and other biochemical parameters — AST, ALT, ALP, total protein (TP), and total cholesterol (TC) were measured to determine the renal carcinogenesis caused by DENA. DENA administration significantly (p<0.001) decreased the body weight and increased the tissue weight. It significantly (p<0.001) enhanced the levels of Cyt P450, Cyt b5 and LPO and decreased the levels of SOD, CAT, GST and GSH content. The activities of AST, ALT and ALP and the TP content and renal markers were also significantly decreased (p<0.001), while TC level was markedly increased after DENA administration, as compared with the normal control group (p<0.001). Pretreatment with EN and ENF counteracted DENA-induced oxidative stress (LPO) and exerted its protective effects by restoring the levels of antioxidants (SOD, CAT, GST and GSH), biochemical parameters (AST, ALT, ALP, TP and TC), renal markers (urea and creatinine) and xenobiotic enzymes (Cyt P450 and Cyt b5) in renal tissue. In conclusion, the present study showed significant anti-carcinogenic potential of the hydro-ethanolic extract of E. neriifolia and ENF against DENA-induced renal carcinogenicity.

In vivo Anti-fatigue activity of total flavonoids from sweet potato [Ipomoea batatas (L.) Lam.] leaf in mice.

The in vivo anti-fatigue activity of the total flavonoids from sweet potato [Ipomoea batatas (L.) Lam.] leaf was investigated in male Kunming mice. The total flavonoids from sweet potato leaf (TFSL) were orally administered at doses of 50, 100 and 200 mg/kg for 4 weeks and the anti-fatigue effect was studied using a weight-loaded swimming test, along with the determination of serum urea nitrogen (SUN), blood lactic acid (BLA) and hepatic and muscle glycogen contents. The results showed that TFSL had significant anti-fatigue effects. TFSL extended the exhaustive swimming time, effectively inhibited the increase of BLA, decreased the level of SUN and increased the hepatic and muscle glycogen content of mice. Thus, TFSL may have potential as an anti-fatigue agent.

Antibacterial activity of flavonoid 5.7.4’-trimethoxyflavone isolated from Praxelis clematides R.M. King & Robinson / Actividad antibacterial del flavonoide 5.7.4’-trimetoxiflavona aislada dePrexelis clematides R.M. King & Robinson

The flavonoids are a large class of polyphenolic compounds found in plants that are known to exhibit biological effects. In the study, the flavonoid 5.7.4’-trimethoxyflavone (TMF) extracted from Praxelis clematidea was evaluated for its antibacterial activity. Microdilution method was used for antibacterial assay of the flavonoid and eleven bacteria strains were used in the study for activities. The results were also compared with the standard drug, Chloramphenicol (100 ug/mL). The results obtained showed activity of the flavonoid against Gram positive and Gram negative bacteria.

Los flavonoides son una clase importante de compuestos polifenólicos encontrados en las plantas que se sabe que presentan efectos biológicos. En el estudio, el flavonoide 5.7.4 '-trimethoxyflavone (TMF) extraído de Praxelis clematidea fue evaluado por su actividad antibacteriana. Se utilizó el método de microdilución para el ensayo antibacteriano del flavonoide y once cepas de bacterias se usaron en el estudio de las actividades. Los resultados se compararon también con el fármaco estándar, Cloranfenicol (100 ug/mL). Los resultados obtenidos mostraron actividad del flavonoide contra bacterias Gram positivas y Gram negativas.

Butein imparts free radical scavenging, anti-oxidative and pro-apoptotic properties in the flower extracts of Butea monosperma

