Trichothecene macrolides from the endophytic fungus Paramyrothecium roridum and their cytotoxic activity.

The chemical investigation of the secondary metabolites of Paramyrothecium roridum (homotypic synonym: Myrothecium roridum), an endophytic fungus isolated from the medicinal plant Morinda officinalis, led to the isolation of twelve cytotoxic trichothecene macrolides, including two new ones, named myrothecines H and I. The structures of the new macrolides were elucidated by extensive spectroscopic measurements analyses. In addition, the cytotoxic activities of these compounds were evaluated against SF-268, NCI-H460, and HepG-2 tumor cell lines, and all isolated compounds (1-12) exhibited significant cytotoxic activity with the IC50 ranging from 0.0002-16.2 µM. Moreover, the inhibitory activity of myrothecines H and I was evidenced by inducing phosphorylation of JNK (c-Jun N-terminal protein kinase) protein and the PARP (poly ADP-ribose polymerase) cleavage, and eventually induce apoptosis of HepG-2 cells. The results indicated that myrothecines H and I could be applied as chemotherapeutic agents.

Four new metabolites from the endophytic fungus Diaporthe lithocarpus A740.

One new benzophenone derivative, named tenllone I (1), two new eremophilane derivatives lithocarins B (2) and C (3), and a new monoterpentoid lithocarin D (4), together with two know compounds (5 and 6) were isolated from the endophytic fungus Diaporthe lithocarpus A740. All of the structures for these new compounds were fully characterized and established on the basis of extensive spectroscopic interpretation. In addition, all the isolated compounds were evaluated in vitro for their cytotoxic activity. Compounds 2, 3, and 5 showed weak inhibitory activities against tumor cell lines.

Two New Metabolites from the Endophytic Fungus Alternaria sp. A744 Derived from Morinda officinalis.

Two new compounds isobenzofuranone A (1) and indandione B (2), together with eleven known compounds (3-13) were isolated from liquid cultures of an endophytic fungus Alternaria sp., which was obtained from the medicinal plant Morinda officinalis. Among them, the indandione (2) showed a rarely occurring indanone skeleton in natural products. Their structures were elucidated mainly on the basis of extensive spectroscopic data analysis. All of the compounds were evaluated with cytotoxic and α-glucosidase inhibitory activity assays. Compounds 11 and 12 showed significant inhibitory activities against four tumor cell lines; MCF-7, HepG-2, NCI-H460 and SF-268, with IC50 values in the range of 1.91-9.67 µM, and compounds 4, 5, 9, 10, 12 and 13 showed excellent inhibitory activities against α-glucosidase with IC50 values in the range of 12.05-166.13 µM.

Three new highly-oxygenated metabolites from the endophytic fungus Cytospora rhizophorae A761.

Cytosporaphenones A-C, one new polyhydric benzophenone and two new naphtopyrone derivatives, along with eight known ones, were isolated from Cytospora rhizophorae, an endophytic fungus from Morinda officinalis. Their structures were fully characterized by means of detailed spectroscopic analysis and X-ray single crystal diffraction. To our knowledge, the three new compounds were the most highly oxygenated metabolites of their families discovered in nature. Moreover, all of the compounds were evaluated for in vitro cytotoxic activities against MCF-7, NCI-H460, HepG-2 and SF-268 tumor cell lines, and the new compound 1 exhibited weak growth inhibitory activity against the tumor cell lines MCF-7 and HepG-2 with IC50 values of 70 and 60µM, respectively.

