Bioactive endophytic fungi isolated from Caesalpinia echinata Lam. (Brazilwood) and identification of beauvericin as a trypanocidal metabolite from Fusarium sp.

Aiming to identify new sources of bioactive secondary metabolites, we isolated 82 endophytic fungi from stems and barks of the native Brazilian tree Caesalpinia echinata Lam. (Fabaceae). We tested their ethyl acetate extracts in several in vitro assays. The organic extracts from three isolates showed antibacterial activity against Staphylococcus aureus and Escherichia coli [minimal inhibitory concentration (MIC) 32-64 μg/mL]. One isolate inhibited the growth of Salmonella typhimurium (MIC 64 μg/mL) and two isolates inhibited the growth of Klebsiella oxytoca (MIC 64 μg/mL), Candida albicans and Candida tropicalis (MIC 64-128 μg/mL). Fourteen extracts at a concentration of 20 μg/mL showed antitumour activities against human breast cancer and human renal cancer cells, while two isolates showed anti-tumour activities against human melanoma cancer cells. Six extracts were able to reduce the proliferation of human peripheral blood mononuclear cells, indicating some degree of selective toxicity. Four isolates were able to inhibit Leishmania (Leishmania) amazonensis and one isolate inhibited Trypanosoma cruzi by at least 40% at 20 μg/mL. The trypanocidal extract obtained from Fusarium sp. [KF611679] culture was subjected to bioguided fractionation, which revealed beauvericin as the compound responsible for the observed toxicity of Fusarium sp. to T. cruzi. This depsipeptide showed a half maximal inhibitory concentration of 1.9 μg/mL (2.43 μM) in a T. cruzi cellular culture assay.

A new cyclic diarylheptanoid from the bark of Myrica rubra / 药学学报

To study the chemical constituents from the bark of Myrica rubra, fourteen compounds were isolated from the methanolic extract using various chromatographic techniques, including silica gel, Sephadex LH-20 and preparative HPLC. Their structures were identified on the basis of chemical properties and spectroscopic data, as 3, 5-dimethoxy-4-hydroxymyricanol (1), myricanol (2), myricanone (3), myricanol 11-sulfate (4), myricitrin (5), quercetin (6), quercetin-3-rhamnoside (7), tamarixol (8), uvaol (9), ursolic acid (10), taraxerol (11), myricadiol (12), β-sitosterol (13) and β-daucosterol (14). Among them, compound 1 is a new compound, named as 3, 5-dimethoxy-4-hydroxymyricanol, compounds 8, 9 were isolated from the genus Myrica for the first time.

Diarylheptanoid-myricanone isolated from ethanolic extract of Myrica cerifera shows anticancer effects on HeLa and PC3 cell lines: signalling pathway and drug-DNA interaction / 中西医结合学报

<p><b>OBJECTIVE</b>To test if myricanone (C21H24O5), a cyclic diarylheptanoid, has anticancer effects on two different cancer cell lines HeLa and PC3. The present study was conducted with a note on the drug-DNA interaction and apoptotic signalling pathway.</p><p><b>METHODS</b>Several studies like cytotoxicity, nuclear damage, annexin-V-fluorescein isothiocyanate (FITC)/propidium iodide (PI)-labelled apoptotic assay and cell cycle arrest, immunoblot and reverse transcriptase-polymerase chain reaction (RT-PCR) were used following standard protocols. Circular dichroism (CD) spectroscopy was also done to evaluate whether myricanone effectively interacted with DNA to bring about conformational changes that could strongly inhibit the cancer cell proliferation.</p><p><b>RESULTS</b>Myricanone showed a greater cytotoxic effect on PC3 cells than on HeLa cells. Myricanone promoted G0/G1 arrest in HeLa cells and S phase arrest in PC3 cells. Nuclear condensation and annexin V-FITC/PI studies revealed that myricanone promoted apoptotic cell death. CD spectroscopic data indicated that myricanone had an interaction with calf thymus DNA that changed DNA structural conformation. RT-PCR and immunoblot studies revealed that myricanone activated the apoptotic signalling cascades through down-regulation of transcription factors like nuclear factor-κB (NF-κB) (p65), and signal transducers and activators of transcription 3 (STAT3); cell cycle regulators like cyclin D1, and survivin and other signal proteins like Bcl-2 and up-regulation of Bax, caspase-9 and caspase-3.</p><p><b>CONCLUSION</b>Myricanone induced apoptosis in both types of cancer cells by triggering caspase activation, and suppression of cell proliferation by down-regulation of NF-κB and STAT3 signalling cascades, which makes it a suitable candidate for possible use in the formulation of therapeutic agent for combating cancer.</p>

Comparison of antioxidant activity and total phenolic contents of some Persian Gulf marine algae

Marine algae, especially brown species, produce a wide range of metabolites with various biological activities. Since marine algae are rich source of dietary fibers, minerals, proteins, vitamins and phenolic components with antioxidant effect, in addition to the rule of oxidative stress in pathogenesis of chronic diseases, the aim of this study was to investigate possible antioxidant activity and total phenolic contents of three brown algae species [Sargassum swartzii, Cystoseira myrica, Colpomenia sinuosa] collected from Asaloye-Niband marine protected area of the Persian Gulf. Antioxidant activity and total phenolic contents of partitional fractions of Hexan, Chlorofrom [CHCL[3]], Ethylacetate [EtOAc] and Methanolic extract of the samples were studied. Total phenolic contents was measured using Folin-Ciocalteu method while ferric reducing antioxidant power [FRAP] assay were used to study their antioxidant activity. MeOH -H[2]O and chloroform fractions of Sargassum swartzii 12.3, 55.32 +/- 4.8 +/- were found to have the highest antioxidant activity as 73.92 0.5, 11.05 +/- mmol Fe[II] per 100 g dried plant and total phenolic contents, 12.0 0.64 mg gallic acid equivalents per 100 g dried plant respectively. There was a significant Correlation [R[2]=0.999] between the antioxidant activity and total phenolic contents of MeOH-H[2]O fractions obtained from total extracts of these algae. It is recommended that these algae could be potential sources of natural antioxidants

