scholarly journals Cytotoxic effect of palladium (II) inclusion compounds in beta-cyclodextrin

Biomédica ◽  
2016 ◽  
Vol 36 (4) ◽  
pp. 603 ◽  
Author(s):  
Nancy Jaimes ◽  
Siham Salmen ◽  
Melisa Carolina Colmenares ◽  
Ana Esperanza Burgos ◽  
Lenka Tamayo ◽  
...  

Introducción. Las tiosemicarbazonas y sus complejos de paladio (II) poseen actividad antineoplásica con pocos efectos secundarios, por lo cual se las considera como una nueva alternativa terapéutica. Sin embargo, existen diferencias en los rangos de la concentración inhibitoria media (CI50) asociada a la divergencia estructural y la solubilidad de los complejos, así como a la sensibilidad de los blancos celulares. La inclusión de fármacos en la beta-ciclodextrina con fines terapéuticos ha mejorado su solubilidad y estabilidad, pero los efectos de su combinación con los complejos de paladio (II) y las tiosemicarbazonas no se han comprobado aún.Objetivo. Estudiar el efecto citotóxico de los complejos de paladio en la beta-ciclodextrina.Materiales y métodos. La actividad citotóxica de los complejos de paladio en la beta-ciclodextrina se evaluó en la línea celular de cáncer de mama (MCF-7), empleando el método de la sulforodamina B.Resultados. Los ligandos MePhPzTSC y Ph2PzTSC, sus complejos de paladio (II) libres e incluidos en la beta-ciclodextrina y el cisplatino mostraron actividad citotóxica en la línea celular MCF-7; sin embargo, la citotoxicidad fue mayor con la inclusión en la beta-ciclodextrina ([Pd(MePhPzTSC)2]•ß-CD y [Pd(Ph2PzTSC)2]•ß-CD). La concentración inhibitoria media (CI50) para estos complejos se obtuvo en concentraciones de 0,14 y 0,49 μM, y con dosis hasta cinco veces inferiores comparadas con las concentraciones de los ligandos libres (1,4 y 2,9 μM), de los complejos de paladio (II) libres (0,57 y 1,24 μM) y del cisplatino (6,87 μM).Conclusiones. El uso de la beta-ciclodextrina mejoró significativamente la actividad citotóxica de las tiosemicarbazonas y sus complejos de paladio (II), lo cual probablemente está asociado al incremento de la solubilidad y biodisponibilidad del compuesto, estrategia que se puede sugerir para el diseño de futuros fármacos antineoplásicos.

Marine Drugs ◽  
2021 ◽  
Vol 19 (3) ◽  
pp. 123
Author(s):  
Yu-Chi Lin ◽  
Yi-Jen Chen ◽  
Shu-Rong Chen ◽  
Wan-Ju Lien ◽  
Hsueh-Wei Chang ◽  
...  

Application of LC-MS/MS-based molecular networking indicated the ethanol extract of octocoral Asterospicularia laurae is a potential source for the discovery of new xenicane derivatives. A natural product investigation of this soft coral resulted in the isolation of four new xenicane diterpenoids, asterolaurins O‒R (1‒4), together with six known compounds, xeniolide-A (5), isoxeniolide-A (6), xeniolide-B (7), 7,8-epoxyxeniolide-B (8), 7,8-oxido-isoxeniolide-A (9), and 9-hydroxyxeniolide-F (10). The structures of isolated compounds were characterized by employing spectroscopic analyses, including 2D-NMR (COSY, HMQC, HMBC, and NOESY) and high-resolution electrospray ionization mass spectrometry (HRESIMS). Asterolaurin O is the first case of brominated tricarbocyclic type floridicin in the family Xeniidae. Concerning bioactivity, the cytotoxic activity of those isolates was evaluated. As a result, compounds 1 and 2 demonstrated a selective cytotoxic effect against the MCF-7 cell line at IC50 of 14.7 and 25.1 μM, respectively.


2021 ◽  
Vol 7 (7) ◽  
pp. 67004-67014
Author(s):  
Camila Franco ◽  
Manoela Lunkes Silva ◽  
Altevir Rossato Viana ◽  
Aline Ferreira Ourique ◽  
Luciana Maria Fontanari Krause

