Efecto citotóxico de diterpenos derivados del ácido ent-kaureno aislados de Coespeletia moritziana (Sch. Bip. ex Wedd.) Cuatrec / Cytotoxic effect of ent-kaurene acid-derived diterpenes isolated from Coespeletia moritziana (Sch. Bip. Ex Wedd.) Cuatrec

The objective of the work was to study the cytotoxic effect of ent-kaurene acid derivatives obtained from Coespeletia moritziana (Sch. Bip. Ex Wedd.) Cuatrec., After analysis by GC/MS, IR and NMR. Isolating: kaurenic acid (I), grandifloric acid (II), 15-α-hydroxy kaurenic acid (III), 15 α-acetoxy-kaur 16-en-19-oic acid (IV), Kaurenol (V); and by hemisynthesis: 15,16-epoxy-17-acetoxy-kauran 19-oic acid (VI), 15-oxo-ent-kaur-16-en-19-oic acid (VIII), ester 2,3,4,6 -15-oxo-kaur-16-en-19-oic acid acetyl α-D-pyranosyl tetra-tetra (VII). Cytotoxicity was tested in human cancer cell lines: uterus (HeLa), lung (A-549), breast (MCF-7), African green monkey kidney non-tumor line (Vero) and human peripheral blood mononuclear cells (CMPS). Compound (I) was active against HeLa, A-549 and Vero. Compounds (II and VIII) showed moderate and good (IC50 ≤ 9 µM) cytotoxicity, respectively, against the five cell lines. Compound (V) showed moderate activity against A-549 and compound (VII), slight cytotoxicity against HeLa and A-549. Results that show the cytotoxic specificity of the isolated kaurenes and derivatives of Coespeletia moritzianaand their therapeutic potential.

El objetivo del trabajo fue estudiar el efecto citotóxico de derivados del ácido ent-kaureno obtenidos de Coespeletia moritziana (Sch. Bip. ex Wedd.) Cuatrec., previo análisis mediante GC/MS, IR y RMN. Aislandose: ácido kaurénico(I), ácido grandiflorénico (II), ácido 15-α-hidroxi kaurénico(III), ácido 15 α-acetoxi-kaur 16-en-19-oico (IV), Kaurenol (V); y por hemisíntesis: ácido 15,16-epoxi-17-acetoxi-kauran 19-oico (VI), ácido15-oxo-ent-kaur-16-en-19-oico (VIII), éster 2,3,4,6-tetra acetil α-D-piranosilo del ácido 15-oxo-kaur-16-en-19-oico (VII). La citotóxicidad fue ensayada en líneas celulares cancerosas humanas: útero (HeLa), pulmón(A-549), mama (MCF-7), línea no tumoral de riñón de mono verde africano (Vero) y células mononucleares humanas de sangre periférica (CMPS). El compuesto (I) resultó activo frente a HeLa, A-549 y Vero. Los compuestos (II y VIII), mostraron moderada y buena (IC50≤9µM) citotoxicidad respectivamente, frente a las cinco líneas celulares. El compuesto (V) presentó moderada actividad frente a A-549 y el (VII), leve citotoxicidad frente a HeLa y A-549. Resultados que evidencian la especificidad citotóxica de los kaurenos aislados y derivados de Coespeletia moritzianay su potencial terapéutico.

Purified novel and new diferuloyl glycerate related phenolic acid from Pandanus odoratissimus flowers shows antioxidant, invertase inhibition and control against diabetic foot ulcer (DFU) causing bacterial pathogens - An in vitro study to establish an effective regulation over type 2 diabetes mellitus

Abstract Chronic type 2 diabetes mellitus (T2DM) and its associated diseases are major concern among human population and also responsible for significant mortality rate. Hence, the present study aims to evaluate and correlate the invertase inhibition, antioxidant activity and control against DFU causing bacterial pathogens by Pandanus odoratissimus flowers. Two dimensional preparative thin layer chromatography (2D PTLC) was adopted to purify the phenolic acid component and LC-MS2 was done to predict the phenolic acid structures. Standard spectrophotometry methods were adopted to investigate the in vitro invertase inhibitory and antioxidant (CUPRAC and ABTS) activities. Agar well diffusion and broth dilution assays were used to record the antibacterial property against DFU causing pathogens isolated from clinical samples. Statistical analyses were used to validate the experiments. A new and novel diferuloyl glycerate related phenolic acid (m/z 442) purified from PTLC eluate has recorded satisfactory cupric ion reducing power (ED50= 441.4±2.5 µg), moderate ABTS radical scavenging activity (IC50= 450.3±10 µg; 32.5±1.5%), and a near moderate, in vitro, invertase mixed type inhibition (24.5±4.5%; Ki: 400 µg). Similarly, bacterial growth inhibitory kinetics has showed a significant inhibition against E. coli and S. aureus.

