Brazilein from Sappan Wood as a Beta-Lactamase Inhibitor
Journal name: The Malaysian Journal of Medical Sciences
Original article title: In Silico Study of the Potential of Brazilein Sappan Wood as a Beta-Lactamase Inhibitor against Extended-Spectrum Beta-Lactamase-Encoding Genes
The Malaysian Journal of Medical Sciences (MJMS) is a peer-reviewed, open-access journal published online at least six times a year. It covers all aspects of medical sciences and prioritizes high-quality research.
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Dwi Krihariyani, Evy Diah Woelansari, Edy Haryanto, Retno Sasongkowati, Anik Handayati, Sri Sulami Endah Astuti
The Malaysian Journal of Medical Sciences:
(A peer-reviewed, open-access journal)
Full text available for: In Silico Study of the Potential of Brazilein Sappan Wood as a Beta-Lactamase Inhibitor against Extended-Spectrum Beta-Lactamase-Encoding Genes
Year: 2024 | Doi: 10.21315/mjms2024.31.3.7
Copyright (license): CC BY 4.0
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Summary of article contents:
Introduction
Infectious diseases pose a significant public health challenge in Indonesia, exacerbated by the rising instances of multi-drug resistant (MDR) bacteria due to the prevalent practice of self-medication within communities. This burgeoning trend has underscored the urgent need for novel therapeutic interventions aimed at counteracting antibiotic resistance. In this context, sappan wood, derived from Caesalpinia sappan L., emerges as a promising candidate for combating enzyme-mediated resistance, specifically focusing on its potential to inhibit extended-spectrum beta-lactamase (ESBL) enzymes, encoded by the blaSHV, blaTEM, and blaCTX-M genes.
Brazilein's Beta-Lactamase Inhibitory Potential
The study evaluates brazilein, a major secondary metabolite found in sappan wood, comparing its inhibitory efficacy against established beta-lactamase inhibitors like clavulanic acid. Utilizing in silico docking techniques, the research demonstrated that brazilein exhibited significant binding stability with the target receptors responsible for the beta-lactamase activity associated with ESBL-producing bacteria. The binding energy values obtained indicated that brazilein, alongside established ligands, could effectively disrupt the enzymatic activity of the beta-lactamases being studied, specifically targeting the blaCTX-M gene. These findings advocate for the exploration of plant-derived compounds like brazilein as viable alternatives in the development of resistance-modifying treatments.
Conclusion
The investigation reveals the substantial capacity of brazilein from sappan wood to inhibit the beta-lactamase activity linked to multiple drug-resistance mechanisms. This suggests a promising avenue for the development of new, plant-based beta-lactamase inhibitors. Future research directions should include in vivo testing and thorough pharmacokinetic assessments to validate its therapeutic potential. By harnessing natural resources in the fight against antibiotic resistance, we may enhance treatment outcomes and reduce reliance on traditional synthetic antibiotics.
FAQ section (important questions/answers):
What was the objective of the study on sappan wood?
The study aimed to assess the potential of sappan wood as an inhibitor of extended-spectrum beta-lactamase (ESBL) enzymes linked to antibiotic resistance, specifically encoded by blaSHV, blaTEM, and blaCTX-M genes.
How did the researchers conduct the testing for beta-lactamase inhibitors?
Researchers conducted in silico testing using the Molegro Virtual Docker tool to simulate and predict the binding interactions of various compounds, including brazilein, with specific beta-lactamase enzymes to evaluate their inhibitory effects.
What were the primary findings regarding brazilein's effectiveness?
The findings revealed that brazilein had significant binding energy against beta-lactamase enzymes, demonstrating its potential to inhibit the activity of iiESBL, especially related to the blaCTX-M gene.
Why is combating antibiotic resistance particularly important in Indonesia?
Indonesia faces serious public health challenges from infectious diseases and antibiotic resistance due to widespread self-medication. Addressing this problem is crucial to preventing the development of multi-drug resistant bacteria.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Brazilein from Sappan Wood as a Beta-Lactamase Inhibitor�. 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) Beta:
Beta refers to beta-lactam antibiotics, a class of antibiotics that includes penicillins and cephalosporins. They are critical in treating bacterial infections. Resistance to these antibiotics, primarily through the action of beta-lactamases, poses significant health challenges, highlighting the need for effective inhibitors to combat multi-drug resistant microorganisms.
2) Table:
Tables in scientific literature serve as essential tools for presenting data systematically, allowing researchers to summarize complex information clearly. They facilitate comparisons and highlight key findings, such as binding energies and interactions among compounds, enabling readers to digest critical results at a glance and support conclusions drawn from studies.
3) Drug:
Drugs are chemical substances used to diagnose, treat, or prevent disease. In the context of antibiotic resistance, the development of new drugs, particularly those inhibiting beta-lactamase enzymes, is critical. Innovative drugs derived from natural sources, such as sappan wood, offer promise in combating resistant bacterial strains effectively.