The flower of Butea monosperma (Lam.) (Fabaceae) has been used in traditional Indian medicine in the treatment of many ailments including liver disorders. To understand the pharmacological basis of its beneficial effects, the extracts of dried flowers in water, methanol, butanol, ethyl acetate and acetone were evaluated for free radical scavenging and pro-apoptotic activities in cell cultures (human hepatoma Huh-7 cell line and immortalized AML-12 mouse hepatocytes). Butrin and butein -the active constituents of flower extracts- were used as reference molecules. The levels of cell injury markers like lactate dehydrogenase, glutathione and lipid peroxidation and primary antioxidant enzymes glutathione S-transferase and catalase were also measured. The aqueous and butanolic extracts exhibited better 2,2-diphenyl-1-picrylhydrazyl scavenging and cytotoxic activities in hepatoma cells than in immortalized hepatocytes. Interestingly, butein inhibited 2,2-diphenyl-1-picrylhydrazyl radical better than butrin. The aqueous and butanolic extracts were further investigated for hepatoprotection against carbon tertrachloride-induced biochemical changes and cell death. Both extracts, just as butrin and butein, significantly reversed the cellular glutathione levels and lipid peroxidation, and glutathione-S-transferase activity. Lactate dehydrogenase leakage and cell death were also prevented. However, only butein revived the catalase activity. Thus, the butein content of Butea monosperma flower extracts is important for free radical scavenging activity, apoptotic cell death and protection against oxidative injury in hepatic cells.

Antiviral activity in vitro and in vivo of natural flavonoids isolated from Heliotropium sinuatum against infectious salmon anemia virus (ISAV) / Actividad antiviral in vitro e in vivo de flavonoides naturales aislados desde Heliotropium sinuatum contra el virus de la anemia infecciosa en salmones (ISAV)

The infectious salmon anemia virus (ISAV) of Orthomyxoviridae family, is responsible for heavy losses in industry aquaculture around the world, affecting several commercial aquatic organisms, mainly Salmo salar. Therefore, it is important to find effective antiviral therapies. In this work we evaluated in vitro and in vivo the antiviral activity of three natural flavonoids isolated from the resinous exudates of the plant Heliotropium sinuatum (Heliotropiaceae) against ISAV. The results show that 7-O-methyleriodictyol was able to inhibit the infectivity of ISAV in vitro assay with EC 50 of 0.20 ug/mL. Despite having a citotoxicity expressed as CC50 of 12.80 ug/mL, the in vivo study showed that this compound protected 100 percent to the fish infected with ISAV keeping 100 percent fish viability. These results allow the proposal of 7-O-methyleriodictyol as a good candidate to be used as antiviral therapy for ISAV in salmon industry.

El virus de la anemia infecciosa en salmón de la familia Orthomyxoviridae, es el responsable de grandes pérdidas en la industria acuícola alrededor del mundo, afectando diversas especies acuáticas comerciales, principalmente Salmo salar. Por lo tanto, es muy importante encontrar una terapia antiviral efectiva. En el presente trabajo, evaluamos la actividad antiviral in vitro e in vivo de tres flavonoides naturales aislados desde el exudado resinoso de la especie vegetal Heliotropium sinuatum (Heliotropiaceae) contra ISAV. Los resultados mostraron que 7-O-metileriodictiol inhibió la infectividad de ISAV in vitro con un EC50 de 0.20 ug/mL. A pesar de tener una citotoxicidad expresada como un CC50 de 12.80 ug/mL, el estudio in vivo mostró que este compuesto protege en un 100 por ciento a los peces infectados con ISAV manteniendo un 100 por ciento de viabilidad. Estos resultados permiten proponer que 7-O-metileriodictiol es un buen candidato para ser usado como terapia antiviral para ISAV en la industria salmonera.

Efecto antioxidante y contenido polifenólico de Syringodium filiforme (Cymodoceaceae)

