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Unveiling the Power of Actinomycin D in Cancer Treatment and Research

Actinomycin D: An Overview of This Chemotherapy Antibiotic

The world of medicine is constantly evolving as new drugs are developed to cure diseases that were once considered fatal. One such drug that has been instrumental in the treatment of cancer is Actinomycin D.

This article provides an overview of Actinomycin D, covering its identification, history, synonyms, mechanism, chemical formula, properties, structure, and uses. This piece aims to educate readers on this powerful chemotherapy antibiotic.

Identification

Actinomycin D is also known as Dactinomycin and is classified under the ATC code L01DC01. Its CAS number is 50-76-0, and it has a molecular formula of C62H86N12O16.

Actinomycin D can be obtained from various sources, including Streptomyces bacteria. It can be identified through various resources such as PubChem, DrugBank, and ChemSpider.

History

Selman Waksman discovered Actinomycin D from Streptomyces parvallus in 1940. Merck Sharpe and Dohme (MSD) received FDA approval for the drug in 1964, and it has been in clinical use since then.

Synonyms

Actinomycin D has a complex chemical name of 2-Amino-4,6-dimethyl-3-oxo-3H-phenoxazine-1,9-dicarboxylic acid bis-[(5,12-diisopropyl-9,13,16-trimethyl-4,7,11,14,17-pentaoxo-hexadecahydro-10-oxa-3a,6,13,16-tetraaza-cyclopentacyclohexadecen-8-yl)-amide].

Mechanism

Actinomycin D has an intricate mechanism of action. It binds to specific areas of DNA called guanine-cytosine base pairs, resulting in the inhibition of transcription.

It also inhibits RNA polymerase and disrupts the formation of DNA duplexes during DNA replication. This interruption of DNA synthesis is what makes Actinomycin D an effective cancer-fighting drug.

Chemical Formula

Actinomycin D has a chemical formula of C62H86N12O16. Its molecular mass is 1255.44 g/mol.

Properties

Actinomycin D is a yellow to orange crystalline material that is water-insoluble. It has a melting point of 280-284C.

Structure

The molecular structure of Actinomycin D is quite complex. It has a phenoxazine ring, which is fused with a cyclohexadecadiene ring system.

The hydrocarbon chain is connected to the cyclohexadecadiene ring system via an amide linkage. Actinomycin D contains a polypeptide chain which is comprised of several amino acids.

Uses

Actinomycin D has several clinical and research uses. In the clinical setting, it is used as a chemotherapy medication to treat various cancers, including rhabdomyosarcoma, gestational trophoblastic neoplasia, and Wilms tumor.

Due to its ability to damage genetic material, Actinomycin D is often referred to as an anti-cancer antibiotic. It is usually administered intravenously under the brand name Cosmegen.

In the research setting, Actinomycin D is utilized to prevent RNA synthesis and study gene expression. It is also used to investigate the mechanisms of DNA replication.

In conclusion, Actinomycin D is a powerful broad-spectrum antibiotic that has revolutionized cancer treatment. With its complex mechanism of action, it inhibits DNA synthesis, hence halting the growth and multiplication of cancerous cells.

It has saved countless lives since its discovery and continues to be one of the most effective chemotherapy agents worldwide. Actinomycin D is not just a powerful chemotherapy medicationit has also found extensive use in the research industry, where it has been critical in understanding the underpinnings of many cellular processes.

This article sheds light on specific research applications of Actinomycin D, including its use as a fluorescent derivative, its role in flow cytometry and microscopy, and its contribution to apoptosis determination.

Fluorescent Derivative

One of the derivatives of Actinomycin D that has found significant use in research is 7-Aminoactinomycin D (7-AAD). This is a fluorescent derivative that is used in flow cytometry to distinguish viable cells from dead cells.

7-AAD stains DNA by intercalating into the double helix and binds more efficiently to damaged DNA, thus identifying dead cells in the population. The utilization of 7-AAD in flow cytometry helps researchers quickly assess cell viability in real-time.

