Cytotoxicity study of some indole derivatives

| Posted in: Science

Journal name: World Journal of Pharmaceutical Research
Original article title: Cytotoxicity study of some indole derivatives
The WJPR includes peer-reviewed publications such as scientific research papers, reports, review articles, company news, thesis reports and case studies in areas of Biology, Pharmaceutical industries and Chemical technology while incorporating ancient fields of knowledge such combining Ayurveda with scientific data.
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Original source:

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Author:

Aswani Purandharan, Jithamol K.P., Sonu Jacob and Kavitha S.


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: Cytotoxicity study of some indole derivatives

Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research

Doi: 10.20959/wjpr202318-29928

Copyright (license): WJPR: All rights reserved


Download the PDF file of the original publication


Summary of article contents:

Introduction

The study conducted by Aswani Purandharan et al. focuses on the cytotoxicity of several synthesized indole derivatives, which are nitrogen-containing bicyclic heterocyclic compounds. These compounds are significant due to their presence in natural and synthetic alkaloids, showcasing various biological activities. Through the brine shrimp lethality bioassay, the researchers aimed to evaluate the cytotoxic effects of these indole derivatives, contributing to the understanding of their biological potential and chemical properties.

Synthesis and Cytotoxicity Testing

A total of seven indole derivatives were synthesized as part of the research. The synthesis involved combining aromatic amines and aromatic aldehydes in a controlled environment, which led to the formation of substituted indoles. The cytotoxicity was then evaluated using the brine shrimp lethality assay, where brine shrimp nauplii were exposed to different concentrations of the synthesized compounds. The percentage of mortality at varying concentrations provided insight into the cytotoxic effects of each derivative.

Biological Activity of Indole Derivatives

The preliminary results from the cytotoxicity study indicated that all synthesized indole derivatives exhibited varying degrees of cytotoxic effects on brine shrimp nauplii. The research highlighted the importance of structural modifications in influencing the biological activity of these compounds. The calculated IC50 values indicated that compounds like IBA4 demonstrated more potent cytotoxicity compared to others, while some derivatives showed moderate activity, enhancing the understanding of how structural changes can impact drug efficacy.

Additional Findings on Structure-Activity Relationship

The findings also emphasized a structure-activity relationship whereby certain substitutions on the indole derivatives, particularly halogen substitutions, resulted in increased cytotoxic activity. This correlation suggests that strategic modifications in molecular structures can significantly enhance the bioactivity of compounds, paving the way for the development of novel therapeutic agents with improved efficacy and safety profiles.

Conclusion

In summary, the research elucidates the potential of indole derivatives as cytotoxic agents and their importance in medicinal chemistry. The systematic approach taken in synthesizing these compounds and assessing their biological activity provides valuable insights into the design of new drugs. Future research should continue to explore the structural modifications of indole derivatives to create more effective therapeutic agents with targeted biological activities, as indicated by the promising results observed in this study.

FAQ section (important questions/answers):

What is the purpose of the cytotoxicity study conducted?

The study aimed to evaluate the cytotoxicity of synthesized indole derivatives using the brine shrimp lethality bioassay, assessing their potential biological activity.

Which method was used to determine cytotoxicity in this research?

Cytotoxicity was determined through brine shrimp lethality bioassay, measuring the survival rate of brine shrimp nauplii exposed to different concentrations of indole derivatives.

What are indole derivatives and why are they important?

Indole derivatives are nitrogen-containing heterocyclic compounds with significant biological activities, including antimicrobial and anticancer properties, making them valuable in medicinal chemistry.

How were the synthesized indole derivatives evaluated for efficacy?

Efficacy was evaluated by calculating IC50 values, indicating the concentration at which 50 percent of brine shrimp nauplii were killed, reflecting cytotoxicity.

What findings were observed regarding the compounds' cytotoxicity?

All synthesized indole derivatives displayed cytotoxic effects, with specific compounds like IBA4 showing enhanced toxicity compared to others in the study.

What significance does structural modification have on the compounds?

Structural modifications of the indole derivatives influenced their bioactivity, indicating that specific substitutions can lead to increased cytotoxicity and potential therapeutic use.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “Cytotoxicity study of some indole derivatives”. This list explains important keywords that occur in this article and links it to the glossary for a better understanding of that concept in the context of Ayurveda and other topics.

1) Toxicity:
Toxicity refers to the degree to which a substance can harm living organisms. In the context of the study, it is crucial to evaluate the cytotoxicity of indole derivatives against brine shrimp. The IC50 values obtained indicate the concentration required to achieve 50% mortality, helping to assess the safety and potential therapeutic use of the compounds.

2) Kerala:
Kerala is a state in southern India, known for its rich biodiversity and unique ecosystems. The study, conducted in Kerala, utilizes local resources for experimentation, emphasizing the significance of regional biodiversity. The research is part of an academic effort within the state’s pharmaceutical and chemical research community.