99m Technetium-HMPAO-labeled platelet scan in practice: Preparation, quality control, and biodistribution studies

Abstract There is no biodistribution or imaging data on 99mtechnetium (Tc)-hexamethyl propylamine oxime (HMPAO)-labeled platelets in the literature. The current study aimed to present updated information about the clinical procedures for preparation and use of labeled platelets. Following two-step centrifugation at 1500 and 2500 rpm, the platelets were extracted from whole blood into platelet-rich plasma (PRP) above the buffy coat and then from PRP into a platelet pellet at the bottom of the tube. The 99mTc-HMPAO-labeled platelets were inspected for purity, viability, release of 99mTc from platelets, and sterility. Also, microscopic examination and thin layer chromatography (TLC) were performed. Biodistribution was assessed following necropsy in BALB/c mice and through imaging of New Zealand rabbits. The separation ratio was estimated at 98%, and radiochemical purity was measured to be 80%. The labeling efficiency was above 30% in more than half of the assays (range: 17-43%). The release of 99mTc from platelets was 9% per hour at 37ºC. After 24 hours, stability was estimated at 54% in the human serum. The target organs of mice included the spleen and liver. In rabbits, the imaging results indicated liver as the target organ. Thyroid uptake was negligible up to 90 minutes. Based on the findings, extraction of platelets and labeling them with 99mTc-HMPAO is a feasible and safe approach in routine practice.

Structural elucidation, mechanism of action, antibacterial proficiency and synergistic forte of purified Euphorbia hirta whole plant extract against multi-drug resistant otitis media infection / Elucidación estructural, mecanismo de acción, competencia antibacteriana y fuerza sinérgica del extracto de planta entera de Euphorbia hirta purificado contra la infección por otitis media resistente a múltiples fármacos

This study investigated the antibacterial potential of Euphorbia hirtawhole plant extracts, honey and conventional antibiotics and their synergistic effects against selected multidrug resistant and typed bacterial strains associated with otitis media. E. hirtawhole plant extract was purified using column chromatography technique. The antibacterial assays of extracts were done using standard microbiological procedures. Protein, sodium and potassium ion leakage of the synergistic mixtures was determined using flame-photometry. At 100 mg/ml, acetone extracts presented highest inhibition against S. aureus (NCTC 6571) with 32 ± 0.83 mm zone of inhibition. The fractional inhibitory concentration indices displayed higher synergism in combination of plant extract, honey and ciprofloxacin against P. mirabilisat 0.02 compared to drug combination synergy standard (≤ 0.5). This work revealed augmentation of ciprofloxacin potency when combined with purified E. hirta acetone extract and honey and implies their high potential in the treatment of multidrug resistant infectionof otitis media.

Este estudio investigó el potencial antibacteriano de extractos de plantas enteras de Euphorbia hirta, miel y antibióticos convencionales y sus efectos sinérgicos contra cepas bacterianas seleccionadas multirresistentes y tipificadas asociadas con la otitis media. El extracto de la planta entera de E. hirtase purificó usando la técnica de cromatografía en columna. Los ensayos antibacterianos de extractos se realizaron utilizando procedimientos microbiológicos estándar. La fuga de iones de proteínas, sodio y potasio de las mezclas sinérgicas se determinó mediante fotometría de llama. A 100 mg/ml, los extractos de acetona presentaron la mayor inhibición contra S. aureus (NCTC 6571) con una zona de inhibición de 32 ± 0,83 mm. Los índices de concentración inhibitoria fraccional mostraron un mayor sinergismo en combinación de extracto de planta, miel y ciprofloxacina contra P. mirabilisa 0,02 en comparación con el estándar de sinergia de combinación de fármacos (≤ 0,5). Este trabajo reveló un aumento de la potencia de la ciprofloxacina cuando se combina con extracto de acetona purificado de E. hirtay miel e implica sualto potencial en el tratamiento de infecciones de otitis media resistentes a múltiples fármacos.

Biological properties and phytochemical characterization from Miconia chamissois Naudin aqueous extract / Propiedades biológicas y caracterización fitoquímica del extracto acuoso de Miconia chamissois Naudin

The objective of this study was to evaluate biological and phytochemical properties of the aqueous extract from the leaves of Miconia chamissois Naudin (AEMC). Phytochemical properties were assessed by analyzing the chromatographic profile and the polyphenol content of AEMC. Biological properties evaluation was conducted based on cytotoxicity assay and by evaluating the antioxidant, antimicrobial, and enzymatic inhibition activities. Results indicated the presence of phytochemicals in AEMC such as flavonoids and polyphenols, including rutin, isoquercitrin and vitexin derivatives. AEMC showed antioxidant activity, which may be attributed to the high polyphenolic content. Moreover, AEMC demonstrated in vitro enzyme inhibition activity against tyrosinase and alpha-amylase, as well as showed low cytotoxicity. On the other hand, AEMC exhibited weak antimicrobial activity against S. aureusand C. albicans. Thus, AEMC is a promising alternative in search of potential drugs for the treatment of diseases induced by oxidative stress and inflammation, conditions due to hyperpigmentation processes, such as melisma, as well as for diabetes.