Actividad antimicrobiana y toxicidad frente a Artemia salina del extracto diclorometánico de raíces de Morinda royoc L / Antimicrobial action and toxicity against Artemia salina of the dichlormethane extract from Morinda royoc L roots

Introducción: las plantas son una fuente de diversidad natural por la gran variedad de compuestos que sintetizan. Particularmente las antraquinonas resultan un importante grupo de metabolitos secundarios con actividad antimicrobiana y antioxidante. Objetivos: evaluar la actividad antimicrobiana del extracto diclorometánico de raíces de Morinda royoc L, así como su toxicidad contra Artemia salina. Métodos: la actividad antimicrobiana se determinó utilizando el método de microdilución en placa de 96 pozos. Se evaluó la actividad del extracto frente a 7 aislados clínicos de Candida spp. y frente a las bacterias Staphylococcus aureus resistente a meticilina, Staphylococcus aureus ATCC 12598, Enterococus faecales, Escherichia coli, Acinetobacter baumanii, Pseudomonas aeruginosa y Klebsiella pneumoniae. La toxicidad del extracto se evaluó mediante el ensayo de letalidad con A salina. Resultados: el extracto crudo fue activo frente a todas las especies de Candida evaluadas. La concentración mínima inhibitoria más baja fue 1,95 µg/mL. El extracto mostró fuerte actividad inhibitoria contra S. aureus, E faecales, y E coli. El valor más bajo de concentración mínima inhibitoria obtenido fue 31,25 µg/mL. El extracto presentó una toxicidad moderada hacia A salina. Conclusiones: los resultados obtenidos demuestran el potencial del extracto diclorometánico de raíces de M. royoc L en el tratamiento de infecciones causadas por bacterias y hongos(AU)

Introduction: plants are a source of natural diversity because of the great variety of compounds that they synthesize. Anthraquinones in particular are an important group of secondary metabolites characterized by their antimicrobial and antioxidant action. Objectives: to evaluate the antimicrobial action of dichloromethane extract from Morinda royoc L roots as well as its toxicity against Artemia salina. Methods: the antimicrobial action was determined by using the brooth microdilution in 96-well plate. The extract action against 7 Candida spp clinical isolates and against bacteria such as methicillin-resistant Staphylococcus aureus, Staphylococcus aureus ATCC 12598, Enterococus faecales, Escherichia coli, Acinetobacter baumanii, Pseudomonas aeruginosa and Klebsiella pneumoniae was evaluated. The extract toxicity was measured using brine shrimp (Artemia salina) lethality test. Results: the crude extract proved to be active against all the tested Candida species. The lowest minimal inhibitory concentration was 1,95 µg/mL. The extract showed strong inhibitory action against S aureus, E. faecales, and E coli. The lowest minimal inhibitory concentration was 31.25 µg/mL. The extract presented moderate toxicity against A salina. Conclusions: the results showed the potentialities of dichloromethane extract from M. royoc L. roots for the treatment of bacterial and fungal infections(AU)

Actividad antimicrobiana y toxicidad frente a Artemia salina del extracto diclorometánico de raíces de Morinda royoc L / Antimicrobial action and toxicity against Artemia salina of the dichlormethane extract from Morinda royoc L roots

Introducción: las plantas son una fuente de diversidad natural por la gran variedad de compuestos que sintetizan. Particularmente las antraquinonas resultan un importante grupo de metabolitos secundarios con actividad antimicrobiana y antioxidante. Objetivos: evaluar la actividad antimicrobiana del extracto diclorometánico de raíces de Morinda royoc L, así como su toxicidad contra Artemia salina. Métodos: la actividad antimicrobiana se determinó utilizando el método de microdilución en placa de 96 pozos. Se evaluó la actividad del extracto frente a 7 aislados clínicos de Candida spp. y frente a las bacterias Staphylococcus aureus resistente a meticilina, Staphylococcus aureus ATCC 12598, Enterococus faecales, Escherichia coli, Acinetobacter baumanii, Pseudomonas aeruginosa y Klebsiella pneumoniae. La toxicidad del extracto se evaluó mediante el ensayo de letalidad con A salina. Resultados: el extracto crudo fue activo frente a todas las especies de Candida evaluadas. La concentración mínima inhibitoria más baja fue 1,95 µg/mL. El extracto mostró fuerte actividad inhibitoria contra S. aureus, E faecales, y E coli. El valor más bajo de concentración mínima inhibitoria obtenido fue 31,25 µg/mL. El extracto presentó una toxicidad moderada hacia A salina. Conclusiones: los resultados obtenidos demuestran el potencial del extracto diclorometánico de raíces de M. royoc L en el tratamiento de infecciones causadas por bacterias y hongos

