Optimization of ultrasound - assisted extraction of phenolic compounds and flavonoids from Hortia oreadica leaf / Optimización de la extracción asistida por ultrasonido de compuestos fenólicos y flavonoides de la hoja de Hortia oreadica

Hortia oreadica is indiscriminated used by people from Cerrado. However, vegetable raw material quality is decisive in obtaining inter mediate and final products. So, this study aimed to establish quality parameters of H. oreadica . For this, we performed the phytochemical screening of H. oreadica leaf and identified the best extractive conditions for phenolic compounds and flavonoids usin g factorial experimental design, varying the alcoholic strength, extraction temperature, and solid/liquid ratio in the ultrasound - assisted extraction method. The optimum extraction condition for phenolic compounds and flavonoids was 60% alcoholic strength, 40°C temperature, and a solid/liquid ratio of 8 mg/m L . Under this setting, the phenolic and flavonoid contents were 0.171 ± 0.002 mg/m L (predicted value = 0.165) and 0.087 ± 0.002 mg/m L (predicted value = 0.084), respectively. The optimized extraction par ameters could be upscaled to develop pharmaceutical drugs or nutraceutical products from this non - traditional plant species using an eco - friendly approach.

Hortia oreadica es utilizada indiscriminadamente por la gente del Cerrado. Sin embargo, la calidad de la materia prima vegetal es determinante en la obtención de productos intermedios y finales. Por lo tanto, este estudio tuvo como objetivo establecer parámetros de calidad de H. oreadica . Para ello, realizamos el tamizaje fitoquímico de la hoja de H. oreadica e identificamos las mejores condiciones extractivas para compuestos fenólicos y flavonoides mediante un diseño experimental factorial, variando el grado alcohólico, la temperatura de extracción y la relación sólido/líquido en el método de extracción asistido por ultrasonido. La condición óptima de extracción para compuestos fenólicos y flavonoides fue de 60% de grado alcohólico, 40°C de t emperatura y una relación sólido/líquido de 8 mg/m L . Bajo esta configuración, los contenidos de fenoles y flavonoides fueron 0,171 ± 0,002 mg/m L (valor previsto = 0,165) y 0,087 ± 0,002 mg/m L (valor previsto = 0,084), respectivamente. Los parámetros de ext racción optimizados podrían ampliarse para desarrollar fármacos o productos nutracéuticos a partir de esta especie de planta no tradicional uti lizando un enfoque ecológico .

Six new coumarins from the roots of Toddalia asiatica and their anti-inflammatory activities / 中国天然药物

We reported the discovery of six novel coumarins, toddasirins A-F (1-6), each endowed with modified isoprenyl or geranyl side chains, derived from the roots of Toddalia asiatica. Comprehensive structural elucidation was achieved through multispectroscopic analyses, single-crystal X-ray diffraction experiments, and advanced quantum mechanical electronic circular dichroism (ECD) calculations. Furthermore, the anti-inflammatory activity of these compounds was assessed. Notably, compounds 1-3 and 6 demonstrated notable inhibitory effects on nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW 264.7 cells, with 50% inhibitory concentration (IC50) values of 3.22, 4.78, 8.90, and 4.31 μmol·L-1, respectively.

Physiochemical and nutritional evaluation of whole kumquat fruits powder and its protective effect on thyroid hormones and blood sugar levels in diabetic rats / Avaliação físico-química e nutricional de frutas inteiras de kumquat em pó e seu efeito protetor sobre os hormônios da tireoide e os níveis de açúcar no sangue em ratos diabéticos

The present study was conducted to evaluate the chemical composition, antioxidant activity and hypoglycemic effects of whole kumquat (Ku) powder in diabetic rats fed a high-fat-high-cholesterol (HFHC) diet. The antioxidant activities were evaluated using stable 1,1-diphenyl 2-picrylhydrazyl (DPPH) free radical scavenging method, 2,2'-azinobis (3-ethyl benzo thiazoline-6-sulphonic acid) radical cation (ABTS) and Ferric reducing antioxidant power (FRAP). Total phenolic content was (51.85 mg GAE/g) and total flavonoid content was (0.24 mg Cateachin Equivalent, CE/g). DPPH and ABTS values were 3.32 and 3.98 mg Trolox equivalent (TE)/g where FRAP value was 3.00 mM Fe²+/kg dry material. A total of 90 albino rats were used in the present study. Rats group were as follows: normal diet; normal treated (2, 4, and 6% Ku.), diabetic rats (non-treated), diabetic + HFHC diet (non-treated), HFHC (non-treated), Diabetic (treated), HFHC (treated) and Diabetic + HFHC (treated). The diets were followed for 8 weeks. Blood samples were collected at the end of the experiment. Serum glucose was recorded and thyroid hormones (T4, Thyroxine and T3, Triiodothyronine) were conducted. Diet supplemented with Kumquat at different concentrations have a hypoglycemic effect and improve the thyroid hormones of both diabetic rats and HFHC diabetic rats.