Novas pesquisas indicam que anti-inflamatórios podem ser aplicados como agentes anti-cancerígenos como indometacina para hepatocarcinoma humano, canceres de colon e estômago. Como sabe-se, indometacina possui efeitos adversos gastrointestinais, cardiovasculares e renais. Uma vez que cancer de mama tem alta incidência e não há estudo da indometacina carreada em nanopartículas para esta aplicação, este estudo envolve o desenvolvimento de nanocapsulas de poli-epsilon-caprolactona carregadas com indometacina para a redução de citotoxicidade como agente quimioprotetor para cancer de mama. O nanocarreador foi preparado por método de deposição interfacial e sua caracterização foi realizada por determinação de pH, diâmetro médio e índice de polidispersão por espalhamento dinâmico de luz, potencial zeta por mobilidade eletroforética, eficiência de encapsulação por método de cromatografia líquida de alta eficiência e seu ensaio de citotoxicidade com linhagem de células queratinócitos (HaCaT) e células de cancer de mama (MCF-7). As formulações branca (C-NC) e contendo indometacina (Ind-OH-NC) mostraram leve pH ácido, diâmetros em torno de 200 nm e PDI0,2 com potencial zeta em torno de -20 mV e eficiência de encapsulação de 99% (1 mg.mL-1), cujo coeficiente de distribuição indicou efeito de permeação e retenção (efeito EPR). Ambas formulações não foram citotóxicas às células HaCaT, provando serem seguras às células normais e Ind-OH-NC teve uma permeação concentração e tempo-dependente e teve eficácia em reduzir a viabilidade celular da linhagem MCF-7.


2021 ◽  
pp. 33-34
Author(s):  
Наталья Александровна Кольберг ◽  
Сергей Леонидович Тихонов ◽  
Наталья Валерьевна Тихонова ◽  
Светлана Александровна Леонтьева

Разработана технология БАД из фабрициевой сумки цыплят-бройлеров. Доказано, что полученная БАД на нарушает жизнеспособность клеток млекопитающих и не проявляет цитотоксических свойств на метаболизм здоровых клеток, что свидетельствует о ее безопасности. Доказан выраженный цитотоксический эффект БАД на опухолевые клетки линии MCF-7. The technology of dietary supplements from the factory bag of broiler chickens has been developed. It was proved that the obtained dietary supplement does not violate the viability of mammalian cells and does not exhibit cytotoxic properties on the metabolism of healthy cells, which indicates its safety. A pronounced cytotoxic effect of dietary supplements on MCF-7 tumor cells has been proven.


2018 ◽  
Vol Volume 11 ◽  
pp. 7669-7677 ◽  
Author(s):  
Maryam Hamzeloo-Moghadam ◽  
Mahmoud Aghaei ◽  
Mohammad Hossein Abdolmohammadi ◽  
Amir Khalaj ◽  
Faranak Fallahian

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1501 ◽  
Author(s):  
Hamdoon A. Mohammed ◽  
Mohsen S. Al-Omar ◽  
Mahmoud Zaki El-Readi ◽  
Ahmad H. Alhowail ◽  
Maha A. Aldubayan ◽  
...  

Background: This study is designed to discover a method for delivering an efficient potent pheophytin a (pheo-a) into more absorbed and small polymeric ethyl cellulose (EC) microparticles. Methods: Silica gel and Sephadex LH-20 columns were used to isolate pheo-a from the chloroform extract of the edible plant, Suaeda vermiculata. Pheo-a was incorporated into EC microparticles using emulsion-solvent techniques. The antioxidant activity of pheo-a microparticles was confirmed by the level of superoxide radical (SOD), nitric oxide (NO), and reducing power (RP) methods. Meanwhile, the cytotoxic effect of the product was investigated on MCF-7 cells using MTT assay. Results: Pheo-a was isolated from S. vermiculata in a 12% concentration of the total chloroform extract. The structures were confirmed by NMR and IR spectroscopic analysis. The formulated microparticles were uniform, completely dispersed in the aqueous media, compatible as ingredients, and had a mean diameter of 139 ± 1.56 µm as measured by a particle size analyzer. Pheo-a demonstrated a valuable antioxidant activity when compared with ascorbic acid. The IC50 values of pheo-a microparticles were 200.5 and 137.7 µg/mL for SOD, and NO respectively. The reducing power of pheo-a microparticles was more potent than ascorbic acid and had a 4.2 µg/mL for IC50 value. Pheo-a microparticles did not show notable cytotoxicity on the MCF-7 cell line (IC50 = 35.9 µg/mL) compared with doxorubicin (IC50 = 3.2 µg/mL). Conclusions: the results showed that water-soluble pheo-a microparticles were prepared with a valuable antioxidant activity in a wide range of concentrations with a noteworthy cytotoxic effect.


Steroids ◽  
2020 ◽  
Vol 160 ◽  
pp. 108656 ◽  
Author(s):  
Ahmed Ismail ◽  
Ahmed S. Doghish ◽  
Bakheet E. M. Elsadek ◽  
Salama A. Salama ◽  
Amr D. Mariee

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