Antioxidant effect and polyphenol content of Syringodium filiforme (Cymodoceaceae). The marine phanerogam Syringodium filiforme, known as "manatee grass", is a common species that grows in coastal areas associated to Thalassia testudinum. With the aim to describe some of its possible chemical characteristics, this study was performed with a sample of 1.2kg, collected in March 2009, in Guanabo beach, Havana, Cuba. The sample was dried (less than 12% humidity) and a total extract prepared; other three extracts were prepared with the use of solvents of increasing polarity. The phytochemical screening and analytical determinations of each fraction were undertaken Total polyphenol content was determined using pyrogallol as reference´s standard; chlorophyll a and b and anthocyanin content were also quantified. Total extract and fractions antioxidant activity were evaluated by using the free radical scavenging activity assay with 1,1- Diphenyl-2-Picrylhydrazyl reactive (knowing as DPPH´s method). The phytochemical screening of the different extracts detected the presence of high concentrations of flavonoids, phenols, terpenes, antocyaninns, reducing sugars and alkaloids. The total extract and methanol fraction showed significant free radical scavenging properties, while the petroleum ether fraction showed moderate activity, and the chloroform fraction and the aqueous soluble precipitate (residual salt) obtained didn’t show antioxidant properties against free radicals. The results of this work confirmed the potentialities of this species for biological purposes. Rev. Biol. Trop. 59 (1): 465-472. Epub 2011 March 01.

La fanerógama marina Syringodium filiforme, conocida comúnmente como "Hierba Manatí", crece en los fondos marinos tropicales asociada con la especie Thalassia testudinum. Este estudio fue realizado con una muestra de S. filiforme (1.2kg peso húmedo) recolectada en la playa de Guanabo en La Habana, Cuba en Marzo 2009. La muestra fue secada hasta humedad inferior al 12% y se realizaron tres extracciones con solventes de polaridad creciente previamente al tamizaje fitoquímico y a las determinaciones analíticas. A partir del extracto total y en las fracciones se detectó la presencia de grupos químicos, fundamentalmente estructuras típicas de los flavonoides, por las absorbancias obtenidas en los espectros ultravioleta-visible. En el tamizaje fitoquímico se corroboró la existencia de altas concentraciones de flavonoides, triterpenos, polifenoles, antocianinas, azúcares reductores y alcaloides en los diferentes extractos obtenidos. El contenido de polifenoles totales de S. filiforme, se cuantificó mediante el uso de pirogalol como patrón de referencia; así como el contenido de clorofilas a y b, y el nivel de antocianinas. La actividad antioxidante se determinó por el método reducción del 1,1-difenil-2-picrilhidrazilo (DPPH). El extracto total y la fracción metanólica mostraron elevada actividad antioxidante en correspondencia con la concentración de polifenoles, mientras que la fracción de éter de petróleo mostró actividad moderada y la fracción clorofórmica y el precipitado remanente no muestran actividad antioxidante significativa. Estos resultados predicen las potencialidades de la especie para su uso con fines biológicos.

Alpinum isoflavone from Erythrina stricta Roxb / Alpinum isoflavona de Erythrina stricta Roxb

Alpinum isoflavone was isolated from the n-hexane extract of stem bark of Erythrina stricta. The structure of the compound was elucidated by extensive spectroscopic studies and comparision with published spectroscopic data.

A partir de un extracto, obtenido con n-hexano de corteza de Erythrina stricta, se aisló la alpinum isoflavona. La estructura del compuesto fue determinada por métodos espectroscópicos y comparación con datos espectroscópicos publicados.

Flavonoids of enhydra fluctuans exhibits analgesic and anti-inflammatory activity in different animal models

Enhydra fluctuans [Compositae], an edible semi aquatic herbaceous vegetable plant, widely used in traditional system of Indian medicine. Total flavonoids of E. fluctuans [TFEF] were screened for analgesic and anti-inflammatory activity. Analgesic activity was studied in acetic acid induced writhing response and by hot plate method in Swiss albino mice. Anti-inflammatory activity was estimated by carrageenan and histamine induced acute inflammation and Freund's complete adjuvant [FCA] induced chronic inflammation in rats. Two flavonoids, baicalein 7-O-glucoside and baicalein 7-O-diglucoside, were isolated from the ethyl acetate fraction. Oral administration of TFEF at the doses of 200 and 400 mg/kg provide 27.05 and 55.49% protection respectively in acetic acid induced writhing method. It also increased the pain threshold in mice evidenced by hot plate method. TFEF showed more potent anti-inflammatory activity. The results of this study may be attributed to high free radical scavenging and antioxidant potential of the flavonoids present in ethyl acetate fraction of Enhydra fluctuans