O presente estudo foi conduzido para avaliar a composição química, a atividade antioxidante e os efeitos hipoglicêmicos do pó de kumquat (Ku) em ratos diabéticos alimentados com uma dieta rica em gordura e colesterol (HFHC). As atividades antioxidantes foram avaliadas usando o método de eliminação de radicais livres de 1,1-difenil 2-picrilhidrazil (DPPH), 2,2'-azinobis (ácido 3-etilbenzotiazolina-6-sulfônico) radical cátion (ABTS) e antioxidante redutor férrico potência (FRAP). O conteúdo fenólico total foi (51,85 mg GAE / g) e o conteúdo total de flavonoides foi (0,24 mg Cateachin Equivalent, CE / g). Os valores de DPPH e ABTS foram 3,32 e 3,98 mg equivalente de Trolox (TE) / g, em que o valor de FRAP foi de 3,00 mM Fe²+ / kg de material seco. Um total de 90 ratos albinos foi usado no presente estudo. O grupo dos ratos foi o seguinte: dieta normal: tratados normais (2, 4 e 6% Ku.), ratos diabéticos (não tratados), diabéticos + dieta HFHC (não tratados), HFHC (não tratados), diabéticos (tratados), HFHC (tratados) e diabéticos + HFHC (tratados). As dietas foram seguidas por 8 semanas. Amostras de sangue foram coletadas ao final do experimento. A glicose sérica foi registrada e os hormônios tireoidianos (T4, Tiroxina e T3, Triiodotironina) foram conduzidos. A dieta suplementada com kumquat em diferentes concentrações tem um efeito hipoglicêmico e melhora os hormônios tireoidianos tanto de ratos diabéticos quanto de ratos diabéticos com HFHC.

Physiochemical and nutritional evaluation of whole kumquat fruits powder and its protective effect on thyroid hormones and blood sugar levels in diabetic rats / Avaliação físico-química e nutricional de frutas inteiras de kumquat em pó e seu efeito protetor sobre os hormônios da tireoide e os níveis de açúcar no sangue em ratos diabéticos

Abstract The present study was conducted to evaluate the chemical composition, antioxidant activity and hypoglycemic effects of whole kumquat (Ku) powder in diabetic rats fed a high-fat-high-cholesterol (HFHC) diet. The antioxidant activities were evaluated using stable 1,1-diphenyl 2-picrylhydrazyl (DPPH) free radical scavenging method, 2,2´-azinobis (3-ethyl benzo thiazoline-6-sulphonic acid) radical cation (ABTS) and Ferric reducing antioxidant power (FRAP). Total phenolic content was (51.85 mg GAE/g) and total flavonoid content was (0.24 mg Cateachin Equivalent, CE/g). DPPH and ABTS values were 3.32 and 3.98 mg Trolox equivalent (TE)/g where FRAP value was 3.00 mM Fe2+/kg dry material. A total of 90 albino rats were used in the present study. Rats group were as follows: normal diet; normal treated (2, 4, and 6% Ku.), diabetic rats (non-treated), diabetic + HFHC diet (non-treated), HFHC (non-treated), Diabetic (treated), HFHC (treated) and Diabetic + HFHC (treated). The diets were followed for 8 weeks. Blood samples were collected at the end of the experiment. Serum glucose was recorded and thyroid hormones (T4, Thyroxine and T3, Triiodothyronine) were conducted. Diet supplemented with Kumquat at different concentrations have a hypoglycemic effect and improve the thyroid hormones of both diabetic rats and HFHC diabetic rats.

Resumo O presente estudo foi conduzido para avaliar a composição química, a atividade antioxidante e os efeitos hipoglicêmicos do pó de kumquat (Ku) em ratos diabéticos alimentados com uma dieta rica em gordura e colesterol (HFHC). As atividades antioxidantes foram avaliadas usando o método de eliminação de radicais livres de 1,1-difenil 2-picrilhidrazil (DPPH), 2,2'-azinobis (ácido 3-etilbenzotiazolina-6-sulfônico) radical cátion (ABTS) e antioxidante redutor férrico potência (FRAP). O conteúdo fenólico total foi (51,85 mg GAE / g) e o conteúdo total de flavonoides foi (0,24 mg Cateachin Equivalent, CE / g). Os valores de DPPH e ABTS foram 3,32 e 3,98 mg equivalente de Trolox (TE) / g, em que o valor de FRAP foi de 3,00 mM Fe2 + / kg de material seco. Um total de 90 ratos albinos foi usado ​​no presente estudo. O grupo dos ratos foi o seguinte: dieta normal: tratados normais (2, 4 e 6% Ku.), ratos diabéticos (não tratados), diabéticos + dieta HFHC (não tratados), HFHC (não tratados), diabéticos (tratados), HFHC (tratados) e diabéticos + HFHC (tratados). As dietas foram seguidas por 8 semanas. Amostras de sangue foram coletadas ao final do experimento. A glicose sérica foi registrada e os hormônios tireoidianos (T4, Tiroxina e T3, Triiodotironina) foram conduzidos. A dieta suplementada com kumquat em diferentes concentrações tem um efeito hipoglicêmico e melhora os hormônios tireoidianos tanto de ratos diabéticos quanto de ratos diabéticos com HFHC.