El objetivo de este estudio fue detectar las propiedades biológicas y fitoquímicos del extracto acuoso de las hojas de Miconia chamissois Naudin (AEMC). Las propiedades fitoquímicas se evaluaron analizando el perfil cromatográfico y el contenido de polifenoles de AEMC. La evaluación de las propiedades biológicas se realizó en base al ensayo de citotoxicidad y evaluando las actividades de inhibición antioxidante, antimicrobiana y enzimática. Los resultados indicaron la presencia de fitoquímicos en AEMC, como flavonoides y polifenoles, que incluyen derivados de rutina, isoquercitrina y vitexina. AEMC mostró una actividad antioxidante considerable, que puede atribuirse al alto contenido polifenólico. Además, AEMC exhibió actividad de inhibición enzimática in vitro contra tirosinasa y alfa-amilasa, así como mostró baja citotoxicidad. Por otro lado, AEMC demostró actividad antimicrobiana débil contra S. aureusy C. albicans. Por lo tanto, AEMC es una alternativa prometedora en busca de posibles drogas para el tratamiento de enfermedades inducidas por el estrés oxidativo y la inflamación, afecciones debidas a procesos de hiperpigmentación, como el melasma, así como para la diabetes.

Chemistry characterization and antioxidant activity of mangosteen (Garcinia mangostana L, Clusiaceae) cultivated in Colombia / Caracterización química y actividad antioxidante del mangostino (Garcinia mangostana L, Clusiaceae) cultivado en Colombia

The objective of this work was to evaluate the antioxidant and inhibitory activities of the ethanolic extracts of the mangosteen (Garcinia mangostana L.) grown in Montenegro, Quindío, Colombia, in three stages of maturation, including the edible (pulp) and inedible parts (pericarp and peduncle). The alcoholic samples were phytochemically characterized by Thin Layer Chromatography (TLC), High Performance Liquid Chromatography (HPLC) and by Fourier Transformation Infrared Spectroscopy (FT-IR); the antioxidant capacities were also evaluated by the diphenyl-picrylhydrazyl (DPPH•) radical method and Oxygen Radical Absorbance Capacity (ORAC), in addition to the inhibitory activity of acetylcholinesterase (AchE) and the total content of phenols and flavonoids. The tests detected phytochemical compounds such as phenols, flavonoids, alkaloids, quinones and xanthones, to which the antioxidant activity and the inhibition of AChE presented, can be attributed. In conclusion, the inedible parts of mangosteen contain higher proportions of secondary metabolites, these being the most promising sources for industrial use.

El objetivo de este trabajo fue el de evaluar las actividades antioxidantes e inhibitoria de acetilcolinesterasa de los extractos etanólicos del mangostino (Garcinia mangostana L.) de Montenegro, Quíndio, Colombia, en tres estados de maduración, incluyendo las partes comestibles (pulpa) y no comestibles (pericarpio y pedúnculo). Las muestras alcohólicas fueron caracterizadas fitoquímicamente por Cromatografía de Capa Delgada (CCD), Cromatografía Líquida de Alta Eficiencia (HPLC) y Espectroscopía Infrarroja por Transformada de Fourier (FT-IR); la capacidad antioxidante fue evaluada también por el método de captación del radical libre 2,2-difenil-1-picrilhidracilo (DPPH• dejar el radical en superíndice) y la Capacidad de Absorción de Radicales de Oxígeno (ORAC), adicionalmente la actividad inhibitoria de la acetilcolinesterasa (AchE) y el contenido total de fenoles y flavonoides. Se detectaron compuestos fitoquímicos como fenoles, flavonoides, alcaloides, quinonas y xantonas, a quienes se les puede atribuir las actividades antioxidantes y de inhibición de la acetilcolinesterasa. En conclusión, las partes no comestibles del mangostino contienen una mayor proporción de metabolitos secundarios, siendo las fuentes más promisorias para uso industrial.

Preparation of polymer nanoparticles loaded with Syzygium aromaticum essential oil: an oral potential application / Preparación de nanoparticulas polimericas cargadas con aceite esencial de Syzygium aromaticum: una potencial aplicación oral

Due to the biological activities of Syzygium aromaticum essential oil, its incorporation in methacrylate polymeric (Eudragit E100) nanoparticles (NP), physical characterization, and antimicrobial essays were evaluated. The clove bears great potential for applications in dentistry. The oil was obtained by hydrodistillation and oil loaded NP using the nanoprecipitation method. Particle size and polydispersity index were determined by photon correlation spectroscopy, and physical morphology by electron microscopy. Loading capacity and in vitro eugenol release were evaluated by gas mass chromatography, and the antimicrobial activity of oil loaded-NP was calculated against Streptococcus mutans. Different chemical ingredients were characterized, and eugenol was the principal compound with 51.55%. Polymer content was directly related to NP homogenous size, which was around 150 nm with spherical morphology. A 73.2% loading capacity of eugenol was obtained. Oil loaded NP presented a fickian-type release mechanism of eugenol. Antimicrobial activity to 300 µg/mL was obtained after 24 h.

