Chlorella sorokiniana and Chlorella minutissima exhibit antioxidant potentials, inhibit cholinesterases and modulate disaggregation of ß-amyloid fibrils

BACKGROUND: Microalgae are aquatic chlorophyll-containing organisms comprising unicellular microscopic forms, and their biomasses are potential sources of bioactive compounds, biofuels and food-based products. However, the neuroprotective effects of microalgal biomass have not been fully explored. In this study, biomass from two Chlorella species was characterized, and their antioxidant, anticholinesterase and anti-amyloidogenic activities were investigated. RESULTS: GC­MS analysis of the extracts revealed the presence of some phenols, sterols, steroids, fatty acids and terpenes. Ethanol extract of Chlorella sorokiniana (14.21 mg GAE/g) and dichloromethane extract of Chlorella minutissima (20.65 mg QE/g) had the highest total phenol and flavonoid contents, respectively. All the extracts scavenged 2,2-diphenyl-1-picrylhydrazyl, 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonate) and hydroxyl radicals. The highest metal chelating activity of the extracts was observed in the ethanol extracts of C. minutissima (102.60 µg/mL) and C. sorokiniana (107.84 µg/mL). Furthermore, the cholinesterase inhibitory activities of the extracts showed that ethanol extract of C. sorokiniana (13.34 µg/mL) exhibited the highest acetylcholinesterase inhibitory activity, while dichloromethane extract of C. minutissima (11.78 µg/mL) showed the highest butyrylcholinesterase inhibitory activity. Incubation of the ß-amyloid protein increased the aggregation of amyloid fibrils after 96 h. However, ethanol extract of C. sorokiniana and C. minutissima inhibited further aggregation of Aß1­42 and caused disaggregation of matured protein fibrils compared to the control. This study reveals the modulatory effects of C. sorokiniana and C. minutissima extracts on some mediators of Alzheimer's disease and provides insights into their potential benefits as functional food, nutraceutics or therapeutic agent for the management of this neurodegenerative disease.

Anti-biofilm activity against Staphylococcus aureus MRSA and MSSA of neolignans and extract of Piper regnellii

ABSTRACT Many infections worldwide are associated with bacterial biofilms. The effects of isolated neolignans (conocarpan and eupomathenoid-5) and the dichloromethane extract of Piper regnellii (Miq.) C. DC., Piperaceae, were tested against isolates of methicillin-resistant Staphylococcus aureus and methicillin-sensitive S. aureus biofilms and S. aureus planktonic cells. The dichloromethane extract presented better results than isolated neolignans against all of the biofilms tested, with a minimum inhibitory concentration <400 µg/ml for preformed biofilms and minimal biofilm inhibitory concentration of 15.6 µg/ml for biofilm formation. The minimum inhibitory concentration to planktonic cells was <12.5 µg/ml. These results indicate a good effect of the dichloromethane extract against methicillin-resistant S. aureus and methicillin-sensitive S. aureus biofilms and efficient prophylaxis.

Actividad antiinflamatoria y analgésica de un extracto orgánico del alga roja Galaxaura rugosa (J. Ellis & Solander) J.V. Lamouroux / Anti-inflammatory and analgesic activity of an organic extract from the red alga Galaxaura rugosa (J. Ellis & Solander) J.V. Lamouroux