Three new coumarins and a new coumarin glycoside from Micromelum integerrimum / 中国天然药物

Three new coumarins, integmarins A-C (1-3), and a new coumarin glycoside, integmaside A (4) were isolated from the leaves and stems of Micromelum integerrimum. Their structures were elucidated on the basis of 1D and 2D NMR and MS data, and their absolute configurations were assigned according to the ECD data of the in situ formed transition metal complexes and comparison of experimental and calculated ECD data. Compounds 1 and 2 are two rare coumarins with butyl and propyl moieties at the C-6 position; compound 3 is a novel coumarin with a highly oxidized prenyl group, and compound 4 is a rare bisdihydrofuranocoumarin glycoside.

Evaluación genotóxica de las moléculas con efectos tripanocida y leishmanicida cantin-6-ona y 5-metoxicantin-6-ona en células de médula ósea de ratones / Genotoxic evaluation of the molecules with trypanocidal and leishmanicidal effects, canthin-6-one and 5-methoxycanthin-6-one in mouse bone marrow cells

La tripanosomiasis americana y la leishmaniasis son problemas de salud pública relevantes en Iberoamérica. Las drogas utilizadas actualmente para el tratamiento de estas enfermedades poseen efectos colaterales tóxicos severos. Varios grupos de investigación están abocados a la búsqueda de productos naturales y sintéticos para encontrar nuevos agentes terapéuticos efectivos que no presenten reacciones colaterales adversas. En la evaluación de compuestos de la especie vegetal Zanthoxylum chiloperone (Rutaceae), se demostró que compuestos aislados del extracto presentaban actividad leishmanicida, tripanocida y antifúngica in vivo. Teniendo como antecedentes estos resultados, en el presente estudio se evaluaron los efectos genotóxico y citotóxico del cantín-6-ona y del 5-metoxicantin-6-ona, moléculas aisladas de la planta, en células de médula ósea de animales tratados. El estudio de los efectos genotóxicos se hizo a través del ensayo de modificaciones en la frecuencia de micronúcleos y el efecto citotóxico por modificaciones en la relación entre eritrocitos policromáticos y eritrocitos normocromáticos. Se realizaron 2 ensayos independientes y en cada ensayo los animales fueron divididos en tres grupos de tratamiento: GRUPO I: control negativo que recibió 200 uL de agua y 2.1% de DMSO, vía oral, GRUPO II: compuesto a ser evaluado (canthin-6-ona o 5-methoxicantin-6-ona) con 2.1% de DMSO, y GRUPO III: control positivo que recibió ciclofosfamida 50mg/kg/peso del animal, vía intraperitoneal. El análisis estadístico mostró que ambos compuestos no presentaron efectos genotóxicos ni citotóxicos. Estos resultados permiten proponer a estas moléculas como candidatas a ser sometidas a estudios más detallados como potenciales fármacos contra estas dos enfermedades

American trypanosomiasis and leishmaniasis are relevant public health problems in Latin America. The drugs currently used to treat these diseases have severe toxic side effects. Several research groups are dedicated to the search of natural and synthetic products to find new effective therapeutic agents that do not present adverse collateral reactions. In the evaluation of compounds of the plant species Zanthoxylum chiloperone (Rutaceae), it was shown that isolated compounds of the extract had leishmanicidal, trypanocidal and antifungal in vivo activities. Based on these results, the genotoxic and cytotoxic effects of canthin-6-one and 5-methoxycanthin-6-one, molecules isolated from the plant, on bone marrow cells of treated mice were evaluated in the present study. The study of genotoxic effects was made through the test of modifications in the frequency of micronuclei and the cytotoxic effects by modifications in the relationship between polychromatic erythrocytes and normochromic erythrocytes. Two independent assays were performed and in each assay the animals were divided into three treatment groups: GROUP I: negative control that received 200 µL of water and 2.1% of DMSO, orally, GROUP II: compound to be evaluated (canthin-6 -one or 5-methoxycanthin-6-one) with 2.1% DMSO, and GROUP III: positive control that received cyclophosphamide 50mg /kg animal weight, intraperitoneal. Statistical analysis showed that both compounds had neither genotoxic nor cytotoxic effects. These results allow these molecules to be proposed as candidates to be subjected to more detailed studies as potential drugs against these two diseases