Debido a las actividades biológicas del aceite esencial de Syzygium aromaticum, se evaluó su incorporación en nanopartículas (NP) de metacrilato polimérico (Eudragit E100), su caracterización y ensayos antimicrobianos. El clavo tiene un gran potencial para aplicaciones en odontología. El aceite se obtuvo por hidrodestilación y las NP cargado de aceite utilizando el método de nanoprecipitación. El tamaño de partícula y el índice de polidispersidad se determinaron mediante espectroscopia de correlación fotónica y su morfología por microscopía electrónica. La capacidad de carga y la liberación de eugenol in vitro se evaluaron mediante cromatografía de gases en masa, y la actividad antimicrobiana se evaluó contra Streptococcus mutans. Se caracterizaron diferentes ingredientes químicos, siendo el eugenol el principal compuesto con 51.55%. El contenido de polímero se relacionó directamente con el tamaño homogéneo de NP, que fue de alrededor de 150 nm con morfología esférica. Se obtuvo un 73,2% de capacidad de carga de eugenol. El aceite cargado en NP presentó un mecanismo de liberación de eugenol de tipo fickiano. La actividad antimicrobiana a 300 µg/mL se obtuvo después de 24 h.

Variación de los perfiles de polifenoles en Ligaria cuneifolia (R. et. P) Tiegh (Loranthaceae), su estudio mediante electroforesis capilar y su relación con la actividad farmacológica. / Polyphenolic profile variation in Ligaria cuneifolia (R. et P.) Tiegh (Loranthaceae), capillary electrophoretic analysis and its relationship with the pharmacological activity

Ligaria cuneifolia (R. et P.) Tiegh. ­Loranthaceae­ es una especie hemiparásita que se desarrolla sobre diferentes hospedantes. Es conocida con el nombre vulgar de "liga" o "liguilla". Debido a su similitud morfológica, constituye el sustituto natural del "muérdago europeo", por lo cual es denominado "muérdago criollo". Las drogas vegetales son matrices complejas en las cuales múltiples componentes actúan en forma sinérgica y son responsables de la acción farmacológica. Con el fin de dar sustento científico al uso folclórico de L. cuneifolia se estudiaron distintas formas de obtención de los extractos, se evaluaron diferentes hospedantes y regiones fitogeográficas. Se desarrolló y validó un método de electroforesis capilar para construir fingerprints o perfiles cromatográficos característicos que permitan evaluar los distintos componentes con el fin de estandarizar los extractos. Se efectuó la comparación con otras técnicas cromatográficas, tales como en cromatografía en capa delgada (TLC) y líquida de alta resolución (HPLC). A su vez, se procedió al aislamiento, purificación y análisis estructural de los compuestos de interés por técnicas espectroscópicas y cromatográficas. Se identificaron diez compuestos, de los cuales cuatro son reportados por primera vez en esta especie. La electroforesis capilar probó ser una técnica adecuada para el control de calidad de los extractos y una alternativa atractiva a las técnicas cromatográficas tradicionales.

Ligaria cuneifolia (R. et P.) Tiegh. ­Loranthaceae­ is a hemiparasite plant which grows on different host trees. It is popularly referred to as "liga" or "liguilla". Due to its morphological similarity, it is considered as the natural substitute for the European mistletoe, for which is known as the "Argentine mistletoe". Herbal drugs are complex matrices in which multiple components acting synergistically are responsible for the pharmacological activity. In order to provide scientific support to the popular use of L. cuneifolia, a capillary electrophoretic method was developed and validated to build a chromatographic profile or fingerprint that allows the evaluation of different components for extract standardization. A comparison was made with other chromatographic techniques such as TLC and HPLC. Isolation, purification and structural analysis of compounds were performed by chromatographic and spectroscopic methods. Ten analytes were identified, four of which are reported for the first time in L. cuneifolia. Capillary electrophoresis proved to be an appropriate tool for the quality control of herbal drugs, as well as an attractive alternative to traditional chromatographic techniques.

Bile acid detection by biosensors-a review / 生物工程学报

Bile acids facilitate the absorption of lipids, and affect the development of various diseases by regulating intestinal flora structure and modulating immunity and metabolism. It is therefore important to quantitatively detect bile acids. Current analytical methods are still immature due to constituent complexity, structural heterogeneity and bioactive variability of bile acids. Detection of individual bile acids is of significance for pharmacological research, clinical diagnosis and disease prevention. Advances have been made in bile acid analysis from multiple sources including serum, bile, urine and feces, although several limitations still exist for bile acid quantification. Here we review research progress in conventional bile acid assays, including spectrophotometry, thin-layer chromatography, liquid/gas chromatography and liquid/gas chromatography-mass spectrometry. Moreover, we emphasize the development of bile acid biosensors that may have promising prospects.