INTRODUCCIÓN: el alga roja Galaxaura rugosa (J. Ellis & Solander) J.V. Lamouroux (Galaxauraceae) es una de las especies más abundantes en la plataforma rocosa del arrecife coralino del archipiélago cubano, sin embargo, poco se conoce de sus propiedades farmacológicas. OBJETIVOS: evaluar la actividad antiinflamatoria y analgésica del extracto en diclorometano del alga roja G. rugosa, así como la composición fitoquímica de esta especie. MÉTODOS: las algas se colectaron en el litoral norte de La Habana. La caracterización fitoquímica del alga se realizó según el Método de Chabra. Para la preparación del extracto se sometió la muestra a extracción Soxhlet con diclorometano a 40 ºC. La actividad antiinflamatoria tópica se estudió en el modelo de edema de la oreja inducido por aceite de Croton en ratones machos OF-1, a las dosis de 10*10-3; 0,125; 0,25; 0,5; 1 y 2 mg/oreja. Se evaluó también la actividad analgésica del extracto en el modelo de contorsiones inducidas por ácido acético al 0,8 %, por vía intraperitoneal (i.p.), a las dosis de 3; 6; 12,5; 25 y 100 mg/kg. RESULTADOS: G. rugosa presentó en su composición fitoquímica compuestos grasos, lactónicos, triterpénicos y/o esteroidales y carbohidratos. El extracto en diclorometano de G. rugosa a partir de la dosis de 0,125 mg/oreja presenta una potente actividad antiinflamatoria (superior al 40 %). El extracto logró reducir las contorsiones en más de un 75 % a partir de la dosis de 6 mg/kg. CONCLUSIONES: los resultados presentados demuestran que el extracto en diclorometano del alga roja G. rugosaestá constituido por una mezcla de compuestos capaces de inhibir con una elevada eficacia farmacológica la respuesta inflamatoria aguda y el dolor inducido por agentes químicos.

INTRODUCTION: the red alga Galaxaura rugosa (J. Ellis & Solander) J.V. Lamouroux (Galaxauraceae) is one of the most abundant species on the rocky platform of the Cuban coral reef. However, little is known about its pharmacological properties. OBJECTIVES: evaluate the anti-inflammatory and analgesic activity of a dichloromethane extract from the red alga G. rugosa and determine the phytochemical composition of the species. METHODS: the algae were collected from the northern coast of Havana. Phytochemical characterization of the alga was performed using Chabra's method. The extract was obtained with a Soxhlet device with dichloromethane at 40 ºC. Topical anti-inflammatory activity was studied with the croton oil ear edema test model in male OF-1 mice at doses of 10*10-3, 0.125, 0.25, 0.5, 1 and 2 mg/ear. The analgesic activity of the extract was evaluated on a model of writhing induced by 0.8 % acetic acid administered intraperitoneally (i.p.) at doses of 3, 6, 12.5, 25 and 100 mg/kg. RESULTS: phytochemical analysis of G. rugosa revealed the presence of fatty, lactonic, triterpenic and/or steroidal compounds, as well as carbohydrates. The dichloromethane extract of G. rugosa at the dose of 0.125 mg/ear displayed a potent anti-inflammatory activity (above 40 %). The extract reduced writhing by more than 75 % with a dose of 6 mg/kg. CONCLUSIONS: results show that dichloromethane extract of the red alga G. rugosa is composed of a mixture of compounds capable of inhibiting the acute inflammatory response and the pain induced by chemical agents with a high pharmacological efficacy. composed of a mixture of compounds capable of inhibiting the acute inflammatory response and the pain induced by chemical agents with a high pharmacological efficacy.

Antitumor Activity of Dichloromethane Extract from Salvia plebeia and Induction of Apoptosis on K562 Cells / 中草药·英文版

Objective To study the antitumor activity of extract from Salvia plebeia and investigate whether the extract induce apoptosis of K562 cells. Methods The aqueous, petroleum ether, dichloromethane (CH2Cl2), ethyl acetate, and butanol extracts were prepared from the aerial parts of 5. plebeia. Taking fluorouracil as reference, the cytotoxic activities of these extracts on HeLa, A549, SGC-7901, HCT-116, K562, LoVo, DU-145, and HepG2 cells were evaluated. To clarify the apoptosis of K562 cells induced by CH2Cl2 extract, the methods of Hoechst 33258 staining, flow cytometry assay, and DNA ladder assay were investigated. Results The CH2Cl2 extract showed the most potent cytotoxic effect against K562 cells, with an IC50 < 15 μg/mL for 3 d treatment. The characteristic apoptotic symptoms such as DNA fragmentation and chromatin condensation were also observed in the K562 cells. Conclusion The CH2Cl2 extract from S. plebeia may inhibit the cancer cell proliferation by inducing cell apoptosis.