Antioxidant and biological activities of essential oil from Colombian Swinglea glutinosa(Blanco) Merr fruit

The objectives of this work were the study of the volatile chemical composition of essential oils (EO’s) from Swinglea glutinosa, as well as to evaluate their antioxidant, repellent and fumigant properties. The EO was obtained by hydrodistillation from the peel of the fruit, gathered in the city of Cartagena, Bolívar (Colombia). The volatile composition was analyzed by gas chromatography coupled to mass spectrometry (GC-MS). The major compounds found in S. glutinosaweregermacrene D (4.8%), limonene (5.2%),-terpineol (6.5%), -pinene (8.5%), nerolidyl acetate (9.8%), and trans-nerolidol (34.6%). S. glutinosashowed antioxidant potential (85.8%) (IC50=142.49 μg mL-1). The EO deployedrepellent activity against the Tribolium castaneumweevil at a concentration of 15.73 nL cm-1at 2 hours of exposure (72%), while the result for the commercial repellent was 50% at the same concentration. EO from S. glutinosadisplayed the best fumigant activity withLC50of 153.4 μg mL-1air. The essential oil from S. glutinosacan be considerated as a natural source of biocides and antioxidants.

Phytochemical screening of extracts from Spiranthera odoratissima A. St.-Hil. (Rutaceae) leaves and their in vitroantioxidant and anti-Listeria monocytogenes activities

Spiranthera odoratissima A. St.-Hil (Rutaceae), a shrub whose common name is manacá do Cerrado in Brazilian Portuguese, is about 1-m high and has been used by folk medicine to treat stomachache, kidney and liver infections, headache, rheumatism and as a blood purifier. This study aimed at preparing hexane, ethyl acetate, methanolic, hydroethanolic and aqueous extracts from S. odoratissima leaves, at carrying out preliminary phytochemical screening and at evaluating their in vitroantioxidant and anti-Listeria monocytogenesactivities. Antioxidant activity was evaluated by the DPPH (2,2-diphenyl-1-picrylhydrazyl), ABTS (2,2-azinobis-3-ethybenzothiazoline-6-sulfonate) and FRAP (ferric reducing antioxidant power) methods. Antibacterial activity was investigated against L. monocytogenesand Minimum Inhibitory Concentration (MIC) values of plant extracts were calculated by the broth microdilution method with the use of 96-well plates. In aqueous, methanolic, hydroethanolic, ethyl acetate and hexane extracts from S. odoratissima leaves, the following classes of compounds were investigated: organic acids, reducing sugars, flavonoids, saponin compounds, coumarin compounds, phenolics, tannins, purine compounds, catechins, flavonol derivatives, sesquiterpene lactonesand anthraquinones. All plant extracts, except the hexane one, exhibited high antioxidant activity. Regarding antibacterial activity, the most polar extracts showed high activity against L. monocytogenes; their MIC values ranged between 12.5 and 62.5 μg mL-1, while the hexane one exhibited low activity (MIC = 1000 μgmL-1). In short, extracts from S. odoratissima leaves may be consideredpromising sources of secondary metabolites with relevant antioxidant and antibacterial activities.

Chemical composition and in vitro antibacterial activity of essential oils from Murraya paniculata (L. ) Jack (Rutaceae) ripe and unripe fruits against bacterial genera Mycobacterium and Streptococcus

This study aims to investigate chemical composition of essential oils from Murraya paniculata (L.) Jack (Rutaceae) ripe and unripe fruits and determine their in vitro antibacterial activity. Essential oils were extracted by hydrodistillation from Murraya paniculata (L.) Jack ripe and unripe fruits collected in the Cerrado, in Rio Verde, southwestern Goiás, Brazil. They were analyzed by gas chromatography with flame ionization detector (GC-FID) and by gas chromatography-mass spectrometry (GC-MS). Sesquiterpenes, which represent the most abundant class of compounds in oils, predominated in both ripe and unripe fruits. Major constituents of essential oils extracted from ripe fruits (RF-EO) were (-caryophyllene (21.3%), (-ylangene (13.3%), germacrene-D (10.9%) and (-zingiberene (9.7%) whereas the ones of unripe fruits (UF-EO) were sesquithujene (25.0%), (-zingiberene (18.2%), germacrene-D (13.1%) and (-copaene (12.7%). In vitro antibacterial activity of essential oils was evaluated in terms of its minimum inhibitory concentration (MIC) values by the broth microdilution method in 96-well microplates. Both essential oils under investigation showed moderate anti-streptococcal activity against the following bacteria: Streptococcus mutans, S. mitis, S. sanguinis, S. sobrinus and S. salivarius. MIC values ranged between 100 and 400 µg/mL. Regarding the antimycobacterial activity, essential oils from M. paniculata (L.) Jack unripe and ripe fruits were active against Mycobacterium kansasii (MIC = 250 µg/mL), moderately active against M. tuberculosis (MIC = 500 µg/mL) and inactive against M. avium (MIC = 2000 µg/mL). This study was pioneer in revealing similar chemical profiles of both essential oils extracted from Murraya paniculata (L.) Jack unripe and ripe fruits, besides describing their in vitro anti-streptococcal and antimycobacterial activities.

