scholarly journals Novel Marine Compounds: Anticancer or Genotoxic?

2004 ◽  
Vol 2004 (2) ◽  
pp. 93-98 ◽  
Author(s):  
Jamal M. Arif ◽  
Amal A. Al-Hazzani ◽  
Muhammed Kunhi ◽  
Fahad Al-Khodairy
Keyword(s):  
Clinical Trials ◽  
Anticancer Agents ◽  
Screening Tests ◽  
Tumor Xenograft ◽  
Anticancer Compounds ◽  
Early Exit ◽  
Marine Compounds ◽  
Xenograft Models ◽  
Pharmaceutical Industries ◽  
Carcinogenesis Models

In the past several decades, marine organisms have generously gifted to the pharmaceutical industries numerous naturally bioactive compounds with antiviral, antibacterial, antimalarial, anti-inflammatory, antioxidant, and anticancer potentials. But till date only few anticancer drugs (cytarabine, vidarabine) have been commercially developed from marine compounds while several others are currently in different clinical trials. Majority of these compounds were tested in the tumor xenograft models, however, lack of anticancer potential data in the chemical- and/or oncogene-induced pre-initiation animal carcinogenesis models might have cost some of the marine anticancer compounds an early exit from the clinical trials. This review critically discusses importance of preclinical evaluation, failure of human clinical trials with certain potential anticancer agents, the screening tests used, and choice of biomarkers.

scholarly journals From Seabed to Bedside: A Review on Promising Marine Anticancer Compounds

Biomolecules ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 248 ◽  
Author(s):  
Edina Wang ◽  
Maria Alba Sorolla ◽  
Priya Darshini Gopal Krishnan ◽  
Anabel Sorolla
Keyword(s):  
Anticancer Agents ◽  
Defense Mechanisms ◽  
Chemical Engineering ◽  
Anticancer Compounds ◽  
Current State ◽  
Cancer Models ◽  
Tumor Selectivity ◽  
Marine Compounds ◽  
New Methodologies ◽  
Marine Bioactives

The marine environment represents an outstanding source of antitumoral compounds and, at the same time, remains highly unexplored. Organisms living in the sea synthesize a wide variety of chemicals used as defense mechanisms. Interestingly, a large number of these compounds exert excellent antitumoral properties and have been developed as promising anticancer drugs that have later been approved or are currently under validation in clinical trials. However, due to the high need for these compounds, new methodologies ensuring its sustainable supply are required. Also, optimization of marine bioactives is an important step for their success in the clinical setting. Such optimization involves chemical modifications to improve their half-life in circulation, potency and tumor selectivity. In this review, we outline the most promising marine bioactives that have been investigated in cancer models and/or tested in patients as anticancer agents. Moreover, we describe the current state of development of anticancer marine compounds and discuss their therapeutic limitations as well as different strategies used to overcome these limitations. The search for new marine antitumoral agents together with novel identification and chemical engineering approaches open the door for novel, more specific and efficient therapeutic agents for cancer treatment.

Cytotoxic Activity and DNA Binding Property of New Aminopyrimidine Derivatives

2020 ◽  
Vol 17 (5) ◽  
pp. 640-654
Author(s):  
Hamidreza Akrami ◽  
Bibi Fatemeh Mirjalili ◽  
Omidreza Firuzi ◽  
Azadeh Hekmat ◽  
Ali Akbar Saboury ◽  
...  
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Lymphoblastic Leukemia ◽  
Cd Spectroscopy ◽  
Myelogenous Leukemia ◽  
Breast Adenocarcinoma ◽  
Binding Property ◽  
Anticancer Compounds ◽  
Calf Thymus ◽  
Dna Binding Property

Background: Chromene and anilinopyrimidine heterocyclics are attractive anticancer compounds that have inspired many researchers to design novel derivatives bearing improved anticancer activity. Methods: A series of pyrimidine-fused benzo[f]chromene derivatives 6a-x were synthesized as anticancer hybrids of 1H-benzo[f]chromenes and anilinopyrimidines. The inhibitory activity of the synthesized compounds 6a-x against cell viability of human chronic myelogenous leukemia (K562), human acute lymphoblastic leukemia (MOLT-4) and human breast adenocarcinoma (MCF-7) cell lines was evaluated using MTT assay. The interaction of the most promising compound with calf-thymus DNA was also studied using spectrometric titrations and Circular Dichroism (CD) spectroscopy. Results: Most compounds showed promising activity against tested cell lines. Among them, 2,4- dimethoxyanilino derivative 6g exhibited the best profile of activity against tested cell lines (IC50s = 1.6-6.1 μM) with no toxicity against NIH3T3 normal cell (IC50 >200 μM). The spectrometric studies exhibited that compound 6g binds to DNA strongly and may change DNA conformation significantly, presumably via a groove binding mechanism. Conclusion: The results of this study suggest that the prototype compound 6g can be considered as a novel lead compound for the design and discovery of novel anticancer agents.

