A structural analysis of the differential cytotoxicity of chemicals in the NCI-60 cancer cell lines

Chakravarti, Suman K.; Klopman, Gilles

doi:10.1016/j.bmc.2008.01.024

Cited by 7 publications

(3 citation statements)

References 23 publications

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“…Estas líneas celulares son conocidas como las líneas NCI -60 y están conformadas por células provenientes de ocho melanomas, seis leucemias, ocho cánceres de mama, dos de próstata, nueve de pulmón, siete de cólon, seis de ovarios, ocho de riñón y seis de cáncer del sistema nervioso central. Con los resultados de las pruebas de citotoxicidad se halla la concentración inhibitoria media (IC 50 ) como la requerida para inhibir el crecimiento celular (21).…”

Section: Discussionunclassified

Evaluación biológica de una fracción de la esponja marina Topsentia ophiraphidites del Caribe colombiano

et al. 2013

Rev MVZ Córdoba

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RESUMENObjetivo. Evaluar la actividad antiproliferativa y genotóxica de una fracción con actividad citotóxica obtenida de la esponja marina del Caribe colombiano Topsentia ophiraphidites (Fracción T4). Materiales y métodos. La fracción T4 de la esponja marina Topsentia ophiraphidites fue obtenida en el laboratorio de Productos Naturales Marinos de la Universidad de Antioquia. La actividad antiproliferativa se evaluó mediante ensayos de eficiencia de clonación, función de acumulación y cinética proliferativa por intercambio de cromátidas hermanas (ICH); la actividad genotóxica se evaluó mediante electroforesis en gel de células individuales (Ensayo cometa) e intercambio de cromátidas hermanas (ICH). Todas las pruebas fueron realizadas sobre las líneas celulares Jurkat y CHO. Resultados. La fracción T4 afectó el ciclo celular de las células CHO y mostró daño genotóxica crónico en las células Jurkat. Conclusiones. Se recomienda la evaluación de la fracción T4 en otras líneas celulares derivadas de tumor con el fin de determinar un posible efecto diferencial, además de evaluar otras actividades de tipo antimicrobiano, antimalárico, entre otros.

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Section: Discussionunclassified

Evaluación biológica de una fracción de la esponja marina Topsentia ophiraphidites del Caribe colombiano

et al. 2013

Rev MVZ Córdoba

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“…Moreover, the compounds could be conducting an antiproliferative activity by means of this receptor, this if the extrinsic pathway were considered; however, another way of action would be the intrinsic or mitochondrial pathway where it is related to oxidative stress (Kroemer et al, 2009). To make it clear, according to the GI50 obtained for the rest of the fractions by the Probit test, they are not worthy to be further investigated for bioactivity since their GI50 do not meet the NCI criteria for the development of drugs (Boyd & Paull, 1995;Chakravarti & Klopman, 2008).…”

Section: Characterization Of Sub-fraction M11bmentioning

confidence: 99%

ISOLATION AND IDENTIFICATION OF A NEW ANTIPROLIFERATIVE INDOLOCARBAZOLE ALKALOID DERIVATIVE EXTRACTED FROM FARMED SHRIMP (Litopenaeus vannamei) MUSCLE

García-Romo

Hernández-Zazueta²,

Gálvez-Iriqui³

et al. 2021

J microb biotech food sci

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Farmed shrimp Litopenaeus vannamei, one of the most consumed seafood in the planet, is a source of antiproliferative extracts still to be fully characterized. This study the isolation and identification of these antiproliferative compounds. From a chloroform-soluble extract from shrimp muscle, hexane- and methanol-soluble fractions were obtained and tested for antiproliferative activity (MTT), a bioassay that guided the fractionation and isolation of bioactive fractions using open column chromatography. MeOH-soluble fraction resulted bioactive and was subjected to further fractionation from which one subfraction outstand for being highly active against prostate cancer cell line. Antiproliferative effects were evaluated using colorimetric assays and cell morphology observations. Further chromatographic procedures resulted in sub-fractions from which one was effective in causing DNA damage and F-actin polymerization, which suggests cellular collapse and apoptosis. According to the structural chemical characterization carried out, dioctyl phthalate, eicosapentaenoic acid, and an indolocarbazole alkaloid type of compound were identified. This last compound, which resulted majorly responsible for the bioactivity, was not found reported in the available databases. Pure EPA control was used to compare it with the subfraction, observing greater activity in the subfraction than when EPA was used, suggesting that another compound different from EPA is providing the highest activity; but, more investigation is needed for a full chemical and structural characterization.

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“…Additionally, unlike current anticholinesterase insecticides that are low-hanging fruits stemming from World War II research on nerve gas, cysteine-targeting chemicals are high-hanging fruits for the following reasons. First, most known alkylating agents or electrophiles cannot be used to target the cysteine residue because these agents, such as Michael acceptors [80], can cause significant human toxicity. Second, it is disadvantageous to establish affinity by designing a long-chain molecule such as bis-(7)-tacrine [25] that binds deep in the active-site gorge, because such molecules are associated with a high likelihood that insects will develop resistance through active-site mutations of AChE, as mentioned above.…”

Section: Development Of Cysteine-targeting Insecticidesmentioning

confidence: 99%

Novel and Viable Acetylcholinesterase Target Site for Developing Effective and Environmentally Safe Insecticides

Pang¹,

Brimijoin²,

Ragsdale³

et al. 2012

CDT

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Insect pests are responsible for human suffering and financial losses worldwide. New and environmentally safe insecticides are urgently needed to cope with these serious problems. Resistance to current insecticides has resulted in a resurgence of insect pests, and growing concerns about insecticide toxicity to humans discourage the use of insecticides for pest control. The small market for insecticides has hampered insecticide development; however, advances in genomics and structural genomics offer new opportunities to develop insecticides that are less dependent on the insecticide market. This review summarizes the literature data that support the hypothesis that an insect-specific cysteine residue located at the opening of the acetylcholinesterase active site is a promising target site for developing new insecticides with reduced off-target toxicity and low propensity for insect resistance. These data are used to discuss the differences between targeting the insect-specific cysteine residue and targeting the ubiquitous catalytic serine residue of acetylcholinesterase from the perspective of reducing off-target toxicity and insect resistance. Also discussed is the prospect of developing cysteine-targeting anticholinesterases as effective and environmentally safe insecticides for control of disease vectors, crop damage, and residential insect pests within the financial confines of the present insecticide market.

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A structural analysis of the differential cytotoxicity of chemicals in the NCI-60 cancer cell lines

Cited by 7 publications

References 23 publications

Evaluación biológica de una fracción de la esponja marina Topsentia ophiraphidites del Caribe colombiano

Evaluación biológica de una fracción de la esponja marina Topsentia ophiraphidites del Caribe colombiano

ISOLATION AND IDENTIFICATION OF A NEW ANTIPROLIFERATIVE INDOLOCARBAZOLE ALKALOID DERIVATIVE EXTRACTED FROM FARMED SHRIMP (Litopenaeus vannamei) MUSCLE

Novel and Viable Acetylcholinesterase Target Site for Developing Effective and Environmentally Safe Insecticides

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