Propuesta de compuestos fenólicos presentes en el extracto metanólico de hojas de Clinopodium pulchellum (Kunth) Govaerts "panisara" / Characterization of phenolic compounds of the metallolic extract of leaves of clinopodium pulchellum (kunth) govaerts «panisara¼

Objetivos. Proponer compuestos fenólicos presentes en el extracto metanólico de hojas de Clinopodium pulchellum (Kunth) Govaerts «panisara¼. Materiales y métodos. Se preparó un extracto metanólico de las hojas de Clinopodium pulchellum (Kunth) Govaerts «panisara¼, se determinó la solubilidad por disolución de extracto en solventes de polaridad creciente. Se detectaron algunos componentes químicos mediante un screening fitoquímico empleando gelatina, tricloruro férrico, reacción de Mayer, reacción de Shinoda, entre otros. Se realizó cromatografía en capa fina, revelándose por aspersión con reactivos cromogénicos y se propone posibles estructuras de componentes mediante espectroscopía UV. Resultados. El extracto metanólico presentó buena solubilidad en solventes de alta y mediana polaridad. El screening fitoquímico dio resultados positivos para la presencia de compuestos fenólicos y compuestos nitrogenados: flavonoides, alcaloides y glicósidos. Conclusión. Se propuso la estructura química de tres flavonoides obtenidos del extracto metanólico de hojas de Clinopodium pulchellum (Kunth) Govaerts «panisara¼.

Objectives. Propose phenolic compounds present in the methanolic extract of Clinopodium pulchellum (Kunth) Govaerts "panisara" leaves. Materials and methods. A methanolic extract of the Clinopodium pulchellum (Kunth) Govaerts "panisara" leaves was prepared by maceration, the solubility was determined by dissolving the extract in solvents of increasing polarity. Some chemical components were detected by phytochemical screening using gelatin, ferric trichloride, Mayer reaction, Shinoda reaction, among others. Thin layer chromatography was performed, revealing by spray with chromogenic reagents and possible component structures by UV spectroscopy. Results. The methanolic extract showed good solubility in solvents of high and medium polarity. Phytochemical screening gave positive results for the presence of phenolic compounds and nitrogen compounds: flavonoids, alkaloids and glycosides. Conclusion. The chemical structure of three flavonoids obtained from the methanolic leaf extract of Clinopodium pulchellum (Kunth) Govaerts "panisara" was proposed.

The diversity of ursodeoxycholic acid precursors from bile waste of commercially available fishes, poultry and livestock in Indonesia

Ursodeoxycholic acid (UDCA), a secondary bile acid (BA), has been used as a drug to treat various liver diseases. UDCA is synthesised from cholic or chenodeoxycholic acid (CA/CDCA), two primary BAs frequently used as the starting materials. Nowadays, swine, cattle, and poultry bile are the main sources of those BAs. However, other commercial animals could be promising sources as well. We identified two livestock, two poultries, and eight fishes that are commercially cultivated in Indonesia. Four free BAs including CA, CDCA, deoxycholic acid (DCA), and lithocholic acid (LA) were identified for their occurrences using thin-layer chromatography and high-performance liquid chromatography. CA was detected in cow, duck, red tilapia, gourami, the common carp, and grouper, whereas CDCA was only detected in two poultries and the common carp. The occurrence of DCA was common and abundant in most tested animals. In contrast, the presence of LA was found to be very low in all samples. The biliary bile of tilapia has been found to contain a high abundance of free CA (43% of the total bile). A simple extraction was able to purify CA from biliary bile of tilapia. This is a new promising and competitive source of CA.

Tempeh & soybean seed coat: the alternative sources of trans-resveratrol as neuroprotective agents / Tempeh y cubierta de semillas de soja: fuentes alternativas de trans-resveratrol como agentes neuroprotectores

Resveratrol is a stilbenoid, a type of natural phenol, and a phytoalexin produced by several plants in response to injury or attack by fungi. The underutilization of soybean seed coat (Glycine max (L.) Merrill.) and tempeh, cheap Indonesia fermented food thus opens up a new opportunity for developing a Resveratrol-based medicine for Plants-Derived Neuroprotective Agents purposes. In this study, it was isolated from tempeh, ordinarily well-known as Indonesian soybean fermented food, and soybean seed coat. The finding of this compound was confirmed by TLC and HPLC analysis applying fluorescence detection. From this, the Rf-value for transresveratrol is 0.64. As eluent, a mixture of chloroform, ethyl acetate, and formic acid (2.5+1+0.1, v/v) was selected. In addition, retention time for tempeh was 14.467 and for soybean seed coat was 11.977. The extraction yield of resveratrol was 65.15 % in tempeh and 55.35 % in soybean seed coat. Resveratrol isolated from Tempeh and Soybean seed coat gave prevents some reaction by modulating intracellular signaling pathways: protein kinase C (PKC), a family of 12 serine/ threonine kinases and providing a new lead molecule for neuroprotective affects in addition to has prevented cell death by apoptosis.