Vasorelaxant effect of Hyptis fruticosa Salzm. ex Benth., Lamiaceae, dichloromethane extract on rat mesenteric artery / Efeito vasorelaxante do extrato diclorometano de Hyptis fruticosa Salzm. ex Benth., Lamiaceae, em artéria mesentérica de ratos

Vasorelaxant effect of Hyptis fruticosa dichloromethane extract (HFDE) on isolated rings of rat mesenteric artery was evaluated in this study. In intact rings, HFDE (0.1-3000 µg/mL) induced concentration-dependent vasorelaxations (Emax = 119±14 percent; n = 6) of phenylephrine tonus that were not modified after endothelium removal (Emax = 116±6 percent; n = 6), after KCl 20 mM (Emax = 135±9 percent; n = 6) or in rings pre-contracted with KCl 80 mM (Emax = 125±4 percent; n = 6). In endothelium denuded rings, HFDE (300 or 1000 µg/mL) inhibited contractions induced by CaCl2 (maximal inhibition = 25±7 percent and 95±1 percent; respectively). Furthermore, HFDE promoted an additional vasorelaxation (15±3 percent; n = 7) after maximal response of 10 µM nifedipine (78±3 percent; n = 7). In conclusion, HFDE induces vasorelaxant effect through an endothelium-independent pathway, which appears to be due in major part to inhibition of the Ca2+ influx through voltage-operated Ca2+ channels.

O efeito vasorelaxante do extrato diclorometano de Hyptis fruticosa Salzm. ex Benth., Lamiaceae (HFDE), em anéis isolados de artéria mesentérica de ratos foi avaliado nesse estudo. Em anéis intactos, pré-contraídos com fenilefrina (10 µM), HFDE (0,1-3000 µg/mL) induziu vasorelaxamento de maneira dependente de concentração (Emax = 119±14 por cento; n = 6), o qual não foi afetado após remoção do endotélio (Emax = 116±6 por cento; n = 6), após KCl 20 mM (Emax = 135±9 por cento; n = 6) ou em anéis pré-contraídos com KCl 80 mM (Emax = 125±4 por cento; n = 6). Em anéis sem endotélio, HFDE (300 ou 1000 µg/mL) inibiu as contrações induzidas por CaCl2 (inibição máxima = 25±7 por cento e 95±1 por cento, respectivamente). Além disso, HFDE promoveu um vasorelaxamento adicional (15±3 por cento; n = 7) sobre o relaxamento máximo de 10 µM de nifedipina (78±3 por cento, n = 7). Em conclusão, HFDE induz efeito vasorelaxante através de uma via independente de endotélio, possivelmente devido à inibição do influxo de Ca2+ através de canais de Ca2+ operados por voltagem.

Antifungal Activity of the Extract from Paeonia japonica against Candida albicans / 대한의진균학회지

BACKGROUND: Candida albicans is one of the normal flora of the skin, mucous membranes and gastrointestinal tract. Vaginal candidiasis remains a significant problem in women of childbearing age, majority of the cases are caused by C. albicans and recurrence is common in spite of topical treatment. OBJECTIVE: The purpose of this study is to develop the antifungal agent from the medicinal herbs traditionally used in Korea. METHODS: In this study, extracts from roots of Paeonia japonica were examined for antifungal activities against C. albicans. Dried roots of Paeonia japonica were extracted with dichloromethane, methanol, water respectively and serially. Liquid column chromatography and thin layer chromatography were used to separate the fractions with antifungal activity, and mass spectrometric analysis was done to determine the mass. RESULTS: Dichloromethane extract showed the highest antifungal activity aginst C. albicans. Result of fractionation and mass spectrometric analysis revealed that there were six materials: propanal, cytidine, hexadecanoic acid, cholesterol, octadecanoic acid and a unidentified material. CONCLUSION: Dichloromethane extract from Paeonia japonica could be a candidate for a new antifungal agent against C. albicans.