Acronyculatin P, A New Isoprenylated Acetophenone from the Stem Bark of Acronychia pedunculata

A new isoprenylated acetophenone, acronyculatin P (1) as well as two known compounds, 3′,5′-diisoprenyl-2′,4′-dihydroxy-6′-methoxyphenylethanone (2) and 3′-isoprenyl-2′,4′,6′-trihydroxyphenylethanone (3) were isolated from the stem bark of Acronychia pedunculata (L.) Miq. The structures were determined by HRESIMS, 1D and 2D NMR. The inhibitory activity of the isoprenylated acetophenone derivatives against murine leukemia P-388 cells showed compound 1 moderate activity with IC₅₀ 15.42 µM.

Meliglabrin, A New Flavonol Derivative from the leaves of Melicope glabra (Blume) T.G. Hartley

A new flavonol derivative, meliglabrin (1) along with three known flavonols, ternatin (2), meliternatin (3), and 5,4′-dihydroxy-3,7,3′-trimethoxyflavon (4) were isolated from the leaves of Melicope glabra (Blume) T.G. Hartley. Their structures were determined using extensive spectroscopic methods, including UV, IR, HRESIMS, 1D and 2D NMR. Compounds 1 – 4 were evaluated for their cytotoxicity against murine leukemia P-388 cells, compound 4 showed moderate activity.

Volatile constituents of Atalantia roxburghiana Hook. f., Tetradium trichotorum Lour. and Macclurodendron oligophlebia (Merr.) Hartl. (Rutaceae) from Vietnam / Compuestos volátiles de Atalantia roxburghiana Hook. f., Tetradium trichotorum Lour. y Macclurodendron oligophlebia (Merr.) Hartl. (Rutaceae) provenientes de Vietnam

The chemical constituents of essential oils obtained by hydrodistillation of the leaves of Atalantia roxburghiana Hook. f. and Tetradium trichotomum Lour., as well as the leaves and fruits of Macclurodendron oligophlebia (Merr.) Hartl. (Rutaceae) are being reported. The essential oils were analysed by using gas chromatography (GC) and gas chromatography coupled with mass spectrometry (GC-MS). Sabinene (36.9%) was the most singly abundant compound in the leaf of A. roxburghiana. The major constituents present in the leaf oil of T. trichotorum were (E)-ß-ocimene (24.8%), α-pinene (10.4%), (Z)-ß-ocimene (9.4%) and ß-caryophyllene (8.0%). On the other hand, while α-pinene (17.5%), ß-caryophyllene (15.5%) and caryophyllene oxide (10.6%) occurred in higher proportion in the leaf of M. oligophlebia, the fruit oil was dominated by benzyl benzoate (16.8%), (E, E)-farnesol (8.3%) and ß-caryophyllene (6.0%).

Se muestran los constituyentes químicos de los aceites esenciales obtenidos, por hidrodestilación, de las hojas de Atalantia roxburghiana Hook. f. y de Tetradium trichotomum Lour., así como de las hojas y frutos de Macclurodendron oligophlebia (Merr.) Hartl. (Rutaceae). Los aceites esenciales fueron analizados por Cromatografía de Gases (CG) y por Cromatografía de Gases acoplada a Espectrometría de Masas (CG-EM). El compuesto más abundante en las hojas de A. roxburghiana es el sabineno (36.9%); mientras que los mayoritarios en el aceite de las hojas de T. trichotomum fueron (E)-ß-ocimeno (24.8%), α-pineno (10.4%), (Z)-ß-ocimeno (9.4%) y ß- cariofileno (8.0%). En las hojas de M. oligophlebia los compuestos más abundantes fueron α-pineno (17.5%), ß-cariofileno (15.5%) y óxido de cariofileno (10.6%); sin embargo, en el aceite obtenido del fruto fueron benzoato de bencilo (16.8%), (E, E)-farnesol (8.3%) y ß- cariofileno (6.0%).