El resveratrol es un estilbenoide, un tipo de fenol natural, y fitoalexina producida por varias plantas en respuesta a una lesión o ataque de hongos. La subutilización de la cubierta de la semilla de soja (Glycine max (L.) Merrill.) y el tempeh, alimento fermentado barato de Indonesia, abren una nueva oportunidad para obtener un medicamento a base de resveratrol para propósitos de desarrollo de agentes neuroprotectores derivados de plantas. En este estudio, se aisló el resveratrol del tempeh, generalmente conocido como alimento fermentado de soja de Indonesia y de la cubierta de la semilla de soja. El hallazgo de este compuesto se confirmó mediante análisis de TLC y HPLC aplicando detección de fluorescencia. A partir de esto, el valor de Rf para trans-resveratrol es 0,64. Como eluyente, se seleccionó una mezcla de cloroformo, acetato de etilo y ácido fórmico (2,5 + 1 + 0,1, v / v). Además, el tiempo de retención para el tempeh fue de 14,467 y para el revestimiento de semilla de soja fue de 11,977. El rendimiento de extracción del resveratrol fue del 65,15 % en tempeh y del 55,35 % en la cubierta de la semilla de soja. El resveratrol aislado de tempeh y de la cubierta de la semilla de soja previno reacciones mediante la modulación de ciertas vías de señalización intracelular: proteína quinasa C (PKC), una familia de 12 serina/treonin quinasas, proporcionando una nueva molécula de plomo con efectos neuroprotectores, además de prevenir la muerte celular por apoptosis.

Morphoanatomical and phytochemical studies for the quality control of Neurolaena lobata (L.) R.Br. ex Cass. (Asteraceae) / Estudios morfoanatomicos y fitoquimicos para el control de calidad de Neurolaena lobata (L.) R.Br. ex Cass. (Asteraceae)

Neurolaena lobata (L.) R.Br. ex Cass. (Asteraceae)Is a popular folk remedy for in Central America. The plant is of commercial value in Guatemala but so far there is not any monograph to guide regional laboratories on ensuring identity and chemical tests for this species. As identity test we here run macro and micro morphoanatomical studies of the characters of the vegetative organs. We also developed standard chemical tests for quality by both TLC and HPLC for infusions and tinctures of varying alcoholic strength. Their radical scavenging activities in DPPH and NO were also measured. Macro and micro morphoanatomical characters of the vegetative organs present a set of characteristics to facilitate the identification of dry powdered samples of this species. We developed optimal conditions for the TLC and HPLC phytochemical fingerprints of the 4 most common pharmacopoeial liquid herbal preparations from this herbal drug, namely infusion, 70%, 45% and 20% hydroalcoholic tinctures. Our work provides the Latin-American industry with a set of analyses to establish the identity and chemistry of N. lobata samples for quality control purposes.

Neurolaena lobata (L.) R.Br. ex cass. (Asteraceae) es un remedio popular popular en América Central. La planta tiene un valor comercial en Guatemala, pero hasta el momento no existe una monografía que guíe a los laboratorios regionales para garantizar la identidad y las pruebas químicas para esta especie. Como prueba de identidad proponemos estudios macro y micro morfoanatómicos de los caracteres de los órganos vegetativos. También desarrollamos pruebas químicas de calidad mediante CCF y CLAR para infusiones y tinturas de grado alcohólico variable. También se midieron sus actividades de captación de radicales en DPPH y NO. Los caracteres macro y micro morfoanatómicos de los órganos vegetativos presentan un conjunto de características para facilitar la identificación de muestras de polvo seco de esta especie. Desarrollamos condiciones óptimas para las huellas dactilares fitoquímicas de CCF y CLAR de las 4 preparaciones herbales líquidas farmacopéicas más comunes de esta droga herbal, a saber, infusión, 70%, 45% y 20% tinturas hidroalcohólicas. Nuestro trabajo proporciona a la industria latinoamericana un conjunto de análisis base para establecer la identidad y la química de las muestras de N. lobata con fines de control de calidad.

Dayak onions ( Eleutherine bulbosa (Mill.) Urb. ) bulbs extracts reduces blood pressure of hypoestrogen model rats by controlling lipids profile / El extracto de bulbos de cebollas dayak ( Eleutherine bulbosa (Mill. ) Urb. ) reduce la presión sanguínea en un modelo hipoestrogénico en ratas controlando el perfil lipídico

To determine the effects of 70 % ethanolic extract of Eleutherine bulbosa (Mill.) L. bulbs contained naphtoquinone in blood pressure and lipids profile level of ovariectomized rats. Thin layer chromatography was performed to analyze the content of the Eleutherine bulbosa (Mill.) bulbs extracts using Chloroform : Methanol (7:1) as eluent. This study used white female Sprague-Dawley rats which were divided into 6 groups: SHAM and OVX, both given 0.5 % carboxymethyl cellulose; the positive control group that was given tamoxifen (0.36 mg/200 g B.W.); the three various of doses of extract namely dose 1, 2, and 3 that were given 8, 12, and 18 mg/200 g BW respectively on day 29 until 50. All groups were ovariectomized on day 1, except sham group. Measurement of blood pressure were performed on the day before ovariectomy using non-invasive tool CODA®; and on the second, third, and fourth weeks post-ovariectomy. Three weeks after treatment of hypoestrogen rats by the dose 18 mg/200 g B.W, Eleutherine bulbosa extracts could decrease the systolic blood pressure level to 28.06 %, the diastolic to 30.47 %. Lipid profile of Dose 3 also showed recovery of Triglyceride, LDL and also Total Cholesterol. Eleutherine bulbosa extracts could improve blood pressure of ovariectomized rats by controlling lipids profile level.