4) Flavonoid:
Flavonoids are a diverse group of phytonutrients found in many plants, known for their antioxidant and anti-inflammatory properties. In this study, the flavonoid brazilein from sappan wood is investigated for its potential as a beta-lactamase inhibitor, showcasing natural compounds' therapeutic potential in addressing antibiotic resistance.
5) Activity:
Activity refers to the biological or pharmacological effects of a substance, such as its ability to inhibit enzymes like beta-lactamases. Assessing the activity of compounds is vital in drug discovery, particularly in determining their efficacy against resistant bacterial strains, thereby helping develop effective therapeutic strategies.
6) Antibiotic (Antibacterial):
Anti-bacterial compounds are essential for preventing or treating bacterial infections. The pursuit of anti-bacterial agents is crucial in an era of rising antibiotic resistance. Research focusing on natural anti-bacterial substances, like those from sappan wood, is vital for developing effective treatments against difficult-to-treat bacterial infections.
7) Study (Studying):
In research, a study encompasses systematic investigations aimed at answering specific scientific questions. This study focuses on the ability of brazilein, a compound in sappan wood, to inhibit beta-lactamase enzymes, contributing valuable insights into potential new treatments for antibiotic-resistant bacterial infections and advancing medicinal chemistry.
8) Knowledge:
Knowledge in the scientific context encompasses the information and understanding gained through research and experimentation. The knowledge obtained from studies on beta-lactamase inhibitors contributes to the scientific community's understanding of antibiotic resistance mechanisms and promotes the development of effective therapeutic strategies against resistant pathogens.
9) Rules:
Rules refer to the established guidelines or principles governing research methodologies, data interpretation, and ethical standards in scientific inquiry. Understanding rules is essential for conducting valid experiments, ensuring replicability and reliability of findings, and facilitating compliance with regulatory requirements in the development of new drugs.
10) Cina:
China is a significant contributor to global health and pharmaceutical research, particularly regarding infectious diseases and antibiotic resistance. The research landscape in China is expanding, with an emphasis on understanding microbial resistance patterns and developing novel antimicrobial agents, reflecting broader efforts to address global health challenges.
11) Substance:
Substances in this context relate to chemical compounds studied for their biological effects. The investigation of various substances, particularly plant-derived compounds like flavonoids, explores their potential as therapeutic agents, shedding light on natural alternatives in combatting antibiotic resistance and enhancing treatment options against resistant pathogens.
12) Relative:
Relative refers to the comparative analysis of data or substances in research. By assessing the relative effectiveness of compounds, such as various inhibitors against beta-lactamase, researchers can identify which substances may offer optimal therapeutic potential, guiding the development of new drugs to fight antibiotic-resistant infections.
13) Pharmacology:
Pharmacology is the study of drugs, their actions, interactions, and effects on biological systems. It plays a critical role in understanding how compounds like beta-lactamase inhibitors work against bacterial pathogens, informing drug development, therapeutic applications, and improving treatment outcomes through a deeper understanding of medicinal properties.
14) Medicine:
Medicine encompasses the science and practice of diagnosing, treating, and preventing disease. Advances in medicine, particularly in developing new antibiotics or inhibitors, are critical for addressing public health challenges posed by antibiotic-resistant bacteria, emphasizing the importance of innovative research in biotechnology and pharmaceuticals.
15) Mutation:
Mutations are changes in the DNA sequence of an organism that can lead to variations in traits. In the context of antibiotic resistance, mutations in bacterial genes can confer resistance to drugs, necessitating ongoing research to understand these changes and develop strategies for overcoming resistance in clinical settings.
16) Channel:
Channel in a pharmacological context often refers to biological pathways or structures through which substances, such as drugs, interact with cells. Understanding how drugs traverse these channels and influence cellular functions is essential for developing effective therapies, particularly in combating drug-resistant bacteria and enhancing treatment efficacy.
17) Rajput:
Rajput likely refers to a researcher or contributor involved in the study. Acknowledging researchers allows appreciation of their scientific contributions. Contributions from diverse experts enhance the research process, improving understanding of complex issues like antibiotic resistance and pushing forward the development of innovative solutions in healthcare.
18) Egypt:
Egypt is an important region for microbiological research and the study of antibiotic resistance, given its varying infection profiles and public health challenges. Research from Egypt contributes to the global understanding of resistance patterns and informs strategies to combat bacterial infections, fostering collaboration across scientific communities.
19) Patil:
Patil likely refers to an author or researcher whose work contributes to understanding antibiotic resistance mechanisms. Research affiliations enhance collaborations on complex health issues, emphasizing the value of diverse expertise in the quest to develop effective treatments and address pressing global health challenges related to infections and resistance.
20) Saha (Shaha):
Saha may refer to an author involved in the presented research, whose contributions play a vital role in advancing knowledge within pharmacology and antibiotic resistance studies. Involving various researchers emphasizes collaborative approaches in scientific inquiries, reflecting the interconnectedness of research efforts in tackling global health challenges.