Estudio fitoquímico y evaluación de la actividad antioxidante de Esenbeckia litoralis Donn.Sm. (Loro grande) / Phytochemical study and evaluation of the antioxidant activity of Esenbeckia litoralis Donn. Sm. (loro)

Introducción: la especie Esenbeckia litoralis Donn.Sm. (Rutaceae) es también conocida como Loro o Loro grande, ha sido empleado en la medicina tradicional para el tratamiento de mordeduras de serpientes, dolor de garganta y lesiones ocasionadas por picaduras de insectos. Esta variedad de actividades son causadas por acción de los compuestos que la constituyen, como lignanos, terpenos, alcaloides, cumarinas y polifenoles que representan un alto potencial farmacológico para esta especie. Objetivo: realizar el estudio fitoquímico y evaluación de la actividad antioxidante de la especie E. litoralis. Métodos: los extractos vegetales de hojas corteza y madera se obtuvieron empleando etanol al 96 por ciento, y posteriormente fueron fraccionados usando técnicas cromatográficas como Cromatografía en Capa Delgada (CCD), Cromatografía en Columna (CC) y Cromatografía en Capa Delgada Preparativa (CCDP). Los compuestos se identificaron mediante el análisis de datos espectroscópicos con el empleo de técnicas instrumentales como: Infrarrojo (IR), Resonancia Magnética Nuclear Protónica y de Carbono trece (RMN-1H y 13C), Espectrometría de Masas (EM) y difracción de rayos x (DRX). La actividad antioxidante se evaluó a través de los métodos radical catiónico ABTS•+, radical libre DPPH• y Potencial de Actividad de Reducción Férrica (FRAP). Resultados: de esta especie se aislaron e identificaron cinco compuestos: cuatro alcaloides y un flavonoide. Los extractos en acetato de etilo de hojas y corteza mostraron una significativa actividad frente a los radicales ABTS•+ con un IC50 de 5,65 y 7,65 µg/mL respectivamente. Conclusiones: de los distintos extractos se aislaron cinco compuestos: 1-hidroxi-3-metoxi-N-metilacridona (1), maculosidina (2) maculina (3), dictamina (4) y gardenina B (5). El extracto en acetato de etilo de hojas y corteza presentaron una significativa actividad antioxidante frente al radical ABTS con un IC50 de 5,65 y 7,65 mg/L, respectivamente(AU)

Introduction: The species Esenbeckia litoralis Donn. Sm. (Rutaceae), also known as loro or loro grande, has been used in traditional medicine to treat snakebites, sore throats and lesions caused by insect bites. The compounds contained in the plant, among them lignans, terpenes, alkaloids, coumarins and polyphenols, are responsible for such a broad variety of activities, granting it great pharmacological potential. Objective: Conduct a phytochemical study and evaluation of the antioxidant activity of the species E. litoralis. Methods: Plant extracts from leaves, stem and wood were obtained using 96 percent ethanol, and then fractioned with chromatographic techniques such as thin-layer chromatography (TLC), column chromatography (CC) and preparative thin-layer chromatography (PTLC). The compounds were identified by spectroscopic data analysis using instrumental techniques such as infrared (IR) spectroscopy, proton and Carbon-13 nuclear magnetic resonance (NMR-1H and 13C), mass spectrometry (MS) and X-ray diffraction (XRD). Antioxidant activity was evaluated with the methods ABTSo+ radical cation, DPPHo free radical and ferric reducing ability power (FRAP). Results: Five compounds were isolated from the species: four alkaloids and one flavonoid. Ethyl acetate extracts from leaves and stem displayed significant activity against ABTSo+ radicals, with a CI50 of 5.65 and 7.65 µg/ml, respectively. Conclusions: Five compounds were isolated from the various extracts: 1-hydroxy-3-methoxy-N-methylacridone (1), maculosidin (2), maculin (3), dictamin (4) and gardenin B (5). The leaf and stem extract in ethyl acetate displayed significant antioxidant activity against the ABTS radical, with a CI50 of 5.65 and 7.65 mg/l, respectively(AU)

Role of Apigenin in Cancer Prevention via the Induction of Apoptosis and Autophagy

Apigenin (4′,5,7-trihydroxyflavone) is a flavonoid commonly found in many fruits and vegetables such as parsley, chamomile, celery, and kumquats. In the last few decades, recognition of apigenin as a cancer chemopreventive agent has increased. Significant progress has been made in studying the chemopreventive aspects of apigenin both in vitro and in vivo. Several studies have demonstrated that the anticarcinogenic properties of apigenin occur through regulation of cellular response to oxidative stress and DNA damage, suppression of inflammation and angiogenesis, retardation of cell proliferation, and induction of autophagy and apoptosis. One of the most well-recognized mechanisms of apigenin is the capability to promote cell cycle arrest and induction of apoptosis through the p53-related pathway. A further role of apigenin in chemoprevention is the induction of autophagy in several human cancer cell lines. In this review, we discuss the details of apigenin, apoptosis, autophagy, and the role of apigenin in cancer chemoprevention via the induction of apoptosis and autophagy.