Screening fitoquímico, antimicrobiano y antioxidante de plantas pre-andinas y del altiplano chileno / Phytochemical, antimicrobial and antioxidant screening of pre-Andean plants and the Chilean highlands

El altiplano o puna por sus características ambientales, es una región natural única en América del Sur, abarca el centro y sur del Perú, el norte de Chile, parte de Bolivia, y el noreste de Argentina. En el altiplano existen muchas especies vegetales, pero hay algunas que despiertan mayor interés en los pobladores locales, ya que son utilizados como combustible o forman parte de su dieta diaria y usos medicinales. En este trabajo se investigaron siete plantas de cuatro géneros diferentes: Caiophora, Senecio, Parastrephia y Myrica, con el objetivo de dar un respaldo científico a las propiedades que la medicina folclórica les atribuye, así como dar a conocer estas especies desde un punto de vista fitoquímico y farmacológico, para lo cual se realizó un screening fitoquímico, antimicrobiano y antioxidante de estas plantas pre-andinas y del altiplano chileno. Para ello se debió obtener los diferentes extractos, infusos y aceite esencial de las distintas plantas a estudiar, para su análisis fitoquímico y evaluación farmacológica, y determinar la actividad antimicrobiana por medio del bioensayo de bioautografía, siembra en superficie de agar y concentración mínima inhibitoria. La evaluación de la actividad antioxidante de los extractos se realizó frente a la enzima xantina oxidasa (XO). La investigación del material vegetal de las siete especies, está constituido por la parte aérea de cada especie en estudio; comenzó con la remoción del exudado resinoso (ERES) usando como disolvente diclorometano, para continuar con el secado y la molienda de la planta sin resina. Posteriormente el material se sometió a extracción usando disolventes de polaridad creciente, comenzando con hexano (EHEX), seguido de diclorometano (EDCM), acetato de etilo (EACET) y metanol (EMEOH), para posterior evaluación microbiológica de cada uno de ellos. Las dos especies del género Caiophora (C. sepiaria y C. rahmeri) presentaron actividad contra bacterias Gram (+). Con la bacteria Gram (-) E. coli, mostraron actividad los aceites esenciales de ambas especies. Además C. rahmeri presentó también efecto con los extractos apolares y polares frente a E. coli. El género Senecio representado por Senecio nutans, Senecio adenophyllus y Senecio trifurcifolius mostró actividad antimicrobiana de amplio espectro, tanto para microorganismos Gram (+) como Gram (-). Al comparar los extractos obtenidos de estas especies, Senecio nutans y Senecio adenophyllus tienen mayor actividad antimicrobiana que el Senecio trifurcifolius. La actividad antimicrobiana en S. nutans la podemos atribuir tanto al exudado resinoso, a los extractos y especialmente al aceite esencial de esta especie. El Senecio nutans fue el único en presentar actividad contra la levadura Saccharomyces cerevisiae, con una concentración mínima inhibitoria (CMI) de 180 µg/mL. Los extractos apolares como el exudado resinoso y el aceite esencial de Parastrephia lúcida presentaron actividad antimicrobiana, siendo superior la del exudado resinoso mostrando un efecto de amplio espectro, tanto con microorganismos Gram (+): M. flavus, B. subtilis y con Gram (-): E. coli y K. pneumoniae teniendo una CMI para el exudado resinoso de 160, 70, 100, 170 µg/mL respectivamente; y para el aceite esencial 160, 160, 160 µg/mL con los mismos microorganismos. Myrica pavonis, presentó actividad antimicrobiana en el exudado resinoso y aceite esencial, mostrando una actividad de amplio espectro, tanto con microorganismos Gram (+): B. subtilis; como Gram (-): E. coli. El exudado resinoso presenta una CMI de 170 y 90 µg/mL para B. subtilis y E. coli respectivamente. Referente a la actividad antioxidante se puede concluir que de las plantas que fueron estudiadas sólo el S. trifurcifolius presentó capacidad antioxidante teniendo un efecto inhibitorio 15,7%, determinada por el método de xantina oxidasa (XO). En las siete plantas en estudio se observó que el aceite esencial obtenido de cada una de ellas fue el que presentó mejor actividad antimicrobiana, confirmando su uso popular y contribuyendo al conocimiento científico de estas especies pre-andinas y de la zona del altiplano, desde el punto de vista químico y farmacológico.

Application of principal component-radial basis function neural networks (PC-RBFNN) for the detection of water-adulterated bayberry juice by near-infrared spectroscopy / 浙江大学学报（英文版）（B辑：生物医学和生物技术）

Near-infrared (NIR) spectroscopy combined with chemometrics techniques was used to classify the pure bayberry juice and the one adulterated with 10% (w/w) and 20% (w/w) water. Principal component analysis (PCA) was applied to reduce the dimensions of spectral data, give information regarding a potential capability of separation of objects, and provide principal component (PC) scores for radial basis function neural networks (RBFNN). RBFNN was used to detect bayberry juice adulterant. Multiplicative scatter correction (MSC) and standard normal variate (SNV) transformation were used to preprocess spectra. The results demonstrate that PC-RBFNN with optimum parameters can separate pure bayberry juice samples from water-adulterated bayberry at a recognition rate of 97.62%, but cannot clearly detect water levels in the adulterated bayberry juice. We conclude that NIR technology can be successfully applied to detect water-adulterated bayberry juice.