3) Study (Studying):
Studying refers to the act of learning or investigating a subject intensively. In the context of this research, studying involves the systematic exploration of indole derivatives and their biological properties. It is an integral part of the scientific process aimed at uncovering new knowledge crucial for advancements in pharmaceuticals.

4) Pharmacological:
Pharmacological pertains to the branch of medicine and biology concerned with the study of drug action. The research described looks into the pharmacological potential of synthesized indole derivatives, investigating their effects on living organisms, thereby contributing to the development of new therapeutic agents and enhancing understanding of their biological activities.

5) Science (Scientific):
Science is a systematic approach to acquiring knowledge through observation and experimentation. The research described utilizes scientific methods to analyze the cytotoxicity of synthesized indole derivatives, exemplifying the rigorous methodologies employed in modern scientific studies to derive meaningful conclusions and advance knowledge in the field.

6) Animal:
Animal in this research context specifically refers to the brine shrimp (Artemia Salina) used as a model organism in the cytotoxicity bioassay. Using a living organism in research facilitates understanding of drug effects and potential toxicity, simulating biological responses in higher organisms, crucial for pharmacological research.

7) Water:
Water is a vital component in life sciences and biological studies. In the research, brine shrimp are hatched in a saline solution, demonstrating the importance of water chemistry in maintaining suitable environments for biological assays. It also plays a crucial role in diluting compounds for testing cytotoxicity.

8) Activity:
Activity refers to the capacity of a substance to produce a biological effect. In this study, the term specifically relates to the cytotoxicity activity of indole derivatives, as assessed through their effects on brine shrimp. The findings highlight how structural modifications can influence biological activity.

9) Indigo:
Indigo is a natural dye derived from plants, historically significant in various cultures for its coloring properties. The historical context of indigo underpins the evolution of indole chemistry, demonstrating how early research on indigo has influenced current understanding and applications of various indole derivatives in medicinal chemistry.

10) Discussion:
Discussion in scientific research is the section where results are interpreted, implications are explored, and hypotheses are examined. In this study, the discussion would include interpretations of cytotoxicity findings, examining how various indole derivatives affect brine shrimp, and considering potential applications or future research directions based on results.

11) Salina (Shalina):
Salina refers to Artemia Salina, a species of brine shrimp utilized in the lethality bioassay for evaluating the cytotoxicity of synthesized compounds. Their resilient biological characteristics make them suitable test subjects for assessing the effects of various substances, thereby serving as a model in pharmacological studies.

12) Botany:
Botany is the scientific study of plants, emphasizing their structure, properties, and biochemical processes. While not the primary focus of this research, understanding botanical compounds and their properties can inform the synthesis of new derivatives and their potential applications in medicinal chemistry, linking plant sciences to drug discovery.

13) Glass:
Glass, in laboratory contexts, typically refers to the equipment used for experiments, such as beakers and flasks. In this study, glass apparatus would be employed for mixing chemicals, conducting assays, and observing reactions, ensuring precision and reliability in the methodology and results obtained from the cytotoxicity tests.

14) Table:
A table in research provides a systematic presentation of data, making it easier to analyze and interpret results. In this study, tables showcase the mortality rates of brine shrimp at different concentrations of indole derivatives, summarizing key findings and facilitating comparisons between the cytotoxic effects of various compounds.

15) Jacob:
Jacob refers to one of the authors of the study, Sonu Jacob, who contributes to the research in the field of Pharmaceutical Chemistry. The involvement of multiple researchers underscores the collaborative nature of scientific inquiry, facilitating diverse expertise and enhancing the quality of the study’s findings.

16) Sam (Sham):
Sham may refer to a control treatment in the context of biological assays. In this study, it is important for comparing results, as a sham treatment helps in determining the baseline activity and ruling out experimental biases. Control measures ensure that observed effects are due to the synthesized compounds.

17) Salt (Salty):
Salt is often used in biological studies, particularly in preparing saline solutions for aquatic organisms. Here, sodium chloride dissolved in water creates an optimal hatching environment for brine shrimp. The concentration of salt is critical for maintaining the health and viability of the test organisms in cytotoxicity assays.

18) Drug:
A drug is any substance used for medical treatment, alleviating symptoms or curing diseases. The study aims to explore the potential of synthesized indole derivatives as new drug candidates by evaluating their cytotoxicity, ultimately contributing to the discovery of safer and more effective therapeutic agents.

Other Science Concepts:

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Discover the significance of concepts within the article: ‘Cytotoxicity study of some indole derivatives’. Further sources in the context of Science might help you critically compare this page with similair documents:

Research article, Biological Activity, Brine shrimp lethality bioassay, IC50 value, Cytotoxicity study, Dimethyl sulphoxide, Dimethyl sulphoxide (DMSO).

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