Para determinar los efectos del 70 % de extracto etanólico de Eleutherine bulbosa (Mill.) L. en bulbos que contenían naftoquinona, se analizó la presión arterial de ratas ovariectomizadas. Se realizó un estudio de cromatografía de capa fina para analizar el contenido de los extractos de bulbos de Eleutherine bulbosa (Mill.) usando cloroformo:metanol (7:1) como diluyente. En este estudio se utilizaron ratas blancas Sprague-Dawley hembras, que se dividieron en 6 grupos: SHAM y OVX, ambos grupos fueron administrados con carboximetilcelulosa al 0,5 %; grupo control positivo, recibió tamoxifeno (0,36 mg / 200 g de B.W.); y tres grupos restantes, que recibieron tres dosis diferentes de extracto, es decir, dosis 1, 2 y 3 a las que se les administró 8, 12 y 18 mg / 200 g de por peso, respectivamente el día 29 hasta el día 50. Todos los grupos fueron sometidos a ovariectomía en el día 1, excepto el grupo simulado. La medición de la presión arterial se realizó el día anterior a la ovariectomía con la herramienta no invasiva CODA®, y, posteriormente, en la segunda, tercera y cuarta semanas de realizada la ovariectomía. Tres semanas después del tratamiento aplicado a las ratas hipoestrógenas, con la dosis de 18 mg / 200 g por peso, los extractos de Eleutherine bulbosa podrían disminuir el nivel de presión arterial sistólica al 28,06 %, y la diastólica al 30,47 %. La dosis 3 del perfil lipídico mostró mejoría en los niveles de Triglicéridos, LDL y Colesterol Total. Los extractos de Eleutherine bulbosa podrían mejorar la presión sanguínea de ratas ovariectomizadas controlando el nivel del perfil lipídico.

Application of fingerprint technology in quality evaluation and process control of traditional Chinese medicine formula granules / 中国中药杂志

The fingerprint technology could reflect the internal chemical characteristics of Chinese herbal medicine or preparation, which has the characteristics of "wholeness" and "fuzziness". It is suitable for evaluating the quality of intermediate and finished products in the production process of traditional Chinese medicine formula granules. In this paper, the applications of high performance liquid chromatography (HPLC), thin layer chromatography (TLC), gas chromatography (GC) and infrared spectrum (IR) fingerprint technology in the quality control of traditional Chinese medicine formula granules were reviewed, and their advantages and disadvantages were analyzed. The aim of this article is to enhance the combined application of various fingerprint technologies in traditional Chinese medicine formula granules. It could provide technical reference for realizing the stability of production process and improving the overall quality of formula granules.

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.

Clusia criuva Cambess. (Clusiaceae): anatomical characterization, chemical prospecting and antioxidant activity

ABSTRACT This study aims the anatomical description and chemical characterization of aerial parts of Clusia criuva Cambess., Clusiaceae in addition to the evaluation of the antioxidant activity of crude extracts, correlated to the flavonoid content. The morphological characterization was performed using traditional techniques of plant anatomy. For phytochemical studies, crude extracts were obtained by static maceration and analyzed by thin layer chromatography. The antioxidant activity and the flavonoids content were determined by colorimetric methods involving, respectively, 2,2-diphenyl-1-picrylhydrazyl free radical and aluminum chloride. C. criuva has uniseriate epidermis, paracytic stomata, hypostomatic leaves, cuticular flanges and cordiform vascular cylinder with accessory bundles. Chemical prospecting confirmed the abundant presence of terpenes and phenols in the extracts of leaves and of fruits. The methanolic extract of seeds showed the lowest EC50 value, but the methanolic extract of pericarps exhibited the highest maximum antioxidant activity. The results suggested a high percentage of flavonoids in the hexanic extract of pericarps, however, this could represent, in fact, the presence of benzophenones. Secretory ducts and the shape of the midrib are diagnostic for C. criuva. The antioxidant activity is not directly related to the flavonoids. The results indicate the importance of future studies with C. criuva chemical constituents.

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.

Biotransformation of bromhexine by Cunninghamella elegans, C. echinulata and C. blakesleeana

