Study on chemical constituents of sponge Mycale sp.from the South China Sea / 药学实践杂志

Objective To investigate the chemical constituents of marine sponge Mycale sp.collected from the South China Sea.Methods The ethyl acetate extract of the marine sponge Mycale sp.was separated and purified by repeated column chromatography on silica gel, Sephadex LH-20 and reversed-phase high-performance liquid chromatography (RP-HPLC).The structures of these compounds were identified by means of various modern spectroscopic techniques and comparison with their physicochemical properties to reported data.The tumor cell growth inhibitory activities of these compounds against human breast cancer cell lines MCF-7 and human lung cancer cell lines PC9 were tested by Cell Counting Kit-8 (CCK-8) method.Results Ten compounds were isolated and identified as cyclo-(Pro-Ile)(1),cyclo-(Pro-Leu)(2),cyclo-(Ile-Leu)(3),cyclo-(Phe-Pro)(4),cyclo-(Phe-Val)(5),cyclo-(Phe-Leu)(6),cyclo-(Phe-Ile)(7), 2′-deoxythymidine (8), thymine (9), 5-hydroxy-3,4-dimethyl-5-pentyl-2(5H)-furanone (10).These compounds showed weak tumor cell growth inhibitory activities toward cells MCF-7 and PC9 in vitro.Conclusion Compounds 1, 2, 4, 5, 6, 7 and 10 were isolated from the sponge Mycale sp.for the first time.It is the first time to report the antitumor activity evaluation for compounds 1~10.

Actividad antiplasmodial in vivo de las esponjas Mycale laxissima y Clathria echinata / In vivo antiplasmodial activity of Mycale laxissima and Clathria echinata sponges

Introducción: la búsqueda de nuevas sustancias antimaláricas incluye entre sus retos el desarrollo de alternativas para el tratamiento de la malaria cerebral, debido a la alta mortalidad y las deficiencias neurológicas persistentes después del tratamiento con los medicamentos recomendados actualmente. Objetivos: evaluar la actividad de fracciones orgánicas de Mycale laxissima y Clathria echinata en el modelo de malaria cerebral producida por la infección de ratones C57BL/6 con Plasmodium berghei ANKA. Métodos: se evaluaron fracciones orgánicas obtenidas mediante cromatografía flash en fase inversa a partir de los extractos crudos de las dos especies. Se realizó un análisis químico cualitativo para detectar la presencia de saponinas, triterpenos/esteroides y alcaloides en estas fracciones. El efecto esquizonticida de las fracciones se determinó mediante la prueba de supresión de la parasitemia al inicio de la infección. Se evaluaron la supervivencia, los síntomas neurológicos y la reducción del peso corporal en los días subsiguientes. Resultados: las fracciones orgánicas de Mycale laxissima a dosis de 200 mg/kg y Clathria echinata a100 mg/kg no mostraron una disminución sustancial del peso de los animales o muertes hasta el día 4; para las cuales se obtuvieron reducciones significativas de las medianas de la parasitemia de 45 % y 53 %, respectivamente. La fracción de Mycale laxissima a 200 mg/kg produjo un incremento significativo en el tiempo de supervivencia hasta 20 d, mientras los animales tratados con Clathria echinata a 100 mg/kg presentaron una mediana de tiempo de supervivencia de 16 d. Ambos incrementos fueron superiores a 7 d. En este período, los animales tratados con las fracciones orgánicas de Clathria echinata y Mycale laxissima no presentaron los síntomas neurológicos observados en los controles. Esta prolongación de la supervivencia fue similar a la observada en presencia de dosis de 7,5 mg/kg de cloroquina. Conclusiones: las fracciones orgánicas de Mycale laxissima y Clathria echinata mostraron actividades antimaláricas, promisorias en el modelo de infección de ratones C57BL/6 con Plasmodium berghei ANKA, que sugieren el estudio de sus constituyentes químicos activos.

Introduction: the search of new antimalarial compounds comprises, among its challenges, the development of therapeutic alternatives for cerebral malaria; due to the high mortality and neurological deficiencies that persist after treatment with recommended drugs. Objectives: to evaluate the activity of organic fractions of Mycale laxissima and Clathria echinata in the cerebral malaria model of infection of C57BL/6 mice with Plasmodium berghei ANKA. Methods: preparative fractions of both species were obtained by reverse-phase flash chromatography. In order to detect the presence of saponins, triterpenods/steroids and alkaloids, a qualitative chemical analysis was performed. The schyzontocidal effect of the extracts was determined by the suppression test at the beginning of the infection. Survival, neurological symptoms and body weight changes were evaluated in subsequent days. Results: the organic fractions of Mycale laxissima at 200 mg/kg and Clathria echinata at 100 mg/kg showed neither substantial reductions of body weights, nor deaths of animals until day 4; but caused significant reductions of median parasitemia of 45 % and 53 % respectively. The fraction of Mycale laxissima at 200 mg/kg caused a significant increase in the median survival time up to day 20, whereas animals treated with Clathria echinata at 100 mg/kg presented a survival of 16 days. Both increases the survival time 7 days. Neurological alterations were not observed in the groups treated with organic fractions when compared to the control group. This survival extension was similar to the effect of administration of 7.5 mg/kg of chloroquine. Conclusions: the organic fractions of Mycale laxissima and Clathria echinata exhibited promising antimalarial activities in the infection model of C57BL/6 mice with Plasmodium berghei ANKA. This indicates that their active chemical constituents should be studied.

Antitumor components from sponge-derived fungus Penicillium auratiogriseum Sp-19 / 中国海洋药物

Objective To isolate and identify the antitumor bioactive components from the fermentation of the fungus Penicillium auratiogriseum Sp-19 derived from sponge Mycale plumose.Methods The antitumor components were isolated by bioassay-guided fractionation and using solvent extraction,silica gel column chromatography and preparative HPLC.Their structures were established by physicochemical properties and spectral analyses.The cytotoxicities of compounds were evaluated by SRB method.Results and Conclusion Five alkaloid compounds were isolated and identified as fructigenines A(1),deacetyl fructigenines A(2),fructigenines B(3),1,4-benzodiazepine-2,5-diones(4) and cyclopenin(5),respectively.Compound 4 and 5 showed cytotoxicity at the concentration of 3 ?g?mL~(-1)against tsFT210 cell line.