21) Kara:
Kara refers to a researcher contributing to the study's findings, highlighting the collaborative efforts in addressing significant health challenges like antibiotic resistance. Recognizing each contributor's role fosters a deeper appreciation of the collective work needed to develop effective strategies for combating resistant bacterial infections.
22) Dari:
Dari might signify a researcher or an element within the study's authors or contributors. It emphasizes the collaborative nature of research in addressing health challenges, showcasing the importance of multidisciplinary approaches in tackling complex issues such as antibiotic resistance and the development of novel therapeutic options.
23) Vila:
Vila may refer to an author involved in antibiotic resistance research or pharmacological studies. Highlighting various researchers underlines the importance of diverse scientific perspectives in furthering our understanding of resistance mechanisms and developing innovative strategies to combat antibiotic-resistant pathogens in healthcare settings.
24) Pain:
Pain in a medical context pertains to the discomfort experienced by individuals, often prompting the need for effective treatment. Researching potential anti-inflammatory or analgesic properties of compounds, such as flavonoids, underscores the broader implications of these substances in enhancing patient care and managing symptoms associated with infections.
25) Inflammation:
Inflammation is a physiological response to infection or injury, often linked to pain and discomfort. Understanding the role of inflammation in infectious diseases is vital for developing therapies, including the use of anti-inflammatory compounds to mitigate inflammatory responses, thereby improving patient outcomes and enhancing the effectiveness of treatments.
26) Discussion:
Discussion sections in scientific papers analyze and interpret data, linking findings to existing research and theoretical frameworks. This critical component contextualizes the study's outcomes and elucidates their implications for future research, therapeutic applications, and public health strategies in addressing challenges such as antibiotic resistance.
27) Developing:
Developing refers to the process of creating or improving therapeutic agents through research and innovation. In combating antibiotic resistance, developing effective beta-lactamase inhibitors from natural sources is essential to enhance treatment options, reinvigorating the arsenal available to healthcare providers against resistant bacterial strains.
28) Science (Scientific):
Scientific refers to knowledge that is derived from systematic studies and experiments. The scientific method underpins research in pharmacology and medicine, ensuring accuracy and reliability in findings. This foundation is crucial for evolving our understanding of complex issues like antibiotic resistance and the development of effective countermeasures.
29) Toxicity:
Toxicity indicates the degree to which a substance can harm organisms. In drug development, assessing toxicity is vital to ensure safety and efficacy in therapeutic agents. Understanding the toxicity profiles of compounds, including natural inhibitors, is crucial for designing drugs that minimize side effects while combating resistant infections.
30) Disease:
Disease encompasses any deviation from normal function in the body, often causing discomfort or dysfunction. Researching ways to combat infectious diseases, particularly those caused by antibiotic-resistant bacteria, highlights the importance of innovative treatments and understanding disease mechanisms to improve public health outcomes.
31) Surface:
Surface in a pharmacological context often refers to the interaction between drugs and their biological targets. Understanding how drug molecules interact with protein surfaces, such as enzymes, is fundamental for optimizing binding and activity, crucial for developing effective inhibitors against mechanisms of antibiotic resistance.
32) Family:
Family in biological terms denotes a group of related organisms. In the context of this research, it could refer to families of bacteria that share resistance characteristics. Understanding the relationships among bacterial families aids in developing strategies to combat drug resistance on a broader scale.
33) Animal:
Animal testing often serves as a precursor to human clinical trials, providing valuable data on the efficacy and safety of new drugs. Research involving animal models is crucial for understanding underlying biological mechanisms and developing effective therapeutic strategies against diseases, particularly those caused by antibiotic-resistant pathogens.
34) Field:
Field denotes a specific area of study or professional practice. In scientific research, fields overlap, such as pharmacology, microbiology, and medicine, enhancing the potential for collaboration. Interdisciplinary knowledge is vital for addressing complex health issues like antibiotic resistance through comprehensive research approaches.
35) Fight:
Fight in a health context refers to the efforts made to combat diseases, infections, and antibiotic resistance. The ongoing fight against antibiotic resistance involves developing new compounds and strategies to ensure effective treatments for infections, reflecting a global challenge requiring collaborative efforts across research, healthcare, and policy sectors.
36) Pose:
Pose indicates the challenges or issues that arise in specific contexts. In discussing antibiotic resistance, the challenges posed by resistant bacteria highlight the urgency for novel solutions and strategies to mitigate the impact of sepsis and other infections, emphasizing the need for innovative research and collaboration.
37) Post:
Post refers to the dissemination or publication of research findings. Posting research results is crucial for sharing knowledge within the scientific community, fostering discussions, and enabling further advancements in understanding and addressing antibiotic resistance, ultimately contributing to the development of effective health interventions.
Other Science Concepts:
Discover the significance of concepts within the article: �Brazilein from Sappan Wood as a Beta-Lactamase Inhibitor�. Further sources in the context of Science might help you critically compare this page with similair documents:
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