Introduction: plants are a source of natural diversity because of the great variety of compounds that they synthesize. Anthraquinones in particular are an important group of secondary metabolites characterized by their antimicrobial and antioxidant action. Objectives: to evaluate the antimicrobial action of dichloromethane extract from Morinda royoc L roots as well as its toxicity against Artemia salina. Methods: the antimicrobial action was determined by using the brooth microdilution in 96-well plate. The extract action against 7 Candida spp clinical isolates and against bacteria such as methicillin-resistant Staphylococcus aureus, Staphylococcus aureus ATCC 12598, Enterococus faecales, Escherichia coli, Acinetobacter baumanii, Pseudomonas aeruginosa and Klebsiella pneumoniae was evaluated. The extract toxicity was measured using brine shrimp (Artemia salina) lethality test. Results: the crude extract proved to be active against all the tested Candida species. The lowest minimal inhibitory concentration was 1,95 µg/mL. The extract showed strong inhibitory action against S aureus, E. faecales, and E coli. The lowest minimal inhibitory concentration was 31.25 µg/mL. The extract presented moderate toxicity against A salina. Conclusions: the results showed the potentialities of dichloromethane extract from M. royoc L. roots for the treatment of bacterial and fungal infections

Anticancer activity of fungal taxol derived from Botryodiplodia theobromae Pat., an endophytic fungus, against 7, 12 dimethyl benz(a)anthracene (DMBA)-induced mammary gland carcinogenesis in Sprague Dawley rats.

Breast cancer is the second most prevalent cancer worldwide and their incidence increases gradually. Taxol (paclitaxel), a potent anticancer drug, is naturally isolated from the bark of the Pacific yew. Taxol is widely used in the treatment of ovarian, lung and breast cancer. The increased demand for taxol, coupled with its limited availability from the protected Pacific yew, has had researchers scrambling for alternate sources. The purpose of the present study is to investigate chemopreventive effect of fungal taxol derived from a novel endophytic fungus Botryodiplodia theobromae Pat., isolated from a medicinal plant Morinda citrifolia Linn. The fungal taxol is found to be active against the 7, 12 dimethyl benz(a)anthracene (DMBA)-induced mammary gland carcinogenesis in Sprague dawley rats. The enzymic and non-enzymic antioxidants i.e. superoxide dismutase (SOD), catalase (CAT), glutatione peroxidase (GPx), glutatione-S-transferase (GST), reduced glutathione (GSH), vitamin C and vitamin E were evaluated in control and experimental groups. Lipid peroxides levels (LPO) were also tested. Histological analysis of breast tissue was analyzed by haematoxylin and eosin staining to assess the cytoprotective role of fungal taxol active against breast cancer. Immunohistochemical analyses were also performed to evaluate the effect of fungal taxol on the inflammatory marker such as Cyclooxygenase-2 (COX-2) in control and experimental groups. The results showed that the fungal taxol significantly suppresses the DMBA-induced breast cancer in Sprague dawley rats.

Ensayo microbiológico en cápsulas de Morinda citrifolia L. (Noni) comercializadas ambulatoriamente en la ciudad de León en el mes de febrero del 2008 / Microbiological assay in capsules of Morinda citrifolia L. (Noni) commercialized ambulatory in the city of León in February 2008

El presente estudio trata de determinar el límite microbiano en las cápsulas de Noni comercializadas ambulatoriamente en la ciudad de León, así como, cuantificar la presencia de bacterias aerobias mesófilas e identificar presencia de microorganismos patógenos como Staphilococcus áureus, Pseudomona aeuruginosa, Escherichia coli y Salmonella spp. evidenciando la presencia de Hongos y Levaduras.