The intravenous to oral switch of taxanes: strategies and current clinical developments

2020 ◽  
Author(s):  
Marit AC Vermunt ◽  
Andries M Bergman ◽  
Eric van der Putten ◽  
Jos H Beijnen
Keyword(s):  
Clinical Trials ◽  
Anticancer Agents ◽  
Hospital Care ◽  
Oral Treatment ◽  
Chemotherapy Treatment ◽  
Intravenous Treatment ◽  
Improve Cost Effectiveness ◽  
Oral Switch ◽  
Tumor Types ◽  
Improve Cost

The taxanes paclitaxel, docetaxel and cabazitaxel are important anticancer agents that are widely used as intravenous treatment for several solid tumor types. Switching from intravenous to oral treatment can be more convenient for patients, improve cost–effectiveness and reduce the demands of chemotherapy treatment on hospital care. However, oral treatment with taxanes is challenging because of pharmaceutical and pharmacological factors that lead to low oral bioavailability. This review summarizes the current clinical developments in oral taxane treatment. Intravenous parent drugs, strategies in the oral switch, individual agents in clinical trials, challenges and further perspectives on treatment with oral taxanes are subsequently discussed.

scholarly journals Predictive Pharmacokinetic-Pharmacodynamic Modeling of Tumor Growth Kinetics in Xenograft Models after Administration of Anticancer Agents

2004 ◽  
Vol 64 (3) ◽  
pp. 1094-1101 ◽  
Author(s):  
Monica Simeoni ◽  
Paolo Magni ◽  
Cristiano Cammia ◽  
Giuseppe De Nicolao ◽  
Valter Croci ◽  
...  
Keyword(s):  
Tumor Growth ◽  
Growth Kinetics ◽  
Anticancer Agents ◽  
Pharmacodynamic Modeling ◽  
Tumor Growth Kinetics ◽  
Xenograft Models

scholarly journals Gamma-radiated immunosuppressed tumor xenograft mice can be a new ideal model in cancer research

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Hamid Khodayari ◽  
Saeed Khodayari ◽  
Solmaz Khalighfard ◽  
Arash Tahmasebifar ◽  
Mahboubeh Tajaldini ◽  
...  
Keyword(s):  
Gamma Radiation ◽  
High Capacity ◽  
Xenograft Model ◽  
Tumor Xenograft ◽  
Whole Body ◽  
Cell Injection ◽  
Tumor Tissues ◽  
Post Radiation ◽  
Xenograft Models ◽  
Xenograft Mice

AbstractTumor xenograft models can create a high capacity to study human tumors and discover efficient therapeutic approaches. Here, we aimed to develop the gamma-radiated immunosuppressed (GIS) mice as a new kind of tumor xenograft model for biomedical studies. First, 144 mice were divided into the control and treated groups exposed by a medical Cobalt-60 apparatus in 3, 4, and 5 Gy based on the system outputs. Then, 144 BALB/c mice were divided into four groups; healthy, xenograft, radiation, and radiation + xenograft groups. The animals in the xenograft and radiation + xenograft groups have subcutaneously received 3 × 106 MCF-7 cells 24 h post-radiation. On 3, 7, 14, and 21 days after cell injection, the animals were sacrificed. Then, the blood samples and the spleen and tumor tissues were removed for the cellular and molecular analyses. The whole-body gamma radiation had a high immunosuppressive effect on the BALB/c mice from 1 to 21 days post-radiation. The macroscopic and histopathological observations have proved that the created clusters' tumor structure resulted in the xenograft breast tumor. There was a significant increase in tumor size after cell injection until the end of the study. Except for Treg, the spleen level of CD4, CD8, CD19, and Ly6G was significantly decreased in Xen + Rad compared to the Xen alone group on 3 and 7 days. Unlike IL-4 and IL-10, the spleen level of TGF-β, INF-γ, IL-12, and IL-17 was considerably decreased in the Xen + Rad than the Xen alone group on 3 and 7 days. The spleen expressions of the VEGF, Ki67, and Bax/Bcl-2 ratio were dramatically increased in the Xen + Rad group compared to the Xen alone on 3, 7, 14, and 21 days. Our results could confirm a new tumor xenograft model via an efficient immune-suppressive potential of the whole-body gamma radiation in mice.

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