Effects of extracts, flavonoids and iridoids from Penstemon gentianoides (Plantaginaceae) on inhibition of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) in LPS-Activated RAW 264.7 macrophage cells and their antioxidant activity / Efectos de extractos, flavonoides e iridoides de Penstemon gentianoides (Plantaginaceae) sobre la inhibición de oxido nitrico sintasa inducible (iNOS), ciclooxigenasa-2 (COX-2) celulas de macrofagos murinos RAW 264.7 activadas con LPS y sus actividades antioxidantes

Penstemon gentianoides (HBK) (Kunth) Poir (Plantaginaceae) is an evergreen shrub that grows the throughout high mountains from Guatemala, Mexico and Southern states of US. Its leaves and roots have been used therapeutically for inflammation-related conditions from Aztec times, but systematic studies of its anti-inflammatory activity are lacking and no specific active components have been identified. In this study, methanol, n-hexane, CH2Cl2, ethyl acetate and methanol/water (6:4) extracts, luteolin, diosmetin, verbascoside, martynoside, pensteminoside, globularisicin and plantarenaloside isolated from this plant were evaluated by determining their inhibitory effects on the production of proinflammatory mediators in lipopolysaccharide (LPS)-activated RAW 264.7 murine macrophage cells. Ethyl acetate extract, luteolin, and diosmetin exhibited potent anti-inflammatory and antioxidant activities. The results indicated that luteolin and diosmetin suppressed the LPS induced production of nitric oxide (NO), through the down-regulation of inducible nitric oxide synthases (iNOS) and cyclo-oxygenase 2 (COX-2) protein expressions and showed a potent antioxidant activity against DPPH, TBARS and DCFH. The inhibition of enzymes and NO production by selected extracts and compounds was dose-dependent with significant effects seen at concentration as low as 50 ìM. Thus, luteolin and diosmetin may provide a potential therapeutic approach for inflammation associated disorders.

Penstemon gentianoides (HBK) (Kunth) Poir (Plantaginaceae) es un arbusto perenne que crece a lo largo de las montañas altas de Guatemala, México y los estados del sur de los EE.UU.. Sus hojas y raíces se han utilizado terapéuticamente para afecciones relacionadas con inflamación desde la época de los aztecas, pero no existen estudios sistemáticos de su actividad anti-inflamatoria y ninguno de los metabolitos activos específicos han sido identificados. En este estudio, los extractos de metanol, n-hexano, CH2Cl2, acetato de etilo y metanol/agua (6:4), junto con, luteolina, diosmetina, verbascósido, martynoside, pensteminoside, globularisicin y plantarenaloside, aislados desde esta planta se evaluaron mediante la determinación de sus efectos inhibitorios sobre la producción de mediadores proinflamatorios en macrófagos murinos activados con lipopolisacárido (LPS)-RAW 264,7. El extracto de acetato de etilo, luteolina y diosmetina exhibieron una potente actividad anti-inflamatoria y antioxidante. Los resultados indican que luteolina y diosmetina suprimen la producción de óxido nítrico (NO), a través de la regulación de óxido nítrico sintasa-inducible (iNOS) y la ciclooxigenasa-2 (COX-2) ambas expresiones de proteínas. Ademas mostró una potente actividad antioxidante contra DPPH, TBARS y DCFH. La inhibición de las enzimas y la producción de NO por los extractos seleccionados y compuestos es dependiente de la dosis con efectos significativos visto en una concentración tan baja como 50 mM. Por lo tanto, luteolina y diosmetina puede proporcionar un enfoque terapéutico potencial para transtornos asociados a los procesos de inflamación.

Compuestos fenólicos presentes en las hojas de la especie colombiana Polygonum segetum Kunth / Fenolic compounds in the leaves of Polygonum segetum Kunth

The flavonoids 5-hydroxy-7,8,4'-trimethoxy isoflavone and 5,3',4'-trihydroxy-7-methoxyflavanon ,the tannin derivate Ethyl gallate and lignang homoegonol 5-(3''-Hydroxypropyl)-7-methoxy-2-(3',4'-dimethoxyphenyl)benzofuran were isolated and purified from Polygonum segetum Kunth leaves using column chromatography and thin layer chromatography methods. These substances were identified on the basis of their physical properties (melting point and Rf value), qualitative chemical reactions and spectroscopic techniques UV and NMR (experiments 1H, 13C, 1H-1H COSY, HMQC) and spectrometric techniques GC-MS according to their complexity.