Abstract Fungi is a well-known model used to study drug metabolism and its production in in vitro condition. We aim to screen the most efficient strain of Cunninghamella sp. among C. elegans, C. echinulata and C. blakesleeana for bromhexine metabolites production. We characterized the metabolites produced using various analytical tools and compared them with mammalian metabolites in Rat liver microsomes (RLM). The metabolites were collected by two-stage fermentation of bromhexine with different strains of Cunninghamella sp. followed by extraction. Analysis was done by thin layer chromatography, high performance thin layer chromatography, Fourier transform infrared spectroscopy, high performance liquid chromatography and Liquid chromatography–mass spectrometry. The role of Cytochrome P3A4 (CYP3A4) enzymes in bromhexine metabolism was studied. Fungal incubates were spiked with reference standard – clarithromycin to confirm the role of CYP3A4 enzyme in bromhexine metabolism. Three metabolites appeared at 4.7, 5.5 and 6.4 min retention time in HPLC. Metabolites produced by C. elegans and RLM were concluded to be similar based on their retention time, peak area and peak response of 30.05%, 21.06%, 1.34%, and 47.66% of three metabolites and bromhexine in HPLC. The role of CYP3A4 enzyme in metabolism of bromhexine and the presence of these enzymes in Cunninghamella species was confirmed due to absence of peaks at 4.7, 5.4 and 6.7 min when RLM were incubated with a CYP3A4 enzyme inhibitor – clarithromycin.

Actividad biológica de tres Curcuminoides de Curcuma longa L. (Cúrcuma) cultivada en el Quindío-Colombia / Biological activity of three curcuminoids from Curcuma longa L. (turmeric) grown in Quindío, Colombia

Introducción: Curcuma longa L. es una planta de la familia Zingiberaceae distribuida en las regiones tropicales y subtropicales, utilizada en la industria alimentaria, en medicina y en cosmética. Su colorante principal es la curcumina, un polifenol con múltiples efectos medicinales. Objetivos: obtener, caracterizar químicamente y evaluar la actividad biológica de tres curcuminoides de C. longa, cultivada en el Quindío-Colombia. Métodos: se purificaron tres curcuminoides (curcumina (C), demetoxicurcumina (DMC) y bisdemetoxicurcumina (BDMC) desde el rizoma de la planta, en estado seco, por cromatografía en columna y se caracterizaron por punto de fusión, espectroscopía infrarroja (IR), espectroscopía UV-vis y espectrometría de masas. Se evaluó la actividad antimicrobiana en bacterias y hongos por el método modificado de pozos de agar, la citotoxicidad sobre células BHK-21 por el método de bromuro de 3-(4,5- dimetiltiazol-2-ilo)-2,5-difeniltetrazol (MTT) y la toxicidad sobre Artemia salina. Finalmente se determinó el efecto de los curcuminoides en células BHK-21 infectadas con dengue virus 2. Resultados: la curcumina presentó mayor punto de fusión (177,3 ºC-183,2 ºC). El espectro IR reveló los grupos funcionales característicos y el UV-vis indicó máximos de absorción para curcumina, demetoxicurcumina y bisdemetoxicurcumina de 419, 418 y 414 nm en cloroformo, respectivamente. El espectro de masas mostró m/z para C: 368, DMC: 338 y BDMC: 308. Se encontró actividad antimicrobiana frente a Staphylococcus aureus y Staphylococcus epidermidis, se determinó que BDMC presentó menor toxicidad y se evidenció mayor efecto inhibitorio sobre viriones infectivos de dengue con curcumina a 20 y 30 M. Conclusiones: la caracterización de los compuestos confirma su composición como polifenoles, lo cual se relaciona a la actividad biológica de éstos, encontrándose principalmente que la curcumina altera la infección por virus dengue en cultivo celular. Esta investigación confirma la importancia de los principios activos de plantas con amplio espectro farmacológico como C. longa(AU)

Introduction: Curcuma longa L. is a plant from the family Zingiberaceae distributed in tropical and subtropical regions and used in the food industry, in medicine and in cosmetics. Its main coloring substance is curcumin, a polyphenol with many medicinal properties. Objectives: Obtain, characterize chemically and evaluate the biological activity of three curcuminoids from C. longa grown in Quindío, Colombia. Methods: Three curcuminoids (curcumin (C), demethoxycurcumin (DMC) and bisdemethoxycurcumin BDMC) from the rhizome of the plant were purified in a dry state by column chromatography and characterized by fusion point, infrared (IR) spectroscopy, UV-vis spectroscopy and mass spectrometry. Antimicrobial activity against bacteria and fungi was evaluated by the modified agar well method, cytotoxicity to BHK-21 cells by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method, and toxicity against Artemia salina. Finally, determination was made of the effect of the curcuminoids in BHK-21 cells infected with dengue virus 2. Results: Curcumin had the highest fusion point (177.3 ºC-183.2 ºC). IR spectroscopy revealed the characteristic functional groups and UV-vis spectroscopy showed maximum absorption values for curcumin, demethoxycurcumin and bisdemethoxycurcumin of 419, 418 and 414 nm in chloroform, respectively. Mass spectrometry found that m/z values were C: 368, DMC: 338 and BDMC: 308. Antimicrobial activity was observed against Staphylococcus aureus and Staphylococcus epidermidis. BDMC was found to have lower toxicity. A greater inhibitory effect against infective dengue virions was observed with curcumin at 20 y 30 µM. Conclusions: Characterization of the compounds confirms their polyphenolic composition, which manifests in their biological activity, mainly the capacity of curcumin to alter infection by dengue virus in cell cultures. The study corroborated the importance of the active principles of plants with a wide pharmacological spectrum, such as C. longa(AU)