The fluorescent property of 7-AAD also makes it useful in microscopy, where it can be used to visualize cells and their organelles.

Flow Cytometry and Microscopy

Actinomycin D is frequently utilized to assess the effects of anti-cancer drugs by analyzing DNA content. In DNA analysis, Actinomycin D inhibits the synthesis of RNA, resulting in cell cycle arrest in the G1 phase of the cell cycle.

The drug then intercalates into the DNA helix, which permits the detection of GC-rich DNA regions and DNA markers via flow cytometry. Researchers use this visualization to understand the mechanism of action of the drug and evaluate the impact of the drug on the cell cycle.

Actinomycin D is also used to investigate chromatin structure and dynamics. Researchers label the DNA fragments with Actinomycin D before analyzing chromatin behavior in real-time.

In addition to this, Actinomycin D can be used in microscopy to analyze chromatin reorganization and transcription site dynamics.

Apoptosis Determination

Actinomycin D plays a critical role in apoptosis determination. Apoptosis is an essential process that permits the self-destruction of abnormal cells, safeguarding the body against diseases like cancer.

During apoptosis, the DNA in cells forms single-stranded DNA (ssDNA) through nucleases. Actinomycin D is used to detect ssDNA formation, which is a hallmark for apoptosis determination.

The drug can also differentiate between live and dead cells by analyzing the intensity of DNA staining. Researchers demonstrate that live cells only incorporate low levels of Actinomycin D into the DNA while dead cells that incorporate high levels due to the permeable DNA membrane.

This differentiation process is important as it permits the accurate determination of cell death, allowing for the understanding of the effects of drugs and the mechanism of interaction between drugs and cells.

In Conclusion

In conclusion, Actinomycin D is not just a chemotherapy medication, but it is also a powerful tool in the research industry. It has many uses in research, including as a fluorescent derivative in flow cytometry and microscopy, in DNA analysis, and chromatin investigation.

The drug is also used in apoptosis determination, where it helps to distinguish between live and dead cells and enables the accurate measurement of cell viability. Actinomycin D has significantly contributed to the discovery of essential cellular processes and advancements in our understanding of the human body.

As such, it remains a valuable tool in scientific examination, and its use continues to expand as researchers discover new applications for this remarkable molecule. In summary, Actinomycin D is a versatile antibiotic that has made incredible contributions to cancer treatment and research.

Its clinical application as a chemotherapy medication has resulted in the successful treatment of many cancer patients. In research, Actinomycin D is critical in flow cytometry and microscopy, DNA analysis, and apoptosis determination.

The fluorescent and staining properties of Actinomycin D make it crucial in visualizing and understanding cellular processes.

FAQs:

Q: What is Actinomycin D?

A: Actinomycin D is a broad-spectrum chemotherapy antibiotic that has been instrumental in cancer treatment. Q: What is 7-AAD?

A: 7-Aminoactinomycin D is a fluorescent derivative of Actinomycin D that researchers use in flow cytometry to distinguish viable cells from dead cells. Q: How is Actinomycin D used in research?

A: Actinomycin D is used in flow cytometry and microscopy, DNA analysis, and apoptosis determination. Q: What is apoptosis?

A: Apoptosis is the process of programmed cell death, which is crucial in preventing the formation of abnormal cells that can lead to diseases like cancer. Q: Can Actinomycin D differentiate between live and dead cells?

A: Yes, Actinomycin D can differentiate between live and dead cells by analyzing the intensity of DNA staining. Q: What is the mechanism of action of Actinomycin D?

A: Actinomycin D inhibits the synthesis of RNA, resulting in cell cycle arrest in the G1 phase of the cell cycle. The drug then intercalates into the DNA helix, allowing for the detection of GC-rich DNA regions and DNA markers via flow cytometry.

Q: How has Actinomycin D contributed to cancer treatment and research? A: Actinomycin D has significantly contributed to the discovery of essential cellular processes and advancements in our understanding of the human body, making it a valuable tool in scientific examination.

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