El presente estudio se encaminó a determinar los metabolitos secundarios presentes en las hojas de la especie vegetal: Polygonum segetum Kunth, colectada del humedal Juan Amarillo (Bogotá-Colombia). Como resultado se aislaron e identificaron a partir de propiedades físicas y técnicas espectroscópicas de UV, 1HRMN, COSY, DEPT 135, HMQC y APT, la 5-hidróxi-7,8,4´-trimétoxi isoflavona, el galato de etilo (derivado de taninos) y la 5,3´,4´-trihidróxi-7-metóxi flavanona. Además, por análisis GC-MS se identifico el lignano 5-(3,4-dimetóxifenil)-7-metóxibenzofuranpropanol homoegonol.

Effect of Scutellaria flavonoids on KCN-induced damages in rat pheochromocytoma PC12 cells.

BACKGROUND & OBJECTIVE: Cerebral hypoxia is known to be involved in many neurodegenerative diseases such as Alzheimer's and cerebrovascular dementia. The present study was designed to investigate the effects of flavonoids from aerial part of Scutellaria baicalensis Georgi (SSF) on potassium cyanide (KCN) -induced hypoxic cytotoxicity in rat pheochromocytoma cell line PC12, and to understand the probable mechanism. METHODS: The rat pheochromocytoma cell line PC12 was subjected to hypoxia by 200 microM KCN for 30 min. The cytotoxicity of KCN was assessed by cell viability assay, morphological observation, lactate dehydrogenase (LDH) release, malondialdehyde (MDA) production, and the activities of superoxide dismutase (SOD) and Na+-K+-ATPase measurements. The effects of SSF on the changes induced by KCN in PC12 cells were detected. RESULTS: Treatment of PC12 cells with 200 micriM KCN for 30 min increased cell death when compared with control, as assayed by MTT reduction, morphological observation and lactate dehydrogenase release measurement. These cell lesions were accompanied by disorders in SOD and Na+-K+-ATPase activities as well as MDA production. In contrast, the PC12 cells pre-treated with SSF for 24 h prior to 200 microM KCN exposure have shown protection against hypoxic toxicity. The KCN - induced decreased cell viability and activities of SOD and Na+-K+-ATPase, as well as increased MDA production were reversed by SSF pre-treatment. INTERPRETATION & CONCLUSION: SSF exerted neuroprotections against KCN - induced hypoxic cytotoxicity in PC12 cells and the probable mechanisms involved free radicals and energy metabolism. Our findings may have implications in future in the treatment of neurodegenerative diseases.

Flavonoids, benzophenones and a new euphane derivative from Clusia columnaris Engl / Flavonóides, benzofenonas e um novo eufano de Clusia columnaris Engl

The polyisoprenylated benzophenones machuone and clusiachromene A have been isolated from the fruits of Clusia columnaris. The hexane extract of the young branches with leaves afforded a new euphane derivative, whose structure was elucidated by spectroscopic methods. On the contrary, the most polar EtOAc and ButOH extracts were constituted of flavonoid C-glucosides (isovitexin, vitexin and vitexin-2"-xyloside) and seven biflavonoids of the so-called Garcinia group.

Dos frutos de Clusia columnaris foram isoladas as benzofenonas poliisopreniladas machuona e clusiacromeno A. Do extrato em hexano obtido de galhos e folhas novas, um novo triterpeno do tipo eufano foi isolado. Sua estrutura foi elucidada através de métodos espectroscópicos. Por outro lado, dos extratos mais polares - em acetato de etila e em butanol, foram isolados os flavonóides C-glicosilados isovitexina, vitexina e vitexina-2"-xilosídeo, além de sete bisflavonóides conhecidos como bisflavonóides do grupo da Garcinia.