Repellent activity of Glycosmis plant extracts against two stored product insects / Actividad repelente de extractos de plantas Glycosmis contra dos insectos de productos almacenados

In the present study, the repellent activities of the leaf and/or stem crude extracts of Glycosmis lucida Wall. ex Huang, G. craibii var. glabra, G. craibii Tanaka, G. oligantha Huang, G. pentaphylla (Retz) Correa. and G. esquirolii (Levl.) Tanaka were analyzed by using assays on petri dishes against Tribolium castaneum and Liposcelis bostrychophila. The leaf and stem extracts of G. lucida, G. craibii var. glabra, G. craibii Tanaka, G. oligantha and G. esquirolii possessed significant repellent activities against T. castaneum, the same level repellent with the positive control, DEET. However, the extracts of G. pentaphylla, no repellency but some insect attractant was observed. Moreover, they also showed repellent activities against L. bostrychophila. These results indicate that extracts from G. lucida and G. oligantha leaf could be a source of novel repellent against insects.

En el presente estudio, las actividades repelentes de la hoja y/o tronco de los extractos crudos de Glycosmis lucida Wall. ex Huang, G. craibii var. glabra, G. craibii Tanaka, G. oligantha Huang, G. pentaphylla (Retz) Correa y G. esquirolii (Levl.) Tanaka se analizaron mediante el uso de ensayos en placas de Petri contra Tribolium castaneum y Liposcelis bostrychophila. Los extractos de las hojas y tallo de G. lucida, G. craibii var. glabra, G. craibii Tanaka, G. oligantha y G. esquirolii poseían actividades repelentes significativas contra T. castaneum, el mismo nivel repelente del control positivo, el DEET. Sin embargo, los extractos de G. pentaphylla, no se observó la repelencia pero sí actividad atrayente de insectos. Por otra parte, también se mostraron las actividades repelentes contra L. bostrychophila. Estos resultados indican que los extractos de hojas de G. lucida y G. oligantha podrían ser una fuente de repelente contra los insectos.

Evaluation of the tickcide, genotoxic, and mutagenic effects of the Ruta graveolens L (Rutaceae) / Avaliação dos efeitos carrapaticida, genotóxico e mutagênico da Ruta graveolens L (Rutaceae)

Current analysis investigated the tickcide effects of the aqueous extract and chloroform fractions of Ruta graveolens L. (rue) on engorged females of Rhipicephalus microplus, as well as their genotoxic and mutagenic effects on human leukocytes. The best tickcide activity (non-dependent dose) and genotoxic / mutagenic effects (dependent-dose) were observed on exposure to chloroform fractions. Results suggest that extract fractions of R. graveolens L are efficient against R. microplus, although the fraction and the tested concentrations show genotoxic and mutagenic potential for human leukocytes.

O efeito carrapaticida do extrato aquoso e frações da Ruta graveolens L. (arruda) sobre teleóginas de Rhipicephalus microplus, bem como seu potencial genotóxico sobre leucócitos humanos foram investigados neste trabalho. A melhor atividade carrapaticida (dose não dependente) e efeito genotóxico / mutagênico (dose dependente) foram observados nas frações clorofórmicas. Os resultados encontrados sugerem que frações clorofórmicas do extrato de Ruta graveolens L. são eficazes contra R. microplus, embora a fração e as concentrações testadas apresentem potencial genotóxico e mutagênico para células leucocitárias humanas.

Murrayafoline A Induces a G0/G1-Phase Arrest in Platelet-Derived Growth Factor-Stimulated Vascular Smooth Muscle Cells

The increased potential for vascular smooth muscle cell (VSMC) growth is a key abnormality in the development of atherosclerosis and post-angioplasty restenosis. Abnormally high activity of platelet-derived growth factor (PDGF) is believed to play a central role in the etiology of these pathophysiological situations. Here, we investigated the anti-proliferative effects and possible mechanism(s) of murrayafoline A, a carbazole alkaloid isolated from Glycosmis stenocarpa Guillamin (Rutaceae), on PDGF-BB-stimulated VSMCs. Murrayafoline A inhibited the PDGF-BB-stimulated proliferation of VSMCs in a concentration-dependent manner, as measured using a non-radioactive colorimetric WST-1 assay and direct cell counting. Furthermore, murrayafoline A suppressed the PDGF-BB-stimulated progression through G0/G1 to S phase of the cell cycle, as measured by [3H]-thymidine incorporation assay and cell cycle progression analysis. This anti-proliferative action of murrayafoline A, arresting cell cycle progression at G0/G1 phase in PDGF-BB-stimulated VSMCs, was mediated via down-regulation of the expression of cyclin D1, cyclin E, cyclin-dependent kinase (CDK)2, CDK4, and proliferating cell nuclear antigen (PCNA), and the phosphorylation of retinoblastoma protein (pRb). These results indicate that murrayafoline A may be useful in preventing the progression of vascular complications such as restenosis after percutaneous transluminal coronary angioplasty and atherosclerosis.

Estudio de plantas antiparasitarias de la farmacopea tacana: Galipea longiflora y Ficus ssp / Study of antiparasitic plants of the tacana pharmacopoeia: Galipea longiflora and Ficus ssp

Farmacopea Tacana. Se realizó el estudio de 2 especies vegetales antiparasitarias de la Farmacopea Tacana: Galipea longiflora (Evanta) y Ficus spp. (Ojé). El estudio de la Evanta comprende a su vez: el estudio de plantines de diferentes tamaños, este se centra en el análisis de variaciones de la mezcla de alcaloides quinolínicos y la actividad antiparasitaria frente a la variación del tamaño del plantin; y la validación del uso tradicional como antiparasitario, mediante un estudio de campo, que compara la efectividad de la decocción de alcaloides de Evanta en jugo de naranja, frente a un fármaco de actividad reconocida (Mebendazol). En el caso del Ojé, se realizaron estudios comparativos de las proteasas contenidas en su látex, colecta do en diferentes zonas [Iquitos-Perú; Provincia Sud Yungas y Provincia Abel Iturralde, La Paz-Bolivia] Materiales y métodos. En el estudio de plantines se obtuvieron los alcaloides totales de plantin (PAT), los cuales fueron analizados por cromatografía de gases - masas (GC/MS) y evaluados frente a promastigotes de Leishmania. Para la validación de Evanta como antiparasitario, se realizó un examen coproparasitológico seriado a niños de la escuela Charcas II, aplicando el método de Ritchie para la evaluación microscópica. En el estudio del Ojé, se emplearon métodos de cuantificación de proteínas (Biuret), determinación de actividad proteolítica sobre azocaseína (Cristen-Marshall) y leche (Balls y Hoover), además de caracterización por SDS-PAGE. Resultados Se identificaron hasta 14 alcaloides quinolínicos, 5 de ellos comunes entre adultos y plantines, otros aparecen cuando el plantin tiene mayor edad. Se obtuvo una mejor actividad biológica para los plantines con respecto al árbol adulto. La validación de Evanta como antiparasitario, en general, muestra un control en los niveles de parasitosis y la disminución de parásitos por muestra. A nivel de tratamientos tanto la decocción de Evanta como el Mebendazol presentan alta tasa de curación para helmintos, en protozoarios los niveles de eliminación son mínimos. La administración de placebo (2013) confirma la eficacia de los tratamientos al existir un incremento en la prevalencia de parásitos; reapareciendo parásitos que se habían eliminado y otros que no se reportaron al inicio del estudio. El estudio del látex de Ojé muestra concentraciones de proteínas, actividad proteolítica y especies proteínicas por SDS-PAGE variables entre zonas de colecta. Además de la conservación. (AU)

Chemical constituents from stems and leaves of Micromelum integerrimum / 药学学报

A new benzene derivative microintegerrin C (1) and a new norsesquiterpenoid microintegerrin D (2), along with six known compounds (3-8), were isolated and identified from stems and leaves of Micromelum integerrimum by various chromatographies such as silica gel, Sephadex LH-20, RP-18 column chromatography and HPLC. Their structures were mainly identified based on the spectral data analysis such as 1D-, 2D-NMR and HR-EI-MS. All known compounds were isolated from this plant for the first time.

Bioactive Constituents from the Leaves of Zanthoxylum schinifolium

Activity-guided separation of the methylene chloride-soluble fraction of the leaves of Zanthoxylum schinifolium, resulted in the isolation of four coumarinoids (1 - 4), two triterpenoids (5, 6) and three fatty acid derivatives (7 - 9) as active principles. Their chemical structures were identified as collinin (1), 8-methoxyanisocoumarin (2), 7-(6'R-hydroxy-3',7'-dimethylocta-2',7'-dienyloxy)-coumarin (3), (E)-4-methly-6-(coumarin-7'-yloxy) hex-4-enal (4), lupeol (5), epi-lupeol (6), phytol (7), hexadec-3-enoic acid (8) and palmitic acid (9), on the basis of spectroscopic (1D, 2D and MS) data analyses and comparing with the data published in the literatures. Compounds 1 and 7 showed potent cytotoxicity against Jurkat T cells with IC50 values of 45.58 and 47.51 microM, respectively. The others showed moderate activity with IC50 values ranging around 80.58 to 85.83 microM, while the positive control, auraptene, possessed an IC50 value of 55.36 microM.